mefloquine (Rx)

Brand and Other Names:
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 250mg

Acute Malaria Infections

Indicated for the treatment of mild-to-moderate acute malaria caused by mefloquine-susceptible strains of P. falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax

1250 mg PO once

Malaria Prevention

250 mg PO qWeek

Start 1-2 weeks before arrival in endemic area; continue 4 weeks after leaving endemic area

Dosing Considerations

If a full-treatment course does not lead to improvement within 48-72 hr, mefloquine should not be used for retreatment; an alternative therapy should be used

Similarly, if previous prophylaxis with mefloquine failed, mefloquine should not be used for curative treatment

Insufficient clinical data exist to document the effect of mefloquine in malaria caused by P. ovale or P. malariae

Patients with acute P. vivax malaria, treated with mefloquine, are at high risk of relapse because mefloquine does not eliminate exoerythrocytic (hepatic phase) parasites; to avoid relapse, after initial treatment of the acute infection with mefloquine, patients should subsequently be treated with an 8-aminoquinoline derivative (eg, primaquine)

Chloroquine-Resistant Malaria (Orphan)

Prevention and treatment of chloroquine-resistant Faciparum malaria

Orphan indication sponsor

  • Mepha AG; 4143 Dornach; Postfash 137, Switzerland

Administration

Take with food and >8 oz water

May repeat full or partial dose if vomited

Dosage Forms & Strengths

tablet

  • 250mg

Acute Malaria Infections

Indicated for the treatment of mild-to-moderate acute malaria caused by mefloquine-susceptible strains of P. falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax

<6 months old: Safety and efficacy not established

>6 months old: 20-25 mg/kg PO as single dose or may divide in 2 doses  

Malaria Prevention

5 to <10 kg: 31.25 mg (1/8 tablet) PO qWeek

10 to <20 kg: 62.5 mg (1/4 tablet) PO qWeek

20 to <30 kg: 125 mg (1/2 tablet) PO qWeek

30-45 kg: 187.5 mg (3/4 tablet) PO qWeek

>45 kg: 250 mg (1 tablet) PO qWeek

Start 1-2 weeks before arrival in endemic area; continue 4 weeks after leaving endemic area

Dosing Considerations

If a full-treatment course does not lead to improvement within 48-72 hr, mefloquine should not be used for retreatment; an alternative therapy should be used

Similarly, if previous prophylaxis with mefloquine failed, mefloquine should not be used for curative treatment

Insufficient clinical data exist to document the effect of mefloquine in malaria caused by P. ovale or P. malariae

Patients with acute P. vivax malaria, treated with mefloquine, are at high risk of relapse because mefloquine does not eliminate exoerythrocytic (hepatic phase) parasites; to avoid relapse, after initial treatment of the acute infection with mefloquine, patients should subsequently be treated with an 8-aminoquinoline derivative (eg, primaquine)

Administration

Take with food and >8 oz water

May repeat full or partial dose if vomited

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Interactions

Interaction Checker

and mefloquine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Anxiety

            Difficulty concentrating

            Headache

            Insomnia

            Lightheadedness

            Vertigo

            Vomiting

            Diarrhea

            Stomach pain

            Nausea

            Visual disturbances

            Tinnitus

            Frequency Not Defined

            Suicidal depression

            Psychiatric Sx

            Pneumonitis

            Seizure

            Abnormal ECG

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            Warnings

            Black Box Warnings

            May cause neuropsychiatric adverse reactions that can persist after mefloquine has been discontinued

            Should not be prescribed for prophylaxis in patients with major psychiatric disorders

            During prophylactic use, if psychiatric or neurologic symptoms occur, the drug should be discontinued and an alternative medication should be substituted

            Contraindications

            Hypersensitivity to mefloquine, related drugs (eg, quinidine, quinine)

            Do not prescribe for prophylaxis in patients with active or recent history of depression, generalized anxiety disorder; history of psychosis, schizophrenia, other major psychiatric disorders, or convulsions

            Cautions

            In case of life-threatening, serious or overwhelming malaria infections due to P. falciparum, patients should be treated with an IV antimalarial drug; following completion of IV treatment, mefloquine may be given to complete the course of therapy

            May increase QT interval; caution with other drugs known to prolong QT interval

            Strong CYP3A4 inhibitors (eg, ketoconazole) should do not coadminister with or within 15 weeks after the last mefloquine dose

            Caution with hepatic impairment

            Agranulocytosis and aplastic anemia reported

            Geographical drug resistance patterns of P. falciparum occur and the preferred choice of malaria prophylaxis might be different from one area to another

            Periodic ophthalmic examinations recommended; retinal abnormalities seen in humans with long-term chloroquine use have not been observed with mefloquine use; however, long- term feeding of mefloquine to rats resulted in dose-related ocular lesions

            Psychiatric and neurologic adverse effects

            • May cause neuropsychiatric adverse reactions, which may be difficult to identify in children; monitor for symptoms, especially in nonverbal children
            • Psychiatric symptoms ranging from anxiety, paranoia, and depression to hallucinations and psychotic behavior can occur; symptoms may occur early in the course of mefloquine use and in some cases, these symptoms have been reported to continue for months or years after mefloquine has been stopped
            • Cases of suicidal ideation and suicide have been reported
            • Should not be prescribed for prophylaxis in patients with active depression, generalized anxiety disorder, psychosis, or schizophrenia or other major psychiatric disorders
            • Dizziness or vertigo, tinnitus, and loss of balance reported; these symptoms were reported to be permanent in some cases
            • May increase the risk of convulsions in patients with epilepsy; prescribed only for curative treatment in such patients and only if there are compelling medical reasons for its use
            • Concomitant administration of mefloquine and quinine or chloroquine may increase the risk of convulsions
            • During prophylactic use, if symptoms emerge, discontinue and substitute treatment with a different antimalarial agent
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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: Minimally excreted in human breast milk; based on a study in a few subjects, low concentrations (3% to 4%) excreted; caution advised

            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

            Structural analog of quinine; exact mechanism unknown, acts as a blood schizonticide

            May increase intravesicular pH in parasites

            Absorption

            Bioavailability: Well absorbed; >85%; food enhances bioavailability by ~40%

            Peak plasma time: 17 hr (range 6-24 hr)

            Peak plasma concentration: 1000-2000 mcg/L (after 7-10 wk of 250 mg once weekly dosing)

            Distribution

            Vd: 20 L/kg; blood, urine, CSF, tissues; enters breast milk

            Protein Bound: 98%

            Metabolism

            Extensively metabolized in liver by CYP3A4

            Metabolites: 2,8-bistrifluoromethyl-4-quinoline carboxylic acid is inactive

            Elimination

            Half-life: 21-22 days

            Total clearance (hepatic): 30 mL/min

            Excretion: Mainly in bile and feces; urine (~1.5-9% as unchanged drug)

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            Formulary

            FormularyPatient Discounts

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            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.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.