CVPR Cardiovascular pharmacology 3 Flashcards
Adverse effects of Niacin
Red flushed face which is ↓ by NSAIDs or long-term use Hyperglycemia Hyperuricemia
What is Hyperuricemia?
Excess uric acid in the blood
PCSK9 inhibitors effect on LDL
↓↓↓
PCSK9 inhibitors effect on HDL
↑
PCSK9 inhibitors effect on triglycerides
↓
PCSK9 inhibitors MOA
- Inactivation of LDL-receptor degradation
- Increasing amount of LDL removed from bloodstream
Adverse effects of PCSK9 inhibitors
- Myalgias
- Delirium
- Dementia
- Other neurocognitive effects
Examples of PCSK9 inhibitors
- Alirocumab
- Evolocumab
Cardiac glycosides
Digoxin
Digoxin MOA
Direct inhibition of Na/K ATPase → indirect inhibition of Na/Ca exchanger ↑[Ca] → (+) ionotropy
Stimulates vagus nerve → ↓ HR
Clinical use of Digoxin
- HF (↑ contractility)
- Atrial fibrillation (↓ conduction at AV node and depression of SA node)
Adverse effects of digoxin
Cholinergic: NVD Blurry yellow vision (think Van Gogh) Arrhythmias AV block Can lead to hyperkalemia which is a poor prognostic indicator
Factors predisposing to Digoxin toxicity
- Renal failure (↓ excretion)
- Hypokalemia (permissive for Digoxin binding at K-binding site on Na/K/ATPase)
- Drugs that displace digoxin from tissue-binding sites ↓ clearance (eg verapamil, amiodarone and quinidine)
Antidote to Digoxin
Slowly normal K Cardiac pacer Anti-digoxin Fab fragments Mg2+
Digoxin diagram
314
Class I sodium channel blockers
Slow or block (↓) conduction (especially in depolarized cells) ↓ slope of phase 0 depolarization Are state dependent (selectively depress tissue that is frequently depolarized [tachycardia]
Antiarrhythmics Class IA
Quinidine Procainamide Disopyramide “The Queen Proclaims Diso’s pyramid”
Class IA Antiarrhythmics MOA
Sodium channel blockers ↑ AP duration ↑ effective refractory period (ERP) in ventricular action potential ↑ QT interval Some potassium channel blocking effects
Clinical uses of Class IA Antiarrhythmics
Both atrial and ventricular arrhythmias Especially re-entrant and ectopic SVT and VT
Adverse effects of Class IA Antiarrhythmics
5 listed
- Cinchonism (headache, tinnitus with quinidine)
- Reversible SLE-like syndrome (procainamide)
- HF (disopyramide)
- Thrombocytopenia
- Torsades du Pointes due to ↑ QT interval
Class IA Antiarrhythmics AP effects
Pg 315
Class IB Antiarrhythmics mnemonic
Lidocaine MexileTine I’d buy Liddy’s Mexican Tacos
Class IB Antiarrhythmics MOA
- ↓AP duration
- Preferentially affect ischemic or depolarized Purkinje and ventricular tissue
- Phenytoin can also fall into the IB category

Phenytoin Class of Antiarrhythmics
Can also fall into the IB category
Clinical uses of Class IB Antiarrhythmics
- Acute ventricular arrhythmias (especially post-MI)
- Digitalis-induced arrhythmias
- IB- is Best post-MI
Adverse effects of Class IB Antiarrhythmics
- CNS
- stimulation/depression
- Cardiovascular depression
Class IB Antiarrhythmics AP
315
Class IC Antiarrhythmics Mnemonic
Class IC Flecainide Propafenone Can I have Fries, Please
Class IC Antiarrhythmics MOA
- Significantly prolongs ERP in AV node and accessory bypass tracts
- No effect on ERP in Purkinje and ventricular tissue
- Minimal effect on AP duration
Clinical use of Class IC Antiarrhythmics
- SVTs (including atrial fibrillation)
- Only as a last resort in refractory VT
Adverse effects of Class IC Antiarrhythmics
- Proarrhythmic, especially Post-MI (contraindicated)
- Class IC is Contraindicated in structural and ischemic heart disease
Class IC Antiarrhythmics contraindicated in?
- Proarrhythmic, especially post-MI (contraindicated)
- IC is Contraindicated in structural and ischemic heart disease
Class IC Antiarrhythmics AP
315

