• It is derived from two Greek words: pharmakon OTHER ROUTES OF DRUG ADMINISTRATION:

(drug or poison) and kinesis (motion).

• Pharmacokinetics is the study of drug
movement throughout the body.
• It also includes what happens to the drug as it
makes this journey.
WHY DOES THE NURSE NEED TO APPLY
KNOWLEDGE OF PHARMACOKINETICS IN DRUG
THERAPY?
Enteral
• Oral (Enteric Coated and Extended Release)
• Sublingual and Buccal
Parenteral
• IV, IM, SC, ID
Oral / Nasal Inhalations
• Both the oral inhalation and nasal routes of
administration provide rapid delivery of drug
across the large surface area of mucous
membranes of the respiratory tract and
pulmonary epithelium.
• Drug effects are almost as rapid as are those with
IV bolus.
• Drugs that are gasses (some anesthetics) and
those that can be dispersed in an aerosol are
administered via inhalation.

Intrathecal / Intraventricular
• The blood-brain barrier typically delays or
prevents the absorption of drug into the central
Fig. 4.1 = The four basic pharmacokinetic processes. nervous system (CNS). When local, rapid effects
Dotted lines represent membranes that must be crossed are needed, it is necessary to introduce drugs
as drugs move throughout the body. directly into the rapid cerebrospinal fluid.

ABSORPTION
Refers to what happens to a drug from the time it is
introduced to the body until it reaches the circulating fluids
and tissues.
Drugs can be absorbed from many different areas in the
body: through the GI tract either orally or rectally, through
mucous membranes, skin, lung, muscle, or
subcutaneous tissues.
Topical
• Is used when a local effect if the drug is desired.
Transdermal
• This route of administration achieves systemic
effects by application of drugs to the skin, usually
via a transdermal patch.
• The rate of absorption can vary markedly,
depending on the physical characteristics of the
skin at the site of application, as well as the lipid
solubility of the drug.

ROUTES OF ADMINISTRATION

Otic = ear

Ocular = eye

Oral = mouth

Sublingual = under tongue

Buccal = between gums & cheek

Inhalation = lungs

Epidural = spine

Rectal = rectum

Topical = skin

Parenteral = IV, IM, SC

 ROUTE OF ABSORPTION
ADMINISTRATION PATTERN
Oral Variable; affected by many
factors
Sublingual Depends on the drug:
Few drugs (for example,
nitroglycerin) have rapid,
direct systemic absorption.
Most drugs erratically or
incompletely absorbed.
Intravenous • Absorption not required.
Intramuscular Depends on drug
diluents:
• Aqueous solution:
prompt
• Depot preparations:
slow and sustained.
Subcutaneous Depends on drug
diluents:
• Aqueous solution:
prompt
• Depot preparations:
slow and sustained
Inhalation • Systemic absorption
may occur; this is not
always desirable.
Topical • Variable; affected by
skin condition, area of
skin, and other factors.
Transdermal (patch) • Slow and sustained
Rectal • Erratic and variable
ADVANTAGES DISADVANTAGES EXAMPLES
• Safest and most common, • Limited absorption of • Acetaminophen
convenient, and economical some drugs. tablets
route of administration. • Food may affect
absorption. • Amoxicillin
• Patient compliance is suspension
necessary.
• Drugs may be metabolized
before systemic
absorption.
• Bypasses first-pass effect. • Limited to certain types of • Nitroglycerin
• Drug stability maintained drugs. • Buprenorphine
because of the pH of saliva • Limited to drugs that can
relatively neutral. be taken in small doses.
• May cause immediate • May lose part of the drug
pharmacological effects. dose if swallowed.
• Can have immediate effects. • Unsuitable for oily • Vancomycin
• Ideal if dosed in large substances. • Heparin
volumes. • Bolus injection may result
• Suitable for irritating in adverse effects.
substances and complex • Most substances must be
mixtures. slowly injected.
• Valuable in emergency • Strict aseptic techniques
situations. needed.
• Dosage titration permissible.
• Ideal for high molecular
weight proteins and peptide
drugs.
• Suitable if drug volume is • Affects certain lab tests • Haloperidol
moderate. (creatine kinase) • Depot medroxy-
• Suitable for oily vehicles and • Can be painful progesterone
certain irritating substances. • Can cause intramuscular
• Preferable to IV if patient hemorrhage (precluded
must self-administer. during anticoagulation
therapy)
• Suitable for slow-release • Pain or necrosis if drug is • Epinephrine
drugs. irritating. • Insulin
• Ideal for some poorly soluble • Unsuitable for drugs • Heparin
suspensions. administered in large
volumes.
• Absorption is rapid; can have • Most addictive route (drug • Albuterol
immediate affects. can enter the brain • Fluticasone
• Ideal for gases. quickly)
• Effective for patients with • Patient may have difficulty
respiratory problems. regulating dose.
• Dose can be titrated. • Some patients may have
• Localized effect to target difficulty using inhalers.
lungs; lower doses used
compared to that with oral or
parenteral administration.
• Fewer systemic side effects.
• Suitable when local effect of • Some systemic absorption • Clotrimazole
drug is desired. can occur. cream
• May be used for skin, eye, • Unsuitable for drugs with • Hydrocortisone
intravaginal, and intranasal high molecular weight or cream
products. poor lipid solubility. • Timolol eye drops
• Minimizes systemic
absorption.
• Easy for patient.
• Bypasses first-pass effect. • Some patients are allergic • Nitroglycerin
• Convenient and painless. to patches, which can • Nicotine
• Ideal for drugs that are cause irritation. • Scopotamine
lipophilic and have poor oral • Drug must be highly
bioavailability. lipophilic.
• Ideal for drugs that are • May cause delayed
quickly eliminated from the delivery of drug to
body. pharmacological site of
action.
• Limited to drugs that can
be taken in small daily
doses.
• Partially bypasses first-pass • Drugs may irritate the • Bisacodyl
effect. rectal mucosa. • promethazine
• Bypasses destruction by • Not a well-accepted route.
stomach acid.
• Ideal if drug causes vomiting.
• Ideal in patients who are
vomiting, or comatose.
 DRUG ABSORPTION ACTIVE TRANSPORT
• Active transport requires a carrier, such as an
• It is the movement of the drug into the
enzyme or protein, to move the drug against a
bloodstream after administration.
concentration gradient.
• Drugs can be absorbed into cells through various
• Energy is required for active absorption. Driven
processes, which include passive diffusion,
by the hydrolysis of ATP.
active transport, and filtration.
• Pinocytosis is a process by which cells carry a
• The rate and extent of absorption depend on the
drug across their membranes by engulfing the
environment where the drug is absorbed,
drug particles in a vesicle.
chemical characteristics of the drug, and the
route of administration (which influences
bioavailability).

PASSIVE DIFFUSION
• The driving force for passive diffusion of a drug
is the concentration gradient across a membrane
separating two body compartments.
• In other words, the drug moves from an area of
high concentration to one of lower concentration.
• Passive diffusion does not involve a carrier, is not
saturable, and shows low structural specificity.

ENDOCYTOSIS
• This type of absorption is used o transport drugs
of exceptionally large size across the cell
membrane.
• Endocytosis involves engulfment of a drug by the
cell membrane and transport into the cell by
pinching off the drug-filled vesicle.

FACILITATED DIFFUSION
• Facilitated diffusion relies on a carrier protein
to move the drug from an area of higher
concentration to an area of lower concentration.
• Passive transport does not require energy to
move drugs across membrane.
BIOAVAILABILITY
• The amount of drug that reaches in the
bloodstream.
• Bioavailability of IV is 100% whereas Orally
administrative drugs is always less than 100%
• Bioavailability is determined by comparing
plasma levels of a drug after a particular route of
administration (for example, oral administration)
with levels achieved by IV administration.
Factors that influence
bioavailability:
1. First-pass hepatic
metabolism
2. Solubility of the drug
3. Chemical instability
Route Factors Affecting Absorption
Intravenous None: direct entry into the venous
system.
Intramuscular Perfusion or blood flow to the muscle.
Fat content of the tissue.
Temperature of the muscle:
• cold causes vasoconstriction
and decreases absorption; heat
causes vasodilation and
increases absorption.
Subcutaneous Perfusion or blood flow to the tissue.
Fat content of the tissue.
Temperature of the tissue:
• cold causes vasoconstriction
and decreases absorption; heat
causes vasodilation and
increases absorption.
PO (oral) Acidity of stomach
Length of time in stomach
Blood flow to gastrointestinal tract
Presence f interacting foods or drugs
PR (rectal) Perfusion or blood flow to the rectum
Lesions in the rectum
Length of time retained for absorption
Perfusion of blood flow to the area
Mucous
membranes Integrity of the mucous membranes
Presence of food or smoking
(sublingual,
buccal) Length of time retained in the area
Topical (skin Perfusion or blood flow to the area
Integrity of skin
Inhalation Perfusion or blood flow to the area
Integrity of lung lining
Ability to administer drug properly
METABOLISM (Biotransformation)
• The chemical alteration of drug structure.
• The LIVER is the primary site of metabolism.
• Everything that is absorbed from the GI tract first
enters the liver to be “treated”. The liver detoxifies
many chemicals and uses other to produce
needed enzymes and structures.
• Most drug metabolism takes place in the liver and
is catalyzed by the cytochrome P450 system of
enzymes.
• The most important consequence of drug
metabolism is promotion of renal drug excretion
by converting lipid soluble drugs into more
hydrophilic forms.
FIRST PASS EFFECT
• Aka First-pass hepatic metabolism.
• When a drug is absorbed from the GI tract, it
enters the portal circulation before entering the
systemic circulation.
• If the drug is rapidly metabolized in the liver or gut
wall during this initial passage, the amount of
unchanged drug entering the systemic circulation
is decreased.
PRODRUG
• It is a compound that is metabolized into an
active pharmacologic substance.
• Prodrugs are often designed to improve drug
bioavailability; instead of administering a drug
directly.
• A corresponding prodrug might be used instead
to improve a pharmacokinetics, decrease
toxicity, or target a specific site of action.
HALF-LIFE ( t ½ )
• It is the time it takes for the amount of drug in the
body to be reduced by half.
• The amount of drug administered, the amount of
drug remaining in the body from previous doses,
metabolism, and elimination affect the half-life of
a drug.
• By knowing the half-life, the time it takes for a
drug to reach a steady state (plateau drug level)
can be determined.
STEADY STATE
• It occurs when the amount of drug being
administered is the same as the amount of drug
being eliminated.
• A steady state of drug concentration is necessary
to achieve optimal therapeutic benefit.
• This takes about four half-lives, if the size of all
doses is the same.
• For example, digoxin--which has a half-life of 36
hours with normal renal function—takes
approximately 6 days to reach a steady state
concentration.
LOADING DOSE
• Large initial dose of drug administration.
• By giving large dose, that is significantly higher
than maintenance dosing, therapeutic effects can
be obtained while a steady state is reached.
• After the loading dose, maintenance dosing is
begun; this is the dose needed to maintain drug
concentration at steady state when given
repeatedly at a consistent dose and constant
dosing interval.

Special Considerations of Drug Metabolism

• Age
• Induction and Inhibition of Drug-Metabolizing
Enzymes
• First Pass Effect
• Nutritional Status
• Competition Between Drugs

DRUG EXCRETION

• It is defined as the removal of drugs from the

body.
• Drugs and their metabolites can exit the body in
urine, bile, sweat, saliva, breast milk, and expired
air.
• The most important organ from drug excretion is
the kidney.

STEPS IN RELAN DRUG EXCRETION

1. Glomerular Filtration – filtration moves drugs
from blood to urine, Protein-bound drugs are not
filtered.
2. Passive Reabsorption – Lipid-soluble drugs
move back into the blood, Polar and ionized
drugs remain in the urine.
3. Active transport – Tubular “pumps” for organic
acids and bases move drugs from blood to urine.

NON-RENAL ROUTES OF EXCRETION

• Breast Milk
• Bile
• Lungs
• Sweat and Saliva