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Olsalazine Sodium

(British Approved Name Modified, US Adopted Name, rINNM)

Drug Nomenclature

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

Olsalazine SodiumSynonyms: Azodisal Sodium; CI Mordant Yellow 5; CJ-91B; Colour Index No. 14130; Olsalatsiininatrium; Olsalazin disodná sůl; Olsalazina sódica; Olsalazinnatrium; Olsalazino natrio druska; Olsalazinum Dinatricum; Olsalazinum Natricum; Olszalazin-nátrium; Sodium Azodisalicylate
BAN: Olsalazine Sodium [BANM]
USAN: Olsalazine Sodium
INN: Olsalazine Sodium [rINNM (en)]
INN: Olsalazina sódica [rINNM (es)]
INN: Olsalazine Sodique [rINNM (fr)]
INN: Natrii Olsalazinum [rINNM (la)]
INN: Натрий Ольсалазин [rINNM (ru)]
Chemical name: Disodium 5,5´-azodisalicylate
Molecular formula: C14H8N2Na2O6 =346.2
CAS: 6054-98-4
ATC code: A07EC03
Read code: y01RB

Pharmacopoeias. In Europe.

European Pharmacopoeia, 6th ed. (Olsalazine Sodium). A yellow, fine, crystalline powder it exhibits polymorphism. Sparingly soluble in water soluble in dimethyl sulfoxide very slightly soluble in methyl alcohol.

Adverse Effects and Precautions

As for Mesalazine. The most common adverse effects associated with olsalazine sodium are diarrhoea, arthralgia, and skin rashes. Diarrhoea may be watery in some patients it may resolve with dosage reduction but can be severe enough to require withdrawal of treatment. Diarrhoea is less likely if the drug is taken after meals. There have been a few reports of blood dyscrasias. If a blood dyscrasia is suspected treatment should be stopped immediately and a blood count performed. Patients or their carers should be told how to recognise signs of haematotoxicity and should be advised to seek immediate medical attention if symptoms such as fever, sore throat, mouth ulcers, bruising, or bleeding develop.

Incidence of adverse effects. In an open study of olsalazine 1 g daily by mouth involving 160 patients with active ulcerative colitis and a history of sulfasalazine intolerance, 103 (64.4%) patients had no adverse effects 29 patients reported only minor adverse effects: gastrointestinal disturbances in 22 patients, transient skin rash in 3, and headache, increased salivation, cough, and irritability each in one patient. The most common adverse effect was frequent loose stools which affected 25 patients, 20 of whom had to stop treatment. This adverse effect occurred early in treatment, within 10 hours of the first dose in 13 patients. Severe diarrhoea was more frequent in patients with widespread disease, but the incidence of diarrhoea did not correlate with disease severity.

A subsequent study in healthy subjects has shown that olsalazine has a significant inhibitory effect on water and electrolyte absorption in the small intestine, which may account, at least in part, for the induction of diarrhoea. Patients with extensive colitis have reduced colonic absorptive function and may be less able to assimilate the increased colonic inflow volumes.

Breast feeding. A study involving a 39-year-old woman with Crohn’s disease found that olsalazine did not appear to present a clinically significant risk to the breast-fed infant. Olsalazine was undetectable in the breast milk for 48 hours after a single oral 500-mg dose, and although small amounts of the metabolite acetylated 5-aminosalicylic acid were detected in breast milk the infant showed no adverse effects during the 3 weeks afterwards in which the mother continued taking olsalazine.

Pharmacokinetics

Very little of an oral dose of olsalazine is absorbed via the upper gastrointestinal tract, and almost the entire dose reaches its site of action in the colon intact. It is broken down by the colonic bacterial flora into 2 molecules of 5-aminosalicylic acid (mesalazine). Some mesalazine is absorbed and acetylated but systemic concentrations of mesalazine and its metabolite are lower than after comparable oral doses of mesalazine, perhaps because there is less release of mesalazine in the small intestine, where absorption is better. Mesalazine concentrations in the colon after a dose of olsalazine are stated to be about 1000 times greater than systemic concentrations.

The small amounts (1 to 2% of the dose or less) of intact olsalazine that are absorbed are excreted mainly in urine the elimination half-life after an intravenous dose has been calculated at about 1 hour. Some olsalazine is metabolised by sulfate conjugation in the liver: the elimination half-life of the metabolite is reported to be about 7 days.

Uses and Administration

Olsalazine consists of two molecules of mesalazine linked with an azo bond. It is activated in the colon where the active mesalazine is released. It is used as the sodium salt in the management of acute mild ulcerative colitis and for the maintenance of remission (see Inflammatory Bowel Disease). The usual initial dose of olsalazine sodium is 1 g by mouth daily in divided doses and this is gradually increased, if necessary, over one week, to a maximum dose of 3 g daily. The usual dose for the maintenance of remission is 500 mg twice daily. Doses should be taken after meals and a single dose should not exceed 1 g. Although not licensed for use in children, the BNFC includes a dose for children aged 2 years and over the adult dose may be given for management of an acute attack of mild ulcerative colitis, and a dose of 250 to 500 mg twice daily may be used for maintenance.

Proprietary Preparations

Argentina: Dipentum

Australia:: Dipentum

Austria: Dipentum

Canada: Dipentum

Chile: Dipentum

Denmark: Dipentum

Finland: Dipentum

France: Dipentum

Germany: Dipentum

Greece: Dipentum

Hong Kong: Dipentum

Hungary: Dipentum

Ireland: Dipentum

Israel: Dipentum

Italy: Dipentum

The Netherlands: Dipentum

Norway: Dipentum

New Zealand: Dipentum

South Africa: Dipentum

Spain: Rasal

Sweden: Dipentum

Switzerland: Dipentum

Turkey: Dipentum

UK: Dipentum

USA: Dipentum

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