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Pronunciation
(ni ZA ti deen)
Generic Available (U.S.)
Yes: Excludes tablet
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment and maintenance of duodenal ulcer; treatment of benign gastric ulcer; treatment of gastroesophageal reflux disease (GERD)
OTC labeling: Prevention of meal-induced heartburn, acid indigestion, and sour stomach
Use: Unlabeled/Investigational
Part of a multidrug regimen for H. pylori eradication to reduce the risk of duodenal ulcer recurrence
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events have not been observed in animal reproduction studies; therefore, the nizatidine is classified as pregnancy category B. Nizatidine crosses the placenta. An increased risk of congenital malformations or adverse events in the newborn has generally not been observed following maternal use of nizatidine during pregnancy. Histamine H2 antagonists have been evaluated for the treatment of gastroesophageal reflux disease (GERD), as well as gastric and duodenal ulcers during pregnancy. Although if needed, nizatidine is not the agent of choice. Histamine H2 antagonists may be used for aspiration prophylaxis prior to cesarean delivery.
Lactation
Enters breast milk/consider risk:benefit
Breast-Feeding Considerations
Following oral administration of nizatidine, 0.1% of the maternal dose is found in breast milk. The highest milk concentrations appear ~2 hours after a maternal dose. According to the manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into account the risk of exposure to the infant and the benefits of treatment to the mother.
Contraindications
Hypersensitivity to nizatidine or any component of the formulation; hypersensitivity to other H2 antagonists (cross-sensitivity has been observed)
Warnings/Precautions
Disease-related concerns:
• Gastric malignancy: Relief of symptoms does not preclude the presence of a gastric malignancy.
• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment recommended.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.
Special populations:
• Pediatrics: Use with caution in children <12 years of age.
Adverse Reactions
>10%: Central nervous system: Headache (16%)
1% to 10%:
Central nervous system: Anxiety, dizziness, fever (reported in children), insomnia, irritability (reported in children), somnolence, nervousness
Dermatologic: Pruritus, rash
Gastrointestinal: Abdominal pain, anorexia, constipation, diarrhea, dry mouth, flatulence, heartburn, nausea, vomiting
Respiratory: Reported in children: Cough, nasal congestion, nasopharyngitis
<1% (Limited to important or life-threatening): Alkaline phosphatase increased, ALT increased, anaphylaxis, anemia, AST increased, bronchospasm, confusion, eosinophilia, exfoliative dermatitis, gynecomastia, hepatitis, jaundice, laryngeal edema, serum-sickness like reactions, thrombocytopenia, thrombocytopenic purpura, vasculitis, ventricular tachycardia
Metabolism/Transport Effects
Inhibits 3A4 (weak)
Drug Interactions
Atazanavir: H2-Antagonists may decrease the absorption of Atazanavir. Management: Specific dose limitations and administration guidelines exist; consult full interaction monograph or atazanavir prescribing information. Risk D: Consider therapy modification
Cefditoren: H2-Antagonists may decrease the serum concentration of Cefditoren. Management: Concomitant use of cefditoren with H2-antagonists and antacids is not recommended. Consider alternative methods to control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of H2-antagonists can not be avoided. Risk D: Consider therapy modification
Cefpodoxime: H2-Antagonists may decrease the absorption of Cefpodoxime. Separate oral doses by at least 2 hours. Risk C: Monitor therapy
Cefuroxime: H2-Antagonists may decrease the absorption of Cefuroxime. Separate oral doses by at least 2 hours. Risk C: Monitor therapy
Dasatinib: H2-Antagonists may decrease the absorption of Dasatinib. Risk D: Consider therapy modification
Delavirdine: H2-Antagonists may decrease the serum concentration of Delavirdine. Management: Chronic therapy with H2-antagonists should be avoided in patients who are being treated with delavirdine. The clinical significance of short-term H2-antagonist therapy with delavirdine is uncertain, but such therapy should be undertaken with caution. Risk X: Avoid combination
Dexmethylphenidate: H2-Antagonists may increase the absorption of Dexmethylphenidate. Specifically, H2-antagonists may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption. Risk C: Monitor therapy
Erlotinib: H2-Antagonists may decrease the serum concentration of Erlotinib. Risk X: Avoid combination
Fosamprenavir: H2-Antagonists may decrease the serum concentration of Fosamprenavir. Cimetidine may also inhibit the metabolism of the active metabolite amprenavir, making its effects on fosamprenavir/amprenavir concentrations difficult to predict. Risk C: Monitor therapy
Gefitinib: H2-Antagonists may decrease the serum concentration of Gefitinib. Risk C: Monitor therapy
Indinavir: H2-Antagonists may decrease the serum concentration of Indinavir. Risk C: Monitor therapy
