Page last updated: 2024-12-05

diethylcarbamazine

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Description

Diethylcarbamazine (DEC) is a medication used to treat and prevent filariasis, a parasitic infection. It is synthesized via a multi-step process starting with diethyl amine and reacting it with a series of reagents. DEC acts by killing microfilariae (immature worms) and inhibiting the development of adult worms. Its effectiveness is attributed to its ability to interfere with the parasitic worms' metabolic pathways and neuromuscular functions. It has been widely used for decades and is considered an essential medicine by the World Health Organization. However, DEC can cause side effects such as nausea, vomiting, and dizziness. Studies continue to investigate its potential for treating other parasitic diseases and its mechanisms of action. '

Diethylcarbamazine: An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3052
CHEMBL ID684
CHEBI ID4527
SCHEMBL ID67289
MeSH IDM0006347

Synonyms (103)

Synonym
BRD-K45542189-048-05-6
KBIO1_000548
DIVK1C_000548
n,n-diethyl-4-methylpiperazine-1-carboxamide
SPECTRUM_000938
PRESTWICK2_000284
BPBIO1_000208
NCGC00178778-01
NCGC00178778-02
1-piperazinecarboxamide, n,n-diethyl-4-methyl-
cypip
1-diethylcarbamyl-4-methylpiperazine
n,n-diethyl-4-methyl-piperazine-1-carboxamide
nsc1364
caricide
BSPBIO_000188
IDI1_000548
SPECTRUM5_000877
PRESTWICK3_000284
BSPBIO_002179
ditrazine base
diethylcarbamazinum [inn-latin]
ethodryl
brn 0143029
diethylcarbamazine [inn:ban]
spatonin
ai3-19612
caracide
dietilcarbamazina [inn-spanish]
notezine
bitirazine
84l
diaethylcarbamazinum
carbamazine
carbilazine
einecs 202-023-3
AB00053457
n,n-diethyl-4-methyl-1-piperazinecarboxamide
diethylcarbamazine
90-89-1
C07968
DB00711
diethyl carbamazine
KBIOGR_001081
KBIO2_001418
KBIO2_003986
KBIOSS_001418
KBIO2_006554
KBIO3_001399
SPECTRUM3_000390
PRESTWICK0_000284
SPECTRUM4_000511
SPBIO_002407
SPBIO_001203
SPECTRUM2_001022
PRESTWICK1_000284
NINDS_000548
chebi:4527 ,
camin
CHEMBL684
diethylcarbamazine (inn)
D07825
camin (tn)
AKOS003268016
4-23-00-00225 (beilstein handbook reference)
dietilcarbamazina
unii-v867q8x3zd
diethylcarbamazinum
v867q8x3zd ,
ec 202-023-3
FT-0624832
S10791
diethylcarbamazine [mi]
diethylcarbamazine [inn]
diethylcarbamazine [who-dd]
SCHEMBL67289
n,n-diethylcarbamazine
caritrol (salt/mix)
1-(n,n-diethylcarbamoyl)-4-methylpiperazine
nemacide (salt/mix)
1-methyl-4-diethylcarbamoylpiperazine
1-diethylcarbamoyl-4-methylpiperzine
1-diethylcarbamoyl-4-methylpiperazine
banocide (salt/mix)
RCKMWOKWVGPNJF-UHFFFAOYSA-N
r.p. 3799
HMS3604F12
AB00053457_12
DTXSID1022928
mfcd00023288
nn-diethyl-4-methyl-1-piperazinecarboxamide
SBI-0051345.P003
mmv002816
DS-9360
Q409267
bitirazine; caracide;carbamazine
BRD-K45542189-048-15-5
NCGC00178778-07
SR-01000759234-8
CS-0013568
HY-12642A
EN300-119374
Z641623606

Research Excerpts

Overview

Diethylcarbamazine (DEC) is an antifilarial drug with potent anti-inflammatory properties as a result of its interference with the metabolism of arachidonic acid. It also has effects on intestinal nematodes, but its mechanism of action remains unclear.

ExcerptReferenceRelevance
"Diethylcarbamazine is an important classic drug used for prevention and treatment of lymphatic filariasis and loiasis, diseases caused by filarial nematodes. "( Diethylcarbamazine activates TRP channels including TRP-2 in filaria, Brugia malayi.
Kashyap, SS; Martin, RJ; Robertson, AP; Verma, S, 2020
)
3.44
"Diethylcarbamazine (DEC) is an antifilarial drug with potent anti-inflammatory properties as a result of its interference with the metabolism of arachidonic acid. "( Diethylcarbamazine attenuates the development of carrageenan-induced lung injury in mice.
Barbosa, KP; da Silva Junior, VA; da Silva, BS; Donato, MA; Fragoso, IT; Gomes, FO; Peixoto, CA; Ribeiro, EL; Rocha, SW; Soares e Silva, AK, 2014
)
3.29
"Diethylcarbamazine (DEC) is a piperazine derivative drug with anti-inflammatory properties."( Inhibition of NF-κB activation by diethylcarbamazine prevents alcohol-induced liver injury in C57BL/6 mice.
da Silva, BS; E Silva, AK; Gomes, FO; Peixoto, CA; Ribeiro, EL; Rocha, SW; Rodrigues, GB, 2014
)
1.4
"Diethylcarbamazine is a drug that is used for the treatment of filariasis in humans and animals; it also has effects on intestinal nematodes, but its mechanism of action remains unclear. "( Diethylcarbamazine increases activation of voltage-activated potassium (SLO-1) currents in Ascaris suum and potentiates effects of emodepside.
Buxton, SK; Martin, RJ; Robertson, AP, 2014
)
3.29
"Diethylcarbamazine (DEC) is a drug that has anti-inflammatory properties due to its effects on the metabolism of arachidonic acid."( Diethylcarbamazine: possible therapeutic alternative in the treatment of alcoholic liver disease in C57BL/6 mice.
de França, ME; de Oliveira, WH; Dos Santos, LA; Gomes, FO; Lós, DB; Peixoto, CA; Rocha, SW; Rodrigues, GB, 2015
)
2.58
"Diethylcarbamazine (DEC) is an anthelmintic piperazine derivative drug with putative immunomodulating properties, including increased platelet and granulocyte adhesion to parasites and enhanced production of cytokines. "( Immunomodulatory activity of diethylcarbamazine on humoral, cellular cytokine response and respiratory burst in BALB/c mice.
Brattig, NW; Castro-Corona, MA; García-Hernández, M; Guerrero-Ramírez, G; Medina-De la Garza, CE; Salinas-Carmona, MC; Torres-López, E, 2012
)
2.11
"Diethylcarbamazine (DEC) is an important drug for treatment and control of lymphatic filariasis. "( Efficacy of DEC against Ascaris and hookworm infections in schoolchildren.
Meyrowitsch, DW; Simonsen, PE, 2001
)
1.75
"Diethylcarbamazine citrate (DEC) is an anthelmintic drug which has been used recently, with varying results, in the treatment of bronchial asthma. "( Actions of diethylcarbamazine in experimental anaphylaxis.
Arruzazabala, ML; de la Vega, AR; García, M; González, R; Pérez, H,
)
1.96
"Diethylcarbamazine proved to be a noncompetitive inhibitor of sulfotransferase and prevented hair growth stimulation by minoxidil but not by minoxidil sulfate."( Minoxidil sulfate is the active metabolite that stimulates hair follicles.
Baker, CA; Buhl, AE; Johnson, GA; Waldon, DJ, 1990
)
1
"Diethylcarbamazine (DEC) is an inhibitor of lipoxygenase, with protective effects in several experimental models of anaphylaxis and lung dysfunction. "( Diethylcarbamazine on pulmonary vascular response to endotoxin in awake sheep.
Brigham, KL; Kobayashi, T; Newman, JH; Zadoff, AD, 1986
)
3.16
"Diethylcarbamazine (DEC) is an effective microfilaricidal drug against Wuchereria bancrofti, Brugia malayi, and Brugia timori--the three lymphatic-dwelling filariae infecting humans. "( Efficacy of diethylcarbamazine in eradicating infection with lymphatic-dwelling filariae in humans.
Ottesen, EA,
)
1.95

Effects

Diethylcarbamazine citrate (DEC) has been known for its efficacy to eradicate bancroftian filariasis in Egypt and other countries. Its efficacy in killing adult worms is only around 50% and its direct mode of action is unclear.

ExcerptReferenceRelevance
"Diethylcarbamazine citrate (DEC) has been known for its efficacy to eradicate bancroftian filariasis in Egypt and other countries in the world. "( Effect of diethylcarbamazine citrate and Setaria equina excretory-secretory material on rat hepatocellular carcinoma.
Abdel-Latif, M; El-Fayoumi, H; El-Mallah, AM; El-Shahawi, G; Sakran, T, 2014
)
2.25
"Diethylcarbamazine (DEC) has been used for decades in control programs as an effective microfilaricide, although its efficacy in killing adult worms is only around 50% and its direct mode of action is unclear."( Comparative analysis of a chemotherapy effect on the cuticular surface of Wuchereria bancrofti adult worms in vivo.
Dreyer, G; Lanfredi, RM; Lins, R; Norões, J; Oliveira-Menezes, A, 2007
)
1.06
"Diethylcarbamazine (DEC) has been proven to be highly effective against lymphatic filariasis, although its effect on vertebrate cells remains uncertain. "( Changes in mouse Leydig cells ultrastructure and testosterone secretion after diethylcarbamazine administration.
Donato, MA; Peixoto, CA; Peres, NG; Saraiva, KL; Silva, VA; Souza, JR; Torres, Dde O, 2008
)
2.02
"Diethylcarbamazine has been used in the treatment of onchocerciasis and human filariasis."( Drug treatment of tropical parasitic infections: recent achievements and developments.
Stephenson, I; Wiselka, M, 2000
)
1.03
"Diethylcarbamazine (DEC) has been successfully administered to millions of people in established villages and towns, but little or no information exists on the use of this drug to control lymphatic filariasis in isolated seminomadic groups. "( Control of lymphatic filariasis in a hunter-gatherer group in Madang Province.
Alpers, MP; Blakie, WM; Bockarie, MJ; Jenkins, C; Lagog, M,
)
1.57

Treatment

Diethylcarbamazine citrate (DEC) treatment of loiasis is complicated by adverse reactions that are correlated with the number of circulating microfilariae (mf) For diethyl carbamazine-albendazole treatment the average mf loss was approximately 83% (ranging from 54% to 100% in the different studies)

