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Cardiac Medications
 Overview
• Inotropes • Diuretics
• Chronotropes • Anticoagulants
• Antianginal Agents • Fibrinolytic
• Antidysrhythmics Enzymes
• Sympathomimetics • Beta Blockers
• Vasopressors • Ca Channel
blockers
Inotropes
 Inotropes
• Agents that affect myocardial contraction
• Positive Inotropes
– Cardiac glycosides
– Bypyridine derivatives (Milrinone)
– PDE-I (Theophylline)
– Catecholamines
• Negative Inotropes
– BB
– CCB
– Class IA & IC anti-arrhythmics
Class Participation Question #1
Which of the following is an
example of a positive inotrope?
a) Docusate
b) Digoxin
c) HCTZ
d) Propranolol
e) Nitroglycerin
Class Participation Question #1
Which of the following is an
example of a positive inotrope?
a) Docusate
b) Digoxin
c) HCTZ
d) Propranolol
e) Nitroglycerin
 Cardiac Glycosides
• Prototype: Digoxin (Lanoxin®, Digitek®,
Lanoxicaps®)
Digoxin MOA
 Digoxin (cont’d)
• Indications/dosage:
– Afib & HF
• LD: 10-15 mcg/kg IV or PO, given in 3 divided doses every 6-
8 hrs, with the first dose equalling approximately 1/2 the total
• MD: 125-350 mcg PO or IV per day, depending on CrCl,
given in 1-2 divided doses
• CrCL < 60 requires renal adjustment
• Monitoring
– ECG
– serum Ca
– Scr/BUN
– serum Mg
– serum K
 Class Participation Question 2:
AJ is a 54 year old male weighing 50kg who
has class III heart failure. AJ’s doctor will
be starting him on Digoxin therapy.
Calculate the Digoxin LOADING dose.
 Class Participation Question 2:
AJ is a 54 year old male weighing 50kg who has
class III heart failure. AJ’s doctor will be starting
him on Digoxin therapy. Calculate the Digoxin
LOADING dose.

• Recall
– LD: 10-15 mcg/kg IV or PO, given in 3 divided doses
every 6-8 hrs, with the first dose equalling
approximately 1/2 the total
 Class Participation Question 2:
• TOTAL dose
100 kg x 10 mcg = 1000 mcg total
kg

• 1st dose is ½ the total dose

1000 mcg / 2 = 500 mg

• 2nd & 3rd dose

500 mg / 2 = 250 mg
 Class Participation Question 2:
• Answer:
– 500 mcg IV or PO initially
– followed by 250 mcg IV or PO every 6 hours x
2 doses
 Latest News on Digoxin

