Tramadol

COMMON BRAND(S): Ultram
GENERIC NAME(S): Tramadol

Tramadol is an opiate pain medication used to treat moderate to moderately severe pain. When taken as an immediate-release oral formulation, the onset of pain relief usually occurs within about an hour. It has two different mechanisms. First, it binds to the μ-opioid receptor. Second, it inhibits the reuptake of serotonin and norepinephrine. Serious side effects may include seizures, increased risk of serotonin syndrome, decreased alertness, and drug addiction. Common side effects include: constipation, itchiness and nausea, among others. A change in dosage may be recommended in those with kidney or liver problems. Its use is not recommended in women who are breastfeeding or those who are at risk of suicide. Tramadol is marketed as a racemic mixture of both R- and S-stereoisomers. This is because the two isomers complement each other’s analgesic activity. It is often combined with paracetamol as this is known to improve the efficacy of tramadol in relieving pain. Tramadol is metabolised to O-desmethyltramadol, which is a more potent opioid. It is of the benzenoid class.
(Read here on Tramadol Withdrawal)

Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. Wikipedia
Formula: C16H25NO2
Onset of action: Less than 1 hour (by mouth)
Duration of action: 6 hours
Excretion: Urine (95%)
Melting point: 180 to 181 °C (356 to 358 °F)
Drug class: Opiate analgesic
Elimination half-life: 6.3 ± 1.4 h

Compound Summary

Tramadol hydrochloride – 2D Structure (source)

3D Conformer (source)

Synonyms

MeSH Entry Terms

  1. Adolonta
  2. Amadol
  3. Biodalgic
  4. Biokanol
  5. Contramal
  6. Jutadol
  7. K 315
  8. K-315
  9. K315
  10. MTW Tramadol
  11. MTW-Tramadol
  12. MTWTramadol
  13. Nobligan
  14. Prontofort
  15. Ranitidin 1A Pharma
  16. Takadol
  17. Theradol
  18. Tiral
  19. Topalgic
  20. Tradol
  21. Tradol Puren
  22. Tradol-Puren
  23. TradolPuren
  24. Tradonal
  25. Tralgiol
  26. Trama 1A Pharma
  27. Trama AbZ
  28. Trama Dorsch
  29. Trama KD
  30. Trama-Dorsch
  31. Tramabeta
  32. Tramadin
  33. Tramadoc
  34. Tramadol
  35. Tramadol 1A
  36. Tramadol acis
  37. Tramadol AL
  38. Tramadol Asta Medica
  39. Tramadol Basics
  40. Tramadol Bayvit
  41. Tramadol Bexal
  42. Tramadol Cinfa
  43. Tramadol Dolgit
  44. Tramadol Edigen
  45. Tramadol Hameln
  46. Tramadol Heumann
  47. Tramadol Hydrochloride
  48. Tramadol Kern
  49. Tramadol Lichtenstein
  50. Tramadol Lindo
  51. Tramadol Mabo
  52. Tramadol Normon
  53. Tramadol PB
  54. Tramadol Ratiopharm
  55. Tramadol Stada
  56. Tramadol-Dolgit
  57. Tramadol-Hameln
  58. Tramadol-ratiopharm
  59. TramadolDolgit
  60. TramadolHameln
  61. Tramadolor
  62. Tramadolratiopharm
  63. TramaDorsch
  64. Tramadura
  65. Tramagetic
  66. Tramagit
  67. Tramake
  68. Tramal
  69. Tramex
  70. Tramundin
  71. Trasedal
  72. Ultram
  73. Xymel 50
  74. Zamudol
  75. Zumalgic
  76. Zydol
  77. Zytram
(source)

