Mefloquine

DEA Class; Rx

Common Brand Names; Lariam

  • Antimalarials

Oral antimalarial agent used for malaria prophylaxis or treatment. Prophylactic dosing should begin 1 week before entering endemic area and continue for 4 weeks after leaving. Alternative antimalarial in areas where chloroquine- and proguanil-resistant strains of malaria exist (i.e., European countries). Treatment of choice for malaria in the United States.

Indicated for the treatment of mild-to-moderate acute malaria caused by mefloquine-susceptible strains of P. falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax

For the treatment of malaria.

Hypersensitivity to mefloquine, related drugs (eg, quinidine, quinine)

Do not prescribe for prophylaxis in patients with active or recent history of depression, generalized anxiety disorder; history of psychosis, schizophrenia, other major psychiatric disorders, or convulsions

  • Anxiety
  • Difficulty concentrating
  • Headache
  • Insomnia
  • Lightheadedness
  • Vertigo
  • Vomiting
  • Diarrhea
  • Stomach pain
  • Nausea
  • Visual disturbances
  • Tinnitus

In case of life-threatening, serious or overwhelming malaria infections due to P. falciparum, patients should be treated with an IV antimalarial drug; following completion of IV treatment, mefloquine may be given to complete the course of therapy

May increase QT interval; caution with other drugs known to prolong QT interval; halofantrine or strong CYP3A4 inhibitors (eg, ketoconazole) should not be administered concomitantly or within 15 weeks of last dose of mefloquine due to risk of a potentially fatal prolongation of QTc interval

Transitory and clinically silent ECG alterations have been reported during therapy; alterations included sinus bradycardia, sinus arrhythmia, first-degree AV-block, and abnormal T waves; benefits of therapy should be weighed against possibility of adverse effects in patients with cardiac disease

Caution with hepatic impairment

If drug is to be administered for a prolonged period, periodic evaluations including liver function tests and evaluations for neuropsychiatric effects should be performed

Agranulocytosis and aplastic anemia reported

Geographical drug resistance patterns of P. falciparum occur and the preferred choice of malaria prophylaxis might be different from one area to another

Periodic ophthalmic examinations recommended; retinal abnormalities seen in humans with long-term chloroquine use have not been observed with mefloquine use; however, long- term feeding of mefloquine to rats resulted in dose-related ocular lesions

Pregnancy Category: B

Lactation: Minimally excreted in human breast milk; based on a study in a few subjects, low concentrations (3% to 4%) excreted; caution advised

Adults

1,250 mg PO once for treatment or 250 mg PO once/week for prophylaxis.

Geriatric

1,250 mg PO once for treatment or 250 mg PO once/week for prophylaxis.

Adolescents

more than 45 kg: 20 to 25 mg/kg PO (Max: 1,250 mg) once for treatment or 250 mg PO once/week for prophylaxis.
30 to 45 kg: 20 to 25 mg/kg PO once for treatment or 187.5 mg (3/4 tablet) PO once/week for prophylaxis.

Children

more than 45 kg: 20 to 25 mg/kg PO (Max: 1,250 mg) once for treatment or 250 mg PO once/week for prophylaxis.
30 to 45 kg: 20 to 25 mg/kg PO once for treatment or 187.5 mg (3/4 tablet) PO once/week for prophylaxis.
20 to 29 kg: 20 to 25 mg/kg PO once for treatment or 125 mg (1/2 tablet) PO once/week for prophylaxis.
less than 20 kg: Safety and efficacy have not been established; however, 20 to 25 mg/kg PO once for treatment or 62.5 mg (1/4 tablet) PO once/week for prophylaxis has been recommended.

Infants

6 to 11 months and weighing 5 kg or more: Safety and efficacy have not been established; however, 20 to 25 mg/kg PO once for treatment or 5 mg/kg/dose PO once/week for prophylaxis has been used.
1 to 5 months or weighing less than 5 kg: Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Mefloquine

tablet

  • 250mg

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