Simbalta - Instructions For Use, Reviews, Price, Capsule Analogues

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

Simbalta

Simbalta: instructions for use and reviews

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

Latin name: Cymbalta

ATX code: N06AX21

Active ingredient: duloxetine (duloxetine)

Manufacturer: Lilly del Caribe Inc. (Puerto Rico)

Description and photo updated: 2019-27-08

Prices in pharmacies: from 1497 rubles.

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Simbalta is an antidepressant.

Release form and composition

Dosage form - enteric capsules: hard gelatinous with an opaque structure, inside the capsules - pellets, from grayish-white to white (7 or 14 pieces in a blister, in a cardboard box 1, 2 or 6 blisters and instructions for use of Simbalta):

• capsule No. 1: blue cap, identification code “9542” applied in white ink; the body is greenish-yellow, a dose of 60 mg is applied in white ink;
• capsule number 3: blue cap, green ink marked with identification code “9543”; the body is white, a dose of 30 mg is applied in green ink.

1 capsule contains:

• active substance: duloxetine hydrochloride - equivalent to the content of 30 mg and 60 mg of duloxetine base;
• auxiliary components: granulated sugar, hypromellose, triethyl citrate, sucrose, hypromellose acetate succinate, white dye (hypromellose, titanium dioxide), talc;
• shell: indigo carmine, titanium dioxide, sodium lauryl sulfate, gelatin (additionally in the capsule shell 30 mg - iron oxide yellow dye);
• ink: white ink TekPrint SB-0007P, green ink TekPrint SB-4028.

Pharmacological properties

Pharmacodynamics

Duloxetine is an antidepressant, serotonin and norepinephrine reuptake inhibitor, dopamine uptake is weak. The substance does not possess a significant affinity for histaminergic, dopaminergic, adrenergic and cholinergic receptors.

In depression, the mechanism of action of duloxetine is based on the suppression of the reuptake of serotonin and norepinephrine, due to which noradrenergic and serotonergic neurotransmission in the central nervous system increases.

The substance has a central mechanism for suppressing pain syndrome, with pains of neuropathic etiology, this is manifested mainly by an increase in the threshold of pain sensitivity.

Pharmacokinetics

Duloxetine is well absorbed after oral administration. Absorption begins 2 hours after taking Simbalta. Time to reach C _max (maximum concentration of the substance) - 6 hours. Food intake has no effect on C _max, while there is an increase in the time to reach this indicator up to 10 hours, which indirectly reduces the degree of absorption (by about 11%).

The apparent volume of distribution of duloxetine is approximately 1640 liters. The substance binds well to plasma proteins (> 90%), mainly albumin and α ₁ -acid globulin. Liver / kidney disorders do not affect the degree of binding to plasma proteins.

Duloxetine is actively metabolized, its metabolites are excreted mainly in the urine. Isoenzymes CYP2D6 and CYP1A2 catalyze the formation of two main metabolites - 4-hydroxyduloxetine glucuronide and 5-hydroxy, 6-methoxyduloxetine sulfate. They have no pharmacological activity.

T _1/2 (half-life) of the substance - 12 hours. Average ground clearance is 101 l / h.

In patients with severe renal impairment (end-stage chronic renal failure) on hemodialysis, the values of C _max and AUC (average exposure) of duloxetine increase 2 times. In these cases, it is necessary to consider the feasibility of reducing the dose of Simbalta.

With clinical signs of hepatic failure, there may be a slowdown in metabolism and excretion of the substance.

Indications for use

• depression;
• generalized anxiety disorder;
• painful form of diabetic peripheral neuropathy;
• chronic pain syndrome of the musculoskeletal system (including conditions with fibromyalgia, chronic pain syndrome in the lower back, osteoarthritis of the knee joint).

Contraindications

• uncompensated angle-closure glaucoma;
• uncontrolled arterial hypertension;
• syndrome of glucose-galactose malabsorption, isomaltase or sucrase deficiency, fructose intolerance;
• liver pathologies accompanied by liver failure;
• a severe form of chronic renal failure with creatinine clearance (CC) less than 30 ml / min;
• simultaneous use of monoamine oxidase (MAO) inhibitors;
• concomitant administration of ciprofloxacin, fluvoxamine, enoxacin (potent inhibitors of the CYP1A2 isoenzyme);
• period of breastfeeding;
• age up to 18 years;
• hypersensitivity to the components of the drug.

