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Deprivox
Last reviewed: 23.04.2024
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Deprivox is an antidepressant. It is included in the category of elective SSRIs of the neuronal type.
Indications of the deprivox
It is used to treat depression, as well as OCD.
Pharmacodynamics
Tests on the synthesis with endings demonstrated that the substance fluvoxamine is a potent SSRI both in vitro and in vivo. It has minimal affinity with subtypes of serotonin receptors.
The drug has a weak ability of synthesis with α-, as well as ß-adrenoreceptors, and in addition with muscarinic, histaminergic, acetylcholine or dopaminergic endings.
Pharmacokinetics
Fluvoxamine is fully absorbed after ingestion of the tablet. Peak plasma values are observed about 3-8 hours after drug use. Due to the fact that the drug is exposed to the effect of the 1st pass, the bioavailability level reaches only 53%. Pharmacokinetic parameters of the substance do not change when combined with food.
In a state in vitro fluvoxamine is synthesized with a plasma protein by 80%. The distribution volume is 25 l / kg.
The substance undergoes intensive hepatic metabolism. Although in in vitro tests the main isoenzyme (a participant in metabolic processes of the active drug component) is the element CYP2D6, the indices inside the plasma in people with a lower level of activity of the element CYP2D6 are only slightly higher than similar values in people with an intensive metabolic process.
The half-life of plasma is approximately 13-15 hours after a single use of the drug and is slightly prolonged (up to 17-22 hours) in case of multiple use. In this case, the parameters of the equilibrium plasma concentration after repeated use of the substance reaches a period of 10-14 days.
Intensive transformation of the component is observed inside the liver - mainly through the process of oxidative demethylation. At the same time, a minimum of 9 decay products excreted by the kidneys are formed. Inactive are the two main decay products of the substance. Fluvoxamine is a potent inhibitor of the CYP1A2 element. In addition, it moderately slows down the effects of CYP2C components with CYP3A4, and also has only a limiting retardation effect on the element CYP2D6.
The pharmacokinetics of the active component of Deprivoks is linear (in the case of taking a single dose of LS).
The equilibrium plasma values exceed the values calculated from the information for a single dose and also disproportionately higher if larger daily doses are used.
Dosing and administration
The medicine should be swallowed without chewing, while washing with water.
With depression (in adults).
The size of the required initial dose is 50 or 100 mg per day. You need to eat it once a day; recommended before bedtime. Increase dosage can be with the appointment of a doctor, do it gradually, until the moment when the clinical result is obtained. The most effective is a daily dose of 100 mg. It is necessary to select the daily dosage individually, taking into account the patient's reaction to the medicine. A day is allowed to take no more than 300 mg. In the case of appointing dosages that exceed the limit of 150 mg, it is necessary to divide its use into several methods per day (2-3 times). According to WHO requirements, after the signs of depression in the patient disappear, you should continue therapy at least for another 6 months.
To prevent the development of relapse, it is necessary to take 100 mg of Deprivoks per day.
In the treatment of OCD (in children from 8 years old and adults).
The starting daily dose is equal to 50 mg during the first 3-4 days of the course, and then it is gradually increased until the maximum possible effective dosage is achieved (in general, its size is 100-300 mg per day). The maximum adult dose per day is 300 mg, and the infant (children over the age of 8 years) is 200 mg. Dosages, the sizes of which do not exceed 150 mg, are consumed once a day (recommended before bedtime). In the case of appointing dosages larger than 150 mg, it is necessary to divide the portion into 2-3 uses per day. After achieving the drug effect, you should continue the course further, in a dosage that is selected taking into account the therapeutic result. In the absence of symptoms of improvement after 10 weeks of the course, it is necessary to reconsider the appropriateness of the subsequent administration of drugs.
Although there is no information on systematic tests regarding the detection of the limits of the permissible duration of use of the drug, since OCD is a chronic disease, it is considered advisable to continue therapy for more than 10 weeks, even to people who have a therapeutic outcome. Dosage is selected for each patient separately, in a careful manner - to ensure that a person maintains maintenance treatment in the least effective portions. Periodically, it is necessary to review the need to continue the course. People who have been helped by pharmacotherapy can also be given behavioral psychotherapy as an auxiliary treatment.
To cancel a medicine it is necessary gradually, without doing it sharply. After deciding to abolish the drug, the dosage should be gradually reduced in the period 1-2 weeks to reduce the likelihood of withdrawal syndrome. If, as a result of a decrease in dosage or after the end of drug use, the symptoms of the aforementioned syndrome still appear, it is necessary to return to the previous treatment regimen. Further reduction of dosage can continue (under the supervision of a doctor), but even more gradually.
Inadequate kidney or liver, as well as cardiac pathologies.
