Active ingredients: Mesalazine (5-aminosalicylic acid)
PENTACOL "400 mg gastro-resistant modified release tablets"
PENTACOL "800 mg gastro-resistant modified release tablets"
PENTACOL "500 mg rectal gel"
PENTACOL "1.5 g granules for rectal suspension"
PENTACOL "2 g rectal foam"
PENTACOL "4 g rectal foam"
PENTACOL "4g / 100ml Rectal suspension"
PENTACOL "500mg suppositories"
Indications Why is Pentacol used? What is it for?
PHARMACOTHERAPEUTIC CATEGORY
Intestinal antiphlogistics - mesalamine.
Therapeutic indications
Modified-release gastro-resistant tablets
Ulcerative colitis, Crohn's disease, intestinal idiopathic inflammation, acute and chronic, localized in the distal ileum and colon.
Rectal gel
Ulcerative proctitis, Crohn's disease, acute and chronic intestinal idiopathic inflammation of anorectal and perianal localization.
Granules for rectal suspension
Ulcerative colitis, acute and chronic intestinal idiopathic inflammation with rectosigmoid localization.
Rectal foam
Ulcerative colitis and acute and chronic intestinal idiopathic inflammation with rectosigmoid localization, left colon and distal portion of the transversus.
Rectal suspension
Rectosigmoid ulcerative colitis.
Suppositories
Ulcerative colitis with rectal localization.
PENTACOL is indicated both in the treatment of the active phases of the disease and in the prevention of relapses. In the severe active phase it is advisable to combine it with cortisone treatment.
Contraindications When Pentacol should not be used
Hypersensitivity to the active substance, to salicylates or to any of the excipients listed in the "Composition" section. Peptic ulcer in active phase. Severe nephropathies. Children under two years of age. Avoid using the product during the last weeks of pregnancy. Avoid using the tablets in children under 6 years of age.
Precautions for use What you need to know before taking Pentacol
Particular caution should be observed in patients with renal and hepatic impairment and in subjects under treatment of oral hypoglycemic agents, diuretics, coumarins and corticosteroids. Prolonged use of the product can give rise to sensitization phenomena. Its use should be avoided in patients with overt renal insufficiency.
Interactions Which drugs or foods can modify the effect of Pentacol
Tell your doctor or pharmacist if you have recently taken any other medicines, even those without a prescription.
During treatment with PENTACOL gastro-resistant modified-release tablets, avoid the intake of lactulose or other products which, by lowering the pH of the colon, can prevent the release of the drug contained in the tablets. See also Precautions for use.
Warnings It is important to know that:
Relapses of objective and subjective symptoms can occur both after discontinuation of treatment with PENTACOL and during inadequate maintenance treatment. In patients who have exceptionally slow gastric digestion or are carriers of pyloric stenosis, it may sometimes be possible to have a release of 5-ASA already in the stomach, with consequent gastric irritation and a loss of efficacy of the drug.
Pregnancy and breastfeeding
Ask your doctor or pharmacist for advice before taking any medicine.
In women who are pregnant, whether known or presumed, it must be used only in case of real need and under the direct supervision of a doctor. The use of the product should be avoided in the last weeks of pregnancy. Mesalazine is not excreted in breast milk.
Effects on ability to drive and use machines
PENTACOL does not affect the ability to drive or use machines.
Important information about some of the ingredients
PENTACOL rectal foam and PENTACOL rectal gel contain E218 methylhydroxy benzoate and E216 propylhydroxy benzoate.
PENTACOL rectal suspension contains E218 methyl hydroxy benzoate
They can cause allergic reactions (even delayed).
PENTACOL rectal foam contains propylene glycol. It can cause skin irritation.
Dose, Method and Time of Administration How to use Pentacol: Posology
400 mg and 800 mg modified release gastro-resistant tablets
Dosage
Ulcerative colitis
Phase of maintenance of remission
In adults, the average dose is 2.4 g / day (6 tablets of 400 mg, or 3 tablets of 800 mg) divided into two or three doses per day.
Phase of induction of remission of ulcerative colitis
In mild acute forms of the disease, the recommended starting daily dose is 2.4 g (6 tablets of 400 mg, or 3 tablets of 800 mg), in two or three divided doses; in acute moderate forms of the disease, the dose can be increased up to 4 g per day (10 tablets of 400 mg, or 5 tablets of 800 mg), divided into two or three divided doses.
Crohn's disease and acute and chronic intestinal idiopathic inflammation localized in the distal ileum and colon
In adults, the average dose is 2 tablets of 400 mg, or 1 tablet of 800 mg, three times a day. In the acute phases the dose can be increased up to 10 tablets of 400 mg or 5 tablets of 800 mg per day, according to the doctor's opinion.
In case of first treatment it is advisable to reach the full dosage after a few days of treatment, gradually increasing the dosage.
There is only limited documentation in favor of an effect in children (aged 6 to 18 years).
Children aged 6 years and over: the dosage should be determined individually by the doctor. It is generally recommended that half the adult dose be administered to children weighing up to 40 kg and the normal adult dose to children over 40 kg.
Avoid using the tablets in children under 6 years of age. The duration of treatment in the active phases is 4-6 weeks. During remission of the disease, which requires long-term maintenance treatment to prevent relapse, the frequency and dosage of PENTACOL gastro-resistant modified-release tablets will be determined by your doctor.
Method of administration
PENTACOL tablets should be swallowed whole (not split or chewed) with a glass of water and between meals.
Rectal gel
Dosage
PENTACOL 500 mg rectal gel is a formulation that allows the drug to be brought immediately into contact with the mucosa affected by the pathological process, in particular in cases where the anal canal, sphincters and perianal area are involved, not directly reachable with the others. available mesalamine formulations (suppositories and enemas).
In the active phase of the disease, the average daily dose for adults is 1.5 g of mesalazine, equal to one tube of PENTACOL gel three times a day at regular intervals, unless otherwise judged by the doctor.
There is little experience and only limited documentation in favor of an effect in children. For children over two years of age, proportionally reduced doses, in the judgment of the physician.
The duration of treatment, in the active phase, is 4-6 weeks.
During remission of the disease, which requires long-term maintenance care to prevent recurrence, the frequency and dosage of PENTACOL gel will be determined by the doctor.
Method of administration
The product should be applied with faeces-free alvo. How Pentacol Gel is applied:
- Unscrew the cap of the single-dose tube and use it (upside down) to pierce the sealing membrane of the tube.
- Remove the cannula from its protective wrapping and screw it onto the tube.
- Gently insert the cannula into the anal orifice and squeeze the contents of the tube completely.
- Spread around the perianal area any excess gel that has come out of the anus.
- Discard the empty tube in the waste container.
Granules for rectal suspension
Dosage
Average scheme for adults in the active phase, unless otherwise advised by the doctor: one enema of 1.5 g (one sachet) of mesalamine twice a day, morning and evening, or one enema of 3 g (two sachets) of mesalamine per day, in the evening before bedtime.
There is little experience and only limited documentation in favor of an effect in children. For children over two years of age, proportionally reduced doses, in the judgment of the physician.
The duration of treatment in the active phases is 4-6 weeks. During remission of the disease, which requires long-term maintenance care to prevent recurrence, the frequency and dosage of PENTACOL granules for rectal suspension will be determined by the doctor.
Method of administration
The extemporaneous enemas of PENTACOL granules for rectal suspension can be prepared with variable dosage and volume, using 1 or 2 enema sachets (1.5 g or 3 g of mesalazine) in volumes from 50 to 100 ml of water, according to the opinion of the physician and the patient's capacity for "retention".
To prepare the enema, as illustrated below, introduce the prescribed dose of mesalazine into the graduated bottle attached to the package and bring to the desired volume with warm or cold tap water. Then screw the rectal cannula to the bottle and shake about a minute, to obtain a homogeneous suspension. The enema is now ready to be administered. The enema should be performed with the intestine free from faeces.
Then remove the cannula cover and, in a lying position on the left side and folded right leg, introduce the cannula into the rectum in the direction of the navel and press the bottle until its contents are completely instilled in the intestine.
To obtain a better therapeutic result, it is recommended that the patient remain lying down for at least 30 minutes, rotating the body on the right and left side in order to favor the contact of the medicine on a larger surface of the intestinal mucosa. In any case, the enema must be held for as long as possible. In patients who find it difficult to hold the 100 ml enemas, it is recommended to start the treatment with a smaller volume, for example 50 ml, subsequently increasing it to the level of safe "retention", following the graduation engraved on the bottle. After administration, unscrew and discard only the used cannula, while the bottle should be rinsed and reused for other enemas with the remaining rectal cannulae attached.
Rectal foam
Dosage
Average scheme in the active phase, unless otherwise prescribed by the doctor:
Adults: 2 g of mesalazine, once or twice a day, morning and evening, or 4 g of mesalazine, in the evening before going to bed.
Children over two years of age, doses halved, in the opinion of the physician. There is little experience and only limited documentation in favor of an effect in children.
DAILY DOSAGE SCHEDULE
Cross over the administrations made during the day.
Attention: the semi-dose (reduced dosage) is obtained with a single pressure; use the same cannula properly cleaned for the administration of a second half-dose after some time.
The full dose is obtained with two consecutive presses.
The duration of treatment, in the active phase, is 4-6 weeks.
During remission of the disease, which requires long-term maintenance care to prevent recurrence, the frequency and dosage of PENTACOL, rectal foam, will be determined by the doctor.
Method of administration
PENTACOL rectal foam should be administered with the alvus free from faeces.
To administer the full dose of 130 ml of foam (from 2 grams or 4 grams of mesalazine) you have to press down and immediately release the can cap for two consecutive times.
By pressing the cap once, half a dose is dispensed, exactly pre-measured: 1 gram or 2 grams of mesalazine. With the delivery of a half-dose the volume of the foam enema is also halved to 65 ml.
PENTACOL rectal foam is then delivered in two exactly premeasured half doses, which must be administered consecutively when the full dose is prescribed (2 or 4 grams of mesalamine). However, the two semi-doses can also be used separately at time intervals, if the doctor deems it appropriate to use reduced and more fractionated dosages.
Warning: the foam is dispensed only when the cap is released and not while it is being pressed (see diagrams 1, 2 and 3 below). The can only works upside down.
The entire dose is dispensed in two half-doses, obtainable by pressing the cap of the can twice consecutively. A residue of product is expected to remain in the can.
INSTRUCTIONS FOR A CORRECT APPLICATION OF THE ENEMA OF PENTACOL RECTAL FOAM
- Shake the container vigorously under pressure before use.
- Remove the plastic safety tab located under the cap.
- Insert the rectal cannula into the nozzle. Turn the cap so as to align the underlying semicircular notch with the nozzle.
- In an upright position, place one foot on a chair and slowly insert the cannula along its entire length into the rectum, in the direction of the navel, with the container under pressure upside down. A preventive lubrication of the cannula will facilitate its insertion. upside down, press firmly and release, two consecutive times, the cap, to instill the entire dose, 130 ml of foam into the rectum. In case the doctor prescribes to halve the dose, press and release the cap only once Then keep the container for subsequent dispensing.
N.B. - Each pressurized multidose container delivers 14 semidoses of rectal foam, each of 1g and 2g of mesalamine. Each pack contains 7 rectal cannulas; each cannula must be used for the administration of one dose or two half doses.
The therapeutic effect of the foam enema is considerably improved if the patient lies down for at least 30 minutes after application, turning from time to time to the right and left, to favor the contact of the drug on a larger surface of the colonic mucosa. The rectal foam must be held for as long as possible, even all night or all the time between an enema and the other.
WARNING: THE CONTAINER UNDER PRESSURE WORKS ONLY IN Upside Down. DO NOT PRESS FURTHER HOOD PRESSURE THAN THE TWO EXPECTED TO DELIVER A FULL DOSE.
Rectal suspension
Adults: 1 4g enema once a day, preferably in the evening before bedtime. Children: proportionally reduced doses in the opinion of the Doctor. There is little experience and only limited documentation in favor of an effect in children. Do not exceed the recommended doses. To avoid relapses, it is advisable to adopt a long-lasting treatment, gradually reducing the dosage adopted in the active phase of the disease.
Method of administration:
- Shake well before use to obtain a homogeneous suspension
- Remove the cannula cover
- To apply, lie down on the left side keeping the left leg straight and bending the right leg
- Insert the rectal cannula attached to the bottle into the anal orifice
- Compress the bottle with gradual and constant pressure until the bottle is completely empty
- After introducing the preparation, remain lying down in the position indicated above for about 30 minutes.
- A better efficacy of the product is obtained by leaving it in place overnight.
Suppositories
Adults: on average 3 suppositories a day, divided into 2-3 administrations in the active phase; 1-2 suppositories a day for the prevention of relapses. To avoid relapses, it is advisable to adopt a long-lasting treatment, gradually reducing the dosage adopted in the active phase of the disease.
Children: proportionally reduced doses in the opinion of the Doctor. There is little experience and only limited documentation in favor of an effect in children. Do not exceed recommended doses.
Method of administration: to obtain a better therapeutic effect it is important that the suppository is introduced after having evacuated and is kept for at least 30 minutes, or better, for longer periods (for example, for the whole night).
Overdose What to do if you have taken an overdose of Pentacol
There are no known cases of overdose. In the event that it occurs after administration of the tablets, resort to gastric lavage and infusion of electrolyte solutions. Cases of overdose following rectal administration are not conceivable.
In case of ingestion / intake of an excessive dose of PENTACOL, notify your doctor immediately or go to the nearest hospital.
If you have any questions about the use of PENTACOL, ask your doctor or pharmacist.
Side Effects What are the side effects of Pentacol
Like all medicines, PENTACOL can cause side effects, although not everybody gets them.
Rashes, itching, headaches, mild gastrointestinal disturbances (nausea, diarrhea, abdominal pain) may rarely occur during treatment with PENTACOL. The possible occurrence of hypersensitivity reactions involves the immediate interruption of treatment. If undesirable effects other than those described above arise, the patient is expressly invited to inform his doctor or pharmacist.
Compliance with the instructions contained in the package leaflet reduces the risk of undesirable effects.
Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. Undesirable effects can also be reported directly through the national reporting system at "https://www.aifa.gov.it/content/segnalazioni-reazioni-avverse". By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
Expiry: see the expiry date indicated on the package.
The expiry date refers to the product in intact and correctly stored packaging.
Warning: do not use the medicine after the expiry date indicated on the package.
Suppositories and tablets: store at a temperature not exceeding 30 ° C.
Rectal gel: store at a temperature not exceeding 25 ° C.
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines you no longer use. This will help protect the environment.
Composition and pharmaceutical form
Composition
PENTACOL 400 mg gastro-resistant modified release tablets
Each 400 mg tablet contains: Active ingredient: Mesalazine (5-aminosalicylic acid) 400 mg.
Excipients: microcrystalline cellulose; Sodium carboxymethyl starch; Cornstarch; Magnesium stearate; Polyvinylpyrrolidone; Mannitol; Precipitated silica; Copolymers of methacrylic acid; Talc; Titanium dioxide; Red iron oxide; Triethyl citrate.
PENTACOL 800 mg gastro-resistant modified release tablets
Each 800 mg tablet contains: Active ingredient: Mesalazine (5-aminosalicylic acid) 800 mg.
Excipients: microcrystalline cellulose; Sodium carboxymethyl starch; Cornstarch; Magnesium stearate; Polyvinylpyrrolidone; Mannitol; Copolymers of methacrylic acid; Talc; Titanium dioxide; Red iron oxide; Triethyl citrate.
PENTACOL 500 mg rectal gel
Each 5 g tube contains: Active ingredient: Mesalazine (5-aminosalicylic acid) 500 mg;
Excipients: Carboxypolymethylene, Triethanolamine, E218 methylhydroxy benzoate, E216 propylhydroxy benzoate, Glycerol, Purified water.
PENTACOL 1,5 granules for rectal suspensionEach sachet contains: Active ingredient: Mesalazine (5-aminosalicylic acid) g 1.50.
Excipients: microcrystalline cellulose; Polyvinylpyrrolidone; Dimethicone.
PENTACOL 2 g rectal foamEach container contains: Active ingredient: Mesalazine (5-aminosalicylic acid) g 2;
Excipients: Polysorbate 20; Emulsifying wax; E218 methylhydroxy benzoate, E216 propylhydroxy benzoate; Propylene glycol; Purified water; Propellants: Isobutane; Nitrogen.
PENTACOL 4 g rectal foamEach container contains: Active ingredient: Mesalazine (5-aminosalicylic acid) g 4;
Excipients: Polysorbate 20; Emulsifying wax; E218 methylhydroxy benzoate, E216 propylhydroxy benzoate; Propylene glycol; Purified water; Propellants: Isobutane; Nitrogen.
PENTACOL 4g / 100ml Rectal suspensionEach single-dose container contains: Active ingredient: mesalazine (5-aminosalicylic acid) g 4.
Excipients: Colloidal silica, Xanthan gum, Sodium carboxymethylcellulose, E218 methylhydroxy benzoate, Sodium metabisulphite, Concentrated phosphoric acid, Purified water.
PENTACOL 500mg suppositories
Each suppository contains: Active ingredient: mesalazine (5-aminosalicylic acid) 500 mg.
Excipients: Solid semisynthetic glycerides.
Pharmaceutical form and content
Modified-release gastro-resistant tablets
Box of 60 tablets of 400 mg of mesalazine; boxes of 30, 60 and 90 tablets of 800 mg of mesalazine.
Rectal gel
Boxes of 10 and 20 tubes in aluminum / epoxy-phenolic resin of 5 g, dosed at 500 mg of mesalazine.
Granules for rectal suspension
Box of 20 sachets of granules of 1.5 g of mesalazine, with attached soft plastic graduated bottle for the preparation and administration of enemas and 20 disposable rectal cannulas.
Rectal foam
2 g rectal foam - 7 single-dose containers under pressure.
Box of 7 containers of 130 ml dosed at 2 g of mesalazine, in aluminum / resin and attached rectal cannula.
4 g rectal foam - 7 single-dose containers under pressure.
Box of 7 containers of 130 ml dosed at 4 g of mesalazine, in aluminum / resin and attached rectal cannula.
2 g rectal foam - 1 pressurized container of 14 g + 7 cannulas.
Box of 1 pressurized container of 14 g in aluminum / resin equipped with 7 rectal cannulas, for 14 deliveries (semi-doses) of 1 g of mesalazine.
4 g rectal foam - 1 pressurized container of 28 g + 7 cannulas.
Box of 1 pressurized container of 28 g in aluminum / resin equipped with 7 rectal cannulas, for 14 deliveries (semi-doses) of 2 g of mesalazine.
Rectal suspension
4g / 100ml Rectal suspension - 7 single-dose containers with cannula
Box of 7 containers of 100ml, dosed at 4g of mesalazine, in polyethylene with rectal cannula.
Suppositories
Box of 20 suppositories of 500 mg in PVC / PE blister, sealed by heat sealing.
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
PENTACOL
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02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
PENTACOL 400 mg gastro-resistant modified release tablets - 60 tablets
Each tablet contains: Active principle: mesalazine (5-aminosalicylic acid) 400 mg.
PENTACOL 800 mg gastro-resistant modified release tablets - 30, 60 and 90 tablets
Each tablet contains: Active principle: mesalazine (5-aminosalicylic acid) 800 mg.
PENTACOL 500 mg rectal gel - 10 and 20 single-dose tubes of 5 g
Each 5g tube contains: Active principle: mesalazine (5-aminosalicylic acid) 500 mg.
PENTACOL 1.5 g granules for rectal suspension - 20 sachets
Each sachet contains: Active principle: mesalazine (5-aminosalicylic acid) g 1.5.
PENTACOL 2 g rectal foam - 7 single-dose pressurized containers
Each container contains: Active principle: mesalazine (5-aminosalicylic acid) g 2.
PENTACOL 4 g rectal foam - 7 single-dose pressurized containers
Each container contains: Active principle: mesalazine (5-aminosalicylic acid) g 4.
PENTACOL 2 g rectal foam - 1 pressurized container of 14 g + 7 cannulas
Each multidose container delivers 14 half doses, each corresponding to 1 g of mesalazine.
Each single dose contains: Active principle: mesalazine (5-aminosalicylic acid) g 2.
PENTACOL 4 g rectal foam - 1 pressurized container of 28 g + 7 cannulas
Each multidose container delivers 14 semi-doses, each corresponding to 2 g of mesalazine.
Each single dose contains: Active principle: mesalazine (5-aminosalicylic acid) g 4.
PENTACOL 4g / 100ml Rectal suspension - 7 single-dose containers with cannula
Each single-dose container contains: Active principle: mesalazine (5-aminosalicylic acid) g 4.
PENTACOL 500mg suppositories - 20 suppositories
Each suppository contains: Active principle: mesalazine (5-aminosalicylic acid) 500 mg.
For the full list of excipients: see section 6.1
03.0 PHARMACEUTICAL FORM
Modified Release Gastro-Resistant Tablets, Rectal Gel, Granules for Rectal Suspension, Rectal Foam, Rectal Suspension, Suppositories.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
PENTACOL gastro-resistant modified-release tablets: ulcerative colitis, Crohn's disease, acute and chronic intestinal idiopathic inflammation localized in the distal ileum and colon.
PENTACOL rectal gel: ulcerative proctitis, Crohn's disease, acute and chronic intestinal idiopathic inflammation with anorectal and perianal localization
PENTACOL granules for rectal suspension: ulcerative colitis, acute and chronic intestinal idiopathic inflammation with rectosigmoid localization.
PENTACOL rectal foam: ulcerative colitis, acute and chronic intestinal idiopathic inflammation with rectosigmoid localization, left colon and distal portion of the transversus.
PENTACOL rectal suspension: Ulcerative colitis with rectosigmoid localization.
PENTACOL suppositories: Ulcerative colitis with rectal localization.
PENTACOL is indicated both in the treatment of the active phases of the disease and in the prevention of relapses. In the severe active phase it is advisable to combine it with cortisone treatment.
04.2 Posology and method of administration
PENTACOL gastro-resistant modified-release tablets
Ulcerative colitis
Phase of maintenance of remission
In adults, the average dose is 2.4 g / day (6 tablets of 400 mg, or 3 tablets of 800 mg) divided into two or three doses per day.
Phase of induction of remission of ulcerative colitis
In mild acute forms of the disease, the recommended starting daily dose is 2.4 g (6 tablets of 400 mg, or 3 tablets of 800 mg), in two or three divided doses; in acute moderate forms of the disease, the dose can be increased up to 4 g per day (10 tablets of 400 mg, or 5 tablets of 800 mg), divided into two or three divided doses.
Crohn's disease and acute and chronic intestinal idiopathic inflammation localized in the distal ileum and colon
In adults, the average dose is 2 tablets of 400 mg, or 1 tablet of 800 mg, three times a day. In the acute phases the dose can be increased up to 10 tablets of 400 mg or 5 tablets of 800 mg per day, according to the doctor's opinion.
There is only limited documentation in favor of an effect in children (aged 6 to 18 years).
Children aged 6 years and over:
• Acute phases: the dosage must be determined individually, starting with 30-50 mg / kg / day in divided doses. Maximum dose: 75 mg / kg / day in divided doses. The total dose should not exceed 4 g / day (maximum adult dose).
• Maintenance treatment: the dosage should be determined individually, starting with 15-30 mg / kg / day in divided doses. The total dose should not exceed 2 g / day (recommended adult dose).
It is generally recommended that half the adult dose be administered to children weighing up to 40 kg and the normal adult dose to children over 40 kg.
Avoid using the tablets in children under 6 years of age.
PENTACOL tablets should be swallowed whole (not split or chewed) with a sip of water and away from meals. In the case of the first treatment it is advisable to reach the full dosage after a few days of treatment, gradually increasing the dosage. The duration of treatment. in the active phases it is 4-6 weeks.
In long-term treatments, to prevent relapses, the daily dosage to be observed must be established by the doctor, according to the patient's condition and the evolution of the disease.
PENTACOL rectal gel
PENTACOL gel, presented in single-dose 5 g tubes, dosed at 500 mg of mesalazine, allows the drug to be brought immediately into contact with the mucosa affected by the pathological process, in particular in cases where the anal canal, sphincters and the area are involved. perianal, not directly reachable with the other mesalamine formulations available (suppositories and enemas). In the active phase of the disease, the average daily dose for adults is 1.5 g of mesalazine, equal to three tubes of Pentacol rectal gel, unless otherwise doctor's judgment. The product should be applied with faecal-free alvo. There is little experience and only limited documentation in favor of an effect in children. For children over two years of age, proportionally reduced doses, according to medical prescription. The duration of treatment, in the active phase, is 4-6 weeks. During remission, which requires long-term maintenance treatment to prevent relapses, the frequency and dosage of Pentacol gel will be determined by the doctor.
How PENTACOL gel is applied:
1. Introduce the cannula (already inserted on the tube) into the anus along its entire length.
2. Squeeze the flexible tube with two fingers (thumb and index finger) until it is completely flattened.
3. Spread any excess gel from the anus around the perianal area.
4. Discard the empty tube in the waste container.
PENTACOL granules for rectal suspension
Average dosage schedule for adults in the active phase, unless otherwise advised by the doctor: a 1.5 g enema (one sachet) of mesalamine twice a day, morning and evening, or a 3 g enema (two sachets) of mesalamine day, in the evening before bedtime. To prepare the enema, introduce the prescribed dose of mesalazine, 1.5 g or 3 g (the content of one or two sachets of granules) into the graduated bottle attached to the package and make up to 100 ml with warm tap water or cold.
Then screw the rectal cannula to the bottle and shake for about one minute to obtain a homogeneous suspension. The enema is now ready to be administered. The enema must be practiced with the intestine free from faeces. To obtain a better therapeutic result, it is advisable that the patient remain lying down for at least 30 minutes, rotating the body on the right and left side in order to favor the contact of the medicine on a more extended surface of the intestinal mucosa. In any case, the enema should be held for as long as possible. In patients who find it difficult to hold the 100 ml enemas, it is recommended to start the treatment with a smaller volume, for example 50 ml, following the graduation engraved on the bottle. C "is little experience and only limited documentation in favor of an effect in children. For children over two years of age, proportionally reduced doses, in the opinion of the doctor.
The duration of treatment in the active phases is 4-6 weeks. During remission of the disease, which requires long-term maintenance care to prevent recurrence, the frequency and dosage of PENTACOL, granules for rectal suspension, will be determined by the doctor.
PENTACOL rectal foam
Average dosage in the active phase, unless otherwise prescribed by the doctor:
Adults: 2 g of mesalazine, once or twice a day or 4 g of mesalazine, in the evening before going to bed.
Children over two years of age: proportionally reduced doses, in the opinion of the doctor. There is little experience and only limited documentation in favor of an effect in children.
PENTACOL rectal foam should be administered with the alvus free from faeces. The duration of treatment in the active phases is 4-6 weeks. During remission of the disease, which requires long-term maintenance care to prevent recurrence, the frequency and dosage of PENTACOL rectal foam will be determined by the doctor. The therapeutic effect of the foam enema is greatly improved if the patient, after application, lies down for at least 30 minutes, slowly turning left and right, to favor the contact of the drug on a larger surface of the colonic mucosa. The foam enema must be held for as long as possible, even all night or all the time between one enema and the other. The delivery of the entire dose (2 or 4 g of mesalamine in 130 ml of foam) is it is obtained by pressing down the cap of the single-dose container under pressure and releasing it immediately afterwards, for two consecutive times, according to the instructions enclosed with the package.
With PENTACOL rectal foam it is therefore possible to dispense two semi-doses (even at time intervals), which can be used if the doctor deems it more appropriate to use reduced and more fractionated dosages.
PENTACOL rectal suspension.
Adults: 1 4g enema, once a day, preferably in the evening before going to bed. Children: proportionally reduced doses in the opinion of the Doctor. There is little experience and only limited documentation in favor of an effect in children. Do not exceed the recommended doses. To avoid relapses, it is advisable to adopt a long-lasting treatment, gradually reducing the dosage adopted in the active phase of the disease.
Method of administration:
1. Shake well before use to obtain a homogeneous suspension.
2. Remove the cannula cover.
3. For the application lie down on the left side keeping the left leg straight and bending the right leg.
4. Insert the rectal cannula attached to the bottle into the anal orifice.
5. Compress the bottle with gradual and constant pressure until the bottle is completely empty.
6. After introducing the preparation, remain lying down in the position indicated above for about 30 minutes.
7. A better efficacy of the product is obtained by leaving it in place overnight.
PENTACOL suppositories
Adults: on average 3 suppositories a day, divided into 2-3 administrations in the active phase; 1-2 suppositories a day for the prevention of relapses. To avoid relapses, it is advisable to adopt a long-lasting treatment, gradually reducing the dosage adopted in the active phase of the disease.
Children: proportionally reduced doses in the opinion of the Doctor. There is little experience and only limited documentation in favor of an effect in children. Do not exceed recommended doses.
Method of administration: to obtain a better therapeutic effect it is important that the suppository is introduced after having evacuated and is kept for at least 30 minutes, or better, for longer periods (for example, for the whole night).
04.3 Contraindications
Hypersensitivity to the active substance, to salicylates, or to any of the excipients listed in section 6.1.
Peptic ulcer in active phase. Severe nephropathies. Children under two years of age. Avoid use of the product during the last weeks of pregnancy (see 4.6). Avoid using the tablets in children under 6 years of age.
04.4 Special warnings and appropriate precautions for use
Relapses of objective and subjective symptoms can occur both after discontinuation of treatment with PENTACOL and during inadequate maintenance treatment. In patients who have exceptionally slow gastric digestion or are carriers of pyloric stenosis, 5-ASA may be released already in the stomach, resulting in gastric irritation and a loss of drug efficacy. Particular caution should be observed in patients with renal and hepatic impairment and in subjects under treatment of oral hypoglycemic agents, diuretics, coumarins and corticosteroids. Prolonged use of the product can give rise to sensitization phenomena. Its use should be avoided in patients with overt renal insufficiency.
Important information about some of the ingredients
PENTACOL rectal foam and PENTACOL rectal gel contain E218 methylhydroxy benzoate and E216 propylhydroxy benzoate.
PENTACOL rectal suspension contains E218 methyl hydroxy benzoate.
They can cause allergic reactions (even delayed).
PENTACOL rectal foam contains propylene glycol. It can cause skin irritation.
04.5 Interactions with other medicinal products and other forms of interaction
Avoid the simultaneous administration of PENTACOL gastro-resistant modified-release tablets and lactulose or other drugs which, by lowering the pH of the colon, may hinder the release of the active ingredient contained in the tablets. In cases of severe colitis, where it is considered appropriate, a treatment with corticosteroids can be advantageously combined with topical Pentacol.
04.6 Pregnancy and lactation
In women who are pregnant, whether known or suspected, PENTACOL should only be used if clearly needed and under the direct supervision of a doctor. However, the use of the product should be avoided in the last weeks of pregnancy. Mesalazine is not excreted in breast milk.
