Procto-gливенол

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT Procto-Glyvenol (Procto-Glyvenol)

Composition:

Active substances: tribenoside, lidocaine base;

1 suppository contains 400 mg of tribenoside and 40 mg of lidocaine base;

Excipients: solid fat No. 1 (Witepsol E 85), solid fat No. 2 (Witepsol W35).

Pharmaceutical form. Rectal suppositories.

Main physicochemical characteristics: yellowish-white, torpedo-shaped suppositories, without grooves, firm, not soft, slightly oily, with a faint characteristic odor.

Pharmacotherapeutic group. Medicinal products for the treatment of hemorrhoids and anal fissures for local use. Other preparations, combinations. ATC code C05AX03.

Pharmacological Properties.

Pharmacodynamics.

Tribenoside belongs to agents for local treatment of hemorrhoids. Tribenoside reduces capillary permeability and increases vascular tone, possessing anti-inflammatory properties. The antagonistic action of the drug is directed against certain endogenous substances that act as mediators in the development of inflammation and pain.

Lidocaine is a local anesthetic that relieves itching, burning, and pain caused by hemorrhoids.

Pharmacokinetics.

Absorption. Systemic bioavailability of tribenoside after rectal administration is only 30% of that achieved with oral or intravenous administration. Maximum plasma concentration of tribenoside and its metabolites is reached 2 hours after rectal administration of 400 mg tribenoside and amounts to 1 μg/mL.

Lidocaine is rapidly absorbed from mucous membranes but poorly absorbed from intact skin. Bioavailability of lidocaine after rectal administration is approximately 50%. Maximum plasma concentration of lidocaine is reached 112 minutes after rectal administration of 300 mg lidocaine and amounts to 0.70 μg/mL.

Distribution. Lidocaine is significantly bound to alpha₁-acid glycoprotein.

Metabolism. Tribenoside is actively metabolized in the body. Lidocaine is rapidly metabolized in the liver.

Excretion. Between 20% and 27% of the rectally administered dose of tribenoside is excreted in urine as metabolites.

Metabolites of lidocaine and less than 10% of unchanged lidocaine are excreted in urine.

Clinical characteristics.

Indications.

Local treatment of external and internal hemorrhoids.

Contraindications.

Hypersensitivity to any component of the medicinal product, including amide-type local anesthetics.

Interaction with other medicinal products and other forms of interaction.

Patients receiving Class 1 antiarrhythmic agents (e.g., tocainide, mexiletine) or other local anesthetics should use the medicinal product with caution due to the risk of additive systemic effects from lidocaine. Monoamine oxidase inhibitors enhance the local analgesic effect of lidocaine.

Special precautions for use.

The medicinal product should be used with caution in patients with severe cardiac, renal or hepatic insufficiency.

Patients are advised to consult a physician if their condition does not improve after one week of use, or if any new symptoms not previously observed appear, in order to exclude other possible causes of these disorders.

In addition, when treating hemorrhoids with Procto-Gливенол, patients should follow recommendations regarding hygiene of the anal area, active lifestyle and healthy diet to ensure soft consistency of stools.

Contact of the medicinal product with eyes should be avoided.

Suppositories must not be swallowed.

Use during pregnancy or breastfeeding

Pregnancy and breastfeeding

Controlled studies on the potential effects of tribenoside and lidocaine in pregnant or breastfeeding women have not been conducted. As a precaution, Procto-Gливенол rectal suppositories should not be used during the first trimester of pregnancy.

The medicinal product may be used from the 4th month of pregnancy and in breastfeeding women, according to the recommended dosage, taking into account the potential risk for both mother and child.

Fertility

Studies show that lidocaine does not affect fertility.

There are no data on the potential effect of tribenoside on fertility.

Ability to influence reaction rate when driving or operating machinery

The use of Procto-Gливенол does not affect or has negligible effect on the ability to drive or operate machinery.

Method of Administration and Dosage

Administer rectally to adults.

One rectal suppository should be administered in the morning and in the evening until acute symptoms disappear. After that, the dose may be reduced to one suppository per day. The duration of treatment is determined by the physician depending on the severity of the disease.

Children.

Do not use in children, as there is no data available on the use of the medicinal product in this age group.

Overdose.

There are no data on overdose with Procto-Gливенол. Overdose is not expected if the drug is used according to the recommended dosage regimen.

In animal studies, lidocaine overdose was associated with effects on the central nervous and cardiovascular systems.

In case of accidental oral ingestion of the medicinal product, gastric lavage should be performed promptly and medical advice should be sought. There is no specific antidote for lidocaine.

Side effects.

Rare side effects reported during treatment include local reactions such as burning, pain, rash, and itching, which may spread beyond the application site. In addition to these adverse effects, the use of Procto-Gливенол rectal suppositories may very rarely cause an anaphylactic reaction, including symptoms such as angioneurotic edema (Quincke's edema) and facial swelling.

