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Pyrimethamine
drug data and news
Pyrimethamine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Pyrimethamine | ||
| Brand Names/Synonyms | 4753 R.P.; BW 5063; CD; Chloridin; Chloridine; Chloridyn; Darachlor; Daraclor; Darapram; Daraprim; Daraprime; Diaminopyritamin; Disulone; Erbaprelina; Ethylpyrimidine; Fansidar; Khloridin; Malacid; Malocid; Malocide; Maloprim; NSC-3061; Pirimecidan; Pirimetamin; Pirimetamina; Primethamine; Pyremethamine; Pyrimethamin; Pyrimethamine; Pyrimethamine Hcl; RP 4753; Tindurin; Tinduring; WR 2978 | ||
| Indication | For the treatment of toxoplasmosis and acute malaria; For the prevention of malaria in areas non-resistant to pyrimethamine | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Pyrimethamine is an antiparasitic compound commonly used as an adjunct in the treatment of uncomplicated, chloroquine resistant, P. falciparum malaria. Pyrimethamine is a folic acid antagonist 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. However, the 4-amino-quinoline compounds are more effective against the erythrocytic schizonts. It does not destroy gametocytes, but arrests sporogony in the mosquito. The action of pyrimethamine against Toxoplasma gondii is greatly enhanced when used in conjunction with sulfonamides. | ||
| Mechanism Of Action | Pyrimethamine inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication. This leads to failure of nuclear division at the time of schizont formation in erythrocytes and liver. | ||
| Pyrimethamine News (When available) |
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| Dosage Forms | TABLET | ||
| Drug_Category | Antiprotozoals; Antimalarials; Folic Acid Antagonists; ATC:P01BD01 | ||
| Absorption | Well absorbed with peak levels occurring between 2 to 6 hours following administration | ||
| Interactions |
-->Interactions for Pyrimethamine: Pyrimethamine may be used with sulfonamides, quinine and other antimalarials, and with other antibiotics. However, the concomitant use of other antifolic drugs or agents associated with myelosuppression including sulfon-amides or trimethoprim-sulfamethoxazole combinations, proguanil, zidovudine, or cytostatic agents (e.g., methotrex-ate) while the patient is receiving pyrimethamine, may increase the risk of bone marrow suppression. If signs of folate deficiency develop, pyrimethamine should be discontinued. Folinic acid (leucovorin) should be administered until normal hematopoiesis is restored. Mild hepatotoxicity has been reported in some patients when lorazepam and pyrimethamine were administered concomitantly. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 5-(4-chlorophenyl)-6-ethyl-pyrimidine-2,4-diamine | ||
| Chemical Formula | C12H13ClN4 | ||
| Molecular Weight | 248.711 g/mol | ||
| Smiles String | CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl | ||
| Melting Point | 233.5 °C | ||
| Water Solubility | 121 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 2.607 | ||
| Isoelectric Point | 7.34 | ||
| Biotransformation | Hepatic | ||
| Half Life | 96 hours | ||
| Protein Binding [%] | 87% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Pyrimethamine.html http://www.rxlist.com/cgi/generic2/pyrime.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00599 | ||
| CAS Registry Number | 58-14-0 | ||
| KEGG Compound ID | C07391 | ||
| PubChem ID | SID:9595 | ||
| PharmGKB ID | PA451193 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 4774 |
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