Endocrine/Reproductive Flashcards
Octreotide
Somatostatin analog
Tx: acromegaly, Upper GI bleeding (varices), hyperinsulinism
Side Effects: Injection site reaction, gallbladder sludge, n/v, glucose intolerance, carcinoid tumors (diarrhea)
IM
Somatropin
Recombinant human GH Tx: GH deficiency, short stature C/I: Active malignancy, ICU pts Side Effects: ICP, SCFE, scoliosis, DM, soft tissue deposition SQ daily
Pegvisomant
Pegylated recombinant GH (GHR antagonist)
Tx: acromegaly
Adverse Fx: Local reaction, hepatitis, tumor growth
SQ
Cross-reacts with GH; use IGF-1 to monitor effects
Bromocriptine
Prototype Dopamine agonist
Tx: hyperprolactinemia
Adverse Effects: n/v, orthostasis (with first dose), blunts antipsychotics
PO daily
Cabergoline
Dopamine agonist
Tx: hyperprolactinemia, acromegaly (mixed adenomas)
Higher affinity with longer-half life than bromocriptine
PO weekly
Fewer adverse effects than bromocriptine
High doses (for Parkinson’s) linked to valvular disease
hCG
Dx pregnancy
Tumor marker for germ cell tumors
Tx: Stimulate ovulation in fertility treatment and IVF, cryptorchidism
FSH
Dx: Precocious puberty or delayed puberty
Tx: Follicle/sperm stimulation in fertility treatment and IVF
Adverse Effects: Multiple gestations, OHSS
Leuprolide
GnRH agonist
Tx: Central precocious puberty, hormone-dependent cancers, endometrious/uterine fibroids, and fertility treatment (short-term therapy)
IM
ACTH
Tx: infantile spasms
Cosyntropin
ACTH fragment
Screen for adrenal insufficiency
IM or IV push
Dexamethasone
Potent, long-acting glucocorticoid with no mineralocorticoid activity
Hormone replacement therapy
Tx: stress, inflammation and cerebral edema, chemo adjunct, immunosuppression
Fludrocortisone
Potent mineralocorticoid
Hormone replacement therapy
Fluticasone
Potent glucocorticoid
Tx: asthma, allergic rhinitis
Inhalant/nasal spray (limit systemic side effects)
Hydrocortisone
Short-acting glucocorticoid (mineralocorticoid at higher doses)
Hormone replacement
Tx: inflammation
Topical prep available
Methylprednisolone
Intermediate-acting glucocorticoid
Hormone replacement therapy
Tx: inflammation
Prednisone
Intermediate-acting glucocorticoid Requires liver metabolism into active prednisolone Hormone replacement therapy Tx: inflammation Used with pregnancy PO
Prednisolone
Intermediate-acting glucocorticoid
Tx: inflammation
Used instead of prednisone with hepatic failure
Triamcinolone
Potent, intermediate-acting glucocorticoid (no MR activity)
Tx: asthma, inflammation, psoriasis
PO, IM, topical
Spironolactone
MR antagonist
Tx: HTN and CHF
Weak androgen receptor antagonist
Tx: hirsutism
Glyburide
Sulfonylurea
Inhibit ATP sensitive K channel (enhances physiological response)
C/I: sulfa allergy, hepatic disease, low GFR
Adverse Effects: hypoglycemia (esp. in elderly), weight gain
1-2 times daily PO, cheap
Glipizide
Sulfonylurea
Inhibit ATP sensitive K channel (enhances physiological response)
C/I: sulfa allergy, hepatic disease, low GFR
Adverse Effects: hypoglycemia (esp. in elderly), weight gain
1-2 times daily PO, cheap
Glimepiride
Sulfonylurea
Inhibit ATP sensitive K channel (enhances physiological response)
C/I: sulfa allergy, hepatic disease, low GFR
Adverse Effects: hypoglycemia (esp. in elderly), weight gain
1-2 times daily PO, cheap
Repaglinide
Meglitinide
Inhibit ATP-sensitive K channel
Most active post-prandially (skip a meal, skip dose)
C/I: hepatic or renal dysfunction, increases cipro and clarithromycin concentration
Side Effects: Hypoglycemia (less than SUs), weight gain
Metformin
Biguanide
Improves insulin sensitivity in liver
C/I: renal or liver dysfunction (risk of lactic acidosis)
Side Effects: B12 deficiency, GI effects (titrate dose up)
No hypoglycemia or weight loss
1st line for T2DM
1-3x daily
Pioglitazone
Thiazolidinediones (TZDs)
