Cymbalta

Release form

Cymbalta is produced by the manufacturer in the form of capsules for oral administration. The dosage of the active substance in each capsule is 30 or 60 mg. The blister contains from 7 to 14 capsules. One package can contain from two to four blisters. The international official name of the drug is Duloxetine . Cymbalta is the trade name of a product manufactured by Lilly.

Cymbalta price, where to buy

Buying Cymbalta 30 mg No. 14 in Russia will cost 880-970 rubles.

In Ukraine, the price of this form of release starts from 750 hryvnia.

Online pharmacies in RussiaRussia

ZdravCity

Cymbalta capsules 60 mg 14 pcs. Lilly del Caribe Inc./Lilly S.A.
RUB 1,720 order
Cymbalta capsules 60 mg 28 pcs. Lilly del Caribe Inc. /Lilly S.A
RUB 3,200 order
Read also: Grandaxin: instructions for use of the drug
Cymbalta capsules 30 mg 14 pcs. Lilly del Caribe Inc. /Lilly S.A
RUB 1,615 order

Compound

The main active ingredient in Cymbalta is duloxetine. It determines the effect of the drug on the body. The dosage indicated on the package corresponds to the concentration of duloxetine.

Excipients include those that create the contents of the capsule and those that make up its wall. The contents include sugar and sucrose, hypromellose and its compounds, as well as talc, white dye and triethyl citrate. The capsule wall is formed by substances such as gelatin, compounds of titanium, iron, sodium, as well as indigo carmine and several dyes. Excipients have no effect on the body.

Composition of the product and release form

Each capsule of the drug is soluble in the intestines and contains 20, 30 or 60 mg of Duloxetinum hydrochloridi, as well as additional substances (indicated for a dose of 30 mg/capsule):

capsule contents : methyloxypropyl cellulose 11.2 mg, sucrose 18.1 mg, granulated sugar 40.6 mg, talc - 23.6 mg, hypromellose acetate succinate - 22.4 mg, E1505 - 4.5 mg, white dye - 14 .9 mg;
capsule shell : E132 – 0.1163 mg, titanium dioxide – 1.773 mg, sodium dodecyl sulfate – 0.0688 mg, E172 – 0.065 mg, green and white TekPrint ink – presence of trace amounts.

The drug is provided in blisters containing 14 tablets, and the package contains from 1 to 6 blisters, depending on the manufacturer:

30 capsules (Actavis, USA);
14 capsules (Kanonpharma, Russian Federation);
28 capsules (Eli Lilly and Company, USA);
14/28 capsules (Elan Pharma International Ltd. - Shannon, Ireland);
14 capsules (Lilli SA, Spain).

In addition to the drug of the same name, two more drugs are produced based on Duloxetine - Cymbalta and Yentreve.

Pharmacological properties

Cymbalta belongs to the group of selective serotonin and norepinephrine reuptake inhibitors. This means that the drug selectively blocks the flow of only two substances from the extracellular space of the nervous system into neurons: norepinephrine and serotonin. However, like most representatives of this group, Cymbalta has a minor effect on dopamine metabolism.

These three mediators: serotonin, norepinephrine and dopamine are responsible for the emotional-volitional sphere of the psyche. When their concentration decreases, depression, anxiety, sleep disorders and various emotional and behavioral disorders develop. In this case, what matters is the reduction in concentration not inside the cells, but in the spaces between them.

Cymbalta increases the content of mediators between cells, which leads to a gradual increase in their synthesis by cells and release into the intercellular space. This mechanism causes an increase in mood when taking the drug systematically and a decrease in anxiety.

