Drugs and Addiction Flashcards
Presynaptic neuron alterations
NT Production- inhibit enzymes, transport of raw materials
NT Release- can block APs from ever arriving, or autoreceptors can provide false feedback
NT Clearance- reuptake inhibitors, or block enzymes
Postsynaptic neuron alterations
NT Receptors- antagonists block receptors from being activated, agonists mimick NTs
Cellular processes- activate second messengers, genes, protein production
Affinity (binding affinity)
How likely the ligand is to bind with a receptor
How long the ligand stays bound (can it actually stay long enough to cause an effect?)
Efficacy (intrinsic activity)
How likely the ligand is to have an effect
Antagonist= very low levels of efficacy Agonist= high efficacy
Dose-Response Curve
Relationship between dosage and observed effect (helped to determine useful and unsafe dose ranges)
Therapeutic effect- balance between drug effectiveness and toxicity (want least negative side effects while still getting desired effect)
Bioavailability
Free to act on target issue
Not bound or broken down prior to having its effect
Biotransformation
Breakdown of drugs into active metabolites, which can have beneficial or harmful effects
Blood-brain barrier
Ligand must be able to pass BBB to have an effect
Pharmacokinetics
Factors that affect the movement of a drug into, through, and out of the body
Tolerance
Building up resistance, and thus only getting a smaller effect with the same dose of a given drug
Metabolic and functional tolerance
Metabolic tolerance
Body clears the drug more quickly, so it has less time to take effect
Functional tolerance
Receptors respond less to the drug
- down-regulation: decreased # of receptors in response to agonist
- up-regulation: increased # of receptors in response to antagonist
Sensitization
Larger effect with the same dose
Particularly common with side effects
Cross-tolerance
Tolerance to a particular drug generalizes to other drugs of the same chemical class
Dependence and Addiction Models
Moral model- lack of self control or character weakness, it’s all the users fault
Disease model- pathological process, largely uncontrollable
Physical dependence model- withdrawal avoidance
Positive reward model- positively reinforcing effects, dopamine/reward circuit