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Pharmacology

Pharmacology. CHAPTER 5. WHAT ARE AUTACOIDS?. OCCUR NATURALLY IN THE BODY. produced in one organ and are transported via the lymph system All occur (made) naturally in the body. Terms & Definitions. Autacoids - Examples:

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Pharmacology

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  1. Pharmacology CHAPTER 5

  2. WHAT ARE AUTACOIDS?

  3. OCCUR NATURALLY IN THE BODY produced in one organ and are transported via the lymph system All occur (made) naturally in the body.

  4. Terms & Definitions • Autacoids - Examples: • Prostaglandins – lipids that are synthesized locally by inflammatory stimuli –↑↑PAIN receptors • Thromboxanes(a vasoconstrictor and a potent hypertensive agent, and facilitates platelet aggregation [clotting]). • Leukotrienes(Inflammatory molecules; precursor of prostaglandins) • “-kinins”- messengers

  5. IS PAIN DIFFERENT FOR EVERYONE?

  6. YES

  7. WHAT ARE PLACEBOS?

  8. ‘’FAKE’ DRUGS For some people, pain can also be effectively treated with inactive pills (placebos)

  9. WHAT ARE ANTIPYRETICS ALSO CALLED?

  10. NON-OPIODS Non opioid analgesics are also called: nonnarcotic, peripheral, mild, and Antipyretic (agents that reduce fever) Opioid analgesics are also called: narcotic, central, or strong analgesics.

  11. Classification of Analgesic Agents 2. Opioids (narcotics) Act primarily within the: central nervous system Depress the central nervous system Effective for severepain Examples: Morphine, Codeine, Agents in cough suppressants We will discuss this area more in the next chapter Difference is in their site of action Difference in their mode of action • Nonopioids (nonnarcotics) • Act primarily at the: peripheral nerve endings • Inhibit prostaglandin synthesis (regulating the contraction and relaxation of smooth muscle tissue) • Not effective for severe pain • 3 subgroups: • Salicylates (aspirin-like group) • NSAIDs • Acetaminophen

  12. WHAT CATEGORY IS ASPIRIN UNDER?

  13. SALICYLATES ASPIRIN is the most useful and common salicylate to reduce pain (analgesic action) acetyl salicylic acid (ASA) – THE CHEMICAL NAME FOR ASPIRIN

  14. WHAT DOES NSAIDS STAND FOR AND WHAT DOES IT MEEAN?

  15. NONSTEROIDAL ANTI-INFLAMMATORY DRUGS

  16. Salicylates • Aspirin belongs to a class of medications called nonsteroidal antiinflammatory drugs (NSAIDs). • Aspirin and other NSAIDs, for example, ibuprofen (eg. Motrin, Advil) and naproxen (eg. Aleve), are widely used to treat fever (antipyretic action), pain (analgesic action), and inflammatory (anti-inflammatory action) conditions such as arthritis • Aspirin is also known for its anti-platelet action

  17. Salicylates: ASA MECHANISM OF ACTION • Aspirinhave: • anti-inflammatory, • antipyretic, • analgesic, and • antiplatelet actions. • These actions are related to the ability to inhibit prostaglandin synthesis Whereas, Acetaminophendrugs have only antipyretic & analgesicactions.

  18. Salicylates: ASA MECHANISM OF ACTION • Aspirin inhibits cyclo-oxy-genase (COX) to block production of prostaglandins • Prostaglandins can sensitize pain receptors to substances such as BRADYKININ(SEE NOTE) • A reduction in prostaglandins results in a reduction in pain

  19. HOW LONG BEFORE ASPIRINS PEAK EFFECT?

  20. 30 MINUTES REMEMBER NOT TO APPLY TOPICALLY TO ORAL MUCOSA!!!!

