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).

Uses for Leuprolide Acetate, Leuprolide Mesylate

Prostate Cancer

Treatment of advanced prostate cancer.

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. Leuprolide is also available as the mesylate salt in an injectable emulsion for sub-Q use in the treatment of advanced prostate cancer.

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

Endometriosis

Treatment of endometriosis (e.g., pain relief, reduction in endometriotic lesions [dysmenorrhea and pelvic pain, tenderness, and induration]).

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.

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

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. Total duration of leuprolide therapy plus add-back therapy should not exceed 12 months because of potential adverse impact on bone mineral density.

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.

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; used in conjunction with iron therapy.

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).

Precocious Puberty

Treatment of central precocious puberty (CPP) in pediatric patients (designated an orphan drug by FDA for this use).

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.

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

Leuprolide Acetate, Leuprolide Mesylate Dosage and Administration

General

Pretreatment Screening

Patients receiving Leuprolide for the Treatment of Prostate Cancer

• Assess potential risks in patients with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities, and in patients taking drugs known to prolong the QT interval.

Pediatric Patients receiving Leuprolide for Treatment of Precocious Puberty

• Perform height and weight evaluations; determine serum testosterone or estrogen concentrations in boys or girls, respectively.

Patients receiving Leuprolide for Treatment of Endometriosis or Uterine Leiomyomata

• Screen patients for chronic alcohol use (>3 units per day), tobacco use, strong family history of osteoporosis, or chronic use of drugs that can decrease BMD (e.g., anticonvulsants, corticosteroids).

• Exclude pregnancy prior to initiating therapy if clinically indicated.

Patient Monitoring

Patients receiving Leuprolide for the Treatment of Prostate Cancer

• Monitor serum testosterone and prostate-specific antigen (PSA) levels periodically.

• Monitor serum lipids, blood glucose, and/or glycosylated hemoglobin (hemoglobin A1c [HbA1c]) concentrations.

• Monitor for signs and symptoms suggestive of cardiovascular disease development.

• Monitor QT/QT_c interval and electrolytes.

Patients receiving Leuprolide for Treatment of Endometriosis or Uterine Leiomyomata

• Monitor for the development or worsening of depressive symptoms.

Pediatric Patients receiving Leuprolide for Precocious Puberty

• Monitor for response to therapy with a GnRH agonist stimulation test, basal luteinizing hormonel (LH) levels, or serum concentrations of sex steroids 1 to 2 months after initiating therapy and as clinically appropriate.

• Monitor height every 3 to 6 months and bone age periodically.

• Monitor for the development or worsening of psychiatric symptoms (e.g., crying, irritability, impatience, anger, aggression) during therapy.

Administration

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

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

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.

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

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. Following reconstitution, administer within 2 hours. Rotate injection sites with each injection. Consult manufacturer's prescribing information for additional details.

Sub-Q Administration

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

Leuprolide acetate for injectable suspension (Eligard): Administer by sub-Q injection to provide continuous release of drug. Reconstitute commercially available powder with supplied prefilled diluent using aseptic technique and gloves prior to administration. Allow the drug to reach room temperature prior to reconstitution; once mixed, administer within 30 minutes or discard. 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. Rotate injection sites with each injection. Consult manufacturer's prescribing information for additional details.

Leuprolide mesylate injectable emulsion (Camcevi): Administer by sub-Q injection once every 6 months. Allow to sit at room temperature for 30 minutes prior to administration. 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). Rotate injection sites with each injection. Consult manufacturer's prescribing information for additional details.

Leuprolide acetate for injectable suspension (Fensolvi): Administer by sub-Q injection once every 6 months. 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. Allow drug to reach room temperature before reconstitution. Following reconstitution, administer within 30 minutes or discard. 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. Rotate injection sites with each injection. Consult manufacturer's prescribing information for additional details.

Dosage

Available as leuprolide acetate and leuprolide mesylate; dosage expressed in terms of the salt.

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). Dosage adjustment may be necessary with changes in body weight. Select the appropriate syringe for the intended dosing frequency.

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.

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.

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

Discontinue therapy at the appropriate age of onset of puberty.

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.

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.

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

Discontinue therapy at the appropriate age of onset of puberty.

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.

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.

