Meperidine hydrochloride is a white crystalline substance with a melting point of 186° C to 189° C. It is readily soluble in water and has a neutral reaction and a slightly bitter taste. The solution is not decomposed by a short period of boiling. The tablets contain 50 mg or 100 mg of DEMEROL brand of meperidine hydrochloride. Inactive Ingredients: Calcium Sulfate, Dibasic Calcium Phosphate, Starch, Stearic Acid, Talc. Chemically, DEMEROL is 4-Piperidinecarboxylic acid, 1-methyl-4-phenyl-, ethyl ester, hydrochloride and has the following structure:

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The major hazards of meperidine, as with other narcotic analgesics, are respiratory depression and, to a lesser degree, circulatory depression; respiratory arrest, shock, and cardiac arrest have occurred. The most frequently observed adverse reactions include lightheadedness, dizziness, sedation, nausea, vomiting, and sweating. These effects seem to be more prominent in ambulatory patients and in those who are not experiencing severe pain. In such individuals, lower doses are advisable. Some adverse reactions in ambulatory patients may be alleviated if the patient lies down. Other adverse reactions include: Nervous System: Mood changes (e.g. euphoria, dysphoria), weakness, headache, agitation, tremor, involuntary muscle movements (e.g. muscle twitches, myoclonus), severe convulsions, transient hallucinations and disorientation, confusion, delirium, visual disturbances. Gastrointestinal: Dry mouth, constipation, biliary tract spasm. Cardiovascular: Flushing of the face, tachycardia, bradycardia, palpitation, hypotension (see WARNINGS), syncope. Genitourinary: Urinary retention. Allergic: Pruritus, urticaria, other skin rashes, wheal and flare over the vein with intravenous injection. Hypersensitivity reactions, anaphylaxis. Histamine release leading to hypotension and/or tachycardia, flushing, sweating, and pruritus. Drug Abuse And Addiction DEMEROL contains meperidine, a mu-agonist opioid with an abuse liability similar to morphine and is a Schedule II controlled substance. Meperidine, like morphine and other opioids used in analgesia, can be abused and is subject to criminal diversion. Drug addiction is characterized by compulsive use, use for non-medical purposes, and continued use despite harm or risk of harm. Drug addiction is a treatable disease, utilizing a multi-disciplinary approach, but relapse is common. “Drug seeking” behavior is very common in addicts and drug abusers. Drug-seeking tactics include emergency calls or visits near the end of office hours, refusal to undergo appropriate examination, testing or referral, repeated “loss” of prescriptions, tampering with prescriptions and reluctance to provide prior medical records or contact information for other treating physician(s). “Doctor shopping” to obtain additional prescriptions is common among drug abusers and people suffering from untreated addiction. Abuse and addiction are separate and distinct from physical dependence and tolerance. Physicians should be aware that addiction may not be accompanied by concurrent tolerance and symptoms of physical dependence in all addicts. In addition, abuse of opioids can occur in the absence of true addiction and is characterized by misuse for non-medical purposes, often in combination with other psychoactive substances. DEMEROL, like other opioids, has been diverted for non-medical use. Careful record-keeping of prescribing information, including quantity, frequency, and renewal requests is strongly advised. Abuse of DEMEROL poses a risk of overdose and death. This risk is increased with concurrent abuse of DEMEROL with alcohol and other substances. Due to the presence of talc as one of the excipients in tablets, parenteral abuse of crushed tablets can be expected to result in local tissue necrosis, infection, pulmonary granulomas, and increased risk of endocarditis and valvular heart disease. In addition, parenteral drug abuse is commonly associated with transmission of infectious diseases such as hepatitis and HIV. Proper assessment of the patient, proper prescribing practices, periodic re-evaluation of therapy, and proper dispensing and storage are appropriate measures that help to limit abuse of opioid drugs. Read the Demerol (meperidine) Side Effects Center for a complete guide to possible side effectsLearn More »

