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Endocrine > Pharm Drugs > Flashcards

Pharm Drugs Flashcards

1
Q

short-acting synthetic insulin

A
  1. lispro
  2. aspart
  3. glulisine
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2
Q

short-acting human insulin

A

regular

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3
Q

intermediate insulin

A
  1. NPH * (bound to protamine which causes “time release”)

2. Lente (high zinc prevents mixing)

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4
Q

long-acting insulin

stable hexamer that lasts 12-14 hrs to mimic basal insulin

A
  1. ultralente
  2. glargine (2 arginines added)
  3. detemir (attached myristic acid to increase albumin binding)
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5
Q

Oral agent that stimulates insulin release (like glucose) by binding to potassium channel and closes it. Use Type 2 DM

A

sulfonylureas

Side effect: hypoglycemia, alcohol-induced flush, hyponatremia

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6
Q

First generation oral agents used to stimulate insulin release (sulfonylureas)

A
  1. tolbutamide
  2. chlorpropamide
  3. tolazamide
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7
Q

Second generation oral agents used to stimulate insulin release (sulfonylureas)

A
  1. glyburide
  2. glipizide
  3. glimepiride
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8
Q

Oral agents that stimulate insulin release but do not contain sulfur

A
  1. repaglinide

2. nateglinide

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9
Q

recombinant IGF1 with binding protein
Use: GH resistance or mutation of GH receptor
Adverse: hypoglycemia

A

mecasermin

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10
Q

decreases hepatic glucose production

contraindicated in renal impairment & with history of lactic acidosis

A

Metformin

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11
Q

increases insulin action by binding to PPAR-gamma and increasing transcription of glucose transporters (ex: GLUT4)
Adverse: fluid retention, weight gain, edema

A
  1. pioglitazone
  2. rosiglitazone
  3. troglitazone (pulled due to liver failure)
    * pioglitazone has increased risk bladder cancer
    * rosiglitazone has increased risk of MI & CVA
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12
Q

inhibit enzymes of the small intestine that digest carbohydrates (brush border enzymes): alpha glucosidase

A
  1. acarbose
  2. miglitol
    Adverse: flatulence & diarrhea
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13
Q

amylin analog, decreasing rate of gastric emptying & promoting satiety, while suppressing glucagon release;
subQ injection after meals

A

pramlinitide

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14
Q

bile acid binding resin that lowers blood glucose by an unknown mechanism

A

colesevelam

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15
Q

glucagon-like peptide 1 analogs that help augment glucose-dependent insulin secretion; must be given by injection since these are peptides

A
  1. exenatide

2. liraglutide

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16
Q

inhibit DPP-4 which is the enzyme that degrades the incretin GLP-1
Increased incretins -> decreases glucagon -> increased secretion of insulin

A
  1. sitagliptin
  2. saxagliptin
    (3. linagliptin)
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17
Q

what may lead to higher incidence of folate deficiency in pregnant women?

A

oral contraceptive use history

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18
Q

What causes nausea & vomiting in pregnancy?

A

hCG

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19
Q

What are the major target organs for insulin?

A 
liver (increased GLUT2)
skeletal muscle (increased GLUT4)
adipose (increased GLUT4, activation of plasma lipoprotein lipase, reduced intracellular lipolysis)
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20
Q

When would insulin secretagogues (ex: sulfonylureas) be ineffective?

A

type 1 diabetes

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21
Q

stimulates rate and force of contraction of the heart; useful for beta-blocker cardiac depression

A

glucagon

Use: severe hypoglycemia & beta-blocker overdose

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22
Q

thiazide derivative that hyperpolarizes potassium channels & relaxes smooth muscle -> used to treat hypertensive crisis but can also be used to treat hypoglycemia by inhibiting insulin release

A

diazoxide

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23
Q

ADH receptor antagonists

A
  1. conivaptan
  2. tolvaptan
    Don’t be vap-id. You don’t need all that water.
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24
Q

used for lithium induced diabetes insipidus (nephrogenic)

