Pentasa

Pentasa exhibits intense anti-inflammatory activity. The drug does not have a systemic effect, showing its effect inside the inflamed areas of the intestine. With supportive use of the medication, the chance of developing colorectal carcinoma is very low.

In individuals with inflammation affecting the intestine, there is a movement of leukocytes, abnormal production of cytokines, an increase in the production of metabolic elements of arachidonic acid (especially for leukotrienes of type B4) and an increase in free radicals within the inflamed intestinal tissues. [1]

Indications Pentasa

Granules and tablets are used in the treatment of moderate and mild forms of ulcerative colitis (non-specific).

Suppositories are usually prescribed for therapy with ulcerative proctitis .

Release form

The release of the medication is made in tablets - 10 pieces inside the cell plate.

Also, the medicine can be produced in the form of powder granules - inside a paper sachet (1 or 2 g).

It is also sold in the form of rectal suppositories (complete with rubber fingertips), 28 pieces per pack.

Pharmacodynamics

By suppressing leukocyte chemotaxis, the medication prevents the movement of leukocytes inside the focus of inflammation, which makes it possible to reduce infiltration. The binding of inflammatory conductors, including leukotrienes, PG and other metabolic components of arachidonic acid, is also weakened.

Pentasa reduces the volume of LPO components, slowing down their damaging effect on intestinal tissues. [2]

Pharmacokinetics

The drug granules have an ethylcellulose coating. Ingested and dissolved mesalazine is then gradually released from all microgranules, while the tablet passes through the gastrointestinal tract (at any intestinal pH). After 60 minutes from the moment of taking the drug inside, microgranules are determined inside the duodenum (this does not depend on the consumption of food). The average period for the passage of drugs inside the intestines in volunteers is 3-4 hours.

Exchange processes.

Mesalazine is transformed into the element N-acetyl-mesalazine (presystemically within the intestinal mucosa and systemically within the liver). Weak acetylation occurs with the help of colon microbes, resulting in the formation of N-acetyl-5-aminosalicylic acid. It is believed that acetyl-mesalazine has no toxic and therapeutic effects.

Absorption.

Within 30-50% of the drug after oral administration is absorbed inside the small intestine. Already after 15 minutes from the moment of application, mesalazine is registered inside the blood plasma. Plasma Cmax values are observed after 1-4 hours from the moment of drug administration. Further, the plasma level of the substance gradually decreases; after 12 hours, it is no longer detected.

Plasma AUC has a similar pattern, but its values are still higher, and elimination is slower. The metabolic intraplasmic proportions of acetyl-mesalazine and mesalazine are in the range of 3.5-1.3 when administered orally 0.5 g 3 times a day, as well as 2 g 3 times a day. This allows us to conclude that they depend on the intensity of acetylation.

Stable average values of mesalazine inside the blood plasma are equal to 2, 8 and 12 μmol / l when administered per day 1.5, 4, and 6 g, respectively. For acetyl-mesalazine, these indicators, respectively, are equal to 6, 13 and 16 μmol / l.

When administered orally, the movement and release of the drug does not depend on the consumption of food, because the substance has weak systemic absorption.

Distribution processes.

The active element of the drug and its metabolite do not overcome the BBB. The protein synthesis of mesalazine is approximately 50%, and that of acetyl-mesalazine is approximately 80%.

Excretion.

The half-life of mesalazine is approximately 40 minutes, and that of acetyl-mesalazine is approximately 70 minutes. Although mesalazine is always released during movement through the gastrointestinal tract, it is impossible to define a term for its half-life when administered orally. Tests have shown that stable values of mesalazine after oral administration are noted for 5 days.

Both elements of drugs are excreted in feces and urine. At the same time, acetyl-mesalazine is mainly excreted in the urine.

Dosing and administration

Granules or tablets should be taken orally without chewing. To facilitate swallowing, the medicine is washed down with juice or plain water. The serving size is selected by the personally treating doctor.

