Documente Academic
Documente Profesional
Documente Cultură
Synthetics
Mydriatic Cyclopentolate, Homatropine Anti-parkinsonism Benztropine (tertiary amine) Anti-asthmatic Ipratropium, Tiotropium (quaternary amine) GIT and Genitourinary Tertiary amines Pirenzepine, Telenzepine, Dicyclomine, Darifenacin, Solifenacin, Oxybutynin, Tolterodine quaternary amines Glycopyrrolate, Trospium, Oxyphenonium, Isopropamide
Absorption
Tertiary amines, well absorbed from gut and membranes In quaternary amines after oral administration only 10-30% of drug absorbed
Distribution
Well distributed, Tertiary amines penetrate CNS Quaternary amines poorly taken up by CNS
Heart, Nerves, Smooth Gallamine, Methoctramine muscles Glands, Smooth muscles, Endothelium
Oxybutynin, Solifenacin, Darifenacin
At toxic doses
Excitement, agitation, hallucination and coma
Eye
Mydriasis Loss of accommodation for near vision Decrease lacrimal secretion, dry eyes
CVS
Heart: Initially Bradycardia then tachycardia, decrease PR interval Blood vessels: Blockage of EDRF and skeletal muscle vasodilation.
Cutaneous vasodilation
Respirator tract
Bronchodilation Reduced bronchial secretion
Gastrointestinal tract
Decrease salivary and basal gastric secretions, Pirenzepine & Telenzepine gastric acid secretion, M1 blockage Pancreatic and intestinal secretion are less effected Relax GIT wall, Prolong gastric and intestinal transit time
Genitourinary tract
Relax smooth muscles of ureters and bladders Precipitation urinary retention in old people
Sweat Glands
Suppression of thermoregulatory sweating Increase body temperature (Atropine fever in children)
Motion sickness
Scopolamine: Vestibular disorder, seasickness, injection, oral Sedation and dry mouth
Ophthalmic disorders
Measurement of refractive error and examination of retina (Mydriasis) Ointments, Glycopyrrolate and atropine Alpha receptor agonist, Phenylphrine, short mydriasis Drug Atropine Scopolamine Homatropine Cyclopentolate Tropicamide Duration of action 7-10 3-7 1-3 1 0.25 Concentration % 0.5-1 0.25 2-5 0.5-2 0.5-1
Respiratory disorders
Ether anesthesia, Atropine and scopolamine Ipratropium: aerosol inhalants, asthma, COPD Thiotropium: COPD in elderly and smokers, once a day
CVS disorders
Atropine: Vasovagal attack and syncope Auto-antibodies against 2nd M2 loop and Trypanosoma cruzi
GIT disorders
In past used to treat ulcer Atropine + Diphenoxylate (opioid): diarrhea, motility
Urinary disorders
Oxybutynin: M3 antagonist, Oral & via catheter Relieve bladder spasm after prostatectomy, Involuntary voiding Trospium comparable efficacy and side effect as oxybutynin Dairfenacin, Slifenacin, Tolterodine, Fesoterodine: Anti-M3, urinary complications Imipramine, incontinence in old people, replaced by propiverine