Tramadol (Opioid analgesic)
Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. It may be sold in combination with paracetamol (acetaminophen) or as longer acting formulations
• Moderate to severe pain
• Intoxication with alcohol
• Centrally acting analgesics
• Psychotropic drugs
This medication is used to help relieve moderate to moderately severe pain. Tramadol is similar to opioid (narcotic) analgesics. It works in the brain to change how your body feels and responds to pain.
• Is an analgesic and antitussive
Nausea, vomiting, constipation, lightheadedness, dizziness, drowsiness, or headache may occur. Some of these side effects may decrease after you have been using this medication for a while. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
To prevent constipation, eat dietary fiber, drink enough water, and exercise. You may also need to take a laxative. Ask your pharmacist which type of laxative is right for you. To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Get medical help right away if you have any very serious side effects, including: fast/irregular heartbeat, severe dizziness, fainting, and seizure.
Tramadol is changed into a strong opioid drug in your body.
In some people, this change happens faster and more completely than usual, which increases the risk of very serious side effects. Get medical help right away if you notice any of the following: slow/shallow breathing, severe drowsiness/difficulty waking up, and confusion.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: brain disorders (such as head injury, tumor, seizures), breathing problems (such as asthma, sleep apnea, chronic obstructive pulmonary disease COPD), kidney disease, liver disease, mental/mood disorders (such as confusion, depression, suicidal thoughts), personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol), stomach/intestinal problems (such as blockage, constipation, diarrhea due to infection, paralytic ileus), difficulty urinating (such as due to enlarged prostate), gallbladder disease, disease of the pancreas (pancreatitis), obesity.
This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).
Tramadol may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.
Tramadol may interact with certain antidepressants and anxiolytics (particularly selective serotonin reuptake inhibitors, serotonin–norepinephrine reuptake inhibitors, monoamine oxidase inhibitors, and tricyclic antidepressants) other opioid analgesics (pethidine, tapentadol, oxycodone, and fentanyl), dextromethorphan, certain migraine medications (triptans, ergots), certain antibiotics (namely, linezolid and isoniazid), certain herbs (e.g. St. John’s wort, passiflora, etc.), stimulants (including amphetamines, phenethylamine, and phentermine), lithium, and methylene blue, as well as numerous other therapeutic agents.
As it is a substrate of CYP3A4 and CYP2D6, any agents with the ability to inhibit or induce these enzymes are 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 receptors.
Well as a potentiator often used with analgesics such as codeine, dihydrocodeine, hydrocodone and the like, is structurally related to the tricyclic antidepressants, so should not be used with tramadol; this is also the case for trazodone.
MECHANISM OF ACTION
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.
5-HT2C blockade may also account for its lowering of the seizure threshold, as 5-HT2Cknockout 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.
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.