Levorphanol Tartrate 2 mg Tablet, 100-count — NDC 0406-2224-01 (Billing 00406-2224-01)
This is a package of 100 tablets of Levorphanol Tartrate 2 mg Tablet from SpecGx LLC, marketed since Dec 2019 and currently FDA-listed; retail pharmacies pay about $10.65 per tablet (NADAC). It is this product's only package size.
Identity & classification
Regulatory identifiers FDA, NLM and CMS codes for this package
Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification
- GSN (GCN sequence number): 004228
- GCN: 16350
- GPI-14 (Medi-Span): 65100040100305
- HICL (First Databank): 001743
- AHFS class code: 28:08.08.00
- RxCUI (RxNorm): 197873
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
- RxNorm (NLM RxNav) · catalog refreshed Oct 1, 2026
- Medi-Span GPI (licensed)
- First Databank (licensed) · refreshed Oct 1, 2026
RxNorm drug class
This medicine belongs to the Opioid Agonist class.
Where does this data come from?
- RxClass (NLM) · catalog refreshed Oct 1, 2026
Clinical
- It treats severe pain that needs an opioid when other treatments haven't worked or can't be tolerated. It isn't meant for long-term use unless your pain remains severe and other op...
- You take the tablets by mouth, usually every 6 to 8 hours as needed for pain. Your prescriber will aim for the lowest dose that works for the shortest time. Don't take extra, and a...
- Nausea, vomiting, constipation, dizziness, itching, flushing, dry mouth and trouble urinating are common with opioids. Call your doctor if they bother you. Slow breathing, extreme...
- Avoid alcohol. Mixing it with benzodiazepines, sleep or anxiety medicines, muscle relaxants, gabapentin or other opioids can cause dangerous sedation and slowed breathing. Tell me...
Patient education
Supplement & herbal interactions
Where does this data come from?
- MedlinePlus (NLM) · refreshed Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
Ask a licensed pharmacist directly — free, answered by our team.
Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $10.646 | $1,064.56 / 100 tablets |
| Medicaid paysCMS SDUD · 12 mo | $14.69 | $1,469.29 / 100 tablets |
| Medicare drug plans payPart D · Q2 2026 | $34.92 | $3,492.04 / 100 tablets |
Where does this data come from?
- CMS NADAC weekly file · file of Sep 30, 2026
- CMS ASP pricing files · refreshed Sep 20, 2026
- CMS Medicaid State Drug Utilization Data · through Q1 2026
- CMS Part D plan pricing files · refreshed Sep 24, 2026
- VA National Acquisition Center price file
Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Marketing end | Status |
|---|---|---|---|---|
| 00406-2224-01 You're viewing this Main listing | 100 TABLET in 1 BOTTLE, PLASTIC | 2019-12-13 | — | Active |
Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Levorphanol Tartrate 2 mg 00054-0438-25 | Hikma | 100 tablets | $10.646 | AB | Availability likely | — |
| Levorphanol Tartrate 2 mgthis 00406-2224-01 | SpecGx | 100 tablets | $10.646 | AB | Availability likely | — |
| Levorphanol Tartrate 2 mg 00527-3236-37 | Lannett | 100 tablets | $10.646 | BX | Availability likely | — |
| Levorphanol Tartrate 2 mg 57664-0762-88 | Sun | 100 tablets | $10.646 | AB | Availability likely | — |
| Levorphanol Tartrate 2 mg 69543-0417-10 | Virtus | 100 tablets | $10.646 | AB | Availability likely | — |
| Levorphanol Tartrate 2 mg 72989-0417-10 | ACERTIS | 100 tablets | $10.646 | AB | Availability likely | — |
| Levorphanol Tartrate 2 mg 63629-2093-01 | Bryant | 100 tablets | — | BX | FDA listed | — |
| Levorphanol Tartrate 2 mg 72162-2309-01 | Bryant | 100 tablets | — | AB | FDA listed | — |
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA Orange Book · refreshed Sep 3, 2026
- CMS NADAC weekly file · file of Sep 30, 2026
Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
- FDA Orange Book · refreshed Sep 3, 2026
Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
Where does this data come from?
IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.- FDA label on DailyMed · label index refreshed Oct 1, 2026
- FDA openFDA NDC Directory · synced Oct 1, 2026
Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
Manufacturer & labeler
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- Drugs@FDA
Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF LEVORPHANOL TARTRATE TABLETS Addiction, Abuse, and Misuse Because the use of Levorphanol Tartrate Tablets exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death, assess each patient’s risk prior to prescribing and reassess all patients regularly for the development of these behaviors and conditions ( see WARNINGS ). Life-Threatening Respiratory Depression Serious, life-threatening, or fatal respiratory depression may occur with use of Levorphanol Tartrate Tablets, especially during initiation or following a dosage increase.
To reduce the risk of respiratory depression, proper dosing and titration of Levorphanol Tartrate Tablets are essential ( see WARNINGS ). Accidental Ingestion Accidental ingestion of even one dose of Levorphanol Tartrate Tablets, especially by children, can result in a fatal overdose of levorphanol ( see WARNINGS ). Risks from Concomitant Use with Benzodiazepines or Other CNS Depressants Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death.
Reserve concomitant prescribing of Levorphanol Tartrate Tablets and benzodiazepines or other CNS depressants for use in patients for whom alternative treatment options are inadequate ( see WARNINGS ). Neonatal Opioid Withdrawal Syndrome (NOWS) Advise pregnant women using opioids for an extended period of time of the risk of Neonatal Opioid Withdrawal Syndrome, which may be life-threatening if not recognized and treated. Ensure that management by neonatology experts will be available at delivery ( see WARNINGS ).
Opioid Analgesic Risk Evaluation and Mitigation Strategy (REMS) Healthcare providers are strongly encouraged to complete a REMS-compliant education program and to counsel patients and caregivers on serious risks, safe use, and the importance of reading the Medication Guide with each prescription ( see WARNINGS ).
🎯 Indications and Usage ▾
INDICATIONS AND USAGE Levorphanol Tartrate Tablets are indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Limitations of Use : Because of the risks of addiction, abuse, misuse, overdose, and death, which can occur at any dosage or duration and persist over the course of therapy ( see WARNINGS ), reserve opioid analgesics, including Levorphanol Tartrate Tablets for use in patients for whom alternative treatment options are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain.
