The document discusses drugs used for pain and inflammation management. It begins by defining inflammation, analgesics, NSAIDs, and antipyretics. NSAIDs like aspirin, ibuprofen, and paracetamol are described in more detail, including their mechanisms of action, pharmacokinetics, therapeutic uses, and adverse effects. Specific concerns for NSAID use in pregnancy and risks of overdose like Reye's syndrome and hepatitis are also summarized. The document provides an overview of pharmacotherapy options for pain and fever treatment.

1. UNIVERSITY OF KABIANGA
KAPKATET CAMPUS
GROUP 11 PRESENTATION
SCHOOL OF: HEALTH SCIENCES
DEPARTMENT: CLINICAL MEDICINE
COURSE TITLE: CLINICAL PHARMACOLOGY
COURSE CODE: BCM 223
INSTRUCTOR: DR. ANTHONY YIAILE
TASK; Discuss the pharmacotherapy of drugs used in
management of pain and inflammation (20mks)

2. GROUP MEMBERS
1. ONYANYI JOSEPH……..BCM/K/0038/2021
2. MAGRINA LETING…….BCM/K/0025/2021
3. TIMOTHY KEITANY……BCM/K/0034/2021
4. SYLVIA NEKESA…………BCM/K/0015/2021
5. BRIAN KIPCHUMBA….BCM/K/0022/2021
6. BRENDA RICHARD…….BCM/K/0503/2021

3. INTRODUCTION
• Inflammation is a vascular response
to injury
• Analgesics are drugs that relieve pain.
• NSAIDS are drugs that reduces inflammation
and are effective against pain and fever.
• Antipyretics are agents that relieve fever
• Pain is initiated by harmful stimuli.
• Pain and fever are common symptoms.

4. Signs of inflammation
• Redness caused by dilation of vessels
• Pain due to increased pressure exerted
by accumulation of interstitial fluid
• Heat caused by increased blood flow
• Swelling due to an extravascular accumulation
of fluid
• Loss of function

5. PAIN
 Is important becauseit signals“disease”
 Its relief is an important duty
of a clinician.
 It also increases perspiration cooling body.
 Analgesia: state where painful stimuli
moderated, although still perceived no
longer painful.

6. PATHOPHYSIOLOGY OF PAIN

7. PATHOPHYSIOLOGY OF FEVER
Fever is elevated body temperature (>37.80 C ).
• Results from rise hypothalamic set points.
• Crucial component initiating fever is pyrogens.
• Are classified as endogenous or exogenous.
• Elevated prostaglandin-E2 alter firing rate of,
• neurons within hypothalamus that control
thermoregulation.

8. DRUGS USED IN MANAGEMENT OF PAIN
● There are opioid and Non-opioid drugs.
● The Non-opioid drugs include NSAIDs.
Differences between NSAIDs and opioid analgesics
● They do not depress the CNS.
● They do not produce physical dependence.
● Weaker analgesic activity except inflammatory pain.
● Act primarily on peripheral pain mechanisms.

9. CLASSIFICATION OF NSAIDS

10. MODE OF ACTION OF NSAIDs
● Posses anti-inflammatory, analgesic and antipyretic properties.
● Inhibit COX that converts endoperoxides into PGs.
● COX enzymes are of 2 types:
● COX 1:cytoprotective PGs in gastric lining.
● COX 2: generate PGs to mediate inflammation.
● NSAIDs only relieve pain secondary to inflammation.

11. THERAPEUTIC ACTIONS OF NSAIDs
● Analgesia: inhibit COX2 mediated PG synthesis.
● anti-Inflammatory: Inhibition of PG synthesis attenuates.
● Antipyretic: Lowers PG levels in hypothalamus.
● closing patent ductus arteriosus in neonates.
● Rx systemic mastocytosis (elevated mast cells).
● Cardio protection.

12. PHARMACOKINETIC PROPERTIES OF NSAIDs
● Absorption: readily absorbed after P.O intake.
peak plasma concertation reached 2-4 hrs.
● Distribution: widely distributed as protein bound.
● Metabolism: hepatic via oxidation and conjugation.
● Elimination: renally through secretion and filtration.
● Half life of individual agents varies.

13. SPECIFIC EXAMPLES OF NSAIDs AND THEIR USES
1.PARACETAMOL (ACETAMINOPHEN)
• Is a mild analgesic and antipyretic.
• MOA: It inhibits synthesis of prostaglandins.
• Pharmacokinetics: is well absorbed from GIT.
• Its distribution is by passive diffusion.
• Metabolism takes place in the liver.
• Eliminated: in urine as glucuronide, sulphate
conjugates.

14. PARACETAMOL Cont…
• Precaution : patients with Hepatic & renal failures.
• Contraindications: Severe renal impairment, Paracetamol
Hypersensitivity.
• Side Effects: Reversible skin rashes and
• Blood dyscrasia, vomiting and stomach ache.
• Dosage - Adult: 1-2 tablets every 4-6 hours
• Children (6-12 years): ½ -1 tablet 3 -4 times daily.

15. 2.ASPRIN (ACETYSALICYLATE)
• Is an Antipyretic and mild analgesic.
• MOA: inhibits both COX-1 and COX-2
• Pharmacokinetics – Absorption: absorbed in the stomach.
• Its distribution is by passive diffusion.
• metabolism takes place in the liver.
• and it's excreted in the urine.

16. ASPRIN Cont…
• Interactions: interferes with the coagulation irreversibly.
• Precautions: renal impairment, Gastric ulcer, Gout.
• Contraindication: Hypersensitivity to NSAIDs, Asthma, Hemophilia.
• S.E: GI disturbances, hypersensitivity reactions, thirst.
• Not used children below 12 years.
• Causes Reye’ssyndrome in age group.

17. 3.IBUPROFEN
• Managing mild to moderate pain, antipyretic.
• MOA: Non-selective inhibitor of COX.
• Pharmacokinetics – Absorption: absorbed in the stomach.
• Its distribution is by passive diffusion.
• Metabolism takes place in the liver.
• Excretion: urine as metabolites and bile.

18. IBUPROFEN Cont…
• Interactions: antidepressants, diuretics and beta-blockers.
• Precautions: Asthma, Bronchospasm, Elderly Hepatic disorders.
• Contraindication: Hypersensitivity to Ibuprofen, Peptic ulcer.
• S.E: GI disturbances, hypersensitivity, visual changes.
• Not recommended for children weighing >5kg.
• Use with caution in hx ulcer.

19. TOPICAL NSAIDs
• Several NSAIDs available as topical preparations.
• They include Ibuprofen and Piroxicam.
• penetrate skin, enter tissues or joints,
• to reduce processes that cause pain.
• Systemic absorption occurs but is modest.
• They cause local irritation of skin.

20. OTHER NSAIDs
• Celecoxib: used for long-term pain management,
• in patients with hx dyspepsia/GI bleeding.
• Dexketoprofen: has Less respiratory side effects.
• Ketorolac: for acute pain management(<5days).
• Indomethacin: powerful anti-inflammatory ,weak analgesic action.
• Naproxen: x20 potent COX inhibitor : aspirin.

21. SYSTEMIC ADVERSE EFFECTS OF NSAIDs
● CVS: fluid retention, HTN, edema, tachycardia.
● GIT: bleeding ulcers, nausea, vomiting, diarrhea.
● CNS: fatigue, insomnia, nervousness, agitation, confusion.
● Uterus: prolongation of gestation and labor.
● Metabolic: hyperglycemia, metabolic acidosis, glycogen depletion.
● Renal :interstitial nephritis, proteinuria, papillary necrosis.

22. NSAID POSOINING
• NSAIDs poisoning common since found OTC.
• Poisoning caused by accidental/suicidal overdose.
• Ibuprofen, acetaminophen, and aspirin poisoning common.
• Aspirin : glucose depletion, inhibiting Krebs cycle,
• Metabolic acidosis, electrolytes loss. Reyes syndrome.
• Corrected using activated charcoal and IV-Na2CO3.

23. PARACETAMOL POISONING
• Occurs dose is 7.5-10g for adults
• And 150-200mg for children.
• M.O.T: Excess metabolized to toxic NAPQI.
•NAQQIdoesn’t react glutathione =hepatocellular injury.
• Symptoms: abdominal pain, tender hepatic edge.
• Treatment: activated charcoal 2hrs after ingestion.
• N-acetylcysteine (antidote) to increase glutathione production.

24. REYE’S SYNDROME
• Condition causes swelling in liver & brain.
• It often affects children and teenagers.
• Happens when a child takes Aspirin.
• Signs and symptoms include Confusion, seizures.
• Early diagnosis & treatment save child's life.
• Caution giving Aspirin to children & teenagers.

25. IBUPROFEN POISONING
• Excess dose >3200mg/day for adults & >400mg/day,
• Overdose causes excessive inhibition of COX-1.
• Causes reduced PG synthesis & metabolic acidosis.
• Symptoms: nausea, vomiting, abdominal pain, dizziness.
• Decontaminant- use activated charcoal absorbed it.
• Forced alkaline diuresis neutralizes metabolic acidosis.

26. PREGNANCY AND LACTATION
• NSAIDs affect fertility & risk pregnancy loss.
• Use in second trimester considered safe,
• But was associated with fetal cryptorchidism.
• Avoided in 3rd trimester, significant fetal risks,
• Such as ductus arteriosus, intracranial hemorrhage.
• low infant exposure through breast milk.

27. REFERENCES
• Drug Index.it. (2019). Drugindex.it; PWA.
https://drugindex.it/clinical_details/169
• Ritter, M. J. (2008). A Textbook of Clinical Pharmacology and
Therapeutics (5th ed.). Hodder Arnold, Copyright.
• Nonsteroidal anti-inflammatory drug - Wikipedia. (2022). Retrieved 2
April 2022, from https://en.wikipedia.org/wiki/Nonsteroidal_anti-
inflammatory_drug
• Brunton, L.(2006). Goodman& Gilman’sthe pharmacologicalbasisof
therapeutics, 11th ed. Mcgraw-Hill Education, Copyright.
• Katzung, B. G. (2018). Basic & clinical pharmacology (14th ed.).
McGraw-Hill Education, Copyright
• www.wikipedia website: the free encyclopedia