Tramadol

Tramadol is an opioid-like painkiller that mitigates moderate to moderately severe pain. Unlike opioids like Morphine, codeine, and others, Tramadol has a different chemical structure. Nevertheless, it has an affinity for the opioid receptors in the brain.

An opioid painkiller is a more powerful pain medication compared to other prescription and OTC pain medications. Opioid medications are also known as narcotics.

Tramadol acts on specific sites in the brain, and alters the way your brain perceives pain. Specifically, Tramadol acts on receptors called opioid receptors. Studies have also shown that Tramadol exerts its pain-relieving effects by blocking the reuptake of brain chemicals such as serotonin and norepinephrine (also called noradrenaline).

Only oral forms of Tramadol are available, which include extended release tablet and capsule, suspension, disintegrating tablet, and normal tablet. Tramadol 50mg and 100mg are the commonly available strengths of the tablet form. The extended release preparations come in various strengths such as 100mg, 250mg, 200mg, and 300mg.

Tramadol may be used alone or combined with other less potent, non-narcotic pain medications like acetaminophen. The combination product is found to have enhanced pain-relieving effect compared to any of the single medications.

Both the intended effects and side effects of Tramadol depend on its level in the bloodstream. Therefore, different dosage forms have variable onset and duration of action, dosing frequency, and associated side effects.

Learn everything you can about Tramadol from your doctor and pharmacist before starting treatment.

Knowing in advance will help to minimize the occurrence of side effects while optimizing the treatment outcomes.

• Unlike other opiates, Tramadol acts in a dual manner to relieve pain. Firstly, it acts directly on the opioid receptors in the central nervous system (CNS) and alters your response to the pain. Secondly, it also increases the concentration of key brain chemicals, serotonin, and norepinephrine, in the brain. Both these actions work in a synergistic manner to provide better pain relief.
• Tramadol is as potent as codeine with regards to its pain-relieving property and has 10% the potency of morphine.
• The most common Tramadol side effects are constipation, dizziness, drowsiness, nausea, and vomiting.
• The abuse potential of Tramadol is lower than other narcotic pain medications. However, this does not mean you cannot get addicted to it.
• Major and potentially serious Tramadol side effects include decreased heart rate, respiration, and blood pressure. Therefore if you have a history of or ongoing problems with respiration and heartbeat, you need to inform your doctor before taking Tramadol.

Many people wonder if Tramadol is a narcotic or an opiate.

Tramadol is a narcotic. You may also call Tramadol an opioid painkiller. Before you learn what an opiate or narcotic is, you should know about the differences between the two similar-sounding terms: opioids and opiates.

There have been different opinions in the past regarding the definitions of opioids and opiates. However, these terms have been adequately defined and the widely-accepted definitions are given below.

Nevertheless, you may use these terms interchangeably while in the non-technical periphery.

Opioid: The term “Opioid” is a representative of all the derivatives of opium, the natural source of medications like morphine and codeine. In the past, the use of this term was limited to only synthetic derivatives.

But now, opioids cover all the opioid compounds that may be natural, synthetic, or semi-synthetic. In fact, the term is now more inclined towards the way these chemicals bind to the opioid receptors in the brain, rather than the source itself. In simple terms, you can call a substance an opioid if it binds to the opioid receptors in the brain.

Opiate: Medical professionals use the term “Opiate” to refer to a specific drug that shows biological effect similar to that of morphine. In essence, “opiate” is a more specific term compared to opioid. Nevertheless, you may use these terms interchangeably while keeping in mind that some differences still exist.

Types of Opioids

• Natural Opioids: These are extracted from the opium poppy and include morphine and codeine.
• Synthetic Opioids: These compounds are not structurally related to morphine or other natural opioid but exhibit similar pharmacological actions. Examples include Methadone, Buprenorphine, Tramadol, and Fentanyl.
• Semi-synthetic opioids: Examples include Hydrocodone, Hydromorphone, Oxycodone and Oxymorphone. These compounds are structurally similar to natural opioids.
• Endogenous Opioids: Also called endorphins, these substances are naturally produced in the body and act on the opioid receptors.

