International nonproprietary name:
1 tablet contains: active substance parabolan dosage 0.5 mg Excipients: lactose, L-leucine, magnesium stearate (E572)
Description: white flat oval tablets with a facet and Valium on one side, engraved with “0.5” on one side of the risks and “CBG” – on the other.
dopamine receptor agonist
ATX code: G02CB03.
parabolan dosage – synthetic ergot alkaloid derivative ergoline dopamine agonist is a long acting inhibiting prolactin secretion. The mechanism of action of parabolan dosage includes stimulation of central dopamine receptors of the hypothalamus. At doses higher than those required for suppression of prolactin secretion, the drug is a central dopaminergic effect due to stimulation of the dopamine D2-receptor. The drug has a dose-dependent manner. Decreasing the amount of prolactin in blood is usually observed after 3 hours and maintained for 2-3 weeks, and therefore to suppress the secretion of milk is usually sufficient single dose of the drug. In the treatment of hyperprolactinemia blood prolactin normalized after 2-4 weeks of application in the effective drug dose. Normal prolactin levels may persist for several months after discontinuation of the drug.
parabolan dosage has a highly selective effect and no effect on basal secretion of other pituitary hormones and cortisol. The only pharmacodynamic effect is not related to mibolerone the therapeutic effect is the reduction of blood pressure (BP). The maximum antihypertensive effect usually develops within 6 hours after a single dose of the drug; the degree of decrease in blood pressure and the incidence of dose-dependent hypotensive effect.
Pharmacokinetics Absorption After oral administration parabolan dosage is rapidly absorbed from the gastrointestinal tract (GIT). Maximum plasma concentration is achieved within 0.5-4 hours. Food does not affect the absorption or distribution of parabolan dosage. Distribution Binding of parabolan dosage (at a concentration of 0.1-10 ng / ml) to plasma proteins is 41-42%. Metabolism In urinary metabolites detected parabolan dosage:. b-allyl-8p-carboxy-ergoline in an amount of 4-6% of the dose, and three other metabolite with a total content of less than 3% of all metabolites in a much lesser degree (compared with parabolan dosage) inhibit secretion prolactin.Excretion
parabolan dosage has a long half-life: T ½ was 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinemia.
In this half-life equilibrium state is reached after 4 weeks. The urine and feces revealed respectively, 18% and 72% of the dose. Contents parabolan dosage unchanged in urine is 3.2%.
The pharmacokinetics is linear up to a dose of 7 mg / day. Pre-clinical safety data , as shown in preclinical studies, parabolan dosage secure a considerable range of doses and has no teratogenic, mutagenic or carcinogenic effects.
- Suppression physiological postpartum lactation (only for medical reasons).
- Suppression already established lactation (only for medical reasons).
- Disturbances associated with hyperprolactinemia (including functional disorders like amenorrhea, oligomenorrhea, anovulation, galactorrhoea).
- Prolactin pituitary adenomas (micro- and macroprolactinoma).
- Postpartum or uncontrolled hypertension.
- Hypersensitivity to parabolan dosage, other ergot alkaloids or to any component of the drug.
- Severe liver dysfunction.
- Adverse events in the lungs, such as pleurisy or fibrosis (including history) associated with the intake of dopamine agonists.
- Psychoses (including history) or the risk of development.
- Pregnancy and develop its pre-eclampsia and eclampsia.
Efficacy and safety of parabolan dosage in children under 16 years of age has not been studied.
Precautions: in patients with cardiovascular disease, hypotension, Raynaud’s syndrome, peptic ulcer or gastrointestinal bleeding, in patients with end-stage renal disease on hemodialysis, or in elderly patients.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation.
To exclude pregnancy before you start taking the drug. It is recommended to avoid pregnancy for at least 1 month after cessation of treatment. . Limited data are available for receiving the drug during pregnancy, obtained during the first 8 weeks after conception. The use of parabolan dosage has not been accompanied by an increased risk of abortion, premature delivery, multiple pregnancy or congenital abnormalities. Other data has not yet been received.
In animal studies, direct or indirect adverse effects of parabolan dosage on pregnancy, embryo / fetal, parturition or postnatal development were found.
