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Spine Medications

A. Non-Steroid Anti-Inflammatory Drugs (NSAIDS)

NSAIDS are a group of medications which help with inflammation and fevers. They do not contain a steroid and are therefore referred to as “non-steroid anti-inflammatories”. However they work similar to steroids by blocking “” (cyclooxygenase, called COX for short) in the body which are needed to produce another chemical called “”. Prostaglandin is a substance which causes inflammation and fevers. By blocking the COX receptor, the body cannot make as much Prostaglandin, and the inflammation or fever is reduced or eliminated. This is how NSAIDS work.

One side effect of blocking Prostaglandin is the fact that it protects the stomach. By blocking it, we do increase the risk of stomach bleeding and ulcers. NSAIDS can also cause us to bleed for longer than would be expected. Aspirin is a NSAID which can cause severe bleeding problems, depending on the dose taken. For that reason Aspirin is not commonly recommended as long-term anti-inflammatory.

NSAIDS are used by spine specialists to reduce inflammation in the spine. They are often used for mild to moderate pain by mouth and for moderate-severe pain by injection (see )

There are many NSAIDS medications on the market, some are over the counter. However, most have to be prescribed by a doctor. Here are some of the differences between the different NSAIDs:

  • The risk of bleeding
  • The risk of developing a stomach ulcer
  • The way they leave the body (elimination)
  • How strong (potent) they are
  • How long they work for (duration of action)

NSAIDS can help with pain and inflammation but also have potential side effects. A patient is not necessarily expected to have any of these side effects, but they are possible. Here are some of them:

  • Nausea, vomiting
  • Rash
  • Stomach bleeding
  • Kidney failure
  • Worsened bleeding after surgery or with trauma
  • Worsening asthma
  • Drowsiness, fatigue

Patients with Diabetes, Kidney disease, and asthma should be cautious when taking NSAIDS and should check with their doctor first.

There are many different NSAIDS available on the market today. Here are some of them:

  1. Aspirin

Aspirin is an NSAID which can cause significant bleeding, not just in the stomach but elsewhere in the body. Due to that it is generally not recommended for the treatment of spine pain for longer periods of time.

Low dose Aspirin (81mg) also called a “Baby Aspirin” is taken to prevent heart attacks. In this low dose, bleeding is less likely.

      2. Ibuprofen (Motrin, Advil)

Ibuprofen is a commonly used NSAID. It is available over-the-counter in a 200mg dose and in higher doses as a prescription drug. Ibuprofen rarely increases the risk of a stroke or heart attack. It is not known to be safe in pregnancy, but can be taken by breastfeeding mothers as it does not get into the breast milk. The maximum does of Ibuprofen for healthy younger adults is 3200 mg (milligrams) per day. High doses should be monitored by a physician.

      3. Naproxen Sodium (Naprosyn, Aleve, Anaprox)

Naproxen Sodium is available over–the-counter as a 220mg tablet. Stronger doses require a prescription. The maximum dose is 1000mg per day.

      4. Diclofenac (Voltaren, Cataflam)

Diclofenac is not available as an over-the-counter medication. The maximum daily dose is 200mg.

      5. Celecoxib (Celebrex)

Celecoxib is in the class of “COX-2” inhibitors. This class blocks a specific cyclooxygenase receptor (COX) called “COX-2”. By blocking this receptor specifically, Celecoxib is less likely to cause stomach irritation and bleeding. It is also less likely to interfere with blood clotting, unlike other NSAIDS. However, this class of NSAIDS has been shown to cause an increased risk of heart attacks in higher doses. Therefore the lowest effective dose should be taken.

Celecoxib is available as a 100mg and 200mg capsule. The recommended dose for most inflammatory spine problems is 100mg twice daily or 200mg one daily.

      6. Ketorolac (Toradol)

Ketorolac is available by mouth (orally), injected into muscle (intramuscular) and into a vein (intravenous). Compared to other NSAIDS it has a higher potency when given by injection. For that reason it can be very useful for moderate to severe pain, whereas other NSAIDS may only be helpful for mild to moderate pain. Due to its high risk of causing bleeding it should be limited to a 5 day course by mouth and 2 days by injection.

