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The active ingredient Duloxetine is a selective serotonin-norepinephrine reuptake inhibitor (SSNRI – English “selective serotonin noradrenaline reuptake inhibitors”). It is used to treat depression, anxiety disorders, incontinence and diabetic polyneuropathy (neuropathy in diabetes). In the USA, the active ingredient for the treatment of fibromyalgia is allowed, but not for the treatment of incontinence. Here you can read everything worth knowing about Duloxetine: action, application and side effects
How Duloxetine works
nerve cells (neurons) in the brain communicate by using messengers (neurotransmitters) to each other: where a cell filled certain neurotransmitters, which then from the next cell by docking points (receptors) are perceived. Because while the next cell can be either inhibited or excited (depending on the receptor and neurotransmitters) and a cell usually connections (synapses) has to many other neurons, thereby creating a highly complex network, which is only understood in the broad guidelines.
It has been shown that certain messenger substances usually cause a certain effect. So it comes with serotonin, commonly referred to as the “happiness hormone”, in low concentrations to depression, in high concentrations to psychosis and delusions. Noradrenaline hand, is a excitatory neurotransmitter, which is responsible for the activation of certain brain areas.
To the nerve cells to communicate with one another to be able to control exactly which neurotransmitters takes emitting neuron also continually returned to the same. Thus, the signal to the next cell is limited in time. Inhibits you this recovery, as indicated by the administration with Duloxetine, the neurotransmitter stay longer on the receptors of the next neuron and thereby act more. A lack of serotonin and norepinephrine, which often manifests itself as depression or anxiety may be so fixed or positively affected.
The analgesic properties of Duloxetine in the treatment of diabetic neuropathy and fibromyalgia arise from the excitation of pain-inhibiting pathways. As a result, especially on sensitive a pain threshold to normal. Likewise, a reinforced closing of the urethral sphincter is caused due to increased stimulation of serotonin and norepinephrine by Duloxetine system, resulting in stress incontinence can be treated.
Up, degradation and excretion of Duloxetine
After taking the drug Duloxetine through the intestine is absorbed into the blood. After six hours, one can measure the highest blood levels of Duloxetine, wherein the drug only to about half reaches the systemic circulation, since it is already partially dismantled immediately after shooting in the liver. About the bloodstream of Duloxetine then reaches the brain. The ineffective degradation products are average excreted within twelve hours halfway through the kidneys into the urine.
When is Duloxetine used?
The active ingredient Duloxetine is approved for the treatment of:
- depression (so-called Major Depression)
- generalized anxiety disorders
- Diabetic Peripheral Neuropathic Pain
- urinary stress incontinence in women
The use of Duloxetine for pain relief in fibromyalgia is happening in Germany “off-label”, ie outside the scope of accreditation.
The treatment with Duloxetine is usually long-term, however, should be reviewed at regular intervals, whether the dose needs to be adjusted or the therapy is still needed.
How Duloxetine is administered
The active ingredient Duloxetine is taken in the form of capsules containing enteric pellets and release the active ingredient only in the intestine. Depending on the field single to be taken twice a day for 30 to 60 milligrams of Duloxetine. The maximum daily dose is 120 milligrams. Better compatibility has begun treatment with a low dose and then gradually increased to the required final dose.
The capsule is taken with or without meals with a glass of water. When dysphagia or diet by the probe Duloxetine pellets can also be taken suspended in water, however, may be chewed in any case.
To end the treatment the Duloxetine dose should be reduced slowly (so-called “tapering off” of the dosage), otherwise there may be serious side effects occur.
What are the side effects of Duloxetine?
Duloxetine side effects are usually amplified at the beginning of treatment and better with time. With more than ten percent of patients experience side effects like, drowsiness, nausea and dry mouth.
Approximately one in ten to one hundred patients reported decreased appetite, insomnia, and cramps, weight loss and urinary retention.
What should be considered when taking Duloxetine?
The reduction of Duloxetine in the liver via certain enzymes (cytochrome P450 1A2 and 2D6) that degrade even more drugs. Are these used concomitantly, there may be increased or decreased blood levels of each active substance. This applies, for example antidepressants such as fLuvoxamine, Amitriptyline, Imipramine and desipramine, remedy for overactive bladder such as tolterodine and agents for treating psychoses such as schizophrenia and Risperidone.
Smoking build Duloxetine faster than Non smoking.
drugs that increase serotonin concentration in the brain, should not be combined with Duloxetine, because it can cause a life-threatening serotonin syndrome otherwise. Among the relevant medicines include antidepressants of type MAOIs (such as moclobemide or tranylcypromine), other antidepressants, St. John’s wort preparations, migraine drugs (such as Sumatriptan and naratriptan), strong painkillers (opioids such as tramadol, fentanyl and pethidine) and serotonin precursors such as tryptophan and 5-Hydroxytryptophan (5-HTP).
In the combination of Duloxetine with anticoagulants such as warfarin, warfarin and aspirin / acetylsalicylic acid, the blood clotting time may change, which is why these should be closely monitored. Eventually, the dosage of the anticoagulant should be adjusted.
Like many other antidepressants can Duloxetine lead to an increased risk of suicide, particularly among young people. For this reason, Duloxetine has been approved at least 18 years and should not be used or only under medical supervision in patients with such passion.
Patients with impaired hepatic or renal function is recommended a reduced dose of Duloxetine.
Duloxetine should not be taken during pregnancy and breast-feeding because it may harm the child.
How to obtain drugs with Duloxetine
preparations with Duloxetine are prescription in each dose and for each application.
Since when Duloxetine is known?
The antidepressant Duloxetine has been developed by scientists from the pharmaceutical company Eli Lilly and Company and 1986 applied for a patent, which issued 1990 levels. The Year 2004 was granted in the US, later in the same year and then in Germany. Early 2014 ran out the patent. Since then, several generics came with the drug Duloxetine on the market.