pac Flashcards
(131 cards)
1
Q
PNS mechanism
A
Ach from CNS/brain neurons - on Nicotinic receptors N - postganglionic fiber release Ach - M3 on exocrine glands & M3 smooth muscle & M2 heart/ muscarinic receptor
2
Q
Muscarinic receptor
A
M2 on heart - G-protein coupled receptor -for Ach
3
Q
cholinergic synapse
A
Ach release
4
Q
SNS mechanism
A
Ach from CNS/ spinal cord neurons -
neuronal Nicotinic Nn receptors on post ganglion - release NE - on the Alpha-1 R on smooth muscle & beta-1 R on heart
N R on adrenal medulla - releasing N and NE in blood
5
Q
NE = NA
A
NorEpinephrine = NorAdrenaline
6
Q
Nicotinic receptors subtypes
A
Nn - nicotinic subtype - the postganglionic neuron - SNS &
Nm - muscle subtype -somatic
7
Q
autonomic nervous system
A
Ach from pre-synaptic - cholinergic - on Nn & muscarinic R & AChe & presynaptic autoreceptor
8
Q
somatic nervous system
A
spinal cord - somatic nerves - Ach - Nm on skeletal muscle
9
Q
AChe
A
primary Ach break down = acetate + choline
10
Q
cholinergic synapse
A
where the Ach is released
11
Q
primary breakdown methods -
A
NE = uptake to presynaptic neuron - Catechol-O-methyl-transferase ACh = AChE - enzyme
12
Q
adrenergic transmission
A
alpha-beta R
presynaptic autoreceptors
primary -reuptake into nerve terminal - catechol-o-methyl-transferase
uptake to tissue - monoamine oxidase MAO
13
Q
NE making
A
Tyrosine - DOPA -dopamine - NE
14
Q
ANS tone
A
basal level of activity (basic life function) - parasympathetic or sympathetic
15
Q
organs with single system control - SNS
A
adrenal gland- release EP
blood vessels - vasoconstriction - gut, skin - Alpha 1 R
blood vessel - vasodilation - skeletal muscle - beta 2 R
16
Q
heart rate PNS vs SNS
A
inc - SNP - beta 1 R by NE
dec - PNS - muscarinic M2 R by Ach
17
Q
respiratory bronchi SNS vs PNS
A
SNS - bronchodilation - beta 2 R
PNS - bronchoconstriction -
18
Q
beta 2 receptor
A
SNS - dilation of vessel and bronchi
19
Q
drugs used for myasthenia gravis and Alzheimers
A
cholinesterase inhibitors
20
Q
ATROPINE
A
non-selectiv muscarinic antagonist
21
Q
M2 receptor
A
GCPR - activates Gi [inhibitory G protein] - dec cAMP
22
Q
nicotinic antagonist use
A
in surgery - intubation - relaxing muscle
23
Q
beta2-Receptor
A
treating asthma - dilate bronchi
24
Q
alpha 2 receptor
A
feedback inhibition - dec NE release
25
alpha 1 R
GPCR - acting through Gq - inc Ca - vasoconstriction - inc BP
26
beta 1 R
GPCR - Gs - inc cAMP - inc Ca - inc Heart force rate
27
alpha 1 agonist
vasoconstriction - inc BP
| dilate pupil
28
COCAINE
blocking NE reuptake
29
AMPHETAMINE
release NE from terminal
30
PRAZOSIN
alpha 1 antagonist - dec BP
31
propranolol
beta 1, 2 antagonist - hypertension, angima, arrhythmia, heart failure
32
lipoprotein[lipid protein complex] classes
```
chylomicron
VLDL
LDL
HDL
(high-low size / triglyceride trend)
```
33
highest TG
chylomicrons
34
highest CHOL
| how
LDL
get most of CHOL of VLDL
bad cholesterol
35
hepatic cholesterol
biosynthesis
catabolism
```
Acetyl CoA - HMG-CoA - HMG-CoA reductase/rate limiting - cholesterol (can also be secret to bile as cholesterol)
bile acid (secreted to bile)
```
36
chylomicrons mechanism
intestine - dietary lipid - LPL / capillary endothelial cells lipolysis -- Fas - tissue - energy utilization / oxidation & energy storage / triglyceride biosynthesis
remnants - liver endocytosis
37
lipoprotein with;
majority of serum triglyceride
most TG
VLDL
| Chylomicron
38
VLDL mechanism
liver - LPL lipolysis / capillary peripheral tissue - Fas - tissue - energy storage and utilization
