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Clinical Life Sciences 2 > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

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1
Q

What are the four main locations that drugs act on?

A
  1. Receptors
  2. On DNA
  3. Enzymes
  4. Membranes
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2
Q

What drugs stimulate receptors?

A

Agonists

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3
Q

What drugs prevent receptor stimulation?

A

Antagonists

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4
Q

What do receptors do?

A

They initiate cellular responses

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5
Q

What are receptors?

A

Proteins in or on cells?

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6
Q

What are the four main types of proteins that receptors are linked to?

A
  1. G-protein coupled receptors
  2. Ion channels
  3. Gene transcription
  4. Enzymes
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7
Q

Name a Beta2 adrenoceptor agonist

A

Salbutamol

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8
Q

Name a Beta2 receptor antagonist

A

Propanol

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9
Q

Name a H1+2 receptor agonist

A

Histamine

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10
Q

Name an opiate Mu receptor agonist

A

Morphine

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11
Q

Name an opiate Mu receptor antagonist

A

Naloxone

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12
Q

Name a M2 muscarinic agonist

A

Acetylcholine

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13
Q

Name a M2 muscarinic antagonist

A

Atropine

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14
Q

How do G protein coupled receptors interact with ion channels?

A

They cause confirmation changes which allow ion exchange

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15
Q

How to G protein coupled receptors affect enzymes?

A

They activate or inhibit enzymes which will result in second messengers being produced or inhibited

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16
Q

What are the two types of opioid analgesics?

A

1 - Morphine based

2 - Synthetic

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17
Q

What are the three main opioid receptors?

A

Delta, Kappa and Mu

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18
Q

What type of receptors do opioids act on?

A

G-Protein Coupled Receptors

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19
Q

What occurs after receptor binding of opioids?

A
  1. Inhibition of adenylate cyclise -> decreased intracellular cAMP
  2. Couple to K:Ca ion channels -> inhibition of transmitter release and postsynapse excitability
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20
Q

75% of presynapse receptors for opioids are….?

A

Mu receptors

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21
Q

By what 3 means do opioid analgesics work?

A
  1. Inhibits pain transmission in dorsal horn
  2. Activates descending pathways in grey matter inhibiting pain transmission (reduced GABA)
  3. Inhibits nociceptive afferents in tissues
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22
Q

How is pain transmission inhibited at the dorsal horn?

A

By inhibiting presynaptic afferent impulses

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23
Q

How are the descending pathways activated?

A

By inhibiting GABA release in periaqueductual grey matter (PAG)

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24
Q

Why does activating the descending pathways inhibit pain?

