Tramadol
Posted on August 6, 2009
Filed Under Japanese Fashion |
Tramadol is a centrally acting analgesic, used for treating moderate to severe pain. It is a synthetic opioid and it appears to have actions at the μ-opioid receptor as well as the noradrenergic and serotonergic systems. Tramadol was developed by the German pharmaceutical company Grünenthal GmbH in the late 1970s. Tramadol’s chemical structure is quite different from those of opiates. The closest chemical relative of tramadol in clinical use is tapentadol, which is a member of the same chemical class as tramadol and also developed by Grünethal.
Tramadol is used to treat moderate to moderately severe pain and most types of neuralgia, including trigeminal neuralgia. It has been suggested that tramadol could be effective for alleviating symptoms of depression, anxiety, and phobias because of its action on the noradrenergic and serotonergic systems. However, health professionals have not yet fully endorsed of its use on a large scale for these disorders, although it may be used when other treatments have failed (under the supervision of a psychiatrist).
Tramadol is usually marketed as the hydrochloride salt (tramadol hydrochloride); the tartrate is seen on rare occasions, and tramadol is available in both injectable (intravenous and/or intramuscular) and oral preparations. It is also available in conjunction with acetaminophen. The solutions suitable for injection are used in Patient-Controlled Analgesia pumps under some circumstances, either as the sole agent or along with another agent such as morphine.
Tramadol comes in many forms, including:
* capsules
* tablets
* extended-release tablets
* extended-release capsules
* chewable tablets
* low-residue and/or uncoated tablets that can be taken by the sublingual and buccal routes
* suppositories
* effervescent tablets and powders
* ampoules of sterile solution for SC, IM, and IV injection
* preservative-free solutions for injection by the various spinal routes (epidural, intrathecal, caudal, and others)
* powders for compounding
* liquids both with and without alcohol for oral and sublingual administration, 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
* tablets and capsules containing paracetamol (acetaminophen) and aspirin and other agents
Tramadol has been experimentally used in the form of an ingredient in multi-agent topical gels, creams, and solutions for nerve pain, rectal foam, concentrated retention enaema, and a skin plaster (transdermal patch) quite similar to those used with lidocaine.
Tramadol has a characteristic taste which is mildly bitter but much less so than morphine and codeine. Oral and sublingual drops and liquid preparations come with and without added flavouring. Its relative effectivness via transmucousal routes (sublingual, buccal, rectal) is around that of codeine, and, like codeine, it is also metabolised in the liver to stronger metabolites (see below).
The maximum dosage for tramadol in any form is 400 mg/day. Certain manufacturers or formulations have lower maximum doses. For example, Ultracet (37.5 mg/325 mg tramadol/APAP tablets) is capped at 8 per day (300 mg/day). Other popular formulations such as Ultram ER are available in 100, 200, and 300 mg/day doses. Patients with impaired hepatic function or using SSRIs should consult with their doctor regarding adjusted dosing.
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