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Leuprolide Acetate, Leuprolide Mesylate (Monograph)

Brand names: Eligard, Lupron Depot, Lupron Depot-Ped, Fensolvi, Camcevi
Drug class: Gonadotropins

Medically reviewed by Drugs.com on Jul 10, 2024. Written by ASHP.

Introduction

Antineoplastic agent and gonadotropin-releasing hormone (GnRH) agonist; a synthetic nonapeptide analog of naturally occurring GnRH (luteinizing hormone-releasing hormone [LHRH], gonadorelin).1 2 3 80 81 116 155 190 191 192 204 205

Uses for Leuprolide Acetate, Leuprolide Mesylate

Prostate Cancer

Treatment of advanced prostate cancer.1 2 3 4 5 27 32 33 34 35 36 37 38 39 40 43 57 63 66 96 111 112 113 114 121 125 190 192 201 205

Leuprolide acetate is available in various commercial preparations for this use, including an injection solution for sub-Q administration, a depot suspension for IM administration, and an injectable suspension for sub-Q administration.1 190 192 Leuprolide is also available as the mesylate salt in an injectable emulsion for sub-Q use in the treatment of advanced prostate cancer.205

Hormonal therapy (also referred to as androgen deprivation therapy) is considered standard treatment of advanced/metastatic prostate cancer.201 Hormonal therapy can be achieved with surgery (bilateral orchiectomy) or medical castration using gonadotropin-releasing hormone (GnRH) agonists (e.g., leuprolide) or antagonists.201 216

Endometriosis

Treatment of endometriosis (e.g., pain relief, reduction in endometriotic lesions [dysmenorrhea and pelvic pain, tenderness, and induration]).5 55 71 96 105 106 107 108 116 126 131 191

Used alone for treatment of endometriosis (e.g., pain relief, reduction of endometriotic lesions) or in conjunction with norethindrone acetate for initial management of painful symptoms of endometriosis and management of recurrence of symptoms.116 191

Used in conjunction with norethindrone acetate (5 mg daily) if symptoms recur after the initial course of therapy (retreatment).116 191 Retreatment with leuprolide alone is not recommended.116 191

Combined use of norethindrone acetate and leuprolide (add-back therapy) is designed to reduce loss of bone mineral density and reduce vasomotor symptoms associated with leuprolide.116 191 Total duration of leuprolide therapy plus add-back therapy should not exceed 12 months because of potential adverse impact on bone mineral density.116 191

The American College of Obstetricians and Gynecologists (ACOG) guidelines include GnRH agonists such as leuprolide for management of pain associated with endometriosis, but state that other methods such as combined oral contraceptives are superior.217

Uterine Leiomyomata

Used for the preoperative hematologic improvement in women with anemia caused by uterine leiomyomata (uterine fibroids) for whom 3 months of hormonal suppression is deemed necessary;116 181 191 used in conjunction with iron therapy.116 181 191

ACOG guidelines recommend GnRH agonists for short-term treatment of abnormal uterine bleeding associated with leiomyomas and uterine enlargement associated with uterine leiomyomas and as a bridge to other treatment strategies (e.g., interventional procedures, surgery, menopause).219

Precocious Puberty

Treatment of central precocious puberty (CPP) in pediatric patients155 157 158 159 160 161 162 163 164 165 166 177 202 203 204 (designated an orphan drug by FDA for this use).179

Leuprolide acetate depot suspension (Lupron Depot-Ped) is indicated for pediatric patients ≥1 year of age and leuprolide acetate injectable suspension (Fensolvi) is indicated for pediatric patients ≥2 years of age.155 204

The American Academy of Pediatrics (AAP) guidelines recommend the use of GnRH analogs to manage CPP, particularly to preserve height potential.221 222

