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Mefloquine

Generic Medicine
Indications

Mefloquine is indicated for:

  • Acute malaria infections caused by mefloquine-sensitive strains of Plasmodium falciparum (including both chloroquine-sensitive and chloroquine-resistant strains) and Plasmodium vivax
  • Prevention (prophylaxis) of malaria due to P. falciparum and P. vivax
Pharmacology

Mefloquine causes swelling of the food vacuoles in Plasmodium falciparum and is thought to act by forming toxic complexes with free heme, which damage parasite membranes and interfere with essential cellular components. It is a blood schizonticidal antimalarial agent, active against the erythrocytic (blood) stage of malaria parasites. However, it does not act on the hepatic (liver) stage of the parasite. Mefloquine is also effective against chloroquine-resistant malaria strains. It is a chiral compound; studies suggest that the (+) enantiomer is more potent against malaria, while the (−) enantiomer binds to adenosine receptors in the central nervous system, which may be related to its neuropsychiatric side effects.

Dosage Administration

Adult:

  • Malaria prevention: 1 tablet (250 mg) once per week starting 1-2 weeks before departure and continued for 4 weeks after leaving malarious area.
  • Malaria treatment: 5 tablets (5X250 mg) in a single dose (up to max. 1.5 gm) or preferably in 2 divided doses 6 to 8 hours apart.

In Children 6 Months and Older:

  • Malaria prevention: Approximately 5 mg/kg body weight once per week (250 mg for children weighing over 45 kg, decreasing in proportion to body weight for children weighing 45 kg or less).
  • Malaria treatment: 20 to 25 mg/kg body weight which may be split into two doses 6 to 8 hours apart to reduce the occurrence or severity of adverse reactions.

Geriatric Use: Experiences have not identified differences in responses between the elderly and younger patients.

Should be taken with food. Best taken with meals & a full glass of water.

Interactions

Mefloquine may interact with several medicines, leading to increased risks: Concomitant use with quinine, chloroquine, antihistamines, tricyclic antidepressants (TCAs), and phenothiazines may increase ECG abnormalities . Combined use with quinidine or quinine may increase seizure risk. Antiepileptic drugs such as valproic acid, phenobarbital, carbamazepine, and phenytoin may have reduced plasma levels, leading to loss of seizure control. Increased risk of QT prolongation and arrhythmia with ketoconazole. Higher risk of cardiotoxicity when used with digoxin, calcium channel blockers, antiarrhythmics, and beta-blockers. Increased risk of ventricular arrhythmias with amiodarone. Increased risk of convulsions with TCAs, SSRIs, bupropion, antipsychotics, and tramadol. Metoclopramide may increase plasma concentration of mefloquine. May reduce immune response to live typhoid vaccine; live attenuated vaccines should be completed at least 3 days before starting therapy.

মেফ্লোকুইন বিভিন্ন ওষুধের সাথে ব্যবহার করলে পারস্পরিক ক্রিয়া দেখা দিতে পারে:

  • কুইনিন, ক্লোরোকুইন, অ্যান্টিহিস্টামিন, ট্রাইসাইক্লিক অ্যান্টিডিপ্রেসেন্ট (TCA) ও ফেনোথিয়াজিনের সাথে ECG পরিবর্তনের ঝুঁকি বাড়ে
  • কুইনিডিন বা কুইনিনের সাথে খিঁচুনির ঝুঁকি বাড়তে পারে
  • ভ্যালপ্রোইক অ্যাসিড, ফেনোবারবিটাল, কার্বামাজেপিন ও ফেনিটয়িনের সাথে রক্তে ওষুধের মাত্রা কমে খিঁচুনি নিয়ন্ত্রণ হারাতে পারে
  • কেটোকোনাজলের সাথে QT ইন্টারভাল দীর্ঘায়িত ও অ্যারিদমিয়ার ঝুঁকি বাড়ে
  • ডিগক্সিন, ক্যালসিয়াম চ্যানেল ব্লকার, অ্যান্টিঅ্যারিদমিক ও বিটা-ব্লকারের সাথে হৃদযন্ত্রের বিষক্রিয়ার ঝুঁকি বাড়ে
  • অ্যামিওডারোনের সাথে ভেন্ট্রিকুলার অ্যারিদমিয়ার ঝুঁকি বাড়ে
  • TCA, SSRI, বুপ্রোপিয়ন, অ্যান্টিসাইকোটিক ও ট্রামাডলের সাথে খিঁচুনির ঝুঁকি বাড়ে
  • মেটোক্লোপ্রামাইড মেফ্লোকুইনের রক্তের ঘনত্ব বাড়াতে পারে
  • লাইভ টাইফয়েড ভ্যাকসিনের কার্যকারিতা কমতে পারে; লাইভ অ্যাটেনুয়েটেড ভ্যাকসিন মেফ্লোকুইন শুরুর অন্তত ৩ দিন আগে সম্পন্ন করতে হবে
Contraindications

Mefloquine should not be used in patients with hypersensitivity to mefloquine or related compounds such as quinine and quinidine. It is contraindicated for malaria prophylaxis in patients with active or recent depression, generalized anxiety disorder, psychosis, schizophrenia, other major psychiatric disorders, or a history of seizures.

Side Effects
  • Prophylaxis: The most common adverse effects include vomiting, dizziness, fainting, extrasystoles, and other symptoms occurring in less than 1% of users.
  • Treatment: Common effects include dizziness, muscle pain, nausea, fever, headache, vomiting, chills, diarrhea, skin rash, abdominal pain, fatigue, loss of appetite, and tinnitus.
Pregnancy & Lactation

There are no adequate controlled studies in pregnancy. However, available clinical evidence has not shown clear teratogenic effects. Mefloquine should be used during pregnancy only if the expected benefit outweighs potential fetal risk.

Small amounts are excreted in breast milk, but infant safety is not fully established. A decision should be made whether to discontinue breastfeeding or the drug, depending on maternal treatment needs.

Precautions & Warnings

Warnings:Mefloquine may cause psychiatric reactions in some patients, ranging from anxiety, paranoia, and depression to hallucinations and psychotic behavior. Rare cases of suicidal thoughts and suicide have been reported, although a direct causal relationship has not been confirmed. It should be used with caution in patients with a history of depression. Concomitant use with quinine or quinidine may lead to ECG abnormalities and may increase the risk of seizures.

Precautions: Mefloquine may increase seizure risk in patients with epilepsy. Patients should exercise caution when performing activities requiring alertness and coordination, such as driving, operating machinery, or flying aircraft. It should be used carefully in patients with psychiatric disorders. In patients with liver impairment, drug elimination may be delayed, leading to increased plasma levels.

Overdose Effects

In case of overdose, symptoms may become more severe. Management includes:

  • Inducing vomiting or performing gastric lavage when appropriate
  • Monitoring cardiac, neurological, and psychiatric status for at least 24 hours (preferably with ECG)
  • Providing supportive and symptomatic treatment, especially for cardiovascular effects
  • Treating vomiting or diarrhea with appropriate fluid therapy
Therapeutic Class

Anti-malarial drugs

Storage Conditions

Store in a cool, dry place, protected from light.

Common Questions

What is Mefloquine for?

What does Mefloquine do?

 What are the side effects of Mefloquine?

What happens if you take too much Mefloquine?

Can Mefloquine be taken during pregnancy?

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