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Pharm 2 > Pharmacodynamics and Pharmacokinetics > Flashcards

Pharmacodynamics and Pharmacokinetics Flashcards

1
Q

Receptors are typically ____ ?

A

Proteins

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2
Q

When receptors are activated what happens?

A

Conformational change in receptor

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3
Q

The number of receptors bound to a drug determines? what drugs are a good example of this?

A

The effect of the drugs
NMB’s

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4
Q

Agonists

A

Activates a receptor by binding to it

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5
Q

What are the different types of bonds (3 mentioned in class)?

A

Ion (electrocovalent… opposite charged ions)
Hydrogen (bonding to a very electronegative atom)
Van der waals interaction (the sum of attractive or repulsive forces; creates an orbital shift)

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6
Q

What type of bond is not reversible?

A

Covalent

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7
Q

Antagonist

A

Binds to a receptor but does not activate it.

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8
Q

Competitive antagonism

A

increasing amounts progressively inhibit the agonist. The antagonist can be out competed by the agonist

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9
Q

Non-competitive antagonism

A

Even high doses of the agonist cannot out compete the antagonist for the binding site.

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10
Q

Partial agonist

A

Binds to the receptor at the agonist site but causes less response even at supramaximal doses

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11
Q

Inverse agonist

A

Binds to the agonist site but produces the opposite effect

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12
Q

What is tachyphylaxis?

A

a tolerance that develops quickly to a drug

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13
Q

What are two examples of tachyphylaxis that were given in class?

A

-Albuterol treatments for asthma, down regulation of receptors d/t repetitive treatments
-Pheochromocytoma, decreased receptors in response to catecholamines

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14
Q

What are 3 locations of receptors?

A

Lipid Bilayer
Intracellular proteins
Circulating proteins

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15
Q

What drug used commonly in the OR for BP causes tachyphylaxis?

A

Ephedrine

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16
Q

What drugs have receptors located in the lipid bilayer?

A

opioids, benzos, beta-blockers, and NMB

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17
Q

What drugs have receptors that are intercellular proteins?

A

Insulin, steroids, milrinone

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18
Q

What drugs have receptors that are circulating proteins?

A

Anticoagulants

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19
Q

what is pharmacokinetics?

A

QUANTITATIVE study of injected and inhaled drugs and their metabolites

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20
Q

What are the four components of pharmacokinetics?

A

Absorption
Distribution
Metabolism
Excretion

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21
Q

Are the pharmacokinetics the same for every patient?

A

No.

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22
Q

What is the 1 compartment model of distribution?

A

Immediately following injection of the drug the drug is diluted by the plasma and then it gets excreted. This is an unrealistic model

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23
Q

What is the central compartment?

A

This is what dilutes the drug within the first minute following injection

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24
Q

What is a “vessel rich group”?

A

These are areas of the body that get a large percentage of cardiac output (brain, lungs, kidneys, liver).
Vessel rich = 10% of body mass and get 75% of CO

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25
Q

Describe a two compartment model?

A

Injected into central compartment, distributed to peripheral compartments, then back to central compartment where it will then go through liver and kidney to be excreted

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26
Q

What drugs are 65% taken up in 1st pass effect

A

lidocaine, propanolol, meperidine, fentanyl, sufentanil, alfentanil

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27
Q

Acidic drugs bind primarily to?

A

Albumin

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28
Q

Alkalotic drugs bind primarily to?

A

Alpha-1 Acid Glycoprotein

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29
Q

Bound or unbound drug can cross cell membranes?

A

FREE “unbound” drug can only cross cell membranes to be distributed

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30
Q

Bound or unbound drugs determine concentration available to receptor (potency)?

A

FREE “unbound” drug

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31
Q

What happens when we give a drug that binds to plasma proteins to a patient with low albumin?

A

There will be more free drug that can have a greater effect.

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32
Q

What types of patients may have decreased plasma proteins (4)?

A

Elderly, hepatic disease, renal failure, pregnancy

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33
Q

If normal free fraction of drug is 2%, but patient has 50% less albumin, what is the free fraction of the drug?

A

4%! it will double.

34
Q

If a drug is poor protein binding and lipophilic will it have large or small volume of distribution? What are some drug examples from class?

A

Large volume of distribution.
Thiopental and Diazepam

35
Q

If a drug is highly protein bound to plasma proteins will it have large or small volume of distribution?
What drug is an example of this?

A

Small volume of distribution.
Warfarin

36
Q

This process converts active lipid soluble drugs into water soluble and inactive metabolites.

A

METABOLISM

37
Q

What are some drugs that have active metabolites?
Why is this important?

A

Diazepam, propanolol, morphine (has 2), prodrugs such as codiene.
The drugs keep working so you may have a build up of drugs

38
Q

Name five ways the body metabolizes drugs.

A

Hepatic microsomal enzymes
plasma (hoffman degradation and ester hydrolysis)
Kidneys
Tissue esterase (GI, and Placenta)

39
Q

What is Phase 1 reaction metabolism?

A

These increase polarity and prep for phase 2 reactions. Involves oxidation, reduction, hydrolysis

40
Q

What is phase 2 reaction metabolism?

A

Covalently link with a highly polar molecule to become water soluble.
Conjugation reactions.

41
Q

CYP450 enzymes

A

Large family … 10 isoforms
Membrane bound
contain a heme facgor
involved in oxidation and reduction

42
Q

CYP2: ___ % homologous

A

40

43
Q

CYP2A: ___% homologous

A

55

44
Q

CYP2A6 is ?

A

The individual enzyme

45
Q

What is the most common Phase 1 enzyme of the CYP450 enzymes

A

CYP3A4
up to 60% of all CYO450 activity
Metabolizes >50% of drugs that anesthesists give

46
Q

What happens when you give a metabolism inducer? What is a drug that can do this?

A

It will increase the amount of the metabolic enzyme that is present and will increase the metabolism of the drug.
Ex// Phenobarbital

47
Q

What happens when you give a metabolism inhibitor?
Example of this?

A

It will decrease the amount of metabolic enzyme activity and you may have the drug sticking around longer causing toxic levels.
Grapefruit juice.

48
Q

Alcohol and weed will do what to anesthetic requirements and why?

A

Increase requirements, because they induce CYP450 enzymes

49
Q

equation for rate of drug metabolism

A

Q (C inflow - C outflow)
(Concentration in minus concentration out) Multiplied by the % of CO that the liver gets.

50
Q

Flow limited clearance

A

% of CO (Q) limits the metabolic rate

51
Q

Capacity limited clearance

A

Liver’s ability to metabolize is the limiting factor

52
Q

Name 3 factors affecting renal clearance.

A

GFR, Active tubular secretion, and passive tubular reabsorption

53
Q

Passive tubular reabsorption is increased in what kind of drug?

A

Lipid soluble drugs have increase passive tubular reabsorption (thiopental). Water soluble drugs have almost zero of this.

54
Q

What is active tubular secretion and name a drug this occurs with?

A

Drug is secreted from peritubular capillaries by an active transport process to be excreted.
Penicillin.

55
Q

Define elimination half time

A

The time necessary to eliminate 50% of drug from PLASMA after a bolus dose.

56
Q

What is context sensitive half time?

A

Time til a 50% decrease after infusion is discontinued.
This assumes the drug was given at a constant concentration.
Typically increases the longer the infusion decreases

57
Q

What is elimiation HALF LIFE?

A

The time it takes to elmiinate 50% from the BODY.

58
Q

What drugs do we really have to worry about with their context sensitive half time? What are some drugs that we don’t worry about? (graph in class)

A
59
Q

When the PK and pH are identical, how much is ionized and non-ionized?

A

50% ionized, 50% nonionized

60
Q

Example of weak acids drug?
They ionize in what pH?

A

Barbituates
acids ionize in alkaline pH

61
Q

Example of weak bases?
They ionize in what pH?

A

Local anesthetics and Opioids
Bases ionize in acidic pH

62
Q
A
63
Q

What is the saying to remember if drugs are nonionized?
What is the trick with weak acids and bases to remember their equation?

A

-“nicely negative numbers are nonionized”
- weak Acids, pk After ph
-weak Bases, pk Before ph

64
Q

what is ion trapping?

A

when the drug becomes ionized and cannot pass the lipid bilayer. Sometimes we want this and sometimes we dont.

65
Q

What is pharmacodynamics?

A

what the drug does to the body, the sensitivity of the body to the drug.

66
Q

What is potency?

A

Looking at how much concentration it take to get the desired effect.
Less drug and more effect = more potent.

67
Q

What is efficacy?

A

The ability of the drug to produce a clinical effect

68
Q

What is relative potency?

A

The time to drug effect. So if the concentration of a drug in the system correlates exactly with when the effects are seen it is more potent. (fentanyl v alfentanil example)

69
Q

ED50

A

Dose required to produce effect in 50% of patients

70
Q

LD50

A

Dose required to produce death in 50% of patients

71
Q

Therapeutic index equation?
Narrow or wide safer?

A

Ld50/ Ed50
Wide TI is safer.

72
Q

What is stereochemistry?

A

How drug molecules are structured in 3 dimensions

73
Q

Chiral compound definition

A

Molecules with asymmetric centers usually in relation to the way carbon molecules are bonded.

74
Q

What are enantiomers?

A

Molecules that are Mirror images , chemically identical, but can’t be superimposed

75
Q

Optical isomers
Left?
Right?

A

enantiomers that rotate light in different directions
Left: Levarotary, sinister
Right: Dextrorotary, Rectus

76
Q

What is a racemic mixture?

A

A 50/50 mixture of a D and L enantiomer. One is active and one is inactive and may have side effects.

77
Q

Pharmacogenetics definition

A

How a single gene or all genes (genome) influences responses to drugs

78
Q

L isomer of bupivicaine has less?

A

Cardiac side effects

79
Q

Cisatracurium has less of what side effect?

A

Histamine release

80
Q

S- enatiomer of ketamine is more potent with less of what side effect?

A

Delirium

Pharm 2 (4 decks)

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