Pharmacology Flashcards

1
Q

Where is the fast response action potential present in?

It is _____ dependent

A
  • atrial and ventricular muscles

- sodium dependent

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2
Q

Explain phases 0-4 action potentials FAST RESPONSE

A

Phase 4 - outward flux of K is dominant
Phase 0 - upstroke, inward flux of Na+ is dominant
Phase 1 - early repolarisation, outward flux of K+ is dominant
Phase 2 - plateau, inward flux of Ca2+ balanced by outward flux of K+
Phase 3 - final depolarisation, outward flux of K+ is dominant

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3
Q

Where is the slow response action potential present in?

It is _____ dependent

A
  • SA, AV node

- calcium dependent

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4
Q

Explain phases 0-4 action potentials SLOW RESPONSE

A

Phase 4 - outward flux of K+, reduced by inward flux of Na+ and Ca+
Phase 0 - opening of L-type Ca2+ channels
Phase 3 - opening of delayed rectifier K+ channels

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5
Q

Sympathetic system effect on the heart
? post ganglionic transmitter
? receptor
? coupled protein

A
  • NA
  • B1 adrenoreceptor
    -Gs coupled protein
    Increase the intracellular cAMP
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6
Q

Parasympathetic system effect on the heart
? post ganglionic transmitter
? receptor
? coupled protein

A
  • Ach
  • M2 muscarinic receptor
  • Gi coupled
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7
Q

Meaning of inotropic?

A

Heart contractility

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8
Q

Meaning of chronotropic?

A

Heart rate

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9
Q

Meaning of dromotropic?

A

conduction velocity in AV node

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10
Q

What does “If” represent

A
  • Funny current

- depolarising current

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11
Q

Explain the funny current

A
  • If
  • depolarising current
  • Na+ current
  • hyperpolarising activates HCN channels in SA node
  • Blocking HCN channels –> decreased HR
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12
Q

What is drug is used as an HCN blocker?

A
  • Ivabradine
  • Block HCN
  • Decreases HR
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13
Q

Explain the action of a beta 1 adrenoceptor agonist

A
  • activates Gs coupled receptor
  • ATP converted into cAMP by adenylyl cyclase
  • activates protein kinase A
  • this phosporylates Ca2+ channels
  • increased Ca2+ –> increased contracility
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14
Q

Examples of b adrenocepetor agonists

A
  • dobutamine
  • adrenaline
  • noradrenaline
  • all examples of catecholamines
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15
Q

What pharmacokinetics does b adrenoceptor agonists have?

A
  • increased force, rate and cardiac output

- decreased efficency

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16
Q

What is adrenaline used in?

A
  • b adrenoceptor agonist
  • cardiac arrest
  • anaphylactic shock
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17
Q

What is dobutamine used in?

A
  • acute potentialy reversible heart failure
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18
Q

b adrenoceptor antagonists examples and their pharmacokinetics

A

May be selective or non-selective beta blockers.
non selective - propranolol
selective - atenolol, bisoprolol

Pharmakinetics: little effect at rest, but during exercise stress, force, CO are depressed

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19
Q

Uses of b adrenoceptor antagonists (beta blockers)

A

treatment of disturbances of cardiac rhythm
treatment of angina
treatment of heart failure
treatment of hypertension

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20
Q

Adverse effects of beta blockers?

A
  • bronchospasm (asthmatics)
  • aggravation of cardiac failure
  • bradycardia
  • hypoglycaemia
  • cold extremities
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21
Q

What would a non-selective muscarinic ACh receptor antagonist be used for?

A
  • bradycardia when the heart rate is lower than 60bmp
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22
Q

What is an example of a muscarinic ACh antagonist?

A

Atropine

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23
Q

What is digoxin used for?

A

it is a cardiac glycoside that increases contractility of the heart
Example of an inotropic drug (causes a leftward shift in the SV, EDV curve)

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24
Q

What does digoxin inhibit to increase contractility?