Note: nephrogenic DI is loss of the kidney’s ability to concentrate urine due to lack of response to ADH

A 
amiloride
Other drugs used for nephrogenic diabetes insipidus:
thiazides
indomethacin (COX inhibitor)
have adequate water intake
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25
Q

Drugs to treat central diabetes insipidus:

Central DI is loss of renal urine concentration due to lack of ADH

A

desmopressin
chlorpropramide
carbamazepine
clofibrate

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26
Q

prostaglandin analogs used to promote uterine contraction/labor in therapeutic abortion

A

misoprostol (PGE1)

dinoprostone (PGE2)

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27
Q

stimulates uterine contraction & milk ejection from mammary glands

A

oxytocin

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28
Q

stimulate uterine contraction & used to reduce post delivery bleeding (post-partum hemorrhage)

A
  1. ergonovine
  2. methylergonovine
    “er gonna stop bleeding now”
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29
Q

Drugs used to stop preterm labor (5) by relaxing uterine smooth muscle

A
  1. terbutaline (beta2 agonist)
  2. ritodrine (beta2 agonist)
  3. nifedipine (calcium channel blocker)
  4. indomethacin (COX inhibitor -> inhibits prostaglandin synthesis)
  5. atosiban (oxytocin receptor antagonist)
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30
Q

recombinant FSH

A

follitropin

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31
Q

mainly FSH

A

urofollitropin

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32
Q

LH & FSH

A

menotropins

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33
Q

acts at the LH receptor

A

hCG

34
Q

diagnostic agent that enhances radioactive iodine uptake

A

thyrotropin

35
Q

POMC-derived peptide for diagnostic use

A

cosyntropin

36
Q

given in pulsatile form and is short-acting ->

stimulates LH/FSH release

A

gonadorelin

37
Q

long-acting GnRH analogs used to suppress LH/FSH

A
  1. leuprolide
  2. histrelin
  3. nafarelin (nasal spray)
  4. goserelin
  5. triptorelin
    by exposing pituitary GnRH receptors to constant rather than pulsatile GnRH, the receptors will be downregulated
38
Q

GnRH receptor antagonists used to suppress LH/FSH by blocking the GnRH receptor at the pituitary

A
  1. ganirelix
  2. cetrorelix
    Those eggs are going to be “relix” because their release is suppressed.
39
Q

Therapeutic use of LH/FSH suppression for what?

A
  • adjunct to infertility treatment
  • precocious puberty
  • chemical castration
  • prostate and breast cancer
40
Q

recombinant human GH used to increase production of IGF1 in GH deficiency

A

somatropin

41
Q

dopamine receptor agonists used to decrease prolactin secretion & decrease GH release
Use: treatment of pituitary adenomas

A
  1. bromocriptine

2. cabergoline

42
Q

somatostatin analogs more selective for the pituitary

A
  1. octreotide

2. lanreotide

43
Q

GH receptor antagonist used to treat acromegaly

A

pegvisomant

“Peg’s got some big hands & feet.”

44
Q

T3

A

liothyronine

45
Q

T4

A

levothyroxine

46
Q

T3 & T4

A

liotrix

47
Q

increase binding of T4 to TBG

A

estrogens

48
Q

decrease binding of T4 to TBG

A

glucocorticoids
androgens
salicylates

49
Q

inhibits peripheral diodination of T4 to T3

[inhibits peroxidase iodide oxidation & coupling of DIT & MIT]

A

propylthiouracil (PTU)
half life: 75 min (very short)
Adverse: agranulocytosis

50
Q

longer half-life thioureylene

[inhibits peroxidase iodide oxidation & coupling of DIT & MIT]

A

methimazole

Adverse: agranulocytosis (most common it’s a rash though)

51
Q

directs follicular development

spermatogenesis

A

FSH

52
Q

stimulates testicular androgen production

A

LH

53
Q

interfere with iodide concentration

A

thiocyanate
perchlorate
fluroborate

54
Q

iodine isotope used for treatment of metastatic thyroid carcinoma & given with TSH to enhance its uptake

