Pharmacology of Cushing's Syndrome and Acetaminophen
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Questions and Answers

What is the primary adverse effect associated with Ketoconazole?

  • Kidney damage
  • Liver toxicity (correct)
  • Hepatic necrosis
  • CNS toxicity

    • Which drug is used specifically as a diagnostic tool rather than for treatment?

  • Ketoconazole
  • Miotrate
  • Acetaminophen
  • Metyrapone (correct)

    • What is a common outcome of an acetaminophen overdose?

  • Seizures
  • Hepatotoxicity (correct)
  • Respiratory depression
  • Kidney failure

    • Which opioid is known for being 80-100 times more potent than morphine?

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

    What is the mechanism of action for Rofecoxib?

    <p>COX 2 inhibitor</p> Signup and view all the answers

    What is the recommended treatment for acetaminophen overdose?

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

    Which medication produces both physical and psychological dependence and poses a risk of life-threatening withdrawal?

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

    Which drug is classified as a kappa agonist and is used in emergency medical services?

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

    What effect does codeine have in relation to morphine?

    <p>It converts into morphine in a percentage of patients</p> Signup and view all the answers

    What is the most serious side effect of long-term use of corticosteroids?

    <p>Adrenal suppression</p> Signup and view all the answers

    What is the mechanism of action of dispositional tolerance?

    <p>Increased enzyme production in the liver requiring more drug</p> Signup and view all the answers

    Which type of antiacid is known to change the pH of the blood?

    <p>Systemic antiacids</p> Signup and view all the answers

    Which class of drugs is effective in suppressing stomach acid by blocking H2 receptors?

    <p>H2 receptor blockers</p> Signup and view all the answers

    What is a unique caution related to potassium competitive acid blockers?

    <p>They should not be given to HIV patients</p> Signup and view all the answers

    What is the major side effect of cimetidine, an H2 receptor blocker?

    <p>High risk for drug-drug interactions</p> Signup and view all the answers

    Which laxative type irritates the GI mucosa to promote peristalsis?

    <p>Irritant/stimulant laxatives</p> Signup and view all the answers

    What is the primary function of sucralfate in the treatment of peptic ulcer disease (PUD)?

    <p>Form a protective barrier over ulcers</p> Signup and view all the answers

    Which formulation of laxatives requires adequate water intake to be effective and avoid worsening symptoms?

    <p>Bulk laxatives</p> Signup and view all the answers

    What is the main advantage of using proton pump inhibitors over other acid-reducing drugs?

    <p>They reduce gastric acid secretion by 98% in 48 hours</p> Signup and view all the answers

    Which type of laxative is typically used to purge the intestine and acts quickly within 1-3 hours?

    <p>Saline and osmotic laxatives</p> Signup and view all the answers

    What is a significant adverse effect associated with ketoconazole?

    <p>Liver toxicity</p> Signup and view all the answers

    What therapeutic use is NOT applicable to metyrapone?

    <p>Cushing syndrome treatment</p> Signup and view all the answers

    Which of the following drugs is used to counteract acetaminophen overdose?

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

    What is the mechanism of action of miotrate?

    <p>Destruction of adrenal cortical cells</p> Signup and view all the answers

    Which opioid is known for having a short duration and is not associated with meiosis?

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

    Which opioid is specifically utilized for treatment of opioid and alcohol dependence?

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

    What adverse effect can be caused by high doses of acetaminophen or its use alongside alcohol?

    <p>Hepatic necrosis</p> Signup and view all the answers

    Which drug class presents a risk of life-threatening dependence and overdose effects like decreased heart rate?

    <p>Sedative hypnotics</p> Signup and view all the answers

    What is a unique effect of buprenorphine compared to full mu agonists?

    <p>Partial mu agonist activity</p> Signup and view all the answers

    Which cannabinoid receptor is primarily located in the brain?

    <p>CB1</p> Signup and view all the answers

    What is the primary function of antiacids?

    <p>Directly neutralize stomach acid</p> Signup and view all the answers

    What distinguishes proton pump inhibitors from other acid-reducing drugs?

    <p>They can completely block acid secretion in the stomach.</p> Signup and view all the answers

    What is a characteristic of behavioral tolerance related to alcohol use?

    <p>Physical adaptation to alcohol effects</p> Signup and view all the answers

    Which type of laxative is known to take days to exert its effect?

    <p>Bulk laxatives</p> Signup and view all the answers

    Why should potassium competitive acid blockers be avoided in HIV patients?

