Active substanceBromocriptineBromocriptine
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains: active substance - bromocriptine 2.5 mg (which corresponds to bromocriptine mesylate 2.87 mg); auxiliary substances: silicon dioxide colloid, disodium edetate, magnesium stearate, maleic acid, corn pregelatinized starch, corn starch, lactose monohydrate.

    Description:

    round, flat with a bevelled edge, almost white, a tablet with a risk and code "XC" on one side, with an inscription "SANDOZ" - another.

    Pharmacotherapeutic group:Dopamine receptor agonist.
    ATX: & nbsp

    N.04.B.C   Stimulants of dopamine receptors

    N.04.B.C.01   Bromocriptine

    Pharmacodynamics:

    Parlodel inhibits the secretion of the hormone of the anterior lobe of the pituitary gland - prolactin, without affecting the normal levels of other pituitary hormones. However, it can reduce elevated levels of growth hormone (STH) in patients with acromegaly.This action is due to the stimulation of dopamine receptors.

    In the postpartum period, prolactin is needed to start and maintain lactation. In other periods of life, an increase in prolactin secretion leads to pathological lactation (galactorrhea) and / or disorders of ovulation and the menstrual cycle.

    Parlodel, as a specific inhibitor of prolactin secretion, can be used to prevent or suppress physiological lactation, as well as to treat pathological conditions caused by prolactin hypersecretion. With amenorrhea and / or anovulatory menstrual cycles (accompanied or not accompanied by galactorrhea) Parlodel can be used to restore the menstrual cycle and ovulation.

    When applying Parlodela for suppressing lactation, there is no need to limit the use of liquid. In addition, Parlodel does not disrupt the postnatal involution of the uterus and does not increase the risk of thromboembolism.

    Parlodel ceases to grow or reduces the size of prolactin secreting pituitary adenomas (prolactin).

    In patients with acromegaly, in addition to reducing the concentration of STH and prolactin in plasma, Parlodel has a beneficial effect on clinical manifestations and glucose tolerance.

    In Parkinson's disease, characterized by a specific deficiency of dopamine in the region of the striatum and black nuclei of the brain, stimulation of dopamine receptors by Parlodel can restore the neurochemical balance in the basal ganglia. Patients with Parkinson's Disease bromocriptine usually prescribed in higher doses than those used for endocrinological indications.

    Parlodel reduces tremor, stiffness, slowness of movements and other symptoms of parkinsonism at all stages of the disease. The effectiveness of the drug usually persists for many years (by now, good results of therapy are described with a treatment duration of 8 years).

    Parlodel reduces the severity of symptoms of depression in patients with Parkinsonism. This is due to its inherent antidepressant properties, confirmed in controlled trials in patients with endogenous or psychogenic depression who did not suffer from Parkinsonism.

    Pharmacokinetics:

    Suction

    After taking Parlodela inside bromocriptine is well absorbed. In healthy volunteers after ingestion of Parlodela in the form of tablets, the half-absorption period of bromocriptineis 0.2-0.5 hours, and the maximum concentration of bromocriptine in the plasma (Cmax) is reached within 1-3 hours. When ingesting 5 mg of bromocriptine, Cmax is 0.465 ng / ml. Prolactin-lowering effect begins 1-2 hours after taking the drug inside, reaches a maximum (decrease in prolactin concentration by more than 80%) after 5-10 hours and remains at a level close to the maximum for 8-12 hours.

    Distribution

    The connection with plasma proteins is 96%.

    Metabolism

    Bromocriptine is subjected to intensive metabolism in the liver during the "first passage" with the formation of a number of metabolites. In urine and feces unchanged bromocriptine practically absent. Bromocriptine has a high relationship to CYP3A. The main way of metabolism is hydroxylation of the proline ring in the composition of the cyclopeptide. Simultaneous use of inhibitors and / or potential substrates CYP3A4 can lead to inhibition of clearance of bromocriptine and an increase in its level in blood plasma. Bromocriptine is a strong inhibitor CYP3A4 with calculated value IC50 1,69 խM. However, due to the low therapeutic concentrations of free bromocriptine in patients, no significant change in the metabolism of concomitant medications is expected,The clearance is carried out with the participation of CYP3A4.

    Excretion

    Excretion of unchanged bromocriptine from the plasma occurs biphasic, the final half-life is about 15 hours (8 to 20 hours). Bromocriptine and its metabolites are almost completely excreted through the liver, only 6% of the dose is excreted by the kidneys.

