Details
Stereochemistry | ACHIRAL |
Molecular Formula | C12H13ClN4 |
Molecular Weight | 248.711 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1=C(C(N)=NC(N)=N1)C2=CC=C(Cl)C=C2
InChI
InChIKey=WKSAUQYGYAYLPV-UHFFFAOYSA-N
InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17)
Molecular Formula | C12H13ClN4 |
Molecular Weight | 248.711 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9554869
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9554869
Pyrimethamine, sold under the trade name Daraprim, is one of the folic acid antagonists that is used as an antimalarial or with a sulfonamide to treat toxoplasmosis. In addition it was approved in Chemoprophylaxis of Malaria. However, resistance to pyrimethamine is prevalent worldwide. It is not suitable as a prophylactic agent for travelers to most areas. Pyrimethamine is well absorbed with peak levels occurring between 2 to 6 hours following administration. It is eliminated slowly and has a plasma half-life of approximately 96 hours. Pyrimethamine is 87% bound to human plasma proteins. Pyrimethamine acts by selectively inhibiting malarial dihydrofolate reductase-thymidylate synthase and the rationale for its therapeutic action is based on the differential requirement between host and parasite for nucleic acid precursors involved in growth. This activity is highly selective against plasmodia and Toxoplasma gondii. Pyrimethamine possesses blood schizonticidal and some tissue schizonticidal activity against malaria parasites of humans. The action of pyrimethamine against Toxoplasma gondii is greatly enhanced when used in conjunction with sulfonamides.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1939 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9554869 |
1.5 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | DARAPRIM Approved UseTreatment of Toxoplasmosis: DARAPRIM is indicated for the treatment of toxoplasmosis when used conjointly with a sulfonamide, since synergism exists with this combination. Treatment of Acute Malaria: DARAPRIM is also indicated for the treatment of acute malaria. It should not be used alone to treat acute malaria. Fast-acting schizonticides such as chloroquine or quinine are indicated and preferable for the treatment of acute malaria. However, conjoint use of DARAPRIM with a sulfonamide (e.g., sulfadoxine) will initiate transmission control and suppression of susceptible strains of plasmodia. Chemoprophylaxis of Malaria: DARAPRIM is indicated for the chemoprophylaxis of malaria due to susceptible strains of plasmodia. However, resistance to pyrimethamine is prevalent worldwide. It is not suitable as a prophylactic agent for travelers to most areas. Launch Date-5.34556803E11 |
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Curative | DARAPRIM Approved UseTreatment of Toxoplasmosis: DARAPRIM is indicated for the treatment of toxoplasmosis when used conjointly with a sulfonamide, since synergism exists with this combination. Treatment of Acute Malaria: DARAPRIM is also indicated for the treatment of acute malaria. It should not be used alone to treat acute malaria. Fast-acting schizonticides such as chloroquine or quinine are indicated and preferable for the treatment of acute malaria. However, conjoint use of DARAPRIM with a sulfonamide (e.g., sulfadoxine) will initiate transmission control and suppression of susceptible strains of plasmodia. Chemoprophylaxis of Malaria: DARAPRIM is indicated for the chemoprophylaxis of malaria due to susceptible strains of plasmodia. However, resistance to pyrimethamine is prevalent worldwide. It is not suitable as a prophylactic agent for travelers to most areas. Launch Date-5.34556803E11 |
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Preventing | DARAPRIM Approved UseTreatment of Toxoplasmosis: DARAPRIM is indicated for the treatment of toxoplasmosis when used conjointly with a sulfonamide, since synergism exists with this combination. Treatment of Acute Malaria: DARAPRIM is also indicated for the treatment of acute malaria. It should not be used alone to treat acute malaria. Fast-acting schizonticides such as chloroquine or quinine are indicated and preferable for the treatment of acute malaria. However, conjoint use of DARAPRIM with a sulfonamide (e.g., sulfadoxine) will initiate transmission control and suppression of susceptible strains of plasmodia. Chemoprophylaxis of Malaria: DARAPRIM is indicated for the chemoprophylaxis of malaria due to susceptible strains of plasmodia. However, resistance to pyrimethamine is prevalent worldwide. It is not suitable as a prophylactic agent for travelers to most areas. Launch Date-5.34556803E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.059 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/8726001 |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: Zidovudine |
PYRIMETHAMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
502.9 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/8726001 |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: Zidovudine |
PYRIMETHAMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
190.56 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/8726001 |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: Zidovudine |
PYRIMETHAMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
13% |
PYRIMETHAMINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1.625 g single, oral Overdose Dose: 1.625 g Route: oral Route: single Dose: 1.625 g Sources: Page: p.19 |
healthy, 1 n = 1 Health Status: healthy Age Group: 1 Sex: M Population Size: 1 Sources: Page: p.19 |
Disc. AE: Vomiting, Convulsions... AEs leading to discontinuation/dose reduction: Vomiting Sources: Page: p.19Convulsions (severe) Cyanosis |
625 mg single, oral Overdose Dose: 625 mg Route: oral Route: single Dose: 625 mg Sources: Page: p.19 |
healthy, 1 n = 1 Health Status: healthy Age Group: 1 Population Size: 1 Sources: Page: p.19 |
Disc. AE: Convulsions, Respiratory failure... AEs leading to discontinuation/dose reduction: Convulsions Sources: Page: p.19Respiratory failure (grade 5) |
1.2 g single, oral Overdose Dose: 1.2 g Route: oral Route: single Dose: 1.2 g Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: M Population Size: 1 Sources: Page: p.19 |
Disc. AE: Cyanosis, Vomiting... AEs leading to discontinuation/dose reduction: Cyanosis Sources: Page: p.19Vomiting (severe) Convulsions Apnoea Haematemesis Cardiac failure (grade 5) |
400 mg single, oral Overdose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: F Population Size: 1 Sources: Page: p.19 |
Disc. AE: Convulsions, Vomiting... AEs leading to discontinuation/dose reduction: Convulsions (severe) Sources: Page: p.19Vomiting Cyanosis Collapse |
625 mg single, oral Overdose Dose: 625 mg Route: oral Route: single Dose: 625 mg Sources: Page: p.19 |
healthy, 3 n = 1 Health Status: healthy Age Group: 3 Sex: F Population Size: 1 Sources: Page: p.19 |
Disc. AE: Convulsions, Unconsciousness... AEs leading to discontinuation/dose reduction: Convulsions (grade 5) Sources: Page: p.19Unconsciousness (grade 5) |
300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Disc. AE: Convulsions, Abdominal pain... AEs leading to discontinuation/dose reduction: Convulsions Sources: Page: p.3Abdominal pain Nausea Vomiting (severe) Excitability Respiratory depression (grade 5) Circulatory collapse (grade 5) |
75 mg 1 times / day multiple, oral (max) Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: Page: p.2 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.2 |
Disc. AE: Folate deficiency... AEs leading to discontinuation/dose reduction: Folate deficiency Sources: Page: p.2 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Cyanosis | Disc. AE | 1.625 g single, oral Overdose Dose: 1.625 g Route: oral Route: single Dose: 1.625 g Sources: Page: p.19 |
healthy, 1 n = 1 Health Status: healthy Age Group: 1 Sex: M Population Size: 1 Sources: Page: p.19 |
Vomiting | Disc. AE | 1.625 g single, oral Overdose Dose: 1.625 g Route: oral Route: single Dose: 1.625 g Sources: Page: p.19 |
healthy, 1 n = 1 Health Status: healthy Age Group: 1 Sex: M Population Size: 1 Sources: Page: p.19 |
Convulsions | severe Disc. AE |
1.625 g single, oral Overdose Dose: 1.625 g Route: oral Route: single Dose: 1.625 g Sources: Page: p.19 |
healthy, 1 n = 1 Health Status: healthy Age Group: 1 Sex: M Population Size: 1 Sources: Page: p.19 |
Convulsions | Disc. AE | 625 mg single, oral Overdose Dose: 625 mg Route: oral Route: single Dose: 625 mg Sources: Page: p.19 |
healthy, 1 n = 1 Health Status: healthy Age Group: 1 Population Size: 1 Sources: Page: p.19 |
Respiratory failure | grade 5 Disc. AE |
625 mg single, oral Overdose Dose: 625 mg Route: oral Route: single Dose: 625 mg Sources: Page: p.19 |
healthy, 1 n = 1 Health Status: healthy Age Group: 1 Population Size: 1 Sources: Page: p.19 |
Apnoea | Disc. AE | 1.2 g single, oral Overdose Dose: 1.2 g Route: oral Route: single Dose: 1.2 g Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: M Population Size: 1 Sources: Page: p.19 |
Convulsions | Disc. AE | 1.2 g single, oral Overdose Dose: 1.2 g Route: oral Route: single Dose: 1.2 g Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: M Population Size: 1 Sources: Page: p.19 |
Cyanosis | Disc. AE | 1.2 g single, oral Overdose Dose: 1.2 g Route: oral Route: single Dose: 1.2 g Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: M Population Size: 1 Sources: Page: p.19 |
Haematemesis | Disc. AE | 1.2 g single, oral Overdose Dose: 1.2 g Route: oral Route: single Dose: 1.2 g Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: M Population Size: 1 Sources: Page: p.19 |
Cardiac failure | grade 5 Disc. AE |
1.2 g single, oral Overdose Dose: 1.2 g Route: oral Route: single Dose: 1.2 g Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: M Population Size: 1 Sources: Page: p.19 |
Vomiting | severe Disc. AE |
1.2 g single, oral Overdose Dose: 1.2 g Route: oral Route: single Dose: 1.2 g Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: M Population Size: 1 Sources: Page: p.19 |
Collapse | Disc. AE | 400 mg single, oral Overdose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: F Population Size: 1 Sources: Page: p.19 |
Cyanosis | Disc. AE | 400 mg single, oral Overdose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: F Population Size: 1 Sources: Page: p.19 |
Vomiting | Disc. AE | 400 mg single, oral Overdose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: F Population Size: 1 Sources: Page: p.19 |
Convulsions | severe Disc. AE |
400 mg single, oral Overdose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: Page: p.19 |
healthy, 2 n = 1 Health Status: healthy Age Group: 2 Sex: F Population Size: 1 Sources: Page: p.19 |
Convulsions | grade 5 Disc. AE |
625 mg single, oral Overdose Dose: 625 mg Route: oral Route: single Dose: 625 mg Sources: Page: p.19 |
healthy, 3 n = 1 Health Status: healthy Age Group: 3 Sex: F Population Size: 1 Sources: Page: p.19 |
Unconsciousness | grade 5 Disc. AE |
625 mg single, oral Overdose Dose: 625 mg Route: oral Route: single Dose: 625 mg Sources: Page: p.19 |
healthy, 3 n = 1 Health Status: healthy Age Group: 3 Sex: F Population Size: 1 Sources: Page: p.19 |
Abdominal pain | Disc. AE | 300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Convulsions | Disc. AE | 300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Excitability | Disc. AE | 300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Nausea | Disc. AE | 300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Circulatory collapse | grade 5 Disc. AE |
300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Respiratory depression | grade 5 Disc. AE |
300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Vomiting | severe Disc. AE |
300 mg single, oral (min) Overdose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.3 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.3 |
Folate deficiency | Disc. AE | 75 mg 1 times / day multiple, oral (max) Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: Page: p.2 |
unhealthy Health Status: unhealthy Condition: Toxoplasmosis Sources: Page: p.2 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
inconclusive [Activation 10 uM] | ||||
inconclusive [Activation 39.8107 uM] | ||||
inconclusive [Activation 5.0119 uM] | ||||
inconclusive [Activation 7.9433 uM] | ||||
inconclusive [Activation >10 uM] | ||||
no [Activation >10 uM] | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/12451431/ |
no | |||
no | ||||
weak [IC50 200.1 uM] | ||||
yes [IC50 0.131 uM] | ||||
yes [IC50 1.8 uM] | ||||
yes [IC50 4.55 uM] | ||||
yes [IC50 45.1 uM] | ||||
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no |
PubMed
Title | Date | PubMed |
---|---|---|
[Pyrimethamine-induced megaloblatic anemia in florid toxoplasmosis]. | 1976 Feb 13 |
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In vivo assessment of antimicrobial agents against Toxoplasma gondii by quantification of parasites in the blood, lungs, and brain of infected mice. | 1990 Aug |
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Pneumocystis carinii dihydrofolate reductase used to screen potential antipneumocystis drugs. | 1991 Jul |
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Treatment of experimental pneumocystosis: review of 7 years of experience and development of a new system for classifying antimicrobial drugs. | 1992 Sep |
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The effect of artesunate combined with standard antimalarials against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum in vitro. | 1999 Jul-Aug |
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Anti-toxoplasma activities of antiretroviral drugs and interactions with pyrimethamine and sulfadiazine in vitro. | 2000 Sep |
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Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. | 2001 Jan |