Special conditions

When serotonin reuptake inhibitors were prescribed in combination with MAO inhibitors, cases of serious reactions, sometimes fatal, were observed (hyperthermia, rigidity, myoclonus, various disorders with possible sharp fluctuations in vital signs and changes in mental status, including severe agitation leading to delirium and to whom). Such reactions are also possible in cases where the serotonin reuptake inhibitor was discontinued shortly before the administration of MAO inhibitors. In some cases, symptoms characteristic of NMS were observed. The effects of combined use of duloxetine and MAO inhibitors have not been evaluated in either humans or animals. The use of Cymbalta simultaneously with MAO inhibitors or within 14 days after their discontinuation is not recommended, because Duloxetine is a serotonin and norepinephrine (norepinephrine) reuptake inhibitor. Based on the T1/2 duration of duloxetine, MAO inhibitors should not be administered for at least 5 days after discontinuation of duloxetine. Like other drugs that have similar effects on the central nervous system, Cymbalta should be used with caution in patients with a history of manic episodes, as well as a history of epileptic seizures. Depressive conditions are accompanied by a high risk of developing suicidal thinking and behavior. As a result, patients diagnosed with depression who are taking duloxetine should inform their physician of any disturbing thoughts and feelings. While using the drug, mydriasis may develop, so caution should be exercised when prescribing duloxetine to patients with increased intraocular pressure or in persons at risk of developing acute angle-closure glaucoma. In patients with severe renal impairment (creatinine clearance <30 ml/min) or severe liver failure, an increase in plasma duloxetine concentrations is observed. If duloxetine is clinically justified in such patients, the drug should be used at lower initial doses. In patients with arterial hypertension and/or other diseases of the cardiovascular system, it is recommended to monitor blood pressure. The drug should be used with caution in patients with chronic alcoholism. Effect on the ability to drive vehicles and operate machinery While taking Cymbalta, sedation and drowsiness may develop, so during the treatment period patients should be careful when driving vehicles and other potentially dangerous activities.

Indications

Cymbalta has a very limited list of indications for use. Prescribing the drug is justified in the following cases:

Treatment of recurrent depressive disorder, current episode of major depression;
A single episode of severe depression;
Severe neuropathic pain syndrome;
Neuropathies in patients with diabetes mellitus;
Anxiety disorder.

Cymbalta is not used to treat mild to moderate depression, nor is it used to prevent depression or treat insomnia. Patients with phobias are also recommended to take treatment with lighter medications. In general, Cymbalta is used in cases where treatment with other means may not be sufficient.

Contraindications

Cymbalta is contraindicated in the following cases:

Hypersensitivity to the components of the drug;
Decompensated stage of renal failure;
Decompensated stage of liver failure;
Uncontrolled arterial hypertension;
Stage 3 hypertension;
Increased intraocular pressure;
History of epilepsy or seizures of another origin;
Bipolar affective disorder;
Taking antibiotics from the fluoroquinolone group;
Children under 18 years of age.

Cymbalta should not be used in combination with monoamine oxidase inhibitors. At least two weeks should pass between taking the latter and prescribing Cymbalta. The reverse order of administration is possible a week after Cymbalta is completely discontinued.

Prescription to pregnant women is allowed only if the benefit to the mother justifies the risk to the fetus.

Side effects

Cymbalta can cause a large number of adverse reactions. All of them are divided into two groups: those that occur while taking the drug and those that appear after stopping treatment. The latter enter the so-called “withdrawal syndrome”. You should learn more about it.

The first group of reactions is currently well studied by the pharmaceutical company. Groups of side effects are identified that occur very often, often, infrequently and rarely. Every tenth patient experiences reactions from the autonomic nervous system: headache, dizziness, dry mouth, periodic nausea. drowsiness. With continued use of the drug, these symptoms disappear spontaneously.

More than one patient out of 100 experiences the following adverse reactions: insomnia, decreased libido, agitation, loss of appetite, weight loss, trembling of the limbs, a feeling of numbness or “crawling” in the limbs, flatulence, bowel and urination disorders, myalgia, hyperhidrosis. These symptoms may disappear on their own or require additional treatment.

More than one patient per 1000 taking the drug experiences symptoms such as: apathy, thoughts of suicide, increased blood sugar, impaired attention, irritability, taste distortion, blurred vision, dilated pupils, increased heart rate, cardiac arrhythmias, increased or decreased blood pressure, orthostatic collapse, nasal and gastrointestinal bleeding, formation of hematomas on the body, increased sensitivity to sunlight, weight gain.

One patient per 10,000 taking the drug may develop the following symptoms: increased intraocular pressure, hypertensive crisis, affect inversion, suicidal attempts, delusional-hallucinatory syndrome, Quincke's edema, anaphylactic shock, toxic hepatitis, convulsions.

If symptoms from the last two groups occur, Cymbalta should be stopped and the patient treated for complications.

Instructions for use of the drug Cymbalta

The medication is administered orally. The capsules are not opened or crushed, but are swallowed whole and washed down with water.

