Cholinergic Pharmacology Drugs

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Acetylcholine(Metacholine)

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Class:Muscarinic Receptor Agonist
Mech:rapid induction of miosis
Use:ophthalmic solution
Side Effects:limited clinical use b/c rapidly metabolized by AChE

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Bethanachol

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Class:Muscarinic Receptor Agonist
Mech:resistant to AChE, longer half-life than ACh
Use:1. Stimulate tone and motility in the G.I. tract, use to treat post op abdominal distention and atony and congenital megacolon. 2. Stimulate urinary bladder motility. 3. May be used as an oral Tx for xerostomia-dry mouth
Side Effects:bronchioconstriction, sweating, flushing, salivation, belching,

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Carbachol

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Class:Muscarinic and Nicotinic Receptor Agonist
Mech:not a substrate for AChE, can stimulate autonomic ganglia, limited clinical use b/c of non-selectivity
Use:Glaucoma, produces miosis to help relieve intraocular pressure
Side Effects:

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Pilocarpine

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Class:Muscarinic Receptor Agonist
Mech:Can penetrate CNS, resistant to hydrolysis via AChE
Use:1.Glaucoma-topical administration lowers intraocular pressure by contrxn of ciliary muscle. 2. xerostomia-preferred drug
Side Effects:sweating up to 2-3 liters/day

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Neostigmine (+Pyridostigmine)

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Class:AChE Inhibitor
Mech:does not cross CNS, affects NMJ preferentially
Use:1. GI tract- enhances contrxns and stimulates motor activity of intestines and stimulates secretions. 2. Glaucoma produces miosis to lower intraocular pressure 3. Myasthenia Gravis- increase conc. of ACh thereby allowing more stimulation of the limited Nm Receptors. 4. Neuromuscular blockade-restores muscle function post op in surgeries where blockade used
Side Effects:Blocks accommodation, can cause depolarization blockade
Pyridostigmine has same effects with longer half life

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Physostigmine

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Class:AChE Inhibitor
Mech:Can enter CNS,
Use:1. Reverse effect of centrally acting muscarinic antagonist. 2. reverse sedative actions of diazepam
Side Effects:

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Edrophonium

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Class:AChE Inhibitor
Mech:Alcohol-fast onset of inhibition, brief duration of action
Use:differential diagnosis of Myasthenia Gravis- can rapidly and transiently increase muscle tone and contrxn
Side Effects:

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Echothiophate

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Class:Irreversible AChE inhibitor
Mech:Organophosphorous compound, irreversibly inhibits AChE and has limited clinical use
Use:Glaucoma-used only after other treatments have failed
Side Effects:

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Atropine

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Class:Muscarinic Receptor Antagonist
Mech:Prototypical Muscarinic Antagonist, bind Muscarinic Rs and blocks cholinergic stimulation,
1. Smooth muscle relaxation. 2. Tachycardia 3. inhibition of glandular secretion
Use:Eye-produces mydriasis(for eye exam). 2. Respiratory tract-prevents mucous prodxn- used during surgeries. 3. Heart-produces tachycardia. 4. GI tract- inhibits GI motility. 5. Urinary- increase capacity of bladder to treat overactive bladder. 6 Anti-AChE poisoning- from overdose of AChE inh.
Side Effects:At high doses can enter the CNS and cause restlessness, confusion, hallucinations, and delirium, dry mouth and constipation

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Scopalamine

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Class:Muscarinic Receptor Antagonist
Mech:Similar to atropine
Use:prevent motion sickness
Side Effects:

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Ipratropium

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Class:Muscarinic Receptor Antagonist
Mech:Inhaled- to reduce respiratory tract excretions.
Use:COPD
Side Effects:

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Tiotropium

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Class:Muscarinic Receptor Antagonist
Mech:inhaled as dry powder-reduce mucous secretions
Use:COPD-last longer than Inpratropium
Side Effects:

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Pirenzepine

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Class:Muscarinic Receptor Antagonist
Mech:Higher affinity for M1, reduces gastric acid secretions
Use:Tx of GI ulcers
Side Effects:

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Tolterodine

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Class:Muscarinic Receptor Antagonist
Mech:Selective for M3- urinary bladder
Use:Tx for urinary incontinence/overactive bladder
Side Effects:

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Oxybutynin

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Class:Muscarinic Receptor Antagonist
Mech:Selective for M3 Rs, targets bladder.
Use:Tx of overactive bladder, decrease bladder contractility
Side Effects:

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Nicotine

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Class:Nicotinic Receptor Agonist
Mech:Stimulates all autonomic ganglia-low doses can facilitate impulses but at high doses can blockade of neurotransmission, can also stimulate epi release from medulla, also can stimulate muscle activity at NMJ
Use:No clinical use, in cigarettes
Side Effects:

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Varenicline

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Class:Nicotinic R agonist
Mech:
Use:to help stop smoking cessation
Side Effects:

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d-Tubocurarine

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Class:Non-depolarizing NMJ blockers
Mech:Binds and blocks Nm activation
Use:in surgery-relax skeletal muscle
Side Effects:may cause Histamine release and bronchospasm, Hypotension

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Doxacurium

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Class:Non-depolarizing NMJ blockers
Mech:blocks Nm and prevents its activation
Use:Surgery to relax skeletal muscle-longer acting that tubocurarine
Side Effects:

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Rocuronium

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Class:Non-depolarizing NMJ blockers
Mech:binds and blocks Nm Receptor-very fast acting
Use:relax skeletal muscle
Side Effects:no histamine release

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Atracurium

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Class:Non-depolarizing NMJ blockers
Mech:blocks Nm
Use:relax skeletal muscle
Side Effects:

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Mivacurium

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Class:Non-depolarizing NMJ blockers
Mech:very short duration of axn,
Use:relax skeletal muscle
Side Effects:

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Succinylcholine

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Class:Depolarizing NMJ blockers
Mech:Short duration(5 min)- severe muscle contrxns first followed by relaxation
Use:surgery
Side Effects:1. hyperkalemia 2. myalgia. 3. Ganglionic stimulation-bradycardia. 4.Malignant hyperthermia

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Diazepam

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Class:Muscle relaxant
Mech:stimulate GABA Rs
Use:reduces muscle tone, reduce muscle spasm
Side Effects:sedation

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Baclofen

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Class:Muscle Relaxant
Mech:binds and stimulates presynaptic GABAb Rs- reduces excitory signals from brain
Use:muscle relaxant
Side Effects:less sedation than diazapam

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Dantrolene

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Class:Muscle relaxant
Mech:Inhibits Ca relase from sarcoplasmic reticulum,
Use:Tx of malignant hyperthermia
Side Effects: