Daraprim

Onset: ~1 hr

Absorption: well absorbed

Distribution: widely, mainly in blood cells, kidneys, lungs, liver, & spleen; crosses into CSF; crosses placenta; enters breast milk

Protein Bound: 80-87%

Metabolism: hepatic

Half-life elimination: 80-95 hr

Peak Plasma Time: 1.5-8 hr

Excretion: urine (20-30% as unchanged drug)

Mechanism of Action

Folic acid antagonist

Print without Office InfoPrint with Office Info

Tell your doctor if you are breastfeeding or plan to breastfeed.

Daraprim has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from Daraprim, a choice should be made whether to stop nursing or to stop use of this medication. The importance of the drug to the mother should be considered.

 

Take Daraprim exactly as prescribed.

This medication is comes in tablet form and is taken up to 2 times a day, with or without food.  If anorexia and vomiting occur, try taking Daraprim with meals. Taking folinic acid is strongly recommended when used for the treatment of toxoplasmosis in all patients.  If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of Daraprim at the same time.

Hypersensitivity reactions, occasionally severe (such as Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, and anaphylaxis), and hyperphenylalaninemia, can occur particularly when pyrimethamine is administered concomitantly with a sulfonamide. Consult the complete prescribing information for the relevant sulfonamide for sulfonamideassociated adverse events. With doses of pyrimethamine used for the treatment of toxoplasmosis, anorexia and vomiting may occur. Vomiting may be minimized by giving the medication with meals; it usually disappears promptly upon reduction of dosage. Doses used in toxoplasmosis may produce megaloblastic anemia, leukopenia, thrombocytopenia, pancytopenia, neutropenia, atrophic glossitis, hematuria, and disorders of cardiac rhythm.

Hematologic effects, however, may also occur at low doses in certain individuals (see PRECAUTIONS; General). Pulmonary eosinophilia has been reported rarely.

Read the entire FDA prescribing information for Daraprim (Pyrimethamine)

Read More »

Administration

Oral Administration

Administer orally.167 If anorexia or vomiting occurs, give with a meal to minimize adverse GI effects.167

For children and others unable to swallow tablets, extemporaneous oral suspensions of pyrimethamine may be prepared by crushing pyrimethamine tablets (single-entity preparation) and mixing with water, cherry syrup, or other sucrose-containing solution.109 (See Stability.) Shake oral suspension prior to each dose.109

Dosage

Pediatric Patients

Cystoisosporiasis† Treatment in HIV-infected Children† Oral

1 mg/kg once daily with oral leucovorin (10–25 mg once daily) for 14 days.156

Treatment in HIV-infected Adolescents† Oral

50–75 mg once daily with oral leucovorin (10–25 mg once daily).155

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Children† Oral

1 mg/kg (up to 25 mg) once daily with oral leucovorin (10–25 mg once daily).156

Can consider discontinuing secondary prophylaxis against cystoisosporiasis if there is sustained improvement for >6 months in CD4+ T-cell counts or CD4 percentages (change from CDC immunologic category 3 to category 1 or 2).156

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Adolescents† Oral

25 mg once daily with oral leucovorin (5–10 mg once daily).155

Can consider discontinuing secondary prophylaxis of cystoisosporiasis if CD4+ T-cell counts remain >200 cells/mm3 for >6 months in response to antiretroviral therapy and there is no evidence of active C. belli infection.155

Malaria Prevention of Malaria Oral

Infants and children <4 years of age: Manufacturer recommends 6.25 mg once weekly.167

Children 4–10 years of age: Manufacturer recommends 12.5 mg once weekly.167

Children >10 years of age: Manufacturer recommends 25 mg once weekly.167

Pyrimethamine-resistant strains prevalent worldwide; not suitable for prevention of malaria in most areas.167 (See Malaria under Uses.)

Treatment of Acute Malaria Oral

Children 4–10 years of age: Manufacturer recommends 25 mg once daily for 2 days, followed by 12.5 mg once weekly for ≥10 weeks.167

Pyrimethamine-resistant strains prevalent worldwide; do not use alone for treatment of acute malaria.167 (See Malaria under Uses.)

