Pharmacokinetics Of Leuprorelin Depot
Because it is a peptide, leuprorelin is not active when given orally and is usually administered through a subcutaneous or intramuscular route.
Pharmacokinetic studies showed that mean peak plasma leuprorelin concentrations were 13.1, 21.8, 47.4, 54.5 and 53 g/L after injection of 3.75, 7.5, 11.25, 15, and 30 mg depot formulations, respectively, and occurred within 1 to 3 hours of administration. After subcutaneous injection of 1 mg of a non-depot formulation, mean Cmax was 35 g/L and occurred 36 to 60 minutes after injection.39 Following injection of 45 mg 6-month depot formulation, there was an early rise in Cmax to 82.0 ng/mL 4.5 hours after the initial administration. On the second injection, 6 months after the initial treatment, mean Cmax was 102 ng/mL and occurred 4.5 hours after the second injection. After these initial increases, mean serum levels remained constant within the 0.2 to 2 ng/mL range.37
The mean volume of distribution of leuprolide after bolus administration in a group of healthy male volunteers was 27 L.39 After a single subcutaneous injection of 1 mg, 3.75 mg, 7.5 mg, or 15 mg leuprorelin, the mean volumes of distribution were 36 L, 33 L, and 27 L, respectively.
Total body clearance and elimination half-life were 9.1 L/hour and 3.6 hours, respectively, after a 1 mg subcutaneous administration. After intravenous bolus, these values were 8.3 L/hour and 2.9 hours, respectively.33
How Should This Medicine Be Used
Leuprolide injection comes as a long-acting suspension that is injected intramuscularly by a doctor or nurse in a medical office or clinic and is usually given once a month or every 3, 4, or 6 months . Leuprolide injection also comes as a long-acting suspension that is injected subcutaneously by a doctor or nurse in a medical office or clinic and is usually given every 1, 3, 4, or 6 months. Leuprolide injection also comes as a long-acting suspension that is injected subcutaneously by a doctor or nurse in a medical office or clinic and is usually given every 6 months. Your doctor will tell you how long your treatment with leuprolide injection will last. When used in children with precocious puberty, leuprolide injection will likely be stopped by your childs doctor before 11 years of age in girls and 12 years of age in boys.
If you receive leuprolide long-acting suspension as a subcutaneous injection, you may notice a small bump at the place where the injection was given when you first receive the medication. This bump should eventually go away.
Leuprolide may cause an increase in certain hormones in the first few weeks after injection. Your doctor will monitor you carefully for any new or worsening symptoms during this time.
Ask your pharmacist or doctor for a copy of the manufacturers information for the patient.
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Lupron Depot 45 Mg For 6
The recommended dose of LUPRON DEPOT 45 mg for 6-month administration is one injection every 24 weeks. Do not use concurrently a fractional dose, or a combination of doses of this or any depot formulation due to different release characteristics.
Incorporated in a depot formulation, the lyophilized microspheres must be reconstituted and should be administered every 24 weeks as a single intramuscular injection.
For optimal performance of the prefilled dual chamber syringe , read and follow the instructions in Section 2.5.
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Reconstitution And Administration For Injection Of Lupron Depot
- Reconstitute and administer the lyophilized microspheres as a single intramuscular injection.
- Inject the suspension immediately or discard if not used within two hours, because LUPRON DEPOT does not contain a preservative.
1. Visually inspect the LUPRON DEPOT powder. DO NOT USE the syringe if clumping or caking is evident. A thin layer of powder on the wall of the syringe is considered normal prior to mixing with the diluent. The diluent should appear clear and colorless.
2. To prepare for injection, screw the white plunger into the end stopper until the stopper begins to turn .
Figure 1
Figure 2
3. Hold the syringe UPRIGHT. Release the diluent by SLOWLY PUSHING the plunger until the first middle stopper is at the blue line in the middle of the barrel .
Figure 3
4. Keep the syringe UPRIGHT. Mix the microspheres thoroughly by gently shaking the syringe until the powder forms a uniform suspension. The suspension will appear milky. If the powder adheres to the stopper or caking/clumping is present, tap the syringe with your finger to disperse. DO NOT USE if any of the powder has not gone into suspension .
