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36 Cards in this Set
- Front
- Back
Lispro/Aspart
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Short acting insulin. Used in Type 1 DM.
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NPH
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Intermediate acting insulin
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Lente/Ultralente
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long acting insulin
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What is the mechanism of action for Sulfonylureas?
What is their most adverse affect? |
Blocks K+ channel in Beta cells, leading to depolarization of the cells. This leads to influx of calcium, which leads to release of insulin.
All can lead to hypoglycemia, CNS effects. Since it is a sulfa drug, can cause hypersensitivity reactions. Can have drug interactions with cimetidine (inhibits P450), salicylates and sulfonamides. |
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Tolbutamide/Chlorpropamide
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1st generation sulfonylureas.
Chlorpropamide is long acting and can induce SIADH (most commonly tested on step 1). Tolbutamide (appropriate in renal dysfunction |
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Glipizide/Glyburide
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2nd generation sulfonyureas
Glipizide – decrease dose in hepatic dysfunction (liver metabolized Glyburide (active metabolite, decrease dose in renal dysfunction |
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Metformin
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does not work through insulin release – increases tissue sensitiviy to insulin….may interfere with gluconeogenesis..makes it go slower. Allows for more glucose uptake and use by cells. Can get lactic acidosis, GI distress.
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Acarbose
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no hypoglycemia..inhibits a-glucosidase in brush small intesinte…decrease formation of absorbable carbohydrates, decreased glucose in blood….decreaesed insulin, so possibly re-sensitization of insulin receptors. Can cuase GI problems and recent concern overy hepatoxicity
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Thiazolidinediones (pioglitazone and rosiglitazone)
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bind to nuclear peroxisome proliferators activating receptors (PPAR’s). Involved in transcription of insulin responsive genes -> change gene expression, so increase sensitized tissues to insulin…decrease gluconeogenesis and triglycerides.
Unlikely to cause hypoglycemia but can cause weight gain due to increase sensitivity to insulin. |
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Diethylstilbestrol (DES)
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non steroidal estrogen...
used for ovarian failure/hypogonadism, HRT in postmenopausal women, men with androgen dependent prostate cancer (negative feedback on HPA axis) all steroids can cause gallbladder disease (gallstones). Estrogens tend to vasodilate (spider angiomas, palmaer erthyhema in alcoholics)…breast tenderness, endometrial hyperplasia…migraine headaches Can lead to thrombosis, Vaginal adenocarcinoma in offspring Increased risk of of breast/endometrial cancer. |
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Ethynyl Estradiol, mestranol
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used for ovarian failure/hypogonadism, HRT in postmenopausal women, men with androgen dependent prostate cancer (negative feedback on HPA axis)
all steroids can cause gallbladder disease (gallstones). Estrogens tend to vasodilate (spider angiomas, palmaer erthyhema in alcoholics)… breast tenderness, endometrial hyperplasia…migraine headaches Can lead to thrombosis, Increased risk of of breast/endometrial cancer |
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Clomiphene
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Partial agonist at receptors in pituatary gland, so prevents normal feedback inhibition and leads to LH and FSH...stimulates ovulation.
Used for LH and FSH...can get multiple pregnancies, visual distrubances, hot flashes, ovarian enlargement. |
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Tamoxifen
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Partial agonist...antagonist on breast tissue, agonist in bone.
Can increase risk of endometrial cancer, but usually used for prophalaxis in women high risk for breast cancer. |
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Raloxifene
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partial agonist....used in bone, reduces reabsorption of bone and used to treat osteoperosis.
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anastrozole
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aromatase inhibitor, used in postmenopausal women with breast cancer.
Site of action is usually in adipose tissue, where androgens are aromatized. |
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Progestin
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Medroxyprogesterone, Norethindrone, Desogestrail
main bind progesterone receptors and reduce growth and vascularization of endometrium. Used in oral contraceptives and in the treatment of endometrial cancer and abnormal uterine bleeding. |
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Mifepristone
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Competitive inhibitor of progestins at progesterone receptors.
used for termination of pregnancy toxicity- heavy bleeding, GI effects, abdominal pain. |
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Oral contraception
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mixture of progestins and estrogens.
Can decrease risk of endometrial and ovarian cancer, decrease incidence of ectopic pregnancy, decrease pelvic infections Disadvantages - incresae triglycerdies, depression, weight gain. hypercoaguable state. Can increase the risk of liver adenoma (benign, heavy vascularization which can cause bleeding)…when stopped, ademoa regresses. |
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What 2 drugs induce P450 enzymes and are extremely teratogenic (contra-indicated for birth control pills)?
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Phenytoin, carbamazepine
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Testosterone
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methyltestosterone, 17-alkly deriaties - oxandrolone, nandrolone.
Used for hypogonadism, athletics. Could use in klinefelters’s syndrome (XXY) Side effects – excessive masculinzation, premature closure of epiphysis (if pregnant and used, would look like 21 hydroxylase deficiency), aggression, cholestatic jaundice, dependence. |
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Finasteride
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5 alpha reductase inhibitor (decreases conversion of testosterone to dihydrotestosterone)
Useful in BPH...also useful in hair growht (propecia) Very teratogenic and applied as an ointment (think of a bald guy with a pregnant wife). |
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Flutamide
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non-steroidal competitive inhibitor of testosterone receptor.
Used for prostate carcinoma |
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Ketoconazole
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inhibits steroid synthesis
can be used in PCOS to prevent hirsutism. |
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spirnolactone
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inhibits steroid binding (used in treatment of PCOS to preent hirsutism)
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Leuprolide
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GnRH analog with agonist properties if used in pulsatile fashion.
Pulsatile - used for infertility. If given continously, will act as antagonist, can use for prostate cancer tx - use with flutamide) |
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Propranolol
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B1 blocker and 5' monodeionidase inhibitor
Used for thyroid storm |
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Sildenafil/vardenafil
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inhibit cGMP phosphodiesterase...leads to smooth muscle relaxation in the corpus caverousom.
Toxicity= headache, flushing, dyspepsia, impaired blue green color vision. Can cause life threatining hypotension with nitrates! "fil" the penis |
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Dinoprostone
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PGE2 analog causing cervical dilation and uterine contraction, induces labor
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Ritodrine/terbutaline
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B2 aonists, relax the uterus
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propylthiouracil/methimazole
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Inhibit organification and coupling of thyroid hormone synthesis.
Propylthiouracil inhibits conversion of T4 to T3. Used for hyperthyrodism. Can get skin rash, agrunulocytosis, aplastic anemia |
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somaterm/somatropin
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GH analog, used in GH deficiency or Turner's syndrome
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octreotide
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somatostatin - used for acromegaly, carcinoid, secratory GI tumors
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cosyntropin
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ACTH analog - used for infantile hypoglycemia causing spasms.
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Desmopressin
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vasopressin analog can be used for central DI
Also can increase vWF and factor VIII. Used in vWF deficiency |
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Bisphosphonates
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stabilizes hydroyapatitie, also induce osteoblasts to inhibit osteoclasts.
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Teriparatide
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recombinant PTH analog. Used once daily to stimulate osteoblasts and bone formation (if it was used all the time, it would increase bone breakdown). If you use this more than 2 years, increase risk of osteosarcoma.
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