Relief

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT RELIEF® (RELIEF®)

Composition:

Active substance: phenylephrine hydrochloride;

1 g of ointment contains phenylephrine hydrochloride 2.5 mg;

Excipients: mineral oil, α-tocopherol, thyme oil, corn oil, glycerin, white soft paraffin, methylparahydroxybenzoate (E 218), propylparahydroxybenzoate (E 216), lanolin, benzoic acid (E 210), lanolin alcohol, paraffin, purified water, white wax.

Pharmaceutical form. Rectal ointment.

Main physicochemical characteristics: yellowish ointment without foreign particles.

Pharmacotherapeutic group.

Local treatment agents for hemorrhoids and anal fissures.

ATC code C05AX.

Pharmacological properties.

Pharmacodynamics.

Phenylephrine hydrochloride exerts a local vasoconstrictive effect. This normalizes the balance between blood inflow to the hemorrhoidal nodes and venous outflow from them, and also helps reduce exudation, swelling, itching, and serous discharge in hemorrhoids and other anorectal disorders.

Pharmacokinetics.

The drug is intended for topical use. Phenylephrine contained in the formulation is inactivated by tissue monoamine oxidase; inactive metabolites are excreted in mucus or in insignificant amounts by the kidneys.

Clinical characteristics.

Indications.

Symptomatic treatment of itching, burning, and discomfort associated with hemorrhoids and other anorectal disorders, as well as with erosions, fissures, and microtraumas in the anal area.

Contraindications.

Hypersensitivity to any component of the drug, significant increase in blood pressure, tachysystolic cardiac arrhythmias, decompensated heart failure, cardiac conduction disorders, severe renal and hepatic insufficiency, thyrotoxicosis, acute pancreatitis, concomitant use with monoamine oxidase inhibitors (MAOIs) or within 15 days after discontinuation of MAOI therapy, thromboembolic disease, granulocytopenia.

Interaction with other medicinal products and other forms of interaction.

Should not be used concomitantly with other vasoconstrictive agents (regardless of the route of administration), or with antihypertensive drugs (ß-adrenergic blockers), since phenylephrine may cause severe hypertension in some individuals due to stimulation of α-adrenergic receptors.

Atropine sulfate blocks the reflex bradycardia caused by phenylephrine and enhances the vasopressor response to phenylephrine. Concurrent use of phenylephrine with ß-adrenergic blockers may lead to arterial hypertension and excessive bradycardia with possible heart block. Use with caution together with thyroid hormones and drugs affecting cardiac conduction (cardiac glycosides, antiarrhythmic agents).

When used concomitantly with drugs causing potassium loss, such as certain diuretics like furosemide, hypokalemia may be intensified and arterial sensitivity to vasopressor agents such as phenylephrine may be reduced.

Concomitant use of phenylephrine and other sympathomimetic agents may lead to additive stimulation of the central nervous system to an extremely high level, resulting in nervousness, irritability, and insomnia. Seizure attacks are also possible.

Physician consultation is required before using MAO inhibitors if phenylephrine is to be applied in the anorectal area. MAO inhibitors used prior to starting phenylephrine therapy potentiate the cardiac and pressor effects of phenylephrine due to reduced metabolism of phenylephrine.

When applying Relief® ointment rectally in the anal area, the excipient white soft paraffin may reduce the strength and safety of latex condoms used simultaneously with the drug.

Special precautions for use

In case of significant bleeding from the anus or presence of symptoms persisting for 7 days of treatment, or if the condition worsens, additional consultation with a proctologist is required.

This medicinal product should be used with caution in patients with arterial hypertension, cardiovascular or cerebrovascular diseases, hyperthyroidism (phenylephrine may cause adverse cardiovascular effects, especially when high doses are used or in sensitive individuals), and in patients with closed-angle glaucoma.

Patients with diabetes mellitus should use this medicinal product with caution: phenylephrine may increase blood glucose concentration. These effects are usually transient and mild but may increase with doses exceeding the recommended levels. Blood glucose levels should therefore be monitored more closely.

Patients with urinary retention due to prostate hypertrophy or tumors: phenylephrine may worsen urinary voiding in patients with prostate hypertrophy due to spasm of the smooth muscles of the bladder neck caused by stimulation of α₁-adrenoceptors.

Use of the drug in patients with hepatitis or urinary disorders is permissible only after careful assessment of the benefit-risk ratio, as determined by the physician.