    In patients with impaired hepatic function, the rate of bromocriptine elimination may decrease, and plasma levels may increase, which requires correction of the dosing regimen.

    Indications:

    Violations of the menstrual cycle, female infertility

    Prolactin-dependent diseases and conditions, accompanied or not accompanied by hyperprolactinaemia:

    • amenorrhea (accompanied and not accompanied by galactorrhea), oligomenorrhea

    • luteal phase insufficiency

    • hyperprolactinemic disorders caused by drugs (eg, some psychotropic or antihypertensive drugs).

    Prolactin-independent female infertility:

    • polycystic ovary syndrome

    • anovulatory cycles (in addition to anti-estrogens, for example clomiphene).

    Hyperprolactinemia in men:
    • Prolactin-dependent hypogonadism (oligospermia, loss of libido, impotence).

    Prolactinomas:
    • conservative treatment of prolactin secreting micro- and macroadenomas of the pituitary gland

    • Preoperative preparation to reduce tumor volume and facilitate its resection

    • Postoperative treatment if the level of prolactin remains elevated.

    Acromegaly:
    • as an additional remedy or, in special cases, as an alternative to surgical or radiotherapy.

    Suppression of lactation:

    • prevention or suppression of postpartum lactation for medical reasons, including at the initial stage of postpartum mastitis

    • prevention of lactation after abortion

    Parlodel is not recommended for use as a prophylactic or to reduce postpartum engorgement of mammary glands in cases where simple analgesics and breast support are effective.

    Parkinson's disease

    • all stages of idiopathic Parkinson's disease and postencephalitic parkinsonism - either in monotherapy or in combination with other antiparkinsonian agents.

    Due to the limited amount of clinical data Parlodel is not recommended for treatmentpremenstrual syndrome and benign breast diseases.

    Contraindications:
    • Hypersensitivity to bromocriptine, or other components of Parlodel, or to other ergot alkaloids.

    • Uncontrolled hypertension. Pregnancy Gestosis (including eclampsia, preeclampsia). Arterial hypertension during pregnancy and in the postpartum period.

    • Ischemic heart disease and other, severe cardiovascular diseases.

    • Severe mental disorders at present and / or in the anamnesis.

    Since the experience of using the drug in children under 7 years of age is limited, Parlodel is not recommended for use in this category of patients.

    Carefully:

    Use in children and adolescents <18 years

    The efficacy and safety of Parlodela have been established for children and adolescents with prolaktomami and acromegaly older than 7 years. Experience in the use of the drug in children under 7 years of age is limited In clinical studies and medical practice, the tolerance of the drug in adults and children was the same. Given the difficult predictable sensitivity of children and adolescents, caution should be exercised in prescribing a drug in this category of patients.

    Patient use> 65 years

    The number of patients 65 years of age or older in clinical trials was not sufficient to assess the possible differences in the response to Parlodel treatment compared to younger patients. However, in clinical trials and medical practice, tolerability of the drug in patients> 65 years and younger was the same. Given the difficult predictable tolerability of the drug in persons> 65 years of age, caution should be exercised in prescribing a drug in this category of patients.

    Application in the puerperium

    In women who took Parlodel in the puerperium for the suppression of lactation, there were rare cases of serious adverse events: hypertension, myocardial infarction, seizures, stroke or mental disorders. In some patients, development of seizures or cerebrovascular disorders was preceded by severe headaches and / or transient visual impairment. Although the cause-and-effect relationship of these phenomena with Parlodela is not established, in women taking the drug in the puerperium to suppress lactation, as well as in patients receiving Parlodel for any other indications, it is necessary to control blood pressure (BP).With the development of hypertension or severe, progressive or persistent headache (accompanied and not accompanied by visual impairment) or signs of abnormal CNS, Parlodel should be abolished and immediately monitored by the patient.

    Particular care should be taken when administering Parlodel to patients who have recently received or continue to take drugs that affect blood pressure, such as vasoconstrictors (sympathomimetics or ergot alkaloids, including ergometrine or methylergomethrin). Women in the postpartum period do not recommend the simultaneous use of parlodela with vasoconstrictive drugs.

    Pregnancy and lactation:

    In patients who want to become pregnant, after the pregnancy is confirmed, Parlodel, like other medicines, should be withdrawn, except for the need to continue therapy for medical reasons. The abolition of Parlodela during pregnancy did not lead to an increase in the incidence of its spontaneous interruption. Clinical experience shows that the use of Parlodel during pregnancy does not adversely affect its course or outcome.

