PHA 334 ANS Drug Review

Pyridostigmine

◦Treats Myasthenia Gravis

◦Acetylcholinesterase inhibitor

Varenicline

◦Nicotinic receptor AGONIST

Nicotine

◦Nicotinic receptor AGONIST

atropine

ANTAGONIST of muscarinic receptors

scopolamine

ANTAGONIST of muscarinic receptors

hyoscyamine

ANTAGONIST of muscarinic receptors

Darifenacin

◦Muscarinic receptor ANTAGONIST

Methacholine

Muscarinic receptor AGONIST

Xanomeline

Centrally-acting muscarinic receptor AGONIST

Trospium

Peripherally-restricted muscarinic receptor ANTAGONIST

Prazosin

◦Anti-hypertensive

◦a₁ adrenergic antagonist – not selective for a₁ subtypes

Clonidine

◦Anti-hypertensive

◦Reduces sympathetic outflow that leads to decreased release of NE on smooth muscles and heart

◦a₂ adrenergic agonist, centrally-acting

Guanfacine

Anti-hypertensive

Reduces sympathetic outflow that leads to decreased release of NE on smooth muscles and heart

a₂ adrenergic agonist, centrally-acting

Lofexidine

Treatment for opioid withdrawal symptoms, which are mediated by hyperactivation of the SNS

a₂ adrenergic agonist, centrally-acting

Propranolol

Nonselective*, beta-adrenergic receptor-blocker (antagonist)

Mirabegron

Treatment for overactive bladder

b₃–selective agonist

Relaxes muscles in bladder

Pilocarpine

Treats presbyopia/far-sightedness; difficulty with close vision

Contracts ciliary muscles, which bulges lens, and contracts sphincter pupillae muscles, which constricts pupils

◦Muscarinic receptor agonist

Aceclidine

Treats presbyopia/far-sightedness; difficulty with close vision

Contracts ciliary muscles, which bulges lens, and contracts sphincter pupillae muscles, which constricts pupils

◦Muscarinic receptor agonist

Tropicamide

◦Induces mydriasis/pupil dilation for retinal examination

◦Blocks contractions of (i.e., relaxes) sphincter pupillae muscles

◦Muscarinic receptor antagonist

Glycopyrronium

◦Treats hyperhidrosis/excessive sweating

◦Muscarinic receptor antagonist applied locally

Sofpironium

◦Treats hyperhidrosis/excessive sweating

◦Muscarinic receptor antagonist applied locally

Cevimeline

◦Muscarinic receptor agonist

Oxymetazoline

Alpha Agonist

Ipratropium

◦Bronchodilator – treats COPD

◦Muscarinic receptor antagonist

◦Short-acting

Tiotropium

◦Bronchodilator – treats COPD

◦Muscarinic receptor antagonist

◦Long-acting once daily maintenance treatment

Albuterol

◦Bronchodilator – Treatment for bronchospasm (“asthma attack”)

◦b₂–selective agonist

◦Short-acting (SABA)

Formoterol

◦Bronchodilator – Prevention of bronchospasms in COPD and asthma (often in combination with a corticosteroid)

◦b₂–selective agonist

◦Long-acting (LABA)

Fluticasone

◦Anti-inflammatory drug for chronic asthma or COPD

◦Inhaled corticosteroid (ICS)

◦Often used in combination therapy, e.g. fluticasone+salmeterol (beta2 agonist) (Advair Diskus)

Budesonide/Formoterol

◦Approved to treat asthma and COPD

◦ICS (budesonide) plus beta2 agonist (formoterol)

Prazosin

◦Treats hypertension with BPH

◦α1-adrenergic receptor antagonist

◦Vasodilator

Phenoxybenzamine

Treats hypertension with pheochromocytoma

Irreversible α1- (and α2-) adrenergic receptor antagonist

Vasodilator

Labetalol

◦Treats hypertension associated with pre-eclampsia in pregnancy

◦Non-selective b1 and α1 adrenergic antagonist

Also a partial agonist at b2 receptors located in the vascular smooth muscle

Minodrine

◦Treatment of symptomatic orthostatic hypotension

◦Midodrine forms an active metabolite, desglymidodrine, that is an alpha1 (a1) agonist,

◦Exerts its actions via activation of the alpha-adrenergic receptors of the arteriolar and venous vasculature, producing an increase in vascular tone and elevation of blood pressure

◦Desglymidodrine diffuses poorly across the blood-brain barrier, and is therefore not associated with effects on the central nervous system

Norepinephrine

◦Treatment for cardiac arrest and hypotension

◦Peripheral vasoconstrictor via alpha1 (a1) stimulation

◦Inotropic stimulator of the heart and dilator of coronary arteries via activation of beta1- and beta2, respectively

Lisdexamfetamine

◦Treats ADHD

◦NET and DAT (dopamine transporter) substrates (stimulates NE and DA release)

Atomoxetine

◦Treats ADHD

◦Selective NET inhibitor