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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Pharmacodynamics meaning

A

Pharmacodynamics describes the effect of the drug on the body

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2
Q

Components of pharmacodynamics

A

Drug Action: invisible changes
Drug effect: visible changes
Drug response

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3
Q

Drug effect definition

A

Physiology changes brought about by a drug

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4
Q

Types of drug effects

A

1). Desired effects
2) Side effects
3) adverse effects

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5
Q

What is desired effect

A

Refers to the physiology changes that are expected and desired
Occurs at the normal therapeutic dose of the drug

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6
Q

What are side effects

A

Refers to physiology changes that are expected but undesired
Occurs at normal therapeutic dose of the drug

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7
Q

Adverse effects meaning

A

Refers to physiological changes that are unexpected and undesired
Can occur at any dose
Can be life threatening

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8
Q

List the use, side effects and adverse effects of aspirin

A

Used to treat clotting problems
Side effect is bleeding
Adverse effects= Reye syndrome that presents as hepatic encephalopathy ie leads to liver and brain damage

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9
Q

Septrin: Desired effect, side effect, adverse effect

A

Desired effects: Used to treat infections
Side effects: Coloration of the urine
Adverse effect: Steven Johnson syndrome (peeling of the skin)

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10
Q

The body responds to a drug in two ways

A

Effectively or lethally

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11
Q

Factors that determine drug effect

A

1) Dose
2) Drug interaction
3) weight
4) Age
5) Genetics
6) Disease
7) Diet

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12
Q

What curve shows the relationship between the dose and drug response

A

LDR curve
Log Drug Response curve

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13
Q

Important things to know about the dose response relationship

A

Dose of a drug is directly proportional to the response
Meaning an increase in the dose= an increase in the response

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14
Q

Features of LDR curve

A

1) It is sigmoid shaped
2) Log dose on the X-axis (abscissa)
3) Response on the Y-axis( ordinate)
4) possess an Emax
5) About 20-80% of the curve is a straight line used for statistical analysis
6) Drugs with similar mechanism of action have parallel curves

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15
Q

List the two experiments used for dose response

A

1) Graded response
2) Quantal response

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16
Q

Characteristics of the graded response experiment

A

1) It Is done on only one subject
2) it is to identify the relationship between the dose and the intensity of effect
3) Used to identify the potency and the Efficacy Emax

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17
Q

Major Parameters gotten from the log dose response graded experiment

A

Potency/ Effective concentration EC50
Efficacy/ Emax

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18
Q

Define potency of a drug/ effective concentration EC50

A

Potency is measured as the dose required to produce 50% of the maximal response

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19
Q

Define efficacy/ E max

A

The maximum drug response that can be achieved

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20
Q

The smaller the dose the __________the potency
The higher the dose the ___________ the potency

A

1). The higher the potency
2) The smaller the potency

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21
Q

Characteristics of quantal experiment

A

1) it is carried out on a population
2) it is also known as All or none response
3) it’s target is to know the frequency of effect
4) outcome: DR- Quantal curve

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22
Q

Parameters for Dose response Quantal curve

A

1) Effective dose ED50
2) Lethal dose LD50
3) Therapeutic Index TI
4) Margin of safety MS

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23
Q

Define Effective Dose 50

A

This refers to the dose required to cause an effect in 50% of the population

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24
Q

Lethal dose 50 meaning

A

This can be defined as the dose required to cause death in 50% of the population

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25
Q

Define therapeutic index

A

This refers to the ratio of the lethal dose in 50% of the population divided by the effective dose for 50% of the population

TI: LD50/ED50

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26
Q

Why is the TI a measure of a drugs safety

A

Because the larger the value of TI indicates a larger LD50 meaning that a large amount of the drug has to be given to cause death

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27
Q

True or false
Large Therapeutic index= toxic drug

A

F
Large therapeutic index means that the lethality is high so it would take a large dose of the drug for it to be toxic

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28
Q

Define margin of safety

A

Refers to the ratio of the lethal dose of 1% of the population divided by the ration of the effective dose for 99% of the population
M.I= LD1/ED99

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29
Q

What is drug interaction

A

Effects of two drugs being used concurrently on each other’s drug effect

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30
Q

Four major drug interaction

A

1) additive
2) synergism
3) potentiation
4) antagonism

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31
Q

Define additive interaction

A

Enhancement of the effect by combining two already effective drugs
1+1=2
E.g paracetamol and ibuprofen

