Pharmacology Flashcards

(94 cards)

1
Q

what activates adenylyl cyclase

A

coupling through Gs protein

Sympathetic

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2
Q

what does coupling through Gi cause

A
  • decreases activity of of adenylate cyclase and reduces [cAMP]
  • opens potassium channels to cause hyperpolarization of SA node
    parasympathetic
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3
Q

what is the inward current/funny current

A

current activated by hyper polarisation and cAMP

carried by sodium

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4
Q

what does blockage of the HCN channel cause

A

decrease in the slope of the pacemaker potential and reduces HR

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5
Q

what do hormones that increase cAMP also do

A

increase HR

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6
Q

how does sympathetic stimulation increase contractility

A

increases phase 2 cardiac AP
enhanced Ca++ entry
increases sensitivity of contractile protein to Ca++

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7
Q

how does sympathetic stimulation decrease duration of systole

A

increased uptake of Ca2+ into the SR

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8
Q

how does parasympathetic stimulation decrease contractility

A

decrease phase 2 cardiac AP

decreased Ca++ entry

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9
Q

how does parasympathetic stimulation decrease conduction in AV node

A

decreased activity of voltage-dependent Ca2+ channels and hyperpolarization via opening of K+ channels

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10
Q

what is located in the t-tuble membrane

A

voltage-gated L-type Ca channels (DHP receptors)

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11
Q

what does calcium activate and what occurs

A

the myofilaments and contraction occurs

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12
Q

how is Ca removed from the cytoplasm

A

SERCA

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13
Q

when is isoprenaline used

A

as a treatment for bradycardia

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14
Q

what does isoprenaline cause

A

bigger calcium ‘transients’

bigger and faster twitches

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15
Q

what is the function of voltage gated calcium channel

A

trigger’ calcium plateau phase of action potential

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16
Q

how is voltage gated calcium channels gated

A

phosphorylated by protein kinase A
increases trigger calcium
increases Ca induced Ca release