It is recommended to prescribe Simbalta with caution to patients with mania and bipolar disorder (including a history), a history of suicidal thoughts and attempts, seizures (including a history), the risk of an acute attack of angle-closure glaucoma, intraocular hypertension, an increased risk of hyponatremia, liver cirrhosis (taking diuretics, old age), with impaired liver function, renal failure (CC 30-60 ml / min).

During pregnancy, the drug is indicated for use only if the expected benefit of therapy for the mother outweighs the potential threat to the fetus.

When prescribing Simbalta, the doctor should warn women of childbearing age that the patient should inform the doctor about planning pregnancy or conception during the period of therapy.

Simbalta, instructions for use: method and dosage

Simbalt capsules are taken orally, regardless of food intake, swallowing whole, without violating the enteric coating.

Recommended dosage:

• depression: the initial and maintenance dose is 60 mg once a day. The therapeutic effect usually occurs after 2–4 weeks of treatment. Clinical studies on the feasibility and safety of using doses in the range above 60 mg to 120 mg per day in patients who do not respond to the initial dose have not confirmed an improvement in the patient's condition. To prevent relapse, it is recommended to continue taking Simbalta for 8-12 weeks after a response to therapy is achieved. Patients with a history of depression and a positive response to duloxetine therapy are shown to take Simbalta at a dose of 60–120 mg per day for an extended period;
• generalized anxiety disorder: the initial dose is 30 mg per day, with insufficient response to therapy, it can be increased to 60 mg, which is the maintenance dose for most patients. The initial and maintenance dose for patients with concomitant depression is 60 mg per day. With good tolerance of therapy to achieve the desired clinical response, an increase in the dose to 90 mg or 120 mg is indicated. After achieving control over the patient's condition, treatment should be continued for 8-12 weeks to prevent relapse of the disease. For elderly patients, an initial dose of 30 mg should be taken for two weeks before switching to 60 mg or more per day;
• painful form of diabetic peripheral neuropathy: initial and maintenance dose - 60 mg 1 time per day, if necessary, it can be increased. The therapeutic effect should be assessed after 8 weeks of regular use of Simbalta. In the absence of a sufficient response at the beginning of therapy, after this period of time, improvement in the condition is unlikely. The doctor should evaluate the clinical effect regularly, every 12 weeks;
• chronic pain syndrome of the musculoskeletal system: the initial dose is 30 mg once a day for one week, then the patient is prescribed 60 mg once a day. The course of treatment is 12 weeks. The expediency of longer use is determined by the attending physician individually, taking into account the tolerance of Simbalta and the clinical condition of the patient.

In renal failure with CC 30–80 ml / min, dose adjustment is not required.

Due to the risk of a withdrawal syndrome, it is necessary to discontinue therapy by gradually reducing the dose of Simbalta over 1-2 weeks.

Side effects

• from the nervous system: very often - drowsiness, headache; often - dizziness, tremors, paresthesias, lethargy; infrequently - hyperexcitability, myoclonus, akathisia, dysgeusia, impaired concentration, dyskinesia, sleep disturbance, restless legs syndrome; rarely - convulsions, serotonin syndrome, extrapyramidal disorders, psychomotor agitation;
• on the part of the psyche: often - insomnia, agitation, anxiety, unusual dreams, disturbed orgasm (including anorgasmia), decreased or loss of libido; infrequently - sleep disorders, disorientation, bruxism, apathy, suicidal thoughts; rarely - mania, aggression and hostility, hallucinations, suicidal behavior;
• from the gastrointestinal tract: very often - dry mouth, nausea; often - abdominal pain, vomiting, dyspepsia, diarrhea, flatulence, constipation; infrequently - belching, gastrointestinal bleeding, gastritis, dysphagia, gastroenteritis; rarely - bad breath, stomatitis, hematochezia;
• from the musculoskeletal and connective tissue: often - muscle spasms, musculoskeletal pain; infrequently - muscle stiffness, muscle cramps; rarely - trismus;
• from the skin and subcutaneous tissues: often - skin rash, itching, increased sweating; infrequently - contact dermatitis, night sweats, cold sweats, urticaria, increased bruising, photosensitivity; rarely - angioedema, Stevens-Johnson syndrome; very rarely - tissue contusion;
• on the part of the kidneys and urinary tract: often - dysuria, increased urination; infrequently - nocturia, urinary retention, polyuria, weakening of the flow of urine, difficult onset of urination; rarely - an unusual smell of urine;
• from the side of the heart: often - a feeling of palpitations; infrequently - supraventricular arrhythmia, tachycardia, atrial fibrillation;
• from the respiratory system, chest and mediastinal organs: often - pain in the oropharynx, yawning; infrequently - nosebleeds, tightness in the throat;
• infections and invasions: infrequently - laryngitis;
• vascular pathologies: often - increased blood pressure (BP), hyperemia (including hot flashes); infrequently - orthostatic hypotension, cold extremities, fainting, hypertension; rarely - hypertensive crisis;
• from the immune system: rarely - hypersensitivity, anaphylactic reaction;
• from the endocrine system: rarely - hypothyroidism;
• on the part of the organ of vision: often - blurred vision; infrequently - dry eyes, blurred vision, mydriasis; rarely - glaucoma;
• on the part of metabolism and nutrition: often - decreased appetite; infrequently - hyperglycemia (more often in patients with diabetes mellitus); rarely - dehydration, hyponatremia, syndrome of inappropriate antidiuretic hormone secretion;
• labyrinthine disorders and the organ of hearing: often - tinnitus; infrequently - ear pain, vertigo;
• from the genitals and mammary gland: often - delayed ejaculation, ejaculation disorder, erectile dysfunction; infrequently - menstrual irregularities, testicular pain, gynecological bleeding, sexual dysfunction; rarely - galactorrhea, hyperprolactinemia, symptoms of menopause;
• from the liver and biliary tract: infrequently - severe liver damage, hepatitis; rarely - jaundice, liver failure;
• laboratory indicators: often - weight loss; infrequently - an increase in the concentration of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, creatine phosphokinase, bilirubin, gamma-glutamyl transpeptidase, a significant deviation in liver enzymes; weight gain, increased blood potassium levels; rarely - an increase in the concentration of cholesterol in the blood;
• general disorders: often - increased fatigue, change in taste, falls; infrequently - a feeling of coldness, chest pain, thirst, atypical sensations, a feeling of heat, malaise, gait disturbance, chills.

The most common side effects of Simbalta include transient conditions such as dry mouth, nausea, headache, dizziness, and drowsiness. They can occur at the beginning of therapy, but gradually their severity decreases.

Overdose

There is information about cases of overdose against the background of a single dose of 3000 mg of duloxetine (only Simbalta or in combination with other drugs). One of these cases was fatal. There are post-marketing reports of taking no more than 1000 mg of the substance, usually in combination with other drugs, which also ended in death.

The main symptoms of an isolated or combined overdose: vomiting, drowsiness, tachycardia, coma, serotonin syndrome, clonic seizures.

The main signs of intoxication associated with overdose, according to the results of preclinical studies (in animals), relate to disorders of the digestive and central nervous systems and include the following manifestations: ataxia, tremors, clonic seizures, loss of appetite and vomiting.

Therapy:

• ensuring an adequate supply of fresh air;
• taking activated carbon (in order to limit the absorption of the substance);
• gastric lavage (indicated in cases where little time has passed since taking Simbalta inside, or as part of symptomatic therapy);
• monitoring of cardiac activity and control of basic vital signs;
• symptomatic and supportive treatment;
• correctional treatment with cyproheptadine and carrying out measures aimed at normalizing body temperature (with serotonin syndrome).

Duloxetine is characterized by a large volume of distribution; therefore, the effectiveness of hemoperfusion, forced diuresis, exchange perfusion is considered questionable. The specific antidote is unknown.

special instructions

Since Simbalta has an effect on the central nervous system, the drug should be used with extreme caution in patients with manic episodes and a history of epileptic seizures.

Due to the high risk of developing suicidal thoughts and suicidal behavior against the background of the use of Simbalta, careful monitoring by medical staff and close relatives of patients with depression and other mental disorders is required. It is necessary to potentiate patients, both during the period of treatment and after discontinuation of the drug, to communicate, more often to be interested in the thoughts and feelings that bother them.

