Clofelin 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. The role of the active ingredient of the drug is clonidine hydrochloride.

In this article, we will look at what doctors prescribe for clopheline, including instructions for use, analogues and prices for this drug in pharmacies. The real testimonials of people who have already taken advantage of clonidine can be read in the comments.

Composition and release form

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

• The active ingredient is clonidine.

Pharmacological group: alpha adrenomimetiki.

Indications for use

The indications for the use of the drug include:

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

pharmachologic effect

Clopheline in a short period of time reduces blood pressure, normalizes the number of heartbeats, has a positive effect on the central nervous system, and also reduces intraocular pressure.

The main function of the analyzed drug performs due to the excitation of postsynaptic alpha 2-adrenergic receptors of special inhibitory structures located in the brain. In addition, the instructions to Clofelin noted that this tool reduces sympathetic impulses, suitable to the heart and the entire vascular network.

Instructions for use

According to the instructions for use Tablets clonidine take, regardless of the meal, 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 hypertension, clofelin is taken 2-3 times a day. The initial 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 in excess of 0.3 mg can be prescribed only in exceptional cases and, preferably, in the hospital. 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, the treatment is supplemented with saluretics or other antihypertensive drugs (except nifedipine). Older patients, especially with manifestations of cerebrovascular disease, recommended an initial dose of 0.0375 mg 2-3 times a day.
• For hypertension, take clofelin tablets 3 times a day for 0.075 mg. During the course of treatment, the dose may subsequently be increased. In elderly and senile age as an additional treatment of atherosclerotic events. Repeal the drug sequentially, reducing the dosage of the drug in stages.

Therapeutic treatment of glaucoma with the use of eye drops. Clonidine suggests instillation of 1 drop three times a day into each conjunctival channel, unless a different dosage is prescribed by the ophthalmologist. If the intraocular pressure does not drop when a 0.25% solution of the drug is instilled, Clofelin is administered with a concentration of 0.5%. With pronounced side effects, the concentration of clopheline should be reduced to 0.125%.

Contraindications

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

1. Hypotension;
2. Obliterating diseases of peripheral arteries;
3. Depression (including historical data);
4. Severe sinus bradycardia;
5. Cardiogenic shock;
6. Sick sinus syndrome (SSS);
7. The simultaneous use of ethanol and other means of depressing the central nervous system (CNS);
8. The combined use of tricyclic antidepressants;
9. AV block II and III degree;
10. Pregnancy and breastfeeding period;
11. Hypersensitivity to the components of the tool.
12. Contraindications for the use of eye drops:
13. Hypotension;
14. Pronounced atherosclerosis 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 I degree.

Side effects

Side effects usually occur in the first days of taking the drug:

• dizziness;
• sexual disorders;
• weight gain;
• constipation;
• nausea, vomiting;
• slow heart rate;
• nightmares;
• dry mouth;
• weakness;
• drowsiness and lethargy;
• feeling tired;
• fainting.

With proper determination of the frequency of reception and dose of clopheline side effects gradually disappear.

Analogs

Analogs of clonidine:

• Hemiton;
• Chlofazolin;
• Catapresan;
• Clonidine hydrochloride.

Attention: the use of analogues should 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 of white or almost white color, flat-cylindrical, with a facet.

pharmachologic effect

Clophelin is an antihypertensive agent whose effect is associated with the effect on the neurogenic regulation of vascular tone.

Clophelin stimulates α2-adrenoreceptors, lowers the tone of the vasomotor center of the medulla oblongata, and reduces impulses in the sympathetic component of the peripheral nervous system at the presynaptic level.

The main manifestation of the effect of clonidine is the hypotensive effect, usually developing 1-2 hours after taking the drug inside and continuing after a single dose for 6-8 hours. The hypotensive effect of clofelin is accompanied by a decrease in cardiac output and a decrease in peripheral resistance of blood vessels, including kidney 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) the somatovegetative manifestations of opiate and alcohol withdrawal. The feeling of fear diminishes, cardiovascular and other disorders gradually pass. These effects are believed to be largely due to the effect of clonidine on central α2-adrenoreceptors.

