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A compulsive pattern of drug seeking and use.
The specific molecular changes produced when a drug binds to its targets site or receptor is called ________.
What does the term drug effect refer to?
The physiological, psychological and behavioral alterations induced by the drug
Therapeutic drug effects are the _______ effects of a drug, while side effects are the ________ effects of the same drug.
What does the term pharmacokinetics refer to?
The factors that contribute to the bioavailability of a drug within the body.
What term is used to describe the physiological and biochemical interactions of drugs with their target tissues?
What are the five key components of pharmacokinectics?
- 1. Drug administration/route
- 2. Absorption and distribution
- 3. Binding to the drug target (and storage depots)
- 4. Inactivation
- 5. Excretion
What does it mean to say that a drug undergoes "first-pass metabolism" and with what form of administration is this most common?
It means that the drug is processed by the liver before being distributed throughout the body, and this most typically occurs when a drug is taken orally
Give the eight different routes of drug administration.
- 1. Oral
- 2. Topical
- 3. Transdermal
- 4. Intramuscular injection
- 5. Intravenous injection
- 6. Subcutaneous injection
- 7. Inhalation
- 8. Epidural
What type of drugs are able to move into cells through passive diffusion along a concentration gradiant?
Drugs that ionize will dissolve in water, but they will be unable to _______.
Cross membranes by passive transport
At what point is a drug 50% ionized?
When the pH of the solution is equal to the pKa of the drug
When the pKa of a drug is greater than the pH of the solution the drug is likely to be ___________ and this allows for increased ______________.
Non - ionized; absorption
When the pKa of a drug is less than the pH of the solution the drug is likely to be ___________ and this allows for increased ______________.
Ionized; binding/drug action
What are four additional factors that affect drug absorption?
- Surface area available for absorption
- The blood-brain barrier
What type of molecules are blocked most effectively by the blood-brain barrier?
Cerebral spinal fluid is the blood of the brain, it is produced in the _______________.
Choroid plexus of the lateral ventricle
What are two different names for the cell type that makes the blood brain barrier work.
Glial cells, astrocytes (same type of cell)
In what two brain areas is the blood-brain barrier absent? What do these areas do?
Area postrema: triggers vomiting when toxic substances are detected
Median eminence of the hypothalamus: allows passage of neurohormones from the hypothalamus to the pituitary gland
Most drugs follow __________ and go through _ half-lives before reaching minimal concentrations.
1st order kinetics; 6
What drug is one of the few to follow zero order kinetics?
Cocaine has a particularily _____ half-life, while SSRIs like prozac have particularily ____ half-lives.
Give the three different types of biotransformations that drugs can go through.
- Enzyme catalyzed chemical changes
- Non-synthetic modifications
- Synthetic modifications
When a drug is used chronically the body may produce additional enzymes to break it down faster, this is called ___________
Monoamine oxidase inhibitors prevent monoamine oxidase from breaking down serotonin at the synapse, this is an example of ____________.
What happens when two drugs share metabolic systems (ie alcohol and barbituates)? What is this called?
There are only so many enzymes to break them down and blood concentrations remain higher for longer; drug competition
What is another factor that influences drug metabolism?
Receptor agonists bind to receptors with ___ affinity and _______ a response; chronic use of agonists leads to _____ regulation of the associated receptors.
High; initiate; down-regulation
Receptor antagonists bind to receptors with _____ affinity and _______ a response; chronic use of antagonists leads to ______ regulation of the associated receptors.
High; inhibit; up-regulation
Receptor ________ have high efficacy, while receptor _________ have low efficacy
What does ED50 stand for? What does TD50 stand for?
- Effective dose (50% of the maximum response)
- Toxic dose (50% of an unwanted side effect)
A competitive antagonist can displace a receptor agonist reducing the drug _______; a non-competitive antagonist reduces the action of the agonist reducing the drug ______
Give the 3 types of drug interactions discussed in class.
- Physiological antagonism
- Additive effects
A diminished response to drug administration with repeated exposure
Give an example of cross-tolerance.
When one becomes tolerant to one drug through use of a different drug that acts on the same system (alcohol and benzodiazapienes)
What are three forms of tolerance?
- Drug disposition (increased metabolism)
- Pharmacodyname (up/down regulation of receptors)
- Behavioral (contextual dependence)
"Reverse tolerance" is referred to as __________ and occurs when pre-exposure to a drug causes an enahnced response upon readminsitration.