Antimalarial drug

Drugs to treat different stages in the life cycle of the malaria parasite are available. Treatment of malaria can be complex. Guidelines are produced by the Health Protection Agency (Malaria Reference laboratory) in the United Kingdom and by the World Health Organization. 

These dmgs treat the acute attack in the blood. They act on the form of plasmodium in the red blood cells. This group of antimalarial dmgs includes quinine and chloroquine. 

The mode of action of these two drugs is not fully understood. Chloroquine inhibits digestion of haemoglobin by the parasite (which it needs) and both dmgs inhibit the disposal of haem, which is toxic to the parasite. 

falciparum is resistant to chloroquine in most parts of the world. This appears to be due to decreased uptake and/or increased removal of the dmg from the parasite. Quinine is now the main dmg used against P. falciparum malaria. Chloroquine is still effective against other forms of malaria. 

Both drugs have similar side effects of nausea, vomiting, dizziness, blurring of vision and headache, although those of quinine can be more severe. 

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F. W. Wfeelogle, Survey of Antimalarial Drugs 1941-46. Edward Brothers, Ann Arbor, Michigan, 1946. 

Antimalarial drug artemisinine, sesquiterpenic 8-lactone with 1,2,5-trioxane (endoperoxide) fragment 98CSR273. 

Trioxane 210 has been used as a model system by Gu and coworkers to study the antimalarial drug artemisinin 211 (Scheme 137) [97CPL234, 99JST103]. It is the boat/twist form rather than the chair conformer of 210 that describes the subunit in 211. Moreover, geometric parameters and vibrational frequencies can only reliably be computed at the DFT level and by post-Hartree-Fock methods. B3-LYP/6-31G calculations on the conformers of 3,3,6,6-tetramethyl-1,2,4,5-tetroxane show that the chair conformer is stabilized with respect to the twisted conformer by about -2.8 kcal/mol [00JST85]. No corresponding boat conformer was found. 

Finally the aminoquinoline bearing a primary amine at the terminal carbon atom of the side chain is itself an effective antimalarial drug. Ring opening of 2-methyltetrahydrofuran by bromine gives the dibromide, 99. The primary halide is sufficiently less hindered so that reaction with potassium phthalimide affords exclusively the product of displacement of that halogen (100). Alkylation of the aminoquinoline with lOO affords the secondary amine, 101. Removal of the phthalimide group by means of hydrazine yields primaquine (102). ... 

Proguanil appears to have a dual activity. Part of it is metabolized to cycloguanil, which subsequently inhibits the protozaon dihydrofolate reduc-tase/thymidylate synthase (DHFR/TS) (Fig. 4). In addition, the native form, proguanil itself, exerts a potent antimalarial activity, especially in combination with other antimalarial drugs. The target of proguanil is unknown. 

The folate antagonists, pyrimethamine and sulfadiazine, inhibit the parasite s DHFR/TS synthase enzyme complex and the DHPS, respectively (Fig. 4) (see antimalarial drugs). To avoid deficiency of folic acid in patients treated with antifolate antagonists, folinic acid supplementation is recommended to reduce bone-marrow suppression. 

Favism is the haemolysis obseived after eating Vica fava. This reaction is observed in individuals with glucose-6-phosphate dehydrogenase deficiency. This common deficiency is also responsible for haemolysis in response to the antimalarial drug primaquine and others. 

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. 

When an antimalarial drug is given to a hospitalized patient for treatment of malaria, the preadministration assessment includes vital signs and a summary of the nature and duration of the symptoms. Laboratory tests may be ordered for the diagnosis of malaria Additional laboratory tests, such as a complete blood count, may be ordered to determine the patient s general health status. 

RISK RDRIM BALANCED NUTRITION, fttients receiving an antimalarial drug may experience nausea Good nutrition... 

When an antimalarial drug is used for prevention of malaria and taken once a week, die patient must take the drug on the same day each week. The program of prevention is usually started 1 week before departure to an area where malaria is prevalent. 

The differential diagnosis for PIH includes the following fixed drug eruption, systemic drug-induced hyperpigmentation, macular amyloid, ashy dermatosis, melasma, and tinea versicolor. Medications such as tetracyclines, antimalarial drugs, arsenic, bleomycin, and doxorubicin can result in hyperpigmentation of the skin. 

Various antimalarial drugs have been studied in biodegradable delivery systems. Wise (89) reported the use of a lactide/glycolide copolymer and also poly(L-lactic acid) for release of drugs such as quinazoline and sulfadiazine. Although in vitro data and experiments in mice were somewhat encouraging, these early formulations failed to reach significant clinical status. 

L. C., Sustained release of an antimalarial drug using a copolymer of glycolic/lactic acid. Life Sci.. 19, 867, 1976. 

Inhibitors of Folate Metabolism Provide Cancer Chemotherapy Antibacterial 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... 

The in vivo antitumor and trypanocidal effects of dimeric [Irn2(CH3COO)4(L)ra]° (L = classical organic antimalarial drugs, n= 1, 2) are reported.494 The dimeric complexes are characterized by IR spectroscopy. Further studies of monomeric Ir11 complexes, IrnL2, where L = alkyl or aryl dithiocarbamates and xanthates, reveal no clear relation between antitumor and antitrypanosomal actvities.495 Structure-activity data for the Ir11 complexes is presented. 

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