On April 28, 2008, Actavis Totowa LLC notified

healthcare professionals of a Class I nationwide
recall of all strengths of Digitek™.
The products are distributed by Mylan
Pharmaceuticals Inc. under a Bertek label and
by UDL Laboratories, Inc. under a UDL label.
 Digitalis Toxicity
• Visual changes (unusual)
• Confusion
• Loss of appetite
• Nausea, vomiting, diarrhea
• Palpitations
• Irregular pulse
• Additional symptoms that may be associated
with digitalis toxicity include:
• Decreased urine output
• Excessive nighttime urination
• Overall swelling
• Decreased consciousness
• Difficulty breathing when lying down
Chronotropes
 Chronotropes
• Agents that change heart rate
– affects the nerves controlling the heart
– changes the rhythm produced by the SA node
 Chronotropes (cont’d)
• Positive Chronotropes • Negative Chronotropes
– Atropine – Beta-blockers
– Quinidine – Acetylcholine
– Dopamine – Digoxin
– Dobutamine – Diltiazem
– Epinephrine – Verapamil
– Isuprel – Ivabradine
– Metoprolol
 Positive Chronotrope
Prototype: Atropine
• belladonna alkaloid
• d,l-hyoscyamine
• Anticholinergic
• Uses
– Symptomatic bradycardia
– Aspiration prophylaxis
– Produces mydriasis
– IBS
– Parkinson’s?
– Organophosphate toxicity
– Adjunct nerve agent &
insecticide poisoning
 Atropine (cont’d)
• MOA
– competitive inhibitor at autonomic postganglionic
cholinergic receptors
• Clinical effects
– “anti-SLUD”
– ↓ in salivary bronchial, & sweat gland secretions;
mydriasis; cycloplegia; changes in heart rate;
contraction of the bladder detrusor muscle and of
the GI smooth muscle; ↓ gastric secretion; and ↓ GI
motility
 Atropine Dosing
• Bradycardia
– 0.5-1 mg IV push; repeat if needed every 5 min up to 2 mg
• Aspiration prophylaxis
– po: 2 mg PO 30-60 min prior to anesthesia
– parental: ≥ 20 kg: 0.2-1 mg (the usual dose is 0.4 mg) IV, IM or
SC 30-60 min prior to anesthesia
• IBS
– po: 0.3-1.2 mg PO every 4-6 hours
• Organophosphate insecticide toxicity
– 1-2 mg IM or IV initially; repeat if needed every 20-30 min as
needed until symptoms dissipate. Adjunct nerve agent &
insecticide poisoning
• Mydriasis
– Opthalmic: drop of 1% solution instilled in eye 1 hour prior to
procedure or, 0.3-0.5 cm of 1% ointment placed in conjunctival
sac up to tid
• Note: Lab monitoring not necessary
Anti-anginal Drugs
 Antianginal Drugs
• Prototype: Nitrites &
Nitrates
• BB
• Calcium Channel
Blockers (CCBs)
Symptoms of Angina
 Nitrites/Nitrates
• Previously known as “coronary dilators”
• Main effect: to produce general
vasodilation of systemic vein & arteries
– ↓preload & ↓afterload
– ↓ cardiac work & oxygen consumption
• 2 main uses
– Angina attacks
– Angina prophylaxis
Class Participation Question #3:
Which is the PREFERRED route for
nitroglycerin during angina attacks?
a) Topical (ointment 2%)
b) IV infusion
c) Transdermal
d) SL
e) Extended release tablets/capsules
Class Participation Question #3:
Which is the PREFFERED route for
nitroglycerin during angina attacks?
a) Topical (ointment 2%)
b) IV infusion
c) Transdermal
d) SL
e) Extended release tablets/capsules
Drug Common Onset Duration
(Trade Name) Dosage

Amyl nitrate 0.3 ml 30-60 sec 10 min

inhalation
(Vaporole®)

ISDN 2.5 - 10 mg SL 2-5 min 2 - 4 hr

(Isordil®) 5 - 30 mg po qid

Nitroglycerin

(Nitro-bid®) 2% ointment 15 min 4 - 8 hr

(Nitrostat®) 0.3 - 0.6 mg SL 1-3 min 10 - 45 min

(Nitrogard®) 1,2,3 mg XR tab 30 min 8 - 12 hr

(Transderm- 2.5 - 15 mg/day 30-60 min 24 hr

Nitro®) Transdermal
patch
 Nitroglycerin (NG)
• Indications
– Angina
– Acute MI
– HF
– HTN
– Hypertensive emergency
– Hypotension induction
– Peri/postoperative HTN
– Pulmonary edema
– Pulmonary HTN
 NG (cont’d)
• Dosing
– 1 tablet (0.3 mg, 0.4 mg, or
0.6 mg strength) SL,
dissolved under the tongue
or in buccal pouch
immediately following
indication of anginal attack
– During drug administration,
the patient should rest,
preferably in the sitting
position
– Symptoms typically improve
within 5 minutes. If needed
for immediate relief of stable
angina symptoms, SL
nitroglycerin may be
repeated every 5 minutes as
needed, up to 3 doses
 NG (cont’d)
• Adverse Effects • Contraindication:
– dizziness or fainting – sildenafil (Viagra®)
– flushing of the face or – tadalafil (Cialis®)
neck – vardenafil (Levitra®)
– headache, this is
common after a dose,
but usually only lasts
• Lab monitoring not
for a short time necessary
– irregular heartbeat,
palpitations
– nausea, vomiting
Antidysrhythmics/Antiarrhythmics
 What are Arrhythmias?
• Cardiac disorder of
– Rate
– Rhythm
– Impulse generation
– Conduction of electrical
impulses in the heart
• Causes
– May develop from a
diseased heart
– Consequence of chronic
drug therapy
• Symptoms
– Mild palpitations 
cardiac arrest
• Treatment goal
– Covert arrhythmia to a
normal rhythm
 Antidysrhythmics/Antiarrhythmics

• Uses
– restore normal cardiac
rhythm
– Successful conversion
of an arrhythmia
depends on the type of
arrhythmia present
 Antidysrhythmics/Antiarrhythmics
• 4 major classes
– Class I
• Class IA
• Class IB
• Class IC
– Class II
– Class III
– Class IV
Cardiac Action Potential
4: resting membrane
potential; steady K+
flux
0: Na+ influx into cell
1: K+ efflux
2: K+ efflux & Ca+
influx
3: K+ efflux
Class Participation Question #4:
True or False?

