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61 Cards in this Set
- Front
- Back
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bethanechol
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muscarinic receptor agonist
(mimic parasymp. stimulation) ACh+methyl and NH2 substitution; selective to muscarinic and resistant to esterases |
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carbachol
(Carbastat) |
muscarinic receptor agonist
(mimic parasymp. stimulation) NH2 substituted for ACh methyl, poor substrate for esterase) |
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methacholine
(Provocholine) |
muscarinic receptor agonist
(mimic parasymp. stimulation) ACh + methyl lowers interaction w/ nicotinic |
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muscarine
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cholinergic agonist, natural alkaloid
muscarinic selective |
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pilocarpine
(Salagen) |
cholinergic agonist, natural alkaloid
muscarinic selective responses in: cardiovascular sweat glands |
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bethanechol
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muscarinic agonist. +methyl&NH2 sub, less nicotinic&poor esterase substrate. used to stimulate smooth muscle post-op.
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carbachol (Carbastat) (Miostat)
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muscarinic agonist. NH2 substitution, poor esterase substrate. used for wide-angle glaucoma (constrict ciliary mm)
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methacholine (Provocholine) (Mecholyl)
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muscarinic agonist. +methyl, less nicotinic interaction. used to test fxn of muscarinic receptors, slow heart, test bronchial hyperactivity
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muscarine
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muscarinic agonist, natural alkaloid
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pilocarpine (Salagen)
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muscarinic agonist, natural alkaloid. CV responses, sweat glands sensitive. Acute glaucoma. Used to increase salivary secretions
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nicotine
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nicotinic agonist
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varenicline (Chantix)
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nicotinic agonist
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ambenonium (Mytelase)
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compet. AChE inhibitor. Carbamate. Used for myasthenia gravis. Lasts 4-8hrs.
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edrophonium (Tensilon)
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compet. AChE inhibitor. Simple alcohol. used in diagnosis of myasthenia gravis, ileus, arrhythmias. 5-15m action.
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neostigmine (Prostigmin)
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compet. AChE inhibitor. Carbamate. increases smooth mm. motility; used for paralytic ileus, bladder atony post op; Tx and Dx of myasthenia gravis; reversal of neuromuscular blockade (curare) lasts .5-2hr
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physostigmine (Antilirium)
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compet. AChE inhibitor. Carbamate. used topically for therapy of wide-angle glaucoma (acute) lasts .5-2 hr
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pyridostigmine (Mestinon)
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compet. AChE inhibitor. Carbamate. used in Tx of myasthenia gravis, pretreatment for exposure to nerve gases, reversal of neuromuscular blockade (curare). Lasts 3-6hr.
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diisopropylfluorophosphate (DFP)
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noncompet. AChE inhibitor. Organophosphate. Insecticide
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echothiophate
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noncompet. AChE inhibitor. Organophosphate. used for glaucoma. lasts 100hr.
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carbaryl (Sevin)
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noncompet. AChE inhibitor. Carbamate. Insecticide
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malathion
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noncompet. AChE inhibitor. Insecticide. used for Tx of head lice
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parathion
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noncompet. AChE inhibitor. used in insecticides, most common agent of O-P poisoning
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tetraethylpyrophosphate (TEPP)
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noncompet. AChE inhibitor. Insecticide.
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sarin
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nerve gas, highly volatile
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soman
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nerve gas, highly volatile
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pralidoxime (2-PAM)
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reverses noncompet. O-P ChE inhibitors by releasing phosphoryl moiety (before ChE becomes "aged"). 1-2g iv fixes nmj in minutes, less autonomic effect, low CNS effect
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atropine
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muscarinic antagonist. Competitive inhibitor. Lasts 5-10hrs. 3' amine. Distributes quickly. (-) resp tract secretions. Used for mydriasis, cycloplegia, urinary incontinence, adjunct for parkinsonism, overcome O-P poisoning. Salivary, bronchial, sweat glands most sensitive
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homatropine
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muscarinic antagonist. Competitive inhibitor. Lasts 2-4 hrs. 3' derivative of atropine. Used most as topical agent for mydriasis and cycloplegia
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scopolamine
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muscarinic antagonist. Competitive inhibitor. Lasts 5-10hrs. 3' amine. Distributes quickly. (-) resp tract secretions. Most effective anti-motion sickness med. Pre-anesthetic med.
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methscopolamine (Pamine)
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muscarinic antagonist. Competitive inhibitor. Lasts 5-10^2hrs. Quaternary derivative of scopolamine, lacks CNS effects of scopolamine, used for GI disease
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trihexyphenidyl (Artane)
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muscarinic antagonist. Competitive inhibitor. Lasts 3-6 hrs. 3' amine. Anti-Parkinson (less uncoordinated movement, salivation). Decrease extra-pyramidal side effects of anti-psychotics.
