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Year 2 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is the clinical aim of pharmcokinetics?

A

To achieve effective drug concentration at site

of action long enough to produce a therapeutic action

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2
Q

What is bioavailability?

A

The proportion of dose of a drug that reaches the site of action

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3
Q

Where is the main site of drug absorption?

A

The small intestine

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4
Q

What is the rate of absorption dependent on?

A

Gut motility

Splanchnic blood flow

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5
Q

Give four characteristics of phase 1 of drug metabolism:

A

Transforms molecular structure of the drug (oxidation, hydrolysis, reduction etc)
Can Introduce polar group/Increase water solubility
Can abolish activity
Can produce toxic or non-toxic metabolites

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6
Q

Describe the second phase of drug metabolism:

A

Transferases attatch an endogenous substance to parent drug or phase 1 metabolite
Increases polarity/water solubility so the metabolites can be eliminated

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7
Q

What is the major route of drug excretion?

A

Renal

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8
Q

What is clearance?

A

The virtual volume of blood cleared of drug per unit time

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9
Q

What are receptors?

A

Proteins inserted into the membrane which bind neurotransmitters, hormones etc and produce a cellular response

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10
Q

What are the four main types of receptors?

A

Ligand gated ion channels
G-protein coupled receptors
Kinase-linked receptors
Receptors linked to gene transcription

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11
Q

What is affinity?

A

How well a drug binds to the receptor

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12
Q

What is efficacy?

A

The measure of response produced by bound drug

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13
Q

What is potency?

A

A combination of affinity and efficacy

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14
Q

What is an agonist?

A

A substance which initiates a physiological response when combined with a receptor.

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15
Q

What are clinical uses of partial agonists?

A

Reduce over-activity but do not block basal activity

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16
Q

What are the three main neurophysiological changes resulting from anaesthesia?

A

Unconsciousness
Analgesia
Loss of reflexes

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17
Q

What is the lipid theory of how anaesthetics work?

A

GA agents dissolve in membrane leading to:
changes in bilayer thickness
changes in order parameters
changes in curvature elasticity

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18
Q

What are the two major problems with the lipid theory?

A

Stereoisomers

Cut off effect of carbon chain length

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19
Q

What are the three main receptors implicated with the anaesthetic protein theory?

A 
GABA receptor (inhibitory)
2 pore K+ channels (control resting potential)
NMDA receptor (excitatory)
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20
Q

Greater solubility in blood of inhaled GA agents leads to what?

A

Slower rate of anaesthesia onset

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21
Q

Give five characteristics of propofol:

A 
Intravenous anaesthetic
Potentiates GABAA receptor responses
Rapidly metabolized in the liver.
Distributes in fatty tissues: high lipophilicity. 
Used as an induction agent.
22
Q

Give four characteristics of thiopental:

A

Intravenous anaesthetic
Barbiturate used to induce anaesthesia.
Potentiates GABAA receptors
Highly lipid soluble

23
Q

Why is halothane no longer widely used in clinical situations?

A

It’s associated with severe hepatotoxicity

24
Q

Which inhaled GA agent is widely used in surgery?

A

Isoflurane

25
Q

In which clinical situation is nitrous oxide generally used?

A

Obstetrics

26
Q

What are the two pain pathways?

A

Peripheral nociceptive afferent neurons activated by noxious stimuli
Central mechanisms by which the afferent input generates a pain sensation

27
Q

What are the two types of pain?

A 
Fast pain (Adelta fibres)
Slower pain (C fibres)
28
Q

Name two non-steroidal anti-inflammatory drugs:

A

Aspirin, ibuprofen

29
Q

What is an opiate?

A

Drugs derived from the opium poppy

30
Q

What is an opioid?

A

Opiates and synthetic opiate substances

31
Q

What are the main CNS effects of Opioids?

A

Profound analgesia
Respiratory depression
Nausea and vomiting

32
Q

Which are the endogenous ligands for opioid receptors?

A

Endorphins and enkephalins

33
Q

What is the main opioid receptor antagonist?

A

Naloxone

34
Q

What makes up the peripheral nervous system?

A

All nerves outside the brain and spinal cord

35
Q

What are the five different steps of neurotransmitter release?

A 
Synthesis
Storage
Release
Activation
Inactivation
36
Q

Which neurones are noradrenaline released from and which is the exception from this?

A 
Postganglionic neurone
Sweat glands (release acetylcholine)
37
Q

Which are the two classes of cholinoceptor that occur the PNS?

A

Nictotinic cholinoceptors

Muscarinic cholinoceptors

38
Q

Which are the two classes of adrenoceptors that occur in the PNS?

A

Alpha-adrenoceptors

Beta-adrenoceptors

39
Q

What type of receptors are nicotinic cholinoceptors?

A

Ligand-gated ion channels

40
Q

What type of receptors are muscarinic cholinoceptors and all subtypes of adrenoceptors?

A

G-protein-coupled receptors

41
Q

What does hemicholinium 3 do?

A

It competitively block the reuptake of choline

42
Q

What does choline acetyltransferase do?

A

It synthesises ACh from precursors choline and acetyl coenzyme A

43
Q

Which drug inhibits uptake and storage of synaptic vesicles?

A

Vesamicol

44
Q

What does tetrodotoxin do?

A

It blocks voltage gated sodium channels

45
Q

What do conatoxins do?

A

They block P/Q and N-type voltage gated calcium channels

46
Q

What does botulinum toxin do?

A

It blocks vesicle fusion

47
Q

What do dendrotoxins do?

A

They block voltage gated potassium channels (More calcium influx- more release)

48
Q

What does ziconotide do, and where does it come from?

A

It acts as a selective N-type voltage-gated calcium channel blocker. It comes from cone snails

49
Q

Which enzyme terminates activation of nicotinic ACh receptors at the NMJ?

A

Acetylcholinesterase

50
Q

What is tubocurarine and what are its two clinical alternatives?

A

It’s a competitive non-depolarising blocker. The alternatives that are actually clinically used are vecuronium and rocuronium

51
Q

What does suxamethonium do?

A

It’s a depolarising blocker which produces the rapid onset of paralysis

Year 2 (5 decks)

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