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Revision lectures (Year 1) > ICPP (12-17) > Flashcards

ICPP (12-17) Flashcards

1
Q

How many types of GPCR do we need to know about

A

7

  • alpha-1,2
  • Beta- 1,2
  • muscarinic-1,2,3
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2
Q

When ligand attaches to the outside of the receptor

A

GaBYGTP turns into aGTP and BY

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3
Q

How many forms of aGTP

A

3

  • asGTP
  • aiGTP
  • aqGTP
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4
Q

Outline QISS QIQ

A

Q- a1
I- a2
S- B1
S- B2

Q- M1
I- M2
Q- M3

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5
Q

asGTP

A

Stimualtes adenylyl cyclase- increasing cAMP

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6
Q

aiGTP

A

Inhibits adenylyl cyclase- decreasing cAMP

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7
Q

aqGTP

A

Stimulates phospholipase C, increasing IP3 and DAG

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8
Q

cAMP

A

Second message which stimulus PKA to phosphorylates proteins

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9
Q

IP3 stimulates

A

Calciumr elease from the ER through calcium channels to

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10
Q

DAG

A

Stimulates PKC to phosphorylates proteins e.g. VOCC

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11
Q

CGMP

A

Stimulates PKG to phosphorylates proteins

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12
Q

Signal amplification

A

1 GPC x multiple G- proteins x multiple effectors x multiple second messenger x calcium induced calcium release

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13
Q

E.g. M2 cholinrecepts with GI in the heart cause

A

Negative chronotoropy when ligands bind

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14
Q

B1 adrenoreceptors with Gs in the heart cause

A

Positive chronotropy when ligand bind

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15
Q

B1- adrenoreceptors wit gq cause

A

Arteriolar vasoconstriction

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16
Q

U- opioid receptors with GI cause

A

Less NT release

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17
Q

Relatively high calcium in

A

Extracellular space

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18
Q

High (ca2+)e created by

A

Sodium calcium exchanger (NCX)

Plasma membrane calcium ATPase (PMCA)

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19
Q

Where else is calcium high

A

In the SER/SR

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20
Q

How is high conc of calcium maintained in SR

A

Smooth endoplasmic reticulum calcium ATPase (SERCA)

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21
Q

What releases calcium into the cytoskeleton false

A

Voltage gated calcium channels and ligand gated Calcium channels

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22
Q

What releases calcium intot he cytoplasms slowly

A

Store operated calcium channels (SOC)

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23
Q

Explain calcium induced calcium release

A
  • IP3 from phospholipase C binds to ligand gated calcium channel not he SR
  • calcium leased
  • calcium binds to different ligand gated calcium channels;s
  • more calcium is released
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24
Q

All fibres in the ANS are

A

Efferent

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25
Q

the ANS is not

A

Under conscious contro

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26
Q

Main devious for he ANS

A

Sympathetic and aradymapthetic

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27
Q

Sympathetic

A

Fight or flight

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28
Q

Parasympathetic

A

Rest and die gets

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29
Q

Preganglionic neuron release

A

ACH into nicotinic acetyl choline receptor in post ganglionic neuron

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30
Q

Sympathetic (fight or flight)

A
  • thoracolumbar emergence
  • ganglaite in peruses paravertebrally or elsewhere
  • medium pre
  • Long post
  • Release NA into a1, a2, B2 adrenoreceptors
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31
Q

Parasympathetic (rests and digest)

A

Cranial sacral (top and bottom) eme3rgence

  • ganglia at the target organ
  • long pre
  • short post
  • release ACH into M1 and m2 and M3 mACHr
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32
Q

What breaks ACetyl choline down

A

Acetylcholineesterase

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33
Q

What makes ACH

A

Actetycholinetransferase

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34
Q

How is adrenaline male

A

Catecholamine synthesis

  • tyrosine -> DOPA —> dopamaine —> NA —> A
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35
Q

What breaks down cytoplasmic NA

A

Monoamine oxidase (MAO)

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36
Q

adrenoceptor agonists

A

increase sympathetic stimulation

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37
Q

adrenoceptor antagonists

A

decrease sympathetic stimulation

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38
Q

muscarinic cholinoceptor agonists increase

A

parasympathetic stimulation

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39
Q

muscarinic cholinoceptors antagonists

A

decrease parasympathetic stimulation

40
Q

name 9 ways drug can be administed

A 
oral
intravenous
intramusuclar
transdermal
intranasal
subcutaneous
sublingual
inhalation
rectal
41
Q

transdermal

A

administered onto the skin

42
Q

intramuscular

A

administered by injecting into a muscle

43
Q

intravenous

A

administer by injecting into a vein

44
Q

sublingual

A

under the tongue

45
Q

subcutaneous

A

administered by injecting under the skin

46
Q

two main ways drugs are delivered

A

enteral

parenteral

47
Q

enteral

A

via GI

48
Q

pareteral

A

not via GI

49
Q

ways drugs are absorbed via enteral delivery

A

passive diffusion
facilitated diffusion
active transport
pinocytosis

50
Q

passive diffusion

A

small non-ionic or unionised lipophilic drugs

51
Q

facilitated diffusion

A

using solute carrier proteins (SLC)

