Lariam

Lariam is part of the drug class:

• Methanolquinolines

If you take too much Lariam, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

Do not use this medication if you are allergic to mefloquine or similar medications such as quinine (Qualaquin) or quinidine (Quinaglute, Quinidex, Quin-Release).

You also should not use mefloquine to prevent malaria if you have a recent history of:

• seizures;
• depression;
• anxiety; or
• schizophrenia or other psychiatric illness.

However, your doctor may prescribe mefloquine to treat malaria even if you do have any of the conditions listed above.

If you have any of these other conditions, you may need a dose adjustment or special tests to safely use this medication:

• liver disease;
• a history of depression;
• epilepsy or other seizure disorder;
• kidney disease;
• severe complications from malaria; or
• uncontrolled vomiting or diarrhea.

FDA pregnancy category C. It is not known whether mefloquine is harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

Malaria is more likely to cause death in a pregnant woman. If you are pregnant, talk with your doctor about the risks of traveling to areas where malaria is common.

Mefloquine can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Mefloquine should not be used to treat malaria in a child younger than 6 months old or who weighs less than 11 pounds. Mefloquine should not be used to prevent malaria in a child who weighs less than 99 pounds.

Do not take halofantrine (Halfan) while you are taking mefloquine or just after you stop taking it. Serious, life-threatening side effects on your heart can occur if you take halofantrine before the mefloquine has cleared from your body.

Avoid taking chloroquine (Aralen Phosphate), quinine (Qualaquin) or quinidine (Quinaglute, Quinidex, Quin-Release) while you are taking mefloquine.

Mefloquine can cause side effects that may impair your thinking or reactions. Be careful if you drive, operate machinery, pilot an airplane, SCUBA dive, or do anything that requires you to be awake and alert.

Your pharmacist can provide more information about mefloquine.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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Some people taking mefloquine have had sudden serious psychiatric or nerve problems, some of which lasted long after they stopped taking this medicine. These side effects can be permanent.

Stop taking mefloquine and call your doctor right away if have any of these side effects: headache, ringing in your ears, dizziness, loss of balance, problems with coordination, anxiety, depression, paranoia, hallucinations, or thoughts about suicide or hurting yourself.

You should not take mefloquine to prevent malaria if you have a recent history of depression, an anxiety disorder, seizures, mental illness (such as schizophrenia), or psychosis.

Since mefloquine is often used as a single dose, you may not be on a dosing schedule. If you are on a weekly schedule, use the missed dose as soon as you remember. Then take the next dose on your next usual dosing day. Do not use extra medicine to make up the missed dose.

Call your doctor for instructions if you forget to take the medicine within 1 week before your travel.

Do not take halofantrine or ketoconazole while you are taking mefloquine and for at least 15 weeks after you stop taking it. Serious, life-threatening side effects on your heart can occur if you take halofantrine before the mefloquine has cleared from your body.

Avoid taking chloroquine, quinine, or quinidine while you are taking mefloquine.

Mefloquine can cause side effects that may impair your thinking or reactions. Be careful if you drive, operate machinery, pilot an airplane, scuba dive, or do anything that requires you to be awake and alert.

Antimalarial; 4-quinolinemethanol derivative; quinine analog.1 2 3 7 161

Metabolized by CYP3A4;1 does not inhibit or induce CYP isoenzymes.1

Substrate for and inhibitor of P-glycoprotein.1

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction with drugs that are CYP3A4 inhibitors (possible increased mefloquine concentrations and increased potential for adverse effects associated with the drug).1 Use concomitantly with caution.1

Potential pharmacokinetic interaction with drugs that are CYP3A4 inducers (possible decreased mefloquine concentrations and possible decreased efficacy of the antimalarial).1 Use concomitantly with caution.1

Pharmacokinetic interactions not expected if mefloquine used concomitantly with drugs that are substrates for CYP isoenzymes.1

Drugs Affecting P-glycoprotein Transport System

Potential pharmacokinetic interactions if used concomitantly with drugs that are substrates for or are known to modify expression of P-glycoprotein; clinical importance unknown.1

