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mefloquine (Lariam)

Tradename: Lariam. Indications: - prevention & treatment of malaria - Plasmodium falciparum, Plasmodium vivax [9] Contraindications: 1) pregnancy (may be used in 2nd & 3rd trimester) 2) avoid in patients with history of psychiatric illness [5] Dosage: - malarial prophylaxis: 250 mg PO weekly from 1 week before exposure to 4 weeks post exposure - acute malaria: 1250 mg single dose Tabs: 250 mg. Pharmacokinetics: 1) bioavailability: > 85% 2) distribution: - breast milk, blood, urine, CSF, concentrates in erythrocytes 3) protein-binding 98% 4) elimination 1/2life: 21-22 days 5) 1.5-9% excreted unchanged in the urine Adverse effects: 1) most common (1-10%) - nausea/vomiting, difficulty concentrating, headache, insomnia, lightheadedness, dizziness, vertigo, diarrhea, epigastric pain, visual disturbances 2) uncommon (< 1%) - sinus bradycardia, extrasystoles, anxiety, syncope, confusion, psychosis, hallucinations, seizures, depression, suicidal ideation 3) other - prolongs QT interval - polymorphisms in MRD1 may predispose to neuropsychiatric adverse effects [6] - boxed warning [8] - neurologic adverse effects - dizziness, ataxia, tinnitus - psychiatric adverse effects - anxiety, mistrustful, depression, hallucinations Drug interactions: 1) quinine 2) quinidine 3) beta-blockers 4) Ca+2 channel blockers 5) chloroquine 6) valproic acid Laboratory: - mefloquine in serum/plasma - mefloquine in urine

Interactions

drug interactions drug adverse effects of antimalarials

Related

malaria prophylaxis for malaria

General

antimalarial

Properties

MISC-INFO: elimination route LIVER 1/2life 2-3 WEEKS protein-binding 98% pregnancy-category C + safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 1175
  3. Medical Knowledge Self Assessment Program (MKSAP) 11, 16. American College of Physicians, Philadelphia 1998, 2012
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Prescriber's Letter 9(7):40 2002 Prescriber's Letter 9(10):57 2002
  6. Aarnoudse ALHJ et al, MDR1 gene polymorphisms are associated with neuropsychiatric adverse effects of mefloquine. Clin Pharmacol Ther 2006, 80:367 PMID: 17015054
  7. Schlagenhauf P, Petersen E. Malaria chemoprophylaxis: strategies for risk groups. Clin Microbiol Rev. 2008 Jul;21(3):466-72 PMID: 18625682
  8. FDA MedWatch. July 29, 2013 Mefloquine Hydrochloride: Drug Safety Communication - Label Changes Due To Risk of Serious Psychiatric and Nerve Side Effects. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm362887.htm
  9. Deprecated Reference