Tramadol

Identification

Name
Tramadol
Accession Number
DB00193 / 0NG5TTM63P
Groups
Act Tramadol/acet
Description

Tramadol, with the chemical formulation cis-2-[(dimethylamino)methyl]-1-(three-methoxyphenyl)-cyclohexanol hydrochloride, is a 4-phenylpiperidine analog of codeine.[A173983] it's miles a normal cross-to remedy as it has less potential for abuse and respiratory melancholy. Tramadol can be discovered as 2 enantiomers with active analgesic homes however, the mechanism of motion of each of the enantiomers differs significantly.[A173980] inside the FDA records, the first accredited tramadol product was advanced by Actavis Elizabeth and FDA permitted in 2002.[L5125]

Pharmacology

Pharmacodynamics

Tramadol inhibits the descending pain pathways at the spinal level.[A173983] There are reports supporting the fact that tramadol activity goes beyond the inhibition of opioid receptors. In this reports the administration of [naloxone] only reduced the activity of tramadol by 30%. Those reports also indicate that the inhibition of metabolic enzymes, used for the generation of M1 which has a very high affinity for opioids, does not affect tramadol-induced analgesia.[A174007] The inhibition of neurotransmitters by both tramadol enantiomers has been shown to enhance the inhibitory descending pathways associated with pain transmission in the CNS.[A173980] At the same time, it presents local anesthetic properties by blocking potassium channels[A173983] and its secondary mechanisms of action are thought to increase the activity of endogenous inhibitory control and decrease pain transmission which would explain the central analgesic effects of tramadol.[A173989] From the racemic form, the (+)-tramadol seems to be more effective but less tolerated if administered alone. This indicates the importance of having the racemic mix in order to have the most optimal results. The effect of this racemic mix is compared to be of about 20% of the effect of morphine.[L5128]

Indication

Tramadol is approved for the management of moderate to severe pain in adults.[FDA label] As an off-label indication, tramadol has been investigated to be used for the treatment of premature ejaculation.[A173986]

Action

Tramadol has a dual action of pain relief by acting as both a central opiate agonist and a central nervous system reuptake inhibitor of norepinephrine and serotonin. (+)-Tramadol and its O-desmethyl metabolite (M1) are selective and weak mu receptor agonist which in order, alter the release of nociceptive neurotransmitters. From these two molecules, the metabolite M1 metabolite has 300 times more affinity for this receptor while (+)-tramadol also inhibits serotonin reuptake. On the other hand, (-)-tramadol inhibits norepinephrine reuptake.[A173980] Other than this major mechanism of action, tramadol is known and fully studied due to its inhibitory activity against alpha2-adrenoreceptors, neurokinin 1 receptors, and muscarinic receptors as well as the inhibition of ion channels via nicotinic acetylcholine receptor and N-methyl-D-aspartate receptor.[A173989]