Clonidine-Darnitsa tablets 0.15 mg No. 50 (10x5)

Pharmacodynamics and pharmacokinetics

What is Clonidine? The active substance, clonidine , is a central alpha-adrenergic agonist. The mechanism of action is based on stimulation of postsynaptic alpha-2 adrenergic receptors located in the vasomotor center in the medulla oblongata, reducing the flow of sympathetic impulses at the presynaptic level to the heart and blood vessels. The drug reduces heart rate, reduces IOC, TPR. The drug has a central effect. With rapid intravenous infusion, a short-term decrease in blood pressure is recorded, caused by stimulation of postsynaptic alpha1-adrenergic receptors located in the walls of blood vessels. Clonfelline reduces blood flow in the brain, increases the tone of cerebral vessels, increases renal blood flow, and has a pronounced sedative effect. The drug is effective for 6-12 hours. When clonidine is instilled into the conjunctival sac, a drop in intraocular pressure is observed. The effect is explained by stimulation of adrenergic receptors upon local contact, which leads to a decrease in the production of intraocular fluid, improvement of its outflow, and weakening of sympathetic tone.

Clonidine-Darnitsa tablets 0.15 mg No. 50 (10x5)

During treatment with clonidine, it is prohibited to drink alcoholic beverages.

Sudden cessation of use of the drug can lead to the development of withdrawal syndrome (increased blood pressure, nervousness, headache, nausea), so discontinuation of the drug should be carried out only gradually, over 1-2 weeks, taking into account concomitant therapy with other drugs.

Withdrawal syndrome may develop 18-72 hours after taking the last dose of the drug. If withdrawal syndrome develops, you should immediately return to the use of the drug and subsequently discontinue it gradually, replacing it with other antihypertensive drugs. Cases of hypertensive encephalopathy, cerebrovascular accident and death have been reported after abrupt discontinuation of the drug. The likelihood of such a reaction to discontinuation of drug therapy increases with the use of high doses or with continued concomitant therapy with beta-blockers, so special caution is recommended in such cases. 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 beta-adrenergic blocker requires temporary discontinuation of treatment, the beta-adrenergic blocker should be discontinued earlier in order to prevent sympathetic hyperreactivity, and then gradually discontinue clonidine, especially if it was used in large doses.

Prescribe with caution to patients with polyneuropathy and constipation.

Patients should be warned that the sedative effect of the drug is enhanced by concomitant use of barbiturates or other sedative drugs.

Prescribe Clonidine-Darnitsa with caution to patients with diabetes mellitus, since clonidine can mask the symptoms of hypoglycemia and reduce insulin secretion. Prescribe with caution to elderly patients - increased sensitivity to the drug is possible; in patients with renal failure, there may be a delay in the elimination of the drug. A transient increase in the concentration of growth hormone is possible. The use of clonidine can lead to a decrease and suppression of salivation, which contributes to the development of caries, periodontal disease, and oral candidiasis.

Ineffective for pheochromocytoma.

Taking Clonidine-Darnitsa can lead to an acute attack of porphyria and is considered dangerous for patients with porphyria.

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

When treating with Clonidine-Darnitsa, it is recommended to regularly monitor blood pressure. You should be careful with prolonged physical activity, especially in an upright position, in hot weather due to the risk of orthostatic reactions. The development of a weakly positive Coombs reaction is possible.

The medicine contains lactose. Patients with rare hereditary problems of galactose intolerance, lactase deficiency or Lapp glucose-galactose malabsorption should not take this medicine.

Use during pregnancy or breastfeeding.

Data on the use of clonidine in pregnant women are limited. Clonidine should not be used during pregnancy, especially during the first trimester, unless the expected benefit to the mother outweighs the risk to the fetus. During pregnancy, the drug should be taken only after a doctor's prescription. Careful monitoring of the condition of the mother and child is necessary when using clonidine.

During pregnancy, preference should be given to the oral form of clonidine; intravenous administration should be avoided.

Clonidine crosses the placental barrier and may reduce the fetal heart rate. A postpartum transient rise in blood pressure in newborns cannot be excluded.

The results of preclinical studies do not indicate the existence of direct or indirect harmful effects on reproductive function.

If it is necessary to use the drug, breastfeeding should be stopped.