  • organic nation transports (OAT)
  • organic cation transporters (OCT)
52
Q

OAT

A

organic nation transports

53
Q

OCT

A

organic cation transporters

54
Q

what may affect drug action

A

first pass metabolism in the stomach and liver via enzymes such as cytochrome p450

55
Q

active transport

A

primary with SLC or secondary with pre-eastibliashed conc gradient using co-transport

56
Q

pinocytosis

A

large molecules like B12

57
Q

what may affect enteral absorption

A

metabolism and contents of the gut

58
Q

bioavailability

A

fraction of drug entering circulation after first pass hepatic metabolism

59
Q

what is the most common reference compartment used in bioavailability

A

CVS compartment bioavailability reference – IV bolus= 100% (no physical/metabolic barriers to overcome)

60
Q

Foral =

A

amount reaching systemic circulation oral/ Amount reach systemic circulation IV

= AUCoral/AUCIV

61
Q

volume of distribution =

A

vd= urgence dose/ [plasma drug]

62
Q

Kd

A

concentration at which 50% of drug binds tor eceptor

63
Q

Bmax

A

concentration at which 100% binding is achieved

64
Q

when there are extra receptors

A

fulll effect may be at 30% bidnding

65
Q

EC50

A

dose at which 50% of the effect is achieved

66
Q

phase 1 of drug metabolism

A

oxidation, reduction and hydrolysis (adds COOOh,- OH and NH2)
–> cytochrome P450 enzyme (CYP450)

67
Q

CYP450 en zyme

A

can be induced or inhibited by various drugs

68
Q

phase 2 of drug metabolism

A

conjugation (adds extra molecules to drug, usually glucoronate)

69
Q

drug excretion

A

permanent removal of drug from body

70
Q

drug excretion is usually

A

renal

  • glomerular filtration
  • proximal tubular secretion
  • distal tubular reabsorption
71
Q

drug excretion may also occur through

A

GI tract, sweat, tears, skin

72
Q

clearance is the

A

rate of elimination

73
Q

total clearance is

A

real clearance e+ hectic clearance

74
Q

linear or first order kinetics means that

A

clearance psi dependent on conc (has a half life)

75
Q

non linear or zero order or saturated kinetics means

A

clearance is independent of concentration (no half life)

76
Q

some drug shave …… at low conc and …… at high conc

A

first order kinetics at low cocnentrations

zero order kinetics at high cocnentrations

(enzymes relevant to clearance become saturated at higher concentrations)

77
Q

ligand

A

molecule that binds to a receptor

78
Q

affinity

A

likelihood of ligand binding to receptor

79
Q

efficacy

A

producing an effect when ligand is bound

80
Q

potency

A

the product of affinity and efficacy

81
Q

intrinsic activity

A

ability of the agonist to activate the receptor

82
Q

agonists

A

ligand with affinity and efficacy

83
Q

partial agonist

A

ligand with affinity and particle effaces

84
Q

antagonist

A

ligand with affinity but no efficacy

85
Q

reversible competitive antagonist

A

affinity to natural ligand binding site (orthosteric)

  • reversible
  • no efficacy
86
Q

irreversible competitive antagonist

A

affinity to natural ligand binding site (orthosteric)

  • non reversible
  • no efficacy
87
Q

non competitive antagonist

A

affinity to allosteric site

  • no efficacy
  • can be reversible and non reversible
88
Q

non reversible

A

due to to covalent bonds

89
Q

reversible

A

due to non-covalent bonds

90
Q

what is salbutamol used to treat

A

bronchospasm in asthma

- administered via inhalation

91
Q

salbutamol has affinity to

A

B2 adrenergic receptors in bronchi

  • Has efficacy
  • B2 agonists
92
Q

which GPC does salbutamol effect

A

Gs

93
Q

outline Gs stimulation via salbutamol

A

1) Salbutamol binds to Gs GPCR
2) GTP for GDP exchange
3) Separation of a and BY subunits
4) a-GTP subunit activates adenlyly cyclase
4) increase in cAMP
5) activation of PKA
6) causes inhabitation of myosin phosphorylation
7) smooth muscle relax
8) easier to rbeath

94
Q

adrenaline autoinjector (EpiPen)

A

treatment of anaphylaxis and anaphylactic shock

95
Q

how is EpiPen administered

A

intramuscular injection to lateral middle thigh

96
Q

EpiPen has an affinity to

A 
adrenergic receptor (agonists)
- reversible

Revision lectures (Year 1) (17 decks)

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