Although antiarrthymics are used for treating

arrhythmias, they can also PRODUCE
arrhythmias.
Class Participation Question #4:
True or False?

Although antiarrthymics are used for treating

arrhythmias, they can also PRODUCE
arrhythmias.

Answer: TRUE
 The Catch 22 with Antiarrhythmics

• People with structural heart disease are at

INCREASED risk for arrhythmias!
• The problem…
– Many antiarrhythmic drugs INCREASE sudden
death in these patients compared to placebo
 Antiarrthymics: Class I
• Na channel blockers
• Common features
– Local anesthetic activity
– Interferes with movement of Na ions
– Slow conduction velocity
– Prolong refractory period
– Decreases automaticity of the heart
 Class IA
• Quinidine (Quinidine sulfate®,
Quinaglute®, Quinidex®, Cardioquin®)
• Disopyramide (Norpace®)
• Procainimide (Procainimide HCI®,
Procan®, Procanabid®, Pronestyl®)
 Class 1A – Quinidine
• Derived from cinchona tree
• Depresses both the myocardium & conduction
system
• Overall effect: slows heart rate
• Pharmacokinetics
– Well absorbed in GI tract after po administration
– Metabolized to several active metabolites
– Primarily excreted by urinary tract
– Cardiac poison when large amounts are present in
blood
 Class 1A – Quinidine (cont’d)
• Adverse Effects
– N/V, diarrhea, weakness, fatigue, cinchonism
• Drug Interactions
– Hyperkalemia
– Digitalis
– propranolol
• Monitoring
– CBC
– ECG
– serum quinidine concentrations (target range
2-6 µg/ml or higher)
• CI: AV block
 Class IB
• prototype: Lidocaine (Xylocaine®)
• Tocainide (Tonocard®)
• Mexiletene (Mexitel®)
• Phenytoin (Dilantin®)
 Lidocaine – Class IB

• MOA: blocks influx of Na fast channels

• What phase of the action potential does this affect?
• Indication: ventricular arrhythmias
 Dosage
• Vfib, Vtach
– IM 300 mg. May be repeated after 60 to 90 min
– IV bolus 50 to 100 mg at rate of 25 to
50 mg/min; may repeat, but do not exceed 200
to 300 mg/h
– Continuous infusion 1 to 4 mg/min
• Lidocaine is prepared by mixing:
– 2 Grams Lidocaine in 500 mL D5W
– 1 Gram Lidocaine in 250 mL D5W
 Lidocaine – Class IB (cont’d)
• Common Adverse Effects
– anxiety, nervousness
– dizziness, drowsiness
– feelings of coldness, heat, or numbness; or
pain at the site of the injection
– N/V
• Monitoring
– LFTs
– Scr/BUN
– serum lidocaine concentrations (target range
2-6 µg/ml): parenteral use
 Lidocaine (cont’d)
• CI
– Hypersensitivity to amide local anesthetics

– Stokes-Adams syndrome
– Wolff-Parkinson-White syndrome
– severe degrees of sinoatrial, AV or intraventricular
block in absence of pacemaker
– ophthalmic use
 Class IC
• prototype: Flecainide (Tambocor®)
• Propafenone (Rhythmol®)
 Flecainide – Class IC

• MOA
– Blocks fast Na channels depresses the upstroke of the
action potential, which is manifested as a decrease in the
maximal rate of phase 0 depolarization.
– significantly slow His-Purkinje conduction and cause QRS
widening
– shorten the action potential of Purkinje fibers without
affecting the surrounding myocardial tissue.

