CNS 1 Flashcards
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Miochol-E (acetylcholine chloride)
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Class: Direct-acting cholinergic agonist.
Pharmacology: Administered intraocular due to AChE metabolism when administered topically, non-selective for receptors, not well absorbed due to quaternary ammonium ion, metabolized by pseudocholinesterase.
Indications: Miosis of the iris in seconds after delivery of the lens in cataract surgery, in penetrating keratoplasty, iridectomy.
Adverse: Corneal edema, corneal clouding, corneal decompensation, rarely bradycardia, hypotension, flushing, breathing difficulties, sweating
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Provocholine (methacholine)
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Class: Direct-acting choline ester cholinergic agonist.
Pharmacology: beta-methyl analog of ACh, resistant to pseudocholinesterase metabolism, S(+) enantiomer is more selective for muscarinic receptors, R(-) enantiomer is a better inhibitor of AChE, given as racemate, causes bronchoconstriction.
Indications: Diagnosis of bronchial airway hyper-reactivity in people who do not have clinically apparent asthma.
Adverse: Airflow limitation, don’t give to those with recent stroke, myocardial infarction, uncontrolled hypertension or pregnancy, must have emergency resuscitation equiptment, oxygen and medications to treat bronchospasm on hand
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Urecholine (bethanechol)
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Class: Direct-acting carbamate ester cholinergic agonist.
Pharmacology: Binds to muscarinic receptors/S(+) enantiomer is more selective for muscarinic receptors, orally more potent, causes contraction of detrusor muscle, stimulates gastric motility/restore peristalsis.
Indications: Urinary retention, especially postoperatively, postpartum or in neurogenic atony of the bladder with retention (spina bifida)
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Miostat (carbachol)
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Class: Direct-acting carbamate ester cholinergic agonist.
Pharmacology: Potent cholinergic agonist, produces constriction of the iris and ciliary body which reduces intraocular pressure.
Indications: To obtain miosis during surgery, to reduce intensity of intraocular pressure, glaucoma.
Adverse: Corneal clouding, persistent bullous karatopathy, retinal detachment, postoperative iritis, side effects of flushing, sweating, epigastric distress, abdominal cramps, tightness in the bladder, headache
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Isopto Carpine (pilocarpine)
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Class: Direct -acting alkaloid cholinergic agonist.
Pharmacology: Muscarinic cholinergic agonist.
Indications:Reduction of intraocular pressure (IOP) in glaucoma or ocular hypertension, prevention of postoperative IOP, induction of miosis.
Adverse: headache/browache, accommodative change, eye irritation/pain, blurred vision/visual impairment
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Salagen (pilocarpine)
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Class: Direct -acting alkaloid cholinergic agonist.
Pharmacology: Muscarinic cholinergic agonist.
Indications: Xerostomia (dry mouth) from salivary gland hypofunction caused from radiotherapy or in patients with Sjogren’s syndrome.
Adverse: headache/browache, accommodative change, eye irritation/pain, blurred vision/visual impairment
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Evoxac (cevimeline)
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Class: Direct -acting alkaloid cholinergic agonist.
Pharmacology: Muscarinic agonist with high affinity for M3 receptors on lacrimal & salivary gland epithelia.
Indications: For long-lasting sialogogic action (increase saliva).
Adverse: Fewer side effects than pilocarpine
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Cognex (tacrine)
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Class: Indirect-acting reversible competitive AChE inhibitor.
Pharmacology: Binds noncovalently to anionic side on AChE, no longer prescribed.
Indications: Alzheimer’s Disease.
Adverse: Hepatoxicity
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Aricept (donepezil)
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Class: Indirect-acting reversible competitive AChE inhibitor.
Pharmacology:Binds noncovalently to anionic side on AChE.
Indications: Alzheimer’s Disease
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Antilirium (physostigmine)
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Class: Indirect-acting semi-reversible AChE inhibitor.
Pharmacology: Carbamyl esters that interact with the anionic site on AChE, temporary covalent bond, targets postganglionic parasympathetic junctions, no quaternary ammonium so can penetrate the BBB.
Indications: Eye drops in treating glaucoma, to reverse the toxic CNS effects due to anticholinergic drugs
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Mestinon (pyridostigmine)
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Class: Indirect-acting semi-reversible AChE inhibitor.
Pharmacology: Carbamyl ester, lasts longer than both neostigmine and physostigmine.
Indications: Oral treatment for myasthenia gravis, was given in anticipation of nerve-agent attack in Persian Gulf War
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Prostigmin (neostigmine)
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Class: Indirect-acting semi-reversible AChE inhibitor.
