PHARMACOLOGY Cardiac Wellness Institute of Calgary Updated May 2010.
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Transcript of PHARMACOLOGY Cardiac Wellness Institute of Calgary Updated May 2010.
Material to be CoveredMaterial to be Covered
ACSM’s Resource Manual for Guidelines for ACSM’s Resource Manual for Guidelines for Exercise Testing and Prescription ( 6Exercise Testing and Prescription ( 6 thth edition) edition)− Chapter 6 (pg. 115-116)Chapter 6 (pg. 115-116)
− Chapter 8 (pg. 145-147)Chapter 8 (pg. 145-147)
− Chapter 38 (pg. 622-624)Chapter 38 (pg. 622-624)
ACSM’s Guidelines for Exercise Testing and ACSM’s Guidelines for Exercise Testing and Prescription (8Prescription (8thth edition) edition)− Appendix A (pg. 274-291)Appendix A (pg. 274-291)
Pharmacology for Nursing Care 5Pharmacology for Nursing Care 5 thth ed ed..
Beta BlockersBeta Blockers
Prescribed for: Angina, Myocardial Infarction Prescribed for: Angina, Myocardial Infarction (MI), arrhythmia, essential tremors (shaking), (MI), arrhythmia, essential tremors (shaking), migrainesmigraines
Mechanism of ActionMechanism of Action::– Competitively block ß-adrenergic receptorsCompetitively block ß-adrenergic receptors
– ßß11 receptors - cardiac stimulation receptors - cardiac stimulation
– ßß22 receptors - vascular and bronchial smooth muscle receptors - vascular and bronchial smooth muscle dilationdilation
– Cardioselective ß-blockers Cardioselective ß-blockers (blocks ß(blocks ß1 1 not ßnot ß22))
Beta-BlockersBeta-Blockers
Hemodynamic Effects:Hemodynamic Effects: myocardial Omyocardial O22 demand ( demand ( HR, HR, diastolic filling diastolic filling
time)time)
HR, BP, myocardial contractility (rest & ex)HR, BP, myocardial contractility (rest & ex)
ischemiaischemia
Exercise Capacity:Exercise Capacity: patients with anginapatients with angina
or or patients without angina patients without angina
– GXT for ischemia - false negative GXT for ischemia - false negative
Beta-BlockersBeta-Blockers Adverse Effects:Adverse Effects:
BP - lightheaded orBP - lightheaded or dizzydizzy
– Coronary artery vasoconstriction/worsening spasmCoronary artery vasoconstriction/worsening spasm
– Exacerbate acute Congestive Heart Failure (CHF)Exacerbate acute Congestive Heart Failure (CHF)
– claudication pain in people with Peripheral Arterial claudication pain in people with Peripheral Arterial DiseaseDisease (PAD); cold hands & feet(PAD); cold hands & feet
– Precipitation/worsening of bronchospasmPrecipitation/worsening of bronchospasm
– Bradycardia or AV blockBradycardia or AV block
– Mask S/S of hypoglycemia in diabetesMask S/S of hypoglycemia in diabetes
– Fatigue, depression, insomnia, vivid dreamsFatigue, depression, insomnia, vivid dreams
triglycerides, triglycerides, HDL-C HDL-C
Beta-BlockersBeta-Blockers
Common ß-blockersCommon ß-blockers– Metoprolol/LopressorMetoprolol/Lopressor
– Atenolol/TenorminAtenolol/Tenormin
– Bisoprolol/MonocorBisoprolol/Monocor
NitratesNitrates
Prescribed for:Prescribed for: Angina & CHFAngina & CHF Mechanism of Action:Mechanism of Action:
– Direct relaxation of vascular smooth muscleDirect relaxation of vascular smooth muscle
myocardial Omyocardial O22 supply by dilating collateral arteries supply by dilating collateral arteries (not atherosclerotic arteries)(not atherosclerotic arteries)
preload & afterload, therefore preload & afterload, therefore end diastolic end diastolic volumevolume
NitratesNitrates
Hemodynamic Effects:Hemodynamic Effects: Rest HR (Baroreceptor-mediated tachycardia)Rest HR (Baroreceptor-mediated tachycardia)
or or Ex HR Ex HR
Rest BP & Rest BP & or or Ex BP Ex BP
time to ischemiatime to ischemia
myocardial Omyocardial O2 2 consumptionconsumption
– May May coronary blood flow d/t coronary blood flow d/t collateral flow or collateral flow or ventricular diastolic pressure ventricular diastolic pressure
– Prevention of spasmPrevention of spasm
NitratesNitrates
Routes of Administration:Routes of Administration:– SublingualSublingual
– OralOral
– IVIV
– TransdermalTransdermal
Use:Use:– PRN or prophylacticallyPRN or prophylactically
Nitrate ToleranceNitrate Tolerance– 10 - 12 hour NTG-free interval10 - 12 hour NTG-free interval
NitratesNitrates
Adverse Effects:Adverse Effects:– HeadacheHeadache
– Dizziness or lightheadedDizziness or lightheaded
– WeaknessWeakness
HRHR
– Flushed faceFlushed face
– Skin irritationSkin irritation
Not for use with drugs such as Viagra, Cialis, Not for use with drugs such as Viagra, Cialis, Levitra etc. (Hypotension!)Levitra etc. (Hypotension!)
