Тертатолол

Description

Tertatolol is a pharmaceutical substance, a non-selective beta-blocker from a series of thiochroman derivatives (2H-1-benzothiopyran). According to the anatomical-therapeutic-chemical classification, it belongs to group C - drugs for the treatment of diseases of the cardiovascular system. The molecule is built according to the general scheme of beta blockers: the thiochroman core is connected through an oxypropanol bridge to a tert-butylamino group. The commercial substance is a racemate, hence the designations dl-Tertatolol and (±)-Tertatolol.

Basic Attributes

• CAS No: 83688-84-0
• Chemical formula: C16H25NO2S
• Molecular weight: 295.44
• Exact weight: 295.44
• EU number: 280-519-9
• ATC code: C - cardiovascular system
• HS code: 2932999099
• PSA Specifications: 66.79000
• XLogP3: 3.24360

Physico-chemical characteristics

• Density: 1.112 ± 0.06 g/cm3
• Melting point: 70–72 °C
• Boiling point: 465.0 ± 45.0 °C (predicted value)
• pKa: 13.84 ± 0.20

Pharmacological group and action

A non-selective beta-adrenergic receptor antagonist without intrinsic sympathomimetic activity, additionally exhibits the properties of an antagonist of serotonin 5-HT1A receptors. A distinctive feature among beta blockers is their vasodilating effect at the level of the renal microcirculation. The half-life from plasma is about 3 hours, while the beta-blocking effect lasts longer than the presence of the substance in the blood, which allows the drug to be used once a day.

Scope of application

• active ingredient of antihypertensive drugs; trade names Artex, Artexal, Prenalex
• standard regimen - 5 mg once a day; if pressure control is insufficient, the dose is increased or a potassium-sparing diuretic is added
• pharmaceutical standard and research object in beta-adrenergic and serotonergic pharmacology

In a long-term observation program involving 2338 patients with mild and moderate arterial hypertension, normalization of blood pressure within a year was achieved in 88.8% - 66.1% with monotherapy and 22.7% with a two-component regimen. Discontinuation due to adverse effects was required in 6.5% of cases.

Storage and transportation conditions

The substance is stored in a tightly closed container, in a dry room, protected from light, at a temperature no higher than room temperature. There are no transport restrictions for classes of dangerous goods in the product card. Handling is in accordance with the rules for working with pharmaceutical substances: protection from dust, control of cross-contamination, batch accounting.