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Activity of gatifloxacin alone or in combination with pyrimethamine or gamma interferon against Toxoplasma gondii. | 2001 Jan |
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A trial of proguanil-dapsone in comparison with sulfadoxine-pyrimethamine for the clearance of Plasmodium falciparum infections in Tanzania. | 2001 Jul-Aug |
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[Therapeutic potential of protein kinase CK2 modulators]. | 2002 |
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Inhibition of glutathione S-transferases by antimalarial drugs possible implications for circumventing anticancer drug resistance. | 2002 Feb 10 |
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In vitro activities of pentamidine, pyrimethamine, trimethoprim, and sulfonamides against Aspergillus species. | 2002 Jun |
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Selection of drugs to test the specificity of the Tg.AC assay by screening for induction of the gadd153 promoter in vitro. | 2003 Aug |
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Effect of immunomodulator daraprim on potentiation of vaccine protection of leishmania major in BALB/c mice. | 2003 Mar |
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[Disulone]. | 2004 Dec |
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Patterns of resistance and DHFR/DHPS genotypes of Plasmodium falciparum in rural Tanzania prior to the adoption of sulfadoxine-pyrimethamine as first-line treatment. | 2004 Jun |
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Dapsone hypersensitivity syndrome masquerading as a viral exanthem: three cases and a mini-review. | 2004 May |
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Pyrimethamine (2,4-diamino-5-p-chlorophenyl-6-ethylpyrimidine) induces apoptosis of freshly isolated human T lymphocytes, bypassing CD95/Fas molecule but involving its intrinsic pathway. | 2005 Dec |
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Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
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Sulfonamide crystals and acute renal failure. | 2006 Jun |
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Presumed dapsone-induced drug hypersensitivity syndrome causing reversible hypersensitivity myocarditis and thyrotoxicosis. | 2006 Nov |
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Suppression of telomerase activity by pyrimethamine: implication to cancer. | 2007 Oct |
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A comparison of vitamin A and leucovorin for the prevention of methotrexate-induced micronuclei production in rat bone marrow. | 2008 Dec |
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Anti-toxoplasmosis effects of oleuropein isolated from Fraxinus rhychophylla. | 2008 Dec |
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Impact of placental Plasmodium falciparum malaria on pregnancy and perinatal outcome in sub-Saharan Africa: part III: placental malaria, maternal health, and public health. | 2008 Mar |
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Changes in malaria indices between 1999 and 2007 in The Gambia: a retrospective analysis. | 2008 Nov 1 |
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Antifolate activity of pyrimethamine enhances temozolomide-induced cytotoxicity in melanoma cells. | 2009 May |
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Self-reported data: a major tool to assess compliance with anti-malarial combination therapy among children in Senegal. | 2009 Nov 17 |
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Cost effectiveness of seasonal intermittent preventive treatment using amodiaquine & artesunate or sulphadoxine-pyrimethamine in Ghanaian children. | 2010 Aug 17 |
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In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models. | 2013 |
|
A new protoberberine alkaloid from Meconopsis simplicifolia (D. Don) Walpers with potent antimalarial activity against a multidrug resistant Plasmodium falciparum strain. | 2013 Dec 12 |
|
Synthesis, characterization and antimalarial activity of quinoline-pyrimidine hybrids. | 2013 Jan 1 |
Patents
Sample Use Guides
Toxoplasmosis: The adult starting dose is 50 to 75 mg of the drug daily, together with 1 to 4 g daily of a sulfonamide of the sulfapyrimidine type, e.g., sulfadoxine. This dosage is ordinarily continued for 1 to 3 weeks, depending on the response of the patient and tolerance to therapy. The dosage may then be reduced to about one half that previously given for each drug and continued for an additional 4 to 5 weeks.
