Archive for May, 2008
Friday, May 30th, 2008
Prior to the development of drug-based muscle relaxants, people have been using natural remedies to alleviate muscle spasms and soothe stiff joints. These natural muscle relaxants are often herbs and common plants that provide the same effect as drug-based relaxants without the compromise of possibly severe side effects. Some of these popular remedies for stiff joints and muscle spasms can be found right in one’s garden or in community health stores.
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Tuesday, May 27th, 2008
As sedatives, benzodiazepines can relieve the symptoms of anxiety and effectively promote sleep for most people, with very few side effects.
Benzodiazepines have also proven to be very effective in the treatment of panic disorders.
Several different benzodiazepines are very effective in preventing panic attacks.
This class of drugs may also be used for effective long-term treatment of anxiety, although this raises concerns about dependency.
Some physicians have also used benzodiazepines to treat other disorders, such as borderline personality disorder; this has been with some positive results.
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Dependence
It is almost universally accepted that long term use of this class of drugs will lead to dependence. Some withdrawal symptoms may include:
Common withdrawal symptoms may include:
Abdominal pains and cramping
Anxiety
Breathing difficulties
Blurred vision
Changes in perception
Depression
Dizziness
Extreme lethargy
Flu-like symptoms
Heavy limbs
Heart palpitations
Hypersensitivity to light
Indigestion
Insomnia
Irritability
Lack of concentration
Lack of co-ordination
Loss of balance
Loss of memory
Muscular aches and pains
Nausea
Nightmares
Panic attacks
Rapid mood changes
Restlessness
Severe headaches
Shaking
Sore eyes
Tightness in the chest
Because of the severity of some symptoms and the high risk of dependence, make sure that you speak to a doctor before taking any benzodiazepines. Also speak to a doctor or pharmacist for more information on dangers and symptoms of benzodiazepine withdrawal.
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Monday, May 26th, 2008
When taken orally, benzodiazepines are absorbed by the stomach and small intestine, and they are metabolized by the liver. Benzodiazepines tend to be highly fat soluble and accumulate in the patient’s fatty tissue.
The benzodiazepines operate in the brain, affecting control of consciousness, emotional reactions, memory, coordination, and concentration.
The benzodiazepines do this by enhancing the action of the neurotransmitter “GABA” (Gamma Amino Butyric Acid). Neurotransmitters are chemicals which enable the brain cells to transmit impulses from one to another. They are released from brain cells by electrical signals. Once released, the neurotransmitters signal inhibition or excitation of neighboring brain cells.
GABA is an inhibitory neurotransmitter, which means that it is a chemical that enables brain cells to slow or calm things down. Benzodiazepines increase the efficiency of GABA, thus causing greater inhibition of signals, or calming.
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Saturday, May 24th, 2008
Benzodiazepines are a very large class of drugs that are characterized as having six primary effects:
Anxiolytic Effect
Sedative Effect
Anticonvulsant Effect
Hypnotic Effect
Amnestic Effect
Muscle Relaxant Effect
Each different benzodiazepine exhibits varying degrees of these and other, more secondary effects; for example, one drug may exhibit stronger sedative effects, while another may have a stronger Anxiolytic effect.
These drugs (also known as “Benzo’s” in the parlance of seasoned users), have also been described as a group of “minor tranquilizers”, which many physicians believe to be a misrepresentation, considering the strength of modern benzodiazepines.
Doctors generally prescribe Benzodiazepines for anxiety conditions, particularly panic attacks, and generalized anxiety disorder (GAD).
Occasionally, benzo’s are also prescribed for seizure disorders, such as epilepsy, or for insomnia and other sleep problems, such as restless leg syndrome (RLS). Benzodiazepines are also quite frequently prescribed as muscle relaxants.
Valium, Xanax, and Alprazolam are among the most common benzodiazepines prescribed in the United States today. Valium has become less common over the past 15 years.
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Friday, May 23rd, 2008
Fibromyalgia features a long list of drug treatment options, however, currently there are no drugs approved by the FDA for treating fibromyalgia, although a few such drugs are in development. Doctors treat fibromyalgia with a variety of drugs developed and approved for other purposes.
On June 21, 2007, Lyrica (pregabalin capsules CV) were approved by the U.S. Food and Drug Administration (FDA) for the treatment of fibromyalgia. The approval of Lyrica was long-awaited because it’s the first medicine that is FDA-approved to treat fibromyalgia. More fibromyalgia drugs are in development. Doctors also treat fibromyalgia with a variety of drugs developed and approved for other purposes. Below are some of the most commonly used categories of fibromyalgia medications:
Analgesics
Analgesics are painkillers. They range from over-the-counter drugs, such as acetaminophen, to prescription drugs, such as tramadol, and even stronger narcotic drugs.
