Cidine (cinitapride) / Eisai, Almirall - LARVOL DELTA

QbD-based formulation development and evaluation of lipid-cellulose-based extended-release multi-particulates of cinitapride and its in-silico PBPK modeling. (PubMed, Int J Biol Macromol) - "The PBPK predicted Cmax, Tmax, AUC0-t, and AUC0-∞ was 361.93 pg/ml, 6.88 h, 4567.8 pg/ml/h, and 5204.7 pg/ml/h, respectively. Lipid-cellulose-based extended-release Cinitapride matrix pellets were successfully prepared and can be effectively used as a single dose regimen for treating functional dyspepsia and gastrointestinal reflux disease."

Journal • Dyspepsia • Gastroenterology • Gastrointestinal Disorder

Efficacy of prokinetic agents in diabetic gastroparesis comparing symptomatology and scintigraphy - An open-label trial. (PubMed, Caspian J Intern Med) - "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."

Journal • Diabetes • Gastrointestinal Disorder • Metabolic Disorders • Type 2 Diabetes Mellitus

Prokinetics for the treatment of functional dyspepsia: an updated systematic review and network meta-analysis. (PubMed, BMC Gastroenterol) - "Metoclopramide and cinitapride may have a better efficacy than other prokinetics in the treatment of FD, and cinitapride may have a lower risk of total adverse events. Further studies using uniform definitions or validated tools to measure the total efficacy rate are needed."

Clinical • Journal • Retrospective data • Review • Dyspepsia

CHRONIC INTESTINAL PSEUDO-OBSTRUCTION IN PATIENTS WITH SYSTEMIC SCLEROSIS (EULAR 2023) - "Regarding CIPO treatment, all of them received dietetic recommendations, 6 (85.7%) prokinetics (cinitapride, prucalopride or erythromycin) and 4 (57.1%) the somatostatin analogue octreotide subcutaneous (sc)...Among them, one improved after initiating octreotide sc, 3 required PTN, 2 IVIG and 1 case was treated with adalimumab...Diet recommendations, prokinetics and octreotide are common initial therapies, reserving IVIG and PTN for refractory cases or with more aggressive onset. Notwithstanding, the mortality related to this gastrointestinal involvement is certainly significant."

Clinical • Cardiovascular • Fibrosis • Gastrointestinal Disorder • Hypertension • Immunology • Interstitial Lung Disease • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • Rheumatology • Scleroderma • Systemic Sclerosis

CYP2C8*3 and *4 define CYP2C8 phenotype: An approach with the substrate cinitapride. (PubMed, Clin Transl Sci) - "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."

Journal • Dyspepsia • Gastroenterology • Gastroesophageal Reflux Disease • Gastrointestinal Disorder • CYP3A4

Efficacy of Pro-Kinetic Agents in Type 2 Diabetes Mellitus Patients With Gastroparesis Using Lactulose Hydrogen Breath Testing: A Randomized Trial. (PubMed, Cureus) - "After randomization, all 50 patients were divided into four arms (cinitapride, metoclopramide, levosulpiride, and domperidone) of different prokinetics and followed up for four weeks; after which, repeat gastroparesis cardinal symptom index score and orocecal transit time were recorded in order to assess the response to the treatment. Conclusion Our study showed statistically significant improvement with four prokinetics drugs in terms of gastroparesis cardinal symptom index score and orocecal transit time, but there was no statistically significant benefit of one prokinetic drug over the other. Our study showed promising results with regard to prokinetic use in diabetic gastroparesis."

Journal • Diabetes • Gastrointestinal Disorder • Metabolic Disorders • Type 2 Diabetes Mellitus

"Good thing about 🇵🇦 Prokinetic options available Domperidone Levosulpiride Cinitapride" (@elrets)

Comparative Efficacy of Various Pharmacological Interventions in the Treatment of Functional Dyspepsia: A Network Meta-Analysis. (PubMed, Dig Dis Sci) - "Our study confirmed the effectiveness of several pharmacological treatments for ameliorating functional dyspepsia. Furthermore, levosulpiride relatively ranked the best in managing FD. Physicians should be encouraged to apply promising pharmacological interventions (e.g., levosulpiride and cisapride). However, the results should be interpreted with caution due to small study effects."

