Yes

Antimalarial Agent

In conjunction with other antimalarial agents, suppression or treatment of chloroquine-resistant P. falciparum malaria; treatment of Babesia microti infection in conjunction with clindamycin; prevention and treatment of nocturnal recumbency leg muscle cramps

X

Tinnitus, optic neuritis, G-6-PD deficiency, hypersensitivity to quinine or any component, history of black water fever, and thrombocytopenia with quinine or quinidine

Use with caution in patients with cardiac arrhythmias (quinine has quinidine-like activity) and in patients with myasthenia gravis

Percentage unknown: Cinchonism (risk of cinchonism is directly related to dose and duration of therapy): Severe headache, nausea, vomiting, diarrhea, blurred vision, tinnitus

<1%: Flushing of the skin, anginal symptoms, fever, rash, pruritus, hypoglycemia, epigastric pain, hemolysis in G-6-PD deficiency, thrombocytopenia, hepatitis, nightblindness, diplopia, optic atrophy, impaired hearing, hypersensitivity reactions

Symptoms of mild toxicity include nausea, vomiting, and cinchonism; severe intoxication may cause ataxia, obtundation, convulsions, coma, and respiratory arrest; with massive intoxication quinidine-like cardiotoxicity (hypotension, QRS and Q-T interval prolongation, A-V block, and ventricular arrhythmias) may be fatal; retinal toxicity occurs 9-10 hours after ingestion (blurred vision, impaired color perception, constriction of visual fields and blindness); other toxic effects include hypokalemia, hypoglycemia, hemolysis and congenital malformations when taken during pregnancy.

Treatment includes symptomatic therapy with conventional agents (anticonvulsants, fluids, positioning, vasoconstrictors, antiarrhythmias). Note: Avoid type 1a and 1c antiarrhythmic drugs; treat cardiotoxicity with sodium bicarbonate; dialysis and hemoperfusion procedures are ineffective in enhancing elimination.

CYP3A3/4 enzyme substrate; CYP3A3/4 enzyme inhibitor

Increased toxicity:

To avoid risk of seizures and cardiac arrest, delay mefloquine dosing at least 12 hours after last dose of quinine

Beta-blockers + quinine may increase bradycardia

Quinine may enhance coumarin anticoagulants and potentiate nondepolarizing and depolarizing muscle relaxants

Quinine may inhibit metabolism of astemizole resulting in toxic levels and potentially life-threatening cardiotoxicity

Quinine may increase plasma concentration of digoxin by as much as twofold; closely monitor digoxin concentrations and decrease digoxin dose with initiation of quinine by 1/2

Verapamil, amiodarone, urinary alkalinizing agents, and cimetidine may increase quinine serum concentrations

Protect from light

Depresses oxygen uptake and carbohydrate metabolism; intercalates into DNA, disrupting the parasite's replication and transcription; affects calcium distribution within muscle fibers and decreases the excitability of the motor end-plate region; cardiovascular effects similar to quinidine

Absorption: Oral: Readily absorbed mainly from the upper small intestine

Protein binding: 70% to 95%

Metabolism: Primarily in the liver

Half-life: Children: 6-12 hours; Adults: 8-14 hours

Time to peak serum concentration: Within 1-3 hours

Elimination: In bile and saliva with <5% excreted unchanged in urine

Oral:

Treatment of chloroquine-resistant malaria: 25-30 mg/kg/day in divided doses every 8 hours for 5-7 days in conjunction with another agent

Babesiosis: 25 mg/kg/day divided every 8 hours for 7 days

Adults:

Treatment of chloroquine-resistant malaria: 260-650 mg every 8 hours for 6-12 days in conjunction with another agent

Suppression of malaria: 325 mg twice daily and continued for 6 weeks after exposure

Babesiosis: 650 mg every 6-8 hours for 7 days

Leg cramps: 200-300 mg at bedtime

Dosing interval/adjustment in renal impairment:

Cl_cr 10-50 mL/minute: Administer every 8-12 hours or 75% of normal dose

Cl_cr <10 mL/minute: Administer every 24 hours or 30% to 50% of normal dose

Dialysis: Not removed

Peritoneal dialysis: Dose as for Cl_cr <10 mL/min

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Dose for Cl_cr 10-50 mL/minute

May be administered with food

Toxic: >10 mg/mL

Positive Coombs' [direct]; false elevation of urinary steroids and catecholamines

None reported

Barbiturates and carbamazepine may decrease serum concentrations of quinine; CYP2D6 inhibitor; may interact with TCAs or beta-blockers; monitor

No information available to require special precautions

No effects or complications reported

Take on schedule as directed, with full 8 oz of water. Do not chew or crush sustained release tablets. You will need to return for follow-up blood tests. You may experience GI distress (taking medication with food, and frequent small meals may help). You may experience dizziness, changes in mentation, insomnia, headache, or visual disturbances (use caution when driving or engaging in tasks requiring alertness until response to drug is known). May discolor urine (black/brown/dark). Report persistent sore throat, fever, chills, flu-like signs, ringing in ears, vision disturbances, or unusual bruising or bleeding. Seek emergency help for palpitations or chest pain. Pregnancy precautions: Use reliable contraception during and for 2 months following treatment.

Do not crush tablets or capsule to avoid bitter taste

Monitor CBC with platelet count, liver function tests, blood glucose, ophthalmologic examination

Capsule, as sulfate: 200 mg, 260 mg, 325 mg

Tablet, as sulfate: 260 mg

Bateman DN, Blain PG, Woodhouse KW, et al, "Pharmacokinetics and Clinical Toxicity of Quinine Overdosage: Lack of Efficacy of Techniques Intended to Enhance Elimination," Q J Med, 1985, 54(214):125-31.

Boland ME, Roper SM, and Henry JA, "Complications of Quinine Poisoning," Lancet, 1985, 1(8425):384-5.

Dyson EH, Proudfoot AT, and Bateman DN, "Quinine Amblyopia: Is Current Management Appropriate?" J Toxicol Clin Toxicol, 1985-6, 23(7-8):571-8.

Jaeger A, Sauder P, Kopferschmitt J, et al, "Clinical Features and Management of Poisoning Due to Antimalarial Drugs," Med Toxicol Adverse Drug Exp, 1987, 2(4):242-73.

Lockey D and Bateman DN, "Effect of Oral Activated Charcoal on Quinine Elimination," Br J Clin Pharmacol, 1989, 27(1):92-4.

Panisko DM and Keystone JS, "Treatment of Malaria - 1990," Drugs, 1990, 39(2):160-89.

Schulbe DE, "Quinine Ban Signals Change for Pharmacists, APhA," Pharmacy Today, 1995, 1(12):6.

White NJ, "The Treatment of Malaria," N Engl J Med, 1996, 335(11):800-6.

Wyler DJ, "Malaria Chemoprophylaxis for the Traveler," N Engl J Med, 1993, 329(1):31-7.

Wyler DJ, "Malaria: Overview and Update," Clin Infect Dis, 1993, 16(4):449-56.