Pharm NMJ part II Flashcards
what are the clinical uses of NMJ blocking drugs
surgical relaxation
endotracheal intubation
control of ventilation
how do NMJ blockers help control ventilation
reduce chest wall R and improve thoracic compliance
permit adequate gas exchange and prevents atelectasis in patients who have ventilatory failure
pancuronium and vecuronium most common if >24 hours
MOA dantrolene
inhibition of RYR Ca Ch blocking release of Ca from SR and so no muscle contraction
side effects dantrolene
generalized muscle weakness, sedation, and occasionally hepatitis
what is dantrolene used for
Tx for spascitiy associated with UMN disorders and management of malignant hyperthermia
what patients are at risk for malignant hyperthermia
hereditary mutations in RyR gene
permits excessive Ca release from SR under certain triggering agents
increase Ca, increase lactic acid, increase temperature
what do we use to reduce Ca in malignant hyperthermia
IV dantrolene
MOA botulinum toxin
cleaves SNARE and blcoks release of ACh by preventing vesicle exocytosis
what is botulinum used for
generalized spastic disorders, cervical dystonia and blepharospasm
what are direct acting cholinomimetics
bind and activate mAChR and nAChR
what are indirect acting cholinesterase inhibitors
inhibit AChE increasing ACh in the celft
where is butyrylcholinesterase made
liver and found inliver and plasma
AChE is found where
highly [ ] postsynaptic end plate and prevents lateral diffusion from adjacent nAChRs
primary target for cholinesterase inhibiting drugs
AChE but also block BuChE
3 chemical groups of cholinesterase inhibitors
Alcohols
Carbamic acid esters
Organophosphates
how does alcohol work as AChE inhibitor
+ charged quaternary ammonium that binds to AChE noncovalently
how do carbamic acid esters work like AChEI
quaternary and tertiary ammonium groups that bind to AChE noncovalently
which AChEI are carbacmic acid esters
neostigmine, pyridostigmine, physostigmine, carbaryl
what AChEI are alcohols
edrophonium
what AChEI are organophosphates
echothiophate, parathion and malathion, sarin, soman, tabun
what is a precaution with organophosphates
CNS toxicity since neutrally charged and lipid soluble
bond between organophosphates and AChE
covalent and irreversible