Pharmacology of Physostigmine and Neostigmine
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Questions and Answers

What is a significant difference between Physostigmine and Neostigmine regarding their source?

  • Physostigmine is derived from natural sources. (correct)
  • Neostigmine is a naturally occurring alkaloid.
  • Both are synthetic drugs.
  • Physostigmine is a synthetic compound.
  • Which of the following pharmacologic actions is not associated with Physostigmine?

  • Direct stimulation of the heart (correct)
  • Stimulation of skeletal muscle
  • CNS stimulation
  • Muscarinic action
  • What is the primary mechanism by which Physostigmine produces miosis in the eye?

  • Direct stimulation of the iris
  • Inhibition of myoneural junction
  • Accumulation of acetylcholine (correct)
  • Stimulation of AChE
  • What is a common therapeutic use for Neostigmine?

    <p>Management of myasthenia gravis (A)</p> Signup and view all the answers

    What type of compound is Physostigmine classified as?

    <p>Tertiary amine (D)</p> Signup and view all the answers

    What is the role of pralidoxime in relation to organophosphate poisoning?

    <p>Regenerates cholinesterase (C)</p> Signup and view all the answers

    Why is it important to administer pralidoxime quickly after organophosphate exposure?

    <p>To prevent enzyme aging (A)</p> Signup and view all the answers

    Which of the following is not a special effect of Physostigmine on the eye?

    <p>Increased intraocular pressure (B)</p> Signup and view all the answers

    What mechanism leads to the miosis effect of Physostigmine on the eye?

    <p>Inhibition of cholinesterase, causing acetylcholine accumulation (D)</p> Signup and view all the answers

    What is a main therapeutic application of Neostigmine?

    <p>Management of myasthenia gravis (B)</p> Signup and view all the answers

    Which characteristic differentiates Physostigmine from Neostigmine in terms of lipid barrier penetration?

    <p>Physostigmine penetrates lipid barriers while Neostigmine does not (C)</p> Signup and view all the answers

    What is the primary source of Physostigmine?

    <p>Natural plant alkaloid (D)</p> Signup and view all the answers

    What effect does Physostigmine have on the gastrointestinal tract?

    <p>Increased motility (A)</p> Signup and view all the answers

    Pralidoxime is most effective when administered within what timeframe after organophosphate exposure?

    <p>12 hours (B)</p> Signup and view all the answers

    Which of the following effects is NOT associated with Neostigmine?

    <p>Miosis (D)</p> Signup and view all the answers

    How does Physostigmine assist in postoperative urinary retention?

    <p>By stimulating bladder contraction (D)</p> Signup and view all the answers

    Flashcards

    Physostigmine (Eserine)

    A natural plant alkaloid that inhibits acetylcholinesterase (AChE), leading to increased acetylcholine levels at various sites, causing muscarinic, nicotinic, and central nervous system (CNS) effects. It can cross the blood-brain barrier.

    Neostigmine

    A synthetic drug that inhibits acetylcholinesterase (AChE) and is used to increase acetylcholine levels. Unlike physostigmine, it does not readily cross the blood-brain barrier.

    Pralidoxime

    A drug that specifically reactivates cholinesterase enzymes that have been inhibited by organophosphate poisons, like those found in pesticides. It works by breaking the bond between the organophosphate and the enzyme.

    Penetration of Lipid Barriers

    The ability of a drug to cross the blood-brain barrier, which separates the bloodstream from the central nervous system. Drugs that can cross this barrier can affect the brain.

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    Cholinergic Action

    The actions of a drug that are related to the release or stimulation of acetylcholine, leading to changes in muscle activity, heart rate, and other bodily functions.

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    Muscarinic Action

    A specific type of cholinergic action that affects muscle movement. This action can be either direct (stimulating muscle directly) or indirect (acting on acetylcholine receptors in the muscle).

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    Nicotinic Action

    A specific type of cholinergic action that affects skeletal muscle, primarily by acting on receptors at the neuromuscular junction, leading to muscle contraction.

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    Anticonvulsants

    Drugs that relieve or prevent convulsions, often used to treat epilepsy and other seizure disorders.

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    Acetylcholinesterase inhibitor (AChEI)

    A chemical compound that blocks the enzyme acetylcholinesterase (AChE), leading to an accumulation of acetylcholine at various sites in the body.

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    Blood-brain barrier penetration

    The ability of a substance to cross the blood-brain barrier, a protective membrane that separates the bloodstream from the central nervous system.

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    Study Notes

    Physostigmine (Eserine) and Neostigmine

    • Physostigmine (Eserine): Natural plant alkaloid, tertiary amine, good absorption
    • Neostigmine: Synthetic, quaternary ammonium compound, poor and irregular absorption
    • CNS Penetration:
      • Physostigmine: Crosses the blood-brain barrier, stimulating the CNS
      • Neostigmine: Does not cross the blood-brain barrier
    • Mechanism of Action: Both inhibit acetylcholinesterase (AChE), leading to acetylcholine accumulation, producing:
      • Muscarinic effects: More pronounced on the gastrointestinal tract (GIT) and urinary bladder
      • Nicotinic effects
      • CNS stimulation (Physostigmine only)
      • Peripheral actions: AChEI and direct stimulant action on skeletal muscle.
    • Special Effects (Physostigmine):
      • Eye: Miosis (constriction of pupils), decreased intraocular pressure (IOP), ciliary muscle contraction (for near vision), lacrimation.
    • Action on Skeletal Muscle:
      • Stimulation via AChE inhibition at the myoneural junction
      • Direct stimulant action
    • Therapeutic Uses (Physostigmine):
      • Glaucoma treatment (less common now)
      • Antidote to atropine overdose (or other antimuscarinic drugs)
      • Stimulate GIT and bladder (e.g., paralytic ileus, post-operative urinary retention)
    • Therapeutic Uses (Neostigmine):
      • Myasthenia gravis management (with atropine to block muscarinic receptors)
      • Antidote for competitive neuromuscular-blocking agents (NMBs)

    Pralidoxime

    • Use: Regenerate cholinesterase after organophosphate poisoning by breaking the phosphorus bond.
    • Importance of Timing: Must be administered as soon as possible after exposure (ideally within 12 hours) due to "aging" of the enzyme.
    • Mechanism: High affinity for phosphorus, enabling it to regenerate the enzyme.

    Anticonvulsants

    • Example: Diazepam

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    Description

    This quiz explores the pharmacological properties of Physostigmine and Neostigmine, including their absorption, CNS penetration, and mechanisms of action. Understand the distinctions between these two compounds and their effects on the autonomic nervous system and skeletal muscle.

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