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The Info List - Antiemetics


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An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, antipsychotic medication and chemotherapy directed against cancer. They may be used for severe cases of gastroenteritis, especially if the patient is dehydrated. Antiemetics, though previously thought to cause birth defects, have been proven safe for use by pregnant women in the treatment of morning sickness and the more serious hyperemesis gravidarum.[1][2]

Contents

1 Types 2 See also 3 References

Types[edit] Antiemetics including:

5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they can be used to treat post-operative and cytotoxic drug nausea & vomiting. However, they can also cause constipation or diarrhea, dry mouth, and fatigue.[3]

Dolasetron
Dolasetron
(Anzemet) can be administered in tablet form or in an injection. Granisetron
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
Ondansetron
(Zofran) is administered in an oral tablet form, orally dissolving tablet form, orally dissolving film, sublingual, or in an IV/IM injection. Tropisetron
Tropisetron
(Setrovel, Navoban) can be administered in oral capsules or in injection form. Palonosetron
Palonosetron
(Aloxi) can be administered in an injection or in oral capsules. Mirtazapine
Mirtazapine
(Remeron) is an antidepressant that also has antiemetic effects[4][5] and is also a potent histamine H1 receptor antagonist, Ki=1.6 nM.[6]

Dopamine antagonists act in the brain and are used to treat nausea and vomiting associated with neoplastic disease, radiation sickness, opioids, cytotoxic drugs and general anaesthetics. Side effects include muscle spasms and restlessness.[3]

Domperidone
Domperidone
(Motilium) Olanzapine
Olanzapine
(Zyprexa) Droperidol, haloperidol, chlorpromazine, prochlorperazine. Some of these drugs are limited in their usefulness by their extra-pyramidal and sedative side-effects. Alizapride Prochlorperazine
Prochlorperazine
(Compazine, Stemzine, Buccastem, Stemetil, Phenotil) Metoclopramide
Metoclopramide
(Reglan) also acts on the GI tract as a pro-kinetic, and is thus useful in gastrointestinal disease; however, it is poor in cytotoxic or post-op vomiting. also a 5-HT3 receptor antagonists

NK1 receptor antagonist

Aprepitant
Aprepitant
(Emend) is a commercially available NK1 Receptor antagonist Casopitant
Casopitant
is an investigational NK1 receptor antagonist Rolapitant
Rolapitant
(Varubi) another recently approved drug from this class

Antihistamines (H1 histamine receptor antagonists) are effective in many conditions, including motion sickness, morning sickness in pregnancy, and to combat opioid nausea.

Cinnarizine, available in the UK. Cyclizine Diphenhydramine
Diphenhydramine
(Benadryl) Dimenhydrinate
Dimenhydrinate
(Gravol, Dramamine) Doxylamine Meclizine
Meclizine
(Bonine, Antivert) Promethazine
Promethazine
(Pentazine, Phenergan, Promacot) can be administered via a rectal suppository for adults and children over 2 years of age. Hydroxyzine
Hydroxyzine
(Vistaril)

Cannabinoids are used in patients with cachexia, cytotoxic nausea, and vomiting, or who are unresponsive to other agents. These may cause changes in perception, dizziness, and loss of coordination.[3]

Cannabis, also known as medical marijuana in the United States, is a Schedule I drug.[citation needed] Dronabinol
Dronabinol
(Marinol/Syndros) is a Schedule III drug in the U.S.[citation needed] Some synthetic cannabinoids such as Nabilone
Nabilone
(Cesamet) or the JWH series. Sativex
Sativex
is an oral spray containing THC and CBD. It is currently legal in Canada and a few countries in Europe but not legal in the U.S.[citation needed]

Benzodiazepines

Midazolam
Midazolam
(Versed) is given at the onset of anesthesia has been shown in recent trials to be as effective as ondansetron.[citation needed] Lorazepam
Lorazepam
(Ativan) is said to be very good as an adjunct treatment for nausea along with first line medications such as Compazine.

