Contents
Pirbuterol,
Bitolterol,
Salmetrol,
Ritodrine
e. Sele
Prenalterol
6.
Clonidine,
Apraclonidine (used in open angle glaucoma),
Brimonidine,
Dexmetomidine,
Guanabenz,
Guanfaciene
g. D1 agonists
Fenoldopam
Errors and Omissions Accepted.
h. D2 agonists
Bromocryptine
Therapeutic classification Sympathomimetics
Used as bronchodilators
salbutamol,
terbutaline,
salmetrol,
adrenaline,
Used for treatment of anaphylaxis
Adrenaline
Used In the Treatment of Hypotensive Shock
Dopamine,
Methoxamine,
Phenylephrine
Used as cardiac stimulants
adrenaline,
isoprenaline,
dopamine,
Classification of Drugs used for Autonomic Nervous System
dobutamine
Used as nasal decongestants
2.2 Sympathomimetics
phenylephrine,
Catecholamines:
xylometazoline,
1. Natural:
phenylpropanolamine,
naphazoline
Adrenaline
Noradrenaline
Used to prolong the effect of local anesthetics
Dopamine
adrenaline,
2. Semi-Synthetic
phenylephrine
Dobutamine
Used as uterine relaxants
3. Synthetic
salbutamol,
isoxsuprine,
Isoprenaline
ritodrine
Non-Catecholamines
Used in the treatment of narcolepsy
1. Natural
amphetamine,
Ephedrine
methyl amphetamine,
dexamphetamine,
2. Synthetic
ephedrine,
a. Non selective
methylphenidate
modafinil
Amphetamines,
Metamephetamine,
Used as mydriatics
Dextroamphetamine,
adrenaline,
Methyl phenidate
phenylephrine
b. Selective adrenoceptor stimulant
As anorectics
Methoxamine,
amphetamines,
Phenyl ephrine (alpha 1),
fenfluramine,
Metaraminol,
phenmetrazine
Midorine (alpha 1)
Xylometazoline and
Used in open angle glaucoma
oxymetazoline
Dipevefrin,
c. Selective
adrenoceptor stimulants
adrenaline,
apraclonidine,
Orciprenaline
brimonidine
Used in attention deficit hyperkinetic disorder
Salbutamol,
Methylphenidate,
Terbutaline,
amphetamines,
modafinil
2.3 Beta Adrenoceptor Blockers
2.4 Alpha Adrenergic Blockers
According to Pharmacodynamics
1. Selective Alpha Blockers
1. Non-selective (beta1, beta2) blockers:
a. Selective Alpha 1 blockers
Quinazolines
a. Pure Blockers (with no ISA)
Sotalol
Prazosin
Terazosin
Timolol
Doxazosin
Nadolol
Alfuzosin
b. With membrane stabilizing activity (MSA)(local anesthetic activity)
Benzensulfonamide
Propanolol
Tamsulosin (Alpha 1a)
c. With intrinsic sympathetic activity (ISA, partial agonists can activate beta receptors)
b. Selective Alpha 2 blockers
Pindolol (MSA )
Indole
Carteolol
Yohimbine
Penbutalol
d. With ISA and MSA
2. Non-selective (both alpha 1 and alpha 1) blockers
Oxyprenolol
Imidazolines
2. Cardio selective (beta 1 blockers)
Phentolamine
Tolazoline
a. Pure blockers
Haloalkylamines(alpha 1 with some alpha 2 activity)
Atenolol
Bisoprolol (most selective)
Phenoxybenzamine
Esmolol (shortest action)
Dibenamine
b. With MSA
3. Mixed alpha and beta adrenoceptor blocking drugs
Metaprolol
Labetalol
Tolamolol
Carvedilol
Betaxolol
Classification based on Mechanism of Action
c. With ISA
Reversible Alpha Blockers
Practolol (clinically not used now)
Celiprolol
Phentolamine
Prazosin
d. With ISA and MSA
Ergot Alkaloids
Albutolol
Irreversible Alpha Blockers
Beta 2 blockers
Phenoxybenzamine.
