Pharmacology of Quinine and Mefloquine Mechanism of action Uses Pharmacokinetics Side effects

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Quinine and Mefloquine are antimalarial medications. • • Quinine • • Classification: • • 1. Antimalarial (4-aminoquinoline) • 2. Antiarrhythmic (Class IA) • • Mechanism of Action: • • 1. Interferes with heme detoxification in Plasmodium parasites • 2. Inhibits β-hematin formation • • Indications: • • 1. Malaria treatment (uncomplicated and severe) • 2. Babesiosis • 3. Arrhythmias (off-label) • • Pharmacokinetics: • • 1. Oral bioavailability: 76-88% • 2. Peak plasma concentration: 2-4 hours • 3. Half-life: 9-12 hours • 4. Metabolism: Hepatic (CYP3A4, CYP2C19) • • Adverse Effects: • • 1. Cinchonism (tinnitus, hearing loss, vertigo) • 2. Hypoglycemia • 3. Hypersensitivity reactions • 4. Cardiac toxicity (QT prolongation) • • Contraindications: • • 1. Hypersensitivity to quinine or cinchona alkaloids • 2. Myasthenia gravis • 3. Optic neuritis • • Mefloquine • • Classification: • • 1. Antimalarial (4-quinolinemethanol) • • Mechanism of Action: • • 1. Interferes with heme detoxification in Plasmodium parasites • 2. Inhibits β-hematin formation • • Indications: • • 1. Malaria prophylaxis and treatment • 2. Chemoprophylaxis for travelers • • Pharmacokinetics: • • 1. Oral bioavailability: 85-90% • 2. Peak plasma concentration: 6-12 hours • 3. Half-life: 20-30 days • 4. Metabolism: Hepatic (CYP3A4) • • Adverse Effects: • • 1. Neuropsychiatric (anxiety, depression, psychosis) • 2. Gastrointestinal (nausea, vomiting) • 3. Cardiovascular (QT prolongation) • 4. Skin reactions • • Contraindications: • • 1. Hypersensitivity to mefloquine or related compounds • 2. History of seizures or epilepsy • 3. Severe psychiatric disorders • #Quinine #Mefloquine

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