Pharmacokinetics Study Notes
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A 30-year-old pregnant woman, currently at 22 weeks gestation and with no known health issues, is planning a trip to Mozambique to visit her grandmother. During a prenatal check-up, the doctor prescribed mefloquine, a drug with high protein binding, for prophylaxis. What effects can be anticipated after the ingestion of this drug?

  • Shortened duration of action
  • High volume of distribution
  • Decreased drug interaction
  • Decreased glomerular filtration (correct)
  • What will be true regarding the termination of action of Paracetamol?

  • Paracetamol must only be excreted from the body to terminate its action
  • Hepatic metabolism and renal excretion are the two most important mechanisms involved (correct)
  • Metabolism of drugs always abolishes their pharmacologic activity
  • Distribution of the drug out of the bloodstream terminates its effects
  • A 33-year-old man complains of shoulder pain for four days, worsened by movement and preventing arm lifting. Abduction exacerbates the pain. He's otherwise healthy and stable. Given the option of oral medication, which drug is most likely to be absorbed effectively from the stomach mucosa?

  • Morphine sulfate
  • Aspirin
  • Naproxen
  • Diclofenac sodium (correct)
  • A 22-year-old male with sneezing, coughing, and shortness of breath for two weeks, worse in the morning and at night, presents to the physician. Bilateral wheezes are heard on auscultation, and various drug treatments with different administration routes are being considered. Which statement about the routes of administration in this patient is true?

    <p>Inhalation route is the most appropriate choice for delivering bronchodilators to relieve wheezing and shortness of breath.</p> Signup and view all the answers

    A 23-year-old male with a sore throat, cough, headache, and runny nose is prescribed amoxicillin-clavulanic acid. What primarily determines the maintenance dose of the medication for this patient?

    <p>Clearance of drug</p> Signup and view all the answers

    Which drug's poisoning causes an altered state of consciousness and hypotension, and needs to be treated via alkaline diuresis?

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

    A 34-year-old man arrives at the ER after a car accident, confused but stable. He has swelling on his forehead and a CT scan shows intracranial bleeding. The doctor gives him thiopentone to reduce pressure in his brain. Why does this drug work so quickly but only lasts for about 15 minutes?

    <p>Marked redistribution due to high lipid solubility</p> Signup and view all the answers

    A 52-year-old with severe right-sided flank pain was treated with tramadol, a weakly basic drug, which relieved his pain. An ultrasound revealed multiple calculi in his right kidney. What's true about the drug in this case?

    <p>It is excreted faster in acidic urine</p> Signup and view all the answers

    A 43-year-old man complained of headaches and neck pain for two months, with no other health issues reported. His blood pressure is 160/100 mm Hg. After a physical exam showing no abnormalities, the doctor prescribes a prodrug that acts for 24 hours. What drug was prescribed?

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

    A 16-year-old girl with breathing issues was given IV corticosteroids. Looking at the plasma concentration-time graph of the drug, what's true about its kinetics?

    <p>The rate of elimination is proportional to plasma concentration</p> Signup and view all the answers

    A 42-year-old man has foot tingling, a pale skin spot on his knee, fever, tiredness, and discomfort. The spot is less sensitive to touch and pinpricks. A biopsy confirms the condition. The doctor plans to prescribe a drug that may change dosage needs by inducing microsomal enzymes. What's the drug linked to the patient's condition?

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

    Aspirin follows zero order kinetics, at higher doses. This indicates which of the following properties?

    <p>Clearance decreases with an increase in plasma concentration</p> Signup and view all the answers

    Warfarin is an anti-coagulant medication with a low distribution volume, indicating which of the following?

    <p>The drug is not extensively distributed to tissues</p> Signup and view all the answers

    Which route would the doctor prefer to give the medication such that he can ensure 100% bioavailability?

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

    The drug nitroglycerine, if given via which of the following routes, will have a high first-pass metabolism?

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

    Which of the following statements about the given plasma concentration curve is correct?

    <p>The area under the curve is the extent of absorption</p> Signup and view all the answers

    Which of the following factors is affected by the bioavailability of the drug?

