Mefloquine Information
Mefloquine (Mefloquine hydrochloride)
Mefloquine (Mefloquine hydrochloride) Description:
Mefloquine (Mefloquine hydrochloride) hydrochloride is an antimalarial agent available as 250-mg tablets of Mefloquine (Mefloquine hydrochloride) hydrochloride (equivalent to 228.0 mg of the free base) for oral administration.
Mefloquine (Mefloquine hydrochloride) 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.
The inactive ingredients are colloidal silicon dioxide, corn starch, crospovidone, lactose monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinized starch, poloxamer and talc.
Mefloquine (Mefloquine hydrochloride) Indications And Usage:
Mefloquine (Mefloquine hydrochloride) hydrochloride tablets are indicated for the treatment of mild to moderate acute malaria caused by Mefloquine (Mefloquine hydrochloride) -susceptible strains of (both chloroquine-susceptible and resistant strains) or by There are insufficient clinical data to document the effect of Mefloquine (Mefloquine hydrochloride) in malaria caused by or
Mefloquine (Mefloquine hydrochloride) Contraindications:
Use of Mefloquine (Mefloquine hydrochloride) hydrochloride tablets are contraindicated in patients with a known hypersensitivity to Mefloquine (Mefloquine hydrochloride) or related compounds (e.g., quinine and quinidine) or to any of the excipients contained in the formulation. Mefloquine (Mefloquine hydrochloride) hydrochloride tablets should not be prescribed for prophylaxis in patients with active depression, a recent history of depression, generalized anxiety disorder, psychosis, or schizophrenia or other major psychiatric disorders, or with a history of convulsions.
Mefloquine (Mefloquine hydrochloride) Precautions:
Hypersensitivity reactions ranging from mild cutaneous events to anaphylaxis cannot be predicted.
In patients with epilepsy, Mefloquine (Mefloquine hydrochloride) may increase the risk of convulsions. The drug should therefore be prescribed only for curative treatment in such patients and only if there are compelling medical reasons for its use (see PRECAUTIONS: Drug Interactions).
Caution should be exercised with regard to activities requiring alertness and fine motor coordination such as driving, piloting aircraft, operating machinery and deep-sea diving, as dizziness, a loss of balance, or other disorders of the central or peripheral nervous system have been reported during and following the use of Mefloquine (Mefloquine hydrochloride) . These effects may occur after therapy is discontinued due to the long half-life of the drug. Mefloquine (Mefloquine hydrochloride) should be used with caution in patients with psychiatric disturbances because Mefloquine (Mefloquine hydrochloride) use has been associated with emotional disturbances (see ADVERSE REACTIONS).
In patients with impaired liver function the elimination of Mefloquine (Mefloquine hydrochloride) may be prolonged, leading to higher plasma levels.
This drug has been administered for longer than 1 year. If the drug is to be administered for a prolonged period, periodic evaluations including liver function tests should be performed. Although retinal abnormalities seen in humans with long-term chloroquine use have not been observed with Mefloquine (Mefloquine hydrochloride) use, long-term feeding of Mefloquine (Mefloquine hydrochloride) to rats resulted in dose-related ocular lesions (retinal degeneration, retinal edema and lenticular opacity at 12.5 mg/kg/day and higher) (see ANIMAL TOXICOLOGY). Therefore, periodic ophthalmic examinations are recommended.
Parenteral studies in animals show that Mefloquine (Mefloquine hydrochloride) , a myocardial depressant, possesses 20% of the antifibrillatory action of quinidine and produces 50% of the increase in the PR interval reported with quinine. The effect of Mefloquine (Mefloquine hydrochloride) on the compromised cardiovascular system has not been evaluated. However, transitory and clinically silent ECG alterations have been reported during the use of Mefloquine (Mefloquine hydrochloride) . Alterations included sinus bradycardia, sinus arrhythmia, first degree AV-block, prolongation of the QTc interval and abnormal T waves (see also cardiovascular effects under PRECAUTIONS: Drug Interactions and ADVERSE REACTIONS). The benefits of Mefloquine (Mefloquine hydrochloride) therapy should be weighed against the possibility of adverse effects in patients with cardiac disease.
Medication Guide: As required by law, a Mefloquine (Mefloquine hydrochloride) Hydrochloride Tablets Medication Guide is supplied to patients when Mefloquine (Mefloquine hydrochloride) is dispensed. Patients should be instructed to read the MedGuide when Mefloquine (Mefloquine hydrochloride) is received. The complete text of the MedGuide is reprinted at the end of this document.
Patients should be advised:
Drug-drug interactions with Mefloquine (Mefloquine hydrochloride) have not been explored in detail. There is one report of cardiopulmonary arrest, with full recovery, in a patient who was taking a beta blocker (propranolol) (see PRECAUTIONS: General). The effects of Mefloquine (Mefloquine hydrochloride) on the compromised cardiovascular system have not been evaluated. The benefits of Mefloquine (Mefloquine hydrochloride) therapy should be weighed against the possibility of adverse effects in patients with cardiac disease.
