leuprolide acetate


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leuprolide acetate (leuprorelin (UK))

Eligard, Lupron, Lupron Depot, Lupron Depot-Ped, Lupron Depot-3 Month, Lupron Depot-4 Month, Lupron-3 Month SR Depot, Prostap (UK)

Pharmacologic class: Gonadotropin-releasing hormone (GnRH) analog

Therapeutic class: Antineoplastic

Pregnancy risk category X

Action

Inhibits and desensitizes GnRH receptors, thus inhibiting gonadotropin secretion when given continuously. This inhibition causes initial increase and then profound decrease in luteinizing hormone and follicle-stimulating hormone levels and, ultimately, reduces testosterone and estrogen sex hormones.

Availability

Eligard Depot: 7.5 mg, 22.5 mg, 30 mg, 45 mg

Injection: 1 mg/0.2 ml

Lupron Depot injection: 3.75 mg/ml, 7.5 mg/ml

Lupron Depot-3 month injection: 11.25 mg, 22.5 mg

Lupron Depot-4 month injection: 30 mg

Lupron Depot-Ped injection: 7.5 mg, 11.25 mg, 15 mg

Indications and dosages

Advanced prostate cancer

Adults: 1 mg subcutaneously daily (1 mg/0.2-ml formulation). For Lupron Depot formulation, 7.5 mg I.M. monthly, 22.5 mg I.M. q 3 months, or 30 mg I.M. q 4 months. For Eligard formulation, 7.5 mg subcutaneously monthly, 22.5 mg subcutaneously q 3 months, 30 mg subcutaneously q 4 months, or 45 mg subcutaneously q 6 months.

Endometriosis

Adults: 3.75 mg I.M. (depot injection) as a single injection once monthly, or 11.25 mg I.M. q 3 months. Duration is up to 6 months.

Adjunct to iron therapy in anemia caused by uterine leiomyomas

Adults: 3.75 mg I.M. monthly or 11.25 mg I.M. q 3 months as a single dose. Recommended duration is 6 months or less.

Central precocious puberty

Children: 50 mcg/kg/day subcutaneously as a single injection, increased in increments of 10 mcg/kg/day as needed

Children weighing more than 37.5 kg (82.5 lb): Initially, 15 mg of Depot-Ped I.M. q 4 weeks, increased in increments of 3.75 mg q 4 weeks as needed

Children weighing 25 to 37.5 kg (55 to 82.5 lb): Initially, 11.25 mg of Depot-Ped I.M. q 4 weeks, increased in increments of 3.75 mg q 4 weeks as needed

Children weighing less than 25 kg (55 lb): Initially, 7.5 mg of Depot-Ped I.M. q 4 weeks, increased in increments of 3.75 mg q 4 weeks as needed

Contraindications

• Hypersensitivity to drug, its components, GnRH, or other GnRH analogs
• Undiagnosed abnormal vaginal bleeding
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• renal, hepatic, or cardiac impairment.

Administration

• Give Eligard within 30 minutes of mixing. After this time, discard.
• Administer Lupron injection immediately after mixing. Otherwise, discard.
• Administer Lupron Depot-Ped only under prescriber's supervision.

Adverse reactions

CNS: anxiety, depression, dizziness, drowsiness, asthenia, fatigue, headache, vertigo, syncope, mood changes

CV: palpitations, angina, arrhythmias, myocardial infarction

EENT: blurred vision

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, anorexia

GU: urinary frequency, hematuria, decreased testes size, erectile dysfunction, decreased libido, gynecomastia

Hematologic: anemia, thrombocytopenia

Respiratory: dyspnea, pleural rub, worsening of pulmonary fibrosis, pulmonary embolism

Skin: alopecia, pruritus, rash, diaphoresis

Other: sour taste, edema, hot flashes, anaphylaxis

Interactions

Drug-diagnostic tests.Blood urea nitrogen, creatinine: increased levels

Pituitary-gonadal system tests: misleading results during and for up to 3 months after therapy

Patient monitoring

• Observe injection site for local reactions.

