Leuprolide

Leuprolide Brand Names

Eligard | Fensolv | Lupron | Lupron Depot | Lupron Depot-Ped | Viadur

What is Leuprolide

Leuprolide is a synthetic analog of naturally occurring gonadotropin-releasing hormone (GnRH).

Leuprolide is similar in activity and indications to goserelin. Leuprolide is used as a hormonal antagonist in the treatment of advanced prostatic cancer, and as hormonal therapy in the treatment of endometriosis and uterine fibroids.

Leuprolide injection is designated as an orphan drug for the treatment of precocious puberty.

Lupron Depot-Ped, a prefilled dual-chamber syringe that delivers leuprolide acetate over 1 to 3 months, is indicated for the treatment of children with central precocious puberty.

Fensolvi is a sterile polymeric matrix formulation of leuprolide acetate, administered by subcutaneous injection, that is indicated for the treatment of children with central precocious puberty. It delivers the drug at a controlled rate over 6 months.

Eligard is a sterile polymeric matrix formulation of leuprolide acetate, administered by subcutaneous injection, that delivers the drug at a controlled rate over a specific time period.

Three formulations of Eligard have been approved by the FDA for the palliative treatment of advanced prostate cancer that deliver leuprolide acetate over 1 to 6 months.

Indications

  1. benign prostatic hyperplasia (BPH)
  2. breast cancer
  3. endometriosis
  4. fertility preservation
  5. infertility
  6. precocious puberty
  7. premenstrual syndrome (PMS)
  8. prostate cancer
  9. stuttering priapism
  10. uterine leiomyomata

For the treatment of benign prostatic hyperplasia (BPH)

Side Effects

  1. abdominal pain
  2. acneiform rash
  3. agitation
  4. alopecia
  5. amblyopia
  6. amenorrhea
  7. amnesia
  8. anaphylactoid reactions
  9. anemia
  10. angina
  11. anorexia
  12. anxiety
  13. appetite stimulation
  14. arrhythmia exacerbation
  15. arthralgia
  16. asthenia
  17. atrial fibrillation
  18. back pain
  19. bladder spasm
  20. blurred vision
  21. bone fractures
  22. bone pain
  23. bradycardia
  24. breast enlargement
  25. chills
  26. colitis
  27. confusion
  28. constipation
  29. cough
  30. dehydration
  31. depression
  32. diabetes mellitus
  33. diarrhea
  34. dizziness
  35. dysgeusia
  36. dysmenorrhea
  37. dyspepsia
  38. dysphagia
  39. dysphonia
  40. dyspnea
  41. dysuria
  42. ecchymosis
  43. edema
  44. elevated hepatic enzymes
  45. emotional lability
  46. eosinophilia
  47. epididymitis
  48. epistaxis
  49. eructation
  50. erythema
  51. erythema multiforme
  52. euphoria
  53. fatigue
  54. feminization
  55. fever
  56. flatulence
  57. GI bleeding
  58. GI obstruction
  59. gingivitis
  60. goiter
  61. growth inhibition
  62. gynecomastia
  63. hallucinations
  64. headache
  65. hearing loss
  66. heart failure
  67. hematoma
  68. hematuria
  69. hemoptysis
  70. hepatitis
  71. hepatomegaly
  72. hiccups
  73. hot flashes
  74. hyperesthesia
  75. hyperglycemia
  76. hyperhidrosis
  77. hyperlipidemia
  78. hyperphosphatemia
  79. hyperreflexia
  80. hypertension
  81. hyperuricemia
  82. hypokalemia
  83. hyporeflexia
  84. hypotension
  85. hypoxia
  86. impaired wound healing
  87. impotence (erectile dysfunction)
  88. increased urinary frequency
  89. infection
  90. influenza
  91. injection site reaction
  92. insomnia
  93. lethargy
  94. leukopenia
  95. libido decrease
  96. libido increase
  97. lymphadenopathy
  98. malaise
  99. mastalgia
  100. melasma
  101. memory impairment
  102. muscle cramps
  103. muscle paralysis
  104. musculoskeletal pain
  105. myalgia
  106. myocardial infarction
  107. myopathy
  108. nasal congestion
  109. nausea
  110. nephrolithiasis
  111. new primary malignancy
  112. night sweats
  113. nocturia
  114. osteopenia
  115. osteoporosis
  116. ovarian enlargement
  117. ovarian hyperstimulation syndrome (OHSS)
  118. palpitations
  119. paresthesias
  120. parosmia
  121. peptic ulcer
  122. peripheral edema
  123. peripheral neuropathy
  124. pharyngitis
  125. phlebitis
  126. photosensitivity
  127. pituitary apoplexy
  128. pleural effusion
  129. prostate pain
  130. ptosis
  131. pulmonary edema
  132. pulmonary embolism
  133. pulmonary fibrosis
  134. purpura
  135. pyuria
  136. QT prolongation
  137. rash
  138. rectal fistula
  139. renal tubular obstruction
  140. rhinitis
  141. rhinorrhea
  142. seborrhea
  143. seizures
  144. sinus tachycardia
  145. sinusitis
  146. skin hyperpigmentation
  147. skin hypopigmentation
  148. skin irritation
  149. skin ulcer
  150. stroke
  151. suicidal ideation
  152. syncope
  153. synovitis
  154. testicular atrophy
  155. testicular pain
  156. thrombocytopenia
  157. thromboembolism
  158. thrombosis
  159. tinnitus
  160. tremor
  161. urinary incontinence
  162. urinary retention
  163. urinary urgency
  164. urticaria
  165. vaginal bleeding
  166. vaginal discharge
  167. vaginitis
  168. vertigo
  169. visual impairment
  170. vomiting
  171. weakness
  172. weight gain
  173. weight loss
  174. wheezing
  175. xerophthalmia
  176. xerosis
  177. xerostomia