    <p>Dose of the drug</p> Signup and view all the answers

    A 48-year-old male reports palpitations and headaches for three months, without any other health issues. His vital signs show a heart rate of 111 beats/min and blood pressure of 165/100 mmHg. Atenolol is prescribed to manage symptoms without needing therapeutic dose monitoring. What's true about therapeutic drug monitoring (TDM)?

    <p>TDM can be done if the drug has erratic pharmacokinetics</p> Signup and view all the answers

    Which of the following drugs is given by the route shown in the figure?

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

    A 53-year-old man complains of cough, weakness, and fever for four days. Pneumonia is diagnosed, and gentamicin is part of the treatment plan. Gentamicin has a half-life of 2-3 hours but can accumulate in the kidney with prolonged dosing, leading to a prolonged half-life of 53 hours. What type of half-life is this?

    <p>Terminal half-life</p> Signup and view all the answers

    A 45-year-old male patient presents to the emergency department with ST-elevation myocardial Infarction. The attending physician immediately started treatment with aspirin, propranolol, clopidogrel, and atorvastatin. Which of these are metabolized by CYP2D6?

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

    Metabolism of drugs occurs in the liver in 2 phases. The first phase involves catabolic reactions, and the second phase involves synthetic reactions that increase drug elimination. Which of the following reactions is a phase 1 reaction?

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

    A 15-year-old girl arrived at the ER after ingesting 15 tablets of an unknown drug, causing altered mental status, rapid breathing, and vomiting. To treat drug toxicity, various methods can remove the drug from the body, such as dialysis. Which drug, when toxic, is eliminated through urine acidification?

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

    A 45-year-old man with asthma was admitted to the hospital for breathing problems and coughing. He was given two drugs, A and B, intravenously every 24 hours for 6 days. What does the graph showing the concentration of these drugs in the blood over time reveal?

    <p>Drug A does not maintain persistent therapeutic levels when administered every 24 hours</p> Signup and view all the answers

    A 50-year-old male underwent orthopedic surgery a few days ago. He has been given a transdermal patch of fentanyl for postoperative pain relief. Which of the following is the advantage of transdermal application?

    <p>They avoid the hepatic first-pass metabolism of the drug</p> Signup and view all the answers

    Which of the following drugs has the highest volume of distribution?

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

    A 40-year-old man comes to the outpatient department with a fever, cough, and difficulty breathing for three days. During the exam, coarse crepitation is heard in his left lower chest. He's prescribed azithromycin 500mg once daily. Which parameter from a plasma concentration vs time graph best indicates the drug's absorption rate?

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

    A 56-year-old patient with heart failure currently on digoxin therapy presents to the emergency department with blurred vision and yellow-green distortion. The plasma digoxin level is 4 ng/ml(normal 0.8- 2.0). Renal function is normal; this patient's plasma t1/2 for digoxin is 1.6 days. How long should digoxin be withheld to reach a safer yet probably therapeutic level of 1 ng/ml?

    <p>3.2 days</p> Signup and view all the answers

    If 4g of antibiotic is administered and its peak plasma concentration is found to be 50 µg/ml, what will be the volume of distribution of the drug?

    <p>80 L</p> Signup and view all the answers

    A 51-year-old woman with hypertension & Type 2 DM has wrist pain, morning stiffness, and joint abnormalities. She has high RF titers and positive anticitrullinated protein antibodies. She's prescribed a renal tubule-secreted drug. Assuming renal clearance, what is the likely clearance of the drug?

    <p>More than the GFR</p> Signup and view all the answers

    Which of the following statements best describes the pKa of a drug?

    <p>pKa of a drug is the pH at which the drug is 50% ionised</p> Signup and view all the answers

    A 38-year-old male patient arrives at the emergency department after consuming morphine for 6 hours. His respiratory rate is 12 breaths per minute, and he has bilateral pinpoint pupils. The plasma half-life of morphine is 3 hours, with a volume of distribution (Vd) of 200 L. The current plasma concentration of morphine is 0.5 mg/L. What is the initial dose of morphine consumed by the person?

    <p>400 mg</p> Signup and view all the answers

    Certain drugs, such as chloroquine, require a high-loading dose followed by regular maintenance doses. Which of the following factors does this loading dose depend on?

    <p>Volume of distribution</p> Signup and view all the answers

    Therapeutic monitoring of the plasma level of the drug is done when the drug's response cannot be measured. Which of the following drugs would not require therapeutic dose monitoring?

