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PCOL Exam 2 Drugs
| Drug | Category | Class/Receptor | MOA | SOA | Side Effects/ADRs | Extra/Key Info | Extra Extra |
|---|---|---|---|---|---|---|---|
| Acetylcholine | Neuromuscular | Agonist | Nicotinic & Muscarinic agonist Depolarizing agent | All over body | DUMBBELSS (agonist) | Diarrhea, Urination, Miosis, Bradycardia, Bronchial constriction, Emesis, Lacrimation, Salivation, Stimulation (CNS) | |
| Varenicline (Chantix) | Neuromuscular | Agonist | α4/β2 Nn partial agonist | CNS (Nn) | Headache, nausea, insomnia, suicidal thoughts, depression, flatulence | FDA warning of mood and behavioral changes; used for smoking cessation | |
| Succinylcholine | Neuromuscular | Agonist | Depolarizing agent (Neuromuscular blockade - nicotinic) | NMJ (Nm) Can affect autonomic (PNS/SNS) ganglia | NMJ paralysis (agonist) 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) | |
| Physostigmine | Neuromuscular | Indirect antagonist | Cholinesterase inhibitor (AChE antagonist) | CNS & periphery | DUMBBELSS (agonist) | Penetrates CNS/cross BBB Treatment for anti-muscarinic poisoning (Atropine) | |
| Donepezil (Aricept) | Neuromuscular | Indirect antagonist | Cholinesterase inhibitor (AChE antagonist) | CNS & periphery | DUMBBELSS (agonist) | Lipophilic --> cross BBB Used for dementia/Alzheimer's Longer t1/2 than Physostigmine | |
| Rivastigmine (Exelon) | Neuromuscular | Indirect antagonist | Cholinesterase inhibitor (AChE antagonist) | CNS & periphery | DUMBBELSS (agonist) | Lipophilic --> cross BBB Used for dementia/Alzheimer's Longer t1/2 than Physostigmine | |
| Galantamine | Neuromuscular | Indirect antagonist | Cholinesterase inhibitor (AChE antagonist) | CNS & periphery | DUMBBELSS (agonist) | Lipophilic --> cross BBB Used for dementia/Alzheimer's Longer t1/2 than Physostigmine | |
| PyriDOstigmine | Neuromuscular | Indirect antagonist | Cholinesterase inhibitor (AChE antagonist) | NMJ | DUMBBELS (agonist) No CNS effects | DO NOT cross BBB Reverse the effects of Curare/treatment of myasthenia gravis | |
| Neostigmine | Neuromuscular | Indirect antagonist | Cholinesterase (AChE antagonist) | NMJ | DUMBBELS (agonist) No CNS effects | DO NOT cross BBB Reverse the effects of Curare/treatment of myasthenia gravis | |
| Edrophonium | Neuromuscular | Indirect antagonist | Cholinesterase inhibitor (AChE antagonist) | NMJ | DUMBBELS (agonist) No CNS effects | Used for diagnosis of myasthenia gravis or medications dose adjustments Short duration of action/reversible | |
| Echothiophate | Neuromuscular | Indirect antagonist | Organophosphate inhibitor of acetylcholinesterase enzyme | M3 receptor in ciliary muscle (eye) | Miosis and blurred vision, lacrimation, stinging/redness of eye | Ophthalmology treatment of glaucoma | |
| Botulinum Toxin (Botox) | Neuromuscular | Antagonist | Prevent ACh release | Presynaptic terminal | Muscle relaxation | Cleaves sites on SNARE protein | |
| Curare & Curare-like drugs: Vecuronium Rocuronium Pancuronium Tubocurarine | Neuromuscular | Antagonist | Nm competitive/reversible antagonist Non-depolarizing agent Direct competitive antagonist --> Binds to Ach binding space | NMJ | NMJ paralysis (antagonist) Histamine release, hypotension & tachycardia No CNS effect | Doesn't allow Ach to bind; Ach is required for muscle contraction | |
| Acetylcholine Methacholine Carbachol Bethanechol | Cholinergic | Agonist | Non-selective Muscarinic agonist (M1, M2, M3) | Central and periphery | DUMBBELSS (agonist) | ||
| Pilocarpine | Cholinergic | Agonist | Non-selective Muscarinic agonist (M1, M2, M3) | Central and periphery | DUMBBELSS (agonist) | Treatment of dry mouth (enhance salivation)/glaucoma | |
| Cevimeline | Cholinergic | Agonist | Non-selective Muscarinic agonist (M1, M2, M3) | Central and periphery | DUMBBELSS (agonist) | Treatment of dry mouth (enhance salivation)/glaucoma | |
