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sooo many drugs
Cardio and peripheral NS drugs
| Trihexyphenidyl | M1 antagonist Tx parkinson's by blocking cholinergic so DA dominates | |
| Darifenacin | M3 antagonist Tx overactive bladder | |
| Fesoterodine | M3 antagonist Tx overactive bladder | |
| Tolterodine | M3 antagonist Tx overactive bladder | |
| Atropine | non-specific muscarinic antagonist Tx muscarine poisoning, long term eye dilation for iridocyclitis/lazy eye (7-14 days), dry out for intubation, anesthesia recovery (give with AntiChE to block GI contraction), prevent vagal contraction in GI surgery. | |
| Glyccopyrrolate | non-specific muscarinic antagonist Tx Anti-motility drug, dry out for intubation, anesthesia recovery (give with AntiChE to block GI contraction), prevent vagal contraction in GI surgery. | |
| Cyclopentolate | non-specific muscarinic antagonist Eye dilation (24 hrs) for pediactrics for refractive error. | |
| Ipratropium bromide | non-specific muscarinic antagonist aerosol for colds, COPD (use with beta2 agonists) | |
| Scopolamine | non-specific muscarinic antagonist; crossed BBB, CNS effects. Motion sickness patch, tranquilizer for surgery | |
| Tropicamide | non-specific muscarinic antagonist; Short term eye dilation. Also acts on cilliary muscles --> blurry vision | |
| Pralidoxime | Reactivates AChE bound by inhibitor; use as antidote for organophosphates | |
| Edrophonium | Anti-ChE; reverses in seconds, used in Dx of MG | |
| Neostigmine | Carbamate (Anti-AChE that reverses in minutes - 'stigmines') used with bethanechol for ileus and urinary bladder atony, Tx MG | |
| Pyridostigmine | Carbamate (Anti-AChE that reverses in minutes - 'stigmines') Tx MG | |
| Physostigmine | Carbamate (Anti-AChE that reverses in minutes - 'stigmines') Tx glycoma, crosses BBB | |
| Galantamine | non-carbamate AChE inhibitor Also: donepezil, tacrine, rivastigimine Tx for alzheimer's, crosses BBB | |
| Sarin | Nerve agent- AChE inhibitor. Sx = depolarized muscle block. Tx by ending exposure, inject atropine and pralidoxine (FAST) Experiences aging (can't be displaced!) Prophylactic tx with carbamate, gallantamine (reversible Anti-ACHE), and BuChE to scavan | |
| Soman | erve agent- AChE inhibitor. Sx = depolarized muscle block. Tx by ending exposure, inject atropine and pralidoxine (FAST) Experiences aging (can't be displaced!) Prophylactic tx with carbamate, gallantamine (reversible Anti-ACHE), and BuChE to scavange | |
| Tabun | erve agent- AChE inhibitor. Sx = depolarized muscle block. Tx by ending exposure, inject atropine and pralidoxine (FAST) Experiences aging (can't be displaced!) Prophylactic tx with carbamate, gallantamine (reversible Anti-ACHE), and BuChE to scavange | |
| VX | erve agent- AChE inhibitor. Sx = depolarized muscle block. Tx by ending exposure, inject atropine and pralidoxine (FAST) Experiences aging (can't be displaced!) Prophylactic tx with carbamate, gallantamine (reversible Anti-ACHE), and BuChE to scavange | |
| carbaryl | carbamate, insecticide (AChE inhibitor) | |
| diazinon | OP, insecticide (AChE inhibitor) | |
| malathion | OP, insecticide (AChE inhibitor); more effective in insects. eliminated quickly in mammals. Converted to maloxon in insects | |
| parathion | OP, insecticide (AChE inhibitor) TOXIC.Coverted to paraoxon in mammals. | |
| Reserpine | Sympatholytic. Monoamine storage blocker. Irreversibly blocks VMAT. Vesicles slowly depleted of NE, DA, 5HT. USES: anti-hypertensive, high dose tranquillizer ADE: psychodepression, exacerbate Parkinson's | |
| Clonidine | Sympatholytic (paradoxically). Alpha2 agonist in the vasomotor center of brain stem -> reduces NE firing. no activation needed, very potent. ADE: drowsy, dry mouth, WITHDRAWAL REBOUND USES: lower BP, opioid withdrawal, anesthetic adjunct, stim GH rel | |
| Methyldopa | Central alpha2 agonist - sympatholytic Activated to methylNE so need larger doses than clonidine, short half life. ** FIRST LINE ANTIHYPERTENSIVE IN PREGNANCY | |
| Alpha 1 blockers | "-osin" Parzosin, Terazosin, Tamsulosin Tx primary hypertension, prostatic hyperplasia, kidney stones. Less postural fall in BP but - 'first dose phenomenon" so give at night. Avoid in elderly. ADE: delayed ejac, priapism, dry mouth, nasal congestion,I | |
| Beta Blockers generations | "olol" = just beta block Begins with N-Z then is 1st generation (non-selective) Begins with A-M then is 2nd generation (beta1) "ilol" or "alol" = 3rd generation - beta block and alpha block. | |
| Beta Blockers USES | Myocardial ischemia, dysrhythmias, Post-infarction, Hyperthyroidism (because thyroid upregs beta receptors), essential hypertension (not first line), HF (long term, low dose), glaucoma (reduces inflow) | |
