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Leuprolide

 
Drug Info: Leuprolide

Brand names: Eligard®Lupron®Viadur™

Chemical formula:



Leuprolide Acetate Solution for injection

What is this medicine?

LEUPROLIDE (loo PROE lide) is a man-made hormone. It is used to treat the symptoms of prostate cancer. This medicine may also be used to treat children with early onset of puberty. It may be used for other hormonal conditions.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•pain or difficulty passing urine
•spinal cord metastasis
•an unusual or allergic reaction to leuprolide, benzyl alcohol, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for injection under the skin or into a muscle. You will be taught how to prepare and give this medicine. Use exactly as directed. Take your medicine at regular intervals. Do not take your medicine more often than directed.

It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or healthcare provider to get one.

A patient information sheet for the product will be given with each prescription and refill. Read this sheet carefully each time. The sheet may change frequently.

Talk to your pediatrician regarding the use of this medicine in children. While this medicine may be prescribed for children as young as 8 years for selected conditions, precautions do apply.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•chasteberry

This medicine may also interact with the following medications:
•herbal or dietary supplements, like black cohosh or DHEA
•female hormones, like estrogens or progestins and birth control pills, patches, rings, or injections
•male hormones, like testosterone

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. During the first week, your symptoms may get worse, but then will improve as you continue your treatment. You may get hot flashes, increased bone pain, increased difficulty passing urine, or an aggravation of nerve symptoms. Discuss these effects with your doctor or health care professional, some of them may improve with continued use of this medicine.

Female patients may experience a menstrual cycle or spotting during the first 2 months of therapy with this medicine. If this continues, contact your doctor or health care professional.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•chest pain
•depression or memory disorders
•pain in your legs or groin
•pain at site where injected
•severe headache
•swelling of the feet and legs
•visual changes
•vomiting

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•breast swelling or tenderness
•decrease in sex drive or performance
•diarrhea
•hot flashes
•loss of appetite
•muscle, joint, or bone pains
•nausea
•redness or irritation at site where injected
•skin problems or acne

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store below 25 degrees C (77 degrees F). Do not freeze. Protect from light. Do not use if it is not clear or if there are particles present. Throw away any unused medicine after the expiration date.

Last updated: 2/21/2005 3:32:00 PM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Leuprolide
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Leuprolide
Systematic (IUPAC) name
N-[1-[[1-[[1-[[1-[[1-[[1-[[5-(diaminomethylideneamino)-1-
[2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxo-pentan-2-
yl]carbamoyl]-3-methyl-butyl]carbamoyl]-3-methyl-
butyl]carbamoyl]-2-(4-hydroxyphenyl)ethyl]
carbamoyl]-2-hydroxy-ethyl]carbamoyl]-2-(1H-indol-3-
yl)ethyl]carbamoyl]-2-(3H-imidazol-4-yl)ethyl]-5-oxo-
pyrrolidine-2-carboxamide
Identifiers
CAS number 53714-56-0
ATC code L02AE02
PubChem 441410
DrugBank DB00007
Chemical data
Formula C59H84N16O12 
Mol. mass 1209.4 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 3 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

X

Legal status

Prescription only

Routes Implant / Injection

Leuprorelin (INN) or leuprolide acetate (USAN) is a gonadotropin-releasing hormone analog (GnRH analog). Proper Sequence: p-Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt

Contents

Mode of action

Leuprolide acts at pituitary GnRH receptors. It down regulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) leading to a dramatic reduction in estradiol levels.

Clinical usage

Like other GnRH agonists, leuprolide may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis[1] or uterine fibroids), to treat precocious puberty,[2] and to control ovarian stimulation in In Vitro Fertilization (IVF). It is considered a possible treatment for paraphilias.[3]

A 2005 paper suggested it as a treatment for autism,[4] the hypothetical method of action being the now defunct theory that autism is caused by mercury, with the additional assumption that mercury binds irreversibly to testosterone and therefore leuprolide can help cure autism by lowering the testosterone level and thereby the mercury level.[5] However, used on children or adolescents it could cause disastrous and irreversible damage to sexual functioning, and there is no scientifically valid or reliable research to show its effectiveness in treating autism.[6] Mark Geier, the proponent of the hypothesis, has frequently been barred from testifying in vaccine-autism related cases on the grounds of not being sufficiently expert in that particular issue.[7][8][9]

Leuprolide has been tested as a treatment for reducing sexual urges in pedophiles and other cases of paraphilia.[10][11]

Leuprolide is also under investigation for possible use in the treatment of mild to moderate Alzheimer's disease.[12]

Approvals

  • Lupron Injection (5 mg/mL for daily subcutaneous injection) was first approved by the FDA for treatment of advanced prostate cancer on April 9, 1985.
  • Lupron Depot (7.5 mg/vial for monthly intramuscular depot injection) was first approved by the FDA for palliative treatment of advanced prostate cancer on January 26, 1989, and subsequently in 22.5 mg/vial and 30 mg/vial for intramuscular depot injection every 3 and 4 months, respectively. 3.75 mg/vial and 11.25 mg/vial dosage forms were subsequently approved for subcutaneous depot injection every month and every 3 months, respectively for treatment of endometriosis or fibroids. 7.5 mg/vial, 11.25 mg/vial, and 15 mg/vial dosage forms were subsequently approved for subcutaneous depot injection for treatment of children with central precocious puberty.
  • Viadur (72 mg yearly subcutaneous implant) was first approved by the FDA for palliative treatment of advanced prostate cancer on March 6, 2000.
  • Eligard (7.5 mg for monthly subcutaneous depot injection) was first approved by the FDA for palliative treatment of advanced prostate cancer on January 24, 2002, and subsequently in 22.5 mg, 30 mg, and 45 mg doses for subcutaneous depot injection every 3, 4, and 6 months, respectively.

