Itopride

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Itopride
Clinical data
Trade namesGanaton
AHFS/Drugs.comInternational Drug Names
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
FMO3), primarily N-oxidation[2]
Elimination half-life5.7±0.3 hours
ExcretionRenal (3.7–4.1% as unchanged itopride, 75.4–89.4% as itopride-N-oxide)[1]
Identifiers
  • N-[[4-(2-Dimethylaminoethoxy)phenyl]methyl]-3,4-dimethoxybenzamide
JSmol)
  • CN(C)CCOC1=CC=C(C=C1)CNC(=O)C2=CC(=C(C=C2)OC)OC

  • as HCl: Cl.COC1=CC=C(C=C1OC)C(=O)NCC1=CC=C(OCCN(C)C)C=C1
  • InChI=1S/C20H26N2O4/c1-22(2)11-12-26-17-8-5-15(6-9-17)14-21-20(23)16-7-10-18(24-3)19(13-16)25-4/h5-10,13H,11-12,14H2,1-4H3,(H,21,23) ☒N
  • Key:QQQIECGTIMUVDS-UHFFFAOYSA-N ☒N

  • as HCl: InChI=1S/C20H26N2O4.ClH/c1-22(2)11-12-26-17-8-5-15(6-9-17)14-21-20(23)16-7-10-18(24-3)19(13-16)25-4;/h5-10,13H,11-12,14H2,1-4H3,(H,21,23);1H
  • Key:ZTOUXLLIPWWHSR-UHFFFAOYSA-N-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

Itopride (

D2 receptor antagonist and acetylcholinesterase inhibitor.[5][6]

Medical uses

Slovak Republic
.

Typically, itopride is indicated in the treatment of GI symptoms caused by reduced GI motility:

Itopride was shown to significantly improve symptoms in patients with functional dyspepsia and motility disorders in placebo-controlled trials.

These studies concluded that the reduction in the severity of symptoms of functional dyspepsia after 8 weeks of treatment with itopride indicated that itopride was significantly superior to placebo and that itopride yielded a greater rate of response than placebo in significantly reducing pain and fullness.[11]

Contraindications and precautions

Itopride is a relatively new drug and it is not currently approved for normal prescribed use nor OTC use in either the US nor the UK. However, this does not necessarily indicate that itopride is not effective or safe.

Patients taking itopride should report any side-effects to their treating physician.

Itopride is contraindicated in hypersensitivity to itopride or

hemorrhage, obstruction or perforation. Itopride may not be indicated for those suffering from Parkinson's disease or other conditions involving dopamine
regulation issues. Itopride should be used with special caution in the young and the elderly. Little information is available at this time regarding the safe use of itopride during pregnancy.

Adverse drug reactions

The most common side-effects of itopride include mild to moderate abdominal pain and diarrhoea.[7] Some other side effects that may occur include: rash, giddiness, exhaustion, back or chest pain, increased salivation, constipation, headache, sleeping disorders, dizziness, galactorrhea, and gynecomastia.

Leukopenia, a reduction in the normal level of white blood cells, can be a potentially life-threatening reaction to itopride.

Central nervous system adverse effects do not tend to occur due to poor penetration across the blood brain barrier, although a slight raising of prolactin levels may occur.[7] Raising of prolactin levels is more common with high dose regimes of itopride.[12]

Cardiac studies

Itopride belongs to the same

arrhythmias. However, itopride does not have any adverse effect on the QT interval.[7]

Later, in a study conducted with healthy adult volunteers, itopride was shown as unlikely to cause cardiac arrhythmias or ECG changes in part to the lack of significant interaction and metabolism via the

benzamides such as cisapride and mosapride, which are 5-HT4 agonists. The affinity of cisapride for 5-HT4 receptors in the heart has been implicated in the undesirable cardiac effects of cisapride itself.[medical citation needed
]

The conclusion of this study revealed that itopride is devoid of any abnormal effect on QT interval. Therefore, it may be possible that itopride could be considered as a better and certainly safer prokinetic agent than either cisapride or mosapride, and itopride should also be considered a welcome treatment addition for symptomatic nonulcer dyspepsia and other gastric motility disorders.[13]

Pharmacology

Itopride acts as a selective dual

D2 receptor antagonist and acetylcholinesterase inhibitor.[5][6]

There is evidence that itopride may have prokinetic effects throughout the gastrointestinal tract from the stomach to the end of the colon.

potassium channels.[16]

Similarly to other D2 receptor antagonists, itopride has been found to dose-dependently increase prolactin levels.[6]

Pharmacokinetics

After oral administration itopride undergoes rapid and extensive absorption with levels of itopride peaking in the blood plasma after only 35 minutes. Itopride is primarily eliminated via the kidneys having an

elimination half-life of approximately 6 hours.[17]

Mechanism of action

Ganaton (Itopride) 50 mg tablets. Engraving says "HC 803"

Itopride increases acetylcholine concentrations by inhibiting dopamine D2 receptors and acetylcholinesterase. Higher acetylcholine increases GI peristalsis, increases the lower esophageal sphincter pressure, stimulates gastric motility, accelerates gastric emptying, and improves gastro-duodenal coordination.[7]

Itopride given as a single dose study found that it also raises levels of motilin, somatostatin and lowers levels of cholecystokinin, as well as adrenocorticotropic hormone. These effects may also contribute to itopride's pharmacology.[18]

Interactions

Anticholinergic agents reduce the action of itopride.[medical citation needed]

Society and culture

Names

Itopride is available under the brand names Ganaton (

RU), Abbott Laboratories), Itoprid PMCS (CZ, SK), Itomed (KG, KZ, MD, RU, UA, UZ) and Prokit (PL), PRO.MED.CS Praha a.s.), Itogard (Apex Pharmaceuticals, Nepal) and others. In Mexico, itopride (50 mg) is sold by Takeda Laboratories under the brand name Dagla. In Bulgaria and other countries of East Europe itopride (50 mg) is sold by Zentiva under the brand name Zirid [19]

References

  1. ^ "Ganaton (itopride hydrochloride) Tablets 50 mg. Prescribing Information" (PDF). Abbott Japan Co., Ltd. Archived from the original (PDF) on 11 December 2015. Retrieved 9 December 2015.
  2. ISBN 978-3-527-32954-0
    .
  3. PMID 8835639
    .
  4. PMID 16495395
    .
  5. ^
    ISBN 978-1-60761-552-1
    .
  6. ^
    ISBN 978-1-4557-0450-7
    .
  7. ^
    PMID 23326147
    .
  8. PMID 18019739
    .
  9. PMID 15305632
    .
  10. ^ Kojecky V, Bernatek J, Bakala J, Weissova D (2005). "[The influence of itopride on the rate and course of the evacuation of stomach of the diabetic patients and their relationship to diabetes control]". Ces.Slov.Gastroent.Hepatol., 2005. 59 (1): 17–20.
  11. PMID 16495395
    .
  12. PMID 16015691
    .
  13. ^ Gupta S, Kapoor V, Gupta BM, Verma U (2005). "Effect Of Itopride hydrochloride on QT interval in adult healthy volunteers" (PDF). JK-Practitioner. 12 (4): 207–10.
  14. PMID 18581598
    .
  15. S2CID 25760696
    .
  16. PMID 11127807
    .
  17. PMID 23960836
    .
  18. S2CID 22219251
    .
  19. ^ "Z".

External links

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