Leuprolide Acetate, Leuprolide Mesylate Dosage and Administration

General

Pretreatment Screening

Patient Monitoring

Administration

Administer by sub-Q or IM injection depending on the formulation and indication.14 116 155 190 191 192 204 Leuprolide acetate depot suspension (Lupron Depot, Lupron Depot-Ped) is administered by IM injection.116 155 190 191 Leuprolide acetate for injectable suspension (Eligard, Fensolvi) and leuprolide acetate injection are administered by sub-Q injection.1 192 204

Leuprolide mesylate injectable emulsion (Camcevi) is administered by sub-Q injection.205

Some formulations of leuprolide are not intended for self-administration and should be administered by a healthcare professional only (e.g., Camcevi,Eligard, Fensolvi, Lupron, Lupron Depot-Ped); consult the manufacturer's prescribing information for details.155 190 191 192 204 205

Each extended-release or depot strength and formulation of leuprolide has different release characteristics.116 155 190 191 192 204 Do not use partial syringes, a combination of syringes, or substitute other extended-release products to achieve a particular dose.116 155 190 191 192 204

IM Administration

Leuprolide acetate powder for depot suspension (Lupron Depot, Lupron Depot-Ped): Reconstitute single-use syringes with the accompanying diluent according to manufacturer's instructions.116 155 190 191 Following reconstitution, administer within 2 hours.116 155 190 191 Rotate injection sites with each injection.116 155 190 191 Consult manufacturer's prescribing information for additional details.116 155 190 191

Sub-Q Administration

Leuprolide acetate injection: Administer sub-Q as single daily injections.1

Leuprolide acetate for injectable suspension (Eligard): Administer by sub-Q injection to provide continuous release of drug.192 Reconstitute commercially available powder with supplied prefilled diluent using aseptic technique and gloves prior to administration.192 Allow the drug to reach room temperature prior to reconstitution; once mixed, administer within 30 minutes or discard.192 Select a specific injection location in an area with sufficient soft or loose sub-Q tissue that does not have excessive pigment, nodules, lesions, or hair and has not been recently used.192 Rotate injection sites with each injection.192 Consult manufacturer's prescribing information for additional details.192

Leuprolide mesylate injectable emulsion (Camcevi): Administer by sub-Q injection once every 6 months.205 Allow to sit at room temperature for 30 minutes prior to administration.205 Select an injection location with sufficient soft or loose sub-Q tissue; avoid brawny or fibrous tissues or areas that could be rubbed or compressed (e.g., with a belt or clothing waistband).205 Rotate injection sites with each injection.205 Consult manufacturer's prescribing information for additional details.205

Leuprolide acetate for injectable suspension (Fensolvi): Administer by sub-Q injection once every 6 months.204 Reconstitute commercially available lyophilized drug with supplied prefilled diluent using aseptic technique and gloves prior to administration; the final concentration after reconstitution is 45 mg/0.375 mL.204 Allow drug to reach room temperature before reconstitution.204 Following reconstitution, administer within 30 minutes or discard.204 Recommended injection sites include abdomen, upper buttocks, or another location with adequate amounts of sub-Q tissue that does not have excessive pigment, nodules, lesions, or hair.204 Rotate injection sites with each injection.204 Consult manufacturer's prescribing information for additional details.204

Dosage

Available as leuprolide acetate and leuprolide mesylate; dosage expressed in terms of the salt.1 116 155 190 191 192 204 205

Pediatric Patients

Central Precocious Puberty
Monthly Therapy with Leuprolide Acetate for Depot Suspension (Lupron Depot-Ped)
IM

Individualize dosage; starting dosage is based on patient's body weight (see Table 1).155 Dosage adjustment may be necessary with changes in body weight.155 Select the appropriate syringe for the intended dosing frequency.155

If satisfactory hormonal and clinical suppression is not achieved with initial dosage, then increase to the next available higher dosage at the next monthly injection.155

Monitor response with a GnRH stimulation test, basal LH, or serum concentration of sex steroid levels beginning 1 to 2 months following initiation of therapy, with changing doses, or further as judged clinically appropriate in order to confirm maintenance of efficacy.155