Class II Antiarrhythmics and examples
β-blockers
Metoprolol
Propranolol
Esmolol
Atenolol
Timolol
Carvedilol
Class II Antiarrhythmics MOA
- Decrease SA and AV nodal activity by ↓ cAMP which ↓Ca currents
- Suppress abnormal pacemakers by ↓ slope of phase 4 AV node is particularly sensitive - ↑PR interval

Esmolol duration of action
Very short acting
Very short acting β-blockers
Esmolol
Class II Antiarrhythmics affinity
AV node is particularly sensitive - ↑PR interval
Class II Antiarrhythmics AP
316

Class II Antiarrhythmics Clinical uses
- SVT
- Ventricular rate control for atrial fibrillation and atrial flutter
Adverse effects of Class II Antiarrhythmics
- Impotence
- Exacerbation of COPD and asthma
- Cardiovascular effects (Bradycardia, AV block, HF)
- CNS effects (sedation, sleep alterations)
- May mask the signs of hypoglycemia (caution in diabetes)
- Metoprolol can cause dyslipidemia
- Propranolol can exacerbate vasospasm in Prinzmetal angina
- β-blockers (except non-selective α- and β-antagonists carvedilol and labetalol) cause unopposed α1 agonism if given alone for pheochromocytoma or cocaine toxicity
Treatment of β-blocker OD
- Saline
- Atropine
- Glucagon
Class III Antiarrhythmics Mnemonic and main action
Potassium channel blockers
AIDS
- Amiodarone
- Ibutilide
- Dofetilide
- Sotalol
Class III Antiarrhythmics MOA
- ↑AP duration
- ↑ERP
- ↑QT interval

Class III Antiarrhythmics AP
316

Clinical use of Class III Antiarrhythmics
- Atrial fibrillation
- Atrial flutter
- Ventricular tachycardia (amiodarone, sotalol)
Adverse effects of Class III Antiarrhythmics
Sotalol - torsades de pointes, excessive β-blockade
Ibutilide - torsades de pointes
Amiodarone - pulmonary fibrosis, hepatotoxicity, hypothyroidism or hyperthyroidism (amiodarone is 40% iodine by weight) acts as a hapten (corneal deposits, blue/gray skin deposits resulting in photodermatitis), neurologic effects, constipation, cardiovascular effects (bradycardia, heart block, HF)
Considerations when using amiodarone?
Remember to check PFTs, LFTs and TFTs when using amiodarone Amiodarone is lipophilic and has class I, II, III and IV effects
Class IV Antiarrhythmics main action and examples
Ca channel blockers Verapamil Diltiazem
Class IV Antiarrhythmics MOA
↓ conduction velocity ↑ ERP ↑ PR interval
Clinical uses of Class IV Antiarrhythmics
- Prevention of nodal arrhythmias (eg SVT)
- Rate control in atrial fibrillation
Adverse effects of Class IV Antiarrhythmics
Constipation Flushing Edema Cardiovascular effects (HF, AV block, sinus node depression)
Class IV Antiarrhythmics AP
317

Other antiarrhythmics
- Adenosine
- Mg2+
Adenosine as an antiarrhythmic
↑K efflux out of cells → hyperpolarizing the cell and ↓ Ica, ↓AV node conduction
Adenosine clinical uses for antiarrhythmia
Drug of choice in diagnosin/terminating certain forms of SVT
Adenosine duration of action
Very short acting (≈ 15 seconds)
Adenosine effects are blunted by?
Caffeine and theophylline (both are adenosine receptor antagonists)
Adverse effects of adenosine
- Flushing
- Hypotension
- Chest pain
- Sense of impending doom
- Bronchospasm
Mg2+ as an antiarrhythmic
Effective in torsades de pointes and digoxin toxicity
Ivabradine MOA
Selective inhibition of funny Na channels (If) prolonging slow depolarization phase 4 ↓ SA node firing: Negative chronotropic effect without ionotropy Reduces cardiac O2 requirement
Clinical uses of Ivabradine
- Chronic stable angina in patients who cannot take β-blockers
- Chronic HF with reduced Ejection fraction
Adverse effects of Ivabradine
Luminous phenomena/visual brightness HTN bradycardia
Adverse effects of quinidine
Cinchonism (headache, tinnitus with quinidine)
Adverse effects of procainamide
Reversible SLE-like syndrome (procainamide)
Adverse effects of disopyramide
HF (disopyramide)
Digoxin drug interactions
- verapamil
- amiodarone
- quinidine