Page 137 - Basic _ Clinical Pharmacology ( PDFDrive )
P. 137
CHAPTER 7 Cholinoceptor-Activating & Cholinesterase-Inhibiting Drugs 123
PREP AR A TIONS Benowitz N: Nicotine addiction. N Engl J Med 2010;362:2295.
A V AIL ABLE Brito-Zerón P et al: Primary Sjögren syndrome: An update on current phar-
macotherapy options and future directions. Expert Opin Pharmacother
2013;14:279.
GENERIC NAME AVAILABLE AS Cahill K et al: Pharmacological interventions for smoking cessation: an overview
and network meta-analysis. Cochrane Database of Systematic Reviews 2013,
DIRECT-ACTING CHOLINOMIMETICS Issue 5.
Acetylcholine Miochol-E Chen L: In pursuit of the high-resolution structure of nicotinic acetylcholine
Bethanechol Generic, Urecholine receptors. J Physiol 2010;588:557.
Carbachol Corradi J, Bourzat C: Understanding the bases of function and modulation of
Ophthalmic (topical) Isopto Carbachol, Carboptic α7 nicotinic receptors: Implications for drug discovery. Mol Pharmacol
2016;90:288.
Ophthalmic (intraocular) Miostat, Carbastat Dineley KT, et al: Nicotinic ACh receptors as therapeutic targets in CNS disorders.
Cevimeline Generic, Evoxac Trends Pharmacol Sci 2015;36:96.
Nicotine Ehlert FJ: Contractile role of M2 and M3 muscarinic receptors in gastrointestinal,
Transdermal Generic, Nicoderm CQ, Nicotrol airway and urinary bladder smooth muscle. Life Sci 2003;74:355.
Inhalation Nicotrol Inhaler, Nicotrol NS Ferré S et al: G protein-coupled receptor oligomerization revisited: Functional and
pharmacological perspectives. Pharmacol Rev 2014;66:413.
Gum Generic, Commit, Nicorette Giacobini E (editor): Cholinesterases and Cholinesterase Inhibitors. London: Martin
Pilocarpine Dunitz, 2000.
Ophthalmic (drops)1, 2, 4, 6 Generic, Isopto Carpine Gilhus NE: Myasthenia gravis. N Engl J Med 2016;375:2570.
Ophthalmic sustained-release Ocusert Pilo-20, Ocusert Pilo-40 Harvey RD, Belevych AE: Muscarinic regulation of cardiac ion channels. Br J
inserts Pharmacol 2003;139:1074.
Oral Salagen Lamping KG et al: Muscarinic (M) receptors in coronary circulation. Arterioscler
Thromb Vasc Biol 2004;24:1253.
Varenicline Chantix Lazartigues E et al: Spontaneously hypertensive rats cholinergic hyper-responsiveness:
CHOLINESTERASE INHIBITORS Central and peripheral pharmacological mechanisms. Br J Pharmacol
Donepezil Generic, Aricept 1999;127:1657.
Echothiophate Phospholine Picciotto MR et al: It is not “either/or”: Activation and desensitization of nicotinic
acetylcholine receptors both contribute to behaviors related to nicotine
Edrophonium Generic, Tensilon addiction and mood. Prog Neurobiol 2008;84:329.
Galantamine Generic, Reminyl, Razadyne Richardson CE et al: Megacystis-microcolon-intestinal hypoperistalsis syndrome
Neostigmine Generic, Prostigmin and the absence of the α3 nicotinic acetylcholine receptor subunit.
Physostigmine Generic, Eserine Gastroenterology 2001;121:350.
Pyridostigmine Generic, Mestinon, Regonol Sánchez-Bayo F et al: Are bee diseases linked to pesticides?—A brief review.
Environ Int 2016;89-90:7.
Rivastigmine Exelon Schroeder C et al: Plasma exchange for primary autoimmune autonomic failure. N
Engl J Med 2005;353:1585.
The Surgeon General: Smoking and Health. US Department of Health and Human
Services, 1979.
REFERENCES Tomizawa M, Casida JE: Neonicotinoid insecticide toxicology: Mechanisms of
Aaron CK: Organophosphates and carbamates. In: Shannon MW, Borron SW, selective action. Annu Rev Pharmacol Toxicol 2005;45:247.
Burns MJ (editors): Haddad and Winchester’s Clinical Management of Wess J et al: Muscarinic acetylcholine receptors: Mutant mice provide new insights
Poisoning and Drug Overdose, 4th ed. Philadelphia: Saunders, 2007:1171. for drug development. Nat Rev Drug Discov 2007;6:721.
Australian Pesticides and Veterinary Medicines Authority: Overview report: Wing VC et al: Measuring cigarette smoking-induced cortical dopamine release: A
11
Neonicotinoids and the health of honey bees in Australia. 2014. https:// [ C]FLB-457 PET study. Neuropsychopharmacology 2015;40:1417.
archive.apvma.gov.au/news_media/chemicals/bee_and_neonicotinoids.php.
C ASE STUD Y ANSWER
The patient’s presentation is characteristic of poisoning by confusion) subside. To treat nicotinic excess, infuse 2-PAM
organophosphate cholinesterase inhibitors (see Chapter 58). (initially a 1–2% solution in 15–30 minutes) followed by infu-
Ask the coworker if he can identify the agent used. Decontami- sion of 1% solution (200–500 mg/h) until muscle fasciculations
nate the patient by removal of clothing and washing affected cease. Respiratory support is required because 2-PAM does not
areas. Ensure an open airway and ventilate with oxygen. For enter the central nervous system and may not reactivate “aged”
muscarinic effects, administer atropine (0.5–5 mg) intrave- organophosphate-cholinesterase complex. If needed, decon-
nously until signs of muscarinic excess (dyspnea, lacrimation, taminate the coworker and isolate all contaminated clothing.