The dosage depends on the nature of the pathology:

Treatment of depression usually begins with a dose of 60 mg/day. In rare cases, the daily dose can be increased to 120 mg, which must be divided into 2 doses. A dose of 60 mg is used once a day. Prescribing a dose exceeding 120 mg/day is inappropriate and unsafe for the body.
To relieve pain in neuropathy, 60 mg/day is prescribed. This dose of medication is used once a day. If necessary, the dose is increased to 120 mg and divided into 2 doses. A noticeable improvement in the patient's condition is observed 2 months after the start of treatment.
For the treatment of generalized anxiety disorder, 30 mg of the drug per day is used. In case of insufficient pharmacological effect, the dose can be increased to 60 or 90 mg per day. Sometimes the dose can be increased to 120 mg/day. A noticeable therapeutic effect of the drug will begin to appear after 2-4 weeks from the start of therapy.

Elderly patients are prescribed the drug in the same dosage as middle-aged patients. However, patients over 65 years of age are not recommended to take the drug in large dosages for a long time.

special instructions

The medication may cause suicidal thoughts and actions, about which the patient’s relatives and/or relatives should be warned. From the beginning of therapy until its end, the patient's actions must be under constant and close supervision. Since the risk of suicidal tendencies persists until the disease remissions.

Patients with epilepsy and a history of manic episodes should be especially careful when treated with Cymbalta, since the drug can aggravate the course of these diseases.

In people with increased intracranial pressure, taking the drug may cause the development of mydriasis. The drug causes an increase in blood pressure in some people, about which the patient should be warned, especially with a history of hypertension.

At the beginning of therapy, symptoms of psychomotor agitation may occur, which usually disappear several weeks after starting the drug.

The drug is contraindicated for use in people with fructose intolerance and malabsorption syndrome, since it contains sucrose.

Since the drug directly affects the human central nervous system, during therapy it is necessary to refuse dangerous work that requires increased concentration. This precaution also applies to driving.

With a sharp refusal of the drug, withdrawal syndrome develops, so it is necessary to stop treatment gradually, reducing the daily dosage over several weeks.

Possible side effects and overdose

Taking the drug Cymbalta sometimes leads to the development of unwanted side reactions. Possible side effects of the medication include:

nausea and vomiting;
dizziness and headache;
constant feeling of thirst;
dyspeptic disorders;
abdominal pain;
bloating;
increased synthesis of liver enzymes;
hepatitis and other liver damage;
sleep disorders;
tremor of the limbs;
loss of appetite and weight loss;
general weakness of the body;
ADH deficiency and sodium deficiency in the body;
apathy;
suicidal tendencies;
apathetic state;
manic episodes;
attacks of aggression and irritability;
decreased sexual desire (libido);
deterioration in the quality of attention;
mydriasis and blurred vision;
dryness of the mucous membrane of the eyes;
seizures;
serotonin syndrome;
withdrawal syndrome;
hyperhidrosis;
hot flashes to the face;
disruptions in the menstrual cycle and anorgasmia;
erectile disfunction;
hyperglycemia;
increased blood pressure;
bleeding;
allergic reactions (skin rashes, itching, urticaria, Steven-Johnson syndrome, etc.);
problems with urination.

Sometimes, when stopping the medication, dizziness, headache and mild nausea may occur.

Data on cases of intoxication with Cymbalta are limited; only a few cases of poisoning with this medication have been recorded. Symptoms of poisoning:

ataxia;
seizures;
nausea and vomiting;
tremor of the limbs;
cardiopalmus;
drowsiness;
decreased appetite.

In rare cases, serotonin syndrome and coma may develop.

It is recommended to detoxify the body in a hospital setting, under constant monitoring of the patient’s cardiac activity. Since there is no specific antidote, symptomatic and supportive therapy is carried out. It is recommended to perform gastric lavage and prescribe activated carbon or other sorbent to reduce the absorption of the drug.

Drug interactions

The medication is not recommended to be taken along with CYP1A2 inhibitors, since this group of drugs affects the metabolism of duloxetine and significantly increases its concentration in the body. In case of urgent need for simultaneous use of CYP1A2 inhibitors and Cymbalta, it is necessary to reduce the daily dosage of the second. CYP2D6 inhibitors also increase the concentration of the drug.

