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PCOL Exam 2 Drugs
MOA, SOA, SEs, Extra Info
| Drug | Section | MOA | SOA | Side Effects/ADRs | Extra/Key Information |
|---|---|---|---|---|---|
| Acetylcholine | Agonist | Nicotinic & Muscarinic Depolarizing Agent | All over body | DUMBBELSS | Diarrhea, Urination, Miosis, Bradycardia, Bronchial constriction, Emesis, Lacrimation, Salivation, Stimulation (CNS) |
| Varenicline (Chantix) | Agonist | α4/β2 Nn partial agonist | CNS (Nn) | Headache, insomnia, suicidal thoughts, depression, flatulence | FDA warning of mood and behavioral changes; used for smoking cessation |
| Succinylcholine | Agonist | 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) |
| Physostigmine | Indirect Antgonist | Cholinesterase Inhibitor (AChE Antagonist) | CNS & Periphery | DUMBBELSS | Penetrates CNS / cross BBB Treatment for anti-muscarinic poisoning (Atropine) |
| Donepezil (Aricept) | Indirect Antagonist | Cholinesterase Inhibitor (AChE Antagonist) | CNS & Periphery | DUMBBELSS | Lipophilic cross BBB Used for dementia / Alzheimer’s Longer t1/2 than Physostigmine |
| Rivastigmine (Exelon) | Indirect Antagonist | Cholinesterase Inhibitor (AChE Antagonist) | CNS & Periphery | DUMBBELSS | Lipophilic cross BBB Used for dementia / Alzheimer’s Longer t1/2 than Physostigmine |
| Galantamine | Indirect Antagonist | Cholinesterase Inhibitor (AChE Antagonist) | CNS & Periphery | DUMBBELSS | Lipophilic cross BBB Used for dementia / Alzheimer’s Longer t1/2 than Physostigmine |
| Edrophonium | Indirect Antagonist | Cholinesterase Inhibitor (AChE Antagonist) | NMJ | DUMBBELSS and NO CNS EFFECTS | Used for diagnosis of myasthenia gravis or medication dose adjustments Short duration of action/reversible |
| PyriDOstigmine | Indirect Antagonist | Cholinesterase Inhibitor (AChE Antagonist) | NMJ | DUMBBELS No CNS effects | DO NOT cross BBB Reverse the effects of Curare / treatment of myasthenia gravis |
| Neostigmine | Indirect Antagonist | Cholinesterase Inhibitor (AChE Antagonist) | NMJ | DUMBBELS No CNS effects | DO NOT cross BBB Reverse the effects of Curare / treatment of myasthenia gravis |
| Echothiophate | Indirect Antagonist | Organophosphate inhibitor of acetylcholinesterase enzyme | M3 receptor in ciliary muscle (eye) | Miosis and blurred vision, lacrimation, stinging / redness of eye | Ophthalmology treatment glaucoma |
| Botulinum Toxin (Botox) | Antagonist | Prevent ACh Release | Presynaptic Terminal | Muscle relaxation | Cleaves sites on SNARE proteins |
| Methacholine | Cholinergic Agonist | Non-selective Muscarinic Agonist (M1, M2, M3) | Central and periphery | DUMBBELSS | N/A |
| Carbachol | Cholinergic Agonist | Non-selective Muscarinic Agonist (M1, M2, M3) | Central and periphery | DUMBBELSS | N/A |
| Bethanechol | Cholinergic Agonist | Non-selective Muscarinic Agonist (M1, M2, M3) | Central and periphery | DUMBBELSS | N/A |
| Pilocarpine | Cholinergic Agonist | Non-selective Muscarinic Agonist (M1, M2, M3) | Central and periphery | DUMBBELSS | Treatment of dry mouth (enhance salivation) / glaucoma |
| Cevimeline | Cholinergic Agonist | Non-selective Muscarinic Agonist (M1, M2, M3) | Central and periphery | DUMBBELSS | 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 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) | CNS – Penetrate CNS more rapidly | Anti-DUMBBELSS (anti-emesis) | Used to treat motion sickness |
| Benztropine (Cogentin) | Cholinergic Antagonist | Non-selective Muscarinic Antagonist (M1, M2, M3) | CNS | Anti-DUMBBELSS | Used to treat Parkinson's |
| Tropicamide | Cholinergic Antagonist | Muscarinic Antagonist | Eyes | Anti-DUMBBELSS | Used for pupil dilation (block M3) |
| Ipratropium (Atrovent) | Cholinergic Antagonist | Non-selective Muscarinic Antagonist (M1, M2, M3) | Lungs | Anti-DUMBBELSS | Short-acting muscarinic antagonist (SAMA) |
| Tiotropium (Spiriva) | Cholinergic Antagonist | SELECTIVE Muscarinic Antagonist (M1 & M3) | Lungs | Anti-DUMBELSS Heart rate not affected because it does not target M2 | Long-acting muscarinic antagonist (LAMA) |
| Aclidinium | Cholinergic Antagonist | Muscarinic Antagonist | Lungs | Anti-DUMBBELSS | Long-acting muscarinic antagonist (LAMA) |
| Umeclidinium | Cholinergic Antagonist | Muscarinic Antagonist | Lungs | Anti-DUMBBELSS | Long-acting muscarinic antagonist (LAMA) |
| Oxybutinin (Ditropan) | Cholinergic Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Have potential to cause Anti-DUMBBELSS Xerostomia and constipation (M3) | Solifenacin, Darifenacin, and Trospium are Most selective for M3 and is least likely to cause anti-DUMBBELSS Used to treat overactive bladder |
| Tolterodine (Detrol) | Cholinergic Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Have potential to cause Anti-DUMBBELSS Xerostomia and constipation (M3) | Solifenacin, Darifenacin, and Trospium are Most selective for M3 and is least likely to cause anti-DUMBBELSS Used to treat overactive bladder |