Depositor-Supplied Synonyms

  1. tramadol hydrochloride
  2. 36282-47-0
  3. Bellatram
  4. Contramal
  5. Zumatran
  6. Omnidol
  7. Radol
  8. Tadol
  9. Melanate
  10. Tradonal
  11. Tramadex
  12. Tramagetic
  13. Tramazac
  14. Dolana
  15. Mabron
  16. Trabar
  17. Tramed
  18. Tramol
  19. Tridol
  20. Tradol-Puren
  21. cis-Tramadol hydrochloride
  22. Tramadol HCl
  23. 22204-88-2
  24. Tramal
  25. CG-315E
  26. (+)-Tramadol Hydrochloride
  27. Zydol hydrochloride
  28. CG 315
  29. Ryzolt
  30. EINECS 252-950-2
  31. 148229-78-1
  32. CHEBI:75733
  33. Tramadol hydrochloride [USAN:JAN]
  34. 53611-16-8
  35. HSDB 7047
  36. Poltram
  37. (+-)-cis-2-((Dimethylamino)methyl)-1-(m-methoxyphenyl)cyclohexanol hydrochloride
  38. (1R,2R)-2-[(Dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol Hydrochloride
  39. Cyclohexanol, 2-((dimethylamino)methyl)-1-(3-methoxyphenyl)-, hydrochloride, cis-
  40. Adolanta
  41. Cemadol
  42. Synapryn
  43. Tridural
  44. Rybix
  45. Viotra
  46. ConZip
  47. Tramal Retard
  48. Ira-Tramadol
  49. Ultram ER
  50. (+-)-cis-2-((Dimethylamino)methyl)-1-(3-methoxyphenyl)cyclohexanol hydrochloride
  51. Cyclohexanol, 2-((dimethylamino)methyl)-1-(3-methoxyphenyl)-, hydrochloride, (1R,2R)-rel-
  52. Rybix ODT
  53. SMR000449308
  54. Zydol XL 150
  55. (1R,2R)-2-((Dimethylamino)methyl)-1-(3-methoxyphenyl)cyclohexanol hydrochloride
  56. (1R,2R)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexan-1-ol;hydrochloride
  57. cis-(+-)-E 383 hydrochloride
  58. U-26225A
  59. EINECS 258-662-3
  60. NIH 10969
  61. Ultram (TN)
  62. tramadole hydrochloride
  63. TRAMADOL/HCL
  64. Tramadol hydrochloride [USAN:USP:JAN]
  65. U 26,225A
  66. (+)-Tramadol,hydrochloride
  67. C16H25NO2.HCl
  68. SCHEMBL41748
  69. tramadol hydrochloride tablets
  70. (R,R)-tramadol hydrochloride
  71. MLS000758218
  72. MLS001424208
  73. CHEMBL1200336
  74. DTXSID7023691
  75. CTK8G3518
  76. HY-B0582A
  77. DTXSID60933340
  78. Tramadol hydrochloride (JP17/USP)
  79. AC-796
  80. MFCD00798507
  81. (+)-(1R,2R)-Tramadol hydrochloride
  82. AKOS015907739
  83. API0000067
  84. API0004461
  85. CCG-101135
  86. CS-2770
  87. KS-1124
  88. MCULE-3504250719
  89. NC00385
  90. 194602-08-9
  91. LS-57120
  92. SC-77562
  93. AX8154449
  94. LS-174590
  95. LS-191406
  96. Tramadol hydrochloride, >=99.0% (HPLC)
  97. U-26,225A
  98. W0081
  99. D01355
  100. K-8120
  101. Tramadol hydrochloride, >=98% (HPLC), solid
  102. 204T882
  103. SR-01000759320
  104. Q-201847
  105. SR-01000759320-5
  106. Q27145507
  107. UNII-9N7R477WCK component PPKXEPBICJTCRU-XMZRARIVSA-N
  108. Tramadol Hydrochloride 1.0 mg/ml in Methanol (as free base)
  109. (+)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol hydrochloride
  110. Tramadol hydrochloride, British Pharmacopoeia (BP) Reference Standard
  111. Tramadol hydrochloride, European Pharmacopoeia (EP) Reference Standard
  112. Tramadol hydrochloride, United States Pharmacopeia (USP) Reference Standard
  113. (1R,2R)-2-(Dimethylaminomethyl)-1-(3-methoxyphenyl)-cyclohexanol hydrochloride
  114. [(1R,2R)-2-hydroxy-2-(3-methoxyphenyl)cyclohexyl]-N,N-dimethylmethanaminium chloride
  115. 2-[(Dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexan-1-ol–hydrogen chloride (1/1)
  116. cis-(+/-)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexan-1-ol hydrochloride
  117. cis-(1)-2-((Dimethylamino)methyl)-1-(3-methoxyphenyl)cyclohexan-1-ol hydrochloride
  118. Cyclohexanol, 2-((dimethylamino)methyl)-1-(3-methoxyphenyl)-, hydrochloride, cis-( -)-
  119. Cyclohexanol, 2-((dimethylamino)methyl)-1-(3-methoxyphenyl)-, hydrochloride, cis-(+-)-
  120. Cyclohexanol, 2-((dimethylamino)methyl)-1-(m-methoxyphenyl)-, hydrochloride, cis-(+-)-
  121. Cyclohexanol, 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-,hydrochloride, (1R,2R)-rel-
  122. cis-Tramadol hydrochloride solution, 1.0 mg/mL in methanol (as free base), ampule of 1 mL, certified reference material
(source)

