Pharmacology Lilley Ch 10 & 44

OPIOID ANALGESICS: INDICATIONS

-Main use: to alleviate moderate to severe pain -Often given with adjuvant analgesic drugs to assist primary drugs with pain relief Opioids are also used for: -Cough center suppression -Treatment of diarrhea -Balanced anesthesia

Treatment of Pain in Special Situations

-PCA and "PCA by proxy" -Patient comfort vs. fear of drug addiction -Opioid tolerance -Recognizing patients who are opioid tolerant -Use of Placebos -Breakthrough pain -Synergistic effect *The effect of a combination of two or more drugs with similar actions is greater than the sum of the individual effects of the same drugs given alone 1+1=3 *Opioid + NSAID or Antidepressant or Antiepileptic or Acetaminophen ** Depending on the cause may also be corticosteriod

CHEMICAL CATEGORIES OF NSAIDS

CHEMICAL CATEGORIES OF NSAIDS -SALICYLATES -ACETIC ACID DERIVATIVES -CYCLOOXYGENASE-2 (COX-2) INHIBITORS -ENOLIC ACID DERIVATIVES -PROPIONIC ACID DERIVATIVES #LILLLEY TABLE 44-1

OPIOID ANALGESICS: CONTRAINDICATIONS

CONTRAINDICATIONS: -Known Drug Allergy -Severe Asthma -Use with extreme caution in patients with *Respiratory insufficiency *Elevated intracranial pressure *Morbid obesity *Sleep apnea *Paralytic Ileus (Intestines not functioning properly) *Pregnancy *Myasthenia Gravis

CLASSROOM RESPONSE QUESTION An 82-year-old woman is taking ibuprofen (Motrin) 3200 mg divided three times daily as treatment for arthritis. She has had no other health problems. What is the most important assessment for the nurse to monitor while the patient is on this therapy? A. Blood sugar B. Liver function studies C. Assessment of hearing D. Renal function studies

D. RATIONALE: NSAIDs disrupt the prostaglandins, which stimulate vasodilation and increase renal blood flow. This disruption may precipitate chronic or acute renal failure in some patients, and elderly patients are at greater risk for this adverse drug reaction.

CLASSROOM RESPONSE QUESTION The nurse is administering medications. One patient has an order for aspirin 325 mg by mouth daily and another patient has an order for aspirin 650 mg 4 to 6 times daily (maximum 4 g/day). The nurse understands that the indication for the 325 mg of aspirin once daily is A. pain management. B. fever reduction. C. treatment of osteoarthritis. D. thromboprevention.

D. RATIONALE: "Low-dose" aspirin, such as 81 or 325 mg once daily, is given for thromboprevention. Dosages for pain, fever, or arthritis are much higher usually.

Chemical Classification of Opioids

Meperidine-like drugs -Meperidine, Fentanyl, Remifentanil, Sulfentanil, Alfentanil Methadone-like drugs -Methadone Morphine-like drugs -Morphine, Heroin, Hydromorphone, Oxymorphone, Codeine, Hydrocodone, Oxycodone *HYDROMORPHONE 7x more potent than morphine* other -Tramadol, Tapentadol #dosages page 154, Lilley text

Safety: Laboratory Values Related to Drug Therapy

ALP - Alkaline Phosphatase Normal Values: 30-120 Units/L -found in many tissues but in highest concentrations in the liver, biliary tract, and bone. Detection of this enzyme is important for determining liver and bone disorders. Enzyme levels of ALP are increased in both extrahepatic and intrahepatic obstructive biliary disease and cirrhosis and/or other liver abnormalities. ALT - Alanine aminotransferase; formerly serum glutamic-pyruvic transaminase (SGPT) NORMAL VALUES: 4-36 units/L -Older adults have slightly higher levels -Is found mainly in the liver and lesser amounts in the kidneys, heart, and skeletal muscle. If there is injury or disease to the liver parenchyma (cells), it will cause a release of this liver cellular enzyme into the bloodstream and thus elevate serum ALT Levels . Most ALT elevations are from liver disease. Therefore, if medications are then metabolized by the liver, this metabolic process will be altered and possibly lead to toxic levels of drugs. GGT - Gama-glutamyl transferase NORMAL VALUES: Male/Female age 45yrs and older: 8-38 units/L -Is an enzyme that is present in liver tissue; when there is damage to the liver cells (Hepatocytes) that manufacture bile, the enzyme will be released throughout the cell membranes and released into the blood. Individuals of African ancestry have normal values that are double the values of those who are white. AST - Aspartate aminotransferase; Formerly called serum glutamic-oxalocetic transaminase (SGOT) NORMAL VALUES: 0-35 units/L -is elevated with hepatocellular diseases. With disease or injury of liver cells, the cells lyse and the AST is released and picked up by the blood; the elevation of AST is directly related to the number of cells affected b disease or injury. LDH - Lactic dehydrogenase NORMAL VALUES: 100-190 units/L -Is found in cells of many body tissues including the heart, liver, RBC, kidneys, skeletal muscles, brain, and lungs. B/C it is in so many tissues, the total LDH level is not a specific indicator of one disease. If there is disease of injury affecting cells containing LDH, the cells lyse and LDH is released from the cells into the bloodstream, thus increasing LDH levels. This enzyme is just part of the total picture of altered liver function, which, if present, will the DECREASE the breakdown/ metabolism of drugs and other chemical compounds, resulting in elevated blood levels of drugs.

