Instructions for Nifecain cream rectal tube 30 g
Composition
active ingredients: nifedipine, lidocaine hydrochloride;
1 g of cream contains nifedipine 3 mg and lidocaine hydrochloride 15 mg;
Excipients: white soft paraffin, propylene glycol, medium chain triglycerides, macrogol stearate, cetostearyl alcohol (type A) emulsified, glycerol monostearate, sodium methylparaben (sodium methylparahydroxybenzoate), propylparaben (propylparahydroxybenzoate), purified water.
Dosage form
Rectal cream.
Main physicochemical properties: homogeneous yellow cream with a slight characteristic odor.
Pharmacotherapeutic group
Topical hemorrhoid and anal fissure treatment products. Other drugs, combinations.
ATX code C05A X03.
Pharmacological properties
Pharmacodynamics.
Nifedipine has a synergistic mechanism of action. Nifedipine is a dihydropyridine calcium channel blocker that, when applied topically, has a relaxing effect on peripheral smooth muscle. Nifedipine acts by reducing hypertonicity of the internal anal sphincter.
Pharmacokinetics.
The pharmacokinetic properties of Nifekain rectal cream were studied in healthy volunteers. Determination of the active substances in the blood using a validated analytical method gave negative results, since nifedipine was not detected in the blood serum. In addition, only minimal traces of lidocaine were detected in 2 patients out of 12. These ultra-low concentrations (below the limit of quantification) are much lower than the concentrations capable of exerting a therapeutic effect with systemic use of lidocaine. Therefore, a systemic effect of Nifekain cream as a result of absorption of the active substances can be excluded. This was confirmed by further clinical studies, during which no undesirable effects were observed due to systemic absorption through the mucous membrane of the anorectal area.
Indication
Treatment of anal fissures and proctalgia associated with anal sphincter hypertonicity.
Contraindication
Hypersensitivity to the active substances, in particular to lidocaine and other amide-type local anesthetics, such as bupivacaine, etidocaine, mepivacaine and prilocaine, or to any of the excipients included in the preparation.
Expected or confirmed pregnancy and breastfeeding period (see section "Use during pregnancy or breastfeeding").
Severe hypotension and heart failure.
Interaction with other medicinal products and other types of interactions
Interaction studies have not been conducted.
Patients taking class I antiarrhythmic drugs (e.g. tocainide, mexiletine) or other local anesthetics should use the drug with caution, as there is a risk of cumulative systemic effects due to the presence of lidocaine. Monoamine oxidase inhibitors enhance the local analgesic effect of lidocaine.
Treatment with Nifecain rectal cream may enhance the effect of antihypertensive agents due to the presence of nifedipine.
Propranolol prolongs the half-life of lidocaine and increases the plasma levels of nifedipine.
Cimetidine may increase plasma levels of nifedipine and lidocaine.
Concomitant use of Nifecain rectal cream by patients taking digoxin may lead to increased plasma digoxin levels.
Application features
Local application of the drug in excessive doses and/or for a long period of time may cause sensitization, local hyperemia and bleeding, which disappear after discontinuation of treatment.
During clinical trials, no undesirable effects due to possible systemic absorption of the drug were recorded.
Nifecain rectal cream should be used with extreme caution in patients with serious mucosal damage and inflammation in the area to be treated, as excessive absorption of the active ingredients is possible in such situations.
Nifecaine should be used with caution in patients with diabetes mellitus or severe hepatic and/or renal insufficiency.
Treatment with Nifecain rectal cream in elderly patients, as well as patients receiving beta-blockers or antihypertensive drugs, should be carried out under the supervision of a physician.
It is recommended to check blood pressure at the beginning of treatment and periodically throughout therapy.
If treatment is ineffective (no improvement or worsening of symptoms), it should be discontinued and a doctor should be consulted.
In addition, when treating hemorrhoids with Nifecain rectal cream, it is recommended to follow the rules of anal hygiene, maintain an active lifestyle, and follow a healthy diet to ensure soft stools.
Glycerol monostearate, which is part of the drug, can have a mild laxative effect.
