Clonidine (clophelinum)
KLOFELIN (Clophelinum). 2 - (2, 6-Dihlorfenilamino) - imidazoline hydrochloride.
Synonyms : Gemiton, Katapresan, Hlofazolin, Atensina, Bapresan, Capresin, Catapres, Catapresan, Chlophazolin, Chlornidinum, Clonidini hydrochloridum, Clonidin hydrochlorid, Clonilon, Clonisin, Clonidine, Haemiton, Hemiton, Hyposyn, Ipotensinum, Namestin, Normopresan, Prescatan and others.
The white crystalline powder. Mg in the water, it is difficult to alcohol.
Clonidine is antihypertensive funds, which is linked to a characteristic of neurogenic influence of the regulation of vascular tone.
On chemical structure, it has similarities with naftizinom (see) and fentolaminom (see), the adrenomimeticheskim and a-adrenoblokiruyuschimi means. Like naftizinu Hydrochloride stimulated peripheral to a 1-adrenoretseptory pressornoe and provides short-term impact. But, penetrating through the blood-brain barrier, it stimulates a 2-adrenoretseptory sosudodvigatelnyh centers, reduces the flow sympathetic impulses from the central nervous system and reduces noradrenalina release of nerve endings, thus offering some simpatoliticheskoe effect.
Therefore, the main manifestation of klofelina an anti-hypertensive effect. Persistent anti-hypertensive action may be preceded by short-hypertensive effect (by instituting a peripheral-adrenoreceptor). Hypertensive phase (continued a few minutes) are usually seen only at high intravenously, and not in other ways or in a slow introduction in the vein. Anti-hypertensive effect usually develops in 1 to 2 h after administration of the drug inside and continued after a single reception 6 to 8 h.
Anti-hypertensive effect klofelina accompanied by a decrease in cardiac ejection and reduced peripheral vascular resistance, including vascular kidney.
Clonidine is also lowering inner pressure due to declining secretions and improve moisture retention watery.
The drug has expressed sedative and analgesic effects.
Klofelina An important feature is its ability to reduce (and remove) somatovegetativnye of opiate and alcohol withdrawal symptoms. Falling fear is gradually undergoing cardiovascular and other disorders. I believe that these phenomena are largely attributable to lower central adrenergicheskoy activity in the coming blockade klofelinom a 2-adrenoreceptor.
Clonidine is widely used as an antihypertensive in various forms of hypertension and edema PNDS crises, and in ophthalmic practice for conservative treatment of primary open-angle.
The drug is effective in very small doses. Doses should select a strictly individual. When administered as a means of antihypertensive appointed, usually beginning with 0,075 mg (0.000075 g), 2 - 4 times a day. If the anti-hypertensive effect is not sufficient to increase the dose every single 1 - 2 days at 0.0375 mg (1 / 2 tablet containing 0.075 mg) to 0.15 - 0.3 mg per admission, up to 3 to 4 times a day .
DSA dose usually 0.3 - 0.45 mg, sometimes 1, 2, 1, 5 mg. При недостаточной эффективности клофелина в дозе 0,45 - 0,6 мг в сутки, целесообразно дополнительно назначать салуретики, резерпин, метилдофу, октадин или другие гипотензивные препараты.
Patients who are middle-aged and older, particularly in the brain vascular sclerosis manifestations possible increased sensitivity to a drug, so they are treated with a dose of 0.0375 mg or half-tablet containing 0.075 mg.
The duration of treatment ranged from 6 weeks to 12 months or more.
In hypertensive crises and high pressure when receiving pills does not make an impact Hydrochloride designate intramuscularly, subcutaneously or intravenously. Intramuscularly or subcutaneously enter .5 1, 5 ml of 0.01% solution (0.05 - 0.15 mg). For intravenous grow 0.5 to 1, 5 ml of 0.01% solution klofelina 10-20 ml isotonic sodium chloride solution and impose slowly for 3 to 5 minutes. Anti-hypertensive effect of the introduction of non-manifested through 3 - 5 minutes, reaching a peak after 15 - 20 minutes and remained 4 - 8 hours Severe cases can be administered parenteral solution klofelina 3 to 4 times a day (in-patient). While injecting, and over 1, 5, 2 h after, the patient must be in a position lying (to avoid orthostatic events).
