Clonidine is an antihypertensive drug with a pronounced hypotensive and sedative effect. It is used for hypertensive crises, as well as for the treatment of hypertension and glaucoma. Clonidine hydrochloride acts as the active substance of the drug.

In this article, we will consider why doctors prescribe Clonidine, including instructions for use, analogues and prices for this drug in pharmacies. REAL REVIEWS people who have already used Clonidine can be read in the comments.

Composition and form of release

Available in the form of eye drops, tablets, injection solution.

• The active ingredient is clonidine.

Pharmacological group: alpha-adrenergic agonists.

Indications for use

The number of indications for use drug includes:

• hypertensive crisis;
• withdrawal symptoms in patients with opioid dependence;
• arterial hypertension and a tendency to increase blood pressure (as symptomatic or as part of complex therapy);
• primary open-angle glaucoma, accompanied by increased intraocular pressure.

pharmachologic effect

Clonidine in a short period of time reduces arterial pressure, normalizes the number of heart contractions, has a positive effect on the central nervous system, and also reduces intraocular pressure.

The main functions of the analyzed drug are due to the excitation of postsynaptic alpha2-adrenergic receptors of special inhibitory structures located in the brain. In addition, in the instructions for Clonidine, it is noted that this remedy reduces sympathetic impulses suitable for the heart and the entire vascular network.

Instructions for use

According to the instructions for use Clonidine tablets are taken, regardless of food intake, inside. The initial dosage is 0.075 mg three times a day. If necessary, the dosage is increased to 0.9 grams per day.

• With arterial hypertension, Clonidine is taken 2-3 times a day. The starting dose is usually 0.075 mg. Every 1-2 days, if necessary, the dose of the drug is gradually increased to 1-2 tablets 3 times a day. Single doses of clonidine exceeding 0.3 mg can be prescribed only in exceptional cases and, preferably, in a hospital setting. The effective therapeutic dose is 0.15 mg (1 tablet). Reception is carried out 2-3 times a day. The highest daily dose is 6 tablets (0.9 mg). If the effectiveness of the drug in high doses is low, treatment is supplemented with saluretics or other antihypertensive drugs (except for nifedipine). Elderly patients, especially with manifestations of cerebrovascular disease, are recommended an initial dose of 0.0375 mg 2-3 times a day.
• With hypertension, Clonidine tablets are taken 3 times a day, 0.075 mg each. During the course of treatment, the dose may subsequently be increased. In old and senile age, as an additional treatment for atherosclerotic phenomena. Cancel medicinal product sequentially, reducing the dosage of the drug in stages.

Therapeutic treatment of glaucoma using Clofelin eye drops involves instilling 1 drop into each conjunctival canal three times a day, unless another dosage is prescribed by the ophthalmologist. If the intraocular pressure does not decrease when a 0.25% solution of the drug is instilled, Clonidine with a concentration of 0.5% is prescribed. With pronounced side effects, the concentration of Clonidine should be reduced to 0.125%.

Contraindications

Contraindications to the use of tablets and solution for injection are:

1. Arterial hypotension;
2. Obliterating peripheral arterial disease;
3. Depression (including history);
4. Severe sinus bradycardia;
5. Cardiogenic shock;
6. Sick sinus syndrome (SSS);
7. The simultaneous use of ethanol and other drugs that depress the central nervous system (CNS);
8. Combined use of tricyclic antidepressants;
9. AV block II and III degree;
10. Pregnancy and breastfeeding period;
11. Hypersensitivity to the components of the product.
12. Contraindications for using eye drops:
13. Arterial hypotension;
14. Severe atherosclerosis of the vessels of the brain;
15. Hypersensitivity to the drug.

The drug should be used with caution in patients after a recent myocardial infarction, as well as in patients with chronic renal failure and atrioventricular block of the 1st degree.

Side effects

Side effects, as a rule, occur in the first days of taking the drug:

• dizziness;
• sexual disorders;
• increase in body weight;
• constipation;
• nausea, vomiting;
• slowing down of heart rate;
• nightmares;
• dry mouth;
• weakness;
• drowsiness and lethargy;
• feeling tired;
• fainting conditions.

With the correct determination of the frequency and dose of Clonidine, side effects gradually disappear.

Analogs

Clonidine analogs:

• Gemiton;
• Chlofazoline;
• Katapresan;
• Clonidine hydrochloride.

Attention: the use of analogs must be agreed with the attending physician.

