Quinine

Absorption

76 - 88%

Toxicity

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.

Description

Quinine, was the first known antimalarial. It is a 4-quinolinemethanol derivative bearing a substituted quinuclidine ring. The use of quinine in Europe began in the seventeenth century, after the Incas of Peru informed the Spanish Jesuits about the antimalarial properties of the bark of an evergreen mountain tree they called quinquina (later called cinchona, after Dona Franciscoa Henriquez de Ribera [1576–1639], Countess of Chinchon and wife of the Peruvian Viceroy).

Description

Quinine, is an extract from the bark of the cinchona tree that has been used for more than three hundred years as an anti-malarial.?Woodward—Doering/Rabe—Kindler total synthesis?of quinine ushered in the modern era of synthetic organic chemistry. The first stereoselective synthesis was reported in 2001.

The Uses of Quinine

Because of its relatively constant and well-known fluorescence quantum yield, quinine is also used in photochemistry as a common fluorescence standard. It has been used for imaging of oxygen evolution and oxide formation. Chloride and bromide have been sh

Background

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.

Indications

For the treatment of malaria and leg cramps

What are the applications of Application

Quinine is an antimalarial

Pharmacokinetics

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.

Metabolism

Hepatic, over 80% metabolized by the liver.