GREEN PACOP BIOCHEM
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Questions and Answers

What is a consideration regarding the proper handling of Nitroglycerin tablets?

  • They are explosive in certain formulations
  • They are affected by temperature changes
  • They are sensitive to light (correct)
  • They are sensitive to humidity

    • Which of the following nitrovasodilators has a bioavailability of about 100%?

  • Amyl nitrite
  • Isosorbide dinitrate
  • Glyceryl trinitrate
  • Isosorbide mononitrate (correct)

    • What is the primary mechanism of action of nitrovasodilators?

  • Nitrate ion released upon denitrification stimulating the production of prostacylin
  • Denitrification by glutathione S-transferase leading to increase cGMP (correct)
  • Nitrate ion released upon denitrification directly stimulating outward K-channels
  • Denitrification by glutathione S-transferase leading to increase cAMP

    • Which of the following tissues exhibit the greatest sensitivity to nitrovasodilators at the lowest effective doses?

    <p>Myocardial tissues</p> Signup and view all the answers

    Why do sublingual tablets of Nitroglycerin lose their potency when stored in plastic containers?

    <p>Because they react with the plastic material</p> Signup and view all the answers

    What is the effect of denitrification of nitrovasodilators?

    <p>Release of nitrite ion, which is then converted to nitric oxide</p> Signup and view all the answers

    What is the effect of nitric oxide on vascular smooth muscles?

    <p>It leads to relaxation</p> Signup and view all the answers

    Which of the following is NOT a characteristic of Nitroglycerin tablets?

    <p>They are affected by temperature changes</p> Signup and view all the answers

    What is the substrate for the synthesis of cAMP?

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

    What is generated as a secondary messenger when a Beta-adrenoceptor is stimulated?

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

    What is the mechanism of action of Sildenafil?

    <p>Inhibits PDE leading to increase cGMP</p> Signup and view all the answers

    What ion's intracellular levels increase due to drugs that activate the phospholipase C-inositol phosphate system?

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

    What characterizes competitive antagonism?

    <p>Shift of the agonist log concentration-effect curve to the right without a change on the slope or amplitude</p> Signup and view all the answers

    What is the minimum dose that produces the maximum achievable response known as?

    <p>E-max</p> Signup and view all the answers

    What generates cAMP as a secondary messenger?

    <p>Adenylyl Cyclase</p> Signup and view all the answers

    What is the effect of stimulating a G-protein-linked receptor?

    <p>Generation of cAMP</p> Signup and view all the answers

    Which of the following substances is absorbed significantly by pinocytosis?

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

    What is the apparent lipid-water partition coefficient of the drug in the given scenario?

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

    What is the primary factor that determines the time to reach the steady-state concentration for a drug given at a constant rate?

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

    How much of the drug will remain in the body 12 hours after a single dose, given a biologic half-life of 4 hours?

    <p>25%</p> Signup and view all the answers

    What is the characteristic of a one-compartment model of drug behavior?

    <p>An AUC above the explored line that is less than 5% of the total AUC</p> Signup and view all the answers

    What is the required rate of infusion of Theophylline to achieve a desired plasma concentration of 10ug/mL in a 70kg patient?

    <p>0.6mL/minute</p> Signup and view all the answers

    What is the significance of the biologic half-life in pharmacokinetics?

    <p>It determines the time to reach the steady-state concentration</p> Signup and view all the answers

    What is the process by which the body eliminates a drug?

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

    What is the most important toxicity associated with pyrazolone derivatives like Phenylbutazone?

    <p>Hematologic toxicities</p> Signup and view all the answers

    Which NSAID is most useful as an analgesic and has been used to replace morphine in mild to moderate post-surgical pain?

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

    What is the primary advantage of drugs like Celecoxib and Etoricoxib?

    <p>Less incidence of gastric irritation or ulceration</p> Signup and view all the answers

    What is the primary reason for the withdrawal of certain COX-2 inhibitors from the market?

    <p>They increase the risk of thrombosis and cardiac deaths</p> Signup and view all the answers

    Which of the following agents is currently used as a first-line DMARD in the management of Rheumatoid Arthritis?

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

    What is a benefit of using Ketorolac with an opioid?

    <p>It decreases the opioid requirement by 25-50%</p> Signup and view all the answers

    What is a common adverse effect of NSAIDs?

    <p>Gastric ulceration</p> Signup and view all the answers

    Why were some NSAIDs withdrawn from the market?