| Beta Blockers ADE | Decrease exercise capacity, bradycardia, difficult to lose weight, Make AV block and HF worse acutely. Reflex vasoconstriction --> cold extremities, Withdrawal excess (upreg of beta receptors), anaphylactic shock - BAD b/c epi doesn't work as well. | |
| Beta Blockers: Effect of beta 2 block - 2 | Vasoconstriction, bronchoconstriction, REDUCE TREMOR, slow recovery from hypoglycemia, block K+ uptake into muscles --> hyperkalemia, distabilize mast cells. | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Propranolol - 2 | Gen 1 beta 1/2 blocker. Not a partial agonist. Metabolized in liver (dose varies) Used for migraines/liver problem | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Timolol - 2 | Non-irritant gen 1 beta blocker. Used in eye drops for glaucoma | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Esmolol - 2 | 2nd gen beta 1 blocker. Avoids beta 2 asthma exacerbation | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Metoprolol - 2 | 2nd gen beta 1 blocker. Avoids beta 2 asthma exacerbation. Documented benefit in HF | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Bisprolol - 2 | 2nd gen beta 1 blocker. Avoids beta 2 asthma exacerbation. Documented benefit in HF | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Atenolol - 2 | 2nd gen beta 1 blocker. Avoids beta 2 asthma exacerbation. | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Carvedilol - 2 | Beta 1,2, and alpha1 blocker. Documented benefit in HF | Beta blocker uses: 1. Reduce mortality after MI 2. Arrythmias (slow afib, aflutter,and VT storm) 3. essential HTN 4. Hyperthyroidism (with up regulated beta receptors) 5. HF - long term 6. glaucoma (decrease inflow) |
| Labetalol | alpha 1/beta 1,2 blocker Used acutely to manage Ca secreting tumors. | |
| Action of direct vasodilators/ arteriodilators | Decreases afterload. Non-postural decrease in BP. High LV filling pressure. But - drop BP stims sympathetic reflex that increases HR and salt retention. ("PSUEDOTOLERENCE") COMBINE WITH BETA BLOCKERS, SYMPATHOLYTICS, or DIURETICs, good for weak pump. | |
| Hydralazine | Arteriodilator, good for weak pump (with sympatholytic or diuretic), met in liver (test for slow acetylaters), potent antioxidant, protects from nitrate tolerance. ADE: lupus like syndrome CAN CAUSE PERICARDITIS | |
| Diazoxide | K-ATP channel opener: Arteriodilator; decreases insulin release; Tx sulonylurea overdose, and hyperinsulinemic hypoglycemia of infant (LOF mut of Katp) | |
| Minoxidil | Potent vasodilator. Last resort for pts refractory to other antihypertensives. activated in liver. NEED TO GIVE WITH LOOP DIURETIC ADE: hypertrichosis (hair growth) | |
| Action of venodilators | Decreases preload. Postural fall in BP. Lowers LV filling pressure. Decreases cardiac work and pulmonary BP. GOOD FOR: pulmonary congestion, MI | |
| Isosorbide dinitrate and isorbide mononitrate | Organic nitrate - venodilator. long half life. Metabolized in liver. Sublingual, oral (worry about tolerance) 9-12 hour break ever 24 hrs. | |
| Organic nitrates action and ADE (isosorbide dinitrate, nitroglycerine) | Relax venous and coronary artery SM but NOT resistance vessels by releasing NO. ADE: HA, posture hypotension TOLERANCE: long term exposure --> oxidative stress --> endothelial disfunction, mito disfunction, etc. - Tx with antioxidants (folate, ascorbat | |
| Nitroglycerine | Organic nitrate. activated by ALDH2 --> nitrite --> NO. pts with Asian glow -> ALDH2 disfunction. Tolerance from ALDH2 inactivation USE: prinzemetal's angina, angina. Sublingually, transdermal patch/paste, IV (actue HF with pulm congestion). | |
| Sodium Nitroprusside | General vasodilator. Relax VEINS, CORONARY ARTERIES, AND RESISTANCE VESSELS. Releases NO into blood IV in hypertensive emergencies. moment-to-moment control of BP. Good for aortic stensis, mitral valve reg. ADE:limit duration because of toxic thiocyana | |
| Sildenafil | Viagra: Phosphodiesterase-5-inhibitor (blocks cGMP break down) Erection is parasympathetic -> increase cGMP --> NO release. DON'T USE NITROVASODILATORS UNTIL 24 HOURS AFTER DOSE | |
| Tadalafil | 17 hour half life. Phosphodiesterase-5-inhibitor (blocks cGMP break down) Erection is parasympathetic -> increase cGMP --> NO release. DON'T USE NITROVASODILATORS UNTIL 48 HOURS AFTER DOSE | |
| Ca Channel blockers mechanism: dihydropyridines and nondihydropyridines | SELECTIVE ARTERIODILATORS. Potent vasodilators. Used in HT, angina, arrhythmias, Raynaud’s. Directly reduce HR, contractility; No retention of Na/water so may not need diuretics. Cav1.2 and Cav1.3 of pore forming unit - high affinity. | |
| Amlodipine | DIHYDROPYRIDINE CA CHANNEL BLOCKER - voltage dependent- vascular dependent. binds to tissue w/ sustained depolarization. Long halflife so Sympathetic reflex rare. Weak diuretic. Combine with betablock for MI. Tx; HT, angina, arrhythmias, Raynaud’s | |
