Pharmacology Test 2

Front 1

Propylthiouracil

Back 1

Inhibit thyroid peroxidase

Front 2

Methimazole

Back 2

Inhibit thyroid peroxidase

Front 3

Octreotide

Back 3

Synthetic analogue of somatostatin.
Inhibits release of GH.
Inhibits release of 5-HT.
Decreases variceal bleeding - vasoconstrictor.

Therapeutic Use:
1) Acromegaly
2) Carcinoid syndrome - neoplasia of enterochromaffin-
like cells that store 5-HT.
3) Alcoholic cirrhosis

Front 4

Prolactin

Back 4

Prolactin stimulates lactation.
2) Release is regulated by prolactin release inhibiting hormone (dopamine).
3) Prolactin can inhibit mid-cycle surge of LH preventing ovulation.
Clinical Considerations:
1) Hypersecretion (prolactinoma) causes galactorrhea and amenorrhea.
2) Treat with dopamine agonist.

Front 5

Bromocriptine

Back 5

Semi-synthetic ergot alkaloid compound.
**Acts as dopamine agonist.
Inhibits prolactin release.
Inhibits GH release in acromegaly.

Therapeutic Use:
1) Acromegaly
2) Prolactinomas
3) Parkinson’s disease

Side Effects - nausea vomiting and dizziness

Front 6

Leuprolide

Back 6

Agonists of GnRH.
Inhibits LH and FSH release when continuously present.

Front 7

Ganirelix

Back 7

GnRH ANTagonist

Inhibits LH release
Therapeutic Use - LH suppression in women undergoing controlled ovarian stimulation (COS).

Side Effects - abdominal pain, increased incidence of ovarian hyperstimulation syndrome (during COS).
Advantage over GnRH agonists - no initial stimulation of gonadotropin release as with leuprolide.

Front 8

Oxytocin

Back 8

made in Posterior Pituitary

1) Contracts myoepithelial cells causing milk ejection.
2) Produces sustained contractions.
3) Oxytocin-induced contractions inhibited by β2- adrenergic agonists (terbutaline).

Front 9

Vasopressin

Back 9

Posterior Pituitary

Front 10

Desmopressin

Back 10

Vasopressin analogue

Possesses 3000 to 1 antidiuretic activity to vasopressor activity.

Front 11

Levothyroxine

Back 11

synthetic T4

Front 12

Liothyronine

Back 12

synthetic T3

Front 13

Iodide

Back 13

1) Inhibits thyroglobulin proteolysis.
2) Onset of action is rapid.
3) Inhibition is transitory - short term use.
4) Decreases the vascularity, size and fragility of gland.

Therapeutic Use:
1) Management of thyroid storm.
2) Preparation for thyroid surgery

Front 14

131Iodide

Back 14

1) Administered orally as sodium iodide.
2) Half-life of 5-7 days.
3) Emits radiation destroying thyroid cells.

Therapeutic Use - treatment of Grave’s disease refractory
to drug treatment.

Front 15

Propranolol

Back 15

Beta antagonist

treat Thyroid Storm

Front 16

Acetazolamide

Back 16

carbonic anhydrase inhibitor

Front 17

Furosemide

Back 17

Loop of Henle Diuretic

Front 18

ethacrynic acid

Back 18

Loop of Henle Diuretic

Front 19

Hydrochlorothiazide

Back 19

Distal Convoluted Tubule Diuretic

Front 20

Indapamide

Back 20

Distal Convoluted Tubule Diuretic

Front 21

spironolactone

Back 21

Potassium Sparing Diuretic

prevention of Na+ reabsorption by blocking action of aldosterone

Front 22

triamterene

Back 22

Potassium Sparing Diuretic

prevention of Na+ reabsorption by

Front 23

amiloride

Back 23

Potassium Sparing Diuretic

prevention of Na+ reabsorption by

Front 24

Nesiritide

Back 24

recombinant human brain-type natriuretic peptide (BNP).

Front 25

Desmopressin

Back 25

Vasopressin analog used in the treatment of neurogenic diabetes insipidus.

Front 26

Normal Physiology:
Proximal Tubule

Back 26

50-70% NaCl, H20, Urea reabsorption/secretion -> isoosmotic
-OATs (uric acid, drugs)

Front 27

Normal Physiology:
Thin descending limb of loop of Henle

Back 27

H20 reabsorption -> Hyperosmotic

Front 28

Normal Physiology:
Thin ascending limb

Back 28

Passive NaCl reabsorption

Front 29

Normal Physiology:
Thick ascending limb

Back 29

active NaCl reabsorption

Front 30

Normal Physiology:
Distal convoluted tubule

Back 30

Active Na+ transport

Front 31

Hydrocortisone

Back 31

Short acting, low potency steroid

Front 32

Prednisone

Back 32

Intermediate acting, medium potency steroid.
2) Possesses high glucocorticoid and low mineralocorticoid activity.
3) Must be converted in the liver to prednisolone for glucocorticoid activity.

Front 33

Dexamethasone

Back 33

Long acting, high potency steroid.
2) Possesses very high glucocorticoid and no mineralocorticoid activity.
3) Used in diagnosis of Cushing’s syndrome.

Front 34

Fludrocortisone

Back 34

Corticosteroid
1) Possesses high mineralocorticoid activity.
2) Increases reabsorption of sodium ions, and excretion of potassium and hydrogen ions.
3) Used in the treatment of Addison’s disease.
4) Side effects include hypertension and hypokalemia.

Front 35

Cosyntropin

Back 35

synthetic ACTH

Front 36

21-hydroxylase defect

Back 36

decreased cortisol;
and in the worse form= decreased aldosterone

HIGH androgens (conversion)

Treat with hydrocortisone

Front 37

Cushing’s Syndrome

Back 37

glucocorticoid excess

Front 38

Fluticasone

Back 38

Nasal sprays for allergic rhinitis.
2) Mechanism - decreases inflammation of mucosa.
3) Low potential for peripheral side effects (pituitary suppression).

Front 39

Beclomethasone

Back 39

Nasal sprays for allergic rhinitis.
2) Mechanism - decreases inflammation of mucosa.
3) Low potential for peripheral side effects (pituitary suppression).

Front 40

Metyrapone

Back 40

Treatment for Cushing's

-Inhibits conversion of 11-deoxycortisol to cortisol.
-Leads to increases in deoxycortisol and deoxycorticosterone (mineralocorticoid).

Front 41

Side effects of Glucocorticoids

Back 41

1) Chronic use (greater than a couple of weeks) with glucocorticoids (e.g. 20 mg prednisone) may lead to iatrogenic Cushing’s disorder.
2) Long term use associated with osteoporosis, diabetes, peptic ulcers and necrosis of the hip.
3) Abrupt withdrawal can cause adrenal insufficiency with fever, weakness, fatique, etc..

Front 42

Diethylstilbestrol

Back 42

Synthetic estrogen analogues that are effective orally

Front 43

Ethinyl Estradiol

Back 43

Synthetic estrogen analogues that are effective orally

Front 44

Medroxyprogesterone

Back 44

Medroxyprogesterone (Provera) used as injectable contraceptive.

Front 45

Norethindrone

Back 45

Synthetic progesterone analogues that are effective orally

Front 46

Levonorgestrel

Back 46

Synthetic progesterone analogues that are effective orally

Front 47

Desogestrel

Back 47

Synthetic progesterone analogues that are effective orally

Front 48

Desogestrel

Back 48

Synthetic progesterone analogues that are effective orally

Front 49

Clomiphene

Back 49

estrogen agonist and antagonist properties.
-Increases release of GnRH - increased LH/FSH release
-Direct ovarian action possible.

Front 50

Tamoxifen

Back 50

Selective Estrogen Receptor Modulators (SERMs).
2) Can have estrogen antagonist (breast) and agonist (bone) actions depending on tissue.
Therapeutic Uses:
1) First-line therapy of ER-positive breast cancer.
2) Prevention of breast cancer (high risk individuals).
3) Treatment of osteoporosis.
Side Effects:
1) Hot flashes and vaginal dryness.
2) Endometrial proliferation (risk of cancer) & DVT- Tamoxifene.

Front 51

Raloxifene

Back 51

Selective Estrogen Receptor Modulators (SERMs).
2) Can have estrogen antagonist (breast) and agonist (bone) actions depending on tissue.
Therapeutic Uses:
1) First-line therapy of ER-positive breast cancer.
2) Prevention of breast cancer (high risk individuals).
3) Treatment of osteoporosis.
Side Effects:
1) Hot flashes and vaginal dryness.

No effect on endometrium

Front 52

Mifepristone

Back 52

Progestin antagonist.
2) Glucocorticoid antagonist.

Therapeutic Use:
1) Approved as an abortifacient (up till day 49).
2) Given with prostaglandin analogue (Misoprostol).

Side Effects: excessive bleeding.

Front 53

Testosterone Enanthate

Back 53

Testosterone analogue given I.M.
Therapeutic Use:
1) Used in replacement therapy in hypogonadal boys.
2) Depot preparations most commonly used.

Front 54

Oxandrolone

Back 54

High anabolic (muscle building) to androgenic (virilizing) ratio.
2) Used by athletes in doses 10-200 times the pharmacol. dose along with stacking.
Side Effects:
1) Impairment of hepatic function.
2) Suppression of spermatogenesis.
3) Mascularization in women (hirsutism, acne, deepening of voice).

Front 55

Finasteride

Back 55

Inhibits conversion of testosterone to dihydrotestosterone by inhibiting 5 α-reductase enzyme.
Therapeutic Uses:
1) Used in treatment of benign prostatic hyperplasia - increases urine flow.
2) Treatment of male pattern baldness.

Front 56

Anastrozole

Back 56

aromatase inhibitor-
Decreases estrogen production by inhibiting aromatase enzyme.
2) Tissue specific inhibition - breast cancer.
3) First line therapy of ER-positive breast cancer.
4) Not appropriate for pre-menopausal patients.
5) Side effects as expected from lower estrogen.

Front 57

Chlorpropamide

Back 57

sulfonylureas.
- Increase insulin release in pancreatic beta cells.
- Some peripheral actions.

Front 58

Glyburide

Back 58

sulfonylureas.
- Increase insulin release in pancreatic beta cells.
-Some peripheral actions.

Front 59

Repaglinide

Back 59

“Glinides” lower blood glucose by stimulating insulin release.
-Fast onset and short duration of action compared with sulfonylureas.
-Hypoglycemia is most common side effect.

Front 60

Metformin

Back 60

Decreases hepatic glucose production.
-Does not increase insulin release.
-Can be used with sulfonylurea - e.g. chlorpropamide.
-Side effects include diarrhea (anorexia) and lactic acidosis (phenformin).

Front 61

Acarbose

Back 61

Reduces glucose absorption from GI tract.
-Inhibits glucosidase enzyme (prevents breakdown of complex sugars).
-GI distress (flatulence).

Front 62

Rosiglitazone

Back 62

Reduces insulin resistance.
Peroxisome proliferator-activated receptors (PPARs)
3) Decreases glycosylated hemoglobin.

Front 63

Exenatide

Back 63

Incretin mimetic similar to glucagon
-like peptide (GLP-1).
lowers glucagon
-Enhances glucose-dependent insulin release.
-Suppresses glucagon secretion.
-Dipeptidyl-peptidase-4 (DPP-4) degrades GLP-1. DPP-4 inhibitors (Sitagliptin) – monotherapy & in combination with other agents.

given subQ

Front 64

Sitagliptin

Back 64

inhibits breakdown of GLP-1