Pharmacodynamics and pharmacokinetics
Clonidine affects neurogenic regulation of vascular tone, belongs to the group of alpha 2 – agonists. The mechanism of action of Clonidine is that it stimulates the alpha1-acnerosacea, located on the periphery and has a temporary pressor effect on the body.
The substance acts directly on I1-and ALPHA2 imidazolinone-adrenaline receptors. As a result it excites neurons of the vasomotor centers of the bottom of rhomboid fossa of the fourth ventricle. The drug also affects the rear nuclear of vagus nerve, increasing the influence of the parasympathetic nervous system on the heart muscle. In the end, it significantly reduces the intensity of the flow of sympathetic impulses of the central researcher and the production of noradrenaline. Also the drug inhibits the secretion of epinephrine adrenal medulla. Due to the decreased production of catecholamines, blood pressure on the vascular wall is significantly reduced. You may buy сlonidine on our website.
The hypotensive effect of Clonidine is accompanied by a decrease in cardiac output and PSS, a decrease in intraocular pressure, drainage of aqueous humor from eyes. It has sedative effect on central nervous system. The drug anesthetizes moderately, alleviates fear, relieves some signs of alcohol and opiate withdrawal lowers the body temperature. The drug has a sedative effect in large doses.
If you make an injection intravenously, the pressure can dramatically increase for a few minutes, so an intravenous medicine is usually not applied. The effect of taking pills develops within 60-120 minutes and lasts up to 8 hours.
The drug is well absorbed by the gastrointestinal tract after oral administration. Biological availability of the drug is from 75 to 95%. The plasma protein binds about 34% of the substance. Metabolism of drugs occurs in the liver. The half-life is 12 to 30 hours. Clonidine is excreted mostly in the urine.
Animal studies have shown that the drug has the ability to focus in the choroid of the eye, damage the cornea and retinal degeneration (however, its functions were not violated).
Indications for use
The drug is prescribed for systemic use:
with hypertensive crisis;
for the treatment of hypertension (including renal genesis).
As for the ophthalmic practice, the drug is used in combination with other assets or within the framework of complex therapy of open-angle glaucoma.
The remedy is contraindicated:
in cardiogenic shock;
to patients who are allergic to the active substance;
with atherosclerosis of brain vessels;
to persons with arterial hypotension;
in case of peripheral vascular disease or AV block 2 and 3 degrees;
if a patient has syndrome sick sinus or bradycardia;
in case of parallel treatment of tricyclic antidepressants;
in a condition of alcoholic intoxication;
in the presence of inflammation in the anterior segment (eye drops).
Caution is advised to observe:
patients who have had a recent myocardial infarction;
during ischemia or congestive heart failure
patients with liver or kidney disease;
patients with diabetes mellitus;
in case of polyneuropathy, cerebrovascular diseases;
individuals suffering from frequent constipation.
The use of the drug may develop the following side reactions:
drowsiness, anxiety, headaches;
dizziness, asthenia, marked sedation, depression, nightmares, restless sleep;
the decrease in blood pressure, bradycardia, intravenous use – high blood pressure;
allergic skin reactions, itching;
fluid retention in the body edema, nasal congestion;
decreased libido (rare), withdrawal syndrome, Hematology crisis;
burning, dryness and itching in the eyes, foreign body sensation, swelling and redness, conjunctivitis (using eye drops).
Clonidine, usage instructions (Method and dose)
The drug is administered orally, parenterally instilled into the conjunctival SAC, administered sublingually. The dosage and treatment regimen is designated by a doctor.
Instructions for Clonidine.
Typically, the initial dose is from 40 to 75 micrograms, 3 times a day. The dose can be increased to 900 micrograms in case of inefficiency (gradually by 37.5 mg every 2 days). The duration of treatment is from 30 days to 2 months. The maximum single dosage for oral administration is about 300 mg.
The maximum daily dose is up to 1.2-1.5 mg. Often you can be additionally prescribe other antihypertensives or saluretics.
The drug is administered intramuscularly at a dosage of 150 mcg, often use 0.01% solution. Intravenous drug is injected slowly (from 3 to 5 minutes), 150 mg of the drug, diluted in 20 ml isotonic R-re chloride sodium.
The effect of intravenous injection occurs within 5 min and persists up to 8 hours.
Do not stop treatment with remedy, it can lead to the development of the syndrome and sudden increase in blood pressure. It is recommended to reduce the dose over 7-10 days.
The instructions for use in ophthalmology
Eye drops are administered into the conjunctival SAC from 2 to 4 times a day. Patients use 0.25% solution in the initial stages of the treatment, then a patient can take 0.5%. If necessary you may use of 0.125% p-p of Clonidine.
The duration of treatment is determined by an attending physician. Clonidine is bought on our site in any amount.