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Pharmacokinetics lecture notes 2

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PHARMACOKINETICS LECTURE NOTES:
DRUG is a substance intended for the use in the
diagnosis, cure, mitigation, treatment, or prevention
DOSAGE FORM OR DRUG PRODUCT -
considered to be drug delivery system that release
and deliver drug to the site of action such that they
produce the desired effect
-Designed specifically to meet the patient’s need
including palatability, convenience, and safety
DOSAGE FORM
SYSTEMIC EFFECT drug enters to the
blood streams
LOCAL EFFECT site of administration
XENOBIOTICS foreign compounds exposed to
the biological system
DRUG PRODUCT PERFORMANCE release
of the drug substances from the drug product either
for local drug action or for drug absorption into the
plasma for systemic therapeutic activity
BIOPHARMACEUTICS the examination of the
interrelationship of the physical/chemical properties
of the drug, the dosage form (drug product) in
which the drug is given, and the route of
administration on the rate and extent of systemic
drug absorption
THE DRUG PRODUCT
PHYSICAL / CHEMICAL PROPERTIES
OF A DRUG (PC)
DOSAGE FORM (DF)
ROUTE OF ADMINISTRATION (RoA)
DRUG DISPOSITION a term used to describe
drug distributions and elimination
IMPORTANCE OF DRUG DISTRIBUTION
Drug disposition characterization is an
important pre-requisite for determination or
modification of dosing regimens for an
individual and group of patients
CLINICAL Pk the application of
pharmacokinetic methods to drug therapy
THERAPEUTIC DRUG MONITORING (TDM)
an application of clinical pk that is used for every
potent drugs (narrow therapeutic range) in order to
optimize efficacy and to prevent any adverse
toxicity
RATE AND EXTENT OF
SYSTEMIC DRUG ABSORPTION
(BIOAVAILABILITY)
ABSORPTION
BLOOD STREAM
PROTEIN BOUND
METABOLISM
DISTRIBUTION
METABOLITES
TISSUE BOUND
ELIMINATION

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Example: Theophylline; Warfarin; aminoglycosides
and anticonvulsant are frequently monitored
Theophylline plasma drug concentration is
monitored
Warfarin proto thrombin clotting time
THERAPEUTIC RANGE OF SOME DRUGS
DRUGS
DISEASE
Digoxin
Congestive
Heart Failure
Gentamicin
Infections
Lidocaine
Arrhythmias
Phenytoin
Epilepsy
Propanol
Angina
Salicylic Acid
Chest Pain
Theophylline
Asthma
PHARMACOLOGY science that deals with the
study of drugs including its mechanism, effects, and
used of drugs. Including pharmacognosy,
pharmacodynamics, pharmacokinetics,
pharmacotherapeutics, and toxicology.
CLINICAL PHARMACOLOGY the
application of pharmacology in clinical medicine
including clinical trial
PHARMACOKINETICS the study of drug
effect including distribution and disposition due to
genetic differences which can affect individuals’
response to drugs which in terms of therapeutic
effect and adverse effect
DRUG CONCENTRATION DRUG RESPONSE
TOXIC
POTENTIALLY TOXIC
THERAPEUTICS
POTENTIALLY SUB THERAPEUTIC
SUBTHERAPEUTIC
PHARMACODYNAMICS is the study of the
biochemical and physiological effects of drugs on
the body; this includes mechanisms of drug action
and relationship between drug concentration and
effect.
DRUG EXPOSURE refers to the dose (drug
input in the body) and various measures of acute or
integrated drug concentration in plasma and other
biological fluid
DRUG RESPONSE direct measure of the
pharmacologic effect of the drug
DRUG RESPONSE MEASURED
CLINICAL REMOTE BIOMAKERS receptor
occupancy
PRESUMED MECHANISTCS EFFECT ace
inhibition
POTENTIAL OR ACCUPTED SURROGATE
effects on blood pressure lipids, or cardiac output
-Full range of short term and long term
TOXICOKINETICS application of
pharmacokinetics principle to the design, conduct
and interpretation of drug safety evaluation studies
and in validating dose related exposure in animals
CLINICAL TOXICOLOGY the study of
adverse effect of drugs and toxic substances
(poison) in the body
LADMER SYSTEM (important in making
decision)
Liberation
Absorption
Distribution
Metabolism
Excretion
Response

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PHARMACOKINETICS LECTURE NOTES: DRUG – is a substance intended for the use in the diagnosis, cure, mitigation, treatment, or prevention ABSORPTION DOSAGE FORM OR DRUG PRODUCT considered to be drug delivery system that release and deliver drug to the site of action such that they produce the desired effect BLOOD STREAM -Designed specifically to meet the patient’s need including palatability, convenience, and safety PROTEIN BOUND DOSAGE FORM ❖ SYSTEMIC EFFECT – drug enters to the blood streams ❖ LOCAL EFFECT – site of administration XENOBIOTICS – foreign compounds exposed to the biological system DRUG PRODUCT PERFORMANCE – release of the drug substances from the drug product either for local drug action or for drug absorption into the plasma for systemic therapeutic activity BIOPHARMACEUTICS – the examination of the interrelationship of the physical/chemical properties of the drug, the dosage form (drug product) in which the drug is given, and the route of administration on the rate and extent of systemic drug absorption THE DRUG PRODUCT RATE AND EXTENT OF SYSTEMIC DRUG ABSORPTION (BIOAVAILABILITY) ❖ PHYSICAL / CHEMICAL PROPERTIES OF A DRUG (PC) ❖ DOSAGE FORM (DF) ❖ ROUTE OF ADMINISTRATION (RoA) METABOLISM DISTRIBUTION METABOLITES TISSUE BOUND ELIMINATION DRUG DISPOSITION – a term used to describe drug distributions and elimination IMPORTANCE OF DRUG DISTRIBUTION ❖ Drug disposition characterization is an important pre-requisite for determina ...
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