| Atropine | Cholinergic | Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) Muscarinic antagonist = "Anti-cholinergic" | Central and periphery | Anti-DUMBBELSS (antagonist) Tachycardia, mydriasis, constipation, dry mouth, bronchial dilation, drowsiness | Treatment of organophosphate poisoning (severe DUMBBELSS) Treatment of muscarinic agonist overdose | |
| Scopolamine | Cholinergic | Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) Antagonist of muscarinic, histamine, and serotonin receptors | CNS Penetrate CNS more rapidly | Anti-DUMBBELSS (anti-emesis) | Used to treat motion sickness | |
| Benzotropine (Cogentin) | Cholinergic | Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) | CNS | Anti-DUMBBELSS (antagonist) | Used to treat Parkinson's | |
| Tropicamide | Cholinergic | Antagonist | Muscarinic antagonist | Eyes | Anti-DUMBBELSS (antagonis) | Used for pupil dilation (block M3) | |
| Ipratropium (Atrovent) | Cholinergic | Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) | Lungs | Anti-DUMBBELSS (antagonist) | Short-acting muscarinic antagonist (LAMA) | |
| Tiotropium (Spiriva) | Cholinergic | Antagonist | SELECTIVE Muscarinic antagonist (M1 & M3) | Lungs | Anti-DUMBBELSS (antagonist) Heart rate not affected because it does not target M2 | Long-acting muscarinic antagonist (LAMA) | |
| Aclidinium Umeclidinium | Cholinergic | Antagonist | Muscarinic antagonist | Lungs | Anti-DUMBBELSS (antagonist) | Long-acting muscarinic antagonist (LAMA) | |
| Oxybutynin (Ditropan) | Cholinergic | Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Potential to cause Anti-DUMBBELSS (antagonist) Xerostomia and constipation (M3) (antagonist) | Used to treat overactive bladder | |
| Tolterodine (Detrol) Fesoterodine (Toviaz) | Cholinergic | Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Potential to cause Anti-DUMBBELSS (antagonist) Xerostomia and constipation (M3)(antagonist) | Used to treat overactive bladder | |
| Solifenacin (Vesicare) Darifenacin Trospium | Cholinergic | Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Potential to cause Anti-DUMBBELSS (antagonist) Xerostomia and constipation (M3)(antagonist) | Most selective for M3 --> least likely to cause anti-DUMBBELSS Used to treat overactive bladder | |
| Nitroglycerine (donor) Nitroprusside (donor) Isosorbide di / mononitrate (donor) | Cholinergic | Donor | Donate nitric oxide NO --> sGC --> ↑cGMP | Endothelium of blood vessels (M3) | Vasodilation Lower blood pressure | cGMP is a potent vasodilator | |
| Sildenafil (Viagra) Tadalafil (Cialis) Vardenafil | Cholinergic | Indirect antagonist | 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 | |
| Phenylephrine | Adrenergic | Agonist | 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 | |
| Cocaine | Adrenergic | Indirect antagonist | NE reuptake inhibitor | CNS | HTN, tachycardia, arrhythmias, restlessness | Used with Lidocaine to control arrhythmias (Na+ channel blocker) | |
| Dextroamphetamine & amphetamine (Adderall) Methylphenidate (Concerta, Ritalin) Lisdexamphetamine (Vyvanse) Dexmethylphenidate (Focalin) | Adrenergic | Indirect antagonist | Stimulate pre-synaptic release of NE & DA | CNS | HTN, tachycardia, arrhythmias, restlessness, loss of appetite | Used for ADHD | |
| Phenelzine | Adrenergic | Indirect antagonist | Non-selective MOA-A & MOA-B irreversible antagonist | CNS | HTN, tachycardia, arrhythmias, restlessness | Inhibits breakdown of NE Serious ADR --> HTN crisis due to dietary Tyramine | |
| Selegiline Rasagiline | Adrenergic | Indirect antagonist | SELECTIVE MAO-B irreversible antagonist | CNS | HTN, tachycardia, arrhythmias, restlessness | Inhibits breakdown of NE Used for depression & Parkinson's | |
| Prazosin Terazosin (Hytrin) Doxazosin (Cardura) Tamsulosin (Flomax; α1a) | Adrenergic | Antagonist | 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) | |
