Meperidine (oral)

{{DrugProjectFormSinglePage |authorTag=Chetan Lokhande, M.B.B.S [1] |genericName=Meperidine |aOrAn=a |drugClass=analgesic opioid |indication=Anesthesia; obstetric pain, pain (moderate to severe), premedication for procedure |adverseReactions=dermatologic: sweating, gastrointestinal: nausea, vomiting, neurologic: dizziness, lightheadedness, sedated |blackBoxWarningTitle=TITLE |blackBoxWarningBody=Condition Name: (Content) |fdaLIADAdult=* Anesthesia; Adjunct: repeated slow IV injections of fractional doses (eg, 10 mg/mL) or continuous IV infusion of more dilute solution (eg, 1 mg/mL); titrate to needs of patient.

• Obstetric pain: 50 to 100 mg IM/subQ every 1 to 3 hours as needed.
• Pain (Moderate to Severe): 50 to 150 mg IM/ORAL/subQ every 3 to 4 hours as needed.
• Pain (Moderate to Severe): (patient-controlled-analgesia), usual dose 10 mg IV administered slowly (range, 1 to 5 mg per incremental dose), lock-out period 6 to 10 minutes; minimum lock-out period 5 minutes; dose, lock-out periods, limits depend on patient status and response.
• Pain (Moderate to Severe): continuous IV infusion, 15 to 35 mg/hr as required; administer slowly.
• Premedication for procedure: 50 to 150 mg IM/subQ 30 to 90 minutes before start of anesthesia

|offLabelAdultGuideSupport=* Anesthetics adverse reaction - Shivering |offLabelAdultNoGuideSupport=* There is limited information about Off-Label Non–Guideline-Supported Use of Meperidine in adult patients. |fdaLIADPed=* Safety and effectiveness of oral meperidine in pediatric patients have not been established; IV meperidine administered via patient-controlled-analgesia syringe pump is not recommended in patients younger than 19 years of age.

• Pain (Moderate to Severe): 1.1 to 1.8 mg/kg IM/ORAL/subQ up to adult dose every 3 to 4 hours as needed.
• Premedication for procedure: 1.1 to 2.2 mg/kg IM/subQ up to adult dose 30 to 90 minutes before start of anesthesia

|offLabelPedGuideSupport=There is limited information about Off-Label Guideline-Supported Use of Meperidine in pediatric patients. |offLabelPedNoGuideSupport=There is limited information about Off-Label Non–Guideline-Supported Use of Meperidine in pediatric patients. |contraindications=* Meperidine 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.)
• Meperidine is contraindicated in patients with severe respiratory insufficiency (see Warnings, respiratory conditions).

|warnings=* Meperidine should not be used for treatment of chronic pain. Meperidine should only be used in the treatment of acute episodes of moderate to severe pain. Prolonged meperidine use may increase the risk of toxicity (e.g. seizures) from the accumulation of the meperidine metabolite, normeperidine.

• Meperidine is an opioid agonist and a Schedule II controlled substance with an abuse liability similar to morphine.
• Meperidine can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing Meperidine in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion.

• Misuse, Abuse, and Diversion of Opioids

• Meperidine is an opioid agonist of the morphine-type. Such drugs are sought by drug abusers and people with addiction disorders and are subject to criminal diversion.
• Meperidine can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing Meperidine in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion.
• Meperidine has been reported as being abused by crushing, chewing, snorting, or injecting the dissolved product. These practices will result in the uncontrolled delivery of the opioid and pose a significant risk to the abuser that could result in overdose or death (see Warnings And Drug Abuse And Addiction).
• Concerns about abuse, addiction, and diversion should not prevent the proper management of pain.
• Healthcare professionals should contact their State Professional Licensing Board or State Controlled Substances Authority for information on how to prevent and detect abuse or diversion of this product.

• Interactions with Alcohol and Drugs of Abuse

• Meperidine may be expected to have additive effects when used in conjunction with alcohol, other opioids, or illicit drugs that cause central nervous system depression.

• Head Injury and Increased Intracranial Pressure

• The respiratory depressant effects of meperidine and its capacity to elevate cerebrospinal fluid pressure may be markedly exaggerated in the presence of head injury, other intracranial lesions, or a preexisting increase in intracranial pressure. Furthermore, narcotics produce adverse reactions which may obscure the clinical course of patients with head injuries. In such patients, meperidine must be used with extreme caution and only if its use is deemed essential.

• Respiratory Conditions

• Meperidine should be used with extreme caution in patients having an acute asthmatic attack, patients with chronic obstructive pulmonary disease or cor pulmonale, patients having a substantially decreased respiratory reserve, and patients with preexisting respiratory depression, hypoxia, or hypercapnia. In such patients, even usual therapeutic doses of narcotics may decrease respiratory drive while simultaneously increasing airway resistance to the point of apnea.

• Hypotensive Effect

• The administration of meperidine may result in severe hypotension in the postoperative patient or any individual whose ability to maintain blood pressure has been compromised by a depleted blood volume or the administration of drugs such as the phenothiazines or certain anesthetics.

• Usage in Ambulatory Patients

• Meperidine may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks such as driving a car or operating machinery. The patient should be cautioned accordingly.
• Meperidine, like other narcotics, may produce orthostatic hypotension in ambulatory patients.

