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Leuprorelin information from DrugsUpdate  

See Available Brands of Leuprorelin in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation
LI - Lab *

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

Pharmacodynamics

Pharmacokinetics

Leuprorelin is a gonadotropin-releasing hormone (GnRH) analogue. Continuous admin leads to down regulation of GnRH receptors and subesquently reduces gonadotrophin secretion. Reduced gonadotrophin levels lead to inhibition of sex hormone (androgen and oestrogen) production.

Absorption
Bioavailiability: 94% (SC admin) and zero if given orally.

Distribution
Protein binding: 43-49%.

Metabolism

Major metabolite: Pentapeptide.

Excretion

Elimination half-life: 3 hours (IV admin). Excreted via urine.

Leuprorelin Indications / Leuprorelin Uses

Information Not Available

Leuprorelin Adverse Reactions / Leuprorelin Side Effects

ECG changes/ischaemia, oedema, insomnia/sleep disorders, pain, headache, dizziness, nervousness, paraesthesias, impotence/decreased libido, gynaecomastia/breast tenderness/changes, hot flushes/sweats, GI disturbances, anorexia, constipation, nausea/vomiting, myalgia, bone pain, urinary frequency/urgency/disorders, haematuria, dyspnoea, anaemia, dermatitis, acne/seborrhoea, asthenia, amenorrhoea, reduced bone density.

Potentially Fatal: Thrombocytopenia and leucopenia.

Precautions

Information Not Available

Special Precautions

Worsening of signs and symptoms of prostatic cancer, osteoporosis (including drug induced). For management of central precocious puberty, treatment should be discontinued before the girl reaches 11 years old or the boy reaches 12 years old.

Other Drug Interactions

Information Not Available

Other Interactions

Information Not Available

Dosage

Parenteral
Palliative treatment of advanced prostate cancer
Adult: 1 mg as a single daily dose by SC injection. As depot preparations: 3.75 mg once a month, as a single IM/SC injection; or 11.25 mg every 3 months via SC injection. Alternatively, an implant containing 72 mg of leuprorelin acetate may be inserted subcutaneously into the inner part of the upper arm; releasing drug at a controlled rate of 120 mcg/day for 12 months. An anti-androgen such as cyproterone acetate may be given for a few days prior to starting treatment and continued for 3 weeks, to prevent disease flare.

Parenteral
Uterine fibroids
Adult: As depot preparations: 3.75 mg every month given as a single IM/SC injection or 11.25 mg every 3 months as IM depot Inj. Initiate treatment during the 1st 5 days of menstrual cycle up to 6 months (for endometriosis) or 3 months (for women with anaemia due to uterine fibroids).

Parenteral
Endometriosis
Adult: As depot preparations: 3.75 mg every month given as a single IM/SC injection or 11.25 mg every 3 months as IM depot injection. Initiate treatment during the 1st 5 days of menstrual cycle up to 6 months (for endometriosis) or 3 months (for women with anaemia due to uterine fibroids).

Parenteral
Precocious puberty
Child: Initially, 50 mcg/kg daily by SC injection, may be titrated upwards by 10 mcg/kg/day if total suppression of ovarian or testicular steroidogenesis is not achieved. As depot preparations: ≤25 kg: 7.5 mg; >25-37.5 kg: 11.25 mg and >37.5 kg: 15 mg; doses to be given via IM/SC injection every 4 weeks; may titrate dose upwards in increments of 3.75 mg every 4 weeks if down-regulation is not achieved.

Parenteral
As preparation for uterine surgery
Adult: As depot preparations: 3.75 mg as a single injection via IM/SC given 5-6 weeks before the procedure, or monthly for 3-4 months prior to surgery for uterine fibroids.

Food(before/after)

Information Not Available

List of Contraindications

Leuprorelin and Pregnancy

Contraindicated in pregnancy

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Leuprorelin and Lactation

Contraindicated in lactation

Leuprorelin and Children

Information Not Available

Leuprorelin and Geriatic

Information Not Available

Leuprorelin and Other Contraindications

Pregnancy, lactation; hypersensitivity to GnRH, GnRH agonist analogs or product excipients; undiagnosed abnormal vaginal bleeding.

Storage

Information Not Available

Lab interference

Information Not Available

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