Panum

Panum is a medicine used to eliminate ulcers or GERD.

[1], [2]

Indications of the panuma

It is used in adults for the treatment of peptic ulcers developing in the gastrointestinal tract, gastrinoma and other pathogens in which gastric secretion increases, and in addition to eliminating the microbe Helicobacter pylori, which occurs against the background of ulcers inside the gastrointestinal tract (in combination with selected antibiotics). Also prescribed for adolescents from 12 years - as a remedy for the elimination of reflux esophagitis.

[3], [4]

Release form

The release occurs in tablets, in an amount of 10 pieces inside the blister plate. In a pack - 1 or 2 blister packs.

Pharmacodynamics

Pantoprazole is a component that replaces benzimidazole, a substance that slows the release of hydrochloric acid by specifically blocking the activity of proton pumps in the area of parietal glandulocytes.

The transformation of pantoprazole into its active form takes place inside an acid medium in the area of parietal glandulocytes, where the H ⁺ -K ⁺ -ATPase enzyme is inhibited (blocking the last stage of production of hydrochloric acid). The degree of deceleration is determined by the size of the dosage and refers to the stimulated, and in addition to the basal secretion of the acid.

Usually, weakening manifestations of the disease is observed after 2 weeks of treatment. The use of pantoprazole, as well as the intake of other drugs that slow down the activity of the proton pump and H2-type conductors, helps to reduce the gastric pH, which leads to an increase in gastrin release (these values are proportional to the decrease in acidity level). The increase in gastrin secretion is reversible.

Because pantoprazole distally synthesizes the enzyme relative to the cell conductor, this substance can slow the release of hydrochloric acid, regardless of the other stimulation (histamine with acetylcholine and gastrin). The degree of exposure to drugs is similar for intravenous administration and oral administration.

The use of pantoprazole leads to an increase in fasting gastrin levels. During short-term admission, they usually remain within the permissible norm, but with prolonged drug therapy, the gastrin content often increases by a factor of 2. But an excessive increase in values is observed only occasionally. Therefore, it is extremely rare with a prolonged medical course to develop a slight or moderate increase in the size of the specific endocrine cells located inside the stomach. But at the same time existing test results show that the formation of cells that are the precursors of neuroendocrine neoplasms (atypical form of hyperplasia) or neuroendocrine gastric neoplasms in humans was not observed.

[5], [6], [7], [8], [9],

Pharmacokinetics

Absorption.

The medicine is quickly absorbed, reaching peak plasma values with a single use of 40 mg of substance. After an average of 2.5 hours after use, serum Cmax is detected, which is approximately 2-3 μg / ml. These values remain stable after multiple use of drugs. The pharmacokinetics of the drug remains unchanged both for single-use and repeated use. Within 10-80 mg of consumed portions, the plasma pharmacokinetics of the drug is maintained linear and after intravenous injection, and after ingestion.

It was revealed that the level of bioavailability of Panuma is about 77%. Admission along with food does not affect the values of AUC or serum Cmax, and therefore does not affect the bioavailability index. Application with food increases only the variability of the latent stage.

Distribution.

Protein synthesis of the substance inside the blood plasma reaches 98%. The distribution volume is approximately 0.15 l / kg.

Metabolic processes.

Almost all pantoprazole undergoes the process of hepatic metabolism. The main way of this process is demethylation with the participation of component CYP2C19, followed by sulfur conjugation. Other routes suggest an oxidation process involving the CYP3A4 substance.

Excretion.

The final half-life is approximately 1 hour, and the clearance level is about 0.1 l / h / kg. There are information on several cases of excretion delay. Due to the specific form of synthesis of the active element with the proton pump of parietal glandulocytes, the half-life does not correlate with a significantly longer period of exposure (slowing down of the acid extraction process).

Most of the products of drug decay are excreted in the urine (approximately 80%), and the remainder is excreted with feces. The main metabolite inside urine and blood serum is desmethylpentoprazole, which has been conjugated with sulfate. The half-life of this element is approximately 1.5 hours, which is not much longer than the half-life of pantoprazole.

[10], [11], [12], [13], [14], [15], [16]

Dosing and administration

Intestinal tablets Panum must be swallowed whole, washed down with water (not crushed or chewed), 1 hour before eating.

