Pharmacology of Quinidine
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Questions and Answers

What is the primary mechanism of elimination for the drug mentioned in the first point?

  • Hepatic metabolism (correct)
  • Biliary excretion
  • Respiratory excretion
  • Renal excretion

    • What is the therapeutic range of the drug mentioned in the first point?

  • 5-10 ug/ml
  • 2.3-5 ug/ml (correct)
  • 1-2 ug/ml
  • 10-15 ug/ml

    • What is a side effect of the drug mentioned in the second point?

  • Hypertension
  • Hypotension
  • Bradycardia (correct)
  • Tachycardia

    • What is the half-life of the drug mentioned in the first point?

    <p>6-8 hours</p> Signup and view all the answers

    What is the common formulation of the drug mentioned in the first point?

    <p>Quinidine sulfate and quinidine gluconate</p> Signup and view all the answers

    What is the mechanism of action of the drug mentioned in the second point?

    <p>Blocks potassium channels</p> Signup and view all the answers

    What is the therapeutic range of the drug mentioned in the second point?

    <p>1-2.5 ug/ml</p> Signup and view all the answers

    What is a unique feature of the drug mentioned in the second point?

    <p>It is an iodine-containing drug</p> Signup and view all the answers

    What percentage of Procainamide is bound to protein?

    <p>20%</p> Signup and view all the answers

    What is the hepatic metabolite of Procainamide?

    <p>N-acetyl procainamide (NAPA)</p> Signup and view all the answers

    What is the minimum dose of Procainamide that may prove effective when given intravenously?

    <p>200 mg</p> Signup and view all the answers

    What is the peak serum level of Procainamide after dosing?

    <p>One hour after the dose</p> Signup and view all the answers

    What is the therapeutic range of Procainamide?

    <p>4-8 ng/mL</p> Signup and view all the answers

    What is the half-life of Procainamide?

    <p>4 hours</p> Signup and view all the answers

    What is the mechanism of action of Verapamil?

    <p>Blocks L-type Ca channels</p> Signup and view all the answers

    What is the therapeutic range of Verapamil?

    <p>80-400 ng/mL</p> Signup and view all the answers

    What is the term for effects that cannot be explained?

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

    What is the primary use of Phenytoin?

    <p>Controlling tonic-clonic seizures</p> Signup and view all the answers

    What is the effect of Phenytoin on sodium and calcium influx?

    <p>It decreases sodium and calcium influx</p> Signup and view all the answers

    What is the therapeutic range of Phenytoin?

    <p>10-20 ug/ml</p> Signup and view all the answers

    What is the half-life of Ethosuximide?

    <p>40-60 hours</p> Signup and view all the answers

    What is the primary toxicity of Phenytoin?

    <p>Initiation of seizures</p> Signup and view all the answers

    What is the protein binding of Phenytoin?

    <p>87-97% bound</p> Signup and view all the answers

    What is the drug of choice for controlling petit mal seizures?

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

    What is the therapeutic level of trazadone?

    <p>2-15 ug/ml</p> Signup and view all the answers

    Which of the following organs require high dosage of Felbamate?

    <p>Heart, liver, and pancreas</p> Signup and view all the answers

    What is the half-life of Felbamate?

    <p>17-40 hours</p> Signup and view all the answers

    What is the major metabolite of Felbamate?

    <p>Desipramine and Nortriptyline</p> Signup and view all the answers

    What is the therapeutic dose of Felbamate?

    <p>300 mg/ml</p> Signup and view all the answers

    What is the toxic effect of Felbamate on the heart?

    <p>Cardiac arrhythmia</p> Signup and view all the answers

    Which of the following is an indication for the use of Felbamate?

    <p>All of the above</p> Signup and view all the answers

    What is the mechanism of action of Fluoxetine?

    <p>Blocks the reuptake of serotonin in central serotonergic pathways</p> Signup and view all the answers

    What is the primary toxic effect of overdosage of acetaminophen?

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

    What is the recommended timing for collecting trough concentration for therapeutic drug monitoring?

    <p>Right before the next dose</p> Signup and view all the answers

    What is the method of testing for acetaminophen levels?

    <p>All of the above</p> Signup and view all the answers

    What is the therapeutic dose of acetaminophen in mg/dL?

    <p>5 mg/dL</p> Signup and view all the answers

    What is the effect of acetaminophen on platelet aggregation?

    <p>Interference with platelet aggregation</p> Signup and view all the answers

    What is the common use of acetaminophen?

    <p>Analgesic and antipyretic</p> Signup and view all the answers

    What is the toxic dose of acetaminophen in mg/dL?

    <p>30 mg/dL</p> Signup and view all the answers

    What is the advantage of immunochemical methods in detecting drug levels?

