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Arthritis Medication                                  See also   Muscle Relaxants

NSAID Nonsteroidal Anti-inflammatory Drugs Aspirin 325 mg 2-3 tab tid Disalcid (Salsalate) 500-750 mg 2 tab bid Ansaid (Flurbiprofen) 50 100 mg tablet. Dose 50 mg 3 4x/d upto 100 mg tid Arthrotec 50 or 75 (50 or 75 mg Diclofenac-Voltaren/ 200 mg Cytotec) 2-3x/day Cataflam (Diclofenac-Voltaren) 50 mg tid Clinoril (Sulindac) 150 200 mg tab. Dose 150 200 mg bid Colchicine 0.6 mg q 1-2 hours  (Max 8-10 mg/day).  Off  if diarrhea occurs. Daypro (Oxaprozin) 600 mg cap bid Disalcid (Salsalate) 500-750 mg 2 tab bid Dolobid (Diflunisal) 250-500 mg bid Feledene (Piroxicam) 20 mg/day Indocin (Indomethacin) 25-50 mg tid Lodine (Etodolac) 200 300 mg capsules. Dose 200 400 mg q6 8h (not to exceed 1200 mg/d) for acute pain. 600 1200 mg/d in divided doses (200 300 mg 2 4x/d) Meloxicam (Mobic) 7.5 mg daily Motrin (Ibuprofen) 200-400-600-800 mg tab tid pc Nalfon (Fenoprofen) 300-600 mg qid Naprosyn (Naproxen) 375 -500 mg tablets. Dose 375 -500 mg bid Orudis (Ketoprofen) 50 75 mg capsules. Dose Start 75 mg tid or 50 mg qid (range 150 300 mg/d) Oruvail (Keotoprofen-Orudis) 200 cap once/day Tolectin (Tolmetin) 400-600 mg tid Relafen (Nabumetone) 500 750 mg tab. Dose Start 500 mg 2 tab once/day, may be up to 200 mg/day Voltaren (Diclofenac Na) 25, 50, 75 mg tablets 2-3x/day, or Voltaren-XR 100 mg tab/day NSAID Group *Proprionic acids group: ibuprofen (Motrin, Advil), naproxen (Naprosyn), fenoprofen (Nalfon), ketoprofen (Orudis), oxaprozin (Daypro), Ansaid (Flurbiprofen) *Salicyclic acids group: indomethacin (Indocin), sulindac (Clinoril), diclofenac (Voltaren), etodolac (Lodine), Ketorolac, tolmetin (Tolectin) *Oxicam group: piroxicam (Feldene) *Anthranilic acids group: meclofenamate, mefenamic acid *Naphthylakanone group: nabumetone (Relafen) *COX-2 (Cyclo-oxygenase Inhibitor) specific or selective group: celecoxib (Celebrex), rofecoxib (Vioxx)

COX-2 Selective Inhibitors: Bextra (Valdecoxib) 10 mg tablet and 20 mg tablet Celebrex (celecoxib) 100-200 mg cap bid Vioxx (Rofecoxib) 12.5 -25 mg - 50 mg once/day tablet or oral suspension (5 ml)     - Discontinued due to increased heart problem !!!10/2004

Muscle Relaxants Flexeril (Cyclobenzaprine) 10 mg tid Norgesic Forte ( Orphenadrine 50 mg & ASA 770 mg & Caffeine 60 mg) 3-4x/day Parafon Forte (Chlorzoxazone 500 mg) qid Robaxin (Methocarbamol) 500-750 mg 1-2x/day Robaxisal (Methocarbamol 400 & ASA 325 mg) 2 tab qid Soma (Carisoprodol) 350 mg tid & hs Skelaxin (Metaxalone) 800 mg 3-4x/day   Do not administer with food.

World Health Organization analgesic ladder: effective in 70%–100% of adult patients Step One: for mild pain - NSAIDs and acetaminophen Step Two: for mild to moderate pain - Weak opioids (e.g., codeine, hydrocodone) - Combination analgesics (e.g., oxycodone/acetaminophen) plus NSAID and adjuvants as needed Step Three: for severe pain - Potent opioids (e.g., morphine, methadone, hydromorphone, fentanyl) plus NSAID and adjuvants as needed Use adjuvant medications at any level of the WHO ladder Corticosteroids (the most widely used adjuvants) Antidepressants, anticonvulsants, and other agents for neuropathic pain Bisphosphonates and radionuclides for bone pain Antibiotics for pain from ulcerating tumors Nonpharmacologic adjuvant therapy External-beam radiation Neurosurgical ablative procedures Psychiatric therapy Anesthesia

