Pentasa - description of the drug, instructions for use, reviews

Write a review

Reviews: 0

Manufacturers: Ferring Arzneimittel Ges.mbH

Active ingredients

• Mesalazine

Disease class

• Crohn's disease [regional enteritis]
• Ulcerative colitis
• Proctitis

Clinical and pharmacological group

• Not indicated. See instructions

Pharmacological action

• Anti-inflammatory

Pharmacological group

• NSAIDs - Salicylic acid derivatives

special instructions

If acute signs of intolerance to Pentasa appear (such as muscle cramps, abdominal pain, fever, severe headache, skin rashes) or symptoms of renal and/or liver dysfunction, therapy should be interrupted.
It is necessary to regularly monitor the creatinine level in the blood throughout the entire period of use of any form of release of the drug Pentasa.

Soft contact lenses, tear fluid and urine may turn yellow-orange.

Impact on the ability to drive vehicles and complex mechanisms

Patients are advised to exercise caution when taking tablets, granules and rectal suspension, driving vehicles and engaging in other potentially hazardous activities that require psychomotor speed and increased concentration, as they may be affected by Pentasa side effects such as nausea, weakness, dizziness, etc.

Composition, forms of medication

There are several forms of release of the drug in question. Let's introduce them right now.

The drug "Pentasa" - tablets (500 mg, 100 mg) of prolonged action. They are white with a grayish tint, as well as with numerous light brown inclusions, regular round in shape, with a notch, chamfer and inscriptions on both sides.

The active element of this medicine is mesalazine. The product also contains inactive ingredients in the form of povidone, ethylcellulose, magnesium stearate, talc and microcrystalline cellulose.

The drug “Pentasa” (tablets), a photo of which is presented in the article, is sold in blisters, which are in cardboard packs.

It should also be noted that the medication in question can be purchased in the form of suppositories, long-acting granules and rectal suspension.

Features of application

Instructions for use mesacol
Granules are prescribed to adults and children over two years of age. It is advisable to take the drug in this form entirely without chewing. If the patient has difficulty swallowing the granules this way, they can be dissolved in boiled water or fruit juice. The resulting product must be drunk immediately after preparation. The dosage will be determined by the doctor individually. It should be borne in mind that, as a rule, treatment of ulcerative colitis and Crohn's disease is a long process, often lifelong.

Pentas suppositories are prescribed only to adult patients. Disposable finger pads are included for hygienic use. It must be taken into account that the residence time of the medicine in the rectum should be at least ten minutes. If necessary, a new candle should be introduced to replace the one removed prematurely. The drug does not cause drowsiness. In addition, the medicine is successfully used for diabetes. Pentasa has the ability to interact with certain medications:

• antitumor drugs Azathioprine and Mercaptopurine;
• blood thinner Warfarin.

In these cases, dose adjustment may be required.

Instructions for a special category of citizens

In this section you can find the information you need to receive safely

Driving or alcohol

During treatment you should stop drinking alcohol.

Pregnancy

Pregnancy is an important and most difficult period of time in the life of any girl. The fact is that at this time a serious load is placed on the girl’s body, including the kidneys. That is why taking medications at this time is extremely undesirable. Pentasa is also no exception.

Reception by children

No information provided.

Kidney dysfunction

The medicine is used to treat kidney diseases.

Liver disorders

Correction may be required.

Dispensing from pharmacies

No recipe needed.

Side effects

Buscopan tablets - instructions for use

The most common symptoms observed with Pentasa are diarrhea (3%), nausea (3%), abdominal pain (3%), headache (3%), vomiting (1%) and skin rash (1%).

(*) The mechanism of development of adverse reactions is presumably allergic in nature.