A

I-131

55
Q

used as pre-op treatment for thyroidectomy, thyrotoxic crisis; effects in 1-3 days & goal is to get patient euthyroid before surgery

A

Iodide

56
Q

glucocorticoids with only GR effects

synthetic modification prevents interaction with MR

A
  1. Triamcinolone
  2. betamethasone
  3. dexamethasone
57
Q

corticosteroid with GR activity but very potent MR activity; used in salt-wasting

A

fludrocortisone

58
Q

enzyme in the kidney that can convert cortisol to cortisone

A

11 beta HSD2

no effect on aldosterone because of “protected OH”

59
Q

enzyme in the liver that can convert prednisone to prednisolone

A

11 beta HSD1

60
Q

MR antagonists

A

spironolactone

eplerenone

61
Q

GR antagonist that was developed as a PR antagonist

A

mifepristone

This is the only glucocorticoid receptor antagonist; no pure one. Can be used to treat cortisol excess.

62
Q

inhibitors of corticosteroid biosynthesis

A
  1. mitotane (lyses adrenal tumor cells)
  2. ketoconazole (inhibits SCC in high dose; inhibits 17,20-lyase at lower doses)
  3. metyrapone, etomidate (11 hydroxylase)
63
Q

antagonizes estrogen feedback effect in the pituitary to induce ovulation

A

clomiphene

64
Q

full estrogen receptor antagonist, in all tissues, used to treat progressive breast cancer after tamoxifen therapy

A

fulvestrant

Adverse: osteoporosis

65
Q

mixed agonist & antagonist SERM used to prevent recurrent breast cancer
anti-estrogen in breast cancer tissue
estrogenic actions on endometrium (can cause endometrial cancer)
estrogenic bone actions (positive effect)

A

tamoxifen

Monitor endometrial lining for thickening since it can cause endometrial cancer

66
Q

derivative of tamoxifen

A

toremifene

67
Q

estrogenic for bone
anti-estrogen for breast, endometrium
developed to treat osteoporosis but not sure if it is as beneficial in breast cancer yet

A

raloxifene

68
Q

PR and GR antagonist used for postcoital implantation abortion in Europe

A

mifepristone

69
Q

decreases bone resorption

decreases calcium and phosphate reabsorption in the kidney

A

calcitonin

70
Q

recombinant PTH used to promote bone growth

A

teriparatide

71
Q

nonsteroidal competitive reversible inhibitors of aromatase

Adverse: decreased production of estrogen in bone

A

anastrozole

letrozole

72
Q

less potent estrogen used for HRT

A

estrone sulfate

73
Q

highly potent synthetic estrogen used for oral contraceptives to suppress LH and FSH stimulation

A

ethinyl estradiol

74
Q

synthetic progestins used in oral contraceptives

Adverse: adrogenic side effects (acne, weight gain, decreased HDL, increased LDL)

A
  1. norethindrone

2. norgestrel

75
Q

synthetic progestins that have less androgenic activity

A
  1. norgestimate

2. desogestrel

76
Q

progestin agonist that is a spironolactone derivative so it also is a MR antagonist

A

drospirenone

77
Q

What is the difference between triphasic or biphasic oral contraceptive? What is the issue with triphasic?

A

the changes in the amount of progestin
The triphasic is the closest to normal physiology, so if a pill is missed at the time of ovulation, might result in ovulation.

78
Q

morning after pill (Plan B)

A

levonorgestrel

79
Q

progesterone receptor modulator with mixed agonist/antagonist effects, suppresses the LH surge & ovulation

A

ulipristal

80
Q

steroidal suicide inactivator of aromatase (binds irreversibly); very potent
Use: adjunct with tamoxifen
Adverse: decreased estrogen production in bone

A

exemstane

81
Q

How does administering large dose of iodides treat hyperthyroidism?

A

inhibits proteolysis of thyroglobulin, so thyroid hormone is synthesized but not released into the blood

82
Q

Functions of calcitonin

A

promotes absorption of calcium by skeletal system

inhibits resorption of bone by osteoclasts

Endocrine (11 decks)

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