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Tramadol Pain reliever, deep History, Best Uses, Side effects, & 10 Brands
Analgesic

Tramadol Pain reliever, deep History, Best Uses, Side effects, & 10 Brands

  • May 11, 2024
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Introduction

Tramadol is a pain reliever medication used to treat moderate to severe pain. It belongs to a class of drugs called opioids, which work by binding to opioid receptors in the brain to reduce the perception of pain. While tramadol can be an effective pain reliever, It can also be approved for short-term treatment of cancer pain.
It’s important to note that tramadol is a potent medication that should only be used under the guidance of a doctor. It is typically prescribed when other pain medications have not provided adequate relief or cannot be tolerated.

Historical Background of Tramadol(pain reliever)

Tramadol, a synthetic opioid analgesic medication, has a rich history dating back to the 1960s. Here’s a brief overview:

Early Development (1960s-1970s)

Tramadol was first developed in the 1960s by the German pharmaceutical company Grünenthal GmbH. At the time, the company was seeking to create a new analgesic medication that would be more effective and have fewer side effects than existing options.

Initial Approval and Marketing (1977)

It was initially approved in Germany in 1977 under the brand name Tramal. It was marketed as a non-opioid analgesic, despite its opioid-like properties.

International Expansion (1980s-1990s)

It gained popularity in the 1980s and 1990s as it became available in more countries, including the United States, where it was approved by the FDA in 1995.

Reclassification as a Controlled Substance (2014)

In 2014, the DEA reclassified tramadol as a Schedule IV controlled substance in the United States, citing concerns about its potential for abuse and addiction.

Present Day (2024s)

Today, tramadol is widely used to treat moderate to severe pain, including postoperative pain, chronic pain, cancer pain, back pain, and headaches.

Why Tramadol (pain reliever) is Essential

Effective Pain Relief: Tramadol provides rapid and effective pain relief, making it an ideal choice for acute pain management.
Versatility: It is used to treat a wide range of pain conditions, including postoperative pain, chronic pain, cancer pain, back pain, and headaches.
Availability: This is widely available in various formulations, including oral tablets, capsules, and injectables, making it accessible for different patient needs.
Affordability: Compared to other opioid analgesics, tramadol is generally more affordable, making it a cost-effective option for pain management.
Lower Risk of Dependence: It has a lower risk of dependence and abuse compared to other opioid analgesics, making it a safer choice for long-term pain management.

Mechanism of Action

Binding to opioid receptors: Tramadol attaches to mu-opioid receptors in the brain and spinal cord, reducing the transmission of pain signals.
Inhibiting serotonin and norepinephrine reuptake: It increases the levels of these neurotransmitters, which helps to reduce pain and enhance feelings of well-being.
Activating GABA receptors: It stimulates the activity of GABA (gamma-aminobutyric acid), a neurotransmitter that helps to calm down nerve activity and reduce pain.
Metabolism by CYP2D6 enzyme: Tramadol is converted into its active metabolite, (+)-O-desmethyl tramadol (M1), which is responsible for its analgesic effects.
Pain relief: Tramadol’s combination of opioid and non-opioid mechanisms provides effective pain relief for moderate to severe pain conditions.

Tramadol uses

Tramadol is a versatile medication that is used to treat various pain management. Here are some important uses of tramadol:

Acute Pain Management

It is commonly prescribed for the management of acute pain, including postoperative pain following surgical procedures such as orthopedic surgeries, dental procedures, and minor surgeries. Its fast onset of action and potent analgesic effects make it a valuable option for providing relief during the immediate postoperative period.

Chronic Pain Conditions

Tramadol is also used in the management of chronic pain conditions, particularly those with neuropathic components or where traditional opioids may be less effective or poorly tolerated. Conditions such as neuropathic pain, fibromyalgia, diabetic neuropathy, and osteoarthritis are among the chronic pain syndromes for which tramadol also prescribed.

Musculoskeletal Pain

Tramadol is effective in relieving musculoskeletal pain associated with conditions such as back pain, joint pain, musculoskeletal injuries, and rheumatoid arthritis. Its analgesic properties help alleviate discomfort and improve functional outcomes in individuals with musculoskeletal disorders.

Cancer Pain

In cancer patients, tramadol is used as a part of a multimodal analgesic regimen to manage cancer-related pain. It can provide relief from both nociceptive and neuropathic components of cancer pain, helping to improve quality of life and overall comfort in individuals undergoing cancer treatment or palliative care.

