Pharmacology

Lec. 2
 Classification
• Each drug can be categorized under a broad
subcategory/ies called classification
Example: aspirin can relieve pain (analgesic)
And reduce fever (antipyretic)
Other Classification:
Adrenergic, Antibiotics, Diuretics, Emetics
Hypnotics and ect…
General information associated with each drugs
Therapeutic uses, most common side effects,
precautions, contraindications, interaction, drug
names, dosages and nursing management..
Identifying Names
1. Generic Name
- Common or general name assigned to the drug
differentiated from trade name by initial lowercase letter;
never capitalized.
Ex.
 Prototype Drugs
 Individual drugs that represent
groups of drugs are called Prototypes
 May be the first drugs of this group to
be developed (e.g., penicillin for
antibiotics, morphine for opioid
analgesics)
2. Trade name
- the name which the pharmaceutical
company identifies it’s product; copyrighted
and used exclusively by that company; can be
distinguished from generic name by
Capitalized first letter and often shown on
labels and references with the symbol after
the name (for registered trademark)
3. Chemical name…The exact molecular
formula of the drug; usually a long, very
difficult name to pronounce and of little
concern to the health care worker.
4. Official name…name of the drug
as it appears in the official reference,
the USP/NF; generally the same as
the generic name
 Legal Accessibility of the Drug
• OTC ..over the counter, no purchasing
restrictions
• Legend drugs ..prescription drug; determined
unsafe for OTC purchase because of possible
side effects if taken indiscriminately; includes
birth control pills, antibiotics, cardiac drugs,
hormones etc..indicated in the Physician’s desk
Reference by the symbol to the far right of the
trade name
• Controlled substance..drug controlled by
prescription requirement because of the danger
of addiction or abuse..indicated by schedule of
numbers C-I to C-V.
 Categories of Controlled
Substances
 Schedule I—not approved for medical use
and have high abuse potentials; LSD,
heroin, peyote, ecstasy (3,4
methyenedioxy-methamphetamine)
 Schedule II—used medically. High abuse
potential (methadone, meperidine,
cocaine, pentobarbital, Tylox)
 Schedule III-less potential for abuse
than I and II but may lead to
psychological or physical dependence
(Vicodin, Tylenol with codeine)
 Schedule IV-drugs have some
potential for abuse (Valium, Dalmane,
Klonopin)
 Schedule V-contain moderate
amounts of controlled substances. An
example is Lomotil (atropine and
diphenoxylate)
Pregnancy Categories
 Cat. A-studies in pregnant women
failed to show risk to the fetus
 Cat. B- animal studies have failed to
show a risk to the fetus but there are
no adequate studies in women
 Cat. C-animal studies have shown an
adverse effect on the fetus, no
adequate human studies, benefits
may outweigh risks
 Cat. D-positive evidence of human
fetal risk
 Cat. X-animal or human studies have
shown fetal abnormalities or toxicity
Drug Actions
Indications –a list of medical conditions or diseases for which the
drug is meant to be used. Ex. Diphenhydramine HCL (Benadryl)
indicated fro allergic rhinitis, mild allergic skin reactions, motion
sickness and mild cases of parkinsonism.
Actions – A description of the cellular changes that occur as a result
of the drug. Ex. Benadryl appears to compete with histamine for cell
receptor sites on effector cells.
Contraindication- A lists of conditions for which the drug should not
be given. Ex. Benadryl should not be given on pregnant and lactating
mothers
Cautions- a list of conditions or types of patients that warrant closer
observation for the specified side effects when given the drug.
Ex. Benadryl have atropine like effect and must be used cautiously
with patient with bronchial asthma or hypertension or with older
adults
Side effects and adverse reactions- a list of possible
unpleasant or dangerous secondary effects, other than
desired effect. Ex Benadryl side effects includes dizziness,
sedation, disturbed coordination, epigastric distress,
anorexia and thickening of bronchial secretions
3 side effects associated with antibiotics
 Ototoxicity – causes damage to 8th Cranial nerve which
results in impaired hearing and ringing in the ears
(tinnitus). Damage maybe reversible or permanent.
