CHAPTER IV

WINONA’S

PSYCHOPHARMACOLOGY

Psychopharmacology: study of effects of drugs on nervous system and

behavior

Drugs Drug effects Sites of action

 Exogenous  Changes that can  Points at which
chemical NOT be observed in an molecules of drugs
necessary for individual’s interact with
normal cellular physiological molecules located
functioning, that processes and on or in cells of the
significantly alters behavior after drug body, affecting
the functions of usage. some biochemical
certain cells of the processes of these
body when taken in cells.
relatively low doses
**exogenous; produced
outside of the body

Pharmacokinetics:
 The activity of drugs in the body over a period of time, including the
processes by which drugs are absorbed, distributed in the body, localized
in the tissues, and excreted.
 Includes the steps by which drugs are:
1) Absorbed
2) Distributed within the body
3) Metabolized
4) Excreted

ABSORPTION: routes of administration

A) Injection: [drug is dissolved or suspended in a liquid and injected through

a hypodermic needle]
i. Intravenous (IV) injections
 Injection into a vein
 Drug is absorbed and distributed immediately,
reaching the brain in a few seconds
 Disadvantages: The disadvantages of IV injections
are the increased care and skill they require in
comparison to most other forms of injection and the
fact that the entire dose reaches the bloodstream at
once. If an individual is especially sensitive to the
drug, there may be little time to administer another
drug to counteract its effects
ii. Intraperitoneal (IP) injections
 Drug is injected through abdominal wall into the
peritoneal cavity (space surrounding stomach,
intestines, liver, and other abdominal organs)
 Rapid but not as fast as IV
CHAPTER IV
WINONA’S

 Commonly used to administer drugs to small

laboratory animals
iii. Intramuscular (IM) injection
 Injection is made directly into a large muscle, such as
those found in upper arm, thigh, or buttocks
 Drug is absorbed into the bloodstream through
capillaries that supply the muscle
iv. Subcutaneous (SC) injection
 Drug is injected into space beneath the skin
B) Oral administration:
 Most common form of administering therapeutic drugs to humans
 Some chemicals cannot be administered orally because they are
destroyed by stomach or digestive enzymes or because they are
not absorbed from the digestive system into the bloodstream
C) Sublingual administration
 Placing beneath the tongue
 Drug is absorbed into bloodstream by capillaries that supply the
mucous membrane that lines the mouth
 E.g., migraine medicines
D) Inhalation
 Through lungs
 Route from lungs to brain is very short and drugs administered
this way have very rapid effects
 E.g., marijuana, nicotine, freebase cocaine, anesthetics
E) Topical administration
 Directly through skin
 Natural or artificial steroid hormones are administered this way
like nicotine
 Insufflation:
 Mucous membrane lining nasal passages also provide a
route for topical administration
 This route delivers drug to brain rapidly
 Commonly abused drugs such as cocaine and bath
salts are often sniffed so that they come into contact
with the nasal mucosa
 Sniffing or snorting is not same as inhalation; when
powdered drugs are sniffed, they enter circulation
through mucous membrane of nasal passages, not
lungs
F) Intracerebral administration
 Drug is injected into the brain or into cerebrospinal fluid of brain’s
ventricular system
 To study effects of a drug in a specific region of the brain a
researcher will inject a very small amount of drug directly into the
brain
G) Intracerebroventricular (ICV) administration
 To achieve a widespread distribution of a drug in the brain a
researcher will get past the blood-brain barrier by injecting the
drug into the cerebral ventricle, the drug is then absorbed into
the brain tissue where it can exert its effects
CHAPTER IV
WINONA’S

DISTRIBUTION: entry of drugs into the brain

 Drugs exert their effects only when they reach their sites of action
 Most sites are located on or in cells of CNS
 LIQUID SOLUBILITY :
 Ability of fat-based molecules to pass through cell
membranes
 Most important factor that determines the rate at which a
drug reaches sites of action within the brain

METABOLISM AND EXCRETION

 Liver plays an especially active role in enzymatic deactivation of drugs but
some deactivating enzymes are also found in the blood
 The brain also contains enzymes that destroy some drugs
 In some cases, enzymes transform drug molecules into other forms that
are biologically active; occasionally the transformed molecule is even
more active than the one that is administered e.g. chlordiazepoxide
(Librium) anxiety med
 Excretion primarily happens in kidneys

DRUG EFFECTIVENESS
 Drugs vary widely in effectiveness, the best way to measure the
effectiveness of a drug is to plot a:
1) Dose-response curve
 To measure a drug’s margin safety use a:
1) Therapeutic index

WHY DO DRUGS VARY IN EFFECTIVENESS

A) Sites of action
Drugs have different sites of action
B) Affinity of drug with its site of action
Affinity: readiness with which the two molecules join together
**A drug with a high affinity will produce effects at a relatively low
concentration, whereas a drug with a low affinity must be
administered in higher doses
** the most desirable drug has a high affinity that produce therapeutic
effects and low affinity for sites of action that produce toxic side
effects

EFFECTS OF REPEATED ADMINISTRATION

Tolerance: drug effects diminish when administered repeatedly

Sensitization: drug becomes more and more effective
Withdrawal symptoms :primarily opposite effects of drug itself, caused by
same mechanisms responsible for tolerance; when the person stops taking
the drug, the compensatory mechanisms make themselves felt as withdrawal
symptoms
Physical dependence: when a person has repeatedly used a drug enough to
produce withdrawal symptoms
CHAPTER IV
WINONA’S

Placebo Effects

Placebo:

SITES OF ACTION

Most drugs that affect behavior do so by affecting synaptic

transmission, these drugs are classified into:
1) Antagonists: those that block or inhibit postsynaptic effects
2) Agonists: those that facilitate postsynaptic effects

PRECURSORS: considered agonists because administering them increasing

activity of neurotransmitter system

VESICLE TRANSPORTERS: pump molecules of the neurotransmitter across

the vesicle membrane, filling the vesicles

Direct agonist: drug that mimics effects of a neurotransmitter

Direct antagonists/ Receptor blockers: drugs that bind with postsynaptic
receptors; molecules bind w/ receptors but block them from being activated;
because they occupy the receptor’s binding site, they prevent
neurotransmitter from activating receptor can have therapeutic effects
Indirect antagonist: drug that attaches to one of alternative sites and
prevents ion channel from opening
Competitive binding: direct agonists and antagonists act directly on
neurotransmitters
Noncompetitive binding: binding of a molecule with alternative sites
Indirect agonist: drug attaches to one of alternative sites and facilitates
opening of ion channel

Reuptake: process that takes back molecules of neurotransmitter into

terminal button of presynaptic cell/ they are deactivated by enzyme