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157 Cards in this Set
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all insulin preparation contain (1); and the ratio of (1): insulin determines (2) and (3) of insulin release
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1= zinc
2 = rate of release 3 = duration of action |
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insulin release is increased by (4)
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1. glucose
2. sulfonylureas 3. M-agonists 4. B2-agonists |
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insulin release is decreased by (1)
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a2 agonists
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insulin Lispro is an (1) insulin and is suitable for use (2)
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1 = ultra-fast acting
2 = immediately before meals |
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what are the only forms of insulin that can be used IV?
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Lispro
Regular insulin |
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crystalline insulin, i.e. (1) is a (2) onset insulin used in (3) or (4)
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1. regular insulin
2. rapid onset, short duration 3. emergency situations 4. subcutaneously as part of maintenance programs |
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what are the intermediate onset insulins ? (2)
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1. isophage insulin suspension (NPH insulin)
2. lente insulin |
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what is the long acting insulins? (2)
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1. ultra-lente insulin
2. glargine |
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ultra-lente insulin
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given in the morning to maintain basal levels for 12-24 hours
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glargine
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provides a peakless basal insulin level that lasts more than 24 hours
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standard mode of insulin delivery is (1)
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subcutaneous injection
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mechanism of action of Insulin Drugs
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bind to insulin TRK
IRS1 binds and gets phosphorylated, SH2 domains bind activation of phosphatases changes in gene expression |
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hazards of insulin use (2)
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1. hypoglycemia
- esp. in pts w/ renal disease, elderly and children 2. development of antibodies - resistance or allergies |
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mechanism of action of sulfonylureas (4)
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1. block K+ channels = depolarization of B cell, opens Ca2+ channels and causes release of insulin granules
2. decrease glucagon release 3. increase insulin R. sensitivity 4. increase number of functional insulin R. in periphery |
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first generation sulfonylureas (3)
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1. acetohexamide
2. tolbutamide 3. chlorpropamide |
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second generations sulfonylureas (3)
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glyburide
glipizide glimeprimide |
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adverse effects of chlorpropamide (3)
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SIADH
disulfuram-like effect liver/kidney disease may increase levels |
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repaglinide is from the (1) class; it also promotes (2) but w/ a (3) onset and duration; it is taken (4)
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1 = meglitinide
2 = insulin release from B cells 3 = rapid onset 4 = before meals to control post-prandial glucose conc |
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nateglinide is a (1) derivative and is used to (2)
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1. D-phenylalanine derivative
2. restore immediate insulin release in response to a glucose load --> taken before meals |
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adverse effects of sulfonylureas
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1. hypoglycemia
- more common w/ 2nd gen. 2. rash 3. allergy 4. weight gain - promotes fatty acid synthesis and storage 5. drug interactions |
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drug interactions of sulfonylureas
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highly bound to plasma proteins --> drugs that compete for protein binding may enhance their hypoglycemic effect
ex. cimetidine, insulin, salicylates, sulfonamides |
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side effect w/ glipizide
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decrease dose in hepatic dysfunction
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side effect w/ glyburide
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decrease dose in renal dysfunction
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biguanides
- do not depend on (1) - example (2) |
1 = functional islet cells
2 = METFORMIN |
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mechanisms of action of biguanides (4)
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1. decrease hepatic gluconeogenesis
2. increase glycolysis in peripheral tissues 3. decrease glucose absorption in GIT 4. decrease plasma glucagon levels |
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Metformin
