What happens in Myasthenia Gravis? Antibodies attack the postsynaptic ACh receptor at the
NMJ.
What is the MOA of anticholinesterases? They bind AChE to inhibit the breakdown of ACh,
leading to an increase in ACh in the cleft.
What is the therapeutic effect of anticholinesterases? They reverse muscle weakness and
fatigue.
What are the adverse effects of anticholinesterases? Nausea, abdominal cramps, diarrhea
(muscarinic side effects of ACh), muscle cramps (nicotinic activity), rare cases of bradycardia,
hypotension, excessive airway secretions. Excessive administration can result in increased
muscle weakness.
What is physostigmine? It is the first discovered anticholinesterase that forms a reversible
covalent bond with AChE and can pass through the BBB.
What is pyridostigmine? It is a longer-acting and frequently used anticholinesterase for MG
today. It forms a reversible covalent bond with AChE but cannot pass through the BBB. Its
duration of action is 3-6 hours.
,What is neostigmine? It has a shorter duration of action and a higher rate of GI effects
compared to pyridostigmine. It forms a reversible covalent bond with AChE but cannot pass
through the BBB.
What is edrophonium? It is a short-acting anticholinesterase that transiently binds to AchE
through electrostatic hydrogen bonds. It cannot pass through the BBB. It is used to differentiate
between a MG disease exacerbation and excessive anticholinesterase medication intake.
What is a myasthenia crisis? It is an acute exacerbation of MG.
What are the symptoms of anticholinesterase overdose? Decreased HR & BP,
bronchospasm, diarrhea, muscle weakness, sialorrhea, bronchorrhea, miosis
What are the symptoms of cholinergic crisis? Increased HR & BP, respiratory distress,
mydriasis
What happens when a small dose of edrophonium is given in case of disease exacerbation?
Symptoms improve
What happens when a small dose of edrophonium is given in case of anticholinesterase
overdose? Symptoms worsen
, What are some examples of immune modulators? Corticosteroids, cyclosporine,
azathioprine, tacrolimus, rituximab
How do high dose glucocorticoids reduce the risk of needing post-op ventilatory support?
Not specified
What are some common psychostimulants? Amphetamine, Methylphenidate, Modafinil
What are the common names for amphetamine? Adderall, Dexedrine, Desoxyn
What is the class and mechanism of amphetamine? Noncatecholamine sympathomimetic
amine- enhances dopaminergic, serotonergic, & non-adrenergic release in neural network
specific regions via complex transporter effects
What is the class and mechanism of methylphenidate? Norepinephrine & dopamine
reuptake inhibitor. Blocks the dopamine transporter (DAT). Has regionally specific effects
similar to amphetamine.
What is the class and mechanism of modafinil? Mechanism is unclear. Does not appear to
involve dopamine or noradrenergic pathways. May involve glutamatergic & GABAergic effects
How is amphetamine metabolized? CYP 2D6 (no active metabolites)