Active ingredients: Nifedipine, Lidocaine
ANTROLIN 0.3% + 1.5% rectal cream
Why is Antrolin used? What is it for?
PHARMACOTHERAPEUTIC CATEGORY
Medicinal product containing nifedipine, dihydropyridine with calcium-antagonist action which, when used locally, has a relaxing effect on peripheral smooth muscle and can reduce the tone of the internal anal sphincter. The action of nifedipine is integrated into the product by the presence of lidocaine, a local surface anesthetic.
THERAPEUTIC INDICATIONS
Treatment of anal fissure and proctalgia generally associated with anal sphincter hypertonus.
Contraindications When Antrolin should not be used
Hypersensitivity to the active ingredients and in particular to lidocaine (and other local anesthetics with a similar structure of the amide type) or to any of the excipients.
Known or suspected pregnancy and lactation (see also "Special warnings").
Severe hypotensive states and cardiovascular insufficiency.
Precautions for use What you need to know before taking Antrolin
During the clinical trial, no undesirable effects resulting from a possible systemic absorption of the drug were reported. ANTROLIN rectal cream must however be used with extreme caution in patients who have severely damaged mucous membranes and inflammation in the region to be treated, as in such situations there could be an excessive absorption of the active ingredients. Furthermore, the medicine should be used with caution in diabetic patients or in those with severe hepatic and / or renal insufficiency.
Treatment with ANTROLIN rectal cream should be carried out under medical supervision in very elderly patients, as well as in those under the age of 18 and in patients being treated with beta-blocking or antihypertensive drugs.
It is advisable to check the blood pressure at the beginning and periodically during the treatment. In case of failure of the therapy (absence of improvement or worsening of the symptoms) it is necessary to suspend the treatment and consult the doctor for other measures.
Interactions Which drugs or foods can modify the effect of Antrolin
Due to the presence of nifedipine, the effect of antihypertensive drugs could be enhanced by the use of ANTROLIN rectal cream. Propanolol prolongs the plasma half-life of lidocaine and increases the plasma levels of nifedipine. Cimetidine may increase the plasma levels of lidocaine and nifedipine. Co-administration of ANTROLIN rectal cream in patients treated with digoxin may lead to increased levels of levels plasma digoxin.
Warnings It is important to know that:
The topical application of the drug in excessive doses and / or for prolonged periods of time can give rise to sensitization phenomena and local reactions of hyperemia and bleeding, which disappear when treatment is suspended.
Use in pregnancy and during lactation
Nifedipine and lidocaine cross the placental barrier and are excreted in breast milk. In studies in rats and rabbits, nifedipine was shown to cause teratogenic effects. Lidocaine did not highlight any risks to the fetus. However, it is recommended not to use the product in pregnant and lactating women.
Warnings related to some excipients present in the medicinal product
ANTROLIN rectal cream contains sodium methyl p-hydroxybenzoate and propyl p-hydroxybenzoate which can cause allergic reactions, even delayed. In addition, ANTROLIN rectal cream contains propylene glycol and cetostearyl alcohol which can cause local skin reactions (eg contact dermatitis).
KEEP THE MEDICINAL PRODUCT OUT OF THE REACH AND SIGHT OF CHILDREN.
Dosage and method of use How to use Antrolin: Dosage
For endorectal and perianal applications.
Apply the cream 2 times a day for at least three weeks.
Method of administration
- Lie down on the bed on the left side;
- unscrew the cap from the tube and screw the cannula into it, let out a small amount of cream to lubricate the cannula and insert it into the anus;
- press the end of the tube, let out the cream contained in about one centimeter of the tube (one centimeter of the tube contains about 2.5 - 3 g of cream).
Overdose What to do if you have taken an overdose of Antrolin
No cases of systemic toxicity from overdose have been reported after topical application of ANTROLIN rectal cream. In the event of intoxication after topical application of the product, the systemic effects should be similar to those induced by the active ingredients with other routes of administration.
In cases of severe Nifedipine intoxication, disturbances of consciousness up to coma, drop in blood pressure and altered heart rhythm and cardiogenic shock may occur. As for the treatment, beta-sympathomimetics can be used for bradycardic heart rhythm disturbances and, in case of severe hypotension, calcium gluconate (10-20ml of 10% solution slowly intravenously) and possibly dopamine or noradrenaline.
Most of the toxic reactions to local anesthetics and lidocaine in humans affect the CNS; there is a sensation of "light-headedness" and dizziness, often followed by visual and auditory disturbances, such as accommodation difficulties and tinnitus and in the most severe cases, CNS depression and convulsions Treatment is symptomatic.
