Tramadol


Description

Tramadol, with the chemical formula cis-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol hydrochloride, is a 4-phenylpiperidine analog of codeine.[

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Pharmacology

Indication

Tramadol is approved for the management of moderate to severe pain in adults.[FDA label]

As an of...
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Pharmacodynamic

Tramadol inhibits the descending pain pathways at the spinal level.[ Read more

Mechanismofaction

Tramadol has a dual action of pain relief by acting as both a central opiate agonist and a central n... Read more

Absorption

Oral administration of a dose of 100 mg of racemic tramadol has been shown to present a very rapid a... Read more

Proteinbinding

About 20% of the administer tramadol is found bound to plasma proteins.[ Read more

Volumeofdistribution

The volume of distribution of tramadol is reported to be in the range of 2.6-2.9 L/kg.[ Read more

Clearance

In clinical trials, the clearance rate of tramadol ranged from 3.73 ml/min/kg in renal impairment pa... Read more

Halflife

Tramadol reported a half-life of 5-6 hours while the M1 metabolite presents a half-life of 8 hours.[... Read more

Routeofelimination

Tramadol is eliminated primarily through metabolism by the liver and the metabolites are excreted pr... Read more

Toxicity

The reported LD50 for tramadol, when administered orally in mice, is 350 mg/kg.[ Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Constipation US
  • Kind: experimental
    • Percent: 24-46%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 24-40%
  • Clinical Trial
    Dizziness/vertigo US
  • Kind: experimental
    • Percent: 26-33%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 18-32%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 16-25%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 9-17%
  • Clinical Trial
    Hallucinations US
  • Kind: experimental
    • Percent: 7-14%
  • Clinical Trial
    Emotional Lability US
  • Kind: experimental
    • Percent: 7-14%
  • Clinical Trial
    Euphoria US
  • Kind: experimental
    • Percent: 7-14%
  • Clinical Trial
    Spasticity US
  • Kind: experimental
    • Percent: 7-14%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 7-14%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 7-14%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 7-14%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 5-13%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 6-12%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 8-11%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 5-10%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 5-10%
  • Clinical Trial
    Sweating US
  • Kind: experimental
    • Percent: 6-9%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Visual Disturbance US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Menopausal Symptoms US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Urinary Frequency US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Urinary Retention US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Vasodilation US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Coordination disturbance US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Miosis US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Euphoria US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Sleep Disorder US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Hypertonia US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 1-<5%
  • Clinical Trial
    Accidental injury US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Allergic Reaction US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Anaphylaxis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Death US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Suicidal tendency US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Weight Loss US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Serotonin Syndrome US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Orthostatic Hypotension US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Syncope US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Tachycardia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Abnormal Gait US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Difficulty in concentration US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Dose Form:
      • Tablet
    • Regions: US
    • Patient Conditions:
        • Name: Opioid contraindication situation caused by Alcohol Intoxication, intoxication with hypnotic agents, intoxication with analgesics, Opioid Intoxication, intoxication with psychotropic drugs
        • Drugbank Id: DBCOND0116936
        • Combination Of:
          • Caused By:
              • Name: Intoxication with psychotropic drugs
              • Drugbank Id: DBCOND0116937
              • Name: Intoxication with analgesics
              • Drugbank Id: DBCOND0116938
              • Name: Opioid Intoxication
              • Drugbank Id: DBCOND0103636
              • Name: Intoxication with hypnotic agents
              • Drugbank Id: DBCOND0116939
              • Name: Alcohol Intoxication
              • Drugbank Id: DBCOND0037955
          • Included Conditions:
              • Name: Opioid contraindication situation
              • Drugbank Id: DBCOND0116940
    • Hypersensitivity:
      • true
    • Regions: US

    Food Interactions

    • Oral administration of tramadol hydrochloride with food does not significantly affect its rate or extent of absorption, therefore, tramadol hydrochloride can be administered without regard to food.

