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62 Cards in this Set
- Front
- Back
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Where does hemicholinium work?
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It blocks the reuptake of choline used for synthesis of acetycholine
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What is the action of Vesamicol
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Blocks the transport of Ach into the storage vesicle
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Muscarinic receptors are G protein coupled or ligand-gated ion?
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G protein coupled
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Basic action of botulinum toxin acts at the___
What does type A do? |
membrane to inhibic Ach release, type A can cleave SNAP-25
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The class of organophosphates work by
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inhibiting acetylcholinesterase
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Pilocarpine, bethanechol, and carbachol are in the general class of
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muscarinic agonists
parasympathomimetics |
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Atropine is in the class of
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muscarinic antagonists
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Succinylcholine is in the class of
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Nicotinic receptor agonist
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Curare is in the class of
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nicotinic receptor antagonist
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A relatively new choline acetyltransferase inhibitor
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Acetylseco hemicholinium
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Describe the action of Letrotoxin
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Triggers exocytosis release of Ach, toxic excess of Ach
*can happen in absence of calcium |
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What are some clinical uses of botulinum toxin
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cervical dystonia, twitching eyelid, strabismus (eye deviation), cosmetic
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Botulinum toxin does not allow what to complex to form
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The SNARE docking complex
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Name 4 irreversible organophosphates in the insecticide category
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Isoflurophate
Echothiophate Malathion Parathion |
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Two Nerve gases that are irreversible AchE inhibitors
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Sarine and Soman
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What are 3 important carbamates and describe their action
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Physostigmine
Neostigmine Pyridostigmine They are all reversible AchE inhibitors used in glucoma and myasthenia gravis treatment |
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Edrophonium is what class of drug
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Ory alcohol that works as a reversible AchE inhibitor
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What are nicotinic and muscarinic effects of cholinesterase inhibitors?
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Muscarinic- stimulation of receptor responses at autonomic effector organs
Nicotinic- Stimulation followed by depression of skeletal muscle |
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Mechanism of organophosphates
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phosphorylation of AchE
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Explain the 5 main symptoms of cholinergic excess toxidrome
(SLUDGE) |
Salivation
Lacrimation Urination Defecation GI symptoms Emesis along with- miosis |
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Cholinergic excess toxidrome over stimulates the parasymathetic system with what outcomes
DUMB BELS |
Diarrhea
Urination Miosis Bronchorrhea Bradycardia Emesis Lacrimation Salivation/sweating |
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Sympathetic receptors on the eye include
Alpha or Beta 1 or 2 |
Alpha 1- for iris dilation
Beta 2- on ciliary muscle for far vision |
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Which parasympathetic receptors are on the eye and what is their action?
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M2-miosis closes pupil
M3- ciliary muscle for near vision |
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Detailed mechanism of isoflurophate
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Covalently bonds to AchE-ase creates irreversible block
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Can Isoflurophate be used therapeutically? How?
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Yes for glaucoma, causes contraction of ciliary muscle and opening of trabecular network
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Name clinical use of
Ambenonium Demecarium Donepezile |
Ambenonium- Myasthenia Gravis
Demecarium- Glaucoma Deonepezil- Dementia Alzheimer's |
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Name clinical use of
Echothiophate Edrophonium Galantamine |
Echothiophate-glaucoma
Edrophonium-Myasthenia Gravis Galantamine-Dementia Alzheimers |
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Name clinical use of
Neostigmine Physostigmine Pyridostigmine |
Neostigmine-myasthenia gravis and urinary retention
Physostigmine- reverse cholinergic block Pyridostigmine- Myasthenia gravis |
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Name clinical use of
Rivastigmine Racrine Isoflurophate |
Rivastigmine- Dementia Alzheimers
Tacarine Dementia Alzheimers Isoflurophate- glaucoma |
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Which cholinesterase inhibitor has a charged quaternary ammonium group and does not efficiently cross blood brain barrier
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Neostigmine
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Does physostigmine work at the neuromuscular junction?