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

Discontinue therapy at the appropriate age of onset of puberty.

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. Discontinue treatment at the appropriate age of onset of puberty.

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.

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

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

Discontinue therapy at the appropriate age of onset of puberty.

Adults

Prostate Cancer

Daily Therapy with Leuprolide Acetate Injection

Sub-Q

1 mg daily.

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.

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.

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.

Camcevi: 42 mg once every 6 months.

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) or 11.25 mg every 3 months as the 3-month formulation for 1 to 2 doses (maximum treatment duration of 6 months). Administer with or without norethindrone acetate (5 mg daily).

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).

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

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.

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

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.

Renal Impairment

No specific dosage recommendations at this time.

Cautions for Leuprolide Acetate, Leuprolide Mesylate

Contraindications

• Known hypersensitivity to GnRH, GnRH analogs, or any ingredient in the respective leuprolide formulation.

• Pregnancy.

• Women with abnormal vaginal bleeding of unknown etiology.

Warnings/Precautions

Warnings

Initial Flare of Symptoms

Transient increases in serum testosterone (in men) or estrogen (in women) can occur. 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. 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.

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. 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.

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.

Monitor for changes in serum lipids, blood glucose, and/or HbA_1c in patients receiving leuprolide for treatment of prostate cancer. Manage metabolic changes according to current standards of care.

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.

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

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

Effect on QT/QTc Interval

Risk of prolonged QT/QT_c interval associated with androgen deprivation therapy. 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. Correct any electrolyte abnormalities.

Consider monitoring electrocardiograms and electrolytes periodically.

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. Monitor pediatric patients receiving leuprolide for development or worsening of psychiatric symptoms during therapy.

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

Seizures

Seizures reported with GnRH agonists, including leuprolide. 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. Manage patients who experience seizures according to current standards of care.

Pseudotumor Cerebri

Pseudotumor cerebri (idiopathic intracranial hypertension) reported in pediatric patients receiving GnRH agonists, including leuprolide. 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).

Laboratory Tests

Monitor serum levels of testosterone following administration of leuprolide in patients with prostate cancer. 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.

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. 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. Carefully weigh the risks and benefits of this therapy in these patients. The duration of Lupron Depottreatment is limited by the risk of loss of BMD. 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. Do not retreat with Lupron Depot without combination norethindrone acetate. Assess BMD before retreatment.

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. Contraindicated during pregnancy; verify pregnancy status prior to initiating therapy. Discontinue leuprolide if female becomes pregnant during treatment and apprise of potential fetal risk. Advise females of reprodutive potential to notify their clinician if they become pregnant.

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

Sensitivity Reactions

Hypersensitivity Reactions

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

Specific Populations

Pregnancy

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

Lactation

No data on presence of leuprolide in either animal or human milk, the effects on breastfed infants, or the effects on milk production. 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.

Females and Males of Reproductive Potential

Exclude pregnancy in women of reproductive potential prior to initiating leuprolide if clinically indicated.

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

Continuous leuprolide therapy may impair fertility in males as a result of the drug’s pharmacologic effects. 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. 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.

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. Safety and effectiveness of leuprolide acetate for injectable suspension for treatment of central precocious puberty (Fensolvi) established in pediatric patients ≥2 years of age.

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.

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

Hepatic Impairment

Pharmacokinetics in patients with impaired hepatic function not determined to date.

Renal Impairment

Pharmacokinetics in patients with impaired renal function not determined to date.

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.

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.

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

Drug Interactions

No formal drug interaction studies to date.

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

Specific Drugs and Laboratory Tests

Leuprolide Acetate, Leuprolide Mesylate Pharmacokinetics

Absorption

Not active when administered orally.

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

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

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

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.

Onset

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

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; mean estradiol concentration is in the menopausal range 21 days following administration.

Distribution

Extent

Not known whether leuprolide crosses the placenta or is distributed into milk.

Plasma Protein Binding

Leuprolide acetate injection: 43–49%.

Elimination

Metabolism

Metabolized mainly by peptidase to several metabolites; major metabolite (M-I) is inactive.

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.

Half-life

Approximately 3 hours following IV administration of leuprolide acetate (based on a 2-compartment model).

Special Populations

Pharmacokinetics in patients with impaired renal or hepatic function not studied.

