Drug



|Drug |Class |Uses |Side effects |Features |

| | | | | |

|Cholinergic Agonists |

|Acetylcholine |Non-selective M & N |NONE |PNS effects |NOT effect PO, shortest |

| | | | |duration (plasma ChE) |

|Carbachol |M-agonist (ester) |Miosis, (IOP |PNS & ganglia (N) effects |Longer-acting (resistant to |

| | | | |both AChE) |

|Bethanechol |Selective M3-agonist (ester) |Urinary retention, GI atony |PNS effects (NOT heart) |Long-duration (NO ChE) |

|Pilocarpine |Selective M-agonist (alkaloid) |DOC for emergency (IOP |PNS effects (especially sweating) |Crosses BBB, NO ChE |

| | |miosis, accommodative spasm | | |

| | | | | |

|Cholinesterase Inhibitors |

|Physostigmine |Natural (Calabar bean); |Miosis, (IOP (wide-angle |PNS, SNS, NMJ, CNS effects |Crosses BBB (3° amine) |

| |Reversible |glaucoma), antidote to Atropine | | |

| | |poisoning | | |

|Neostigmine |Synthetic |Bladder & GI atony (myasthenia |PNS, SNS & NMJ effects |NOT cross BBB (4° amine) |

| |Reversible |gravis) | | |

|Edrophonium |Neostigmine w/o carbamyl |Reverses NMJ blockers; Dx test for|PNS, SNS & NMJ effects |NOT cross BBB; extremely |

| |Reversible |myasthenia gravis | |short-acting |

|Isoflurophate (DFP) |Irreversible (organophosphate) |Prolonged miosis |PNS, SNS, CNS, NMJ effects |Crosses BBB (lipid soluble) |

|Echothiophate | |Glaucoma (risk of cataracts) | |Long-duration |

|Parathion |Irreversible (organophosphate) |Insecticide (accidental |PNS, SNS, CNS, NMJ effects |Crosses BBB (lipid soluble) |

| | |poisonings) | | |

|Soman |Irreversible (organophosphate) |Nerve gas |PNS, SNS, CNS, NMJ effects |Crosses BBB |

| | | | | |

|Muscarinic Antagonists |

|Atropine |Natural alkaloid (A. belladonna &|Inhibit PNS & CNS; antidote to |(intraocular pressure in |Mad, hot, blind, red, dry |

| |Jimson weed); 3° amine; |AChE inhibitors |narrow-angle glaucoma |7d duration! |

| |non-selective | | | |

|Scopolamine |Natural alkaloid; 3° amine |Motion sickness (slow-release |CNS depression |Same as Atropine BUT > CNS, |

| | |transdermal patch) | |eye, (secretions |

|Pirenzepine |Selective M1-antagonist |Peptic ulcers (synergy w/ |NO CNS or heart effects |M1>M3>>M2 |

| | |H2-antagonists | |(gastric acid w/o (HR |

|Benztropine |Non-selective |Adjunct w/ L-Dopa for Parkinson’s | |Crosses BBB |

| | |Rx | | |

|Propantheline |4° amine; non-selective |(GI motility, GU incontinence, |NO CNS effects |NOT cross BBB |

|Glycopyrrolate | |(secretions | | |

|Ipratropium |Non-selective; inhaled |Adjunct prevents vagal |Minimally absorbed from lung |NOT cross BBB |

| | |bronchoconstriction (COPD) | | |

|Cyclopentolate |6-24h duration |Mydriasis & cycloplegia |Minimally absorbed from eye | |

|Tropicamide |1-3h duration | | | |

| | | | | |

|Ganglionic (Nicotinic) Blocker |

|Hexamethonium |Selective, competitive |Immediate (BP & blood loss |Orthostatic hypotension |NOT cross BBB (4°); excreted |

|Trimethaphan |Short-acting | | |unchanged |

| | | | | |

|NMJ (Nicotinic) Blockers |

|Succinylcholine |Depolarizing; 2ACh joined | |Hyperkalemia (deep muscle pain), |NOT reverse w/ AChE inhibitor |

| |Short-term ((1>() |(+)inotropism ((CO w/o (HR) |(high dose) | |

|Dobutamine |(1-agonist |CHF ((contractility w/o (HR) |Arrhythmias (high dose) |Racemic mixture |

| | |Small (BP & TPR | |NOT orally active |

|Albuterol |(2-agonist, inhaled |Asthma, chronic bronchitis, |Minimal (low absorption) | |

| | |premature labor (relax SM) |Tremor, (HR (high dose) | |

|Phenethylamines |Direct (1-agonists |Hemorrhage, hypotension, Mydriasis| |Pseudoephedrine |