| Nicardipine, Nifedipine | DIHYDROPYRIDINE CA CHANNEL BLOCKER - voltage dependent- vascular dependent. binds to tissue w/ sustained depolarization. Long halflife so Sympathetic reflex rare. Weak diuretic. Combine with betablock for MI. Tx; HT, angina, arrhythmias, Raynaud’s | |
| nondihydropyridines Verapamil, diltiazem | "non = not the pines, no betablockers" Frequency dependent binding Ca channel blocker. Cardio selective. Potent cardiodeppressors and effective vasodilators. DON'T USE WITH BETA BLOCKER. NOT GOOD WITH DEPRESSED CF. Tx; HT, angina, arrhythmias, Raynaud’s | |
| Verapamil | "non = not the pines, no betablockers" nondihydropyridine Ca channel blocker. Cardio selective. Potent cardiodeppressors and effective vasodilators. DON'T USE WITH BETA BLOCKER. NOT GOOD WITH DEPRESSED CF. Tx; HT, angina, arrhythmias, Raynaud’s | |
| Diltiazem | "non = not the pines, no betablockers" nondihydropyridine Ca channel blocker. Cardio selective. Potent cardiodeppressors and effective vasodilators. DON'T USE WITH BETA BLOCKER. NOT GOOD WITH DEPRESSED CF. Tx; HT, angina, arrhythmias, Raynaud’s | |
| Angiotensin II functions | vasoconstriction, enhances sympathetics (rapid), Na/water absoprtion, K secretion (slow), promotes remodeling. | |
| Renin-angiotensin inhibitors (Uses, ADE) | USES: HF (inhibit remodeling, renal function is preserved with diabetes), Antihypertensive Adverse effects: dizzy, hypotension, hyper-K, renal failure with renal artery stenosis, teratogenic! | |
| ACE inhibitors | "prils" - blocks AII formation (AII= vasoconstrictive & pro-proliferative); ACE also breaks down bradykinin (vasodilator) EFFECT: HIGH RENIN, LOW AII, aldosterone slowly FALLS, but AII may escape long term. ADE: dry cough, angioedema (bradykinin) | |
| Captopril | ACEI, short half life. Renal excretion. | |
| Lisinopril | ACEI | |
| Enalapril | Prodrug ACEI, renal excretion | |
| Enalaprilat injectable | ACEI for hypertensive emergencies. | |
| Spironolactone | Aldosterone receptor blocker K sparing diuretic. Aldosterone increases Na retention, K excretion; is regulated by AII, K+ and corticotropin. ADE: fibrosis of vessels, hyperK. Acts at other steroidal receptors --> bad effects. USE: HF with ACEI, post | |
| Eplerenone | Aldosterone receptor blocker K sparing diuretic. Aldosterone increases Na retention, K excretion; is regulated by AII, K+ and corticotropin. ADE: fibrosis of vessels, hyperK. Acts only on aldosterone R. USE: HF with ACEI, postMI. | |
| Angiotensin II receptor blockers (ARBs) | "Sartan" Blocks AT1 receptors (which cause vasoconstriction, aldosterone release, remodeling, NE release) HIGH RENIN, HIGH AI, AII. AT2 receptors (vasodilating, antiproliferative) not blocked. ADE: plaque rupture, adverse vasculature remodeling. | |
| Candesartan | ARB | |
| Losartan | ARB | |
| Valsartan | ARB | |
| Aliskiren | Renin inhibitor; Blocks the production of Angiotensin I by renin. | |
| Digoxin | ONLY oral inotrope, ^vagal,decr sym tone. USE: lower HR in AFIB, decr hosp in HF. X give with hypokalemia (^binding-^Ca-^arrhyth) Inhib Na/K->^Na->Na/Ca exch->^Ca-> ^contraction. ADE: slow HR, toxic arrhythmia (DAD), hypoK, yellow/green halos. | |
| Dobutamine | IV only. Inotrope. Beta agonist. Increase contractility, relaxation, HR. 1. pharmacological stress test 2. Acute inotrope in HF (better than dopamine. doesn't increase NE release --> no alpha effect. 3. circulatory shock ADE: arrhythmias. | |
| Dopamine | Inotrope and pressor. IV only Vasodilates kidney/GI inhibiting Na reabsoption. medium dose: increase CO, still helps kidneys high dose: dopamine can act on beta1 receptors, NE release --> alpha constriction. ADE: arrhythmias. GOOD FOR SHOCK, acute H | |
| Milrinone | Inotrope - IV only phosphodiesterase III inhibitor prevents CAMP breakdown --> increase contraction. Don't do bolus because drops BP quickly! ADE: arrythmias | |
| ANP, BNP | released by the heart with increased stretch. Increases Na excretion. High levels in severe HF. BNP is biomarker for MI, HF | |
| Nesiritide | recominant human BNP. hort term reduction of dyspnea in severe acute HF. Not long term. | |
| How do you treat Atrial flutter? | 1. if >48 hrs --> anticoagulate for 2+ weeks 2. Control ventricular rate (Ca channel block, beta block 3. Class III anti-K to convert to sinus rhythm 4. Ablation (tricuspid to IVC) | |
| How do you treat Atrial Fibrillation acutely | 1. Anticoagulant 2. Control ventricular rate (beta block, CA channel block, digoxin) 3. If still symptomatic and NO HEART DZ --> class 1c or class III antiarrythmics can be tried. With decreased LV fxn --> class III. | |