Potential interaction between phenylephrine applied locally in the anorectal area and MAO inhibitors should be considered, especially if sufficient systemic absorption occurs, as this may potentiate hypertensive effects.

Potential for phenylephrine applied locally in the anorectal area to cause severe hypertension due to stimulation of α-adrenoceptors should be considered, particularly in patients concurrently using antihypertensive agents.

To minimize systemic effects, the recommended dose should not be exceeded unless otherwise directed by a physician.

Use during pregnancy or breastfeeding

As the safety of using Relif® (phenylephrine) during pregnancy has not been studied, the drug may be used only if, in the physician’s opinion, the benefit to the mother outweighs the potential risk to the fetus/child.

Pregnant women should consult a physician before starting treatment with this drug.

It is unknown whether local application of Relif® (phenylephrine) results in sufficient systemic absorption to lead to measurable excretion in breast milk. Therefore, the physician must decide whether the importance of the drug for the mother warrants discontinuation of breastfeeding or discontinuation of the drug.

Studies on the effect of the drug on fertility have not been conducted.

Ability to influence reaction speed when driving or operating machinery
No effects on the ability to drive or operate machinery have been observed.

Method of Administration and Dosage

For adults and children aged 12 years and older, the medication should be used after completing hygienic procedures. Remove the protective cap from the applicator. Attach the applicator to the tube and squeeze out an adequate amount of ointment to fill the applicator. Carefully apply the ointment via the applicator to the affected areas externally or internally around the anus, in an amount sufficient to cover the affected areas, up to 4 times daily, preferably in the evening, in the morning, or after each bowel movement. Continue use until symptoms resolve. After each use, thoroughly wash the applicator and return it to the protective cap. Do not use if the protective covering is missing or damaged.

Children. The efficacy and safety of Relief® in children under 12 years of age have not been studied. Data are lacking.

Overdose.

Overdose has not been reported in medical practice; there are no data on systemic, including toxic, reactions of the body in response to rectal administration of Relief®. However, in case of overdose, an intensification of adverse reactions may occur, especially with prolonged use. Possible symptoms include arterial hypertension, chest pain and discomfort, palpitations, dyspnea, non-cardiogenic pulmonary edema, excitement, seizures, sleep disturbances, anxiety, paranoia, irritability, hallucinatory psychoses, weakness, anorexia, nausea, vomiting, oliguria, urinary retention, facial flushing, cold sensation in the extremities, paresthesia, increased sensitivity, hyperglycemia, hypokalemia, reduced blood flow to vital organs, which may lead to impaired renal perfusion, metabolic acidosis, and increased cardiac workload due to elevated total peripheral vascular resistance. Treatment is symptomatic.

Side effects.

This medicinal product is generally well tolerated, but in isolated cases adverse reactions associated with phenylephrine hydrochloride may occur.

Cardiovascular system: reflex bradycardia, arrhythmia, possible disturbances in heart rhythm, increased arterial pressure.

Immune system: allergic reactions, including cross-reactions in patients with allergy to other sympathomimetics, which may manifest as rashes, itching, angioedema.

Endocrine system: worsening of hyperthyroidism symptoms.

Skin and subcutaneous tissues: contact dermatitis.

Nervous system: dizziness, nervousness, headache, tremor, insomnia, feeling of fear, sensation of facial flushing.

At the site of application: irritation, hyperemia, rash, itching, swelling, mild pain/burning sensation in case of injury or bleeding from the anus.

Methylparahydroxybenzoate and propylparahydroxybenzoate may cause allergic reactions (possibly delayed) and, in rare cases, bronchospasm. Lanolin may cause local skin reactions (e.g. contact dermatitis). Benzoic acid may moderately irritate skin, eyes, and mucous membranes.

Shelf life. 2 years.

Opening the tube and starting to use the product does not affect the shelf life, provided the tube is tightly closed with the cap after each use. Do not use after the expiry date stated on the packaging.

Storage conditions.

Keep out of reach of children, at a temperature not exceeding 25 °C.

Packaging. Primary: sealed laminated tube with a plastic cap.

Secondary: cardboard box. Supplied with a rectal applicator and instructions for medical use.

Supply classification. Over-the-counter (without prescription).

Manufacturer.

Famar A.V.E. Avlon Plant /
Famar A.V.E. Avlon Plant.

Manufacturer's address and location of operations.

49th km National Road Athens-Lamia, Avlona Attiki, 19011, Greece /
49th km National Road Athens-Lamia, Avlona Attiki, 19011, Greece.