ICPP (12-17) Flashcards

(96 cards)

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
the ANS is not
Under conscious contro
26
Main devious for he ANS
Sympathetic and aradymapthetic
27
Sympathetic
Fight or flight
28
Parasympathetic
Rest and die gets
29
Preganglionic neuron release
ACH into nicotinic acetyl choline receptor in post ganglionic neuron
30
Sympathetic (fight or flight)
- thoracolumbar emergence - ganglaite in peruses paravertebrally or elsewhere - medium pre - Long post - Release NA into a1, a2, B2 adrenoreceptors
31
Parasympathetic (rests and digest)
Cranial sacral (top and bottom) eme3rgence - ganglia at the target organ - long pre - short post - release ACH into M1 and m2 and M3 mACHr
32
What breaks ACetyl choline down
Acetylcholineesterase
33
What makes ACH
Actetycholinetransferase
34
How is adrenaline male
Catecholamine synthesis - tyrosine -> DOPA —> dopamaine —> NA —> A
35
What breaks down cytoplasmic NA
Monoamine oxidase (MAO)
36
adrenoceptor agonists
increase sympathetic stimulation
37
adrenoceptor antagonists
decrease sympathetic stimulation
38
muscarinic cholinoceptor agonists increase
parasympathetic stimulation
39
muscarinic cholinoceptors antagonists
decrease parasympathetic stimulation
40
name 9 ways drug can be administed
``` oral intravenous intramusuclar transdermal intranasal subcutaneous sublingual inhalation rectal ```
41
transdermal
administered onto the skin
42
intramuscular
administered by injecting into a muscle
43
intravenous
administer by injecting into a vein
44
sublingual
under the tongue
45
subcutaneous
administered by injecting under the skin
46
two main ways drugs are delivered
enteral parenteral
47
enteral
via GI
48
pareteral
not via GI
49
ways drugs are absorbed via enteral delivery
passive diffusion facilitated diffusion active transport pinocytosis
50
passive diffusion
small non-ionic or unionised lipophilic drugs
51
facilitated diffusion
using solute carrier proteins (SLC) - organic nation transports (OAT) - organic cation transporters (OCT)
52
OAT
organic nation transports
53
OCT
organic cation transporters
54
what may affect drug action
first pass metabolism in the stomach and liver via enzymes such as cytochrome p450
55
active transport
primary with SLC or secondary with pre-eastibliashed conc gradient using co-transport
56
pinocytosis
large molecules like B12
57
what may affect enteral absorption
metabolism and contents of the gut
58
bioavailability
fraction of drug entering circulation after first pass hepatic metabolism
59
what is the most common reference compartment used in bioavailability
CVS compartment bioavailability reference – IV bolus= 100% (no physical/metabolic barriers to overcome)
60
Foral =
amount reaching systemic circulation oral/ Amount reach systemic circulation IV = AUCoral/AUCIV
61
volume of distribution =
vd= urgence dose/ [plasma drug]
62
Kd
concentration at which 50% of drug binds tor eceptor
63
Bmax
concentration at which 100% binding is achieved
64
when there are extra receptors
fulll effect may be at 30% bidnding
65
EC50
dose at which 50% of the effect is achieved
66
phase 1 of drug metabolism
oxidation, reduction and hydrolysis (adds COOOh,- OH and NH2) --> cytochrome P450 enzyme (CYP450)
67
CYP450 en zyme
can be induced or inhibited by various drugs
68
phase 2 of drug metabolism
conjugation (adds extra molecules to drug, usually glucoronate)
69
drug excretion
permanent removal of drug from body
70
drug excretion is usually
renal - glomerular filtration - proximal tubular secretion - distal tubular reabsorption
71
drug excretion may also occur through
GI tract, sweat, tears, skin
72
clearance is the
rate of elimination
73
total clearance is
real clearance e+ hectic clearance
74
linear or first order kinetics means that
clearance psi dependent on conc (has a half life)
75
non linear or zero order or saturated kinetics means
clearance is independent of concentration (no half life)
76
some drug shave ...... at low conc and ...... at high conc
first order kinetics at low cocnentrations zero order kinetics at high cocnentrations (enzymes relevant to clearance become saturated at higher concentrations)
77
ligand
molecule that binds to a receptor
78
affinity
likelihood of ligand binding to receptor
79
efficacy
producing an effect when ligand is bound
80
potency
the product of affinity and efficacy
81
intrinsic activity
ability of the agonist to activate the receptor
82
agonists
ligand with affinity and efficacy
83
partial agonist
ligand with affinity and particle effaces
84
antagonist
ligand with affinity but no efficacy
85
reversible competitive antagonist
affinity to natural ligand binding site (orthosteric) - reversible - no efficacy
86
irreversible competitive antagonist
affinity to natural ligand binding site (orthosteric) - non reversible - no efficacy
87
non competitive antagonist
affinity to allosteric site - no efficacy - can be reversible and non reversible
88
non reversible
due to to covalent bonds
89
reversible
due to non-covalent bonds
90
what is salbutamol used to treat
bronchospasm in asthma | - administered via inhalation
91
salbutamol has affinity to
B2 adrenergic receptors in bronchi - Has efficacy - B2 agonists
92
which GPC does salbutamol effect
Gs
93
outline Gs stimulation via salbutamol
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
adrenaline autoinjector (EpiPen)
treatment of anaphylaxis and anaphylactic shock
95
how is EpiPen administered
intramuscular injection to lateral middle thigh
96
EpiPen has an affinity to
``` adrenergic receptor (agonists) - reversible ```