Lutrate Depot (leuprolide acetate)
LHrH(GNrH) Agonist Analog Pituitary Suppressants Intramuscular Vial (EA)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Leuprolide, a synthetic nonapeptide analog of naturally occurring porcine or ovine gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin), is used as an antineoplastic agent and for its endocrine effects.
Leuprolide is a gonadotropin-releasing hormone (GnRH) analog that shares the action of the naturally occurring hormone.
Leuprolide differs structurally from naturally occurringGnRH by the presence of the d-isomer of leucine at position 6 and an ethylamide group replacing glycine at position 10. These structural modifications result in increased potency of leuprolide (in terms of luteinizing hormone release) compared with naturalGnRH. The drug does not appear to affect receptor affinity for gonadotropins.
The pharmacology of leuprolide is complex and several mechanisms of action may be involved. Repeated dosing of leuprolide results in suppression of the pituitary-gonadal system and decreased secretion of gonadotropins (e.g., follicle stimulating hormone (FSH) and luteinizing hormone (LH)), which suppresses ovarian and testicular steroidogenesis. This inhibitory effect is reversible upon discontinuance of therapy.
The drug does not appear to affect receptor affinity for gonadotropins.
Leuprolide is a peptide that is primarily metabolized by peptidase into smaller inactive peptides. Because of its polypeptide nature, leuprolide acetate is destroyed in the GI tract and, therefore, usually is administered parenterally. Following subcutaneous administration, leuprolide acetate is rapidly and almost completely absorbed.
In adults, bioavailability of leuprolide acetate following subcutaneous administration is comparable to that following IV+ administration. Bioavailability of the drug reportedly is about 94% in rats following subcutaneous administration. Following IM administration of the long-acting depot suspension (Lupron Depot(R)) or subcutaneous administration of the long-acting injectable suspension (Eligard(R), Fensolvi(R)), or emulsion (Camcevi(R)), the drug is released slowly and gradually from its biodegradable copolymer-containing vehicle (after an initial, rapid absorption of immediately available drug), thus providing a prolonged duration of action.
Plasma protein binding of leuprolide has been reported to range from 43-49%. In healthy male volunteers, the terminal elimination half-life of leuprolide following IV administration was approximately 3 hours (based on a 2-compartment model). The pharmacokinetics of leuprolide in patients with impaired renal or hepatic function have not been determined to date.
USES: Leuprolide is used to treat advanced prostate cancer. It is not a cure. Most types of prostate cancer need the hormone testosterone to grow and spread.
Leuprolide works by reducing the amount of testosterone that the body makes. This helps slow or stop the growth of cancer cells and helps relieve symptoms such as painful/difficult urination. Talk to your doctor about the risks and benefits of treatment.
Generic name: leuprolide acetate
Pronunciation: (LOO-proe-lide)
Drug class: LHrH(GNrH) Agonist Analog Pituitary Suppressants
Therapeutic class: Antineoplastics
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Lutrate Depot
Indications
The following indications are listed for Lutrate Depot:
- Advanced Prostatic Carcinoma
Also known as: Advanced Cancer Of Prostate Gland, Advanced Malignant Neoplasm Of Prostate, Advanced Prostate Cancer, Advanced Prostate Malignancy, Advanced Prostatic Cancer.
Dosing
No dosing information is available for this tab.
Leuprolide acetate is administered by subcutaneous or IM injection depending on the formulation and indication. Leuprolide acetate depot suspension (e.g., LupronDepot(R), LupronDepot-Ped(R)) is administered by IM injection. Leuprolide acetate injectable suspension (Eligard(R), Fensolvi(R)) and leuprolide acetate injection are administered by subcutaneous injection.
Leuprolide mesylate emulsion (Camcevi(R)) is administered by subcutaneous injection.
Extended-release or depot formulations of leuprolide have different release characteristics. Do not use partial syringes, a combination of syringes, or substitute other extended-release products to achieve a particular dose.
