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Understanding Drug Antagonism Types

Buspirone is a selective agonist for the serotonin 5-HT1A receptor. It works by activating 5-HT1A receptor activity, which helps modulate processes in the body like decreasing heart rate and blood pressure, causing vasodilation, and relieving anxiety. Naloxone is a competitive antagonist that binds to opioid receptors and blocks the effects of opioids like heroin and morphine, reversing their effects and causing withdrawal symptoms. Competitive antagonists compete with agonists for the same receptor binding site, while non-competitive antagonists bind elsewhere on the receptor to prevent its activation.

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Muhammad Masroor
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124 views4 pages

Understanding Drug Antagonism Types

Buspirone is a selective agonist for the serotonin 5-HT1A receptor. It works by activating 5-HT1A receptor activity, which helps modulate processes in the body like decreasing heart rate and blood pressure, causing vasodilation, and relieving anxiety. Naloxone is a competitive antagonist that binds to opioid receptors and blocks the effects of opioids like heroin and morphine, reversing their effects and causing withdrawal symptoms. Competitive antagonists compete with agonists for the same receptor binding site, while non-competitive antagonists bind elsewhere on the receptor to prevent its activation.

Uploaded by

Muhammad Masroor
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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 AGONIST:

An agonist is a chemical OR drug that binds


to a receptor and activates the receptor to
produce a biological response that is an agonist
causes an action.
For Example: Buspirone is a selective agonist for
serotonin 5-HT1A receptor.
MECHANISM OF ACTION:
5-HT1A receptors works for neuromodulation in the
body i.e. decreasing heart rate, blood pressure,
vasodilation and relieving anxiety. Buspirone is a
drug that activates 5HT1A receptor activity.
 An antagonist is a type of receptor ligand or drug that
blocks or dampens a biological response by binding to and
blocking a receptor . They are sometimes called blockers;
examples include alpha blockers, beta blockers,
and calcium channel blockers.
 In pharmacology, antagonists have affinity but no efficacy
for their cognate receptors, and binding will disrupt the
interaction and inhibit the function of an agonist or inverse
agonist at receptors.

TYPES OF PHARMACOLOGIC ANTAGONIST:


1. Competitive Antagonist:
a) Reversible Antagonist
b) Irreversible Antagonist
2. Non-Competitive Antagonist

 Competitive antagonists bind to receptors at the


same binding site (active site) as the endogenous ligand or
agonist, but without activating the receptor.
 Agonists and antagonists "compete" for the same binding
site on the receptor.
 Once bound, an antagonist will block agonist binding.
Sufficient concentrations of an antagonist will displace the
agonist from the binding sites, resulting in a lower
frequency of receptor activation.
 FOR EXAMPLE:

Naloxone (also known as NALOX) is used to


reverse opioid overdose caused by drugs such
as heroin or morphine. It produces withdrawal symptoms by
competing for opiate receptor sites within the CNS (a
competitive antagonist, not a direct agonist), thereby
preventing the action of opiods.
a) REVERSIBLE ANTAGONIST:
Many antagonists are reversible antagonists that, like most
agonists, will bind and unbind a receptor. They form weak
bonds with the receptor and their maximal response is
concentration dependant.
b) IRREVERSIBLE ANTAGONIST:
An irreversible antagonist is a type of antagonist that binds
permanently to a receptor, either by forming a covalent
bond to the active site, or alternatively just by binding so
tightly that the rate of dissociation is effectively zero at
relevant time scales. Irreversible enzyme inhibitors that act
similarly are clinically used and include drugs such
as aspirin, omeprazole and monoamine oxidase inhibitors.

 non-competitive
antagonist binds to an
allosteric (non-agonist)
site on the receptor to
prevent activation of the
receptor.

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