Assess height (for calculation of growth rate) and bone age every 6 to 12 months.155

Discontinue therapy at the appropriate age of onset of puberty.155

Table 1. Dosage Recommendations for Monthly Therapy with Leuprolide Acetate for Depot Suspension (Lupron Depot-Ped)155

Weight

Once-monthly Recommended Dosage

≤25 kg

7.5 mg

25–37.5 kg

11.25 mg

>37.5 kg

15 mg
Every 3-Month Therapy with Leuprolide Acetate for Depot Suspension (Lupron Depot-Ped)
IM

11.25 mg or 30 mg once every 3 months (12 weeks) given as a single dose.155

Monitor response with a GnRH stimulation test, basal LH, or serum concentration of sex steroid levels at 2 to 3 months, 6 months, and further as judged clinically appropriate in order to confirm maintenance of efficacy.155

Assess height (for calculation of growth rate) and bone age every 6 to 12 months.155

Discontinue therapy at the appropriate age of onset of puberty.155

Every 6-Month Therapy with Leuprolide Acetate for Depot Suspension (Lupron Depot-Ped)
IM

45 mg once every 6 months (24 weeks) given as a single dose.155

Monitor response with a GnRH stimulation test, basal LH, or serum concentration of sex steroid levels at months 5 to 6 and further as judged clinically appropriate in order to confirm maintenance of efficacy.155

Assess height (for calculation of growth rate) and bone age every 6 to 12 months.155

Discontinue therapy at the appropriate age of onset of puberty.155

Every 6-Month Therapy with Leuprolide Acetate for Injectable Suspension (Fensolvi)
Sub-Q

Pediatric patients ≥2 years of age: 45 mg administered by sub-Q injection once every 6 months.204 Discontinue treatment at the appropriate age of onset of puberty.204

Monitor response with a GnRH agonist stimulation test, basal serum LH levels, or serum concentration of sex steroid levels at 1 to 2 months following initiation of therapy and as needed to confirm adequate suppression of pituitary gonadotropins, sex steroids, and progression of secondary sexual characteristics.204

Measure height (for calculation of growth velocity) every 3 to 6 months and monitor bone age periodically.204

If treatment with leuprolide is not adequate, it may be necessary to switch to an alternative GnRH agonist with the ability for dosage adjustment.204

Discontinue therapy at the appropriate age of onset of puberty.204

Adults

Prostate Cancer
Daily Therapy with Leuprolide Acetate Injection
Sub-Q

1 mg daily.1

Dosages up to 20 mg daily have been used by some clinicians; however, dosages >1 mg daily have not resulted in a greater incidence of remission.1 2 10 22 23 33

Therapy with Long-acting Formulations
IM

Lupron Depot: 7.5 mg once monthly (every 4 weeks) as the monthly formulation, 22.5 mg every 12 weeks as the 3-month formulation, 30 mg every 16 weeks as the 4-month formulation, or 45 mg once every 24 weeks as the 6-month formulation.190

Sub-Q

Eligard: 7.5 mg once monthly, 22.5 mg once every 3 months, 30 mg once every 4 months, or 45 mg once every 6 months.192

Camcevi: 42 mg once every 6 months.205

Endometriosis
Initial Treatment
IM

Lupron Depot: 3.75 mg once monthly as the monthly formulation for 1 to 6 doses (maximum treatment duration of 6 months)116 or 11.25 mg every 3 months as the 3-month formulation for 1 to 2 doses (maximum treatment duration of 6 months).191 Administer with or without norethindrone acetate (5 mg daily).116 191

Retreatment after Initial Treatment

Retreatment with additional courses of leuprolide alone is not recommended; if retreatment is considered, administer a single 6-month course of leuprolide acetate suspension in conjunction with norethindrone acetate (and elemental calcium 1 g daily) after assessment of bone mineral density (BMD).116 191

Treatment should not exceed 12 months due to concerns about adverse impact on bone mineral density.116 191

