Amitriptyline Nycomed

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Amitriptyline Nycomed: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Amitriptyline-Nycomed

ATX code: N06AA09

Active ingredient: amitriptyline (Amitriptylinum)

Producer: Takeda Pharma A / S (Denmark), Nycomed Danmark ApS (Denmark)

Description and photo update: 2018-22-10

Prices in pharmacies: from 65 rubles.

Buy

Film-coated tablets, Amitriptyline Nycomed

Amitriptyline Nycomed is a drug with an antidepressant effect.

Release form and composition

Dosage form of release of Amitriptyline Nycomed:

coated tablets (50 pcs. in dark glass bottles, 1 bottle in a cardboard box);
film-coated tablets: white, biconvex, round (50 pcs. in dark glass bottles, 1 bottle in a cardboard box).

The active substance is in the composition of 1 coated / film-coated tablet: amitriptyline - 10 or 25 mg.

Auxiliary components in 1 coated tablet: microcrystalline cellulose, polypropylene glycol, potato starch, magnesium stearate, lactose monohydrate, titanium dioxide, talc, methylhydroxypropyl cellulose, corn starch, gelatin, croscarmellose sodium, purified water polyvidone.

Auxiliary components in 1 film-coated tablet (10/25 mg):

core: magnesium stearate - 0.25 / 0.5 mg; povidone - 0.83 / 0.6 mg; talc - 2.25 / 4.5 mg; microcrystalline cellulose - 9.5 / 18 mg; potato starch - 28.2 / 38 mg; lactose monohydrate - 27 / 40.2 mg;
shell: propylene glycol - 0.2 / 0.3 mg; titanium dioxide - 0.8 / 0.9 mg; hypromellose - 1.2 / 1.4 mg; talc - 0.8 / 0.9 mg.

Pharmacological properties

Pharmacodynamics

Amitriptyline Nycomed is one of the tricyclic antidepressants from the group of non-selective monoamine reuptake inhibitors. It has a pronounced thymoanaleptic and sedative effect.

The mechanism of action is associated with an increase in the content of serotonin and norepinephrine in the synaptic cleft in the central nervous system. The accumulation of these neurotransmitters occurs due to inhibition of their reuptake by the membranes of presynaptic neurons.

Amitriptyline is a blocker of alpha-1-adrenergic receptors, H1-histamine receptors, M1- and M2-muscarinic cholinergic receptors. Based on the so-called monoamine hypothesis, there is a correlation between the function of neurotransmitters at the synapses of the brain and emotional tone.

A clear correlation between the plasma concentration of amitriptyline in the blood and the clinical effect has not been shown, but, probably, the optimal clinical effect is achieved at a concentration of 100 to 260 μg / L.

Clinical relief of depression is achieved after 2–6 weeks of treatment (later than equilibrium plasma concentration in the blood is reached).

Amitriptyline Nycomed also has a quinidine-like effect on the innervation of the heart.

Pharmacokinetics

After oral administration, amitriptyline is completely and rapidly absorbed from the gastrointestinal tract. Achievement of maximum concentration in blood plasma (C _max) is observed for 2-6 hours after administration.

Plasma concentration of amitriptyline in the blood of different patients can vary significantly. The bioavailability of amitriptyline is approximately 50%. About 95% of the substance binds to blood plasma proteins. The time to reach the maximum concentration (Tc _max) after oral administration is 4 hours, the equilibrium concentration is approximately 7 days from the start of therapy. The volume of distribution is approximately 1085 l / kg. The substance crosses the placenta and is excreted in breast milk.

Metabolism occurs in the liver, about 50% is metabolized during the first passage through the liver. In addition, amitriptyline undergoes N-demethylation by cytochrome P450, followed by the formation of an active metabolite, nortriptyline. The substance and its active metabolite undergo hydroxylation in the liver. N-hydroxy-, 10-hydroxymetabolite amitriptyline, 10-hydroxynortriptyline also have activity. Amitriptyline and nortriptyline are conjugated with glucuronic acid (the conjugates are inactive). The main factor determining renal clearance and plasma concentration in the blood is the rate of hydroxylation. In a small percentage of patients, delayed hydroxylation is observed (it is genetically determined). In the presence of impaired hepatic function, the half-life of amitriptyline / nortriptyline in blood plasma is increased.