ExcerptReferenceRelevance
"Diethylcarbamazine citrate (DEC) treatment of loiasis is complicated by adverse reactions that are correlated with the number of circulating microfilariae (mf). "( A Randomized, Placebo-controlled, Double-blind Pilot Study of Single-dose Humanized Anti-IL5 Antibody (Reslizumab) for the Reduction of Eosinophilia Following Diethylcarbamazine Treatment of Loa loa Infection.
Fay, MP; Herrick, J; Holland-Thomas, N; Klion, AD; Legrand, F; Makiya, M; Nutman, TB; Ramanathan, R; Rampertaap, S; Stoddard, J; Thompson, R; Ware, J, 2021
)
2.26
"Diethylcarbamazine treatment significantly weakened reactive oxygen species production and reduced the levels of tumor necrosis factor (TNF)‑α, interleukin‑6 and NF‑κB/p65 in AMI rats."( Protective effect of diethylcarbamazine inhibits NF-κB activation in isoproterenol-induced acute myocardial infarction rat model through the PARP pathway.
Jia, G; Liu, X; Zao, M, 2017
)
1.5
"For diethylcarbamazine-albendazole treatment the average mf loss was approximately 83% (ranging from 54% to 100% in the different studies) and worm-productivity loss was 100% (in all studies)."( Model-based analysis of trial data: microfilaria and worm-productivity loss after diethylcarbamazine-albendazole or ivermectin-albendazole combination therapy against Wuchereria bancrofti.
de Kraker, ME; Habbema, JD; Stolk, WA; van Oortmarssen, GJ, 2006
)
1.04
"Diethylcarbamazine (DEC) treatment led to a significant increase in IgG and IgM levels in microfilaraemic individuals."( Antibody response to a filarial antigen fraction in individuals exposed to Wuchereria bancrofti infection in India.
Bal, M; Das, MK, 1999
)
1.02
"Diethylcarbamazine treatment eliminated microfilariae in 78% of the positives."( Prevalence and intensity of Wuchereria bancrofti antigenaemia in Sri Lanka by Og4C3 ELISA using filter paper-absorbed whole blood.
Gunawardena, NK; Itoh, M; Kimura, E; Qiu, XG; Weerasooriya, MV,
)
0.85
"Diethylcarbamazine treatment caused a marked increase in living and dead microfilariae in the cornea, punctate opacities, and limbitis during the first week of therapy."( Treatment of onchocerciasis. The ocular effects of ivermectin and diethylcarbamazine.
Aziz, MA; Cupp, EW; D'Anna, SA; Greene, BM; Keyvan-Larijani, E; Murphy, RP; Newland, HS; Taylor, HR; White, AT, 1986
)
1.23
"Mass treatment with diethylcarbamazine (DEC)-medicated salt has been used in a number of places as a control measure for lymphatic filariasis. "( Diethylcarbamazine (DEC)-medicated salt for community-based control of lymphatic filariasis.
Adinarayanan, S; Critchley, J; Das, PK; Gelband, H, 2007
)
2.11
"Treatment with diethylcarbamazine reversed both the physical and lymphoscintigraphic abnormalities."( Diethylcarbamazine-induced reversal of early lymphatic dysfunction in a patient with bancroftian filariasis: assessment with use of lymphoscintigraphy.
Johnston, W; Kenney, RT; Moore, TA; Nutman, TB; Reynolds, JC, 1996
)
2.08
"Retreatment with diethylcarbamazine again caused pruritus, but this was tolerated as were subsequent treatments."( Subcutaneous nodules as a manifestation of onchocerciasis. A rare condition in the United States.
Beaver, PC; Bray, DM; Grannis, FW; Palomar, JM, 1976
)
0.58
"Treatment with diethylcarbamazine (DEC) triggered a transient increase in serum levels of filarial antigens bearing the epitope recognized by the monoclonal antibody HC 11."( Parasite antigenemia in untreated and treated lymphatic filarial infections.
Cheng, WF; Fang, RL; Piessens, WF; Tao, ZH; Xu, M; Zheng, HJ, 1990
)
0.62

Toxicity

Lymphatic filariasis has remained endemic in Fiji despite repeated mass drug administration. Ivermectin, diethylcarbamazine, and albendazole as a combination is as safe and well tolerated as DA to use in MDA campaigns with no life-threatening adverse events.

