Class: Histamine H 2 antagonist
- Solution, oral 15 mg/mL
- Tablets 75 mg
- Capsules 150 mg
- Capsules 300 mg
Reversibly and competitively blocks histamine at H 2 receptors, particularly those in gastric parietal cells, leading to inhibition of gastric acid secretion.
Absolute bioavailability is more than 70%, C max is 700 to 1,800 mcg/L (150 mg dose) and 1,400 to 3,600 mcg/L (300 mg dose), and T max is 0.5 to 3 h. Food increases nizatidine AUC and C max by approximately 10%.
Vd is 0.8 to 1.5 L/kg and the plasma protein binding is about 35%, mainly to alpha-1 acid glycoprotein.
Less than 7% of nizatidine is metabolized as N2-monodesmethylnizatidine (main metabolite). Other metabolites include N2-oxide (less than 5%) and S-oxide (less than 6%).
Eliminated in urine (90% excreted; 60% as unchanged) and feces (less than 6%). The t 1/ 2 is 1 to 2 h, plasma Cl is 40 to 60 L/h, and renal Cl is 500 mL/min.
Special PopulationsRenal Function Impairment
Moderate to severe renal function impairment prolongs nizatidine t 1/ 2 and decreases Cl. Reduce amount and frequency of dose according to severity.
Indications and Usage
Treatment and maintenance of duodenal ulcer, gastroesophageal reflux disease (GERD) (including erosive or ulcerative disease), and benign gastric ulcer; prevention of heartburn, acid indigestion, and sour stomach brought on by consuming food and beverages.
Prevention of olanzapine-induced weight gain; prevention of NSAID-induced gastroduodenal ulcer, in combination with amoxicillin and clarithromycin for Helicobacter pylori infection.
Hypersensitivity to H 2 antagonists.
Dosage and AdministrationDuodenal Ulcer (Active)
PO 300 mg at bedtime or 150 mg twice daily for up to 8 wk.Maintenance
PO 150 mg at bedtime.Benign Gastric Ulcer (Active)
PO 300 mg at bedtime or 150 mg twice daily.Moderate to Severe Renal Function Impairment
CrCl 20 to 50 mL/min: 150 mg daily; maintenance dose 150 mg every other day. CrCl less than 20 mL/min: 150 mg every other day; maintenance dose 150 mg every 3 days.GERD
PO 150 mg twice daily.Children 12 yr of age and older
PO (oral solution) 150 mg twice daily for up to 8 wk (max, 300 mg/day).Moderate to Severe Renal Function Impairment
CrCl 20 to 50 mL/min: 150 mg daily; maintenance dose 150 mg every other day. CrCl less than 20 mL/min: 150 mg every other day; maintenance dose 150 mg every 3 days.Acid Reduction
Adults and Children 12 yr of age and older
PO 75 mg with water before eating or up to 1 h before consuming food and beverages that may cause symptoms. Can be used up to twice daily.
Oral solution: Store at 59° to 86°F. Protect from light. Capsules and tablets: Store at 68° to 77°F. Protect from light.
Increased salicylate levels in patients taking very high doses of aspirin (3.9 g/day).Ethanol
Peak plasma ethanol levels may be increased.Ketoconazole
Effects of ketoconazole may be reduced.
Laboratory Test Interactions
False-positive tests for urobilinogen with Multistix may occur.
Headache (17%); dizziness (5%); asthenia, insomnia (3%); abnormal dreams, anxiety, somnolence (2%); nervousness (1%). Children: irritability, pyrexia (greater than 5%).
Pruritus, rash (2%).
Rhinitis (10%); pharyngitis (3%); amblyopia (1%). Children: nasal congestion, nasopharyngitis (greater than 5%).
Abdominal pain (8%); diarrhea (7%); dyspepsia, flatulence, nausea (5%); vomiting (4%); constipation (2%); anorexia, dry mouth, GI disorder, nausea and vomiting, tooth disorder (1%). Children: diarrhea, vomiting (greater than 5%).
Eosinophilia, thrombocytopenia, thrombocytopenic purpura.
Elevated liver enzymes.
Back pain, myalgia (2%).
Increased cough, sinusitis (2%). Children: cough (greater than 5%).
Pain (4%); chest pain, fever, infection (2%); accidental injury (1%); anaphylaxis, serum sickness–like reaction.
Category B .
Excreted in breast milk.
Safety and efficacy not established (capsules and tablets). Safety and efficacy not established in children younger than 12 yr of age (oral solution).
Decreased Cl may occur in patients with renal function impairment; reduced dosage may be needed.
Use drug with caution in patients with hepatic function impairment; decreased Cl may occur. In patients with uncomplicated hepatic function impairment, nizatidine disposition is generally normal.
Abnormalities appear to be reversible after discontinuation of drug.
- Advise patient to take medication after breakfast and at bedtime if prescribed twice-daily regimen or at bedtime if prescribed once-daily dosage.
- Caution patient to stay active and to increase fluid and roughage in diet to prevent constipation.
- Instruct patient to take missed dose as soon as possible, and caution not to double doses.
- Advise patient to avoid cigarette smoking, which increases gastric acid secretions and, therefore, decreases effectiveness of nizatidine therapy.
- Instruct patient to report the following symptoms to health care provider: abdominal pain, coffee-ground emesis, extreme fatigue, tarry stools, or weakness.
Copyright © 2009 Wolters Kluwer Health.