| Fesoterodine (Toviaz) | Cholinergic Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Have potential to cause Anti-DUMBBELSS Xerostomia and constipation (M3) | Solifenacin, Darifenacin, and Trospium are Most selective for M3 and is least likely to cause anti-DUMBBELSS Used to treat overactive bladder |
| Solifenacin (Vesicare) | Cholinergic Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Have potential to cause Anti-DUMBBELSS Xerostomia and constipation (M3) | Solifenacin, Darifenacin, and Trospium are Most selective for M3 and is least likely to cause anti-DUMBBELSS Used to treat overactive bladder |
| Darifenacin | Cholinergic Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Have potential to cause Anti-DUMBBELSS Xerostomia and constipation (M3) | Solifenacin, Darifenacin, and Trospium are Most selective for M3 and is least likely to cause anti-DUMBBELSS Used to treat overactive bladder |
| Trospium | Cholinergic Antagonist | Non-selective Muscarinic antagonist (M1, M2, M3) More selective for M3 | M3 in Bladder | Have potential to cause Anti-DUMBBELSS Xerostomia and constipation (M3) | Solifenacin, Darifenacin, and Trospium are Most selective for M3 and is least likely to cause anti-DUMBBELSS Used to treat overactive bladder |
| Nitroglycerin | Donor | Donate nitric oxide NO--> sGC--> ↑cGMP | Endothelium of blood vessels (M3) | Vasodilation Lower blood pressure | cGMP is a potent vasodilator |
| Nitroprusside | Donor | Donate nitric oxide NO--> sGC--> ↑cGMP | Endothelium of blood vessels (M3) | Vasodilation Lower blood pressure | cGMP is a potent vasodilator |
| Isosorbide di/mononitrate | Donor | Donate nitric oxide NO--> sGC--> ↑cGMP | Endothelium of blood vessels (M3) | Vasodilation Lower blood pressure | cGMP is a potent vasodilator |
| Sildenafil (Viagra) | 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 |
| Tadalafil (Cialis) | 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 |
| Vardenafil | 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, arrythmias, restlessness | Used with Lidocaine to control arrythmias (Na+ channel blocker) |
| Dextroamphetamine & Amphetamine (Adderall) | Adrenergic Indirect Antagonist | Stimulate pre-synaptic release of NE & DA | CNS | HTN, tachycardia, arrythmias, restlessness, loss of appetite | Used for ADHD |
| Methylphenidate (Concerta, Ritalin) | Adrenergic Indirect Antagonist | Stimulate pre-synaptic release of NE & DA | CNS | HTN, tachycardia, arrythmias, restlessness, loss of appetite | Used for ADHD |
| Lisdexamphatamine (Vyvanse) | Adrenergic Indirect Antagonist | Stimulate pre-synaptic release of NE & DA | CNS | HTN, tachycardia, arrythmias, restlessness, loss of appetite | Used for ADHD |
| Dexmethylphenidate (Focalin) | Adrenergic Indirect Antagonist | Stimulate pre-synaptic release of NE & DA | CNS | HTN, tachycardia, arrythmias, restlessness, loss of appetite | Used for ADHD |
| Phenelzine | Adrenergic Irreversible Antagonist | 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 |
| Selegiline | Adrenergic Irreversible Antagonist | SELECTIVE MAO-B irreversible antagonist | CNS | HTN, tachycardia, arrythmias, restlessness | Inhibits breakdown of NE Used for depression & Parkinson’s |
| Rasagiline | Adrenergic Irreversible Antagonist | SELECTIVE MAO-B irreversible antagonist | CNS | HTN, tachycardia, arrythmias, restlessness | Inhibits breakdown of NE Used for depression & Parkinson’s |
| Prazosin | Adrenergic Reversible 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) |
| Terazosin (Hytrin) | Adrenergic Reversible Antagonist | SELECTIVE α1 antagonist reversible 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) |
| Doxazosin (Cardura) | Adrenergic Reversible 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) |
| Tamsulosin (Flomax) --> α1a | Adrenergic Reversible 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 Reversible 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) |
| Clonidine (Catapres) | 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 |
| Brimonidine (Alphagan P) | 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 |
| Tizanidine (Zanaflex) | 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 |
| Guanfacine (Intuniv) | 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 |
| 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 / arrythmias 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 Toprolol) | Adrenergic Antagonist | SELECTIVE β1 antagonist “β1 beta-blockers” | Heart Kidneys Brain | Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression | N/A |
| Atenolol (Tenormin) | Adrenergic Antagonist | SELECTIVE β1 antagonist “β1 beta-blockers” | Heart Kidneys Brain | Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression | N/A |