Dimensions of dosages during therapy with reflux-esophagitis.

For a day, you need to take 1 tablet with a volume of 40 mg. Sometimes it is possible to increase the dose by half (taking 2 tablets with a volume of 40 mg), especially if there is no positive result after using other medications.

To eliminate the violation, usually 1 month is needed. If the required result after this time is not available, one should expect a cure during the following month.

The sizes of portions for the destruction of Helicobacter pylori (together with 2 antibiotics).

People with peptic ulcer in the gastrointestinal tract, as well as a positive result of the Helicobacter pylori test, are required to eradicate it using complex treatment. In doing so, it is necessary to take into account local information on bacterial resistance, as well as national recommendations for the designation and use of appropriate antibacterial drugs. Taking into account the sensitivity of pathogens, the following medicament combinations can be used to kill the H. Pylori element in an adult:

• taking the 1st pill with 40 mg twice a day in combination with amoxicillin (1 g of the drug twice a day) or clarithromycin (0.5 g of the drug twice a day);
• taking the 1st Panuma tablet (40 mg) 2 times / day together with metronidazole (0.4-0.5 g) or tinidazole (0.5 g) twice a day, or with clarithromycin (0.25-0.5 d) twice a day;
• use the 1st pill of the drug (40 mg) 2 times / day together with amoxicillin (1 g LS) twice a day, either metronidazole (0.4-0.5 g) or tinidazole (0.5 g) twice a day.

During the combined course of treatment aimed at eradicating H. Pylori, the 2nd pill of Panuma should be consumed in the evening, before taking dinner (approximately 60 minutes). The term of therapy lasts 1 week and can be increased for another 7 days if necessary. In general, the duration of treatment can not be more than 14 days.

If necessary, further use of pantoprazole for the healing of ulcerative lesions, it is required to consider the recommended dosage regimens used for the therapy of ulcers in the gastrointestinal tract. If there is no comprehensive treatment in the indications (for example, people with a negative result of Helicobacter pylori test), it is required to use Panuma monotherapy in such doses:

• when treating gastric ulcer - 1 tablet per day. Sometimes the size of the portion can be doubled (up to 2 tablets), especially if the use of other drugs does not work. To eliminate ulcerative pathology in the stomach, usually 1 month is enough. Occasional cure is observed only during the next month;
• when treating an intestinal ulcer - taking the 1st pill for a day. It is also possible to increase the dosage in half - up to 2 tablets. Intestinal ulcers are usually eliminated in 14 days. Occasionally, it may take another 2 weeks.

The sizes of doses at treatment of gastrinoma and other morbid conditions, against which the secretory function of the stomach increases.

With a long treatment course to eliminate gastrinoma and other conditions with increased secretion, you first need to take 80 mg / day (2 tablets). If there is such a need, the portion is allowed to titrate, decreasing or increasing it taking into account the values of gastric pH. Daily dosage, which exceeds 2 tablets (serving 80 mg), is recommended to be divided into 2 separate uses. It may be possible for a while to increase the dose to values exceeding 160 mg, but this course should last only for the period required for adequate control of the pH level.

With the elimination of gastrinoma, the appropriate duration of the therapeutic course is determined by the clinical picture and is assigned individually.

In disorders in the work of the liver.

It is forbidden to use more than 1 tablet with a volume of 20 mg per day (with a mild form of pathology). People with moderate or severe form of the disease are prohibited from using the drug for killing the microbe Helicobacter pylori (complex therapy).

Use of the panuma during pregnancy

There is only limited information about taking Panuma by pregnant women. There is no information about the potential risk of complications in humans. It is forbidden to prescribe medication during this period (except for extreme cases).

There is information that the medicine is excreted with human milk. Decide whether to give up breastfeeding or to cancel the drug by the treating doctor, taking into account the benefits of therapy for the mother and the degree of risk to the infant.

Contraindications

Among the contraindications:

• the presence of intolerance against pantoprazole, benzimidazole derivatives or other elements of the drug;
• it is forbidden to prescribe to children under 12 years of age, because the information on the severity of the exposure and safety of the use of drugs in this group of patients is limited;
• Persons with a disorder of renal activity should not use the medicine to kill Helicobacter pylori (complex therapy), because there is no information about the safety of its reception, and also the effectiveness of the action.