The ability to influence the speed of reactions when driving vehicles or other mechanisms.

During treatment, you should refrain from driving vehicles and engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Indications for use

Clonidine - what is it for? It is used for hypertensive crisis , for arterial hypertension (including kidney pathology), for pheochromocytoma (for diagnosis), for acute myocardial infarction (if symptoms of cardiogenic shock are not diagnosed), for dysmenorrhea , headaches of vascular origin, for withdrawal syndrome in patients with drug addiction (complex treatment), Gilles de la Tourette syndrome, nicotine addiction. Clonidine eye drops are used for primary open-angle glaucoma.

Side effects of Clonidine

Digestive tract: loss of appetite, dry mouth, decreased secretion of gastric juice, constipation , vomiting, nausea.

Nervous system: “nightmare”, vivid dreams, depression, nervousness, anxiety, slower speed of motor and mental reactions, drowsiness, asthenia .

Cardiovascular system: short-term decrease in blood pressure during intravenous infusion, orthostatic hypotension, bradycardia.

Side effects from the genitourinary system: decreased libido, impaired potency. It is possible to develop a “hemitonic crisis” with abrupt discontinuation of the drug, swelling of the ankles, and Raynaud’s syndrome .

When using eye drops topically, there is a burning sensation in the eyes and dryness of the conjunctiva. The most common systemic reactions are: bradycardia, constipation, drowsiness.

Clonidine

All information is provided for informational purposes only and does not constitute medical advice. The system, methods, methods of treatment, necessary medications can only be prescribed by your attending physician.

Clonidine (Clophelinum) is one of the antihypertensive drugs used to lower blood pressure (BP).

Active substance

The active substance in Clonidine is Clonidine hydrochloride (Clonidini hydrochloridum) or 2,6-dichloro-N-2-imidazolidinylidenebenzenes.

Clonidine belongs to the group of imidazoline derivatives, and has the chemical formula C9H9Cl2N3.

According to physical properties, it is a white crystalline powder. It is highly soluble in water, but poorly soluble in organic solvents: ethyl alcohol, chloroform, and ether.

Mechanism of action

This is an antihypertensive drug with a central mechanism of action. Its ability to lower blood pressure is associated with its effect on certain brain structures, namely the vasomotor center of the medulla oblongata.

Here are neurons, impulses from which lead to an increase in blood pressure by spasm of peripheral small arteries (arterioles). These neurons are elements of the sympathetic nervous system. In this way, the sympathetic system realizes its hypertensive effect aimed at increasing blood pressure.

In addition, under the influence of sympathetic impulses, the frequency and strength of heart contractions increases, which also leads to an increase in blood pressure. The conduction of these impulses through synapses (contacts between neurons) is ensured by norepinephrine. Clonidine does not affect the synthesis of norepinephrine in presynaptic (located in front of the synapse) neurons.

But under its influence, the reserves of norepinephrine in presynaptic neurons are quickly depleted. This mechanism is realized due to its effect on alpha-2 adrenergic receptors in the central neurons of the vasomotor center.

As a result, the release of norepinephrine is inhibited, the inhibitory neurons of the vasomotor center are activated, and the conduction of sympathetic impulses to the vessels is blocked.

In a similar way, it inhibits the synthesis of adrenaline in the adrenal medulla. Adrenaline, like norepinephrine, belongs to the group of catecholamine substances that play an important role in the development of hypertension. In addition, under its emission, the vagus nerve, which belongs to the parasympathetic nervous system, is activated.

This part of the autonomic nervous system is an antagonist of the sympathetic system with directly opposite effects, including hypotension. Its hypotensive effect is manifested by expansion of the lumen of arterioles, a decrease in their peripheral resistance, and a decrease in the frequency and strength of heart contractions.

The last factor is associated with the elimination of myocardial hypertrophy during long-term use of the drug, because the load on the heart muscle is reduced.

Clonidine hydrochloride owes its central action to its ability to penetrate the BBB (blood-brain barrier) between the blood and the brain matter. The effect on brain structures, in addition to hypotension, also manifests itself in other effects.

First of all, it is analgesia - pain relief. Analgesia is achieved through inhibition of central sensitive pain receptors - nociceptors. It potentiates, enhances anesthesia. Therefore, it can be used as an adjuvant (auxiliary) agent during general anesthesia.