Pneumocystis jiroveci (Pneumocystis carinii) Pneumonia† Prevention (Primary Prophylaxis) in HIV-infected Adolescents† Oral

50 mg once weekly with oral leucovorin (25 mg once weekly) and oral dapsone (50 mg once daily).134 155 Alternatively, 75 mg once weekly with oral leucovorin (25 mg once weekly) and oral dapsone (200 mg once weekly).134 155

Alternatively, 25 mg once daily with oral leucovorin (10 mg once daily) and oral atovaquone (1.5 g once daily).155

Criteria for initiating or discontinuing primary prophylaxis of PCP† in HIV-infected adolescents are the same as those for adults.155 (See Adults under Dosage and Administration.)

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Adolescents† Oral

50 mg once weekly with oral leucovorin (25 mg once weekly) and oral dapsone (50 mg once daily).134 155 Alternatively, 75 mg once weekly with oral leucovorin (25 mg once weekly) and oral dapsone (200 mg once weekly).134 155

Alternatively, 25 mg once daily with oral leucovorin (10 mg once daily) and oral atovaquone (1.5 g once daily).155

Criteria for initiating or discontinuing secondary prophylaxis of PCP in adolescents are the same as those for adults.155 (See Adults under Dosage and Administration.)

Toxoplasmosis Treatment Oral

Manufacturer recommends 1 mg/kg daily in 2 divided doses for 2–4 days, then reduce dosage by 50% and continue for approximately 1 month.167 Must be used in conjunction with a sulfonamide.167

Treatment of Congenital Toxoplasmosis Oral

2 mg/kg once daily for 2 days, then 1 mg/kg once daily for 2–6 months, then 1 mg/kg 3 times weekly; used with oral or IM leucovorin (10 mg with each pyrimethamine dose) and oral sulfadiazine (50 mg/kg twice daily).156

Recommended duration in HIV-infected infants is 12 months.156

Treatment in HIV-infected Infants and Children Oral

2 mg/kg (up to 50 mg) once daily for 3 days, then 1 mg/kg (up to 25 mg) once daily; used with oral leucovorin (10–25 mg once daily) and oral sulfadiazine (25–50 mg/kg [up to 1–1.5 g] 4 times daily).156 Alternatively, pyrimethamine 2 mg/kg (up to 50 mg) once daily for 3 days, then 1 mg/kg (up to 25 mg) once daily; used with oral leucovorin (10–25 mg once daily) and oral or IV clindamycin (5–7.5 mg/kg [up to 600 mg] 4 times daily).156

Continue acute treatment for ≥6 weeks; longer duration may be appropriate if disease is extensive or response incomplete at 6 weeks.156

Treatment in HIV-infected Adolescents Oral

200-mg loading dose, then 50 mg once daily in those weighing <60 kg or 75 mg once daily in those weighing ≥60 kg; used with oral leucovorin (10–25 mg once daily; may be increased to 50 mg once or twice daily) and oral sulfadiazine (1 g every 6 hours in those weighing <60 kg or 1.5 g every 6 hours in those weighing ≥60 kg).155

Alternatively, 200-mg loading dose, then 50 mg once daily in those weighing <60 kg or 75 mg once daily in those weighing ≥60 kg; used with oral leucovorin (10–25 mg once daily; may be increased to 50 mg once or twice daily) and oral or IV clindamycin (600 mg every 6 hours), oral atovaquone (1.5 g twice daily), or oral azithromycin (0.9–1.2 g once daily).155

Continue acute treatment for ≥6 weeks; longer duration may be appropriate if disease is extensive or response incomplete at 6 weeks.155

Prevention (Primary Prophylaxis) in HIV-Infected Infants and Children† Oral

1 mg/kg (up to 25 mg) once daily used with oral leucovorin (5 mg once every 3 days) and oral dapsone (2 mg/kg or 15 mg/m2 once daily [up to 25 mg]) in those ≥1 month of age.156

If pyrimethamine (and leucovorin) used in conjunction with atovaquone as alternative for primary prophylaxis in those 4–24 months of age, regimen of pyrimethamine 1 mg/kg or 15 mg/m2 (up to 25 mg) once daily with oral leucovorin (5 mg once every 3 days) and oral atovaquone (45 mg/kg once daily) recommended.156

