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Brimonidine

(Alphagan)
Selective α1 receptor agonist

-(lower IOP in open angle glaucoma)
Albuterol

(Proventil, Ventolin)
Selective β2 agonist

For bronchospasms, asthma, COPD
Arecoline
Cholinergic alkaloid

-From Betel nut (chewed in Orient)
-Muscarinic ~ Nicotinic
Atracurium

(Tracurium)
NMJ blocker

-Non-depolarizing NMJ blocker
-Relatively short acting
Baclofen

(Lioresal)
Centrally-acting skeletal muscle relaxant

-(GABA agonist)
Acetylcholine
Cholinergic neurotransmitter

-Very short half-life due to rapid hydrolysis
-Formed from ACoA and choline via choline acetyltransferase enzyme
Amphetamine

(Adderall)
Indirect adrenergic agonist

-Stimulates release of catecholamine from monoamine terminal
-Major CNS action, elevation of central DA levels -> positive reinforcement
-(treatment of ADHD)
-(schedule II DEA-controlled agent)
Atenolol

(Tenormin)
β1 receptor antagonist

-Cardioselective, β1 >>> β2
-(treatment of htn, angina)
Atropine

(Atropen, Atropisol)
Muscarinic receptor antagonist

-The major beladonna alkaloid
Doxazosin

(Cardura)
Selective α1 receptor antagonist

-Treatment of BPH
-(treatment of htn)
Verenicline

(Chantix)
Partial nicotinic AChR agonist

-Adjunct in smoking cessation treatment
Hyoscyamine

(Levsin, Anaspaz, Cystospaz)
Muscarinic receptor antagonist

-(for relief of GI spasms, irritable bowel syndome, spastic colon)
-(management of rhinitis, hyperhidrosis)
Pyridostigmine

(Mestinon)
Cholinesterase inhibitor

-Carbamate type of ChE inhibitor
-4° amine does not cross BBB
-Increased muscle tone in myasthenia gravis, reversal of nondepolarizing NMJ blockers
Pseudoephedrine

(Sudafed, Triaminic)
Partial indirect adrenergic agonist

-Part of its action due to release of NE
-Precursor for illegal synthesis of methamphetamine
-Widely used decongestant
Echothiophate

(Phospholine)
Cholinesterase inhibitor

-Treatment of glaucoma
-(organophosphate)
Terazosin

(Hytrin)
Selective α1 receptor antagonist

-Treatment of BPH
-(treatment of htn)
Parathion
Cholinesterase inhibitor

-Prodrug
-Converted into an organophosphate
-Somewhat safe due to inactivation by mammals and birds
-Widely used agricultural insecticide - used in aerial crop spraying, mosquito control
Benztropine

(Cogentin)
Muscarinic receptor antagonist

-(for treatment of Parkinson's disease)
Tyramine
Pure indirect adrenergic agonist

-Not a therapeutic agent
-Natural constituent in some food (high levels in fermented foods)
-Normally inactivated by MAO
-MAO inhibition leads to conversion to octopamine (false transmitter)
-Raises bp if not metabolized.
Timolol

(Timoptic, Istalol, Blocadren, Betimol)
β receptor antagonist

-Nonselective (β1 ~ β2)
-Treatment of glaucoma, elevated IOP
-(treatment of htn, prophylaxis post-myocardial infarction, management of migraines)
Donepezil

(Aricept)
Cholinesterase inhibitor

-Some improvement in cognitive function in Alzheimer's disease
-(noncompetitive ChE inhibitor)
Scopolamine

(Transderm-Scop, Scopace)
Muscarinic antagonist
Selegiline (also named Deprenyl)

(Emsam, Carbex)
Selective MAO-B inhibitor
-Better tolerated than MAO-A inhibitors.

