PHARMACOLOGY Cardiac Wellness Institute of Calgary Updated May 2010.

PHARMACOLOGYPHARMACOLOGY

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..

Cardiac MedicationsCardiac Medications

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


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


– ““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


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


Adverse Effects:Adverse Effects:– BleedingBleeding

– BruisingBruising

– GI bleedGI bleed

Other Commonly Used Other Commonly Used MedicationsMedications

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


– 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


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


– 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

PHARMACOLOGY Cardiac Wellness Institute of Calgary Updated May 2010.

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Transcript of PHARMACOLOGY Cardiac Wellness Institute of Calgary Updated May 2010.