Panum

Panum is a medicine used to treat ulcers or GERD.

[ 1 ], [ 2 ]

Indications Panuma

It is used in adults to treat ulcerative pathologies developing in the gastrointestinal tract, gastrinomas and other pathogenic conditions in which gastric secretion increases, and also to destroy the Helicobacter pylori microbe that occurs against the background of ulcers inside the gastrointestinal tract (in combination with selected antibiotics). It is also prescribed to adolescents from 12 years of age - as a means of eliminating reflux esophagitis.

[ 3 ], [ 4 ]

Release form

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

Pharmacodynamics

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

The conversion of pantoprazole into its active form occurs within the acidic environment of the parietal glandulocytes, where the H ⁺ -K ⁺ -ATPase enzyme is inhibited (blocking the final stage of hydrochloric acid production). The degree of inhibition is determined by the dosage and relates to stimulated and also basal acid secretion.

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

Because pantoprazole synthesizes the enzyme distally relative to the cellular conductor, this substance can slow down the secretion of hydrochloric acid regardless of the stimulation carried out by other components (histamine with acetylcholine and gastrin). The degree of action of the drug is similar with intravenous administration and oral administration.

Taking pantoprazole increases fasting gastrin levels. During short-term use, they usually remain within the permissible norm, but with long-term drug therapy, the gastrin level often increases by 2 times. But excessive increases in values are observed only occasionally. Therefore, a mild or moderate increase in the size of specific endocrine cells located inside the stomach can develop extremely rarely during a long course of treatment. However, the current test results show that the formation of cells that are precursors of neuroendocrine neoplasms (atypical form of hyperplasia) or neuroendocrine gastric neoplasms in humans has not been noted.

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

Pharmacokinetics

Absorption.

The drug is rapidly absorbed, reaching peak plasma values after a single dose of 40 mg of the substance. On average, 2.5 hours after use, serum Cmax is observed, which is approximately 2-3 μg/ml. These values remain stable after repeated use of the drug. The pharmacokinetics of the drug remains unchanged with both single and repeated use. Within the range of 10-80 mg of the doses used, the plasma pharmacokinetics of the drug remains linear after both intravenous injection and oral administration.

Panum has been shown to have a bioavailability of approximately 77%. Taking it with food does not affect AUC or serum Cmax, and therefore does not affect bioavailability. Taking it with food only increases the variability of the latent phase.

Distribution.

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

Metabolic processes.

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

Excretion.

The terminal half-life is approximately 1 hour and the clearance rate is approximately 0.1 l/h/kg. Several cases of delayed excretion have been reported. Due to the specific form of synthesis of the active ingredient with the proton pump of the parietal glandulocytes, the half-life does not correlate with a significantly longer period of action (slowing down of the acid secretion processes).

Most of the drug's breakdown products are excreted in the urine (approximately 80%), and the remainder in the feces. The main metabolite in the urine and blood serum is the element desmethylpantoprazole, which has undergone conjugation with sulfate. The half-life of this element is approximately 1.5 hours, which is slightly longer than the half-life of pantoprazole.

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

Dosing and administration

Panum enteric-coated tablets must be swallowed whole with water (not crushed or chewed), 1 hour before meals.

Dosage sizes during therapy for reflux esophagitis.

It is necessary to take 1 tablet of 40 mg per day. Sometimes it is allowed to double the dose (take 2 tablets of 40 mg), especially if there is no positive result after taking other medications.

To eliminate the disorder, 1 month is usually required. If the desired result is not achieved after this time, the cure should be expected during the following month.

Serving sizes for Helicobacter pylori eradication (along with 2 antibiotics).

People with peptic ulcer disease in the gastrointestinal tract, as well as a positive test result for Helicobacter pylori, need to eradicate it using complex treatment. In this case, it is necessary to take into account local information on bacterial resistance, as well as national recommendations for the appointment and use of appropriate antibacterial drugs. Taking into account the sensitivity of pathogenic organisms, the following drug combinations can be used to destroy the H.pylori element in an adult:

• taking 1 tablet of 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 1 tablet of Panum (40 mg) 2 times a day together with metronidazole (0.4-0.5 g) or tinidazole (0.5 g) twice a day, or with clarithromycin (0.25-0.5 g of the drug) twice a day;
• taking 1 tablet of the drug (40 mg) 2 times a day together with amoxicillin (1 g of the drug) twice a day or metronidazole (0.4-0.5 g) or tinidazole (0.5 g) twice a day.

During the combined course of treatment aimed at destroying H.pylori, the 2nd tablet of Panum should be taken in the evening, before dinner (approximately 60 minutes). The therapy lasts 1 week and can be extended for another 7 days if necessary. In general, the duration of treatment cannot exceed 14 days.

If it is necessary to continue using pantoprazole to heal ulcerative lesions, it is necessary to consider the recommended dosage regimens used for the treatment of ulcers in the gastrointestinal tract. In the absence of indications for complex treatment (for example, people with a negative test result for Helicobacter pylori), it is necessary to use monotherapy with Panum in the following doses:

• for the treatment of gastric ulcers - 1 tablet per day. Sometimes the portion size can be doubled (up to 2 tablets), especially if the use of other drugs does not bring results. To eliminate ulcer pathology in the stomach, 1 month is usually enough. Rarely, healing is observed only during the next month;
• when treating intestinal ulcers - take 1 tablet per day. It is also possible to double the dosage - up to 2 tablets. Intestinal ulcers are usually eliminated in 14 days. Rarely, this may require another 2 weeks.