In addition, under its influence, sedation develops - calmness, disappearance of anxiety and fear. By influencing nociceptive structures, it is able to reduce the severity of withdrawal syndrome caused by alcohol abuse and the use of various narcotic substances, incl. and opiates.

However, it does not bind to opiate receptors, and addiction does not develop to it. There is evidence of its effect on the thermoregulation centers of the brain, resulting in a decrease in high temperature. However, the antipyretic power of the drug is small.

Among the peripheral effects of Clonidine is an improvement in renal blood flow due to dilation of the renal arteries during hypotension, as well as a decrease in IOP (intraocular pressure). The decrease in IOP is due to a decrease in the production of intraocular fluid and an improvement in its outflow due to sympathetic blockade.

It stimulates not only central alpha-2 adrenergic receptors, but also peripheral alpha-1 adrenergic receptors in arterioles, which leads to their spasm. In this case, short-term hypertension develops, which is then replaced by hypotension.

This two-phase effect on blood pressure is more typical for injection forms, and is practically not observed when using tablets. Large jumps in blood pressure are extremely undesirable for patients with myocardial infarction and cerebrovascular accident.

It should be borne in mind that Clonidine, penetrating the BBB, can cause cerebral vasospasm. The feeling of dry mouth is also associated with its stimulation of peripheral adrenergic receptors.

Over time, addiction develops to it, manifested in a decrease in antihypertensive activity and the need to increase doses. There is evidence that long-term use, especially in elderly patients, can lead to senile dementia - Alzheimer's disease.

Interesting Facts

It is known to many not only as a medicine. It gained its notorious fame thanks to its widespread use in criminal practice. In this regard, songs, publications, and feature films are named after him.

Its use for evil purposes is based on its hypotensive and sedative effects, which are enhanced in combination with alcohol. After all, alcohol initially dilates cerebral vessels, and Clonidine penetrates the BBB better and in greater quantities.

As a result of a rapid drop in blood pressure, depression of consciousness and a decrease in cardiac activity, “the client passes out.” This condition has varying degrees of severity, including death.

It is especially difficult to take liquid forms in combination with alcohol. Unlike tablets, liquid Clonidine (injection solution, eye drops) dissolves better in ethyl alcohol.

History of creation

It was synthesized in the 60s of the last century. At first it was planned as a remedy for the common cold due to its peripheral adrenergic stimulating effect and the ability to spasm the capillaries of the nasal mucosa. However, its hypotensive properties were immediately noted.

It was used as an antihypertensive drug for several decades in the USSR and abroad. The peak of its popularity was in the late 70s and early 80s. It was often combined with other drugs - Raunatin, Octadine, Reserpine, which were widely used in those days to treat arterial hypertension.

Subsequently, its use decreased sharply, and its injectable form practically disappeared from the pharmacy chain. This is due to the criminal component, but only partly.

Further use was limited by its hemodynamic and central nervous system side effects. In addition, progressive methods of treating hypertension have been developed using new, more effective drugs.

Currently, its tablets are rarely used, mainly when it is necessary to lower blood pressure in a short time.

Synthesis technology

Clonidine hydrochloride is produced through chemical reactions involving one or more biodegradable polymers. In addition to the main active substance, the following are used in the production of solid tablet forms: lactose, magnesium stearate, corn starch. These substances act as fillers.

Release forms

• extended-release tablets 0.000075 g (75 mcg) and 0.00015 g (150 mcg);
• Ampoules 1 ml 01% solution for injection;
• Tube droppers 1.5 ml of 0.125%, 0.25% and 0.5% solution in the form of eye drops.

It is produced under the names Clonidine and Clonidine (Apo-Clonidine, Clonidine-M) by many pharmaceutical companies in Russia and Ukraine.

In addition to Clonidine, other generics have been and are used in the USSR and Russia, in which Clonidine acts as the active ingredient:

• Catapresan – tab., solution for injection, Boehringer Ingelheim (Germany), Zdravle (Yugoslavia);
• Chlofazolin – tab., Farmakhim (Bulgaria);
• Barklid – tab., Biogalenika Laboratory, France;
• Gemiton – tab., AVD, Germany.

