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Antidiarrheals (cont.)

Described in this site are:

  • Albumin Tannate
  • Attapulgite
  • Bismuth Compounds
  • Bran
  • Chalk
  • Difenoxin
  • Diphenoxylate
  • Ispaghula
  • Kaolin
  • Lidamidine
  • Loperamide
  • Racecadotril
  • Smectites
  • Zaldaride

Difenoxin

Drug Nomenclature

Synonyms: Difenoxilic Acid; Difenoxina; Diphenoxylic Acid; McN-JR-15403-11
BAN: Difenoxin
USAN: Difenoxin
INN: Difenoxin [rINN (en)]
INN: Difenoxina [rINN (es)]
INN: Difénoxine [rINN (fr)]
INN: Difenoxinum [rINN (la)]
INN: Дифеноксин [rINN (ru)]
Chemical name: 1-(3-Cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylic acid
Molecular formula: C28H28N2O2 =424.5
CAS: 28782-42-5
ATC code: A07DA04

Difenoxin Hydrochloride

Drug Approvals

(British Approved Name Modified, rINNM)

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

Drug Nomenclature

Synonyms: Difenoxina, hidrocloruro de; Difenoxylic Acid Hydrochloride; Diphenoxylic Acid Hydrochloride; R-15403
BAN: Difenoxin Hydrochloride [BANM]
INN: Difenoxin Hydrochloride [rINNM (en)]
INN: Hidrocloruro de difenoxina [rINNM (es)]
INN: Difénoxine, Chlorhydrate de [rINNM (fr)]
INN: Difenoxini Hydrochloridum [rINNM (la)]
INN: Дифеноксина Гидрохлорид [rINNM (ru)]
Molecular formula: C28H28N2O2,HCl =461.0
CAS: 35607-36-4
ATC code: A07DA04

Profile

Difenoxin is the principal active metabolite of diphenoxylate and has similar actions and uses. It is given orally as the hydrochloride, but doses are in terms of the base difenoxin hydrochloride 1.1 mg is equivalent to about 1 mg of difenoxin.

In the treatment of diarrhoea, the usual dose in adults is the equivalent of difenoxin 2 mg initially, followed by 1 mg after each loose stool or every 3 to 4 hours as required, up to a maximum of 8 mg daily.

Preparations of difenoxin usually contain subclinical amounts of atropine sulfate in an attempt to discourage abuse.

Proprietary Preparations

USA: Motofen.

Lidamidine Hydrochloride

Lidamidine HydrochlorideDrug Nomenclature

Synonyms: Lidamidina, hidrocloruro de; WHR-1142A
USAN: Lidamidine Hydrochloride
INN: Lidamidine Hydrochloride [rINNM (en)]
INN: Hidrocloruro de lidamidina [rINNM (es)]
INN: Lidamidine, Chlorhydrate de [rINNM (fr)]
INN: Lidamidini Hydrochloridum [rINNM (la)]
INN: Лидамидина Гидрохлорид [rINNM (ru)]
Chemical name: N-(2,6-Dimethylphenyl)-N’-[imino(methylamino)methyl]urea hydrochloride
Molecular formula: C11H16N4O,HCl =256.7
CAS: 66871-56-5 (lidamidine); 65009-35-0 (lidamidine hydrochloride)

Profile

Lidamidine is an alpha2-adrenergic receptor stimulant used as the hydrochloride for the management of diarrhoea and other gastrointestinal disorders.

Proprietary Preparations

Mexico: Idealid ; Supra.

Racecadotril

Drug Nomenclature

Synonyms: Acetorphan; Racecadotrilo
INN: Racecadotril [rINN (en)]
INN: Racecadotrilo [rINN (es)]
INN: Racécadotril [rINN (fr)]
INN: Racecadotrilum [rINN (la)]
INN: Рацекадотрил [rINN (ru)]
Chemical name: (±)-N-{2-[(Acetylthio)methyl]-1-oxo-3-phenylpropyl}glycine phenylmethyl ester; N-[(R,S)-3-acetylthio-2-benzylpropanoyl]glycine benzyl ester; (±)-N-[α-(Mercaptomethyl)hydrocinnamoyl]glycine benzyl ester acetate
Molecular formula: C21H23NO4S =385.5
CAS: 81110-73-8
ATC code: A07XA04

Pharmacopoeias. In Europe.

European Pharmacopoeia, 6th ed. (Racecadotril). A white or almost white powder. Practically insoluble in water freely soluble in methyl alcohol and in dichloromethane.

Profile

Racecadotril is an enkephalinase inhibitor that inhibits the breakdown of endogenous opioids, thus reducing intestinal secretions. It is given orally in doses of 100 mg three times daily before meals for up to 7 days for the symptomatic management of acute diarrhoea.

The S-form of racecadotril (sinorphan, ecadotril — see Natriuretic Peptides) has been investigated for hypertension and heart failure.

Proprietary Preparations

Brazil: Tiorfan

France: Tiorfan

Germany: Tiorfan

Greece: Hidrasec

Indonesia: Hidrasec

Mexico: Hidrasec

Portugal: Tiorfan

Spain: Tiorfan

Thailand: Hidrasec

Venezuela: Hidrasec.

Smectites

Смектиты
ATC — A07BC05 (diosmectite).
ATC Vet — QA07BC05 (diosmectite).

Profile

Smectites are natural mineral clays composed mainly of aluminium silicates and include aluminium magnesium silicate, bentomte, and Fuller’s earth. They have adsorbent properties and some, such as dioctahedral smectite (diosmectite), have been used in the management of diarrhoea. They are also used as pharmaceutical excipients and in industry.

Preparations

Proprietary Preparations

Czech Republic: Smecta

France: Smecta

Germany: Colina

Greece: Smecta

Hong Kong: Smecta

Hungary: Smecta

Italy: Diosmectal Nodia

Malaysia: Smecta

Poland: Smecta

Russia: Smecta

Singapore: Smecta

Thailand: Smecta.

Multi-ingredient

Belgium: Barexal

Germany: Colina Spezial.

Zaldaride

ZaldarideDrug Nomenclature

Synonyms: CGS-9343B (zaldaride maleate); Zaldarida
INN: Zaldaride [rINN (en)]
INN: Zaldarida [rINN (es)]
INN: Zaldaride [rINN (fr)]
INN: Zaldaridum [rINN (la)]
INN: Зальдарид [rINN (ru)]
Chemical name: (±)-1-{1-[(4-Methyl-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl)methyl]-4-piperidyl}-2-benzimidazolinone
Molecular formula: C26H28N4O2 =428.5
CAS: 109826-26-8 (zaldaride); 109826-27-9 (zaldaride maleate)

Profile

Zaldaride is a calmodulin antagonist that has been investigated as the maleate for the treatment of diarrhoea.

Diarrhoea

Studies in patients with travellers’ diarrhea have indicated that zaldaride in oral doses of 20 mg as the maleate four times daily is an effective antidiarrhoeal. It was somewhat less effective than loperamide when given without a loading dose, but a regimen of 40 mg initially, followed by 20 mg, about every 6 hours was as effective as loperamide 4 mg initially followed by 2 mg after each unformed stool.

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