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Rational Medical Therapy of Functional GI Disorders
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
Richard M. Sperling, Kenneth R. McQuaid
The effects of 5-HT3 antagonists on gut afferent sensation are only beginning to be studied. In a study of 12 patients (nine with diarrhea), Prior and Read (248) demonstrated significant increases in the mean threshold of latex-balloon-inflation volumes for perception of gas, stool urgency, and discomfort and a significant decrease in postprandial anorectal motility after administration of i.v. granisetron. However, in a slightly different study that employed barostats in the descending colon and rectum of 10 healthy volunteers and five diarrhea-predominant IBS patients, Camilleri et al. (249) could not detect a difference in rectal sensitivity or tone after ondansetron. Whether there are particular differences in efficacy between ondansetron and granisetron remains to be established.
Dermal and Transdermal Drug Delivery Systems
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
Kenneth A. Walters, Majella E. Lane
Granisetron (Figure 1.10, Table 1.2) is a serotonin 5-HT3 receptor antagonist that is used as an anti-emetic to treat nausea and vomiting during and following chemotherapy. The drug was approved for use in the USA in 1994 and a transdermal system (Sancuso®, ProStrakan Inc) was approved in September 2008. Sancuso® is a drug-in-adhesive matrix patch that contains 34.3 mg granisetron in a 52 cm2 patch. The patch nominally delivers 3.1 mg/24 h and is worn for up to seven days. The pharmacokinetics of transdermal granisetron were described by Howell et al. (2009) using data from a phase I study in healthy volunteers and from phase II and III studies (a total of over 800 subjects). Following a 2 mg oral dose, plasma Cmax was reached two hours after dosing and Cave was 2.6 ng/mL. Following application of a 52 cm2 patch plasma Cave was 2.2 ng/mL over six days. Clearance was not affected by age, gender, weight or renal function.
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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Granisetron is metabolised primarily in the liver by oxidation followed by conjugation. The major compounds are 7-OH-granisetron and its sulphate and glycuronide conjugates. Although antiemetic properties have been observed for 7-OH-granisetron and indazoline N-desmethyl granisetron, it is unlikely that these contribute significantly to the pharmacological activity of granisetron in man. Clearance is predominantly by hepatic metabolism. Urinary excretion of unchanged granisetron averages 12% of dose whilst that of metabolites amounts to about 47% of dose. The remainder is excreted in faeces as metabolites.
An acryl resin-based swellable microneedles for controlled release intradermal delivery of granisetron
Published in Drug Development and Industrial Pharmacy, 2018
Guozhong Yang, Meilin He, Suohui Zhang, Man Wu, Yunhua Gao
Granisetron is serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy for up to five consecutive days. Currently, GRB transdermal patch (SANCUSO®) is widely used clinically. The patch may be applied to the upper outer arm for 24–48 h before chemotherapy as appropriate [22]. The lag time of release of GRB shows more than 12 h. In this study, we designed a new type of microneedle formulations which realized controlled-release for about six days and shortened the lag time. The solubility of GRB in water is 0.147 mg/mL. To solve the problems of six day controlled-release and loading capacity of GRB, an alcohol-soluble pharmaceutical excipient, EUDRAGIT RL100 acrylic resin, as SMNs matrix materials was chosen.
Attenuation of spinal anesthesia induced hypotension with granisetron in type I diabetic parturients: A randomized controlled clinical trial
Published in Egyptian Journal of Anaesthesia, 2022
Abdelrhman Alshawadfy, EmadEldeen Ahmed Ibrahim, Amr Helmy, Mohamed A. Elsadany, Wesam F. Alyeddin
Our results revealed that granisetron caused a significant reduction in the total dose and the need for further bolus doses of ephedrine. In addition, granisetron significantly reduced nausea and vomiting. Apgar score after 5 minutes from delivery showed a significantly higher score in the granisetron group compared with the control group. The intraoperative HR and systolic, diastolic, and mean arterial blood pressures were significantly reduced in the control group compared to the granisetron group at different intraoperative time intervals.
Comparison between serratus anterior plane block versus erector spinae plane block for postoperative analgesia after video-assisted thoracoscopic surgery (VATS)
Published in Egyptian Journal of Anaesthesia, 2023
Sameh Salem Hafny Taha, Beshoy Eshak Aziz Hanna, Gamal Eldin Mohammad Ahmed Elewa, Hadil Magdy Abd Elhamid Mohamed, Dalia Fahmy Emam Ali, Mohamed MoienMohamed Elsaid
Fentanyl (1 µg/kg), propofol (2 mg/kg) and atracurium (0.5 mg/kg) were IV utilized for general anesthesia induction. Intubation was done using a double-lumen endobronchial tube. Anesthesia was continued using isoflurane 2 vol. %, 50% O2 and 50% air. Moreover, three milligram of Granisetron was given as prophylactic against nausea and vomiting post-operatively. During operation, 6 mL/kg/h of Ringer’s solution was administered.