The weight of tablets and the concentration of the injection solution are the same for all generics. The quality of foreign medicines is better, but they are more expensive than their Russian counterparts.

Along with Clonidine, other centrally acting antihypertensive drugs are also used in medical practice. These are Rilmenidine (Albarel, Hyperdix), Moxonidine (Tensotran, Physiotens). Since the active ingredients in these drugs are different, they differ in their characteristics and mechanism of action from Clonidine.

Dosages

75 mcg is prescribed orally 2-4 times a day. If necessary, the dose is gradually increased by 37.5 mcg every 1-2 days, bringing it to 150-300 mcg per dose 3-4 times.

In some cases, the daily dose can be increased to 300-450 mcg. A further increase in dose is hardly justified. In these situations, it is recommended to combine Clonidine with diuretic drugs-saluretics.

The injection solution is administered intramuscularly, subcutaneously and intravenously. 0.5-1.5 ml is injected intramuscularly and subcutaneously. When administered intravenously, this amount is diluted in 10-20 ml of saline, and in order to avoid a rise in blood pressure, it is administered slowly over 3-5 minutes. At this time and 1.5-2 hours after administration, the patient should lie down, because collapse is possible.

Eye drops are instilled into the conjunctival sac, 1-2 drops 2-4 times a day. Start with a 0.25% solution. If the reduction in IOP is insufficient, switch to a 0.5% solution, and in case of side effects, switch to a 0.125% solution.

Treatment with tablets is carried out for a long time, for 6-12 months. You should not immediately cancel KGO - there may be a deterioration in the condition, an increase in blood pressure and hypertensive crises. Therefore, 7-10 days before stopping treatment completely, it is recommended to gradually reduce the dose, replacing it with other antihypertensive drugs.

Pharmacodynamics

The hypotensive effect develops 1-2 hours after oral administration, 15-20 minutes after intravenous administration, and lasts 6-8 hours. It is quickly absorbed into the gastrointestinal tract. Bioavailability is 65%, but can reach 100%.

The maximum concentration in blood plasma is formed 1.5-2.5 hours after ingestion. 20-40% of Clonidine ingested is bound to plasma proteins.

In the liver, 50% of it undergoes metabolic transformations. Excreted by the kidneys (40-60%) and through the intestines (20%). The half-life is 12-16 hours, but if renal function is impaired, it can increase to 41 hours.

Indications

• Arterial hypertension – primary, renal, hypertensive crises;
• Alcohol and drug withdrawal;
• Open-angle primary glaucoma (eye drops).

Side effects

• Cardiovascular system: hypotension, rarely – bradycardia, edema syndrome;
• Central nervous system: dizziness, weakness, drowsiness, nervousness, depression, paresthesia, slowing of mental and motor reactions;
• Eyes: dry conjunctiva, burning and itching in the eyes;
• Skin: allergic rash, itching;
• ENT organs: nasal congestion;
• Reproductive system: erectile dysfunction, decreased libido.

Contraindications

• Individual intolerance to Clonidine;
• Hypotension, shock, collapse;
• Sinus bradycardia (heart rate less than 50 beats/min);
• Second degree atrioventricular block;
• Sick sinus syndrome;
• Depressive states;
• Obliterating endarteritis;
• Atherosclerosis of cerebral vessels.

Its use is contraindicated when performing work that requires quick motor reactions, including while driving vehicles and working with complex, potentially dangerous machines and mechanisms.

Interaction

• Beta-blockers, Captopril - sudden withdrawal of Clonidine leads to a sharp increase in blood pressure;
• Hormonal contraceptives - enhance the sedative effect of Clonidine;
• Calcium channel blockers – conduction disturbances in the myocardium;
• Tricyclic antidepressants – reducing the hypotensive effect;
• Levodopa, Piribedil - decreased antiparkinsonian effect of these drugs;
• Prazosin – a violation of the hypotensive effect of Clonidine;
• Propranolol, Atenolol - increased hypotensive effect, dry mouth, sedation;
• Cyclosporine - increasing the concentration of this drug in the blood plasma;
• Ethyl alcohol – severe hypotension, toxic damage to the central nervous system.

