Írta: jefanaenly - Dátum: 01-12-2012 20:44
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Isoniazid (brand names include: Laniazid / Nydrazid / Isokin / Isonex / Isoniazid / Isozid / Pycazide / Rimifon / Tibinil-I) belongs to a group of medicines known as antitubercular agents.
Isoniazid is used for the treatment and prevention of tuberculosis, including the treatment of latent tuberculosis infection (LTBI).
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Isoniazid is available in tablet, syrup, and injectable forms (given intramuscularly or intravenously). It is available worldwide, is inexpensive and is generally well tolerated. It is manufactured from isonicotinic acid, which is produced from 4-methylpyridine.[ [edit] As P450 is required for porphyrin synthesis, its deficiency leads to poor heme formation in early red blood cells, leading to sideroblastic anemia. (See also INDICATIONS): Isoniazid is recommended for all forms of tuberculosis in which organisms are susceptible. However, active tuberculosis must be treated with multiple concomitant anti-tuberculosis medications to prevent the emergence of drug resistance. Single-drug treatment of active tuberculosis with isoniazid, or any other medication, is inadequate therapy. Isoniazid reaches therapeutic concentrations in serum, cerebrospinal fluid, and within caseous granulomas. It is metabolized in the liver via acetylation. Two forms of the enzyme are responsible for acetylation, so some patients metabolize the drug more quickly than others. Hence, the half-life is bimodal, with peaks at one and three hours in the US population. The metabolites are excreted in the urine. Doses do not usually have to be adjusted in case of renal failure. If you experience any of the following serious side effects, stop taking isoniazid and seek emergency medical attention or contact your doctor immediately: Nervous System Reactions: Peripheral neuropathy is the most common toxic effect. It is dose-related, occurs most often in the malnourished and in those predisposed to neuritis (e.g., alcoholics and diabetics), and is usually preceded by paresthesias of the feet and hands. The incidence is higher in "slow inactivators".
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Metabolic And Endocrine Reactions: Pyridoxine deficiency, pellagra, hyperglycemia, metabolic acidosis, and gynecomastia. Ketoconazole: Potential interaction of Ketoconazole and Isoniazid may exist. When Ketoconazole is given in combination with isoniazid and rifampin the AUC of ketoconazole is decreased by as much as 88% after 5 months of concurrent Isoniazid and Rifampin therapy4. For following patient compliance: the Potts-Cozart test9, a simple colorimetric6 method of checking for isoniazid in the urine, is a useful tool for assuring patient compliance, which is essential for effective tuberculosis control. Additionally, isoniazid test strips are also available to check patient compliance Concomitant administration of pyridoxine (B6) is recommended in the malnourished and in those predisposed to neuropathy (e.g., alcoholics and diabetics) Gastrointestinal Reactions: Nausea, vomiting, and epigastric distress. numbness or tingling in your hands or feet;
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Isoniazid is available in tablet, syrup, and injectable forms (given intramuscularly or intravenously). It is available worldwide, is inexpensive and is generally well tolerated. It is manufactured from isonicotinic acid, which is produced from 4-methylpyridine.[ Metabolism Recent converters, as indicated by a tuberculin skin test ( ≥ 10 mm increase within a 2-year period for those < 35 years old; ≥ 1 5 mm increase for those ≥ 35 years of age). All infants and children younger than 4 years of age with a > 10 mm skin test are included in this category. Adults: 5 mg/kg up to 300 mg daily in a single dose; or 15 mg/kg up to 900 mg/day, two or three times/week The risk of hepatitis must be weighed against the risk of tuberculosis in positive tuberculin reactors over the age of 35. However, the use of isoniazid is recommended for those with the additional risk factors listed above (1-6) and on an individual basis in situations where there is likelihood of serious consequences to contacts who may become infected Isoniazid is odorless, and occurs as a colorless or white crystalline powder or as white crystals. It is freely soluble in water, sparingly soluble in alcohol, and slightly soluble in chloroform and in ether. Isoniazid is slowly affected by exposure to air and light. Mechanism of action
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DOSAGE AND ADMINISTRATION Isoniazid (Laniazid, Nydrazid), also known as isonicotinylhydrazine (INH), is an organic compound that is the first-line medication in prevention and treatment of tuberculosis. The compound was first synthesized in the early 20th century,[1] but its activity against tuberculosis was first reported in the early 1950s, and three pharmaceutical companies attempted unsuccessfully to simultaneously patent the drug[2] (the most prominent one being Roche, which launched its version, Rimifon, in 1952). With the introduction of isoniazid, a cure for tuberculosis was first considered reasonable. Isoniazid is bactericidal to rapidly dividing mycobacteria, but is bacteriostatic if the mycobacteria are slow-growing.[citation needed]
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Gastrointestinal Reactions: Nausea, vomiting, and epigastric distress. Isoniazid is odorless, and occurs as a colorless or white crystalline powder or as white crystals. It is freely soluble in water, sparingly soluble in alcohol, and slightly soluble in chloroform and in ether. Isoniazid is slowly affected by exposure to air and light. Phenytoin: Isoniazid may increase serum levels of phenytoin. To avoid phenytoin intoxication appropriate adjustment of the anticonvulsant should be made5,6. Metabolic And Endocrine Reactions: Pyridoxine deficiency, pellagra, hyperglycemia, metabolic acidosis, and gynecomastia. numbness or tingling in your hands or feet; Close contacts of persons with newly diagnosed infectious tuberculosis ( ≥ 5 mm). In addition, tuberculin-negative ( < 5 mm) children and adolescents who have been close contacts of infectious persons within the past 3 months are candidates for preventive therapy until a repeat tuberculin skin test is done 12 weeks after contact with the infectious source. If the repeat skin test is positive ( > 5 mm), therapy should be continued. yellow skin or eyes;