Iron Salts: H2-Antagonists may decrease the absorption of Iron Salts. Exceptions: Ferric Gluconate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Risk C: Monitor therapy
Itraconazole: H2-Antagonists may decrease the serum concentration of Itraconazole. Management: When this combination is used, the itraconazole should be administered with a cola beverage (8 ounces). Itraconazole oral suspension may be less sensitive to this interaction. Monitor patient response to itraconazole closely. Risk D: Consider therapy modification
Ketoconazole: H2-Antagonists may decrease the serum concentration of Ketoconazole. Management: Administer oral ketoconazole at least 2 hours prior to use of any H2-receptor antagonist. Monitor patients closely for signs of inadequate clinical response to ketoconazole. Risk D: Consider therapy modification
Ketoconazole (Systemic): H2-Antagonists may decrease the serum concentration of Ketoconazole (Systemic). Management: Administer oral ketoconazole at least 2 hours prior to use of any H2-receptor antagonist. Monitor patients closely for signs of inadequate clinical response to ketoconazole. Risk D: Consider therapy modification
Mesalamine: H2-Antagonists may diminish the therapeutic effect of Mesalamine. Histamine H2-Antagonist-mediated increases in gastrointestinal pH may cause the premature release of mesalamine from specific sustained-release mesalamine products. Management: Consider avoiding concurrent administration of high-dose histamine H2-receptor antagonists with sustained-release mesalamine products. Risk D: Consider therapy modification
Methylphenidate: H2-Antagonists may increase the absorption of Methylphenidate. Specifically, H2-antagonists may interfere with the normal release of drug from the extended-release capsules (Ritalin LA brand), which could result in both increased absorption (early) and decreased delayed absorption. Risk C: Monitor therapy
Nelfinavir: H2-Antagonists may decrease the serum concentration of Nelfinavir. Concentrations of the active M8 metabolite may also be reduced. Risk C: Monitor therapy
Posaconazole: H2-Antagonists may decrease the serum concentration of Posaconazole. Management: Avoid concurrent use whenever possible. Monitor patients closely for decreased antifungal effects if this combination is used. Consider using a noninteracting antifungal as appropriate. Risk D: Consider therapy modification
Saquinavir: H2-Antagonists may increase the serum concentration of Saquinavir. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may cause gastric mucosal irritation).
Food: Administration with apple juice may decrease absorption.
Mechanism of Action
Competitive inhibition of histamine at H2-receptors of the gastric parietal cells resulting in reduced gastric acid secretion, gastric volume and hydrogen ion concentration reduced. In healthy volunteers, nizatidine suppresses gastric acid secretion induced by pentagastrin infusion or food.
Pharmacodynamics/Kinetics
Distribution: Vd: 0.8-1.5 L/kg
Protein binding: 35% to α1-acid glycoprotein
Metabolism: Partially hepatic; forms metabolites
Bioavailability: >70%
Half-life elimination: 1-2 hours; prolonged with renal impairment
Time to peak, plasma: 0.5-3.0 hours
Excretion: Urine (90%; ~60% as unchanged drug); feces (<6%)
Dosage
Oral:
Children:
<12 years: GERD (unlabeled use): 10 mg/kg/day in divided doses given twice daily; may not be as effective in children <12 years
≥12 years:
GERD: Refer to adult dosing
Meal-induced heartburn, acid indigestion and sour stomach: Refer to adult dosing
Adults:
Duodenal ulcer:
Treatment of active ulcer: 300 mg at bedtime or 150 mg twice daily
Maintenance of healed ulcer: 150 mg/day at bedtime
Gastric ulcer: 150 mg twice daily or 300 mg at bedtime
GERD: 150 mg twice daily
Meal-induced heartburn, acid indigestion, and sour stomach: 75 mg tablet [OTC] twice daily, 30 to 60 minutes prior to consuming food or beverages
Helicobacter pylori eradication (unlabeled use): 150 mg twice daily; requires combination therapy
Dosing adjustment in renal impairment:
Active treatment:
Clcr 20-50 mL/minute: 150 mg/day
Clcr <20 mL/minute: 150 mg every other day
Maintenance treatment:
Clcr 20-50 mL/minute: 150 mg every other day
Clcr <20 mL/minute: 150 mg every 3 days
Test Interactions
False-positive urine protein using Multistix®, gastric acid secretion test, skin tests allergen extracts, serum creatinine and serum transaminase concentrations, urine protein test
Patient Education
May cause drowsiness. Report fever, sore throat, tarry stools, CNS changes, or muscle or joint pain.
Geriatric Considerations
H2 blockers are the preferred drugs for treating peptic ulcer disorder (PUD) in the elderly due to cost and ease of administration. These agents are no less or more effective than any other therapy. The preferred agents (due to side effects and drug interaction profile and pharmacokinetics) are ranitidine, famotidine, and nizatidine. Treatment for PUD in the elderly is recommended for 12 weeks since their lesions are larger, and therefore, take longer to heal. Always adjust dose based upon creatinine clearance.