ANALGESICS

ANALGESICS (pain relieving meds) -Medications that relieve pain w/o causing loss of consciousness -"Painkillers" -Opioid analgesics -Adjuvant analgesic drugs

ANALGESICS: NURSING IMPLICATIONS

ANALGESICS: NURSING IMPLICATIONS *Before beginning therapy, perform a thorough history regarding allergies and use of other medications, including alcohol, health history, and medical history *Obtain baseline vital signs and I&O *Assess for potential contraindications and drug interactions *Perform a thorough pain assessment, including pain intensity and character, onset, location, description, precipitating and relieving factors, type, remedies, and other pain treatments **Pain is now considered a "fifth vital sign" **Rate pain on a 0 to 10 or similar scale *Be sure to medicate patients before the pain becomes severe so as to provide adequate analgesia and pain control *Pain management includes pharmacologic and nonpharmacologic approaches; be sure to include other interventions as indicated *Patients should not take other medications or OTC preparations without checking with their HCP *Patients should discuss herbal medications being taken with HCP *Instruct patients to notify HCP for signs of allergic reaction or adverse effects

ANTIDEPRESSANT DRUGS FOR PAIN

ANTIDEPRESSANT DRUGS FOR PAIN -TRICYCLICS *PO *Neuropathic pain *Adverse: anorexia, dry mouth, blurred vision, constipation, gynecomastia, sexual dysfunction, altered blood glucose level, urinary retention, agitation, anxiety, ataxia, cognitive impairment, sedation, headache, insomnia, skin rash, photosensitivity, weight changes, orthostatic hypotension, blood dyscrasias *Don't take with alcohol, don't use with MAOI drugs in previous 14 days, not recommended for patients with acute or chronic cardiac problems or seizures both associated with high risk of death with overdose. _________________________________________ -SNRIs *Duloxetine (Cymbalta) *PO *Diabetic peripheral neuropathy *Adverse: Dizziness, drowsiness, headache, GI upset, anorexia, hepatotoxicity *Don't use with MAOI drugs in previous 14 days, don't use with certain antipsychotic drugs *Drug interactions: Lilley table 16-6 (MAOI = MONOAMINE OXIDASE INHIBITORS) (SNRI=SEROTONIN-NOREPINEPHERINE REUPTAKE INHIBITORS)

ANTIEPILEPTIC FOR PAIN

ANTIEPILEPTIC FOR PAIN (ADJUVANTS) ____________________________________ GABAPENTIN (NEURONTIN) *PO *Neuropathic pain *Adverse effects **Dizziness, drowsiness, nausea, visual and speech changes, edema *Drug interactions table 14-5 Lilley ___________________________________ -PREGABALIN (LYRICA) *PO *Neuropathic pain and fibromyalgia *Adverse effects **Dizziness, drowsiness, peripheral edema, blurred vision -Contraindications: allergic reaction

Classification of Pain by ONSET and DURATION

Acute Pain: -sudden onset -usually subsides once treated Chronic Pain: -Persistent or recurring -Lasts 3 to 6 months or longer -Often difficult to treat -Often treated with medication to be taken around the clock Pg 145-146

ADJUVANT DRUGS

Adjuvant Drugs -Assist primary drugs in relieving pain *NSAIDs *ANTIDEPRESSANTS *ANTICONVULSANTS *CORTICOSTEROIDS NON-OPIOID ANALGESICS *A2-ADRENERGIC AGONISTS -Example: Adjuvant Drugs For Neuropathic Pain -Amitriptyline, Nortriptyline, Duloxetine (Cymbalta) (ANTIDEPRESSANT) -Gabapentin or Pregabalin (Anticonvulsants)

CLASSROOM RESPONSE QUESTIONS A patient is taking ibuprofen 800 mg three times a day by mouth as treatment for osteoarthritis. While taking a health history, the nurse finds out that the patient has few beers on weekends. What concern would there be with the interaction of the alcohol and ibuprofen? A. Increased bleeding tendencies B. Increased chance for gastrointestinal bleeding C.Increased nephrotoxic effects D.Reduced antiinflammatory effects of the nonsteroidal antiinflammatory drug (NSAID)

B. RATIONALE: NSAIDS TAKEN W/ ALCOHOL MAY RESULT IN INCREASED RISK OF GI BLEEDING

CLASSROOM RESPONSE QUESTION A patient with a history of heavy alcohol use needs a medication for pain. The recommended maximum daily dose of acetaminophen for this patient would be A. 1000 mg. B. 2000 mg. C. 3000 mg. D. 4000 mg.

B. RATIONALE: Chronic heavy alcohol abusers may be at increased risk of liver toxicity from excessive acetaminophen use. For this reason, a maximum daily dose of 2000 mg is generally recommended for these persons.

CLASSROOM RESPONSE QUESTIONS A hospitalized patient has an order for ketorolac (Toradol). The nurse notes that the order is only for 5 days. What is the reason for this? A. The patient's pain should subside by that time. B. There are concerns about addiction to the drug. C. The drug can cause severe renal and gastrointestinal effects. D. The drug loses its effectiveness over time.

C. RATIONALE: The main adverse effects of ketorolac include renal impairment, edema, gastrointestinal pain, dyspepsia, and nausea. It is important to note that the drug can only be used for 5 days because of its potential adverse effects on the kidney and gastrointestinal tract (GI bleeding).

