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Itopride

Obolensky OP
668 Items
2019-09-19
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$32.19
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Clinical Pharmacology

A means of stimulating GI motility. Itopride enhances gastrointestinal propulsion motility due to antagonism against dopamine D2-receptors and dose-dependent inhibition of acetylcholinesterase activity. Itopide activates the release of acetylcholine and inhibits its destruction. Itopod has a specific effect on the upper GI tract, accelerates transit through the stomach and improves its emptying. It also has an antiemetic effect due to interaction with D2-receptors located in the trigger zone. Itopride caused dose-dependent suppression of vomiting caused by apomorphine. Does not affect the serum level of gastrin.

Pharmacokinetics

Quickly and well absorbed in the digestive tract. Relative bioavailability - 60%. Сmax - 0.28 micron / ml, TCmax - 0.5-0.75 h after administration of 50 mg of the drug. With repeated administration of 50–200 mg 3 times a day for 7 days, pharmacokinetics is linear, cumulation is minimal. Communication with proteins - 96% (mainly with albumin; with alpha1-acid glycoprotein - less than 15%). Distributed in the kidneys, small intestine, liver, adrenal glands, stomach. The volume of distribution - 6.1 l / kg. In therapeutic doses, slightly penetrates into the brain and spinal cord, into breast milk. Metabolized in the liver by the action of flavin-dependent monooxygenase. Three metabolites have been identified, only one of them shows insignificant activity (2-3% of itopride activity), which has no pharmacological value. Excreted by the kidneys. T1 / 2 - 6 h, in patients with trimethylaminuria T1 / 2 increases.

Indications

Symptomatic treatment of functional non-ulcer dyspepsia (chronic gastritis), in particular, relief of abdominal distention (flatulence), pain or discomfort in the epigastric region (gastralgia), anorexia, heartburn, nausea, vomiting, feelings of rapid satiation.

Composition

Active ingredient: itopride hydrochloride 50.0 mg.

Itopride is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Itopra Obolensky OP Russia pills
Ittomed PRO.MED.CS Praha a.s Czech pills
Ganaton Maylan EPD GK USA pills

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Itopride

Dosage and Administration

Is ingested 50 mg 3 times / day. The recommended daily intake is 150 mg. This dose may be reduced based on the age of the patient.

Adverse reactions

From the hemopoietic system:leukopenia, thrombocytopenia.

On the part of the endocrine system:increase in prolactin level, gynecomastia.

From the side of the central nervous system: dizziness, headache, tremor.

From the digestive system:diarrhea, constipation, abdominal pain, increased salivation, nausea, jaundice.

Allergic reactions: skin flushing, itching, rash, anaphylaxis.

Hypersensitivity to itopride or any auxiliary component of the drug, gastrointestinal bleeding, mechanical obstruction and perforation of the gastrointestinal tract, children under 16 years of age, pregnancy and lactation (breastfeeding).

Drug interactions

Accelerates absorption of other medicines. The prokinetic effect of the drug does not change under the influence of anti-ulcer agents (cimetidine, ranitidine, teprenone, cetraxate). Cholinergic drugs weaken the effect of the drug.

Pregnancy and Lactation

Contraindicated use during pregnancy and lactation (breastfeeding).

Special instructions

Caution should be taken with itoprid in patients for whom the occurrence of cholinergic adverse reactions (associated with the enhancement of the action of acetylcholine under the influence of itopride) may worsen the course of the underlying disease.

  • Brand name: Itopra
  • Active ingredient: Itopride
  • Dosage form: Pills.
  • Manufacturer: Obolensky OP
  • Country of Origin: Russia

Studies and clinical trials of Itopride (Click to expand)

  1. Chromatographic determination of itopride hydrochloride in the presence of its degradation products
  2. Determination of itopride hydrochloride by high-performance liquid chromatography with Ru(bpy)32+ electrogenerated chemiluminescence detection
  3. PI-4The effects of itopride on plasma gut-regulatory peprides and stress-related hormones levels in healthy humans
  4. PI-74Influence of itopride on in vitro protein binding of digoxin and warfarin
  5. PII-62Evaluation of in vitro inhibitory effect of itopride on cytochrome P450
  6. Quantitation of itopride in human serum by high-performance liquid chromatography with fluorescence detection and its application to a bioequivalence study
  7. Spectrophotometric simultaneous determination of Rabeprazole Sodium and Itopride Hydrochloride in capsule dosage form
  8. Electrogenerated chemiluminescence sensor for itopride with Ru(bpy)32+-doped silica nanoparticles/chitosan composite films modified electrode
  9. Effects of nizatidine and itopride hydrochloride on esophageal motor function
  10. Optimized method for the determination of itopride in human plasma by high-performance liquid chromatography with fluorimetric detection
  11. The effects of itopride on oesophageal motility and lower oesophageal sphincter function in man
  12. A double-blind, randomized, placebo-controlled trial of itopride (100 and 200 mg three times daily) on gastric motor and sensory function in healthy volunteers
  13. Effect of itopride on gastric emptying in longstanding diabetes mellitus
  14. Determination of Pantoprazole, Rabeprazole, Esomeprazole, Domperidone and Itopride in Pharmaceutical Products by Reversed Phase Liquid Chromatography Using Single Mobile Phase
  15. LC–MS Simultaneous Determination of Itopride Hydrochloride and Domperidone in Human Plasma
  16. Stability indicating high performance thin-layer chromatographic method for simultaneous estimation of pantoprazole sodium and itopride hydrochloride in combined dosage form
  17. Tardive dyskinesia associated with long-term administration of escitalopram and itopride in major depressive disorder
  18. Pitfalls in designing trials of functional dyspepsia: the ascent and demise of itopride
  19. Itopride in the Treatment of Functional Dyspepsia in Chinese Patients
  20. Bioavailability and Tolerability of Combination Treatment With Revaprazan 200 mg + Itopride 150 mg: A Randomized Crossover Study in Healthy Male Korean Volunteers
  21. Determination of itopride hydrochloride in human plasma by RP-HPLC with fluorescence detection and its use in bioequivalence study
  22. S1068 Rabeprazole vs. Itopride: A Randomized, Multicenter Trial in Nagoya to Determine Efficacy in Japanese Patients with Functional Dyspepsia
  23. A Multicenter Open-Label Randomized Trial Comparing Rabeprazole Versus Itopride in Japanese Functional Dyspepsia: The NAGOYA Study

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