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MODULE 1
1) Discuss the significance of the Cytochrome P450 system on metabolism of drugs.
1. It is a group of 12 closely related enzyme families. CYP1, CYP2, CYP3
metabolize drugs. The other 9 families metabolize endogenous compounds
(ex. Fatty acids, steroids).
2) Discuss the major hepatotoxic drugs and possible effects on drug
metabolism. 1.
3) List various routes of drug elimination—review normal renal function including
glomerular filtration, passive tubular reabsorption and active tubular secretion;
describe the implications on drug clearance and how elimination affects
prescribing.
1.
4) Discuss terms used to describe drug actions-agonist, partial agonist, antagonist.
1. Agonist: molecules that activate receptors
2. Partial agonist: Only has moderate intrinsic activity. Maximal effect that a
partial agonist can produce is lower than that of a full agonist.
3. Antagonist: Produce their effects by preventing receptor activation by
endogenous regulatory molecules and drugs.
5) Discuss the impact of food on drug absorption, drug metabolism and on drug
toxicity and action—as well as the timing of drug administration.
LIFESPAN
1. Hepatic metabolism and GFR increase during pregnancy, dosages of some
drugs may need to be increased.
2. Rate of albumin to water decreases
1. Third trimester: Renal blood flow is doubled and renal excretion is
accelerated (drugs excreted rapidly)
2. Tone and mobility of bowel decrease
3. Prolongation of drug effects Total (½ life increases)
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3. Understand stages of development in pregnancy
1. Conception: through week 2
2. Embryonic period: week 3-week 8
a) Gross malformations can be produced by teratogens
3. Fetal period: week 9-delivery
4. Understand pregnancy labeling
1. 3 categories now
a) Pregnancy, lactation, male & female reproductive potential
5. How do you decrease risk in the infant during breastfeeding?
1. Take meds immediately after breastfeeding, avoid drugs that
have long half-lives, choose drugs that tend to be excluded from milk,
avoid drugs that are known to be hazardous.
6. How do pediatric patients differ in their response to medications?
1. Absorption
a) Oral?
1. Neonates: drug remain in the stomach longer which
increases the levels, low acidity can affect the absorption
of acid labile drugs
b) Parenteral?
1. Reponses are slow and erratic.
2. Infancy: absorption is more rapid than in neonates & adults
3. Best avoided in infants
c) Transdermal?
1. Greater skin permeability which increases topical drug
absorption and increases the risk for toxicity
2. Distribution
a) Protein binding
1. Neonates: less protein-binding—increased availability of
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highly protein bound drugs such as phenytoin, diazepam,
and phenobarbital. Reduced dosages needed in these highly
bound drugs.
b) Blood Brain Barrier
1. Not fully developed at birth, drugs have easy access to the
CNS, doses should be reduced.
3. Metabolism
a) Hepatic function?
1. Liver hasn’t reached full maturation—sensitive to drugs
eliminated by the CYP450. Liver’s ability to
metabolize drugs increases about one month after birth.
b) T half life
1. Decreased by as much as 48-72 hours
4. Excretion
a) Renal?
1. GFR is significantly reduced at birth, drugs eliminated by
the kidneys must be given in a reduced dosage and longer
dosing intervals.
2. What are the BON rules and regulations for prescriptive authority for the
advance practice nurse?
1) Texas is very restricted
2) Describe the pharmacokinetic processes of absorption, distribution, metabolism
and elimination and how differences in these areas affect drug action.
1. Absorption
1. Drug’s movement from the site of administration into the blood.
2. Distribution
1. Drug’s movement from the blood into the interstitial space
of tissues and from there into cells.
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3. Metabolism
1. Biotransformation is the enzymatically mediated alteration of drug
structure.
4. Elimination
1. Combination of metabolism and excretion
3) Compare and contrast pharmacokinetics and pharmacodynamics of
special populations—pediatrics, older adults and those that are pregnant.
1. Pediatrics—they have organ immaturity, elderly—they have organ
degeneration, loss of nephrons, excretion of drug is decreased and you have to
give this population a lower dose of medication. Medication can pass through
milk of lactating females.
4) Analyze a drug interaction to determine an appropriate course of action.
1. Basic mechanism of drug-drug interactions through pharmacokinetic
interactions are altered absorption, altered distribution, altered metabolism, and
altered renal excretion.
5) Identify medications with a narrow therapeutic index requiring drug
level monitoring.
1.
6) Discuss the effect of ionization and pH on absorption.
1. Drugs that are weak acids are best absorbed in acidic environments. Acidic drugs
accumulate on the alkaline side, basic drugs accumulate on the acidic side
known as ion trapping. Ionization of the drugs is pH dependent, when the pH and
the fluid on one side of the membrane differs from the pH on the other side, drug
molecules tend to accumulate on the side where the pH most favors ionization.
7) Discuss factors affecting drug distribution.
1. Competition for protein binding and alteration of extracellular pH
8) Discuss barriers affecting drug distribution—such as placental membrane,
blood brain barrier and volume of distribution.