NitratesNitrates
Common NitratesCommon Nitrates– Nitroglycerin sprayNitroglycerin spray
– Isosorbide mononitrate/ImdurIsosorbide mononitrate/Imdur
– Nitro-Dur (patch)Nitro-Dur (patch)
Calcium Channel BlockersCalcium Channel Blockers (CCBs)(CCBs)
Prescribed for:Prescribed for: Angina, MI, spasm, hypertensionAngina, MI, spasm, hypertension Mechanism of Action:Mechanism of Action:
– Selective blockade of transmembrane calcium Selective blockade of transmembrane calcium flow flow
Limits calcium entry into cardiac & smooth Limits calcium entry into cardiac & smooth muscle cellsmuscle cells
OROR Relaxation of vascular smooth muscleRelaxation of vascular smooth muscle
CCBsCCBs
No direct effect on myocardial contractility or No direct effect on myocardial contractility or SA/AV node conductionSA/AV node conduction
– Most CCBs work only on arteriolesMost CCBs work only on arterioles
ExceptionException: Diltiazem & Verapamil: Diltiazem & Verapamil – HRHR
– AV node conductionAV node conduction
CCBsCCBs
Hemodynamic Effects:Hemodynamic Effects:
– or or Rest HR & Ex HR Rest HR & Ex HR
– BPBP
– ischemiaischemia
Exercise Capacity:Exercise Capacity:
– in patients with anginain patients with angina
– in patients without anginain patients without angina
CCBsCCBs
Adverse Effects:Adverse Effects: (vary with each medication)(vary with each medication)
– CHFCHF– HypotensionHypotension– BradycardiaBradycardia– Dizzy/syncopalDizzy/syncopal– FlushingFlushing– SwellingSwelling– HeadachesHeadaches– ConstipationConstipation– Dry mouthDry mouth– NauseaNausea
CCBsCCBs
Common Calcium Channel BlockersCommon Calcium Channel Blockers– Amlodipine/NorvascAmlodipine/Norvasc
– Diltiazem/Cardizem/TiazacDiltiazem/Cardizem/Tiazac
– Verapamil/IsoptinVerapamil/Isoptin
– Nifedepine/AdalatNifedepine/Adalat
Angiotensin Converting Angiotensin Converting Enzyme (ACE) InhibitorsEnzyme (ACE) Inhibitors
Prescribed for:Prescribed for: HTN, CHF, MI and Diabetic HTN, CHF, MI and Diabetic nephropathynephropathy
Mechanism of Action:Mechanism of Action:– ACE Inhibitors block the reaction of angiotensin I to ACE Inhibitors block the reaction of angiotensin I to
angiotensin II, which is a potent vasoconstrictor.angiotensin II, which is a potent vasoconstrictor.
