Galpharm Constipation Relief 5mg Tablets
1 NAME OF THE MEDICINAL PRODUCT
Bisacodyl 5mg Tablets
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Bisacodyl BP 5 mg
Excipient with known effect: Lactose
For the full list of excipients, see section 6.1
3. PHARMACEUTICAL FORM
Yellow, biconvex, enteric coated tablets
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
For short term use for the relief of constipation.
4.2 Posology and method of administration
Posology
FOR CONSTIPATION:
Adults and children over 10 years of age: 1 or 2 tablets to be taken at night.
It is recommended to start with the lowest dose. The dose may be adjusted up to the maximum recommended dose to produce regular stools. The maximum daily dose should not be exceeded.
The elderly:
The usual adult dose is normally appropriate; however, a reduced dose may be required in certain circumstances.
In the management of constipation, once regularity has been restarted dosage should be reduced and can usually be stopped.
It is recommended to take the coated tablets at night to have a bowel movement the following morning. They should be swallowed whole with an adequate amount of fluid.
The coated tablets should not be taken together with products which reduce the acidity of the upper gastrointestinal tract, such as milk, antacids or proton pump inhibitors, in order not to prematurely dissolve the enteric coating
4.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
Contraindicated in patients with intestinal obstruction, ileus and those where a contact laxative is contraindicated.
Contraindicated in patients with acute surgical abdominal conditions such as appendicitis, acute inflammatory bowel diseases and severe abdominal pain associated with nausea and vomiting which may be indicative of the aforementioned severe conditions.
Contraindicated in severe dehydration.
4.4 Special warnings and precautions for use
As with all laxatives, Galpharm Constipation Relief 5mg Tablets should not be taken on a continuous daily basis for more than five days without investigating the cause of constipation.
Prolonged use may precipitate the onset of an atonic, non-functioning colon.
Prolonged and excessive use may lead to fluid and electrolyte imbalance and hypokalaemia.
Intestinal loss of fluids can promote dehydration. Symptoms may include thirst and oliguria. In patients suffering from fluid loss where dehydration may be harmful (e.g. renal insufficiency, elderly patients) bisacodyl should be discontinued and only be restarted under medical supervision.
Laxatives do not help in long-term weight loss.
Dizziness and/or syncope have been reported in patients during defecation, consistent with defecation syncope (or syncope attributable to straining at stool), or with a vasovagal response to abdominal pain which may be related to the constipation that prompted these patients to resort to the use of laxatives.
Patients may experience haematochezia (blood in stool) that is generally mild and self-limiting.
There have been isolated reports of abdominal pain and bloody diarrhoea occurring after taking Bisacodyl. Some cases have been shown to be associated with colonic mucosal ischaemia.
Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase insufficiency and the Lapp lactase deficiency should not take this medicine.
Paediatric population
Bisacodyl should not be taken by children under 10 years without medical advice.
4.5 Interaction with other medicinal products and other forms of interaction
The concomitant use of antacids and milk products may reduce the resistance of the coating of the tablets and result in dyspepsia and gastric irritation.
The concomitant use of diuretics or adreno-corticosteroids may increase the risk of electrolyte imbalance if excessive doses of bisacodyl are taken.
Electrolyte imbalance may lead to increased sensitivity to cardiac glycosides.
4.6 Fertility, pregnancy and lactation
Pregnancy
There are no adequate and well-controlled studies in pregnant women. Long experience has shown no evidence of undesirable or damaging effects during pregnancy.
Breast-feeding
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, Bisacodyl 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.
Fertility
No studies on the effect on human fertility have been conducted.
4.4 Special warnings and precautions for use
As with all laxatives, Bisacodyl 5mg Tablets should not be taken on a continuous daily basis for more than five days without investigating the cause of constipation.
Prolonged use may precipitate the onset of an atonic, non-functioning colon.
Prolonged and excessive use may lead to fluid and electrolyte imbalance and hypokalaemia.
Intestinal loss of fluids can promote dehydration. Symptoms may include thirst and oliguria. In patients suffering from fluid loss where dehydration may be harmful (e.g. renal insufficiency, elderly patients) bisacodyl should be discontinued and only be restarted under medical supervision.
Laxatives do not help in long-term weight loss.
Dizziness and/or syncope have been reported in patients during defecation, consistent with defecation syncope (or syncope attributable to straining at stool), or with a vasovagal response to abdominal pain which may be related to the constipation that prompted these patients to resort to the use of laxatives.
Patients may experience haematochezia (blood in stool) that is generally mild and self-limiting.
