Medications for Common Heart Conditions

A little About Ourselves:

Names: Rakesh Dewan, Lily Liang, Janet Truong, and Josh McPherson

We are 2nd year pharmacy students from the University of British Columbia

Purpose

We will focus on the use of common medications used for different cardiovascular conditions

We hope to provide you with information that will lead to a safe, effective, and positive medication experience

Objectives

Learn how different medications work

Become aware of potential side effects and how to manage them

Dispel common myths about heart medications

Outline StatinsACE inhibitors ARBsDiuretics Beta-blockersCalcium channel blockersBlood thinnersNitrates

Cholesterol Lowering Drugs HMG-CoA Reductase Inhibitors (AKA: “Statins”)

Examples: Drug (brand) Simvastatin (Zocor) Atorvastatin (Lipitor) Fluvastatin (Lescol) Pravastatin (Pravachol) Lovastatin (Mevacor) Rosuvastatin (Crestor)

Statins most effective and well tolerated LDL lowering agents

38-54% reduction of LDL

used in addition to dietary and lifestyle modifications to lower LDL cholesterol

lowering of LDL has been shown to reduce risk of heart attack and stroke

equally effective at heart attack and stroke prevention

How Statins WorkHMG-CoA reductase is an enzyme that is

responsible for an important step in the production of cholesterol in the liver.

Statins block the action of HMG-CoA reductase leading to lowered LDL (bad cholesterol)

HMG-CoA molecule Mevalonate Cholesterol

HMG-CoA Reductase blocked by statins

How Statins Work

Primary action through lowering the liver production of LDL

Side Effects Statins are generally well tolerated

Upset stomach: can manage by taking Statin medication with food

Headache: can manage by treatment with non-prescription pain medication (Tylenol or Advil)

Unexplained muscle pain: Contact Doctor or Pharmacist

Tips

AVOID Grapefruit juice: grapefruit juice can increase the side effects of most statins

liver function test

total cholesterol:

20% diet + 80% produced in liver

Skill Testing Question Statins work by:

a) Blocking the actions of cholesterol b) Inhibiting HMG-CoA which is an enzyme found

in the liver responsible for LDL production c) Inhibiting HMG-CoA which is an enzyme found

in the kidney responsible for LDL production d) Inhibiting HMG-CoA which is an enzyme found

in the liver responsible for HDL production

Inhibitors of AngiotensinAngiotensin Converting Enzyme (ACE) InhibitorsAngiotensin Receptor Blockers (ARBs)

General Used For:High Blood PressureHeart FailureStable AnginaPost Myocardial Infarction......

BUT HOW DO THEY WORK, SIDE EFFECTS..??

Angiotension Converting Enzyme Inhibitors (ACEI)

What are some of these medications?Captopril (CAPOTEN)Enalapril (VASOTEC)Ramipril (ALTACE)Lisinopril (PRINIVIL, ZESTRIL)Quinapril (ACCUPRIL)Trandolapril (MAVIK)Benazepril (LOTENSIN)

“The Prils...”

2.5 mg

5 mg

10 mg

20 mg

25 mg

ACEI: How Does It Work?To understand how ACE inhibitors and also

how ARBs work, one must understand the Angiotensin-Renin Pathway......

20% of patients with hypertensionhave abnormally HIGH renin-angiotnesinactivity

ACE Inhibitors: A Closer LookAngiotensin Converting Enzyme (ACE) is a

natural enzyme found in our body that works to increase blood pressure

ACE Inhibitors work by preventing this enzyme from working, thereby, decreasing diastolic/ systolic blood pressure

ACEI: But Are They Effective?in Post- MI patients:

reduce afterload and preload prevent complications such as left ventricular

remodeling (aka hypertrophy) and HF

shown to improve overall survival, decrease development of severe heart failure, and reduce re-infarction and heart failure hospitalization rates

• benefits begin within first few days of therapy

ACE Inhibitors: Side EffectsDry Cough!

-> SOLUTION?

Sore Throat/ Fever?

Others: metallic taste feeling, rash possibly, hypotension (low blood pressure)

Ace Inhibitors: TipsImportant that Doctor and Pharmacist are

aware of all prescription, non-prescription, and natural health medications

NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)

Others: Iron, Lithium, Diuretics, Allopurinol to name a few

ACEI: What Do You Think?ACEIs are known to increase potassium

levels in the blood, would a diuretic that is not potassium sparing:

a) Increase the potassium further in the bloodb) Decrease the potassium in the blood to

balance it with the ACEIc) Do nothing

Angiotension Receptor Blockers (ARBs)What are some of these medications?