Use during pregnancy or breastfeeding
Nifedipine and lidocaine cross the placental barrier and are excreted in breast milk. Studies in rats and rabbits have shown that nifedipine is teratogenic. Lidocaine has not shown any risk to the fetus.
Acute pulmonary edema has been observed when calcium channel blockers, including nifedipine, have been used as tocolytic agents during pregnancy, especially in cases of multiple pregnancy (twins or more), intravenously and/or with concomitant use of beta-2 agonists.
Therefore, this drug is not recommended for use by pregnant and breastfeeding women.
Ability to influence reaction speed when driving vehicles or other mechanisms
Simultaneous administration of nifedipine with alcohol may adversely affect reaction speed.
The drug Nifecain, rectal cream, is intended for topical use and acts locally, therefore it is not possible to predict the effect of the drug on the ability to drive vehicles or other mechanisms.
Method of administration and doses
For endorectal and perianal use. Apply the cream twice daily for at least three weeks.
Method of use: Lie on your left side, remove the cap from the tube and fix the cannula, squeeze out a small amount of cream to lubricate the cannula and insert it into the anus. Press the end of the tube to squeeze out about one centimeter of cream (one centimeter of the tube contains about 2.5-3 g of cream).
Children
Not recommended for use in children due to lack of data on safety and efficacy.
Overdose
No cases of systemic toxicity due to overdose with topical application of Nifecain rectal cream have been reported. In case of poisoning following topical application of the drug, systemic effects are expected to be similar to those commonly observed with other routes of administration of active substances.
In case of severe nifedipine intoxication, disorders of consciousness may occur, including coma, decreased blood pressure, cardiac arrhythmias, and cardiogenic shock.
In case of accidental ingestion of the drug (in case of swallowing a few grams of cream), systemic symptoms caused by the use of lidocaine hydrochloride are expected. Depending on the dose, they may manifest themselves in the form of severe cardiovascular disorders (decreased blood pressure, increased sweating, pallor of the skin, bradycardia, arrhythmia, depression of cardiac function, shock, and in particularly severe cases - cardiac arrest) or reactions associated with disorders of the central nervous system (headache, dizziness, blurred vision, diplopia, tinnitus, drowsiness, numbness of the extremities, chills, anxiety, convulsions, dyspnea, and in particularly severe cases - respiratory failure). Methemoglobinemia is possible.
Treatment: In case of overdose, careful monitoring of vital signs, supportive measures to ensure oxygen levels, and symptomatic treatment of central nervous system and cardiovascular disorders are required, for example, beta-sympathomimetics can be used for bradycardia, atropine, and in case of severe hypotension, calcium gluconate (10–20 ml intravenously slowly of a 10% solution) and possibly dopamine or noradrenaline.
A significant proportion of toxic reactions to local anesthetics and lidocaine have CNS manifestations; dizziness occurs, often accompanied by visual and auditory disturbances, such as difficulty with accommodation and tinnitus. In the most severe cases, CNS depression and seizures are possible. Treatment is symptomatic.
Adverse reactions
Local reactions such as pain, burning, itching, redness and bleeding may occur. These effects subside upon discontinuation of treatment.
In very rare cases, topical use of lidocaine-containing products has caused allergic reactions (in severe cases, anaphylactic shock).
No adverse effects due to possible systemic absorption of the two active ingredients (headache, dizziness, peripheral vasodilation, hypotension, lightheadedness and tremor) were observed during clinical trials.
Frequency unknown: pulmonary edema*.
Systemic adverse reactions associated with lidocaine are identical in manifestations to those associated with local anesthetics of the amide group.
*Cases have been reported when used as a tocolytic during pregnancy (see section “Use during pregnancy or breastfeeding”).
Expiration date
3 years.
Use within 30 days after opening the tube.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
30 g of cream in a tube with a cap; 1 tube complete with a cannula in a cardboard box.
Vacation category
According to the recipe.
Producer
New.Fa.Dem. S.r.l.
Location of the manufacturer and address of its place of business.
ZONA INDUSTRIAL - 80014 GIUGLIANO IN CAMPANIA (NA), Italy
