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Excipient
An inactive ingredient added to a drug formulation to provide stability, improve taste or texture, or aid in drug delivery
Antibiotic
Kills living organisms (bactericidal agents)
Analgesic
Relieves pain
Example of Analgesic
Acetylsalicylic acid (Aspirin)
Example of Antibiotic
Penicillin V, Erythromycin, Metronidazole
Example of Antiemetic
Diphenhydramine hydrochloride (Benadryl), Dimenhydrinate (Gravol, Dramamine), Doxylamine pyridoxine (Diclectin)
Antiemetic
Reduces or stops vomiting (Antinauseant)
Antifungal
Kills fungi including yeast
Example of Antifungal
Miconazole (Monistat)
Antiinflammatory
Decreases inflammatory response
Example of Antiinflammatory
Acetylsalicylic acid (Aspirin), Ibuprofen (Motrin)
Antiprotozoal antibiotic amoebicide
Kills anaerobic bacteria and protozoa
Antipyretic
Reduces fever
Example of Antiprotozoal antibiotic amoebicide
Metronidazole (Flagyl)
Example of Antipyretic
Acetaminophen (Tylenol)
Cervical Ripener
Causes the cervix to soften
Example of Cervical Ripener
Prostaglandin E2, dinoprostone (Prepidil)
Pharmacodynamics
Refers to what a drug does to the body. It explains the effects, both intended and unintended, that a drug has once it has reached its site of action.
Affinity
Refers to the strength of the binding between a drug and its receptor.
Drug-Receptor Complex
Formed when a drug binds to its specific receptor.
Pharmacodynamics
Refers to what a drug does to the body. It explains the effects, both intended and unintended, that a drug has once it has reached its site of action.
Drug actions
Can be described from several different perspectives: cellular level, organism level, and population level.
Cellular level
Describes drug actions on a cellular level.
Efficacy
Refers to the maximum effect that a drug can produce.
Potency
Refers to the amount of drug required to produce a certain effect.
Second messengers
Explained in Chapter 4, these are molecules involved in transmitting signals from receptors to target molecules.
Autonomic nervous system
An overview of the autonomic nervous system is provided in Chapter 5.
Affinity
The binding of drugs and receptors occurs at a certain rate called the association rate. The dissociation rate describes how quickly the drug detaches or dissociates from its receptor.
Dissociation constant (Kd)
The ratio of the rate of breakdown to the rate of formation of the drug-receptor complex. Drugs with a high dissociation constant do not bind well to their receptors.
Drug-receptor complex
For most drugs, the first step to having any effect is binding to a receptor on the cell surface. A receptor is normally a protein or glycoprotein that sits on the cell surface and if a drug binds to its receptor, it forms a drug-receptor complex.
What does the dissociation constant (Kd) predict?
How much of the drug will bind to its receptor
What is the relationship between dissociation constant and affinity?
Drugs with a low dissociation constant have a high affinity to their receptor
What is the equation for the formation of drug-receptor complex?
D + R ⇌ DR
What is the equation for the dissociation of drug-receptor complex?
DR ⇌ D + R
Affinity
The strength of the drug-receptor binding
Agonist
A drug that binds to a receptor and has the same effect as the natural ligand
Efficacy
The ability of a drug to produce a therapeutic effect
Potency
The amount of drug needed to produce a specific effect
Chapter 3
Population Level Therapeutic Index
Drug actions described in terms of affinity for receptor at cellular level in Chapter 1.
True
Efficacy and potency of a drug explained with agonism and antagonism at organism level in Chapter 2.
True
Quantal effects refer to responses that can be categorized as 'yes' or 'no'.
True
The dose-response curve demonstrates the relationship between the dose of a drug and the response it produces.
True
Dose-response curves can be used to calculate the effective dose at which 50% of the population will respond.
True
The ED50 is the effective dose to treat 50% of the people.
True
Dose-response curves can also be created for side effects of a drug.
True
Therapeutic window is the difference between the effective dose and the dose that causes unacceptable side effects.
True
LD50 is the lethal dose for 50% of the population.
True
Therapeutic index (TI) is the ratio of the LD50 to the ED50.
True
An ideal drug would...
treat an illness without having any side effects
The difference between the dose of drug that is effective and the dose that causes unacceptable side effects is...
important
The lethal dose for 50 of the population is called...
LD 50
Unacceptable side effects depend on...
the condition being treated
Clinicians and patients may tolerate more side effects from drugs used to treat...
serious illness
The difference between doses can be expressed as...
therapeutic index, therapeutic ratio, or margin of safety
The doseresponse curve shows the relationship between...
drug dose and the response it produces
A drug with a wide therapeutic window...
has a lot of difference between the effective dose and the toxic dose
Drugs with narrow therapeutic windows are typically used to treat...
serious ailments
Clinicians have to start with a very low dose of toxic drugs and...
slowly increase the dose while monitoring patients carefully
The therapeutic index is calculated by dividing...
the lethal dose (LD 50) by the effective dose (ED 50)
The therapeutic index compares...
the amount of drug that causes the therapeutic effect to the amount that causes toxic effects
The therapeutic window is the space between...
the doseresponse curves for therapeutic effect and toxicity
Therapeutic indices using the onset of toxic effects compared to the ED 50 may also be used to calculate...
the therapeutic index
A drug with a large therapeutic index...
will not immediately result in serious side effects if the dose is miscalculated
Drugs with large therapeutic indices are often given in large amounts to...
ensure their effectiveness
NTI stands for...
narrow therapeutic index
An index cannot be narrow, instead it should be called a...
low therapeutic index or a low therapeutic ratio
A small therapeutic index means that...
the drug has only a narrow window in which the therapeutic effect outweighs the negative side effects
To evaluate the effectiveness of a treatment, a doseresponse curve can be created by...
plotting the dose of the drug against the number of people responding to the treatment
The therapeutic window is the difference between...
the lethal dose (LD 50) and the effective dose (ED 50)
The therapeutic index is the ratio of...
the LD 50 to the ED 50
A drug with a small therapeutic index is also called...
