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Pharmacology > Intro to Clinical Pharmacology > Flashcards

Intro to Clinical Pharmacology Flashcards

0
Q

Pharmacology

A

The study of drugs and their interaction in living systems

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1
Q

Drug

A

Any chemical that can affect living processes

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2
Q

Clinical pharmacology

A

Study of drugs in humans

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3
Q

Therapeutics

A

Use of drugs to diagnose, prevent, and treat disease or to prevent pregnancy

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4
Q

Properties of an Ideal Drug

A
  • Effectiveness: elicit the responses for which it is given
  • Safety: drug cannot produce harmful effects
  • Selectivity: elicits only the response for which it is given
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5
Q

Factors that determine the intensity of drug responses

A

Administration, pharmacokinetics, pharmacodynamics, sources of individual variation

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6
Q

Pharmacokinetics

A

Impact of body on the drugs; absorption, distribution, metabolism, excretion, time course of drug responses

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7
Q

Application of pharmacokinetics in therapeutics

A

By applying knowledge of pharmacokinetics to drug therapy, we can help maximize beneficial effects and minimize harm

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8
Q

Absorption

A

Movement of a drug from its site of administration into the blood

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9
Q

Rate of absorption

A

Determines how soon effects will begin

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10
Q

Amount of absorption

A

Helps determine how intense the effects will be

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11
Q

Factors affecting drug absorption

A

Rate of dissolution, surface area, blood flow, lipid solubility, pH partitioning

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12
Q

Distribution

A

Movement of drugs throughout the body

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13
Q

How is drug distribution determined? (3 factors)

A
  • Blood flow to tissues
  • Exiting the vascular system
  • Entering cells
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14
Q

Blood Flow to Tissues

A
  • Drugs are carried by the blood to tissues and organs of the body
  • Blood flow determines rate of delivery
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15
Q

Abscesses and tumors (reg. blood flow to tissues)

A
  • Low regional blood flow impacts therapy
  • Pus-filled pockets, not internal blood vessels
  • Solid tumors have limited blood supply
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16
Q

Blood-Brain Barrier (BBB)

A

Tight junction between the cells that compose the walls of most capillaries in the CNS
-Drugs must be able to pass through cells of the capillary wall; only drugs that are lipid soluble or have a transport system can cross the BBB to a significant degree

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17
Q

Placental Drug Transfer

A

Membranes of the placenta do NOT constitute an absolute barrier to the passage of drugs; movement determined in the same way as other membranes

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18
Q

Risk with placental drug transfer

A

Birth defects: mental retardation, gross malformations, low birth weight; mother’s use of habitual opioids: birth of drug-dependent baby

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19
Q

Protein Binding

A

Drugs can form reversible bonds with various proteins; Plasma albumin is the most abundant and important > large molecule that always remains in the bloodstream; impacts drug distribution

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20
Q

Entering cells

A
  • Some drugs must enter cells to reach the side of action
  • Most drugs must enter cells to undergo metabolism and excretion
  • Many drugs produce their effects by binding with receptors on the external surface of the cell membrane > do not need to cross the cell membrane to act
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21
Q

Drug Metabolism

A

Biotransformation; the enzymatic alteration of drug structure > most often takes place in the liver

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22
Q

P450 System

A

Most drug metabolism that takes place in the liver is performed by the hepatic microsomal enzyme system; metabolism doesn’t always result in a smaller molecule

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23
Q

Special Considerations in Drug Metabolism

A

Age, induction of drug-metabolizing enzymes, first-pass effect, nutritional status, competition between drugs

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24
Q

Excretion

A

Removal of drugs from the body; drugs and their metabolites can exit the body through urine, sweat, saliva, breast milk, or expired air

25
Q

Renal routes of drug excretion

A

Glomerular filtration, passive tubular reabsorption, active tubular secretion (kidneys)

26
Q

Factors that modify renal drug exretion

A

pH-dependent ionization, competition for active tubular transport, age

27
Q

Nonrenal routes of drug excretion

A

Breast milk, bile, lungs (especially anesthesia), sweat/saliva

28
Q

Pharmacodynamics

A

Study of biochemical and physiologic effects of drugs and the molecular mechanisms by which those effects are produced; study of what drugs do to the body and how they do it

29
Q

Sources of individual variation

A 
Physiologic variables (age, gender, weight)
Pathologic variables (diminished renal and liver function)
Genetic variables (can alter drug metabolism)
Drug interactions (no two patients alike)
30
Q