Caution should also be exercised when taking Cymbalta and medications that are metabolized by the CYP2D6 enzyme at the same time, as duloxetine increases their concentration.

Since the drug has a direct effect on the central nervous system, it must be carefully prescribed along with other medications with a similar and sedative effect.

The medicine is not recommended to be combined with alcohol and alcohol-containing products.

When taken in combination with St. John's wort, antidepressants, tramadol, tryptophan, peptidine and other serotonergic drugs, the risk of serotonin syndrome increases. Also, the risk of this syndrome is increased by the combination of Cymbalta and MAO inhibitors. It is recommended to start taking Cymbalta only 14 days after the last MAOI dose.

Concomitant use with anticoagulants and other medications that thin the blood can lead to bleeding.

Overdose

In clinical studies, no deaths were observed with an overdose of Cymbalta. Exceeding the recommended dose may lead to the development of serotonin syndrome, accompanied by delirium, delirium and hallucinations. In addition, impaired consciousness up to coma is possible. Often, with a small overdose, drowsiness, vomiting and increased heart rate occur. In rare cases - convulsive syndrome.

There is no specific treatment for a Cymbalta overdose. Detoxification therapy is carried out.

Cymbalta®

From the side of the central nervous system:

≥10% - dizziness (except vertigo), sleep disturbances (drowsiness or insomnia), headache (headache was less common than when taking placebo); from ≥1% to <10% - tremor, weakness, lethargy, anxiety, yawning; ≤1% - agitation, disorientation.

From the digestive system:

≥10% - dry mouth, nausea, constipation; from ≥1% to <10% - diarrhea, vomiting, loss of appetite, weight loss, abnormal liver laboratory tests, changes in taste; ≤1% - hepatitis, jaundice, increased activity of alkaline phosphatase, ALT, AST and bilirubin levels, belching, gastroenteritis, stomatitis.

From the musculoskeletal system:

from ≥1% to <10% - muscle tension and/or twitching;
≤1% - bruxism .
From the cardiovascular system:

from ≥1% to <10% - palpitations; ≤1% - orthostatic hypotension, syncope (especially at the beginning of therapy), tachycardia, increased blood pressure, cold extremities.

From the reproductive system:

from ≥1% to <10% - anorgasmia, decreased libido, delayed and impaired ejaculation, erectile dysfunction.

From the urinary system:

from ≥1% to <10% - difficulty urinating; ≤1% - nocturia.

From the side of metabolism:

from ≥1% to <10% - weight loss, increased sweating, hot flashes, night sweats; ≤1% - hyponatremia, thirst, weight gain, dehydration.

From the senses:

from ≥1% to <10% - blurred vision, change in taste; ≤1% - glaucoma, glaucoma, mydriasis, visual impairment.

Allergic reactions:

≤1% - anaphylactic reactions, chills, angioedema, rash, Stevens-Johnson syndrome, urticaria.

Other:

≤1% - chills, feeling unwell, feeling hot and/or cold, photosensitivity. When discontinuing the drug, dizziness, nausea, and headache were often observed. Patients with painful diabetic neuropathy may experience a slight increase in fasting blood glucose.

In clinical trials in patients with painful diabetic neuropathy

The following data were identified on the possible effect of duloxetine on glucose concentrations. With short-term use (up to 12 weeks), a slight increase in fasting blood glucose is possible while maintaining a stable level of glycated hemoglobin. During long-term therapy (up to 52 weeks), a slight increase in the level of glycated hemoglobin was noted, which was 0.3% higher than the increase in the corresponding indicator in patients receiving other treatment; There was also a slight increase in fasting glucose and total cholesterol concentrations in the blood.

Post-marketing messages

From the endocrine system:

<0.01% - impaired ADH secretion.

From the side of the central nervous system:

<0.01% - extrapyramidal syndrome, serotonin syndrome; 0 .01% -0.1% - hallucinations.

From the urinary system:

0.01%-0.1% - urinary retention.

Instructions for use

For depressive disorders and chronic pain, the average therapeutic dose is 60 mg. The drug should be taken once a day, optionally in the morning or evening. If this treatment is ineffective, the dosage is increased to the maximum possible - 120 mg. In this case, the daily dose is divided into two times - one capsule in the morning and evening. The effectiveness of treatment can be assessed after 8 weeks.

