Clonidine

Clonidine – hypotensive drug.

Form of release and structure

Clonidine is produced in the following dosage forms:

• Tablets (in dark glass or polymeric jars on 50 pieces, after 1 bank in a cardboard pack; in blister strip packagings on 10 pieces, on 1, 2 or 5 packagings in a cardboard pack);
• Solution for intravenous administration (in ampoules on 1 ml with a knife ampoule, on 10 ampoules in a cardboard pack);
• Drops eye (in tubes droppers on 1,3 ml, on 5 tubes in a cardboard pack).

Is a part of 1 tablet:

• Active agent: a clonidine – 0,075 or 0,15 mg (in the form of a hydrochloride);
• Auxiliary components: monohydrate of lactose (milk sugar) – 47,925/133,35 mg, potato starch – 11,4/15 mg, magnesium stearate – 0,6/1,5 mg.

For intravenous administration is a part of 1 ml of solution:

• Active agent: a clonidine – 0,1 mg (in the form of a hydrochloride);
• Auxiliary components: 0,1 M Acidum hydrochloricum solution – to рН 4-5,5, water for injections – to 1 ml.

Eye is a part of 1 ml of drops:

• Active agent: a clonidine – 1,25, 2,5 or 5 mg (in the form of a hydrochloride);
• Auxiliary components: sodium chloride, a dihydrate dihydrosodium phosphate, dodecahydrate hydrosodium phosphate, water for injections.

Indications to use

• Tablets: arterial hypertension;
• Solution for intravenous administration: stopping of hypertensive crisis;
• Drops are eye: primary open angle glaucoma with moderately increased or high intraocular pressure and the stabilized visual functions.

Contraindications

• The expressed atherosclerotic changes of vessels of a brain;
• Depression;
• Arterial hypotension;
• Pregnancy and period of a lactation;
• Age up to 18 years (efficiency and safety of use of Clonidine for this group of patients is not established);
• Hypersensitivity to drug components.

In addition contraindications to use of Clonidine in the form of tablets and solution for injections are:

• Atrioventricular block of II and III degrees;
• The expressed sinus bradycardia;
• Cardiogenic shock;
• Sick sinus syndrome;
• Obliterating diseases of arteries;
• Simultaneous use with tricyclic antidepressants and ethanol.

Drug should be used with care the patient after recently postponed myocardial infarction, and also to patients with a chronic renal failure and an atrioventricular block of the I degree.

Route of administration and dosage

Clonidine in the form of tablets is accepted inside, without chewing and washing down with a small amount of liquid, it is more preferable – in time or after food.

Drug is effective in rather small doses (the doctor sets the dosing mode individually).

Therapy is begun, as a rule, with small doses (2-3 times a day on 0,075 mg). At insufficiency of anti-hypertensive effect perhaps gradual (each 1-2 days on 0,0375 mg) increase in a single dose up to 0,15 mg.

At elderly patients, in particular at manifestations of an angiosclerosis of a brain, treatment begin with a dose 0,0375 mg (because of possible existence of hypersensitivity to drug components).

Usually daily doses fluctuate within 0,3-0,45 mg, in some cases – 1,2-1,5 mg. The maximum single dose – 0,3 mg, daily – 2,4 mg.

Solution of Clonidine is entered intravenously. The doctor selects doses individually.

For intravenous administration of 0,5-1,5 ml of solution of Clonidine dissolve 0,9% of solution of sodium chloride in 10-20 ml. The drug is administered slowly – for 3-5 minutes.

For drop introduction of 4 ml of solution it is necessary to dissolve 5% of solution of glucose in 500 ml. Introduction is carried out with an average speed – 20 drops a minute. The maximum speed of infusion – 120 drops a minute. In stationary conditions it is possible to enter Clonidine parenterally 3-4 times a day.

Drops eye apply in the form of instillations. A single dose – 1 drop, frequency rate of use – 2-4 times a day. At insufficient effect performing the combined treatment is possible (along with miotika).

Therapy is begun with 0,25% of solution. At insufficient decrease in intraocular pressure pass to use 0,5% of solution, at development of side effects – 0,125% of solution.