OPIOID ANALGESICS

Ceiling effect -Drug reaches a maximum analgesic effect -Analgesia does not improve, even with higher doses *AGONIST (ex: Codeine) *AGONIST-ANTAGONIST (Ex: PENTAXOCINE & NALBUPHINE) Opioid Tolerance -a common physiologic result of chronic opioid treatment -Result: Larger dose is required to maintain the same level of analgesia Opioid Naive -patients receiving opioid analgesics for the first time and not accustomed to their effects.

Pain Medication Treatment

Consider Nonpharmacological Treatment Options (BOX 10-1 Pg 144) Nociceptive Pain -usually responsive to opioids and nonopioid medications Neuropathic Pain -multimodal approach -antiseizure drugs -opioid analgesics -Serotonin norepinephrine reuptake inhibitors (SNRIS) Antidepressants -A2-Adrenergic Agonists *Also seeing Antidepressants used in chronic pain #TCAs (Tricyclic Antidepressants) and SNRIs (serotonin-norepinephrine reuptake inhibitors) share the ability to modulate (modify/control) the neurotransmission of both serotonin and norepinephrine This appears to affect the pain circuitry both at the cerebral and at the spinal column level. #Neuropathic pain often is not well controlled by opioid analgesics alone. #Treatment frequently necessitates a multimodal approach combining various adjuvant analgesics including: TCAs (e.g., amitriptyline, notriptyline [Pamelor], desipramine [Norpramin]) Associated with more adverse effects than SNRIs. #Serotonin norepinephrine reuptake inhibitors (e.g., venlafaxine [Effexor], duloxetine [Cymbalta], bupropion [Wellbutrin, Zyban]) #Antiseizure drugs (e.g., gabapentin [Neurontin], pregabalin [Lyrica]. They think these drugs block the flow of pain signals from the CNS. #Transdermal lidocaine #a2-adrenergic agonists (e.g., clonidine [Catapres], act in the descending inhibitory tracts of the spinal cord. #NMDA receptor antagonists such as ketamine have shown promise in alleviating neuropathic pain refractory to other drugs. (N-Methyl-D-Aspartate receptor) #Antiseizure meds also used in treating fibromyalgia

CLASSROOM RESPONSE QUESTION A patient who has metastasized bone cancer has been on transdermal fentanyl patches for pain management for 3 months. He has been hospitalized for tests and has told the nurse that his pain is becoming "unbearable." The nurse is reluctant to give him the ordered pain medication because the nurse does not want the patient to get addicted to the medication. The nurse's actions reflect A. appropriate concern for the patient's best welfare. B. appropriate caution for a patient who is already on a long-term opioid. C. an uncaring attitude toward the patient. D. a failure to manage the patient's pain properly.

D. RATIONALE: Pts with severe pain, including metastatic pain or bone pain, may need higher and higher doses of analgesics. The nurse is responsible for ensuring that the patient experiences adequate pain relief.

CLASSROOM RESPONSE QUESTION A patient is recovering from an appendectomy. She also has asthma and allergies to shellfish and iodine. To manage her postoperative pain, the physician has prescribed patient-controlled analgesia (PCA) with hydromorphone (Dilaudid). Which vital sign is of greatest concern? A. Pulse B. Blood pressure C. Temperature D. Respirations

D. RESPIRATIONS RATIONALE: THIS PT HAS A HX OF ASTHMA & ALLERGIES, AND SHE WILL BE RCVING A DRUG THAT CAN DEPRESS RESPIRATIONS

HEBRAL PRODUCTS: GLUCOSAMINE AND CHONDROITIN

HERBAL PRODUCTS: GLUCOSAMINE AND CHONDROITIN *USED TO TREAT the pain of osteoarthritis usually taken orally but some injectable forms available _____________________________ ADVERSE EFFECTS *GI discomfort for both *Drowsiness, headache, skin reactions (glucosamine) _________________________________ DRUG INTERACTIONS *Enhances effects of anticoagulants *May increase insulin resistance (glucosamine) #Safety: herbal therapies and dietary supplements pg 702 in text 8th ed Both mainly used to for cartilage support but also used for other problems but there is lack of scientific evidence supporting use for some problems. Some other info. Chondroitin (one of the building blocks of cartilage): people who have shellfish allergies, asthma, or prostate cancer should not take. Can also effect clotting (prolong). Not recommended for children or women who are pregnant or breastfeeding (lack of safety evidence). Glucosamine: may have upset stomach, heartburn, drowsiness, headache with high doses. Caution if shellfish allergy. Check with HCP if kidney or heart disease, bleeding disorders, hypertension. Do not use with children, pregnant, or breast feeding.