Candesartan(ATACAND)Eprosartan (TEVETEN) Irbesartan (AVAPRO)Losartan (COZAAR)Olmesartan (BENICAR)Telisartan (MICARDIS)Valsartan (DIOVAN)

Do you see a pattern in the naming?

ARB: How Does It Work?Recall the renin-angiotensin pathway......

ARBs Inhibitors: A Closer Look

Again, the main action is to relax the arteries in order to allow for more blood flow....

Uses are similar to ACEI, recall....hypertension, post-MI, heart failure, stable angina....often useful if ACEI intolerable

Benefits? similar to ACEI; first-line in non-blacks and for patients with diabetes or ischemic heart disease

ARBs: Side Effects

Digestive Nausea, vomiting, diarrheaBody: headache, dizzinessWhat about cough?? Others: metallic taste, hypotension, rash

Side effects are usually mild and transient

ARBs: TipsImportant that Doctor and Pharmacist are aware of all

prescription, non-prescription, and natural health medications

Diuretics: may occasionally experience an excessive reduction of blood pressure after initiation of therapy; can be minimized by discontinuing the diuretic prior to initiation of treatment and/or lowering the initial dose of ARB

Potassium Supplements/ Drugs that Increase Potassium (ie. Potassium sparing diuretics).....

ARBs: What do You think?Which of the following is FALSE?

a) ARB stands for Angiotensin Receptor Blockerb) ARBs can cause coughing, just like ACEIsc) ARBs are useful for the management of hypertension

What else?What else can I do?

Manage a health weightRegular exercise: 23 ½ hours?? Healthy eatingMedication compliance Find Heart Disease Resource Groups!

Diuretics 3 classes – “water pill”

I. Thiazides

II. Loop Diuretics

III. Potassium Sparing Diuretics

How do diuretics lower blood pressure?Removal of sodium (salt) and water from the body

I. Thiazide DiureticsCommon Examples: HydrochlorothiazideIndapamideChlorothiazideMetoazone

How do Thiazides work?A: They act on the DCT and inhibit Na+ and Cl- transporters

USES: High blood pressure

I. Thiazide DiureticsWhere do Thiazides work?

What percentage of sodium reabsorption happen in the DCT?

~5%

II. Loop DiureticsCommon Examples: Furosemide (Lasix)

How do Loop Diuretics work?A: Similar to Thiazides except they act on the ascending

loop of Henle

USES: High blood pressure, and edema associated with heart failure

II. Loop DiureticsWhere do Loop Diuretics work?

What percentage of sodium reabsorption happens in the ascending loop of Henle?

~25%

III. Potassium Sparring DiureticsCommon Examples: AmilorideTriamtereneSpironolactone

How do Potassium Sparring Agents work?A: Prevent the loss of potassium and interferes with the

sodium-potassium exchange sites in the CT

USES: High blood pressure, combination with other diuretic drugs to prevent hypokalemia

DiureticsCommon Side Effects:

Upset stomach/Abdominal pain Frequent Urination Dryness of mouth Thirst Dizziness Photosensitivity* Low potassium levels*

DiureticsHelpful Tips:

Take with food Take medication early in the day, or at a flexible time to

suit you Drink lots of water Rise slowly from a seat or lying position Apply sunscreen* Potassium rich foods*

II. Beta-BlockersCommon Examples: Propanolol PindololLabetaololMetoprolol Bisoprolol Atenolol

How do Beta-Blockers work?A: reducing heart rate and blood pressure

USES: High blood pressure, angina, and heart failure

II. Beta-BlockersCommon Side Effects:

Drowsiness Fatigue Dizziness and lightheadedness Dryness of the mouth, eyes and skin Cold hands and feet

II. Beta-BlockersHelpful Tips:

Rise slowly from a seat or lying position Drink lots of water Prepare ahead of time Exercise

Calcium Channel Blockers

Drug (Brand) _

Amlodipine (Norvasc) Nifedipine (Adalat) Felodipine (Plendil) Diltiazam (Cardizem) Verapamil (Isoptin)

Calcium Channel Blockers Used alone or in combination with other

medications for the treatment of:

- hypertension -angina -irregular heart beats -migraines -Reynaud's syndrome -Brain aneurysm complications

