Pharmacology Flashcards

1
Q

Pharmacology and PT

A
  1. Optimal response to therapy
  2. Interaxns with rehab procedures
  3. Adverse effects
  4. Compliance
  5. Drug alternatives
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2
Q

Pharmacotherapeutics

A

Use of specific drugs to prevent, treat or diagnose disease

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3
Q

Pharmacokinetics

A
What BODY does to the drug:
   Absorbtion
   Distribution
   Metabolism
   Elimination
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4
Q

Pharmacodynamics

A

What DRUG does to body:
=Mechanism of action

Drug/Ligand + Receptor –> Drug-Receptor Complex

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5
Q

Toxicology

A

Side effects

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6
Q

Pharmacy

A

Preparation and dispensing of drugs

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7
Q

Chemical Name

A

Name of chemical composing drug

Ex: N-Acetyl-p-aminophenol

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8
Q

Generic Name

A

Common name of drug, describes chemical compound.
*Never capitalized

Ex: acetaminophen

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9
Q

Brand/Trade Name

A

Name of drug, chosen by marketers or pharmaceutical company
*Always capitalized

Ex: Tylenol

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10
Q

Patent

A

Company that creates drug has rights to it for 7-10yrs

  • ->generic versions
    • same therapeutic use
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11
Q

Drug Development

A
  1. What constitutes drug
  2. FDA (Efficacy + Safety)
  3. Animal studies (Preclinical tests)
  4. Human studies (Clinical trials - Phases I-III)
  5. New drug approval
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12
Q

Clinical Trials

A

Drug testing conducted on humans post animal studies of efficacy + safety:

Phase I: Small # healthy indiv (<1 yr)
*Effect, dosage, pharmacokinetics

Phase II: Limited # with target disease (2 yrs)
*Efficacy of treating specific disease

Phase III: 1000-3000 pts with target disease (3yrs)
*Efficacy + Safety in larger population

Phase IV: General population (Indefinite)
*Monitor problems post approval

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13
Q

OTC Medication

A
  • Availability/convenience
  • High safety profile (lower dose = harder to harm)
  • Note in patients
  • PT implications
  • Interaxns with other drugs (doubling up)
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14
Q

Controlled Substances

A

Drugs with abuse potential, decreases with higher schedule:

Sched I - High Abpot / No med use
Sched II - High Abpot / Some med use
Sched III - Lower Abpot / Med use
Sched IV - Lower Abpot / Med use + barbituates
Sched V - Derivatives of high Abpots
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15
Q

Schedule I

A

Controlled substances with highest abuse potential
*No medical use

Ex: Heroin, LSD, Marijuana (THC), MDMA

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16
Q

Schedule II

A

Controlled substances with high abuse potential
*Some medical use

Ex: Morphine, Methadone, Methamphetamine,
Oxycontin

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17
Q

Schedule III

A

Controlled substances with lower abuse potential
*Medical use

Ex: Codeine, Anabolic Steroids, hydrocodone

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18
Q

Schedule IV

A

Controlled substances with low abuse potential
*Medical use + barbituates

Ex: Meprobromate, phenobarbitol, alprazolam,
diazepam

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19
Q

Barbituates

A

CNS depressant

  • Sedation
  • Anesthetic
  • Mild analgesic effects
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20
Q

Analgesic

A

Painkiller

Ex: acetaminophen, NSAIDs, opioids

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21
Q

Schedule V

A

Controlled substances with lowest abuse potential
*Contain derivatives of high abuse medicines

Ex: Codeine cough syrup, antidiarrheal preps,
phenergan

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22
Q

Dose

A

Quantity of drug administered at one time

*Concentration of drug at receptor site

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23
Q

Dosage

A

Administration of drug per unit of time

*How much to give (BID/SID/etc.)