OPIOID AGONIST

Hydrocodone w/ Acetaminophen; w/ Aspirin; w/ Ibuprophen -With Acetaminophen *NORCO, LORTAB, VICODIN *Not as strong as Oxycodone *Schedule II *High Abuse Potential *PO ___________________________________________ -Oxycodone with or without Acetaminophen or Aspirin, IR, SR *Schedule II *High Abuse Potential *w/ Acetaminophen (PERCOCET) *PO *W/ Aspirin (PERCODAN) *PO *W/O Acetaminophen or Aspirin; OXYIR, OXYCONTIN (Continuous release) *PO _____________________________________ -CODEINE SULFATE *Schedule II *If combined with acetaminophen Schedule III *Used primarily as Antitussive *Has a "Ceiling Effect" after a certain point -Increase dose will not increase response -Less effective as an analgesic *PO #IR=Immediate release #SR=Sustained release

MISCELLANEOUS ANALGESIC

MISCELLANEOUS ANALGESIC TRAMADOL HYDROCHLORIDE (ULTRAM) *Weak bond to the mu opioid receptor and inhibits reuptake of norepinephrine and serotonin *Weak opioid receptor activity, but not currently a controlled substance *Oral form only. Absorbed rapidly and not affected by food -ADVERSE EFFECTS *Drowsiness, dizziness, headache, nausea, constipation, respiratory depression, seizures -CONTRAINDICATED *Allergy to drug and may include opioids (cross-reactivity), acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids, psychotropic drugs #Also available in combination acetaminophen and an extended-release formulation.

OPIOID ANALGESICS: MECHANISM OF ACTION

Mechanism of action: -Agonist (Some are stronger than others) *Bind to an opioid pain receptor in the brain *cause an analgesic response (reduction of pain sensation) -Agonist-Antagonists (Partial agonist, mixed with agonist) *Bind to a pain receptor *cause a weaker pain response than a full agonist *Not normally used as first line analgesics *Less sedation than agonist -Antagonist (competitive antagonists) *Bind to pain receptor and reverse the effects of agonist and agonist-antagonists *Competes for receptor sites w/ agonist and agonist-antagonist *Bind to a pain receptor and exert no response ****DO NOT GIVE AGONIST AND AGONIST-ANTAGONIST TOGETHER****

METHODONE HYDROCHLORIDE OPIOID AGONIST

Methodone Hydrochloride Opioid AGONIST -Methodone Hydrochloride *DOLOPHINE *SCHEDULE II *OPIOID OF CHOICE FOR DETOXIFICATION TREATMENT OF OPIOID ADDICTS IN METHADONE MAINTENANCE PROGRAMS *CHRONIC PAIN *PO/IM/IV/SUBQ #Does not have the euphoric effect. #Unique in that it's half-life (25hr); caution is necessary to prevent overdose #Careful titration doses the drug accumulates in tissues, slowly released, allowing 24hr dosing. #Used for chronic pain, withdrawl treatment #very expensive

NONOPIOID ANALGESICS

NONOPIOID ANALGESICS ACETAMINOPHEN (TYLENOL) -Analgesic and antipyretic effects -Does not have anti-inflammatory effects -PO/rectal/IV -Available over the counter and in combination products with opioids -Alternative for those who cannot take Aspirin -Mechanism of Action *Blocks pain impulses peripherally by inhibiting prostaglandin synthesis *Lowers fever by acting on the hypothalamus ________________________ -Indications *Mild to moderate pain *Fever *Alternative for those who cannot take aspirin products or NSAIDS _____________________ -Dosage *Maximum daily dose for healthy adults is FDA is 4000 mg and manufacturer recommends max dose of 3000 mg/day *2000 mg for elderly, those with liver disease or chronic alcohol consumption *Inadvertent excessive doses may occur when different combination drug products are taken together **Be aware of the acetaminophen content of all medications taken by the patient (OTC and prescription) _____________________________ -Acetaminophen: Contraindications/Interactions/Adverse reactions *Liver dysfunction (extreme caution) **Risk of liver failure ______________________________________ -Should not be taken in the presence of *Drug allergy *Severe liver disease *G6PD deficiency = GLUCOSE-6-PHOSPHATE DEHYDRONASE IS A HEREDITARY CONDITION **Red blood cells break down when the body is exposed to certain drugs or stress of infection *Dangerous interactions may occur if taken with alcohol or other drugs that are hepatotoxic *Adverse: skin disorders, N/V and Less common: anemias, nephrotoxicity, hepatotoxicity ____________________________________________ -Acetaminophen: Toxicity and Managing Overdose *Even though available over the counter, lethal when overdosed *Overdose, whether intentional or resulting from chronic unintentional misuse, causes hepatic necrosis: hepatotoxicity *Long-term ingestion of large doses also causes nephropathy (kidney damage) *Recommended antidote: acetylcysteine regimen (IV, PO, NG, OG) **Most effective if started within 10 hr of overdose **Smells like rotten eggs **Mix with cola, flavored water and drink through a straw *May be given Activated Charcoal to decrease absorption of acetaminophen **Do not give both activated charcoal and acetylcysteine orally, by NG or OG tube. #Do not give both activated charcoal and acetylcysteine orally or by NG tube. Activated charcoal will bind to acetylcysteine. Some brand names: Mucomyst, Acetadote, Cetylev Also used for respiratory conditions to help clear mucus and inhaled. More common side effects of solution are inflammation of mouth, N/V, Fefer, runny nose, drowsiness, clamminess, chest tightness, coughing, wheezing or difficulty breathing. #Combination products now limited to 325 mg of acetaminophen _________________________________________ *Lidoderm transdermal Patch *Treatment for some neuropathic pain conditions **Example: Postherapetic neuralgia **Pain relief 4-12 hr *Up to 3 patches can be placed; commonly used on back, hip, and neck *Topically (minimal to no systemic effects) **Apply only to intact skin Max 12 hr/day to avoid systemic effects *Use alone or with antidepressants, opioids, or anticonvulsants *May experience redness or edema, unusual skin sensations and usually mild and transient. *Dispose securely -dangerous to children or pets #Lidocaine - affects rhythm of the heart

