Generic
Mefloquine
2 brands available in the market
At a glance
Mefloquine is an antiparasitic medicine used for the treatment and prophylaxis of malaria. It acts as a blood schizonticide active against the erythrocytic stages of Plasmodium species.
Description
Mefloquine is a 4-methanolquinine antimalarial agent that interferes with the parasite's ability to metabolize and utilize erythrocyte hemoglobin. It produces swelling of Plasmodium falciparum food vacuoles. It is effective against chloroquine-resistant malaria parasites.
Indications
- Acute malaria infections caused by Plasmodium falciparum (chloroquine-susceptible and resistant strains)
- Malaria caused by P. vivax
- Prophylaxis of P. falciparum and P. vivax malaria infections
Therapeutic class
Anti-malarial Drugs
Pharmacological class
4-Methanolquinine Antimalarial
Pharmacology
Mefloquine acts as a blood schizonticide active against the erythrocytic stages of Plasmodium species. It produces swelling of Plasmodium falciparum food vacuoles and forms toxic complexes with free heme, damaging membranes.
Mechanism of action
Destroys the erythrocytic stage of malaria parasites to treat and prevent infection.
Dosage
Adult Dose (Oral):
- Acute malaria: 5 tablets (total 1250 mg) as a single dose OR 750 mg initially, then 500 mg 6-12 hours later
- Malaria prophylaxis: 250 mg once weekly (start 1-3 weeks before exposure, continue 4 weeks after leaving)
Children (6 months+): 20-25 mg/kg single dose (max 1250 mg) OR 15 mg/kg initially, then 10 mg/kg 6-12 hours later
Administration
- Swallow tablet whole; do not chew, crush or break
- Take with food (with a full glass of water)
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Prophylaxis (except <1%):
- Vomiting, dizziness, syncope, extrasystoles
Treatment:
- Dizziness, myalgia, nausea, fever
- Headache, vomiting, chills, diarrhea, skin rash
- Abdominal pain, fatigue, loss of appetite, tinnitus
Precautions & warnings
- May cause psychiatric symptoms (anxiety, paranoia, depression to hallucinations and psychotic behavior)
- Increased risk of seizures in patients with epilepsy
- Caution when driving, piloting aircraft, and operating machinery
- Prolonged elimination in patients with impaired liver function
Contraindications
- Hypersensitivity to mefloquine or related compounds (quinine, quinidine)
- Active depression, recent history of depression, generalized anxiety disorder, psychosis, schizophrenia
- History of convulsions
- Severe hepatic impairment
- Concomitant use with halofantrine
Drug interactions
- Increased risk of ECG abnormalities with quinine/chloroquine, antihistamines, TCAs, phenothiazines
- Increased seizure risk with quinidine/quinine
- Loss of seizure control with valproic acid, phenobarbital, carbamazepine, phenytoin
- Increased QT prolongation and arrhythmia risk with ketoconazole
- Cardiotoxicity risk with digoxin, Ca channel blockers, antiarrhythmics
- Potentially fatal cardiac arrhythmias with halofantrine (avoid)
Food interactions
Caution with alcohol; consult your doctor.
Use in pregnancy
Use in Pregnancy: Mefloquine may be unsafe during pregnancy; animal studies have shown harmful effects on the fetus. Consult your doctor.
Use in lactation
Use in Lactation: Mefloquine is excreted in breast milk in small amounts; probably safe but caution is advised.
Pediatric use
Dose established for children over 6 months.
Geriatric use
No differences in responses between elderly and younger patients observed.
Renal / hepatic impairment
Renal Impairment: Limited information available; consult your doctor.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed; not recommended in severe liver disease.
Overdose effects
Overdose symptoms more pronounced; induce vomiting or gastric lavage; monitor cardiac function, neurologic and psychiatric status; symptomatic treatment.
Storage conditions
Store in a cool dry place, protected from light; keep out of reach of children.
Chemical structure
Mefloquine