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euglycemic drug used to decrease postprandial glucose levels
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mechanism of action of Metformin
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bypasses R. in cell and activates PPARy's in the cell
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side effects of metformin (3)
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1. lactic acidosis
2. GI distress = N/diarrhea 3. inhibits vitamin B12 absorption ** esp. in pts w/ renal or liver disease, alcoholism or conditions of anoxia |
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alpha glucosidase inhibitors (2)
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acarbose
miglitol |
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mechanism of action of acarbose
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inhibits a-glucosidase in brush borders of small intestine = decreases formation of absorbable carbs thus, decreasing postprandial glucose levels
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side effects of acarbose (3)
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1. GI discomfort
2. flatulence and diarrhea 3. potential hepatotoxicty |
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thiazolidinediones - (2)
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1. pioglitazone
2. rosiglitazone |
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thiazolidinediones - mechanisms of action
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bind to PPARs involved in TXN of insulin responsive genes --> sensitization of tissues to insulin, decreased hepatic gluconeogenesis and increased insulin receptor numbers
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side effects of thiazolidinediones
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1. hypoglycemia - less than others
2. weight gain 3. edema 4. induce CYP3A4 - reduce conc. of other drugs 5. allergies |
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exenatide
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long acting GLP1 receptor full agonist
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side effects of exenatide
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nausea and hypoglycemia when used w/ oral sulfonylureas
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sitagliptin - Januvia
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inhibits dipeptidyl peptidase (DPP4) --> inhibits inactivation of GLP1
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GLP1
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augments glucose-dependent insulin secretion
-- released from small intestine post-prandially |
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pramlintide - 3 main actions
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synthetic amylin
- slows rate at which food is absorbed in small intestine - decreases glucose production - decrease appetite |
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replacement therapy in ADDISON's disease (primary adrenocortical insufficiency) (2)
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1. hydrocortisone
- 2/3 dose in am, 1/3 dose in pm 2. fludrocortisone |
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replacement therapy in secondary and tertiary adrenocortical insufficiency
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hydrocortisone
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what drug is used for diagnosis of Cushing's disease?
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dexamethosone
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which steroids are used to Tx. bronchial asthma and allergic rhinitis? (2)
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1. beclomethasone dipropionate
2. triamcinolone ** applied topically to resp. tract which minimizes systemic effects |
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which steroid is used for maturation of fetal lungs?
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beclamethosone --> IM to mother 48 hrs and 24 hrs prior to birth
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which steroid is safe to use in pregnancy?
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prednisone
- prodrug which is not converted by fetal liver |
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side effects of STEROID use (10)
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1. osteoporosis
2. increased appetite 3. Cushing-like syndrome 4. increased frequency of cataracts/ glaucoma 5. hyperglycemia 6. hypokalemia 7. decreased growth in children 8. increased risk of infection 9. peptic ulcers - increased gastric acid secretion 10. peripheral edema |
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acute adrenal insufficiency syndrome
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long term use of steroids suppresses the HPA axis, if they are abruptly stopped causes a stress crises and may be lethal
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metpyarone used for (1) and (2)
- mechanism (3) |
1 = tests of adrenal function
2 = tx. of pregnant women w/ Cushing's 3 = blocks final step in glucocorticoid synthesis (11 hydroxylation) |
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aminoglutethimide
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inhibits conversion of cholesterol to pregnenalone --> blocks synthesis of all hormonally active steroids
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aminoglutethimide is used for treatment of (1) and (2)
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1. breast cancer = eliminates E and androgen production
- used w/ dexamethosone 2. malignancies of adrenal cortex |
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ketoconazole is used to treat cortisol imbalance?
