Mechanism of action-
Tramadol is a centrally acting μ-opioid receptor agonist and SNRI (serotonin/norepinephrine reuptake-inhibitor) that is structurally related to codeine and morphine. Tramadol binds weakly to κ- and δ-opioid receptors and to the μ-opioid receptor with 6000-fold less affinity than morphine.
Tramadol exists as a racemic mixture consisting of two pharmacologically active enantiomers that both contribute to its analgesic property through different mechanisms: (+)-tramadol and its primary metabolite (+)-O-desmethyl-tramadol (M1) are agonists of the μ opioid receptor while (+)-tramadol inhibits serotonin reuptake and (-)-tramadol inhibits norepinephrine reuptake. These pathways are complementary and synergistic, improving tramadol's ability to modulate the perception of and response to pain.
Pharmacokinetics-
Tramadol is rapidly and almost completely absorbed following intramuscular administration.
The volume of distribution of tramadol is reported to be in the range of 2.6-2.9 L/kg.
About 20% of the administered dose is found to bind to plasma proteins.
Tramadol undergoes extensive first-pass metabolism in the liver by N- and O- demethylation and conjugation.
Tramadol is eliminated primarily through metabolism by the liver and the metabolites are excreted primarily by the kidneys, accounting for 90% of the excretion while the remaining 10% is excreted through feces.
Tramadol reported a half-life of 5-6 hours while the O-desmethyl-tramadol metabolite presents a half-life of 8 hours
Common side effect of tramadol includes:
- Redness, and swelling at the injection site
- Headache
- Drowsiness
- Fatigue
- Vomiting
- Constipation
- Dry mouth
- Sweating
Do not use this injection in the following conditions:
-
Decreased function of the adrenal gland
- Asthma
- A low seizure threshold
- Benzodiazepine overdose
- Kidney disease with likely reduction in kidney function
- Inherited dysfunction of autonomic nerve function
Following drugs may interact with tramadol:
-
Sertraline
- Cetirizine
- Alprazolam
- Warfarin
- Pregabalin
- Hydrocodone
- Gabapentin
- Duloxetine
- Diphenhydramine
- Zolpidem