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20 Cards in this Set

  • Front
  • Back
Pharmacokinetics
To be effective, a drug must reach its site of action
In order to do so, a drug must:
1.Enter the body
2.Enter the bloodstream
3.Be carried to the organs they act on
4.Leave the blood stream
5.Contact the molecules with which they will interact
6.For most of the drugs we will be addressing this also means they must enter the CNS
7.Also once they enter the body, drugs begin to be metabolized (broken down by enzymes and dispersed or eliminated)
Routes of Administration: Intravenous
Injection into a vein
Routes of Administration: Intraperitoneal
Injection into a peritoneal cavity
Routes of Administration: Intramuscular
Injection into a muscle
Routes of Administration: Subcutaneous
Injection beneath the skin
Routes of Administration: Oral
Administration into the mouth and swallowed
Routes of Administration: Sublingual
Placed beneath the tongue
Routes of Administration: Intrarectal
Administration into the rectum
Routes of Administration: Inhalation
Vaporous substance into the lung
Routes of Administration: Topical
Administration onto the skin
Routes of Administration: Intracerebral
Administration directly into the brain
Routes of Administration: Intracerebroventricular
Into the cerebral ventricles
Other Distribution Issues
Drugs that are lipid soluble pass the blood brain barrier much quicker that drugs which are water soluble
Drugs also often bind with tissues or proteins in the blood, this is known as depot binding
Drugs do not remain in the body indefintely
Many are broken down by enzymes
All are eventually excreted
The liver plays an especially active role in the enzymatic deactivation of drugs
Sites of Drug Action
Location of effect
On production of neurotransmitters
On storage and release of neurotransmtters
On receptors
On reuptake or destruction of neurotransmitters
(See diagram on page 109)
Antagonist
A drug that opposes or inhibits the effect of a particular neurotransmitter on the postsynaptic cell
Agonist
A drug that facilitates the effects of a particular neurotransmitter on the postsynaptic cell
Serotonin
Six major pathways from the mid brain looping around the various parts of the brain

Believed to influence a great deal of our behavior, particularly the way we process information

Regulates our behavior, moods, and thought processes

Low levels associated with aggression, suicide, impulsive overeating, and excessive sexual behavior

Although not directly responsible for these behaviors, low serotonin activity may make us more vulnerable to certain problematic behaviors
Dopamine
Implicated in such disorders as schizophrenia - it is thought that in schizophrenia dopamine circuits may be too active

In the two major dopamine pathways in the mesolimbic and mesostriatal regions of the brain dopamine seems to act as a switch that turns on various brain circuits that are then inhibited or facilitated by other neurotransmitters

Dopamine circuits merge and cross with serotonin circuits at many points and therefore influence many of the same behaviors

Dopamine is associated with exploratory, outgoing, & pleasure seeking behaviors – serotonin is associated with inhibition and constraint, Thus in a since they balance each other
Norepinephrine
Primarily stimulates two groups of receptors called alpha-andrenergic and beta-andrenergic receptors

A number of norepinephrine circuits have been identified – one major circuit begins in the hind brain, in an area that controls basic bodily functions such as respiration

Another appears to influence emergency reactions or alarm responses

Thus norepinephrine may bear some relationship to states of panic

Beta-blockers help regulate hypertension or heart rate
Gamma Aminobutyric Acid
GABA for short, reduces post synaptic activity, which in turn, inhibits a wide variety of behaviors and emotions

Its best known effect is to reduce anxiety

The GABA pathways seem to reduce levels of anger, hostility, aggression, and perhaps even positive emotional states such as eager anticipation and pleasure