| How do you treat AFIB long term? | Long term: if asymptomatic - rate control. Can't control rate --> ablation (AV node with permanent pace, pulmonary veins, or MAZE procedure in serious cases) | |
| Antiarrhythmics uses, ADE | USE: aflutter, afib if still symptomatic, reduces shocks in pts with ICDs | |
| How do you treat AVNRT (AV node reentry tach)or AVRT (AV node reciprocating tach - WPW) | VAVA 1. valsalva 2. adenosine - activates K flow, heart stops then normal sinus rhythm. broncospasm. 3. OR Verapramil (Ca Channel blocker) - used in asthmatics. 4. Ablation Long term: block AV node (beta blockers, CCB, ablation, NO ANTIARRYTHMICS!) | |
| How do you treat STABLE wide complex tachycardia acutely? | 1. Amiodarone (class III, 1st line) 2. procainamide (1A) 3. Lidocaine (1B) 4. Magnesium - polymorphic VT, very few downsides. Shortens QT. 5. Betablockers - esp VT storm | |
| How do you treat STABLE wide complex tachycardia chronically? | If no structural heart disease --> ablation of pt source Otherwsie - ICD! Give ICDs if there is low EF. | |
| Procainamide | Class 1A antiarrythmic: Na channel blocker. Reduces excitability in non-nodal tissues. 1A: also blocks K channels so increases QT interval. PROARRYTHMIC used only acutely. NOT FOR PTS WITH STRUCTURAL HEART DISEASE Can cause pericarditis! | |
| Quinidine | Class 1A antiarrythmic: Na channel blocker. Reduces excitability in non-nodal tissues. 1A: also blocks K channels so increases QT interval. PROARRYTHMIC used only acutely. NOT FOR PTS WITH STRUCTURAL HEART DISEASE | |
| Disopyramide | Class 1A antiarrythmic: Na channel blocker. Reduces excitability in non-nodal tissues. 1A: also blocks K channels so increases QT interval. PROARRYTHMIC used only acutely. NOT FOR PTS WITH STRUCTURAL HEART DISEASE | |
| Lidocaine | Class 1B antiarrythmic: Na channel blocker. Reduces excitability in non-nodal tissues. 1B: DECREASES AP duration and QT interval. USES: VT acutely, digatalis toxic arythmias. | |
| Flecainide | Class 1C antiarrythmic: Na channel blocker. Reduces excitability in non-nodal tissues. 1A: AP duration unaffected NOT FOR PTS WITH STRUCTURAL HEART DISEASE | |
| Class II antiarrythmics | Beta blockers Acebutolol, esmolol, metoprolol. More effective with exercise. WIDELY used. decreases rate during Afib, Afluter, used in VT, SVT | |
| Amiodarone -2 | Class III antiarrythmic K+ channel blocker with class, 1-4 properties. Increases refractory pd, prolong QT. | ADE:long QT syndrom and torsade, Low HR, increases defib threshold, hypo/hyperthroid, fibrosis lungs. Monitor thyroid. give fluids; L-threo-3,4-dihydroxyphenylserine (L-DOPS), has TWEEN as detergent and therefore had ADR of hypotension |
| Dofetilide | Class III antiarrythmic K+ channel blocker Increases refractory pd, prolong QT. ADE:long QT syndrom and torsade | |
| Sotalol | Class III antiarrythmic K+ channel blocker and beta blocker Increases refractory pd, prolong QT. ADE:long QT syndrom and torsade | |
| Class IV antiarrythmics | Verapamil, diltiazem Ca channel blocker. More effect with exercise because blocks adrenergic input. Blocks AV/SA node. WIDELY used. | |
| Lovastatin | Red yeast rice Statin - LOWERS LDL- Inhibits HMG coA reductase production of chol, decrease LDLR.Increase endothelial fxn, plaque stabilizer, decrease oxidative stress, inflammation. ADE: liver, muscle pain, TERATOGENIC, polyneuropaty, P450 interaction | |
| Pravastatin | NOT CYP450 metabolized, water sol. Statin - LOWERS LDL- Inhibits HMG coA reductase production of chol, decrease LDLR.Increase endothelial fxn, plaque stabilizer, decrease oxidative stress, inflammation. ADE: liver, muscle pain, TERATOGENIC, polyneuropa | |
| Atorvastatin | Synthetic Statin - LOWERS LDL- Inhibits HMG coA reductase production of chol, decrease LDLR.Increase endothelial fxn, plaque stabilizer, decrease oxidative stress, inflammation. ADE: liver, muscle pain, TERATOGENIC, polyneuropaty, P450 interactions | |
| Rosovustatin | Statin - LOWERS LDL- Inhibits HMG coA reductase production of chol, decrease LDLR.Increase endothelial fxn, plaque stabilizer, decrease oxidative stress, inflammation. ADE: liver, muscle pain, TERATOGENIC, polyneuropaty, P450 interactions | |
| Cholestyramine | Bile Acid Binding resin. bind bile acids and secreted in feces. Give with statins so liver cant make LDL and has to upreg LDLRs. HORSE PILL/gross liquid. Give to lower LDL after statins. ADE: GI, bind acidic substances like vitamins and drugs. | |
| Niacin (extended release) | Nicotinic Acid. INCREASE HDL. B vit -> nicotinamide. Give large dose, decre lipolysis and FFA. Less liver TG synthesis. VLDL decr, some LDL decr, some lipoprotein A decre ADE: hyperglycemia, PG flush, GI. X ingout, peptic ulcer, liver disease, diabetes | |
