Product Information
Opioids: Short-Acting Agents
Codeine and Acetaminophen: Short-Acting Combination Agent (eg, Capital® and Codeine,
Tylenol® with Codeine)
Dosage form and route of administration: Oral (tablets, capsules)
Indications: These agents are indicated for the relief of mild-to-moderately severe pain. In patients
receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s
opioid tolerance.
Contraindications: Codeine and acetaminophen are contraindicated in patients who have previously exhibited hypersensitivity to codeine and acetaminophen.
Drug interactions: The effects of other opioid analgesics, antipsychotics, antianxiety agents, or central nervous system (CNS) depressants may be enhanced when used concomitantly with codeine and acetaminophen.
Adverse events: The most frequently reported adverse events associated with this pharmacologic treatment include lightheadedness, dizziness, sedation, shortness of breath, nausea, vomiting, and constipation. Other adverse reactions include allergic reactions, including anaphylactic symptoms and asthmatic episodes.1-2
Other cautions: Regular acetaminophen use is associated with hepatocellular enzyme changes. Hepatotoxicity can occur with excessive use of acetaminophen, and practitioners need to educate and caution patients about
all the various sources of acetaminophen in over-the-counter (OTC) and prescription medications. Patients using alcohol on a regular basis, or with a past history of alcohol abuse, should limit acetaminophen use by at
least 50%.
1Capital and Codeine [package insert]. Aliso Viejo, California: Valeant Pharmaceuticals North America; 2007.
2Tylenol with Codeine [package insert]. Titusville, New Jersey: Ortho-McNeil-Janssen Pharmaceuticals, Inc.; 2000.
For more information on these agents, click here.
Warning: Codeine Products in Nursing Mothers May Lead to Life-Threatening Side Effects in Babies.
August 17, 2007.
Fentanyl: Rapid-Onset Formulation (eg, Actiq®, Fentora®)
Dosage form and route of administration: Oral (oral transmucosal units [Actiq]; buccal tablets [Fentora])
Indications: These agents are indicated only for the management of patients with breakthrough cancer pain with malignancies who are already receiving and who are tolerant to opioid therapy for their underlying persistent cancer pain. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in opioid-intolerant patients and should only be taken by patients who are opioid tolerant.
Drug interactions: The effects of CNS depressants, monamine oxidase (MAO) inhibitors, and agents that affect CYP 3A4 and P450 3A4 activity may be enhanced when used concomitantly with fentanyl.
Adverse events: The most frequently reported adverse events associated with this treatment include headache, dizziness, nausea, vomiting, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with chronic use. Other adverse events include respiratory depression (rare in opioid-tolerant patients) and potential for psychological dependence.1-2
Other cautions: Usual dosing is no more often than every two hours to avoid dose accumulation. Since these formulations are indicated for breakthrough pain, more than 4 doses in 24 hours suggest a need to reevaluate the baseline analgesic dose.
1Actiq [package insert]. Salt Lake City, Utah: Cephalon, Inc.; 2007.
2Fentora [package insert]. Salt Lake City, Utah: Cephalon, Inc.; 2007.
For more information on these agents, click here.
Warning: Serious Side Effects with use of Fentora. September 26, 2007.
Hydrocodone and Acetaminophen: Short-Acting Combination Agent (eg, Anexsia®, Lortab®, Vicodin®)
Dosage form and route of administration: Oral (tablets, capsules)
Indications: These agents are indicated for the relief of moderate-to-moderately severe pain. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity to hydrocodone and acetaminophen.
Drug interactions: The effects of other opioid analgesics, antihistamines, antipsychotics, antianxiety agents, CNS depressants, MAO inhibitors, and tricyclic antidepressants (TCAs) may be enhanced when used concomitantly with hydrocodone and acetaminophen.
Adverse events: The most frequently reported adverse events associated with these agents include lightheadedness, dizziness, sedation, nausea, vomiting, and respiratory depression.1-3
Other cautions: Regular acetaminophen use is associated with hepatocellular enzyme changes. Hepatotoxicity can occur with excessive use of acetaminophen and practitioners need to educate and caution patients about
all the various sources of acetaminophen in OTC and prescription medications. Patients using alcohol on a regular basis, or with a past history of alcohol abuse, should limit acetaminophen use by at
least 50%.