How Calcium Channel Blockers WorkWhen a muscle fibre is stimulated, calcium channels

open and allow calcium to rush inCalcium activates a protein called calmodulin Calmodulin bound to calcium starts the pathway

that leads to muscle contraction Calcium channel blockers block the calcium

channels that are present on the muscle fibres of vasculature and the heart

End result is less contraction of vasculature and heart muscles leading to dilated vasculature or decreased force of heart contraction

How Calcium Channel Blockers Work

block calcium influx

decreased muscle

contraction

dilated blood

vessels and softer

heart contractio

ns

Side Effects Dizziness: changing positions slowly may help to avoid sudden

dizziness

Flushing: strategies to help cool down may include the use of

fans, layering clothes, or applying cool water to over-heated areas

Ankle Swelling: support socks or stockings and elevation of the legs

may be helpful

TipsGrapefruit juice may increase the levels of

calcium channel blockers leading to increased risk of side effects

Some herbal supplements may counteract the desired effects of calcium channel blockers

Some herbal supplements may lead to additive decrease in blood pressure leading to increased side effects.

Skill Testing Question While on a Calcium Channel Blocker:

a) Grapefruit juice should be regularly consumed to ensure effective therapy

b) Blood vessels are usually constricted due to calcium channel blocker

c) Herbal supplements that are known to decrease blood pressure may lead to more side effects (dizzyness, flushing, etc.)

d) A common side effect is joint and muscle pain

Blood Thinners: Anti-Coagulants

Delay the clotting time through inferring with a series of chemical reactions that result in blood clots in arteries and veins.

Oral examples:Warfarin (Coumadin)Dabigatran (Pradax)Rivaroxaban (Xarelto)

WarfarinHow does it work?

Inhibit the synthesis of vitamin K dependent clotting factors by blocking vitamin K reduction enzyme activity.

WarfarinSide effects:

GasFatigue, dizzinessDecreased clotting time for woundsEasily bruisedGI bleeds

Tips of taking warfarin:Regular INR blood test Unexpected bleedings (e.g increased frequency

of nose bleeds)Take on an empty stomachSame time daily

WarfarinSpecial Dietary consideration:

1) Vitamin K:-high intake can reduce the effectiveness of warfarin-daily dietary needs are 80 mcg (recommended 90-

120mcg)- mainly in dark leafy green vegetables.

Examples: Cabbage, brussel sprouts, collard greens, kale, lentils, soybean oil, spinach, turnip greens, asparagus, cheese, beef liver, green tea.

*Does that mean I have to cut off from green vegetables?-No

Or considering eating more low Vitamin K greens:- Green beans, peas, celery, cucumber, pepper, zucchini.

Warfarin2) Alcohol: - >3 drinks daily can increase the effect of warfarin.

1 drink = 5 ounces of wine, 12 ounces of beer, 1 ½ ounces of liquor

*Best to avoid all alcoholic beverages.

3) Vitamin E:-avoid high doses (1,000 IU increases the risk of bleeding, 800 IU may be safe, more studies needed).

4) Herbal Supplements:Examples: garlic, ginkgo biloba, St. John’s Wort, arnica, wheat grass, bilberry, ginger.*check with pharmacist

5) OTC:- Limit use of Advil, Motrin, Aleve, Aspirin.

Game of Truth……….or False1) Warfarin reduces already formed clots.

False

Dabigatran (Pradax)How does it work?

Direct reversible inhibition of thrombin that mediates a coagulation cascade producing blood clotting.

DabigatranSide effects:

nausea, diarrheaUpset stomach, stomach painsHeart burn, indigestionEasily bruised (mild)

Interactions:herbal supplement and OTC similar to those of warfarin.antacids

Tips:With or without foodSwallow wholeOutside stable for 30 days.

Warfarin or Dabigatran?Advantages of Dabigatran:

Less incidences of bleedingsLess INR monitoring are needed Less dosage adjustment are needed.May have less drug interactions.Less food interaction, especially no restrictions on

Vit K foods.

Disadvantages of Dabigatran:Twice daily dosing rather than one daily dosing in

Coumadin.Relative new drug, long term effects are no knownMore expensive, not covered by Pharmacare.

Blood Thinner: Platelet Aggregation Inhibitor

Inhibit platelets from clumping together to form blood clots in vessels.

