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  • Compare and Contrast Neostigmine and The Organophosphate Compounds

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    DonkeyMan
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    Neostigmine and organophosphates are acetylcholinesterase inhibitors that compete with acetylcholine for binding sites on acetylcholinesterase, increasing acetylcholine levels at nicotinic and muscarinic receptors. Neostigmine reversibly inhibits the enzyme through hydrolysis of its carbamate bond, while organophosphates cause irreversible inhibition via a phosphate covalent bond. Organophosphates can more easily cross the blood-brain barrier, potentially causing central nervous system effects like seizures. Both drug classes result in similar peripheral effects through muscarinic and nicotinic receptor stimulation such as bradycardia, bronchoconstriction, and increased gastrointestinal motility.

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    compare and contrast neostigmine and the organophosphate compounds

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    Neostigmine and organophosphates are acetylcholinesterase inhibitors that compete with acetylcholine for binding sites on acetylcholinesterase, increasing acetylcholine levels at nicotinic and muscarinic receptors. Neostigmine reversibly inhibits the enzyme through hydrolysis of its carbamate bond, while organophosphates cause irreversible inhibition via a phosphate covalent bond. Organophosphates can more easily cross the blood-brain barrier, potentially causing central nervous system effects like seizures. Both drug classes result in similar peripheral effects through muscarinic and nicotinic receptor stimulation such as bradycardia, bronchoconstriction, and increased gastrointestinal motility.

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    2 views1 page

    Compare and Contrast Neostigmine and The Organophosphate Compounds

    Uploaded by

    DonkeyMan
    Neostigmine and organophosphates are acetylcholinesterase inhibitors that compete with acetylcholine for binding sites on acetylcholinesterase, increasing acetylcholine levels at nicotinic and muscarinic receptors. Neostigmine reversibly inhibits the enzyme through hydrolysis of its carbamate bond, while organophosphates cause irreversible inhibition via a phosphate covalent bond. Organophosphates can more easily cross the blood-brain barrier, potentially causing central nervous system effects like seizures. Both drug classes result in similar peripheral effects through muscarinic and nicotinic receptor stimulation such as bradycardia, bronchoconstriction, and increased gastrointestinal motility.

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    of 1

     Neostigmine and organophosphates are acetylcholinesterase inhibitors, compete with Ach for binding to

    anti-cholinesterase, thus increase [Ach] at nAchR and mAchr (also some action on plasma cholinesterase)
     ACE rapidly hydrolyses Ach, anionic site binds the quaternary amine of Ach, esteratic site hydrolyses the
    ester bond releasing choline and acetylating the esteratic site, acetylated esteratic site then rapidly
    hydrolysed to release acetic acid

    neostigmine Organophosphates
    Pharmaceutics
     MOA  Quaternary amine group of  Quaternary amine group binds to
    neostigmine binds to anionic site, anionic site, ester bond of
    ester bond of neostigmine is organophosphate binds to esteratic
    hydrolysed by esteratic site of ACE, site of ACE, results in phosphate
    results in transfer of a carbamate based covalent bond, inactivating
    group to esteratic site inactivating ACE
    ACE  Phosphate based covalent bond
     Carbamate bond undergoes hydrolysis does not undergo hydrolysis, thus is
    (T1/2 20mins), thus is reversible irreversible, reactivation of ACE
    relies on synthesis of new enzyme
    (months)
     Includes sarin gas, pesticides,
    echothiopate (glaucoma)
    Pharmacokinetics  IV or PO  Inhibition of ACE is irreversible,
     Onset 5 mins, peak effect 10 mins, relies on new synthesis of ACE
    duration 1 hr enzyme
     Quaternary amine group – poor lipid  Tertiary amine – high lipid solubility,
    solubility, does not cross BBB does cross BBB (therefore CNS
     50% excreted unchanged in urine, symptoms below), can be easily
    50% metabolised (by liver and plasma absorbed from skin, lungs GIT
    esterases, there is an active
    metabolite)
     T1/2B 1hr
    Pharmacodynamics
     CNS  Minimal, quaternary ammonium  Tertiary amine, crosses BBB,
    excitation, agitation, confusion,
    seizures, respiratory depression
     CVS  Bradycardia, hypotension  Similar
     Resp  Bronchoconstriction, increased  Similar
    secretions/lacrimation/salivation
     GIT  Increased peristalsis, NV, diarrhoea  Similar
     Urinary  Increased frequency  Similar
     MSK  Increased transmission at NMJ,  Similar
    reversal of ND NMDs (dose
    0.04mg/kg), fasciculation, muscle
    weakness

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