    <p>There is no evidence of their effectiveness in this population.</p> Signup and view all the answers

    Which of the following statements about H2 receptor blockers is true?

    <p>They can suppress gastric acid secretion for up to 70% in 24 hours.</p> Signup and view all the answers

    What is a notable feature of saline and osmotic laxatives?

    <p>They can effectively purge the intestine in 1-3 hours.</p> Signup and view all the answers

    What role does sucralfate play in treating peptic ulcer disease?

    <p>It coats ulcers to protect them while healing occurs.</p> Signup and view all the answers

    Which of the following laxative types irritates the GI mucosa to promote peristalsis?

    <p>Irritant/stimulant laxatives</p> Signup and view all the answers

    What is a significant concern with cimetidine among H2 receptor blockers?

    <p>It increases estrogen levels and has drug interaction risks.</p> Signup and view all the answers

    Study Notes

    Ketoconazole

    • MOA: Blocks adrenal gland enzymes, inhibiting cortisol production; antifungal.
    • Therapeutic use: Cushing's syndrome.
    • Adverse effects: Liver toxicity; alters sex hormone and steroid synthesis.

    Metyrapone

    • NOT for treatment, used as a diagnostic tool.
    • Therapeutic use: Cushing's syndrome.
    • Adverse effects: Toxicity.

    Mitotane

    • MOA: Destroys adrenal cortex.
    • Adverse effects: GI, CNS toxicity, adrenal crisis.

    Acetaminophen

    • Analgesic and antipyretic; not anti-inflammatory.
    • Uses: Headache (not migraine), osteoporosis, fever (especially in children).
    • MOA: Unknown.
    • Absorption: GI tract.
    • Peak concentration: 20-30 minutes.
    • Half-life: 2 hours.
    • Metabolism: Liver → sulfates and glucuronides.
    • Elimination: Delayed by liver issues.
    • Low adverse effects; rare pseudoallergic reactions.
    • High doses/alcohol use: Risk of hepatic necrosis (especially in elderly).
    • Overdose treatment: Acetylcysteine.

    Acetaminophen Overdose

    • Symptoms (24 hours post-overdose): Nausea, vomiting, anorexia, abdominal pain.
    • Jaundice (2-4 days post-overdose).
    • Hepatotoxicity: 12 hours post-overdose.

    Salicylates (Aspirin, Diflunisal)

    • Not for children under 8 years old.

    Arylpropionic Acid Derivatives (Ibuprofen, Naproxen)

    • Ibuprofen.
    • Naproxen (Aleve): 8-13 hours duration.

    Arylacetic Acid Derivatives (Ketorolac)

    • Ketorolac (Toradol): IM or IV use.
    • Potential Kidney Damage (no ceiling effect like morphine).
    • Use in kidney stone pain.

    COX-2 Inhibitors (Rofecoxib)

    • MOA: COX-2 inhibitor.
    • NOT FDA approved due to cardiovascular risk (heart attacks).

    Opioid Analgesics

    Hydromorphone (Dilaudid)

    • 8-10x more potent than morphine.
    • Short duration.
    • Available as a suppository.

    Oxymorphone

    • Similar to hydromorphone; different dosages.

    Heroin

    • 2-4x more potent than morphine.
    • Faster blood-brain barrier penetration than morphine.
    • Metabolized into morphine.

    Codeine (Methylmorphine)

    • 1/10th potency of morphine.
    • Lower efficacy than morphine.
    • 10% conversion to morphine; some poor metabolizers exist.
    • Rapid conversion in some populations (Northern Pacific Islanders).

    Oxycodone

    • 10x more potent than codeine.
    • Metabolized into oxymorphone.
    • Controlled-release (OxyContin).

    Hydrocodone

    • Similar to oxymorphone.
    • Abuse potential (crushing or chewing).

    Meperidine

    • ¼ potency of morphine.
    • Short duration.
    • No metabolism.
    • Seizure risk.

    Fentanyl

    • 80-100x more potent than morphine.
    • Anesthetic use.
    • Short duration, rapid onset.
    • Available as lollipop and transdermal patch.

    Methadone

    • Same oral potency as morphine, 4x more potent IV.
    • Treats opioid/alcohol dependence.
    • Longer duration.

    Buprenorphine

    • Partial mu agonist, kappa 3 agonist, kappa 1 antagonist.

    Nalbuphine

    • Kappa agonist, Mu antagonist.
    • Used in ambulances.
    • Lower abuse potential.