Because of the danger of a potentially fatal prolongation of the QTc interval, halofantrine must not be given simultaneously with or subsequent to Mefloquine (Mefloquine hydrochloride) (see WARNINGS).
Concomitant administration of Mefloquine (Mefloquine hydrochloride) and other related compounds (e.g., quinine, quinidine and chloroquine) may produce electrocardiographic abnormalities and increase the risk of convulsions (see WARNINGS). If these drugs are to be used in the initial treatment of severe malaria, Mefloquine (Mefloquine hydrochloride) administration should be delayed at least 12 hours after the last dose. There is evidence that the use of halofantrine after Mefloquine (Mefloquine hydrochloride) causes a significant lengthening of the QTc interval. Clinically significant QTc prolongation has not been found with Mefloquine (Mefloquine hydrochloride) alone.
This appears to be the only clinically relevant interaction of this kind with Mefloquine (Mefloquine hydrochloride) , although theoretically, coadministration of other drugs known to alter cardiac conduction (e.g., anti-arrhythmic or beta-adrenergic blocking agents, calcium channel blockers, antihistamines or H-blocking agents, tricyclic antidepressants and phenothiazines) might also contribute to a prolongation of the QTc interval. There are no data that conclusively establish whether the concomitant administration of Mefloquine (Mefloquine hydrochloride) and the above listed agents has an effect on cardiac function.
In patients taking an anticonvulsant (e.g., valproic acid, carbamazepine, phenobarbital or phenytoin), the concomitant use of Mefloquine (Mefloquine hydrochloride) may reduce seizure control by lowering the plasma levels of the anticonvulsant. Therefore, patients concurrently taking antiseizure medication and Mefloquine (Mefloquine hydrochloride) should have the blood level of their antiseizure medication monitored and the dosage adjusted appropriately (see PRECAUTIONS: General).
When Mefloquine (Mefloquine hydrochloride) is taken concurrently with oral live typhoid vaccines, attenuation of immunization cannot be excluded. Vaccinations with attenuated live bacteria should therefore be completed at least 3 days before the first dose of Mefloquine (Mefloquine hydrochloride) .
No other drug interactions are known. Nevertheless, the effects of Mefloquine (Mefloquine hydrochloride) on travelers receiving comedication, particularly diabetics or patients using anticoagulants, should be checked before departure.
In clinical trials, the concomitant administration of sulfadoxine and pyrimethamine did not alter the adverse reaction profile.
Use of Mefloquine (Mefloquine hydrochloride) to treat acute, uncomplicated malaria in pediatric patients is supported by evidence from adequate and well-controlled studies of Mefloquine (Mefloquine hydrochloride) in adults with additional data from published open-label and comparative trials using Mefloquine (Mefloquine hydrochloride) to treat malaria caused by in patients younger than 16 years of age. The safety and effectiveness of Mefloquine (Mefloquine hydrochloride) for the treatment of malaria in pediatric patients below the age of 6 months have not been established.
In several studies, the administration of Mefloquine (Mefloquine hydrochloride) for the treatment of malaria was associated with early vomiting in pediatric patients. Early vomiting was cited in some reports as a possible cause of treatment failure. If a second dose is not tolerated, the patient should be monitored closely and alternative malaria treatment considered if improvement is not observed within a reasonable period of time (see DOSAGE AND ADMINISTRATION).
Mefloquine (Mefloquine hydrochloride) Adverse Reactions:
At the doses used for treatment of acute malaria infections, the symptoms possibly attributable to drug administration cannot be distinguished from those symptoms usually attributable to the disease itself.
Among subjects who received Mefloquine (Mefloquine hydrochloride) for prophylaxis of malaria, the most frequently observed adverse experience was vomiting (3%). Dizziness, syncope, extrasystoles and other complaints affecting less than 1% were also reported.
Among subjects who received Mefloquine (Mefloquine hydrochloride) for treatment, the most frequently observed adverse experiences included: dizziness, myalgia, nausea, fever, headache, vomiting, chills, diarrhea, skin rash, abdominal pain, fatigue, loss of appetite, and tinnitus. Those side effects occurring in less than 1% included bradycardia, hair loss, emotional problems, pruritus, asthenia, transient emotional disturbances and telogen effluvium (loss of resting hair). Seizures have also been reported.
Two serious adverse reactions were cardiopulmonary arrest in one patient shortly after ingesting a single prophylactic dose of Mefloquine (Mefloquine hydrochloride) while concomitantly using propranolol (see PRECAUTIONS: Drug Interactions), and encephalopathy of unknown etiology during prophylactic Mefloquine (Mefloquine hydrochloride) administration. The relationship of encephalopathy to drug administration could not be clearly established.