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Cushing's syndrome
-- inhibits all gonadal and steroid hormone synthesis |
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trilostane
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reversible inhibits 3B-hydroxysteroid dehydrogenase
--> affects aldosterone, cortisol and gonadal hormone synthesis |
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mifepristone
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tx. of patients w/ ectopic ACTH syndrome
--> glucocorticoid antagonist and antiprogestin |
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spirinolactone is used to treat (3) things
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1. antihypertensive
2. hyperaldosteronism 3. hirsutism in women |
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mechanism of action of spirinolactone
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competes for mineralocorticoid R and thus, decreases Na+ reabsorption and antagonizes aldosterone/T synthesis
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adverse effects of spirinolactone (4)
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1. hyperkalemia
2. gynecomastia 3. menstrual irregularities 4. skin rashes |
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eplerenone
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aldosterone antagonist at mineralocorticoid receptor
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eplerenone is used for treatment of
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hypertension
- minimizes gynecomastia bc of specificity |
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fludrocortisone
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mineralocorticoid
- favored for replacement therapy after adrenalectomy |
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antagonists of aldosterone receptor (2)
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1. spirinolactone
2. eplerenone |
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clinical uses of estrogens (9)
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1. contraception
2. hormone replacement therapy 3. atrophic vaginitis 4. primary hypogonadism 5. hirsutism and amenorrhea 6. prostate cancer - rarely 7. dysmenorrhea 8. uterine bleeding 9. acne |
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premarin
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conjugated equine natural estrogen
-> isolated from urine of pregnant mares --> used orally for HRT |
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steroidal estrogens (2)
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1. ethinyl estradiol
2. mestranol |
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nonsteroidal estrogen
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diethystilbestrol
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DES is associated w/ (3)
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diethylstilbestrol
1. infertility 2. ectopic pregnancy 3. vaginal adenocarcinomas in daughters |
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adverse effects of estrogens (9)
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1. nausea
2. breast tenderness 3. endometrial hyperplasia 4. increased gall bladder disease 5. migraine 6. hypertension 7. hyperpigmentation/photosensitivity 8. increased blood coagulation 9. increased risk of breast cancer |
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absolute C/I for estrogen use (5)
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1. undiagnosed genital bleed
2. pituitary tumors 3. undiagnosed breast tumors 4. history of liver disease 5. history of thromboembolism |
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relative C/I for estrogen use (4)
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1. diabetes w/ retinopathy
2. hypertension 3. epilepsy 4. migraines |
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"19 nor, 13 ethyl" compounds w/ low androgenic activity (3)
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1. desogestrol
2. gestodene 3. norgestimate |
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medroxyprogesterone
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progestin w/ androgenic activity
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progestin w/ estrogenic activity
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lynestrol
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progestin w/ anti-estrogenic activity
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L-norgestrel
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progestin w/ anabolic activity
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"19 no" compounds
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progestins w/ anti-mineralocorticoid activity (2)
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hydroxyprogesterone
medroxyprogesterone |
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clinical uses of progestins (3)
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1. hormone replacement therapy
2. contraception 3. endometriosis (danazol) |
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adverse effects of progestins (9)
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1. weak androgen actions (skin)
2. hypertension 3. impaired glucose tolerance 4. thromboembolic states 5. decreased HDL, increased LDL 6. breakthrough bleeding 7. antiestrogenic - block lipid changes 8. decreased bone density w/ long term use 9. delayed resumption of ovulation |
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examples of progestins (5)
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1. medroxyprogesterone
2. norethindrone 3. L-norgestril 4. desogesrel 5. norgestimate |
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mifepristone
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oral abortifacient --> morning after pill, used w/ PGE/PGF
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synthetic androgens (2)
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1. methyltestosterone
2. fluoxymesterone |
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anabolic steroids
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1. oxandrolone
2. nandrolone 3. stanozolol |
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clinical uses of androgens (6)
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1. male hypogonadism
2. boys w/ delayed puberty 3. anabolic - illicit use in athletics 4. anemia - stimulate RBC prod 5. promote weight gain in wasting syndromes 6. enhance libido |
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side effects of androgens (6)
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1. excessive masculinization
2. premature closure of epiphyses = decreased growth 3. cholestatic jaundice 4. aggression 5. dependence 6. males - gynecomastia, testicular shrinkage, infertility |
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androgen antagonists (3)
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flutamide
leuprolide finasteride |
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flutamide
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non-steroidal, competitive antagonist at androgen receptor used for AR + prostate cancer
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leuprolide
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GnRH analog
--> used for AR (+) prostate cancer in advanced state --> chemical castration |
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finasteride
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5-alpha reductase inhibitor
--> prevents conversion of T to DHT |
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clinical uses of finasteride
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BPH
male pattern baldness * DHT is responsible for hair loss and prostatic enlargement |
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caution w/ finasteride bc...
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teratogen --> women in close proximity to partner taking this drug may be affected
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anastrazole
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aromatase inhibitor = decreases estrogen synthesis
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anastrazole is used for treatment of...
