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97 Cards in this Set

  • Front
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What is the MOA/ Indication for Class 1a drugs?
(antiarrhythmic medications)
Sodium Channel Blockers

Na+ channel blockers; Slow conduction velocity & repolarization

Indication: Supraventricular & ventricular arrhythmias
What is the MOA/ Indication for Class 1b drugs?
(antiarrhythmic medications)
Sodium Channel Blockers

Weak Na+ channel blockers (not very potent antiarrhythmics)

Indication: Ventricular & supraventricular arrhythmias (more effective w/ventricular arrhythmias)
What is the MOA/ Indication for Class 1c drugs?
(antiarrhythmic medications)
Sodium Channel Blockers

Potent Na+ channel blockers; Eliminate reentry by slowing conduction to the point where impulse is halted

Indication: Supraventricular arrhythmias
What is the MOA/ Indication for Class II drugs?
(antiarrhythmic medications)
Beta Blockers

Affect slow-channel tissue (SA & AV nodes); decreases rate of automaticity, slows conduction velocity (most effective in tachycardic arrhythmias), prolong refractoriness

Indications: Sinus tachycardia, atrial fibrillation, atrial flutter, ventricular fibrillation
What is the MOA/ Indication for Class III drugs?
(antiarrhythmic medications)
Potassium Channel Blockers

K+ channel blockers; Prolong refractoriness in atrial & ventricular tissue
Amiodarone also blocks Na+ channels (fast kinetics), **nonselective beta-blocking actions, ***some Ca+ blocking actions

Indications: Supraventricular & ventricular arrhythmias
What is the MOA/ Indication for Class IV drugs?
(antiarrhythmic medications)
Calcium Channel Blockers (Non DHP)

Block Ca+ channels; Slows conduction, prolongs refractoriness, decreases automaticity

Indications: Supraventricular tachyarrhythmias
Class 1a antiarrhythmics are treated with what type of drug?

Give an example?
Sodium Channel Blockers

Quinidine, procainamide, disopyramide
Class 1b antiarrhythmics are treated with what type of drug?

Give an example?
Sodium Channel Blockers

Lidocaine, mexiletine
Class 1c antiarrhythmics are treated with what type of drug?

Give an example?
Sodium Channel Blockers

Propafenone, flecainide, moricizine
Class II antiarrhythmics are treated with what type of drug?

Give an example?
Beta Blockers

Metoprolol, esmolol, atenolol
Class III antiarrhythmics are treated with what type of drug?

Give an example?
Potassium Channel Blockers

Amiodarone, sotalol, dofetilide, ibutilide
Class III antiarrhythmics are treated with what type of drug?

Give an example?
Calcium Channel Blockers (Non DHP)

Diltiazem, verapamil
What is the MOA/ Indication for low molecular weight heparins (LMWH)?
Binds to AT-III to produce anticoagulant effect

Indications: Prophylaxis of thromboembolism, STEMI, ischemia

Ex: Dalteparin (Fragmin)
Enoxaparin (Lovenox)
Tinzaparin (Innohep)
What is the MOA/ Indication for Factor Xa?
Synthetic pentasaccharide that causes AT-III inhibitor of Factor Xa to prevent thrombin formation

For treatment & prophylaxis of thromboembolism

Ex:Fondaparinux (Arixtra)
What is the MOA/ Indication for Warfarin (Coumadin)?

Oral Anticoagulation
MOA: Stops conversion of vitamin K epoxide to active vitamin K --> Lack of activated clotting factors II, VII, IX, X and Protein C & S

Indications: Treatment (in conjunction w/heparin or LMWH or fondaparinux for 1st several days. It takes a while to be effective.) & prophylaxis of thromboembolism, atrial fibrillation, cardiac valves
Will Amiodarone increase or decrease INR when used with Warfarin?
Increase
Will ETOH (acute use) increase or decrease INR when used with Warfarin?
Increase
Will aspirin increase or decrease INR when used with Warfarin?
Increase
Will NSAIDs (Ibuprofen, naproxen, etc) increase or decrease INR when used with Warfarin?
Increase
Will Celecoxib (Celebrex) increase or decrease INR when used with Warfarin?
Increase
Will antibiotics increase or decrease INR when used with Warfarin?

Bactrim, Flagyl, Cephalosporins, Fluoroquinolones, Erythromycin, Tetracycline, etc
Increase
Will Fluconazole (Diflucan) increase or decrease INR when used with Warfarin?
Increase
What type of drug do you use to treat 2nd and 3rd degree heart blocks?
None!
Potentially Fatal
Where are all Na+ channel blockers metabolized?
Antiarrhythmics Class I
Hepatic (P450)
When treating a patient with:
Sinus tachycardia, Atrial Fibrillation,
Atrial Flutter, or Ventricular Fibrillation

What type of drug would you administer?
Antiarrhythmic Class II Drugs

Beta Blockers
Metoprolol, esmolol, atenolol
Recap!

What do we know about Selective Beta 1 Blockers?
Adrenergic Antagonist (block sympathetic response)
The neurotransmitters blocked include:
Biogenic Amines/ Catecholamines/Epinephrine and Norepinephrine

Selective Beta 1 Blockers include:
Metoprolol (Lopressor, Toprol XL), atenolol (Tenormin), acebutolol (Sectral), esmolol (Brevibloc)

Hypertension Treatment…..vasodilation

Class II/ III Heart Failure…..blocking sympathetic response; A sympathetic response puts a lot of demands on the heart “It expects great output” to deal with fight or flight situations.

1st agent for Ischemic Heart Disease… Reduces myocardial oxygen demand, decrease HR, BP, and contractility

Antiarrhythmic Class II for sinus tachy, AFib, Aflutter, and VFib (Metoprolol, esmolol, atenolol
)…..Affect SA/AV Node and decrease rate of automaticity and conduction velocity
Class I, III, IV antiarrhythmics all treat supraventricular arrhythmias, which also treat ventricular arrhythmias?
Class Ia/Ib and Class III

Note: Class Ib are not very potent antiarrhythmics, but are more effective with ventricular arrhythmias. (Lidocaine, Mexiletine )
What type of drugs are
Antiarrhythmics Class Ia ?
Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Indicated with Supraventricular & ventricular arrhythmias
What type of drugs are
Antiarrhythmics Class Ib ?
Sodium Channel Blockers
Lidocaine, Mexiletine

Indicated with Supraventricular & ventricular arrhythmias (more effective with ventricular arrhythmias)
What type of drugs are
Antiarrhythmics Class Ic ?
Sodium Channel Blockers
Propafenone (Rhythmol), Flecainide, Moricizine

Indicated with Supraventricular arrhythmias
What type of drugs are
Antiarrhythmics Class II ?
Beta 1 Blockers
Metoprolol, Esmolol, Atenolol

Indicated with Sinus tachycardia, atrial fibrillation, atrial flutter, ventricular fibrillation
What type of drugs are
Antiarrhythmics Class III ?
Potassium Channel Blockers
Amiodarone, Sotalol, Dofetilide (Tikosyn), Ibutilide (Corvert)

Indicated with Supraventricular & ventricular arrhythmias
What type of drugs are
Antiarrhythmics Class IV ?
Calcium Channel Blockers
Diltiazem, Verapamil

Indicated with Supraventricular arrhythmias
Antiarrhythmics Class I: Na+ Blocker

MOA
Class Ia- Na+ channel blockers; Slow conduction velocity & repolarization

Class Ib- Weak Na+ channel blockers (not very potent antiarrhythmics)

Class Ic- Potent Na+ channel blockers; Eliminate reentry by slowing conduction to the point where impulse is halted
Antiarrhythmics Class I: Na+ Blocker

Pharmacokinetics
Class Ia- Intermediate kinetics

Class Ib- Fast (Express effects only at fast heart rates)

Class Ic- Slow (Express effects at all heart rates)
Antiarrhythmics: Class Ia
Quinidine
ADE’s: N/V/D, cinchonism (tinnitus, CNS effects), HF exacerbation, hypotension, TdP
Drug Intxns: Warfarin (increase INR), digoxin, amiodarone

Procainamide
ADE’s: *Lupus-like syndrome (SLE), hypotension, HF exacerbation, TdP
Drug Intxns: Fluoroquinolones, amiodarone, Bactrim, TCA’s
Avoid in renal & hepatic dysfnxn****

Disopyramide (Norpace)
ADE’s: Anticholinergic (tachycardia, constipation, dry eyes, urinary retention), HF exacerbation, TdP
Drug Intxns: CytP450 3A4 inhibitors, fluoroquinolones
Notes: Caution in glaucoma*** like all anticholinergics
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

All Class Ia drugs have a possible adverse effect of heart failure exacerbation and/ or cause torsades, but which drug can possibly cause cinchonism?
Quinidine

Cinchonism is caused by an overdose of quinine and can cause tinnitus and CNS effects like blurred vision, impaired hearing, confusion, etc.

Note: quinine can also be found in tonic drinks as the bittering agent
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

All Class Ia drugs have a possible adverse effect of heart failure exacerbation and/ or cause torsades, but which drug can possibly cause a Lupus like syndrome (SLE?
Procainamide
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

All Class Ia drugs have a possible adverse effect of heart failure exacerbation and/ or cause torsades, but which drug can possibly cause anticholinergic effects?
Disopyramide (Norpace)

remember anticholinergic effects include tachycardia, constipation, dry eyes, and urinary retention.

All anticholinergics should be avoided in patients with glaucoma
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Which drug interacts with Warfarin; increasing INR?
Quinidine
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Which drug interacts with the efficacy of Fluoroquinolones?
Procainamide and Disopyramide (Norpace)
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Which drug interacts with Amiodarone (K+ channel blocker)?
Quinidine and Procainamide

Note: procainamide also interacts with Bactrim
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Which drug interacts with tricyclic antidepressants (TCAs)?
Procainamide
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Which drug should be avoided with patients who have renal or hepatic dysfunction?
Procainamide
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Which drug interacts with Digoxin a glycoside used to treat AFib, Aflutter, and heart failure?
Quinidine
Antiarrhythmics: Class Ia

Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace)

Which drug interacts with CytP450 3A4 inhibitors (ex: erythromycin, azole antifungals, CCB nondhp)
Disopyramide (Norpace)
Antiarrhythmics Class Ib
Lidocaine, Mexiletine

Which is contraindicated in 3rd degree heart blocks?
Both
Antiarrhythmics: Class 1b
Indicated in Ventricular, Supraventricular arrhythmias

Lidocaine & Mexiletine

Both meds can cause CNS effects; which is responsible for peri-oral numbness, seizures, confusion, blurry vision, tinnitus, muscle twitching, sedation, slurred speech, and even psychosis.

This drug will slow the heart rate down, but can make you CRAZY!
Lidocaine

note: Mexiletine can cause N/V, GI upset, dizziness, confusion, anxiety, tremor
Antiarrhythmics: Class 1b
Indicated in Ventricular, Supraventricular arrhythmias

Lidocaine & Mexiletine

Both interact with phenytoin and fluoroquinolones, but which also interacts with theophylline a drug used to treat respiratory distress (COPD/ Asthma)?
Mexiletine

Note: Lidocaine also interacts with amiodarone (K+ channel blocker/Class II) and beta blockers (Class III)

Remember Phenytoin interacts with all Class 1 drugs because it is an enzyme inducer and reduces their efficacy.
Lidocaine & Mexiletine

What class antiarrhythmics do these meds belong to and when would they be indicated?
Antiarrhythmics: Class 1b
Indicated in Ventricular, Supraventricular arrhythmias
(more effective with ventricular arrhythmias)

Weak Na+ blocker
Fast Kinetics/ Express effects at fast heart rates
Antiarrhythmics: Class 1c
indicated in Supraventricular Arrhythmias

Propafenone (Rhythmol) & Flecainide

both can exacerbate heart failure, but which can cause the patient to have a metallic taste, feel dizzy and fatigued, and possibly experience bronchospasms?
Propafenone (Rhythmol)

note: Flecainide can cause the patient to feel dizzy, blurred vision, dyspnea, and tremors
Antiarrhythmics: Class 1c
indicated in Supraventricular Arrhythmias

Propafenone (Rhythmol) & Flecainide

both interact with Digoxin, but which drug causes and increased [Digoxin] concentration of 70%?

What type of symptoms would the patient exhibit?
Propafenone (Rhythmol)


Digoxin is used to treated AFib, AFlutter, and sometimes heart failure.

Dig tox can cause a patient to experience N/V, Confusion, Blurred Vision, See Halos, New Arrhythmias, and/or PVCs

note: Flecainide will increase [Digoxin] by 25%.
Antiarrhythmics: Class 1c
indicated in Supraventricular Arrhythmias

Propafenone (Rhythmol) & Flecainide

both interact with digoxin and SSRIs, but which drug interacts with tricyclic antidepressants (TCAs) with an increase risk of torsades?
Flecainide
Antiarrhythmics: Class 1c
indicated in Supraventricular Arrhythmias

Propafenone (Rhythmol) & Flecainide

Which drug is contraindicated for a patient with coronary artery disease (CAD)?
Flecainide
Choosing an antiarrhythmic!

This drug affects slow channel tissue (SA and AV nodes); decreases rate of automaticity and slows conduction of velocity.

It is most effective in tachycardic arhythmias (sinus tachy, AFib, Aflutter, VFib) and prolongs refractory.
Beta Blockers
(Metoprolol, esmolol, atenolol)

Class II arrhythmias
This drug blocks potassium, sodium, some calcium, and provides nonselective beta blocking actions all in one!
Amiodarone

K+ channel blockers
Class III Antiarrhythmics
This drug is used most often to treat arrhythmias, but can cause pulmonary fibrosis, hypothyroidism, neurologic toxicity, hypotension, torsades, optic neuritis, photosensitivity, N/V/C, and increase LFTs.
Amiodarone

K+ channel blockers
Class III Antiarrhythmics

Note: amiodarone has a long 1/2 life and symptoms can show up long after administration.

Remember Amiodarone is metabolized in liver (CYP 450 3A4), causing so many ade.
This drug could cause your patient to turn blue-gray.
Amiodarone

K+ channel blockers
Class III Antiarrhythmics
What drugs interact with Amiodarone?
Warfarin (increased INR)

Digoxin (1/2 dose)

Statins (rhabdomyolysis)

Grapefruit Juice (inhibition)

Phenytoin (enzyme inducing/dec. efficacy)
What other drugs are Class III antiarrhythmics?
K+ channel blockers

Sotalol, Dofetilide, Ibutilide
Which Class III antiarrhythmic can exacerbate heart failure, cause torsades and lead to bradycardia and wheezing?

Remember that all Class 1 antiarrhythmics can also exacerbate heart failure and torsades. (Na+ chan.blocker)
Sotalol
What drugs interact with Sotalol?

(K+ channel blocker/ Class III antiarrhythmic)
Class 1 drugs (remember same ade)

Tricyclic antidepressants (TCAs)

Fluroquinolones

Clonidine (alpha 2 agonist)
used for hypertension, insomnia, adhd, and tourettes
Which other antiarrhythmics also interact with TCAs?
Class 1a (Procainamide)

Class 1c (Flecainide)

Class III (Sotalol, Ibutilide)
Which antiarrhythmics are contraindicated with a prolonged QT interval?
Class III Antiarrhythmics
K+ Channel Blockers

Dofetilide (Tikosyn) and Ibutilide (Corvert)
Which Class III antiarrhythmic interacts with Hydrachlorthiazides, Verapamil, and Fluroquinolones?

