Zolopent

Zolopent is a drug that slows down the activity of the proton pump.

Indications Zolopenta

It is used to treat the following disorders:

• having moderate or severe reflux esophagitis;
• destruction of the H.pylori microbe in people with peptic ulcers caused 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 therapeutic agent is released in tablets of 40 mg. These tablets are packaged in blisters of 14 or 10 pieces. Inside the pack there is 1 blister pack with 14 tablets or 3 packs with 10 tablets.

Pharmacodynamics

Pantoprazole blocks secretion processes inside the stomach. The substance suppresses the activity demonstrated by H ⁺ /K ⁺ -ATPase inside the gastric parietal glandulocytes, resulting in the blocking of the final stage of hydrochloric acid secretion. This effect allows to reduce the basal secretion rates without reference to the etiology of the irritation that has arisen.

The medicine has antibacterial properties demonstrated against Helicobacter pylori and helps other medications to have an anti-Helicobacter effect. The medicinal effect after taking a single dose develops quite quickly, lasting for the next 24 hours.

Pharmacokinetics

Absorption.

Pantoprazole is absorbed at a high rate. Cmax values in blood plasma are already noted after a single use of a 20 mg dose. After 2-2.5 hours (on average) after use, the serum Cmax value is recorded, which is approximately 1-1.5 μg/ml. These values remain stable even after repeated use of the drug.

The therapeutic parameters of the drug do not change with single or repeated use. In the dosage range of 10-80 mg, the pharmacokinetic characteristics of pantoprazole in plasma remain linear both when taken orally and when injected intravenously.

The bioavailability of Zolopant has been determined to be approximately 77%. Taking it with food does not affect the AUC or serum Cmax levels, and therefore does not affect the bioavailability values. Combined use with food only prolongs the variability of the latent period.

Distribution processes.

Plasma synthesis of the drug with proteins is approximately 98%. The distribution volume is approximately 0.15 l/kg.

Exchange processes.

The drug is almost completely metabolized by the liver. Metabolism is mostly carried out by demethylation via CYP2C19, and then via sulfur conjugation processes. Other metabolic pathways include oxidation involving the CYP3A4 element.

Excretion.

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

Most of the metabolic products of pantoprazole are excreted in urine (approximately 80%), with the remainder in faeces. The major metabolic product in both serum and urine is desmethylpantoprazole, which undergoes sulfate conjugation.

The half-life of the main metabolic product (approximately 90 minutes) is only slightly longer than that of pantoprazole.

Dosing and administration

Therapy for reflux esophagitis of severe or moderate intensity involves taking 40 mg of the drug once a day. Sometimes the dosage can be doubled.

People with ulcerative lesions that occur inside the gastrointestinal tract and a positive test result for Helicobacter pylori need to destroy the bacteria using complex treatment, the schemes of which depend on the sensitivity of the microbes that cause the disease.

Monotherapy for ulcerative lesions in the gastrointestinal tract involves taking 1 tablet of 40 mg once a day. The duration of such therapy is determined by the medicinal need.

The tablet should be taken 60 minutes before breakfast, swallowing it whole, without crushing or chewing, with plain water.

Use Zolopenta during pregnancy

Zolopant is prohibited for use during lactation or pregnancy.

If there is a need to take the medication during lactation, you should stop breastfeeding for this period.

Contraindications

Main contraindications:

• severe intolerance to the components of the drug;
• liver cirrhosis or hepatitis;
• people with moderate or severe liver dysfunction;
• combination with atazanavir.

Side effects Zolopenta

Taking Zolopant can cause a variety of negative symptoms:

• leukopenia or thrombocytopenia;
• diarrhea, pain affecting the epigastric region, bloating and constipation;
• vomiting with severe nausea;
• edema of a peripheral nature;
• increased liver enzymes or triglycerides, as well as increased temperature and tubulointerstitial nephritis;
• anaphylactic manifestations, including anaphylaxis;
• signs of allergy (rash on the epidermis and itching);
• myalgia or arthralgia;
• dizziness, headaches, visual disturbances.

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Overdose

Signs of intoxication: ataxia, hypoactivity, and tremor.

If overdose is suspected, symptomatic measures should be taken. Dialysis is not necessary.

Interactions with other drugs

Zolopant helps to reduce the degree of absorption of drugs whose bioavailability is determined by gastric pH (for example, ketoconazole).

Pantoprazole is metabolized in the liver, with the participation of the P450 hemoprotein enzyme system. It cannot be ruled out 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 were found with most of these drugs (this list includes phenytoin, metoprolol, diclofenac, as well as carbamazepine with ethyl alcohol and caffeine, as well as naproxen with diazepam and glibenclamide with phenprocoumon, theophylline and nifedipine; in addition, this includes piroxicam, warfarin and oral contraception).

No interactions were observed when the drug was used together with antacids.

Tests conducted on the effects that occur when combining the drug with certain antibiotics (including metronidazole with clarithromycin and amoxicillin) did not reveal any clinically significant connections between these drugs.

It was found that the use of 0.3 g atazanavir/0.1 g ritonavir together with omeprazole (single dose of 40 mg per day) or 0.4 g atazanavir together with lansoprazole (single dose of 60 mg) leads to a significant decrease in the bioavailability of atazanavir in volunteers. The degree of absorption of atazanavir is determined by pH values. Because of this, drugs that inhibit proton pump activity, including pantoprazole, are prohibited from being combined with atazanavir.

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Storage conditions

Zolopant must be kept in a dark place, out of reach of children. Temperature values - maximum 25°C.

Shelf life

Zolopant can be used within 3 years from the date of manufacture of the drug.

Application for children

In pediatrics, the drug is not used for children under 12 years of age.

Analogues

Analogues of the drug are the drugs Controloc, Panocid, Pantasan with Ulsepan, as well as Nolpaza, Proxium, Zovanta, Pangastro with Pulcet and Pantokar.

Reviews

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