Note: Categorization of Tramadol as a semi-synthetic opioid has also been observed in some cases.

Tramadol or its combination is suitable for both short-term (acute) and long-term (chronic) pain management.

Tramadol is used for relief of moderate to severely moderate pain associated with:

• Surgery: Tramadol is useful in the management of postoperative pain which is acute in nature.
• Cancer: Cancer pain is a chronic debilitating condition that runs for a longer duration.
• Osteoarthritis: Tramadol may be useful in treating pain due to osteoarthritis, joint pain, and stiffness due to aging or other factors.
• Neuropathic pain: Also called nerve pain, this is a chronic type of pain that arises due to injury to the nerve cells in the brain. Neuropathic pain is a result of incorrect impulses reaching the pain centers from the damaged nerves.

In addition to the conditions mentioned above, Tramadol may also be used for conditions other than mentioned in the label or medication guide.

Your doctor, after assessing the risks and benefits of use, may prescribe Tramadol for other conditions too. For example, your doctor may recommend Tramadol for headache.

Tramadol dosage can vary depending on your medical condition, the prescribed dosage form, and your response to the drug. If you are responding well to the supplied dosage, you may not need the increased dosage. Likewise, doctors also practice a gradual Tramadol dosage increment to lower the incidence of adverse effects and measure your response more accurately.

In any case, the daily Tramadol dosage should not exceed 400 mg. For patients above 75 years old, the maximum daily dose is 300 mg.

Because Tramadol is a very powerful medication, you need to follow your doctor’s instructions strictly. Doing so will prevent a number of adverse effects and may also help to lower the risk of dependence.

If you are using Tramadol 50 mg immediate-release tablet or capsule, you should take it every 4 to 6 hours depending on the condition and need for pain relief.

If you are taking the extended-release formulation, you should take it every 12-24 hours.

In any case, never take more than the recommended dosage, more frequently, or for a longer duration than recommended by your doctor.

While Tramadol dosage varies depending on several factors, the normal dosage pattern is as follows.

For immediate-release tablet

• Adult Dosage: For patients aged 18 years to 64 years, the initial daily dose is 25 mg in the morning.
• Depending on your response, your doctor may increase the dose gradually in the following pattern:
  • Add 25 mg to your current dose every 3 days until the total dose reaches 100 mg per day. If you can tolerate the increased dose, add 50 mg to the current dose every 3 days till the maximum daily dose reaches 400 mg.

For maintenance therapy, a single dose of Tramadol 50 mg - 100 mg every 4-6 hours is recommended.

For extended-release tablet or capsule

• Adult Dosage (who are not on therapy with the immediate-release Tramadol preparation): For patients aged 18 years to 64 years, the initial dose is 100 mg once a day.
• Depending on your response, your doctor may increase the dose gradually in the following pattern:
  • Add 100 mg to your current dose every 5 days till the maximum daily dose reaches 300 mg.
• Adult Dosage (who are currently on therapy with immediate-release Tramadol preparation): For patients aged 18 years to 64 years, the initial dose is based on the dosage of the immediate-release preparation. Depending on your response, your doctor may slowly increase the dose every 5 days till the maximum daily dose reaches 300 mg.

Note: The above-mentioned doses are intended for adults who otherwise have no other health problems or are not taking other medications. Discuss with your doctor to understand Tramadol dosage in individuals aged more than 64 years. The use of Tramadol in children below 18 years is not recommended.

Factors Affecting Tramadol Dosage

Apart from pain severity and response to the drug, there are various other patient characteristics and drug formulation factors that influence Tramadol dosage. These include:

• Age: Generally, aging causes a reduction in the functional ability of the liver and kidneys. The liver is the major organ that breaks down a drug and the kidneys flush the drug out of the body. Therefore, seniors may have to take lower doses of Tramadol.
• Liver function: Impaired liver function due to a disease or natural causes may warrant a reduced Tramadol dosage in the affected persons.
• Kidney function: When your kidneys are not working at their best, you may have to take a lower dose of Tramadol.
• Respiratory function: Tramadol is known to slow down breathing rate. If you have any breathing problems due to asthma, chronic obstructive pulmonary disease (COPD), or other conditions, consult your doctor if you need a dose reduction or complete avoidance of Tramadol.
• History of head injury or mental disorders: Talk to your doctor if a current or past head injury symptoms such as pressure inside the head is exacerbated by Tramadol.
• Substance addiction: Tramadol carries a certain risk of addiction and can become habit-forming after continuous use. Therefore, if you struggled with addiction in the past or have an addiction problem, talk to your doctor without any hesitation.

Tramadol 50 mg Immediate-Release Tablet and Tramadol 100 mg Extended-Release Tablet

Keep in mind that there are fundamental differences between the immediate-release and extended-release formulations.

Immediate-release tablets and capsules are conventional dosage forms that release the active drug right after ingestion. Devoid of any release modifications, these formulations offer rapid absorption and relatively faster drug effects.

On the contrary, the extended-release formulations have benefits of modified drug release that offers better patient compliance. In addition, the dosing frequency with such formulations is at least half of that of the immediate-release formulation.

You should not chew, crush or break the extended Tramadol tablet. If you do so, the tablet will lose its release characteristics and a higher dose may be released unintentionally.

Tramadol side effects can range from symptoms as simple as abdominal pain to serious ones like loss of consciousness, irregular heartbeat, and severe respiratory depression.

The following are the side effects that have been reported with the use of Tramadol.

Common Tramadol side effects

• Upset stomach, pain in the stomach
• Constipation or diarrhea
• Restlessness
• Anxiety
• Lightheadedness
• Cough
• Dizziness and drowsiness
• Dryness of mouth
• Emotional emptiness or sadness
• Abnormal sensation of cold or warmth
• Fever
• Headache
• Burning sensation in the chest
• Reduced hunger
• Feeling irritated without a cause
• Itchy skin
• Pain in the joint, muscles or throat
• Inability to enjoy the activities that were previously enjoyable
• Apathy
• Weakness
• Nausea
• Nervousness
• Red skin on the face, neck, and arms
• Increased nasal secretion or congested nose
• Excessive sleepiness
• Excessive sweating
• Inability to focus

Rare Tramadol side effects

• Abnormal dreams
• Pain in the back, whole body or visceral organs like urinary bladder
• Blood in the urine
• Difficulty passing urine
• Skin irritation and formation of blisters
• Red skin
• Cold and moist skin
• Problems with hearing
• Symptoms of cold or flu
• Mental confusion
• Cough often accompanied by mucus
• Decreased sex drive or libido
• Concentration problems
• Congested ear or discharge from the ear
• Earache
• Balance problems
• Feeling abnormally well or excited
• Feeling ill or discomfort
• Severe throbbing headache
• Changes in voice or complete loss of voice
• Erectile dysfunction
• Inflamed and painful joints
• Muscle twitching
• Congested nose
• Excessive sweating at night
• Tender eyes or areas around the eyes
• Swollen extremities
• Chest discomfort
• Loss of sleep
• Breathing difficulties
• Changes in weight

The aforementioned Tramadol side effects are not serious in nature and tend to go away as your body becomes habituated to the drug.

However, if any of these symptoms persist, worsen, or cause significant trouble, you need to consult your doctor right away.

Tramadol side effects that require immediate medical attention

In addition, if you experience any of the following symptoms while taking Tramadol, consult your doctor immediately.

• Severe abdominal distension or bloating
• Unusual touch sensation
• Skin blisters
• Bloody or pale urine
• Problem passing urine
• Elevated blood pressure
• Vision problems like blurred vision
• Balance problems
• Chest discomfort
• Feeling of excessive warmth or cold
• Seizures
• Excessive dizziness
• Loss of consciousness
• Rapid and irregular heart rhythm
• Increased urinary frequency
• Failure to memorize objects, places or date
• Tingling sensations in the face or limbs
• Body pain including pain in the calves
• Radiating body pain that often leads to back pain
• Bluish discoloration of the limbs
• Periodic fever
• Hallucinations, both auditory and visual
• Rapid shallow breathing
• Excessive sweating
• Shakiness and tremors
• Loss of pulsation in the legs or pulses too weak to feel
• Yellowish skin or portion of the eyes which is normally white

Certain medications, supplements, and food items, when taken concomitantly with Tramadol, may alter its effects or cause other health problems. This is when a drug interaction is said to occur.