Activates PPARgamma - Regulates FA metabolism and improve insulin sensitivity
Long time (weeks to months) for maximum response
C/I: CHF/edema, hepatic disease, retinopathy, drug interactions (phenyotin, warfarin and amiodarone)
Side Effects: hepatotoxic, weight gain, edema, increase CV risk
1-2x daily
Acarbose
Alpha-glucosidase inhibitor Reduce carbohydrate absorbtion Taken with meals Variable response GI side effects
Sitagliptin
DPPIV Inhibitor
Increases endogenous incretin levels
C/I: acute pancreatitis, heart failure, renal dysfunction
Side Effects: Hypersensitivity (angioedema and urticaria), nasopharyngitis
Daily dosage, costly
Saxagliptin
DPPIV Inhibitor
Increases endogenous incretin levels
C/I: acute pancreatitis, heart failure, renal dysfunction
Side Effects: Hypersensitivity (angioedema and urticaria), nasopharyngitis
Daily dosage, costly
Canagliflozin
SGLT-2 Inhibitor
Lowers renal glucose reabsorption - osmotic diuresis
C/I: renal dysfunction, elderly, diuretics, hypovolemia, bladder cancer
Side Effects: GU infection, polyuria, volume depletion, LDL increase
Improves blood pressure
Daily dosing, costly
Liraglutide
GLP-1 analog
Stimulates insulin release;decreases gastric emptying; suppress appetite
C/I: acute pancreatitis, medullary thyroid cancer
Side Effects: GI, tachycardia, acute pancreatitis
Exenatide
GLP-1 analog
Stimulates insulin release;decreases gastric emptying; suppress appetite
C/I: acute pancreatitis, medullary thyroid cancer, GFR < 30
Side Effects: GI, tachycardia, acute pancreatitis
Pramlintide
Amylin agonist
Decreases glucagon secretion; slows gastric emptying; satiety
Frequent injections (before meals)
Lispro
Rapid-acting bolus insulin - post-prandial hyperglycemia
PK suited to carbohydrate absorption
Costly
Aspart
Rapid-acting bolus insulin - post-prandial hyperglycemia
PK suited to carbohydrate absorption
Costly
Glulisine
Rapid-acting bolus insulin - post-prandial hyperglycemia
PK suited to carbohydrate absorption
Costly
Insulin
Short-acting bolus insulin
Low immunogenicity, cheap
Must taken 30 minutes before meal; PK don’t overlap w/ CHO absorb.
Delayed post-prandial hyperglycemia
NPH
Intermediate acting, basal insulin
Inexpensive; can be mixed with bolus insulin
Mixed insulin (70 aspart protamine suspension/30 aspart; 70 NPH/30 insulin)
Twice daily at breakfast and dinner
Mimic physiologic insulin
Glargline
Long-acting basal insulin
Once daily dose; ~ body’s basal secretion
Less hypoglycemia
More costly; Cannot be mixed
Acidic - forms microprecipitates –> slow release
Acidity causes injection site irritation
Determir
Long-acting basal insulin Once daily dose; ~ body's basal secretion Albumin-bound --> slow release Less hypoglycemia More costly Cannot be mixed
Iodine
Blocks thyroid hormone release (Wolff-Chaikoff effect) and decreases gland vascularity
Tx thyroid storm (MUST give thionamide first)
Methimazole
Thionamide - TPO inhibitor; does not inhibit deiodinase
1st line tx for hyperthyroidism
Teratogenic during 1st trimester
Side Effects: Rash, LFTs, lupus-like syndrome, agranulocytosis
Once daily dosing
Propylthiouracil (PTU)
Thionamide - TPO inhibitor; Type I 5’-deiodinase inhibitor
2nd line tx for hyperthyroidism
Drug of choice in pregnancy - doesn’t penetrate placenta
Hepatotoxic
Side Effects: Rash, LFTs, lupus-like syndrome, agranulocytosis
Twice daily dosing
Radioactive Sodium Iodide
Ablates thyroid gland
C/I: children and pregnant women
Few side effects - doesn’t concentrate in other parts of body
Requires lifetime thyroid hormone replacement therapy
Levothyroxine
T4 hormone replacement
7 day half-life - Takes 6-8 weeks for steady state concentration
Liothyronine
T3
7 hour half-life
4x more potent than T4
Side effects: tachycardia and jitteriness (due to rapid onset)
Beta blockers
Tx symptoms of hyperthyroidism
Atenolol has advantages of single-day dosing
