Proxium powder for solution for injection 40mg 1pc — Made in Spain — Free Delivery

Brand: Laboratorios Normon S.A
Product Code: Proxium
Availability: In Stock

$21.88

Description

Pharmacological properties

Pharmacodynamics. Mechanism of action. Pantoprazole is a substituted benzimidazole that inhibits the secretion of hydrochloric acid in the stomach by specifically blocking the proton pump of parietal cells. pantoprazole is transformed into an active form in an acidic medium in parietal cells, where it inhibits the h + -k + -atphase enzyme, that is, it blocks the final stage of the production of hydrochloric acid in the stomach. inhibition is dose dependent and suppresses both basal and stimulated acid secretion. in most patients, symptoms disappear within 2 weeks. the use of pantoprazole, as in the case of other proton pump inhibitors and h2-receptor inhibitors, reduces acidity in the stomach and thus increases gastrin secretion in proportion to the decrease in acidity. the increase in gastrin secretion is reversible. since pantoprazole binds the enzyme distally to the cellular receptor, it can inhibit the secretion of hydrochloric acid regardless of stimulation by other substances (acetylcholine, histamine, gastrin). the effect when administered orally and intravenously is the same.

When using pantoprazole, the level of fasting gastrin increases. With short-term use of the preparation, the gastrin level in most cases does not exceed the upper limit of the norm. With long-term treatment, gastrin levels double in most cases. Excessive growth, however, occurs only in rare cases. As a consequence, in a small number of cases with long-term treatment, there is a weak or moderate increase in the number of enterochromaffin-like cells (ECL cells) in the stomach (similar to adenomatoid hyperplasia). However, according to the studies carried out to date, the formation of precursor cells of neuroendocrine tumors (atypical hyperplasia) or neuroendocrine tumors of the stomach, which have been identified in animal experiments, have not been observed in humans.

Based on the results of animal studies, it is impossible to exclude the effect of prolonged (more than one year) treatment with pantoprazole on the endocrine parameters of the thyroid gland.

Pharmacokinetics. Pharmacokinetic properties do not change after single or repeated administration. In the dose range of 10–80 mg, the pharmacokinetics of pantoprazole in blood plasma remains linear both when taken orally and when administered intravenously.

Distribution. The binding of pantoprazole to blood plasma proteins is about 98%. The volume of distribution is about 0.15 l / kg.

Metabolism. The substance is metabolized almost exclusively in the liver. The main metabolic pathway is demethylation by CYP 2C19 followed by sulfur conjugation; other metabolic pathways include oxidation by CYP 3A4.

Excretion. The final T½ is about 1 hour and the ground clearance is 0.1 l / h / kg. There are several cases of delayed elimination. Due to the specific binding of pantoprazole to the proton pump of parietal cells, T½ does not correlate with a much longer duration of action (inhibition of acid secretion).

Most of the metabolites of pantoprazole are excreted in the urine (about 80%), the rest in the feces. The main metabolite in both blood plasma and urine is desmethylpantoprazole conjugated with sulfate. T½ of the main metabolite (about 1.5 hours) is slightly higher than that of pantoprazole.

Special patient groups. Slow metabolizers. About 3% of Caucasians have low functional activity of the CYP 2C19 enzyme; they are called slow metabolizers. In such individuals, the metabolism of pantoprazole is probably mainly catalyzed by the CYP 3A4 enzyme. After taking a single dose of 40 mg of pantoprazole, the average AUC was approximately 6 times higher in slow metabolizers than in individuals with a functionally active CYP 2C19 enzyme (fast metabolizers). Cmax in blood plasma increased by about 60%. These results do not affect the dose of pantoprazole.

Impaired renal function. There are no recommendations for dose reduction when prescribing pantoprazole to patients with impaired renal function (including patients on dialysis). As in healthy people, the T1 / 2 of pantoprazole is short. Only very small amounts of pantoprazole are dialyzed. Despite the fact that the main metabolite has a moderately long T1 / 2 (2-3 hours), excretion is still fast, so no cumulation occurs.

Liver dysfunction. Although in patients with liver cirrhosis (classes A and B according to the Child-Pugh classification) T1 / 2 increases to 7-9 hours, and AUC - 5-7 times, Cmax in blood plasma increases only slightly - 1.5 times compared with healthy volunteers.

Elderly patients. A slight increase in AUC and Cmax in elderly volunteers compared to younger volunteers also has no clinical significance.