B. Steroid Anti-Inflammatory Drugs

  1. Prednisone

Prednisone is a commonly used steroid. When taken by mouth, it is converted to its active form (Prednisolone) in the liver. It can also be given into the muscle (intramuscular) or into a vein (intravenous). It is used for many different inflammatory conditions.

For spine conditions, steroids such as Prednisone are only recommended for short periods of time. An example would be pain from severe sciatica. Prednisone for spinal inflammation is typically given as a “taper dose” or “short course”. A “taper” is a method to give a large dose on the first day and then progressively less each day until stopping. (i.e. 40mg day 1, 30mg day 2, 20mg day 3, 10mg day 4, then stop). A “short” course is using the same dose each day for a short period of time (i.e. 20mg per day for 1 week).

However due to the many potential side effects of steroids, chronic use is not recommended. Here are some examples of side effects of Prednisone:

  1. Increased blood sugar levels, especially in Diabetes
  2. Trouble sleeping (insomnia)
  3. Increased appetite
  4. Mood swings
  5. Depression, mania
  6. Swelling of the face
  7. Bone thinning (Osteoporosis)
  8. Nausea, ulcers

      2. Dexamethasone (Decadron)

Dexamethasone is a very potent steroid which is available by mouth (orally), and by injection into muscle (intramuscular) and into a vein (intravenous). It is 6.6 times as potent as Prednisone.

Similar to Prednisone it is only recommended for very short periods of time for severe spine inflammation such as pain from severe sciatica. Due to its potency, courses of dexamethasone are shorter than Prednisone. It can be given as a “taper” or “short course”.

A “taper” is a short course of the medication starting atthe highest dose and then progressively less until gone (i.e. 20mg day 1, 10mg day 2, 5mg day 3, 2mg day 4, stop day 5). A “short course” is using the same dose each day for a short period (i.e. 10mg twice a day for 5 days).

Similar to other steroids, Dexamethasone has potential side effects which can be significant.

Here are some examples of side effects from Prednisone:

  1. Increased blood sugar levels, especially in Diabetes
  2. Trouble sleeping (insomnia)
  3. Increased appetite
  4. Mood swings
  5. Depression, mania
  6. Swelling of the face
  7. Bone thinning (Osteoporosis)
  8. Nausea, ulcers

      3. Methylprednisolone (Medrol, Solu-Medrol)

Methylprednisolone is available in pill form, and injectable. The injectable form can be used for injections into muscles, veins, and joints. Orally, Methylprednisolone is often given as a “Medrol Dose Pack”, or “Blister Pack”. This means it is prescribed as a “taper dose”. Patients start on the highest dose on day 1, less on day 2, and so on, until the medication is finished.

In intravenous form, Methylprednisolone is commonly used to treat spinal cord problems, such a paralysis after an injury. In this case it is given as early as possible after the injury to the spinal cord. Some data suggests this may be helpful in recovering some function of the spinal cord.

Methylprednisolone is also used as for injection into inflamed joints.

 

C. Muscle Relaxants

Muscle relaxants are a group of medications which are designed to decrease muscle tone of muscles of our skeleton.

Muscle relaxants can be grouped into 2 groups, “spasmolytics” and “neuromuscular blockers”.

“Spasmolytics” are muscle relaxants which act on the brain and spinal cord (centrally) and block nerve transmission signals to achieve muscle relaxation. “Neuromuscular blockers” work by blocking the signal between the nerve and the muscle.

“Spasmolytics” are the group of medications which are used for spine spasms. Since they all work on the brain and spinal cord, they have side effects. Here are some of them:

  1. Fatigue (sedation)
  2. Confusion
  3. Dry mouth
  4. Blurred vision
  5. Stomach ache, nausea, vomiting
  6. Rash

Here are some examples of the “spasmolytics” (work on the brain and spinal cord):

  1. Carisoprodol (SOMA)

Carisoprodol may be habit-forming. It is usually prescribed as 350mg every 8 hours as needed. It is one of the first muscle relaxants in the group of “spasmolytics” and was discovered in 1959. Like narcotic medications, tolerance can develop with this medication. In general, other non-habit forming muscle relaxants are preferred by many spine specialists.