NONSTEROIDAL ANTI-INFLAMMATORY DRUGS - NSAIDS

NONSTEROIDAL ANTI-INFLAMMATORY DRUGS - NSAIDS -Large and chemically diverse group of drugs with the following properties: *Analgesic *Antiinflammatory *Antipyretic *Aspirin-also platelet inhibition

NSAIDS

NSAIDS -NSAIDS ARE ALSO USED FOR THE RELIEF OF: *Mild to moderate pain *headaches *Myalgia *Neuralgia *Arthralgia *Menstrual cramps *Alleviation of postoperative pain *Relief of the pain associated with arthritic disorders, such as rheumatoid arthritis, juvenile arthritis, ankylosing spondylitis, and osteoarthritis *Adjunctive pain relief in patients with chronic pain #Appropriate selection is clinical judgment based on patient history, previous medical conditions, intended use of the drug, previous experience with NSAIDs, patient preference, cost

NSAIDS - TOPICAL

NSAIDS - TOPICAL -DICLOFENAC SODIUM *For mild to moderate acute pain and OA pain *topical gel, topical patch, topical solution *other topical NSAIDS approved in other countries

NSAIDS INTERACTIONS

NSAIDS INTERACTIONS TABLE 44-5 *SERIOUS INTERACTIONS CAN OCCUR WHEN GIVEN WITH: -ALCOHOL -ANTICOAGULANTS -ASPIRIN -CORTICOSTEROIDS AND OTHER ULCEROGENIC DRUGS -PROTEIN BOUND DRUGS -DIURETICS AND ACE INHIBITORS -OTHER TABLE 44-5 #Drugs that are protein bound: Drugs not bound to proteins are active. The effects of highly protein-bound drugs may be enhanced if their dosages are not adjusted to accommodate low albumin concentrations. More drug actions if competing with other protein bound drugs. Reduced hypotensive and diuretic effects Increased bleeding tendencies

NSAIDs mechanism of action

NSAIDS MECHANISM OF ACTION *Inhibition of the leukotriene pathway, the prostaglandin pathway, or both *Blocking the chemical activity of the enzyme called cyclooxygenase (COX) promotes the synthesis of prostaglandins _______________________________________ -Cyclooxygenase-1 (COX-1) **Has a role in maintaining the GI mucosa **Risk of GI ulceration when blocked _________________________________________ -Cyclooxygenase-2 (COX-2) **DECREASE risk of ADVERSE EFFECT OF GASTROINTESTINAL ULCERATION

NSAIDS: ACETIC ACID DERIVATIVES

NSAIDS: ACETIC ACID DERIVATIVES -indomethacin (Indocin) -ketorolac (Toradol) -diclofenac sodium (Voltaren) -sulindac (Clinoril) -tolmetin (Tolectin) -etodolac (Lodine) -meclofenamate (generic only) -mefenamic acid (Ponstel) ________________________________________ -USED TO TREAT arthritis, acute gouty arthritis, acute bursitis, tendonitis, ankylosing spondylitis *Oral and Rectal -Ketorolac (Toradol) has powerful analgesic effects *Sometimes used in place of opioids *Only used short-term, max of 5 days **Effects on kidney and GI tract (GI Bleed) *For moderate-severe pain *PO, IM, IV and also an ophthalmic form #Toradol - max 5 days!

NSAIDS: ADVERSE EFFECTS

NSAIDS: ADVERSE EFFECTS -GASTROINTESTINAL *Dyspepsia, heartburn, epigastric distress, nausea *GI bleeding* *Mucosal lesions* (erosions or ulcerations) *Misoprostol (Cytotec) can be used to reduce these dangerous effects. -RENAL *Reductions in creatinine clearance *Acute tubular necrosis with renal failure -CARDIOVASCULAR *Noncardiogenic pulmonary edema #Black stools, red blood or coffee ground emesis, bruising Liver injury with ASA with high doses or overdose

NSAIDS: COX-2 INHIBITOR

NSAIDS: COX-2 INHIBITOR -CELECOXIB (CELEBREX) *First and only remaining COX-2 inhibitor *PO *Indicated for arthritis, acute pain, primary dysmenorrhea, ankylosing spondylitis *GI issues less common *Little effect on platelet function *Celecoxib is not to be used in patients with known sulfa allergy. Similar structure to sulfa antibiotics #Ankylosing spondylitis is an inflammatory disease that can cause some of the vertebrae in your spine to fuse together

NSAIDS: ENOLIC ACID DERIVATIVES

NSAIDS: ENOLIC ACID DERIVATIVES *PIROXICAM, MELOXICAM, NABUMETONE *USED TO TREAT mild to moderate arthritis, and gouty arthritits *PO

