Short-term treatment of active benign gastric ulcer.
Maintenance of healing and reduction in recurrence of gastric ulcer.
Gastroesophageal Reflux (GERD)
Treatment of GERD to achieve acid suppression, control symptoms, and prevent complications.
Treatment of erosive esophagitis (endoscopically diagnosed) in patients with GERD.
Maintain healing and decrease recurrence of erosive esophagitis.
Self-medication as initial therapy for less severe symptomatic GERD†.
Short-term self-medication for treatment of heartburn (pyrosis) symptoms associated with acid indigestion and sour stomach in adults and adolescents ≥12 years of age.
Short-term self-medication for prevention of heartburn symptoms associated with acid indigestion and sour stomach brought on by ingestion of certain foods and beverages in adults and children ≥12 years of age.
Increasing Gastric pH in Neonates Undergoing Extracorporeal Membrane Oxygenation (ECMO)
May be useful for increasing gastric pH in neonates (<1 month of age) at risk for GI hemorrhage during ECMO†.
Dosage and Administration
Administration
Administered orally.
Administered by IM or slow IV injection, or by intermittent or continuous IV infusion in hospitalized patients with pathologic GI hypersecretory conditions or intractable duodenal ulcer, or when oral therapy is not feasible.
Administered by slow IV injection or intermittent IV infusion in children 1 month to 16 years of age for the treatment of duodenal ulcer.
Administered by slow IV injection or intermittent or continuous IV infusion to decrease gastric pH in neonates <1 month of age receiving ECMO.
Oral Administration
Administer antacids concomitantly as necessary for relief of pain.
Dissolve each dose to be administered as 150-mg effervescent tablets in 180–240 mL (6–8 ounces) of water as directed prior to ingestion. Effervescent tablets should not be chewed, swallowed whole, or dissolved on the tongue.
Dissolve each 25-mg effervescent tablet in ≥5 mL of water prior to administration. Allow tablet to completely dissolve before administering to the infant or child. May use a calibrated dropper or oral syringe to administer resultant solution in infants.
Administer tablets for self-medication with a glass of water.
IM Injection
May be administered undiluted.
Intermittent Direct IV Injection
Dilution
Dilute 50-mg dose to a concentration no greater than 2.5 mg/mL (i.e., total of 20 mL) with 0.9% sodium chloride injection or other compatible IV solution before direct IV injection.
Rate of Administration
Inject the 20-mL diluted solution (containing 50 mg/20 mL) at rate ≤4 mL/minute (i.e., over at least 5 minutes).
Intermittent IV Infusion
Dilution
Dilute 50-mg dose to a concentration ≤0.5 mg/mL (i.e., 100 mL total) in 5% dextrose injection or other compatible IV solution.
No additional dilution required for commercially available infusion solution (50 mg ranitidine in 50 mL of 0.45% sodium chloride).
Rate of Administration
Infuse 50 mg/100 mL dilution at ≤5–7 mL/minute (i.e., over 15–20 minutes).
Infuse commercially available infusion solution (50 mg in 50 mL of 0.45% sodium chloride) over 15–20 minutes.
Continuous IV Infusion
Dilution
Dilute 150 mg in 250 mL of 5% dextrose injection or other compatible IV solution.
Dilute to concentration ≤2.5 mg/mL in 5% dextrose injection or other compatible IV solution for Zollinger-Ellison syndrome or other pathologic GI hypersecretory conditions.
Rate of Administration
Infuse 150 mg/250 mL dilution at 6.25 mg/hour over 24 hours.
Infuse dilution for Zollinger-Ellison syndrome or other pathologic GI hypersecretory conditions at initial rate of 1 mg/kg per hour; adjust subsequent rate to individual requirements.
Children 1 month to 16 years of age: 2–4 mg/kg twice daily.
Maximum 300 mg daily.
IV
Children 1 month to 16 years of age: 2–4 mg/kg daily given as divided doses every 6–8 hours.
Maximum 50 mg every 6–8 hours.
Maintenance of Healing of Duodenal Ulcer
Oral
Children 1 month to 16 years of age: 2–4 mg/kg once daily.
