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PCOL Exam 2 Drugs
| Drug | MOA | SOA | ADRs | Key Info | Class |
|---|---|---|---|---|---|
| Acetylcholine | Nicotinic & Muscarinic Depolarizing agent | All over body | DUMBBELSS | Diarrhea, Urination, Miosis, Bradycardia, Bronchial constriction, Emesis, Lacrimation, Salivation, Stimulation (CNS) | Agonist |
| Varenicline (Chantix) | α4/β2 Nn partial agonist | CNS (Nn) | Headache, insomnia, suicidal thoughts, depression, flatulence | FDA warning of mood and behavioral changes; used for smoking cessation | Agonist |
| Succinylcholine | Depolarizing agent (Neuromuscular blockade – nicotinic) | NMJ (Nm) Can affect autonomic (PNS / SNS) ganglia | NMJ Paralysis Hyperkalemia, HTN & arrhythmias, muscle pain (myalgia), hyperthermia | Phase 1: binds to Ach binding space and keeps all Na+ channels open (cannot repolarize) Phase 2: blocks Na+ channels (cannot depolarize) | Agonist |
| Physostigmine | Cholinesterase Inhibitor (AChE Antagonist) | CNS & periphery | DUMBBELSS | Penetrates CNS / cross BBB Treatment for anti-muscarinic poisoning (Atropine) | Indirect Agonist |
| Donepezil (Aricept) Rivastigmine (Exelon) Galantamine | Cholinesterase Inhibitor (AChE Antagonist) | CNS & periphery | DUMBBELSS | Lipophilic cross BBB Used for dementia / Alzheimer’s Longer t1/2 than Physostigmine | Indirect Agonist |
| PyriDOstigmine Neostigmine | Cholinesterase Inhibitor (AChE Antagonist) | NMJ | DUMBBELS No CNS effects | DO NOT cross BBB Reverse the effects of Curare / treatment of myasthenia gravis | Indirect Agonist |
| Edrophonium | Cholinesterase Inhibitor (AChE Antagonist) | NMJ | DUMBBELS No CNS effects | Used for diagnosis of myasthenia gravis or medication dose adjustments Short duration of action/reversible | Indirect Agonist |
| Echothiophate | Organophosphate inhibitor of acetylcholinesterase enzyme | M3 receptor in ciliary muscle (eye) | Miosis and blurred vision, lacrimation, stinging / redness of eye | Ophthalmology treatment glaucoma | Indirect Agonist |
| Botulinum Toxin (Botox) | Prevent ACh release | Presynaptic terminal | Muscle relaxation | Cleaves sites on SNARE protein | Antagonist |
| Curare & Curare like Mivacurium Vecuronium Rocuronium Pancuronium Tubocurarine | NON-depolarizing agent Direct competitive antagonist Binds to Ach binding space | NMJ | NMJ Paralysis Histamine release, hypotension & tachycardia No CNS effect | Doesn’t allow Ach to bind; Ach is required for muscle contraction | Antagonist |
| Acetylcholine Methacholine Carbachol Bethanechol | Non-selective Muscarinic Agonist (M1, M2, M3 | Central and periphery | DUMBBELSS | Agonist | |
| Pilocarpine Cevimeline | Non-selective Muscarinic Agonist (M1, M2, M3) | Central and periphery | DUMBBELSS | Treatment of dry mouth (enhance salivation) / glaucoma | Agonist |
| Atropine | Non-selective Muscarinic Antagonist (M1, M2, M3) Muscarinic Antagonist = “Anti-cholinergic” | Central and periphery | Anti-DUMBBELSS Tachycardia, mydriasis, constipation, dry mouth, bronchial dilation, drowsiness | Treatment of organophosphate poisoning (severe DUMBBELSS) Treatment of muscarinic agonist overdose | Antagonist |
| Scopolamine | Non-selective Muscarinic Antagonist (M1, M2, M3) | CNS – Penetrate CNS more rapidly | Anti-DUMBBELSS (anti-emesis) | Used to treat motion sickness | Antagonist |
| Benztropine (Cogentin) | Non-selective Muscarinic Antagonist (M1, M2, M3) | CNS | Anti-DUMBBELSS | Used to treat Parkinson’s | Antagonist |
| Tropicamide | Muscarinic Antagonist | Eyes | Anti-DUMBBELSS | Used for pupil dilation (block M3) | Antagonist |
| Ipratropium (Atrovent) | Non-selective Muscarinic Antagonist (M1, M2, M3) | Lungs | Anti-DUMBBELSS | Short-acting muscarinic antagonist (SAMA) | Antagonist |
| Tiotropium (Spiriva) | SELECTIVE Muscarinic Antagonist (M1 & M3) | Lungs | Anti-DUMBBELSS Heart rate not affected because it does not target M2 | Long-acting muscarinic antagonist (LAMA) | Antagonist |