• Indications
– Afib
– Atrial flutter
– Paroxysmal supraventricular tachycardias
– Ventricular tachycardia prophylaxis
– Wolff-Parkinson-White Syndrome
 Flecainide – Class IC
• Adverse Reactions
– visual impairment, dizziness, asthenia, edema, abdominal
pain, constipation, headache, fatigue, and tremor, N/V,
arrhea, dyspepsia, anorexia, rash, diplopia, hypoesthesia,
paresthesia, paresis, ataxia, flushing, increased sweating,
vertigo, syncope, somnolence, tinnitus, anxiety, insomnia,
and depression.
• Avoid in
– CHF
– Acute MI
– Hx of MI (LVEF < 30%)
• Monitoring
– ECG
– serum creatinine/BUN: baseline
 Class II – Beta Blockers
• Propranolol (Inderal®)
• Acebutolol (Sectral®)
• Atenolol (Tenormin®)
• Betaxolol (Kerlone®)
• Bisoprolol (Zebeta®)
• Carvedilol (Coreg®)
• Esmolol (Brevibloc®)
• Metoprolol(Toprol®, Lopressor®)
• Nadolol (Corgard®)
• Timolol (Blocadron®)
 Propranolol Warning
• 2 situations in which propranolol requires
extreme caution
– AV block
– CHF
– Asthma or emphysema
 Class III
• K+ channel blockers
• Drugs:
– Prototype: Amiodarone (Cordarone)
– Bretylium (Bretylol)
– Sotalol (Betapace)
 Amiodarone – Class III
MOA
– noncompetitively inhibits alpha- and beta-receptors,
– possesses both vagolytic and calcium-channel
blocking properties
– relaxes both smooth and cardiac muscle

• Indications
– Vfib
– Vtach
 Vfib Amiodarone Dosage
• po
– Initially, 800-1600 mg/day PO in single or divided doses
for a minimum of 1-3 weeks in a monitored setting until
an initial therapeutic response is achieved
– followed by 600-800 mg/day PO in one or divided doses
for about one month.
– Then reduce dosage again to the lowest effective
maintenance dose, usually 400 mg/day PO in one or
divided doses
• iv
– initial IV rapid infusion of 150 mg over the first 10
minutes. Then begin a slow IV infusion of 1 mg/min for
the next 6 hours (total dose infused = 360 mg). Then,
the infusion rate is lowered to 0.5 mg/min for the next 18
hours (total dose infused = 540 mg). After the first 24
hours, a maintenance IV infusion of 0.5 mg/minute (720
mg/day) is recommended.
 Amiodarone – Adverse Reactions
• Cardiovascular: exacerbation of the arrhythmias, CHF (3%) and bradycardia.
Cardiac arrhythmias, CHF, sinoatrial node dysfunction (1% to 3%); cardiac conduction
abnormalities, hypotension (less than 1%)
• CNS: 20% to 40% of patients and including malaise and fatigue, peripheral neuropathy, poor
coordination & gait, & tremor and involuntary movements; they are rarely a reason to stop
therapy and may respond to dose reductions or discontinuation; Abnormal gait/ataxia,
dizziness, lack of coordination, malaise and fatigue, paresthesias, tremor/abnormal involuntary
movements (4% to 9%); decreased libido, headache, insomnia, sleep disturbances (1% to 3%).
• Dermatologic: ~15% of patients, with photosensitivity being most common (approximately
10%). Sunscreen and protection from sun exposure may be helpful, and drug discontinuation is
not usually necessary. Prolonged exposure to amiodarone occasionally results in a blue-gray
pigmentation; Solar dermatitis/photosensitivity (4% to 9%); alopecia, blue skin discoloration,
rash, spontaneous ecchymosis (less than 1%).
• Endocrine: Hyperthyroidism, hypothyroidism (1% to 3%).
• GI: GI complaints, most commonly anorexia, constipation, N/V (10% to 33%); anorexia,
constipation (4% to 9%); abdominal pain (1% to 3%)
• Hepatic: Abnormal liver function tests (4% to 9%); nonspecific hepatic disorders (1% to 3%)
• Ophthalmic: optic neuropathy and/or optic neuritis, in some cases progressing to corneal
degeneration, eye discomfort, lens opacities, macular degeneration, papilledema, permanent
blindness, photosensitivity, and scotoma, have been reported . Asymptomatic corneal
microdeposits are present in virtually all adult patients who have been on the drug for more than
6 months. Some patients develop eye symptoms of dry eyes, halos, and photophobia. Vision is
rarely affected and drug discontinuation is rarely needed. Visual disturbances (4% to 9%)
• Respiratory: Fibrosis, pulmonary inflammation (4% to 9%)
• Miscellaneous: Abnormal salivation, abnormal taste and smell, coagulation abnormalities,
edema, flushing (1% to 3%).
 Amiodarone – Class III (cont’d)
• Monitoring
– CBC
– chest x-ray
– ECG
– LFTs
– ophthalmologic exam
– PFTs: baseline
– thyroid function tests (TFTs)
 Class IV