    If Parlodel is withdrawn in pregnant women with pituitary adenoma, careful monitoring of the patients throughout the gestation period is necessary. In case of signs of pronounced increase in prolactinoma, for example, headaches or narrowing of the visual fields, Parlodel treatment can be resumed or performed surgical intervention.

    Since Parlodel suppresses lactation, it should not be administered to nursing mothers.

    Dosing and Administration:

    Parlodel should be taken orally during meals.

    Violations of the menstrual cycle, female infertility

    Assign 1.25 mg (1/2 tablet) 2-3 times a day; if the effect is insufficient, the dose of the drug is gradually increased to 5-7.5 mg per day (folding dose 2-3 times / day). Treatment continues until the menstrual cycle is normalized and / or ovulation is restored.

    If necessary, to prevent relapses, treatment can be continued for several cycles.

    Hyperprolactinemia in men

    Assign 1.25 mg (1/2 tablet) 2-3 times a day, gradually increasing the dose to 5-10 mg (2-4 tablets) per day.

    Prolactinomas

    Assign 1.25 mg (1/2 tablets) 2-3 times a day with a gradual increase in dose and the selection of dosage, providing an adequate decrease in the concentration of prolactin in the plasma.The maximum recommended dose for children and adolescents aged 7-12 years is 5 mg / day, for the age of 13-17 years - 20 mg.

    Acromegaly

    The initial dose is 1.25 mg (1/2 tablet) 2-3 times a day, further, depending on the clinical effect and tolerability, the daily dose of the drug is gradually increased to 10-20 mg (4-8 tablets). The maximum recommended dose for children and adolescents aged 7-12 years is 10 mg / day, for the age of 13-17 years - 20 mg.

    Suppression of lactation for medical reasons

    On the first day, 1.25 mg (1/2 tablet) is prescribed 2 times (during meals at breakfast and dinner), then for 14 days - 2.5 mg (1 tablet) 2 times a day. To prevent lactation, the drug should be taken several hours after birth or abortion, but only after stabilizing vital functions. After 2 or 3 days after drug withdrawal, there is sometimes a slight secretion of milk. It can be eliminated by recommencing the drug at the same dose for another 1 week.

    Beginning postpartum mastitis

    On the first day, 1.25 mg (1/2 tablet) is prescribed 2 times (during meals at breakfast and dinner), then for 14 days - 2.5 mg (1 tablet) 2 times a day. Additionally, an antibiotic is prescribed.

    Parkinson's disease

    In order to ensure optimal tolerability during the first week, treatment should begin with a low dose of 1.25 mg (1/2 tablet) once a day (preferably in the evening). To select an individual minimum effective dose, increase the amount of the drug taken slowly, by the "titration" method. The dose of the drug is increased gradually - every day the daily dose is increased by 1.25 mg; The daily dose is divided into 2-3 doses. An adequate therapeutic response is achieved on average for 6-8 weeks of treatment. In the absence of clinical effect after 6-8 weeks of use, it is possible to further increase the daily dose by 2.5 mg every week.

    Typically, the therapeutic range of doses of bromocriptine for mono- or combination therapy is 10 mg to 40 mg per day, but some patients may require higher doses.

    If unwanted reactions occur during the selection of a dose, the daily dose should be reduced and maintained at a lower level for at least 1 week. When reversing side effects, the dose of the drug can be raised again.

    Patients with impaired movement on the background of taking levodopa, it is recommended to lower the dose of levodopa before the application of Parlodela.After achieving a satisfactory clinical effect in the treatment of Parlodel, a further gradual decrease in the dose of levodopa can be made. In some patients taking Parlodel, complete cancellation of levodopa is possible.

    Side effects:

    Below are the undesirable reactions listed by the frequency of their development, starting with the most frequent. The frequency of unwanted reactions is estimated as follows: very often (> 1/10); often (> 1/100, <1/10); sometimes (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000), including individual messages:

    Mental disorders:

    Sometimes: confusion, psychomotor agitation, hallucinations;

    Rarely: psychotic disorders, insomnia.

    Rarely: increased libido, hypersexuality

    From the side of the central nervous system:

    Often: headache, drowsiness, dizziness;

    Sometimes: movement disorders;

    Rarely: drowsiness, paresthesia;

    Rarely: increased drowsiness during the day, sudden falling asleep.