[17], [18], [19], [20],

Side effects of the panuma

The use of drugs can lead to the appearance of certain side-effects:

• violations of the function of systemic blood flow together with lymph: leuko-, thrombocyto- or pancytopenia, as well as agranulocytosis;
• immune disorders: manifestations of hypersensitivity (this includes anaphylaxis and other anaphylactic disorders);
• metabolic disorders: the emergence of hyperlipidemia, and in addition the increase in lipids (cholesterol with triglycerides), weight change, hypokalemia with hyponatremia, as well as kipocalcemia and hypomagnesemia;
• mental disorders: problems with sleep, depression (also at the stage of exacerbation), a sense of disorientation (also in a state of exacerbation), the appearance of hallucinations. There may also be confusion (especially in people with a tendency to develop such disorders, in addition, if there are these signs, their aggravation occurs);
• manifestations in the field of NA: the development of headaches, paresthesias, dizziness, as well as problems with gustatory perception;
• reactions of visual organs: visual fuzziness or frustration;
• abnormalities in the function of the digestive tract: the appearance of nausea, flatulence, diarrhea, vomiting, and at the same time dryness of the oral mucosa, constipation, abdominal discomfort or pain in this area;
• manifestations of the hepatobiliary system: an increase in the values of liver enzymes (GGT with transaminases) and bilirubin values, and in addition the development of liver failure or jaundice and hepatocyte damage;
• lesions affecting the subcutaneous layer and skin surface: itching with rashes, Quinck edema, hives, TEN, Stevens-Johnson syndrome, photosensitivity and erythema polyforma;
• musculature and bone system reactions: the development of myalgia, muscle spasms or arthralgia, and at the same time fractures of the wrists, thighs or spine;
• disturbances of urinary function: tubulointerstitial nephritis (subsequently development of kidney failure is possible);
• disorders in the work of reproductive organs: development of gynecomastia;
• systemic manifestations: a feeling of malaise or fatigue, an increase in temperature, the development of asthenia or peripheral edemas.

[21], [22]

Interactions with other drugs

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

Panum is able to weaken the absorption of drugs whose bioavailability limits are determined by the values of gastric pH (this list includes individual antimycotic substances-among them itraconazole, and in addition ketoconazole with pozaconazole, as well as other agents, eg erlotinib).

Means for the treatment of HIV (such as atazanavir).

With a combination of drugs slowing the activity of the proton pump, with atazanavir and other means for HIV treatment, the level of absorption of which is determined by the indicators of gastric pH, it is possible to significantly reduce the bioavailability of the latter, as well as their effectiveness. In this regard, the combined use of these drugs is prohibited.

Anticoagulants with indirect effects (such as warfarin or fenprokumone).

Although during the clinical trials there was no interaction between Panum and warfarin or fenprocumone taken in combination, during the post-marketing studies there was a single change in the numbers of MSR. Therefore, people who use drugs such as warfarin or fenprokumone for treatment need to constantly monitor the MRI / MI indicators after taking pantoprazole and taking it off, and at the same time if it is not used regularly.

Methotrexate.

There is evidence that the use of methotrexate in large portions (eg 0.3 g) in combination with substances that slow down the activity of the proton pump, raises the value of methotrexate inside the blood in certain groups of patients. People who use methotrexate in high dosages (for example, in the treatment of psoriasis or cancer), it is necessary for a while to refuse admission Panuma.

[23]

Storage conditions

Panum should be kept in a locked place from the access of small children. The temperature should not exceed 30 ° C.

Special instructions

Reviews

Panum is a very effective tool in the treatment of gastritis. Testimonies indicate that to achieve the result, the medicine should be taken only with the appointment of a doctor, an independent reception is strictly prohibited. Of the advantages noted the absence of special contraindications, as well as a low probability of overdose. The disadvantage is a fairly high price for the drug, although its effectiveness justifies this cost.

[24]

Shelf life

Panum can be used for 3 years after the release of the drug.