Phenoxybenzamine
Butoxamine
Drugs that block both alpha and beta receptors
2.5 Ergot Alkaloids
Labetalol
Derivatives &constituents of ergot
Carvedilol
Bucindolol
1. Amine alkaloids
Based on Pharmacokinetic Pattern
6-methyl ergoline
lysergic acid
Lipid soluble (extensive first pass metabolism)
lysergic acid diethylamide (LSD)
Ergometrine
Propanolol
methysergide
Timolol
Metoprolol
2. Peptide alkaloids
Penbutolol
ergotamine
Water Soluble
alpha ergocryptine
bromocriptine
Nadolol
Atenolol
3. Non-specific constituents
Acebutolol
Acetylcholine
Based on Duration of Action
histamine
tyramine
Ultra short acting Half life
Esmolol
9 minutes
2.6 Parasympathomimetic Drugs
Intermediate acting
A. Directly Acting
Propranol
3 - 5 hours
B. Indirectly Acting
Timolol
3 - 5 hours
A. Directly Acting Cholinergic Drugs:
Pindolol
3 - 4 hours
Metaprolol
3 - 4 hours
I. Choline Esters
Long acting
Acetylcholine
Carbachol
Nadolol
10 - 20 hours
Methacholine
Atenolol
5 - 8 hours
Bethanechol
Bisoprolol
11 - 17 hours
II. Cholinomimetic Alkaloids
Newer Classification
a. Mainly Muscarinic Agonists
1st generation drugs
Natural Alkaloids:
Beta non selective drugs
Muscarine
2nd generation drugs
Pilocarpine
Cardio selective drugs (beta 1 selective)
Arecholine
3rd generation drugs
Synthetic Alkaloid:
Drugs with other activities as well
Oxotramorine
Selective M3 agonists
Cevimeline
b.
Mainly Nicotinic Agonists
2. ALCOHOLS:
Natural Alkaloids:
Edrophonium
Nicotine
Ii.
Irreversible (organophosphate compounds)
Lobeline
1. INSECTICIDES:
Synthetic Alkaloids:
Dyflos
Dimethyl phenyl piperazinium (DMPP)
Diisopropyl fluorophosphates (DFP)
Varenicline
Tetra methyl pyrophosphate (TMPP)
Octa methyl pyrophosphotetraamide (OMPA)
Tertiary alkaloids
Parathion
Pilocarpine
Malathion
Nicotine
2. War gases
Lobeline
Sarin
Quaternary amines
Tabun
Muscarine
Soman
B. Indirectly Acting Cholinergic Drugs (Anticholinesterases)
3.
Therapeutically useful drugs:
I- Reversible
Echothiophate
a. Carbamates
2.8 Anticholinergic drugs
b. Alcohols
Muscarinic Antagonists/Antimuscarinics
II- Irreversible
1. Non-selective
a. Natural
I- Reversible
Atropine
a. Carbamates
Hyoscine (Scopolamine)
b. Semi-synthetic/Synthetic
Tertiary amines
Tertiary amines
Quaternary amines
Physostigmine
2. Selective
Quaternary Ammonium compounds
a. M1 antagonists
Pirenzepine
Neostigmine
Telenzepine
Pyridostigmine
Dicyclomine
Distigmine
b. M2 antagonists
Ambenonium
AF-DX 116
Demecarium
Methoctramine
b. Alcohols
Gallamine
Tripitramine
Edrophonium
Himbacine
c. M3 antagonists (urinary incontinence)
Darifenacin
Oxybutanin
Solefencicin
Tolterodine
c. Miscellaneous
Quaternary amines
Tacrine
Trospium,
Donepezil
Ipratropium,
Galantamine
Propanetheline,
Rivastigmine
Methanetheline,
Glycopyrrolate,
II. Irreversible Anticholinesterases (Organophosphorus Compounds)
Anisotropine,
1. Therapeutically useful:
Isopropamide
Ecothiophate
Tertiary amines
2. War Gases:
Homatropine,
Eucatropine,
Sarin
Tropicamide,
Tuban,
Cyclopentolate,
Soman
Oxybutynin,
3. Insecticides:-
Dicylcomine
Parathion
Therapeutic classification of Anticholinergics
Malathion
Mydriatics
DiisopropylFlurophosphate (DFP)
Tetramethyl Pyrophosphate (TMPP)
Tertiary amines:
Octamethyl Pyrophosphotetraamide (OMPA)
Homatropine,
2.7 Anticholinesterases
hydro bromide,
eucatropine,
A. Centrally Acting (Used for the treatment of Alzh
cyclopentolate,
tropicamide.