Uterine Leiomyomata
IM

Lupron Depot: 3.75 mg once monthly as the monthly formulation for up to 3 consecutive months in conjunction with iron therapy.116

Lupron Depot: 11.25 mg of the 3-month formulation as a single injection in conjunction with iron therapy.191

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.1 116 155 191 192 204 205

Renal Impairment

No specific dosage recommendations at this time.1 116 155 191 192 204 205

Detailed Leuprolide dosage information

Cautions for Leuprolide Acetate, Leuprolide Mesylate

Contraindications

Warnings/Precautions

Warnings

Initial Flare of Symptoms

Transient increases in serum testosterone (in men) or estrogen (in women) can occur.1 10 32 33 35 108 115 116 145 146 155 190 191 192 May result in worsening (flare) of signs and/or symptoms (e.g., increased bone pain) of hormone-dependent disease (e.g., endometriosis, prostatic carcinoma, central precocious puberty) during initial 1–2 weeks of therapy; generally subsides during continued therapy.1 10 32 33 35 108 115 116 145 146 155 190 191 192 In pediatric patients, this can cause an increase in signs and symptoms of puberty, such as vaginal bleeding, during first weeks of therapy or after subsequent doses.155 204

Risk of spinal cord compression, which may contribute to paralysis with or without fatal complications and/or ureteral obstruction (dysuria, hematuria), in men with prostate cancer.1 82 145 190 192 205 192 Following first dose of leuprolide for treatment of endometriosis, uterine leiomyomata, or central precocious puberty, sex steroids may temporarily rise; therefore, an increase in symptoms may be observed during initial days of therapy.116 155 204

Metabolic Changes

Possible metabolic changes such as hyperglycemia, diabetes mellitus, hyperlipidemia, and non-alcoholic fatty liver disease in patients receiving GnRH agonists for treatment of prostate cancer.1 190 192 205

Monitor for changes in serum lipids, blood glucose, and/or HbA1c in patients receiving leuprolide for treatment of prostate cancer.1 190 192 205 Manage metabolic changes according to current standards of care.1 190 192 205

Cardiovascular Diseases

Possible increased risk of certain cardiovascular diseases (e.g., MI, sudden cardiac death, stroke) in patients receiving GnRH agonists, including leuprolide, for treatment of prostate cancer.1 190 192 205

Carefully evaluate patients for cardiovascular risk factors and carefully weigh benefits and risks of GnRH agonist therapy before selecting treatment for prostate cancer.1 190 192 205

Monitor patients for manifestations of cardiovascular disease during therapy; manage cardiovascular disease according to current standards of care.1 190 192 205

Effect on QT/QTc Interval

Risk of prolonged QT/QTc interval associated with androgen deprivation therapy.1 190 192 205 Carefully weigh benefits and risks of androgen deprivation therapy in patients with congenital long QT syndrome, CHF, frequent electrolyte abnormalities, and in patients receiving drugs known to prolong the QT interval.1 190 192 205 Correct any electrolyte abnormalities.1 190 192 205

Consider monitoring electrocardiograms and electrolytes periodically.1 190 192 205

Psychiatric Events

Psychiatric events, including symptoms of emotional lability (e.g., crying, irritability, impatience, anger, aggression), reported in pediatric patients receiving GnRH agonists, including leuprolide.155 204 Monitor pediatric patients receiving leuprolide for development or worsening of psychiatric symptoms during therapy.155 204

Depression may occur or worsen during therapy with GnRH agonists, including leuprolide, in female patients receiving treatment for endometriosis and/or uterine leiomyomatas.116 191 Carefully observe female patients for depression, particularly those with a history of depression, and consider whether risks of continued therapy outweigh the benefits.116 191 Refer women with new or worsening depression to a mental health professional, as appropriate.116 191

