Pentamin (Solution) Instructions for Use

ATC Code

C02BC (Bis-quaternary ammonium compounds)

Active Substance

Azamethonium bromide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Ganglioblocking agent

Pharmacotherapeutic Group

Antihypertensive agents; antiadrenergic agents, ganglioblockers; bis-quaternary ammonium compounds.

Pharmacological Action

Ganglioblocker, a bis-quaternary ammonium compound. It has hypotensive, arterio- and venodilating effects. It blocks the n-cholinergic receptors of the autonomic ganglia and, in connection with this, inhibits the transmission of nerve impulses from preganglionic to postganglionic fibers of the autonomic nerves.

The autonomic ganglia also become less sensitive to the excitatory action of a number of cholinergic stimulants (including acetylcholine, nicotine, lobeline, cytisine). By interrupting the conduction of nerve impulses through the autonomic ganglia, ganglioblockers change the functions of organs supplied with autonomic innervation.

This results in a decrease in blood pressure, which is mainly associated with a reduction in the influx of vasoconstrictor impulses to the blood vessels and the expansion of the peripheral vascular bed (primarily arterioles).

Inhibition of impulse conduction along cholinergic nerve fibers leads to impaired accommodation, bronchial dilation, decreased motility of the gastrointestinal tract organs, inhibition of gland secretion, increased heart rate, and decreased bladder tone. Inhibition of n-cholinergic receptors in the chromaffin tissue of the adrenal glands leads to a decrease in the release of adrenergic substances and a weakening of reflex pressor reactions.

In high doses, it can block the n-cholinergic receptors of skeletal muscles and the central nervous system.

Azamethonium bromide is somewhat inferior to benzohexonium in terms of activity and duration of action.

Indications

Diseases and conditions caused by spasms of peripheral vessels (including endarteritis, intermittent claudication).

As part of combination therapy for hypertensive crisis, pulmonary edema, cerebral edema.

In anesthesiological practice – for controlled arterial hypotension.

In urological practice – during cystoscopy in men (to facilitate the passage of the cystoscope through the urethra).

ICD codes

Dosage Regimen

Administer Pentamin solution intramuscularly or intravenously; the route depends on the clinical urgency and desired onset of action.

Set the dose individually for each patient, titrating against blood pressure response and therapeutic goal.

For hypertensive crisis, administer intravenously to achieve a rapid, controlled reduction in blood pressure.

For controlled arterial hypotension in surgery, use intravenous administration under continuous hemodynamic monitoring.

For peripheral vascular spasms, intramuscular injection is typically employed.

For cystoscopy in men, administer intramuscularly to facilitate instrument passage through the urethra.

Initiate therapy with a low test dose, approximately half the intended therapeutic dose, to assess individual tolerance.

Keep the patient in a supine position before injection and for 1-2 hours post-injection to mitigate the risk of orthostatic collapse.

Monitor blood pressure and pulse frequently during and after administration.

Do not exceed the maximum single dose of 150 mg for intramuscular administration.

Do not exceed the maximum daily dose of 450 mg for intramuscular administration.

Adjust dosage cautiously in elderly patients due to increased sensitivity to hypotensive effects.

Discontinue therapy if signs of severe intolerance or progressive hypotension occur.

Adverse Reactions

From the cardiovascular system: possible increased pulse, orthostatic collapse (due to inhibition of reflex mechanisms that maintain a constant level of blood pressure).

From the digestive system: dry mouth; with long-term use in high doses, intestinal atony (up to paralytic intestinal obstruction) is possible.

From the central nervous system: possible general weakness, dizziness.

From the organ of vision: mydriasis, accommodation paresis, injection of scleral vessels.

From the urinary system: with long-term use in high doses, bladder atony with anuria is possible.

Contraindications

Angle-closure glaucoma, acute phase of myocardial infarction, pronounced arterial hypotension, shock, impaired liver and/or kidney function, pheochromocytoma, degenerative diseases of the central nervous system, hypersensitivity to azamethonium bromide.

Use in Pregnancy and Lactation

Data on the safety of azamethonium bromide use during pregnancy and lactation (breastfeeding) are not available.

Use in Hepatic Impairment

Contraindication: impaired liver function.

Use in Renal Impairment

Contraindication: impaired kidney function.

Geriatric Use

Azamethonium bromide should be used with caution in elderly patients.

Special Precautions

Azamethonium bromide should be used with caution in bronchial asthma with difficult sputum discharge, intestinal and bladder atony of various etiologies, in thrombosis, thrombophlebitis, degenerative diseases of the central nervous system, bronchial asthma (with difficult sputum discharge), and in elderly patients.

Treatment with ganglioblockers should be carried out under close medical supervision.

To avoid the development of orthostatic collapse, it is recommended that the patient be in a lying position before the administration of azamethonium bromide and for 1-2 hours after the injection. It is recommended at the beginning of treatment to check the patient’s reaction to small doses of azamethonium bromide: administer 1/2 of the average dose and monitor the patient’s condition.

It should be borne in mind that with elevated blood pressure, the hypotensive effect is more pronounced.

In open-angle glaucoma, a decrease in intraocular pressure may be observed, which is due to a decrease in the production of aqueous humor under the influence of ganglioblockers.

Drug Interactions

With simultaneous use, ganglioblockers enhance the effect of adrenomimetics.

Anticholinesterase drugs are antagonists of ganglioblockers.

With simultaneous use with tricyclic antidepressants, the hypotensive effect of ganglioblockers is reduced.

Storage Conditions

Store at 15°C (59°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.