If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Similar drugs:

• Dexamethasone Solution for intravenous and intramuscular administration
• ARTRADOL (Artradol) Lyophilisate for the preparation of solution for injection
• Dicloberl N 75 (Dicloberl N 75) Solution for injection
• Calcium gluconate Chewable tablets
• Nimesil Granules for the preparation of suspension for oral administration
• Next Oral tablets
• Dimexid Solution for local and external use
• Pulmicort Suspension for inhalation
• Ibufen Oral suspension
• Panoxen Oral tablets

** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before you start using Pentasa, you should consult your doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

Are you interested in Pentasa? Do you want to know more detailed information or do you need a doctor's examination? Or do you need an inspection? You can make an appointment with a doctor - the Euro lab is always at your service! The best doctors will examine you, advise you, provide the necessary assistance and make a diagnosis. You can also call a doctor at home . Euro lab clinic is open for you around the clock.

** Attention! The information presented in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of the drug Pentasa is provided for informational purposes only and is not intended for prescribing treatment without the participation of a doctor. Patients need to consult a specialist!

If you are interested in any other drugs and medications, their descriptions and instructions for use, information about the composition and form of release, indications for use and side effects, methods of use, prices and reviews of drugs, or you have any other questions and suggestions - write to us, we will definitely try to help you.

Side actions

Kvamatel tablets - instructions for use

In some cases, the medication in question causes the following side effects:

• stomatitis, tremors of extremities, dry mouth, dizziness, nausea, depressive mood;
• loss of appetite, feeling of rapid heartbeat, heartburn, shortness of breath during physical activity, vomiting;
• hematuria, diarrhea syndrome, tachycardia, hepatitis, chest pain;
• increased liver enzymes, fluctuations in blood pressure, pancreatitis, polyneuropathy;
• crystalluria, tinnitus, proteinuria (protein secretion), migraine headaches;
• oliguria, leukopenia, anuria (lack of urination), thrombocytopenia, the formation of nephrotic syndrome;
• hypoprothrombinemia, agranulocytosis, eosinophilia, anemia.

It should also be noted that while taking this drug, the patient may experience: oligospermia, alopecia, photosensitivity, weakness in the limbs, lupus-like syndrome, decreased production of tear fluid, mumps.

Pharmacology of a medicinal product

What is the medicine "Pentasa"? The instructions for use state that this is a drug that has an anti-inflammatory effect and is used to treat UC and Crohn's disease.

The anti-inflammatory properties of this drug appear only when used topically. This effect is due to the synthesis of leukotrienes and prostaglandins, as well as inhibition of lipoxygenase (neutrophil) activity. In addition, this drug can slow down the secretion of immunoglobulins by lymphocytes and inhibit degranulation, migration and phagocytosis of neutrophils.

Drugs with similar effects

Pentasa is a prescription drug. The price of the drug depends on the form of release. 50 bags of granules cost from 5763 to 6566 rubles. The price for a package of suppositories (28 pieces) ranges from 2741 to 2865 rubles. There are medications with similar active ingredients from different price categories.

Medicines containing mesalazine - table

Analogs

Among the presented analogues, we can highlight such drugs as: Tidokol, 5-ASA, Mezakol, Samezil, Kansalazine, Mesacol, Mesalazine, Asacol, Salofalk, Salozinal, Mezavant, Sulfasalazine.

• If you have any symptoms of the disease, you should immediately consult a doctor. You can view a list of gastroenterology clinics on our website
• You will be interested! The article describes symptoms that make it possible to suspect the presence of liver disease in the early stages
• You will also be interested in learning more about the treatment of various diseases of the gastrointestinal tract

Pharmacodynamics and pharmacokinetics

The anti-inflammatory drug exhibits an immunosuppressive effect. In the body, it breaks down due to intestinal flora to sulfapyridine, which suppresses the transformation of lymphocytes. The second metabolite is 5-aminosalicylic acid, which successfully copes with inflammatory processes in the colon.

The mechanism of action of the drug is based on the binding of oxygen free radicals, local suppression of cyclooxygenase and lipoxygenase, which are mediators of inflammation and precursors of prostaglandin, within the intestinal wall. Up to a third of the dose of tablets or powder is absorbed by the walls of the large intestine, the rest disintegrates.

The active substance enters the intestines with bile and is slightly excreted in the urine. The half-life is 5-10 hours. Released sulfapyridine undergoes hepatic metabolism (through acetylation, conjugation with glucuronic acid, hydroxylation) and is excreted by the kidneys. A third of mesalazine (metabolite) is acetylated by the liver and excreted in urine or feces unchanged.

Pharmacokinetics of the drug

How is the drug Pentasa absorbed? The instructions for use indicate that microgranules of disintegrated tablets reach the duodenum within the first 60 minutes.

Approximately 30-50% of the dose taken is absorbed in the small intestine. The binding of mesalazine to plasma proteins is 43%, and N-acetyl-penta-aminosalicylic acid is 73-85%.

Mesalazine, as well as its derivatives, do not penetrate the BBB. The cumulative properties of the drug appear only when high dosages are used (about 1500 mg per day).

Mesalazine undergoes acetylation in the intestinal mucosa and liver. This substance is excreted in urine, breast milk and feces.

Pharmacological properties

Pharmacodynamics

Mesalazine, 5-aminosalicylic acid, is the active component of sulfasalazine. The therapeutic effect of mesalazine after oral or rectal administration is largely due to local effects on inflamed intestinal tissue rather than systemic effects.

The therapeutic effect of mesalazine occurs upon local contact with the affected intestinal mucosa.

Mesalazine inhibits leukocyte chemotaxis, reduces the production of cytokines and leukotriene, and reduces the formation of free radicals in inflamed intestinal tissue. But the exact mechanism of action of mesalazine is not fully understood.

Pharmacokinetics

Absorption: after administration, the Pentasa tablet disintegrates into microgranules, which act as independent forms of the drug with a slow release. This ensures the therapeutic effect of Pentasa throughout the entire length from the duodenum to the rectum at any pH value. The microgranules reach the duodenum within an hour after taking the tablet. The average passage time for the drug through the small intestine is 3–4 hours.

Distribution: About 30-50% of the dose taken is absorbed, mainly in the small intestine. The maximum concentration of mesalazine in plasma is reached 1 hour after administration and lasts up to 4 hours, gradually decreasing.

Metabolism: mesalazine undergoes acetylation in the intestinal mucosa and liver, and also, to a small extent, by enterobacteria, forming the main metabolite N-acetyl-5-aminosalicylic acid. 43% of mesalazine and 73-83% of the metabolite are bound to plasma proteins. Mesalazine and its metabolite do not cross the blood-brain barrier but pass into breast milk. The clearance of mesalazine is 18 l/hour. When taking high doses (up to 1500 mg/day), a cumulative effect may be observed.

Elimination: The half-life of mesalazine from plasma is approximately 40 minutes, the metabolite is about 70 minutes. Mesalazine and its metabolites are excreted from the body in urine and feces.

The principle of action of the medical product

How does the medicine "Pentasa" work? The instructions for use state that the therapeutic effect of this drug appears immediately after local contact of mesalazine with the intestinal mucosa.

After taking the oral medication, the tablet immediately disintegrates into microgranules, which act as independent forms and slowly release the active substance - mesalazine. This ensures the effectiveness of the medication from the duodenum to the rectum at any pH level.

pharmachologic effect

Pentasa has a pronounced anti-inflammatory effect. The drug does not have a systemic effect; it exhibits its activity in inflamed areas of the intestine.

By inhibiting the chemotaxis of leukocytes, the drug prevents their migration into the pathological focus, thereby reducing infiltration. The synthesis of inflammatory mediators, for example, prostaglandins, leukotrienes and other metabolites of arachidonic acid, is reduced. Pentasa reduces the amount of lipid peroxidation products, inhibiting their damaging effects on intestinal tissue.

Clinically, maintenance use of Pentasa is associated with a low risk of colorectal cancer.

