Quinine Sulfate

Trade Names:
Qualaquin
- Capsules 324 mg

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

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

Exposure is higher in patients with malaria than in healthy subjects. T _max in healthy subjects or patient with malaria is 2.8 h and 5.9 h, respectively. C _max in healthy subjects or patients with malaria is 3.2 and 8.4 mcg/mL, respectively.

Distribution

In healthy subjects, the Vd ranged from 2.5 to 7.1 L/kg. In patients with malaria, the Vd decreases in proportion to the severity of the infection. Protein binding ranges from 69% to 92% in healthy subjects and 78% to 95% in patients with malaria. Penetration into the CSF is relatively poor in patients with cerebral malaria, reaching approximately 2% to 7% of plasma concentrations. Concentrations in placental cord blood and breast milk are approximately 32% and 31%, respectively, of concentrations in maternal plasma. Less than 2 to 3 mg/day of quinine is secreted into breast milk.

Metabolism

Metabolism is almost exclusively via CYP pathways, primarily CYP3A4; other isozymes, including CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP2E1, are less influential in quinine metabolism.

Elimination

Elimination is primarily by hepatic biotransformation. Approximately 20% is excreted unchanged in the urine. Half-life is 4 to 5 h. Elimination is twice as rapid in an acid urine compared with an alkaline urine. In healthy subjects, the mean plasma Cl ranges from 0.08 to 0.47 L/h/kg, with a mean plasma elimination half-life of 9.7 to 12.5 h.

Special Populations

The effects of mild and moderate renal impairment on pharmacokinetics and efficacy of quinine are not known. Because the plasma half-life is prolonged from 26 h in patients with severe chronic renal impairment compared with 9.7 h in healthy controls, dosage adjustments are needed in patients with severe chronic renal failure. Negligible amounts are removed by hemodialysis or hemofiltration.

In patients with mild to moderate hepatic impairment, dosage adjustment is not needed; however, monitor patient for adverse reactions.

Mean AUC is approximately 38% higher in healthy subjects 65 to 78 yr of age compared with subjects 20 to 35 yr of age. Mean T _max and C _max are similar in elderly and younger subjects. Mean oral Cl is decreased and mean elimination half-life is increased in elderly compared with younger subjects. The proportion of quinine excreted unchanged in the urine is larger in elderly compared with younger patients. Despite these pharmacokinetic differences, no alteration in dosage is needed.

Pharmacokinetics are similar in children 1.5 to 12 yr of age compared with adults with uncomplicated malaria. Mean total Cl and Vd are reduced in children with malaria compared with healthy pediatric controls.

Indications and Usage

Treatment of uncomplicated Plasmodium falciparum malaria.

Unlabeled Uses

Prevention and treatment of nocturnal recumbency leg cramps.

Contraindications

Blackwater fever; pregnancy (except Qualaquin ); hypersensitivity to any component of the product; G-6-PD deficiency; history of thrombocytopenia; optic neuritis; tinnitus.

Prolonged QT interval; myasthenia gravis.

Dosage and Administration

PO 260 to 975 mg 3 times daily for 6 to 12 days.

648 mg every 8 h for 7 days. In patients with acute uncomplicated malaria and severe chronic renal failure, administer a 648 mg loading dose followed 12 h later by maintenance dosages of 324 mg every 12 h.

General Advice

• Administer with food to minimize GI upset.

Storage/Stability

Store at 59° to 86°F. Protect from moisture. Protect from light.

Store at 77° to 86°F.

Drug Interactions

Causes delayed or decreased quinine absorption.

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

Plasma concentrations of these drugs may be elevated, increasing the pharmacologic effects and risk of adverse reactions.

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

Plasma concentrations of these agents may be reduced, decreasing the efficacy.

Quinine may inhibit the metabolism of these substrates, increasing the pharmacologic effects and risk of adverse reactions.

May cause increased digoxin serum concentration.

Quinine metabolism may be inhibited, increasing the risk of adverse reactions.

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.

May potentiate neuromuscular blockade and may result in respiratory difficulties.

Quinine metabolism may be increased, reducing plasma concentrations and decreasing the efficacy.

Risk of life-threatening arrhythmias, including torsades de pointes, may be increased; coadministration of quinine is not recommended.

Quinine plasma concentrations may be elevated, increasing the risk of adverse reactions.

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

Angina, atrioventricular block, bradycardia, cardiac arrest, chest pain, disturbances in cardiac rhythm or conduction, hypotension, irregular rhythm, nodal escape beats, palpitations, postural hypotension, QT prolongation, syncope, tachycardia, torsades de pointes, unifocal premature ventricular contractions, U waves, vasodilation, ventricular tachycardia.

