COLPERMIN CAPSULE 187MG FOR ORAL USE

Product Information

Registration Status: Active

COLPERMIN CAPSULE 187MG is approved to be sold in Singapore with effective from 2004-04-11. It is marketed by WELLCHEM PHARMACEUTICALS PTE LTD, with the registration number of SIN13034P.

This product contains Peppermint Oil 187mg in the form of CAPSULE, ENTERIC-COATED. It is approved for ORAL use.

This product is manufactured by SwissCo Services AG Tillotts Pharma AG in SWITZERLAND.

It is an Over-the-counter Medicine that can be freely obtained from any retailer

Description

Extracted from the stem, leaves, and flowers of _Mentha piperita_ L. plant, peppermint oil (Mentha piperita) is a popular essential oil used in aromatherapy for both external and internal use. Mentha piperita is a hybrid of spearmint (Mentha spicata) and water mint (Mentha aquatica) [A33065]. Medicinal use of herbal ingredients such as peppermint oil has a long history of treating digestive disorders and upper respiratory symptoms and cough [A33055]. There are various over-the-counter and commercial uses of peppermint oil due to its carminative, cholagogue, antibacterial, secretolytic, and choleretic actions [A33056]. Peppermint oil contains pulegone, which is a naturally-occurring pesticide [F77]. Other active constituents of peppermint oil include [DB00825], menthone, cineol, and several other volatile oils [A33055, A33056]. Peppermint oil is used as a flavouring agent in foods and fragrance in hygienic or cosmetic products, and as an anti-itch and cooling agent in topical pharmaceutical products. It is also an active ingredient in topical analgesics for the relief of joint and muscle pain. Peppermint oil can be applied topically to temporarily relieve tension-type headache. The use of peppermint oil in the management of irritable bowel syndrome (IBS) has been investigated in many clinical studies due to its relaxing effects on smooth muscle; however the evidence supporting this use is unclear. Due to its effectiveness in relaxing GI smooth muscle but ability to induce gastroesophageal reflux, enteric-coated formulations of peppermint oil has been established which bypass the upper GI tract unmetabolized, thereby facilitating its effect in the lower GI tract without effects in the upper tract [A33055]. Peppermint oil is safe and well-tolerated at commonly recommended dosage [A33055].

Indication

Indicated for the over-the-counter use for: -the symptomatic relief of minor spasms of the gastrointestinal tract, flatulence and abdominal pain, especially in patients with irritable bowel syndrome. -the temporary relief of itching associated with insect bites, eczema, minor burn, sunburn, minor skin irritations, minor cuts, scrapes, atopic dermatitis and other skin disorders. -the temporary symptomatic relief of mild joint and muscle pain as a local topical analgesic. -the temporary relief of tension-type headache.

Mechanism of Action

Dose-dependent antispasmodic effect of peppermint oil is largely mediated by its menthol constituent [A33056]. It is proposed that peppermint oil relaxes gastrointestinal smooth muscle and attenuates contractile responses by reducing the influx of extracellular calcium ions. In rabbit jejunum smooth muscle cells investigated via whole cell clamp configuration technique, peppermint oil was shown to inhibit the potential-dependent calcium currents in a concentration-dependent manner [A33056]. Both a reduction in peak current amplitude and an increase in the rate of current decay were observed, indicating that the pharmacological activity peppermint oil resembles that of dihydropyridine calcium antagonists [A33056]. In a rat small intestine study, peppermint oil in the intestinal lumen inhibited enterocyte glucose uptake via a direct action on the brush border membrane and inhibited intestinal secretion [A33056]. There is also evidence that menthol is an antagonist of L-type Ca2+ channels via interacting with dihydropyridine binding sites and blocks the currents of low-voltage-activated calcium channels [A33056]. Peppermint oil may facilitate hair growth by promoting the conservation of vascularization of hair dermal papilla, which may contribute to the induction of early anagen stage of active growth phase of hair follicles [A33044].

Pharmacokinetics

Absorption: After oral administration, peppermint is rapidly absorbed [A33056]. Menthol is highly fat-soluble therefore rapidly absorbed from the proximal gut [A33059].
Distribution: No pharmacokinetic data available.
Metabolism: The predominant biliary metabolite of peppermint oil is menthol glucuronide, which undergoes enterohepatic circulation [A33056]. The urinary metabolites are products of hydroxylation at the C-7 methyl group at C-8 and C-9 of the isopropyl moiety, forming a series of mono- and dihydroxymenthols and carboxylic acids, some of which are excreted in part as glucuronic acid conjugates [A33056].
Elimination

Clearance

No pharmacokinetic data available.

Toxicity

Oral LD50 value in rat is 2426 mg/kg [MSDS]. In fasted mice, the LD50 following oral administration was 2410 mg/kg [F77]. Higher doses of peppermint oil has the potential to induce menstruation, bronchospasm, tongue spasms, and, possibly, respiratory arrest [A33055] in addition to potential hepatotoxicity and nephrotoxicity [A33065]. Overdose may cause severe gastrointestinal symptoms, diarrhoea, rectal ulceration, epileptic convulsions, loss of consciousness, apnoea, nausea, disturbances in cardiac rhythms, ataxia and other CNS problems, probably due to the presence of menthol [F78]. In the event of overdose, the stomach should be emptied by gastric lavage. Observation should be carried out with symptomatic treatment if necessary [F78]. A near fatal case of high dose peppermint oil ingestion was reported, the overdose was characterized by comatose and reduced heart rate [A33065].

Active Ingredient/Synonyms

Source of information: Drugbank (External Link). Last updated on: 3^rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.