CLASSIFICATION OF 5-HYDROXY TRYPTAMINE (5-HT) ANTAGONISTS

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5-hydroxytryptamine (5-HT) antagonists

5-hydroxytryptamine (5-HT) antagonists are known as serotonin receptor antagonists. They are a type of medication that prevents serotonin from acting in the body. Serotonin is a neurotransmitter and it regulates mood, appetite, sleep, and other things.

EXAMPLE

  • Ondansetron: This is a medication used to prevent nausea and vomiting, particularly in cancer patients undergoing chemotherapy.
  • Cyproheptadine: This is an antihistamine that is also used to treat migraines and serotonin syndrome.
  • Ketanserin: This medication is used to treat hypertension and Raynaud’s disease.
  • Methysergide: This medication is used to prevent migraines.
  • Pizotifen: This medication is also used to prevent migraines

5-HT antagonists work by binding to serotonin receptors and preventing serotonin from activating these receptors. This can help treat conditions where serotonin levels are high or where excessive activation of serotonin receptors is causing symptoms. It is important to note that serotonin has important physiological functions, and completely blocking its effects can result in unwanted side effects.

Uses

  • Prevention of nausea and vomiting:– Ondansetron and granisetron are common medications used to prevent nausea and vomiting, especially in cancer patients undergoing chemotherapy.
  • Migraine prevention:- Methysergide, pizotifen, and cyproheptadine are medications used to prevent migraines, possibly by reducing serotonin release in the brain.
  • Treatment of hypertension:- Ketanserin is a hypertension medication that works by blocking the effects of serotonin on blood vessels.
  • Treatment of serotonin syndrome:- Cyproheptadine is occasionally used to treat serotonin syndrome, which is a potentially fatal condition caused by an excess of serotonin in the body.
  • Management of irritable bowel syndrome:– Alosetron is a medication used to treat irritable bowel syndrome symptoms, possibly by decreasing the gut’s sensitivity to serotonin.
  • Management of anxiety and depression:– Some 5-HT antagonists, such as pindolol, have been studied as potential treatments for anxiety and depression by modulating serotonin effects in the brain.

CLASSIFICATION

CLASSIFICATION OF 5-HYDROXYTRYPTAMINE ANTAGONISTS
CLASSIFICATION OF 5-HYDROXY TRYPTAMINE (5-HT) ANTAGONISTS

CLASSIFICATION OF 5-HYDROXY TRYPTAMINE (5-HT) ANTAGONISTS

  • Nonselective antagonists & partial agonists/antagonists– Ergotamine, Lysergic acid diethyl amide (LSD), 2-Bromo LSD, Methysergide, Cyproheptadine, Cinnarizine
  • 5-HT2 Antagonists– Ketanserin, Ritanserin, Clozapine, Risperidone
  • 5-HT3 Antagonists-Ramosetron, Ondansetron, Granisetron, Tropisetron, Palonosetron

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