Pregnancy and lactation

Clonidine is able to penetrate the placental barrier and into breast milk. This can cause negative changes in the cardiovascular system and central nervous system in the fetus. Therefore, it is contraindicated during pregnancy and during breastfeeding.

Storage

Store at a temperature not exceeding 250C. Shelf life: tablets - 4 years, ampoules - 3 years, tube droppers - 2 years. The drug is not dispensed without a doctor's prescription.

Material prepared by: Anesthesiologist-reanimatologist Andrey Anatolyevich Dotsenko
Last modified: 2020-12-1 Date of writing: 2015-08-26

Clonidine, instructions for use (Method and dosage)

The tablets are taken orally, regardless of meals. The initial dosage is 0.075 mg three times a day. If necessary, the dosage is increased to 0.9 grams per day.

Elderly patients with concomitant atherosclerosis are prescribed 0.0375 three times a day.

The drug is withdrawn gradually over two weeks.

Dysmenorrhea: 14 days before menstruation, as well as during the cycle, take 0.025 mg twice a day.

For hypertensive crisis, the medicine is used sublingually, intramuscularly, or intravenously at a dose of 0.15 mg. Before jet intravenous infusion, the drug is dissolved in sodium chloride and administered for 10 minutes.

According to the instructions for use, Clonidine eye drops are instilled 2-4 times a day into each conjunctival sac, 1-2 drops. Therapy begins with the use of a 0.25% solution. If the required level of intraocular pressure is not achieved, a 0.5% solution is used. When significant side effects are registered, the concentration of the solution is reduced to 0.125%.

Clonidine 15 mcg No. 30 tab.

