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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 |
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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) |
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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 |
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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 |
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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 |
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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 |
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Class 1a antiarrhythmics are treated with what type of drug?
Give an example? |
Sodium Channel Blockers
Quinidine, procainamide, disopyramide |
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Class 1b antiarrhythmics are treated with what type of drug?
Give an example? |
Sodium Channel Blockers
Lidocaine, mexiletine |
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Class 1c antiarrhythmics are treated with what type of drug?
Give an example? |
Sodium Channel Blockers
Propafenone, flecainide, moricizine |
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Class II antiarrhythmics are treated with what type of drug?
Give an example? |
Beta Blockers
Metoprolol, esmolol, atenolol |
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Class III antiarrhythmics are treated with what type of drug?
Give an example? |
Potassium Channel Blockers
Amiodarone, sotalol, dofetilide, ibutilide |
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Class III antiarrhythmics are treated with what type of drug?
Give an example? |
Calcium Channel Blockers (Non DHP)
Diltiazem, verapamil |
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What is the MOA/ Indication for low molecular weight heparins (LMWH)?
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Binds to AT-III to produce anticoagulant effect
Indications: Prophylaxis of thromboembolism, STEMI, ischemia Ex: Dalteparin (Fragmin) Enoxaparin (Lovenox) Tinzaparin (Innohep) |
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What is the MOA/ Indication for Factor Xa?
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Synthetic pentasaccharide that causes AT-III inhibitor of Factor Xa to prevent thrombin formation
For treatment & prophylaxis of thromboembolism Ex:Fondaparinux (Arixtra) |
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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 |
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Will Amiodarone increase or decrease INR when used with Warfarin?
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Increase
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Will ETOH (acute use) increase or decrease INR when used with Warfarin?
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Increase
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Will aspirin increase or decrease INR when used with Warfarin?
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Increase
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Will NSAIDs (Ibuprofen, naproxen, etc) increase or decrease INR when used with Warfarin?
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Increase
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Will Celecoxib (Celebrex) increase or decrease INR when used with Warfarin?
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Increase
|
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Will antibiotics increase or decrease INR when used with Warfarin?
Bactrim, Flagyl, Cephalosporins, Fluoroquinolones, Erythromycin, Tetracycline, etc |
Increase
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Will Fluconazole (Diflucan) increase or decrease INR when used with Warfarin?
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Increase
|
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What type of drug do you use to treat 2nd and 3rd degree heart blocks?
|
None!
Potentially Fatal |
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Where are all Na+ channel blockers metabolized?
Antiarrhythmics Class I |
Hepatic (P450)
|
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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 |
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Class I, III, IV antiarrhythmics all treat supraventricular arrhythmias, which also treat ventricular arrhythmias?
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Class Ia/Ib and Class III
Note: Class Ib are not very potent antiarrhythmics, but are more effective with ventricular arrhythmias. (Lidocaine, Mexiletine ) |
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What type of drugs are
Antiarrhythmics Class Ia ? |
Sodium Channel Blockers
Quinidine, Procainamide, Disopyramide (Norpace) Indicated with Supraventricular & ventricular arrhythmias |
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What type of drugs are
Antiarrhythmics Class Ib ? |
Sodium Channel Blockers
Lidocaine, Mexiletine Indicated with Supraventricular & ventricular arrhythmias (more effective with ventricular arrhythmias) |
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What type of drugs are
Antiarrhythmics Class Ic ? |
Sodium Channel Blockers
Propafenone (Rhythmol), Flecainide, Moricizine Indicated with Supraventricular arrhythmias |
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What type of drugs are
Antiarrhythmics Class II ? |
Beta 1 Blockers
Metoprolol, Esmolol, Atenolol Indicated with Sinus tachycardia, atrial fibrillation, atrial flutter, ventricular fibrillation |
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What type of drugs are
Antiarrhythmics Class III ? |
Potassium Channel Blockers
Amiodarone, Sotalol, Dofetilide (Tikosyn), Ibutilide (Corvert) Indicated with Supraventricular & ventricular arrhythmias |
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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) |
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Antiarrhythmics: Class Ia
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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 |
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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 |
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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
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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 |
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Antiarrhythmics: Class Ia
Sodium Channel Blockers Quinidine, Procainamide, Disopyramide (Norpace) Which drug interacts with Warfarin; increasing INR? |
Quinidine
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Antiarrhythmics: Class Ia
Sodium Channel Blockers Quinidine, Procainamide, Disopyramide (Norpace) Which drug interacts with the efficacy of Fluoroquinolones? |
Procainamide and Disopyramide (Norpace)
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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 |
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Antiarrhythmics: Class Ia
Sodium Channel Blockers Quinidine, Procainamide, Disopyramide (Norpace) Which drug interacts with tricyclic antidepressants (TCAs)? |
Procainamide
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Antiarrhythmics: Class Ia
Sodium Channel Blockers Quinidine, Procainamide, Disopyramide (Norpace) Which drug should be avoided with patients who have renal or hepatic dysfunction? |
Procainamide
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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
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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)
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Antiarrhythmics Class Ib
Lidocaine, Mexiletine Which is contraindicated in 3rd degree heart blocks? |
Both
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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 |
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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. |
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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 |
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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 |
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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%. |
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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
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Antiarrhythmics: Class 1c
indicated in Supraventricular Arrhythmias Propafenone (Rhythmol) & Flecainide Which drug is contraindicated for a patient with coronary artery disease (CAD)? |
Flecainide
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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 |
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This drug blocks potassium, sodium, some calcium, and provides nonselective beta blocking actions all in one!
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Amiodarone
K+ channel blockers Class III Antiarrhythmics |
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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.
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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. |
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This drug could cause your patient to turn blue-gray.
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Amiodarone
K+ channel blockers Class III Antiarrhythmics |
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What drugs interact with Amiodarone?
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Warfarin (increased INR)
Digoxin (1/2 dose) Statins (rhabdomyolysis) Grapefruit Juice (inhibition) Phenytoin (enzyme inducing/dec. efficacy) |
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What other drugs are Class III antiarrhythmics?
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K+ channel blockers
Sotalol, Dofetilide, Ibutilide |
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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
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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 |
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Which other antiarrhythmics also interact with TCAs?
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Class 1a (Procainamide)
Class 1c (Flecainide) Class III (Sotalol, Ibutilide) |
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Which antiarrhythmics are contraindicated with a prolonged QT interval?
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Class III Antiarrhythmics
K+ Channel Blockers Dofetilide (Tikosyn) and Ibutilide (Corvert) |
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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. |
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True or False
All Class I/ III antiarrhythmics can cause torsades. |
True
Sodium and Potassium channel blockers |
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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 |
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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 |
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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 |
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What drugs interact with Digoxin?
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Verapamil (increase intracellular Ca+)
Amiodarone Thiazides Quinidine Azoles Macrolides |
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When is Digoxin absolutely contraindicated?
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Ventricular Fibrillation
Heart is one beat/ fibrillation away from asystole and digoxin inhibits sympathetic response |
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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
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Hepariin
note: can be administered SubQ and IV; rapid absorption and widely distributed |
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This drug is recommended for treatment/ prophylaxis of thromboembolism as well as Atrial Fibrillation.
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Heparin
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Which drug reverses the effects of Heparin?
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Protamine Sulfate
(forms inactive protamine-heparin complex) note: just 1mg of protamine can neutralize 100 units of heparin (slow reversal/ infusion) |
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This anticoagulant can cause bleeding, thrombocytopenia, and skin necrosis.
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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 |
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If Heparin cause "HIT" and a patient's platelets drop below 100,000 what can be prescribed as an alternative treatment?
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Argatroban
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This medication is not a LMWH, but is treated like one. It can be used in the presence of HIT!
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Fondaparinux (Arixtra)
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These drugs are indicated for prophylaxis of thromboembolism, STEMI, and ischemia.
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Low Molecular Weight Heparins (LMWH) & Factor Xa Inhibitor
Dalteparin (Fragmin) Enoxaparin (Lovenox) Tinzaparin (Innohep) |
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These drugs are unable to bind to thrombin very effectively, but do bind to AT-III to produce anticoagulant effects.
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Low Molecular Weight Heparins (LMWH) & Factor Xa Inhibitor
Dalteparin (Fragmin) Enoxaparin (Lovenox) Tinzaparin (Innohep) |
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Who has a longer 1/2 time life heparin or LMWH?
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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) |
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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) |
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True or False
LMWH is ok to use when a patient has experienced HIT. |
False
absolute contraindication (alternative:Argatroban and Fondaparinux (Arixtra)) |
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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*** |
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Which drug is only a Factor Xa Inhibitor?
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Fondaparinux (Arixtra)
administered SubQ |
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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!
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Fondaparinux (Arixtra)
This drug is eliminated renally and could last even longer when a patient has renal dysfunction. |
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Which anticoagulants are contraindicated <30 renal function?
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LMWH/ Factor Xa Inhibitor
Dalteparin (Fragmin) Enoxaparin (Lovenox) Tinzaparin (Innohep) Factor Xa Inhibitor Fondaparinux (Arixtra) |
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Which anticoagulant is contraindicated in patients who weight
>150 kg <50 kg |
>150 kg (LMWH)
<50 kg Fondaparinux (Arixtra) |
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Note:
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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) |
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This anticoagulant can be give oral, IV and PO. It is dosing equivalent IV/PO. It is also a Vitamin K antagonist.
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Warfarin (Coumadin)
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MOA: Stops conversion of vitamin K epoxide to active vitamin K -->Lack of activated clotting factors II, VII, IX, X and Protein C & S
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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 |
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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. |
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Which anticoagulant has the greatest incidence of bleeding?
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Warfarin (2.4 to 29%)
including epistaxis,GI bleeds, bleeding gums, hematuria 2.8% chance of a fatal bleed |
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Which anticoagulant has the severest form of necrosis at the site of injection and why?
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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 |
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What is purple toe syndrome?
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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 |
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Warfarin Drug Interactions that increase INR.
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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 |
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Warfarin drug interactions that decrease INR.
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EtOH (chronic)
Barbiturates/ Phenobarbital (enzyme inducers; rapid metabolism; eliminated quicker and less efficacy) Carbamazepine (Tegretol) Phenytoin (enzyme inducer) Vitamin K |
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Warfarin drug interactions that impair absorption.
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Bile acid sequestrants (hyperlipidemias)—Questran ; local and bind to GI tract interfering with absorption.
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