Tramadol

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Tramal
Tramal

Tramadol is a opioid that also acts as a SNRI. It is used as a prescription drug in many countries to treat moderate pain (often combined with paracetamol), and also sees recreational use for its euphoric effects. Due to its complex and atypical nature, it has also been investigated for use in the treatment of many conditions, including PTSD, opioid withdrawal, OCD and the management of diabetic side-effects.

History

Tramadol was first discovered in 1962 in Germany, and was later released under the brand name Tramal in 1977 - lauded due to its additional SNRI action. It later became a popular choice as a prescription drug for pain treatment around the world. Despite its branding and institutional view as a drug with little potential for abuse, it has increasing amounts of recreational use since release.

In 2013, it was discovered that tramadol is produced naturally in high concentrations in the root of the African pin cushion tree.

Dosage

Doses are given on a tolerance scale, since it accrues quickly; users should note that the lowering of the seizure threshold occurs regardless of tolerance.

Oral (No Tolerance)
Light 50-100mg
Common 75-200mg
Strong 250mg+
Oral (Tolerance)
Medium-High Tolerance 200-250mg
Very High Tolerance 300-400mg (seizure threshold is dangerously lowered)
Extremely High Tolerance 400mg+ (potentially fatal for new users)

Duration

Long onset, slowly building to a peak by hour 4 with maximum blood concentration achieved near hour 4.5.

Oral
Onset 1-2 hours
Peak 3-4 hours
Total 5-7 hours

Effects

Positive

  • Euphoria
  • Pain relief
  • Elevated mood
  • Overall feeling of contentedness

Neutral

  • Itching

Negative

Some users may experience

  • Nausea
  • Constipation
  • CNS depression
  • Drowsiness
  • Hot/cold flashes
  • Dizziness
  • Vomiting
  • Urinary retention (difficulty urinating)

In high doses, overdoses, or in patients not tolerant to opiates, tramadol can cause shallow breathing, bradycardia, cold-clammy skin, apnea, hypotension, miosis, circulatory collapse, respiratory arrest, and death.

Chemistry and Pharmacology

Tramadol acts as a μ-opioid receptor agonist, serotonin releasing agent (SRA), serotonin and norepinephrine reuptake inhibitor (SNRI), NMDA receptor antagonist, 5-HT2C receptor antagonist, 5 nicotinic acetylcholine receptor antagonist,TRPV1 receptor agonist, and M1 and M3 muscarinic acetylcholine receptorantagonist. and can cause seizures, serotonin syndrome and even death when combined with certain stimulants and other reuptake inhibitors.

Harm Reduction

  • Do not drive or operate machinery while under the influence of tramadol.
  • Alcohol and many other drugs are extremely dangerous to combine with tramadol, for a list of interactions refer to Drug combinations.
  • Mainly, do not combine with benzos, other opiates, or other serotogenic drugs
  • Tramadol effects serotonin levels in the brain. For this reason it is recommended to taper on and taper off use over an extended time period.

Seizure Risk

We cannot stress this enough; if you have a history of seizures, we strongly urge you to stay away from tramadol as a recreational substance. By itself, it can decrease the seizure threshold. When combined with SSRIs, tricyclic antidepressants, or in patients with epilepsy, the seizure threshold is further decreased. Seizures have been reported in humans receiving excessive single oral doses (700 mg) or large intravenous doses (300 mg). However, there have been several rare cases of people having grand-mal seizures at doses as low as 100-400 mg orally.

Legal Status

Tramadol (Ultram) was unscheduled in the United States and available by prescription only. But it was recently classified Schedule IV. This means that sales and distribution are allowed only by those with a license and only to those with a prescription (according to FDA regulations). Possession is illegal without a prescription.

  • Australia: Schedule IV
  • Canada: Tramadol is unscheduled, but most pharmacies will not sell to those without a prescription
  • UK: Class C drug
  • Most of EU: Available by prescription only

Links

Wikipedia

Erowid's Tramadol Vault