Cholinergic Drugs Anticholinergic Drugs Drugs Acting on Autonomic Ganglia Adrenergic Drugs Histamine and Anti histaminics 5-Hydroxytryptamine Prostaglandins Nonsteroidal Anti inflammatory Drugs and Antipyretic-Analgesics Anti rheumatoid and Antigout Drugs

1. PHARMACOLOGICAL
CLASSIFICATION
Siddhant S. Bansode
M.Pharm (Pharmacology)

2. Contents:
Cholinergic Drugs
Anticholinergic Drugs
Drugs Acting on Autonomic Ganglia
Adrenergic Drugs
Histamine and Anti histaminics
5-Hydroxytryptamine
Prostaglandins
Nonsteroidal Anti inflammatory Drugs and Antipyretic-Analgesics
Anti rheumatoid and Antigout Drugs

3. CHOLINERGIC DRUGS
Choline esters Alkaloids
Acetylcholine Muscarine
Methacholine Pilocarpine
Carbachol Arecoline
Bethanechol
ANTICHOLINESTERASES
• Reversible:
1. Carbamates:
e.g. Physostigmine (Eserine), Neostigmine, Pyridostigmine,
Edrophonium, Rivastigmine, Donepezil, Galantamine
2. Acridine: e.g. Tacrine
• Irreversible:
1. Organophosphates
e.g. Dyflos (DFP), Echothiophate, Malathion*, Diazinon* (TIK-20),
Tabun£, Sarin£, Soman £
2. Carbamates
e.g. Carbaryl* (SEVIN), Propoxur* (BAYGON)
(note: *Insecticides, £Nerve gases for chemical warfare)
ANTICHOLINERGIC DRUGS (Muscarinic receptor antagonists,
Atropinic, Parasympatholytic)
1. Natural alkaloids: Atropine, Hyoscine
(Scopolamine).
2. Semisynthetic derivatives:Homatropine,
Atropine methonitrate, Hyoscine butyl
bromide, Ipratropium bromide, Tiotropium
bromide.
3. Synthetic compounds:
(a) Mydriatics: Cyclopentolate, Tropicamide.
(b) Antisecretory-antispasmodics:
(i) Quaternary compounds: Propantheline,
Oxyphenonium, Clidinium, Pipenzolate
methyl bromide, Isopropamide, Glycopyrrolate.
(ii) Tertiary amines: Dicyclomine, Valethamate,
Pirenzepine.
(c)Vasicoselective: Oxybutynin, Flavoxate,
Tolterodine.
(d)Antiparkinsonian: Trihexyphenidyl (Benzhexol),
Procyclidine, Biperiden.

4. GANGLIONIC STIMULANTS:
• Selective nicotinic agonists
e.g. Nicotine (small dose), Lobeline
Dimethyl phenyl,
piperazinium (DMPP) Tetramethyl
ammonium (TMA),
Varenicline.
• Nonselective/ muscarinic agonists
e.g. Acetylcholine, Carbachol,
Pilocarpine, Anticholinesterases,
MCN 343-A
GANGLION BLOCKING AGENTS:
A. Competitive blockers
• Quaternary ammonium compounds
Hexamethonium, Pentolinium
• Amines (secondary/tertiary)
Mecamylamine, Pempidine
• Monosulfonium compound
Trimethaphan camforsulfonate
B. Persistent depolarising blockers
Nicotine (large dose)
Anticholinesterases (large dose)

5. ADRENERGIC DRUGS
I. Pressor agents
Noradrenaline, Phenylephrine,
Ephedrine, Methoxamine,
Dopamine, Mephentermine,
II. Cardiac stimulants
Adrenaline, Dobutamine,
Isoprenaline
III. Bronchodilators
Isoprenaline, Salmeterol,
Salbutamol, Formoterol,
(Albuterol), Bambuterol,
Terbutaline
IV. Nasal decongestants
Phenylephrine, Naphazoline,
Xylometazoline, Pseudoephedrine,
Oxymetazoline, Phenyl propanolamine,
V. CNS stimulants
Amphetamine, Methamphetamine,
Dexamphetamine
VI. Anorectics
Fenfluramine, Sibutramine,
Dexfenfluramine
VII. Uterine relaxant and vasodilators
Ritodrine, Salbutamol,
Isoxsuprine, Terbutaline

