Pronunciation: MEF-loe-kwin HYE-droe-KLOR-ide
Class: Antimalarial preparation
- Tablets, oral 250 mg
Antimalarial agent that acts as a blood schizonticide. Mechanism of action is unknown.
T max is 6 to 24 h. Food enhances the rate and extent of absorption, increasing bioavailability approximately 40%.
Vd is approximately 20 L/kg and the protein binding is 98%.
Metabolized in the liver by CYP3A4. Two metabolites have been identified.
The total Cl is 30 mL/min and the half-life is between 2 and 4 wk (mean, approximately 3 wk).
Indications and Usage
Treatment of mild to moderate acute malaria caused by mefloquine-susceptible strains of Plasmodium falciparum or Plasmodium vivax . Prevention of malaria caused by P. falciparum or P. vivax .
Hypersensitivity to any component of the product or to related compounds (eg, quinine, quinidine); for prophylaxis in patients with active depression, generalized anxiety disorder, a recent history of depression, psychosis, or schizophrenia or other major psychiatric disorders, or with a history of convulsions.
Dosage and AdministrationTreatment of Malaria
PO 1,250 mg as a single dose.Children (6 mo and older)
PO 20 to 25 mg/kg as a single dose or split into 2 doses 6 to 8 h apart.Prevention of Malaria
PO 250 mg once weekly starting 1 wk before exposure and continuing 4 wk after.Children
PO 5 mg/kg once weekly starting with 1 wk before exposure and continuing 4 wk after.Weight 20 to 30 kg
PO ½ tablet.Weight 30 to 45 kg
PO ¾ tablet.Weight more than 45 kg
PO 1 tablet.
- Administer with food and at least 240 mL of water.
- The dose may be crushed and suspended in a small amount of water, milk, or other beverage.
- Patients with acute P. vivax need subsequent treatment with 8-aminoquinoline derivative to prevent relapse.
- If a full treatment course with mefloquine does not lead to improvement within 48 to 72 h, do not use mefloquine for re-treatment. Similarly, if prophylaxis with mefloquine has failed, do not use mefloquine for curative treatment.
- In children, use of mefloquine has been associated with early vomiting. If a significant loss of drug product is observed or suspected because of vomiting, a second full dose should be administered to patients who vomit less than 30 min after receiving a dose. If vomiting occurs 30 to 60 min after a dose, an additional half-dose should be given. If vomiting recurs, monitor the patient closely and consider alternative treatment if improvement is not observed within a reasonable time frame.
Store at 59° to 86°F.
Drug InteractionsAnticonvulsants (eg, carbamazepine, phenobarbital, phenytoin, valproic acid)
Reduced seizure control. Monitor anticonvulsant blood concentrations and adjust the dosage as necessary.Bacterial vaccines, live (ie, oral live typhoid vaccines)
When mefloquine is taken concurrently with oral live typhoid vaccines, attenuation of immunization cannot be excluded. Vaccinations with attenuated live bacteria should be completed at least 3 days before the first dose of mefloquine.Beta-adrenergic blockers (ie, propranolol)
There has been 1 report of cardiopulmonary arrest with full recovery in a patient taking propranolol.Chloroquine
The risk of convulsions may be increased with concomitant mefloquine. In addition, the risk of ECG abnormalities may be increased. If chloroquine is used in the initial treatment of severe malaria, delay mefloquine administration until at least 12 h after the last dose of chloroquine.Drugs known to alter cardiac conduction (eg, antiarrhythmic, antidepressants, antihistamines, beta-adrenergic blockers, calcium channel blockers, H 2 blockers, paliperidone, tricyclic phenothiazines, ziprasidone)
Potential for QT interval prolongation. If coadministration is not contraindicated in the respective product information, monitor patients for QT prolongation, especially when a new drug is added to a stable regimen of another QT-prolonging agent.Halofantrine, ketoconazole
Concurrent use can cause potentially fatal QTc interval prolongation. Do not give halofantrine with or within 15 wk of the last dose of mefloquine.Protease inhibitors (eg, ritonavir)
Protease inhibitor plasma concentrations may be reduced, decreasing the efficacy. Additional clinical monitoring is warranted.Rabies vaccine
Antibody response to rabies vaccine may be decreased. Mean serum titers of rabies antibody may be lower than expected. International travelers should complete a 3-dose rabies vaccination series before starting mefloquine. If this is not possible, the rabies vaccine should be given IM and not intradermally.Related compounds (eg, quinine, quinidine)
Increased risk of seizures and ECG abnormalities. If these agents are to be used in the initial treatment of severe malaria, delay mefloquine administration until at least 12 h after the last dose of quinine or quinidine.Rifampin
Mefloquine plasma concentrations may be reduced, decreasing the pharmacologic effects. Coadminister with caution.Warfarin
Anticoagulant effects of warfarin may be increased. Monitor anticoagulant activity and adjust the warfarin dose as needed.
