Drug Guide

Generic Name

Leuprolide Acetate

Brand Names Lupron, Lupron Depot, Lupron Depot-ped Kit, Viadur, Eligard Kit, Leuprolide Acetate For Depot Suspension, Fensolvi Kit

Classification

Therapeutic: Hormonal agent / Gonadotropin-releasing hormone (GnRH) agonist

Pharmacological: GnRH receptor agonist

FDA Approved Indications

Prostate cancer
Endometriosis
Uterine fibroids
Central precocious puberty
palliative treatment of breast cancer in postmenopausal women

Mechanism of Action

Leuprolide acetate acts as a GnRH agonist, initially stimulating then downregulating GnRH receptors in the pituitary gland, leading to decreased secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), resulting in decreased sex hormone production (testosterone and estrogen).

Dosage and Administration

Adult: Dosing varies based on condition; for prostate cancer, typically 7.5 mg IM every month or 22.5 mg IM every 3 months; for endometriosis, 3.75 mg IM monthly or 11.25 mg IM every 3 months; for prostate cancer, 45 mg subcut every 6 months for Viadur.

Pediatric: Dosing for central precocious puberty: 11.25 mg IM every 3 months, adjusted based on response.

Geriatric: Adjust based on response and tolerability; no specific dose alterations provided.

Renal Impairment: No specific adjustments, but caution as with all GnRH analogs.

Hepatic Impairment: No specific data; use caution.

Pharmacokinetics

Absorption: Administered as depot injections; absorption is slow from the injection site.

Distribution: Distributed into tissues; specifics not well defined.

Metabolism: Metabolized in the liver.

Excretion: Excreted mainly in urine.

Half Life: Approximately 3-4 hours for plasma; depot formulations provide sustained release.

Contraindications

Hypersensitivity to leuprolide or GnRH analogs

Precautions

Pregnancy category X; contraindicated in pregnancy
Liver function impairment
Monitor for tumor flare in prostate cancer patients
Use with caution in patients with osteoporosis

Adverse Reactions - Common

Hot flashes (Common)
Injection site reactions (Common)
Reduced libido (Common)
Fatigue (Common)

Adverse Reactions - Serious

Bone mineral density reduction (Less common)
Cardiovascular events (Rare)
Tumor flare syndrome (Rare in prostate cancer initiation)

Drug-Drug Interactions

Additive effects with other hormonal therapies
Potential interaction with CYP450 substrate drugs (less significant)

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor hormone levels, tumor markers, bone density as indicated, and for tumor flare during initiation.

Diagnoses:

Risk for decreased bone density
Risk for ineffective tissue perfusion (tumor flare)

Implementation: Administer injections as scheduled; monitor for adverse reactions; educate about menopausal symptoms.

Evaluation: Assess symptom relief, monitor side effects, and adjust treatment as necessary.

Patient/Family Teaching

Explain the purpose of medication and expected effects
Report any severe pain, hot flashes, or signs of allergic reaction
Use contraception if applicable, as pregnancy is contraindicated
Maintain regular follow-up appointments for monitoring

Special Considerations

Black Box Warnings:

Tumor flare risk at initiation in prostate cancer
Emotional and metabolic changes during treatment

Genetic Factors: None specific to leuprolide acetate

Lab Test Interference: Potential alterations in testosterone and estrogen levels

Overdose Management

Signs/Symptoms: Symptoms are unlikely but may include hormonal imbalance effects.

Treatment: Supportive therapy; no specific antidote.

Storage and Handling

Storage: Store in a refrigerator at 2-8°C (36-46°F). Protect from light.

Stability: Stable until expiration date if stored properly.