Sympthatic pharmacology

1. Pharmaceutical Chemistry-I Dr. Sultan Al-Kaleh
Pharmacy Students (2nd level) Aljazeera University
Autonomic Nervous System Drugs (ANS)
1-Sympathetic (Adrenergic) 2-Parasympathetic (Cholinergic)
Agonist
(Sympathomimetics)
Antagonist (blocker)
(Sympatholytics)
Agonist
(Parasympathomimetics)
Antagonist
(Parasympatholytics)
Direct
Indirect Mixed   Adrenergic Neuron Direct[1] Indirect[2]
(Anticholinesterase) Natural
Semi-
synthetic
Synthetic
Non-
specific
Specific
-Adrenaline
-N.E
-Dopamine
1:
-Phenylephrine
-Methoxamine
-Naphazoline
-
Tetrahydrazoline
-Xylometazoline
-Oxylometazoline
2:
1- α-methyl dopa
2. Clonidine
3-Apraclonidine
4-Guanfacine
5-Guanbenz
1
1-Dobutamine
2-Prenalterol
2
1-Salbutamol
2-Terbutaline
3-Hexoprenaline
4-Fenoterol
5-Salmetrol
6-Formoterol
7-Ritodrine
1,2,3
Isoprenaline
Drugs:
- Amphetamines
-Methylphenidate
-Mazindol
Drugs:
-Ephedrine
-Pseudoephedrine
-Metaraminol
-Mephenteramine
Selective Non-selective Selective
Non-
selective Central Peripheral
Natural
-Acetylcholine
-Pilocarpine
-Muscarine
-Arecoline
Synthetic:
-Methacholine
-Carbachol
-Bethanechol
-Trimorine
-Oxotrimorine
- Cevimeline
Reversible ACE (-):
Short-acting:
-Edrophonium
Medium-acting:
-Neostigmine
-Physostigmine
-Pyridostigmine
-Ambenonium
-Demecarium
With selective CNS
effect:
-Donepezil
-Galantamine
-Rivastigmine
-Tacrine
Irreversible ACE (-):
Organic phosphor:
-Echothiophate
-Isoflurophate/DFP
-Dyelos
-Nerve gases
e.g. Tabun, sarin, soman
Insecticides:
-Malathion
-Parathion
Alkaloids:
1-Atropine
2-Hyoscine
(Scopolamine)
Drugs:
-Homatropine
methylbromide
-Hyoscine butylbromide
-Eucatropine HCL
Mydriatics:
-Tropicamide
-Cyclopentolate
Antisecretory,antispasmodics
1-Quaternary compounds:
-Clidinium
-Propantheline
-Glycopyrrolate
2-Tertiary amines:
-Pirenzepine
-Telenzepine
-Oxybutynine
-Dicylomine
Anti-parkinsonism
-Trihexophenidyl(benzhexol)
-Procyclidine
-Benztropine
-Biperiden
Used in (COPD)
-Ipratropium
1 2 α 1,2 1 2 β1,2
Drugs:
-Prazocin
-Trimazocin
-Indoramin
-Terazocin
-Doxazosin
-Tamsulosin
-Ketanserin
-Uropidil
Yohimbine
Competitive:
1-Ergot alkaloids:
-Ergotamine
-Ergotoxin
2-Hydrogenated ergot
alkaloid:
-Dihydroergotamine
-Dihydroergotoxine
3-Imidazolines:
-Tolazolamine
-Phentolamine
4-Phenothiazines:
-Chlorpromazine
Non-competitive:
-Phenoxybenzamine
-Dibenzamine
1-Without
I.S.A:
-Metorolol
- Atenolol
- Esmolol
- Betaxolol
2-With I.S.A:
- Acebutolol
Butoxamine
1-Without I.S.A:
-Propranolol
-Nadolol
-Timolol
2-With I.S.A:
-Pindolol
-Oxprenolol
-Alprenolol
3-With additional
-blocking
activity:
-Labetalol
Drugs:
- α-methyl dopa
- Reserpine
- Clonidine
Action:
Act  V.M.C 
V.D
Drugs
- Guanethidine
Action:
V.D
[1] Specific stimulation of muscarinic receptors directly [2] Anticholinestrase I.S.A: Intrinsic sympathomimetic activity N.E: Nor-epinephrine (noradrenalin) V.M.C: Vasomotor center
V.D: Vasodilatation DFP: Diisopropyle fluorophosphates
Receptors
α (stimulation) β (stimulation)
α1 α2 β1 β2 β3
Action
1- Erection of hair
2- Mydriasis
3- Vasoconstriction of blood vessels
4 - Spasm of sphincters of GIT & UT )
1- Inhibit sympathetic activity in CNS
2- Decrease noradrenaline release
3-Decrease insulin release
4- Increase platelet aggregation 
clotting
1-CNS stimulation
2 -Cardiac stimulation
-Tachycardia
- contractility
- conductivity
- excitability
3-Release of rennin from kidney  B.P
4-Lipolysis
1-Vasodilatation of blood vessels in
skeletal muscles.
2-Bronchodilation
3- insulin release  hypoglycemia
4-Relax walls of GIT & UT
1- lipolysis