List of side effects.

The side effects are listed below by system organ classes according to MedDRA. Frequency of occurrence: very common (≥ 1/10); common (≥ 1/100 to <1/10); uncommon (≥ 1/1,000 to <1/100); rare (≥ 1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are listed in order of decreasing severity.

Immune system disorders
Very rare	Anaphylactic reactions
Cardiac disorders
Very rare	Cardiovascular disorders
Respiratory, thoracic and mediastinal disorders
Very rare	Bronchospasm
Skin and subcutaneous tissue disorders
Rare	Urticaria, contact dermatitis
Very rare	Quincke's edema
General disorders and administration site conditions
Rare	Sensation of discomfort, mild burning, itching, rash, pain at application site
Very rare	Facial swelling, fever, haemorrhoidal haemorrhages

Considering that lidocaine is rapidly absorbed from the mucous membrane, systemic effects are possible.

Shelf life.

5 years.

Storage conditions.

Store at a temperature not exceeding 30 °C.

Keep out of reach of children.

Packaging. 5 suppositories in an aluminum foil laminated with polyethylene and polypropylene; 2 blisters in a cardboard box.

Classification. Over-the-counter (without prescription).

Manufacturer.

TEMMELER ITALIA S.R.L.

Manufacturer’s address.

Via delle Industrie, 2, 20061, Carugate (MI), Italy.

INSTRUCTIONS

for medical use of the medicinal product

Procto-Glyvenol

(Procto-Glyvenol)

Composition:

Active substances: tribenoside, lidocaine base;

1 suppository contains tribenoside 400 mg, lidocaine base 40 mg;

Excipients: solid fat No. 1 (Witepsol E 85), solid fat No. 2 (Witepsol W35).

Pharmaceutical form. Rectal suppositories.

Main physicochemical properties: yellowish-white, torpedo-shaped suppositories, without grooves, firm, not soft, slightly oily, with a weak characteristic odor.

Pharmacotherapeutic group. Drugs for treatment of hemorrhoids and anal fissures for local use. Other preparations, combinations. ATC code C05AX03.

Pharmacological Properties

Pharmacodynamics

Tribenoside belongs to agents for local treatment of hemorrhoids. Tribenoside reduces capillary permeability and increases vascular tone, and has anti-inflammatory properties. The antagonistic effect of the drug is directed against certain endogenous substances that act as mediators in the development of inflammation and pain.

Lidocaine is a local anesthetic that relieves itching, burning, and pain caused by hemorrhoids.

Pharmacokinetics

Absorption. Systemic bioavailability of tribenoside after rectal administration is only 30% of that which would be achieved with oral or intravenous administration of the substance. Maximum plasma concentration of tribenoside and its metabolites is reached 2 hours after rectal administration of 400 mg tribenoside and amounts to 1 µg/mL.

Lidocaine is rapidly absorbed from the mucous membrane, but poorly absorbed from intact skin. Bioavailability of lidocaine after rectal administration is approximately 50%. Maximum plasma concentration of lidocaine is reached 112 minutes after rectal administration of 300 mg lidocaine and amounts to 0.70 µg/mL.

Distribution. Lidocaine is significantly bound to alpha1-acid glycoprotein.

Metabolism. Tribenoside is actively metabolized in the body. Lidocaine is rapidly metabolized in the liver.

Excretion. From 20% to 27% of the rectally administered dose of tribenoside is excreted in urine as metabolites.

Metabolites of lidocaine and less than 10% of unchanged lidocaine are excreted in urine.

Clinical characteristics.

Indications.

Local treatment of external and internal hemorrhoids.

Contraindications.

Hypersensitivity to any component of the medicinal product, including amide-type local anesthetics.

Interaction with other medicinal products and other forms of interaction.

Patients taking Class 1 antiarrhythmic agents (e.g., tocainide, mexiletine) or other local anesthetics should use the medicinal product with caution due to the risk of additive systemic effects from lidocaine. Monoamine oxidase inhibitors enhance the local analgesic effect of lidocaine.

Special precautions for use.

The medicinal product should be used with caution in patients with severe heart failure, renal failure, and hepatic failure.

Patients are advised to consult a physician if their condition does not improve after one week of treatment, or if any new symptoms not previously observed appear, in order to rule out other possible causes of these disorders.

Additionally, when treating hemorrhoids with the medicinal product Procto-Gливенол, it is necessary to follow recommendations regarding hygiene of the anal area, an active lifestyle, and healthy diet to ensure soft bowel movements.

Avoid contact of the medicinal product with the eyes.

Suppositories must not be swallowed.

