vinorelbine

Action and Spectrum

Mechanism of action 

Vinca alkaloids are a class of drugs that inhibit cell division by binding to and destabilizing microtubules, which are important structural components of cells. This leads to the inhibition of mitosis at the metaphase stage, and blocks the use of glutamic acid, leading to inhibition of nucleic acid and protein synthesis. These drugs are typically used to treat cancer, as they specifically target cells that are rapidly dividing. 

Spectrum 

It is a semi-synthetic vinca alkaloid used to treat various types of cancer, including non-small cell lung cancer, breast cancer, and ovarian cancer. It works by inhibiting cell division by binding to and destabilizing microtubules, leading to mitosis inhibition. Vinorelbine has a broad spectrum of activity, which can be effective against a wide range of cancer types. However, it is most used to treat non-small cell lung cancer and breast cancer. It is usually administered intravenously and can be given as a single agent or combined with other chemotherapy drugs. 

Drug Interaction

Adverse Reaction

Frequency defined:  

>10% 

Granulocytopenia 

Elevated AST 

Asthenia 

Fatigue 

Vomiting 

Stomatitis 

Leukopenia 

Anemia 

Nausea 

Constipation 

Peripheral neuropathy 

Anorexia 

Alopecia 

1-10% 

Chest pain 

SOB 

Dyspnea 

Rash 

Hemorrhagic cystitis 

Post-marketing reports 

Hepatic toxicity 

Pulmonary toxicity 

Bowel obstruction 

Respiratory failures 

Black Box Warning

Black box warning 

It can cause severe neurotoxicity, which is damage to the nerves. Symptoms of neurotoxicity can include numbness, tingling, burning or weakness in the hands and feet, difficulty with coordination and balance, and muscle weakness. These symptoms can be severe and long-lasting and, in some cases, can lead to permanent nerve damage. 

Contraindication / Caution

Contraindications 

None 

Caution 

It is a chemotherapy drug that may cause some serious side effects. Patients should be closely monitored for toxicity by a healthcare professional experienced in chemotherapy. 

Patients should be informed of the risk of severe neurotoxicity, as vinorelbine may cause damage to the nerves, which can lead to symptoms such as numbness, tingling, burning or weakness in the hands and feet, difficulty with coordination and balance, and muscle weakness. 

Other side effects may include decreased white blood cells and platelets, leading to an increased risk of infections and bleeding. Nausea, vomiting, hair loss, and anemia are also commonly reported. 

Patients should report any side effects to the healthcare professional immediately. Patients should also inform their healthcare professionals if they are pregnant or breastfeeding, as vinorelbine may cause harm to the fetus or baby. 

Pregnancy / Lactation

Pregnancy consideration: May cause fetal harm 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

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 available 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 

It has a mechanism of action like other vinca alkaloids, such as vincristine and vinblastine. These drugs bind to the tubulin protein, a component of microtubules, and prevent the formation of new microtubules. This leads to the destruction of rapidly dividing cancer cells. 

It is selectively toxic to dividing cells, which is why it has been mainly used in the treatment of solid tumors such as breast cancer and non-small cell lung cancer. 

Pharmacodynamics 

It works by binding to the beta-tubulin subunit of microtubules and preventing their polymerization; this interferes with the mitotic spindle formation and cell division and ultimately leads to apoptosis or programmed cell death. 

It selectively targets cancer cells because they have a higher rate of cell division than normal cells. This makes it a helpful chemotherapy drug for treating certain types of cancer, such as lung and breast cancer. 

Pharmacokinetics 

Absorption: It is administered intravenously, so it is not absorbed through the gut. It is rapidly and almost completely metabolized by the liver. As the drug is administered intravenously, bioavailability is 100%.  

Distribution: It distributes throughout the body but tends to accumulate in the liver, spleen, and bone marrow. The drug is also known to cross the blood-brain barrier, which means it can reach the brain and spinal cord. The volume of distribution of vinorelbine is estimated to be around 3.2 L/kg. 

Metabolism: It is rapidly and almost completely metabolized by the liver. The active metabolites formed are vinblastine, vincristine, and vinorelbine-N-oxide.  

Elimination and excretion: It have a relatively short half-life in the body, between 2 and 4 hours. It is eliminated primarily through the kidneys. The clearance of vinorelbine is estimated to be around 41-112 mL/min. 

Adminstartion

Administration 

• It is administered intravenously (IV) in a hospital or clinic. The drug is usually given once a week; the dosage depends on the type and stage of cancer and the patient’s overall health. 
• The usual dose for adult patients is 30 mg/m2, given over 10-15 minutes once a week. The treatment is usually given for 6 to 8 cycles or until the disease progresses. 
• It is important to note that the drug should be administered only by a healthcare professional experienced in cancer chemotherapy. The healthcare professional will also closely monitor the patient during and after the administration of the drug, as vinorelbine can cause side effects such as fatigue, nausea, and a decrease in white blood cells, which can increase the risk of infection. 
• Patients should also be well hydrated before receiving vinorelbine; this can help prevent the formation of kidney stones. Suppose the patient develops a fever or chills during or after the administration of the drug. In that case, they should inform the healthcare professional immediately, as this may signify an infusion reaction. 
• It is also essential to follow the treatment schedule prescribed by the healthcare professional and not miss any doses. If a dose is missed, the patient should contact their healthcare professional for instructions on how to proceed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: vinorelbine 

Pronounced: [ vin-OR-el-been] 

Why do we use vinorelbine? 

It is a chemotherapy drug that is used to treat certain types of cancer, including: 

• Non-small cell lung cancer (NSCLC) is often used with other chemotherapy drugs to treat advanced or metastatic NSCLC. It can also be used as a second-line treatment after the failure of other chemotherapy regimens. 
• Breast cancer is used to treat advanced or metastatic breast cancer, especially in women who have failed other chemotherapy regimens. It is also used with other drugs to treat early-stage breast cancer. 

• Head and neck cancer: Vinorelbine is used with other chemotherapy drugs to treat advanced head and neck cancer. 

• Esophageal cancer: Vinorelbine is used with other chemotherapy drugs to treat advanced esophageal cancer. 

• Other solid tumors: Vinorelbine has also been used to treat other solid tumors such as ovarian, prostate, and bladder cancer.