⏱️ Dosage and Administration ▾
DOSAGE AND ADMINISTRATION Important Dosage and Administration Instructions Levorphanol Tartrate Tablets should be prescribed only by healthcare professionals who are knowledgeable about the use of opioids and how to mitigate the associated risks. Use the lowest effective dosage for the shortest duration of time consistent with individual patient treatment goals ( see WARNINGS ). Because the risk of overdose increases as opioid doses increase, reserve titration to higher doses of Levorphanol Tartrate Tablets for patients in whom lower doses are insufficiently effective and in whom the expected benefits of using a higher dose opioid clearly outweigh the substantial risks.
Many acute pain conditions (e.g., the pain that occurs with a number of surgical procedures or acute musculoskeletal injuries) require no more than a few days of an opioid analgesic. Clinical guidelines on opioid prescribing for some acute pain conditions are available. There is variability in the opioid analgesic dose and duration needed to adequately manage pain due both to the cause of pain and to individual patient factors.
Initiate the dosing regimen for each patient individually, taking into account the patient’s underlying cause and severity of pain, prior analgesic treatment and response, and risk factors for addiction, abuse, and misuse ( see WARNINGS ). Respiratory depression can occur at any time during opioid therapy, especially when initiating and following dosage increases with Levorphanol Tartrate Tablets. Consider this risk when selecting an initial dose and when making dose adjustments ( see WARNINGS ).
Patient Access to an Opioid Overdose Reversal Agent for the Emergency Treatment of Opioid Overdose Inform patients and caregivers about opioid overdose reversal agents (e.g., naloxone, nalmefene). Discuss the importance of having access to an opioid overdose reversal agent, especially if the patient has risk factors for overdose (e.g., concomitant use of CNS depressants, a history of opioid use disorder, or prior opioid overdose) or if there are household members (including children) or other close contacts at risk for accidental ingestion or opioid overdose.
The presence of risk factors for overdose should not prevent the management of pain in any patient ( see WARNINGS, Addiction, Abuse, and Misuse ; Life-Threatening Respiratory Depression ; Risks from Concomitant Use with Benzodiazepines or Other CNS Depressants ). Discuss the options for obtaining an opioid overdose reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program). There are important differences among the opioid overdose reversal agents, such as route of administration, product strength, approved patient age range, and pharmacokinetics.
Be familiar with these differences, as outlined in the approved labeling for those products, prior to recommending or prescribing such an agent. Initial Dosage Use of Levorphanol Tartrate Tablets as the First Opioid Analgesic Initiate treatment with Levorphanol Tartrate Tablets in a dosing range of 1 to 2 mg every 6 to 8 hours as needed for pain, at the lowest dose necessary to achieve adequate analgesia, provided the patient is assessed for signs of hypoventilation and excessive sedation. Titrate the dose based upon the individual patient’s response to their initial dose of Levorphanol Tartrate Tablets.
If necessary, the dose may be increased to up to 3 mg every 6 to 8 hours, after adequate evaluation of the patient’s response. Higher doses may be appropriate in opioid tolerant patients. Dosage should be adjusted according to the severity of the pain; age, weight and physical status of the patient; the patient’s underlying diseases; use of concomitant medications; and other factors ( see CLINICAL PHARMACOLOGY, Individualization of Dosage , WARNINGS , PRECAUTIONS ).
Conversion from Other Opioids to Levorphanol Tartrate Tablets There is inter-patient variability in the potency of opioid drugs and opioid formulatio… [Excerpted — this section continues on DailyMed.]
⛔ Contraindications ▾
CONTRAINDICATIONS Levorphanol Tartrate Tablets are contraindicated in patients with: Significant respiratory depression ( see WARNINGS ) Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment ( see WARNINGS ) Known or suspected gastrointestinal obstruction, including paralytic ileus ( see WARNINGS ) Hypersensitivity to levorphanol or any of the formulation excipients (e.g., anaphylaxis) ( see WARNINGS ).
⚠️ Warnings ▾
WARNINGS Addiction, Abuse, and Misuse Levorphanol Tartrate Tablets contain levorphanol, a Schedule II controlled substance. As an opioid, Levorphanol Tartrate Tablets expose users to the risks of addiction, abuse, and misuse ( see DRUG ABUSE AND DEPENDENCE ). Although the risk of addiction in any individual is unknown, it can occur in patients appropriately prescribed Levorphanol Tartrate Tablets.
Addiction can occur at recommended dosages and if the drug is misused or abused. The risk of opioid-related overdose or overdose-related death is increased with higher opioid doses, and this risk persists over the course of therapy. In postmarketing studies, addiction, abuse, misuse, and fatal and non-fatal opioid overdose were observed in patients with long-term opioid use ( see ADVERSE REACTIONS, Postmarketing Experience ).
Assess each patient’s risk for opioid addiction, abuse, or misuse prior to prescribing Levorphanol Tartrate Tablets, and reassess all patients receiving Levorphanol Tartrate Tablets for the development of these behaviors and conditions. Risks are increased in patients with a personal or family history of substance abuse (including drug or alcohol abuse or addiction) or mental illness (e.g., major depression). The potential for these risks should not, however, prevent the proper management of pain in any given patient.
Patients at increased risk may be prescribed opioids such as Levorphanol Tartrate Tablets, but use in such patients necessitates intensive counseling about the risks and proper use of Levorphanol Tartrate Tablets along with frequent reevaluation for signs of addiction, abuse and misuse. Consider recommending or prescribing an opioid overdose reversal agent ( see WARNINGS , DOSAGE AND ADMINISTRATION ). Opioids are sought for nonmedical use and are subject to diversion from legitimate prescribed use.
Consider these risks when prescribing or dispensing Levorphanol Tartrate Tablets. Strategies to reduce these risks include prescribing the drug in smallest appropriate quantity and advising the patient on careful storage of the drug during the course of treatment and proper disposal of unused drug. Contact local state professional licensing board or state-controlled substances authority for information on how to prevent and detect abuse or diversion of this product.
Life-Threatening Respiratory Depression Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids even when used as recommended. Respiratory depression, if not immediately recognized and treated, may lead to respiratory arrest and death. Management of respiratory depression may include close observation, supportive measures, and use of opioid overdose reversal agents, depending on the patient’s clinical status ( see OVERDOSAGE ).
Carbon dioxide (CO 2 ) retention from opioid-induced respiratory depression can exacerbate the sedating effects of opioids. While serious, life-threatening, or fatal respiratory depression can occur at any time during the use of Levorphanol Tartrate Tablets, the risk is greatest during the initiation of therapy or following a dosage increase. To reduce the risk of respiratory depression, proper dosing and titration of Levorphanol Tartrate Tablets are essential ( see DOSAGE AND ADMINISTRATION ).
