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Quinine sulfate
Quinine sulfate (Formula Q, Legatrim)
Quinine sulfate
(KWYE-nine)
Pregnancy Category: X Formula Q Legatrim M-KYA Quinamm (Rx)

Classification: Antimalarial

Action/Kinetics: Natural alkaloid having antimalarial, antipyretic, analgesic, and oxytocic properties. Use in treating malaria is important due to emergence of resistant forms of vivax and falciparum; no resistant forms of the parasite have been found for quinine. Antimalarial mechanism not known precisely; quinine does affect DNA replication and may raise intracellular pH. Eradicates the erythrocytic stages of plasmodia. Increases the refractory period of skeletal muscle, decreases the excitability of the motor end-plate region, and affects the distribution of calcium within the muscle fiber, thus making it useful for nocturnal leg cramps. Is oxytocic and may cause congenital malformations. Rapidly and completely absorbed from the upper small intestine; widely distributed in body tissues. Peak plasma levels: 1-3 hr; plasma levels following chronic use: 7 mcg/mL. t1/2: 4-5 hr. Highly bound to protein (70%-85%); about 5% excreted unchanged in urine. Small amounts found in saliva, bile, feces, and gastric juice. Acidifying the urine increases the rate of excretion.
Pharmacokinetics of quinine are affected by malaria, with a decrease in volume of distribution and systemic clearance. Protein binding, which is normally 70% to 85%, increases to more than 90% in clients with cerebral malaria, in pregnancy, and in children.

Uses: Alone or in combination with pyrimethamine and a sulfonamide or a tetracycline for resistant forms of Plasmodium falciparum. As alternative therapy for chloroquine, sensitive stains of P. falciparum, P. malariae, P. ovale and P. vivax. Mefloquine and clindamycin may also be used with quinine, depending on where the malaria was acquired. Investigational: Prevention and treatment of nocturnal recumbency leg cramps.

Contraindications: Use with tinnitus, G6PD deficiency, optic neuritis, history of blackwater fever, and thrombocytopenia purpura associated with previous use of quinine.

Special Concerns: Use with caution in clients with cardiac arrhythmias and during lactation. Hemolysis, with a potential for hemolytic anemia, may occur in clients with G6PD deficiency.

Side Effects: Use of quinine may result in a syndrome referred to as cinchonism. Mild cinchonism is characterized by tinnitus, headache, nausea, slight visual disturbances. Larger doses, however, may cause severe CNS, CV, GI, or dermatologic effects.
Allergic: Flushing, cutaneous rashes (papular, scarlatinal, urticarial), fever, facial edema, pruritus, dyspnea, tinnitus, sweating, asthmatic symptoms, visual impairment, gastric upset. GI: N&V;, epigastric pain, hepatitis. Ophthalmologic: Blurred vision with scotomata, photophobia, diplopia, night blindness, decreased visual fields, impaired color vision and perception, amblyopia, mydriasis, optic atrophy. CNS: Headache, confusion, restlessness, vertigo, syncope, fever, apprehension, excitement, delirium, hypothermia, dizziness, convulsions. Otic: Tinnitus, deafness. Hematologic: Acute hemolysis, hemolytic anemia, thrombocytopenic purpura, agranulocytosis, hypoprothrombinemia. CV: Symptoms of angina, ventricular tachycardia, conduction disturbances, vasculitis. Miscellaneous: Sweating, hypoglycemia, lichenoid photosensitivity.

Overdose Management: Symptoms: Dizziness, intestinal cramping, skin rash, tinnitus. With higher doses, symptoms include apprehension, confusion, fever, headache, vomiting, and seizures. Treatment: Induce vomiting or undertake gastric lavage. Maintain BP and renal function. If necessary, provide artificial respiration. Sedatives, oxygen, and other supportive measures may be required. Give IV fluids to maintain fluid and electrolyte balance. Treat angioedema or asthma with epinephrine, corticosteroids, and antihistamines. Urinary acidification will hasten excretion; however, in the presence of hemoglobinuria, acidification of the urine will increase renal blockade.

Drug Interactions: Acetazolamide / Blood levels with potential for quinine toxicity R/T rate of elimination Aluminum-containing antacids / Or delayed quinine absorption Anticoagulants, oral / Additive hypoprothrombinemia R/T synthesis of vitamin K-dependent clotting factors Cimetidine / Quinine effect R/T rate of excretion Digoxin / Digoxin serum levels Heparin / Heparin effect Mefloquine / Risk of ECG abnormalities or cardiac arrest; also, risk of convulsions.Do not use together; delay mefloquine administration at least 12 hr after the last dose of quinine. Neuromuscular blocking agents (depolarizing and nondepolarizing) / Respiratory depression and apnea Rifabutin, Rifampin / Hepatic clearance of quinine; can persist for several days following discontinuation of the rifampin Sodium bicarbonate / Quinine blood levels with potential for quinine toxicity R/T elimination rate

How Supplied: Capsule: 180 mg, 200 mg, 324 mg, 325 mg; Tablet: 260 mg

Dosage
•Capsules, Tablets Chloroquine-resistant malaria.
Adults: 650 mg q 8 hr for at least 3 days (7 days in Southeast Asia) along with pyrimethamine, 25 mg b.i.d. for the first 3 days and sulfadiazine, 2 g/day for the first 5 days. There are two alternative regimens: (1) quinine, 650 mg q 8 hr for at least 3 days (7 days in Southeast Asia) along with a tetracycline, 250 mg q 6 hr for 10 days or (2) quinine, 650 mg q 8 hr for 3 days with sulfadoxine, 1.5 g and pyrimethamine, 75 mg as a single dose.
Chloroquine-sensitive malaria.
Adults: 600 mg q 8 hr for 5-7 days. Pediatric: 10 mg/kg q 8 hr for 5-7 days.
Nocturnal leg cramps.
Adults: 260-300 mg at bedtime.