Ruggles Lecture 3

Question 1

Used, often prophylatctically, in pts at high risk for for thrombus formation where atherosclerotic plaques have ruptured, or in those with a history of thrombi

Answer 1

Antiplatelet drugs

Question 2

Suppresses platelet aggregation by inhibiting the synthesis of prostaglandins and thromboxanes; inhibit platelets irreversibly; especially useful during the acute phase of MI (limits progression of platelet induced occlusion); used to prevent stroke caused by cerebral ischemia and infarction (not hemorrhagic strokes); used to prevent incidence of initial attack in susceptible individuals

Answer 2

Aspirin (ASA)

• Benefit must outweigh risk of bleeding
• Men = protection against MI. Women = protection against ischemic stroke.
• Can be given alone or in combination with other antiplatelet medications
• weak inhibitor of platelet activity
• May increase the risk of intracranial hemorrhage
• Can be poorly tolerated - tinnitus = toxicity

Question 3

Used primarily to prevent thrombosis in patients at risk for MI or ischemic stroke, including those with unstable angina, acute coronary syndrome, atrial fibrillation, and similar conditions; Also used to prevent infarction following percutaneous coronary angioplasty, placement of a coronary artery stent, and other surgical procedures; Dual antiplatelet strategy; Moderate inhibitors of platelets; Response varies

Answer 3

ADP receptor blocker

- ADP = chemical signal that incr. platelet activity

Question 4

What are the 3 ADP receptor blockers?

Answer 4

1. Clopidogrel (Plavix)
2. Prasugrel (Effient)
3. Ticlopidine (Ticlid)

Question 5

Inhibits the ability of fibrinogen to activate platelets; Block the GP receptor on the platelet membrane that is stimulated by fibrinogen and other chemical mediators; Most powerful platelet inhibitors; Given IV before and during surgical procedures to help maintain coronary flow and decrease mortality

Answer 5

Glycoprotein IIb-IIIa Receptor Blockers

Question 6

What are the 3 Glycoprotein IIb-IIIa Receptor Blockers?

Answer 6

1. Abciximab (ReoPro)
2. Eptifabatide (Integrilin)
3. Tirofiban (Aggrastat)

Question 7

What are the ADRs of antiplatelet drugs?`

Answer 7

1. Bleeding – be alert for unexplained or heavy bleeding
2. Symptoms indicating hemorrhage are sudden increase in joint or back pain and severe headaches
3. Gastric irritation
4. GP IIb-IIIa inhibitors - hypotension

Question 8

Abnormally high concentration of lipids in the bloodstream; One of the primary causes of cardiovascular disease; Causes deposits of fatty plaque-like lesions on the walls of arteries (atherosclerosis) which can lead to thrombosis and infarction; Atherosclerosis can precipitate increased clotting and thromboembolic disease; Usually caused by poor diet and lifestyle, and by genetic and metabolic conditions that cause disorders in lipid metabolism

Answer 8

Hyperlipidema

Question 9

Inhibit HMG Co-A reductase enzyme that catalyzes one of the early steps of cholesterol synthesis; decrease cholesterol production, especially in the liver; Generally decrease total cholesterol (TC) and LDL; Decrease the risk of major cardiac events by up to 50%

Answer 9

HMG-CoA Reductase Inhibitors (Statins)

- extremely effective at decreasing LDLs

Question 10

Primarily decrease triglyceride levels; Exact mechanism is unclear; may have anti-inflammatory properties; Two types: Fenofibrate (Tricor) and Gemfibrozil (Lopid)

Answer 10

Fibric Acids (Fibrates)

Question 11

Attach to bile acids and increase their fecal excretion → cholesterol breakdown is accelerated to replace the lost bile acids → decreased plasma cholesterol; may help regulate glucose levels

Answer 11

Bile Acid Sequestrants

• Cholestyramine (Questran)
• Colesevelam (Welchol)
• Colestipol (Colestid)

Question 12

Binds to specific receptors in fat cells and initiates lipolysis and reduced entry of fatty acids into the bloodstream; Benefits virtually all aspects of the lipid profile

Answer 12

Niacin

Question 13

Inhibits the absorption of cholesterol from the GI tract; not very beneficial and very expensive

Answer 13

Ezetimibe (Zetia)

Question 14

What are the ADRs of antihyperlipidemic agents?

