Endocrine Drugs Flashcards
Somatropin/somatotropin
Recombinant form of GH. Acts at GH-R to increase IGF1
USE: GH deficiency, increase final height in individuals with short stature from other causes
TOXICITIES:
-Children –> pseudomotor cerebir, scoliosis progression, edema, hyperglycemia (insulin resistance induction)
-Adults –> peripheral edema, myalgiam arthralgia, carpal tunnel
Mescasermin
Recombinant IGF1
USE: IGF1 replacement for IGF1 deficiency assoicated with GH resistance
Toxicities:
hypoglycemia (potentiates insulin)
Octreotide
Lanreotide
Somatostatin analogs –> inhibit GH production
USE: acromegaly, (GH secreting tumor), carcinoid syndrome, gastrinoma, glucagonoma, esophageal varices
Toxicity: N/V, abdominal cramps, gallstones, sinus bradycardia, conduction disturbances
Pegvisomant
GH-R antagonist
USE: acromegaly
Tolerated very well
urofollitropin
follitropin alpha and beta
FSH receptor agonists
USES:
women - controlled ovarian hyperstimulation in IVF, ovulation stimulation if patients dont respond to other agents
me - infertility due to hypogonadism
Toxicity:
Ovarian hyperstimulation syndrome (OHSS)
Multiple pregnancies
Lutropin alpha
LH-R agonist Use - ovarian hyperstimulation procedures for stimulation of follicle development in infertile women with profound LH deficiency Toxicity: Ovarian hyperstimulation syndrome (OHSS) Multiple pregnancies
Choriogonadotropin alpha
Agonist at LH-R (hCG analog)
USES:
women - controlled ovarian hyperstimulation in IVF, ovulation stimulation if patients dont respond to other agents
me - infertility due to hypogonadism
Toxicity:
Ovarian hyperstimulation syndrome (OHSS)
Multiple pregnancies
Leuprolide
GnRH receptor agonist
Effect: increases LH and FSH secretion with intermittent administration, decreases LH and FSH secretion with prolonged continuous administration
Uses: (all continuous admin)
-ovarian suppression during controlled ovarian hyperstimulation procedures
-Endometriosis
-Uterine fibroids
-Prostate cancer
-Central precocious puberty
Toxicities:
-hypoestrogenic symptoms (hot flash, sweat, headache, vaginal dryness, dyspareunia, decreased libido, mood swings, depression, UTIs, reduced bone density)
-Men -hot flashes, edema, gynecomastia, decreased hematocrit, asthenia
Goserelin
Histrelin
Nafarelin
Triptorelin
GnRH receptor agonist
Effect: increases LH and FSH secretion with intermittent administration, decreases LH and FSH secretion with prolonged continuous administration
Uses: (all continuous admin)
-ovarian suppression during controlled ovarian hyperstimulation procedures
-Endometriosis
-Uterine fibroids
-Prostate cancer
-Central precocious puberty
Toxicities:
-hypoestrogenic symptoms (hot flash, sweat, headache, vaginal dryness, dyspareunia, decreased libido, mood swings, depression, UTIs, reduced bone density)
-Men -hot flashes, edema, gynecomastia, decreased hematocrit, asthenia
Ganirelix
Cetrorelix
GnRH receptor antagonist –> reduces LH and FSH production
Use: prevention of premature LH surges during controlled ovarian hyperstimulation procedures
Toxicity: lower rish of OHSS, but greater risk of severe hypoestrogenic effects with prolonged use
Degarelix
GnRH receptor antagonist –> reduces LH and FSH production
Use: symptomatic advanced prostate cancer
Toxicity: androgen deprivation (hot flashes, edema)
Elagolix
GnRH receptor antagonist –> reduces LH and FSH production
Use: moderate-severe endometriosis pain
Toxicity: decreased risk of hypoestrogenic effects
Bromocriptine
Dopamine D2 receptor agonist
Suppresses pituitary release of prolactin
Use: hyperprolactinemia
Toxicity: psychiatric manifestations (may take months to resolve), Nausea (lessened by vaginal admin), headache, light-headedness
Cabergoline
Dopamine D2 receptor agonist
Suppresses pituitary release of prolactin
Use: hyperprolactinemia
