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Endocrine Module 10
endocrine drugs
105
Pharmacology
Graduate
04/14/2011

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Term
Nafarelin acetate (Synarel Nasal solution)
Definition
endometriosis; agonist of GnRH; spray in morn and even b/w days 2 and 4 of menstrual cycle; sneezing dec bioavailability
Term
Leuprolide (Lupron)
Definition
prostate CA, endometriosis, kids c precocious puberty; inhibits gonadotropin secretion by desensitizing LHRH receptors; causes edema, hot flashes, impotence, dec libido
Term
Somatropin (Humatrope, Serostim, Genotropin)
Definition
cachexia in AIDS, and kids c growth failure sec to lacking endogenous GH; IM or SC injection; may induce insulin resistance, hypothyroidism, inhibit growht promoting effect
Term
Somatrem (Protropin)
Definition
cachexia in AIDS and kids c growth failure sec to lacking endo GH; IM or SC; may induce insulin resistance, inhibit growth promotion, hypothyroidism
Term
hypothyroidism
Definition
hyposecretion of TSH resulting in atrophy and dec secretory activity of thyroid --> myxedema in adults and cretinism in kids
Term
Thyrotropin (Thytropar)
Definition
diff b/w primary and sec hypothyroidism; IM or SC; can cause facial flushing, N/V, HA
Term
what are purified gonadotropin products used for
Definition
to induce ovulation and PG in infertile women
Term
Human chorionic gonadotropin (hCG)(APL, Pregnyl, Profast)
Definition
PG test obtained from urine of PG women and induces ovulation only after pre-test c menotropins; same activity as LH with some FSH activity; IM ONLY; may have multiple births when on this drug
Term
Menotropins (Pergonal, Repronex)
Definition
induction of ovulation and PG in anovulatory infertile women; produce ovarian follicular growth in women s primary ovarian failure; IM c hCG;
Term
Clomiphene (Clomid, Serophene)
Definition
infertility in women c norm ovarian and pituitary fxn but s normal hypothalamic stimulus; promotes pituitary release of FSH and LH; PO;
Term
Vasopressin (ADH) (Pitressin)
Definition
post op abd distention, bleeding esophageal varices (unlabeled use), V fib/pulseless V tach cardiac arrest (unlabeled), DI (limited); acts on V1 and V2 receptors and released in response to changes in blood osmolality; IV or intraarterial injection- parenterally; may cause facial pallor, N, belching, abd cramps, bronchial constriction; caution in pts c vascular disease, epilepsy, migraines, asthma, or heart failure
Term
Desmopressin (DDAVP)
Definition
DOC for DI, pediatric enuresis, and adult enuresis; synthetic analog of ADH; intranasal sln BID or PO injection for enuresis; induce V1 receptor SE including antidiuretic effects, abd cramping, angina, HTN
Term
Oxytocin
Definition
induction of labor, abortion (unlabeled), control PP bleeding; released in response to hormonal changes at term PG; IV; may cause PCVs, harm or death to mom or infant; CI in CPD and unfavorable fetal position
Term
Effects of V1 receptors
Definition
cause GI and vascular smooth muscle contraction
Term
Effects of V2 receptors
Definition
cause water conservation and release of blood coagulation facotrs
Term
What is full blown hypothyroid syndrome called in adults?
Definition
myxedema coma (cold intolerance, wt gain, constipation, lethargy, thick dry skin, and puffy appearance
Term
what is full blown hypothyroid syndrome called in children?
