Clonidine

General characteristics. Structure:

Active ingredient: 0,075 mg or 0,15 clonidine (clonidine) in 1 tablet.

Excipients: potato starch, sugar milk (lactose), calcium stearate.

Pharmacological properties:

Pharmacodynamics. Treats the list of strong and toxic agents of Standing committee on control of drugs. Hypotensive drug of the central action, getting through a blood-brain barrier, stimulates postsynaptic alfa2-adrenoceptors of vasomotor centers, thereby reducing a flow of sympathetic impulses from the central nervous system (medullary substance and a myelencephalon) and reduces release of noradrenaline from nerve terminations, having, thus, sympatholytic effect. Braking of a sympathetic impulsation leads to a lowering of arterial pressure (ABP), an urezheniye of the heart rate (HR), decrease in the general peripheric vascular and renal resistance (the renal blood stream at the same time does not change).

Brakes excretion of catecholamines and their metabolites with urine. Bradycardia is caused both by reduction sympathetic, and increase in a vagal tone.

Increase of a vagal tone leads to increase in reflex sensitivity of baroreceptors. Reduces activity of a renin in a blood plasma. Has the sedative effect connected with influence on a reticular formation of a brain.

Duration of action from 2 to 24 hours.

Pharmacokinetics. It is quickly soaked up from digestive tract after intake (bioavailability is equal to 60-95%). Maximum concentration in a blood plasma is reached in 2-4 hours and about 5 hours remain. Communication with proteins of a blood plasma - 20-40% Easily and quickly gets through a blood-brain barrier. The elimination half-life of drug is equal to 12-16 hours, at a renal failure - till 41 o'clock. Duration of action from 2 to 24 hours. It is metabolized in a liver (about 50% of the soaked-up dose), 65% of drug are removed in the form of metabolites with urine, 20% - with excrements.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Drug is effective in very small doses. Doses should be selected strictly individually.

Clonidine is accepted in time or after food, without chewing, washing down with a small amount of liquid. Usually treatment begin with small doses (0,075 mg 2-3 times a day). If the hypotensive effect is insufficient, the single dose is gradually increased every 1-2 day by 0,0375 mg to 0,15 mg.

At patients of advanced age, especially with manifestation of an angiosclerosis of a brain, hypersensitivity to drug therefore their treatment begin 0,0375 mg with a dose is possible.

Daily doses usually make 0,3-0,45 mg, sometimes 1,2-1,5 mg.

Features of use:

Pregnancy and lactation. Results of clinical trials of clonidine at pregnant women are limited. Use during pregnancy is contraindicated. The clonidine gets into breast milk therefore in need of use of drug in the period of a lactation it is necessary to stop breastfeeding.

The course of treatment depends on the received results, duration of a course of treatment is determined by the doctor. The termination of administration of drug should be carried out gradually (to reduce doses) within 7-10 days in order to avoid development of hypertensive crisis ("withdrawal"). At development of a syndrome at once are returned to administration of drug and further cancel it gradually, replacing with other anti-hypertensive means. For the prevention of a syndrome it is not necessary to appoint drug the patient who does not have conditions for his regular reception.

During treatment clonidine forbids the use of alcoholic drinks.
 
Influence on ability to manage vehicles and mechanisms. Drug reduces mental and physical reactions at different types of operator activity. Treatment of patients whose work demands bystry mental and physical reaction (a profession of the driver, the pilot, etc.) is admissible only in the conditions of a hospital or is out-patient with release from work.

Side effects:

Frequency: very often - more than 1/10 (at 1 patient from 10), it is frequent - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, is rare - more than 1/10000 and less than 1/1000, is very rare - less than 1/10000, including isolated cases.

From the central nervous system: very often - dizziness; often - a headache, a depression, a sleep disorder; not often - paresthesias, disturbance of perception, a hallucination, nightmares; frequency "is known - confusion of consciousness.

From sense bodys: seldom - decrease in products of the lacrimal liquid; frequency is unknown - accommodation disturbance.

From cardiovascular system: very often - orthostatic hypotension; infrequently - a sinus bradycardia, Reynaud's syndrome; seldom - an atrioventricular block; frequency is unknown - a bradyarrhythmia.

From respiratory system: seldom - a xeromycteria.

From the alimentary system: very often - dryness of a mucous membrane of an oral cavity; often - a lock, nausea, pain in sialadens, vomiting; seldom - pseudo-obstruction of a large intestine; frequency is unknown - hepatitis.

From integuments: infrequently - a skin itch, rash (including a small tortoiseshell); seldom - an alopecia.

From reproductive system: often - erectile dysfunction; frequency is unknown - decrease in a libido; seldom - a gynecomastia.

From laboratory indicators: seldom - a hyperglycemia; frequency is unknown - change of functional trials of a liver.

Interaction with other medicines:

Anti-hypertensive drugs of other groups (beta adrenoblockers, diuretics, spasmolysants, etc.) strengthen hypotensive effect of clonidine. At combined use with cardiac glycosides toxicity of the last amplifies. The means oppressing the central nervous system increase drowsiness and a depression, and drugs propranolol and гуанетидин - when sharing can provoke development of heart failure.

Tricyclic antidepressants, neuroleptics of a fenotiazinovy row, Pipofezinum, пирлинбдол, amphetamine reduce anti-hypertensive effect of clonidine.

The effect is strengthened by antihistaminic drugs; weaken non-steroidal anti-inflammatory drugs.

Contraindications:

Individual intolerance of components of drug, atrioventricular block of II and III degrees, the expressed sinus bradycardia, sick sinus syndrome, the expressed atherosclerotic changes of vessels of a brain obliterating diseases of arteries, a depression, arterial hypotension, cardiogenic shock, pregnancy, the feeding period of a breast, simultaneous use of tricyclic antidepressants and ethanol, age up to 18 years (efficiency and safety are not established).

With care. Recently postponed myocardial infarction, a chronic renal failure.

Overdose:

Symptoms: decrease or increase in the ABP, bradycardia, lengthening of the QRS complex, delay of atrioventricular conductivity, a syndrome of early repolarization, slackness, a miosis, a hypothermia, respiratory depression (it is possible up to an apnoea), a collapse, a loss of consciousness.

Treatment: symptomatic.

Storage conditions:

List No. 1 of strong substances PKKN. In protected from light and the place, unavailable to children. A period of validity - 4 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,075 mg and 0,15 mg. On 10 tablets in a blister strip packaging. On 50 tablets in banks of light-protective glass or polymeric. Each can or 5 planimetric packagings together with the application instruction are placed in a pack from a cardboard.