 Milnacipran, the first in a new class of anti-depressants, affects serotonin and noradrenaline levels without causing side effects
What makes Milnacipran different from the SSRI drugs like Prozac and SNRI antidepressant types like Effexor, is that Milnacipran affects two neurotransmitters - norepinephrine and serotonin - almost equally (a 3:1 norepinephrine to serotonin balance). In contrast an SNRI, tends to act much more on serotonin than norepinephrine, (Effexor has a 1:30 norepinephrine to serotonin ratio).
It is this essentially "equal" potency that makes Milnacipran a promising treatment for chronic pain conditions like Fibromyalgia and Lupus.
It is believed that the combination of Milnacipran's norepinephrine and serotonin enhancement action has an analgesic, (pain-killing) effect. The second generation, Tricyclic antidepressants (TCA's), like Amitriptyline (which has a 1.6:1 norepinephrine to serotonin balance), have a proven record in treating chronic pain. Unfortunately, the TCA medications are also known for having more negative side-effects than the SSRI and SNRI antidepressants which have followed them. It is hoped that the newer antidepressants like Milnacipran will be able to affect multiple pain mechanisms in a manner similar to that seen with some tricyclic antidepressants, but without the negative side effects of the TCA's.
Milnacipran not only inhibits the reuptake of Serotonin, it also has an action to inhibit the uptake of Noradrenaline. Both these factors have been shown to be efficacious in the treatment of depression.
However, most SSRIs have some particular unwelcome side effects. The most common being an increase in the prevalence of erectile dysfunction, or a decrease in libido (sex drive). These effects have not been noted with Milnacipran, which is why it has been receiving a lot of attention as a "new kind" of anti-depressant. In fact, Milnacipran appears to be as effective as the tri-cyclic anti-depressants whilst having fewer side effects than most SSRIs.
Fibromyalgia Trials: This trial is the first to evaluate Milnacipran as a potential treatment for Fibromyalgia Syndrome (FMS). FMS is a chronic pain syndrome that is estimated to affect 2-4% of the general population. The symptoms of FMS can be debilitating, and are characterized by chronic and widespread pain throughout the body, often accompanied by severe fatigue and poor sleep.
A preliminary analysis of the randomized, double blind, placebo-controlled, flexible dose escalation mono-therapy trial was conducted on 95 patients, or 76% of the total patients enrolled in the trial. A total of 125 patients are enrolled in the trial - the remaining 30 patients have recently completed the study. Patients were randomized to receive placebo or Milnacipran (either once or twice per day) for four weeks of dose escalation, followed by eight weeks of constant dose.
The study evaluated the efficacy and safety of Milnacipran for the treatment of pain and associated symptoms such as fatigue, depressed mood and sleep. Patients were asked to characterize their pain, fatigue, sleep and related symptoms several times each day on an electronic diary.
Milnacipran-treated patients randomized to the twice a day dosing group (BID) showed statistically significant improvements in pain compared to those who received placebo. Of the 95 patients that had completed the trial as of the date of this analysis, 87 percent of all Milnacipran-treated patients reported overall improvement, compared to 33 percent in the placebo group (p less than 0.001). Further, 36 percent of Milnacipran BID-treated patients reported at least a 50 percent reduction in pain intensity, compared to 9 percent of patients who received placebo, a difference that was statistically significant (p=0.030, intent to treat analysis). In addition, Milnacipran-treated patients showed significant improvements in fatigue and depressed mood.
"It is extraordinary to see such a significant improvement in symptoms in this patient population," said Dr. Daniel Clauw, Professor of Medicine, Division of Rheumatology; director, Center for Advancement of Clinical Research; and director, Chronic Pain and Fatigue Research Center, The University of Michigan.
"Milnacipran, a novel dual-acting reuptake inhibitor that acts on two key neurotransmitters in the human body, norepinephrine and serotonin, which are involved with the central modulation and processing of chronic pain, is distinguished from other dual reuptake inhibitors by its preference for norepinephrine reuptake inhibition over serotonin reuptake inhibition. Based on these preliminary results, Milnacipran appears to have the potential to relieve several of the symptoms associated with FMS, and perhaps other related Functional Somatic Syndromes."
Eighty-four percent of all Milnacipran patients escalated to the highest dose with no tolerability issues. The most common dose-related side effect reported by patients was nausea, particularly early in the study. Most adverse events were mild to moderate in intensity, and transient in duration.