• Ca channel blockers
• Drugs
– Adenosine (Adenocard ®)
– Diltiazim (Cardizem®, Tiazac®)
– Verapamil (Dovera®, Isoptin®, Calan®)
• Clinical Effects
– widen the blood vessels
– may decrease the heart’s pumping strength
Sympathomimetics
 Sympathomimetics
• 2 classes: • SE:
– α- agonist
– hypertension,
• Phenylephrine
– excessive cardiac
• Clonidine stimulation
• Oxymetazoline – cardiac arrhythmias
• Tetrahydralazine
– Long-term use increases
• Xylometazoline mortality in heart failure
patients.
– β-agonist • CI
• Prototype: Epinephrine
– CAD  
• Norepinephrine
• Dopamine
• Dobutamine
• Isoproterenol
Epinephrine
• “fight or flight “hormone
• Aka “adrenaline”
• increases heart rate
and stroke volume
• dilates the pupils
• constricts arterioles in
the skin and
gastrointestinal tract
while dilating arterioles
in skeletal muscles
Epinephrine MOA
 Epinephrine (cont’d)
• Indications • IV Dosage
– Vfib – IV: 1 mg (10 ml of a
– Ventricular asystole 1:10,000 solution) IV;
– Cardiac arrest may repeat every 3-5
minutes
– Pulseless electrical
– Each dose may be
activity
given by peripheral
injection followed by a
20 ml flush of IV fluid.
 Epinephrine
• Common Adverse Effects
– anxiety or nervousness
– dry mouth
– drowsiness or dizziness
– headache
– increased sweating
– nausea
– weakness or tiredness

• Monitoring
– ECG: in patients receiving IV therapy
– PFTs
Vasopressors
 Vasopressors
• Vasoconstrictors vs. Vasodilators
• 2 Vasoconstrictor Classes
– Sympathomimetics
– Vasopressin Analogs
• Vasodilators
• Alpha-adrenoceptor antagonists (alpha-blockers)
• Angiotensin converting enzyme (ACE) inhibitors
• Angiotensin receptor blockers (ARBs)
• Beta2-adrenoceptor agonists (b2-agonists)
• Calcium-channel blockers (CCBs)
• Centrally acting sympatholytics
• Direct acting vasodilators
• Endothelin receptor antagonists
• Ganglionic blockers
• Nitrodilators
• Phosphodiesterase inhibitors
• Potassium-channel openers
• Renin inhibitors
 Vasoconstrictor
• any agent that produces vasoconstriction
and a rise in blood pressure (usually
understood as increased arterial pressure)
• Drugs
– Prototype: Vasopressin
– Epinephrine
– Dobutamine
– Dopamine
– Norepinephrine
 Vasopressin
• aka : “AVP” or “ADH”
• MOA
– ↑ the resorption of
water at the renal
collecting ducts
– Vasoconstrictive
property: stimulates
the contraction of
vascular smooth
muscle in coronary,
splanchnic, GI,
pancreatic, skin, and
muscular vascular
beds
 Vasopressin (cont’d)
• FDA indication: Diabetes Insipidus
• Non-FDA indications
– Cardiac arrest
– Cardiogenic shock
– Cardiopulmonary resuscitation
– Hypotension
– Septic shock
– And many more….
 Vasopressin (cont’d)

