• Users Online: 134
  • Print this page
  • Email this page

 Table of Contents  
Year : 2022  |  Volume : 8  |  Issue : 2  |  Page : 116-119

Repurposed oral tapentadol as an intravenous drug of abuse in opioid dependence

Department of Psychiatry, Deccan College of Medical Sciences, Hyderabad, Telangana, India

Date of Submission07-Nov-2022
Date of Decision08-Nov-2022
Date of Acceptance09-Nov-2022
Date of Web Publication16-Dec-2022

Correspondence Address:
Dr. Mazher Ali
Department of Psychiatry, Deccan College of Medical Sciences, DMRL X Road, Santosh Nagar Main Road, Kanchan Bagh, Hyderabad - 500 058, Telangana
Login to access the Email id

Source of Support: None, Conflict of Interest: None

DOI: 10.4103/tjp.tjp_48_22

Rights and Permissions

We present to you a case series of a group of individuals who presented to us with a history of intravenous drug abuse of repurposed oral tapentadol. Tapentadol is a synthetic benzenoid with a dual mode of action, as an agonist for the μ-opioid receptor and a norepinephrine reuptake inhibitor, with potential anti-nociceptive activity. The prevalence of current opioid use in India is reported to be 4% in males and 0.2% in females. Limited availability and difficulty in procuring the recommended drugs for detoxification and maintenance therapy in opioid dependence give reasons to consider treatment alternatives for the same. This case series aims to address the need and effectiveness of evidence-based treatment in opioid dependence.

Keywords: Addiction, opioid dependence, repurposed oral tapentadol

How to cite this article:
Fathima A, Nasirabadi MZ, Ahmed A, Ali M. Repurposed oral tapentadol as an intravenous drug of abuse in opioid dependence. Telangana J Psychiatry 2022;8:116-9

How to cite this URL:
Fathima A, Nasirabadi MZ, Ahmed A, Ali M. Repurposed oral tapentadol as an intravenous drug of abuse in opioid dependence. Telangana J Psychiatry [serial online] 2022 [cited 2023 Jun 5];8:116-9. Available from: https://tjpipstsb.org/text.asp?2022/8/2/116/363979

  Introduction Top

Tapentadol hydrochloride is the hydrochloride salt of tapentadol, a synthetic benzenoid with a dual mode of action, as an agonist for the μ-opioid receptor (MOR) and a norepinephrine reuptake inhibitor, with potential antinociceptive activity.[1],[2] It modulates pain signals in both ascending and descending neural pathways. It is used for the management of musculoskeletal pain and neuropathic pain associated with diabetic peripheral neuropathy.

The national survey in 2019 reported the prevalence of current opioid use to be 4% in males and 0.2% in females.[3] Worldwide, about 275 million people (or 5.5% of the global population aged 15–64 years) used drugs at least once in 2019. Among them, about 62 million people used opioids.[4]

Management of opioid dependence

Signs and symptoms can be monitored using Clinical Opiate Withdrawal Scale. Withdrawal starts at 6–8 h, peaks at 36–72 h, and lasts for 7–10 days. Withdrawal symptoms include rhinorrhea, fever, chills, severe body aches, muscle cramps, nausea, vomiting, diarrhea, dehydration, agitation, hypertension, severe anxiety, insomnia, severe weakness, piloerection, and yawning.

Treatment includes detoxification and maintenance therapy. Opioids like buprenorphine as well as methadone are recommended for detoxification. Buprenorphine can be initiated at 0.4 to 0.8 mg per day as per withdrawal symptoms, titrated up to 6–8 mg/day, and tapered down over 10–14 days. Methadone detox is initiated with 10 mg/day and can go up to 20–40 mg/day followed by slow tapering at 5 mg/day for a few weeks.

Treatment strategies

  1. Opioid substitution treatment (OST) is a strategy wherein opioid-injecting drug users are provided with long-acting opioid agonist medications aiming to replace illicit drug use with medically prescribed use[5]
  2. Oral substitution treatment includes the administration of slow-release oral Morphine/dihydrocodeine
  3. Methadone/buprenorphine maintenance treatment
  4. Medication-assisted treatment is the use of medications such as buprenorphine, methadone, and naltrexone in combination with counseling and behavioral therapies.[6]

Maintenance therapy aims to achieve abstinence from drug use, including cessation of substitution treatment and relapse prevention strategies.

  Case Series Top

We present to you a case series of individuals who presented to us with a history of repurposed oral tapentadol as an intravenous (IV) drug of abuse.

Case 1

A 24-year-old male, working as a delivery agent presented with complaints of decreased sleep, anxiety, headache, feeling fearful, and seeing cobwebs with a history of abuse of Tapentadol for 8 months which began with friends at the workplace. Tapentadol was self-administered intravenously after crushing the tablets and mixing them in water and injecting them through insulin syringes in both forearms. Needle sharing was present. He began with 10 tablets (of 50 mg each) in a day as a single dose and gradually increased to 25 tablets in three divided doses. The patient has a history of self-harm and a suicide attempt.

