Pharmacology Basics and Objectives

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Questions and Answers

If Drug X has an initial peak of 500 mcg/L and is given every 12 hours, what will be the drug level just before the 31st dose is given?

  • 500 mcg/L (correct)
  • 1000 mcg/L
  • 250 mcg/L
  • 2000 mcg/L

At plateau, the peak drug level is always double the initial drug peak.

True (A)

What must occur for a drug to have an effect in the body?

The drug must bind to a receptor.

Food can either ____ or ____ the absorption of a drug.

<p>increase, decrease</p> Signup and view all the answers

Match the following food impacts on drug absorption with their effects:

<p>Milk = Binds tetracycline Fiber = Binds digoxin High-calorie meal = Increases absorption of Invirase Fasting = Decreases absorption rate</p> Signup and view all the answers

What does the term 'potency' refer to in pharmacology?

<p>The amount of drug required to elicit a desired response (C)</p> Signup and view all the answers

Agonists do not activate receptors.

<p>False (B)</p> Signup and view all the answers

What happens as the dosage of a drug increases?

<p>The response becomes progressively larger.</p> Signup and view all the answers

An antagonist causes pharmacological effects by blocking the activation of _______.

<p>receptors</p> Signup and view all the answers

Which drug has greater efficacy in relieving pain according to the described dose-response relationship?

<p>Meperidine (D)</p> Signup and view all the answers

A highly potent drug will always have a higher maximal efficacy.

<p>False (B)</p> Signup and view all the answers

What is the relationship between selectivity of a drug and its side effects?

<p>The more selective a drug is, the fewer side effects it will produce.</p> Signup and view all the answers

Match each type of drug action with its correct definition:

<p>Agonist = Molecule that activates receptors Antagonist = Blocks receptor activation Efficacy = Maximal response a drug can produce Potency = Amount of drug needed for response</p> Signup and view all the answers

What is the primary role of a receptor in drug interactions?

<p>To bind drugs and produce effects. (D)</p> Signup and view all the answers

An antagonist activates a receptor to produce a physiological response.

<p>False (B)</p> Signup and view all the answers

What type of molecule would you classify norepinephrine as in the context of cardiac output?

<p>Agonist</p> Signup and view all the answers

Drugs with _____ affinity for a receptor have a higher potency.

<p>high</p> Signup and view all the answers

Match the types of drug interactions with their definitions:

<p>Agonist = Activates receptors Partial agonist = Produces a response but not as great as an agonist Antagonist = Blocks the activation of a receptor Affinity = Measure of binding strength to receptors</p> Signup and view all the answers

Which statement is true regarding drug-receptor interaction?

<p>Modified occupancy theory suggests that drugs with higher affinity have higher potency. (C)</p> Signup and view all the answers

Cardiac output can be decreased by drugs that act as agonists on the receptors for norepinephrine.

<p>False (B)</p> Signup and view all the answers

Describe the effect of a partial agonist compared to a full agonist.

<p>Producing a smaller physiological response than a full agonist.</p> Signup and view all the answers

Which of the following drugs can cause discoloration of developing teeth in children?

<p>Tetracyclines (A)</p> Signup and view all the answers

Older adults are less sensitive to drugs compared to younger adults.

<p>False (B)</p> Signup and view all the answers

What is one major reason for poor adherence to medication in older adults?

<p>Multiple medications or complex regimens</p> Signup and view all the answers

In older adults, renal function undergoes progressive decline beginning in early ________.

<p>adulthood</p> Signup and view all the answers

Match the following age-related effects with their related drugs:

<p>Glucocorticoids = Growth suppression Tetracyclines = Discoloration of developing teeth Sulfonamides = Kernicterus in neonates Aspirin = Increased bleeding risk in elderly</p> Signup and view all the answers

Which factor is NOT a reason for increased adverse drug reactions in older adults?

<p>Lower sensitivity to medications (B)</p> Signup and view all the answers

The Beers Criteria is a guideline that helps prevent inappropriate prescribing in older adults.

