Midterm 2 Part 2 Flashcards
Where are weak acids better absorbed?
stomach
Where are weak bases better absorbed?
intestine
bioassay
provides information on the pharmacological activity of new or chemically-undefined substances
pharmacodynamics
What the drug does to the body
Quantitative relationship between concentration and receptor interaction AND specific cellular response
Steeper quantal dose response curve means
lower variation in the population
Less steep, slow-rising quantal dose response curve means
higher variation in the population
Minimal effective dose, MED
Lowest dose that will produce the desired therapeutic respond
Makes up the lower part of the therapeutic window
Maximum tolerated dose (MTD)
highest dose that can be administered w/o adverse/toxic effects
Makes up the higher part of the therapeutic window
ED50
Effective dose in 50% of the concentration
Makes the lower part of the therapeutic index
TD50
toxic effect in 50% of the population at this dose
Makes up the upper part of the therapeutic index
Potency
A comparative expression of drug activity.
Does not indicate efficacy. Just because one drug is more potent, doesn’t mean it is more effective
Potency increases as EC50 decreases
What receptor is LSD an agonist for?
serotonin receptor. It is less potent than serotonin however.
Non-competitive antagonists
Bind to allosteric site rather than orthostatic site. Form a strong bond and thus slowly or does not dissociate from receptor –insurmountable because you can’t add more agonist to displace the antagonist. Emax decreases
Psychoactive drug
Drug that affects the CNS and alters behaviour including mood and cognition
Can be therapeutic or recreational
Tolerance
When repeated exposure to drugs decreases effectiveness of the drug. Lower response to a given dose of drug.
Need higher dose to get the same ‘desired’ effect
METABOLIC tolerance
body gets more efficient at elimination of the drug
cellular tolerance
target tissue has decrease sensitivity. The number of receptors is reduced or else they just become less sensitive
How are some ways the body will try to maintain homeostasis when on drugs?
If taking an agonist - body might try to reduce the receptors to reduce the response
If taking on antagonist - body might try to increase the number of receptors to increase the response
Learned tolerance
Adapt behaviour based off experience to compensate for the effects of the drug. Consciously or unconsciously you have learned how you respond to the drug.
Lowers the response
Cross tolerance
Tolerance of one drug can be transferred over to another drug within the same family. Therefore, you can exhibit tolerance for a drug that you have never taken before.
Drug sensitization
Intermittent exposure to a drug can lead to enhanced responses to subsequent exposure to the same dose.
Can last a long time and occur after a single use.
Amphetamines
Enhance the release of dopamine AND block re-uptake transporters of NE, 5-HT, and dopamine. 1
Caffeine
Is an antagonist that binds to caffeine receptors and prevents a response from occurring.
Caffeine tolerance - neurons synthesize more adenosine receptors - makes it so that more caffeine is required to block the additional receptors.
- SO when you stop drinking coffee and have many receptors - increased sensitivity to adenosine - sleepy
Nicotine
Binds and activates the nicotinic ACh receptor (Na+ flows in)
At low initial doses - acts as a stimulant
At high initial does - acts as a relaxant
Leads to release of dopamine
Rapid tolerance
Acetylcholinesterase inhibitors
Used for treatment of Alzheimers and dementia