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Anes. Pharm. Me > Basic Concepts > Flashcards

Basic Concepts Flashcards

1
Q

The specific protein molecule of lipid bilayer of cell membrane with which an administered drug interacts.

A

receptor

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2
Q

KNOW:

Concentration (number) of receptors at site of action may change. True or false?

A

true

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3
Q

Name the receptors in order pictured:

A

membrane receptor

ligand-gated channel

voltage-gated ion channel

enzyme

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4
Q

2 molecules having the same chemical composition but different orientations around a central atom – mirror images are:

A

entantiomers

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5
Q

equal amounts of left- and right-handed enantiomers of a chiral molecule

A

racemic mixture

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6
Q

a drug that produces its clinical effect by binding to a receptor and activating it (mimetic)

A

agonist

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7
Q

a drug that produces its clinical effect by binding to a receptor WITHOUT activating it and simultaneously prevents an agonist from stimulating it (blocking)

A

antagonist

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8
Q

drug that combines directly with its receptor to trigger its physiologic response

A

directly-acting receptor agonist

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9
Q

drug that produces its physiologic response by increasing the concentration of ENDOGENOUS substrate (neurotransmitter or hormone) at receptor site

A

Indirectly-acting receptor agonist

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10
Q

receptor inhibition which can be overcome by INCREASING the concentration of the agonist at the receptor site (reversible blockade)

A

competitive antagonism

Example: Roc

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11
Q

receptor inhibition which CANNOT be overcome by increasing the concentration of the agonist (irreversible blockade)

A

Noncompetitive

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12
Q

Terminology of Drug Responses (8)

A

Hyperactive
Hypersensitive (allergic)
Hypo reactive (tolerant)
Tachyphylaxis
Additive effect
Synergistic effect
Antagonistic effect
Prodrug

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13
Q

Routes of Administration (2)

A

enteral

parenteral

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14
Q

Enteral routes: (3)

A
  • oral
  • sublingual–bypass liver and goes directly to heart and systemic circulation
  • rectal
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15
Q

Parenteral – “aside from” the alimentary tract routes (8)

A
  • Intravenous (IV)
  • Intraarterial–very few (calcium blocker for neuro pts to localize vasodilation, for example)
  • Intramuscular (IM)–more muscle, faster effect
  • Intrathecal–CSF, spinal
  • Subcutaneous (SC)
  • Nasal
  • Pulmonary
  • Transdermal, Topical
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16
Q

Subcutaneous injection is placed under the _____ layer.

A

dermal

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17
Q

Site-specific factors affecting absorption (3)

A

Blood flow from site
Surface area for absorption
Solubility of drug at site

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18
Q

Ok, so now that it’s in, where does the drug go? (3)

A

Compartment Model
Volume of distribution
Ionization

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19
Q

THEORY: the body is composed of multiple compartments having calculated volumes is known as:

A

Compartmental Models

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20
Q

Compartmental Models

We can examine the pharmacokinetics of drugs we administer in terms of what compartments they travel to (4 + ect.) and what happens when they reach those compartments (clinical effect, metabolism, storage, etc.)

A

(circulating blood, central nervous system, liver, fat, etc.)

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21
Q

Which compartment involves rapid uptake of drug?

A

Central compartment

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22
Q

Central compartment – rapid uptake of drug includes: (6)

A

intravascular fluid and highly perfused tissues like the lungs, heart, brain, kidneys, and liver

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23
Q

This compartment involves slower uptake and includes less vascular tissues like fat, bone, and inactive skeletal muscle.

A

Peripheral compartment

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24
Q

2-Compartment Model

Drugs equilibrate between compartments and are eventually eliminated from the _____ compartment.

A

central

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25
Q

What model?

A

compartment model

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26
Q

What is indicated by this picture?

A

there is no movement of drug out of the beaker, so the graph shows only a steep rise to maximum followed by a plateau.

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27
Q
A

a route of elimination is present, and the graph shows a slow decay after a sharp rise to a maximum. Because the level of material in the beaker falls, the “pressure” driving the elimination process also falls, and the slope of the curve decreases.

This is an exponential decay curve.

28
Q
A

drug placed in the first compartment (“blood”) equilibrates rapidly with the second compartment (“extravascular volume”) and the amount of drug in “blood” declines exponentially to a new steady state.

29
Q
A

illustrates a more realistic combination of elimination mechanism and extravascular equilibration. The resulting graph shows an early distribution phase followed by the slower elimination phase.