<p>True (A)</p> Signup and view all the answers

What happens to the hepatic metabolism in older adults?

<p>It declines with age.</p> Signup and view all the answers

Which of the following drugs is most commonly associated with allergic reactions?

<p>Penicillins (D)</p> Signup and view all the answers

Idiosyncratic effects of drugs are always caused by the dosage of the drug.

<p>False (B)</p> Signup and view all the answers

What is a paradoxical effect in the context of drug responses?

<p>The opposite of the intended drug response.</p> Signup and view all the answers

The state of having adapted to a drug such that withdrawal symptoms occur if the drug is discontinued is called ______.

<p>physical dependence</p> Signup and view all the answers

Match the following drug interactions with their definitions:

<p>Addition = 1 + 1 = 2 Synergism = 1 + 1 &gt; 2 Inhibition = 1 + 1 &lt; 2 Intensification = Increased effects from drug interactions</p> Signup and view all the answers

What is an example of an iatrogenic disease?

<p>Parkinson’s-like symptoms from antipsychotics (A)</p> Signup and view all the answers

Drug-drug interactions can only intensify the effects of drugs.

<p>False (B)</p> Signup and view all the answers

What is the goal of Phase I in drug development?

<p>To evaluate drug metabolism, pharmacokinetics, and biologic effects.</p> Signup and view all the answers

Factors that determine the intensity of drug responses vary from ______ to ______.

<p>person, person</p> Signup and view all the answers

Which of the following terms refers to a decrease in drug effects from interactions?

<p>Inhibition (C)</p> Signup and view all the answers

What is a common consequence of the drug interaction between aspirin and warfarin?

<p>Increased adverse effects (D)</p> Signup and view all the answers

The liver is not crucial in many drug-drug interactions due to its limited metabolic capacity.

<p>False (B)</p> Signup and view all the answers

What is one way to minimize adverse drug-drug interactions?

<p>Minimize the number of drugs a patient receives.</p> Signup and view all the answers

The ______ interval measures the time required for the ventricles to repolarize after each contraction.

<p>QT</p> Signup and view all the answers

Match the following terms related to drug interactions with their descriptions:

<p>Cytochrome P450 = Group of enzymes involved in drug metabolism Hepatotoxic = Substance toxic to the liver Adverse Drug Reaction (ADR) = Unexpected harmful effect of a drug Boxed Warning = Strongest drug safety warning</p> Signup and view all the answers

Which of the following factors can reduce drug absorption?

<p>Elevated gastric pH (C)</p> Signup and view all the answers

Drugs that prolong the QT interval can increase the risk of life-threatening dysrhythmias.

<p>True (A)</p> Signup and view all the answers

Name a drug that is known to be hepatotoxic.

<p>Acetaminophen.</p> Signup and view all the answers

Children are ______ little adults in terms of drug metabolism and therapeutic responses.

<p>not</p> Signup and view all the answers

Match the following drugs with their specific target organ toxicity:

<p>Amphotericin B = Kidneys Doxorubicin = Heart Amiodarone = Lungs Aminoglycoside = Inner ear</p> Signup and view all the answers

Which factor contributes to increased drug interactions?

<p>Increasing number of drugs a patient is taking (B)</p> Signup and view all the answers

The interaction of Propranolol and Albuterol results in reduced therapeutic effects.

<p>True (A)</p> Signup and view all the answers

What is the primary function of the cytochrome P450 system in drug metabolism?

<p>To facilitate the metabolism of drugs in the liver.</p> Signup and view all the answers

Flashcards

Drug Half-Life (T1/2)

The time it takes for the concentration of a drug in the body to decrease by half.

Drug Plateau

The steady state of a drug in the body, where the amount of drug eliminated equals the amount of drug administered.

Drug Trough

The drug concentration in the body just before the next dose is administered.

Drug Peak

The maximum drug concentration in the body after a dose is administered.

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Pharmacokinetics

The study of how the body affects the drug, including absorption, distribution, metabolism, and excretion.