Seizures

Seizures reported with GnRH agonists, including leuprolide.116 155 190 191 192 204 205 Seizures observed in patients with or without a history of seizures, epilepsy, cerebrovascular disorders, and CNS anomalies or tumors and in patients receiving concomitant medications associated with seizures.116 155 190 191 192 204 Manage patients who experience seizures according to current standards of care.190 192 205

Pseudotumor Cerebri

Pseudotumor cerebri (idiopathic intracranial hypertension) reported in pediatric patients receiving GnRH agonists, including leuprolide.155 204 Monitor patients for signs and symptoms (e.g., headaches, papilledema, blurred vision, diplopia, loss of vision, pain behind the eye or pain with eye movement, tinnitus, dizziness, nausea).155 204

Laboratory Tests

Monitor serum levels of testosterone following administration of leuprolide in patients with prostate cancer.1 190 192 205 In the majority of patients treated with leuprolide, testosterone levels increased above baseline during first week, and then declined thereafter to castration levels (<50 ng/dL) within 4 weeks.1 190 192 205

Loss of Bone Mineral Density

Lupron Depot3.75 mg and Lupron Depot 11.25 mg induce a hypoestrogenic state resulting in loss of bone mineral density (BMD), some of which may not be reversible after treatment discontinuation.116 191 In women with major risk factors for decreased BMD (e.g., chronic alcohol use [>3 units each day], tobacco use, strong family history of osteoporosis, chronic use of medications that decrease BMD [such as anticonvulsants and corticosteroids]), use of Lupron Depot may pose an additional risk.116 191 Carefully weigh the risks and benefits of this therapy in these patients.116 191 The duration of Lupron Depottreatment is limited by the risk of loss of BMD.116 191 When using Lupron Depot for the management of endometriosis, addition of norethindrone acetate (add-back therapy) is effective in reducing BMD loss that occurs with leuprolide acetate.116 191 Do not retreat with Lupron Depot without combination norethindrone acetate.116 191 Assess BMD before retreatment.116 191

Embryo-fetal Toxicity

May cause fetal harm if administered to a pregnant female, based on data from animal reproduction studies and the drug's mechanism of action.116 190 191 192 205 Contraindicated during pregnancy; verify pregnancy status prior to initiating therapy.116 190 191 192 205 Discontinue leuprolide if female becomes pregnant during treatment and apprise of potential fetal risk.116 190 191 192 205 Advise females of reprodutive potential to notify their clinician if they become pregnant.116 190 191 192 205

Some leuprolide dosage regimens may inhibit ovulation and menstruation; however, contraception is not ensured.116 190 191 192 205 If contraception is indicated, advise females of reproductive potential to use non-hormonal methods of contraception while on therapy.116 190 191 192 205

Sensitivity Reactions

Hypersensitivity Reactions

Hypersensitivity reactions, including anaphylaxis, reported.1 116 155 190 191 192 204 205 Leuprolide is contraindicated in patients with a history of hypersensitivity to GnRH or GnRH agonist analogs.1 116 155 190 191 192 204 205 In clinical trials, adverse events of asthma were reported in women with preexisting histories of asthma, sinusitis, and environmental or drug allergies.116 191 Symptoms consistent with an anaphylactoid or asthmatic process reported during postmarketing experience.1 116 190 191 205

Specific Populations

Pregnancy

May cause fetal harm based on animal studies and the drug’s mechanism of action.1 116 155 190 191 192 204 205 Discontinue leuprolide if pregnancy occurs during treatment and inform patient of potential risk to fetus.116 191 Contraindicated in pregnant females.116 155 191 204

Lactation

No data on presence of leuprolide in either animal or human milk, the effects on breastfed infants, or the effects on milk production.116 191 204 Consider developmental and health benefits of breastfeeding along with the mother's clinical need for leuprolide and any potential adverse effects on the breastfed infant from leuprolide or from the underlying maternal condition.116 191 204

Females and Males of Reproductive Potential

Exclude pregnancy in women of reproductive potential prior to initiating leuprolide if clinically indicated.116 155 191 204

