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SRNAPharmacology I > Basics of Pharmacology: Pharmacodynamics > Flashcards

Basics of Pharmacology: Pharmacodynamics Flashcards

1
Q

What is the definition of PHARMACODYNAMICS

A

What the drug does to the body.

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2
Q

The pharmacological effect is produced when?

A

When the drug from a complex with the drug receptor.

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3
Q

Change in drug effect ______(is or is not) proportional to the change in drug dose or concentration.

A

is not proportional

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4
Q

Pharmacodynamics follow the law of

A

Mass action

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5
Q

What is mass action

A

The concentration of a ligand plus the concentration of receptors –> Drug -receptor complex change.

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6
Q

Receptor theory :LOCK and KEY” hypothesis

A

The drug need to have the key to the receptor (lock). drug need a particular shape to enter lock. (Chemical structure of drug and receptor should match)

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7
Q

Lock and key governed by 2 basic concepts

A

Affinity

Intrinsic activtiy.

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8
Q

What is Affinity

A

how well a particular compound is drawn into and held a the binding site.

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9
Q

What is Intrinsic activity?

A

Describe effect the ligand has when it interacts with a receptor site.

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10
Q

What is affinity and intrinsic activity determined by?

A

Chemical structure.

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11
Q

Concentration vs response curves

A

relationship between the dose of the drug given and the resulting pharmacologic effect.

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12
Q

Concentration vs response curves help described

A

Potency
Slope
Efficacy
Individual responses

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13
Q

What is EC 50? What is it a measure of?

A

the concentration associated with 50% of peak drug effect and is a measure of drug POTENCY

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14
Q

What is Emax?

A

Maximum possible drug effect and no further increases in drug dose produce a GREATER EFFECT.

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15
Q

The smaller EC 50 the (more /less ) ______potent.

A

The MORE POTENT the drug

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16
Q

What are the factors affecting POTENCY?

A

Pharmacokinetics (ADME) + affinity to the receptors.

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17
Q

Potency refers to :

A

the quantity of drug that must be administered to produce a specific drug effect.

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18
Q

Effective Dose (ED) of a drug is

A

The dose required to produce a specific effect

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19
Q

The lower the ED the (more/less) potent

A

the more potent

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20
Q

What is ED 50?

A

Dose of a drug required to produce a speficic desired in 50% of INDIVIDUALS RECEIVING THE DOSE>

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21
Q

What is Median ED 50?

A

Dose of a drug required to produce a speficic desired in 50% of INDIVIDUALS RECEIVING THE DOSE>

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22
Q

What is ED 90?

A

Dose of a drug required to produce a specific desired in 90% of INDIVIDUALS RECEIVING THE DOSE

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23
Q

Median Lethal dose (LD50)

A

Dose of a drug required to produce DEATH in 50% of INDIVIDUALS RECEIVING THE DOSE

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24
Q

The closer the ED and LD are: the more/less dangerous

A

The more diligent you should be with your DOSING

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25
Q

Efficacy definition

A

Measure the INTRINSIC ABILITY of a drug to produce a given physiological effect.

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26
Q

Efficacy is more/less ______Important than potency

A

More

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27
Q

What is the Therapeutic index OR

A

Margin of safety– the DIFFERENCE between the dose of a drug that produces a desired effect and the dose that produces undesirable effect.

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28
Q

What is the TI mathematically?

A

LD50/ED 50

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29
Q

The LARGER THE THERAPEUTIC INDEX, The ______the drug is for administration.

A

SAFER

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30
Q

Therapeutic window

A

Therapeutic window is the range of steady-state

concentrations of drug that provides therapeutic efficacy with MINIMAL toxicity

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31
Q

INDIVIDUAL VARIATION (meaning)? What can it influence?

A

Diffrent people have different response, Can influence efficacy and safety of a drug.

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32
Q

________lean body mass and ______Body fat tissue increases the Vd of lipid soluble drugs

A

Decreased: increased

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33
Q

**What is decreased in the elderly making them at risk for decrease clearance of opioids, hypnotics and benzo? What consideration should be made?

A

Decreased CO, liver blood flow and liver metabolic clearance.
Decrease the dose.

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34
Q

**A decreased in plasma protein binding does what to the free drug form

A

Increase the effect of highly protein bound drugs.

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35
Q

Classic example of highly drug bound DRUG? What happens with low protein state

A

Phenytoin; severe phenytoin toxicity may occur.

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36
Q

***Myasthenia Travis patients have _______ number of post-synaptic nicotinic receptors on skeletal muscles. They are sensitive to muscle relaxants (e.g. Succynylcholine) that act on the ______ ______ receptors:

A

Decreased; NICOTINIC ACETYLCHOLINE.

