Block 2 Drugs

Question 1

Beta-2 adrenergic agonist (short-acting)

Answer 1

Salbutamol (short-acting)

Terbutaline (short-acting)

Question 2

Beta-2 adrenergic agonist (long-acting)

Answer 2

Salmeterol (long-acting)

Formoterol (long-acting)

Question 3

Beta-2 adrenergic agonist MoA

Answer 3

Stimulation of airway bronchiolar smooth muscle relaxation via adrenergic activation!

• Increases action of adenylate cyclase, increasing cAMP within cytoplasm
• cAMP activates Protein Kinase A - drives Ca2+ into storage vesicles away from cytoplasm
• Reduced cytoplasmic Ca2+ levels reduce smooth muscle contraction = bronchodilation
• Inactivation of MLCK also reduces smooth muscle contraction, promoting dilation of airway.

Question 4

Beta-2 adrenergic agonist: Side Effects

Answer 4

Tremor

Tachycardia

Cardiac arrhythmia

Question 5

Anti-muscarinic (short-acting)

Answer 5

Ipratropium (short-acting)

Question 6

Anti-muscarinic (long-acting)

Answer 6

Tiotropium (long-acting)

Glycopyrronium (long-acting)

Question 7

Anti-muscarinics MoA

Answer 7

Block M3 muscarinic receptors of cholinergic activity in airway smooth muscle = muscle relaxation

• Reduces phospholipasde C enzyme (PLC)
• Reduces IP3 generation and Ca2+ release into cytoplasm
• Reduced cytoplasmic Ca2+ levels reduce smooth muscle contraction = bronchodilation

Question 8

Anti-muscarinics: Side Effects

Answer 8

Dry mouth

Urinary retention

Question 9

Methylxanthine’s

Answer 9

Theophylline

Aminophylline

Question 10

Methylxanthine’s MoA

Answer 10

Inhibit phosphodiesterase, increasing cellular cAMP = bronchodilation

Emergency only - need to monitor serum levels!

Question 11

Methylxanthine’s: Side Effects

Answer 11

Cardiac arrhythmias

Seizures (can be fatal)

Question 12

Glucocorticoid/Corticosteroid

Answer 12

Beclomethasone (inhaled)
Fluticasone (inhaled)
Prednisolone (oral)
Hydrocortisone (IV)

Question 13

Glucocorticoid/Corticosteroid MoA

Answer 13

Activate glucocorticoid receptors in immune cells, reducing airway inflammation

(Prevent late phase effects of asthma)

• Cellular Targets: immune cells of the lungs macrophages/T-lymphocytes/eosinophils
• Molecular Target: Intracellular Glucocorticoid Receptor (GR) is TRANSCRIPTION FACTOR
• Activated GR interacts with selected DNA sequences and influences expression of genes
• Suppression of pro-inflammatory mediators e.g. TH2 cytokines such as IL-3, IL-5
• Expression of anti-inflammatory products e.g. SLPI

Question 14

Glucocorticoid/Corticosteroid: Side Effects

Answer 14

Moon face

Increased abdominal fat

Osteoporosis

Question 15

Leukotriene receptor antagonist

Answer 15

Montelukast

Zafirlukast

Question 16

Leukotriene receptor antagonist MoA

Answer 16

Block proinflammatory leukotriene signalling - CysLT1 leukotriene receptor.

