Basic Pharmacology Cardio Drugs

Basic PharmacologyCardiovascular Drugs

Case Study 1

35 YO male, a police officer, 5’11’’, weight=258 lbs (BMI=??____)

Hx: hypertension (BP 140/80), anxiety. Has taken testosterone supplements in past, now uses “body building” shakes.

Family Hx: Father, paternal grandfather-DMLabs: FBS=79, TSH normal

Case Study 1Visit 1 TC= 167 TG= 539 HDL= 18 LDL= 243

Diagnosis?What drug/s will you prescribe? Discuss the available preparation, dosing, MOA, drug

interaction, adverse effect, excretion of the chosen drug/s.

Case Study 2

39 YO male with frequent urination causing sexual activity disturbance, with excessive thirst, blurred vision.

Hx: Obesity, BMI= 33Family Hx: Mother has DMMeds: NoneNon-fasting Accucheck (Total chol)= 297

Case Study 2

TCTC 305305 252252TrigTrig 540540 149149HDLHDL 170170 3333LDLLDL 295295 190190HgbA1CHgbA1C 11.911.9 5.65.6

Diagnosis?What drug/s will you prescribe? Discuss the available preparation, dosing, MOA, drug interaction, excretion, adverse effect of the chosen drug/s.

Case Study 3

62 YO Female with CHD s/p CABG wanted me to manage lipids. She also has Hypertension.

Meds: Clopidogrel, Atenolol, Lisinopril, Atorvastatin (stopped by Pt due tomyalgias)

Current labs:TC= 248Trig= 178HDL= 22LDL= 156

Case Study 3

• Diagnosis?• What drug/s will you prescribe? • Discuss the available preparation, dosing,

MOA, drug interaction, excretion, adverse effect of the chosen drug/s.

Case Study 458 Year old male, smokerFamily Hx: Mother with DM, sister died age 35 from MIBP= 160/90 Pulse 78Labs: TC= 310, TG= 250, HDL=29, LDL=156, FBS=88

• Based on score, what is LDL goal?• Diagnosis?• What drug/s will you prescribe? • Discuss the available preparation, dosing, MOA, drug

interaction, excretion, adverse effect of the chosen drug/s.

Case study 574 Year old Male (smoker), experiencing angina on and off, had

MI last year, advised angioplastyFam. Hx: Mother with NIDDM, sister died age 70 from MIBP= 120/70 Pulse 82Labs: TC= 210, TG= 132, HDL=35, LDL=236, FBS 139

• Diagnosis?• What drug/s will you prescribe? • Discuss the available preparation, dosing, MOA, drug

interaction, adverse effect, excretion of the chosen drug/s.

Case Study 648 Year old male, smoker, diabeticFamily Hx: Mother withHPN, father had strokeBP= 130/90 Pulse 69Labs: TC= 210, TG= 370, HDL=46, LDL=216, FBS=149

• Based on score, what is LDL goal?• Diagnosis?• What drug/s will you prescribe? • Discuss the available preparation, dosing, MOA, drug

interaction, excretion, adverse effect of the chosen drug/s.

Thank You

• Questions?

JOSEPHINE S. JIMENEZ, MDINTERNAL MEDICINE

UPCM 2006

Thank you!!

ATHEROSCLEROSIS

The Heart

The function of the heart --circulate blood throughout the body by:

•Pumping blood through the lungs removes carbon dioxide and refreshes the blood with oxygen

•The oxygenated blood is pumped to the body to provide oxygen and nutrients and to remove waste products.

•The coronary arteries are the blood vessels that supply blood and oxygen to the heart muscle.

Coronary Artery Disease• Coronary artery disease is one of the most common and serious

effects of aging. • Fatty deposits build up in blood vessel walls and narrow the

passageway for the movement of blood. • The resulting condition, called atherosclerosis often leads to

eventual blockage of the coronary arteries and a “heart attack”.

Signs and Symptoms• None: This is referred to as silent ischemia.

Blood to your heart may be restricted due to CAD, but you don’t feel any effects.

• Chest pain: If your coronary arteries can’t supply enough blood to meet the oxygen demands of your heart, the result may be chest pain called angina.