Price

The average price of CLOFELIN tablets in pharmacies (Moscow) is 35 rubles.

each tablet contains

active substance: clonidine hydrochloride (clonidine) - 0.15 mg;

excipients:lactose monohydrate, magnesium stearate, potato starch.

Description

tablets white or almost white, flat-cylindrical, with a chamfer.

pharmachologic effect

Clonidine is an antihypertensive agent, the action of which is associated with the effect on the neurogenic regulation of vascular tone.

Clonidine excites α2-adrenergic receptors, lowers the tone of the vasomotor center of the medulla oblongata and reduces impulses in the sympathetic link of the peripheral nervous system at the presynaptic level.

The main manifestation of the action of clonidine is the hypotensive effect, which usually develops 1-2 hours after taking the drug inside and continues after a single dose for 6-8 hours. The hypotensive effect of clonidine is accompanied by a decrease in cardiac output and a decrease in peripheral vascular resistance, including renal vessels.

The drug has a pronounced sedative, as well as some analgesic effect.

An important feature of clonidine is its ability to reduce (and remove) somatovegetative manifestations of opiate and alcohol withdrawal. The feeling of fear decreases, cardiovascular and other disorders gradually disappear. It is believed that these phenomena are largely due to the effect of clonidine on the central α2-adrenergic receptors.

Pharmacokinetics

Clonidine is rapidly and completely absorbed from gastrointestinal tract; the peak plasma concentration is observed after 1.5-2.5 hours. The half-life is 12-16 hours with normal renal function and up to 41 hours when it is impaired. Easily penetrates the histohematogenous barriers (blood-brain, ophthalmic and others). Plasma protein binding - 20-40%. It is metabolized in the liver (about 50% of the absorbed dose). It is excreted mainly by the kidneys - 40-60% unchanged, through the intestines - 20%.

Indications for use

Hypertensive crisis treatment.

Contraindications

Hypersensitivity to active substance or any other component of the drug, severe sinus bradycardia, AV block II-III degree, sick sinus syndrome, pregnancy, lactation, childhood up to 15 years old.

Carefully:depression (including history), ischemic heart disease (especially recent myocardial infarction), severe CHF, cerebrovascular diseases, intracardiac conduction disorders (including mild bradyarrhythmia and medium), impaired peripheral circulation, polyneuropathy, constipation, chronic renal failure, concomitant use with tricyclic antidepressants, diabetes mellitus.

Pregnancy and lactation

The drug is contraindicated in pregnancy. If necessary, use during lactation should stop breastfeeding.

Method of administration and dosage

Assign to adults inside, regardless of food intake.

Doses and treatment regimens for clonidine should be selected strictly individually.

With a hypertensive crisis appoint 0.15 - 0.3 mg (1-2 tablets) sublingually (in the absence of severe dry mouth).

Patients with renal impairment.The dose of the drug must be adjusted in accordance with the degree of renal failure and the individual patient's response to treatment, which can vary significantly in this category of patients; careful monitoring is necessary.

Children.Due to the lack of adequate data on the safety of the use of clonidine in children and adolescents under the age of 18, the use of clonidine in pediatric practice is not recommended.

Side effect

Development frequency side effects given in the following gradation: very often (\u003e 1/10); often (\u003e 1/100,<1/10); нечасто (>1/1000, <1/100); редко (>1/10000, <1/1000); очень редко (<1/10000); неизвестная частота (по имеющимся данным определить частоту встречаемости не представляется возможным).

On the part of the cardiovascular system: very often:orthostatic hypotension; infrequently:raynaud's syndrome, bradycardia; seldom:atrioventricular block; unknown frequency:bradyarrhythmia.

From the digestive system: very often:dryness of the oral mucosa; often:constipation, nausea, vomiting, pain in the salivary glands; seldom:intestinal obstruction; rarely:hepatitis.

From the nervous system and sensory organs: very often:dizziness, sedation; often:headache, sleep disturbance, depression; infrequently:anxiety, paresthesia, hallucinations, nightmares; unknown frequency:slowing down the speed of mental and motor reactions, violation of accommodation, reduced production of tear fluid.

From the respiratory system: rarely:nasal congestion.

From the endocrine system: rarely:gynecomastia.

On the part of the skin and subcutaneous tissue: infrequently:skin rash, hives, itching; seldom:alopecia.

From the reproductive system and mammary glands: often:erectile disfunction; seldom:gynecomastia; unknown frequency:decreased libido.

General violations: often:fatigue; infrequently:malaise.