People with these disorders need to begin treatment with Deprivox using the lowest possible effective doses. At the same time during the therapy the patient should be constantly monitored by the doctor in charge.
[4]
Use of the deprivox during pregnancy
Epidemiological data show that the use of elective SSRIs (including fluvoxamine) during pregnancy, especially in its late stages, may increase the likelihood of developing pulmonary hypertension in the newborn (persistent type). The incidence of such a violation as a result of drug use was fixed at 5 per 1000 pregnancies. In general, there are 1-2 such cases per 1000.
It is forbidden to prescribe Deprivox to pregnant women. Such an application can be justified exclusively in situations where the patient's condition requires the use of this medication.
Single cases of development of the withdrawal syndrome in newborns as a result of using drugs at later stages of pregnancy were noted. Due to the use of SSRIs during the 3rd trimester, some newborns experienced breathing / swallowing problems, as well as hypoglycemia, convulsions, muscle tone disorder, cyanosis, and tremor. Also, unstable temperature indicators, trembling, sensation of drowsiness, lethargy and irritability, constant crying, sleep disorder and vomiting were noted. All these manifestations may require an extension of the period of hospitalization.
Small parts of the medicine pass into the mother's milk, because of which it is forbidden to prescribe it to nursing mothers.
Contraindications
Among the contraindications: combined use with ramelteon, tizanidine or MAOI. Therapy is allowed to begin at least 2 weeks after the discontinuation of the use of irreversible MAOIs, as well as the next day after the discontinuation of the use of reversible MAOIs (such as linezolid or moclobemide). To start using any medicine from the MAOI category is allowed at least one week after the end of the Deprivoks application.
It is forbidden to appoint also to people with intolerance of the substance maleate fluvoxamine or other elements of the drug.
Side effects of the deprivox
Reception of tablets can provoke occurrence of such by-effects:
- reactions of systemic blood flow and lymph: bleeding occurs (this includes bleeding in the gastrointestinal tract, gynecological type, as well as purpura with ecchymoses);
- endocrine pathologies: an inadequate indicator of ADH secretion and the development of hyperprolactinaemia;
- eating disorders and metabolic disorders: loss of appetite, accompanied by anorexia, decreased or increased weight, as well as the development of hyponatremia;
- mental illness: a sense of confusion, the appearance of suicidal thoughts, hallucinations, the development of mania or suicidal behavior;
- disturbances in the work of the National Assembly: the appearance of a sensation of nervousness, drowsiness, agitation, and anxiety. Tremor, insomnia, headache, ataxia, and in addition extrapyramidal disorders and dizziness may develop. There are also convulsions, symptoms similar to neuroleptic malignant syndrome, and in addition serotonin intoxication, dysgeusia and paresthesia with akathisia / psychomotor agitation;
- manifestations in the field of visual organs: the development of mydriasis or glaucoma;
- violations of cardiac function: tachycardia and increased heart rate;
- cardiovascular disorders: orthostatic collapse;
- reactions from the digestive tract: development of constipation, nausea, abdominal pain, dyspepsia, vomiting, diarrhea and dryness of oral mucous membranes;
- manifestations of the hepatobiliary system: a disorder in the liver;
- dermatological disorders and subcutaneous layer reactions: the appearance of hyperhidrosis, signs of photosensitivity, as well as manifestations of allergies (such as itching, rash and edema Quincke);
- dysfunction of ODA, bone and connective tissues: the development of myalgia or arthralgia, as well as fractures of bones. Epidemiological tests, which were mainly performed with patients over 50 years of age, demonstrated an increased likelihood of bone fractures in people taking tricyclics or SSRIs. It was not possible to determine the mechanism causing such a violation;
- impaired renal function and urinary system: problems with urination (this includes urinary incontinence and retention, as well as enuresis and nocturia with pollakiuria);
- manifestations of the mammary glands and reproductive organs: the development of anorgasmia or galactorrhea, as well as delayed ejaculation and menstrual disorders (among them hypomenorrhea with amenorrhea, as well as bleeding from the uterus and hypermenorrhea);
Systemic disorders: development of asthenia or general condition of malaise, as well as withdrawal syndrome.
[3]
Overdose
Signs of an overdose - vomiting, diarrhea and nausea, as well as dizziness and a feeling of drowsiness. In addition, there were reports of disorders of kidney function, bradycardia with tachycardia and a decrease in pressure, and in addition to the state of coma and convulsions.
Fluvoxamine has a wide range of safety in case of intoxication. Data on the fatal outcome due to poisoning with fluvoxamine are single. The highest dosage, which was recorded in case of an overdose, is 12 g. The patient who used the dose, subsequently recovered completely. There were cases of development of severe complications with intentional overdose of Deprivox in combination with other drugs.