Opioids                                    See also constipation_rx.pdf Indications Acute pain Trauma-related pain Postoperative pain Cancer pain Some chronic noncancer pain (e.g., osteoarthritis, low back pain, neuropathic pain) Choice of agent Based on drug and patient characteristics Morphine plus gabapentin may be more effective for neuropathic pain than either agent alone Failure of response to an adequate trial of one opioid should be followed by an adequate trial of another opioid Administration Oral or transdermal For systemic treatment of chronic conditions if possible Intravenous Rapid titration and onset of analgesia Avoids first-pass hepatic degradation Yields higher bioavailability and opportunity to reduce total dose May provide consistent level of analgesia Useful alternative for patients unable to take orally Increased risk of systemic side effects Subcutaneous injection When small fluid volumes sufficient to deliver prescribed dose Rapid titration and onset of analgesia Shortened duration of effect requires continuous infusion or frequent redosing to maintain constant pain relief Risk of side effects is greater than with oral route Rectal Absorption and first-pass metabolism varies Cannot be used in patients with diarrhea, transmucosal lesions, neutropenia, or severe thrombocytopenia Transdermal When oral route is unavailable Limited by available skin surface Not effective for fluctuating pain levels Intramuscular: avoid because of erratic absorption and associated pain Patient-controlled analgesia (PCA) For initiation of parenteral opioid therapy, rapid opioid titration, or treatment of incident pain Continuous infusion may be programmed to supplement PCA doses, enabling sleep and covering baseline pain Equivalent or superior analgesia with the following advantages: Less total opioid consumption Fewer side effects No greater likelihood of dependence May be used in the home Intraspinal For patients requiring large doses Only for patients who have had pain relief but intolerable side effects with other regimens Achieves analgesia at significantly smaller doses than with systemic administration Intrathecal morphine is 100 times more potent than I.V. Epidural morphine is 10 times more potent than I.V. Dosing Begin with immediate-release oral agent with a short half-life for 24–48 hr and monitor consumption, efficacy of pain relief, and side effects Patients in severe pain may need rapid titration of a potent opioid via continuous I.V. infusion Long-acting or sustained-release forms may be prescribed once titration to optimal dose is achieved Change doses in increments of one third to one half the prior dose Reduce or eliminate dose gradually (in increments < 25% of daily dose) if patient becomes pain free Short-acting, immediate-release opioids to cover breakthrough pain for patients on long-acting therapy Single rescue doses of 10%–20% of total daily dose or 25%–30% of single standing dose Adjusted as appropriate for the individual Where possible, use the same agent for standing and breakthrough medications Conversion Inflammatory or neuropathic pain may be better treated with adjuvant analgesics than with modification of opioid therapy Pain of opioid side effects may only need treatment of the adverse effect Refractory pain or intolerable side effects may require conversion in these settings: Pain is opioid responsive Current drug was titrated to maximal effect Side effects are already optimally managed Choice of opioids may be based on patient's past experience with opioids of a given class or receptor profile Equianalgesic conversion tables should be consulted to arrive at a starting point for dosing If patient is receiving multiple opioids, conversion should be based on total dose of all prior agents, expressed as morphine equivalents If conversion is prompted by intolerable side effects but pain control is adequate, the calculated dose should next be reduced by ~ 25%–50% If conversion is prompted by inadequate analgesia, the new agent may be started at or near an equianalgesic dose Provide additional short-acting opioids during titration of new drug for breakthrough pain Reassess pain and total daily dose for the first 2 wk after conversion, with titration of extended-release and breakthrough doses as appropriate Avoid inadequate pain control and excessive narcosis during conversion Side effects Sedation Occurs with onset of therapy or increase in dose; usually resolves within 3–7 days Of concern in the elderly and those taking concurrent sedating medications Eliminate nonessential sedating medications Use stimulants (e.g., caffeine, methylphenidate) for cancer patients with significant persistent sedation Use with caution in the elderly Not recommended for patients with sedation due to opioid management of chronic pain Nausea Frequently resolves shortly after treatment onset Antiemetics during first 1–2 days of opioids may help Ondansetron, 4 mg I.V. Prochlorperazine, 5–10 mg t.i.d.–q.i.d. Hydroxyzine May alleviate centrally induced nausea Dose: 25–100 mg t.i.d.–q.i.d. Metoclopramide May reduce nausea caused by slowed gastric motility Dose: 10 mg q.i.d.; maximum daily dose, 500 µl/kg Scopolamine May alleviate motion-exacerbated nausea in ambulatory patients Dose: transdermal, 1.5 mg postauricular patch q. 3 days May have significant anticholinergic side effects, particularly in the elderly Constipation Does not improve with time Often underdiagnosed May lead to anorexia, vomiting, abdominal pain, obstruction, impaction, and perforation Appropriate dietary changes Assess for constipation in patients on around-the-clock opioids Stool softeners and stimulant laxatives Respiratory depression Rare side effect in opioid-naive patients receiving large doses and in head injury or pulmonary disease Monitor sedation level and respiratory status during first 24 hr of therapy in opioid-naive patients Stop opioids until depression resolves, then resume at 75% of previous dose Spirometry and oxygen may be useful Treat severe respiratory depression with I.V. naloxone Dose: 2 mg I.V. in 500 ml normal saline or D5W Confusion Occurs primarily in high-dose or prolonged opioid therapy and in decreased renal function Patients with previous cognitive impairment at additional risk Symptoms include delirium, agitation, myoclonus, hyperalgesia Of particular concern in the elderly or those with concurrent CNS disease Nonessential medications with CNS effects should not be prescribed for elderly patients requiring opioid therapy Neuroleptics may be useful against confusion, mental clouding, or persistent delirium Pruritus Diphenhydramine, 25–50 mg q. 4–6 hr Hydroxyzine, 25–100 mg t.i.d.–q.i.d. Myoclonus Clonazepam, 0.5 mg t.i.d.; increase by 0.5–1 mg q. 3 days to maximum of 20 mg/day Tolerance A higher dose of agent is required to maintain a given effect There is no clinical limit to tolerance Rarely develops in stable disease Increasing requirements for previously controlled chronic pain should prompt comprehensive evaluation Physical dependence A withdrawal syndrome could be produced by the following: Abrupt cessation of drug administration Rapid reduction in dose Decreasing blood level of drug Administration of an antagonist or mixed agonist-antagonist Universal with prolonged opioid therapy To avoid withdrawal, all patients receiving opioids for e 1 wk should have drug tapered rather than abruptly discontinued Psychological dependence (addiction) Differentiate from physical dependence Impaired control over drug use, compulsive use, continued use despite harm, and craving Extremely low prevalence in patients taking opioids for pain relief Pseudoaddiction More common than true addiction Patients with poorly managed pain mimic signs of psychological dependence Drug seeking Increased focus on obtaining medications Possibly illicit drug use or deception Behaviors resolve with effective pain management May be exacerbated by curtailing of opioid therapy

