Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/366
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ZANTAC (Injection)
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Parenteral Administration: In some hospitalized patients with pathological
hypersecretory conditions or intractable duodenal ulcers, or in patients
who are unable to take oral medication, ZANTAC may be administered
parenterally according to the following recommendations:<br/>Intramuscular Injection: 50 mg (2 mL) every 6 to 8 hours.
(No dilution necessary.)<br/>Intermittent Intravenous Injection:<br/>Continuous Intravenous Infusion: Add ZANTAC Injection to 5% dextrose injection or
other compatible IV solution (see Stability). Deliver at a rate of
6.25 mg/h (e.g., 150 mg [6 mL] of ZANTAC Injection
in 250 mL of 5% dextrose injection at10.7 mL/h). For Zollinger-Ellison patients, dilute ZANTAC Injection
in 5% dextrose injection or other compatible IV solution (see Stability)
to a concentration no greater than 2.5 mg/mL. Start the infusion
at a rate of 1.0 mg/kg per hour. If after 4 hours either
a measured gastric acid output is>10 mEq/h or the patient becomes
symptomatic, the dose should be adjusted upward in 0.5-mg/kg per hour
increments, and the acid output should be remeasured. Dosages up to
2.5 mg/kg per hour and infusion rates as high as 220 mg/h
have been used.<br/>Pediatric Use: While limited data exist on the administration of
IV ranitidine to children, the recommended dose in pediatric patients
is for a total daily dose of 2 to 4 mg/kg, to be divided and
administered every 6 to 8 hours, up to a maximum of 50 mg
given every 6 to 8 hours. This recommendation is derived from
adult clinical studies and pharmacokinetic data in pediatric patients.
Limited data in neonatal patients (less than one month of age) receiving
ECMO have shown that a dose of 2 mg/kg is usually sufficient
to increase gastric pH to>4 for at least 15 hours. Therefore,
doses of 2 mg/kg given every 12 to 24 hours or as a continuous
infusion should be considered.<br/>ZANTAC Injection Premixed
in Flexible Plastic Containers:<br/>Instructions for Use:<br/>Preparation for Administration: Use aseptic technique.<br/>Caution: ZANTAC Injection Premixed in flexible plastic containers
is to be administered by slow IV drip infusion only. Additives should not be introduced into this solution. If used with a primary IV fluid system, the primary solution should
be discontinued during ZANTAC Injection Premixed infusion. Do not administer unless solution is clear and container
is undamaged.<br/>Warning: Do not use flexible plastic container in series
connections.<br/>Dosage Adjustment for Patients
With Impaired Renal Function: 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, the recommended dosage
in patients with a creatinine clearance<50 mL/min is 50 mg
every 18 to 24 hours. Should the patient's condition require,
the frequency of dosing may be increased to every 12 hours or
even further with caution. Hemodialysis reduces the level of circulating
ranitidine. Ideally, the dosing schedule should be adjusted so that
the timing of a scheduled dose coincides with the end of hemodialysis. 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).<br/>Stability: Undiluted, ZANTAC Injection tends to exhibit a yellow
color that may intensify over time without adversely affecting potency.
ZANTAC 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 Injection Premixed in flexible plastic containers
is sterile through the expiration date on the label when stored under
recommended conditions. Note: Parenteral drug products should be inspected visually
for particulate matter and discoloration before administration whenever
solution and container permit.
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The active ingredient in ZANTAC Injection and
ZANTAC 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 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.<br/>Sterile Injection for Intramuscular
or Intravenous Administration: Each 1 mL of aqueous solution contains ranitidine
25 mg (as the hydrochloride); phenol 5 mg as preservative;
and 0.96 mg of monobasic potassium phosphate and 2.4 mg
of dibasic sodium phosphate as buffers.<br/>Sterile, Premixed Solution
for Intravenous Administration in Single-Dose, Flexible Plastic Containers: Each 50 mL contains ranitidine HCl equivalent
to 50 mg of ranitidine, sodium chloride 225 mg, and citric
acid 15 mg and dibasic sodium phosphate 90 mg as buffers
in water for injection. It contains no preservatives. The osmolarity
of this solution is 180 mOsm/L (approx.), and the pH is 6.7 to
7.3. The flexible plastic container is fabricated
from a specially formulated, nonplasticized, thermoplastic co-polyester
(CR3). Water can permeate from inside the container into the overwrap
but not in amounts sufficient to affect the solution significantly.
Solutions inside the plastic container also can leach out certain
of the chemical components in very small amounts before the expiration
period is attained. However, the safety of the plastic has been confirmed
by tests in animals according to USP biological standards for plasticcontainers.