Instructions for medical use of the drug CLOPHELINE-HEALTH Trade name Clonidine-Zdorovye International nonproprietary name Clonidine Dosage form Tablets, 0.15 mg Composition One tablet contains the active substance - clonidine hydrochloride 0.15 mg, excipients: lactose monohydrate, magnesium stearate, starch potato or corn. Description Tablets of white or white with a yellowish tint, flat-cylindrical shape with a chamfer. Pharmacotherapeutic group Antihypertensive drugs. Central agonists. Alpha2-adrenomimetics are central, imidozoline derivatives. Clonidine. ATC code C02AC01 Pharmacological properties Pharmacokinetics After oral administration, the hypotensive effect begins to appear within 30 - 60 minutes. The maximum effect develops after 2 - 4 hours and lasts for about 5 - 12 hours. The duration of action in some patients is 24 - 36 hours. It is well absorbed from the gastrointestinal tract, regardless of food intake, the maximum concentration in the blood plasma is achieved after 1.5 - 2.5 hours. Bioavailability with long-term use is about 65%. Binding to blood proteins – 20 – 40%. Metabolized in the liver (about 50% of the absorbed dose). The half-life with normal renal function is 12–16 hours, with impaired renal function it increases to 41 hours. It easily passes through histohematic barriers, including the blood-brain and placental barriers, and penetrates into breast milk. It is excreted by the kidneys (40–60%), as well as through the intestines (20%). During hemodialysis, it is practically not released (up to 5%). Pharmacodynamics Clonidine-Zdorovye is an antihypertensive agent that acts at the level of neurohumoral regulation of vascular tone. After passing through the blood-brain barrier, clonidine selectively stimulates a2-adrenergic receptors in the nuclei of the vasomotor center of the medulla oblongata, inhibits sympathetic impulses from the central nervous system, causing vasodilation and a decrease in blood pressure. A decrease in sympathetic activity is accompanied by a decrease in the level of catecholamines (especially norepinephrine) in the blood plasma and urine, although clonidine does not have a direct effect on the synthesis of catecholamines, but inhibits the release of norepinephrine from nerve endings through a negative feedback mechanism as a result of stimulation of central α2-adrenergic receptors. Clonidine is an imidazoline receptor agonist. The use of clonidine leads to a decrease in heart rate, systolic and diastolic blood pressure, as well as total peripheral vascular resistance. Minute blood volume and stroke volume of the heart decrease slightly. Long-term use of clonidine leads to a decrease in myocardial hypertrophy and improvement in left ventricular function. Clonidine has a sedative and moderate analgesic effect. Due to its central action, it is able to eliminate somatovegetative manifestations of opiate and alcohol withdrawal. Clonidine lowers intraocular pressure by reducing secretion and improving the outflow of aqueous humor from the eye. Long-term use is accompanied by fluid retention in the body. Indications for use - hypertensive crises (with the exception of hypertensive crisis in pheochromocytoma) - arterial hypertension (as part of complex therapy) - withdrawal syndrome in opioid addiction (as part of complex therapy) Method of administration and dosage: Prescribed orally for adults, regardless of food intake. The dose should be selected strictly individually. The drug is withdrawn gradually over 1 to 2 weeks. Hypertensive crisis. Prescribe 0.15 - 0.3 mg (1 - 2 tablets) sublingually (in the absence of severe dry mouth). Arterial hypertension. The initial dose is usually 0.075 mg (clonidine preparations of other dosages) 2 times a day. If necessary, as directed by the doctor, the dose is gradually increased to an effective therapeutic dose, which averages 0.15 mg 2-3 per day. Single doses of clonidine above 0.3 mg can only be prescribed in exceptional cases and, if possible, in a hospital setting. The doctor determines the duration of treatment individually, depending on the course of the disease, clinical effectiveness and tolerability of the drug. Withdrawal syndrome. Prescribed in a hospital setting at a daily dose of 0.3 – 0.75 mg, divided into 4-6 doses with daily monitoring of blood pressure and pulse rate. Side effects - From the nervous system: headache, increased fatigue, drowsiness, dizziness, slower speed of mental and motor reactions, confusion, anxiety, nervousness, depression, anorexia, sleep disturbances, vivid or “nightmare” dreams, hallucinations, paresthesia, tremor - From the cardiovascular system: bradycardia or tachycardia, orthostatic hypotension, Raynaud's syndrome (pallor, cold extremities), atrioventricular block - From the digestive system: dry mouth, pain in the salivary glands, decreased appetite, nausea, vomiting, constipation , decreased gastric secretion, pseudo-obstruction of the colon, hepatitis - From the organs of vision: decreased production of tear fluid, impaired accommodation - From the respiratory organs: dry nasal mucosa, nasal congestion - Allergic reactions: skin rash, itching, alopecia, hyperemia, urticaria , angioedema. Extremely rarely with sublingual use - swelling of the mucous membranes, difficulty breathing. - From the genitourinary system: urinary retention, decreased libido and potency, gynecomastia, retention of sodium and water ions (manifested by swelling of the feet and legs) - From laboratory parameters: thrombocytopenia, hyperglycemia, changes in liver function tests Contraindications - increased individual sensitivity to clonidine or any of the auxiliary components of the drug - arterial hypotension - cardiogenic shock - atrioventricular