N30 clonidine 0,00015g

General characteristics. Structure:

International and chemical nazvaniya:clonidine; N-[(2,6 dichlorophenyl) amine] - 2 imidazoles a hydrochloride; main physical and chemical properties: tablets of color, white or white with a yellowish shade, a ploskotsilindrichesky form with a facet; structure: 1 tablet contains clonidine (a hydrochloride clonidine) of 0,15 mg; excipients: lactoses monohydrate, magnesium stearate, starch potato or corn (in terms of starch with humidity of 13%).

Pharmacological properties:

Pharmacodynamics. The anti-hypertensive means operating at the level with it-rogumoralnoy regulation of a vascular tone. After passing through a blood-brain barrier the clonidine selectively stimulates 2 adrenoceptors of kernels of a vasomotor center of a myelencephalon at the expense of what brakes a sympathetic impulsation from the central nervous system, causing a vazodilatation and a lowering of arterial pressure. Decrease in sympathetic activity is followed by lowering of the level of catecholamines (especially noradrenaline) in a blood plasma and urine though the clonidine has no direct effect on synthesis of catecholamines, and release of noradrenaline from nerve terminations on a negative feedback mechanism as a result of stimulation of the central 2 adrenoceptors oppresses.

The clonidine is an agonist of imidazolinovy receptors. Use of a clonidine leads to decrease in heart rate, systolic and diastolic arterial pressure, and also general peripheral vascular resistance. The minute volume of blood and a stroke output of heart decrease slightly. Prolonged use of a clonidine leads to reduction of a hypertrophy of a myocardium and improvement of function of a left ventricle. The clonidine has sedative and moderate analgeziruyushchy effect. Due to the central action it is capable to eliminate somatovegetativny manifestations of opiate and alcoholic abstinence. The clonidine lowers intraocular pressure due to reduction of secretion and improvement of outflow of watery moisture of an eye. Prolonged use is followed by a liquid delay in an organism.

Pharmacokinetics. After intake the hypotensive effect begins to be shown in 30 – 60 min. The maximum effect develops in 2 – 4 h and about 5 - 12 h remain. Action duration at some sick 24 – 36 h. It is well soaked up from digestive tract irrespective of meal, the maximum concentration in a blood plasma is reached in 1,5 – 2,5 h. Bioavailability at prolonged use – about 65%. Linkng with blood proteins – 20 – 40%. It is metabolized in a liver (about 50% of the soaked-up dose). The elimination half-life at normal function of kidneys of 12-16 h, at a renal failure – increases to 41 h. Easily passes through gistogematichesky barriers, including hematoencephalic and placental, gets into breast milk. It is removed by kidneys (40 – 60%), and also through intestines (20%). At a hemodialysis it is practically not allocated (to 5%).

Indications to use:

Arterial hypertension, hypertensive crises, abstinence syndrome of opium drug addiction (as a part of complex therapy).

Route of administration and doses:

Appoint to adults and teenagers 15 years inside, irrespective of meal are more senior. Drug is effective in small doses. The dose should be selected strictly individually. Drug withdrawal is carried always out gradually within 1 – 2 weeks.

Arterial hypertension. The initial dose usually makes 0,075 mg (drugs of a clonidine of other dosage) 2 – 3 times a day. If necessary the dose is gradually increased to an average daily dose – 0,9 mg (6 tablets). Usually effective therapeutic dose makes 0,15 mg (1 tablet) 2 – 3 times a day. The maximum single dose – 0,3 mg (2 tablets), the maximum daily dose – 1,5 mg (10 tablets).

To patients of advanced age, especially in the presence of displays of a cerebrovascular disease, at the beginning treatment is appointed by clonidine drugs with a possibility of dosing of 0,0375 mg 3 times a day.

Hypertensive crisis. Appoint 0,15 – 0,3 mg (1 – 2 tablets) sublingual (in the absence of the expressed dryness in a mouth).

Abstinence syndrome. Appoint in the conditions of a hospital 0,15 – 0,3 mg (1 – 2 tablets) 3 times a day with an interval of 6 - 8 h within 5 – 7 days. At development of side effects single doses gradually reduce within 2 – 3 days then, if necessary, drug is cancelled.

To teenagers 15 years are more senior (with body weight not less than 45 kg) appoint 0,15 mg (1 tablet) 2 – 3 times a day. If necessary a daily dose increase to effective therapeutic (usually 0,01 – 0,02 mg/kg/days in 3 receptions).

