Elavil (Amitriptyline)

$ 111.94$ 230.17

Category: Anti-Depressants
Commercial name: Elavil (Generic)
Active ingredient: Amitriptyline
Production form: Pills
Available dosage: 5mg, 25mg, 50mg

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Description

Elavil (Amitriptyline). Dosage, Side Effects, Interactions

Elavil (Amitriptyline) like doxepin and trimipramine, is one of the tricyclic antidepressants. Amitriptyline is mainly used as amitriptyline hydrochloride in the treatment of depression, where a calming and anxiolytic effect is desired.

Elavil (Amitriptyline) is mainly used in the treatment of depression, where a calming and anxiolytic effect is desired. Due to its very well proven effectiveness, amitriptyline is the first or second choice for migraine prophylaxis . Numerous studies also prove the benefit against tension headaches.

 

How Elavil (Amitriptyline) works

Amitriptyline from the class of tricyclic antidepressants belongs to the psychotropic substances and has a pronounced sedative effect component as well as an analgesic effect. Given acutely, amitriptyline inhibits the neuronal uptake of the neurotransmitters norepinephrine and serotonin, thereby increasing the concentration of these two neurotransmitters in the synaptic cleft. Amitriptyline also affects acetylcholine circulation in the brain. The increased availability of the neurotransmitters serotonin and noradrenaline as well as the anticholinergic effect explain the dampening and calming effect of the active ingredient.

The pain-relieving effect of amitriptyline can be explained by its influence on the serotonin concentration. Serotonin plays an important role in the brain’s perception of pain by filtering incoming pain signals.

Furthermore, the active substance has antagonistic properties on the M-choline receptors (M 1 and M 2 ), histamine receptors (H 1 stronger than H 2 ), on α-adrenoceptors (α- 1 stronger than α- 2 ) and serotonin receptors (5-HT 2 stronger than 5-HT 1 ).

 

Pharmacokinetics

After oral intake, the active ingredient is slowly but completely absorbed. Maximum plasma concentrations are reached after 1-5 (-8) hours. Systemic bioavailability is approximately 50% compared to intravenous administration. Due to the pronounced lipophilicity of amitriptyline, it is distributed throughout the organism. The active ingredient is predominantly bound to tissue and plasma proteins. Only 3-6% are free in the plasma.

Metabolism occurs mainly in the liver by N-demethylation ( CYP3A4 ) and hydroxylation. About 3-5% of the population can have very high plasma levels because they have a reduced ability to hydroxylate due to genetic differences in the cytochrome P 450 system.

The metabolites are excreted in both free and conjugated form. The plasma half-life after oral administration is approximately 10-28 hours. Older people have a longer half-life.

 

Dosage of Elavil (Amitriptyline)

Amitriptyline is dosed gradually or gradually. On an outpatient basis, the maximum daily dose is 150 mg; in the inpatient setting, the dose can be increased to up to 300 mg daily.

 

Side effects of Elavil (Amitriptyline)

The most common side effects of amitriptyline include the symptoms typical of many antidepressants, such as dry mouth, dizziness, headaches and fatigue. Gastrointestinal complaints are also not uncommon, as is a loss of sexual desire or potency. These side effects and other undesirable effects such as tachycardia or low blood pressure usually decrease with continued use.

The following are very common and common side effects of amitriptyline:

Very common (≥ 1/10):

Cardiac arrhythmias, fatigue, drowsiness, dizziness, speech disorders, tremor, nasal congestion, dry mouth, constipation, sweating, hypotension, orthostatic dysregulation, weight gain, transient increase in liver enzyme activity, aggression. These side effects are to be expected especially at the beginning of the treatment. Accommodation disorders are also a very common side effect. However, this can occur at any time during treatment.

Common (≥1/100 to <1/10):

Hyponatraemia, micturition disorders, skin rashes, thirst, loss of libido, impotence, inner restlessness, in elderly patients there is an increased risk of developing delirious syndromes.

Children have an increased risk of developing tooth decay. It is advised to pay more attention to daily dental care. In patients with a brain-organic psychosyndrome, the possible generation of pharmacogenic delirium must be considered.

 

Interactions

Interactions with various active ingredients and substance classes can impair the effect of amitriptyline or be influenced in its effect by its effect.

Enhancement of the effect of amitriptyline under:

  • other drugs with anticholinergic effects
  • fluoxetine
  • fluvoxamine
  • neuroleptics
  • cimetidine

Reduced effectiveness of amitriptyline under:

  • St. John’s Wort (Hypericum)

Amitriptyline increases the effect of the following drugs and substance classes:

  • drugs with a central depressant effect
  • sympathomimetic amines

Amitriptyline reduces the effect of the following drugs and substance classes:

Antihypertensives of the guanethidine or clonidine type . Patients treated with clonidine are at risk of rebound hypertension.

In any case, irreversible MAO inhibitors should be discontinued at least 14 days and reversible MAO inhibitors at least 1 day before starting therapy with amitriptyline. Otherwise, severe side effects such as agitation, delirium, coma, hyperpyrexia, seizures and severe blood pressure fluctuations must be expected. An additional administration of MAO inhibitors is only possible in individual cases in the case of therapy-resistant depression and taking all necessary precautionary measures and slowly increasing the dose.

Amitriptyline can influence the effect of coumarin derivatives (eg phenprocoumon ). If amitriptyline and coumarins are taken at the same time, continuous monitoring of the blood coagulation parameters is necessary.

Concomitant administration of drugs that also prolong the QT interval (e.g. class IA or III antiarrhythmics, cisapride , antibiotics , antimalarials, antihistamines , neuroleptics), lead to hypokalemia (e.g. certain diuretics ) or can inhibit the hepatic breakdown of amitriptyline (e.g. MAO inhibitors, imidazole antifungals) should be avoided.

 

Contraindication

The use of amitriptyline is contraindicated in the following cases:

  • Hypersensitivity to the active substance
  • Acute intoxication with alcohol, sleeping pills, painkillers and psychotropic drugs
  • urinary retention
  • delirium
  • untreated angle-closure glaucoma
  • Prostatic hyperplasia with residual urine
  • Pyloric stenosis (narrowing of the area around the stomach outlet)
  • Paralytic ileus (obstruction of the bowel due to paralysis of the bowel).

Pregnancy

Amitriptyline should not be used during pregnancy, especially in the first and last trimester, unless clearly necessary. Animal studies have shown reproductive toxicity after high doses of amitriptyline.

Withdrawal symptoms in the form of cardiac and respiratory disorders, urination and defecation, and restlessness were observed in newborns after administration of higher doses of antidepressants before birth.

 

Lactation

Amitriptyline passes into breast milk and should therefore not be taken while breastfeeding. If there is a compelling indication, breastfeeding should be discontinued.

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Additional information

Dosage

10 mg, 25 mg, 50 mg

Quantity

30, 60, 90, 120, 180

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