Monitoring Parameters

  • blood glucose
  • blood pressure
  • glycosylated hemoglobin A1c (HbA1c)
  • prostate-specific antigen (PSA)
  • serum gonadotropin concentrations
  • serum testosterone concentrations

Contraindications

  • apheresis
  • AV block
  • benzyl alcohol hypersensitivity
  • bradycardia
  • brain tumor
  • breast-feeding
  • cardiac disease
  • cardiomyopathy
  • celiac disease
  • cerebrovascular disease
  • children
  • contraception requirements
  • depression
  • diabetes mellitus
  • dysfunctional uterine bleeding
  • females
  • fever
  • geriatric
  • Gonadotropin-Releasing Hormone (GnRH) analogs hypersensitivity
  • heart failure
  • human immunodeficiency virus (HIV) infection
  • hypercholesterolemia
  • hyperglycemia
  • hyperparathyroidism
  • hypertension
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypothermia
  • hypothyroidism
  • long QT syndrome
  • menstruation
  • myocardial infarction
  • obesity
  • osteopenia
  • osteoporosis
  • pheochromocytoma
  • pituitary insufficiency
  • pregnancy
  • pregnancy testing
  • QT prolongation
  • renal impairment
  • rheumatoid arthritis
  • seizure disorder
  • sickle cell disease
  • sleep deprivation
  • spinal cord compression
  • stroke
  • suicidal ideation
  • systemic lupus erythematosus (SLE)
  • tobacco smoking
  • urinary tract obstruction
  • vaginal bleeding