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32
Q

Define Potentiation

A

Enhancement of the effect of one drug by another that has no effect by itself, when combined
1+0=2
E.g Levodopa +Carbidopa
Used for treating pakinstons disease
Or
Amoxicillin+ Clavulanic acid( augumentin) for treating infections

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33
Q

Define synergism

A

Enhancement of the effect of one drug by another which has the same effect, than when used individually
1+1>2
E.g penicillin + aminoglycoside
Prednisolone + NSAIDS

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34
Q

Define antagonistic drug interaction

A

Attenuation/ decrease of the effect of one drug by another which has the opposite effect
1+1<= 1
Propranolol + salbutamol
Pilocarpine + Atropine

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35
Q

Types of antagonism

A

1) chemical antagonism
2) physiological antagonism
3) pharmacological antagonism

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36
Q

Amlodipine and atenolol is for treating what and what type of drug interaction is it

A

Additive drug interactions
Anti hypertensive drug

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37
Q

List an additive analgesic drug combination

A

Aspirin and paracetamol

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38
Q

Nitric oxide and halothane is used for treating what and is what type of interaction

A

Additive drug interaction
Used as a general anasthetic

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39
Q

List an example of hypoglycaemic drugs that are additive

A

Glibenclamide + metformin

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40
Q

Ephedrine + theophyline is used for treating what and is what type of interaction

A

An additive interaction
As a bronchodilator

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41
Q

Fentanyl

A

Highly potent drug used as pain medication

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42
Q

Low potent drug also used for pain relief

A

Meperidine

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43
Q

Types of drugs that undergo chemical antagonism

A

Dimercaprol and mercuric ion
Deferoxamine and iron

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44
Q

Histamine and adrenaline undergo what type of antagonism

A

Physiological

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45
Q

Types of drugs that undergo stimulation

A

Pilocarpine on salivary glands , adrenaline on heart muscle

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46
Q

Types of drugs that undergo depression

A

Barbiturates on CNS, quinidine on heart, omeprazol on gastric secretion

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47
Q

Types of drugs that undergo replacement

A

Levodopa in Parkinson’s disease
Insulin in diabetes mellitus

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48
Q

Types of drug that undergo cytotoxic action

A

Cyclophosphamide, zidovudine, penicillin

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49
Q

Examples of drugs that use physical mechanisms of drug action: when the drug does not produce any chemical reaction or change in the cells of the body and the effect is only physical

A

Activated charcoal binding with poisons in the stomach
Mannitol used as an osmotic diuretic
Bulk laxative e.g ispaghula

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50
Q

Examples of chemical mechanisms of drug action

A

1) sodium bicarbonate as an antacid
2) dimercaprol, deferoxamine, pennicillamine (copper poisoning) as chelating agents
3) pralidoxamine: organophosphate poisoning
4) cholestyramine

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51
Q

Examples of competitive inhibitors

A

Angiotensin converting enzymes e.g Captopril
Reversible Anticholinesterases e.g neostigmine, physostigmine
Alloprinol to inhibit xanthine oxidase

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52
Q

Examples of non competitive inhibitors

A

Irreversible anticholinesterases e.g organophosphorous compounds
Aspirin inhibits cyclooxygenase enzymes
Monoamine oxidase inhibitors used to treat depression e.g imipramine
Proton pump inhibitors e.g omeprazole inhibits the H+/k+/ATpase in parietal cells of the stomach

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53
Q

List the sodium channel drugs

A

Quinidine, procainamide, local anaesthetics

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54
Q

Define chemical antagonism

A

Caused by combination of agonists with antagonist with resulting inactivation of the agonist e.g dimercarpol and mercuric ion

55
Q

Define physiological antagonism

A

Caused by agonist and antagonists acting at two independent sites and inducing independent but opposite effects e.g histamine and adrenaline

56
Q

Define pharmacological antagonism

A

In this case the term competitive and non competitive antagonism are used

57
Q

T or F in competitive antagonism
The Emax is unchanged
The potency or km is decreased

A

T
Competitive the potency is decreased
Emax remains the same

58
Q

T or F in non-competitive antagonism
The Emax is unchanged
The potency or km is decreased

A

F
Emax is decreased
Potency remains the same

59
Q

Are Acetylcholine and atropine types of competitive or non competitive antagonists

A

Competitive

60
Q

List types of non competitive agonists

A

Epinephrine and dibenamine

61
Q

What type of drug action does eosinopril give

A

Depression
Reduces blood pressure

62
Q

What type of drug action does methylsalicitic acid give

A

Irritation

63
Q

Calcium channel drugs

A

Nifedipine, verapamil, diltiazem
Block the voltage gated calcium channels useful in hypertension and arrhthmias