• Usage in Pregnancy

• Meperidine should not be used in pregnant women prior to the labor period, unless in the judgment of the physician the potential benefits outweigh the possible risks, because safe use in pregnancy prior to labor has not been established relative to possible adverse effects on fetal development.

• Labor and Delivery

• Meperidine crosses the placental barrier and can produce depression of respiration and psychophysiologic functions in the newborn. Resuscitation may be required (see OVERDOSAGE). Therefore meperidine is not recommended during labor.

• Nursing Mothers

• Meperidine appears in the milk of nursing mothers receiving the drug. Due to the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the potential benefits of the drug to the nursing woman.

|clinicalTrials=* 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.

|drugInteractions=* 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 Meperidine 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 Meperidine, may enhance the neuromuscular blocking action of skeletal muscle relaxants and produce an increased degree of respiratory depression.

|FDAPregCat=C |useInPregnancyFDA=* Animal reproduction studies have not been conducted with meperidine. It is also not known whether Meperidine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Meperidine should be given to a pregnant woman only if clearly needed. |useInLaborDelivery=* Meperidine crosses the placental barrier and can produce depression of respiration and psychophysiologic functions in the newborn. Resuscitation may be required (see OVERDOSAGE). Therefore meperidine is not recommended during labor. |useInNursing=* Meperidine appears in the milk of nursing mothers receiving the drug. Due to the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the potential benefits of the drug to the nursing woman. |useInPed=* 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. |useInGeri=* Clinical studies of Meperidine 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. |useInRenalImpair=* 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. |useInHepaticImpair=* 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. |overdose=* 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 Meperidine 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.

|drugBox=

Meperidine (oral)
Systematic (IUPAC) name
Ethyl 1-methyl-4-phenylpiperidine-4-carboxylate
Identifiers
CAS number	57-42-1
ATC code	N02AB02
PubChem	4058
DrugBank	DB00454
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	247.33g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	50–60% (Oral), 80-90% (Oral, in cases of hepatic impairment)
Protein binding	65-75%
Metabolism	Liver
Half life	2.5-4 hours, 7-11 hours (liver disease)
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status	Controlled (S8)(AU) Schedule I(CA) Class A(UK) Schedule II(US) Class B3 (NZ)
Routes	oral, intravenous, intramuscular, subcutaneous

|mechAction=* Meperidine hydrochloride is a narcotic analgesic with multiple actions qualitatively similar to those of morphine; the most prominent of these involve the central nervous system and organs composed of smooth muscle. The principal actions of therapeutic value are analgesia and sedation.

• There is some evidence which suggests that meperidine may produce less smooth muscle spasm, constipation, and depression of the cough reflex than equianalgesic doses of morphine.

|structure=* 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 Meperidine brand of meperidine hydrochloride.
• Inactive Ingredients: Calcium Sulfate, Dibasic Calcium Phosphate, Starch, Stearic Acid, Talc.
• Chemically, Meperidine is 4-Piperidinecarboxylic acid, 1-methyl-4-phenyl-, ethyl ester, hydrochloride and has the following structure:

This image is provided by the National Library of Medicine.

|howSupplied=* 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).

|storage=* Store at 25° C (77° F); excursions permitted to 15° – 30° C (59° – 86° F) [See USP Controlled Room Temperature]. Revised November 2011 Manufactured for: sanofi-aventis U.S. LLC Bridgewater, NJ 08807 ©2011 sanofi-aventis U.S. LLC |fdaPatientInfo=* If clinically advisable, patients receiving DEMEROL (meperidine hydrochloride) tablets or their caregivers should be given the following information by the physician, nurse, pharmacist, or caregiver:

• Patients should be aware that Meperidine tablets contain meperidine, which is a morphine-like substance.
• Patients should be advised to report pain and adverse experiences occurring during therapy. Individualization of dosage is essential to make optimal use of this medication.
• Patients should be advised not to adjust the dose of Meperidine without consulting the prescribing professional.
• Patients should be advised that Meperidine may impair mental and/or physical ability required for the performance of potentially hazardous tasks (e.g., driving, operating heavy machinery).
• Patients should not combine Meperidine with alcohol or other central nervous system depressants (sleep aids, tranquilizers) except by the orders of the prescribing physician, because dangerous additive effects may occur, resulting in serious injury or death.
• Women of childbearing potential who become, or are planning to become pregnant should be advised to consult their physician regarding the effects of analgesics and other drug use during pregnancy on themselves and their unborn child.
• Patients should be advised that Meperidine is a potential drug of abuse. They should protect it from theft, and it should never be given to anyone other than the individual for whom it was prescribed.
• Patients should be advised that if they have been receiving treatment with Meperidine for more than a few weeks and cessation of therapy is indicated, it may be appropriate to taper the Meperidine dose, rather than abruptly discontinue it, due to the risk of precipitating withdrawal symptoms. Their physician can provide a dose schedule to accomplish a gradual discontinuation of the medication.
• Patients should be instructed to keep Meperidine in a secure place out of the reach of children. When Meperidine is no longer needed, the unused tablets should be destroyed by flushing down the toilet.

|alcohol=* Alcohol-Meperidine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication. }} {{#subobject:

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