STUDENT’S GUIDE

General Objectives

In this SGD Session, students will be able to:

1. Discuss the Acetaminophen’s mechanism of action, half-life, therapeutic and toxic blood
levels

2. Explain the metabolism of Acetaminophen to hepatotoxic metabolites

3. Know the antidote to be given in Acetaminophen Toxicity

4. Know where drug biotransformation occurs

5. Know the Phase I and Phase II reactions in drug biodisposition

6. Demonstrate on the proper way of making a prescription.

Case:
S.P, a 21-year-old female, was brought by her boyfriend in the emergency room after
learning that S.P ingested 50 tablets of Paracetamol 500mg/tablet 2 days ago. This is her 3rd
self-harm attempt in the last 13 months. She’s diagnosed with depression 3 years ago and is
taking Duloxetine as her anti-depressant. She’s also known to have Hepatitis B infection. She
arrived in the emergency room disoriented and complaining also of chest pain, abdominal pain
and vomiting.

Physical Examination:

General survey: awake, disoriented, appears weak, not in respiratory distress

BP 120/70 HR 98 RR 23 T. 36.9

HEENT: icteric sclerae, pink palpebral conjunctiva, no cervical lymphadenopathy

Skin: dry, (+) jaundice
Chest/ Lung: ECE,CBS
CVS: distinct heart sounds, normal rate, regular rhythm, no murmur
Abdomen: flabby, normoactive bowel sounds, not tender
GUT: unremarkable
Extremities: cool to touch, strong pulses

Lab: Alkaline Phosphatase = 323 ( 41-133mg/dl) ALT= 361 ( 7-56 mg/dl)

Total Bilirubin =4. 54 (0.1-1.2 mg/dl)

Creatinine: 2.5 mg/dl (0.8-1.2 mg /dl)

Plasma Acetaminophen concentration : 75 mcg/ml (10-20)

Questions:

1. What is Acetaminophen? What is its mechanism of action?

2. Describe acetaminophen based on the table below

Oral Availability (F) (%) 88

Urinary Excretion (%) 3

Note: Assuming creatinine clearance 100 mL/min/70 kg.

Bound in Plasma (%) 0

Clearance (L/h/70 kg)2 21

Volume of Distribution (L/70 kg) 67

Half-life (h) 2

Target Concentration 15mg/L

Toxic Concentration >300 mg/L

3. What is the safe therapeutic doses of Acetaminophen in adults?

4. What is the Acetaminophen’s half -life?

5. What is Acetaminophen’s therapeutic and toxic blood levels?

6. Is the patient having ongoing liver failure?

7. What antidote should be given to the patient?

8. In the history of the patient, what could be the contributing factor in compromising the
Acetaminophen’s safety?

9. Explain the Metabolism of acetaminophen to hepatotoxic metabolites

10. Where do drug biotransformation occur?

11. What is first-pass effect?

12. What are Phase I and Phase II reactions?