ANTI-INFLAMMATORY AGENTS • Children and pregnant women
• Strong anti-inflammatory and analgesic effects but very little antipyretic • PONSTAN, DOLFENAL effects • Piroxicam – 20 mg as single or divided dose daily • Inhibit prostaglandin synthesis by inhibiting the enzyme cyclooxygenase • RA and OA, GA, dysmenorrhea (Cox-1 and Cox-2) • Effects of therapy seen in two weeks Uses • Better compliance • Mild to moderate pain • Take with food • Dysmenorhea • Report abdominal pain, bruising, change in color of stools • Discomfort from minor surgery • FELDENE • Inflammatory processes • Tinoxicam – 20 mg • Arthritis • RA,OA,GA, tendonitis, bursitis Classifications • Se: edddema, wt gain, inc BUN, volume depletion • Proprionic Acid derivatives; • ASA: inc GI symtos – Ibuprofen (Alaxan,Muskelax, Advil) • Don’t give with anti-coag & pot. Sparing diuretics – Naproxen – (Naprosyn, Flanax) • Take with meals – Flubiprofen (Ansaid) • TILCOTIL – Ketoprofen (Orudis • Indomethacin 25 mg BID or TID, max 150-200mg per day – Oxaprozin (Daypro) • Not for routine use Classifications • GA, OA, pre-term labor • Acetic Acids: • CI: angioedema, PUD, pregnancy , asthma – Diclofenac (Volotaren • GI: life threatening: thrombocytopenia, aplastic anemia, – Etodolac (Lodine) hypokalemia – Ketorolac (Torodal) • DI: decreases effect of antihypertensives – Nabumetone (Relafen • Tke with food, blood tests – sulindac (Clinoril) • INDOCIN – Tolmetin (Tolectin) COX-2 INHIBITORS • Fenamates: Action: decreases pain and inflammation by blocking only COX-2, which keeps the – Mefenamic acid ( Ponstan, Dolfenal stomach lining intact, hence bleeding and gastric discomfort – meclofenamate Therapeutic uses: • Oxicams – Osteoarthritis – Piroxicam (Feldene) – Rheumatoid arthritis – Tinoxicam (Tilcotil) – Acute pain and dysmenorrhea • Indoles Advantages: decreased gastric irritation, better compliance with single daily doses – indomethacin Disadvantages: contraindicated in patients allergic to ASA and sulfonamides, may Contraindications impair bone healing, more expensive, and increase the risk of cardiovascular events • Allergies to NSAIAs including MI. • Salicylates CI :in patients prone to stroke & heart attacks • Peptic ulcer Preparations: • Known GI bleeding celecoxib (Celebrex) 200 mg OD or 100mg Bid. • Pregancy or lactation rofecoxib (Vioxx) 12.5– 25 mg po Adverse reactions & side effects • GI irritation Non-Opiate • Diarhea, n/V, abdominal pain (Non- Narcotic) • Vomiting, flatulence Analgesics-Antipyretics • Bleeding • Dizziness, lightheadedness SALICYLATES • rash analgesic, antipyretic, anti-inflammatory, decreased platelet aggregation • Ibuprofen -300 mg 4x daily PO or 400-800 mg 3-4x daily • Acetylsalicylic acid (ASA, Aspirin), • Monitor for gastric iritation & visual changes • choline magnesium trisilicate, • Take with meals, • choline salicylate, • MIDOL, ALAXAN, MUSKELAX • salsalate • Naproxen – 250-500 mg 2x daily PO Actions • Do not give with ASA, give with meals • Relieve pain by inhibiting prostaglandin through the inhibition of • May prolong bleeding time, monitor CBC cyclooxygenase an enzyme needed for its production • Observe for development of black stools Cox -1 protects stomach lining & regulates • Periodic eye exam blood platelets, Inhibition decreases • - FLANAX, NAPROSYN stomach protection hence bleeding may occur • Diclofenac – 50-75 mg 2-3x /day PO Cox 2 – triggers pain and inflammation. When • Use in pregnancy may cause miscarriage inhibited pain is reduced and inflammation • VOLTAREN • Ketorolac • Anti-pyretic effect by blocking of a prostaglandin mediator of pyrogens that • IM 30-60 mg, then 15-30 q 6h can increase body temperature at the thermoregulating center of the • Oral: 10 mg q 4-6h hypothalamus • IV 15-30 mg q 6h not to exceed 120 mg/day • Inhibit platelet aggregation by inhibiting thromboxane A synthesis • Use only for less than 1 week • Administer round the clock for best effect Therapeutic Uses • TORODAL • Mild to moderate pin • Mefenamic acid – 500 mg q 4-6h PO, max of 1 week • Fever of bacterial and viral origin • CTBT, ( agranulocytosis, aplastic anemia) • arthritis and muscular pains • give with food, • prophylaxis for myocardial infarction • do not use for more than 1 week Contraindications… • Enhances effect of oral coagulants • Child with varicella and influenza • CI: PUD, IBD, hepatic & renal ds • Hemophilia and other bleeding disorders • Peptic