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axid tablets |
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axid tablets Manufacturer: Reliant (nizatidine capsules, USP) DESCRIPTION The structural formula is as follows:
Nizatidine has the empirical formula C 12 H 21 N 5 O 2 S 2 representing a molecularweight of 331.47 axid tablets. It is an off-white to buff crystalline solid that is solublein water axid tablets. Nizatidine has a bitter taste and mild sulfur-like odor axid tablets. Each Pulvule®(capsule) contains for oral administration gelatin, pregelatinized starch, dimethicone,starch, titanium dioxide, yellow iron oxide, 150 mg (0.45 mmol) or 300 mg (0.91mmol) of nizatidine, and other inactive ingredients axid tablets. The 150-mg Pulvule alsocontains magnesium stearate, and the 300-mg Pulvule also contains croscarmellosesodium, povidone, red iron oxide, and talc axid tablets.
Antisecretory Activity-- 1 axid tablets. Effects on Acid Secretion: Axid significantly inhibitednocturnal gastric acid secretion for up to 12 hours axid tablets. Axid also significantlyinhibited gastric acid secretion stimulated by food, caffeine, betazole, andpentagastrin (Table 1) axid tablets. Table 1
Intrinsic Factor: Oral administration of 75 to 300 mg of Axid increased betazole-stimulatedsecretion of intrinsic factor axid tablets. Serum Gastrin: Axid had no effect on basal serum gastrin axid tablets. No rebound of gastrinsecretion was observed when food was ingested 12 hours after administrationof Axid axid tablets. 3 axid tablets. Other Pharmacologic Actions -- a axid tablets. Hormones: Axid was not shown to affect the serum concentrations of gonadotropins,prolactin, growth hormone, antidiuretic hormone, cortisol, triiodothyronine,thyroxin, testosterone, 5(alpha)-dihydrotestosterone, androstenedione, or estradiol axid tablets. b axid tablets. Axid had no demonstrable antiandrogenic action axid tablets. 4 axid tablets. Pharmacokinetics--The absolute oral bioavailability of nizatidine exceeds70% axid tablets. Peak plasma concentrations (700 to 1,800 µg/L for a 150-mg dose and1,400 to 3,600 µg/L for a 300-mg dose) occur from 0.5 to 3 hours followingthe dose axid tablets. A concentration of 1,000 µg/L is equivalent to 3 µmol/L;a dose of 300 mg is equivalent to 905 µmoles axid tablets. Plasma concentrations 12hours after administration are less than 10 µg/L axid tablets. The elimination half-lifeis 1 to 2 hours, plasma clearance is 40 to 60 L/h, and the volume of distributionis 0.8 to 1.5 L/kg axid tablets. Because of the short half-life and rapid clearance of nizatidine,accumulation of the drug would not be expected in individuals with normal renalfunction who take either 300 mg once daily at bedtime or 150 mg twice daily axid tablets. Axid exhibits dose proportionality over the recommended dose range axid tablets. The oral bioavailability of nizatidine is unaffected by concomitant ingestionof propantheline axid tablets. Antacids consisting of aluminum and magnesium hydroxides withsimethicone decrease the absorption of nizatidine by about 10% axid tablets. With food, theAUC and C max increase by approximately 10% axid tablets. In humans, less than 7% of an oral dose is metabolized as N2-monodes methylnizatidine,an H 2 -receptor antagonist, which is the principal metabolite excreted in theurine axid tablets. Other likely metabolites are the N2-oxide (less than 5% of the dose)and the S-oxide (less than 6% of the dose) axid tablets. More than 90% of an oral dose of nizatidine is excreted in the urine within12 hours axid tablets. About 60% of an oral dose is excreted as unchanged drug axid tablets. Renal clearanceis about 500 mL/min, which indicates excretion by active tubular secretion axid tablets. Less than 6% of an administered dose is eliminated in the feces axid tablets. Moderate to severe renal impairment significantly prolongs the half-life anddecreases the clearance of nizatidine axid tablets. In individuals who are functionally anephric,the half-life is 3.5 to 11 hours, and the plasma clearance is 7 to 14 L/h axid tablets. Toavoid accumulation of the drug in individuals with clinically significant renalimpairment, the amount and/or frequency of doses of Axid should be reduced inproportion to the severity of dysfunction ( see Dosage and Administration ) axid tablets. Approximately 35% of nizatidine is bound to plasma protein, mainly to (alpha)1 -acid glycoprotein axid tablets. Warfarin, diazepam, acetaminophen, propantheline, phenobarbital,and propranolol did not affect plasma protein binding of nizatidine in vitro axid tablets. 2 axid tablets. Maintenance of Healed Duodenal Ulcer: Treatment with a reduced dose of Axidhas been shown to be effective as maintenance therapy following healing of activeduodenal ulcers axid tablets. In multicenter, double-blind, placebo-controlled studies conductedin the United States, 150 mg of Axid taken at bedtime resulted in a significantlylower incidence of duodenal ulcer recurrence in patients treated for up to 1year (Table 3) axid tablets. Table 3
In patients with erosive or ulcerative esophagitis, 150 mg b.i.d axid tablets. of Axid givento 88 patients compared with placebo in 98 patients in Study 1 yielded a higherhealing rate at 3 weeks (16% vs 7%) and at 6 weeks (32% vs 16%, P <0.05) axid tablets. Of 99 patients on Axid and 94 patients on placebo, Study 2 at the same dosageyielded similar results at 6 weeks (21% vs 11%, P <0.05) and at 12 weeks(29% vs 13%, P <0.01) axid tablets. In addition, relief of associated heartburn was greater in patients treatedwith Axid axid tablets. Patients treated with Axid consumed fewer antacids than did patientstreated with placebo axid tablets. 4 axid tablets. Active Benign Gastric Ulcer: In a multicenter, double-blind, placebo-controlledstudy conducted in the United States and Canada, endoscopically diagnosed benigngastric ulcers healed significantly more rapidly following administration ofnizatidine than of placebo (Table 4) axid tablets. Table 4 Week Treatment Healing Rate vs axid tablets. Placebo
Axid is indicated for maintenance therapy for duodenal ulcer patients, at areduced dosage of 150 mg h.s axid tablets. after healing of an active duodenal ulcer axid tablets. Theconsequences of continuous therapy with Axid for longer than 1 year are notknown axid tablets. Axid is indicated for up to 12 weeks for the treatment of endoscopically diagnosedesophagitis, including erosive and ulcerative esophagitis, and associated heartburndue to GERD axid tablets. Axid is indicated for up to 8 weeks for the treatment of active benign gastriculcer axid tablets. Before initiating therapy, care should be taken to exclude the possibilityof malignant gastric ulceration axid tablets.
