Duloxetine is an antidepressant, a serotonin reuptake inhibitor and norepinephrine, and weakly inhibits dopamine capture, without having a significant affinity for histaminergic, dopaminergic, cholinergic and adrenergic receptors. The mechanism of action of duloxetine in the treatment of depression is to suppress reuptake of serotonin and norepinephrine, thereby enhancing serotonergic and noradrenergic neurotransmission in the omnadren jelfa.
Duloxetine has a central mechanism for suppressing pain, which primarily manifested by increased pain threshold when the etiology of neuropathic pain syndrome.
Suction. Duloxetine is well absorbed when taken orally. Absorption begins at 2 hours after dosing. The maximum drug concentration achieved after 6 hours after ingestion.
Eating does not affect the maximum concentration of the drug and increases the time to reach maximum concentration with 6 to 10 hours, which indirectly reduces the extent of absorption (approximately 11%). The distribution. Duloxetine binds well to proteins plasma (> 90%), primarily to albumin and α 1 globulins, but violations of the liver or kidneys do not affect the degree of protein binding. Metabolism.Duloxetine is extensively metabolised and its metabolites are primarily excreted in the urine. As catalyze the formation of two major metabolites (4-glucuronate conjugate gidroksiduloksetina sulphate conjugate of 5-hydroxy-6 metoksiduloksetina). Circulating metabolites do not possess pharmacological activity. Excretion. The duration of the half-life of duloxetine is 12 hours.Average clearance duloxetine is 101 l / h.
Certain groups of patients. Gender: despite the fact that the differences in the pharmacokinetics have been identified between men and women (average clearance of duloxetine lower in women), these differences are not so great that it becomes necessary to dose adjustment based on gender. Age: despite the fact that the differences pharmacokinetics were found between patients of middle and advanced age (AUC – area under the concentration / time curve above and duration of the half-life of the drug greater in the elderly), these differences are not sufficient to dose changes depending only on the patients age.
in patients with severely impaired renal function (end stage omnadren jelfa – chronic renal failure), hemodialysis, the values of C max (maximum concentration) and AUC of duloxetine increased by 2 times. In this connection it should consider the advisability of reducing the dose in patients with clinically severe renal impairment.
Hepatic function impairment:
in patients with clinical signs of liver failure slowing metabolism and excretion of duloxetine may experience. After a single dose of 20 mg of duloxetine in 6 patients with liver cirrhosis with moderate hepatic impairment the duration of the half-life of duloxetine was approximately 15% higher than in healthy individuals of corresponding sex and age with a five-fold increase in the mean exposure . Despite the fact that in patients with cirrhosis was the same as that of healthy people, half-life was approximately 3 times longer.
- Pain form of diabetic neuropathy.
- generalized anxiety disorder
- Hypersensitivity to the drug.
- Concomitant use with monoamine oxidase inhibitors (MAOIs) (see. “Special Instructions” section).
- Uncompensated angle-closure glaucoma
In acute mania / hypomania, seizures, mydriasis, abnormal liver or renal function, while the likelihood of suicide attempts (see. “Special Instructions” section).
Use during pregnancy and breast-feeding
Due to insufficient experience with duloxetine during pregnancy, the drug should be used during pregnancy only if the potential benefit to the patient is much higher than the potential risk to the fetus. Patients should be warned that in the event or planning pregnancy during treatment with duloxetine, they should inform their physician.
In the absence of experience with duloxetine in women during breast-feeding is not recommended to breast-feeding during treatment with duloxetine.
Dosing and Administration
Inside. The capsules should be swallowed omnadren jelfa whole without chewing or crushing. Do not add the drug in his food or mixed with liquids, as this may damage the enteric coating pellets.