Leuprolide

LUPRON

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Pronunciation: loo-PROE-lide

Leuprolide ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Leuprolide ballicule

Leuprolide LUPRON / ELIGARD mascot mnemonic cartoon — Visual mnemonic: Leuprolide mascot
**“Eligard Loops the nards (indirectly)”**
QT prolongation

What it isGnRH receptor agonist causing downregulation; prostate cancer, endometriosis, fibroids and precocious puberty.

Why this oneIts broad depot range supports sustained suppression across oncology, gynecology, and precocious puberty.

What limits itAn initial testosterone flare requires antiandrogen cover in prostate cancer. Hot flushes and bone loss.

Leuprolide molecular structure (skeletal formula) — Molecular structure: Leuprolide

FDA-approved for

prostate cancer/endometriosis (1985)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Advanced prostate cancer (palliative)	Adults	1 mg SC QD	1 mg SC QD	1 mg SC QD

Renal Undefined

Hepatic Undefined

Instructions

Single daily subcutaneous injection; vary injection site periodically.
Inspect solution for discoloration/particulates before each use.

Available strengths

inj 3.75, 7.5, 11.25, 15, 21, 22.5, 30, 42, 45 mg

Contraindications

Known hypersensitivity to GnRH, GnRH agonist analogs, or excipients (anaphylaxis reported)

Cautions

Transient testosterone surge in first weeks → tumor flare (bone pain, urinary obstruction, worsening vertebral metastases/neurologic symptoms)
Decreased bone density with long-term use
Pituitary apoplexy (rare), some within hours of first dose

Adverse reactions

Hot flashes
Peripheral edema, ECG changes/ischemia
Decreased testicular size, gynecomastia, impotence, general pain, asthenia

Pregnancy May cause fetal harm based on animal data (malformations); no human data. Safety/efficacy not established in females.

Lactation No information; safety/efficacy not established in females.

Cost

Leuprolide (LUPRON)

Strength		#/mo	CostPlus
3.75 mg	inj	per unit	not offered
7.5 mg	inj	per unit	not offered
11.25 mg	inj	per unit	not offered
15 mg	inj	per unit	not offered
21 mg	inj	per unit	not offered
22.5 mg	inj	per unit	not offered
30 mg	inj	per unit	not offered
42 mg	inj	per unit	not offered
45 mg	inj	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Leuprolide is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry1998

NO BOXED WARNINGS

Principal riskTestosterone flare needing antiandrogen cover; bone loss

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger0 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.

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Memory aids: interaction avatars

no kinetic interactions

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