Ruggles Lecture 3 Flashcards
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
Antiplatelet drugs
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
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
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
ADP receptor blocker
- ADP = chemical signal that incr. platelet activity
What are the 3 ADP receptor blockers?
- Clopidogrel (Plavix)
- Prasugrel (Effient)
- Ticlopidine (Ticlid)
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
Glycoprotein IIb-IIIa Receptor Blockers
What are the 3 Glycoprotein IIb-IIIa Receptor Blockers?
- Abciximab (ReoPro)
- Eptifabatide (Integrilin)
- Tirofiban (Aggrastat)
What are the ADRs of antiplatelet drugs?`
- Bleeding – be alert for unexplained or heavy bleeding
- Symptoms indicating hemorrhage are sudden increase in joint or back pain and severe headaches
- Gastric irritation
- GP IIb-IIIa inhibitors - hypotension
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
Hyperlipidema
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%
HMG-CoA Reductase Inhibitors (Statins)
- extremely effective at decreasing LDLs
Primarily decrease triglyceride levels; Exact mechanism is unclear; may have anti-inflammatory properties; Two types: Fenofibrate (Tricor) and Gemfibrozil (Lopid)
Fibric Acids (Fibrates)
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
Bile Acid Sequestrants
- Cholestyramine (Questran)
- Colesevelam (Welchol)
- Colestipol (Colestid)
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
Niacin
Inhibits the absorption of cholesterol from the GI tract; not very beneficial and very expensive
Ezetimibe (Zetia)
What are the ADRs of antihyperlipidemic agents?
- Flushing w/ Niacin
- Liver dysfunction
- Gallstones
- Pancreatitis
- Neuromuscular problems w/ statins – myopathy (muscular pain, inflammation, weakness)
What are the risk factors for pts taking statins from developing neuromuscular problems?
- high dose
- advanced age
- genetic factors
- multiple diseases
- frail stature
- immunosuppressant drugs
- 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
What are the 2 primary respiratory drugs?
- Drugs that treat acute and relatively minor problems (nasal congestion, coughing, seasonal allergies)
- Drugs that treat more chronic and serious airway obstruction (bronchial asthma, chronic bronchitis, emphysema)
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
Antitussives
- Benzonatate (Tessalon) – local anesthetic effect on respiratory mucosa
- Codeine – narcotic that inhibits the cough reflex
- Dextromethorphan – inhibits the cough reflex
What are the respiratory drugs that treat acute and relatively minor problems?
- Antitussives
- Decongestants
- Antihistamines
- Mucolytics
- Expectorants
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
Decongestants
- Oxymetazoline (Afrin) – nasal spray
- Phenylephrine – oral or nasal spray
- Pseudoephedrine (Sudafed) – oral
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
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
decrease the viscosity of respiratory secretions; Acetylcysteine (Mucomyst); Given via inhalation
Mucolytics
facilitate production and ejection of mucus; Guaifenesin (Mucinex); GI upset when taken on an empty stomach
Expectorants
What drugs are used in long-term management of asthma?
- Glucocorticoids - first line; Inhaled not readily absorbed into systemic circulation; Reduce the inflammation
- Beta-2 agonists - maintain bronchodilation; long acting and short acting (symptomatic tx of attack; rescue therapy)
- Leukotriene inhibitor - decrease airway inflammation
- Theophylline - powerful bronchodilator but use is limited due to toxicity
What are the drugs used for COPD?
- Anticholinergics are used first-line
- LABA – can be used in combination with an anticholinergic to promote bronchodilation
- Theophylline – used as an alternative for patients who fail to respond to other bronchodilators
- Glucocorticoids – no clear therapeutic benefit
- Drug therapy is directed toward maintaining airway patency and preventing airflow restriction
What drugs are used to treat CF?
- 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
What are the drugs that treat more chronic and serious airway obstruction?
- Beta-Adrenergic Agonists
- Xanthine Derivatives
- Anticholinergic Drugs
- Glucocorticoids
- Cromones
- Leukotriene Inhibitors
- Leukotriene Inhibitors
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
Beta-Adrenergic Agonists
- usually given via metered-dose inhaler or nebulizer
What are the types of Beta-Adrenergic Agonists?
- Albuterol (Proventil, Ventolin) – 3-6 hour duration
- Levalbuterol (Xopenex) – 5-6 hour duration
- Aformoterol (Brovana) – 12 hour duration
- Formoterol (Foradil, Perforomist) – 12 hour duration
- Salmeterol (Serevent) – 12 hour duration
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
Xanthine Derivatives
- Aminophylline
- Dyphylline
- Theophylline
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
Anticholinergic Drugs
- Ipratropium (Atrovent) – dosed 3-4 times per day
- Tiotropium (Spiriva) – longer-acting – dosed once daily
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
Glucocorticoids
- Budesonide (Pulmicort) – inhalation
- Fluticasone (Flovent) – inhalation
- Dexamethasone – oral, IV, IM
- Methylprednisolone – oral, IV, IM
- Prednisone – oral
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
Cromones
- Cromolyn sodium – inhalation
- Nasalcrom – nasal spray for allergic rhinitis associated with seasonal allergies
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
Leukotriene inhibitors
- Montelukast (Singulair)