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No. it works at the postganglionic parasympathetic
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Name 4 drugs for Alzheimer associated dementia
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Donpezil Tacarin Rivastigmine and Galantamine
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Name clinical use of
Neostigmine Physostigmine Pyridostigmine |
Neostigmine-myasthenia gravis and urinary retention
Physostigmine- reverse cholinergic block Pyridostigmine- Myasthenia gravis |
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Name clinical use of
Rivastigmine Racrine Isoflurophate |
Rivastigmine- Dementia Alzheimers
Tacarine Dementia Alzheimers Isoflurophate- glaucoma |
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Which cholinesterase inhibitor has a charged quaternary ammonium group and does not efficiently cross blood brain barrier
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Neostigmine
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Does physostigmine work at the neuromuscular junction?
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No. it works at the postganglionic parasympathetic
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Name 4 drugs for Alzheimer associated dementia
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Donpezil Tacarin Rivastigmine and Galantamine
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Name 3 drugs that stimulate the muscarinic receptor directly
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Bethanecol, Carbechol, and Pilocarpine
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Of the cholinergic stimulants, name two that do not stimulate the N receptor and one that does stimulate the N receptor
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Does not stimulate N receptor- Bethanecol and Pilocarpine
Does stimulate- Carbechol |
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Which cholinergic stimulant would you use to stimulate the bladder and GI contractions after abdominal surgery
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Bethanecol
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Muscarinic or Nicotinic
Pilocarpine Lobeline |
Pilocarpine- muscarinic
Lobeline- Nicotinic |
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Typical side effects of cholinergic drugs
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SLUDGE, Decreased BP, bronchospasm
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Are carbechol and bethenechol broken down by AchEsterase?
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No
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Clinical use of direct-acting cholinomimetics
Acetylcholine Bethanechol Carbechol |
Acetylcholine- miosis for surgery
Bethanechol- urinary retention Carbechol- glaucoma |
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Clinical use of direct cholinomimetics
Cevimeline Pilocarpine Varenicline |
Cevimeline- dry mouth
Pilocarpine- Glaucoma and dry mouth Varenicline- smoking cessation |
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Major drug used as a muscarinic receptor antagonist
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Atropine
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Which drug increases heart rate by blocking the parasympathetic activity of the vagus on the heart?
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Atropine
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What is atropine's action on the GI tract
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to relax the GI system
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What is the use of pralidoximine
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Can treat in organophosphate poisoning to break the covalent bond between organophosphate and AchE
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What is the class and clinical use of Ipratropium
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Muscarinic Blocker
Used as a bronchodilator in asthma |
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What is the class and clinical use of Scopolamine
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Muscarinic blocker (alkaloid in datura)
CNS depressent for antiemetic used in motion sickness |
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What is the class and action of Tolterodine
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Muscarinic blockers, used for overactive bladder
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Sympathetic receptors of the bladder
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Alpha 1- contracts spincter
Alpha 2 receptors to inhibit parasymp Beta 2- inhibit detrusor |
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Overall effect of sympathetic stimulation on bladder
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Urine Retention
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Parasympathetic receptors and action on the bladder
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M2- contraction
Sacral Fibers Connect to voluntary conrol of micturition |
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Side effects of Cholinergic blockade (like atropine)
Mad as a... |
Mad as a hatter- CNS delerium
Blind as a bat- mydriasis Dry as a bone- dry mouth decreased tear Red as a beet- sympathetic flush Hos as a pistol- loss of sweating |
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Two main nicotinic receptor agonists
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nicotine and sucinylcholine
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Two nicotinic receptor Antagonists
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Curare and alpha bungarotoxin
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Are competitive nicotinic antagonists depolarizing or non depolarizing blockers?
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nondepolarizing
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Is curare nondepolarizing or depolarizing blocker?
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Non-depolarizing
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Succinylcholine is competitive or noncompetitive? Does AchE work on it?
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Non-competetive
AchE does NOT break it down |
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Dexamethonium and mecamylamine are what class
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Ganglionic blockers of Nicotinic receptors
used to reduce blood pressure |
