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Pharmacology > Mechanisms of drug action > Flashcards

Mechanisms of drug action Flashcards

1
Q

The penicillin molecule binds to a bacterial enzyme and prevents ‘cross links’ in the bacterial cell wall

A

Transpeptidase

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2
Q

Drugs always only alter the pace of ongoing activity T/F

A

F
They do except those gene based

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3
Q

Types of Drug action

A

Stimulation
Depression
Irritation
Replacement
Cytotoxic action

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4
Q

Examples of stimulators drugs

A

Adrenaline on heart
Pilocarpine of salivary glands

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5
Q

Examples of drugs that undergo selective diminution of activity of specialized cells

A

Barbiturates on CNS
Quinidine on the heart
Omeprazole on gastric secretion

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6
Q

lrritation is applied to specialized cells

A

F
Irritation is applied to non specialized cells

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7
Q

Drugs that cause irritation

A

Bitters on salivary and gastric secretion

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8
Q

Replacement drugs

A

Levodopa in Parkinson’s disease
Insulin in DM

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9
Q

Drugs that cause cytotoxic action on invading organisms

A

Cyclophosphamide
Zidovudine
Penicillin

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10
Q

Mechanisms of drug action

A

Physical
Chemical

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11
Q

Physical mechanism of drug action examples

A

Activated charcoal binds with poisons
Mannitol as osmotic diuretic
Bulk laxatives e.g ispaghula

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12
Q

Drugs that act by producing chemical reactions in the body

A
  1. Antacid - NaHCO3
  2. Chelating agents - Dimercaprol, penicillamine, desferrioxamine
  3. AChE Reactivator - Pralidoxime
  4. Sequestration - Cholestyramine
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13
Q

Target biomolecules of drugs

A
  1. Enzymes
    2, Carrier molecules
  2. Ion channels
  3. Receptors
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14
Q

Examples of competitive inhibitors of enzymes

A
  1. ACE inhibitors - Captopril
  2. Reversible antiChE - Neostigmine, Physostigmine
  3. Xanthine oxidase inhibitor - Allopurinol (used in gout)
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15
Q

Non-competitive inhibition

A
  1. Irreversible AntiChE - Organophosphorous compounds
  2. Aspirin
  3. Imipramine
  4. Omeprazole
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16
Q

Aspirin inhibits what enzyme and therefore prostaglandin synthesis

A

Cyclooxygenase enzyme

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17
Q

Imipramine is a MOA inhibitor used to treat

A

Depression

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18
Q

Omeprazole is an electron pump inhibitor

A

F
Proton pump inhibitor

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19
Q

Omeprazole inhibits the H+/K+ ATPase in

A

parietal cells of the stomach

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20
Q

Na channel drugs

A

Quinidine
Procainamide

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21
Q

Sodium channel drugs block the sodium channels thus, depolarization does NOT take place T/F

A

T
No nerve conduction

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22
Q

Quinidine as a sodium channel drug is used in

A

Cardiac Arrhythmias

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23
Q

Procainamide as a sodium channel drug is used as

A

Local Anaesthetic

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24
Q

Drugs that block block the voltage gated Calcium channels

A

Nifedipine
Verapamil
Diltiazem

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25
Q

Calcium channel blockers are useful in

A

Hypertension
Arrhythmias

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26
Q

Potassium channel blockers

A

Amiodarone
Sulfonylureas

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27
Q

Amiodarone is used in

A

Arrhythmias

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28
Q

Blockade of Potassium channels leads to

A

A prolonged refractory period

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29
Q

Chloride channel drug

A

Benzodiazepines

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30
Q

Benzodiazepines act on which receptors

A

GABA A receptors

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31
Q

Benzodiazepines lead to HYPERpolarization of the neuron, which inhibits neurotransmission and action potential T:F

A

T

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32
Q

Carrier molecules or transporters are ………………… by certain drugs

A

Inhibited

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33
Q

Inhibition of choline carrier by

A

Hemicholinium

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34
Q

Reserpine inhibits

A

Noradrenaline vesicular uptake

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35
Q

NEURONAL uptake of noradrenaline is inhibited by

A

Desipramine

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36
Q

Fluoxetine inhibits the neuronal uptake of

A

Serotonin

37
Q

What drug inhibits uric acid carrier

A

Probenecid
(Thus enhancing the excretion of uric acid)

38
Q

Examples of antagonists

A

Atropine, Scopolamine, Phenoxybenzamine

39
Q

Example of inverse agonist

A

Beta carbolines

40
Q

Two essential functions of receptors

A

Recognition and Transduction

41
Q

Criteria for classifying receptors

A
  1. Pharmacological - Muscarinic, Nicotinic
  2. Tissue distribution - Beta 1, Beta 2
  3. Ligand binding - 5-HT
  4. Transducer pathway - G-proteins, Na+ channels
  5. Molecular cloning
42
Q

What type of receptors are plasma proteins

A

Silent receptors (Drug acceptors or Sites of loss)