• Dosage for cardiac arrest including

ventricular asystole and pulseless electrical
activity (PEA) during cardiopulmonary
resuscitation (CPR)
– IV or intraosseous dosage:
• Adults: A single dose of 40 units IV (or intraosseous)
may be given one time to replace the first or second
dose of epinephrine during cardiac arrest
• Do not interrupt cardiopulmonary resuscitation to
administer drug therapy.
 Vasopressin (cont’d)
• Adverse Effects
– Cardiovascular: Cardiac arrest; circumoral pallor;
arrhythmias; decreased cardiac output; angina;
myocardial ischemia; peripheral vasoconstriction; and
gangrene
– CNS: Tremor; vertigo; “pounding” in head
– Dermatologic: Sweating; urticaria; cutaneous gangrene
– GI: Abdominal cramps; nausea; vomiting; passage of gas
– Hypersensitivity: Anaphylaxis (cardiac arrest and/or
shock) has been observed shortly after injection
– Respiratory: Bronchial constriction.

• Monitoring
– serum osmolality
– serum Na
Diuretics
 Diuretics
• “water pill”
• Promotes formation
of urine by the
kidney  forced
diuresis
• Uses
– HTN
– Edema
– Glaucoma
– Anuria
 Diuretic Properties
Diuretic agent Site of Action & Misc.
Chlorothiazide PO/IV Distal Tubule
Hydrochlorothiazide Calcium Reabsorption Increased
Indapamide May transiently increase Lipids, BG and UA
Metolazone (Mykrox) Hypomagnesemia (may complicate K+ correction)
Severe Potassium Depletion – Creation of Combos ???
Pregnancy categories: B and C
Furosemide Ascending Limb of Henle
Torsemide Ototoxocity (reversible and irreversible)
Bumetanide Hypokalemia (supplement with K+)
Ethacrynic acid Pregnancy categories: B

Amiloride Distal and Proximal tubule Impact

Triamterene Hyperkalemia and serum creatinine elevations
Avoidance: BUN > 30 mg/dl or SCr > 1.5 mg/dl
Eplerenone Distal and Aldosterone receptor Impact
Spironolactone Same as amiloride and triamterene – avoid K spare combos
 Diuretics
• Prototype: Furosemide (Lasix®)
• MOA
– inhibits the reabsorption of sodium and chloride in the
ascending limb of the loop of Henle
• Indications
– Edema
– HF
– HTN
– Nephrotic syndrome
– Pulmonary edema
– Renal impairment
 Furosemide – Edema Dosage
• po: Initially, 20-80 mg as a
single dose; may repeat
dose in 6-8 hr. Titrate
upward in 20-40 mg
increments. The usual
dosage is 40-120 mg/day.
Max dosage is 600 mg/day.
• IV or IM: Initially, 20-40 mg,
increasing by 20 mg every 2
hours prn to attain clinical
response. Administer IV
doses slowly. A max
infusion rate of 4 mg/min
has been recommended
when administering doses
>120 mg or for patients with
cardiac or renal failure
 Furosemide
• Common Adverse Reactions
Cardiovascular: Orthostatic hypotension may occur and be aggravated by
alcohol, barbiturates or narcotics.

CNS: Tinnitus and hearing loss, paresthesias, vertigo, dizziness, headache,

blurred vision, xanthopsia.
Dermatologic: Exfoliative dermatitis, erythema multiforme, purpura,
photosensitivity, urticaria, rash, pruritus.
GI: Pancreatitis, jaundice (intrahepatic cholestatic jaundice), anorexia, oral
and gastric irritation, cramping, diarrhea, constipation, nausea, vomiting.
Hematologic: Aplastic anemia (rare), thrombocytopenia, agranulocytosis
(rare), hemolytic anemia, leukopenia, anemia.
Hypersensitivity: Systemic vasculitis, interstitial nephritis, necrotizing
angiitis.
Miscellaneous: Hyperglycemia, glycosuria, hyperuricemia, muscle spasm,
weakness, restlessness, urinary bladder spasm, thrombophlebitis, fever.
 Furosemide (cont’d)
• Monitoring
– audiometry
– blood glucose
– serum creatinine/BUN
– serum electrolytes
– serum uric acid

• CI/Precautions
– Sulfa allergy
– Kidney failure
– Anuria
Anticoagulants
 Antiplatelets/Anticoagulants

