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15 Cards in this Set

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Quinidine // Procainamide // Disopyramide
Type IA Antiarrhythmics

Mech: Block Na+ Channels and K+ channels.

Effects:
↓ Na+ channels open
Ventricles/Atria: Prolong Phase 0 Depolarization.
Nodes (AV/SA): ↓ # of funny Na channels open --> longer time to depolarize
↓ K+ channels open
Ventricles/Atria: Prolongs Phase 3 (repolarization) --> Longer Refractory Period & Longer QT

Use:
Atrial & Ventricular Arrhythmias
Ectopic and Reentrant SVT & V-Tach

Toxicities:
Quinidine - Thrombocytopenia, Torsades De Pointes, & Tinnitus
Procainamide - SLE-like syndrome
Phenytoin // Lidocaine // Mexilitine // Tocainide
Type IB Antiarrhythmics

Mech: Na Channel Blocker & K+ Channel Opener

Effects:
Na Channel Blocker
Ventricles/Atria: ↓ slope of Phase 0
SA/AV Nodes: ↓ # of funny Na Channels --> Longer to Depolarize Nodes
K+ Channel Opener
Atria/Ventricle: ↓ repolarization time --> ↓ Refractory time & ↓ QT

Use: Ischemic or Depolarized Purkinje/Ventricle. POST-MI
Acute Ventricular Arrhythmia (POST-MI)
Digitalis Induced Arrhythmia

Toxicity: Local Anesthetic, CV Depression
Flecainide // Encainide // Propafenone
Type IC Antiarrhythmics

Mech: Na Channel Blocker (No effect on K+ channels)

Effect:
Atria/Ventricles: Lengthens Depolarization Time (Phase 0)
AV/SA Node: ↓ # of funny Na channels, longer to depolarize

Use: ONLY HEALTHY TISSUE
SVT & VTach-->V-Fib

Toxicity: Proarrhythmic (↑↑↑ POST MI)

**only used as LAST RESORT for refractory VENTRICULAR TACHYARRHYTHMIAS**
Type II Antiarrhythmics
Beta-Blockers (Propanolol, Timolol, Esmolol, Metoprolol)

Mech: Block Beta Adrengergic Receptors

Effects:
Nodal Cells (AV Node VERY SENSITIVE)
1. ↓ Dromotropy: ↓ Open Ca Channels. ↓ conduction velocity through AV Node
2. ↓ Chronotropy: ↓ Funny Na Channels open --> Longer to depolarize, ↓ HR.
*Also ↓ contractility by ↓ intracellular Ca

Use:
SVT
V-Tach
↓ ventricular rate with Aflutter & Afib
Tachycardia
HTN

Toxicities:
Impotence
CV Depression (Bradycardia, AV Block)
Asthma Exacerbation
**Metoprolol: Dyslipidemia**

Basic Pharm Note:
Remember: Beta adrenergic receptors are Gs receptors and work via ↑ Adenylyl Cyclase --> ↑ cAMP --> ↑ Prot. Kinase A --> Phosphorylation of Proteins
Type III Antiarrhythmics
Drugs: Sotalol, Ibutilide, Amiodarone

Mech: K+ Channel Blockers

Effect: Prolong Phase 3 (repolarization) of ONLY VENTRICULAR/ATRIAL cells. ↑ Refractory Period, ↑ QT

Use: When other antiarrhythmics FAIL.

Toxicity:
Amiodarone: Pulmonary Fibrosis, Hepatotoxicity, Thyroid Abnormalities (hypo or hyper). [check PFTs, LFTs, TFTs]; also photosensitivity
Sotalol: Beta Blockade; Torsades
Isobutilide: Torsades
Type IV Antiarrhythmics
Verapamil & Diltiazem

Mech: Calcium Channel Blockers; ESPECIALLY in AV Node.

Effects:
↑ PR Interval, ↑ Refractory Period
↓ Conduction Velocity

Use: Prevention of NODAL Arrhythmias

Toxicities:
CHF
AV Block
Flushing
Constipation

**Heart: Verapamil>Diltiazem>Nifedipine**
**Vessels: Nifedipine>Diltiazem>Verapamil**
Statins (Simvastatin, Atorvastatin, etc.)
Mech: HMG-CoA Reductase Inhibitors

Effects:
↓↓↓ LDL
↑ HDL
↓ Triglycerides

Toxicity: Rhabdomyolysis
Niacin
Mech: Inhibits Lipolysis in adipose tissue and ↓ secretion of VLDL

Effects:
↓↓ LDL
↑↑ HDL
↓ TG

Toxicity:
↑ Uric Acid
Flushing

C/I: GOUT
Bile Acid Resins (Cholestyramine // Colestipol)
Mech: Bind Bile Acids in the Intestine which Inhibits the reuptake of Cholesterol. The Liver then needs to synthesize more cholesterol to make into bile. So, it upregulates its B-100 receptors and uptakes more LDL --> ↓ LDL

Effects:
↓↓ LDL
± HDL
± TG

Toxicity: Tastes bad, ↓ absorption of Fat-soluble Vit., risk of gallstones

C/I: Gallstones
Cholesterol Absorption Blockers
Mech: Block absorption of cholesterol by the intestinal brush border

Effects:
↓↓ LDL
No effect on HDL
No effect on TG

Toxicity: Rare ↑ LFTs
Fibrates (Gemfibrozil // Clofibrate)
Mech: Upregulate Lipoprotein Lipase Activity --> ↑ TG Clearance

Effects:
↓ LDL
↑ HDL
↓↓↓ TG

Toxicity: Myositis, ↑ LFTs
What Cholesterol/Triglyceride Lowering Drug Should you use if your primary goal is to ↑ HDL?
Niacin.

Mech: Inhibits Lipolysis in adipose tissue and ↓ VLDL secretion
What Cholesterol/Triglyceride Lowering Drug Should you use if your primary goal is to ↓ Triglycerides?
Fibrates

Mech: ↑ Lipoprotein Lipase Activity --> ↑ Triglyceride Clearance
What Cholesterol/Triglyceride Lowering Drug Should You Use if Your Primary Goal is to ↓ LDL?
You can use any of them, except FIBRATES.

1st Line is probably Statins.
Important Contraindications to consider when prescribing certain Cholesterol/Triglyceride lowering drugs?
Niacin: GOUT

Cholestyramine - GALLSTONES