Lupus Trials: Lupus is a chronic autoimmune disease in which the immune system turns against the body and harms healthy cells and tissues. Lupus, which is also considered a rheumatic (arthritic) disease, can affect many parts of the body including the joints, skin, kidneys, lungs, heart or brain. Some of the most common symptoms include extreme fatigue, painful or swollen joints, unexplained fever, skin rashes, and kidney problems.
Scientific evidence indicates that lupus is caused by a combination of genetic and environmental factors. Studies show that lupus runs in families, meaning that certain genes predispose you to the disease. Environmental triggers may include ultraviolet light, bacterial and viral infections, medications, diet and stress.
There are three major types of lupus:
Systemic Lupus Erythematosus is the most serious form of the disease. It is a chronic, inflammatory, multisystem disorder of the immune system that may affect parts of the body such as the joints, skin, kidneys, heart, lungs, blood vessels or brain.
Discoid Lupus primarily affects the skin. A red, raised rash may appear and become thick and scaly. Lesions usually occur on the face or other sun-exposed areas and may scar.
Drug-induced Lupus is caused by a small number of prescription medications. Usually when the medicine is stopped, the disease goes away. The most common drugs that can cause lupus are procainamide (for heart problems), hydralazine (for high blood pressure) and dilantin (for seizures).
Lupus is characterized by periods of increased or intensified disease activity, called flares. Some patients may have persistent disease activity without distinct flares. Understanding how to prevent flares and how to treat them when they do occur helps people with lupus maintain better health.
According to the National Institute of Health, nine out of ten people who have lupus are women. It often first appears during the childbearing years—ages 15 to 45. Lupus is three times more common in African American women than in Caucasian women, and is also more common in women of Hispanic, Asian, and Native American descent.
Treatments may differ, depending upon the person with lupus and the physician. There is, however, a general consensus on several forms of treatment:
Physical and emotional rest
Avoidance of, or protection from direct sunlight
Healthy diet
Prompt treatment of infections
Avoidance of known allergens and aggravating factors
Female patients must plan pregnancy for times when the disease is in remission
Medications most frequently used to control symptoms are nonsteroidal anti-inflammatory drugs (NSAIDs)
Antimalarials
Corticosteroids
Immunosuppressant (or cytotoxic drugs)
other medications may be necessary to control specific manifestations
Lupus is one of many autoimmune diseases that can cause widespread pain, extreme fatigue, and a host of other symptoms. Unlike Fibromyalgia and Chronic Fatigue; Lupus can be life-threatening, but it can also be quite mild. In Lupus your immune system can attack anything… any of the major organs including the kidneys, the heart, the lungs, the blood system and the brain. Milnacipran is proving to be very effective in helping with Lupus.
According to the clinical trials, one should begin to see the pain reduction benefit at about week number 8.
The phase II clinical trials in the US were recently completed and the results were very positive. No one dropped out of the trial because of side effects, which is virtually unheard of. Plus numerous rheumatologists who are involved in treating people with Fibromyalgia and Chronic Fatigue, say they just cannot wait until this medication is available. As professionals they feel the previous therapies they have offered their patients have met with limited success. It is wonderful that there is now a medication that promises to improve the quality of life of so many people.
Dosage: For depression is usually in the order of 25mg to 50mg daily, (maximum 100mg). For FMS and Lupus seek your physician's guidance.
Safety: Like most anti-depressants there are contraindications with other anti-depressants and MAO inhibiting drugs, these would include Gerovital-H3, Deprenyl and Manerix etc., therefore combined use is not advised, (unless under the guidance of a physician). Furthermore, we would not advise combination with other Serotonin or Noradrenaline enhancing agents such as Adrafinil, Modafinil, Paxil, Prozac, Yohimbine and Zoloft etc., (unless you are under the guidance of a physician).
Store in a dry place. Keep out of the reach of children.
Persons taking prescription medication and pregnant or lactating women should consult a physician before using this product. Long-term use of this product should be supervised and monitored by a health care professional.
Disclaimer: This product and its statements have not been evaluated by the FDA. This product is not intended to treat, cure or prevent any disease. The above information is provided under the supplying company's terms and conditions and should not replace the advice of your personal physician.
Restrictions: This product is not available for shipment to the EU
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