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Drugs List > Block 2 Drugs > Flashcards

Block 2 Drugs Flashcards

1
Q

Heparin

A

Anticoagulant

Binds reversibly to anti-thrombin III and enhances its inactivation of thrombin and FXa

  • Unfractioned heparin: inhibits FXa and thrombin
  • LMWH: Primarily inhibits FXa

Used for:

  • Low dose: prophylaxis, prevention of VTE
  • Treatment dose: prevents progression of existing clots
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2
Q

Warfarin

A

Anticoagulant

Affects vitamin K metabolism by inhibiting synthesis of vitamin K-dependent coagulation factors (VII, IX, X and prothrombin/FII) (1972)

Used for :

  • Prophylaxis and treatment of VTE
  • Prevention of ischaemic stroke in AF
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3
Q

Dabigatran

A

New Oral Anticoagulant (NOAC)

Competitive, reversible inhibitor of thrombin

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4
Q

B2-Adrenergic Agonists

A
  • Salbutamol (Short acting)
  • Terbutaline (Short acting)
  • Salmeterol (Long acting)
  • Formoterol (Long acting)
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5
Q

B2-Adrenergic Agonists:

MoA

Side Effects

A

Cellular target: Bronchiolar smooth muscle cells

Molecular target: Stimulation of B2-adrenergic receptors

  • Activation of B2AR activates G-protein
  • Increases activation of adenylate cyclase
  • Adenylate cyclase converts ATP to cAMP
  • Increased cAMP activates protein kinase A which:
    • Drives Ca2+ into intracellular storage vesicles away from cytoplasm.
    • Reduces activity of myosin light chain kinase = reduced muscle contraction
    • Dephosphorylation of myosin light chain = reduced muscle contraction
  • Reduced cytoplasmic Ca2+ levels reduce smooth muscle contraction resulting in bronchodilation.

Side effects:

  • Tremor
  • Tachycardia
  • Cardiac arrhythmias
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6
Q

What is the difference in the MoA of short and long acting B2-Adrenergic Agonists?

A

Short acting: directly binds to activation site on B2-adrenergic receptor

Long acting:

  • Formoterol: Binds to depot in lipid bilayer before binding to active site on B2AR
  • Salmeterol: Membrane translocation for 30 mins before binding to active site.
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7
Q

Anti-cholinergics

Drugs

MoA

Side Effects

A
  • Ipratropium (short acting)
  • Tiotropium (long acting)

Blocks M3 muscarinic acetylcholine receptors preventing stimulating effects of ACh:

  • Inhibits activation of G-protein therefore inhibits activation of phospholipase C enzyme (PLC)
  • PLC therefore cannot release calcium from intracellular stores
  • Cytoplasmic Ca2+ levels do not rise therefore bronchiolar smooth muscle contraction does not increase (inhibits bronchoconstriction)
  • =Bronchiolar relaxation

Side Effects:

  • Dry mouth
  • Constipation
  • Urinary retention
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8
Q

Methylxanthines

Drugs

MoA

Side Effects

A
  • Theophylline
  • Aminophylline

Inhibit phosphodiesterase enzymes (PDE) preventing it from inhibiting CAMP.

CAMP levels maintained therefore protein kinase A enzyme activated which stores intracellular Ca2+ into storage vesicles.

Reduced cytoplasmic Ca2+ results in less smooth muscle contraction so less bronchoconstriction

Side effects:

  • Cardiac arrhythmias
  • Seizures
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9
Q

Glucocorticoids

Drugs

MoA

Side Effects

A
  • Beclomethasone
  • Prednisolone
  • Fluticasone
  • Hydrocortisone

Targets immune cells of the lungs: macrophages, T-lymphocytes, eosinophils.

Activates glucocorticoid receptors which interact with selected nuclear DNA sequences and influences the expression of genes:

  • Repression of pro-inflammatory mediators: IL-3, IL-5, Th​2 cytokines
  • Expression of anti-inflammatory products: secreted leukocyte peptidase inhibitor (SLPI), Lipcortin-1 and upregulation of B2 adrenoceptors.

Side Effects:

  • Hyperglycaemia
  • Muscle wasting
  • Thinning skin
  • Osteoporosis
  • Increased risk of infection
  • Moon face (facial swelling)
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10
Q

Leukotriene Receptor Antagonists:

Drugs

MoA

Side Effects

A
  • Montekulast
  • Zafirlukast

Leukotrienes released from mast cell upon activation, normally binds to CysLT1 leukotriene receptor to:

  • Stimulate bronchiolar smooth muscle constriction
  • Bind to and recruit immune cells such as eosinophils by guiding eosinophil chemotaxis.

Leukotriene receptor antagonists block CysLT1 receptors on smooth muscle and eosinophils blocking the above effects.

