Cinitapride Tartrate

It is pertinent to objectively assess the severity of diabetic gastroparesis and tailor treatment accordingly. The current study was planned to document gastroparesis by gastric emptying scintigraphy (GES) objectively and see the effect of medications and diet control on clinical and GES after four weeks.

A prospective, open-label randomized trial was conducted in the Department of Internal Medicine at a tertiary care teaching hospital over twelve months. Type 2 diabetic patients aged 18-65 years diagnosed with a case of delayed gastric emptying by gastric scintigraphy were included. All baseline GSCI was recorded, and then they were allotted to 3 groups - Group-1 (Levosulpiride 25mg once daily), group-2 (Cinitapride 1mg thrice daily), and Group-3 (Waitlisted control) by block randomization and followed-up weekly till four weeks. After four weeks duration, if not improved clinically, then Group-3 on diet and diabetic control only, were randomized into Levosulpiride 25mg once daily (Group 1), and Cinitapride 1mg Thrice daily (Group 2) for the next four weeks.

Forty confirmed cases with diabetic gastroparesis documented by Gastroparesis Symptom Cardinal Index (GCSI) scoring and later by Scintigraphy (GES) were included in this study. However, there was no statistically significant difference between the Levosulpiride and Cinitapride groups when all symptoms were taken into account. Levosulpiride was significantly more effective than Cinitapride in improving individual symptoms like nausea, vomiting, stomach fullness, and early satiety.

Levosulpiride is better than Cinitapride in improving the symptoms of diabetic gastroparesis but no significant effect on gastric scintigraphy.

Cinitapride is a gastrointestinal prokinetic drug, prescribed for the treatment of functional dyspepsia, and as an adjuvant therapy for gastroesophageal reflux disease. In this study, we aimed to explore the impact of relevant variants in CYP3A4 and CYP2C8 and other pharmacogenes, along with demographic characteristics, on cinitapride pharmacokinetics and safety; and to evaluate the impact of CYP2C8 alleles on the enzyme's function. Twenty‐five healthy volunteers participating in a bioequivalence clinical trial consented to participate in the study. Participants were genotyped for 56 variants in 19 genes, including cytochrome P450 (CYP) enzymes (e.g., CYP2C8 or CYP3A4) or transporters (e.g., SLC or ABC), among others. CYP2C8*3 carriers showed a reduction in AUC of 42% and Cmax of 35% compared to *1/*1 subjects (p = 0.003 and p = 0.011, respectively). *4 allele carriers showed a 45% increase in AUC and 63% in Cmax compared to *1/*1 subjects, although these differences did not reach statistical significance. CYP2C8*3 and *4 alleles may be used to infer the following pharmacogenetic phenotypes: ultrarapid (UM) (*3/*3), rapid (RM) (*1/*3), normal (NM) (*1/*1), intermediate (IM) (*1/*4), and poor (PM) metabolizers (*4/*4). In this study, we properly characterized RMs, NMs, and IMs; however, additional studies are required to properly characterize UMs and PMs. These findings should be relevant with respect to cinitapride, but also to numerous CYP2C8 substrates such as imatinib, loperamide, montelukast, ibuprofen, paclitaxel, pioglitazone, repaglinide, or rosiglitazone.