Overestimating the Levorphanol Tartrate Tablets dosage when converting patients from another opioid product can result in a fatal overdose with the first dose. Accidental ingestion of even one dose of Levorphanol Tartrate Tablets, especially by children, can result in respiratory depression and death due to an overdose of Levorphanol Tartrate Tablets. Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose ( see PRECAUTIONS, Information for Patients ).
The initial dose of Levorphanol Tartrate Tablets should be reduced by 50% or more… [Excerpted — this section continues on DailyMed.]
🤒 Adverse Reactions ▾
ADVERSE REACTIONS In approximately 1400 patients treated with Levorphanol Tartrate Tablets in controlled clinical trials, the type and incidence of side effects were those expected of an opioid analgesic, and no unforeseen or unusual toxicity was reported. Drugs of this type are expected to produce a cluster of typical opioid effects in addition to analgesia, consisting of nausea, vomiting, altered mood and mentation, pruritus, flushing, difficulties in urination, constipation, and biliary spasm. The frequency and intensity of these effects appears to be dose related.
Although listed as adverse events these are expected pharmacologic actions of these drugs and should be interpreted as such by the clinician. The following adverse events have been reported with the use of Levorphanol Tartrate Tablets: Body as a Whole: abdominal pain, dry mouth, sweating Cardiovascular System: cardiac arrest, shock, hypotension, arrhythmias including bradycardia and tachycardia, palpitations, extra-systoles Digestive System: nausea, vomiting, dyspepsia, biliary tract spasm Nervous System: coma, suicide attempt, convulsions, depression, dizziness, confusion, lethargy, abnormal dreams, abnormal thinking, nervousness, drug withdrawal, hypokinesia, dyskinesia, hyperkinesia, CNS stimulation, personality disorder, amnesia, insomnia Respiratory System: apnea, cyanosis, hypoventilation Skin & Appendages: pruritus, urticaria, rash, injection site reaction Special Senses: abnormal vision, pupillary disorder, diplopia Urogenital System: kidney failure, urinary retention, difficulty urinating Postmarketing Experience The following adverse reactions have been identified during post-approval use of levorphanol.
Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Serotonin syndrome: Cases of serotonin syndrome, a potentially life-threatening condition, have been reported during concomitant use of opioids with serotonergic drugs. Adrenal insufficiency: Cases of adrenal insufficiency have been reported with opioid use, more often following greater than one month of use.
Anaphylaxis: Anaphylaxis has been reported with ingredients contained in Levorphanol Tartrate Tablets. Androgen deficiency: Cases of androgen deficiency have occurred with use of opioids for an extended period of time ( see CLINICAL PHARMACOLOGY ). Hyperalgesia and Allodynia: Cases of hyperalgesia and allodynia have been reported with opioid therapy of any duration ( see WARNINGS ).
Hypoglycemia: Cases of hypoglycemia have been reported in patients taking opioids. Most reports were in patients with at least one predisposing risk factor (e.g., diabetes). Opioid-induced esophageal dysfunction (OIED): Cases of OIED have been reported in patients taking opioids and may occur more frequently in patients taking higher doses of opioids, and/or in patients taking opioids longer term ( see WARNINGS ).
Adverse Reactions from Observational Studies A prospective, observational cohort study estimated the risks of addiction, abuse, and misuse in patients initiating long-term use of Schedule II opioid analgesics between 2017 and 2021. Study participants included in one or more analyses had been enrolled in selected insurance plans or health systems for at least one year, were free of at least one outcome at baseline, completed a minimum number of follow-up assessments, and either: 1) filled multiple extended-release/long-acting opioid analgesic prescriptions during a 90 day period (n=978); or 2) filled any Schedule II opioid analgesic prescriptions covering at least 70 of 90 days (n=1,244).
Those included also had no dispensing of the qualifying opioids in the previous 6 months. Over 12 months: approximately 1% to 6% of participants across the two cohorts newly met criteria for addiction, as assessed with two validated interview-based measures of moderate-to-severe… [Excerpted — this section continues on DailyMed.]
🔄 Drug Interactions ▾
Drug Interactions Benzodiazepines and Other Central Nervous System (CNS) Depressants Due to additive pharmacologic effect, the concomitant use of benzodiazepines or other CNS depressants, including alcohol, and other sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, gabapentinoids (gabapentin or pregabalin), and other opioids, can increase the risk of hypotension, respiratory depression, profound sedation, coma, and death. Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate.
Limit dosages and durations to the minimum required. Inform patients and caregivers of this potential interaction, educate them on the signs and symptoms of respiratory depression (including sedation). If concomitant use is warranted, consider recommending or prescribing an opioid overdose reversal agent ( see WARNINGS , DOSAGE AND ADMINISTRATION ).
Serotonergic Drugs The concomitant use of opioids with other drugs that affect the serotonergic neurotransmitter system, such as selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptans, 5-HT3 receptor antagonists, drugs that affect the serotonin neurotransmitter system (e.g., mirtazapine, trazodone, tramadol), certain muscle relaxants (i.e., cyclobenzaprine, metaxalone), and monoamine oxidase (MAO) inhibitors (those intended to treat psychiatric disorders and also others, such as linezolid and intravenous methylene blue), has resulted in serotonin syndrome ( see PRECAUTIONS, Information for Patients ).
If concomitant use is warranted, frequently evaluate the patient, particularly during treatment initiation and dose adjustment. Discontinue Levorphanol Tartrate Tablets if serotonin syndrome is suspected. Mixed Agonist/Antagonist and Partial Opioid Analgesics The concomitant use of opioid with other opioid analgesics, such as butorphanol, nalbuphine, pentazocine, may reduce the analgesic effect of Levorphanol Tartrate Tablets and precipitate withdrawal symptoms.
Advise patient to avoid concomitant use of these drugs. Muscle Relaxants Levorphanol may enhance the neuromuscular blocking action of skeletal muscle relaxants and produce an increased degree of respiratory depression. If concomitant use is warranted, because respiratory depression may be greater than otherwise expected, decrease the dosage of Levorphanol Tartrate Tablets and/or the muscle relaxant as necessary.
Due to the risk of respiratory depression with concomitant use of skeletal muscle relaxants and opioids, consider recommending or prescribing an opioid overdose reversal agent ( see WARNINGS , DOSAGE AND ADMINISTRATION ). Examples: Cyclobenzaprine, metaxalone. Diuretics Opioids can reduce the efficacy of diuretics by inducing the release of antidiuretic hormone.