Tacrine
Donepezil
Anti Spasmodic
Rivastigmine
Galanthamine
Quaternary ammonium compounds:
B.
Peripherally Acting
Propantheline,
methantheline,
I. Reversible
oxyphenonium,
glycopyrrolate,
1. CARBAMATES:
hyosine butyl bromide
a) Tertiary Amines
Tertiary amines:
Physostigmine
Dicyclomine,
b) Quaternary Ammonium Compounds
oxyphencyclimine,
piperidolateamprotropine,
Neostigmine
oxybutynin chloride
Pyridostigmine
Ambenonium
Distigmine
Demecarium
Anti-Parkinsonian Agent
2. Steroid Derivatives
These are tertiary amines, e.g.
Panuronium
Pipecuronium
trihexyphenidyl,
Rapacuronium
benztropine,
Procuronium
orphenadrine,
Vecuronium
biperidine,
procyclidine,
Depolarizing Neuromuscular Blockers (agonists)
cycrimine,
Suxamethonium
ethopropazine
Suxethonium
Anti ulcer
Decamethonium
Telenzepine,
Centrally acting
Pirenzepine
Benzodiazepines
Anti-Asthmatics
Diazepam,
Ipratropium,
clonazepam,
Oxytropium
Nitrazepam
Pre anesthetics
GABA Analogues
Atropine,
Baclofen
Hyosine,
Progabide
Glycopyronium
Propanediol Derivatives
Motion sickness
Mephenesin
Hyosine
Meprobamate
Urinary Incontinence
Miscellaneous Compounds
Non- selective:
Cyclobenzaprine
Methocarbamol
Trospium
Orphenadrine
Selective M3 antagonists:
Tizanidine
Darifenacin,
DIRECTLY ACTING
Oxybutynin,
Dantrolene
Solefenacin,
Tolterodine
Selective Anti-Muscarinic Drugs
Ipratropium
Oxitropium
Oxybutynin
Tolterodine
2.9 Adrenergic Neuron Blockers
Classification of Drugs used for Cardiovascular System
Drugs which prevent release of noradrenaline
3.1 Drugs used in cardiac failure
Guanethidine
a. Diuretics (alone or with K+ sparing diuretics)
Guanadrel
i. Thiazides
Bethanidine
Debrisoquine
Bendrofluazide,
Bretylium
polythiazide
Drugs that inhibit storage of noradrenaline
ii. Loop diuretic
Reserpine
Frusemide
Drugs that interfere with synthesis of noradrenaline:
b. ACE inhibitors
Metyrosine
Captopril,
enalapril etc
2.10 Central Sympathoplegics
c. ARBS
Alpha methyldopa (Aldomit)
Losartan,
Clonidine
valsartan etc
Apraclonidine
d. Cardiotonic drugs
Cardiac glycosides
Brimonidine
Digoxin,
Guanfacine
digitoxin
Guanabenz
Bipyridine derivatives
2.11 Skeletal muscle relaxants
Inamrinone,
milrinone
Peripherally acting
1 selective agonists (Catecholamines)
Non Depolarizing Neuromuscular Blockers
1. Isoquinoline Derivatives
Dobutamine,
prenalterol
d-Tubocurarine
Atracurium
e. Vasodilators
Nitrates
Cisatracurium
Doxacurium
f. Blockers
Mivacurium
Metocurium
Carvedilol,
metoprolol etc.
Miscellaneous
Gallamine