 Nephrotoxicity – damage to the kidneys, resulting to
impaired kidney function, decreased output and renal
failure.
 Photosensitivity – increased reaction to sunlight with
the danger of intense sunburn
Interactions – A lists of drugs or foods that may alter the
effect of the drug and usually should not be given during
the same course of therapy. Ex. MAO inhibitors intensify
effect of Benadryl causing serious BP changes and death
when taken with other drugs and some food.
SOURCES OF DRUGS
• PLANTS
• MINERALS
• ANIMALS
• SYNTHETIC
Effects of drugs
1.Systemic – reaches widespread area
of the body
2.Local – is limited to area of the body
where it administered
PHARMACOKINETICS
The LADME scheme
LADME describes the pharmacokinetic processes
which follow a given dosage regimen.
•L = Liberation, the release of the drug from it's dosage
form.
•A = Absorption, the movement of drug from the site of
administration to the blood circulation.
•D = Distribution, the process by which drug diffuses
or is transferred from intravascular space to
extravascular space (body tissues).
•M = Metabolism, the chemical conversion or
transformation of drugs into compounds which are
easier to eliminate.
•E = Excretion, the elimination of unchanged drug or
metabolite from the body via renal, biliary, or pulmonary
processes
Liberation is the first step in the process by
which medication enters the body and
liberates the active ingredient that has
been administered. The
pharmaceutical drug must separate from the
vehicle or the excipient that it was mixed with
during manufacture.
Absorption
 -process that occurs from the time a
drug enters the body to the time it
enters the bloodstream to be circulated
 Factors affecting absorption include:
dosage form, route of administration,
blood flow to the site of administration,
gastrointestinal function, presence of
food or other drugs
 For many medications, food in the
stomach slows absorption
 BIOAVAILABILITY
 Is the portion of a dose that reaches
the systemic circulation and is
available to act on body cells
 IV administration is 100% bioavailable
 Subcutaneous administrations has
more rapid absorption than does the
oral route
 Mucous membranes allow for rapid
and direct absorption into the
bloodstream
HALF LIFE
Half-life refers to the measurement of the
time it takes the body to break down and
excrete one half of the drug.
 This is an important factor in the creation

of drugs because it tells the

manufacturer how long it takes the body
to rid itself of the drug.
DISTRIBUTION
 Involves the transport of drug
molecules within the body
 After the drug is absorbed into the
bloodstream, it is carried by the
blood or tissue fluids to its sites of
pharmacologic action, metabolism
and excretion
 Protein binding is an important
factor in drug distribution
 Drug distribution into the CNS is limited because
of the blood-brain barrier
 Blood-brain barrier is composed of capillaries
with tight walls which limits movement of drug
molecules into brain tissue
 Only drugs that are lipid soluble or have a
transport system can cross the blood-brain
barrier and reach therapeutic concentrations in
brain tissue
 Drug distribution during pregnancy
and lactation is unique as most
drugs cross the placenta or in the
case of lactation, pass into breast
milk
Protein binding
 Most drugs form a compound with plasma
proteins, mainly albumin, which act as
carriers
 Only the free or unbound portion of a
drug acts on body cells
 As unbound drug acts on cells, the
decrease in plasma drug level causes
some of the bound drug to be released
 Protein binding allows a part of a drug
dose to be stored and released as
needed
METABOLISM
 Method by which drugs are
inactivated or
biotransformed by the
body
 Some drugs yield
metabolites that are also
active and exert effects on
the body until they are
excreted (normeperidine)
 Most drugs are lipid
soluble which aids their
passage across the cell
membrane
 Most drugs are metabolized by the
cytochrome P450 enzymes in the
liver
 Liver contains complex system of
enzymes, three of which are key in
the metabolism of
medications/drugs
Cytochrome p450
 CYP enzymes catalyze the chemical
reactions which ultimately metabolize the
medications
 With chronic administration (greater than
1-3 weeks), some drugs stimulate
hepatocytes to produce larger amounts of
drug metabolizing enzymes (inducers).
Enzyme induction accelerates drug
metabolism. Result is that larger doses of
the drug may be need for therapeutic
effects.
 Enzyme inhibition may occur with
concurrent administration of two or more
drugs that compete for the same
metabolizing enzymes (e.g., Dilantin,
EES(erythromycin ethyl succinate),
Tagamet)
 Oral meds are generally absorbed by the
GI tract and carried to the liver. Drug
may undergo extensive metabolism
leaving little for systemic use. This is
called the first pass effect.
The first pass effect (also known
as first-pass metabolism or presystemic
metabolism) is a phenomenon of drug
metabolism whereby the concentration of
a drug, specifically when administered
orally, is greatly reduced before it
reaches the systemic circulation.
Serum Drug Levels
 Lab measurement of the amount of a
drug in the blood at a particular time
 Minimum effective concentration
(MEC)-must be present before a drug
exerts its pharmacologic action on body
cells
 Duration of action-time during which
serum drug levels are at or above the
MEC (may measure serum drug levels
when the drugs have a low therapeutic
index)
EXCRETION
 Refers to the
elimination of a
drug from the
body
 Most are excreted
by the kidneys
although some are
excreted in the
bile then the
feces
 Excretion usually is by kidneys.
Need to be water soluble for this to
occur. Thus, one function of
metabolism is to convert fat soluble
medications to water soluble ones.
 Hepatic drug metabolism or
clearance is a major mechanism for
terminating drug action and
eliminating drug molecules from the
body
PHARMACODYNAMICS - the response of
the body to the drug. It refers to the relationship
between drug concentration at the site of action
and any resulting effects namely, the intensity and
time course of the effect and adverse effects.
Pharmacodynamics--Receptors
 Involves drug actions on target cells
and the resulting alterations in cellular
biochemical reactions
 Most drugs chemically bind with
receptors at the cellular level
 Drug-receptor complex initiates
physiochemical reactions that
stimulate or inhibit cellular functions
 Receptors vary in type, location,
number and functional capacity
 When drug molecules chemically
bind with cell receptors,
pharmacologic effects result from
agonism or antagonism
 Agonists-are drugs that produce effects similar
to those produced by naturally occurring
hormones, neurotransmitters and others.
Agonists may accelerate or slow normal
cellular processes depending on the type of
receptor activated. Examples of Opioid
agonists: Morphine, Hydrocodone (pain relief
/euphoria)
 Antagonists—drugs that inhibit cell function by
occupying receptor sites.
 Not all drugs act on receptors. Examples
include: antacids, osmotic diuretics, chelators
example of Opioid receptors, examples of
Antagonists are Naloxone (Narcan),
Naltrexone and Nalmefene.
An antidote is a drug,
chelating substance, or
a chemical that
counteracts
(neutralizes) the effects
of another drug or a
poison.
Drug Interactions
Synergism – the action of 2 drugs working together in which
one helps the other simultaneously for an effect that neither
could produce alone. Drugs that work together are
synergistic.
Ex. Use of two opioids like morphine and oxycodone may be
more effective than just one because both opioids have a
slightly different action on opioid receptors
Desirable synergism- giving small amounts can relieve pain
safely ex. Promethazine (phenergan) and meperidine
(demerol). Large amounts could be addictive.
Undesirable synergism- sedatives and barbiturates given in
combination can depress CNS to dangerous levels depending
on the strength of each
Potentiation- the action of 2 drugs in which one prolongs or multiplies
the effect of the other.
EX, many macrolides (erythromycin, troleandomycin), which are
antibiotics, potentiate the effects of ergot derivatives such as
ergotamine which is a vasoconstrictor agent. The explanation of this
potentiation responsible of serious adverse effects is that macrolides
inhibit the inactivation of ergotamine which accumulates in the body
at toxic levels
Desirable potentiation – to build up a high level of some forms of
penicillin (antibiotic) in the blood, the drug probenecid (benemid)
antigout given simultaneously. Benemid potentiates the effect of
penicillin by slowing the excretion rate of the antibiotic
Undesirable potentiation – toxic effect may result if cimetidine
(tagamet/gastric antisecretory) is given simultaneously with
tofranil(antidepressant). Tagamet potentiates the level of
antidepressant concentration in the blood.
Variables that affect drug actions
 Dosage
 Route
 Drug-diet interactions. Food may slow
absorption or foods may actually interact
with certain medications (tyramine and
MAO inhibitors; tetracycline and milk
products; ingestion when taking certain
antihypertensive medications
 Drug-drug interations-additive
effects such as seen with sedatives
and ethanol. Synergism as seen
with acetaminophen and codeine.
 Antidote—drug can be given to
antagonize the toxic effects of
another drug
Variables that affect drug actions
 Age
 Pregnancy
 Body weight
 Gender-hormonal
effects
 Pathologic conditions
 Placebo response
DOSAGE – amount of drug given for a particular therapeutic or
desired effect.
1. Minimum dose- smallest amount of drug that produce therapeutic
effect
2. Maximum dose – largest amount of drugs that will produce desired
effect without producing symptoms of toxicity
3. Loading dose – initial high dose (Max. dose) use to quickly elevate th
level of drug in the blood followed by a series of low maintenance
doses.
4. Maintenance dose- dose required to keep the blood level at a steady
state in order to maintain the desired effect
5. Toxic dose- amount that will produce harmful side effects or
symptoms of poisoning
6. Lethal dose- dose that causes death
7. Therapeutic dose- customarily given (ave. adult dose based on body
weight of 150lbs; adjusted according to variations from the norm
ROUTE
2 Category
1. GI routes
 Oral (PO)
 Nasogastric (NG)
 Rectal (R)
2. Parenteral
 Sublingual( SL) or buccal
 Injection routes
 Intravenous (IV)
 Intramuscular (IM)
 Subcutaneous (subQ)
 Intradermal (ID)
 Intracardiac, intraspinal, intracapular
 Topical (T)
 Dermal (D)
 Mucosal
 Inhalation
Oral route –easiest
IV route
– fastest administered by IV push or bolus
(Concentrated drug solution)or diluted infused slowly by
IVdrip
-administered by physician, RN or paramedic
-best route for emergency treatment
Parenteral routes- are choice if NPO status or drug not
suitable for GI absorption
IM route – is fairly rapid because muscles are highly
vascular, desirable to retard the speed of absorption,
can be added to oily base drugs
UNEXPECTED RESPONSES TO DRUGS
TERATOGENIC – causes development of physical
defects to fetus in vitro
IDIOSYNCRACY – unique, unusual response to a drug.
Ex. Tranquilizer causes agitation and excitement rather
than tranquility
PARAXODICAL- Opposite effect from that expected
TOLERANCE – decreased response to a drug that
develops after repeated doses. To achieve desired
effect dosage is increased or replaced.
DEPENDENCE- Acquired need for a drug that
may produce psychological or physical
symptoms of withdrawal when drug is
discontinued.
Psychological-craving, no physical symptoms of
withdrawal other than anxiety
Physical – cells actually have need of the drug
like retching, nausea, pain tremors or sweating
HYPERSENSITIVITY –immune response (allergy) to a drug
in varying degrees
-rash , hives after 3-4 days of drug therapy
ANAPHYLACTIC REACTION – severe, possibly fatal.
Allergic (hypersensitivity) response
-signs are itching, urticarial(hives), hyperemia (reddened
warm skin) vascular collapse, shock, cyanosis, laryngeal
edema, dyspnea.
- tx….. includes CPR, epinephrine(adrenaline) to raise BP,
corticosteroid (Solu-medrol) to reduce inflammation and
immune response or antihistamine (Benadryl) to
suppress histamine, thereby reducing redness, itching
and edema