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.
References in periodicals archive ?
Leuprolide acetate (750 [micro]g/kg IM; Lupron) was administered twice at a 2-week interval in the postoperative period to suppress ovarian activity and reduce the risk of ectopic ovulation after salpingohysterectomy.
Food and Drug Administration, "LUPRON DEPOT[R]3 Month 11.25 mg (leuprolide acetate for depot suspension) 3-month formulation," 2012, https://www.accessdata.fda.gov/ drugsatfda_docs/label/2012/020708s033lbl.pdf.
Characteristics of current medical strategies in the prevention of ovarian hyp er stimulation syndrome Medical strategies /characteristics Studies GnRH agonist trigger Thomsen et al.(3) - buserelin 0.5 mg Casper et al.(12) - triptorelin 0.2 mg Engmann et al.(14) - leuprolide acetate Gulekli et al.(16) 0.5-4 mg Humaidan et al.(21) Griesenger et al.(22) Fatemi et al.(26) GnRH antagonist Al-Inany et al.(37) regimens Giliam (38) - single 0.3 mg Xiao et al.
Atwood, "Leuprolide acetate: a drug of diverse clinical applications," Expert Opinion on Investigational Drugs, vol.
The PEARL II study, a randomized prospective trial, included women suffering from symptomatic uterine fibroids who received either an intramuscular injection of leuprolide acetate or treatment with ulipristal acetate (5 or 10 mg) [74].
One of the patients used triptorelin acetate and the others used leuprolide acetate. All patients had different disorders; however, before the GnRH analogue treatment, none of them had neither predispositions such as obesity, Addison disease, drugs etc.
Effectiveness and limitations of the use of the gonadotropin-releasing hormone agonist leuprolide acetate in the diagnosis of delayed puberty in males.
Leuprolide acetate (3.75 mg) was injected for three cycles, with an interval of 28 days, to treat leiomyoma.
A case of atypical absence seizures induced by leuprolide acetate. Pediatr Neurol 2000; 23: 266-8.
In case of long protocol, down regulation was achieved using leuprolide acetate (Lupride, Sun pharmaceuticals, Gujarat, India) at a dose of 0.5 mg subcutaneously daily starting from day 21 of the previous menstrual cycle till the day of hCG administration.
The patient has been put on injection leuprolide acetate (3.75 mg) subcutaneously every 28 days for six months.
It is to assess enzalutamide at a dose of 160mg to be taken orally once daily and leuprolide acetate will be given as an injection of 22.5mg once every 12 weeks for a minimum of three doses.