Children. After a single administration of pantoprazole at a dose of 0.8 or 1.6 mg / kg of body weight to children aged 2–16 years, there was no significant relationship between the clearance of pantoprazole and the age or body weight of the patient. AUC and volume of distribution are comparable to those obtained from studies with adults.

Indications

Stomach and duodenal ulcers, reflux esophagitis, Zollinger-Ellison syndrome and other pathological conditions of hypersecretion.

Application

The preparation is used in adults as directed and under the direct supervision of a physician. IV administration of pantoprazole is recommended only when oral administration is not possible. there is data on the duration of IV treatment up to 7 days. therefore, as soon as oral administration of pantoprazole becomes possible, a transition is made from intravenous proxy administration to oral administration of pantoprazole at a dose of 40 mg.

Recommended doses. Stomach and duodenal ulcers and reflux esophagitis. 1 bottle (40 mg pantoprazole) per day.

Long-term treatment of Zollinger-Ellison syndrome and other pathological conditions of hypersecretion. The recommended daily dose is 80 mg of pantoprazole. If necessary, the dose can be titrated (increased or decreased) depending on the rate of acid secretion in the stomach. Doses exceeding 80 mg / day must be divided into 2 administrations. A temporary increase in the dose of pantoprazole more than 160 mg is possible, but the duration of use should be limited only by the period necessary for adequate control of acid secretion.

If a rapid decrease in acidity is required, an initial dose of 80 mg 2 times is sufficient for most patients to achieve the desired level (10 meq / h) within 1 hour.

General instructions for use. The powder is dissolved in 10 ml of physiological sodium chloride solution, adding it to the bottle. This solution can be administered directly, as well as mixed with 100 ml of physiological sodium chloride solution or 5% glucose solution in plastic or glass bottles.

The preparation must not be prepared or mixed with solvents other than those indicated above.

IV injection should be carried out within 2-15 minutes. The prepared solution can be stored for 12 hours at a temperature of 25 ° C. From a microbiological point of view, the diluted preparation must be used immediately.

The bottle is for single use only. Before use, it is necessary to visually check the vials with the preparation (in particular, for discoloration, the presence of sediment).

The remains of the preparation or the preparation, the physicochemical properties of which have changed (in particular, the color has changed, a precipitate has appeared), must be disposed of in accordance with the requirements of local legislation.

Liver failure. Patients with severely impaired liver function should not exceed a daily dose of 20 mg (½ bottle of Proxium, 40 mg powder).

Renal failure Patients with impaired renal function do not require dose adjustment.

Elderly patients do not require dose adjustment.

Contraindications

Hypersensitivity to the active substance, benzimidazole derivatives and other components of the preparation.

Side effects

The occurrence of adverse reactions can be expected in about 5% of patients. a frequent adverse reaction is thrombophlebitis at the injection site. diarrhea and pain occurred in about 1% of patients.

In terms of frequency of occurrence, side effects are classified into the following categories: very often (≥1 / 10), often (≥1 / 100 and 1/10), infrequently (≥1 / 1000 and 1/100), rarely (≥1 / 10,000 and 1/1000), very rarely (1/10 000), unknown (frequency not determined from available data).

From the side of the blood and lymphatic system: rarely - agranulocytosis; very rarely - leukopenia, thrombocytopenia, pancytopenia.

From the immune system: rarely - hypersensitivity reactions (including anaphylactic reactions, anaphylactic shock).

Metabolism and metabolic disorders: rarely - hyperlipidemia and increased lipid levels (triglycerides, cholesterol), changes in body weight; unknown - hyponatremia, hypomagnesemia (see SPECIAL INSTRUCTIONS), hypocalcemia1, hypokalemia.

Mental disorders: infrequently - sleep disorders; rarely - depression (including exacerbations); very rarely - disorientation (including exacerbations); unknown - hallucination, confusion (especially in patients with a tendency to these disorders, as well as exacerbation of these symptoms if they have a history).

From the nervous system: infrequently - headache, dizziness; rarely - taste disturbances; unknown - paresthesia.

From the side of the organ of vision: rarely - visual impairment / blurred vision.

From the digestive tract: infrequently - diarrhea, nausea, vomiting, bloating, constipation, dry mouth, abdominal pain and discomfort.

On the part of the hepatobiliary system: infrequently - an increase in the level of hepatic enzymes (transaminases, GGT); rarely - an increase in the level of bilirubin; unknown - damage to hepatocytes, jaundice, hepatocellular insufficiency.