Maximum 150 mg daily.
Gastric Ulcer
Treatment
Oral
Children 1 month to 16 years of age: 2–4 mg/kg twice daily.
Maximum 300 mg daily.
Maintenance of Healing of Gastric Ulcer
Oral
Children 1 month to 16 years of age: 2–4 mg/kg once daily.
Maximum 150 mg daily.
Gastroesophageal Reflux
Treatment of GERD
Oral
Children 1 month to 16 years of age: 5–10 mg/kg daily, usually administered as 2 equally divided doses.
Treatment of Erosive Esophagitis
Oral
Children 1 month to 16 years of age: 5–10 mg/kg daily, usually administered as 2 equally divided doses.
Self-medication for Heartburn
Oral
Children ≥12 years of age: 75 or 150 mg once or twice daily.
Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Self-medication for Prevention of Heartburn
Oral
Children ≥12 years of age: 75 or 150 mg once or twice daily; administer 30–60 minutes before ingestion of causative food or beverage.
Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Increase Gastric pH in Neonates Undergoing ECMO
IV
Neonates (<1 month of age) at risk for GI hemorrhage: Consider 2 mg/kg every 12–24 hours (or as continuous infusion).
A dose of 2 mg/kg usually is sufficient to increase gastric pH to >4 for at least 15 hours.
Adults
General Parenteral Dosage
Hospitalized Patients with Pathologic Hypersecretory Conditions or Intractable Duodenal Ulcer, or Short-term Use When Oral Therapy is not Feasible
IM
50 mg every 6–8 hours.
Increase dosage when necessary by administering 50 mg more frequently.
Maximum 400 mg daily.
Intermittent Direct IV Injection
50 mg every 6–8 hours.
Increase dosage when necessary by administering 50 mg more frequently.
Maximum 400 mg daily.
Intermittent IV Infusion
50 mg every 6–8 hours.
Increase dosage when necessary by administering 50 mg more frequently.
Maximum 400 mg daily.
Continuous IV Infusion
150 mg/24 hours (6.25 mg/hour). See Pathologic GI Hypersecretory Conditions under Dosage.
Duodenal Ulcer
Treatment of Active Duodenal Ulcer
Oral
Usual dosage: 150 mg twice daily.
Alternative: 300 mg daily after evening meal or at bedtime for optimum convenience and compliance.
100 mg twice daily reported to be as effective in healing ulcers as 150 mg twice daily.
Healing usually within 4 weeks; may occur in 2 weeks.
Additional 4 weeks of therapy may be beneficial.
Maintenance of Healing of Duodenal Ulcer
Oral
150 mg daily at bedtime.
Gastric Ulcer
Oral
150 mg twice daily.
Healing usually within 6 weeks.
Maintenance of Gastric Ulcer Healing
Oral
150 mg daily at bedtime.
Gastroesophageal Reflux
Treatment of GERD
Oral
150 mg twice daily.
Treatment of Erosive Esophagitis
Oral
150 mg 4 times daily.
Maintenance of Healing of Erosive Esophagitis
Oral
150 mg twice daily.
Self-medication for Heartburn
Oral
75 mg or 150 mg once or twice daily.
Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Self-medication for Prevention of Heartburn
Oral
75 or 150 mg once or twice daily; administer 30–60 minutes before ingestion of causative food or beverage.
Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Pathologic GI Hypersecretory Conditions
Oral
150 mg twice daily; may administer more frequently, if needed.
Adjust dosage according to patient response.
Dosages up to 6 g daily have been used for severe disease.
Continue as long as necessary.
Continuous IV Infusion
Initiate at 1 mg/kg per hour.
Titrate upward in 0.5 mg/kg per hour increments and redetermine gastric acid secretion if symptoms occur or gastric acid output is >10 mEq per hour after 4 hours.
Dosages up to 2.5 mg/kg per hour and infusion rates up to 220 mg/hour have been used.