      2. Cyclobenzaprine (Flexeril)

Cyclobenzaprine is the most studied muscle relaxant. Potential side effects are drowsiness, dry mouth, and dizziness amongst many others. However it is a potent muscle relaxant and can be useful for acute spasm, such as that from a disc herniation in the spine. Common doses are 10mg by mouth twice daily as needed.

      3. Methocarbamol (Robaxim)

Methocarbamol has a very low abuse potential. It tends to be better tolerated than Cyclobenzaprine. It is also available for injection. In this form it can be used intravenously to break a cycle of severe spasms. Methocarbamol is available as a 500mg and 750mg tablet, to be taken 3 times daily as needed.

      4. Metaxalone (Skelaxin)

Metaxolone has an overall low side effect profile and is well tolerated. It is available as an 800mg tablet to be taken 3 times daily as needed. It should be taken with food as more of the medicine is available in this way.

      5. Diazepam (Valium)

Diazepam can be used as a muscle relaxant for severe spine spasms. It is not in the group of muscle relaxants per se and has many potential side effects. However, it does have significant muscle relaxant properties. For that reason it is often used as a sedative or treatment for pain and anxiety. Diazepam is from a group of medications called “benzodiazepines”.

 

D. Pain Killers (analgesics)

  1. Non-Narcotic

a. Acetaminophen (Tylenol)

Acetaminophen is a pain medication used for mild pain. For more severe pain it is often taken in combination with NSAIDS or narcotic pain killers. Its action is not completely understood but appears similar to NSAIDS. However it does not have the same side effects such as bleeding and stomach ulcers. It is not an anti-inflammatory, but does reduce fevers.

Acetaminophen is usually active in the body about 11 minutes after taking it, and will last from 1-4 hours depending on the dose. The daily recommended dose is not to exceed 4,000 mg, but should be reduced in the elderly and those with liver disease.

Tylenol is broken down by the liver. When taken as an overdose or in high doses for longer periods of time it can cause liver failure. In fact Acetaminophen is the number one cause of liver failure.

b. Tramadol (Ultram)

Tramadol is used for the treatment of moderate pain. It is a synthetic, non-narcotic medication, meaning it is made artificially, rather than something that occurs naturally, such as Morphine. It comes in pill form and is injectable.

Tramadol relieves pain by stimulating a specific narcotic receptor just like narcotics. However unlike narcotics, it only works on one receptor (mu-receptor), the receptor which blocks pain. Narcotics on the contrary, work on many different narcotic receptors, some of which cause euphoria, nausea or constipation.

Tramadol also works similar to some antidepressant medications by increasing the levels of serotonin and norepinephrine in the brain. These two substances transmit nerve information. Increasing these chemicals in the brain can help with anxiety and depression.

Tramadol does have the potential for addiction and withdrawal, usually less so than narcotic pain medications.

Here are some potential side effects of Tramadol:

  • Nausea, constipation
  • Dizziness
  • Drowsiness
  • Sweating, itching

The most commonly available dose of Tramadol is a 50mg pill. The maximum daily dose is 400mg for the pill form Tramadol also comes in combination with Acetaminophen (Tylenol). This form contains 37.5mg Tramadol and 325mg of Acetaminophen (Ultracet).

      2. Narcotics (opioids)

The word “narcotic” comes from an ancient Greek word “narcos” which means “numb”. Narcotics are also called “opioids” due to the fact that most are derived from “opium” which is naturally occurring in poppy seeds. Opioids are amongst the oldest known drugs in human history dating back thousands of years. Opioids reduce pain by binding to specific “opioid receptors” in the brain and spinal cord. They stimulate these receptors which can block pain, but also cause other consequences. Some of these “opioid receptors” can cause the following side effects:

- Drowsiness, confusion

- Nausea, vomiting, constipation

- Itching

- Dry mouth

There are many other potential side effects. In high doses, especially when combined with other medications or alcohol, opioids can lead to death by depressing our ability to breathe (respiratory depression).