64
Q

List potassium channel drugs

A

Amiodarone, sulfonylureas

65
Q

List chloride channel drug

A

Benzodiazepines

66
Q

What drug inhibits choline carrier

A

Hemicholinium

67
Q

Inhibition of noradrenaline vesicular uptake is by _________

A

Reserpine

68
Q

Examples of agonist drugs

A

Acetylcholine, adrenaline, noradrenaline, benzodiazepines( for gaba receptors)

69
Q

Examples of antagonistic drugs

A

Atropine, scopolamine ( both inhibit acetylcholine receptors)
Phenylbenzamine ( inhibit adrenergic receptors)
Flumazenil

70
Q

Examples of inverse agonist drugs

A

Beta carbolines inverse agonists of gaba receptors

71
Q

Inhibition of neuronal reuptake of noradrenaline is by ________

A

Desipramine

72
Q

Inhibition of neuronal reuptake of serotonin is by ________

A

Fluoxetine

73
Q

Inhibition of weak acid carrier by drugs ________

A

Probenecid

74
Q

Antagonists of gaba receptors

A

Flumazenil

75
Q

Carbolines are inverse agonists of what receptors

A

Gaba receptors

76
Q

Most drugs produce their effects by interacting with a discrete target bio molecule list them

A

RICE
1) Enzymes
2) carrier molecules
3) ion channels
4) receptors

77
Q

What are ligands

A

Ligands are substances that interact at the receptor binding site
Could be endogenous or exogenous

78
Q

List characteristics of receptors

A

1) sensitivity
2) specificity
3) selectivity
4) saturability

79
Q

Define specificity of a receptor

A

A drug only binds to one single type of receptor and causes one single effect

80
Q

Define selectivity of a receptor

A

A drug binds to one or a few types of receptors with higher affinity than other receptors

81
Q

Define saturability of a receptor

A

A receptor has a limited number of binding sites and is therefore saturated at high ligand concentrations

82
Q

List the molecules serving as receptors

A

1) Enzyme
2) membrane proteins (glycoproteins, lipoproteins)
3) Nucleic acid
4) complex polysaccharide

83
Q

Define an agonist

A

An agent which activates a receptor to produce an effect similar to the physiological signal molecule

84
Q

Define antagonist

A

An agent which prevents the action of an agonist on a receptor but does not have an effect on its own

85
Q

Define partial agonist

A

An agent that activates a receptor to produce submaximal effect, but antagonizes the effect of a full agonist

86
Q

T or F grapefruit inhibits cyp450 enzymes

A

T

87
Q

T or F
Garlic causes increased bleeding when used with anticoagulant

A

T

88
Q

T or F tyramine containing foods should be taken with monoamine oxidase inihibitors

A

F

89
Q

Is phenobarbital an enzyme inhibitor or inducer

A

It is an enzyme inducer

90
Q

Inhibitors of cyp450 enzymes include (CIG POKER)

A

Cimetidine
Isoniazid
Grapefruit juice
Phenelzine (Mao inhibitor)
Omeprazole
Ketoconazole
Erythromycin
Retonavir

91
Q

Criteria for classifying receptors

A

Pharmacological criteria
Tissue distribution
Ligand binding
Transducer pathway
Molecular cloning

92
Q

Define inverse agonists

A

An agent which activates a receptor to produce an effect to the opposite direction to that of the agonist

93
Q

List drugs that have covalent bonds

A

Several anti cancer drugs
Organophosphate anticholinesterases

94
Q

Examples of ligands

A

Drugs, hormones, neurotransmitters

95
Q

List all the receptor theories

A

1) Occupancy theory
2) Rate theory
3) Stephenson theory
4) Ariens theory
5) The induced fit theory
6) Macromolecular perturbation theory

96
Q

What type of receptors does acetylcholine have

A

Nicotinic and muscarinic receptors
M1, M2, M3 etc
Nm and Nn

97
Q

List the criteria for classifying receptors

A

1) pharmacological criteria: Muscarinic, nicotinic, alpha and beta adrenergic
2) Tissue distribution: the cardiac beta adrenergic receptor as beta 1 and bronchial as beta 2
3) ligand binding
4) Transducer pathway
5) Molecular cloning

98
Q

What are silent receptors

A

These are sites which bind specific drugs but no pharmacological response is elicited