block II and III degrees - severe bradycardia - sick sinus syndrome - coronary heart disease - recent myocardial infarction - cerebrovascular accident (including severe cerebral atherosclerosis) - severe disorders peripheral circulation - severe renal dysfunction - obliterating diseases of the peripheral arteries (including Raynaud's syndrome) - depressive states - simultaneous use of tricyclic antidepressants - pregnancy and lactation - children under 18 years of age Drug interactions When Clonidine-Zdorovye is used together with: - drugs , depressing the central nervous system - it is possible to increase the depressive effect on the central nervous system and the development of depressive disorders - tricyclic antidepressants, anorexigenic (except fenfluramine), sympathomimetic, non-steroidal anti-inflammatory drugs and nifedipine - weakening of the hypotensive effect of clonidine - vasodilators, diuretics, antihistamines - increased hypotensive effect of clonidine - β-blockers and cardiac glycosides - increased risk of developing bradycardia or (in some cases) atrioventricular block - atenolol, propranolol - development of additive hypotensive effect, sedation and dry mouth - hormonal contraceptives when taken orally - possible enhancement sedative effect of clonidine - levodopa and piribedil in patients with Parkinson's disease - a possible decrease in the effectiveness of levodopa and piribedil - cyclosporine - a possible increase in the concentration of cyclosporine in the blood - glucose - a possible increase in the concentration of glucose in the blood due to a decrease in insulin secretion Special instructions During treatment with clonidine, it is forbidden to use alcoholic drinks. Sudden cessation of use of the drug can lead to the development of withdrawal syndrome: increased blood pressure, nervousness, headache, nausea, so discontinuation of the drug should be carried out only gradually over 1 to 2 weeks, taking into account concomitant therapy with other drugs. If withdrawal syndrome develops, they immediately return to using the drug and subsequently discontinue it gradually, replacing it with other antihypertensive drugs. If the combined use of Clonidine-Zdorovye and a β-adrenergic receptor blocker requires temporary cessation of treatment, then the β-adrenergic receptor blocker should be discontinued earlier in order to prevent sympathetic hyperreactivity, and then gradually discontinue Clonidine-Zdorovye, especially. During treatment with Clonidine-Zdorovye, it is recommended to regularly monitor blood pressure. Caution should be exercised during prolonged physical activity, especially in an upright position in hot weather, due to the risk of orthostatic reactions. Clonidine-Zdorovye should be prescribed with caution to patients with diabetes mellitus, since clonidine can mask the symptoms of hypoglycemia and reduce insulin secretion. The drug is prescribed with caution to elderly patients - increased sensitivity to the drug is possible; for patients with renal failure - there may be a delay in drug elimination; with polyneuropathy; constipation During the use of clonidine, a transient increase in the concentration of growth hormone is possible; reduction and inhibition of salivation, which contributes to the development of caries, periodontal disease, and oral candidiasis; development of a weakly positive Kumbus reaction. Patients using contact lenses should remember that the drug may reduce tear production. The drug contains lactose, which should be taken into account in patients with rare hereditary forms of lactose intolerance, lactase deficiency, and glucose-galactose malabsorption syndrome. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms During drug therapy, potentially dangerous activities that require increased attention and rapid mental and motor reactions should be avoided. Overdose In case of overdose, the following symptoms may develop: drowsiness, miosis (severe constriction of the pupils), bradycardia, periodic vomiting, xerostomia, respiratory depression (up to apnea), impaired consciousness, collapse, decrease or increase in blood pressure, widening of the QRS complex on the electrocardiogram, hypothermia , possible slowing of atrioventricular conduction and early repolarization syndrome. Treatment: symptomatic therapy (fluid infusion, for severe depression of the central nervous system or apnea - 2 - 4 mg of naloxone intravenously, repeated if necessary). Tolazoline can be used as a specific antidote: 1 mg of tolazoline when administered intravenously or 50 mg when administered orally neutralizes the effect of 0.6 mg of clonidine. Release form and packaging 30 tablets each in a blister pack made of polyvinyl chloride film and aluminum foil. 1 contour package along with instructions for medical use in the state and Russian languages ​​in a cardboard box. Contour packages of 30 tablets without packaging, along with the appropriate number of instructions for medical use in the state and Russian languages, in corrugated cardboard boxes. Storage conditions Store in original packaging at a temperature not exceeding 25 o C. Keep out of the reach of children! Shelf life: 4 years Do not use the drug after the expiration date indicated on the package! Conditions for dispensing from pharmacies By prescription Manufacturer LLC “Pharmaceutical Company “Zdorovye”. Ukraine, 61013, Kharkov, st. Shevchenko, 22. Owner of the registration certificate of Pharmaceutical Company “Zdorovye” LLC, Ukraine. Address of the organization that accepts claims from consumers on the quality of products (products) on the territory of the Republic of Kazakhstan: Pharm-Euro LLP 050039, Almaty, st. Mailina, 72, apt. 34 Tel. Fax E-mail