| Aclidinium Umeclidinium | Muscarinic Antagonist | Lungs | Anti-DUMBBELSS | Long-acting muscarinic antagonist (LAMA) | Antagonist |
| Oxybutynin (Ditropan) Tolterodine (Detrol) Fesoterodine (Toviaz) Solifenacin (Vesicare) Darifenacin Trospium | Non-selective Muscarinic antagonist (M1, M2, M3) All are more selective for M3 | M3 in Bladder | All have potential to cause Anti-DUMBbELSs Xerostomia and constipation (M3) | Solifenacin, Darifenacin, and Trospium are Most selective for M3 least likely to cause anti-DUMBbELSS Used to treat overactive bladder | Antagonist |
| Nitroglycerine Nitroprusside Isosorbide di / mononitrate | Donate nitric oxide NO sGC ↑cGMP | Endothelium of blood vessels (M3) | Vasodilation Lower blood pressure | cGMP is a potent vasodilator | Donor |
| Sildenafil (Viagra) Tadalafil (Cialis) Vardenafil | Blocks PDE increase cGMP | Endothelium of blood vessels (M3) | Vasodilation Lower blood pressure | Blocks enzyme that breaks down cGMP = more cGMP Used to treat erectile dysfunction | Indirect Agonist |
| Phenylephrine | α1 agonist | Blood vessels Eyes | HTN, Burning & nasal discharge, rebound congestion | Used as nasal decongestant and ophthalmics (mydriasis) Down-reg rebound congestion Avoid in patients with HTN | Agonist |
| Cocaine | NE reuptake inhibitor | CNS | HTN, tachycardia, arrythmias, restlessness | Used with Lidocaine to control arrythmias (Na+ channel blocker) | Indirect Agonist |
| Dextroamphetamine & amphetamine (Adderall) Methylphenidate (Concerta, Ritalin) Lisdexamphetamine (Vyvanse) Dexmethylphenidate (Focalin) | Stimulate pre-synaptic release of NE & DA | CNS | HTN, tachycardia, arrythmias, restlessness, loss of appetite | Used for ADHD | Indirect Agonist |
| Phenelzine | Non-selective MOA-A & MOA-B irreversible antagonist | CNS | HTN, tachycardia, arrythmias, restlessness | Inhibits breakdown of NE Serious ADR HTN crisis due to dietary Tyramine | Indirect Agonist |
| Selegiline Rasagiline | SELECTIVE MAO-B irreversible antagonist | CNS | HTN, tachycardia, arrythmias, restlessness | Inhibits breakdown of NE Used for depression & Parkinson’s | Indirect Agonist |
| Prazosin Terazosin (Hytrin) Doxazosin (Cardura) Tamsulosin (Flomax) α1a | SELECTIVE α1 antagonist reversible | Brain Eye Nose Blood vessels Urethra | Headache Blurred vision Orthostatic hypotension reflex tachycardia Sexual dysfunction | Used to treat HTN, BPH, and PTSD (prazosin only) Decrease preload and afterload (blood vessels) | Antagonist |
| Phenoxybenzamine | Non-selective α1 & α2 antagonist irreversible Decrease peripheral resistance | Brain Eye Nose Blood vessels Urethra GI | Orthostatic hypotension reflex tachycardia GI stimulation (α2 on PNS fiber blocked) Headache, Miosis | Can be used for HTN crisis caused by phenelzine (short term control) Longer duration of action (irreversible highest affinity for α1 | Antagonist |
| Mirtazapine (Remeron) | NON-SELECTIVE α2 antagonist α1 antagonist Muscarinic antagonist H1 antagonist 5-HT 2a antagonist | CNS Enhances release of NE & 5-HT (serotonin) Blocks H1 release drowsiness | Drowsiness, weight gain, increased cholesterol xerostomia, constipation, peripheral edema, HTN | Used for MDD Rare side effect: agranulocytosis α2’s located in small blood vessels cause vasoconstriction antagonist will cause vasodilation peripheral edema | Antagonist |
| Clonidine (Catapres) Brimonidine (Alphagan P) Tizanidine (Zanaflex) Guanfacine (Intuniv) Dexmedetomidine (Precedex) | α2 agonist | CNS Enhance inhibitory / suppress SNS | Sedation, dry mouth, hypotension, bradycardia, sexual dysfunction, depression, constipation (activates GI inhibitory negative feedback pathway less Ach) | Hypertensive crisis can occur if taken off drug abruptly due to up-regulation of receptors | Agonist |
| Dobutamine | β1 agonist | Heart Kidneys Brain | Increased heart rate and contractility Tachycardia / arrythmias Increased RAAS CNS stimulation | LOW dose: β1 selective HIGH dose: β1 > β2 > α1 Used in patients with systolic dysfunction and congestive heart failure | Agonist |
