Pharmacology Flashcards

1
Q

Pentazocine mode of action

A

Agonist at κ-opioid receptors antagonizing μ-opioid receptors

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2
Q

Clozapine mode of action

A

Atypical antipsychotic. Partial agonist at D2 and antagonist at 5-HT2A

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3
Q

Competitive antagonist dose response curve action

A

Shift curve to right. CMax unaltered

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4
Q

Antagonists may also act as agonists - true/false

A

Yes, if mixed antagonist/agonist e.g. pentazocine

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5
Q

What is ED50

A

Effective concentration 50 - refers to dose of the drug. Dose required to produce an effect in 50% of the population that take it

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6
Q

Therapeutic index calculation

A

Lethal dose / ED50

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7
Q

Wrt log-dose response curve - how do you assess potency

A

Position of ED50

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8
Q

G-protein CR subunits

A

alpha, beta, gamma subunits

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9
Q

Insulin receptor - Mode of Action

A

Via tyrosine kinase - NOT GPCR

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10
Q

Mixed antagonist/agonist drugs

A

Opioids (Pentazocine, Nalbuphine and Buprenorphine), Mirtazepine, Pindolol and Xameterol

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11
Q

Xameterol MoA

A

Mixed beta agonist/antagonist

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12
Q

Pindolol MoA

A

Non-selective Beta-blocker with partial beta-agonist activity. It also has partial agonist / antagonist activity at the 5-HT1A recepto

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13
Q

Time constants vs Half life

A

An exponential process is said to be complete after 3 time constants, as opposed to 5 half-lives thus TC is longer

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14
Q

Time constant definition

A

Time taken for expontential process to fall by 37% or 1/e its previous value

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15
Q

ACh subunits

A

2 alpha, 1 beta, 1 delta and epsilon (replaced by gamma in foetus)

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16
Q

Loop diuretic effects

A

Hypomagnesium, kalaemia and natraemia

Metabolic alkalosis

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17
Q

Cimetidine - enzyme inducer or inhibitor

A

Inhibitor

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18
Q

Csf constituents

A
Magnesium higher 
Glucose lower
Potassium lower
Chloride higher
Sodium marginally lower
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19
Q

Svr calculation

A

Svr = (map-cvp) / co

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20
Q

Vaporiser output calculation

A

(Carrier gas flow x svp) / ambient pressure - svp

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21
Q

MET O2 consumption

A

3.5ml O2 / kg / min = 1 met

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22
Q

Adenosine diphosphate effect

A

Conformational change in fibrinogen receptor which secures platelet plug

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23
Q

Endothelin effect

A

Most potent vasoconstrictior

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24
Q

Disinfection

A

Cleans everything but bacterial spores

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25
Q

Sterilization

A

Cleans everything including bacterial spores

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26
Q

From thick ascending limb of loop of Henle - what is absorbed via secondary active transport?

A

K and Cl cotransported

H countertransported

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27
Q

Sodium movement in DCT

A

Via specific sodium channel AND cotransport with Cl

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28
Q

H2O resorption

A

70% PCT, 25% DCT

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29
Q

K resorption

A

90% in PCT

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30
Q

What is urinary concentration of K dependent on

A

Secretion in DCT/collecting ducts

Passive secretion via channels and K/Cl cotransport and active transport via Na/K ATPase

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31
Q

Plasma conc. for renal threshold of glucose

A

11 mmol/L

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32
Q

Potassium resorption

A

55% PCT

30% Loop of Henle

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33
Q

Do ADH and Angiotensin II suppress renin?

A

Yes

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34
Q

Angiotensin II effects

A

Stimulate thirst
Constrict afferent and efferent arterial (Efferent > afferent, thus increasing GFR)
Aldosterone release
ADH release
Act directly on Na/H antiporters in PCT to cause Na and H2O retention

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35
Q

ANP renal effects

A

Afferent arteriolar dilation and efferent arteriolar constriction, thus increasing net filtration pressure

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36
Q

Renal clearance equation

A

Clearance = (urinary concentration x urinary flow rate) aka renal excretion / plasma concentration of substance

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37
Q

Renal blood flow equation

A

Renal blood flow = renal plasma flow / (1-HCT)

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38
Q

Critical temperature of O2

A

-118 deg C

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39
Q

Temp in VIE

A

-160 to -180 deg C

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40
Q

Nitrous critical temp

A

36.4 degrees

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41
Q

What are medical gas cylinders made of?

A

Molybdenum steel

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42
Q

What do the plastic neck rings around gas cylinders signify?

