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Antiemetics

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Antiemetics can be used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer. 

 

They may be used for gastroenteritis.

5 classes antidopaminergic drugs, antiserotoninergic, antihistamines, anticholinergics and neurokinins.

Antidopaminergic antiemetics are associated with be a threefold increased risk of stroke shortly after the initiation of treatment: domperidone, metopimazine, and metoclopramide.

5-hydroxytryptamine 3 receptor antagonists odansetron, granisetron dolasetron,and palonesetron.

Palonesetron is a second generation 5-HT3RA and has a significantly longer half-life than the first generation compounds.

Aprepitant, fosaprepitant, fosapretant, rolapitant, netipitant, fosnetupitant are neurokinin-1 receptor antgonists

Antiemetic

 

5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. 

 

 

5-HT3 receptor antagonists can be used to treat post-operative and cytotoxic induced drug nausea and vomiting. 

 

 

5-HT3 receptor antagonists can cause constipation or diarrhea, dry mouth, and fatigue.

 

 

Dolasetron (Anzemet) can be administered in tablet form or in an injection.

 

 

Granisetron (Kytril, Sancuso) can be administered in tablet (Kytril), oral solution (Kytril), injection D(Kytril), or in a single transdermal patch to the upper arm (SANCUSO).

 

 

Ondansetron (Zofran) is administered in an oral tablet form, orally dissolving tablet form, orally dissolving film, sublingual, or in an IV/IM injection.

 

 

Tropisetron (Setrovel, Navoban) can be administered in oral capsules or in injection form.

 

 

Palonosetron (Aloxi) can be administered in an injection or in oral capsules.

 

 

Dopamine antagonists act on the brainstem and are used to treat nausea and vomiting associated with cancer, radiation sickness, opioids, cytotoxic drugs and general anaesthetics. 

 

 

Side effects of dopamine antagonists include muscle spasms and restlessness.

 

 

Olanzapine (Zyprexa)

 

 

Haloperidol 

 

 

Alizapride

 

 

Prochlorperazine (Compazine) 

 

 

Chlorpromazine 

 

 

Metoclopramide

 

 

NK1 receptor antagonists

 

 

Aprepitant (Emend) 

 

 

Antihistamines-H1 histamine receptor antagonists are effective in motion sickness, morning sickness in pregnancy, and to combat opioid nausea. 

 

 

H1 receptors are present in brain central areas include area postrema and vomiting center in the vestibular nucleus. 

 

 

Antihistamines have anticholinergic properties that block muscarinic receptors at the same sites.

 

 

Agents include:

 

 

Cyclizine

 

 

Diphenhydramine 

 

 

Dimenhydrinate 

 

 

Doxylamine

 

 

Mirtazapine an antidepressant that also has antiemetic effects it is also a potent histamine H1 receptor antagonist.

 

 

Meclizine 

 

 

Promethazine can be administered via a rectal suppository, intravenous injection, oral tablet or oral suspension for adults and children over 2 years of age.

 

 

Hydroxyzine 

 

 

Cannabinoids are used in patients with cachexia, cytotoxic nausea, and vomiting, or who are unresponsive to other agents. 

 

 

Dronabinol 

 

 

Nabilone 

 

 

Sativex an oral spray contains THC and CBD. 

 

 

Benzodiazepines 

 

 

Midazolam 

 

 

Lorazepam 

 

 

Anticholinergics

 

 

Hyoscine 

 

 

Atropine

 

 

Diphenhydramine

 

 

Steroids

 

 

Dexamethasone 

 

 

Trimethobenzamide is thought to work on the CTZ

 

 

Ginger contains 5-HT3 antagonists 

 

 

Emetrol

 

 

Propofol 

 

 

Peppermint 

 

 

Muscimol

 

 

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