9/7/23

PROF. MARIVIC E. ILARDE

FACUTLY- COLLEGE OF NURSING
OLFU-VALENZUELA CAMPUS

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At the end of the topic,

learners will be able to:

q Understand the concept of

pharmacokinetics
q Discuss the phases and
processes of drugs once
inside the body

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3 Phases of • PHARMACEUTIC 3 Phases of • PHARMACEUTIC

Drug action PHASE Drug action PHASE

the 1st phase of drug action the 1st phase of drug action
2 Phases
In the GI tract, drugs need to be in In the GI tract, drugs need to be in 1. Disint
solution so they can be absorbed solution so they can be absorbed
• PHARMACOKINETIC parts
• PHARMACOKINETIC The drug disintegrates into The drug disintegrates into
PHASE 2. Disso
PHASE small particles to dissolve into a small particles to dissolve into a
liquid liquid smaller
The rate of dissolution is the The rate of dissolution is the
time it takes the drug to
dissolve
time it takes the drug to
disintegrate and dissolve to disintegrate and dissolve to
become available for the body
• PHARMACODYNAMIC to absorb it
• PHARMACODYNAMIC
become available for the body
to absorb it
PHASE PHASE

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3 Phases of • PHARMACEUTIC 3 Phases of • PHARMACEUTIC

Drug action PHASE Drug action PHASE

2 Phases of Pharmaceutic Phase Tablets are not 100% drug

1. Disintegration – breakdown into smaller Fillers and inert substances – excipients

parts • PHARMACOKINETIC • PHARMACOKINETIC

Allow drug to take on particular size and shape and to enhance drug
dissolution
PHASEinto even
2. Dissolution – further breakdown PHASE
smaller parts in GIT for faster absorption; PROF. MARIVIC E. ILARDE
dissolve into liquid FACUTLY- COLLEGE OF NURSING
OLFUVALENZUELA CAMPUS

• PHARMACODYNAMIC • PHARMACODYNAMIC
PHASE PHASE

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the 1st phase of drug action
In the GI tract, drugs need to be in
solution so they can be absorbed 2
The drug disintegrates into
small particles to dissolve into a
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Dissolution Dissolu
Form of drug ( LIQUIDVS. Form
3 Phases of • PHARMACEUTIC 3 Phases
SOLID) of absorbed
– liquids more • PHARMACEUTIC SOL
Drug action PHASE Drug action
than solid, already in
rapidly available for GI
solution, PHASE than
rapi
absorption abso
Gastric pH( acidic vs. alkaline) – Gas
acidic media faster acid
disintegration & absorption disin
• PHARMACOKINETIC normal gastric pH – 1.5-3.5
• PHARMACOKINETIC norm
PHASE Age – young & elderly PHASE Age
– increase pH decrease – inc
absorption abso
Aid in the
processing of the Protect, support or Assist in product Assist in the Assist in
enhance stability, identification, and effectiveness and maintaining the
drug delivery
system during its bioavailability, or enhance any /or delivery of the integrity of the
manufacture
patient
acceptability • PHARMACODYNAMIC
attribute of the
overall safety
drug in use drug product
during storage • PHARMACODYNAMIC
PHASE PHASE
Important Uses of Drug Excipients
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3 Phases of • PHARMACEUTIC 3 Phases of • PHARMACEUTIC

Drug action PHASE Drug
Factors action
Affecting
PHASE
Rate of Dissolution
Factors Affecting Rate of Enteric coated drugs – resist disintegration in
Dissolution Factors
gastric Affecting Rate occurs
acid Disintegration of Dissolution
only in
Form of drug ( LIQUIDVS.
SOLID) – liquids more
Enteric coated drugs
alkaline environment ( intestine) – resist disintegration
Should not be in
• PHARMACOKINETIC • PHARMACOKINETIC
gastric acid: Disintegration occurs only in
absorbed than solid, already a crushed
PHASE alkaline environment PHASE
solution: rapidly available for
GI absorption
Presence of food – interfere(intestine):
with Should not
Gastric pH( acidic vs. alkaline)
be crushed
dissolution &PROF.
absorption, enhance
MARIVIC E. ILARDE
– acidic media: faster Presence
absorption FACUTLY-of food
COLLEGE
ofOLFUVALENZUELA
other – may
mayinterfere
OF NURSING
drugs, be with
CAMPUS
disintegration & absorption dissolution
protectants & absorption,
of gastric mucosa. may enhance
• PHARMACODYNAMIC
normal gastric pH – 1.5-3.5 • PHARMACODYNAMIC
absorption of other drugs, may be
Age – young & elderly
PHASE protectants of gastric mucosa PHASE
– increase pH:
decrease absorption
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3 Phases of • PHARMACOKINETIC
Drug action PHASE