Two very common issues with opioids especially when taking them for longer periods of time are addiction and tolerance:                                                                                                

Addiction is the psychological dependence on an opioid. That often means that a patient is taking the medication for the euphoria or relaxation they may experience rather than pain relief. These patients may go through great length to obtain the medication. Tolerance means that over time it may take more medication to achieve the same amount of relief. For instance, taking two pills a day now, may require 3 pills a day in a few weeks or months in order to feel the same amount of pain relief.

The government has divided opioids into different categories (schedules). They range from Schedule I through V. Schedule I drugs are for investigational use only. Commonly prescribed opioids are divided based on their potency and abuse potential into schedules II-V, II being the strongest.

Here are some examples of commonly prescribed opioids:

  1. Codeine

Codeine is relatively weak opioid, used for mild to moderate pain, as well as cough suppression. Codeine is most commonly prescribed in pill form, but also comes as a liquid. The liquid form is commonly used for cough suppression.

Codeine is available by itself as well as in combination with Acetaminophen (Tylenol with codeine). 30mg and 60mg strength are the most commonly available.

      2. Hydrocodone (Vicodin, Lortab, Lorcet, Norco)

Hydrocodone is typically used for moderate pain as well as cough suppression.It is more potent than codeine.

In the U.S. it is only available in combination with Acetaminophen or Ibuprofen. Due to this combination, high doses of this drug are limited not just by the Hydrocodone content, but even more so by the amount of Acetaminophen or Ibuprofen. The most common combination of Hydrocodone is with Acetaminophen which makes high doses a risk for liver failure to occur. It is available in pill and liquid form, but not injectable.

Hydrocodone has a high abuse potential. Along with Oxycodone it is one of the most commonly abused prescription drug in the U.S..

      3. Oxycodone (Percocet, Percodan, Oxy-IR, Oxycontin)

Oxycodone is commonly prescribed for moderate to severe pain. It is available by itself or in combination, most commonly with Acetaminophen, but is also available in combination with anti-inflammatories. Due to the common combinations of Oxycodone with other drugs such as Acetaminophen, toxicity can occur from both the Oxycodone as well as the Acetaminophen when taken in high doses. A common risk is liver failure.

Oxycodone is only available in pill form in the U.S.

Oxycontin is the long-release (time release) preparation of Oxycodone.

Similar to Hydrocodone, Oxycodone has a high risk of addiction and tolerance.

      4. Hydromorphone (Dilaudid)

Hydromorphone is a direct derivative of Morphine and is used for moderate to severe pain. It is available without combining it with other medications such as Acetaminophen. Hdyromorphone is available in pill form and by injection. In injection form it is often used to control pain after surgery. It is highly potent, and has similar risks for addiction and tolerance as other strong opioids.

      5. Morphine (MS-Contin, MSIR, Avinza, Kadian, Roxanol)

Morphine is used to treat severe pain conditions. Morphine is the gold-standard opioid drug. Other opioids are compared to it to measure their potency and other properties.

Morphine is available in pill form and as an injectable. In the U.S., it is typically prescribed by itself without other added drugs. As an injectable it is often used to control pain after surgery.

Morphine has a high potential for addiction and tolerance.

      6. Methadone

Methadone is synthetic drug, and unlike most opioids is not derived from poppy seeds. However it does work on the opioid receptors and therefore is included here among them. It is widely used to treat the withdrawal from addiction. However it does have pain relieving properties and can be used to treat moderate to severe chronic pain. Methadone may also have some nerve pain relieving properties which other opioids are not very effective in treating.

      7. Fentanyl Patches (Duragesic)

"Transdermal" Fentanly is a slow release patch placed on the skin. Initially the drug is absorbed through the skin and forms a "depot" under the skin. From the "depot", the medication is released into the blood stream.

E. Nerve Pain Medications

  1. Pregabalin (Lyrica)

Pregabalin is a drug from the category of anti-seizure medications (anti-convulsants).