Figure 4
5. Keep the syringe UPRIGHT. With the opposite hand pull the needle cap upward without twisting.
6. Keep the syringe UPRIGHT. Advance the plunger to expel the air from the syringe. Now the syringe is ready for injection.
Figure 5
Figure 6
8. Inject the entire contents of the syringe intramuscularly.
Figure 7
Systemic Therapy For Metastatic Disease
The most common use of hormone therapy today is to treat men whose prostate cancer has metastasized to other parts of the body. If prostate cancer cells escape the prostate, they migrate first to surrounding structures, such as the seminal vesicles and lymph nodes, and later to the bones or, rarely, to other soft tissues.
Hormone therapy is recommended as a palliative treatment, to relieve symptoms such as bone pain. And while hormone therapy is not a cure, in that it cant eliminate prostate cancer completely, it often extends life for many years. By reducing testosterone levels, hormone therapy can shrink a prostate tumor and its metastases and slow further progression of the cancer for so long that sometimes a man with this disease dies of something other than prostate cancer.
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Combined Androgen Blockade: Pro And Con
Pro:
Crawford ED, Eisenberger MA, McLeod DG, et al. A Controlled Trial of Leuprolide With and Without Flutamide in Prostatic Carcinoma. New England Journal of Medicine 1989 321:41924. PMID: 2503724.
Con:
Eisenberger MA, Blumenstein BA, Crawford ED, et al. Bilateral Orchiectomy With or Without Flutamide for Metastatic Prostate Cancer. New England Journal of Medicine 1998 339:103642. PMID: 9761805.
Two large meta-analyses that reviewed many studies comparing combined androgen blockade to monotherapy concluded that the combination offered only a small survival advantage and even that finding was inconsistent between the two analyses. One analysis, which reviewed 27 randomized studies involving 8,275 men, estimated that combined androgen blockade improved five-year survival by only 2% to 3%, at most. However, an advantage of only 2% to 3%, when applied to thousands of men undergoing treatment, translates into hundreds of lives extended obviously an important benefit to the men who gain months and even years of life as a result. That is why I use combined therapy for all of my patients who undergo hormone treatments.
Lupron Depot 225 Mg For 3
The recommended dose of LUPRON DEPOT 22.5 mg for 3-month administration is one injection every 12 weeks. Do not use concurrently a fractional dose, or a combination of doses of this or any depot formulation due to different release characteristics.
Incorporated in a depot formulation, the lyophilized microspheres must be reconstituted and should be administered every 12 weeks as a single intramuscular injection.
For optimal performance of the prefilled dual chamber syringe , read and follow the instructions in Section 2.5.
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What Is Intermittent Adt
Researchers have investigated whether a technique called intermittent androgen deprivation can delay the development of hormone resistance. With intermittent androgen deprivation, hormone therapy is given in cycles with breaks between drug administrations, rather than continuously. An additional potential benefit of this approach is that the temporary break from the side effects of hormone therapy may improve a mans quality of life.
Randomized clinical trials have shown similar overall survival with continuous ADT or intermittent ADT among men with metastatic or recurrent prostate cancer, with a reduction in some side effects for intermittent ADT .
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Treatment By Stage Of Prostate Cancer
Different treatments may be recommended for each stage of prostate cancer. Your doctor will work with you to develop a specific treatment plan based on the cancers stage and other factors. Detailed descriptions of each type of treatment are provided earlier on this same page. Clinical trials may also be a treatment option for each stage.
Early-stage prostate cancer
Early-stage prostate cancer usually grows very slowly and may take years to cause any symptoms or other health problems, if it ever does at all. As a result, active surveillance or watchful waiting may be recommended. Radiation therapy or surgery may also be suggested, as well as treatment in clinical trials. For those with a higher Gleason score, the cancer may be faster growing, so radical prostatectomy and radiation therapy are often recommended. Your doctor will consider your age and general health before recommending a treatment plan.