remanent VHDL = IDL - removal of apolipoprotein & lipolysis of triglyceride - LDL / blood
39
intermediate density lipoprotein
IDL is the VLDL remanent
40
LDL
from the IDL - LDL - peripheral tissue + 50% liver /endocytosis
41
immature HDL
apolipoproteins [ApoAI, ApoAll] + phospholipids
42
HDL
liver - HDL immature - during VLDL & chylomicrons lipolysis get lipid/cholesterol + get cholesterol from peripheral tissue - uptake by SR-BI - liver - bile acid - bile / or can directly from cholesterol add to bile - excursion
43
bad
good
cholesterol
LDL
| HDL
44
hyperlipoproteinemias
heterogenous group of disorders
can be monogenic , polygenic/common,
differ based on cause, lipoprotein affected, cholesterol and most important their CVD risk increase
45
hyperlipoproteinemias
based on the lipoprotein affected determine which lipid will elevate in blood
46
hypercholesterolemia
hypertriglyceridemia
mixed hyperlipidemia
major inc in;
LDL
VLDL
VLDL + LDL
47
disease associated with high cholesterol = high CVD
| bad cholesterol = LDL
hypercholesterolemia
| hyperlipidemia
48
treatments for the CVD
achieve lower LDL cholesterol l
49
atherosclerosis
red blood flow
CVD, stroke, kidney failure
severity with again genetic
high LDL - primary risk factor
50
atherosclerosis risk relation
+ LDL:HDL, total cholesterol, LDL
| - HDL / inverse cholesterol transport mechanism
51
TLC
Therapeutic life style change
| 10-30% LDL red
52
statin
open lactose ring
competitive inhibitor of HMG CoA reductase
primary action = inc hepatocyte LDL receptors -
53
statin use
most effective for dec LDL
primary prevention of CVD
anti-inflammation - anti-coagulant
54
statin adverse effects
muscle pain
reversible liver toxicity
cardiomyopathy
drug interaction
55
bile acid binding resins
anion exchange resins
| in small intestine
56
resin bile acid function
- excreted in feces
- red intestinal-bile acid reabsorption & return to liver
- red liver bile acid - inc Bile acid biosynthesis in liver - dec hepatic cholesterol
- inc LDL receptor - inc hepatic LDL uptake
- lower blood LDL
- dec plasma total cholesterol and LDL
57
resin side effect
diarrhea, constipation, irritation
58
resins inc chol in liver
1- inc LDL R on liver
| 2- inc biosynthesis of cholesterol - so statin is used with resin to inhibit HMG CoA - cholesterol biosynthesis
59
cholesterol absorption inhibitor
inhibit internalization of sterol-bound NPC1L1
60
NPC1L1
Niemann-Pick C1-Like 1
| on luminal face of enterocyte - bind& internalize sterol in small intestine - absorption of CHOL
61
EZETIMIBE
cholesterol absorption inhibitor drug
62
ezetimibe mechanism
red cholesterol-chylomicron delivery to liver - red hepatic chol -inc LDL R - inc LDL uptake to liver - dec total and LDL chol-
63
ezetimibe function benefits
primary; dec LDL cholesterol
dec TG
in HDL cholesterol
64
ezetimibe adverse effect - rare
reversible impaired liver function
| myositis/muscle inflammation
65
PCSK9 inhibitor
newest LDL lowering drug
monoclonal antibodies - injection
second line medication - narrow usage indication
with diet & max statin therapy
66
PCSK9 inhibitor usage
sever hypercholesterolemia
| atherosclerotic CVD - max statin used but need further LDL lowering
67
PCSK9
Proprotein Convertase Substilisin/Kexin type 9
| enzyme
68
PCSK9 -inhibitor mechanism
monoclonal antibodies - bind to PCSK9 - inhibit PCSK9 attach to LDL receptor - LDL R internalized & not degrade - LDL degraded - inc LDL R on hepatocyte - Inc LDL uptake from blood
69
niacin mechanism