The half-life (T1 / 2) of amitriptyline from blood plasma is from 9 to 46 hours; nortriptyline - from 18 to 95 hours

Excretion occurs mainly in the form of metabolites by the kidneys and through the intestines. Only a small part of the dose taken is excreted unchanged through the kidneys. With impaired renal function, the metabolism of amitriptyline and nortriptyline does not change, although their excretion slows down. Amitriptyline is not removed from blood plasma by dialysis (due to its connection with blood proteins).

Indications for use

Amitriptyline Nycomed is prescribed for the treatment of endogenous depression and other depressive disorders.

Contraindications

Absolute:

myocardial infarction (including recent ones);
acute delirium;
acute alcohol intoxication;
acute intoxication with drugs with hypnotic, analgesic and psychotropic effects;
angle-closure glaucoma;
arrhythmias;
intraventricular / atrioventricular conduction disorders;
lactose intolerance, lactase deficiency and glucose-galactose malabsorption;
hyperplasia of the prostate with urinary retention;
bradycardia;
hypokalemia;
paralytic intestinal obstruction, pyloric stenosis;
congenital long QT syndrome, as well as combination therapy with drugs that lead to a prolongation of the QT interval;
combination therapy with monoamine oxidase inhibitors, including a period of 14 days before starting use;
age up to 18 years;
lactation period;
individual intolerance to the components of the drug.

Relative (when prescribing Amitriptyline Nycomed, caution and medical supervision are required):

diseases of the blood and cardiovascular system, including angina pectoris and arterial hypertension;
acute angle of the eye chamber and flat anterior chamber of the eye;
angle-closure glaucoma;
increased intraocular pressure;
retention of urine;
hyperplasia of the prostate;
epilepsy (the use of Amitriptyline Nycomed can lead to a decrease in the seizure threshold);
convulsive conditions;
hyperthyroidism;
hypotension of the bladder;
schizophrenia;
bipolar disorder;
abnormal liver or kidney function;
chronic alcoholism;
combination therapy with drugs with hypnotic and antipsychotic effects;
pregnancy;
elderly age.

Instructions for the use of Amitriptyline Nycomed: method and dosage

Amitriptyline Nycomed tablets 25 mg or 10 mg are taken orally, preferably immediately after a meal. Do not chew the tablets.

The standard dosage regimen for adult patients: at the beginning of treatment - 25-50 mg in 2 divided doses, if necessary, the daily dose is gradually increased to 200 mg; duration of use - 6 months or longer (in order to prevent relapse).

The initial daily dose of Amitriptyline Nycomed for elderly patients is 25-30 mg in 1 dose (at night). If necessary, until a therapeutic effect is achieved, the dose is increased every other day to 50–10 mg per day. Appointment of a repeated course requires additional examination.

In liver failure, Amitriptyline Nycomed is prescribed in a reduced dose.

To avoid the onset of withdrawal symptoms (in the form of headache, sleep disturbances, irritability and general ill health), the drug should be withdrawn gradually. These symptoms are not a sign of drug dependence.

Side effects

Some of the following undesirable effects (in particular, tremors, headaches, decreased libido and concentration, constipation) can be symptoms of depression, and when depression subsides, they usually go away.

More than 50% of patients while using Amitriptyline Nycomed may develop one or more of the following disorders. The drug can lead to the development of side reactions similar to those caused by other tricyclic antidepressants.

Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):