An adult with a relapse of NUC or Crohn's disease should take 4000 mg of the medication per day. The size of the maintenance dosage in the case of Crohn's disease is 4 g of the drug, and in the case of NUC - 2 g. The daily portion is allowed to be divided into several applications.

Children are prescribed 30 mg / kg of medication; the daily portion should also be consumed over several uses.

Rectal suppositories are inserted inside the anus - 1-2 pieces per day, until the resistance to this procedure from the circular muscle stops. Before performing the introduction, you need to cleanse the intestine with an enema. To ensure the required hygiene during the procedure, you should use the rubber fingertips that come with the medicine. To facilitate the insertion of the candle, it can be moistened with water.

If the suppository spontaneously fell out of the intestine, the procedure must be repeated over the next 10 minutes.

• Application for children

Cannot be administered to persons under 2 years of age.

Use Pentasa during pregnancy

Pentasu is not prescribed for pregnant women. The drug can be used only in the 1st trimester, if there are strict indications. To end the use of the drug should be a month before childbirth (if the course of the pathology allows it).

For the period of treatment, you need to stop breastfeeding.

Contraindications

The main contraindications:

• severe intolerance associated with mesalazine and its metabolic elements (cross-resistance against salicylates is observed);
• use in persons with severe hepatic or secretory dysfunction;
• impaired blood clotting;
• ulcerative pathology.

Side effects Pentasa

Among the side symptoms:

• disorders in the gastrointestinal tract: dyspeptic disorders, abdominalgia, nausea, stool disorders. Sometimes vomiting occurs. Also, with biochemical tests, an increase in the action of liver enzymes may be noted;
• problems with central nervous system function: discoordination, tinnitus, dizziness, depression, tremors and tingling in the extremities;
• violations of secretory activity: hematuria or proteinuria, as well as urinary disorders, which can develop into anuria;
• signs of allergies: epidermal burning or itching, as well as exanthema;
• lesions associated with CVS: pain in the sternum, subjective feeling of cardiac fading, increase or decrease in SBP, bradycardia and dyspnea;
• blood test indications: immunosuppression, suppression of all hematopoietic germs and coagulation disorder;
• others: occasionally alopecia appears or the process of lacrimation decreases.

Overdose

There is only limited information regarding Pentasa poisoning. Symptoms are usually similar to those that appear with salicylate salt intoxication. Along with dehydration, there is hyperventilation of the lungs, a violation of acid-base parameters and hypoglycemia.

Symptomatic actions are carried out, and the victim is hospitalized in a hospital. The medicine has no antidote.

During the first hours after taking the drug inside, gastric lavage is performed. Also, regular monitoring of electrolyte and CBS parameters, as well as renal activity is carried out.

Interactions with other drugs

The introduction of the drug together with methotrexate, mercaptopurine, and azathioprine increases the toxic properties of the latter.

The medicine weakens the effect of warfarin.

Pentasa enhances the hypoglycemic activity of sulfonylurea derivatives.

The carcinogenic effect of GCS is enhanced when combined with the drug.

The drug potentiates the therapeutic effect of anticoagulants.

The drug effect of rifampicin, sulfonamides and thiazide-type diuretics is weakened in the case of a combination with the active element of the drug.

Combination with the drug leads to suppression of the absorption of cyanocobalamin.

The introduction together with uricosuric substances increases their medicinal effect.

Storage conditions

The pentasa must be kept at temperatures not exceeding the 25 ° C mark.

Shelf life

Pentasa can be used within 24 months from the date of manufacture of the therapeutic product.

Analogs

The analogs of the drug are the substances Budenofalk, Tykveol, Medrol and Probifor with Hydrocortisone, St. John's wort with Defenorm, and in addition, Depo-medrol, Atzilakt and Cortef with Solu-medrol, as well as Bifiliz and Cinquefoil rhizome.