Pharmacology Quiz on Hypertension Medications

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Questions and Answers

Which medication should be avoided in combination with aliskiren due to the risk of hypotension and hyperkalemia?

  • Losartan
  • Telmisartan
  • Enalaprilat
  • Lisinopril (correct)

Which medication class selectively blocks the vasoconstrictive effects of angiotensin II?

  • ARBs (correct)
  • Direct renin inhibitors
  • ACE inhibitors
  • Aldosterone Inhibitors

A patient is prescribed olmesartan for hypertension. What potential adverse effect should be monitored?

  • Hypotension
  • Hypokalemia
  • Hypernatremia
  • Renal decline (correct)

Which of the following medications is classified as a direct renin inhibitor?

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

What is the mechanism of action of ACE inhibitors in treating hypertension?

<p>Inhibiting angiotensin-converting enzyme (A)</p> Signup and view all the answers

Which of the following characteristics enables a drug to bypass Phase I metabolism?

<p>Already possessing polar molecule groups. (B)</p> Signup and view all the answers

Which of the following is NOT a typical outcome of Phase I drug metabolism?

<p>Direct excretion of the drug from the body. (D)</p> Signup and view all the answers

What is the primary purpose of Phase II drug metabolism?

<p>To attach hydrophilic groups to drugs or their Phase I metabolites. (B)</p> Signup and view all the answers

Which of the following receptor types involves direct alteration of DNA transcription?

<p>Intracellular receptors. (A)</p> Signup and view all the answers

Which best describes the function of an antagonist?

<p>It prevents receptor activation by agonists. (D)</p> Signup and view all the answers

The 'rebound phenomenon' associated with sudden drug discontinuation is most closely related to which receptor type?

<p>G protein-coupled receptors. (B)</p> Signup and view all the answers

What is a 'Quantal' dose-reponse?

<p>The rate of individuals in a population exhibiting a defined response at a given dose. (B)</p> Signup and view all the answers

How does a partial agonist behave in the presence of a full agonist?

<p>It acts as an antagonist, reducing the response of the full agonist. (D)</p> Signup and view all the answers

What factor determines the time it takes to reach steady state for a drug?

<p>The drug's half-life (A)</p> Signup and view all the answers

A drug with a significant first-pass effect would likely require which of the following?

<p>A higher dose to achieve the desired therapeutic effect (A)</p> Signup and view all the answers

Which route of administration is LEAST likely to be affected by first-pass metabolism?

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

A drug has a therapeutic index of 2:1. What does this suggest about its safety?

<p>The drug is relatively unsafe because a dose only twice the effective dose could be lethal. (A)</p> Signup and view all the answers

If a drug's half-life is 8 hours, approximately how long will it take to reach steady state?

<p>24-40 hours (B)</p> Signup and view all the answers

A pro-drug is best described as:

<p>An inactive drug that needs to be metabolized into its active form. (D)</p> Signup and view all the answers

What does bioavailability represent in pharmacokinetics?

<p>The proportion of the drug dose that reaches systemic circulation. (B)</p> Signup and view all the answers

During which phase of drug metabolism do oxidation, reduction, and hydrolysis reactions typically occur?

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

An infant (older than 28 days but less than 12 months) receives a topical medication. What physiological factor increases the risk of toxicity compared to an adult?

<p>Enhanced transdermal absorption due to differences in skin physiology. (A)</p> Signup and view all the answers

A neonate (0-28 days) requires medication. What is the primary concern regarding renal clearance in this age group?

<p>Low renal clearance, potentially causing drug accumulation and toxicity. (B)</p> Signup and view all the answers

A 6-month-old infant needs a hydrophilic drug. What dosage adjustment should be considered due to the infant's body composition?

<p>A higher dose due to a greater percentage of body weight being water. (D)</p> Signup and view all the answers

A physician is attempting to determine the correct dosage of a highly lipophilic drug for a 9-month-old infant. What consideration regarding the infant's body composition is most important?

<p>Infants have decreased percentage of body fat, leading to a smaller volume of distribution. (A)</p> Signup and view all the answers

Compared to adults, how does the rate of drug metabolism generally differ in children older than 1 year?

<p>Drug metabolism is generally faster in children, potentially requiring increased dosages or more frequent administration. (B)</p> Signup and view all the answers

An infant (older than 28 days but less than 12 months) is prescribed a medication that is primarily metabolized through Phase II metabolism. What should the prescriber consider?

