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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
Drugs to treat central diabetes insipidus: | Central DI is loss of renal urine concentration due to *lack of ADH*
desmopressin chlorpropramide carbamazepine clofibrate
26
prostaglandin analogs used to promote uterine contraction/labor in therapeutic abortion
misoprostol (PGE1) | dinoprostone (PGE2)
27
stimulates uterine contraction & milk ejection from mammary glands
oxytocin
28
stimulate uterine contraction & used to reduce post delivery bleeding (post-partum hemorrhage)
1. ergonovine 2. methylergonovine "er gonna stop bleeding now"
29
Drugs used to stop preterm labor (5) by relaxing uterine smooth muscle
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)
30
recombinant FSH
follitropin
31
mainly FSH
urofollitropin
32
LH & FSH
menotropins
33
acts at the LH receptor
hCG
34
diagnostic agent that enhances radioactive iodine uptake
thyrotropin
35
POMC-derived peptide for diagnostic use
cosyntropin
36
given in pulsatile form and is short-acting -> | stimulates LH/FSH release
gonadorelin
37
long-acting GnRH analogs used to suppress LH/FSH
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
GnRH receptor antagonists used to suppress LH/FSH by blocking the GnRH receptor at the pituitary
1. ganirelix 2. cetrorelix Those eggs are going to be "relix" because their release is suppressed.
39
Therapeutic use of LH/FSH suppression for what?
- adjunct to infertility treatment - precocious puberty - chemical castration - prostate and breast cancer
40
recombinant human GH used to increase production of IGF1 in GH deficiency
somatropin
41
dopamine receptor agonists used to decrease prolactin secretion & decrease GH release Use: treatment of pituitary adenomas
1. bromocriptine | 2. cabergoline
42
somatostatin analogs more selective for the pituitary
1. octreotide | 2. lanreotide
43
GH receptor antagonist used to treat acromegaly
pegvisomant | "Peg's got some big hands & feet."
44
T3
liothyronine
45
T4
levothyroxine
46
T3 & T4
liotrix
47
increase binding of T4 to TBG
estrogens
48
decrease binding of T4 to TBG
glucocorticoids androgens salicylates
49
inhibits peripheral diodination of T4 to T3 | [inhibits peroxidase iodide oxidation & coupling of DIT & MIT]
propylthiouracil (PTU) half life: 75 min (very short) Adverse: agranulocytosis
50
longer half-life thioureylene | [inhibits peroxidase iodide oxidation & coupling of DIT & MIT]
methimazole | Adverse: agranulocytosis (most common it's a rash though)
51
directs follicular development | spermatogenesis
FSH
52
stimulates testicular androgen production
LH
53
interfere with iodide concentration
thiocyanate perchlorate fluroborate
54
iodine isotope used for treatment of metastatic thyroid carcinoma & given with TSH to enhance its uptake
I-131
55
used as pre-op treatment for thyroidectomy, thyrotoxic crisis; effects in 1-3 days & goal is to get patient euthyroid before surgery
Iodide
56
glucocorticoids with only GR effects | synthetic modification prevents interaction with MR
1. Triamcinolone 2. betamethasone 3. dexamethasone
57
corticosteroid with GR activity but very potent MR activity; used in salt-wasting
fludrocortisone
58
enzyme in the kidney that can convert cortisol to cortisone
11 beta HSD2 | no effect on aldosterone because of "protected OH"
59
enzyme in the liver that can convert prednisone to prednisolone
11 beta HSD1
60
MR antagonists
spironolactone | eplerenone
61
GR antagonist that was developed as a PR antagonist
mifepristone | This is the only glucocorticoid receptor antagonist; no pure one. Can be used to treat cortisol excess.
62
inhibitors of corticosteroid biosynthesis
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
antagonizes estrogen feedback effect in the pituitary to induce ovulation
clomiphene
64
full estrogen receptor antagonist, in all tissues, used to treat progressive breast cancer after tamoxifen therapy
fulvestrant | Adverse: osteoporosis
65
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)
tamoxifen | Monitor endometrial lining for thickening since it can cause endometrial cancer
66
derivative of tamoxifen
toremifene
67
estrogenic for bone anti-estrogen for breast, endometrium developed to treat osteoporosis but not sure if it is as beneficial in breast cancer yet
raloxifene
68
PR and GR antagonist used for postcoital implantation abortion in Europe
mifepristone
69
decreases bone resorption | decreases calcium and phosphate reabsorption in the kidney
calcitonin
70
recombinant PTH used to promote bone growth
teriparatide
71
nonsteroidal competitive reversible inhibitors of aromatase | Adverse: decreased production of estrogen in bone
anastrozole | letrozole
72
less potent estrogen used for HRT
estrone sulfate
73
highly potent synthetic estrogen used for oral contraceptives to suppress LH and FSH stimulation
ethinyl estradiol
74
synthetic progestins used in oral contraceptives | Adverse: adrogenic side effects (acne, weight gain, decreased HDL, increased LDL)
1. norethindrone | 2. norgestrel
75
synthetic progestins that have less androgenic activity
1. norgestimate | 2. desogestrel
76
progestin agonist that is a spironolactone derivative so it also is a MR antagonist
drospirenone
77
What is the difference between triphasic or biphasic oral contraceptive? What is the issue with triphasic?
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
morning after pill (Plan B)
levonorgestrel
79
progesterone receptor modulator with mixed agonist/antagonist effects, suppresses the LH surge & ovulation
ulipristal
80
steroidal suicide inactivator of aromatase (binds irreversibly); very potent Use: adjunct with tamoxifen Adverse: decreased estrogen production in bone
exemstane
81
How does administering large dose of iodides treat hyperthyroidism?
inhibits proteolysis of thyroglobulin, so thyroid hormone is synthesized but not released into the blood
82
Functions of calcitonin
promotes absorption of calcium by skeletal system | inhibits resorption of bone by osteoclasts

Endocrine (11 decks)

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