Definition
cretinism- development of abnormalities, short body, mental retardation
Term
Levothyroxine (Sythroid, Levoxyl)
Definition
DOC for hypothyroidism; synthetic levothyroxine; PO daily; may cause hyperthyroidism if dosage is too high, angina and a fib in elderly; cholestyramine and orlistat may interfere c absorption; thyroxine inc anticoag effect of warfarin
Term
Liothyronine (Cytomel)
Definition
hypothyroidism; synthetic form of T3; short duration of activity; used in "augmentation therapy" with antidepressants
Term
signs and symptoms of hyperthyroidism
Definition
wt loss in setting of hyperphagia, tremor, nervousness, and atrial tachycardias
Term
propylthiouracil
Definition
DOC for hyperthyroidism in PG and during breastfeeding; also used for life-threatening thyroid storm; interfere with incorporation of iodine into tyrosine residues of thyroglobulin; PO but effect may take weeks; may cause hepatotoxicity, agranulocytosis; PG category D
Term
Methimazole (Tapazole)
Definition
preferred to PTU due to fewer SE; used for hyperthyroidism; interferes with incorporation of iodine into tyrosine residues of thyroglobulin; PO; skin rash, leukopenia
Term
Radioactive iodine
Definition
hyperthyroidism; emission of beta rays destroys the thyroid cells; supplement with T4 replacement
Term
sodium etidronate, alendronate (Fosamax), risedronate (Actonel)
Definition
first line for Paget's disease, also prevention of osteoporosis; bind irreversibly to bone and resists action of osteoclasts; pt should remain sitting up for 30 min after taking the drug; causes gastric irritation;
Term
fortical (nasal spray)
Definition
calcitonin for osteoporosis and Paget's disease; inhibits bone resoroption and enhances bone formation; causes hypocalcemia, nausea
Term
Vitamin D
Definition
for long-term control of hypocalcemia; recommends 1000-1500 mg/d Ca and 400 IU vitamin D to dec bone loss during aging
Term
Teriparatide injection (Forteo; Fortco)
Definition
treatment of osteoporosis in postmenopausal women and men at risk; first agent approved for osteoporosis that stimulates new bone formation
Term
Cypionate (Depo-Testosterone)
Definition
testosterone deficiency (dec sex drive, impotence, dec bone density); promotes development and maintenance of male sex organs and secondary sex characteristics and inhibit spermatogenesis; IM as oily solutions but not effective PO; PG women should NOT touch, metabolized to DHT and CI in men with breast or prostate CA
Term
Nandrolone decanoate (Deca-Durabolin)
Definition
replacement therapy in primary or secondary hypogonadism; schedule IV; work as endo androgens; high dose produces androgenic effects; causes sodium and water retention, gynecomastia, acne, sterility; CI pts c cancer of prostate or male breast, nephrosis or PG; BB Warn peliosis hepatitis, liver, cell tumors and blood lipid changes
Term
Oxymetholone (Anadrol-50)
Definition
anabolic steroids; dysmenorrheal, dec menopausal sx, dec PP breast engorgement, provide sx relief in breast CA; schedule IV; sodium and water retention, gynecomastia, acne; BB Warn peliosis hepatitis, liver cell tumors and blood lipid changes; CI in pts with prostate or male breast CA, nephrosis or PG
Term
Bicalutamide (Casodex)
Definition
anti-androgens; first line for advanced prostate cancer (combo with LHRH); inhibits action of androgens by binding androgen receptors; causes hot flashes and diarrhea
Term
Finasteride (Propecia, proscar)
Definition
anti-androgens; proscar for BPH and propecia for hair loss; 5-alpha-reductase inhibitor (prevents conversion of testoterone to potent DHT); may cause impotency, dec libido, breast tenderness; PG X and women should not handle tablets
Term
Dutasteride (Avodart)
Definition
anti-androgen; symptomatic BPH; inhibits conversion of testosterone to DHT; subject to enzyme inhibition and PG X so don't handle tabs
Term
estrogen (estradiol is most potent), estrone & estriol
Definition
PG mare urine is natural source; for menopausal/postmenopausal women, ovulation and prevent PP breast discomfort and dec bone resorption & conservation of calcium; weakly anabolic so dec plt adhesiveness, inc serum clot factors, dec lactation PP, inc levels of thyroxin and cortisol and dec beta lipoproteins/cholesterol; made in liver with complete absorption; inc in incidence of breast CA and DVT; CI in women with undx genital bleeding, estrogen dependent CA, thromboembolism hx or PG
Term
Premarin or ethinyl estradiol
Definition
relieve menopausal hot flashes with no CV benefit, prevents vulvovaginal atrophy; use lowest dose possible; risk for ischemic stroke
Term
Raloxifen (Evista)
Definition
non-steroidal benzothiophene SERM; prevention of postmenopausal osteoporosis, dec risk of breast CA, inc bone mineral density and lowers LDL; agonist in some estrogen receptors and antagonist at others; inc risk of thromboembolism, hot flashes and leg cramps; fewer GI SE and drug interactions than Fosamax and not associated c SE of estrogen therapy
Term
What is first line therapy for postmenopausal osteoporosis?
