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Primary FRCA > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Tranylcypromine

A

A non-selective MAOI
Prevents breakdown of monoamines
Can precipitate hypertensive crisis due to increased levels of noradrenaline if high dietary intake of tyramine

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2
Q

Caudal blocks

A 
Use 0.25% bupivicaine 
Sacral procedures - 0.5ml/kg
Inguinal procedures - 0.75ml/kg 
Lower thoracic procedures - 1ml/kg
Mid-thoracic procedures - 1.5ml/kg
Because of varying degrees of spread of LA required 
Toxic dose 2mg/kg
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3
Q

Clozapine

A

Partial agonist at D2 receptors

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4
Q

ED50

A

Dose of the drug that produces a response that is 50% of maximal response

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5
Q

EC50

A

Drug concentration at which response is 50% of maximal

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6
Q

Cyclic AMP

A

Is a hydrophilic molecule

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7
Q

Pindolol

A

Partial agonist at beta-1 receptors
Non-selective beta blocker
Partial agonist/antagonist at 5HT1A receptors

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8
Q

Mixed agonists-antagonists

A 
Mirtazapine 
Pindolol 
Nalbuphine 
Pentazocine 
Buprenorphine 
Xameterol (at beta adrenoceptors)
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9
Q

Chemical bonds

A

Strong —> weak:
Ionic - electrostatic attraction between oppositely charged ions involving loss/gain of electrons
Covalent - sharing of electrons in the outer shells (can increase in strength with double and triple covalent bonding)
Hydrogen bonds - force of attraction between a positively charged H atom and an electronegative atom
Van Der Waals - constant movement of electrons creates temporary dipoles in atoms which cause forces of attraction

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10
Q

Adenylate cyclase

A

Membrane-bound form and soluble cytoplasmic form
Activated by G-protein which is coupled to adrenoceptors
Converts ATP to cAMP

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11
Q

Triamterene

A

A potassium-sparing diuretic
Acts in the DCT to inhibit Na reabsorption in exchange for K (blocks ENaC)
Works in the same way as amiloride

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12
Q

CSHT

A

Context sensitive half time
Time taken for plasma concentration of a drug to fall to 50% after an infusion has finished
A function of the duration of infusion, not concentration

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13
Q

Metabolism of volatile agents

A

Desflurane is a fluorinated ether and is minimally metabolised (0.02%) to produce trifluoroacetate and fluoride ions
Halothane is the only volatile agent to contain Br ions
C-F bond is stronger than C-Br bond
CYP450 enzymes which metabolise Halothane are induced by barbiturate intake
Halothane is 20% metabolised
Enflurane is 2-2.5% metabolised

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14
Q

Levorphanol

A

Pure opioid agonist

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15
Q

Phenazocine

A

Pure opioid agonist

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16
Q

Azapropazone and phenylbutazone

A

pyrazolone derivative NSAIDs

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17
Q

Aspirin

A

Rapidly metabolised by esterases in the intestinal mucosa and liver to acetic acid + salicylate which is conjugated to water soluble molecules and excreted via the kidneys
Aspirin can compete with urate for renal tubular secretion
80-90% plasma protein bound
Largely unionised in the stomach (pH 2) because it is a weak acid with pKa 3.5

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18
Q

Hypotensive effects of morphine

A

Dose-dependent histamine release
Vagal stimulation
Inhibition of central sympathetic activity
Direct vasodilation

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19
Q

Pethidine

A

More lipid soluble than morphine
Chemically related to atropine and has anti-cholinergic effects
Terminal half life is 3-5hrs
Metabolised to active metabolite norpethidine which is excreted via the kidneys
Has some local anaesthetic activity

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20
Q

Disopyramide

A

Class 1A anti-arrhythmic
Negatively inotropic —> reduces BP (but no direct action on bld vessels)
Prolongs duration of AP
May cause VT, VF or TdP

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21
Q

Diazoxide

A

Vasodilator and hyperglycaemic drug
Opens ATP-sensitive K channels in the Beta islet cells and inhibits insulin release
Causes hyperpolarisation via K efflux and decreased Ca influx
Chemically similar to thiazides

22
Q

Sumatriptan

A

Used in the treatment of migraine
5HT1 receptor agonist
Can cause Brady and tachy arrhythmias
Lipid soluble and can cross BBB

23
Q

Drugs causing uterine relaxation

A 
Indomethacin (NSAIDs)
Nifedipine (CCBs)
Magnesium 
Terbutaline and ritodrine (adrenergic agonists)
Oxytocin antagonists (atosiban)
NO donors e.g. nitroglycerin 
Volatiles
24
Q

Flumazenil

A

BDZ antagonist with similar structure to BDZs
Low oral bioavailability due to extensive FPM so only give parenterally
Rapid hepatic metabolism results in short DOA
Can be given by continuous infusion
Lack of response to 5mg IV suggests BDZ OD not cause