| Fibrates | Gemfibrozil, Fenofibrate LOWER TG. Acts at PPAR receptor (FA sensor) -> RXR dimer --> gene transcribed --> incr breakdown TG (down reg VLDL and up reg lipoprotein lipase), increase oxidation of FFA in liver, increase HDL. | |
| Unfractionated Heparin (USE/ADE, mech - 2 slides) | ANTICOAGULANT. Tx: DVT, PE, MI, ischemic stroke (DO CT FIRST). IV or subQ (prophylaxis) Monitor aPTT. ADE: BLEEDING, HIT or HIT with thrombosis (clots everywhere) - tx with direct thrombin inhibitor. PREGNANCY SAFE. MONITOR aPTT | binds antithrombin cofactor. dose dep half life (shorter with PE, longer with renal disease), binds to macrophages, acute phase reactants - levels differ with disease. MONITOR aPTT. Works at clot bound thrombin (IIa) & factor X |
| Enoxaparin | Low molecular weight heparin USE: DVT, PE, MI, ischemic stroke Activate antithrombin. Fewer petasaccharids, works better against Xa, MORE PREDICATABLE, less binding to proteins. Don't have to monitor. SAFE IN PREGNANCY ADE: bleeding, some HI | |
| Warfarin (use/ADE, mech) 2 slides | Use: AFIB anticoag, VTE, PE, prosthetic valves, ischemic stroke, low EF (maybe). 99% bound to albumin. MANY drug interactions. ADE: bleeding, severe skin reaction, X in pregnancy! MEASURE INR to see if working ONCE A DAY Tx. | Works against vit K dependent clotting factors (II, VII, IX, X, C, S, Z from liver). prevents v.K reduction. Doesn't block existing clotting factors so takes 3-5 days to work. Can test for genes to choose dose, but most just start low. Met by cyt2C9. |
| Bivalirudin (use/ADE, mech) 2 slides | ANTICOAGULANT Direct thrombin inhibitor IV only, short half life. Tx: HIT, mainly in cath lab during PCI. ADE: bleeding, monitor with ACT (active clotting time) | Inactivates soluble and fibrin bound thrombin. blocks catalytic site and fibrin binding site. also inactivates some intrinsic coag factors. inhibits platelet agg. |
| Dabigatran(use/ADE, mech) 2 slides | ANTICOAGULANT Direct Thrombin inhibitor One drug interaction: rifampin (decreases bioavailibility). May have life threatening bleeds - new drug | Works on factor II. Inhibits free and clot bound thrombin. inhibits thrombin induced platelet agg. 2ce a day. Don't have to monitor INRs. renal excretion. |
| Difference between red and white thrombus? (2 slides) | Red thrombus: coagulation system (thrombin, fibrin, plasmin, RBCs) - in VENOUS clots (DVTs, PE, AFIB, ischemic stroke) - tx with ANTICOAGULANTS | White thrombus: platelet mediated, arterial clots. |
| When to use thrombolytics | Use in LARGE thromboembolism, STEMI, ischemic stroke (check CT), interventional radiology. DO NOT USE IN NSTEMI OR UNSTABLE ANGINA.or if recent surgery, bleeding, stroke, aortic dissection, pericarditis, HTN. ADE: bleeding | |
| Alteplase (tPA) | 'plase'=tPA Thrombolytic. Tissue plasminogen activator (turns plasminogen to plasmin to break clots) Clot specific drug. Complicated infusion regiment | |
| Reteplase (tPA) | 'plase'=tPA Thrombolytic. Clot specific drug. recombinant tPA (turns plasminogen to plasmin to break clots) . longer half life, just 2 IV boluses | |
| Tenecteplast (tPA) | 'plase'=tPA Thrombolytic Clot specific drug. (turns plasminogen to plasmin to break clots) ONE dose, but is weight based so hard to use in ER. | |
| Streptokinase | Thrombolytic: works on fibrin everywhere. Only used in Europe. Need loading doses to counter Abs and some are allergic or have febrile rxns. Activates plasmin to break clots. | |
| Aspirin (Acetyl Salicylic Acid) | USES: primary prevention of cardiac dz, stable angina, acute MI, after CABG to maintain vessel potency, decrease strokes in pts with stroke Hx. Allergy: wheezing ADE: GI(give PPI), drug interaction Permanent for platelet life. blocks COX so no TxA, PGI | |
| Dipyridamole | ANTIPLATLET In pts who had strokes and pts with mechanical valves to prevent strokes. CNS/GI effects, not well tolerated. Blocks phosphodiesterase which breaks down cAMP in platelets. Inhibits TxA1 formation | |
| Clopidogrel (2 cards) | ANTIPLATLET adenosine (ADP) receptor (P2Y12R) antagonist. ADP binding activates GP 2b3a. Two activations by CYP2C19. dose dependent inhibition. irreversible so wait 7-10 days for surgery. | Used after stent to reduce in stent thrombus,reduce risk in CAD,cerebral vascular dz and peripheral vascular dz. Side effects - not bad, rash, GI. Can use PPI to reduce GI bleeds |
| Prasugrel | ANTIPLATLET adenosine (ADP) receptor (P2Y12R) antagonist. ADP binding activates GP 2b3a. One Cyp450 activation only. Irreversibly bind. accumulates in ESRD. Good at preventing death but more bleeds than clopidogrel. x in pts with stroke hx, >70, <60kg. | |
| Ticagrelor | New ANTIPLATLET drug adenosine (ADP) receptor (P2Y12R) antagonist. doesn't need activation. 7-8 hr half life. | |