    Butorphanol

    • Kappa agonist, Mu receptor antagonist.
    • Nasal spray.
    • 5x more efficacy in women.

    Naloxone

    • Short half-life.
    • Ineffective orally.
    • Injected or nasal spray.

    Cannabinoids

    • CB1 receptors (brain), CB2 receptors (periphery).
    • Endocannabinoids as own receptors.
    • Mild physical dependence; no psychological dependence.

    CNS Stimulants

    • MOA: Indirect-acting sympathomimetics.
    • Overdose: Psychosis, CV problems.
    • Treatment: Antipsychotics, antianginals.
    • Psychological and mild physical dependence.

    Dissociative Anesthetics (Ketamine)

    • MOA: Glutamate receptor antagonist.
    • Potential for life-threatening dependence.
    • Overdose: Life support needed.
    • Seizures (treat with benzodiazepines).

    Sedative-Hypnotics (Benzodiazepines, Barbiturates)

    • MOA: GABA action.
    • Physical and psychological dependence.
    • Life-threatening withdrawal.
    • Overdose: Further sedation (decreased HR, BP, RR).
    • Treatment:
      • Barbiturates/alcohol: Life support.
      • Benzodiazepines: Flumazenil.

    Opioids (General Information)

    • Act on Mu receptors.
    • Kappa receptors produce dysphoria.
    • Physical and psychological dependence.
    • Withdrawal possible, but not always life-threatening.
    • Short-acting withdrawal: 12 hours.
    • Long-acting withdrawal: 30 hours.
    • Withdrawal symptom relief: Clonidine, lofexidine.

    Volatile Intoxicants

    • Paint, nitrites.
    • Overdose: Life support.
    • Physical dependence, acute withdrawal.

    Potassium Competitive Acid Blockers (Used for HIV)

    • Azans

    Drug Tolerance

    • Initiate tolerance: Genetic predisposition to faster metabolism.
    • Dispositional tolerance: Increased liver enzymes lead to needing more drug.
    • Pharmacodynamic tolerance: Downregulation of receptors.
    • Behavioral tolerance: Adjusting behavior to compensate for drug effects.

    Antiacids

    • Non-systemic: Hydroxide, carbonate; stay in GI tract.
    • Systemic: Sodium bicarbonate (changes blood pH).
    • MOA: Neutralizes stomach acid by converting it to water.
    • Hydroxide formulations generally more effective than carbonate ones.
    • Few side effects.

    H2 Receptor Blockers (-dine)

    • Block H2 receptors on parietal cells.
    • reduce stomach acid secretion
    • Effective in reducing acid by up to 70% in 24 hours.
    • Few side effects.
    • Cimetidine: High risk of drug interactions with CYP450 enzymes and potential estrogen elevation.

    Proton Pump Inhibitors (-azole)

    • Block proton pumps in the stomach.
    • Strong acid reduction (98% in 48 hours).
    • Treatment duration: 4-8 weeks for healing.
    • These drugs disrupt the proton pump mechanism by interfering with potassium cofactor action.
    • No proven advantage over PPIs.
    • DO NOT use in HIV patients.

    Prostaglandins (Misoprostol)

    • Treat NSAID-induced stomach ulcers (especially in elderly).
    • Avoid in females due to uterine effects.

    Laxatives (Bulk)

    • Psyllium, bran, methylcellulose.
    • Increase bowel volume, trigger stretch receptors.
    • Use with plenty of water.
    • Slow action (days).

    Laxatives (Irritant/Stimulant)

    • Castor oil, senna, bisacodyl.
    • Irritate GI mucosa, fluid into lumen, increased peristalsis.

    Laxatives (Saline/Osmotic)

    • Effective in 1-3 hours.
    • Used for bowel cleansing.
    • Osmotic force draws fluid into bowel, increases volume and triggers peristalsis.

    Sucralfate (Carafate)

    • Prevent and treat peptic ulcer disease (requires acidic pH).
    • Forms a protective layer over ulcers.
    • May interfere with drug/nutrient absorption.

    Bismuth Chelate

    • Also treats H. pylori (some antimicrobial activity).

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    Description

    This quiz covers the pharmacological details of medications like Ketoconazole, Metyrapone, Mitotane, and Acetaminophen, focusing on their mechanisms of action, therapeutic uses, and adverse effects. It also delves into the implications of acetaminophen overdose and its treatment. Test your knowledge on these critical pharmaceutical concepts.

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