When used at the recommended dose and dosing interval for the treatment of endometriosis and uterine leiomyomata, leuprolide usually inhibits ovulation and stops menstruation.116 191 Contraception, however, is not ensured by taking leuprolide.116 155 191 204 If contraception is indicated, advise women to use nonhormonal methods of contraception while on treatment with leuprolide.116 191 204

Continuous leuprolide therapy may impair fertility in males as a result of the drug’s pharmacologic effects.5 6 7 8 12 13 88 116 190 Continuous leuprolide therapy may also impair fertility in females as a result of decreased gonadotropin release and subsequent inhibition of estrogen production, ovulation, and corpus luteum formation.5 88 116 191 Clinical and pharmacologic studies in adults receiving leuprolide acetate and similar analogs have shown reversibility of fertility suppression when the drugs were discontinued after continuous administration for periods of up to 24 weeks.116 155 191 204

Pediatric Use

Safety and effectiveness of leuprolide acetate depot suspension for treatment of central precocious puberty (Lupron Depot-Ped) established in pediatric patients ≥1 year of age.155 Safety and effectiveness of leuprolide acetate for injectable suspension for treatment of central precocious puberty (Fensolvi) established in pediatric patients ≥2 years of age.204

Geriatric Use

Safety and efficacy established in older adult male patients for treatment of prostate cancer; in clinical trials, majority of patients were ≥65 years of age.1 190 192 205

Not indicated in postmenopausal women and not studied in this population.116 191

Hepatic Impairment

Pharmacokinetics in patients with impaired hepatic function not determined to date.1 116 155 191 192 204 205

Renal Impairment

Pharmacokinetics in patients with impaired renal function not determined to date.1 116 155 191 192 204 205

Common Adverse Effects

Adverse reactions (≥10%) in males receiving leuprolide for treatment of prostate cancer: Hot flashes/sweats, general pain, hypertension, testicular atrophy, injection site reaction, GI disorders, joint disorders, musculoskeletal pain, urinary disorder, lethargy/fatigue.1 190 192 205

Adverse reactions (≥10%) in females receiving leuprolide for treatment of endometriosis and uterine leiomyomata: Hot flashes/sweats, headache, vaginitis, depression/emotional lability, general pain, asthenia, weight gain/loss, nausea/vomiting, decreased libido, dizziness, constipation, diarrhea, acne, skin reactions.116 191

Adverse reactions (≥10%) in pediatric patients receiving leuprolide for treatment of CPP: Injection site reactions (including pain), nasopharyngitis, pyrexia, headache, psychiatric events, cough.155 204

Drug Interactions

No formal drug interaction studies to date.1 116 155 191 192 204

Metabolism does not involve CYP isoenzymes;1 116 155 191 pharmacokinetic interactions associated with CYP isoenzymes are therefore unlikely to occur.1 116 155 191

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

Antiandrogens (e.g., flutamide, bicalutamide, nilutamide)

Potential additive antineoplastic effects by producing complete androgen withdrawal49 102 111 125 140 141 142 143

Used concomitantly in prostate cancer for additive therapeutic effect195 200

Tests, diagnostic tests of pituitary gonadotropic and gonadal function

Due to suppression of the pituitary-gonadal system by leuprolide, results of diagnostic tests of pituitary gonadotropic and gonadal functions conducted during and after therapy may be affected190 192
Leuprolide drug interactions (more detail)

Leuprolide Acetate, Leuprolide Mesylate Pharmacokinetics

Absorption

Not active when administered orally.116 155 190 191

Leuprolide acetate injection is rapidly and well absorbed following sub-Q administration.1 29

Peak plasma concentrations usually attained within 4 hours following IM administration of depot suspension (Lupron Depot) in prostate cancer patients and in female patients.116 190

Peak plasma concentrations usually attained 3.3–5 hours following sub-Q administration of long-acting injectable suspension (Eligard) in prostate cancer patients.192