ASCO, the American Urological Association, American Society of Radiation Oncology, and the Society of Urologic Oncology recommend that patients with high-risk early-stage prostate cancer that has not spread to other areas of the body should receive radical prostatectomy or radiation therapy with hormonal therapy as standard treatment options.
Locally advanced prostate cancer
Watchful waiting may be considered for older adults who are not expected to live for a long time and whose cancer is not causing symptoms or for those who have another, more serious illness.
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How Effective Is It For Treating Prostate Cancer
Although Lupron for prostate cancer is not a novel idea, studies on this subject are scarce. Current evidence confirms administration of leuprolide acetate can, indeed, suppress the production of testosterone, i.e., it is effective for androgen deprivation.
Not only is leuprolide effective in suppressing testosterone, but it is also well-tolerated.
Not every patient with prostate cancer will need to take Lupron. Doctors recommend and prescribe leuprolide acetate to men with late-stage prostate cancer.
Its highly unlikely for most doctors to start treating early-stage prostate cancer with hormonal therapies, including Lupron.
Doctors may prescribe Lupron for cases when cancer comes back after surgery or radiation therapy.
Hormone therapy such as Lupron may be recommended to patients whose cancers spread too much for radiation therapy and surgery to cure it.
Patients who cant have surgery or radiation therapy could benefit from Lupron and other hormone therapy approaches to treat prostate cancer.
Doctors may also recommend Lupron to shrink cancer before employing radiation therapy.
Prostate cancer patients undergoing radiation therapy and having a high risk of cancer returning may also get a prescription for Lupron therapy.
Now youre probably wondering why doctors cant start with hormonal therapy such as Lupron at early prostate cancer stages? Whats stopping them?
However, cancer may become resistant to the medication and stop responding to the treatment.
How To Use Lupron Solution
Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start using leuprolide and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
This medication is given by injection under the skin as directed by your doctor, usually once a day.
In children, the dosage is based on weight and response to treatment. The doctor should consider stopping treatment before age 11 for girls and age 12 for boys. Consult the doctor for details.
If you are using this medication at home, learn all preparation and usage instructions from your health care professional and the product package. Learn how to store and discard medical supplies safely.
Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Before injecting each dose, clean the injection site with rubbing alcohol. Change the injection site each time to lessen injury under the skin.
Use this medication regularly to get the most benefit from it. To help you remember, use it at the same time each day.
During the first few weeks of treatment, your hormone levels will actually go up before they go down. This is a normal response to this medication. Your symptoms may get worse for a few weeks.
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Restoring Sexual Function After Lupron/cancer Treatment
Facts about Prostate Cancer: Prostate cancer is a highly prevalent disease afflicting one in five American men. It is the most commonly diagnosed cancer in men and the second leading cause of cancer death after lung cancer. Treatments for localized prostate cancer include: Observation, Surgery and Radiation therapy ± androgen ablation. Treatments for advanced prostate cancer: Androgen ablation and Chemotherapy
Facts About Lupron, Zoladex: Lupron/Zoladex are synthetic GnRH agents which means that these agents mimic the messages made by the hypothalamus to stimulate the pituitary. Initially there is a burst of LH/FSH and elevation of testosterone ultimately, there is absent LH/FSH and therefore absent testosterone synthesis. Lupron/Zoladex are very effective agents stopping testicle biosynthesis of testosterone. Blood levels of testosterone fall below the reference values. Example: Pre-Lupron/Zoladex Testosterone 450 . Post-Lupron/Zoladex Testosterone 50 .
Therapies utilized for men who develop ED after treatment for prostate cancer:
MUSE/Intracavernosal therapy: MUSE and Caverject are both FDA approved for ED treatment and are more likely to be effective if the cause of the ED is disrupted erection nerve integrity. Side effects include penile pain and poor efficacy. Other intracavernosal agents may be used when Caverject is either not tolerated or not effective. Such alternative agents include papaverine and phentolamine and papaverine, phentolamine and PGE 1 .
