Active Substance: Amitriptyline
US Brand: Elavil
Indian (Generic) Brand: Amitone
Form release: blister 10 tabs
Shipping time: 9 – 18 days
Despite the availability of BZRAs and the development of safer compounds within the category, low-dose sedating antidepressants represent an increasingly used modality for the management of insomnia. Specifically trazodone, and secondarily doxepin, mirtazapine, and amitriptyline, are being used for the treatment of insomnia even in the absence of a depressive disorder. There has been much speculation as to the increased use of these medications for the management of insomnia given that their use for their primary indication, treatment of depression, is declining due to safety-toxicity concerns. Although the BZRAs produce their sleep-promoting effects via the GABAA receptor, the mechanism of action of the low-dose sedating antidepressants is not fully understood. For the tricyclic antidepressants, their antihistaminic (H1) activity is critical. The role of their anticholinergic activity in the modulation of sleep has not been made clear. Trazodone is a mild inhibitor of serotonin reuptake, and also has antagonistic action at the alpha 1 and alpha 2 adrenoreceptors.
There have been several hypotheses proposed for the use of low-dose sedating antidepressants: Insomnia patients typically also have depression; perceived safety at “lower” doses; availability of cheaper generics; nonschedule status; and the absence of quantity limits.
It inhibits the reuptake of the neurotransmitters (norepinephrine, serotonin) presynaptic nerve terminals of neurons, causing the accumulation of monoamines in the synaptic cleft and postsynaptic strengthens impulses. With prolonged use reduces the functional activity (desensitization), beta-adrenergic, and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, impaired in depressive states. Does m-choline and histamine receptors of the central nervous system.
Application of the substance Amitriptyline
Depression different etiology (especially with severe anxiety and agitation), including: endogenous, involutional, reactive, neurotic, with organic brain damage, drug; schizophrenic psychoses, mixed emotional disorders, behavioral disorders, bulimia nervosa, child enuresis (excluding children with hypotonia of the bladder), chronic pain (neurogenic nature), migraine prevention.
In a joint application of ethanol and drugs which depress the central nervous system (including the others. Antidepressants, barbiturates, benzadiazepinov and general anesthetics) may significantly increased inhibitory action on CNS, respiratory depression and hypotensive effect. Increases sensitivity to drinks containing ethanol.
Increases anticholinergic effect of drugs with anticholinergic activity (eg, phenothiazine derivatives, antiparkinsonian drugs, amantadine, atropine, biperiden, antihistamine drugs), which increases the risk of side effects (CNS, vision, bowel and bladder). In a joint application with holinoblokatorami, phenothiazine derivatives and benzodiazepines – mutual enhancement of the sedative and central anticholinergic effects and increased risk of seizures (lowering the threshold for seizure activity); phenothiazine derivatives, may further increase the risk of neuroleptic malignant syndrome.
In a joint application with antiepileptic drugs may increase depressant effects on the central nervous system, lowering the threshold for seizure activity (when used in high doses) and a decrease in the efficiency of the latter.
In a joint application with antihistamine drugs, clonidine – increased inhibitory action on the central nervous system; with atropine – increases the risk of paralytic ileus; with drugs, cause extrapyramidal reactions – increasing frequency and severity of extrapyramidal effects.
With simultaneous use of amitriptyline and indirect anticoagulants (coumarin derivatives or indadiona) may increase the anticoagulant activity of the latter. Amitriptyline may enhance the depression caused by glucocorticosteroids (GCS). Medicines for the treatment of hyperthyroidism increases the risk of agranulocytosis. Reduces the effectiveness of phenytoin and alpha-blockers.
Inhibitors of microsomal oxidation (cimetidine), extend T1 / 2, increase the risk of toxic effects of amitriptyline (may require dose reduction of 20-30%), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) reduce the concentration in the plasma and reduce the effectiveness of amitriptyline.
The combined use of disulfiram and others. Atsetaldegidrogenazy inhibitors provokes delirium.
Fluoxetine and fluvoxamine increase in plasma concentration of amitriptyline (may require amitriptyline dose reduction by 50%).
Estrogensoderjath oral contraceptive drugs and estrogens may increase the bioavailability of amitriptyline.