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Pharmacology > Endocrine Drugs > Flashcards

Endocrine Drugs Flashcards

1
Q

Somatropin/somatotropin

A

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

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2
Q

Mescasermin

A

Recombinant IGF1
USE: IGF1 replacement for IGF1 deficiency assoicated with GH resistance
Toxicities:
hypoglycemia (potentiates insulin)

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3
Q

Octreotide

Lanreotide

A

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

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4
Q

Pegvisomant

A

GH-R antagonist
USE: acromegaly
Tolerated very well

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5
Q

urofollitropin

follitropin alpha and beta

A

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

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6
Q

Lutropin alpha

A 
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
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7
Q

Choriogonadotropin alpha

A

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

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8
Q

Leuprolide

A

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

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9
Q

Goserelin
Histrelin
Nafarelin
Triptorelin

A

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

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10
Q

Ganirelix

Cetrorelix

A

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

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11
Q

Degarelix

A

GnRH receptor antagonist –> reduces LH and FSH production
Use: symptomatic advanced prostate cancer
Toxicity: androgen deprivation (hot flashes, edema)

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12
Q

Elagolix

A

GnRH receptor antagonist –> reduces LH and FSH production
Use: moderate-severe endometriosis pain
Toxicity: decreased risk of hypoestrogenic effects

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13
Q

Bromocriptine

A

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

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14
Q

Cabergoline

A

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

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15
Q

Oxytocin (pitocin)

A

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

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16
Q

Desmopressin acetate

A

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

17
Q

Conivaptan

A

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

18
Q

Tolvaptan

A

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

19
Q 
hydrocortisone
cortisone
prednisone
prednisolone
dexamethasone

-mechanism and effects

A

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

20
Q 
hydrocortisone
cortisone
prednisone
prednisolone
dexamethasone

clinical indications (adrenal disorders only), primary toxicities

A
  • 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

21
Q

fludrocortisone

A

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

22
Q

Ketoconazole

A

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

23
Q

Metyrapone

A

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

24
Q

Mitotane

A

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

25
Q

mifepristone

A

MECHANISM: competitive inhibitor of GC receptors
EFFECT: ameliorate effects of excess cortisol production
CLINICAL INDICATION: Cushing syndrome/disease
TOXICITY: Menstrual abnormalities, hypokalemia, nausea, and fatigue

26
Q

Cabergoline

A

MECHANISM: Dopamine D2 agonist
EFFECT: suppress pituitary secretion of ACTH
CLINICAL INDICATION: Treatment of Cushing’s disease
TOXICITY: cardiac valvulopathy, orthostatic hypotension, psychiatric manifestations, headache, light-headedness

27
Q

Pasireotide

A

MECHANISM: Somatostatin receptor agonist (especially SST5 subtype expressed in piuitary adenoma)
EFFECT: Supresses pituitary secretion of ACTH
CLINICAL INDICATION: treatment of cushings disease
TOXICITY: conduction disturbances, bradycardia, hyperglycemia, diarrhea

28
Q

spironolactone

Eplerenone

A

MECHANISM: competitively inhibit MC-Receptor
EFFECT: diuretic effects and ameliorate excess aldosterone effects
CLINICAL INDICATIONS: treatment of aldosteronism
TOXICITY:
-Spironolactone–>hyperkalemia, cardiac arrhythmia, menstrual abnormalities, gynecomastia
-Eplerenone–>hyperkalemia

29
Q

phenoxybenzamine

A

MECHANISM: irreversible alpha antagonist
EFFECT: lowers BP
CLINICAL INDICATION: HTN assocoiated with pheochromocytoma
TOXICITIES: orthostatic hypotension, tachycardia

30
Q

prazosin
terazosin
doxazosin

A

MECHANISM: competitive alpha antagonist
EFFECT: lowers BP
CLINICAL INDICATION: HTN associated with pheochromocytoma
TOXICITIES: orthostatic hypotension

31
Q

Metyrosine

A

MECHANISM: inhibitor of catecholamine synthesis - competitively inhibits tyrosine hydroxylase
EFFECT: lowers BP
CLINICAL INDICATION: treatment of HTN associated with pheochromocytoma

Pharmacology (7 decks)

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