On examination, the patient had tremors, lacrimation, pupils dilated to 7 mm, multiple drug injection marks, indurated hyperpigmented superficial veins on both forearms, and multiple marks of hesitation cuts on the left forearm and neck [Figure 1].
Figure 1: Case 1

Click here to view

Case 2

A 27-year-old male, an auto driver by profession, came with 6 months' history of injecting 2–3 tablets of tapentadol (100 mg each) dissolved in water in 3–4 divided doses. His usage increased with stress. On cessation, he reported becoming weak, anxious, and unable to sleep along with complaints of generalized body pains. He developed recurrent abscesses on the injection sites, which had to be drained. The patient felt ashamed by the need to cover up his forearms all the time and hence turned up for de-addiction.

Examination revealed multiple abscesses and injection marks on both the arms. The patient had tremors, visible perspiration, and a resting pulse rate of 115 bpm [Figure 2].
Figure 2: Case 2

Click here to view

Case 3

A 20-year-old male college dropout, a painter by profession, was brought to the outpatient department by his cousin with a history of IV abuse of Tapentadol for over a period of 1 year wherein he dissolves 2 tablets (50 mg each) in a glass of water and injects it throughout the day in 5–6 divided doses. He has a history of working for a few days and using up all of the money he earns for substance abuse in the subsequent days and repeating the same. He was restricted at home for 3 days and had complaints of restlessness where he had frequent shifting of limbs, aching of joints, tearing of eyes, and a runny nose along with gross tremors.

The cousin reported a history of polysubstance abuse in the past with current abuse of IV Tapentadol and cigarette smoking.

The patient was observed to be restless throughout the examination and kept yawning. He also was found to have slight observable tremors.

Case 4

A 29-year-old male, who works at a Kirana store owned by his father, was brought by the father with complaints of irritability, anxiousness, multiple episodes of diarrhea, and running nose. He has a 1½-year history of IV Tapentadol abuse of 10–12 tablets (of 100 mg each) crushed and mixed with water and injected in the superficial veins of forearms and feet.

Examination revealed fine tremors with arms extended and pupils bilaterally dilated to 5 mm and a pulse rate of 114 bpm.

Case 5

A 23-year-old male, brother of the patient in case report 4 who also works at the Kirana store owned by their father was brought by the father after few months following the deaddiction of his elder son. The patient had a history of 6–7 months of IV tapentadol abuse (8–10 tablets of 50 mg each). The patient had complaints of anxiousness, irritability, and increased sweating for the past 2 days after restricting the drug abuse.

On examination, inflamed fingers were found with injection marks on both hands. Multiple hesitation cuts were also seen on both wrists. Pupils were bilaterally dilated, tremors were found along with anxiety and irritability.

Cases 1 and 3 were treated as in-patients, while the other cases were treated on an outpatient basis with a close follow-up of 2 days. The patients received gabapentin 300 mg/twice daily, clonidine 0.3 mg in divided doses, lorazepam 8 mg in divided doses, and tramadol (50 mg) half tablet/thrice daily, along with symptomatic treatment.

  Discussion Top

Treatment strategy for opioid dependence includes detoxification and maintenance therapy, for which buprenorphine and methadone are recommended.

Methadone is a schedule II narcotic drug. Buprenorphine is a schedule III narcotic analgesic. The treatment strategy followed is different from the recommendation due to restricted availability and hence the difficulty in procuring the drugs.[7] Although there is a combination of naltrexone and buprenorphine in the market today, it could not be used because of the limited availability, high pricing, and affordability of our patients.

Our treatment strategy was based on available evidence regarding the use of gabapentin, clonidine, lorazepam, and tramadol in the treatment of opioid withdrawal with the intention of overcoming these barriers.

Gabapentin reduces the severity of withdrawal symptoms experienced by patients with opioid dependence.[8] By blocking calcium influx, gabapentin reduces the release of glutamate and Substance P from primary nociceptive afferents, thereby modulating nociceptive transmission.[9] Clonidine is an important new treatment option for selected opiate addicts and may be the treatment of choice when detoxification using methadone is inappropriate, unsuccessful, or unavailable.[10],[11] It is a nonopioid anti-hypertensive drug that inhibits noradrenergic activity thereby counteracting the anxiogenic effects of opioid withdrawal.[12] Benzodiazepines enhance the effect of the neurotransmitter GABA at the GABA-A receptor, resulting in effects that can be very helpful in relieving opiate withdrawal symptoms.[13] Tramadol is an atypical analgesic with a dual mechanism of action as a serotonin and norepinephrine reuptake inhibitior and modest μ-opioid agonist.[14] It has a low abuse potential, hence was used as a substitution for the culprit opioid as an aid in reducing the symptoms of withdrawal.

