what is Tramadol drug

1. By: Zahraa Rahman

2. Tramadol is a narcotic-like pain reliever.
Tramadol is used to treat moderate to severe pain.
The extended-release form of tramadol is for around-the-clock treatment of pain.
This form of tramadol is not for use on an as-needed basis for pain.
Tramadol may also be used for purposes not listed in this medication guide.
You should not take tramadol if you have used alcohol, sedatives, tranquilizers, or
narcotic medications within the past few hours.
Tramadol can slow or stop your breathing, especially when you start using this
medicine or whenever your dose is changed. Never take tramadol in larger
amounts, or for longer than prescribed. Do not crush, break, or open an extended-
release pill. Swallow it whole to avoid exposure to a potentially fatal dose.

3. The most common adverse effects of tramadol include nausea, dizziness, dry mouth, indigestion,
abdominal pain, vertigo, vomiting, constipation, drowsiness and headache.[16][17] Compared to
other opioids, respiratory depression and constipation are considered less of a problem with
tramadol.
There are suggestions that chronic opioid administration may induce a state of immune
tolerance,although tramadol, in contrast to typical opioids, may enhance immune function.
Some have also stressed the negative effects of opioids on cognitive functioning and personality.

4. Before taking this medicine
You should not take tramadol if you are allergic
to it, or if you have:
severe asthma or breathing problems;
a blockage in your stomach or intestines;
if you have recently used alcohol, sedatives
tranquilizers, or narcotic medications.
, Seizures have occurred in some people taking
tramadol. Talk with your doctor about your seizure risk
, which may be higher if you have:
a history of head injury, epilepsy or other seizure disorder;
a history of drug or alcohol addiction;
a metabolic disorder; or
if you are also using certain medicines to treat migraine headaches, muscle spasms, depression,
mental illness, or nausea and vomiting.
To make sure tramadol is safe for you, tell your doctor if you have:
liver or kidney disease;
a stomach disorder; or
a history of drug abuse, alcohol addiction, mental illness, or suicide attempt.
Tramadol is more likely to cause breathing problems in older adults and people who are severely ill,
malnourished, or otherwise debilitated.
Tramadol may be habit forming and should be used only by the person it was prescribed for. Never
share this medicine with another person, especially someone with a history of drug abuse or
addiction. Keep the medication in a place where others cannot get to it. Selling or giving away
tramadol to any other person is against the law.

5. Tramadol has inhibitory actions on the 5-HT2C receptor. Antagonism of 5-HT2C could be partially
responsible for tramadol's reducing effect on depressive and obsessive-compulsive symptoms in
patients with pain and co-morbid neurological illnesses.[46] 5-HT2C blockade may also account for
its lowering of the seizure threshold,
as 5-HT2C knockout mice display significantly increased vulnerability to epileptic seizures,
sometimes resulting in spontaneous death. However, the reduction of seizure threshold could be
attributed to tramadol's putative inhibition of GABAA receptors at high doses.
[45] In addition, tramadol's major active metabolite, O-desmethyltramadol, is a high-affinity ligand of
the δ- and κ-opioid receptors, and activity at the former
receptor could be involved in tramadol's ability
to provoke seizures in some individuals,
as δ-opioid receptor agonists are well known to induce seizures.

6. Tramadol undergoes hepatic metabolism via the cytochrome P450 isozyme CYP2B6, CYP2D6 and
CYP3A4, being O- and N-demethylated to five different metabolites. Of these, O-desmethyltramadol
is the most significant since it has 200 times the μ-affinity of (+)-tramadol, and furthermore has an
elimination half-life of nine hours, compared with six hours for tramadol itself. As with codeine, in the
6% of the population that have reduced CYP2D6 activity (hence reducing metabolism),
There is therefore a reduced analgesic effect. Those with decreased CYP2D6 activity require a dose
increase of 30% in order to achieve the same degree of pain relief than those with a normal level of
CYP2D6 activity.[52][53]
Phase II hepatic metabolism renders the metabolites water-soluble, which are excreted by the
kidneys. Thus, reduced doses may be used in renal and hepatic impairment.[10]
Its volume of distribution is approximately, 306 L after oral administration and 203 L after parenteral
administration.[10]

7. Tramadol interacts, potentially fatally, with such serotonergics, monoamine oxidase inhibitors,
tricyclic antidepressants, selective serotonin reuptake inhibitors, serotonin-norepinephrine 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, phenethylamines/Substituted phenethylamines,
phentermine, lithium, methylene blue as well as numerous other therapeutic agents.[4][9] As it is a
substrate of CYP3A4 and CYP2D6, hence any agents with the ability to inhibit or induce these
enzymes will likely interact with tramadol.
A pressor response similar to the so-called "cheese effect" was noted in combinations of
amphetamine and tramadol, which appears to cause dysfunction of or toxicity to
epinephrine/norepinephrine re

8. Its use is not advised for people deficient in CYP2D6 enzymes which accounts for about 6–10% of
Caucasians and 1–2% of Asians, as they are crucial to the therapeutic effects of tramadol, by means
of enabling tramadol's metabolism to O-desmethyltramadol.

9. Tramadol is used primarily to treat mild-severe pain, both acute and chronic.
Tramadol is recommended for the management of pain in fibromyalgia by the
European League Against Rheumatism.Its analgesic effects take about one hour to
come into effect and 2–4 hours to peak after oral administration with an immediate-
release formulation.[9] On a dose-by-dose basis tramadol has about one-tenth the
potency of morphine and is approximately equally potent when compared to pethidine
and codeine.
For pain moderate in severity its effectiveness is equivalent to that of morphine; for
severe pain it is less effective than morphine.These painkilling effects peak at about 3
hours, post-oral administration and last for approximately 6 hours.
These analgesic effects are only partially reversed by naloxone, hence indicating that
its opioid action is unlikely the sole contributing factor; tramadol's analgesic effects are
also partially reversed by α2 adrenergic receptor antagonists like yohimbine and the 5-
HT3 receptor antagonist, ondansetron.
Pharmacologically, tramadol is similar to levorphanol and tapentadol in that it not only
binds to the mu opioid receptor, but also inhibits the reuptake of serotonin and
norepinephrine.
due to its action on the noradrenergic and serotonergic systems, such as its "atypical"
opioid activity.
Available dosage forms include capsules, tablets, including extended release
formulations and injections.

10. Its use in pregnancy is generally advised against as it may cause some reversible
withdrawal effects in the newborn.[14] A small prospective study in France found that,
while there was an increased risk of miscarriages, there were no major malformations
reported in the newborn.[14] Its use during lactation is also generally advised against,
but a small trial found that infants breastfed by mothers taking tramadol were exposed
to about 2.88% of the dose the mothers were taking. There was no evidence of this
dose having a harmful effect on the newborn.

11. Its use as an analgesic during labour is generally advised against due to its long-onset of action (one
hour).[14] The ratio of the mean concentration of the drug in the fetus compared to that of the
mother when it is given intramuscularly for labour pains has been estimated to be 94.

12. Its use in children is generally advised against, although it may be done under the supervision of a
specialist.
Elderly
There is an increased risk of opioid-related adverse effects such as respiratory depression, falls,
cognitive impairment and sedation.
Liver and kidney failure
It is advised that the drug be used with caution in those with liver or kidney failure, due to the high
dependence of the drug on the liver and kidneys for metabolism to O-desmethyltramadol and
elimination, respectively.