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    Adrenergic Drugs I

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    Mirumbi Kefa Momanyi
    Adrenergic drugs work by mimicking or stimulating the release of norepinephrine in the sympathetic nervous system. They are used therapeutically to treat life-threatening conditions like asthma attacks and shock. There are two main types of adrenergic receptor sites - alpha receptors, which are associated with constriction and relaxation of various muscles, and beta receptors, which relax bronchial muscles, increase heart rate and force of contractions, and divert blood from non-essential organs. The sites have features like anionic and hydrogen bonding sites that allow agonists like norepinephrine to bind.

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    Adrenergic Drugs I

    Uploaded by

    Mirumbi Kefa Momanyi
    98 views3 pages
    Adrenergic drugs work by mimicking or stimulating the release of norepinephrine in the sympathetic nervous system. They are used therapeutically to treat life-threatening conditions like asthma attacks and shock. There are two main types of adrenergic receptor sites - alpha receptors, which are associated with constriction and relaxation of various muscles, and beta receptors, which relax bronchial muscles, increase heart rate and force of contractions, and divert blood from non-essential organs. The sites have features like anionic and hydrogen bonding sites that allow agonists like norepinephrine to bind.

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    Adrenergic drugs work by mimicking or stimulating the release of norepinephrine in the sympathetic nervous system. They are used therapeutically to treat life-threatening conditions like asthma attacks and shock. There are two main types of adrenergic receptor sites - alpha receptors, which are associated with constriction and relaxation of various muscles, and beta receptors, which relax bronchial muscles, increase heart rate and force of contractions, and divert blood from non-essential organs. The sites have features like anionic and hydrogen bonding sites that allow agonists like norepinephrine to bind.

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    © All Rights Reserved
    Download as DOC, PDF, TXT or read online from Scribd
    Download as doc, pdf, or txt
    98 views3 pages

    Adrenergic Drugs I

    Uploaded by

    Mirumbi Kefa Momanyi
    Adrenergic drugs work by mimicking or stimulating the release of norepinephrine in the sympathetic nervous system. They are used therapeutically to treat life-threatening conditions like asthma attacks and shock. There are two main types of adrenergic receptor sites - alpha receptors, which are associated with constriction and relaxation of various muscles, and beta receptors, which relax bronchial muscles, increase heart rate and force of contractions, and divert blood from non-essential organs. The sites have features like anionic and hydrogen bonding sites that allow agonists like norepinephrine to bind.

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    Adrenergic Drugs I

    Introduction:

    Adrenergic nerves release norepinephrine as the


    neurotransmitter for the sympathetic nervous system. The
    sympathetic system activates and prepares the body for
    vigorous muscular activity, stress, and emergencies. Adren
    drugs stimulate the adrenergic nerves directly by mimickin
    action of norepinephrine or indirectly by stimulating the re
    of norepinephrine.

    Therapeutically, these drugs are used to combat life-threat


    disorders, which include acute attacks of bronchial asthma
    shock, cardiac arrest, and allergic reactions. In addition the
    drugs are used in nasal decongestants and appetite suppres

    Adrenergic Nerve Transmissions:

    Adrenergic nerves release the neurotransmitters:


    Norepinephrine (noradrenaline, NE), epinephrine, EP, and
    dopamine DA. The synthesis of the neurotransmitters DA
    NE and EP and the hormones NE and EP takes place by a
    pathway that involves 5 enzymes. Tyrosine is generally
    considered the starting point to synthesize DOPA (1a), DA
    (1b), and NE (1c). Norepinephrine is stored at (2).

    Norepinephrine is released from the nerve ending in respo


    a nerve impulse or drug (3). NE interacts with alpha and b
    receptor sites at (4). Its receptor action is terminated by
    recapture and storage in the original nerve ending or inacti
    by an enzyme. For example chloropheniramine, an
    antihistamine, can inhibit the mechanism for uptake and
    recapture of norepinephrine.

    There are at least two adrenergic receptor sites (alpha or b


    Norepinephrine activates primarily alpha receptors and
    epinephrine activates primarily beta receptors, although it
    also activate alpha receptors. Stimulation of alpha receptor
    associated with constriction of small blood vessels in the
    bronchial mucosa and relaxation of smooth muscles of the
    intestinal tract. Beta receptor activation relaxes bronchial
    smooth muscles which cause the bronchi of the lungs to di

    In addition beta receptor stimulatory effects cause an incre


    in the rate and force of heart contractions. As a result incre
    amounts of blood leave the heart and is diverted from nona
    organs to areas that actively participate in the body's reacti
    stress such as skeletal muscles, brain, and liver.
    Adrenergic Receptor Sites:

    Alpha Receptor Site: Important features of the site includ


    order of importance:

    1) An anionic site - which binds the positive ammonium g

    2) One hydrogen bonding area

    3) A flat area non-polar area for the aromatic ring.

    Beta Receptor Site: Important features of the site include


    order of importance - also see the graphic on the left:

    1) An anionic site - shown as Asp anionic negative acid gr


    which binds the positive ammonium group.

    2) Two hydrogen bonding areas - shown as two Serine wit


    alcohol (OH) groups hydrogen bonding to the phenol OH
    groups of the NE.

    3) A flat area non-polar area for the aromatic ring.

     
     Tissue Receptor  Agonists  Antago
    Subtype
      NE, EP,
    atenolol
     Heart   beta1 dobutamine,
    metopro
    xamoterol
      beta1,
     Adipose tissue    
    beta 3?
    Vascular Smooth  EP, salbutamol,
     beta 2 butoxam
    Muscle terbutaline, salmeterol
     terbutaline,
    Airway Smooth salbutamol,
      beta 2 butoxam
    Muscle salmeterol and
    zinterol,
     Smooth muscle  alpha 1  NE, EP, prazosin
    contraction phenylephrine, doxazoc
    oxymetazoline)
     Inhibition of
    clenbuterol, alpha- yohimb
    transmitter
    methylnoradrenaline, idazoxa
    release
     alpha 2 dexmedetomidine, atipame
    Hypotension,
    and mivazerol, efaroxan
    anaesthesia,
    clonidine, clenbuterol rauwols
    Vasoconstriction
    Receptor Sites
     alpha-receptor  beta-receptor
     Vasoconstriction  vasodilation (b2)
     iris dilation  cardioacceleration (b1)
     intestinal relaxation  intestinal relaxation (b2)
     intestinal sphincter
     uterus relaxation(b2)
    contraction
     bladder sphincter contraction  bronchodilation (b2)

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