- Granisetron Extended-Release Injection: A Review in Chemotherapy-Induced Nausea and Vomiting. [Journal Article]
- DDrugs 2016 Dec 03
- An extended-release (ER) subcutaneously injectable formulation of the first-generation 5-HT3 receptor antagonist granisetron is now available in the USA (Sustol(®)), where it is indicated for the pre...
An extended-release (ER) subcutaneously injectable formulation of the first-generation 5-HT3 receptor antagonist granisetron is now available in the USA (Sustol(®)), where it is indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) following moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide combination chemotherapy regimens in adults. Granisetron ER is administered as a single subcutaneous injection and uses an erosion-controlled drug-delivery system to allow prolonged granisetron release. Primary endpoint data from phase III studies after an initial cycle of chemotherapy indicate that, when used as part of an antiemetic regimen, granisetron ER injection is more effective than intravenous ondansetron in preventing delayed CINV following highly emetogenic chemotherapy (HEC); is noninferior to intravenous palonosetron in preventing both acute CINV following MEC or HEC and delayed CINV following MEC; and is similar, but not superior, to palonosetron in preventing delayed CINV following HEC. The benefits of granisetron ER were seen in various patient subgroups, including those receiving anthracycline plus cyclophosphamide-based HEC, and (in an extension of one of the studies) over multiple MEC or HEC cycles. Granisetron ER injection is generally well tolerated, with an adverse event profile similar to that of ondansetron or palonosetron. Thus, granisetron ER injection expands the options for preventing both acute and delayed CINV in adults with cancer receiving MEC or anthracycline plus cyclophosphamide-based HEC.
- Safety and efficacy of NEPA, an oral fixed combination of netupitant and palonosetron, in older patients. [Journal Article]
- JGJ Geriatr Oncol 2016 Nov 23
- CONCLUSIONS: NEPA is highly effective in older patients receiving MEC or HEC regimens. NEPA is also well tolerated, demonstrating suitability for use in older patients who may have comorbidities.
- NEPA, a fixed oral combination of netupitant and palonosetron, improves control of chemotherapy-induced nausea and vomiting (CINV) over multiple cycles of chemotherapy: results of a randomized, double-blind, phase 3 trial versus oral palonosetron. [Journal Article]
- SCSupport Care Cancer 2016 Nov 24
- CONCLUSIONS: NEPA, a convenient, guideline-consistent, fixed antiemetic combination is effective and safe over multiple cycles of chemotherapy.
- Palonosetron, aprepitant, and dexamethasone for prevention of nausea and vomiting after high-dose melphalan in autologous transplantation for multiple myeloma: A phase II study. [Journal Article]
- IJInt J Hematol 2016 Nov 21
- Chemotherapy-induced nausea and vomiting (CINV) is a significant side effect in multiple myeloma (MM) patients receiving high-dose melphalan treatment followed by autologous stem cell transplantation...
Chemotherapy-induced nausea and vomiting (CINV) is a significant side effect in multiple myeloma (MM) patients receiving high-dose melphalan treatment followed by autologous stem cell transplantation (ASCT). We evaluated the efficacy and safety of a triple antiemetic combination of palonosetron, aprepitant, and low-dose dexamethasone in 24 MM patients who received melphalan conditioning (100 mg/m(2) on days 1-2) before ASCT (on day 4). Intravenous palonosetron (0.75 mg on day 1), oral aprepitant (125 mg on day 1; 80 mg on days 2-4), and intravenous dexamethasone (6.6 mg on days 1-4) were administered for prevention of CINV. Complete response (no emesis and no rescue antiemetic) and complete control (no emesis, no rescue antiemetic, and no more than mild nausea) rates were 75 and 68% during the overall phase (0-120 h), while they were 88 and 86% in the acute phase (0-48 h), 75 and 68% in the delayed phase (48-120 h), and 67 and 59% in the extended phase (120-168 h), respectively. There were no serious adverse events related to the antiemetic therapy. In conclusion, the three-antiemetic regimen consisting of palonosetron, aprepitant, and dexamethasone was safe and effective for controlling CINV due to high-dose melphalan treatment, especially during the delayed phase.
- Erratum to "Efficacy of palonosetron in postoperative nausea and vomiting (PONV)-a meta-analysis" [J Clin Anesth 2016:34(459-482)]. [Published Erratum]
- JCJ Clin Anesth 2016; 35:492
- Palonosetron-Induced Anaphylaxis During General Anesthesia: A Case Report. [Case Reports]
- AAAllergy Asthma Immunol Res 2017; 9(1):92-95
- Palonosetron is a 5-hydroxytryptamine-3 (5-HT-3) receptor antagonist used for preventing postoperative nausea and vomiting. Compared with ondansetron and granisetron, it is a better drug because of p...