    From the sense organs:

    Rarely: impaired vision, blurred vision, tinnitus.

    From the cardiovascular system:

    Sometimes: arterial hypotension, orthostatic hypotension (very rarely leading to fainting);

    Rarely: effusion to the pericardium, constrictive pericarditis, tachycardia, bradycardia, arrhythmia. Rarely: fibrosis of the heart valves, reversible paleness of the fingers and toes caused by hypothermia (especially in patients with Raynaud's syndrome in the anamnesis).

    From the respiratory system, chest and mediastinum:

    Often: nasal congestion;

    Rarely: pleural effusion, pleural fibrosis, pleurisy, pulmonary fibrosis, dyspnea.

    From the digestive system:

    Often: nausea, constipation, vomiting;

    Sometimes: dry mouth;

    Rarely: diarrhea, abdominal pain, retroperitoneal fibrosis, gastrointestinal ulcers, gastrointestinal bleeding (black feces, blood in vomit masses).

    From the skin and subcutaneous tissue:

    Sometimes: allergic skin reactions, hair loss.

    From the side of the musculoskeletal system and connective tissue:

    Sometimes: cramps calf muscles.

    Common violations and uyeakii at the place of introduction:

    Sometimes: increased fatigue;

    Rarely: peripheral edema;

    Rarely: in the case of a sharp reversal of Parlodela development of a condition similar to a malignant neuroleptic syndrome.

    In the application of Parlodel in high doses (as well as other dopamine agonists), reversible changes in sexual behavior, increased libido and hypersexuality, which disappeared after lowering the dose of the drug or stopping treatment, were rarely noted.

    Application Parlodela for suppression of physiological lactation in the postpartum period in rare cases was accompanied by the development of arterial hypertension, myocardial infarction, seizures, stroke or mental disorders.

    Overdose:

    In all cases, when there was an overdose of only Parlodel, there were no lethal outcomes. The maximum once-accepted dose of Parlodel, known to date, is 325 mg. In case of an overdose, nausea, vomiting, dizziness, arterial hypotension, postural hypotension, tachycardia, drowsiness, drowsiness, lethargy, hallucinations were observed.

    When Parlodela was accidentally taken in by children (isolated reports), vomiting, fever, and drowsiness were noted. Improvement of patients' condition occurred spontaneously or several hours after the appropriate therapy.

    In case of an overdose, it is recommended to take Activated carbon; it is possible to perform gastric lavage immediately after taking the drug.

    Treatment of acute poisoning is symptomatic. To stop vomiting or hallucinations can be appointed metoclopramide.

    Interaction:

    Bromocriptine is both a substrate and an inhibitor of the enzyme CYP3A4. Care should be taken when concomitant administration of bromocriptine and other inhibitors and / or substrates CYP3A4 (azole antimycotics, HIV protease inhibitors). Simultaneous reception of macrolide antibiotics and Parlodela ( erythromycin or josamycin) causes an increase in the concentration of bromocriptine in the blood plasma. Simultaneous use of octreotide and bromocriptine in patients with acromegaly is accompanied by an increase in the level of the latter in blood plasma.

    The therapeutic efficacy of bromocriptine, associated with the stimulation of central dopamine receptors, may be reduced by the use of dopamine antagonists

    receptors, such as antipsychotics (phenothiazines, butyrophenones and thioxantines), as well as metoclopramide and domperidone.

    Portability of parlodel may decrease with the use of alcohol.

    Simultaneous appointment of Parlodela with antihypertensive drugs can lead to increased severity of blood pressure lowering.

    Parlodel can be administered either as monotherapy or in combination with other antiparkinsonian agents (both in the early and late stages of the disease). Combination with levodopa leads to an increased antiparkinsonian action, which often makes it possible to reduce the dose of levodopa. The use of parodel in patients receiving levodopa treatment is particularly useful when the therapeutic effect of levodopa is weakened or when complications such as pathological involuntary movements (choreo-athetoid dyskinesia and / or painful dystonia) develop, the effect is depleted by the end of the dose of levodopa, the phenomenon of " off " ("on-off).

    Special instructions:

    Treatment Parlodel can restore the ability to procreate. Therefore, women of childbearing age who do not want pregnancy, should use a reliable method of contraception.