NSAIDs and Acetaminophen No tolerance or physical dependence Indications Especially useful for muscle and joint, bone, dental, postoperative, and inflammatory pain May suffice for mild or moderate pain For severe pain, may be added to an opioid regimen for opioid-sparing effect and enhanced pain relief Ceiling effect for analgesia NSAID side effects GI symptoms GI bleeding Hypersensitivity Kidney dysfunction CNS effects Often dose dependent NSAIDs may be used with GI-protective drugs Use acetaminophen with caution in patients with liver disease

Corticosteroids Indications Cancer pain Pain of spinal cord compression Increased intracranial pressure Superior vena cava syndrome Metastatic bone pain Neuropathic pain secondary to infiltration or compression by tumor Hepatic capsule distention High doses for inpatients with advanced disease in acute pain crisis Pain related to musculoskeletal conditions Oral or injectable Side effects Well tolerated for short-term treatment Toxicities Often arise with prolonged high-dose therapy Adrenocortical insufficiency Hypertension Immune suppression, masking of signs of infection Glaucoma Electrolyte imbalances GI ulceration and/or bleeding Osteoporosis and/or pathologic fracture Psychiatric disturbance or psychosis Avoid withdrawal syndrome upon discontinuance

Antiepileptic Drugs Indications Adjuvants for neuropathic pain Peripheral diabetic neuropathy Postherpetic neuralgia Reflex sympathetic dystrophy Trigeminal and glossopharyngeal neuralgia HIV neuropathy Spinal cord injury–related dysesthesias Postlaminectomy pain Phantom limb pain Cancer pain Gabapentin (Neurontin):  first-line treatment for neuropathic pain Well tolerated (except for cognitive effects in the elderly) Side effects: sedation, nausea/vomiting, dizziness Dose: 100 mg p.o., q. 8 hr (maximum, 3,600 mg/day in divided doses) Carbamazepine (Tegretol) First-line treatment for trigeminal neuralgia Second- or third-line agent for other neuropathic pain conditions Dose: 50–60 mg/day Monitor for hyponatremia and leukopenia Use only if gabapentin has failed or is not tolerated May cause thrombocytopenia or liver damage Topiramate (Topamax): adjuvant analgesic for neuropathic pain Dose: 100–200 mg/day Must be titrated slowly (no faster than 25 mg/wk) to decrease side effects such as cognitive slowing and paresthesias

Tricyclic Antidepressants (TCAs) Indications Adjuvants for neuropathic pain Painful diabetic neuropathy Postherpetic neuralgia Chronic facial pain Central pain Adjuvants for chronic pain Cancer pain Chronic low back pain Osteoarthritis Efficacy: comparable to antiepileptics Amitriptyline (Elavil): alternate choice Strongest anticholinergic profile Given at bedtime Nortriptyline (Pamelor): alternate choice Less anticholinergic effect Better choice for older patients Imipramine (Tofranil): alternate choice Dose for TCAs: 10–25 mg, to maximum of 150 mg/day, if tolerated Side effects of TCAs: elderly are most susceptible Sedation Hypotension Constipation Urinary retention May cause lethal cardiac arrhythmias at very high doses (contraindicated in patients with conduction abnormalities)

Selective Serotonin Reuptake Inhibitors (SSRIs) Useful in managing neuropathic pain Second-line choice for refractoriness or poor tolerability with other agents Paroxetine (Paxil) Dose: 20–50 mg/day Venlafaxine (Effexor)   Dose: 37.5–225 mg/day

2006