Zirid

Ziride is a drug that stimulates peristalsis.

Indications Zirida

It is used in the treatment of dyspeptic symptoms and gastrointestinal dysfunction: a feeling of fullness in the stomach, flatulence, discomfort or pain in the upper abdomen, as well as heartburn, vomiting and loss of appetite with nausea.

Release form

The release occurs in tablets, in the amount of 10 pieces inside a blister. A separate pack contains 4 or 10 blister packs with tablets.

Pharmacodynamics

Itopride hydrochloride promotes activation of gastrointestinal motility – by antagonizing the effect on dopamine D2 receptors and slowing down acetylcholinesterase. The active component of the drug activates the process of releasing the element acetylcholine and slows down its degradation.

In addition, the drug has antiemetic properties - due to interaction with D2 receptors located inside the chemoreceptor-trigger site. The active component of the drug promotes gastric emptying (achieved due to the specific effect on the upper part of the gastrointestinal tract).

Itopride hydrochloride has no effect on serum gastrin levels.

Pharmacokinetics

The drug is almost completely and rather quickly absorbed in the gastrointestinal tract. The level of relative bioavailability is approximately 60% (due to the effect of the first liver passage - the so-called presystemic metabolism). Food intake does not affect bioavailability indicators. In plasma, peak values of the drug are observed after 30-45 minutes (in the case of taking 50 mg of the drug).

With repeated use of the drug in doses within 50-200 mg (taken three times a day), linearity of the pharmacokinetic properties of the active ingredient with its decay products (during a 7-day course of therapy) was found with minimal accumulation rates of the substance.

Protein synthesis within the blood plasma is about 96%. The process is carried out mainly with the help of albumins. The drug is also synthesized with α-1-acid glycoprotein (less than 15%).

Most of the drug is distributed within various tissues (distribution volume index: 6.1 l/kg), excluding the central nervous system. The substance reaches high values in the small intestine, kidneys, stomach, and adrenal glands with the liver. Only a small part of the drug penetrates the central nervous system. Itopride hydrochloride is also excreted in breast milk.

The drug undergoes intensive hepatic metabolism. Three products of drug breakdown were detected, of which only one has weak activity, which has no medicinal significance (about 2-3% of the medicinal effect of the active substance). The main breakdown product is N-oxide, formed by oxidation of the tertiary category of amino-N-dimethyls.

The drug is metabolized by flavin-containing monooxygenase (FMO). The potency and amount of human FMO isoenzymes may vary due to genetic polymorphism, which may result in the rare autosomal recessive disorder trimethylaminuria. The half-life of the substance may be longer in people with this disorder.

In vivo pharmacokinetic tests using CYP-mediated reactions revealed that the active ingredient of the drug has neither an inducing nor an inhibiting effect on the elements of CYP2C19, nor CYP2E1. In addition, the use of itopride hydrochloride did not affect the content of CYP enzymes and the activity of the element UGT1A1.

Most of the active substance of the drug and its breakdown products are excreted in the urine. When volunteers used the drug in a single standard dose, its excretion (under the form of the active drug substance and N-oxide) was 3.7% and 75.4%, respectively.

The half-life of itopride is about 6 hours.

Dosing and administration

The total daily dose of the medicine is 150 mg (1 tablet three times a day before meals). It is also allowed to reduce this dosage to 0.5 tablets three times a day (taking into account the course of the disease). In general, the tablets should be taken at approximately equal intervals. The medicine is taken without chewing and washed down with water.

The duration of the course is prescribed by the attending physician, taking into account the severity of the disease. However, it cannot last longer than 2 months.

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Use Zirida during pregnancy

There is no data on whether it is safe to take Zirid during pregnancy. Therefore, it is necessary to stop using the drug during this period. Also, before starting to take the drug, it is necessary to make sure that the patient is not pregnant.

There is also no information on the use of drugs during lactation, which is why nursing women are advised to refrain from using the tablets.

Contraindications

Main contraindications:

• intolerance to the active component of the drug, as well as any of its additional elements;
• problems in the gastrointestinal tract – perforation, obstruction or development of bleeding.

Side effects Zirida

Taking the medication may cause some side effects:

• Blood and lymphatic dysfunction: sometimes leukopenia develops. Rarely – neutropenia. Thrombocytopenia may develop;
• immune disorders: anaphylactoid symptoms may occur;
• manifestations from the nervous system: sometimes dizziness appears, and in addition to this, sleep disorders and headaches. Tremor may develop;
• reactions of the gastrointestinal tract: sometimes abdominal pain, constipation, hypersalivation and diarrhea occur. Dryness of the oral mucosa and nausea may develop;
• disorders in the functioning of the hepatobiliary system: jaundice may develop;
• disorders of the urinary system and kidneys: sometimes problems with urination are observed in people with prostate hypertrophy, and the creatinine level with urea nitrogen also increases;
• damage to the subcutaneous layer and skin: occasionally itching, redness and rash appear;
• dysfunction of the musculoskeletal system and connective tissues: sometimes there is pain in the back or sternum;
• problems with the endocrine system: sometimes there is an increase in prolactin levels. The development of galactorrhea or gynecomastia is possible;
• systemic disorders: sometimes there is a feeling of fatigue;
• mental disorders: sometimes a feeling of irritability appears;

Laboratory test results: possible increase in ALT, AST, GGT, bilirubin, and alkaline phosphatase levels.

Overdose

There are currently no reports of cases of poisoning from the drug.

In case of an overdose, it is necessary to carry out standard procedures for such situations - gastric lavage and elimination of symptoms of disorders.

Interactions with other drugs

When the drug was combined with diazepam, nifedipine and wafarin, as well as the substances ticlopidine, nicardipine chloride and diclofenac, no pharmacological interactions occurred.

At the hemoprotein P450 level, interactions should also not be expected because the drug is metabolized by the FMO element.

Itopride has a gastrokinetic effect that can affect the absorption of oral medications taken with Ziride. In this case, it is especially necessary to carefully monitor the indicators of drugs with a narrow spectrum of medicinal action, drugs with a slow process of release of the active component, and drugs whose dosage form has a shell soluble in the stomach.

Anticholinergic agents can reduce the effectiveness of the drug.

The elements ranitidine, cetraxate, as well as cimetidine with teprenone do not affect the prokinetic properties of itopride.

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Storage conditions

No special conditions are required for storing the medicinal product. It must be kept out of the reach of small children.

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Special instructions

Reviews

Zirid has quite good reviews regarding its medicinal effectiveness. Patients note that the medicine works best when they feel heaviness and fullness in the stomach, as well as flatulence. It also quickly eliminates heartburn - after a few days of taking the tablets. Rapid normalization of intestinal peristalsis and return of appetite are also noted.

Shelf life

Ziride can be used for a period of 3 years from the date of manufacture of the medicine.