On the part of laboratory parameters: rarely:increased blood glucose levels; rarely:changes in liver function tests.

Overdose

Symptoms:constriction of the pupils (miosis), general weakness, bradycardia, arterial hypotension, hypothermia, drowsiness, including coma and respiratory depression (up to apnea).

Paradoxical arterial hypertension is caused by stimulation of peripheral α-receptors. Transient hypertension can occur with doses over 10 mg.

Treatment:there is no specific antidote for clonidine overdose. If necessary, you can take activated carbon. Supportive therapy includes the administration of atropine sulfate for bradycardia, inotropic sympathomimetics for hypotension. In severe arterial hypertension, correction with α-adrenergic receptor blockers is possible. For clonidine-induced respiratory depression, naloxone is administered.

Interaction with other medicinal products

It is not recommended to use clonidine together with antidepressants (weakening of the hypotensive effect) and with antipsychotics (increased sedation, severe depressive disorders may occur). Should not be used concomitantly with benzodiazepines due to the latter's intensification of the depressive effect of clonidine. The hypotensive effect of clonidine decreases under the influence of nifedipine (antagonism in the effect on the intracellular current of Ca 2+ ions). When clonidine is used together with vasodilators, diuretics and antihistamines, its hypotensive effect is enhanced. In combination with quinidine, it causes severe bradycardia. It is inappropriate to combine the use of clonidine with methyldopa (dopegit), guanfacine, antacids. Clonidine enhances the depressing effect of ethanol on the central nervous system; enhances the specific effect of ketamine, narcotic analgesics, droperidol. In combination with sodium thiopental, enflurane, isoflurane, it can cause severe bradycardia and hypotension. Α 2 -adrenoceptor antagonists such as mirtazapine can neutralize clonidine-mediated effects on α 2 -adrenergic receptors; this relationship is dose-dependent. Clonidine should not be used in conjunction with adrenaline, norepinephrine, reserpine, phenothiazines (aminazine), oral hypoglycemic agents. Non-steroidal anti-inflammatory drugs reduce the antihypertensive effect of clonidine. When used simultaneously with β-blockers or cardiac glycosides (digoxin), the risk of developing atrioventricular block and severe bradycardia increases. When carrying out therapy with clonidine in combination with β-blockers, in order to avoid an undesirable increase in blood pressure in case of discontinuation of therapy, you must first gradually end treatment with β-blockers, and then also by slowly reducing the dose, stop taking clonidine. It is not recommended to use clonidine together with antidepressants ( weakening of the hypotensive effect) and with antipsychotics (increased sedation, the occurrence of severe depressive disorders is possible). Should not be used concomitantly with benzodiazepines due to the latter's increased depressive effect of clonidine The hypotensive effect of clonidine decreases under the influence of nifedipine (antagonism in the effect on the intracellular current of Ca 2+ ions). When clonidine is used together with vasodilators, diuretics and antihistamines, its hypotensive effect is enhanced. In combination with quinidine, it causes severe bradycardia. It is inappropriate to combine the use of clonidine with methyldopa (dopegit), guanfacine, antacids. Clonidine enhances the depressing effect of ethanol on the central nervous system; enhances the specific effect of ketamine, narcotic analgesics, droperidol. In combination with sodium thiopental, enflurane, isoflurane, it can cause severe bradycardia and hypotension. Α 2 -adrenoceptor antagonists such as mirtazapine can neutralize clonidine-mediated effects on α 2 -adrenergic receptors; this relationship is dose-dependent. Clonidine should not be used in conjunction with adrenaline, norepinephrine, reserpine, phenothiazines (aminazine), oral hypoglycemic agents. Non-steroidal anti-inflammatory drugs reduce the antihypertensive effect of clonidine. When used simultaneously with β-blockers or cardiac glycosides (digoxin), the risk of developing atrioventricular block and severe bradycardia increases. When carrying out therapy with clonidine in combination with β-blockers, in order to avoid an undesirable increase in blood pressure in case of discontinuation of therapy, you must first gradually end treatment with β-blockers, and then also by slowly reducing the dose, stop taking clonidine.

Precautions

Special care should be taken in patients with depression or cerebrovascular disease. a sharp decrease in blood pressure can cause a change in mental status.

When treating patients with heart failure with clonidine, careful monitoring is necessary.

Ineffective for pheochromocytoma.

During treatment, it is prohibited to consume alcoholic beverages.