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37
Q

**G6PD deficiency– Certain medication can cause

A

HEMOLYTIC ANEMIA

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38
Q

Warfarin variability –________enzyme and receptor _____

A

polymorphisms- CYP2C9

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39
Q

BRIEF : STEREOCHEMISTRY , what is it

A

The branch of organic chemistry that describes how molecules ARE STRUCTURED in 3 Dimensions (3D)

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40
Q

What is an isomer

A

compounds with same MOLECULAR formula.

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41
Q

StereoISOMER

A

kind of isomer, different only in the way ATOMS ARE ORIENTED IN SPACE (molecular formula is identical)

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42
Q

Enantiomers definition? do they interact the same.

A

pair of molecules existing in 2 forms that are MIRROR images of another but cannot be SUPERIMPOSED.

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43
Q

Drugs may have CHIRAL CARBON, why?

A

It is where the molecules can move to change the arrangement.

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44
Q

Any enatiomers have

A

CHIRAL CARBON>

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45
Q

A drug can have more than ______chiral carbon? examples is________ , it has _____ enantimers, meaning ?

A

more than 1 enantiomer; Labetalol; you administer 4 enantiomers (4 mechanism actions, same molecular formula, arranged differently–> 4 actions>) with labetalol.

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46
Q

Enantiomers naming system: when dissolved in solution , can be distinguished that rotated

A

POLARIZED Light

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47
Q

***d or +

A

rooted POLARIZED light to the RIGHT (clockwise)

48
Q

*** l or (-)

A

rooted POLARIZED light to the LEFT (counterclockwise)

49
Q

***What is a racemic mixtures? Does it rotate to polarized light?

A

50:50 mixtures of 2 isomers; NO

50
Q

All drugs are racemic mixtures

A

NO

51
Q

A drug with R is _____ and S is _____

A

Rectus; Sinister

52
Q

The binding of a chemical to a receptor is

A

STEREOSPECIFIC

53
Q

The majority of drugs has to _______ ____ ____ ______

A

bind to a receptor

54
Q

Some examples of RACEMIC MIXTURES: ________and ________

A

Thiopental

Methohexital

55
Q

All volatile anesthetics are racemic mixtures except:

A

Sevoflurane (one enantiomer)

56
Q

Ketamine is a racemic mixtures of :

A

S and R

57
Q

S (+) form in Ketamine

A

has a greater NMDA receptor affinity ; is MORE POTENT is LESS LIKELY to produce EMERGENCE DELIRIUM

58
Q

R (-) form in Ketamine

A

form is weaker and PRODUCES emegence and delirium

59
Q

Local anesthetics such as ______ and ______ are racemic mixtures

A

Bupivacaine and Prilocaine.

60
Q

MEMORIZE: Hyperractive

A

low doses of medications leads to HIGHER expected effect.

61
Q

MEMORIZE: Hypersensitive

A

when a patient is allergic (sensitive) to a drug

62
Q

MEMORIZE: Hyporeactive

A

high doses of medication required to evoke desired effect

63
Q

Types of hyporeactivity :Tolerance

A

Hyporeactivity required from chronic exposure to a drug.

64
Q

MEMORIZE**Types of hyporeactivity: Cross-tolerance

A

Tolerance to a drugs through continued used of another drugs /substance, with similar pharm. effects.

65
Q

Example of cross tolerance ; Ask what question

A

Volatile anesthetics and Alcohol use (ask how much patient drinks)

66
Q

Types of hyporeactivity :Tachyphylaxis

A

Tolerance that develops rapidly only after a few doses. (loss of drug response after a few doses)

67
Q

3 types of hyporeactive reactions

A

Tolerance
Cross tolerance
Tachyphylaxis

68
Q

Mechanism of action of TOLERANCE

A

NEURONAL ADAPTION as a cellular tolerance
Decreased in number of receptors
Enzyme induction
Decrease neurotransmitter release.

69
Q

2 Types of HYPERREACTIVITY

A

immunity

idiosyncrasy – Unusual effect (NO IDEA about why and how)

70
Q

Drug to drug interactions: additive

A

Additive effect: 1+1 = 2 (increase predictable

Ex: anesthetic effect 2 different inhaled anesthetics

71
Q

drug to drug interaction : Synergistic

A

1+1 =4 two drugs interact to produce a much greater effect. ex: mepivacaine + bupivacaine

72
Q

Drug to drugs : Antagonistic

A

Agonist with antagonist (fentanyl and narcan)

73
Q

What is a receptor?

A

cellular protein macromolecule to which a drug binds to bring about a response.

74
Q

What is an Agonist?

A

ACTIVATOR; mimics the expected receptor response

75
Q

What is a full agonist

A

High efficacy or HIGH INTRINSIC activity –> FULL/Maximal response.

76
Q

Agonist can be (examples)

A

Drug, molecule or neurotransmitter

77
Q

What is a PARTIAL AGONIST

A

Not as good of a response as a full agonist. LOW INTRINSIC ACTIVITY at the receptor.

