Page last updated: 2024-11-11

heroin

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Description

Heroin: A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

heroin : A morphinane alkaloid that is morphine bearing two acetyl substituents on the O-3 and O-6 positions. As with other opioids, heroin is used as both an analgesic and a recreational drug. Frequent and regular administration is associated with tolerance and physical dependence, which may develop into addiction. Its use includes treatment for acute pain, such as in severe physical trauma, myocardial infarction, post-surgical pain, and chronic pain, including end-stage cancer and other terminal illnesses. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5462328
CHEMBL ID459324
CHEBI ID27808
SCHEMBL ID35150
MeSH IDM0006166

Synonyms (114)

Synonym
mexican brown [street name]
scag
crap [street name]
noise [street name]
scag [street name]
smack [street name]
unii-70d95007sx
horse [street name]
boy [street name]
hairy [street name]
persian brown [street name]
joy powder [street name]
white stuff [street name]
white junk [street name]
indian pink [street name]
harry [street name]
penang pink [street name]
malaysian pink [street name]
black tar [street name]
70d95007sx ,
rufus [street name]
17-methyl-7,8-didehydro-4,5alpha-epoxymorphinan-3,6alpha-diyl diacetate
CHEBI:27808 ,
dea no. 9200
einecs 209-217-7
D07286
diamorphine (ban)
smack
white junk
diasetylmorfiimi
junk
diasetilmorfin
BOY ,
(5alpha,6alpha)-7,8-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol diacetate (ester)
aspron
morphinan-3,6-diol, 7,8-didehydro-4,5-epoxy-17-methyl-, diacetate (ester), (5alpha,6alpha)-
dooje
o,o'-diacetylmorphine
morphacetin
rufus
harry
persian
crap
black tar
amsterdam marble
diazetylmorphine
diaphorm
7,8-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol diacetate (ester)
mexican brown
morphinan-3,6-alpha-diol, 7,8-didehydro-4,5-alpha-epoxy-17-methyl-, diacetate (ester)
eclorion
heroiin
hsdb 6473
scot
diamorfina
persian brown
herolan
joy powder
3,6-o-diacetylmorphine
morphine diacetate
hairy
morphinan-3,6-diol, 7,8-didehydro-4,5-epoxy-17-methyl-, (5alpha,6alpha)-, diacetate (ester)
diacetylmorfin
tnt (narcotic)
acetomorphine
stuff
dujie
white stuff
7,8-dihydro-4,5-alpha-epoxy-17-methylmorphinan-3,6-alpha-diol diacetate
indian pink
preza
iroini
penang pink
malaysian pink
acetomorphin
diacetyl morphine
acetomorfine
diasetielmorfien
3,6-diacetylmorphine
eroina
diacephin
heroien
diacetylmorphine
561-27-3
heroin
C06534
diamorphine
DB01452
NCGC00168253-01
j6.494g ,
ids-nh-001
ids-nh-001(sect.3)
CHEMBL459324
tox21_112612
dtxsid6046761 ,
cas-561-27-3
dtxcid4026761
heroin [hsdb]
diamorphine [who-dd]
diacetylmorphine [mi]
(5.alpha.,6.alpha.)-7,8-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol diacetate (ester)
diamorphine-
SCHEMBL35150
gtpl9082
[(4r,4ar,7s,7ar,12bs)-9-acetyloxy-3-methyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-yl] acetate
heroin, analytical standard, >=98% (hplc)
heroin (diacetylmorphine) 1.0 mg/ml in acetonitrile
heroin (diacetylmorphine)
diacetylmorphine (heroin)
3,6-diacetylmorphine (heroin)
Q60168
[(4r,4ar,7s,7ar,12bs)-9-acetyloxy-3-methyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl] acetate
heroin (3,6-diacetylmorphine), 1mg/ml in acetonitrile
heroin (3,6-diacetylmorphine)

Research Excerpts

Overview

Heroin is a semi-synthetic opioid that is commonly abused drugs in the world. Heroin inhalation is a common practice and can lead to leukoencephalopathy,. Heroin itself is a prodrug and is converted to the most active metabolite 6-monoacetylmorphine.

ExcerptReferenceRelevance
"Heroin overdose is a leading cause of mortality among drug users. "( Fatal and Non-Fatal Heroin-Related Overdoses: Circumstances and Patterns.
Beisel, L; Niethammer, R; Richter, C; Schneider, S, 2021
)
2.39
"Heroin is a semi-synthetic opioid that is commonly abused drugs in the world. "( Determination of metabolic phenotype and potential biomarkers in the liver of heroin addicted mice with hepatotoxicity.
Cao, H; Kuang, H; Li, J; Li, L; Wang, Q; Zhao, H; Zhou, Z, 2021
)
2.29
"Heroin is a highly addictive drug that causes axonal damage. "( Heroin Addiction Induces Axonal Transport Dysfunction in the Brain Detected by In Vivo MRI.
Bao, S; Chen, L; Deng, A; Ke, T; Li, Q; Liao, C; Luo, Y; Yang, J; Zhang, Y, 2022
)
3.61
"Heroin is an opioid agonist commonly abused for its rewarding effects. "( Heroin and its metabolites: relevance to heroin use disorder.
Badiani, A; Barra, M; Caprioli, D; D'Ottavio, G; De Pirro, S; Milella, MS, 2023
)
3.8
"Heroin (diamorphine) is a highly addictive opioid drug synthesized from morphine. "( The influence of carboxylesterase 1 polymorphism and cannabidiol on the hepatic metabolism of heroin.
Gilliland, TK; Markowitz, JS; Qian, Y, 2020
)
2.22
"Heroin addiction is a chronic relapsing brain disorder with negative social consequences. "( Histone 3 lysine 9 acetylation of BRG1 in the medial prefrontal cortex is associated with heroin self‑administration in rats.
Hong, Q; Lai, M; Lin, Z; Liu, H; Liu, J; Xu, W; Xu, Z; Zhou, W; Zhu, H; Zhuang, D, 2020
)
2.22
"As heroin is a chiral compound with five stereogenic centres, the methods of chiroptical spectroscopy supplemented by density functional theory (DFT) calculations were applied to study its conformations in chloroform solution."( Structure of heroin in a solution revealed by chiroptical spectroscopy.
Fagan, P; Králík, F; Kuchař, M; Setnička, V, 2020
)
1.44
"Heroin dependence is a complex disease with multiple phenotypes. "( Association studies of dopamine synthesis and metabolism genes with multiple phenotypes of heroin dependence.
Chen, Y; Lai, J; Li, Y; Shi, X; Wei, S; Zhang, J; Zhu, Y, 2020
)
2.22
"Heroin inhalation is a common practice and can lead to leukoencephalopathy."( "Chasing the Dragon": A Fatal Case Report of Toxic Leucoencéphalopathie Due to Inhaled Heroin.
Carvajal-Guevara, JD; Coral-Leiton, AM; Gutiérrez-Sanjuán, ÓI; Gutiérrez-Segura, JC; Ochoa-Orozco, SA; Trejos-Orozco, EA,
)
1.08
"Heroin itself is a prodrug and is converted to the most active metabolite 6-monoacetylmorphine (6-MAM) responsible for the acute toxicity of heroin and then to a relatively less-active metabolite morphine responsible for the long-term toxicity of heroin."( Systematic Structure-Based Virtual Screening Approach to Antibody Selection and Design of a Humanized Antibody against Multiple Addictive Opioids without Affecting Treatment Agents Naloxone and Naltrexone.
Jin, Z; Kim, K; Zhan, CG; Zhang, CH; Zheng, F, 2021
)
1.34
"Heroin use disorder is a chronic relapsing brain disease containing multiple phenotypes. "( Association study of Catechol-o-methyltransferase and Alpha-1-adrenergic receptor gene polymorphisms with multiple phenotypes of heroin use disorder.
Chen, Y; Deji, C; Lai, J; Li, Y; Wei, S, 2021
)
2.27
"Heroin is a highly abused opioid and incurs a significant detriment to society worldwide. "( Development of a Clinically Viable Heroin Vaccine.
Banks, ML; Bremer, PT; Janda, KD; Poklis, JL; Schlosburg, JE; Steele, FF; Zhou, B, 2017
)
2.17
"Heroin is a growing national crisis in America. "( Blocking drug activation as a therapeutic strategy to attenuate acute toxicity and physiological effects of heroin.
Kim, K; Zhan, CG; Zhang, T; Zheng, F; Zheng, X, 2018
)
2.14
"Heroin is a highly abused opioid that has reached epidemic status within the United States. "( Heat shock proteins: A dual carrier-adjuvant for an anti-drug vaccine against heroin.
Ellis, B; Hwang, CS; Janda, KD; Zhou, B, 2019
)
2.18
"Heroin abuse is a serious problem that endangers human health and affects social stability. "( Comparison of the Detection Windows of Heroin Metabolites in Human Urine Using Online SPE and LC-MS/MS: Importance of Morphine-3-Glucuronide.
Liang, C; Ni, C; Shen, H; Sheng, Z; Wang, L; Wang, R; Zhang, Y, 2020
)
2.27
"Heroin dependence is a chronic relapsing brain disorder, characterized by the compulsion to seek and use heroin. "( Reduction in cerebral perfusion after heroin administration: a resting state arterial spin labeling study.
Borgwardt, S; Denier, N; Gerber, H; Klarhöfer, M; Lang, UE; Riecher-Rossler, A; Vogel, M; Walter, M; Wiesbeck, GA, 2013
)
2.1
"Heroin abuse is a significant public health issue and is on the rise because of the unintended consequences of strengthening controls for nonmedical use of prescription pain killers. "( Detection of codeine, morphine, 6-monoacetylmorphine, and meconin in human umbilical cord tissue: method validation and evidence of in utero heroin exposure.
Jones, B; Jones, JT; Jones, M; Lewis, D; Plate, C; Sulaiman, K, 2015
)
2.06
"Heroin addiction is a disease of chronic relapse affecting over half of its users. "( Greater avoidance of a heroin-paired taste cue is associated with greater escalation of heroin self-administration in rats.
Grigson, PS; Imperio, CG, 2015
)
2.17
"Heroin addiction is a severe relapsing brain disorder associated with impaired cognitive control, including deficits in attention allocation. "( Abnormal functional integration of thalamic low frequency oscillation in the BOLD signal after acute heroin treatment.
Borgwardt, S; Denier, N; Gerber, H; Huber, CG; Lang, UE; Radue, EW; Riecher-Rossler, A; Schmidt, A; Vogel, M; Walter, M; Wiesbeck, GA, 2015
)
2.08
"Heroin addiction is a disease of chronic relapse that harms the individual through devaluation of personal responsibilities in favor of finding and using drugs. "( Assessment of individual differences in the rat nucleus accumbens transcriptome following taste-heroin extended access.
Colechio, EM; Freeman, WM; Grigson, PS; Imperio, CG; Masser, DR; McFalls, AJ; Vrana, KE, 2016
)
2.1
"Heroin addiction is a chronic, relapsing brain disease. "( Variants of opioid system genes are associated with non-dependent opioid use and heroin dependence.
Blanken, P; Butelman, ER; da Rosa, JC; Kreek, MJ; Levran, O; Ott, J; Randesi, M; van den Brink, W; van Ree, JM; Yuferov, V, 2016
)
2.1
"Heroin addiction is a chronic relapsing disease, best treated with opioid-agonist substitution therapy such as methadone maintenance. "( Scientific and political challenges in North America's first randomized controlled trial of heroin-assisted treatment for severe heroin addiction: rationale and design of the NAOMI study.
Anis, A; Brissette, S; Gartry, C; Guh, D; Krausz, M; Marsh, DC; Nosyk, B; Oviedo-Joekes, E; Schechter, MT, 2009
)
2.02
"Heroin is an illicit narcotic abused by millions of people worldwide. "( The influence of heroin abuse on glutathione-dependent enzymes in human brain.
Barańczyk-Kuźma, A; Gutowicz, M; Kaźmierczak, B, 2011
)
2.15
"Heroin craving is a trigger for relapse and dropping out of treatment. "( Heroin anticraving medications: a systematic review.
Amar, R; Casarella, J; Drexler, K; Fareed, A; Vayalapalli, S, 2010
)
3.25
"Heroin addiction is a wide-reaching problem with a spectrum of damaging social consequences. "( A vaccine strategy that induces protective immunity against heroin.
Edwards, S; Janda, KD; Koob, GF; Mayorov, AV; Misra, KK; Schlosburg, JE; Schulteis, G; Stowe, GN; Vendruscolo, LF; Zakhari, JS, 2011
)
2.05
"Heroin addiction is a wide-reaching problem with a spectrum of damaging social consequences. "( Developing a vaccine against multiple psychoactive targets: a case study of heroin.
Edwards, S; Janda, KD; Koob, GF; Misra, KK; Schlosburg, JE; Schulteis, G; Stowe, GN; Vendruscolo, LF; Zakhari, JS, 2011
)
2.04
"Heroin dependence is a chronic relapsing disorder characterized by the compulsion to seek and use heroin. "( The impact of diacetylmorphine on hypothalamic-pituitary-adrenal axis activity and heroin craving in heroin dependence.
Borgwardt, SJ; Gerber, H; Gerhard, U; Joechle, W; Riecher-Rössler, A; Schmid, O; Walter, M; Wiesbeck, GA, 2012
)
2.05
"Heroin is an illicit, highly addictive drug. "( [Heroin addiction].
Hosztafi, S, 2011
)
2.72
"Heroin is a highly addictive drug, and heroin abuse is considered to be a serious criminal act. "( Distinguishing heroin abuse from codeine administration in the urine of Chinese people by UPLC-MS-MS.
Bu, J; Huang, Y; Shen, B; Zhan, C; Zhuo, X, 2013
)
2.19
"Heroin is a semi-synthetic morphine derivative. "( [Heroin: a useful analgesic?].
Furunes, H; Slørdal, L; Spigset, O, 2003
)
2.67
"Heroin overdose is a serious consequence of heroin use and one of the leading causes of premature death and illness in Australia. "( Transient changes in behaviour lead to heroin overdose: results from a case-crossover study of non-fatal overdose.
Bammer, G; Dietze, P; Fry, C; Jolley, D, 2005
)
2.04
"Heroin is a suitable alternative to morphine (particularly for intramuscular administration) if differences in milligram potency are taken into account, but has no advantages in terms of either analgesic efficacy or side effects."( Oral morphine in chronic cancer pain.
Walsh, TD, 1984
)
0.99
"Heroin acts as a pro-drug that allows rapid and complete central nervous system absorption; this accounts for the drug's euphoric and toxic effects."( Acute heroin overdose.
Sporer, KA, 1999
)
1.51
"Heroin abuse is a major social and public health problem in many parts of the world, yet relatively little is known about its etiology. "( Association analysis of polymorphisms in the DRD4 gene and heroin abuse in Chinese subjects.
Collier, DA; Hu, X; Li, T; Liu, X; Sham, PC; Zhao, J; Zhu, ZH, 2000
)
1.99
"Heroin overdose is a major cause of death among heroin users, and often occurs in the company of other users. "( Should we conduct a trial of distributing naloxone to heroin users for peer administration to prevent fatal overdose?
Hargreaves, KM; Lenton, SR, 2000
)
2
"Heroin abuse is an increasing problem in Australia. "( Heroin overdose and myoglobinuric acute renal failure.
Atkins, RC; Becker, GJ; Isbel, NM; McMahon, LP; Rice, EK, 2000
)
3.19

Effects

Heroin has a half-life of 2-6min and is metabolized too quickly to be detected in autopsy samples. Heroin itself has a strong potential to produce subjective experiences characterized by intense euphoria, relaxation and release from craving.