Composition and release form

The drug Pentasa (Latin name Pentasa) can be found in pharmacies in two dosage forms: granules for oral administration and rectal suppositories. In both cases, the active component is the substance mesalazine. It affects the body's immune response and the course of inflammatory reactions. To prepare candles and granules, the manufacturer uses several additional components.

Pentasa is available in the form of granules for oral administration.

Composition of granules and suppositories - table

Pentasa drug overdose, symptoms and treatment

Tablets and granules . Considering the unique dosage form in the form of long-acting granules and the specific pharmacokinetic properties of mesalazine, only a small part of the active substance has a systemic effect, so one should not expect the development of overdose symptoms even when using the drug in high doses. Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness. Treatment is symptomatic: gastric lavage, use of laxatives; restoration of COR depending on the clinical situation and replacement of electrolyte loss in mixed alkalosis/acidosis; replenishment of fluid volume during hyperhidrosis, vomiting; for hypoglycemia - administration of glucose. Monitoring kidney function. Suppositories . There is no experience studying overdose.

special instructions

Treatment of patients with impaired liver or kidney function is possible only after assessing the degree of their severity.

During the entire course of treatment and especially at the beginning, renal function (creatinine level in the blood) should be regularly monitored.

If you suspect the development of pericarditis, myocarditis and changes in the blood count, treatment should be interrupted. Manifestations of the above adverse reactions can occur with pronounced pathological changes in blood composition - increased bleeding, subcutaneous hemorrhages, sore throat and fever; with pericarditis and/or myocarditis - fever and chest pain combined with shortness of breath.

In some cases of an allergic reaction to sulfasalazine, it is possible to develop intolerance to Pentasa (risk of allergy to salicylates).

Patients who are “slow acetylators” are at increased risk of developing side effects.

Possible staining of urine and tear fluid in a yellow-orange color, staining of soft contact lenses.

Impact on the ability to drive vehicles and operate machinery

The drug does not affect the ability to drive vehicles or operate machinery.

Special information

If you miss one dose of mesalazine, it is recommended to take it along with the next one or as soon as possible. If several doses have been missed, you should immediately consult a doctor. In this case, it is forbidden to stop treatment on your own.

Sometimes, while using the drug in question, patients experience a yellowish-orange coloration of their urine and contact lenses.

During treatment with mesalazine, constant medical monitoring of the patient’s renal system is necessary. You should also regularly test the patient's urine and blood (during the entire course of therapy, as well as after its completion).

The likelihood of adverse reactions occurring while taking this medication increases in those who are “slow acetylators.”

If acute intolerance syndrome to the active ingredient develops, Pentasa should be immediately discontinued.

Interaction with other drugs

Concomitant use of Pentasa with azathioprine, mercaptopurine and methotrexate will increase the toxicity of the latter.

Pentasa reduces the effectiveness of warfarin when used in parallel.

The drug potentiates the hypoglycemic effect of sulfonylurea derivatives.

The carcinogenicity of glucocorticoids increases when taken together with Pentasa.

Pentasa enhances the effect of anticoagulants.

The clinical effectiveness of sulfonamide, rifampicin and thiazide diuretics is reduced by the influence of the active substance Pentasa.

The drug inhibits the absorption of cyanocobalamin.

Simultaneous use of Pentasa with uricosuric drugs will increase their effectiveness.

Directions for use and dosage

Instructions for using Sulfasalazine are practically no different from using the tablet or powder form of the drug. Both types of medicine are taken orally, the dosage is prescribed by the doctor, as is the duration of the course of treatment. The amount of medication taken depends on the type of disease, severity, and patient tolerance.

Sulfasalazine tablets

According to the instructions, the tablets are taken orally after meals, washed down with water. For ulcerative colitis and Crohn's disease (granulomatous enteritis), patients over 16 years of age are prescribed 2 g in 4 divided doses on the first day, 4 g in 4 divided doses on the second day, 6-8 g in 4 divided doses on the third and subsequent days. After stopping the exacerbation, the maintenance daily dose is 1.5-2 g in 3-4 doses.