ExcerptReferenceRelevance
" In other trials, prior treatment with diethylcarbamazine (DEC) was found to potentiate the lethality of FN, while cyproheptadine (CHP) pretreatment attenuated FN's toxic effects."( A characterization of the acute cardiopulmonary toxicity of fenfluramine in the rat.
Hunsinger, RN; Wright, D,
)
0.4
" Clinical adverse reactions were recorded in four ivermectin, ten DEC and three placebo patients."( A double-blind comparison of the efficacy and safety of ivermectin and diethylcarbamazine in a placebo controlled study of Senegalese patients with onchocerciasis.
Aziz, MA; Badiane, S; Diallo, JS; Diallo, S; Diop-Mar, I; Gaxotte, P; Lariviere, M; N'Dir, O; Py, D; Schulz-Key, H, 1986
)
0.5
"464 persons of whom 189 proved to be infected with microfilariae of Wuchereria bancrofti and/or Onchocerca volvulus were examined for adverse reactions due to diethylcarbamazine, which was administered during a filariasis control campaign."( Studies on Bancroftian filariasis in Liberia, West Africa. IV. Notes on side effects observed during a diethylcarbamazine treatment campaign in a rural area endemic for Wuchereria bancrofti and Onchocerca volvulus.
Chlebowsky, HO; Zielke, E, 1980
)
0.67
" Carriers were examined and questioned regarding their experience of adverse reactions, which were graded 0 to 3 according to severity, at 6, 12 and 24 hours and at 4 days after treatment."( Safety trial of single-dose treatments with a combination of ivermectin and diethylcarbamazine in bancroftian filariasis.
Cartel, JL; Chanteau, S; Gay, VM; Glaziou, P; Martin, PM; Moulia-Pelat, JP; Nguyen, LN, 1993
)
0.52
" Eight patients did not develop any adverse reactions."( The efficacy, tolerability and safety of diethylcarbamazine-fortified salt in the treatment of the microfilaraemias of brugian filariasis: an open, hospital-based study.
Kumaraswami, V; Kuttikkal, VV; Shenoy, RK; Varghese, J, 1998
)
0.57
" All subjects experienced adverse reactions of one form or another, lasting for up to 48 h post-treatment; these included fever, myalgia, headache, and lethargy."( Treatment of microfilaraemia in asymptomatic brugian filariasis: the efficacy and safety of the combination of single doses of ivermectin and diethylcarbamazine.
George, LM; John, A; Kumaraswami, V; Shenoy, RK; Suma, TK, 1998
)
0.5
" Both DEC and ivermectin show, as expected, an adverse event profile compatible with the destruction of microfilariae."( An analysis of the safety of the single dose, two drug regimens used in programmes to eliminate lymphatic filariasis.
Addiss, DG; Awadzi, K; Beach, MJ; Belizario, VY; Dunyo, SK; Espinel, M; Gyapong, JO; Horton, J; Hossain, M; Ismail, MM; Jayakody, RL; Lammie, PJ; Lazdins, JK; Makunde, W; Ottesen, EA; Richard-Lenoble, D; Selve, B; Shenoy, RK; Simonsen, PE; Wamae, CN; Weerasooriya, MV; Witt, C, 2000
)
0.31
" It is feasible that both are due to the accumulation of toxic metabolite(s), and arene oxides may probably be considered as damaging derivatives of carbamazepine metabolism."( Carbamazepine-provoked hepatotoxicity and possible aetiopathological role of glutathione in the events. Retrospective review of old data and call for new investigation.
Kalapos, MP, 2002
)
0.31
" Both the DEC and albendazole were well tolerated when given alone or in combination, no adverse events being observed."( The pharmacokinetics, safety and tolerability of the co-administration of diethylcarbamazine and albendazole.
Arun, SR; Fleckenstein, LL; John, A; Kumaraswami, V; Na-Bangchang, K; Shenoy, RK; Suma, TK, 2002
)
0.55
" Safety was assessed by monitoring if adverse events (AEs) over 5 days affected daily acivities."( Safety, tolerability, efficacy and plasma concentrations of diethylcarbamazine and albendazole co-administration in a field study in an area endemic for lymphatic filariasis in India.
Deshmukh, PR; Fleckenstein, L; Garg, BS; Gogtay, NJ; Ingole, NS; Kadam, VS; Karbwang, J; Kirodian, BG; Kshirsagar, NA; Lazdins-Helds, JK; Mehendale, AM; Rajgor, DD, 2004
)
0.57
" viteae homogenate did not protect against adverse reactions to a subsequent microfilaricidal treatment."( Lethal LPS-independent side effects after microfilaricidal treatment in Acanthocheilonema viteae-infected rodents.
Müller, HA; Zahner, H, 2005
)
0.33
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" Adults were randomized into 2 treatment arms, DEC 6 mg/kg + ALB 400 mg (N = 12) or DEC 6 mg/kg + ALB 400 mg + IVM 200 μg/kg (N = 12), and monitored for microfilaria, parasite antigenemia, adverse events (AEs), and serum drug levels."( Efficacy, Safety, and Pharmacokinetics of Coadministered Diethylcarbamazine, Albendazole, and Ivermectin for Treatment of Bancroftian Filariasis.
Baea, M; Fleckenstein, LL; Kazura, JW; King, CL; Lombore, B; Maki, E; Sanuku, N; Satofan, S; Schmidt, MS; Siba, PM; Thomsen, EK; Weil, GJ, 2016
)
0.68
"Triple-drug therapy is safe and more effective than DEC + ALB for Bancroftian filariasis and has the potential to accelerate elimination of lymphatic filariasis."( Efficacy, Safety, and Pharmacokinetics of Coadministered Diethylcarbamazine, Albendazole, and Ivermectin for Treatment of Bancroftian Filariasis.
Baea, M; Fleckenstein, LL; Kazura, JW; King, CL; Lombore, B; Maki, E; Sanuku, N; Satofan, S; Schmidt, MS; Siba, PM; Thomsen, EK; Weil, GJ, 2016
)
0.68
" When distributing microfilaricides however, considerable care is needed to minimise the risk of severe adverse events (SAEs) in areas that are co-endemic for onchocerciasis or LF and loiasis."( Identifying co-endemic areas for major filarial infections in sub-Saharan Africa: seeking synergies and preventing severe adverse events during mass drug administration campaigns.
Basáñez, MG; Cano, J; O'Hanlon, SJ; Pullan, RL; Rebollo, MP; Tekle, AH; Wanji, S; Zouré, HG, 2018
)
0.48
"To provide context for the results of a large-scale, international safety trial of MDA using triple drug therapy, we searched Ovid Medline for studies published from 1985-2017 that reported adverse events (AEs) following treatment of LF with IVM, DEC, ALB, or any combination of these medications."( Adverse events following single dose treatment of lymphatic filariasis: Observations from a review of the literature.
Andersen, BJ; Budge, PJ; Herbert, C; Weil, GJ, 2018
)
0.48
"In this open-label cohort study, treatment-naïve microfilaremic (>50 mf/mL, n = 32) and uninfected (circulating filarial antigen negative, n = 24) adults residing in Agboville district, Côte d'Ivoire, were treated with a single dose of IVM plus DEC plus ALB, and evaluated for adverse events (AEs) until 7 days post treatment."( Pharmacokinetics, safety, and efficacy of a single co-administered dose of diethylcarbamazine, albendazole and ivermectin in adults with and without Wuchereria bancrofti infection in Côte d'Ivoire.
Bjerum, CM; Chhonker, YS; Edi, C; King, CL; Koudou, BG; Méité, A; Murry, DJ; Ouattara, AF; Penali, LK; Weil, GJ, 2019
)
0.74
" There were no severe or serious adverse events."( Pharmacokinetics, safety, and efficacy of a single co-administered dose of diethylcarbamazine, albendazole and ivermectin in adults with and without Wuchereria bancrofti infection in Côte d'Ivoire.
Bjerum, CM; Chhonker, YS; Edi, C; King, CL; Koudou, BG; Méité, A; Murry, DJ; Ouattara, AF; Penali, LK; Weil, GJ, 2019
)
0.74
" Adverse events (AEs) are common after LF treatment."( Systems analysis-based assessment of post-treatment adverse events in lymphatic filariasis.
Andersen, BJ; Curtis, K; Fischer, PU; Hertz, MI; King, CL; Kupritz, J; Meite, A; Mitreva, M; Rosa, BA; Serge, T; Weil, GJ, 2019
)
0.51
" Both treatments were well tolerated, and there were no serious adverse events."( Efficacy and Safety of a Single Dose of Ivermectin, Diethylcarbamazine, and Albendazole for Treatment of Lymphatic Filariasis in Côte d'Ivoire: An Open-label Randomized Controlled Trial.
Aboulaye, M; Andersen, BJ; Bjerum, CM; King, CL; Kouadio, O; Koudou, BG; Marius, VK; Ouattara, AF; Weil, GJ, 2020
)
0.81
"Fear of adverse events (AEs) negatively affects compliance to mass drug administration (MDA) for lymphatic filariasis (LF) elimination program."( Frequency and Clinical Significance of Localized Adverse Events following Mass Drug Administration for Lymphatic Filariasis in an Endemic Area in South India.
Krishnamoorthy, K; Kuttiatt, VS; Purushothaman, J; Somani, RK; Swaminathan, S; Weil, GJ, 2020
)
0.56
"Lymphatic filariasis has remained endemic in Fiji despite repeated mass drug administration using the well-established and safe combination of diethylcarbamazine and albendazole (DA) since 2002."( The safety of combined triple drug therapy with ivermectin, diethylcarbamazine and albendazole in the neglected tropical diseases co-endemic setting of Fiji: A cluster randomised trial.
Grobler, AC; Hardy, M; Kaldor, JM; Kama, M; King, CL; Robinson, LJ; Romani, L; Samuela, J; Steer, AC; Tuicakau, M; Weil, GJ; Whitfeld, MJ, 2020
)
1
" Participants were monitored for adverse events (AE), parasite antigenemia, and microfilaremia."( Safety and efficacy of co-administered diethylcarbamazine, albendazole and ivermectin during mass drug administration for lymphatic filariasis in Haiti: Results from a two-armed, open-label, cluster-randomized, community study.
Beau de Rochars, VM; Bogus, J; Direny, AN; Dubray, CL; Ernest, JR; Fayette, CR; Goss, CW; Hast, M; Lemoine, JF; O'Brian, K; Pavilus, GE; Sabin, DF; Sircar, AD; Weil, GJ; Wiegand, RE, 2020
)
0.83
" This paper aims to describe Samoa's experience with program coverage and adverse events (AEs) in the first round of triple-drug MDA."( A community survey of coverage and adverse events following country-wide triple-drug mass drug administration for lymphatic filariasis elimination, Samoa 2018.
Gass, K; Graves, PM; Kearns, T; Lau, CL; Mayfield, HJ; Naseri, T; Sheridan, S; Thomsen, R; Willis, GA, 2020
)
0.56
" Adverse events (AEs) were monitored actively for two days and passively for five more days."( An open label, block randomized, community study of the safety and efficacy of co-administered ivermectin, diethylcarbamazine plus albendazole vs. diethylcarbamazine plus albendazole for lymphatic filariasis in India.
Dwivedi, GP; Jambulingam, P; Krishnamoorthy, K; Kuttiatt, VS; Rahi, M; Raju, HKK; Somani, RK; Srividya, A; Subramanian, S; Suryaprakash, MK; Weil, GJ, 2021
)
0.83
" The triple therapy had a similar adverse effect compared with the dual therapy group."( Efficacy and safety of triple therapy versus dual therapy for lymphatic filariasis: A systematic review and meta-analysis.
Abd-Elsalam, S; Abdelazeem, B; Abuelazm, MT; Ashraf, M; Badr, H; Gamal, M, 2022
)
0.72
" Adverse events (AE) were assessed by active follow-up for 2 days and passive follow-up for an additional 5 days."( Safety and efficacy of mass drug administration with a single-dose triple-drug regimen of albendazole + diethylcarbamazine + ivermectin for lymphatic filariasis in Papua New Guinea: An open-label, cluster-randomised trial.
Amuga, M; Bieb, S; Bjerum, C; Goss, CW; Howard, C; John, LN; Karl, S; Kerry, Z; King, CL; Kotty, B; Kualawi, M; Kumai, S; Laman, M; Lorry, L; Makita, L; O'Brian, K; Pomat, W; Robinson, LJ; Samuel, A; Tavul, L; Tisch, DJ; Wangi, J; Weil, GJ, 2022
)
0.94
"We conducted a community-based, observational, cohort event monitoring study to compare the types, frequency, severity, and predictors of adverse events following dual versus triple therapy in 20,421 eligible residents."( Comparative Safety Surveillance of Triple (IDA) Versus Dual Therapy (DA) in Mass Drug Administration for Elimination of Lymphatic Filariasis in Kenya: A Cohort Event Monitoring Study.
Aklillu, E; Barry, A; Guantai, A; Khaemba, C; Kirui, E; Njenga, SM; Oluka, M; Omondi, WP; Parthasarathi, G, 2023
)
0.91
" Adverse events were actively monitored through house-to-house visits on days 1, 2, and 7 after MDA."( Comparative Safety Surveillance of Triple (IDA) Versus Dual Therapy (DA) in Mass Drug Administration for Elimination of Lymphatic Filariasis in Kenya: A Cohort Event Monitoring Study.
Aklillu, E; Barry, A; Guantai, A; Khaemba, C; Kirui, E; Njenga, SM; Oluka, M; Omondi, WP; Parthasarathi, G, 2023
)
0.91
"Overall, 5807 and 3102 adverse events were reported by 2839 and 1621 individuals in the IDA and DA groups, respectively."( Comparative Safety Surveillance of Triple (IDA) Versus Dual Therapy (DA) in Mass Drug Administration for Elimination of Lymphatic Filariasis in Kenya: A Cohort Event Monitoring Study.
Aklillu, E; Barry, A; Guantai, A; Khaemba, C; Kirui, E; Njenga, SM; Oluka, M; Omondi, WP; Parthasarathi, G, 2023
)
0.91
"Ivermectin, diethylcarbamazine, and albendazole as a combination is as safe and well tolerated as DA to use in MDA campaigns with no serious life-threatening adverse events."( Comparative Safety Surveillance of Triple (IDA) Versus Dual Therapy (DA) in Mass Drug Administration for Elimination of Lymphatic Filariasis in Kenya: A Cohort Event Monitoring Study.
Aklillu, E; Barry, A; Guantai, A; Khaemba, C; Kirui, E; Njenga, SM; Oluka, M; Omondi, WP; Parthasarathi, G, 2023
)
1.29
"One hundred sixty-four individuals were treated, and monitored for treatment emergent adverse events (TEAE)."( Safety and tolerability of moxidectin and ivermectin combination treatments for lymphatic filariasis in Côte d'Ivoire: A randomized controlled superiority study.
Bjerum, CM; Budge, PJ; Fischer, PU; Gabo, PT; Goss, CW; King, CL; Koudou, BG; Lew, D; Ouattara, AF; Weil, GJ, 2023
)
0.91

Pharmacokinetics

The pharmacokinetic parameters of diethylcarbamazine were compared in the plasma and peritoneal fluid of 5 non-infected rodents.

