Pharmacology Flashcards
How does a non-competitive inhibitor affect the dose-response curve
Shifts it to the right and downwards, reducing efficacy and potency of the drug.
What is EC50
The concentration of drug needed for half the maximal response.
What is receptor reserve
Activation of just a fraction of existing receptors can cause a maximal response.
Not present for partial agonists.
Meaning of inverse agonists
When binding to a receptor causes an opposite response, not the same as antagonist which causes no response.
What are the 2 g-proteinc coupled receptor enzymes
Phospholipase C
Adenylyl cyclase
Example of non-selective B2 agonist
Isoprenaline
Examples of transporter-targeting drugs
Diuretics, PPIs, SSRIs,
What does a first order reaction entail?
Rate of drug diffusion into tissues is directly proportional to plasma concentration.
What is a partial agonist?
An agonist where the maximal response cannot be reached despite any concentration level.
3 ways in which a receptor can become desensitised
Uncoupled - agonist unable to interact with a GPCR
Internalised - the receptor is taken into an intracellular vesicle (endocytosis)
Degraded
What is given in aspirin overdose and why?
Bicarbonat because it makes urine more alkaline, allowing for more aspirin to exist in ionized form to be excreted rather than reabsorbed.
What is the meaning of volume of distribution?
It is the volume (litres) that the drug would occupy if it was distributed through all the compartments as if they were all plasma
Volume of distribution = Total amount of drug in body /Concentration of drug in plasma
Gentamicin S.E
Nephrotoxicity, ototoxicity.
What is an augmented drug adverse effect?
When there is an extension of the clinical effect of the drug - e.g aceI causing hypotension, diuretics causing dehydration, etc.
What is a chronic adverse drug reaction?
Reaction that occurs after long term usage such as steroids causing osteoporosis, NSAIDs & nephrotoxicity etc.