Pharmacokinetics

Clophelin is rapidly and completely absorbed from the gastrointestinal tract; peak plasma concentrations are observed after 1.5-2.5 hours. The half-life is 12-16 hours with normal renal function and up to 41 hours if it is impaired. Easily penetrates histohematogenous barriers (hematoencephalic, ophthalmic, and others). Binding to plasma proteins - 20-40%. Metabolized in the liver (about 50% of the absorbed dose). Excreted mainly by the kidneys - 40-60% unchanged, through the intestines - 20%.

Indications for use

Treatment of hypertensive crisis.

Contraindications

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

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

Pregnancy and lactation period

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

Dosage and administration

Assign adults inside, regardless of the meal.

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

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

Patients with renal failure.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 considerably in this category of patients; careful monitoring is required.

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

Side effect

The frequency of side effects is given in the following grades: 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).

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

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

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

On the part of the respiratory system: rarely:nasal congestion.

On the part of the endocrine system: rarely:gynecomastia.

From the skin and subcutaneous tissue: infrequently:skin rash, urticaria, itching; seldom:alopecia.

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

General violations: often:fatigue; infrequently:malaise.

From the laboratory indicators: rarely:increased blood glucose levels; very rarely:change in liver function tests.

Overdose

Symptoms:constriction of the pupils (miosis), general weakness, bradycardia, 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 be observed when taking doses in excess of 10 mg.

Treatment:there is no specific antidote for overdose of clonidine. If necessary, it is possible to receive activated carbon. Maintenance therapy includes the introduction of atropine sulfate in bradycardia, inotropic sympathomimetics for hypotension. In severe hypertension, correction with α-adrenoreceptor blockers is possible. In case of clonid-induced respiratory depression, naloxone is administered.

Interaction with other drugs

It is not recommended to use clonidine together with antidepressants (weakening of the hypotensive effect) and with neuroleptics (increased sedation, there may be pronounced depressive disorders). It should not be used simultaneously with benzodiazepines due to the recent increase in the depressive effect of clonidine. The hypotensive effect of clonidine is reduced under the influence of nifedipine (antagonism in the effect on the intracellular current of Ca 2+ ions). When using clonidine along with vasodilators, diuretics and antihistamines, its hypotensive effect is enhanced. In combination with quinidine, it causes marked bradycardia. It is impractical to combine the use of clonidine with methyldopa (dopegitom), guanfacin, antacid agents. Clofelin enhances the inhibitory effect of ethanol on the central nervous system; enhances the specific effect of ketamine, narcotic analgesics, droperidol. In combination with thiopental sodium, enflurane, isoflurane, it can cause marked bradycardia and hypotension. Α 2 -adrenoreceptor antagonists, such as mirtazapine, can level clonidine-mediated effects on α 2 -adrenoreceptors; this relationship is dose-dependent. Clofelin can not be used in conjunction with adrenaline, noradrenaline, reserpine, phenothiazines (aminazin), oral hypoglycemic agents. Non-steroidal anti-inflammatory drugs reduce the antihypertensive effect of clonidine. Concurrent use with β-adrenoblockers or cardiac glycosides (digoxin) increases the risk of atrioventricular blockade and severe bradycardia. When conducting therapy with clofelin in combination with β-blockers, in order to avoid an undesirable increase in blood pressure in case of cessation of therapy, you must first gradually end treatment with β-blockers, and then also by slow dose reduction to stop taking clonidine. weakening of the hypotensive effect) and with neuroleptics (increased sedative effect, the occurrence of pronounced depressive disorders may occur). It should not be used simultaneously with benzodiazepines due to the recent increase in 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 using clonidine along with vasodilators, diuretics and antihistamines, its hypotensive effect is enhanced. In combination with quinidine, it causes marked bradycardia. It is impractical to combine the use of clonidine with methyldopa (dopegitom), guanfacin, antacid agents. Clofelin enhances the inhibitory effect of ethanol on the central nervous system; enhances the specific effect of ketamine, narcotic analgesics, droperidol. In combination with thiopental sodium, enflurane, isoflurane, it can cause marked bradycardia and hypotension. Α 2 -adrenoreceptor antagonists, such as mirtazapine, can level clonidine-mediated effects on α 2 -adrenoreceptors; this relationship is dose-dependent. Clofelin can not be used in conjunction with adrenaline, noradrenaline, reserpine, phenothiazines (aminazin), oral hypoglycemic agents. Non-steroidal anti-inflammatory drugs reduce the antihypertensive effect of clonidine. Concurrent use with β-adrenoblockers or cardiac glycosides (digoxin) increases the risk of atrioventricular blockade and severe bradycardia. When conducting therapy with clofelin in combination with β-blockers, in order to avoid an undesirable increase in blood pressure in case of cessation of therapy, you must first gradually end treatment with β-blockers, and then also by slowly reducing the dose, stop taking clonidine.