If concomitant use is warranted, evaluate patients for signs of diminished diuresis and/or effects on blood pressure and increase the dosage of the diuretic as needed. Anticholinergic Drugs The concomitant use of anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus. If concomitant use is warranted, evaluate patients for signs of urinary retention or reduced gastric motility when Levorphanol Tartrate Tablets are used concomitantly with anticholinergic drugs.
🤰 Pregnancy ▾
Pregnancy Risk Summary Use of opioid analgesics for an extended period of time during pregnancy may cause neonatal opioid withdrawal syndrome ( see WARNINGS ). Available data with Levorphanol Tartrate Tablets in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage. In animal reproduction studies, oral levorphanol produced malformations and nearly 50% embryo lethality in mice at 10 and 12 times the human daily dose of 12 mg/day, respectively.
Paternal exposure to levorphanol prior to mating to an untreated female resulted in reduced litter birth weights, developmental delays, and aberrant behavior in a swim maze at 34 times the human daily dose of 12 mg/day. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.
Clinical Considerations Fetal/Neonatal Adverse Reactions Use of opioid analgesics for an extended period of time during pregnancy for medical or nonmedical purposes can result in physical dependence in the neonate and neonatal opioid withdrawal syndrome shortly after birth. Neonatal opioid withdrawal syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high pitched cry, tremor, vomiting, diarrhea, and failure to gain weight. The onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of the drug by the newborn.
Observe newborns for symptoms of neonatal opioid withdrawal syndrome and manage accordingly ( see WARNINGS ). Labor or Delivery Opioids cross the placenta and may produce respiratory depression and psycho-physiologic effects in neonates. An opioid overdose reversal agent, such as naloxone or nalmefene, must be available for reversal of opioid-induced respiratory depression in the neonate.
Levorphanol Tartrate Tablets are not recommended for use in pregnant women during or immediately prior to labor, when other analgesic techniques are more appropriate. Opioid analgesics, including Levorphanol Tartrate Tablets can prolong labor through actions which temporarily reduce the strength, duration, and frequency of uterine contractions. However, this effect is not consistent and may be offset by an increased rate of cervical dilation, which tends to shorten labor.
Monitor neonates exposed to opioid analgesics during labor for signs of excess sedation and respiratory depression. Animal Data In a published study, levorphanol has been shown to cause central nervous system malformations consistent with neural tube defects (kinking of the spinal cord, hydromyelia, dilation of the fourth ventricle, and brachyury) in pregnant mice when given a single subcutaneous dose of 25 mg/kg (10 times the human daily dose of 12 mg/day based on a body surface area comparison) on Gestation Day 9.
Subcutaneous administration of 30 mg/kg levorphanol to pregnant mice on Gestation Day 9 resulted in approximately 50% mortality of the mouse embryos (12 times the human daily dose of 12 mg/day). In another published study, male mice were injected subcutaneously twice daily with increasing daily doses of levorphanol up to 42 mg/kg/day (34 times the human daily dose of 12 mg based on body surface area) for 5.5 to 8.5 days prior to mating with an untreated female. Paternal exposure to levorphanol resulted in reduced birth weights of the litters, developmental delays in the offspring, and aberrant swim patterns in the progeny when measured at 6.5 to 8.5 weeks of age.
🧒 Pediatric Use ▾
Pediatric Use Levorphanol Tartrate Tablets are not recommended in children under the age of 18 years as the safety and efficacy of the drug in this population has not been established.
🧓 Geriatric Use ▾
Geriatric Use Elderly patients (aged 65 years or older) may have increased sensitivity to levorphanol. In general, use caution when selecting a dosage for an elderly patient, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy. The initial dose of Levorphanol Tartrate Tablets should be reduced by 50% or more in the infirm elderly patient.
Respiratory depression is the chief risk for elderly patients treated with opioids, and has occurred after large initial doses were administered to patients who were not opioid- tolerant or when opioids were co-administered with other agents that depress respiration. Titrate the dosage of Levorphanol Tartrate Tablets slowly in geriatric patients and frequently reevaluate the patient for signs of central nervous system and respiratory depression ( see WARNINGS ). This drug is known to be substantially excreted by the kidney, and the risk of adverse reactions to this drug may be greater in patients with impaired renal function.
Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to regularly evaluate renal function.
🆘 Overdosage ▾
OVERDOSAGE Clinical Presentation Acute overdose with Levorphanol Tartrate Tablets can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary edema, bradycardia, hypotension, hypoglycemia, partial or complete airway obstruction, atypical snoring, and death. Marked mydriasis rather than miosis may be seen with hypoxia in overdose situations ( see CLINICAL PHARMACOLOGY ). Toxic leukoencephalopathy has been reported after opioid overdose and can present hours, days, or weeks after apparent recovery from the initial intoxication.
Treatment of Overdose In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed. Employ other supportive measures (including oxygen and vasopressors) in the management of circulatory shock and pulmonary edema as indicated. Cardiac arrest or arrhythmias will require advanced life-support measures.
For clinically significant respiratory or circulatory depression secondary to opioid overdose, administer an opioid overdose reversal agent such as naloxone or nalmefene. Because the duration of opioid reversal is expected to be less than the duration of action of levorphanol in Levorphanol Tartrate Tablets, carefully monitor the patient until spontaneous respiration is reliably reestablished. If the response to an opioid overdose reversal agent is suboptimal or only brief in nature, administer additional reversal agent as directed by the product’s prescribing information.
In an individual physically dependent on opioids, administration of the recommended usual dosage of the opioid overdose reversal agent will precipitate an acute withdrawal syndrome. The severity of the withdrawal symptoms experienced will depend on the degree of physical dependence and the dose of the reversal agent administered. If a decision is made to treat serious respiratory depression in the physically dependent patient, administration of the reversal agent should be initiated with care and by titration with smaller than usual doses of the reversal agent.
🧬 Clinical Pharmacology ▾
CLINICAL PHARMACOLOGY Mechanism of Action Levorphanol is a full opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of levorphanol is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with levorphanol.
Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression. The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.
Pharmacodynamics Effects on the Central Nervous System The principal therapeutic action of levorphanol is analgesia. Levorphanol produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide retention and electrical stimulation.
