MEFLOQUINE HYDROCHLORIDE (me-flo'quine)
Lariam Classifications: antimalarial; Therapeutic: antimalarial Prototype: Chloroquine Pregnancy Category: C
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Availability
250 mg tablets
Action
Antimalarial agent, structurally related to quinine.
Therapeutic Effect
Effective against all types of malaria, including chloroquine-resistant malaria.
Uses
Treatment of mild to moderate acute malarial infections, prevention of chloroquine-resistant malaria caused by Plasmodium falciparum and P. vivax.
Contraindications
Hypersensitivity to mefloquine or a related compound; with a calcium channel blocking agent, severe heart arrhythmias, history
of QTc prolongation; aggressive behavior; active depression, or history of depression, suicidal ideation; generalized anxiety
disorder, psychosis, schizophrenia, or other major psychiatric disorders; seizure disorders; pregnancy (category C); lactation.
Cautious Use
Persons piloting aircraft or operating heavy machinery.
Route & Dosage
Note: FDA has NOT approved use of mefloquine in children, and the U.S. Public Health Service does NOT recommend its use in children <15
kg or in pregnant women
Treatment of Malaria Adult: PO 1250 mg (5 tablets) as single oral dose taken with at least 8 oz of water Child: PO 2030 mg/kg as single dose
Prophylaxis for Malaria Adult: PO 250 mg once/wk x 4 wk (beginning 1 wk before travel), then 250 mg every other wk for duration of exposure
and for 2 doses after leaving endemic area Child: PO 1519 kg, 1/4 tablet; 2030 kg, ? tablet; 3145 kg, ? tablet
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Administration
Oral
- Give with food and at least 8 oz water.
- Do not give concurrently with quinine or quinidine; wait at least 12 h beyond last dose of either drug before administering
mefloquine.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)
Body as a Whole: Arthralgia, chills,
fatigue, fever.
CNS: Dizziness, nightmares, visual disturbances, headache, syncope, confusion, psychosis, aggression, suicide ideation (rare).
CV: Bradycardia, ECG changes (including QT
c prolongation), first-degree AV block.
GI: Nausea, vomiting, abdominal pain, anorexia, diarrhea.
Skin: Rash, itching.
Diagnostic Test Interference
Transient increase in liver transaminases.
Interactions
Drug: Mefloquine can prolong cardiac conduction in patients taking
beta blockers,
calcium channel blockers, and possibly
digoxin. Quinine may decrease plasma mefloquine concentrations. Mefloquine may decrease
valproic acid serum concentrations by increasing its hepatic metabolism. Administration with
chloroquine may increase risk of seizures. Increased risk of cardiac arrest and seizures with
quinidine.
Pharmacokinetics
Absorption: 85% absorbed, concentrates in red blood cells.
Onset: 59 and 28 h for parasite and fever clearance times in patients with
P. vivax infections, respectively; 166 and 93 h in patients with
P. malariae infections.
Distribution: Concentrated in red blood cells due to high-affinity binding to red blood cell membranes; 98% protein bound; distributed
minimally into breast milk.
Metabolism: In liver.
Elimination: Primarily in bile and feces.
Half-Life: 1021 d (shorter in patients with acute malaria).
Nursing Implications
Assessment & Drug Effects
- Monitor carefully during prophylactic use for development of unexplained anxiety, depression, restlessness, or confusion;
such manifestations may indicate a need to discontinue the drug.
- Evaluate cardiac and liver functions periodically with prolonged use.
- Lab tests: Monitor periodically CBC with differential during prolonged use.
- Monitor blood levels of anticonvulsants with concomitant therapy closely.
Patient & Family Education
- Take drug on the same day each week when used for malaria prophylaxis.
- Do not perform potentially hazardous activities until response to drug is known.
- Report any of the following immediately: Fever, sore throat, muscle aches, visual problems, anxiety, confusion, mental depression,
hallucinations.