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PHARMACOLOGY

Cardiac Wellness Institute of Calgary. PHARMACOLOGY. Updated May 2010. Material to be Covered. ACSM’s Resource Manual for Guidelines for Exercise Testing and Prescription ( 6 th edition) Chapter 6 (pg. 115-116) Chapter 8 (pg. 145-147) Chapter 38 (pg. 622-624)

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PHARMACOLOGY

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  1. Cardiac Wellness Institute of Calgary PHARMACOLOGY Updated May 2010

  2. Material to be Covered • ACSM’s Resource Manual for Guidelines for Exercise Testing and Prescription ( 6th edition) • Chapter 6 (pg. 115-116) • Chapter 8 (pg. 145-147) • Chapter 38 (pg. 622-624) • ACSM’s Guidelines for Exercise Testing and Prescription (8th edition) • Appendix A (pg. 274-291) • Pharmacology for Nursing Care 5th ed.

  3. Cardiac Medications

  4. Beta Blockers • Prescribed for: Angina, Myocardial Infarction (MI), arrhythmia, essential tremors (shaking), migraines • Mechanism of Action: • Competitively block ß-adrenergic receptors • ß1 receptors - cardiac stimulation • ß2 receptors - vascular and bronchial smooth muscle dilation • Cardioselective ß-blockers (blocks ß1 not ß2)

  5. Beta-Blockers • Hemodynamic Effects: •  myocardial O2 demand ( HR, diastolic filling time) •  HR, BP, myocardial contractility (rest & ex) •  ischemia • Exercise Capacity: •  patients with angina •  or  patients without angina • GXT for ischemia - false negative

  6. Beta-Blockers • Adverse Effects: • BP - lightheaded ordizzy • Coronary artery vasoconstriction/worsening spasm • Exacerbate acute Congestive Heart Failure (CHF) •  claudication pain in people with Peripheral Arterial Disease(PAD); cold hands & feet • Precipitation/worsening of bronchospasm • Bradycardia or AV block • Mask S/S of hypoglycemia in diabetes • Fatigue, depression, insomnia, vivid dreams •  triglycerides,  HDL-C

  7. Beta-Blockers • Common ß-blockers • Metoprolol/Lopressor • Atenolol/Tenormin • Bisoprolol/Monocor

  8. Nitrates • Prescribed for:Angina & CHF • Mechanism of Action: • Direct relaxation of vascular smooth muscle •  myocardial O2 supply by dilating collateral arteries (not atherosclerotic arteries) •  preload & afterload, therefore  end diastolic volume

  9. Nitrates • Hemodynamic Effects: •  Rest HR (Baroreceptor-mediated tachycardia) •  or  Ex HR •  Rest BP &  or  Ex BP •  time to ischemia •  myocardial O2 consumption • May  coronary blood flow d/t  collateral flow or  ventricular diastolic pressure • Prevention of spasm

  10. Nitrates • Routes of Administration: • Sublingual • Oral • IV • Transdermal • Use: • PRN or prophylactically • Nitrate Tolerance • 10 - 12 hour NTG-free interval

  11. Nitrates • Adverse Effects: • Headache • Dizziness or lightheaded • Weakness •  HR • Flushed face • Skin irritation • Not for use with drugs such as Viagra, Cialis, Levitra etc. (Hypotension!)

  12. Nitrates • Common Nitrates • Nitroglycerin spray • Isosorbide mononitrate/Imdur • Nitro-Dur (patch)

  13. Calcium Channel Blockers(CCBs) • Prescribed for:Angina, MI, spasm, hypertension • Mechanism of Action: • Selective blockade of transmembrane calcium flow • Limits calcium entry into cardiac & smooth muscle cells OR • Relaxation of vascular smooth muscle

  14. CCBs • No direct effect on myocardial contractility or SA/AV node conduction • Most CCBs work only on arterioles • Exception: Diltiazem & Verapamil •  HR •  AV node conduction

  15. CCBs • Hemodynamic Effects: •  or  Rest HR & Ex HR •  BP •  ischemia • Exercise Capacity: •  in patients with angina •  in patients without angina

  16. CCBs • Adverse Effects:(vary with each medication) • CHF • Hypotension • Bradycardia • Dizzy/syncopal • Flushing • Swelling • Headaches • Constipation • Dry mouth • Nausea

  17. CCBs • Common Calcium Channel Blockers • Amlodipine/Norvasc • Diltiazem/Cardizem/Tiazac • Verapamil/Isoptin • Nifedepine/Adalat

  18. Angiotensin Converting Enzyme (ACE) Inhibitors • Prescribed for: HTN, CHF, MI and Diabetic nephropathy • Mechanism of Action: • ACE Inhibitors block the reaction of angiotensin I to angiotensin II, which is a potent vasoconstrictor.