| Phenoxybenzamine | Adrenergic | Antagonist | 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) | |
| Mirtazepine (Remeron) | Adrenergic | Antagonist | 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: α2’s located in small blood vessels cause vasoconstriction --> antagonist will cause vasodilation --> peripheral edema | |
| Clonidine (Catapres) Brimonidine (Alphagan P) Tizanidine (Zanaflex) Guanfacine (Intuniv) Dexmedetomidine (Precedex) | Adrenergic | Agonist | 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 | |
| Dobutamine | Adrenergic | Agonist | β1 agonist | Heart, kidneys, brain | Increased heart rate and contractility, tachycardia/arrhythmias, increased RAAS, CNS stimulation | LOW dose: β1 selective HIGH dose: β1 > β2 > α1 Used in patients with systolic dysfunction and congestive heart failure | |
| Metoprolol (Lopressor or Toprol) Atenolol (Tenormnin) Nebivolol (Bystolic) "MAN" | Adrenergic | Antagonist | SELECTIVE β1 antagonist "β1 beta-blockers" | Heart, kidneys, brain | Decreased heart rate and contractility, fatigue/dizziness, bradycardia, decreased RAAS, CNS depression | ||
| SABA: Albuterol (Ventolin) Levalbuterol (Xopenex) LABA: Salmeterol Formoterol | Adrenergic | Agonist | β2 agonist | Lungs, vasculature, CNS | Bronchial dilation, vasodilation, excitation | ||
| Propranolol (Inderal) Timolol (Betimol) | Adrenergic | Antagonist | 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 | |
| Pindolol | Adrenergic | Antagonist (Partial agonist) | 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 | |
| Carvedilol (Coreg) Labetalol (Trandate) | Adrenergic | Antagonist | 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 | |
| Mirabegron | Adrenergic | Agonist | β3 agonist | Bladder | Relief for overactive bladder | Less side effects than muscarinic antagonists | |
| Epinephrine | Adrenergic | Agonist | β1, β2 agonist (blood vessels) | Heart and vasculature | 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 | |
| Norepinephrine (Levophed) | Adrenergic | Agonist | α1, β1 agonist | Heart and vasculature | Increase TPR, heart rate, contractility | Used for shock (life support) | |
| Isoproterenol | Adrenergic | Agonist | β1, β2 agonist (lungs) | Heart and lungs | Hyperglycemia, palpitations, tachycardia, arrhythmias | Used for asthma (not 1st line), bradycardia, and heart block (AV) | |
| Aliskiren | RAAS | Antagonist | 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 | |
| Captopril Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) | RAAS | Antagonist | ACE inhibitor (Angiotensin converting enzyme inhibitor) REVERSIBLE antagonist | 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) Bonus effect: Ang I goes down alternate pathway & converted to Ang 1-7 which bind to AT2 = oppose AT1 Bonus effect 2: increase levels of bradykinin (dilator)=dry cough | Most are Pro-drugs = improve ADMET profile 1st line for HTN |
| Losartan (Cozaar) Valsartan (Diovan) Olmesartan (Benicar) Telmisartan (Micardis) Irbesartan (Avapro) Medoxomil | RAAS | Antagonist | 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 na even more active metabolite - very effective | Most are Pro-drugs = improve ADMET profile High affinity for AT1 |
| Spironolactone Eplerenone | RAAS | Antagonist | Potassium-sparing diuretic Mineralocorticoid (MR) receptor antagonist | Kidney => collecting duct of nephron | Hyperkalemia, diarrhea, drowsiness Males: gynecomastia &. impotence | These drugs are aldosterone antagonists | Aldosterone enhances the production of Na+/K+ channels (lumen) &pumps (interstitial space side of cell)& these drugs bind to same space therefore not allowing aldosterone to bind = decreasing the production of these channels &pumps = less Na+ reabsorption |
| Metoprolol | RAAS | Antagonist | Selective β1 blocker | Kidney | Less renin production = no RAAS pathway |
Created by:
salmouie