Pharmacology: Analgesics and Anti-inflammatory Drugs
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Questions and Answers

Which of the following best describes the mechanism of action of pyrantel pamoate?

  • It increases the muscular activity of the adult worms, causing them to detach and be expelled from the body.
  • It directly inhibits cholinesterase, causing muscle contractions in the worms.
  • It inhibits the growth and development of pinworm larvae, preventing them from reaching adulthood.
  • It acts as a depolarizing neuromuscular agent, stimulating acetylcholine release and inhibiting cholinesterase, leading to paralysis. (correct)

    • According to the content provided, what is a key concern when using antacids relating to drug interactions?

  • Antacids do not cause drug interactions, and are safe to take with any other medication.
  • Antacids cause the stomach pH to decrease, leading to increased absorption of some medications.
  • Antacids decrease the rate of metabolism of most drugs, causing increased plasma concentrations.
  • Antacids increase the gastric pH, which can alter the absorption and effectiveness of some drugs. (correct)

    • What is the maximum dose of pyrantel base that should be administered to a child or adult, according to the provided text?

  • There is no maximum dose listed in this text
  • 11 grams
  • 11 mg/kg
  • 1 gram (correct)

    • What is the primary mechanism of action for azole antifungals, such as clotrimazole, miconazole, and tioconazole, in treating vulvovaginal candidiasis?

    <p>They inhibit the synthesis of ergosterol by blocking the CYP450 enzymes, which is essential for fungal cell membrane synthesis. (C)</p> Signup and view all the answers

    Which of the following is true regarding the interaction between codeine and dextromethorphan based on the content provided?

    <p>Codeine is the prodrug, whereas dextromethorphan is an active compound. (C)</p> Signup and view all the answers

    Which of the following best describes the effect of CYP2D6 inhibitors on codeine?

    <p>They reduce the effect of codeine. (B)</p> Signup and view all the answers

    Why does dextromethorphan not have analgesic properties, unlike codeine?

    <p>It is a different enantiomer from its analog of levorphanol. (B)</p> Signup and view all the answers

    Which of the following is the primary pharmacological action of guaifenesin?

    <p>It thins mucus in the lower respiratory tract. (A)</p> Signup and view all the answers

    A patient with mild renal impairment is prescribed calcium carbonate as an antacid. What might be a potential concern with long term use?

    <p>Increased risk of renal calculi. (D)</p> Signup and view all the answers

    Which medication is known to cause antiandrogenic effects, such as decreased libido and gynecomastia in men?

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

    Which of the following medications would have an interaction with citalopram due to its inhibition of the CYP2C19 enzyme?

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

    What is the approximate onset of action for H2 receptor antagonists such as famotidine?

    <p>30-45 minutes (A)</p> Signup and view all the answers

    Concurrent use of which medication class alongside dextromethorphan is most likely to increase the risk of serotonergic effects?

    <p>Selective Serotonin Reuptake Inhibitors (SSRIs) and Monoamine Oxidase Inhibitors (MAOIs) (C)</p> Signup and view all the answers

    Acetaminophen's mechanism of action involves which detoxification process?

    <p>Glutathione-dependent conjugation (D)</p> Signup and view all the answers

    A patient with a history of a bleeding disorder should not take which of the following medications?

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

    Which of the following medications poses the highest risk of hypertension when used with linezolid?

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

    Which of the following is a common side effect associated with first-generation antihistamines such as diphenhydramine?

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

    Which second-generation antihistamine is known for causing the most sedation?

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

    Intranasal corticosteroids like fluticasone work by inhibiting multiple cell types and mediators, impacting which of the following processes?

    <p>The allergic cascade (D)</p> Signup and view all the answers

    A deficiency in which of the following vitamins is a contraindication for aspirin use?

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

    The use of intranasal corticosteroids over a long period of time has been linked with what potential adverse effect?

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

    Which medication must be used one week prior to allergen exposure to be considered effective?

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

    Codeine's antitussive action primarily occurs through its effect on which part of the brain?

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

    Which of the following best describes the primary function of ergosterol?

    <p>A fungal sterol found in the cell membrane. (D)</p> Signup and view all the answers

    For pregnant women experiencing vaginal itching and irritation, which of the following treatment durations is generally advised?

    <p>7 days. (A)</p> Signup and view all the answers

    An individual experiencing overactive bladder is prescribed oxybutynin patches. What is the primary mechanism of action of this medication?