in adipose tissue - niacin bind niacin receptor - inhibit hormone-sensitive lipase = lipolysis of TG- dec plasma fas - dec hepatic triglyceride synthesis - red VLDL synthesis - red plasma LDL
red apoA-1 clearance from plasma = inc apolipoprotein - inc HDL - inc reverse cholesterol transport = cholesterol excursion in bile
70
niacin function
inc HDL
| dec LDL & total chol
71
niacin usage
niacin + other drugs = hyperlipidemia
72
niacin adverse effect
high does
| flushing, hot flush, GIT irritation, hepatotoxicity
73
fibrates
used for;
| high TG and low HDL
74
vibrates are
PPAR alpha
75
PPAR alpha
Peroxisome Proliferator Activated Receptor Alpha
76
fibrates
PPAR alpha agonist
77
PPAR Alpha
ligand activated transcription factor
78
PPAR alpha function
inc expression gene involved in lipid metabolism;
endothelial lipoprotein lipase;
hepatic and muscle fas oxidation enzyme ;
hepatic apo A-I & apo A-II;
79
Fibrate - inc Endothelial Lipoprotein Lipase
inc clearance chylomicrons/VLDL;
- dec TG plasma
- inc Fas - uptake and oxidation in muscle
80
fibrate - inc hepatic fas oxidation enzyme
dec TG biosynthesis - dec VLDL secretion -
| dec plasma TG
81
fibrate - inc hepatic apo A-I and apo A-II
inc plasma HDL
82
treatments;
hypercholesterolemia; high LDL
hyperglyceridemia; high VLDL
hyperlipidemia; LDL+ VLDL
- TLC, niacin, resin, statin, ezetimide, PCSK9-inhibitor
- TLC, niacin, fibrate
- TLC, niacin, fibrate, resin, statin, PCSK9 inhibitor
83
homozygote hypercholesterolemia
min effect to resin, statin or combination
| TLC+Niacin - effective
84
hypertension
| High BP
systolic BP > 140 mmHg
| diastolic BP > 90 mmHg
85
RAS
Renin Angiotensin System
86
RAS mechanism
Angiotensinogen - Renin - angiotensin I - ACE -Angiotensin II - receptors on;
vascular - vasoconstriction
adrenal glands - aldosterone - inc NA H2O - inc blood volume
87
diuretics
naturiesis + diuresis
88
loop and thiazide diuretics
loss of NA and K /excretion
| hypokalemia
89
K sparing diuretics
loss of Na
gain of K in blood - less excretion
hyperkalemia
90
diuretics for diseases;
thiazide
k sparing
Loop
hypertension
CHF
CHF
91
CHF
Congestive Heart Failure
92
sympatholytic drugs
| not first line drugs
centrally-acting; dec SNS, central vasometer centre in brain, dec BP
beta-blockers;
short term, beta 1 blockers in heart, dec HR, contraction, CO, BP
long term, beta 1 blocker in kidney, vasodilation, dec renin, aldosterone, NA+H2O, BP
alpha1-blocker; blocking SNS acting on vascular smooth muscles, vasodilation, red BP
93
orthostatic hypertension is
adverse effect of alpha 1 blocker
94
angiotensin inhibitors RAS
| first line drugs
1- ACE inhibitor ACE-I ; dec AI to AII - dec AII - vasodilation, dec BP, Na
2- All(angiotensin II) antagonist;
block AII R on vessel, vasodilation, dec BP
block AII R on adrenal gland, dec aldosterone, NA, BP
3- direct renin inhibitor; dec AI or AII
95
vasodilator
| first line drug
Ca channel blocker; CCB
Nifedipine; act on blood vessel
diltiazem & verapamil; act on blood vessel and heart
dec ca, dec contraction, vasodilation - dec BP
heart - dec HR, CO = dec BP
96
first line drugs - commonly used
Thiazide, ACE-I, ARB, CCB
97
Orthostatic hyportension
head rush
| alpha 1 blocker
98
ACE Inhibitor = ACE-I
cough, teratogenic
99
AII antagonist ARB
no cough, teratogenic
100
MI
myocardial infraction
101
coronary arteries diseases treatment
aspirin ; red clot
| statin ; red LDL
102
ASA
Aspirin - red platelet aggregation
| anti-thrombotic
103
vasodilator
organic nitrates
104
NITROGLYCERIN
organic nitrate for vasodilation
105
nitrate/nitroglycerin mechanism