Drug Label Information

BOXED WARNING SECTION

HEPATOTOXICITY

Tramadol hydrochloride and acetaminophen tablets contains acetaminophen and tramadol HCl. Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at doses that exceed 4,000 milligrams per day, and often involve more than one acetaminophen-containing product (see WARNINGS). (source)   

Warnings Section

Hepatotoxicity

Tramadol hydrochloride and acetaminophen tablets contains acetaminophen and tramadol HCl. Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at doses that exceed 4,000 milligrams per day, and often involve more than one acetaminophen-containing product. The excessive intake of acetaminophen may be intentional to cause self-harm or unintentional as patients attempt to obtain more pain relief or unknowingly take other acetaminophen-containing products (see Boxed Warning).

The risk of acute liver failure is higher in individuals with underlying liver disease and in individuals who ingest alcohol while taking acetaminophen.

Instruct patients to look for acetaminophen or APAP on package labels and not to use more than one product that contains acetaminophen. Instruct patients to seek medical attention immediately upon ingestion of more than 4,000 milligrams of acetaminophen per day, even if they feel well.

Serious Skin Reactions

Rarely, acetaminophen may cause serious skin reactions such as acute generalized exanthematous pustulosis (AGEP), Stevens-Johnson Syndrome (SJS), and toxic epidermal necrolysis (TEN), which can be fatal. Patients should be informed about the signs of serious skin reactions, and use of the drug should be discontinued at the first appearance of skin rash or any other sign of hypersensitivity.

Seizure Risk

Seizures have been reported in patients receiving tramadol within the recommended dosage range. Spontaneous postmarketing reports indicate that seizure risk is increased with doses of tramadol above the recommended range. Concomitant use of tramadol increases the seizure risk in patients taking:

Selective serotonin reuptake inhibitors (SSRI antidepressants or anorectics),

Tricyclic antidepressants (TCAs), and other tricyclic compounds (e.g., cyclobenzaprine, promethazine, etc.), or

Other opioids.

Administration of tramadol may enhance the seizure risk in patients taking:

MAO inhibitors (see also WARNINGS – Use with MAO Inhibitors and Serotonin Re-uptake Inhibitors),

Neuroleptics, or

Other drugs that reduce the seizure threshold.

Risk of convulsions may also increase in patients with epilepsy, those with a history of seizures, or in patients with a recognized risk for seizure (such as head trauma, metabolic disorders, alcohol and drug withdrawal, or CNS infections). In tramadol overdose, naloxone administration may increase the risk of seizure.

Suicide Risk:

Do not prescribe tramadol hydrochloride and acetaminophen tablets for patients who are suicidal or addiction-prone.

Prescribe tramadol hydrochloride and acetaminophen tablets with caution for patients taking tranquilizers or antidepressant drugs and patients who use alcohol in excess and who suffer from emotional disturbance or depression.

The judicious prescribing of tramadol is essential to the safe use of this drug. With patients who are depressed or suicidal, consideration should be given to the use of non-narcotic analgesics.