Monitor cardiovascular and respiratory status carefully to detect serious adverse reactions.
• Evaluate neurologic status. Institute safety measures as needed to prevent injury.
• Periodically monitor serum testosterone and prostate-specific antigen levels.

Patient teaching

• Inform patient that localized reaction may occur at injection site. Tell him to contact prescriber if symptoms don't resolve.
• Advise patient and family to watch for and report signs or symptoms of depression.
• Tell patient drug may cause libido changes or erectile dysfunction. Encourage him to discuss these problems with prescriber.
• Teach patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.

Instruct female of childbearing age to use reliable contraception during therapy. Tell her to stop drug immediately and contact prescriber if she suspects pregnancy.

Tell female patient not to breastfeed.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the tests mentioned above.

leu·pro·lide ac·e·tate

(lū'prō-līd as'ĕ-tāt),
A synthetic nonapeptide analog of naturally occurring gonadotropin-releasing hormone; used in the palliative treatment of advanced prostatic cancer.

leuprolide acetate

[lo̅o̅′prōlīd]
an analog of gonadotropin-releasing hormone. It is an agonist administered at levels that desensitize the pituitary gland from responding to it or to endogenous gonadotropin-releasing hormone, thereby preventing pituitary stimulation of sex hormone production by the ovaries or testes.
indications It is used for the palliative treatment of advanced prostatic cancer, in the management of endometriosis, and for the treatment of children with central precocious puberty.
contraindications Caution should be exercised during the beginning of leuprolide acetate therapy when symptoms of bone pain, urinary obstruction, and neurological problems may increase. Known hypersensitivity to the drug or pregnancy prohibits its uses.
adverse effects Among adverse effects reported are hot flashes, transient increases in testosterone levels, dizziness, pain, headache, decreased libido, impotence, and injection site irritation.
References in periodicals archive ?
This turkey was treated with the same regimen of leuprolide acetate and deslorelin acetate implants at the same time intervals as the turkey in case 1.
Anecdotal evidence has suggested that leuprolide acetate also boosts cognition in some men taking it for prostate cancer, said Dr.
With the new Atrix product, an ATRIGEL formulation containing leuprolide acetate is injected subcutaneously as a liquid, where it solidifies and releases a predetermined dose of leuprolide continuously over a 30-day period as it is bioabsorbed.
Acromegaly lanreotide acetate octreotide acetate Hormone Therapy Medroxyprogesterone Somatropin Infectious Disease Interferon Metabolic Exenatide Oncology Neoplastic Meningitis Cytarabine Prostate leuprolide acetate leuprolide acetate triptorelin pamoate Schizophrenia Fluphenazine Haloperidol paliperidone palmitate olanzapine risperidone Substance Abuse naltrexone Reproductive Health Estradiol valerate Depo-estradiol Depo-testosterone
Key words: ovarian neoplasia, ovarian adenocarcinoma, ovarian adenoma, ascites, leuprolide acetate, deslorelin, gonadotropin-releasing hormone agonist, avian, cockatiel, Nymphicus hollandicus
She had amenorrhea as a result of 5 years of treatment with leuprolide acetate and add-back therapy.
Depo subQ provera 104 (DMPA-SC), which contains 104 mg medroxyprogesterone acetate, treats endometriosis pain as effectively as leuprolide acetate, but is associated with significantly less bone loss and fewer vasomotor symptoms, according to data provided by Pfizer Inc.
This new patent is specific to the composition of our proprietary Atrigel drug delivery system with leuprolide acetate, the active component in our Eligard prostate cancer products.
5 mg three-month depot, leuprolide acetate for the treatment of advanced prostate cancer, to the German regulatory authority, Bundesinstitut fur Arzneimittel und Medizinprodukte (BfArM), as the reference member state under a mutual recognition process.
In vitro fertilization treatment cycles have historically been initiated with the administration of leuprolide acetate to suppress the premature release of leutenizing hormones (LH), which trigger ovulation.
Tenders are invited for Supply of Leuprolide Acetate 3.