Heroin abuse has increased substantially during the past decade in the United States. Heroin has a half-life of 2-6min and is metabolized too quickly to be detected in autopsy samples. To the west, Mexican-sourced "black tar" (BTH) is the main heroin available.

ExcerptReferenceRelevance
"Heroin itself has a strong potential to produce subjective experiences characterized by intense euphoria, relaxation and release from craving."( Reduction in cerebral perfusion after heroin administration: a resting state arterial spin labeling study.
Borgwardt, S; Denier, N; Gerber, H; Klarhöfer, M; Lang, UE; Riecher-Rossler, A; Vogel, M; Walter, M; Wiesbeck, GA, 2013
)
1.38
"Heroin has a half-life of 2-6 min and is metabolized too quickly to be detected in autopsy samples. "( Identifying cases of heroin toxicity where 6-acetylmorphine (6-AM) is not detected by toxicological analyses.
Davis, GG; Dye, DW; Ellis, AD; McGwin, G, 2016
)
2.2
"The heroin epidemic has existed for decades, but a sharp rise in opioid overdose deaths (OODs) jolted the nation in the mid-twenty-teens and continues as a major health crisis to this day. "( The Opioid Epidemic: a Crisis Disproportionately Impacting Black Americans and Urban Communities.
Abijo, T; Gondré-Lewis, MC; Gondré-Lewis, TA, 2023
)
1.47
"Heroin use has increased from 6 per 10,000 women in 2004-05 to 18 per 10,000 women in 2016-17 (Average percent change = 20.8; 95% 11.2, 31.2)."( Trends in heroin use among women of reproductive age in the United States, 2004-2017.
Alshaarawy, O; Parker, MA; Vanderziel, A, 2020
)
1.68
"Heroin itself has a strong potential to produce subjective experiences characterized by intense euphoria, relaxation and release from craving."( Reduction in cerebral perfusion after heroin administration: a resting state arterial spin labeling study.
Borgwardt, S; Denier, N; Gerber, H; Klarhöfer, M; Lang, UE; Riecher-Rossler, A; Vogel, M; Walter, M; Wiesbeck, GA, 2013
)
1.38
"Heroin abuse has increased substantially during the past decade in the United States. "( Trends and characteristics of heroin overdoses in Wisconsin, 2003-2012.
Meiman, J; Paulozzi, L; Tomasallo, C, 2015
)
2.15
"Heroin has a half-life of 2-6 min and is metabolized too quickly to be detected in autopsy samples. "( Identifying cases of heroin toxicity where 6-acetylmorphine (6-AM) is not detected by toxicological analyses.
Davis, GG; Dye, DW; Ellis, AD; McGwin, G, 2016
)
2.2
"heroin consumers have been divided from the full range of available products: east of the Mississippi River, Colombian-sourced powder heroin (PH) dominates the market while, to the west, Mexican-sourced "black tar" (BTH) is the main heroin available."( The Textures of Heroin: User Perspectives on "Black Tar" and Powder Heroin in Two U.S. Cities.
Bourgois, P; Ciccarone, D; Karandinos, G; Mars, SG; Montero, F,
)
1.2
"Heroin use in the US has exploded in recent years, and heroin overdoses requiring naloxone are very common. "( Do heroin overdose patients require observation after receiving naloxone?
Liss, DB; Mullins, ME; Schwarz, ES; Willman, MW, 2017
)
2.52
"Heroin body packing has clearly defined diagnostic features that can be seen with CT. "( Heroin body packing: clearly discerning drug packets using CT.
Feng, J; Lai, SS; Li, L; Lin, BQ; Xu, YK; Yang, RM; Ye, XH; Yu, T, 2009
)
3.24
"Heroin users have been advised of the risk."( An outbreak of infection with Bacillus anthracis in injecting drug users in Scotland.
Ahmed, S; Brooks, T; Browning, LM; Hawkins, G; Hood, J; Penrice, G; Ramsay, CN; Smith, J; Stirling, A, 2010
)
1.08
"Heroin has been shown to cause spongiform leukoencephalopathy (SLE) in heroin addicts. "( Activation of caspase-3 and c-Jun NH2-terminal kinase signaling pathways involving heroin-induced neuronal apoptosis.
Cao, Q; Jing, H; Lai, B; Liu, X; Pu, H, 2011
)
2.04
"Heroin use has seriously threatened public heath in many countries, but the existing therapies continue to have many limitations. "( A morphine/heroin vaccine with new hapten design attenuates behavioral effects in rats.
Li, QQ; Lu, L; Luo, YX; Shi, HS; Shi, J; Sun, CY; Xue, YX; Zhai, HF; Zhu, WL, 2011
)
2.2
"Heroin has been hypothesized to activate opiate receptors and inhibit gamma-aminobutyric acid (GABA) release from inhibitory GABAergic interneurons which, in turn, activates dopamine projection cells. "( GABAergic mechanisms of heroin-induced brain activation assessed with functional MRI.
Li, SJ; Stein, EA; Wu, G; Xi, ZX, 2002
)
2.06
"Heroin use has been associated with increased impulsive behaviour. "( Impulse control differences between abstinent heroin users and matched controls.
Lee, TM; Pau, CW, 2002
)
2.02
"Heroin has been prescribed in England for almost a hundred years, and the "British system" was once the subject of international curiosity."( Prescribing heroin.
Carnwath, T,
)
1.23
"Heroin purity in NSW has remained low, with perhaps a 10% increase above the lowest recorded levels."( Documenting the heroin shortage in New South Wales.
Day, C; Degenhardt, L; Hall, W, 2006
)
1.4
"Heroin has been shown to elevate dopamine (DA) level. "( Heroin-administered mice involved in oxidative stress and exogenous antioxidant-alleviated withdrawal syndrome.
Li, B; Li, G; Lin, H; Wang, Z; Xu, B; Zheng, Q; Zheng, R, 2006
)
3.22
"Heroin has no apparent unique advantages or disadvantages for the relief pain in patients with cancer."( Analgesic and mood effects of heroin and morphine in cancer patients with postoperative pain.
Grabinski, PY; Houde, RW; Kaiko, RF; Rogers, AG; Wallenstein, SL, 1981
)
1.27
"Heroin abuse has been a long-standing problem in the United States, especially in New York City, which is a major heroin trafficking center and home to the largest population of heroin addicts in the country. "( An overview of heroin trends in New York City: past, present and future.
Frank, B,
)
1.93
"Heroin has characteristic subjective effects that contribute importantly to its widespread abuse. "( Discriminative stimulus effects of intravenous heroin and its metabolites in rhesus monkeys: opioid and dopaminergic mechanisms.
Platt, DM; Rowlett, JK; Spealman, RD, 2001
)
2.01

Actions

Heroin use can cause respiratory complications including asthma, chronic obstructive pulmonary disease (COPD) and bronchiectasis (BD) Heroin exposure can cause various complications like seizures, stroke, spongiform encephalopathy, transverse myelopathy, plexopathy, compartment syndrome, rhabdomyolysis and renal failure. Heroin could be a cause more common than thought of leukoencephalopathy.

ExcerptReferenceRelevance
"Heroin use can cause respiratory complications including asthma, chronic obstructive pulmonary disease (COPD) and bronchiectasis (BD)."( [Bronchial diseases and heroin use. A systematic review].
Brousse, G; Jaafari, N; Peiffer, G; Perriot, J; Underner, M,
)
1.88
"The heroin-associated increase in fALFF was mainly dominated by slow-4 (0.027-0.073 Hz) oscillations."( Abnormal functional integration of thalamic low frequency oscillation in the BOLD signal after acute heroin treatment.
Borgwardt, S; Denier, N; Gerber, H; Huber, CG; Lang, UE; Radue, EW; Riecher-Rossler, A; Schmidt, A; Vogel, M; Walter, M; Wiesbeck, GA, 2015
)
1.11
"The heroin-evoked increase in premature responses is mimicked by a D1 agonist and prevented by a D1 antagonist or genetic ablation of the D1 receptor gene."( Dopamine D1 and D3 Receptors Modulate Heroin-Induced Cognitive Impairment through Opponent Actions in Mice.
Lai, J; Li, Y; Qiao, X; Wang, Y; Wei, S; Yan, P; Yin, F; Zhang, H; Zhu, Y, 2017
)
1.21
"Heroin addiction may increase the risk of pulmonary involvement. "( Life-threatening asthma after heroin inhalation. A case report and a review of the literature.
Chetta, A; Elia, D; Marinou, A, 2010
)
2.09
"Heroin could be a cause more common than thought of leukoencephalopathy. "( [Toxic leucoencephalopathy after use of sniffed heroin, an unrecognized form of beneficial evolution].
Cotton, F; Drouet, A; Felten, D; Guilloton, L; Havé, L; Lamboley, JL; Quesnel, L; St-Pierre, G, 2012
)
2.08
"Heroin exposure can cause various complications like seizures, stroke, spongiform encephalopathy, transverse myelopathy, plexopathy, compartment syndrome, rhabdomyolysis and renal failure due to various mechanisms. "( Rhabdomyolysis, acute kidney injury and transverse myelitis due to naive heroin exposure.
Agarwal, SK; Gupta, A; Khaira, A; Lata, S; Tiwari, SC, 2011
)
2.04
"Heroin can inhibit the immunofunction especially the celluar immunity of the teenager heroin addicts. "( [Changes of the immune cells, cytokines and growth hormone in teenager drug addicts].
He, WY; Hua, C; Kuang, Y; Kuang, YM; Sun, Y; Zhu, YC, 2007
)
1.78
"This heroin-induced increase in cocaine's reinforcing potency may be a contributing factor to abuse of cocaine and heroin combinations (i.e., "speedballs") in humans."( Self-administration of cocaine and heroin combinations by rhesus monkeys responding under a progressive-ratio schedule.
Rowlett, JK; Woolverton, WL, 1997
)
1.03
"Heroin can cause fatal respiratory insufficiency, and in 1996 a total of 104 deaths related to heroin overdoses were reported in Oslo."( [Prehospital treatment of heroin intoxication in Oslo in 1996].
Hansen, TB; Nilsen, JE; Stokland, O, 1998
)
1.32
"The heroin injectors had lower educational status, spent less money on day-to-day heroin usage, but had longer drug-using careers than the heroin smokers. "( Characteristics of hospitalized heroin smokers and heroin injectors in Taiwan.
Chen, CK; Lin, SK; Su, LW, 1999
)
1.15

Treatment

Heroin-assisted treatment comprises the use of diacetylmorphine (pharmaceutical heroin) for individuals with severe opioid use disorder. Heroin Assisted Treatment (HAT) is an alternative treatment modality for people for whom more traditional forms of opioid substitution therapy, such as methadone, have been ineffective.