A

Date of last safety check (Every 5 hrs)

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43
Q

Inspiratory limb within expiratory limb breathing system

A

Bain (Coaxial mapleson D)

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44
Q

Expiratory limb within inspiratory limb

A

Lack (CoAxial mapleson A)

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45
Q

Fresh gas runs in inner tube of this coaxial system

A

Bain

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46
Q

Fresh gas flow in outer tube of this coaxial variant

A

Lack

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47
Q

Soda lime equations

A
  1. CO2 + H2O → H2CO3 (slow, rate-limiting step)
  2. H2CO3 + 2 NaOH →2 H2O + Na2CO3
  3. Na2CO3 + Ca(OH)2 →2 NaOH + CaCO3
  4. H2CO3 + Ca(Oh) 2 - - > CaCO3 + 2H2O
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48
Q

What is the Pethick check

A

Checks for inner tube defect in Bain system

49
Q

Euler’s number

A

2.718

50
Q

Time constant definition

A
  1. It is the time required for a process to complete if it continued at its initial rate of fall, i.e. it is the tangent to the graph at time = 0
  2. The graph (Fig 1) shows that it is the time taken for the magnitude of the variable to fall to 37% of its initial value
  3. The time to fall to 1/e or 1/eth of its original value.
51
Q

Relationship between tau and k

A

τ = 1/k

52
Q

1/2 life and t relationship

A

t½ = τ x 0.693

53
Q

Clearance equation

A

Clearance = drug infusion rate/blood concentration

The relationships between clearance and the rate and time constants can be expressed mathematically as:

Cl = k x Vd

or

Cl = Vd/τ

54
Q

adrenaline low dose effects

A

Increased beta effects

55
Q

adrenaline high dose effects

A

increased alpha effects

56
Q

What sympathomimetic may cause diastolic to fall due to B2 linked peripheral vasodilation

A

Adrenaline

57
Q

D1 receptor activation

A

Vasodilation of renal and mesenteric beds

58
Q

Dopamine effects

A

It increases atrio-ventricular conduction
Can cause tachycardia at higher doses particularly with inadequate preload
It stimulates noradrenaline release

59
Q

Dobutamine site of action

A

Mainly B1 with some B2 and a1 effects

60
Q

Similar structure to isoprenaline

A

dobutamine

61
Q

Dobutamine effect on peripheral vessels

A

Decreases left ventricular end diastolic pressure (LVEDP, see Starling’s law) via its action on peripheral β2-receptors. β2 linked peripheral vasodilatation reduces venous return and systemic vascular resistance

62
Q

Dopexamine mode of action

A

Dopamine analogue. Mainly b2 action with some D1 action. no A1 action
Inotropic via B1
Reduces SVR and afterload via B2

63
Q

Levosimendan mechanism

A

Increases myocyte sensitivity to Ca2+ by binding to Trop C without increasing intracellular Ca2+

Relaxes vascular smooth muscle by opening ATP-sensitive K channels causing peripheral vasodilation

64
Q

Methyldopa MoA

A
a2 agonist (+ minimal a1)
S/E - Positive direct coombs test 10-20% of cases
65
Q

Clonidine MoA

A

a2 agonist (+ minimal a1).
Also inhibits ADH + inhibits insulin release
Rebound HTN following acute cessation

66
Q

Guanethidine MoA

A

Enters adrenergic neurone via neuronal reuptake and displaces norad thus prevent further norad release

Leads to decreases a1 stimulation
S/E - diarrhoea and postural hypotension
Commonly used now to manage chronic pain

67
Q

Trimetaphan

A

Ganglion blocking agent - non depolarizing competitive antagonist at ganglion type nicotinic receptors of autonomic ganglia

S/E - assoc histamine release
side effects mainly to parasympathetic NS

68
Q

Sodium nitroprusside side effects

A

Reacts with OxyHb to form cyanide, NO, and methaem. 5 cyanide molecules per SNP
Broken down in light, so syringes covered in foil

69
Q

Sodium nitroprusside MoA

A

Given only parenterally
Rapid onset and offset
Acts on arterioles and venules
Increases ICP but autoregulation maintained
Activates renin/angiotensin system and increases plasma catecholamines which can cause rebound hypertension if treatment is stopped abruptly
Hypoxic pulmonary vasoconstriction can be inhibited causing shunt

70
Q

Magnesium anti hypertensive effect

A

Direct action on vascular smooth muscle

71
Q

ACE inhibitor subgroups

A

Active drug, metabolized to active metabolites – Captopril
Pro drugs activated in liver – Ramipril
Active drugs excreted unchanged in urine – Lisinopril

72
Q

Phentolamine

A

Short acting competitive antagonist for a1 and a2

A1&raquo_space;> A2

73
Q

Phenoxybenzamine

A

Non selective alpha antagonist. More selective for alpha 1

Irreversible blockade of alpha receptors + inhibit catecholamine uptake

74
Q

Can induce AF due to decreased atrial refractory period - which antiarrhythmic/drug used in SVT

A

adenosine

75
Q

Raises risk of dig toxicity

A
HypoK
HypoMag
HyperNa
HyperCa
Hypoxia
Renal failure
Other drugs - amiod, verapamil, diazepam
76
Q

Fentanyl metabolism - where, to what and active or not

A

Hepatic, norfentanyl, inactive metabolite

77
Q

Efficacy Definition

A

Measure of maximal effect of agonist + describes ability to produce a therapeutic effect

78
Q

Term pregnancy respiratory chances

A

Lower frc + rv, Lower chest compliance, lower airway resistance

Higher minute ventilate due to higher tidal volume and RR (TV > RR

79
Q

Cerebral autiregulation

A

60-140mmhg

80
Q

Cytochrome isoform responsible for metabolism of opiates/benzos

A

CYP3A4

81
Q

Cytochrome isoform responsible for metabolism of sevo/iso/halothane

A

CYP2E1

82
Q

Does sevo inhibit pulmonary vasoconstriction

A

true

83
Q

Vapour that sensitises heart to catecholamines

A

halothane

84
Q

Esmolol - selective or non selective?

