Clonidine: instructions for use, what it is, price, where to buy

The drug Clonidine, the effect of this drug on humans is well known. The drug has been used for more than a year in medicine and, unfortunately, in criminal activities.

In the 1960s, a new substance was synthesized - clonidine. Clonidine is available under different trade names, Clonidine being the best known. Belongs to a group of drugs with antihypertensive effects.

It was originally planned that the drug would become an effective treatment for the common cold. The active ingredient relieves vasospasm and makes breathing easier. Over time, clonidine was found to markedly lower blood pressure and induce sleep.

Fraudsters began to use this for criminal purposes. Why do clonidine specialists mix it into drinks and how long does it take for clonidine to start working?

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.

Description of the drug

Clonidine is an antihypertensive agent that affects the mechanisms of blood pressure adjustment. The medication has a strong sedative effect and reduces the manifestations of alcohol abstinence.

Long-term or short-term exposure to the body may result in the following effects:

The systematicity of myocardial contractions is significantly reduced. This reduces blood pressure.
The dynamic functioning of the nervous system decreases. This affects the feeling of sleepiness. The medication has a sedative effect.
The pressure level of the eyeball is significantly reduced.
Sleeping pills have a good analgesic effect due to their strong central nervous system suppression.
The medicine has a good effect on patients who are experiencing opiate withdrawal syndrome. There is an elimination of symptoms such as anxiety, fear, and tension. The medication also helps reduce disorders in the functioning of the heart muscle.

Important! Taking sleeping pills has an effect within 15 minutes after using the drug.

25-30 minutes after taking the medication, a drop in blood pressure is noted. The medicinal effect can last up to 12 hours.

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, 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.

Clonidine and alcohol

Clonidine is soluble in water. It is practically insoluble in alcohol, forming a cloudy suspension. It has a bitter taste but no odor.

How to protect yourself in unfamiliar company:

Don't let the bottle of alcohol out of sight. You need to make sure that the drink is uncorked in front of you.
If the liquid looks suspicious, it is better to refuse the drink.
If Clonidine poisoning does occur, you cannot concentrate your gaze on one point - consciousness immediately disappears.
If your consciousness is absent-minded, you should not drive.
While you have the strength, you need to call for help.

And the main rule is to drink only in trusted company or fill your glass yourself.

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 in crimes

In the criminal world, clonidine is known as a drug with a hypnotic effect. There are known cases when prostitutes added crystalline powder to vodka in order to put the client to sleep. After several such cases, female criminals began to be called clonidine addicts.

Who are clofilins? In a broad sense, these are not only girls of easy virtue who, instead of providing services, rob clients, but also all women who lure men and then take money and valuables.

Since Clonidine has hypnotic properties, it is used for kidnapping and illegal transportation of people, rape and other crimes.