ExcerptReferenceRelevance
"Heroin-assisted treatment comprises the use of diacetylmorphine (pharmaceutical heroin) for individuals with severe opioid use disorder. "( Experiences with take-home dosing in heroin-assisted treatment in Switzerland during the COVID-19 pandemic-Is an update of legal restrictions warranted?
Dürsteler, KM; Köck, P; Meyer, M; Strasser, J; Vogel, M; Walter, M, 2022
)
2.44
"Heroin-assisted treatment has proven effective in reducing criminal offenses in opioid dependent individuals. "( Exploring why patients in heroin-assisted treatment are getting incarcerated-a qualitative study.
Dürsteler, KM; Lang, UE; Meyer, M; Rist, B; Strasser, J; Vogel, M; Walter, M, 2022
)
2.46
"Heroin-treated animals exhibited anxiety-like behavior when tested in the elevated plus-maze, showed blunted heroin-induced analgesia, but exhibited no effect on naloxone-induced hyperalgesia."( The long-term effects of repeated heroin vapor inhalation during adolescence on measures of nociception and anxiety-like behavior in adult Wistar rats.
Creehan, KM; Gutierrez, A; Harvey, EL; Taffe, MA, 2022
)
1.72
"Heroin-assisted treatment (HAT) is effective for individuals with severe opioid use disorder (OUD) who do not respond sufficiently to other opioid agonist treatments. "( Safety and feasibility of intranasal heroin-assisted treatment: 4-week preliminary findings from a Swiss multicentre observational study.
Baumgartner, S; Beck, T; Binder, H; Bröer, R; Devaud, N; Dürsteler, KM; Falcato, L; Kormann, A; Krausz, RM; Kurmann, M; Meyer, M; Salim Hassan Fadlelseed, R; Sanwald, U; Simon, O; Strasser, J; Vogel, M; Westenberg, JN, 2023
)
2.63
"Heroin-assisted treatment (HAT) is a proven effective treatment option for individuals with severe opioid use disorder (OUD). "( Feasibility, safety, and acceptability of intranasal heroin-assisted treatment in Switzerland: protocol for a prospective multicentre observational cohort study.
Dürsteler, KM; Falcato, L; Krausz, M; Meyer, M; Strasser, J; Vogel, M; Westenberg, JN, 2023
)
2.6
"Heroin Assisted Treatment (HAT) is an alternative treatment modality for people for whom more traditional forms of opioid substitution therapy, such as methadone, have been ineffective."( More than just 'free heroin': Caring whilst navigating constraint in the delivery of diamorphine assisted treatment.
Ahmed, D; Harris, M; Moore, HJ; Poulter, HL; Riley, F; Towl, G; Walker, T, 2023
)
1.95
"Heroin-Assisted Treatment (HAT) is well evidenced internationally to improve health and social outcomes for people dependent on opioids who have not been helped by traditional treatment options. "( 'This is hardcore': a qualitative study exploring service users' experiences of Heroin-Assisted Treatment (HAT) in Middlesbrough, England.
Ahmed, D; Harris, M; Moore, HJ; Poulter, HL; Riley, F; Towl, G; Walker, T, 2023
)
2.58
"Heroin-assisted treatment (HAT) involves supervised dispensing of medical heroin (diacetylmorphine) for people with opioid use disorder. "( Patients' satisfaction with heroin-assisted treatment: a qualitative study.
Arnevik, EA; Ellefsen, R; Wüsthoff, LEC, 2023
)
2.65
"Heroin-related treatment demand dropped, as did heroin-related mortality."( Changes in patterns of injecting drug use in Hungary: a shift to synthetic cathinones.
Csesztregi, T; Horváth, GC; Nyírády, A; Péterfi, A; Tarján, A,
)
0.85
"Heroin-assisted treatment (HAT) can improve the condition of heroin addicts still using street heroin after a methadone treatment. "( Efficacy of Heroin-assisted Treatment In Belgium: A Randomised Controlled Trial.
Ansseau, M; Charlier, C; De Roubaix, J; Deblire, C; Demaret, I; Dubois, N; Lemaître, A; Litran, G; Magoga, C; Quertemont, E, 2015
)
2.24
"And, heroin-assisted treatment was associated with better retention than methadone among treatment-refractory patients."( Retention in medication-assisted treatment for opiate dependence: A systematic review.
Cucciare, MA; Garrison-Diehn, C; Schultz, NR; Timko, C; Vittorio, L, 2016
)
0.89
"If a heroin user is treated in the ED, how long must the patient stay under observation before being safe for discharge? Five articles addressing the duration of ED observation required for patients treated with naloxone for opioid overdoses."( Do heroin overdose patients require observation after receiving naloxone?
Liss, DB; Mullins, ME; Schwarz, ES; Willman, MW, 2017
)
1.53
"Heroin treatment caused cellular necrosis as revealed by the fragmentation of cytoplasmic materials in follicular epithelial cells of the gland."( Effects of sub-lethal heroin administration on thyroid stimulating hormone (TSH), thyroid hormones (T3, T4) and thyroid gland of Mus norvegicus.
Bhoir, KK; Pandey, AK; Suryawanshi, SA, 2009
)
1.39
"Heroin-treated animals exhibited significant progressive increases in locomotor activity."( Impulsive choice, as measured in a delay discounting paradigm, remains stable after chronic heroin administration.
Halperin, JM; Harty, SC; Ranaldi, R; Whaley, JE, 2011
)
1.31
"Heroin-assisted treatment (HAT) is a solution for improving the condition of treatment-resistant heroin addicts. "( Staff concerns in heroin-assisted treatment centres.
Ansseau, M; Demaret, I; Lemaître, A, 2012
)
2.16
"Heroin-assisted treatment is a long-term effective treatment for severely dependent opiate addicts with respect to stabilization of health, reduction of illegal drug use and improvement of social integration. "( [Social integration after 4 years of heroin-assisted treatment].
Degkwitz, P; Schäfer, I; Verthein, U, 2013
)
2.11
"Heroin-assisted treatment is thus efficacious in the long-term course of treatment and is still effective after termination of treatment with respect to living conditions and use of illicit substances."( Evaluating long-term effects of heroin-assisted treatment: the results of a 6-year follow-up.
Gschwend, P; Güttinger, F; Rehm, J; Schulte, B; Uchtenhagen, A, 2003
)
1.32
"Heroin treatment or abusive drug addiction influences many physiological functions, including the reactions of the immune system. "( Augmented production of proinflammatory cytokines and accelerated allotransplantation reactions in heroin-treated mice.
Blahoutová, V; Holán, V; Krulova, M; Wilczek, H; Zajícová, A, 2003
)
1.98
"heroin. Systemic treatment with physostigmine, an inhibitor of acetylcholinesterase, modestly reduced the acquisition and rate of heroin self-administration, and this suppression of heroin intake was reversed by pretreatment with scopolamine but not by mecamylamine."( Role of acetylcholine transmission in nucleus accumbens and ventral tegmental area in heroin-seeking induced by conditioned cues.
Kalivas, PW; Lai, M; Liu, H; Tang, S; Zhang, F; Zhou, W; Zhu, H, 2007
)
1.28
"Heroin-assisted treatment has been found to be effective for people with severe opioid dependence who are not interested in or do poorly on methadone maintenance."( Heroin-assisted treatment for opioid dependence: randomised controlled trial.
Berger, J; Degkwitz, P; Haasen, C; Krausz, M; Naber, D; Verthein, U, 2007
)
3.23
"Heroin-assisted treatment is more effective for people with opioid dependence who continue intravenous heroin while on methadone maintenance or who are not enrolled in treatment. "( Heroin-assisted treatment for opioid dependence: randomised controlled trial.
Berger, J; Degkwitz, P; Haasen, C; Krausz, M; Naber, D; Verthein, U, 2007
)
3.23
"Heroin-assisted treatment (HAT) is a new form of treatment for heroin-dependent patients not responding to conventional interventions such as methadone maintenance treatment. "( Pregnancy and birth under maintenance treatment with diamorphine (heroin): a case report.
Dilg, C; Garbe, W; Haasen, C; Hartwig, C; Lichtermann, D; Reimer, J; Wuellenweber, L, 2008
)
2.03
"Heroin pretreatment (0.1-0.18 mg/kg i.m.) did not change the cocaine discrimination dose-effect curve."( A primate model of polydrug abuse: cocaine and heroin combinations.
Drieze, J; Lukas, SE; Mello, NK; Mendelson, JH; Negus, SS; Sholar, JW, 1995
)
1.27
"909 heroin users, 452 in treatment and 457 out of treatment."( Cocaine use among heroin users in Spain: the diffusion of crack and cocaine smoking. Spanish Group for the Study on the Route of Administration of Drugs.
Barrio, G; De la Fuente, L; Díaz, A; Rodríguez-Artalejo, F; Royuela, L, 1998
)
1.19
"Heroin overdoses are treated on site by ambulance personnel."( [Prehospital treatment of heroin intoxication in Oslo in 1996].
Hansen, TB; Nilsen, JE; Stokland, O, 1998
)
1.32
"Heroin-assisted treatment has been examined broadly in Switzerland since 1994 within the context of scientific studies. "( [Heroin-assisted treatment of opiate addicts--former and current research emphasis].
Blättler, R; Dobler-Mikola, A; Gutzwiller, F; Kaufmann, B; Steffen, T; Uchtenhagen, A,
)
2.48
"Heroin-supported treatment led to favourable progress of the dermatological situation among patients."( [Development of skin diseases in intravenous drug dependent patients treated with heroin substitution].
Conrad, C; Gutzwiller, F; Steffen, T, 2000
)
1.25
"Heroin pretreatment also shifted the dose-response function for the cocaine-like DS effects of GBR 12909 to the left in the former three monkeys, and did not alter the effects of GBR 12909 in the fourth monkey."( Similar enhancement of the discriminative stimulus effects of cocaine and GBR 12909 by heroin in squirrel monkeys.
Platt, DM; Rowlett, JK; Spealman, RD, 2001
)
1.25
"Heroin treatment was followed by the typical "running fit" in the C57 mice, while the DBA strain was unaffected."( Effects of heroin, alone or in combination with other drugs, on the locomotor activity in two inbred strains of mice.
Castellano, C; Filibeck, L; Oliverio, A, 1976
)
1.37
"Treatment of heroin overdose by administration of i.n."( Intranasal naloxone for the treatment of suspected heroin overdose.
Dietze, P; Kelly, AM; Kerr, D, 2008
)
0.95

Toxicity

The observed side effects were similar to the common toxic signs elicited by heroin at high doses, although cebranopadol did not fully substitute heroin's discriminative stimulant effects. All had signs of heroin use-related adverse events within 1 h after receiving pre-hospital naloxone.

ExcerptReferenceRelevance
" Segmental, sympathetic and any adverse effects were sought."( Extradural versus intramuscular diamorphine. A controlled study of analgesic and adverse effects in the postoperative period.
Conacher, ID; Hull, CJ; Jacobson, L; Phillips, PD, 1983
)
0.27
" This empirical work, based on interview and spatial analysis, is presented as a basis for theorizing the socio-spatial construction of heroin use and for assessing the prospects for safe injecting."( Safety becomes danger: dilemmas of drug-use in public space.
Choi, Y; Dovey, K; Fitzgerald, J, 2001
)
0.51
" Our data show that opioid drugs (heroin and morphine) are more toxic than stimulant drugs (d-amphetamine and cocaine)."( Toxic effects of opioid and stimulant drugs on undifferentiated PC12 cells.
Macedo, TR; Morgadinho, MT; Oliveira, CR; Oliveira, MT; Rego, AC, 2002
)
0.59
"Our objective was to illustrate the dramatic neuroimaging findings of toxic leukoencephalopathy caused by heroin vapor inhalation."( Neuroimaging features of heroin inhalation toxicity: "chasing the dragon".
Andrews, GT; Forkheim, KE; Graeb, DA; Keogh, CF; Spacey, SD, 2003
)
0.84
" No deaths, serious adverse events, or withdrawals due to adverse events occurred."( Safety and efficacy of oral slow release morphine for maintenance treatment in heroin addicts: a 6-month open noncomparative study.
Alexieva, DZ; Pavlova, RZ; Vasilev, GN, 2006
)
0.56
" All had signs of heroin use-related adverse events within 1 h after receiving pre-hospital naloxone."( Recurrent opioid toxicity after pre-hospital care of presumed heroin overdose patients.
Alaspää, AO; Boyd, JJ; Kuisma, MJ; Randell, TT; Repo, JV; Vuori, E, 2006
)
0.91
" Some of these toxic effects are probably mediated by the gas nitric oxide (NO)."( Increased densities of nitric oxide synthase expressing neurons in the temporal cortex and the hypothalamic paraventricular nucleus of polytoxicomanic heroin overdose victims: possible implications for heroin neurotoxicity.
Bernstein, HG; Bielau, H; Bogerts, B; Dobrowolny, H; Krebs, P; Steiner, J; Trübner, K, 2014
)
0.6
"We sought to determine if a "treat and release" clinical pathway is safe in prehospital patients with suspected opioid overdose."( Is a Prehospital Treat and Release Protocol for Opioid Overdose Safe?
Cohn, BG; Keim, SM; Kolinsky, D; Schwarz, ES; Yealy, DM, 2017
)
0.46
" These results imply that a "treat and release" policy might be safe with rare complications."( Is a Prehospital Treat and Release Protocol for Opioid Overdose Safe?
Cohn, BG; Keim, SM; Kolinsky, D; Schwarz, ES; Yealy, DM, 2017
)
0.46
"To review the safety profile of injectable hydromorphone and diacetylmorphine and explore if adverse events (AEs) or serious adverse events (SAEs) were associated with dose and patterns of attendance."( Safety profile of injectable hydromorphone and diacetylmorphine for long-term severe opioid use disorder.
Anis, AH; Brissette, S; Guh, D; Harrison, S; Janmohamed, A; Jutha, S; Krausz, M; MacDonald, S; Marchand, K; Marsh, DC; Oviedo-Joekes, E; Schechter, MT; Zhang, DZ, 2017
)
0.46
" Very few diseases are known to produce such high levels of GFAP, indicating a toxic effect on astrocytes."( Heroin-induced acute myelopathy with extreme high levels of CSF glial fibrillar acidic protein indicating a toxic effect on astrocytes.
Herrman, L; Hietala, MA; Sveinsson, O, 2017
)
1.9
" In this analysis, using the Medical Dictionary for Regulatory Activities coding system we report somnolence (ie, drowsiness, sleepiness, grogginess) and opioid overdose as adverse events."( Adverse Events During Treatment Induction With Injectable Diacetylmorphine and Hydromorphone for Opioid Use Disorder.
Anis, AH; Brissette, S; Guh, D; Harrison, S; MacDonald, S; Marsh, DC; Oviedo-Joekes, E; Palis, H; Schechter, MT,
)
0.13
" There were 34 related somnolence and adverse event (AE) overdoses (4."( Adverse Events During Treatment Induction With Injectable Diacetylmorphine and Hydromorphone for Opioid Use Disorder.
Anis, AH; Brissette, S; Guh, D; Harrison, S; MacDonald, S; Marsh, DC; Oviedo-Joekes, E; Palis, H; Schechter, MT,
)
0.13
" We describe female and male patients treated for acute recreational drug toxicity, and look for gender differences in clinical state, treatment, and toxic agents taken."( Gender differences in acute recreational drug toxicity: a case series from Oslo, Norway.
Brekke, M; Grimsrud, MM; Heyerdahl, F; Hovda, KE; Persett, PS; Syse, VL; Vallersnes, OM, 2019
)
0.51
"This project offers new epidemiological estimates for DSM-IV cocaine dependence among sub-groups of newly incident cocaine users in the United States (US), including estimated attack rates for 21 dependence-related cocaine side effect problems and experiences occurring <12 months after onset."( Cocaine dependence: "Side effects" and syndrome formation within 1-12 months after first cocaine use.
Anthony, JC; Chandra, M, 2020
)
0.56
" For several cocaine side effect problems and experiences (e."( Cocaine dependence: "Side effects" and syndrome formation within 1-12 months after first cocaine use.
Anthony, JC; Chandra, M, 2020
)
0.56
", pre-dating onset); (2) Powder-using initiates become cocaine dependent and then start using crack; (3) The cocaine delivery variant of 'crack-smoking' is more toxic than powder insufflation."( Cocaine dependence: "Side effects" and syndrome formation within 1-12 months after first cocaine use.
Anthony, JC; Chandra, M, 2020
)
0.56
" The observed side effects were similar to the common toxic signs elicited by heroin at high doses, although cebranopadol did not fully substitute heroin's discriminative stimulant effects in our drug discriminative tests."( Cebranopadol reduces cocaine self-administration in male rats: Dose, treatment and safety consideration.
Wei, H; Zhan, CG; Zhang, T; Zheng, F, 2020
)
0.79
" Safe supply programs are required now more than ever to address the high rate of drug toxicity overdose deaths caused by illicit fentanyl and its analogues."( Investigating opioid preference to inform safe supply services: A cross sectional study.
Buxton, JA; Ferguson, M; Lock, K; Papamihali, K; Parmar, A; Weng, A, 2022
)
0.72
" To create effective safe supply programs, we need to engage PWUD about their drugs of choice."( Investigating opioid preference to inform safe supply services: A cross sectional study.
Buxton, JA; Ferguson, M; Lock, K; Papamihali, K; Parmar, A; Weng, A, 2022
)
0.72
" Little is known about behavior change after fentanyl testing and the attitudes around fentanyl knowledge and testing along the US-Mexico border in the context of a safe consumption site."( Behavior change after fentanyl testing at a safe consumption space for women in Northern Mexico: A pilot study.
Angulo, L; Arredondo, J; Cambou, MC; Gonzalez-Nieto, P; Goodman-Meza, D; Loera, A; Pitpitan, EV; Shoptaw, S; Slim, S, 2022
)
0.72
"This was a pilot quantitative and qualitative study with 30 women who use drugs at an unsanctioned safe consumption site in Mexicali, Mexico."( Behavior change after fentanyl testing at a safe consumption space for women in Northern Mexico: A pilot study.
Angulo, L; Arredondo, J; Cambou, MC; Gonzalez-Nieto, P; Goodman-Meza, D; Loera, A; Pitpitan, EV; Shoptaw, S; Slim, S, 2022
)
0.72
" We aimed to characterize injecting practices among real-world populations of persons who regularly inject buprenorphine, as well as associated adverse events reported in order to inform a possible future BUP iOAT intervention."( Patterns of use and adverse events reported among persons who regularly inject buprenorphine: a systematic review.
Bozinoff, N; Le Foll, B; Rubin-Kahana, DS; Tardelli, VS, 2022
)
0.72
" We searched MEDLINE, EMBASE, and PsycINFO from inception through July 2020 and used backwards citation screening to search for publications reporting on dose, frequency among persons who regularly inject the drug, or adverse events associated with intravenous use of buprenorphine."( Patterns of use and adverse events reported among persons who regularly inject buprenorphine: a systematic review.
Bozinoff, N; Le Foll, B; Rubin-Kahana, DS; Tardelli, VS, 2022
)
0.72
" Adverse events could be characterized as known side effects of opioids/buprenorphine or injection-related complications."( Patterns of use and adverse events reported among persons who regularly inject buprenorphine: a systematic review.
Bozinoff, N; Le Foll, B; Rubin-Kahana, DS; Tardelli, VS, 2022
)
0.72
" Sociodemographic characteristics, current HAT regimen, reasons for starting IN DAM, IN DAM doses, number of injection events in the sample, IN DAM continuation rate, and appearance of adverse events and nose-related problems were evaluated."( Safety and feasibility of intranasal heroin-assisted treatment: 4-week preliminary findings from a Swiss multicentre observational study.
Baumgartner, S; Beck, T; Binder, H; Bröer, R; Devaud, N; Dürsteler, KM; Falcato, L; Kormann, A; Krausz, RM; Kurmann, M; Meyer, M; Salim Hassan Fadlelseed, R; Sanwald, U; Simon, O; Strasser, J; Vogel, M; Westenberg, JN, 2023
)
1.18
" No severe adverse events were reported."( Safety and feasibility of intranasal heroin-assisted treatment: 4-week preliminary findings from a Swiss multicentre observational study.
Baumgartner, S; Beck, T; Binder, H; Bröer, R; Devaud, N; Dürsteler, KM; Falcato, L; Kormann, A; Krausz, RM; Kurmann, M; Meyer, M; Salim Hassan Fadlelseed, R; Sanwald, U; Simon, O; Strasser, J; Vogel, M; Westenberg, JN, 2023
)
1.18
"After four weeks, IN DAM was a feasible and safe alternative to other routes of administration for patients with severe OUD in HAT."( Safety and feasibility of intranasal heroin-assisted treatment: 4-week preliminary findings from a Swiss multicentre observational study.
Baumgartner, S; Beck, T; Binder, H; Bröer, R; Devaud, N; Dürsteler, KM; Falcato, L; Kormann, A; Krausz, RM; Kurmann, M; Meyer, M; Salim Hassan Fadlelseed, R; Sanwald, U; Simon, O; Strasser, J; Vogel, M; Westenberg, JN, 2023
)
1.18
" We examined associations between highest BUP-NX and methadone doses, and (1) percentage of opioid-positive urine drug screens (UDS); (2) retention in the assigned treatment; and (3) adverse events (AEs)."( Associations of methadone and buprenorphine-naloxone doses with unregulated opioid use, treatment retention, and adverse events in prescription-type opioid use disorders: Exploratory analyses of the OPTIMA study.
Ahamad, K; Bakouni, H; Foll, BL; Jutras-Aswad, D; Lim, R; McAnulty, C; Socias, ME; Tatar, O, 2023
)
0.91