  19. ACE Inhibitors • Hemodynamic Effects: •  Rest & Ex HR •  Rest & Ex BP •  or prevent ventricular remodeling • Exercise Capacity: •  or  in patients with CHF •  in patients without CHF

  20. ACE Inhibitors • Adverse Effects: • Dry cough • Kidney failure • Swelling of face, tongue or lips (angioedema) •  BP (dizziness or lightheaded) • Common ACE Inhibitors • Ramipril/Altace • Enalapril/Vasotec • Fosinopril/Monopril • Lisinopril/Prinivil/Zestril

  21. Angiotensin II Receptor Blockers(ARBs) • Prescribed for:HTN, CHF and Diabetic nephropathy • Mechanism of Action: • ARBs block access of angiotensin II to its receptors • Results in vasodilation and reduced secretion of aldosterone and vasopressin, ultimately reducing BP and myocardial workload

  22. ARBs • Hemodynamic Effects: •  Rest & Ex HR •  Rest & Ex BP • Exercise Capacity: • No effect • Adverse Effects: • Headache • Angioedema • Low Blood Pressure

  23. ARBs • Common ARBs • Irbesartan/Avapro • Losartan/Cozaar • Valsartan/Diovan

  24. Diuretics • Prescribed for:HTN, CHF, Peripheral edema • Mechanism of Action: •  renal secretion of salt and water • Inhibits sodium re-absorption at various sites of the nephron •  intravascular volume & edema

  25. Diuretics • Hemodynamic Effects: •  in Rest & Ex HR •  or  in Rest & Ex BP •  , PVCs or false positive on ECG • Exercise Capacity: • No change

  26. Diuretics • Adverse Effects: • Electrolyte abnormalities • Hyper/Hypokalemia •  LDL-C & triglycerides • Hypovolemia • Common Diuretics • Esidrix/Hydrochlorothiazide (HCTZ) • Furosemide/Lasix • Spironolactone/Aldactone

  27. Digitalis • Prescribed for:CHF and Atrial Arrhythmia • Mechanism of Action: • Inhibits Na+-K+-ATPase • Limits ionic movement across myocardial cell membrane • Positive inotropic effect ( myocardial contractility)

  28. Digitalis • Hemodynamic Effects: • Sinus rhythm:  HR • Afib or CHF:  Rest & Ex HR •  Rest & Ex BP • “Dig effect” • Non-specific ST-T changes and false positive exercise ECG • Exercise Capacity: •  in patients with Afib or CHF •  in others

  29. Digitalis • Adverse Effects: • Toxicity • Visual and neurological symptoms • Arrhythmias • Common Digitalis Medications • Lanoxin/Digoxin

  30. Anti-Arrhythmic Agents • Classified by electrophysiological effect: • Class I: •  conduction velocity, excitabilty & automaticity •  peripheral vasodilation • Prolong QRS or Long QT Syndrome • Common Class I Meds • Lidocaine/Xylocaine • Propafenone/Rhythmol

  31. Anti-Arrhythmic Agents • Class II: - ß-Blockers • Class III: • Mechanism of Action: • Blocks Na+ channels • Negative chronotropic effect •  conduction •  myocardial O2 demand • Delays repolarization

  32. Anti-Arrhythmic Agents • Class III (con’t) • Hemodynamic Effect: •  Rest & Ex HR •  Rest & Ex BP •  ECG • Exercise Capacity: • No effect • Adverse Effects: •  arrythmias  Photosensitivity • Bradycardia/AV block  Dermatological, GI, • Hypotension  Hepatic or thyroid • Electrolyte disturbance abnormalities

  33. Anti-Arrhythmic Agents • Class III (con’t) • Common Class III Meds • Amiodarone/Cordarone • Sotalol/Betapace • Class IV: • Calcium Channel Blockers

  34. Platelet Aggregation Inhibitors • Mechanism of Action: • Different for each med • ASA:  production of thromboxane A2 • Plavix:  binding of ADP to its platelet receptor • Hemodynamic Effect: • No effect • Exercise Capacity: • No effect

  35. Platelet Aggregation Inhibitors • Adverse Effects: • Bruise easily • Bleeding gums • Cuts and nicks bleed longer • GI upset • Common Platelet Aggregation Inhibitors • Clopidigrel/Plavix • Ticlopidine/Ticlid • Aspirin/Asaphen/ASA