1Anexsia [package insert]. St. Louis, Missouri: Mallinckrodt Inc.; 2005.
2Lortab [package insert]. Smyrna, Georgia: UCB Pharma, Inc.; 2002.
3Vicodin [package insert]. North Chicago, Illinois: Abbott Laboratories; 2007.
For more information on these agents, click here.
Hydromorphone: Short-Acting Agent (eg, Dilaudid®)
Dosage form and route of administration: Oral (tablets, capsules, oral solution); Parenteral (injection);
Rectal (suppositories)
Indications: These agents are indicated for the management of pain in patients for whom an opioid analgesic is appropriate. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to hydromorphone.
Drug interactions: The effects of MAO inhibitors, antihistamines, TCAs, anticholinergics, phenothiazines, tranquilizers, and sedatives may be enhanced when used concomitantly with hydromorphone.
Adverse events: The most frequently reported adverse events associated with this pharmacologic treatment include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, sexual dysfunction due to decreased sex hormone levels with regular use, and respiratory depression.1
Other cautions: Use with other CNS-depressant drugs, including alcohol, can cause potentially life-threatening respiratory depression, especially during sleep.
1Dilaudid [package insert]. North Chicago, Illinois: Abbott Laboratories; 2006.
For more information on these agents, click here.
Morphine: Immediate-Release Formulation (eg, Roxanol™, Morphine Sulfate
Immediate Release® [MSIR])
Dosage form and route of administration: Oral (tablets and capsules swallowed whole, oral solution);
Rectal (suppositories)
Indications: These agents are indicated for the relief of moderate-to-severe pain. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to morphine.
Drug interactions: The effects of MAO inhibitors, antihistamines, TCAs, anticholinergics, phenothiazines, tranquilizers, and sedatives may be enhanced when concomitantly used with morphine.
Adverse events: The most frequently reported adverse events associated with these agents include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1-2
1Roxanol [package insert]. Columbus, Ohio: Boehringer Ingelheim Roxane, Inc.; 2006.
2MSIR [package insert]. Stamford, Connecticut: Purdue Pharma L.P.; 2004.
For more information on these agents, click here.
Oxycodone: Immediate-Release Formulation, Used Alone or in Combination with Acetaminophen or Aspirin (eg, OxyIR®, Percocet®, Percodan®, Roxicodone™)
Dosage form and route of administration: Oral (oral solution, tablets, and capsules)
Indications: These agents are indicated for the relief of moderate-to-moderately severe pain. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to oxycodone.
Drug interactions: The effects of other opioid analgesics, CNS depressants, anticholinergics, phenothiazines, tranquilizers, sedatives, amiodarone, quinidine, and polycyclic antidepressants may be enhanced when concomitantly used with oxycodone.
Adverse events: The most frequently reported adverse events associated with this treatment include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1-4
Other cautions: Regular acetaminophen use is associated with hepatocellular enzyme changes. Hepatotoxicity can occur with excessive use of acetaminophen and practitioners need to educate and caution patients about
all the various sources of acetaminophen in OTC and prescription medications. Patients using alcohol on a regular basis, or with a past history of alcohol abuse, should limit acetaminophen use by at
least 50%.
1OxyIR [package insert]. Stamford, Connecticut: Purdue Pharma L.P.; 2007.
2Percocet [package insert]. Chadds Ford, Pennsylvania: Endo Pharmaceuticals Inc.; 2006.
3Percodan [package insert]. Chadds Ford, Pennsylvania: Endo Pharmaceuticals Inc.; 2006.
4Roxicodone [package insert], Columbus, Ohio: Boehringer Ingelheim Roxane, Inc.; 2000.
For more information on these agents, click here.
Oxymorphone (eg, Numorphan®, Opana®)
Dosage form and route of administration: Oral (tablets [Opana]); Parenteral (injection [Numorphan]); Rectal (suppositories [Numorphan])
Indications: These agents are indicated for the relief of moderate-to-severe pain. Numorphan injection is also indicated for preoperative medication, for support of anesthesia, for obstetrical analgesia, and for relief of anxiety in patients with dyspnea associated with pulmonary edema secondary to acute left ventricular dysfunction. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to oxymorphone.
