Week 1: Pharmacology Lecture Review Flashcards
In a KFP about a drug mechanism what information is important to include?
Chemistry
Class of drug
Drug target - receptors etc (is this a GPCR etc)
Effect at target - reversible, competitive etc
Resulting signalling effect
Physiological effect
How this presents clincally
Explain the difference between pharmacology and therapeutics?
Pharmacolofy - drug focused, understainging MOA and concentration dependent effects
Therapeutics - patient focused, the clinical application or how the drug can help the patient, views drugs as medicine used to treat disease, dose dependent effects
What is the the difference between a generic and a brand name?
Generic - name of the actual drug - best one
Brand - name of the company, name on the box
What word ending indicates a local anaesthetic?
Caine
What is the mechanism of action of adalimumab?
If a monoclonal antibody
Targets TNF alpha
What is the mechanism of aaction of atenolol?
Is a beta blocker
Targets a Beta receptor (GPCR)
Acts as a competitive antagonist - prevents normal substrate from binding.
What is the difference between a primary and secondary mechanism of drug action?
Primary - ligand activity target
Secondary - effect on physiology
What is the general mechanism of action of aspirin?
Is an NSAID
Targets COX enzymes
Contains an acetyl group that allows it to irreversibly bind to and inhibit the COX enzyme.
This decreases prostaglandin synthesis, leading to decreased blood flow and decreased vascular leakage helping to resolve inflammation.
Side effects: Anti-thrombotic so can lead to GI bleeding.
What is the structural difference between esomeprazole and omeprazole?
Omeprazole - is a racemate so 50/50 of each isomer
Esomeprazole - is the S isomer only.
What is the use of proglumide?
Targets CCK2 receptor
Acts as an antagonist
Prevents gastrin from binding to receptor
Decrease acid secretion
What is the use of misoprostol?
Is a prostaglandin analogue: agonist
Stomach - binds to prostaglandin receptors ER2/3R to reduce activity on the proton pump increase protective effects on gastric mucosa by decreasing acid secretion, increasing bicarbonate and mucus secretion.
In cervix/uterus - binds to prostaglandin receptors to increase the strength and frequency of contractions and decrease cervical tone which can induce abortions
What is the use of H2 blockers in acid secretion?
Prevent histamine binding to H2 receptors on parietal cells.
Adenylate cyclase is not activated
cAMP is not increased
Protein Kinase A is not activated
H+/K+ ATPase is not activated.
Competitive antagonists
What is the use of atropine related to acid secretion?
Binds to M3 receptors
Inhibits activation of phospholipase C
Inhibits production and cleavage of IP3
Inhibits the increase in intracellular Ca2+
Inhibits the activation of calmodulin kinase
Decrease activity of the proton pump.
What properties are included in pharmacodynamics?
Effects are concentration dependent
Affinity (dissociation constant)
Efficacy (EC50)
Selectivity
What processes are involved in pharmacokinetics?
Effects are dose-dependent
Absorption - bioavailability
Distribution - volume of distribution
Metabolism
Excretion/Elimination
This includes clearance or half-life