Side Effects What are the side effects of Antrolin
Reactions such as pain, burning, itching, hyperemia and bleeding may occur locally.
These effects subside after discontinuation of treatment.
In very rare cases, local application of lidocaine preparations has caused allergic reactions (in severe cases anaphylactic shock.
During the clinical trial phase, no undesirable effects due to possible systemic absorption of the two active ingredients (headache, dizziness, peripheral vasodilation, hypotension, dizziness and tremors) were highlighted.
Notify your doctor or pharmacist of any undesirable effects that are not described or cannot be explained here.
Expiry and Retention
Check the expiration date indicated on the package
Store in a tightly closed package; store at a temperature not exceeding 25 ° C.
The expiry date refers to the product in intact packaging, correctly stored.
The validity of the product after first opening is 30 days (write the date of first opening in the space provided on the tube)
WARNING: Do not use the medicine after the expiry date indicated on the package and after 30 days from the first opening
Keep this medicine out of the reach of children
Composition and pharmaceutical form
COMPOSITION
100 g of cream contain:
Active ingredients: Nifedipine g 0.3 - Lidocaine hydrochloride g 1.5 -
Excipients: White Vaseline Propylene glycol, Liquid semisynthetic glycerides, Polyethylene glycolstearate, Cetostearyl alcohol, Glyceryl monostearate, Sodium methyl p-hydroxybenzoate, Propyl p-hydroxybenzoate, Purified water.
PHARMACEUTICAL FORM AND CONTENT
Rectal cream. 30 g aluminum tube, with cannula, in cardboard box.
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT
ANTROLIN
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
100 g of cream contain:
Active principles:
Nifedipine 0.3 g
Lidocaine hydrochloride 1.5 g
For excipients see 6.1
03.0 PHARMACEUTICAL FORM
Rectal cream
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Treatment of anal fissure and proctalgia generally associated with anal sphincter hypertonus.
04.2 Posology and method of administration
For endorectal and perianal applications. Apply the cream twice a day for at least three weeks (see Section 6.6).
04.3 Contraindications
Hypersensitivity to the active ingredients and in particular to lidocaine (and other local anesthetics with a similar structure of the amide type) or to any of the excipients.
Known or suspected pregnancy and lactation (see Section 4.6).
Severe hypotensive states and cardiovascular insufficiency.
04.4 Special warnings and appropriate precautions for use
The topical application of the drug in excessive doses and / or for prolonged periods of time can give rise to sensitization phenomena and local reactions of hyperemia and bleeding, which disappear when treatment is suspended.
During the clinical trial, no undesirable effects resulting from a possible systemic absorption of the drug were reported. ANTROLIN rectal cream must however be used with extreme caution in patients who have severely damaged mucous membranes and inflammation in the region to be treated, as in such situations there could be an excessive absorption of the active ingredients.
Furthermore, the medicine should be used with caution in diabetic patients or in those with severe hepatic and / or renal insufficiency.
Treatment with ANTROLIN rectal cream should be under medical supervision in very elderly patients, as well as in those under the age of 18 and in patients being treated with beta-blocking or antihypertensive drugs.
It is advisable to check blood pressure at the beginning and periodically during treatment.
In case of therapy failure (absence of improvement or worsening of symptoms), it is necessary to suspend the treatment and consult the doctor for other measures.
Warning: ANTROLIN rectal cream contains sodium methyl p-hydroxybenzoate and propyl p-hydroxybenzoate which can cause allergic reactions, even delayed. In addition, ANTROLIN rectal cream contains propylene glycol and cetostearyl alcohol which can cause local skin reactions (eg contact dermatitis).
Keep this medicine out of the reach and sight of children.
04.5 Interactions with other medicinal products and other forms of interaction
Due to the presence of nifedipine, the effect of antihypertensive drugs could be enhanced by the use of ANTROLIN rectal cream. Propanolol prolongs the plasma half-life of lidocaine and increases the plasma levels of nifedipine. Cimetidine may increase the plasma levels of lidocaine and nifedipine. Co-administration of ANTROLIN rectal cream in patients receiving digoxin may result in increased plasma levels of digoxin.
04.6 Pregnancy and lactation
Nifedipine and lidocaine cross the placental barrier and are excreted in breast milk. In studies in rats and rabbits, nifedipine was shown to cause teratogenic effects. Lidocaine did not highlight any risks to the fetus. However, it is recommended not to use the product in pregnant and lactating women.