    <p>An anti-cholinergic that block muscarinic receptors reducing bladder contractions. (C)</p> Signup and view all the answers

    A topical analgesic product contains 2-16% menthol and 3.2% camphor. What sensation is typically expected from the application of this product?

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

    Which vitamin deficiency is most closely associated with macrocytic anemia?

    <p>Vitamin B12 (D)</p> Signup and view all the answers

    Folic acid is crucial for preventing which condition?

    <p>neural tube defects. (C)</p> Signup and view all the answers

    Which vitamin, when used topically can help minimize the appearance of scars?

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

    Besides heart health, Coenzyme Q10 is also useful in what condition?

    <p>reducing statin associated adverse effects. (A)</p> Signup and view all the answers

    A patient with a diagnosis of hypertriglyceridemia asks about supplements. Which would be the most suitable product to recommend?

    <p>Fish Oil. (B)</p> Signup and view all the answers

    Which of the following is paired correctly?

    <p>Valerian root : Anxiety. (C)</p> Signup and view all the answers

    Which herbal supplement is primarily associated with the treatment of depression, anxiety, and OCD?

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

    What is a significant adverse effect associated with the use of Kava?

    <p>Severe liver damage (D)</p> Signup and view all the answers

    Which group of supplements are known for potentially reducing the duration of colds?

    <p>Echinacea, Sambucus nigra, vitamin C and zinc (B)</p> Signup and view all the answers

    What is the primary function of probiotics?

    <p>Restoring GI flora. (D)</p> Signup and view all the answers

    Which of the following is a primary therapeutic use of Saw Palmetto?

    <p>Benign Prostatic Hyperplasia (BPH) (C)</p> Signup and view all the answers

    Black cohosh is primarily used for which of the following?

    <p>Menopausal and premenstrual symptoms (D)</p> Signup and view all the answers

    Evening primrose oil is primarily used to manage which conditions?

    <p>Premenstrual syndrome (PMS) and menopause (C)</p> Signup and view all the answers

    Based on the information available, with which type of drugs are interactions most likely to occur?

    <p>Antidepressants and blood thinners + herbal supplements (D)</p> Signup and view all the answers

    According to gastroenterologists, what kind of probiotics are preferred?

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

    A patient presents with symptoms of BPH. Which of these herbal supplements should be considered?

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

    Flashcards

    Acetaminophen (APAP)

    A common analgesic used for mild-moderate pain and fever reduction. Metabolized by CYP450 and detoxified by glutathione during Phase II conjugation.

    NSAIDs

    A group of drugs that inhibit prostaglandin synthesis from arachidonic acid by blocking both COX-1 and COX-2 enzymes.

    Acetylcysteine

    An antidote used to treat acetaminophen overdose.

    Pseudoephedrine

    A decongestant that directly binds and displaces norepinephrine from storage vesicles and pre-junctional nerve terminals.

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    1st Generation Antihistamines

    First-generation antihistamines that are more sedating due to their anticholinergic, antiserotonin and anti-alpha-adrenergic effects.

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    2nd Generation Antihistamines

    Second-generation antihistamines that are generally less sedating than first-generation antihistamines.

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    Intranasal Corticosteroids

    Intranasal corticosteroids that inhibit the release of multiple inflammatory mediators, including histamine, and can effectively stop the allergic cascade.

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    Cromolyn Sodium

    A mast cell stabilizer that must be used at least one week before exposure to allergens for maximum effect.

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    Codeine

    A prodrug antitussive that acts centrally on the medulla to increase the cough threshold.

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    Mast Cell Stabilizers

    A group of drugs that inhibit the release of mast cell mediators, may decrease cellular recruitment, and have a slower onset of action than first-generation antihistamines.

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    Codeine Metabolism

    Codeine is a prodrug, meaning it needs to be metabolized by the body to become active. Poor metabolizers may not benefit from codeine because they don't convert it effectively.

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    Codeine Over-metabolism

    Extensive metabolizers are at an increased risk for sedation and respiratory depression when taking codeine.

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    Dextromethorphan: How it works

    Dextromethorphan is a cough suppressant that works by blocking the action of certain chemicals in the brain that cause coughing.

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    Dextromethorphan Drug Interactions

    Dextromethorphan can interact with certain medications, including SSRIs and MAOIs, increasing the risk of side effects like serotonin syndrome.