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For Relief of Pain Dosage should be adjusted according to the severity of the pain and the response of the patient. Meperidine is less effective orally than on parenteral administration. The dose of DEMEROL should be proportionately reduced (usually by 25 to 50 percent) when administered concomitantly with phenothiazines and many other tranquilizers since they potentiate the action of DEMEROL. Adults: The usual dosage is 50 mg to 150 mg orally, every 3 or 4 hours as necessary. Pediatric Patients: The usual dosage is 1.1 mg/kg to 1.8 mg/kg orally, up to the adult dose, every 3 or 4 hours as necessary (see PRECAUTIONS, Pediatric use). Safety And Handling DEMEROL (meperidine HCl) tablets contain meperidine hydrochloride which is a controlled substance. Like morphine, meperidine is controlled under Schedule II of the Controlled Substances Act. Meperidine, like all opioids, is liable to diversion and misuse and should be handled accordingly. Patients and their families should be instructed to flush DEMEROL tablets that are no longer needed. DEMEROL has been targeted for theft and diversion by criminals. Healthcare professionals should contact their State Professional Licensing Board or State Controlled Substance Authority for information on how to prevent and detect abuse or diversion of this product.

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Also see WARNINGS. Acyclovir: Plasma concentrations of meperidine and its metabolite, normeperidine, may be increased by acyclovir, thus caution should be used with concomitant administration. Cimetidine: Cimetidine reduced the clearance and volume of distribution of meperidine and also the formation of the metabolite, normeperidine, in healthy subjects and thus, caution should be used with concomitant administration. CNS Depressants: Concomitant use of CNS depressants with usual doses of Demerol may result in respiratory depression, hypotension, profound sedation, coma or death (see PRECAUTIONS, Interactions with other CNS Depressants). Phenytoin: The hepatic metabolism of meperidine may be enhanced by phenytoin. Concomitant administration resulted in reduced half-life and bioavailability with increased clearance of meperidine in healthy subjects, however, blood concentrations of normeperidine were increased, thus exercise caution when phenytoin is used concomitantly with meperidine. Ritonavir: Plasma concentrations of the active metabolite normeperidine may be increased by ritonavir, thus concomitant administration should be avoided. Opioid analgesics, including DEMEROL, may enhance the neuromuscular blocking action of skeletal muscle relaxants and produce an increased degree of respiratory depression. Special Risk Patients Meperidine should be given with caution and the initial dose should be reduced in certain patients such as the elderly or debilitated, and those with severe impairment of hepatic or renal function, Sickle Cell Anemia, hypothyroidism, Addison's disease, Pheochromocytoma and prostatic hypertrophy or urethral stricture. In patients with pheochromocytoma, meperidine has been reported to provoke hypertension. Usage in Hepatically Impaired Patients Accumulation of meperidine and/or its active metabolite, normeperidine, can occur in patients with hepatic impairment. Meperidine should therefore be used with caution in patients with hepatic impairment. Usage in Renally Impaired Patients Accumulation of meperidine and/or its active metabolite, normeperidine, can also occur in patients with renal impairment. Meperidine should therefore be used with caution in patients with renal impairment.Read the Demerol Drug Interactions Center for a complete guide to possible interactions Learn More »

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DEMEROL is indicated for the relief of moderate to severe pain.

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DEMEROL is contraindicated in patients with hypersensitivity to meperidine or to any of its ingredients. Meperidine is contraindicated in patients who are receiving monoamine oxidase (MAO) inhibitors or those who have recently received such agents. Therapeutic doses of meperidine have occasionally precipitated unpredictable, severe, and occasionally fatal reactions in patients who have received such agents within 14 days. The mechanism of these reactions is unclear, but may be related to a preexisting hyperphenylalaninemia. Some have been characterized by coma, severe respiratory depression, cyanosis, and hypotension, and have resembled the syndrome of acute narcotic overdose. Serotonin syndrome with agitation, hyperthermia, diarrhea, tachycardia, sweating, tremors and impaired consciousness may also occur. In other reactions the predominant manifestations have been hyperexcitability, convulsions, tachycardia, hyperpyrexia, and hypertension. Although it is not known that other narcotics are free of the risk of such reactions, virtually all of the reported reactions have occurred with meperidine. If a narcotic is needed in such patients, a sensitivity test should be performed in which repeated, small, incremental doses of morphine are administered over the course of several hours while the patient's condition and vital signs are under careful observation. (Intravenous hydrocortisone or prednisolone have been used to treat severe reactions, with the addition of intravenous chlorpromazine in those cases exhibiting hypertension and hyperpyrexia. The usefulness and safety of narcotic antagonists in the treatment of these reactions is unknown.) DEMEROL is contraindicated in patients with severe respiratory insufficiency (see WARNINGS, Respiratory Conditions). Last reviewed on RxList: 11/9/2011
This monograph has been modified to include the generic and brand name in many instances.

