1 Flashcards
Presynaptic toxin that prevent fusion of the vehicle with membrane:
Botulinum
Therapeutic uses of Butulinum toxin:
1) bleopharospasm: uncontrolled contraction of eyelid
2) cerebral palsy: reduce muscle rigidity and uncontrolled spasms
Drugs inhibitAchE:
Anticholinestrases
E.g. organophosphate insecticides
Examples of reversalble anticholinstrase:
Edrophonium
Neostigmine
Physostigmine
Pyridostigmine
Examples of irreversible effects (long acting) antiCholinestrase:
Organophosphate compounds:
Isoflurophate
Parathion
Malathion
what are the amplifiers of endogenous ACh:
AntiCholinestrase
Therapeutic uses of anticholinestrase :
1) Myasthenia gravus (NMJ)
2) Alzheimer’s disease (CNS)
3) To reverse the neuromuscular blockade produced
during surgical anesthesia by neuromuscular blocker
4) Overdosage of Atropine(anticholinergic), Tricyclic antidepressant
Drugs uses to treat Myasthenia gravis:
Neostigmine
Pyridostigmine
Drugs used to treat Alzheimer’s disease:
Donepezil
Galantamine
Rivastigmine
Drugs used to reverse the neuromuscular blockade produced during surgical anesthesia by neuromuscular blocker:
neostigmine
edrophonium
Drugs used to treat Overdosage of Atropine, Tricyclic antidepressant:
physostigmine
Treatment of anticholinesterase overdose / poisoning:
1) Artificial ventilation if necessary
2) Block muscarinic actions of ACh(Atropine)
3) Cholinesterase reactivator (Pralidoxime & obidoxime)
4) The oximes have high affinity for the phosphorus atom & can hydrolyze the phosphorylated enzyme
and regenerate active enzyme from the
organophosphorus-cholinesterase complex.
Cholinesterase reactivator
oximes( pralidoxime and obidoxime)
muscarinic agonists
parasympathomimetics
muscarinic antagonists
parasympatholytics
Examples of muscarinic agonists:
Choline esters: Acetylcholine Methacholine Bethanechol carbachol
Natural alkaloids:
Pilocarpine
muscarine
nicotine.