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Analgesic Drugs

Understanding Pain
• Most common symptom prompting people to seek health care • Occurs when tissue damage activates free nerve endings of peripheral nerves • Cerebral cortex analyzes messages and determines actions • Activation of opiate receptors in CNS inhibits pain transmission

Understanding Pain
• Pain is a subjective experience • People differ in their perceptions, behavior and tolerance of pain • Stressors increase pain • Diversionary activities tend to decrease pain– deep breathing, listening to music, visual imagery, others?

• Acute pain can be super-imposed on chronic pain

• Try alternative measures for pain control in addition to drugs • Promote circulation and musculoskeletal function • Use heat or cold as ordered • Relieve pain ASAP • Administer analgesic before pain producing activities • Use the least amount of the mildest drug likely to be effective

Types of Pain
• • • • Acute pain Chronic pain Superficial pain Deep pain

NARCOTICS OPIOIDS
• Opioid-any derivative of opium plant or any synthetic drug that imitates natural narcotics • Opioid agonists-include opium derivatives and synthetic drugs w/similar properties (Kee p.332) • Decrease pain without losing consciousness • Opioid antagonists – Block effects of opioid agnoists – Used to reverse drug reactions-RD, CNS depression – Narcan (always keep antagonist nearby)

• Opioid agonists
– Any route – Inhalation uncommon – Absorbed from GI tract – Transmucosal / intrathecal fast acting – IV provides most rapid and almost immediate – Sub Q and IM delayed absorption
• Poor circulation can cause further delay

– Metabolized extensively in the liver
• Administration of meperedine > 48 hours increases risk of neurotoxicity and seizures from buildup

Pharmacodynamics
• Reduce pain by binding to opiate receptors in PNS/CNS • Stimulation of opiate receptors-mimic effects of endorphins –the body’s naturally occurring opiates • Cause dilation of blood vessels in head, neck, face – could result in increased cranial pressure • With the exception of Demerol, suppress cough center to have antitussive effect • Adverse / Side effects include constipation, respiratory depression, nausea, vomiting, urinary retention, orthostatic hypotension • Morphine – relieve dyspna r/t pulmonary edema

• Nursing process
– Assess pain before and after administration – Monitor for adverse reactions / side effects – Monitor for tolerance dependence
• Shortened duration of effect

– Evaluate respiratory status before each dose
• Respiratory depression • Restlessness

Mechanisms by Which Opioid Analgesics Work
• Reduce the perception of pain sensation • Produce sedation • Decrease emotional upsets associated with pain

Characteristics of Opioid Analgesics
• • • • Most are Schedule II or III drugs Morphine (MSO4) is the prototype May be given PO, IV, IM, SQ, or topically Oral drugs undergo significant first-pass metabolism • Metabolized by liver and excreted in urine

• Exert CNS effects • Use cautiously in clients with renal or hepatic disease, respiratory depression or increased intracranial pressure • Exert depressant effect on GI tract • Not recommended for prolonged periods of use except with chronic pain or malignant diseases

Morphine
• Naturally occurring opium alkaloid • Used to relieve severe pain • Maximum analgesia occurs in 10-20 minutes with IV route • Controlled released tablets given for chronic pain • May be given intrathecally or epidurally • Route determines time interval or frequency of administration

Hydromorphone (Dilaudid)
• Synthetic derivative of morphine • Same actions, uses, adverse effects as morphine • More potent on a mg per mg basis • More effective orally than morphine • Effects last longer than morphine

Meperidine (Demerol)
• Synthetic drug similar to morphine • Dose of 100mg is equivalent to Morphine 10mg • Has shorter duration • Has less respiratory depression and little antitussive effect • Causes less smooth muscle spasm

Codeine
• Naturally occurring opium alkaloid • Used for milder pain • Acts as an antitussive (found in cough meds) • Often combined with acetaminophen • Preferred analgesic with head trauma

Oxycodone
• Semisynthetic derivative of codeine • Used to relieve moderate pain • More potent and more likely to produce abuse than codeine • Available in combination with acetaminophen

• Reverse or block analgesia, CNS and respiratory depression of opioid agonists • Compete with opioids for opioid receptor sites in brain • Do not relieve depressant effects of anti-anxiety drugs or antipsychotics • Naloxone - oldest, most commonly known • Nalmefene - newer with longer duration • Naltrexone - used in maintenance of opiate free states in opiate addicts

Opioid Antagonists

Client Teaching For Opioid Analgesics
• Narcotics may be alternated with a non-narcotic analgesic • If pain relief not achieved notify physician • Do not drink alcohol or take other drugs that cause drowsiness • Do not smoke, cook, drive a car or operate machinery after taking

• Constipation is a common adverse effect • Do not crush or chew long acting tablets • Decrease dose or omit if adverse effects occur

Use In Older Adults
• Use cautiously if debilitated or hepatic, renal or respiratory impairment • Start with lower dose and increase gradually • Give less often? • Give opioid analgesic with short half-life (Oxycodone) • Monitor for sedation or confusion • Monitor urinary output • Assess ability to self-medicate

Characteristics of Withdrawal From Opiates
• Generalized body aches • Insomnia • Lacrimation • Rhinorrhea • Perspiration • Pupil dilation • • • • • Piloerection Anorexia N/V/D Increased vital signs Abdominal and other muscle cramps

