Each Enteric-coated tablet contains
Bisacodyl B.P. 5 mg
Short term relief of constipation.
Constipation, either chronic or of recent onset, whenever a stimulant laxative is required. Bowel clearance before surgery or radiological investigation. Replacement of the evacuant enema in all its indications.
Bisacodyl is rapidly hydrolyzed to the active principle bis(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), mainly by esterases of the enteric mucosa. Administration as an enteric coated tablet was found to result in maximum BHPM plasma concentrations between 4 – 10 hours post administration whereas the laxative effect occurred between 6 – 12 hours post administration. Hence, the laxative effect of bisacodyl does not correlate with the plasma level of BHPM instead, BHPM acts locally in the lower part of the intestine and there is no relationship between the laxative effect and plasma levels of the active moiety. For this reason bisacodyl coated tablets are formulated to be resistant to gastric and small intestinal juice. This results in a main release of the drug in the colon, which is the desired site of action.
After oral administration, only small amounts of the drug are absorbed and are almost completely conjugated in the intestinal wall and the liver to form the inactive BHPM glucuronide. The plasma elimination half-life of BHPM glucuronide was estimated to be approximately 16.5 hours. Following the administration of bisacodyl coated tablets, an average of 51.8% of the dose was recovered in the faeces as free BHPM and an average of 10.5% of the dose was recovered in the urine as BHPM glucuronide.
Bisacodyl is a locally acting laxative from the diphenylmethane derivative group having a dual action. As a contact laxative, for which also antiresorptive hydragogue effects have been described, bisacodyl stimulates after hydrolysis in the large intestine, the mucosa of both the large intestine and of the rectum. Stimulation of the mucosa of the large intestine results in colonic peristalsis with promotion of accumulation of water, and consequently electrolytes, in the colonic lumen. This results in a stimulation of defecation, reduction of transit time and softening of the stool. Stimulation of the rectum causes increased motility and a feeling of rectal fullness. The rectal effect may help to restore the “call to stool” although its clinical relevance remains to be established.
PREGNANCY AND LACTATION
There are no adequate and well-controlled studies in pregnant women. Long experience has shown no evidence of undesirable or damaging effects during pregnancy. Clinical data show that neither the active moiety of bisacodyl (BHPM or bis-(p-hydroxyphenyl)-pyridyl-2-methane) nor its glucuronides are excreted into the milk of healthy lactating females. Nevertheless, as with all medicines, Belax should not be taken in pregnancy, especially the first trimester, and during breast feeding unless the expected benefit is thought to outweigh any possible risk and only on medical advice. No studies on the effect on human fertility have been conducted.
The most commonly reported adverse reactions during treatment are abdominal pain and diarrhoea. Adverse events have been ranked under headings of frequency using the following convention: Very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/1000); rare (≥1/10000, <1/1000); very rare (<1/10000).
Immune system disorders
Rare: anaphylactic reactions, angioedema, hypersensitivity.
Metabolism and nutrition disorders
Nervous system disorders
Dizziness and syncope occurring after taking bisacodyl appear to be consistent with a vasovagal response (e.g. to abdominal spasm, defaecation).
Uncommon: haematochezia (blood in stool), vomiting, abdominal discomfort, anorectal discomfort.
Common: abdominal cramps, abdominal pain, diarrhoea and nausea.
If high doses are taken watery stools (diarrhoea), abdominal cramps and a clinically significant loss of fluid, potassium and other electrolytes can occur. Laxatives when taken in chronic overdose may cause chronic diarrhoea, abdominal pain, hypokalaemia, secondary hyperaldosteronism and renal calculi. Renal tubular damage, metabolic alkalosis and muscle weakness secondary to hypokalaemia have also been described in association with chronic laxative abuse.
After ingestion of oral forms of BELAX, absorption can be minimised or prevented by inducing vomiting or gastric lavage. Replacement of fluids and correction of electrolyte imbalance may be required. This is especially important in the elderly and the young. Administration of antispasmodics may be of value.
Store below 30oC.
Protect from light, heat and moisture.
Keep all medicines out of the reach of children.
Belax 5mg tablets: Pack of 10 x 10’s tablets.
ROCK PHARMACEUTICAL LABORATORIES (PVT) LTD.
134-B & 135-B Nowshera Industrial Estate
Sunlight Links Pharm Ltd.
135, Brono Way, Ebute-Metta