ulcer – Hepatic and renal function tests • Children with viral fevers – Administer with a full glass of water Drug Interactions… – Assess type and intensity of pain • Anticoagulants and Thrombolytics [ increases risk of bleeding – Assess patient’s temperature • NSAIA and corticosteroids - increased risk for GI bleeding – Avoid alcohol as it increases liver toxicity Usual dosage… – Avoid combination with ASA, NSAIA • Fever, mild to moderate musculoskeletal pain: – do not use for more than 5 days in children and 10 days in – 325-650 mg PO q 3-4h for pain adults • Dysmennorrhea: 650 mg PO q 4-6 h • Report signs of toxicity: N/V, abdominal pain, • Rheumatic fever 975-1300 mg PO 4-6x daily • Methemoglobinemia: SOB, weakness, headache, dizziness • Rheumatoid arthritis: 3.6-5.4 g PO daily in divided doses • Hemolytic anemia: paleness, weakness, skipped heart beats • Prevent TIAs; 325 mgPO qid or 650 mg PO bid • Chronic poisoning: SOB, fast weak pulse, cold extremeties, unexplained • Prevent recurrent MI: 325 mg PO daily bleeding, bruising,sore throat, fatigue Adverse effects… • Liver toxicity: jaundice, dark urine, clay colored stools • GI: nausea, vomiting, diarrhea, epigastric pain and GI bleeding are most • PREPARATIONS: common. Give with food. – Anadol • CNS: salicylsm at overdose levels – Panadol • Allergic reactions are also common – Tylenol • Respiatory: alkalosis – Biogesic • Prolonged use – bilateral hearing loss – D/c drug – Calpol Salicylism (overdose toxicity) – Tempra • Occurs with high doses of ASA Drugs to Treat Pain, Inflammation and Fever: Analgesics & Antipyretics • Mild: N/V, hyperventilation, headache, mental confusion, dizziness, tinnitus PAIN • Severe: restlessness, delirium, hallucinations, convulsions, coma, • UNPLEASANT SENSATION respiratory and metabolic acidosis, death from respiratory failure • CAUSES DISCOMFORT, Treatment… • DISTURBS SLEEP • Gastric lavage • INTERFERES WITH NORMAL DAILY ACTIVITIES • Activated charcoal through NGT • SYMPTOM OF AN UNDERLYINF DISEAS PROCESS. • Forced alkaline diuresis PAIN CONCEPTS • Hemodialysis • COMPONENTS: • Treat hyperthermia and convulsions – PHYSICAL – SENSATION OF PAIN • correct acid-base balance – PSYCHOLOGICAL – EMOTIONAL RESPONSE Nursing responsibilities… Sources of Pain • Take medicines with a full glass of water, peferrably with food • Illness • Monitor history of GI disorder, bleeding • Medical or surgical procedures • Assess pt for reactions to salicylate and signs of overdosage • Injury/trauma • Report hearing loss • Immobility • Do not use below 18 y.o – linked Reye’s syndrome in children • Nursing procedures • Discard tabs with a vinegar-like odor • Movement • Do not crush or chew • Dressing change • Wound care NON-SALICYLATES Types of Pain • Acetaminophen/paracetamol • Acute vs Chronic – ACTION: hypothalamic effect sweating and vasodilation; – Acute –needed upon request, parenteral inhibit CNS prostaglandin synthesis – Chronic – regular schedule, oral – Antipyretic-analgesic with less GI effects • Mild, Moderate vs Severe – no Reye’s syndrome, • Superficial, Visceral and Somatic – does not alter blood clotting or respiration – superficial – skin, mucus membranes* – no significant anti-inflammatory effect – Visceral – smooth muscles, organ systems* – DOSE: 325-260 mg q 4-6 hours – Somatic – skeletal muscles, joints, ligaments • Therapeutic Uses * narcotics – Fever in bacterial or viral infections Pain Measurement – myalgia, musculoskeletal pain, immunization • Pain Threshold – level of stimulus resulting in the perception of pain • Adverse effects • Pain Tolerance – amount of pain an individual can withstand without – Hepatoxicity , jaundice, nephrotoxicity, disrupting normal function and without requiring an analgesic. – allergy, Pain Theories – hemolytic anemia • Gate Theory • Precautions – PAINFUL STIMULI CAUSES RELEASE PF HISTAMINE – C/I in malnourished clients and chronic ROH abuse SEROTONIN – Overdose in acute hepatic failure can cause death BRADYKININ – Adminsister antidote within 8-10 hours of overdose: PROSTAGLANDIN acetylcysteine IV to reduce liver damag - STIMULI INITIATE ACTION POTENTIALS ALONG A – Do not take with alcohol SENSOY NERVE • Drug interactions - SENSITIZE PAIN RECEPTORS – Alcohol increases toxicity] Gate Theory – Loop diuretics – decreases plasma renin activity • A Fibers – NSAIDS – increases risk of hypertension – Large covered with myelin