Therefore, you should avoid taking certain prescription and OTC medications, supplements, or food items while taking Tramadol.

Don’t take Tramadol with:

• Alcohol: Alcohol potentiates the sedative actions of Tramadol causing a dangerous drop in blood pressure, heart rate, and respiration.
• Carbamazepine: Carbamazepine reduces the effects of Tramadol and using these two medications together may make you more prone to convulsions.
• Antidepressants: Using Tramadol with antidepressants such as fluoxetine, paroxetine, citalopram, duloxetine, etc. can result in a serious rise in serotonin levels in the brain. This condition is called Serotonin Syndrome and is characterized by symptoms such as rapid heart rhythm, restlessness, elevated body temperature, nausea, and vomiting.
• Selegiline, Phenelzine, Isocarboxazid and other drugs of the class “Monoamine Oxidase Inhibitors (MAOIs)”: Such concomitant use can also cause Serotonin Syndrome.
• Lithium: Lithium is used to treat Bipolar disorder. Tramadol and Lithium, when used together, may cause Serotonin Syndrome.
• Sumatriptan or other similar medications: Your risk of Serotonin Syndrome is significantly raised when you take Tramadol with any of these drugs to treat migraine and cluster headache.
• St. John’s Wort: This widely used herbal product for depression may also cause Serotonin Syndrome when used concomitantly with Tramadol.
• Chlorpromazine and other antipsychotic agents: Do not take Tramadol if you are already taking Chlorpromazine or other antipsychotic agents. If you do so, you may experience severely reduced breathing, heartbeat and blood pressure.
• Other opioid pain medications, Digoxin, and Warfarin.
• Antibiotics such as rifampin (used in the treatment of Tuberculosis), erythromycin, and telithromycin.
• Antifungal medications such as Ketoconazole.
• Antiviral agents such as Indinavir, and Darunavir.
• Medications that treat problems with heart rhythms, such as Amiodarone.

Note: Every individual is uniquely different and there are always a few chances of exceptions. Taking this into consideration, it’s not always possible to include every individual case of drug interaction. Therefore, you should consult your doctor prior to using any drug, especially when your condition demands the use of more than one medication at a time.

Being a member of the opioid class of medications, Tramadol carries a significant risk of abuse, physical dependence, and subsequent addiction. Therefore, careful use of opioid medications is recommended.

Long-term use can lead to Tramadol withdrawal symptoms if the patient ceases Tramadol treatment.

According to the Drug Enforcement Administration (DEA), Tramadol is a Schedule IV chemical. This means that the abuse potential of Tramadol is lower than that of other narcotics such as heroin, hydrocodone, hydromorphone, methadone, fentanyl, and other opioids in Schedule I, II and III.

Recent data shows addiction may develop after continuous use for more than a few weeks or months.

Accidental or deliberate overdose of Tramadol can be fatal if the person fails to receive prompt medical care. Tramadol overdose is a medical emergency.

While many symptoms of overdose may overlap with other side effects, you need to take care of other factors such as suicidal tendency or mental state of the patient, signs that the patient has taken an excessive amount of the drug, mental status of the patient, and other relevant information.

If you notice any of the following symptoms of Tramadol overdose, seek emergency medical help.

• Loss of consciousness or severely impaired consciousness
• Delayed or even absence of response to stimuli
• Labored breathing
• Loss of muscle tone
• Severe dizziness or drowsiness
• Severely constricted pupils
• Slowed heart rhythm
• Abnormal physical weakness or lethargy

The pregnancy category of Tramadol is C, which means your doctor may prescribe it if the potential benefits outweigh the risks. Nonetheless, special precautions and watchful treatment are always recommended..

Inform your doctor if you are pregnant or planning to conceive.

Lactation

There is a possibility that the infant may be exposed to Tramadol through breast milk. If you are breastfeeding, consult your doctor to know if using Tramadol is safe for the infant.