Used as preventer

Side Effects:

  • Abdo pain
  • Headaches
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11
Q

Beta-Adrenergic Receptor Antagonists

Drugs

MoA

Uses

Side Effects

A
  • Bisoprolol
  • Atenolol (B1 cardioselective)
  • Propranolol (B1 and B2)

Competitive inhibitors of adrenaline and noradrenaline at beta-adrenergic receptors, inhibit sympathetic stimulation of heart muscle.(B1 antagonists selective for cardiomyocytes and contractility) by inhibiting cAMP cascade (PKA etc) which in cardiomyocytes drives contraction (opposite to bronchiolar smooth muscle)

  • Negative inotropes and chronotropes.
  • Reduce workload of the heart relieving oxygen demand. (reduced heart rate = reduced cardiomyocyte contractility)

Side Effects:

  • Dizziness
  • Constipation

Contraindicated in asthmatic patients

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12
Q

Calcium Channel Inhibitors:

Drugs

MoA

Side Effects

A
  • Nifedipine
  • Amlodipine

Prevent opening of L-type voltage-gated calcium channels reducing influx of Ca2+ into cells.

Reduces intracellular calcium has vasodilator effect on resistance vessels = reduced afterload. Causes dilation of coronary arteries increasing blood flow.

Do not act on veins.

Side Effects:

  • Ankle swelling
  • Palpitations
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13
Q

HMG-CoA Reductase Inhibitors:

Drugs

MoA

A
  • Atorvastatin
  • Simvastatin

Reduce cholesterol reducing risk of atherosclerosis

Inhibit HMG-CoA Reductase (HMGCR) enzyme which reduces circulating cholesterol by:

  • Reducing intrinsic production of cholesterol
  • Promote uptake of excess cholesterol by liver.

Uses:

  • Treatment of HF without affecting BP
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14
Q

Nitrate Vasodilators

Drugs

MoA

Side Effects

A
  • Glyceryl Trinitrate (GTN)
  • Isosorbide Mononitrate (ISMN)

Metabolised to release NO which diffuses into cell and stimulates soluble guanylate cyclase.

Increases cGMP in vascular smooth muscle cells:

  • Drives dephosphorylation of myosin light chains via activation of MLC phosphatase.
  • Inhibits influx of Ca2+ into smooth muscle cytoplasm causing relaxation.

Works on vascular smooth muscle of arteries and veins:

  • Venodilation: reduces cardiac preload (capacitance)
  • Arteriodilation: coronary artery vasodilation increases blood flow to myocardium
  • Moderate arteriolar dilation: reduces cardiac afterload

Side Effects:

  • Headache
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15
Q

Anti-cholinergics for emergency treatment:

Drugs

MoA

Uses

A
  • Atropine

Blockage of muscarinic M2 acetylcholine receptors on cardiomyocytes. Inhibits effects of parasympathetic, cholinergic vagus nerve transmission which normally exerts negative chronotropy. Increases heart rate by accelerating repolarisation rate in cardiac muscle.

Uses:

  • Sinus bradycardia
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16
Q

Sympathomimetics:

Drugs

MoA

A
  • Adrenaline (alpha and beta)
  • Noradrenaline (alpha)
  • Dobutamine (beta)

Adrenaline: Binds and stimulates cardiomyocyte B1-adrenergic receptors. Used in cardiac arrest to drive cardiac muscle contraction and restore heart function. Positive inotrope and chronotrope

17
Q

Neprilysin Inhibitors:

Drugs

MoA

Uses

A
  • Sacubitril

Inhibition of neprilysin enzyme preventing its inactivation of natriuretic peptides.

Prolonging of natriuretic peptides enhances their action of excreting water and sodium.

Effective when used with angiotensin II receptor blockers e.g. valsartan

Uses:

  • Heart failure with reduced ejection fraction
18
Q

Antiplatelets:

Drugs

MoA

Uses

A
  • Aspirin

Blocks the enzyme action of platelet COX enzyme which is required for the synthesis of thromboxane A2 (TXA2).

Reduced TXA2 synthesis results in inhibition of platelet activation and thrombus formation.

  • Clopidogrel

ADP receptor blocker: binds to and block the function of ADP receptors on platelet surfaces, inhibiting platelet activation and subsequent thrombus formation.

Uses:

  • Treatment and prevention of cardiovascular disease without affecting blood pressure
    *
19
Q

Thrombolytics:

Drugs

MoA

A
  • Alteplase
  • Streptokinase
  • Urokinase

Activates plasminogen to plasmin which digests fibrin and fibrinogen to restore blood flow.

Side Effects:

  • Arrhythmias
  • Bleeding
  • Streptokinase can only be used once as an immune response is generated, memory B cells produce anti-streptokinase ABs.
20
Q

Angiotensin II receptor blockers

Drugs

MoA

Uses

A
  • Losartan
  • Valsartan

Directly block activation of the angiotensin II receptor therefore prevents it from inducing vascular smooth muscle constriction and increasing BP. Reduces peripheral resistance and cardiac afterload.

Uses:

  • HTN
21
Q

Angiotensin Converting Enzyme (ACE) Inhibitors

Drugs

MoA

Uses

Side Effects

A
  • Ramipril

Inhibits angiotensin converting enzyme, preventing it from converting angiotensin I to angiotensin II. This prevents it from inducing contraction in vascular smooth muscle and increasing BP. This reduces peripheral resistance and cardiac afterload.

Less angiotensin II also results in less aldosterone secretion, therefore sodium and water retention is decreased which helps to lower BP by reducing plasma volume. This reduces preload.

Uses:

  • HTN

Side effects:

  • Persistent cough
  • Decreased GFR as angiotensin normally constricts efferent arterioles

Drugs List (6 decks)

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