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Granisetron (Clinical Pharmacology)
In this article, we will discuss Granisetron (Clinical Pharmacology). So, let’s get started. Clinical PharmacologyGranisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT1; 5-HT1A; 5-HT1B/C; 5-HT2; for alpha1-, alpha2-, or beta-adrenoreceptors; for dopamine-D2; or for histamine-H1; benzodiazepine;…
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Granisetron
In this article, we will discuss Granisetron (Dosage Overview). So, let’s get started. IndicationsGranisetron hydrochloride tablets USP are indicated for the prevention of:• Nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin.• Nausea and vomiting associated with radiation, including total body irradiation and fractionated…
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Granisetron
Common Brand Names: Kytril
Therapeutic Class: Antiemetic, selective 5-HT3 receptor antagonist
Common Injectable Dosage Forms:
Solution for Injection: 1 mg/mL (1 mL, 4 mL vials) and 0.1 mg/mL (1 mL vials)
Dosage Ranges:
Prophylaxis of chemotherapy-related emesis in patients 2 years and older: 10 mcg/kg/dose (maximum 1 mg/dose) given 30 minutes prior to chemotherapy.
For some chemotherapy drugs with longer onset of action: 10 mcg/kg every 12 hours.
No adjustment necessary in renal/hepatic impairment.
Given on scheduled basis, not PRN basis, because it has not been shown to be effective once nausea and vomiting have begun.
Administration and Stability: Administer IV push over 30 seconds or as a 5–10-minute infusion. Store vials at room temperature and protect from light. Granisetron is stable when mixed in NS or D5W for 7 days refrigerated or 3 days at room temperature. pH 4-7.3
Pharmacology/Pharmacokinetics: Granisetron is a selective 5-HT3 receptor antagonist, blocking serotonin both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone. Effects usually last up to 24 hours. Terminal half0life is 5-9 hours. Granisetron is distributed widely throughout the body, its volume of distribution is 2-4 L/kg.
Drug and Lab Interactions: Granisetron is a substrate of CYP3A4 and may enhance the hypotensive effects of apomorphine. St. John’s Wort may decrease granisetron levels.
Contraindications/Precautions: Granisetron is contraindicated in patients with a pervious hypersensitivity to it or other 5-HT3 receptor antagonists. Use caution following abdominal surgery as granisetron may mask progressive ileus or gastric distention. Safety and efficacy in children <2 years old has not been established. Injection contains benzyl alcohol and should be used in neonates. Pregnancy Category B.
Monitoring Parameters: Monitor patient for chest pain, respiratory difficulty, pain, or itching, as well as s/s of nausea/vomiting.
Adverse Effects: Headache, constipation, musculoskeletal weakness, and hypertension have been reported to some degree. Also possible are pain, fever, dizziness, insomnia, somnolence, anxiety, agitation, and rash.
Common Clinical Applications: Used for the prophylaxis of nausea and vomiting associated with emetogenic chemotherapy and radiation therapy.
Inilah Obat Antimual Akibat Kemoterapi Pertama yang Bertahan 5 Hari dalam Tubuh
Inilah Obat Antimual Akibat Kemoterapi Pertama yang Bertahan 5 Hari dalam Tubuh
Majalah Farmasetika (V1N6-Agustus 2016). Mual dan muntah adalah efek samping yang umum dari pengobatan kemoterapi untuk kanker. Efek samping ini umumnya dapat dikontrol dengan penggunaan obat anti-mual, salah satunya adalah granisetron.
Heron Therapeutics mendapatkan persetujuan dari US Food and Drug Administration (FDA) untuk obat anti-mual akibat kemoterapi dalam bentuk extended-release, Sustol…
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CDER New April 8, 2013
FDA (U.S. Food and Drug Administration) [ http://www.fda.gov/?source=govdelivery ] *What's New on the FDA Drugs Site* *April 5, 2013* * Current Drug Shortages Index [ http://www.fda.gov/Drugs/DrugSafety/DrugShortages/ucm050792.htm?source=govdelivery ] (updated) * Drugs to be Discontinued: Granisetron HCl Injection [ http://www.fda.gov/Drugs/DrugSafety/DrugShortages/ucm050794.htm?source=govdelivery ] * Drug Firm Annual Registration Status Download File [ http://www.fda.gov/Drugs/InformationOnDrugs/ucm135778.htm?source=govdelivery ] (updated) * Drug Firm Annual Registration Status [ http://www.accessdata.fda.gov/scripts/cder/drls/default.cfm?source=govdelivery ] (updated) * Guidance for Industry: Providing Postmarket Periodic Safety Reports in the ICH E2C(R2) Format (Periodic Benefit-Risk Evaluation Report) (PDF – 183KB) [ http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM346564.pdf?source=govdelivery ] * Medical, Statistical, and Clinical Pharmacology Reviews of Pediatric Reviews (FDASIA) [ http://www.fda.gov/Drugs/DevelopmentApprovalProcess/DevelopmentResources/ucm316937.htm?source=govdelivery ] (updated) * Medication Guides [ http://www.fda.gov/Drugs/DrugSafety/ucm085729.htm?source=govdelivery ] (updated) * MedWatch Safety Alert: BIVIGAM Immune Globulin Intravenous (Human), 10 Percent Liquid, 100 mL Sterile Vial: Recall - Visible Particles Observed [ http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm346771.htm?source=govdelivery ] * National Drug Code Directory [ http://www.fda.gov/Drugs/InformationOnDrugs/ucm142438.htm?source=govdelivery ] (updated)