While the application klofelina with heart failure, as well as edema pain in patients with acute heart attack.
In treatment klofelinom regularly measure AD horizontally and vertically patient. Treatment should not stop suddenly, as this can lead to hypertension Stroke (lifting syndrome "). Before lifting klofelina be within 7 to 10 days, gradually lowering the dose. In developing the "syndrome lifting" must immediately return to the reception klofelina and in the future to abolish it gradually replacing antigipertenzivnymi other means.
In applying klofelina could experience dry mouth (particularly in the early days), constipation. In the early days, there is also sedative effect, a sense of fatigue, sleepiness.
In the first minutes after intravenous in some cases there may be a short-term (a few minutes), a modest increase AD.
Injecting klofelina application to be carried out only in the United States.
Clonidine should not appoint kardiogennom in shock, arterial hypotension, vnutriserdechnoy blockade abrupt changes vascular brain in patients with of depression.
During treatment klofelinom forbidden alcohol. A sedative effect and the possibility of slower reactivity should be taken into account when taking medication those who drive cars or profession which requires quick mental or physical reaction.
Bear in mind that excessive doses klofelina or application can be shown to cause severe phenomenon : violation of consciousness, collapse, etc.
Clonidine should not assign patients who can not take it regularly (to avoid the development of "lifting syndrome").
Not recommended Hydrochloride with antidepressants (weakening of the anti-hypertensive), and high doses Neuroleptics (increased sedative effect). Anti-hypertensive effect klofelina reduced by nifedipina (antagonism into effect on the intracellular Ca ion currents' ~).
When alcohol or opium abstinence, Clonidine appointed interior in hospital on the 0.15 - 0.3 mg three times a day at intervals of 6 to 8 hours for 5 to 7 days. In developing side effects, dosage gradually decreasing doses time within 2 to 3 days, then medication if necessary repeal.
When glaucoma Hydrochloride used as a local instillyatsy konyunktivalny bag in the eye. Anti-hypertensive effect klofelina with glaucoma explain local adrenomimeticheskim actions and partly Eferent actions stemming from his nose blowing shell eyes. The drug reduces the secretion and improves the flow of watery mist. Mioza is.
Treatment starts with backfilling 0.25% solution. With insufficient effects using 0.5% solution in the development of side effects from 0,125% solution. Apply 1 drop 2 to 4 times a day.
The drug can be appointed without miotikov, but with little effect, in combination with miotikami.
Duration of klofelina depends on the degree of anti-hypertensive effect (inner); If effect, the drug is used long-term (months, years). If no effect during the first 1 to 2 days it overturned.
Drops klofelina recommended after antiglaukomatoznyh operations in oftalmotonusa decompensation.
Since Hydrochloride vsasyvaetsi minute shell eyes, and its application in the form of eye drops are possible downgrading AD, aetiology, dry mouth, drowsiness.
In stark expressed atherosclerosis and vascular brain expressed arterial hypotension eye drops clonidine (klofelina) can not receive.
Method of issuance : pills for 0.000075 grams (0,075 mg) and 0.00015 grams (0.15 mg) in a package of 50 or 100 pieces; 0.01% injection (0.1 mg) in combination on 1 ml pack, to 10 or 100 vials; 0.125%, 0.25% and 0.5% solutions (eye drops) in tyubik- drip containing 1, 5 ml, and 2 tyubik- looks in the package.
Storage : powder klofelina A-list; Dosage forms list B. In the dark spot.
Release all dosage forms klofelina only be prescribed and used strictly for medical reasons.
Abroad, for the treatment of glaucoma eye drops produced, containing 0.125%, 0.25% and 0.5% clonidine (klofelina), entitled "Izoglaukon (Isoglaucon").
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