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ZANTAC is a competitive, reversible inhibitor
of the action of histamine at the histamine H-receptors,
including receptors on the gastric cells. ZANTAC does not lower serum
Ca++ in hypercalcemic states. ZANTAC is not an anticholinergic agent.<br/>Pharmacokinetics:<br/>Absorption: ZANTAC is absorbed
very rapidly after intramuscular (IM) injection. Mean peak levels
of 576 ng/mL occur within 15 minutes or less following a 50-mg IM
dose. Absorption from IM sites is virtually complete, with a bioavailability
of 90% to 100% compared with intravenous (IV) administration. Following
oral administration, the bioavailability of ZANTAC Tablets is 50%.<br/>Distribution: The volume
of distribution is about 1.4 L/kg. Serum protein binding averages
15%.<br/>Metabolism: In humans,
the N-oxide is the principal metabolite in the urine; however, this
amounts to<4% of the dose. Other metabolites are the S-oxide (1%)
and the desmethyl ranitidine (1%). The remainder of the administered
dose is found in the stool. Studies in patients with hepatic dysfunction
(compensated cirrhosis) indicate that there are minor, but clinically
insignificant, alterations in ranitidine half-life, distribution,
clearance, and bioavailability.<br/>Excretion: Following
IV injection, approximately 70% of the dose is recovered in the urine
as unchanged drug. Renal clearance averages 530 mL/min, with a total
clearance of 760 mL/min. The elimination half-life is 2.0 to 2.5 hours. Four patients with clinically significant renal function
impairment (creatinine clearance 25 to 35 mL/min) administered
50 mg of ranitidine intravenously had an average plasma half-life
of 4.8 hours, a ranitidine clearance of 29 mL/min, and a
volume of distribution of 1.76 L/kg. In general, these parameters
appear to be altered in proportion to creatinine clearance (see DOSAGE
AND ADMINISTRATION).<br/>Geriatrics: The plasma half-life is prolonged and total clearance
is reduced in the elderly population due to a decrease in renal function.
The elimination half-life is 3.1 hours (see PRECAUTIONS: Geriatric
Use and DOSAGE AND ADMINISTRATION: Dosage Adjustment for Patients
with Impaired Renal Function).<br/>Pediatrics: There
are no significant differences in the pharmacokinetic parameter values
for ranitidine in pediatric patients (from 1 month up to 16 years
of age) and healthy adults when correction is made for body weight.
The pharmacokinetics of ZANTAC in pediatric patients are summarized
in Table 1. T= Terminal
half-life; CLp = Plasma clearance of ranitidine. ECMO = extracorporeal membrane oxygenation. Plasma clearance in neonatal patients (less than 1
month of age) receiving ECMO was considerably lower (3 to 4 mL/min/kg)
than observed in children or adults. The elimination half-life in
neonates averaged 6.6 hours as compared to approximately 2 hours in
adults and pediatric patients.<br/>Pharmacodynamics: Serum concentrations
necessary to inhibit 50% of stimulated gastric acid secretion are
estimated to be 36 to 94 ng/mL. Following single IV or IM 50-mg
doses, serum concentrations of ZANTAC are in this range for 6 to 8 hours.<br/>Antisecretory Activity:<br/>Other Pharmacologic Actions:<br/>Pediatrics: The ranitidine concentration necessary to suppress
basal acid secretion by at least 90% has been reported to be 40 to
60 ng/mL in pediatric patients with duodenal or gastric ulcers. In a study of 20 critically ill pediatric patients
receiving ranitidine IV at 1 mg/kg every 6 hours, 10 patients
with a baseline pH���4 maintained this baseline throughout the
study. Eight of the remaining 10 patients with a baseline of pH���2
achieved pH���4 throughout varying periods after dosing. It should
be noted, however, that because these pharmacodynamic parameters were
assessed in critically ill pediatric patients, the data should be
interpreted with caution when dosing recommendations are made for
a less seriously ill pediatric population. In
another small study of neonatal patients (n = 5) receiving
ECMO, gastric pH<4 pretreatment increased to>4 after a 2 mg/kg
dose and remained above 4 for at least 15 hours.<br/>Clinical Trials:<br/>Active Duodenal Ulcer: In a multicenter, double-blind, controlled, US study
of endoscopically diagnosed duodenal ulcers, earlier healing was seen
in the patients treated with oral ZANTAC as shown in Table 3. *All patients were permitted
p.r.n. antacids for relief of pain. P<0.0001. In these studies,
patients treated with oral ZANTAC reported a reduction in both daytime
and nocturnal pain, and they also consumed less antacid than the placebo-treated
patients.<br/>Pathological Hypersecretory
Conditions (such as Zollinger-Ellison syndrome): ZANTAC inhibits gastric acid secretion and reduces
occurrence of diarrhea, anorexia, and pain in patients with pathological
hypersecretion associated with Zollinger-Ellison syndrome, systemic
mastocytosis, and other pathological hypersecretory conditions (e.g.,
postoperative, "short-gut" syndrome, idiopathic). Use of oral ZANTAC
was followed by healing of ulcers in 8 of 19 (42%) patients who were
intractable to previous therapy. In a retrospective
review of 52 Zollinger-Ellison patients given ZANTAC as a continuous
IV infusion for up to 15 days, no patients developed complications
of acid-peptic disease such as bleeding or perforation. Acid output
was controlled to���10 mEq/h.