30
Q

Which model does this describe?

CONCEPT: the total approximation of all the compartments to which a drug goes
Relates the amount of drug in the body to the concentration of drug in the blood or plasma

A

Volume of Distribution

31
Q

This is known as what? Note x and y axis.

A

Plasma Concentration Curves

32
Q

______ Phase – immediately after administration of drug – movement from central to peripheral compartments.

A

Distribution

33
Q

_______ Phase – more gradual as drug is removed from circulation

A

Elimination

34
Q

Protein Binding

Many drugs travel on proteins in the blood (2)

A
  • albumin–binds acidic drugs and not metabolized in liver, stays in central circulation
  • alpha-1-acid glycoproteins–binds basic drugs, anesthetics
35
Q

Degree of protein binding is INVERSELY PROPORTIONAL to what?

A

VOLUME OF DISTRIBUTION

36
Q

_______ drug crosses cell membranes

A

Unbound

37
Q

_____ drug is more available for elimination.

A

Free

38
Q

KNOW!

Drug that is protein bound is pharmacologically inert. True or false?

A

false

NOT inert!

39
Q

The rate of a chemical reaction is directly proportional to the molecular concentrations of the reacting substances is known as what?

A

law of mass action

40
Q

Whether or not a drug exists predominately in an ionized vs. nonionized state affects how well it permeates membranes is known as:

A

ionization

41
Q

What determines the degree of ionization of a drug? (2)

A

pK of substrate
pH of surrounding fluid

42
Q

If a membrane separates areas of 2 differing pHs (ex. stomach, renal tubules, placenta), then the nonionized portion of a drug diffuses and equilibrates, but the ionized form does not, so large concentration differences exist on either side of the given membrane. Known as what?

A

Ion trapping

43
Q

‘removal of drug from plasma is known as:

A

Clearance

44
Q

KNOW:

Clearance involves what organs? (2)

A
  • kidneys – ester hydrolysis
  • **liver ** – Hofmann elimination, water soluble metabolites

Note: Cis is metabolized by Hofmann elimination!

45
Q

Enzymatic alteration of drug’s chemical structure is known as:

A

metabolism

46
Q

Metabolism – enzymatic alteration of drug’s chemical structure – 4 major types of reactions

A

oxidation – conjugation
reduction – hydrolysis

47
Q

When does propofol reach the brain in the flowchart?

A

Drug concentration at site of action

48
Q

What typeof receptor is a ß-agonist receptor?

What type of drug acts on this receptor?

A

membrane

phenylephrine

49
Q

What type of receptor is a GABA (gamma-aminobutyric acid) receptor?

A

ligand-gated

50
Q

What drug acts on a GABA receptor?

A

Versed allows the influx of Cl-

51
Q

The Na+ channel receptor is an example of what type of receptor?

A

voltage-gated ion channel

52
Q

What tyype of drug acts on the Na+ channel?

A

local anesthetics

53
Q

Phosphodiesterase inhibitors are an example of what type of receptor?

A

enzyme

54
Q

Milrinone is an example of this type of receptor:

A

enzyme receptor

55
Q

What type of drug can run out of endogenous substrate (tachyphalaxis)?

A

ephedrine

56
Q

KNOW

Ephedrine is an example of an ______ acting receptor agonist.

A

indirectly

Can run out of substrate–>tachyphalaxis–> more drug needed to produce response

57
Q

What is the definition of a hyperactive response to drug?

A

give a small dose and get an exaggerated response

58
Q

What is the definition of tachyphylaxis?

A

Have to increase the dose to get the original effect

59
Q

What is the definition of an additive effect of a drug response?

A

1+1=2

Example: MAC of inhalational agents

60
Q

What is the definition of an antagonistic effect?

A

Less effect if 2 drugs are combined.

61
Q

What is the definition of a prodrug?

What is an example of a prodrug?

A

Metabolized in the liver and becomes active

Morphine or codeine

62
Q

Intraosseous route is preferred when?

A

Mostly in kids too little to do IV

63
Q

KNOW:

2-Compartment Model

The central compartment represents ____% of cardiac output and ____% of body mass.

A

75

10

64
Q

What does it mean when drug has low Vd?

A

Wants to stay in the central compartment, like Roc.

65
Q

How much drug stays in the central compartment?

What does it mean when drug has high Vd?

A

Drug wants to redistribute, like propofol.

Anes. Pharm. Me (15 decks)

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