Proktoaktif (Suppositories) Instructions for Use

Marketing Authorization Holder

Avva Rus, JSC (Russia)

ATC Code

C05AX (Other preparations for the treatment of hemorrhoids and anal fissures for topical application)

Active Substance

Phenylephrine (Rec.INN registered by WHO)

Dosage Form

Proktoaktif

Rectal suppositories 5 mg

Dosage Form, Packaging, and Composition

Rectal suppositories

3 pcs. – contour cell packaging (2 pcs.) – cardboard packs (6 pcs.) – Over-the-counter
3 pcs. – contour cell packaging (4 pcs.) – cardboard packs (12 pcs.) – Over-the-counter
5 pcs. – contour cell packaging (2 pcs.) – cardboard packs (10 pcs.) – Over-the-counter
6 pcs. – contour cell packaging – cardboard packs (6 pcs.) – Over-the-counter
6 pcs. – contour cell packaging (2 pcs.) – cardboard packs (12 pcs.) – Over-the-counter

Pharmacotherapeutic Group

Angioprotectors; agents for the treatment of hemorrhoids and anal fissures for topical use; other agents for the treatment of hemorrhoids and anal fissures for topical use

Pharmacological Action

Adrenomimetic. It has a direct stimulating effect mainly on α-adrenergic receptors.

When used systemically, it causes constriction of arterioles, increases total peripheral vascular resistance and blood pressure. Cardiac output does not change or decreases, which is associated with reflex bradycardia (increased vagus nerve tone) in response to arterial hypertension. Phenylephrine increases blood pressure less sharply than norepinephrine and epinephrine, but acts for a longer time. This is apparently due to the fact that Phenylephrine is more stable and is not destroyed under the influence of COMT. In average therapeutic doses, it has practically no effect on the central nervous system.

When used topically in ophthalmology, Phenylephrine has a pronounced vasoconstrictor effect, causes mydriasis, and can lower intraocular pressure in open-angle glaucoma.

When used in ENT practice, it has a vasoconstrictor effect due to stimulation of α₁-receptors in the mucous membranes of the nasal cavity, reduces swelling of the mucous membranes and tissue hyperemia, congestion in the nasal mucosa, and improves the patency of the nasal airways.

When used rectally, it has a local vasoconstrictor effect, which helps reduce exudation, tissue swelling and itching in the anorectal area.

Pharmacokinetics

After oral administration, Phenylephrine is poorly absorbed from the gastrointestinal tract. It is metabolized with the participation of MAO in the intestinal wall and during the “first pass” through the liver. The bioavailability of phenylephrine is low.

After topical application, it undergoes systemic absorption.

Indications

Parenterally: to increase blood pressure in collapse and arterial hypotension associated with decreased vascular tone; as a vasoconstrictor during local anesthesia.

Topically in ophthalmology: iridocyclitis (to prevent the occurrence of posterior synechiae and reduce exudation from the iris); for diagnostic pupil dilation during ophthalmoscopy and other diagnostic procedures necessary to monitor the condition of the posterior segment of the eye; conducting a provocative test in patients with a narrow anterior chamber angle profile and suspected angle-closure glaucoma; differential diagnosis of superficial and deep injection of the eyeball; “red eye” syndrome (to reduce hyperemia and irritation of the mucous membrane of the eye); accommodation spasm.

Topically in ENT practice: to reduce swelling of the nasopharyngeal mucosa in colds and allergic diseases.

Rectally: as a symptomatic remedy for hemorrhoids, anal fissures, anal itching.

ICD codes

Dosage Regimen

For rectal use only. Wash hands thoroughly before and after the procedure.

Remove one suppository from its protective foil wrapping immediately before use.

Assume a comfortable position lying on your side with the lower leg straightened and the upper leg bent towards the stomach.

Gently insert the suppository, narrow end first, completely into the rectum.

Remain lying down for a few minutes to allow the suppository to melt and be absorbed.

Apply one suppository into the rectum up to four times daily.

The usual duration of treatment is up to seven days.

Do not use the suppositories for more than seven consecutive days unless directed by a physician.

If symptoms persist or worsen after one week of treatment, discontinue use and consult a doctor.

Do not exceed the recommended dosage.

For proper hygiene, use a protective finger cot or disposable glove during insertion.

Avoid using mineral oil-based lubricants as they may damage the latex of contraceptive devices; use water-based lubricants if necessary.

Store suppositories in a cool place to prevent melting.

Adverse Reactions

Systemic reactions increase or decrease in blood pressure, palpitations, bradycardia, tachycardia, ventricular arrhythmias, angina pectoris, pulmonary edema, coronary artery occlusion, pulmonary embolism, cardiac arrest, insomnia, nervousness, tremor, anxiety, increased excitability, confusion, irritability, headache, dizziness, cerebral hemorrhage, paresthesia, weakness, exacerbation of hyperthyroidism, eye pain, mydriasis, dysuria, urinary retention, nausea, vomiting, increased salivation, dyspnea, allergic reactions, increased sweating, facial skin pallor.

Local reactions: with parenteral use – necrosis and scab formation when entering tissues or with subcutaneous injections; with use in ophthalmology – conjunctivitis, periorbital edema, burning sensation, blurred vision, irritation, feeling of discomfort in the eye, increased lacrimation, increased intraocular pressure, reactive miosis the day after use; with use in ENT practice – feeling of burning, tingling or prickling in the nose, irritation of the mucous membranes of the nasal cavity; with rectal use – contact dermatitis.