Palonosetron is a 5-hydroxytryptamine-3 (5-HT-3) receptor antagonist used for preventing postoperative nausea and vomiting. Compared with ondansetron and granisetron, it is a better drug because of prolonged action and minimal side effects. Some adverse effects of palonosetron have been reported. In this report, we describe a 37-year-old male who developed severe hypersensitivity reactions to palonosetron during surgery for kidney donation. His medical history was unremarkable, except for inguinal hernia with herniorrhaphy 8 years ago. The surgery was uneventful until 2 hours 20 minutes. After palonosetron injection, his blood pressure dropped to 80/50 mm Hg, and facial edema, rash, conjunctival swelling, and wheezing developed. The patient was resuscitated by administration of ephedrine, hydrocortisone, and peniramine. Following the surgery, the patient was monitored for 3 days, and there were no subsequent anaphylactic reactions or other complications. The skin test on postoperative day 54 was positive for hypersensitivity to palonosetron. Although palonosetron is known for its safety, other hypersensitivity events have been reported. Ondansetron is another widely used 5-HT-3 antagonist, which has been reported to cause anaphylaxis. Therefore, clinicians should be aware of the possibility of patients experiencing severe adverse reactions to palonosetron.
- In silico investigation into the interactions between murine 5-HT3 receptor and the principle active compounds of ginger (Zingiber officinale). [Journal Article]
- JMJ Mol Graph Model 2016 Oct 26; 70:315-327
- Gingerols and shogaols are the primary non-volatile actives within ginger (Zingiber officinale). These compounds have demonstrated in vitro to exert 5-HT3 receptor antagonism which could benefit chem...
Gingerols and shogaols are the primary non-volatile actives within ginger (Zingiber officinale). These compounds have demonstrated in vitro to exert 5-HT3 receptor antagonism which could benefit chemotherapy-induced nausea and vomiting (CINV). The site and mechanism of action by which these compounds interact with the 5-HT3 receptor is not fully understood although research indicates they may bind to a currently unidentified allosteric binding site. Using in silico techniques, such as molecular docking and GRID analysis, we have characterized the recently available murine 5-HT3 receptor by identifying sites of strong interaction with particular functional groups at both the orthogonal (serotonin) site and a proposed allosteric binding site situated at the interface between the transmembrane region and the extracellular domain. These were assessed concurrently with the top-scoring poses of the docked ligands and included key active gingerols, shogaols and dehydroshogaols as well as competitive antagonists (e.g. setron class of pharmacologically active drugs), serotonin and its structural analogues, curcumin and capsaicin, non-competitive antagonists and decoys. Unexpectedly, we found that the ginger compounds and their structural analogs generally outscored other ligands at both sites. Our results correlated well with previous site-directed mutagenesis studies in identifying key binding site residues. We have identified new residues important for binding the ginger compounds. Overall, the results suggest that the ginger compounds and their structural analogues possess a high binding affinity to both sites. Notwithstanding the limitations of such theoretical analyses, these results suggest that the ginger compounds could act both competitively or non-competitively as has been shown for palonosetron and other modulators of CYS loop receptors.
- Neurokinin-1 Receptor Antagonist-Based Triple Regimens in Preventing Chemotherapy-Induced Nausea and Vomiting: A Network Meta-Analysis. [Review]
- JNCIJ Natl Cancer Inst 2017; 109(2)
- CONCLUSIONS: Different NK-1RAs-based triple regimens shared equivalent effect on CINV control. Various triple regimens had superior antiemetic effect than duplex regimen in patients with HEC. Only aprepitant-based triple regimen showed better CINV control compared with duplex regimen in patients receiving MEC. Palonosetron and first-generation 5HT3RAs might share equivalent CINV control in the combination of NK-1RAs and dexamethasone. Lower doses of dexamethasone might be applied when used with NK-1RAs and 5HT3RAs.
- Palonosetron and granisetron in postoperative nausea vomiting: A randomized double-blind prospective study. [Journal Article]
- AEAnesth Essays Res 2016 Sep-Dec; 10(3):402-407
- CONCLUSIONS: Prophylactic therapy with palonosetron is more effective than granisetron in the prevention of PONV after laparoscopic surgeries under general anesthesia.
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- Comparison of the Prophylactic Antiemetic Efficacy of Aprepitant Plus Palonosetron Versus Aprepitant Plus Ramosetron in Patients at High Risk for Postoperative Nausea and Vomiting After Laparoscopic Cholecystectomy: A Prospective Randomized-controlled Trial. [Journal Article]
- SLSurg Laparosc Endosc Percutan Tech 2016; 26(5):354-357
- We compared the antiemetic efficacy of aprepitant plus palonosetron versus aprepitant plus ramosetron in patients after laparoscopic cholecystectomy. A total of 88, nonsmoking, female patients underg...
We compared the antiemetic efficacy of aprepitant plus palonosetron versus aprepitant plus ramosetron in patients after laparoscopic cholecystectomy. A total of 88, nonsmoking, female patients undergoing laparoscopic cholecystectomy were randomly allocated to 2 groups of 44 each who received palonosetron 0.075 mg (aprepitant plus palonosetron group) and ramosetron 0.3 mg (aprepitant plus ramosetron group) after induction of anesthesia. All patients received aprepitant 80 mg 2 hours before surgery. The incidence of postoperative nausea and vomiting (PONV), use of rescue antiemetic, pain severity, and any side effects were assessed for 24 hours after surgery. The incidence of PONV and use of rescue antiemetic were less in aprepitant plus palonosetron group than in aprepitant plus ramosetron group for 24 hours after surgery (P<0.05, respectively). There was no difference in pain severity and side effects including headache and drowsiness. Aprepitant plus palonosetron significantly prevents PONV, compared with aprepitant plus ramosetron in patients at high risk for PONV after laparoscopic cholecystectomy.