sense organs: very often - decreased visual acuity, impaired accommodation (during therapy, reading glasses may be required); often - mydriasis; infrequently - increased intraocular pressure, tinnitus; rarely - aggravation of narrow-angle glaucoma, loss of the ability to accommodate;
skin: very often - hyperhidrosis; infrequently - urticaria, cutaneous vasculitis, rash; rarely - alopecia, photosensitivity;
urinary system: often - urinary retention;
nervous system: very often - sedative effect (manifested in the form of lethargy, tendency to sleep), dizziness, tremor, headache; often - taste disturbance, decreased concentration of attention, paresthesia, extrapyramidal symptoms (ataxia, akathisia, parkinsonism), tardive dyskinesia, dystonic reactions, slow speech; infrequently - convulsions;
cardiovascular system: very often - tachycardia, palpitations, orthostatic hypotension; often - arrhythmia (including conduction disturbances, lengthening of the QT interval), hypotension, conduction block along the bundle branch, AV block; infrequently - increased blood pressure; rarely - myocardial infarction;
psyche: very often - disorientation, confusion (in elderly patients it manifests itself as anxiety, sleep disturbances, difficulty in remembering, psychomotor agitation, confusion of thoughts, delirium); often - decreased concentration of attention; infrequently - nightmares, manic syndrome, cognitive impairment, hypomania, mania, anxiety, fear, insomnia; rarely - delirium, aggressiveness, hallucinations (in patients with schizophrenia); very rarely - suicidal behavior / thoughts;
reproductive system: very often - strengthening / weakening of sexual desire; often (in men) - impotence, erectile dysfunction; rarely (in women) - delayed orgasm, galactorrhea, loss of the ability to achieve orgasm; rarely (in men) - delayed ejaculation, gynecomastia;
digestive system: very often - constipation, dry mouth, nausea; often - inflammation of the oral cavity, gum recession, burning sensation in the mouth, dental caries; infrequently - vomiting, diarrhea, swelling of the tongue; rarely - cholestatic jaundice, paralytic intestinal obstruction, abnormal liver function, swelling of the parotid gland, hepatitis;
hematopoietic organs: rarely - thrombocytopenia, agranulocytosis, depression of bone marrow functions, eosinophilia, leukopenia;
laboratory parameters: often - expansion of the QRS complex, lengthening of the QT interval, ECG changes; rarely - an increase in the activity of transaminases and alkaline phosphatase, abnormal liver function tests;
metabolism: very often - weight gain, increased appetite; rarely - decreased appetite; very rarely - syndrome of inappropriate secretion of antidiuretic hormone;
the body as a whole: often - weakness; infrequently - facial swelling; rarely - an increase in body temperature.

Abrupt cessation of taking Amitriptyline Nycomed can cause the development of disorders such as nausea, malaise and headache. Gradual withdrawal of therapy is associated with the following transient symptoms (during the first two weeks of dose reduction): agitation, irritability, sleep and dream disturbances; in rare cases (within 2-7 days after the termination of prolonged therapy) - hypomania, mania.

Overdose

Overdose reactions vary significantly in different patients.

Moderate / severe intoxication in adults is observed when taking amitriptyline at a dose of more than 500 mg, taking about 1000 mg can be fatal.

The main symptoms of an overdose of Amitriptyline Nycomed can occur suddenly or develop gradually. In the first 2 hours, psychomotor agitation or drowsiness, hallucinations and symptoms are observed that are associated with the anticholinergic effect of the drug, in particular, convulsions, tachycardia, mydriasis, dry mucous membranes, urinary retention, weakening of intestinal motility, an increase in body temperature. Then there may be a disturbance of consciousness, respiratory failure, a sharp depression of the functions of the central nervous system, progressing to coma.

Cardiac symptoms manifest as arrhythmias (ventricular tachyarrhythmias, fibrillation, and ventricular flutter). The characteristic changes on the ECG are prolongation of the PR interval, widening of the QRS complex, depression of the ST segment, prolongation of the QT interval, inversion or flattening of the T wave, and intracardiac conduction blockade to varying degrees, which can lead to cardiac arrest. Possible occurrence of heart failure, arterial hypotension, cardiogenic shock, metabolic acidosis and hypokalemia, confusion, agitation, hallucinations and ataxia.

Other symptoms:

central nervous system: suppression of its functions, convulsions, strong craving for sleep, coma;
vascular system: hypotension;
respiratory system: respiratory failure;
psyche: hallucinations, psychomotor agitation;
m-anticholinergic effects: muscle cramps, impaired accommodation, dry mouth, urinary retention.

In case of an overdose, symptomatic and supportive therapy is indicated, including discontinuation of Amitriptyline Nycomed, gastric lavage (even if some time has passed since taking the drug), and taking activated charcoal.

Even in seemingly uncomplicated cases, the patient's condition must be carefully monitored. It is necessary to observe the heart rate and respiration, the level of consciousness, the magnitude of blood pressure. The level of gases and electrolytes in the blood needs frequent monitoring. In order to prevent respiratory arrest, it is necessary to ensure airway patency and artificial ventilation.

ECG control is carried out for 3-5 days. With the expansion of the QRS complex, ventricular arrhythmias and heart failure, it can be effective to shift the pH of the blood to the alkaline side (use of sodium bicarbonate solution or hyperventilation) with the rapid introduction of hypertonic sodium chloride solution (100-200 mmol Na +). With ventricular arrhythmias, traditional antiarrhythmic drugs can be used, for example, intravenous lidocaine at a dose of 50-100 mg (1-1.5 mg / kg) followed by infusion at a rate of 1 to 3 mg / min.

