Cecila
I also have to write a report on the pharmacology of Tramadol, could someone help me out? Preferably the guy who answered my codeine question.
Helen
Tramadol Hydrochloride (Zydol, Tramacip, Ultram, (Ultracet, Tramacet - when combined with APAP)EffectsTramadol 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 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 in the same manner, some barely metabolise any into odesmeth... hence many complain that Tramadol is ineffectual. This is the reason why usually.Also, the high from Tramadol lasts longer than that of most other opioids, sometimes up to 16 hours.FormsCapsules (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 tablets 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 tablets and powdersAmpules 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)PowdersLiquids 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.Pharmacokinetic InformationBioavailability = 68 - 72% (this increases with repeated dosing due to increasing amounts of o-desmethyltramadol)Half life = ~5-7 hoursMetabolism = Hepatic demethylation (to odesmethyltramadol) & glucuronidationSide EffectsDrowsinessFatigueConstipationDizzinessNauseaVomitingDry MouthHeadacheIndigestionSeizure (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 informationAny 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 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! :)
Mitsuko
Tramadol is a synthetic stripped-down piperidine-analog of the phenantherane alkaloid codeine and, as such, is an opioid and also a pro-drug (codeine is metabolized to morphine, tramadol is converted to M-1 aka O-desmethyltramadol). Opioids are chemical compounds which act upon one or more of the human opiate receptors (the euphoria, addictive nature and respiratory depression are mainly caused by the Mu(μ) 1 and 2 receptor. The opioid agonistic effect of Tramadol and its major metabolite(s) are almost exclusively mediated by the substance's action at the μ-opioid receptor. This characteristic distinguishes tramadol from many other substances (including morphine) of the opioid drug class, which generally do not possess tramadol's degree of subtype selectivity.
Clay
i take tremadol its pretty cool my doc says it tricks the mind into thinkin your on narcotics. makes me feel high. no body pain.
Balta
Kettleman City
Rubidoux
Friona
Margaret
Lakeview