cinnarizine and Vomiting

Cinnarizine was evaluated for the prevention of seasickness in a laboratory and sea study. The effects of 25 mg cinnarizine on the vestibulo-ocular reflex were investigated in 13 subjects. Significant reduction of the gain in response to sinusoidal oscillations at 0.02, 0.08, and 0.16 Hz (p < 0.05) and increased phase lead at 0.16 Hz (p < 0.01) were observed. The effect of 25 and 50 mg cinnarizine on seasickness severity was examined in 95 subjects during a voyage in rough seas. Seasickness symptoms were improved in 69% of the subjects by 50 mg cinnarizine versus 35% and 31% in the groups receiving 25 mg cinnarizine and placebo (p < 0.05 and p < 0.01, respectively). The percentage of vomiting protection provided by 50 mg cinnarizine was 63% (p < 0.05). We conclude that 50 mg cinnarizine is an effective drug for the prevention of seasickness. The reduction in vestibular sensitivity observed even after administration of 25 mg cinnarizine may explain the potency of cinnarizine in the prevention of seasickness.

Topics: Adolescent; Adult; Cinnarizine; Double-Blind Method; Humans; Male; Motion Sickness; Reflex, Vestibulo-Ocular; Severity of Illness Index; Vomiting

The antiemetic efficacy of cinnarizine was assessed in 17 cancer patients receiving platin-based chemotherapy (cisplatin dose-range 30-160 mg, or carboplatin 270-600 mg) in a randomised, cross-over study. The patients were prophylactically given oral metoclopramide 3 x 1 mg/kg and lorazepam 2 x 1 mg with or without cinnarizine 3 x 75 mg. The antiemetic combination with cinnarizine prevented emesis completely on 51% of 35 days with chemotherapy and less than 3 emetic episodes occurred on 86% of the days, compared with 43% and 57% (p less than 0.01) without cinnarizine respectively. Severe nausea was significantly less frequent with cinnarizine and 59% of the chemotherapy days were without nausea, compared to 46% of the days without cinnarizine (p less than 0.05). Side-effects were uncommon and minor with both antiemetic regimens. The study suggests that addition of cinnarizine to metoclopramide and lorazepam improves antiemetic prophylaxis in low to medium dose platin-based chemotherapy.

Topics: Adult; Aged; Carboplatin; Cinnarizine; Cisplatin; Combined Modality Therapy; Female; Humans; Lorazepam; Male; Metoclopramide; Middle Aged; Nausea; Vomiting

The objective of the study was to investigate the effect of iron oxide in the development of mucoadhesive tablets of cinnarizine using Eudragit RLPO polymer. A simplex lattice design was employed for optimizing the drug delivery system.. Different concentrations of Eudragit RLPO (X1), iron oxide (X2) and PVP K 30 (X3) were taken as independent variables and mucoadhesive strength, t50%, t90%, MDT and tablet tensile strength were the selected response variables. Contour and 3D plots were drawn to portray the relationship between independent and response variables. Ex vivo studies were performed for the determination of mucoadhesive strength of formulated tablets employing texture analyzer. ATR-FTR, DSC and zeta potential determination were conducted for drug-excipient and ionic interaction studies.. Friability, hardness and tensile strength of mucoadhesive tablet formulation were found to be 0.42 ± 0.21%, 3.93 ± 1.57 kg/cm(2) and 0.65 ± 0.26 mN/m(2), respectively. Mucoadhesive strength was found to be ranging between 5.75 ± 4.41 and 42.85 ± 3.94 g. Value of release exponent (n) was found to be 0.65 ± 0.22, indicating anomalous drug release behavior from the formulations. Numerical optimization using the desirability approach was employed for developing optimized formulation by setting constraints of the dependent and independent variables. The mucoadhesive tablet formulation composition consisting of 8.58% w/w Eudragit RLPO, 7.02% w/w iron oxide and 7.26% w/w PVP K 30 fulfilled maximum requirements of an optimum formulation with better regulation of the selected constraints.. Eudragit RLPO and iron oxide combination showed high level potential for fabricating gastroretentive as well as mucoadhesive drug delivery systems.

Topics: Chemistry, Pharmaceutical; Cinnarizine; Delayed-Action Preparations; Drug Delivery Systems; Excipients; Ferric Compounds; Gastric Mucosa; Gastrointestinal Tract; Histamine H1 Antagonists; Microscopy, Electron, Scanning; Nausea; Polymethacrylic Acids; Spectroscopy, Fourier Transform Infrared; Tablets; Tensile Strength; Vomiting

An oral combination of cinnarizine and lorazepam was studied for the prophylaxis of nausea and vomiting induced by strongly emetogenic cancer chemotherapy. 56% of 59 chemotherapy courses in 29 patients were completed without emesis. Of the 42 cisplatin-containing regimens, 52% were without vomiting and 62% free of nausea. A further 11 patients (17 courses) received non-cisplatin emetogenic chemotherapy. In this group full emetic control was achieved in 65% of the courses. Diarrhea in 4% of the courses was the only side effect of this new oral combination.

Topics: Administration, Oral; Adult; Antiemetics; Antineoplastic Agents; Cinnarizine; Cisplatin; Drug Therapy, Combination; Female; Humans; Lorazepam; Male; Middle Aged; Nausea; Pilot Projects; Prospective Studies; Vomiting