NR565 Advanced Pharmacology
Fundamentals Week 1
A provider may consider testing for CYP2D6 variants prior to starting tamoxifen for breast
cancer to: - ANS-Reduce the likelihood of therapeutic failure with tamoxifen treatment
The movement of a drug into the blood from its site of administration is known as absorption
(ANS). Variables that influence absorption:
-blood flow at site of administration
-dosage form
-route (compatibility, bioavailability, action onset and duration) .... Parenteral, oral, topical
African Americans - ANS-Studied more than any other ethnic group in relation to differences in
drug metabolism & response
-underlying hypertension prevalence is among the highest in the world-HTN occurs at an earlier
age than in other races
-require a high dosage of ACE inhibitors or combined therapy with low dose diuretics to
effectively reduce blood pressure
-show less effective monotherapy with beta blocker and ACE inhibitors than Caucasians
-The first drug, specifically labeled for use by African Americans, isosorbide
dinitrate/hydralazine (BiDil) is approved by the US FDA. -African American Heart Failure Trial
(A-HeFT) demonstrates that by adding isosorbide dinitrate/hydralazine (BiDil) to standard
therapy for heart failure increases survival in black patients with advanced failure
-require a higher dose of glucocorticoids than Caucasians do to manage their asthma
symptoms, regardless of the severity or status of their asthma. agonists - ANS-Agonists, or full
agonists, are drugs that produce receptor stimulation and a conformational change every time
they bind. Full agonists do not need all of the available receptors to produce a maximum
response. --
-Less than 10% needed for maximum response.
Always consider drug-drug interactions with: - ANS-st john's wort
ssri
snri
statin
ACE/ARB
PPI
Warfarin
Bactrim
Drugs that occupy receptors without stimulating them are known as antagonists (ANS).
Antagonists occupy a receptor site and prevent other molecules, such as agonists, from
occupying the same site and producing a response. -
, -Antagonists produce no direct response. Following administration of antagonists, we observe
a response as a result of agonists stimulating their inhibiting receptors. For example, beta
blockers such as propranolol and atenolol act as antagonists at the beta-adrenoceptor.
Asians and Hispanics - ANS--ethnic variation in drug response
-need lower doses of sedatives and anti-psychotics
Clinical Stage - ANS-Phase 1: Biological effects, safe dosage
Phase 2: New drug treats small amount of patients
Phase 3: Larger size, must be as good as or better than others.
Cultural assessment - ANS--languages spoken; need for interpreter?
-health beliefs and practice
-previous uses of medicine, including home remedies, herbal treatments, and folk remedies
-treatments and medications available over-the-counter (OTC) Cultural considerations in
pharmacology - ANS--USA culturally diverse
-cultural assessment part of cultural competency for professional nurses-ethnicity
-ethno-pharmacology
-race? ; Race is defined socially and politically. -health beliefs and practices
-barriers to adequate healthcare
Cultural considerations in the nursing process - ANS--influence of ethnicity on genetics and
drug response
-drug polymorphism
-adherence with therapy
-environmental and economic considerations
-pharmacokinetics
-pharmacodynamics
-varying drug response in different racial or ethnic groups
CYP 2D6 - ANS-responsible for metabolizing codeine into morphine and hydrocodone into
hydromorphone. about 7% of caucasians lack this enzyme and may not get effective pain relief
from these medications.
Pts with a highly active CYP 2D6 are at risk for toxicity following admin of either codeine or
hydrocodone
CYP 450 and Drug Metabolism - ANS-The majority of drugs are metabolized in the liver by
hepatic isoenzymes, the most important of which is the CYP450 isoenzyme.
Variation in the CYP 450 enzyme causes differences in drug metabolism.These variations can
be developmental, genetic, or caused by disease states.
It is possible to speed up or speed up these enzymes. Concurrent therapy by an inhibitor or
inducer may alter metabolism of a medication.
CYP3A4 - ANS-Major drug metabolizing enzyme.