Defibrillation and cardioversion are prescribed if necessary. Circulatory insufficiency can be corrected with plasma-substituting solutions, and in severe cases, dobutamine is infused (initial dose - 2-3 mcg / kg / min, further, depending on the effect, the dose can be increased). Convulsions and agitation can be controlled with diazepam.

Standard therapy is indicated for patients with metabolic acidosis. Dialysis is ineffective because the concentration of amitriptyline in the blood is low.

special instructions

Prior to the appointment of Amitriptyline Nycomed, blood pressure control is required (at an initially low / labile pressure, it can decrease even more).

Caution should be exercised with a sudden transition to an upright position from a lying or sitting position, since there is an increased risk of bone fractures during therapy.

In some cases, hypokalemia or agranulocytosis may occur, and therefore it is recommended to control peripheral blood, especially with an increase in body temperature, tonsillitis and the appearance of flu-like symptoms. With long-term treatment, it is recommended to monitor the function of the liver and cardiovascular system.

You can not take alcohol during therapy with Amitriptyline Nycomed.

Due to the m-anticholinergic action of the drug, it is possible to develop attacks of increased intraocular pressure, a decrease in lacrimation and a relative increase in the amount of mucus in the lacrimal fluid, which can cause damage to the corneal epithelium in patients wearing contact lenses.

There is information about a case of lethal arrhythmia that occurred 56 hours after an overdose of amitriptyline.

In suicidal patients, the suicidal risk may persist until depressive symptoms improve significantly. In this regard, during the first 2–4 weeks of using the drug, such patients need careful monitoring. For the condition of patients who previously had suicidal phenomena / expressed suicidal thoughts or who tried to commit suicide before or during treatment, constant medical supervision is required. Amitriptyline Nycomed should be given to them by a trusted person. It must be borne in mind that the drug in persons under 24 years of age may itself increase the frequency of suicides, therefore, the benefit / risk ratio must be assessed before prescribing.

In case of manic-depressive syndrome, taking the drug can provoke a manic phase, which requires its cancellation.

Before performing surgical operations, Amitriptyline Nycomed should be canceled if possible. In case of emergency operations, the anesthesiologist must be warned about the therapy.

Amitriptyline Nycomed may affect the effect of insulin and the change in glucose concentration after a meal. For patients with diabetes mellitus, correction of hypoglycemic therapy may be required. Depression can also affect glucose metabolism. When combined with other m-anticholinergics, the m-anticholinergic effect of amitriptyline may increase.

Dry mouth can lead to inflammation, changes in the oral mucosa, a burning sensation and tooth decay. In this regard, it is necessary to warn the dentist about the treatment being carried out and undergo regular examinations.

Influence on the ability to drive vehicles and complex mechanisms

It is recommended to refuse to drive vehicles while taking Amitriptyline Nycomed.

Application during pregnancy and lactation

pregnancy: efficacy / safety has not been studied, the appointment of Amitriptyline Nycomed, especially in the I and III trimesters, is possible only in cases where the expected benefit is greater than the possible harm (neurological disorders, drowsiness, urinary retention in a newborn);
lactation period: therapy is contraindicated.

Pediatric use

According to the instructions, Amitriptyline Nycomed is not prescribed to patients under 18 years of age.

With impaired renal function

Therapy for impaired renal function requires caution.

For violations of liver function

Therapy for violations of hepatic function requires caution.

Use in the elderly

The appointment of Amitriptyline Nycomed to elderly patients requires caution.

Drug interactions

Inhibition of the central nervous system by means of general anesthesia, anticonvulsants, antipsychotics, hypnotics and sedatives, narcotic / central analgesics, alcohol is potentiated by taking Amitriptyline Nycomed. Amitriptyline, like other tricyclic antidepressants, is metabolized by the CYP2D6 isoenzyme of hepatic cytochrome P450, which has several isoforms in humans.

The isoenzyme CYP2D6 can be inhibited by various psychotropic drugs, in particular, antipsychotics, serotonin reuptake inhibitors (excluding citalopram, which is a very weak inhibitor), antiarrhythmic drugs of the latest generation (phenytoin, procainamide, esmolol, amiodarone, propafenoblockers) and β-adrenoblockers.