| Nebivolol (Bystolic) | Adrenergic Antagonist | SELECTIVE β1 antagonist “β1 beta-blockers” | Heart Kidneys Brain | Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression | N/A |
| SABA: Albuterol (Ventolin) | Adrenergic Agonist | β2 agonist | Lungs Vasculature CNS | Bronchial dilation Vasodilation Excitation | N/A |
| SABA: Levalbuterol (Xopenex) | Adrenergic Agonist | β2 agonist | Lungs Vasculature CNS | Bronchial dilation Vasodilation Excitation | N/A |
| LABA: Salmeterol | Adrenergic Agonist | β2 agonist | Lungs Vasculature CNS | Bronchial dilation Vasodilation Excitation | N/A |
| LABA: Formoterol | Adrenergic Agonist | β2 agonist | Lungs Vasculature CNS | Bronchial dilation Vasodilation Excitation | N/A |
| Propranolol (Inderal) | Adrenergic Antagonist | NON-SELECTIVE Beta-blockers β1 & β2 antagonist | 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 (PARTIAL AGONIST) | 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 |
| 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 |
| Carvedilol (Coreg) | 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 |
| 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 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 |
| Norepinephrine (Levophed) | Adrenergic Agonist | α1, β1 agonist | Heart & vasculature | Increase TPR, heart rate, contractility | Used for shock (life support) |
| Isoproterenol | Adrenergic Agonist | β1, β2 agonist (lungs) | Heart & lungs | Hyperglycemia Palpitations Tachycardia Arrythmias | Used for asthma (not 1st line), bradycardia, and heart block (AV) |
| Aliskiren | RAAS REVERSIBLE 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 | RAAS REVERSIBLE Antgonist | 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) Bonus effect 1: Ang 1-->Alt path to Ang 1-7 (binds to AT2 and opposes AT1) Bonus effect 2: Increase levels of bradkykinin-->dry cough (1st line HTN) |
| Enalapril (Vasotec) | RAAS REVERSIBLE Antgonist | 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) Bonus effect 1: Ang 1-->Alt path to Ang 1-7 (binds to AT2 and opposes AT1) Bonus effect 2: Increase levels of bradkykinin-->dry cough (1st line HTN) |
| Lisinopril (Prinivil) | RAAS REVERSIBLE Antgonist | ACE inhibitor Angiotensin converting enzyme inhibitor REVERSIBLE antagonists | Blood Stream | 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 1: Ang 1-->Alt path to Ang 1-7 (binds to AT2 and opposes AT1) Bonus effect 2: Increase levels of bradkykinin-->dry cough (1st line HTN) |
| Benazepril (Lotensin) | RAAS REVERSIBLE Antgonist | ACE inhibitor Angiotensin converting enzyme inhibitor REVERSIBLE antagonists | Blood Stream | 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 1: Ang 1-->Alt path to Ang 1-7 (binds to AT2 and opposes AT1) Bonus effect 2: Increase levels of bradkykinin-->dry cough (1st line HTN) |
| Quinapril (Accupril) | RAAS REVERSIBLE Antgonist | ACE inhibitor Angiotensin converting enzyme inhibitor REVERSIBLE antagonists | Blood Stream | 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 1: Ang 1-->Alt path to Ang 1-7 (binds to AT2 and opposes AT1) Bonus effect 2: Increase levels of bradkykinin-->dry cough (1st line HTN) |
| Ramipril (Altace) | RAAS REVERSIBLE Antgonist | ACE inhibitor Angiotensin converting enzyme inhibitor REVERSIBLE antagonists | Blood Stream | 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 1: Ang 1-->Alt path to Ang 1-7 (binds to AT2 and opposes AT1) Bonus effect 2: Increase levels of bradkykinin-->dry cough (1st line HTN) |
| Losartan (Cozaar) | RAAS REVERSIBLE Antgonist | 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 |
| Valsartan (Diovan) | RAAS REVERSIBLE Antgonist | 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 |
| Olmesartan (Benicar) | RAAS REVERSIBLE Antgonist | 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 |
| Telmisartan (Micardis) | RAAS REVERSIBLE Antgonist | 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 |
| Irbesartan (Avapro) | RAAS REVERSIBLE Antgonist | 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 |
| Medoxomil | RAAS REVERSIBLE Antgonist | 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 |
| Spironolactone | MR 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) and pumps, and these drugs bind to the same space therefore not allowing aldosterone to bind, decreasing the production of channels and pumps. |
| Eplerenone | MR 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) and pumps, and these drugs bind to the same space therefore not allowing aldosterone to bind, decreasing the production of channels and pumps. |
| Metoprolol | RAAS Antagonist | Selective β1 blocker | Kidney | Less renin production -->no RAAS pathway | N/A |
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Rhettstering
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