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What is Tramadol?

Tramadol is a prescription pain medication that works in the brain and nervous system to reduce pain. It belongs to a class of medications called opiate agonists and works by binding to opioid receptors. Tramadol Purchase is available under the brand names Ultram, Ultram ER, Conzip, and Ryzolt.

Chemical Structure

The chemical structure of tramadol consists of two enantiomers, (+)-tramadol and (-)-tramadol. The (+)-tramadol enantiomer exerts a greater affinity for μ-opioid receptors, which contributes to its analgesic effects.

Mechanism of Action

Tramadol has a dual mechanism of action. It works as both a weak opioid agonist and inhibits the reuptake of serotonin and norepinephrine. The opioid effects activate μ-opioid receptors, which inhibits pain signals. The effects on serotonin and norepinephrine enhance the pain relieving effects.

Metabolism

Tramadol undergoes extensive first-pass liver metabolism. About 30% of an oral dose is converted to O-desmethyltramadol by the enzyme CYP2D6. This active metabolite has a much higher affinity for μ-opioid receptors compared to tramadol itself.

O-desmethyltramadol

O-desmethyltramadol is the primary active metabolite of tramadol. It has 200 times greater analgesic potency compared to tramadol due to its higher μ-opioid receptor affinity. Levels of this metabolite play a key role in the analgesic efficacy of tramadol.

What Conditions is Tramadol Used to Treat?

Tramadol is mainly used to help relieve moderate to moderately severe pain following surgery, injury, or due to conditions such as osteoarthritis. It also has uses for chronic pain management.

Moderate to Moderately Severe Pain

Tramadol is commonly prescribed off-label to treat many types of acute pain after surgery or trauma when over-the-counter medicines like acetaminophen or NSAIDs are not sufficient. It provides more powerful pain relief due its dual opioid and non-opioid effects.

Chronic Pain

While tramadol is only FDA approved for short-term use, it is very frequently prescribed off-label to treat various chronic pain conditions.

Low Back Pain

Tramadol may be used to treat low back pain that is moderate to severe when acetaminophen or NSAIDs do not provide enough relief.

Osteoarthritis Pain

Tramadol is commonly taken to reduce osteoarthritis pain in joints like the knees, hips, hands, and spine. It can enable increased mobility when anti-inflammatories are not adequately effective.

Fibromyalgia

For fibromyalgia patients, tramadol is frequently prescribed to help relieve widespread muscle pain and tenderness. It offers analgesia without having as strong of an anti-inflammatory effect as NSAIDs.

Post-Surgical Pain

Managing post-surgical pain is one of the main uses for tramadol. It provides more powerful analgesic effects than acetaminophen or NSAIDs alone following invasive procedures. The extended release forms of tramadol allow longer lasting relief.

How is Tramadol Taken?

Tramadol is available in immediate and extended release oral formulations to be taken by mouth. It also comes in a solution for injection.

Forms of Tramadol

Tramadol comes in tablet, capsule, and liquid forms that are taken orally. There is also an injectable solution used mainly in hospitals.

Immediate Release Tramadol

The regular immediate release tablet or oral solution is taken usually 4-6 times per day. It offers relief for 4-6 hours per dose.

Extended Release Tramadol

Extended release tramadol tablets and capsules contain a higher dose that is slowly released over 12-24 hours. This minimizes gaps in pain control and allows once or twice daily dosing.

Dosage

The recommended tramadol dosage depends on the pain severity and previous opioid exposure.

Initial Dosage

The typical starting dose is 50-100 mg every 4-6 hours as needed for pain for regular tablets. The maximum dose is 400 mg per day.

Titration

The dose is usually slowly increased over time for better pain control or reduced if side effects occur. Finding the minimum effective dose helps avoid issues.

Side Effects and Risks

Common tramadol side effects include nausea, dizziness, drowsiness, vomiting, and constipation. More severe reactions like serotonin syndrome and seizures are rare but possible.

Common Side Effects

Like other opioids, tramadol frequently causes certain bothersome side effects, especially when first starting. Tolerance develops over time so the symptoms may improve.

Nausea

Feelings of stomach upset, indigestion, and nausea are reported by around a quarter of people taking tramadol. This tends to resolve within 1-2 weeks. Taking it with food helps.

Drowsiness

Drowsiness and fatigue are common due to the inhibitory effects in the CNS. This may reduce after using tramadol for a week or two as tolerance increases. Avoid driving when first taking it.

Constipation

Decreased gut motility leading to constipation occurs in 15-30% of people taking tramadol. Staying hydrated, exercise, fiber, and laxatives help manage it.

Serotonin Syndrome

In rare cases, tramadol may cause excessive serotonin activity leading to serotonin syndrome. Symptoms are confusion, fever, tremors, and poor coordination. Seek emergency help if these occur.

Seizures

Seizures can very rarely occur in patients taking the highest doses of tramadol or in those with epilepsy or a history of seizures. Lower doses are safer.

Suicidal Thoughts

There is a slight risk of emerging suicidal ideation, especially in young adults. Seek medical help immediately if such thoughts occur when taking tramadol.

Alternatives to Tramadol

Other medications that may be used instead of tramadol for pain relief include OTC analgesics like acetaminophen, NSAIDs like ibuprofen, or opioids like codeine. Each option has pros and cons to weigh with your doctor.

Acetaminophen

Acetaminophen (Tylenol) is less effective than tramadol for many types of pain but has fewer side effects. It lacks anti-inflammatory qualities but may still be helpful.

NSAIDs

Non-steroidal anti-inflammatory drugs like ibuprofen help by reducing inflammation. They work well for arthritis but less for non-inflammatory pain like neuropathy. Upset stomach and ulcers are risks.

Opioids

Stronger traditional opioids like hydrocodone or oxycodone may provide better pain relief but have greater dependency risks. Tramadol is less tightly controlled and regulated in most regions.

Conclusion

Tramadol is a prescription opioid medication mainly used for the treatment of moderate to moderately severe acute and chronic pain. Common conditions it helps with include back pain, osteoarthritis, and fibromyalgia. While tramadol does not cause euphoria and has a lower dependence profile, side effects like nausea and fatigue are still common. Working with your doctor to find the right dose with tolerable side effects provides the best pain relief results.

FAQs

What is tramadol most commonly prescribed for?

The most common uses of tramadol are relieving moderate acute pain after surgery and reducing flair ups of chronic pain conditions like arthritis. It offers more powerful pain relief than OTC analgesics for these purposes.

What should you avoid when taking tramadol?

Avoid driving, operating machinery, and other dangerous activities when first starting tramadol until you know how the dizziness and drowsiness will affect you. Also avoid alcohol and benzodiazepine tranquilizers which increase risks.

Can tramadol be addictive?

While tramadol has a lower addiction and dependence potential than traditional opioids, addiction is still possible, especially with long-term use at high doses. Always take the medication as directed by your doctor.

What should you do if tramadol makes you feel faint or dizzy?

Feeling lightheaded, dizzy or faint after taking tramadol needs prompt medical attention. Lie down and lift your feet above heart level if you can. Call 911 or emergency services if you faint, have chest pain or trouble breathing.

Who should not take tramadol?

People who should avoid tramadol or require extreme caution include those with severe liver or kidney dysfunction, gastric issues, head injuries, epilepsy or seizure disorders, and suicidal thoughts or tendencies. Children under 18 should also not take it.