| Abciximab (two slides | Most potent ANTIPLATELET Glycoprotein IIIb/IIA inhibitor Expensive, irreversible, platelet effect only for 24 hrs. Binds activated and non-activated platelets. Prevents binding of fibrinogen and vWF. USUALLY ONLY STEMI IN CATH LAB | All glycoprotein IIIB/IIA inhibitors: ADE: bleeding, thrombocytopenia (monitor!), CNS hemorrhage rarely. Used in STEMI, and NSTEMI/unstable angina only if they still have pain. Mainly used in cath lab. |
| Eptifibatide - two slides | Most potent ANTIPLATELET Glycoprotein IIIb/IIA inhibitor Short half life. NOT USED FOR STEMI, used for NSTEMI and PCI. | All glycoprotein IIIB/IIA inhibitors: ADE: bleeding, thrombocytopenia (monitor!), CNS hemorrhage rarely. Used in STEMI, and NSTEMI/unstable angina only if they still have pain. Mainly used in cath lab. |
| Tirofiban | Most potent ANTIPLATELET Glycoprotein IIIb/IIA inhibitor Not used. | |
| Prostaglandin E1 | Used to keep patent ductus arteriosus in pt with transposition of great vessels. | |
| Ranolazine | Novel antianginal drug. Inhibits late Na current. used if others don't work. | |
| Phenoxybenzamine - 2 cards | Alpha 1 & 2 blocker. irreversible Tx Ca secreting tumors (alpha blockers 1st then beta blocker) or acute hypertensive crisis, not for primary HTN because of postural fall in BP. ADE: dizzy on standing, palpitations from alpha2/NE | Remember: alpha1 block -> vasodilate, relax iris and GU muscles, risk of priatism alpha2 block -> increase NE release |
| Phentolamine - 2 cards | Alpha 1 & 2 blocker. competitive, short term ER injection Tx Ca secreting tumors (alpha blockers 1st then beta blocker) or acute hypertensive crisis, not for primary HTN because of postural fall in BP. ADE: dizzy on standing, palpitations from alpha2/N | alpha1 block -> vasodilate, relax iris and GU muscles, risk of priatism alpha2 block -> increase NE release |
| Prazosin - 2 cards | Alpha 1 blocker "osin" Short half life, drop BP. "First dose phenomenon" drop in BP - give at night, not to elderly; Tx; HTN, kidney stones, prostatic hyperplasia ADE: delayed ejaculation, +erection, dry mouth, nasal congestion, IFIS | alpha1 block -> vasodilate, relax iris and GU muscles, risk of priatism alpha2 block -> increase NE release |
| Terazosin - 2 cards | Alpha 1 blocker "osin" Short half life, drop BP. "First dose phenomenon" drop in BP - give at night, not to elderly; Tx; HTN, kidney stones, prostatic hyperplasia ADE: delayed ejaculation, +erection, dry mouth, nasal congestion, IFIS | alpha1 block -> vasodilate, relax iris and GU muscles, risk of priatism alpha2 block -> increase NE release |
| Tamsulosin - 2 cards | Alpha 1 blocker "osin" Short half life, drop BP. "First dose phenomenon" drop in BP - give at night, not to elderly; Tx; HTN, kidney stones, prostatic hyperplasia ADE: delayed ejaculation, +erection, dry mouth, nasal congestion, IFIS | alpha1 block -> vasodilate, relax iris and GU muscles, risk of priatism alpha2 block -> increase NE release |
| Yohimbine - 2 cards | Alpha 2 blocker Increase NE release and outflow from CNS! Tx - sympathetic insufficiency and disautonomias (ex. pts who overexpress alpha2R --> too little insulin --> diabetes) ADE: palpitations, incr GI motility | alpha1 block -> vasodilate, relax iris and GU muscles, risk of priatism alpha2 block -> increase NE release |
| Zileuton | 5-LOX inhibitor (lipoxygenase) Blocks generation pathway of LT. Does not block action of existing LT. Tx for asthma. X in breastfeeding, hepatic disease, pregnancy, regular ROH consumption | |
| Zafirlukast | CysLT1 Receptor blocker Antagonist of LTD4. Can REVERSE loss of airway conduction. Tx for asthma ADE: abd pain, dizziness, HA, rhinitis, ST | |
| Glucocorticoid inhaler | Tx of asthma Blocks AA production upstream of LT generation. | |
| Montelukast | CysLT1 Receptor blocker Antagonist of LTD4. Can REVERSE loss of airway conduction. Tx for asthma ADE: abd pain, dizziness, HA, rhinitis, ST | |
| Cromolyn Na and Nedocromil Na | URT and Asthma tx Prophylactic, not well understood | |
| Diphenhydramine - 2 | Benadryl early 1st generation antihistamine - SEDATIVE, ANTI-MUSCARINIC Tx Motion sickness, nausia X in benign prostatic hypertrophy, glaucoma | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Dimenhydrinate - 2 | Dramamine early 1st generation antihistamine - SEDATIVE, ANTI-MUSCARINIC Tx Motion sickness, nausia | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Promethazine -2 | Early 1st generation antihistamine Inj only in ER, sedative, anti-muscarinic Tx nausia | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Hydroxyzine - 2 | early 1st generation antihistamine - SEDATIVE, used as opioid adjunct in OR. | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Cyclizine/meclizine -2 | Marezine/Bonine Late 1st generation antihistamine - LESS SEDATIVE, shorter half