Prescribing Limits
Pediatric Patients
Gastroesophageal Reflux
Self-medication for Heartburn
Oral
Adolescents ≥12 years of age: Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Self-medication for Prevention of Heartburn
Oral
Adolescents ≥12 years of age: Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Duodenal Ulcer
Treatment of Active Duodenal Ulcer
Oral
Children 1 month to 16 years of age: Maximum 300 mg daily.
IV
Children 1 month to 16 years of age: Maximum 50 mg every 6–8 hours.
Maintenance of Healing of Duodenal Ulcer:
Oral
Children 1 month to 16 years of age: Maximum 150 mg daily.
Gastric Ulcer
Treatment of Gastric Ulcer
Oral
Children 1 month to 16 years of age: Maximum 300 mg daily.
Maintenance of Healing of Gastric Ulcer
Oral
Children 1 month to 16 years of age: Maximum 150 mg daily.
Adults
General Parenteral Dosage
Hospitalized Patients with Pathologic Hypersecretory Conditions or Intractable Duodenal Ulcer, or Short-term Use When Oral Therapy is not Feasible
IM
Maximum 400 mg daily.
Maximum 50 mg per dose.
Intermittent Direct IV
Maximum 400 mg daily.
Maximum 50 mg per dose.
Maximum concentration 2.5 mg/mL (50 mg/20 mL).
Maximum injection rate: 4 mL/minute (i.e., over 5 minutes).
Intermittent IV Infusion
Maximum 400 mg daily.
Maximum 50 mg per dose.
Maximum concentration 0.5 mg/mL (50 mg/100 mL).
Maximum infusion rate: 5–7 mL/minute (100 mL over 15–20 minutes).
Commercially available infusion solution (50 mg in 50 mL of 0.45% sodium chloride): over 15–20 minutes.
Gastroesophageal Reflux
Self-Medication for Heartburn
Oral
Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Self-medication for Prevention of Heartburn
Oral
Maximum 150 mg (as 75-mg tablets) or 300 mg (as 150-mg tablets) in 24 hours; maximum 2 weeks of continuous use as self-medication.
Duodenal Ulcer
Treatment of Active Duodenal Ulcer
Oral
Safety and efficacy for >8 weeks have not been established.
Gastric Ulcer
Treatment of Active Benign Gastric Ulcer
Oral
Safety and efficacy for >6 weeks have not been established.
Pathologic GI Hypersecretory Conditions
Continuous IV Infusion
Zollinger-Ellison Syndrome: Maximum concentration 2.5 mg/mL.
Up to 2.5 mg/kg per hour or 220 mg/hour has been used.
Special Populations
Renal Impairment
Clcr <50 mL/minute
Oral
150 mg once every 24 hours. If necessary, may cautiously increase dosage frequency to every 12 hours or more frequently.
IM
50 mg every 18–24 hours. If necessary, may cautiously increase dosage frequency to every 12 hours or more frequently.
Intermittent Direct IV
50 mg every 18–24 hours. If necessary, may cautiously increase dosage frequency to every 12 hours or more frequently.
Intermittent IV Infusion
50 mg every 18–24 hours. If necessary, may cautiously increase dosage frequency to every 12 hours or more frequently.
Continuous IV Infusion
Not evaluated.
Hemodialysis
Decreases blood levels; administer at the end of hemodialysis.
Geriatric Patients
Careful dosage selection recommended because of possible age-related decrease in renal function. (See Geriatric Use under Cautions.)
Do not use for self-medication if swallowing is difficult.
Do not use for self-medication with other drugs that decrease gastric acid secretion.
Do not use for self-medication if difficulty or pain occurs when swallowing food, if experiencing vomiting with blood, or if passing bloody or blackened stools. Instead, consult a clinician since such manifestations may indicate presence of a serious condition requiring alternative treatment.
Warnings/Precautions
General Precautions
Gastric Malignancy
Response to ranitidine does not preclude presence of gastric malignancy.
Hepatic Effects
Discontinue immediately in patients with hepatitis. Occasional hepatotoxicity, rarely, hepatic failure and death have been reported.
Increased serum ALT concentrations have occurred with ≥5 days of histamine H2-receptor antagonist therapy at higher than recommended IV dosages. Monitor serum ALT from day 5 to end of therapy when ranitidine is administered IV at dosages ≥400 mg daily for ≥5 days.