Tramadol-related deaths have occurred in patients with previous histories of emotional disturbances or suicidal ideation or attempts as well as histories of misuse of tranquilizers, alcohol, and other CNS-active drugs (see WARNINGS, Risk of Overdosage).

Serotonin Syndrome Risk

The development of a potentially life-threatening serotonin syndrome may occur with the use of tramadol products, including tramadol hydrochloride and acetaminophen tablets, particularly with concomitant use of serotonergic drugs such as SSRIs, SNRIs, TCAs, MAOIs, and triptans, with drugs which impair metabolism of serotonin (including MAOIs), and with drugs which impair metabolism of tramadol (CYP2D6 and CYP3A4 inhibitors). This may occur within the recommended dose (see CLINICAL PHARMACOLOGY, Pharmacokinetics).

Serotonin syndrome may include mental-status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination) and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea).

Hypersensitivity/Anaphylaxis

Serious and rarely fatal anaphylactic reactions have been reported in patients receiving therapy with tramadol. When these events do occur it is often following the first dose. Other reported allergic reactions include pruritus, hives, bronchospasm, angioedema, toxic epidermal necrolysis and Stevens-Johnson syndrome. Patients with a history of anaphylactoid reactions to codeine and other opioids may be at increased risk and therefore should not receive tramadol and acetaminophen (see CONTRAINDICATIONS).

There have been postmarketing reports of hypersensitivity and anaphylaxis associated with the use of acetaminophen. Clinical signs included swelling of the face, mouth, and throat, respiratory distress, urticaria, rash, pruritus, and vomiting. There were infrequent reports of life-threatening anaphylaxis requiring emergency medical attention. Instruct patients to discontinue tramadol hydrochloride and acetaminophen immediately and seek medical care if they experience these symptoms. Do not prescribe tramadol hydrochloride and acetaminophen for patients with acetaminophen allergy.

Respiratory Depression

Administer tramadol hydrochloride and acetaminophen tablets cautiously in patients at risk for respiratory depression. In these patients, alternative non-opioid analgesics should be considered. When large doses of tramadol are administered with anesthetic medications or alcohol, respiratory depression may result. Respiratory depression should be treated as an overdose. If naloxone is to be administered, use cautiously because it may precipitate seizures (see WARNINGS, Seizure Risk and OVERDOSAGE).

Interaction With Central Nervous System (CNS) Depressants

Tramadol hydrochloride and acetaminophen tablets should be used with caution and in reduced dosages when administered to patients receiving CNS depressants such as alcohol, opioids, anesthetic agents, narcotics, phenothiazines, tranquilizers or sedative hypnotics. Tramadol increases the risk of CNS and respiratory depression in these patients.

Interactions with Alcohol and Drugs of Abuse

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

Increased Intracranial Pressure or Head Trauma

Tramadol hydrochloride and acetaminophen tablets should be used with caution in patients with increased intracranial pressure or head injury. The respiratory depressant effects of opioids include carbon dioxide retention and secondary elevation of cerebrospinal fluid pressure and may be markedly exaggerated in these patients. Additionally, pupillary changes (miosis) from tramadol may obscure the existence, extent, or course of intracranial pathology. Clinicians should also maintain a high index of suspicion for adverse drug reactions when evaluating altered mental status in these patients if they are receiving tramadol hydrochloride and acetaminophen tablets (see WARNINGS, Respiratory Depression).

Use in Ambulatory Patients

Tramadol 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 using this drug should be cautioned accordingly.

Use With MAO Inhibitors and Serotonin Re-uptake Inhibitors

Use tramadol hydrochloride and acetaminophen tablets with great caution in patients taking monoamine oxidase inhibitors. Animal studies have shown increased deaths with combined administration of MAO inhibitors and tramadol. Concomitant use of tramadol with MAO inhibitors or SSRIs increases the risk of adverse events, including seizure and serotonin syndrome.

