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A-Z Drug Facts > Quinine Sulfate

Quinine Sulfate

Pronouncation: (KWIE-nine SULL-fate)
Class: Cinchona alkaloid

Trade Names:
Quinine sulfate
- Capsules 200 mg
- Capsules 260 mg
- Capsules 325 mg
- Tablets 260 mg

Apo-Quinine (Canada)
Quinine-Odan (Canada)

Pharmacology

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Causes pH elevation in intracellular organelles of parasites; also has skeletal muscle relaxant effects and CV effects similar to those of quinidine.

Pharmacokinetics

Absorption

Complete and readily absorbed PO, mainly from upper small intestines. T max is 1 to 3 h (single dose). Bioavailability is about 80%.

Distribution

Protein binding is 70% to 85%, increases up to more than 90% in patients with cerebral malaria, pregnant women, and children. Crosses placenta and into fetal tissues and CSF. Vd is about 1.2 L/kg (cerebral malaria in adult patients), 1.7 L/kg (adult uncomplicated malaria), and 0.8 L/kg (children with uncomplicated malaria).

Metabolism

Metabolized in the liver. Metabolites have less activity than the parent drug.

Elimination

Occurs in the urine (less than 5% as unchanged), metabolites excreted in urine mainly as hydroxy derivatives, small amounts appear in feces, gastric juice, and bile. Urine excretion of drug is twice as fast as when urine is acidic.

Indications and Usage

Treatment of chloroquine-resistant falciparum malaria; alternative treatment for chloroquine-sensitive strains of P. falciparum , P. malariae , P. ovale , and P. uivae .

Unlabeled Uses

Prevention and treatment of nocturnal recumbency leg cramps.

Contraindications

G-6-PD deficiency; optic neuritis; tinnitus; history of blackwater fever and thrombocytopenic purpura associated with previous quinine ingestion; pregnancy.

Dosage and Administration

Chloroquine-resistant P. falciparum Malaria
Adults

PO 650 mg every 8 h for 5 to 7 days.

Children

PO 25 mg/kg/day in divided doses every 8 h for 5 to 7 days.

Chloroquine-Sensitive Malaria
Adults

PO 600 mg every 8 h for 5 to 7 days.

Children

PO 10 mg/kg every 8 h for 5 to 7 days.

Nocturnal Leg Cramps
Adults

PO 260 to 300 mg at bedtime.

Storage/Stability

Store in tight container at controlled room temperature (59° to 86°F).



Drug Interactions

Aluminum-containing antacids

Causes delayed or decreased quinine absorption.

Anticoagulants, oral

May cause depression of hepatic enzyme system that synthesizes vitamin K-dependent clotting factors and may enhance action of oral anticoagulants.

Cimetidine

May reduce quinine's Cl and prolong its half-life in body.

Digoxin

May cause increased digoxin serum concentration.

Mefloquine

May cause ECG abnormalities or cardiac arrest and may increase risk of convulsions. Do not use concurrently. Delay administration 12 h after last dose of quinine.

Neuromuscular blocking agents

May potentiate neuromuscular blockade and may result in respiratory difficulties.

Urinary alkalinizers

May increase quinine serum concentrations and potentiate toxicity.

Laboratory Test Interactions

Urinary 17-ketogenic steroids may have elevated values with Zimmerman method.

Adverse Reactions

Cardiovascular

Anginal symptoms.

CNS

Vertigo; dizziness; headache; fever; apprehension; restlessness; confusion; syncope; excitement; delirium; hypothermia; seizures.

EENT

Visual disturbances (eg, photophobia, blurred vision with scotomata, night blindness, amblyopia, diplopia, diminished visual fields, mydriasis, optic atrophy) tinnitus; deafness.

GI

Nausea; vomiting; diarrhea; epigastric pain.

Genitourinary

Renal tubular damage; anuria.

Hepatic

Hepatitis.

Hematologic

Acute hemolysis; hemolytic anemia; thrombocytopenic purpura; agranulocytosis; hypoprothrombinemia.

Miscellaneous

Cinchonism (headache, tinnitus, nausea, diarrhea, disturbed vision, skin, CV and CNS symptoms at very high doses); hypersensitivity (rash, pruritus, flushing, sweating, facial edema, asthmatic symptoms).

Precautions

Pregnancy

Category X .

Lactation

Excreted in breast milk.

Cardiac disease

Patients with cardiac arrhythmias may have exacerbation of symptoms with quinine, which acts similarly to quinidine. May cause cardiotoxicity. In patients with atrial fibrillation, quinine requires same precautions as for quinidine.

Hemolysis

Has been associated with G-6-PD deficiency. Discontinue immediately if hemolysis appears.

Overdosage

Symptoms

Tinnitus, dizziness, skin rash, GI disturbance, diarrhea, arrhythmias, convulsions, blurred vision, headache, nausea/vomiting, fever, confusion.

Patient Information

  • Caution patient that this medication must not be taken during pregnancy or when pregnancy is possible. Advise patient to use reliable form of birth control while taking this drug.
  • If medication is being used to treat malaria, advise patient to take medication around clock and to take full course of treatment even if feeling better.
  • Emphasize importance of medical follow-up when this course of therapy has been completed to ensure that therapy has been successful.
  • If medication is being used to treat nocturnal leg cramps, advise patient to take drug before bedtime.
  • Instruct patient to consult health care provider before combining any new medications with this drug.
  • Advise patient to take medication with or after meals or snack to minimize GI distress.
  • Instruct patient to report the following symptoms to the health care provider: flushing, itching, rash, fever, difficulty breathing, vision problems, ringing in ears, diarrhea, nausea/vomiting, vertigo.
  • Advise patient that drug may cause dizziness and vision problems, and to use caution while driving or performing other tasks requiring mental alertness.
  • Instruct patient not to take OTC medications (especially cold preparations) without consulting health care provider.



More Quinine Sulfate resources:

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