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    Guaifenesin: Expectorant

    Guaifenesin is an expectorant, which means it helps to loosen mucus in the lungs and make it easier to cough up.

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    Antacids

    Antacids work by neutralizing stomach acid, providing temporary relief from heartburn and indigestion. Each type has different properties and potential side effects.

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    H2 Receptor Blockers

    H2 Receptor Blockers, like cimetidine and famotidine, work by blocking the action of histamine in the stomach. This reduces acid production and provides relief from heartburn and ulcers.

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    Proton Pump Inhibitors (PPIs)

    Proton Pump Inhibitors (PPIs) are powerful medications that block the production of stomach acid, providing long-lasting relief from heartburn and ulcers.

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    What is a prodrug?

    A drug that requires metabolic conversion to become active. For example, codeine is metabolized by CYP2D6 to morphine, which is the active form.

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    How does stomach pH impact drug interactions?

    Increasing the acidity of the stomach can cause more drug interactions because it changes the way some medications are absorbed.

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    How does Pyrantel pamoate (Pin-X) treat pinworms?

    Pyrantel pamoate is an anti-parasitic medication that works by paralyzing the worms and causing them to be passed out in the stool.

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    Compare codeine and dextromethorphan.

    Codeine is a prodrug meaning it needs to be activated by CYP2D6 to become morphine. Dextromethorphan is an active drug. Both interact significantly with the CYP2D6 enzyme.

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    What are the maximum daily dosages of acetaminophen, ibuprofen, and naproxen for adults and pediatrics?

    Acetaminophen (paracetamol) is an analgesic and antipyretic. It is limited to a maximum of 1000mg for adults and 30mg/kg for children (up to 3000mg). Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) with a maximum of 800mg for adults. Naproxen is another NSAID with a maximum of 1250mg for adults but is not recommended for children.

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    Ergosterol

    A type of fungal sterol found in the cell membranes of fungi.

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    Hydrocortisone 1%

    A topical medication used to treat vaginal itching and irritation. It is a corticosteroid that reduces inflammation.

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    Benzocaine 5 to 10%

    A topical medication used to treat vaginal itching and irritation. It is a local anesthetic that numbs the area.

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    Oxybutynin patches

    A medication used to treat overactive bladder. It works by blocking the action of acetylcholine at the bladder muscle.

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    Anti-muscarinic drugs

    A class of drugs that block the action of acetylcholine at the muscarinic receptors.

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    Overactive bladder

    A condition characterized by frequent urination, urgency, and sometimes incontinence.

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    Anemia

    The condition of having a decreased number of red blood cells, which carry oxygen to the body's tissues.

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    Macrocytic anemia

    A type of anemia characterized by the presence of abnormally large red blood cells.

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    Microcytic anemia

    A type of anemia characterized by the presence of abnormally small red blood cells.

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    Osteoporosis

    A condition in which bone density is reduced, making bones weak and prone to fractures.

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    St. John's Wort

    A plant extract used to treat depression, anxiety and OCD.

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    Kava

    A plant extract often used to treat mild anxiety and insomnia. Can cause severe liver damage if used incorrectly.

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    Echinacea

    A plant extract often used to support the immune system, potentially reducing the duration of cold symptoms.

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    Sambucus Nigra (Elderberry)

    A plant extract often used to support the immune system and may have antiviral properties, potentially reducing the duration of cold symptoms.

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    Probiotics

    Living microorganisms taken orally that can benefit the host by restoring normal gut flora.

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    Saw Palmetto

    A plant extract used to treat benign prostatic hyperplasia (BPH) in men.

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    Black Cohosh

    A plant extract used to treat premenstrual syndrome, dysmenorrhea, and menopause symptoms in women.

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    Evening Primrose Oil

    A plant oil used to treat premenstrual syndrome and menopause symptoms in women.

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    Herbal Supplement Interactions

    Potential drug interactions with herbal supplements are most likely to occur with antidepressants and blood thinners.

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    Herbal Supplements vs. Conventional Medicine

    Herbal supplements should not be used as a substitute for conventional medical treatment.

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    Evidence for Herbal Supplements

    The benefits of herbal supplements are not always backed by scientific evidence.