NSAIDS: NURSING IMPLICATIONS

NSAIDS: NURSING IMPLICATIONS *BEFORE BEGINNING THERAPY, ASSESS FOR CONDITIONS THAT MAY BE CONTRAINDICATIONS TO THERAPY, ESPECIALLY: **Documented NSAID or Aspirin allergy **GI lesions or peptic ulcer disease **Risk for bleeding (example: Bleeding disorders, thrombocytopenia) **Severe renal and hepatic disease *ASSESS FOR CONDITIONS THAT REQUIRE CAUTIOUS USE *Associated with both maternal bleeding and neonatal toxicity during perinatal period. Excreted into human milk. *Stop at least 1 week prior to surgery including oral or dental *Perform laboratory studies as indicated (cardiac, renal, and liver function studies, CBC, platelet count) *Do not give salicylates to children and teenagers because of the risk of Reye's syndrome *Because these drugs generally cause GI distress, they are often better tolerated if taken with food to avoid irritation *Explain to patients that therapeutic effects may for full anti-inflammatory effect may be up to 7 days and analgesic effects 30-60 minutes *Perform medication history **Several serious drug interactions exist #Analgesic effects 30-60 minutes *Educate patients about the various adverse effects of NSAIDs, and inform them to notify their prescriber *Inform patients to watch closely for the occurrence of any unusual bleeding, such as in the stool (Black stools or red blood in stool), bruising, bleeding gums *Report persistent GI or abdominal pain or easy bruising *Report any signs of salicylate toxicity *Advise patients that enteric-coated tablets should not be crushed or chewed *Educate about drug interactions *Monitor for therapeutic effects, which vary according to the condition being treated **Decrease in swelling, pain, stiffness, and tenderness of a joint or muscle area *If IM administer slowly into large muscle *Follow IV administration for specific Drug *Always check allergies before administering any medication **If a patient tells you they are allergic to a medication ask them to describe their reaction

NSAIDS: PROPIONIC ACID DERIVATIVES

NSAIDS: PROPIONIC ACID DERIVATIVES -FENOPROFEN (NALFON) -FLURBIPROFEN (ANSAID) -IBUPROFEN (MOTRIN, ADVIL) MOST COMMON -KETOPROFEN (ORUDIS KT) -NAPROXEN (NAPROSYN, ALEVE) SECOND MOST COMMON -OXAPROZIN (DAYPRO) *Used for their analgesic effects in treating rheumatoid arthritis, osteoarthritis, primary dysmenorrhea, gout, dental pain, and musculoskeletal disorders *PO *Ibuprofen also now available IV *Also used for antipyretic effects *Naproxen has fewer drug interactions with angiotensin-converting enzyme inhibitors given for hypertension #No drug monitoring, usual dose 1200-3200 mg/day

NSAIDS: SALICYLATE TOXICITY

NSAIDS: SALICYLATE TOXICITY *Cardiovascular: Increased heart rate *CNS: Tinnitus, hearing loss, dimness of vision, headache, dizziness, mental confusion, lassitude, drowsiness *Gastrointestinal: Nausea, vomiting, diarrhea *Metabolic: Sweating, thirst, hyperventilation, hypoglycemia, or hyperglycemia **Can also --> Liver damage (↑ ALT, AST) but not common *Hypoglycemia can develop and be life threatening *GI bleed _______________________ Treatment: -MILD **Reduce dose or Discontinue **Symptomatic and supportive therapy -SEVERE **Discontinue **Intensive symptomatic and supportive therapy #Dialysis if (see table 44-4) #Lassitude: stat of physical or mental weariness; lack of energy, fatigue, apathy

NSAIDS: SALICYLATES

NSAIDS: SALICYLATES -acetylsalicylic acid (aspirin- 1st NSAID) *Examples: aspirin, diflunisal (Dolobid), choline magnesium trisalicylate (Trilisate), and salsalate (Salsitab) **ASA- example: Aspercreme, Excedrin (also includes **acetaminophen), Ecotrin *PO/topical cream/rectal *Inhibits platelet aggregation *Antithrombotic effect: used in the treatment of MI and other thromboembolic disorders *Arthritis, Juvenile rheumatoid arthritis, lupus, pleurisy, pericarditis *Headache, neuralgia, myalgia, arthralgia, #Also in combination products High dose for pain, Low dose for heart DO NOT GIVE ASPRIN TO CHILDREN under 18 swelling of liver and brain

Classification of Pain by Underlying Pathology (Neuropathic Pain)

Neuropathic Pain: -Damage to peripheral nerve or CNS; Numbing, hot-burning, shooting, stabbing, or electrical in nature; Sudden, intense, short-lived, or lingering *Centrally Generated -Injury to the brain and/or Spinal cord *Peripherally Generated -Injury to the peripheral nerves *Idiopathic (UNEXPLAINED)

Classification of Pain by Underlying Pathology

Nociceptive: -pain results from stimulation of sensory nerve fibers called nociceptors -these receptors transmit pain signals from various body regions to the spinal cord and brain which leads to the sensation of pain *can be superficial or deep *Bone, Joint, Muscle, Skin, or Connective Tissue *Internal organs such as the intestine and bladder *Usually from tumor or obstruction #Somatic pain=often is further categorized as superficial or deep #Superficial pain=arises from skin, mucous membranes, and subcutaneous tissues and often is described as SHARP, BURNING, or PRICKLY. #Visceral pain=comes from the activation of nociceptors in the internal organs and lining of the body cavities such as the thoracic and abdominal cavities. #Visceral nociceptors = respond to inflammation, stretching, and ischemia. #Stretching of hollow viscera in the intestines and bladder that occurs from tumor involvement or obstruction can produce intense cramping pain. #Deep pain = is often characterized as deep, aching, or throbbing and originates in bone, joint, muscle, skin, or connective tissue.