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estrogen dependent, post-menopausal breast cancer
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examples of highly selective, competitive inhibitors of aromatase (2)
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1. anastrozole
2. letrozole |
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examples of highly selective, irreversible inhibitors of aromatase (2)
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1. testolactone
2. exemestane |
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GnRH analogs examples (6)
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1. gonadorelin
2. buserelin 3. goserelin 4. triptorelin 5. nafarelin 6. leuprolide |
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clinical use of GnRH analogs (6)
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1. endometriosis
2. precoccious puberty 3. polycystic ovary syndrome 4. hirsutism 5. sex hormone dep. cancers 6. uterine myomas |
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adverse effects of GnRH analogs
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1. menopausal syndrome - hot flashes
2. osteoporosis w/ prolonged use |
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clomiphene
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fertility pill
--> increases FSH and LH release, triggering ovulation |
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adverse effect of clomiphene
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increased multiple births
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selective estrogen receptor modulators (SERMs) (2)
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1. tamoxifen
2. raloxifene |
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tamoxifen
- agonist in (1) - antagonist in (2) - partial agonist in (3) |
1 = bone
2 = breast 3 = endometrium |
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tamoxifen is used for (2)
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1. treatment of estrogen-dep breast cancer
2. prophylaxis in high risk patients |
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tamoxifen increases the risk of..
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endometrial cancer - causes endometrial hyperplasia
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raloxifene
- agonist in (1) - antagonists in (2) |
1 = bone
2 = breast and uterus |
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raloxifene - clinical uses (2)
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prophylaxis of postmenopausal osteoporosis
decreases risk of breast cancer in high risk women |
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adverse effects of raloxifene/tamoxifen
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hot flashes - antagonist effect
increased DVT risk -agonist effect |
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danazol
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weak partial agonist
- binds to progestin, androgen and glucocorticoid R. and inhibits P45- enzymes involves in gonadal steroid synthesis |
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danazol - clinical uses (2)
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1. endometriosis
2. fibrocystic disease of breast |
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benefits of hormone replacement therapy (4)
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1. reduction in menopausal symptoms
2. reduction in osteoporosis 3. cosmetic -> improved skin 4. psychological aspects - potentially reduced incidence of Alzheimer's |
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risks of hormone replacement therapy (5)
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1. increased risk of endometrial cancer
2. increased risk of breast cancer 3. small increase in risk of DVT 4. uterine bleeding 5 minor effect such as GI upset, mood changes |
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types of OCP (4)
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1. progestin only pills
2. combined pills 3. post coital contraceptives 4. implantable progestin preparations |
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absolute C/I for OCP (4)
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1. history of liver disease/jaundice
2. thromboembolic disorders 3. carcinoma of breast, cervix or uterus 4. undiagnosed genital bleeding |
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relative C/I for OCP (5)
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1. migraine
2. allergy 3. hypertension 4. diabetes 5. women > 35 yo who smoke |
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benefits of C/I
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1. decreased risk of endometrial and ovarian cancer
2. decreased dysmenorrhea 3. decreased endometriosis 4. decreased pelvic inflammatory disease 5. decreased osteoporosis |
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somatrem
somatropin |
GH analogs
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clinical uses of somatrem (5)
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1. pituitary dwarfism
2. osteoporosis 3. failure to thrive 4. HIV/AIDs 5. prevents aging? |
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octreotide
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somatostatin analog
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clinical uses of octreotide (3)
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1. acromegaly
2. carcinoid syndrome 3. secretory GI tumors |
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cosyntropin
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ACTH analogue
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cosyntropin is used for...