For a subset of people with fibromyalgia, narcotic medications are prescribed for severe muscle pain. However, there is no solid evidence showing that narcotics actually work to treat the chronic pain of fibromyalgia, and most doctors hesitate to prescribe them for long-term use because of the potential that the person taking them will become dependent on them.
NSAIDs
NSAIDs (nonsteroidal anti-inflammatory drugs) are used to treat inflammation. Although inflammation is not a symptom of fibromyalgia, NSAIDs also relieve pain. NSAIDs include:
* aspirin
* ibuprofen
* naproxen
NSAIDs work by inhibiting prostaglandins, which play a role in pain and inflammation. These drugs, some of which are available over-the-counter, may help ease the muscle aches of fibromyalgia. They may also relieve menstrual cramps and the headaches often associated with fibromyalgia.
Antidepressants
Perhaps the most useful medications for fibromyalgia are several in the antidepressant class. Antidepressants elevate the levels of certain chemicals in the brain, including serotonin and norepinephrine. Low levels of these chemicals are associated not only with depression, but also with pain and fatigue. Increasing the levels of these chemicals can reduce pain in people who have fibromyalgia. Doctors prescribe several types of antidepressants for people with fibromyalgia.
Tricyclic Antidepressants
When taken at bedtime in dosages lower than those used to treat depression, tricyclic antidepressants can help promote restorative sleep in people with fibromyalgia. They also can relax painful muscles and heighten the effects of the body’s natural pain-killing substances called endorphins.
Tricyclic antidepressants have been around for almost half a century. Some examples of tricyclic medications used to treat fibromyalgia include:
* amitriptyline
* cyclobenzaprine
* doxepin
* nortriptyline
Selective Serotonin Reuptake Inhibitors (SSRIs)
If a tricyclic antidepressant fails to bring relief, doctors sometimes prescribe a newer type of antidepressant called a SSRI. As with tricyclics, doctors usually prescribe these for people with fibromyalgia in lower dosages than are used to treat depression. By promoting the release of serotonin, these drugs may reduce fatigue and some other symptoms associated with fibromyalgia. The group of SSRIs includes:
* fluoxetine
* paroxetine
* sertraline
SSRIs may be prescribed along with a tricyclic antidepressant. Doctors rarely prescribe SSRIs alone. Because they make people feel more energetic, they also interfere with sleep, which often is already a problem for people with fibromyalgia.
Cymbalta (duloxetine) is a selective serotonin and norepinephrine reuptake inhibitor (SSNRI) that is also showing promise.
Mixed Reuptake Inhibitors
Some newer antidepressants raise levels of both serotonin and norepinephrine, and are therefore called mixed reuptake inhibitors. Examples of these drugs include:
* venlafaxine
* nefazodone
Researchers are actively studying the efficacy of these drugs in treating fibromyalgia.
Benzodiazepines
Benzodiazepines help some people with fibromyalgia by relaxing tense, painful muscles and stabilizing the erratic brain waves that can interfere with deep sleep. Benzodiazepines also can relieve the symptoms of restless legs syndrome, which is common among people with fibromyalgia. Restless legs syndrome is characterized by unpleasant sensations in the legs as well as twitching, particularly at night. Because of the potential for addiction, doctors usually prescribe benzodiazepines only for people who have not responded to other therapies. Benzodiazepines include:
* clonazepam
* diazepam
* triazolam
* temazepam
Other Medications For Fibromyalgia
Doctors may prescribe other medications, depending on a person’s specific symptoms or fibromyalgia-related conditions. For example:
* Tegaserod and alosetron are FDA approved for the treatment of irritable bowel syndrome.
* Gabapentin is being studied as a treatment for fibromyalgia.
* Pregabalin (Lyrica) is the first medicine that is FDA-approved to treat fibromyalgia.
* Modafinil may help with fatigue.
* Sodium oxybate may help with excessive sleepiness.
Symptom-Specific Drugs
Other symptom-specific drugs include:
* various headache remedies
* sleep aids such as:
o zolpidem
o eszopiclone
o ramelteon
o zaleplon
* muscle relaxants
such as:
o carisoprodol (soma)
o metaxalone
o methocarbamol
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Thursday, May 22nd, 2008
Are The Newer Arthritis Drugs Always The Better Choice?