43
Q

Receptor related diseases

A
  1. Myasthenia gravis (autoimmune diseases directed at receptor proteins)
  2. Mutations of genes encoding GCPRs - Hypoparathyrodism, cancers
  3. Thyroid hypersecretion - Autoantibodies mimic agonists
  4. Insulin resistant diabetes
  5. Testicular feminization
  6. Familial Hypercholesterolaemia
44
Q

Categories of transducer mechanisms

A
  1. GPCR
  2. Receptors with intrinsic ion channel
  3. Enzyme linked receptors
  4. Transcription factors
45
Q

Structure of GCPRs

A

7 alpha helical hydrophobic amino acid segments (3 extra,3 intracellular loops)

46
Q

Ion channel types

A

Ligand gated
Voltage gated

47
Q

Receptors can be divided into 4 groups

A
  1. Ionotropic
  2. GPCR
    3.,Receptor tyrosine kinase
  3. Intracellular hormone receptor
48
Q

Ionotropic receptors are confined to

A

Excitable tissues - CNS, NMJ, autonomic ganglia

49
Q

What regulates actin cytoskeletal remodeling during movement and migration

A

G12/13

50
Q

The three second messenger systems

A
  1. cAMP
  2. cGMP
  3. Ca and Phosphoinositol second messenger system
51
Q

What channel does Go affect and how ?

A

Ca2+ channels, inhibits

52
Q

Substrates of Go

A

K+ channel in heart

53
Q

Gq substrates

A

M1,M3,Alpha 1, H1

54
Q

Gi substrates

A

M2,M4,Alpha 2, D2

55
Q

Gs substrates

A

B1,B2,H2,D1

56
Q

Gi leads to the opening of what channel

A

K+

57
Q

Gs leads to the opening of what channel

A

Ca2+

58
Q

Go stimulates/inhibits Ca2+ channels

A

inhibits

59
Q

GABA B coupler

A

Gi,Go

60
Q

5-HT1 coupler

A

Gi

61
Q

5-HT2 coupler

A

Gq

62
Q

Dopamine, D2 coupler

A

Gi

63
Q

H2 coupler

A

Gs

64
Q

PKa functions in

A
  1. Cardiac contractility through troponin
  2. Muscle relaxation through phospholambin and Ca2+
65
Q

Adenyl Cyclase-cAMP Pathway leads to

A
  1. Increased contractility
  2. Smooth muscle relaxation
  3. Glycogenolysis
  4. Lipolysis
  5. Inhibition of secretion
  6. Hormone secretion
66
Q

cAMP activity is terminated by

A

Phosphodiesterases

67
Q

Phosphodiesterases hydrolyse cAMP to

A

5-AMP

68
Q

IP3 acts on IP3 receptors found where to elicit what

A

Smooth ER; Ca2+ release

69
Q

DAG diffuses along the plasma membrane to activate

A

pkC

70
Q

One bound agonist molecule can activate several G proteins

A

T

71
Q

To form resting G protein, GTP is hydrolysis to GDP by

A

GTPase activity of alpha subunit

72
Q

Metab, growth and differentiation are controlled by what type of receptors

A

Enzyme-linked receptors

73
Q

Main targets of intracellular receptors are

A

Transcription factors

74
Q

cAMP dependent protein kinase is

A

Protein kinase A

75
Q

Triggered by IP3, Ca2+ acts through what substances to produce effects

A

Calmodulin, PKC

76
Q

3rd Messenger of IP3-DAG pathway

A

Ca2+

77
Q

3 Major pathways of GCPR

A
  1. cAMP pathway
  2. IP3-pathway
  3. Channel regulation
78
Q

Results of IP3-DAG pathway

A
  1. Mediates Contaction
  2. Secretion Release
  3. Neuronal excitability
  4. Intracellular movements
  5. Eicosanoid synthesis
  6. Cell proliferation
79
Q

Activated G proteins can open or close ion channels without the intervention of cAMP or IP/DAG

A

T

80
Q

Which receptor(s) open K+ channels in heart and muscle and close Ca+ channels in neurons

A

Go,Gi

81
Q

ACh opens what channels causing depolarization at ganglia and adrenal medulla

A

Na+ channels

82
Q

Receptor theories

A
  1. Occupancy theory
  2. Rate theory
  3. Stephenson’s theory
  4. Ariens’ theory
  5. The induced-fit theory
  6. Macromolecular perturbation theory
83
Q

Maximal response occurs when all receptors are occupied

A

Occupancy Theory

84
Q

Response is proportional to rate of Drug-receptor complex dissociation

A

Rate theory

85
Q

Response is proportional to the fraction of occupied receptors and the intrinsic activity

A

Stephenson’s

86
Q

Ariens’ theory

A

Response is a function of affinity, maximum response can be produced with full receptor occupancy

87
Q

What theory nullifies the lock and key concept

A

Induced fit

88
Q

Macromolecular perturbation theory

A

One of two occurs
Specific conformational - response
Non-conformational - no response

Pharmacology (11 decks)

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