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Adrenergic Drugs I

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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123 views3 pages

Adrenergic Drugs I

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.

Uploaded by

Mirumbi Kefa Momanyi
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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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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