Is tramadol an enzyme inducer?
Tramadol is a prodrug that is metabolised by cytochrome P450 (CYP) enzymes CYP2D6 and CYP3A4 to its more potent metabolites particularly O-desmethyltramadol (M1) as well as N, O-desmethyltramadol (M5).
Which CYP2D6 phenotype is associated with increased risk for toxicity with tramadol?
In PMs for CYP2D6, reduced analgesic effects have been observed, whereas in UMs cases of life-threatening toxicity have been reported with tramadol and codeine. CYP2D6 PM phenotype has been associated with an increased risk of toxicity of metoprolol, timolol, carvedilol and propafenone.
What gene metabolizes tramadol?
Background and objective: Tramadol is metabolized by the highly polymorphic enzyme cytochrome P450 (CYP)2D6. Patients with different CYP2D6 genotypes may respond differently to tramadol in terms of pain relief and adverse events.
What receptors does tramadol work?
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.
What is CYP2D6 polymorphism?
The polymorphism of the enzyme results in poor, intermediate, efficient or ultrarapid metabolisers (UMs) of CYP2D6 drugs. The polymorphism of CYP2D6 significantly affects the pharmacokinetics of about 50% of the drugs in clinical use, which are CYP2D6 substrates.
What is tramadol hydrochloride used for?
Tramadol is a strong painkiller. It’s used to treat moderate to severe pain, for example after an operation or a serious injury. It’s also used to treat long-standing pain when weaker painkillers no longer work.
Is tramadol metabolized by CYP2D6?
The CYP2D6 enzyme converts tramadol to the active metabolite, O-desmethyltramadol (M1), which has a significantly higher affinity for the mu-opioid receptor than tramadol. The M1 metabolite is up to 6 times more potent than tramadol in producing analgesia.
Are there any cytochrome P450 3A4 inducers for tramadol?
Use of cytochrome P450 3A4 inducers, 3A4 inhibitors, or 2D6 inhibitors with Tramadol requires careful consideration of the effects on the parent drug, tramadol, and the active metabolite, M1 (see WARNINGS, PRECAUTIONS; Drug Interactions).
Are there any inhibitors or inducers of CYP2B6?
(a) Strong inhibitor of CYP1A2 and CYP2C19, and moderate inhibitor of CYP2D6 and CYP3A. (b) We currently do not have index inhibitors for CYP2B6. (c) Strong inhibitor of CYP2C8, weak inhibitor of CYP2B6, and inhibitor of OATP1B1. The glucoronide metabolite is also an inhibitor for CYP2C8 and OATP1B1.
What should I know about tramadol hydrochloride tablets?
Important information about Tramadol Hydrochloride Tablets, USP: 1 Get emergency help right away if you take too much Tramadol Hydrochloride Tablets, USP (overdose) . 2 Taking tramadol hydrochloride tablets, USP with other opioid medicines, benzodiazepines, alcohol,… 3 Never give anyone else your tramadol hydrochloride tablets, USP.
When to switch from tramadol hydrochloride to extended release?
Conversion from Tramadol Hydrochloride Tablets to Extended-Release Tramadol The relative bioavailability of tramadol hydrochloride tablets compared to extended-release tramadol is unknown, so conversion to extended-release formulations must be accompanied by close observation for signs of excessive sedation and respiratory depression.