Leuprolide acetate is marketed by Bayer AG under the brand name Viadur, by Sanofi-Aventis under the brand name Eligard, and by TAP Pharmaceuticals (1985-2008) and Abbott Laboratories (2008-current) under the brand name Lupron. It is available as a slow-release implant or subcutaneous/intramuscular injection.

In the UK, leuprorelin is marketed by Wyeth as Prostap SR(one month injection) and Prostap 3 (three month injection).

Warnings

Further, an article by Carla K. Johnson of the AP, dated August 26, 2009 noted a recent study that found that this prostate cancer drug is very risky especially for men with heart problems. The AP article stated, "The hormone treatment was linked with a 96 percent higher risk of death after adjusting for other risk factors." A similar study issued in JAMA in July 2008 also found that the drug offered no life-prolonging benefits in men with advanced prostate cancer vs. men who did not take any form of hormone therapy, or conservative management. Women with Endometriosis also suffer significant side effects. Another reliable source with documented information is lupronvictimshub.com. Carefully review the labeling, which was recently undated to include the adverse event of "pituitary apoplexy" (bleeding-out of a tumor on the pituitary gland) Also, in June 2009 the label was changed again to warn about "convulsion" in the post-marketing surveillance. The label shows that 98% of women had adverse events including 65% suffering headache/migraine, 31% depression, 31% insomnia, and 25% Nausea/vomiting. Many other adverse events are listed in the label. See full label at FDA.gov. The label also notes that women with no history of depression or psychiatric illness reported suicidal ideation and attempt.

See also

External links

References

  1. ^ Crosignani PG, Luciano A, Ray A, Bergqvist A (January 2006). "Subcutaneous depot medroxyprogesterone acetate versus leuprolide acetate in the treatment of endometriosis-associated pain". Human reproduction (Oxford, England) 21 (1): 248–56. doi:10.1093/humrep/dei290. PMID 16176939. http://humrep.oxfordjournals.org/cgi/pmidlookup?view=long&pmid=16176939. 
  2. ^ Badaru A, Wilson DM, Bachrach LK, et al. (May 2006). "Sequential comparisons of one-month and three-month depot leuprolide regimens in central precocious puberty". The Journal of clinical endocrinology and metabolism 91 (5): 1862–7. doi:10.1210/jc.2005-1500. PMID 16449344. http://jcem.endojournals.org/cgi/pmidlookup?view=long&pmid=16449344. 
  3. ^ Saleh F, Niel T, Fishman M (2004). "Treatment of paraphilia in young adults with leuprolide acetate: a preliminary case report series". J Forensic Sci 49 (6): 1343–8. doi:10.1520/JFS2003035. PMID 15568711. http://www.astm.org/cgi-bin/SoftCart.exe/JOURNALS/FORENSIC/PAGES/JFS2003035.htm?E+mystore. 
  4. ^ Geier M, Geier D (2005). "The potential importance of steroids in the treatment of autistic spectrum disorders and other disorders involving mercury toxicity". Med Hypotheses 64 (5): 946–54. doi:10.1016/j.mehy.2004.11.018. PMID 15780490. 
  5. ^ Allen A (2007-05-28). "Thiomersal on trial: the theory that vaccines cause autism goes to court". Slate. http://www.slate.com/id/2166939/. Retrieved 2008-01-30. 
  6. ^ "Testosterone regulation". Research Autism. 2007-05-07. http://www.researchautism.net/interventionitem.ikml?id=24. Retrieved 2007-08-19. 
  7. ^ "John and Jane Doe v. Ortho-Clinical Diagnostics, Inc", US District Court for the Middle District of North Carolina, July 6, 2006
  8. ^ "Dr. Mark Geier Severely Criticized", Stephen Barrett, M.D., Casewatch.org
  9. ^ Mills S, Jones T (2009-05-21). "Physician team's crusade shows cracks". Chicago Tribune. http://www.chicagotribune.com/health/chi-autism-lupron-geiers-may21,0,983359.story. Retrieved 2009-05-21. 
  10. ^ Schober JM, Byrne PM, Kuhn PJ. (2006). "Leuprolide acetate is a familiar drug that may modify sex-offender behaviour: the urologist's role.". BJU international 97 (4): 684–6. doi:10.1111/j.1464-410X.2006.05975.x. PMID 16536753. 
  11. ^ Schober JM, Kuhn PJ, Kovacs PG, Earle JH, Byrne PM, Fries RA. (2005). "Leuprolide acetate suppresses pedophilic urges and arousability.". Archives of Sexual Behavior 34 (6): 691–705. doi:10.1007/s10508-005-7929-2. PMID 16362253. 
  12. ^ Doraiswamy PM, Xiong GL. (2006). "Pharmacological strategies for the prevention of Alzheimer's disease". Expert Opin Pharmacother 7 (1): 1–10. doi:10.1517/14656566.7.1.1. PMID 16370917. 

 
 

 

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