Block 2 Drugs Flashcards

1
Q

Beta-2 adrenergic agonist (short-acting)

A

Salbutamol (short-acting)

Terbutaline (short-acting)

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2
Q

Beta-2 adrenergic agonist (long-acting)

A

Salmeterol (long-acting)

Formoterol (long-acting)

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3
Q

Beta-2 adrenergic agonist MoA

A

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.
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4
Q

Beta-2 adrenergic agonist: Side Effects

A

Tremor

Tachycardia

Cardiac arrhythmia

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5
Q

Anti-muscarinic (short-acting)

A

Ipratropium (short-acting)

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6
Q

Anti-muscarinic (long-acting)

A

Tiotropium (long-acting)

Glycopyrronium (long-acting)

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7
Q

Anti-muscarinics MoA

A

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
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8
Q

Anti-muscarinics: Side Effects

A

Dry mouth

Urinary retention

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9
Q

Methylxanthine’s

A

Theophylline

Aminophylline

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10
Q

Methylxanthine’s MoA

A

Inhibit phosphodiesterase, increasing cellular cAMP = bronchodilation

Emergency only - need to monitor serum levels!

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11
Q

Methylxanthine’s: Side Effects

A

Cardiac arrhythmias

Seizures (can be fatal)

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12
Q

Glucocorticoid/Corticosteroid

A

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

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13
Q

Glucocorticoid/Corticosteroid MoA

A

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
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14
Q

Glucocorticoid/Corticosteroid: Side Effects

A

Moon face

Increased abdominal fat

Osteoporosis

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15
Q

Leukotriene receptor antagonist

A

Montelukast

Zafirlukast

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16
Q

Leukotriene receptor antagonist MoA

A

Block proinflammatory leukotriene signalling - CysLT1 leukotriene receptor.

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

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17
Q

Leukotriene receptor antagonist: Side Effects

A

Abdominal pain

Headache

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18
Q

Angiotensin-converting enzyme (ACE) inhibitor

A

Ramipril

Lisinopril

19
Q

Angiotensin-converting enzyme (ACE) inhibitor MoA

A

Inhibits conversion of angiotensin I to angiotensin II: reduces vasoconstriction

20
Q

Angiotensin-converting enzyme (ACE) inhibitor: Side Effects

A

Persistant Cough

21
Q

Angiotensin II receptor blocker (ARBs)

A

Losartan

Valsartan

22
Q

Angiotensin II receptor blocker (ARBs) MoA

A

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
23
Q

Beta adrenergic receptor antagonist aka beta blocker

cardioselective, beta-1 antagonist

A

Bisoprolol (cardioselective, beta-1 antagonist)

Atenolol (cardioselective, beta-1 antagonist)

24
Q

Beta adrenergic receptor antagonists aka beta blocker

beta-1 and beta-2 antagonist

A

Propranolol (beta-1 and beta-2 antagonist)

25
Q

Beta adrenergic receptor antagonist aka beta blocker MoA

A

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

26
Q

Beta adrenergic receptor antagonist aka beta blocker: Side Effects

A

Dizziness

Constipation

27
Q

HMG-CoA Reductase Inhibitor aka statins

A

Atorvastatin

Simvastatin

28
Q

HMG-CoA Reductase Inhibitor aka statins MoA

A

Inhibition of mavelonate metabolism in cholesterol synthesis pathway

29
Q

Calcium channel antagonist (uses: heart failure and hypertension)

A

Nifedipine

Amlodipine

30
Q

Calcium channel antagonist MoA

A

Blocks L-type calcium channels, promoting vasodilation

31
Q

Calcium channel antagonist: Side Effects

A

Ankle swelling

Palpitations

32
Q

Nitrate vasodilator

A

Glycerol trinitrate (GTN)

Isosorbide mononitrate (ISMN)

33
Q

Nitrate vasodilator MoA

A

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

34
Q

Anti-muscarinic (for emergency bradycardia treatment)

A

Atropine

35
Q

Anti-muscarinic (for emergency bradycardia treatment) MoA

A

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

36
Q

Sympathomimetic

A

Noradrenaline

Dobutamine

Adrenaline

37
Q

Sympathomimetic MoA

A

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

38
Q

Neprilysin inhibitors (used with an ARB drug)

A

Sacubitril (used with valsartan, ARB drug)

39
Q

Neprilysin inhibitors (used with an ARB drug) MoA

A

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

40
Q

Antiplatelet drug (COX inhibitor)

A

Aspirin

41
Q

Antiplatelet drug (COX inhibitor) MoA

A

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.

42
Q

Antiplatelet drug (ADP receptor antagonist)

A

Clopidogrel

43
Q

Antiplatelet drug (ADP receptor antagonist) MoA

A

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