Use With Alcohol

Tramadol hydrochloride and acetaminophen tablets should not be used concomitantly with alcohol consumption. The use of tramadol hydrochloride and acetaminophen tablets in patients with liver disease is not recommended.

Use With Other Acetaminophen-containing Products

Due to the potential for acetaminophen hepatotoxicity at doses higher than the recommended dose, tramadol hydrochloride and acetaminophen tablets should not be used concomitantly with other acetaminophen-containing products.

Misuse, Abuse and Diversion

Tramadol has mu-opioid agonist activity. Tramadol hydrochloride and acetaminophen tablets, a tramadol-containing product, can be sought by drug abusers and people with addiction disorders and may be subject to criminal diversion. The possibility of illegal or illicit use should be considered when prescribing or dispensing tramadol hydrochloride and acetaminophen tablets in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion. Misuse or abuse poses a significant risk to the abuser that could result in overdose and death (see DRUG ABUSE AND DEPENDENCE and OVERDOSAGE).

Concerns about abuse, addiction, and diversion should not prevent the proper management of pain. The development of addiction to opioid analgesics in properly managed patients with pain has been reported to be rare. However, data are not available to establish the true incidence of addiction in chronic pain patients.

Risk of Overdosage

Patients taking tramadol should be warned not to exceed the dose recommended by their physician. Tramadol products in excessive doses, either alone or in combination with other CNS depressants, including alcohol, are a cause of drug-related deaths. Patients should be cautioned about the concomitant use of tramadol products and alcohol because of potentially serious CNS additive effects of these agents. Because of its added depressant effects, tramadol should be prescribed with caution for those patients whose medical condition requires the concomitant administration of sedatives, tranquilizers, muscle relaxants, tricyclic antidepressants, or other CNS depressant drugs. Patients should be advised of the additive depressant effects of these combinations.

Serious potential consequences of overdosage with tramadol are central nervous system depression, respiratory depression and death. Some deaths have occurred as a consequence of the accidental ingestion of excessive quantities of tramadol alone or in combination with other drugs. In treating an overdose, primary attention should be given to maintaining adequate ventilation along with general supportive treatment (see OVERDOSAGE).

A serious potential consequence of overdosage with acetaminophen is hepatic (centrilobular) necrosis, leading to hepatic failure and death. Emergency help should be sought immediately and treatment initiated immediately if overdose is suspected, even if symptoms are not apparent.

(source)

What side effects can this medication cause?

Tramadol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • sleepiness
  • difficulty falling asleep or staying asleep
  • headache
  • nervousness
  • uncontrollable shaking of a part of the body
  • muscle tightness
  • changes in mood
  • heartburn or indigestion
  • dry mouth

Some side effects can be serious. If you experience any of these symptoms or those mentioned in the IMPORTANT WARNING section, call your doctor immediately or get emergency medical treatment:

  • seizures
  • hives
  • rash
  • blisters
  • difficulty swallowing or breathing
  • swelling of the eyes, face, throat, tongue, lips, hands, feet, ankles, or lower legs
  • hoarseness

agitation, hallucinations (seeing things or hearing voices that do not exist), fever, sweating, confusion, fast heartbeat, shivering, severe muscle stiffness or twitching, loss of coordination, nausea, vomiting, or diarrhea

  • nausea, vomiting, loss of appetite, weakness, or dizziness
  • inability to get or keep an erection
  • irregular menstruation
  • decreased sexual desire
  • changes in heartbeat
  • loss of consciousness

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Tramadol may cause other side effects. Tell your doctor if you have any unusual problems while you are taking this medication.

(source

Drug Abuse and Dependence

Abuse:

Tramadol has mu-opioid agonist activity. Tramadol hydrochloride and acetaminophen tablets, a tramadol-containing product, can be abused and may be subject to criminal diversion.

Addiction is a primary, chronic, neurobiologic disease, with genetic, psychosocial, and environmental factors influencing its development and manifestations. Drug addiction is characterized by behaviors that include one or more of the following: impaired control over drug use, compulsive use, use for non-medical purposes, continued use despite harm or risk of harm, and craving. Drug addiction is a treatable disease, utilizing a multidisciplinary 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 tramadol hydrochloride and acetaminophen tablets can occur in the absence of true addiction and is characterized by misuse for non-medical purposes, often in combination with other psychoactive substances.

