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.

q

Daraprim

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

Daraprim

A brand name for PYRIMETHAMINE.
References in periodicals archive ?
Gottlieb had said that the main problem behind high drug prices isn't the cost of new, specialty drugs but instead old drugs whose sellers can indiscriminately raise prices because there isn't enough competition from generics, like in the case of Daraprim.
The answer is that no company could seek FDA approval for a generic version, because Turing had put Daraprim under "restricted distribution," a designation--in this case, self-imposed--allowing drug makers to limit who can acquire their products, even when there's no post-market data suggesting the drug is dangerous.
Summary: Shkreli, 34, is best known for raising the price of a drug, Daraprim, by 5,000 per cent in a move that was widely condemned by the public and politicians
He is a man who needs to take responsibility for his actions." Unapologetic from the beginning, when he was roundly publicly criticized for defending the 5,000 percent price increase of Daraprim, a previously cheap drug used to treat HIV, Shkreli seemed to drift through his criminal case as if it was one big joke.
Progress Towards a High School Synthesis of Daraprim. Paper presented at the New South Wales Organic Chemistry Group 37th Annual One-Day Symposium, Macquarie University.
Four other Medicaid drugs increased more than 300% year over year: Epitol, an anticonvulsant (460%); the antimalaria drug Hydroxychloroquine Sulfate, or Plaquenil, (489%); Phenergan (417%), an allergy medication; and Daraprim (874%), from Turing Pharmaceuticals AG.
In 2015 the price for Daraprim, a drug used to treat a parasitic infection in pregnant women and those with compromised immune systems due to cancer or HIV/ AIDS went from $13.50 to $750 per pill overnight.
Daraprim, the drug in question, had gone from costing around $13.50 per pill to $750 for each tablet.
In 2015, Turing Pharmaceuticals CEO Martin Shkreli raised the price of Daraprim from $13.50 to $750 per pill, generating a wave of negative publicity and prompting the swift passage of Section 602 in the Bipartisan Budget Act of 2015 (BBA).
Daraprim, the company that bought the rights to the drug and increased its price, is just the latest entry in the ongoing debate about whether some drugs are effective enough to justify the cost.
Martin Shkreli, CEO of Turing Pharmaceuticals caused a huge stir when he raised the price of Daraprim from $13.50 a tablet to $750 (Pollack and Tavernise, 2015).
Hedge fund manager Shkreli, the former CEO of Turing Pharmaceuticals, who infamously raised the price of Daraprim from $13.50 to $750 per tablet, recently "took the Fifth" while testifying before Congress.