Will Lupron Depot Affect My Ability To Get Pregnant Or Get My Partner Pregnant
Lupron Depot may temporarily decrease fertility in adults. However, once Lupron Depot treatment ends, this decrease in fertility typically goes away after a period of time. And use of Lupron Depot-Ped in children isnt known to affect fertility long term.
In some cases, Lupron Depot is prescribed off-label as a part of an infertility treatment called the luteal Lupron protocol.
For more details about Lupron Depot and fertility, see the Lupron Depot and pregnancy section below.
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Lupron Depot 30 Mg For 4
The recommended dose of LUPRON DEPOT 30 mg for 4-month administration is one injection every 16 weeks. Do not use concurrently a fractional dose, or a combination of doses of this or any depot formulation due to different release characteristics.
Incorporated in a depot formulation, the lyophilized microspheres must be reconstituted and should be administered every 16 weeks as a single intramuscular injection.
For optimal performance of the prefilled dual chamber syringe , read and follow the instructions in Section 2.5.
What To Expect During Treatment
Doctors often use hormone therapies, such as Lupron, in combination with radiation therapy or other treatments. They may also use it following surgery.
Healthcare professionals administer Lupron as a depot, which is a small implant that they inject under the persons skin. The individual can often choose an injection site that is suitable for them. Common injection sites include:
- upper arms
- outer thighs
The treatment regimen for Lupron will depend on the individuals circumstances, and a person can work with their doctor to determine the best dosage. Some typical dosages include:
- 7.5 mg one injection every 4 weeks
- 22.5 mg one injection every 12 weeks
- 30 mg one injection every 16 weeks
- 45 mg one injection every 24 weeks
When a person first starts treatment with Lupron, they may have a testosterone flare. Later on, they may experience side effects due to having very low testosterone levels in their body. After treatment stops, testosterone levels begin to return to normal.
When a person first takes Lupron, their testosterone levels may rise, or flare, before dropping to very low levels. For some people, particularly those with advanced prostate cancer, a testosterone flare can temporarily cause their symptoms to worsen.
The symptoms of a testosterone flare can include:
- blockage of the ureters, the tubes that carry urine from the kidneys to the bladder
- spinal cord compression
- issues with urination
Possible side effects of hormone therapies, such as Lupron, can
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Lupron Depot Side Effects
Lupron Depot can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking Lupron Depot. These lists do not include all possible side effects.
For more information on the possible side effects of Lupron Depot, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be bothersome.
Note: The Food and Drug Administration tracks side effects of drugs they have approved. If you would like to report to the FDA a side effect youve had with Lupron Depot, you can do so through MedWatch.
How Often Should I Receive Lupron Depot
Lupron Depot is given as an intramuscular injection into the muscle in your upper arm, buttock or thigh. Lupron Depot is available as single dose kits that contain a prefilled injection syringe of:
Depot formulations continuously release medicine into your body over a certain period of time after injection. This means you may not need to get a shot every day, or even every month. Your healthcare provider will give you Lupron Depot injection, and together you can decide which treatment dose and schedule might work best for you.
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Lupron Side Effects List For Healthcare Professionals
Clinical Trials
- In the majority of patients testosterone levels increased above baseline during the first week, declining thereafter to baseline levels or below by the end of the second week of treatment.
- This transient increase was occasionally associated with a temporary worsening of signs and symptoms, usually manifested by an increase in bone pain.
- In a few cases a temporary worsening of existing hematuria and urinary tract obstruction occurred during the first week.
- Temporary weakness and paresthesia of the lower limbs have been reported in a few cases.
- Potential exacerbations of signs and symptoms during the first few weeks of treatment is a concern in patients with vertebral metastases and/or urinary obstruction which, if aggravated, may lead to neurological problems or increase the obstruction.
- In a comparative trial of Lupron Injection versus DES, in 5% or more of the patients receiving either drug, the following adverse reactions were reported to have a possible or probable relationship to drug as ascribed by the treating physician.
- Often, causality is difficult to assess in patients with metastatic prostate cancer.
- Reactions considered not drug related are excluded.
Endocrine SystemLibido increase, Thyroid nodule
Postmarketing
Hemic and Lymphatic System-Decreased WBC