99
Q

Silent receptors are better called

A

Drug acceptors or sites of loss e.g plasma proteins

100
Q

What are spare receptors

A

A drug can produce the maximal response when even less that 1% of the receptor is occupied, the remaining unoccupied receptors are just serving as receptor reserve and are called spare receptors

101
Q

List dieases linked to receptor malfunction

A

1) myasthenia gravis : autoantibodies that inactivate nicotinic acetylcholine receptors
2) hypoparathyroidism: mutation of genes encoding GPCR’s
3) cancers: mutation of genes encoding GPCR’s
4) insulin resistant diabetes
5) Testicular feminisation
6) Familial Hypercholesterolaemia

102
Q

Ligand binding and channel binding opening occur on a millisecond timescale so they are confined to excitable tissues such as:

A

CNS, NMJ, autonomic ganglia

103
Q

G proteins are heterotrimeric molecules having 3 subunits ____, ____, _____

A

Galpha Gbeta Ggamma

104
Q

CAMP regulates many aspects of cellular functions such as

A

Cell division, cell replication, ion channels, ion transport

105
Q

Results of IP3-DAG pathway

A

1) Mediates/ modulates contraction
2) Secretion/ transmitter release
3) Neuronal excitability
4) Intracellular movements
5) eicosanoid synthesis
6) cell proliferation

106
Q

Examples of drugs that use enzyme linked receptors

A

Insulin receptors
Cytokine receptors

107
Q

Examples of drugs that use intracellular receptors

A

Steriod drugs

108
Q

Examples of drugs that use ligand gated receptors

A

GABA receptors
Nicotinic cholinergic receptors

109
Q

Examples of drugs that use G protein coupled receptors

A

Adrenergic receptors
Muscarinic cholinergic receptors

110
Q

List the types of receptors based on transduction pathway

A

Ligand gated ion channels
G protein coupled receptors
Intracellular receptors
Enzyme linked receptors

111
Q

List the 4 biomolecular structures that drugs can interact with in the biochemical way

A

RICE
Receptors
Ion channels
Carrier proteins
Enzymes

112
Q

List the classification of receptors

A

Pharmacological
Ligand binding
Transducer pathway
Tissue distribution
Molecular cloning

113
Q

What experiment is also called all or none rule

A

Quantal experiment

114
Q

If the drug binds to the same recognition site as the endogenous agonist it is called what

A

Primary agonist/ orthosteric

115
Q

If the drug binds to a different recognition site as the endogenous agonist it is called what

A

Allostetic agonists

116
Q

T or F adrenaline antagonizes histamine

A

T because the both bind to different sites on the lungs adrenaline and adrenaline causes bronchodilation by binding to beta 2 receptors which is opposite to bronconstriction caused by histamine through H1 receptors

117
Q

What is tachyphylaxis

A

Is a type of tolerance which occurs very rapidly

118
Q

What is desensitization

A

Decreased response to the agonist after it’s repeated injection in small doses

119
Q

Example of competitive antagonists

A

Atropine- acetylcholine
Morphine- Naloxone
Adrenaline- histamine

120
Q

Example of non competitive antagonists

A

Diazepam- Bicuculline

121
Q

Repeated administrations of a drug results in

A

Diminished effect (tolerance)

122
Q

Which type of tolerance occurs very rapidly

A

Tachyphylaxis

123
Q

What is desensitization

A

Decreased response to the agonist after it’s repeated injection in small doses

124
Q

Tolerance may be due to

A

1) masking or internalization of the receptors
2) loss of receptors (down regulation)- decreased synthesis increased destruction
3) exhaustion of mediators( depletion of catecholamine)

125
Q

Examples of competitive antagonism

A

Acetylcholine and atropine
Morphine and naloxone

126
Q

Examples of non competitive antagonists

A

Diazepam and bicuculline

127
Q

Examples of ion channel physiological Ligands

A

Acetylcholine(M2), GABA

128
Q

Example of ion channel ligand gated drugs

A

Nicotine, gabapentin

129
Q

Example of ion channel voltage gated drugs

A

Lidocaine and verapamil

130
Q

List the functional families of GPCR

A

Beta adrenergic receptors
Muscarinic cholinergic receptors
Eicosanoid receptors

131
Q

Example of GPCR beta adrenergic receptor drugs

A

Dobutamine

132
Q

Example of GPCR muscarinic cholinergic receptor drugs

A

Atropine

133
Q

Example of GPCR eicosanoid receptor drugs

A

Misoprostol
Monteluskat

Pharmacology (7 decks)

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