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NUR-641E Study Guide 1.Midterm

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NUR-641E Study Guide 1.Midterm Understand what a prodrug is, and activation/inactivation by liver enzymes, and how it differs from active drugs. Know what Bioavailability (BA) Bioavailability is affected by chemical instability, solubility and first-pass metabolism Bioequivalence does not affect bioavailability Understand what the Cytochrome P450 system is in the liver Inhalation, oral and parenteral drug action and onset of effects? Know the mechanism of action of anticoagulants (e.g., warfarin, apixaban, heparin) Know what pulmonary emboli are, where they come from and what these emboli do in the body Know the risk factors for cerebrovascular accident (CVA) Know the elements involved in the action potential of myocardial tissue Calcium…?? Know what tuberculosis is and its epidemiology in the world ..........................

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NUR-641E Mid-Term Exam
Study Guide
Note: Read the questions: the questions only have one answer unless the question specifically
states there is more than one correct answer.

Understand what a prodrug is, and activation/inactivation by liver enzymes, and
how it differs from active drugs.

The liver is the principal site of drug metabolism. Although metabolism typically inactivates
drugs, some drug metabolites are pharmacologically active—sometimes even more so than the
parent compound. An inactive or weakly active substance that has an active metabolite is called a
prodrug, especially if designed to deliver the active moiety more effectively.



Know what Bioavailability (BA)

a term used in pharmacology and nutritional and environmental sciences. In
pharmacology, it refers to the degree and rate at which an administered drug is
absorbed by the body's circulatory system, the systemic circulation. Bioavailability is
an essential measurement tool since it determines the correct dosage for non-
intravenous administration of a drug availability means

Bioavailability. In pharmacology, bioavailability (BA or F ) is a subcategory of
absorption and is the fraction of an administered dose of unchanged drug that reaches
the systemic circulation



Bioavailability is affected by chemical instability, solubility and first-pass
metabolism

The first pass effect- is a phenomenon of drug metabolism whereby the concentration
of a drug is greatly reduced before it reaches the systemic circulation. It is the fraction
of drug lost during the process of absorption which is generally related to the liver and
gut wall.

Bioequivalence does not affect bioavailability

Bioequivalence is the similarity of two drugs that share the same desired outcome for
patients. Pharmaceutical equivalence means two drugs release the active ingredient into

, the bloodstream at the same amount and same rate. When assessing how well a generic
drug works, scientists evaluate its bioequivalence to the name-brand version.

Understand what the Cytochrome P450 system is in the liver

Cytochrome P450 enzymes are primarily found in liver cells but are also located in
cells throughout the body.....Cytochrome P450 enzymes account for 70 percent to 80
percent of enzymes involved in drug metabolism. Cytochrome P450 enzymes also
function to metabolize potentially toxic compounds, including drugs and products of
endogenous metabolism such as bilirubin, principally in the liver.



Clopidogrel (Plavix) is a prodrug and must be activated by hepatic CYP2C19 metabolism;
individuals who are poor metabolizers may not form the active metabolite and have reduced
antiplatelet response.



A drug’s half-life determines how often the drug is administered?

The elimination half-life of a drug is a pharmacokinetic parameter that is
defined as the time it takes for the concentration of the drug in the
plasma or the total amount in the body to be reduced by 50%. In other
words, after one half-life, the concentration of the drug in the body will
be half of the starting dose.

Steady state of a drug is reached in approximately 5 to 6 times the half-life

Inhalation, oral and parenteral drug action and onset of effects?

Inhalational administration can be used. The lungs serve as an effective route of
administration of drugs. The pulmonary alveoli represent a large surface and a minimal
barrier to diffusion. The lungs also receive the total cardiac output as blood flow. Thus,
absorption from the lungs can be very rapid and complete.

Bioavailability of drugs administered orally varies greatly.

Parenteral administration refers to any routes of administration that do not involve
drug absorption via the GI tract (par = around, enteral = gastrointestinal), including the
IV, intramuscular (IM), subcutaneous (SC or SQ), and transdermal routes

Know the mechanism of action of anticoagulants (e.g., warfarin, apixaban, heparin).
Warfarin competitively inhibits the vitamin K epoxide reductase complex 1 (VKORC1), which
is an essential enzyme for activating the vitamin K available in the body. Through this
mechanism, warfarin can deplete functional vitamin K reserves and therefore reduce the
synthesis of active clotting factors

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