DrugEd Chp 5

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5.

What are the

approximate
yearly sales of the
pharmaceutical
industry?

Sales exceeding $189 billion per year.

Distinguish
between brand,
generic and
chemical names
for drugs.

Brand- Specifies a particular formulation and manufacturer, and the trademark belongs to that manufacturer.
Usually quite simple and as meaningful (in terms of the indicated therapeutic use) as the company can make it.
Generic- official (legal) names of drugs and are listed in the United States Pharmacopoeia (USP). Usually shorter
and simpler than the complete chemical name. Generic names are in the public domain, meaning they can't be
trademarked.
Chemical- the chemical name of a compound gives a complete chemical description of the molecule and is derived
from the rules of organic chemistry for naming any compound. Chemical names of drugs are rarely used except in a
laboratory situation where biochemists or pharmacologists are developing and testing new drugs

What drug name

is the official,
legal name that is
listed in the
United States
Pharmacopeia
(USP)?

Generic

Give a basic
outline and
several examples
of the five drug
categories.

1). Stimulant drugs- produce wakefulness and a sense of energy and well-being. The more powerful stimulants, such
as cocaine and amphetamines, can at high doses produce a manic state of excitement combined with paranoia and
hallucinations. (ex. Cocaine, amphetamines, caffeine).
2). Depressant drugs- at low doses they appear to depress inhibitory parts of the brain, leading to disinhibition or
relaxation and talkativeness that can give way to recklessness. As the dose is increased, other neural functions
become depressed, leading to slowed reaction times, uncoordinated movements, and unconsciousness. Regular use
can lead to a withdrawal syndrome characterized by restlessness, shakiness, hallucinations, and sometimes
convulsions. (Ex. alcohol, barbiturates, sedatives, sleeping pills, inhalants).
3). Opioids- a group of analgesic (pain-killing) drugs that produce a relaxed, dream-like state; moderately high
doses often induce sleep. This group is known pharmacologically as the narcotics, and it is important to distinguish
them from the "downers", or depressants. With opioids there is a clouding of consciousness without the reckless
abandon, staggering, and slurred speech produced by alcohol and other depressants. Regular use of any opioids can
lead to a withdrawal syndrome different from that of depressants and characterized by diarrhea, cramps, chills, and
profuse sweating. (Ex. Morphine, codeine, heroin, methadone).
4). Hallucinogens- produce altered perceptions, including unusual visual sensations and quite often changes in the
perception of one's own body. (Ex. Mescaline, LSD, PCP).
5). Psychotherapeutic drugs- include a variety of drugs prescribed by psychiatrists and other physicians for the
control of mental problems. The antipsychotics, such as haloperidol (Haldol), are also called neuroleptics. They can
calm psychotic patients and over time help them control hallucinations and illogical thoughts. The antidepressants,
such as fluoxetine (Prozac), help some people recover more rapidly from seriously depressed mood states. Lithium is
used to control manic episodes and to prevent mood swings in bipolar disorder.
-6). Marijuana- often thought of as a relaxant, depressive type of drug, but it doesn't share most of the features of the
drugs in that class. It is sometimes listed as a hallucinogen because high doses can produce altered perceptions, but
that is not always an appropriate classification. Can be a stimulant because the heart rate increases.
-7). Nicotine- often thought of as being a mild stimulant, but it also seems to have some of the relaxant properties of
a low dose of a depressant

Distinguish
between specific
effects of drugs
and non-specific
factors
associated with
drug actions.

Nonspecific (placebo) effects: The effects of a drug do not depend solely on chemical reactions with the body's
tissues. The influences of expectancy, experience, and setting are also important determinants of the drug's effect.
Nonspecific effects of a drug are those that derive from the user's unique background and particular perception of the
world. Include anything except the chemical activity of the drug and the direct effects of this activity. Also sometimes
called placebo effects, because they can often be produced by an inactive chemical that the user believes to be a drug.
Specific effects: Dose-response relationship- when the dose of the drug is varied and the size of the effect changes
directly with the drug dose.

What is placebo? How is

depression impacted by placebo's?

An inactive drug. Depends on what the user expects to experience. At least 1/3 of
psychologically depressed patients treated with placebos show improvement. About 80% of the
effectiveness of antidepressant drugs could be obtained from a placebo.

What is the best method of

evaluating drug effects? Why?

Double blind- neither the subject nor the administrator should know.

Define threshold dose, effective

dose, margin of safety, and
therapeutic index.

