Abstract

Background:
Nausea and vomiting are the upsetting side effects of chemotherapy and adversely affects the health-oriented quality of life in cancer patients and its side effects are not well managed up till now especially nausea. Chemotherapeutic agents such as Cisplatin exhibit various stressful side effects including nausea & vomiting, but still more research work is needed to fully explore the side effects of anticancer agents. Chemotherapeutic drugs used to treat cancer caused nausea and vomiting in 80% of the people. The occurrence of nausea and vomiting reduced the oral ingestion of fluid and foods by initiating the loss of appetite. The oncologists use international guidelines to manage CINV properly but still they are failed.

Aim:
To investigate the antiemetic potential of gabapentinoids (Pregsal & Gabapentsal) derivatives against emetogenic.

Methods:
Pigeons of specific weight range were used for vomiting studies. Their vomiting behavior was recorded up to 03 hr. Vomiting was induced by Cisplatin (7 mg/kg IV), CuSO4 & Ipecac. CuSO4 and ipecac were delivered orally, and the response with or without oral ejection was deemed one emetic episode. Preparations of rabbit jejunum were allowed to be stabilized in Tyrode's solution to investigate the calcium ion channel blocking activity of the compound.

Results:
The gabapentinoids derivatives have analgesic, anxiolytic and anticonvulsant and used in management of neuropathic pain. These effects of Gabapentin & Pregabalin are reported to be intervened by inhibitory effects on neuropeptide “Substance P” and Immunoreactive peptides. It is therefore stated that Gabapentin & Pregabalin interact with the α2δ subunit of the calcium channels & modulate the release of neurotransmitters implicated in the mechanisms of neuropathy. Gabapentinoids derivatives are hypothesized to have antiemetic effects for inhibition of neuropeptides and neurotransmitters involved in the act of vomiting.

Conclusion:
The antiemetic activity of Pregsal and Gabapentsal against emetogenic as well as inhibition of Ca ions channels leading to antiemetic response against various emetogenic along with studied possible mechanism of action in pigeons provide future direction for the test compounds to be screened in human for the better management of CINV in clinics.

Key words: Emesis; Pigeon; Cisplatin; CuSO4; Ipecac.