Diastop

Country: New Zealand

Language: English

Source: Medsafe (Medicines Safety Authority)

Active ingredient:

Atropine sulfate monohydrate 0.025mg; Diphenoxylate hydrochloride 2.5mg;  

Available from:

Viatris Limited

INN (International Name):

Atropine sulfate monohydrate 0.025 mg

Pharmaceutical form:

Tablet

Composition:

Active: Atropine sulfate monohydrate 0.025mg Diphenoxylate hydrochloride 2.5mg   Excipient: Colloidal silicon dioxide Magnesium stearate Microcrystalline cellulose Pregelatinised maize starch

Units in package:

Blister pack, 20 tablets

Class:

Pharmacy only

Prescription type:

Pharmacy only

Manufactured by:

Boehringer Ingelheim Pharma GmbH & Co KG

Therapeutic indications:

DIASTOP is indicated as an adjunctive therapy to proper rehydration in acute and chronic diarrhoea; after colostomy or ileostomy for control of stool formation; and for relief of symptoms in ulcerative colitis.

Product summary:

Package - Contents - Shelf Life: Blister pack, - 20 tablets - 24 months from date of manufacture stored at or below 25°C - Blister pack, - 100 tablets - 24 months from date of manufacture stored at or below 25°C

Authorization date:

1979-04-05

Summary of Product characteristics

NEW ZEALAND DATA SHEET 
DIASTOP 
_DIPHENOXYLATE HYDROCHLORIDE 2.5 MG AND _
_ATROPINE SULPHATE 0.025 MG TABLET _
_ _
PRESENTATION 
White biconvex tablet, 7/32” in diameter and blank on
both sides.  Each DIASTOP tablet contains 2.5 mg of 
diphenoxylate hydrochloride and 0.025 mg of atropine sulphate. 
USES 
_ACTIONS _
Diphenoxylate is an opiate derivative. The antidiarrhoeal effects
of opioids may be due to their effects on the 
opiate receptors controlling smooth muscle contraction in the small
intestine and colon. The resulting 
increase in tone and segmenting activity increases the
resistance to flow of luminal contents. It is essentially 
devoid of “morphine type subjective effects” at therapeutic
doses. 
Atropine is a non-selective muscarinic antagonist. It is included
in the formulation as an anti-abusing agent 
contributing to the safe use of the product.  The dose of
atropine sulphate contained in each tablet is sub-
therapeutic therefore a pharmaceutical effect due to
atropine should not be detected taken at normal 
therapeutic doses.  
_PHARMACOKINETICS _
_DIPHENOXYLATE HYDROCHLORIDE  _
Diphenoxylate is rapidly absorbed reaching peak blood levels in
about two hours. Its relatively short plasma 
half-life (about 2.5 hours) and large plasma clearance suggests its
rapid biotransformation. Metabolism is 
principally in the liver. The major
metabolic pathway of diphenoxylate in man is the hydrolysis of
the ester 
group to give diphenoxylic acid - a pharmacologically active
metabolite. Diphenoxylate metabolites probably 
undergo enterohepatic circulation. Diphenoxylic acid has a
greater average peak plasma concentration, and 
a shorter time to maximum plasma concentration, than diphenoxylate.
The AUC is about five times greater 
for diphenoxylic acid than for diphenoxylate, and may
reflect enhanced bioavailability of diphenoxylic acid. 
Onset of pharmacological effect is 45 to 60 minutes, and
dura