Levorphanol causes miosis, even in total darkness. Pinpoint pupils are a sign of opioid overdose but are not pathognomonic (e.g., pontine lesions of hemorrhagic or ischemic origins may produce similar findings). Marked mydriasis rather than miosis may be seen due to hypoxia in overdose situations.
Effects on the Gastrointestinal Tract and Other Smooth Muscle Levorphanol causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone may be increased to the point of spasm, resulting in constipation.
Other opioid-induced effects may include a reduction in biliary and pancreatic secretions, spasm of sphincter of Oddi, transient elevations in serum amylase, and opioid-induced esophageal dysfunction (OIED). Effects on the Cardiovascular System Levorphanol produces peripheral vasodilation which may result in orthostatic hypotension or syncope. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension.
Effects on the Endocrine System Opioids inhibit the secretion of adrenocorticotropic hormone (ACTH), cortisol, and luteinizing hormone (LH) in humans ( see ADVERSE REACTIONS ). They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagon. Use of opioids for an extended period of time may influence the hypothalamic-pituitary-gonadal axis, leading to androgen deficiency that may manifest as low libido, impotence, erectile dysfunction, amenorrhea, or infertility.
The causal role of opioids in the clinical syndrome of hypogonadism is unknown because the various medical, physical, lifestyle, and psychological stressors that may influence gonadal hormone levels have not been adequately controlled for in studies conducted to date ( see ADVERSE REACTIONS ). Effects on the Immune System Opioids have been shown to have a variety of effects on components of the immune system. The clinical significance of these findings is unknown.
Overall, the effects of opioids appear to be modestly immunosuppressive. Concentration-Efficacy Relationships The minimum effective analgesic concentration will vary widely among patients, especially among patients who have been previously treated with opioid agonists. The minimum effective analgesic concentration of levorphanol for any individual patient may increase over time due to an increase in pain, the development of a new pain syndrome, and/or the development of analgesic tolerance ( see DOSAGE AND ADMINISTRATION ).
Concentration-Adverse Reaction Relationships There is a relationship between increasing levorpha… [Excerpted — this section continues on DailyMed.]
🧬 Mechanism of Action ▾
Mechanism of Action Levorphanol is a full opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of levorphanol is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with levorphanol.
Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression. The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.
📦 How Supplied / Storage and Handling ▾
HOW SUPPLIED Levorphanol Tartrate Tablets USP Dosage Strength Tablet Color Tablet Shape Tablet Debossing Tablet Scored NDC Number 2 mg White to off white round, flat faced debossed logo “M” inside square on one side and a score on the opposite side Yes 0406-2224-01 Bottles of 100 tablets. Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Store Levorphanol Tartrate Tablets securely and dispose of properly ( see PRECAUTIONS, Information for Patients ). Dispense in a tight, light-resistant container as defined in the USP.
Manufactured by: SpecGx LLC Webster Groves, MO 63119 USA © 2026 Par Health, Inc. or one of its affiliates. Rev 01/2026 Par Health™
📋 Description ▾
DESCRIPTION Levorphanol Tartrate Tablets contain levorphanol, an opioid agonist with a molecular formula of C 17 H 23 NO • C 4 H 6 O 6 • 2H 2 O and molecular weight 443.5. Each milligram of levorphanol tartrate is equivalent to 0.58 mg levorphanol base. Levorphanol's chemical name is levo-3-hydroxy-N-methylmorphinan.
The USP nomenclature is 17- methylmorphinan 3-ol tartrate (1:1)(Salt) dihydrate. The material has 3 asymmetric carbon atoms. The chemical structure is: Levorphanol tartrate is a white crystalline powder, soluble in water and ether, but insoluble in chloroform.
Levorphanol Tartrate Tablets, for oral administration, is available in one strength, distinguishable by the shape, size and debossing on the tablet surface: 2 mg tablet: white to off white, round, flat faced tablet, debossed logo “M” inside square on one side and a score on the opposite side of the tablet. In addition, each tablet contains lactose anhydrous, pregelatinized corn starch, and magnesium stearate. Chemical Structure
💬 Information for Patients ▾
Information for Patients Storage and Disposal Because of the risks associated with accidental ingestion, misuse, and abuse, advise patients to store Levorphanol Tartrate Tablets securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home. Inform patients that leaving Levorphanol Tartrate Tablets unsecured can pose a deadly risk to others in the home ( see WARNINGS , DRUG ABUSE AND DEPENDENCE ). Advise patients and caregivers that when medicines are no longer needed, they should be disposed of promptly.
Expired, unwanted, or unused Levorphanol Tartrate Tablets should be disposed of by flushing the unused medication down the toilet if a drug take-back option is not readily available. Inform patients that they can visit www.fda.gov/drugdisposal for a complete list of medicines recommended for disposal by flushing, as well as additional information on disposal of unused medicines. Advise the patient to read the FDA-approved patient labeling (Medication Guide).
Addiction, Abuse, and Misuse Inform patients that the use of Levorphanol Tartrate Tablets even when taken as recommended, can result in addiction, abuse, and misuse, which can lead to overdose and death ( see WARNINGS ). Instruct patients not to share Levorphanol Tartrate Tablets with others and to take steps to protect Levorphanol Tartrate Tablets from theft or misuse. Life-Threatening Respiratory Depression Inform patients of the risk of life-threatening respiratory depression, including information that the risk is greatest when starting Levorphanol Tartrate Tablets or when the dosage is increased, and that it can occur even at recommended dosages.
Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose ( see WARNINGS, Life-Threatening Respiratory Depression ). Accidental Ingestion Inform patients that accidental ingestion, especially by children, may result in respiratory depression or death ( see WARNINGS ). Interactions with Benzodiazepine and Other CNS Depressants Inform patients and caregivers that potentially fatal additive effects may occur if Levorphanol Tartrate Tablets are used with benzodiazepine or other CNS depressants, including alcohol [e.g., non-benzodiazepine sedative/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, gabapentinoids (gabapentin or pregabalin), and other opioids], and not to use these drugs concomitantly unless supervised by a healthcare provider ( see WARNINGS , PRECAUTIONS, Drug Interactions ).
Patient Access to an Opioid Overdose Reversal Agent for the Emergency Treatment of Opioid Overdose Inform patients and caregivers about opioid overdose reversal agents (e.g., naloxone, nalmefene). Discuss the importance of having access to an opioid overdose reversal agent, especially if the patient has risk factors for overdose (e.g., concomitant use of CNS depressants, a history of opioid use disorder, or prior opioid overdose) or if there are household members (including children) or other close contacts at risk for accidental ingestion or opioid overdose.