04.7 Effects on ability to drive and use machines
PENTACOL does not affect the ability to drive or use machines.
04.8 Undesirable effects
Only rarely can mild gastrointestinal disturbances (nausea, diarrhea, abdominal pain), itching, skin rashes, headaches occur.
The possible occurrence of hypersensitivity reactions involves the immediate interruption of treatment.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions that occur after authorization of the medicinal product is important, as it allows continuous monitoring of the benefit / risk ratio of the medicinal product.
Healthcare professionals are asked to report any suspected adverse reactions via the Italian Medicines Agency, website: https://www.aifa.gov.it/content/segnalazioni-reazioni-avverse
04.9 Overdose
There are no known cases of overdose. If it occurs after administration of the tablets, resort to gastric lavage or infusion of electrolyte solutions. Cases of overdose following rectal administration are not conceivable.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Therapeutic drug category: Intestinal antiphlogistics - mesalazine.
ATC code: A07EC02
The therapeutic usefulness of mesalazine (5-aminosalicylic acid or 5-ASA) in the treatment of acute and chronic inflammatory intestinal diseases (colitis and ulcerative proctitis, Crohn's disease) can now be considered an acquisition of great clinical importance. In these pathologies, mesalazine has an "exclusively topical anti-inflammatory action, while it is inactive and potentially nephrotoxic systemically. Mesalazine is the active metabolite of salazosulfapyridine (SASP), an azo compound used for decades in inflammatory diseases of the colon. Salazosulfapyridine for orally, it acts as a carrier of mesalazine, which is released in the intestine by cleavage of the azo compound by local bacteria. numerous undesirable side effects. In order to eliminate these serious drawbacks and to be able to use the active principle in adequate dosages, it was necessary to use mesalazine as such, in gastroenteroprotected tablets that reproduce the carrier function of salazosulfapyridine. To carry out its local activity, mesalazine must therefore reach directly the intestinal mucosa affected by the pathological process: distal ileus and colon, without being absorbed during transit in the upper GI tract. To achieve this goal it was necessary to resort to particular techniques of protective coating, to allow the drug a free transit through the stomach and small intestine and its release in the distal ileum and colon, where its topical action must be carried out. of the gastroenteric-protective lining is only required when mesalazine is to be taken orally in tablets. For formulations intended for the rectal route (suspension and foam enemas, suppositories, anorectal gel) no protection is required. The formulations of PENTACOL respond rationally to the pharmacological treatment of inflammatory bowel disease, especially according to the location and stage of the morbid phenomenon.
05.2 Pharmacokinetic properties
Orally, PENTACOL gastro-resistant tablets with modified release, with pH dependent release, crosses the upper part of the intestine unscathed and releases the active ingredient in the segments affected by the disease, distal ileus and colon, in which the pH is higher than 6.5. . Rectally PENTACOL is available in five formulations (granules for rectal suspension, rectal foam, rectal gel, rectal suspension, suppositories), formulations that allow the drug to be optimally delivered directly to the mucous membranes of an extended part of the lower intestine, from "anal orifice at the distal portion of the transverse colon. Absorption via the rectum is minimal: after administration of 4 g in aqueous suspension by means of 100 ml enemas, a maximum serum level of 7 mcg / ml was found; no accumulation was found in plasma after repeated daily administrations. L " urinary excretion, mainly in acetylated form, gives dose-dependent values in the order of 10%. The gastro-resistant modified-release tablets, due to their particular coating, disintegrate only in an environment with pH> 6.5 in the ileum and in the colon.The absorption of 5-ASA is modest, with evidence of average plasma levels of 1.3 mcg / ml after administration of 6 tablets. The substance is eliminated in the faeces, while the absorbed portion passes into the urine as N-acetyl - derivative. Acetyl-5-aminosalicylic acid binds to plasma proteins for about 80%, has a half-life of about 6 hours and a renal clearance of 200-300 ml / min.
The formulation in suppositories allows to treat the forms of ulcerative proctitis and colitis located in the last segments of the intestine.
05.3 Preclinical safety data
Acute toxicity
Toxicity for prolonged administration
Subacute toxicity:
Chronic toxicity:
Teratogenesis - Effects on reproduction and fertility - Peri and postnatal toxicity.
No toxic and teratogenic effects were detected even at the maximum doses used.
Mutagenesis - Carcinogenesis.
No mutagenic or carcinogenic effects were detected.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
400 mg modified-release gastro-resistant tablets: microcrystalline cellulose, sodium carboxymethyl starch, maize starch, magnesium stearate, polyvinylpyrrolidone, mannitol, precipitated silica, methacrylic acid copolymers, talc, titanium dioxide, red iron oxide, triethyl citrate.
800 mg modified-release gastro-resistant tablets: microcrystalline cellulose, sodium carboxymethyl starch, maize starch, magnesium stearate, polyvinylpyrrolidone, mannitol, methacrylic acid copolymers, talc, titanium dioxide, red iron oxide, triethyl citrate.
Granules for rectal suspension: microcrystalline cellulose, polyvinylpyrrolidone, dimethicone.
Rectal gel: carboxypolymethylene, triethanolamine, E218 methylhydroxy benzoate, E216 propylhydroxy benzoate, glycerol, purified water.