Pharmacokinetics

The terminal half-life of heroin resembles that of morphine and is maintained by the rate-determining return of distributed heroin from esterase-free tissues. We use pharmacokinetic modeling to calculate parameters of the distribution of heroin, 6-MAM and morphine in blood and brain tissue after subcutaneous heroin administration in mice.

ExcerptReferenceRelevance
" These pharmacodynamic studies, along with prior dispositional studies, suggest that the ability of DAM and AM to rapidly cross the blood-brain barrier determines their potency and time-action differences from M in centrally mediated bioassays."( Pharmacodynamics of subcutaneously administered diacetylmorphine, 6-acetylmorphine and morphine in mice.
Inturrisi, CE; Umans, JG, 1981
)
0.26
" Nevertheless, the terminal half-life of 60-90 min resembles that of morphine and is maintained by the rate-determining return of distributed heroin from esterase-free tissues."( Pharmacokinetics of morphine and its surrogates IV: Pharmacokinetics of heroin and its derived metabolites in dogs.
Garrett, ER; Gürkan, T, 1980
)
0.69
" Because of the lack of information on this route of administration, we evaluated the pharmacokinetic and pharmacodynamic properties of intranasal heroin."( Pharmacokinetics and pharmacodynamics of intranasal "snorted" heroin.
Cone, EJ; Darwin, WD; Goldberger, BA; Grant, TM; Holicky, BA, 1993
)
0.73
"60 ml min-1 kg-1, the elimination half-life was 11."( Morphine, morphine-6-glucuronide and morphine-3-glucuronide pharmacokinetics in newborn infants receiving diamorphine infusions.
Barker, DP; Barrett, DA; Pawula, M; Rutter, N; Shaw, PN, 1996
)
0.29
"In order to evaluate pharmacokinetic interactions between heroin and alcohol and their role in the etiology of heroin-related deaths (HRD), the alcohol concentration in blood (BAC), the free (FM) and total morphine (TM) concentrations in blood (determined by DPC Coat-A-Count radioimmunoassay before and after enzymatic hydrolysis), and the TM concentration in urine and bile (DPC Coat-A-Count after enzymatic hydrolysis) in a population of 39 lethal cases included in the records of the Department of Legal Medicine and Public Health at the University of Pavia from the period January 1997-April 1998 were examined."( The role of alcohol abuse in the etiology of heroin-related deaths. Evidence for pharmacokinetic interactions between heroin and alcohol.
Groppi, A; Montagna, M; Polettini, A,
)
0.64
" The pharmacokinetic profiles of M and inactive morphine-3-glucuronide (M3G) in morphine-treated mice nearly overlapped those in heroin-treated mice, with the only difference being the presence of 6-monoacetylmorphine (AM) in profiles of the latter group."( Pharmacokinetics and cytokine production in heroin and morphine-treated mice.
Bacosi, A; di Carlo, S; Pacifici, R; Pichini, S; Zuccaro, P, 2000
)
0.77
" The pharmacokinetic profile of intranasal diamorphine in adults has been systematically studied."( Intranasal diamorphine as an alternative to intramuscular morphine: pharmacokinetic and pharmacodynamic aspects.
Kendall, JM; Latter, VS, 2003
)
0.32
"The stimulant effect of caffeine, as an additive in diacetylmorphine preparations for study purposes, may interfere with the pharmacodynamic effects of diacetylmorphine."( Population pharmacokinetics of caffeine and its metabolites theobromine, paraxanthine and theophylline after inhalation in combination with diacetylmorphine.
Beijnen, JH; de Jonge, ME; den Hoed, R; Hendriks, VM; Huitema, AD; Sparidans, RW; van den Brink, W; van Ree, JM; Zandvliet, AS, 2005
)
0.33
"To develop an integrated population pharmacokinetic model for heroin (diamorphine) and its pharmacodynamically active metabolites 6-acetylmorphine, morphine, morphine-3-glucuronide and morphine-6-glucuronide."( Population pharmacokinetics of heroin and its major metabolites.
Beijnen, JH; Huitema, AD; Rook, EJ; van den Brink, W; van Ree, JM, 2006
)
0.86
" Here, we use pharmacokinetic modeling on data from the aforementioned study to calculate parameters of the distribution of heroin, 6-MAM and morphine in blood and brain tissue after subcutaneous heroin administration in mice."( Pharmacokinetic modeling of subcutaneous heroin and its metabolites in blood and brain of mice.
Andersen, JM; Boix, F; Mørland, J, 2013
)
0.86
" In order to optimize conditions for measuring heroin and its metabolites in samples collected for pharmacokinetic studies in rats, we investigated the time course of degradation of heroin, 6-MAM, and morphine in four biological matrices: rat blood, rat brain homogenate, bovine serum, and human plasma under various conditions."( Stability of heroin, 6-monoacetylmorphine, and morphine in biological samples and validation of an LC-MS assay for delayed analyses of pharmacokinetic samples in rats.
Birnbaum, AK; Harmon, TM; Jones, JM; Keyler, DE; Pentel, PR; Raleigh, MD; Remmel, RP, 2013
)
1.02
"Ethanol and heroin are both depressant drugs on the central nervous system, and combined use is known to be dangerous due to pharmacodynamic interactions, leading to an even higher risk of respiratory depression and death."( Pharmacokinetic interactions between ethanol and heroin: a study on post-mortem cases.
Andersen, JM; Handal, M; Høiseth, G; Mørland, J; Thaulow, CH, 2014
)
1.04
" This pharmacokinetic interaction could further complicate the outcome after combined use of heroin and ethanol, in addition to the already well-known pharmacodynamic interactions."( Pharmacokinetic interactions between ethanol and heroin: a study on post-mortem cases.
Andersen, JM; Handal, M; Høiseth, G; Mørland, J; Thaulow, CH, 2014
)
0.88
" The simultaneous quantification of morphine, fentanyl and its metabolites via this simple and time- and cost-efficient method could be successfully applied to samples taken for pharmacokinetic evaluation (antemortem and postmortem) after a single dose of morphine or co-administration of morphine with other drugs (e."( Determination of Morphine, Fentanyl and Their Metabolites in Small Sample Volumes Using Liquid Chromatography Tandem Mass Spectrometry.
Gleba, J; Kim, J, 2020
)
0.56

Compound-Compound Interactions

The largest increases occurred in combination with heroin among all PO (4.5%). The substantial presence of alcohol in conjunction with cocaine, heroin and methadone among ME cases.

ExcerptReferenceRelevance
"Published data confirm the substantial presence of alcohol in combination with cocaine, heroin and methadone among ME cases."( Alcohol use in combination with cocaine, heroin and methadone by medical examiner cases.
Dufour, MC; Haberman, PW; Noble, JA, 1995
)
0.78
" Within this proof-of-concept study, which was done in cooperation with the German Federal Criminal Police Office (Bundeskriminalamt, BKA), the adaptability of comprehensive two-dimensional (2D) gas chromatography (GCxGC) combined with a pixel-based chemometric data processing method is demonstrated."( Application of two-dimensional gas chromatography combined with pixel-based chemometric processing for the chemical profiling of illicit drug samples.
Ahrens, B; Drew, K; Eschner, M; Gröger, T; Pütz, M; Schäffer, M; Zimmermann, R, 2008
)
0.35
"In summary, results from this study suggest that maintenance on dextromethorphan in combination with quinidine has a limited role in the treatment of opioid dependence."( Evaluation of the reinforcing and subjective effects of heroin in combination with dextromethorphan and quinidine.
Comer, SD; Sullivan, MA; Vosburg, SK,
)
0.38
" Changes in PO deaths in combination with other psychoactive substances may provide a partial explanation."( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances.
Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017
)
0.46
" We calculated (1) changes in proportions of deaths in combination with benzodiazepines, antidepressants, heroin, alcohol, cocaine between the two periods, and (2) proportions of increase in deaths attributable to each substance among PO and synthetic opioids other than methadone (SO-M) deaths, by age, gender, race/ethnicity."( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances.
Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017
)
0.67
" The largest increases occurred in combination with heroin among all PO (4."( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances.
Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017
)
0.71
"Increased PO overdose deaths over the last decade may be partially explained by increased deaths in combination with other psychoactive substances."( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances.
Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017
)
0.46
" In this work, we developed an ultra-performance liquid chromatography-time-of-flight mass spectrometry method (UPLC-TOF-MS) with online data acquisition and multiple post-data-mining technologies combined with a multivariate statistical and batch validation analysis workflow to assess the characteristic urine metabolites of heroin abusers."( Identification of characteristic heroin metabolites in urine based on data-mining technology and multivariate statistics analysis combined with a targeted verification approach for distinguishing heroin abusers.
Cui, Y; Guo, D; Li, Q; Liu, G; Liu, Y; Qiao, S; Wang, W; Xu, H; Xu, W; Yang, W; Yu, H; Zhang, W, 2020
)
1.01
"5 years (January 2019-June 2021) of driving under the influence of drugs (DUID) and medico-legal death investigation (MDI) cases was investigated, including other drugs detected in combination with xylazine."( Xylazine: Pharmacology Review and Prevalence and Drug Combinations in Forensic Toxicology Casework.
Barbieri, EJ; Kacinko, SL; Logan, BK; Mohr, ALA, 2022
)
0.72

Bioavailability

The bioavailability of inhaled heroin was estimated to be 53% (95% CI 43.5-53%). The bioavailability of smoked heroin was highly variable. Research studies with experienced heroin and cocaine users indicated that an intranasally administered drug provided lower blood concentrations of drug.

