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38 Cards in this Set

  • Front
  • Back
What are the 3 Choline esters(muscarinic agonists)?
1. Ach
2. Carbachol
3. Bethenechol

ABC ester's
What are the two muscarinic natural alkaloids?
1. Pilocarpine
2. Muscarine
What are the 4 cholinesterase reversible inhibitors?
1. Edrophonium
2. Physostigmine
3. Neostigmine
4. Donepezil

PNED
What are the cholinesterase irreversible inhibitors?
1. Organophosphates
What are the cholinesterase reactivators?
1. Pralidoxime
What is the MOA of all choline esters and natural alkaloids?(3)
1. Activate M1, M2, and M3 receptors
2. Activating postsynaptic receptors to the effectors
3. Activating presynaptic receptors to inhibit NT release
What does the initial and prolonged activation of nicotonic receptors cause?
1. Initially an AP and response in effector
2. Prolonged causes a depolarization blockade to inhibit further response
What receptors do the Choline esters activate?(3)
1. Ach = M1,M2,M3 and Nn
2. Carbachol = M1, M3 and Nn
3. Bethenechol = M1, M3
What are the effects of the choline esters?
1. DUMBBELSS
Where are choline ester's distributed, excreted, and how are they administerd?
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
What are the adverse affects of topical choline esters?(3)
1. Iritis
2. Retinal detachment
3. Cataracts
Ach and Carbachol
What are the adverse affects of systemic choline esters?(3)
1. Hypotension
2. Flushing
3. Bronchospasm
Bethenachol
What are the contraindications of choline esters?(6)
1. Iritis(locally)
2. Asthma
3. Hypotension and cadiac Dz
4. IBS and bowel Dz
5. Urinary obstruction
6. Hyperthyroidism
What is the chemistry for the natural alkaloids? And their MOA?
1. Pilocarpine is tertiary amine
2. Muscarine is quaternary ammonia from mushrooms
3. Only activate M1, M2 and M3
What is the pharmacalogic effect of natural alkaloids?
1. Salivation and Sweating, with other DUMBBELSS in peripheral tissues
2. Central effects cause arousal, headaches and tremors
What is myecetism? Symptoms?
1. Poisoning by mushrooms
2. Within 1 hour
3. DUMBBELSS to convulsions and coma
What are the contraindications and precautions to natural alkaloids?
1. Similar to choline esters(6)
What are the therapeutic uses for natural alkaloids?(2)
1. Pilocarpine for glaucoma and Sjorgrens or radiation Xerostomia
2. None for muscarine
What are the reversible(4) and irreversible(1) cholinesterase inhibitors?
1. Physo and neostigmine
2. Edrophonium
3. Donepazil
4. Organophosphates
What are the MOA of cholinesterase inhibitors?
1.Substrates of ACH-E that bind them 1000x better than ACH
What are the short and long acting ACH-E-I?
1. Edrophonium at 10 min
2. Neo and physostigmine at 1-6 hours
What is aging?
The loss of an alkyl group over time that makes the irreversible ACH-E-I stronger
The ACH-E-I that enter the CNS cause what?
1. Moderate = increased alertness
2. High = confision, ataxia, convulsions, coma and respiratory paralysis
What do the ACH-E-I do in the eye, GI and GU? CV system? Adrenal?
1. PS
2. DUMBBELSS
3. Adrenals = release of E
What are the net effects of the ACH-E-I in the Heart?
1. Moderate = bradycardia
2. High = bradycardia and hypotension
What do the ACH-E-I do at the NMJ?
1. Moderate = increase contraction strength
2. High = causes neuromuscular blockade
What is the oral absorption like for ACH-E-I?(3)
1. Good for physostigmine
2. Bad for neostigmine and erdophonium
3. Great for Organophosphates, also in the skin
Where do the ACH-E-I go in the body?
1. Physo in all including CNS
2. Neo and Erdo in periphery
3. Organo everywhere
What causes death with ACH-E-I?
1. Central respiratory failure
How to tx ACH-E-I poisoning?(4)
1. Maintence of vital signs(O2 and ventillator)
2. Convulsions with Diazepam
3. Atropine
4. Cholinesterase reactivators is time is not long(aging)
What is the overall name of cholinesterase reactivators?
1. Pralidoxamine
What are the pharm effects of cholinesterase reactivators? When do you use it?
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
When do you not use ACH-E reactivators?
1. when you need DUMBBELSS going on
2. Hyperthryoidism
3. Seizure disorder
4. Parkinson's
What are the therapuetic uses for Cholinergic drugs in the Eye?
1. Glaucoma, reduces interoccular pressure at the canal of schlem
What are the therapuetic uses for Cholinergic drugs in the GI and GU?(2)
1. Xerostomia
2. Urinary retention
What are the therapuetic uses for Cholinergic drugs in the Neuromuscular system?
1. Myasthenia gravis
2. Dx with erdophonium if you see an increase in strength
3. Tx with Neostigmine
What is the difference between a cholinergic crisis and a myasthenic crisis?
1. further Decrease in muscle strength
2. Improved muscle strength
What are some tx for glaucoma that are cholinomimetics?(2)
1. Carbachol, Pilocarpine, Physostigmine
2. Increase the aq humor outflow through the canal of schlemm

PCP in my Eye