Precautionary measures

Special care should be taken in patients with depression or cerebrovascular diseases, since 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 with pheochromocytoma.

During treatment it is forbidden to consume alcoholic beverages.

Sudden cessation of the drug can lead to the development of withdrawal syndrome (especially in patients taking more than 0.9 mg / day): high blood pressure, nervousness, headache, nausea, therefore, the drug should be discontinued only gradually over 1-2 weeks from considering concomitant therapy with other drugs. With the development of withdrawal syndrome, they immediately return to the use of the drug and are subsequently canceled gradually, replacing with other antihypertensive drugs. To prevent withdrawal of 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 the β-adrenoreceptor blocker requires a temporary cessation of treatment, then the β-adrenoreceptor blocker must be canceled earlier in order to prevent sympathetic hyperreactivity, and then gradually cancel clonidine, especially if it was used in large doses.

With caution prescribed clonidine patients with diabetes, because clonidine may mask the symptoms of hypoglycemia and reduce insulin secretion. Patients with diabetes may need to increase the dose of hypoglycemic drugs.

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

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

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

When treating clonidine, it is recommended to regularly monitor blood pressure. Caution should be exercised during prolonged physical exertion, 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 together with methylphenidate. The safety of using methylphenidate with clonidine has not been systematically evaluated.

The drug contains lactose, so patients with rare hereditary intolerance to galactose, Lappa lactase deficiency, or impaired glucose / galactose absorption should not take this drug.

Pediatric use.Adolescents over 15 years old are prescribed the drug with extreme caution because of the danger of an overdose: a toxic effect in children is possible when taking 0.1 mg clonidine.

Impact on the ability to drive motor vehicles and other potentially dangerous machinery.During drug therapy, you should avoid potentially hazardous activities that require increased attention, quick mental and motor reactions.

Release form

10 tablets in a blister pack; on 50 tablets in banks. Each can or three; five planimetric packagings together with the application instruction are placed in a pack from a cardboard.
   Packaging for hospitals: 15 cans with the appropriate number of instructions for use are placed in a cardboard box.

Storage conditions

In the place protected from moisture and light at a temperature not higher than 25 ° C.

Keep out of the reach of children.

Shelf life

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

Pharmacy sales terms

On prescription.

Clofelin analogues, synonyms and drugs of the group

Self-medication can be detrimental to your health.
   You must consult with your doctor, as well as read the instructions before use.

The combined effect of clopheline with alcohol leads to a violation of the cardiovascular and persistent suppression of the central nervous system. At best, this manifests itself in a heavy and prolonged sleep, at worst - in a deep coma.