A

It inhibits the discharge of the Dorsal Horn

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25
What does the dorsal horn project into?
The Thalamus
26
What does the thalamus project in to?
The Cortex
27
Why does respiratory depression occur when morphine is administered?
The activation of Mu receptors reduce the respiratory centres sensitivity to CO2
28
Why can nausea and vomiting occur when morphines administered?
Activation of the chemoreceptors trigger zone
29
Why can pupillary constriction occur when morphine is administered?
Activation of the kappa receptors leads to the stimulation of the oculomotor nucleus (parasympathetic NS)
30
Why is it important to be cautious when administering morphine to someone with asthma?
It can cause histamine release leading to bronchospasm and hypotension
31
What does tissue damage lead to the production of? Causing activation of nociceptive fibres?
Bradykinins ATP H ions Prostaglandins
32
What non analgesic effects to kappa opiod receptors have on the body? (3)
Decreased RR Pupil miosis Sedation
33
What non analgesic effects to mu opiod receptors have on the body? (2)
``` Resp depression (resp centre - medulla oblongata) Euphoria ```
34
What is histamine?
An inflammatory mediator
35
What does IgE production in an allergic reaction lead to?
Mast cell degranulation and histamine release
36
What are the main effects of H1 receptors? (3)
Vasodilation Increased cap permeability Bronchospasm
37
What are the main effects of H2 receptors? (4)
CNS effects Gastric acid production Smooth muscle relaxation T cell and Cytokine proliferation
38
What actions does chloraphenamine have? (4)
Anti-allergic Sedative Anti-muscarinic Anti-emetic
39
What is chloraphenamine?
A potent H1 antihistamine
40
What are the main two things chloraphenamine reduces?
Urticaria and Bronchoconstriction
41
What are receptors that regulate gene transcription called?
Nuclear receptors
42
Where are nuclear receptors located?
The cytosol
43
Name some glucocorticoids (4)
Oestrogen Progesterone Steroid hormones Thyroid hormones
44
How are inflammatory mediators produced by glucocorticoids
Glucocorticoid > nuclear receptor > conformation change > binds to DNA > gene expression (transcription, translation and mRNA synthesis > production and release of inflammatory mediators
45
What are enzymes?
Proteins that catalyse chemical reactions in the body
46
True or False enzymes have specific binding sites for substrates?
True
47
What is aspirin?
An enzyme inhibitor
48
How does aspirin work?
Irreversibly inactivates COX
49
What does inactivation of COX by aspirin lead to?
Reduction in prostaglandin and thromboxane production
50
Do most other NSAIDs and COXIBs bind irreversibly or reversibly?
Reversibly
51
Low doses of aspirin irreversibly block TXA2 formation in platelets... what effect does this have?
It has an antithrombotic effect and helps reduce heart attack risk
52
What drugs act on non mammalian cell targets? (4)
Anti-virals Anti-biotics Anti-parasitics Anti-fungals
53
What class of antibiotic is penicillin?
A beta-lactam antibiotic (bacteriocidal)
54
What do bacteriocidal antibiotics do?
Lead to cell lysis and death
55
What does penicillin bind to?
Penicillin binding protein (DD-transpeptidase)
56
What does pencillin binding to a bacterium result in?
Inability to cross link peptidoglycan in cell wall which leads to cell wall degredation, cell lysis and death
57
Why does penicillin usually have minimal side effects?
As it acts on bacterial proteins (little effect on host) - selective toxicity
58
What does the ABCDE of adverse drug reactions (ADR) stand for?
``` Augmented Bizzare Chronic Delayed End of Use ```
59
Name an augmented ADR
Decreased RR with morphin (predictable, common, dose dependent)
60
Name a bizzare ADR
Anaphylaxis (unpredictable, uncommon, cure=stop use)
61
Name a chronic ADR
Growth retardation with corticosteroid therapy
62
Name a delayed ADR
Teratogenic drugs (thalidomide)
63
Name an end of use ADR
Withdrawal from benzodiazipines
64
How does paracetamol act?
Selectively inhbits COX and weakly inhibits prostaglandins
65
What are the parasympathetic spinal cord outputs?
Craniosacral
66
What are the sympathetic spinal cord outputs?
Thoracolumbar
67
What the two main alpha receptor agonists?
Adrenaline and Noradrenaline
68
What 3 main effects does beta1 receptor stimulation have on the heart?
changes... Rate Force Contractility
69
What effect does beta2 receptor stimulation have on the lungs?
Smooth muscle dilation
70
How does ipatropium bromide function?
It 'deactivates' parasympathetic influence stopping bronchial smooth muscle contraction
71
What kind of antagonist is ipatropium bromide?
A cholinergic antagonist
72
What do pumps and carriers on cell membranes allow?
A cell to regulate it's internal environment
73
List some drugs that act on pumps and carriers
- Diuretics - Digoxin - Anaesthetics
74
What are voltage-operated channels?
Channels in a cell membrane that are activated by electrical membrance changes
75
How does tetracaine work?
It blocks sodium channels
76
True or False sodium must ionise and enter the intracellular axon to function?
True
77
What are chelating agents?
Chemical compounds that react with metal ions to form a stable water soluble complex

Clinical Life Sciences 2 (7 decks)

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