For spine pain it is used for its properties of relieving nerve pain (neuropathic pain). It is also FDA approved for the treatment of Fibromyalgia. It is not a narcotic and has very little if any abuse potential. This medication is often slowly increased over time until it is most effective for nerve pain. Pregabalin should not be stopped abruptly when taken in high doses or for longer periods of time. It may have to be tapered slowly.

The most common side effects are dizziness and drowsiness.

It is most commonly available in 50mg, 75mg and 100mg pills. The maximum daily dose is 600mg.

      2. Gabapentin (Neurontin)

Gabapentin is a drug in the group of anti-seizure medications (anticonvulsants), but is often used for the treatment of nerve pain (neuropathic pain).

The most common side effects are drowsiness, dizziness, fatigue and weight gain.

Similar to Pregabalin (Lyrica), Gabapentin often has to be slowly increased to achieve its maximum benefit for nerve pain. No maximum dose of Gabapentin is known, however side effects tend to worsen somewhat with higher doses. Gabapentin should not be discontinued abruptly, especially when taken in high doses or for longer periods of time. It must be slowly tapered before stopping.

F. Anti-Anxiety Medications

Anti-anxiety medications are sometimes used for spine pain patients who have associated anxiety. Here are some of these medications:

  1. Benzodiazepines

These drugs are often used in low doses for short periods of time (weeks) to help with anxiety related to back pain. In higher doses these medications can cause significant sedation. If used for longer periods of time patients can experience symptoms of dependence and withdrawal. Some of these medications also have muscle relaxation properties.

a. Diazepam (Valium) [see above]

Acts quickly (within 20-30 minutes) and last for moderate length of time (6-8 hours, depending on dose). However, Diazepam can take 7-10 days to completely eliminated by the body.

b. Alprazolam (Xanax)

Acts quickly (within 10-20 minutes, depending on dose) and lasts for shorter periods of time (4-6 hours)

c. Lorazepam (Ativan)

Takes longer to take effect than Diazepam and Alprazolam (30-60 minutes), but can last for a longer period of time (8-12 hours, depending on dose)

G. Selective Serotonin Reuptake Inhibitors

SSRI medications increase the level of Serotonin in the brain. Serotonin is a nerve transmitter chemical. Increasing the levels of Serotonin in the brain can help with anxiety, depression and nerve pain (neuropathic pain). In spine care, this group of medications is often used for their nerve pain relieving properties.

Here are some examples of SRI’s:

  1. Paroxetin (Paxil)
  2. Sertraline (Zoloft)
  3. Citalopram (Celexa)

 

  1. Pregabalin (Lyrica)

Pregabalin is in the group of anti-seizure medications. Apart from its nerve pain relieving properties it also has good anti-anxiety properties.

H. Antidepressants

  1. Tricyclic Antidepressants (TCA)

TCA’s are older style antidepressants, first introduced in the 1950’s. As antidepressants they have largely been replaced by newer medications. However, they are still used for relieve of nerve pain for spine conditions. It is not known what the exact nerve pain relieving properties are.

TCA’s can have significant side effects when first starting on one of these medications. The most common ones are drowsiness and dry mouth. For that reason they are often taken in small doses at night. Here are some TCA’s available by prescription:

  1. Amitriptyline (Elavil)
  2. Nortriptyline (Pamelor)
  3. Doxepin (Sinequan)

 

      2. Selective Serotonin Reuptake Inhibitors - SSRI (increase levels of Serotonin)

SSRI medications increase the level of Serotonin in the brain. Serotonin is a nerve transmitter chemical. Increasing the levels of Serotonin in the brain can help with anxiety, depression and nerve pain (neuropathic pain). In spine care, this group of medications is often used for their nerve pain relieving properties.

