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CHEM358 Pharmacology > Anaesthetics > Flashcards

Anaesthetics Flashcards

1
Q

general anasthesia is given ??? and exerts main effects on the CNS

A

systemically

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2
Q

Local and Regional Anaesthesia block the conduction of impulses in ??? nerves

A

peripheral sensory

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3
Q

Stage one of general anaesthetics is ??? when you’re still conscious

A

Analgesia/Amnesia

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4
Q

STAGE II is ??? but it is avoided by a short‐acting IV anaesthetic before
inhalation anaesthetics

A

Excitement

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5
Q

what occurs at Stage II of general anaesthetics?

A

Loss of consciousness but responsive to painful stimuli; may move, have incoherent speech, vomiting, and irregular breath

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6
Q

STAGE III General anaesthesia is ??? where reflexes disappear. Respiration initially more regular but depression develops with increasing depth of anaesthesia; muscle relaxation

A

Surgical anaesthesia

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7
Q

STAGE IV ??? respiratory arrest and cardiovascular collapse; death

A

Medullary Depression

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8
Q

??? i.e. diazepam, fentanyl
‐ Relieve anxiety
‐ Produce sedation & amnesia
‐ Relieve pain
‐ Reduce secretions
‐ Reduce post operative‐nausea & vomiting
‐ Reduce volume & acidity of gastric contents
‐ Modify the automatic response
‐ Reduce pain during venipuncture

A

pre-medication

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9
Q

Premedication Agents are Benzodiazepines such as diazepam, Lorazepam, Midazolam. These are taken as oral or IV, and are for ???

A

For sedation & to decrease anxiety
Anxiolytic, amnesic and hypnotic

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10
Q

Benzodiazepines mechanism of action is: enhance ??? mediated inhibition in CNS

A

GABA

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11
Q

??? is the second phase of general anaesthesia procedure. It is defined as the period of time from onset of administration to the
development of effective surgical anaesthesia in the patients

A

Induction

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12
Q

TRUE or FALSE: Intravenous anaesthetics act more rapidly than inhalation as even the fastest‐acting inhalation anaesthetics (e.g. nitrous oxide) takes a few minutes to act and cause a period of excitement before anaesthesia is achieved

A

true

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13
Q

Intravenous anaesthetics act rapidly, producing unconsciousness in about ~20s; as soon as the drugs reaches the brain. Recovery from intravenous anaesthetics is due to the ??? from sites in CNS

A

distribution

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14
Q

TRUE or FALSE: opioids are frequently used together with anaesthetics due to their analgesic properties

A

TRUE

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15
Q

the combination of morphine and ??? provides good anaesthesia for cardiac surgery

A

nitrous oxide

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16
Q

??? can cause hypotension, respiratory depression and muscle rigidity as well as post‐anaesthetic nausea and vomiting

A

Opioids

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17
Q

Phase 3: Maintenance is the period during which the patient is ???

A

surgically anaesthetised

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18
Q

nitrous oxide, halogenated hydrocarbons are examples of anaesthetic drugs used for ??? phase

A

maintenance

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19
Q

Elimination of ??? is predominantly through exhalation of the unchanged gas

A

nitrous oxide, halogenated

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20
Q

Phase 4: Recovery is the reverse of induction, dependant on how fast the ??? diffuses from the brain (rather than metabolism of the drug)

A

anaesthetic drug

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21
Q

3 main neurophysiological changes occur during anaesthesia:
‐ unconsciousness
‐ loss of pain response
‐ loss of motor & autonomic reflexes
All can cause death at ??? doses

A

supra anaesthetic

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22
Q

Most anaesthetics cause cardiovascular depression by effects on myocardium and blood vessels as well as NS. ??? anaesthetics likely to cause dysrhythmias.

A

Halogenated

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23
Q

All agents apart from ??? produce similar neurophysiological effects but have different pharmacokinetics/toxicity.

A

apart from ketamine, NO and
xenon

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24
Q

The Meyer‐Overton hypothesis suggests a hydrophobic site of action, as it was shown there was a close correlation between
anaesthetic ??? and lipid solubility (oil:gas partition coefficient).

