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Worksheets[PHARM] Endo 1 GnRH drugs
Total questions: 27
Worksheet time: 14mins
• Acetate salt of synthetic human GnRH
• Administered IV or SQ
• Half-life (IV): 4 minutes
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
• Female infertility
- Used to initiate an LH surge and ovulation induction with gonadotropins
Dosing
• 2.5 μg/pulse IV or SQ every 120 minutes
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
• Male infertility
- For infertility in men with hypothalamic hypogonadotropic hypogonadism
Dosing
• Portable pump infuses IV every 90 minutes
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Adverse effects
• Headache, lightheadedness, nausea, flushing
• Local swelling a SQ injection sites, generalized
hypersensitivity dermatitis (long-term SQ administration)
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Adverse effects
• Sudden pituitary apoplexy and blindness with patients that have gonadotropin-secreting tumors
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
• Substitution of amino acids at the 6 position or replacement of the C-terminal glycine-amide produces synthetic agonists
• More potent and longer-lasting
Gonadorelin
Synthetic GnRH analogs
Native GnRH
Synthetic GnRH analogs
• IV and SQ
Goserelin
Nafarelin
Triptorelin
Synthetic GnRH analogs
• Intranasal
Goserelin
Nafarelin
Triptorelin
Synthetic GNRH analogs
• SQ or IM monthly or every 3 months
Goserelin
Nafarelin
Triptorelin
Indications
• Controlled Ovarian Stimulation
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin,and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
• Controlled Ovarian Stimulation
- Daily SQ injections with 0.1 mg daily for 10 days or until menstrual bleeding occurs
- Dose is then reduced to 0.5 mg daily until hCG is administered
Leuprolide
Nafarelin
Goserelin
Histrelin
Indications
• Controlled Ovarian Stimulation
- Daily nasal application initiated with 400 μg twice daily
- Decreased to 200 μg when menstrual bleeding
occurs
Leuprolide
Nafarelin
Goserelin
Histrelin
Indications
• Endometriosis
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
• Uterine Leiomyomata
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
• Prostate Cancer
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
- Precipitate pain in patients with bone metastases
- Precipitate tumor growth and neurologic symptoms in patients with vertebral metastases
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
- Temporarily worsen symptoms of urinary obstruction
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide, Goserelin, Histrelin, and Triptorelin
Indications
• Central Precocious Puberty
- Treatment is generally continued to age 11 in females and age 12 in males
Gonadorelin
Leuprolide and Nafarelin
Leuprolide, Goserelin, and Nafarelin
Leuprolide and Histrelin
Adverse effects
• In women: typical symptoms of menopause
• Reduced bone density and osteoporosis in prolonged use
• In men:
- Hot flushes and sweats
- Edema
- Gynecomastia
- Decreased libido
- Decreased hematocrit
- Reduced bone density
- Asthenia
- Injection site reactions
Gonadorelin
Synthetic GnRH analogs
Native GnRH
Adverse effects
• May cause or aggravate sinusitis
Gonadorelin
Leuprolide
Nafarelin
Goserelin
Indications
• Approved for use in ovarian stimulation procedures
• Well tolerated when used for controlled ovarian stimulation
• Absorbed rapidly after subcutaneous (SQ) injection
Ganrelix and Cetrorelix
Degarelix and Abarelix
Leuprolide and Nafarelin
Adverse effects
• Nausea
• Headache
Ganrelix and Cetrorelix
Degarelix and Abarelix
Leuprolide and Nafarelin
Indications
• Approved for men with advanced prostate cancer
Ganrelix and Cetrorelix
Degarelix and Abarelix
Leuprolide, and Nafarelin
Indications
• Approved for men with advanced prostate cancer
- Initiated with 240mg administered 2 SQ injections
- Maintenance dosing: 80mg SQ injection every 28 days
Ganrelix
Cetrorelix
Degarelix
Abarelix
Indications
• Approved for men with advanced prostate cancer
- Initiated with 100mg IM every 2 weeks for 3 doses and every 4 weeks thereafter
Ganrelix
Cetrorelix
Degarelix
Abarelix
Adverse effects
• Continuous use lead to signs and symptoms of androgen deprivation such as hot flushes and weight gain
Ganrelix and Cetrorelix
Degarelix and Abarelix
Leuprolide and Nafarelin
Adverse effects
• Caused injection site reactions and increases liver enzymes during treatment of men with prostate cancer
Ganrelix
Cetrorelix
Degarelix
Abarelix
