ANTROLIN RECTAL CREAM 30G

ANTROLIN




International nonproprietary name

No



Dosage form

Rectal cream 30 g

Compound

100 g of cream contain

active substances

Nifedipine  0.3 g

Lidocaine hydrochloride   1.5 g

White paraffin, propylene glycol, medium chain triglycerides, macrogol stearate, cetostearyl alcohol, glyceryl monostearate, sodium methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified water.

Description

Homogeneous yellow cream with a slight characteristic odor.




Pharmacotherapeutic group

Other antihemorrhoidal drugs for topical use.

ATX code C05AX

Pharmacological properties

Pharmacokinetics

The pharmacokinetic properties of ANTROLIN cream for rectal use were studied in healthy volunteers. Determination of active substances in the blood using an analytical method had negative results; Nifedipine was not detected in the blood serum

In addition, only minimal traces of lidocaine were detected in 2 of 12 patients. These low concentrations are, however, well below those that are therapeutically effective following systemic administration. Therefore, the systemic effect of ANTROLIN cream as a result of absorption of active substances is excluded. To further confirm this, no adverse reactions caused by systemic absorption of the two active ingredients in the anorectal mucosa were observed during clinical studies.

Lidocaine

The absorption and bioavailability of lidocaine after rectal administration of the cream and suppository is about 30 and 24%, respectively. T1/2 of lidocaine from blood plasma is 1-2 hours. In the human body, lidocaine is metabolized by 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, and with 70% of the drug is excreted in the urine as this metabolite.

Pharmacodynamics

The mechanism of action of ANTROLIN cream for rectal use is of the synthetic type. Nifedipine, a dihydropyridine with calcium channel blocker activity, when applied topically, has a relaxing effect on peripheral smooth muscle. Nifedipine acts by reducing hypertonicity of the anal sphincter. Nifedipine acts together with lidocaine, a local anesthetic, which is also included in the drug.

Lidocaine

Lidocaine is a local anesthetic: pain relief is achieved by suppressing the formation and conduction of nerve impulses along afferent nerve fibers by depolarizing sodium channels.

Indications for use

- treatment of anal fissures and proctological diseases associated with hypertonicity of the anal sphincter.




Directions for use and doses

For endorectal and perianal use. Apply the cream twice daily for at least three weeks.

Method of administration

Lie on your left side, remove the cap from the tube and secure the cannula, squeeze out a small amount of cream to lubricate the cannula and insert it into the anus. Press the tube to squeeze out approximately one centimeter of cream (one centimeter contains approximately 2.5-3 g of cream).

Contraindications

- hypersensitivity to the active substances, in particular to lidocaine (and other local anesthetics of the amide type) or to any other excipients in the composition of the drug

- suspected or confirmed pregnancy and breastfeeding

- severe hypotension and heart failure

- children and adolescents under 18 years of age (due to the lack of efficacy and safety data)

Special instructions

Treatment with ANTROLIN rectal cream may cause the effect of antihypertensive drugs due to the presence of nifedipine. Propanol prolongs the plasma half-life of lidocaine and increases plasma levels of nifedipine. Cimetidine may increase plasma levels of nifedipine and lidocaine. Concomitant use of ANTROLIN rectal cream in patients taking digoxin may result in increased plasma digoxin levels.

Pregnancy and lactation Nifedipine and lidocaine cross the placental barrier and enter breast milk. Studies in rats and rabbits have shown that nifedipine may be teratogenic. Lidocaine has not been shown to pose any risk to the fetus. However, this drug is not recommended for pregnant and lactating women. Features of the effect of the drug on the ability to drive vehicles or potentially dangerous mechanisms

Nifedipine, when taken orally with alcohol, may adversely affect the ability to react. ANTROLIN cream for rectal use is intended for topical use and acts locally. There is no reason to believe that this drug may affect the ability to control machinery.



Treatment: in case of accidental ingestion, gastrointestinal lavage is recommended, as well as symptomatic supportive therapy.




Release form and packaging

30 g of the drug in an aluminum tube, sealed with a cap. One tube, along with a cannula and instructions for use in the state and Russian languages, is placed in a cardboard box.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children!

Shelf life

3 years

After opening: 30 days

Do not use after the expiration date indicated on the package.







Conditions for dispensing from pharmacies

On prescription




Manufacturer

New.Fa.Dem. S.r.l.

Viale Ferrovie dello Stato Zona A.S.I., Giugliano in Campania (NA), Italy.




Registration Certificate Holder

New.Fa.Dem. S.r.l.

Viale Ferrovie dello Stato Zona A.S.I., Giugliano in Campania (NA), Italy.