  36. Anticoagulants • Prescribed for: Venous thrombosis, pulmonary embolism, Afib with embolization, prophylaxis after MI • Mechanism of Action: • Coumadin: inhibit synthesis of Vit K dependant clotting factors • Heparin: prevents progression of existing clot by inhibiting any further clotting processes

  37. Anticoagulants • Hemodynamic Effects: • No effect • Exercise Capacity: • No effect • Adverse Effects: • Bleeding • Bruising • GI bleed

  38. Other Commonly Used Medications

  39. Diabetes Management • Oral hypoglycemic agents • Used in Type 2 diabetes only • Used in conjunction with diet and exercise • 1 & 2) Sulfonylureas & Meglitinides • Mechanism of Action:stimulates release of insulin frompancreatic islets to lower blood glucose • Adverse Effects:Hypoglycemia • Common Medications • Glyburide/DiaBeta • Repaglinide/Gluconorm

  40. Diabetes 3)Alpha-glucosidase Inhibitors • Mechanism of Action: • Reduce the rate of digestion of CHO, primarily lowering postprandial glucose concentrations • Adverse Effects: • Flatulance • Cramps • Abdominal distension, diarrhea • Liver dysfunction • *** Minimal chance of hypoglycemia

  41. Diabetes 4)Biguanides • Mechanism of Action: •  production of glucose in the liver;  glucose utilization at the muscle • Adverse Effects: • Lactic acidosis, nausea, diarrhea, loss of appetite • *** no risk of hypoglycemia • Metformin/Glucophage

  42. Diabetes 5)Thiazolidinediones (Glitazones) • Mechanism of Action: •  insulin resistance;  production of glucose by liver,  glucose uptake by muscle • Adverse Effects: • Expands blood volume; weight gain, edema • Headache • Sinusitis • Myalgia •  LDL-C & HDL-C, Triglycerides • Pioglitazone/Actos

  43. COPD Management 1) Glucocorticosteroids • Prescribed for allergy symptoms and asthma • Mechanism of Action: suppresses inflammation • Adverse Effects: • Hoarseness, difficulty speaking, slow growth in children, increased risk of cataracts, osteoporosis & peptic ulcer disease • Fluticasone Propionate/Flovent

  44. COPD 2)Leukotriene Receptor Antagonists • To prevent symptoms caused by asthma, chronic bronchitis, emphysema and other lung diseases. • Mechanism of Action: • Block cysteinylleukotrienes from binding to their receptors, preventing bronchoconstriction and mucous production • Adverse Effects: • Generally well tolerated • Monteluekast Sodium/Singulair

  45. COPD 3)Beta2-adrenergic Stimulants • To prevent symptoms caused by asthma, chronic bronchitis, emphysema and other lung diseases. • Mechanism of Action: • Selective activation of Beta2-adrenergic receptors to promote bronchodilation and relieve bronchospasm. • Adverse Effects: • ß1 –adrenergic receptors in the heart could be stimulated causing Tachyarrhythmias and Angina • Musculoskeletal tremors • Albuterol/Ventolin

  46. COPD 4) Anticholinergics • To prevent symptoms caused by asthma, chronic bronchitis, emphysema and other lung diseases. • Mechanism of Action: • Promotes bronchodilation • Adverse Effects: • Dry mouth • Irritation of pharynx • Atrovent/Ipratropium Bromide

  47. Lipid Management 1)HMG CoA Reductase Inhibitors (STATINS) • Mechanism of Action: •  cholesterol production • Increase number of LDL receptors on hepatocytes, enhancing the elimination of LDL from the blood • Beneficial Cardiovascular Actions: •  LDL,  HDL, Promote plaque stability • Improve abnormal endothelial function; enhanced vessel dilation & reduce risk of thrombosis

  48. Lipids • Adverse Effects: • Generally well tolerated • Headache; rash; GI disturbance; Myopathy (Rhabdomyolysis) • Common Medications: • Atorvastatin/Lipitor • Simvastatin/Zocor • Rosuvastatin/Crestor • Pravastatin/Pravachol

  49. Lipids 2)Ezetimibe/Ezetrol •  TC, LDL, Trigs & can HDL • Mechanism of Action: • Blocks absorption of dietary and bile-secreted cholesterol • Adverse Effects: • Generally well tolerated

  50. Lipids 3)Fibric Acid Derivatives (FIBRATES) • Most effective for Trigs &  HDL • Mechanism of Action: • Activate receptors to accelerate the clearance of VLDLs, and thereby reduce levels of TGs • Adverse Effects: • Generally well tolerated • Rashes and GI disturbances • Gemfibrizol/Lopid

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