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Pharmacology Flashcards

1
Q

What is an opioid?

A

Endogenous or synthetic substance that produces morphine life effects

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2
Q

What are the main groups of synthetic analogues of opiods?

A
  1. Piperidines
  2. Methadone-like drugs
  3. Benzomorphans
  4. Thebaine derivatives
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3
Q

Which receptors are responsible for most of the analgesic effects of opioids?

A

mu

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4
Q

All types of opioid receptors are what type of receptors?

A

Gi/Go proteins

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5
Q

Describe the effects of morphine

A
  1. Analgesia
  2. Euphoria and sedation
  3. Respiratory depression and suppression of cough
  4. Nausea/vomiting
  5. Pupillary construction
  6. Reduced GI motility
  7. Histamine release causing bronchoconstriction
  8. Hypotension
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6
Q

Which opioid cause physical dependance?

A

u-receptor agonists

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7
Q

What may relieve withdrawal symptoms?

A

Long acting u-receptor agonists such as methadone and buprenorphine

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8
Q

Which opioids are less likely to cause dependance?

A

codeine, pentazocine, buprenorphine and tramdol

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9
Q

Define pain

A

Unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage

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10
Q

What are the main pain receptors?

A

Polymodal nociceptors

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11
Q

Name some chemical stimuli of pain receptors

A

Bradykinin, protons, ATP and vanilloids

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12
Q

Describe the fibres of pain pathways

A

Mostly non-myelinated C fibres whose endings respond to thermal, mechanical and chemical stimuli

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13
Q

Through where do nociceptive neutrons run and where are their cell bodies?

A

Peripheral sensory nerves

Their cell bodies lie in the dorsal root ganglia or peripheral nerves just inside the spine

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14
Q

Describe the myelination of nociceptive neurones

A

Lightly or non-myelinated

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15
Q

Where do C fibres and some Aδ fibres terminate?

A

Laminae I and II (aka the substantia gelatinosa)

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16
Q

What does the substantial gelatinosa contain a lot of?

A

Endogenous opioid receptors

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17
Q

What neurotransmitters do the nociceptive afferent neurons release when they synapse in the dorsal horn?

A

Glutamate, substance P and ATP

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18
Q

Where do pain signals travel up the spinal cord?

A

Contralateral white matter called the spinothalamic tract

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19
Q

Describe some processes involved in modulation of pain transmission

A

Periaqueductal grey, endogenous opioid peptides

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20
Q

Name the 3 types of endogenous opioid peptides

A
  1. Enkephalins
  2. Endorphins
  3. Dynorphins
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21
Q

What is the gate control theory of pain?

A

Non-painful input closes the ‘gates’ to painful input, which prevents pain sensation from travelling to the CNS. Therefore, stimulation by non-noxious input is able to suppress pain

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22
Q

Name the different types of opioid receptors

A

Delta, mu, kappa receptors

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23
Q

What are the 2 types of cholinergic receptors?

A

Nicotinic nAChR and muscarinic mAChR subtypes

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24
Q

Describe the nAChr and where it is found

A

Directly coupled to caption channels and mediate fast excitatory synaptic transmission at the neuromuscular junction, autonomic ganglia and various sites in the CNS

