Palzen0.5 mg

Palzen 0.5 mg is indicated for the prevention and management of the following conditions:

• Acute and delayed nausea and vomiting
• Uncontrolled nausea and vomiting
• Chemotherapy-induced nausea and vomiting (CINV) — including acute CINV occurring on the day of treatment with certain types of chemotherapy
• Delayed CINV occurring in the days following treatment with certain types of chemotherapy
• Radiotherapy-induced nausea and vomiting (RINV)
• Post-operative and post-discharge nausea and vomiting (PONV & PDNV)

* Always take this medicine according to the advice of a registered physician.

Palzen 0.5 mg belongs to the therapeutic class of Anti-emetic drugs (5-HT3 receptor antagonists).

Palzen 0.5 mg is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors. Chemotherapeutic agents are believed to produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine. The released serotonin then activates 5-HT3 receptors located on the vagal nerve terminals in the periphery and centrally in the chemoreceptor trigger zone of the area postrema, initiating the vomiting reflex.

Post-operative nausea and vomiting is influenced by multiple patient, surgical, and anesthesia-related factors, and is triggered by the release of 5-HT3 in a cascade of neuronal events involving both the central nervous system and the gastrointestinal tract. The 5-HT3 receptor has been shown to selectively participate in the emetic response. Palzen 0.5 mg works by blocking the action of serotonin at the 5-HT3 receptor, thereby preventing the signals that trigger nausea and vomiting. It is likely that Palzen 0.5 mg acts primarily in the small intestine, though it may also exert effects in the brain.

Pharmacokinetics

Palzen 0.5 mg exhibits linear, dose-proportional pharmacokinetics over the dose range of 1–90 mcg/kg in both healthy subjects and cancer patients. In cancer patients receiving single intravenous doses within this range, the mean maximum plasma concentration (C_max) ranges from 0.89 to 3.36 ng/mL, and the area under the plasma concentration-time curve (AUC_0-∞) ranges from 13.8 to 957 ng·h/mL.

Key pharmacokinetic properties include:

• Volume of distribution: approximately 6.9–7.9 L/kg
• Plasma protein binding: approximately 62%
• Metabolism: around 50% is metabolized into two inactive metabolites (each with <1% of the 5-HT3 antagonist activity), primarily via hepatic CYP2D6, with contributions from CYP3A4 and CYP1A2
• Excretion: approximately 40% of the drug is excreted unchanged in the urine within 144 hours after a single IV dose
• Total body clearance: 160 ± 35 mL/h/kg; renal clearance 66.5 ± 18.2 mL/h/kg in healthy subjects
• Half-life: approximately 40 hours — notably longer than earlier 5-HT3 antagonists

In controlled clinical trials, Palzen 0.5 mg injection has been safely co-administered with corticosteroids, analgesics, antiemetics/antinauseants, antispasmodics, and anticholinergic agents. Palzen 0.5 mg did not inhibit the antitumor activity of cisplatin, cyclophosphamide, cytarabine, doxorubicin, or mitomycin C in murine tumor models.

Concomitant administration of Palzen 0.5 mg and metoclopramide produces no significant pharmacokinetic interactions. In vitro studies indicate that Palzen 0.5 mg is neither an inhibitor of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, CYP2E1, or CYP3A4/5 (CYP2C19 was not investigated), nor an inducer of CYP1A2, CYP2D6, or CYP3A4/5. As a result, the potential for clinically significant drug interactions with Palzen 0.5 mg appears to be low.

Palzen 0.5 mg is generally well tolerated. The most commonly reported adverse reactions are:

• Headache
• Constipation

If any side effect persists or worsens, or if signs of an allergic reaction appear, patients should consult a registered physician promptly.

Pregnancy Category B. Palzen 0.5 mg should be used during pregnancy only if clearly needed and under the guidance of a physician. It is not known whether Palzen 0.5 mg is excreted in human breast milk. Because many drugs are excreted in breast milk, caution should be exercised when administering Palzen 0.5 mg to a nursing mother.

For IV administration only. Not for intradermal, subcutaneous, or IM administration. Do not administer if particulate matter, cloudiness, or discoloration is noted. Discard any unused solution. Do not save unused solution for later administration. Do not mix with other medications.

There is no known antidote to Palzen 0.5 mg. In the event of an overdose, treatment should focus on supportive care and management of symptoms as they arise. Patients suspected of overdose should be monitored by a healthcare professional.

Store in a cool and dry place, protected from light. Keep all medicines out of the reach of children.

Intravenous: Nausea and vomiting associated with cancer chemotherapy: Physically and chemically stable at concentrations of 5 and 30 mcg/ml in glucose 5%, sodium chloride 0.9%, glucose 5% in lactated Ringer's for at least 48 hr at room temperature, exposed to light and for 14 days under refridgeration.

Anti-emetic drugs

Palzen 0.5 mg is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine and that the released serotonin then activates 5-HT3 receptors that are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema, to initiate the vomiting reflex. Postoperative nausea and vomiting is influenced by multiple patient, surgical and anesthesia related factorcs and is triggered by release of 5-HT3 in a cascade of neuronal event involving both the central nervous system and the gastrointestinal tract. The 5-HT3 receptor has been demonstrated to selectively participate in the emetic response. Palzen 0.5 mg works by blocking the actions of Serotonin, associated with nausea and vomiting, at 5-HTs receptor. It is likely that Palzen 0.5 mg works in the small intestine but it may also work in the brain.Pharmacokinetics: Palzen 0.5 mg exhibits linear dose-proportional pharmacokinetics over the doserange 1-90 pg/kg in healthy subjects and in patients with cancer. In cancer patients receiving single intravenous doses of Palzen 0.5 mg in this dose range, the mean maximum plasma concentration (Cmax) ranges from 0.89 to 336 ng/ml and the area under the plasma concentration-time curve from zero to infinity (AUCo-co) ranges from 13.8 to 957 ng.h/ml. Palzen 0.5 mg has a volume of distribution of approximately 6.9-7.9 L/kg, with approximately 62% bound to plasma proteins. Approximately 50% of Palzen 0.5 mg is metabolized into two inactive metabolites that exhibit <1% of the 5-HT3 receptor antagonist activity. Approximately 40% of the drug is metabolised via kidney, 50% by liver CYP2D6 (mainly), CYP3A4 and CYP1A2 isoenzymes. About 50% of the drug goes under metabolism. After a single intravenous dose, approximately 40% is excreted as unchanged drug in the urine after 144 hours. Total body clearance of Palzen 0.5 mg is 160±35 ml/h/kg, and renal clearance is 66.5±18.2 ml/h/kg in healthy subjects. Palzen 0.5 mg exhibits a longer half-life (40 hours) and has a greater 5-HT3 receptor binding affinity.

Pregnancy category 'B'. It is not known whether Palzen 0.5 mg is excreted in breast milk.

Use in elderly patients: No dosage adjustment is recommended in elderly patients >65 years of age.Use in Children: (1 month to 10 years): A single IV dose at 20 mcg/kg body weight. Which maximum dose is 1.5 mg.Use in patients with impaired renal and hepatic function: No dosage adjustment is recommended in patients with renal and hepatic dysfunction.