DRUGS

Disopyramide

Class: 1a (Na+ Channel Blocker)

Class Action: Increase QRS, QT, AP, ERP, SLOWS PHASE 0 DEPOLARIZATION

Procainamide

Class: 1a (Na+ Channel Blocker)

Class Action: Increase QRS, QT, AP, ERP, SLOWS PHASE 0 DEPOLARIZATION

Adverse Effects: Rash

Quinidine

Class: 1a (Na+ Channel Blocker)

Class Action: Increase QRS, QT, AP, ERP, SLOWS PHASE 0 DEPOLARIZATION

MOA: Slows uptake of action potentials

Adverse Effects: Cinchonism

Lidocaine

Class: 1b (Na+ Channel Blocker)

Class Action: Decrease QT, ± QRS, AP, ERP, SHORTENS PHASE 3 REPOLARIZATION AND DECREASES DURATION OF ACTION POTENTIAL

Choose to give IV because heavy first pass metabolism

Mexilitine

Class: 1b (Na+ Channel Blocker)

Class Action: Decrease QT, ± QRS, AP, ERP, SHORTENS PHASE 3 REPOLARIZATION AND DECREASES DURATION OF ACTION POTENTIAL

Choose to give IV because heavy first pass metabolism

Flecainide

Class: 1c (Na+ Channel Blocker)

Class Action: Increase ARS, ± QT/AP; SLOWS PHASE 0 DEPOLARIZATION

Propafenone

Class: 1c (Na+ Channel Blocker)

Class Action: Increase ARS, ± QT/AP; SLOWS PHASE 0 DEPOLARIZATION

Atenolol

Class: 2 (Beta Blocker)

Class Action: Decrease HR/Conduction Velocity, Increase PR interval; DECREASE RATE OF PHASE 4 DEPOLARIZATION (decrease automaticity, reduce myocardial oxygen demand), PROLONG REPLOARIZATION (increase effective refractory period, decrease re-entry).

Indication: HTN, angina, anti-arryhthmic

Esmolol

Class: 2 (Beta Blocker)

Class Action: Decrease HR/Conduction Velocity, Increase PR interval; DECREASE RATE OF PHASE 4 DEPOLARIZATION (decrease automaticity, reduce myocardial oxygen demand), PROLONG REPLOARIZATION (increase effective refractory period, decrease re-entry).

INDICATIONS: Acute arrhythmias during surgery or emergency situations

Adverse Effects: Dissipate quickly when drug is stopped

antiarrhymic

Propranolol

Class: 2 (Beta Blocker)

Class Action: Decrease HR/Conduction Velocity, Increase PR interval; DECREASE RATE OF PHASE 4 DEPOLARIZATION (decrease automaticity, reduce myocardial oxygen demand), PROLONG REPLOARIZATION (increase effective refractory period, decrease re-entry).

INDICATIONS: Longterm management of agina pectoris, prevention of sudden death and re-infarction after MI

angina antiarrhymic htn

Acebutolol

Class: 2 (Beta Blocker)

Class Action: Decrease HR/Conduction Velocity, Increase PR interval; DECREASE RATE OF PHASE 4 DEPOLARIZATION (decrease automaticity, reduce myocardial oxygen demand), PROLONG REPLOARIZATION (increase effective refractory period, decrease re-entry).

antiarrhymic htn

Metoprolol

Class: 2 (Beta Blocker)

Class Action: Decrease HR/Conduction Velocity, Increase PR interval; DECREASE RATE OF PHASE 4 DEPOLARIZATION (decrease automaticity, reduce myocardial oxygen demand), PROLONG REPLOARIZATION (increase effective refractory period, decrease re-entry).

INDICATIONS: Rate control of Afib/aflutter, Post-MI, long term treatment for angina pectoris

Contraindications: Avoid with SSRIs, antipsychotics, antiretroviral, antimalarial, and other antiarrythmics such as PROPAFENONE, QUINIDINE

Adverse Effects: Sudden discontinuation in pts with ischemic heart disease can cause severe angina, MI, and ventricular arrhythmias ( have to gradually reduce dosage over weeks )

antiarrhymic angina htn

Labetolol

Class: 2 (Beta Blocker)

Class Action: Decrease HR/Conduction Velocity, Increase PR interval; DECREASE RATE OF PHASE 4 DEPOLARIZATION (decrease automaticity, reduce myocardial oxygen demand), PROLONG REPLOARIZATION (increase effective refractory period, decrease re-entry).