78
Q

**What happens when a partial agonist is given with a full agonist?

A

act as a partial agonist and DECREASES the effects of a full agonist. Ex: Buprenorphine (partial agonist at the Mu receptor) and morphine (Full agonist at the opioid mu receptor)

79
Q

A partial agonist given a alone Does it act an antagonist.?

A

Does not act as an antagonist

80
Q

What is a antagonist

A

Bind, doest not activate, and prevent agonist from binding.

81
Q

No intrinsic activity or affinity to the receptor is :

A

ANTAGONIST

82
Q

Atropine is

A

Blocks the effects of ACh at a muscarinic receptor

83
Q

Beta blockers

A

Beta receptor antagonist.

84
Q

Flumanezil does what

A

Blocks the effect of diazepam at the bentzo site

85
Q

Competitive antagonists (REVERSIBLE)

A

binds to a receptor at the same binding site as the ENDOGENOUS LIGANTS or agonist, THEY COMPETE

86
Q

The maximal effect can still be achieved if sufficient agonist is given in

A

Competitive antagonists

87
Q

Competitive antagonists (REVERSIBLE) example

A

All non-depolarizing NEUROMUSCULAR Blocking agents.

88
Q

NONCOMPETITIVE IRREVERSIBLE ANTAGONIST

A

binds permanently via COVALENT bond to the active site

89
Q

NONCOMPETITIVE PSEUDO- IRREVERSIBLE ANTAGONIST

A

Does not bind covalently

90
Q

The log dose effect curve is shifted: agonist in presence of noncompetitive antagonist

A

DOWNWARD slightly to the right

91
Q

Allosteric (Non-competitive) antagonist

A

binds to a different sites (different binding site from agonist)

92
Q

Does allosteric compete with agonist at active site.

A

NO

93
Q

***ALLOSTERIC POTENTIATION

A

Compound acts at an ALLOSTERIC SITE and enhances the AFFINITY of the normal agonist at its binding site

94
Q

ALL benzo are -_____________

A

Allosteric potentiators ( they bind to the GABAa complex to increase the affinity of GABA to its binding site)

95
Q

INVERSE AGONIST is

A

Binds selectively to the INACTIVE STATE of the receptor and shift the equilibrium of the receptors to the inactive ; keep them in the inactive state, THEY HAVE NEGATIVE INTRINSIC ACTIVITY.

96
Q

Clinically: inverse agonist exert ______ effect of pharmacological

A

exert the OPPOSITE OF THE PHARMACOLOGY EFFECT of a receptor agonist.

97
Q

Examples of inverse Agonist

A

Antihistamine drugs at histamine-1 receptors.

98
Q

Up-regulation of receptors

A

Increase in the number of receptors –> Cells become hypersensitive to the receptor agonist

99
Q

Down regulation of receptors

A

Decreased in the number of receptors.

100
Q

***REMEMBER: if drugs form COVALENT BOND WITH A RECEPTOR…

A

It is always IRREVERSIBLE>

101
Q

Termination of drugs response: ADME

A

Metabolism–> inactive –> no longer active

Excretion –>

102
Q

Redistribution is when –>

A

drugs distributes from site of action to other tissues

103
Q

Main factor in terminating drugs that are HIGHLY LIPID SOLUBLE (like waking up from anesthesia is )

A

RESTRIBUTION

104
Q

With regard to drug-receptor binding:

A competitive antagonist ________intrinsic activity –

A

A competitive antagonist has no intrinsic activity –

105
Q

A partial agonist:

A

Has a dose response curve similar to that of a full agonist in the presence of a non-competitive antagonist.

106
Q

A Basic drug with a pKa of 8.7

A

Will be predominantly ionized at plasma p

107
Q

The CNS effects after bolus injection of an IV anesthetic agent are terminated primarily by__________

A

REDISTRIBUTION

108
Q

______ is an increase in the number of receptor; Occurs from lack of use of the receptor

A

Up-regulation

109
Q

Down-regulation – ________ in the number of receptors

A

decrease

110
Q

Occurs from excessive stimulation from an agonist or overuse of the
receptor

A

down regulation

111
Q

Receptors have 2 major functions

A

Ligand Binding

Signal Transduction – Message Propagation

112
Q

Receptors have 2 functional domains

A

Ligand-Binding domain

Effector domain

113
Q

Non-surmountable IRREVERSIBLE ANTAGONIST

A

PHENOXYBENZAMINE

114
Q

Antagonist Competitive reversible example

A

i.e.: Non-depolarizing neuromuscular blockers

115
Q

Examples of enantiomeric differences important in anesthesia:

A

cisatracurium is an atracurium isomer that doesn’t cause histamine release

SRNAPharmacology I (29 decks)

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