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24
Q

Dose-Response Curve

A

Relation between dose administration (magnitude of drug) and observed response
–>Shows effect of drug at any given dose

Plotted as Dose (x) vs Effect/Response (y)

  • Threshold
  • Potency
  • Max effect
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25
Q

Drug Response

A

Extent to which drug reaches intended effect

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26
Q

Potency

A

Measure of drug dose needed to produce a therapeutic effect
*Potency does not equal efficacy

Higher = less drug needed for target effect
Lower = more drug needed for target effect

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27
Q

Subtherapeutic

A

Threshold, dose less than amount needed to produce target effect

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28
Q

Max Effect

A

Point at which increase in dose will not increase effect

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29
Q

Dose-Response Function

A

-Must specify dose and species
-One drug can have multiple
-Larger dose doesn’t equal greater magnitude of
response (due to max effect)
Max effect = no increase in response with
increase in dose

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30
Q

Quantal Dose-Response Curve

A

Relation between drug concentration in blood (x) and response percentage of a population (y) to a specified effect chosen for the drug.
-Determines relative safety and efficacy of a particular drug

ED50
Therapeutic Effect

TD50
Toxic Effect

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31
Q

ED50

A

(Median Effective Dose); Quantal D-R Curve
= Min dose required to produce desired effect in 50% of the
population

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32
Q

Therapeutic Effect

A

Point at which dose of drug has effect on the body

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33
Q

TD50

A

(Median Toxic Dose)
= Min dose required to produce toxic effect in 50% of the
population

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34
Q

Toxic Effect

A

Point at which dose of drug becomes harmful to the body

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35
Q

Therapeutic Index

A

Ratio of dose that causes toxicity to dose that causes desired effect in a population

TI = (TD50 / ED50)

36
Q

Absorption

A

1st step of pharmacokinetics

  • Depends on:
    - Route of admin
    - Drug factors (lipid/water sol, size, ionization)
    - Body factors (SA, pH, vascularity)
37
Q

Bioavailability

A

Percentage of drug that reaches bloodstream

  • Oral ~ 50%
  • IV (Direct) ~ 100%
38
Q

Routes of Administration

A
  1. Enteral = GI Tract
    • Oral
    • Sublingual
    • Rectal
  2. Parenteral = Everything else, *more direct
    • Inhalation
    • Injection (IV, IM, IT, SC)
    • Topical
  3. Transdermal (Placed on skin –> bloodstream)
  4. Implanted drug delivery
  5. Controlled release preparations
  6. Targeted drug delivery
39
Q

Enteral Administration

A

(Route of administration, GI Tract)

1. Oral: 
     - Safe, easy
     - Ltd absorption, 1st pass metab to liver, compliance

 2. Sublingual: 
     - Rapid onset, no 1st pass metab
     - Must absorb into mucosa easily

 3. Rectal:
     - Local effect
     - Incomplete absorption, irritation
40
Q

Parenteral Administration

A

(Route of administration, Direct)

1. Inhalation
      - Rapid onset, respiratory, increased SA
      - Irritation, administration, compliance

2. Injection (IV, IM, IT, SC)
      - Direct, rapid onset
      - Infexn, self-administration

3. Topical 
      - Local effects
      - Can be absorbed into bloodstream
41
Q

Transdermal Administration

A

(Route of administration, Placed on skin –> Bloodstream)

 - Steady, prolonged delivery
 - Ltd, drug must penetrate skin unchanged
42
Q

IA

A

(Intra-arterial)

= Specific

43
Q

SC

A

(Subcutaneous)
= Local response needed

Ex: Novacaine, insulin

44
Q

IM

A

(Intramuscular)

Ex: Botox for spasticity

45
Q

IT

A

(Intrathecal)
= subarachnoid space of spinal cord

Ex: Analgesics, spasticity

46
Q

Implanted Drug Delivery

A

Route of administration

-PCA Pump

47
Q

Controlled Release Preparations

A

Route of administration

= Encapsulation to release in intervals, fewer manual
doses

48
Q

Targeted Drug Delivery

A

Route of administration

-Monoclonal Ab's (Drug + Ab --> specific problem)
-Viral Transport
-Gene Therapy (Viral cells enter DNA, give new 
       instructions
-Enzyme Activation (Drugs only activated by specific 
       enzymes
49
Q

