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Pcol 417 exam 1
ANS
| Question | Answer |
|---|---|
| Reversible Cholinesterase Inhibitors | Edrophonium, Neostigmine, Physostigmine |
| Lead to Carbamoylation of cholinesterase (forms covalent bond) | Physostigmine, Neostigmine |
| Competes with Ach for binding to cholinesterase | Edrophonium |
| hydrolyzed to regenerate the active enzyme during metabolism of ACh | acetate group |
| ACh binds to enzyme active site through interactions with | amino acid residues |
| bind to same active site of the cholinesterase as ACh | Carbamate Derivitives |
| cleavage of the carbamate yields | amino alcohol & carbamoylated enzymes complex |
| suicide substrates | Carbamates |
| Lead to phosphorylation of Serine residue in cholinesterase active site, stable, does not dissosiate | Organophosphates- DFP, malathione, echothiphate, soman, tabun |
| Permanently inactivates enzymatic activity of cholinesterase | Aging |
| Can regenerate Cholinesterase active site prior to aging | strong nucleophile 2-PAM |
| Allows rapid absorption from GI, lungs, skin, conjunctiva for quick irreversible damage | Lipophilicity of organophosphates (Non-polar can distribute well and partition into fats) |
| during inhibiton of AChE when one of the O-C bonds is broken losing a propyl group | MOA for AGING to become more resistant to hydrolysis |
| CV effects of AChEI | decrease HR, force, and CO small or no change in BP |
| GI effects of AChEI | increase motility & digestive secretions flatulence, cramps, defecation |
| Eye effects of AChEI | miosis, increase accommodation for near vision Increase then decrease in IOP |
| Respiratory effects of AChEI | increase bronchial tone, increase mucosal secretions |
| CNS effects of AChEI | increased alertness, convulsions, seizures, coma |
| NM junction effects of AChEI | increased muscle strength, faciculations, ataxia, tremors |
| Enhance cholinergic response to the iris to increase aqueous flow and decrease IOP | Physostigmine, Echothiphate, DFP |
| improve GI and urinary motility | Neostigmine PO or SC |
| improve neuromuscular transmission in myasthenia gravis | Edrophonium -Dx Neostigmine, Pyridostigmine -Tx |
| reverse NM blockade after surgery (Wake up)after neostigmine administration | d-Tubocurarine, Pancuronium |
| Reverse Atropine toxicity | physostigmine |
| Symptoms to AChEI toxicity | SLUDGE & CNS excitation, NM blockade salivation Lacrimation Urination Defecation Gas Emesis |
| Antedote for AChEI toxicity | Atropine to block M receptors 2-PAM to regenerate phosphorylated site |
| Nn Receptor location | nerve cells in the ganglia |
| Nm Receptor location | skeletal muscle endplates |
| subtypes of nicotinic antagonists | non-depolarizing & depolarizing of motor endplate |
| Nondepolarizing blockers | d-tubocurarine, pancuronium, vencuronium, rocuronium, atracurium |
| Depolarizing blockers | succinylcholine, decamethonium |
| reason depolarizing nicotinic antagonists are not used therapeutically | behave like partial agonists that produce a partial depolarization that blocks it from further depolarizations FLACID PARALYSIS |
| partially depolarized motor endplate results in N receptors in the | inactive state |
| can bind both alpha subunits on AChE | Succinylcholine |
| paralysis that cannot be overcome with increased concentration of ACh | Flacid paralysis from a depolarizing nicotinic antagonist |
| Binding of these agents prevents ACh from binding to N receptors at the NM junction to prevent depolarization | Non-depolarizing agents Tubocurarine, Pancuronium, Gallamine, Atracurium |
| IV administration leads to paralysis of small rapid muscles followed by larger, and finally the diaphragm | Nicotinic Antagonists: Non-depolarizing blockers |
| Therapeutic uses of non-depolarizing N antagonists | produce skeletal muscle paralysis for surgery, reduce amount of anesthesia, setting fractures, intubations, bronchoscopy, endoscopy |
| Used to reverse non-depolarizing N antagonist paralysis | Neostigmine & Physostigmine by increasing Ach |
| ADR of Nicotinic antagonists | apnea, cardiovascular collapse |
| ADR of d-TC, metocurine, succinylcholine, and atracurium | histamine release=blockage of airway, massive decrease in BP |
| ADR of depolarizing blockers | Malignant hyperthermia due to excessive release of Ca+ from SR |
| Tx for Malignant hyperthermia | Dantrolene |
| more susceptible to nondepolarizing agents and less to depolarizing agents | neonates |
| Drug interactions for anti-nicotinics | Inhalation anesthetics, aminoglycosides, Ca2+ channel blockers, Opiods, Lidocaine, Phenytoin, MagOx, Chloroquine |
| Selective alpha 1 adrenergic agonists | Phenylephrine, Methoxamine |
| Non-Selective alpha 1 adrenergic agonists | Oxymetazoline, tetrahydrozoline, naphazoline (Visine-A) |
| Selective alpha 2 Adrenergic agonists | Clonidine, apraclonidine, methyldopa, brimonidine (Alphagan-P), tizanidine |
| Selective beta 2 adrenergic agonists | albuterol, salmeterol, levalbuterol, fometerol, metaproterenol, terbutaline |
| mixed sympatheticomimetic amines | amphetamine, dextroampetamine, methylphenidate, dexmethylphenidate, methamphetamine |
| potencies at alpha receptors | epinephrine > norepinephrine >> isoproterenol |
| potencies at beta receptors | isoproterenol > epinephrine > norepinephrine |
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