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Primary FRCA > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Isomerism

A

Structural - dynamic or static
Stereo - enantiomers or diastereoisomers

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2
Q

Chiral centre

A

Central atom bound to 4 dissimilar groups

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3
Q

Enantiomer

A

Stereoisomer with a single chiral centre, producing non-superimposable isomers

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4
Q

Tautomerism

A

Dynamic change between 2 different forms depending on environmental conditions

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5
Q

Optical isomerism

A

Ability to rotate polarised light in different directs

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6
Q

Time constant

A

Time taken for plasma conc to fall to 0 if initial rate of elimination continued
Reciprocal of the rate constant 1/e
Always longer than half life (half life is shorter by a factor of 0.693)

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7
Q

Clearance

A

Volume of plasma cleared per unit time

Cl = Input/plasma conc

Cl = Ke x Vd (where Ke is elimination rate constant)

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8
Q

Loading dose

A

Vd * desired concentration

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9
Q

Maintenance dose

A

Steady state con x clearance

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10
Q

First Order Kinetics

A

Rate depends on conc of reactants.
Constant proportion; half life and clearance are constant
Exponential

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11
Q

Zero Order Kinetics

A

Independent of the conc of reactants
Constant rate
Fixed amount cleared; half life decrease

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12
Q

Michaelis-Menten Equation

A

Predicts rate according to substrate concentration and specific enzyme characteristics

V= Vmax[substrate]/Km + [substrate]

Where Km = substrate conc at which velocity is half of max (equivalent to ED50)

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13
Q

Agonists

A

Demonstrate affinity and intrinsic activity;
full agonists = 1
partial agonists < 1

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14
Q

Antagonists

A

Demonstrate affinity but no intrinsic activity

Competitive antagonists:
-same site binding
-shift the dose response to the right, but can achieve the same Emax with increased dose

Non-competitive antagonists
-allosteric binding
-reduce the Emax, effect not overcome by ^^ dose

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15
Q

Mixed agonist/antagonists

A

Opioids - pentazocine, buprenorphine
Mirtazepine
Pindolol, xameterol

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16
Q

Volume of Distribution

A

Theoretical volume a drug would have to occupy to produce plasma conc.

Vd= dose/conc

Small non polar molecules distribute freely = large Vd 40L
Small polar molecules exit circulation to ECF = Vd ~ 14L
Large polar molecules trapped in circulation = small Vd 5l

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17
Q

Vd larger than total body water?

A

This effect can be due to protein binding, plasma degradation, sequestration into other tissues e.g. propofol into adipose

18
Q

Extraction ratio

A

The efficiency of an organ in eliminating a drug

If ER is high, then clearance depends only on blood flow.

19
Q

Phase 1 Elimination Reactions

A

Makes a substance water soluble, unmasks function group

CYP450 reactions;
oxidation - barbs, benzos, paracetamol, omeprazole
reduction - prednisone to prednisolone
hydrolysis - mao > adrenaline, esterases > remifentanil, atracurium, alcohol dehydrogenase > ethanol to acetic acid

20
Q

Phase 2 Elimination Reactions

A

Conjugation with a functional group

Glucuronidation - morphine activation, propofol inactiv
Acetylation - isoniazid, hydralazine
Sulphation - paracetamol
Methylation - catecholamines
Glutathione conjug - paracetamol

21
Q

TCI Models

Marsh

A

Developed for plasma effect site

Requires lean body weight

22
Q

TCI Models

Schnider

A

Requires ABW, age, height, gender
Smaller initial bolus so safer for old/frail/high ASA

23
Q

Efficacy

A

Magnitude of receptor response

24
Q

Affinity

A

Ability to bind to receptor
Reciprocal of the equilibrium dissociation constant

25
Q

Potency

A

Conc (EC50) or dose (ED50) required to produce 50% max effect
LHS with increasing potency

26
Q

Tolerance

A

Decrease in response following repeated administration
-pharmacodynamic: receptor subunit modification
-pharmacokinetic: CYP450 enzyme induction
-behavioural: learning to function

27
Q

Tachyphylaxis

A

Hyperacute tolerance after only 1-2 doses

28
Q

Adverse Drug Reactions

Type A

A

Augmented
85-90% of ADR
Related to pharmacological effects, dose related.
e.g. cough with ACEI

29
Q

Adverse Drug Reactions

Type B

A

10-15% of ADRs
Unpredictable
e.g. MH, sux apnoea

30
Q

Concentration effect

A

The phenomenon by which the speed of onset of inhalational anaesthetic agents is increased when they are administered with N2O

31
Q

The Second Gas Effect

A

The phenomenon by which the rise in the alveolar partial pressure of nitrous oxide is disproportionately rapid when administered in high concentrations

N2O diffuses into blood faster than N2 diffuses out thereby shrinking the alveolar volume and concentrating the remaining gas

32
Q

Volatiles

Lipid Solubility

A

Ability to cross the BBB and exert effect
Potency

High lipid solubility = high potency = low MAC = high OG coefficient

33
Q

Volatiles

Water Solubility

A

Ability to dissolve into the blood
Speed of onset

Low water solubility = slow speed of onset = low BG coefficient

34
Q

MAC

Definition

A

Minimum alveolar concentration of anaesthetic vapour @ equilibirum required to prevent movement to standard surgical stimulus in 50% of unpremedicated subjects at 1 atm

35
Q

MAC

Agents in ascending order

A

Halothane 0.75
Isoflurane 1.17
Enflurane 1.68
Sevo 2
Des 6.6
Xenon 71
N20 105

36
Q

Factors increasing MAC

A

Childhood

Hyperthermia/hyperthyroidism
Hypernatraemia

Catecholamines/sympathomimetics
Chronic opioids/ETOH
Acute Amphetamines

37
Q

Factors decreasing MAC

A

Neonates/old age
Pregnancy

Hypotension/hypothermia/hypothyroidism
Lithium

Alpha agonists/sedatives
Acute opioids/ETOH
Chronic amphetamines

38
Q

Nitrous Oxide

A

Manufactured by heating ammonium nitrate to 250 C
Stored as a liquid in French blue, @ 5 bar
Filling ratio 0.75 (less in warmer climates)

Critical temp = 36.5
Critical pressure = 72bar
Mol weight = 44
MAC = 105
BP = -88
SVP = 5200
BG = 0.47
OG = 1.4

39
Q

Xenon

A

Odourless, inert gas produced by fractional distillation of air, expensive.

MW = 131
BP = -108
MAC = 71
BG = 0.14
OG = 1.9

Variable increase in CBF; analgesic; no affect on contractility

40
Q

Halothane

A

Halogenated hydrocarbon containing bromine, chlorine and fluorine

Primary FRCA (3 decks)

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