Initiate primary prophylaxis against T. gondii encephalitis in all HIV-infected children <6 years of age with severe immunosuppression who are seropositive for Toxoplasma IgG antibody and have CD4+ T-cell percentages <15%.156 Initiate primary prophylaxis in HIV-infected children >6 years of age who are seropositive for Toxoplasma IgG antibody with CD4+ T-cell counts <100/mm3.156

Safety of discontinuing primary prophylaxis against toxoplasmosis in HIV-infected children whose immunologic status improves with potent antiretroviral therapy not extensively studied to date.156 Do not discontinue primary prophylaxis in HIV-infected children <1 year of age.156 Based on data from adults, can consider discontinuing primary prophylaxis in those 1 to <6 years of age who have received ≥6 months of antiretroviral therapy if CD4+ T-cell percentages remain ≥15% for >3 months.156 For children ≥6 years of age who have received ≥6 months of antiretroviral therapy, can consider discontinuing if CD4+ T-cell counts remain >200/mm3 for >3 months.156

Reinitiate primary prophylaxis against toxoplasmosis if CD4+ T-cell percentages decrease to <15% in HIV-infected children <6 years of age or if CD4+ T-cell counts decrease to <100–200/mm3 in HIV-infected children ≥6 years of age.156

Prevention (Primary Prophylaxis) in HIV-Infected Adolescents† Oral

50 mg once weekly used with oral leucovorin (25 mg once weekly) and oral dapsone (50 mg once daily).155 Alternatively, 75 mg once weekly used with oral leucovorin (25 mg once weekly) and oral dapsone (200 mg once weekly).155

Alternatively, 25 mg once daily used with oral leucovorin (10 mg once daily) and oral atovaquone (1.5 g once daily).155

Criteria for initiating or discontinuing primary prophylaxis against toxoplasmosis in adolescents are the same as those for adults.155 (See Adults under Dosage and Administration.)

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Infants and Children† Oral

1 mg/kg or 15 mg/m2 (up to 25 mg) once daily used with oral leucovorin (5 mg once every 3 days) and oral sulfadiazine (42.5–60 mg/kg twice daily [up to 2–4 g daily]) or, alternatively, oral clindamycin (7–10 mg/kg 3 times daily).156

If pyrimethamine (and leucovorin) used in conjunction with atovaquone as alternative for secondary prophylaxis in those 4–24 months of age, regimen of pyrimethamine 1 mg/kg or 15 mg/m2 (up to 25 mg) once daily with oral leucovorin (5 mg once every 3 days) and oral atovaquone (45 mg/kg once daily) recommended.156

Safety of discontinuing secondary prophylaxis against toxoplasmosis in HIV-infected children receiving potent antiretroviral therapy not extensively studied.156 If child has completed initial toxoplasmosis treatment, is asymptomatic for toxoplasmosis, and has received ≥6 months of antiretroviral therapy, can consider discontinuing secondary prophylaxis in those 1 to <6 years of age if CD4+ T-cell percentages remain ≥15% for >6 consecutive months or in those ≥6 years of age if CD4+ T-cell counts remain >200/mm3 for >6 consecutive months.156

Reinitiate secondary prophylaxis against toxoplasmosis if CD4+ T-cell percentages decrease to <15% in HIV-infected children <6 years of age or if CD4+ T-cell counts decrease to <200/mm3 in HIV-infected children ≥6 years of age.156

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Adolescents† Oral

25–50 mg once daily used with oral leucovorin (10–25 mg once daily) and oral sulfadiazine (2–4 g daily in 2–4 divided doses) or, alternatively, oral clindamycin (600 mg every 8 hours).155

Alternatively, 25 mg once daily with oral leucovorin (10 mg once daily) and oral atovaquone (750–1500 mg twice daily).155

Criteria for initiating or discontinuing secondary prophylaxis against toxoplasmosis in adolescents are the same as those for adults.155 (See Adults under Dosage and Administration.)