2 axid tablets. Because nizatidine is excreted primarily by the kidney, dosage should bereduced in patients with moderate to severe renal insufficiency ( see Dosageand Administration ) axid tablets. 3 axid tablets. Pharmacokinetic studies in patients with hepatorenal syndrome have not beendone axid tablets. Part of the dose of nizatidine is metabolized in the liver axid tablets. In patientswith normal renal function and uncomplicated hepatic dysfunction, the dispositionof nizatidine is similar to that in normal subjects axid tablets. Laboratory Tests-- False-positive tests for urobilinogen with Multistix®may occur during therapy with nizatidine axid tablets.
Carcinogenesis, Mutagenesis, Impairment of Fertility-- A 2-year oral carcinogenicitystudy in rats with doses as high as 500 mg/kg/day (about 80 times the recommendeddaily therapeutic dose) showed no evidence of a carcinogenic effect axid tablets. There wasa dose-related increase in the density of enterochromaffin-like (ECL) cellsin the gastric oxyntic mucosa axid tablets. In a 2-year study in mice, there was no evidenceof a carcinogenic effect in male mice; although hyperplastic nodules of theliver were increased in the high-dose males as compared with placebo axid tablets. Femalemice given the high dose of Axid (2,000 mg/kg/day, about 330 times the humandose) showed marginally statistically significant increases in hepatic carcinomaand hepatic nodular hyperplasia with no numerical increase seen in any of theother dose groups axid tablets. The rate of hepatic carcinoma in the high-dose animals waswithin the historical control limits seen for the strain of mice used axid tablets. The femalemice were given a dose larger than the maximum tolerated dose, as indicatedby excessive (30%) weight decrement as compared with concurrent controls andevidence of mild liver injury (transaminase elevations) axid tablets. The occurrence of amarginal finding at high dose only in animals given an excessive and somewhathepatotoxic dose, with no evidence of a carcinogenic effect in rats, male mice,and female mice (given up to 360 mg/kg/day, about 60 times the human dose),and a negative mutagenicity battery are not considered evidence of a carcinogenicpotential for Axid axid tablets. Axid was not mutagenic in a battery of tests performed to evaluate its potentialgenetic toxicity, including bacterial mutation tests, unscheduled DNA synthesis,sister chromatid exchange, the mouse lymphoma assay, chromosome aberration tests,and a micronucleus test axid tablets. In a 2-generation, perinatal and postnatal fertility study in rats, doses ofnizatidine up to 650 mg/kg/day produced no adverse effects on the reproductiveperformance of parental animals or their progeny axid tablets. Pregnancy--Teratogenic Effects--Pregnancy Category B --Oral reproduction studiesin pregnant rats at doses up to 1500 mg/kg/day (9000 mg/m 2 /day, 40.5 timesthe recommended human dose based on body surface area) and in pregnant rabbitsat doses up to 275 mg/kg/day (3245 mg/m 2 /day, 14.6 times the recommended humandose based on body surface area) have revealed no evidence of impaired fertilityor harm to the fetus due to nizatidine axid tablets. There are, however, no adequate andwell-controlled studies in pregnant women axid tablets. Because animal reproduction studiesare not always predictive of human response, this drug should be used duringpregnancy only if clearly needed axid tablets. Nursing Mothers-- Studies conducted in lactating women have shown that 0.1%of the administered oral dose of nizatidine is secreted in human milk in proportionto plasma concentrations axid tablets. Because of the growth depression in pups reared bylactating rats treated with nizatidine, a decision should be made whether todiscontinue nursing or discontinue the drug, taking into account the importanceof the drug to the mother axid tablets. Pediatric Use-- Safety and effectiveness in pediatric patients have not beenestablished axid tablets. Geriatric Use-- Of the 955 patients in clinical studies who were treated withnizatidine, 337 (35.3%) were 65 and older axid tablets. No overall differences in safetyor effectiveness were observed between these and younger subjects axid tablets. Other reportedclinical experience has not identified differences in responses between theelderly and younger patients, but greater sensitivity of some older individualscannot be ruled out axid tablets. This drug is known to be substantially excreted by the kidney, and the riskof toxic reactions to this drug may be greater in patients with impaired renalfunction axid tablets. 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 renalfunction ( see Dosage and Administration ) axid tablets. |
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