Nsaids & Nonopioid Analgesics PDF

NONOPIOID (NONNARCOTIC) - It is the "House Keeping" enzymes ANALGESICS that regulate the normal cellular processes such as: - Safer than opioids...

NONOPIOID (NONNARCOTIC) - It is the "House Keeping" enzymes ANALGESICS that regulate the normal cellular processes such as: - Safer than opioids Gastric cytoprotection - Produce fewer side effects Vascular homeostasis - Not addicting Platelet aggregation - Act principally at the peripheral Kidney function nerve endings - Inhibits the synthesis of 2. COX-2 prostaglandins - It is constitutively expressed only in brain, kidney and bone ** Nonopioid analgesics are more effective - Its expression at other sites is if given before the pain and inflammation increased in inflammation associated with prostaglandin synthesis - It is responsible for the elevated occur, production of postanoids in ** Nonopioid analgesics are never inflammation and disease completely effective because they do not **The selective COX-2 inhibitors have been affect the formation of the primary pain synthesized mediators such as bradykinin. ** Its expression is inhibited by Glucocorticoids (NSAIDS) NONSTEROIDAL ANTI INFLAMMATORY DRUGS 3. COX-3 - more effects in CNS - Block COX reaction by inactivation of the enzyme preventing NON-SELECTIVE COX INHIBITORS biosynthesis of prostaglandin (INHIBITORS OF COX 1 & I1) - STEROIDS Reduce availability of A. DRUGS WITH ANALGESIC & prostaglandin precursor by MARKED WITH ANTI- means of synthesis of a INFLAMMATORY EFFECTS protein or peptide that blocks phospholipase A2 activity Salicylic Acid Derivatives Aspirin 1. COX-1 (Cyclooxygenase) Diflunisal - It is responsible for the physiologic Sodium Salicylate production of prostanoids Magnesium Chlorine Salicylate ***Prostanoids are powerful vasodilators (open up blood vessels) which allow more ACETYLSALICYLIC ACID (ASPIRIN) blood to flow through the narrowed vessels in the lungs. This family of drugs work in a 1. ANALGESIA similar way to naturally occurring - Inhibition of prostaglandin synthesis substances called prostaglandins produced by aspirin-like drug leads to by the body, albeit in much smaller analgesia by decreasing the quantities. sensitivity of pain fibers to the presence of pain-producing substances. 2. ANTIPYRESIS gastrointestinal disturbances - Results from inhibition of petechial hemorrhages prostaglandin synthesis in the - In more severe cases of salicylism: hypothalamus = returning to normal psychological temperature circulatory *** Increased prostaglandin levels produce respiratory changes an increased body temperature. - the symptoms usually disappears when th edrug is withdrawn 3. ANTIINFLAMMATORY EFFECTS - The lethal adult dose of aspirin is - Inhibits the synthesis of between 10 to 30 gm prostaglandin Hyperventilation renal excretion of 4. PLATELET EFFECT bicarbonate, sodium and - Aspirin prolongs bleeding time potassium - mechanisms of action of aspirin = decreasing the buffering acetylation of platelet capacity of the extracellular cyclooxygenase and subsequent fluid reduction of thromboxane. system is predisposed to *** It is recommended that aspirin therapy respiratory and metabolic be stopped at least 1 week before extensive acidosis surgery so that the patient's platelets will - Children likely to be given aspirin return to normal are more likely to have a reduced fluid intake and may be constipated 5. ADVERSE EFFECTS - When aspirin is prescribed for a - GASTROINTESTINAL EFFECTS child, one should ensure the ff: Gastrointestinal discomfort the dosage is accurately - HYPOPROTHROMBINEMIA determined Aspirin is knwn to prolong adequate fluid intake is the prothrombin time and maintained inhibit platelet function. - PREGNANCY AND NURSING the parent is cognizant of the danger of salicylate For near-term, high dose can prolong gestation, delay child does not have influenza parturition and increase the or chickenpox risk of hemorrhage in the newborn. 