5-HT3 Receptor Antagonists include-
Alosetron, Dolasetron, Ondansetron, Palonosetron, Granisetron, Hydrolastron

Refer - 5-HT3 Receptor Antagonists

Since  palosetron  does not induce or inhibit CYP enzymes, potential for drug interactions are low.
Palmosetron stability not affected by concomittant use of most of chemotherapy agents.

Prevention of Nausea/Vomiting associated with chemotheraphy

Adverse reactions-

Cardiovascular - Bradycardia, hypotension, sustained tachcardia, (1% )
                              extrasustoles,  hypertension,  myocardial ischemia,
                              sinus arrhythmia,   sinus tachycardia,
                              supraventricular extrasystoles   and QT prolongation,
                              vein discoloration, vein distention ( < 1% )

CNS -                    Anxiety,   dizziness ( 1% )  , euphoric mood, fatigue, hypersomnia,
                              insomnia,  paresthesia, somnolence ( < 1% )

Dermatologic-     Allergic dermatis,  rash ( less than 1% )

GI -                       Diarrhea ( 1% )  abdominal pain , dry  mouth, dyspepsia,
                             flatulance, hiccups (< 1% )

GU-                      urinary distention, ( < 1% )

Hepatic -            transcient asymptomatic increases in AST and bilirubin  < 1%

 Ophthalmic-        Amblyopia, eye irritation, < 1%

Musculoskeletal - Arhralgia ( <1% )

Miscellaneous -   weakness 1%,  fever, flu-like syndrome, hot flush, motion sickness,
                              tinnitus, (<1% )

 
Most common adverse reactions are headache, constipation, dizziness, and diarrhea

5-HT3 Receptor Antagonists include-
Alosetron, Dolasetron, Ondansetron, Palonosetron, Granisetron, Hydrolastron

Refer - 5-HT3 Receptor Antagonists

Pregnancy and lactation

Date of Approval       2009

Indication-

Prevention of Nausea/Vomiting associated with chemotherapy

Dosage- Injection-

10mcg/kg administered intravenously (IV ) within 30 minutes before intiation of chemotherapy
and only on days chemotherapy is given
Used as 0.25 mg and 0.75mg intravenously.

Administer 0.25mg by single i.v.bolus injection over over 30 seconds
approximately 30 minutes  prior to chemotherapy

Not recommended for patients under 18 years of age

Dosage - oral-
2mg once daily ( 1 hour before chemotherapy ) or 1mg twice daily ( give the first 1mg dose
upto 1 hour before chemotherapy  and second 1mg  dose 12 hours after the first dose.
Either regimen is administered only on the days chemotherapy is given

. 

5-HT3 Receptor Antagonists include-
Alosetron, Dolasetron, Ondansetron, Palonosetron, Granisetron, Hydrolastron

Refer - 5-HT3 Receptor Antogonists

Pharmacology

- Palonosetron is a highly potent selective second generation 5-HT receptor antgonist that has a strong receptor binding affinity,e which is 100 fold higher than other 5-HT3 receptor antagonists. Patonosetron blocks the 5-HT receptor present in CTZ( chemorecptor trigger zone )/NTS ( neucleus tractus soltari ) so the impulses from the GI tract do not reach to the vomiting center. CTZ and NTS have direct input to the vomiting center and receive input from the various receptors in the body, they specifically receive vagally mediated input from the GI tract

Pharmacokietics-

After admin of radiolabelled palonosetron it accounted for 72% of total radioactivity in plasma over 95h with a mean plasma level elimnation half life of 37hr. Over 80% of administered palonosetron was recovered within 144hr and total 40% of this dose was recovered as parent palonoseton

5-HT3 Receptor Antagonists include-
Alosetron, Dolasetron, Ondansetron, Palonosetron, Granisetron, Hydrolastron

Refer - 5-HT3 Receptor Antagonists

5-HT3 Receptor Antagonists include-
Alosetron, Dolasetron, Ondansetron, Palonosetron, Granisetron, Hydrolastron

Refer - 5-HT3 Receptor Antagonists