Pharm - Endocrine Drugs

Front 1

Lispro/Aspart

Back 1

Short acting insulin. Used in Type 1 DM.

Front 2

NPH

Back 2

Intermediate acting insulin

Front 3

Lente/Ultralente

Back 3

long acting insulin

Front 4

What is the mechanism of action for Sulfonylureas?

What is their most adverse affect?

Back 4

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.

Front 5

Tolbutamide/Chlorpropamide

Back 5

1st generation sulfonylureas.
Chlorpropamide is long acting and can induce SIADH (most commonly tested on step 1).

Tolbutamide (appropriate in renal dysfunction

Front 6

Glipizide/Glyburide

Back 6

2nd generation sulfonyureas
Glipizide – decrease dose in hepatic dysfunction (liver metabolized

Glyburide (active metabolite, decrease dose in renal dysfunction

Front 7

Metformin

Back 7

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.

Front 8

Acarbose

Back 8

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

Front 9

Thiazolidinediones (pioglitazone and rosiglitazone)

Back 9

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.

Front 10

Diethylstilbestrol (DES)

Back 10

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.

Front 11

Ethynyl Estradiol, mestranol

Back 11

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

Front 12

Clomiphene

Back 12

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.

Front 13

Tamoxifen

Back 13

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.

Front 14

Raloxifene

Back 14

partial agonist....used in bone, reduces reabsorption of bone and used to treat osteoperosis.

Front 15

anastrozole

Back 15

aromatase inhibitor, used in postmenopausal women with breast cancer.

Site of action is usually in adipose tissue, where androgens are aromatized.

Front 16

Progestin

Back 16

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.

Front 17

Mifepristone

Back 17

Competitive inhibitor of progestins at progesterone receptors.

used for termination of pregnancy

toxicity- heavy bleeding, GI effects, abdominal pain.

Front 18

Oral contraception

Back 18

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.

Front 19

What 2 drugs induce P450 enzymes and are extremely teratogenic (contra-indicated for birth control pills)?

Back 19

Phenytoin, carbamazepine

Front 20

Testosterone

Back 20

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.

Front 21

Finasteride

Back 21

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).

Front 22

Flutamide

Back 22

non-steroidal competitive inhibitor of testosterone receptor.

Used for prostate carcinoma

Front 23

Ketoconazole

Back 23

inhibits steroid synthesis

can be used in PCOS to prevent hirsutism.

Front 24

spirnolactone

Back 24

inhibits steroid binding (used in treatment of PCOS to preent hirsutism)

Front 25

Leuprolide

Back 25

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)

Front 26

Propranolol

Back 26

B1 blocker and 5' monodeionidase inhibitor

Used for thyroid storm

Front 27

Sildenafil/vardenafil

Back 27

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

Front 28

Dinoprostone

Back 28

PGE2 analog causing cervical dilation and uterine contraction, induces labor

Front 29

Ritodrine/terbutaline

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B2 aonists, relax the uterus

Front 30

propylthiouracil/methimazole

Back 30

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

Front 31

somaterm/somatropin

Back 31

GH analog, used in GH deficiency or Turner's syndrome

Front 32

octreotide

Back 32

somatostatin - used for acromegaly, carcinoid, secratory GI tumors

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cosyntropin

Back 33

ACTH analog - used for infantile hypoglycemia causing spasms.

Front 34

Desmopressin

Back 34

vasopressin analog can be used for central DI

Also can increase vWF and factor VIII. Used in vWF deficiency

Front 35

Bisphosphonates

Back 35

stabilizes hydroyapatitie, also induce osteoblasts to inhibit osteoclasts.

Front 36

Teriparatide

Back 36

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.