Contraindications

Hypersensitivity to phenylephrine; severe diseases of the cardiovascular system, pheochromocytoma; arterial hypertension, glucose-6-phosphate dehydrogenase deficiency, porphyria, thyrotoxicosis, diabetes mellitus, angle-closure glaucoma, use simultaneously with MAO inhibitors and for 14 days after discontinuation of therapy with them; halothane or cyclopropane anesthesia; pregnancy, breastfeeding period; prematurity, childhood – depending on the dosage form; impaired tear production (for use in ophthalmology).

With caution coronary artery disease (especially after a recent myocardial infarction), angina pectoris, thrombosis of coronary, mesenteric and other visceral or peripheral vessels, pulmonary hypertension, ventricular arrhythmias, thromboembolism, atherosclerosis, obliterating thromboangiitis (Buerger’s disease), Raynaud’s disease, tendency of blood vessels to spasms during frostbite, diabetic endarteritis, thyroid dysfunction, metabolic acidosis, hypercapnia, hypoxia, impaired renal and/or liver function, use in patients with prostate diseases who have an increased risk of urinary retention, granulocytopenia, sickle cell anemia; old age; wearing contact lenses, after surgical interventions (for use in ophthalmology).

Use in Pregnancy and Lactation

Use during pregnancy and breastfeeding is not recommended.

Use in Hepatic Impairment

It should be used with caution in patients with impaired liver function.

Use in Renal Impairment

It should be used with caution in patients with impaired renal function.

Pediatric Use

Use in children is possible according to indications, in doses and dosage forms recommended according to age. It is necessary to strictly follow the instructions in the instructions for phenylephrine preparations regarding contraindications to the use of specific dosage forms of phenylephrine in children of different ages.

Geriatric Use

It should be prescribed with caution to elderly patients to avoid worsening of concomitant diseases.

Special Precautions

When used parenterally, during treatment, ECG indicators, blood pressure, minute blood volume, circulation in the extremities and at the injection site should be monitored. Before starting or during therapy for shock conditions, correction of hypovolemia, hypoxia, acidosis and hypercapnia is mandatory. To prevent a repeated decrease in blood pressure after discontinuation of phenylephrine, the dose should be reduced gradually, especially after a long infusion. The infusion is resumed if systolic blood pressure decreases to 70-80 mm Hg.

With age, the number of adrenergic receptors sensitive to phenylephrine decreases. MAO inhibitors, increasing the pressor effect of sympathomimetics, can cause headaches, arrhythmias, vomiting, and hypertensive crisis, therefore, when patients have taken MAO inhibitors in the previous 2-3 weeks, the doses of sympathomimetics should be reduced.

When phenylephrine is used topically, systemic adverse reactions may occur.

When phenylephrine is used topically in ophthalmology, repeated instillations over a short period of time may lead to less pronounced mydriasis than previously observed. This effect is more common in elderly patients. Due to significant contraction of the pupil dilator muscle, 30-45 minutes after instillation under the influence of phenylephrine, pigment particles from the pigment layer of the iris may be detected in the moisture of the anterior chamber of the eye. The suspension in the chamber moisture must be differentiated from manifestations of anterior uveitis or from the entry of formed blood elements into the moisture of the anterior chamber.

Effect on the ability to drive vehicles and mechanisms

During treatment, patients should avoid driving vehicles and other activities that require high concentration and speed of psychomotor reactions.

Drug Interactions

When using phenylephrine against the background of general anesthesia caused by halothane or cyclopropane, the development of ventricular fibrillation is possible.

With simultaneous use with MAO inhibitors, potentiation of the effects of phenylephrine is observed (including with topical use).

With simultaneous use, phenothiazines, alpha-blockers (phentolamine), furosemide and other diuretics reduce the vasoconstrictor effect of phenylephrine.

With simultaneous use, guanethidine enhances the mydriatic effect of phenylephrine (with systemic absorption).

With simultaneous use, oxytocin, ergot alkaloids, tricyclic antidepressants, furazolidone, procarbazine, selegiline, sympathomimetics enhance the pressor effect, and the latter also increase arrhythmogenicity.

With simultaneous use, beta-blockers reduce cardiotonic activity; against the background of reserpine, arterial hypertension is possible.

With simultaneous use, Phenylephrine reduces the antianginal effect of nitrates, which, in turn, can reduce the pressor effect of phenylephrine and increase the risk of arterial hypotension.

With simultaneous use, thyroid hormones increase (mutually) the effectiveness of phenylephrine and the associated risk of coronary insufficiency (especially with coronary atherosclerosis).

With simultaneous use of phenylephrine with digoxin or other cardiac glycosides, the risk of cardiac arrhythmias and myocardial infarction increases.

The use of phenylephrine during childbirth to correct arterial hypotension against the background of the use of labor-stimulating agents (vasopressin, ergotamine, ergometrine, methylergometrine) can cause a persistent increase in blood pressure in the postpartum period.

When used topically in ophthalmology, the mydriatic effect of phenylephrine is enhanced when used in combination with the topical use of atropine. Due to the enhancement of the vasopressor effect, the development of tachycardia is possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

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.