ACE InhibitorsACE Inhibitors
Hemodynamic Effects:Hemodynamic Effects: Rest & Ex HRRest & Ex HR
Rest & Ex BPRest & Ex BP
or prevent ventricular remodelingor prevent ventricular remodeling
Exercise Capacity:Exercise Capacity: or or in patients with CHF in patients with CHF
in patients without CHFin patients without CHF
ACE InhibitorsACE Inhibitors
Adverse Effects:Adverse Effects:– Dry coughDry cough
– Kidney failureKidney failure
– Swelling of face, tongue or lips (angioedema)Swelling of face, tongue or lips (angioedema)
BP (dizziness or lightheaded)BP (dizziness or lightheaded)
Common ACE InhibitorsCommon ACE Inhibitors– Ramipril/AltaceRamipril/Altace
– Enalapril/VasotecEnalapril/Vasotec
– Fosinopril/MonoprilFosinopril/Monopril
– Lisinopril/Prinivil/ZestrilLisinopril/Prinivil/Zestril
Angiotensin II Receptor Angiotensin II Receptor BlockersBlockers (ARBs)(ARBs)
Prescribed forPrescribed for:: HTN, CHF HTN, CHF and Diabetic and Diabetic nephropathynephropathy
Mechanism of Action:Mechanism of Action:– ARBs block access of angiotensin II to its receptorsARBs block access of angiotensin II to its receptors
Results in vasodilation and reduced secretion of Results in vasodilation and reduced secretion of aldosterone and vasopressin, ultimately reducing aldosterone and vasopressin, ultimately reducing BP and myocardial workloadBP and myocardial workload
ARBsARBs
Hemodynamic Effects:Hemodynamic Effects: Rest & Ex HRRest & Ex HR
Rest & Ex BPRest & Ex BP
Exercise Capacity:Exercise Capacity:– No effectNo effect
Adverse Effects:Adverse Effects:– HeadacheHeadache
– AngioedemaAngioedema
– Low Blood PressureLow Blood Pressure
ARBsARBs
Common ARBsCommon ARBs– Irbesartan/AvaproIrbesartan/Avapro
– Losartan/CozaarLosartan/Cozaar
– Valsartan/DiovanValsartan/Diovan
DiureticsDiuretics
Prescribed for:Prescribed for: HTN, CHF, Peripheral edemaHTN, CHF, Peripheral edema Mechanism of Action:Mechanism of Action:
renal secretion of salt and waterrenal secretion of salt and water
– Inhibits sodium re-absorption at various sites of the Inhibits sodium re-absorption at various sites of the nephronnephron
intravascular volume & edemaintravascular volume & edema
DiureticsDiuretics
Hemodynamic Effects:Hemodynamic Effects: in Rest & Ex HRin Rest & Ex HR
or or in Rest & Ex BP in Rest & Ex BP
, PVCs or false positive on ECG, PVCs or false positive on ECG
Exercise Capacity:Exercise Capacity:– No changeNo change
DiureticsDiuretics
Adverse Effects:Adverse Effects:– Electrolyte abnormalitiesElectrolyte abnormalities
Hyper/HypokalemiaHyper/Hypokalemia
LDL-C & triglyceridesLDL-C & triglycerides
– HypovolemiaHypovolemia
Common DiureticsCommon Diuretics– Esidrix/Hydrochlorothiazide (HCTZ)Esidrix/Hydrochlorothiazide (HCTZ)
– Furosemide/LasixFurosemide/Lasix
– Spironolactone/AldactoneSpironolactone/Aldactone
DigitalisDigitalis
Prescribed forPrescribed for:: CHF and Atrial ArrhythmiaCHF and Atrial Arrhythmia Mechanism of Action:Mechanism of Action:
– Inhibits NaInhibits Na++-K-K++-ATPase-ATPase Limits ionic movement across myocardial cell Limits ionic movement across myocardial cell
membranemembrane
– Positive inotropic effect ( Positive inotropic effect ( myocardial myocardial contractility)contractility)
DigitalisDigitalis
Hemodynamic Effects:Hemodynamic Effects:– Sinus rhythm: Sinus rhythm: HR HR
– Afib or CHF: Afib or CHF: Rest & Ex HR Rest & Ex HR
Rest & Ex BPRest & Ex BP
– ““Dig effect”Dig effect” Non-specific ST-T changes and false positive Non-specific ST-T changes and false positive
exercise ECGexercise ECG
Exercise Capacity:Exercise Capacity: in patients with Afib or CHFin patients with Afib or CHF
in othersin others