Some formulations of leuprolide are not intended for self-administration and should be administered by a healthcare professional only (e.g., Camcevi(R), Eligard(R), Fensolvi(R), Lupron(R), Lupron Depot-Ped(R)); consult the manufacturer's prescribing information for details.
Store leuprolide acetate injection at a temperature of less than 25degreesC in carton until time of use and protect from light; avoid freezing.
Store leuprolide acetate powder for injectable suspension (Lupron Depot(R), Lupron Depot-Ped(R)) and its diluent at a controlled room temperature of 25degreesC; excursions permitted to temperatures ranging from 15-30degreesC. It is not necessary to store the drug or its diluent under refrigeration;avoid freezing.
Store leuprolide acetate injectable suspension (Eligard(R) and Fensolvi(R)) at 2-8degreesC. Once outside the refrigerator,Eligard(R) and Fensolvi(R) may both be stored at 15-30degreesC in their original packaging for up to 8 weeks prior to reconstitution and administration.
Store leuprolide mesylate injectable emlusion (Camcevi(R)) at 2-8degreesC in carton until time of use and protect from light; do not freeze or shake.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed to date with leuprolide.
Metabolism of leuprolide does not involve cytochrome P-450 (CYP) isoenzymes; pharmacokinetic interactionsassociated with CYP isoenzymesare therefore unlikely to occurwith leuprolide.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to gonadotropin-releasing hormone (GnRH), GnRH analogs, or any ingredient in the respective leuprolide formulation.
*Pregnancy.
*Women with abnormal vaginal bleeding of unknown etiology.
- Pregnancy
- Atherosclerotic cardiovascular disease
- Cerebrovascular accident
- Chronic heart failure
- Congenital long QT syndrome
- Hypokalemia
- Hypomagnesemia
- Prolonged QT interval
- Diabetes mellitus
- Disease of liver
- Hypercholesterolemia
- Hypertension
- Obesity
- Osteopenia
- Seizure disorder
- Tobacco smoker
- Urinary tract obstruction
- Vertebral metastases
Adverse reactions
Common adverse reactions occurring in >10% of males receiving leuprolide for the treatment of prostate cancer include hot flashes/sweats, general pain, hypertension, testicular atrophy, injection site reaction, GI disorders, joint disorders, musculoskeletal pain, urinary disorder, and lethargy/fatigue.
Common adverse reactions occurring in >10% of females receiving leuprolide for the treatment of endometriosis and uterine leiomyomata include hot flashes/sweats, headache, vaginitis, depression/emotional lability, general pain, asthenia, weight gain/loss, nausea/vomiting, decreased libido, dizziness, constipation, diarrhea, acne, and skin reactions.
Common adverse reactions occurring in >=10% or more of pediatric patients receiving leuprolide for the treatment of centralprecocious pubertyinclude injection site reactions (includingpain), nasopharyngitis, pyrexia, headache, psychiatric events,and cough.