04.7 Effects on ability to drive and use machines
Nifedipine, if taken orally at the same time as alcoholic beverages, can reduce the ability to react. In the case of ANTROLIN rectal cream, the product is intended to be administered and act locally. Therefore, effects that could affect the ability to drive or use machines are not foreseeable.
04.8 Undesirable effects
Reactions such as pain, burning, itching, hyperemia and bleeding may occur locally. These effects subside after discontinuation of treatment.
In very rare cases, local application of lidocaine preparations has caused allergic reactions (in severe cases, anaphylactic shock).
During the clinical trial phase, no undesirable effects due to possible systemic absorption of the two active ingredients (headache, dizziness, peripheral vasodilation, hypotension, dizziness and tremors) were highlighted.
04.9 Overdose
There have been no reports of systemic toxicity from overdose with ANTROLIN rectal cream. In the event of intoxication after topical application of the product, the systemic effects should be similar to those usually induced by the active ingredients with other routes of administration.
In cases of severe Nifedipine intoxication, disturbances of consciousness up to coma, drop in blood pressure, altered heart rhythm and cardiogenic shock may occur. Regarding the treatment, beta-sympathomimetic drugs can be used for bradycardic heart rhythm disturbances and, in case of severe hypotension, calcium gluconate (10-20 ml of 10% solution slowly intravenously) and possibly dopamine or noradrenaline.
Most of the toxic reactions to local anesthetics and lidocaine affect the CNS; there is a sensation of "light head" and dizziness, often followed by visual and auditory disturbances, such as accommodation difficulties and tinnitus. In severe cases, CNS depression and convulsions may occur. Treatment is symptomatic.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: ATC code C05AX - Other antihemorrhoids for topical use.
The mechanism of action of ANTROLIN is synergistic. Nifedipine, a dihydropyridine with a calcium-antagonist action, exerts, if used locally, a relaxing action on peripheral smooth muscles. It works by reducing the hypertonicity of the internal anal sphincter muscle. The action of nifedipine is integrated into the product by the presence of lidocaine, a local surface anesthetic.
05.2 Pharmacokinetic properties
The pharmacokinetic properties of ANTROLIN rectal cream were studied in healthy volunteers. The determination of the active ingredients in the blood, carried out with a validated analytical method, gave a negative result, as the presence of nifedipine was not detected in any serum. Furthermore, only minimal traces of lidocaine were found in 2 out of 12. These very low concentrations (below the quantization limits of the method) are in any case much lower than the therapeutically effective ones found after systemic administration. Therefore, it is reasonable to exclude that local application of Antrolin may cause the appearance of systemic effects resulting from the absorption of its active ingredients. To further confirm this, no undesirable effects resulting from the systemic absorption of the two active ingredients by the anorectal mucosa were highlighted during clinical studies.
05.3 Preclinical safety data
An acute toxicity study performed in rats revealed no toxic or lethal effects up to administration of 50 times the single therapeutic dose. Subacute toxicity tests have shown that Antrolin rectal cream does not significantly change the blood chemistry parameters of the treated animals and is well tolerated. In a study on the irritant potential of the medicine, conducted in rabbits, Antrolin was classified as "non-irritating".
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
White petroleum jelly; Propylene glycol, liquid semisynthetic glycerides; polyethylene glycolstearate; cetostearyl alcohol; glyceryl monostearate; sodium methyl p-hydroxybenzoate; propyl p-hydroxybenzoate; purified water.
06.2 Incompatibility
As compatibility studies have not been conducted, the medicinal product must not be mixed with other products.
06.3 Period of validity
Intact packaging: 3 years.
After first opening: 30 days
06.4 Special precautions for storage
Store in tightly closed packaging, at a temperature not exceeding 25 ° C.
06.5 Nature of the immediate packaging and contents of the package
Aluminum tube of 30 g of cream with cannula, in cardboard box.
06.6 Instructions for use and handling
Lie down on the bed on your left side, unscrew the cap from the tube and screw the cannula into it, let out a small amount of cream to lubricate the cannula and insert it into the anus. Press the end of the tube, let out the cream contained in about a centimeter of tube (one centimeter of the tube contains about 2.5 - 3 g of cream).
07.0 MARKETING AUTHORIZATION HOLDER
New.Fa.Dem srl Pharmaceuticals and chemicals with registered office and production workshop in Viale Ferrovie dello Stato, A.S.I. Giugliano in Campania NA
08.0 MARKETING AUTHORIZATION NUMBER
035396011
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
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10.0 DATE OF REVISION OF THE TEXT
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