Drug interactions: Patients using oxymorphone concomitantly with CNS depressants and opioid agonist and antagonist analgesics may exhibit an additive CNS depression.
Adverse events: The most frequently reported adverse events associated with this treatment include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1-2
1Numorphan [package insert]. Chadds Ford, Pennsylvania: Endo Pharmaceuticals Inc.; 2004.
2Opana [package insert]. Chadds Ford, Pennsylvania: Endo Pharmaceuticals Inc.; 2006.
For more information on these agents, click here.
Propoxyphene: Short-Acting Agent, Used Alone or in Combination with Acetaminophen or Aspirin (eg, Darvocet®, Darvon®)
Dosage form and route of administration: Oral (capsules, oral suspension, tablets)
Indications: These agents are indicated for the relief of mild-to-moderate pain. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to propoxyphene.
Drug interactions: The effects of CNS depressants, anticonvulsants, and antidepressants may be enhanced when used concomitantly with propoxyphene.
Adverse events: The most frequently reported adverse events associated with this treatment include dizziness, sedation, nausea, vomiting, and psychotomimetic effects in older patients. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1-2
Other cautions: Regular acetaminophen use is associated with hepatocellular enzyme changes. Hepatotoxicity can occur with excessive use of acetaminophen and practitioners need to educate and caution patients about
all the various sources of acetaminophen in OTC and prescription medications. Patients using alcohol on a regular basis, or with a past history of alcohol abuse, should limit acetaminophen use by at
least 50%.
1Darvocet [package insert]. Newport, Kentucky: Xanodyne Pharmaceuticals Inc.; 2006.
2Darvon [package insert]. Newport, Kentucky: Xanodyne Pharmaceuticals Inc.; 2006.
For more information on these agents, click here.
Tramadol: Immediate-Release Formulation, Used Alone or in Combination with Acetaminophen or Aspirin (eg, Ultracet®, Ultram®)
Dosage form and route of administration: Oral (tablets)
Indications: These agents are indicated for the relief of moderate-to-moderately severe pain. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with hypersensitivity, and in any situation in which opioids are contraindicated, including acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids, or psychotropics.
Drug interactions: The effects of CYP 3A4 inhibitors, CYP 2D6 inhibitors, quinidine, carbamazepine, and cimetidine may be enhanced when used concomitantly with tramadol.
Adverse events: The most frequently reported adverse events associated with these agents include drowsiness, dizziness, gastrointestinal upset, nausea, agitation, and constipation. Other adverse events include seizures (usually with overdosage), serotonin syndrome with antidepressants, respiratory depression, and anaphylactoid reactions.
Other cautions: One-half of a 50-mg tablet may be ineffective for many patients, but slow dose escalation is recommended in older and frail patients to avoid untoward cognitive effects. Patients who are elderly or have hepatic dysfunction should take smaller doses at longer intervals. Regular acetaminophen use is associated with hepatocellular enzyme changes. Hepatotoxicity can occur with excessive use of acetaminophen, and practitioners need to educate and caution patients about all the various sources of acetaminophen in OTC and prescription medications. Patients using alcohol on a regular basis, or with a past history of alcohol abuse, should limit acetaminophen use by at least 50%.
1Ultracet [package insert]. Titusville, New Jersey: Ortho-McNeil-Janssen Pharmaceuticals, Inc.; 2003.
2Ultram [package insert]. Titusville, New Jersey: Ortho-McNeil-Janssen Pharmaceuticals, Inc.; 2004.
For more information on these agents, click here.
Opioids: Long-Acting Agents
Fentanyl: Continuous Systemic Delivery Transdermal Agent (Duragesic®)
Dosage form and route of administration: transdermal patch
Indications: Duragesic is indicated for management of persistent, moderate-to-severe chronic pain that requires continuous, around-the-clock opioid administration for an extended period of time and cannot be managed by other means such as non-steroidal analgesics, opioid combination products, or immediate-release opioids. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: Duragesic is contraindicated in patients with hypersensitivity; patients who are opioid-intolerant; for the management of acute, post-operative, mild, or intermittent pain; and in the setting of respiratory depression, acute or severe bronchial asthma, and paralytic ileus. Starting doses for fentanyl must be individualized based on the status of each patient.