This drug is also metabolized in the liver (CYP450 3A4 ) like amiodarone.
Dofetilide (Tikosyn): new

Note: better tolerated than amiodarone, but very expensive and harder to approve; ade only include dizziness, diarrhea, toursades, and chest pain.
True or False

All Class I/ III antiarrhythmics can cause torsades.
True

Sodium and Potassium
channel blockers
The MOA for this group of drugs blocks Ca+ channels, slows conduction, and prolongs refractory; decrease automaticity.

When are they indicated?
Calcium Channel Blockers (NonDHP)

Diltiazem and Verapamil

Indication: Supraventricular Tachyarrhythmias
This drug inhibits Na-K+ ATPase-->Increases intracellular Na concentration-->Increased intracellular Ca concentratio-->Positive inotropic effect, decreased sympathetic response & decreased renin-angiotensis system output

Indications: AFIB/AFlutter
Digoxin (Lanoxin)

1-3 hours peak
Digoxin is metabolized in the liver (Cyt450-dependent) and has active metabolites which account for long 1/2 life and numerous adverse effects.

What type of ADEs are seen?
Diarrhea

Loss of Appetite

Nausea and Vomiting

Headache/ Visual disturbances

Cardiac Dysrhythmias/ PVCs
What drugs interact with Digoxin?
Verapamil (increase intracellular Ca+)

Amiodarone

Thiazides

Quinidine

Azoles

Macrolides
When is Digoxin absolutely contraindicated?
Ventricular Fibrillation

Heart is one beat/ fibrillation away from asystole and digoxin inhibits sympathetic response
MOA: Binds to antithrombin III to form a complex that inactivates clotting factors II (thrombin), XII, IXa and Xa, preventing conversion of fibrinogen to fibrin and the formation of new thrombi
Hepariin

note: can be administered SubQ and IV; rapid absorption and widely distributed
This drug is recommended for treatment/ prophylaxis of thromboembolism as well as Atrial Fibrillation.
Heparin
Which drug reverses the effects of Heparin?
Protamine Sulfate

(forms inactive protamine-heparin complex)

note: just 1mg of protamine can neutralize 100 units of heparin (slow reversal/ infusion)
This anticoagulant can cause bleeding, thrombocytopenia, and skin necrosis.
Heparin

If thrombocytopenia is going to occur it will do so typically within 5-10 days; stop heparin once platelets are lower than 100,000. (HIT)

If this occurs heparin nor any LMWH can ever be administered
If Heparin cause "HIT" and a patient's platelets drop below 100,000 what can be prescribed as an alternative treatment?
Argatroban
This medication is not a LMWH, but is treated like one. It can be used in the presence of HIT!
Fondaparinux (Arixtra)
These drugs are indicated for prophylaxis of thromboembolism, STEMI, and ischemia.
Low Molecular Weight Heparins (LMWH) & Factor Xa Inhibitor

Dalteparin (Fragmin)
Enoxaparin (Lovenox)
Tinzaparin (Innohep)
These drugs are unable to bind to thrombin very effectively, but do bind to AT-III to produce anticoagulant effects.
Low Molecular Weight Heparins (LMWH) & Factor Xa Inhibitor

Dalteparin (Fragmin)
Enoxaparin (Lovenox)
Tinzaparin (Innohep)
Who has a longer 1/2 time life heparin or LMWH?
Low Molecular Weight Heparins (LMWH) & Factor Xa Inhibitor

Dalteparin (Fragmin)
Enoxaparin (Lovenox)
Tinzaparin (Innohep)


note: must be adjusted in patients with renal inefficiencies.