| Metoprolol (Lopressor or Toprol) Atenolol (Tenormin) Nebivolol (Bystolic) “MAN” | SELECTIVE β1 antagonist “β1 beta-blockers” | Heart Kidneys Brain | Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression | Antagonist | |
| SABA: Albuterol (Ventolin) Levalbuterol (Xopenex) LABA: Salmeterol Formoterol | β2 agonist | Lungs Vasculature CNS | Bronchial dilation Vasodilation Excitation | Agonist | |
| Propranolol (Inderal) Pindolol (PARTIAL AGONIST) Timolol (Betimol) | NON-SELECTIVE Beta-blockers β1 & β2 antagonist | Heart Kidneys Brain Lungs Vasculature | Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression | Mask symptoms of hypoglycemia no nervousness / tremors Propranolol given at low dose for anxiety (target β1 in brain) Contraindicated for asthma pts | Antagonist |
| Carvedilol (Coreg) Labetalol (Trandate) | β1 & β2 antagonist, & α1 antagonist | Heart Kidneys Brain Lungs Vasculature | Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression | Mask symptoms of hypoglycemia no nervousness / tremors Contraindicated for asthma pts | Antagonist |
| Mirabegron | β3 agonist | Bladder | Relief for overactive bladder | Less side effects than muscarinic antagonists | Agonist |
| Epinephrine | β1, β2 agonist (blood vessels | Heart and vasculature Adrenergic receptors | SNS activation | Low dose: β1 & β2 High dose: everything Used for shock (life support) / anaphylaxis Patients must be weaned off due to down regulation of receptors | Agonist |
| Norepinephrine (Levophed) | α1, β1 agonist | Heart & vasculature | Increase TPR, heart rate, contractility | Used for shock (life support) | Agonist |
| Isoproterenol | β1, β2 agonist (lungs) | Heart & lungs | Hyperglycemia Palpitations Tachycardia Arrythmias | Used for asthma (not 1st line), bradycardia, and heart block (AV) | Agonist |
| Aliskiren | Selective Renin inhibitor REVERSIBLE antagonist | Blood stream (Renin - 1st step in RAAS pathway) | Lower TPR Lower aldosterone Decrease sodium and water reabsorption Angioedema, hypotension, cough, headache, diarrhea, skin rash | Low drug bioavailability but high affinity for renin Renin is the rate limiting enzyme for the RAAS pathway | Antagonist |
| Captopril Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) | ACE inhibitor Angiotensin converting enzyme inhibitor REVERSIBLE antagonists | Blood stream | Lower TPR Lower aldosterone Decrease sodium and water reabsorption Dry cough, hyperkalemia, angioedema, first dose hypotension, fetopathic potential | Primary effect: inhibit ACE (ACE converts Ang I to Ang II & breaks down bradykinin) Most are Pro-drugs improve ADMET profile 1st line for HTN | Antagonist |
| Losartan (Cozaar) Valsartan (Diovan) Olmesartan (Benicar) Telmisartan (Micardis) Irbesartan (Avapro) Medoxomil | ARB Angiotensin II receptor blocker REVERSIBLE antagonists | Blood stream | Lower TPR Lower aldosterone Decrease sodium and water reabsorption Hyperkalemia, angioedema | Primary effect: Block AT1 Bonus effect 1: increase AT2 activation (oppose AT1) Losartan is an active drug that turns into an even more active metabolite – very effective Most are Pro-drugs improve ADMET profile High affinity for AT1 | Antagonist |
| Spironolactone Eplerenone | Potassium-sparing diuretic Mineralocorticoid (MR) receptor antagonist | Kidney Collecting duct of nephron | Hyperkalemia, diarrhea, drowsiness Males: gynecomastia & impotence | Aldosterone enhances the production of Na+/K+ channels (lumen) and pumps (interstitial space side of cell), and these drugs bind to the same space not allowing aldosterone to bind and thus decreasing the production of these channels and pumps less Na+ | Antagonist |
| Metoprolol | Selective β1 blocker | Kidney | Less renin production no RAAS pathway | Antagonist |
Created by:
beezy41
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