Amitriptyline Hydrochloride

Generic name: amitriptyline, amitriptyline hydrochloride.
Brand names: Elavil, Endep and many others.

Amitriptyline is one of the most common first generation antidepressants. Despite the fact that many decades have passed since its first use, new antidepressants have appeared and continue to appear, it still remains the drug with the most powerful antidepressant effect. All newly developed antidepressant drugs are compared with amitriptyline as the benchmark for antidepressants.

Amitriptyline is a drug from the group of tricyclic antidepressants with sedative and anxiolytic effects. It is used, on the one hand, to treat depression and, on the other hand, to treat chronic pain (e.g. nerve pain, headache prevention, irritable bowel). Numerous precautions and possible interactions are considered when using amitriptyline. The most common side effects include dry mouth, nausea, constipation, weight gain, tremor, drowsiness, headache, dizziness, increased sweating, and impaired accommodation.

Amitriptyline is a kind of drug. Although these are useful for stress as well as depression, lower doses may also be popular to block the long term (chronic) pain of some rheumatic ailments. A few other antidepressants can be useful for long-term pain. The compounds rebalances in the central nervous system, which relax the muscles can alleviate pain and enhance sleep. Additionally, it may help at depression and any stress caused by the pain, though low doses aren’t enough on their very own to treat depression that is serious. The impact on sleep is generally prompt, if amitriptyline works for you, as well as disposition and your pain will likely improve within two to six weeks.

Why am I being prescribed amitriptyline?

A consultant rheumatologist can prescribes amitriptyline for long-term pain due to:

• arthritis
• fibromyalgia
• long-term (tension) head aches

Are there any reasons I will not be prescribed amitriptyline?

Amitriptyline will not be prescribed if you are recuperating from a recent heart attack (myocardial infarction) or if you’ve:

• Acute porphyria (an enzyme disorder causing serious nerve or skin symptoms)
• Specific types of glaucoma (increased pressure inside the eyeball).

Structure and properties

Elavil (C20H23N, Mr = 277.4 g / mol) is as amitriptyline hydrochloride as a white or almost white powder before or as colorless crystals. The dibenzo-cycloheptadiene derivative is derived from imipramine and belongs to the tricyclic antidepressants. In the liver it is metabolized by N-demethylation by cytochrome also in the pharmacologically active metabolite nortriptyline.

Effects

Amitriptyline (N06AA09 ATC) is an antidepressant, anxiolytic, stress relieving, agitation absorbing, sedating and promotes sleep. It has anticholinergic, antihistamine and analgesic properties.

Mechanism of action

Amitriptyline affects the neurotransmitter system in the central nervous system. It inhibits the reuptake of serotonin and norepinephrine in the presynaptic neuron.

Amitriptyline also acts on muscarinic acetylcholine receptor antagonist, on histamine receptor of type 1, the 5-HT2 receptor and the alpha1-adrenoreceptor.

Indications

Amitriptyline is used for various depressive disorders, including the endogenous, reactive and neurotic depression and depression in geriatrics. It can be used in combination with the antipsychotic drug on depressive symptoms in schizophrenic psychoses from the group of response forms. Amitriptyline is also indicated for the treatment of mood disorders in somatic.

Amitriptyline is approved for patients with chronic pain who have not responded to conventional treatment. It is with irritable bowel used in fibromyalgia, nerve pain and prevent tension headaches.

Depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, medicinal, with brain lesions).

As part of complex therapy for mixed emotional disorders, psychosis in schizophrenia, alcohol withdrawal, behavioral disorders (activity and attention), nocturnal enuresis (except for patients with bladder hypotension), bulimia nervosa, chronic pain syndrome. migraine, rheumatic diseases, atypical pain in the face, postherpetic neuralgia, post-traumatic neuropathy, diabetic or other peripheral neuropathy), headache, migraine (prevention), gastric ulcer and duodenal ulcer.

Dosage

According to the SPC. The dose is adjusted individually. The dosage is built up slowly and the taken are generally in the evening. Upon satisfying effect, the maintenance dose is adjusted to ensure the therapeutic effect. The antidepressant effect usually occurs only after 2 to 3 weeks. The completion of the therapy is tapering.

Adults

For adults with depression, the initial dose is 25-50 mg at night, then the dose can be gradually increased, taking into account the effectiveness and tolerability of the drug, up to a maximum of 300 mg / day. in 3 divided doses (most of the dose is taken at night). When a therapeutic effect is achieved, the dose can be gradually reduced to the minimum effective, depending on the patient’s condition. The duration of the course of treatment is determined by the patient’s condition, the effectiveness and tolerability of the therapy and can range from several months to 1 year, and, if necessary, even more. In old age, with mild disorders, as well as with bulimia nervosa, as part of complex therapy for mixed emotional disorders and behavioral disorders, psychosis with schizophrenia and alcohol withdrawal, it is prescribed at a dose of 25-100 mg / day (at night), after reaching the therapeutic effect, they switch to the minimum effective dose – 10-50 mg/day.

For the prevention of migraine, with chronic pain syndrome of a neurogenic nature (including prolonged headaches), as well as in the complex therapy of gastric ulcer and duodenal ulcer – from 10-12.5-25 to 100 mg/day. (the maximum part of the dose is taken at night).

Children

Children as an antidepressant: from 6 to 12 years old – 10-30 mg/day. or 1-5 mg/kg/day. fractionally, in adolescence – up to 100 mg/day.

With nocturnal enuresis in children 6-10 years old – 10-20 mg/day. at night, 11-16 years old – up to 50 mg/day.

Contraindications

Hypersensitivity to amitriptyline, immediate recovery period after myocardial infarction, cardiac conduction disorders and acute poisoning with alcohol, barbiturates and opiates. Amitriptyline should not be combined with MAOIs (including moclobemide and selegiline), since serious and sometimes fatal reactions have been observed. The drug is contraindicated in pyloric stenosis, prostatic hyperplasia with urinary retention, and paralytic ileus. Because amitriptyline is also an anticholinergic agent, untreated narrow-angle glaucoma is also contraindicated. Amitriptyline should not be used during pregnancy and lactation and in children and adolescents under 18 years of age. Amitriptyline is contraindicated when taking cisapride because of possible cardiac side effects, including QT prolongation and arrhythmias.