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Preventive And Social Medicine II > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What the body does to the drug

A

Pharmacokinetics

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2
Q

What is the movement of drug into, through and out the body?

A

Pharmacokinetics

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3
Q

What is the flow of the drug?

A

ABDME

  • Absorption
  • Bioavailability
  • Distribution
  • Metabolism
  • Excretion
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4
Q

Pharmacokinetics is determined by the drug’s

A

1) physiochemical properties
2) formulation
3) route of administration

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5
Q

How do drugs cross the membranes?

A 
By:
      Passive diffusion
      Facilitated passive diffusion
      Active transport
      Pinocytosis
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6
Q

What are the 3 primary processes of pharmacokinetics?

A

IDE

Input
Distribution
Elimination

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7
Q

It is the amount of drug in the body in relation to the concentration of drug in the plasma.

A

Volume of Distribution

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8
Q

Where is the drugs with very high VD concentrated?

A

Extravascular tissue

than vascular compartment not homogeneously distributed

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9
Q

Why is VD generally uneven?

A

D/t the differences in blood perfusion, tissue binding, regional pH, and permeability of cell membranes.

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10
Q

What is the factor that predicts the rate of elimination in relation to the drug concentration?

A

Clearance

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11
Q

Clearance: first-order

A

Elimination - not saturable

Rate of elimination directly proportional to concentration

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12
Q

It is also known as:

Mixed-order
Saturable
Dose or conc dependent
Nonlinear
Michaelis Menten Elimination
A

Capacity-limited elimination

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13
Q

What is saturable and also called Vmax?

A

Maximum elimination capacity

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14
Q

It is the Km-drug conc at wc rate of elimination is 50% of Vmax.

A

Capacity limited elimination

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15
Q

Conc that are high relative to the elimination rate is almost independent of

A

Conc state of “pseudo-zero order” elimination

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16
Q

What if dosing rate exceeds elimination capacity?

A

Steady state cannot be achieved

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17
Q

Relationship of conc and dosing

A

Conc will keep rising as long as dosing continues

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18
Q

Where does the elimination of drugs depend?

A

Primarily on the rate of drug delivery to the organ of elimination

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19
Q

What is the main determinant of drug delivery?

A

Bld flow to the organ

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20
Q

Any conc of drug, most of the drug in bld perfusing the organ is eliminated on the

A

First pass of the drug through it

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21
Q

What is the time required to change the amount of drug in the body by one-half during elimination?

A

Half-life

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22
Q

Also time req to attain 50% of steady state or to decay 50% from steady state conditions after a change in the rate of drug administration

A

Half-life

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23
Q

Fraction remaining can be predicted from the dosing interval and t1/2

A

Drug accumulation

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24
Q

Fraction of unchanged drug reaching the systemic circulation following administration by any route

A

Bioavailability

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25
Q

What has the most rapid onset?

A

IV (100% Bioavailability)

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26
Q

Large volume, often feasible, may be painful, 75-100%, 90°

A

IM

  • most common: deltoid (5mL)
  • glutes (10mL)
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27
Q

Smaller vol than IM, may be painful, 75-100%, 45°

E.g vaxx, insulin

A

SC

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28
Q

Most convenient, 5-100%, first pass effect may be impt

A

Oral

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29
Q

Less first pass effect than oral, 30-<100%

A

Rectal

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30
Q

<100%, often very rapid onset

A

Inhalation

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31
Q

Usually very slow absorption, used for lack 1st pass effect, prolonged duration of action, 80-100%

A

Transdermal

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32
Q

What refers to extent and rate at wc active moiety (drug/metabolite) enters systemic circulation thus accessing site of action?

A

Bioavailability

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33
Q

What are drug products that contain the same active cmpd in the same amt and meet current official std?

Same cmpd, diff brand names

A

Chemical equivalence

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34
Q

What are drug products when given to same px in same dose result in equivalent concs of drug in plasma and tissues

A

Bioequivalence

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35
Q

What are drug products that when given to same px in same dose have same therapeutic and adverse effects?

A

Therapeutic equivalence

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36
Q

What is the principal site of drug met?

A

Liver

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37
Q

Inactive/weakly active subs that has an active metabolite

A

Prodrug

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38
Q

What is the goal of drug met/drug brkdwn?

A

Make drug easier to excrete

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39
Q

Formation of a new/modified fxnal grp or cleavage (oxidation, redxn, hydrolysis)

A

Phase I

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40
Q

Conjugation with an endogenous substance

A

Phase II

41
Q

What is determined by site of administration and drug formation?

A

Rate of absorption

42
Q

Rate is independent of amt of drug remaining in the gut

A

Zero-order

- eg det by rate of gastric emptying tume or by ctrlled-release formulation

43
Q

Dose us dissolved in GI fluids

A

First order

- e.g rate of absorption proportional to GI fluid conc

44
Q

Produced the desired therapeutic effect

A

Target conc

45
Q

Steady state of drug
Most impt to consider-clearance

Dosing rate = rate of elimination (clearance x target conc)

A

Maintenance dose

46
Q

Dose that promptly raises the conc of drug in plasma to the target conc

A

Loading dose (antibiotics)

47
Q

What is the single most impt factor determining drug conc?

A

Clearance

48
Q

What are the factors affecting protein binding?

A
  • albumin conc (low in many dse states)
  • a1-acid glycoprotein conc (inc in acute inflam dis)
    Quinidine, Lidocaine, Propanolol
  • capacity-limited protein binding
  • binding to rbc
49
Q

What are the factors affecting protein binding?

A
  • albumin conc (low in many dse states)
  • a1-acid glycoprotein conc (inc in acute inflam dis)
    Quinidine, Lidocaine, Propanolol
  • capacity-limited protein binding
  • binding to rbc
50
Q

What is the principal organ for drug excretion?

A

Kidneys

51
Q

Small amount of drug is excreted into:

A

Int, saliva, sweat, breast milk, lungs

52
Q

Influence of drug conc on the magnitude of the response

A

Pharmacodynamics

53
Q

Component of the biologic sys to wc a drug binds to bring about a change in fxn of the system

A

Receptor

54
Q

A drug that activates its receptor upon binding

A

Agonist

55
Q

Component of the biologic sys that accomplishes the biologic effect afte being activated by the receptor; often a channel or enz

A

Effector

56
Q

A drug that binds to its receptor w/o activating it

A

Pharmacologic antagonist

57
Q

A pharma antagonist that can be overcome by increasing the dose of agonist e.g beta blockers

A

Competitive antagonist

58
Q

A pharma antagonist that cannot be overcome by inc the dose of agonist

A

Irreversible antagonist

59
Q

A drug that counters the effects of another by binding to a different receptor and causing opposing effects

A

Physiologic antagonist

60
Q

A drug that counters the effects of another by binding the drug and preventing its action, drugs for OD or poisoning (eg antedote)

A

Chemical antagonist

61
Q

Effects of AchE

A

Mimicked by muscarine and nicotine

Blocked by atropine

62
Q

No requirement for highly specific chemical structure

A

Mannitol

63
Q

Conc of drug increase, magnitude of pharmacologic effect also increase

A

Graded dose response relations

64
Q

Response is continuous and gradual

A

Response-graded effect

65
Q

Drug-receptor interaction characterized by

A
  • Binding of drug to receptor
  • Gov by affinity
  • Potent drugs-elicit a response by binding to a number of particular receptor type at low conc (high affinity)
66
Q

Characterize one drug vs another

A

Relative efficacy

67
Q

Magnitude of response is equal to

A

Amt of receptors bound or occupied

68
Q

Occurs when all receptors are bound

A

Emax

69
Q

Controlled by receptor density, efficacy, affinity, and efficiency of the stimulus-response mechanism of the tissue

A

Potency

70
Q

What is the conc (EC50) or dose (ED50) of a drug required to produce 50% of that drug’s maximal effect?