Side effects

At Clonidine use inside and intravenously possibly development of the following side effects (very often – from 1/10; often – from 1/100 and to 1/10; infrequently – from 1/1000 and to 1/100; seldom – from 1/10000 and to 1/1000; very seldom – to 1/10000, including single messages):

• Cardiovascular system: in rare instances at the beginning of therapy – short-term paradoxical increase in arterial pressure; very often – orthostatic hypotension; infrequently – Reynaud's syndrome, a sinus bradycardia; seldom – an atrioventricular block; with an unknown frequency – a bradyarrhythmia;
• Alimentary system: very often – dryness of a mucous membrane of an oral cavity; often – a lock, nausea, a loss of appetite, pain in sialadens, decrease in gastric secretion, vomiting; seldom – pseudo-obstruction of a large intestine; with an unknown frequency – hepatitis;
• Central nervous system: very often – drowsiness, dizziness, increased fatigue, delay of speed of motor and mental reactions; often – sleep disorders, nervousness, a headache, a depression; infrequently – paresthesias; seldom – perception disturbance, an adynamy, hallucinations, "dreadful" or bright dreams; with an unknown frequency – confusion of consciousness;
• Respiratory system: seldom – a xeromycteria;
• Reproductive system: often – erectile dysfunction; with an unknown frequency – decrease in a libido; seldom – a gynecomastia;
• Integuments: infrequently – rash (including a small tortoiseshell), a skin itch; seldom – an alopecia;
• Sense bodys: seldom – decrease in a slezootdeleniye; with an unknown frequency – accommodation disturbance;
• Laboratory indicators: seldom – a hyperglycemia; with an unknown frequency – change of functional trials of a liver;
• Others: with an unknown frequency – Reynaud's phenomenon, the delay of water and sodium which is shown hypostases of anklebones and feet; infrequently – a nose congestion; at sudden cancellation – a syndrome of "cancellation".

At use of Clonidine in the form of eye drops there can be such disturbances as: bradycardia, weakness, dryness in a mouth, drowsiness, an excessive lowering of arterial pressure, feeling of a foreign subject or burning in an eye.

Special instructions

During use of Clonidine it is forbidden to take alcoholic drinks.

Duration of a course of therapy is defined by the received results. In order to avoid development of a withdrawal the termination of administration of drug is carried out gradually for 7-10 days. In case of development of a syndrome it is necessary to return at once to Clonidine reception, further it is cancelled gradually with replacement with other anti-hypertensive drugs.

At intravenous use of Clonidine for prevention of developing of orthostatic hypotension the patient needs to be in a prone position during administration of drug and within 1,5-2 hours after the end of a procedure.

In the absence of effect in the first 2 days of use of eye drops therapy is cancelled.

It is necessary to consider that Klofelin in all dosage forms lowers physical and mental reactions at different types of operator activity. Treatment of patients whose work demands bystry physical and mental reaction (drivers, pilots, etc.) is recommended to be carried out only in stationary conditions or it is out-patient with release for the period of treatment for work.

Medicinal interaction

At simultaneous use of Clonidine with some medicines there can be following effects:

• The drugs oppressing the central nervous system: development of depressive frustration and strengthening of the depriving of bonuses influence on the central nervous system;
• Tricyclic antidepressants, sympathomimetic, anorexigenic (except a fenfluramin) medicines, nifedipine and non-steroidal anti-inflammatory drugs: easing of hypotensive effect of Clonidine;
• Cardiac glycosides and beta adrenoblockers: increase in risk of development of bradycardia or (in some cases) atrioventricular block;
• Atenolol, propranolol: development of the additive hypotensive effect, sedative action, dryness in a mouth;
• Levodopa, piribedit: reduction of their efficiency;
• Diuretics, vazodilatator, antihistamines: increase in hypotensive effect of Clonidine;
• Prazozinum: change of anti-hypertensive action of a clonidine;
• Cyclosporine: increase in its concentration in a blood plasma;
• Hormonal contraceptives for intake: strengthening of sedative action of a clonidine;
• Tolperisonum: strengthening of myorelaxation action;
• Tofizopamum: strengthening of anxiolytic action;
• Phenylephrinum: strengthening of pressor effect;
• Mirtazapin: development of hypertensive crisis;
• Haloperidol: strengthening of oppression of the central nervous system;
• Sulpiridum: strengthening of effect of a clonidine;
• Insulin, hypoglycemic means for intake: weakening of hypoglycemic effect of Clonidine.

Terms and storage conditions

To store in protected from light, the place, unavailable to children.

Period of validity:

• Drops eye – 2 years at a temperature up to 15 °C;
• Solution for intravenous administration – 3 years at a temperature up to 30 °C;
• Tablets – 4 years at a temperature up to 30 °C.