ExcerptReferenceRelevance
"Using the rate of absorption of paracetamol following oral administration of the drug, gastric emptying was measured in 21 patients following hysterectomy."( Gastric emptying following hysterectomy with extradural analgesia.
Littlewood, DG; Nimmo, WS; Prescott, LF; Scott, DB, 1978
)
0.26
" The bioavailability of smoked heroin was highly variable."( Pharmacokinetics and pharmacodynamics of smoked heroin.
Cone, EJ; Henningfield, JE; Jenkins, AJ; Keenan, RM, 1994
)
0.83
" Research studies with experienced heroin and cocaine users indicated that an intranasally administered drug generally provided lower blood concentrations of drug and a slower onset of action compared to the intravenous route; however, intranasal doses are easily manipulated by the user and adequate bioavailability and desired drug effects can be achieved."( Recent discoveries in pharmacokinetics of drugs of abuse.
Cone, EJ, 1998
)
0.58
"In this controlled clinical study, the bioavailability and pharmacodynamics of inhaled heroin are evaluated and compared between 'chasing the dragon' and inhalation from a heating device, and at three dose levels, 25, 50 and 100 mg heroin, in two separate study phases."( Heroin self-administration by means of 'chasing the dragon': pharmacodynamics and bioavailability of inhaled heroin.
Blanken, P; Bosman, IJ; Hendriks, VM; van den Brink, W; van Ree, JM, 2001
)
1.98
"On the basis of the linear pharmacokinetics, the high bioavailability of intramuscular diacetylmorphine, and the rapid and extended morphine absorption from oral diacetylmorphine, the intramuscular and oral routes can be recommended as safe and feasible alternatives to the intravenous route for medical prescription of diacetylmorphine."( Pharmacokinetics of high doses of intramuscular and oral heroin in narcotic addicts.
Fattinger, K; Girardin, F; Kullak-Ublick, GA; Maggiorini, M; Meier, PJ; Pauli-Magnus, C; Rentsch, KM; Schwab, MA, 2003
)
0.56
"The physicochemical properties of diamorphine (3,6-diacetylmorphine) enhance its bioavailability compared with more lipid-soluble opioids when administered into the epidural space."( Is the clinical efficacy of epidural diamorphine concentration-dependent when used as analgesia for labour?
Columb, MO; McLeod, GA; Munishankar, B, 2005
)
0.33
" The bioavailability was approximately 60%."( Population pharmacokinetics of caffeine and its metabolites theobromine, paraxanthine and theophylline after inhalation in combination with diacetylmorphine.
Beijnen, JH; de Jonge, ME; den Hoed, R; Hendriks, VM; Huitema, AD; Sparidans, RW; van den Brink, W; van Ree, JM; Zandvliet, AS, 2005
)
0.33
" Not much is known about the pharmacokinetics profile and bioavailability of this specific administration method."( Pharmacokinetics and pharmacodynamics of high doses of pharmaceutically prepared heroin, by intravenous or by inhalation route in opioid-dependent patients.
Beijnen, JH; Hendriks, VM; Hillebrand, MJ; Huitema, AD; Rook, EJ; van den Brink, W; van Ree, JM, 2006
)
0.56
"The bioavailability of inhaled heroin was estimated to be 53% (95% CI 43."( Population pharmacokinetics of heroin and its major metabolites.
Beijnen, JH; Huitema, AD; Rook, EJ; van den Brink, W; van Ree, JM, 2006
)
0.91
" They constitute the first report of a demonstration of the effect of the EHC on morphine bioavailability in an addict, and could be considered as indication, without supporting circumstantial evidence, that the morphine level in bile is related to chronic opiate use."( Bile analysis in heroin overdose.
Cacaci, C; Froldi, R; Tassoni, G; Zampi, M, 2007
)
0.68
" Morphine bioavailability after high-dose oral diacetylmorphine is considerably higher than would be predicted from low-dose trials."( Oral diacetylmorphine (heroin) yields greater morphine bioavailability than oral morphine: bioavailability related to dosage and prior opioid exposure.
Diterich, I; Eich-Höchli, D; Fattinger, K; Halbsguth, U; Rentsch, KM, 2008
)
0.66
" However, morphine bioavailability was considerably higher in chronic users [diacetylmorphine 45."( Oral diacetylmorphine (heroin) yields greater morphine bioavailability than oral morphine: bioavailability related to dosage and prior opioid exposure.
Diterich, I; Eich-Höchli, D; Fattinger, K; Halbsguth, U; Rentsch, KM, 2008
)
0.66
" The relative extended to immediate release bioavailability was calculated to be 86% by non-compartmental analysis and 93% by deconvolution analysis."( Oral heroin in opioid-dependent patients: pharmacokinetic comparison of immediate and extended release tablets.
Fattinger, K; Kullak-Ublick, GA; Perger, L; Rentsch, KM; Verotta, D, 2009
)
0.87
"The pharmacokinetic profile and systemic bioavailability of a substance is often described by blood or total tissue concentrations."( Simultaneous measurement of heroin and its metabolites in brain extracellular fluid by microdialysis and ultra performance liquid chromatography tandem mass spectrometry.
Boix, F; Gottas, A; Morland, J; Oiestad, EL; Pettersen, BS; Ripel, A; Thaulow, CH; Vindenes, V, 2012
)
0.67
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Groups of rats were trained to self-administer cocaine, heroin, or cocaine/heroin combinations using a within session dosing procedure in which three doses were available each session. AA and ANA rats were first subjected to three within-session dose-response determinations during which they were allowed to respond for ascending heroin doses.

