Parlodel inhibits the secretion of anterior pituitary hormone – prolactin without affecting normal levels of other pituitary hormones. However, it can reduce the elevated levels of growth hormone (GH) in patients with acromegaly. This action is caused by stimulation of dopamine receptors. In postpartum prolactin is necessary to initiate and sustain lactation. In testosterone cypionate vs enanthate other periods of life increase prolactin secretion leads to pathological lactation (galaktoree) and / or disorders of ovulation and the menstrual cycle. Parlodel as a specific inhibitor of prolactin secretion, can be used for the prevention or suppression of physiological lactation, and also for the treatment of pathological conditions caused by hypersecretion of prolactin. When amenorrhea and / oranovulatory menstrual cycles (accompanied or not accompanied by galactorrhea) Parlodel can be used to restore menstrual cycles and ovulation.
In the application of Parlodel for suppression of lactation there is no need to limit fluid intake. In addition, Parlodel does not violate the postpartum uterine involution and does not increase the risk of thromboembolism. Parlodel stop growth or reduces the size of prolactin pituitary adenoma (prolactin). In patients with acromegaly, in addition to reducing the concentration of growth hormone and prolactin in plasma, Parlodel favorably influences the clinical manifestations and tolerance glucose.In Parkinson’s disease, is characterized by a specific deficiency of dopamine in the striatum and black nuclei of the brain, stimulation of dopamine receptors Parlodel can restore the neurochemical balance in the basal ganglia. Patients with Parkinson’s disease bromocriptine usually administered at higher doses than those used for endocrinological indications. Parlodel reduces a tremor, rigidity, slowness of movement and other symptoms of Parkinson’s disease at all stages of the disease. Efficacy is usually kept for many years (so far good results of therapy are described in the treatment duration up to 8 years). Parlodel reduces the severity of symptoms of depression in Parkinson’s patients. This is due to its inherent antidepressant properties, confirmed in controlled studies in patients with endogenous or psychogenic depression, not suffering from Parkinson’s disease.
Pharmacokinetics Absorption After oral bromocriptine Parlodel inside well absorbed. In healthy volunteers after oral administration in tablet form Parlodel poluabsorbtsii period of 0.2-0.5 hours, bromocriptine, bromocriptine and maximum concentration in plasma (Cmax) is achieved within 1-3 hours. When administered 5 mg of bromocriptine, Cmax of 0.465 ng / ml. Prolaktinsnizhayuschy effect starts within 1-2 hours after ingestion of the drug, peaks (decrease prolactin concentration of more than 80%) in 5-10 hours and is maintained at close to the maximum level for 8-12 hours. Distribution Relationship to plasma proteins is 96%. The metabolism of bromocriptine is extensively metabolized in the liver “first pass” with the formation of a number of metabolites. The urine and feces unchanged bromocriptine is virtually absent. Bromocriptine has a high affinity for testosterone cypionate vs enanthate.
The main route of metabolism is the hydroxylation of proline ring as part of the cyclopeptide. The simultaneous use of inhibitors and / or potential CYP3A4 substrates can lead to inhibition of bromocriptine clearance and increase its level in the blood plasma. Bromocriptine is a strong inhibitor of CYP3A4 with a calculated value of the IC50 1.69 uM. However, due to the low therapeutic concentrations of free bromocriptine in patients who are not expected significant changes in the metabolism of both the drugs, the clearance of which is carried out with the participation of CYP3A4. Excretion Excretion of unchanged bromocriptine plasma takes place bi-phase, terminal half-life is about 15 hours (8 to 20 h). Bromocriptine and its metabolites are almost completely excreted through a liver, only 6% of the dose is excreted by the kidneys. In patients with impaired liver function the rate of excretion of bromocriptine may be reduced, and the plasma levels – to rise, which requires correction dosing regime.
INDICATIONS menstrual irregularities, female infertility Prolaktinzavisimye diseases and conditions, accompanied or not accompanied by hyperprolactinemia:
Prolaktinnezavisimoe female infertility:
- Polycystic ovary syndrome
- anovulatory cycles (in addition to antiestrogens such as clomiphene).
Hyperprolactinemia in men :
- prolaktinzavisimy hypogonadism (oligospermia, loss of libido, impotence).
- Conservative treatment of prolactin pituitary micro- and macroadenomas
- preoperative preparation to reduce the volume of the tumor and facilitate its resection
- postoperative treatment if prolactin levels remain elevated.
- as an additional testosterone cypionate vs enanthate means or, in special cases, as an alternative to surgery or radiation treatment.
Suppression of lactation :
- prevention or suppression of postpartum lactation for medical reasons, including the initial stage of postpartum mastitis
- prevention of lactation after abortion
Parlodel is not recommended as a preventive measure or to reduce postpartum breast engorgement in cases where the performance of the simple analgesics and breast support.
- all stages of idiopathic Parkinson’s disease and parkinsonism postentsefaliticheskogo – either as monotherapy or in combination with other antiparkinsonian agents.
Due to the limited amount of clinical data Parlodel not recommended for the treatment of premenstrual syndrome and benign breast disease.
- Hypersensitivity to bromocriptine Parlodel or other components, or to other ergot alkaloids.
- Uncontrolled hypertension. Preeclampsia pregnancy (including eclampsia, pre-eclampsia). Hypertension during pregnancy and the postpartum period.
- Coronary heart disease and other serious cardiovascular diseases.
- Severe mental disorder testosterone cypionate vs enanthate at the moment and / or history. As the experience of the drug in children younger than 7 years limited Parlodel is not recommended in these patients.