OPIOID ADMINISTRATION

OPIOID ADMINISTRATION * IV PUSH -Dilute in normal saline 5mL unless directed to dilute further -Administer slow IV push (the length of time to administer depends on the dosage) * CONTINUAL RELEASE ORAL FORMS -DO NOT CHEW or CRUSH * TRANSDERMAL PATCH -remove old patch when applying new patch -Do not cut the patch -Do not expose to heat -Place on a hairless area on upper body -Dispose of unused patches (Flush) -Keep away from children -Only good for 3 days #Fentanyl patches are often cut into pieces and sold on the streets as "chicklets" #Cutting and exposure to heat accelerates the diffusion of the drug and patient receives too much of the drug. *When switching from IV to PO -Dosage will be HIGHER -NO First-Pass Effect with IV, so Lower dosage needed

OPIOID AGONIST

OPIOID AGONIST *MORPHINE SULFATE -MS-CONTIN (Continual release), ORAMORPH (continual release), MSIR, ROXANOL -Schedule II -Severe Pain -High abuse potential -Potential toxic metabolite known as MORPHINE-6-GLUCURONIDE can accumulate in patient with RENAL IMPAIRMENT -IV/IM/SUBQ/PO/SL or BUCCAL/RECTAL #PG156 *HYDROMORPHONE -Dilaudid -Schedule II -Very potent -approx. 7x more potent than Morphine -Severe Pain -Safer for pts w/ renal impairment than morphine -IV/IM/PO *low dosage 0.25-1 mg for IV where Morphine starts at 2 mg IV *FENTANYL -Duragesic (patch), FENTORA, ACTIQ, ORALET -Schedule II -Very potent (dose in MCG) -High Abuse potential -Moderate to severe pain -IV/IM/ Transdermal Patch/ Buccal lozenge/ Buccal Lozenge on a stick/ Nasal spray -Transdermal patch *For chronic or cancer pain in opioid-tolerant patients *Not to be used for acute pain *Not for the opioid naive pt *Change every 72hrs *****Key points—disposal, effect time, multiple patches, change patch (every 72 hours), Don't cut, don't apply heat, clean skin with water and let dry, hairless area of chest/back/side/ or outer side of upperarm. 6-12 hr for steady state. Patch effective for moderate-severe chronic pain, cancer pain.***

OPIOID AGONIST-ANTAGONIST

OPIOID AGONIST-ANTAGONIST *PARTIAL AGONIST/ AGONIST-ANTAGONIST/ MIXED AGONIST -Bind to Mu pain receptor and compete with other substances for site -varying degrees of agonist and antagonist effects on opioid receptors -Lower risk of misuse and addiction -not used for long-term chronic pain -Antagonistic activity can produce withdrawal symptoms in opioid-dependent patients -can help prevent overmedication and reduce post-treatment addictive cravings in clients with hx of addiction -Do not give concurrently with full opioid agonist (May reduce analgesic effects and can cause withdrawal s/s in opioid-tolerant patients) #May be used in pain management in obstetrical patients to avoid over-sedation of mother and fetus. Pg150 _________________________________________ AGONIST/ANTAGONIST -Buprenorphine (Buprenex) -Butorphanol (Stadol) -Nalbuphine (Nubain) -Pentazocine (Talwin) ORAL, INJECTABLE, INTANASAL ADVERSE RXs -Similar to opioid -lower incidence of respiratory depression

OPIOID ANALGESICS

OPIOID ANALGESICS *Natural Alkaloids (from opium poppy plant) -MORPHINE AND CODEINE *Synthetic Modifications of Opium Alkaloids Produced 3 different chemical classes of opioids: -MORPHINE-LIKE Drugs -MEPERIDINE-LIKE Drugs -METHADONE-LIKE Drugs *Drugs that bind to the opiate receptors to relieve pain *Strong pain relievers *Prescription only *Depending on the medication, can cause abnormal increase in ALP, ALT, GGT, AST, LDH ALP = Alkaline Phosphatase ALT = Alanine aminotransferase GGT = Gama-Glutamyl transferase AST = Aspertate aminotransferase LDH = Lactic dehydrogenase

OPIOID ANALGESICS: ADVERSE EFFECTS

OPIOID ANALGESICS: ADVERSE EFFECTS *Severe hypersensitivity and Anaphylaxis is RARE *CNS -sedation -Disorientation -Euphoria -Lightheadedness -Dysphoria *CARDIOVASCULAR -Hypotension -Flushing -Bradycardia *GENITOURINARY -Urinary retention *GASTROINTESTINAL -Nausea -Vomiting -Constipation -Biliary tract spasm *SKIN (Integumentary) -itching -rash *RESPIRATORY -RESPIRATORY DEPRESSION -Possible aggravation of Asthma *HIGH ABUSE POTENTIAL *PSYCHOLOGICALLY DEPENDENT RISK _______________________________________ #ANY ALLERGIES? WHAT IS THEIR RESPIRATION RATE?? Dysphoria- state of feeling unease, unhappy, unwell, or dissatisfaction Euphoria- feeling or state of excitement, intense happiness, well being Histamine release caused by opioids thought to cause itching, rash, peripheral arteries & veins to dilate leading to flushing and orthostatic hypotension natural opiates (morphine) elicit the most histamine release Urinary retention caused by increasing bladder tone Constipation- decrease peristalsis and increase water absorption N/V- irritate the GI tract and can trigger the center in the CNS that causes nausea Euphoria due to affinity for mu receptors with a rapid onset of action that produces euphoria