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infantile spasms
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urofollitropin
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FSH analogue
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placental hCG
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LH analogue
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menotropins
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FSH and LH analogues
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FSH/LH analogs used in (2)
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1. hypogonadal states
2. infertility in men/women |
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DA agonists (2)
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bromocriptine
pergolide |
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clinical uses of DA analogues
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hyperprolactinemia
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clinical use of oxytocin
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induction of labor - stimulates uterine contraction
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clinical use of desmopression (4)
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1. neurogenic diabetes insipidus
2. hemophillia A (increases factor VIII) 3. increases vWF in endothelium 4. primary nocturnal enuresis |
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clinical use of GHRH analogs
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diagnosis of cause of GH deficiency
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clinical use of TRH analog (protirelin)
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diagnostic testing of thyroid dysfunction
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GnRH antagonists (2)
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1. ganirelix
2. cetrorelix |
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clinical use of GnRH antagonists
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prevent premature LH surges during controlled ovarian hyperstimulation
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clinical use of menotropins
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combine w/ hCG in treatment of:
- hypogonadal states - controlled ovarian hyperstimulation - assisted repro. technology |
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clinical use of prolactin
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prolactin is not used in therapy
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what are the monovalent cations that affect thyroid function? (3)
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1. perchlorate (ClO4-)
2. pertechnetate (TcO4-) 3. thiocyanate (SCN-) |
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mechanism of action of monovalent cations?
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inhibition of I- transport to thyroid gland
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clinical use of perchlorate
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pts w/ iodide-induced hyperthyroidism
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adverse effects of perchlorate (3)
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1. thyroid enlargement
2. hypothyroidism 3. aplastic anemia - rare |
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progoitrin
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found in diet in cassava root
--> too much may cause HYPOthyroidism and goiter |
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what are the thioamides? (3)
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1. methimazole
2. carbimazole 3. propylthiouracil |
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mechanisms of action of thioamides? (3)
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1. inhibition of thyroid peroxidase
2. inhibition of organification of iodide to MIT/DIT on TG 3. coupling of MIT and DIT to form T3/T4 |
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conversion of T4--> T3 in the periphery is blocked by ? (2)
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1. propylthiouracil
2. propranolol |
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which thioamide is preferred in pregnancy?
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propylthiouracil
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IV forms of what drugs are useful in thyroid storm? (2)
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1. methimazole (Favistan)
2. thaimazol |
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adverse effects of thioamides? (7)
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1. agranulocytosis
- usually in older pts w/ high doses 2. hypothyroidism 3. thyroid hypertrophy 4. skin reactions 5. arthralgia 6. vasculitis 7. lymphadenopathy |
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low doses of iodide may (1) thyroid function and prevent (2), whereas excess iodide (3) thyoid function
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1. increase
2. goiter 3. inhibits |
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Lugol's solution
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potassium iodide + iodine
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Lugol's solution is used to treat ? (2)
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1. thyroid storm
2. preparation of hyperthyroid pts prior to surgery |
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How does Lugol's solution work? (2)
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1. inhibits iodination of tyrosine in thyroid gland
2. decreases gland size, fragility and vascularity |
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what is the first line drug for treatment of hyperthyroidism in USA?
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radioactive iodide
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mechanism of action of radioactive iodide
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taken up and processes in thyroid same way as iodide, but it emits beta particles which exert cytotoxic effects on cells of thyroid --> effect present for 2-4 months
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adverse effects of radioactive iodide
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1. hypothyroidism
2. crosses placenta - should not be used in pregnancy |
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thyroid hormones used in replacement?
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1. levothyroxine (T3)
2. liotyronine (T4) |
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dextrothyroxin
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D isomer of thyroxin --> decreases cholesterol blood levels, formerly used as a hypolipemic drug
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amiodarone and thyroid function?
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1. inhibits TH synthesis and release w/ induction of hypothyroidism
2. inhibits 5' deiodinase in periphery 3. may also cause thyrotoxicosis |
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Acute management of Thyroid Storm (5)
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1. propranolol
2. methimazole or propylthiouracil 3. Lugol's iodine 4. hydrocortisone 5. cooling blanket |
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ipodate
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iodinated radiocontrast media
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mechanism of ipodate
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suppresses conversion of T4 --> T3 in periphery, inhibits TH release
--> useful for rapidly decreasing T3 conc. in thyrotoxicosis |
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what is the drug of choice for thyroid hormone replacement therapy?
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levothyroxine (T4)
-- bc T3 has shorter half life and is more expensive |
