Chapter 7: Medicines and Pharmacology Flashcards

1
Q

Drug admin: do not pass through liver first (no first-pass metabolism)

A

Sublingual and rectal drugs

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2
Q

Drug admin: based on lipid solubility through the epidermis

A

Skin absorption

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3
Q

Drug admin: restricted to nonionized, lipid-soluble drugs

A

CSF absorption

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4
Q

Largely responsible for binding drugs (PCNs and warfarin 90% bound)

A

Albumin

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5
Q

Will displace unconjugated bilirubin from albumin in newborns (avoid in newborns)

A

Sulfonamides

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6
Q

Where are tetracycline and heavy metals stored?

A

In bone

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7
Q

Constant amount of drug is eliminated regardless of dose

A

Zero order kinetics

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8
Q

Drug eliminated proportional to dose

A

First order kinetics

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9
Q

How many half-lives for a drug to reach steady state?

A

5

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10
Q

Amount of drug in the body divided by the amount of drug in plasma or blood.

A

Volume of distribution

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11
Q

Drugs with a high volume of distribution: extravascular vs intravascular concentratoins

A

High volume of distribution: higher concentrations in extravascular compartment (e.g., fat tissue) compared with intravascular concentrations

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12
Q

Fraction of unchanged drug reaching the systemic circulation

A

Bioavailability

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13
Q

Bioavailability intravenous drugs

A

100% bioavailability IV drugs, less other routes (e.g., oral)

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14
Q

Drug level at which desired effect occurs in 50% of patients

A

ED-50

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15
Q

Drug level at which death occurs in 50% of patients

A

LD-50

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16
Q

Effect at an unusually low dose

A

Hyperactive

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17
Q

Tolerance after only a few doses

A

Tachyphylaxis

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18
Q

Dose required for effect

A

Potency

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19
Q

Ability to achieve result without untoward effect

A

Efficacy

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20
Q

Drug metabolism: components of Phase 1

A

Demethylation, oxidation, reduction, hydrolysis reactions (mixed function oxidases, requires NADPH/oxygen)

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21
Q

Drug metabolism: components of Phase 2

A

Glucuronic acid (#1) and sulfates attached (forms water-soluble metabolite); usually inactive and ready for excretion.

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22
Q

Def: biliary excreted drugs may become deconjugated in intestines with reabsorption, some in active form

A

Entero-hepatic recirculation (eg, cyclosporine)

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23
Q

Inhibitors of p-450

A

Cimetidine. Isoniazid. Ketoconazole. Erythromycin. Cipro. Flagyl. Allopurinol. Verapamil. Amiodarone. MAOIs. Disfulfiram.

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24
Q

Inducers of p-450

A

Cruciform vegetables. ETOH. Insecticides. Cigarette smoke. Phenobarbital (barbiturates). Dilantin. Theophylline. Warfarin.

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25
Q

Most important organ for eliminating most drugs (glomerular filtration and tubular secretion)

A

Kidney

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26
Q
  • Ionized
  • Water soluble
  • More likely to be eliminated in unaltered form
A

Polar drugs

27
Q
  • Non-ionized
  • Fat soluble
  • More likely metabolized before excretion
A

Nonpolar drugs

28
Q

Caused by uric acid build up

- End product of purine metabolism

A

Gout

29
Q

Anti-inflamamtory

- Binds tubulin and inhibits migration of WBCs

A

Colchicine

30
Q
  • NSAID

- Inhibits prostaglandin synthesis (reversible cyclooxygenase inhibitor)

A

Indomethacin

31
Q
  • Xanthine oxidase inhibitor

- Blocks uric acid formation from xanthine

A

Allopurinol

32
Q

Increases renal secretion of uric acid

A

Probenecid

33
Q

Binds bile acids in gut, forcing body to resynthesize bile acids from cholesterol, thereby lowering body cholesterol; can bind vitamin K and cause bleeding tendency

A

Cholecystramine (lipid-lowering agents)

