atovaquone/proguanil (Rx)

Brand and Other Names:Malarone
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

atovaquone/proguanil

tablet

  • 250mg/100mg
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Malaria

Prophylaxis

  • 250 mg/100 mg (1 tablet) PO daily, beginning 1-2 days before travel to malaria-endemic area and continued until 7 days after return 

Treatment

  • 1 g/400 mg (4 tablets) PO daily for 3 days

Dosing considerations

  • In event of vomiting within 1 hour of dose, repeat dose
  • In geriatric patients, cautious dose selection is necessary because of decreased hepatic/renal/cardiac function and increased systemic exposure to cycloguanil

Dosing Modifications

CrCl <30 mL/min: Prophylactic use not recommended; only use for treatment if benefits of therapy greatly outweigh risks

CrCl 30-80 mL/min: No dosage adjustments necessary

Administration

Take at same time daily with food or milky drink

For children with difficulty swallowing, may be crushed and mixed with condensed milk just before administration

Dosage Forms & Strengths

atovaquone/proguanil

tablet

  • 62.5mg/25mg
more...

Malaria

Prophylaxis

  • <11 kg: Safety and efficacy not established
  • 11-20 kg: 62.5 mg/25 mg (1 pediatric tablet) PO daily
  • 21-30 kg: 125 mg/50 mg (2 pediatric tablets) PO daily
  • 31-40 kg: 187.5 mg/75 mg (3 pediatric tablets) PO daily
  • >40 kg: 250 mg/100 mg (1 adult tablet) PO daily, beginning 1-2 days before travel to malaria-endemic area and continued until 7 days after return 

Treatment

  • <5 kg: Safety and efficacy not established
  • 5-8 kg: 125 mg/50 mg (2 pediatric tablets) PO daily for 3 days
  • 9-10 kg: 187.5 mg/75 mg (3 pediatric tablets) PO daily for 3 days
  • 11-20 kg: 250 mg/100 mg (1 adult tablet) PO daily for 3 days
  • 21-30 kg: 500 mg/200 mg (2 adult tablets) PO daily for 3 days
  • 31-40 kg: 750 mg/300 mg (3 adult tablets) PO daily for 3 days
  • >40 kg: 1 g/400 mg (4 adult tablets) PO daily for 3 days

Dosing considerations

  • In event of vomiting within 1 hour of dose, repeat dose
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Interactions

Interaction Checker

and atovaquone/proguanil

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Abdominal pain (3-31%)

            Transaminase increases (17-27%)

            Headache (3-14%)

            Vomiting (1-13%)

            Nausea (12%)

            1-10%

            Asthenia (8%)

            Diarrhea (1-8%)

            Pruritus (6%)

            Anorexia (5%)

            Dizziness (5%)

            Dyspepsia (1-4%)

            Gastritis (0-3%)

            <1%

            Fever

            Cough

            Postmarketing Reports

            Hematologic/lymphatic: Neutropenia, anemia (rarely), pancytopenia (patients with severe renal impairment treated with proguanil)

            Immunologic: Allergic reactions, including angioedema, urticaria, and rare cases of anaphylaxis and vasculitis

            Neurologic: Rare cases of seizures and psychotic events (eg, hallucinations)

            GI: Stomatitis

            Hepatic: Elevated liver function tests (LFTs), rare cases of hepatitis, cholestasis

            Skin: Photosensitivity, rash, and rare cases of erythema multiforme and Stevens-Johnson syndrome

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            Warnings

            Contraindications

            Hypersensitivity

            Not to be used for prophylaxis of Plasmodium falciparum in severe renal impairment (CrCl <30 mL/min)

            Cautions

            Administration does not provide radical cure, nor does it prevent delayed primary attacks of P vivax and P ovale

            Patients with severe malaria are not candidates for oral therapy; not evaluated in treatment of cerebral malaria or severe manifestations of malaria (eg, hyperparasitemia, pulmonary edema, renal failure)

            Elevated LFTs and rare cases of hepatitis have been reported

            Absorption may be reduced in patients with diarrhea or vomiting; monitor closely, and consider antiemetic use

            Monotherapy may result in parasite relapse of P vivax malaria

            Recrudescent P falciparum infection or chemoprophylactic failure after monotherapy should be treated with different schizonticide

            Prophylaxis should not be prematurely discontinued

            Complete prophylaxis includes therapy, protective clothing, insect repellents, and bednets

            No chemoprophylactic regimen is 100% effective; patient should seek medical care for any febrile illness that occurs

            P falciparum malaria carries higher risk of death and serious complications in pregnant women; patient should discuss risks and benefits of travel, and if travel cannot be avoided, additional prophylaxis, including protective clothing, must be employed

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Proguanil is excreted into milk in small quantities, but excretion of atovaquone is 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.

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            Pharmacology

            Mechanism of Action

            Antiparasitic activity

            Atovaquone: Selective inhibitor of parasite mitochondrial electron transport

            Proguanil: Primary effect through metabolite cycloguanil, a dihydrofolate reductase inhibitor in malaria parasite, which leads to disruption of deoxythymidylate synthesis

            Absorption

            Bioavailability: Oral absorption of atovaquone is poor but increases to 23% with high-fat meal (AUC increased 2-3 times and Cmax 5 times over fasting); administer with food or milk; proguanil is extensively absorbed

            Distribution

            Protein bound: Atovaquone, >99%; proguanil, 75%

            Vd: Atovaquone, 8.8 L/kg

            Metabolism

            Proguanil is metabolized to cycloguanil (primarily by CYP2C19)

            Elimination

            Half-life: Atovaquone, 2-3 days; proguanil, 12-21 hr

            Clearance: Atovaquone, 1.32-6.61 L/hr; proguanil, 29.5-67.9 L/hr

            Excretion: Atovaquone, feces as unchanged drug (94%); proguanil, urine (40-60%)

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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