Term
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Definition
| a substance that alters the physiology of the body but is not a food or toxin. Definition depends on intention of user. Must have a site of action to act upon. |
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Term
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Definition
| Chemical, Generic, and Trade Names |
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Term
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Definition
| What a drug does to the body |
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Term
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Definition
| How a drug acts to produce an effect |
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Term
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Definition
| tissue element (usually a protein) with which a drug acts to produce a characteristic biological effect |
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Term
| Ehrlich's receptor theory of drug addiction |
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Definition
| A drug must interact by combining or interacting with a receptor at a certain site of action to produce an initial series of events to produce a biological effect. This forces the drug to attract to the receptor. |
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Term
| Drug-receptor Interactions |
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Definition
| Ionic bonding, covalent bonding, Van der Waals forces, hydrogen bonding |
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Term
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Definition
| charged. Forming ionic bonds. |
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Term
| Key Analogy of Drugs and Receptors |
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Definition
| Ionic bonds are the major knotches on a key allowing it to enter a lock (receptor), hydrogen bonds are the smaller knotches on a key which allow the key to partially turn, and Van der Waals forces are the smaller knotches on a key which allow it to completely turn and open the lock. |
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Term
| What defines the behavioral or physiological effects of a drug? |
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Definition
| The concentration of a drug in the body. Dependent on body weight, sex, age, route of administration, species, prior experience. |
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Term
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Definition
| Amount of drug given to an individual to produce a certain biological effect |
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Definition
| Shows the effects of a drug over a long time period |
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Definition
| The maximal binding to a receptor. 100% of receptors are occupied. AKA Bitch you fucked up. |
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Term
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Definition
| The measure of the effectiveness (affinity) of a drug at a particular receptor. The LOWER the Kd the less drug needed to achieve maximal effect. (ex. Morphine has a lower Kd than Aspirin) |
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Term
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Definition
| Effective Dose in 50% of individuals tested. The lower the ED50, the lower the Kd, meaning the drug is more potent. |
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Term
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Definition
| The amount of drug needed to achieve a certain effect of a given intensity. Lower the Kd and ED50 the higher the potency. Route of administration will affect the potency. |
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Term
| Best way to analyze effect of drug |
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Definition
| Over a wide range of doses, producing a full dose-response curve. |
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Term
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Definition
| Lethal Dose 50. The dose that causes lethal effects in 50% of the population given to. |
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Term
| Therapeutic ratio or index |
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Definition
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Definition
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Term
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Definition
| elicits a biological response upon binding but the magnitude of response (efficacy) is reduced |
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Term
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Definition
| The efficacy of a drug refers to the maximum biological response a drug can elicit while the affinity of the drug refers to the potency (how much of a drug is required to elicit the drug's maximal biological effect). The two are independent. |
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Term
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Definition
| Drugs that bind to a receptor and induce a biological response |
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Term
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Definition
| Drugs that interact with a receptor but do not induce a biological response |
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Term
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Definition
Binds reversibly to a receptor site that a drug would bind to. Can be displaced by excessive agonist. (Can be kicked off)
Causes a shift to the right in the dose-response curve. Results in a reduction in the number of agonists binding as well. |
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Term
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Definition
Concentration of a drug that results in 50% reduction in radioligand binding. AKA the dose at which 50% of receptors are blocked by antagonists.
Lower Ki's correspond to MORE POTENT antagonists. Higher Ki's = less potent antagonists. |
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Term
| Non-competitive Antagonists |
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Definition
Antagonists that bind to an agonist's or active drug's receptor site and cannot be kicked off despite excessive agonists being presented.
Decreases the maximal response of a drug. Modest shift to the right on the DRC. |
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Term
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Definition
| A drug that binds with full efficacy to a receptor site but elicits the opposite biological response that a traditional full agonist would. Often mistaken for an antagonist because they inhibit the effects of an agonist but they are different mechanisms. |
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Term
| Quantal Dose-Response functions |
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Definition
| Show information regarding the margin of safety. Difference between desired drug effects and toxic effects. |
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Term
| Time-Response Curve Phases |
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Definition
| Time for onset of action, time for peak effect, duration of action. |
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Term
| 4 Processes of Pharmacokinetics |
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Definition
| Absorption, Distribution, Metabolism/Inactivation, Excretion |
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Term
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Definition
A part of absorption. How a drug is transferred from one side of the biological barrier to the other without changing form.
Passive Diffusion, Facilitated Diffusion, Active Transport |
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Term
| What method of administration does not involve absortion? |
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Definition
| Intravenous injection because the drug is placed directly into the blood stream. |
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Term
| What causes a drug to pass through barriers more rapidly? |
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Definition
| Higher blood flow, smaller drug molecules, fat solubility for BBB as well as ionization state or presence of transporter proteins. |
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Term
| How do water-soluble drugs enter the brain? |
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Definition
| Must be facilitated with a transporter protein |
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Term
| How to tell best way to intake a certain drug? |
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Definition
Each route of administration has a different pH and drugs will interact differently. Different routes have different onset times as well.
Drug must be non-ionized to be absorbed. |
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Term
| What types of drugs are absorbed in the stomach? |
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Definition
| Drugs which are acids are absorbed here because the stomach is an acidic environment meaning acids are non-ionized here so they can be absorbed. |
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Term
| What kind of drugs are absorbed in the intestines? |
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Definition
| Drugs which are basic. Same deal as the stomach except basic instead of acidic. |
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Term
| 3 Major Processes of Drug Termination |
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Definition
| Excretion, biotransformation, and tissue redistribution. These processes determine the duration of action for a drug. |
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Term
| Methods of Drug Excretion |
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Definition
| Sweat, saliva, breath, urine, tears, nasal excretion, milk, and feces. |
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Term
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Definition
| Occurs through detoxification or drug metabolism. Often (but not always) the metabolized drug is inactive and less toxic. |
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Term
| General ways a drug can be modified by enzymes |
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Definition
| Synthetic and non-synthetic reactions |
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Term
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Definition
| Conjugation (pairing of drug with another molecule) usually inactivates drug. |
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Term
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Definition
| Oxidation, reduction or hydrolysis. Products not always inactive, may be more toxic. Often conjugated after non-synthetic reactions rather than directly excreted. |
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Term
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Definition
| Located on the smooth endoplasmic reticulum |
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Term
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Definition
| Enzymes which catalyze reaction with drugs. Major one is CYP-3A4 which is blocked by grapefruit juice. CYP-3A4 catalyzes ~50% of drug biotransformations |
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Term
| What effects CYP activity? |
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Definition
| Tolerance and sensitization. (and grapefruit juice) |
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Term
| Rate of elimination depends upon |
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Definition
| first-order kinetics. Depends upon the concentration of a drug in the blood at any given time. |
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Term
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Definition
| Independent of drug concentration in the blood |
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Term
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Definition
| Depends on concentration of drug in the blood. Uses half life. |
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Term
| Disease (addiction) process |
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Definition
| Preoccupation/anticipation -> binge/intoxication -> withdrawal/negative effect |
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Term
| Validation of an animal model of addiction |
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Definition
| Construct validity, predictive validity, face validity, reliability |
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Term
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Definition
| Drugs which are PR's will increase the probability of operant behavior when the drug is presented/available |
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Term
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Definition
| Drugs which are NR's will increase the probability of operant behavior when the drug is removed |
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Term
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Definition
| high face validity, high predictive validity for abuse potential, very reliable patterns. LOW predicitive validity for dopamine receptor antagonists. |
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Term
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Definition
| Point at which the subject will stop responding to a "progressive ratio schedule". Higher the break point = more "addicted" |
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Term
| Intracranial Self-Stimulation |
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Definition
| Subjects may press a lever or button to stimulate certain areas of the brain |
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Term
| Non-operant Drug Self Administration |
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Definition
| Example: two sipper tubes available 24/7 one with water and one with a drug solution. Does not require an animal response to receive drug. |
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Term
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Definition
| >5 drinks in 2 hours for a male or >4 drinks in 2 hours for a female |
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Term
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Definition
| May be biased or unbiased. Best to perform experiments unbiasedly. Take a drug a lot at one place tolerance increases, go to new place and take same amount could overdose. |
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Term
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Definition
| Experiment with mice and cocaine. Must run to the end of a runway and cross a line to get cocaine. Erratic behavior soon develops in animals getting cocaine but those that get heroine instead always run straight to finish line. Good predictive validity, decent face validity. |
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Term
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Definition
Extinction/Reinstatement models
Abstinence Models
Conditioned Withdrawal models |
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Term
| Models of Transition to Addiction |
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Definition
Long-access self-administration
Self-administration in dependent animals |
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Term
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Definition
The study of blood flow or circulation.
Two methods of hemodynamics used:
-Radiotracers in blood
-Nuclear magnetic resonance of chemicals in blood |
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Term
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Definition
PET scan (only technique to measure direct level of proteins, detects high energy gamma rays)
SPECT (less expensive than PET, lower resolution and spatial recognition) |
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Term
| Magnetic Resonance Methods |
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Definition
MRI (measures radio signals, very detailed images of the brain, no functional images)
fMRI (MRI but shows functions of the brain as well) |
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Term
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Definition
| lessening of a drug effect from repeated administration of a drug. Downward or right shift in DRC |
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Term
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Definition
| May occur after first use |
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Term
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Definition
| Tolerance to one drug creates tolerance to drugs of same class |
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Term
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Definition
Pharmacokinetic/metabolic tolerance: increase in rate or ability to metabolize drug
Behavioral Tolerance: ex. going high or drunk to work.
Pharmacodynamic/physiological/cellular tolerance: homeostasis trigger, feedback loops. Agonists reduce receptor activation (downregulation), antagonists increase receptor activation (upregulation) |
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Term
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Definition
| Means physical dependence. Readministration of drug stops symptoms. |
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Term
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Definition
| Experiment: mice receive morphine injections, one group on hot plate for 3 days, the other group in home cage for 3 days. On 4th day first group exhibits tolerance to morphine, second group has no tolerance when placed on hot plate. |
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Term
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Definition
| heightening of a drug effect over time. Upward or left shift in DRC, tends to increase over time. |
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Term
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Definition
Pharmacokinetic/metabolic: decrease in rate or ability to metabolize drug
Pharmacodynamic/physiological/cellular sensitization: elevate drug effect due to changes in body. Agonist increases receptor activation (upregulation), antagonist decreases receptor activation (downregulation) |
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Term
| Costs associated with drug abuse/addiction |
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Definition
Illicit drugs $161 billion/year
Alcohol $180 billion/year
Tobacco $155 billion/year |
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Term
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Definition
Substance abuse and dependence replaced with "addictions and related disorders" which is broken down by drug type and has gambling in it.
"drug craving" added to criteria, while "problems with law enforcement" is taken out
"cannabis withdrawal" added |
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Term
| Comorbid pyschiatric disorders |
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Definition
| ~20-35% of individuals with drug dependence exhibit the criterion for another major psychological disorder |
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Term
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Definition
| Developmental factors (age first exposed), genetic factors |
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Term
| Majors Views of Addiction |
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Definition
| Dependence, Psychiatric, Psychodynamic, Social Psychological/Self-regulation, Neuroadaptational |
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Term
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Definition
| observed by drug withdrawal. Cons include addiction which does not have physical cues. |
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Term
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Definition
| addiction has both aspects of impulse control disorders and compulsive disorders. Transition from positive to negative reinforcement. |
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Term
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Definition
| individuals take drugs to self-medicate and cope with painful or threatening emotions |
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Term
| Social Psychological/Self-regulation View |
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Definition
| Addiction a result of failure to self-regulate |
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Term
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Definition
| Sensitization, Opponent Process, Motivational (allostatic) |
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Term
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Definition
| Process by which the body rids itself of drugs. Sometimes accompanied by fatal withdrawal symptoms. 1st step of recovery |
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Term
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Definition
| Cognitive-Behavioral Therapy (CBT), Contingency Management Therapy, Motivational Enhancement Therapy (MET), 12-Step Facilitation Therapy, Behavioral Couples and Multidimensional Family Therapy |
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Term
| Pharmacological Treatments |
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Definition
| Substitution or Replacement Therapy, Partial Agonist Therapy, Antagonist Therapy, Aversion Therapy, Vaccine Therapy |
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