NTI (narrow therapeutic index)
The binding of a to its receptor is just one step in having an effect.
The binding has to be translated into a change inside of the cell. For this, a second messenger is often required.
When acetylcholine binds to its receptor on a somatic motor nerve, the ion channel opens and sodium rushes in and depolarizes the membrane.
The mechanism of this is shown in Figure 41, the left side of which shows a ligand binding to a receptor bound to an ion channel. When the drug binds, the channel opens. However, most drugs do not work in this way.
A complex series of reactions occur after a ligand binds to its receptor.
The drug itself never penetrates the cell membrane. Instead, a second messenger is released to convey the message to the target, such as the nucleus.
The main reason second messengers are required is that the ligand cannot directly enter the cell or affect the target.
Instead, the ligand binds to a receptor on the cell surface, which then activates a second messenger inside the cell to carry out the desired effect.
Autonomic nervous system (ANS)
The branch of the nervous system that helps maintain homeostasis in the body by controlling involuntary muscles and glands.
Autonomic
Working autonomously and independently.
Visceral motor nervous system
The part of the autonomic nervous system that controls the muscles of the intestines and other organs and blood vessels.
Visceral efferents
The part of the autonomic nervous system that controls smooth muscle.
Visceral afferents
Sensory neurons of the autonomic nervous system.
Chapter 11
Routes of Drug Administration
Route of Administration
The path by which a drug or other substance is taken into the body
Enteric
The most common route of administration where drugs enter the body via the gastrointestinal (GI) tract
Parenteral
A route of drug administration that does not involve the GI tract
Enteral
Through the intestines, reached via the GI tract
Drug absorption
The movement of a drug from its site of application to the blood.
Site of application
The location where a drug is applied or administered.
Cutaneous membrane
The skin, which is a barrier that drugs can be absorbed through.
Mucous membranes
Membranes lining body cavities that drugs can be absorbed through, such as the lungs, oral cavity, nasal cavity, or vagina.
Gastrointestinal wall
The wall of the gastrointestinal tract, which drugs can be absorbed through.
Factors affecting absorption
Various factors that can influence drug absorption, including drug solubility, characteristics of the membrane being crossed, size of the drug molecule, and its affinity to other molecules.
Drug solubility
The ability of a drug to dissolve in a liquid, which can impact its absorption.
Phospholipid bilayer
A double layer of phospholipids that forms the plasma membrane of cells.
Charged molecules
Molecules that have an electric charge, which may have difficulty crossing the lipid bilayer of the plasma membrane.
Drug distribution
The process by which a drug moves from the bloodstream into various tissues of the body.
Factors influencing drug distribution
Water solubility, ionization, pH of body fluids
Water solubility
A drug's ability to dissolve in water, which determines its movement in the blood.
Ionization
The process in which molecules gain or lose ions, affecting their solubility in blood and distribution throughout the body.
pH of body fluids
The acidity or alkalinity of body fluids, which can impact the solubility and distribution of drugs.
Drug Distribution
After a drug has been absorbed, it distributes into the fluids and tissues of the body.
Factors Influencing Distribution
Water solubility and pH of body fluids
Water Solubility
A drug's solubility in water is key to its movement in blood.
Ionized Molecules
Ionized molecules dissolve easily in the blood and are rapidly distributed throughout the body.
pH of Body Fluids
The pH of body fluids affects the solubility and distribution of drugs.
Barriers in the Body
Certain barriers in the body can alter the movement of drugs.
Acids and Bases
Acids are ionized in basic solutions, while bases are ionized in acidic solutions.
Blood pH
The blood has a pH of about 7.4, which is weakly basic.
Solubility in Lipids
Acidic drugs that are relatively soluble in blood are relatively insoluble in lipids.
Drug metabolism
The process in which the body changes drugs
Metabolism purpose
Elimination of the drug
Drug metabolism pathways
Several pathways by which the body metabolizes drugs
Location of drug-metabolizing enzymes
Greatest concentration in the liver, lesser extent in the gut
Metabolizing enzymes in the GI tract
Reflects the fact that most drugs enter the body orally and are first exposed to the gut
Main organ that metabolizes drugs
Liver
Other organs that metabolize drugs
Kidneys and gut wall
Some drugs that do not need to be metabolized
Penicillin G, for example
Volume of Distribution
The variable that relates plasma drug concentration to dose. It determines how much drug stays in plasma and how much distributes to the tissues.
Target Organs
The organs or tissues where drugs distribute to have their effect.
Total Body Water
The sum of all water in the body, which includes intracellular and extracellular fluid.
Plasma Drug Concentration
The concentration of a drug in the plasma or serum.
Vd (Volume of Distribution)
The variable that relates plasma drug concentration to dose. If a drug has a high Vd, it tends to leave the plasma and enter the tissue.
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Scholarly Assistant's Insights
A comprehensive pharmacology flashcard deck covering drug classifications, actions, pathways, and administration routes.
Pharmacology
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Drug Administration
Drug Absorption
Pharmacodynamics
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