Discuss with the patient the options for obtaining an opioid overdose reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program) ( see WARNINGS , DOSAGE AND ADMINISTRATION ). Educate patients and caregivers on how to recognize the signs and symptoms of an overdose. Explain to patients and caregivers that effects of opioid overdose reversal agents like naloxone and nalmefene are temporary, and that they must call 911 or get emergency medical help right away in all cases of known or suspected opioid overdose, even if an opioid overdose reversal agent is administered ( see OVERDOSAGE ).
Advise patients and caregivers: how to treat with the overdose reversal agent in the event of an opioid overdose to tell f… [Excerpted — this section continues on DailyMed.]
💬 Medication Guide ▾
To obtain a printable copy of the Medication Guide, visit parhealth.com/products Medication Guide Levorphanol Tartrate (lee vor' fa nol tar' trate) Tablets, CII Levorphanol Tartrate Tablets are: A strong prescription pain medicine that contains an opioid (narcotic) that is used to manage pain, severe enough to require an opioid pain medicine when other pain treatments such as non-opioid pain medicines do not treat your pain well enough or you cannot tolerate them. An opioid pain medicine that can put you at risk for overdose and death.
Even if you take your dose correctly as prescribed you are at risk for opioid addiction, abuse, and misuse that can lead to death. Important information about Levorphanol Tartrate Tablets: Get emergency help or call 911 right away if you take too much Levorphanol Tartrate Tablets (overdose). When you first start taking Levorphanol Tartrate Tablets, when your dose is changed, or if you take too much (overdose), serious or life-threatening breathing problems that can lead to death may occur.
Ask your healthcare provider about medicines like naloxone or nalmefene that can be used in an emergency to reverse an opioid overdose. Taking Levorphanol Tartrate Tablets with other opioid medicines, benzodiazepines, gabapentinoids (gabapentin or pregabalin), alcohol, or other central nervous system depressants (including street drugs) can cause severe drowsiness, decreased awareness, breathing problems, coma and death. Never give anyone else your Levorphanol Tartrate Tablets.
They could die from taking it. Selling or giving away Levorphanol Tartrate Tablets is against the law. Store Levorphanol Tartrate Tablets securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home.
Do not take Levorphanol Tartrate Tablets if you have: severe asthma, trouble breathing, or other lung problems a bowel blockage or have narrowing of the stomach or intestines previously had an allergic reaction to levorphanol. Before taking Levorphanol Tartrate Tablets, tell your healthcare provider if you have a history of: head injury, seizures problems urinating abuse of street or prescription drugs, alcohol addiction, opioid overdose, or mental health problems. liver, kidney, thyroid problems pancreas or gallbladder problems Tell your healthcare provider if you are: noticing your pain getting worse.
If your pain gets worse after you take Levorphanol Tartrate Tablets, do not take more of Levorphanol Tartrate Tablets without first talking to your healthcare provider. Talk to your healthcare provider if the pain that you have increases, if you feel more sensitive to pain, or if you have new pain after taking of Levorphanol Tartrate Tablets. pregnant or planning to become pregnant. Use of Levorphanol Tartrate Tablets for an extended period of time during pregnancy can cause withdrawal symptoms in your newborn baby that could be life-threatening if not recognized and treated. breastfeeding.
Levorphanol passes into breast milk and may harm your baby. Carefully observe infants for increased sleepiness (more than usual), breathing difficulties, or limpness. Seek immediate medical care if you notice these signs. living in a household where there are small children or someone who has abused street or prescription drugs. taking prescription or over-the-counter medicines, vitamins, or herbal supplements.
Taking Levorphanol Tartrate Tablets with certain other medicines can cause serious side effects that could lead to death. When taking Levorphanol Tartrate Tablets: Do not change your dose. Take Levorphanol Tartrate Tablets exactly as prescribed by your healthcare provider.
Use the lowest dose possible for the shortest time needed. For acute (short-term) pain, you may only need to take Levorphanol Tartrate Tablets for a few days. You may have some Levorphanol Tartrate Tablets left over that you did not use.
See disposal information at the bottom of this section for directions on how to safe… [Excerpted — this section continues on DailyMed.]
⚠️ Precautions ▾
PRECAUTIONS Information for Patients Storage and Disposal Because of the risks associated with accidental ingestion, misuse, and abuse, advise patients to store Levorphanol Tartrate Tablets securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home. Inform patients that leaving Levorphanol Tartrate Tablets unsecured can pose a deadly risk to others in the home ( see WARNINGS , DRUG ABUSE AND DEPENDENCE ). Advise patients and caregivers that when medicines are no longer needed, they should be disposed of promptly.
Expired, unwanted, or unused Levorphanol Tartrate Tablets should be disposed of by flushing the unused medication down the toilet if a drug take-back option is not readily available. Inform patients that they can visit www.fda.gov/drugdisposal for a complete list of medicines recommended for disposal by flushing, as well as additional information on disposal of unused medicines. Advise the patient to read the FDA-approved patient labeling (Medication Guide).
Addiction, Abuse, and Misuse Inform patients that the use of Levorphanol Tartrate Tablets even when taken as recommended, can result in addiction, abuse, and misuse, which can lead to overdose and death ( see WARNINGS ). Instruct patients not to share Levorphanol Tartrate Tablets with others and to take steps to protect Levorphanol Tartrate Tablets from theft or misuse. Life-Threatening Respiratory Depression Inform patients of the risk of life-threatening respiratory depression, including information that the risk is greatest when starting Levorphanol Tartrate Tablets or when the dosage is increased, and that it can occur even at recommended dosages.
Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose ( see WARNINGS, Life-Threatening Respiratory Depression ). Accidental Ingestion Inform patients that accidental ingestion, especially by children, may result in respiratory depression or death ( see WARNINGS ). Interactions with Benzodiazepine and Other CNS Depressants Inform patients and caregivers that potentially fatal additive effects may occur if Levorphanol Tartrate Tablets are used with benzodiazepine or other CNS depressants, including alcohol [e.g., non-benzodiazepine sedative/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, gabapentinoids (gabapentin or pregabalin), and other opioids], and not to use these drugs concomitantly unless supervised by a healthcare provider ( see WARNINGS , PRECAUTIONS, Drug Interactions ).