sheath – Oral contraceptives – increase liver breakdown of – Alpha, beta, gamma and delta fibers acetaminophen – Alpha – largest, rapid transmission, sharp well localized pain – Rifampin – increased hepatoxicity from peripheral areas – Isoniazid – increased risk of hepatotoxicity – Delta – smaller – Smoking – decrease serum acetaminophen levels and increased • C Fibers liver breakdown of acetaminophen – Small, unmyelinated • NURSING RESPONSIBILITIES: – Slow transmission of impulses – Dull, nonlocalized pain • constipation, nausea & vomiting, lightheadedness, constipation, confusion, Gate Theory disorientation, orthostatic hypotension itching • Pain and other sensory fibers enter SC and ascend to the brain (spinal gate) • Adverse effects (Reportable) • respiratory depression (morphine, fentanyl • Cells in substantia geltinosa (Dorsal horn) – acts as a gate to regulate flow of • and hydromorphone – c/I labor, impulses • lactating and children) – Alters sensation of pain from peripheral nerve fibers to the • euphoria and dependence brain • laryngospasm, apnes PAIN STIMULI Morphine – Moderate to severe pain, post-op A Fibers C Fibers – Acute MI – Cancer (liquid morphine –Roxanol) Closes dorsal Horn gate opens gate in dorsal horn – Severe pain in terminally ill patients – Dosage: oral 10-30 mg q 4h • SC 5-20 mg q 4h, IV: 1.5-2.5 mt Decrease Transmission of impulses • Children –IV, SC IM .1-.2 mg/kg q 1-2 h transmission of impulses cortex • Rectal: 10-20 mg q 4 • Fentanyl citrate (Sublimaze) Endorphins & Enkephalins • Brain peptides found to have opiate like activity – epidural anesthesia and analgesia • Act as neurotransmitters/neuromodulators – Cancer • Pain stimuli release of endorphins/enkephalins bind to opiate receptors – Monitor closely for respiratory depression in CNS inhibit impulse transmission – Dosage IM,IV Adults: .02-.1 mg Basis for Pain Management • Children 2-12 y: 2-3 mcg/kg • Treatment of cause • Transdermal patch: one patch q 48-72 h, 25 • Safest and most effective analgesic mcg/hr • Psychological support • Use of other measures, position change, back rubs, etc. • Hydromorphone (Dilaudid) Analgesics – moderate to severe pain with tolerance to morphine – Long term analgesia as in cancer Drugs that relieve pain without causing loss of consciousness – Terminal diseases Non-narcotics and Narcotics – Dose – 5-10 mg q 4-6 h Opiods – Administer round the clock in severe pain Opiod agonists – Respiratory depression more common than in morphine Opiod Antagonists • Methadone Non-opiods – severe pain in end stage cancer, HIV, chronic surgical pain – Less sedation unless after repeated doses Selecting the Proper Analgesic • Effectiveness of the agent – Common SE: constipation • Duration of Action – Dose • Desired duration of therapy • A: 2.5-10 mg q 3-4 h • Ability to cause drug interactions • C: .1 mg/kg q 6-8 h • Hypersensitivity of the client • Meperidine (demerol) • Available routes of administration – Kappa receptors Mechanisms of Action – Shorter action than morphine • Opiod & Opiod-like – bind to opiod receptors in the CNS act as agonists – Metabolized in the liver of endogenously occuring peptides decrease permeability of cell – Potentiate CNS depressants membrane to Sodium diminished transmission of pain impulses – Monitor respirator depression and liver dysfunction • Opiod antagonists – bind with opiod receptors, block the binding of opiod – 50-150 mg q 4h po/IM/SC (A) and opiod-like drugs, endorphins and enkephalins – 1.1-1.8 mg/kg bw q3-4h not to exceed 100 mg Therapeutic effects: • Codeine – 15-60 mg PO IM SC analgesia, cough suppression, decrease GI motility, adjunct to anesthesia – Analgesic antitussive, antidiarrheal effects, mild to moderate • Common SE: sedation, nausea, vomiting pain • Monitor: orthostatic hypotension, respiratory depression, urinary retention – Fluid hydration Mechanisms of Action – Administer with food or milk to reduce gi distress • Non-opiods: • Tramadol (Tramal) – Salicylates – affect hypothalamus, inhibits prostaglandin – 50 mg cap 3-4x /day max 400 mg synthesis preventing sensitization of pain receptors • Levorphanol (Levo-Dromoran) – Non-steroidal anti-inflammatory agents – inhibit prostaglandin – Oderate to severe pain, visceral pain assoc with terminal CA, synthesis renal & biliary colic< MI, tauma, post-op pain OPIODS • (Dolophine) • Opium – poppy plant, produces euphoria – Primarily to