Adults

Cystoisosporiasis† Treatment in HIV-infected Adults† Oral

50–75 mg once daily with oral leucovorin (10–25 mg once daily).155

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Adults† Oral

25 mg once daily with oral leucovorin (5–10 mg once daily).155

Can consider discontinuing secondary prophylaxis of cystoisosporiasis if CD4+ T-cell counts remain >200 cells/mm3 for >6 months in response to antiretroviral therapy and there is no evidence of active C. belli infection.155

Malaria Prevention of Malaria Oral

Manufacturer recommends 25 mg once weekly.167

Pyrimethamine-resistant strains prevalent worldwide; not suitable for prevention of malaria in most areas.167 (See Malaria under Uses.)

Treatment of Acute Malaria Oral

Manufacturer recommends 50 mg once daily for 2 days, followed by 25 mg once weekly for ≥10 weeks.167

Manufacturer states 25 mg once daily for 2 days in conjunction with a sulfonamide will initiate transmission control and suppression of non-falciparum malaria.167

Pyrimethamine-resistant strains prevalent worldwide; do not use alone for treatment of acute malaria.167 (See Malaria under Uses.)

Pneumocystis jiroveci (Pneumocystis carinii) Pneumonia† Prevention (Primary Prophylaxis)† Oral

50 mg once weekly used with oral leucovorin (25 mg once weekly) and oral dapsone (50 mg once daily).134 155 Alternatively, 75 mg once weekly with oral leucovorin (25 mg once weekly) and oral dapsone (200 mg once weekly).134 155

Alternatively, 25 mg once daily with oral leucovorin (10 mg once daily) and oral atovaquone (1.5 g once daily).155

Initiate primary prophylaxis against PCP in HIV-infected adults and adolescents with CD4+ T-cell counts <200/mm3 or a history of oropharyngeal candidiasis.155 Also consider primary prophylaxis if CD4+ T-cell percentage is <14% or there is a history of an AIDS-defining illness.155

Primary prophylaxis against PCP generally can be discontinued in HIV-infected adults and adolescents if CD4+ T-cell counts remain ≥200/mm3 for ≥3 months in response to antiretroviral therapy.155

Reinitiate primary prophylaxis if CD4+ T-cell count decreases to <200/mm3.155

Prevention of Recurrence (Secondary Prophylaxis)† Oral

50 mg once weekly used with oral leucovorin (25 mg once weekly) and oral dapsone (50 mg once daily).134 155 Alternatively, 75 mg once weekly with oral leucovorin (25 mg once weekly) and oral dapsone (200 mg once weekly).134 155

Alternatively, 25 mg once daily with oral leucovorin (10 mg once daily) and oral atovaquone (1.5 g once daily).155

Initiate chronic maintenance therapy (secondary prophylaxis) to prevent recurrence in those with a history of PCP.155

Secondary prophylaxis against PCP generally can be discontinued in HIV-infected adults and adolescents if CD4+ T-cell counts remain >200/mm3 for >3 months in response to antiretroviral therapy.155

Reinitiate secondary prophylaxis if CD4+ T-cell counts decrease to <200/mm3.155 However, secondary prophylaxis probably should be continued for life (regardless of CD4+ T-cell count) if PCP was diagnosed or recurred when CD4+ T-cell counts >200/mm3.155

Toxoplasmosis Treatment Oral

Manufacturer recommends 50–75 mg once daily in conjunction with a sulfonamide for 1–3 weeks; reduce dosage of both drugs by 50% and continue for 4–5 additional weeks.167

Treatment in HIV-infected Adults Oral

200-mg loading dose, then 50 mg once daily in those weighing <60 kg or 75 mg once daily in those weighing ≥60 kg; used with oral leucovorin (10–25 mg once daily; may be increased to 50 mg once or twice daily) and oral sulfadiazine (1 g every 6 hours in those weighing <60 kg or 1.5 g every 6 hours in those weighing ≥60 kg).155

Alternatively, 200-mg loading dose, then 50 mg once daily in those weighing <60 kg or 75 mg once daily in those weighing ≥60 kg; used with oral leucovorin (10–25 mg once daily; may be increased to 50 mg once or twice daily) and oral or IV clindamycin (600 mg every 6 hours), oral atovaquone (1.5 g twice daily), or oral azithromycin (0.9–1.2 g once daily).155

