Endocrine Drugs Flashcards
(71 cards)
Somatotropin
Somatropin
- recombinant form of GH that acts through GH receptors to increase IGF-1 production
- restores normal growth and metabolic GH effects in GH-deficient individuals
- increases final adult height in some children with short stature not due to GH deficiency
- Primary Clinical Applications: replacement in GH deficiency; increased final adult height in children with short stature due to certain conditions
- Primary Toxicities (children): pseudotumor cerebri, progression of scoliosis, edema, hyperglycemia, risk of asphyxia and sleep apnea in obese PWS patients
- Primary Toxicities (adults): peripheral edema, myalgias, arthralgias, carpal tunnel syndrome
Mecasermin
- recombinant form of IGF-1 that stimulates IGF-1 receptors
- improves growth and metabolic IGF-1 in individuals with IGF-1 deficiency due to severe GH resistance
- Primary Clinical Application: replacement in IGF-1 deficiency that is not responsive to exogenous GH
- Toxicity: hypoglycemia
Octreotide
Lanreotide
- somatostatin (SST) analogs
- agonists at SST receptors
- inhibit production of GH
- Primary Clinical Application: acromegaly caused by GH-secreting tumors
- Toxicities: nausea, vomiting, abd cramps, flatulence, gallstones, sinus bradycardia, conduction disturbances
Pegvisomant
- GH receptor antagonist
- blocks GH receptors
- ameliorates effects of excess GH production
- Primary Clinical Application: acromegaly
- Toxicity: well tolerated
Urofollitropin
Follitropin alpha and beta
- FSH analog
- activate FSH receptors
- mimic effects of endogenous FSH
- Primary Clinical Application: controlled ovarian hyperstimulation in women; infertility due to hypogonadotropic hypogonadism in men
- Toxicities: ovarian hyperstimulation syndrome, multiple pregnancies
Lutropin alpha
- LH analog
- agonist at LH receptors
- mimics effects of endogenous LH
- Clinical Application: used in combination with follitropin alpha in controlled ovarian hyperstimulation procedures for stimulation of follicular development in infertile women with profound LH deficiency
- Toxicities: ovarian hyperstimulation syndrome, multiple pregnancies
Choriogonadotropin alpha
- hCG analog
- agonist at LH receptors
- mimics effects of endogenous LH
- Clinical Applications: controlled ovarian hyperstimulation in women; infertility due to hypogonadotropic hypogonadism in men
- Toxicities: ovarian hyperstimulation syndrome, multiple pregnancies
Leuprolide
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
Goserelin
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
Histrelin
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
Nafarelin
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
Triptorelin
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
Ganirelix, Cetrorelix, Degarelix
- GnRH antagonist
- blocks GnRH receptors
- reduces endogenous production of LH and FSH
- Clinical Application: prevention of premature LH surges during controlled ovarian hyperstimulation procedures; Degarelix is approved for treatment of symptomatic advanced prostate cancer
- continuous treatment with degarelix causes symptoms of androgen deprivation (e.g. hot flashes, edema)
Bromocriptine
- dopamine (DA) agonist
- activate dopamine D2 receptors
- suppress pituitary secretion of prolactin
- Clinical Application: treatment of prolactinemia
- Toxicities: nausea, headache, lightheadedness, orthostatic hypotension, fatigue, psychiatric manifestations
- nausea lessened by vaginal administration
Cabergoline
- dopamine (DA) agonist
- activate dopamine D2 receptors
- suppress pituitary secretion of prolactin; suppresses pituitary secretion of ACTH
- Clinical Application: treatment of prolactinemia; treatment of Cushing’s disease
- Toxicities: nausea, headache, lightheadedness, orthostatic hypotension, fatigue, psychiatric manifestations
- associated with incidence of cardiac valvulopathy
- nausea lessened by vaginal administration
Oxytocin
- activates oxytocin receptors