(Used as a preventer - prevent late phase effects of asthma)

Question 17

Leukotriene receptor antagonist: Side Effects

Answer 17

Abdominal pain

Headache

Question 18

Angiotensin-converting enzyme (ACE) inhibitor

Answer 18

Ramipril

Lisinopril

Question 19

Angiotensin-converting enzyme (ACE) inhibitor MoA

Answer 19

Inhibits conversion of angiotensin I to angiotensin II: reduces vasoconstriction

Question 20

Angiotensin-converting enzyme (ACE) inhibitor: Side Effects

Answer 20

Persistant Cough

Question 21

Angiotensin II receptor blocker (ARBs)

Answer 21

Losartan

Valsartan

Question 22

Angiotensin II receptor blocker (ARBs) MoA

Answer 22

Directly block cell signalling induced by angiotensin II

• Reduced Angiotensin II decreases vasoconstriction in peripheral blood vessels = reduced SVR and afterload = lowers BP.
• Also adosterone secretion reduced = increased Na and water loss - lowers plasma volume and decreases cardiac preload

Question 23

Beta adrenergic receptor antagonist aka beta blocker

cardioselective, beta-1 antagonist

Answer 23

Bisoprolol (cardioselective, beta-1 antagonist)

Atenolol (cardioselective, beta-1 antagonist)

Question 24

Beta adrenergic receptor antagonists aka beta blocker

beta-1 and beta-2 antagonist

Answer 24

Propranolol (beta-1 and beta-2 antagonist)

Question 25

Beta adrenergic receptor antagonist aka beta blocker MoA

Answer 25

Blockade of beta-adrenergic receptors on cardiomyocytes, reducing inotropy & chronotropy

Question 26

Beta adrenergic receptor antagonist aka beta blocker: Side Effects

Answer 26

Dizziness | Constipation

Question 27

HMG-CoA Reductase Inhibitor aka statins

Answer 27

Atorvastatin Simvastatin

Question 28

HMG-CoA Reductase Inhibitor aka statins MoA

Answer 28

Inhibition of mavelonate metabolism in cholesterol synthesis pathway

Question 29

Calcium channel antagonist (uses: heart failure and hypertension)

Answer 29

Nifedipine Amlodipine

Question 30

Calcium channel antagonist MoA

Answer 30

Blocks L-type calcium channels, promoting vasodilation

Question 31

Calcium channel antagonist: Side Effects

Answer 31

Ankle swelling Palpitations

Question 32

Nitrate vasodilator

Answer 32

Glycerol trinitrate (GTN) Isosorbide mononitrate (ISMN)

Question 33

Nitrate vasodilator MoA

Answer 33

Release of nitric oxide = relaxation (venodilation) of vascular smooth muscle in coronary arteries and veins

Question 34

Anti-muscarinic (for emergency bradycardia treatment)

Answer 34

Atropine

Question 35

Anti-muscarinic (for emergency bradycardia treatment) MoA

Answer 35

Blockade of cardiac M2 muscarinic receptors = increased chronotropy via inhibiting parasympathetic cholinergic vagus nerve

Question 36

Sympathomimetic

Answer 36

Noradrenaline Dobutamine Adrenaline

Question 37

Sympathomimetic MoA

Answer 37

Binds + stimulates cardiomyocyte β1-adrenergic receptors = increased cardiac inotropy and chronotropy

Question 38

Neprilysin inhibitors (used with an ARB drug)

Answer 38

Sacubitril (used with valsartan, ARB drug)

Question 39

Neprilysin inhibitors (used with an ARB drug) MoA

Answer 39

Inhibition of natriuretic peptide breakdown, promotes natriuresis (water & sodium excretion) and reduces cardiac preload

Question 40

Antiplatelet drug (COX inhibitor)

Answer 40

Aspirin

Question 41

Antiplatelet drug (COX inhibitor) MoA

Answer 41

Reduces activation of platelets to prevent thrombosis: inhibition of thromboxane A2 production Aspirin (cyclo-oxygenase inhibitor) blocks enzyme action of platelet COX enzyme. COX is required for synthesis of thromboxane A2 (TXA2). Reduced TXA2 inhibits platelet activation and thrombus formation.

Question 42

Antiplatelet drug (ADP receptor antagonist)

Answer 42

Clopidogrel

Question 43

Antiplatelet drug (ADP receptor antagonist) MoA

Answer 43

Reduce activation of platelets to prevent thrombosis: blockade of platelet ADP receptors