Cardiovascular Effects
Rapid IV administration: associated rarely with bradycardia. Avoid rapid administration.
Acute Intermittent Porphyria
Ranitidine may precipitate acute porphyric attacks. Avoid use in such patients.
Respiratory Effects
Administration of H2-receptor antagonists has been associated with an increased risk for developing certain infections (e.g., community-acquired pneumonia).
Phenylketonuria
Zantac® EFFERdose® tablets for solution contain aspartame (NutraSweet®), which is metabolized in the GI tract to provide 2.81 or 16.84 mg of phenylalanine per 25- or 150-mg tablet, respectively.
Specific Populations
Pregnancy
Category B.
Self-medication in pregnant women: Consult clinician before using.
Lactation
Distributed into milk; use with caution.
Self-medication in nursing women: Consult clinician before using.
Pediatric Use
Oral: Safety and efficacy for erosive esophagitis healing maintenance or pathologic hypersecretory condition treatment not established in pediatric patients.
Oral: Safety and efficacy not established in neonates (< 1 month of age).
Oral: Safety and efficacy established in infants, children, and adolescents 1 month to 16 years of age for duodenal and gastric ulcer treatment and healing maintenance, GERD treatment, and erosive esophagitis treatment.
Parenteral: Safety and efficacy not established in pediatric patients for treatment of pathologic hypersecretory conditions.
Parenteral: Safety and efficacy established in infants, children, and adolescents 1 month to 16 years of age for duodenal ulcer treatment.
Parenteral (IV) use in neonates (< 1 month of age) receiving extracorporeal membrane oxygenation (ECMO): Limited data in neonates suggest that ranitidine may be safe and useful to increase gastric pH in infants at risk of GI hemorrhage.
Geriatric Use
No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.
Use with caution due to greater frequency of decreased renal function observed in the elderly.
Select dosage with caution; monitoring renal function may be useful.
Hepatic Impairment
Use with caution. (See Hepatic Effects under Cautions.)
Renal Impairment
Use with caution; dosage adjustment necessary based on degree of renal impairment. (See Renal Impairment under Dosage and Administration.)
Common Adverse Effects
Oral or parenteral therapy: Headache, sometimes severe.
IM therapy: Transient pain at injection site.
IV therapy: Transient local burning or itching.
Interactions
Binds weakly to hepatic CYP isoenzyme system in vitro.
Affinity for CYP isoenzyme system is about 10% that of cimetidine; inhibition of CYP isoenzyme system is 2.4 times less than cimetidine.
Does not inhibit CYP isoenzymes at recommended dosages.
May minimally inhibit hepatic metabolism of some drugs, or affect bioavailability by another mechanism (e.g., pH-dependent absorption, altered volume of distribution).
Dose-dependent inhibition of acetaminophen metabolism in vitro
Alcohol
Moderate alcohol consumption by individuals receiving concurrent ranitidine unlikely to result in clinically important alterations of blood alcohol concentration and/or alcohol metabolism
Controversy about psychomotor impairment potential; observe usual precautions about alcohol intake and hazardous tasks requiring mental alertness or physical coordination
Pharmacokinetic studies: up to 400 mg daily had no effect on warfarin clearance or PT
Pharmacokinetics
Absorption
Bioavailability
Rapidly absorbed after oral or IM administration.
Oral bioavailability: About 50%; similar in children 3.5–16 years of age.
Oral: Peak plasma concentration attained within 2–3 hours in adults and geriatric patients and within 1.6–2 hours in children 1 month to 16 years of age.
IM: about 90–100% absorption.
Commercially available oral solution, effervescent tablets, and conventional tablets are bioequivalent.
Duration
Following oral administration of a single 150-mg dose, substantial inhibition of gastric acid secretion reportedly continues for about 9.5 hours.
In pediatric patients, oral administration of 6–10 mg/kg daily (in 2 or 3 divided doses), maintained gastric pH throughout the dosing interval.