There have been isolated reports of abdominal pain and bloody diarrhoea occurring after taking Bisacodyl. Some cases have been shown to be associated with colonic mucosal ischaemia.
Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase insufficiency and the Lapp lactase deficiency should not take this medicine.
Paediatric population
Bisacodyl should not be taken by children under 10 years without medical advice.
4.8 Undesirable effects
The most common 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, <1/100); rare (> 1/10000, <1/1000); very rare (<1/10000).
Not known - incidence cannot be estimated from the available data.
Immune system disorders
Rare: anaphylactic reactions, angio-oedema and other hypersensitivity.
Metabolism and nutrition disorders Rare: dehydration
Nervous system disorders Uncommon: dizziness Rare: syncope
Dizziness and syncope occurring after taking bisacodyl appear to be consistent with a vasovagal response (e.g. abdominal spasm, defaecation).
Gastrointestinal disorders
Uncommon: vomiting, haematochezia (blood in stool), anorectal discomfort Common: Abdominal discomfort, abdominal pain, abdominal cramps, nausea and diarrhoea.
Rare: Colitis including ischaemic colitis.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.
4.9 Overdose
Symptoms
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.
Management
After ingestion of oral forms of bisacodyl 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.
4.7 Effects on ability to drive and use machines
Bisacodyl 5mg Tablets has moderate influence on the ability to drive and use machines.
No studies on the effects of Bisacodyl on the ability to drive and use machines have been performed.
However, patients should be advised that due to a vasovagal response (e.g. to abdominal spasm) they may experience dizziness and / or syncope. If patients experience abdominal spasm they should avoid potentially hazardous tasks such as driving or operating machinery.
5.2 Pharmacokinetic properties
Following either oral or rectal administration, 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. In contrast, following the administration as a suppository, the laxative effect occurred on average approximately 20 minutes post administration; in some cases it occurred 45 minutes after administration. The maximum BHPM-plasma concentrations were achieved 0.5 - 3 hours following the administration as a suppository. 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 and rectal 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. Following the administration as a suppository, an average of 3.1% of the dose was recovered as BHPM glucuronide in the urine. Stool contained large amounts of BHPM (90% of the total excretion) in addition to small amounts of unchanged bisacodyl.
5.3 Preclinical safety data
None stated.
6. PHARMACEUTICAL PARTICULARS
6.1. List of excipients
Lactose, Maize Starch, Light Liquid Paraffin, Magnesium Stearate,
Coating:
Opadry White YS-1-7027 (containing Hypromellose, Titanium Dioxide and Triacetin) and Acryleze Yellow 93052191 (containg Methacrylic Acid Copolymer Type C, Talc, Titanium Dioxide, Triethyl Citrate, Quinoline Yellow, Colloidal Anhydrous Silica, Sodium Bicarbonate, and Sodium Lauryl Sulphate).
6.2 Incompatibilities
None stated.
6.3. Shelf life
Three years
6.4 Special precautions for storage
Do not store above 25oC.
6.5. Nature and contents of container
Standard blister form specification comprising of 20q aluminium foil blister lidding with clear 250q polyvinyl chloride (PVC) / polyvinylidene chloride (PVdC) at 40 grams per square meter forming film, containing 20 tablets.
Standard blister form specification comprising of 20q aluminium foil blister lidding with clear 250q polyvinyl chloride (PVC) / polyvinylidene chloride (PVdC) at 60 grams per square meter forming film, containing 20 tablets.
6.6 Special precautions for disposal
No special requirements for disposal. Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
7 MARKETING AUTHORISATION HOLDER
Galpharm Healthcare Limited
Wrafton
Braunton
Devon
EX33 2DL
United Kingdom
8 MARKETING AUTHORISATION NUMBER(S)
PL 16028/0022
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
26/09/1995 / 28/10/2005
10 DATE OF REVISION OF THE TEXT
24th June 2016
6.5 Nature and contents of container
Standard blister form specification comprising of 20p aluminium foil blister lidding with clear 250p polyvinyl chloride (PVC) / polyvinylidene chloride (PVdC) at 40 grams per square meter forming film, containing 20 tablets.
Standard blister form specification comprising of 20p aluminium foil blister lidding with clear 250p polyvinyl chloride (PVC) / polyvinylidene chloride (PVdC) at 60 grams per square meter forming film, containing 20 tablets.
6.6 Special precautions for disposal
No special requirements for disposal. Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
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9
MARKETING AUTHORISATION HOLDER
Galpharm Healthcare Limited
Wrafton
Braunton
Devon
EX33 2DL
United Kingdom
MARKETING AUTHORISATION NUMBER(S)
PL 16028/0022
DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 26/09/1995 / 28/10/2005