Antimalarial Drug Small Volume Parenteral Quinine Dihydrochloride Injection

Antimalarial Drug Small Volume Parenteral Quinine Dihydrochloride Injection

Product : Quinine Dihydrochloride Injection

Specification : 200mg/2ml; 400mg/4ml; 600mg/2ml

Standard : BP, USP

Packing : 10 x 10amps/box

Description :

An alkaloid derived from the bark of the cinchona tree. It is used as an antimalarial drug, and is the active ingredient in extracts of the cinchona that have been used for that purpose since before 1633. Quinine is also a mild antipyretic and analgesic and has been used in common cold preparations for that purpose. It was used commonly and as a bitter and flavoring agent, and is still useful for the treatment of babesiosis. Quinine is also useful in some muscular disorders, especially nocturnal leg cramps and myotonia congenita, because of its direct effects on muscle membrane and sodium channels. The mechanisms of its antimalarial effects are not well understood.

Indication:

For the treatment of malaria and leg cramps

Structured Indications:

Malaria caused by Plasmodium falciparum

Pharmacodynamics

Quinine is used parenterally to treat life-threatening infections caused by chloroquine-resistant Plasmodium falciparum malaria. Quinine acts as a blood schizonticide although it also has gametocytocidal activity against P. vivax and P. malariae. Because it is a weak base, it is concentrated in the food vacuoles of P. falciparum. It is thought to act by inhibiting heme polymerase, thereby allowing accumulation of its cytotoxic substrate, heme. As a schizonticidal drug, it is less effective and more toxic than chloroquine. However, it has a special place in the management of severe falciparum malaria in areas with known resistance to chloroquine.

Mechanism of action

The theorized mechanism of action for quinine and related anti-malarial drugs is that these drugs are toxic to the malaria parasite. Specifically, the drugs interfere with the parasite's ability to break down and digest hemoglobin. Consequently, the parasite starves and/or builds up toxic levels of partially degraded hemoglobin in itself.

Contraindications

G6PD deficiency, history of quinineinduced blackwater fever or thrombocytopenic purpura, hypersensitivity to quinine or its components, optic neuritis, pregnancy, tinnitus

Interactions

drugs

acetazolamide, sodium bicarbonate: Increased risk of quinine toxicity

aluminum-containing antacids: Possibly delayed or decreased quinine absorption

aminophylline, theophylline: Possibly increased quinine adverse effects

antimyasthenics: Possibly antagonized antimyasthenic effect on skeletal muscle

atorvastatin: Increased blood atorvastatin level; increased risk of myopathy or

rhabdomyolysis

carbamazepine, phenobarbital, phenytoin: Possibly increased blood level of these

drugs; possibly decreased blood quinine level

cimetidine: Possibly reduced quinine clearance

class 1A antiarrhythmics such as disopyramide, procainamide, quinidine and class III antiarrhythmics such as amiodarone, dofetilide, sotalo; CYP3A4 substrates such as astemizole, cisapride,halofantrine, pimozide, quinidine, terfenadine; macrolide antibiotics such as erythromycin; mefloquine: Increased risk of QT prolongation and life-threatening

arrythmias

debrisoquine, desipramine, dextromethorphan, flecainide, metoprolol, paroxetine: Possibly increased blood levels of these drugs; increased risk of adverse reactions digoxin: Increased blood digoxin level

erythromycin, ketoconazole, ritonavir, troleandomycin: Possibly increased blood quinine level

flecainide, quinidine: Increased risk of prolongation of QRS interval

hemolytics, neurotoxic drugs, ototoxic drugs: Increased risk of toxicity of these drugs

hepatic enzyme inducers, rifampin: Possibly decreased blood quinine level

mefloquine: Increased risk of seizures

neuromuscular blockers: Potentiated

neuromuscular blockade oral anticoagulants: Possibly increased anticoagulant effects and risk of bleeding

verapamil: Increased risk of prolonged PR interval

Adverse Reactions

CNS: Dizziness, headache

CV: Prolonged PR, QRS or QT intervals;

torsades de pointes; ventricular arrhythmias

EENT: Blurred vision, hearing loss,

tinnitus, vision changes including blindness

ENDO: Hypoglycemia

GI: Abdominal or epigastric pain, diarrhea,

nausea, vomiting

HEME: Thrombocytopenia

SKIN: Diaphoresis, flushing