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Antiemetics

Antiemetics are a diverse group of drugs used to treat or prevent nausea and vomiting, including that associated with cancer therapy, anaesthesia, and motion sickness (see below).

The choice of drug depends partly on the cause of nausea and vomiting. For example, hyoscine or an antihistamine are used in motion sickness whereas dopamine antagonists (such as metoclopramide and domperidone) and serotonin 5-HT3-receptor antagonists (5-HT3 antagonists), such as ondansetron, are ineffective. Conversely, nausea and vomiting associated with cancer chemotherapy is often hard to control and special regimens have been devised including the use of the 5-HT3 antagonists, dexamemasone, and, more recently, the neurokinin-1 receptor antagonist aprepitant.

Described in this site are:

  • Alizapride
  • Aprepitant
  • Azasetron
  • Bromopride
  • Cerium Oxalate
  • Clebopride
  • Difenidol
  • Dolasetron
  • Domperidone
  • Dronabinol
  • Fosaprepitant
  • Ginger
  • Granisetron
  • Indisetron
  • Itopride
  • Mecloxamine Citrate
  • Metoclopramide
  • Metopimazine
  • Nabilone
  • Ondansetron
  • Palonosetron
  • Ramosetron
  • Tropisetron

Azasetron Hydrochloride

Drug Nomenclature

Synonyms: Azasetrón, hidrocloruro de; Nazasetron Hydrochloride; Y-25130
INN: Azasetron Hydrochloride [rINNM (en)]
INN: Hidrocloruro de azasetrón [rINNM (es)]
INN: Azasétron, Chlorhydrate d’ [rINNM (fr)]
INN: Azasetroni Hydrochloridum [rINNM (la)]
INN: Азасетрона Гидрохлорид [rINNM (ru)]
Chemical name: (±)-6-Chloro-3,4-dihydro-4-methyl-3-oxo-N-3-quinuclidinyl-2H-1,4-benzoxazine-8-carboxamide hydrochloride
Molecular formula: C17H20ClN3O3,HCl =386.3
CAS: 123040-69-7 (azasetron); 141922-90-9 (azasetron hydrochloride)

Profile

Azasetron is a 5-HT3 antagonist with general properties similar to those of ondansetron. It is used as an antiemetic in the management of nausea and vomiting induced by cytotoxic therapy. Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously.

Proprietary Preparations

Argentina: Serotone

Japan: Serotone.

Bromopride

Drug Nomenclature

Synonyms: Bromoprida; CM-8252; VAL-13081
INN: Bromopride [rINN (en)]
INN: Bromoprida [rINN (es)]
INN: Bromopride [rINN (fr)]
INN: Bromopridum [rINN (la)]
INN: Бромоприд [rINN (ru)]
Chemical name: 4-Amino-5-bromo-N-(2-diethylaminoethyl)-o-anisamide
Molecular formula: C14H22BrN3O2 =344.2
CAS: 4093-35-0
ATC code: A03FA04

Profile

Bromopride is a substituted benzamide similar to metoclopramide, used in a variety of gastrointestinal disorders including nausea and vomiting and motility disorders. It is given in a usual oral dose of 20 to 60 mg daily in divided doses, or 20 mg daily by intramuscular or intravenous injection. The hydrochloride is also used.

Preparations

Proprietary Preparations

Brazil: Bilenzima Bromoprid Digerex Digesan Digesprid Digestil Digesting Digeston Pangest Plamet Prided I

Italy: Procirex Valopride

Multi-ingredient

Brazil: Digecap-Zimatico Enziprid Lansoprid Primeral

Portugal: Modulanzime.

Cerium Oxalate

Drug Nomenclature

Synonyms: Cerii Oxalas; Cerio, oxalato de; Ceriumoksalaatti; Ceriumoxalat
CAS: 139-42-4 (anhydrous cerous oxalate); 15053-73-3 (cerous oxalate decahydrate)
ATC code: A04AD02

Note

Cerium oxalate has been defined as consisting of about 50% of cerous oxalate ((C2O4)3Ce2,10H2O) with the oxalates of numerous other rare earths, especially lanthanum, praseodymium, and neodymium. Oxalates of the form (C2O4)3Ce2,xH2O are also referred to as cerium or cerous oxalate.

Profile

Cerium oxalate has been used as an antiemetic.