Dose sizes for the treatment of gastrinoma and other painful conditions that increase the secretory function of the stomach.

In long-term treatment for gastrinoma and other conditions with increased secretion, 80 mg/day (2 tablets) should be taken initially. If necessary, the dose may be titrated up or down based on gastric pH values. Daily doses exceeding 2 tablets (80 mg dose) should be divided into 2 separate doses. The dose may be increased temporarily to values exceeding 160 mg, but such a course should only last as long as is required to adequately control the pH level.

When eliminating gastrinoma, the appropriate duration of the therapeutic course is determined by the clinical picture and is prescribed individually.

For liver disorders.

It is prohibited to take more than 1 tablet of 20 mg per day (in case of mild form of pathology). People with moderate or severe form of the disease are prohibited to use the drug to destroy the microbe Helicobacter pylori (complex therapy).

Use Panuma during pregnancy

There is only limited information about Panum use in pregnant women. There is no information about the potential risk of complications in humans. It is prohibited to prescribe the drug during this period (except for extreme cases).

There is information that the drug is excreted in breast milk. The decision to refuse breastfeeding or to cancel the drug should be made by the attending physician, taking into account the benefit of therapy for the mother and the degree of risk to the infant.

Contraindications

Among the contraindications:

• the presence of intolerance to pantoprazole, benzimidazole derivatives or other components of the drug;
• It is prohibited to prescribe to children under 12 years of age, because information about the severity of the effect and safety of the drug in this group of patients is limited;
• People with kidney dysfunction are prohibited from using the drug to destroy Helicobacter pylori (complex therapy), because there is no information about the safety of its use, as well as its effectiveness.

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

Side effects Panuma

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

• dysfunction of the systemic blood flow together with lymph: leukopenia, thrombocytopenia or pancytopenia, as well as agranulocytosis;
• immune disorders: manifestations of hypersensitivity (this includes anaphylaxis and other anaphylactic disorders);
• metabolic disorders: the occurrence of hyperlipidemia, as well as an increase in lipid levels (cholesterol with triglycerides), weight changes, hypokalemia with hyponatremia, as well as hypocalcemia and hypomagnesemia;
• mental disorders: sleep problems, depression (also in the acute stage), feeling of disorientation (also in the acute stage), hallucinations. Confusion may also be observed (especially in people with a tendency to develop such disorders; in addition, in the presence of these symptoms, they worsen);
• manifestations in the nervous system: development of headaches, paresthesia, dizziness, as well as problems with taste perception;
• visual reactions: blurred or impaired vision;
• gastrointestinal dysfunction: the appearance of nausea, flatulence, diarrhea, vomiting, and along with this, dryness of the oral mucosa, constipation, abdominal discomfort or pain in this area;
• manifestations from the hepatobiliary system: an increase in liver enzyme values (GGT with transaminases) and bilirubin values, as well as the development of liver failure or jaundice and damage to hepatocytes;
• lesions affecting the subcutaneous layer and the surface of the skin: itching with rashes, Quincke's edema, urticaria, TEN, Stevens-Johnson syndrome, photosensitivity and erythema multiforme;
• reactions of the musculature and skeletal system: development of myalgia, muscle spasms or arthralgia, and along with this, fractures of the wrists, hips or spine;
• urinary dysfunction: tubulointerstitial nephritis (which may subsequently lead to kidney failure);
• disorders in the functioning of the reproductive organs: development of gynecomastia;
• systemic manifestations: feeling of malaise or fatigue, increased temperature, development of asthenia or peripheral edema.

[ 21 ], [ 22 ]

Interactions with other drugs

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

Panum is capable of weakening the absorption of drugs whose bioavailability limits are determined by gastric pH values (this list includes certain antifungal substances – among them itraconazole, and also ketoconazole with posaconazole; as well as other drugs, for example, erlotinib).

HIV treatments (such as atazanavir).

When combining proton pump inhibitors with atazanavir and other HIV medications whose absorption is determined by gastric pH, there may be a significant decrease in the bioavailability of the latter, as well as their effectiveness. Therefore, the combined use of these medications is prohibited.

Indirect acting anticoagulants (such as warfarin or phenprocoumon).

Although no interactions between Panum and warfarin or phenprocoumon taken in combination were observed during clinical trials, changes in INR values have been observed in post-marketing studies. Therefore, people taking drugs such as warfarin or phenprocoumon for treatment should regularly monitor their INR/PT values after starting and stopping pantoprazole, and also in case of irregular use.

Methotrexate.

There is evidence that the use of methotrexate in large doses (for example, 0.3 g) in combination with substances that slow down the activity of the proton pump increases the values of methotrexate in the blood in certain groups of patients. People taking methotrexate in high doses (for example, when treating psoriasis or cancer) should temporarily stop taking Panum.

[ 23 ]

Storage conditions

Panum should be stored in a place out of reach of small children. Temperature marks should not exceed 30°C.

Special instructions

Reviews

Panum is quite an effective remedy for treating gastritis. Reviews indicate that in order to achieve results, the drug should be taken only with a doctor's prescription; self-administration is strictly prohibited. Among the advantages, there are no special contraindications, as well as a low probability of overdose. The disadvantage is considered to be a fairly high price for the drug, although its effectiveness justifies this cost.

[ 24 ]

Shelf life

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