Relifipine, gel 20 mg/g+3 mg/g 20 g

Pharmacotherapeutic group

Hemorrhoid treatment

ATX code: C05AXO3.

Pharmacological properties Pharmacodynamics

Nifedipine

Nifedipine is a selective slow calcium channel blocker, a 1,4-dihydropyridine derivative. The mechanism of action in rectal administration is associated with reduction of extracellular calcium flow inside the smooth muscle cells of the sphincter of the anus. Nifedipine eliminates hypertonicity of the sphincter of the anus, which in turn leads to a reduction in the severity of pain in patients with hemorrhoids and anal fissures. Decrease of sphincter sphincter tone of the anal canal improves blood supply to ischemic zones of the mucous membrane of the anal canal and improves its functional condition. Pharmacological activity of nifedipine causes reduction of the intensity of the inflammatory reaction and has a modulating effect on the microcirculation.

Lidocaine

Lidocaine is a local anesthetic. Its mechanism of action when used rectally is due to disruption of the functional activity of sodium channels, which prevents the generation of pain impulses in the endings of sensitive nerves and conduct of pain impulses along the nerve fibres. The analgesic effect develops 1-5 minutes after application of the drug to the skin or mucous membranes and lasts 30-60 minutes.

Pharmacokinetics

Nifedipine is practically not absorbed when applied topically, being determined in blood plasma at therapeutically insignificant concentration, insufficient for determination of other pharmacokinetic parameters.

Lidocaine when applied to the mucous membranes is absorbed and enters the systemic bloodstream. It is metabolized in the liver (90-95%) by oxidative N-dealkylation, hydrolysis of the amide bond and hydroxylation of the aromatic ring to form 4-hydroxy-2,6-xylidine, which is the main metabolite. It is excreted mainly by the kidneys as this metabolite.

Indications

Treatment of anal fissures against the background of chronic hemorrhoids; symptomatic treatment of acute hemorrhoids.

Active ingredient

Lidocaine, Nifedipine

Composition

1 g of the drug contains:

The active ingredients:

Lidocaine hydrochloride monohydrate 0.0213 g (in terms of lidocaine hydrochloride) (0.0200 g)

Nifedipine 0.0030 g

Excipients:

Poloxamer 188 0.0500 g

Poloxamer 407 0.1750 g

Polyethylene oxide 400 (Macrogol 400) 0.3000 g

Methyl parahydroxybenzoate (Nipagin) 0.0007 g/p>

Sodium hydroxide (sodium hydroxide) 0.0007 g

Propylparahydroxybenzoate (nipazole) 0.0003 g

Purified water up to 1 g

How to take, the dosage

The combined preparation lidocaine + nifedipine should be used after preliminary hygienic treatment of the perianal area 2 times a day: in the morning and in the evening at intervals of about 12 hours for not more than 28 days. Press a small amount of gel (about the size of a pea) onto your finger, apply it to the skin around the anus and into the anal canal to a depth of 1 cm. To overcome sphincter resistance, apply the gel with the tip of your finger.

Interaction

Interaction of the combined drug lidocaine + nifedipine with other drugs has not been studied in experimental studies in animals. When concomitant use of the drug with antiarrhythmic drugs prolongation of the QT interval is possible, in very rare cases, ventricular fibrillation may occur. When concomitant use of the drug with nitrate-containing drugs, arterial hypotension may occur in very rare cases.

Special Instructions

Physician should be consulted regarding the lack of indication for surgical treatment of anal fissure.

Ingestion of the gel or contact with the eyes should be avoided. If you accidentally get gel in your eyes, flush them with copious amounts of water.

Wash hands thoroughly after using the gel.

In this clinical trial the efficacy and safety of treatment with Relifipin was evaluated in patients with anal fissures associated with chronic stage 1-2 hemorrhoids. Efficacy was not evaluated in patients with anal fissures against the background of chronic stage 3-4 hemorrhoids and in the presence of more than one anal fissure. If there is a history of rectal surgery, Relifipin should be used with caution and under medical supervision.

The effect on the ability to drive vehicles, machinery

It has not been revealed.

Synopsis

Homogeneous gel of light yellow to yellow color. Air bubbles may be present.

Contraindications

High sensitivity to the drug components; age under 18 years; pregnancy; breast-feeding; anal fissure complicated by abscess, fistula; cancer diseases of the large intestine and rectum; rectal stenosis; significant arterial hypotension, chronic heart failure with unstable hemodynamic parameters, Crohn’s disease, signs of infectious affection of the rectum.
With caution
Surgical interventions on the rectum in the anamnesis.

Side effects

Allergic reactions, anaphylactic shock, very rare – reactions at the injection site (pain, burning, itching, hyperemia), rectal bleeding.

Overdose

If the drug is accidentally taken orally (several grams of gel are swallowed) or if an excessive amount of the drug is administered rectally, the most severe reactions are possible from the cardiovascular system (decreased blood pressure, bradycardia, bradyarrhythmia, sinus node suppression, cardiac arrest) and central nervous system (convulsions, respiratory depression, respiratory arrest). Treatment is symptomatic.

Pregnancy use

Lidocaine + nifedipine combination drug has not been investigated in pregnant women and during breastfeeding. It is contraindicated for use during pregnancy and breastfeeding.