• Prevents/interferes with coagulation

• Uses
– deep vein thrombosis (DVTs), pulmonary
embolism, myocardial infarctions & strokes in
those who are predisposed
 Types of
Antiplatelets/Anticoagulants
• Antiplatelets
– Aspirin
– Dipyridamole
– Thienopyridines
• Clopidogrel (Plavix)
• Ticlopidine (Ticlid)
– Glycoprotein IIb/IIIa antagonists
• Abciximab (ReoPro)
• Eptifibatide (Integrelin)
• Tirofiban (Aggrastat)
 Antiplatelets/Anticoagulants
• Anticoagulants
– Heparin
– LMWH
• Enoxaparin (Lovenox®)
• Dalteparin (Fragmin®)
• Tinzaarin (Innohep®)
– Factor Xa inhibitors
• Fondaparinux (Arixtra®)
– Direct Thrombin Inhibitors
• Argatroban
• Lepirudin (Refludan®)
– Oral Anticoagulants
• Prototype: Warfarin
 Heparin Recall in 2008
• In February 2008, the FDA issued a MedWatch in response to an
increase in the number of serious adverse events including allergic or
hypersensitivity-type reactions with the administration of higher bolus
doses of heparin. The reports have mainly involved the use of Baxter
multiple-dose vials; however, there have been reports of these reactions
occurring when the combination of multiple- and single-dose vials have
been used to administer a bolus dose. In February 2008, Baxter
International announced expanding their voluntary recall to include all
lots and doses of its Heparin Sodium UPS multi-dose, single-dose
vials, and HEP-LOCK heparin flush products. The company initially
recalled nine lots of heparin sodium injection multi-dose vials as a
precautionary measure due to a higher than usual number of reports of
adverse patient reactions involving the product. In March 2008, the FDA
announced that the contaminant found in samples of Baxter's heparin was
oversulfated chondroitin sulfate, a substance derived from animal cartilage.
The FDA also stated that it does not know whether this contaminant
caused the adverse events, only that a contaminant has been
identified. Investigations continue as to whether this contaminant was
added to heparin by accident or intentionally. Customers with questions
regarding the Baxter recall may contact the Center for One Baxter at 1-800-
422-9837.
Coagulation Cascade
 Warfarin – Oral Anticoagulant

• MOA: Warfarin inhibits the synthesis of vitamin K-dependent

coagulation factors II, VII, IX, and X and anticoagulant
proteins C and S
Warfarin (cont’d)
• Indications
– Stroke
– DVT
– Post MI
– Afib
– Cardiomyopathy….and many more!

• Dosage
– Initially, 2-5 mg PO or IV once daily, with dosage
adjustments made according to INR result
 Warfarin Warnings

Bleeding Risk!
• Warfarin can cause major or fatal bleeding. Bleeding is more
likely to occur during the starting period and with a higher dose
(resulting in a higher international normalized ratio [INR]). Risk
factors for bleeding include high intensity of anticoagulation (INR of
more than 4), 65 years of age and older, highly variable INRs,
history of GI bleeding, hypertension, cerebrovascular disease,
serious heart disease, anemia, malignancy, trauma, renal function
impairment, concomitant drugs, and long duration of warfarin
therapy. Regular monitoring of INR should be performed on all
treated patients. Those at high risk of bleeding may benefit from
more frequent INR monitoring, careful dose adjustment to desired
INR, and a shorter duration of therapy. Patients should be
instructed about prevention measures to minimize risk of
bleeding and to report immediately to health care provider
signs and symptoms of bleeding
• Pregnancy Category X
 Warfarin (cont’d)
• SE
– Hemorrhage: Signs of severe bleeding resulting in the loss of large
amounts of blood depend upon the location and extent of bleeding.
Symptoms include: chest, abdomen, joint, muscle, or other pain;
difficult breathing or swallowing; dizziness; headache; low blood
pressure; numbness and tingling; paralysis; shortness of breath;
unexplained shock; unexplained swelling; weakness

• Monitoring
– INR
– prothrombin time (PT)
– stool guaiac
– bleeding
– DDIs
• NSAIDs
• 3 G’s
– Garlic
– Ginger
– Ginsing
– Vitamin K intake
Class Participation Question #5:

Which foods are high in vitamin K?

Class Participation Question #5:

Which foods are high in vitamin K?