nitrate, nitric oxide in VSM, activate enzyme Guanylyl cyclase, convent GTP to CGMP, dec phosphorylation of myofilament, relax blood vessel
106
nitroglycerin & sildenafil drug interaction
sildenafil; inhibit CGMP to GMP conversion by phosphodiesterase PDE = inc CGMP, - high dec in BP
107
calcium channel blockers CCB
nifedipine; in VSM, dilate vessel, dec vasospasm = inc o2 supply- dilate arteries, dec afterload = dec o2 demand
verapamil & diltiazem;
dec O2 demand and Inc O2 supply; in VSM -
in heart;
dec contraction =dec work, dec HR =dec O2 demand
108
beta blocker
dec O2 demand;
| dec HR, contraction, after load (RAS), work of heart
109
SNS and RAS remodelling
hypertrophy
apoptosis
fibrosis
dilation
110
CHF drugs
positive inotropic drugs; inc contraction, CO
inhibit RAS; ARBs & ACEIs; red remodelling
inhibit SNS; beta-blocker; red remodelling
aldosterone antagonists/K sparing & other diuretics/loop; red pulmonary & systemic congestion
vasodilator; dec pre-load & after-load
111
carvedilol
beta1,2 - alpha 1 blocker
beta1 blocker= dec HR, renin
beta 2 blocker = asthma not good
alpha 1 blocker =vasodilation - dec after load
112
ICD
Implantable Cardioverter-Defibrillator
113
drugs classes fro tachycardias
```
class I; Na channel blocker
Class II; Beta blocker
class III; K channel blocker
class IV; Ca channel blocker = diltiazem, verapamil
other; digoxin
```
114
tachycardias drugs with similar effect
class II, IV, other like adenosine and digoxin
115
synthesis;
Ach
NE
acetyl coa + choline = Ach
| tyrosine- dopa - dopamine- NE
116
NE degradation adrenergic
uptake to pre-synapse; catechol-O-methyl-transferase
| uptake to post-synapse; monoamine oxidase
117
indirect agonist of Ach cholinergic
for Alzheimer and myasthenia gravis
118
agonists;
cholinergic
adrenergic
indirect;
inhibit AChE
inhibit NE reuptake & inc NE release
119
alpha 1 R
vasoconstriction - inc BP
| dilate pupil
120
```
drugs;
atropine
cocaine
amphetamine
prazosin
propranolol
```
muscarininc antagonist -non-selettive - cholinergic antagonist
inhibit NE reuptake - adrenergic indirect agonist
amphetamine - inc NE secretion - indirect adrenergic agonist
alpha-1 antagonist - red BP - adrenergic antagonist -selective
beta antagonists - non-selective - adrenergic antagonist
121
HDL
liver -immature; Apolipoproteins [apoAl, appall] + phospholipid
acquire cholesterol;
-during lipolysis of chylomicrons & VLDL
-from peripheral tissue
122
statin mechanism
for high LDL patients;
- inhibitor of HMG CoA reductase
- so the hepatic cholestrol drops
- liver makes more LDL receptors - dec LDL blood
123
statin drug
best for LDL lowering
| primary prevention of CVD
124
resin combination
with statin
| to dec the cholesterol biosynthesis
125
ezetimibe
cholesterol absorption inhibitor
| inhibit internalization of sterol-bound NPC1L1
126
PCSK9 inhibitor
new for LDL lowering - severe heterozygous hypercholesterolemia
combine with max statin and diet
monoclonal antibodies
second line
127
niacin mechanism
inhibit TG lipolysis - dec Fas, hepatic TG, VLDL, LDL
| red apoA-I clearance - inc HDL
128
fibrate
best for high TG & red HDL
| PPARalpha agonists
129
PPARalpha
transcription factor - inc gene expression for lipid metabolism;
endothelial lipoprotein lipase
fatty acid oxidation
apo A-I apo A-II
130
RAS renin angiotensin system
angiotensinogen
Renin
AI
Angiotensin-Converting Enzyme ACE
All
1- AII R on the vessel - vasoconstriction
2-AII R on adrenal gland - aldosterone - inc Na + H2O - inc Blood volume
131
k sparing diuretic
aldosterone antagonist