Following a single 150-mg oral dose, serum concentrations required to inhibit 50% of stimulated gastric acid secretion are maintained for up to 12 hours.
IM or IV: Following a 50-mg dose, serum concentrations required to inhibit 50% of stimulated gastric acid secretion are maintained for 6–8 hours.
Food
Food does not appear to substantially affect absorption or peak plasma concentrations.
Special Populations
Oral: In geriatric individuals, AUC may be substantially increased.
In individuals with cirrhosis, oral bioavailability appears to increase to about 70% and peak serum ranitidine concentrations appear to be higher because of reduced first-pass metabolism; considered minor, clinically unimportant.
Distribution
Extent
Widely distributed throughout body.
Distributed into CSF following oral administration; CSF concentrations in individuals with uninflamed meninges are about 3–5% of concurrent peak serum concentrations.
Distributed into human milk; milk concentrations appear to be 25–100% of concurrent serum concentrations.
Plasma Protein Binding
10–19%.
Special Populations
In individuals with cirrhosis, minor but clinically unimportant alterations in distribution occur following oral administration.
Elimination
Metabolism
Extensive first-pass metabolism after oral administration.
Metabolized in the liver to ranitidine N-oxide, desmethyl ranitidine, and ranitidine S-oxide.
Elimination Route
Excreted principally in urine.
Following oral administration, excretion of unchanged ranitidine in urine is dose-dependent; about 16–36% (unchanged) is excreted in urine within 24 hours.
Following oral administration, about 4% as ranitidine N-oxide, 1–2% as desmethyl ranitidine, and 1% as ranitidine S-oxide is excreted in urine within 24 hours.
Most of the urinary excretion occurs within the first 6 hours after administration.
The remainder of an orally administered dose is eliminated in feces.
Following IV administration, approximately 70% is excreted in urine as unchanged drug.
Half-life
Adults: Averages 1.7–3.2 hours and may be positively correlated with age.
Children 3.5–16 years of age: Averages 1.8–2 hours (range: 1.4–2.9 hours).
Neonates (<1 month of age): Averages 6.6 hours.
Special Populations
In patients with renal impairment, plasma clearance appears to be decreased and elimination half-life prolonged.
In patients with cirrhosis, minor but clinically unimportant alterations in half-life and reduced clearance occur following oral administration.
In geriatric individuals, clearance appears to be reduced and half-life prolonged because of decreased renal function; although half-life reported to be 3–4 hours following oral or parenteral administration in geriatric patients, in one clinical study it was about 6 hours following an oral 100-mg dose.
Stability
Storage
Oral
Tablets and Tablets for Self-medication
Tablets: 15–30°C in tight, light resistant container. Replace cap securely after opening.
Tablets for self-administration: 20–25°C.
Tablets, Effervescent for Solution (foil-packaged)
2–30°C.
Solution
4–30°C in tight, light resistant container.
Parenteral
Injection
4–25°C; may be exposed to temperatures up to 30°C.
Protect from light.
Protect from freezing.
Darkening of undiluted injection does not affect potency.
Dilutions in most IV solutions: stable for up to 48 hours at room temperature.
Injection for IV infusion only
2–25°C. Brief exposure to temperatures up to 40°C does not affect stability.
Protect from light.
Protect from freezing.
Compatibility
For information on systemic interactions resulting from concomitant use, see Interactions.
Competitively inhibits histamine at parietal cell H2 receptors.
Advice to Patients
Importance of patients informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs.
Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients with phenylketonuria that oral effervescent tablets for solution contain aspartame.
When used for self-medication, importance of reading the product labeling and carefully reviewing the warning information provided by the manufacturer.
Importance of following dosage instructions, unless otherwise directed by a clinician, when ranitidine is administered for self-medication.
Importance of promptly informing clinician of persistent abdominal pain or difficulty swallowing.
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
1 mg (of ranitidine) per mL (50 mg) in 0.45% Sodium Chloride
Zantac® Premixed (in flexible plastic container; preservative-free)
GlaxoSmithKline
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 09/2009. For the most current and up-to-date pricing information, please visit www.drugstore.com. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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