Neuropathic Pain

Tramadol’s dual mechanism of action, which includes inhibition of norepinephrine reuptake and modulation of serotonin levels, makes it effective for neuropathic pain conditions such as diabetic neuropathy, postherpetic neuralgia, and peripheral neuropathy. By targeting multiple pathways involved in neuropathic pain processing, tramadol can help alleviate symptoms and improve function in affected individuals.

Adjunctive Therapy in Multimodal Analgesia

It also used as a part of a multimodal analgesic approach, where it is combined with other analgesic agents such as nonsteroidal anti-inflammatory drugs (NSAIDs), acetaminophen, or adjuvant medications like gabapentin or pregabalin. This combination therapy aims to optimize pain relief while minimizing the use of high-dose opioids and reducing the risk of opioid-related side effects and complications.

Tramadol use in Pregnancy

Tramadol, a synthetic opioid analgesic, is generally not recommended for use during pregnancy, especially in the first trimester, due to potential risks to the developing fetus.
Risks Associated with Tramadol Use in Pregnancy:
Neonatal Opioid Withdrawal Syndrome (NOWS): Babies exposed to tramadol in the womb may experience withdrawal symptoms after birth.
Respiratory Depression: It can slow down the baby’s breathing, leading to respiratory depression.
Increased Risk of Birth Defects: Some studies suggest a link between tramadol use in early pregnancy and an increased risk of birth defects, such as heart defects and cleft palate.
Preterm Labor: It also increase the risk of preterm labor and delivery.
Fetal Growth Restriction: Tramadol use during pregnancy may lead to fetal growth restriction.

Dosage Information for Tramadol

Acute Pain Management

Adults (17 years or older): 50-100 mg orally every 4-6 hours as needed for pain
Maximum daily dose: 400 mg

Chronic Pain Conditions

Adults (18 years or older): 100 mg orally once a day (extended-release)
Maximum daily dose: 300 mg

Musculoskeletal Pain

Adults (17 years or older): 50-100 mg orally every 4-6 hours as needed for pain
Maximum daily dose: 400 mg

Cancer Pain

Adults (18 years or older): 100-300 mg orally once a day (extended-release)
Maximum daily dose: 300 mg

Neuropathic Pain

Adults (18 years or older): 100-300 mg orally once a day (extended-release)
Maximum daily dose: 300 mg

Adjunctive Therapy in Multimodal Analgesia

Adults (18 years or older): 50-100 mg orally every 4-6 hours as needed for pain
Maximum daily dose: 400 mg

Tramadol Side effects

Tramadol, like any medication, causes side effects. Here are some side effects associated with this medication:

Serious side effects

  • Possibly deadly breathing problems in both adults and children
  • Serious, possibly fatal health risks, such as extreme sleepiness, slowed or stopped breathing, coma and death
  • The risk of opioid misuse, abuse and addiction, and death
  • Accidental ingestion, overdose, death
  • Dangerous, complex drug interactions due to enzyme alterations
  • Severe allergy if you are allergic to tramadol or other opioids

Common side effects

  • Dizziness or vertigo
  • Nausea, vomiting
  • Constipation
  • Stomach pain, heartburn
  • Diarrhea
  • Headache
  • Dry mouth
  • Weakness or asthenia
  • Decreased appetite
  • Itching
  • Sweating
  • Tiredness, somnolence, drowsiness, sleepiness
  • Nervousness, anxiety, agitation

Other side effects

  • Seizures
  • Serotonin syndrome
  • Suicide or attempted suicide
  • Adrenal insufficiency
  • Severe hypotension
  • Abnormal heart rhythms
  • Severe hypersensitivity reactions

Tramadol interaction with other drugs

Tramadol interactions with other drugs can be dangerous and even life-threatening. Here are some detailed interactions to be aware of:

Opioid Analgesics: Concurrent use with other opioid analgesics can increase the risk of overdose and death.

Benzodiazepines: Associated use with benzodiazepines or other central nervous system (CNS) depressants can increase the risk of respiratory depression, sedation, and death.

Antidepressants:

  • SSRIs (Selective Serotonin Reuptake Inhibitors): Increased risk of serotonin syndrome, a potentially life-threatening condition.
  • SNRIs (Serotonin-Norepinephrine Reuptake Inhibitors): Increased risk of serotonin syndrome.
  • TCAs (Tricyclic Antidepressants): Increased risk of serotonin syndrome and increased tramadol levels.

Muscle Relaxants: Concomitant use with muscle relaxants can enhance sedative effects.

Antipsychotics: Concurrent use with antipsychotics can increase the risk of respiratory depression, sedation, and death.

Anti-Anxiety Medications: Concomitant use with anti-anxiety medications can enhance sedative effects.

Sleep Medications: Concomitant use with sleep medications can enhance sedative effects.