<p>Phase II metabolism is reduced in infants, potentially leading to drug accumulation. (B)</p> Signup and view all the answers

What ethical principle emphasizes the importance of equitable distribution of benefits and consequences in healthcare decisions, ensuring that patient needs are prioritized?

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

According to the provided content, Which of the following is a true consideration regarding intramuscular (IM) absorption in neonates (0-28 days old)?

<p>IM absorption is slowed in neonates, potentially affecting drug onset and efficacy. (B)</p> Signup and view all the answers

According to the content, what is the major concern when there are adverse drug effects due to immature organs?

<p>Minimum effective concentration is longer. (C)</p> Signup and view all the answers

What ethical principle stresses that the patient be informed about decisions, and gives consent?

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

What is the primary goal of antibiotic stewardship programs?

<p>To limit inappropriate antibiotic use and improve clinical outcomes. (B)</p> Signup and view all the answers

Which of the following best describes a time-dependent antibiotic?

<p>Its efficacy is related to the duration that drug concentration is above the minimum inhibitory concentration (MIC). (B)</p> Signup and view all the answers

Oseltamivir (Tamiflu) is most effective when administered within what timeframe of influenza symptom onset?

<p>Within 48 hours. (B)</p> Signup and view all the answers

Which of the following is a common mechanism of action for inhaled medications used in asthma and COPD?

<p>Smooth muscle relaxation. (D)</p> Signup and view all the answers

Why is combination therapy required for the treatment of tuberculosis (TB)?

<p>To prevent the development of drug resistance. (C)</p> Signup and view all the answers

Which of the following directly describes the mechanism of action of corticosteroids in asthma and COPD treatment?

<p>Altering the expression of pro-inflammatory cytokines. (D)</p> Signup and view all the answers

Which of the following describes the function of pyrazinamide in the treatment of tuberculosis?

<p>Used during the first 2 months to shorten treatment duration. (A)</p> Signup and view all the answers

Which of the following properties describes concentration dependent antibiotics?

<p>Rate of killing bacteria increases with increased concentration (A)</p> Signup and view all the answers

What is the function of Ethambutol in TB treatment?

<p>Prevents rifampin resistance (B)</p> Signup and view all the answers

What is the therapeutic goal of Beta 2 agonists?

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

Which medication is typically considered first-line for managing hypertension in patients with heart failure?

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

A patient with heart failure and a history of angioedema should be monitored for which of the following adverse drug reactions when taking ACE inhibitors?

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

Which of the following antihypertensive medications is LEAST likely to be used in the treatment of heart failure?

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

Which of the following adverse effects is specifically associated with nitroprusside use, especially in patients with renal failure?

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

Which of the following is an example of an angiotensin II receptor blocker (ARB)?

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

A patient is prescribed amoxicillin-clavulanate (Augmentin) for a bacterial infection. What is the role of clavulanic acid in this combination?

<p>To prevent the breakdown of amoxicillin by beta-lactamases (A)</p> Signup and view all the answers

What is the most appropriate route of administration for vancomycin to treat a systemic infection?

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

A patient receiving vancomycin develops flushing, itching, and a rash. What is the MOST likely cause of these symptoms?

<p>Vancomycin flushing syndrome (C)</p> Signup and view all the answers

Which of the following beta-lactam antibiotics has the lowest risk of cross-reactivity in patients with a penicillin allergy?

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

Which of these medications is a direct renin inhibitor?

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

Which of the following antibiotics is typically used as a single-dose oral treatment for uncomplicated urinary tract infections (UTIs)?

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

Which of the following antibiotics is LEAST likely to cause a Clostridium difficile infection?

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

What condition would warrant the use of bacitracin?

<p>Topical skin infection (A)</p> Signup and view all the answers

Which beta-lactamase inhibitor is combined with piperacillin to form the antibiotic Zosyn?

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

Which of the following classes of antibiotics is generally considered safe to use during pregnancy and breastfeeding?

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

Flashcards

Pro-drug

An inactive drug that must be metabolized into its active form.

First pass metabolism

Metabolism of a drug in the liver before it reaches systemic circulation.

Half-life

The time required for half of a drug to be eliminated from the body.

Bioavailability

The proportion of a drug that enters the circulation when introduced into the body.

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Therapeutic index

The ratio of a drug's therapeutic effect to its toxicity.

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Steady state

Condition where drug absorption equals the amount eliminated.

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Phase I reaction

Metabolic reactions involving oxidation, reduction, or hydrolysis.