A

potency

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25
Q

It was postulated the anaesthetic drug distorted the lipid component of the cell membrane and caused:
a) volume expansion or
b) altered ???

A

membrane fluidity

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26
Q

Evidence against the lipid theory is provided by the fact that not all
general anaesthetics are particularly ???

A

lipid soluble

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27
Q

Anaesthetics are thought to potentate inhibitory ??? receptors such as:
* ??? receptors
* Glycine receptors

A

ligand‐gated ion channel

GABAA

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28
Q

Anaesthetics thought to inhibit
excitatory ligand gated ion channel
receptors such as:
* NMDA
* 5‐HT3
* ???

A

Nicotinic acetylcholine

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29
Q

The ??? receptor is a pentamer usually consisting of 2x α, 2x β and 1x γ subunit

A

GABAA

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30
Q

each subunit of the GABAA receptor has many variants that cause different ???

A

binding properties

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31
Q

The presence of a particular domain, or binding site on ??? receptor is necessary for potentiating effects of a given anaesthetic agent.

A

GABAA

32
Q

The isoform of ??? receptor containing the β3 variant subunit may mediate loss of consciousness, while isoforms containing the β2 variant subunit mediate sedation.

A

GABAA

33
Q

Binding to GABAA receptors INCREASES or DECREASES (?) concentration of agonist required to achieve a maximal response =
prolonged synaptic current.

A

decreases

34
Q

GABAA receptors: Volatile or IV anaesthetics bind at interface of α‐ β‐subunits?

A

volatile

35
Q

GABAA receptors: Volatile or IV bind only at β‐subunit?

A

IV

36
Q

Glutamate is major excitatory neurotransmitter in the CNS and has 3 classes of ionotropic receptor, ???, AMPA and Kainate.

A

NMDA

37
Q

NMDA is an important site of action for anaesthetics including, nitrous oxide, xenon and ???

A

ketamine

38
Q

Ketamine or xenon (?) blocks the pore of the NMDA channel

A

ketamine

39
Q

Xenon or ketamine (?) inhibits NMDA receptors by competing with glycine for its regulatory site

A

xenon

40
Q

What is the most common form of general anaesthetic for induction of anaesthesia, followed by an inhalation agent?

A

intravenous general anaesthesia agents

41
Q

IV general anaesthesia agents are not ideal for maintenance due to their ???

A

slow rates of elimination

42
Q

propofol: Facilitates inhibitory neurotransmission mediated by ???

A

GABAA

43
Q

propofol has a high lipid solubility = ??? onset of action (cross BBB rapidly)

A

rapid

44
Q

t1/2 is short (2‐8 mins), so recovery is also quick and has less hangover (low nausea). this describes propofol, thiopental, or etomidate?

A

propofol

45
Q

what agent can be used to induce and/or maintain anaesthesia for example, in day surgery where rapid
recovery is desirable BUT not usually used for maintenance due to slow elimination

A

propofol

46
Q

propofol infusion syndrome: severe metabolic acidosis, skeletal muscle
necrosis, hyperkalaemia, lipaemia,
hepatomegaly, renal failure, arrhyrthmia and ???

A

cardiovascular collapse

47
Q

what is the only remaining barbiturate in common use as an
anaesthetic and is administered via IV?

A

thiopental

48
Q

??? has a higher lipid solubility than propofol and very fast onset of action as a result. given as a sodium salt due to high lipidity and poor water solubility

A

thiopental

49
Q

TRUE or FALSE: thiopental has a short duration due to redistribution (mostly to muscle) rather than metabolism/ elimination. It accumulates in body fat, restricting ability to give repeated doses.

A

TRUE

50
Q

thipental cause tissue damage if extravascular injection accidentally takes place or injected into ???

A

artery

51
Q

??? is similar to thiopental but more rapidly metabolised. Binds to GABAA receptor, especially the R enantiomer. Has greater therapeutic window

A

Etomidate

52
Q

Thiopentalm, propofol, or etomidate is structurally unrelated to other anaesthetics due to an imidazole ring that allows water solubility under acidic conditions and lipid solubility under physiological pH

A

etomidate

53
Q

ketamine’s mode of action differs from other agents and has been demonstrated to be an ???
receptor antagonist ‐ specific ketamine receptors and interactions with opioid receptors have been postulated. S enantiomer more potent indicates a stereospecific receptor.