For anxiety disorder, the starting dosage is lower. In this case, Cymbalta is prescribed 30 mg once a day. If treatment is ineffective, you can double the dose, also dividing it into two doses. Gradually, you can increase the dosage by another 30 mg, and then by another 30 mg, reaching a maximum dose of 120 mg. Exceeding this value is not recommended due to the risk of side effects. The expected effect will appear after 4 weeks of use.

Capsules are washed down with plenty of water; food intake does not affect the absorption of the medication.

How to stop taking it without withdrawal symptoms

In order to avoid withdrawal syndrome, it is recommended to gradually reduce the dosage of the drug until you completely stop taking it. Once every two weeks, the dose should be reduced by no more than 30 mg per day. It should be borne in mind that the capsule cannot be opened and its contents cannot be divided.

If the patient took 120 mg per day, which is equivalent to two 60 mg capsules, in the first two weeks of withdrawal he needs to purchase capsules with a dosage of 30 mg. Its daily dose is 90 mg, that is, one 60 mg capsule in the morning and one 30 mg in the evening. For the next two weeks, you need to take one 60 mg capsule per day. After another two weeks - one 30 mg capsule.

Discontinuation of the drug should take place under the strict supervision of the attending physician. You should pay attention to any change in the general condition of the body.

Analogs

There are only a few analogues that have the same active ingredient as Cymbalta, these include:

Duloxetine canon;
Predanta;
Duloxenta.

In addition, there are drugs that belong to the same pharmacological group and have a similar mechanism of action. These include:

Velaxin;
Velafax;
Venlafaxine;
Milnacipran;
Ixel.

All listed drugs are not interchangeable.

Reviews

Regina P .: “I took Cymbalta for about six months due to severe depression. The drug helped me, but not right away. For about the first month I felt dizzy and had a headache, but I didn’t notice any effect from the drug. After about a month, all the side effects went away, and my mood began to improve little by little. I took Cymbalta for 4 months until I completely got rid of depression.”

Denis M .: “I started taking Cymbalta because of constant anxiety. I have suffered from generalized anxiety disorder since childhood and am periodically hospitalized. I took 30 mg, but there was no effect. When the dosage was increased, my anxiety began to decrease, but tremors appeared in my arms and legs, and my blood pressure began to rise. I had to stop taking Cymbalta and switch to another drug.”

Review from a psychiatrist : “In the domestic market of antidepressants, Cymbalta is not the most popular drug. It is very effective in combating even advanced cases of depression, but there are several pitfalls. First of all, a large number of side effects greatly limits the purpose of the drug. The patient must undergo a thorough examination before receiving the drug. In addition, Cymbalta should only be started in a hospital setting under supervision. This is associated with an increased risk of suicide attempts in susceptible patients with severe depression. As a rule, doctors prefer safer drugs, using Cymbalta as a reserve drug. Western colleagues prescribe Cymbalta more often.”

Content

Pharmacokinetics of the drug

The drug begins to be absorbed orally within 2 hours, and the maximum concentration is reached after 6 hours.
Concurrent food intake does not affect the concentration of the drug in the body, but increases the accumulation time of maximum doses to 10 hours. This leads to a decrease in the percentage (up to 12%) of absorption. About 90% of the drug is bound to albumin and alpha-1-acid glycoprotein, or orosomucoid.

A history of renal and hepatic failure does not in any way affect the activity of the drug and its binding to plasma proteins. This is primarily due to the fact that the metabolites have no pharmacological activity, and 98% of the metabolites are excreted in the urine.

The formation of two main metabolites (glucurone conjugate 4-hydroxy and sulfate conjugate 5-hydroxy-6-methoxy-duloxetine) is catalyzed by cytochrome P450 isoenzymes (CYP2D6 and CYP1A2). The half-life is 11-13 hours, and the clearance (i.e., the rate of elimination) is 101 l/hour.

A feature of the pharmacokinetics of Duloxetine is the clearance of the drug in women and men - in the former it is significantly lower.

As for age, it is also reduced in elderly patients, but this does not require dose adjustment of the drug.

In patients undergoing “classical” or peritoneal hemodialysis, the maximum concentration is increased by 2 times.

Slow elimination and decreased metabolic processes of the drug are observed in patients with severe forms of liver failure.