Lariam Indication:

For the treatment of mild to moderate acute malaria caused by Lariamuine-susceptible strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. Also for the prophylaxis of Plasmodium falciparum and Plasmodium vivax malaria infections, including prophylaxis of chloroquine-resistant strains of Plasmodium falciparum.

Lariam Mechanism Of Action:

Lariam has been found to produce swelling of the Plasmodium falciparum food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components.

Lariam Drug Interactions:

Anisindione Lariam can increase the anticoagulant effect
Dicumarol Lariam can increase the anticoagulant effect
Acenocoumarol Lariam can increase the anticoagulant effect
Warfarin Lariam can increase the anticoagulant effect
Halofantrine Increased risk of cardiac toxicity
Rifampin Rifampin lowers mefloquine levels
Ritonavir Lariam decreases the effect of ritonavir
Ziprasidone Increased risk of cardiotoxicity and arrhythmias

Lariam Food Interactions:

Avoid alcohol.
Take with food.
Take with a full glass of water.

Lariam Generic Name:

Synonyms:

  • Mefloquine aziridine
  • Mefloquine HCL
  • Mefloquinone

Drug Type:

Small Molecule; Approved

Absorption:

Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption.

Toxicity (Overdose):

Oral, rat: LD50 = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss.

Protein Binding:

98%

Biotransformation:

Hepatic. Two metabolites have been identified in humans. The main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, is inactive against Plasmodium falciparum. The second metabolite, an alcohol, is present in minute quantities.

Half Life:

2 to 4 weeks

Dosage Forms of Lariam:

Tablet Oral

Chemical IUPAC Name:

[2,8-bis(trifluoromethyl)quinolin-4-yl]-piperidin-2-ylmethanol

Organisms Affected:

Plasmodium

Lariam to general, pharmacology

General, pharmacology..