Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1220
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Kytril (Injection, Solution)
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NOTE: KYTRIL 1 MG/1 ML CONTAINS BENZYL ALCOHOL .<br/>Prevention of Chemotherapy-Induced Nausea and Vomiting: The recommended dosage for KYTRIL Injection is 10 mcg/kg administered intravenously within 30 minutes before initiation of chemotherapy, and only on the day(s) chemotherapy is given.<br/>Infusion Preparation: KYTRIL Injection may be administered intravenously either undiluted over 30 seconds, or diluted with 0.9% Sodium Chloride or 5% Dextrose and infused over 5 minutes.<br/>Pediatric Patients: The recommended dose in pediatric patients 2 to 16 years of age is 10 mcg/kg . Pediatric patients under 2 years of age have not been studied.<br/>Geriatric Patients, Renal Failure Patients or Hepatically Impaired Patients: No dosage adjustment is recommended .<br/>Prevention and Treatment of Postoperative Nausea and Vomiting: The recommended dosage for prevention of postoperative nausea and vomiting is 1 mg of KYTRIL, undiluted, administered intravenously over 30 seconds, before induction of anesthesia or immediately before reversal of anesthesia. The recommended dosage for the treatment of nausea and/or vomiting after surgery is 1 mg of KYTRIL, undiluted, administered intravenously over 30 seconds.<br/>Pediatric Patients: Safety and effectiveness of KYTRIL Injection have not been established in pediatric patients for the prevention or treatment of postoperative nausea or vomiting.<br/>Geriatric Patients, Renal Failure Patients or Hepatically Impaired Patients: No dosage adjustment is recommended .
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| dailymed-instance:descripti... |
KYTRIL (granisetron hydrochloride) Injection is an antinauseant and antiemetic agent. Chemically it is endo-N-(9-methyl-9-azabicyclo [3.3.1] non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride with a molecular weight of 348.9 (312.4 free base). Its empirical formula is CHNO���HCl, while its chemical structure is: Granisetron hydrochloride is a white to off-white solid that is readily soluble in water and normal saline at 20��C. KYTRIL Injection is a clear, colorless, sterile, nonpyrogenic, aqueous solution for intravenous administration. KYTRIL 1 mg/1 mL is available in 1 mL single-use and 4 mL multi-use vials. KYTRIL 0.1 mg/1 mL is available in a 1 mL single-use vial. 1 mg/1 mL: Each 1 mL contains 1.12 mg granisetron hydrochloride equivalent to granisetron, 1 mg; sodium chloride, 9 mg; citric acid, 2 mg; and benzyl alcohol, 10 mg, as a preservative. The solution's pH ranges from 4.0 to 6.0. 0.1 mg/1 mL: Each 1 mL contains 0.112 mg granisetron hydrochloride equivalent to granisetron, 0.1 mg; sodium chloride, 9 mg; citric acid, 2 mg. Contains no preservative. The solution's pH ranges from 4.0 to 6.0.
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| dailymed-instance:clinicalP... |
Granisetron is a selective 5-hydroxytryptamine(5-HT) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT; 5-HT; 5-HT; 5-HT; for alpha-, alpha- or beta-adrenoreceptors; for dopamine-D; or for histamine-H; benzodiazepine; picrotoxin or opioid receptors. Serotonin receptors of the 5-HTtype are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. During chemotherapy-induced vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HTreceptors. This evokes vagal afferent discharge and may induce vomiting. Animal studies demonstrate that, in binding to 5-HTreceptors, granisetron blocks serotonin stimulation and subsequent vomiting after emetogenic stimuli such as cisplatin. In the ferret animal model, a single granisetron injection prevented vomiting due to high-dose cisplatin or arrested vomiting within 5 to 30 seconds. In most human studies, granisetron has had little effect on blood pressure, heart rate or ECG. No evidence of an effect on plasma prolactin or aldosterone concentrations has been found in other studies. KYTRIL Injection exhibited no effect on oro-cecal transit time in normal volunteers given a single intravenous infusion of 50 mcg/kg or 200 mcg/kg. Single and multiple oral doses slowed colonic transit in normal volunteers.<br/>Pharmacokinetics:<br/>Chemotherapy-Induced Nausea and Vomiting: In adult cancer patients undergoing chemotherapy and in volunteers, mean pharmacokinetic data obtained from an infusion of a single 40 mcg/kg dose of KYTRIL Injection are shown in Table 1.<br/>Distribution: Plasma protein binding is approximately 65% and granisetron distributes freely between plasma and red blood cells.<br/>Metabolism: Granisetron metabolism involves N-demethylation and aromatic ring oxidation followed by conjugation. In vitro liver microsomal studies show that granisetron's major route of metabolism is inhibited by ketoconazole, suggestive of metabolism mediated by the cytochrome P-450 3A subfamily. Animal studies suggest that some of the metabolites may also have 5-HTreceptor antagonist activity.<br/>Elimination: Clearance is predominantly by hepatic metabolism. In normal volunteers, approximately 12% of the administered dose is eliminated unchanged in the urine in 48 hours. The remainder of the dose is excreted as metabolites, 49% in the urine, and 34% in the feces.<br/>Subpopulations:<br/>Gender: There was high inter- and intra-subject variability noted in these studies. No difference in mean AUC was found between males and females, although males had a higher Cgenerally.<br/>Elderly: The ranges of the pharmacokinetic parameters in elderly volunteers (mean age 71 years), given a single 40 mcg/kg intravenous dose of KYTRIL Injection, were generally similar to those in younger healthy volunteers; mean values were lower for clearance and longer for half-life in the elderly patients (see Table 1).<br/>Pediatric Patients: A pharmacokinetic study in pediatric cancer patients (2 to 16 years of age), given a single 40 mcg/kg intravenous dose of KYTRIL Injection, showed that volume of distribution and total clearance increased with age. No relationship with age was observed for peak plasma concentration or terminal phase plasma half-life. When volume of distribution and total clearance are adjusted for body weight, the pharmacokinetics of granisetron are similar in pediatric and adult cancer patients.<br/>Renal Failure Patients: Total clearance of granisetron was not affected in patients with severe renal failure who received a single 40 mcg/kg intravenous dose of KYTRIL Injection.<br/>Hepatically Impaired Patients: A pharmacokinetic study in patients with hepatic impairment due to neoplastic liver involvement showed that total clearance was approximately halved compared to patients without hepatic impairment. Given the wide variability in pharmacokinetic parameters noted in patients and the good tolerance of doses well above the recommended 10 mcg/kg dose, dosage adjustment in patients with possible hepatic functional impairment is not necessary.<br/>Postoperative Nausea and Vomiting: In adult patients (age range, 18 to 64 years) recovering from elective surgery and receiving general balanced anesthesia, mean pharmacokinetic data obtained from a single 1 mg dose of KYTRIL Injection administered intravenously over 30 seconds are shown in Table 2. The pharmacokinetics of granisetron in patients undergoing surgery were similar to those seen in cancer patients undergoing chemotherapy.