Rectal foam: polysorbate 20, emulsifying wax, E218 methylhydroxy benzoate, E216 propylhydroxy benzoate, propylene glycol, purified water. Propellants: isobutane, nitrogen.
Rectal suspension: Colloidal silica, Xanthan gum, Sodium carboxymethylcellulose, E218 methylhydroxy benzoate, Sodium metabisulfite, Concentrated phosphoric acid, Purified water.
Suppositories: Solid semisynthetic glycerides.
06.2 Incompatibility
Not known.
06.3 Period of validity
2 years.
06.4 Special precautions for storage
Avoid direct exposure to sunlight and heat sources.
Suppositories and tablets: Store at a temperature not exceeding 30 ° C.
Rectal gel: store at a temperature not exceeding 25 ° C.
06.5 Nature of the immediate packaging and contents of the package
gastro-resistant modified-release tablets
Box of 60 tablets of 400 mg of active ingredient, in PVC / aluminum blister
Box of 30 tablets of 800 mg of active ingredient, in PVC / aluminum blister
Box of 60 tablets of 800 mg of active ingredient, in PVC / aluminum blister
Box of 90 tablets of 800 mg of active ingredient, in PVC / aluminum blister
gel rectal.
Box of 20 tubes of aluminum / epoxy-phenolic resin of 5 g, dosed at 500 mg of mesalazine
Box of 10 tubes of aluminum / epoxy-phenolic resin of 5 g, dosed at 500 mg of mesalazine
granules for rectal suspension.
Box of 20 sachets of 1.5 g granules of active ingredient, with attached soft plastic graduated bottle for the preparation and administration of enemas and 20 disposable rectal cannulas
foam.rectal
2 g rectal foam - 7 single-dose containers under pressure
Box of 7 containers of 130 ml dosed at 2 g of mesalazine, in aluminum / resin and attached rectal cannula
4 g rectal foam - 7 single-dose containers under pressure
Box of 7 containers of 130 ml dosed at 4 g of mesalazine, in aluminum / resin and attached rectal cannula
2g rectal foam - 1 pressurized container of 14g + 7 cannulas
Box of 1 pressurized container of 14 g in aluminum / resin equipped with 7 rectal cannulas, for 14 deliveries (semi-doses) of 1 g of mesalazine
4g rectal foam - 1 pressurized container of 28 g + 7 cannulas
Box of 1 pressurized container of 28 g in aluminum / resin equipped with 7 rectal cannulas, for 14 sprays (semi-doses) of 2 g of mesalazine
Rectal suspension
4g / 100ml Rectal suspension - 7 single-dose containers with cannula
Box of 7 bottles of 100ml, dosed at 4g of mesalazine, in polyethylene with rectal cannula.
Suppositories
Box of 20 suppositories of 500mg in PVC / PE blister, sealed by heat sealing.
06.6 Instructions for use and handling
No particular instructions for disposal.
07.0 MARKETING AUTHORIZATION HOLDER
SOFAR S.p.A. - Via Firenze 40, Trezzano Rosa MI
08.0 MARKETING AUTHORIZATION NUMBER
1.5 g granules for rectal suspension - 20 sachets AIC 026925038
400 mg gastro-resistant modified release tablets - 60 tablets AIC 026925040
800 mg gastro-resistant modified release tablets - 30 tablets AIC 026925166
800 mg gastro-resistant modified release tablets - 60 tablets AIC 026925053
800 mg gastro-resistant modified-release tablets - 90 tablets AIC 026925178
500 mg rectal gel - 20 single-dose 5g tubes AIC 026925065
500 mg rectal gel - 10 single-dose 5g tubes AIC 026925180
2 g rectal foam - 7 single-dose containers under pressure AIC 026925089
4 g rectal foam - 7 single-dose containers under pressure AIC 026925077
2 g rectal foam - 1 pressurized container of 14 g + 7 cannulas AIC 026925127
4 g rectal foam - 1 pressurized container of 28 g + 7 cannulas AIC 026925115
4g / 100ml Rectal suspension - 7 single-dose containers with cannula AIC 026925141
500mg suppositories - 20 suppositories AIC 026925154
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
1.5 g granules for rectal suspension - 20 sachets May 1989 / February 2005
400 mg gastro-resistant modified-release tablets - 60 tablets May 1989 / February 2005
800 mg gastro-resistant modified release tablets - 30 tablets February 2008
800 mg gastro-resistant modified release tablets - 60 tablets December 1998 / February 2005
800 mg gastro-resistant modified-release tablets - 90 tablets February 2008
500 mg rectal gel - 20 single-dose tubes of 5 g December 1998 / February 2005
500 mg rectal gel - 10 single-dose tubes of 5 g October 2008
2 g rectal foam - 7 single-dose containers under pressure December 1998 / February 2005
4 g rectal foam - 7 single-dose containers under pressure December 1998 / February 2005
2 g rectal foam - 1 pressurized container of 14 g + 7 cannulas July 2002 / February 2005
4 g rectal foam - 1 pressurized container of 28 g + 7 cannulas July 2002 / February 2005
4g / 100ml Rectal suspension - 7 single-dose containers with cannula February 2010
500mg suppositories - 20 suppositories February 2010
10.0 DATE OF REVISION OF THE TEXT
June 2015