• Shortness of breath: Some people may not be aware they have CAD until they develop symptoms of congestive heart failure- extreme fatigue with exertion, shortness of breath and swelling in their feet and ankles.

• Heart attack: Results when an artery to your heart muscle becomes completely blocked and the part of your heart muscles fed by that artery dies.

Signs & Symptoms

NoneChestPain

ShortnessOf Breath

HeartAttack

• High blood cholesterol• High blood pressure• Smoking• Obesity• Lack of physical activity

Risk FactorsNonmodifiable

•Sex•Hereditary•Race•Age

Modifiable

•High blood pressure•High blood cholesterol•Smoking•Physical activity•Obesity•Diabetes•Stress and anger

Management

• Many people are able to manage coronary artery disease with lifestyle changes and medications.

• Other people with severe coronary artery disease may need angioplasty or surgery.

Stenting• a stent is introduced into a blood vessel on a balloon catheter and advanced into the blocked area of the artery

• the balloon is then inflated and causes the stent to expand until it fits the inner wall of the vessel, conforming to contours as needed

• the balloon is then deflated and drawn back

•The stent stays in place permanently, holding the vessel open and improving the flow of blood.

Angioplasty• a balloon catheter is passed through the guiding catheter to the area near the narrowing. A guide wire inside the balloon catheter is then advanced through the artery until the tip is beyond the narrowing.

• the angioplasty catheter is moved over the guide wire until the balloon is within the narrowed segment.

• balloon is inflated, compressing the plaque against the artery wall

• once plaque has been compressed and the artery has been sufficiently opened, the balloon catheter will be deflated and removed.

Bypass surgery

• healthy blood vessel is removed from leg, arm or chest

• blood vessel is used to create new blood flow path in your heart

• the “bypass graft” enables blood to reach your heart by flowingaround (bypassing) the blocked portion of the diseased artery. The increased blood flow reduces angina and the risk of heart attack.

DYSLIPIDEMIA

Bad Effects of Dyslipidemia

According to the Third Report of the National Cholesterol Education Program Expert Panel on Detection, Evaluation and Treatment of High Cholesterol in Adults

(NCEP ATP-III):

High LDL levels are a leading cause of coronary heart disease (CHD) and should be the main target of any cholesterol lowering regimen

ATP III Lipid and Lipoprotein Classification

LDL Cholesterol (mg/dl) HDL Cholesterol (mg/dl)<100 Optimal < 40 Low100-129 Near/Above Optimal > 60 High (Desirable)130-159 Borderline High160-189 High>190 Very High

Categories of Risk that Modify LDL GoalsCHD and CHD risk equivalents <100Multiple (2+) risk factors <130Zero to one risk factor <160

Current ATP III Guidelines for Treating LDL Cholesterol

Risk Risk CategoryCategory

LDL GoalLDL Goal(mg/dl)(mg/dl)

LDL level to LDL level to initiate TLCinitiate TLC

LDL level to LDL level to consider Rx consider Rx therapytherapy

CHD or CHD or EquivalentsEquivalents

<100<100<70 Ideal<70 Ideal

> 100> 100 >> 130 130(100-129 Rx (100-129 Rx optional)optional)

2+ Risk 2+ Risk FactorsFactors

<130<130 > 130> 130 >> 130 (10 Year 130 (10 Year risk 10-20%)risk 10-20%)>> 160 (Risk <10%) 160 (Risk <10%)

0-1 Risk 0-1 Risk FactorFactor

<160<160 > 160> 160 >> 190 190(160-189 Rx (160-189 Rx optional)optional)

Specific Dyslipidemias: Very High LDL (> 190mg/dl)

Causes and Diagnosis

• Genetic disordersMonogenic familial hypercholesterolemiaFamilial defective apolipoprotein B-100 (Apo B)Polygenic hypercholesterolemia

• Family testing to detect affected relatives

Specific Dyslipidemias: Low HDL

Causes of Low HDL (<40 mg/dl)

• Elevated triglycerides• Overweight and obesity• Physical Inactivity• Type 2 diabetes• Cigarette smoking• Very high carb. intakes (>60% energy)• Medications (some beta blockers, anabolic steroids,

progestational agents)

Specific Dyslipidemias: Elevated Triglycerides

Classification of Serum Triglycerides

Normal <150 mg/dl Borderline High 150-199 mg/dl High 200-499mg/dl Very High >500 mg/dl


