Zantac Information
Zantac (Ranitidine) Description
The active ingredient in Zantac (Ranitidine) Injection and Zantac (Ranitidine) Injection Premixed is ranitidine hydrochloride (HCl), a histamine H-receptor antagonist. Chemically it is N[2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]-N′-methyl-2-nitro-1,1-ethenediamine, hydrochloride. It has the following structure:
The empirical formula is CHNOS●HCl, representing a molecular weight of 350.87.
Ranitidine HCl is a white to pale yellow, granular substance that is soluble in water.
Zantac (Ranitidine) Injection is a clear, colorless to yellow, nonpyrogenic liquid. The yellow color of the liquid tends to intensify without adversely affecting potency. The pH of the injection solution is 6.7 to 7.3.
Zantac (Ranitidine) Clinical Pharmacology
Zantac (Ranitidine) is a competitive, reversible inhibitor of the action of histamine at the histamine H-receptors, including receptors on the gastric cells. Zantac (Ranitidine) does not lower serum Ca++ in hypercalcemic states. Zantac (Ranitidine) is not an anticholinergic agent.
Zantac (Ranitidine) Indications And Usage
Zantac (Ranitidine) Injection and Zantac (Ranitidine) Injection Premixed are indicated in some hospitalized patients with pathological hypersecretory conditions or intractable duodenal ulcers, or as an alternative to the oral dosage form for short-term use in patients who are unable to take oral medication.
Zantac (Ranitidine) Contraindications
Zantac (Ranitidine) Injection and Zantac (Ranitidine) Injection Premixed are contraindicated for patients known to have hypersensitivity to the drug.
Zantac (Ranitidine) Precautions
Ranitidine has been reported to affect the bioavailability of other drugs through several different mechanisms such as competition for renal tubular secretion, alteration of gastric pH, and inhibition of cytochrome P450 enzymes.
Ranitidine may alter the absorption of drugs in which gastric pH is an important determinant of bioavailability. This can result in either an increase in absorption (e.g., triazolam, midazolam, glipizide) or a decrease in absorption (e.g., ketoconazole, atazanavir, delavirdine, gefitinib). Appropriate clinical monitoring is recommended.
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There was no indication of tumorigenic or carcinogenic effects in life-span studies in mice and rats at oral dosages up to 2,000 mg/kg/day.
Ranitidine was not mutagenic in standard bacterial tests (, ) for mutagenicity at concentrations up to the maximum recommended for these assays.
In a dominant lethal assay, a single oral dose of 1,000 mg/kg to male rats was without effect on the outcome of 2 matings per week for the next 9 weeks.
The safety and effectiveness of Zantac (Ranitidine) Injection have been established in the age-group of 1 month to 16 years for the treatment of duodenal ulcer. Use of Zantac (Ranitidine) in this age-group is supported by adequate and well-controlled studies in adults, as well as additional pharmacokinetic data in pediatric patients, and an analysis of the published literature.
Safety and effectiveness in pediatric patients for the treatment of pathological hypersecretory conditions have not been established.
Limited data in neonatal patients (less than 1 month of age) receiving ECMO suggest that Zantac (Ranitidine) may be useful and safe for increasing gastric pH for patients at risk of gastrointestinal hemorrhage.
Clinical studies of Zantac (Ranitidine) Injection did not include sufficient numbers of subjects aged 65 and over to determine whether they responded differently from younger subjects. However, in clinical studies of oral formulations of Zantac (Ranitidine) , of the total number of subjects enrolled in US and foreign controlled clinical trials, for which there were subgroup analyses, 4,197 were 65 and over, while 899 were 75 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
This drug is known to be substantially excreted by the kidney and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, caution should be exercised in dose selection, and it may be useful to monitor renal function (see CLINICAL PHARMACOLOGY: Pharmacokinetics: Geriatric Use and DOSAGE AND ADMINISTRATION: Dosage Adjustment for Patients With Impaired Renal Function).
Zantac (Ranitidine) Adverse Reactions
Transient pain at the site of IM injection has been reported. Transient local burning or itching has been reported with IV administration of Zantac (Ranitidine) .
The following have been reported as events in clinical trials or in the routine management of patients treated with oral or parenteral Zantac (Ranitidine) . The relationship to therapy with Zantac (Ranitidine) has been unclear in many cases. Headache, sometimes severe, seems to be related to administration of Zantac (Ranitidine) .
Zantac (Ranitidine) Overdosage
There has been virtually no experience with overdosage with Zantac (Ranitidine) Injection and limited experience with oral doses of ranitidine. Reported acute ingestions of up to 18 g orally have been associated with transient adverse effects similar to those encountered in normal clinical experience (see ADVERSE REACTIONS). In addition, abnormalities of gait and hypotension have been reported.
When overdosage occurs, clinical monitoring and supportive therapy should be employed.
Studies in dogs receiving dosages of Zantac (Ranitidine) in excess of 225 mg/kg/day have shown muscular tremors, vomiting, and rapid respiration. Single oral doses of 1,000 mg/kg in mice and rats were not lethal. Intravenous LD values in mice and rats were 77 and 83 mg/kg, respectively.
Zantac (Ranitidine) Dosage And Administration
The administration of ranitidine as a continuous infusion has not been evaluated in patients with impaired renal function. On the basis of experience with a group of subjects with severely impaired renal function treated with Zantac (Ranitidine) , the recommended dosage in patients with a creatinine clearance
Elderly patients are more likely to have decreased renal function, therefore caution should be exercised in dose selection, and it may be useful to monitor renal function (see CLINICAL PHARMACOLOGY: Pharmacokinetics: Geriatric Use and PRECAUTIONS: Geriatric Use).
Undiluted, Zantac (Ranitidine) Injection tends to exhibit a yellow color that may intensify over time without adversely affecting potency. Zantac (Ranitidine) Injection is stable for 48 hours at room temperature when added to or diluted with most commonly used IV solutions, e.g., 0.9% sodium chloride injection, 5% dextrose injection, 10% dextrose injection, lactated ringer's injection, or 5% sodium bicarbonate injection.
Zantac (Ranitidine) Injection Premixed in flexible plastic containers is sterile through the expiration date on the label when stored under recommended conditions.
Note:
Zantac (Ranitidine) How Supplied
NDC 0173-0362-38, 2-mL single-dose vials (Tray of 10)
NDC 0173-0363-01, 6-mL multidose vials (Singles)
Exposure of pharmaceutical products to heat should be minimized. Avoid excessive heat; however, brief exposure up to 40°C does not adversely affect the product. Protect from freezing.
GlaxoSmithKline
Research Triangle Park, NC 27709
Zantac (Ranitidine) Injection:
GlaxoSmithKline
Research Triangle Park, NC 27709
Zantac (Ranitidine) Injection Premixed:
Manufactured for GlaxoSmithKline
Research Triangle Park, NC 27709
by Hospira, Inc., Lake Forest, IL 60045
Zantac (Ranitidine) is a registered trademark of Warner-Lambert Company, used under license.
MULTISTIK is a registered trademark of Bayer Healthcare LLC.
©2009, GlaxoSmithKline. All rights reserved.
April 2009
ZNJ:5PI
Zantac (Ranitidine) Principal Display Panel
Zantac (Ranitidine)
Rantidine Hydrochloride Injection
50 mg
5 x 2 ml Single-Dose Vials
