mefloquine (Lariam)
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Introduction
Tradename: Lariam.
Indications
- prevention & treatment of malaria
Contraindications
- pregnancy (may be used in 2nd & 3rd trimester)
- 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
- bioavailability: > 85%
- distribution:
- breast milk, blood, urine, CSF, concentrates in erythrocytes
- protein-binding 98%
- elimination 1/2life: 21-22 days
- 1.5-9% excreted unchanged in the urine
elimination via liver
1/2life = 2-3 weeks
protein binding = 98 %
Adverse effects
- most common (1-10%)
- uncommon (< 1%)
- other
- prolongs QT interval
- polymorphisms in MRD1 may predispose to neuropsychiatric adverse effects[6]
- boxed warning[8]
- neurologic adverse effects
- psychiatric adverse effects
- anxiety, mistrustful, depression, hallucinations
Drug interactions
Laboratory
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 1175
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, 16. American College of Physicians, Philadelphia 1998, 2012
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 5.0 5.1 Prescriber's Letter 9(7):40 2002 Prescriber's Letter 9(10):57 2002
- ↑ 6.0 6.1 Aarnoudse ALHJ et al, MDR1 gene polymorphisms are associated with neuropsychiatric adverse effects of mefloquine. Clin Pharmacol Ther 2006, 80:367 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17015054
- ↑ Schlagenhauf P, Petersen E. Malaria chemoprophylaxis: strategies for risk groups. Clin Microbiol Rev. 2008 Jul;21(3):466-72 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18625682
- ↑ 8.0 8.1 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
- ↑ 9.0 9.1 Deprecated Reference
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=40692
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=456309
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4046
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=441362
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=332535