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Symptoms Serious overdosage with meperidine is characterized by respiratory depression (a decrease in respiratory rate and/or tidal volume, Cheyne-Stokes respiration, cyanosis), extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, hypothermia, cold and clammy skin, and sometimes bradycardia and hypotension. In severe overdosage, particularly by the intravenous route, apnea, circulatory collapse, cardiac arrest, and death may occur. Treatment Primary attention should be given to the reestablishment of adequate respiratory exchange through provision of a patent airway and institution of assisted or controlled ventilation. The narcotic antagonist, naloxone hydrochloride, is a specific antidote against respiratory depression which may result from overdosage or unusual sensitivity to narcotics, including meperidine. Therefore, an appropriate dose of this antagonist should be administered as necessary, preferably by the intravenous route, simultaneously with efforts at respiratory resuscitation. An antagonist should not be administered in the absence of clinically significant respiratory or cardiovascular depression. Oxygen, intravenous fluids, vasopressors, and other supportive measures should be employed as indicated. In cases of overdosage with DEMEROL tablets, the stomach should be evacuated by emesis or gastric lavage. NOTE: In an individual physically dependent on narcotics, the administration of the usual dose of a narcotic antagonist will precipitate an acute withdrawal syndrome. The severity of this syndrome will depend on the degree of physical dependence and the dose of antagonist administered. The use of narcotic antagonists in such individuals should be avoided if possible. If a narcotic antagonist must be used to treat serious respiratory depression in the physically dependent patient, the antagonist should be administered with extreme care and only one-fifth to one-tenth the usual initial dose administered.

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For Oral Use Tablets are white, round and convex. The 50 mg is a scored tablet and has a stylized “W” on one side and “D” over “35” on the other side. The 100 mg is not a scored tablet and has a stylized “W” on one side and “D” over “37” on the other side. Tablets of 50 mg, HDPE plastic bottles of 100 (NDC 0024-0335-05) and 100 mg, HDPE plastic bottles of 100 (NDC 0024-0337-05). Store at 25° C (77° F); excursions permitted to 15° - 30° C (59° - 86° F) [See USP Controlled Room Temperature]. Revised October 2011. Manufactured for: sanofi-aventis U.S. LLC Bridgewater, NJ 08807.Last reviewed on RxList: 11/9/2011
This monograph has been modified to include the generic and brand name in many instances.

