Daraprim


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pyrimethamine

Daraprim

Pharmacologic class: Folic acid antagonist

Therapeutic class: Antiprotozoal, antimalarial

Pregnancy risk category C

Action

Inhibits reduction of dihydrofolic acid to tetrahydrofolic acid (folinic acid) by binding to and reversibly inhibiting dihydrofolate reductase

Availability

Tablets: 25 mg

Indications and dosages

To control plasmodia transmission and suppress susceptible strains Adults and children ages 10 and older: 25 mg P.O. daily for 2 days, given with a sulfonamide

Toxoplasmosis

Adults: Initially, 50 to 75 mg P.O. daily for 1 to 3 weeks, given with a sulfonamide. Depending on response and tolerance, reduce dosages of both drugs by 50% and continue therapy for 4 to 5 more weeks.

Children: 1 mg/kg P.O. daily in two equally divided doses for 2 to 4 days, then reduced to 0.5 mg/kg/day for approximately 1 month. Alternatively, 2 mg/kg (up to 100 mg) P.O. daily in two equally divided doses for 3 days, then 1 mg/kg (up to 25 mg) in two equally divided doses for 4 weeks, given with sulfadiazine for 4 weeks.

Prophylaxis of malaria caused by susceptible plasmodia strains

Adults and children older than age 10: 25 mg P.O. weekly

Children ages 4 to 10: 12.5 mg P.O. weekly

Infants and children younger than age 4: 6.25 mg P.O. weekly

Off-label uses

• Isosporiasis
• Prophylaxis of Pneumocystis jiroveci pneumonia

Contraindications

• Hypersensitivity to drug
• Megaloblastic anemia caused by folate deficiency
• Concurrent folate antagonist therapy

Precautions

Use cautiously in:
• anemia, bone marrow depression, hepatic or renal impairment, G6PD deficiency
• history of seizures
• patients more than 16 weeks pregnant
• breastfeeding patients.

Administration

• Administer with meals.
• When giving tablets to young children, crush them and administer as oral suspension in water, cherry syrup, or sweetened solution.
• Know that because of worldwide resistance to pyrimethamine, its use alone to prevent or treat acute malaria is no longer recommended.
• Be aware that fixed combination of pyrimethamine and sulfadoxine is available and has been used for uncomplicated mild to moderate malaria caused by chloroquineresistant Plasmodium falciparum and for presumptive self-treatment by travelers.

Adverse reactions

CNS: headache, light-headedness, insomnia, malaise, depression, seizures

CV: arrhythmias

EENT: dry throat

GI: nausea, vomiting, diarrhea, anorexia, atrophic glossitis

GU: hematuria

Hematologic: megaloblastic anemia, leukopenia, pancytopenia, thrombocytopenia

Metabolic: hyperphenylalaninemia

Respiratory: pulmonary eosinophilia

Skin: pigmentation changes, dermatitis, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome

Other: fever, anaphylaxis

Interactions

Drug-drug. Lorazepam: hepatotoxicity Myelosuppressants (including antineoplastics): increased risk of bone marrow depression

Drug-diagnostic tests. Platelets, white blood cells: decreased counts

Patient monitoring

• Monitor CBC. Watch for evidence of blood dyscrasias.
• Assess for signs and symptoms of folic acid deficiency.
• Closely monitor neurologic and cardiovascular status. Stay alert for seizures and arrhythmias.

Watch for evidence of erythema multiforme, including sore throat, cough, mouth sores, rash, iritic lesions, and fever. Report early signs before condition can progress to Stevens-Johnson syndrome.

Patient teaching

• Advise patient to take with meals.

Tell patient to discontinue drug and contact prescriber at first sign of rash.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

Daraprim

(dâr′ə-prĭm′)
A trademark for the drug pyrimethamine.

Daraprim

a trademark for an antimalarial (pyrimethamine).

Daraprim

A brand name for PYRIMETHAMINE.
References in periodicals archive ?
We believe we now have an extremely cost-effective way to provide access to a Daraprim alternative.
A month ago, Turing Pharmaceuticals LLC, the single provide of Daraprim, mounted the rate of this prescription drug from $13.
Daraprim has been around for 50 years and costs 64p a tablet to produce.
He insisted Daraprim profits will fund research and raise awareness of toxoplasmosis.
Ex-hedge fund boss Mr Shkreli, 32, runs Turing Pharmaceuticals which acquired the rights to Daraprim last month for almost PS36million.
Baum added, "The recent announcement that we are offering combination pyrimethamine and leucovorin formulations for physicians to consider prescribing for their patients as a low cost alternative to Daraprim, brought Imprimis worldwide media attention and went viral on social media channels.
Former hedge fund boss Mr Shkreli, 32, last month acquired the rights to Daraprim, which has been around for 62 years, for PS36million.
In particular, the Committee wishes to learn more about Turing Pharmaceuticals' recent acquisition of the rights to sell Daraprim, a drug used to treat and prevent infections, from Impax Laboratories and Turing's subsequent decision to increase the price of Daraprim from $13.
Daraprim (pyrimethamine) for the treatment of Toxoplasmosis in combination with sulfonamide and Vecamyl(r) (mecamylamine HCl tablets) for hypertension are Turing's first commercial products.
NASDAQ: IMMY), a specialty pharmaceutical company focused on the development and commercialization of proprietary compounded drug therapies, today announced it has made available a customizable compounded formulation of pyrimethamine and leucovorin available for physicians to consider prescribing for their patients as a low cost alternative to Daraprim.
For example, the price of Daraprim, a drug used to fight an AIDS related infection, has increased in cost from $13.
rights to the Daraprim brand to Turing Pharmaceuticals AG for approximately $55 million.