Pharmacology: Carbamyl ester, lasts longer than physostigmine.
Indications: Oral treatment for myasthenia gravis, competitively reverse neuromuscular block induced during surgery
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Reminyl/Razadyne (galantamine)
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Class: Indirect-acting reversible competitive AChE inhibitor.
Pharmacology: May be a nicotinic receptor agonist, inhibitors of CYP3A4 and 2D6 will increase bioavailability.
Indications: Alzheimer’s Disease
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Exelon (rivastigmine)
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Indirect-acting pseudo-irreversible AChE inhibitor.
Pharmacology: Crosses BBB, inhibits AChE for 10 hours, available as transdermal patches.
Indicaitons: Alzheimer’s Disease.
Adverse: Nausea, vomiting, anorexia, weight loss
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Isolurophate (Floropryl)
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Indirect-acting irreversible AChE inhibitor.
Pharmacology: Topical as ointment, acts for 4 weeks, reduce IOP.
Indications: Glaucoma.
Adverse: Toxicity associated with generation of cataracts and retinal detachments
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Echothiophate (Phospholine)
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Indirect-acting irreversible AChE inhibitor.
Pharmacology: Topical as solution, acts for 4 weeks, reduce IOP.
Indicaitons: Glaucoma.
Adverse: Toxicity associated with generation of cataracts and retinal detachments
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Ovide (malathion)
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Indirect-acting irreversible AChE inhibitor.
Pharmacology: Reacts with AChE to form a phosphorylated enzyme which then undergoes “aging” (loss of alkyl groups) that prevents reactiation of the enzyme via hydrolysis.
Indications: Head lice (Pediculus humanus capitis).
Adverse: Contraindicated in neonates & infants due to scalps being more permeable
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2-PAM/Pralidoxime/Protopam Chloride
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Antidote for irreversible AChE inhibitor.
Pharmacology: Must be given before aging occurs (within 36-48 hours of exposure to organophosphate).
Indications: Treatment for nerve gas agents
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Atropine
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Class: Muscarinic competitive antagonist.
Pharmacology: Nonselective, acts in CNS and periphery.
Indications: Causes mydriasis and cycloplegia (paralysis of ciliary muscle in the eye), retinal examination, prevention of synechiae (adherence of iris to cornea or lens) after surgery, antidote for cholinergic crisis, given pre/peroperatively to decrease respiratory secretion & prevent vagal stimulation, treats sinus bradycardia or nodal block, treats myocardial infarction.
Adverse: Increased IOP
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Scopolamine
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Class: Muscarinic competitive antagonist.
Pharmacology: Penetrates CNS better than atropine, reduces vertigo & post-op nausea.
Indications: Prevention of motion sickness (transdermal patch), post-op nausea/vomiting (IM), combined with morphine to induce anesthesia.
Adverse: Tachycardia, blurred vision, xerostomia, delirium, interacts with other antimuscarinics
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Dicyclomine, Hyoscyamine, Glycopyrrolate, Methscopolamine
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Class: Muscarinic competitive antagonist.
Pharmacology: Targets M3 receptors, reduces smooth muscle and secretory activity of the gut, hyoscyamine has longer duration of action.
Indications: Irritable bowel syndrome, minor diarrhea.
Adverse: tachycardia, confusion, urinary retention, increased IOP, interacts with other antimuscarinics
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Ipratropium, Tiotropium
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Class: Muscarinic competitive antagonist.
Pharmacology: Nonselective, tiotropium has longer duration of action, reduces or prevents bronchospasm.
Indications: Prevention and relief of bronchospasm.
Adverse: Xerostomia, cough, interacts with other antimuscarinics
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Oxybutynin, Darifenacin*, solifenacin*, tolterodine*, trospium
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Class: Muscarinic antagonist.
Pharmacology: Slightly selective for M3, reduces detrusor smooth muscle tone, spasms, * has greater selectivity for M3 receptors, trospium has less CNS effect.
Indications: Incontinence, postoperative spasms.
Adverse: tachycardia, constipation, increased IOP, xerostomia, interacts with other antimuscarinics
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Robinul (glycopyrrolate)
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Class: Muscarinic antagonist.
Pharmacology: Blocks muscarinic receptors on eccrine sweat glands, can also use Botox for hyperhidrosis (blocks ACh release from nerve endings).
Indications:Topical treatment for hyperhidrosis (excessive sweating).
Adverse: Anticholinergic side effects
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Kemadrin (procyclidine HCl), Akineton (biperiden HCl), benztropine (atropine & diphenhydramine)
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Class: Muscarinic antagonist.
