Action and Spectrum

Actions and Spectrum: 

Action: netupitant’s primary action is as an antagonist of the neurokinin-1 (NK-1) receptor. The NK-1 receptor is part of the tachykinin receptor family and is involved in transmitting signals of substance P, a neuropeptide involved in various physiological processes, including nausea and vomiting. 

Spectrum: netupitant has demonstrated impressive effect in preventing both acute and delayed chemotherapy-induced nausea and vomiting associated with highly emetogenic (likely to cause vomiting) and moderately emetogenic chemotherapy protocols.By targeting the NK-1 receptor, netupitant enhances the antiemetic (anti-vomiting) effects of palonosetron, a serotonin 5-HT3 receptor antagonist. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Erythema (skin redness) 

Constipation 

Fatigue 

Indigestion 

Weakness 

Headache 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: netupitant should not be used in individuals with a known allergy or hypersensitivity to the active ingredient or any of the other components of the medication. 

Use with pimozide or thioridazine: netupitant may interact with these medications and cause potentially serious adverse effects. Therefore, it is essential to avoid co-administration. 

Severe hepatic impairment: Patients with severe liver problems may have difficulty metabolizing the drug, The possibility of elevated drug concentrations in the system and the potential for adverse reactions may arise consequently. 

Use with strong CYP3A4 inducers: netupitant is metabolized by the enzyme CYP3A4. Co-administration with strong CYP3A4 inducers may reduce the effectiveness of netupitant. 

Pregnancy and breastfeeding: The safety of netupitant has not undergone sufficient investigation concerning its effects during pregnancy and breastfeeding. As a result, it is generally not advisable for use in pregnant or breastfeeding women unless the potential benefits are deemed to outweigh the associated risks. 

Use in children: The safety and efficacy of netupitant in children have not been established, so its use in pediatric populations may not be recommended. 

Use with certain medications: netupitant may interact with other medications, including those that are metabolized by CYP3A4, and result in potential drug interactions. Therefore, ensuring that you disclose all the medications you are currently using to your healthcare provider is of utmost importance prior to initiating netupitant treatment. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

netupitant is a substance used in combination with palonosetron as an antiemetic drug. It aims to alleviate nausea and vomiting that often accompanies chemotherapy treatment. 

Pharmacodynamics:  

netupitant is a selective antagonist of the neurokinin-1 (NK-1) receptor. The NK-1 receptor is located within the brain and plays a crucial role in transmitting signals responsible for inducing feelings of nausea and triggering the vomiting reflex. By blocking this receptor, netupitant helps to inhibit the emetic (vomiting) response triggered by certain chemicals in the body, particularly substance P.   

Pharmacokinetics: 

Absorption 

netupitant is absorbed from the gastrointestinal tract and enters the bloodstream. 

Distribution 

Once in the bloodstream, netupitant is distributed throughout the body. It may bind to plasma proteins, such as albumin. The drug can cross the blood-brain barrier, allowing it to exert its effects in the brain, where it acts as a neurokinin-1 (NK1) receptor antagonist to prevent nausea and vomiting. 

Metabolism 

netupitant undergoes metabolism primarily in the liver, mainly through the cytochrome P450 (CYP) enzyme system. The main metabolite is hydroxylated netupitant, which is further metabolized through glucuronidation.  

Excretion and Elimination 

After metabolism, netupitant and its metabolites are eliminated from the body mainly through the feces and, to a smaller extent, in the urine. The elimination half-life of netupitant is around 90 to 120 hours, indicating a relatively long duration of action. 

Adminstartion

Administration:  

• netupitant is usually taken orally in the form of a capsule, which should be swallowed whole with a glass of water. 
• The capsule can be taken with or without food, as directed by the healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: netupitant 

Why do we use netupitant?  

Chemotherapy-induced nausea and vomiting (CINV): netupitant is commonly prescribed to cancer patients undergoing chemotherapy to reduce the likelihood of experiencing nausea and vomiting as side effects. 

Radiation-induced nausea and vomiting (RINV): It may also be used in patients receiving radiation therapy, particularly when the radiation field includes the abdomen or other sensitive areas that can trigger nausea and vomiting. 

Post-operative nausea and vomiting (PONV): netupitant can be used in some cases to prevent nausea and vomiting after surgery.