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By: Zahraa Rahman
Tramadol is a narcotic-like pain reliever.
Tramadol is used to treat moderate to severe pain.
The extended-release form of...
The most common adverse effects of tramadol include nausea, dizziness, dry mouth, indigestion,
abdominal pain, vertigo, vo...
Before taking this medicine
You should not take tramadol if you are allergic
to it, or if you have:
severe asthma or breat...
Tramadol has inhibitory actions on the 5-HT2C receptor. Antagonism of 5-HT2C could be partially
responsible for tramadol's...
Tramadol undergoes hepatic metabolism via the cytochrome P450 isozyme CYP2B6, CYP2D6 and
CYP3A4, being O- and N-demethylat...
Tramadol interacts, potentially fatally, with such serotonergics, monoamine oxidase inhibitors,
tricyclic antidepressants,...
Its use is not advised for people deficient in CYP2D6 enzymes which accounts for about 6–10% of
Caucasians and 1–2% of Asi...
Tramadol is used primarily to treat mild-severe pain, both acute and chronic.
Tramadol is recommended for the management o...
Its use in pregnancy is generally advised against as it may cause some reversible
withdrawal effects in the newborn.[14] A...
Its use as an analgesic during labour is generally advised against due to its long-onset of action (one
hour).[14] The rat...
Its use in children is generally advised against, although it may be done under the supervision of a
specialist.
Elderly
T...
Tramadol
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Tramadol

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what is Tramadol drug

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Tramadol

  1. 1. By: Zahraa Rahman
  2. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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.

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