Leuprolide 

Trade names:  Eligard ^TM, Lupron^®, Lupron Depot^®, Viadur^TM 

Generic name:   Leuprolide  

Other names: Leuprorelin Acetate  

Therapeutic Class: LHRH agonist (hormone therapy) 

Manufacturer / Distributor: Astellas Pharma 

Availability: Leuprolide is available by prescription only  

Dosage form: Leuprolide is given by subcutaneous (under the skin) injection  

Indications: Leuprolide is used to treat the following medical conditions: 

• prostate cancer  
• breast cancer 
• ovarian cancer 
• endometrial cancer
• endometriosis 
• infertility  
• Benign prostatic hypertrophy [(BPH), a non cancerous prostate disease].  

Leuprolide can also be used to treat other medical conditions that are not mentioned in this article; talk to your doctor or pharmacist for more information.  

Dosage: to prescribe you an appropriate dosage, your oncologist will consider your health in general, other drugs you are taking, the characteristic of the cancer (aggressive or not), and especially your body surface area (BSA). Recommended doses of Leuprolide vary greatly depending to these criteria and the response of your body to the drug.  

In general, Leuprolide is given by injection under the skin. You may be recommended to take the drug once a month or once of every 3, 4 or 6 months. In some cases, your doctor may indicate another dosage. Whatever the dosage prescribed, it is important to follow and complete the treatment as recommended by your doctor. It is also necessary to respect the time interval required between the doses. If for some unavoidable reasons you cannot take the medication at the appointed time, call your doctor as soon as you can. However, the best thing is to take Leuprolide as prescribed.   

Your oncologist may do an implant under your skin to inject the drug. If so, keep the area where you received the implant clean and dry for 24 hours; therefore, swimming and/or bathing is not recommended during 24 hours after an Leuprolide injection. You may also need to cover the area with a bandage until the wound heals.  

Storage: The vials or kits of Leuprolide should be refrigerated at a temperature between 2 ° C and 8 ° C, and protected from light. Do not let the drug at the children reach. After opening, powder and solvent for the solution must be reconstituted and administered immediately. The physicochemical stability of the reconstituted solution last about 30 minutes at 25 ° C.  

Overdose: Leuprolide overdose is very rare, in fact, no cases of misuse or overdose has been reported in clinical practice. However, if overdose occurs, medical attention is very important. In some cases, symptomatic treatment can be recommended.  

Missing dose: if for some reasons you forget a dose or cannot be present at the hospital for the treatment, contact your oncologist before the date of the appointment. In fact, this case is rarely reported. 

Contraindications : Leuprolide is contraindicated, or should be used with precaution in the following conditions:  

• allergy to Leuprolide  or any of its ingredients 
• allergy to other GnRH agonists 
• patient having a history of orchiectomy, removal of one or the two testicles  
• As monochemotherapy for patients with prostate cancer associated with bone metastases or spinal cord compression.  

Mechanism of action (MOA): Your body produces a group of cells called gonadotropes. Located in the pituitary glands (hypophysis), those cells produce the gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH). FSH and LH are controlled by gonadotropin-releasing hormone (GnRH), another hormone produced and controlled by the hypothalamus. Certain cancer cells such as those of prostate and breast cancers need those hormones to survive.  Leuprolide works by inhibiting the secretion of gonadotropes.  

Interactions: no p harmacokinetic studies of drug interactions with Leuprolide have been shown. However, for preventive measures, before starting a treatment with Leuprolide , tell your doctor about all prescription and nonprescription medications you are taking; the list include but not limited to aspirin, vitamins supplements, and the following dugs:  

• dexamethasone (Decadron, Dexone) 
• methylprednisolone (Medrol) 
• Prednisone (Deltasone) 
• Lanthanum carbonate (Fosrenol); 
• Phenothiazine 
• Sevelamer (Renagel) 
• Cyclosporine (Neoral, Restasis, Sandimmune) 
• Diuretics ('water pills').   

Side effects: attacking cancer cells,Leuprolide also affects normal (healthy) cells, which lead to, in certain patients, the following side effects:       

• hot flashes 
• hair loss 
• fatigue  
• headache 
• nausea and vomiting  
• decreased appetite 
• bowel disorder (diarrhea or constipation)
• weight loss  
• anxiety or nervousness
• memory and concentration problems 
• drying or darkening of the skin or nails 
• sensitivity of skin to sunlight 
• tingling in the hands or feet 
• increased need to urinate, especially at night 
• breast tenderness or change in breast size (both men and women) 
• incapacity or decrease in sexual desire in men and women
• decrease in size of testicles 
• vaginal discharge, dryness, or itching (women) 
• absence of menstrual periods (women) 
• Firmness or hardness at subcutaneous injection spot. 

If the side effects above become severe or persist for weeks, contact your oncologist. In addition, contact your doctor immediately if you experience any of these symptoms:  

• fever 
• chills 
• bone pain  
• persistent cough  
• testicular or prostate pain 
• inability to move arms or legs 
• painful or difficult urination 
• painful urination or red urine 
• unusual bruising or bleeding 
• swelling of the feet or legs 
• numbness, tingling, weakness, or pain in the feet or lower legs 
• Yellowing of the skin or eyes.  

References: 

1 - vidalpro.net, LEUPROLIDE ^® 45 mg – leuproréline 

2 - santecheznous.com 

3 - nlm.nih.gov