Indications: Adjunct therapy for stage 1 and stage 2 of IParkinson’s disease to treat tremors to control extrapyramidal disorders secondary to neuroleptic drug therapy
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Trimethaphan camsylate
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Class: Non-depolarizing nicotinic ganglion antagonist.
Pharmacology: inhibit autonomic activity by interfering with neurotransmission within autonomic ganglia.
Indications: Hypertensive emergencies, to produce controlled hypotension during surgery.
Adverse: Excessive hypotension and impotence due to sympatholytic effect, constipation, urinary retension and dry mouth due to parasympatholytic effect, can also stimulate histamine release
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Anectine (succinylcholine)
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Class: Depolarizing nicotinic neuromuscular antagonist.
Pharmacology: Brief duration of action due to hydrolysis of plasma cholinesterase, 2 linked ACh molecules, initial metabolite has very weak neuromuscular blocking effect
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Tubocurarine, Tracrium (atracurium), Nuromax (doxacurium), Mivacron (mivacurium)
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Class: Non-depolarizing nicotinic neuromuscular antagonist.
Pharmacology: Limited lipid-solubility, isoquinoline derivatives
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Pavulon (pancuronium), Norcuron (vercuronium), Arduan (pipecuronium), Zemuron (rocuronium)
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Class: Non-depolarizing nicotinic neuromuscular antagonist.
Pharmacology:Limited lipid-solubility, steroid derivatives
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Cognex (Tacrine), Aricept (Donezepril), Reminyl (Galantamine)
Questions:
Agonist or Antagonist?
Direct or Indirect?
Reversible/ Semi/ Pseudo/ or Irreversible?
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Cholinergic Agonist
Indirect Acting
Reversible
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Antilirium (Physostigme), Mestinon (Pyridostigmine), Neostigmine (Prostigmin)
Questions:
Agonist or Antagonist?
Direct or Indirect?
Reversible/ Semi/ Pseudo/ or Irreversible?
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Cholinergic Agonist
Indirect Acting
Semi Reversible
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Floropryl (Isofluorophate), Phospholine (Ethothiophate), Ovide (Melathion)
Questions:
Agonist or Antagonist?
Direct or Indirect?
Reversible/ Semi/ Pseudo/ or Irreversible?
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Cholinergic Agonist
Inidrect Acting
Irreversible
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Exelon (Ravastigmine)
Questions:
Agonist or Antagonist?
Direct or Indirect?
Reversible/ Semi/ Pseudo/ or Irreversible?
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Cholinergic Agonist
Indirect Acting
Pseudo-Irreversible
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Miochol E
Questions:
Agonist or Antagonist?
Direct or Indirect?
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Cholinergic Agonist
Acetyl Choline
Direct Acting
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Miostate (Carbachol), Urecholine (Bethanechol), Provocholine (Methacholine)
Questions:
Agonist or Antagonist?
Direct or Indirect?
Type?
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Cholinergic Agonist
Direct
Choline/Carbamate esters (Mimic ACh)
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Evoxac (Cevimeline)
Questions:
Agonist or Antagonist?
Direct or Indirect?
Type?
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Cholinergic agonist
Direct acting
Alkaloid
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Pilocarpine (Isopto Carpine, Ocusert, Salagen)
Questions:
Agonist or Antagonist?
Direct or Indirect?
Type?
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Cholinergic Agonist
Direct Acting
Alkaloid
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Scopolamine, Atropine, Ipatropium, Oxybutynin, Glycopyrrulate, Diclycoamine, Procyclidine, Biperiden, Benztropine
Questions:
Agonist or Antagonist?
Muscarinic or Nicotinic?
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Cholinergic Antagonist
Muscarinic
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Nicotine
Agonist or Antagonist?
Nicontinic or Muscarinic?
Type?
Depolarizing or nondepolarizing?
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Cholinergic Antagonist
Nicotinic
Ganglionic Blocker
Depolarizing Agent
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Trimethaphan Camsylate
Agonist or Antagonist?
Nicontinic or Muscarinic Receptors?
Type?
Depolarizing or nondepolarizing?
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Cholinergic Antagonist
Nicotinic
Ganglionic Blocker
Non-Depolarizing Agent
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Succinylcholine
Agonist or Antagonist?
Nicontinic or Muscarinic?
Type?
Depolarizing or nondepolarizing?
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Cholinergic Antagonist
Nicotinic
Neuromuscular blocking Agent
Depolarizing
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Isoquinoline & Steroid derivatives
Agonist or Antagonist?
Nicontinic or Muscarinic?
Type?
Depolarizing or nondepolarizing?
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Cholinergic Antagonist
Nicotinic Receptors
Neuromuscular Blocking Agent
Non-Depolarizing Agent
