1. Prepared and Presented by Clinical pharmacist Dr. Alan R. Mohammed
Pharmacy Practice Experience II Lecture One Anti-Inflammatory Drugs Part one For 4th Year Students/College of Pharmacy
Prepared and Presented by
Clinical pharmacist
Dr. Alan R. Mohammed

2. Contents
-Acetaminophen -Non-steroidal anti-inflammatory drugs (NSAID): -Non-selective (NSAID): - Ibuprofen - Naproxen - Cox-2-selective (NSAID): - Celecoxib - Etoricoxib

3. Learning Outcomes
Understand the indications, dosage forms, doses, cautions, contraindications, and side effects of commonly used non-steroidal anti-inflammatory drugs and of acetaminophen.
Demonstrate effective patient counseling abilities.
Understand the mechanisms of action of selective and non-selective non-steroidal anti-inflammatory drugs and of acetaminophen.

4. Acetaminophen
Mechanisms of action: 1- Inhibits brain prostaglandin synthesis which account for its analgesic and antipyretic effects. 2- It has a weak cox enzyme inhibition in the peripheral tissue. 3- May work peripherally to block pain impulse generation.

5. Acetaminophen (cont.)
Brand name: Tylenol, Panadol Generic name: Paracetamol, acetaminophen Dosage forms: Tablets, Caplets, Capsules, Gelcap/Geltab, Extended release caplets, Oral-disintegrating tablets, Syrups, Injections. Indications & Doses: Analgesia and fever: mg/4-8 hours, not to exceed 3250 mg/day, (Max mg/day under medical supervision).

6. Acetaminophen (cont.)
Cautions: Liver disease, severe renal impairment, G6PD, chronic malnutrition, pulmonary disease, cardiac disease, alcoholics, etc. Contraindication: Hypersensitivity, severe active liver disease. Side Effects: Angioedema, dizziness, rash, hepatotoxicity, pancytopenia, gastrointestinal hemorrhage, etc. Drug Interaction: Tinidazole (↑ level), Warfarin (↑effect), Isoniazid (↑ level), Ivacaftor(↑ level), etc…….

7. Acetaminophen (cont.)
Patient Counseling and other information: 1- If you give more than one product containing acetaminophen, do not forget to calculate the total dose. 2- Do not exceed the maximum dose. 3- Its available as OTC product.

8. Non-Steroidal Anti-inflammatory Drugs
NSAIDs can be divided generally into two groups: 1- Traditional (non-selective) NSAIDs such as: Ibuprofen, aspirin, naproxen, mefenamic acid, meloxicam, aceclofenac, diclofenac, etc.. 2- Selective cyclo-oxygenase-2 (COX-2) inhibitors such as: Celecoxib, etoricoxib Therapeutic effects: This group has analgesic, anti-inflammatory, and antipyretic effects. It can be used in the following conditions:

9. Non-Steroidal Anti-inflammatory Drugs
Rheumatoid arthritis
Osteo-arthritis
Fractures
Sprains
Sports and other soft tissue injuries
Postoperative pain
Dental pain
Menstrual pain
Headache
Migraine

10. Non-Steroidal Anti-inflammatory Drugs
There are two common isoforms of COX enzymes: 1- Cox-1: is a constitutive enzyme expressed in many tissues, its main role in tissue homeostasis. Its prostaglandin products are useful in gastric protection, platelet aggregation, renal blood flow autoregulation, etc… 2- Cox-2: is induced in cells in inflammatory condition. It is present in CNS as a constitutive enzyme.

11. Non-Steroidal Anti-inflammatory Drugs
Mechanism of action: They inhibit prostaglandin synthesis by inhibiting the oxidation of arachidonic acid by the fatty acid enzyme (Cyclo-oxygenase). It may inhibit chemotaxis, alter lymphocyte activity, decrease proinflammatory cytokine activity, and inhibit neutrophil aggregation.

12. Ibuprofen
Brand name: Advil, Motrin Generic name: Ibuprofen Dosage forms: Tablets, Capsules, Suspension, Chewable tablets. Indications & Doses: 1-fever, Pain, Dysmenorrhea: mg/4-6 hours. 2- Inflammatory diseases: mg/6-8 hours, max mg/day.

13. Ibuprofen (cont.)
Cautions: Cardiovascular risk, GIT risk, asthma, hypertension, systemic lupus erythematosus , etc… Contraindication: Hypersensitivity, preoperative pain in the setting of (CABG), Active bleeding, etc… Side Effects: Dizziness, rash, epigastric pain, constipation, tinnitus, fluid retention, etc. Drug Interaction: ACE-I (antagonism), Anticoagulants (↑effect), betablockers (antagonism), steroids(synergism ↑GI toxicity), etc…….