Fibrinolytic Enzymes
 Fibrinolytic Enzymes
• “clotbusters”
• MOA: stimulate the synthesis of
fibrinolysin which breaks the clot into
soluble products
• Drugs
– Urokinase (Abbokinase®)
– Anistreplase (Eminase®)
– Alteplase (Activase®)
– Reteplase (Retevase®)
– Prototype: Streptokinase (Strepase®)
 Streptokinase (cont’d)
• Indications
– Acute MI
– Acute ischemic stroke
– Pulmonary embolism
– Lysis of DVT
• Dose Administration
– Parental infusion (usually IV)
– Deep vein or arterial thrombosis
• IV: 250,000 IU over 30 min followed by 100,000 IU
per hour up to 72 hours
 Streptokinase (cont’d)
• Adverse Effects
– Hemorrhage
– Concomitant use of heparin, oral
anticoagulants, NSAIDs is NOT
recommended because of the increased risk
of bleeding
– Allergic reactions
Streptokinase (cont’d)
Beta Blockers
 Beta Blockers
• MOA: bind to beta-adrenergic receptors &
block the effects of EPI & NE
• Indications
– Angina
– HTN
– Arrhythmias
– Glaucoma
– Migraine prophylaxis
– Post MI
 Beta Blockers (cont’d)

• Non-Selective BB • Selective B-1 Blockers

– carvedilol (Coreg®) – acebutolol (Sectral®)
– labetalol – altenolol (Tenormin®)
(Normodyne®) – bisoprolol (Zebeta®)
– nadolol (Corgard®) – esmolol (Brevibloc®)
– pindolol (Visken®) – metoprolol tartrate
– propranolol (Lopressor®)
(Inderal®) – metoprolol succinate
– timolol (Blocadren®) (Toprol XL)
 Propranolol
• HTN Dosage
– po: initially, 40 mg PO twice daily, then increase at
3-7 day intervals up to 160-480 mg/day, given in 2-
3 divided doses. Maximum dosage is 640 mg/day
• Main Effects
– ↓ in rate, force of contraction, & conduction velocity
of the heart
– Blocks carbohydrate & lipid metabolism
 Propranolol (cont’d)
• Adverse Reactions
– changes in blood sugar
– cold hands or feet
– difficulty breathing, wheezing
– difficulty sleeping, nightmares
– dizziness or fainting spells
– hallucinations (seeing and hearing things that are not really there)
– muscle cramps or weakness
– skin rash, itching, dry peeling skin
– slow heart rate (less than 50 beats per minute)
– swelling of the legs and ankles
– vomiting
– dark coloration of skin
– diarrhea
– dry sore eyes
– hair loss
– nausea
– sexual difficulties (impotence or decreased sexual urges)
– weakness or tiredness
 Propranolol (cont’d)
• Lab monitoring NOT
necessary
• Check vital signs
frequently with
parenteral drug
administration
• Observe patient for
signs of cardiac
depression &
hypotension
Calcium Channel Blockers
 Calcium Channel Blockers (CCBs)
• MOA
– prevent calcium from entering cells of the heart and blood
vessel walls
– relax and widen blood vessels by affecting the muscle
cells in the arterial walls

• Indications:
– HTN
– Angina
– Migraine prophylaxis
– Brain aneurysm complications
– Arrhythmia
– Reynaud's disease
– Pulmonary HTN
 CCBs (cont’d)
Drugs:
• Amlodipine (Norvasc®)
• Diltiazem (Cardizem LA®, Dilacor XR®,
Tiazac®)
• Felodipine (Plendil®)
• Isradipine (DynaCirc CR®)
• Nicardipine (Cardene®, Cardene SR®)
• Nifedipine (Procardia®, Procardia XL®, Adalat
CC®)
• Nisoldipine (Sular®)
• Verapamil (Calan®, Verelan®, Covera-HS®)
 Amlodipine
• Indications
– hypertension, chronic stable angina pectoris,
and Prinzmetal's variant angina

• Dosage
– Initially, 5 mg PO qd
– Maximum dosage is 10 mg qd
 Amlodipine
http://online.factsandcomparisons.com/MonoDisp.aspx?
monoID=fandc-
hcp10122&inProdGen=true&quick=Amlodipine&search=Amlodipine
 Amlodipine
• Monitoring
– No lab monitoring needed
• CI
– Known sensitivity to amlodipine
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