Arthritis drugs have long been considered the “traditional” treatment option. Since individual response to drugs can vary and because potential side effects and adverse reactions are also a factor, finding the most effective combination of arthritis drugs can be a more difficult process than one would expect. Patients should become knowledgeable about the various arthritis drugs so they can make decisions with their doctor.
NSAIDs / COX-2 Inhibitors
NSAIDs (nonsteroidal anti-inflammatory drugs) are among the most commonly prescribed and widely used arthritis drugs. There are three types of NSAIDs: salicylates (both acetylated, such as aspirin, and nonacetylated such as (Disalcid) salsalate, (Trilisate) choline magnesium trisalicylate and (Doan’s Pills, Novasal) magnesium salicylate), the traditional NSAIDs, and COX-2 selective inhibitors.
NSAIDs work by blocking the activity of the enzyme, cyclooxygenase, also known as COX. Research has revealed that there are two forms, known as COX-1 and COX-2. NSAIDs affect both forms. COX-1 is involved in maintaining healthy tissue, while COX-2 is involved in the inflammation pathway. COX-2 selective inhibitors became a new subset of NSAIDs born of this research.
Traditional NSAIDs Include:
* Ansaid (Flurbiprofen)
* Arthrotec (Diclofenac/Misoprostol)
* Cataflam (Diclofenac potassium)
* Clinoril (Sulindac)
* Daypro (Oxaprozin)
* Dolobid (Diflunisal)
* Feldene (Piroxicam)
* Ibuprofen (Motrin, Advil)
* Indocin (Indomethacin)
* Ketoprofen (Orudis, Oruvail)
* Lodine (Etodolac)
* Meclomen (Meclofenamate)
* Mobic (Meloxicam)
* Nalfon (Fenoprofen)
* Naproxen (Naprosyn, Aleve)
* Ponstel (Mefanamic Acid)
* Relafen (Nabumetone)
* Tolectin (Tolmetin)
* Voltaren (Dicolfenac Sodium)
COX-2 Inhibitors include:
* Celebrex (Celecoxib)
* Vioxx (Rofecoxib)(no longer on market)
* Bextra (Valdecoxib)(no longer on market)
DMARDs
DMARDs (Disease-Modifying Anti-Rheumatic Drugs) have also been labeled “slow-acting anti-rheumatic drugs” (because they take weeks or months to work) and “second-line agents”. However, research has shown the effectiveness of DMARDs in the treatment of rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis and the importance of early, aggressive treatment with these drugs. For some, these drugs can stop disease progression and halt joint damage.
DMARDs Include:
* Arava (Leflunomide)
* Auranofin (Ridaura, Oral Gold)
* Azulfidine (Sulfasalazine)
* Mycophenolate (CellCept)
* Myochrysine (Injectable Gold)
* Cyclosporine (Neoral,Sandimmune)
* Cytoxan (Cyclophosphamide)
* Imuran (Azathioprine)
* Leukeran (Chlorambucil)
* Methotrexate (Rheumatrex, Trexall)
* Minocin (Minocycline)
* Penicillamine (Cuprimine, Depen)
* Plaquenil (Hydroxychloroquine)
Corticosteroids (Steroids)
Corticosteroids or glucocorticoids, often called “steroids”, are potent drugs which can reduce swelling and inflammation quickly. These drugs are closely related to cortisol, a hormone produced on the cortex of the adrenal glands. They are prescribed in widely varying doses depending on the condition and goal of treatment. Used to control inflammation of the joints and organs in diseases such as rheumatoid arthritis, lupus, polymyalgia rheumatica, vasculitis, it has been determined that the potential for serious side effects increases at high doses or with longterm use. Doctors can prescribe short-term, high-dose intravenous steroids in some situations, or give shots or injections with drugs such as Triamcinolone (Kenalog) locally into a specific joint for relief.
Corticosteroids Include:
* Betamethasone (Celestone)
* Cortisone (Cortone)
* Dexamethasone (Decadron)
* Hydrocortisone (Cortef)
* Methylprednisolone (Medrol)
* Prednisolone (Prelone)
* Prednisone (Deltasone)
Analgesics (Pain Killers)
Analgesics are pain relieving drugs. Controlling pain is a vital part of treating arthritis. However, unlike NSAIDs, analgesics do not relieve inflammation. Acetaminophen (Tylenol) is the most commonly used analgesic. Narcotic analgesic drugs can also be prescribed for more severe pain.
