Solid Forms:
PILLS drugs shaped spherically to - Tolerance for a drug that develops after
be swallowed
POWDERS not as popular as they
once were
TABLETS powders compressed
into disk-like form.
SUPPOSITORIES drugs mixed
with a wax-like base that melts at
body temp.
CAPSULES Gelatin containers
filled with powders or tiny pills
Liquid Forms
SOLUTIONS water/ oil based
TINCTURES prepared using an
alcohol extraction process
SUSPENSIONS preparation in
which the solid does not dissolve in
the solvent.
EMULSIONS suspensions with an
oily substance in the solvent
SPIRITS - solution of an volatile
drug in alcohol
ELIXIRS alcohol and water
solvent ; often with flavoring
SYRUP sugar, water and drug
solutions.
Action of Drugs:
- Bind to a receptor site
- Change physical properties
- Chemically combine with other substances
after a normal metabolic pathway
Responses to Drug Administration:
SIDE EFFECTS
-Unintended respond to a drug
ALLERGIC REACTION
- Hypersensitivity
IDIOSYNCRASY
- Drug effect unique to an individual
TOLERANCE
- Decreased response to the same amount
CROSS TOLERANCE
administration of a diff. drug
TACHYPHYLAXIS
- Rapidly occurring tolerance to a drug
CUMULATIVE DRUG
- Increased effectiveness when a drug is
given in several doses.
DRUG DEPENDENCE
- Patient becomes accustomed to the drugs
presence in his body.
DRUG INTERACTION
- Effects of one drug alter the response to
another drug.
DRUG ANTAGONISM
- Effects of one drug block the response to
another drug
SUMMATION
- Also known as additive effect, two drugs
withsame effect are given together similar to
1+1=2
SYNERGISM two drugs with the same
effect are given together and produce a
response greater than the sum of their
individual responses
- Similar to 1 + 1 = 3
POTENTIATION one drug enhances the
effect of another
INTERFERENCE - the direct biochemical
interaction between two drugs; one drug
affect, the pharmacology of another drug
Factors affecting Drug Response
- Age
- Body Mass
- Sex
- Environment
Time of Administration
- Pathology
- Genetics
- Psychology
Drug Names
Chemical Name drugs chemical
composition and molecular structure
Generic Name name given by the United (Search sa net ang ADMET)
States Adopted Name Council Drug R&D discovery and development
-Allows the drug to be marketed phase
Brand name also called trade name 10-15 years to develop a new medicine
(proprietary name) Likelihood of success: 10%
- drug has a registered trademark; use of the Cost $800 Million- $1 Billion Dollars (US)
name is restricted by the drugs owner
(usually the manufacturer)
- allows the drug to be commercially
distributed
- the superscript R is registered by the U.S.
Patent Office and approved by the FDA
DRUG NAMES : example
Chemical name
(+/-)-2-(p-isobutylphenyl) propionic
acid
Importance of PK studies:
US Drug Legislation
patients may suffer
1970: Comprehensive drug abuse
Toxic drugs may accumulate
Prevention and Control Act
Useful drugs may have no benefit
- Also known as controlled subs, act:
because doses are too small to
Classifies drugs according to their abuse
establish therapy.
potential
- Regulates the manufacture and distance of A drug can be rapidly metabolized
drugs causing dependence Routes of Administration
Parenteral and Enteral
Philippine Drug Legislation
ABSORPTION
-The comprehensive dangerous drugs act of
-the process by which drug proceeds from
2002
the site of administration to the site of
- Republic act no. 9165 enacted on June 7,
measurement( blood stream) within the
2002
body.
Republic Act No. 8203
-Necessary for the production of a
- An act of prohibiting counterfeit drugs
therapeutic effects.
enacted on July 22, 1996
-Most drugs undergo gastrointestinal
Pharmacokinetics absorption.
-Study of the disposition of a drug This is extent to which drug is absorbed
-The disposition of a drug includes the from gut lumen into portal circulation.
processes of -Exception: IV Drug
ADMET IV Drugs
-Absorption -immediately(dose)
-Distribution -Completely
-Metabolism Oral Drug
-Excretion -delayed(dose)
-Toxicity -incomplete
The Process -Physiological volumes
Absorption relies on All of the fluid in the body(referred to as the
-Passage through membranes to reach the total body water), in which a drug can be
blood dissolved, can be roughly divided onto three
-Passive diffusion of lipid soluble species. compartments:
The Rule of Five Formulation Intravascular (Blood plasma found within
-Poor absorption or permeation are more blood vessels)
likely when: Interstitial (fluid surrounding the cell)
There are more than 5 H-bond Intercellular (fluid within the cell)
donors The distribution of a drug into these
The molecular weight is over 500 compartments is dictated by its physical
The LogP is over 5 and chemical properties.
There are more than 10 H-Bond
acceptors. VASCULAR
-3L
ABSORPTION AND IONIZATION
-4% BW
-non-ionized drug
-more lipid soluble drug EXTRAVASCULAR
-Diffuse across cell membranes more easily. -9L
-13% BW
Determination of bio-availability
- A drug given by the intravenous route will INTRACELLULAR
have an absolute bio-availability of 1 -28L
(F=1 or 100% bio-availability) -41% BW
-While drugs given by other routes usually Volume Distribution
-apparent volume of distribution
have an absolute bio-availability of less
(Vd)=
than one
-amount of drug in the body divided by
-The absolute bio-availability in the area
plasma drug concentration (vascular)
under curve (AUC) non-intravenous
divided by AUC intravenous -volume of distribution for some drugs
-Drug Vd(L)
TOXICITY
The therapeutic index is the degree of -Cocaine 140
separation between toxic and therapeutic -Clonazepam 210
doses. -Amitriptyline 1050
-Relationship between dose, therapeutic -Amiodarone -5000
effect and toxic effect. The therapeutic index
Factors affecting Drug VD
is narrow for most cancer drugs.
Blood flow
Distribution
-rate varies widely as function of
-The movement of drug from the blood to
and from the tissues. tissue
Determined by: Muscle: slow Organs:fast
-Partitioning across various membranes Capillary Structure
-Binding to tissue components -most capillaries are leaky and do not
-Binding to blood components (RBC, impede diffusion of drugs.
Plasma protein)
-Blood-brain barrier formed by high level of
tight junction between cells
-Blood Brain Barrier is impermeable to most
water-soluble drugs
Blood Brain Barrier
-distribution by osmotic means
-Use of endogenous transport systems
-Blocking of active efflux transporters
-inter-cerebral implantation
-Etc
Plasma Protein Binding
-manu drugs bind to plasma proteins in the
blood stream
-Plasma protein binding limits distribution
-A drug that binds plasma protein diffuses
less efficiently, than a drug that doesnt