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

    Avoid which laxative in a 7-year-old child with constipation and a history of rheumatic fever on erythromycin prophylaxis due to the risk of arrhythmia?

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

    A 5 ml ampoule containing 5 mg/ml NTG. One ampoule is added to normal saline to make a total of 500 ml solution. Calculate the infusion rate if NTG is required at ten mcg/min. (Consider 1 micro drip = 60 drops/mL)

    <p>12 drops/min</p> Signup and view all the answers

    Which of the following statements best describes drug distribution?

    <p>Plasma protein binding affects drug distribution</p> Signup and view all the answers

    A 57-year-old man is in the CCU post-treatment for ST-elevation myocardial infarction. Which of the following antiplatelet drugs might cause unexpected results based on the CYP2C19 genotype of the patient?

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

    Study Notes

    Pharmacokinetics Study Notes

    • Drug Absorption: Drugs absorbed from the stomach mucosa are often lipid-soluble and non-ionized. Diclofenac sodium is an example.
    • Drug Elimination: Paracetamol is primarily eliminated through hepatic metabolism and renal excretion.
    • Routes of Administration: Inhalation is the preferred route for bronchodilators to treat respiratory issues like wheezing and shortness of breath.
    • Maintenance Dose: The maintenance dose of a drug is primarily determined by its clearance from the body.
    • Drug Poisoning & Treatment: Phenobarbital poisoning requires alkaline diuresis as a treatment.
    • Drug Action Duration: Thiopentone's rapid action (15 seconds) and short duration (15 minutes) are due to high lipid solubility and resulting redistribution.
    • Drug Excretion in Urine: Tramadol, a weakly basic drug, is excreted faster in acidic urine.
    • Drug Metabolism: Glucuronidation is the most common phase II drug metabolic reaction, making drugs water-soluble for excretion.
    • Prodrug: Enalapril, a prodrug, exerts its action for 24 hours.
    • Drug Kinetics: Drugs following first-order kinetics have a constant half-life, while those following zero-order kinetics have a variable half-life.

    Specific Examples & Concepts

    • Mefloquine: High protein binding of mefloquine leads to decreased glomerular filtration and prolonged duration of action, impacting drug interactions.
    • Absorption: Factors like lipid solubility, ionization at physiological pH, and presence of tissue-specific transporters affect drug absorption.
    • Bioavailability: The intravenous route ensures 100% bioavailability, while oral administration can be affected by first-pass metabolism and variability. Nitroglycerin, given orally, has high first-pass metabolism.
    • Volume of Distribution (Vd): A low Vd, like warfarin, indicates limited distribution into tissues. Chloroquine has a high volume of distribution.
    • Plasma Concentration-Time Graphs: The area under the curve (AUC) represents the extent of absorption. Tmax is the time taken to reach the maximum concentration (Cmax)
    • Therapeutic Drug Monitoring (TDM): TDM is used for drugs with a narrow therapeutic index or erratic pharmacokinetics which cannot be monitored easily by simple tests.
    • Enzyme Inducers: Rifampicin is an enzyme inducer.
    • Zero-order Kinetics: Aspirin, at higher doses, exhibits zero-order kinetics, where the rate of elimination is independent of plasma concentration.
    • Drug Half-Life (t½): Gentamicin's half-life can vary significantly depending on prolonged dosing in the kidneys resulting in a so called terminal half-life.
    • CYP Enzymes: Certain drugs are metabolized by specific CYP enzymes (e.g., Propranolol by CYP2D6, warfarin by CYP2C9). Genetic variations in CYP enzymes can affect drug metabolism.
    • Acidification/Alkalinization of Urine: Acidification or alkalinization of urine is used to enhance excretion of certain drugs, such as weak acids or weak bases, to treat poisoning or toxicity.
    • Calculating Infusion Rates & Drug Concentrations: Examples are given where calculations using the drug concentration, volume, and desired infusion rate can be performed to calculate the required infusion rate.

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    Description

    Explore key concepts in pharmacokinetics, including drug absorption, elimination, and routes of administration. This quiz covers critical topics such as maintenance dosage, drug poisoning treatments, and metabolic reactions. Test your understanding of how drugs interact with the body and their physiological effects.

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