Anticholinergics

Hyoscine (also known as scopolamine)

Steroids

Dexamethasone
Dexamethasone
(Decadron) is given in low dose at the onset of a general anesthetic as an effective antiemetic. The specific mechanism of action is not fully understood.[citation needed]

Other

Trimethobenzamide
Trimethobenzamide
is thought to work on the CTZ Ginger
Ginger
contains 5-HT3 antagonists gingerols, shogaols,[7] and galanolactone.[8] Preliminary clinical data suggests ginger may be effective for treatment of nausea and/or vomiting in a number of settings.[9][10][11] Emetrol
Emetrol
is also claimed to be an effective antiemetic. Propofol
Propofol
is given intravenously. It has been used in an acute care setting in hospital as a rescue therapy for emesis.[citation needed] Peppermint
Peppermint
is claimed to help nausea or stomach pain when added into a tea or peppermint candies. Muscimol
Muscimol
is purported to have antiemetic activity.[12] Ajwain
Ajwain
is purported to be antiemetic. It is a popular spice in India, Ethiopia
Ethiopia
and Eritrea.[citation needed]

See also[edit]

Cancer
Cancer
and nausea Emetic
Emetic
– substances that induce nausea and vomiting

References[edit]

^ Quinlan, Jeffrey D.; Hill, D. Ashley (1 June 2003). " Nausea and Vomiting
Vomiting
in Pregnancy - American Family Physician". American Family Physician. 68 (1): 121–128. Retrieved 2015-10-09.  ^ Schaefer, Christof; Scialli, Anthony; Rost van Tonningen, Margreet (2001). "Antiemetics and hyperemesis gravidarum". Drugs During Pregnancy and Lactation: Handbook of Prescription Drugs and Comparative Risk Assessment. Gulf Professional Publishing. ISBN 978-0-444-50763-1.  ^ a b c http://www.mesotheliomaweb.org/mesothelioma/treatment/chemotherapy/anti-Enausea-treatment/[permanent dead link] ^ Pae C-U. "Low-dose mirtazapine may be successful treatment option for severe nausea and vomiting". Progress in Neuro-Psychopharmacology and Biological Psychiatry. 30 (6): 1143–5. doi:10.1016/j.pnpbp.2006.03.015.  ^ Kast RE, Foley KF (July 2007). " Cancer
Cancer
chemotherapy and cachexia: mirtazapine and olanzapine are 5-HT3 antagonists with good antinausea effects". European Journal of Cancer
Cancer
Care. 16 (4): 351–4. doi:10.1111/j.1365-2354.2006.00760.x. PMID 17587360.  ^ National Institute of Mental Health. PDSD Ki Database (Internet) [cited 2013 Sep 27]. Chapel Hill (NC): University of North Carolina. 1998-2013. Available from: "Archived copy". Archived from the original on 2013-11-08. Retrieved 2013-12-01.  ^ Abdel-Aziz H, Windeck T, Ploch M, Verspohl EJ (2006-01-13), "Mode of action of gingerols and shogaols on 5-HT3 receptors: binding studies, cation uptake by the receptor channel and contraction of isolated guinea-pig ileum.", Eur J Pharmacol, 530 (1-2): 136–43, doi:10.1016/j.ejphar.2005.10.049, PMID 16364290  ^ Huang, Q.; Iwamoto, Y.; Aoki, S.; Tanaka, N.; Tajima, K.; Yamahara, J.; Takaishi, Y.; Yoshida, M.; Tomimatsu, T.; Tamai, Y. (1991). "Anti-5-hydroxytryptamine3 effect of galanolactone, diterpenoid isolated from ginger". Chemical & pharmaceutical bulletin. 39 (2): 397–399. doi:10.1248/cpb.39.397. PMID 2054863.  ^ Marx, WM; Teleni L; McCarthy AL; Vitetta L; McKavanagh D; Thomson D; Isenring E. (2013). " Ginger
Ginger
(Zingiber officinale) and chemotherapy-induced nausea and vomiting: a systematic literature review". Nutr Rev. 71 (4): 245–54. doi:10.1111/nure.12016. PMID 23550785.  ^ Ernst, E.; Pittler, M.H. (1 March 2000). "Efficacy of ginger for nausea and vomiting: a systematic review of randomized clinical trials" (PDF). British Journal of Anesthesia. 84 (3): 367–371. doi:10.1093/oxfordjournals.bja.a013442. PMID 10793599. Retrieved 6 September 2006.  ^ O'Connor, Anahad (August 21, 2007). "The Claim: Eating Ginger
Ginger
Can Cure Motion Sickness". The New York Times.  ^ hoe 2#section1 Muscimol. Chemical Data Sheet[permanent dead link], Database of Hazardous Materials, CAMEO chemicals

v t e

Pharmacology: major drug groups

Gastrointestinal tract/ metabolism (A)

stomach acid

Antacids H2 antagonists Proton pump inhibitors

Antiemetics Laxatives Antidiarrhoeals/Antipropulsives Anti-obesity drugs Anti-diabetics Vitamins Dietary minerals

