Hydralazine↑ cGMP → smooth muscle relaxation. Vasodilates arterioles > veins; afterload reduction. Clinical use:- Severe hypertension (particularly acute)- HF (with NO)- Safe to use during pregnancy.- Frequently ...
HMG-CoA reductase inhibitorsLovastatin, pravastatin LDL ↓↓↓ HDL ↑Triglycerids ↓ Inhibit conversion of HMG-CoA to mevalonate, a cholesterol precursor; ↓ mortality in CAD patients. Side effects: - Hepatotoxicity (↑ ...
Bile acid resinsCholestyramine, colestipol, colesevelam LDL ↓↓HDL slightly ↑Triglycerides slightly ↑ Prevent intestinal reabsorption of bile acids; liver must use cholesterol to make more. Side effects: GI ...
EzetimibePrevents cholesterol absorption at the small intestine brush border by inhibiting the Niemann-Pick C1-like 1 (NPC1L1) transporter protein, which transports dietary cholesterol from the gastrointestinal ...
Antiarrhythmics - Class IaQuinidine, Procainamide, Disopyramide (The Queen proclaims Diso's pyramid) - ↑ AP duration, ↑ effective refractory period (ERP), ↑ QT interval, some potassium channel blocking effects. Clinical ...
Antiarrhythmics - Class IbLidocaine, Mexiletine (I'd buy Liddy's Mexican Tacos) - ↓ AP duration- Preferentially affect ischemic or depolarized Purkinje and ventricular tissue. - Phenytoin can also fall into the Ib category. ...
Antiarrhythmics - Class IcFlecainide, Propafenone (Can I have fries, please?) - Significantly prolongs ERP in AV node and accessory bypass tracts.- No effect on ERP in Purkinje and ventricular tissue.- Minimal effect on AP duration. ...
Antiarrhythmics - Class II (β-blockers)Metoprolol, propanolol, esmolol, atenolol, timolol, carvedilol - Decrease SA and AV nodal activity by ↓ cAMP, ↓ Ca2+ currents. Suppress abnormal pacemakers by ↓ slope of phase 4.- AV node particularly ...
Antiarrhythmics - Class IV (calcium channel blockers) ...Verapamil, diltiazem - ↓ conduction velocity, ↑ ERP, ↑ PR interval Use: Prevention of nodal arrhythmias (eg, SVT), rate control in atrial fibrillation. Adverse effects:- Constipation, flushing, ...
Magnesium- Antiarrhythmic Use:- Torsades de pointes (may be caused by class Ia and class III antiarrhythmias) - Effective in digoxin toxicity
AT-receptor blockersLosartan - block AT1 receptors - Same results as ACE-inhibitors on BP mechanisms
Renin inhibitorAliskiren - blocks formation of angiotensin I - same results as ACE-inhibitors on BP mechanisms
Nitroprusside- ↓ TPR via dilation of both arterioles and venules Use: hypertensive emergencies (used IV) Side effect:- cyanide toxicity
Minoxidil- Opens K+ channel, causing hyperpolarziation of smooth muscle - Results in arteriolar vasodilation Use:- Severe hypertension- slows hair loss Side effects:- hypertrichosis- Reflex tachycardia
Treatment of pulmonary hypertensionBosentan- Endothelin-IA-receptor antagonist- Side effects associated with vasodilation (headache, flushing, hypotension, etc)- Contraindication: pregnancy Sidenafil- Inhibits type V PDE- ↑ cGMP- Pulmonary ...
Wolff-Parkinson-White Syndrome therapy- arrhythmetics Ia or III (block accessory pathway) - Avoid digoxin, β-blocker, Ca2+ channel blockers, adenosin (slow AV conduction)
Nesiritide- recombinant form of B-type natriuretic peptide (BNP) - binds to natriuretic peptide receptors, thus ↑ cGMP, resulting in vasodilation - Used in acutely decompensated CHF
AdenosineAntiarrhymic Causes Gi-coupled decrease in cAMP.- ↑ K+ out of cells → hyperpolarizing the cell and ↓ ICa, decreasing AV node conduction.- ↓ SA and AV nodal activity- Affects phase 4 of the ...
NitratesNitroglycerin, isosorbide dinitrate, isosorbide mononitrate.- Nitroglycerin: sublingual, transdermal, IV- Isosorbide: oral, extended release for chronic use Vasodilate by ↑ NO in vascular smooth muscle ...
RanolazineInhibits the late phase of sodium current thereby reducing diastolic wall tension and oxygen consumption. Does not affect heart rate or contractility. Use: Angina refractory to other medical therapies. ...
Orlistat- Therapeutic use: weight loss - inhibits pancreatic lipase --> ↓ triglyceride breakdown in the intestine Side effects:- oily stools (steatorrhea)- diarrhea- ↓ absorption of lipid-soluble vitamins ...
Hypertensive emergencyTreat with clevidipine, fenoldopam, labetalol, nicardipine, or nitroprusside. Nitroprusside: Short acting; ↑ cGMP via direct release of NO. Can cause cyanide toxicity (releases cyanide). Fenoldopam: ...
MilrinoneSelective PDE-3 inhibitor. In cardiomyocytes: ↑ cAMP accumulation → ↑ Ca2+ influx → ↑ inotropy and chronotropy.In vascular smooth muscle: ↑ cAMP accumulation → inhibition of MLCK ...
PCSK9 inhibitorsAlirocumab, evolocumab LDL ↓↓↓HDL ↑Triglycerids ↓ Inactivation of LDL-receptor degradation, increasing amount of LDL removed from bloodstream Side effects: Myalgias, delirium, dementia, other ...
IvabradineSelective inhibition of funny sodium channels (If), prolonging slow depolarization phase 4.↓ SA node firing; negative chronotropic effect without inotropy. Reduces cardiac O2 requirement. Clinical use: ...
NeprylisinMetalloprotease that cleaves and inactivates endogenous peptides including natriuretic peptides (eg, BNP), glucagon, oxytocin and bradykinin. Inhibition of neprilysin leads to increased levels of endogenous ...
CilostazolPhosphodiesterase 3 inhibitor with therapeutic focus on cAMP. It inhibits platelet aggregation and widens arteries (direct arterial vasodilator). Use: Intermittent claudication in patients with peripheral ...