A sudden discontinuation of the drug can lead to the development of a withdrawal syndrome (especially in patients taking more than 0.9 mg / day): increased blood pressure, nervousness, headache, nausea, therefore, the drug should be withdrawn only gradually over 1-2 weeks with taking into account concomitant therapy with other drugs. With the development of the withdrawal syndrome, they immediately return to the use of the drug and in the future it is canceled gradually, replacing with other antihypertensive drugs. To prevent withdrawal syndrome, the drug should not be prescribed to patients who do not have the conditions for its regular use.

If the combined use of clonidine and a blocker of β-adrenergic receptors requires a temporary discontinuation of treatment, then the blocker of β-adrenergic receptors must be canceled earlier in order to prevent sympathetic hyperreactivity, and then gradually cancel clonidine, especially if it was used in large doses.

Clonidine is prescribed with caution in patients with diabetes mellitus, because clonidine may mask symptoms of hypoglycemia and decrease insulin secretion. In patients with diabetes mellitus, an increase in the dose of hypoglycemic drugs may be required.

Clonidine and its metabolites are largely excreted in the urine. The dose of the drug must be adjusted in accordance with the individual patient's response to treatment, which can vary significantly in patients with renal insufficiency; careful monitoring is necessary. Because only small amounts of clonidine are removed during hemodialysis, no additional drug intake is necessary.

The drug is prescribed with caution to elderly patients - hypersensitivity to the drug is possible; patients with renal insufficiency - a delay in elimination of the drug is possible. A transient increase in the concentration of growth hormone is possible. The use of clonidine can lead to a decrease and inhibition of salivation, which contributes to the development of caries, periodontal disease, candidiasis of the oral cavity.

Patients using contact lenses should remember that the drug reduces the production of tear fluid.

When treating with clonidine, it is recommended to regularly monitor blood pressure. Care should be taken with prolonged physical activity, especially in an upright position in hot weather, due to the risk of orthostatic reactions.

Serious adverse reactions, including sudden death, have been reported when used with methylphenidate. The safety of methylphenidate with clonidine has not been systematically evaluated.

The medicinal product contains lactose, therefore patients with rare hereditary galactose intolerance, Lapp lactase deficiency or impaired absorption of glucose / galactose should not take this medicinal product.

Application in pediatrics.For adolescents over 15 years of age, the drug is prescribed with extreme caution because of the danger of overdose: toxic effects in children are possible when taking 0.1 mg of clonidine.

Influence on the ability to drive vehicles and other potentially dangerous mechanisms.During drug therapy, potentially dangerous activities requiring increased attention, rapid mental and motor reactions should be avoided.

Release form

10 tablets in a blister; 50 tablets in jars. Each can or three; five contour packs, together with instructions for use, are placed in a cardboard box.
Hospital packaging: 15 cans with the appropriate number of instructions for use are placed in a cardboard box.

Storage conditions

In a place protected from moisture and light at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

Do not use after the expiration date printed on the package.

Terms of dispensing from pharmacies

On prescription.

Clonidine analogs, synonyms and group drugs

Self-medication can be harmful to your health.
It is necessary to consult a doctor, and also read the instructions before use.

The combined action of Clonidine with alcohol leads to a violation of the cardiovascular and persistent suppression of the central nervous system. At best, this is manifested by heavy and prolonged sleep, at worst - a deep coma.

Properties of the drug

The drug belongs to the group of blockers of alpha-2 adrenergic receptors, which are located in the nuclei of the medulla oblongata, which regulate blood pressure. Under normal conditions, irritation of these receptors stimulates the production of norepinephrine, a neurotransmitter of the sympathetic nervous system.

The vasomotor center sends impulses to the adrenal glands, which produce adrenaline and norepinephrine. This increases blood pressure, increases physical activity, narrows the pupils, and increases the heart rate. The human body is mobilized to perform specific tasks.

Clonidine is completely absorbed in the gastrointestinal tract, enters the vessels, moves through them to the brain, without interacting with any other substances. The drug targets exclusively the alpha-2 adrenergic receptors in it.

Unlike other medicines that lower blood pressure, Clonidine works exclusively through the central nervous system. Blocked medulla oblongata receptors do not respond to changes in the biochemical composition of the flowing blood.

In therapeutic doses, the action of the drug leads to the following effects:

• lowering blood pressure;
• decreased heart rate;
• lowering intraocular pressure;
• slight dilation of the pupils;
• dryness of the conjunctiva;
• muscle relaxation;
• constipation;
• sleepiness.

