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Antiemetics (cont.)

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

Fosaprepitant

Drug Nomenclature

Fosaprépitant; Fosaprepitantum.

{3-[((2R,3S)-2-{(1R)-1-[3,5-bis(Trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)morpholin-4-yl)methyl]-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl}phosphonic acid.
Фозапрепитант
C23H22F7N4O6P = 614.4.
CAS — 172673-20-0.

Fosaprepitant Meglumine

Drug Nomenclature

Fosaprepitant Dimeglumine; Fosaprepitant meglumina; Fosaprépitant
Méglumine; Meglumini Fosaprepitantum; MK-0517.

1-Deoxy-1-(methylamino)-D-glucitol {3-[((2R,3S)-2-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)-4-morpholinyl)methyl]- 2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl}phosphonate.
Меглумина Фозапрепитант
C23H22F7N4O6P, 2C7H17NO5 = 1004.8.
CAS — 265121-04-8.

Stability. US licensed product information states that, once reconstituted and diluted as directed in sodium chloride 0.9%, a solution of fosaprepitant meglumine is stable for 24 hours at room temperature (at or below 25°).

Adverse Effects and Precautions

As for Aprepitant.

Interactions

As for Aprepitant.

Pharmacokinetics

Fosaprepitant is rapidly converted to aprepitant for the pharmacokinetics of aprepitant.

Uses and Administration

Fosaprepitant is aprodrug of the antiemetic aprepitant, which is a neurokinin-1 receptor antagonist. Fosaprepitant meglumine is used for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic or moderately emetogenic cancer chemotherapy. Doses are expressed in terms of the base 188 mg of fosaprepitant meglumine is equivalent to about 115 mg of fosaprepitant. A dose of fosaprepitant meglumine equivalent to 115 mg fosaprepitant may be given intravenously instead of oral aprepitant, with a corticosteroid and a 5-HT3 antagonist (for details, see Administration, under Aprepitant). The reconstituted dose of fosaprepitant is diluted in llOmL of sodium chloride 0.9% to a final concentration of 1 mg/mL and infused over 15 minutes.

Proprietary Preparations

Czech Republic: Ivemend

Portugal: Ivemend

United Kingdom: Ivemend

USA: Emend.

Ginger

Drug Nomenclature

Synonyms: Gengibre; Gingembre; Gyömbér gyökértörzs; Imbierų šakniastiebiai; Ingefära; Ingwer; Inkivääri; Jengibre; Zázvorový oddenek; Zingib.; Zingiber; Zingiberis Rhizoma

Pharmacopoeias. In China, Europe, Japan, and US. US also includes the powdered form.

European Pharmacopoeia, 6th ed. (Ginger). The dried, whole or cut rhizome of Zingiber officinale, with the cork removed, either completely or from the wide flat surfaces only. Whole or cut, it contains not less than 1.5% of essential oil, calculated with reference to the anhydrous drug. It has a characteristic aromatic odour. Protect from light.

The BP 2008 states that ginger may be known in commerce as unbleached ginger.

The United States Pharmacopeia 31, 2008 (Ginger). The scraped, partially scraped, or unscraped rhizome of Zingiber officinale (Zingiberaceae), known in commerce as unbleached ginger. It contains not less than 4.5% of alcohol-soluble extractive and not less than 10% of water-soluble extractive. Store at 8° to 15°. Protect from light and moisture.

Drug Profile

Ginger has carminative properties. It is used as a flavouring agent and has been tried for the prophylaxis of motion sickness and nausea and vomiting in pregnancy, although it does not seem to be effective for postoperative nausea and vomiting.

Ginger oil is used in aromatherapy.

Homoeopathy. Ginger has been used in homoeopathic medicines under the following names: Zingiber Zingiber officinale Zing.

Preparations

BP 2008: Aromatic Cardamom Tincture; Strong Ginger Tincture; Weak Ginger Tincture

The United States Pharmacopeia 31, 2008: Ginger Capsules; Ginger Tincture.

Proprietary Preparations

Australia: Travacalm Natural

Canada: Gravol Natural Source

Germany: Zinto-na

Switzerland: Zintona

Thailand: Zinaxin

UK: Travel Sickness; Zinaxin.

