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Steps in autonomic transmission: Effects of some drugs. (Transmitter…
Steps in autonomic transmission: Effects of some drugs.
Transmitter release
cholinergic
Cholinergic vesicles Prevents ACh release
adrenergic
amphetamine, tyramine, ephedrine Promote transmitter release
Enzymatic inactivation
of transmitter
cholinergic
SHORT-ACTING CHOLINESTERASE INHIBITOR (ALCOHOL)
Edrophonium
Tacrine, Donepezil
INTERMEDIATE-ACTING CHOLINESTERASE INHIBITORS (CARBAMATES)
Don't cross BBB: Neostigmine, Pyridostigmine, Ambenonium
Cross BBB: Rivastigmine, Galantamine, Physostigmine
insecticides: aldicon, proponer, carbaryl
LONG-ACTING CHOLINESTERASE INHIBITORS (ORGANOPHOSPHATES)
Echothiophate, Malathione, Parathione, Isoflurophate
Chemical weapons: Soman, VX, Sarin
adrenergic
Monoamine Oxidase Inhibitors: Tranylcypromine
Catechol-O-methyl transferase (COMT) Inhibitors: entacapone and tolcapone
Receptor activation
or blockade
Cholinoceptor
Activating
DIRECT-ACTING MUSCARINIC ALKALOIDS OR SYNTHETICS
Pilocarpine
Cevimeline: M-3 selective
DIRECT-ACTING NICOTINIC AGONISTS
Leboline
DIRECT-ACTING ESTERS
Carbamic Esters
Carbachol: Nonselective muscarinic and nicotinic
Bethanechol: Muscarinic
Choline Esters
MetaCh: Muscarinic
ACh: Nonselective muscarinic and nicotinic
Blocking
muscarinic
non-selective
Nitrogen 3
Atropine, (، propiverine ،oxybutynin ،propantheline?) ،Scopolamine ،Homatropine ، Dicyclomine, (clidinium, hyoscine?), Cyclopentolate Benztropine ،Biperiden ،Trihexyphenidyl
Nitrogen 4 (only peripheral)
Methyl scopolamine, Methylatropine, Clidinium, Ipratropium,
(Tiotropium?)،Propantheline ، Glycopyrrolate
selective
M1: Telenzepine ، Pirenzepine
M2: Himbacine ، Methocramine
nicotinic
Neuromuscular junction blockers
Ganglion blockers
Adrenoceptor
Agonist
beta
2
Albuterol
3
Mirabegron
1
Dobutamine
1 + 2: :isoproterenol; salbutamol + albuterol + terbutaline (b2>>b1)
dopamine
1
Fenoldopam
2
Bromocriptine
alpha
1
Midodrine
2
Clonidine
1 + 2: phenylephrine + :)methoxamine (both a1>a2)
Antagonist
alpha
non-selective
irreversible, long lasting: phenoxybenzamine
reversible, short: phentolamine + tolazoline
selective
1: tamsulosin ،doxazosin ،terazosin ،prazosin ،indoramin
2: rauwolscine ،yohimbine
beta
1st generation (classical non-selective): propranolol, timolol, nadolol
2nd generation (β 1 selective): metoprolol, atenolol
3rd generation
non -selective β-blockers with additional action: carvedilol (antioxidant activity), labetolol (a1 R antagonist), tilisolol (K channel opening)
β1-selective blockers with additional action: celiprolol (b2 R agonist), betaxolol (Ca entry blockade)
partial agonist: penbutolol ،pindolol ،acebutolol
Action potential
propagation
Transmitter synthesis
cholinergic
Hemicholiniums: Block uptake of choline
adrenergic
metyrosine: Inhibits tyrosine hydroxylase
Transmitter storage
cholinergic
Vesamicol: VAT on vesicles Prevents storage
adrenergic
Reserpine: VMAT on vesicles Prevents storage
Transmitter reuptake
after release
adrenergic
Cocaine, tricyclic antidepressants: Inhibit uptake
cholinergic