    <p>Can detect drug levels in the nanomolar ranges</p> Signup and view all the answers

    Study Notes

    Anti-Arrhythmic Drugs

    • Quinidine: • 85% protein bound; eliminated by hepatic metabolism • Suppresses the conversion of T4 to T3; helpful in patients with thyrotoxicosis • Therapeutic range: 2.3 – 5 ug/ml • Toxic range: >5 ug/ml • Half-life: 6-8 hours • Common formulations: quinidine sulfate and quinidine gluconate • Peak serum level: 2 hours after an oral dose (sulfate); 4-5 hours for gluconate • Toxic effects: nausea, vomiting, abdominal discomfort, cardiovascular toxicity

    • Amiodarone (Cordarone): • Iodine-containing drug that can cause hypothyroidism or hyperthyroidism • Used to treat ventricular arrhythmias • Therapeutic range: 1 – 2.5 ug/ml • Toxic effects: bradycardia, hepatitis, photodermatitis • Blocks several channels (e.g., K+ and inactivated Na+ channels) and β-adrenoceptors • Often effective when other drugs have failed, but should be used sparingly due to serious side effects (e.g., photosensitivity, thyroid disorders, neuropathy, and pulmonary alveolitis)

    Class 3 Anti-Arrhythmic Drug

    • Sotalol: • Has both Class III and Class II (β-blocking) actions, but lacks the side-effects of amiodarone • Has the side-effects of β-blockers (e.g., increased ANA)

    Calcium Channel Blocker

    • Verapamil: • Used to treat angina, hypertension, and supraventricular arrhythmias • Blocks L-type Ca channels, especially on the AVN, where conduction is entirely dependent on Ca2+ spikes • Therapeutic range: 80-400 ng/ml • Toxic effects: hypotension, peripheral edema, ventricular fibrillation

    Other Anti-Arrhythmic Drugs

    • Disopyramide (Norpace): • Used to treat cardiac arrhythmias; used as a substitute for quinidine • Therapeutic range: 2-5 ug/ml • Toxic effects: nausea, vomiting, abdominal discomfort, cardiovascular toxicity • Half-life: 6-8 hours • Protein binding: 20-30%

    • Procainamide (Pronestyl, Procanbid, Procan SR): • Sodium channel blocker • Used to treat cardiac arrhythmia • Oral administration is the common route • GIT absorption is rapid and complete • 20% protein bound; eliminated by renal filtration and hepatic metabolism • Hepatic metabolite: N-acetylprocainamide (NAPA) • Therapeutic range: 4-8 ug/ml • Toxic effects: reversible lupus-like syndrome (Increase ANA), nephrotic syndrome, urticaria

    Anticonvulsant Drugs

    • Phenytoin: • Used to control seizures (tonic-clonic, simple partial seizures) and as a short-term prophylactic agent in brain injury • Decreases sodium and calcium influx into hyperexcitable neurons • IV administered; GIT absorption is incomplete • 87-97% protein bound; eliminated by hepatic pathway • Therapeutic range: 10-20 ug/ml • Toxic range: >20 ug/ml • Half-life: 6-24 hours • Major toxicity: initiation of seizures, teratogenic action (cleft lip & palate), vitamin D deficiency, folate deficiency

    • Ethosuximide (Zarontin): • Drug of choice for controlling petit mal (absence) seizure • Orally administered • Not protein bound • Therapeutic range: 40-100 ug/ml • Half-life: 40-60 hours • Toxic effects: GI disturbances, ataxia, SLE, aplastic anemia, pancytopenia

    Other Anticonvulsant Drugs

    • Felbamate (Felbatol): • Indicated for use in severe epilepsies – mixed seizure disorder, Lennox-Gaustat syndrome, adults with epilepsy • Orally administered – complete absorption of GIT • Half-life: 14-22 hours • Eliminated by renal and hepatic metabolism • Therapeutic dose: 30-60 ug/mL • Toxic effects: fatal aplastic anemia and hepatic failure

    • Other Anti-epileptic Drugs: • Therapeutic dose: 5 mg/dL • Side Effects: GI disturbances, interference with platelet aggregation • Toxic dose: >30 mg/dl • Toxic effects: mixed acid-base disturbance (metabolic acidosis and respiratory alkalosis), hypoglycemia, Reye syndrome

    Therapeutic Drug Monitoring (TDM)

    • Sample Collection: • Serum or plasma – specimen of choice • Timing of specimen collection: the single most important factor in TDM • Trough concentration drawn right before the next dose • Peak concentration drawn one hour after an orally administered dose (except digoxin)

    • Methods: • Immunochemical Methods (immunoassays) • Provides rapid analyses of blood and urine samples • Can detect drug levels in the nanomolar ranges

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    Description

    This quiz covers the properties and effects of quinidine, a medication used to treat thyrotoxicosis, including its protein binding, therapeutic range, and toxic effects.

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