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General Opioid analgesics can have a narrow therapeutic index in certain patient populations, particularly when combined with CNS depressant drugs. The use of these products should be reserved for cases where the benefits of opioid analgesia outweigh the known risks of respiratory depression, altered mental state, and postural hypotension. Use of DEMEROL may be associated with increased potential risks and should be used with caution in the following conditions: sickle cell anemia, pheochromocytoma, acute alcoholism; adrenocortical insufficiency (e.g., Addison's disease); CNS depression or coma; delirium tremens; debilitated patients; kyphoscoliosis associated with respiratory depression; myxedema or hypothyroidism; prostatic hypertrophy or urethral stricture; severe impairment of hepatic, pulmonary, or renal function; and toxic psychosis (see PRECAUTIONS, Special Risk Patients). The administration of meperidine may obscure the diagnosis or clinical course in patients with acute abdominal conditions. All opioids may induce or aggravate seizures in some clinical settings. Interactions with Other CNS Depressants DEMEROL should be used with caution and consideration should be given to starting with a reduced dosage in patients who are concurrently receiving other central nervous system depressants including sedatives or hypnotics, general anesthetics, phenothiazines, other tranquilizers, and alcohol. Drug-drug interactions may result in respiratory depression, hypotension, profound sedation,coma, or death if these drugs are taken in combination with the usual doses of DEMEROL. Interactions with Mixed Agonist/Antagonist Opioid Analgesics Agonist/antagonist analgesics (i.e., pentazocine, nalbuphine, butorphanol, and buprenorphine) should be administered with caution to a patient who has received or is receiving a course of therapy with a pure opioid agonist analgesic such as meperidine. In this situation, mixed agonist/antagonist analgesics may reduce the analgesic effect of meperidine and/or may precipitate withdrawal symptoms in these patients due to competitive blocking of receptors. Supraventricular Tachycardias Meperidine should be used with caution in patients with atrial flutter and other supraventricular tachycardias because of a possible vagolytic action which may produce a significant increase in the ventricular response rate. Convulsions Meperidine may aggravate preexisting convulsions in patients with convulsive disorders. If dosage is escalated substantially above recommended levels because of tolerance development, convulsions may occur in individuals without a history of convulsive disorders. Acute Abdominal Conditions The administration of meperidine or other narcotics may obscure the diagnosis or clinical course in patients with acute abdominal conditions. Tolerance and Physical Dependence Meperidine has the potential to produce tolerance and drug dependence. Tolerance is the need for increasing doses of opioids to maintain a defined effect such as analgesia (in the absence of disease progression or other external factors). Physical dependence is manifested by withdrawal symptoms after abrupt discontinuation of a drug or upon administration of an antagonist. Physical dependence and tolerance are not unusual during chronic opioid therapy. The opioid abstinence or withdrawal syndrome is characterized by some or all of the following: restlessness, lacrimation, rhinorrhea, yawning, perspiration, chills, myalgia, mydriasis. Other symptoms also may develop, including: irritability, anxiety, backache, joint pain, weakness, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhea, or increased blood pressure, respiratory rate, or heart rate. In general, opioids used regularly should not be abruptly discontinued. Use in Drug and Alcohol Addiction DEMEROL is an opioid with no approved use in the management of addictive disorders. Its proper usage in individuals with drug or alcohol dependence, either active or in remission, is for the management of pain requiring opioid analgesia. DEMEROL should be used with caution in patients with alcoholism and other drug dependencies due to the increased frequency of narcotic tolerance, dependence, and the risk of addiction observed in these patient populations. Abuse of DEMEROL in combination with other CNS depressant drugs can result in serious risk to the patient. Carcinogenesis, Mutagenesis, Impairment of Fertility Studies to assess the carcinogenic or mutagenic potential of meperidine have not been conducted. Studies to determine the effect of meperidine on fertility have not been conducted. Pregnancy: Teratogenic Effects Pregnancy Category C: Animal reproduction studies have not been conducted with meperidine. It is also not known whether DEMEROL can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. DEMEROL should be given to a pregnant woman only if clearly needed. Labor and Delivery See WARNINGS. Nursing Mothers See WARNINGS. Pediatric Use The safety and effectiveness of meperidine in pediatric patients has not been established. Literature reports indicate that meperidine has a slower elimination rate in neonates and young infants compared to older children and adults. Neonates and young infants may also be more susceptible to the effects, especially the respiratory depressant effects. If meperidine use is contemplated in neonates or young infants, any potential benefits of the drug need to be weighed against the relative risk of the patient. Geriatric Use Clinical studies of DEMEROL during product development did not include sufficient numbers of subjects aged 65 and over to evaluate age-related differences in safety or efficacy. Literature reports indicate that geriatric patients have a slower elimination rate compared to young patients and they may be more susceptible to the effects of meperidine. Reducing the total daily dose of meperidine is recommended in elderly patients and the potential benefits of the drug should be weighed against the relative risk to a geriatric patient.Last reviewed on RxList: 11/9/2011
This monograph has been modified to include the generic and brand name in many instances.

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