Definition
bisphosphonates
Term
Alendronate (Fosamax)
Definition
bisphosphonate; for osteoporosis in postmenopausal women; take 30 min before anything c plain water only and avoid laying down for 30 min; may cause esophagitis
Term
Tamoxifen (Nolvadex)
Definition
anti-estrogen; SERM drug; agonist on endometrial proliferation, bone resorption & lipoproteins anti-estrogen on breast CA; inc endometrial thickness and risk of CA and inc venous thromboemboli events
Term
Progesterone information
Definition
transforms proliferative endometrium into secretory endometrium and influences spontaneous contractile activity of the uterus and dec GnRH release sustains PG and reduces incidence of endometrial hyperplasia
Term
Progesteron indications
Definition
progestin-only for tx of AUB, amenorrhea and endometriosis; long acting is for OCP
Term
Progesterone MOA
Definition
produced by corpus luteum, testes, adrenal glands and placenta during PG
Term
Progesterone SE
Definition
GI upset, H/A, dizziness, N/V, thromboemboli, cholestatic jaundice and depression
Term
Progesteron CI
Definition
CI in pt c PMH of thromboembolic disease, breast CA or genital organs CA or impaired liver function
Term
progesterone in oil (progestaject) IM (progesterone vag gel),
Definition
progesterone product
Term
medroxyprogesteron acetate (Provera tablets)
Definition
progesterone
Term
hydroxyprogesteron caproate in oil (Hylutin)
Definition
progesterone
Term
norethindrone acetate (aygestin tabs)
Definition
progesterone
Term
megestrol acetate (Megace tabs and PO suspension)
Definition
progesteron
Term
SE of OCP and warnings
Definition
N, V, wt gain, cramping; warning of thromboembolism and HTN; PG cat X
Term
progesterone only Micronor, Nor-QD
Definition
for women who can't stand estrogen; OC of choice in SLE pt; taken QD c no pill-free interval and changes endometrial and cercial mucous environment; take at exactly the same time daily; may cause breakthrough bleeding, ectopic PG risk and inc need for compliance
Term
combination pill = combo of estrogen and progestin
Definition
taken daily for 21 d then a 7 d pill free interval; others have 81 d dosage c only 4 menses/yr; 1 prep is a year- long dosage schedule
Term
combination pill SE
Definition
worse in first 3 mo- N, dizziness, edema, and abd cramping; constant SE- H/A thromboembolic sm, dec libido; worse over time- h/a and hirusitism
Term
combination pill CI and warnings
Definition
enzyme induces dec OCP effectiveness; use second method of contraception; CI in thrombophlebitics, CVA, ischemic artery disease, PG, smokers > 35 y/o; severe h/a, migraine, HTN
Term
Minera
Definition
contraceptive progestin-containing IUD; recommended for women who have had at least 1 child and pt taking anticonvulsants; lasts 5 yrs;
Term
Depo-Provera
Definition
long-acting injectable progestins; administered every 3 mo; long acting injectable and used to tx endometrial and renal carcinoma; prevents follicular maturation and ovulation; PP for women breastfeeding; causes amenorrhea, wt gain and inc risk osteoporosis; BB warn dec BMD and not used more than 2 yrs
Term
Implanon
Definition
contains progestin etonogestrel; single rod inserted subdermally in upper arm for 3 yrs; may cause irregular bleeding and amenorrhea, h/a, wt gain, breast and abd pain
Term
NuvaRing
Definition
estonogestrel/ethinyl vaginal ring indicated for prevention of PG; release estrogen and progestin over three weeks then removed for one week; may cause vaginitis, h/a, UTI, N, wt gain
Term
OrthoEvra
Definition
provides 60% more estrogen than typical OCP; applied to area where it won't be rubbed off; worn for 1 week at a time for 3 consecutive weeks and wk 4 is patch free; BB Warn of cigarettemokg and risk of CV adverse effects
Term
Preven
Definition
for emergency contraception; 2 tabs w/in 72 hrs of unprotected intercourse and 2 tabs 12 hrs later; doses are much higher than in OCP; combo levonorgestrel and ethinyl estradiol
Term
Plan B
Definition
emergency contraception; progestogen prep w/ 1 tab w/in 72 hr of unprotected intercourse and 2nd tab 12 hrs later; contraceptive not an abortifactant and acts by preventing ovulation and may prevent implantation
Term
spermicidees
Definition
nonoxynol 9 & octoxynol; apply 10 min but not > 1 hr before intercourse and apply high in vagina prior to intercourse;
Term
Clomiphene Citrate (Clomid, Serophene)
Definition
nonsteroidal ovulatory stimulant and fertility drug; 80% of women become PG; inc output of GnRH and pituitary gonadotropin; CI hepatic dysfunction, abnormal bleeding
Term
ergonovine (erogtrate)
Definition
vasoconstrictor used PP oxytocins to prolong intense contractions of uterus for hemostasis; PO or IM; uterine cramping, N/V/D; CI in eclampsia, CVA, limb ischemia
Term
Prostaglandins
Definition
produced from arachidonic acid; used as abortifactant for cervical ripening; regulate sperm motility, stimulate anterior pituitary release of LH, inhibit activity of corpus luteum and control smooth muscle tone; most serious SE = uterine rupture or cervical perforation, drowsyness, HTN, dyspnea
Term
Misoprostol (Cytotec)
Definition
abortifacient and unlabeled use as "vaginal ripening" at term; 2 tabs inserted vaginally or PO;
Term
Terbutaline (Brethine)
Definition
beta 2 agonist that suppresses labor; SC administration; unapproved use
Term
Magnesium sulfate
Definition
inhibits myometrial contractility and tx eclampsia; IV; lacks FDA approval
Term
What is the insulin of choice?
Definition
rapid acting insulins lispro or aspart
Term
function of insulin
Definition
facilitate transport of glucose across cell membranes & to enhance phosphorylation of glucose within cells
Term
what is the most serious SE of insulin?
Definition
hypoglycemia
Term
treatment of severe hypoglycemia
Definition
treated with 50% glucose solution or glucagon IV
Term
insulin drug interactions
Definition
ACTH, glucocorticoids, thyroid, thiazides, estrogens inc blood sugar; epi inhibits secretion of insulin; BB, NSAIDs, ethanol, salicylates, lithium with hypoglycemic effects; OCAs, beta-2 agonists, CCB, phenytoin with hyperglycemic effects
Term
insulin lispro (LYS-Pro Humalog)
Definition
rapid or immediate onset short acting; 15 min ac or immediately pc; peak 1 hr;
Term
insulin Aspart (Novolog)
Definition
insulin of choice for use in insulin pumps; faster absorption, onset of action and shorter duration of action than regular insulin;
Term
Glulisine insulin (Apidra)
Definition
approved for use with insulin pump; administered 15 min ac or 20 min pc and faster onset and shorter duration of action than reg insulin;
Term
Insulin injection (regular insulin)
Definition
insulin of choice for tx of abrupt onset hyperglycemia or ketoacidosis; short acting; IV and SC:
Term
Isophane (NPH)
Definition
intermediate prep c insulin conjugated c protamine; peaks 4-12 hrs and take bid; used in insulin mixtures
Term
Detemir Insulin (Levemir)
Definition
as effective as NPH c same incidence of hypoglycemia; once or twice-daily SC use and can be used as monotherapy or added to PO antidiabetic agents or rapid-acting insulin; provides up to 24 hr duration of action;
Term
Glargine (Lantus)
Definition
lower incidence of nocturnal hypoglycemia than NPH; more dense crystal structure; SC once daily with flat insulin profile for 24 hrs; should not be admin IV and not diluted or mixed with other insulin or solution
Term
Amylin
Definition
suppresses glucagon secretion and slows gastric emptying; contributes to glucose control during post prandial period
Term
Pramlintide (Symlin)
Definition
synthetic analog of amylin approved in pts c type 1 or 2 diabetes who inject insulin at mealtimes and have failed to acheive glucose control; ac to dec post-prandial plasma glucose and dec short-acting insulin required; N/V and inc risk of severe hypoglycemia when given c insulin; do not mix insulin in same syringe
Term
Glyburide
Definition
sec gen sulfonylurea; PO hypoglycemic; stimulate pancreatic cells to secrete insulin; initial dose with first main meal; may cause hypoglycemic coma and GI upset; PG cat C
Term
Glyburide interactions
Definition
chloramphenicol, MAOI, salicylates and sulfonamides inc risk of hypoglycemia; NSAIDs and salicylates affect prostaglandin activity which regulates glucose
Term
Glipizide (Glucotrol; Glucotrol XL)
Definition
sec gen sulfonylurea that stimulates pancreatic beta cells to secrete insulin; take 30 min ac; may cause hypoglycemic coma or GI upset; PG cat C
Term
Repaglinide (Prandin)
Definition
meglitinides; PO hypoglycemic that stimulates the release of insulin from the pancreas; PO within 15 min of meal; hypoglycemia
Term
Nateglinide (Starlix)
Definition
meglitinides; lower blood glucose or HgbA1C; sensitizes beta cells to glucose c rapid onset and short duration of action; take 1 to 30 min ac;
Term
Metformin (Glucophage) general info
Definition
biguanide anti-hyperglycemic; monotherapy first line or when used in combo may have syngergistic effect
Term
Metformin (Glucophage) actions and MOA
Definition