Propanolol can also inhibit Type I 5’-deiodinase (SLOW effect; contributes little)
Thyrotropin Alfa
Recombinant TSH
Monitor recurrence of thyroid cancer - “reveals” thyroid cells
Increases radioablation efficacy - stimulates thyroid uptake of I
Dessicated Procine Thyroid Extract
“Natural” thyroid hormone derived from dsesicated porcine thyroid glands
Thryolar
Synthetitc combination of T4 and T3
Lithium
Tx hyperthyroidism; MOA unknown
In vitro, decreases colloid droplet formation within thyroid cells - decreased pinocytosis and proteolytic digestion
Dexamethasone
Anti-inflammatory
Blocks T4 to T3 conversion
Tx: thyroid storm
Abiraterone
17alpha-hydroxylase inhibitor
Decreases androgen (adrenal and gonadal) production
Tx castration-resistant prostrate cancer
Used in combination with glucocorticoid (inhibits production)
Pregnant women and children should avoid
Degarelix
GnRH receptor antagonist
Suppresses gonadotropin release; immediate action
Tx prostate cancer
Danazol
Weak synthetic androgen
Suppresses FSH/LH release
Tx endometriosis and fibrocystic breast disease
Finasteride
5alpha-reductase inhibitor; Type II (urogenital tract)
Prevents conversion of T to DHT
Tx BPH and androgenic alopecia (some Type I inhibition)
Larger dose for BPH; often in combo with alpha-1 adrenergic blockers
Avoid in pregnant women (danger to male fetus)
Dutasteride
5alpha reductase inhibitor (both type)
Tx BPH and androgenic alopecia
Avoid contact with pregnant women
Bicalutamide
Androgen receptor antagonist
No cross-specificity
Treat prostate cancer
Does not inhibit HPA (used in conjunction with leuprolide)
Receptor eventually develops acquired resistance –> agonist effects
Fluoxymestrone
Potent synthetic androgen HRT for hypogonadism in males 17alpha-alkylated (slow metabolism, PO) Liver toxicity Reduced estrogenic activity; not a good substrate for aromatase
Methyltestosterone
Synthetic androgen
HRT for hypogonadism in males
17-alkylated (slow metabolism; PO)
Liver toxicity, edema, virilization, gynecomstic, polycythemia, prostate
Nandrolone
Synthetic androgen
Anabolic steroid abused by athletes
Testosterone and ester derivatives
HRT for hypogonadism and delayed puberty in males
Transdermal patch, gel and buccal capsule for T
Esters delivered by IM injection (slowly absorbed, more sustained)
Estradiol and esterifid/conjugated derivatives
HRT in women
Tx abnormal uterine bleeding, and atrophic vaginitis
Also used in OCP
Drospirenone
Synthetic progestin
Spironolactone derivative (can lower BP)
Used in OCP
Hydroxyprogesterone caproate
Synthetic progesterone
Tx amenorrhea, metorrhagic and induction of secretory endometrium
Norethindrone
Synthetic potent progestin
HRt, amenorrhea and OCP
Norgestrel and Norgestimate
3rd generation progestins
OCP, emergency contraception
Medroxyprogesterone acetate (MPA)
Synthetic progestin
HRT, endometrial hyperplasia, prostate cancer and sex offenders
Progestin-only OCp
Progesterone
HRT, amennorrhea
Estradiol/Norethindrone
Combination of E and P for HRT in postmenopausal women
Estrogen/Medroxyprogesterone
E and P combo
HRT
Estrogen/Methyltestosterone
Estrogen and T
HRT in postmenopausal women
Tamoxifen
SERM
Mixed function estrogen receptor agonist/antagonist
Tx breast cancer (chemotherapy and chemoprevention)
Thromoboembolic risk
Stimulates GU growth
Doesn’t prevent hot flashes
Raloxifene
SERM
Primary indication in osteoporosis prevention and PM HRT
Chemoprevention in breast cancer
Clomiphene
Anti-estrogen
Induce ovulation in female infertility
Stimulates gonadotropin release in male infertility
Mifepristone
Anti-progestin
Abortion pill
Must be used in combination with misoprostol
Fulvestrant
Anti-estrogen
Tx breast cancer in PM women
Anastrozole
Aromatase inhibitor
Tx locally advanced or metastatic breast cancer (postmenopausal only)
Can cause joint pain