Multi-ingredient

Australia: Bioglan Ginger-Vite Forte Bioglan Psylli-Nucil Plus Boswellia Complex Boswellia Compound Broncafect Cal Alkyline Diaco Digestive Aid Dyzco Extralife Arthri-Care Feminine Herbal Complex Ginkgo Plus Herbal Plus Formula I Of Herbal Cleanse Herbal Digestive Formula Lifesystem Herbal Plus Formula II Ginkgo PC Regulax Peritone PNS Support PNT Complex Travelaide

Austria: Nariazeller

Brazil: Broncol Tussifen

Canada: Cayenne Plusf Chase Kolik Gripe Water

Czech Republic: Klosterfrau Nelisana Naturland Grosser Swedenbitter

France: Arthrolib Evacrine

Germany: Fovysat Gallexier Gastricard Gastrosecur Gastrysat JuVitorr Najocarmin forte Presselin Dyspeptikum Unex Amarum

Hong Kong: Nagesto

India: Carmicide Happy’tizer Papytazyme Tummy Ease Well-Beeing

Indonesia: Avogin Pectum Pregnasea

Italy: Donalg Lozione Same Urto Pik Gel

Malaysia: Dandelion Complex Strepsils Cough Lozenge Strepsils Cough Syrup Total Marr Zinaxin Plus

Philippines: Bo-D-Fense Ruflex

Poland: Nelisana Klosterfrau

Russia: Dipana (Дипана); Doktor Mom (Доктор Мом); Doktor Mom Herbal Cough Lozenges (Доктор Мом Растительные Пастилки От Кашля); Maraslavin (Мараславин); Original Grosser Bittner Balsam (Оригинальный Большой Бальзам Биттнера); Suprima-Broncho (Суприма-бронхо);

South Africa: Hel-montskruie Lewensessens Wonderkroonessens

Singapore: Artrex

Switzerland: Padma-Lax Padmed Laxan Tisane pour les problemes de prostate

Thailand: Carmicide Flatulence Magesto Mesto-O Papytazyme Zinaxin Plus

United Kingdom: Arheumacare Digestive HRI Golden Seal Digestive; Indian Brandee Indigestion Reliet Neo Baby Gripe Mixture Neo Gripe Mixture Traveleeze Wind & Dyspepsia Reliet Zinopin

Venezuela: Ervossil Jengimiel Jengimiel Sabila

Indisetron Dihydrochloride

Drug Nomenclature

Synonyms: Indisetron Dihydrochloride; N-3389
INN: Indisetron Hydrochloride [rINNM (en)]
INN: Hidrocloruro de indisetrón [rINNM (es)]
INN: Indisétron, Chlorhydrate d’ [rINNM (fr)]
INN: Indisetroni Hydrochloridum [rINNM (la)]
INN: Индисетрона Гидрохлорид [rINNM (ru)]
Chemical name: N-(3,9-Dimethyl-endo-3,9-diazabicyclo[3.3.1]non-7-yl)-1H-indazole-3-carboxamide dihydrochloride
Molecular formula: C17H23N5O,2HCl =386.3
CAS: 141549-75-9 (indisetron); 160472-97-9 (indisetron dihydrochloride)

Drug Profile

Indisetron is a 5-HT3-receptor antagonist with general properties similar to those of ondansetron it is also stated to be an antagonist at 5-HT4 receptors. Indisetron hydrochloride is used as an antiemetic in the management of nausea and vomiting associated with chemotherapy.

Itopride Hydrochloride

Drug Nomenclature

Synonyms: HC-803; HSR-803; Itoprida, hidrocloruro de
INN: Itopride Hydrochloride [rINNM (en)]
INN: Hidrocloruro de itoprida [rINNM (es)]
INN: Itopride, Chlorhydrate d’ [rINNM (fr)]
INN: Itopridi Hydrochloridum [rINNM (la)]
INN: Итоприда Гидрохлорид [rINNM (ru)]
Chemical name: N-{p-[2-(Dimethylamino)ethoxy]benzyl}veratramide hydrochloride
Molecular formula: C20H26N2O4,HCl =394.9
CAS: 122898-67-3 (itopride)

Drug profile

Itopride hydrochloride is a substituted benzamide with general properties similar to those of metoclopramide that has been used for its prokinetic and antiemetic actions in oral doses of 50 mg three times daily before meals.