ExcerptRelevanceReference
" This information is being applied to the development of parenteral dosage forms of DAM hydrochloride."( Simple high-performance liquid chromatographic method for the separation of 3,6-diacetylmorphine hydrochloride (heroin) and hydrolysis products.
Cradock, JC; Poochikian, GK, 1979
)
0.47
" Plasma testosterone levels decreased signifcantly when heroin dosage was between 45 and 65 mg/day contrasted to predrug base-line levels."( Effects of heroin and methadone on plasma cortisol and testosterone.
Ellingboe, J; McDougle, M; Mendelson, JH; Meyer, RE; Mirin, SM, 1975
)
0.89
" The enkephalin dose-response line was shifted to the right, considered a sign of the development of cross-tolerance."( Oxytocin blocks the development of heroin-enkephalin cross-tolerance in mice.
Kovács, GL; Kriván, M; Sarnyai, Z; Szabó, G; Telegdy, G, 1992
)
0.56
" The data suggest that this dosage regimen of diamorphine is safe."( Diamorphine infusion in the preterm neonate.
Barrett, DA; Davis, SS; Elias-Jones, AC; Rutter, N; Shaw, PN, 1991
)
0.28
" To extend that study, we report herein the results of a dose-response and antagonist challenge experiment."( Effects of heroin and naloxone on cerebral blood flow in the conscious rat.
Fuller, SA; Stein, EA, 1991
)
0.67
" The results suggest that the currently used dosing regimen of diamorphine achieves a safe and effective morphine concentration in the premature newborn but that the loading dose could be modified to achieve a more rapid onset of analgesia."( Morphine kinetics after diamorphine infusion in premature neonates.
Barrett, DA; Davis, SS; Elias-Jones, AC; Rutter, N; Shaw, PN, 1991
)
0.28
" The severity of abstinence symptoms correlated with maternal methadone dosage in both term and preterm infants."( Neonatal opiate abstinence syndrome in term and preterm infants.
Doberczak, TM; Kandall, SR; Wilets, I, 1991
)
0.28
" Heroin hydrochloride was supplied as the bulk powder by the National Institute on Drug Abuse and in the formulated dosage form by Evans Medical, Ltd."( Stability of heroin hydrochloride in infusion devices and containers for intravenous administration.
Davis, K; Duafala, ME; Flora, KP; Hines, J; Kleinberg, ML; McDaniel, A; Nacov, C; Scott, D, 1990
)
1.56
"The purpose of this open, uncontrolled study in a group of confirmed heroin addicts of both sexes was to determine whether clonidine by itself suppresses opiate withdrawal reactions, its maximal effective dosage range, the time of maximal effect, duration of its effectiveness and the extent of cardiovascular side effects."( Evaluation of clonidine suppression of opiate withdrawal reactions: a multidisciplinary approach.
Beroniade, V; Cuthill, JD; Salvatori, VA; Viguié, F, 1990
)
0.51
" Pimozide, a drug thought to attenuate the reinforcing effects of both cocaine and heroin, shifted the functions without disturbing the dose-response relations; pimozide reliably decreased the time between successive cocaine infusions across a 4-fold range of pimozide doses."( Pharmacological regulation of intravenous cocaine and heroin self-administration in rats: a variable dose paradigm.
Gerber, GJ; Wise, RA, 1989
)
0.75
" After drug combinations had been tested, the nicotine dose-response curve was unchanged from its previous values, and naltrexone alone produced no tendency to decrease response rate."( Evidence for opioid mechanisms in the behavioral effects of nicotine.
Coen, KM; Corrigall, WA; Herling, S, 1988
)
0.27
" Complete dose-response data for morphine, heroin, etorphine, d- and l-ethylketazocine, d- and l-pentazocine, and d- and l-N-allylnormetazocine revealed a predominant response of hyperthermia."( Body temperature effects of opioids in rats: intracerebroventricular administration.
Adler, MW; Geller, EB; Rowan, CH, 1986
)
0.53
" The drug was injected intramuscularly in a single administration at a dosage of 600 mg."( Effect of sulpiride on chronic abstinence syndrome in addicted patients.
Drago, F; Marano, P; Nicoletti, F; Patti, F; Scapagnini, U, 1986
)
0.27
"Selected methodological issues of appropriate control procedures and dose-response relationships are discussed with respect to the issue of interpretation."( Issues of methodology and interpretation in clinical and animal behavioral teratology studies.
Hutchings, DE,
)
0.13
" Miconazole was found to be an effective agent in some patients when administered in a dosage of 2400 mg/day."( Fungal endophthalmitis in narcotic abusers. Medical and surgical therapy in 10 patients.
Billson, F; Clifton-Bligh, P; Gallo, J; Gregory-Roberts, J; Grunstein, H; Playfair, J, 1985
)
0.27
"53) between pupillary constriction 120 minutes after drug dosing and the average dollar value of subjects' reported heroin use per week."( Pupillary response to methadone challenge in heroin users.
Bigelow, GE; Higgins, ST; Liebson, IA; McCaul, ME; Stitzer, ML, 1985
)
0.74
" Specifically in the case of morphine it is clear that: it is a very effective analgesic given orally, dosage must be individualized, parenteral use or exotic analgesic 'cocktails' are usually unnecessary, and tolerance, dependence and respiratory depression are rarely common or serious problems which prevent effective pain control provided morphine is used appropriately in accordance with its pharmacological characteristics."( Oral morphine in chronic cancer pain.
Walsh, TD, 1984
)
0.27
" Because the two maintenance programs differed in clinical practices and in enforcement of rules, it was concluded that clients who continue chronic heroin use need not only long-term dosage increases, but also clear, consistently applied program policies."( Chronic heroin use during methadone treatment: a test of the efficacy of high maintenance doses.
Havassy, BE; Tschann, JM, 1984
)
0.9
" It is suggested that previously reported respiratory depression using these techniques is associated with the administration of other analgesics contemporaneously; that dosage should be limited to one-fifth of the estimation intramuscular dose; and that patients should be observed in a recovery ward for 24 hours."( Postoperative analgesia in major orthopaedic surgery. Epidural and intrathecal opiates.
Barron, DW; Strong, JE, 1981
)
0.26
" The dose-response and naloxone antagonism studies suggest that the receptor mechanisms which may subserve opiate convulsions differ from those mediating either analgesia or depressant lethality."( Heroin: analgesia, toxicity and disposition in the mouse.
Inturrisi, CE; Umans, JG, 1982
)
1.71
"Diacetylmorphine (DAM) and 6-acetylmorphine (AM) exhibit virtually identical dose-response and time-action profiles in studies in antinociceptive, excitatory, antidiarrheal and antidiuretic activity after subcutaneous administration to mice."( Pharmacodynamics of subcutaneously administered diacetylmorphine, 6-acetylmorphine and morphine in mice.
Inturrisi, CE; Umans, JG, 1981
)
0.26
" Stress hormone concentrations were reduced at six hours in both dosage groups; differences between loading doses were not significant."( Randomised, double blind trial of two loading dose regimens of diamorphine in ventilated newborn infants.
Barker, DP; Barrett, DA; Pawula, M; Rutter, N; Shaw, PN; Simpson, J, 1995
)
0.29
" Dose-response curves were subsequently determined under conditions of no stress, restraint, corticosterone (3 mg/kg, IP), and saline."( Effects of restraint stress and intra-ventral tegmental area injections of morphine and methyl naltrexone on the discriminative stimulus effects of heroin in the rat.
Shaham, Y; Stewart, J,
)
0.33
" Bicuculline (GABAA receptor antagonist) and picrotoxin (chloride ion channel blocker) given intrathecally produced rightward shifts in the dose-response curves of DPDPE and heroin given intracerebroventricularly."( Spinal GABA receptors mediate brain delta opioid analgesia in Swiss Webster mice.
Fujimoto, JM; Rady, JJ, 1995
)
0.48
" Results suggest that a dose-response relationship exists between the concentration of buprenorphine in hair and the administered dose."( Hair analysis for buprenorphine and its dealkylated metabolite by RIA and confirmation by LC/ECD.
Cirimele, V; Edel, Y; Jamey, C; Kintz, P; Mangin, P, 1994
)
0.29
"4 mg/kg) reduced final ratios and an inverted U dose-response relationship was established for the unit heroin doses 12."( Heroin self-administration in rats under a progressive ratio schedule of reinforcement.
Bennett, SA; Roberts, DC, 1993
)
1.94
" A good dose-response relationship was found between the 100% suppressive withdrawal sign doses of DHE and the degree of withdrawal sign in heroin addicts."( [Clinical assessment of physical dependence potential of dihydroetorphine hydrochloride (DHE)].
Cai, ZJ; Ge, Y; Li, M; Sun, WL, 1994
)
0.49
" The fentanyl dose-response line shifted to the right, and was considered to be a sign of the development of cross-tolerance."( Oxytocin blocks the development of heroin-fentanyl cross-tolerance in mice.
Kovács, GL; Kriván, M; Sarnyai, Z; Szabó, G; Telegdy, G, 1995
)
0.57
" All the dogs received an acute bolus of purified heroin at dosage of 12."( Evaluation of pulmonary perfusion following an acute heroin overdose in dogs.
Di Pasquale, P; Licata, G; Parrinello, G; Paterna, S; Procaccianti, P; Scaglione, R,
)
0.63
"A procedure was employed in the present study to obtain dose-response curves for heroin self-administration within each experimental session."( Within-session determination of dose-response curves for heroin self-administration in rats: Comparison with between-session determination and effects of naltrexone.
Dworkin, SI; Martin, TJ; Sizemore, GM; Smith, JE; Walker, LE, 1996
)
0.77
"03 mg/kg per infusion), AA and ANA rats were first subjected to three within-session dose-response determinations during which they were allowed to respond for ascending heroin doses (0."( Intravenous heroin and ethanol self-administration by alcohol-preferring AA and alcohol-avoiding ANA rats.
Hyytiä, P; Koob, GF; Schulteis, G, 1996
)
0.87
" Treatment included naloxone (12 patients), admission to the pediatric intensive care unit (8), ventilation (5), and reduction in dosage (1)."( Opiate-induced respiratory depression in pediatric patients.
Choonara, IA; Cousins, A; Gill, AM; Nunn, AJ, 1996
)
0.29
" Male long-Evans rats were shaved prior to dosing to obtain their drug-free hair."( Quantitative analysis of methadone and two major metabolites in hair by positive chemical ionization ion trap mass spectrometry.
Foltz, RL; Gygi, SP; Nagasawa, PR; Rollins, DE; Wilkins, DG, 1996
)
0.29
" The sweat patch was applied 10 min before the first dosage and removed approximately 24 h later, minutes before the next dosage."( Sweat testing for heroin and metabolites in a heroin maintenance program.
Brenneisen, R; Bundeli, P; Kintz, P; Mangin, P, 1997
)
0.63
" In dose-response studies, 3-methoxynaltrexone (2."( 3-Methoxynaltrexone, a selective heroin/morphine-6beta-glucuronide antagonist.
Brown, GP; Chang, A; King, MA; Leventhal, L; Pasternak, GW; Rossi, GC; Yang, K, 1997
)
0.58
" Further benefit from lofexidine may be possible with revised dosing regimens."( Double-blind randomised controlled trial of lofexidine versus clonidine in the treatment of heroin withdrawal.
Hu, WH; Lin, SK; Strang, J; Su, LW; Tsai, CJ, 1997
)
0.52
" A dose-response relationship was observed between the monthly cumulative dose of BTH injected subcutaneously or intramuscularly and the development of WB (chi2 for linear trend, 26."( Wound botulism associated with black tar heroin among injecting drug users.
Mac Kenzie, WR; McGee, J; Passaro, DJ; Vugia, DJ; Werner, SB, 1998
)
0.57
" Because of similar metabolic degradation, calculation of the time-dependent ratio of the concentration of morphine and its glucuronide metabolites in blood or serum allows a rough estimation of increased dosage and of time elapsed since the last application."( Formation and clearance of active and inactive metabolites of opiates in humans.
Aderjan, RE; Skopp, G, 1998
)
0.3
" Symptoms are easily recognised; pharmacological treatment can consist of either sedatives or replacement drugs whose dosage depends on the severity of withdrawal symptoms evaluated using a score system."( Neonatal drug addiction.
Fabris, C; Perathoner, C; Prandi, G; Soldi, A, 1998
)
0.3
"5; 250/9, and 500/18 micrograms/infusion; n = 4) under a fixed ratio (FR) 10: 20-s time-out schedule of reinforcement/multicomponent dosing session."( Synergistic elevations in nucleus accumbens extracellular dopamine concentrations during self-administration of cocaine/heroin combinations (Speedball) in rats.
Co, C; Dworkin, SI; Hemby, SE; Smith, JE, 1999
)
0.51
"Controlled human dosing studies with drugs of abuse have revealed the importance of the chosen route of administration on the delivery of drugs to the bloodstream and to their site of action."( Recent discoveries in pharmacokinetics of drugs of abuse.
Cone, EJ, 1998
)
0.3
" Rates of withdrawal symptoms were low and did not differ across dosing schedules."( Plasma concentrations of buprenorphine 24 to 72 hours after dosing.
Chawarski, MC; O'Connor, PG; Pakes, J; Schottenfeld, RS, 1999
)
0.3
" Inclusion of a fixed dose of 3-O-methylnaltrexone significantly shifted the analgesic dose-response curves for 6-acetylmorphine and heroin without altering the morphine dose-response curves."( Antagonism of heroin and morphine self-administration in rats by the morphine-6beta-glucuronide antagonist 3-O-methylnaltrexone.
Izzo, E; King, M; Koob, GF; Pasternak, GW; Walker, JR, 1999
)
0.87
") that was inactive against DAMGO, did not affect endomorphin-1-induced antinociception but shifted the dose-response curve of endomorphin-2 3-fold to the right."( Differential antagonism of endomorphin-1 and endomorphin-2 spinal antinociception by naloxonazine and 3-methoxynaltrexone.
Fujimura, T; Hayashi, T; Kastin, AJ; Murayama, K; Sakurada, C; Sakurada, S; Sakurada, T; Takeshita, M; Yonezawa, A; Yuhki, M; Zadina, JE, 2000
)
0.31
" Oral and rectal doses and dosage intervals were adequate to produce flash and high effects without any cardiovascular and respiratory side-effects nor withdrawal symptoms."( Pharmacodynamics and pharmacokinetics of intravenously, orally and rectally administered diacetylmorphine in opioid dependents, a two-patient pilot study within a heroin-assisted treatment program.
Bourquin, D; Brenneisen, R; Gyr, E; Hug, I; Lehmann, T; Vonlanthen, D, 2000
)
0.5
" Buprenorphene may be one alternative to methadone, however the optimum dosage pattern is as yet unknown."( [Review of scientific evidence on alternatives to methadone in the psychopharmacologic treatment of opiate dependence].
Aizpuru, A; Aizpurua, I; Iruín, A; Ruiz de Apodaka, J; Zapiraín, E,
)
0.13
" Results demonstrated that alprazolam produced a leftward shift of the heroin dose-response curve in the conditioned place preference test."( Benzodiazepine modulation of opiate reward.
Ettenberg, A; Walker, BM, 2001
)
0.54
" As previously reported urine concentrations varied greatly between subjects and within subjects with time after dosing but were much more predictable when values were reported as amount of drug per unit of creatinine."( Urinary excretion profiles for total morphine, free morphine, and 6-acetylmorphine following smoked and intravenous heroin.
Cone, EJ; Darwin, WD; Jenkins, AJ; Paul, BD; Shimomura, ET; Smith, ML; Summers, J, 2001
)
0.52
" When administered as a pretreatment, heroin shifted the dose-response function for cocaine to the left in the three monkeys for which heroin engendered cocaine-lever responding, but did not alter the DS effects of cocaine in the fourth monkey."( Similar enhancement of the discriminative stimulus effects of cocaine and GBR 12909 by heroin in squirrel monkeys.
Platt, DM; Rowlett, JK; Spealman, RD, 2001
)
0.8
" In the abstaining from heroin dependence, therefore, it should consider that sufficient quantum antioxidants such as VC, VE and beta-CAR are dosed to the HAs so as to abate the injuries to their bodies."( Primary studies on heroin abuse and injury induced by oxidation and lipoperoxidation.
Cai, D; Ding, D; Ma, S; Peng, F; Ruan, Z; Si, P; Sun, L; Xu, S; Yan, X; Yuan, H; Zhou, J, 2001
)
0.95
" Cumulative dose-response curves were determined by infusing increasing drug doses at 60 min intervals over 290 min."( The effects of heroin on prolactin levels in male rhesus monkeys: use of cumulative-dosing procedures.
Bowen, CA; Kelly, M; Mello, NK; Negus, SS, 2002
)
0.67
"Stimulus control by buprenorphine was maintained throughout the study and was not changed by repeated daily dosing or by an acute injection of large doses of buprenorphine."( Characterization of the discriminative stimulus effects of buprenorphine in pigeons.
Brandt, MR; France, CP; Galici, R, 2002
)
0.31
" The modest increase in Amsterdam is explained by low background risk of overdose mortality, low starting dosage and the low threshold to treatment."( An increase in overdose mortality during the first 2 weeks after entering or re-entering methadone treatment in Amsterdam.
Buster, MC; van Brussel, GH; van den Brink, W, 2002
)
0.31
" Individuals exposed to opioid treatment for pain management during surgical procedures or maintained on oral methadone for treatment of drug addiction show either no effect or a suppressed immune system, depending on dosage and, in the case of methadone-maintained patients, duration of drug treatment."( Opioids, immunology, and host defenses of intravenous drug abusers.
Alonzo, NC; Bayer, BM, 2002
)
0.31
" Dose-response functions for heroin, methadone, LAAM, three other isomers of acetylmethadol: alpha- d-acetylmethadol, beta- d-acetylmethadol, beta- l-acetylmethadol, and its precursor, beta- l-methadol were examined."( Heroin discriminative stimulus effects of methadone, LAAM and other isomers of acetylmethadol in rats.
Beardsley, PM; May, EL; Newman, JL; Vann, RE, 2002
)
2.05
"Systemic or regional administration of the non-competitive NMDA antagonist dizocilpine into the VTA significantly increased the rate of heroin SA and shifted the heroin dose-response curve to the right."( Blockade of ionotropic glutamatergic transmission in the ventral tegmental area reduces heroin reinforcement in rat.
Stein, EA; Xi, ZX, 2002
)
0.74
" Appropriate daily dosing to achieve these levels is usually between 50 and 150 mg methadone, with the occasional need for even higher doses in the third trimester."( Methadone trough levels in pregnancy.
Berghella, V; Drozdick, J; Hill, M; Kaltenbach, K, 2002
)
0.31
"To determine whether maternal methadone dosage affects duration and degree of neonatal narcotic withdrawal."( Relationship between maternal methadone dosage and neonatal withdrawal.
Dashe, JS; Jackson, GL; Olscher, DA; Sheffield, JS; Todd, SJ; Wendel, GD, 2002
)
0.31
" We evaluated indices of neonatal withdrawal according to the maximum daily methadone dosage in the last week of pregnancy."( Relationship between maternal methadone dosage and neonatal withdrawal.
Dashe, JS; Jackson, GL; Olscher, DA; Sheffield, JS; Todd, SJ; Wendel, GD, 2002
)
0.31
" Median methadone dosage was 20 mg (range 0-150 mg), and 32 infants (46%) were treated for narcotic withdrawal."( Relationship between maternal methadone dosage and neonatal withdrawal.
Dashe, JS; Jackson, GL; Olscher, DA; Sheffield, JS; Todd, SJ; Wendel, GD, 2002
)
0.31
"Maternal methadone dosage was associated with duration of neonatal hospitalization, neonatal abstinence score, and treatment for withdrawal."( Relationship between maternal methadone dosage and neonatal withdrawal.
Dashe, JS; Jackson, GL; Olscher, DA; Sheffield, JS; Todd, SJ; Wendel, GD, 2002
)
0.31
" Both dose-response analyses and the determination of the strength of the reinforcing properties of opiates using a "breakpoint" analysis were examined."( Gender differences in the intravenous self-administration of mu opiate agonists.
Aylward, SC; Cicero, TJ; Meyer, ER, 2003
)
0.32
"The study aimed to identify the range of buprenorphine doses required to comfortably alleviate symptoms in patients undergoing inpatient heroin withdrawal using a symptom-triggered titration dosing regime, and to identify the patient characteristics that impact upon the buprenorphine dose requirements."( Buprenorphine dosing regime for inpatient heroin withdrawal: a symptom-triggered dose titration study.
Bammer, G; Jolley, DJ; Lintzeris, N; Rushworth, L; Whelan, G, 2003
)
0.79
" The combination of alprazolam and varying doses of intravenous heroin resulted in a leftward shift of the heroin dose-response curve."( The effects of alprazolam on conditioned place preferences produced by intravenous heroin.
Ettenberg, A; Walker, BM, 2003
)
0.78
" The 164 subjects included 41 patients in 1-mg, 41 patients in 3-mg, and 41 patients in 8-mg dosage group of buprenorphine, and also 41 patients in the 30-mg dosage group of methadone."( Methadone versus buprenorphine maintenance for the treatment of heroin-dependent outpatients.
Ahmadi, J, 2003
)
0.56
"Consumed amount of narcotics per day and the course of dosage of injectable heroin in different treatment regimes."( Dosage regimes in the prescription of heroin and other narcotics to chronic opioid addicts in Switzerland--Swiss national cohort study.
Blättler, R; Bürki, C; Christen, S; Gschwend, P; Gutzwiller, F; Rehm, J; Seidenberg, A; Steffen, T, 2004
)
0.82
" The mean daily dosage was 474 mg for intravenous application and 993 mg for the smokeable form."( Dosage regimes in the prescription of heroin and other narcotics to chronic opioid addicts in Switzerland--Swiss national cohort study.
Blättler, R; Bürki, C; Christen, S; Gschwend, P; Gutzwiller, F; Rehm, J; Seidenberg, A; Steffen, T, 2004
)
0.59
" Groups of rats were trained to self-administer cocaine, heroin, or cocaine/heroin combinations using a within session dosing procedure in which three doses were available each session."( Effects of 2beta-propanoyl-3beta-(4-tolyl)-tropane (PTT) on the self-administration of cocaine, heroin, and cocaine/heroin combinations in rats.
Davies, HM; Martin, TJ; Sizemore, GM; Smith, JE, 2004
)
0.79
" In one group of rats, we studied (1) acquisition of heroin self-administration behavior using a continuous-reinforcement (fixed-ratio (FR) 1) schedule, (2) heroin dose-response relationships using an FR1/variable-dose schedule, and (3) reinforcing efficacy of heroin using a progressive-ratio schedule."( Exposure to delta-9-tetrahydrocannabinol (THC) increases subsequent heroin taking but not heroin's reinforcing efficacy: a self-administration study in rats.
Goldberg, SR; Panlilio, LV; Solinas, M, 2004
)
0.81
"Powder filled sachets containing a 3:1 (w/w) powder mixture of diacetylmorphine base and caffeine anhydrate were developed as a dosage form for smokable heroin used for the treatment of chronic, treatment-resistant heroin addicts."( Process characterisation, optimisation and validation of production of diacetylmorphine/caffeine sachets: a design of experiments approach.
Beijnen, JH; Klous, MG; Nuijen, B; Van den Brink, W; Van Ree, JM, 2004
)
0.52
" A pharmaceutical dosage form for inhalable heroin was developed for this trial, consisting of a 3:1 powder mixture of diacetylmorphine base and caffeine anhydrate."( Development and manufacture of diacetylmorphine/caffeine sachets for inhalation via 'chasing the dragon' by heroin addicts.
Beijnen, JH; Klous, MG; Nuijen, B; van den Brink, W; van Ree, JM, 2004
)
0.8
" However, heroin, but not SNC-80 or U50488, significantly shifted the dose-response curve for THC discrimination to the left."( Involvement of mu-, delta- and kappa-opioid receptor subtypes in the discriminative-stimulus effects of delta-9-tetrahydrocannabinol (THC) in rats.
Goldberg, SR; Solinas, M, 2005
)
0.73
