drug classes autonomics and cardio
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- ALPHA-1 AGONISTS
- arterial vasoconstriction, ↑ contractility
- Phenylephrine (Neosynephrine)
- Pure and potent, tx paroxysmal a-tach
- Methoxamine
- Pure and potent
- Norepinephrine
- Shock
- Epinephrine
- ↑ BP
- Dopamine
- Low dose
- ALPHA-1 ANTAGONISTS
- Phentolamine
- α1 and α2 antagonists
- Phenoxybenzamine
- Prazosin (Minipress)
- Selective α1 blocker, prazosin syncope, first dose effect, tachyphylaxis (tolerance)
- Terazosin (Hytrin)
- Selective α1 blocker, longer τ (less first dose effect), Tx BPH
- Doxazosin (Cardura)
- Tamsulosin (Flomax)
- Urological indications
- Alfuzosin (Urotraxal)
- Clonidine (Catapres)
- ↓BP and CNS, Clonidine rebound, mild ↓ cholesterol, Raynaud’s, ↓ CNS
- Methyldopa (Aldomet) à α-methylnorepinephrine
- ↓BP and CNS, safer mild CO effect, delay in onset (6 hrs), hemolytic anemia (rare)
- Tizanidine (Zanaflex)
- Shorter Ï„ (2 hrs), rebound, tx muscular spasm
- Guanfacine
- Long Ï„ (17 hrs), less withdrawl
- Guanabenz
- ALPHA-2 ANTAGONISTS
- ↑ sympathetics, ↑ NE release
- Yohimbine
- Aphrodisiac
- BETA AGONISTS
- Isoproterenol
- Non-selective, ↑HR, CO, contractility
- Dobutamine
- ß1 selective, no ΔBP
- BETA ANTAGONISTS
- nonselective tx: portal HT, tremor, vascular headache
- Propranolol (Inderal) – the original
- Non-selective, cheap, heavy liver metab
- Metoprolol (Lopressor)
- ß1 selective, no bronchoconstriction (asthma), ß2 hyperresponse?
- Atenolol (Tenormin)
- ß1 selective, no bronchoconstriction (asthma)
- Nadolol (Corgard)
- Not lipophilic, Europe, ~ Propranolol
- Esmolol
- Labetalol
- α1 blocker (S,R), ↑ potency orally; ß1 antag and partial ß2 agonist (R,R: higher clearance) [1:7]
- Carvedilol
- Potent α1 blocker à ↓PVR à tx CHF, racemic mixture
- Pindolol
- Some agonist activity
- Timolol
- DOPAMINE receptor Drugs
- D1 – vasodilation, D2 – emesis, ↓prolactin, D4 – risk taking
- Bromocriptine
- Dopamine Agonists
- Fenoldopam (9x D1)
- Apomorphine
- Metoclopramide
- Dopamine Antagonists
- Haloperidol
- Domperidone
- INDIRECT-ACTING Phenylethylamines
- Tyramine
- Displaces NE into synaptic cleft – cheese, wine, ham
- Ephedrine (Ephedra, Ma Huang)
- Weight loss, ↑ SKM and CNS
- Amphetamine
- More potent CNS
- Hydroxyamphetamine
- Tyramine-like, test for more central Horner’s syndrome
- Phenylpropanolamine (Dexatrim)
- Sympathomimetic and vasoconstriction
- Pseudoephedrine (Sudafed)
- Replacement Dexatrim analog
- (-) metyrosine
- MUSCARINIC AGONISTS
- Acetylcholine
- Rapid hydrolysis, rarely used
- Bethanechol
- Gastric emptying, tx urinary retention
- Pilocarpine
- Miosis and salivation, Tx open-angle glaucoma
- Methacholine
- Bronchoconstriction, methacholine challenge
- Carbachol
- Muscarine, Arecholine
- Naturally occurring
- MUSCARINIC ANTAGONISTS
- Atropine – Deadly nightshade (Atropa belladonna)
- ↑HR, dilate pupils
- Jimson Weed (Datura stramonium)
- Hallucinogen
- Hyoscine – Henbane (Hyoscyamus niger)