• PHARMACOKINETIC
PHASE

• PHARMACODYNAMIC
PHASE

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PROF. MARIVIC E. ILARDE

FACUTLY- COLLEGE OF NURSING
OLFUVALENZUELA CAMPUS

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- mo
into
aft
- 80%
by
- Mo
mo
adm
circ

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Physico-chemical
(Drug)
- movement of the drug
into the bloodstream
Blood flow to solubility
after administration. absorbing site
- 80% of drugs are taken
by mouth – enteral Chemical stability
- Movement of drug Total surface area
for absorption
molecules from site of Bioavailability Lipid to water
administration to • is availability of drug to partition
coefficient
circulatory system the general circulation or Time of arrival and
contact time at
site of pharmacological absorption site Degree of
actions. ionization

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Physico-chemical Physico-chemical
(Drug) (Drug)
Solubility
Solubility
Blood flow to
• water soluble: easily absorbed
Blood flow to Chemical stability
• fat soluble needs to be dissolved in alkaline
absorbing site environment absorbing site • water or fat
• A weak acid is more lipid-soluble in an acidic solution
• A weak base is more lipid-soluble in an alkaline stability
solution. Chemical stability
• A weak acid is more WATER-soluble in an alkaline
Total surface area solution Total surface area
for absorption • A weak base is more WATER-soluble in an acidic for absorption
solution. Lipid to water Lipid to water
partition partition
coefficient coefficient
Time of arrival and Time of arrival and
contact time at contact time at
absorption site Degree of absorption site Degree of
ionization ionization

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Physico-chemical Physico-chemical
(Drug) (Drug)

Solubility Solubility
Blood flow to Blood flow to
absorbing site absorbing site

Chemical stability
Lipid to water partition
Chemical stability
Total surface area coefficient Total surface area
for absorption • meds stored in water is for absorption
Degree of Ionization
Lipid to water
faster to absorb • Charged or ionized are slowly
partition
absorbed because it can’t
coefficient
Time of arrival and Time of arrival and penetrate a semipermeable
contact time at contact time at membrane, it needs ATP
absorption site Degree of absorption site • Eg: (+)aluminum, chromium
ionization • (-) chloride, iodide, oxide

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Passive Pinocytosis Active

transport Transport

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Passive transport Passive transport

2. Facilitated diffusion
1.Diffusion • requires a carrier such as
• Drugs move across Pinocytosis Active
enzyme or protein to move Pinocytosis
the cell membrane
Transport
the drug against a
concentration gradient
from an area of • Diffusion takes place in the aqueous • does not require energy.
and lipid environment
higher concentration • Aqueous: interstitial compartments • Low lipid solubility like
that surrounds tissues glucose penetrate
to one of lower • Lipid soluble drugs diffuse rapidly in membrane more rapidly
concentration the cell membrane because cell
membrane is lipid
• Small molecules penetrate membrane
rapidly

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Pinocytosis Active
Transport

• is the process by • requiresActive

which cells carry a
drug across their
membrane by
engulfing the drug
particles in a vesicle
energy to
Transport
facilitate the transport
of drug molecules
against a concentration
gradient, which usually
occurs at specific sites
• Iron salts, levodopa for Parkinson’s
in the small intestine disease, antithyroid drugs

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• is the movement of the drug

from the circulation to body
tissues.

• process by which drug becomes available to

body fluids and tissues.
• is the movement of the drug from the
circulation to body tissues.

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but they
faster.

Transporters
• help drugs get across biological barriers (such Factors Affecting
the Distribution of
as the gut lining) or work to exclude them
Drugs
from a part of the body (such as the brain)
• are direct targets for many drugs, and most
drugs are thought to interact with at least Size of
one transporter. the
organ

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which
chemi
drugs
that ca
• refers to the reversible
association of a drug with the
proteins of the plasma
compartment of blood, and this
binding is due to electrostatic
and hydrophobic forces between
drug and protein.
• Agents that are minimally protein
bound penetrate tissue better
than those that are highly bound,
but they are excreted much
faster.
• unbound drug are
pharmacologically active

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• some drugs are metabolized to an inactive form

and excreted--- reduced amount of active drug

AKA: biotransformation • a drug gets metabolized at a specific location in

• is the process by which
the body chemically
changes drugs into a
form that can be
excreted
• Active to inactive form
the body that results in a reduced concentration
of the active drug upon reaching its site of action
or the systemic circulation
• some drugs are metabolized to an inactive form
and excreted--- reduced amount of active drug

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• Different d
pharmacologically active (PRODRUG) lives; how
• Decreased drug metabolism rate will
rule: after
result to excess drug accumulation that 50% of the
Cytochrome P450 system (CYP)
can lead to toxicity removed f
• Heme-containing liver enzymes that
convert drugs to metabolites, making
the drug inactive
• Some metabolites are still
pharmacologically active (PRODRUG)
• Decreased drug metabolism rate will
result to excess drug accumulation that
can lead to toxicity
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• a steady state of drug

concentration is necessary
to achieve optimal
therapeutic benefit.
Drug half-life Therapeutic Effect of the
• is the time it takes for the amount of Drug
drug in the body to be reduced by half • can be achieved when the
amount of drug being
• Different drugs have different half-lives; administered is the same
however, they all follow this rule: after as the amount of drug
Cytochrome P450 system (CYP) Cytochro
being eliminated.
one half-life has passed, 50% of the
• Heme-containing liver enzymes
• a steady state of drug that • Heme-
initial drug amount is removed from the concentration is necessary
body.
convert drugsoptimal
to achieve to metabolites, conver
therapeutic benefit.
making the drug inactive making
45 • Decreased
46 drug metabolism rate • Decrea
will result to excess drug will res
accumulation that can lead to accum
toxicity toxicity
Example: Example:
• Half-life/ Elimination half-
• Ibuprofen has a half life of life (t ½)- time it • Ibuprofen ha
about 2 hours. takes for one half of drug about 2 hour
• if the patient takes 200 mg, concentration to be eliminated • if the patient
in 2 hours, 50% of the drug • Short t1/2= 4-8hrs: given in 2 hours, 50
will be gone, leaving 100 mg. • Half-life/ Elimination
several times a day (ex. will be gone,
• after 2 hours - 50 mg.
half-life (t ½)- time it
Penicillin G) • after 2 hours
takes for one half
• of drug
Long t ½ = >12 hours: given
• after 2 hours – 25 mg • after 2 hours
concentration to be 2x or 1x/day
• after 2 hours – 12.5 mg eliminated • after 2 hours
• (Ex. Digoxin)
• after 2 hours – 6.25 mg • Short t1/2= 4-8hrs: given • after 2 hours
several times a day (ex.
47 Penicillin G)48
• Long t ½ = >12 hours:
given 2x or 1x/day
• (Ex. Digoxin) 12
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me
dru
oth
slow
Genetics

FACTORS FACTORS
Drug Stress
Metabolism
Physiologic
Genetics
Environment Physiologic Drug Metabolism Environment

Stress

49 50

some people Liver disease

metabolize
Genetics drugs rapidly,
Infants Genetics
others more Elderlies
slowly

FACTORS FACTORS
Physiologic Drug Metabolism Environment Physiologic Drug Metabolism Environment

Stress Stress

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Smoking
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Genetics Genetics

FACTORS FACTORS
Physiologic Drug Metabolism Environment Physiologic Drug Metabolism Environment

prolonged
illness,
Stress Smoking
surgery
Stress
Drugs

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Liver disease Liver disease

Infants Infants
Elderlies Elderlies

• removal of the drug

from the body
• Drug is changed
into inactive form
and excreted by the
body

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Routes: Routes:
• Urine
• Urine • Bile: digoxin, warfarin
• Bile • Sweat: opiates, amphetamines, and
• Sweat buprenorphine
• Saliva • Saliva: caffeine, phenytoin, and
theophylline.
• Tears • Tears: phenobarbital, carbamazepine,
• Milk • Milk: paracetamol, antibiotics
• Stool • Stool: streptomycin, neomycin
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Routes:
Kidney- main organ for drug elimination: Factors
Affecting
Kidney
Renal
Molecular
Concentration
leave the body through urine the Rate
Urine pH of
of disease
blood
drug
weight
inflow
the
Drug
plasma
Free or/unbound/water soluble drugs- Elimination

filtered in the kidney: excreted easily

(+) kidney disease- dose must be
decreased

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• Milk
• Stool

Urine pH
DRUG Clearance
Factors Kidney
Molecular Affecting disease
weight the Rate of
• urine pH influences drug excretion
Drug • normal urine pH 4.6-8
Elimination
Concentration Renal • acidic urine promotes elimination of weak base
of drug in the blood flow
plasma
drugs.
• alkaline urine promotes elimination of weak acid
drugs.

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• Bioavailability

• biotransformation

• Drug elimination of drug clearance

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