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AXID

Pharmacological Classified : Antacids & Antiulcerants.

CONTENTS: Nizatidine.

PRESENTATION: Cap 150 mg x 20's. 300 mg x 10's.

DESCRIPTION: Nizatidine is N-[2-[[[2-[(dimethylamino)methyl]-4-thiazolyl]-methyl]thio]-ethyl]-N'-methyl-2-nitro- 1,1-ethenediamine. Nizatidine has the empirical formula of C12H21N5O2S2, representing a molecular weight of 331.45. It is an off-white to buff crystalline solid that is soluble in water. Nizatidine has a bitter taste and milds sulfur-like odor.

ACTIONS: Histamine H2-receptor antagonist.

Pharmacology: Nizatidine is a competitive, reversible inhibitor of histamine at the histamine H2-receptors particularly those in gastric parietal cells.

Antisecretory Activity:

1. Effects on Acid Secretion: Nizatidine significantly inhibited nocturnal gastric acid secretion for up to 12 hrs. Nizatidine also significantly inhibited gastric acid secretion stimulated by food, caffeine, betazole and pentagastrin (see Table 1).

 

Table 1. Effect of Oral Nizatidine on Gastric Acid Secretion
  Time After Dose, (hrs) % Inhibition of Gastric Acid Output by Dose, (mg)
20-50 75 100 150 300
Nocturnal Up to 10 57 -- 73 -- 90
Betazole Up to 3 -- 93 -- 100 99
Pentagastrin Up to 6 -- 25 -- 64 67
Meal Up to 4 41 64 -- 98 97
Caffeine Up to 3 -- 73 -- 85 96

 

2. Effects on Other Gastrointestinal Secretions: Pepsin: Oral administration of 75-300 mg of nizatidine did not affect pepsin activity in gastric secretions. Total pepsin output was reduced in proportion to the reduced volume of gastric secretions. Intrinsic Factor: Oral administration of 75-300 mg of nizatidine increased betazole-stimulated secretion of intrinsic factor. Serum Gastrin: Nizatidine had no effect on basal serum gastrin. No rebound of gastrin secretion was observed when food was ingested 12 hrs after administration of nizatidine.

 

3. Other Pharmacologic Actions:

a. Hormones: Nizatidine was not shown to affect the serum concentrations of gonadotropins, prolactin, growth hormone, antidiuretic hormone, cortisol, triiodothyronine, thyroxine, testosterone, 5α-dihydrotestosterone, androstenedione or estradiol. b. Nizatidine had no demonstrable, antiandrogenic action.

 

Table 2. Healing Response of Ulcers to Nizatidine.

 

Nizatidine

Placebo

 

300 mg at bedtime

150 mg 2 times a day

 

Number Entered

Healed/

Evaluable

Number Entered

Healed/

Evaluable

Number Entered

Healed/

Evaluable

Study 1

Week 2

Week 4

 

 

276

93/265 (35%)*

198/259 (76%)*

279

55/260 (21%)

94/243 (39%)

Study 2

Week 2

Week 4

108

24/103 (23%)*

65/97 (67%)*

106

27/101 (27%)*

66/97 (68%)*

101

9/93 (10%)

24/84 (29%)

Study 3

Week 2

Week 4

Week 8

92

22/90 (24%)+

52/85 (61%)*

68/83 (82%)*

 

 

98

13/93 (14%)

29/88 (33%)

39/79 (49%)

*P <0.01 as compared with placebo.

+P <0.05 as compared with placebo.

 

Pharmacokinetics: The absolute oral bioavailability of nizatidine exceeds 70%. Peak plasma concentrations (700-1800 mcg/L for a 150-mg dose and 1400-3600 mcg/L for a 300-mg dose) occur from 0.5-3 hrs following the dose. A concentration of 1000 mcg/L is equivalent to 3 Ámol/L; a dose of 300 mg is equivalent to 905 Ámoles. Plasma concentrations 12 hrs after administration are <10 mcg/L. The elimination half-life is 1-2 hrs, plasma clearance is 40-60 L/hr, and the volume of distribution is 0.8-1.5 L/kg. Because of the short half-life and rapid clearance of nizatidine, accumulation of the drug would not be expected in individuals with normal renal function who take either 300 mg once daily in the evening or 150 mg twice daily. Nizatidine exhibits dose proportionality over the recommended dose range.

 

The oral bioavailability of nizatidine is unaffected by concomitant ingestion of propantheline. Antacids consisting of aluminum and magnesium hydroxides with simethicone decrease the absorption of nizatidine by about 10%. With food the AUC and Cmax increase by approximately 10%. In humans, <7% of an oral dose is metabolized as N2-monodesmethylnizatidine, an H2-receptor antagonist, which is the principal metabolite excreted in the urine. Other likely metabolites are the N2-oxide (<5% of the dose) and the S-oxide (<6% of the dose). More than 90% of an oral dose of nizatidine is excreted in the urine within 12 hrs. About 60% of an oral dose is excreted as unchanged drug. Renal clearance is about 500 mL/min, which indicates excretion by active tubular secretion. Less than 6% of an administered dose is eliminated in the feces.

 

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