Drug Interactions: Patients using Duragesic concomitantly with all cytochrome P450 3A4 inhibitors, agents that affect CYP 3A4 activity, CNS depressants, or MAO inhibitors should be monitored carefully.
Adverse events: The most frequently reported adverse events associated with Duragesic include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, sexual dysfunction due to decreased sex hormone levels with regular use, and bradycardia.
Other cautions: Use of Duragesic with other CNS-depressant drugs, including alcohol, can cause potentially life-threatening respiratory depression, especially during sleep.1
1Duragesic [package insert]. Titusville, New Jersey: Ortho-McNeil-Janssen Pharmaceuticals, Inc.; 2008.
For more information on Duragesic, click here.
Warning: Deaths and Serious Injuries from Improper Use of Fentanyl Skin Patch. December 21, 2007.
Levorphanol: Pharmacologically Long-Acting Agent With Long Half-Life (Levo Dromoran®)
Dosage form and route of administration: Oral (tablets); Parenteral (intravenous [IV], intramuscular, or subcutaneous injection)
Indications: Levo Dromoran is indicated for the management of moderate-to-severe pain or as a preoperative medication in a setting in which an opioid analgesic is appropriate. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: Levo Dromoran is contraindicated in patients with known intolerance or hypersensitivity
to levorphanol.
Drug interactions: The effects of other opioid analgesics, antihistamines, antipsychotics, antianxiety agents, CNS depressants, MAO inhibitors, or TCAs may be enhanced when used concomitantly with levorphanol.
Adverse events: The most frequently reported adverse events associated with Levo Dromoran include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1
1Levo Dromoran [package insert]. Aliso Viejo, California: Valeant Pharmaceuticals International; 2004.
For more information on Levo Dromoran, click here.
Methadone: Pharmacologically Long-Acting Agent With Long Half-Life (Dolophine®, Methadose™)
Dosage form and route of administration: Oral (tablets, oral concentrate, and dispersible tablets)
Indications: These agents are indicated for the treatment of moderate-to-severe pain not responsive to non-narcotic analgesics; for detoxification treatment of opioid addiction (heroin or other morphine-like drugs);
and for maintenance treatment of opioid addiction in conjunction with appropriate social and medical services. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to methadone.
Drug interactions: The effects of pentazocine, desipramine, MAO inhibitors, CNS depressants, anti-retroviral agents, and CYP 3A4 inducers and inhibitors may be enhanced when used concomitantly with methadone.
Adverse events: The most frequently reported adverse events associated with this treatment include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1-2
Other cautions: Dolophine and Methadose have a highly variable half-life that makes titration and related pharmacodynamic effects unpredictable. Doses may accumulate, leading to accidental overdose, especially during sleep. Concomitant use of other CNS depressants increases this risk. Methadone has dose-related effects on cardiac QT interval that can lead to fatal arrhythmias. Use of methadone for acute or chronic pain control should be under the supervision of a physician with considerable experience with methadone and outpatient administration.
1Dolophine [package insert]. Columbus, Ohio: Boehringer Ingelheim Roxane, Inc.; 2006.
2Methadose [package insert]. St. Louis, Missouri: Mallinckrodt Inc.; 2008.
For more information on these agents, click here.
Warning: Methadone Use May Result in Death and Life-Threatening Changes. Updated July 2007.
Morphine: Controlled-, Extended-, and Sustained-Release Formulations (Avinza®,
Duramorph®, Kadian®)
Dosage form and route of administration: Oral (tablets and capsules swallowed whole); Parenteral (injection [IV, epidural, intrathecal])
Indications: These agents are indicated for the relief of moderate-to-severe pain requiring continuous, around-the-clock opioid therapy for an extended period of time. Duramorph is a systemic narcotic analgesic for administration by the IV, epidural, or intrathecal routes. It is used for the management of pain not responsive to non-narcotic analgesics. Duramorph administered epidurally or intrathecally provides pain relief for extended periods without attendant loss of motor, sensory, or sympathetic function. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to morphine.
Drug interactions: The effects of MAO inhibitors, antihistamines, TCAs, anticholinergics, phenothiazines, tranquilizers, and sedatives may be enhanced when used concomitantly with morphine.
