Pharmacology Flashcards

1
Q

HCN/funny current blocker and what disease it is used for?

A

Ivabradine

Used for angina

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2
Q

Name a beta 1 agonist used sometimes in heart failure?

A

Dobutamine

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3
Q

Propranolol is a …. and atenolol and bisoprolol are ….?

A

Non-selective beta antagonist and selective beta 1 antagonist

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4
Q

Give some adverse effects of beta blockers?

A

Worsen asthma
Worsen heart failure (at high doses)
Cold extremities

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5
Q

Which class of drug is atropine + main use?

A

Muscarinic antagonist + bradycardia

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6
Q

Digoxin mechanism?

A

Blocks the Na/K ATPase which increases intraceullar Na which blocks Na/Ca exchange
Increased Ca causes increased contraction

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7
Q

Digoxin is toxic when used in people with…. and can also induce ….?

A

Hypokalaemia and arrhythmias

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8
Q

What does Levosimendan (used in heart failure) do?

A

Binds to troponin C to increase its affinity for Ca

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9
Q

What do nitrates combine with to liberate NO + what molecule do they activate to produce cGMP?

A

SH groups + guanyl cyclase

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10
Q

Give an example of a short-acting and long-acting nitrate + 2 main side effects?

A

GTN and isosorbide mononitrate + headache and hypotension

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11
Q

ACEi name ending + 2 CIs + 2 side effects?

A

Pril + renal artery stenosis and pregnancy + cough and hyperkalaemia

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12
Q

ARB name ending + 2 CIs + side effect?

A

Artan + renal artery stenosis and pregnancy + hyperkalaemia

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13
Q

CCBs are selective for which type of calcium channel?

A

L-type channels

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14
Q

CCB (dihydropyridines) name ending + 2 key side effects?

A

Pine + periperipheral oedema and flushes

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15
Q

Name a K+ channel agonist + what disease is it used for?

A

Nicorandil + angina

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16
Q

Name an alpha 1 blocker + key side effect?

A

Doxazosin + postural hypotension

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17
Q

Give an example of a thiazide, loop and potassium sparing diuretic?

A

Bendrofluazide, furosemide, spironolactone

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18
Q

3 side effects of thiazide and loop diuretics?

A

Hypokalaemia, hyperglycaemia and gout (increased uric acid)

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19
Q

2 side effects of spironolactone?

A

Gynecomastia (breast swelling) and hyperkalaemia

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20
Q

Name 2 oral antiplatelets + their mechanism + key side effect?

A

Aspirin (blocks COX)

Clopidogrel (blocks P2Y12) + GI bleeds

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21
Q

Warfarin route + mechanism + side effect + CI?

A

Oral + inhibits vitamin K + haemorrhage + pregnancy

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22
Q

Heparin route + mechanism (+ exception) + CI?

A

IV/SC + increases AT III affinity for serine proteases IIa and Xa (LMWH only blocks Xa) + renal disease

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23
Q

Fibrinolytic route + mechanism + examples?

A

IV + activates plasmin which breaks down fibrin + strptokinase, duteplase and alteplase

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24
Q

What makes up the hydrophobic core of a lipoprotein?

A

Cholsterol esters

Triglycerides

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25
Q

Key molecule on the surface of lipoproteins?

A

Apoproteins

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26
Q

What apo does VLDL contain?

A

apoB100

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27
Q

What apo do chylomicrons contain?

A

apoB48

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28
Q

Place of formation + role of chylomicrons and VLDL?

A

Chylomicrons made in enterocytes and transport dietary triglycerides + VLDL made in the liver and transport liver triglycerides

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29
Q

Chylomicron to remnant summary?

A

MTP lipidates apoB48 to allow more triglycerides to enter
ApoA1 allows chylomicron to leave
ApoCII from HDL allows LPL to bind and break down triglycerides

30
Q

How cholesterol esters + triglycerides are formed?

A

Esterification of cholsterol and monoglyceride + fatty acid

31
Q

Lipoproteins travel by the lymphatics then venous system. True or False?

A

True

32
Q

What are chylomicron and VLDL remnants?

A

Particles with no triglycerides but still containing cholesterol ester

33
Q

ApoCII is returned to HDL in exchange for which apoprotein? How does this facilitate clearance of apoB lipoprotein + key enzyme in the liver?

A

ApoCII is returned to HDL in exchange for apoE

High affinity ligand for receptor-mediated clearance + heapatic lipase

34
Q

What percent of apoB48 and apoB100 chylomicrons are removed by receptor mediated clearance?

A

100% of apoB48

Only 50% of apoB100

35
Q

What happens to the remaining apoB100 remnants?

A

Become enriched in cholesterol esters and become LDL via IDL

36
Q

Which receptor is vital for LDL clearance + where is it?

