Description of the medicine: Clophelin (Clophelinum)
Clophelinum. 2- (2, 6-Dichlorophenylamino) -imidazoline hydrochloride.
Synonyms: Hemiton, Catapresane, Chlofazolin, Atensina, Bapresan, Capresin, Catapres, Catapresan, Chlophazolin, Chlornidinum, Clonidini hydrochloridum, Clonidin hydrochloride, Clonilon, Clonisin, Clonidine, Haemiton, Hemiton, Hyposyn, Ipotensinum, Namestin, Normopresan, Prescatan and others.
White crystalline powder. It is soluble in water, it is difficult - in alcohol.
Clopheline is an antihypertensive agent whose action is associated with a characteristic effect on the neurogenic regulation of vascular tone.
According to its chemical structure, it has elements of similarity to naphthysine (see) and phentolamine (see), respectively, adrenomimetic and a-adrenoblocking agents. Like naphthyzine, clonidine stimulates peripheral a 1, -adrenoceptors and has a short pressor effect. But, penetrating through the blood-brain barrier, it stimulates a 2-adrenoreceptors of the vasomotor centers, reduces the flow of sympathetic pulses from the CNS, and reduces the release of norepinephrine from the nerve endings, thus providing a certain sympatholytic effect.
In connection with this, the main manifestation of the action of clonidine is the hypotensive effect. Persistent hypotensive action may be preceded by a short-term hypertensive effect (due to the excitation of peripheral a-adrenoreceptors). The hypertensive phase (lasting several minutes) is usually observed only with a rapid intravenous injection and is absent in other ways of administration or with a slow introduction into the vein. The hypotensive effect usually develops 1 to 2 hours after ingestion and continues after a single dose of 6 to 8 hours.
The hypotensive effect of clonidine is accompanied by a decrease in cardiac output and a decrease in the peripheral resistance of the vessels, including the vessels of the kidneys.
Clopheline also causes a decrease in intraocular pressure, associated with a decrease in secretion and an improvement in the outflow of aqueous humor.
The drug has a pronounced sedative, as well as an analgesic effect.
An important feature of clonidine is also its ability to reduce (and remove) somatovegetative manifestations of opioid and alcohol abstinence. The sense of fear decreases, cardiovascular and other disorders gradually go away. It is believed that these phenomena are largely due to a decrease in central adrenergic activity, occurring when blockade with clonidine a 2-adrenoreceptors.
Clopheline is widely used as an antihypertensive drug for various forms of hypertension and for the management of hypertensive crises, and in ophthalmic practice for conservative treatment of patients with primary open-angle glaucoma.
The drug is effective in very small doses. Doses should be selected strictly individually. When administered orally as an antihypertensive agent is prescribed, usually starting from 0.075 mg (0.000075 g) 2 to 4 times a day.