Following IM administration of the long-acting depot suspension (Lupron Depot) or sub-Q administration of the injectable suspension (Eligard, Fensolvi) or emulsion (Camcevi), the drug is released slowly and gradually from its biodegradable copolymer-containing vehicle.101 116 155 117 118 190 192

Onset

Serum testosterone concentrations reach castrate levels 2–4 weeks following administration of leuprolide acetate injection or the depot suspension (Lupron Depot).190

Onset of estradiol suppression occurs 4–28 days following IM administration of a single 11.25-mg dose of the long-acting injectable suspension in healthy women;191 mean estradiol concentration is in the menopausal range 21 days following administration.191

Distribution

Extent

Not known whether leuprolide crosses the placenta or is distributed into milk.82 116 155 191

Plasma Protein Binding

Leuprolide acetate injection: 43–49%.1 116 155 190 191 192 204 205

Elimination

Metabolism

Metabolized mainly by peptidase to several metabolites;116 155 major metabolite (M-I) is inactive.1 116 191 192

Elimination Route

Following IM administration of leuprolide acetate injectable suspension (3.75 mg), <5% of dose recovered in urine as parent drug and M-I metabolite.116

Half-life

Approximately 3 hours following IV administration of leuprolide acetate (based on a 2-compartment model).1 82 155 190 205

Special Populations

Pharmacokinetics in patients with impaired renal or hepatic function not studied.1 116 155 191 192 204 205

Stability

Storage

Sub-Q

Injection Solution

<25°C;1 do not freeze.1 Protect from light; store vial in carton until time of use.1

Injectable Suspension (Eligard and Fensolvi)

2–8°C.192 204 Once outside the refrigerator, may store in original packaging, at 15–30°C for up to 8 weeks prior to reconstitution and administration.192 204

Suspension in polymeric delivery system should not be stored for >30 minutes after mixing;192 discard if suspension not administered within 30 minutes.192

Injectable Emulsion (Camcevi)

2–8°C.205 Store in carton until time of use and protect from light; do not freeze or shake.205

IM

Depot Suspension (Lupron Depot or Lupron Depot-Ped)

20–25°C (excursions permitted to 15–30°C). 116 155 190 191

Actions

Advice to Patients

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Leuprolide Acetate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

For depot suspension, for IM injection

3.75 mg

Lupron Depot (available as prefilled dual-chambered syringes)

AbbVie

7.5 mg

Lupron Depot (available as prefilled dual-chambered syringes)

AbbVie

Lupron Depot-Ped (available as prefilled dual-chambered syringes)

AbbVie

11.25 mg

Lupron Depot (available as prefilled dual-chambered syringes)

AbbVie

Lupron Depot-Ped (available as prefilled dual-chambered syringes)

AbbVie

15 mg

Lupron Depot-Ped (available as prefilled dual-chambered syringes)

AbbVie

22.5 mg

Lupron Depot (available as prefilled dual-chambered syringes)

AbbVie

30 mg

Lupron Depot (available as prefilled dual-chambered syringes)

AbbVie

Lupron Depot-Ped (available as prefilled dual-chambered syringes)

AbbVie

45 mg

Lupron Depot (available as prefilled dual-chambered syringes)

AbbVie

Lupro

For injectable suspension, for subcutaneous use

45 mg

Eligard

Tolmar Pharmaceuticals

Fensolvi

Tolmar Pharmaceuticals

Injection, for subcutaneous use

5 mg/mL*

Leuprolide Acetate Injection
Leuprolide Mesylate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injectable emulsion, for subcutaneous use

42 mg (of leuprolide)

Camcevi (available as a prefilled syringe)

Foresee Pharmaceuticals

AHFS DI Essentials™. © Copyright 2025, Selected Revisions July 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

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13. Labrie F, Cusan L, Seguin C et al. Antifertility effects of LHRH agonists in the male rat and inhibition of testicular steroidogenesis in man. Int J Fertil. 1980; 25:157-70. https://pubmed.ncbi.nlm.nih.gov/6108924

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