A

NMDA

54
Q

??? causes a neuroleptic state i.e dissociative anaesthesia where patient appears conscious but amnesic and insensitive to pain. Thalamus dissociated from limbic cortex

A

ketamine

55
Q

what drug causes hallucinations, disturbing dreams and delirium, however is a “complete” anaesthetic
in that it produces analgesia, amnesia and unconsciousness. Side effects less in children so sometimes used in paediatrics

A

ketamine

56
Q

In contrast to other agents ketamine ??? arterial blood pressure, heart rate and cardiac output. Also causes increased intracranial pressure. Respiration unaffected.

A

increases

57
Q

Commonly use inhalation or IV (?) anaesthetic drugs in maintenance (rather than induction) of anaesthesia

A

inhalation

58
Q

Isoflurane, sevoflurane and desflurane are typical modern ??? anaesthetics that have excellent pharmacokinetic properties, are non‐flammable and have few side‐effects.

A

inhalation

59
Q

what are generally small, lipid‐soluble molecules that readily cross the alveolar membranes.

A

Isoflurane, sevoflurane and desflurane and Nitric oxide

60
Q

define an anaesthethics pharmacokinetics

A

Rate of delivery of the drug to the lungs by inspired air and rate of delivery of drug from the lungs by the bloodstream and then to the tissues

61
Q

blood:gas parition coefficient = solubility in blood or fat?

A

blood

62
Q

oil: gas partition coefficient = solubility in blood or fat?

A

fat

63
Q

for rapid control of inhaled anaesthetics, you want the blood concentration to follow as quickly as possible the changes in ??? of the drug in inspired air

A

partial pressure

64
Q

which coefficient determines induction rate and recovery?

A

blood: gas coefficient

65
Q

TRUE or FALSE: The higher the blood/gas coefficient the greater the anaesthetic’s solubility and the greater the uptake by pulmonary circulation = alveolar pressure rises slower, prolonging induction.

A

TRUE

66
Q

alveolar pressure is ??? by the residual lung gas (i.e. oxygen) when anaesthetic first inhaled

A

reduced

67
Q

(blood-gas) if an anaesthetic is more soluble, it has a fast or slow onset?

A

slow onset

68
Q

(solubility in lipids) More lipophilic anaesthetics have lower or higher potency?

A

higher

69
Q

(solubility in lipids = potency) Lipophilic anaesthetics gradually accumulate in ??? = prolonged “hang‐over”

A

body fat

70
Q

why is there an issue of giving anaesthetic drugs with high lipophilic nature?

A

low blood flow to adipose tissue means it takes many hours for drug to enter and exit fat following rapid blood‐gas exchange

71
Q

what type of anaesthetic inhibits voltage‐dependent Na+‐channels within neuronal cell membrane. Prevents neuronal action potential propagation by penetrating neuronal phospholipid cell membrane in non‐ionised (lipophilic) form, is protonated inside the neuron, and then binds to internal surface of Na+‐ channels in their ionised form

A

local anaesthetic

72
Q

Local Anaesthetic preferentially blocks open Na+‐channels = “Use dependence”, ie. degree of
blockade is proportional to the ???

A

rate of stimulation of the nerve

73
Q

Local anaesthetic esters: Relatively unstable in solution, inactivated quickly by non‐specific esterases
in plasma and tissue. Metabolism of most esters produces ??? ‐‐ known to
cause allergic reaction

A

para‐ aminobenzoate (PABA)

74
Q

local anaesthetic amides: Stronger bond, more stable in solution,
longer shelf‐ life ~2 yrs. Heat stable or instable?

A

stable

75
Q

TRUE or FALSE: all Local Anaesthetics are weak bases

A

TRUE

76
Q

local anaesthetic potency: Higher lipid solubility = better able to cross cell membranes = ???

A

more potent

77
Q

local anaesthetic duration of action: Higher protein binding = less free fraction available for metabolism = ???

A

longer duration of drug

CHEM358 Pharmacology (11 decks)

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