    <p>They increase the risk of thrombosis and cardiac deaths</p> Signup and view all the answers

    What is the maximum serum level of Theophylline above which toxicities and side effects occur?

    <p>20mg/L</p> Signup and view all the answers

    Which group of individuals has a faster clearance of Theophylline?

    <p>Neonates, young infants, and adults</p> Signup and view all the answers

    What happens to the clearance of Theophylline among chronic smokers?

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

    What is the serum level of Theophylline above which seizures and arrhythmias are more common?

    <p>40mg/L</p> Signup and view all the answers

    What is true about the use of anti-cholinergic agents in COPD and bronchial asthma?

    <p>They are available as tertiary ammonium compounds</p> Signup and view all the answers

    What is the mechanism of action of Nedocromil?

    <p>Increase inward chloride conductance leading to hyperpolarization of mast cell membrane</p> Signup and view all the answers

    What is the mechanism of action of Zafirlukast and Montelukast?

    <p>Pharmacologic antagonism of Luekotriene D4 action</p> Signup and view all the answers

    What is not a characteristic of the use of anti-cholinergic agents in COPD and bronchial asthma?

    <p>They are more effective than beta-2 agonists in COPD</p> Signup and view all the answers

    Study Notes

    Pharmacology Study Notes

    Cyclic Adenosine Monophosphate (cAMP)

    • cAMP is generated as a secondary messenger by the action of the enzyme Adenylyl Cyclase
    • The substrate for the synthesis of cAMP is ATP (Adenosine Triphosphate)

    Beta-adrenoceptor Stimulation

    • Stimulation of Beta-adrenoceptor, a G-protein-linked receptor, involves the generation of a secondary messenger known as cAMP
    • This is in contrast to IP3 (Inositol Triphosphate), DAG (Diacylglycerol), and calcium ions, which are secondary messengers involved in other receptor stimulation

    Sildenafil (Viagra) Mechanism of Action

    • Sildenafil, a drug popularly known as Viagra, inhibits Phosphodiesterase (PDE) leading to an increase in cGMP (Cyclic Guanosine Monophosphate)

    Phospholipase C-Inositol Phosphate System

    • Activation of alpha-adrenergic agonists like phenylephrine primarily causes an increase in intracellular calcium ion levels

    Competitive Antagonism

    • Competitive antagonism is characterized by a shift of the agonist log concentration-effect curve to the right without a change in slope or amplitude
    • This is in contrast to other types of antagonism, which exhibit different effects on the agonist log concentration-effect curve

    Pharmacological Principles

    • Potency refers to the minimum dose that produces the maximum achievable response
    • ED50 (Effective Dose 50) is the dose required to produce 50% of the maximum response

    Drug Absorption and Distribution

    • Pinocytosis is a mechanism of absorption for certain substances, including Vitamin K and Cyanocobalamin
    • The apparent lipid-water partition coefficient of a drug can be calculated based on its concentration in an aqueous solution and octanol

    Pharmacokinetics

    • The rate of infusion of a drug to achieve a desired plasma concentration depends on the clearance of the drug
    • The biologic half-life of a drug determines the time it takes for the drug concentration to decrease by half
    • Compartmental analysis of serum drug concentration versus time plots can be used to determine the pharmacokinetic behavior of a drug

    Nitrovasodilators

    • Nitrovasodilators, such as nitroglycerin, have a bioavailability of about 100% when administered sublingually
    • The primary mechanism of action of nitrovasodilators involves the release of nitric oxide, which activates guanylyl cyclase leading to an increase in cGMP
    • Nitrovasodilators exhibit the greatest sensitivity in veins, followed by arterioles and arteries

    Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

    • Pyrazolone derivatives like Phenylbutazone are associated with hepatotoxicity and hematologic toxicities
    • Ketorolac is an NSAID that is useful as an analgesic and has been used successfully to replace morphine in some situations involving mild to moderate post-surgical pain
    • COX-2 inhibitors like Celecoxib and Etoricoxib have a lower incidence of gastric irritation or ulceration compared to traditional NSAIDs

    Disease Management

    • Methotrexate is currently used as a first-line DMARD (Disease-Modifying Anti-Rheumatic Drug) in the management of Rheumatoid Arthritis
    • Anti-cholinergic agents are used in COPD and bronchial asthma, but their use is limited due to side effects

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    Pharmacology Answer Key-PINK PACOP PDF

    Description

    This quiz assesses knowledge of physiology and biochemistry concepts, including hormone regulation and secondary messenger systems.

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