Treatment Of Withdrawal Syndrome
• Gradually reduce the opioid over several days • Substitute methadone and slowly reduce dose over a longer time • Clonidine reduces withdrawal symptoms

NONNARCOTICS SALICYLATES
• Salicylates-produce peripheral blood vessel dilation – Most common pain reliever – Control pain – Reduce fever-stimulate hypothalmus – Reduce inflammation – ASA is oldest nonnarcotic analgesic – Bonus effect-inhibits platelet aggregrate – Guideline • Use lowest dose that produces analgesia • Highly protein bound-can interfere w/other drugs – Heparin,methotrexate, oral antidiabetic meds, insulin

• Adverse reactions
– – – – – – – – – – Hearing loss Diarrhea Thirst Sweating Tinnitus Confusion Dizziness Impaired vision Hyperventilation Reye’s syndrome-when given to children (do not use < 12 yrs old)

• Common side effects
– Gastric distress – Bleeding tendencies – NVD

• • • •

Give w/food May crush except enteric coated Hold and notify MD for bleeding Stop ASA 5-7 days before elective surgery • Salicylate hypersensitivity
– Tinnitus or hearing loss – Vertigo – Bronchospasm – Urticaria – Need to avoid prunes, raisins, paprika, licorice

ACETAMINOPHEN
• Acetaminophen – Antipyretic and analgesic – IS NOT ANTI INFLAMMATORY – Drug of choice for children with flulike symptoms – Risk of liver disease • Phenytoin, barbituates, INH, ETOH – Rarely cause GI distress-may cause LIVER toxicity • Monitor total daily dose (adults 4g max.)

Phenazopyridine hydrochloride
– Pyridium-now OTC – Dye used in commercial coloringanalgesic effect on urinary tract – Relieves pain, burning, itching, urgency,

• Teach
– Urine orange – Stains fabric-contact lenses – Notify in ineffective

Anti Inflammatory Drugs

• Anti inflammatory agents
– Reduce body temperature – Relief of pain – Anticoagulant (ASA) – Reduce inflammation

• ASA – oldest • NSAIDS- reduce inflammation & pain for arthritic conditions • Inhibit enzyme COX

• OTC –Ibuprofen, Motrin, Nuprin, Advil, Medipren –Naproxen (Aleve) –Motrin only available in 200 mg form • MD must prescribe higher dose

• Second generation NSAIDS – COX-2 inhibitors • COX 1 inhibitor – Decreased protection of lining of stomach – Clotting time decreased-benefit cardiovascular patients

• NSAIDS
– Inhibit prostaglandin synthesis
• Prostaglandins produced / released in inflammatory disorders

– Ankylosing spondylitis – Moderate to severe arthritis – Osteoarthritis – Acute gouty arthritis – Dysmenorrhea – Migranes – Bursitis, tendonitis

• Adverse reactions
– – – – – – – – – – – – – – – Abdominal pain, bleeding Anorexia Diarrhea, nausea Ulcers Liver toxicity Drowsiness Headache Tinnitus Confusion Vertigo Depression Blood in urine, bladder infection, kidney necrosis Sodium & water retention Heart failure Pedal edema

• Nursing implications
– CBC, platelet count, PT – Monitor hepatic / renal function – Bronchospasm – Monitor for s/s of bleeding – Take w/meals – Avoid alcohol

Corticosteroids
– prednisone / prednisolone / dexamethasone – Suppresses components of inflammatory process at the injured site – NOT THE DRUG OF CHOICE FOR ARTHRITIC CONDITIONS – USED TO CONTROL FLARE UPS – Must taper dose when D/C

DMARDS-disease modifying antirheumatic drugs
– Toxic – Alter disease process – Gold/Gold Salts • IM/PO • Used for relief of symptoms • Immunosuppressive agents-used when antiinflammatories do not work-cytoxan, methotexrate/cancer drugs • Antimalarials-when all other tx fails

Antiinflammatory Gout Drugs
– “gouty arthritis” – Urinary calculi – Gouty nephrophaty

• Increase fluid intake • Avoid foods rich in purine - organ meats, sardines, salmon, gravy, legumes • Avoid alcohol, caffeine, large doses of vitamin C • Zyloprim - inhibits final steps of uric acid • Colchicine - first drug, inhibits migration of leukocytes to the inflamed site

Propionic Acid Derivatives
• Ibuprofen (Motrin) - prototype; ketoprofen (Orudis), naproxen (Naprosyn) • Used as anti-inflammatory agents in gout, arthritis, tendonitis • Used as analgesic for dysmenorrhea, episiotomy, minor trauma • Used as antipyretic

• Better tolerated than ASA but more expensive • Similar adverse affects as with ASA • May lead to renal impairment • Inhibits platelets only while drug molecules in bloodstream • Combined with other drugs

Acetic Acid Derivatives
• Indomethacin (Indocin) - prototype; Tolmetin (Tolectin), Sulindac (Clinoril) • Used to treat moderate to severe rheumatoid arthritis, osteo-arthritis, gouty arthritis, bursitis, pericarditis for antiinflammatory effects • Prescription drug • Has increased incidence and severity of adverse effects

Client Teaching Guidelines
• Take ASA and NSAIDS with full glass of water and food • Drink 2-3 quarts of fluid daily with NSAIDS • Report signs of bleeding • Avoid or minimize alcoholic beverages • Do not take more than prescribed amount • Do not take more that 3 days for fever or 10 days for pain • Read labels of other OTC medications