Antituberculous drugs

More recent investigations on the antimycobacterial activity of pamamycin-607 (lb) on 25 independent M. tuberculosis clinical isolates (either susceptible, mono-, or multiresistant to the first line antituberculous drugs) established minimum inhibitory concentrations MICjoo in the range of 1.5-2.0 pg/ml, while the MICjoo of lb for a bioluminescent laboratory strain of M. tuberculosis (H37Rv) was determined as 0.55 pg/ml [3a]. Parallel studies on the effect of lb on the cell cycle distribution of human (HL-60) cells by flow cytometry indicated no... 

Sulthiame (H7, 04), phcnacoraidc (H15), chloramphenicol (C5),dicou-marol (H6), antituberculous drugs (K23), disulfiram and phenyramidol (S23) have been described as inhibitors of phenytoin metabolism, while alcohol and possibly phenobarbitone have the reverse effect. Clinical and experimental evidence regarding the latter are confusing (B16, B29, C11,C12). 

This may be induced in the main by viral infection and by drugs, typically paracetamol (acetaminophen) overdose but occasionally dose independently by antidepressants and antituberculous drugs amongst others (Table 5). 

Direct hepatocellular injury, e.g. antituberculous drugs (e.g. rifampicin), erythromycin, high-dose penicillins (e.g. flucloxacillin), fluconazole and flucytosine Granulocytopaenia, e.g. high-dose penicillins/cephalosporins Immune thrombocytopaenia/Coombs positive anaemia, e.g. penicillins, cephalosporins... 

Rifampin, usually 600 mg/d (10 mg/kg/d) orally, must be administered with isoniazid or other antituberculous drugs to patients with active tuberculosis to prevent emergence of drug-resistant mycobacteria. In some short-course therapies, 600 mg of rifampin are given twice weekly. Rifampin 600 mg daily or twice weekly for 6 months also is effective in combination with other agents in some atypical mycobacterial infections and in leprosy. Rifampin, 600 mg daily for 4 months as a single drug, is an alternative to isoniazid prophylaxis for patients with latent tuberculosis only, who are unable to take isoniazid or who have had exposure to a case of active tuberculosis caused by an isoniazid-resistant, rifampin-susceptible strain. 

As with all antituberculous drugs, resistance to ethambutol emerges rapidly when the drug is used alone. Therefore, ethambutol is always given in combination with other antituberculous drugs. 

NMR and ultraviolet (UV) methods have been used to study the interesting adducts formed between the antituberculous drug isoniazid and cofactor NAD (nicotinamide adenine dinucleotide) <20050BC670>. Studies... 

Iproniazid 24, an alkyl analog of the antituberculous drug isoniazid 25 (Figure 2.8), surprisingly showed mood-improving activity in several depressed tuberculosis patients, which turned out to result from a monoamine oxidase (MAO) inhibitory activity. Since the compound was already registered as an antituberculosis drug and since it constituted the very first effective treatment of depression, more than 400 000 patients received it within only one year after the first announcement of its antidepressant activity [2, 33], Later it was withdrawn from therapy, due to hepatotoxic side effects. 

Britisch Medical Association and Royal Pharmaceutical Society of Great Britain. Antituberculous drugs. Br Natl Formulary 1998 35 160. 

Antituberculous drugs, Barbiturates, Carbamazepine, Cephalosporins, Erythromycin, Frusemide, Gold, Gentamicin, Isoniazid, Nitrofurantoin, Penicillins, Phenothiazines, Phenylbutazone, Phenytoin, Sul-phonamides. Thiazides. 

Aminosalicylate competitively antagonizes metabolism of para-aminobenzoic acid, resulting in bacteriostatic activity against Mycobacterium tuberculosis. Aminosalicylate is indicated in the treatment of tuberculosis (in combination with other antituberculous drugs) caused by susceptible strains of tubercle bacilli. 

Rifampin (600 mg once daily) is indicated in the treatment of all forms of tuberculosis in conjunction with at least one other antituberculous drug. Frequently used regimens include isoniazid and rifampin ethambutol and rifampin or isoniazid, ethambutol, and rifampin or isoniazid, pyrazi-namide, and rifampin. In addition, it is used in the treatment of asymptomatic carriers of Neisseria meningitis in order... 

D. Cycloserine Cycloserine is an antimetabolite that blocks the incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan. Because of its potential neurotoxicity (tremors, seizures, psychosis), cycloserine is only used to treat tuberculosis caused by organisms resistant to first-line antituberculous drugs. 

Hepatotoxicity can occur with several antituberculous drugs including ethionamide, isoniazid, pyrazinamide and rifampicin and high alcohol consumption/chronic alcoholism has been reported to increase the risk. However, one study in patients with active tuberculosis taking rifampicin and pyrazinamide, found that of the 14 patients who developed hepatotoxicity, only 5 of these reported alcohol use (not quantified), and alcohol was not found to be associated with an increased risk of hepatotoxicity. Similarly, another study found that alcohol consumption was not a risk factor for antimycobacterial-induced hepatotoxicity. ... 

O Reilly D, Ba an G, Hourihan B, Ivkicfarlane JT. Interaction between phenytoin and antituberculous drugs, Thorax( 9Z7) 42y 736. 

Peschke B, Ernst W, Gossmaim J, Kachel HG, Schoeppe W, Scheuermann EH. Antituberculous drugs in kidney transplant recipients treated with cyclosporine. Transplantation (1993)... 

Baker JT, Pioli E, Williams WJ (1974) In-vitro detection of hypersensitivity to antituberculous drugs. Lancet 11 967... 

Isoniazide, an antituberculous drug, was determined in alveolar macrophages by high-performance liquid chromatography (Guillaumont et al. 1982). 

The organization of this review is similar to that used in previous years with the exception that compounds having only in vitro activity are discussed with the corresponding class of closely related systemic agents, such as nitrofurans, sulfonamides and antituberculous drugs. This arrangement should allow for an insight into structure-activity relationships. 

As a consequence, several drugs have been developed by enhancing the side effect of another drug. For example, the mood-improving effect of iproniazid was discovered when it was tested as an antituberculous drug antidepressant inhibitors of neurotransmitter reuptake, like imipramine and desipramine, stem from the antipsychotic dopamine antagonist chlorpromazine, which itself was derived from Hi antihistaminics [35,36,51]. 

Makhlouf HA, Helmy A, Fawzy E, El-Attar M, Rashed HA. A prospective study of antituberculous drug-induced hep-atotoxicity in an area endemic for liver diseases. Hepatol Int 2008 2(3) 353-60. 

Oleszkifiwicz, Z. (1975) The effect of major antituberculous drugs used in the treatment of tuberculosis on recent memory. Gruzl. Chor. Pluc., 43, 383. 

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