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atovaquone (Mepron)

 

Classes: Antimalarials

Dosing and uses of Mepron (atovaquone)

 

Adult dosage forms and strengths

tablet

  • 250mg

oral suspension

  • 750mg/5mL

 

Malaria (P. falciparum)

1000 mg (with proguanil 400 mg) PO qDay x3 days

 

Pneumocystis Carinii Pneumonia

Treatment: 750 mg PO BID x21 days

Prophylaxis: 1500 mg/day PO, qDay or divided BID, with food

 

Other Information

See also combo with proguaniL

 

Pediatric dosage forms and strengths

tablet

  • 250mg

oral suspension

  • 750mg/5mL

 

Malaria (P. Falciparum)

11-20 kg: 250 mg (with proguanil 100 mg)

21-30 kg: 500 mg (with proguanil 200 mg)

31-40 kg: 750 mg (with proguanil 300 mg)

All PO qDay x3 days

 

Mepron (atovaquone) adverse (side) effects

>10%

Abdominal pain (4-21%)

Cough (14-25%)

Depression (undefined)

Diarrhea (19-42%)

Dyspnea (15-21%)

Fever (14-40%)

Headache (16-31%)

Infection (18-22%)

Insomnia (10-19%)

Myalgia (undefined)

Nausea (21-32%)

Rash (22-46%)

Rhinitis (5-24%)

Vomiting (14-22%)

Weakness (8-31%)

 

1-10%

Amylase increased (7-8%)

Anemia (4-6%)

Anorexia (<7%)

Anxiety (<7%)

BUN/creatinine increased (<1%)

Constipation (<3%)

Dyspepsia (<5%)

Dizziness (3-8%)

Hyperglycemia (<9%)

Hypoglycemia (<1%)

Hyponatremia (7-10%)

Liver enzymes elevated (4-8%)

Neutropenia (3-5%)

Pruritus (5-10%)

Oral moniliasis (5-10%)

Taste perversion (<3%)

 

Warnings

Contraindications

Hypersensitivity

Monotherapy for malaria

 

Cautions

Admin proguanil concomitantly for malaria

Admin w/ food

 

Pregnancy and lactation

Pregnancy category: C

Lactation: excretion in milk unknown; use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Mepron (atovaquone)

Absorption: significantly increased with a high-fat meaL

Distribution: 3.5 L/kg

Protein Bound: >99%

Metabolism: undergoes enterohepatic recirculation

Bioavailability: tablet: 23%; suspension: 47%

Half-life, elimination: 2-3 d

Excretion: feces (94% as unchanged drug)

 

Mechanism of action

Inhibits electron transport chain in Plasmodium