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PHARMACOLOGY Dela Rosa Edition

INTRODUCTION :BASIC PHARMACOLOGY


PHARMACOLOGY
Science of drug interactions between living
systems & moleculess introduced from outside the
system
Study of substances that interact with living
systems through chemical processes, especially by
binding to regulatory molecules and activating or
inhibiting normal body processes.
GOAL OF PHARMACOLOGY
To understand the mechanism by which drugs
interact with the biologic systems in the diagnosis
& treatment of disease
DRUG
An agent intended for use in the diagnosis ,
mitigation , treatment
ent ,cure, or prevention of
disease in man or in animal
A natural product ,chemical substance, or
pharmaceutical preparation to be used in the
diagnosis or treatment of a disease
Varies in terms of
o Molecular size
o Shape
o Chemical nature
DRUG NAMES :
Chemical name

Chemical

N-acetyl-

structure of the

paminophenol

drug
Non proprietary

Generic name

acetaminophen

Trade name or

Tylenol

1. Pharmacy
involved in the compounding, preparation,
collection, standardization and dispensing of the
drug.
2. Pharmacognosy
recognize the drugs (description, sources, chemical
composition, nature of doing, etc)
study of the physical and chemical properties of the
drugs with the description and identification of
their sources and nature.)
3. Biochemorphology
(structure activity relationship or SAR)
how the chemical structure of the drug is related to
physiological, biological and biochemical effects.
endogenous catecholamines

synthesized in the body

(epinephrine, norepinephrine, dopamine, tyrosine)


synthetic (exogenous) catecholamines

from outside given to the body

(isoproterenol)
ephedrine
acting sympathomimetic
symp
agent; CNS

mixed-acting
stimulation; not a catecholamine but its effects on
bronchi and other smooth muscles are
quantitatively similar to those of epinephrine
amphetamine
acts indirectly by releasing norepinephrine; also a

CNS stimulant; depresses the appetite by affecting


the feeding center in the lateral hypothalamus
Norepinephrine affects 1, 2 and 1
Epinephrine affects 1, 2, 1 and 2

name
Proprietary name

brand name
BRANCHES OF PHARMACY

4. Toxicology
- study of the harmful effects of drugs and other
chemicals on human, animals and plants
5. Posology
- deals with the dosage of the drug required to
produce a therapeutic response
6. Molecular Pharmacology
studies the mechanism of
enzymatic level (gene therapy;
engineering)

action of a drug at
genetic

7. Developmental Pharmacology
- deals w// drug given to mother as it affects the
fetus during natal, prenatal,
perinatal &
neonatal periods.
8. Pharmacogenetics
- studies the influence of heredity on
the
pharmacokinetic and pharmacodynamic response
of the drug.
9. Pharmacogenomic
- describes the use of genetic information to guide
the choice of drug therapy on an individual basis

discovers which specific gene variations are


associated with a good or poor therapeutic
response to a particular drug

10. Pharmacoepidemiology

studies the response in population at a given time


and space of the pharmacologic events, whether
they are adverse or beneficial with the use of
measures of epidemiology

PHASES OF A CLINICAL DRUG INVESTIGATION


PHASE
I
II
III
IV

PURPOSE
establish safety
Establish efficacy and dose
Verify efficacy and detect ADRS
Obtain additional data following approval

PHASES OF DRUG MANUFACTURE


11. Pharmacoeconomics

studies the cost effectiveness of drug treatment

deals with the interethnic differences in response


to or metabolism of chemical substances, and the
presence and absence of enzymes in different
regions of
the Phil. or of different races.

I
ANIMAL
TESTING
Pre-clinical
testing

13. Clinical Pharmacology

tested in at least 2 rodent & 1 non


rodent species
1 to 3 yrs. (ave. 18 months) here you
determine for the:
o Acute toxicity - observation of animal
7-14 days using a simple dosage of the
drug being tested.
o Subacute toxicity - 2 weeks to 3
months.
o Chronic toxicity - 6 months to 2 years.
-

12. Ethnopharmacology

PHASE

Deals w/ rational development of drugs, their safe


& effective use, and other proper evaluation of
drugs in humans for the prevention, diagnosis,
treatment, alleviation or cure of a disease.
refers to the rational use of
criteria)

drugs (ESSC

II
FDA
III
CLINICAL
TESTING

Efficacy considers pharmacodynamics,


pharmacokinetics, of the different drug groups;
ability of drug to accomplish what it is intended to
do.
Safety side effects, toxicity, frequency and
severity

30 days safety review


Includes humans (healthy adult males)
2-10 yrs (average 5-6 yrs)
the lowest effective dose given to man because
humans can react differently to the drug
pediatric patients not included in the testing
because some drugs can have adverse effects on
the development of the patient.
Short term
Long term (chronic toxicity, reproduction,
teratogenicity)
Phase I

Suitability convenience, compliance, practicality,


contraindications and possible interactions.

Cost

involves normal healthy adult male


to measure the initial drug safety,
biological effects, metabolism, kinetics
done by the clinical pharmacologist

Phase II

involves selected patients, needing the


treatment

to measure therapeutic efficacy, dosage


range, metabolism, kinetics

done by clinical pharmacologist

14. Pharmacokinetics (kinetic=bodydrug)


- what the body does to the to the drug
- movement of the drug in the body and
how the
body acts on the drug
- fate of drug in the body
Involves four processes (ADME)

Phase III

Absorption
Distribution
Metabolism (biotransformation)
Excretion
15. Pharmacodynamics (dynamic = drugbody)
- what the drug does to the body
- biochemical and physiological effects
of drugs
and their mechanism of action
(includes enzymatic or molecular level and also
toxicological or adverse effects.)

involves large sample of selected patients


to measure the safety and efficacy
done by clinical investigators

IV
New Drug
Application
(NDA)

- Review (BFAD)
- Marketing approval

V.
Post
Marketing
Surveillance
(PMS)

-to look for chronic effects


Phase IV
drug is available commercially

Involves patient given the drug treatment


to look for adverse reactions, patterns of
drug utilization, additional indications
discovered.

Done by all physicians.

PHASES OF PRODUCT DEVELOPMENT

It takes 12 years on average for an experimental drug


to travel from lab to medicine chest.
Only five in 5,000 compounds that enter preclinical
testing make it to human testing. One of these five
tested in people is approved.

SYSTEMIC- produces a systemic effect even if you just


apply it on your on your skin; sprayed or injected
ACTIONS IN RELATION TO SPECIFIC EFFECTS
Cathartic
Laxative
Hypnotic
Diuretic

increases bowel movement


for constipated patients
induces sleep
increases urination

AntacidVasodilator

has buffering actions; neutralizes HCl


relaxed vascular smooth muscles (Ca 2+
blocker)

VARIABLES INVOLVED IN DRUG ACTIVITY


Dose of drug administered

Pharmaceutical phase
(bioavailability)
(disintegration and dissolution)

Pharmacokinetic Phase
(ADME)

Pharmacodynamic phase
(drug-cell, drug-receptor, drug-drug interactions;
individual sensitivity; pathological conditions)

Placebo I shall please


Used to achieve blindness and subjective bias
Response may involve objective, physiologic and
biochemical changes as well as change in subjects
complaints associated with the disease.
Two types:
1. do not contain pharmacologically active
ingredients (used for negative control)
2. contain some compound with
pharmacological activity different from the test
drug (used for positive control)
FUNDAMENTAL TYPES OF DRUG ACTION
STIMULATION enhances the specialized tissues
DEPRESSION diminished functional activity of specialized
tissues
IRRITATION either stimulate or depress non-specialized
tissues
OTHER DRUG ACTIONS
REPLACEMENT THERAPY- replaces what is sufficient and
deficient
ANTI-INFECTIVE- entails the use of anti-microbial agents
LOCAL- Topically applied, and action is just on the area
itself

Effects
(toxic, therapeutic, subtherapeutic)

PHARMACEUTICAL PHASE
involves disintegration of dosage form (generally
water soluble) & dissolution
of active
ingredients (lipid soluble)
Bioavailability
fraction of unchanged drug reaching the systemic
circulation following administration by any route
PHARMACODYNAMIC PHASE
Drug-drug interaction
simultaneous intake of two different drugs, one drug may
displace another for Its binding site
another may reduce the metabolism of the other
Individual sensitivity interpatient variability (for
hyperactive and hypoactive people.
Pathological conditions renal, cardiac, hepatic
dysfunctions, malnutrition

DEFINITION OF TERMS : DIDACTIC STUDY GUIDE


PHARMACOLOGY

Science of drug interactions between living systems & molecules introduced from outside
the system

DRUG ACTION AND


EFFECT
PHARMACOKINETICS
BIOAVAILABILITY

what the body does to the to the drug


movement of the drug in the body and how the body acts on the drug
fraction of unchanged drug reaching the systemic circulation following administration by
any route

FIRST ORDER KINETICS


ZERO ORDER KINTICS
VOLUME OF
DISTRIBUTION
CLEARANCE
STEADY STATE
CONCENTRATION
HALF LIFE

The measure of the apparent space in the body available to contain the drug .
The measure of ability of the body to eliminate the drug

Is the time required to change the amount of drug in the body by one half during
elimination
-t1/2

LOADING DOSE
MAINTENANCE DOSE
PEAK AND THROUGH
LEVEL OF DRUGS
PHARMACODYNAMIC

-what the drug does to the body


-biochemical and physiological effects

of drugs and their mechanism of action

EFFICACY
POTENCY
AFFINITY
AGONIST
PARTIAL AGONIST
MEDIAN EFECTIVE DOSE
THERAPEUTIC INDEX
RECEPTOR/SPARE
RECEPTOR
TOLERANCE
TACHYPHYLAXIS
OVERSHOOT OR REBOUND
PHENOMENOM
UP/DOWN REGULATION
IDIOSYNCRASY
PLACEBO/PLACEBO
RESPONSE
CLINICAL
PHARMACOLOGY

XENOBIOTICX
PHARCOEGENOMICS

Used to achieve blindness and subjective bias


Asses drug interaction

To produce its characteristic effect, a drug must be present in an appropriate


concentration at its site of action (bioavailable amount). The effect may be
subtherapeutic (lacking); while too much would cause toxicity.
Substances that are absorbed across the lungs or skin or more commonly ingested either
unintentionally
Is the study of the genetic variation that cause differences in drug response among
individuals or populations