Narcotics Include:
* Codeine (Tylenol#3)
* Darvocet (Propoxyphene/Acetaminophen)
* Darvon (Propoxyphene)
* Duragesic (Fentanyl Skin Patch)
* Hydromorphone (Palladone)
* (no longer on market) Morphine Sulphate (MS Contin)
* Oxycodone (OxyContin)
* Percocet (Oxycodone/Acetaminophen)
* Percodan ( Oxycodone/ Aspirin)
* Talwin NX (Pentazocine/Naloxone)
* Ultracet (Tramadol/Acetaminophen)
* Ultram (Tramadol)
* Vicodin (Hydrocodone/Acetaminophen)
Biologic Response Modifiers (Biologics)
Biologic Response Modifiers (BRMs) stimulate or restore the ability of the immune system to fight disease or infection. BRMs are drugs derived from living sources as opposed to being synthesized chemicals.
Enbrel (etanercept), Remicade (infliximab), and Humira (adalimumab), target TNF-alpha, one of the most important cytokines involved in rheumatoid arthritis. BRMs which bind to TNF-alpha, render it inactive, interfering with inflammatory activity and ultimately decreasing joint damage.
Kineret (anakinra), also a BRM, is considered an IL-1 antagonist. Kineret is the first selective blocker of interleukin-1 (IL-1), a protein which is found in excess in rheumatoid arthritis patients.
By blocking IL-1, Kineret inhibits inflammation and pain associated with rheumatoid arthritis. Kineret can be used alone, or in combination with DMARDs other than anti-TNF drugs.
Orencia (abatacept) is the first T-cell co-stimulation modulator approved for the treatment of rheumatoid arthritis.
Rituxan, the world’s best-selling cancer drug, was FDA approved 3/1/2006 to be used in combination with methotrexate to treat rheumatoid arthritis by reducing the signs and symptoms in adult patients who have moderately-to-severely active rheumatoid arthritis and have failed one or more anti-TNF drugs. Rituxan is the first treatment for rheumatoid arthritis which selectively targets the CD20-positive B-cells.
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Wednesday, May 21st, 2008
When are muscle relaxers appropriately prescribed for arthritis patients? How do muscle relaxers work? Are muscle relaxers a short-term treatment or can they be part of a long-term maintenance regimen for arthritis patients to control aches and pains?
Short-Term Treatment Vs. Long-Term Maintenance
Muscle relaxers are often prescribed as a temporary treatment for patients who get muscular pain, typically affecting the spine.
In some patients who have fibromyalgia, these drugs are used daily to help them with chronic muscle spasm or as a way to improve sleep. Some examples include:
# Robaxin (methocarbamol)
# Soma (carisoprodol)
# Flexeril (cyclobenzaprine)
# Skelaxin (metaxalone)
Of these medications, Skelaxin is the least likely to cause drowsiness making it more compatible with day time use.
Improve Sleep & Pain Relief
Although not FDA approved for long term use, rheumatologists will often prescribe Flexeril nightly on a routine basis to increase stage 4 sleep so patients feel more refreshed in the morning.
In addition to helping sleep in fibromyalgia patients, Flexeril is also felt to help with pain separate from the pain relief fibromyalgia patients get with better sleep.
The Central Nervous System
While marketed as a muscle relaxant, Flexeril is similar in its mechanism of action to some of the tricyclic anti-depresssants such as Elavil (amitriptyline).
In fact, the muscle relaxants in general, are felt to exert their beneficial effects on the central nervous system (brain and spinal cord), as opposed to a direct effect on skeletal muscle.
Doctors treat fibromyalgia with a variety of medications developed and approved for other purposes.More attention needs to be paid to the often dismissed symptom of sleep disruption in people with arthritis. Interrupted sleep is equally as problematic as joint pain and limited mobility for many people with arthritis. Poor quality of sleep and waking pain can also create a vicious cycle affecting mood and
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Tuesday, May 20th, 2008
Sedation is the most commonly reported adverse effect of muscle relaxant medications. These drugs should be used with caution in patients driving motor vehicles or operating heavy machinery. More absolute contraindications do exist to the use of carisoprodol, cyclobenzaprine, and diazepam. Rare idiosyncratic reactions have also been reported to carisoprodol and its metabolites such as meprobamate. Benzodiazepines have potential for abuse and their use should be avoided. By initially prescribing muscle relaxants at bedtime, the physician might take advantage of their sedative effects and minimize daytime drowsiness.