Postmarketing surveillance indicates that the same kind of adverse experiences are reported during prophylaxis, as well as acute treatment.
The most frequently reported adverse events are nausea, vomiting, loose stools or diarrhea, abdominal pain, dizziness or vertigo, loss of balance, and neuropsychiatric events such as headache, somnolence, and sleep disorders (insomnia, abnormal dreams). These are usually mild and may decrease despite continued use.
Occasionally, more severe neuropsychiatric disorders have been reported such as: sensory and motor neuropathies (including paresthesia, tremor and ataxia), convulsions, agitation or restlessness, anxiety, depression, mood changes, panic attacks, forgetfulness, confusion, hallucinations, aggression, psychotic or paranoid reactions and encephalopathy. Rare cases of suicidal ideation and suicide have been reported though no relationship to drug administration has been confirmed.
Other infrequent adverse events include:
The most frequently observed laboratory alterations which could be possibly attributable to drug administration were decreased hematocrit, transient elevation of transaminases, leukopenia and thrombocytopenia. These alterations were observed in patients with acute malaria who received treatment doses of the drug and were attributed to the disease itself.
During prophylactic administration of Mefloquine (Mefloquine hydrochloride) to indigenous populations in malaria-endemic areas, the following occasional alterations in laboratory values were observed: transient elevation of transaminases, leukocytosis or thrombocytopenia.
Because of the long half-life of Mefloquine (Mefloquine hydrochloride) , adverse reactions to Mefloquine (Mefloquine hydrochloride) may occur or persist up to several weeks after the last dose.
Mefloquine (Mefloquine hydrochloride) Overdosage:
In cases of overdosage with Mefloquine (Mefloquine hydrochloride) , the symptoms mentioned under ADVERSE REACTIONS may be more pronounced. The following procedure is recommended in case of overdosage: Induce vomiting or perform gastric lavage, as appropriate. 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.
Mefloquine (Mefloquine hydrochloride) How Supplied:
Mefloquine (Mefloquine hydrochloride) Hydrochloride Tablets are available as:
250 mg: White, oval-shaped, flat-faced, beveled-edge, scored tablet containing 250 mg of Mefloquine (Mefloquine hydrochloride) hydrochloride.
Debossed with stylized
on the scored side and plain on the other side.
Available in bottle of:
7 tablets NDC 21695-449-07
25 tablets NDC 21695-449-25
Store at 20°-25°C (68°-77°F); excursions permitted to 15°-30°C (59°-86°F) [see
USP].
Mefloquine (Mefloquine hydrochloride)
Mefloquine (Mefloquine hydrochloride) Medication Guide
An information wallet card is provided at the end of this Medication Guide. Cut it out and carry it with you when you are taking Mefloquine (Mefloquine hydrochloride) .
This Medication Guide was revised in September 2003. Please read it before you start taking Mefloquine (Mefloquine hydrochloride) and each time you get a refill. There may be new information. This Medication Guide does not take the place of talking with your prescriber (doctor or other health care provider) about Mefloquine (Mefloquine hydrochloride) and malaria prevention. Only you and your prescriber can decide if Mefloquine (Mefloquine hydrochloride) is right for you. If you cannot take Mefloquine (Mefloquine hydrochloride) , you may be able to take a different medicine to prevent malaria.
Do not take Mefloquine (Mefloquine hydrochloride) to malaria if you
To prevent malaria
Mefloquine (Mefloquine hydrochloride) , like all medicines, may cause side effects in some patients. The most frequently reported side effects with Mefloquine (Mefloquine hydrochloride) when used for prevention of malaria include nausea, vomiting, diarrhea, dizziness, difficulty sleeping, and bad dreams. These are usually mild and do not cause people to stop taking the medicine.
Mefloquine (Mefloquine hydrochloride) may cause serious mental problems in some patients. (See “What is the most important information I should know about Mefloquine (Mefloquine hydrochloride) ?”).
Mefloquine (Mefloquine hydrochloride) may affect your liver and your eyes if you take it for a long time. Your prescriber will tell you if you should have your eyes and liver checked while taking Mefloquine (Mefloquine hydrochloride) .
Medicines are sometimes prescribed for conditions not listed in Medication Guides. If you have any concerns about Mefloquine (Mefloquine hydrochloride) , ask your prescriber. This Medication Guide contains certain important information for travelers visiting areas with malaria. Your prescriber or pharmacist can give you information about Mefloquine (Mefloquine hydrochloride) that was written for health care professionals. Do not use Mefloquine (Mefloquine hydrochloride) for a condition for which it was not prescribed. Do not share Mefloquine (Mefloquine hydrochloride) with other people.
This Medication Guide has been approved by the U.S. Food and Drug Administration.
BR-171
Repackaged by:
Rebel Distributors Corp
Thousand Oaks, CA 91320
Mefloquine (Mefloquine hydrochloride) Principal Display Panel