Here are some examples of SRI’s:

  1. Paroxetin (Paxil)
  2. Sertraline (Zoloft)
  3. Citalopram (Celexa)

I. Topical Analgesics (medications applied to the skin)

Topical analgesics can be divided into these groups:

  1. Rubefacients

This group of medications increases the blood flow to the skin and makes the skin red (“rubor”).This can help absorb the medication better. Here are some Rubefacients:

      2. Medications

    • Salicylates such as Methyl Salicylate
      • Examples are Bengay and Icy Hot which also contain Menthol
      • They produce heat which is useful for muscle pain and spasms

 

  • Capsaicin which is a pepper extract used for nerve pain
    • It works by lowering a chemical (substance P) which transmits pain information to the spinal cord
  • Menthol

      3. Herbs

  • Gloves
  • Garlic
  • Ginger
  • Eucalyptus

      4. Topical Non-Steroid Anti-Inflammatory medications (NSAIDS)

Some NSAIDS are available as topical medications. These drugs are often used for muscle pain, sprains and strains, as well as arthritis pain. They come in gels, sprays and foams. They do require a prescription.

Since these medications are absorbed in a small area of the body, they typically do not have the same side effects as taking them by mouth.

Here are some examples of topical NSAIDS:

  1. Diclofenac (Voltaren) gel
  2. Ketoprofen gel
  3. Piroxicam gel

 

      5. Topical Local Anesthetics

Topical local anesthetics are used to numb a painful area of the skin. They can be useful for nerve pain.

Here are some examples:

  1. Lidocaine patch 5% (Lidoderm)
  2. Lidocaine cream 4% (LidoCream)
  3. Lidocaine/Prilocaine cream (EMLA)

G. Insomnia Medications (Sleep Agents)

Sleep disturbances are common in patients with spine pain. While the goal often is to control the pain which would help with sleep, sometimes sleep agents are used to regulate the sleep cycle of spine patients. Some of these medications can have significant side effects including dependency, withdrawal and rebound insomnia. They are generally recommended for short-term use.

Here are some examples of Sleep Agents:

  1. Zolpidem (Ambien, Ambien CR)

Usually takes effect within 10-20 minutes and lasts about 6-8 hours, depending on dose

      2. Zaleplon (Sonata)

Usually takes about 30 minutes for effect and lasts 4-6 hours, depending on dose

      3. Eszopiclone (Lunesta)

Usually takes 15-30 minutes to take effect and can last 5-7 hours, depending on dose.

 

H. Smoking Cessation (stopping smoking)

Smoking has a direct relationship to back pain. Some Pain Physicians help their patients with medications to stop smoking.

Here are some examples:

  1. Nicotene Replacement Therapy

These are FDA approved medications which release low levels of nicotine into the body to help with the withdrawal symptoms when patients stop smoking. Smokers are 50-70% more likely to stop smoking with the help of these medications:

  1. Transdermal Nicotine (patches)
  2. Nicotine Gum
  3. Nicotine Spray
  4. Nicotine Lozengers
  5. Nicotine Inhalers

 

      2. Antidepressants

There is one FDA approved medication in this class:

  1. Buprion (Zyban)

Buprion (FDA approved) works by increasing the levels of certain chemicals (dopamine, norepinephrine) in the brain. This helps with the cravings and withdrawal symptoms from Nicotine. Buprion doubles the chance of quitting smoking when used for at least 3 months.

      2. Nortriptyline

This medication is in the group of It seems to be similar in effectiveness to Buprion, but has a higher likelihood to cause sedation and dry mouth.

 

      3. Nicotine Receptor Agonists (Medication which works on the receptor for Nicotine)

  1. Varenicline Tartrate (Chantix)

This medication (FDA approved) works on the body’s receptors for nicotine which helps with the cravings and withdrawal from Nicotine. There is some evidence that this medication may be more effective than Buprion or Nicotine Replacement Therapy.

      4. Sympatholytic Medications

This group of medications lowers the tone of a certain part of our nervous system (sympathetic nervous system).

  1. Clonidine

This medication helps with the withdrawal from Nicotine. It may have side effects such as drowsiness and dry mouth. Patients taking this medication are twice as likely to stop smoking than if they took placebo.

 

I. Anti-Obesity Medications

Since obesity and spine pain appear to be linked, some Spine Specialists will prescribe medications for weight loss.

Currently there is only one FDA approved medication for weight loss in the United States:

  1. Orlistat (Xenical)

This medication reduces the absorption of fat in the intestines.

      2. Lorcaserin (Belviq)

This drug was recently approved by the FDA. It works on a receptor in the brain to make people eat less and feel fuller.