leuprorelin


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Related to leuprorelin: goserelin

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.

leuprorelin

A GONADOTROPHIN-releasing hormone drug used to treat ENDOMETRIOSIS in women and prostate cancer in men. In prostate cancer, the effect of leuprorelin is said to be equivalent to that of orchiectomy, and disease progression is prevented in up to 95 per cent of patients. A brand name is Prostap.
References in periodicals archive ?
8 sgb v on medicines with the active ingredient leuprorelin (atc: L02ae02 + h01ca04) within the period from 1.7.2019 to 30.6.2021 with possibility of contract conclusion at any time (open-house model).
The study involved around 280 patients, who were randomised 1:1 to receive either 40mg of relugolix, administered once daily, or leuprorelin acetate, which was administered via injection once every four weeks.
All patients received 6 months ADT with monthly 3.75mg leuprorelin acetate intramuscular injection.
We administered either distilled water (sham operated) or leuprorelin 0.5 mg/kg subcutaneously once to the backs of androgen-deprived rats.
She had curettage (dilation and curettage) followed by GnRH-a (leuprorelin acetate microspheres for injection, Shanghai Livzon Pharmaceutical Co., Ltd., China) 3.75 mg subcutaneous injection, and was advised to stop Marvelon.
Pharmacokinetics, safety and tolerability of three dosage regimens of buccal adhesive testosterone tablets in healthy men suppressed with leuprorelin. J Endocrinol 2002,175(3):813-9.
Among these polymers, polylactide (PLA), and poly(L-lactide-co-glycolide) (PLGA) have attracted growing attention [1, 2], Now, the PLA or PLGA microspheres with good biocompatibility and biodegradation have been used for incorporating bone morphogenetic protein and leuprorelin acetate and applications or interactions with the eye, central nervous system, and lymphoid tissue and their relevance to vaccine development [3].
On Day 5, our patient was started on leuprorelin and parenteral steroids.
Sica et al., "Luteinizing hormone-releasing hormone analogue: leuprorelin acetate for the prevention of menstrual bleeding in premenopausal women undergoing stem cell transplantation," Bone Marrow Transplantation, vol.
Postoperative close surveillance and leuprorelin injections, a gonadotropin-releasing hormone (GnRH) analog, were advised.
Okada, "One- and three-month release injectable microspheres of the LH-RH superagonist leuprorelin acetate," Advanced Drug Delivery Reviews, vol.
In the Australian phase 3 trial of Denham, all patients were given six months of leuprorelin, and radiotherapy to the prostate and seminal vesicles after 5 months from randomisation.