Oral examples:Acetylsalicylic acid (Aspirin, Anacin,

Entrophen)Clopidogrel (Plavix)Dipyridamole (Parsantine)

ASA (Aspirin) How does it work?

Permanent blockage of COX-1, leading to inactivation of COX system and subsequent blood clotting.

COX-1 derives TXA2, which induces platelet aggregation.

ASA

Does that mean I have no functional platelets while I am ASA?

-New platelets are continuously produced-10-20% platelet replaced-ASA inhibition for 1 hour out of 24 hour cycle

- low percentage of platelets are inactivated.

ASASide effects:

Heart burn, upset stomachNauseaincreased risk of GI bleeds

Things to avoid/limit:1) NSAIDs (Aleve, Advil, Motrin)

Infrequent use take ASA 1st.

2) Alcohol

3) Curry powder, paprika and licorice (large amount)

3) Herbal supplements examples: Glucosamine, ginkgo biloba, ginseng *check with pharmacist.

ASATips:

75mg -325mg daily used in practice.Don’t crush EC tabletFull glass of water (8 ounces)Avoid laying down for 10 minutes after useShould not be taken in event of a stroke.

Cool facts:Can prevent vascular death by 15% and

nonfatal vascular events by 30%.

Clopidogrel (Plavix)How does it work?

Permanent inhibition of adenosin diphosphate (ADP) binding to platelet receptors on platelet membrane that causes aggregation.

ClopidogrelSide effects:

Easily bruisedFatigue, dizziness and headacheDiarrhea, constipationIncreased risks of GI bleedingSkin related reactions (rashes, itchiness) *due to nature of

reaction may resemble that of allergic reaction, consult your pharmacist or doctor before continuing or discontinuing.

Interactions: 1) NSAIDs (Advil and Aleve)

2) Herbal Examples: blueberry, anise, garlic, ginger, ginkgo biloba, ginseng, green tea Check with pharmacist*

Tips:Take with or without food.

Anti-coagulants or antiplatelets

Question: Aren’t they both anti-clotting agents, don’t they do the same thing? Should I take both?

Different mechanisms in blood clotting formations.

Ongoing debate on which is more effective in prevention of stroke or thrombus.

Decision for taking combination therapy is highly dependent on the medical condition and should only be made in discussion with your doctor.

Are there non-drugs measures I can do to prevent blood clots in blood vessels?Avoid squatting, sitting or crossing

your legs for long periods of time.inactive for long time, walk around

for few minutes every one to two hours.

flex your ankles, curl your feet or toes more often through the trip.

Exercise.

Prevent dehydrations.

Limit your salt intake.

Nitroglycerin (Nitrates)Prevention vs. Treatment

Nitrate (Nitroglycerin): How Does It Work?Vasodilator that works by relaxing the blood

vessels, decreasing the need for the heart to work as hard and lessen its need of oxygen.

Nitroglycerin: Treat or Prevent?Why do we have all these different

dosage forms?

Short-acting: treating attacks of angina and can prevent angina if taken few minutes before engaging in activities that can trigger angina (sublingual tablet or sprays)

Long-acting: Prevention of angina attacks, not for emergency relieve. (Transdermal patches, ointment, and extended releases capsules.

Nitrate (Nitroglycerin): How To Take?Pumpspray?

Nitrate (Nitroglycerin): How To Take?Patch?

Nitrate (Nitroglycerin): How To Take?.

Ointment?

Every 6 to 8 hours if necessary, and wiped off at bedtime to provide a nitrate-free interval; may require as much as 10 to 12.5 cm and/or application every 4 hours.

Apply to nonhairy skin area may be used; some patients prefer the chest.

Sublingual Tablets?

Sudden Attack?

Preventative Use?

.

Nitrate (Nitroglycerin): Side Effects& Interactions

Side Effects:Headache is most common.Others: flushing, dizziness, weakness, palpitations Nausea,

vomiting, diarrhea

Side effects are usually mild and transient

Interactions:AlcoholPhosphodiesterase 5 inhibitors: sildenafil (Viagra)Herbals: long list (ginger, ginseng, licorice)….check with

pharmacist if unsure

Nitrate (Nitroglycerin): TipsAvoid taking alcohol

Store in tight sealing container

Protect from light

Use your dosage form correctlyCan I crush/ chew my SL Tablets?

Last T or FNitroglycerin (short-acting) can be taken

multiply times throughout the day without serious side effects.

True

THE ENDThank you for listening!

Any questions?

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