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17
Q

what is the function of ryanodine receptors and how is it regulated

A

Ca-induced Ca release from SR

Regulated by protein kinase A

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18
Q

what is the function of troponin

A

regulates actin/myosin interaction using calcium

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19
Q

what phosphorylates troponin and how does the affect it

A

protein kinase A

reduces its affinity for Ca - accelerates relaxation

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20
Q

how do hormones increases FOC

A

increase cAMP and activate PKA

increase Ca influx and release

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21
Q

how do hormones shorten the contractile cycle

A

increase cAMP and activate PKA

increase Ca reuptake

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22
Q

what are the effects of beta-adrenoceptor agonist

A

↑ Force, rate, CO, O2 consumption

↓ cardiac efficiency

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23
Q

what are side effects of beta-adrenoceptor agonist

A

arrhythmias

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24
Q

when is adrenaline used

A

cardiac arrest

anaphylactic shock

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25
drug selective for beta1-adrenoceptors and when is it used
Dobutamine | acute heart failure
26
what is a non-selective beta blocker
propranolol
27
what are beta-adrenoceptor antagonist
beta-blockers
28
what are selective beta 1 blockers
atenolol
29
what does Digoxin do
increases contractility of the heart by blocking the SARCOLEMMA Na/K ATPase
30
what happens in the presence of digoxin
Na+/K+ATPase blocked | ↑storage of Ca2+ in SR
31
what is the effect of digoxin on action potentials
shortens AP and refractory period in myocytes - useful in HF coupled with AF
32
side effects of digoxin
heart block | dysrhytmias
33
what are examples of inotropes
digoxin, levosimendan
34
what channels does calcium enter through
L-type Ca2+ channel | GPCR coupled to Gq/11
35
what is the steps to contraction
``` 1 - Ca2+ enters the cell 2 - binds with Calmodulin 3 - Ca-CaM binds with MLCK 4 - active MLCK causes myosin-LC to phosphorylate 5 - contraction ```
36
what is the steps to relaxation
1 - cGMP binds with Myosin-LC-phosphatase 2 - myosin-LC-phosphatase becomes active 3 - dephosphorylates myosin-LC 4 - relaxation
37
what are side effects of organic nitrates
headaches hypotension collapse
38
which organic nitrate is resistant to first-pass metabolism
isosorbide mononitrate
39
what is the receptor for endothelin-1
ETa receptor
40
renin inhibitor
aliskiren
41
what do ACEi cause
``` venous dilatation (↓preload) arteriolar dilatation (↓afterload and ↓TPR) decreasing BP and cardiac load ```
42
ACEi increases contractility - true or false
false | has no affect on contractility
43
when does ACEi especially cause hypotension
in combination with diuretics
44
when should ARB and ACEi not be used
Pregnancy | Bilateral renal artery stenosis
45
what do beta 1 blockers do
decrease myocardial oxygen requirement | decreases duration of diastole
46
how do beta blockers help restore normal BP
reduce CO | reduce renin release
47
what do calcium antagonist interact with and where are they
L-type calcium channels | in the heart and smooth
48
what are the three main types of calcium antagonist
amlodipine, verapamil, diltiazem
49
what is an immediate selective calcium antagonist
diltiazem
50
when are calcium channel blockers used
Hypertension Angina Dysrhythmias
51
alpha blockers
prazosin | doxazosin
52
what is the pathway of platelet reactions following endothelial damage
``` 1 - endothelial damage 2 - adhesion, activation and aggregation of platelets 3 - secretion and synthesis of mediators 4 - further aggregation of platelets 5 - fibrin clot ```
53
what are the mediators excreted by platelets
ADP TXA2 5-HT
54
what factors cause further aggregation of platelets
Thrombin (IIa) | Fibrinogen
55
what is the pathway of blood coagulation following endothelial damage
1 - endothelial damage 2 - VIIa, XIIa, XIa cause conversion of X to Xa 3 - Xa causes conversion of Prothrombin (II) to Thrombin (II) 4 - Thrombin causes conversion of fibrinogen to fibrin 5 - fibrin clot
56
what are the clotting factors
Prothrombin (II), VII, IX and X
57
what are the serine proteases
Thrombin (IIa), VIIa, IXa and Xa
58
what are the stages of conversion by Vit K reductase
1 - vitamin K oxidised form - epoxide 2 - vitamin K - quinone 3 - vitamin K reduced form - hydroquinone
59
what does warfarin do
competes with vit K for binding to vit K reducatse preventing conversion of epoxide to hydroquinone
60
what factors does warfarin render inactive
II, VII, IX and X
61
what is an inhibitor of coagulation
Antithrombin III
62
what does Heparin do
bind to ATIII increasing its affinity for Xa and IIa to increase rate of inactivation
63
Heparin must bind to both AT III and IIa to inhibit IIa - true or falee
true
64
Heparin needs to bind to AT III and Xa to inhibit Xa - true of false
false | only needs to bind to ATIII
65
what does LMWH inhibit
factor Xa | still works as Xa upstream
66
side effects of heparin and LMWH
haemorrhage osteoporosis hypoaldosteronism
67
orally active inhibitors
dabigatran etexilate - inhibitts thrombin | rivaroxaban - inhibits Xa
68
what is the mechanism of action of aspirin
irreversibly blocks COX preventing TXA2 synthesis and production of prostaglandin I2
69
what is the mechanism of clopidogrel
Links to P2Y12 receptor
70
when is tirofiban given
IV to prevent MI in patients with unstable angina
71
what causes plasminogen to convert to plasmin
endogenous tissue plasminogen activator
72
what is the role of plasmin
converts fibrin to fibrin fragments | leading to clot lysis
73
what are Alteplase and duteplase
recombinant tissue plasminogen activator (rt-PA)
74
how can the risk of haemorrhage from fibrinolytic be controlled
tranexamin acid | inhibits plasminogen activation
75
what should a CCB never be given in
Heart Failure
76
what is given to treat valvular AF
warfarin
77
why should organic nitrates not be stored in a clear bottle
as they are photosensitive and are rendered useless
78
what are side effects of statins
muscle aches
79
side effects of nicorandil
mouth ulcers
80
what is a potassium sparing diuretic
Triamterene Spironolactone Eplerenone
81
side effects of digoxin
``` elderly patients with renal impairment can get toxicity Digoxin Toxicity Nausea, vomiting Yellow vision Bradycardia, Heart Block Ventricular Arrhythmias ```
82
what does spironolactone block
aldosterone
83
what are anti anginal drugs
Beta Blockers Calcium Antagonists Nitrates Nicorandil
84
what are diuretic side effects
hypokalaemia (tired + arrhytmias) hyperglycaemia (diabetes) increase uric acid (gout) impotence
85
when are cardioselective beta blockers used
angina, hypertension, heart failure
86
when is nonselective beta blockers used
thyrotoxicosis/hyperthyroidism
87
what are the two types of CCB
Dihydropyridines - Amlodipine | Rate limiting calcium antagonist - verapamil, diltiazem
88
what do alpha blockers do and when are they used
Block α adrenoceptors to cause vasodilatation | Hypertension, prostatic hypertrophy
89
side effects of alpha blocker
postural hypotension
90
what are SE of anti platelet agents
Haemorrhage Peptic ulcer Aspirin sensitivity in Asthma
91
when are fibrinolytic drugs not to be used
``` recent haemorrhage trauma bleeding tendencies severe diabetic retinopathy peptic ulcer ```
92
what is used to treat Supraventricular Arrhythmias in acute phase
Adenosine
93
what is used to treat Ventricular/Supraventricular Arrhythmias
Amiodarone Beta Blockers Flecainide
94
what are the side effects of anti-arrhythmic drugs
phototoxicity pulmonary fibrosis thyroid abnormalities (hypo or hyper)