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    Study Notes

    Analgesics and Antipyretics

    • APAP (Acetaminophen): Metabolized by CYP450 and detoxified by glutathione (Phase II conjugation).
    • Adverse effects in adults: nausea, vomiting, headache, insomnia. Adverse effects in children: nausea, vomiting, constipation, pruritus, agitation. Hepatotoxicity is associated with acute liver failure, sometimes resulting in liver failure or death. Injury occurs when the recommended maximum daily limit is exceeded.
    • Acetylcysteine is the antidote.

    Nonsteroidal Anti-inflammatory Drugs (NSAIDs)

    • Adverse effects: gastrointestinal ulcers, perforation, bleeding, increased risk of myocardial infarction (MI), heart failure (HF), hypertension (HTN), stroke, sodium and water retention causing edema.
    • Methotrexate clearance is decreased.
    • P2Y12 inhibitors and SSRIs increase the risk of bleeding.
    • Bisphosphonates increase the risk of gastrointestinal bleeding and ulcers.

    Anti-inflammatory Drugs

    • ASA (Acetylsalicylic Acid): Inhibits prostaglandin synthesis from arachidonic acid by inhibiting both isoforms of the COX enzyme (COX-1 and COX-2). Contraindicated in patients with vitamin K deficiency, bleeding disorders, or children with influenza or chicken pox (due to Reye's syndrome risk). Similar to NSAIDs.
    • Similar to NSAIDs. Valproic acid displacement from protein binding sites and inhibition of valproic metabolism is noted.
    • Sulfonylureas increase the risk of hypoglycemia.

    Antihistamines

    • Diphenhydramine (1st gen): Sedating. Competes with histamine at central and peripheral histamine type 1 receptor sites, preventing histamine receptor interaction and subsequent mediator release.
    • Chlorpheniramine: Same mechanism as diphenhydramine.
    • Doxylamine: Same mechanism as diphenhydramine and chlorpheniramine.
    • Loratadine (2nd gen): Non-sedating. Inhibits release of mediators like histamine.
    • Cetirizine (2nd gen): Non-sedating. Inhibits release of mediators.

    Other Drugs

    • Pseudoephedrine/Sudafed: Decongestant. Acts as a direct binding and displacement of norepinephrine from storage.

    Corticosteroids

    • Budesonide, Fluticasone, Triamcinolone (intranasal corticosteroids): Inhibit multiple cell types and mediators, including histamine.

    Mast Cell Stabilizers

    • Cromolyn sodium: Mast cell stabilizer used to prevent exposure to allergens, blocks calcium influx into mast cells.

    Opioid Analgesics

    • Codeine: Prodrug. Metabolized to morphine by CYP2D6.
    • Dextromethorphan: Active compound, not a prodrug. Metabolized by CYP2D6. A cough suppressant.
    • CYP2D6 interactions are important to note for both drugs.

    Other OTC Medications

    • Guaifenesin (Mucinex): Expectorant/loosens respiratory secretions.
    • Mucinex D (guaifenesin + pseudoephedrine): Combination product.
    • Mucinex DM (guaifenesin + dextromethorphan): Combination product.
    • Antacids (for example: Aluminum-based and magnesium-based antacids).
    • Cimetidine, Famotidine, Omeprazole, Esomeprazole, Lansoprazole. Proton Pump Inhibitors (PPIs).
    • Pyrantel pamoate (Pin-X): Treats pinworms.

    Other

    • Echinacea, Sambucus nigra (elderberry), vitamin C, prophylactic and treatment of colds, can reduce the length of infection.
    • Probiotics: Gastrointestinal flora restoration.
    • Saw Palmetto, Black Cohosh, Evening primrose oil: Used for various conditions, primarily in women.
    • Important: Drug interactions are possible with antidepressants and blood thinners.

    Other specifics

    • OTC drugs are mentioned—it's important to review specific dosage recommendations for various age groups as noted in the text.

    Additional Notes from the Text

    • Various interactions are mentioned—interactions with other drugs should be referenced when considering use of these drugs to avoid adverse outcomes.

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    Description

    This quiz covers key concepts regarding analgesics, antipyretics, and anti-inflammatory drugs, including their metabolism, adverse effects, and interactions. Understand the implications of drug overdose and the use of antidotes, specifically acetylcysteine for acetaminophen toxicity. Assess your knowledge of nonsteroidal anti-inflammatory drugs (NSAIDs) and their potential complications.

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