Half life

A

Time required for the amount of drug in the body to decrease by 50%; determines the dosing interval

31
Q

Controlled Substance Act (Landmark Drug Legislation)

A

Established categories into which controlled substances are placed; Schedule I-V

32
Q

Schedule I drugs

A

No accepted use in US and have high potential for addiction (ie. heroin, LSD, cigarette marijuana)

33
Q

Schedule II drugs

A

Accepted medical use, high abuse potential; written prescription needed/no refills allowed (ie. dilaudid, cocaine, dura morph, codeine)

34
Q

Schedule III drugs

A

Medical use, less abuse potential (ie. marinol, vicodin)

35
Q

Schedule IV drugs

A

Phenobaritol, ambien, lorazepam

36
Q

Schedule V drugs

A

Lomotil, robitussin AC (codeine)

37
Q

New Drug Development

A

Pre-clinical testing (animal testing): toxicity, pharmacokinetics, useful effects
Clinical testing (2-10 years)
-Phase I: healthy volunteers (check toxicity)
-Phase II/III: patients (on sick patients, adverse effects)
-Phase IV: Aftermarket surveillance (once drug has been approved)

38
Q

Drug Names

A

Chemical, generic (nonproprietary), trade (brand)

39
Q

Consequences of drug-drug interactions

A

Intensified effects, increased therapeutic effects, increased adverse effects

40
Q

Basic mechanisms of drug-drug interactions

A

Direct chemical or physical interaction; pharmacokinetic interactions: altered absorption, altered distribution, altered metabolism, altered renal excretion, interactions that involve P-glycoprotein

41
Q

Ways to reduce medication errors

A

Replace handwritten medication orders with a computerized order entry system; have a senior clinical pharmacist accompany physicians on rounds; use a bar-code system

42
Q

Individual variation in drug responses

A

Gender, race, failure to take medicine as prescribed, drug interaction, diet

43
Q

Efficacy

A

Maximum effect that a drug can produce, regardless of dose

44
Q

Potency

A

Amount of a drug tat is needed to produce a given effect

45
Q

Drugs

A

Chemicals that produce effects by interacting with other chemicals

46
Q

Receptors

A

Special chemicals in the body that most drugs interact with to produce effects

47
Q

Important properties of receptors

A
  • Receptors are normal points of control of physiologic processes
  • Under physiologic conditions, receptor function is regulated by molecules supplied by the body
  • Drugs can only mimic or block the body’s own regulatory molecules
  • Drugs cannot give cells new functions
48
Q

Agonists

A

Molecules that activate receptors

49
Q

Antagonists

A

Preventing receptor activation; noncompetitive and competitive

50
Q

Partial agonists

A

Agonists that only have a moderate intrinsic activity; maximal effect that a partial agonist can produce is less than that of a full agonist. Can act as antagonists as well as agonists

51
Q

Noncompetitive antagonists

A

Bind irreversibly to receptors, reduce the maximal response that an agonist can elicit, impact not permanent

52
Q

Competitive antagonists

A

Compete with agonists for receptor binding, bind reversibly to receptors; equal affinity: receptor occupied by whichever agent is present in the highest concentration

53
Q

Interpatient variability in drug responses

A

Initial dose of a drug is necessarily an approximation, subsequent doses must be “fine tuned” based on the patient’s response

54
Q

ED50

A

Effective dose in 50% of the population tested

55
Q

LD50

A

Average lethal dose to 50% of the animals treated

56
Q

Therapeutic Index

A

Measure of drug’s safety; ratio of drug’s LD50 to its ED50. Higher the therapeutic index, the safer the drug; lower the therapeutic index, less safe the drug

57
Q

Drug-drug interations

A

Interactions occur whenever a patient takes more than one drug; some are intended and others are undesired

58
Q

Consequences of drug-drug interactions

A

Intensification of effects (increased therapeutic/adverse effects), reduction of effects, creation of a unique response

59
Q

Clinical significance of drug-drug interactions

A
  • Potential to significantly impact the outcome of therapy
  • Responses may be increased or reduced
  • Risk for serious drug interaction is directly proportionate to the number of drugs a patient is taking
  • Interactions are especially important in drugs w/ low therapeutic index
  • Many interactions are yet to be identified
60
Q

Grapefruit juice effect

A

Inhibits metabolism of certain drugs; raises the drugs’ blood levels

61
Q

Timing of drug administration

A

Some drugs are better tolerated on an empty stomach, others should be taken with food esp. for nausea

Pharmacology (14 decks)

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