Clonidine

General characteristics. Structure:

Active ingredient: 0,00015 g of clonidine (clonidine) in 1 tablet.

Pharmacological properties:

Pharmacodynamics. Clonidine is anti-hypertensive means which action is connected with influence on neurogenic regulation of a vascular tone. Has a promoting effect on pre-and postsynaptic α2-адренорецепторы, at the same time, has also affinity to imidazolinovy receptors.

Clonidine stimulates central α2-адренорецепторы and imidazolinovy I1 receptors which are localized in neurons of kernels of a solitary path and lowers a tone of the vasculomotor center, reduces an impulsation in a sympathetic link of a peripheral nervous system at the presynaptic level. At the same time the tone of vagus nerves raises.

The main manifestation of effect of clonidine is the hypotensive effect developing usually in 1 — 2 h after administration of drug inside and proceeding after a single dose during 6 — 8 h. The expressed and persistent hypotension is result of decrease in cordial emission, reduction of heart rate and peripheric resistance of vessels, including vessels of kidneys.

Drug renders the expressed sedative, and also some analgeziruyushchy action.

Important feature of clonidine is its ability to reduce (and to remove) somatovegetativny manifestations of opiate and alcoholic abstinence. Sensation of fear decreases, gradually there take place cardiovascular and other frustration. Believe that these phenomena are substantially caused by decrease in the central adrenergic activity.

Pharmacokinetics. Clonidine is quickly and completely soaked up from digestive tract; the peak of concentration in plasma is observed in 1,5 — 2,5 h. The elimination half-life makes 12 — 16 h at normal function of kidneys and till 41 o'clock — at its disturbance. Easily gets through gistogematichesky barriers (hematoencephalic, ophthalmic and others). Linkng with proteins of a blood plasma — 20 — 40%. It is metabolized in a liver (about 50% of the soaked-up dose). It is removed preferential by kidneys — 40 — 60% in not changed look, through intestines — 20%.

Indications to use:

Clonidine is applied as anti-hypertensive means at various forms of an idiopathic hypertensia and it is especially wide — for stopping of hypertensive crises.

It can be applied as a part of complex therapy at patients with an abstinence syndrome of opium drug addiction.

Use at menopausal rushes of blood to the person, Tourett's syndrome is possible.

Route of administration and doses:

Doses and schemes of treatment by clonidine should be selected strictly individually. Drug is effective in very small doses. At intake as anti-hypertensive means clonidine is appointed, usually since 0,075 mg (1/2 tablets) 2 — 4 times a day. If the hypotensive effect is insufficient, increase a single dose every 1 — 2 day by 0,0375 mg (on 1/4 tablets) to 0,15 — 0,3 mg (1 — 2 tablets) on reception to 3 — 4 times a day. Daily doses usually make 0,3 — 0,45 mg (2 — 3 tablets), sometimes — 1,2 mg (8 tablets).

At heavy arterial hypertension it is possible to begin 0,15 mg (1 tablet) with a dose, gradually increasing a dose on 0,075 mg (1/2 tablets) before achievement of anti-hypertensive effect, but the maximum daily dose should not be higher than 1,2 mg (8 tablets).

At insufficient efficiency of clonidine in a dose of 0,45 — 0,6 mg (3 — 4 tablets) in days it is reasonable to appoint in addition saluretics in small doses, beta adrenoblockers, vazodilatator of direct action (гидралазин, minoksidit), postsynaptic α1-адреноблокаторы (Prazozinum). At patients of advanced age, especially with displays of atherosclerosis of vessels of a brain, hypersensitivity to drug therefore their treatment begin 0,0375 mg (1/4 tablets) with a dose is possible.

Duration of a course of treatment makes from several weeks to 6 — 12 months and more.

Because of risk of development of a withdrawal the dose of clonidine should be reduced gradually, to complete cessation of administration of drug.

In case of use of clonidine at alcoholic or opiate abstinence drug is appointed inside in the conditions of a hospital on 0,15 — 0,3 mg (1 — 2 tablets) by 3 times a day with an interval of 6 — 8 hours within 5 — 7 days. At development of by-effects the dose is gradually reduced (within 2 — 3 days), then drug is cancelled if necessary.

Features of use:

During treatment it is not necessary to be engaged in potentially dangerous types of activity requiring special attention and psychomotor reactions.

During treatment clonidine forbids the use of alcoholic drinks.

At the sudden termination of therapy by clonidine development of a withdrawal is possible.

It is not necessary to appoint drug the patient who cannot apply it regularly (in order to avoid development of a withdrawal).

Side effects:

From cardiovascular system: seldom — hypostases, bradycardia.

From the alimentary system: decrease in gastric secretion, dryness in a mouth, is rare — a lock.

From TsNS and peripheral nervous system: feeling of fatigue, drowsiness, delay of speed of mental and motor reactions; seldom — nervousness, concern, a depression, dizziness, paresthesias.

From reproductive system: seldom — decrease in a libido, impotence.

Allergic reactions: skin rash, itch.

Others: nose congestion.

Interaction with other medicines:

It is not recommended to apply clonidine together with antidepressants (weakening of hypotensive action) and with neuroleptics (strengthening of sedation, emergence of the expressed depressive frustration is possible). It is not necessary to apply along with benzodiazepines owing to strengthening of depressive effect of clonidine by the last. Hypotensive effect of clonidine decreases under the influence of nifedipine (antagonism in influence on intracellular current of ions of Sa 2+).

When performing therapy by clonidine in a combination with beta adrenoblockers, in order to avoid undesirable increase in arterial pressure in case of the therapy termination, at first it is necessary to finish gradually treatment with beta adrenoblockers, and then also by a slow dose decline to stop clonidine reception.

Contraindications:

Hypersensitivity to clonidine, cardiogenic shock, arterial hypotension, the expressed atherosclerosis of vessels of a brain, obliterating diseases of peripheral arteries, the expressed sinus bradycardia, AV blockade of the II—III degree, a syndrome of weakness of a sinus node, depressions (including in the anamnesis).

Restrictions to use: pregnancy, a lactation (it is necessary to refuse breastfeeding), the work connected with need of bystry mental and (or) physical reaction.

Overdose:

Symptoms: consciousness disturbance, a collapse, bradycardia, broadening of the QRS complex, is possible delay of AV of conductivity and a syndrome of early repolarization.

Treatment: symptomatic therapy, maintenance of the vital functions.

Issue conditions:

According to the recipe

Packaging:

Tablets of 0,15 mg in blister strip packagings No. 10х3, No. 10х5. Tablets 0,15mg in banks No. 50.