Granisetron; Indications, Dosage, Side Effect, Interactions, Pregnancy

Granisetron
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Granisetron is an indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
Granisetron is a Serotonin-3 Receptor Antagonist. The mechanism of action of granisetron is as a Serotonin 3 Receptor Antagonist.

Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors

Mechanism of Action of Granisetron

Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zoneThe drug is structurally and pharmacologically related to ondansetron, another selective inhibitor of 5-HT3 receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

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Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.

Indications of Granisetron

Contra Indications of Granisetron

Dosage of Granisetron

Strengths: 1 mg , 2 mg,10 mg ,40 mcg/kg, 2 mg/10 mL; 1 mg/mL  IV;

Nausea/Vomiting in Chemotherapy Induced

  • IV: 10 mcg/kg over 5 minutes, beginning 30 minutes before initiation of chemotherapy.
  • Orally: 2 mg, given up to 1 hour before chemotherapy, or 1 mg twice a day (the first dose is given up to 1 hour before chemotherapy, and the second dose is given 12 hours later).
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Nausea/Vomiting in Postoperative

  • IV: 1 mg undiluted over 30 seconds, given before induction of anesthesia, or immediately before reversal of anesthesia; or give after surgery.

Nausea/Vomiting in Radiation Induced

  • slow or irregular heartbeat

2 mg orally given within 1 hour of radiotherapy.

Side Effects of Granisetron

The most common

Common

Rare

Drug Interactions of Granisetron

Granisetron may interact with following drugs, supplyments, & may change the efficacy of drugs

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Pregnancy & Lactation of Granisetron

FDA Pregnancy Risk Category B
Pregnancy

There are no available data on the use of granisetron in pregnant women; however, animal studies have revealed no teratogenic effects. Granisetron injection, patch, and oral formulations are classified as FDA pregnancy risk category B. It is not known if granisetron crosses the placenta; however, due to its low molecular weight, passage across the placental barrier is expected.

Lactation

It is unknown whether granisetron or its metabolites are excreted in human milk. As a precautionary measure, breastfeeding should not be advised during treatment with Granisetron.

  1. References

    1. https://www.drugs.com/mtm/granisetron.html
    2. https://pubchem.ncbi.nlm.nih.gov

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