Toxicity: Cardiac valvulopathy, psychiatric manifestations (may take months to resolve), Nausea (lessened by vaginal admin), headache, light-headedness
Oxytocin (pitocin)
agonist at oxytocin receptors which increases uterine contractions
USE: induction/augmentation of labor, uterine hemorrhage control (following delivery)
Toxicities:
-Fetal distress, placental abruption, or uterine rupture if excessive
-CI if fertal distress, abnormal fetal rpesentaiton, or predisposed to uterine rupture
-inadvertent activation of vasopressin receptors –> fluid retention, HF, seizures
Desmopressin acetate
Selective agonist at vasopressin (ADH) V2 receptor which decreases kidney excretion of H2O. Also increase release of factor 8 and vWF
Use: Central Diabetes Insipidus (given intranasally every 12-24 hours - ameliorates polyuria and polydipsia), von willebrand disease, sleep enuresis, hemophilia A
Toxicity: rare - headache, nausea, abdominal cramps, agitation, allergic reaction
Conivaptan
Antagonists at vasopressin receptors
Promote renal excretion of H2O (diuresis)
Use: SIADH, reduce symtpoms of excessive ADH release in hyponatremia, HF
Toxicity: infusion site reactions
Tolvaptan
Antagonists at vasopressin receptors
Tolvaptan is mroe selective for V2 receptor
Promote renal excretion of H2O (diuresis)
Use: SIADH, reduce symtpoms of excessive ADH release in hyponatremia, HF
Toxicity: risk of hepatotoxicity - treatment limited to 30 days
hydrocortisone cortisone prednisone prednisolone dexamethasone
-mechanism and effects
MECHANISM: acts through GC receptor and GC receptor elements on DNA. regulate transcription of many genes
EFFECTS:
Metabolic - hyperglycemia, fat deposition
Catabolic - muscle protein catabolism, wasting in lymphoid and connective tissue, fat, and skin
Immunosuppressive- inhibit the function of macrophages and other APCs
Anti-inflammatory - affects distribution and function of leukocytes, suppress inflammatory cytokines and chemokines
hydrocortisone cortisone prednisone prednisolone dexamethasone
clinical indications (adrenal disorders only), primary toxicities
- Replacement therapy in Addison’s disease (primary adrenocortical insufficiency)
- Replacement therapy in Congenital Adrenal Hyperplasia
Toxicities:
- protein catabolism–>growth retardation, osteoporosis, muslce wasting, thinning of skin + purpura, poor wound healing
- Fat metabolism –>central obesity (redistribution)
- Hyperglycemia, DM
- Other - depression, anxiety, hypomania, insomnia, glaucoma, cataracts
Androgenic effects- hirsutism, sweating, acne
fludrocortisone
MECHANISM: MC-Receptor and effects MC receptor elements on DNA to regulate transcription - so in nucleus
EFFECT: maintain plasma volume and blood pressure
CLINICAL INDICATION: -Replacement therapy in Addison’s disease (primary adrenocortical insufficiency)
and Congenital Adrenal Hyperplasia
TOXICITY: Hypertension, hypokalemia, metabolic alkalosis
Ketoconazole
MECHANISM: adrenal steroid biosynthesis inhibitor - inhibits P450C17, C17, 20-lyase, 3B-hydroxy-steroid dehydrogenase, P450C11
EFFECT: selectively inhibit production of cortisol and aldosterone
CLINICAL INDICATION: treatment of inoperable recurrent, or persistent Cushing’s disease
TOXICITY: Hepatotoxicity, GI upset
Metyrapone
MECHANISM: adrenal steroid biosynthesis inhibitor - selectively inhibits P450C11
EFFECT: inhibit production of cortisol and aldosterone
CLINICAL INDICATION: treatment of inoperable recurrent, or persistent Cushing’s disease
TOXICITY: Blood pressure and electrolyte abnormalities, adronergic effects
Mitotane
MECHANISM: adrenal steroid biosynthesis inhibitor - inhibits P450C11
EFFECT: non-selectively inhibit production of cortisol and aldosterone
CLINICAL INDICATION: treatment of inoperable recurrent, or persistent Cushing’s disease
TOXICITY: CNS disturbances, somnolence, lethargy
GI upset + diarrhea