Continue acute treatment for ≥6 weeks; longer duration may be appropriate if disease is extensive or response incomplete at 6 weeks.155

Prevention (Primary Prophylaxis) in HIV-Infected Adults† Oral

50 mg once weekly used with oral leucovorin (25 mg once weekly) and oral dapsone (50 mg once daily).155 Alternatively, 75 mg once weekly with oral leucovorin (25 mg once weekly) and oral dapsone (200 mg once weekly).155

Alternatively, 25 mg once daily used with oral leucovorin (10 mg once daily) and oral atovaquone (1.5 g once daily).155

Primary prophylaxis against toxoplasmosis generally can be discontinued in HIV-infected adults and adolescents if CD4+ T-cell counts remain >200/mm3 for >3 months in response to antiretroviral therapy.155

Reinitiate primary prophylaxis if CD4+ T-cell counts decrease to <100–200/mm3.155

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Adults† Oral

25–50 mg once daily used with oral leucovorin (10–25 mg once daily) and oral sulfadiazine (2–4 g daily given in 2–4 divided doses) or, alternatively, oral clindamycin (600 mg every 8 hours).155

Alternatively, 25 mg once daily with oral leucovorin (10 mg once daily) and oral atovaquone (750–1500 mg twice daily).155

Initiate chronic maintenance therapy (secondary prophylaxis) in all patients who have completed initial treatment of toxoplasmic encephalitis.155

Secondary prophylaxis against toxoplasmosis generally can be discontinued in HIV-infected adults and adolescents who have successfully completed initial therapy for toxoplasmic encephalitis, remain asymptomatic with respect to toxoplasmic encephalitis, and have CD4+ T-cell counts that remain >200/mm3 for >6 months in response to antiretroviral therapy.155 Some experts would obtain a brain magnetic resonance image as part of their evaluation to determine whether or not discontinuance of secondary prophylaxis is appropriate.155

Reinitiate secondary prophylaxis if CD4+ T-cell counts decrease to <200/mm3.155

Prescribing Limits

Pediatric Patients

Cystoisosporiasis† Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Children† Oral

Maximum 25 mg daily.156

Toxoplasmosis Treatment of HIV-infected Children Oral

Maximum 25–50 mg per dose.156

Prevention of Recurrence (Secondary Prophylaxis) in HIV-infected Infants and Children† Oral

Maximum 25 mg per dose.156

Special Populations

No special population dosage recommendation at this time.167

Absorption

Bioavailability

Well absorbed from GI tract;125 167 peak serum concentrations attained within 2–6 hours.125 167

Serum concentrations in children receiving recommended dosages are similar to those in adults.125

Distribution

Extent

Distributed mainly to kidneys, lungs, liver, and spleen.106 125

Distributed into CSF.125

Crosses the placenta.168

Distributed into milk.147 167

Plasma Protein Binding

Approximately 80–90%.161 167

Elimination

Metabolism

Metabolized in the liver125 to several unidentified metabolites.168

Elimination Route

Unchanged drug and metabolites eliminated principally by kidneys.125 168

Half-life

Approximately 96 hours.167

Special Populations

Half-life may not be affected by end-stage renal failure.125 168

Keep this medicine out of the reach of children. Overdose is especially dangerous in children.

If this medicine upsets your stomach or causes vomiting, it may be taken with meals or a snack.

If you are taking this medicine to treat malaria, take the number of tablets your doctor told you to take (up to 3) once, as a single dose, along with other medicine your doctor gave you. If you develop a fever and are not near a medical facility, and are taking this medicine to treat what you think may possibly be malaria, take the number of tablets your doctor told you to take (up to 3) once, as a single dose.

