Professional Documents
Culture Documents
● Absorption
INTRODUCTION TO PHARMACOLOGY ● Distribution
● Metabolism / Biotransformation
3 Phases Of Drug When Taken By Mouth Like ● Excretion / Elimination
Tablet or Capsule: Nursing responsibilities:
Drugs in liquid form are more rapidly available 1. the movement of drug particles from the GI tract to
for GI absorption than are solids. body fluids by passive absorption, active
absorption, or pinocytosis.
Drugs are both disintegrated and absorbed
faster in acidic fluids with a pH of 1 or 2. 2. Most oral drugs are absorbed into the surface
area of the small intestine through the action of the
(Alkaline drugs would become ionized and extensive mucosal villi.
have difficulty crossing cell membrane
barriers.)
Mechanism of Absorption
Drug absorption is generally slower for those
A. Passive absorption occurs mostly by diffusion
drugs absorbed primarily in the stomach.
(movement from higher concentration to lower
Enteric-coated drugs resist disintegrated in the concentration)
gastric acid of the stomach, so disintegration B. Active absorption requires a carrier such as an
does not occur until the drug reaches the enzyme or protein to move the drug against a
concentration gradient. Energy is required for
alkaline environment of the small intestine.
active absorption.
o Enteric-coated tablets can remain in
C. Pinocytosis is a process by which cells carry a
the stomach for a long time; therefore, drug across their membrane by engulfing the drug
their effect may be delayed in onset. particles.
Enteric-coated tablets or capsules and
sustained-release (beaded) capsules
should not be crushed.
o Crushing would alter the place and
time of the absorption of the drug,
Food in the GI tract may interfere with the
dissolution of certain drugs.
PHARMACOKINETIC PHASE
in muscles that have more blood vessels (e.g.,deltoids) Oral drugs that have a high first-pass hepatic
metabolism may have a bioavailability of only 20%
than in those that have fewer blood vessels (e.g.,
to 40% on entering systemic circulation.
gluteals). Subcutaneous tissue has fewer blood
To obtain the desired drug effect, the oral dose could
vessels, so absorption is slower in such tissue.
be higher than the drug dose for IV use.
4. Lipid Solubility - The GI membrane is composed
mostly of lipid (fat) and protein, so drugs that are lipid
soluble pass rapidly through the GI membrane. Water-
soluble drugs need a carrier, either enzyme or protein,
to pass through the membrane. Large particles pass
through the cell membrane if they are nonionized
(have no positive or negative charge).
The process in which the drug passes to the liver first: Factors that alter bioavailability include:
• Some drugs do not go directly into the systemic (1) the drug form (e.g., tablet, capsule, sustained
circulation following oral absorption but pass from release, liquid, transdermal patch, rectal
the intestinal lumen to the liver via the portal vein. suppository, inhalation)
• In the liver, some drugs may be metabolized to an (2) route of administration (e.g., oral, rectal, topical,
inactive form that may then be excreted, thus parenteral)
reducing the amount of active drug.
(3) GI mucosa and motility
• Some drugs do not undergo metabolism at all in the
liver, and others may be metabolized to drug (4) food and other drugs, and
metabolite, which may be equally or more active
(5) changes in liver metabolism caused by liver
than the original drug
dysfunction or inadequate hepatic blood flow.
Rapid absorption - increases the bioavailability of the patient’s plasma protein and albumin levels, because a
drug and can cause an increase in drug decrease in plasma protein (albumin) decreases
concentration. Drug toxicity may result.
protein-binding sites, permitting more free drug in the
Slow absorption - can limit the bioavailability of the
circulation.
drug, thus causing a decrease in drug serum
concentration.
1. blood flow
Volume of drug distribution (Vd) is dependent on drug ➢ Abscesses, exudates, body glands, and tumors
dose and its concentration in the body. Drugs with a
hinder drug distribution. Antibiotics do not distribute
larger volume of drug distribution have a longer
well at abscess and exudate sites
half-life and stay in the body longer.
➢ some drugs accumulate in particular tissues such
Protein-binding effect- As drugs are distributed in the
as fat, bone, liver, muscle, and eye tissues.
plasma, many are bound to varying degrees
(percentages) with protein (primarily albumin).
The (blood-brain barrier (BBB) is a
semipermeable membrane in the central
nervous system (CNS) that protects the
brain from foreign substances. Highly
lipid-soluble drugs are able to cross the
BBB. Drugs that are not bound to proteins
and are not lipid soluble are not able to
cross the BBB, which makes it difficult to
distribute the drug.
During pregnancy, both lipid-soluble and
❖ The portion of the drug that is bound is inactive lipid-insoluble drugs are able to cross the
placental barrier, which can affect the
because it is not available to receptors, and the portion fetus and the mother. The risk-benefit
that remains unbound is free, active drug. ratio should be considered before drugs
are given during pregnancy
❖ Only free drugs (drugs not bound to protein) are During lactation, drugs can be secreted into
active and can cause a pharmacologic response. breast milk, which could affect the nursing
infant. The nurse needs to check which
drugs may cross into breast milk before
❖ As the free drug in the circulation decreases, more administering to a lactating patient
bound drug is released from the protein to maintain the
balance of free drug. Drugs bound to proteins cannot
leave the systemic circulation to get to the site of 3. Metabolism (or Biotransformation)
action. This is why only free drug is active.