On the part of the skin and subcutaneous tissues: infrequently - skin rash, itching; rarely - urticaria, angioedema; very rarely - Stevens-Johnson syndrome, Lyell's syndrome, erythema multiforme, photosensitivity, subacute cutaneous lupus erythematosus (see SPECIAL INSTRUCTIONS).

From the musculoskeletal system and connective tissue: infrequently - fractures of the hip, wrist, spine (see. SPECIAL INSTRUCTIONS); rarely - arthralgia, myalgia; muscle spasm 2.

From the kidneys and urinary system: unknown - interstitial nephritis (with the possible development of renal failure).

From the reproductive system and mammary glands: rarely - gynecomastia.

General disorders: often - thrombophlebitis at the injection site; infrequently - asthenia, fatigue, malaise; rarely - an increase in body temperature, peripheral edema.

1 Hypocalcemia simultaneously with hypomagnesemia.

2 Muscle spasm as a result of electrolyte imbalance.

special instructions

Malignant neoplasms of the stomach. a symptomatic response to pantoprazole may mask the symptoms of gastric malignancies and postpone their diagnosis. in the presence of alarming symptoms (for example, in the case of significant unintentional weight loss, intermittent vomiting, dysphagia, vomiting of blood, anemia, melena), as well as if a stomach ulcer is suspected or present, the presence of a malignant process should be excluded, since pantoprazole treatment can mask symptoms and delay establishing a diagnosis. if symptoms persist with adequate treatment, additional testing is necessary.

Liver dysfunction. In patients with severely impaired liver function, it is necessary to regularly monitor the level of liver enzymes. In case of an increase in the level of liver enzymes, treatment should be discontinued (see APPLICATION).

HIV protease inhibitors. The combined use of pantoprazole with HIV protease inhibitors (such as atazanavir), the absorption of which depends on gastric pH, is not recommended due to a significant decrease in their bioavailability (see INTERACTIONS).

Gastrointestinal infections caused by bacteria. Pantoprazole, like other proton pump inhibitors, can increase the number of bacteria that are commonly found in the upper GI tract. Treatment with the preparation may slightly increase the risk of gastrointestinal infections caused by bacteria such as Salmonella and Campylobacter or C. difficile.

Sodium. The preparation contains 1 mmol of sodium (23 mg) in a vial, that is, in fact, it is a "sodium-free" preparation.

Hypomagnesemia. Cases of severe hypomagnesemia have been reported in patients treated with proton pump inhibitors such as pantoprazole for at least 3 months, and in most cases within a year. The following serious clinical manifestations of hypomagnesemia may occur and initially develop imperceptibly: fatigue, tetany, delirium, convulsions, dizziness, and ventricular arrhythmia. In the case of hypomagnesemia, in most cases, the patient's condition improved after replacement corrective therapy with magnesium preparations and discontinuation of proton pump inhibitors.

Patients who require long-term therapy, or patients taking proton pump inhibitors concurrently with digoxin or preparations that can cause hypomagnesemia (such as diuretics), should have magnesium levels measured before starting proton pump inhibitors and periodically during treatment.

Bone fractures. Long-term treatment (more than 1 year) with high doses of proton pump inhibitors may slightly increase the risk of fractures of the hip, wrist and spine, mainly in the elderly or in the presence of other risk factors. Observational studies indicate that the use of proton pump inhibitors can increase the overall risk of fracture by 10–40%. Some of these may be due to other risk factors. Patients at risk of developing osteoporosis should receive treatment according to current clinical guidelines and consume adequate amounts of vitamin D and calcium.

Subacute cutaneous lupus erythematosus. The use of proton pump inhibitors is associated with very rare cases of subacute cutaneous lupus erythematosus. If a lesion occurs, especially in areas exposed to sunlight, and this is accompanied by arthralgia, the patient should immediately consult a doctor who will consider the need to discontinue Proxium. The occurrence of subacute cutaneous lupus erythematosus in patients during previous therapy with proton pump inhibitors may increase the risk of its development with the use of other proton pump inhibitors.

Use during pregnancy and lactation. Pregnancy. The available data on the use of the preparation Proxium in pregnant women (about 300-1000 reports of pregnancy results) indicate the absence of embryonic or fetal / neonatal toxicity of the preparation. Reproductive toxicity has been observed in animal studies. As a precautionary measure, the use of Proxium in pregnant women should be avoided.

