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1
Q

Codeine difference to morphine

A

methyl group on C3

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2
Q

Naloxone difference to morphine

A

methylation on the amine group

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3
Q

Heroin difference to morphine

A

acetylation of C3/C6 hydroxyl groups

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4
Q

Protein binding fentanyl

A

85%

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5
Q

Protein binding alfentanyl

A

90%

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6
Q

Protein binding morphine

A

35%

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7
Q

Protein binding remi

A

70%

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8
Q

T1/2 B morphine

A

160 mins

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9
Q

T1/2 B fentanyl

A

190 mins

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10
Q

Vd morphine

A

4L/kg

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11
Q

Potency compared to morphine - fentanyl

A

100x

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12
Q

Potency compared to morphine - alfentanyl

A

10-20x

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13
Q

Potency compared to morphine - codeine

A

0.1x

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14
Q

Morphine oral bioavailability

A

25%

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15
Q

Morphine clearance

A

15ml/kg/min

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16
Q

Morphine metabolism

A

Hepatic glucuronidation
M3G, M6G metabolites.
Active
M3G no analgesic property, neurotoxic + seizure
M6G 10x more potent than parent
renal excretion

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17
Q

Pethidine metabolism

A

de-methylation -> norpethidine -> 50% potency
- Convulsant property

Ester hydrolysis -> pethidinic acid -> inactive

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18
Q

Effects of pethidine other than opioid effect

A

anti-cholinergic - tachycardia, dry mouth
LA effect
SSRI - interaction with MAO inhibitors -> serotonin syndrome

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19
Q

Metabolism fentanyl

A

hepatic -> norfentanyl, inactive
also significant first pass pulmonary endothelium uptake