treat withdrawal syndrome in heroine or morphine • Morphine – active component isolated from Opium dependence • Uses: • Oxymorphone ( Numorphan) – moderate to severe pain from visceral sources (GIT, internal – Similar to morphine, except:causes more N/V and psychic organs) effects, less constipating and less cough suppression – Cough suppressant – Moderate to severe pain, pre-op med. OB analgesia, – Suppression of GI motility and secretions – 1-1.5 mg IM or Sc q 6 h, .5mg IV, 5 mg q 4-6h rectally – General anesthetic adjunct – Give with milk or meals • Specific mechanism: • Propoxyphene (Darvon) – Act on mu, kappa and sigma receptors – Mild analgesic, may be combined with ASA or acetaminophen • Mu- control morphine-like effects – analgesia, – Used in patients with history of alcohol intake euphoria and respiratory depression • Mixtures • Kappa – analgesia, sedation miosis • Brompton’s cocktail • Sigma – control hallucinatory activity, respiratory – Mixture of morphine, cocaine, dextroamphetamine and alcohol and vasomotor stimulation – Given to terminally ill clients for relief of sever cancer pain – Medullary cough center suppression –codeine CONTRAINDICATIONS – Suppression of gi motility – Drug allergies • Common side effects – Increased ICP – Acute asthma, chronic airway problems – Abdominal cramps – Elderly with renal ds. Pulmonary ds. CHF, liver ds, – Tachycardia, – alcoholism – hypertension – Headache Drug interactions – Reversal of analgesia and return of pain • ROH , antihistamines, anesthetics, CNS depressants, Sedatives, Important drugs Phenothiazines – potentiation, additive depression and drowsiness, • Naloxone (Narcan) coma – Therapeutic effects occur within 1-2 IV and 2-5 mins (IM/SC) • Cimetidine – increased CNS toxicity, disorientation, confusion, depression minutes and last for 1-2 hours and seizures. – Assess level of pain Nursing Responsibilities – Resuscitation equipment ready – Assess BP, RR, PR. Notify MD for HR above 120 bpm and BP • Assess character of pain over 140/90 • Obtain SBP – withold if RR below 12 and SBP belo 90 – Monitor for signs of withdrawal • Admin before pain peaks • Monotor for RD • Turn to sides q two hours • Monitor for hypotension – suppine position • Fluids and fiber for constipation • Anti-emetics for nausea and vomiting • Monitory mental status- safety • Palpate abdomen for retention • PO – snacks to decrease GI irritation • Health teachings • Naloxone for morphine overdosage • Institute after pain relief measures
Opiate Agonists-Antagonists
• Stimulates some receptors but antagonizes others
• Suppress CNS and alter patients perception and responses to pain • Antagonistic effects reduces potential for narcotic abuse • No antitussive effects • Fewer gastrointestinal side effects General uses: moderate to severe pain Adverse : • Similar to morphine • Withdrawal symptoms in patients addicted to narcotics: anorexia, nausea, vomiting, intestinal cramps, fever syncope or lightheadedness • Pentazocine (Talwin) can cause life threatening effects when given as injection to patients addicted to narcotics Important Drugs • Pentazocine – (Talwin) o Moderate to severe pain o Control pain during labor o SE: more frequent- sedation, euphoria, N/V o Less freq- dryness of mouth, headache, visual disturbance, flushing, constipation, urinary frequency. Increased anxiety o Adverse: tachycardia, skin rash, facial edema, hypertension, respiratory difficulty • Nalbuphine (Nubain) o Analgesia equivalent to morphine • Brupenorphine (Buprenex) o 30x more potent than morphine but low potential for abuse • Butorphanol (Stadol) o 3-5x more potent than morphine o Moderate to severe pain o Adjunct to anesthesia Nursing Responsibilities • Mental status assessment – dizziness confusion • Provide for safety. Avoid hazardous activities and those that need mental concentration • Assess for RD • Stool softeners, laxatives, high fiber diet • Do not discontinue abruptly Opioid Antagonists • Drugs that block the effect of agonists by competing for receptor sites • Block objective and subjective effects of opioids • Will precipitate withdrawal symptoms in patients physically dependent on opiods • Indicated for emergency treatment of opioid overdose Uses: – Diagnose opioid toxicity – Reverse CNS and respiratory depression caused by narcotics – Treat babies born to addicted mothers Prec: contraindicated in clients addicted to narcotics