Journal • Retrospective data • Dyspepsia

GASTROPARESIS SECONDARY TO PULMONARY VEIN CRYOABLATION: A FACTOR TO CONSIDER. (PubMed, Rev Esp Enferm Dig) - "A 72-year-old woman with history of symptomatic paroxysmal atrial fibrillation treated with edoxaban...Treatment with intravenous erythromycin was prescribed for 3 days and subsequently with oral cinitapride with good evolution...Endoscopic treatment is saved for more severe patients (3). The new techniques of pulmonary ablation have increased the cases of symptomatic gastroparesis so it is important to recognize this trigger factor (2)."

Journal • Atrial Fibrillation • Cardiovascular • CNS Disorders • Diabetes • Gastrointestinal Disorder • Metabolic Disorders • Movement Disorders • Pain • Parkinson's Disease

Luetic gastritis: an uncommon cause of gastritis. (PubMed, Rev Esp Enferm Dig) - "This was associated with general symptoms including myalgia, fatigue, epigastric pain, nausea and vomiting. The patient had been taking omeprazole and cinitapride with little improvement."

Journal • Dermatology • Fatigue • Gastrointestinal Disorder • Musculoskeletal Pain • Pain

Pharmacokinetics and tolerability of Cinitapride in healthy Chinese volunteers: a randomized, open-label, single- and multiple-dose study. (PubMed, Xenobiotica) - "The pharmacokinetic parameters of this study were consistent with study results of non-Chinese subjects. Good tolerability was demonstrated in both single- and multiple-dose studies with dosage range from 1 to 4 mg in healthy Chinese subjects."

Clinical • Journal • PK/PD data • Biosimilar

Development of an UPLC-MS/MS micromethod for quantitation of cinitapride in plasma and its application in a pharmacokinetic interaction trial. (PubMed) - Bioanalysis - "The method proved to be rapid, accurate and stable within a range between 50 and 2000 pg/ml and was successfully validated and applied in a pharmacokinetic interaction trial, where it was demonstrated that oral co-administration of simethicone does not modify the bioavailability of CIN."

Journal • Biosimilar

Sleep related painful erection: an algorithm for evaluation and management. (PubMed, Basic Clin Androl) - "Cinitapride is very promising, but only one case was studied and no side effects were reported. Clozapine can be very dangerous although highly effective. Based on the limited number of treatment trials and reported cases, the low level of evidence and the lack of randomized clinical trials, no treatment consensus for SRPE can be reached. We suggested a useful tool for clinicians: an algorithm for the management of SRPE to facilitate their access to the literature without exhaustive return to case reports and series upon each case faced."

Journal • Review

Stability and in vitro release kinetic studies of cinitapride (1mg) mouth dissolving tablets. (PubMed, Pak J Pharm Sci) - "Accelerated stability testing data showed excellent results of drug assay (>99%) along with physical characteristics indicating the absence of drug degradation as well excipient interaction. The estimated shelf life period of various optimized trial formulations was found in between 33 to 41 months."

Journal • Preclinical

Effects of superdisintegrants in oral dissolving formulation of cinitapride tablets. (PubMed, Pak J Pharm Sci) - "The assay and content uniformity of FC2 were estimated to be 100.02±0.36 and 99.66±1.70 percent correspondingly. On the basis of the findings it was concluded that MDT could be successfully developed by incorporating appropriate concentration of superdisintegrant and their combinations."

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Formulation design, characterization and optimization of cinitapride (1mg) immediate release tablets using direct compression technology. (PubMed, Pak J Pharm Sci) - "Trial optimized formulations were highly stable with the shelf lives of 58-64 months. So, keeping in view the results of present investigation, it is concluded that the technique of manufacturing and optimization is found to be excellent for developing immediate release cinitapride tablets."

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Development and validation of stability indicating assay method for cinitapride in bulk & tablets. (PubMed, Pak J Pharm Sci) - "However; drug estimation was not influenced in presence of degradation moieties formed during acid, base, oxidation, thermal and photolytic breakdown. Overall, the investigated technique is robust and specific that would be successfully used to quantify the cinitapride hydrogen tartarate in pharmaceutical dosage and bulk form in future."

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