Found in the lining of the stomach (affected by food)
Nifedipine, which is in grapefruit juice, prevents - Higher blood levels in: azole antifungals,
statins, prednisone, prednisolone, dexamethasone, carbamazepine
Cytochrome P450 Enzymes - ANS--major drug metabolizing enzyme system
-race, gender, age, nutrition, stress, and environment are factors that may alter gene
expression of families and subfamilies of CYP 450
Fundamentals Week 1
A provider may consider testing for CYP2D6 variants prior to starting tamoxifen for breast
cancer to: - ANS-Reduce the likelihood of therapeutic failure with tamoxifen treatment
The movement of a drug into the blood from its site of administration is known as absorption
(ANS). Variables that influence absorption:
-blood flow at site of administration
-dosage form
-route (compatibility, bioavailability, action onset and duration) .... Parenteral, oral, topical
African Americans - ANS-Studied more than any other ethnic group in relation to differences in
drug metabolism & response
-underlying hypertension prevalence is among the highest in the world-HTN occurs at an earlier
age than in other races
-require a high dosage of ACE inhibitors or combined therapy with low dose diuretics to
effectively reduce blood pressure
-show less effective monotherapy with beta blocker and ACE inhibitors than Caucasians
-The first drug, specifically labeled for use by African Americans, isosorbide
dinitrate/hydralazine (BiDil) is approved by the US FDA. -African American Heart Failure Trial
(A-HeFT) demonstrates that by adding isosorbide dinitrate/hydralazine (BiDil) to standard
therapy for heart failure increases survival in black patients with advanced failure
-require a higher dose of glucocorticoids than Caucasians do to manage their asthma
symptoms, regardless of the severity or status of their asthma. agonists - ANS-Agonists, or full
agonists, are drugs that produce receptor stimulation and a conformational change every time
they bind. Full agonists do not need all of the available receptors to produce a maximum
response. --
-Less than 10% needed for maximum response.
Always consider drug-drug interactions with: - ANS-st john's wort
ssri
snri
statin
ACE/ARB
PPI
Warfarin
Bactrim
Drugs that occupy receptors without stimulating them are known as antagonists (ANS).
Antagonists occupy a receptor site and prevent other molecules, such as agonists, from
occupying the same site and producing a response. -
, -Antagonists produce no direct response. Following administration of antagonists, we observe
a response as a result of agonists stimulating their inhibiting receptors. For example, beta
blockers such as propranolol and atenolol act as antagonists at the beta-adrenoceptor.
Asians and Hispanics - ANS--ethnic variation in drug response
-need lower doses of sedatives and anti-psychotics
Clinical Stage - ANS-Phase 1: Biological effects, safe dosage
Phase 2: New drug treats small amount of patients
Phase 3: Larger size, must be as good as or better than others.
Cultural assessment - ANS--languages spoken; need for interpreter?
-health beliefs and practice
-previous uses of medicine, including home remedies, herbal treatments, and folk remedies
-treatments and medications available over-the-counter (OTC) Cultural considerations in
pharmacology - ANS--USA culturally diverse
-cultural assessment part of cultural competency for professional nurses-ethnicity
-ethno-pharmacology
-race? ; Race is defined socially and politically. -health beliefs and practices
-barriers to adequate healthcare
Cultural considerations in the nursing process - ANS--influence of ethnicity on genetics and
drug response
-drug polymorphism
-adherence with therapy
-environmental and economic considerations
-pharmacokinetics
-pharmacodynamics
-varying drug response in different racial or ethnic groups
CYP 2D6 - ANS-responsible for metabolizing codeine into morphine and hydrocodone into
hydromorphone. about 7% of caucasians lack this enzyme and may not get effective pain relief
from these medications.
Pts with a highly active CYP 2D6 are at risk for toxicity following admin of either codeine or
hydrocodone
CYP 450 and Drug Metabolism - ANS-The majority of drugs are metabolized in the liver by
hepatic isoenzymes, the most important of which is the CYP450 isoenzyme.
Variation in the CYP 450 enzyme causes differences in drug metabolism.These variations can
be developmental, genetic, or caused by disease states.
It is possible to speed up or speed up these enzymes. Concurrent therapy by an inhibitor or
inducer may alter metabolism of a medication.
CYP3A4 - ANS-Major drug metabolizing enzyme.
Found in the lining of the stomach (affected by food)
Nifedipine, which is in grapefruit juice, prevents - Higher blood levels in: azole antifungals,
statins, prednisone, prednisolone, dexamethasone, carbamazepine
Cytochrome P450 Enzymes - ANS--major drug metabolizing enzyme system
-race, gender, age, nutrition, stress, and environment are factors that may alter gene
expression of families and subfamilies of CYP 450