Answer 14

1. Flushing w/ Niacin
2. Liver dysfunction
3. Gallstones
4. Pancreatitis
5. Neuromuscular problems w/ statins – myopathy (muscular pain, inflammation, weakness)

Question 15

What are the risk factors for pts taking statins from developing neuromuscular problems?

Answer 15

1. high dose
2. advanced age
3. genetic factors
4. multiple diseases
5. frail stature
6. immunosuppressant drugs
7. Combining a statin + fibric acid
   - Usually reversible -4-6 week recovery as long as it doesn’t progress to a more serious form rhabdomyolysis - early detection is key for reversibility

Question 16

What are the 2 primary respiratory drugs?

Answer 16

1. Drugs that treat acute and relatively minor problems (nasal congestion, coughing, seasonal allergies)
2. Drugs that treat more chronic and serious airway obstruction (bronchial asthma, chronic bronchitis, emphysema)

Question 17

Suppress coughing associated with the common cold; Should not be used to treat an active, productive cough ; Not recommended for children <6 years old; Adverse effects – sedation, dizziness, GI upset

Answer 17

Antitussives

• Benzonatate (Tessalon) – local anesthetic effect on respiratory mucosa
• Codeine – narcotic that inhibits the cough reflex
• Dextromethorphan – inhibits the cough reflex

Question 18

What are the respiratory drugs that treat acute and relatively minor problems?

Answer 18

1. Antitussives
2. Decongestants
3. Antihistamines
4. Mucolytics
5. Expectorants

Question 19

Bind to alpha-1 adrenergic receptors on blood vessels of the nasal mucosa and stimulate vasoconstriction; Can mimic the effects of increased sympathetic nervous system activity

Answer 19

Decongestants

• Oxymetazoline (Afrin) – nasal spray
• Phenylephrine – oral or nasal spray
• Pseudoephedrine (Sudafed) – oral

Question 20

blocks the effects of histamine on the upper airway; these drugs help decrease nasal congestion, mucosal irritation and discharge, and conjunctivitis caused by inhaled allergens; Adverse effect – sedation, fatigue, dizziness, blurred vision, incoordination, GI distress

Answer 20

Antihistamines

• Histamine – endogenous chemical involved in normal regulation of certain physiological functions and hypersensitivity reactions
• First generation: diphenhydramine, chlorpheniramine, doxylamine; Cross the BBB – causes sedation
• Second generation: Loratidine (Claritin), Cetirizine (Zyrtec), Fexofenadine (Allegra) – non-sedating

Question 21

decrease the viscosity of respiratory secretions; Acetylcysteine (Mucomyst); Given via inhalation

Answer 21

Mucolytics

Question 22

facilitate production and ejection of mucus; Guaifenesin (Mucinex); GI upset when taken on an empty stomach

Answer 22

Expectorants

Question 23

What drugs are used in long-term management of asthma?

Answer 23

1. Glucocorticoids - first line; Inhaled not readily absorbed into systemic circulation; Reduce the inflammation
2. Beta-2 agonists - maintain bronchodilation; long acting and short acting (symptomatic tx of attack; rescue therapy)
3. Leukotriene inhibitor - decrease airway inflammation
4. Theophylline - powerful bronchodilator but use is limited due to toxicity

Question 24

What are the drugs used for COPD?

Answer 24

1. Anticholinergics are used first-line
2. LABA – can be used in combination with an anticholinergic to promote bronchodilation
3. Theophylline – used as an alternative for patients who fail to respond to other bronchodilators
4. Glucocorticoids – no clear therapeutic benefit
   - Drug therapy is directed toward maintaining airway patency and preventing airflow restriction

Question 25

What drugs are used to treat CF?