❑ is the process by which the body inactivates or
❖ A low serum protein level decreases the number of biotransforms drugs. Drugs can be metabolized in
protein-binding sites and can cause an increase in the several organs; however, the liver is the primary site of
amount of free drug in the plasma. Drug toxicity may metabolism.
then result.
❑ Most drugs are inactivated by liver enzymes and are
❖ To avoid possible drug toxicity, checking the protein then converted or transformed by hepatic enzymes to
binding percentage of all drugs administered to a
patient is important. The nurse should also check the
inactive metabolites or water-soluble substances for ✓ breast milk
excretion.
➢The kidneys filter free unbound drugs, watersoluble
❑ a large percentage of drugs are lipid soluble; thus drugs, and drugs that are unchanged.
the liver metabolizes the lipid-soluble drug substance
➢The lungs eliminate volatile drug substances and
to a watersoluble substance for renal excretion
products metabolized to carbon dioxide (CO2) and
❑ When the drug metabolism rate is decreased, water (H2O).
excess drug accumulation can occur and lead to
➢The urine pH influences drug excretion. Urine pH
toxicity.
varies from 4.5 to 8.
The half-life (t 1/2 ) of a drug is the time it takes for
one half of the drug concentration to be eliminated. ➢Acidic urine promotes elimination of weak base
Metabolism and elimination affect the half-life of a drugs, and alkaline urine promotes elimination of weak
A drug goes through several half-lives before more ➢ With a kidney disease that results in decreased
than 90% of the drug is eliminated. If the patient takes glomerular filtration rate (GFR) or decreased renal
650 mg of aspirin and the half-life is 3 hours, it takes 3 tubular secretion, drug excretion is slowed or impaired.
hours for the first half-life to eliminate 325 mg, 6 hours
➢ A decrease in GFR results in an increase in serum
for the second half-life to eliminate an additional 162
creatinine level and a decrease in urine creatinine
mg, and so on until the sixth half-life (or 18 hours),
clearance.
when 10 mg of aspirin is left in the body.
➢ Urea nitrogen is a waste product that your kidneys
remove from your blood. Higher than normal BUN
levels may be a sign that your kidneys aren't working
well. People with early kidney disease may not have
any symptoms. A BUN test can help uncover kidney
problems at an early stage when treatment can be
more effective
✓Saliva
RECEPTOR THEORY
a) kinase-linked receptors
b) ligand-gated ion channels
3. INHIBITION OR KILLING OF ORGANISMS - Drugs If the drug is given orally, the peak time might be 1 to 3
that inhibit or kill organisms interfere with bacterial cell hours after drug administration.
growth (e.g., penicillin exerts its bactericidal effects by
If the drug is given IV, the peak time might occur in 10
blocking the synthesis of the bacterial cell wall)
minutes.
4. IRRITATION - Drugs also can act by the mechanism
If a peak drug level is ordered, a blood sample should
of irritation (e.g., laxatives irritate the inner wall of the
be drawn at the proposed peak time, according to the
colon, thus increasing peristalsis and defecation).
route of administration.
DRUG NAMES
FEDERAL LEGISLATION - Through federal
legislation, the public is protected from drugs that are Chemical Name
- highlights the need for nurses to use knowledge and Assimilation occurs when a less powerful group
research from the social sciences as well as the changes its ways to blend in with the dominant cultural
biologic and physical sciences to provide holistic group. Adults who immigrate to a new region usually
nursing care take longer to assimilate than do younger people.
response to a drug due to genetic factors. The nurse traditional beliefs and mainstream health practices.
must integrate knowledge of pharmacogenetics within Alternative Health Practices it is called when a
patients’ cultural contexts. dominant group adopts health practices from a
nondominant group.
Culture is defined as sets of learned behavior and Pharmacogenomics refers to the general study of all
ideas that human beings acquire as members of a the different genes that determine drug behavior.
community.
TRANSCULTURAL NURSING
DRUG INTERACTIONS
PEDIATRIC AND GERIATRIC PHARMACOKINETIC
Drug-Food
Geriatric Distribution
- interaction is known to increase, decrease, or delay
drug absorption. Food can bind with drugs, causing
less or slower drug absorption. An example of food
binding with a drug is the interaction of tetracycline and
dairy products. The result is a decrease in the plasma
concentration of tetracycline. Because of the binding
effect, tetracycline should be taken 1 hour before or 2
hours after meals and should not be taken with dairy
products
Drug-Laboratory interaction
Clinical Significance
PEDIATRIC
- Phenobarbital, when given to
pregnant women near term, can
induce fetal hepatic enzymes
responsible for the glucuronidation of
bilirubin.
Pediatric Distribution - Chloramphenicol can produce grey
• GI absorption slower in infancy, but baby syndrome in neonates.
absorption from intra-muscular
injection is faster. GERIATRIC
• In neonates common practice to use Golden rule for drug therapy in elderly
IV preparations - Smallest number of drugs
• Infant skin is thin and percutaneous - In lowest possible doses
absorption can cause systemic - For shortest possible time
toxicity (ex. If potent steroids are - In simplest regimen
applied too extensively)
• Body fat content in infants low, water
content is high Pediatric Pharmodynamic
● Check compliance
GERIATRIC PHARMODYNAMIC
● Think before adding a new drug to the regimen
Pharmacodynamic Changes:
● Stopping is as important as Starting.
● Greater sensitivity to medications affecting the CNS
(benzodiazepines and opioids)