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Z.Fiser > Fiser.07.Pharmacology > Flashcards

Fiser.07.Pharmacology Flashcards

(90 cards)

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1
Q

What is first-pass metabolism?

A

Metabolism through the liver

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2
Q

What two modes of administration avoid first-pass metabolism?

A

sublingual and rectal

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3
Q

what aspect of a drug determines its skin absorption?

A

based on lipid solubility through the epidermis

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4
Q

What types of drugs can be absorbed into CSF? (2 characteristics)

A

restricted to nonionized drugs & lipid soluble

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5
Q

Which blood component is largely responsible for binding drugs?

A

albumin

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6
Q

what percent of penicillin is albumin-bound?

A

90%

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7
Q

what percent of warfarin is albumin-bound?

A

90%

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8
Q

why should you avoid sulfonamides in newborns?

A

displaces unconjugated bilirubin from albumin in newborns

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9
Q

what body part is tetracycline stored in?

A

stored in bone

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10
Q

what body part are heavy metals stored in?

A

bone

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11
Q

define zero-order kinetics?

A

constant amount of drug eliminated regardless of dose

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12
Q

define first-order kinetics?

A

drug eliminated proportional to dose

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13
Q

how many half-lives does it take for a drug to reach steady state?

A

5

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14
Q

define volume of distribution (formula)

A

amount of drug in the body divided by the amount of drug in plasma/blood Vd = (Total Drug) / (Drug in Plasma/Blood)

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15
Q

Where do drugs with high volumes of distribution have higher [x]? (extravascular & intravascular)

A

higher [x] in extravascular tissue (ex: fat)

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16
Q

define bioavailability

A

the fraction of unchanged drug reaching the systemic circulation

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17
Q

what is the bioavailability of IV drugs? How does this compare to PO drugs?

A

IV drugs assumed to have 100% bioavailability, PO drugs are less bioavailable

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18
Q

Define ED50

A

median effective dose: drug level at which desired effect is attained in 50% of patients

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19
Q

Define LD50

A

lethal dose: drug level at which death occurs in 50% of patients

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20
Q

What does “hyperactive” mean in pharmacology?

A

effect at an unusually low dose

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21
Q

define “tachyphylaxis” in pharmacology

A

tolerance after only a few doses

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22
Q

define “potency” in pharmacology

A

dose required for effect

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23
Q

define “efficacy” in pharmacology

A

ability to achieve result without untoward effect

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24
Q

where in the hepatocyte does drug metabolism occur? (2)

