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The study of how the body acts on drug

(absorption, distribution, metabolism and drug excretion)

Pharmacokinetics
Drug therapy
prevent, cure or control various disease states
Adequate drug doses must be delivered to the
target tissues
drug will result into toxic effects
drug will not lead to desired therapeutic effects.

Routes of Drug Administration


Determined by properties of the drug
Oral, Sublingual and Rectal are Enteral routes
Intravascular, Intramuscular and Subcutaneous are
Parenteral routes

Parenteral Routes
Used for drugs that are; unstable, poorly absorbed
in the GIT, unconscious patients or in an event that
require a rapid onset of action.
Provides the most control over the actual dose
delivered to the body
Pros
Fast! 15-30 sec for IV
3-5 minutes for IM & SC
100% bioavailability
For drugs not absorbed by
gut or irritant drugs that
cause vomit such as cancer
therapy
IV can deliver continuous
medication.
Ex; Saline
and Morphine

Cons
Addiction
Belonephobia
Infection
from
shared
needle
more threat than enteral
fetal air boluses can occur
need
strict
asepsis
[Asepsis is the state of being
free
from
disease-causing
contaminants]

Intravascular (IV)

most common parenteral route


For drugs which are not absorbed orally
Bypasses the liver
Permits a rapid effect and a maximal degree of
control over the circulating levels of the drug
Can cause hemolysis and bacterial contamination

Rectal
Useful if the drug induces vomiting if given orally or
if the patient is already vomiting
Bypasses the portal circulation
Prevents the destruction of the drug by intestinal
enzymes and low pH in the stomach
commonly used to administer antiemetic agents
[An antiemetic is
a drug that
against vomiting and nausea]

is

effective

Other Routes
Inhalation
Provides a rapid delivery of a drug across a large
surface area of the mucus membranes of the
respiratory and the pulmonary epithelium
Effect is as rapid as IV injection
For gaseous drugs
Pros
Fastest method, 7-10s for
drug to reach the brain

Cons
Instant gratification which
may leads to addiction
Difficult
in
adjusting
dosage
Difficulties in using inhaler

Intranasal
Through the nose
Eg., desmopressin, salmon calcitonin, cocaine

Intrathecal, intraventricular
Introducing drugs directly into the cerebrospinal
fluid (CSF)
Eg., amphotericin B

Topical
Is used when a local effect of a drug is required
Eg., clotrimazole, atropine

Transdermal

Intramuscular (IM) and Subcutaneous (SC)

This route of administration achieves systemic


effects by application of drugs to the skin, usually
by using a transdermal patch.
Rate of absorption varies markedly
Eg., nitroglycerin

Aqueous solution & specialized depot preparations


For drug those requires absorption which is
somewhat slower than the IV route

ABSORPTION OF DRUGS

Enteral Routes
Oral
most affordable, variable, common & complicate
Non - invasive
most drugs are absorbed in the GIT & encounter
the liver before distributed into circulation

Sublingual
Placement under the tongue and diffuse into
capillaries to enter circulation
the drug bypasses the intestine & liver & thus
avoids 1st pass metabolism

The transfer of a drug from its site of


administration to the bloodstream
Transportation of drugs from GIT has two
mechanisms
Passive diffusion
Move from to
Majority of drugs gain
access to body by this
mechanism

Active transport
Required ATP & transport
proteins
Can move drug against
concentration gradient

Factors Influencing Absorption


Blood flow to the absorption site
Total surface area available for absorption
Contact time at the absorption surface

Bioavailability

DRUG ELIMINATION

The extent to which a drug or other substance is


taken up by a specific tissue or organ after
administration; the proportion of the dose of a drug
that reaches the systemic circulation intact after
administration by a route other than intravenous.
Also called systemic availability

Routes are via bile, intestine, lung or milk but


Mostly occurs in kidney or urine.
Those drugs that have been made water soluble in
liver are often excreted in kidneys.
Kidney dysfunction will lead to toxic levels of the
drug

Drug Distribution
The process by which a drug reversibly leaves the
bloodstream & enters the interstitium (extracellular
fluid) and/or the cells of the tissues.
Affected by the following factors:
Blood Flow
Capillary permeability (capillary structure & blood
brain barrier )
Binding of Drugs to proteins

Binding of Drugs to Plasma


Proteins
Bound drugs are pharmacologically INACTIVE,
FREE & UNBOUND drug can act on target sites in
the tissues, elicit a biologic response & be available
to the processes of elimination
ALBUMIN has the strongest affinity for ANIONIC
DRUGS & HYDROPHOBIC DRUGS. [albumin binding
capacity is reversible]

DRUG METABOLISM
Eliminated by biotransformation and excreted into
bile or urine.
Liver is major site of drug metabolism

Reactions of Drug Metabolism


Kidney cannot efficiently eliminate lipophilic drugs
Liver will metabolizes lipophilic drugs by 2 phase
before being excreted by kidney
Phase I
Converts lipophilic molecules into more polar
molecules
Metabolism may increase, decrease or
unaltered pharmacologic activity of the drug.
Involved Cytochrome P450 isoenzyme system
Phase II
Consists of conjugation reactions
Uses substrates like glucuronic acid, sulfuric
acid, acetic acid, or an amino acid
Renders the metabolites INACTIVE and more
water soluble
Highly polar drug conjugates may then be
excreted by the kidney or bile

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