Cholinomimetics Indirect Flashcards
pyridostigmine
mech
4a amine- doesnt cross BBB
pyridostigmine
tx
myasthenia gravis
reverse neuromuscular blockade
neostigmine
mech
4a amine- doesnt cross BBB
neostigmine
Tx
Myasthenia gravis
reverse neuromuscular blockade (competitive blockers like curare)
post op urinary retention/ paralytic ileus
lowers IOP
Endophobium
mech
4a amine- doesnt cross BBB
endrophobium
tx
used to diagnose MG
- give endrophobium to see if muscle weakness improves
- if muscle weakness doesnt improve– cholinergic crisis
used to evaluate tx of MG
- if muscle weakness improves- dose is too low
- if muscle weakness increases- dose is too high– due to depolarizing blockade
physostigmine
mech
Crosses BBB*****
direct agonist effects at nicotinic receptors
physositgmine
tx
DRUG OF CHOICE FOR ANTICHOLINERGIC POISONING (AKA ATROPINE OVERDOSE)
ambenobium
tx
Myasthenia Gravis
4a amine- doesn’t cross BBB
Carbaryl
tx
used as insecticide
what drugs are used to Tx Alzheimers
Galantamine
Rivastigmine
Donepezil
Galantamine
mech + tx
AchE inhibitor
Tx Alzheimers
Rivastigmine
mech + tx
AchE inhibitor
Tx Alzheimers AND Parkinsons
Dopenezil
mech + tx
reversible anticholinesterase with a better selectivity for AchE (better than the other inhibitors)
Tx Alzheimers
what drugs are 4a amines
pyridostigmine
neostigmine
endrophobium
( ambenobium )
what drugs are irreversible cholinesterase inhibitors
Echothiophate (phospholine)
Thiophosphate insectisides [Malathion + parathion ]
Nerve Agents [Sarin, Soman, Tabun Vx]
Ectothiophate (phospholine)
mech + tx
irreversible
low lipid solubility (no CNS involvement)
Tx glaucoma
Malathion + Parathion
mech + Tx
irreversible
thiophosphate insecticides
Malathion is converted into non toxic metabolites by birds and mammals
parathion isnt- more dangerous
Nerve agents
examples and mech
Sarin, Soman, Tabum, Vx
extremely strong irreversible cholinesterase inhibitors, much greater intrinsic toxicity than the thiophosphate insecticides
act on Nicotinic and muscarinic receptors to produce (DUMBBELS and MATCH)
Nerve agents effect on CNS
irritability, guiddiness, lethargy, amnesia, coma seizures and RESPIRATORY DEPRESSION ( cause of death)
Tx for Nerve agents
effect of pyridostigmine??
Pralidoxime before aging process occurs
Atropine (anticholinesterase inhibitor)
pyridostigmine ( used prophillactically for people that have increased risk of exposure – since it is a reversible AchE inhibitor it can block the effect of nerve agents and it gives exposed people more time to be tx with pralidoxime and atropine)