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Peaks and troughs

High and low levels of drug concentration in the blood.

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Angiotensin II Receptor Blockers (ARBs)

Medicines that block the effects of angiotensin II, lowering blood pressure.

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Common ADRs of ARBs

Adverse effects include angioedema, hyperkalemia, and renal decline.

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Direct Renin Inhibitors

Medications that block the enzyme renin to decrease blood pressure.

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ACE Inhibitors

Drugs that inhibit angiotensin converting enzyme to relax blood vessels.

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Mechanism of Action (MOA) of ARBs

Selective agents that block vasoconstrictive and aldosterone effects of angiotensin II.

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Phase I Drug Metabolism

The initial stage where drugs are converted to water-soluble metabolites or active compounds.

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Polar Molecule Groups

Chemical structures in drugs allowing them to skip Phase I metabolism.

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Phase II Drug Metabolism

The stage adding hydrophilic groups to drugs, making them more excretable.

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Pharmacodynamics (PD)

The study of drug effects and actions on the body via receptors.

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Agonist

A substance that activates a receptor to elicit a biological response.

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Antagonist

A substance that blocks receptors and prevents a biological response.

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Partial Agonist

A substance that binds to a receptor and partially activates it, often acting as an antagonist.

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Graded vs. Quantal Response

Graded response relates to dose, while quantal response indicates presence or absence of effect in a population.

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Neonates

Infants aged 0-28 days with unique physiological traits.

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Blood-Brain Barrier (BBB) in Neonates

Increased permeability of BBB increases drug absorption risks.

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Drug Absorption in Infants

Increased intestinal absorption leads to toxicity risk.

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Transdermal Absorption

Enhanced in infants, increasing risk with topical medications.

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Volume of Distribution (Vd)

Increased body fat in infants reduces Vd of lipophilic drugs.

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Protein Binding in Infants

Less protein binding until 10-12 months increases drug distribution.

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Phase II Metabolism in Infants

Reduced phase II metabolism leads to variable drug metabolism.

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Children 1 year and older

Pharmacokinetics become similar to adults with faster drug metabolism.

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Ethical Principle: Justice

Benefits and consequences of care should be equitable based on patient needs.

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Ethical Principle: Nonmaleficence

Commitment to do no harm when providing care.

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Minimum Bactericidal Concentration (MBC)

The lowest dose of an antibiotic that kills 99% of bacteria.

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Time Dependent Dosing

Effectiveness relies on the duration drug concentration is above the minimum inhibitory concentration (MIC).

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Concentration Dependent Dosing

Effectiveness is determined by peak concentration and the area under the curve.

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Antibiotic Stewardship

A system to optimize antibiotic use and limit resistance through data and policies.

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Oseltamivir (Tamiflu)

An antiviral neuraminidase inhibitor effective against influenza A and B if started within 48 hours.

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First-Line TB Therapy

Combination therapy for TB includes Rifampin and Isoniazid for best resistance prevention.

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Pyrazinamide in TB

Used in the first 2 months to shorten therapy duration to 6 months.

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Beta 2 Agonists

Medications that induce smooth muscle relaxation for bronchodilation in asthma and COPD.

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Corticosteroids MOA

Alter the expression of pro-inflammatory cytokines to reduce inflammation in lungs.

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ADRs of Inhaled Drugs

Adverse reactions including tolerance can occur with inhaled beta-2 agonists.

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Aldosterone antagonists

Medications that counteract aldosterone, used for hyperaldosteronism and heart failure.

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First line diuretics for HF

Medications used as a primary treatment for heart failure to remove excess fluid.

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Beta blockers

Medications that end in 'lol' used to manage heart failure by reducing heart rate.

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SGLT2 inhibitors

Medications ending in 'flozin' used for heart failure and diabetes management.

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Nitroprusside

A potent vasodilator used to quickly manage severe heart failure.

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Calcium channel blockers in HF

Medications not recommended for heart failure due to lack of benefit.

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Monitoring HF medications

Key elements include blood pressure, heart rate, urinary output, and kidney function.

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Common ADRs of HF medications

Side effects include hypotension, arrhythmias, and hyperkalemia among others.

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Penicillins

A class of antibiotics that inhibit cell wall synthesis, not given if patient has SJS/TEN.

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Vancomycin

An antibiotic given IV that can cause flushing syndrome; requires slow infusion.

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Cephalosporins

Antibiotics with a broader spectrum than penicillins, known for certain side effects.

