Introduction to Pharmacology Flashcards
What is Thermodynamics?
The effect a drug has on the body (biological effects and mechanisms)
What is Pharmacokinetics?
How the body responds to the drug.
Name X3 Drug Targets
- Proteins
- DNA
- RNA
What are Agonistic Drugs?
Mimics a neurotransmitter and binds to a receptor to activate and produce a cellular response.
Explain the X3 step how an Agonistic drug functions.
1) Agonist binds to receptor, this is reversible. (Binding step)
2) Receptor undergoes a conformational. (Affinity Steps)
3) Change in receptor conformation which activates the receptor. This is temporary.
Are Agonistic and Antagonistic drugs effects reversible?
-YES
What X2 Features does Agonistic drugs have?
- Efficacy
- Affinity
What is Efficacy?
- The ability a drug has to evoke a cellular response
- (‘e’-effect)
What is Affinity?
- This is attraction between receptors and ligand (drugs)
- Determined by the chemical bonds between ligands and receptors.
What are Antagonistic Drugs?
-1) Bind to receptors (reversible) and block them. DO NOT ACTIVATE
Why do Antagonists not have Efficacy?
-They do NOT evoke e cellular response because they bind rot the receptor and block binding-No response occurs
What x2 types of graphs can show relationship between concentration and dose?
- Sigmoidal
- Hyperbolic- Logarithmic (more accurate)
Compare the Efficacies between Partial and Full Agonists
Partial-Low Efficacy
Full-High Efficacy
What is drug potency?
The amount of a drug that is needed to produce a given effect
What is Reversible Competitive Antagonism?
-When Antagonist drug blocking effect can be overcome by increasing the concentration of the Agonist drug.
What is the name of the site where Competitive Antagonists and Agonist drugs bind?
-Orthosteric Site
Where do Non-Competitive Antagonistic Drugs bind?
- Separate site
- Allosteric site
What X2 things happen to a curve graph when Competitive and Non-Competitive Antagonists bind?
Competitive- Parallel shift to RIGHT (competitive- always right :)
Non-Competitive- Depresses the slope
What affect does increasing concentration of an Agonist?
-Shifts curve to the RIGHT
What effect does increasing concentration of a Competitive Antagonist and Non-Competitive have?
Competitive-Shifts more to the right
Non-Competitive- Depresses slope further
What do Hydrophilic Signalling Molecules include?
neurotransmitters, hormones, endogenous molecules, peptides etc.
What are Ligand-Gated Ion Channels?
Open in response to ligand binding
-Transmembrane Proteins
What are G-Protein Coupled Receptors (GPCRs)?
Targeted by ‘Therapeutic Agents’-drugs
- Signal via Secondary Messenger Systems
- inbox for messages in the form of light energy, peptides, lipids, sugars, and proteins.
What are Kinase-Linked Receptors?
uses second messenger signaling that triggers a cascade of cellular events.
What are Nucleated Receptors?
- In nucleus
- Slow timescale-hours/days
- Alter gene expression
What type of channel are Voltage Gated Ion Channels: ?
- Ligand Gated
- Opne in response to voltage
How do G-Protein Coupled Receptors control effector activity?
-Secondary Messenger Systems
How are G-Protein Coupled Receptors linked to Secondary Messenger Systems?
-Intermediate-G-Proteins
What type of protein are receptors?
-Integral
What is the structure of a receptor’s polypeptide and what terminus to they possess?
- NH2 and COOH Termini
- Single Polypeptide Chain
Wha is the structure of a G-Protein Coupled Receptor?
Polypeptide chain is connected to X7 transmembrane spans- are 3 intracellular AND 3 extracellular connecting loops
What is the result when G-Protein Coupled Receptors are activated and what is this process called?
- Activation of G-Proteins
- G-Cycle
What are the X3 G-Protein sub-units?
Alpha, Beta and Gamma
What type of protein are G-Proteins?
-Peripheral (Outside)
What do G-Proteins called and act as when activated?
- Intermediate-G-Proteins
- Intermediate between G-Protein Coupled Receptors and Effectors
Explain what happens in the G-Cycle
Active State:
- Alpha sub-unit dissociates off from polypeptide
- GTP binds to Alpha sub-unit
- GDP dissociates off (not-needed)
Deactivation of GCPRs:
- Agonist dissociates off from receptor
- Signalling can continue because G-Protein has been already activated
- Alpha sub-units acts as an enzyme and breaks the GTP that’s is attached > GDP +Pi
- Signal now turned off
- Alpha sub unit re-joins polypeptide
- G Cycle is COMPLETE!
Are receptors used as signalling pathways?
- YES
- Bind to signalling molecules to form signalling pathway
What type of signalling molecules are Steroid Hormones?
-Hydrophobic
What type of cascade is formed by Kinase-Linked receptors once bound to hydrophilic signalling molecules-causing Phosphorylation ?
- Phosphorylation cascade
- As kinase enzymes trigger phosphorylation
How do Nucleated Receptors Signal?
- This causes dissociation of Inhibitory HSP protein
- Hydrophilic and receptor complex moves to the nucleus and form a ‘Dimer’ (two receptors joint) - and binds to HREs (Hormone Response Elements)
What does ‘Transpressed’ and ‘Transactivated’ mean in Transcription?
-Switched on= Transactivated
Switched off =Transpressed
What type of factors are Nucleated Receptors
- Transcription Factors
- Control DNA Transcription
