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MBChB > Pharmacology > Flashcards

Pharmacology Flashcards

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1
Q

When is digoxin used?

A

Rate control in AF/Atrial Flutter

Heart Failure

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2
Q

What is the MoA of digoxin?

A 
Positively inotropic (increases contractility)
Negatively chronotropic (decreased HR)

Inhibits the Na/K ATPase
Na accumulates inside the cell 
Activates the Na/Ca exchanger
Ca pumped into the cell 
Ca increases the force of contraction

Digoxin increases the vagal parasympathetic activity

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3
Q

What side effects are associated with digoxin?

A

Bradycardia
Visual disturbances (blurred/yellow vision)
Dizziness
GI disturbances

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4
Q

What are the main pharmacokinetics/pharmacodynamic principles of digoxin?

A

Narrow therapeutic window
Digoxin toxicity –> arrhythmias (life-threatening)
Long t1/2 - once daily dosing

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5
Q

When is aspirin used?

A

Secondary prevention of thrombotic events
Management of ACS
(Pain relief)

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6
Q

What is the MoA of aspirin?

A

Binds irreversibly to the cyclooxygenase (COX) enzyme
Reduces production of thromboxane –> reduces platelet aggregation and thrombus formation
Reduces endothelial prostaglandin production –> reduces nociceptive sensitisation and inflammation

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7
Q

What side effects are associated with aspirin?

A 
Gastric bleeding (1%)
Peptic ulceration 
Bronchospasm - hypersensitivity
Angiooedema
Reyes syndrome (rare)
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8
Q

What advice should be given to patients on aspirin?

A

PPI can be useful in LT uses
Avoid drug preparations that contain aspirin
Aspirin should be avoided in under 16s –> increased risk of Reyes Syndrome

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9
Q

What are the common doses of aspirin?

A

ACS: 300mg then 75mg OD

2ry prevention: 75mg OD

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10
Q

When is Clopidogrel used?

A

Secondary prevention of thrombotic events

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11
Q

What is the MoA of Clopidogrel?

A

Irreversibly blocks the ADP receptor on platelet cell membrane
Prevents formation of GPIIb/IIIa complex needed for platelet aggregation
Reduces thrombus formation

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12
Q

What side effects are associated with Clopidogrel?

A

Bleeding (GI, IC, post-surgery) in 1-10%
GI upset (dyspepsia, diarrhoea, abdo discomfort) in 1-10%
Rarely, thrombocytopenia

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13
Q

What advice needs to be given to patients on Clopidogrel?

A

Stop 7d prior to surgery

Don’t stop without consulting dr if have an arterial stent in-situ

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14
Q

Give examples of recombinant tissue plasminogen activator drugs

A

Alteplase

Tenecteplase

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15
Q

Describe the MoA of rTPA

A

Recombinant tissue plasminogen activator
Catalyse the conversion of plasminogen into plasmin
Lysis of the fibrin clot

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16
Q

What are the indications for the use of rTPA?

A

Within 4.5h of an acute ischaemic stroke
Within 12h of MI
Massive PE

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17
Q

What are the side effects associated with rTPA?

A

Bleeding

Allergic reaction/angiooedema (1%)

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18
Q

How is Alteplase administered?

A

Bolus-infusion regimen

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19
Q

How is Tenecteplase administered?

A

Single bolus

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20
Q

What pharmacodynamic interaction is associated with rTPA?

A

Interaction with anti-platelets and anti-coagulant drugs

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21
Q

Describe the MoA of unfractionated heparin

A

Enhances the activity of antithrombin III which inhibits thrombin
Also inhibits multiple other factors in the coagulation pathway
Has an anti-coagulant effect

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22
Q

What are the indications for heparin?

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A

Treatment and prevention of thromboembolic events
Renal dialysis
Treatment of Acute Coronary Syndrome

23
Q

What are the side effects associated with heparin?

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A

Bleeding - risk as great as 3.5%
Heparin-induced thrombocytopenia
Osteoporosis

24
Q

How is heparin administered?

