Description
Pharmacological action
Pharmacotherapeutic group: alpha-adrenergic blocker
ATX code: 02CA
Pharmacological properties of
Pharmacodynamics
Proroxan has a hypotensive and antipruritic effect. Blocks postsynaptic 1 and presynaptic 2-adrenergic receptors, regardless of their location. It has a peripheral and central influence. Reduces the sensitivity of adrenoreceptors to adrenaline, changing the permeability of cell membranes. It reduces the intensity of stimulation of hypothalamic structures, reducing the secretion of tropic hormones, hormones of peripheral glands. It weakens the transmission of adrenergic vasoconstrictive impulses, eliminates spasm and dilates peripheral vessels, especially arterioles and precapillaries. Improves blood supply to muscles, skin, mucous membranes. Suppresses the excitability of brain diencephalic structures and regulates the tone of the sympathoadrenal system.
Pharmacokinetics
It is established that the drug is well absorbed in the gastrointestinal tract, but an effective concentration is achieved only after 30-40 minutes and lasts 3-4 hours. Plasma protein binding is weak. The drug has a large volume of distribution, it quickly penetrates into various tissues and fluids, including cerebrospinal fluid. It penetrates well through the histohematological barriers, including the blood-brain barrier. Selectively lingers in the hypothalamus, the posterior region of which contains predominantly noradrenergic neurons. It is excreted mainly by the kidneys. About 70% of the administered dose is excreted by the kidneys in the first 24 hours.
In animal experiments with intraperitoneal administration, the half-life was not established, while less than 5% of the administered dose remained in the blood plasma 1 hour after administration, and after 2 hours – only traces. After 1 hour, 22% was found in the brain, after 2 hours – 6% of the maximum concentration. It was also shown in experiments with carbon labeled with prooxane that the products of its metabolism are able to linger for a long time (up to 10 days) in various organs and tissues (plasma, brain, liver, kidneys).
Indications
– Somatoform autonomic dysfunction proceeding according to the sympathoadrenal type, incl. with an increase in blood pressure (as a symptomatic agent as part of complex therapy)
– allergic dermatitis (as a symptomatic agent as part of complex therapy for relief of pruritus).
Contraindications
Hypersensitivity to the active substance or auxiliary components of the drug
severe atherosclerosis
severe cerebrovascular insufficiency (including strokes, transient ischemic attacks in history)
II ischemic heart disease Grade III
arterial hypotension
cardiogenic shock
bradycardia
myocardial infarction
galactose intolerance, glucose-galactose malabsorption, la failure ktazy
children under 18 years old.
Caution
Caution should be used in elderly patients, coronary heart disease, arrhythmias, and gastric ulcer.
It is recommended to control the concentration of glucose in the blood (possibly an increase in the level of endogenous insulin).
Use during pregnancy and lactation
Use during pregnancy and during breast-feeding is contraindicated.
Special instructions
Features of the drug when taking
for the first time A sharp decrease in blood pressure, fainting, headache, weakness, palpitations and worsening of the subjective state ( ² Ñthe phenomenon of the first dose ² Ñ), which is not a reason for drug withdrawal, since this effect disappears with repeated use. Drowsiness, a passing sensation of numbness of the tongue are also noted. In addition, it is recommended to control the concentration of glucose in the blood due to a possible increase in the level of endogenous insulin. In this connection, it is necessary to begin treatment under the supervision of a doctor with the minimum effective dose and observe bed rest after taking the drug for 6-8 hours.
Influence of the drug on the ability to drive vehicles,
mechanisms During the treatment with the drug, it is not recommended to drive vehicles and engage in potentially dangerous activities, requiring increased concentration of attention and speed of psychomotor reactions.
Composition
Active ingredient: propoxane hydrochloride – 15 mg
Excipients: ludipress ® [lactose monohydrate – 78.3 mg, povidone K-30 – 2.95 mg, crospovidone – 2.95 mg] – 84, 2 mg of magnesium stearate – 0.8 mg.
Dosage and administration of
In somatoform autonomic dysfunction, proceeding according to the sympatho-adrenal type as part of complex therapy, 15-30 mg (1-2 tablets) are prescribed orally 2-3 times a day. The duration of treatment is determined by the attending physician.
In allergic dermatitis, it is recommended that 15-30 mg (1-2 tablets) be taken orally before bedtime as part of complex therapy. The duration of treatment is determined by the attending physician.
Side effects
From the cardiovascular system: bradycardia, arterial hypotension, the occurrence of angina attacks in susceptible patients, orthostatic hypotension, arrhythmias, dizziness, flushing of the skin, nasal congestion.
From the gastrointestinal tract: diarrhea, increased secretion of hydrochloric acid in the stomach.
If any of the side effects indicated in the instructions are aggravated, or you notice any other side effects not listed in the instructions, inform your doctor.
Drug interaction
Enhances the action of antipsychotics (derivatives of phenothiazine, butyrophenone, diphenylbutylpiperidine, thioxanthene)
with the use of procainamide, it is possible to reduce the stroke volume of the heart
with simultaneous use with adrenaline, it may be distorted – the development of a depressant effect instead of pressor
, the simultaneous use of prooxan with hypotensive agents leads to the mutual potentiation of their effects on lowering blood pressure.
If you are taking other medicines, be sure to consult your doctor before taking the drug.
Overdose
Symptoms: bradycardia, orthostatic collapse, a sharp decrease in blood pressure.
Treatment: symptomatic, aimed at maintaining vital functions.
Storage conditions
Dry, a place protected from light at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
The Expiration of
is 3 years.
Deystvuyuschee substances
Proroksan
Doctor tvennaya form
tablets
