국가: 남아프리카
언어: 영어
출처: South African Health Products Regulatory Authority (SAHPRA)
Schering
PHYSIOTENS 0,2 Film-coated tablets PHYSIOTENS 0,3 Film-coated tablets PHYSIOTENS 0,4 Film-coated tablets SCHEDULING STATUS: S3 PROPRIETARY NAME (and dosage form): PHYSIOTENS 0,2 Film-coated tablets PHYSIOTENS 0,3 Film-coated tablets PHYSIOTENS 0,4 Film-coated tablets COMPOSITION Each film-coated tablet contains 0,2, 0,3 or 0,4 mg moxonidine PHARMACOLOGICAL CLASSIFICATION A. 7.1.3 Other hypotensives. PHARMACOLOGICAL ACTION Pharmacodynamic properties In different animal models moxonidine has been shown to have antihypertensive effects. Available experimental data suggest that the site of the antihypertensive action of moxonidine is the central nervous system. Within the brainstem, moxonidine has been shown to selectively interact with I 1 -imidazoline receptors. These imidazoline-sensitive receptors are concentrated in rostral ventrolateral medulla, an area critical to the central control of the peripheral sympathetic nervous system. The net effect of this interaction with the I 1 -imidazoline receptors appears to result in a reduced activity of sympathetic nerves (demonstrated for cardiac, splanchnic and renal sympathetic nerves). Moxonidine exhibits only low affinity to central alpha 2 -adrenoceptors. In humans moxonidine leads to a reduction of systemic vascular resistance and consequently in arterial blood pressure. Pharmacokinetic properties Approximately 90% of an oral dose of moxonidine is absorbed; it is not subject to first-pass metabolism and its bioavailability is 88%. Food intake does not interfere with moxonidine. Moxonidine is 10 to 20% metabolised, mainly to 4,5-dehydromoxonidine and to a guanidine derivative by opening of the imidazoline ring. The hypotensive effect of 4,5-dehydromoxonidine is only 1/10, and that of the guanidine derivative is less than 1/100 of that of moxonidine. The 전체 문서 읽기