DigitalisDigitalis
Adverse Effects:Adverse Effects:
– ToxicityToxicity Visual and neurological symptomsVisual and neurological symptoms ArrhythmiasArrhythmias
Common Digitalis MedicationsCommon Digitalis Medications
– Lanoxin/DigoxinLanoxin/Digoxin
Anti-Arrhythmic AgentsAnti-Arrhythmic Agents
Classified by electrophysiological effect:Classified by electrophysiological effect: Class IClass I::
conduction velocity, excitabilty & automaticityconduction velocity, excitabilty & automaticity
peripheral vasodilationperipheral vasodilation
– Prolong QRS or Long QT SyndromeProlong QRS or Long QT Syndrome
Common Class I MedsCommon Class I Meds– Lidocaine/XylocaineLidocaine/Xylocaine
– Propafenone/RhythmolPropafenone/Rhythmol
Anti-Arrhythmic AgentsAnti-Arrhythmic Agents Class IIClass II::
- ß-Blockers- ß-Blockers
Class IIIClass III::
– Mechanism of ActionMechanism of Action:: Blocks NaBlocks Na++ channels channels Negative chronotropic effectNegative chronotropic effect conductionconduction
myocardial Omyocardial O22 demand demand
Delays repolarizationDelays repolarization
Anti-Arrhythmic AgentsAnti-Arrhythmic Agents Class IIIClass III (con’t) (con’t)
– Hemodynamic Effect:Hemodynamic Effect: Rest & Ex HRRest & Ex HR Rest & Ex BPRest & Ex BP ECGECG
Exercise Capacity:Exercise Capacity: No effectNo effect
Adverse Effects:Adverse Effects: arrythmiasarrythmias Photosensitivity Photosensitivity Bradycardia/AV blockBradycardia/AV block Dermatological, GI, Dermatological, GI, HypotensionHypotension Hepatic or thyroid Hepatic or thyroid Electrolyte disturbance abnormalitiesElectrolyte disturbance abnormalities
Anti-Arrhythmic AgentsAnti-Arrhythmic Agents
Class IIIClass III (con’t) (con’t)
– Common Class III MedsCommon Class III Meds Amiodarone/CordaroneAmiodarone/Cordarone Sotalol/BetapaceSotalol/Betapace
Class IVClass IV::– Calcium Channel BlockersCalcium Channel Blockers
Platelet Aggregation InhibitorsPlatelet Aggregation Inhibitors
Mechanism of Action:Mechanism of Action:– Different for each medDifferent for each med
– ASAASA: : production of thromboxane A production of thromboxane A22
– PlavixPlavix: : binding of ADP to its platelet receptor binding of ADP to its platelet receptor
Hemodynamic Effect:Hemodynamic Effect:– No effectNo effect
Exercise Capacity:Exercise Capacity:– No effectNo effect
Platelet Aggregation InhibitorsPlatelet Aggregation Inhibitors
Adverse Effects:Adverse Effects:– Bruise easilyBruise easily
– Bleeding gumsBleeding gums
– Cuts and nicks bleed longerCuts and nicks bleed longer
– GI upsetGI upset
Common Platelet Aggregation InhibitorsCommon Platelet Aggregation Inhibitors– Clopidigrel/PlavixClopidigrel/Plavix
– Ticlopidine/TiclidTiclopidine/Ticlid
– Aspirin/Asaphen/ASAAspirin/Asaphen/ASA
AnticoagulantsAnticoagulants
Prescribed for: Venous thrombosis, pulmonary Prescribed for: Venous thrombosis, pulmonary embolism, Afib with embolization, prophylaxis embolism, Afib with embolization, prophylaxis after MIafter MI
Mechanism of Action:Mechanism of Action: – CoumadinCoumadin: inhibit synthesis of Vit K dependant : inhibit synthesis of Vit K dependant
clotting factorsclotting factors
– HeparinHeparin: prevents progression of existing clot by : prevents progression of existing clot by inhibiting any further clotting processesinhibiting any further clotting processes
AnticoagulantsAnticoagulants
Hemodynamic Effects:Hemodynamic Effects:– No effectNo effect
Exercise Capacity:Exercise Capacity:– No effectNo effect
Adverse Effects:Adverse Effects:– BleedingBleeding
– BruisingBruising
– GI bleedGI bleed
Diabetes ManagementDiabetes Management
Oral hypoglycemic agentsOral hypoglycemic agents– Used in Type 2 diabetes onlyUsed in Type 2 diabetes only
