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DRUG PROFILE:
Drug
:Tramadol
Drug category
: NSAID
Structure
: 2-[(Dimethylamino)methyl]-1-(3-
methoxyphenyl)cyclohexanol
Molecular Formula
: C16H25NO2
Molecular Weight
: 263.4 g/mol
DRUG PROFILE
PHARMACOKINETIC PROPERTIES:
Bioavailability
: 7075% (oral)
Half-life
: 6.3 1.4 hr
Absorption
Protein binding
Metabolism
: 20 %
: Liver-mediated demethylation and glucuronidation via
: O-Desmethyltramadol, N-Desmethyltramadol, O-
Desmethyl-tramado glucuronide
Time of peak action
: 2-3 hrs
Excretion
: Urine (95%)
include nausea, dizziness, dry mouth, indigestion, abdominal pain, vertigo, vomiting,
constipation, drowsiness and headache. Compared to other opioids, respiratory depression
and constipation are considered less of a problem with tramadol.
PHARMACODYNAMICS:
Mechanism of action: 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
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DRUG PROFILE
Contraindications: Its use is not advised for people deficient in CYP2D6 enzymes which
accounts for about 610% of Caucasians and 12% of Asians, as they are crucial to the
therapeutic effects of tramadol, by means of enabling tramadol's metabolism to Odesmethyltramadol.
INTERACTIONS:
Drug interactions: Tramadol interacts with such serotonergics, monoamine oxidase
inhibitors, tricyclic antidepressants, selective serotonin reuptake inhibitors, serotoninnorepinephrine reuptake inhibitors, noradrenergic and specific serotonergic antidepressants,
serotonin antagonist and reuptake inhibitors, certain analgesics (pethidine (meperidine),
tapentadol, oxycodone, dextromethorphan and fentanyl), certain anxiolytics (such as the
SSRIs and buspirone), certain antibiotics (namely, linezolid and isoniazid), certain herbs
(e.g.
St.
John's
wort,
passiflora,
etc.),
amphetamines/substituted
amphetamines,
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