    Women with a pathology that is not associated with hyperprolactinemia, Parlodel should be prescribed in the effective minimum dose necessary for relief of symptoms.This is important to prevent a decrease in the concentration of prolactin in the plasma below the normal level, which leads to a violation of the function of the yellow body.

    During Parlodel treatment, careful monitoring of patients with a history of peptic ulcer is necessary.

    A careful examination and monitoring of patients with pleuropulmonary diseases of unclear etiology and discontinuation of Parlodel therapy in the course of progression of the disorders is necessary.

    For early diagnosis of retroperitoneal fibrosis at the reversible initial stage of the process, the doctor is recommended to monitor the manifestation of such symptoms as back pain, swelling of the lower limbs, impaired renal function. Parlodel should be discontinued with confirmed fibrotic changes in the retroperitoneal space or suspected of their presence.

    The use of prolactin secreting adenomas

    Since patients with pituitary macroadenomas may exhibit signs of hypopituitarism as a result of compression or destruction of the pituitary gland, a full functional assessment of the pituitary gland and appropriate substitution therapy should be performed prior to the appointment of Parlodel.In patients with secondary adrenal insufficiency, it is necessary to carry out glucocorticosteroid replacement therapy.

    Patients with macropenomas of the pituitary gland should constantly evaluate the dynamics of tumor size. With the increase of the tumor, surgical methods of treatment are possible. Careful surveillance of pregnant patients, previously treated with Parlodel about prolactin pituitary adenoma, as during pregnancy may increase the size of the tumor. In such patients Parlodel treatment often leads to a decrease in tumor size and rapid positive dynamics from defects in the visual fields. In severe cases, with the development of compression of the visual or other cranial nerves, urgent surgical intervention on the pituitary gland is possible.

    A known complication of macroprolactin is the loss of visual fields. Effective treatment Parlodel reduces hyperprolactinemia and eliminates visual field disturbances. Nevertheless, in some patients, secondary changes in the visual fields are possible, despite the normalization of prolactin levels and the reduction in tumor size.This may be due to the displacement of the visual crosshair down, due to the release of the volume in the area of ​​the Turkish saddle. In this case, a decrease in the dose of bromocriptine, which leads to an increase in the level of prolactin and an increase in the tumor size to some extent, can contribute to the elimination of visual field defects. In this regard, monitoring of visual fields in patients with macroprolactinoma is indicated for the early detection of secondary fallout of visual fields caused by the spatial protrusion of the visual crossover into the cavity of the saddle and adaptation to the action of a given dose of the drug.

    Some patients with prolatin secreting adenomas taking Parlodel had cases of cerebrospinal rhinorrhea. According to the results of clinical studies, cerebrospinal rhinorrhea may be caused by a decrease in the volume of invasive tumors. Patients with rare hereditary forms of intolerance to galactose, severe lactase deficiency, malabsorption of glucose-galactose, Parlodel should not be taken.

    Effect on the ability to drive transp. cf. and fur:

    Patients receiving Parlodel should be especially careful when driving vehicles or when working with mechanisms,as against the background of the use of the drug, especially during the first days of treatment, arterial hypotension may result, leading to a decrease in the rate of reactions.

    During the period of treatment, Parlodel noted drowsiness and episodes of sudden falling asleep, especially in patients with Parkinson's disease. Episodes of sudden falling asleep against the background of daytime wakefulness, arising without previous drowsiness, were noted extremely rarely. Before the appointment of Parlodel, the physician should inform the patient of the indicated risk factors and recommend refraining from driving vehicles, controlling the mechanisms, and also by engaging in other potentially hazardous activities requiring increased attention and speed of response. With the development of severe drowsiness or the appearance of episodes of sudden falling asleep, you should reduce the dose of the drug or completely abolish it.

    Form release / dosage:

    Tablets 2.5 mg

    Packaging:

    10 pieces. in the blister pack. 3 blisters together with instructions for use in a cardboard bundle.

    30 pcs. in the bottle of dark glass. 1 bottle with instructions for use in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    The drug should be stored out of the reach of children.

    Shelf life:

    3 years.

    Terms of leave from pharmacies:On prescription
    Registration number:П N015275 / 01
    Date of registration:11.08.2008
    Date of cancellation:2017-04-04
    The owner of the registration certificate: Meda AB Meda AB Sweden
    Manufacturer: & nbsp
    MEDA, AB Sweden
    Information update date: & nbsp04.04.2017
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