Pharmacolohy Exam 1--- Cholinergic Pharmacology

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CHOLINE ESTERS

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Acetylcholine
Bethanechol

Hint 1

cholinomimetic drugs (agents thatvdirectly enchance cholinergic function)

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Natural occuring cholingeric stimulants (alkaliods)

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Nitotine
Muscarine
Pilocarpine

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Anticholinestarase agents: Reversible agents

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Physostigmine
Edrophonium
Pyridostigmine (mestinon)
Donepezil

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agents that indirectly increase cholingeric function

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anticholinesterase agents: irreversible agents

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Parathion

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Muscarinic Blocking Drugs

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Atropine
Scopolamine
Tropicamide
Benztropine
Oxybutynin

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Ganglionic Transmission: Stimulants

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Nicotine

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Ganglionic Blockade

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Hexamethonium

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Cholingeric Transmission

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All neurons in the peripheral or central nervous system that releases acetylcholine (ACh) are referred to as cholingeric

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Cholingeric Synapses

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Hemicholinium (HC-3)

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blocks the transport of choline and consequently will eventually cause an inhibition of cholingeric function

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Botulinium toxin

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prevents the release of ACh from nerve terminal. leads to death

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Latrotoxin (blavk widow venom)

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cause excessive fusing of the granules with the nerve membrane that leads to excessive release and eventual depletion of the transmitter

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Muscarinic

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Heart ---- decreases heart rate decrease conduction
Vascular Smooth Muscle --- no effect
Eye ---- myosis (closing of pupil) and cyclotonia (spasm of accommodation)
GI tract --- increase tone and motility, relaxes lower esophagus sphincter
Bronchiolar Smooth Muscle ---- relaxation
Secretory Glands --- causes sweat
CNS

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Nicotinic Receptors

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NMJ
Automonic ganglia
Adrenal medulla- release of ephinephrine and norepinephrine
CNS

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Acetylcholine

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must be injected (intravenously)
not used as a therapeutic agent
(increasr mobility)

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Methacholine

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long duration of action --- used for asthma

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Bethanechol

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well established clinical ultlity
treating postoperative urinary retention anf atony of the GI tract (enzyme breakdown)

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Nicotine

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stimulates all nicotinic receptors
activate all autonomic ganglia and stimulates the skeletal muscles endplate

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Muscarine

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mushroom poisoning
atropine as antidote
stimulate all muscarinic receptors whethrt innervated or noninnervated

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Pilocarpine

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south America shrub
readily crossee membrane barriers
treats glaucoma!!!!

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Anticholinesterase agents

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indirectly enchance cholingeric function
ACh can remain on synapse longer period
effective as antidotes to curare

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ACHASE inhibitors (anticholinestarase)

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reversible
treatment of myasthenia gravis and glaucoma

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Physostigmine

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treatment of atropime posioning and atropine poisoning

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Reversible Agents

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Physostigmine
Pyridostigmine
Edrophonium
Donepezil
Parathon

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Pyridostigmine

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treat myasthenia gravis
long-term process -- patient tolerance or allergies may occur

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Edrophonium

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short duration of action
inhibits ACHASE only for minutes and thus is valuable for the diagnosis of M.G.
May experience skeletal weakness

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Donepezil

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treat cognitive dysfunction seen in patients with Alzheimer's disease

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Parathion

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irreverisble agent
common insecticides

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Muscarinic Blocking Drugs

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lack of motility and secretiond of all parasympathetic innervated organs
alterations of heart rate, mydriasis, and cycloplegia as well as CNS effects

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Atropine

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oral adminstration
poison to children
hot dry skin, dilated pupils and maniacal behavior (RED AS A BEET...HOT AS A PISTOL...DRY AS A BONE...MAD AS A HATTER)

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Scopolamine

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topical administration
prevent motion sickness

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Tropicamide

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used for genersl opthalmological exams for the short duration muscarinic antagonist

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Ipratropium

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applied typically to the airway by means of metered inhaler
COPD --- bronchodilation
bronical asthma
best if combined with other bronchodilators

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Benztropine

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Antimuscarinic drug
Relieve symptoms of Parkinson disease

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Oxybutynin

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treat spasms of the bladder seen after urologic surgery and in some neurological disorders producing bladder hyperactivity

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Ganglionic transmissionv-- Hexamethonium

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experimental tool
blocks all autonomic gangliavbut compete with ACh at the nicotinic receptors found in endplate region of skeletal muscle

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USUAL PREDOMINANCE OF SYMPATHETIC (adrenergic) OR PARASYMPATHETIC (cholinergic) TONE OF VARIOUS EFFECTOR SITES

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