Pyrroxan pills 15mg, 50pcs

Composition

Active ingredient:

proroxane hydrochloride – 15 mg;

Auxiliary substances:

ludipress® [lactose monohydrate-78.3 mg,

povidone K-30-2.95 mg,

crospovidone-2.95 mg] – 84.2 mg;

magnesium stearate-0.8 mg

Pharmacological action

Pharmacotherapy group:

alpha-adrenoblocker

ATX code: C 02 CA

Pharmacological properties

Pharmacodynamics

Proroxan has antihypertensive and antipruritic effects. Blocks postsynaptic_α1-and presynaptic_α2-adrenergic receptors, regardless of their location. It has a peripheral and central influence. Reduces the sensitivity of adrenoreceptors to epinephrine, changing the permeability of cell membranes. Reduces the intensity of stimulation of hypothalamic structures, reducing the release of tropic hormones, hormones of peripheral glands. Reduces the transmission of adrenergic vasoconstrictor impulses, eliminates spasm and dilates peripheral vessels, especially arterioles and precapillaries. Improves blood supply to muscles, skin, and mucous membranes. It suppresses the excitability of the brain’s diencephalic structures and regulates the tone of the sympathoadrenal system.

Pharmacokinetics

It was found that the drug is well absorbed in the gastrointestinal tract, but the effective concentration is reached only after 30 – 40 minutes and persists for 3-4 hours. Binding to plasma proteins is weak. The drug has a large volume of distribution, it quickly penetrates into various tissues and fluids, including the cerebrospinal fluid. It penetrates well through histohematic barriers, including the blood-brain barrier. Selectively delayed in the hypothalamus, the posterior region of which contains mainly noradrenergic neurons. It is mainly excreted by the kidneys. About 70% of the administered dose is excreted by the kidneys in the first 24 hours.

In animal experiments with intraperitoneal use, the half-life was not established, while in the blood plasma 1 hour after use, less than 5% of the administered dose of the drug remained, and after 2 hours – only traces. In the brain,22% of the maximum concentration was detected after 1 hour, and 6% of the maximum concentration was detected after 2 hours. It was also shown in experiments with carbon-labeled proroxane that the products of its metabolism can linger for a long time (up to 10 days) in various organs and tissues (plasma, brain, liver, kidneys).

Indications

-Somatoform autonomic dysfunction that occurs according to the sympathoadrenal type, including with increased blood pressure (as a symptomatic agent in complex therapy);

– allergic dermatitis (as a symptomatic agent in complex therapy for relieving itching).

Use during pregnancy and lactation

Contraindicated use during pregnancy and lactation.

Contraindications

• Hypersensitivity to the Active ingredient or auxiliary components of the drug;

• pronounced atherosclerosis,

• severe cerebrovascular disease (including stroke, transient ischemic attack in history);

• ischemic heart disease (II-IV functional class),

• circulatory failure II-III degree;

• hypotension;

• cardiogenic shock;

• bradycardia;

• myocardial infarction;

• galactose intolerance, glucose-galactose malabsorption, lactase deficiency;

• children up to age 18 years.

With caution

It should be used with caution in elderly patients with coronary heart disease, arrhythmias, and stomach ulcers.

It is recommended to monitor the concentration of glucose in the blood (possibly an increase in the level of endogenous insulin).

Side effects

From the cardiovascular system: bradycardia, arterial hypotension, angina attacks in predisposed patients, orthostatic hypotension, arrhythmias, dizziness, hyperemia of the skin, nasal congestion.

From the gastrointestinal tract: diarrhea, increased secretion of hydrochloric acid in the stomach.

If any of the side effects listed in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Interaction

• Increases the effect of neuroleptics (derivatives of phenothiazine, butyrophenone, diphenylbutylpiperidine, thioxanthene);

• against the background of the use of novocainamide, it is possible to reduce the stroke volume of the heart;

• when used simultaneously with epinephrine, its action may be perverted – the development of a depressive effect instead of pressor;

• simultaneous use of proroxane with antihypertensive agents leads to mutual potentiation of their effects on lowering blood pressure.

If you are taking other medications, be sure to consult your doctor before taking the drug.

How to take, course of use and dosage

With somatoform autonomic dysfunction, which occurs according to the sympatho-adrenal type, as part of complex therapy,15-30 mg (1-2 tablets) is prescribed orally 2-3 times a day. The duration of treatment is determined by the attending physician.

For allergic dermatitis as part of complex therapy, it is recommended to prescribe 15-30 mg (1-2 tablets) orally before bedtime. The duration of treatment is determined by the attending physician.

Overdose

Symptoms: bradycardia, orthostatic collapse, a sharp drop in blood pressure.

Treatment: symptomatic, aimed at maintaining vital functions.

Special instructions

Features of the action of the drug at the first intake

When taking the first dose of the drug, there may be a sharp drop in blood pressure, fainting, headache, weakness, palpitations and deterioration of the subjective state (the”first dose phenomenon”), which is not a reason for discontinuing the drug, since this effect disappears with repeated use. Also note drowsiness, a rapidly passing sensation of numbness of the tongue. In addition, it is recommended to monitor the concentration of glucose in the blood because of the possible increase in the level of endogenous insulin. In this regard, it is necessary to start treatment under the supervision of a doctor with the minimum effective dose and observe bed rest after taking the drug for 6-8 hours.

Effect of the drug on the ability to drive vehicles, mechanisms

During treatment with the drug, it is not recommended to drive vehicles and engage in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 3 years.

Active ingredient

Proroxan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets