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Pharmacology- Science that deals with the fate of the drugs in
the body and their actions on the body.
- Closely related to
PharmacyScience of the preparation of drugsTherapeutics
Treatment of disease, by drugs and othermeans
Both a basic (i.e., molecules, cells, organ, etc) and
clinically applied science (i.e., on human
species for treatment of disease)
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Purpose of Pharmacology- To test drugs quantitatively and standardize
them so that they are available to the doctor
and patient in uniform and dependable forms.
- To determine how drugs produce their effects
- To develop new drugs
- To establish rational and safe dosaging
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What is a Drug?Any substance, other than a normal constituent
of the body or one that is required for normal
body function (e.g., food, water, oxygen), thatwhen applied to or introduced into a living
organism, has the effect of altering body
function/s.
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Drug Names and Classifications
Chemical Name
Chemical makeup
Generic name
Name the manufacturer gives a drug
Nonproprietary drug, not protected by
trademark
Lowercase letter
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Drug Names and Classifications
Brand name
Trade name
Copyrighted and used exclusively
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Drug Names and Classifications
Guidelines for drug names
Active component in single word
When two or more components, list
principal, active ingredient first
Use of common stems for drug groups
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Generic Drugs
Must be equivalent to the brand-namedrugs
FDA has an A/B rating system to establish
therapeutic equivalence of generic drugs FDA has identified generics not
therapeutically equivalent; in OrangeBook
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Generic Drugs
Patent grants the sponsor the sole right tomanufacture a drug while the patent is in
effect
Under a patent, generic and brand nameof a drug belong to the drug sponsor
Once patent expires, other companies can
produce this drug as a generic
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Components of a DrugActive Ingredients --- the substance or
substances that produce the
pharmacological and therapeutic action.
Inactive or Inert Ingredients --- thesubstance or substances that have no
therapeutic effect but are necessary inthe formulation of the preparation.
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Medicinal Drugs
Pharmacologic effects
Drug actions on living system
Classifications Therapeutic drugs: relieve symptoms
of a disease
Prophylactic drugs: prevent ordecrease the severity of disease
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Synthetically Produced Drugs
Many drugs produced syntheticallyfrom chemical substances
Sulfonamides, aspirin, sodium
bicarbonate
Biopharmaceuticals
Produced by recombinant DNA
technology
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Classifications of DrugsAccording to origin:
Natural Preparation or galenicals
Pure compounds Semi-synthetic substances
Purely synthetic compounds
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Pharmacognosy
Study and identification of natural
sources for drugs
Plants, animals, minerals, chemicals,
Ergotamine from rye fungi, digoxin from
foxglove, and morphine from the opium
poppy
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Classifications of DrugsAccording to its preparation:I. Oral solid forms
II. Oral solutions
III. Oral suspension
IV. Parenterals
V. Topical preparations applied to the skin
VI. Other topical preparations
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Classifications of DrugsAccording to BFAD product registration:
Prescription DrugsorEthical Drugs
Non-Prescription DrugsorOver-the-Counter (OTC) Drugs.
Dangerous Drugs*
ProhibitedRegulated
* These can be bought only with special prescriptions controlled bythe Dangerous Drugs Boardlike the S-2 prescription.
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Classifications of DrugsAccording to therapeutic action (Philippine National Drug Formulary):
Drugs Acting on the Nervous System
Drugs Acting on the Musculoskeletal System and Joints
Anti-Infectives
Immunologicals Cardiovascular Drugs
Diuretics
Respiratory Drugs
Anti-Allergics
Antineoplastics and Immunosuppressants Drugs Affecting the Blood
Blood Products and Blood Substitutes
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Classifications of DrugsAccording to therapeutic action:(Philippine National Drug Formulary): Antidotes
Gastrointestinal Drugs
Hormones and Hormone Antagonists
Drugs Acting on the Uterus Solutions Correcting Water Electrolyte, Acid-Base, and Caloric
Disturbances
Diagnostic Agents
Dermatologicals and Mucous Membrane Agents (Topical)
Opthalmological Preparations Ear, Nose, and Throat Preparations
Vitamins and Minerals
Disinfectants
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Routes of Drug Administration
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Scope and Division of Pharmacology
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Alternative Medicine
Billions of dollars are spent every
year on alternative medicine
Includes herbs, supplements, and
homeopathic remedies
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Concerns About
Alternative Medicine
Legitimate scientific data is scarce
Patients often do not tell prescriber and
pharmacist they are taking alternative
medicines Interaction can often occur between prescribed
drug and alternative medicine
Many alternative medicines are not
covered by governmental regulations
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Clinical Trials of New Drugs
Patients typically separated into 2 groups
Experimental group receives drug to be tested
Control group receives a standard treatment for
the illness or placebo
Double blind study
Trial participants nor study staff know whether a
particular participant is in which group Best way to determine what a new drug does
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Four Phases of Clinical Trials
Phase I Studied in 20 to 100 healthy people
Phase II Studied in patients who have the
condition it is intended to treat
Phase III Compared to commonly used
treatments
Phase IV Continuation of testing after approved
for marketing
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FDA Approval Process
FDA approval process took 7 to 10 years
FDA has made urgently needed drugs
available sooner
Prescription User Fee Act of 1992shortened the FDAs review process for
new drugs
Act on standard applications within 10 months
Act on priority applications within 6 months
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FDA Approval Process
FDA considers a new drug safe enough to
be approved when the benefits outweigh
the risk
Drugs are not tested on pregnant women
Based on all available information, drugs
are grouped into safety categories for use
during pregnancy
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FDA Pregnancy Categories
Category Risk Level
A No risk
B Risk cannot be ruled out
C Caution is advised
D Is a definite risk
X Do not use
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Postmarketing Surveillance
Office of Compliance, a branch of the FDA,
oversees drug manufacturing process
Professionals and consumers can report serious
adverse reactions to MedWatch, FDAs Medical
Products Reporting Program If drug poses a health risk, FDA will remove it
from the market even though it has already been
approved
Ensures that manufacturers follow good
manufacturing practices in FDA regulations
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Removing Drugs from
the Market
Safe does not mean harmless
every drug has risks
FDA evaluates significant adverse effects
to determine the seriousness andlikelihood that they were drug related
If risk outweighs the benefits, FDA will ask
manufacturer to withdraw a drug from the
market voluntarily
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Black Box Warning
For drugs on the market and found to be
problematic, but still provide therapy for
specific conditions
Black Box warning on package insert
Alerts prescribers to known problems
Thousands of drugs on the market have
Black Box warnings
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Controlled Substances
Controlled Substances Act, 1970
Combat escalating drug abuse
1973, establishment of DEA, branch
of the U.S. Justice Department
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Controlled Substances
Label Abuse Potential
C-I highest potential
C-II high possibility, which can lead
to severe dependence
C-III less potential
C-IV low potential
C-V lowest potential
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Drug Actions
Drugs work by a variety of chemical
mechanisms
Body continually fights to maintain a state
ofhomeostasis (stability) Achieved by a system of control and feedback
mechanisms
Drugs can be used to restore and maintain
homeostasis
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Messengers and Receptors
Cells communicate through the action of
chemical messengers, which theyproduce and send into extracellular fluids
Some chemical messengers: histamine,prostaglandin, bradkinin
Messengers recognize and communicate
with target cells via receptors (specific
protein molecules)
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Receptors
Receptor site may have specificity
Affinity is the strength by which aparticular chemical messenger binds
to its receptor site or cell
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Drug Receptor Theory
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Pharmacodynamics
The study of mechanism of action of
drugs is what is called
pharmacodynamics.
It is the study ofwhat the drug does to
the body.
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Mechanisms of Drug Action
Drugs act like chemical messengers toperform their specific actions in the body
By binding to receptors on or within body
cells, drugs can Mimic orblock the action of chemical
messengers
Exert powerful and specific actions inthe body
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Mechanisms of Drug Action
Agonist drugs bind to a particularreceptor and trigger the same cellular
response as the bodys own chemical
messenger Antagonist drugs compete to block the
action of the endogenous messenger
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Mechanisms of Drug Action
Some drugs produce their effects by
embedding themselves in cellmembranes
Cell membranes made up mostly of
lipids, which repel water
Effectiveness of these drugs is
related to their lipid solubility
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Mechanisms of Drug Action
Some drugs combine with specificmolecules in the body such as enzymes,transport proteins, and nucleic acids
Example: some antidepressants Some drugs act without any direct
interaction within the cell
Example: Mannitol interferes osmotically with
water reabsorption by the kidneys
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Pharmacokinetics
Activity of a drug within the body over a
period of time
Includes ADME: absorption, distribution,metabolism, and excretion of a drug
Also includes the metabolites of a drug inrelation to the time they are in the body
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Absorption,
Distribution,
Metabolism,
and Excretion
of a Drug
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AbsorptionProcess of movement of a drug from
the site of application into the
extracellular compartment of thebody
Rate of absorption affects duration andintensity of drug action
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Distribution Rate of distribution is determined by the
physicochemical characteristics of the drug,
cardiac output and blood flow.
Drug Reservoirs
Plasma Protein and other extracellular
reservoirs
Cellular reservoirs
Fat
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ADME
Absorption: process whereby a drugenters the circulatory system
Distribution: process by which adrug moves from the blood into other
body fluids and tissues and to its
sites of action
Blood flow is rate-limiting factor
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ADME
Metabolism: process by which drugs arechemically converted to compounds and
then excreted through metabolic pathways
Metabolite is substance into which a drug isconverted by metabolism
Induction: drugs enhance drug metabolism
Inhibition: drugs decrease drug metabolism
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ADME
Elimination: removal of a drug or itsmetabolites from the body
Clearance is the rate at which a drugis eliminated from a specific volume
of blood per unit of time
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Excretion / Elimination
- More polar, less lipid soluble
compounds are more easily eliminated
- Kidney, GIT, Breast milk, Pulmonary
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DiscussionWhat are the primary sites of
elimination in the body?
The kidneys and the liver, but can also
be exhaled by the lungs or excreted in
perspiration.
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Pharmacokinetic Parameters
Pharmacokinetic processes determine
how a drug should be administered to
obtain a specific response
Treat disease state, not produce toxicity
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Dose
Quantity of drug administered at one
time
Ceiling effect is a point at which no
clinical response occurs with
increased dosage
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Dose Response Curve
D t i i H th B d
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Determining How the Body
Handles a Drug
Testing of fluids over timedemonstrates how the body handles
a drug Trough is lowest level of drug in blood
Peak is highest level of drug in blood
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BioavailabilityProportion of the drug that reaches the
systemic circulation after a particular
route of administration
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Bioavailability
Portion of dose that becomes biologically
active in the body
Oral drugs go into intestinal wall, liver,
blood, and then to systemic site
Metabolism in the liver before a drug
reaches systemic circulation is first-passeffect
Fi P Eff
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First Pass Effect
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Therapeutic Range
Optimum dosage that provides best
chance for successful drug therapy
When the amount of drug givesdesired response, drug is at
therapeutic level
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Therapeutic Range
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Duration of Action
Length of time a drug gives the
desired response or is at therapeutic
level
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Duration of Action
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DiscussionHow is a drugs volume of distribution,
clearance, and half-life used in dosingdrugs?
Volume of distribution is important forcalculating the loading dose, clearance forcalculating the maintenance dose, and
half-life for determining the dosing interval.
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Drug Effects
Beneficial Responses
Therapeutic Effect: action for whichthe drug is prescribed
Local Effect: confined to a specific partof the body
Systemic Effect: generalized, all-
inclusive effect on entire body
Prescribers Considerations
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Prescriber s Considerations
When Selecting a Drug
Indications: the diseases, symptoms,and conditions for which the drug is
known to be of benefit
Contraindications: the diseases,symptoms, and conditions for which the
drug will not be beneficial and may do
harm
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Side Effects
Secondary responses to a drug other
than the primary therapeutic effect for
which the drug was intended
Allergic responses
Drug dependence, addiction,
abuse, and tolerance
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Drug Interactions
One drug can have an effect on the
action of another
Foods and other substances such as
alcohol and nicotine can interact withdrugs
Common way a substance can interact
is by inducing or inhibiting enzymes thatmetabolize the drug
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Common Drug Relationships
Addition The combined effect of twodrugs equals the sum of
the effects of each drug
taken alone.
Antagonism The action of one drugnegates the action of a
second drug.
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Common Drug Relationships
Potentiation An effect that occurs when a drugincreases or prolongs the action
of another drug, and the total
effect is greater than the sum ofthe effects of each drug used
alone.
Synergism Joint action of drugs in which
their combined effect is moreintense or longer in duration than
the sum of their individual effects.
Factors that Modify Drug
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Factors that Modify DrugEffects and Drug Dosage
Medication errors and patientcompliance
Placebo effects
Body weight and volume distribution
Age
F t th t M dif D
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Factors that Modify DrugEffects and Drug Dosage
Gender
Route of administration
Time of administration Rate of elimination
Tolerance
Factors that Modify Drug
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Factors that Modify DrugEffects and Drug Dosage
Physiologic variables
Pathologic factors
Genetic factors Drug interactions