"A solid dosage form for multiple use was developed for parenteral administration of diacetylmorphine in a clinical trial on co-prescription of heroin to heroin addicts."( Pharmaceutical development of an intravenous dosage form of diacetylmorphine hydrochloride.
Beijnen, JH; Klous, MG; Nuijen, B; van den Brink, W; Van Ree, JM,
)
0.33
"In this prospective, randomised, double-blind study, we compared the effects of two dosage regimens."( Effects of a height and weight adjusted dose of local anaesthetic for spinal anaesthesia for elective Caesarean section.
Boyne, I; Brown, A; Hannah, P; Harten, JM; Varveris, D, 2005
)
0.33
" The 35- to 37-kDa isoforms of deltaFosB, also referred to as the chronic Fras, were measured in the nucleus accumbens, caudate putamen, and frontal cortex of male Sprague-Dawley rats after either an acute injection of morphine or an escalating dosing schedule of morphine for 10 days."( D1 dopamine receptors modulate deltaFosB induction in rat striatum after intermittent morphine administration.
Muller, DL; Unterwald, EM, 2005
)
0.33
" A dose-response relationship was observed between the self-reported amount of heroin used and likelihood of overdose (e."( Transient changes in behaviour lead to heroin overdose: results from a case-crossover study of non-fatal overdose.
Bammer, G; Dietze, P; Fry, C; Jolley, D, 2005
)
0.83
" No beneficial influence was revealed of methadone dosage or program attendance in itself on the risk of relapse into cocaine."( Prediction of relapse to frequent heroin use and the role of methadone prescription: an analysis of the Amsterdam Cohort Study among drug users.
Geskus, R; Krol, A; Prins, M; Termorshuizen, F; van Ameijden, EJ; van den Brink, W, 2005
)
0.61
" Sprague-Dawley rats were implanted with guide cannula targeting the VTA, after which a heroin-induced CPP dose-response curve was determined (2."( Intra-ventral tegmental area heroin-induced place preferences in rats are potentiated by peripherally administered alprazolam.
Ettenberg, A; Walker, BM, 2005
)
0.84
"5-5 mg/kg) produced a rightward shift of a heroin dose-response curve, while vigabatrin (75-300 mg/kg), baclofen (0."( Role of opioidergic mechanisms and GABA uptake inhibition in the heroin-induced discriminative stimulus effects in rats.
Filip, M; Krówka, T; Przewłocki, R; Solecki, W,
)
0.63
" Nevertheless, many clinicians report that some patients can be stably maintained on lower methadone dosages to optimal effect, and clinic dosing practices vary substantially."( Determining effective methadone doses for individual opioid-dependent patients.
Humphreys, K; Minkel, J; Trafton, JA, 2006
)
0.33
" Among patients who achieved heroin abstinence, higher methadone dosages were predicted by having a diagnosis of posttraumatic stress disorder or depression, having a greater number of previous opioid detoxifications, living in a region with lower average heroin purity, attending a clinic where counselors discourage dosage reductions, and staying in treatment longer."( Determining effective methadone doses for individual opioid-dependent patients.
Humphreys, K; Minkel, J; Trafton, JA, 2006
)
0.63
" Dosing guidelines should focus more heavily on appropriate processes of dosage determination rather than solely specifying recommended dosages."( Determining effective methadone doses for individual opioid-dependent patients.
Humphreys, K; Minkel, J; Trafton, JA, 2006
)
0.33
"In preparation for a trial on co-prescription of heroin to chronic treatment-resistant addicts, a pharmaceutical dosage form for smokable heroin was developed."( Volatilisation of diacetylmorphine: in vitro simulation of 'chasing the dragon'.
Beijnen, JH; Klous, MG; Lee, WC; Van den Brink, W; Van Ree, JM, 2006
)
0.59
" The average DAM dosage was 274."( Controlled trial of prescribed heroin in the treatment of opioid addiction.
Carrasco, F; March, JC; Oviedo-Joekes, E; Perea-Milla, E, 2006
)
0.62
"Retention rate after 1 year; number of serious adverse events; dosage of DAM over time; subjective tolerance of study medication."( A prospective cohort study on orally administered heroin substitution for severely addicted opioid users.
Ammann, J; Frick, U; Kovacic, S; Rehm, J; Uchtenhagen, A, 2006
)
0.59
" drug injection, combining heroin with cocaine shifted the heroin dose-response function leftward, and isobolographic analysis indicated that the combined effects were dose-additive."( Modulation of heroin and cocaine self-administration by dopamine D1- and D2-like receptor agonists in rhesus monkeys.
Platt, DM; Rowlett, JK; Spealman, RD; Yao, WD, 2007
)
1
" It consisted of a 24-day uniform double-blind induction phase followed by single-blind flexible dosing based on structured clinical criteria, for a total of 6 months."( A stepped care strategy using buprenorphine and methadone versus conventional methadone maintenance in heroin dependence: a randomized controlled trial.
Grönbladh, L; Heilig, M; Kakko, J; Nilsson, LH; Rawlings, B; Rück, C; Svanborg, KD; von Wachenfeldt, J, 2007
)
0.55
" The opioids of choice have altered over recent years and the dosage regimens used can vary between institutions."( Survey of intrathecal opioid usage in the UK.
Aitkenhead, A; Bedforth, N; Giovannelli, M, 2008
)
0.35
"Different doses and concentrations of heroin appeared to have different effects on intracellular free Ca2+ concentrations, with a dosage dependent short linear increase in the fluorescence intensity (i."( [The effects of heroin on intracellular free Ca2+ of rat myocardium].
Chen, YC; Hao, ZR; Li, HX; Li, ZH; Liu, SP; Liu, XS; Wu, JD, 2007
)
0.96
"Heroin could affect concentrations of [Ca2+]i in myocardium and its dosage related effect needs further investigation."( [The effects of heroin on intracellular free Ca2+ of rat myocardium].
Chen, YC; Hao, ZR; Li, HX; Li, ZH; Liu, SP; Liu, XS; Wu, JD, 2007
)
2.13
" The animals in the heroin group received heroin subcutaneously at a dosage of 10 mg/kg/day on embryonic days (E) 9-18, while those in the saline group were treated as drug-naive."( Prenatal exposure to heroin in mice elicits memory deficits that can be attributed to neuronal apoptosis.
Han, TZ; Wang, Y, 2009
)
1
" The greater benefit of HAT in reducing alcohol use may be due to the greater daily frequency of dispensing heroin coupled with a requirement of sobriety at each dosing occasion."( Effects of heroin-assisted treatment on alcohol consumption: findings of the German randomized controlled trial.
Dilg, C; Eiroa-Orosa, FJ; Haasen, C; Reimer, J; Schäfer, I; Soyka, M; Verthein, U, 2009
)
0.96
" There were no differences in the response between heroin and 6MAM, although we observed a shift to the left of the dose-response curve for the maximal response of heroin."( Increased locomotor activity induced by heroin in mice: pharmacokinetic demonstration of heroin acting as a prodrug for the mediator 6-monoacetylmorphine in vivo.
Andersen, JM; Boix, F; Mørland, J; Normann, PT; Ripel, A, 2009
)
0.87
" In cocaine-trained monkeys, coadministration of cocaine and heroin produced leftward shifts in the cocaine dose-response function."( Asymmetric generalization and interaction profiles in rhesus monkeys discriminating intravenous cocaine or intravenous heroin from vehicle.
Platt, DM; Rowlett, JK; Spealman, RD, 2010
)
0.81
" Importantly, the methadone dosage used in the MMT group was correlated with the FA value in the left splenium of CC and in the right frontal lobe."( White matter impairment in heroin addicts undergoing methadone maintenance treatment and prolonged abstinence: a preliminary DTI study.
Li, Q; Li, W; Wang, W; Wang, Y; Yang, W; Zhu, J, 2011
)
0.67
"1 mg/kg/infusion) generated an inverted U-shaped dose-response function."( Effects of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) and quipazine on heroin self-administration in rhesus monkeys.
France, CP; Koek, W; Li, JX; Maguire, DR, 2013
)
0.62
"1 mg/kg/infusion) generated a typical inverted U-shaped dose-response curve."( Interactions between Δ(9)-tetrahydrocannabinol and heroin: self-administration in rhesus monkeys.
France, CP; Koek, W; Li, JX, 2012
)
0.63
" Bipolar 1 patients needed a higher methadone dosage in the stabilization phase, but this difference was not statistically significant."( The long-term outcomes of heroin dependent-treatment-resistant patients with bipolar 1 comorbidity after admission to enhanced methadone maintenance.
Akiskal, H; Bacciardi, S; Maremmani, AGI; Maremmani, I; Osso, LD; Pacini, M; Paolo Pani, P; Rovai, L; Rugani, F, 2013
)
0.69
" To thoroughly assess vaccine efficacy, full dose-response curves were generated for heroin-induced analgesia in both hot plate and tail immersion tests."( Injection route and TLR9 agonist addition significantly impact heroin vaccine efficacy.
Bremer, PT; Janda, KD; Lively, JM; Schlosburg, JE, 2014
)
0.87
" Half of the mice then continued in a heroin dose-response study, while extinction from heroin SA was studied in the other half."( Mouse model of the OPRM1 (A118G) polymorphism: differential heroin self-administration behavior compared with wild-type mice.
Blendy, JA; Butelman, ER; Ho, A; Kreek, MJ; Picetti, R; Zhang, Y, 2015
)
0.93
"The purpose of this study was to evaluate the effects of a morphine-conjugate vaccine (M-KLH) on the acquisition, maintenance, and reinstatement of heroin self-administration (HSA) in rats, and on heroin and metabolite distribution during heroin administration that approximated the self-administered dosing rate."( Pharmacokinetic correlates of the effects of a heroin vaccine on heroin self-administration in rats.
LeSage, MG; Pentel, PR; Raleigh, MD, 2014
)
0.86
" Plasma TNF-α and IL-6 levels were significantly correlated with the dairy methadone dosage administered, and the IL-1β level was significantly correlated with the duration of methadone maintenance treatment."( Inflammatory response in heroin addicts undergoing methadone maintenance treatment.
Chan, YY; Chang, JL; Lin, JC; Lin, JG; Lo, WY; Yang, SN, 2015
)
0.72
" The present study compared the dose-response functions for intravenous self-administration of cocaine and heroin between male HIV-1 transgenic (HIV-1 Tg) and Fischer 344 rats."( Increased Sensitivity to Cocaine Self-Administration in HIV-1 Transgenic Rats is Associated with Changes in Striatal Dopamine Transporter Binding.
Childers, SR; Hemby, SE; McIntosh, S; Pattison, LP; Sexton, T, 2015
)
0.63
", administration route, average dosage and number of consumers) contribute to depict a realistic representation of the phenomenon in the investigated area."( Data triangulation in the context of opioids monitoring via wastewater analyses.
Been, F; Benaglia, L; Delémont, O; Esseiva, P; Gervasoni, JP; Lucia, S, 2015
)
0.42
"To analyse drug users' views and experiences of naloxone during emergency resuscitation after illicit opiate overdose to identify (i) any evidence of harm caused by excessive naloxone dosing ('over-antagonism'); and (ii) implications for the medical administration of naloxone within contemporary emergency settings."( Naloxone--does over-antagonism matter? Evidence of iatrogenic harm after emergency treatment of heroin/opioid overdose.
Neale, J; Strang, J, 2015
)
0.64
" Participants believed that hospital staff should administer naloxone selectively and cautiously, and prescribe counter-naloxone medication if dosing precipitated withdrawals."( Naloxone--does over-antagonism matter? Evidence of iatrogenic harm after emergency treatment of heroin/opioid overdose.
Neale, J; Strang, J, 2015
)
0.64
" Dosage increase(26."( [Overdose of heroin and influencing factors in intravenous drug users in parts of Yunnan].
Cao, XB; Luo, W; Wu, ZY; Zhang, B; Zhou, Y, 2016
)
0.8
"Although the DRD2 TaqI B genotype was not associated with methadone use requirements, borderline index was revealed as a potential predictive marker for the adjustment of methadone dosage requirements in heroin addicts."( Relationship among methadone dose, polymorphisms of dopamine D2 receptor and tri-dimensional personality questionnaire in heroin-addicted patients.
Chiang, TA; Huang, CS; Huang, MW; Lo, PY, 2016
)
0.83
"When injectable hydromorphone and diacetylmorphine are individually dosed and monitored, their opioid-related side effects, including potential fatal overdoses, are safely mitigated and treated by health care providers."( Safety profile of injectable hydromorphone and diacetylmorphine for long-term severe opioid use disorder.
Anis, AH; Brissette, S; Guh, D; Harrison, S; Janmohamed, A; Jutha, S; Krausz, M; MacDonald, S; Marchand, K; Marsh, DC; Oviedo-Joekes, E; Schechter, MT; Zhang, DZ, 2017
)
0.46
" Given that opioid novices have limited tolerance to opioids, a slight imprecision in dosing inherent in heroin use is likely to be an important factor contributing to the growth in heroin-related over dose fatalities in recent years."( Increased use of heroin as an initiating opioid of abuse.
Cicero, TJ; Ellis, MS; Kasper, ZA, 2017
)
1.01
") dose-dependently decreased oxycodone self-administration, and shifted the oxycodone dose-response curve downward."( The novel dopamine D3 receptor antagonists/partial agonists CAB2-015 and BAK4-54 inhibit oxycodone-taking and oxycodone-seeking behavior in rats.
Bi, GH; Boateng, C; Cao, J; Gao, JT; Gardner, EL; He, Y; Newman, AH; Xi, ZX; You, ZB, 2017
)
0.46
"The Opiate Dosage Adequacy Scale (ODAS) is a clinical tool to individually measure the "adequacy" of opioid doses in patients on maintenance treatment."( Evidence of validity and reliability of the Opiate Dosage Adequacy Scale (ODAS) in a sample of heroin addicted patients in buprenorphine/naloxone maintenance treatment.
Alcaraz, S; González-Saiz, F; Lozano Rojas, O; Pérez de Los Cobos, J; Siñol, N; Trujols, J, 2018
)
0.7
" Lorcaserin pretreatment produced a dose-dependent flattening of the dose-response function for heroin self-administration in each subject."( Lorcaserin decreases the reinforcing effects of heroin, but not food, in rhesus monkeys.
Bergman, J; Kohut, SJ, 2018
)
0.95
" Mean initial buprenophine dosage did not differ between groups."( Impact of Fentanyl Use on Buprenorphine Treatment Retention and Opioid Abstinence.
Chang, Y; Flood, J; Metlay, J; Regan, S; Rigotti, N; Wakeman, SE; Yu, L,
)
0.13
"Naloxone is an established antidote for the treatment of heroin poisoning; however, dosing regimens vary widely, with a current trend towards small titrated intravenous dosing."( One single large intramuscular dose of naloxone is effective and safe in suspected heroin poisoning.
Brier, AJ; Harris, K; Isoardi, KZ; Page, CB; Parker, L; Samantray, S, 2020
)
1.03
" New research is also suggested to address such questions as: What is the time course of exposure to the start of heroin use? How does the frequency and dosage of exposure matter? Continued analyses of MTF data, as well as exploration of other data are needed to address these and related compelling issues."( Pathways to Heroin Use: Commentary on McCabe et al.
Compton, WM; Lopez, MF,
)
0.72
" As predicted, WIN-treated rats showed a rightward shift in the dose-response relationship across all behavioral/physiological measures when compared to vehicle-treated controls."( Chronic cannabinoid exposure produces tolerance to the dopamine releasing effects of WIN 55,212-2 and heroin in adult male rats.
Cheer, JF; Everett, TJ; Gomez, DM; Hamilton, LR; Oleson, EB; Ranganath, A, 2021
)
0.84
" We included any duration of drug treatment and any dosage given continuously or as bolus; we excluded studies that gave opioids to ventilated infants for procedures."( Opioids for newborn infants receiving mechanical ventilation.
Bellù, R; Bruschettini, M; de Waal, KA; Nava, C; Romantsik, O; Zanini, R, 2021
)
0.62
"This case demonstrates how patient-centered dose responses with a focus on functional outcomes supersede existing opioids agonist treatment dosing ranges, especially in the context of a patient with a higher than typical opioid tolerance."( Patient With Very High Opioid Tolerance Enrolled in Opioid Agonist Treatment: A Case Report.
Lim, R; Wilson, P,
)
0.13
" Drug deliveries calculated as percent vehicle followed a prototypical inverted-U shaped dose-response curve for cannabinoids and heroin except for THC and JWH-018 (in males)."( Self-administration of inhaled delta-9-tetrahydrocannabinol and synthetic cannabinoids in non-human primates.
Cooper, ZD; Evans, SM; Foltin, RW, 2021
)
0.83
" In a locale where fentanyl is responsible for the majority of non-fatal opioid overdoses, we compared the concentration of fentanyl in blood to naloxone dosing in the presence and absence of a concurrent sedative-hypnotic exposure."( Sentanyl: a comparison of blood fentanyl concentrations and naloxone dosing after non-fatal overdose.
Babu, KM; Chapman, BP; Devin-Holcombe, K; Fogarty, MF; Krotulski, AJ; Logan, BK; Marks, SJ; Merchant, RC; Ontiveros, ST; Trieu, H, 2022
)
0.72
" Among the sedative-hypnotic exposed, fentanyl concentrations were lower, but naloxone dosing was similar to those without a concomitant exposure."( Sentanyl: a comparison of blood fentanyl concentrations and naloxone dosing after non-fatal overdose.
Babu, KM; Chapman, BP; Devin-Holcombe, K; Fogarty, MF; Krotulski, AJ; Logan, BK; Marks, SJ; Merchant, RC; Ontiveros, ST; Trieu, H, 2022
)
0.72
" The goal of this study was to determine the contribution of discrete or discriminative drug cues and drug dosage to time-dependent increases in drug-seeking."( Drug-associated cues and drug dosage contribute to increased opioid seeking after abstinence.
Floris, G; Sillivan, SE; Zanda, MT, 2021
)
0.62
" Furthermore, mQTL rs5326 was associated with the susceptibility and effective dosage of MMT for heroin use disorder, and demonstrated allele-specific correlation with the expression of the DRD1 gene in the human caudate."( Methylation quantitative trait locus rs5326 is associated with susceptibility and effective dosage of methadone maintenance treatment for heroin use disorder.
Fan, Y; Gao, K; Ma, T; Xiao, Y; Xu, M; Zhang, J; Zhou, J; Zhu, Y, 2021
)
1.04
" The mice in the heroin-addicted group were injected subcutaneously in the first ten days with an increased dosage of heroin from 10 mg/kg to 55 mg/kg."( Determination of metabolic phenotype and potential biomarkers in the liver of heroin addicted mice with hepatotoxicity.
Cao, H; Kuang, H; Li, J; Li, L; Wang, Q; Zhao, H; Zhou, Z, 2021
)
1.19
" The role of NMDA receptor in the regulatory mechanisms of methadone dosage in heroin dependent patients is so far not clear."( Association of the D-amino acid oxidase gene with methadone dose in heroin dependent patients under methadone maintenance treatment.
Chen, ACH; Chung, RH; Fang, CP; Kuo, HW; Liu, SC; Liu, TH; Liu, YL; Tsou, HH; Wang, SC, 2022
)
1.18
" However, ESI stress induced an upward shift of heroin dose-response curve in female mice and increased motivation and seeking for heroin in both sexes."( Early social isolation stress increases addiction vulnerability to heroin and alters c-Fos expression in the mesocorticolimbic system.
Davis, A; Singh, A; Wang, ZJ; Xie, Y, 2022
)
1.21
" However, evidence to guide appropriate dosing of pharmacotherapy for the treatment of opioid use disorder, such as methadone, based on self-reported opioid use during pregnancy is limited."( Does self-reported consumption of heroin correlate with dose of methadone among pregnant people with opioid use disorder?
Arlandson, ME; Gonzalez, AM; Patel, A; Premkumar, A, 2022
)
1
" Time-concentration profiles of diamorphine and its metabolites reflected disposition changes with age and were used to describe intravenous and intranasal dosing regimens."( Pharmacokinetic modeling and simulation to understand diamorphine dose-response in neonates, children, and adolescents.
Anderson, BJ; Gastine, S; Morse, JD; Standing, JF; Wong, ICK, 2022
)
0.72
" In the long term, we observed an improvement on delay discounting correlated with the duration and dosage of SROM."( Does slow release oral morphine have impact on craving and impulsivity in heroin dependent individuals?
Calzada, G; Colombo, L; Giustiniani, J; Penzenstadler, L; Rothen, S; Thorens, G; Zullino, D, 2023
)
1.14
" A need exists to adapt methadone dosing from opioid treatment programs (OTPs) in this era."( Adapting methadone inductions to the fentanyl era.
Buresh, M; Nahvi, S; Steiger, S; Weinstein, ZM, 2022
)
0.72
" Greater intrathecal diamorphine dosing was positively associated with higher number of cases per month (rho=0."( Intrathecal diamorphine for perioperative analgesia during colorectal surgery: a cross-sectional survey of current UK practice.
Alderman, J; Gao-Smith, F; Morgese, C; Patel, J; Sharma, A, 2022
)
0.72
" Therefore, high-quality randomised dose-response trials are needed to investigate the relationship between doses of intrathecal diamorphine and patient outcomes."( Intrathecal diamorphine for perioperative analgesia during colorectal surgery: a cross-sectional survey of current UK practice.
Alderman, J; Gao-Smith, F; Morgese, C; Patel, J; Sharma, A, 2022
)
0.72
" Data collected included baseline demographics, history of illicit drug use, temporal trend in methadone dosage modulation, and co-use of illicit drugs during the MMT."( Methadone Maintenance Treatment for Opioid Dependents: a Retrospective Study.
Abdul Rashid, Q; Jamaluddin, R; Khalid, K; Mohammad Yusoff, MZA; Ooi, YT, 2022
)
0.72
"Novel buprenorphine dosing strategies have emerged with an aim to transition patients from opioid agonists to buprenorphine without prerequisite opioid withdrawal."( Factors that distinguish opioid withdrawal during induction with buprenorphine microdosing: a configurational analysis.
D M, S; E J, M; K K, A, 2022
)
0.72
"3 mg/kg) produced the same degree of rightward shift in the dose-response curves for heroin- and THC-induced antinociception, respectively."( Functional consequences of short-term exposure to opioids versus cannabinoids in nonhuman primates.
Ding, H; Kiguchi, N; Kishioka, S; Ko, MC; Mabry, KM, 2023
)
1.13
" ITS analyses showed that immediately postrescheduling, quarterly hydrocodone dispensing decreased by 177M dosage units while codeine, oxycodone, and morphine dispensing increased by 49M, 62M, and 4M dosage units, respectively."( The impact of hydrocodone rescheduling on utilization, abuse, misuse, and overdose deaths.
Ajao, A; Chai, GP; Ding, Y; Gill, R; Karami, S; Major, JM; McAninch, J; Meyer, T; Secora, A; Wong, J; Zhang, D; Zhao, Y, 2023
)
0.91
" We used whole-body plethysmography to first establish dose-response curves by recording breathing for 60 minutes post-intravenous opioid injection."( Heroin- and Fentanyl-Induced Respiratory Depression in a Rat Plethysmography Model: Potency, Tolerance, and Sex Differences.
Carlson, ER; Frye, EV; Hampson, A; Hastings, LE; Koob, GF; Lewis, SJ; Marchette, RCN; Mejias-Torres, G; Vendruscolo, JCM; Vendruscolo, LF; Volkow, ND, 2023
)
2.35
"The study drew data from OPTIMA, a pan-Canadian, multicenter, pragmatic, two-arm randomized control trial comparing supervised methadone and flexible take-home dosing buprenorphine/naloxone models of care among adults with NH-OUD conducted between 2017 and 2020."( Correlates of nonfatal overdose among treatment-seeking individuals with non-heroin opioid use disorder: Findings from a pragmatic, pan-Canadian, randomized control trial.
Bach, P; Brar, R; Crepeault, H; Jutras-Aswad, D; Le Foll, B; Lim, R; Socias, ME; Ti, L; Wood, E, 2023
)
1.14
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
opioid analgesicA narcotic or opioid substance, synthetic or semisynthetic agent producing profound analgesia, drowsiness, and changes in mood.
mu-opioid receptor agonistA compound that exhibits agonist activity at the mu-opioid receptor.
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
morphinane alkaloidAn isoquinoline alkaloid based on a morphinan skeleton and its substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (2)

