For the use of registered Medical Practitioner or Laboratory or Pharmacy
COLSTATE
(Mebeverine, Sulpiride and Simethicone Tablets)
COMPOSITION
Each film coated tablet contains:
Mebeverine Hydrochloride BP 135 mg
Sulpiride BP 25 mg
Simethicone USP 180 mg
Excipients q.s.
PHARMACEUTICAL FORM
Tablet
PHARMACOLOGICAL PROPERTIES
Pharmacodynamic:
Mebeverine Hydrochloride
Pharmacotherapeutic group: Synthetic anticholinergics, esters with tertiary amino group
ATC code: A03A A04
Mechanism of action: Mebeverine is a musculotropic antispasmodic with a direct action on the smooth muscle of the gastrointestinal tract, relieving spasm without affecting normal gut motility. Since the autonomic nervous system is not involved in this mechanism of action, typical systemic anticholinergic side-effects are absent.
Sulpiride
Pharmacotherapeutic group: Psycholeptics; Benzamides
ATC code: N05AL01
Mechanism of action: Sulpiride is a member of the group of substituted benzamides, which are structurally distinct from the phenothiazines, butyrophenones and thioxanthenes.
Simethicone
Mechanism of action: Simeticone is an inert surface-active agent with anti-foaming properties thereby potentially relieving gas related symptoms associated with diarrhoea.
Pharmacokinetics:
Mebeverine Hydrochloride
Absorption: Mebeverine is rapidly and completely absorbed after oral administration of tablets. The modified release formulation permits a twice daily dosing scheme.
Distribution: No significant accumulation occurs after multiple doses.
Biotransformation: Mebeverine hydrochloride is mainly metabolised by esterases, initially splitting the ester bonds into veratric acid and mebeverine alcohol. The main metabolite in plasma is DMAC (Demethylated carboxylic acid). The steady state elimination half-life of DMAC is 5.77h. During multiple dosing (200 mg b.i.d.) the Cmax of DMAC is 804 ng/ml and tmax is about 3 hrs. The relative bioavailability of the modified release capsule appears to be optimal with a mean ratio of 97%.
Elimination: Mebeverine is not excreted as such, but metabolised completely; the metabolites are excreted nearly completely. Veratric acid is excreted into the urine; mebeverine alcohol is also excreted into the urine, partly as the corresponding carboxylic acid (MAC) and partly as the demethylated carboxylic acid (DMAC).
Paediatric population: No pharmacokinetic studies have been performed in children under 10 years old.
Sulpiride: Peak sulpiride serum levels are reached 3 – 6 hours after an oral dose. The plasma half-life in man is approximately 8 hours. Approximately 40% sulpiride is bound to plasma proteins. 95% of the compound is excreted in the urine and faeces as unchanged sulpiride.
Simethicone: The simeticone component is not absorbed.
INDICATION
Mebeverine Hydrochloride: Irritable colon syndrome in it’s primary porm, or associated with lesions of G.I Tract.
Sulpiride: The treatment of acute and chronic schizophrenia, depression, tourette’s disorder, alcoholic addition, duodenal ulcer, inadequate lactation.
Simethicone: Simethicone is primarily indicated in conditions like esophagitis, gastric bloating, gastrocardiac sysndrome, irritable bowel syndrome, itchy dermatitis, meteorism, oesophagitis, peptic ulcer, skin irritations.
DOSAGE AND ADMINISTRATION
One tablet 3 times daily. When the desired effect has been obtained the dosage may be reduced by the physician.
CONTRAINDICATIONS
Hypersensitivity to the active substance or to any of the excipients.
Pregnancy and Breast feeding.
ADVERSE EFFECTS
Some of the common side effects of Mebeverine, Sulpiride and Simethicone Tablets include diarrhea, stomach pain, dryness in mouth, headache, dizziness, flatulence, weakness and head ache.
WARNINGS AND PRECAUTIONS
Mebeverine Hydrochloride: Paediatrics, contraindicated in age under 2 year, preganancy and lactation.
Sulpiride: The treatment of acute and chronic schizophrenia, depression, tourette’s disorder, alcoholic addition, duodenal ulcer, inadequate lactation.
Simethicone: Simethicone is primarily indicated in conditions like esophagitis, gastric bloating, gastro cardiac syndrome, irritable bowel syndrome, itchy dermatitis, meteorism, oesophagitis, peptic ulcer, skin irritations.
MODE OF ADMINISTRATION
For Oral Use
MODE OF SELLING
Prescription Only Medicine
SHELF LIFE
36 months from the date of manufacturing.
STORAGE CONDITIONS
Store at a temperature not exceeding 300C. Protect from light and moisture.
Keep out of the reach of children.
PRESENTATION
30 Tablets packed in an Alu/Alu blister and packed in a carton with package insert.
The Holder of Trademark and Marketing Authorization is Sterlist Pharma LTD, England.
Manufactured exclusively for Sterlist Pharma LTD, England.