Use during pregnancy or breastfeeding

Pregnancy and breastfeeding

Controlled studies on the potential effects of tribenoside and lidocaine in pregnant women or women who are breastfeeding have not been conducted. As a precaution, Procto-Gливенол rectal suppositories should not be used during the first trimester of pregnancy.

The medicinal product may be used from the 4th month of pregnancy and in breastfeeding women, following the recommended dosage, while considering the potential risk to both mother and child.

Fertility

Studies indicate that lidocaine does not affect fertility.

There are no data available on the potential effect of tribenoside on fertility.

Ability to influence reaction speed when driving vehicles or operating machinery

The use of Procto-Gливенол has no effect or has a negligible effect on the ability to drive vehicles or operate machinery.

Method of Administration and Dosage

Administer rectally to adults.

One rectal suppository should be administered in the morning and in the evening until acute symptoms disappear. After that, the dose may be reduced to one suppository per day. The duration of treatment is determined by the physician depending on the severity of the disease course.

Children.

Do not use in children, as there are no data on the use of this medicinal product in this age group.

Overdose.

There are no data on overdose with Procto-Gливенол. Overdose is not expected if the drug is used according to the recommended dosage regimen.

In animal studies, lidocaine overdose was associated with effects on the central nervous and cardiovascular systems.

In case of accidental oral ingestion of the medicinal product, gastric lavage should be performed promptly and medical advice should be sought. There is no specific antidote for lidocaine.

Adverse reactions.

Rare adverse reactions reported during treatment include local reactions such as burning, pain, rash, and pruritus, which may extend beyond the application site. In addition to these undesirable effects, the use of Procto-Gливенол rectal suppositories may very rarely cause an anaphylactic reaction, including symptoms such as angioedema (Quincke's edema) and facial swelling.

List of adverse reactions.

Adverse reactions are listed below by system organ classes according to MedDRA. Frequency of occurrence: very common (≥ 1/10); common (≥ 1/100 to <1/10); uncommon (≥ 1/1,000 to <1/100); rare (≥ 1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are listed in order of decreasing severity.

Immune system disorders
Very rare	Anaphylactic reactions
Cardiac disorders
Very rare	Cardiovascular disorders
Respiratory, thoracic and mediastinal disorders
Very rare	Bronchospasm
Skin and subcutaneous tissue disorders
Rare	Urticaria, contact dermatitis
Very rare	Quincke's edema (angioedema)
General disorders and administration site conditions
Rare	Feeling of discomfort, mild burning, itching, rash, pain at application site
Very rare	Facial swelling, fever, hemorrhoidal hemorrhages

Since lidocaine is rapidly absorbed from the mucous membrane, systemic effects are possible.

Shelf life.

5 years.

Storage conditions.

Store at a temperature not exceeding 30 °C.

Keep out of reach of children.

Packaging.

5 suppositories in an aluminum foil laminated with polyethylene and polypropylene, 2 blisters in a cardboard box.

Prescription status. Over-the-counter.

Manufacturer.

Delfarm Unieux S.A.S.

Manufacturer's address and place of business.

26 rue de la Chapelle, 68330 Unieux, France.

INSTRUCTIONS

for medical use of the medicinal product

Procto-Glyvenol

(Procto-Glyvenol)

Composition:

Active substances: tribenoside, lidocaine base;

1 suppository contains 400 mg of tribenoside and 40 mg of lidocaine base;

Excipients: solid fat No. 1 (Witepsol E 85), solid fat No. 2 (Witepsol W35).

Pharmaceutical form. Rectal suppositories.

Main physicochemical properties: yellowish-white, torpedo-shaped suppositories, without grooves, firm, not soft, slightly oily, with a weak characteristic odor.

Pharmacotherapeutic group. Drugs for treatment of hemorrhoids and anal fissures for local use. Other combinations. ATC code C05AX03.

Pharmacological properties.

Pharmacodynamics.

Tribenoside belongs to agents for local treatment of hemorrhoids. Tribenoside reduces capillary permeability and increases vascular tone, and has anti-inflammatory properties. The antagonistic action of the drug is directed against certain endogenous substances that play a role as mediators in the development of inflammation and pain.

Lidocaine is a local anesthetic that relieves itching, burning, and pain caused by hemorrhoids.

Pharmacokinetics.

Absorption. Systemic bioavailability of tribenoside after rectal administration is only 30% of that which would be achieved with oral or intravenous administration of the substance. Maximum plasma concentration of tribenoside and its metabolites is reached 2 hours after rectal administration of 400 mg of tribenoside and amounts to 1 μg/mL.

Lidocaine is rapidly absorbed from the mucous membrane, but poorly absorbed from intact skin. Bioavailability of lidocaine after rectal administration is approximately 50%. Maximum plasma concentration of lidocaine is reached 112 minutes after rectal administration of 300 mg of lidocaine and amounts to 0.70 μg/mL.