Patient Access to an Opioid Overdose Reversal Agent for the Emergency Treatment of Opioid Overdose Inform patients and caregivers about opioid overdose reversal agents (e.g., naloxone, nalmefene). Discuss the importance of having access to an opioid overdose reversal agent, especially if the patient has risk factors for overdose (e.g., concomitant use of CNS depressants, a history of opioid use disorder, or prior opioid overdose) or if there are household members (including children) or other close contacts at risk for accidental ingestion or opioid overdose.
Discuss with the patient the options for obtaining an opioid overdose reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program) ( see WARNINGS , DOSAGE AND ADMINISTRATION ). Educate patients and caregivers on how to recognize the signs and symptoms of an overdose. Explain to patients and caregivers that effects of opioid overdose reversal agents like naloxone and nalmefene are temporary, and that they must call 911 or get emergency medical help right away in all cases of known or suspected opioid overdose, even if an opioid overdose reversal agent is administered ( see OVERDOSAGE ).
Advise patients and caregivers: how to treat with the overdose reversal agent in the event of an opioid overdo… [Excerpted — this section continues on DailyMed.]
🍼 Nursing Mothers ▾
Lactation Risk Summary The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Levorphanol Tartrate Tablets and any potential adverse effects on the breastfed infant from Levorphanol Tartrate Tablets or from the underlying maternal condition. Clinical Considerations Infants exposed to Levorphanol Tartrate Tablets through breast milk should be monitored for excess sedation and respiratory depression. Withdrawal symptoms can occur in breastfed infants when maternal administration of an opioid analgesic is stopped, or when breastfeeding is stopped.
Data Studies of levorphanol concentrations in breast milk have not been performed. However, morphine, which is structurally similar to levorphanol, is excreted in human milk. Because of the potential for serious adverse reactions from levorphanol in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
🧬 Pharmacokinetics ▾
Pharmacokinetics The pharmacokinetics of levorphanol have been studied in a limited number of cancer patients following intravenous (IV), intramuscular (IM) and oral (PO) administration. Following IV administration plasma concentrations of levorphanol decline in a triexponential manner with a terminal half-life of 11 to 16 hours and a clearance of 0.78 to
1.1L/kg/hr. Based on terminal half-life, steady-state plasma concentrations should be achieved by the third day of dosing. Levorphanol is rapidly distributed (<1 hr) and redistributed (1 to 2 hours) following IV administration and has a steady-state volume of distribution of 10 to 13 L/kg.
In vitro studies of protein binding indicate that levorphanol is only 40% bound to plasma proteins. No pharmacokinetic studies of the absorption of IM levorphanol are available, but clinical data suggests that absorption is rapid with onset of effects within 15 to 30 minutes of administration. Levorphanol is well absorbed after PO administration with peak plasma concentrations occurring approximately 1 hour after dosing.
The bioavailability of Levorphanol Tartrate Tablets compared to IM or IV administration is not known. Plasma concentrations of levorphanol following chronic administration in patients with cancer increased with the dose, but the analgesic effect was dependent on the degree of opioid tolerance of the patient. Expected steady-state plasma concentrations for a 6-hour dosing interval can reach 2 to 5 times those following a single dose, depending on the patient's individual clearance of the drug.
Very high plasma concentrations of levorphanol can be reached in patients on chronic therapy due to the long half-life of the drug. One study in 11 patients using the drug for control of cancer pain reported plasma concentrations from 5 to 10 ng/mL after a single 2 mg dose and up to 50 to 100 ng/mL after repeated oral doses of 20 to 50 mg/day. Animal studies suggest that levorphanol is extensively metabolized in the liver and is eliminated as the glucuronide metabolite.
This renally excreted inactive glucuronide metabolite accumulates with chronic dosing in plasma at concentrations that reach fivefold that of the parent compound. The effects of age, sex, hepatic and renal disease on the pharmacokinetics of levorphanol are not known. As with all drugs of this class, patients at the extremes of age are expected to be more susceptible to adverse effects because of a greater pharmacodynamic sensitivity and probable increased variability in pharmacokinetics due to age or disease.
Clinical Trials Clinical trials have been reported in the medical literature that investigated the use of Levorphanol Tartrate Tablets as a preoperative medication, as a postoperative analgesic, and in the management of chronic pain due primarily to malignancy. In each of these clinical settings Levorphanol Tartrate Tablets have been shown to be an effective analgesic of the mu-opioid type and similar to morphine, meperidine, or fentanyl. Levorphanol Tartrate Tablets have been studied in chronic cancer patients.
Dosages were individualized to each patient's level of opioid tolerance. In one study, starting doses of 2 mg twice a day often had to be advanced by 50% or more within a few weeks of starting therapy. A study of Levorphanol Tartrate Tablets indicates that the relative potency is approximately 4 to 8 times that of morphine, depending on the specific circumstances of use.
In postoperative patients, intramuscular levorphanol was determined to be about 8 times as potent as intramuscular morphine, whereas in cancer patients with chronic pain, it was found to be only about 4 times as potent. Individualization of Dosage Accepted medical practice dictates that the dose of any opioid analgesic be appropriate to the degree of pain to be relieved, the clinical setting, the physical condition of the patient, and the kind and dose of concurrent medication. Levorphanol has a long half-life similar to methadone or other… [Excerpted — this section continues on DailyMed.]
🧬 Pharmacodynamics ▾
Pharmacodynamics Effects on the Central Nervous System The principal therapeutic action of levorphanol is analgesia. Levorphanol produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide retention and electrical stimulation.
Levorphanol causes miosis, even in total darkness. Pinpoint pupils are a sign of opioid overdose but are not pathognomonic (e.g., pontine lesions of hemorrhagic or ischemic origins may produce similar findings). Marked mydriasis rather than miosis may be seen due to hypoxia in overdose situations.
Effects on the Gastrointestinal Tract and Other Smooth Muscle Levorphanol causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Propulsive peristaltic waves in the colon are decreased, while tone may be increased to the point of spasm, resulting in constipation.
Other opioid-induced effects may include a reduction in biliary and pancreatic secretions, spasm of sphincter of Oddi, transient elevations in serum amylase, and opioid-induced esophageal dysfunction (OIED). Effects on the Cardiovascular System Levorphanol produces peripheral vasodilation which may result in orthostatic hypotension or syncope. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension.
Effects on the Endocrine System Opioids inhibit the secretion of adrenocorticotropic hormone (ACTH), cortisol, and luteinizing hormone (LH) in humans ( see ADVERSE REACTIONS ). They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagon. Use of opioids for an extended period of time may influence the hypothalamic-pituitary-gonadal axis, leading to androgen deficiency that may manifest as low libido, impotence, erectile dysfunction, amenorrhea, or infertility.