Adverse events: The most frequently reported adverse events associated with this treatment include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1-3
Other cautions: Concomitant use of modified-release opioids (ie, CR, SR, or ER formulations) with alcohol may result in increased plasma levels, leading to accidental overdose.
1Avinza [package insert].San Diego, California: Ligand Pharmaceuticals Incorporated; 2003.
2Duramorph [package insert]. Deerfield, Illinois: Baxter Healthcare Corporation; 2005.
3Kadian [package insert]. Piscataway, New Jersey: Alpharma Pharmaceuticals LLC; 2007.
For more information on these agents, click here.
Oxycodone: Controlled-, Sustained-Released Formulation (OxyContin®)
Dosage form and route of administration: Oral (tablets swallowed whole)
Indications: OxyContin is indicated for the management of relief of moderate-to-severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: These agents are contraindicated in patients with known intolerance or hypersensitivity
to oxycodone.
Drug interactions: The effects of other opioid analgesics, CNS depressants, anticholinergics, phenothiazines, tranquilizers, sedatives, amiodarone, quinidine, and polycyclic antidepressants may be enhanced when used concomitantly with oxycodone.
Adverse events: The most frequently reported adverse events associated with this treatment include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1
Other cautions: Concomitant use of modified-release opioids (ie, CR, SR, or ER formulations) with alcohol may result in increased plasma levels, leading to accidental overdose.
1OxyContin [package insert]. Stamford, Connecticut: Purdue Pharma L.P.; 2008.
For more information on OxyContin, click here.
Warning: FDA Strengthens Warnings for OxyContin. July 25, 2001.
Oxymorphone: Extended-Release Formulation (Opana® ER)
Dosage form and route of administration: Oral (tablets swallowed whole)
Indications: Opana ER is indicated for the relief of moderate-to-severe pain in patients requiring continuous, around-the-clock opioid treatment for an extended period of time. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: Opana ER is contraindicated in patients with known intolerance or hypersensitivity to the agents, and in patients with pain in the immediate post-operative period (first 12–24 hours), mild pain, paralytic ileus, and moderate and severe hepatic impairment.
Drug interactions: The effects of opioid analgesics, CNS depressants and opioid agonist and antagonist analgesics may be enhanced when used concomitantly with Opana ER.
Adverse events: The most frequently reported adverse events associated with this treatment include sedation, drowsiness, dizziness, nausea, constipation, itching/hives, urinary hesitancy, and sexual dysfunction due to decreased sex hormone levels with regular use. Other adverse events include respiratory depression, physical and psychological dependence, and opioid tolerance.1
Other cautions: Concomitant use of modified-release opioids (ie, CR, SR, or ER formulations) with alcohol may result in increased plasma levels, leading to accidental overdose.
1Opana ER [package insert]. Chadds Ford, Pennsylvania: Endo Pharmaceuticals Inc.; 2006.
For more information on this agent, click here.
Tramadol: Extended-Release Formulation (Ultram®, ER)
Dosage form and route of administration: Oral (tablets swallowed whole)
Indications: Ultram ER is indicated for the management of moderate-to-moderately severe chronic pain in adults who require around-the-clock treatment of their pain for an extended period of time. In patients receiving opioids, the dose and duration of analgesia will vary substantially depending on the patient’s opioid tolerance.
Contraindications: Ultram ER is contraindicated in patients with hypersensitivity and in any situation in which opioids are contraindicated, including acute intoxication with alcohol, hypnotics, and use of centrally acting analgesics, opioids, or psychotropics.
Drug Interactions: The effects of CYP 3A4 inhibitors, CYP 2D6 inhibitors, quinidine, carbamazepine, and cimetidine may be enhanced when used concomitantly with tramadol.
Adverse events: The most frequently reported adverse events associated with this treatment include drowsiness, dizziness, gastrointestinal upset, nausea, agitation, and constipation. Other adverse events include seizures (usually with overdosage), serotonin syndrome with antidepressants, respiratory depression, and anaphylactoid reactions.
1Ultram ER [package insert]. Titusville, New Jersey: Ortho-McNeil-Janssen Pharmaceuticals, Inc.; 2006.
For more information on Ultram ER, click here.