Tramadol; Uses, Dosage, Side Effects, Interactions

Tramadol
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Tramadol is a synthetic codeine analog, tramadol has central analgesic properties with effects similar to opioids, such as morphine and codeine, acting on specific opioid receptors. Used as a narcotic analgesic for severe pain, it can be addictive and weakly inhibits norepinephrine and serotonin reuptake.
Tramadol is an opioid analgesic used for the therapy of mild-to-moderate pain. Tramadol overdose can cause acute liver failure. Pharmacologic use of tramadol has not been associated with cases of the clinically apparent drug-induced liver disease.

Tramadol is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually occurs within an hour. It is often combined with paracetamol (acetaminophen) as this is known to improve the efficacy of tramadol in relieving pain.

Mechanism of Action of Tramadol

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 a 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.
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Tramadol is a racemic mixture (R & S) that has a complicated mechanism of action. It has some mu-opioid receptor action, but this effect is 10 times lower than codeine and 6000 times lower than morphine. Tramadol also inhibits the reuptake of norepinephrine (NE) and serotonin (5 HT) and produces secondary effects on alpha-2 adrenergic receptors in pain pathways. One isomer has a greater effect on 5 HT reuptake and greater affinity for mu-opiate receptors. The other isomer is more potent for NE reuptake and less active for inhibiting 5 HT reuptake. Taken together, the effects of tramadol may be explained through inhibition of 5 HT reuptake, action on alpha2 receptors, and mild activity on opiate mu-receptors.
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The transient receptor potential vanilloid 1 (TRPV1) and the transient receptor potential ankyrin 1 (TRPA1), which are expressed in sensory neurons, are polymodal nonselective cation channels that sense noxious stimuli. Recent reports showed that these channels play important roles in inflammatory, neuropathic, or cancer pain, suggesting that they may serve as attractive analgesic pharmacological targets. Tramadol is an effective analgesic that is widely used in clinical practice. Reportedly, tramadol and its metabolite (M1) bind to mu-opioid receptors and/or inhibit reuptake of monoamines in the central nervous system, resulting in the activation of the descending inhibitory system. However, the fundamental mechanisms of tramadol in pain control remain unclear. TRPV1 and TRPA1 may be targets of tramadol; however, they have not been studied extensively. We examined whether and how tramadol and M1 act on human embryonic kidney 293 (HEK293) cells expressing human TRPV1 (hTRPV1) or hTRPA1 by using a Ca imaging assay and whole-cell patch-clamp recording. Tramadol and M1 (0.01-10 uM) alone did not increase in intracellular Ca concentration ([Ca]i) in HEK293 cells expressing hTRPV1 or hTRPA1 compared with capsaicin (a TRPV1 agonist) or the allyl isothiocyanate (AITC, a TRPA1 agonist), respectively. Furthermore, in HEK293 cells expressing hTRPV1, pretreatment with tramadol or M1 for 5 minutes did not change the increase in [Ca] I induced by capsaicin. Conversely, pretreatment with tramadol (0.1-10 uM) and M1 (1-10 uM) significantly suppressed the AITC-induced [Ca] I increases in HEK293 cells expressing hTRPA1. In addition, the patch-clamp study showed that pretreatment with tramadol and M1 (10 uM) decreased the inward currents induced by AITC. These data indicate that tramadol and M1 selectively inhibit the function of hTRPA1, but not that of hTRPV1 and that hTRPA1 may play a role in the analgesic effects of these compounds.

Indications of Tramadol

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Therapeutic Indications of Tramadol

  • Analgesics, Opioid; Narcotics
  • Tramadol hydrochloride tablets, USP are indicated for the management of moderate to moderately severe pain in adults.
  • Tramadol hydrochloride extended-release tablets are indicated for the management of moderate to moderately severe chronic pain in adults who require around-the-clock treatment of their pain for an extended period of time.

Contra-Indications of Tramadol

Tramadol is contraindicated in those with hypersensitivity,

Dosage of Tramadol

Strengths: 50 mg; 100 mg/24 hours; 200 mg/24 hours;

Pain

Immediate-release

  • 50 to 100 mg orally every 4 to 6 hours as needed for pain
  • Maximum dose: 400 mg per day

Chronic Pain

Immediate-Release (IR)

  • Initial dose: 25 mg orally once a day; titrate in 25 mg increments every 3 days to reach a dose of 25 mg four times a day; thereafter increase by 50 mg as tolerated every 3 days to reach a dose of 50 mg four times a day
  • Maintenance dose: After titration, 50 to 100 mg orally as needed for pain every 4 to 6 hours
  • Maximum dose: 400 mg per day

Extended-Release (ER)

  • Initial dose (tramadol-naive): 100 mg orally once a day
  • Individually titrate in 100 mg increments every 5 days to an effective dose that minimizes adverse reaction
  • Maximum Dose: 300 mg orally per day
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Geriatric Pain

  • Age: 75 years or older: Maximum dose: 300 mg per day

Geriatric, Chronic Pain

  • Age: 75 years or older: Maximum dose: 300 mg per day

Pediatric Dose for Pain

17 years or older

  • Immediate-release: 50 to 100 mg orally every 4 to 6 hours as needed for pain
  • Maximum dose: 400 mg per day

Immediate-Release

  • Initial dose: 25 mg orally once daily; titrate in 25 mg increments every 3 days to reach a dose of 25 mg four times a day; thereafter increase by 50 mg as tolerated every 3 days to reach a dose of 50 mg four times a day
  • Maintenance dose: After titration, 50 to 100 mg orally as needed for pain every 4 to 6 hours
  • Maximum dose: 400 mg per day

Side Effects of Tramadol

The most common

More common

Rare

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Drug Interactions of Tramadol

Tramadol may interact with following drugs, supplements & may change the efficacy of drugs

Pregnancy & Lactation of Tramadol

FDA pregnancy category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately

Lactation

Tramadol can increase serum prolactin.However, the prolactin level in a mother with established lactation may not affect her ability to breastfeed.A randomized study compared tramadol and naproxen for post-cesarean section pain. Patients received the drugs either on a fixed schedule or as needed. No difference in breastfeeding rates was seen among the groups.

References

  1. PubChem
    Data deposited in or computed by PubChem

    https://pubchem.ncbi.nlm.nih.gov

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