life. Not anti-muscarinic Tx Motion sickness | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Chlorpheniramine/brompheniramine -2 | chlortrimeton/dimatapp Late 1st generation antihistamine - Anti muscarinic, LESS SEDATIVE, shorter half life. | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Cetirizine -2 | Zyrtec 2nd generation antihistamine Least sedation, no CNS effect, less lipophilic. longer half life. not antimuscarinic Tx: allergies, hay fever, etc. | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Desloratidine/Loratidine -2 | Clarinex/Claritin 2nd generation antihistamine Least sedation, no CNS effect, less lipophilic. longer half life. not antimuscarinic Tx: allergies, hay fever, etc. | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Fexofenadine -2 | Allegra 2nd generation antihistamine Least sedation, no CNS effect, less lipophilic. longer half life. not antimuscarinic Tx: allergies, hay fever, etc. | Antihistamines: reversible, competative antagonists, often with antimuscarinic effects and anesthetic effects (similar in structure) |
| Cocaine - 2 | NE/DA uptake inhibitor Blocks NET (high affinity reuptake) Used in Dx of horner's syndrome. | Systemic use: ADE:increase BP, HR, can cause MI/ischemia/arrythmia Chronic-> HF from hypertrophy/dilatation, early ahtrosclerosis, contraction band necrosis, hypothermia, kidney damage from myoglocin leak from SK muscles. |
| Amphetamine | NE releaser - non-vesicular release by NET. Tolerance with long use. Psychostimulent. Tx: ADHD, narcolepsy | |
| Ephedrine/pseudoephedrine | NE releaser - non-vesicular release by NET. Tolerance with long use. ALSO weakly stim beta2 receptors to relax SM. Tx: decongestant, vasopressor, tx urinary incontinence | |
| Hydroxyamphetamine | NE releaser - non-vesicular release by NET. Tolerance with long use. Dx in horner's syndrom. If this dilates both eyes, then 3rd order neuron is fine! | |
| Methamphetamine | NE releaser - non-vesicular release by NET. Tolerance with long use. METH - psychostimulent | |
| Tyramine | NE releaser - non-vesicular release by NET. Found in aged foods, broken down by MAO in the liver. With MAOIs there is a lot of NE in the cytoplasm, so tyramine/releasers --> massive NE release--> hypertensive crisis. | |
| Phenylephrine | alpha 1 agonists Vasoconstrictor Nasal decongestant, vasopressor, and PUPIL DILATOR | |
| Brimonidine | Alpha 2 agonists Tx glaucoma. Increases the permiability of BV so increases absorption | |
| apraclonidine | Alpha 2 agonists Tx glaucoma. Increases the permiability of BV so increases absorption | |
| Clonidine | Alpha 2 agonists Decreases NE firing CENTRALLY, sympatholytic. Very potent. Used to decrease BP, opioid withdrawal, as an anesthetic adjunct, stim GH release. ADE: drowsiness, dry mouth, withdrawal rebound (if stop, sudden rise in sympathetic tone) | |
| methyldopa | Alpha 2 agonists Activated to methyNE. Decreases NE firing CENTRALLY, sympatholytic. Very potent. 1st line anti-HTN in pregnancy | |
| Fenoldopam | Selective D1 agonist. Short term tx of severe hypotension IV. | |
| Albuterol - 2 | SABA (short acting beta2 agonist) resistant to COMT/MAO, slower uptake. Partial agonist Asthma tx (1st line) | All asthma beta agonists - regulates mast cells, bronchodilate, ADR: tremor, tachycardia, low BP, hypoglycemia, hypokalemia, tolerance. |
| Formoterol - 2 | LABA (Long acting beta2 agonist)- fast acting Must combine with glucocorticoid inhaler or increases severity of rxns. FULL agonist, Asthma tx. | All asthma beta agonists - regulates mast cells, bronchodilate, ADR: tremor, tachycardia, low BP, hypoglycemia, hypokalemia, tolerance. |
| Salmeterol - 2 | LABA (Long acting beta2 agonist) - slower acting Must combine with glucocorticoid inhaler or increases severity of rxns. Partial agonist, Asthma tx. | All asthma beta agonists - regulates mast cells, bronchodilate, ADR: tremor, tachycardia, low BP, hypoglycemia, hypokalemia, tolerance. |
| Ritodrine | Beta agonist: tocolytic (delays preterm labor) | |
| What are 5-HT agonists and what do they cause? | amphetamine derivatives, ergot derivatives, MDMA, DA agonists, etc Can cause valvulopathy by activating 5HT 2B receptors - thickening of the heart and causing regurgitation! | |
| Ergonovine | alpha 1 partial agonist Vasoconstriction, to prevent postpartum hemorrhage | |
| Ergotamine | alpha 1 partial agonist Abort migratory headaches prophylactically. | |
| Botulinum toxin | local muscle relaxant and used to tx crossedeyes. works by preventing the docking of NT vesicles! Abobotulinum toxin A Onabotulinum toxin A (botox) - blocks tSNARE SNAP 25 Rimabotulinum Toxin B - blocks the vSNARE: VAMP | |
