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

Active ingredient

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

Interaction

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

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

Overdose

Pregnancy use