CAT2 Pharmacology (P2)

Mediators of bronchoconstriction

Histamine, leukotrienes, acetylcholine via muscarinic receptors

Mediators of bronchodilation

Adrenaline bind to beta-2 adrenergic receptors → cAMP

Short-acting B2 agonists

Albuterol

Bronchodilation

Use of SABA

Used in acute exacerbation

Long-acting B2 agonists

Salmeterol, formoterol; Bronchodilation

Use of LABA

Used in combination with corticosteroids

Inhaled corticosteroids

Fluticasone, budesonide

Suppress cytokine production, eosinophil apoptosis

Adverse effect of Inhaled corticosteroids

Oral candidiasis

Short-acting muscarinic antagonists

Ipratropium bromide

Bronchodilation

Long-acting muscarinic antagonists

Tiotropium

Bronchodilation

Use of SAMA + LAMA

COPD

Classes for Heart Failure

Beta-blockers

Mineralocorticoid receptor antagonists

ACE inhibitors + Angiotensin receptor blockers

Neprilysin inhibitors

Loop diuretic (furosemide)

Mineralocorticoid receptor antagonists

Spironolactone, Eplerenone

MoA of Mineralocorticoid receptor antagonists

Aldosterone antagonists → Increase sodium and water excretion → weak diuretics

Adverse effects of Mineralocorticoid receptor antagonists

Increase risk of hyperkalemia, particularly in renal impairment

Neprilysin Inhibitors

Sacubitril

MoA of Neprilysin Inhibitors

Neprilysin → inactivates ANP, BNP, and AT-II

Inhibitors → ↑ ANP, ↑ BNP, ↑ AT-II

Use of Neprilysin Inhibitors

Used with angiotensin-II receptor blocker

Loop Diuretic

Furosemide

MoA of Furosemide

Inhibition of Na/K/Cl transporter in ascending limb of loop of Henle

Increased ion concentration in the tubule → reduce water resorption in collecting duct → diuresis

Use of Furosemide

Fluid retention and pulmonary edema

Used in combination with ACE-inhibitor

Three Anti-platelet medications

Aspirin

P2Y12 receptor inhibitors

Glycoprotein IIb/IIIa inhibitors

MoA of Aspirin

Irreversible inhibitor of cyclooxygenase enzyme → ↓ TXA2 → Antithrombotic

Use of Aspirin

Cardiovascular or cerebrovascular disease, Kawasaki disease

Adverse effects of Aspirin

Bleeding, gastric ulcer disease, tinnitus, kidney injury, allergic reactions

P2Y12 receptor inhibitors

Clopidogrel

Ticlopidine

MoA of Clopidogrel

Cardiovascular disease (PCI), alternative to aspirin

Adverse effects of Clopidogrel

Thrombotic thrombocytopenic purpura

Glycoprotein IIb/IIIc inhibitors

Abciximab

Eptifibatide

Tirofiban

MoA of Abciximab

Fragment of monoclonal antibody (Fab region vs GpIIb/IIIaR)

Four Anti-cogulation medications

Heparin

Warfarin

Direct thrombin inhibitors

Direct Xa inhibitors

MoA of Heparin

Potentiates antithrombin → ↓ Xa activity, ↓ IIa (Thrombin) activity

Uses of Heparin

Anticoagulation, DVT prophylaxis, does not cross placenta (pregnancy)

Monitoring of Heparin

aPTT + Platelet count

MoA of Unfractionated heparin

Blocks thrombin (IIa) and Xa equally

Short half-life, easily reversible

MoA of Low molecular weight heparin

Blocks Xa

↑ Bioavailability, longer half-life

MoA of Warfarin

Inhibition of vitamin K epoxide reductase → ↓ II, VII, IX, X, Protein C and S

Long half live (vs heparin)

Monitoring of Warfarin

PT/INR

Direct thrombin inhibitors

Dabigatran

Bivalirudin

Argatroban

Direct Xa inhibitors

Apixaban

Rivaroxaban