INDICATIONS: Hypertensive emergency, pregnancy

htn

Bisoprolol

Class: 2 (Beta Blocker)

Class Action: Decrease HR/Conduction Velocity, Increase PR interval; DECREASE RATE OF PHASE 4 DEPOLARIZATION (decrease automaticity, reduce myocardial oxygen demand), PROLONG REPLOARIZATION (increase effective refractory period, decrease re-entry).

INDICATIONS: Angina

Amiodarone

Class: 3 (K+ channel blockers)

Class Action: Prolongs ADP, QT interval, QRS, ERP, Prolongs phase 3 repolarization, Slows HR, Delays AV conduction

INDICATIONS: SVT (Afib), prevents recurrent ventricular tachy, low doses can restore and maintain sinus rhythm in patients with afib

Contraindications: Increases exposure to other drugs like statins, digoxin, warfarin

Adverse Effects: Blue people, pulmonary fibrosis

Dofetilide

Class: 3 (K+ channel blockers)

Class Action: Prolongs ADP, QT interval, QRS, ERP, Prolongs phase 3 repolarization, Slows HR, Delays AV conduction

INDICATIONS: persistent afib

Dronedarone

Class: 3 (K+ channel blockers)

Class Action: Prolongs ADP, QT interval, QRS, ERP, Prolongs phase 3 repolarization, Slows HR, Delays AV conduction

Like amiodarone but less toxic

Ibutilide

Class: 3 (K+ channel blockers)

Class Action: Prolongs ADP, QT interval, QRS, ERP, Prolongs phase 3 repolarization, Slows HR, Delays AV conduction

INDICATIONS: acute chemical cardioversion

Sotalol

Class: 3 (K+ channel blockers)

Class Action: Prolongs ADP, QT interval, QRS, ERP, Prolongs phase 3 repolarization, Slows HR, Delays AV conduction, beta blocker effects

INDICATIONS: SVT/VT

Diltiazem

Class: 4 (CCB) Non-dyhydropiridine

[ Dhydropiridines have NO antiarrhythimic properties and are used in hypertension ]

Class Action: Decreased rate of phase 4 spontaneous depolarization in AV and SA nodes (decrease excitability of SA, prolong AV node), INHIBITS ACTION POTENTIAL IN SA AND AV NODES

INDICATIONS: Prevention of vasospastic and classical angina

Verapamil

Class: 4 (CCB) Non-dyhydropiridine

[ Dhydropiridines have NO antiarrhythimic properties and are used in hypertension ]

Class Action: Decreased rate of phase 4 spontaneous depolarization in AV and SA nodes (decrease excitability of SA, prolong AV node), INHIBITS ACTION POTENTIAL IN SA AND AV NODES

INDICATIONS: 2nd choice for acute treatment of vasospastic and stable angina

Adverse Effects: Constipation, hyperprolactinemia

Adenosine

Class Action: INHIBITS conduction IN SA AND AV NODES

INDICATIONS: SVT

Adverse Effects: Flushing

Digoxin

Class Action: Inhibits Na/K ATPase

INDICATIONS: HF

Contraindications: Chronic Kidney disease, hypokalemia promotes toxicity → be careful with loop diuretics

Adverse Effects: Dose dependent → neurologic, GI, visual (yellow disturbances), AV Block

Magnesium Sulfate

Class Action: Blocks calcium channels

INDICATIONS: Acute treatment of torsades

Ranolazine

Class Action: Prolongs QT → inhibits fatty acid B-ox in myocytes

INDICATIONS: chronic stable angina, refractory atrial and ventricular arrhythmias

Contraindications: Increases exposure to other drugs like statins, digoxin, warfarin

Atorvastatin

Class: HMG CoA Reductase Inhibitors

Class Action: Activates sterol regulatory element binding protein 2 (SREBP2) to UPREGULATE LDL receptor; SREBP is inactive at the ER when activated it moves to the Golgi complex; dose dependent - LDL is reduced by 6% with each dose doubling (max effect in 7-10 days); Tg will decrease, HDL will increase, standard to give post MI

INDICATIONS: Adolescent patients with HeFH

Contraindications: Amiodarone, Verapamil, Lipophilic

Additional: Long acting

Adverse Effects: Hepatotoxicity, myopathy (increase creatinine kinase), rhabdomylosis, Hives, Edema of face/lips/tongue/throat

