Week 2 Flashcards
Pharmacokinetics?
faar·muh·kow·kuh·neh·tuhks
Absorption, distribution, metabolism and elimination of drugs
–”What the body does to the drug”
-How moving into the body
Pharmaceutics?
faar·muh·soo·tuhks
preparing drugs for administration
“Dosage Forms”
Pharmacodynamics?
Action or effects of drugs on living systems
“What the drug does to the body”
Levels of Drug Activity? 4
Body Systems
Component Tissues
Cellular Level
Molecular Level
Drugs modify existing functions
What are they? 3
Interrupt
-ipratropium/slow down mucus membrane
Replace
-Fe for anemia
-insulin
Potentiate
-Cathartics before sigmoidoscopy
Beta-Blockers
a) Body Systems
b) Component Tissues
c) Cellular Level
d) Molecular Level
a) Reduces pulse rate
b) Negative chronotrope
c) Prevents elevation of cAMP
d) Competitive antagonism of norepinephrine to cardiac beta1 receptors
Agonist?
Activates!!
A drug interact with a receptor and fully activate it.
Intrinsic activity equals 1
Partial Agonism
A drug interact with a receptor and partially activate it
Intrinsic activity between 0(0%) and 1(100%)
Antagonism?
A drug binds a receptor and prevents a response from occuring
Blocking receptor to being fully stimulate
Competitive Antagonism?
Agonist and antagonist both trying to bind to the same receptor
Noncompetitive Antagonism?
Binding of an antagonist to one receptor prevents an agonist from bind to another receptor
Eternal administration
Mouth
Thin lining, rich blood supply
Sublingual and buccal routes
Eternal administration
Stomach
Medium surface area, rich blood supply
Acidic pH
Drugs don’t stay long
Eternal administration
Small Intestine
Hugh surface area
Rich blood supply
Basic pH
Parenteral Administration
Advantages
Can be used for drugs that are poorly absorbed
Can provide an immediate onset of action (IV)
Can provide a longer lasting effect (IM/SQ)
Can concentrate drug at a specific location
Can provide a more predictable response
Can provide titratable dosage
Parenteral Administration
Disadvantages
Pain
Irreversible
Extravasation 血管外漏出
Phlebitis 静脈炎
Not useful for self-administration
Contamination/infection
Parenteral Administration 7
Intravenous into a vein
Intra-arterial into a artery
Intramuscular into the muscle
Epidural epidural space
Intrathecal into the CSF
Subcutaneous into the sab layer of the skin
Intra-articular Joint
Topical Administration
Skin
Ointments, creams, patches
Local and systemic
Topical Administration
a) Eyes
b) Ears
c) Intranasal
a)Drops, ointments
Local distribution
b)Local distribution
c)Spray and drops
Local and systemic
Topical Administration
a) Inhalation
b) Vaginal
a) Local and systemic
b) Local and systemic
Oral Dosage Forms 8
Dissolved Liquid (elixir, syrup)
Suspensions
Powders
Capsules
Tablets
Coated Tablets
Enteric-Coating
Sustained-Release
Pharmacokinetic Phase
Absorption
Movement of drug molecules into the body
Passive: high to low
Facilitated diffusion: solutes through transport proteins in the plasma membrane.
Pharmacokinetic Phase
Rate of absorption can determine?
Onset of action
Duration of action
Intensity of response
Variables Affecting Absorption 4
Nature of absorbing surface
Surface area/small vs. large
Blood flow to site of administration
pH at the site of absorption
Name 3 ways that drug interactions can occur as a result of altered absorption.
Complexation
pH change
GI motility change
What is enzyme induction?
Certain drugs capable of increasing metabolic enzymes in the liver
What is enzyme inhibition?
A number of drugs are capable of decreasing the activity of cytochrome P450 enzymes
Place either enzyme induction or inhibition
a. Happens slowly
b. Results in toxicity
c. Increases amount of enzyme
d. Happens quickly
e. Causes ineffective treatment
f. Most common way a serious DI can occur
a) induction
a,c,e
b) inhibition
b,d,f
Mechanism of altered absorption
Complexation
Bile acid resins
OTC+ prescription drug
Drug that from chemical complexes with other drug
lower the rate of drug absorption
"Take meds at different time!"
Mechanism of altered absorption
Change in pH
Most drug likes basic pH environment
If the drug change the pH, not absorb as suppose to be
Poop out then drug is not working
Mechanism of altered absorption
GI motility
Slowing motility
= increase absorption time
Speeding motility
=decrease absorption time
Problem with sustains-release meds
CYP2D6 is including what enzyme?
Cytochrome P-450
genetic enzyme
someone has a lots, someone has a little
Factors affecting drug metabolism
Age
neonate, premature baby
-not developed organs
-not have specific enzyme to metabolize
Elderly
-life experience(smoke, drinking)
-decease body function (liver, kidney)
Factors affecting drug metabolism
disease states
Hepatic cancer etc
OIs drug clear by liver?
overdose danger!
Factors affecting drug metabolism
pregnancy
Placenta has a lot of enzyme
smoke causes to produce more enzyme
After delivered placenta, need to adjust dosage
Enzyme induction
Active drug to inactive drug
Make more enzyme=decrease drug work
Onset 5days,max eff 2weeks (slowly work)
Offset 2-3 weeks
Enzyme inhibition
Increase plasma concentration
=stop breaking drugs
=more drug action
Onset reach max in 24 hours
Offset within 24h hours
Result toxicity
Pharmacodynamic interaction
Drug A increase HR
Drug B decrease HR
Antagonistic
Change nothing
Cancel out
Pharmacodynamic interaction
Taking lower BP med, 2 days later taking another lower BP med to have greater result
Synergistic/Additive Therapeutic Effect
Pharmacodynamic interaction
Taking a CNS drug and starts taking another drug also causes CNS depression
Synergistic/Advance Effects