Download Pharmacology is hard and easy subject and more Cheat Sheet Pharmacology in PDF only on Docsity! Prepared By: Nehal V. Trambadiya Asst. Professor Smt. N. M. Padalia Pharmacy College ļ¬ Conventionally, anticholinergic drugs are those which block actions of ACh on autonomic effectors and in the CNS exerted through muscarinic receptors. ļ¬ Though nicotinic antagonists also block certain actions of ACh, they are generally referred to as āganglion blockersā and āneuromuscular blockersā. ļ¬ Atropine, the prototype drug of this class, is highly selective for muscarinic receptors Tertiary amine: -Dicyclomine -Oxybutynin -Flevoxate -Pirenzepine -Telenzepine c) Antiparkinsonian: - Benzhexol -Procyclidine -Biperiden -Benzatropine -Cycrimide -Ethopropazine Atropine: B.S: Atropa belladonna Family: Solanaceae L-isomer is more potent than d-isomer Mode of action:
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3) Gastro intestinal tract: -Small dose ļ decrease gastric acid secretion and reduction motor activity of intestine. -Relaxes the gall bladder and bile duct. 4) Smooth muscle: -Relaxes bronchi and bronchioles ļ resulting widening of the airway. -Bronchial secretion are dried up ļ lead to mucous plug formation and obstruction. -Ureter ļ Tone and contraction is decreases. -Detrusor muscle of bladder is relaxes. ļ¬ urinary retention can occur in older males with prostatic hypertrophy 5) Effect on secretion: -Markedly decrease the sweat, salivary, tracheobronchial and lachrymal secretion by M3 receptor blocking. (Hexahydrosiladifenidol, Darifenacin) -Skin and eye become dry. -Talking and swallowing become difficult. 6) Effect on eye: -Intrinsic muscle of eye have a dual nerve supply. 1) Parasympathetic ļ carried via oculomotor nerve ļ stimulate the constrictor (sphincter) pupillae ļ miosis. 2) Sympathetic ļ carried via superior cervical ganglia ļ stimulate the dilator pupillae ļ mydriasis. ļ¬ Mydriasis produces by atropine pushes the mass of iris muscle against the cornea and blocking the cornea iris angle where drainage canal of schelmm lies ļ reduces the efficacy of drainage of ciliary fluid ļ IOP rises ļ Glaucoma. 7) Body temp: -On higher dose ļ body temp. rises due to inhibition of sweating as well as stimulation of temp. regulating center in the hypothalamus. Adverse effects: Dryness of mouth and throat Skin is dry, hot and red Body temp. rise Blurred vision due to paralysis of accommodation Urinary retention Tachycardia and palpitation Constipation Atropine / belladonna poisoning: Due to over dose of atropine (1gm) ļ¬ Symptoms: Severely dryness of mouth Wide pupillary dilatation Dysphasia Tachycardia Redness of skin, Rise body temp. Muscle inccordination Delirium, hallucination Stupor, coma Respiratory collapse ļ¬ Diagnosis Methacholine 5 mg or neostigmine 1 mg s.c. fails to induce typical muscarinic effects. Drug Rout Dose Use Hyoscine butyl bromide Oral 20-40 mg Esophageal and gastrointestin al spastic condition Atropine methonitrate Oral 2.5-10 mg Bronchial asthma and asthmatic bronchitis Ipratropium bromide Inhalation 40-80 Āµg COPD Propanthelin Oral 15-30 mg Peptic ulcer and gastritis Oxyphenonium oral 5-10 mg Peptic ulcer and gastrointestinal hyper motility Clidinium oral 2.5-5 mg Peptic ulcer, irritable colon nervous dyspepsia Pipenzolate methyl bromide oral 5-10 mg Infantile colics, gastrointestinal spasm Isopropamide oral 5 mg Hyper acidity nervous dyspepsia, irritable bowel Glycopyrolate Oral I.V. 1-2 mg 0.1- 0.2mg Preanesthetic medication DRUGS ACTING On AUTONOMIC GANGLIA ļ¬ Acetylcholine is the primary excitatory neurotransmitter in both sympathetic and parasympathetic ganglia. ļ¬ Drugs which inhibit synthesis (hemicholinium) or release (botulinus toxin, procaine) of ACh can interfere with ganglionic transmission, but drugs which act on cholinergic receptors in the ganglia are more selective. ļ¬ Drugs can either stimulate or block the ganglia ļ¬ Ganglionic stimulants ļ¬ Selective nicotinic agonists ļ¬ Nicotine (small dose) ļ¬ Lobeline, Dimethyl phenyl piperazinium (DMPP) ļ¬ Nonselective/muscarinic agonists ļ¬ Acetylcholine ļ¬ Carbachol ļ¬ Pilocarpine ļ¬ Nicotine (from Nicotiana tabacum) is important in the context of smoking or chewing tobacco, but there is no clinical application of ganglionic stimulant ļ¬ Nicotine transdermal has recently become available for treatment of nicotine dependence and as an aid to smoking cessation Newer drugs: Tripitamine:- -Newer m2 selective antagonist. -Use in treating vagal bradycardia Derifenacin:- -m3 selective antagonist -Use in smooth muscle, glandular overactivity disorder Drotaverine:- novel anticholinergic smooth muscle antispasmodic which act by inhibiting phosphodiesterase-4(PDE-4). -Elevation of intracellular cAMP/ cGMP ļ smooth muscle relaxation