ExcerptReferenceRelevance
" The effects of other antiepileptics on the serum protein binding, erythrocyte distribution and metabolism of ZNS were also studied in vitro to elucidate the mechanism of pharmacokinetic interaction of ZNS."( Pharmacokinetic interaction of zonisamide in rats. Effect of other antiepileptics on zonisamide.
Fukuchi, H; Kimura, M; Kimura, Y; Kitaura, T; Miyake, K; Tanaka, N, 1992
)
0.28
"The pharmacokinetic parameters of diethylcarbamazine were compared in the plasma and peritoneal fluid of 5 non-infected rodents."( Experimental filariasis of Dipetalonema dessetae in Proechimys oris: 3. Effects of parasitism on the pharmacokinetics of diethylcarbamazine.
Auget, JL; Gayral, P; Jacquot, C; Kani, F; Mahuzier, G; Pfaff-Dessales, MC,
)
0.62
" 2 Selected pharmacokinetic parameters, plasma half-life (T1/2), area under the plasma concentration-time curve (AUC), elimination rate constant (Kel) and 24 h urinary excretion were regressed versus parameters indicative of renal function."( The effect of renal disease on the pharmacokinetics of diethylcarbamazine in man.
Adjepon-Yamoah, KK; Breckenridge, AM; Edwards, G; Orme, ML; Ward, SA, 1982
)
0.51
" 4 The elimination half-life (T1/2) of DEC and the area under the plasma concentration v time curve (AUC) were significantly increased when an alkaline urinary pH was maintained compared with the values of these parameters obtained on a second occasion when an acidic urinary pH was maintained."( The effect of variations in urinary pH on the pharmacokinetics of diethylcarbamazine.
Adjepon-Yamoah, KK; Breckenridge, AM; Edwards, G; Orme, ML; Ward, SA, 1981
)
0.5
" Similarly, evaluation of the pharmacokinetic properties of halofantrine has led to the demonstration that poor and erratic absorption could be just as likely to explain therapeutic failure as resistance of the parasite to effects of this drug."( Clinical pharmacokinetics in the treatment of tropical diseases. Some applications and limitations.
Edwards, G; Ward, SA; Winstanley, PA, 1994
)
0.29
"The concentration of diethylcarbamazine in saliva was used to determine pharmacokinetic parameters, in comparison to plasma and urine concentrations."( Pharmacokinetics of diethylcarbamazine: prediction by concentration in saliva.
Afonne, OJ; Chilaka, KC; Ilondu, N; Obi, E; Ofoefule, S; Orisakwe, OE; Orish, C, 2000
)
0.95
" Serum eliminating half-life was decreased upon treatment with AC (7."( Acceleration of body clearance of diethylCarbamazine by oral activated charcoal.
Afonne, OJ; Ilondu, NA; Ofoefule, SI; Orisakwe, OE; Orish, CN, 2000
)
0.59
" The method is currently being used for pharmacokinetic studies of DEC in healthy volunteers."( Gas chromatographic assay of diethylcarbamazine in human plasma for application to clinical pharmacokinetic studies.
Fleckenstein, L; Miller, JR, 2001
)
0.6
" Blood samples for pharmacokinetic study were collected at specified intervals before and after drug administration."( The pharmacokinetics, safety and tolerability of the co-administration of diethylcarbamazine and albendazole.
Arun, SR; Fleckenstein, LL; John, A; Kumaraswami, V; Na-Bangchang, K; Shenoy, RK; Suma, TK, 2002
)
0.55
"There was no difference in AUC0-inf or Cmax between LF-infected and uninfected participants (P>0."( Pharmacokinetics, safety, and efficacy of a single co-administered dose of diethylcarbamazine, albendazole and ivermectin in adults with and without Wuchereria bancrofti infection in Côte d'Ivoire.
Bjerum, CM; Chhonker, YS; Edi, C; King, CL; Koudou, BG; Méité, A; Murry, DJ; Ouattara, AF; Penali, LK; Weil, GJ, 2019
)
0.74
" Pharmacokinetic parameters were determined using standard non-compartmental analysis methods."( Pharmacokinetics of Moxidectin combined with Albendazole or Albendazole plus Diethylcarbamazine for Bancroftian Filariasis.
Alshehri, A; Bala, V; Bjerum, C; Budge, PJ; Chhonker, YS; Fischer, PU; Gabo, TP; King, CL; Koudou, BG; Meïté, A; Murry, DJ; Ouattara, AF; Weil, GJ, 2023
)
1.14

Compound-Compound Interactions

Diethylcarbamazine (DEC) combined with 400 mg albendazole (ALB) on the microfilariae (mf) of the lymphatic filarial parasite Brugia timori. No statistically significant difference in the efficacy of the two drug regimens in lowering the mf.

ExcerptReferenceRelevance
" However, the highest clearance rate was observed in persons treated with DEC at 6 mg/kg combined with ivermectin."( Reduction of Wuchereria bancrofti adult worm circulating antigen after annual treatments of diethylcarbamazine combined with ivermectin in French Polynesia.
Moulia-Pelat, JP; Nguyen, LN; Nicolas, L; Plichart, C, 1997
)
0.52
" In this double-blind, placebo-controlled study, the efficacy of local treatment of the affected limb combined with repeated doses of ivermectin or DEC, in preventing the occurrence of ADL in Brugia malayi lymphatic filariasis, was examined."( Prevention of acute adenolymphangitis in brugian filariasis: comparison of the efficacy of ivermectin and diethylcarbamazine, each combined with local treatment of the affected limb.
Kumaraswami, V; Rajan, K; Shenoy, RK; Suma, TK, 1998
)
0.51
"We report the successful implementation of a community-based lymphatic filariasis control program using annual single-dose treatment with diethylcarbamazine (DEC) in combination with albendazole."( Community empowerment in the control of lymphatic filariasis in Misima, Milne Bay Province using diethylcarbamazine in combination with albendazole.
Bwadua, S; Eddie, C; James, K; Melrose, W; Misa, M; Samuel, R; Selve, BP; Turner, P; Usurup, JP; Yad, W,
)
0.55
"The long-term effect of a single oral dose of 6 mg/kg bodyweight of diethylcarbamazine (DEC) combined with 400 mg albendazole (ALB) on the microfilariae (mf) of the lymphatic filarial parasite Brugia timori was studied on Alor island, Indonesia from April 2001 to April 2002."( Long-lasting reduction of Brugia timori microfilariae following a single dose of diethylcarbamazine combined with albendazole.
Bradley, M; Djuardi, Y; Fischer, P; Ismid, IS; Rückert, P; Supali, T,
)
0.59
" The treatment arms administered with DEC alone and DEC+ALB demonstrated long-term benefits in reducing microfilaraemia significantly (P<0."( Impact of single dose of diethylcarbamazine and other antifilarial drug combinations on bancroftian filarial infection variables: assessment after 2 years.
Dash, AP; Mani, TR; Munirathinam, A; Rajendran, R; Reuben, R; Sunish, IP, 2006
)
0.64
" These data showed no statistically significant difference in the efficacy of the two drug regimens in lowering the microfilaria reservoir, but they support the use of diethylcarbamazine combined with albendazole in mass treatment programs on the basis of greater activity against adult worms."( Efficacy of single-dose diethylcarbamazine compared with diethylcarbamazine combined with albendazole against Wuchereria bancrofti infection in Papua New Guinea.
Alpers, MP; Bockarie, MJ; Hazlett, F; Ibam, I; Kastens, W; Kazura, JW; Tavul, L; Tisch, DJ, 2007
)
0.84
" We assessed whether a single dose of doxycycline combined with the standard DEC regimen would reduce the incidence and severity of adverse reactions and increase the efficacy of standard treatment."( A single dose of doxycycline in combination with diethylcarbamazine for treatment of bancroftian filariasis.
Nuchprayoon, S; Sanprasert, V; Sujariyakul, A, 2010
)
0.62
" Albendazole (ALB) is being administered with diethyl carbamazine (DEC) in filariasis endemic areas to eliminate lymphatic filariasis (LF) and helminth infections."( Impact on prevalence of intestinal helminth infection in school children administered with seven annual rounds of diethyl carbamazine (DEC) with albendazole.
Kalimuthu, M; Kumar, VA; Munirathinam, A; Nagaraj, J; Rajendran, R; Sunish, IP; Tyagi, BK, 2015
)
0.42
" The present study was designed to investigate the possible protective effects of diethylcarbamazine (DEC) (50mg/kg, acting as an anti-inflammatory drug, interferes with the arachidonic acid metabolism) when administrated in combination with hesperidin (HDN) (200mg/kg, a flavanone glycoside with potent antioxidant and anti-inflammatory activities) against alcoholic liver fibrosis in wistar rats compared to silymarin (Sil) (100mg/kg)."( Antifibrotic effect of diethylcarbamazine combined with hesperidin against ethanol induced liver fibrosis in rats.
El-Sisi, AEE; Mohamed, DZ; Shebl, AM; Sokar, SS, 2017
)
0.99
"We included randomized controlled trials (RCTs) and cluster-RCTs that compared albendazole to placebo or no placebo, or compared albendazole combined with a microfilaricidal drug to a microfilaricidal drug alone, given to people known to have lymphatic filariasis or communities where lymphatic filariasis was known to be endemic."( Albendazole alone or in combination with microfilaricidal drugs for lymphatic filariasis.
Budhathoki, SS; Garner, P; Johnson, S; Macfarlane, CL; Richardson, M, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" In the filarial animals, the absorption rate constant and the elimination rate constant were significantly increased."( Experimental filariasis of Dipetalonema dessetae in Proechimys oris: 3. Effects of parasitism on the pharmacokinetics of diethylcarbamazine.
Auget, JL; Gayral, P; Jacquot, C; Kani, F; Mahuzier, G; Pfaff-Dessales, MC,
)
0.34
"The relative bioavailability of four different carbamazepine products, showing large differences in in vitro dissolution profiles, was studied in healthy volunteers to correlate the occurrence of side effects with a measure of the rate of absorption in vivo for bioequivalence testing."( Bioavailability of carbamazepine from four different products and the occurrence of side effects.
Barends, DM; Groen, C; Lake, OA; Mensinga, TT; Meulenbelt, J; Olling, M, 1999
)
0.3
" Relative bioavailability of carbamazepine after administration of nanoemulsion was 160% compared to unmodified substance."( Experimental investigation of pharmacodynamics and pharmacokinetics of carbamazepine nanoemulsion.
Abramov, DA; Kapitsa, IG; Kaplun, AP; Prokhorov, DI; Sariev, AK; Seifulla, RD; Shiriaeva, MV; Voronina, TA; Zhuravko, AS, 2014
)
0.4
" As part of an effort to stimulate the discovery and development of new macrofilaricides, particularly for onchocerciasis, research has recently been devoted to the development of new formulations that would afford high oral bioavailability of FBZ, paving the way for potential clinical development of this repurposed drug for the treatment of human filariases."( Flubendazole as a macrofilaricide: History and background.
Geary, TG; Mackenzie, CD; Silber, SA, 2019
)
0.51
" malayi, possibly due to reduced bioavailability in the lymphatic system."( Diethylcarbamazine mediated potentiation of emodepside induced paralysis requires TRP-2 in adult Brugia malayi.
Kashyap, SS; Martin, RJ; McHugh, MA; Robertson, AP, 2022
)
2.16

Dosage Studied

A dosage of 6 mg diethylcarbamazine citrate (DEC-C)/kg body weight was administered either daily or weekly. The results so far obtained from these pilot experiments, which are still in progress, suggest that a close approach to the eradication of filariasis from the endemic areas could be reached.

