Nizatidine Information
Nizatidine ()
Nizatidine () Description
Nizatidine () USP is a histamine H2-receptor antagonist. Chemically, it is -[2-[[[2-[(dimethylamino)methyl]-4-thiazolyl]methyl]thio]ethyl]--methyl-2-nitro-1,1-ethenediamine.
The structural formula is as follows:
Nizatidine () has the molecular formula CHNOS representing a molecular weight of 331.46. It is an off-white to buff crystalline solid that is soluble in water. Nizatidine () has a bitter taste and mild sulfur-like odor.
Each capsule for oral administration contains Nizatidine () 150 mg (0.45 mmol) or 300 mg (0.91 mmol), pregelatinized starch, povidone, corn starch, talc, croscarmellose sodium, dimethicone, gelatin, titanium dioxide, pharmaceutical glaze (modified), synthetic black iron oxide, propylene glycol, FD&C blue #2 aluminum lake, FD&C red #40 aluminum lake, FD&C blue #1 aluminum lake, and D&C yellow #10 aluminum lake. The 150 mg capsule also contains yellow iron oxide, and the 300 mg capsule also contains D&C red #28, FD&C blue #1, and FD&C yellow #6.
Nizatidine () Clinical Pharmacology
Nizatidine () is a competitive, reversible inhibitor of histamine at the histamine H2-receptors, particularly those in the gastric parietal cells.
Nizatidine () Indications And Usage
Nizatidine () is indicated for up to 8 weeks for the treatment of active duodenal ulcer. In most patients, the ulcer will heal within 4 weeks.
Nizatidine () is indicated for maintenance therapy for duodenal ulcer patients, at a reduced dosage of 150 mg h.s. after healing of an active duodenal ulcer. The consequences of continuous therapy with Nizatidine () for longer than 1 year are not known.
Nizatidine () is indicated for up to 12 weeks for the treatment of endoscopically diagnosed esophagitis, including erosive and ulcerative esophagitis, and associated heartburn due to GERD.
Nizatidine () is indicated for up to 8 weeks for the treatment of active benign gastric ulcer. Before initiating therapy, care should be taken to exclude the possibility of malignant gastric ulceration.
Nizatidine () Contraindications
Nizatidine () is contraindicated in patients with known hypersensitivity to the drug. Because cross sensitivity in this class of compounds has been observed, H2-receptor antagonists, including Nizatidine () , should not be administered to patients with a history of hypersensitivity to other H2-receptor antagonists.
Nizatidine () Precautions
Symptomatic response to Nizatidine () therapy does not preclude the presence of gastric malignancy.
Because Nizatidine () is excreted primarily by the kidney, dosage should be reduced in patients with moderate to severe renal insufficiency (see ).
Pharmacokinetic studies in patients with hepatorenal syndrome have not been done. Part of the dose of Nizatidine () is metabolized in the liver. In patients with normal renal function and uncomplicated hepatic dysfunction, the disposition of Nizatidine () is similar to that in normal subjects.
A 2-year oral carcinogenicity study in rats with doses as high as 500 mg/kg/day (about 13 times the recommended human dose based on body surface area) showed no evidence of a carcinogenic effect. There was a dose-related increase in the density of enterochromaffin-like (ECL) cells in the gastric oxyntic mucosa. In a 2-year study in mice, there was no evidence of a carcinogenic effect in male mice; although hyperplastic nodules of the liver were increased in the high-dose males as compared with placebo. Female mice given the high dose of Nizatidine () (2,000 mg/kg/day, about 27 times the recommended human dose based on body surface area) showed marginally statistically significant increases in hepatic carcinoma and hepatic nodular hyperplasia with no numerical increase seen in any of the other dose groups. The rate of hepatic carcinoma in the high-dose animals was within the historical control limits seen for the strain of mice used. The female mice were given a dose larger than the maximum tolerated dose, as indicated by excessive (30%) weight decrement as compared with concurrent controls and evidence of mild liver injury (transaminase elevations). The occurrence of a marginal finding at high dose only in animals given an excessive and somewhat hepatotoxic dose, with no evidence of a carcinogenic effect in rats, male mice, and female mice (given up to 360 mg/kg/day, about 5 times the recommended human dose based on body surface aea), and a negative mutagenicity battery are not considered evidence of a carcinogenic potential for Nizatidine () .
Nizatidine () was not mutagenic in a battery of tests performed to evaluate its potential genetic toxicity, including bacterial mutation tests, unscheduled DNA synthesis, sister chromatid exchange, mouse lymphoma assay, chromosome aberration tests, and a micronucleus test.
In a 2-generation, perinatal and postnatal fertility study in rats, doses of Nizatidine () up to 650 mg/kg/day (about 17.5 times the recommended human dose based on body surface area) produced no adverse effects on the reproductive performance of parental animals or their progeny.
Teratogenic Effects–Pregnancy Category B:
Of the 955 patients in clinical studies who were treated with Nizatidine () , 337 (35.3%) were 65 and older. No overall differences in safety or effectiveness were observed between these and younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function (see ).
Nizatidine () Adverse Reactions
Worldwide, controlled clinical trials of Nizatidine () included over 6,000 patients given Nizatidine () in studies of varying durations. Placebo-controlled trials in the United States and Canada included over 2,600 patients given Nizatidine () and over 1,700 given placebo. Among the adverse events in these placebo-controlled trials, anemia (0.2% vs 0%) and urticaria (0.5% vs 0.1%) were significantly more common in the Nizatidine () group.
Nizatidine () Overdosage
Overdoses of Nizatidine () have been reported rarely. The following is provided to serve as a guide should such an overdose be encountered.
To obtain up-to-date information about the treatment of overdose, a good resource is your certified Regional Poison Control Center. Telephone numbers of certified poison control centers are listed in the Physicians’ Desk Reference (PDR). In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in your patient.
If overdosage occurs, use of activated charcoal, emesis, or lavage should be considered along with clinical monitoring and supportive therapy. The ability of hemodialysis to remove Nizatidine () from the body has not been conclusively demonstrated; however, due to its large volume of distribution, Nizatidine () is not expected to be efficiently removed from the body by this method.
Nizatidine () Dosage And Administration
The dose for patients with renal dysfunction should be reduced as follows:
Some elderly patients may have creatinine clearances of less than 50 mL/min, and, based on pharmacokinetic data in patients with renal impairment, the dose for such patients should be reduced accordingly. The clinical effects of this dosage reduction in patients with renal failure have not been evaluated.
Nizatidine () How Supplied
Nizatidine () Capsules USP, 150 mg are available as white opaque body and yellow opaque cap, imprinted “ 150” on the body and cap in black ink. They are available in bottles of:
14 caps NDC 21695-375-14
28 caps NDC 21695-375-28
60 caps NDC 21695-375-60
Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature].
Sandoz, Inc.
Princeton, NJ 08540
Rev. 03/06
MF0150REV03/06
OS7855
MG #16856
Repackaged by:
Rebel Distributors Corp
Thousand Oaks, CA 91320
Nizatidine () Principal Display Panel