Drugs Affecting QT Interval

Possibility of prolongation of QT interval if used concomitantly with other drugs that alter cardiac conduction, including antiarrhythmic agents, β-adrenergic blocking agents, calcium-channel blocking agents, antihistamines, tricyclic antidepressants, and phenothiazines.1 Some experts state that mefloquine may be used concomitantly with β-adrenergic blocking agents in patients without an underlying arrhythmia.105 134

Specific Drugs

• Importance of reading the medication guide supplied with mefloquine.1 Advise patients to carry the information wallet card with them when they are taking mefloquine.1

• For prevention of malaria, necessity of starting mefloquine prophylaxis 1–2 weeks before arriving in an area with malaria.1

• Necessity of taking protective measures to reduce contact with mosquitoes (protective clothing, insect repellents, mosquito nets, remaining in air-conditioned or well-screened areas).1 113 115 121 134

• Possibility of contracting malaria during travel, regardless of prophylactic regimen used.1 113 115 121 134

• Importance of seeking medical attention as soon as possible if febrile illness develops during or after return from a malaria-endemic area and of informing clinician of possible malaria exposure, including instances when such illness was self-treated as malaria during travel.1 113 115 121 134

• Advise patients that some people are unable to take mefloquine because of adverse effects and that it may be necessary to change medications if this occurs.1

• Advise patients that dizziness or vertigo, loss of balance, tinnitus, and other central or peripheral nervous system effects have occurred in patients receiving mefloquine; such effects can persist for months or years after the drug is discontinued and may be permanent in some cases.1 If such symptoms occur, importance of avoiding activities requiring alertness and fine motor coordination (e.g., driving, piloting aircraft, operating machinery, deep-sea diving).1 Caution patients receiving mefloquine for malaria prevention to discontinue the drug and contact their clinician if neurologic effects (e.g., dizziness or vertigo, loss of balance) occur; an alternative antimalarial should be substituted.1

• Advise patients that neuropsychiatric symptoms ranging from severe anxiety, paranoia, and depression to hallucinations and psychotic behavior have occurred in patients receiving mefloquine;1 some manifestations (e.g., acute anxiety, depression, restlessness, confusion) suggest a risk for more serious psychiatric events or adverse neurologic effects.1 Caution patients receiving mefloquine for malaria prevention to discontinue the drug and contact their clinician if neuropsychiatric manifestations or suicidal ideation occurs; an alternative antimalarial should be substituted.1

• Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal products, and any concomitant illnesses.1

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 Advise women of childbearing potential to use effective contraceptive measures while receiving mefloquine and for up to 3 months after drug discontinuance.1

• Importance of advising patients of other important precautionary information.1 (See Cautions.)

Lariam (mefloquine hydrochloride) is an antimalarial agent available as 250-mg tablets of mefloquine hydrochloride (equivalent to 228.0 mg of the free base) for oral administration.

Mefloquine hydrochloride is a 4-quinolinemethanol derivative with the specific chemical name of (R*, S*)-(±)-α-2-piperidinyl-2,8-bis (trifluoromethyl)-4-quinolinemethanol hydrochloride. It is a 2-aryl substituted chemical structural analog of quinine. The drug is a white to almost white crystalline compound, slightly soluble in water.

Mefloquine hydrochloride has a calculated molecular weight of 414.78 and the following structural formula:

The inactive ingredients are ammonium-calcium alginate, corn starch, crospovidone, lactose, magnesium stearate, microcrystalline cellulose, poloxamer #331, and talc.

Symptoms and Signs

In cases of overdosage with Lariam, the symptoms mentioned under ADVERSE REACTIONS may be more pronounced.

Treatment

Patients should be managed by symptomatic and supportive care following Lariam overdose. There are no specific antidotes. Monitor cardiac function (if possible by ECG) and neuropsychiatric status for at least 24 hours. Provide symptomatic and intensive supportive treatment as required, particularly for cardiovascular disturbances.

LactMed Record Number

294

Last Revision Date

20160226

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