Propacetamol is a prodrug of paracetamol (acetaminophen). It is a water-soluble ester of paracetamol, which is converted to paracetamol in the body via enzymatic hydrolysis. Propacetamol is used as an analgesic and antipyretic. It is particularly useful in patients with gastrointestinal problems, as it is less likely to cause stomach irritation than paracetamol. It is also commonly used in children. Propacetamol is synthesized by reacting paracetamol with propionic anhydride. It is then hydrolyzed to paracetamol in the body. The hydrolysis of propacetamol is catalyzed by the enzyme carboxylesterase. Propacetamol is studied for its analgesic and antipyretic effects, as well as its safety and efficacy. It is important to note that propacetamol is not a drug that is widely available in all countries. In some countries, it is only available by prescription. The use of propacetamol is generally considered safe and effective, but it is important to consult with a healthcare professional before taking any medication. It is important to note that the information provided here is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified healthcare provider with any questions you may have regarding a medical condition. Never disregard professional medical advice or delay in seeking it because of something you have read here.'
propacetamol: prodrug for acetaminophen; structure given in UD; RN given refers to HCl; RN for parent cpd not available 5/90
ID Source | ID |
---|---|
PubMed CID | 68865 |
CHEMBL ID | 1851805 |
CHEBI ID | 135089 |
SCHEMBL ID | 26155 |
MeSH ID | M0175922 |
Synonym |
---|
propacetamolum [latin] |
n,n-diethylglycine, ester with 4'-hydroxyacetanilide |
propacetamol [inn] |
einecs 266-390-1 |
propacetamol |
propacetamol (inn) |
D07294 |
66532-85-2 |
CHEBI:135089 |
(4-acetamidophenyl) 2-(diethylamino)acetate |
propacetamol [inn:ban] |
propacetamolum |
5chw4jmr82 , |
unii-5chw4jmr82 |
CHEMBL1851805 |
FT-0630766 |
AKOS015890722 |
propacetamol [mi] |
propacetamol [who-dd] |
SCHEMBL26155 |
cas-66532-85-2 |
tox21_113811 |
NCGC00253689-01 |
dtxsid3057800 , |
dtxcid7031589 |
glycine, n,n-diethyl-, 4-(acetylamino)phenyl ester |
DB09288 |
4-acetamidophenyl 2-(diethylamino)acetate |
BCP13498 |
Q907888 |
MS-23737 |
CS-0374746 |
HY-145453 |
Propacetamol is an APAP prodrug, which is clinically bioequivalent to APAP. It was found to be a major suspected drug of pharmacologically associated hypotension in Korea.
Excerpt | Reference | Relevance |
---|---|---|
"Propacetamol did not enhance analgesia, nor did it decrease cumulative opioid consumption or reduce adverse effects in a dose of 2 g given every sixth hour for 3 days after surgery." | ( Propacetamol as adjunctive treatment for postoperative pain after cardiac surgery. Hakala, T; Hendolin, H; Hynynen, M; Kokki, H; Lahtinen, P, 2002) | 2.48 |
Intravenous propacetamol may be a safe and effective choice for pediatric URTI patients presenting with fever. It induced a small morphine-sparing effect, it did not change the incidence of morphine-related adverse effects in the postoperative period.
The pharmacokinetic parameters of paracetamol were studied after 15 min intravenous infusion. 5 neonates aged less than 10 days and 7 infants aged between 1 and 12 months.
Propacetamol and ketorolac, combined with patient-controlled analgesia morphine, show similar analgesic efficacy after gynecologic surgery.
Excerpt | Reference | Relevance |
---|---|---|
" The population was divided into two groups: group 1 received 20 mg of nalbuphine hydrochloride and group 2 received 2 g of propacetamol combined with 10 mg of nalbuphine hydrochloride." | ( [Comparison of the analgesic efficacy of nalbuphine and its combination with propacetamol during the immediate postoperative period in gynecologic-obstetric surgery]. Granry, JC; Jacob, JP; Monrigal, C, 1994) | 0.72 |
"Propacetamol and ketorolac, combined with patient-controlled analgesia morphine, show similar analgesic efficacy after gynecologic surgery." | ( A double-blinded evaluation of propacetamol versus ketorolac in combination with patient-controlled analgesia morphine: analgesic efficacy and tolerability after gynecologic surgery. Agrò, F; Aloe, L; Ballabio, M; De Cillis, P; De Nicola, A; Giunta, F; Ischia, S; Marinangeli, F; Stefanini, S; Varrassi, G, 1999) | 2.03 |
Excerpt | Reference | Relevance |
---|---|---|
"49) corresponding to a mean oral bioavailability of paracetamol of 82." | ( Tolerance and pharmacokinetics of propacetamol, a paracetamol formulation for intravenous use. de Schepper, PJ; Depré, M; Gerin, M; Tjandra-Maga, TB; van Hecken, A; Verbesselt, R, 1992) | 0.56 |
The aim of this study was to describe propacetamol pharmacokinetics in term and preterm neonates to suggest dosing regimens. Postoperatively the propacetmol dosage was repeated twice and diclofenac once on the ward.
Class | Description |
---|---|
alpha-amino acid ester | The amino acid ester derivative obtained the formal condensation of an alpha-amino acid with an alcohol. |
[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] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 37.5780 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 2.9849 | 0.0010 | 22.6508 | 76.6163 | AID1224838 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 2 (1.67) | 18.7374 |
1990's | 36 (30.00) | 18.2507 |
2000's | 50 (41.67) | 29.6817 |
2010's | 20 (16.67) | 24.3611 |
2020's | 12 (10.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (43.59) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 64 (51.61%) | 5.53% |
Reviews | 5 (4.03%) | 6.00% |
Case Studies | 5 (4.03%) | 4.05% |
Observational | 1 (0.81%) | 0.25% |
Other | 49 (39.52%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
[NCT02116257] | 108 participants (Actual) | Interventional | 2013-11-30 | Completed | |||
[NCT02577068] | 84 participants (Actual) | Interventional | 2015-11-15 | Completed | |||
Perioperative Regular Usage of Propacetamol to Reduce Post Cesarean Section Uterine Contraction Pain and Opioid Consumption [NCT03878082] | 100 participants (Actual) | Interventional | 2019-08-12 | Completed | |||
The Effect of Dexamethasone Versus Local Infiltration Technique on Postoperative Nausea and Vomiting After Tonsillectomy in Children: A Randomized Double-blind Clinical Trial [NCT02355678] | 129 participants (Actual) | Interventional | 2015-01-31 | Completed | |||
[NCT01833728] | 16 participants (Actual) | Interventional | 2013-04-30 | Completed | |||
Comparison of the Effect of Propacetamol, Ibuprofen or Their Combination on Postoperative Pain and Quality of Recovery After Laparoscopic Hernia Repair in Children [NCT03352362] | 159 participants (Actual) | Interventional | 2017-12-15 | Completed | |||
[NCT02515188] | 98 participants (Actual) | Interventional | 2015-08-07 | Completed | |||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |