Endocrine Drugs

Question 1

Octreotide

Answer 1

Somatostatin analog
(GH inhibiting horone)
uses: acromegaly, suppress ectopic hormone production by tumors

goal: decrease GH and IGF-1 levels to normal

Question 2

Somatotropin

Answer 2

recombinant GH
ROA- parenteral
Uses- pituitary dwarfism

Question 3

Pegvisomant

Answer 3

GH receptor antagonist (binds to GH receptor but doesn’t activate JakStat or stimulate IGF-1)
uses: Acromegaly

Question 4

Mecasermin

Answer 4

recombinant IGF-1

Laron Syndrome

Question 5

Bromocriptine

Answer 5

dopamine analog
DA receptor agonist (D2>D1)
reduces prolactin release
given orally
used for prolacinoma, drug induced via antipsychotics or metoclopramide
adverse effects – gynecomastia, galactorrhea, inappropriate lactiation, infertility, nausea, vomiting

Question 6

Desmopressin

Answer 6

Vasopressin analog
ROA- oral, intranasal, parenteral
MOA- v2 receptor agonist in nephron
Uses- central diabetes insipidus, von willebrand disease type I, hemophilia A, nocturnal enuresis

Question 7

Sermorelin

Answer 7

GHRH

uses: diagnostic
orphan drug status– GH deficiency, AIDS associated weight loss

Question 8

Conivaptan

Answer 8

v2 receptor antagonist

SIADH

Question 9

Oxytocin

Answer 9

IV

induction of labor, postpartum uterine bleeding

Question 10

Vasopressin

Answer 10

MOA– v1 activatior of pressor response –> inc. blood pressure
Therapeutic uses:
- advanced cardiac life support
- bleeding esophageal varices

Question 11

Alprostadil

Answer 11

PGE1

Question 12

Bimatoprost

Answer 12

PGF2alpha

Question 13

Carboprost Tromethamine

Answer 13

PGF2alpha analog
IM
uses: 2nd trimester abortion, post partum hemorrhaging

diarrhea/vomiting, nausea, endometritis, sepitic shock,

Question 14

Dinoprostone

Answer 14

PGE2
vaginal insert, gel, suppository
uses: 2nd trimester abortion, missed abortion, evacuation of fetus, cervical ripening (collagenase), hydatiform mole

fever, nausea/vomiting, abdominal pain

Question 15

Latanoprost

Answer 15

PGF2a

irreversible brown pigmentation of eyelashes

Question 16

Tafluprost

Answer 16

PGF2a

Question 17

Travoprost

Answer 17

PGF2a analog

AEs: inc pigmentation of iris and periorbital tissue, elongation and growth of eyelashes

Question 18

Epoprostenol

Answer 18

therapy of pulmonary arterial hypertension

Question 19

Misoprostol

Answer 19

prevention of NSAID-induced gastric ulcers

induction of early abortion

Question 20

T4- Levothyroxine

Answer 20

(hypothyroidsm)
treatment of choice for replacement therapy
IV
long half life

Question 21

T3– Liothyronine

Answer 21

active thyroid hormone
given for hypothyroidsm
cardiotoxic
MOA-- IV
can be used for immediate therapy followed by t4 therapy

Question 22

propylthiouracil (thioamine)

Answer 22

MOA– blocks iodination (thyroperoxidase), conjugation, and 5-deiodinase (actiaves T3 in target tissues)
-used for: mild thyrotoxicosis and preparation for subtotal thyroidectomy
slow onset of action
inhibit peripheral deiodination of T3 and T4
AE- agranulocytosis
preferred in pregnancy

Question 23

Radioactive Iodine

Answer 23

I-131: MOA destroys thyroid gland tissue (B and gama radiation)
AE = must manage hypothyroidism with T4

I-123: emits gama particles– used for diagnosis and imaging. shorter half life than 131 (8 hrs vs 8 days)

Question 24

Potassium iodide (KI)

Answer 24

MOA– inhibit hormone release, organificatio nad decrease size and vascularity of hyperplastic gland

Wolf-Chaikoff effect– acute inhibition of iodination of tyrosine (transient– not for long term effect)
use: thyroid storm and surgical preparation.

Question 25

Propanolol

Answer 25

MOA- blocks B-adrenergic receptor and inhibits conversion of T4 to T3 helps control symptoms of hyperthyroidism

Question 26

Glimepriride/glyburide

Answer 26

insulin secretagogue increase insulin production by pancreas bind to SUR1 subunit of ATP sensitive K+ channel on B-cells and inactivates channel (analogous to fed state)

Question 27

Metformin

Answer 27

Insulin sensitizer in liver decreases glucose production by liver MOA: activates AMPK: decreases hepatic gluconeogenesis, glycogenolysis and peripheral resistance to insulin). Usually staritng treatment for DM II

Question 28

Rosiglitazone

Answer 28

insulin sensitizer in muscle and other tissues. increase uptake of sugar by muscle and fat cells MOA-- selective PPARgama agonist causing activation of insulin-responsive genes regulating carbohydrate and lipid metabolism site-- fat (also muscle and liver) effects = increased adiponectin and decrease in FFA and resistin

Question 29

Acarbose

Answer 29

alpha glucosidase inhibitor for DMII inhibits breakdown of starch --> monosaccharides slows absorption of carbs, blunts postprandial rise in plasma glc, increases noxious smell/freqent bloating and farting

Question 30

Exenatide

Answer 30

insulin secretagogue injection GLP1 receptor agonist// incretin mimetic suppresses glucagon secretion, slows gastric emptying, decreases appetite

Question 31

Cholecalciferol (ergocalciferol-- plant form of Vit D//D2)

Answer 31

animal form of Vit D (d3) converted to calcitriol ("active" form) used: replacement therapy (rickets, osteomalacia); psoriasis, some cancer, innate immunity effects: inc. intestinal Ca2+ and PO42- absorption provides ca2+ and PO42- for bone mineral formation vit D won't be effective in regulation of Ca2+ homeostasis during renal failure (need calcitriol)

Question 32

Calcitriol

Answer 32

biologically active form = 1,25(OH)2-D D2 and D3 converted in Liver then Kidney --> calcitriol. used for RENAL FAILURE. replace calcitriol due to loss of 1-hydroxylation in nephrons. Low calcitriol leads to inadequate intestinal Ca2+ absorption which leads to hypocalcemia and subsequent hyperparathyroidism, bone resportion and continuing cascade of bone disease calcitriol is used to correct calcium homeostasis in this condition AE-- hypercalcemia

Question 33

Teriparatide

Answer 33

ROA- parenteral (SC) MOA- parathyroid hormone (1-34) analog use- promote bone formation in severe osteoporosis

Question 34

Calcitonin

Answer 34

hormone replacement ROA- intranasal or SC (salmon calcitonin) use- direct suppression osteoclastic activity (osteoporosis, hypercalcemia of malignancy, Paget's disease) usually not primary therapy for anything-- useful actuely in some forms of hypercalcemia when waiting on other approaches to kick in.

Question 35

Cinacalcet

Answer 35

MOA- calcium memitic (CaSR agonist) --> decreases PTH release (in presence of Ca2+). Helpful in renal failure patients preventing ongoing osteoporosis. Also should provide calcitriol to patient used: primary hyperparathyroidism, secondary hyperparahtyroidsim in renal disease, parahtyoid carcinoma CaSR becomes sensitized to serum Ca2+ and changes rate of PTH secretion so that is is suppressed by lower than normal amounts

Question 36

hydrocortisone (cortisol)

Answer 36

Glucocorticoids addison crisis (acute adrenal insufficiency/crisis) IV until stable followed by oral therapy Can get addisonian crisis if you abruptly stop taking glucocorticoids (i.e. Prednisone and dexamethasone). Glucocorticoid hormones (prednisone/dexa), often used to treat inflammatory illnesses like rheumatoid arthritis & asthma block the release of CRH and ACTH. Normally, CRH instructs the pituitary gland to release ACTH. If CRH levels drop, the pituitary is not stimulated to release ACTH, and the adrenals then fail to secrete sufficient levels of cortisol.

Question 37

fludrocortisone

Answer 37

mineralocorticoid increas dose during exercise, sweating, diarrhea used to replace missing aldosterone in different forms of adrenal insufficiency (such as addisons)

Question 38

Ketoconazole

Answer 38

coricosteroid synthesis inhibitor anti-fungal agent inhibits several P450 enzymes involved in steroid biosynthesis Cushing's inhibits androgen synthesis (can cause gynecomastia in males)

Question 39

Spironolactone

Answer 39

mineralocorticoid receptor antagonist aldosterone receptor antagonist-- K+ sparing diuretic relatively slow onset- wait for proetein synthesis effects of aldosterone to wear off following initial blockade also binds to androgen receptor (cometes with DHT) and also used as anti-androgen

Question 40

Mifeprisotone

Answer 40

glucocorticoid receptor antagonist management of Cushing's syndrome progesterone antagonist, too