Carbamazepine: Reduced tramadol efficacy due to increased metabolism.

Quinidine: Increased tramadol levels due to inhibited metabolism.

Monoamine Oxidase Inhibitors (MAOIs): Increased risk of serotonin syndrome.

Selective Serotonin Reuptake Inhibitors (SSRIs): Increased risk of serotonin syndrome.

Antihistamines: Enhanced sedative effects.

Anticonvulsants: Increased risk of respiratory depression, sedation, and death.

Precautions and Warnings

While using Tramadol it is essential to be aware of certain warnings and precautions.

Warnings

  1. Addiction and Abuse: It has a high potential for abuse and addiction, which can lead to overdose and death.
  2. Respiratory Depression: It cause severe, possibly fatal, breathing problems, especially when starting the medication or increasing the dose.
  3. Opioid Overdose: Teach family members and caregivers how to recognize and treat opioid overdose, and have naloxone available.
  4. Pregnancy and Breastfeeding: Use tramadol during pregnancy only when clearly needed, and avoid using it for a long time or in high doses near the expected delivery date.
  5. Pediatric Use: Children under 12 years old should not use tramadol, and children between 12 and 18 years old should not use it after certain surgeries or if they are obese or have breathing problems.

Precautions

  1. Allergic Reactions: Inform your doctor if you are allergic to tramadol or have any other allergies.
  2. Medical History: Share your medical history, especially brain disorders, breathing problems, kidney or liver disease, diabetes, mental/mood disorders, and substance use disorders.
  3. Heart Rhythm: It cause QT prolongation, a condition affecting heart rhythm. Inform your doctor if you have heart problems or are taking drugs that may cause QT prolongation.
  4. Seizure Risk: It increase the risk of seizures, especially in patients with a history of seizure disorders.
  5. Serotonin Syndrome: Tramadol may increase the risk of serotonin syndrome when used with other serotonergic agents.

Tramadol: Brands Names and Globle Presence

Here are some Tramadol brand names available in Pakistan and globally, along with their manufacturers and country of origin:

Brands in Pakistan

  1. Tramalex (Getz Pharma, Pakistan)
  2. Tramjet (Hilton Pharma, Pakistan)
  3. Tramazac (Searle Company, Pakistan)
  4. Tramadin (Indus Pharma, Pakistan)
  5. Tram (Pharmawise, Pakistan)
  6. Tramol (Kanon Pharma, Pakistan)
  7. Tonoflex-P(Sami Pharma)
  8. Tramacet (Zafa Pharma, Pakistan)
  9. Tramundin (Unison Pharma, Pakistan)
  10. Dolotram (Sami Pharmaceuticals, Pakistan)

Global Presence

  1. Ultram (Johnson & Johnson, USA)
  2. Tramadol (Sandoz, Switzerland)
  3. Tramal (Grünenthal, Germany)
  4. Zydol (Grünenthal, Germany)
  5. Tramacet (Grünenthal, Germany)
  6. Ryzolt (Labopharm, Canada)
  7. Ultracet (Johnson & Johnson, USA)
  8. Conzip ( Vertical Pharmaceuticals, USA)

Frequently Asked Questions

Can you take tramadol with acetaminophen, ibuprofen, or aspirin?

Yes, it is safe for most people to take tramadol with acetaminophen, ibuprofen, or aspirin ¹ ² ³. Here are some things to keep in mind:
Tramadol and Acetaminophen: The combination of these two medications provides better pain relief than either medicine used alone, and in some cases, you may get relief with lower doses of each medicine.
Tramadol and Ibuprofen: Taking these medications together is safe and may provide additional pain relief. However, be aware that 800mg ibuprofen is a high dose that may cause gastrointestinal side effects such as abdominal pain or reflux if taken long term.
Tramadol and Aspirin: It is safe for adults to take tramadol with aspirin, but it is not recommended for children under 16 years old.

Is Tramadol safe in Pregnancy?

Tramadol is not safe to use during pregnancy, as it can cause life-threatening withdrawal symptoms in the newborn. While there is no conclusive evidence that tramadol increases the risk of miscarriage, birth defects, preterm delivery, or low birth weight, opioids in general may be associated with a small increased risk of birth defects.

Is Tramadol a MAOI?

Tramadol is not a traditional MAOI (Monoamine Oxidase Inhibitor), but it has some MAOI-like effects. As a synthetic opioid, it acts on the central nervous system to reduce pain, but it can also increase serotonin levels, leading to serotonin syndrome when combined with other serotonergic medications. It should not be used within 14 days of another MAOI or with food and beverages high in tyramine.

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