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Drug-receptor interaction

A cellular response is triggered by the interaction between a drug and a receptor.

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Receptor

A functional molecule within a cell to which a drug binds to produce its effects.

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What are receptors typically bound to?

Receptors are generally reserved for the body's regulators, such as hormones, neurotransmitters, and other molecules.

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How do drugs produce therapeutic effects?

Drugs work by stimulating or inhibiting the body's natural processes.

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Agonist

A molecule that activates a receptor, triggering a cellular response.

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Partial agonist

A molecule that partially activates a receptor, producing a weaker response than a full agonist.

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Antagonist

A molecule that blocks the activation of a receptor, preventing a cellular response.

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Affinity

The intensity of a drug's response is determined by the strength of its binding to the receptor, known as affinity.

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Drug Efficacy

The maximum effect a drug can produce. It's measured by the height of the dose-response curve.

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Drug Potency

The amount of drug needed to elicit a desired response. It's determined by the position of the dose-response curve.

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Drug Selectivity

The higher the selectivity of a drug, the fewer side effects it will produce.

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Reversible Drug Binding

The binding of a drug to its receptor is often reversible, meaning that it can be undone.

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Receptor Regulation

The activity of a receptor is regularly controlled by endogenous compounds, like hormones and neurotransmitters.

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Receptors and Drug Action

A drug's effect is determined by its interaction with receptors, which are specific for certain molecules.

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Allergic reaction

An immune response, primarily determined by the patient's sensitivity to the drug, rather than the dosage. It can change over time and is not always severe. Penicillin is a common cause.

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Idiosyncratic effect

An uncommon drug response resulting from a genetic predisposition. It is often unpredictable and can lead to reactions that are not expected based on the usual effects of the drug.

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Paradoxical effect

The opposite effect of the intended drug response. For example, a sedative might cause excitement instead of sleepiness.

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Physical dependence

A state where the body adapts to long-term drug use, resulting in withdrawal symptoms if the drug is stopped abruptly. This is common with opioids, alcohol, barbiturates, and amphetamines.

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Iatrogenic disease

A disease caused by medical treatment, often by medications. For example, some psychiatric medications can cause Parkinson's-like symptoms.

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Drug-Drug Interaction: Addition

Two drugs with similar effects are combined, resulting in an additive effect.

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Drug-Drug Interaction: Synergism

Two drugs interact to enhance each other's effects, resulting in a greater effect than the sum of their individual effects.

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Drug-Drug Interaction: Inhibition

One drug interferes with the effects of another drug, reducing the overall effect.

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Drug-Drug Interaction: Intensification of effects

Drugs that increase a desired effect (therapeutic) or an undesired effect (adverse).

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Drug-Drug Interaction: Reduction of effects

Drugs that reduce a desired effect (therapeutic) or an undesired effect (adverse).

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What are the Beers Criteria?

The Beers Criteria is a list of medications that are potentially inappropriate for older adults due to increased risk of adverse drug reactions. Using this list, prescribers can ensure they are using safer alternatives for their senior patients.

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How does body composition impact drug distribution in older adults?

Older adults typically have higher percentages of body fat compared to younger adults. This leads to increased storage of lipid-soluble drugs, which necessitates dose adjustments to ensure proper therapeutic effect.

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How does aging affect drug metabolism in older adults?

The liver's ability to metabolize drugs declines with age. This decline can affect drug elimination, leading to increased drug half-lives and intensified effects.

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How does aging affect drug excretion in older adults?

Renal function generally declines with age, resulting in slower elimination of drugs from the body. The accumulation of drugs can increase the risk of adverse reactions and toxicity in older adults.

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How does serum albumin affect drug distribution in older adults?

Older adults often experience reduced levels of serum albumin. This can lead to decreased protein binding of medications, resulting in higher levels of free, active drug, which can amplify effects and enhance the risk of adverse reactions.

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How do age-related changes affect drug responses in older adults?