CNS

Acute dystonic reaction, aphasia, apprehension, ataxia, altered mental status, asthenia, coma, confusion, disorientation, dizziness, headache, restlessness, seizures, suicide, tremor, vertigo.

Dermatologic

Acrinal necrosis, allergic contact dermatitis, bullous dermatitis, cutaneous rash (including popular, scarlatinal, or urticarial rashes), cutaneous vasculitis, erythema multiforme, exfoliative dermatitis, facial edema, fixed drug eruption, photosensitivity reactions, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN), urticaria.

EENT

Blindness, burred vision, deafness, diminished visual fields, diplopia, disturbances in color perception, fixed papillary dilatation, hearing impairment, night blindness, optic neuritis, photophobia, sudden loss of vision, tinnitus, visual impairment (including blurred vision with scotomata).

GI

Abdominal pain, diarrhea, epigastric pain, esophagitis, gastric irritation, nausea, vomiting.

Genitourinary

Acute interstitial nephritis, hemoglobinuria, renal failure, renal impairment.

Hematologic-Lymphatic

Acute hemolysis, agranulocytosis, aplastic anemia, blackwater fever, coagulopathy, DIS, ecchymosis, hemolytic anemia, hemolytic uremic syndrome, hemorrhage, hypoprothrombinemia, idiopathic thrombocytopenic purpura, leukopenia, lupus anticoagulant, neutropenia, pancytopenia, petechiae, thrombocytopenia, thrombotic thrombocytopenic purpura.

Hepatic

Abnormal LFTs, granulomatous hepatitis, hepatitis, jaundice.

Hypersensitivity

Hypersensitivity reactions.

Metabolic-Nutritional

Anorexia; hypoglycemia.

Musculoskeletal

Myalgia, muscle weakness.

Respiratory

Asthma, dyspnea, pulmonary edema.

Miscellaneous

Chills, fever, flushing, lupus-like syndrome, sweating.

Precautions

Pregnancy

Category X .

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in children younger than 16 yr of age.

Elderly

Studies did not include sufficient numbers of subjects older than 65 yr of age to determine if they respond differently from younger subjects.

Hypersensitivity

Serious hypersensitivity reactions, including anaphylactic and anaphylactoid reactions, angioedema, Stevens-Johnson syndrome, and TEN, have been reported.

Renal Function

Adjust dose in patients with severe chronic renal failure. Effects of mild and moderate renal impairment are not known.

Hepatic Function

Use with caution.

Atrial fibrillation

Use with caution.

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 the same precautions as for quinidine.

Hemolysis

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

Hypoglycemia

Release of insulin from the pancreas may be stimulated, increasing the risk of hypoglycemia, especially in pregnant women.

Interrupted therapy

May predispose patients to serious complications of blackwater fever, including anemia, RBC destruction, and renal failure.

Myasthenia gravis

Muscle weakness may be exacerbated.

QT prolongation

Unpredictable, serious, and life-threatening hypersensitivity reactions may occur. Potentially fatal cardiac arrhythmias, including torsades de pointes and ventricular fibrillation. Avoid use in patients with known QT interval prolongation or conditions know to prolong the QT interval (eg, bradycardia, certain cardiac conditions, uncorrected hypokalemia).

Overdosage

Symptoms

Adult respiratory distress syndrome, cardiogenic shock, cardiotoxicity (including bundle branch block, increased QT interval, PR prolongation, sinus tachycardia, T-wave inversion, widening of the QRS complex), cinchonism (symptoms may include abdominal pain, blindness, blurred vision, cardiac arrhythmias, circulatory collapse, deafness, diarrhea, flushing, headache, hearing impairment, hypoglycemia, nausea, sweating, tinnitus, vertigo, vomiting), CNS toxicity (eg, ataxia, coma, convulsions, disturbed consciousness, drowsiness, respiratory depression), death, exacerbation of myocardial depression caused by decreased coronary perfusion, hypoglycemia, hypotension, pulmonary edema, ventricular arrhythmias (including AV block, bradycardia, idioventricular rhythm, torsades de pointes, ventricular fibrillation, ventricular tachycardia,), visual impairment (including blurred vision, effective color perception, visual field constriction and permanent blindness).

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.
• 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.
• Instruct patient that if a dose is missed, not to double the next dose. If it has been more than 4 h since the missed dose, advise the patient to wait and take the regular dose at the next scheduled time. Instruct patient to call health care provider if not sure what to do.

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