Pantokar

Pantokar is a medicine used for therapy in acid-dependent pathologies. Included in the group of drugs that slow down the activity of the proton pump.

Indications of the pantokar

It is used to eliminate such violations:

• moderate and severe stages of reflux esophagitis;
• destruction of the H. Pylori bacterium in persons with peptic ulcer pathology caused by this bacterium (combined - together with a certain type of antibiotic);
• Peptic ulcer (peptic character) in the gastrointestinal tract;
• gastrinoma and other pathological conditions, against which hypersecretion is observed.

Release form

The release occurs in tablets of enteric type with a volume of 40 mg, 10 units inside the blister cell. In a pack - 3 blisters.

Pharmacodynamics

The component of pantoprazole is the main active medicinal element of Pantokar. It depresses the process of releasing hydrochloric acid. This happens through the implementation of a specific effect on parietal glandulocytes (more specifically, on a proton pump).

Pantoprazole undergoes transformation into an active component inside an acid medium. Inside the gastric parietal glandulocytes, it inhibits the final stage of the formation of hydrochloric acid (H ⁺ / K ⁺ -ATPase), regardless of the origin of the causative agent that stimulates its formation. The degree of inhibition is determined by the size of the dosage. The drug also suppresses stimulated and basal secretion of gastric juice.

Therapy with the use of Pantokar reduces the gastric pH, which is proportional to the increase in secretion of gastrin. The drug has an antibacterial effect against Helicobacter pylori and supports manifestations of anti-Helicobacter pills of other drugs.

Pharmacological action after a single use of the drug begins quickly and lasts for 24 hours. The medicine promotes rapid weakening of pathological symptoms and healing of the intestinal ulcer.

Pharmacokinetics

Absorption.

Pantoprazole undergoes rapid absorption. The peak plasma level is observed already with a single use of drugs in a dosage of 40 mg. 2.5 hours after consumption, on average, there is a peak serum level of about 2-3 μg / ml, and this index remains the same after repeated use. The drug characteristics for single-use and multiple-use tablets remain the same.

At dosages in the range of 10-80 mg, the pharmacokinetic properties of LS inside the plasma are kept linear both in case of ingestion and with iv injection. It was found that the bioavailability of tablets is about 77%.

When combined with food changes in the level of AUC or peak serum values are not observed, so does not change the bioavailability index. In the case of reception, along with food, only the variability of the latent stage increases.

Distribution.

The protein synthesis of pantoprazole within the plasma is approximately 98%. The distribution volume is approximately 0.15 l / kg.

Metabolism.

The active component almost completely passes the process of hepatic metabolism. Its main path is the process of demethylation with the participation of the element CYP2C19. Further, sulfur conjugation is carried out. Another way is the oxidation process with the participation of the CYP3A4 component.

Excretion.

The final half-life is approximately 1 hour, and the clearance rate is 0.1 l / h / kg. There are information on several cases of excretion delay. Due to the specific process of synthesis of pantoprazole with the proton pump located inside the parietal glandulocyte, the half-life does not correlate with the longer duration of the exposure (slowing the release of acid).

Most decay products of the active substance are excreted in the urine (approximately 80%), and the remainder - with feces. The main metabolite both inside the blood serum and inside the urine is a component of dimethylpentoprazole, which has been conjugated with sulfate.

The half-life of dimethylpentoprazole (approximately 1.5 hours) is only slightly longer than the half-life of pantoprazole.

Dosing and administration

The medicine is intended for oral use - the tablet can not be chewed, it is necessary to swallow whole, washing down with water.

To eliminate the intestinal or gastric ulcer, as well as GERD, adults should take 40 mg twice a day.

The course of therapy with gastric peptic ulcer is 0.5-1.5 months; with a similar intestinal ulcer - 0.5-1 month; with GERD - 1-2 months.

When supporting treatment with GERD is required during the first year to use once a day, 40 mg of the drug.

During treatment of exacerbated chronic gastritis of a hyperacid nature or non-ulcerous type of non-ulcer type, 2-3 weeks should be consumed 40-80 mg of medicinal product per day.

In the treatment of gastrinoma, the size of the initial portion of the drug is 3 tablets per day. If necessary, this dose can be increased. In general, dosages are selected for each person individually.

[1]

Use of the pantokar during pregnancy

Lactating and pregnant women Pantokar can be prescribed only in cases where the probability of benefit for a woman is higher than the risk of complications in the fetus / child.

Contraindications

The main contraindications:

• intolerance of pantoprazole or other elements of the drug;
• complex treatment for the purpose of destroying the H. Pylori bacterium in people with moderate or severe kidney failure;
• application in combination with atazanavir,
• children's age is less than 12 years.

Side effects of the pantokar

Use of the drug may lead to the appearance of some side-effects:

• development of leuko- or thrombocytopenia;
• epigastric pain, constipation, diarrhea, or bloating;
• nausea or vomiting;
• dryness of the oral mucosa;
• swelling of peripheral nature;
• an increase in the values of liver enzymes, an increase in temperature, a severe degree of hepatocellular pathology, which subsequently develops into jaundice;
• anaphylactic manifestations, among which anaphylaxis;
• signs of allergy (skin rash and itching);
• myalgia or arthralgia, erythema polyforma, TEN, urticaria, Quincke edema and photosensitivity;
• visual disorders, dizziness or headaches;
• tubulointerstitial nephritis;
• the appearance of hallucinations, a feeling of excitement or disorientation, the development of depression.

Overdose

During intoxication, the patient develops a feeling of weakness or drowsiness, vomiting, dizziness, and diarrhea.

To eliminate the disorders, it is necessary to perform gastric lavage, and also give the patient plenty of fluid and maintain a balance of water and electrolytes in the body.

Interactions with other drugs

The effect of the drug on the degree of absorption of other drugs.

Pantoprazole is able to weaken the degree of absorption of drugs, the level of bioavailability of which is determined by the indicators of gastric pH (this list includes separate antimycotics - drugs itraconazole with ketoconazole, as well as posaconazole or other drugs such as erlotinib).

Drugs used for HIV therapy (such as atazanavir).

The combination of Pantokar with atazanavir and other drugs against HIV, the degree of absorption of which is determined by the level of gastric pH, can cause a significant decrease in their bioavailability, and in addition to influence the severity of their properties. Because of this, it is forbidden to combine these drugs during treatment.

Combination with anticoagulants of indirect influence (such as warfarin with fenprocumone).

Despite the lack of drug interaction with a combination of drugs with warfarin or fenprokumonom during the implementation of clinical tests, in post-marketing studies, the changes in the PSI values were noted. Because of this, those who use drugs from the above category need to monitor the level of PIF / MI from the time of initiation of therapy, after the end of therapy, or with the intermittent use of pantoprazole.

Methotrexate.

There is information about the combined use of methotrexate in large portions (eg, 0.3 g) with Pantokar. In some patients, there was an increase in the value of methotrexate within the blood. People who use methotrexate in large doses (for example, in the treatment of psoriasis or cancer), it is required to temporarily stop using pantoprazole.

[2], [3]

Storage conditions

Pantokar must be kept in a place where moisture does not penetrate. The temperature should not exceed 25 ° C.

[4]

Shelf life

Pantokar can be used for 2 years from the date of manufacture of the drug.