Term
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Definition
ANY biologically active compound that affects processes of living tissues |
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Term
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Definition
Biomedical science concerned with interactions of chemicals (drugs) with living materials |
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Term
What is Pharmacokinetics? |
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Definition
actions of the BODY on the DRUG
processes that determine the concentration of drugs in the body fluids and tissues over time |
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Term
How is pharmacokinetics broken down? |
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Definition
Drug absorption
distribution
biotransforamtion
excretion |
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Term
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Definition
how drug absorbed from the site of administration or indirectly into plasma
(injection, skin, oral) |
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Term
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Definition
distribute into the interstitial and intracellular fluids
(throughout the body to the target) |
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Term
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Definition
metabolism of the drug by the liver, kidneys, or other tissues |
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Term
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Definition
he drug and its metabolites are removed from the body in the urine, bile, or feces (sweat as well) |
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Term
What is pharmacodynamics? |
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Definition
Actions of the DRUG on the BODY
Biochemical mechanisms:
receptors and signal transduction
Dose-response relationships:
Potency and Efficacy |
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Term
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Definition
receptors
signal transduction |
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Term
Dose-response relationships |
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Definition
Potency (concentration-related)
Efficacy (response-related) |
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Term
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Definition
application of drugs in Prevention, Cure, Alleviation, Treatment, or Diagnosis of disease
business end of pham |
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Term
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Definition
To PREVENT development of diseases |
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Term
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Definition
Treatment of diseases caused by parasitic or invading organisms
only situation in which give drug to kill off and destroy an organism or cancer |
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Term
What types of nomenclature are used to name drugs? |
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Definition
Chemical name
generic- used for class
Non-proprietary
official
proprietary
brand |
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Term
Why aren't proprietary (brand/trade) names used in class?
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Definition
existence of multiple names and gets confusing although may provide clues to the therapeutic action/ classification |
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Term
What is a tablet and capsule? |
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Definition
Tablet- packed
Capsule- usually in gelatin caplet that dissolves usually faster than a thick compressed tablet
different rates of disintegration and dissolution may cause differences in bioavalability of drugs from different tablet formulations
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Term
What are different characteristics of tablets and capsules? |
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Definition
enteric coating- coating to protect the stomach from the drug until it passes through or to keep the drug from being dissolved until it reaches the desired location
Sustained relaese (SR) or extended release (XR):
Controlled diffusion
controlled dissolution
osmotic pressure |
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Term
What are solutions and suspensions? |
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Definition
the most common liquid pharmaceutical preparations
faster absorption than a tablet or capsule and is directly absorbed
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Term
What are the uses for solutions and suspensions? |
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Definition
oral
parenteral- other than enteral ( injection, topical, drops in eye, etc) |
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Term
What are some preperations of solutions and suspensions? |
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Definition
elixirs- contain alcohol used to dissolve the drug
syrups- contain sugar to make the drug more palatable
sterile solutions |
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Term
What are some other preparations of drugs? |
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Definition
skin patches- (nicotine, hormones) drug must be available for absorption through the skin parentral
aerosols- topical (sunscreen) inhaled (asthma)
ointments, creams, lotions- more messy than skin patch
suppositories- rectal |
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Term
What is important to consider when testing drugs? |
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Definition
Risk/Benefit ratio
what are the benefits versus what are the risks |
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Term
How many phases are there in drug trials? |
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Definition
There are 4 phases
1) test on young normal males
2) test on diseased people well into disease state
3) if drug effective test again to make sure then released by FDA
4) post-marketing given out by docs and then company collects adverse rxn information to make sure drug still safe or pulled off the market |
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Term
How many patients are needed to indicate a significant adverse response? |
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Definition
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Term
What does DSHEA stand for and what is the definition? |
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Definition
Dietary supplement health and education act of 1994
Not intended for the diagnosis, prevention, treatment, or cure of any disease.
no regulations or studies must be done before the drug is put on the market |
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Term
What factors should be considered when selecting a drug? |
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Definition
each patient is differnt
therapy may be initiated without all the data
patient status may change
patient on multiple drugs |
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Term
When a drug is administered where must it be moved into for passage throughout the body?