– Used in conjunction with diet and exerciseUsed in conjunction with diet and exercise
1 & 2) 1 & 2) Sulfonylureas & MeglitinidesSulfonylureas & Meglitinides– Mechanism of Action:Mechanism of Action: stimulates release of insulin fromstimulates release of insulin from
pancreatic islets to lower blood glucosepancreatic islets to lower blood glucose
– Adverse Effects:Adverse Effects: HypoglycemiaHypoglycemia
– Common MedicationsCommon Medications Glyburide/DiaBetaGlyburide/DiaBeta Repaglinide/GluconormRepaglinide/Gluconorm
DiabetesDiabetes
3)3) Alpha-glucosidase InhibitorsAlpha-glucosidase Inhibitors Mechanism of Action:Mechanism of Action:
– Reduce the rate of digestion of CHO, primarily lowering Reduce the rate of digestion of CHO, primarily lowering postprandial glucose concentrationspostprandial glucose concentrations
Adverse Effects:Adverse Effects:– FlatulanceFlatulance
– Cramps Cramps
– Abdominal distension, diarrheaAbdominal distension, diarrhea
– Liver dysfunctionLiver dysfunction
– *** Minimal*** Minimal chance chance of hypoglycemia of hypoglycemia
DiabetesDiabetes
4)4) BiguanidesBiguanides Mechanism of Action:Mechanism of Action:
production of glucose in the liver; production of glucose in the liver; glucose utilization glucose utilization at the muscleat the muscle
Adverse Effects:Adverse Effects:
– Lactic acidosis, nausea, diarrhea, loss of appetiteLactic acidosis, nausea, diarrhea, loss of appetite
– *** no risk of hypoglycemia*** no risk of hypoglycemia
Metformin/GlucophageMetformin/Glucophage
DiabetesDiabetes
5)5) Thiazolidinediones (Glitazones)Thiazolidinediones (Glitazones) Mechanism of Action:Mechanism of Action:
insulin resistance; insulin resistance; production of glucose by liver, production of glucose by liver, glucose uptake by muscleglucose uptake by muscle
Adverse Effects:Adverse Effects:– Expands blood volume; weight gain, edemaExpands blood volume; weight gain, edema– HeadacheHeadache– SinusitisSinusitis– MyalgiaMyalgia LDL-C & HDL-C, LDL-C & HDL-C, TriglyceridesTriglycerides
Pioglitazone/ActosPioglitazone/Actos
COPD ManagementCOPD Management
1) 1) GlucocorticosteroidsGlucocorticosteroids Prescribed for allergy symptoms and asthmaPrescribed for allergy symptoms and asthma Mechanism of Action:Mechanism of Action: suppresses suppresses
inflammation inflammation Adverse Effects:Adverse Effects:
– Hoarseness, difficulty speaking, slow growth in Hoarseness, difficulty speaking, slow growth in children, increased risk of cataracts, osteoporosis & children, increased risk of cataracts, osteoporosis & peptic ulcer diseasepeptic ulcer disease
Fluticasone Propionate/FloventFluticasone Propionate/Flovent
COPDCOPD
2)2) Leukotriene Receptor AntagonistsLeukotriene Receptor Antagonists To prevent symptoms caused by asthma, chronic To prevent symptoms caused by asthma, chronic
bronchitis, emphysema and other lung diseases.bronchitis, emphysema and other lung diseases. Mechanism of Action:Mechanism of Action:
– Block cysteinyl leukotrienes from binding to their Block cysteinyl leukotrienes from binding to their receptors, preventing bronchoconstriction and mucous receptors, preventing bronchoconstriction and mucous productionproduction
Adverse Effects:Adverse Effects:– Generally well toleratedGenerally well tolerated
Monteluekast Sodium/SingulairMonteluekast Sodium/Singulair
COPDCOPD
3)3) BetaBeta22-adrenergic Stimulants-adrenergic Stimulants To prevent symptoms caused by asthma, To prevent symptoms caused by asthma,
chronic bronchitis, emphysema and other lung chronic bronchitis, emphysema and other lung diseases.diseases.