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A

Continuous IV infusion

SC injection

25
How can the anti-coagulant effect of heparin be reversed?
Protamine
26
How is the effect of heparin monitored?
aPTT
27
What are the indications for Warfarin?
Thromboprophylaxis in AF, metallic heart valves, cardiomyopathy Treatment of thromboembolism
28
What is the MoA of Warfarin?
Inhibits Vit K epoxide reductase Prevents the recycling of Vitamin K to reduced form after carboxylation of coagulation factors II, VII, IX and X Prevents thrombus formation
29
What side effects are associated with Warfarin?
Bleeding (Increased risk with increasing INR) Warfarin necrosis Osteoporosis
30
What are the key PD/PK principles of Warfarin?
Multiple interactions with other drugs/foods Requires regular monitoring of INR and dose adjustment (requires compliance) Can be reversed with Vit K
31
Give an example of a direct thrombin inhibitor
Dabigatran
32
What is the MoA of Dabigatran?
Direct thrombin inhibitor Inhibits conversion of fibrinogen into fibrin Prevents thrombus formation
33
What are the indications for Dabigatran?
Venous thrombus prophylaxis post surgery | Thromboprophylaxis in non-valvular AF
34
What are the side-effects associated with Dabigatran?
Bleeding | Dyspepsia
35
What are the key PD/PK principles of Dabigatran?
Rapid onset Not metabolised by cytochrome p450 so no drug/food interactions No monitoring required No antidote available
36
What is the MoA of Rivaroxaban?
Inhibits the conversion of prothrombin into thrombin Reduces the concentration of thrombin in the blood Inhibits the formation of fibrin clots
37
What are the indications for Rivaroxaban?
Venous thromboembolism prophylaxis (post-surgery) Thromboprophylaxis in non-valvular AF Treatment of venous thromboembolism
38
What side effects are associated with RIvaroxaban?
Bleeding | Nausea
39
What are the key PD/PK principles of Rivaroxaban?
Metabolised by cyrochrome p450 No antidote No therapeutic monitoring required
40
What is the MoA of metformin?
Suppresses gluconeogenesis Reduces amount of glucose absorbed in the gut Increases uptake of glucose into skeletal muscle
41
What side effects are associated with metformin
Dose related GI upset | Lactic acidosis
42
What is the MoA of sulphonylureas (glipizide, gliclazide)?
Binds to the SU receptor on the surface of beta cells Blocks K ATPase --> cell depolarises L-type Ca channels open --> influx of Ca into cell Exocytosis of insulin
43
What side effects are associated with sulphonylureas (glipizide, gliclazide)?
``` Prolonged severe hypoglycaemia Bone marrow toxicity Skin rashes GI upset Increased appetite --> weight gain ```
44
What is the MoA of meglitinides (Repaglitinide, nateglitinide)?
Binds to SU receptor on B cell will less potency compared to sulphonylureas (lower risk of hypoglycaemia)
45
What is the MoA of thiozolidinediones (Pioglitazone?)
Binds to PPAR-gamma receptor (present in adipose tissue, liver and muscle) Increases lipogenesis Increases uptake of fatty acid and glucose
46
What side effects are associated with thiozolidinediones (Pioglitazone)?
Fluid retention (worsens heart failure) Increased risk of fracture Increased risk of bladder cancer Weight gain
47
What is the MoA of alpha-glucosidase inhibitors (acarbose)?
Delays carbohydrate absorption
48
What side effects are associated with alpha-glucosidase inhibitor (acarbose)?
Flatulence Loose stools/diarrhoea Abdominal bloating Abdominal pain (useful in obese patients)
49
What is the MoA of incretin mimics (exenatide, liraglutide)?
Increases insulin secretion Decreases glucagon secretion Slows gastric emptying
50
What side effects are associated with incretin mimics (exenatide, liraglutide)?
Hypoglycaemia Range of GI effects Pancreatitis
51
What is the MoA of -gliptans?
Competitively inhibit DDP4 Increase GLP-1 in circulation Increase insulin secretion Reduce glucagon secretion
52
What side effects are associated with -gliptans?
GI Liver disease Worsening of pancreatitis, heart failure
53
What is the MoA of SGLT-2 inhibitors (-flozin)?
Inhibit SGLT2 channel in PCT Reduce amount of glucose reabsorbed from filtrate More glucose lost in urine
54
What side effects are associated with SGLT-2 inhibitors (-flozin)?
Hypoglycaemia UTI Genital candidiasis

MBChB (14 decks)

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