Buy Mebeverine (Colofac, Colospa) online

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Category: Antispasmodic; smooth muscle relaxant.

Mebeverine has a direct non-specific relaxant effect on vascular, cardiac, and other smooth muscle. Studies indicate that the spasmolytic activity of mebeverine is not restricted to one particular system, but the compound possesses a polyvalent spasmolytic action in which at least three types of mechanisms are involved:

  • a direct musculotropic action involving calcium ion exchange and stabilization of excitable membranes;
  • a competitive antimuscarinic activity of about 0.05-0.1 times that of atropine;
  • a local anaesthetic activity together with potentiation of sympathetic inhibitory influences due to blockade of noradrenaline uptake into sympathetic nerve endings.

    In in vitro studies mebeverine hydrochloride has be en shown to have a papaverine-like spasmolytic effect on the smooth muscle of the ileum, uterus and the gall bladder. It possesses a strong local anaesthetic activity.

    When tested in vivo in various species, mebeverine hydrochloride was found to be three to five times more powerful than papaverine in blocking spasm of smooth muscle and in relieving the carbachol-induced spasm of the sphincter of Oddi in rabbits, mebeverine hydrochloride proved to be twenty times more active than papaverine. In vivo studies also demonstrate that mebeverine has only minor effects on normal intestinal peristalsis but possesses spasmolytic activity when hypermotility is induced. The spasmolytic activity is found in all parts of the gastrointestinal tract and in some experimen ts has been found to be more active on colonic smooth muscle.

    Studies with mebeverine hydrochloride 100 mg tablets indicate that mebeverine is free of central anticholinergic effects, and practically free of peripheral effects with an activity of less than 0.001 times that of atropine. Colofac (Mebeverine) does not show central depressant or analgesic effects, and only in high doses are some central stimulating effects observed. No ganglion blocking or interference with neuromuscular transmission occurs.

    Mebeverine injected intravenously in animals produces transient cardiac arrhythmias, bradycardia and ECG changes.


    Following oral administration of 3H and 14C labelled mebeverine hydrochloride in man, absorption was followed by the appearance in the plasma of veratric acid and an oxidised metabolite of the mebeverine alcohol moiety of the drug, mebeverinic acid. Thus the primary metabolic step in mebeverine degradation is hydrolysis of the ester function. Maximum plasma radioactivity levels were found 1-3 hours after dosing. Binding of mebeverine to human serum albumin was 75%. The major route of excretion of the metabolites is via the urine (95%) and the peak rate of excretion usually occurs within two hours. Virtually 98% urinary recovery of the conjugated and unconjugated metabolites was observed after a period of 24 hours. No unchanged mebeverine was excreted with the urine.

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