Due to the fact that Clonidine freely penetrates the blood-brain barrier (BBB), an increased dose of the drug quickly acts on the cerebral cortex. The patient may develop auditory and visual hallucinations.

Clonidine has an international non-trade name - Clonidine, which acts in a similar way. Preparations under any brand name that contain this substance cause the effects of Clonidine.

According to pharmacokinetic studies, Clonidine penetrates not only into the brain and blood vessels of the placenta, but also into breast milk. The half-life of the drug varies in the following time intervals: from two hours to a day.

That is, that is how long Clonidine is in the active state in the blood. The half-life in women lasts longer than in men. The drug is not recommended to be taken until the age of 18, during pregnancy and lactation.

Under normal conditions, the action of Clonidine begins in half an hour, with intravenous administration or inside in drops, a drop in blood pressure is noted after 3-5 minutes.

The drug is excreted in the urine, therefore, in people with renal insufficiency, the effect of Clonidine lasts longer than one day.

The full compatibility of Clonidine with antiplatelet agents and cardioprotectors has been proven. If you drink the drug for a long time, pathological heart hypertrophy decreases.

Methods and indications for admission

The tool is used in tablets, in a solution for intravenous injection, drops into the conjunctival sac. The concentration of solutions for the eyes and for intravascular administration is the same and is 0.1 milligrams. The tablet contains a safe oral dosage of 0.075 mg. If necessary, the dose is doubled, and a tablet is prescribed, which contains 0.15 mg. The ophthalmologist usually prescribes no more than one drop.

The drug is used to treat hypertension. The remedy is used in cases where no other medicine works, or to provide emergency medical care in a hypertensive crisis.

With the help of Klofelin, narcologists stop the state of intoxication with alcoholism and drug addiction.

The end of treatment is carried out gradually using a safe dosage reduction method. Since with a sharp cessation of taking Clonidine, a withdrawal syndrome is noted, which is manifested by the following symptoms:

• increased blood pressure;
• headache;
• nausea;
• irritability.

Alcohol and Clonidine

Consumption of alcoholic beverages at the same time as Clonidine is strictly prohibited. The lethal dose of Clonidine and alcohol does not have a clear numerical designation. A lethal outcome is possible from one tablet, and from several eye drops (the solution has the same dosage as for intravenous administration) if they are drunk with alcohol.

How alcohol affects the effect of the drug

Ethanol, like Clonidine, freely penetrates through the vascular wall into the brain. If you drink both substances at the same time, you can get poisoned.

Ethyl alcohol tenfold enhances the effect of Clonidine, causing an overdose at the smallest doses of the drug. In case of an overdose, the vasomotor center is turned off, which leads to cardiac arrest and respiratory arrest.

Clonidine and alcohol - from the point of view of clinical pharmacology - are incompatible substances. From the point of view of chemical interaction, taking Clonidine with vodka, as well as with other drinks containing ethanol (wine or beer), has a synergistic effect - they enhance the effect of each other.

For example, Clonidine and beer cause severe alcohol intoxication from one mug. Even one drop of the drug can be fatal if mixed with vodka or wine.

Poisoning symptoms

Poisoning with Clonidine and ethanol is manifested by signs of an overdose:

• lowering blood pressure;
• slowing down the pulse;
• strong intoxication - inadequate amount of alcohol consumed;
• dizziness;
• lethargy;
• dilated pupils;
• dry mouth;
• drowsiness;
• muscle lethargy;
• loss of coordination and orientation in space;
• respiratory depression;
• loss of consciousness;
• cardiac arrest.

A terrible complication in the form of respiratory arrest and heart failure occurs against the background of pathological sleep. It is very difficult to wake up a person who has taken an alcoholic drink with Clonidine. The condition is similar to narcotic sleep and requires resuscitation. Health workers need to act decisively to avoid unpleasant consequences.

Consequences of simultaneous reception

The consequences of taking Clonidine and alcohol are determined by the degree of poisoning. If the amount of the drug in the blood is insignificant, and the dose of alcohol is small, there are times when a person just falls asleep during a banquet, and in the morning he feels a strong hangover.

The effect of the drug on the body is insignificant. With moderate poisoning, a person falls asleep at the table, but responds to loud sounds, comes to his senses, is able to move independently. The condition resembles a severe degree of intoxication with a relatively low amount of alcohol consumed.

In case of severe poisoning, sleep overtakes a person in any position, who has taken a dose of Clonidine with vodka, loses consciousness and faints. In this case, the victim needs urgent medical attention. You can drink Clonidine no earlier than a day after the alcohol party.