Simvistatin

Class: HMG CoA Reductase Inhibitors

Class Action: Activates sterol regulatory element binding protein 2 (SREBP2) to UPREGULATE LDL receptor; SREBP is inactive at the ER when activated it moves to the Golgi complex; dose dependent - LDL is reduced by 6% with each dose doubling (max effect in 7-10 days); Tg will decrease, HDL will increase, standard to give post MI

Contraindications: Amiodarone, Verapamil, Grapefuit juice, Cyp3A4, Lipophilic

Additional: short acting

Adverse Effects: Hepatotoxicity, myopathy (increase creatinine kinase), rhabdomylosis

Lovastatin

Class: HMG CoA Reductase Inhibitors

Class Action: Activates sterol regulatory element binding protein 2 (SREBP2) to UPREGULATE LDL receptor; SREBP is inactive at the ER when activated it moves to the Golgi complex; dose dependent - LDL is reduced by 6% with each dose doubling (max effect in 7-10 days); Tg will decrease, HDL will increase, standard to give post MI

INDICATIONS: Adolescent patients with HeFH

Contraindications: Amiodarone, Verapamil, Grapefuit juice, Cyp3A4, Lipophilic

Additional: short acting

Adverse Effects: Hepatotoxicity, myopathy (increase creatinine kinase), rhabdomylosis

Rouvastatin

Class: HMG CoA Reductase Inhibitors

Class Action: Activates sterol regulatory element binding protein 2 (SREBP2) to UPREGULATE LDL receptor; SREBP is inactive at the ER when activated it moves to the Golgi complex; dose dependent - LDL is reduced by 6% with each dose doubling (max effect in 7-10 days); Tg will decrease, HDL will increase, standard to give post MI

Contraindications: Amiodarone, Verapamil, Hydrophilic (causes less maylgias)

Additional: long acting

Pravastatin

Class: HMG CoA Reductase Inhibitors

Class Action: Activates sterol regulatory element binding protein 2 (SREBP2) to UPREGULATE LDL receptor; SREBP is inactive at the ER when activated it moves to the Golgi complex; dose dependent - LDL is reduced by 6% with each dose doubling (max effect in 7-10 days); Tg will decrease, HDL will increase, standard to give post MI

INDICATIONS: Adolescent patients with HeFH

Contraindications: Amiodarone, Verapamil, Hydrophilic

Additional: Only statin where absorption is not improved with food; metabolized by non-p450 pathways; short acting

Fluvastatin

Class: HMG CoA Reductase Inhibitors

Class Action: Activates sterol regulatory element binding protein 2 (SREBP2) to UPREGULATE LDL receptor; SREBP is inactive at the ER when activated it moves to the Golgi complex; dose dependent - LDL is reduced by 6% with each dose doubling (max effect in 7-10 days); Tg will decrease, HDL will increase, standard to give post MI

Contraindications: Amiodarone, Verapamil, Hydrophilic

Additional: short acting

Pitavastatin

Class: HMG CoA Reductase Inhibitors

Class Action: Activates sterol regulatory element binding protein 2 (SREBP2) to UPREGULATE LDL receptor; SREBP is inactive at the ER when activated it moves to the Golgi complex; dose dependent - LDL is reduced by 6% with each dose doubling (max effect in 7-10 days); Tg will decrease, HDL will increase, standard to give post MI

Contraindications: Amiodarone, Verapamil

Colestipol, Cholestyramine, Colesevelam

Class: Bile Acid Sequestrates

Class Action: Binds bile acids in the intestinal lumen and prevents reabsorption or return to liver; upregulate of LDL receptors, increased hepatic synthesis of bile acids from cholesterol (reduce hepatic cholesterol content)

INDICATIONS: Isolated increased LDL, used as a second drug if statin is not properly working

Contraindications: HoFH (lack LDL receptors), hypertryglyceridemia

Additional: Increase levels or other oral medications to combat decreased absorption due to drug, decreased absorption of fat soluble vitamins

Niacin / VitB3

Class: Nicotinic Acids

Class Action: Inhibits HSL in adipose tissue preventing the breakdown of triglycerides