Proprietary Preparations

Czech Republic: Ganaton

India: Itoprid

Japan: Ganaton

Malaysia: Ganaton.

Mecloxamine Citrate

Drug Nomenclature

INN: Mecloxamine Citrate [rINNM (en)]
INN: Citrato de mecloxamina [rINNM (es)]
INN: Mécloxamine, Citrate de [rINNM (fr)]
INN: Mecloxamini Citras [rINNM (la)]
INN: Меклоксамина Цитрат [rINNM (ru)]
Chemical name: 2-[1-(4-Chlorophenyl)-1-phenylethoxy]-N,N-dimethyl-1-propanamine citrate
Molecular formula: C19H24ClNO,C6H8O7 =510.0
CAS: 5668-06-4 (mecloxamine); 56050-03-4 (mecloxamine citrate)

Drug profile

Mecloxamine citrate is reported to have antimuscarinic properties and has been used for its antiemetic action in antimigraine preparations.

Preparations – Multi-ingredient

Austria: Avamigran

Turkey: Avmigran.

Metopimazine

Drug Approvals

(British Approved Name, US Adopted Name, rINN)

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

Synonyms: EXP-999; Metopimazina; RP-9965
BAN: Metopimazine
USAN: Metopimazine
INN: Metopimazine [rINN (en)]
INN: Metopimazina [rINN (es)]
INN: Métopimazine [rINN (fr)]
INN: Metopimazinum [rINN (la)]
INN: Метопимазин [rINN (ru)]
Chemical name: 1-[3-(2-Methylsulphonylphenothiazin-10-yl)propyl]piperidine-4-carboxamide
Molecular formula: C22H27N3O3S2 =445.6
CAS: 14008-44-7
ATC code: A04AD05

Pharmacopoeias. In France.

Drug profile

Metopimazine, a phenothiazine dopamine antagonist, is an antiemetic with general properties similar to those of chlorpromazine. It is used in the management of nausea and vomiting, including that associated with cancer chemotherapy. It is given in usual oral doses of 15 to 30 mg daily, in 2 to 4 divided doses similar daily doses have been given by rectum in 3 divided doses. It has also been given by injection in a dose of 10 to 20 mg daily, usually intramuscularly but occasionally by the intravenous route. Higher doses of 30 to 50 mg daily by intramuscular injection or intravenous infusion have been given for chemotherapy-induced nausea and vomiting.

Proprietary Preparations

Denmark: Vogalene

France: Vogalene Vogalib.

Ramosetron Hydrochloride

Drug Nomenclature

Synonyms: Ramosetrón, hidrocloruro de; YM-060
INN: Ramosetron Hydrochloride [rINNM (en)]
INN: Hidrocloruro de ramosetrón [rINNM (es)]
INN: Ramosétron, Chlorhydrate de [rINNM (fr)]
INN: Ramosetroni Hydrochloridum [rINNM (la)]
INN: Рамосетрона Гидрохлорид [rINNM (ru)]
Chemical name: (-)-(R)-1-Methylindol-3-yl 4,5,6,7-tetrahydro-5-benzimidazolyl ketone hydrochloride
Molecular formula: C17H17N3O,HCl =315.8
CAS: 132036-88-5 (ramosetron); 132907-72-3 (ramosetron hydrochloride)

Drug profile

Ramosetron is a 5-HT3 antagonist with general properties similar to those of ondansetron. Ramosetron hydrochloride is given for its antiemetic properties in the management of nausea and vomiting induced by cancer chemotherapy in usual doses of 300 micrograms once daily intravenously, or 100 micrograms once daily by mouth. Ramosetron is also under investigation in the management of diarrhea-predominant irritable bowel syndrome.

Proprietary Preparations

Indonesia: Nasea

Japan: Nasea

Philippines: Nasea

Thailand: Nasea

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