14. Ibuprofen (cont.)
Patient Counseling and other information: 1- Avoid use in severe hepatic impairment. 2- Its available as OTC drug. 3- Take with food 4- Monitor for renal, cardiac, and GIT side effects.

15. Naproxen
Brand name: Naprosyn Generic name: Naproxen Dosage forms: Tablets, Capsules , Delayed release tablets, Extended release tablets, Suspensions. Indications & Doses: 1-Pain: mg/6-12 hours, max mg/day for limited time. 2-Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis: /day, divided every 12 hours. 3-Dysmenorrhea 4-Acute gout 5-Migraine

16. Naproxen (Cont.) Cautions:
Cardiovascular risk, GIT risk, hypertension, hepatic impairment, renal impairment, coagulation disorders, etc.
Contraindication:
Hypersensitivity, preoperative pain in the setting of (CABG) .
Side Effects:
Abdominal pain, constipation, dizziness, drowsiness, headache, dyspnea, etc.
Drug Interaction:
ACE-I (antagonism), beta blockers (antagonism), Methotrexate (↑ level), Digoxin(hyperkalemia), etc…….

17. Naproxen (Cont.)
Patient Counseling and other information: 1- Take with food or ml of water to avoid GIT upset. 2- Not recommended in severe renal impairment. 3- Onset of action: minutes. 4- Its available as OTC drug. 5- Monitor for renal, cardiac, and GIT side effects.

18. Celecoxib
Brand name: Celebrex Generic name: Celecoxib Dosage forms: Capsules Indications & Doses: 1-Acute pain and primary dysmenorrhea: 400 mg initially then 200 mg on need on first day, then 200 mg/12 hours. 2-Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis: mg/day, once daily or divided every 12 hours. 3- Familial adenomatous polyposis: 400 mg/12 hours.

19. Celecoxib (Cont.) Cautions:
Cardiovascular risk, GIT risk, asthma, hepatic impairment, renal impairment, coagulation disorders, etc.
Contraindication:
Hypersensitivity, chronic hepatitis, preoperative pain in the setting of (CABG) .
Side Effects:
Headache, hypertension, fever, dyspepsia, upper respiratory tract infection, etc.
Drug Interaction:
ACE-I (antagonism), beta blockers (antagonism), Fluoroquinolones (↑ CNS toxicity), Anticoagulants (↑ bleeding risk), etc…….

20. Celecoxib (Cont.)
Patient Counseling and other information: 1- Take with food 2- If you have hypersensitivity to sulfonamide, do not take celecoxib. 3- Monitor for renal, cardiac, and GIT side effects.

21. Etoricoxib Brand name: Arcoxia Generic name: Etoricoxib
Dosage forms: Tablets
Indications & Doses:
1- Osteoarthritis: mg/24 hrs.
2-Rheumatoid arthritis, ankylosing spondylitis: 90 mg/24 hrs.
3- Acute gout: 120 mg/24 hrs. .

22. Etoricoxib (cont.)
Cautions: Cardiac impairment, coagulation defects, connective tissue disorders, crohn’s disease, dehydration, etc. Contraindication: Hypersensitivity, active GIT bleeding, ulceration, cerebrovascular disease, ischemic heart disease, mild to severe heart failure, uncontrolled hypertension, peripheral arterial disease, inflammatory bowel disease. Side Effects: Ecchymosis, fatigue, influenza-like symptoms, palpitation, anxiety, appetite change, ….etc. Drug Interaction: ACE-I (antagonism), beta blockers (antagonism), Anticoagulants (↑ bleeding risk), etc…….

23. Etoricoxib (cont.)
Patient Counseling and other information: 1- Monitor blood pressure. 2- If possible avoid in patients with renal impairment.

24. Questions

25. References
Mancano MA, Gallagher JC. Frequently Prescribed Medications; Drugs You Need to Know Jones & Bartlett Learning (ISBN: )
Hochadel M. Mosby’s drug reference for health professions. 4th edition, Elsevier, USA. (ISBN: )
British National Formulary (BNF).
Trevor AJ, Katzung BG, Hall MK. Pharmacology: examination and board review. 11th edition, Mc Graw Hill Education Lange, USA.
Rang HP, Dale’s MM. Pharmacology.7th edition, Elsevier Churchill Livingstone, UK.

26. Thank you