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Definition
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Term
Enteral, Parenteral, and other are what? |
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Definition
routes of drug administration |
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Term
What are examples of Enteral drug administration? |
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Definition
oral
sublingual- under the tongue
buccal- between cheeks and gums
rectal |
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Term
what are the different types of Parenteral drug administration? |
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Definition
intravascular- IV
intramuscular- IM
subcutaneous- SC |
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Term
What are other types of drug administration? |
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Definition
inhalation
inranasal
intrathecal- into the brain
intraventricular- into the ventricles of the brain
topical
transdermal |
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Term
What is the most common and variable enteral route of administration? |
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Definition
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Term
Why is oral the most variable? |
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Definition
interaction with food and gastric acid
food slows gastric emptying (less absorption)
intestinal transit- food, illness, blunt trauma
metabolism by the liver(first-pass) or gut enzymes/flora
physico-chemical properties of drug perparation
stomach v. duodenum- increased surface area and absorption in small intestine
can't use in comatose, sedated, or nauseous patients |
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Term
Absorption into the venous capillary network which drains into superior vena cava is an advantage of sublingual and buccal because______ |
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Definition
bypasses GI tract and first-pass liver metabolism
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Term
What are some drawbacks to sublingual and buccal administration? |
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Definition
requires low doses
requires good solubility in water and lipid |
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Term
How is rectal medication prepared? |
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Definition
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Term
When is a suppository most useful? |
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Definition
in children or in vomiting unconcsious patients |
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Term
Approximately what percentage of the drug that is absorbed by the rectum will bypass the liver? |
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Definition
50% which reduces the influence of first-pass hepatic metabolism |
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Term
What is a disadvantage of rectal administration? |
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Definition
often irregular, incomplete, and can cause irritation |
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Term
What are the main reasons for using Parenteral administration? |
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Definition
drugs that are poorly absorbed in he GI
for unconscious or uncooperative patients
more rapid onset |
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Term
What is the most common method of parenteral administration? |
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Definition
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Term
What are the advantages of IV administration? |
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Definition
absorption instantaneous
mainly for drugs in aqueous solutions or drugs not absorbed orally
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Term
What are the disadvantages of IV? |
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Definition
cannot be recalled
chance of air emboli- gets stuck in the lungs causing pulmonary embolism
sepsis
dependent upon patient accessible veins |
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Term
Which type of parenteral admin is appropriate for aqueous or suspensions? |
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Definition
SC
suspension- not dissolved and part of the solution but remains in solid state
aqueous- dissolved in solution
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Term
What type of parenteral admin provides slow and constant absorption and can be combined with vasoconstrictor to slow absorption? |
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Definition
SC
small pellet can also be implanted under the skin |
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Term
What type of parenteral admin is similar to subcu but provides a greater depot |
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Definition
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Term
IM absorption depends on? |
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Definition
blood flow to the muscle
exercise increases blood flow |
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Term
Why is it necessary to use Intrathecal admin? |
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Definition
blood brain barrier and blood CSF barrier impede entrance into the CNS
used to infections and tumor treatment |
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Term
Why is inhalation a good method for drug admin? |
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Definition
absorbed by the lungs which have large surface area for absorption which reaches the blood supply quickly and avoids first-pass metabolism
need to worry less about systemic effect and more about local effect |
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Term
What is the second fastest route for drug admin? |
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Definition
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Term
What is a disadvantage of inhalation? |
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Definition
site of entry for toxins and allergens |
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Term
What are some advantages of topical application? |
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Definition
local effect desired
direct application and no need for needles
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Term
What are some routes for topical admin? |
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Definition
skin
eye
nasal
throat
vagina
urethra |
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Term
What are some disadvantages of topical application? |
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Definition
few drugs penetrate the skin
absorption proportional to surface area
condition of the skin affects absorption
inflammation increases cutaneous blood flow and absorption
enhanced by suspension in oily vehicle and rubbing into skin |
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Term
What factors influence absorption? |
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Definition
phyisco-chemical properties of the barrier
- passive, facilitated, or active diffusion
physical properties of the system
- blood flow, surface area, contact time
physio-chemical properites of the drug
- molecular size, lipid solubility, ionization
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Term
Do smaller or larger molecules diffuse more readily |
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Definition
smaller <200 MW
not applicable to facilitated diffusion, active transport, or endocytosis |
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Term
The____ the partition coefficient, the______ the lipid-solubility of the drug, and the greater its diffusion across the membrane |
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Definition
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Term
Most drugs are small_______ ________ |
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Definition
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Term
Membranes are much more permeable to what type of ion? |
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Definition
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Term
The fraction of drug that is non-ionized depends on its? |
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Definition
chemical nature, pKa, and pH |
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Term
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Definition
that pH at which there is a 50/50 ratio of unionized to ionized |
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Term
The pKa is solely dependent upon the chemical nature of? |
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Definition
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Term
A drug that carries an extra electron so it will always be (-) charged when not bound to an H ion is a (n)? |
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Definition
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Term
A drug that carries a (+) charge because it is missing an electron when bound to an H ion is a(n)? |
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Definition
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Term
_____ are increasingly ionized with increasing pH (basic environment) |
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Definition
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Term
_______ are increasingly ionized with decreasing pH (acidic env) |
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Definition
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Term
Where would someone look if wanted to determine if there was an overdose on a weak acid? |
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Definition
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Term
Where would someone look if wanted to determine if a person overdosed on a weak base? |
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Definition
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Term
What is the Henderson-Hasselbalch equation? |
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Definition
log (protonated) / (unprotonated) = pKa - pH |
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Term
the protonated for (HA) will ALWAYS predominate (be reabsorbed) when? |
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Definition
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Term
the unprotonated for (A-) will ALWAYS predominate (trapped) when? |
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Definition
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Term
if protonated form (BH+) will ALWAYS predominate |
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Definition
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Term
uprotonated form (B) will ALWAYS predominate |
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Definition
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Term
The fraction of administered drug that reaches systemic circulation is? |
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Definition
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Term
What factors influence drug bioavailability? |
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Definition
solubility of drug
chemical instability
formulation
first-pass hepatic metabolism |
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Term
When drugs are pharmaceutical equivalents, contain the same active ingredients and are identical in dose, dosage form, and route of admin they are considered to be? |
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Definition
bioequivalent
only exists if the rates and extent of bioavailability of their active ingredients are not significantly different |
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Term
What is therapeutic equivalence? |
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Definition
when 2 drugs are similar if they have comparable efficacy and safety |
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