Mechanism of Action:Mechanism of Action:– Selective activation of BetaSelective activation of Beta22-adrenergic receptors to -adrenergic receptors to
promote bronchodilation and relieve bronchospasm.promote bronchodilation and relieve bronchospasm. Adverse Effects:Adverse Effects:
– ßß1 1 –adrenergic receptors in the heart could be –adrenergic receptors in the heart could be stimulated causing stimulated causing Tachyarrhythmias and AnginaTachyarrhythmias and Angina
– Musculoskeletal tremorsMusculoskeletal tremors Albuterol/VentolinAlbuterol/Ventolin
COPDCOPD
4) 4) AnticholinergicsAnticholinergics To prevent symptoms caused by asthma, To prevent symptoms caused by asthma,
chronic bronchitis, emphysema and other lung chronic bronchitis, emphysema and other lung diseases.diseases.
Mechanism of Action:Mechanism of Action:– Promotes bronchodilationPromotes bronchodilation
Adverse Effects:Adverse Effects:– Dry mouthDry mouth
– Irritation of pharynxIrritation of pharynx
Atrovent/Ipratropium Bromide Atrovent/Ipratropium Bromide
Lipid ManagementLipid Management
1)1) HMG CoA Reductase Inhibitors (STATINS)HMG CoA Reductase Inhibitors (STATINS)
Mechanism of Action:Mechanism of Action: cholesterol productioncholesterol production
– Increase number of LDL receptors on hepatocytes, Increase number of LDL receptors on hepatocytes, enhancing the elimination of LDL from the bloodenhancing the elimination of LDL from the blood
Beneficial Cardiovascular ActionsBeneficial Cardiovascular Actions:: LDL, LDL, HDL, Promote plaque stability HDL, Promote plaque stability
– Improve abnormal endothelial function; enhanced Improve abnormal endothelial function; enhanced vessel dilation & reduce risk of thrombosisvessel dilation & reduce risk of thrombosis
LipidsLipids
Adverse Effects:Adverse Effects:– Generally well toleratedGenerally well tolerated
– Headache; rash; GI disturbance; Myopathy Headache; rash; GI disturbance; Myopathy (Rhabdomyolysis)(Rhabdomyolysis)
Common Medications:Common Medications:– Atorvastatin/LipitorAtorvastatin/Lipitor
– Simvastatin/ZocorSimvastatin/Zocor
– Rosuvastatin/CrestorRosuvastatin/Crestor
– Pravastatin/PravacholPravastatin/Pravachol
LipidsLipids
2)2) Ezetimibe/EzetrolEzetimibe/Ezetrol TC, LDL, Trigs & can TC, LDL, Trigs & can HDLHDL Mechanism of Action:Mechanism of Action:
– Blocks absorption of dietary and bile-secreted Blocks absorption of dietary and bile-secreted cholesterolcholesterol
Adverse Effects:Adverse Effects:– Generally well toleratedGenerally well tolerated
LipidsLipids
3)3) Fibric Acid Derivatives (FIBRATES)Fibric Acid Derivatives (FIBRATES)
Most effective for Most effective for Trigs & Trigs & HDL HDL
Mechanism of Action:Mechanism of Action:– Activate receptors to accelerate the clearance of Activate receptors to accelerate the clearance of
VLDLs, and thereby reduce levels of TGsVLDLs, and thereby reduce levels of TGs
Adverse Effects:Adverse Effects:– Generally well toleratedGenerally well tolerated
– Rashes and GI disturbancesRashes and GI disturbances
Gemfibrizol/LopidGemfibrizol/Lopid
LipidsLipids
4)4) Nicotinic AcidNicotinic Acid Mechanism of Action:Mechanism of Action: VLDL production, VLDL production,
therefore therefore LDL levels and LDL levels and HDL levels HDL levels Adverse Effects:Adverse Effects: flushing, GI disturbances, flushing, GI disturbances,
gallstones, hepatotoxicitygallstones, hepatotoxicity Common Medications:Common Medications:
– Niacin/NiaspanNiacin/Niaspan