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38 Cards in this Set
- Front
- Back
What are the 3 Choline esters(muscarinic agonists)?
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1. Ach
2. Carbachol 3. Bethenechol ABC ester's |
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What are the two muscarinic natural alkaloids?
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1. Pilocarpine
2. Muscarine |
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What are the 4 cholinesterase reversible inhibitors?
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1. Edrophonium
2. Physostigmine 3. Neostigmine 4. Donepezil PNED |
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What are the cholinesterase irreversible inhibitors?
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1. Organophosphates
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What are the cholinesterase reactivators?
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1. Pralidoxime
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What is the MOA of all choline esters and natural alkaloids?(3)
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1. Activate M1, M2, and M3 receptors
2. Activating postsynaptic receptors to the effectors 3. Activating presynaptic receptors to inhibit NT release |
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What does the initial and prolonged activation of nicotonic receptors cause?
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1. Initially an AP and response in effector
2. Prolonged causes a depolarization blockade to inhibit further response |
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What receptors do the Choline esters activate?(3)
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1. Ach = M1,M2,M3 and Nn
2. Carbachol = M1, M3 and Nn 3. Bethenechol = M1, M3 |
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What are the effects of the choline esters?
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1. DUMBBELSS
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Where are choline ester's distributed, excreted, and how are they administerd?
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1. In the peripheral tissues
2. In the kidneys 3. Ach and carbachol given topically on the Eyes 4. Bethenechol is given PO, SC but never IV |
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What are the adverse affects of topical choline esters?(3)
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1. Iritis
2. Retinal detachment 3. Cataracts Ach and Carbachol |
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What are the adverse affects of systemic choline esters?(3)
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1. Hypotension
2. Flushing 3. Bronchospasm Bethenachol |
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What are the contraindications of choline esters?(6)
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1. Iritis(locally)
2. Asthma 3. Hypotension and cadiac Dz 4. IBS and bowel Dz 5. Urinary obstruction 6. Hyperthyroidism |
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What is the chemistry for the natural alkaloids? And their MOA?
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1. Pilocarpine is tertiary amine
2. Muscarine is quaternary ammonia from mushrooms 3. Only activate M1, M2 and M3 |
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What is the pharmacalogic effect of natural alkaloids?
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1. Salivation and Sweating, with other DUMBBELSS in peripheral tissues
2. Central effects cause arousal, headaches and tremors |
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What is myecetism? Symptoms?
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1. Poisoning by mushrooms
2. Within 1 hour 3. DUMBBELSS to convulsions and coma |
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What are the contraindications and precautions to natural alkaloids?
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1. Similar to choline esters(6)
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What are the therapeutic uses for natural alkaloids?(2)
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1. Pilocarpine for glaucoma and Sjorgrens or radiation Xerostomia
2. None for muscarine |
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What are the reversible(4) and irreversible(1) cholinesterase inhibitors?
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1. Physo and neostigmine
2. Edrophonium 3. Donepazil 4. Organophosphates |
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What are the MOA of cholinesterase inhibitors?
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1.Substrates of ACH-E that bind them 1000x better than ACH
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What are the short and long acting ACH-E-I?
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1. Edrophonium at 10 min
2. Neo and physostigmine at 1-6 hours |
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What is aging?
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The loss of an alkyl group over time that makes the irreversible ACH-E-I stronger
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The ACH-E-I that enter the CNS cause what?
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1. Moderate = increased alertness
2. High = confision, ataxia, convulsions, coma and respiratory paralysis |
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What do the ACH-E-I do in the eye, GI and GU? CV system? Adrenal?
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1. PS
2. DUMBBELSS 3. Adrenals = release of E |
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What are the net effects of the ACH-E-I in the Heart?
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1. Moderate = bradycardia
2. High = bradycardia and hypotension |
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What do the ACH-E-I do at the NMJ?
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1. Moderate = increase contraction strength
2. High = causes neuromuscular blockade |
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What is the oral absorption like for ACH-E-I?(3)
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1. Good for physostigmine
2. Bad for neostigmine and erdophonium 3. Great for Organophosphates, also in the skin |
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Where do the ACH-E-I go in the body?
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1. Physo in all including CNS
2. Neo and Erdo in periphery 3. Organo everywhere |
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What causes death with ACH-E-I?
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1. Central respiratory failure
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How to tx ACH-E-I poisoning?(4)
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1. Maintence of vital signs(O2 and ventillator)
2. Convulsions with Diazepam 3. Atropine 4. Cholinesterase reactivators is time is not long(aging) |
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What is the overall name of cholinesterase reactivators?
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1. Pralidoxamine
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What are the pharm effects of cholinesterase reactivators? When do you use it?
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1. Works at the NMJ
2. Does not work well in the brain(doesn't enter) or the autonomic effector sites 3. Use it for organophosphate poisoning |
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When do you not use ACH-E reactivators?
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1. when you need DUMBBELSS going on
2. Hyperthryoidism 3. Seizure disorder 4. Parkinson's |
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What are the therapuetic uses for Cholinergic drugs in the Eye?
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1. Glaucoma, reduces interoccular pressure at the canal of schlem
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What are the therapuetic uses for Cholinergic drugs in the GI and GU?(2)
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1. Xerostomia
2. Urinary retention |
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What are the therapuetic uses for Cholinergic drugs in the Neuromuscular system?
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1. Myasthenia gravis
2. Dx with erdophonium if you see an increase in strength 3. Tx with Neostigmine |
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What is the difference between a cholinergic crisis and a myasthenic crisis?
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1. further Decrease in muscle strength
2. Improved muscle strength |
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What are some tx for glaucoma that are cholinomimetics?(2)
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1. Carbachol, Pilocarpine, Physostigmine
2. Increase the aq humor outflow through the canal of schlemm PCP in my Eye |