Zolopent

Zolopent is a means of slowing the activity of the proton pump.

Indications Zolopenta

It is used to treat the following disorders:

• having a moderate or severe form of intensity of reflux esophagitis;
• destruction of H. Pylori microbe in people with peptic ulcers, provoked by the activity of this microbe (in combination with other antibiotics);
• ulcers affecting the gastrointestinal tract;
• gastrinoma and other pathological conditions of a hypersecretory nature.

Release form

The release of the therapeutic agent occurs in tablets with a volume of 40 mg. These tablets are packaged in blisters of 14 or 10 pieces. Inside the pack contains 1 blister pack with 14 tablets or 3 packs with 10 tablets.

Pharmacodynamics

Pantoprazole blocks the processes of secretion inside the stomach. The substance inhibits the activity exhibited by the H ⁺ / K ⁺ -ATPases inside the gastric parietal glandulocytes, resulting in blockage of the final stage of hydrochloric acid evolution. Such influence allows to lower the parameters of basal secretion without binding to the etiology of the irritation.

The medicine has anti-bacterial properties, demonstrated in relation to Helicobacter pylori, and helps other medicines to have anti-Helicobacter influence. The drug effect after taking 1-fold portion develops quickly enough, remaining for the next 24 hours.

Pharmacokinetics

Absorption.

Absorption of pantoprazole occurs at high speed. Values of Cmax within the blood plasma are noted already with a 1-time application of a 20 mg dose. After 2-2.5 hours (on average) after consumption, a serum Cmax value of approximately 1-1.5 μg / ml is recorded. These indicators remain stable after multiple use of drugs.

The therapeutic parameters of the medicament do not change with a 1-time or repeated application. In the dosage range in the range of 10-80 mg, the pharmacokinetic characteristics of pantoprazole inside the plasma are kept linear both when ingested and intravenously.

It is determined that the bioavailability of Zolopent is about 77%. Consumption with food does not affect the level of AUC or serum Cmax, therefore, accordingly, does not affect the bioavailability values. Combined use with food lengthens only the variability of the latent gap.

Distribution processes.

Plasma synthesis of the drug with proteins is approximately 98%. At the same time, the distribution volume index is approximately 0.15 l / kg.

Exchange processes.

The drug is almost completely exposed to hepatic metabolic processes. Metabolism is mostly carried out by demethylation through CYP2C19, and then through the processes of sulfur conjugation. Other metabolic pathways are oxidation involving the element CYP3A4.

Excretion.

The final stage of the half-life is approximately 60 minutes, and the clearance rate is 0.1 l / h / kg. There were cases with a delay in the excretion of the drug. The specific synthesis of pantoprazole with a proton pump of parietal glandulocytes does not allow the half-life to correspond to a longer-lasting drug effect (suppression of acid secretion).

Most of the metabolic products of pantoprazole are excreted in the urine (approximately 80%), and the remainder - with feces. The main metabolic product, both inside the serum and inside the urine, is desmethylpentoprazole, which undergoes conjugation with sulfate.

The half-life of the basic metabolic product (approximately 90 minutes) is only slightly higher than the half-life of pantoprazole.

Dosing and administration

Therapy with reflux esophagitis, which has a severe or moderate degree of intensity, assumes a one-off daily intake of 40 mg of the drug. Sometimes the dosage is allowed to double.

People with ulcerative lesions occurring inside the gastrointestinal tract and a positive response to the test with Helicobacter pylori are required to destroy the bacterium by applying a complex treatment whose schemes depend on the sensitivity of the microbes that are the causative agents of the disease.

Monotherapy for ulcerative lesions in the zone of the gastrointestinal tract involves the use of the 1st tablet with a volume of 40 mg 1-fold per day. The duration of such therapy is determined by the drug requirement.

Take the pill 60 minutes before breakfast, swallowing it whole, without chopping or chewing, squeezed with plain water.

Use Zolopenta during pregnancy

Zolopent is prohibited from use in lactation or pregnancy.

If there is a need for taking a medicine during lactation, you need to give up for this period from breastfeeding.

Contraindications

The main contraindications:

• severe intolerance to the elements of the medication;
• hepatic cirrhosis or hepatitis;
• people with insufficiency of hepatic function in moderate or severe form;
• combination with atazanavir.

Side effects Zolopenta

Reception Zolopent can cause a variety of negative symptoms:

• leukopenia or thrombocytopenia;
• diarrhea, painful sensations affecting the epigastric zone, bloating and constipation;
• vomiting with severe nausea;
• swelling of peripheral nature;
• an increase in the parameters of liver enzymes or triglycerides, and in addition an increase in temperature and tubulointerstitial nephritis;
• anaphylactic manifestations, among which anaphylaxis;
• signs of allergies (rash on the epidermis and itching);
• myalgia libido arthralgia;
• dizziness, headaches, visual disorders.

[1]

Overdose

Signs of intoxication: ataxia, hypoactivity, and also tremor.

If the development of an overdose is suspected, symptomatic procedures must be performed. Dialysis is not necessary.

Interactions with other drugs

Zolopent helps to reduce the extent of absorption of drugs whose bioavailability is determined by indicators of gastric pH (eg, such as ketoconazole).

Metabolism pantoprazole is produced inside the liver, with the participation of the enzyme system of hemoprotein P450. It can not be excluded that the drug will interact with other drugs, whose metabolic processes also occur with the participation of this system.

When performing special tests, no clinically significant interactions with most of these drugs were found (in this list, phenytoin, metoprolol, diclofenac, and in addition carbamazepine with ethyl alcohol and caffeine, as well as naproxen with diazepam and glibenclamide with fenprocumone, theophylline and nifedipine; In addition, piroxicam, warfarin and oral contraception are included).

When using the drug together with antacids, no interaction was observed.

Conducted tests on the effects of combining the drug with certain antibiotics (among those metronidazole with clarithromycin and amoxicillin), did not find clinically significant connections between these drugs.

It was found that the use of 0.3 g of atazanavir / 0.1 g of ritonavir together with omeprazole (a single dose of 40 mg per day) or 0.4 g of atazanavir together with lansoprazole (1-fold use of 60 mg) leads to a significant lowering the level of bioavailability of atazanavir in volunteers. The degree of absorption of atazanavir is determined by pH. Because of this, drugs that slow down the activity of the proton pump, including pantoprazole, are forbidden to combine with atazanavir.

[2]

Storage conditions

Zolopent is required to be kept in a dark place, closed from children's access. Temperature values are a maximum of 25 ° C.

Shelf life

Zolopent can be used within 3 years from the date of manufacture of the medicament.

Application for children

In pediatrics, children under the age of 12 do not take medicine.

Analogues

The analogues of the medication are Controlul, Panocid, Pantasan with Ulsepan, and also Nolpasa, Proxium, Zovanta, Pangastro with Pulcit and Pantokar.

Reviews

Zolopent receives good reviews from people with gastric ulcers - the medicine eliminates the unpleasant symptoms of this disease, such as a burning sensation and a bitter taste in the mouth. The drug is also effective in GERD. In addition, it is noted that it rarely leads to any negative symptoms.