- Hallucinogen
- Pirenzepine
- M1 selective blocker, gastric acid release
- NICOTINIC AGONISTS
- Nicotine
- ↑Symp & PS, Bezold-Jarisch reflex
- NICOTINIC ANTAG/ SKM RELAXANT
- Respirator, histamine release
- Tubocuranine
- Nondepolarizing blocker, long Ï„, reversible by adding ACh
- Succinylcholine
- Depolarizing blocker, short Ï„, Pseudocholinesterase deficiency
- ANTICHOLINESTERASES
- SLUDGE
- Physostigmine
- Enters CNS à restless, apprehension, HT, nausea
- Neostigmine
- Does not enter CNS, tx myasthenia gravis & glaucoma
- Edrophonium (Tensilon)
- Treat MG
- Ambenonium
- Pyridostigmine
- Parathion à Paraoxon
- Phosphorothionates à oxidation ↑AChE
- Malathion
- Insecticide
- Tacrine (Cognex)
- ALZ, L toxic
- Donezapil (Aricept)
- ALZ, replaced Tacrine
- Rivastigmine (Exelon)
- Pralidoxime
- Counteracts AChE’s and reactivates ChE
- WAR GASES
- Organophosphates – insecticides -- ↑ ALL cholinergic transmission (N&M)
- Sarin Gas
- Irreversible cholinesterase inhibitors (N & M)
- VX
- Binary agents, death by asphyxiation
- SPASMOLYTICS
- Dantrolene
- ↓ Ca release à relax muscles, tx malignant hyperthermia
- Baclofen
- Muscle relaxant, partial GABA agonist
- Diazepam
- Anti-anxiety agents that ↓ nerves in muscles
- Chlordiazepoxide
- Carisoprodol
- Meprobamate
- Strychnine
- Glycine antagonist à ↑ respiration, convulsions
- NO-DEPENDENT VASODILATORS
- A&V vasodilation, SM relaxation, Tolerance
- Nitroglycerin (TNG)
- Nitrate ester, Sublingual, high clearance (minutes)
- IsoSorbide DiNitrate (Isordil)
- Nitrate ester, Oral, variable Ï„ of metabolites, intermediate clearance
- Isosorbide MonoNitrates (2-IMN > 5-IMN)
- Nitrate ester, 100% bioavailable, less variable, low clearance
- **Sildenafil (Viagra)
- Inhibits cGMP phosphodiesterase V à ↑postural hypotension
- Nitroprusside (Nipride) à NO + CN
- Spontaneous conversion to NO + CN, Thiocyanate toxicity (tx Na thiosulfate), no light, short Ï„
- DIRECT VASODILATORS
- Hydralazine (Apresoline)
- Arterial vasodilator, tx HT & CHF
- Minoxidil (Loniten)
- Arterial vasodilator, tx HT
- CALCIUM CHANNEL BLOCKERS
- ↓ Ca à vasodilation, long acting, inhibit CYP3A4
- Nifedipine (1,4-dihydropyridine)
- L channel, ↑ chronotropy and CO, ↑ symp, variable partition coefficients, oral > sublingual
- Amlodipine
- High partition coefficient à high Vd, slow onset of action, prolonged duration
- Verapamil (phenylalkylamine)
- Most potent AV blocking, hypotensive; AVOID: wide-complex tachy,WPW,CHF,AVblock,DIG
- Diltiazem (benzothiazepines)
- IV, AV node blocking w/o hypotension, great for A-fib
- Mibefradil
- T Channel, FDA removed, vasodilation > cardiac depression
- Angiotensin Converting Enzyme Inhibitors
- ↑ bradykinin, renin, ang I, ↓angiotension II
- Captopril
- Sulfhydryl, shorter Ï„, prostaglandin effect
- Fosinopril
- Phosphinyl, L&K
- Trandolapril
- Enalapril
- Carboxyl
- Lisinopril
- Benazepril
- Quinapril
- Ramipril
- Moexipril
- Angiotensin Receptor Blockers
- ↑ bradykinin, renin, ang I, ↑ angiotensin II, fetotoxic