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20
Q

Opioid with highest lipid solubility

A

sufentanyl

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21
Q

Vd alfentanil

A

0.6L/kg

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22
Q

Methadone T1/2B

A

12-60 hours, unpredictable

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22
Q

Methadone

A
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23
Q

Methadone bioavailability

A

75%

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24
Methadone protein binding
90%
25
Methadone side effects
QT prolongation other opioid related side effects
26
Tramadol enantiomers
(+) - SSRI effect (-) - SNRI effect
27
Tramadol bioavailability
90%
28
Tramadol metabolism
2D6 Demethylation -> glucuronidation ODMT -> high affinity for opioid receptors, 10x more potent
29
Tapentadol metabolism
Extensive hepatic, no active metabolite
30
Aspirin - pKa
3
31
Aspirin - PO bioavailability
70%
32
Aspirin - protein binding
85%
33
Aspirin - metabolism
rapidly to salicylic acid via intestinal and hepatic esterase's active metabolite with longer T1/2B of 3 hours
34
Aspirin - what is Reye's syndrome
fatty liver, encephalopathy, cerebral oedema
35
Aspirin - overdose pathophys
uncoupling of oxidative phosphorylation Increased aspirin level -> direct stimulation of resp centre -> resp alkalosis Anaerobic glycolysis -> metabolic acidosis
36
Aspirin - overdose Sx
sweating, tinnitus, blurred vision tachycardia pyrexia hyperventilation
37
Parecoxib onset and peak effect
15 mins 2 hours
38
Basic structure of LA
Hydrophilic tail - determines degree of ionisation Lipophilic aromatic ring - determines lipid solubility Intermediate link - determines type of LA (amide vs. ester
39
LA binding site on VG NAC
domain IV, segment 6
40
what is frequency dependent blockade
LA molecules have greater access to Na channels when they are in activated open state. increase opening -> increase access to LA binding site of Na channels
41
Protein binding of lignocaine
70%
42
Protein binding of bupivocaine
95%
43
Ranking of vasodilatory effect of LA
Prilocaine > lignocaine > bupivocaine > ropivocaine
44
LA systemic absorption route in order of decreasing rate
Intravenous > intercostal > caudal block > epidural > peripheral nerve > submit infiltration
45
Metabolite of lignocaine
hydroxy-xylidine, active metabolite
46
Lignocaine dose dependent systemic effect
1-5ug/ml - analgesia 5-10 - tingling, visual disturbance 10-15 - seizure 15-20 - hypotension, coma >20 - respiratory depression, CV collapse
47
T1/2 B lignocaine
1.5hrs
48
T1/2B bupivocaine
2.5hrs
49
T1/2 B ropivocaine
2.0 hrs
50
Ropivocaine pharmaceutics
Enantiopure, S enantiomer
51
Prilocaine pKa
7.7, 33% unionised
52
Protein binding prilocaine
50%
53
Define Eutectic
A mixture of substances that has a lower melting point than that of its constituents
54
Cocaine max dose
1.5mg/kg
55
Cocaine MOA
LA + uptake 1 and MAO inhibitor
56
Structure-activity sympathomimetics - requirement for direct activity
-OH group on C3 + Beta carbon
57
Structure-activity sympathomimetics - indirect activity
non-bulky terminal amine to allow reuptake
58
Structure-activity sympathomimetics - phenylephrine
Lacks -OH 4, non-catecholamine Direct activity due to -OH on C3 and BC No beta activity
59
Steps of adrenaline synthesis
tyrosine -> DOPA -> L-DOPA -> Norad -> adrenaline
60
Classify ionotropes
B-1 agonists, catecholamines Phosphodiesterase inhibitors Glucagon Thyroid hormone Ca2+ Levosimenden Digoxin
61
Classify a-antagonists
Non-selective: phentolamine (short), phenoxybenamine (long) Selective a1 - a1: prazosin - a2: yohimbine (indicated for impotence)
62
Classify B-antagonist
Non-selective - propranolol Cardio selective - metoprolol, atenolol, esmolol Mixed - labetalol Intrinsic sympathomimetic activity - Present: pindolol, absent: metoprolol
63
Centrally acting anticholinergics
atropine hyoscine
64
GI effect of atropine
reduce LOS tone Reduce GI acid secretion Reduce GIT motility
65
Atropine metabolism
Extensive hepatic esterases Renal excretion
66
Timing of action of atropine
tachycardia onset 2-4 mins T1/2B 2.5 hours Duration of action 3 hours
67
Is atropine racemic?
Yes, but only L-isomer is active
68
What are the brand names of hyoscine?
buscopan scopolamine
69
Glycopyrulate metabolism
Minimal metabolism Renal excretion unchanged 85%
70
Class 1a anti-arrhythmic - example and MOA
Quinidine, procainamide Na blockade + increase duration of refractory period and AP
71
Class 1b anti-arrhythmic - example and MOA
Lignocaine NA blockade + decrease duration of refractory period and AP
72
Class 1c anti-arrhythmic - example and MOA
flecanide NA blockade + no change to refractory period
73