This medicine works best when you take it on a regular schedule. If you are to take two doses a day, one dose may be taken with breakfast and the other one with the evening meal. Make sure that you do not miss any doses. If you have any questions about this, check with your health care professional.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For the treatment of malaria:
  • Adults and adolescents: 25 milligrams of pyrimethamine daily together with a sulfonamide for 2 days. These two medicines may also be taken with other medicine. This will be determined by your doctor.
  • Children: Dose is based on body weight and will be determined by the doctor. Pyrimethamine may be taken together with other medicines.
• For the treatment of toxoplasmosis:
  • Adults and adolescents: Starting dose if 50 to 75 milligrams of pyrimethamine daily taken together with other medicines for several weeks. After one to three weeks, your doctor may lower your dose. The proper dose for you must be determined by the doctor.
  • Children: Dose is based on body weight and must be determined by the doctor.
• For the prevention of malaria:
  • Adults and adolescents: 25 milligrams taken once a week.
  • Children: Dose is based on age and must be determined by the doctor.

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Fever or chills.
• A heartbeat that does not feel normal.
• Feeling very tired or weak.
• Seizures.
• Blood in the urine.
• Any unexplained bruising or bleeding.
• Sore throat.
• Pale skin.
• Pinpoint red spots on the skin.
• Rash.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take Daraprim or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to Daraprim (pyrimethamine). This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

The dosage of pyrimethamine required for the treatment of toxoplasmosis has a narrow therapeutic window. If signs of folate deficiency develop (see ADVERSE REACTIONS), reduce the dosage or discontinue the drug according to the response of the patient. Folinic acid (leucovorin) should be administered in a dosage of 5 to 15 mg daily (orally, IV, or IM) until normal hematopoiesis is restored. Data in 2 humans indicate that pyrimethamine may be carcinogenic; a 51-year-old female who developed chronic granulocytic leukemia after taking pyrimethamine for 2 years for toxoplasmosis3 and a 56-year-old patient who developed reticulum cell sarcoma after 14 months of pyrimethamine for toxoplasmosis.4

Pyrimethamine has been reported to produce a significant increase in the number of lung tumors in mice when given intraperitoneally at doses of 25 mg/kg.5

Daraprim should be kept out of the reach of infants and children as they are extremely susceptible to adverse effects from an overdose. Deaths in pediatric patients have been reported after accidental ingestion.

VYERA
PHARMACEUTICALS

NDC 69413-330-10

Daraprim®
(pyrimethamine) 25mg tablets

Each scored tablet contains
25 mg

Rx only 100 Tablets

018939

LOT

EXP

Applies to pyrimethamine: oral tablet

Along with its needed effects, pyrimethamine (the active ingredient contained in Daraprim) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking pyrimethamine:

Less common

• Black, tarry stools
• blood in urine or stools
• cough or hoarseness
• fever or chills
• irritation or soreness of tongue
• lower back or side pain
• painful or difficult urination
• pinpoint red spots on skin
• unusual bleeding or bruising

Rare

• Bleeding or crusting sores on lips
• chest pain or discomfort
• muscle cramps or pain
• redness, blistering, peeling, or loosening of skin
• skin rash
• sores, ulcers, and/or white spots in mouth
• sore throat
• unusual tiredness or weakness

Frequency not known

• Blood in urine
• diarrhea
• difficulty swallowing
• dizziness
• fainting spells
• fast, slow, or irregular heartbeat
• hives
• itching
• joint or muscle pain
• lightheadedness
• pale skin
• pounding or rapid pulse
• puffiness or swelling of the eyelids or around the eyes, face, lips or tongue
• rapid breathing
• red, irritated eyes
• red skin lesions, often with a purple center
• shortness of breath
• swollen glands
• tightness in chest
• unexplained bleeding or bruising
• wheezing

Symptoms of overdose

• Abdominal or stomach pain
• convulsions (seizures)
• increased excitability
• vomiting (severe and continuing)

Some side effects of pyrimethamine may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common

• Diarrhea
• loss of appetite
• nausea
• vomiting

Pyrimethamine is excreted into human milk. In three women treated with a combination of dapsone and pyrimethamine, the milk:serum ratio of pyrimethamine ranged from 0.46 to 0.66. The manufacturer reports that after a single 75 mg dose, approximately 3 to 4 mg of the drug is estimated to pass on to the feeding child over 48 hours. The American Academy of Pediatrics considers pyrimethamine to be compatible with breast-feeding. The manufacturer recommends that due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.