7. TREATMENT - May be accomplished by inducing 6. TOXIC EFFECTS EMESIS, GASTRIC LEVERAGE, - Mild toxic reaction to Salicylic Acid OR ADMINISTRATION OF is called SALICYLISM ACTIVATED CHARCOAL - Characterized by: 8. FOR SEVERE TOXIC REACTION Tinnitus - Require immediate hospital attention Headache and use of IV fluids to correct Nausea acidosis and electrolyte imbalance. Vomitting dimness of vision 9. FOR HYPOGLYCEMIA AND With antacid-buffering agent HYPOKALEMIA (Bufferin) - treated symptomatically by the Buffered solutions (Alka- ministration of glucose and Seltzer potassium. With another analgesics (Gemnisyn and codeine) 10. ADMINISTRATION, ABSORPTION, With sedatives or METABOLISM antihistamines - Always administered ORALLY, With caffeine (Anacin) partially absorbed from the stomach but mainly from the small intestine. B. DRUGS WITH ANALGESIC & - Metabolic products of salicylic acid MARKED WITH ANTI- include salicyluric acid, the ether or INFLAMMATORY EFFECTS phenolic glucuronide and the acyl or ester glucoronide. 1. Pyrazolon Derivatives - Small amounts are also metabolized Apazone to gentistic and genitsuric acid. Phenylbutazone - Metabolic products are formed Oxyphenbutazone principally in the liver 2. Oxicams 11. EXCRETION Piroxicam - Excreted in the kidney - Very little salicylate is excreted in Tenoxicam the feces. 3. Nephthylacetic Acid Prodrug 12. USES Nabumetone - Used as an analgesic for mild to moderate pain 4. Propionic Acid Derivatives - Treatment for RHEUMATIC FEVER Ibuprofen AND ARTHRITIS Fenoprofen - Used to prevent thromboses Flurbiprofen Ketoprofen 13. DOSAGE AND PREPARATION Naproxen - Adult age of aspirin for pain and Oxaprozin fever is 650mg every 4 hours Carprofen - for children, 65mg/kg/24hr or 10 to Tiaprofen 20 mg/kg every 6hours divided into four to six doses. 14. AVAILABLE PREPARATOINS CONTAINING ASPIRIN - Regular aspirin (25mg and 75mg) - Enteric-coted aspirin - dissolves in intestine - Sustained-release aspirin - Combinations OTHER NOTES FOR NSAIDS PHARMACOKENETIC USUALLY TO PICK YOU NSSAIDS USUALLY gastric cytoprotection - prperty 1 TO 2 HOURS, METABOLIZES IN of certian proprties particularly THE LIVER AND EXCRETED BY THE the prostoglandin when use to KIDNEY non secretary dose, to protect the gastric mucosa from becoming PHARMACOLOGIC EFFECTS inflamed and necrotic -ANALGESIC- THERES AN INHIBITIN OF ENZYME CYCLOOXYGENASE cox2 make prostoglandin that are (COX) AND THROMBOXANES mainly involved in inflammation - ANTIPYRETIC- EFFECT IT (COX) AND THROMBOXANES cox2 inhibitors mostly they block - ANTIPYRETIC EFFECT IT the inflammation INVOLVES THE INHIBITON OF PROSTOGLANDIN SYNTHESIS IN cox3 more effects on cns YOUR HYPOTHALAMUS - it place a key role in biosynthesis - IT HAS ANTI INFLAMMATORY of prostanoids known to be EFFECT important mediators in pain and - THERES AN INHIBITION IF fever. PROSTOGLANDIN SYNTHESIS AND OTHER LOCAL MEDIATORS OF SALICYLIC ACID: THE INFLAMMATORY RESPONSE be aware of fh toxicity THUS RESULTING FROM ANTI counsel patient whos taking INFLAMMATORY PROPERTIES recognize the toxic effect - ANTI GOUT YOUR NSAID POVIDES induce emesis and activated RELIEF THROUGH ANALGEISIC charcoal AND ANTI INFLAMMATORY vomiting REACTION immediate medical treatment - DYSMENORRHEA induce emesis and activated - NSAIDS INHIBITS YOUR INTRA charcoal UTERINE PROSTOGLANDIN vomiting immediate medical treatment ADVERSE REACTION OF NSAIDS - GI EFFECT (GI IRRITATION, GI NSAIDS ARE GROUP OF PAIN, BLEEDING PROBLEMS). ANELGESIC COMPOUNDS WHOS THUS IT CAUSES TARRY STOOLS MCHANISM AND FUNCTION IS ‡PROSTOGLANDIN SAME WITH ASPIRIN STIMULATES MECHANISM AND ACTION OF - GI EFFECT (GI IRRITATION, GI NSAIDS IT INHIBITS THE ENZYME PAIN, BLEEDING PROBLEMS). CYCLOOXYGENASE(COX) THUS IT CAUSES TARRY STOOLS RESULTING REDUCTON IN THE ‡PROSTOGLANDIN FORMATION OF PROSTOGLANDIS STIMULATES - RENAL EFFECT ( RENAL FAILURE, CYSTITIS AND IT CAUSES UTI) CNS SIDE EFFECT 1. SEDATION 2. DIZZINESS CONFUSION MENTAL DEPRESSION HEADACHE VERTIGO CONVULSION BLOC CLOTTING NSAIDS REVERSIVELY INHIBIT PLATELET AGGREVASION WHY? NSAID INHIBIT TXA2 OTHER EFFECTS OF NSAID - MUSCLE WEAKENESS - RINGING OF EARS - BLURRED VISION oral manifestatiom of nsaid - ulcerative stomatitis gingival ulceration therapeutic uses 1. medical - nsaid can be use fr osteoarthritis, humatoid arthritis, gouty arthritis, fever, dysmenorrhea and pain 2 dental - dental pain 2 common nsaid - ibuprofen - acetaminophen