Absorption Factors

A

Related to drugs:
Lipid/water sol Molecular/particle size
Ionization Physical form
Dosage form Formulation
Concentration

Related to body:
SA Vascularity
pH Other substances present
GI motility Functional integrity
Disease

50
Q

Exogenous

A

Introduced to body from outside

51
Q

Endogenous

A

Native to body

52
Q

Membranes that Affect Absorption and Distribution

A

Based on lipid solubility:

  1. GI –> Bloodstream
  2. ECF –> ICF
  3. ICF –> ECF
  4. Kidneys –> Bloodstream
53
Q

Passive Diffusion

A

Water soluble: Drug crosses membrane via aqueous
channel

Lipid soluble: Drug dissolved through membrane

54
Q

Distribution

A

2nd step of pharmacokinetics

  • Affected by:
    - Blood flow
    - Capillary permeability
    - Binding
55
Q

Depot Binding

A

Binding of drug to substance besides site of action

  • ->Need to increase dose to get desired effect
    - ->Adverse/toxic effects
56
Q

Vd

A

(Volume of Distribution of drug)
-If evenly dist, = to total body fluid volume

= how much of drug is in bloodstream

57
Q

Membranes that Affect Distribution

A
  • Cell membranes
  • Capillary walls
  • Blood brain barrier (Glial cells)
  • Placental barrier (not real barrier)
58
Q

Blood Brain Barrier

A

Series of unique properties of blood vessels in the nervous system that regulate movement of molecules between blood and neural tissue.

  1. Glial (Support) Cells
    - Astrocyte –> End feet form sheath around BV
  2. Tight junctions of endothelial cells
  3. Breaks –> detect chemicals
    - Area Postrema (Medulla)
    - Median Eminence (HT)
  4. Purpose:
    - Block toxins
    - Maintain homeostasis of brain
59
Q

Metabolism

A

3rd step of Pharmacokinetics
= Biotransformation of drug from parent compound into
metabolite
-1st Pass Metabolism
-Lipid-sol –> Water-sol for kidney excretion

*High = drug has less effect
Low = drug has more effect

59
Q

Biotransformation

A

Chemical change of drug

*Not really “broken” down

60
Q

Metabolite

A

Daughter compound of drug

60
Q

1st Pass Metabolism

A

GI Tract –> Portal Circulation –> Liver –> Target Site

*Bypassed by IV drug admin

61
Q

First-Order Kinetics

A

Rate of metab & elim proportional to concentration of drug

*Higher dose –> Higher metab of drug

61
Q

Zero-Order Kinetics

A

Constant rate of metab regardless of concentration of drug

*Higher does –> Metab stays the same

62
Q

Enzyme Induction

A

Tolerance = Increase in concentration of enzymes to be able to biotransform drug

 - Drug has less effect due to upreg of enzymes
     - ->More drug required for same effect
62
Q

Cytochrome P450 System

A

Component of drug metabolism, in liver / GI tract
-Diversified, nonspecific

 -Phase I
     Oxidation (+O2, -H+)
     Reduxn (-O2, +H+)
     Hydrolysis

 -Phase II (Some drugs enter directly)
     Conjugation = coupling to endogenous compound
                          -->Inactivation --> Water soluble
63
Q

Elimination

A

4th step of Pharmacokinetics

Filtration system via kidneys:

  • Nephron / Glomerulus / Bowman’s Capsule
    - 1L blood/min, 1cm3 urine produced
    - Lipid-sol drug –> water-sol drug –> Excretion

*Lipid-sol drugs reabsorbed and return to liver until water-sol

64
Q

CL Total

A

(Total Body Clearance)
Rate at which drug is eliminated from the body, sum of hepatic, renal, pulmonary, integumentary clearances