34
Q
  • Statin drugs
  • Can cause liver dysfunction
  • Rhabdomyolysis
A

HMG-CoA Reductase Inhibitors

35
Q
  • Inhibits cholesterol synthesis
  • Can cause flushing
  • Tx: ASA
A

Niacin

36
Q
  • Inhibits dopamine receptors
  • SE: tardive dyskinesia
  • Tx: diphenhydramine (Benadryl)
A

Promethazine (Phenergan, antiemetic)

37
Q
  • Inhibits dopamine receptors

- Can be used to increase gastric and gut motility

A

Metoclopramide (Reglan, prokinetic)

38
Q

Central-acting serotonin receptor inhibitor

A

Ondansetron (Zofran, antiemetic)

39
Q
  • Proton pump inhibitor

- Blocks H/K ATPase in stomach parietal cells

A

Omeprazole

40
Q

Histamine H2 receptor blockers

- Decrease acid in stomach

A

Cimetidine / ranitidine

41
Q

Long-acting somatostatin analogue

- Decreases gut secretions

A

Octreotide

42
Q
  • Inhibits Na/K ATPase and increases myocardial calcium
  • Slows atrial-ventricular conduction
  • Inotrope
  • Not cleared with dialysis
  • SE: Visual changes (yellow hue), fatigue, arrhythmias
A

Digoxin

43
Q

Why has digoxin been implicated in causing mesenteric ischemia?

A

Decreases blood flow to intestines

44
Q
  • Good for acute atrial and ventricular arrhythmias

- SE: pulmonary fibrosis w/ prolonged use; can also cause hypo- and hyperthyroidism

A

Amiodarone

45
Q

Used to treat tornadoes de pointes (ventricular tachycardia)

A

Magnesium

46
Q

Causes transient interruption of the AV node

A

Adenosine

47
Q
  • Best single agent shown to improve survival in patients with CHF
  • Can prevent CHF after MI
  • Can prevent progression of renal dysfxn in pts with HTN and DM.
  • Can precipitate renal failure in patients with renal artery stenosis
A

ACE inhibitors

angiotensin-converting enzyme inhibitors

48
Q

What increases the sensitivity of the heart to digitalis?

A

Hypokalemia

- Can precipitate arrhythmias or AV block

49
Q
  • May prolong life in patients with severe LV failure

- Reduce risk of MI and atrial fibrillation post

A

Beta blockers

50
Q

Best single agent shown to improve survival after myocardial infarction

A

Beta-blockers

51
Q
  • Acetylcholine antagonist

- Increases heart rate

A

Atropine

52
Q
  • Inhibit adrenal steroid synthesis

- Used in patients with adrenocortical CA

A

Metyrapone and aminoglutethimide

53
Q
  • analogue of GnRH and LHRH
  • Inhibitors release of LH and FSH form pituitary when given continuously (paradoxic effect)
  • Used in patients with metastatic prostate CA
A

Leuprolide

54
Q

Inhibits prostaglandin synthesis and leads to decreased mucus and HCO3- secretion and increased acid production (mechanism of ulcer formation)

A

NSAIDs

55
Q

a PGE1 derivative; a protective prostaglandin used to prevent peptic ulcer disease; consider use in patients on chronic NSAIDs

A

Misoprostol

56
Q
  • Antipsychotic
  • Inhibits dopamine receptors
  • Can cause extrapyramidal manifestations (Tx: benadryl)
A

Haldol

57
Q

Tinnitus, headaches, nausea, and vomiting.

A

ASA poisoning

58
Q

Two manifestations of aspirin poisoning

A

1st: respiratory alkalosis
2nd: metabolic acidosis

59
Q

MC side effect of gadolinium

A

Nausea

60
Q

Iodine:

  • MC side effect?
  • MC side effect requiring medical treatment?
A

Iodine:

  • MC side effect: nausea
  • MC side effect requiring medical treatment: dyspnea
61
Q

Tx: tylenol overdose

A

N-acetylcysteine

62
Q

pharmacokinetics principles

A
dissolution
absorption
distribution
metabolism 
secretion
63
Q

mechanism of cholestyramine

A

bind of bile acids and prevent reabsorption?

64
Q

mechanism of weight loss medication?

A

sibutramine –> inhibition of neurotransmitter reuptake

orlistat –> bind and inhibits gastric and pancreatic lipases –> prevent absorption of free fatty acid and decrease triglycerides production