Distribution. Lidocaine is significantly bound to alpha₁-acid glycoprotein.

Metabolism. Tribenoside is actively metabolized in the body. Lidocaine is rapidly metabolized in the liver.

Excretion. From 20% to 27% of the rectally administered dose of tribenoside is excreted in urine as metabolites.

Metabolites of lidocaine and less than 10% of unchanged lidocaine are excreted in urine.

Clinical characteristics.

Indications.

Local treatment of external and internal haemorrhoids.

Contraindications.

Hypersensitivity to any component of the medicinal product, including amide local anaesthetics.

Interaction with other medicinal products and other forms of interaction.

Patients receiving Class 1 antiarrhythmic agents (e.g., tocainide, mexiletine) or other local anaesthetics should use the medicinal product with caution due to the risk of additive systemic effects arising from the presence of lidocaine. Monoamine oxidase inhibitors enhance the local analgesic effect of lidocaine.

Special precautions for use.

The medicinal product should be used with caution in patients with severe heart failure, renal impairment, and hepatic impairment.

Patients are advised to consult a physician if there is no improvement after one week of treatment, or if any new symptoms not previously observed appear, in order to rule out other possible causes of these disorders.

In addition, when treating hemorrhoids with Procto-Gливенол, it is recommended to follow hygiene practices for the anal area, maintain an active lifestyle, and adhere to a healthy diet to ensure soft bowel movements.

Contact of the medicinal product with the eyes must be avoided.

Suppositories must not be swallowed.

Use during pregnancy or breastfeeding

Pregnancy and breastfeeding

Controlled studies on the potential effects of tribenoside and lidocaine in pregnant women or women who are breastfeeding have not been conducted. As a precaution, Procto-Gливенол rectal suppositories should not be used during the first trimester of pregnancy.

The medicinal product may be used from the 4th month of pregnancy and in breastfeeding women, following the recommended dosage regimen, taking into account the potential risk for both mother and child.

Fertility

Studies indicate that lidocaine does not affect fertility.

There are no data available on the potential effect of tribenoside on fertility.

Ability to influence reaction speed when driving vehicles or operating machinery

The use of Procto-Gливенол does not affect or has negligible effect on the ability to drive vehicles or operate machinery.

Method of administration and dosage.

Administer rectally to adults.

One rectal suppository should be administered in the morning and in the evening until acute symptoms disappear. After that, the dose may be reduced to one suppository per day. The duration of treatment is determined by the physician depending on the severity of the disease.

Children.

Do not use in children, as there is no data available on the use of the medicinal product in this age group.

Overdose.

There are no data on overdose with the medicinal product Procto-Glyvenol. Overdose is not expected if the drug is used according to the recommended dosage regimen.

In animal studies, overdose of lidocaine was associated with effects on the central nervous and cardiovascular systems.

In case of accidental oral ingestion of the medicinal product, the stomach should be promptly washed out and medical advice should be sought. There is no specific antidote for lidocaine.

Side effects

Rare side effects reported during treatment include local reactions such as burning, pain, rash, and itching, which may extend beyond the application site. In addition to these adverse effects, the use of Procto-Glyvenol rectal suppositories may very rarely cause an anaphylactic reaction, including symptoms such as Quincke's edema and facial swelling.

List of side effects

Side effects are listed below by system organ classes according to MedDRA. Frequency of occurrence: very common (≥ 1/10); common (≥ 1/100 to <1/10); uncommon (≥ 1/1,000 to <1/100); rare (≥ 1/10,000 to <1/1,000); very rare (<1/10,000); unknown (cannot be estimated from the available data). Within each frequency group, side effects are presented in order of decreasing severity.

Immune system
Very rare	Anaphylactic reactions
Cardiac disorders
Very rare	Cardiovascular disorders
Respiratory, thoracic and mediastinal disorders
Very rare	Bronchospasm
Skin and subcutaneous tissue disorders
Uncommon	Urticaria, contact dermatitis
Very rare	Angioedema (Quincke's edema)
General disorders and administration site conditions
Uncommon	Sensation of discomfort, mild burning, itching, rash, pain at application site
Very rare	Facial swelling, fever, haemorrhoidal haemorrhage

Since lidocaine is rapidly absorbed from the mucous membrane, systemic effects are possible.

Shelf life.

5 years.

Storage conditions.

Store at a temperature not exceeding 30 °C.

Keep out of reach of children.

Packaging. 5 suppositories in an aluminum foil, laminated with polyethylene and polypropylene; 2 blisters in a cardboard box.

Availability. Over-the-counter.

Manufacturer.

ZETA FARMACEUTICI S.P.A.

Manufacturer's location and address of business activity.

VIA GALVANI, 10 - 36066 SANDRIGO (VI), Italy.