Cetrorelix
Cetrorelix Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Cetrorelix is a brand name. Its generic name is Cetrorelix.
Cetrorelix Introduction
Cetrorelix is a synthetic peptide agonist of gonadotropin-releasing hormone (GnRH) used as a hormonal anti-cancer therapy and for the treatment of endometriosis. It was approved by the US Food and Drug Administration (FDA) in 2003. Cetrorelix is a member of a class of drugs called GnRH agonists, which are used to treat a variety of conditions, including infertility, endometriosis, and certain types of cancer.
Uses for Cetrorelix
Cetrorelix is indicated for:
- Prostate cancer treatment
- Endometriosis
- Polycystic Ovarian Syndrome (PCOS)
Mechanism of Action
Cetrorelix binds to GnRH receptors in the pituitary gland and blocks the production of luteinizing hormone (LH) and follicle stimulating hormone (FSH). This reduces the production of testosterone and estradiol, leading to decreases in growth of hormone-dependent tumors and relieving symptoms of endometriosis.
How Long Does it Take to Work?
The effects of Cetrorelix usually begin within 24-48 hours after using it and last for up to a month.
Absorption
Cetrorelix has minimal systemic absorption after subcutaneous injection and is mostly metabolized in the liver by cytochrome P450 enzymes.
Route of Elimination
Cetrorelix is primarily metabolized in the liver by cytochrome P450 enzymes and is then eliminated through the feces as metabolites.
Dosage
The recommended dose of Cetrorelix for treating endometriosis and prostate cancer is 0.25 mg as a single subcutaneous injection. For patients with polycystic ovarian syndrome, the recommended dose is 0.25 mg given in two divided doses.
Administration
Cetrorelix should be administered as a single subcutaneous injection once daily, one to two hours before or after meals.
Side Effects
Common side effects of Cetrorelix include:
- Hot flashes
- Vaginal dryness
- Decrease in sex drive
- Headache
- Nausea
- Diarrhea
Toxicity
Cetrorelix has an LD50 (lethal doses) of >5000 mg/kg in rats. There have been no reported cases of toxicity from Cetrorelix in humans.
Precautions
It is important to tell your doctor if you are pregnant, breastfeeding, or have liver or kidney disease before starting Cetrorelix. Cetrorelix is not recommended for use in people younger than 18 years of age.
Interactions
Cetrorelix may interact with certain medications, such as birth control pills, hormone replacement therapy, antacids, and calcium channel blockers. It is important to tell your doctor about all medications you are taking.
Disease Interactions
Cetrorelix may interact with certain diseases, such as thyrotoxicosis, hypertension, and diabetes mellitus. It is important to tell your doctor about any chronic diseases you may have.
Drug Interactions
Cetrorelix may interact with certain drugs, such as antidepressants, antiepileptic drugs, and lithium. It is important to tell your doctor about all medications you are taking.
Food Interactions
Cetrorelix may interact with certain foods. It is important to tell your doctor about all foods, including supplements, that you are consuming.
Pregnancy Use
Cetrorelix should not be used during pregnancy as it may cause birth defects.
Lactation Use
Cetrorelix should not be used during lactation as it passes through breast milk and may cause adverse effects in the infant.
Acute Overdose
In case of an acute overdose, contact your healthcare provider or poison control center immediately.
Contraindication
Cetrorelix is contraindicated in patients with hypersensitivity to GnRH agonists, or any of the components of the product.
Use Directions
Cetrorelix should be administered as a single subcutaneous injection once daily, one to two hours before or after meals.
Storage Conditions
Cetrorelix should be stored at room temperature away from direct light and moisture.
Volume of Distribution
The volume of distribution of Cetrorelix is approximately 2 L/kg.
Half-Life
The half-life of Cetrorelix is approximately 3-4 hours.
Clearance
The clearance of Cetrorelix is approximately 0.7 L/h/kg.
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