Older adults can experience a wide range of age-related physiologic changes that can affect drug responses. These changes might lead to increased sensitivity to drugs, slower metabolism, and slower excretion, increasing the risk of adverse reactions.

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What is polypharmacy and why is it a concern for older adults?

Older adults are more prone to polypharmacy, taking multiple medications simultaneously. This can significantly increase the risk of drug interactions, adverse effects, and non-adherence.

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Why might adhering to medication regimens be challenging for older adults?

Older adults face many challenges that can contribute to their difficulty adhering to medication regimens. This includes factors like forgetfulness, difficulty understanding instructions, and lack of support.

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Drug-Drug Interaction

A situation where one drug affects the action of another, potentially altering its effects on the body. This can be beneficial, by increasing the therapeutic effects, or harmful, by enhancing adverse effects.

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Intensification of Effects

A type of drug-drug interaction where the effects of one drug are increased. This could lead to stronger therapeutic benefit or a higher chance of side effects.

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Reduction of Effects

A type of drug-drug interaction where the effects of one drug are reduced. This could weaken the intended therapeutic effect or minimize undesirable side effects.

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Drug Absorption

The process by which a drug enters the bloodstream from its point of administration.

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Drug Distribution

The process by which a drug is transported throughout the body to its target site.

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Drug Metabolism

The process by which the body breaks down a drug into inactive metabolites.

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Drug Excretion

The process by which the body eliminates a drug from the bloodstream.

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Cytochrome P450 (CYP)

A group of enzymes primarily found in the liver that are responsible for metabolizing many drugs. They can be induced (increased activity) or inhibited (decreased activity) by other drugs, leading to interactions.

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Altered Absorption

A type of drug-drug interaction where the absorption of one drug is altered by the other. This could be increased absorption, leading to stronger effects, or decreased absorption, weakening effects.

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Altered Distribution

A type of drug-drug interaction where the distribution of one drug is altered by the other. This could happen through competition for protein binding or changes in the body's pH.

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Altered Renal Excretion

A type of drug-drug interaction where the excretion of one drug is altered by the other, potentially affecting its concentration in the body. This involves changes in filtration, reabsorption, or active secretion of drugs in the kidneys.

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Altered Metabolism

A type of drug-drug interaction where the metabolism of one drug is altered by the other, affecting its breakdown and duration of action in the body.

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CYP Inducer

A drug that increases the activity of CYP enzymes, potentially leading to faster metabolism of other drugs.

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CYP Inhibitor

A drug that decreases the activity of CYP enzymes, potentially leading to slower metabolism of other drugs and increased drug levels in the body.

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Study Notes

Pharmacology: The Basics

  • A drug is any chemical substance that affects living processes.
  • Pharmacology is the study of drugs and their interactions with living systems.
  • Clinical pharmacology is the study of drugs in humans.
  • Therapeutics, or pharmacotherapeutics, is the use of drugs to diagnose, prevent, or treat disease.

Pharmacology: The Therapeutic Objective

  • The goal of drug therapy is to provide the most benefit with the least harm.
  • Skills, judgment, knowledge, and the desire to do good are necessary for effective drug therapy.

Properties of an Ideal Drug

  • Effectiveness: a drug must be effective at achieving its purpose.
  • Safety: the drug should produce the desired effects with minimal or no adverse side effects.
  • Selectivity: the drug should only affect the intended target without harming other parts of the body.
  • Reversibility: the drug's effects should be reversible.
  • Predictability: the drug should produce the same response in different people, assuming the same dose.
  • Ease of administration: administration should be safe and effective for the patient.
  • Freedom from drug interactions: the drug should not affect or be affected by other drugs.
  • Low cost: the drug must be cost-effective.
  • Chemical stability: the drug must remain stable during storage and use.
  • Simple generic names: the names should be easy to understand for all users.

Drug-Drug Interactions

  • Intensification of effects: some drugs may increase the therapeutic or adverse effects of other drugs.
  • Reduction of effects: some drugs may reduce the therapeutic or adverse effects.

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