A

Potency

71
Q

The extent or degree of an effect that can be achieved in the px
Impt for making clin decisions when large doses are needed

A

Maximal efficacy

72
Q

What is the dose required to produce a particularly toxic effect in 50% of animals?

A

Median toxic dose (TD50)

73
Q

Dose required to produce a desired effect to that wc produces an undesired effect

A

Therapeutic index

- tells u the safety of the drug

74
Q

In animals the ratio is

A

TD50:ED50

75
Q

Its normal fxn is to act as receptors for endogenous regulatory ligands

A

Proteins

76
Q

What are drugs that bind to physiologic receptors and mimic the regulatory effects of the endogenous signaling compounds?

A

Agonist

77
Q

What stabilize the receptor in its inactive conformation?

A

Inverse agonists

78
Q

What bind to receptors w/o regulatory effect, but their binding blocks the binding of the endogenous agonist?

A

Antagonists

79
Q

High affinity for receptor

Form covalent bonds w receptor

A

Irreversible antagonist

80
Q

Need not be present in unbound form to inhibit agonist responses once the receptor has been occupied

A

Irreversible antagonist

81
Q

Duration of action
Independent: rate of elimination
More dependent: turnover of receptor mol.

A

Irreversible antagonist

82
Q

What is an example of irreversible antagonist?

A

Phenoxybenzamine

  • irreversible alpha-adrenoceptor antagonist
  • usee to ctrl HPN c/b pheochromocytoma
83
Q

Decrease in actual num of receptors in the cell/tissue

Generally occurs only after prolonged or repeated exposure to agonist (over hrs or dayz)

A

Down-regulation

84
Q

Parts of a prescription

A 
1 superscription
2 inscription
3 subscription
4 avoid confusion
5 proper px info
6 all prescription written in ink
7 date of prescription
8 choice of drug product
9 prescriber's ID
10 errors in drug orders should be minimized
85
Q

Parts of Superscription

A 
Date
Name
Address
Wt
Age
Rx
86
Q

Parts of Inscription

A

Name of drug
Amt
Strength to be dispensed

(write generic name)

Official gen and approved brand name

87
Q

Parts of Subscription

A 
Instructions to pharmacist
Signa/sig
- how to take prescription
- English
- avoid abbrev or symbols
88
Q

Prescriber’s ID

A 
Physician's name and professional degree
Add
Phone number
License number
PTR number
S2 license number (aka dangerous drugs license)
89
Q

SCHEDULE I

A
  • High potential for abuse
  • No accepted med use in US
  • Heroin, methylene dioxymethamphetamine, lysergic acid diethylamide, mescaline
90
Q

SCHEDULE II

A
  • High pot for abuse
  • Has currently accepted medical use in US
  • Abuse may lead to severe psychological/physical dependence
  • Morphine, oxycodone, fentanyl, meperidine, dextroamphetamine, cocaine, amobarbital
91
Q

SCHEDULE III

A
  • Abuse potential less than I and II
  • Has currently acceptable med use
  • Abuse may lead to mod or low physical dependence or high psychological dependence
  • Anabolic steroids, nalorphine, ketamine, certain sched II in suppositories, mixtures limited amnts per dosage unit
92
Q

SCHEDULE IV

A
  • Abuse potential
93
Q

SCHEDULE V

A
  • Low potential for abuse
  • Some may be sold in limited amnts w/o a prescription
  • Buprenorphine, products cont a low dose of an opiod plus a non narcotic s/a codeine and guaifenesin
94
Q

Oral orders

A

3, 4 & 5

2 if emergency

95
Q

Refills

A

3 & 4 - orally or in writing, not >5 refills or 6 months after issue date

2 - NOT to be refilled under any circumstance

96
Q

What is the best documented barrier to compliance?

A

Px w multiple drugs, multiple illness, chronic dse

96
Q

What is the best documented barrier to compliance?

A

Px w multiple drugs, multiple illness, chronic dse

97
Q

Most common barrier to compliance

A

High cost

Preventive And Social Medicine II (32 decks)

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