Question bank · 2025 October · Pharmacology · 1 + 2 + 3 + 4 marks

One word separated the exceptional answers
— non-competitive.

Show the model answerAttempt it first — that is what makes it stick

What earns the marks10 marks

(a) Non-competitive1 mark. The commonest single error was calling the antagonism competitive
(a) Two clinical features, explicitlySome described the concept without stating two features as asked, and lost the mark for it
(b) Two DISTINCT pathways2 marks. Many detailed the NMDA receptor's cellular function instead of naming a second pathway
(b) Move beyond NMDAOpioid receptors, monoamine reuptake inhibition, or voltage-gated ion channels
(c) Norketamine is LESS potent3 marks. A frequent misconception was that it is more potent than the parent compound
(c) Beyond the metaboliteEnzyme induction with chronic use, and tolerance and dependence, were universally omitted
(d) Justify each indication4 marks, and the highest scoring part. Justification, not a list
(d) Do not include contraindicationsA few suggested induction in severe cardiac disease or uncontrolled raised ICP
a

1 mark

The mechanism of dissociative anaesthesia, with two key clinical features

One mark, three sentences. The adjective on the antagonism is what is being tested.

Mechanism, in the order it should be written

The binding
Ketamine is a non-competitive antagonist at the NMDA receptor, binding the phencyclidine recognition site inside the open channel. Glutamate can still bind; the block is not overcome by raising it.
The network effect
This inhibits NMDA-mediated glutamatergic input to the GABAergic system, producing functional dissociation between the thalamocortical and limbic systems — the cortex and thalamus are depressed while parts of the limbic system, including the hippocampus, are stimulated.
The state
A cataleptic state, unlike the sleep-like unconsciousness of the GABAergic agents. Electroencephalographically, the α rhythm is replaced by θ and δ activity.
Non-competitive, at a site inside the channel, producing dissociation between two systems rather than generalised depression. Three clauses, and the mark is secure.

Commonly lost: A common point of confusion was describing the antagonism as competitive rather than the correct term, non-competitive. The distinction is not semantic: a competitive antagonist is by definition surmountable by more agonist, and this one is not, because its site is inside the channel rather than at the glutamate site.

b

2 marks

Two of the pathways by which ketamine produces analgesia

Two distinct pathways. Elaborating on the NMDA receptor twice is one pathway described at length, not two.
PathwayMechanismConsequence
NMDA receptor antagonismNon-competitive block at the spinal dorsal horn inhibits wide-dynamic-range neuronal activity and prevents central sensitisation; supraspinally it acts in the thalamic and limbic systems responsible for interpreting the pain signalPrevents wind-up and central sensitisation; prevents opioid-induced hyperalgesia and attenuates acute opioid tolerance
Opioid receptor interactionAntagonist at μ and agonist at κ; the S(+) isomer carries some μ activityA direct analgesic contribution independent of the NMDA action
Monoamine reuptake inhibitionInhibits reuptake of noradrenaline and serotonin, and activates descending inhibitory monoaminergic pathwaysAugments endogenous descending pain inhibition
Voltage-gated sodium channel inhibitionShares a binding site with the local anaestheticsA local-anaesthetic-like membrane-stabilising contribution
Anti-inflammatory actionReduces tumour necrosis factor alpha, interleukin-6 and interleukin-8, and suppresses NF-κB expressionA contribution to analgesia in inflammatory pain states

Commonly lost: Many candidates detailed the NMDA receptor’s cellular function at length rather than outlining a second distinct pathway. Stronger answers moved beyond the NMDA receptor to opioid receptors, monoamine reuptake inhibition, or effects on voltage-gated ion channels. Two marks, two pathways: name the second one in its own sentence.

c

3 marks

The metabolism of ketamine and its clinical significance

Three marks, and the metabolite is only the first of them. Two further significances were universally omitted.

The metabolic pathway

Step 1 — hepatic N-demethylation
Hepatic microsomal cytochrome P450 enzymes demethylate ketamine to norketamine, the principal metabolite. Clearance is high, approximately equal to liver blood flow, giving an elimination half-life of 2 to 3 hours.
Step 2 — hydroxylation
Norketamine is hydroxylated to hydroxynorketamine.
Step 3 — conjugation and excretion
Conjugated to water-soluble glucuronides and excreted in the urine.
A three-step hepatic pathway. The clinical significance sits at each step, not only at the metabolite.
PointDetail
Norketamine is active, and LESS potent than ketamineReported at 20–30%, or one-third to one-fifth, of the potency of the parent compound. It contributes to prolonged analgesia after a bolus or an infusion — which is why analgesia outlasts the anaesthetic
Clearance approximates liver blood flowA high hepatic extraction ratio, so clearance is flow-limited. A fall in hepatic blood flow — or any drug that reduces cardiac output — prolongs the effect, whereas enzyme activity itself matters relatively little
Extensive first-pass metabolismBioavailability is 93% parenterally but only 20–30% orally, and about 40–50% intranasally. This is why the oral dose is several times the intravenous dose and why the intranasal route exists
Enzyme induction with chronic useUniversally omitted. Repeated administration induces the hepatic enzymes that metabolise it, contributing to tolerance
Tolerance and dependenceAlso universally omitted. A consequence of both enzyme induction and receptor-level adaptation, and the reason chronic infusions lose effect
No dependence on plasma cholinesterase or renal function for the parent drugThe conjugates are renally excreted, but the offset of a single dose does not depend on the kidney

Commonly lost: A frequent misconception was that norketamine is more potent than its parent compound; it is in fact less. And two significances were universally omitted: enzyme induction with chronic use, and the potential for tolerance and dependence. In a three-mark part, naming the metabolite is one mark — the other two are in what follows from it.

d

4 marks — the highest scoring part

The clinical indications of ketamine, with justification

The instruction was to justify. An indication without its pharmacological reason is half an answer.
IndicationJustification
Induction in the shocked or hypovolaemic patientSympathetic stimulation through increased central sympathetic outflow and inhibition of catecholamine reuptake raises heart rate, cardiac output and blood pressure, where every other induction agent lowers them
Induction in severe asthma or bronchospasmBronchodilatation, consistent with its muscarinic antagonism and sympathomimetic action
Anaesthesia where the airway must keep workingRespiratory drive is largely preserved and laryngeal reflexes relatively so, so ventilation need not be taken over. Useful in the difficult airway and in field or resource-limited settings
Analgesia — acute, chronic and opioid-sparingIntense analgesia at sub-anaesthetic concentrations; prevents opioid-induced hyperalgesia and attenuates opioid tolerance through NMDA antagonism. Reversal of opioid tolerance at 0.3 mg/kg/h
Procedural sedation and analgesia, particularly in childrenA single agent providing analgesia, amnesia and immobility, with intramuscular, oral and intranasal routes available when no vein is
Burns dressing changes and repeated painful proceduresProfound analgesia without cardiovascular depression, and it can be repeated intramuscularly
Obstetric haemorrhageMaintains maternal blood pressure where propofol and thiopentone would not
Treatment-resistant depressionAn S(+)-ketamine nasal spray is approved for this indication — worth a clause, and outside the operating theatre

Commonly lost: A minimal number of candidates suggested its use in contraindicated situations — induction in severe cardiac disease, or in uncontrolled raised intracranial pressure. Both turn a mark into a lost one. In ischaemic heart disease the tachycardia and hypertension raise myocardial oxygen demand while shortening diastole; in uncontrolled intracranial hypertension in a spontaneously breathing patient ketamine can raise intracranial pressure further.

The teaching behind this answer — ketamine and dissociative anaesthesia

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