Blood
Blood
and blood forming organs (B)

Antithrombotics

Antiplatelets Anticoagulants Thrombolytics/fibrinolytics

Antihemorrhagics

Platelets Coagulants Antifibrinolytics

Cardiovascular system (C)

cardiac therapy/antianginals

Cardiac glycosides Antiarrhythmics Cardiac stimulants

Antihypertensives Diuretics Vasodilators Beta blockers Calcium channel blockers renin–angiotensin system

ACE inhibitors Angiotensin II receptor antagonists Renin inhibitors

Antihyperlipidemics

Statins Fibrates Bile acid sequestrants

Skin (D)

Emollients Cicatrizants Antipruritics Antipsoriatics Medicated dressings

Genitourinary system (G)

Hormonal contraception Fertility agents SERMs Sex hormones

Endocrine system (H)

Hypothalamic–pituitary hormones Corticosteroids

Glucocorticoids Mineralocorticoids

Sex hormones Thyroid hormones/Antithyroid agents

Infections and infestations (J, P, QI)

Antimicrobials: Antibacterials (Antimycobacterials) Antifungals Antivirals Antiparasitics

Antiprotozoals Anthelmintics Ectoparasiticides

IVIG Vaccines

Malignant disease (L01–L02)

Anticancer agents

Antimetabolites Alkylating Spindle poisons Antineoplastic Topoisomerase inhibitors

Immune disease (L03–L04)

Immunomodulators

Immunostimulants Immunosuppressants

Muscles, bones, and joints (M)

Anabolic steroids Anti-inflammatories

NSAIDs

Antirheumatics Corticosteroids Muscle
Muscle
relaxants Bisphosphonates

Brain and nervous system (N)

Analgesics Anesthetics

General Local

Anorectics Anti-ADHD agents Antiaddictives Anticonvulsants Antidementia agents Antidepressants Antimigraine
Antimigraine
agents Antiparkinson
Antiparkinson
agents Antipsychotics Anxiolytics Depressants Entactogens Entheogens Euphoriants Hallucinogens

Psychedelics Dissociatives Deliriants

Hypnotics/Sedatives Mood Stabilizers Neuroprotectives Nootropics Neurotoxins Orexigenics Serenics Stimulants Wakefulness-promoting agents

Respiratory system (R)

Decongestants Bronchodilators Cough medicines H1 antagonists

Sensory organs (S)

Ophthalmologicals Otologicals

Other ATC (V)

Antidotes Contrast media Radiopharmaceuticals Dressings Senotherapeutics

v t e

Antiemetics (A04)

5-HT3 serotonin ion channel antagonists

Alosetron Azasetron Bemesetron Cilansetron Clozapine Dazopride Dolasetron Granisetron Lerisetron Metoclopramide Mianserin Mirtazapine Olanzapine Ondansetron Palonosetron
Palonosetron
(+netupitant) Quetiapine Ramosetron Ricasetron Tropisetron Zatosetron

5-HT serotonin G-protein receptor antagonists

Clozapine Cyproheptadine Hydroxyzine Olanzapine Risperidone Ziprasidone

CB1 agonists (cannabinoids)

Dronabinol Nabilone Tetrahydrocannabinol
Tetrahydrocannabinol
(cannabis)

D2/D3 antagonists

Alizapride Bromopride Chlorpromazine Clebopride Domperidone Haloperidol Hydroxyzine Itopride Metoclopramide Metopimazine Prochlorperazine Thiethylperazine Trimethobenzamide

H1 antagonists (antihistamines)

Cyclizine Dimenhydrinate Diphenhydramine Hydroxyzine Meclizine Promethazine

mACh antagonists (anticholinergics)

Atropine Diphenhydramine Hydroxyzine
Hydroxyzine
(very mild) Hyoscyamine Scopolamine

NK1 antagonists

Aprepitant Casopitant Ezlopitant Fosaprepitant Maropitant Netupitant Rolapitant Vestipitant

Others

Cerium oxalate Dexamethasone Lorazepam

.