A

It inhibits the sarcolemma ATPase

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25
Lipids are _____ in water a) insoluble b) soluble
a) insoluble
26
How are non-polar lipids transported in blood
They are transported within lipoproteins
27
What are the 2 types of lipoproteins
- High Density Lipoproteins (HDL) - Low Desnsity Lipoproteins (LDL) - VLDL - Chylomicrons
28
CVD is associated with elevated _______ Density Lipoproteins levels and decreased ________Density Lipoproteins
- Elevated LDL | - Decreased HDL
29
Explain the structure of a lipoprotein
- hydrophobic core | - hydrophillic coat
30
Explain the makeup of the hydrophobic core of a lipoprotein
- esterified cholestrol and triacyglycerols
31
Explain the makeup of the hydrophilic coat of a lipoprotein
- monolayer of amphiatic cholestrol, phospholipids and apoproteins
32
What are apoproteins
- recgonised by receptors in the liver and other tissues, allowing lipoproteins to bind to cells
33
4 classes of lipoproteins and their carrier apoprotein
- HDL particles (apoA-1 + apoA-2) - LDL particles (ApoB-100) - VLDL particles (ApoB-100) - chylomicrons (ApoB-48)
34
What Apoprotein is associated with LDL
apoB-100
35
What Apoprotein is associated with Chylomicrons
apoB-48
36
What Apoprotein is associated with HDL
apoA-1 + apoA-2
37
What do ApoB lipoproteins do?
- deliver TAGs to muscle for ATP biogensis | - adipocytes for storage
38
Where are chylomicrons formed and what is their pathway
- formed in interstinal cells | - exogenous pathway
39
Where are LDL formed and what is their pathway
- formed in the liver | - endogenous pathway
40
How are chylomicrons and VLDL particles activated?
- activated by the transfer of apoC-II from HDL particles
41
What apoprotein is involved in the metabolism of apoB lipoproteins
apoE | which is a high affinity ligand for receptor mediated clearance --> remnants
42
What is the definition of haemostasis?
- arrest of blood loss from a damaged vessel at the site of injury
43
What are the 3 main processes of haemostasis?
- vascular wall damage - primary haemostasis - activation of blood clotting
44
Explain what part vascular wall damage plays in haemostasis
- injury to vascular wall - collagen exposed - platelets bind to the collagen and become activated - activated platelets releases thromboxane A2 (TXA2)
45
What does TXA2 do in haemostasis?
- TXA2 binds to TXA2 GPCR receptors, releasing 5-HT (Serotonin) and ADP
46
What is serotonin role in haemostasis
causes vasoconstriction
47
What is ADP role in haemostasis
- released from TXA2 GPCR - binds to purine receptors (P2Y12) - Activates further platelets - expresses acidic phoshoplipid to form a solid clot
48
Explain the coagulation cascade
``` X --> activates IX and VIII II --> activates X and V Produces thrombin (IIa) thrombin cleaves fibrinogen --> fibrin fibrin --> solid clot ```
49
What cleaves fibrinogen to fibrin?
thrombin
50
What is thrombosis?
- pathological haemostasis | - forms a haematological plug in abscence of bleeding
51
What colour are arterial thrombus?
- white
52
What colour are venous thrombus?
- red
53
How do you treat arterial thrombus?
- anti-platelet | - asprin
54
How do you treat venous thrombus?
- anti-coagulant | - warfarin
55
What are the risks of anti-coagulants
- haemorrhage
56
What factors does Warfarin block?
II, VII, IX , X
57
What does heparin bind to?
- antithrombin III
58
Name 2 low molecular weight heparins?
- dalteparin | - enoxaprin
59
What factor does LMWH act on?
Xa
60
How do anti-platelet drugs work?
- prevents TXA2 synthesis
61
How do fibrinolytics work?
- fibrin broken down to firbin fragments | - reopens occluded arteries