Product Information
Registration Status: ActiveGUTRON TABLET 5mg is approved to be sold in Singapore with effective from 2001-04-28. It is marketed by TAKEDA PHARMACEUTICALS (ASIA PACIFIC) PTE LTD, with the registration number of SIN11500P.
This product contains Midodrine 5mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by Takeda GmbH (Oranienburg plant) in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
An ethanolamine derivative that is an adrenergic alpha agonist. It is used as a vasoconstrictor agent in the treatment of hypotension. [PubChem]
Indication
For the treatment of symptomatic orthostatic hypotension (OH).
Mechanism of Action
Midodrine forms an active metabolite, desglymidodrine, that is an alpha1-agonist, and exerts its actions via activation of the alpha-adrenergic receptors of the arteriolar and venous vasculature, producing an increase in vascular tone and elevation of blood pressure. Desglymidodrine does not stimulate cardiac beta-adrenergic receptors.
Pharmacokinetics
- Absorption
- Rapidly absorbed following oral administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food.
- Distribution
- Metabolism
- Thorough metabolic studies have not been conducted, but it appears that deglycination of midodrine to desglymidodrine takes place in many tissues, and both compounds are metabolized in part by the liver.
- Elimination
Clearance
* Renal cl=385 mL/minute
Toxicity
Symptoms of overdose could include hypertension, piloerection (goosebumps), a sensation of coldness and urinary retention. The single doses that would be associated with symptoms of overdosage or would be potentially life- threatening are unknown. The oral LD50 is approximately 30 to 50 mg/kg in rats, 675 mg/kg in mice, and 125 to 160 mg/kg in dogs. Desglymidodrine is dialyzable.
Active Ingredient/Synonyms
(+-)-2-amino-N-(beta-hydroxy-2,5-dimethoxyphenethyl)acetamide | 1-(2',5'-Dimethoxyphenyl)-2-glycinamidoethanol | 2-Amino-N-(2,5-dimethoxy-beta-hydroxyphenethyl)acetamide | DL-N1-(beta-Hydroxy-2,5-dimethoxyphenethyl)glycinamid | Midodrin | Midodrina | Midodrinum | Midodrine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.