ExcerptRelevanceReference
" Levamisole at a dosage of 3 mg/kg daily for 8 days showed marked reduction in both microfilaria rate and microfilaria density and immediately thereafter mf-rate steadily increased almost up to pre-treatment level, the mf-density however showed only marginal increase."( Levamisole and mebendazole in the treatment of bancroftian infection.
Das, M; Narasimham, MV; Rao, CK; Roychowdhury, SP, 1978
)
0.26
" Amodiaquine in a total dose of 40 mg/kg appears to be macrofilaricidal, but because of the slight possibility of blood dyscrasias, mass chemotherapy with this dosage could not be recommended."( Preliminary screening of antifilarial activity of levamisole and amodiaquine on Wuchereria bancrofti.
McMahon, JE, 1979
)
0.26
" At 20 days after infection when Brugia were in the 4th larval stage, and at 8 weeks when worms were young adults, cats were divided into groups to test the efficacy of diethylcarbamazine citrate (DEC) at various dosage levels."( Effect of diethylcarbamazine citrate on fourth stage and adult Brugia malayi in cats.
Emerson, GA; Ewert, A, 1979
)
0.86
" Diethylcarbamazine citrate (DEC), a lipoxygenase inhibitor, inhibited these effects of ethanol in a dosage of 200 mg/kg."( Effects of acute ingestion of ethanol on hemodynamics and hypoxic pulmonary vasoconstriction in dogs--role of leukotrienes.
Lu, CY; Wang, DX; Yu, SB, 1992
)
1.19
"We evaluated the long term effects of three different dosage regimes of diethylcarbamazine--6, 9 and 12 mg per kg body weight--to a total of 72 mg on 93 microfilaria carriers of Brugia malayi."( Daily diethylcarbamazine for the treatment of Brugia malayi microfilaria carriers.
Krishnamoorthy, K; Panicker, KN; Prathiba, J; Sabesan, S,
)
0.84
" The results observed during the 12-month period which followed this last treatment have confirmed that (i) in terms of immediate clearance or complete negativation of microfilaremia, the efficacy of ivermectin is higher than that of DEC (at dosage of 3 or 6 mg/kg), (ii) DEC is more effective than ivermectin in sustaining the reduction of microfilaremia over a longer period of time and (iii) the efficacy of repeated single doses of either DEC 3 mg/kg or ivermectin 100 mcg/kg is much higher when given semi-annually than annually."( Compared efficacy of repeated annual and semi-annual doses of ivermectin and diethylcarbamazine for prevention of Wuchereria bancrofti filariasis in French Polynesia. Final evaluation.
Cardines, R; Cartel, JL; Martin, PM; Moulia-Pelat, JP; Nguyen Ngnoc, L; Plichart, R; Roux, JF; Spiegel, A, 1992
)
0.51
" The 5-lipoxygenase inhibitor diethylcarbamazine and the LTD4/LTE4 receptor antagonist LY 171883 markedly reduced mortality in dose-response fashion."( Effects of some nonsteroidal anti-inflammatory agents on experimental radiation pneumonitis.
Gross, NJ; Holloway, NO; Narine, KR, 1991
)
0.57
" These results indicate that incomplete drug regimens, differences in serum drug levels, and inadequate drug dosage are not the primary causes of treatment failure and suggest there is a degree of parasite tolerance for DEC."( Evidence of nonsusceptibility to diethylcarbamazine in Wuchereria bancrofti.
Dickinson, CM; Eberhard, ML; Lammie, PJ; Roberts, JM, 1991
)
0.56
" Dose-response studies showed that minoxidil sulfate is 14 times more potent than minoxidil in stimulating cysteine incorporation in cultured follicles."( Minoxidil sulfate is the active metabolite that stimulates hair follicles.
Baker, CA; Buhl, AE; Johnson, GA; Waldon, DJ, 1990
)
0.28
" All mf carriers detected after the mass blood survey were given a single course of DEC at the dosage of 6 mg/kg of body wt/day for 12 days."( Prevalence of bancroftian filariasis & its control by single course of diethyl carbamazine in a rural area in Tamil Nadu.
Balakrishnan, N; Das, LK; Mariappan, T; Pani, SP; Rajavel, AR; Ramaiah, KD; Sadanandane, C; Subramanian, S; Vanamail, P, 1989
)
0.28
"A combined weekly low dosage and short term standard dose treatment with diethylcarbamazine (DEC) to control Timorian filariasis is described."( Combined low dosage and short term standard dose treatment with diethylcarbamazine to control Timorian filariasis.
Partono, F, 1985
)
0.74
" bancrofti with this dosage schedule."( Persistence of parasite antigenemia following diethylcarbamazine therapy of bancroftian filariasis.
Ghosh, TK; Jain, DC; Santhanam, S; Sethumadhavan, KV; Weil, GJ, 1988
)
0.53
" Thirty minute infusions of DEC at respectively 100 mg, 400 mg, 2 g, 5 g, 10 g and 15 g (one dosage per dog) did not alter the hypoxic pulmonary pressor response."( Effects of diethylcarbamazine and cromolyn sodium on hypoxic pulmonary vasoconstriction in dogs.
Leeman, M; Lejeune, P; Naeije, R,
)
0.52
" Safety is increased through temporary discontinuation or dosage reduction of lithium in special risk situations."( New developments in long-term preventive therapy.
Schou, M, 1986
)
0.27
" The dose-response analysis showed significantly elevated frequencies of micronuclei (MN) for all the doses tested, but failed to show any influence of the dose on the induction of MN."( Genotoxic potential of diethylcarbamazine, an antifilarial drug.
Das, RK; Roy, B, 1988
)
0.59
" When the different dosage regimens (4 mg/kg, 6 mg/kg and 8 mg/kg) were compared at 6 and 12 months after treatment, the 6 mg/kg regimen was found to be more effective than the 4 mg/kg regimen in reducing the microfilarial count, and it produced fewer adverse reactions than the 8 mg/kg regimen."( The efficacy of annual single-dose treatment with diethylcarbamazine citrate against diurnally subperiodic bancroftian filariasis in Samoa.
Kimura, E; Penaia, L; Spears, GF, 1985
)
0.52
" The procedure was successfully applied to analysis of drug content in representative dosage forms with good accuracy."( DC polarographic assay of piperazines.
Ibrahim, FA; Rizk, MS; Walash, MI,
)
0.13
"Previous work on monkeys and on human volunteers led to the development of a schedule of diethylcarbamazine dosage suitable for the chemoprophylaxis of loiasis."( Experiments on the chemoprophylaxis of Onchocerca volvulus infection.
Duke, BO, 1968
)
0.47
" From those positive patients, 208 have received a cure of DEC at the dosage of 6 mg/kg/day during ten days."( [Lymphatic filariasis in Haiti. Results of treatment with diethylcarbamazine in the town of Limbe].
Boncy, J; Hodges, W; Raccurt, C,
)
0.38
"The results of mass treatment using low dosage diethylcarbamazine (DEC) in three small villages in West Flores, Indonesia, endemic for Brugia timori are described."( Low dosage diethylcarbamazine administered by villagers for the control of timorian filariasis.
Oemijati, S; Partono, F; Soewarta, A, 1984
)
0.91
" perstans using different dosage schedules."( Clinical trial on furapyrimidone in filariasis.
Chen, MG; Fu, S; Hua, XJ; Ren, YF; Shi, ZJ; Wang, MJ; Yuan, YZ, 1984
)
0.27
" These three dosage regimes were also associated, respectively, with 92."( Protection developed against reinfection by Dictyocaulus viviparus following anthelmintic treatment of a one-day-old primary infection in cattle.
Oakley, GA, 1981
)
0.26
"The relation between the dosage and plasma level of diethylcarbamazine (DEC) in jirds and hamsters was examined by gas-liquid chromatography."( Plasma level of diethylcarbamazine in jirds and hamsters.
Aoki, Y; Kimura, E; Nakajima, Y; Niwa, M, 1984
)
0.86
"Seventy-eight microfilaraemic patients with Wuchereria bancrofti and Brugia malayi infections were treated with various oral levamisole hydrochloride total dosage regimes of 150 to 3,150 mg and total diethylcarbamazine citrate (DEC) of 36 and 126 mg per kg body-weight."( Drug trials with levamisole hydrochloride and diethylcarbamazine citrate in Bancroftian and Malayan filariasis.
Mak, JW; Zaman, V, 1980
)
0.71
" 6 Plasma half-life, and area under the plasma concentration-time curve were increased and 24 h urinary excretion of DEC was significantly reduced in patients with chronic renal function impairment, compared with normal volunteer subjects receiving an identical dosage of DEC at acidic urinary pH."( The effect of renal disease on the pharmacokinetics of diethylcarbamazine in man.
Adjepon-Yamoah, KK; Breckenridge, AM; Edwards, G; Orme, ML; Ward, SA, 1982
)
0.51
" 5 The clinical significance of these observations is discussed both with respect to dose modification under conditions of changing urinary pH and the possibility of the manipulation of urinary pH in order to produce more effective dosage regimens."( The effect of variations in urinary pH on the pharmacokinetics of diethylcarbamazine.
Adjepon-Yamoah, KK; Breckenridge, AM; Edwards, G; Orme, ML; Ward, SA, 1981
)
0.5
"In recent years major advances have been made in the clinical pharmacology of many drugs used for the treatment of tropical diseases, particularly in the design and development of dosage regimens for the treatment of severe malaria."( Clinical pharmacokinetics in the treatment of tropical diseases. Some applications and limitations.
Edwards, G; Ward, SA; Winstanley, PA, 1994
)
0.29
" However, the higher dosage regimes gave severe reactions."( The role of primary health care in filariasis control in Indonesia.
Oemijati, S, 1993
)
0.29
" Side effects were dependent on the drug dosage irrespective of infection status."( Tolerance of diethylcarbamazine by microfilaraemic and amicrofilaraemic individuals in an endemic area of Bancroftian filariasis, Recife, Brazil.
Coutinho, A; de Andrade, LD; Dreyer, G; Figueredo-Silva, J; Lopes, E; Medeiros, Z; Noroes, J; Pires, ML; Tenorio, J,
)
0.5
" As compared to results from other studies with diethylcarbamazine and IVER at different dosages and periodicities, the dosage of IVER 400 seems the most effective; but a yearly intake might not be sufficient."( Long-term efficacy of single-dose treatment with 400 micrograms.kg-1 of ivermectin in bancroftian filariasis: results at one year.
Cartel, JL; Chanteau, S; Glaziou, P; Martin, PM; Moulia-Pelat, JP; Nguyen, LN, 1993
)
0.54
" Each zone was treated with a different dosage of the combination ivermectin (IVR) and diethylcarbamazine (DEC) as follows: (1) IVR 400 micrograms/kg plus DEC 6mg/kg, (2) IVR 400 micrograms/kg alone, (3) DEC 6 mg/kg alone (4) IVR 400 micrograms/kg plus DEC 3 mg/kg."( Advantages of an annual single dose of ivermectin 400 micrograms/kg plus diethylcarbamazine for community treatment of bancroftian filariasis.