PathwayProteinsCompounds
Heroin Metabolism Pathway45
Heroin metabolism03

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cellular tumor antigen p53Homo sapiens (human)Potency26.60320.002319.595674.0614AID651631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (140)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cholesterol biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
response to toxic substanceLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol effluxLiver carboxylesterase 1Homo sapiens (human)
negative regulation of cholesterol storageLiver carboxylesterase 1Homo sapiens (human)
epithelial cell differentiationLiver carboxylesterase 1Homo sapiens (human)
cholesterol homeostasisLiver carboxylesterase 1Homo sapiens (human)
reverse cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
medium-chain fatty acid metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cellular response to cholesterolLiver carboxylesterase 1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusLiver carboxylesterase 1Homo sapiens (human)
cholesterol ester hydrolysis involved in cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid secretionLiver carboxylesterase 1Homo sapiens (human)
lipid catabolic processLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
sterol esterase activityLiver carboxylesterase 1Homo sapiens (human)
methylumbelliferyl-acetate deacetylase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylesterase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylic ester hydrolase activityLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
cytoplasmLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulum lumenLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
cytosolLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID412236Lipophilicity, log P of the compound2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Comparison of benzil and trifluoromethyl ketone (TFK)-mediated carboxylesterase inhibition using classical and 3D-quantitative structure-activity relationship analysis.
AID19246Partition coefficient of cation (logD)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Octanol-, chloroform-, and propylene glycol dipelargonat-water partitioning of morphine-6-glucuronide and other related opiates.
AID456232Activity at human recombinant CES1 expressed in baculovirus-infected Spodoptera frugiperda Sf21 cells assessed as substrate hydrolysis by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID19240Partition coefficient of Zwitterion (logD)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Octanol-, chloroform-, and propylene glycol dipelargonat-water partitioning of morphine-6-glucuronide and other related opiates.
AID25846Amine pKa of compound1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Octanol-, chloroform-, and propylene glycol dipelargonat-water partitioning of morphine-6-glucuronide and other related opiates.
AID18980Log D of compound; LogD at pH 7.41996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Octanol-, chloroform-, and propylene glycol dipelargonat-water partitioning of morphine-6-glucuronide and other related opiates.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5,922)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901989 (33.59)18.7374
1990's852 (14.39)18.2507
2000's1207 (20.38)29.6817
2010's1211 (20.45)24.3611
2020's663 (11.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials373 (5.87%)5.53%
Reviews356 (5.60%)6.00%
Case Studies682 (10.72%)4.05%
Observational20 (0.31%)0.25%
Other4,928 (77.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (14)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Open-label Pilot Comparison Between Alfentanil and Diamorphine for Palliative Care Patients Who Require Subcutaneous Opioids [NCT01049672]18 participants (Actual)Interventional2010-09-30Completed
The Effects of Diacetylmorphine (Heroin) on Human Brain Functions and Stress Response [NCT01174927]Phase 160 participants (Actual)Interventional2010-03-31Completed
An Evaluation of the Effectiveness of Ibuprofen and Opioid (Morphine or Diamorphine) for Acute Pain in Sickle Cell Disease: a Double-blind, Placebo-controlled Randomised Trial [NCT00880373]Phase 4320 participants (Anticipated)Interventional2011-03-31Terminated(stopped due to The funding withdrawal and early termination of the trial is based upon lack of suitable recruitment figures in order to reach the required trial endpoints.)
Pain Relief After Colorectal Surgery: Single-shot Spinal Combined With Painbuster® vs Painbuster® Alone. A Pilot Randomised Controlled Trial [NCT02210260]79 participants (Actual)Interventional2013-09-30Completed
Phase III Study of Maintenance Treatment for Opiate Dependence With Heroin (Diamorphine) Compared to Methadone [NCT00268814]Phase 31,015 participants (Actual)Interventional2002-03-31Completed
Reinforcing Effects of Intravenous Buprenorphine Versus Buprenorphine/Naloxone in Buprenorphine-maintained Intravenous Drug Users (P05207) [NCT00710385]Phase 319 participants (Actual)Interventional2007-09-30Completed
The Impact of Intravenous Heroin Use on Immune Activation in Treated HIV [NCT03976258]190 participants (Actual)Observational2017-07-14Completed
Phase 1A/1B Clinical Trials of Multivalent Opioid Vaccine Components [NCT04458545]Phase 1/Phase 245 participants (Anticipated)Interventional2020-10-08Recruiting
Randomised, Observer Blinded, Controlled Trial of Intrathecal Diamorphine Versus Femoral Nerve Block for Post-operative Analgesia Following Primary Total Knee Arthroplasty [NCT01931332]120 participants (Actual)Interventional2010-02-28Completed
[NCT02700217]101 participants (Actual)Interventional2016-03-16Completed
Buprenorphine/Naloxone Treatment for Opioid Dependence-Experiment I(2) [NCT00000327]Phase 20 participants (Actual)Interventional1997-06-30Withdrawn
North American Opiate Medication Initiative (NAOMI): Multi-Centre, Randomized Controlled Trial of Heroin-Assisted Therapy for Treatment-Refractory Injection Opiate Users [NCT00175357]Phase 3192 participants (Actual)Interventional2005-03-31Completed
SALOME: Multi-Centre, Double Blind Randomized Controlled Trial Comparing The Effectiveness Of Diacetylmorphine Vs. Hydromorphone For The Treatment Of Long-Term Injection Opioid Users Who Do Not Benefit From Available Therapies [NCT01447212]Phase 3202 participants (Actual)Interventional2011-12-31Completed
Buprenorphine/Naloxone Treatment for Opioid Dependence-Experiment 1(1) [NCT00000326]Phase 20 participants (Actual)Interventional1997-04-30Withdrawn
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00710385 (2) [back to overview]"Drug Liking"
NCT00710385 (2) [back to overview]Drug's Breakpoint

"Drug Liking"

"Participant's subjective ratings of how much they Like the dose they just received on a scale of 0 -100." (NCT00710385)
Timeframe: Peak (highest) rating obtained following drug administration throughout the entire 3 hr session

Interventionunits on a scale (Mean)
Heroin41.5
Naloxone3
Low Bup Dose29.8
High Bup Dose42.5
Lower Bup/Nal Dose10.5
High Bup/Nal Dose27
Placebo1

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Drug's Breakpoint

"Measure of a drug's reinforcing effects. The Breakpoint is the point at which the participant stop performing an operant task (clicks on a mouse) in order to received the drug. Therefore, the reported breakpoint is the total amount of work the participant was willing to perform to receive the dose being tested" (NCT00710385)
Timeframe: Single measurement taken following each of the 7 IV experimental doses

Interventionnumber of clicks on a mouse (Mean)
Heroin1200
Naloxone10
Low Bup Dose1100
High Bup Dose1200
Lower Bup/Nal Dose300
High Bup/Nal Dose750
Placebo0

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