Answer 25

• Treatment is focused on maintaining airway patency
  1. Bronchodilators, mucolytics, and/or expectorants – limit the formation of mucous plugs
  2. Inhaled glucocorticoids cannot penetrate through the thick mucus secretions in the airways of people with CF
  3. High dose NSAID – controls inflammation, may slow progression
  4. Anti-infectious agents – esp. azithromycin
  5. Respiratory hygiene

Question 26

What are the drugs that treat more chronic and serious airway obstruction?

Answer 26

1. Beta-Adrenergic Agonists
2. Xanthine Derivatives
3. Anticholinergic Drugs
4. Glucocorticoids
5. Cromones
6. Leukotriene Inhibitors
7. Leukotriene Inhibitors

Question 27

Respiratory smooth-muscle cells contain the beta-2 subtype of adrenergic receptors. These drugs work to stimulate these receptors results in relaxation of bronchiole smooth muscle and bronchodilation

Answer 27

Beta-Adrenergic Agonists

- usually given via metered-dose inhaler or nebulizer

Question 28

What are the types of Beta-Adrenergic Agonists?

Answer 28

1. Albuterol (Proventil, Ventolin) – 3-6 hour duration
2. Levalbuterol (Xopenex) – 5-6 hour duration
3. Aformoterol (Brovana) – 12 hour duration
4. Formoterol (Foradil, Perforomist) – 12 hour duration
5. Salmeterol (Serevent) – 12 hour duration

Question 29

Enhance bronchodilation by inhibiting the phosphodiesterase (PDE) enzyme located on bronchial smooth muscle; PDE breaks down cAMP which is a bronchodilator; Anti-inflammatory ; Blocks the effects of adenosine; Given orally or IV; Adverse effects: Toxicity – nausea, confusion, irritability, restlessness → cardiac arrhythmias, seizure

Answer 29

Xanthine Derivatives

• Aminophylline
• Dyphylline
• Theophylline

Question 30

Block muscarinic cholinergic receptors to prevent acetylcholine-induced bronchoconstriction and improve airflow; Drug of choice for COPD; Adverse effects – all anticholinergics blurred vision, urinary retention, dry mouth, constipation, and tachycardia

Answer 30

Anticholinergic Drugs

• Ipratropium (Atrovent) – dosed 3-4 times per day
• Tiotropium (Spiriva) – longer-acting – dosed once daily

Question 31

Inhibit the inflammatory response that leads to bronchospasm; Drug of choice for asthma; Available by inhalation, oral route, or IV –inhaled route is preferred because of decreased chance of systemic side effects; Adverse effects – osteoporosis, retardation of growth in children, cataracts, glaucoma, hyperglycemia –minimal risk when administered via inhalation

Answer 31

Glucocorticoids

• Budesonide (Pulmicort) – inhalation
• Fluticasone (Flovent) – inhalation
• Dexamethasone – oral, IV, IM
• Methylprednisolone – oral, IV, IM
• Prednisone – oral

Question 32

Not bronchodilators –ineffective for acute attacks; Prevent bronchoconstriction by inhibiting the release of inflammatory mediators (histamine, leukotriene) from pulmonary mast cells –also called mast cell stabilizers; Adverse effects
Well-tolerated, Some irritation of the nasal and upper respiratory passages

Answer 32

Cromones

• Cromolyn sodium – inhalation
• Nasalcrom – nasal spray for allergic rhinitis associated with seasonal allergies

Question 33

Inhibits inflammatory compounds important in mediating the airway inflammation underlying COPD and asthma; Oral administration; Can be combined with other drugs to provide optimal management in specific patients with COPD and asthma - Glucocorticoid sparing; Adverse effects - hepatic impairment

Answer 33

Leukotriene inhibitors

- Montelukast (Singulair)