Additional Information
Giving dose at 6 PM (rather than 10 PM) may better suppress nocturnal acid secretion
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause dizziness or drowsiness; may rarely cause insomnia
Mental Health: Effects on Psychiatric Treatment
May rarely cause agranulocytosis; use caution with clozapine and carbamazepine
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule, oral: 150 mg, 300 mg
Axid®: 150 mg [DSC]
Solution, oral: 15 mg/mL (473 mL)
Axid®: 15 mg/mL (480 mL) [bubblegum flavor]
Tablet, oral:
Axid® AR: 75 mg [DSC]
Pricing: U.S. (www.drugstore.com)
Capsules (Axid)
150 mg (60): $172.98
300 mg (30): $169.98
Capsules (Nizatidine)
150 mg (60): $51.98
300 mg (30): $53.99
300 mg (30): $54.00
Solution (Axid)
15 mg/mL (480): $409.84
Solution (Nizatidine)
15 mg/mL (473): $272.00
Tablets (Axid AR)
75 mg (30): $25.99
Extemporaneously Prepared
A 2.5 mg/mL oral solution may be made with capsules and one of four different vehicles (lemon-lime Gatorade®, Ocean Spray® Cran-Grape® juice, apple juice, or V8® 100% vegetable juice). Empty the contents of one 300 mg capsule in a mortar. Add small portions of the chosen vehicle and mix to a uniform paste; mix while adding the vehicle in incremental proportions to almost 120 mL; transfer to a calibrated bottle, rinse mortar with vehicle, and add quantity of vehicle sufficient to make 120 mL. Label "shake well". Stable for 2 days refrigerated.
Nahata MC, Pai VB, and Hipple TF, Pediatric Drug Formulations, 5th ed, Cincinnati, OH: Harvey Whitney Books Co, 2004.
References
Abdel-Rahman SM, Johnson FK, Connor JD, et al, "Developmental Pharmacokinetics and Pharmacodynamics of Nizatidine," J Pediatr Gastroenterol Nut, 2004, 38(4):442-5.
Abdel-Rahman SM, Johnson FK, Gauthier-Dubois G, et al, "The Bioequivalence of Nizatidine (Axid) in Two Extemporaneously and One Commercially Prepared Oral Liquid Formulations Compared With Capsule," J Clin Pharmacol, 2003, 43(2):148-53.
Callaghan JT, Bergstrom RF, Rubin A, et al, “A Pharmacokinetic Profile of Nizatidine in Man,” Scand J Gastroenterol Suppl, 1987, 136:9-17.
Chey WD and Wong B, “American College of Gastroenterology Guideline on the Management of Helicobacter pylori Infection,” Am J Gastroenterol, 2007 102(8):1808-25.
Chey WD, Kochman ML, Traber PG, et al, “Possible Nizatidine-Induced Subfulminant Hepatic Failure,” J Clin Gastroenterol, 1995, 20(2):164-7.
Fennerty MD and Higbee M, “Drug Therapy of Gastrointestinal Disease,” Geriatric Pharmacology, Bressler R and Katz MD, eds, New York, NY: McGraw-Hill, 1993, 585-608.
Kahrilas PJ, Shaheen NJ, Vaezi MF, et al, “American Gastroenterological Association Medical Position Statement on the Management of Gastroesophageal Reflux Disease,” Gastroenterology, 2008, 135(4):1383-91.
Knadler MP, Bergstrom RF, Callaghan JT, et al, “Nizatidine, An H2-Blocker. Its Metabolism and Disposition in Man,” Drug Metab Dispos, 1986, 14(2):175-82.
Mikawa K, Nishina K, Maekawa N, et al, “Effects of Oral Nizatidine on Preoperative Gastric Fluid pH and Volume in Children,” Br J Anaesth, 1994, 73(5):600-4.
Rudolph CD, Mazur LJ, Liptak GS, et al, “Guidelines for Evaluation and Treatment of Gastroesophageal Reflux in Infants and Children: Recommendations of the North American Society for Pediatric Gastroenterology and Nutrition,” J Pediatr Gastroenterol Nutr, 2001, 32(Suppl 2):1-31.
Simeone D, Caria MC, Miele E, et al, “Treatment of Childhood Peptic Esophagitis: A Double-Blind Placebo-Controlled Trial of Nizatidine,” J Pediatr Gastroenterol Nutr, 1997, 25(1):51-5.
Sullivan TJ, Reese JH, Buchmann KA, et al, “Bioavailability Study of Nizatidine When Administered in Food,” Am J Ther, 1995, 2:275-8.
Vargas R, Ryan J, McMahon G, et al, “Pharmacokinetics and Pharmacodynamics of Oral Nizatidine,” J Clin Pharmacol, 1988, 28(1):71-5.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
Content last modified May 2011
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