Interactions

  • Aclidinium; Formoterol
  • Albuterol
  • Albuterol; Ipratropium
  • Alfuzosin
  • Amiodarone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amoxapine
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Anagrelide
  • Androgens
  • Apomorphine
  • Arformoterol
  • Aripiprazole
  • Arsenic Trioxide
  • Artemether; Lumefantrine
  • Asenapine
  • Atomoxetine
  • Azithromycin
  • Bedaquiline
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Brexpiprazole
  • Budesonide; Formoterol
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Cariprazine
  • Ceritinib
  • Chloroquine
  • Chlorpromazine
  • Ciprofloxacin
  • Cisapride
  • Citalopram
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  • Clofazimine
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  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Crizotinib
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  • Dasatinib
  • Desflurane
  • Desipramine
  • Deutetrabenazine
  • Dextromethorphan; Promethazine
  • Dextromethorphan; Quinidine
  • Disopyramide
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  • Dolasetron
  • Dolutegravir; Rilpivirine
  • Donepezil
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  • Doxepin
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  • Eliglustat
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  • Encorafenib
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  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluoxymesterone
  • Fluphenazine
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Fluvoxamine
  • Formoterol
  • Formoterol; Mometasone
  • Foscarnet
  • Gemifloxacin
  • Gemtuzumab Ozogamicin
  • Gilteritinib
  • Glasdegib
  • Glycopyrrolate; Formoterol
  • Granisetron
  • Halogenated Anesthetics
  • Haloperidol
  • Halothane
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydroxychloroquine
  • Hydroxyzine
  • Ibutilide
  • Iloperidone
  • Imipramine
  • Indacaterol
  • Indacaterol; Glycopyrrolate
  • Inotuzumab Ozogamicin
  • Isoflurane
  • Itraconazole
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  • Ketoconazole
  • Lapatinib
  • Lefamulin
  • Lenvatinib
  • Levalbuterol
  • Levofloxacin
  • Lithium
  • Lofexidine
  • Long-acting beta-agonists
  • Loperamide
  • Loperamide; Simethicone
  • Lopinavir; Ritonavir
  • Lorcaserin
  • Loxapine
  • Macimorelin
  • Maprotiline
  • Mefloquine
  • Meperidine; Promethazine
  • Metaproterenol
  • Methadone
  • Methyldopa
  • Methyltestosterone
  • Metoclopramide
  • Metronidazole
  • Midostaurin
  • Mifepristone
  • Mirtazapine
  • Molindone
  • Moxifloxacin
  • Nandrolone Decanoate
  • Nilotinib
  • Nortriptyline
  • Octreotide
  • Ofloxacin
  • Olanzapine
  • Olodaterol
  • Ondansetron
  • Osilodrostat
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  • Oxaliplatin
  • Oxandrolone
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  • Ozanimod
  • Paliperidone
  • Panobinostat
  • Pasireotide
  • Pazopanib
  • Pentamidine
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenylephrine; Promethazine
  • Pimavanserin
  • Pimozide
  • Pirbuterol
  • Pitolisant
  • Posaconazole
  • Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
  • Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
  • Primaquine
  • Procainamide
  • Prochlorperazine
  • Promethazine
  • Propafenone
  • Protriptyline
  • Quetiapine
  • Quinidine
  • Quinine
  • Ramelteon
  • Ranolazine
  • Reserpine
  • Ribociclib
  • Ribociclib; Letrozole
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  • Risperidone
  • Romidepsin
  • Salmeterol
  • Saquinavir
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  • Sertraline
  • Sevoflurane
  • Short-acting beta-agonists
  • Siponimod
  • Solifenacin
  • Sorafenib
  • Sotalol
  • Sunitinib
  • Tacrolimus
  • Tamoxifen
  • Telavancin
  • Telithromycin
  • Terbutaline
  • Testolactone
  • Testosterone
  • Tetrabenazine
  • Thioridazine
  • Thiothixene
  • Tiotropium; Olodaterol
  • Tolterodine
  • Toremifene
  • Trandolapril; Verapamil
  • Trazodone
  • Triclabendazole
  • Tricyclic antidepressants
  • Trifluoperazine
  • Trimipramine
  • Umeclidinium; Vilanterol
  • Vandetanib
  • Vardenafil
  • Vemurafenib
  • Venlafaxine
  • Verapamil
  • Voriconazole
  • Vorinostat
  • Ziprasidone
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