Fluvoxamine does not have an antidote. When poisoning with a medicine, it is necessary to perform gastric lavage as quickly as possible, and then to carry out procedures aimed at eliminating signs of disturbances, as well as maintaining the condition of the victim. Together with this, it is required to take activated charcoal, and also, if necessary, a laxative LS of an osmotic type. Procedures for hemodialysis or forced diuresis will be ineffective.
Interactions with other drugs
It is forbidden to combine medicine with MAOI (among them linezolid), because there is a possibility of developing serotonin intoxication.
The effect of fluvoxamine on oxidative metabolism of other drugs.
Fluvoxamine is able to inhibit the metabolism of those drugs that are metabolized by individual hemoprotein isoenzymes (CYP). In vitro and in vivo tests demonstrate a strong inhibitory effect of the drug relative to CYP1A2 with 2C19, but the slowing of the elements of CYP2C9 with CYP2D6, as well as CYPZA4, is less noticeable. Means that are mainly metabolized with the participation of these isoenzymes are excreted more slowly and may have increased plasma values in the case of a combination with the substance fluvoxamine.
Treatment with deprivox in combination with similar drugs must be corrected to the lowest and at the same time effective dosage. Indices inside the plasma, the effects or side effects of concomitant medication should be carefully monitored, followed by a reduction in dosage if necessary. In particular, this is important with drugs that have a narrow drug index.
The substance is ramelteon.
Taking 100 mg of fluvoxamine twice daily for a period of 3 days, and then taking a single dose of ramelteon (16 mg) together with a fluvoxamine dose caused an increase in the AUC of ramelteon by approximately 190 times compared with the latter using monotherapy. Also increased and the peak level of the drug (70 times).
Combinations with drugs that have a narrow drug index.
It is necessary to closely monitor the status of persons taking fluvoxamine along with drugs from the above category (among such theophylline with phenytoin, tacrine and cyclosporine with methadone and carbamazepine, and mexiletine). Their metabolism is carried out exclusively with the help of the CYP system or with the participation of CYP, which are slowed down by fluvoxamine. If necessary, you should change the dosage of this drug.
Neuroleptics and tricycles.
There is evidence of an increase in the plasma values of tricyclics (such as amitriptyline with clomipramine, as well as imipramine), as well as neuroleptics (including olanzapine with clozepine and quetiapine), which are mainly metabolized with the help of hemoprotein P450 1A2 in combination with fluvoxamine. It is necessary to consider the option of reducing the dosage of these drugs in the case of combining them with Deprivox.
Benzodiazepines.
In the case of combination with Deprivox, an increase in the plasma level of benzodiazepines metabolized by oxidation (among them midazolam with diazepam, as well as triazolam with alprazolam) may be observed. It is required to reduce the dosages of these agents when combined with the substance fluvoxamine.
Situations with increasing indices inside the plasma.
As a result of simultaneous use with ropinirole, an increase in the plasma level of this drug is possible, which increases the likelihood of intoxication. Therefore, in the process of therapy, it is necessary to monitor the patient's condition and reduce the dose of ropinirole, if necessary (when combined with fluvoxamine, and after the latter is discontinued).
Since the plasma values of propranolol, when combined with deprivoksom increase, you can expect to reduce the size of the dose.
Combination with warfarin leads to a significant increase in its plasma level, as well as an increase in PTV.
Situations with an increased risk of side effects.
There are separate data on the development of cardiotoxic effects in the case of combination of the drug with thioridazine.
The plasma index of caffeine can increase when combined with fluvoxamine. Possible development of side effects of caffeine (such as heart palpitations, insomnia, tremors and nausea, as well as a sense of anxiety). As a result, people who often consume caffeine-containing beverages need to reduce their intake while using fluvoxamine.
Drug Interactions.
Perhaps the potentiation of serotonergic effects when the drug is combined with other serotonergic drugs (among them are St. John's wort, tryptans, SSRIs and tramadol).
Simultaneous reception of drugs with lithium (patients who suffer from severe forms of pathology) should be performed cautiously, because lithium (and, possibly, the substance tryptophan) is capable of potentiating the serotonergic properties of fluvoxamine. Because of this, the combination of these drugs should be limited to use only in people with severe depression, resistant to therapy.
It is necessary to closely monitor the condition of people who combine Deprivox with oral anticoagulants, since in this case it is possible to increase the likelihood of bleeding.
It is necessary to refrain from drinking alcohol during the period of fluvoxamine use.
[5]
Storage conditions
Deprivox should be kept out of reach of small children. Temperature conditions - no more than 25 ° С.
[6]
Shelf life
Deprivox can be used in the period of 3 years from the date of release of the drug.
Attention!
To simplify the perception of information, this instruction for use of the drug "Deprivox" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.