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ZANTAC Injection and ZANTAC Injection Premixed
are contraindicated for patients known to have hypersensitivity to
the drug.
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ZANTAC Injection, 25 mg/mL, containing phenol 0.5% as preservative, is available
as follows: NDC 0173-0362-38, 2-mL single-dose
vials (Tray of 10) NDC 0173-0363-01, 6-mL multidose
vials (Singles) Store
between 4��and 25��C (39��and 77��F); excursions
permitted to 30��C (86��F). Protect from light. ZANTAC Injection Premixed, 50 mg/50 mL, in 0.45% sodium chloride, is available as
a sterile, premixed solution for IV administration in single-dose,
flexible plastic containers (NDC 0173-0441-00) (case of 24).
It contains no preservatives. Store between 2��and 25��C (36��and
77��F). Protect from light. 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 Injection: GlaxoSmithKline Research Triangle Park, NC 27709 ZANTAC Injection Premixed: Manufactured for GlaxoSmithKline Research Triangle
Park, NC 27709 by Hospira, Inc., Lake Forest,
IL 60045 ZANTAC is a registered trademark of
Warner-Lambert Company, used under license. ��2008, GlaxoSmithKline. All rights reserved. March 2008ZNJ:2PI
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There has been virtually no experience with overdosage
with ZANTAC 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 in excess of 225 mg/kg per 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 LDvalues
in mice and rats were 77 and 83 mg/kg, respectively.
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ranitidine hydrochloride
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ZANTAC (Injection)
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Transient pain at the site of IM injection has
been reported. Transient local burning or itching has been reported
with IV administration of ZANTAC. The following
have been reported as events in clinical trials or in the routine
management of patients treated with oral or parenteral ZANTAC. The
relationship to therapy with ZANTAC has been unclear in many cases.
Headache, sometimes severe, seems to be related to administration
of ZANTAC.<br/>Central Nervous System: Rarely, malaise, dizziness, somnolence, insomnia,
and vertigo. Rare cases of reversible mental confusion, agitation,
depression, and hallucinations have been reported, predominantly in
severely ill elderly patients. Rare cases of reversible blurred vision
suggestive of a change in accommodation have been reported. Rare reports
of reversible involuntary motor disturbances have been received.<br/>Cardiovascular: As with other H-blockers, rare reports
of arrhythmias such as tachycardia, bradycardia, asystole, atrioventricular
block, and premature ventricular beats.<br/>Gastrointestinal: Constipation, diarrhea, nausea/vomiting, abdominal
discomfort/pain, and rare reports of pancreatitis.<br/>Hepatic: In normal volunteers,
SGPT values were increased to at least twice the pretreatment levels
in 6 of 12 subjects receiving 100 mg q.i.d. intravenously
for 7 days, and in 4 of 24 subjects receiving 50 mg
q.i.d. intravenously for 5 days. There have been occasional reports
of hepatocellular, cholestatic, or mixed hepatitis, with or without
jaundice. In such circumstances, ranitidine should be immediately
discontinued. These events are usually reversible, but in rare circumstances
death has occurred. Rare cases of hepatic failure have also been reported.<br/>Musculoskeletal: Rare reports of arthralgias and myalgias.<br/>Hematologic: Blood count changes (leukopenia, granulocytopenia,
and thrombocytopenia) have occurred in a few patients. These were
usually reversible. Rare cases of agranulocytosis, pancytopenia, sometimes
with marrow hypoplasia, and aplastic anemia and exceedingly rare cases
of acquired immune hemolytic anemia have been reported.<br/>Endocrine: Controlled studies in animals and humans have shown
no stimulation of any pituitary hormone by ZANTAC and no antiandrogenic
activity, and cimetidine-induced gynecomastia and impotence in hypersecretory
patients have resolved when ZANTAC has been substituted. However,
occasional cases of gynecomastia, impotence, and loss of libido have
been reported in male patients receiving ZANTAC, but the incidence
did not differ from that in the general population.<br/>Integumentary: Rash, including rare cases of erythema multiforme.
Rare cases of alopecia and vasculitis.<br/>Repiratory: A large epidemiological study suggested an increased
risk of developing pneumonia in current users of histamine-2���receptor
antagonists (HRAs) compared to patients who had stopped
HRAs treatment, with an observed adjusted relative risk
of 1.63 (95% CI, 1.07���2.48). However, a causal relationship
between use of HRAs and pneumonia has not been established.<br/>Other: Rare cases of hypersensitivity reactions (e.g.,
bronchospasm, fever, rash, eosinophilia), anaphylaxis, angioneurotic
edema, acute interstitial nephritis, and small increases in serum
creatinine.
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ZANTAC Injection and ZANTAC 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.
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ZANTAC
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