-Adjunct to treat Parkinson's disease
-Decreases incidence of dyskinesias, on-off fluctuations
-Prolongs usefulness of levodopa
Entacapone

(Comtan)
COMT inhibitor

-Adjunct in treatment of Parkinson's disease
-Prevents peripheral metabolism of L-dopa
-Smooths response to L-dopa
Succinylcholine

(Anectine, Quelicin)
Depolarizing neuromuscular blocker

-Depolarizing agent (initial stimulation followed by depolarizing blockade)
-Short acting
-Hydrolyzed by BChE
-Not hydrolyzed by AChE
Pancuronium

(Pavulon)
Neuromuscular blocker

-Long lasting
-Adjunct to general anesthesia, facilitation of tracheal intubation, mechanical respiration
Phentolamine

(Rogitine)
α receptor antagonist

-Nonselective (α1 ~ α2)
Physostigmine

(Eserine)
Cholinesterase inhibitors

-Carbamate type
-3° amine crosses BBB
-(natural alkaloid from Calabar bean)
Pralidoxime
2-PAM

(Propam)
Cholinesterase reactivator

-Only useful with organophosphate poisoning
-Most useful within several hours of poisoning, before aging of the ChE-organophosphate complex
Propranolol

(Inderal)
β receptor antagonist

-Prototype β blocker
-Nonselective (β1 ~ β2)
Phenoxybenzamine

(Dibenzyline)
α receptor antagonist

-Long-acting irreversible inhibitor
-Treatment of pheochromocytoma
-(prodrug)
Phenylephrine

(Neo-synephrine, Phenoptic, Sinex)
α1 receptor agonist
Pilocarpine

(Pilopine, Isopto-Carpine, Ocusert, Piloptic, Pilostat, Salagen, Pilagan)
Muscarinic agonist

-3° amine, crosses membranes well
-Treatment of glaucoma (open and closed angle)
-Treatment of xerostomia
Prazosin

(Minipress)
α1 selective adrenergic receptor antagonist

-(antihypertensive agent)
Reserpine

(Serpasil)
-Used to be used to treat HTN, off market now
-Inhibits transport of monoamine transmitters into synaptic vesicles
-Causes depletion of synaptic vesicle monoamine (NE & 5-HT) stores -> sympatholytic effects
-Crosses BBB -> CNS depression
-Severe depression and suicide
Methyldopa

(Aldomet)
α2 receptor agonist (prodrug)

-Prodrug converted to the active agent (αCH3-NE) in the CNS
-αCH3-NE is a selective α2 receptor agonist
-(antihypertensive agent)
Phentermine

(Fastin, Ionamin)
Partial indirect adrenergic agonist

-Anorexic agent (suppresses appetite)
-Mild psychostimulant
-(DEA Schedule IV substance)
Norepinephrine
Noradrenergic neurotransmitter

-Good α and β1 agonist
-Weak β2
Methylphenidate

(Ritaline)
Indirect adrenergic agonist

-Stimulates release of catecholamine from monoamine terminals
-Somewhat less active than amphetamine
-(treatment of ADHD)
-(Schedule II DEA-controlled agent)
Methoxamine

(Vasoxyl)
α1 selective receptor agonist

-(for rapid increase in BP in hypotensive emergencies)
Neostigmine

(Prostigmin)
Cholinesterase inhibitor

-Carbamate type of ChE inhibitor
-4° amine does not cross BBB
-Increases muscle tone in myasthenia gravis
-Reversal of nondepolarizing NMJ blockers
Nicotine

(Nicotrol, Commit, Nicorette, Habitrol, Nicoderm, Prostep)
Ganglionic > NMJ agonist

-Depolarization blockade at high doses
-Stimulates release of DA in CNS
-Rx for smoking cessation
Octapamine
False transmitter

-Formed from tyramine in the presence of MAOI
-Accumulates in adrenergic synaptic vesicles -> sympatholytic effects, decreased BP
Esmolol

(Brevibloc)
β1 receptor antagonist

-Cardioselective (β1 >>> β2)
-Short acting
-(management of tachycardia)
Labetalol

(Trandate, Normodyne)
Mixed β > α1 receptor antagonist

-(antihypertensive agent)
Mecamylamine

(Inversine)
Ganglionic blocker

-(treatment of severe hypertension)
Methamphetamine
Indirect adrenergic agonist

-Prominent CNS action
-High abuse potential
-Similar to amphetamine but more potent
-Easy synthesis from pseudoephedrine
-(Schedule II DEA-controlled agent)
Guanethidine

(Ismelin, Isimil)
Sympatholytic

-Slow depletion of NE from nerve terminals
-No CNS activity
-(treatment of severe hypertension)
Isoproterenol

(Isuprel, Medihaler)
β receptor agonist

-Management of bronchospasms
Malathion
Cholinesterase inhibitor

-Prodrug
-Converted to an organophosphate
-Somewhat safe due to inactivation by mammals and birds
-Widely used agricultural insecticide - used in aerial crop spraying, mosquito control
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