Digoxin - PO bioavailability
80%
74
Digoxin protein binding
25%
75
Digoxin metabolism
Minimally metabolised. Renal excreted
76
Digoxin toxic plasma level
>2.5ng/ml
77
Cardiac toxic effects of digoxin
premature ventricular contraction AV blocks junctional rhythm prolonged PR VT/VF
78
How is dig toxicity treated?
Early - gastric lavage Correct hyper / hypo K, acid-base imbalance Treat bradycardia Digoxin-specific Fab (digibind) - for Plasma level > 20ng/ml
79
Contraindication of adenosine
asthma 2nd and 3rd degree HB sick sinus syndrome
80
Amiodarone metabolism and excretion
extensive liver metabolism to N-desmethyl amiodarone Mainly excreted in bile but also lacrymal gland
81
Protein binding amiodarone
>95%, can potentiate effect of highly protein bound drugs like warfarin and phenytoin
82
Mg toxicity levels
2-3mmol/L - therapeutic 5 - loss of reflex 7.5 - respiratory depression, heart block >12 - cardiac arrest
83
GTN metabolism
rapid hepatic and RBC hydrolysis to glycerol di-nitrate and NO 80% urine excretion
84
Pathophys cyanide toxicity
Free CN- ions can bind to cytochrome oxidase to uncouple oxidative phosphorylation -> histotoxic hypoxia
85
Classify anti-HTN
Ace-inhibitor B-blockers Ca channel blockers A2 agonists A1 antagonists Nitrites Hydralazine Diuretics Anaesthetic agents
86
MOA methyldopa
prodrug - converts centrally to methyl-noradrenaline Acts as a central A2 agonist - sympatholysis effect
87
Examples of MAO inhibitors
Non-selective / irreversible - phenelzine Selective, reversible MAO-A - Moclobemide Selective irreversible MAO-B - selegiline
88
MOA of TCA
Inhibit reuptake of serotonin, noradrenaline M-AchR, H1/H2 receptors, A1 receptors, NMDA receptors
89
Compare SSRI with TCA effects
Antidepressant - no difference Less sedation, fewer anti-cholinergic, less cardio toxic More sexual dysfunction Higher rate of N/V
90
What is serotonin syndrome
Triad of cognitive, autonomic and neuromuscular symptoms due to excess serotonin activity both centrally and peripherally
91
Signs of serotonin syndrome
Cognitive: confusion, agitation, hallucination Autonomic: sweating, hyperthermia, hypertension, tachycardia Neuro: hyper-reflexia, myoclonus, tremor
92
What does MAO-A break down?
deamination of 5HT, noradrenaline, dopamine
93
What does MAO-B break down
deamination of dopamine, tyramine, phenyl-ethylamine
94
What happens when MAO inhibitors are mixed with cheese?
tyramine -> hypertensive crisis
95
What is neuroleptic malignant syndrome triggered by?
All drugs with D2 antagonist properties Blockade of DA receptors in corpus striatum to cause excessive heat production and spasticity of skeletal muscles
96
How is NMR different to serotonin syndrome?
More slow onset Rigidity, hyporeflexia Normal pupils No GI symptoms
97
Phenyltoin bioavailability
70-100%
98
Phenyltoin protein binding
90%
99
Phenyltoin metabolism
Hepatic hydroxylation, saturable process -> zero order kinetics Enzyme inducer
100
Metabolism of gabapentinoids?
negligible metabolism, excreted unchanged in urine
101
How is levodopa administered, and why?
Orally with carbidopa, a peripheral decarboxylase inhibitor to increase % of drug crossing into the BBB.
102
Classify drugs acting on the serotonin pathway
Agonist - sumatriptan, paracetamol Antagonist - ondansetron Reuptake inhibition - SSRI, TCA Prevention of breakdown - MAO-i
103
How is the MOA of clopidogrel different to ticagrelor
Ticagrelor is a reversible P2Y12 antagonist. Also not a prodrug
104
Drug that the IIa/IIIb receptors?
Tirofiban
105
Which fluid can be used for their anti-platelet effect?
dextran - induces a type 1 VWF deficiency state
106
Classify side effects of heparin
Dose-dependent: bleeding, hypotension, osteoporosis, skin necrosis, hyperkalaemia due to reduced aldosterone secretion Severe: allergy, HITT
107
What is heparin
polyanionic polysaccharide derived from bovine or porcine sources MW 5000-25000Da
108
Advantage of enoxaparin
single daily dose due to longer T1/2B lower risk of bleeding, more predictable effect Less risk of thromobocytopenia Monitoring not required Does not cross the placenta
109
Side effects of protamine
histamine release allergy pulmonary HTN due to complement activation anticoagulation in excess interaction with some insulin formulation
110
What is fondaparinux
synthetic anticoagulant that resembles the active site of heparin -> increases ATIII activity by 300x specifically to FXa
111
How is dabigatran metabolised?
Prodrug, converts to active drug by liver and plasma esterase's
112
What is the equivalent dose of 4mg dexamethasone for other steroids?
hydrocortisone - 100mg prednisolone - 25mg Methylpred - 20mg

Definition Deck (5 decks)

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