Term
| 3 classes of cholinesterase inhibitors |
|
Definition
reversible Noncovalent inhibitors
reversible carbamate inhibitors
Irreversible organophosphates |
|
|
Term
| Noncovalent AChE inhibitors |
|
Definition
Edrophonium- quatnernary (do NOT cross BBB)
Tacrine, donepezil- tertiary (cross BBB) |
|
|
Term
|
Definition
| neostigmine, pyridostigmine, physostigmine, rivastigmine |
|
|
Term
|
Definition
| react w/serine in the active site to form carbamoylated AChE |
|
|
Term
|
Definition
neo and pyri (poor absorption in GI)do NOT cross BBB.
phys and riva enter BBB
undergo non-enzymatic hydrolysis |
|
|
Term
|
Definition
| DFP, echothiophate, parathion, malathion |
|
|
Term
|
Definition
| All enter CNS except Echothiophate |
|
|
Term
| Organophosphate mech of action |
|
Definition
| react w/serine in catalytic triad- phosphorylated intermediate |
|
|
Term
| Pharm effects on cholinergic nerve stimulation |
|
Definition
stimulation of musc. receptors
stimu then depress of ganglia (nicotinic) |
|
|
Term
|
Definition
conjunctivial hyperemia, miosis
blurred vision
reduced intraocular pressure w/wide-angle glaucoma |
|
|
Term
| AChE block effect on GI tract |
|
Definition
|
|
Term
| AChE block effect on resp. tract |
|
Definition
|
|
Term
|
Definition
anxiety, restlessness
resp depression, convulsions |
|
|
Term
|
Definition
neostigmine, pyridostigmine, ambenonium- enhance ACh in the cleft
Corticosteroids and cyclosporine |
|
|
Term
|
Definition
| acetazolamide, mannitol, and pilocarpine |
|
|
Term
|
Definition
Pilocarpine (miotic)
Timolo (beta blocker) decr aqueous humor
Demecarium,
echothiophate |
|
|
Term
| First inhibitor approved for AD |
|
Definition
Tacrine
short half life; very hepatoxic! |
|
|
Term
| AD drug HIGHLY selective for CNS AChE |
|
Definition
Donepzil
Longest half-life
Very LITTLE hepatoxicity |
|
|
Term
| AD drug- once daily transdermal patch |
|
Definition
|
|
Term
| Adynamic Ileus of bladder after surgery |
|
Definition
|
|
Term
|
Definition
| PHysostigmine reverses it |
|
|
Term
| Side effects of AChE Inhibitor |
|
Definition
Increase PS effects
occasional cataracts, lenticiular opacities |
|
|
Term
|
Definition
Insecticides- parathion/malathion
80% of hospital admissions |
|
|
Term
|
Definition
SLUDGE and DUMBELS- muscarinic
Nicotinic- respiratory difficult, arrest. muscle weakness
CNS: malaise, memory loss, confusion, delirium, seizures and coma |
|
|
Term
|
Definition
|
|
Term
|
Definition
| pyridostigmine administered to soldiers in case of nerve gas |
|
|
Term
| Cholinesterase regenerator |
|
Definition
|
|