Causes of Elevated Triglycerides

• Obesity and overweight• Physical Inactivity• Cigarette smoking• Excess alcohol intake• High carb. diets• Several diseases (Type 2 DM, chronic renal failure, nephrotic

syndrome• Medications (corticosteroids, estrogens, retinoids, higher

doses of beta blockers


Management of Very High Triglycerides (>500 mg/dl)

• Goal of therapy: Prevent acute pancreatitis• Very low fat diets (< 15% of caloric intake)• Triglyceride-lowering drug usually required (fibrate or

nicotinic acid)• Reduce triglycerides before lowering LDL

Anti Anginal Drugs

• Organic Nitrates• Calcium Channel Blockers

• Beta receptor Blockers

Coronary vessels:Coronary vessels: blood supply for the blood supply for the heartheart

1. OVERVIEW1. OVERVIEW

Coronary atherosclerosis:Coronary atherosclerosis: cause of cardiac ischemiacause of cardiac ischemia

Myocardial Myocardial oxygen demandoxygen demand is is diminisheddiminished by:by:

• Reducing contractilityReducing contractility• Reducing heart rate Reducing heart rate • Reducing the preloadReducing the preload• Reducing the afterloadReducing the afterload


Wall tension Wall tension


•Myocardial Myocardial oxygen oxygen supplysupply is chiefly is chiefly determined by:determined by:

• AV oxygen differenceAV oxygen difference• Regional myocardial Regional myocardial distribution distribution • coronary blood flow: coronary blood flow: • vascular resistance, artery pressure

Effects of antianginal drugs:Effects of antianginal drugs:

Reducing oxygen demandsReducing oxygen demands Reducing heart rate and contractilityReducing heart rate and contractility Dilating systemic arteries and veins ( Dilating systemic arteries and veins ( wall tension by wall tension by

lowering heart loads)lowering heart loads)

Increasing oxygen supplyIncreasing oxygen supply Dilating conduct coronary arteries ( Dilating conduct coronary arteries ( coronary blood flow) coronary blood flow) Promoting regional distribution ( Promoting regional distribution ( in ischemic regions) in ischemic regions)

Others:Others: Anti- platelet coagulation and thrombus formationAnti- platelet coagulation and thrombus formation


2.1 Nitrates2.1 NitratesNitroglycerinNitroglycerin

A. Pharmacological actionsA. Pharmacological actions

Dilating vessels and reducing heart loadsDilating vessels and reducing heart loads wall tension wall tension ; ; reflex tachycardiareflex tachycardia Redistribution of coronary circulationRedistribution of coronary circulation dilating conduct artery:dilating conduct artery: collateral circulation collateral circulation reducing wall tension:reducing wall tension: blood flow in ischemic subendocardial area blood flow in ischemic subendocardial area

2. Antianginal drugs2. Antianginal drugs

B. Clinical usesB. Clinical uses• Angina pectoris: Angina pectoris: all kinds, especially stable typeall kinds, especially stable type• Heart failureHeart failure ：： reducing heart loads due to vasodilationreducing heart loads due to vasodilation

C. Adverse reactionsC. Adverse reactions• Increase in heart rate and contractilityIncrease in heart rate and contractility• Symptoms due to vasodilation:Symptoms due to vasodilation: headache, flash, postural headache, flash, postural hypotension, collapse, hypotension, collapse, etcetc..• Others:Others: methaemoglobinaemia methaemoglobinaemia• Tolerance : avoiding steady-state plasma concentration; avoiding steady-state plasma concentration; • supplement of agents containing supplement of agents containing ––SH SH (captopril)(captopril)


2.1 Other nitrates Isosorbide dinitrate Isosorbide-5-mononirate Compared with nitroglycerin:Compared with nitroglycerin:• Similar but weaker effect• Acting slowly but lasting longer• Larger individual variation and more adverse effects


2.2 2.2 receptor blockers receptor blockersA. Pharmacological actionA. Pharmacological action• Reducing oxygen demand:Reducing oxygen demand:• heart rate and contractility heart rate and contractility • Increasing oxygen supply:Increasing oxygen supply:• diastolic period diastolic period : : perfusion time perfusion time • vascular tone in normal regions vascular tone in normal regions : : • blood flow in ischemic regions blood flow in ischemic regions