Maintenance treatment lasts several months, but it is not prescribed to patients under 16 years of age with a body weight of less than 65 kg. Children are prescribed no more than 2 g of the drug per day, adults - 8 g. For ankylosing spondylitis, treatment of which with hormones and non-steroidal anti-inflammatory drugs is ineffective, Sulfasalazine is prescribed as a basic drug to inhibit inflammation in the joints.

The course lasts 3-6 months until the desired effect occurs and the patient experiences relief. The drug should be used in the maximum dosage without taking other medications. After relief occurs, the dosage is reduced. Sulfasalazine does not stop the pathological process itself, but the effect of its treatment lasts for a couple of months. Then you can repeat the course.

The drug in powder form is taken orally after meals with water or milk. With a left-sided distal location of the colitis focus, microenemas and suppositories can be made on its basis - 1 g of the product mixed with 1.6 g of cocoa butter is injected into the rectum twice a day. For juvenile and other types of rheumatoid arthritis, in the first week of treatment, patients over 16 years of age are prescribed 500 mg of Sulfasalazine, in the second - 100 mg, divided into two doses, in the third - 1500 mg, divided into three doses.

The daily therapeutic dose is 1.5-3 g, treatment lasts at least 6-10 weeks, but can last up to six months. When used in pediatrics, dosages change: children 6-8 years old with a body weight of 20-29 kg - 500 mg twice a day, 8-12 years old with a body weight of 30-39 kg - 500 mg three times a day, 12-16 years old with a body weight 40-45 kg – 500 mg three times a day or 1000 mg twice a day. After 16 years and reaching a weight of 50 kg, you can take 1000 mg twice a day. The course of treatment lasts 2 months. During a colitis crisis, take 500 g 4 times a day. Do not exceed the children's norm of 30-40 mg per kg of weight.

The mechanism of the anti-inflammatory action of Pentasa

It is thanks to the immune system that man has managed to successfully exist on a planet inhabited by bacteria and viruses. Immunity is omnipresent. Its fighters supervise all cells and tissues. Their main task is to identify and destroy alien objects in a timely manner. To protect the body from viruses, bacteria and its own altered structures, there are white blood cells called leukocytes. They either directly destroy pathogens or produce special antibody proteins.

Leukocytes are the main fighters of the immune system

A unique protective mechanism is the inflammatory response. Its task is to prevent hostile agents from breaking deep inside the body. Not only leukocytes play a role here, but also special chemicals. Most are relatives of arachidonic acid. The drug Pentasa affects all aspects of immune and inflammatory reactions. It causes white blood cells to less actively search for their opponents and produce antibodies. In addition, under the influence of this drug, less arachidonic acid and other participants in inflammation are formed.

Pentasa has an anti-inflammatory effect

Pentasa, instructions for use: method and dosage

Long-acting tablets

Pentas tablets are taken orally after meals, without chewing. If the patient cannot swallow the tablet whole, it is allowed to divide it into several parts, or dissolve it in juice or water immediately before taking it.

Recommended dosage regimen for adults:

• Ulcerative colitis: during exacerbation – 2 pcs. 2-4 times a day; maintenance treatment – ​​1 pc. 2-3 times a day;
• Crohn's disease: during exacerbation - 2-4 pcs. 4 times a day; maintenance treatment – ​​2-4 pcs. 2 times a day or 2-3 pcs. 3 times a day.

An individual dose of mesalazine is selected for children, usually at the rate of 0.02-0.03 g/kg body weight per day in several doses.

Long-acting granules

Pentas granules are taken orally after meals without chewing. The contents of one sachet should be poured onto the tongue, then washed down with juice or water.

Daily dose of mesalazine (selected individually, it should be divided into several doses):

• Adults: during exacerbation - up to 4 g; maintenance treatment – ​​2-4 g;
• Children from 6 years of age and adolescents: during exacerbation - 0.02-0.03 g/kg body weight, but not more than 4 g (the maximum single dose should not exceed 0.075 g/kg); maintenance treatment – ​​0.02-0.03 g/kg, maximum – no more than 2 g.

