Active Ingredient:

Each tablet contains Mefloquine Hydrochloride USP equivalent to 250 mg of mefloquine base.

Excipients:

• Lactose monohydrate
• Corn starch
• Magnesium stearate
• Sodium starch glycolate
• Microcrystalline cellulose
• Hypromellose
• Titanium dioxide (E171)
• Macrogol 4000

For a full list of excipients, see section 6.1.

Tablets

White to off-white, round, biconvex tablets, approximately 11 mm in diameter, scored on one side.

The tablet can be divided into equal halves.

4.1 Therapeutic Indications

Treatment of uncomplicated malaria

• Treatment of acute, uncomplicated Plasmodium falciparum malaria in adults and children weighing more than 5 kg
• Treatment of acute, uncomplicated Plasmodium vivax malaria

Prophylaxis of malaria

• Prophylaxis of P. falciparum malaria, including areas where chloroquine resistance has been reported

4.2 Posology and Method of Administration

Adults including elderly:

• Treatment: 5 tablets (1250 mg) as a single dose
• Prophylaxis: 1 tablet (250 mg) once weekly

Children:

• Treatment: Approximately 25 mg/kg total dose administered as a single dose
• Prophylaxis: Approximately 5 mg/kg once weekly

Method of Administration:

For oral use. Tablets should be taken with food and at least 240 ml of water.

4.3 Contraindications

• Hypersensitivity to mefloquine or related compounds (quinine, quinidine)
• History of seizures or epilepsy
• Severe psychiatric disorders including depression, anxiety, or psychosis
• Concurrent use of chloroquine
• Pregnancy (first trimester)

4.4 Special Warnings and Precautions

Neuropsychiatric reactions:

• May cause anxiety, depression, hallucinations, or psychotic reactions
• Monitor patients for psychiatric symptoms
• Discontinue if neuropsychiatric symptoms develop

Cardiac effects:

• May cause QT interval prolongation
• Use with caution in patients with cardiac arrhythmias

Pregnancy and lactation:

• Contraindicated in first trimester of pregnancy
• Use with caution in second and third trimesters
• Excreted in breast milk - use with caution

4.5 Interaction with Other Medicinal Products

Contraindicated combinations:

• Chloroquine - increased risk of convulsions
• Quinidine, quinine - increased cardiac toxicity

Combinations requiring precautions:

• Anti-arrhythmics - increased QT prolongation risk
• Antipsychotics - increased neuropsychiatric effects
• Antiepileptics - reduced mefloquine efficacy

4.6 Fertility, Pregnancy and Lactation

Pregnancy:

• First trimester: contraindicated
• Second/third trimesters: use only if benefit outweighs risk

Lactation:

• Excreted in breast milk
• Use with caution in breastfeeding women

4.7 Effects on Ability to Drive and Use Machines

May cause dizziness, vertigo, or neuropsychiatric effects that may impair ability to drive or operate machinery. Patients should be advised accordingly.

4.8 Undesirable Effects

Very common (≥10%):

• Nausea, vomiting, diarrhea
• Dizziness, vertigo
• Headache
• Sleep disturbances, abnormal dreams

Common (1-10%):

• Anxiety, depression
• Fatigue, weakness
• Abdominal pain
• Pruritus, rash

Rare (<1%):

• Seizures
• Psychotic reactions
• Cardiac arrhythmias
• Severe skin reactions

4.9 Overdose

Symptoms:

• Nausea, vomiting, abdominal pain
• Dizziness, confusion, seizures
• Cardiac arrhythmias

Management:

• Gastric lavage if within 1 hour of ingestion
• Activated charcoal
• Supportive care and monitoring
• Treat seizures with benzodiazepines

5.1 Pharmacodynamic Properties

Pharmacotherapeutic group: Antimalarial (ATC code: P01BB01)

Mechanism of action:

Mefloquine is a 4-quinoline methanol compound with blood schizonticidal activity. It acts by inhibiting heme polymerization in the malaria parasite food vacuole, leading to toxic heme accumulation and parasite death.

Pharmacodynamic effects:

• Rapid parasite clearance
• Fever resolution within 48-72 hours
• Long duration of action

5.2 Pharmacokinetic Properties

Absorption:

• Rapidly absorbed from gastrointestinal tract
• Tmax: 6-8 hours post-dose
• Bioavailability: >90%

Distribution:

• Volume of distribution: 20-30 L/kg
• Protein binding: 99% to albumin
• Extensive tissue distribution

Metabolism:

• Hepatic metabolism via CYP3A4
• Minor metabolites identified

Elimination:

• Terminal half-life: 2-3 weeks
• Primarily fecal excretion
• Renal excretion: <10%

5.3 Preclinical Safety Data

Animal toxicity:

• No significant toxicity at therapeutic doses
• No evidence of carcinogenicity
• No mutagenic potential in standard assays

Reproductive toxicity:

• No teratogenic effects in animal studies
• High doses associated with fetal toxicity

6.1 List of Excipients

• Lactose monohydrate
• Corn starch
• Magnesium stearate
• Sodium starch glycolate
• Microcrystalline cellulose
• Hypromellose
• Titanium dioxide (E171)
• Macrogol 4000
• Purified water

6.2 Incompatibilities

Not applicable.

6.3 Shelf Life

3 years when stored in original packaging.

6.4 Special Precautions for Storage

Store in a dry place at room temperature (20-25°C). Protect from light. Keep container tightly closed.

6.5 Nature and Contents of Container

Packaging:

• Blister packs of 10 tablets
• Blister packs of 20 tablets
• HDPE bottles of 100 tablets

Container materials:

• PVC/PVDC blister foil
• Aluminum blister foil
• High-density polyethylene bottles

6.6 Special Precautions for Disposal

Any unused medicinal product or waste material should be disposed of in accordance with local requirements.

Taj Pharmaceuticals Ltd.

Valsad, Gujarat, India 396155

India

Telephone: 24/7 +91 84484 44095 / 8071 555 357

Email: info@tajpharma.com

Marketing Authorisation Number: IN/ML/2024/001

Date of Authorisation: 15 January 2024

Date of Revision: 15 January 2024

Date of Revision: 15 January 2024