Drug properties

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

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

Clopheline is completely absorbed in the gastrointestinal tract, enters the blood vessels, moves along them to the brain, without interacting with any other substances. The drug targets exclusively alpha-2 adrenoreceptors in it.

Unlike other blood pressure lowering medications, Clofelin acts exclusively through the central nervous system. The blocked receptors of the medulla oblongata do not respond to changes in the biochemical composition of the blood flowing.

At therapeutic doses, the effect of the drug leads to the following effects:

• lower blood pressure;
• decrease in heart rate;
• lowering intraocular pressure;
• slight pupil dilation;
• conjunctival dryness;
• muscle relaxation;
• constipation;
• drowsiness.

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

Klofelin has an international non-commercial name - Clonidine, which acts similarly. Preparations under any trade name that contain this substance cause the effects of clofelin.

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

That is, so much time is clophelin in the blood in an active state. The half-life in women lasts longer than in men. The drug is not recommended to take until the age of 18, during pregnancy and lactation.

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

The drug is excreted in the urine, so in people with renal insufficiency, the action of clonidine lasts longer than one day.

Proved full compatibility of clonidine with antiplatelet agents and cardioprotectors. If you drink the drug for a long time, pathological hypertrophy of the heart decreases.

Methods and indications for admission

Means is applied in tablets, in solution for intravenous injections, drops in a conjunctival sac. The concentration of solutions for the eyes and for intravascular administration is the same and amounts to 0.1 milligram. The tablet contains a safe dosage for oral administration, which is 0.075 mg. If necessary, the dose is doubled, and a pill is prescribed, which contains 0.15 mg. An ophthalmologist usually prescribes no more than one drop.

The drug is used to treat hypertension. The tool is used in cases where no other medicine is not valid, or to provide emergency medical care for hypertensive crisis.

With the help of Clofelin, narcologists stop the state of intoxication during alcoholism and drug addiction.

The end of treatment is carried out gradually, using a safe method to reduce the dosage. Since abrupt discontinuation of clonidine, withdrawal syndrome is observed, which manifests itself in the following symptoms:

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

Alcohol and Clofelin

Reception of alcoholic beverages simultaneously with clonidine is strictly prohibited. Lethal dose of clofelin and alcohol does not have a clear numeric designation. Fatal 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 Clofelin, freely passes through the vascular wall into the brain. If you drink both substances at the same time, you can get poisoned.

Ethyl alcohol enhances the action of clonidine dozens of times, causing an overdose at the lowest doses of the drug. An overdose turns off the vasomotor center, which leads to cardiac arrest and respiration.

Clopheline and alcohol - from the point of view of clinical pharmacology - are incompatible substances. From the standpoint of chemical interaction, the intake of clofelin with vodka, as well as with other beverages containing ethanol (wine or beer), has a synergistic effect - they reinforce the action of each other.

For example, Clofelin and beer cause severe intoxication from a single mug. Even one drop of the drug can be fatal to the body if mixed with vodka or wine.

Symptoms of poisoning

Poisoning with clofelyn and ethanol is manifested by signs of overdose:

• lowering blood pressure;
• slow pulse;
• severe intoxication - inadequate amount of alcohol consumed;
• dizziness;
• lethargy;
• dilated pupils;
• dry mouth;
• sleepiness;
• 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 arises against the background of pathological sleep. It is very difficult to wake up a person who took alcohol with clonidine. The condition is similar to a narcotic sleep and requires resuscitation. Health workers need to act decisively to avoid unpleasant consequences.

Consequences of simultaneous reception

The effects of taking clofelin 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 cases when a person just falls asleep during a banquet, and in the morning feels a strong hangover.

The effect of the drug on the body is insignificant. With a moderate severity of poisoning, a person falls asleep at the table, but responds to loud noises, comes to himself, 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, having taken a dose of von Clofelin with vodka, faints and faints. In this case, the victim needs urgent medical care. Clonidine can drink no earlier than a day after the alcohol party.