Hascoët, H; Luquiaud, P; Moulia-Pelat, JP; Nguyen, LN; Nicolas, L,
)
0.59
"05), compared with mice dosed with CBZ alone (1,000 mg/kg/day)."( Effect of treatment with phenobarbital and stiripentol on carbamazepine-induced teratogenicity and reactive metabolite formation.
Amore, BM; Bajpai, M; Bennett, GD; Finnell, RH; Levy, RH; Slattery, JT, 1995
)
0.29
" Regardless of the DEC dosage and schedule used, all nodules contained damaged and degenerating adult worms."( Histological evidence for adulticidal effect of low doses of diethylcarbamazine in bancroftian filariasis.
Brito, C; Coutinho, A; Dreyer, G; Figueredo-Silva, J; Jungmann, P; Norões, J; Piessens, WF; Rocha, A,
)
0.37
" Vessels were exposed to thiacetarsamide and dose-response relationships were applied to methacholine and nitroglycerin."( Thiacetarsamide depresses relaxation of canine pulmonary artery in vitro.
Kaiser, L; Maksimowich, DS; Williams, JF, 1996
)
0.29
" Thus, new drugs or dosing schedules are needed to achieve the goal of killing all filarial parasites in the majority of patients."( Prolonged clearance of microfilaraemia in patients with bancroftian filariasis after multiple high doses of ivermectin or diethylcarbamazine.
Abeyewickreme, W; Dissanaike, AS; Ismail, MM; Jayasinghe, KS; Perera, CS; Premaratne, UN; Rajaratnam, HN; Sheriff, MH; Weil, GJ,
)
0.34
" Beginning 7 d later, the dosage of DEC and duration of treatment were progressively increased for 7-10 weeks."( Assessment of the efficacy of diethylcarbamazine on adult Wuchereria bancrofti in vivo.
Addiss, D; Dreyer, G; Medeiros, Z; Mendes, VG; Norões, J; Santos, A,
)
0.42
" This indicates that an annual dosage scheme is applicable to high-endemicity areas."( Efficacy of five annual single doses of diethylcarbamazine for treatment of lymphatic filariasis in Fiji.
Kimura, E; Koroivueta, J; Mataika, JU; Shimada, M, 1998
)
0.57
"1), and the means of various pharmacokinetic parameters were compared for any dosing time-related changes using a paired t-test at a probability level of 95%."( Pharmacokinetics of diethylcarbamazine after single oral dose at two different times of day in human subjects.
Boinpally, RR; Bolla, S; Devaraj, R; Jasti, BR; Poondru, S, 2002
)
0.64
"001), indicating that high total dosage of DEC is necessary for optimal reduction of active infection."( Long-term follow-up of treatment with diethylcarbamazine on anti-filarial IgG4: dosage, compliance, and differential patterns in adults and children.
Haarbrink, M; Mangali, A; Sartono, E; Terhell, AJ; van den Biggelaar, A; Yazdanbakhsh, M, 2003
)
0.59
" The results so far obtained from these pilot experiments, which are still in progress, suggest that a close approach to the eradication of filariasis from the endemic areas could be reached through the administration of diethylcarbamazine at a suitable dosage to microfilaria carriers and the simultaneous application of control measures against the vector mosquitos."( Pilot experiments in the control of bancroftian filariasis in Japan and Ryukyu.
SASA, M, 1963
)
0.43
"A six-age class dosage schedule of Diethylcarbamazine (DEC) of 50mg (1-2 years), 100mg (3-4 years), 150mg (5-8 years), 200mg (9-11 years), 250mg (12-14 years) and 300mg for above 14 years is being adopted for annual single dose MDA for LF elimination treat Wuchereria bancrofti microfilaria carriers."( Tolerability and efficacy of a three-age class dosage schedule of Diethylcarbamazine citrate (DEC) in the treatment of microfilaria carriers of Wuchereria bancrofti and its implications in mass drug administration (MDA) strategy for elimination of lymphat
Das, LK; Pani, SP; Vanamail, P, 2005
)
0.84
" However, there is no uniform pattern either in the dosage of DEC or in the use of antibiotics."( Clinicians' practices related to management of filarial adenolymphangitis and lymphoedema in Orissa, India.
Babu, BV; Kerketta, AS; Swain, BK, 2007
)
0.34
" In order to investigate the effect of aggressive therapy on Wuchereria bancrofti (Wb) microfilariae, DEC was given to 29 patients who were positive for the circulating filarial antigen (CFA) assay but did not have clinical manifestations of filariasis, at 6 mg/kg/day for 12 days and again six months later using the same dosing regimen."( Ultrastructural analysis of microfilariae of Wuchereria bancrofti obtained from persistent carriers after repeated courses of diethylcarbamazine.
Alves, LC; Araújo, HR; Brayner, FA; Cavalcanti, MG; Paiva, MH; Silva, GM; Veras, DL,
)
0.34
" Differential dosing led to seizure freedom in 64."( Higher evening antiepileptic drug dose for nocturnal and early-morning seizures.
Bergin, A; Bourgeois, BF; Guilhoto, LM; Kothare, SV; Loddenkemper, T; Vendrame, M, 2011
)
0.37
" In regions where the disease is endemic, local production and distribution of medicated salt dosed with diethylcarbamazine (DEC) has been an effective method for eradicating LF."( A low-tech analytical method for diethylcarbamazine citrate in medicated salt.
Bollman, EB; Brown, P; Huey, S; Lieberman, M; Magallon, M; Mares, D; Streit, TG; Weaver, A, 2011
)
0.86
"Adjusting MDA dosage schedules according to weight-for-age and sex may be may contribute to reduce the occurrence of adverse drug reactions in the population."( Adverse reactions following mass drug administration with diethylcarbamazine in lymphatic filariasis endemic areas in the Northeast of Brazil.
Braga, C; Costa, GM; Lima, AW; Medeiros, Z; Santos, ZC, 2012
)
0.62
" In the absence of alternative drugs, the use of higher or more frequent dosing with the existing drugs needs to be explored."( A randomized controlled trial of increased dose and frequency of albendazole with standard dose DEC for treatment of Wuchereria bancrofti microfilaremics in Odisha, India.
Dwibedi, B; Horton, J; Kar, SK; Kerketa, AS; Maharana, A; Mohanty, PC; Panda, SS; Ramachandran, CP, 2015
)
0.42
" Between August 1998 and July 1999, all individuals aged 8 months from Magoda and Mpapayu villages in north-eastern Tanzania, were administered with monthly low dose diethylcarbamazine (DEC) at a dosage of 50mg in children aged < 15 years and 100mg in adults aged ≥ 15 years."( Impact of insecticide treated mosquito nets and low dose monthly diethylcarbamazine on lymphatic filariasis infection between 1999 and 2004 in two endemic communities of north-eastern Tanzania.
Bygbjerg, IC; Gesase, S; Lemnge, MM; Mmbando, BP; Segeja, MD, 2012
)
0.81
" In particular, dosing unpredictably relative to motility phase means the gastrointestinal environment is a random variable within a defined range."( Gastrointestinal Motility Variation and Implications for Plasma Level Variation: Oral Drug Products.
Amidon, GL; Price, JC; Talattof, A, 2016
)
0.43
" This was independent of age (p = 0·27), symptomatic status (p = 0·57) and semi-annual/bi-annual dosing (p = 0·46)."( Lymphatic pathology in asymptomatic and symptomatic children with Wuchereria bancrofti infection in children from Odisha, India and its reversal with DEC and albendazole treatment.
Agrawala, BK; Das, BK; Dwibedi, B; Horton, J; Kar, SK; Ramachandran, CP, 2017
)
0.46
" bancrofti infected population exhibited lymphatic pathology which was reversible with annual dosage of DEC and albendazole."( Lymphatic pathology in asymptomatic and symptomatic children with Wuchereria bancrofti infection in children from Odisha, India and its reversal with DEC and albendazole treatment.
Agrawala, BK; Das, BK; Dwibedi, B; Horton, J; Kar, SK; Ramachandran, CP, 2017
)
0.46
"The World Health Organization (WHO) currently recommends height or age-based dosing as alternatives to weight-based dosing for mass drug administration lymphatic filariasis (LF) elimination programs."( Dosing pole recommendations for lymphatic filariasis elimination: A height-weight quantile regression modeling approach.
Dubray, C; Fischer, PU; Goss, CW; Hardy, M; Jambulingam, P; King, CL; Laman, M; Lemoine, JF; O'Brian, K; Robinson, LJ; Samuela, J; Schechtman, KB; Subramanian, S; Supali, T; Weil, GJ, 2019
)
0.51
" Weight-based dosing for diethylcarbamazine (DEC; 6 mg/kg) and ivermectin (IVM; 200 ug/kg) with tablet numbers derived from a table of weight intervals was treated as the "gold standard" for this study."( Dosing pole recommendations for lymphatic filariasis elimination: A height-weight quantile regression modeling approach.
Dubray, C; Fischer, PU; Goss, CW; Hardy, M; Jambulingam, P; King, CL; Laman, M; Lemoine, JF; O'Brian, K; Robinson, LJ; Samuela, J; Schechtman, KB; Subramanian, S; Supali, T; Weil, GJ, 2019
)
0.82
"Using a novel modeling approach, we developed a simple dosing pole that would markedly reduce underdosing for DEC and IVM in MDA programs compared to current WHO recommended height or age-based dosing."( Dosing pole recommendations for lymphatic filariasis elimination: A height-weight quantile regression modeling approach.
Dubray, C; Fischer, PU; Goss, CW; Hardy, M; Jambulingam, P; King, CL; Laman, M; Lemoine, JF; O'Brian, K; Robinson, LJ; Samuela, J; Schechtman, KB; Subramanian, S; Supali, T; Weil, GJ, 2019
)
0.51
"These results demonstrate a clear dose-response relationship for the effect of ALB on clearance of CFA and microfilaremia."( Results From 2 Cohort Studies in Central Africa Show That Clearance of Wuchereria bancrofti Infection After Repeated Rounds of Mass Drug Administration With Albendazole Alone Is Closely Linked to Individual Adherence.
Awaca-Uvon, NP; Boussinesq, M; Campillo, JT; Chesnais, CB; Kuyangisa-Simuna, G; Louya, F; Missamou, F; Pion, SDS; Tambwe, JP; Weil, GJ, 2021
)
0.62
" Recent studies showed that a single dosage of triple therapy (Ivermectin, Diethylcarbamazepine, and Albendazole) is more effective than dual therapy (Ivermectin plus Albendazole or Diethylcarbamazepine plus Albendazole) for clearing microfilaria from the blood."( Efficacy and safety of triple therapy versus dual therapy for lymphatic filariasis: A systematic review and meta-analysis.
Abd-Elsalam, S; Abdelazeem, B; Abuelazm, MT; Ashraf, M; Badr, H; Gamal, M, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
N-methylpiperazine
N-carbamoylpiperazine
[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]