Preparations – Multi-ingredient

Spain: Novonausin

Clebopride

Drug Approvals

(British Approved Name, US Adopted Name, rINN)

INNs in other languages (French, Latin, and Spanish):

Synonyms: LAS-9273
BAN: Clebopride
USAN: Clebopride
INN: Clebopride [rINN (en)]
INN: Cleboprida [rINN (es)]
INN: Clébopride [rINN (fr)]
INN: Clebopridum [rINN (la)]
INN: Клебоприд [rINN (ru)]
Chemical name: 4-Amino-N-(1-benzyl-4-piperidyl)-5-chloro-o-anisamide
Molecular formula: C20H24ClN3O2 =373.9
CAS: 55905-53-8
ATC code: A03FA06

Clebopride Malate

Drug Approvals

(British Approved Name Modified, rINNM)

INNs in main languages (French, Latin, and Spanish):

Synonyms: Cleboprida, malato de; Clebopridi Malas; Kleboprid malát; Kleboprid-malát; Klebopridimalaatti; Klebopridmalat; Kleboprido malatas
BAN: Clebopride Malate [BANM]
INN: Clebopride Malate [rINNM (en)]
INN: Malato de cleboprida [rINNM (es)]
INN: Clébopride, Malate de [rINNM (fr)]
INN: Clebopridi Malas [rINNM (la)]
INN: Клебоприда Малат [rINNM (ru)]
Molecular formula: C20H24ClN3O2,C4H6O5 =508.0
CAS: 57645-91-7
ATC code: A03FA06

Pharmacopoeias. In Europe.

European Pharmacopoeia, 6th ed. (Clebopride Malate). A white or almost white, crystalline powder. Sparingly soluble in water and in methyl alcohol slightly soluble in dehydrated alcohol practically insoluble in dichloromethane. The pH of a 1% solution in water is 3.8 to 4.2. Protect from light.

Profile

Clebopride is a substituted benzamide similar to metoclopramide, that is used for its antiemetic and prokinetic actions in nausea and vomiting and various other gastrointestinal disorders. It is given as the malate but doses are expressed in terms of the base. Clebopride malate 679 micrograms is equivalent to about 500 micrograms of clebopride. Clebopride malate is given in a usual oral dose equivalent to clebopride 0.5 mg three times daily before meals or 0.5 to 1 mg by intramuscular or intravenous injection for acute symptoms. For dosage in children see below.

Administration in children. Adolescents aged 12 to 20 years may be given clebopride malate orally in a dose equivalent to clebopride 250 micrograms three times daily. An oral dose of 15 to 20 micrograms/kg daily in 3 divided doses may be used for children under 12 the following doses have been recommended:

• 1 to 4 years: 50 micrograms 3 times daily

• 4 to 8 years: 100 micrograms 3 times daily

• 8 to 10 years: 150 micrograms 3 times daily

• 10 to 12 years: 200 micrograms 3 times daily

Preparations

Proprietary Preparations

Argentina: Gastridin

Indonesia: Clast

Italy: Motilex

Portugal: Clebofex Clebutec

Spain: Cleboril.

Multi-ingredient

Argentina: Eudon Gastridin-E Somasedan

Spain: Clanzoflat Flatoril.

Difenidol Hydrochloride

Drug Approvals

(British Approved Name Modified, rINNM)

INNs in main languages (French, Latin, and Spanish):

Synonyms: Difenidol, hidrocloruro de; Diphenidol Hydrochloride; SKF-478 (difenidol); SKF-478-A; SKF-478-J (difenidol embonate)
BAN: Difenidol Hydrochloride [BANM]
USAN: Diphenidol Hydrochloride
INN: Difenidol Hydrochloride [rINNM (en)]
INN: Hidrocloruro de difenidol [rINNM (es)]
INN: Difénidol, Chlorhydrate de [rINNM (fr)]
INN: Difenidoli Hydrochloridum [rINNM (la)]
INN: Дифенидола Гидрохлорид [rINNM (ru)]
Chemical name: 1,1-Diphenyl-4-piperidinobutan-1-ol hydrochloride
Molecular formula: C21H27NO,HCl =345.9
CAS: 972-02-1 (difenidol); 3254-89-5 (difenidol hydrochloride); 26363-46-2 (difenidol embonate)

Pharmacopoeias. In China, and Japan.

Profile

Difenidol hydrochloride is an antiemetic that probably acts through the chemoreceptor trigger zone. It is claimed to control vertigo by means of a specific effect on the vestibular apparatus. Difenidol also has a weak peripheral antimuscarinic action.

It has been used in the treatment of some forms of nausea and vomiting such as those associated with surgery, radiotherapy, and cancer chemotherapy. It has also been used for the symptomatic treatment of vertigo, nausea and vomiting due to Meniere’s disease, and other labyrinthine disturbances.

It has been given in oral doses equivalent to 25 to 50 mg of difenidol every 4 hours as required. Difenidol hydrochloride has also been given parenterally.

Proprietary Preparations

Brazil: Vontrol

Chile: Vontrol

Hong Kong: Cephadol

Japan: Cephadol

Malaysia: Cephadol

Mexico: Biomitin Diphafen Hemetiken Lansenol Nautrol Normavom Serratol Sons Vontrol Voxamine

Philippines: Cephadol

Singapore: Cephadol

Thailand: Cephadol.

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