The pediatric dosage of DARAPRIM (PYRIMETHAMINE) is 1 mg/kg/day divided into 2 equal daily doses; after 2 to 4 days this dose may be reduced to one half and continued for approximately 1 month. The usual pediatric sulfonamide dosage is used in conjunction with DARAPRIM.
Treatment of Acute Malaria: at a dosage of 25 mg daily for 2 days with a sulfonamide will initiate transmission control and suppression of non-falciparum malaria. The adult dosage for acute malaria is 50 mg for 2 days; children 4 through 10 years old may be given 25 mg daily for 2 days. In any event, clinical cure should be followed by the once-weekly regimen described below for chemoprophylaxis. Regimens which include suppression should be extended through any characteristic periods of early recrudescence and late relapse, i.e., for at least 10 weeks in each case.
For Chemoprophylaxis of Malaria: Adults and pediatric patients over 10 years — 25 mg (1 tablet) once weekly. Children 4 through 10 years — 12.5 mg (1/2 tablet) once weekly. Infants and children under 4 years — 6.25 mg (1/4 tablet) once weekly.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18392083
Curator's Comment: The cytotoxic influence of Pyrimethamine on prostate cell line was investigated using an in vitro colometric assay. Cytotoxicity analysis of pyrimethamine revealed a dose-dependent fashion. An apoptotic influence of pyrimethamine was also confirmed by data obtained from TUNEL assay. Dose-dependent inhibitory effect on matrix metalloproteinases (MMP) was seen in pyrimethamine. A potent inhibitory effect of pyrimethamine was also established by data achieved from TRAPeze telomerase detection kit.
Unknown
Substance Class |
Chemical
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Record UNII |
Z3614QOX8W
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Validated (UNII)
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Classification Tree | Code System | Code | ||
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LIVERTOX |
NBK548044
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NDF-RT |
N0000000191
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NDF-RT |
N0000000191
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WHO-ATC |
P01BD51
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NDF-RT |
N0000175934
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WHO-ESSENTIAL MEDICINES LIST |
6.5.3.1 (SUL/PYR)
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FDA ORPHAN DRUG |
232206
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EPA PESTICIDE CODE |
600071
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WHO-ESSENTIAL MEDICINES LIST |
6.5.4
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IARC | Pyrimethamine | ||
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NCI_THESAURUS |
C271
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NCI_THESAURUS |
C2153
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WHO-ATC |
P01BF04
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CFR |
21 CFR 520.2215
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WHO-VATC |
QP51AX51
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WHO-ATC |
P01BD01
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M9368
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PRIMARY | Merck Index | ||
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D011739
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Z3614QOX8W
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1589007
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4993
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CHEMBL36
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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PYRIMETHAMINE
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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PRIMARY | Description: A white, crystalline powder; odourless. Solubility: Practically insoluble in water; slightly soluble in ethanol (~750 g/l) TS and acetone R. Category: Antimalarial. Storage: Pyrimethamine should be kept in a well-closed container, protected from light. Definition: Pyrimethamine contains not less than 99.0% and not more than 101.0% of C12H13ClN4, calculated with reference to the dried substance. | ||
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PYRIMETHAMINE
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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2215
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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9010
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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58-14-0
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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8673
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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4800
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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DB00205
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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Z3614QOX8W
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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SUB10169MIG
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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C788
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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3061
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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DTXSID9021217
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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100000080868
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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200-364-2
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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Pyrimethamine
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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Sulfadoxine and Pyrimethamine
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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2332
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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8042
Created by
admin on Wed Jul 05 22:51:55 UTC 2023 , Edited by admin on Wed Jul 05 22:51:55 UTC 2023
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT |
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BINDER->LIGAND |
BINDING
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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