25
Q

Diamorphine

A

3,6-diacetylmorphine
Di-ester of 1 molecule of morphine with 2 molecules of acetic acid
Metabolised to 3 and 6-monoacetylmorphine which is active (diamorphine has no affinity for opioid receptors) and morphine
Requires a free -OH gp at position 3
More rapid onset and shorter duration of action than morphine when give epidurally due to greater lipid solubility

26
Q

Propranolol

A

Half life 4hrs
Metabolised to 4-hydroxypropranolol which has some activity
Oral bioavailability 30%
Lipid soluble therefore can cross the BBB and cause central effects e.g. sleep disturbance

27
Q

Tetracyclines

A

Have a wide spectrum of anti-bacterial activity

Prevent bacterial proteinsynthesis by binding to ribosomes and preventing translation of mRNA

28
Q

Side effects of oxytocin

A

Transient hypotension if given rapidly
Sinus tachycardia
Nausea and vomiting
Water intoxication (due to ADH-like activity)

29
Q

Noradrenaline

A

Presented only as the L-isomer because the D-isomer is much less potent

30
Q

Opioids

A

can stimulated 5HT3 receptors and cause N&V

31
Q

Buprenorphine

A

Partial agonist with high affinity for mu opioid receptors
Elimination half life of 3-4hrs but much longer DOA
Extensive FPM
30x more potent than morphine

32
Q

Induction doses of IV agents

A

Etomidate: 0.3mg/kg
Thiopental: 3-5mg/kg
Ketamine: 1-2mg/kg
Propofol: 2mg/kg

33
Q

Thiopental

A

Causes respiratory depression via direct action on medullary respiratory centre
80% plasma protein bound at pH 7.4
Highly lipid soluble
Distributes rapidly into well perfused tissues (water compartments)
Slowly metabolised in the liver (low HER)

34
Q

Ester LAs

A

Include amethocaine and cocaine

Highly protein bound

35
Q

Atropine

A

Less potent than glycopyrrolate
Presented as a racemic mixture of D- and L-hyoscyamine
Causes mydriasis and raised IOP
Decreases GI motility and secretions
Causes bronchodilation and increased physiological dead space
Non-selective mAChR antagonist

36
Q

Protein binding

A

Acidic and neutral drugs bind to albumin:
- phenytoin, diazepam, NSAIDs, propofol
Basic drugs bind to alpha1 acid glycoprotein:
- LAs, opioids

37
Q

Bioavailability

A 
Aspirin 65%
Oramorph 25%
Paracetamol 90%
Ibuprofen >80%
Diclofenac 50%
38
Q

Cisatracurium

A

3-4x more potent than atracurium
Predominantly metabolised by Hoffman degradation
Metabolism unaffected by renal function

39
Q

Ester LAs

A

Highly protein bound

40
Q

Fade in NMB

A

Caused by blockade of pre-junctional nAchRs which normally provide positive feedback during high stimulation

41
Q

Heparin

A

Does not cross the placenta as low lipid solubility so does not affect the foetus
Causes hyperkalemia by inhibiting aldosterone

42
Q

Ketamine

A

Indirect positive inotropic effect via catecholamine release
Direct negative inotropic effect

43
Q

Etomidate

A

Broken down by Ester hydrolysis

10-20x more potent than thiopental

44
Q

Alfentanil

A

90% unionised at pH7.4
90% protein bound (more than other opioids)
Lower clearance but smaller Vd than morphine and fentanyl
10x less potent than fentanyl

45
Q

Sevoflurane

A

BP 58’C

Causes dose dependent resp depression

46
Q

Thiopental

A 
Sulphur analogue of pentobarbital 
Forms a sodium salt
Weak acid with pKa 7.6
Forms an alkaline solution in water 
Acid may precipitate out of solution so sodium carbonate is added and it is stored in vials with N2
80% ionised at physiological pH
Rapid onset due to high lipid solubility
Rapid emergence due to redistribution 
Contraindicated in porphyria
47
Q

Xenon

A

3x denser and twice as viscous as nitrous oxide

48
Q

Systemic absorption of LAs

A 
In order of increasing absorption:
Subcutaneous 
Femoral 
Brachial plexus 
Epidural 
Caudal 
Intercostal
Poor absorption when injected subcut or around plexi/large veins
49
Q

LAs

A

Most have vasodilator effects at low conc and vasoconstrictor effects at high conc
Cocaine is a pure vasoconstrictor

50
Q

Drugs undergoing zero order kinetics

A 
Phenytoin 
Ethanol 
Salicylates
Thiopental 
Theophylline
“PESTT”
51
Q

Inodilators

A

Improve cardiac contractility and vasodilation
Reduce preload and afterload
Include dopexamine (acts via dopamine and B2 receptors)
PDE3 inhibitors e.g. milrinone and enoximone
Theophylline is NOT an inodilator
Levosimendan is NOT an inodilator (calcium sensitiser)

Primary FRCA (3 decks)

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