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tropicamide (Mydriacyl)
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muscarinic antagonist. Competitive inhibitor. Lasts .5-1.5hrs. 3' amine. Used topically for ocular Tx. Mydriasis/cycloplegia.
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cyclopentolate (Cyclogyl)
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muscarinic antagonist. Competitive inhibitor.
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ipratropium (Atrovent)
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muscarinic antagonist. Competitive inhibitor. Quaternary derivative of atropine. Used as aerosol to dilate bronchi and minimize mucociliary drying
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tiotropium (Spiriva)
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muscarinic antagonist. Competitive inhibitor. Used as aerosol to dilate bronchi and minimize mucociliary clearance problems. Longer acting
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darifenacin (Enablex)
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muscarinic antagonist. M3 selective (smoothmm). Longer duration of action. Relax mm of genitourinary
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solifenacin (Vesicare)
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muscarinic antagonist. M3 selective (smoothmm). Longer duration of action. Relax mm of genitourinary
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tolterodine (Detrol)
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muscarinic antagonist. M3 selective (smoothmm). Longer duration of action. Relax mm of genitourinary
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mecamylamine (Inversine)
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nicotinic nondepolarizing antagonist. 2' amine. Improve absorption from GI, given orally. Lasts 12hrs. CNS effects: tremors, confusion, seizures, mania, depression
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trimethaphan (Arfonad)
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nicotinic nondepolarizing antagonist. 4' ammonium. IV infusion (lasts minutes). Administered during surgery to minimize blood loss in operative area (lower arterial pressure to decrease bleeding)
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succinylcholine
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depolarizing neuromuscular blocker, inactivated by plasma cholinesterase
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curare (d-tubocurarine)
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nicotinic nondepolarizing antagonist. Long acting. Benzylisoquinolones
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atracurium (Tracrium)
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nicotinic nondepolarizing antagonist. Benzylisoquinolones
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cisatracurium (Nimbex)
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nicotinic nondepolarizing antagonist. Intermediate acting.
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mivacurium (Mivacron)
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nicotinic nondepolarizing antagonist. Short acting. Benzylisoquinolones
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pancuronium (Pavulon)
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nicotinic nondepolarizing antagonist. Long acting. Ammonio steroid.
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vecuronium (Norcuron)
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nicotinic nondepolarizing antagonist. Intermediate acting. Ammonio steroid.
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demecarium (Humorsol)
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compet. AChE inhibitor. Carbamate. Used for glaucoma (acute). Lasts 4-6hrs
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cevimeline
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used for treating dry mouth in Sjogren's syndrome
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Acute closed angle glaucoma therapy
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lower intraocular pressure by contracting ciliary body, better aqueous humor outflow, decreased secretion. Muscarinic agonist (pilocarpine) and AChE inhibitor (physostigmine) for acute - med. Emergency cases
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smooth muscle motility stimulation
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if NOT obstructed, bethanechol, neostigmine typically used in GI. Pilocarpine increases salivary secretion, cevimeline treats dry mouth
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NMJ therapy
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ChE inhibitors are used (edrophonium, pyridostigmine, neostigmine, ambenonium)
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how to overcome toxicities of cholinergic agonists
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atropine and/or norepinephrine
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drug to use when mydriasis and cycloplegia both required
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antimuscarinic drugs. Topical application of atropine (long), homatropine (intermediate) tropicamide (short) acting
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CNS effects of antimuscarinics
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anti-parkinson, anti-motion sickness, amnesia for surgery
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tertiary amine antimuscarinics and uses
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atropine, scopolamine, homatropine, trihexiphenidyl. topical use in eye, CNS effects, able to cross mucous membranes
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quaternary ammonium antimuscarinic uses
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charged N group, poor lipid solubility. Chosen to avoid CNS effects
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cycloplegia
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loss of accomodation
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Benzylisoquinolones
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neuromuscular blockers. devoid of vagolytic and ganglionic blocking activity (less cross reactivity); elicit some histamine release. D-tubocurarine, atracurium, mivacurium.
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ammonio steroids
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neuromuscular blockers. No histamine release. Some muscarinic block, eliciting vagal blockade and tachycardia. Newer agents eliminate tachycardia. Pancuronium, veuronium, rocuronium.
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antagonism of neuromuscular blocking agents
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cholinesterase inhibitor drugs: Edrophonium, Neostigmine (reversible, competitive). Drugs allow Ach to rise and compete of nm blockers
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