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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
Calcium channel blockers are useful in
Hypertension Arrhythmias
26
Potassium channel blockers
Amiodarone Sulfonylureas
27
Amiodarone is used in
Arrhythmias
28
Blockade of Potassium channels leads to
A prolonged refractory period
29
Chloride channel drug
Benzodiazepines
30
Benzodiazepines act on which receptors
GABA A receptors
31
Benzodiazepines lead to HYPERpolarization of the neuron, which inhibits neurotransmission and action potential T:F
T
32
Carrier molecules or transporters are ………………… by certain drugs
Inhibited
33
Inhibition of choline carrier by
Hemicholinium
34
Reserpine inhibits
Noradrenaline vesicular uptake
35
NEURONAL uptake of noradrenaline is inhibited by
Desipramine
36
Fluoxetine inhibits the neuronal uptake of
Serotonin
37
What drug inhibits uric acid carrier
Probenecid (Thus enhancing the excretion of uric acid)
38
Examples of antagonists
Atropine, Scopolamine, Phenoxybenzamine
39
Example of inverse agonist
Beta carbolines
40
Two essential functions of receptors
Recognition and Transduction
41
Criteria for classifying receptors
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
What type of receptors are plasma proteins
Silent receptors (Drug acceptors or Sites of loss)
43
Receptor related diseases
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
Categories of transducer mechanisms
1. GPCR 2. Receptors with intrinsic ion channel 3. Enzyme linked receptors 4. Transcription factors
45
Structure of GCPRs
7 alpha helical hydrophobic amino acid segments (3 extra,3 intracellular loops)
46
Ion channel types
Ligand gated Voltage gated
47
Receptors can be divided into 4 groups
1. Ionotropic 2. GPCR 3.,Receptor tyrosine kinase 4. Intracellular hormone receptor
48
Ionotropic receptors are confined to
Excitable tissues - CNS, NMJ, autonomic ganglia
49
What regulates actin cytoskeletal remodeling during movement and migration
G12/13
50
The three second messenger systems
1. cAMP 2. cGMP 3. Ca and Phosphoinositol second messenger system
51
What channel does Go affect and how ?
Ca2+ channels, inhibits
52
Substrates of Go
K+ channel in heart
53
Gq substrates
M1,M3,Alpha 1, H1
54
Gi substrates
M2,M4,Alpha 2, D2
55
Gs substrates
B1,B2,H2,D1
56
Gi leads to the opening of what channel
K+
57
Gs leads to the opening of what channel
Ca2+
58
Go stimulates/inhibits Ca2+ channels
inhibits
59
GABA B coupler
Gi,Go
60
5-HT1 coupler
Gi
61
5-HT2 coupler
Gq
62
Dopamine, D2 coupler
Gi
63
H2 coupler
Gs
64
PKa functions in
1. Cardiac contractility through troponin 2. Muscle relaxation through phospholambin and Ca2+
65
Adenyl Cyclase-cAMP Pathway leads to
1. Increased contractility 2. Smooth muscle relaxation 3. Glycogenolysis 4. Lipolysis 5. Inhibition of secretion 6. Hormone secretion
66
cAMP activity is terminated by
Phosphodiesterases
67
Phosphodiesterases hydrolyse cAMP to
5-AMP
68
IP3 acts on IP3 receptors found where to elicit what
Smooth ER; Ca2+ release
69
DAG diffuses along the plasma membrane to activate
pkC
70
One bound agonist molecule can activate several G proteins
T
71
To form resting G protein, GTP is hydrolysis to GDP by
GTPase activity of alpha subunit
72
Metab, growth and differentiation are controlled by what type of receptors
Enzyme-linked receptors
73
Main targets of intracellular receptors are
Transcription factors
74
cAMP dependent protein kinase is
Protein kinase A
75
Triggered by IP3, Ca2+ acts through what substances to produce effects
Calmodulin, PKC
76
3rd Messenger of IP3-DAG pathway
Ca2+
77
3 Major pathways of GCPR
1. cAMP pathway 2. IP3-pathway 3. Channel regulation
78
Results of IP3-DAG pathway
1. Mediates Contaction 2. Secretion Release 3. Neuronal excitability 4. Intracellular movements 5. Eicosanoid synthesis 6. Cell proliferation
79
Activated G proteins can open or close ion channels without the intervention of cAMP or IP/DAG
T
80
Which receptor(s) open K+ channels in heart and muscle and close Ca+ channels in neurons
Go,Gi
81
ACh opens what channels causing depolarization at ganglia and adrenal medulla
Na+ channels
82
Receptor theories
1. Occupancy theory 2. Rate theory 3. Stephenson’s theory 4. Ariens’ theory 5. The induced-fit theory 6. Macromolecular perturbation theory
83
Maximal response occurs when all receptors are occupied
Occupancy Theory
84
Response is proportional to rate of Drug-receptor complex dissociation
Rate theory
85
Response is proportional to the fraction of occupied receptors and the intrinsic activity
Stephenson’s
86
Ariens’ theory
Response is a function of affinity, maximum response can be produced with full receptor occupancy
87
What theory nullifies the lock and key concept
Induced fit
88
Macromolecular perturbation theory
One of two occurs Specific conformational - response Non-conformational - no response

Pharmacology (11 decks)

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