Less Frequent
- Infection
Rare or Very Rare
- Abnormal hepatic function tests
- Acute generalized exanthematous pustulosis
- Acute myocardial infarction
- Anaphylaxis
- Anemia
- Angina
- Asthma
- Bullous dermatitis
- Cellulitis
- Cerebrovascular accident
- Chronic heart failure
- Deep venous thrombosis
- Diabetes mellitus
- DRESS syndrome
- Drug-induced hepatitis
- Epididymitis
- Erythema multiforme
- Exfoliative dermatitis
- Fracture
- Granulocytopenic disorder
- Hemoptysis
- Hepatocellular damage
- Hepatomegaly
- Hypertension
- Hypogonadotropic hypogonadism
- Hypotension
- Idiopathic intracranial hypertension
- Injection site infection
- Injection site necrosis
- Interstitial lung disease
- Leukopenia
- Lymphadenopathy
- Neutropenic disorder
- Ophthalmoplegia
- Paralysis
- Pituitary apoplexy
- Pulmonary edema
- Pulmonary emphysema
- Pulmonary thromboembolism
- Pyelonephritis
- Seizure disorder
- Steatosis of liver
- Stevens-johnson syndrome
- Suicidal
- Suicidal ideation
- Toxic epidermal necrolysis
- Transient cerebral ischemia
More Frequent
- Abnormal vaginal bleeding
- Amenorrhea
- Depression
- Dizziness
- Drug-induced hot flash
- Dyspepsia
- Edema
- Fatigue
- Headache disorder
- Hyperhidrosis
- Malaise
- Nausea
- Pain
- Stinging of skin
- Testicular atrophy
- Upper respiratory infection
- Vaginitis
- Vomiting
- Weight gain
Less Frequent
- Acne vulgaris
- Arthralgia
- Constipation
- Erectile dysfunction
- Female hirsutism
- General weakness
- Gynecomastia
- Hypercholesterolemia
- Hypersensitivity drug reaction
- Hypertriglyceridemia
- Injection site sequelae
- Insomnia
- Libido changes
- Mastalgia
- Mood changes
- Myalgia
- Nervousness
- Paresthesia
- Tumor flare reaction
Rare or Very Rare
- Aggressive behavior
- Agitation
- Alopecia
- Anorexia
- Balanitis
- Dysphagia
- Dyspnea
- Ecchymosis
- Epistaxis
- Eructation
- Fever
- Glossitis
- Hostility
- Hyperglycemia
- Hyperkinesis
- Hypoesthesia
- Induration of skin
- Injection site abscess
- Irritability
- Lethargy
- Melanosis
- Muscle atrophy
- Non-cardiac chest pain
- Osteopenia
- Peptic ulcer
- Peripheral neuropathy
- Pharyngitis
- Skin hypertrophy
- Skin photosensitivity
- Skin rash
- Syncope
- Tenosynovitis
- Testicular pain
- Urinary incontinence
- Urinary tract infection
- Urticaria
Precautions
No enhanced messaging available.
Safety and effectiveness of leuprolide acetate depot suspension for treatment of central precocious puberty (Lupron Depot-Ped(R)) have been established in pediatric patients >=1 year of age. Safety and effectiveness of leuprolide acetate forinjectable suspension for treatment of central precocious puberty (Fensolvi(R)) have been established in pediatric patients >=2 years of age.
Leuprolide acetate injection may cause fetal harm when administered to a pregnant female based on findings from animal studies and the drug's mechanism of action. Discontinue leuprolide if pregnancy occurs during treatment and inform patients of potential risk to the fetus. Leuprolide is contraindicated in pregnant females.
Based on animal reproduction studies, leuprolide may be associated with an increased risk of pregnancy complications, including early pregnancy loss and fetal harm. In animal reproduction studies, subcutaneous administration of leuprolide acetate to rabbits during the period of organogenesis caused embryofetal toxicity, decreased fetal weights, and a dose-dependent increase in major fetal abnormalities in animals at doses less than the recommended human dose based on body surface area using an estimated daily dose. Similarstudiesin ratsshowed increased fetal mortality and decreased fetal weights but no increase infetal malformations at doses less than the recommended human dose based on body surface area using an estimated daily dose.
There are no data on the presence of leuprolide in either animal or human milk, the effects on breastfed infants, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for leuprolide and any potential adverse effects on the breastfed infant from the drug or underlying maternal condition.
Safety and efficacy of leuprolide were established in older adult male patients for the treatment of prostate cancer; in clinical trials; 69-80% of patients were >=65 years of age.
Leuprolide is not indicated in postmenopausal women and has not been studied in this population.
ICD codes
| Code | Type | Description |
|---|---|---|
| Advanced prostatic carcinoma | ||
| C61 | ICD10CM | Malignant neoplasm of prostate |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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