Overdose

Manifested by slowing of atrioventricular conduction, decreased blood pressure, collapse, respiratory depression, impaired consciousness, widening of the QRS complex on the ECG, early repolarization syndrome , hypothermia, miosis, lethargy. Therapy is carried out syndromic.

Symptoms of poisoning with a substance: immersion in deep sleep or coma, depressed consciousness, blood pressure and pulse drop very strongly, mental disorder.

The lethal dose of Clonidine for humans is 50-100 mcg per kg of weight.

Interaction

The drug enhances the effects of medications that depress the central nervous system, ethanol. Antihistamines, diuretics , vasodilators enhance the effect of clonidine, and anorexigenic drugs, tricyclic antidepressants , sympathomimetics, NSAIDs, on the contrary, weaken the effectiveness. When prescribing cardiac glycosides and beta-blockers, the risk of developing atrioventricular block and bradycardia . Clonidine eye drops are not recommended to be prescribed with antipsychotics and antidepressants.

special instructions

In today's medical practice, Clonidine is practically not used due to a pronounced, sharp, short-term decrease in blood pressure with its subsequent increase, the so-called “hemitonic crises” . The drug is not recommended to be prescribed for withdrawal symptoms in patients with drug addiction, for vasomotor disorders due to menopause and dysmenorrhea, and for acute myocardial infarction. In such cases, it is preferable to prescribe imidazoline receptor agonists. With long-term use of the drug, monitoring of intraocular pressure is required. In order to prevent orthostatic hypotension during intravenous infusions, the patient should be in a horizontal position. During the treatment period, a weakly positive Coombs reaction may be recorded. Clonidine affects traffic control and attention. If there is no effect from using eye drops within 2 days, the drug is discontinued. In order to prevent the development of systemic side effects after instillations, it is recommended to press the projection of the conjunctival sac with your finger for 1-2 minutes.

Clonidine is described on Wikipedia as the active ingredient Clonidine.

Clonidine recipe in Latin:

Rp.: Clophelini 0.15 mg D. td N 10 in tabul. S.

Clonidine tablets 0.15 mg No. 50 (10x5)

Patients should be instructed not to discontinue treatment without consulting their physician. Sudden cessation of taking the drug can lead to the development of withdrawal syndrome due to an increase in the concentration of catecholamines in the blood plasma: a rapid increase in blood pressure, nervousness, agitation, headache, palpitations, tachycardia, nausea, sweating, tremor. Therefore, discontinuation of the drug should be carried out gradually over 1-2 weeks, taking into account concomitant therapy.

Withdrawal symptoms may occur 18 to 72 hours after the last dose of clonidine. If withdrawal syndrome develops, you should immediately resume use of the drug and then gradually discontinue it, replacing it with other antihypertensive drugs. Cases of hypertensive encephalopathy, cerebrovascular accident, and death have been reported after abrupt discontinuation of clonidine.

The likelihood of such a reaction to discontinuation of clonidine treatment increases with the use of high doses of the drug or with continued concomitant therapy with beta blockers, so special caution is recommended in such situations.

If, during combination treatment with beta-blockers, it becomes necessary to interrupt or discontinue antihypertensive therapy, beta-blockers (to prevent sympathetic hyperreactivity) should always be withdrawn first, gradually, several days before the start of tapering of Clonidine, especially if it was used in large doses.

To prevent withdrawal syndrome, the drug should not be prescribed to patients who do not have the conditions for its regular use.

The drug should be used with caution:

• patients with mild to moderate bradyarrhythmia;
• patients with diabetes mellitus, since clonidine can mask the symptoms of hypoglycemia and reduce insulin secretion;
• patients with polyneuropathy, constipation;
• elderly patients - due to the risk of hypersensitivity to the drug;
• patients with impaired renal function - due to the risk of delayed drug elimination;
• For people who use contact lenses for vision correction, clonidine may cause dry eyes.

For hypertension caused by pheochromocytoma, no therapeutic effect of clonidine is expected.

The use of clonidine may lead to a decrease in salivation. This contributes to the development of caries, periodontal disease, and oral candidiasis. A transient increase in the concentration of growth hormone is possible. The development of a weakly positive Coombs reaction is possible.

During treatment with Clonidine, it is prohibited to drink alcoholic beverages.

Patients should be warned that the sedative effect of the drug is enhanced by concomitant use of alcohol, barbiturates or other sedatives.

During treatment with Clonidine, it is recommended to regularly monitor blood pressure.

Caution should be exercised during prolonged physical activity, especially in an upright position in hot weather, due to the risk of orthostatic reactions.

The drug contains lactose, so its use is contraindicated in patients with rare hereditary conditions such as galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding.

The use of the drug during pregnancy is contraindicated.

If it is necessary to use the drug, breastfeeding should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

During the treatment period, you should refrain from driving vehicles and engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Analogs

Level 4 ATC code matches:
Tenzotran

Moxonitex

Albarel

Moxonidine

Physiotens

Analogues are Gemiton , Catapresan , Chlofazolin .