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  • H01043-Hoá Dươc 2-Lecture 4-Antiparkinsons Drugs

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    This document discusses antiparkinsonian drugs. It begins by outlining the goals of understanding how Parkinson's disease develops from neuronal death and how various drugs work to elevate dopamine levels in the brain. Parkinson's disease results from the progressive degeneration of dopaminergic neurons in the substantia nigra, disrupting the balance between dopamine and acetylcholine. Common drugs for Parkinson's include L-DOPA which is converted to dopamine in the brain, COMT and MAO-B inhibitors which prolong the effects of L-DOPA, dopamine agonists which mimic dopamine, and muscarinic antagonists which balance acetylcholine levels.

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    This document discusses antiparkinsonian drugs. It begins by outlining the goals of understanding how Parkinson's disease develops from neuronal death and how various drugs work to elevate dopamine levels in the brain. Parkinson's disease results from the progressive degeneration of dopaminergic neurons in the substantia nigra, disrupting the balance between dopamine and acetylcholine. Common drugs for Parkinson's include L-DOPA which is converted to dopamine in the brain, COMT and MAO-B inhibitors which prolong the effects of L-DOPA, dopamine agonists which mimic dopamine, and muscarinic antagonists which balance acetylcholine levels.

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    15 views20 pages

    H01043-Hoá Dươc 2-Lecture 4-Antiparkinsons Drugs

    Uploaded by

    KTrọng Nghĩa
    This document discusses antiparkinsonian drugs. It begins by outlining the goals of understanding how Parkinson's disease develops from neuronal death and how various drugs work to elevate dopamine levels in the brain. Parkinson's disease results from the progressive degeneration of dopaminergic neurons in the substantia nigra, disrupting the balance between dopamine and acetylcholine. Common drugs for Parkinson's include L-DOPA which is converted to dopamine in the brain, COMT and MAO-B inhibitors which prolong the effects of L-DOPA, dopamine agonists which mimic dopamine, and muscarinic antagonists which balance acetylcholine levels.

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    of 20

    Lecture 4

    Antiparkinson’s drugs
    Phuong-Thuy Thi PHAN, M.S.
    Recommended Reading
    1) Beale, J.M., Block, J.H. (2011). Wilson and Gisvold’s Textbook
    of Organic Medicinal and Pharmaceutical Chemistry 12th
    Lippincott Williams & Wilkins: Baltimore. edition,
    dopaminergic signalingChapter
    agents, p.p. 471-490. 13.
    Central
    2) Beale, J.M., Block, J.H. (2011). Wilson and Gisvold’s Textbook of
    Organic Medicinal and Pharmaceutical Chemistry 12th edition,
    Lippincott Williams & Wilkins: Baltimore. Chapter 17. Cholinergic
    drugs and related agents, p.p. 558-606.

    3) Thomas L.L., David A.W. (2013). Foye’s Principle of Medicinal


    Chemistry 7th edition, Lippincott Williams & Wilkins:
    Chapter 13. Drugs used to treat neuromuscular Baltimore.
    antiparkinsonian and spasmolytic agents, p.p. 419-437.
    2
    5/8/2020 H01043-LECTURE 4-ANTIPARKINSON'S DRUGS disorders:
    Goals
    1) Know the MPP+ neurotoxicity and other toxic compounds that can
    lead to nigrostriatal neuronal death

    2) Demonstrate how L-DOPA/ carbidopa elevates dopamine levels

    3) Desmonstrate how COMT and MAO-B inhibitors elevate L-DOPA/


    carbidopa/ dopamine levels

    4) Describe properties of muscarinic antagonists as a


    means to balance ACh/ DA input

    5/8/2020 3
    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Parkinson’s disease
    • Progressive degeneration of nigrostriatal dopaminergic neurons with
    a resultant loss of dopaminergic/ cholinergic balance

    • Symptoms include muscle tremor, rigidity, bradykinesia…

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Biosynthesis of dopamine

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Metabolism of dopamine

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Central dopadecarboxylase

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Chemical induction of Parkinson’s disease

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Central dopadecarboxylase

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Peripheral dopadecarboxylase

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    COMT inhibitors

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    MAO-B inhibitors

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    MAO-B inhibitors

    Active site - directed irreversible enzyme inhibition

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    MAO-B inhibitors

    Radical scavenger

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    MAO-B inhibitors
    Metabolism

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Dopamine agonists

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Dopamine agonists

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Muscarinic antagonists

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Adenosine antagonists

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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS
    Diagnostic imaging agents

    Image available from https://www.parkinson.org/blog/whats-hot/update-DAT-scanning


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    H01043-LECTURE 4-ANTIPARKINSON'S DRUGS

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