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Beta-lactamase inhibitors

Medications that prevent the breakdown of beta-lactam antibiotics by bacteria.

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Study Notes

Exam 1 Blueprint

  • Students have 75 minutes for the exam

  • The blueprint outlines the approximate distribution of questions across different content areas of pharmacology

  • Pharmacokinetics/Pharmacodynamics (PK/PD) covers 9 questions

  • Pharmacokinetics (PK): the body's interaction with a drug.

    • Basic concepts include first-pass metabolism, half-life, bioavailability, and therapeutic index.
    • Absorption: how well the body takes up a drug
    • Distribution: how well the drug is transported to the site of action, including volume of distribution (Vd).
      • Vd: the amount of circulating drug in the body
      • Factors influencing distribution relate to the route of administration and blood flow
    • Metabolism: transforming drugs into a more water-soluble form to be excreted
      • usually involves the liver
      • Parent drug: the initial drug form
      • Pro-drug/inactive: Inactive form of drug that needs metabolism to become active
    • Elimination: how a drug is cleared from the body.
      • First-pass metabolism: hepatic metabolism before reaching the systemic circulation.

  • Half-life: time for half of the total drug to be eliminated from the body.

    • Longer half-life = stays longer in the body
    • Shorter half-life = quicker/more frequent dosing

  • Bioavailability: portion of the drug dose that reaches systemic circulation

  • Therapeutic index: ratio of dose causing undesirable effect to dose resulting in a desirable effect.

  • Steady state: amount of drug absorbed equals the amount eliminated. Reached at 3 to 5 half-lives.

Phase I and II Reactions

  • Phase I: non-synthetic reactions, involve oxidation, reduction, or hydrolysis (often via CYP enzymes) to create water-soluble/active metabolites

    • Drugs may skip phase I; Phase I reactions can convert inactive drugs to active ones.

  • Phase II: synthetic/conjugation reactions, adds hydrophilic groups to parent drugs to create more water-soluble and easily excreted metabolites

    • Usually involves glucuronidation.
    • Phase II reactions usually make a drug inactive.

Pharmacodynamics (PD)

  • Drug response: the reaction of the body to the drug.

    • Graded response: a continuous increase in response as dose increases
    • Quantal response: either present or absent response in a given population

  • Drug action: the interaction between a drug and a receptor

    • Agonist: elicits a response when binding to a receptor
    • Antagonist: blocks receptor binding to prevent a response
    • Partial agonist: partially activates a receptor, acting as an antagonist in the presence of a full agonist, thus reduces the response

Prescribing

  • P-drugs = first-line drug, well-tolerated
  • P-treatment: first-line, non-pharmacological approach: demonstrate calculation of correct pediatric doses, calculate initial dosages based on body surface area

Older Adults

  • Physiologic changes in older adults: decreased kidney function, absorption, metabolism, and excretion.

Pediatrics

  • Physiological variations (neonates, infants): permeability of the blood-brain barrier (BBB), intestinal and other absorption changes
  • Neonates & Infants: Clearance & other metabolic differences

Pharmacokinetics/Pharmacogenetics and CYP Enzymes

  • CYP enzymes: (Cytochrome P450) that metabolize many drugs.
    • Poor metabolizers (PM), have diminished CYP, will have more pronounced adverse effects
    • Extensive metabolizers (EM), have robust CYP, have more rapid metabolic reaction
    • CYP1, CYP2, CYP3: important enzymes involved in drug metabolism

Adverse Drug Reactions (ADRs)

  • Type I: Immediate, IgE-mediated (e.g., allergic reactions)
  • Type II: Cytotoxic, antibody-mediated (e.g., hemolytic anemia)
  • Type III: Immune complex-mediated (e.g., serum sickness)
  • Type IV: Cell-mediated (e.g., contact dermatitis)

Drug-drug interactions

  • Several factors influence this, including interactions between drugs through absorption, metabolism, distribution and excretion; interactions among medications.

Pharmacoeconomics

  • Deals with the economic value of health care outcomes
  • Factors involved include societal, insurance, healthcare organization, and the patient

Adherence

  • Adherence = ratio of prescribed drugs taken to the number of prescribed doses, MPR (medication possession ratio.)
  • Factors affecting adherence include personal beliefs, past history, economics, socioeconomic determinants of health
  • Improving adherence involves lowest number of daily doses, the least expensive medications with fewest side effects, open communication and a shared decision-making model.
  • Non-adherence can lead to negative health outcomes

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