Bioassays (76)

Assay IDTitleYearJournalArticle
AID1201416Antifilarial activity against Brugia malayi microfilaria assessed as reduction in motility after 5 days by MTT dye reduction assay2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1201417Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Brugia malayi microfilaria2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1201414Antifilarial activity against Brugia malayi adult worm assessed as reduction in motility after 5 days by MTT dye reduction assay2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID108407Filaricidal activity against Dipetalonema viteae in Mastomys at a dosage of 175 mg/kg x 5 administered subcutaneous1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID103499Antifilarial activity against Molinema dessetae in vivo in Proechimys oris the natural host at a dose of 200 mg/kg subcutaneously once a day for 5 days. Value is expressed as number of infected P. oris.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides.
AID108420Filaricidal activity against Brugia malayi in Mastomys at a dosage of 50 mg/kg x 5 administered intraperitoneally at a day of 81986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1079936Choleostatic 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]
AID1149795Antifilarial activity against Litomosoides carinii infected in gerbil assessed as microfilaria count at 25, 50, 100 and 200 mg/kg administered on days 0, 1, 2 and 3 respectively measured on day 11 relative to control1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Antifilarial agents. 1,2-Cyclobutanediamines as analogues of diethylcarbamazine. Status of structure-activity relationships among diethylcarbamazine analogues.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID646616Antifilarial activity against microfilariae Brugia malayi by motility assay2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: a new class of antifilarial agents.
AID1149790Antifilarial activity against Litomosoides carinii infected in gerbil assessed as microfilaria count at 25, 50, 100 and 200 mg/kg administered on days 0, 1, 2 and 3 respectively measured on day 1 relative to control1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Antifilarial agents. 1,2-Cyclobutanediamines as analogues of diethylcarbamazine. Status of structure-activity relationships among diethylcarbamazine analogues.
AID108421Filaricidal activity against Brugia malayi in Mastomys at a dosage of 50 mg/kg x 5 administered intraperitoneally at a day of 911986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID108425Filaricidal activity against Dipetalonema viteae in Mastomys at a dosage of 175 mg/kg x 5 administered subcutaneous at a day of 211986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID103502Effective concentration of compound necessary to kill 50% of infective larvae of Molinema dessetae after 7 days was determined in vitro1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides.
AID647825Antifilarial activity against adult Brugia malayi infected in jird assessed as sterilized female worm at 100 mg/kg, sc administered for 5 consecutive days measured on day 512012European journal of medicinal chemistry, Apr, Volume: 50Galactolipids from Bauhinia racemosa as a new class of antifilarial agents against human lymphatic filarial parasite, Brugia malayi.
AID625294Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in O'Brien data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1201421Antifilarial activity against Brugia malayi microfilariae infected in jird model assessed as microfilaricidal activity at 100 mg/kg, sc after 5 days measured till day 45 relative to control2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID43623Time taken for In vitro anti-filarial activity to immobilize breinlia booliati (adult worms)1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID101681Antifilarial activity against Litomosoides carinii infections in the Jird at dose 100 mg/kg administered subcutaneously1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Synthesis and antifilarial activity of N-[4-[[4-alkoxy-3-[(dialkylamino)methyl]phenyl]amino]- 2-pyrimidinyl]-N'-phenylguanidines.
AID251930Percent inhibition of filarial parasite Setaria cervi by compound at 10 ug/mL concentration; NI = no inhibition2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors.
AID646620Antifilarial activity against adult Brugia malayi by motility assay2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: a new class of antifilarial agents.
AID1201415Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Brugia malayi adult worm2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID251763Percent inhibition of filarial parasite Setaria cervi by compound at 40 ug/mL concentration2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID108419Filaricidal activity against Brugia malayi in Mastomys at a dosage of 50 mg/kg x 5 administered intraperitoneally at a day of 631986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1149793Antifilarial activity against Litomosoides carinii infected in gerbil assessed as microfilaria count at 25, 50, 100 and 200 mg/kg administered on days 0, 1, 2 and 3 respectively measured on day 9 relative to control1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Antifilarial agents. 1,2-Cyclobutanediamines as analogues of diethylcarbamazine. Status of structure-activity relationships among diethylcarbamazine analogues.
AID195835Filaricidal activity against Litomosoides carinii in cotton rats at a dosage of 6 mg/kg x 5 administered intraperitoneally at a day of 81986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID646618Growth inhibition of adult Brugia malayi by MTT assay2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: a new class of antifilarial agents.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID108426Filaricidal activity against Dipetalonema viteae in Mastomys at a dosage of 175 mg/kg x 5 administered subcutaneous at a day of 421986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID103482Antifilarial activity against Molinema dessetae in vivo against female adult worms at a dose of 200 mg/kg subcutaneously once a day for 5 days; Active1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides.
AID1079935Cytolytic 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]
AID1201419Antifilarial activity against Brugia malayi adult worm infected in jird model assessed as adulticidal activity at 100 mg/kg, sc after 5 days measured till day 45 relative to control2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID195833Filaricidal activity against Litomosoides carinii in cotton rats at a dosage of 6 mg/kg x 5 administered intraperitoneally at a day of 211986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1201420Antifilarial activity against Brugia malayi adult worm infected in jird model assessed as sterile female at 100 mg/kg, sc after 5 days measured till day 45 relative to control2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID108427Filaricidal activity against Dipetalonema viteae in Mastomys at a dosage of 175 mg/kg x 5 administered subcutaneous at a day of 81986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID75768Oral antiallergic activity in the Guinea Pig Anaphylaxis (GPA) at the dose of 200 mg/kg; 3 guinea pigs were challenged with the antigen1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antiallergy activity of N-[2-(dimethylamino)ethyl]-4-aryl-1-piperazinecarboxamide derivatives.
AID625295Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in Pfizer data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID103505Effective in vitro concentration necessary to kill 90% of infective larvae of Molinema dessetae after 7 days1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079938Chronic 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]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID108405Filaricidal activity against Brugia malayi in Mastomys at a dosage of 50 mg/kg x 5 administered intraperitoneally1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID101694Antifilarial activity against Litomosoides carinii infections in the Jird at dose 50 mg/kg administered subcutaneously1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Synthesis and antifilarial activity of N-[4-[[4-alkoxy-3-[(dialkylamino)methyl]phenyl]amino]- 2-pyrimidinyl]-N'-phenylguanidines.
AID108418Filaricidal activity against Brugia malayi in Mastomys at a dosage of 50 mg/kg x 5 administered intraperitoneally at a day of 421986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID43622Time taken for In vitro anti-filarial activity to immobilize breinlia booliati (Microfilaria)1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID1149797Antifilarial activity against Litomosoides carinii infected in cotton rat assessed as reduction of microfilaria relative to control1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Antifilarial agents. 1,2-Cyclobutanediamines as analogues of diethylcarbamazine. Status of structure-activity relationships among diethylcarbamazine analogues.
AID103491Antifilarial activity against Molinema dessetae in vivo against male adult worms at a dose of 200 mg/kg subcutaneously once a day for 5 days; Active1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides.
AID1201418Cytotoxicity against African green monkey Vero cells after 72 hrs by resazurin dye-based fluorescence assay2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID108417Filaricidal activity against Brugia malayi in Mastomys at a dosage of 50 mg/kg x 5 administered intraperitoneally at a day of 211986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID192893Filaricidal activity against Litomosoides carinii in cotton rats at a dosage of 6 mg/kg x 5 administered intraperitoneally1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID647803Antifilarial activity against adult Brugia malayi after 48 hrs by MTT assay2012European journal of medicinal chemistry, Apr, Volume: 50Galactolipids from Bauhinia racemosa as a new class of antifilarial agents against human lymphatic filarial parasite, Brugia malayi.
AID251762Percent inhibition of filarial parasite Setaria cervi by compound at 20 ug/mL concentration2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors.
AID251922Percent inhibition of filarial parasite Setaria cervi by compound at 5 ug/mL concentration; NI = no inhibition2005Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
Syntheses of 2,4,6-trisubstituted pyrimidine derivatives as a new class of antifilarial topoisomerase II inhibitors.
AID123289Lethal dose that killed mice in 48 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079933Acute 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
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079931Moderate 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]
AID647823Antifilarial activity against adult Brugia malayi infected in jird assessed as worm mortality at 100 mg/kg, sc administered for 5 consecutive days measured on day 512012European journal of medicinal chemistry, Apr, Volume: 50Galactolipids from Bauhinia racemosa as a new class of antifilarial agents against human lymphatic filarial parasite, Brugia malayi.
AID195834Filaricidal activity against Litomosoides carinii in cotton rats at a dosage of 6 mg/kg x 5 administered intraperitoneally at a day of 421986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics.
AID647804Antifilarial activity against microfilariae Brugia malayi after 48 hrs by MTT assay2012European journal of medicinal chemistry, Apr, Volume: 50Galactolipids from Bauhinia racemosa as a new class of antifilarial agents against human lymphatic filarial parasite, Brugia malayi.
AID1149791Antifilarial activity against Litomosoides carinii infected in gerbil assessed as microfilaria count at 25, 50, 100 and 200 mg/kg administered on days 0, 1, 2 and 3 respectively measured on day 3 relative to control1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Antifilarial agents. 1,2-Cyclobutanediamines as analogues of diethylcarbamazine. Status of structure-activity relationships among diethylcarbamazine analogues.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,891)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901054 (55.74)18.7374
1990's299 (15.81)18.2507
2000's275 (14.54)29.6817
2010's199 (10.52)24.3611
2020's64 (3.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 84.52