In case of cardiovascular diseases, it is recommended to measure blood pressure regularly.

Nonspecific symptoms of hyponatremia include drowsiness, dizziness, nausea, vomiting, weakness, confusion, lethargy; in more severe forms, the patient may faint, fall, and seizures.

Hyponatremia often occurs in elderly patients who are prone to changes in fluid balance in the body.

In patients with nicotine dependence, the level of duloxetine concentration in the blood plasma is reduced by almost half of the norm.

Influence on the ability to drive vehicles and complex mechanisms

During the period of treatment, care should be taken when driving vehicles and complex mechanisms.

Application during pregnancy and lactation

• pregnancy: Simbalta can only be used under medical supervision in cases where the benefits to the mother are significantly higher than the potential risk to the fetus, since the experience of using the drug in this group of patients has not been sufficiently studied;
• lactation period: therapy is contraindicated.

During the period of treatment with duloxetine, in case of planning or pregnancy, you must inform your doctor about this.

The use of selective serotonin reuptake inhibitors during pregnancy, especially in late pregnancy, may increase the likelihood of persistent pulmonary hypertension in newborns.

In cases of application of Simbalta by a mother in late pregnancy, newborns may experience withdrawal syndrome, which is characterized by tremor, low blood pressure, difficulty feeding, syndrome of increased neuro-reflex excitability, convulsions, and respiratory distress syndrome. Most of these disorders are usually observed during labor or in the first few days after birth.

Pediatric use

Simbalta is not prescribed to patients under 18 years of age.

With impaired renal function

• severe chronic renal failure (in patients with CC less than 30 ml / min): therapy is contraindicated;
• renal failure (in patients with CC 30-60 ml / min): Simbalta should be used under medical supervision.

For violations of liver function

• liver diseases occurring with liver failure: therapy is contraindicated;
• impaired hepatic function: Simbalta should be used under medical supervision.

Drug interactions

With simultaneous use with Simbalta:

• MAO inhibitors: can contribute to the development of serotonin syndrome, therefore, these combinations should not be used within 14 days after the abolition of MAO inhibitors, and after stopping treatment with duloxetine, you can start taking MAO inhibitors only after 5 days;
• isoenzyme inhibitors: CYP1A2 slow down the metabolism of duloxetine and increase its concentration in plasma, therefore, when combined, the dose of Simbalta should be reduced;
• paroxetine, fluoxetine [selective serotonin reuptake inhibitors (SSRIs)], tricyclic antidepressants (clomipramine, amitriptyline), St.
• paroxetine and other inhibitors of the isoenzyme CYP2D6: reduce the mean clearance of duloxetine and increase its concentration;
• antagonists of H ₂ -histamine receptors and antacids: do not significantly affect the absorption of the drug;
• anticoagulants and antithrombotic agents: cause an increased risk of bleeding;
• drugs that bind significantly to plasma proteins: can lead to an increase in the content of free fractions of each of the drugs.

It is recommended to use duloxetine with caution in combination with drugs with a narrow therapeutic index and a metabolizable CYP2D6 isoenzyme system.

Analogs

Simbalta's analogs are: Duloxenta, Duloxetine, Duloxetine Canon.

Terms and conditions of storage

Store at temperatures up to 15-30 ° C. Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Simbalta

Reviews about Simbalta, characterizing its effectiveness, are mostly positive. To achieve a therapeutic effect, a pass in the appointment is not allowed. There are many reports of addiction, severe side effects, and withdrawal. The cost is assessed as high.

The price for Simbalta in pharmacies

The approximate price for Simbalta is 1619-1950 rubles (in a package of 14 capsules of 30 mg), 1,717-1989 rubles (in a package of 14 capsules of 60 mg) or 3299-3865 rubles (in a package of 28 capsules of 60 mg).

Simbalta: prices in online pharmacies

Drug name Price Pharmacy

Simbalta 30 mg enteric capsules 14 pcs. 1497 RUB Buy

Simbalta 60 mg enteric capsules 14 pcs. RUB 1526 Buy

Simbalta 60mg capsules 14 pcs. 1684 RUB Buy

Simbalta capsules 30mg 14 pcs. 1901 RUB Buy

Simbalta 60 mg enteric capsules 28 pcs. 2281 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes and does not replace the official instructions. Self-medication is hazardous to health!