The causal role of opioids in the clinical syndrome of hypogonadism is unknown because the various medical, physical, lifestyle, and psychological stressors that may influence gonadal hormone levels have not been adequately controlled for in studies conducted to date ( see ADVERSE REACTIONS ). Effects on the Immune System Opioids have been shown to have a variety of effects on components of the immune system. The clinical significance of these findings is unknown.
Overall, the effects of opioids appear to be modestly immunosuppressive. Concentration-Efficacy Relationships The minimum effective analgesic concentration will vary widely among patients, especially among patients who have been previously treated with opioid agonists. The minimum effective analgesic concentration of levorphanol for any individual patient may increase over time due to an increase in pain, the development of a new pain syndrome, and/or the development of analgesic tolerance ( see DOSAGE AND ADMINISTRATION ).
Concentration-Adverse Reaction Relationships There is a relationship between increasing levorphanol plasma concentration and increasing frequency of dose-related opioid adverse reactions such as nausea, vomiting, CNS effects, and respiratory depression. In opioid-tolerant patients, the situation may be altered by the development of tolerance to opioid-related adverse reactions ( see DOSAGE AND ADMINISTRATION ).
🔬 Clinical Studies ▾
Clinical Trials Clinical trials have been reported in the medical literature that investigated the use of Levorphanol Tartrate Tablets as a preoperative medication, as a postoperative analgesic, and in the management of chronic pain due primarily to malignancy. In each of these clinical settings Levorphanol Tartrate Tablets have been shown to be an effective analgesic of the mu-opioid type and similar to morphine, meperidine, or fentanyl. Levorphanol Tartrate Tablets have been studied in chronic cancer patients.
Dosages were individualized to each patient's level of opioid tolerance. In one study, starting doses of 2 mg twice a day often had to be advanced by 50% or more within a few weeks of starting therapy. A study of Levorphanol Tartrate Tablets indicates that the relative potency is approximately 4 to 8 times that of morphine, depending on the specific circumstances of use.
In postoperative patients, intramuscular levorphanol was determined to be about 8 times as potent as intramuscular morphine, whereas in cancer patients with chronic pain, it was found to be only about 4 times as potent.
🔒 Drug Abuse and Dependence ▾
DRUG ABUSE AND DEPENDENCE Controlled Substance Levorphanol Tartrate Tablets contain levorphanol, a Schedule II controlled substance. Abuse Levorphanol Tartrate Tablets contain levorphanol, a substance with high potential for misuse and abuse, which can lead to the development of substance use disorder, including addiction ( see WARNINGS ). Misuse is the intentional use, for therapeutic purposes, of a drug by an individual in a way other than prescribed by a healthcare provider or for whom it was not prescribed.
Abuse is the intentional, non-therapeutic use of a drug, even once, for its desirable psychological or physiological effects. Drug addiction is a cluster of behavioral, cognitive, and physiological phenomena that may include a strong desire to take the drug, difficulties in controlling drug use (e.g., continuing drug use despite harmful consequences, giving a higher priority to drug use than other activities and obligations), and possible tolerance or physical dependence. Misuse and abuse of Levorphanol Tartrate Tablets increases risk of overdose, which may lead to central nervous system and respiratory depression, hypotension, seizures, and death.
The risk is increased with concurrent abuse of Levorphanol Tartrate Tablets with alcohol and other CNS depressants. Abuse of and addiction to opioids in some individuals may not be accompanied by concurrent tolerance and symptoms of physical dependence. In addition, abuse of opioids can occur in the absence of addiction.
All patients treated with opioids require careful and frequent reevaluation for signs of misuse, abuse, and addiction, because use of opioid analgesic products carries the risk of addiction even under appropriate medical use. Patients at high risk of Levorphanol Tartrate Tablets abuse include those with a history of prolonged use of any opioid, including products containing levorphanol, those with a history of drug or alcohol abuse, or those who use Levorphanol Tartrate Tablets in combination with other abused drugs. “Drug-seeking” behavior is very common in persons with substance use disorders.
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 healthcare provider(s). “Doctor shopping” (visiting multiple prescribers to obtain additional prescriptions) is common among people who abuse drugs and people with substance use disorder. Preoccupation with achieving adequate pain relief can be appropriate behavior in a patient with inadequate pain control.
Levorphanol Tartrate Tablets, like other opioids, can be diverted for nonmedical use into illicit channels of distribution. Careful record-keeping of prescribing information, including quantity, frequency, and renewal requests, as required by state and federal law, is strongly advised. Proper assessment of the patient, proper prescribing practices, periodic reevaluation of therapy, and proper dispensing and storage are appropriate measures that help to limit abuse of opioid drugs.
Risks Specific to Abuse Levorphanol Tartrate Tablets Abuse of Levorphanol Tartrate Tablets poses a risk of overdose and death. The risk is increased with concurrent use of Levorphanol Tartrate Tablets with alcohol and/or other CNS depressants. Parenteral drug abuse is commonly associated with transmission of infectious diseases such as hepatitis and HIV.
Dependence Both tolerance and physical dependence can develop during use of opioid therapy. Tolerance is a physiological state characterized by a reduced response to a drug after repeated administration (i.e., a higher dose of a drug is required to produce the same effect that was once obtained at a lower dose). Physical dependence is a state that develops as a result of a physiological adaptation in response to repeated drug use, manifest… [Excerpted — this section continues on DailyMed.]
🔒 Controlled Substance ▾
Controlled Substance Levorphanol Tartrate Tablets contain levorphanol, a Schedule II controlled substance.
📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ▾
Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Long-term studies in animals to evaluate the carcinogenic potential of levorphanol have not been conducted. Mutagenesis Animal studies to evaluate the mutagenic potential of levorphanol have not been conducted. Impairment of Fertility Animal studies to determine the effect of levorphanol on fertility have not been conducted.
Infertility Use of opioids for an extended period of time may cause reduced fertility in females and males of reproductive potential. It is not known whether these effects on fertility are reversible ( see ADVERSE REACTIONS ).
📄 Package Label / Principal Display Panel ▾
Package Display Panel - 2 mg Label NDC 0406- 2224 -01 100 Tablets Levorphanol Tartrate Tablets USP CII 2 mg Rx only PHARMACIST: Dispense the Medication Guide provided separately to each patient. Par Health™ L00L09 Rev 01/2026 Package Display Panel - 2 mg Label