*Contraindicated when CrCl <30mL/min, because of increased bleeding risk (will continue if benefit outweighs risk)
Heparin or LMWH

Which is contraindicated in obesity?
LMWH

Contraindicated in obesity (>150kg), because of LMW it is not distributed as widely/ Less effective than heparin (injected into abdominal tissue/ less distributed with excess FAT)
True or False

LMWH is ok to use when a patient has experienced HIT.
False

absolute contraindication

(alternative:Argatroban and Fondaparinux (Arixtra))
True or False

LMWH risk of bleeding is decreased due to small molecular size.
False

approximately same risk

Remember Protamine can reverse heparin, but it can only reverse enoxaparin!

note: 1mg protamine : 1mg enoxaparin***
Which drug is only a Factor Xa Inhibitor?
Fondaparinux (Arixtra)

administered SubQ
LMWH has a longer 1/2 life (4hrs) than Heparin, but which drug has a 1/2 life of 17- 21 hours and lends well to once daily dosing!
Fondaparinux (Arixtra)

This drug is eliminated renally and could last even longer when a patient has renal dysfunction.
Which anticoagulants are contraindicated <30 renal function?
LMWH/ Factor Xa Inhibitor
Dalteparin (Fragmin)
Enoxaparin (Lovenox)
Tinzaparin (Innohep)

Factor Xa Inhibitor
Fondaparinux (Arixtra)
Which anticoagulant is contraindicated in patients who weight

>150 kg

<50 kg
>150 kg (LMWH)

<50 kg Fondaparinux (Arixtra)
Note:
LMWH or Factor-Xa Inhibitor v. Heparin

Easier dosing **once daily available
Less lab monitoring (lmw and FXA)
Can be used at home* (heparin cannot)
Unknown effects in renal insufficiency & obesity (Heparin is o.k. here)
More expensive (LMW and Factor xa)
This anticoagulant can be give oral, IV and PO. It is dosing equivalent IV/PO. It is also a Vitamin K antagonist.
Warfarin (Coumadin)
MOA: Stops conversion of vitamin K epoxide to active vitamin K -->Lack of activated clotting factors II, VII, IX, X and Protein C & S
Warfarin (Coumadin)

Indications: Treatment (in conjunction w/heparin or LMWH or fondaparinux for 1st several days. It takes a while to be effective.) & prophylaxis of thromboembolism, atrial fibrillation, cardiac valves
LMWH has a longer 1/2 life (4hrs) than Heparin and Fondaparinux has an even longer 1/2 life (17-21hrs) and can be given once daily.

Warfarin's T1/2 life is 20- 60 hours, but what is its drawback?
Onset 36-72 hrs
Effect 5-7 days
SS-10-14 days

It is rapidly absorbed but it does take time to become effective and will take adjustments for proper dosing.
Which anticoagulant has the greatest incidence of bleeding?
Warfarin (2.4 to 29%)
including epistaxis,GI bleeds, bleeding gums, hematuria

2.8% chance of a fatal bleed
Which anticoagulant has the severest form of necrosis at the site of injection and why?
Warfarin

Significant thrombosis of venules & capillaries within SubQ fat tissue (abdomen, buttocks, thighs, breasts)
Occurs due to deficiency in Proteins C & S
Typically occurs by Day 10 of therapy initiation
Tx—Temporarily stop warfarin (initiate heparin/LMWH) and gradually restart & titrate warfarin
What is purple toe syndrome?
Systemic cholesterol microembolism resulting from release of atheromatous plaque (plaque is released from vessels in blood and depositing in toes.)

Typically occurs within 3-10 weeks of warfarin initiation
Warfarin Drug Interactions that increase INR.
Amiodarone (potassium channel blocker/ Class III)
EtOH (acute*)
ASA (aspiriin)
NSAID’s (Ibuprofen, naproxen, etc.)
Celecoxib (Celebrex) anti inflammatory
Most antibiotics (Bactrim, Flagyl, Cephalosporins, Fluoroquinolones, Erythromycin, Tetracycline, etc.)
Fluconazole (Diflucan)
Garlic, gingko, ginseng, green tea
Warfarin drug interactions that decrease INR.
EtOH (chronic)
Barbiturates/ Phenobarbital (enzyme inducers; rapid metabolism; eliminated quicker and less efficacy)
Carbamazepine (Tegretol)
Phenytoin (enzyme inducer)
Vitamin K
Warfarin drug interactions that impair absorption.
Bile acid sequestrants (hyperlipidemias)—Questran ; local and bind to GI tract interfering with absorption.