A

LDL receptor in liver

37
Q

LDL clearance summary?

A

LDL undergoes hydrolysis and releases cholesterol

38
Q

Normal 2 effects of HMG-CoA reductase?

A

Increase cholesterol synthesis and decrease LDL liver receptors

39
Q

LDL role in athersclerosis?

A

Macrophages oxidise it to OXLDL to form foam cells

40
Q

Athersclerosis summary?

A

Damaged endothelial express ICAM and VCAM
Macrophage and T lymphs migrate into cell wall
Macrophage oxidises LDL to OXLDL to form foam cell/plaque
Smooth muscle cells accumulate and cause hypertrophy

41
Q

3 drugs to lower cholesterol?

A

Statins, fibrates and PCSK 9 inhibitors

42
Q

How do statins work + 2 side effects + better taken at what time?

A

Inhibit HMG CoA reducatase + rhabdomylosis and myalgia + at night

43
Q

Drug for hypertriglyceridaemia + mechanism?

A

Fibrates + lower VLDL production in the liver

44
Q

Drug for familial hypercholesterolaemia + mechanism + example?

A

PCSK 9 inhibitor + blocks PCSK 9 from binding LDL receptors so more are available + alirocumab

45
Q

What are the 3 components of Virchow’s triad?

A

Hypercoaguability, venous stasis and endothelial dysfunction

46
Q

Colour + treatment for venous and arterial thrombus and which is more common?

A

Venous is red and treated with anticoagulants (more common)

Arterial is white and treated with antiplatelets

47
Q

Soft clots are coated with … and hard clots are coated with …?

A

Fibrinogen and fibrin

48
Q

Soft clot formation summary?

A
Damaged site exposes collagen
Platelets bind and form TXA2 via COX
TXA2 causes ADP serotonin/5-HT release
5-HT causes vasoconstiction
ADP binds P2Y12 to activate more platelets
TXA2 and GP receptors bind fibrinogen
49
Q

Hard clot formation?

A

VII (tenase) converts X to Xa (prothrombinase)
Xa converts II (prothrombin) to X (thrombin)
Thrombin converts fibrinogen to firbrin

50
Q

Name the 4 inactive precursors of the main clotting factors involved in coagulation that are blocked by warfarin?

A

II, VII, IX, X

51
Q

Inactive precursors are … and have to undergo …. to form …?

A

Glycoproteins and gamma-carboxylation and serine proteases

52
Q

What does the enzyme which carries out gamma-carboxylation of clotting factor precursors require?

A
Vitamin K
(in its reduced, hydroquinone form)
53
Q

What are the two forms of Vitamin K that exist?

A

K1 from diet

K2 from bacteria in intestine

54
Q

Where are clotting factors released from?

A

The liver

55
Q

How might a warfarin overdose be treated?

A

Vitamin K/clotting factor infusion

56
Q

What does Antithrombin III (ATIII) do?

A

Inhibits serine proteases (IIa and Xa)

57
Q

Give 2 examples of LMWHs?

A

Enoxaparin

Dalteparin

58
Q

Dabigatran route + mechanism?

A

Oral + blocks thrombin

59
Q

Rivaroxiban route + mechanism?

A

Oral + blocks Xa

60
Q

Which enzyme aids platelet synthesis of TXA2?

A

COX

61
Q

Tirofiban route + mechanism?

A

IV + blocks GPIIb/IIIa receptors

62
Q

Class I anti arrhythmic examples + mechanism + phase they affect?

A

Lignocaine, lidocaine, quinidine, flecainide, propafenone + block Na channels + phase 0

63
Q

Class 2 anti arrhythmic examples + mechanism + phase they affect?

A

Propanolol + beta blocker + phase 4

64
Q

Class 3 anti arrhythmic examples + mechanism + phase they affect?

A

Amiodarone and sotalol + blocks K channels + phase 3

65
Q

Class 4 anti arrhythmic examples + mechanism + phase they affect?

A

Verapamil and diltiazem + blocks Ca channel + phase 2

66
Q

Adenosine mechanism?

A

Blocks AVN

67
Q

Magnesium sulphate mechanism + used in?

A

Blocks Ca and Na channels + Torsades des Pointes

68
Q

Ivabradine mechanism + used in?

A

Blocks the funny current (HCN channel) + angina

69
Q

Atropine mechanism + used in?

A

Decreases vagal innervation on SAN + bradycardia

70
Q

Thiazide vs loop diuretics vs spironolactone block what transporter + where?

A
Thiazide = Na/Cl in the distal tubule
Loop = Na/K/Cl in the ascending Loop of Henle
Spironolactone = Na ENaC channel in the nephron