What is the main narcotic in Tramacet (tramadol)?

The Main Narcotic in Tramacet

The main narcotic component in Tramacet is tramadol, which is a centrally acting synthetic opioid analgesic that binds to μ-opioid receptors and inhibits the reuptake of norepinephrine and serotonin. 1, 2

Pharmacology of Tramadol

• Tramadol is a synthetic 4-phenyl-piperidine analogue of codeine with a dual mechanism of action: opioid activity through μ-receptor binding and monoaminergic activity through inhibition of norepinephrine and serotonin reuptake 2
• The analgesic effect of tramadol comes from both the parent compound and its active metabolite M1 (O-desmethyl-tramadol), which has up to 6 times more potent analgesic effects and 200 times higher μ-opioid binding affinity than tramadol itself 1
• Tramadol is a racemic mixture of two enantiomers with complementary actions: (+)-tramadol preferentially inhibits serotonin reuptake and binds to μ-receptors, while (-)-tramadol mainly inhibits norepinephrine reuptake 2

Tramacet Composition

• Tramacet (also known as Zaldiar, Ixprim, or Kolibri) is a fixed-dose combination containing tramadol hydrochloride 37.5 mg and paracetamol (acetaminophen) 325 mg per tablet 3
• The combination provides multimodal analgesia with tramadol acting centrally and paracetamol providing peripheral analgesic effects 3

Clinical Properties of Tramadol

• Analgesia begins approximately within one hour after administration and reaches peak effect in approximately two to three hours 1
• Tramadol has about one-tenth the analgesic potency of morphine following parenteral administration 4
• It is metabolized primarily in the liver via O- and N-demethylation, with CYP2D6 responsible for producing the active M1 metabolite 4
• The mean elimination half-life of tramadol is approximately 6 hours 4

Safety Considerations

• Tramadol carries risks of seizures, especially at doses exceeding the recommended range or when combined with medications that lower seizure threshold 1
• Concomitant use with serotonergic drugs increases the risk of serotonin syndrome, a potentially life-threatening condition 1
• Respiratory depression is less common with tramadol compared to other opioids, but still requires caution, particularly in high-risk patients 5
• In patients with liver cirrhosis, tramadol should be limited to 50 mg every 12 hours due to increased bioavailability 6

Clinical Applications

• Tramadol is indicated for moderate to severe pain and is considered a step 2 analgesic according to the World Health Organization pain ladder 2
• It is used for both acute pain (postoperative, trauma) and chronic pain conditions, particularly neuropathic pain 4
• The combination of tramadol with paracetamol in Tramacet provides effective pain relief for moderate to severe pain with potentially fewer side effects than higher doses of either component alone 3

In summary, tramadol is the narcotic component in Tramacet, functioning as a centrally acting analgesic with both opioid and non-opioid mechanisms of action, making it unique among opioid medications.