- Saralasin
- Original, IV, partial agonist
- Losartan à EXP-3174
- Non-peptide, short Ï„, normal-high renin levels, uricosuric effect
- Valsartan
- Irbesartan
- Candesartan
- Osmotic Diuretics
- Most of tubule: IV volume expansion (filtered, not reabsorbed)
- Mannitol
- IV
- Urea
- IV
- Glycerin
- Oral
- Carbonic Anhydrase Inhibitors
- PT: ↓NaHCO3 reabsorption (metabolic acidosis), sulfonamides
- Acetazolamide (Diamox)
- Tx glaucoma
- Dichlorphenamide
- Loop Diuretics (high ceiling)
- TALH: NaKCl2 symport inhibitor, MOST potent, Ca and Mg loss
- Furosemide (Lasix)
- Releases vasodilator prostaglandin from kidneys à ↑ venous capacitance
- Bumetanide (Bumex)
- Ethacrynic Acid (Edecrin)
- Non-sulfamide
- Torsemide (Demadex)
- Thiazides
- DCT: NaCl cotransport inhibitor, ↑ Glu,Urea,Ca; ↓ K,H,Na
- Chlorothiazide (Diuril)
- Hydrochlorothiazide (HCTZ, Esidrex)
- Sulfonamide, hyperuricemia à gout; tx diabetes insipidus
- Chlorthalidone (Hygroton)
- Metolazone (Zaroxolyn)
- K Sparing Diuretics
- CT: Na channel inhibitors, ↓ K excretion; careful! (ACEI, ↑K, ARF)
- Amiloride
- Partially absorbed; inhibits NaH antiporter (lumen) and NaK ATPas (basal); tx Liddle’s
- Triamterene
- Well absorbed, renal and metabolism
- Aldosterone Antagonists
- steroid analogues compete with aldosterone, best for cirrhosis
- Spironolactone à Canrenone
- Affects estrogen receptors (gynecomastia), tx Cohn’s
- Eplerenone
- Newer version
- ADH Antagonists
- CT: ↓ADH effects and ↓water reabsorption
- Demeclocycline (Declomycin)
- Tetracycline derivative; tx SIADH
- ANTIARRYTHMIC DRUGS
- Class I
- Na Channel Blockers, “local anestheticsâ€
- Class Ia
- Intermediate recovery (1-5s), ↑ QRS, QT, APD, blocks Na and K channels;
- Quinidine
- α receptor block and vagal inhibition; ↑DIG
- Procainamide à N-acetylprocainamide (NAPA)
- Metabolite blocks K channels only, renal dose adjustment, lupus syndrome
- Disopyramide
- Aggravates CHF and prostatism, effect ↑ with dose
- Class Ib
- Fast recovery (<1s), shorten repolarization
- Lidocaine
- IV, ↓ v-fib, ↑ mortality, CNS toxicity, dose adjustment (CHF and liver)
- Mexiletine
- Oral, CNS toxic
- Tocainide
- Oral ,CNS toxic, agranulocytosis
- Phenytoin
- Anticonvulsant, effective for digitalis intoxication
- Class Ic
- Slow recovery, marked ↑PR, ↑QRS, ± QT
- Flecainide
- Very long τ from block, very effective for isolated PVC, RSVT, ↑DIG
- Encainide
- ↑ mortality post-MI, FDA removed
- Propafenone
- ~ Flecainide, Weak ß blocker (↑ at high conc),
- Moricizine
- Phenothiazine analog, unique, weaker version, multiple metabolites
- Class II
- Beta Blockers, ↓ HR and ↑ PR (slow down)
- Propranolol
- Sotalol
- Non-selective ß blocker, causes TdP
- Acebutolol
- Class III
- K channel blockers, ↑ AP duration, ↑ QT
- Amiodarone
- Class I,II,III,IV actions, effective most arr, multiple toxic (esp lung), LONG τ (50d), ↑DIG
- Bretylium
- No longer marketed, still available – biphasic NE effects (↑ then ↓)
- Dofetilide
