Module 2: pharmacodynamics

Pharmacodynamics

what a medicine does to the body

Ligand

a substance usually a molecule that forms a complex with a body protein to serve a biological purpose

three ways medicines may be in the body

- free
- bound to a receptor
- bound to a non-functional molecule in a cell/tissue

ligand-gated ion channel

Type of membrane receptor that has a region that can act as a "gate" when the receptor changes shape.

G-protein coupled receptors

sense molecules/lipids outside the cell and activate the g-protein, inside the cell, in which then stimulates cellular responses. (e.g enzymes)

Enzyme-linked receptors

binding of a ligand to an enzyme-linked receptor stimulates intracellular enzymatic activity. The enzyme-linked receptor has two functions- it is the receptor and possesses enzymatic activity.

stimulate, inhibit

When the medicine is distributed to the body. The medicine receptor complex initiates physiochemical reactions that stimulate or inhibit cellular functions.

why do some medicines inhibit while some stimulate cellular functions by binding to the same receptor?

some drugs (agonsit) bind to receptors and activate the receptor. other drugs (antagonist) can bind to the same receptor but block receptor activation

Antagonist

when a frug binds to a receptor but blocks its activation. as a result, the effects observed are often opposite to the stimulation of the receptor

agonist

when a drug stimulates a receptor. it mimics the engogenous transmitter.

affinity

refers to the strength of attraction between a drug on its receptor. drugs that are high in this are strongly attracted to their receptors

Specficity

related to a degree of selectivity. a drug is highly specific if it only interacts with one receptor type.

efficacy

is the ability of a drug to produce an effect at a receptor. it is a measure if the maximum biology effect resulting from a drug binding to its target e.g morphine is much more higher in this compared to paracetamol as it is a much more stronger pain kill

potency

describes the amount of drug needed to produce a desired effect. if you use more of this type of drug. a lower dose should be administered to produce the desired effects.

misuse

inappropriate use of medicines

drug dependence

the condition is which administration fo a substance is compulsory sought in the absence of a therapeutic indication e.g abuse of a pain killer

drug tolerance

is when repeated doses of a drug cause decreasing effects or if doses gave to be increased to maintain the same affect,

used to describe a medicine that has the same effect on a receptor as the endogenous chemical messenger?

agonist

used to describe a medicine that binds to a receptor, fails to activate it and prevents the endogenous chemical messenger from binding?

antagonist

used to describe a medicine that binds to a receptor, and activates it, but to a lesser extent than the endogenous chemical messenger?

partial agonist

inverse agonist

binds to a receptor and stabalises the inactive form of the protein such that endogenous messenger cannot bind

the maximum biological effect resulting from a medicine binding to its target

efficacy

the measure of how strongly a medicine binds to a receptor?

affinity

applies to the amount of medicine required to produce a defined biological effect?

potency

name the four main protein targets (receptor types) that ligands can bind to

ligand-gated channels, enzyme-linked receptor, G-protein linked receptor, and intracellular receptor.

Endogenous

produced from within; due to internal causes