A

Non selective

85
Q

Beta blockers metabolised by kidney mainly:

propranolol, sotalol, labetalol, atenolol, metoprolol

A

atenolol, sotalol

86
Q

Labetalol

Effect

A

Beta > alpha
3:1 oral and 7:1 IV
Retrograde ejaculation due to alpha blocking action
Significant intrinsic sympathomimetic activity
Significant postural hypotension

87
Q

Dopexamine

MoA + effect on splanchnic blood flow

A
Analogue of dopamine
No alpha activity
Mainly beta + on D1/2
Inhibits uptake-1
Powerful splanchnic vasodilator, thus reducing afterload
88
Q

Etomidate moa

A

Enhances GabaA

Lower ceberal blood flow and icp

89
Q

Etomidate isomer

A

Stereoisomer
Two enantiomers
Only R is biologically active

90
Q

Nernst equation

A

Proportional to RT (universal gas constant + absolute temp on kelvin)

Inversely proportional to zF (ionic valency and Faraday constant)

91
Q

Kinetic energy

A

1/2mv^2

92
Q

BP changes in pregnancy

A

SVR fall
SBP fall by 10% by 20 weeks, then back to normal by term
DBP fall by 25% by 20 weeks, then back to normal by term

93
Q

RBCs and pregnancy

A

Red blood cell volume falls during the first 8 weeks, rises to non-pregnant levels by 16 weeks and rises to 30% above non-pregnant levels by term

94
Q

Respiratory changes in pregnancy

A

Respiratory changes in pregnancy are as follows (Fig 1):

Alveolar ventilation ↑ by 70% at term
Tidal volume ↑ by 45% at term
Respiratory rate ↑ by 10%
Minute ventilation ↑ by 50% due to larger tidal volumes

95
Q

Synthetic catecholamines

A

Isoprenaline, dobutamine

96
Q

Rate limiing step in catecholamine synthesis

A

L-Tyrosine –> DOPA via tyrosine hydroxylase

97
Q

Nitrous effects

A

Direct myocardial depressent, but also increases sympathetic tone
Increase cerebral blood flow
Inhibits NMDA receptors, stimulates alpha adrenoreceptors + dopaminergic receptors
Oxidies cobalt ion in B12
Avoid first trimester of pregnancy
Directly activates opioid receptors + stimulates endogenous opioid release

98
Q

force

A

kg/ms^2

99
Q

pressure

A

kg/m/s^2

100
Q

Joule

A

kgm^2/s^2

101
Q

power

A

m^2kg/s^3

102
Q

Defibs

A

AC charges defib
DC delivered to patient. Rectifier converts AC to DC
Capacitor stores charge before discharge
Current produced during shock is about 35 A

103
Q

Normal PT

A

12-16s

104
Q

Normal APTT

A

23-31s

105
Q

TT

A

13-15s

106
Q

Bleeding time

A

3-9 mins

107
Q

MRI + atom aligning + MoA

A

The magnetic field of an MRI scanner aligns atoms with an odd number of protons plus neutrons
Bursts of radiofrequency energy are then applied ,which are taken up by hydrogen nuclei in water and knocked out of alignment
The energy is subsequently released again as the hydrogen ions ‘relax’ and is picked up by an external radiofrequency coil.

108
Q

Strength of an MRI

A

less than 2 Tesla

109
Q

Initial concentration equation

A

initial concentration = Dose/Vd

110
Q

Atracurium metabolism

A

Ester hydrolysis (60%) to laudanosine, quaternary alcohol and quaternary acid

Sped up by acididy

Hoffman degradation, slowed by acidity and hypothermia, to laudanosine and quaternary monoacrylate

111
Q

Cisatracurium metabolism

A

Hoffman degradation to mono quaternary acrylate

112
Q

Ketamine metabolism

A

De methylated in liver

Active metabolite - norketamine

113
Q

the context sensitive half time is proportional to the duration of an infusion - True/False

A

False - CSHT is always constant. Also is equal to the half life

114
Q

rate of elimination = clearance multiplied by drug concentration

A

true

115
Q

Surrogate measure of LVEDP

A

Wedge pressure

Will also equal capillary pressure, left atrial pressure + pulmonay artery pressure

116
Q

Cerebral autoregulation MAP

A

50-140mmHg

117
Q

Vd, dose, plasma concentration equation

A

Vd = dose/plasma concentration.

118
Q

Clearance = dose / auc

A

As above