Quinine antimalarial drug

Pinworm is a helminHi infection that is universally common most oHier helminth infections are predomi-lianHy found in countries or areas of the world that lack proper sanitary facilities. Malaria is rare in the United States, but it is sometimes seen in individuals who have traveled to or lived in areas where this disease is a healtii problem. The first antimalarial drug, quinine, is derived from the bark of the cinchona tree. Amebiasis is seen Hiroughout the world, but it is less common in developed countries where sanitary facilities prevent Hie spread of the causative organism. 

Malaria is transmitted from person to person by a certain species of the Anopheles mosquito. The four different protozoans causing malaria are Plasmodium falciparum, P. malariae, P. ovale, and P. vivax. Drugp used to treat or prevent malaria are called anti malarial drags. Three antimalarial drugs are discussed in the chapter chloroquine, doxycycline, and quinine sulfate. Other examples of antimalarial drugs in use today are listed in the Summary Drug Table Antimalarial Drugs. 

Cinchona alkaloids have been used as drugs for the treatment of several diseases. Quinine is very popular as an antimalarial drug against the erythrocyte stage of the parasite [34]. Recently, Shibuya et al. (2003) reported the microbial transformation of four Cinchona alkaloids (quinine, quini-dine, cinchonidine, and cinchonine) by endophytic fungi isolated from Cin-... 

The next milestone in the development of organic synthesis was the preparation of the first synthetic dye, mauveine (aniline purple) by Perkin in 1856 Perkin, 1856, 1862). This is generally regarded as the first industrial organic synthesis. It is also a remarkable example of serendipity. Perkin s goal was the synthesis of the antimalarial drug quinine by oxidation of N-allyl toluidine (Fig. 2.4). 

The foundation of the synthetic dye industry is universally attributed to William Henry Perkin on account of his discovery in 1856 of a purple dye which he originally gave the name Aniline Purple, but which was later to become known as Mauveine. Perkin was a young enthusiastic British organic chemist who was carrying out research aimed not initially at synthetic dyes but rather at developing a synthetic route to quinine, the antimalarial drug. His objective in one particular set of experiments was... 

Initially approved in the 1930s as antimalarial drug, quinacrine (2) became one of the first potential substitutes to quinine. The total synthesis of quinacrine would be achieved in 1931 by German scientists at Bayer,and it would be subsequently marketed as Mepacrine or Atebrine. However, quinacrine would soon be replaced by another synthetic and more efficient antimalarial drug, chloroquine (3). 

The Cinchona tree remains the only economically practical source of quinine. Although the development of synthetic quinine is considered a milestone in organic chemistry, it has never been produced industrially as a substitute for naturally occurring quinine. Nevertheless, the implications of the total synthesis of quinine in new strategies for the development of safer and more efficient antimalarial drugs, as we will show in the course of the next paragraphs, is priceless. But, let us discuss this total synthesis first. 

Quinidine (6) and quinine (7) are diastereomeric quinoline alkaloids obtained from Cinchona spp. Quinidine (6) is included in many pharmacopeias for its antiarrhythmic effects.Quinine was the first antimalarial drug and served as an effective remedy for this deadly infectious disease in colonial times, making European settlement in many tropical and subtropical parts of the world possible.Owing to the development of resistance to synthetic antimalarials, quinine is still reverted to some extent for this... 

Antimalarial drugs are designed to prevent or treat malaria. Antimalarial drugs currently used for treatment for prophylaxis are mefloquine, primaquine, chloroquine, pyrimethamine, amodiaquin, quinine/quinidine, chloroguanide. 

In terms of its type of action, quinine is an antimalarial drug similar to chloroquine, although it is inferior in its activity. 

Zhao, X. J. and Ishizaki, T. (1997) Metabolic interactions of selected antimalar-ial and non-antimalarial drugs with the major pathway (3-hydroxylation) of quinine in human liver microsomes. Br. J. Clin. Pharmacol. 44, 505-511. 

Knowledge of local resistance patterns is important to determine the treatment regimen. There is increasing chloroquine and pyrimethamine-sulfado-xine (Fansidar) resistance in Africa and in some areas at the border of Thailand there is resistance for almost all antimalarial drugs including halofantrine, mefloquine and quinine. In these areas only the artemisinin derivatives (artemether, arteether, arte-sunate, dihydroartemisinin) are effective. 

Quinine Quinine, molecular formula C20H24N2O2, is a white crystalline quinoline alkaloid, isolated from Cinchona hark Cinchona succirubra), and is well known as an antimalarial drug. Quinine is extremely bitter, and also possesses antipyretic, analgesic and anti-inflammatory properties. While quinine is stiU the drug of choice for the treatment of Falciparum malaria, it can be also used to treat nocturnal leg cramps and arthritis. Quinine is an extremely basic compound, and is available in its salt forms, e.g. sulphate, hydrochloride and gluconate. 

Clinical Use. Mefloquine (Lariam) has emerged as one of the most important antimalarial agents.61 This drug is especially important in the prevention and treatment of malaria that is resistant to traditional antimalarial drugs such as chloroquine and quinine.50 Mefloquine is often the drug of choice for antimalarial prophylaxis, especially in areas of the world where chloroquine-resistant strains of malaria are common.23 Mefloquine can be used alone, but combining this... 

QUININE ANTIMALARIALS - MEFLOQUINE Risk of seizures Additive effect Warn patients of the risk patients should be advised to avoid driving while taking these drugs in combination... 

In view of the known basic antimalarial drugs (such as chloroquine, quinine) that are being used as salts for injection, it was proposed that introducing an amino group into the qinghaosu molecule may lead to water-soluble derivatives. Thus, five types of basic qinghaosu derivatives were synthesized (Structure... 

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