- Pure class III, Renal dose adjustment, causes TdP (1-3%)
- Ibutilide
- Acute IV, stop A-flutter (60%) and A-fib (40%), block K, opens Na, Causes TdP (6%)
- *N-acetylprocainamide
- Might have some class III effects
- Class IV
- Ca channel blockers, ↓ HR and ↑ PR
- Adenosine
- Purinergic receptor blocker, ultra-short acting AV blocker (seconds) – acute tx, rapid IV, short Sx
- THROMBOLYTIC
- plasminogen activators
- Streptokinase (SK)
- 1° Non-enzymatic protein from streptococci, indirect, antibodies to SK à agg
- Urokinase (UK)
- 1° Trypsin-like enzyme, LMW, direct, (-) PAI-1, non-antigenic
- Aniosylated Plasminogen Streptokinase Complex (APSAC)
- 2° SK and human plasminogen complex à spontaneous deacylation, long τ (60m), IV bolus, Ab
- t-PA (Alteplase)
- 2° Fibrin/clot-specific binding (1000x), glycosylation, short τ (6m), (-) PAI-1
- Reteplase
- 3° t-PA derivative, kringle #2 and protease domain, non-glycosylated, no EGF à longer τ (15m)
- TNK-t-PA (Tenecteplase)
- 3° no glycosylation, less PAI-1 effect, ↑ fibrin specificity
- Amicar (ε-aminocaproic acid)
- Antifibrinolytic – inhibits plasmin to stop bleeding
- Tranexamic acid
- DIGITALIS
- inhibits NaKATPase à ↑ Calcium; treat CHF, Arrhythmias; DigiToxicity
- INOTROPICS
- oral agents for ↑ contractility
- Ibopamine
- Dopaminergic agonist
- Inamrinone (Amrinone)
- PDE inhibitor ↑cAMP à ↑CO and ↓SVR, short-term CHF tx, ↑AV cond, ARR, oral ↑toxic
- Milrinone (Primacor)
- Shorter Ï„ (30 min vs 2.5 h), more selective, fewer side fx (e.g. thrombocytopenia, gi, liver, fever)
- Vesnarinone
- PDE inhibitor
- Pimobendan
- PDE inhibitor w/ Ca sensitizing properties
- Nesiritide
- Natriuretic peptide
- Omapatrilat
- Neutral endopeptidase inhibitor—blocks both ACE and natriuretic peptide degradation
- ANTI-platelets
- Aspirin
- Irreversibly acylates cyclooxygenase, blocking TxA2 synth
- Dipyridamole (Persantine)
- Inhibits PDE à ↑cAMP
- ASA w/ Dipyridamole (Aggrenox)
- Work together well
- Ticlopidine (Ticlid)
- Inhibit ADP platelet activation, more potent
- Clopidogrel (Plavix)
- Inhibit ADP platelet activation, less potent
- Abciximab (Reopro)
- GP IIb/IIIa antagonist prevents fibrinogen binding
- AntiCoagulants
- Unfractioned Heparin
- Indirect thrombin and Xa inhibitor
- Enoxaparin (LMW Heparin)
- Indirect Xa inhibitor
- Dalteparin
- Less variability and monitoring, slower clearance
- Tinzaparin
- Protamine
- Treat heparin overdose
- Fondaparinux
- Pentasaccharide Factor Xa inhibitor
- Lepirudin
- Direct thrombin inhibitor, tx HIT, renal clearance
- Argatroban
- Direct thrombin inhibitor (active site only), tx HIT, liver metab
- Bivalrudin
- Direct thrombin inhibitor, tx angioplasty, renal clearance
- Hirudin
- Direct thrombin inhibitor, leech recombinant protein
- Warfarin (Coumadin)
- Vitamin K antagonist -- ↓post-translational carboxylase, ↓factor 2,7,9,10,C,S, INR
- Various Enzymes
- And Stuff
- Tyrsosine hydroxylase ***
- Tyrosine à DOPA
- Dopa Decarboxylase (aromatic-L-aminoacid decarboxylase)
- DOPA à Dopamine