How does the painkiller Tramadol(Generic Ultram) work?
I also have to write a report on the pharmacology of Tramadol(Generic Ultram), could someone help me out? Preferably the guy who answered my codeine question.
Answer by Jacob
(Zydol, Tramacip, Ultram, (Ultracet, Tramacet – when combined with APAP)
Tramadol causes instant inhibition of serotonin and norepenephrine reuptake. This leads to increased feeling of wellbeing and happiness.
Tramadol itself acts weakly on the μ-opioid (μ is the greek letter Mu) receptors (the ones responsible for euphoria and analgesia).
Now, once the Tramadol(Generic Ultram) has been metabolised in the liver, it’s M1 metabolite (odesmethyltramadol) then binds to the aforementioned opioid receptors causing a much more powerful euphoria (200x more potent than that of morphine), however, the amount of odesmethyltramadol is quite small, so the potency is relative.
The metabolisation must be considered, because not everyone metabolises Tramadol(Generic Ultram) in the same manner, some barely metabolise any into odesmeth… hence many complain that Tramadol(Generic Ultram) is ineffectual. This is the reason why usually.
Also, the high from Tramadol(Generic Ultram) lasts longer than that of most other opioids, sometimes up to 16 hours.
Capsules (regular and extended release) (Doses usually ranging from 50mg IR (Instant release), 100mg SR (sustained release) to 200mg SR)
Tablets (regular, extended release, chewable, low-residue and/or uncoated pills that can be taken by the sublingual and buccal routes)
Suppositories (bypasses hepatic demethylation)
Tablets and capsules containing (acetaminophen/APAP), aspirin and other agents. (for analgesic synergy)
Effervescent pills and powders
Ampules of sterile solution for SC, IM, and IV injection (bypasses hepatic demethylation)
Preservative-free solutions for injection by the various spinal routes (epidural etc) (bypasses hepatic demethylation)
Liquids with and without alcohol for oral and/or sub-lingual use, available in regular phials and bottles, dropper bottles, bottles with a pump similar to those used with liquid soap and phials with droppers built into the cap.
Bioavailability = 68 – 72% (this increases with repeated dosing due to increasing amounts of o-desmethyltramadol)
Half life = ~5-7 hours
Metabolism = Hepatic demethylation (to odesmethyltramadol) & glucuronidation
Seizure (Usually only with overdose)
Serious contraindications – Important!
SSRI medications can cause too much serotonin to build up in the brain and cause the deadly Serotonin Syndrome! AKA Serotonin Storm!
DXM (Dextromethorphan Hydrobromide), because it has Serotonin inhibiting properties and can cause the same syndrome as above.
Atypical antipsychotics are also at great risk of causing dangerous interactions when combined with tramadol.
Other notable information
Any other route except oral bypasses the hepatic demethylation, weakening the opioid effects of the drug.
Although not often warned or mentioned by prescribing doctors, Tramadol(Generic Ultram) DOES have an addiction profile and should be considered an addictive substance if abused.
I’m Jacob, who advised you on your codeine question. I’ve put all the info you’d need on here. Good luck! 🙂