  21. Salicylates: ASA ADVERSE REACTIONS • Reye’s Syndrome • Associated with use of aspirin in children & adolescents who took it when they had the chickenpox or influenza • Fatal disease that causes numerous detrimental effects to many organs, especially the brain and liver. • ACETAMINOPHEN and NSAIDs are now used for fever (antipyretic action) or pain (analgesic action) in pediatric and adolescents to reduce the chances of Reye’s Syndrome

  22. WHAT DRUG SHOULD YOU NOT TAKE WITH ASPIRIN?

  23. WARFARIN A drug interaction between aspirin and Warfarin can result in significant bleeding

  24. NSAIDs • A rapidly growing group with important application in dentistry • Mechanism of action and many of their pharmacologic effects and adverse reactions resemble aspirin • Many authors agree that the NSAIDs are the most useful drug group for the treatment of dental pain. • Most are available without a prescription.

  25. WHEN IS THE PEAK PERIOD FOR MOST NSAIDS?

  26. 1-2 hours

  27. NSAIDs PHARMACOKINETICS • Most NSAIDs peak in about 1-2 hours • Well absorbed orally and food reduces the rate but not the extent of absorption • Metabolized in liver, excreted in kidneys

  28. NSAIDs PHARMACOLOGIC EFFECTS • have a significant anti-inflammatory effect • Similar as aspirin: • analgesic • antipyretic • anti-inflammatory • They inhibit prostaglandin synthesis

  29. ARE NSAIDS ADDICTING?

  30. NO! NSAIDs are not addicting, tolerance does NOT develop, and no withdrawal syndrome can be induced.

  31. NSAIDs ADVERSE REACTIONS 7. Pregnancy and Nursing • Contraindicated in pregnancy; • Like aspirin, NSAIDs given late in pregnancy can prolong gestation • IBUPROFENis drug of choice for nursing

  32. DENTAL PAIN IS BEST MANAGED BY HOW MUCH MG OF IBUPROFEN?

  33. 400MG In usual prescription doses, NSAIDs can be shown to be statistically significantly better than codeine alone, aspirin, acetaminophen, or placebo.

  34. NSAIDs CONTRAINDICATIONS & CAUTIONS • NSAIDs should be used with caution in patients with: • asthma • cardiovascular disease • Renal diseases with fluid retention • coagulation problems • peptic ulcer disease • ulcerative colitis Contraindicated in pregnancy

  35. WHAT IS THE MOST COMMONLY USED NSAID?

  36. IBUPROFEN

  37. WHAT HAS NO ANTI-INFLAMMATORY EFFECT?

  38. ACETAMINOPHEN

  39. Acetaminophen • Used as an analgesic and antipyretic in children and adults when aspirin is contraindicated • Has no anti-inflammatory action

  40. Acetaminophen PHARMACOKINETICS • Rapidly and completely absorbed from the GI tract • Peak plasma level in 1 – 3 hours • Half life of 1 to 4 hours • Metabolized by the liver • Excreted by the kidneys in 24 hours • When large doses are ingested, an intermediate metabolite is produced that is thought to be hepatotoxic and possibly nephrotoxic. .

  41. AN ACUTE OVERDOSE OF ACETAMINOPHEN CAN CAUSE WHAT?

  42. LIVER DAMAGE

  43. Acetaminophen USES • Acetaminophen is used as an: • Analgesic agent (↓ pain) • Antipyretic agent (↓ fever)

  44. Acetaminophen USES • Used when hypersensitivity to aspirin or for patients experiencing aspirin-gastric induced irritation. • Used as an antipyretic instead of aspirin for young children; due to aspirin’s association with Reye’s syndrome. • Can be used in all stages of pregnancy (always ask doctor)

  45. WHAT DRUGS ARE USED TO TREAT GOUT?

  46. Allopurinol AND Probenecid

  47. Drugs Used to Treat Gout Allopurinol (Zyloprim) • used in PREVENTION of a gout attack. • Inhibits the synthesis of uric acid • Also used in patients receiving either chemotherapy or irradiation • If a pruritic rash should occur, the drug should be promptly discontinued Probenecid (Benemid) • used in PREVENTIONof a gout attack. • Is an uricosuric drug that increases uric acid excretion in the urine

  48. CHAPTER 6

  49. WHAT ARE OPIODS USED TO TREAT?

  50. MODERATE TO SEVERE PAIN At first referred to drugs that are derivatives of opium poppy Opioid or narcotic analgesics are used to manage dental pain in patients in whom NSAIDs are contraindicated

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