NUR-641E Mid-Term Exam Study Guide
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
Heparin produces rapid anticoagulation by binding with antithrombin III, and
inhibits factors IXa, Xa, XIIa, and XIII.
Monitor heparin with a PTT (low dose SC heparin [5000 units BID] does not
require aPTT monitoring).
Warfarin inhibits vitamin K-dependent blood factors II, VII, IX and X; takes
several days for its anticoagulant effect.
Monitor the International Normalized Ratio (INR) when warfarin is used.
Blood Factor IIa inhibitor (direct thrombin inhibitor): dabigatran (Pradaxa).
An antidote to dabigatran-induced hemorrhage is idarucizumab.
Blood Factor Xa inhibitors: apixaban (Eliquis), edoxaban (Savaysa), rivaroxaban
(Xarelto), fondaparinux (Arixtra).
Know what pulmonary emboli are, where they come from and what these
emboli do in the body
Pulmonary embolism is a blockage in one of the pulmonary arteries in your lungs.
In most cases, pulmonary embolism is caused by blood clots that travel to the lungs
from the legs or, rarely, other parts of the body (deep vein thrombosis).
Know the risk factors for cerebrovascular accident (CVA)
Some stroke risk factors, such as gender, age and family history, can't be
controlled. Lifestyle factors that increase your risk of stroke include high blood
, pressure, smoking, diabetes, high blood cholesterol levels, heavy drinking, high
salt and high fat diet and lack of exercise.
Know the elements involved in the action potential of myocardial tissue
Calcium…??
Know what tuberculosis is and its epidemiology in the world.
Tuberculosis (TB) is one of the top 10 causes of death worldwide.
In 2017, 10 million people fell ill with TB, and 1.6 million died from the disease
(including 0.3 million among people with HIV).
In 2017, an estimated 1 million children became ill with TB and 230 000 children
died of TB (including children with HIV associated TB).
TB is a leading killer of HIV-positive people.
Isoniazid (INH) is famous for causing jaundice when combined with other
drugs in a multidrug combination for treating TB.
Be able to explain the side effects of multidrug therapy/polypharmacy
3.1 Increased Healthcare Costs. Polypharmacy contributes to health care costs to
both the patient and the healthcare system. ...
3.2 Adverse Drug Events. ...
3.3 Drug-Interactions. ...
3.4 Medication Non-adherence. ...
3.5 Functional Status. ...
3.6 Cognitive Impairment. ...
3.7 Falls. ...
3.8 Urinary Incontinence.
Know the difference between vertical and horizontal transmission of
organisms
In general, transmission of viruses can occur through two pathways: horizontal and
vertical transmission. In horizontal transmission, viruses are transmitted among
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
Heparin produces rapid anticoagulation by binding with antithrombin III, and
inhibits factors IXa, Xa, XIIa, and XIII.
Monitor heparin with a PTT (low dose SC heparin [5000 units BID] does not
require aPTT monitoring).
Warfarin inhibits vitamin K-dependent blood factors II, VII, IX and X; takes
several days for its anticoagulant effect.
Monitor the International Normalized Ratio (INR) when warfarin is used.
Blood Factor IIa inhibitor (direct thrombin inhibitor): dabigatran (Pradaxa).
An antidote to dabigatran-induced hemorrhage is idarucizumab.
Blood Factor Xa inhibitors: apixaban (Eliquis), edoxaban (Savaysa), rivaroxaban
(Xarelto), fondaparinux (Arixtra).
Know what pulmonary emboli are, where they come from and what these
emboli do in the body
Pulmonary embolism is a blockage in one of the pulmonary arteries in your lungs.
In most cases, pulmonary embolism is caused by blood clots that travel to the lungs
from the legs or, rarely, other parts of the body (deep vein thrombosis).
Know the risk factors for cerebrovascular accident (CVA)
Some stroke risk factors, such as gender, age and family history, can't be
controlled. Lifestyle factors that increase your risk of stroke include high blood
, pressure, smoking, diabetes, high blood cholesterol levels, heavy drinking, high
salt and high fat diet and lack of exercise.
Know the elements involved in the action potential of myocardial tissue
Calcium…??
Know what tuberculosis is and its epidemiology in the world.
Tuberculosis (TB) is one of the top 10 causes of death worldwide.
In 2017, 10 million people fell ill with TB, and 1.6 million died from the disease
(including 0.3 million among people with HIV).
In 2017, an estimated 1 million children became ill with TB and 230 000 children
died of TB (including children with HIV associated TB).
TB is a leading killer of HIV-positive people.
Isoniazid (INH) is famous for causing jaundice when combined with other
drugs in a multidrug combination for treating TB.
Be able to explain the side effects of multidrug therapy/polypharmacy
3.1 Increased Healthcare Costs. Polypharmacy contributes to health care costs to
both the patient and the healthcare system. ...
3.2 Adverse Drug Events. ...
3.3 Drug-Interactions. ...
3.4 Medication Non-adherence. ...
3.5 Functional Status. ...
3.6 Cognitive Impairment. ...
3.7 Falls. ...
3.8 Urinary Incontinence.
Know the difference between vertical and horizontal transmission of
organisms
In general, transmission of viruses can occur through two pathways: horizontal and
vertical transmission. In horizontal transmission, viruses are transmitted among