Features of use:

 During treatment Clonidine forbids to take alcoholic beverages.

Sudden phase-out of drug can lead to development of a withdrawal: to increase in arterial pressure, nervousness, a headache, nausea therefore drug withdrawal should be carried out only gradually within 1 – 2 weeks taking into account the accompanying therapy by other medicines. At development of a withdrawal are returned to use of drug at once and further cancel it gradually, replacing with other antihypertensives. For the prevention of a withdrawal it is not necessary to appoint drug the patient who does not have conditions for its regular use.

If at the combined use of Clonidine and a blocker - adrenoceptors the temporary termination of treatment, then a blocker is necessary - adrenoceptors it is necessary to cancel earlier to prevent sympathetic hyperreactivity, and then gradually to cancel Clonidine, especially, if it was applied in high doses.

With care appoint Clonidine a sick diabetes mellitus as the clonidine can mask symptoms of a hypoglycemia and reduce insulin secretion.

With extra care drug is appointed to teenagers because of danger of overdose: toxic action at children is possible at reception of 0,1 mg of a clonidine.

With care drug is appointed the patient of advanced age hypersensitivity to drug is possible; the patient with a renal failure the drug removal delay is possible. Perhaps tranzitorny increase in concentration of somatotropic hormone. Use of Clonidine can lead to reduction and oppression of salivation that promotes development of caries, periodontosis, oral cavity candidiasis.

At treatment Clonidine recommends to control arterial pressure regularly. It is necessary to be careful at a long exercise stress, especially in vertical position at hot weather because of risk of orthostatic reactions.

Use during pregnancy and feeding by a breast. Drug is contraindicated at pregnancy. In need of use during feeding by a breast it is necessary to stop feeding.

Influence on ability to manage vehicles or to work with difficult mechanisms. During therapy by drug it is necessary to avoid potentially dangerous types of activity requiring special attention, bystry mental and motor reactions.

Side effects:

From the central nervous system: increased fatigue, drowsiness, delay of speed of mental and motor reactions, uneasiness, nervousness, depression, bright or "dreadful" dreams, dizziness. From cardiovascular system: bradycardia, orthostatic hypotension. From the alimentary system: dryness in a mouth, a loss of appetite, nausea, vomiting, a lock, decrease in gastric secretion. Allergic reactions: skin rash, itch; extremely seldom at sublingual use (at hypertensive crisis) hypostasis of mucous membranes, breath difficulty. Other: nose congestion, urination delay, decrease in a libido and potentiality; seldom Reynaud's syndrome (pallor, cold snaps of extremities).

Interaction with other medicines:

At combined use with the drugs oppressing the central nervous system, perhaps mutual strengthening of the depriving of bonuses influence on the central nervous system and development of depressive frustration. Hypotensive effect of a clonidine tricyclic antidepressants, anorexigenic (except for a fenfluramin), sympathomimetic weaken, non-steroidal anti-inflammatory drugs and nifedipine; raise vazodilatator, diuretics, antihistamines. - Adrenoblockers and cardiac glycosides increase risk of development of bradycardia or (in some cases) lead to development of an atrioventricular block. At simultaneous use with atenololy, propranolol the additive hypotensive effect, sedative action and dryness in a mouth develops. Hormonal contraceptives at intake can strengthen Clonidine sedation. The clonidine can reduce efficiency of a levodopa and piribedil at patients with Parkinson's disease. The clonidine can increase concentration of cyclosporine, and also concentration of glucose in blood due to decrease in secretion of insulin that needs to be considered at simultaneous use with insulin.

Contraindications:

The increased individual sensitivity to a clonidine or any of auxiliary components of drug; arterial hypotension, cardiogenic shock, an atrioventricular block of II and III degrees, the expressed bradycardia, a syndrome of weakness of a sinus node, disturbance of cerebral circulation, Reynaud's syndrome, depressions (including in the anamnesis), simultaneous use of tricyclic antidepressants, the period of pregnancy and feeding by a breast, children's age up to 15 years.

Overdose:

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

Treatment: symptomatic therapy (liquid infusion, at the expressed depression of the central nervous system or an apnoea of 2 - 4 mg of Naloxonum intravenously, if necessary repeat). 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:

To store in the place protected from light at a temperature from 8 °C to 25 °C. To store in the place, unavailable to children.

Period of validity – 4 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,15 mg No. 30 in the blister in a box; No. 30 in the blister.