A

smooth ER; P450 system

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25
name four reactions that occur in Phase 1 of drug metabolism & 2 required substrates
demethylation; oxidation; reduction; hydrolysis mixed function oxidases, require NADPH / O2
26
name two reactions that occur in phase 2 of drug metabolism and its overall effect
glucuronic acid attaches; sulfates attach --\> this results in a water-soluble metabolite to make it ready for excretion
27
Describe the process of enterohepatic circulation of drugs and give an example of a drug that undergoes it
biliary excreted drugs may become deconjugated in intestines with reabsorption, sometimes in active form. Ex: cyclosporine
28
name 11 inhibitors of P450
My - Macrolides; Sullen - Sulfonamides; Robot - Ritonavir; And Amiodarone; A cute - Acute alcohol abuse; Kangaroo - Ketoconazole; Couldn’t - Ciprofloxacin; Quickly - Quinidine; Get the - Gemfibrozil; Cement -Cimetidine; Gliding on - Grapefruit juice; Ice - Isoniazid
29
name 8 inducers of P450
Momma - Modafinil; Da - Dilantin; Grizzly - Griseofulvin; Bear - Barbituates; Cruelly - Chronic alcohol use; Steals - St. John’s wort / Cigarette Smoke; Phen-phen (and) - Phenytoin, Phenobarbital; While - Warfarin; Racing- Rifampin; Cars - Carbamazepine / Cruciform Vegetables
30
what is the most important organ for eliminating most drugs?
kidney
31
name two ways the kidney eliminates drugs
glomerular filtration; tubular secretion
32
which type of drug is water-soluble? (polar v. nonpolar)
polar drugs (ionized)
33
which type of drug is more likely to be fat-soluble (polar v. nonpolar)
nonpolar drugs (nonionized)
34
which type of drug is more likely to be eliminated in unaltered form? (polar v. nonpolar)
polar drugs (ionized)
35
which type of drug is more likely to be metabolized before excretion? (polar v. nonpolar)
nonpolar drugs (nonionized)
36
What metabolic process results in uric acid?
purine metabolism --\> uric acid
37
what is the underlying (pathophys) of gout?
caused by uric acid buildup
38
name four drugs that treat gout
colchicine; indomethacin; allopurinol; probenecid
39
what is the MOA of colchicine?
antiinflammatory; binds tubulin & inhibits migration of WBCs
40
what is the MOA of indomethacin?
NSAID, reversible COX inhibitor = reduced prostaglandin synthesis
41
what is the MOA of allopurinol?
xanthine oxidase inhibitor, blocks uric acid formation from xanthine
42
what is the MOA of probenecid?
increased renal secretion of uric acid
43
what is the MOA of cholestyramine?
binds bile acids in gut --\> forces body to resynthesize bile acid --\> lowers total body cholesterol
44
name one adverse effect of cholestyramine and how it occurs
cholestyramine can bind vitamin K in the gut --\> increased bleeding tendency
45
what is the MOA of statins?
HMG-CoA reductase inhibitor
46
name two AEs of statins
liver dysfunction; rhabdomyolysis
47
what is the MOA of niacin?
lipid lowering agent by inhibiting cholesterol synthesis
48
name 1 AE of niacin and its tx
flushing, tx with ASA
49
what is the MOA of promethazine?
phenergan is an antiemetic by inhibiting dopamine receptors
50
name 1 AE of promethazine and its tx
AE: tardive dyskinesia; tx: diphenydramine (Benadryl)
51
what is the indication and MOA of metoclopramide?
Reglan is a prokinetic, used to increase gut/gastric motility. MOA: inhibits dopamine Rs
52
what is the MOA of ondansetron?
Zofran is an antiemetic that is a central-acting serotonin-R inhibitor
53
what is the MOA of omeprazole
PPI, blocks H/K-ATPase in stomach parietal cells
54
what is the MOA of cimetidine/ranitidine
H2-receptor (histamine) blocker, therefore reduce acid in the stomach
55
what is the indication and MOA of octreotide?
long-acting somatostatin analogue, therefore reduce gut secretions
56
name the MOA of digoxin
inhibits Na/K-ATPase, therefore increase myocardial calcium
57
name 2 cardiac effects of digoxin
slows AV conduction, inotrope
58
is digoxin cleared with hemodialysis?
nope
59
why is digoxin a/w mesenteric ischemia?
digoxin can reduce blood flow to intestines = mesenteric ischemia
60
name the electrolyte abnormality a/w digoxin & 2 resulting effects
digoxin --\> hypokalemia --\> increased cardiac sensitivity to digitalis --\> can lead to arrhythmias/AV block
61
name the 5 AEs a/w digoxin?
reduced blood flow to intestines; hypokalemia; visual changes (yellow hue); arrhythmias; fatigue
62
name two indications to use amiodarone
acute atrial & ventricular arrhythmias
63
name 3 AEs of amiodarone
pulmonary fibrosis with prolonged use; hypothyroidism; hyperthyroidism
64
which arrhythmia can be treated with magnesium?
torsades de pointes (Vtach)
65
what is the role of ACE-inhibitors in CHF patients
best single agent to increase survival in CHF patients
66
what is the MOA of ACE inhibitors?
angiotensin-converting enzyme inhibitors
67
why use ACE-inhibitors s/p MI?
prevents CHF s/p MI
68
why are ACE inhibitors used in patients with HTN/DM?
prevents progression of renal dysfx in pts with HTN/DM
69
why should you avoid ACE-inhibitors in patients with renal artery stenosis?
can precipitate renal failure
70
why are beta blockers used s/p MI
best single agent to improve survival after MI
71
why do you use beta blockers in patients with LV failure?
may prolong life in patients with severe LV failure
72
what 2 postop complications are prevented by beta blockers
postop MI & Afib
73
what is the MOA and effect of atropine
acethylcholine antagonist = increased HR
74
what is the MOA and indication for metyrapone?
inhibits adrenal steroid synthesis; indicated for adrenocortical CA
75
what is the MOA and indication for aminoglutethimide?
inhibits adrenal steroid synthesis; used for adrenocortical CA
76
what is the pharmacologic structure of leuprolide
analogue of GnRH and LHRH
77
what is the effect of continuous admin of leuprolide
paradoxic effect, inhibits release of LH/FSH from the pituitary
78
which cancer is treated with leuprolide?
metastatic prostate CA
79
what is the MOA of NSAIDs
inhibit prostaglandin synthesis
80
name 3 ways NSAIDs increase risk of peptic ulcers
reduce mucus; reduce bicarb; increase acid production
81
what is the MOA of misoprostol?
a PGE1 derivative, a protective prostaglandin
82
what is misoprostol used to treat?
prevent peptic ulcer disease in patients on chronic NSAIDs
83
what is the MOA of Haldol?
antipsychotic; inhibits dopamine receptors
84
what is the 1 AE of Haldol and its tx
extrapyramidal sx; tx = Benadryl
85
name of 4 S/Sx of ASA poisoning?
tinnitus; HA; nausea; vomiting
86
what are the 1st and 2nd acid/base effects of ASA poisoning?
1st: respiratory alkalosis; 2nd: metabolic acidosis
87
what is the MC side effect of gadolinium?
nausea
88
what is the MC side effect of iodine contrast?
nausea
89
what is the MC side effect of iodine contrast requiring medical treatment?
dyspnea
90
what is the tx for tylenol overdose
N-acetylcysteine

Z.Fiser (22 decks)

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