- increased uterine contractions
- Clinical Applications: induction and augmentation of labor; control of uterine hemorrhage after delivery
- Toxicities: excessive stimulation of uterine contractions can cause fetal distress, placental abruption, or uterine rupture; inadvertent activation of vasopressin receptors can cause fluid retention, hyponatremia, heart failure, and seizures
Vasopressin; Desmopressin
- ADH receptor agonists
- relatively selective activation of vasopressin V2 receptors
- antidiuretic effects (decreases water excretion)
- Clinical Application: treatment of diabetes insipidus
- Toxicities: overdose can cause hyponatremia and seizures; vasopressin (but not desmopressin) can cause vasoconstriction and should be used with caution in patients with CAD
Hydrocortisone (Cortisol), Cortisone, Prednisone, Prednisolone, Methylprednisolone, Betamethasone, Dexamethasone
- glucocorticoids
- act through GC receptors and GC receptor elements on DNA to regulate the transcription of numerous genes
- Effects (metabolic): hyperglycemia, fat deposition in certain anatomical locations
- Effects (catabolic): muscle protein catabolism, wasting in lymphoid and connective tissue, fat, and skin
- Effects (immunosuppressive): inhibit the functions of tissue macrophages and other antigen presenting cells
- Effects (anti-inflammatory): affect distribution and function of leukocytes, suppress inflammatory cytokines and chemokines
- Clinical Application: replacement in primary adrenocortical insufficiency (Addison’s disease); replacement in congenital adrenal hyperplasia
- Toxicities (protein catabolism): growth retardation; osteoporosis; muscle wasting; thinning of skin and purple striae (bruising); poor wound healing
- Toxicities (fat metabolism): fat redistribution with central obesity
- Toxicities (glucose metabolism): hyperglycemia; diabetes mellitus
- Toxicites (other): depression; anxiety; hypomania; insomnia; glaucoma and cataracts; hirsutism; sweating; acne
Fludrocortisone
- Mineralocorticoid (MC)
- act through MC receptors and MC receptor elements on DNA to regulate gene transcription
- Effects: promote sodium and water retention and secretion of potassium and protons in the distal tubule of the nephron; maintains plasma volume and blood pressure
- Clinical Applications: replacement in primary adrenocortical insufficiency (Addison’s disease); replacement in congential adrenal hyperplasia
- Toxicities: hypertension; hypokalemia; metabolic alkalosis
Ketoconazole
- inhibitor of adrenal steroid biosynthesis
- non-selectively inhibits the P450C17, C17, 20-lyase, 3-beta-hydroxy-steroid dehydrogenase, and P450C11 enzymes
- inhibit the production of cortisol and aldosterone
- treatment of Cushing’s syndrome/disease
- treatment of PCOS to prevent hirsuitism
- Toxicity: hepatotoxicity, gynecomastia, amenorrhea
Metyrapone
- inhibitor of adrenal steroid biosynthesis
- selectively inhibits the P450C11 enzyme
- inhibits the production of cortisol and aldosterone
- treatment of Cushing’s syndrome/disease
- Toxicity: salt and water retention, hirsutism
Mifepristone
- GC receptor antagonist
- competitively inhibits GC receptors
- ameliorates effects of excess cortisol production
- treatment of Cushing’s syndrome/disease
- Toxicity: menstrual abnormalities
Pasireotide
- somatostatin (SST) receptor agonist
- activates SST receptors
- suppresses pituitary secretion of ACTH
- treatment of Cushing’s disease
- Toxicities: nausea, diarrhea, hyperglycemia, bradycardia, conduction disturbances
Spironolactone, Eplerenone
- mineralocorticoid receptor antagonsits
- competitively inhibit MC receptors
- diuretic effects
- ameliorates effects of excess aldosterone production
- Spironolactone also inhibits steroid binding, 17-alpha-hydroxylase, and 17,20-desmolase
- treatment of aldosteronism
- Spironolactone also used to treat PCOS
- Toxicities (spironolactone): hyperkalemia, cardiac arrhythmia, menstrual abnormalities, gynecomastia, hirsutism
- Toxicities (eplerenone): hyperkalemia