Grp 2B.

Mechanism of Action Syeda Barjees

Pharmacodynamics Describes the biochemical interaction between a Sonia Alam
Pharmacodynamics is the study of how drugs interact drug and organism. Drugs do NOT induce new Sumaya Aslam
functions in tissues, they alter the rate or strength of Tania haq
with a molecular target, i.e.; effect of the drug on the
body. existing functions.
Tachyphylaxis
Enzyme Interactions
The receptor may become desensitized
Receptor Drug molecules selectively Non-Selective due to too much agonist stimulation
Protein molecules with one or more binding sites, bind to naturally occurring Receptor Interactions Interactions Drug resulting in diminished response. This
located on catalysts Drug molecules molecules physically phenomenon, called tachyphylaxis.
cell membranes. Receiv e a signal from the body’s selectively bind to interfere with, or
chemicals: neurotransmitters, hormones, enzymes. reactive sites on cell chemically alter cellular
Chemicalbinding surfaces
alters the enzyme structures & processes.. Down-regulation
interaction with
A decrease in total receptor number in the
normal target cell due to endocytosis and subsequent
Transmembrane ligand-gated lon channels Antagonists
molecules to 1 or degradation of the receptors caused by
more commonly, Agonists Bind to cell
Antagonism may occur either by blocking long-term exposure to agonists.
The extracellular portion of ligand-gated lon channels reaction rotes receptors to function
the drug’s ability to bind to the receptor or
contains the drug-binding site. The channel is usually by blocking its ability to activate the
closed until the receptor is activ ated by an agonist, receptor
Full Agonists
which opens the channel for a few milliseconds.
Allosteric antagonists Up-regulation of receptors
Depending on the ion conducted through these if a drug binds to a receptor Competitive antagonists
channels, these receptors mediate div erse functions, and produces a maximal if the antagonist binds to
An allosteric antagonist binds In which receptor reserv es are inserted into
including neurotransmission and muscle contraction. biologic response that mimics the same site on the
to a site (allosteric site) other the membrane, increasing the number of
the response to the receptor as the agonist
Enzyme-linked receptors in a rev ersible manner, it than the agonist-binding site receptors av ailable.
endogenous ligand, it is a full
agonist is “competitive and prevents receptor
This family of receptors undergoes activ ation by the agonist.
conformational changes when activ ated Partial Agonists Partial agonists Irreversible antagonists
by a ligand, resulting in increased hav e intrinsic activ ites greater Functional antagonism Desensitization
than zero but less than one rev ersible antagonists
intracellular enzyme activ ity. This response
bind cov alently to the An antagonist may act at a Repeated or continuous administration of
lasts for minutes to hours. Inverse Agonists activ e site of the completely separate receptor an agonist or antagonist often leads to
Transmembrane G protein-coupled receptors receptor, thereby initiating effects that are
inv erse agonists have an intrinsic changes in the responsiv eness of the
permanently reducing functionally opposite those of receptor.
There are many kinds of G proteins for example, Gs, activ ity less than zera, rev erse the number of receptors the agonist
Gi, and Gq. Gs: activ ates adenylyl cyclase → the activ ation state of receptors av ailable to the agonist
produces CAMP. Gi: inhibits the activation of and exert the opposite
pharmacological effect of
adenylyl cyclase. Gq: generates secondary
agonists.
managers (1. IP2 and 2. DAG)
Intracellular receptors Dose-response relationship
Toxic Dose 50% (ED50) The
Efficacy (emax) Alterations in absorption, dose which results in an
The primary targets of activated intracellular the maximum response to distribution, metabolism adverse effect in 50% of the Therapeutic Index (TI) Describes
receptors are transcription factors in the cell a drug produced in and excretion change sample population a margin of safety between the
nucleus that regulate gene expression. Other randomized control trials. effects of a giv en dose effectiv e and toxic dose
Potency (EC50) Effective Dose 50% (ED50)
targets of intracellular ligands are structural TI = TD50/ED50
the concentration of a The dose which results in
proteins, enzymes, RNA, and ribosomes. drug required to produce therapeutic effect in 50% of
50% of emax the sample population.