Concerns about abuse and addiction should not prevent the proper management of pain. However, all patients treated with opioids require careful monitoring for signs of abuse and addiction, because use of opioid analgesic products carries the risk of addiction even under appropriate medical use.

Proper assessment of the patient and periodic re-evaluation of therapy are appropriate measures that help to limit the potential abuse of this product.

Tramadol hydrochloride and acetaminophen tablets are intended for oral use only.

Dependence:

Tolerance is the need for increasing doses of drugs 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 (see also WARNINGS, Withdrawal).

The opioid abstinence or withdrawal syndrome is characterized by some or all of the following: restlessness, lacrimation, rhinorrhea, yawning, perspiration, chills, myalgia, and 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.

Generally, tolerance and/or withdrawal are more likely to occur the longer a patient is on continuous therapy with tramadol hydrochloride and acetaminophen tablets.

(source)

Over Dosage

Tramadol hydrochloride and acetaminophen tablets is a combination product. The clinical presentation of overdose may include the signs and symptoms of tramadol toxicity, acetaminophen toxicity or both. The initial symptoms of tramadol overdosage may include respiratory depression and/or seizures. The initial symptoms seen within the first 24 hours following an acetaminophen overdose are: anorexia, nausea, vomiting, malaise, pallor and diaphoresis. An overdosage of tramadol hydrochloride and acetaminophen tablets may be a potentially lethal polydrug overdose, and consultation with a regional poison control center is recommended.

Tramadol:

Acute overdosage with tramadol can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, seizures, bradycardia, hypotension, cardiac arrest, and death.

Deaths due to overdose have been reported with abuse and misuse of tramadol (see WARNINGS, Misuse, Abuse, and Diversion). Review of case reports has indicated that the risk of fatal overdose is further increased when tramadol is abused concurrently with alcohol or other CNS depressants, including other opioids.

In the treatment of tramadol overdosage, primary attention should be given to the re-establishment of a patent airway and institution of assisted or controlled ventilation. Supportive measures (including oxygen and vasopressors) should be employed in the management of circulatory shock and pulmonary edema accompanying overdose as indicated. Cardiac arrest or arrhythmias may require cardiac massage or defibrillation.

While naloxone will reverse some, but not all, symptoms caused by overdosage with tramadol, the risk of seizures is also increased with naloxone administration. In animals, convulsions following the administration of toxic doses of tramadol hydrochloride and acetaminophen tablets could be suppressed with barbiturates or benzodiazepines but were increased with naloxone. Naloxone administration did not change the lethality of an overdose in mice. Hemodialysis is not expected to be helpful in an overdose because it removes less than 7% of the administered dose in a 4 hour dialysis period.

Acetaminophen

In acetaminophen overdosage, dose-dependent, potentially fatal hepatic necrosis is the most serious adverse effect. Renal tubular necrosis, hypoglycemic coma, and coagulation defects also may occur. Early symptoms following a potentially hepatotoxic overdose may include: nausea, vomiting, diaphoresis, and general malaise. Clinical and laboratory evidence of hepatic toxicity may not be apparent until 48 to 72 hours post-ingestion.

In the treatment of acetaminophen overdosage, gastric decontamination with activated charcoal should be administered just prior to N-acetylcysteine (NAC) to decrease systemic absorption if acetaminophen ingestion is known or suspected to have occurred within a few hours of presentation. Serum acetaminophen levels should be obtained immediately if the patient presents 4 or more hours after ingestion to assess potential risk of hepatotoxicity; acetaminophen levels drawn less than 4 hours post-ingestion may be misleading. To obtain the best possible outcome, NAC should be administered as soon as possible where impending or evolving liver injury is suspected. Intravenous NAC may be administered when circumstances preclude oral administration.