Lactation. Animal studies have shown the excretion of pantoprazole in breast milk. There are insufficient data on the excretion of pantoprazole into breast milk, but such excretion has been reported. Risk to newborns / babies cannot be ruled out. The decision to discontinue breastfeeding or to discontinue treatment with Proxium should be made in light of the benefits of breastfeeding for the baby and the benefits of treatment with Proxium for women.

Fertility Pantoprazole has not impaired fertility in animal studies.

Children. The safety and efficacy of the preparation in children (under the age of 18) have not been established, therefore the preparation is not used in patients of this age group.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Pantoprazole does not affect or has very little effect on the reaction rate when driving or using other mechanisms. It is necessary to take into account the possible development of adverse reactions, such as dizziness and visual disturbances (see SIDE EFFECTS). In such cases, you should not drive vehicles or work with mechanisms.

Interactions

Medicines, the absorption of which depends on the pH. as a result of complete and long-term inhibition of hydrochloric acid secretion, pantoprazole can affect the absorption of preparations for which the pH value of gastric juice is an important factor in their bioavailability (for example, some antifungal preparations such as ketoconazole, itraconazole, posaconazole, or other preparations such as erlotinib).

HIV protease inhibitors. The combined use of pantoprazole with HIV protease inhibitors (such as atazanavir), the absorption of which depends on gastric pH, is not recommended, due to a significant decrease in their bioavailability (see SPECIAL INSTRUCTIONS).

In the case when the combined use of HIV protease inhibitors with proton pump inhibitors cannot be avoided, careful clinical monitoring (for example, viral load) is recommended. Do not exceed the daily dose of pantoprazole 20 mg. It may be necessary to adjust the dose of HIV protease inhibitors.

Indirect anticoagulants (phenprocoumon and warfarin). The combined use of pantoprazole with warfarin or fenprocoumon did not affect the pharmacokinetics of warfarin, fenprocoumon, or MNI. However, an increase in MNI and a prolongation of prothrombin time have been reported in patients who used proton pump inhibitors and warfarin or phenprocoumon in combination. An increase in MNI and a lengthening of prothrombin time can lead to the development of pathological bleeding and even death. In the case of such a combined use, it is necessary to monitor the PIM and prothrombin time.

Methotrexate. The concomitant use of high doses of methotrexate (eg 300 mg) and proton pump inhibitors has been reported to increase blood levels of methotrexate in some patients. Patients taking high doses of methotrexate, such as those with cancer or psoriasis, are advised to temporarily discontinue pantoprazole treatment.

Other interactions. Pantoprazole is largely metabolized in the liver through the cytochrome P450 enzyme system. The main metabolic pathway is demethylation by CYP 2C19 and other metabolic pathways, including oxidation by the CYP 3A4 enzyme. Studies with preparations that are also metabolized by these pathways, such as carbamazepine, diazepam, glibenclamide, nifedipine and oral contraceptives containing levonorgestrel and ethinyl estradiol, have not revealed clinically significant interactions.

Interaction of pantoprazole with other preparations that are metabolized through the same enzyme system cannot be ruled out.

The results of a number of studies of possible interactions indicate that pantoprazole does not affect the metabolism of active substances that are metabolized by CYP 1A2 (eg caffeine, theophylline), CYP 2C9 (eg piroxicam, diclofenac, naproxen), CYP 2D6 (eg metoprolol), CYP 2E1 (e.g. ethanol), does not affect p-glycoprotein, which is associated with digoxin absorption.

There was no interaction with concomitantly prescribed antacids.

Studies have been carried out to study the interaction of pantoprazole with concurrently prescribed certain antibiotics (clarithromycin, metronidazole, amoxicillin). There were no clinically significant interactions between these preparations.

Medicines that inhibit or induce CYP 2C19. Inhibitors of CYP 2C19, such as fluvoxamine, may increase the systemic effects of pantoprazole. The need to reduce the dose of the preparation should be considered for patients receiving long-term therapy with high doses of pantoprazole, and for patients with impaired liver function. Enzyme inducers that affect CYP 2C19 and CYP 3A4, such as rifampicin and St. John's wort (Hypericum perforatum), can reduce plasma concentrations of proton pump inhibitors that are metabolized through these enzyme systems.

Overdose

Overdose symptoms are unknown.

Doses of up to 240 mg, administered IV over 2 minutes, were well tolerated. Because pantoprazole binds extensively to proteins, it is not a preparation that can be easily cleared by dialysis.

In case of an overdose with the appearance of clinical signs of intoxication, symptomatic and supportive therapy is used. There are no specific therapy recommendations.

Storage conditions

In its original packaging at a temperature not exceeding 25 ° C.

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