Clofelin - instructions for use, reviews, analogs and forms of release (tablets of 0.075 mg and 0.15 mg, injections in injections, eye drops) of the drug for the management of hypertensive crises in adults, children and in pregnancy
In this article, you can read the instructions for using the drug Clophelin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of specialists in the use of Clofelin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of clopheline in the presence of existing structural analogues.Use for the treatment of glaucoma and cupping of hypertensive crisis in adults, children, as well as in pregnancy and lactation. Joint reception with alcohol and the results of such interaction and symptoms of drug poisoning.
Clophelin - antihypertensive remedy of central action. The mechanism of action is due to the stimulation of postsynaptic alpha2-adrenergic receptors of the vasomotor center of the medulla oblongata and reduces the flow of sympathetic impulse to the vessels and the heart at the presynaptic level. The hypotensive effect is caused by a decrease in OPSS, a decrease in heart rate and cardiac output.
With rapid intravenous administration, a short-term increase in blood pressure is possible, due to stimulation of postsynaptic alpha-1-adrenergic receptors of blood vessels. Increases renal blood flow; increasing the tone of the vessels of the brain, reduces cerebral blood flow; has a pronounced sedative effect.
The duration of the therapeutic effect is 6-12 hours.
When instilled into the conjunctival sac, the intraocular pressure decreases due to local adrenostimulating action,as a result of which the production of intraocular fluid decreases and to some extent its outflow improves, as well as by weakening the sympathetic tone due to the central effects of the active substance, part of which has undergone resorption.
Composition
Clonidine + excipients.
Pharmacokinetics
When ingestion is well absorbed from the digestive tract. Metabolized in the liver about 50% of the absorbed dose. It is excreted by the kidneys - 40-60% unchanged, through the intestine - 20%.
Indications
For systemic use:
- arterial hypertension (including symptomatic hypertension of renal genesis)
- hypertensive crisis.
For topical application in ophthalmology:
- open-angle glaucoma (as a monotherapy or in combination with other drugs that reduce intraocular pressure).
Forms of release
Tablets 0.075 mg and 0.15 mg.
Solution for intravenous administration 0.01% (injections in ampoules for injection).
Eye drops 0.125%, 025% and 0.5%.
Instructions for use and dosing regimen
Pills
Inside, during or after a meal, without chewing, squeezed a small amount of liquid. The dose is selected strictly individually.
Usually, treatment starts with small doses (0.075 mg 2-3 times a day). With an insufficiently expressed hypotensive effect, the single dose is gradually increased every 1-2 days by 0.0375 mg to 0.15 mg.
In elderly patients, especially with the manifestation of cerebral vascular sclerosis, treatment begins with a dose of 0.0375 mg.
Daily doses are usually 0.3-0.45 mg, sometimes 1.2-1.5 mg.
Ampoules
Intramuscularly, subcutaneously or intravenously.
With hypertensive crises - in / m, n / k or iv. В / м and п / к - on 0,5-1,5 ml of 0,01% solution. If the hypotensive effect is not expressed enough, injections are prescribed up to 3-4 times a day. For intravenous injection of 0.5-1.5 ml of 0.01% solution is diluted in 10-20 ml of isotonic sodium chloride solution and injected slowly for 3-5 minutes.
Eye Drops
Bury in the conjunctival sac 1-2 drops 2-4 times a day. Treatment begins with the appointment of 0.25% solution. In case of insufficient decrease in intraocular pressure, 0.5% solution is used. With the development of side effects associated with the use of 0.25% solution, 0.125% solution is prescribed.
Side effect
- asthenia;
- drowsiness;
- slowing the speed of mental and motor reactions;
- anxiety;
- nervousness;
- headache;
- dizziness;
- night trouble;
- euphoria;
- depression;
- bright or nightmarish dreams;
- bradycardia;
- orthostatic hypotension;
- skin rash;
- itching;
- nasal congestion;
- decreased potency and / or libido;
- dryness of the conjunctiva;
- itching or burning in the eyes;
- the feeling of a foreign body;
- conjunctivitis.
Contraindications
- hypersensitivity;
- cardiogenic shock;
- arterial hypotension;
- pronounced atherosclerosis of cerebral vessels;
- obliterating diseases of peripheral arteries;
- AV blockade of 2-3 degrees;
- pronounced sinus bradycardia;
- syndrome of weakness of the sinus node;
- depression;
- porphyria;
- simultaneous use of ethanol (alcohol) and other drugs that exert a depressing effect on the central nervous system (co-administration of Clofelin and alcohol is prohibited);
- pregnancy;
- lactation period;
- increased sensitivity to clonidine;
- inflammatory diseases of the anterior part of the eye (for eye drops).
Application in pregnancy and lactation
Contraindicated in pregnancy and lactation.
Symptoms of poisoning and overdose
Impairment of consciousness, collapse, for the state of acute poisoning, bradycardia, broadening of the QRS complex, possible AV conduction slowdown and early repolarization syndrome are characteristic.
special instructions
Use with caution after a recent myocardial infarction, with chronic renal failure.
With sudden discontinuation of therapy, it is possible to develop withdrawal syndrome: increased blood pressure, nervousness, headaches, tremors, nausea.
When using Clopheline in combination with beta-blockers, in order to avoid an undesirable increase in blood pressure in the event of discontinuation of therapy, it is first necessary to gradually finish the treatment with beta-blockers, and then also by slowing the dose to stop taking clonidine.
To prevent the occurrence of orthostatic hypotension with IV administration of clonidine, the patient should be in the prone position during the administration and within 1.5-2 hours after the administration.
In the absence of effect during the first 1-2 days, the drug is canceled. To reduce the systemic effect of the drug after instillation, it is necessary to press the area of the lacrimal sac for 1-2 minutes.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, potentially dangerous activities that require increased attention and rapid psychomotor reactions should be avoided.
Drug Interactions
In patients receiving beta-blockers, in the event of a sudden withdrawal of Clopheline, a sharp increase in blood pressure is possible. It is believed that this is due to an increase in the content of catecholamines in the circulating blood and an increase in their vasoconstrictor action.
With the simultaneous use of hormonal contraceptives for oral administration, it is possible to enhance the sedative effect of clonidine.
With the simultaneous use of tricyclic antidepressants (including imipramine, clomipramine, desipramine), the antihypertensive effect of clofelin decreases.
With simultaneous application with clonidine, an increase in the duration of action of vecuronium is possible.
At simultaneous application with Verapamil there is a message on development of blockade of heart at the patient with an arterial hypertensia.
It is believed that Clofelin suppresses increased production of catecholamines, which results from hypoglycemia, and, consequently, symptoms of hypoglycemia (tachycardia, palpitation, increased sweating), which are caused by the influence of catecholamines. In addition, there are reports that clonidine increases blood glucose, presumably due to a decrease in insulin secretion.This must be taken into account when using insulin simultaneously.
When switching from clonidine to captopril, the antihypertensive effect of the latter develops gradually. In the case of sudden withdrawal of clonidine in patients receiving captopril, a sharp increase in blood pressure is possible.
There have been reports of a decrease in the efficacy of levodopa and pyribedil in patients with Parkinson's disease.
With simultaneous use with prazozinom it is possible to change the antihypertensive effect of clonidine.
With the simultaneous use of propranolol, Atenolol develops an additive hypotensive effect, a sedative effect, dry mouth.
When used simultaneously with cyclosporine, there is a report of an increase in the concentration of cyclosporine in the blood plasma.
Analogues of the drug Clophelin
Structural analogs for the active substance:
- Hemiton.
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