ITOPRIDE OF HYDROCHLORIDE:
Chemically speaking, itopride HCL is known as N-[4-[2-(Dimethyl-amino) ethoxy]benzyl]-3,4-dimethoxybenzamide hydrochloride. As a substituted benzamide, itopride hydrochloride is used. The empirical formula for it is C20H26N2O4. HCl with a 394.89 g/mol molecular weight.
INDICATIONS:
Treatment for gastrointestinal symptoms with itopride hydrochloride is available.
1- Functional dyspepsia
2- Non-ulcer dyspepsia, also known as chronic gastritis, i.e.
- Bloating sensation.
- satiety in the early stages.
- Discomfort or pain in the stomach.
- Anorexia.
- Heartburn.
- Nausea.
- Vomiting
MECHANISMS OF ACTION:
Due to its acetyl-cholinesterase inhibitory and dopamine D2 antagonistic properties, topside hydrochloride stimulates gastrointestinal propulsive motility.Acetylcholine is released upon itopride administration and is not degraded.
PHARMACODYNAMICS:
Through its interactions with D2 receptors found in the chemoreceptor trigger zone, itopride hydrochloride also has antiemetic effects. It has been demonstrated that itopride hydrochloride quickens gastric emptying in people. Itopride hydrochloride has a very specific effect on the upper GI tract. The serum levels of gastrin are not affected by itopride hydrochloride.
PHARMACOKINETIC PROPERTIES:
Absorption
The full dosage of itopride hydrochloride is absorbed. from the digestive system. The first-pass liver metabolism is estimated to account for 60% of the relative bioavailability. Food has no impact on bioavailability.
Distribution
Itopride hydrochloride is 96 percent bound to plasma proteins. The majority of the binding comes from albumin. Less than 15% of binding can be attributed to alpha-1-acid glycoprotein.
Metabolism
In people, itopride hydrochloride is extensively metabolized in the liver. Only 3 identified metabolites (which accounts for about 2% to 3% of the itopride) exhibits any pharmacologically significant activity. The oxidation of the N-dimethyl group on the tertiary amine produces N-oxide, which is the main metabolite in humans. A flavin-dependent mono-oxygenase (FM03) breaks down itopride hydrochloride. Trimethylaminuria, also known as fish odor syndrome, is an uncommon autosomal recessive condition that can be caused by genetic polymorphisms that affect the quantity and function of the human FMO-isozymes.
Patients with trimethylaminuria may therefore have longer itopride hydrochloride half-lives. Itopride hydrochloride did not inhibit or induce CYP2C19 or CYP2E1, according to in vivo pharmacokinetic studies on CYP-mediated reactions: CYP content and uridine diphosphate glucuronosyltransferase activity were unaffected by Itopride administration.
Excretion
The majority of the itopride hydrochloride and its metabolites are eliminated in the urine. Following oral administration to healthy subjects, the urinary excretions of itopride HCI and its N- oxide were 37% and 75.4 percent, respectively.
CONTRAINDICATIONS:
It should not be taken by patients who have previously developed an allergy to itopride hydrochloride or any of the excipients. Itopride hydrochloride should not be administered to patients in whom an increase in gastrointestinal motility poses a risk, such as abdominal perforation, mechanical obstruction, or hemorrhage.
PRECAUTIONS:
General
Acetylcholine is made to work better by itopride hydrochloride, but it also has potential cholinergic side effects.
Drug reactions
Metabolic interactions are not anticipated because flavin mono-oxygenase, not CYP450, metabolizes itopride hydrochloride in the majority of cases. Concurrent administration of warfarin, diazepam, diclofenac sodium, ticlopidine hydrochloride, nifedipine, and nicardipine hydrochloride did not alter protein binding in any way. Due to its gastroprokinetic effects, itopride hydrochloride may affect how well other oral medications are absorbed when taken concurrently. With drugs that have a narrow therapeutic index, sustained release, or enteric-coated formulations, extra caution should be exercised. Itopride's gastroprokinetic action is unaffected by anti-ulcer medications such as cimetidine, ranitidine, teprenone, and cetraxate.Itopride hydrochloride may act less effectively when taken with anticholinergic medications.
Pregnancy and Nursing
Pregnant women have not been the subject of sufficient, reliable studies. Therefore, unless the advantages outweigh the potential risks, itopride hydrochloride should not be used during pregnancy. Itopride hydrochloride is excreted in milk and there is a chance that nursing infants could experience negative side effects, so it should be decided whether to stop nursing or stop taking the medication, taking into account how important the medication is to the mother.
Geriatric Use
Itopride hydrochloride should generally be administered and monitored with the appropriate caution in elderly patients due to the higher frequency of decreased renal and hepatic function as well as co-occurring diseases or other drug therapy.
ADVERSE REACTION:
Itopride hydrochloride patients have experienced the following side effects:.
- Thrombocytopenia as well as leucopenia.
- Anaphylactic reaction.
- Gynecomastia and an increase in prolactin levels.
- Headache, tremor, and wooziness.
- Nausea, increased salivation, diarrhea, constipation, and abdominal pain.
- Rash with redness and itching.
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