Drug Action Flashcards
Absorption
movement of drug particles from the GI tract to the body fluids by passive absorption, active absorption, or pinocytosis
most oral drugs are absorbed…
into the surface area of the small intestine through the action of the extensive mucosal villi
What happens to absorption if the villi decreases?
Absorption decreases because of disease, drug, effect or the removal of the small intestine
What happens to protein-based drugs in the small intestine?
they are destroyed by digestive enzymes
passive absorption
-occurs mostly by diffusion -does not require energy to move across the membrane
diffusion
movement from high concentration to lower concentration
active absorption
-requires a carrier as an enzyme or protein to move the drug against the concentration gradient -energy required
pinocytosis
process by which cells carry a drug across the membrane by engulfing the drug particles
GI membrane is composed of…
mostly lipid (fat) and protein
Drugs that are __________ pass rapidly through the GI membrane
lipid-soluble
________ need a carrier to pass through the membrane
water-soluble
Large particles pass through cell membrane if…
they are nonionized
nonionized
no positive or negative charge
weak acid drugs are..
less ionized in the stomach and they pass through the stomach lining easily and rapidly
an infant’s GI secretions are..
higher pH (alkaline) than those of adults
drugs that are _____ and _______ are absorbed faster than _______ and ________
-lipid-soluble, nonionized -water-soluble, ionized
What can affect drug absorption?
-blood flow -pain -stress -hunger -fasting -food -pH
Poor circulation to the stomach…
hampers absorption
What could cause poor circulation to the stomach?
result of shock, vasoconstrictor drugs, or disease
What could cause slow gastric emptying time?
-pain -stress -foods that are solid, hot, or high in fat
What is bad about a slow gastric emptying time when it comes to medication?
drug remains in stomach longer
exercise can…..
decrease blood flow by causing more blood to flow to the peripheral muscle, thereby decreasing blood circulation to the GI tract
Drugs given IM…
are absorbed faster than subQ due to there being more blood vessels in the muscle
Drugs are absorbed faster in the deltoid due to…
very vascular
Some drugs do not go directly into the systemic circulation following oral absorption….
they pass from the intestinal lumen to the liver via the portal vein
In the liver, what happens to drugs?
first-pass effect
first-pass effect
process in which the drug passes to the liver first
- drug is metabolized to inactive form that may be excreted, thus reducing the amount of active drug
- do not undergo any metabolism
- drug is metabolized to drug metabolite, which may be equally or more active than the original drug
most drugs given orally are…
affected by first-pass metabolism
bioavailability
-subcategory of absorption -% of drug administered that reaches the systemic circulation
for oral route, bioavailability…
occurs after absorption and first-pass metabolism
The % of bioavailability for the oral route is…
always less than 100%
The % of bioavailability for the IV route is…
100%
Oral drugs that have a high first-pass metabolism…
may have availability of only 20% to 40% on entering systemic circulation
To obtain the best drug effect, oral dose could be…
higher than the drug dose for IV use
Factors that alter bioavailability
- drug form 2. route 3. GI mucosa and motility 4. food and other drugs 5. changes in liver metabolism caused by liver dysfunction or inadequate hepatic blood flow
decreased liver function or decreased hepatic blood flow….
leads to increased bioavailability of a drug, but only if the drug is metabolized by the liver -less drug is destroyed by the hepatic metabolism in the presence of liver disorder
With some oral drugs, rapid absorption…
increases the bioavailability of the drug and can cause an increase in drug concentration -drug toxicity may result
slow absorption can…
limit the bioavailability of the drug, thus causing a decrease in drug serum concentration
Distribution
process by which the drug becomes available to body fluids and body tissues
Distribution is influenced by..
-blood flow -drug’s affinity to the tissue -protein-binding effect
protein-binding effect
as drugs are distributed in the plasma, many are bound to varying degrees with protein
Vd
Volume of drug distribution -dependent on drug dose and its concentration in the body
drugs with larger volume of drug distribution….
have a longer half-life and stay in the body longer
>89% bound to protein
highly protein-bound drugs
61%-89% bound to protein
moderately highly protein-bound drugs
30%-60% bound to protein
moderately protein-bound drugs
free active drug
-drugs not bound to protein -active and can cause a pharmacologic response
the portion of the drug that is bound to protein is…
inactive and not available to receptors
as the free active drug decreases over time…
more bound drug is released from the protein to maintain the balance of free drug
bound drugs cannot…
leave systemic circulation to get to site of action
When two highly protein-bound drugs are given concurrently…
they compete for protein-binding sites, thus causing more free drug to be released into circulation
What could result from two highly protein-bound drugs given at the same time?
drug accumulation and possible drug toxicity
low serum protein level decreases…
the number of protein-binding sites
low number of protein-binding sites can cause…
increase in the amount of free drug in the plasma and drug toxicity may result
drug is dosed and prescribed according to…
the % in which the drug binds to protein
Who would have low serum albumin levels?
-patients with liver or kidney dz -malnourished patients
Who is more likely to have hypoalbuminemia?
OAs
with some health conditions that result in low serum protein levels….
excess free or unbound drug goes to nonspecific tissue binding sites until needed -excess free drug in the circulation does not occur
To avoid possible drug toxicity, checking the…
protein-binding % of all drugs administered to a patient is important
RN should check pt’s plasma protein and albumin levels because…
a decrease in plasma protein (albumin) decreases the available protein-binding sites, permitting more free drug in the circulation -could be life threatening based on drug
What hinders drug distribution?
-abscesses -exudates -body glands -tumors
_______ do not distribute well at abscess and exudate sites
antibiotics
some drugs accumulate in particular tissues such as…
-fat -bone -liver -muscle -eye tissues
BBB
blood brain barrier -semipermeable membrane in the CNS that protects the brain from foreign substances
____________ drugs are able to cross the BBB
highly lipid-soluble
What type are drugs are not able to cross the BBB?
-drugs not bound to proteins -drugs that are not lipid-soluble
What is made difficult by drugs not being able to cross the BBB?
it is difficult to distribute the drug
During pregnancy, what type of drugs are able to cross the placental barrier?
both lipid-soluble and lipid-insoluble drugs -can affect both fetus and mother
What is considered before administering drugs to pregnant mothers?
risk-benefit ratio