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25
Describe the mAChR and where they are found
1. mAChRs are typical GPCRs with 5 molecular subtypes (M1-M5) 2. M1,3&5 couple with Gq to activate the inositol pathway 3. M2/4 act through Gi to inhibit adenylate cyclase and reduce cAMP 4. mAChRs mediate acetylcholine effects at postganglioic parasympathetic synapses
26
Where are the different muscarinic receptors found?
M1 - neural M2 - cardiac M3 - glandular/smooth muscle M4/5 - mostly CNS
27
Choline is acetylated to form ACh by which enzyme?
Choline acetyl transferase
28
What is the source of acetyl groups?
Acetyl-coenzyme A
29
How is Ach released from the vesicles into the synaptic space when an AP arrives at the pre-synaptic neuron?
Ca2+ mediated exocytosis
30
What type of receptors are found at the neuromuscular junction?
Nicotinic
31
How does a presynaptic action potential produce only 1 postsynaptic action potential?
ACh is hydrolysed within about 1ms by acetylcholinesterase
32
Name some muscarinic agonists and their uses
1. Acetylcholine carbachol 2. Methacholine 3. Muscarine and pilocarpine 4. Mainly used for glaucoma
33
Name some muscarinic antagonists and their uses
1. Atropine 2. Hyoscine 3. Ipratropium and pirenzepine 4. Sinus bradycardia 5. Prevention of motion sickness 6. Asthma or COPD
34
Name some nicotinic agonists and their uses
1. Nicotine 2. Carbachol 3. No real therapeutic use except for aiding stopping cigarette smoking 4. NB succinylcholine is an agonist although behaves like an antagonist
35
Name some nicotinic antagonists and their uses
1. Hexamethonium 2. Tubocurarine 3. Treat hypertension 4. Relax skeletal muscles during surgery
36
Name a non-depolarising neuromuscular-blocking agent
1. Tubocurarine 2. Pancuronium 3. Atracurium
37
Name a depolarising neuromuscular blocking agent
Suxamethonium
38
What are 2 main forms of cholinesterase?
1. Acetylcholinesterase AChE | 2. Butyrylcholinesterase BuChE
39
Give 2 examples of cholinesterase inhibitors
1. Neostigmine | 2. Physosyigmine
40
Describe the symptoms you would get in a cholinergic crisis
Diarrhoea, urination, muscle weakness, bradycardia, bronchorrhoea, emesis, lacrimation, salivating/sweating
41
Describe the symptoms you would get in an anticholinergic crisis
High body temperature, mydriasis, dry mouth, dry eyes, decreased sweat, flushed, delirium
42
How does a presynaptic action potential produce only one postsynaptic action potential?
ACh is hydrolysed within about 1ms by acetylcholinesterase
43
Define pharmacokinetics
What the body does to the drug
44
How do rugs cross lipid membranes?
1. Passive diffusional transfer | 2. Carrier mediated transfer
45
What does ADME stand for?
Absorption, Distribution, Metabolism, Excretion
46
What determines the rate of passive diffusional transfer of a drug across membranes?
Lipid solubility
47
What kind of drugs does albumin bind?
Mainly acidic drugs
48
Describe some factors absorption of a drug from the gut depends on
Gastrointestinal motility, gastrointestinal pH, particle size, physiochemical interaction with gut contents
49
Define bioavailability
Fraction of an ingested dose of a drug that gains access to the systemic circulation
50
Why might bioavailability be low?
Absorption is incomplete, or because the drug is metabolised in the gut wall over liver before reaching the systemic circulation
51
In drug metabolism, what does phase 2 involve?
Oxidation, reduction and hydrolysis
52
In drug metabolism, what does phase 2 involve?
Conjugation of a reactive group
53
Can drugs cross the filtration barrier at the glomerulus of the kidney?
Yes, unless highly bound to plasma proteins
54
Which drugs aren't efficiently excreted in the urine and why?
Lipid soluble drugs are passively reabsorbed by diffusion
55
Which drugs are actively secreted into the renal tubule and thus more rapidly excreted?
Weak acids and bases
56
What fundamental parameter describes the elimination of a drug?
Total clearance
57
How is rate of elimination worked out?
Total clearance multiples by the plasma concentration
58
What are the 3 main stages of drug development?
1. Drug discovery 2. Preclinical development 3. Clinical development
59
What processes are involved in the drug discovery part of drug development?
Candidate molecules are chosen on the basis of their pharmacological properties
60
What processes are involved in the preclinical development part of drug development?
Wide range of non-human studies (eg toxicity testing, pharmacokinetic analysis and formulation)
61
What processes are involved in the clinical development part of drug development?
The selected compound is tested for efficacy, side effects and potential dangers in volunteers and patients
62
What happens during lead finding?
High throughput screening using assays or in silico (computer prediction models) - end up with around 100 potential candidates
63
What happens during lead optimization?
Candidates are tested on wider range of assays to determine things like selectivity and metabolic stability - identifies one or more candidates for further development
64
What are the 4 main parts to pre-clinical development?
1. Safety pharmacology (test the drug doesn’t cause arrhythmias, ataxia, bronchoconstriction) 2. Toxicology (finding out lethal dose, post-mortems of animals to look at histology) 3. Pharmacokinetic testing (ADME) 4. Chemical development - can the drug me made on a large scale?
65
What are the stages of clincal development?
Phase 1 - small group (20-80) healthy volunteers to check things like tolerability, dangerous effects, pharmacokinetic properties etc Phase 2 - 100-300 patients to test for efficacy and establish dose Phase 3 - double-blind RCT on thousands of patients to compare new drug with already available ones Phase 4: Post-marketing surveillance to monitor long-term use

Phase 2a (3 decks)

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