Professional Documents
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PHARMACOLOGY
Prepared By: Cristina Benito
LEARNING OUTCOMES:
2. Outline the steps involved in developing ad approving a new drug in the United
States.
3. Differentiate between generic and brand-name drugs and over -the-counter and
prescription drugs.
4. Describe how body cells respond to the presence of drugs that are capable of
Advantages:
Quality can be controlled
Process is easier and cheaper
More potent and safer
Large scale production
SYNTHETIC DRUGS
AMOXICILLIN
MARIJUANA (cannabis)
Active ingredient delta-9-tetra hydrocannabinol
Drug Names
STAGES OF DEVELOPMENT:
a.) Preclinical Trials:
Subject: Animals: Safety, toxicity, pharmacokinetics, and metabolism of
the new chemical.
FDA: reviews extensive animal studies and data on the safety and
effectiveness of the proposed drugs.
Chemicals that may have therapeutic value are tested on laboratory
animals for two main purposes:
1. determine whether they have the presumed effects in living tissue
2. evaluate any adverse effects
FDA approves an application for an Investigational New Drug (IND)
Preclinical Trials
At the end of the preclinical trials, some chemicals are discarded for the
following reasons:
a. the chemical lacks the therapeutic activity when used with living
animals.
b. the chemical is too toxic to living animals to be worth the risk of
developing into a drug.
c. the chemical is highly teratogenic
d. the safety margins are so small that the chemical would not be useful
in the clinical setting.
Stages of Development
b.) Phase I Studies:
Uses human volunteers to test the drugs (20-80)
These studies are more tightly controlled than preclinical trials
Performed by specially trained clinical investigators
Some chemicals are therapeutic in animals but have no effects in
humans
Investigators scrutinize the drugs being tested for effects in humans
> Toxicity and adverse effects
Phase I Studies
At the end of phase I studies, many chemicals are dropped from the
process for the following reasons:
I. Absorption: the transfer of a drug from its site of administration to the blood
stream.
>Mechanisms of
absorption
* Passive diffusion: A drug moves from an area of higher concentration to one of
lower concentration.
> requires no cellular energy
* Active Transport: A drug moves from an area of lower concentration to one of
higher concentration.
> requires cellular energy
> is used to absorbed electrolytes like sodium and potassium and some drugs
like Levodopa
FACTORS AFFECTING RATE OF DRUG
ABSORPTION
1. Route of Administration
a. Oral
b. Intravenous
2. Dosage/ Concentration: Increase in the concentration of the chemical
there is also an increase in the rate of diffusion
3. Lipid-Solubility: A drug needs to be lipid soluble to penetrate
membrane.
Factors Affecting Absorption
4 Steps in Pharmacokinetics
II. Distribution: Process that allows drug delivery to tissues and fluid of the
body
Factors affecting drug distribution:
a. Blood Flow
Drug is distributed rapidly to organs with a large blood supply.
It is distributed more gradually to other internal organs, skin, fat and
muscle.
Example: A diabetic client with lower leg infection and patient with
peripheral arterial disease (Raynaud Syndrome)
b. Drug Solubility
> a lipid soluble drug can cross the cell membrane more quickly than water
soluble drugs can.
FACTORS AFFECTING DRUG DISTRIBUTION
c. Protein-Binding Capability: refers to the degree to which medications
attach to proteins within the blood.
Some drugs are tightly bound and are released very slowly thus they
have a very long duration of action because they are not free to be
broken down or excreted
Drugs that are loosely bound tend to act quickly and be excreted
quickly.
FACTORS AFFECTING DRUG DISTRIBUTION
d. Blood-Brain Barrier: A protective system of cellular activity that keeps
many things away from the CNS.
• Drugs that are highly lipid soluble are more likely to pass through the
blood-brain barrier and reach the CNS
• Drugs that are not lipid soluble are not able to pass the blood-brain
barrier.
FACTORS AFFECTING DRUG DISTRIBUTION
e. Placenta and Breast Milk:
> Many drugs readily pass through the placenta and affect the
developing fetes in pregnant mother
4 Steps in Pharmacokinetics
III. Metabolism/Biotransformation:
It alters a drug to a more active or less active form
Helps convert the drug to a more water soluble form, facilitating
excretion
Primary Site for drug metabolism: Liver
First pass effect
Factors Affecting Metabolism:
Drugs that induced enzyme activity
Drugs that inhibit enzyme activity
Disease, such as cirrhosis and heart failure
4 Steps in Pharmacology
IV. Excretion: Elimination of drugs from the body
Routes Of Excretion:
Kidneys via urine
Liver via bile and into feces
Lungs via exhaled air
Saliva, sweat, and tears
Processes by which a drug is handled by the
Body
ONSET, PEAK, AND DURATION
Onset of Action: refers to the time period from a drug’s
administration to the beginning of its therapeutic
effect.
Peak Level: occurs when the body absorbs more
drug, the level rises in the blood, and more drug
reaches the site of action.
Duration of Action: the length of time a drug produces
therapeutic effects.
HALF- LIFE
The time needed for the total amount of a drug in the body to decrease
by 50%