CL = 0.69 x (Vd / (t1/2))

65
Q

Half-life (t1/2)

A

Time it takes for 50% of drug to be eliminated from bloodstream

t1/2 = 0.69 x (Vd / CL)

Percentages of original dose:
2 t1/2 = 75%
4 t1/2 = 94%
6 t1/2 = 98%

Ex: 100mg drug
    1 t1/2 = 50mg (50% of orig dose)
    2 t1/2 = 25mg (75% of orig dose)
    3 t1/2 = 12.5mg
    4 t1/2 = 6.25mg (94% of orig dose)
66
Q

Steady State Concentration

A

Amt administered = Amt Eliminated

  • Takes 5-6 t1/2
  • Determined by dose, dose interval, t1/2
    • ->predictable accumulation

*Repeated fixed dose = continuous oscillations in
plasma concentrations of drug

*Single fixed dose = single peak in plasma
concentration –> decline in drug level

67
Q

Tolerance

A

Decreased response to effects of given amt of drug from previous exposure

- Pharmacokinetic: Enzymes (Cross-tolerance)
- Pharmacodynamic: Receptors/Neurotransmitters

= More drug for desired effect

68
Q

Dependence

A

Drug use necessary for physiological/psychological well-being

69
Q

Cytochrome P450 System

A

Component of drug metabolism, in liver / GI tract
-Diversified, nonspecific

 -Phase I
     Oxidation (+O2, -H+)
     Reduxn (-O2, +H+)
     Hydrolysis

 -Phase II (Some drugs enter directly)
     Conjugation = coupling to endogenous compound
                          -->Inactivation --> Water soluble
70
Q

Elimination

A

4th step of Pharmacokinetics

Filtration system via kidneys:

  • Nephron / Glomerulus / Bowman’s Capsule
    - 1L blood/min, 1cm3 urine produced
    - Lipid-sol drug –> water-sol drug –> Excretion

*Lipid-sol drugs reabsorbed and return to liver until water-sol

71
Q

CL Total

A

(Total Body Clearance)
Rate at which drug is eliminated from the body, sum of hepatic, renal, pulmonary, integumentary clearances

= 0.69 x (VD/(t1/2))

72
Q

Half-life (t1/2)

A

Time it takes for 50% of drug to be eliminated

Percentages of original dose:
2 t1/2 = 75%
4 t1/2 = 94%
6 t1/2 = 98%

Ex: 100mg drug
    2 t1/2 = 50mg
    4 t1/2 = 25mg
    3 t1/2 = 12.5mg
    4 t1/2 = 6.25mg (94% of original dose
73
Q

Steady State Concentration

A

Amt administered = Amt Eliminated

  • Takes 5-6 t1/2
  • Determined by dose, dose interval, t1/2
    • ->predictable accumulation

*Repeated fixed dose = continuous oscillations in
plasma concentrations of drug

*Single fixed dose = single peak in plasma
concentration –> decline in drug level

74
Q

Tolerance

A

Decreased response to effects of given amt of drug from previous exposure

= More drug for desired effect

75
Q

Dependence

A

Drug use necessary for physiological/psychological well-being

76
Q

Drugs

A

Exogenous substances that mimic endogenous substances

77
Q

Receptor

A

Protein with binding site for endogenous substances

78
Q

Ligand

A

Substance capable of binding to a receptor

Ex: Drug, hormone

79
Q

Selectivity

A

Enzymes: Nonspecific
Receptors: Very specific

80
Q

Affinity

A

Drug ability to bind to receptor

-Could block or open

81
Q

Neurotransmitters

A

Acetylcholine
Norepinephrine
GABA

82
Q

Agonist

A

=Opener
Exogenous ligand that binds receptor & causes biological effect
-Has affinity + efficacy

83
Q

Antagonist

A

=Blocker
Exogenous ligand that binds receptor and blocks effect
-Has affinity + efficacy (if intended effect was to block)