These drugs can inhibit the metabolism of Amitriptyline Nycomed and significantly increase its concentration in blood plasma. The isoenzymes CYP3A and CYP2C19 are also involved in the metabolism of amitriptyline.

Contraindicated combination - with monoamine oxidase inhibitors: development of serotonin syndrome, including spasms with excitement, myoclonus, coma, delirium. You can start therapy with monoamine oxidase inhibitors 2 weeks after discontinuation of amitriptyline, you can start taking Amitriptyline Nycomed 2 weeks after discontinuation of an irreversible, non-selective monoamine oxidase inhibitor and 24 hours after discontinuation of a reversible inhibitor of moclobemide. In any case, you need to start treatment with these drugs with small doses, gradually increasing them depending on the effect.

Combinations with Amitriptyline Nycomed not recommended:

clonidine, methyldopa: weakening their hypotensive effect;
adrenaline, ephedrine, isoprenaline, norepinephrine, dopamine, phenylephedrine, used, for example, for general / local anesthesia or in the form of nasal drops: increasing their effect on the cardiovascular system;
drugs that can prolong the QT interval, including H1-histamine receptor blockers (for example, terfenadine), antiarrhythmics (quinidine, etc.), some antipsychotics (especially sertindole, pimozide), anesthetics (isoflurane, droperidol), sotalol, chloral hydrate: increase the risk of developing ventricular arrhythmia;
phenothiazine derivatives, antiparkinsonian drugs, blockers of H1-histamine receptors, atropine, biperiden: enhancement of their action on the central nervous system, visual organs, bladder and intestines; an increase in the likelihood of intestinal obstruction and a strong increase in body temperature;
lithium salts: increased toxicity of lithium, which manifests itself in the form of tremor, tonic-clonic seizures, difficulty in remembering, mismatches of thought, hallucinations, neuroleptic malignant syndrome;
fluconazole, terbinafine: an increase in the serum concentration of amitriptyline in the blood and an increase in the associated toxicity; fainting, ventricular fibrillation / flutter are possible.

Careful combinations:

barbiturates and other inducers of microsomal liver enzymes, including carbamazepine, rifampicin: increased metabolism of amitriptyline and a decrease in its plasma concentration in the blood, which leads to a weakening of the antidepressant effect of Amitriptyline Nycomed;
drugs that depress the central nervous system, including drugs with hypnotics and sedatives, strong analgesics, alcohol: increased inhibition of the functions of the central nervous system caused by their use;
antipsychotics: mutual inhibition of metabolism; this can cause a decrease in the seizure threshold and the development of seizures (dose adjustment may be required); a combination with sleeping pills (droperidol) requires extreme caution;
methylphenidate, cimetidine, slow calcium channel blockers: an increase in the plasma concentration of amitriptyline in the blood, which can occur with increased toxicity;
valproic acid: a decrease in the plasma clearance of amitriptyline, which can lead to an increase in its concentration, including the concentration of nortriptyline (metabolite); with combined use, monitoring of these indicators is required (it may be necessary to adjust the dose of Amitriptyline Nycomed);
sucralfate: weakening the absorption of amitriptyline and its antidepressant effect;
St. John's wort preparations: a decrease in the maximum concentration of amitriptyline in the blood plasma (it may be necessary to adjust the dose of Amitriptyline Nycomed);
phenytoin: inhibition of its metabolism, an increase in the likelihood of its toxic effects (tremor, hyperreflexia, ataxia, nystagmus); at the beginning of therapy, patients receiving phenytoin need to control its concentration; it is necessary to control the therapeutic effect of Amitriptyline Nycomed, since an increase in its dose may be required.

Analogs

Amitriptyline Nycomed analogs are Amitriptyline, Saroten retard.

Terms and conditions of storage

Store at 15-25 ° C. Keep out of the reach of children.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Amitriptyline Nycomed

According to reviews, Amitriptyline Nycomed is an effective drug. The main advantages include its availability and quick action. It is noted that the drug relaxes, soothes, relieves neurosis and insomnia. Of the shortcomings, they usually indicate the development of adverse reactions, including drowsiness, dry mouth, indifference, slight numbness of the tongue, increased appetite.

The price of Amitriptyline Nycomed in pharmacies

The approximate price for Amitriptyline Nycomed 25 mg (50 pcs. Per package, film-coated tablets or film-coated tablets) is 46-60 or 44-50 rubles.