Intro To Pharmacology Flashcards
What to drugs bind to?
Most drugs bind to proteins to exert their action.
what are the 4 classes of proteins targeted by drugs?
Enzymes, transporters, ions gated channels and receptors.
Define an agonist
Drug/chemical mediators that bind to a receptor to produce a response
They are bound within the pocket of a G-protein receptor
Define an antagonist
Drugs that inhibit the response of an agonist. They do NOT produce a response
What is a ligand
A ligand is any molecule that bind to a receptor
What is a bioassay?
A bioassay is a method used to determine the effect of a substance which is determined by the biological response it produces.
Why are bioassays important?
They are important for:
-Measuring the activity of the substance
-The unwanted side effects
-investigating the function of endogenous mediators
What is found within receptor families?
we find different subtypes with distinct subunit
DIFFERENT SUBUNITS HAVE DIFFERENT SUBUNITS
What can drugs that lack specificity cause?
Side affects
Why can drugs have different effects?
Because the same receptors are found in diffferent places around the body
What must drug molecules exert in order to produce a pharmacological response?
A chemical influence on one or more parts of a cell
Why are side effects caused by drugs that lack specificity?
Many receptors are found in more than one organ and drugs bind to receptors wherever they are located as a result leading to side effects
What do opioid receptors have and what do they do?
They have a natural receptor and they can increase the feeling of reward, relaxation and motivation
What is a G-coupled receptor?
A G-coupled receptor is a family of proteins that act as molecular switches inside cells. They are responsible for transmitting signals from outside a cell to its interior.
How can paracrine signalling be affected by drugs acting on RECEPTORS?
*Paracrine signalling is local signalling
-Mast cells located under skin detect allergen
-Activated mast cells secrete mediators e.g. histamine which act LOCALLY to produce vasodilation and activate neurons involved in itch
-Allergy medicines contain drugs that block receptors for histamine
How can paracrine signalling be affected by drugs acting on enzymes?
*think of inflammation
-Prostaglandins are lipid-derived paracrine mediators that cause inflammation
-Drugs like paracetamol can target enzymes that synthesise the mediators
What does CAR T stand for?
Chimeric Antigen Receptor T cell therapy
What is CAR T immunotherapy?
its a type of immunotherapy that uses the patient’s own immune cells to fight cancer.
What are CARs?
they are receptors designed to recognise and bind to specific proteins on the surface of cancer cells.
How does CAR T immunotherapy work?
T cells collection
Genetic engineering - producing CARs
T cell expansion - growing more (modified) T cells in the lab
T cell infusion - inject back into patient
What type of signalling does CAR T immunotherapy use?
Contact Dependent Signalling
What drugs can affect Paracrine Signalling?
Drugs acting on receptors - e.g. antihistamine (this is also an example of an antagonist)
Drugs acting on enzymes - e.g. paracetamol (targets enzymes which synthesise he mediators for signalling)
What does Nitric Oxide do?
it causes relaxation of smooth muscle cells and vasodilation
How does Viagra maintain an erection?
it inhibits the enzyme responsible for the breakdown of cGMP, allowing smooth muscles to relax and so maintains a good bloodflow to the penis
How does Botox work?
its a toxin (drug) targetting the machinary involved in the release of neurotransmitters in the area its injected
it cleaves proteins which are part of the synaptic machinary (paralyses local muscles)
over time new proteins can be made to replace the ones that have been cleaved
Which agonist and antagonist work on a nicotinic acetyl choline receptor?
agonist –> nicotine
antagonist –> curare
Which agonist and antagonist work on a Mucarini acetyle choline receptor?
agonist –> Muscarine
antagonist –> Atropine
What’s Anaphylaxis?
Allergic reaction
CAUSES airways to get blocked - no breathing = fatal
EpiPen is used for treatment - Adrenaline shot which causes the airway muscle to relax allowing the person to breathe
