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pyrimethamine

Structure via PubChem · Public domain (PubChem)

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pyrimethamine

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Also known as Daraprim®, GNF-Pf-5586, TCMDC-125860, Primethamine, Chloridyn, Chloridine, CD, Ethylpyrimidine

Pyrimethamine, sold under the brand name Daraprim among others, is a medication used with leucovorin (leucovorin is used to decrease side effects of pyrimethamine; it does not have intrinsic anti-parasitic activity) to treat the parasitic diseases toxoplasmosis and cystoisosporiasis. It is also used with dapsone as a second-line option to prevent Pneumocystis jiroveci pneumonia in people with HIV/AIDS. It was previously used for malaria but is no longer recommended due to resistance. Pyrimethamine is taken by mouth.

Key facts

Drug.Watchedfields
changed
Drug.verifiedrevid
464377204
Drug.image
Pyrimethamine2DACS.svg
Drug.image_class
skin-invert-image
Drug.width
150px
Drug.image2
Pyrimethamine 3D.png
Drug.image_class2
bg-transparent
Drug.caption
Above: molecular structure of pyrimethamine Below: 3D representation of a pyrimethamine molecule
Drug.tradename
Daraprim, others
Drug.MedlinePlus
a601050
Drug.DailyMedID
Pyrimethamine
Drug.licence_US
Pyrimethamine
Drug.pregnancy_AU
B3
Drug.routes_of_administration
By mouth
Drug.ATC_prefix
P01
Drug.ATC_suffix
BD01
Drug.ATC_supplemental
(combinations)
Drug.legal_AU
S4

via Wikipedia infobox

Chemical data

Formula
C12H13ClN4
Molecular weight
248.71 g/mol
IUPAC name
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
SMILES
CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl
InChIKey
WKSAUQYGYAYLPV-UHFFFAOYSA-N
XLogP
2.7
Polar surface area
77.8 Ų
H-bond donors
2
H-bond acceptors
4
Formal charge
0

via PubChem

~11 min read

Encyclopedic overview

19 sections
Contents
  • Medical uses
  • Toxoplasmosis
  • Pregnancy consideration
  • Malaria
  • Contraindications
  • Side effects
  • Interactions
  • Mechanism of action
  • Other medications
  • Mechanism of resistance
  • History
  • Society and culture
  • Economics
  • United States
  • Other countries
  • Research
  • See also
  • References
  • External links

Pyrimethamine, sold under the brand name Daraprim among others, is a medication used with leucovorin (leucovorin is used to decrease side effects of pyrimethamine; it does not have intrinsic anti-parasitic activity) to treat the parasitic diseases toxoplasmosis and cystoisosporiasis. It is also used with dapsone as a second-line option to prevent Pneumocystis jiroveci pneumonia in people with HIV/AIDS. It was previously used for malaria but is no longer recommended due to resistance. Pyrimethamine is taken by mouth.

Common side effects include gastrointestinal upset, severe allergic reactions, and bone marrow suppression. It should not be used by people with folate deficiency that has resulted in anemia. There is concern that it may increase the risk of cancer. While occasionally used in pregnancy it is unclear if pyrimethamine is safe for the baby. Pyrimethamine is classified as a folic acid antagonist. It works by inhibiting folic acid metabolism and therefore the making of DNA.

Excerpted from Wikipedia’s “pyrimethamine” article, available under the CC BY-SA 4.0 licence.

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