Threshold dose- at some low dose, an effect on the response system is being monitored and
observed.
Effective dose- there are more molecular interactions and a greater effect on the response
system. At the point where the system shows maximal response, further additions of the drug
have no effect.
Margin of safety- dosage difference between an acceptable level of effectiveness and the lowest
toxic dose.
Therapeutic index- ratio of LD50 to ED50. (lethal dose/effective dose for 50% ). Since the
lethal dose should always be greater than the effective dose, the TI should always be greater
than 1.

9.

Define "side effects".

Unintended effects that accompany therapeutic effects; are not relevant to the treatment.

10.

Define potency!

Measured by the amount of drug required to produce an effect.

11.

Define cumulative effects of drugs.

If doses are taken too close together, the maximum blood level will increase with each dose
and can result in cumulative effects.

Describe the relationship between

lipid solubility and psychoactive
drug absorption in the brain

The extent to which a chemical can be dissolved in oils and fats is called its lipid solubility.
Most psychoactive drugs dissolve to some extent in either water or lipids, and some of the drug
would be found in each. Important in how some drugs get to the brain.

What are the primary drug delivery

methods?

1). Oral administration - Most common method. Simplest way. Absorption from
gastrointestinal tract is most complicated way to enter the bloodstream.
2). Injections- IV injection - Hypodermic syringe.
Subcutaneous intramuscular injections
3). Inhalation
4). Absorption- Topical
Rectal/Vaginal
Mucous

What are the advantages of IV

injection as a route of
administration?

Much more rapid than than oral administration or with other means of injection. Irritating
material can be injected this way because blood vessel walls are relatively insensitive. Can
deliver very high concentrations of drugs intravenously(both advantage and danger).

What are the disadvantages of IV

injection as a route of
administration?

The vein wall loses some of its strength and elasticity in the area around the injection site.
Many injections into a small segment of a vein, the wall of that vein eventually collapses, and
blood no longer moves through it, necessitating the use of another injection site. Introducing
infections.

Compare the absorption speed

among intramuscular injections to
the thigh, buttocks, and deltoid
muscle.

Deltoid most rapid, then thigh, buttocks is slowest. Depends on the medicine and your body
and the condition.

What are the limitations of

inhalation as a route of
administration?

Must not be irritating to mucous and lungs. Control of dose is more difficult. No depot (holding
spot) of drug in the body (drug must be given as long as effect is desired when drug admin is
stopped the effect rapidly decreases.)

What body system is the main

mode of transportation for drugs
from their place of entry to the site
of action?

Bloodstream (blood proteins?)

What is the major constituent of

the blood-brain barrier? What is
the most important implication?

Capillaries in the brain(capillary wall?) 85% of capillary cells covered with Glial cells(?).
Active transport necessary to move chemicals in and out of brain. Lipid soluble- the faster a
drug has an effect, the more reinforcing it is, then the more likely it will be addictive.

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What is the effect of cerebral

trauma on the blood brain
barrier

Can disrupt the barrier and permit agents to enter that normally would be excluded. Concussions and
cerebral infections frequently cause enough trauma to impair effectiveness of this screen.

How do psychoactive drugs

alter the availability of a
neurotransmitter?

Psychoactive drugs can alter the availability of a neurotransmitter by increasing or decreasing the
transmitter chemical's rate of synthesis, metabolism, release from storage vesicles, or reuptake into
the releasing neuron. Or the drug might act directly on the receptor, either to activate it or prevent the
neurotransmitter chemical from releasing it

Before a drug can cease to

have an effect, one of two
things must happen to it?
What are they?

1). Excreted unchaged from the body- urine.

2). Chemically changed so that it no longer has the same effect on the body- digestion, liver enzymes.

What is the main organ of

drug metabolism?

Liver

What is an "active" metabolite

and a "pro drug"?

"active" metabolite: Metabolites that have drug actions of their own. Produce effects similar to those
of the original(parent) drug and prolong the effect considerably.
prodrugs: drugs that are inactive until altered by liver enzymes

25.

Distinguish between
behavioral tolerance, drug
disposition tolerance and
pharmacodynamic tolerance.

Behavioral tolerance - With experience the impairment may be reduced; tolerance caused by learned
adaptation to the drug.
Drug disposition tolerance - tolerance caused by more rapid elimination of the drug. Sometimes use
of a drug increases the drug's rate of metabolism or excretion
Pharmacodynamic tolerance - tolerance caused by altered nervous system sensitivity. Leads to
reduced effectiveness of drug and also to withdrawal reactions. After several days the compensating
homeostatic mechanisms return to a normal state, the withdrawl symptoms cease and individual is
no longer tolerant to the drug