Stability

Storage

Sub-Q

Injection Solution

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

Injectable Suspension (Eligard and Fensolvi)

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

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

Injectable Emulsion (Camcevi)

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

IM

Depot Suspension (Lupron Depot or Lupron Depot-Ped)

20–25°C (excursions permitted to 15–30°C).

Actions

• A synthetic nonapeptide analog of GnRH; structural modifications result in increased potency (in terms of luteinizing hormone release) compared with naturally occurring GnRH.

• A potent inhibitor of gonadotropin secretion and suppresser of ovarian and testicular steroidogenesis when given continuously; decreases release through down-regulation of GnRH receptors.

• Initially, circulating levels of LH, FSH, testosterone, dihydrotestosterone (DHT) estrone and estradiol surge transiently. Following long-term administration (generally, 2–4 weeks after initiation of therapy), produces a sustained decrease in LH and FSH secretion and a marked reduction of testicular and ovarian steroidogenesis. This inhibitory effect is reversible following discontinuation of therapy.

• Reductions in serum testosterone concentrations in males during therapy are comparable to those achieved after surgical castration (i.e., <50 ng/dL). Testicular and prostatic atrophy may occur.

• During continuous therapy, reduces serum estradiol concentrations in most premenopausal women to menopausal levels.

• Induces reductions in myometrial and leiomyomal volumes; possibly from decreased secretion of somatotropin (growth hormone) and estrogen-dependent growth factors (e.g., insulin-like growth factor I, IGF-I).

• Reduces gonadotropins in children with central precocious puberty and resultant depression of ovarian and testicular steroidogenesis may allow for normal physical and psychological growth and development. Effects appear to be reversible; pubertal development resumes following discontinuance of the drug.

Advice to Patients

• Advise patients of the risk of anaphylaxis and other hypersensitivity reactions. Advise patients to seek appropriate medical care if symptoms of hypersensitivity reactions occur.

• Advise patients that leuprolide may cause loss of bone mineral density (BMD) and that treatment is limited. Inform patients about other factors that can increase and decrease their risk of BMD loss.

• Advise patients that they may experience an increase in symptoms during the initial days of leuprolide therapy. These symptoms should dissipate with continued therapy.

• Advise patients that there is an increased risk of metabolic changes such as hyperglycemia, diabetes, hyperlipidemia, and non-alcoholic fatty liver disease with leuprolide therapy in patients with prostate cancer. Inform patients that monitoring for metabolic changes is required.

• Inform patients of the increased risk of myocardial infarction, sudden cardiac death, and stroke with leuprolide treatment. Advise patients to immediately report signs and symptoms associated with these events to their healthcare provider.

• Advise patients of the risk of QT/QT_c prolongation. Advise patients to immediately contact their healthcare provider if syncope, presyncopal symptoms, or cardiac palpitations occur.

• Advise patients that transient burning, stinging, pain, bruising, and redness may occur at the site of injection. Advise patients to contact their healthcare provider if they experience rash or severe injection site reactions.

• Advise patients that leuprolide treatment may cause impotence.

• Inform patients that leuprolide may cause infertility during treatment.

• Advise patients of the risk of new or worsening symptoms of depression while receiving leuprolide therapy. Advise patients and caregivers that emotional lability, such as crying, irritability, impatience, anger, and aggression, may occur in pediatric patients. Instruct patients and caregivers to monitor for development or worsening of psychiatric symptoms, including depression, during treatment.

• Advise patients of the risk of seizures. Inform patients to seek medical attention if seizures occur.

• Inform patients and caregivers that pseudotumor cerebri (idiopathic intracranial hypertension) has been observed in pediatric patients receiving leuprolide and to monitor for symptoms (e.g., headache and vision issues such as blurred vision, double vision, loss of vision, pain behind the eye or pain with eye movement, ringing in the ears, dizziness, nausea). Advise patients and caregivers to contact their clinician if any symptoms occur.

• Advise patients to inform their clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Advise women to inform their clinician if they are or plan to become pregnant or plan to breast-feed; advise women to avoid pregnancy and use nonhormonal contraceptive measures during therapy. Advise pregnant women of potential risk to the fetus.

• Inform patients of other important precautionary information.

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

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