| What are aminoglycosides effect on the peripheral nervous system? | Amikacin, gentamicin, kanamycin Disrupt cholinergic transmission. Blocks Ca2+ transport in presynaptic terminals of nicotinic neurons Abx like neomycin, and tetracylines also block cholinergic transmission. | |
| Acetylcholine - 2 | Cholinergic agonist Binds muscarinic and nicotinic receptors. | Muscarinic agonists are generally used for: 1. increasing GI activity 2. increasing bladder activity 3. via M3R - constrict in the eye (glaucoma or after cateract surgery) 4. Tx xerostromia (dry mouth) |
| Bethanechol- 2 | Muscarinic agonist AChE resistant Use for increased GI motility, to tx urinary retension, and eye constriction (glaucoma) | Muscarinic agonists X use in astma, hyperthyroid (afib), coronary insufficiency, peptic ulcer (increased seretion), mechanical obstruction in GI, peritonitis |
| Pilocarpine-2 | Muscarinic agonist ONLY ONE THAT IS UNCHARGED and can cross the BBB. Used in glaucoma and for dry mouth (xerostomia) | Cholinergic agonists are generally used for: 1. increasing GI activity 2. increasing bladder activity 3. via M3R - constrict in the eye (glaucoma or after cateract surgery) 4. Tx xerostromia (dry mouth) |
| Carbamylcholine (carbachol)-2 | N>M cholinergic agonist Use for increased GI motility, to tx urinary retension, and eye constriction (glaucoma) | Muscarinic agonists X use in astma, hyperthyroid (afib), coronary insufficiency, peptic ulcer (increased seretion), mechanical obstruction in GI, peritonitis |
| d-tubocurarine | Nicotinic cholinergic antagonist (skeletal muscle relaxant) NON-DEPOLARIZING, Competative inhibitor. More sensitive: babies, MG pt, hypokalemia (hyperpolarization) Side effects: increased histamine release, autonomic ganglionic block | |
| Atracurium- 2 | Nicotinic cholinergic antagonist (skeletal muscle relaxant) NON-DEPOLARIZING, Competative inhibitor. DEGRADED BY HOFFMAN ELIM (can use with dmage to circulatory system or liver) | Non-depolarizing inhibitors: More sensitive: babies, MG pt, hypokalemia (hyperpolarization) Side effects: increased histamine release, autonomic ganglionic block |
| Mivacurium- 2 | Nicotinic cholinergic antagonist (skeletal muscle relaxant) NON-DEPOLARIZING, Competative inhibitor. Fast acting. Degraded by esterase. | Non-depolarizing inhibitors: More sensitive: babies, MG pt, hypokalemia (hyperpolarization) Side effects: increased histamine release, autonomic ganglionic block |
| SuccinylCholine -2 | Nicotinic cholinergic antagonist (skeletal muscle relaxant) DEPOLARIZING inhibitor. Low levels of channel activation --> Na channels inactivate increasing threshold. "dual block' after hours when AChR/SCh change and can't respond 2 agonist Tx: intubat | Degraded by BuChE ADE: histamine release, increase intraoccular pressure, malignant hyperthermia (tx with dantrolene) hypothermia - more sensitive |
| Varenicline | Central nicotinic antagonist Help stop smoking Partial agonist of nAChR. high concentration blocks. low concentration activates. | |
| Bupropion | Central nicotinic anagonist Stop smoking cravings Blocks AChRalpha7. Is also a weak DA, NE uptake inhibitors. Reduces craving | |
| Epinephrine - 2 | Sympathomimetics USES: anaphylactic shock Cardiac arrest (last ditch to get blood to brain and heart) Vassopressor Decongestant Localizer of anestheti | Low conc - dilate (B2 dominates) High conc - constric (alpha dominates - like NE) ADE:HA,palpitations |
| Dipivalylepinephrine - 2 | Sympathomimetics - broken into epi. low dose, lipid soluble. Reduces systemic side effects, but doesn't help with reactive hyperemia (when put in eyes). Poor midratic. Unreliable except in horner's syndrome. | USE anaphylactic shock Cardiac arrest (last ditch) Vassopressor Decongestant Localizer of anestheti Low conc - dilate (B2) High conc - constrict (alpha - like NE) |
| Norepinephrine | Sympathomimetic Activates alpha1, 2, and beta 1. Vassopressor Decongestant Localizer of anesthetic | |
| Isoproterenol | Sympathomimetic Activates beta 1 and beta 2. Vasodilation. Drop in TPR, diastolic, increase in systolic and HR. USed to be used for asthma, but increase in HR not good (now use beta2 agonists) | |
| Adenosine - 1 | K channel opener. 1. Vasodilates 2. Decreases HR/AV conduction 3. cardiopretective Used in ischemic pre/postconditioning And as stres test to induce angina (divert blood away from ischemic area). Also for tx SVT. | Causes bronchospasm so counterindicated for those with asthma. |
| Metyrosine | Sympatholytic. NE synthesis inhibitor. Used in CA secreting tumors. | |
| Ezetimibe | Cholesterol absorption inhibitor Lower LDL after statins. Tx pts with sitosterolemia (high plant sterols) blocks sterol transporter in the gut (NpC1L1). enterohepatic cycling, so excreted in feces. NOT proven to reduce CAD/mortality |
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