These agents have been found to be effective when used either alone or in combination with an analgesic/anti-inflammatory agent within seven days of symptom onset. The prescribing physician should monitor patients receiving these medications and tailor dosages in an attempt to minimize the drowsiness and sedation often associated with their use. The use of benzodiazepines does not appear to offer any significant benefit to patients experiencing acute low back pain. Further research is needed before the role of baclofen and dantrolene sodium in the treatment of muscle spasm of local origin can be more clearly defined.
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Monday, May 19th, 2008
Muscle spasm of local origin needs to be clinically differentiated from spasticity and sustained muscle contraction in the setting of the central nervous system (CNS) and upper motor neuron injury. Baclofen and dantrolene sodium are two agents whose use is indicated in the setting of spasticity of CNS etiology. Dantrolene sodium is of particular interest, as its mechanism of action is purely at the muscular level where it serves to inhibit the release of calcium form the sarcoplasmic reticulum.
Casale studied the effectiveness of dantrolene sodium, 25-mg daily, in the treatment of low back pain and found patients to demonstrate significant improvements in visual analogue scores, pain behavior, and electromyographic (EMG) evaluations of “antalgic reflex motor unit firing,” when compared with the placebo group. The findings of this study are interesting in that they demonstrate improvement secondary to a pure muscle relaxant, which does not possess other outside anti-nociceptive properties.
Baclofen is a derivative of gamma-aminobutryic acid (GABA) and is believed to inhibit mono and polysynaptic reflexes at the spinal level. Treatment with baclofen was compared to placebo in a double blind, randomized study of 200 patients with acute low back pain. Patients with initially severe discomfort were found to benefit from baclofen, 30- to 80-mg daily, on days four and ten of follow up. Forty-nine percent of treatment patients complained of sleepiness, 38% of nausea, and 17% discontinued treatment.
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Saturday, May 17th, 2008
In an attempt to determine the mechanism of action of carisoprodol (Soma) in the treatment of low back pain, a double blind study was carried out comparing its effectiveness to that of a sedative control, butabarbital (a sedative), and a placebo in the treatment of 48 laborers with acute lumbar pain. Carisoprodol was found to be significantly more effective in providing both subjective pain relief and objective improvements in range of motion when evaluated by finger to floor testing. The results of this study suggest that the effects of carisoprodol are not secondary to its sedative effects alone.
In 1989, Basmajian compared the effectiveness of cyclobenzaprine (Flexeril) alone with diflunisal, placebo, and a combination of cyclobenzaprine and diflunisal in the treatment of acute low back pain and spasm. During the ten-day study period, the combined treatment group demonstrated significantly superior improvements in global ratings on day four, but not on day two or seven. This study suggested some effectiveness of combined analgesic and muscle relaxant therapy when utilized early in the initial week of pain onset.
Borenstein compared the effects of combined cyclobenzaprine and naproxen (Naprosyn) with naproxen alone and also found combination therapy to be superior in reducing tenderness, spasm, and range of motion in patients presenting with ten days or less of low back pain and spasm. Adverse effects, predominantly drowsiness, were noted in 12 of 20 in the combined group and only four of 20 treated with naproxen alone.
Cyclobenzaprine and carisoprodol were compared in the treatment of patients with acute thoracolumbar pain and spasm rated moderate to severe and of no longer than seven days duration. Both drugs were found to be effective, without significant differences between the treatment groups. Significant improvements were noted in physician rated mobility and in patients’ visual analogue scores on follow up days four and eight. While 60% of patients experienced adverse effects in the form of drowsiness or fatigue, these differences were not significantly different between groups, and only eight percent of patients from each group discontinued treatment.
Baratta found cyclobenzaprine, 10-mg t.i.d. (three times per day), superior to placebo in a randomized, double blind study of 120 patients with acute low back pain presenting within five days of symptom onset. Significant improvement was noted in range of motion, tenderness to palpation, and pain scores on follow up days two through nine. Sixty percent of treatment group patients reported drowsiness or dizziness compared with 25% of those in the placebo group.
In an earlier study, diazepam (Valium) was found to offer no significant subjective or objective benefit, when compared to placebo, in patients treated for low back pain. Carisoprodol was found to be superior to diazepam in the treatment of patients with “at least moderately severe” low back pain and spasm of no longer than seven days duration. In this study, the overall incidence of adverse reactions was higher in the diazepam treated group but was not of statistical significance.
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