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| dailymed-instance:contraind... |
KYTRIL Injection is contraindicated in patients with known hypersensitivity to the drug or to any of its components.
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KYTRIL Injection, 1 mg/1 mL (free base), is supplied in 1 mL Single-Use Vials and 4 mL Multi-Use Vials. CONTAINS BENZYL ALCOHOL. NDC 0004-0239-09 (package of 1 Single-Use Vial)NDC 0004-0240-09 (package of 1 Multi-Use Vial) KYTRIL Injection, 0.1 mg/1 mL (free base), is supplied in 1 mL Single-Use Vials. CONTAINS NO PRESERVATIVE. NDC 0004-0242-08 (package of 5 Single-Use Vials)<br/>Storage: Store single-use vials and multi-use vials at 25��C (77��F); excursions permitted to 15��to 30��C (59��to 86��F). [See USP Controlled Room Temperature] Once the multi-use vial is penetrated, its contents should be used within 30 days. Do not freeze. Protect from light.
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There is no specific antidote for KYTRIL Injection overdosage. In case of overdosage, symptomatic treatment should be given. Overdosage of up to 38.5 mg of granisetron hydrochloride injection has been reported without symptoms or only the occurrence of a slight headache.
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granisetron hydrochloride
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Kytril (Injection, Solution)
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| dailymed-instance:adverseRe... |
Chemotherapy-Induced Nausea and Vomiting: The following have been reported during controlled clinical trials or in the routine management of patients. The percentage figures are based on clinical trial experience only. Table 10 gives the comparative frequencies of the five most commonly reported adverse events (���3%) in patients receiving KYTRIL Injection, in single-day chemotherapy trials. These patients received chemotherapy, primarily cisplatin, and intravenous fluids during the 24-hour period following KYTRIL Injection administration. Events were generally recorded over seven days post-KYTRIL Injection administration. In the absence of a placebo group, there is uncertainty as to how many of these events should be attributed to KYTRIL, except for headache, which wasclearly more frequent than in comparison groups. In over 3,000 patients receiving KYTRIL Injection (2 to 160 mcg/kg) in single-day and multiple-day clinical trials with emetogenic cancer therapies, adverse events, other than those in Table 10, were observed; attribution of many of these events to KYTRIL is uncertain. Hepatic: In comparative trials, mainly with cisplatin regimens, elevations of AST and ALT (>2 times the upper limit of normal) following administration of KYTRIL Injection occurred in 2.8% and 3.3% of patients, respectively. These frequencies were not significantly different from those seen with comparators (AST: 2.1%; ALT: 2.4%). Cardiovascular: Hypertension (2%); hypotension, arrhythmias such as sinus bradycardia, atrial fibrillation, varying degrees of A-V block, ventricular ectopy including non-sustained tachycardia, and ECG abnormalities have been observed rarely. Central Nervous System: Agitation, anxiety, CNS stimulation and insomnia were seen in less than 2% of patients. Extrapyramidal syndrome occurred rarely and only in the presence of other drugs associated with this syndrome. Hypersensitivity: Rare cases of hypersensitivity reactions, sometimes severe (eg, anaphylaxis, shortness of breath, hypotension, urticaria) have been reported. Other: Fever (3%), taste disorder (2%), skin rashes (1%). In multiple-day comparative studies, fever occurred more frequently with KYTRIL Injection (8.6%) than with comparative drugs (3.4%, P<0.014), which usually included dexamethasone.<br/>Postoperative Nausea and Vomiting: The adverse events listed in Table 11 were reported in���2% of adults receiving KYTRIL Injection 1 mg during controlled clinical trials. In a clinical study conducted in Japan, the types of adverse events differed notably from those reported above in Table 11. The adverse events in the Japanese study that occurred in���2% of patients and were more frequent with KYTRIL 1 mg than with placebo were: fever (56% to 50%), sputum increased (2.7% to 1.7%), and dermatitis (2.7% to 0%).
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Hypersensitivity reactions may occur in patients who have exhibited hypersensitivity to other selective 5-HTreceptor antagonists.
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KYTRIL Injection is indicated for:
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Kytril
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