|Phenylephrine |(structural analogs of Epi) |(w/o cycloplegia) | | |

| | |(IOP, nasal decongestion, | |(BP ( activates M-receptors ( |

| | |atrial tachycardia | |(HR (vagal) |

|Imidazolines |Direct (1-agonists | | | |

| |(unrelated to Epi) | | | |

|Cocaine |Indirect (1-agonist |HTN, depression, local anesthetic | |Blocks NE reuptake |

|Amphetamines |Indirect (1-agonists |Local anesthetic, appetite |Euphoria, (BP, arrhythmias, HTN, |Promotes NE release & blocks |

| | |suppression, narcolepsy, ADHD |psychosis, convulsion, |reuptake |

| | | |tachyphylaxis | |

|Monoamine oxidase |Indirect (1-agonists |HTN & depression |Hypertensive crisis (w/ |Tranylcypromine |

|inhibitors (MAOIs) | | |Amphetamines) |Inhibits degrading NE on |

| | | | |mitochondrial membrane |

| | | | | |

|Sympatholytics |

|Methyldopa |(2-agonist |(TPR ((SNS thru receptors in NTS) | |Prodrug converted in nerve |

| | | | |terminal to (-methylNE |

|Clonidine |(2-agonist |Opiate & nicotine withdrawal, |Sedation, dry mouth, hemolytic | |

| |(most commonly used) |vascular headaches, |anemia | |

| | |HTN (2nd-line), ulcerative | | |

| | |colitis, Tourette’s | | |

|Apraclonidine | |(aqueous humor production | | |

|Tamsulosin |Selective (1A-antagonists |Benign prostatic hyperplasia (w/o | | |

|Prazosin |Competitive |causing hypotension) | | |

|Phentolamine |Non-selective (1-antagonist |Pheochromocytoma, HTN, (HDL, (LDL |Edema, 1st-dose syncope, postural |Combine w/ diuretic |

| | | |hypotension | |

|Phenoxybenzamine |Non-selective, irreversible |Pheochromocytoma, HTN, (HDL, (LDL |Same as above |Combine w/ diuretic |

| |(1-antagonist | | | |

|Propanolol |Non-selective (-blocker |Ischemic heart dz, HTN, CHF, |Exacerbate airway & peripheral |(HR, (contractility, |

| | |arrhythmias |vascular dz, glucose dysregulation|blocks renin secretion |

|Timolol | |(aqueous humor production |((2) |Contraindicated in DM |

|Metoprolol |Selective (1-blocker |Ischemic heart dz, HTN, CHF, |Sedation, fatigue, hypotension, | |

| | |arrhythmias |bradycardia, (TGs, (HDL | |

|Labetalol |Non-selective |CHF (reverses hypertrophy) |Orthostatic hypotension, fatigue, | |

|Carvedilol |( & (-blockers | |sedation | |

|Reserpine |Non-selective | |Hypotension, insomnia, sedation, |Destroys storage granules & |

| |( & (-blocker | |depression |depletes NE |

|Guanethidine |Blocks Ca2+-dependent release of | |Hypotension, bradycardia | |

| |NE | | | |

| | | | | |

|Asthma |

|Salmeterol |(2-agonist, inhaled |Nocturnal asthma prophylaxis, | |Inhaler off market, now |

| |Slow-onset, long-acting |adjuvant to ICS | |combined w/ Fluticasone |

|Beclomethasone |Inhaled corticosteroids (ICS) |Asthma prophylaxis |Candidiasis (reduced w/ spacers) |Expensive |

|Fluticasone | |((COX-2 & PA2) |Minimal (low absorption) |Different strengths |

| | | | |Monitor growth in kids |

|Prednisone |Oral corticosteroids |Short-term “burst” therapy w/ |Adrenal suppression (long-term), |Cheap |

|Prednisolone | |severe exacerbations |weight gain, poor glucose control,| |

| | | |CNS effects, osteoporosis | |

|Hydrocortisone |Parenteral corticosteroids |Status asthmaticus (reduce late | | |

| | |phase response) | | |

|Cromolyn |Mast-cell stabilizer |Asthma prophylaxis |Essentially NONE |Must give 4X daily |

|Nedocromil | |(NOT effective in all patients) | |Longer acting (tid) |

|Theophylline |Bronchodilator |Adjunct for severe asthma |Narrow therapeutic index, tremors,|Many drug interactions |

|Aminophylline |Limited hanti-inflammatory |Nocturnal asthma in kids, COPD |seizures, diuresis, hyperglycemia,| |

| | | |(HR | |

|Zafirlukast |Leukotriene-receptor antagonists |Asthma prophylaxis, adjuvant to |Unknown |Inhibit p450 in liver |

|Montelukast | |ICS | |NO food or liver interaction |

|Zileuton |5-lipoxygenase inhibitor |Asthma prophylaxis, cold |Unknown | |

| |((leukotriene synthesis) |air-induced asthma | | |

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