Nizatidine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Nizatidine competes with histamine for binding at the H2-receptors on the gastric basolateral membrane of parietal cells. Competitive inhibition results in reduction of basal and nocturnal gastric acid secretions. The drug also decreases the gastric acid response to stimuli such as food, caffeine, insulin, betazole, or pentagastrin.
Pharmacology
Nizatidine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Nizatidine is a competitive, reversible inhibitor of histamine at the histamine H2-receptors, particularly those in the gastric parietal cells. By inhibiting the action of histamine on stomach cells, nizatidine reduces stomach acid production. Nizatidine had no demonstrable antiandrogenic action. Full-dose therapy for the problems treated by nizatidine lasts no longer than 8 weeks. It has been demonstrated that treatment with a reduced dose of nizatidine is effective as maintenance therapy following healing of active duodenal ulcers.
Metabolism
Nizatidine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
Protein Binding
Nizatidine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 35%
Half-life
Nizatidine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1-2 hours
Absorption
Nizatidine¿¡ ´ëÇÑ Absorption Á¤º¸ Rapid (bioavailability of nizatidine exceeds 70%)
Biotransformation
Nizatidine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Less than 7% of an oral dose is metabolized as N2-monodes-methylnizatidine, an H2-receptor antagonist, which is the principal metabolite excreted in the urine. Other likely metabolites are the N2-oxide (less than 5% of the dose) and the S-oxide (less than 6% of the dose).
Toxicity
Nizatidine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, rat LD50: 301 mg/kg. Symptoms of overdose include cholinergic-type effects including lacrimation, salivation, emesis, miosis, and diarrhea.
Drug Interactions
Nizatidine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Atazanavir This gastric pH modifier decreases the levels/effects of atazanavirEnoxacin The agent decreases the absorption of enoxacinItraconazole The anti-H2 decreases the absorption of the imidazoleKetoconazole The anti-H2 decreases the absorption of the imidazole
Nizatidine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid excessive quantities of coffee or tea (Caffeine).No iron, zinc or fluoride within 2 hours of taking this medication.May take Vitamin D.Do not take Aluminum or magnesium antacids or supplements while on this medication.Take without regard to meals.
Nizatidine¿¡ ´ëÇÑ Description Á¤º¸ A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. [PubChem]
The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. NIZATIDINE [GGT Increase] [Composite Activity] (Score)I (Marginal) 1 (Active) 0