6. α ADRENERGIC BLOCKING DRUGS
I. Nonequilibrium type
(i) β-Haloalkylamines—Phenoxybenzamine.
II. Equilibrium type (competitive)
A. Nonselective
• (i) Ergot alkaloids—Ergotamine, Ergotoxine
• (ii) Hydrogenated ergot alkaloids—
Dihydroergotamine
• (DHE), Dihydroergotoxine
• (iii) Imidazoline—Phentolamine
• (iv) Miscellaneous–Chlorpromazine
B. α1 selective—Prazosin, Terazosin,
Doxazosin, Alfuzosin, Tamsulosin
C. α2 selective—Yohimbine
β ADRENERGIC BLOCKING DRUGS
Nonselective (β1 and β2)
a. Without intrinsic sympathomimetic
activity
Propranolol, Sotalol, Timolol.
b. With intrinsic sympathomimetic activity
Pindolol
c. With additional α blocking property
Labetalol, Carvedilol
Cardioselective (β1)
Metoprolol, Atenolol, Acebutolol,
Bisoprolol, Esmolol, Betaxolol, Celiprolol,
Nebivolol

7. AUTACOIDS
Amine autacoids: Histamine,
5-Hydroxytryptamine
(Serotonin)
Lipid derived autacoids:
Prostaglandins, Leukotrienes,
Platelet activating factor
Peptide autacoids: Plasma
kinins (Bradykinin, Kallidin),
Angiotensin
HISTAMINERGIC AGONISTS
1. Non selective agonists:
histamine, betahistine
2. Selective H1 agonist: 2-
methyl histamine, 2-pyridyl
ethylamine, 2-thizolyl
ethylamine
3. Selective H2 agonist:
dimaprit, Impromidine
4. Selective H3 agonist: (R) α-
methylhistamine imetit

8. H1 ANTAGONISTS
Highly Sedative: Moderately Sedative: Mildly Sedative: Second Generation
Diphenhydramine Pheniramine Chlorpheniram (Nonsedating) Anti-histaminics:
Dimenhydrinate Cyproheptadine Dexchlorpheniramine Fexofenadine
Promethazine Meclozine Triprolidine Loratadine
Hydroxyzine Cinnarizine Clemastine Desloratadine
Cetirizine
Levocetirizine
Azelastine
Mizolastine
Ebastine

9. PROSTAGLANDINS (PGs)
Natural PGs:
Dinoprostone
Gemeprost
Dinoprost
Alprostadil
Prostacyclin
Prostaglandin Analogues:
Carboprost
Misoprostol
Latanoprost
Travoprost
bimatoprost
5-HYDROXY TRYPTAMINE (5-HT) ANTAGONISTS
1. Nonselective antagonists and partial agonist/antagonist:
Ergotamine
Lysergic acid diethyl (LSD)
2-bromo LSD
Methysergide
Cyproheptadine
Cinnarizine
5-HT2 Antagonists:
Ketanserin, Ritanserin, Clozapine, Risperidone
5-HT3 Antagonists
Ondansetron
Granisetron
Tropisetron
Palonosetron
ramosetron

10. Nonsteroidal Anti inflammatory Drugs and Antipyretic-Analgesics
• A. Nonselective COX inhibitors (traditional NSAIDs):
1. Salicylates: Aspirin.
2. Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen, Flurbiprofen.
3. Fenamate: Mephenamic acid.
4. Enolic acid derivatives: Piroxicam, Tenoxicam.
5. Acetic acid derivatives: Ketorolac, Indomethacin, Nabumetone.
6. Pyrazolone derivatives: Phenylbutazone, Oxyphenbutazone.
• B. Preferential COX-2 inhibitors:
Nimesulide, Diclofenac, Aceclofenac, Meloxicam, Etodolac.
• C. Selective COX-2 inhibitors: Celecoxib, Etoricoxib, Parecoxib.
• D. Analgesic-antipyretics with poor antiinflammatory action:
1. Paraaminophenol derivative: Paracetamol (Acetaminophen).
2. Pyrazolone derivatives: Metamizol (Dipyrone), Propiphenazone.
3. Benzoxazocine derivative: Nefopam.

11. ANTIRHEUMATOID DRUGS
I. Disease modifying antirheumatic drugs
(DMARDs).
A. Nonbiological drugs
1. Immunosuppressants: Methotrexate,
Azathioprine, Cyclosporine
2. Sulfasalazine
3. Chloroquine or Hydroxychloroquine
4. Leflunomide
B. Biological agents
1. TNFα inhibitors: Etanercept, Infliximab,
Adalimumab
2. IL-1 antagonist: Anakinra
II. Adjuvant drugs
Corticosteroids: Prednisolone and others
(Gold and penicillamine are obsolete DMARDs.)
DRUGS USED IN GOUT
For acute gout
NSAIDs
Colchicine
Corticosteroids
For chronic gout/hyperuricaemia
1. Uricosurics
Probenecid
Sulfinpyrazone
2. Synthesis inhibitors
Allopurinol
Febuxostat