Children weighing 40 kg or more are recommended to take adult doses of Pentasa.

The duration of the course of therapy is determined by the attending physician.

Rectal suppositories

Pentas rectal suppositories are intended for insertion into the rectum.

The manipulation is carried out after bowel movement. It is necessary to use a rubber fingertip to ensure hygiene of the procedure. To facilitate administration, the suppository can be moistened with water and then inserted into the anus until the resistance of the muscle sphincter stops. If the suppository comes out within 10 minutes after administration, you need to repeat the procedure using another suppository.

Recommended dosage of Pentasa: 1 pc. 1-2 times a day; the maximum permissible daily dose is 6-8 pcs.

Rectal suspension

The drug is used once a day before bedtime as an enema. It is advisable to empty your bowels before the procedure.

The recommended daily dose of Pentasa is 1 g (1 bottle of 100 ml).

Immediately before use, open the package and shake the contents of the bottle. Tighten the tip with the valve until it stops, ensuring that the suspension flows out in one direction. Lie on your side to perform the procedure and carefully insert the tip as deep as possible into the rectum.

The average duration of therapy with rectal forms of Pentasa (suspension, suppositories) is 8-12 weeks, an indicator of its effectiveness is the achievement of clinical and endoscopic remission. The maximum duration of the course, including maintenance and anti-relapse therapy, is not limited.

Prohibitions on the use of the drug

Under what conditions should a remedy such as Pentasa not be used? The instructions (tablets and other forms of the drug have the same contraindications) speak of the following prohibitions:

• hemorrhagic diathesis;
• blood diseases;
• lactation period;
• gastrointestinal ulcer;
• last 2-5 weeks of pregnancy;
• lack of glucose-6-phosphate dehydrogenase;
• age up to two years;
• renal failure is severe;
• hypersensitivity to the substances of the drug;
• liver failure is severe.

The medicine in question should be used with extreme caution in the first trimester of pregnancy, as well as in case of liver and kidney failure.

Side effect

The most common symptoms observed with Pentasa are diarrhea (3%), nausea (3%), abdominal pain (3%), headache (3%), vomiting (1%) and skin rash (1%).

(*) The mechanism of development of adverse reactions is presumably allergic in nature.

Local reactions may also be observed, such as itching, discomfort, and the urge to defecate.

If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Terms of sale and storage

Sulfasalazine is a prescription drug that should be stored away from children at temperatures below 25 degrees for no longer than five years.

To replace the drug, you can allocate funds with the same or a different active ingredient, but with a similar effect. Analogs of Sulfasalazine are:

• Asacol - anti-inflammatory suppositories containing mesalazine;
• Mesacol - antimicrobial tablets based on mesalazine;
• Pentasa - granules, suspension, tablets and suppositories based on mesalazine;
• Samezil - tablets, rectal suppositories and suspension based on mesalazine;
• Salazopyrine En is an antimicrobial tablet containing sulfasalazine.

Sulfasalazine En - difference from Sulfasalazine

The most famous analogue of Sulfasalazine is Sulfasalazine En. The drugs have the same active ingredient, but differ in the structure of the film shell. The drug with the prefix En has an enteric film coating, which improves its bioavailability and absorption rates to 90% compared to 70% of the analogue. Another difference between the products is the cost - Sulfasalazine En is a third more expensive.

Similar medications and consumer reviews

Do you know what can replace the medication in question? Your doctor should inform you about this. As a rule, the following drugs are considered analogues of this drug: “Mesakol”, “Salozinal”, “Salofalk”, “Mezavant”, “Mesalazine”, “Asacol”.

What do consumers say about this product? According to their reviews, the mentioned medication is a highly effective medicine that can be purchased at any pharmacy. Patients claim that mesalazine works very well not only in therapy, but also in the prevention of Crohn's disease, as well as nonspecific ulcerative colitis.