• Others:Others:• Improving myocardial metabolismImproving myocardial metabolism• Inhibiting coagulation of plateletsInhibiting coagulation of platelets


B. Clinical usesB. Clinical uses stablestable and and unstableunstable pectorispectoris, , especially associated with especially associated with

hypertension or arrhythmias, even with myocardial infarctionhypertension or arrhythmias, even with myocardial infarction; ; but not but not used forused for variant angina pectorisvariant angina pectoris

C. NotesC. Notes• Dose individualization: Dose individualization: starting from small dosestarting from small dose • Withdraw gradually and slowly: Withdraw gradually and slowly: symptomsymptom reboundrebound

• Combination with nitroglycerinCombination with nitroglycerin


2.3 Calcium channel blockers2.3 Calcium channel blockers


2.3 Calcium channel blockers2.3 Calcium channel blockers

A. Pharmacological actionsA. Pharmacological actions

• Reducing myocardial oxygen remand:Reducing myocardial oxygen remand:• heart loads heart loads : : nifedipinenifedipine• heart rate and contractilityheart rate and contractility :: verapamil and diltiazemverapamil and diltiazem

• Increasing myocardial blood supplyIncreasing myocardial blood supply• Protecting ischemic myocardial cellsProtecting ischemic myocardial cells• Inhibiting coagulation of plateletsInhibiting coagulation of platelets


Actions of calcium channel blockersActions of calcium channel blockers

B. Clinical usesB. Clinical uses

stable and variant type:stable and variant type: nifedipine, verapamil, diltiazemnifedipine, verapamil, diltiazem

unstable type:unstable type: verapamil, diltiazemverapamil, diltiazem


Actions of DHP (like nifedipine) are similar to those of nitroglycerinActions of DHP (like nifedipine) are similar to those of nitroglycerin

Actions of verapamil and diltiazem are similar to those of Actions of verapamil and diltiazem are similar to those of blockers blockers

2.4 Other drugs2.4 Other drugs

ACEIs ACEIs •Treating hypertension and preventing ischemic heart Treating hypertension and preventing ischemic heart disease disease •Reducing heart loadsReducing heart loads•Inhibiting cardial remodeling Inhibiting cardial remodeling

NicorandilNicorandil• Opening ATP-sensitive KOpening ATP-sensitive K++ channel (K channel (KATPATP) ) • Lowering intracellular CaLowering intracellular Ca2+2+

• Providing NO (like nitroglycerin)Providing NO (like nitroglycerin)•Inducing ischemic preconditioning Inducing ischemic preconditioning


Molsidomine Molsidomine •Inhibiting adenosine uptake and cAMP degradation Inhibiting adenosine uptake and cAMP degradation •Inhibiting pletelet aggregationInhibiting pletelet aggregation•Promoting collateral circulation after long-term usePromoting collateral circulation after long-term use

DipyridamoleDipyridamole• Inhibiting adenosine uptake and cAMP degradation Inhibiting adenosine uptake and cAMP degradation •Inhibiting pletelet aggregationInhibiting pletelet aggregation•Promoting collateral circulation after long-term usePromoting collateral circulation after long-term use


nitroglycerinnitroglycerin blockers blockers CaCa2+2+ antagonists antagonists combination*combination*Heart rateHeart rate Contractility Contractility //Wall tensionWall tension // //

Oxygen demandOxygen demand Blood pressureBlood pressure

: increase, : increase, : markedly increase; : markedly increase; : decrease, : decrease, : markedly : markedly decrease; decrease; : variable according to the dose and effect of each drug ; : variable according to the dose and effect of each drug ;

* * blockers blockers combined with nitroglycerin or Cacombined with nitroglycerin or Ca2+2+ antagonists ( antagonists (nifedipine; nifedipine; combination with verapamil/diltiazem not be recommendatedcombination with verapamil/diltiazem not be recommendated))

Caution:Caution: Combination may potentiate the antianginal Combination may potentiate the antianginal effects, but may induce severe hypotensioneffects, but may induce severe hypotension

3. Summary of antianginal drugs3. Summary of antianginal drugs

Basic Pharmacology Cardio Drugs

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