Jasoquin Tablet

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.

Quinine is an alkaloid used to treat uncomplicated Plasmodium falciparum malaria.

For the treatment of malaria and leg cramps

• Malaria caused by Plasmodium falciparum

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.

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.

76 - 88%

• 1.43 ± 0.18 L/kg [Healthy Pediatric Controls]
• 0.87 ± 0.12 L/kg [P. falciparum Malaria Pediatric Patients]
• 2.5 to 7.1 L/kg [healthy subjects who received a single oral 600 mg dose]

Approximately 70%

Quinine is eliminated primarily via hepatic biotransformation. Approximately 20% of quinine is excreted unchanged in urine.

Approximately 18 hours

• 0.17 L/h/kg [healthy]
• 0.09 L/h/kg [patients with uncomplicated malaria]
• 18.4 L/h [healthy adult subjects with administration of multiple-dose activated charcoal]
• 11.8 L/h [healthy adult subjects without administration of multiple-dose activated charcoal]
• Oral cl=0.06 L/h/kg [elderly subjects]

Quinine is a documented causative agent of drug induced thrombocytopenia (DIT). Thrombocytopenia is a low amount of platelets in the blood. Quinine induces production of antibodies against glycoprotein (GP) Ib-IX complex in the majority of cases of DIT, or more rarely, the platelet-glycoprotein complex GPIIb-IIIa. Increased antibodies against these complexes increases platelet clearance, leading to the observed thrombocytopenia.

• Take with food. Food reduces irritation.

• Oral: 600 mg (of quinine salt) every 8 hours for 7 days.
• Parenteral: lf the patient is seriously ill quinine should be given by intravenous infusion. The adult dosage regimen for quinine by infusion is loading dose of 20 mg/kg (up to maximum 1.4 g) of quinine salt infused over 4 hours then after 8-12 hours maintenance dose of 10 mg/kg (up to maximum 700 mg) of quinine salt infused over 4 hours every 8-12 hours (until patient can swallow tablets to complete the 7 days course).

• Oral: Quinine is well tolerated by children. The dosage regimen for quinine by mouth for children is 10 mg/kg (of quinine salt) every 8 hours for 7 days.
• Parenteral: The dosage regimen for quinine by intravenous infusion for children is calculated on a mg/kg basis as for adult.