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index84.52 (24.57)
Research Supply Index7.74 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index154.31 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (84.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials194 (9.18%)5.53%
Reviews114 (5.39%)6.00%
Case Studies250 (11.83%)4.05%
Observational2 (0.09%)0.25%
Other1,554 (73.51%)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
A Cluster Randomised Trial of the Safety of Co-Administration of IDA (Ivermectin, Diethylcarbamazine and Albendazole) & Azithromycin for Integrated Treatment of Neglected Tropical Diseases [NCT03676140]Phase 320,000 participants (Actual)Interventional2018-10-01Completed
A Randomized, Placebo-controlled, Double-Blind Pilot Study of Single-Dose Humanized Anti-IL5 Antibody (Reslizumab) for the Reduction of Eosinophilia Following Diethylcarbamazine Treatment of Loa Loa Infection [NCT01111305]Phase 231 participants (Actual)Interventional2010-04-30Completed
A Pharmacokinetic and Pharmacodynamic Evaluation of Co-Administration of IDA (Ivermectin, Diethylcarbamazine and Albendazole) & Azithromycin for Integrated Treatment of Neglected Tropical Diseases [NCT03664063]Phase 242 participants (Actual)Interventional2018-09-01Completed
Effect of Albendazole Dose and Interval on Brugia Malayi Microfilarial Clearance in India: A Randomized, Open Label Study [NCT00511004]Phase 240 participants (Actual)Interventional2007-07-31Completed
A Clinical Trial to Assess the Safety and Efficacy of Moxidectin Combination Treatments vs. Ivermectin Combination Treatments for Bancroftian Filariasis [NCT04410406]Phase 3164 participants (Actual)Interventional2020-08-20Active, not recruiting
Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of Single Dose Treatment With Diethylcarbamazine, Albendazole and Ivermectin in Humans With and Without Wuchereria Bancrofti Infection in Côte d'Ivoire [NCT02845713]Phase 166 participants (Actual)Interventional2016-04-17Completed
Evaluate Triple-Drug Therapy With Diethylcarbamize (DEC), Albendazole (ALB) and Ivermectin (IVM) That Could Accelerate LF Elimination Outside of Africa [NCT01975441]Phase 2182 participants (Actual)Interventional2014-05-31Completed
Alternate Chemotherapy Regimens for the Clearance of W.Bancrofti Infection: Double Blind Randomised Clinical Trial (RCT) to Study the Efficacy of Different Co-administration and Sequential Administration [NCT02005653]Phase 4146 participants (Actual)Interventional2009-02-28Completed
Alternative Chemotherapies for Lymphatic Filariasis (LF) Treatment and Elimination in Africa [Cote d'Ivoire] [NCT02974049]189 participants (Actual)Interventional2015-01-31Completed
Safety and Efficacy of Novel Combination Regimens for Treatment of Onchocerciasis [NCT06070116]Phase 2300 participants (Anticipated)Interventional2024-01-15Not yet recruiting
Host Response to Infection and Treatment in the Filarial Diseases of Humans [NCT00001230]500 participants (Anticipated)Observational1991-03-15Recruiting
Optimization of Mass Drug Administration With Existing Drug Regimens for Lymphatic Filariasis and Onchocerciasis [NCT01905423]17,108 participants (Actual)Observational2011-05-31Completed
Studies on the Interaction Between HIV Infection, Lymphatic Filariasis and Diethylcarbamazine [NCT00295698]0 participants Interventional2001-08-31Completed
Comparison Between the Post-Treatment Reactions After Single-dose Ivermectin or DEC in Subjects With Loa Loa Infection [NCT01593722]Phase 4155 participants (Actual)Interventional2012-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00511004 (4) [back to overview]Adult Worm Burdens at 2 Years
NCT00511004 (4) [back to overview]Brugia Specific Immunoglobulin G4 (IgG4) Antibodies
NCT00511004 (4) [back to overview]Microfilarial Counts at 1 Year
NCT00511004 (4) [back to overview]Microfilarial Levels at 2 Years
NCT01111305 (4) [back to overview]Frequency of AE's
NCT01111305 (4) [back to overview]Peak Eosinophil Count Post-treatment
NCT01111305 (4) [back to overview]Markers of Eosinophil Activation
NCT01111305 (4) [back to overview]Proportion of Subjects Who Clear Blood Microfilariae
NCT01593722 (5) [back to overview]Proportion of Subjects Who Clear Microfilaremia
NCT01593722 (5) [back to overview]The Frequency of Adverse Events
NCT01593722 (5) [back to overview]The Peak % of Baseline Eosinophil Count Measured During the First 7 Days Post-treatment.
NCT01593722 (5) [back to overview]Treatment Efficacy
NCT01593722 (5) [back to overview]Eosinophil Activation
NCT01905423 (6) [back to overview]Prevalence of Ascaris Infection
NCT01905423 (6) [back to overview]Prevalence of Circulating Filarial Antigen in Blood as Determined by ICT Card Test
NCT01905423 (6) [back to overview]Prevalence of Hookworm Infection
NCT01905423 (6) [back to overview]Prevalence of Microfilaria in Blood as Determined by Microscopy of Participant Blood
NCT01905423 (6) [back to overview]Prevalence of Positive Brugia Rapid Antifilarial Antibody Tests
NCT01905423 (6) [back to overview]Prevalence of Trichuris Infection

Adult Worm Burdens at 2 Years

Doppler detected worm nests at 2 years (NCT00511004)
Timeframe: 2 years from the time enrolled.

InterventionNumber of nests (Median)
Standard Therapy Annual DEC/ALB0
High Dose Annual DEC/ALB0
High Dose Semiannual DEC/ALB0

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Brugia Specific Immunoglobulin G4 (IgG4) Antibodies

IgG4 antibodies directed against Brugia malayi antigen (NCT00511004)
Timeframe: 2 years

Interventionng/ml (Median)
Standard Therapy Annual DEC/ALB150
High Dose Annual DEC/ALB224
High Dose Semiannual DEC/ALB128

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Microfilarial Counts at 1 Year

Night time microfilarial counts at 1 year (NCT00511004)
Timeframe: 1 year from time enrolled

InterventionMF/ML (Median)
Standard Therapy Annual DEC/ALB0
High Dose Annual DEC/ALB0
High Dose Semiannual DEC/ALB0

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Microfilarial Levels at 2 Years

Night time microfilarial levels at 2 years (NCT00511004)
Timeframe: 2 years from time enrolled

InterventionMF/ML (Median)
Diethylcarbamazine/Albendazole -STD0
Diethylcarbamazine/Albendazole- HD10
Diethylcarbamazine/Albendazole-HD20

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Frequency of AE's

Adverse events during the first week of DEC treatment (NCT01111305)
Timeframe: 7 days following initiation of DEC treatment

Interventionadverse events (Number)
Reslizumab + DEC29
Placebo + DEC28

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Peak Eosinophil Count Post-treatment

Peak eosinophil count during the first 7 days of treatment as a percent of the baseline count (NCT01111305)
Timeframe: during the first 7 days of DEC treatment

Interventionpercent of baseline eosinophil count (Geometric Mean)
Reslizumab + DEC61
Placebo + DEC245.6

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Markers of Eosinophil Activation

serum eosinophil granule protein levels on day 7 measured as % baseline (NCT01111305)
Timeframe: one week

,
Intervention% change (Geometric Mean)
% day 0 EDN at day 7% day 0 EPO at day 7
Placebo + DEC377203
Reslizumab + DEC115138

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Proportion of Subjects Who Clear Blood Microfilariae

(NCT01111305)
Timeframe: 3, 7, and 28 days after initiation of treatment with DEC

,
InterventionParticipants (Count of Participants)
3 days7 days28 days
Placebo244
Reslizumab244

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Proportion of Subjects Who Clear Microfilaremia

(NCT01593722)
Timeframe: 14 days

Interventionparticipants (Number)
Diethylcarbamazine3
Ivermectin0

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The Frequency of Adverse Events

Symptoms, signs and laboratory abnormalities occurring in the 7 days post-treatment (NCT01593722)
Timeframe: 7 days

Interventionevents (Number)
Diethylcarbamazine115
Ivermectin103

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The Peak % of Baseline Eosinophil Count Measured During the First 7 Days Post-treatment.

(NCT01593722)
Timeframe: 7 days

Interventionpercentage of baseline (Geometric Mean)
Diethylcarbamazine196
Ivermectin165

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Treatment Efficacy

Proportion of subjects without signs of infection (NCT01593722)
Timeframe: 6 months

Interventionparticipants (Number)
Diethylcarbamazine0
Ivermectin1

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Eosinophil Activation

Levels of surface marker expression on eosinophils (NCT01593722)
Timeframe: 3 days

,
Intervention% cells expressing CD69 (Geometric Mean)
%CD69 expression on eosinophils at peak%CD69 expression on eosinophils at baseline
Single Dose DEC21.51.7
Single Dose IVM21.51.5

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Prevalence of Ascaris Infection

Prevalence of Ascaris infection is defined by the number of participants with any Ascaris worm eggs present in their stool sample as analyzed with microscopy. (NCT01905423)
Timeframe: 2 Years

,,,,
InterventionParticipants (Count of Participants)
BaselineYear 1Year 2
Lewomada (1x Annual MDA)561718
Paga (1x Annual MDA)88135107
Pekalongan (1x Annual MDA)19110
Pekalongan (2x Annual MDA)5860
Pruda (2x Annual MDA)3473

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Prevalence of Circulating Filarial Antigen in Blood as Determined by ICT Card Test

"Prevalence of filarial antigenemia (detected with the Binax Filariasis Now card test ICT card test) among the population surveyed. Prevalence data are expressed as %." (NCT01905423)
Timeframe: 3 years

,,,,
InterventionParticipants (Count of Participants)
BaselineYear 1Year 2Year 3
Lewomada (1x Annual MDA)47121336
Paga (1x Annual MDA)14020
Pekalongan (1x Annual MDA)1185100
Pekalongan (2x Annual MDA)1026300
Pruda (2x Annual MDA)2359110672

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Prevalence of Hookworm Infection

Prevalence of hookworm infection is defined by the number of participants with any hookworm eggs present in their stool sample as analyzed with microscopy. (NCT01905423)
Timeframe: 2 years

,,,,
InterventionParticipants (Count of Participants)
BaselineYear 1Year 2
Lewomada (1x Annual MDA)22611897
Paga (1x Annual MDA)2511865
Pekalongan (1x Annual MDA)000
Pekalongan (2x Annual MDA)000
Pruda (2x Annual MDA)359087

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Prevalence of Microfilaria in Blood as Determined by Microscopy of Participant Blood

Microfilariae (filarial parasites) will be detected in blood smears by microscopy. Samples will be collected in annual and semiannual community surveys. Prevalence rates (a measure of the disease rates in the population sampled) are expressed as % positive for microfilaremia (having microfilaria in the blood). (NCT01905423)
Timeframe: 3 years

,,,,
InterventionParticipants (Count of Participants)
Baseline (pre-MDA)Year 1Year 2Year 3
Lewomada (1x Annual MDA)36963
Paga (1x Annual MDA)541160
Pekalongan (1x Annual MDA)462800
Pekalongan (2x Annual MDA)453000
Pruda (2x Annual MDA)146371512

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Prevalence of Positive Brugia Rapid Antifilarial Antibody Tests

This outcome is reported as the frequency of participants with positive Brugia Rapid antifilarial antibody tests. Data was only collected at baseline and at year 3 for this outcome measure and no antibody data was collected for the Pekalongan study sites. (NCT01905423)
Timeframe: 3 years

,,,,
InterventionParticipants (Count of Participants)
BaselineYear 1Year 2Year 3
Lewomada (1x Annual MDA)22916813436
Paga (1x Annual MDA)1750016
Pekalongan (1x Annual MDA)0000
Pekalongan (2x Annual MDA)0000
Pruda (2x Annual MDA)2970037

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Prevalence of Trichuris Infection

Prevalence of trichuris infection is defined by the number of participants with any trichuris worm eggs present in their stool sample as analyzed with microscopy. (NCT01905423)
Timeframe: 2 years

,,,,
InterventionParticipants (Count of Participants)
BaselineYear 1Year 2
Lewomada (1x Annual MDA)452523
Paga (1x Annual MDA)689384
Pekalongan (1x Annual MDA)120350
Pekalongan (2x Annual MDA)352650
Pruda (2x Annual MDA)8813

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