Clonidine

General characteristics. Structure:

Active ingredient: 75 mkg or 150 mkg of a clonidine.

Excipients: potato starch, lactose (sugar milk), magnesium stearate in a blister strip packaging of 10 pieces or in glass jars on 50 pieces; in a pack of cardboard 5 packagings or in a cardboard box 1 glass jar respectively.

The hypotensive medicine having direct effect on vasomotor centers of a brain.

Pharmacological properties:

Pharmacodynamics. Anti-hypertensive central acting agent. The mechanism of action is caused by stimulation postsynaptic α2-адренорецепторов a vasomotor center of a myelencephalon and reduces a flow of a sympathetic impulsation to vessels and heart at the presynaptic level. The hypotensive effect is caused by decrease in OPSS, reduction of ChSS and cordial emission.

At bystry in introduction perhaps short-term increase in the ABP caused by stimulation postsynaptic α1-адренорецепторов vessels. Increases a renal blood stream; raising a tone of vessels of a brain, reduces a brain blood stream; has the expressed sedative effect.

Duration of therapeutic effect - 6-12 h.

At an instillation in a conjunctival sac there is a decrease in intraocular pressure owing to local adrenostimuliruyushchy action as a result of which products of intraocular liquid decrease and somewhat its outflow, and also thanks to weakening of the sympathetic tone caused central effects of active agent which part underwent a resorption improves.

Pharmacokinetics. At intake it is well absorbed from a GIT, Cmax in a blood plasma is reached in 2-4 h. Linkng with proteins - 20-40%. About 50% of the absorbed dose are metabolized in a liver. T1/2 at normal function of kidneys is 12-16 h, at a renal failure - to 41 h. It is removed by kidneys - 40-60% in not changed look, through intestines - 20%.

Indications to use:

For system use: arterial hypertension (including symptomatic hypertensia of renal genesis), hypertensive crisis.

For topical administration in ophthalmology: an open angle glaucoma (as monotherapy or in combination with other drugs reducing intraocular pressure).

Route of administration and doses:

Establish individually. An initial dose - on 37.5-75 mkg of 3 times/days. If necessary a dose gradually increase 900 mkg to an average daily dose. The course of treatment averages 1-2 months.

At in oil or in introduction the single dose makes 150 mkg.

Maximum doses: at intake a single dose - 300 mkg, a daily dose - 2.4 mg.

For use in ophthalmology: dig in in a conjunctival sac of 2-4 times/days. Treatment begin 0.25% of solution with appointment. In case of insufficient decrease in intraocular pressure use 0.5% solution. At development of the by-effects connected with use of 0.25% of solution appoint 0.125% solution.

Features of use:

With care to apply after recently postponed myocardial infarction, at a chronic renal failure.

At the sudden termination of therapy development of a withdrawal is possible: increase in the ABP, nervousness, headaches, tremor, nausea.

When performing therapy by a clonidine in a combination with beta adrenoblockers, in order to avoid undesirable increase in the ABP 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 reception of a clonidine.

For prevention of developing of orthostatic hypotension at in introduction of a clonidine of the patient has to be in a prone position during introduction and during 1.5-2 h after introduction.

In the absence of effect during the first 1-2 days drug is cancelled. For reduction of systemic action of drug after instillation it is necessary to press for 1-2 min. a finger area of a dacryocyst.

Influence on ability to driving of motor transport and to control of mechanisms

During treatment it is necessary to avoid potentially dangerous types of activity requiring special attention and bystry psychomotor reactions.

Side effects:

From cardiovascular system: seldom - hypostases, bradycardia; at in introduction orthostatic hypotension is possible.

From the alimentary system: decrease in gastric secretion, dryness in a mouth; seldom - 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.

Local reactions: dryness of a conjunctiva, an itch or burning in eyes.

Interaction with other medicines:

At the patients receiving beta adrenoblockers in case of sudden cancellation of a clonidine perhaps sharp increase in the ABP. Believe that it is connected with increase in maintenance of catecholamines in the circulating blood and strengthening of their vasopressor action.

At simultaneous use of hormonal contraceptives for intake strengthening of sedative action of a clonidine is possible.

At simultaneous use of tricyclic antidepressants (including Imipraminum, a klomipramin, desipramine) anti-hypertensive action of a clonidine decreases.

At simultaneous use with a clonidine increase in duration of action a vekuroniya is possible.

At simultaneous use with verapamil there is a message on development of a heart block in the patient with arterial hypertension.

Believe that the clonidine suppresses the raised products of catecholamines arising owing to a hypoglycemia, and, therefore, hypoglycemia symptoms (tachycardia, palpitation, the increased sweating) which are caused by influence of catecholamines. Besides, there are messages that the clonidine increases the content of glucose in blood, apparently, due to insulin secretion reduction. It needs to be taken into account at simultaneous use of insulin.

Upon transition from reception of a clonidine to captopril anti-hypertensive action of the last develops gradually. In case of sudden cancellation of a clonidine at the patients receiving captopril, perhaps sharp increase in the ABP.

Patients have messages on reduction of efficiency of a levodopa and a piribedil with Parkinson's disease.

At simultaneous use with Prazozinum change of anti-hypertensive action of a clonidine is possible.

At simultaneous use of propranolol, an atenolol the additive hypotensive effect, sedative action, dryness in a mouth develops.

At simultaneous use with cyclosporine there is a message on increase in concentration of cyclosporine in a blood plasma.

Contraindications:

Arterial hypotension, the expressed atherosclerosis of vessels of a brain, obliterating diseases of peripheral arteries, the expressed sinus bradycardia, SSSU, AV blockade of II and III degrees, cardiogenic shock, depression (including in the anamnesis), simultaneous use of tricyclic antidepressants, simultaneous use of ethanol and other means exerting the oppressing impact on TsNS, pregnancy, the lactation period, hypersensitivity to a clonidine.

Overdose:

Symptoms:
- drowsiness, a miosis (the expressed narrowing of pupils);
- bradycardia, continuous vomiting, xerostomia;
- respiratory depression (up to an apnoea);
- consciousness disturbance, collapse;
- decrease or increase in arterial pressure (especially at teenagers);
- expansion of the QRS complex, hypothermia;
- delay of atrioventricular conductivity and a syndrome of early repolarization is possible.

Treatment: symptomatic therapy (liquid infusion, at the expressed depression of the central nervous system or an apnoea – 2 – 4 mg of Naloxonum intravenously, at need are repeated).
As a specific antidote Tolazolinum can be used: 1 mg of Tolazolinum at intravenous administration or 50 mg at appointment inside neutralize effect of 0,6 mg of a clonidine.

Storage conditions:

List No. 1 of strong substances PKKN (tablet). To store in protected from light and the place, unavailable to children, at a temperature not over 30 ºС.

Issue conditions:

According to the recipe

Packaging:

On 10 pieces of tablets - planimetric strip packagings (5) - packs cardboard.
On 50 pieces of tablets - banks of dark glass (1) - a pack cardboard.