anti-hyperglycemic that lowers LDL and inc HDLs; do not stimulate pancreatic insulin secretion; dec glucose production by liver by dec gluconeogenesis inc glucose oxidation; dec glucose absorption
Term
Metformin (Glucophage) kinetics
Definition
food dec extend and delays absorption however it should be given c the morning and evening meals to dec gastric upset
Term
Metformin (Glucophage) SE and CI
Definition
GI distress and less hypoglycemia or wt gain; CI in pts with renal dysfunction or metabolic acidosis; cimetidine causes inc in concentration and AUC; BB warn lactic acidosis
Term
Rosiglitazone (Avandia), Pioglitazone (Actos)
Definition
combination therapy c sulfonylureas, diet and exercise in pts with type 2 diabetes; inc glucose uptake, dec insulin resistance, and inc sensitivity of insulin receptors; once daily; fluid retention that may lead to heart failure; inc risk of hypoglycemia when given c insulin
Term
Acarbose (Precose) Miglitol (Glyset)
Definition
alpha-glucosidase inhibitors; used to dec postprandial plasma glucose & potentiate the hypoglycemic effect of insulin & sulfonylureas; reversibly bind to & inhibit alpha-glycosidase at brush borders of the small intesine; take at first bite of each meal; GI symptoms;
Term
Sitagliptin (Januvia) and Saxagliptin (Onglyza)
Definition
dipeptidyl peptidase-4 inhibitors; tx type 2 diabetes and do not cause hypoglycemia or wt loss; inc availability of GLP-1;
Term
Glucogon
Definition
polypeptide hormone produced by alpha cells of pancreatic islets for tx of severe hypoglycemia; stimulates glycogenolysis and produces neoglucogenesis; IV c glucose in tx of acute hypoglycemic rxn
Term
Indications for corticosteroids
Definition
Deficiency states (i.e Addison's dx), cerebral edema, lumbar disc dz, organ transplant, asthma, arthritis, collagen dx, ocular inflammation, cutaneous d/o, UC, MG, leukemia, allergic rhinits, URI
Term
MOA of corticosteroids
Definition
gluconeogenesis, protein catabolism, fatty acid metabolism, anti-inflammatory effects, lymphoid tissue and immune response suppression, sex hormone regulation
Term
mineralocortoid effects
Definition
aldosterone evokes distal renal tubular reabsorp of Na in exchange for K
Term
glucocorticoid effects
Definition
cortisol influences glucose, fat, and protein metabolism and produces anti-inflammatory response
Term
corticosteroid withdrawal SE
Definition
fever, myalgia, arthralgias, malaise
Term
long term corticosteroid use in large doses SE
Definition
pituitary adrenal suppression, fluid/lytes imbalance, hyperglycemia, PU, inc susceptibility to infection, osteoporosis, myopathy, cataracts, arrest of growth, cushing habitus
Term
hydrocortisone (Cortef, hydrocortone)
Definition
chronic adrenal insufficiency, UC; cortisol secreted by adrenal cortex regulated by ACTH from ant pit; causes sodium and water retention; antacids interfere with PO absorption, enzyme inducers
Term
Prednisone
Definition
more potent corticosteroid than hydrocortisone; DOC for long-term EOD tx to dec suppression of HPA axis and for autoimmune diseases; analog of cortisol; converted to prednisolone in gut; taper drugs! may cause adrenal insufficiency
Term
Dexamethasone (Decadron)
Definition
tx for certain types of cerebral edema; fluorinated derivative with anti-inflammatory effects; suppresses HPA axis and not likely to cause Na and H2O retention;
Term
Fludrocortisone (Florinef)
Definition
mineralocorticoid for deficiency states such as addison's disease; glucocorticoid c potent mineralocorticoid properties; sodium and water retention
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