INDICATIONS: Most effective agent for increasing HDL

Contraindications: Avoid in diabetes and gout

Gemfibrozil/Fenofibrate

Class: Fibrates

Class Action: PPAR-alpha activator; upregulates LPL → upregulates ApoA1 and apoa2, decrease apoc3 -→ MAJOR DECREASE IN TAGS

INDICATIONS: Hypertrygliceridemia

Contraindications: Hepatic/Renal Dysfunction, biliary tract disease

Additional: Avoid warfarin with both, but avoid statins with gemfibrozil

Ezetimibe

Class: Cholesterol absorption Inhibitor

Class Action: Inhibit NPC1 in intestinal lumen → works synergistic effects on LDL when used with statins

INDICATIONS: Isolated increased LDL, used as a second drug if statin is not properly working

Contraindications: Statins if they have hepatic disease or elevated serum transaminases

Additional: Increase levels with fibrates; decrease with cholestyramine

Lomitapide

Class: MTP inhibitor

Class Action: Binds and inhibits MTP → stops assembly of cholymicrons and VLDL

Contraindications: Hepatotoxicity

Additional: Grapefruit juice

Mipomersen

Class: Antisense inhibition of ApoB100 synthesis

Idications: HoFH

Contraindications: Hepatotoxictiy

Alirocumab, Evolocumab

Class: PCSK9 Inhibitors

Class Action: Inactivate PCSK9 to reduce LDL receptor degradation, reduce LDL cholesterol in plasma, increase LDL receptors on hepatocytes

Contraindications: Not FDA approved for treatment of hyperlipidemia in statin- intolerant patients without known ASCVD, expensive

Additional: When used with statins produces an additional 36-59% reduction in LDL

Adverse Effects: Nasopharyngitis, Flu-like symptoms

Amlodipine

Class: 4 (CCB) Dyhydropiridine

[ Dhydropiridines have NO antiarrhythimic properties and are used in hypertension ]

Class Action: Vasodilation

Indications: HTN

Felodipine

Class: 4 (CCB) Dyhydropiridine

[ Dhydropiridines have NO antiarrhythimic properties and are used in hypertension ]

Nifedipine

Class: 4 (CCB) Dyhydropiridine

[ Dhydropiridines have NO antiarrhythimic properties and are used in hypertension ]

Class Action: Vasodilation → directly dilates peripheral arterioles

Indications: Vasospastic Angina, prophylaxis of HTN

Contraindications: Cimetidine (causes 80% increase in levels), dose adjustment needed for Chronic liver disease

Nitroglycerin

Class: Nitrates

Class Action: GST and MtADH2 (increases cGMP)→ release nitric oxide → venodilation

Indications: Angina (immead relief)

Increases cGMP in arterial smooth muscle

Contraindications: PDE5 inhibitors

Can gain tolerance, no first pass metabolism, dermal patches, tolerance develops (12hr intervals), very low bioavailability

Isosorbide Mononitrate is a stable alternative that has less hepatic breakdown

Captopril, Enalapril, Fosinopril, Lisinopril

Class: ACE Inhibitor

Indications: HTN, heart failure

Contraindications: Pregnancy, bilateral renal artery stenosis

Side Effects: COUGH, angioedema, teratogenicity, creatinine increase, hyperkalemia, hypotension

Azilsartan, Candesartan, Losartan, Valsartan

Class: Angiotensin II receptor blockers (ARBs) → AT1 receptors

Indications: HTN, heart failure

Contraindications: Pregnancy

Note: Oral bioavailability is low except for azilsartan and irbesartan; protein binding is high

Side Effects: COUGH, angioedema, hyperkalemia, fetal toxicity

Aliskiren

Class: Renin Inhibitor

Indications: HTN

Contraindications: w/ ACE and ARB in DM

Side Effects: fetal toxicity

Hydralazine

Class: cGMP increase

Indications: HTN

Side Effects: drug induced lupus

Doxazosin

Class: Alpha 1 blocker

Indications: Benign Prostatic Hyperplasia, HTN

Prazosin

Class: Alpha 1 blocker

Indications: HTN

Clonidine

Class: Alpha 2 receptor agonists

Indications: HTN

Side Effects: If stop too quickly → rebound HTN

Methyldopa

Class: Alpha 2 receptor agonists

Indications: HTN during pregnancy

Side Effects: Transient sedation, drowsiness, depression, hepatotoxicity, HEMOLYTIC ANEMIA