Active Ingredient History

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Tramadol (sold under the brand name Ultram) is a narcotic analgesic proposed for moderate to severe pain. Tramadol and its O-desmethyl metabolite (M1) are selective, weak OP3-receptor agonists. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. The analgesic properties of Tramadol can be attributed to norepinephrine and serotonin reuptake blockade in the CNS, which inhibits pain transmission in the spinal cord. The (+) enantiomer has the higher affinity for the OP3 receptor and preferentially inhibits serotonin uptake and enhances serotonin release. The (-) enantiomer preferentially inhibits norepinephrine reuptake by stimulating alpha(2)-adrenergic receptors. Tramadol is used primarily to treat mild-severe pain, both acute and chronic. Its analgesic effects take about one hour to come into effect and 2 h to 4 h to peak after oral administration with an immediate-release formulation. On a dose-by-dose basis, tramadol has about one-tenth the potency of morphine and is approximately equally potent when compared to pethidine and codeine. The most common adverse effects of tramadol include nausea, dizziness, dry mouth, indigestion, abdominal pain, vertigo, vomiting, constipation, drowsiness, and headache. Compared to other opioids, respiratory depression and constipation are considered less of a problem with tramadol.   NCATS

  • SMILES: COc1cccc(c1)C2(O)CCCCC2CN(C)C
  • InChIKey: TVYLLZQTGLZFBW-UHFFFAOYSA-N
  • Mol. Mass: 263.38
  • ALogP: 2.63
  • ChEMBL Molecules:
More Chemistry
  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$0.0135 - $12.8143

Australia

$0.0880 - $4.9154
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Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Combination drugs

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cg-315e | conzip | dromadol sr | dromadol xl | invodol sr | larapam sr | mabron | maneo | marol | maxitram sr | nobligan ret | oldaram | racemic tramadol | rybix odt | ryzolt | tilodol sr | tradolan | tradorec xl | tramacet | tramadol | (+/-)-tramadol | (+)-tramadol | tramadol hcl | tramadol hydrochloride | tramadol hydrochloride and acetaminophen | tramadon | tramake | tramake insts | tramquel sr | tramulief sr | (+)-trans-2-(dimethylaminomethyl)-1-(m-methoxyphenyl)cyclohexanol | u-26225a | ultracet | ultram | ultram er | zamadol | zamadol 24hr | zamadol melt | zamadol sr | zeridame sr | zydol | zydol sr | zydol xl

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