Studies have proved the efficacy of drugs such as gabapentin, benzodiazepines, clonidine, and tramadol in reducing the severity of withdrawal symptoms caused by opioid drug abuse. With the increasing prevalence of opioid dependence and limited resources for adequate treatment, health-care providers need to evolve evidence-based strategies to overcome the barrier of availability. Centers with access to a large pool of such patients could conduct robust and well-designed randomized clinical trials to gather data to ascertain the possibility of using this nonstandard treatment scheme.

Declaration of patient consent

The authors certify that they have obtained all appropriate patient consent forms. In the form the patient (s) has/have given his/her/their consent for his/her/their images and other clinical information to be reported in the journal. The patients understand that their names and initials will not be published and due efforts will be made to conceal their identity, but anonymity cannot be guaranteed.


We would like to thank Dr. Khan Mohammed Zeeshan Ali.

Financial support and sponsorship


Conflicts of interest

There are no conflicts of interest.

  References Top

Chang EJ, Choi EJ, Kim KH. Tapentadol: Can it kill two birds with one stone without breaking windows? Korean J Pain 2016;29:153-7.  Back to cited text no. 1
Singh DR, Nag K, Shetti AN, Krishnaveni N. Tapentadol hydrochloride: A novel analgesic. Saudi J Anaesth 2013;7:322-6.  Back to cited text no. 2
Singh B, Rao R. Perspectivesis there an opioid epidemic in India? J Public Health (Oxf) 2021;43:i43-50.  Back to cited text no. 3
Available from: https://www.who.int/news-room/fact-sheets/detail/opioid-overdose. [Last accessed on 2022 Nov 03].  Back to cited text no. 4
Mohapatra S, Nayak MR, Dash M. A clinical study of opioid substitution therapy in a tertiary care Center of Eastern India. Indian J Psychol Med 2017;39:756-9.  Back to cited text no. 5
[PUBMED]  [Full text]  
National Academies of Sciences, Engineering, and Medicine; Health and Medicine Division; Board on Health Sciences Policy; Committee on Medication-Assisted Treatment for Opioid Use Disorder. 2, The Effectiveness of Medication-Based Treatment for Opioid Use Disorder. In: Mancher M, Leshner AI, editors. Medications for Opioid Use Disorder Save Lives. Washington (DC): National Academies Press (US); 2019. Available from: https://www.ncbi.nlm.nih.gov/books/NBK541393. [Last accessed on 2022 Sep 21].  Back to cited text no. 6
Preuss CV, Kalava A, King KC. Prescription of Controlled Substances: Benefits and Risks. In: StatPearls. Treasure Island (FL): StatPearls Publishing; 2022. Available from: https://www.ncbi.nlm.nih.gov/books/NBK537318. [Last updated on 2022 Sep 21].  Back to cited text no. 7
Behnam B, Semnani V, Saghafi N, Ghorbani R, Dianak Shori M, Ghooshchian Choobmasjedi S. Gabapentin effect on pain associated with heroin withdrawal in Iranian crack: A randomized double-blind clinical trial. Iran J Pharm Res 2012;11:979-83.  Back to cited text no. 8
Available from: https://www.sciencedirect.com/topics/neuroscience/gabapentin. [Last accessed on 2022 Nov 03].  Back to cited text no. 9
Washton AM, Resnick RB. Clonidine in opiate withdrawal: Review and appraisal of clinical findings. Pharmacotherapy 1981;1:140-6.  Back to cited text no. 10
Kleber HD. Pharmacologic treatments for opioid dependence: Detoxification and maintenance options. Dialogues Clin Neurosci 2007;9:455-70.  Back to cited text no. 11
Adetunji B, Mathews M, Williams A, Rufai O. Evidence-based addiction medicine: The use of lofexidine for opioid detoxification. Psychiatry (Edgmont) 2004;1:32-5.  Back to cited text no. 12
Diaper AM, Law FD, Melichar JK. Pharmacological strategies for detoxification. Br J Clin Pharmacol 2014;77:302-14.  Back to cited text no. 13
Ziaaddini H, Ziaaddini A, Asghari N, Nakhaee N, Eslami M. Trial of tramadol plus gabapentin for opioid detoxification. Iran Red Crescent Med J 2015;17:e18202.  Back to cited text no. 14


  [Figure 1], [Figure 2]


Similar in PUBMED
   Search Pubmed for
   Search in Google Scholar for
 Related articles
Access Statistics
Email Alert *
Add to My List *
* Registration required (free)

  In this article
Case Series
Article Figures

 Article Access Statistics
    PDF Downloaded44    
    Comments [Add]    

Recommend this journal