AV block, bradycardia, chest pain, extrasystoles, flushing, hypertension, hypotension, irregular heart rate, syncope, tachycardia or palpitation (postmarketing).
Dizziness, fatigue, headache; aggression, agitation, anxiety, asthenia, confusion, convulsions, depression, encephalopathy, hallucinations, malaise, memory impairment, mood swings, panic attacks, psychotic or paranoid reactions, restlessness, sensory and motor neuropathies, sleep disorders, somnolence, suicidal ideation, suicide, vertigo (postmarketing).
Skin rash; erythema, erythema multiforme, exanthema, hair loss, hyperhidrosis, pruritus, Stevens-Johnson syndrome, urticaria (postmarketing).
Tinnitus; vestibular disorders including hearing impairment, visual disturbances (postmarketing).
Vomiting (3%); abdominal pain, diarrhea, loss of appetite, nausea; dyspepsia (postmarketing).
Leukocytosis, thrombocytopenia; agranulocytosis, aplastic anemia (postmarketing).
Drug-related hepatic disorders from asymptomatic transient transaminase elevations to hepatic failure (postmarketing).
Decreased Hct, transient elevation of transaminases.
Myalgia; arthralgia, muscle cramps, muscle weakness (postmarketing).
Dyspnea, pneumonitis of possible allergic etiology (postmarketing).
Chills; fever (postmarketing).
Category B .
Excreted in breast milk.
Safety and efficacy in children younger than 6 mo have not been established.
Weigh the benefits of therapy against the possibility of adverse cardiac effects in elderly patients.
Reactions may occur, ranging from mild cutaneous events to anaphylaxis.
Elimination of mefloquine may be prolonged, leading to higher plasma levels and a higher risk of adverse reactions.
Special Risk Patients
Use with caution in patients with a history of depression or psychiatric disturbances.
May cause psychiatric symptoms ranging from anxiety, paranoia, and depression to hallucinations and psychotic behavior. Occasionally, these symptoms continue long after therapy with mefloquine has stopped. Rare cases of suicidal ideation and suicide have been reported.
Risk of ECG alterations, sinus bradycardia, sinus arrhythmia, first-degree AV block, prolonged QTc interval, and abnormal T waves.
Increased risk of seizures.
Agranulocytosis and aplastic anemia have been reported.
ECG abnormalities, neuropsychiatric symptoms.
- Instruct patients to read the Medication Guide before use and to carry the information wallet card with them.
- Advise patients to take each prophylactic dose at the same time each day with food and at least 8 oz of water.
- Instruct patients taking mefloquine for prophylaxis that the first dose should be taken 1 wk prior to arrival in a malaria-infected area and that subsequent doses should be taken on the same day of the week while in the malaria-infected area and for 4 wk after leaving the malaria-infected area.
- Advise patients that protective clothing, insect repellants, and bednets are important components of malaria prophylaxis.
- Instruct patients taking prophylactic doses to discontinue the drug and notify their health care provider immediately if any of the following develop: acute anxiety, depression, restlessness, confusion, paranoia, hallucinations, or change in behavior. Alternative therapy will be necessary if mefloquine is discontinued.
- Advise patients to notify their health care provider if severe or persistent vomiting or diarrhea develops, vomiting within 1 h of taking a dose occurs often, other bothersome adverse reactions occur, or therapy is prematurely discontinued for any reason.
- Advise patients that the drug may cause dizziness or other nervous system disorders, and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
- Advise patients that if a febrile illness develops during or after return from a malaria-endemic area, they should seek medical attention and inform their health care provider of possible malaria exposure.
Copyright © 2009 Wolters Kluwer Health.
More about mefloquine
- Other brands: Lariam