OPIOID ANALGESICS: ANTAGONISTS

OPIOID ANALGESICS: ANTAGONISTS OPIOID ANTAGONISTS -NALOXONE (NARCAN) *complete or partial reversal of opioid induced respiratory depression *IV Push/ Acts in less than 2mins/ half-life is shorter than opioids *Nasal route until IV can be established *Monitor level of Consciousness and respirations *May have to administer additional doses *MOST COMMON ADVERSE EFFECT IS OPIOID WITHDRAWAL/ OPIOID ABSTINENCE SYNDROME -manifested as: anxiety, irritability, chills and hot flashes, joint pain, lacrimation, rhinorrhea, diaphoresis, nausea, vomiting, abdominal cramps, diarrhea, confusion _______________________ NALTREXONE (ReVia) *PO and used as adjunct for maintenance of an opioid-fee state in former opioid addicts *Nausea and tachycardia most common adverse effect *Regardless of withdrawal symptoms, when a patient experiences severe respiratory depression, an opioid antagonist should be given. #If patient does not respond to presumed opioid overdose, condition may not be related to overdose. Naltrexone also used as adjunct to psychosocial treatments of alcoholism and reversal of postoperative opioid-induced respiratory depression. Nausea and tachycardia most common adverse effects.

OPIOID ANALGESICS: INTERACTIONS

OPIOID ANALGESICS: INTERACTIONS *ADDED RESPIRATORY DEPRESSION AND SEDATION -Alcohol -Antihistamines -Barbiturates -Benzodiazepines -Phentothiazines -other CNS depressents -Monoamine oxidase inhibitors (can result in respiratory depression, siezures, hypotension)

OPIOID ANALGESICS: NURSING IMPLICATIONS

OPIOID ANALGESICS: NURSING IMPLICATIONS *Oral forms should be taken with food to minimize gastric upset *May have order for anti-nausea medication *Ensure safety measures, such as keeping side rails up and call light in patient reach to prevent injury *Withhold dose and contact physician if there is a decline in the patient's condition or if vital signs are abnormal, especially if respiratory rate is less than 10 to 12 breaths/min *Older adult, neonate, infants-drug effects more pronounced *Check dosages carefully (6 rights=right pt, right drug, right time, right dose, right route, right documentation) *Follow proper administration guidelines for IM injections, including site rotation *Follow proper guidelines for IV administration, including dilution, rate of administration, and so on -Constipation is a common adverse effect and may be prevented with adequate fluid and fiber intake -Instruct patients to follow directions for administration carefully and to keep a record of their pain experience and response to treatments -Patients should be instructed to change positions slowly to prevent possible orthostatic hypotension -Monitor for adverse effects **Contact physician immediately if vital signs change, patient's condition declines, or pain continues **Respiratory depression may be manifested by respiratory rate of less than 10 breaths/min, dyspnea, diminished breath sounds, or shallow breathing, decrease in oxygen saturation -Assess: Ask patient *when pain started, what caused pain, description of pain, rate pain, what makes pain worse, what makes pain better -Identify comfort-function goal -Chronic severe pain: take as directed around the clock -Monitor for therapeutic effects *Decreased complaints of pain *Decreased severity of pain **Rate on a 1-10 scale before administering medication and again after administration 15-30 minutes depending on route of administration. Document in patient chart. *Increased periods of comfort *Improved activities of daily living, appetite, and sense of well-being _______________________________________ #PQRSTU Good indicator of effective pain medication is what can they do now that they could not do before. Must be a realistic goal and something they had done before pain came about.

PEDIATRICS & SALICYLATES...

PEDS & SALICYLATES... *DO NOT GIVE SALICYLATES TO CHILDREN AND TEENAGERS W/ FLULIKE SYMPTOMS BC OF THE RISK OF REYE'S SYNDROME ---REYES SYNDROME *PROGRESSIVE NEUROLOGIC LOSSESS *LIVER DAMAGE *COMA *DEATH

OPIOIDS:

PHYSICAL DEPENDENCE -Physiological adaptation of the body to the presence of an opioid -opioid tolerance and physical dependence are expected with long-term opioid treatment and should not be confused with psychologic dependence (addiction) _______________________________________ PSYCHOLOGIC DEPENDENCE -a pattern of compulsive drug use characterized by a continued craving for an opioid and the need to use the opioid for effects other than pain relief.

Pain Threshold & Pain Tolerance

Pain Threshold: level of stimulus needed to produce the perception of pain a measure of the physiologic response of the nervous system Pain Tolerance: The amount of pain a person can endure w/o it interfering with normal function Varies from person to person Subjective response to pain, not a physiologic fx Varies by attitude, environment, culture, ethnicity CH10 P45

Pain

an unpleasant sensory and emotional experience associated with actual or potential tissue damage A personal and individual experience WHATEVER THE PATIENT SAYS IT Exists when the patient says it exists Objectify pts pain by using a pain scale (0-10). Pain is subjective (ask them to describe their pain).

PCA

patient controlled analgesia Waveform capnography represents the amount of carbon dioxide CO2 in exhaled air, which assesses ventilation. It consists of a number and a graph. The number is capnometry, which is the partial pressure of CO2 detected at the end of exhalation. This is end tidal CO2 (ETCO2) which is normally 35-45 mm HG. OPIOIDS WILL CAUSE RESPIRATORY DEPRESSION. #1 Concern