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

What is the mechanism of action for Rofecoxib?

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

What is the recommended treatment for acetaminophen overdose?

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

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

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

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

<p>Adrenal suppression (B)</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 (A)</p> Signup and view all the answers

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

<p>Systemic antiacids (C)</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 (C)</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 (B)</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 (A)</p> Signup and view all the answers

Which laxative type irritates the GI mucosa to promote peristalsis?

<p>Irritant/stimulant laxatives (C)</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 (D)</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 (C)</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 (C)</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 (B)</p> Signup and view all the answers

What is a significant adverse effect associated with ketoconazole?

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

What therapeutic use is NOT applicable to metyrapone?

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

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

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

What is the mechanism of action of miotrate?

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

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

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

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

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

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

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

Which cannabinoid receptor is primarily located in the brain?

<p>CB1 (D)</p> Signup and view all the answers

What is the primary function of antiacids?

<p>Directly neutralize stomach acid (B)</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. (B)</p> Signup and view all the answers

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

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

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

<p>Bulk laxatives (C)</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. (A)</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. (C)</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. (C)</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. (B)</p> Signup and view all the answers

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

<p>Irritant/stimulant laxatives (D)</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. (C)</p> Signup and view all the answers

Flashcards

Dispositional Tolerance

Repeatedly increasing the enzyme in the liver, requiring more of a drug because the liver breaks it down faster.

Pharmacodynamic Tolerance

Downregulation of the body's response to a drug.

Behavior Tolerance

Altering behavior to compensate for the effects of a drug (e.g., alcohol).

Antiacids (Non-systemic)

Stay in the GI tract, neutralizing stomach acid without affecting the bloodstream. Examples: hydroxide, carbonate.

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Antiacids (Systemic)

Can impact blood pH, neutralizing stomach acid. Example: sodium bicarbonate.

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H2 Receptor Blockers

Block receptors that signal stomach acid production, reducing stomach acidity.

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Proton Pump Inhibitors

Block the proton pump in stomach acid production; highly effective and reduce acidity to a high level.

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Bulk Laxatives

Increase bowel content volume, triggering intestinal stretch receptors.

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Saline/Osmotic Laxatives

Draw fluid into the bowel to increase volume and stimulate peristalsis, fast-acting.

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Sucralfate

Creates a protective layer over stomach ulcers/lesions, allowing healing while reducing acid.

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Ketoconazole MOA

Blocks cortisol production in the adrenal glands by interfering with enzymes; also antifungal.

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Acetaminophen therapeutic use

Pain relief (headaches, not migraines), fever reduction, and treating mild to moderate pain.

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Acetaminophen overdose treatment

N-acetylcysteine (NAC) is a common antidote.

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Acetaminophen overdose symptoms

Symptoms include nausea, vomiting, abdominal pain, and jaundice.

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Ketorolac (Toradol) injection

Powerful pain reliever, but injecting it has no ceiling effect and leads to kidney damage.

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Rofecoxib (COX-2 inhibitor)

A COX-2 inhibitor once used but was removed from the market due to cardiovascular risks, particularly heart attacks.

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Hydromorphone (Dilaudid)

Strong opioid pain reliever, 8-10 times more potent than morphine, short duration.

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Fentanyl potency

80-100 times more potent than morphine.

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Naloxone use

Emergency treatment for opioid overdose, not effective orally.

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Cannabinoid receptors

CB1 (brain) and CB2 (peripheral receptors).

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Metyrapone Use

NOT used for treatment. It's used to diagnose Cushing's syndrome.

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Miotrate MOA

Destroys adrenal cortex cells, which produce cortisol.

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Acetaminophen MOA

Unknown, but reduces pain and fever. It's not an anti-inflammatory.

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Salicylates for Children

Aspirin and Diflunisal are NOT safe for children under 8 years old.

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Ketorolac Injection

Powerful pain reliever that has no ceiling effect, BUT causes kidney damage.

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What's the mechanism of action of antiacids?

They neutralize stomach acid by using hydroxide or carbonate ions to react with hydrogen ions (H+), forming water. This directly reduces acidity in the stomach.

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Hydroxide vs. Carbonate Formulations

Hydroxide formulations of antiacids are generally 2-3 times more effective than carbonate formulations.

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What are H2 Receptor Blockers?

They block histamine (H2) receptors on parietal cells, which are responsible for signaling acid secretion via the proton pump.

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What's a Proton Pump Inhibitor?

They directly inhibit the proton pump, which is the final stage in acid secretion. This stops acid from entering the stomach lumen.

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How do Potassium Competitive Acid Blockers (PKABs) Work?

They bind to the potassium (K+) binding site on the proton pump, preventing K+ entry. Without K+ , hydrogen ions (H+) cannot be secreted into the stomach.

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How do Bulk Laxatives Work?

They increase the volume of bowel content, stimulating stretch receptors in the intestinal wall, promoting bowel movement.

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How do Stimulant Laxatives Work?

They irritate the GI mucosa, pulling fluid into the intestinal lumen and stimulating peristalsis, promoting bowel movement.

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How do Saline/Osmotic Laxatives Work?

They draw fluid into the bowel by osmotic force, increasing intestinal volume and triggering peristalsis.

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What is Sucralfate's Mechanism of Action?

It forms a protective layer over ulcers and lesions in the stomach, preventing acid from damaging the damaged tissue.

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What are Chelated Bismuth Used for?

They are used to treat H. pylori infection, which is a common cause of peptic ulcers. They have some antimicrobial activity.

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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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