Vigorous supportive therapy is required in severe intoxication. Procedures to limit the continuing absorption of the drug must be readily performed since the hepatic injury is dose-dependent and occurs early in the course of intoxication.
(source)

 

Recognised risk factors for tramadol overdose include depression, addiction, and seizures. Naloxone only partially reverses the toxic effects of tramadol overdose and may increase the risk of seizures.

 

Deaths with tramadol overdose have been reported and are increasing in frequency in Northern Ireland; the majority of these overdoses involves other drugs including alcohol. There were 254 tramadol-related deaths in England and Wales in 2013, and 379 in Florida in 2011. In 2011, 21,649 emergency room visits in the United States were related to tramadol.

(source)

In case of emergency/overdose

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

While taking tramadol, you may be told to always have a rescue medication called naloxone available (e.g., home, office). Naloxone is used to reverse the life-threatening effects of an overdose. It works by blocking the effects of opiates to relieve dangerous symptoms caused by high levels of opiates in the blood. You will probably be unable to treat yourself if you experience an opiate overdose. You should make sure that your family members, caregivers, or the people who spend time with you know how to tell if you are experiencing an overdose, how to use naloxone, and what to do until emergency medical help arrives. Your doctor or pharmacist will show you and your family members how to use the medication. Ask your pharmacist for the instructions or visit the manufacturer’s website to get the instructions. If someone sees that you are experiencing symptoms of an overdose, he or she should give you your first dose of naloxone, call 911 immediately, and stay with you and watch you closely until emergency medical help arrives. Your symptoms may return within a few minutes after you receive naloxone. If your symptoms return, the person should give you another dose of naloxone. Additional doses may be given every 2 to 3 minutes, if symptoms return before medical help arrives.

Symptoms of overdose may include the following:

 
  • decreased size of the pupil (the black circle in the center of the eye)
  • difficulty breathing
  • extreme drowsiness
  • unconsciousness
  • coma (loss of consciousness for a period of time)
  • slowed heartbeat
  • muscle weakness
  • cold, clammy skin 

Misuse

Illicit use of the drug is thought to be a major factor in the success of the Boko Haram terrorist organization. When used at higher doses, the drug “can produce similar effects to heroin.” Said one former member, “whenever we took tramadol, nothing mattered to us anymore except what we were sent to do because it made us very high and very bold, it was impossible to go on a mission without taking it.” Tramadol misuse is also found as a coping mechanism in the Gaza Strip.
(source

Tramadol FAQ

Is Tramadol stronger than codeine?
Tramadol and codeine are much less potent than other opiates like morphine, heroin, and its synthetic counterpart Fentanyl. Because of this, short-term use of tramadol and codeine for cough or moderate pain symptoms comes with a relatively low risk of addiction or withdrawal. 

What is tramadol used for? 
This medication is used to help relieve moderate to moderately severe pain. Tramadol is similar to opioid analgesics. It works in the brain to change how your body feels and responds to pain.

Does tramadol make you sleepy?
Tramadol oral tablet may cause drowsiness. You should not drive, use heavy machinery, or perform any dangerous activities until you know how this drug affects you. Tramadol may also cause other side effects.

Is tramadol a narcotic?
Tramadol is a specific type of narcotic medicine called an opioid that is approved to treat moderate to moderately severe pain in adults. It is available under the brand names Ultram, Ultram ER, Conzip, and also as generics.

How strong is 50 mg of Tramadol?
The recommended dose of tramadol is 50-100 mg (immediate release tablets) every 4-6 hours as needed for pain. The maximum dose is 400 mg/day. To improve tolerance patients should be started at 25 mg/day, and doses may be increased by 25-50 mg every 3 days to reach 50-100 mg/day every 4 to 6 hours.

Is tramadol a muscle relaxer?
Flexeril (cyclobenzaprine) and Ultram (tramadol) are used to treat back pain. Flexeril is indicated as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions. Ultram is used to treat moderate to moderately severe pain in adults.

Is one Tramadol a day addictive?
Tramadol is an opioid painkiller used to treat moderate pain. While it’s considered to be less habit forming than other prescription opioids, users can still develop an addiction to tramadol

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