Reliefipin (Gel) Instructions for Use

Marketing Authorization Holder

BAYER, JSC (Russia)

Manufactured By

C.P.M. Contractpharma GmbH (Germany)

Contact Information

BAYER AG (Germany)

ATC Code

C05AX03 (Preparations for the treatment of hemorrhoids and anal fissures in combination)

Active Substances

Nifedipine (Rec.INN registered by WHO)

Lidocaine (Rec.INN registered by WHO)

Dosage Form

Reliefipin

Gel for rectal and external use 20 mg+3 mg/1 g: tube 20 g

Dosage Form, Packaging, and Composition

Gel for rectal and external use from light yellow to yellow, homogeneous; the presence of air bubbles is allowed.

Excipients : poloxamer 188 – 0.05 g, poloxamer 407 – 0.165 g, polyethylene oxide 400 (macrogol 400) – 0.3 g, methylparahydroxybenzoate (nipagin) – 0.0007 g, sodium hydroxide – 0.00068 g, propylparahydroxybenzoate (nipasol) – 0.0003 g, purified water – up to 1 g.

20 g – aluminum tubes (1) – cardboard packs.

Clinical-Pharmacological Group

Drug for topical treatment of hemorrhoids

Pharmacotherapeutic Group

Hemorrhoid treatment agent

Pharmacological Action

A combined drug, the action of which is due to the properties of its constituent components.

Nifedipine is a selective blocker of slow calcium channels, a derivative of 1,4-dihydropyridine.

The mechanism of action during rectal application is associated with a decrease in the influx of extracellular calcium into the smooth muscle cells of the anal sphincter.

Nifedipine eliminates hypertonicity of the anal sphincter, which, in turn, leads to a reduction in pain severity in patients with hemorrhoids and anal fissure.

The reduction in anal sphincter tone contributes to improved blood supply to ischemic areas of the anal canal mucosa and improvement of its functional state.

The pharmacological activity of nifedipine causes a reduction in the intensity of the inflammatory reaction and has a modulating effect on microcirculation.

Lidocaine is a local anesthetic.

The mechanism of action during rectal application is due to the disruption of the functional activity of sodium channels, which prevents the generation of pain impulses in the endings of sensory nerves and the conduction of pain impulses along nerve fibers.

The analgesic effect develops 1-5 minutes after application of the drug to the skin or mucous membranes and lasts for 30-60 minutes.

Pharmacokinetics

Nifedipine

With external application, it is practically not absorbed, being detected in blood plasma at a therapeutically insignificant concentration, insufficient for determining other pharmacokinetic parameters.

Lidocaine

Absorption

When applied to mucous membranes, it is absorbed and enters the systemic circulation.

Metabolism

It is metabolized in the liver (by 90-95%) through oxidative N-dealkylation, hydrolysis of the amide bond, and hydroxylation of the aromatic ring with the formation of 4-hydroxy-2,6-xylidine, which is the main metabolite.

Excretion

It is excreted mainly by the kidneys in the form of this metabolite.

Indications

• Anal fissures against the background of chronic hemorrhoids;
• Symptomatic treatment of acute hemorrhoids.

ICD codes

Dosage Regimen

The drug should be applied after preliminary hygiene of the perianal area 2 times/day in the morning and evening with an interval of about 12 hours for no more than 28 days.

Squeeze a small amount of gel (approximately the size of a pea) onto a finger, apply it to the skin around the anus and into the anal canal cavity to a depth of 1 cm. To overcome the resistance of the sphincter, apply the gel with the fingertip.

Adverse Reactions

Possible allergic reactions, anaphylactic shock, very rarely – reactions at the application site (pain, burning, itching, hyperemia), rectal bleeding.

Contraindications

• Hypersensitivity to the components of the drug;
• Anal fissure complicated by the presence of an abscess, fistula;
• Oncological diseases of the large intestine and rectum;
• Stenosis of the rectum;
• Severe arterial hypotension;
• Chronic heart failure with unstable hemodynamic parameters;
• Crohn’s disease;
• Signs of infectious lesions of the rectum;
• Pregnancy;
• Breastfeeding period;
• Age under 18 years.

With caution surgical interventions on the rectum in the anamnesis.

Use in Pregnancy and Lactation

The combined drug lidocaine + nifedipine has not been studied in pregnant women and during breastfeeding.

The use of the drug is contraindicated during pregnancy and breastfeeding.

Pediatric Use

Contraindicated for use under the age of 18 years.

Special Precautions

It is necessary to consult a doctor regarding the absence of indications for surgical treatment of anal fissure.

It is necessary to avoid swallowing the gel or contact with the eyes. If the gel accidentally gets into the eyes, rinse them with plenty of water.

After applying the gel, wash hands thoroughly.

In the conducted clinical study, the efficacy and safety of treatment with Reliefipin were evaluated in patients with anal fissure against the background of chronic hemorrhoids of stages 1-2.

Efficacy was not evaluated in patients with anal fissure against the background of chronic hemorrhoids of stages 3-4 and in the presence of more than one anal fissure. In case of a history of surgical intervention on the rectum, the drug should be used with caution, under medical supervision.

Effect on the ability to drive vehicles and mechanisms

Not identified.

Overdose

Symptoms in case of accidental oral intake of the drug (swallowing several grams of gel) or rectal administration of an excessive amount of the drug, the most severe reactions are possible from the cardiovascular system (decreased blood pressure, bradycardia, bradyarrhythmia, suppression of sinus node function, cardiac arrest) and the central nervous system (convulsions, respiratory depression, respiratory arrest).

Treatment symptomatic therapy.

Drug Interactions

The interaction of the drug with other drugs has not been studied in experimental animal studies.

With simultaneous use of the drug with antiarrhythmic drugs, QT interval prolongation is possible; in very rare cases, the development of ventricular fibrillation is possible. With simultaneous use of the drug with nitrate-containing agents, in very rare cases, the development of arterial hypotension is possible.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

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.