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
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 MalariaAdults
PO 650 mg every 8 h for 5 to 7 days.
ChildrenPO 25 mg/kg/day in divided doses every 8 h for 5 to 7 days.
Chloroquine-Sensitive MalariaAdults
PO 600 mg every 8 h for 5 to 7 days.
ChildrenPO 10 mg/kg every 8 h for 5 to 7 days.
Nocturnal Leg CrampsAdults
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 antacidsCauses delayed or decreased quinine absorption.
Anticoagulants, oralMay cause depression of hepatic enzyme system that synthesizes vitamin K-dependent clotting factors and may enhance action of oral anticoagulants.
CimetidineMay reduce quinine's Cl and prolong its half-life in body.
DigoxinMay cause increased digoxin serum concentration.
MefloquineMay 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 agentsMay potentiate neuromuscular blockade and may result in respiratory difficulties.
Urinary alkalinizersMay 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.
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