Granisetron (HCl)
Granisetron is an oral and parenteral antiemetic agent. Granisetron (HCl) is commonly used to treat nausea and vomiting from highly emetogenic cancer chemotherapy. The actions, uses and adverse effects similar to those of ondansetron, but unlike ondansetron, Granisetron (HCl) is not approved for postoperative emesis. Granisetron selectively blocks type 3 serotonin (5-HT3) receptors. 5-HT3 receptors are found centrally in the chemoreceptor trigger zone and peripherally at vagal nerve terminals in the intestines. Whether the action of granisetron is mediated centrally, peripherally, or a combination of both remains to be determined.Granisetron injection was approved by the FDA on December 29, 1993. The oral dosage form was subsequently approved March 20, 1995 and has been shown to be as effective as IV ondansetron for chemotherapy-induced nausea and vomiting.
Primary Characteristics
It is of Synthetic origin and belongs to Inazole.
Molecular Weight: 348.9 · Solubility in Water: > 1 in 10 · Solubility in Alcohol: 1 in 120 · Non-proprietary name: Granisetron (HCl).
Pharmacokinetics
Absorption: Granisetron (HCl) has an oral bioavailability is 50% (±50%), pre-systemic (first-pass) metabolism accounts for 46.5% (±12.5%).
Distribution: Granisetron (HCl) has a volume of distribution is 243 litre. plasma protein binding is 65 %.
Elimination: plasma half-life is 3.9 hr, renal excretion is 12 % unchanged.
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Indications
Granisetron (HCl) is primarily indicated in conditions like Nausea and vomiting (chemotherapy induced), Nausea and vomiting (chemotherapy induced), prevention, Nausea and vomiting associated with chemotherpy, Post operative vomiting, Post-operative nausea and vomiting.
Contraindications
Granisetron (HCl) is contraindicated in conditions like Hypersensitivity, Sub-acute intestinal obstruction.
Dosage
Granisetron (HCl)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 3 mg | 3 mg | — | IV-Inf (over 5 min) | Prevention, before start of chemotherapy (up to 2 additional doses may be given within 24 hrs). |
| 3 mg | 3 mg | — | Iv-Inf (over 5 min) | Treatment, as for prevention (the two additional doses must not be given < 10 min apart), Max.9 mg in 24hrs. |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
The signs and symptoms that are produced after acute overdosage of Granisetron (HCl) are Headache.
Granisetron (HCl) is known to cause more or less tolerable side effects which are usually transient. These include Constipation , Decreased GI motility, Headache, Hypersensitivity reactions, Rashes .
Warnings / Precautions
Interference in Pathology
Granisetron (HCl) may interfere in the diagnosis of None well documented.
Available Brands
Storage Conditions
Drug Classification
- 1.17.2 — Antiemetics & antinauseants