Naurif

Granisetron is a highly selective 5-HT3 receptor antagonist with little or no affinity for other serotonin receptors. It blocks serotonin peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone.

Serotonin receptors of the 5-HT3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. During chemotherapy that induces vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT3 receptors. This evokes vagal afferent discharge, inducing vomiting. Animal studies demonstrate that, in binding to 5-HT3 receptors, 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.

Induced metabolism with phenobarbital. Risk of serotonin syndrome with other serotonergic agents e.g. SSRIs, and serotonin and norepinephrine reuptake inhibitors (SNRIs). Altered clearance with CYP enzyme inducers or inhibitors. Concomitant use with drugs known to prolong QT interval may result in clinical consequences.

Headache, insomnia, constipation, diarrhoea, elevated hepatic transaminases; QT prolongation; bradycardia, palpitations, sick sinus syndrome, chest pain. Application site reactions (transdermal): Rash, pain, erythema, pruritus, irritation, burn, vesicles, urticaria, discolouration; patch non-adhesion.

Pregnancy Category B. No evidence of impaired fertility or harm to the animal fetus have been found. However, this drug may be used in pregnancy only if clearly needed. It is not known whether granisetron is excreted in human milk. So cautions hould be exercised when granisetron is administered to a nursing mother.

Patient with cardiac co-morbidities, on cardiotoxic chemotherapy and/or woth concomitant electrolyte abnormalities. May mask progressive ileus and/or gastric distention. Childn. Pregnancy and lactation.

Pediatric Uses: Safety and effectiveness of granisetron in paediatric patients under 2 years have not been established.

Geriatric use: Efficacy and safety were maintained with increasing age

Anti-emetic drugs, Supportive Care Therapy

Store between 15-30°C. Protect from light.