    Interactions

    Type in a drug name to check for interaction with Tramadol

    The risk or severity of adverse effects can be increased when Tramadol is combined with (R)-warfarin.
    The risk or severity of adverse effects can be increased when Tramadol is combined with (S)-Warfarin.
    The therapeutic efficacy of Tramadol can be decreased when used in combination with 1,10-Phenanthroline.
    2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Tramadol.
    2,5-Dimethoxy-4-ethylthioamphetamine may increase the analgesic activities of Tramadol.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Tramadol.
    4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Tramadol.
    4-Bromo-2,5-dimethoxyphenethylamine may increase the central nervous system depressant (CNS depressant) activities of Tramadol.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Tramadol.
    4-Methoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Tramadol.
    The metabolism of 5-androstenedione can be decreased when combined with Tramadol.
    The risk or severity of adverse effects can be increased when Tramadol is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Tramadol can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Tramadol.
    The metabolism of Tramadol can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    7-Nitroindazole may increase the central nervous system depressant (CNS depressant) activities of Tramadol.
    The risk or severity of serotonin syndrome and seizure can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Tramadol.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Tramadol.
    Tramadol may decrease the excretion rate of Abacavir which could result in a higher serum level.
    The metabolism of Tramadol can be increased when combined with Abatacept.

    References

    • 1 . Dayer P, Desmeules J, Collart L: [Pharmacology of tramadol]. Drugs. 1997;53 Suppl 2:18-24. [PubMed: 9190321]
    • 2 . Harati Y, Gooch C, Swenson M, Edelman S, Greene D, Raskin P, Donofrio P, Cornblath D, Sachdeo R, Siu CO, Kamin M: Double-blind randomized trial of tramadol for the treatment of the pain of diabetic neuropathy. Neurology. 1998 Jun;50(6):1842-6. [PubMed: 9633738]
    • 3 . Harati Y, Gooch C, Swenson M, Edelman SV, Greene D, Raskin P, Donofrio P, Cornblath D, Olson WH, Kamin M: Maintenance of the long-term effectiveness of tramadol in treatment of the pain of diabetic neuropathy. J Diabetes Complications. 2000 Mar-Apr;14(2):65-70. [PubMed: 10959067]
    • 4 . Gobel H, Stadler T: [Treatment of post-herpes zoster pain with tramadol. Results of an open pilot study versus clomipramine with or without levomepromazine]. Drugs. 1997;53 Suppl 2:34-9. [PubMed: 9190323]
    • 5 . Boureau F, Legallicier P, Kabir-Ahmadi M: Tramadol in post-herpetic neuralgia: a randomized, double-blind, placebo-controlled trial. Pain. 2003 Jul;104(1-2):323-31. [PubMed: 12855342]
    • 6 . Beakley BD, Kaye AM, Kaye AD: Tramadol, Pharmacology, Side Effects, and Serotonin Syndrome: A Review. Pain Physician. 2015 Jul-Aug;18(4):395-400. [PubMed: 26218943]
    • 7 . Shin HW, Ju BJ, Jang YK, You HS, Kang H, Park JY: Effect of tramadol as an adjuvant to local anesthetics for brachial plexus block: A systematic review and meta-analysis. PLoS One. 2017 Sep 27;12(9):e0184649. doi: 10.1371/journal.pone.0184649. eCollection 2017. [PubMed: 28953949]
    • 8 . Martyn-St James M, Cooper K, Kaltenthaler E, Dickinson K, Cantrell A, Wylie K, Frodsham L, Hood C: Tramadol for premature ejaculation: a systematic review and meta-analysis. BMC Urol. 2015 Jan 30;15:6. doi: 10.1186/1471-2490-15-6. [PubMed: 25636495]
    • 9 . Monteiro BP, Klinck MP, Moreau M, Guillot M, Steagall PV, Pelletier JP, Martel-Pelletier J, Gauvin D, Del Castillo JR, Troncy E: Analgesic efficacy of tramadol in cats with naturally occurring osteoarthritis. PLoS One. 2017 Apr 12;12(4):e0175565. doi: 10.1371/journal.pone.0175565. eCollection 2017. [PubMed: 28403198]
    • 10 . Stoops WW, Lofwall MR, Nuzzo PA, Craig LB, Siegel AJ, Walsh SL: Pharmacodynamic profile of tramadol in humans: influence of naltrexone pretreatment. Psychopharmacology (Berl). 2012 Oct;223(4):427-38. doi: 10.1007/s00213-012-2739-4. Epub 2012 May 24. [PubMed: 22623016]
    • 11 . Vazzana M, Andreani T, Fangueiro J, Faggio C, Silva C, Santini A, Garcia ML, Silva AM, Souto EB: Tramadol hydrochloride: pharmacokinetics, pharmacodynamics, adverse side effects, co-administration of drugs and new drug delivery systems. Biomed Pharmacother. 2015 Mar;70:234-8. doi: 10.1016/j.biopha.2015.01.022. Epub 2015 Feb 7. [PubMed: 25776506]
    • 12 . FDA approvals [Link]
    • 13 . WHO reports [Link]

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