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  • β2 Agonists Mechanism of Action and Drug Examples

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    Mohamed Ismail
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    The document provides information about beta-2 agonists including their mechanism of action, therapeutic uses for treating conditions like asthma and COPD, examples of short-acting, long-acting, and ultra-long acting beta-2 agonists, and some of their key characteristics. It includes tables and diagrams showing the names of specific beta-2 agonists and notes about their structures, durations of action, and common uses.

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    Beta - 2 Agonists

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    The document provides information about beta-2 agonists including their mechanism of action, therapeutic uses for treating conditions like asthma and COPD, examples of short-acting, long-acting, and ultra-long acting beta-2 agonists, and some of their key characteristics. It includes tables and diagrams showing the names of specific beta-2 agonists and notes about their structures, durations of action, and common uses.

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    13 views13 pages

    β2 Agonists Mechanism of Action and Drug Examples

    Uploaded by

    Mohamed Ismail
    The document provides information about beta-2 agonists including their mechanism of action, therapeutic uses for treating conditions like asthma and COPD, examples of short-acting, long-acting, and ultra-long acting beta-2 agonists, and some of their key characteristics. It includes tables and diagrams showing the names of specific beta-2 agonists and notes about their structures, durations of action, and common uses.

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    of 13

    2021

    β 2 Agonists

    Lab D2.1
    Group D1.1
    Mechanism of action
    • β adrenergic receptors are coupled to a Gs protein of adenylyl
    cyclase.
    • This enzyme produces the second messenger cAMP.
    • cAMP decreases calcium within cells and activates protein
    JANUARY 2021

    kinase A.
    • Inactivate myosin light-chain kinase.
    • Activate myosin light-chain phosphatase.

    S M T W T F S

    1 2
    3 4 5 6 7 8 9

    10 11 12 13 14 15 16

    17 18 19 20 21 22 23

    24 25 26 27 28 29 30

    31
     They are synthetic non – catecholamines.
    • Pharmacological effects:
    1- Bronchodilatation.
    2- Uterine relaxation.
    3- Decreased peripheral resistance.
    FEBRUARY 2021

    • Therapeutic uses:
    1- Used in ttt of bronchial asthma & COPD.
    2- Used to delay preterm labour.

    S M T W T F S

    1 2 3 4 5 6

    7 8 9 10 11 12 13

    14 15 16 17 18 19 20

    21 22 23 24 25 26 27

    28
    MARCH 2021 Adverse effects

    Agitation Tremors Insomnia

    S M T W T F S

    1 2 3 4 5 6

    7 8 9 10 11 12 13

    14 15 16 17 18 19 20

    21 22 23 24 25 26 27

    29 29 30 31
    Tachycardia
    APRIL 2021 (Short – acting) Salbutamol (albuterol)

    S M T W T F S
    SAR
    1 2 3  The tertiary butyl group makes it more selective
    for β2 receptor.
    4 5 6 7 8 9 10
     The drug is sold in racemic mixture.
    11 12 13 14 15 16 17
     (S) – enantiomer blocks metabolism pathway.
    18 19 20 21 22 23 24
     while (R) – enantiomer shows activity.
    25 26 27 28 29 30
    MAY 2021 (SABA) Terbutaline

    S M T W T F S

    1
    • The tertiary butyl
    2 3 4 5 6 7 8 group increases β2
    • Resorcinol ring increases
    9 10 11 12 13 14 15 receptor selectivity.
    β2 receptor selectivity.
    16 17 18 19 20 21 22 • Not metabolized by
    • Not metabolized by MAO.
    23 24 25 26 27 28 29
    COMT.
    30 31
    Ritodrine
    Used to stop preterm
    labor
    JUNE 2021 (SABA)

    S M T W T F S

    1 2 3 4 5

    6 7 8 9 10 11 12

    13 14 15 16 17 18 19

    20 21 22 23 24 25 26 the 4-hydroxy group makes it susceptible


    to metabolism by COMT.
    27 28 29 30
    JULY 2021 (Long – acting) Salmeterol

    S M T W T F S

    1 2 3
    - This bulkiness makes the compound
    4 5 6 7 8 9 10 more lipophilic and makes it selective to
    β2 adrenergic receptors.
    11 12 13 14 15 16 17

    18 19 20 21 22 23 24
    - Its effect lasts for 12 hours.
    25 26 27 28 29 30 31
    AUGUST 2021 (LABA) Formoterol

    S M T W T F S

    1 2 3 4 5 6 7

    8 9 10 11 12 13 14

    15 16 17 18 19 20 21

    22 23 24 25 26 27 28
     Used in combination with fluticasone
    29 30 31 propionate and budesonide.
    SEPTEMBER 2021 (LABA) Bambuterol

    S M T W T F S

    1 2 3 4
    - It is a prodrug of terbutaline.
    5 6 7 8 9 10 11

    12 13 14 15 16 17 18 - Which make it has longer


    duration of action.
    19 20 21 22 23 24 25

    26 27 28 29 30
    OCTOBER 2021 (Ultra – LABA) Indacaterol

    S M T W T F S

    1 2
    3 4 5 6 7 8 9

    10 11 12 13 14 15 16

    17 18 19 20 21 22 23 It needs to be taken
    24

    31
    25 26 27 28 29 30
    once daily
    NOVEMBER 2021 (Ultra – LABA) Olodaterol

    S M T W T F S

    1 2 3 4 5 6

    7 8 9 10 11 12 13

    14 15 16 17 18 19 20

    21 22 23 24 25 26 27

    28 29 30
    Synthesis
    DECEMBER 2021 (Ultra – LABA) Vilanterol

    S M T W T F S

    1 2 3 4 In combination with
    In combination with muscarinic
    5 6 7 8 9 10 11 corticosteroid antagonist
    12 13 14 15 16 17 18
     It has structural similarity to salmeterol.
    19 20 21 22 23 24 25

    26 27 28 29 30 31

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