Given the limited experience with the use of parabolan dosage in pregnancy, when it is planning drug should be discontinued. In case of pregnancy during treatment with parabolan dosage immediately overturned. In connection with the expansion of pre-existing tumors should be monitored signs of increased pituitary gland in pregnant women.
Because parabolan dosage inhibits lactation, the drug should not be administered to mothers who choose to breast-feeding infants. During treatment with parabolan dosage should stop breastfeeding.
Dosage and administration
parabolan dosage is taken orally, preferably during meals. Adults Treatment of disorders associated with hyperprolactinemia recommended initial dose – 0.5 mg per week in one or two divided doses (eg on Monday and Thursday). The dosage is gradually increased, usually 0.5 mg / week at intervals of 1 month to achieve optimum therapeutic effect. Maintenance dose – 1 mg / week (0.25 – 2 mg / week); . in some cases, patients with hyperprolactinemia to 4,5 mg / week when using the drug in doses greater than 1 mg / week, it is recommended to divide the weekly dose by 2 or more receptions depending on tolerability. For the suppression of lactation: the recommended dose – 1 mg once daily within the first 24 hours after birth. use in patients with impaired hepatic or renal function The information presented in the “contraindications” and “special instructions”. use in the elderly Given the indications for use, experience with parabolan dosage in elderly patients is limited. Available data show no specific risks.
Unwanted effects are usually dose-dependent and decreases with its gradual decline. Suppression of lactation: adverse events develop in approximately 14% of patients. The most common: reduction in blood pressure (12%), dizziness (6%) and headache (5%). Long-term treatment increases the frequency of these effects up to 70%. Frequent (more than 1/100, less than 1/10) of the nervous system: . Depression, headache and dizziness, paresthesia, fatigue, somnolence From the cardiovascular system (CVS ): low blood pressure, palpitations and chest pain. On the part of the digestive tract: nausea, vomiting, gastralgia, gastritis, constipation. Skin and subcutaneous tissue:. Hyperemia skin Uncommon (more than 1/1000, less than 1/100) From the side view: hemianopsia. From the CCC: . Epistaxis Rare (more than 1/10000, less than 1/1000) : Allergic reaction : skin rash. From the CCC: fainting. From the musculoskeletal system: cramps in the fingers and calves. on the part of the digestive tract: abnormal liver function. blood pressure reduction (systolic over 20 mm Hg and diastolic by more than.. 10 mm Hg. Art.) noted 3-4 days after a single dose of parabolan dosage at a dose of 1 mg in women after childbirth.Adverse events usually occur within the first two weeks, then decrease or disappear. Cancel the drug due to side effects was required in 3% of cases. Post-marketing surveillance parabolan dosage treatment was accompanied by excessive daytime sleepiness and episodes of suddenly falling asleep, particularly in patients with Parkinson’s disease. There are reports of increasing libido in patients with Parkinson’s disease with dopamine agonists in the treatment including parabolan dosage, especially at high doses. Also observed in the treatment of parabolan dosage pleural effusions, pleural fibrosis, valvulopatiya, respiratory disorders (including respiratory failure).
Data on overdose are not present. Based on the results of animal experiments, we can expect the appearance of symptoms caused by hyperstimulation of dopamine receptors: nausea, vomiting, decreased blood pressure, impaired consciousness / psychosis or hallucinations. If shown, it should take steps to restore blood pressure. Furthermore, in severe CNS symptoms (hallucinations) may require the use of dopamine antagonists.
Interaction with other drugs
Effect of macrolide antibiotics on parabolan dosage plasma levels when used together has not been studied. Given the possibility of increasing the level of parabolan dosage, the drug is not recommended for use in combination with macrolides.
The mechanism of action of parabolan dosage is associated with the direct stimulation of dopamine receptors, so it should not be used in combination with antagonists of dopamine receptors (phenothiazines, butyrophenones, thioxanthenes, metoclopramide).
No information is available about the interaction parabolan dosage with other ergot alkaloids, however, not recommended for long-term use of such a combination.
Given the pharmacodynamics of parabolan dosage (hypotensive effect), it is necessary to take into account the interaction with drugs that reduce blood pressure.
In clinical studies in patients with Parkinson’s disease pharmacokinetic interaction with levodopa, or selegiline were found. Pharmacokinetic interactions with other drugs on the basis of the available information about the metabolism of parabolan dosage is impossible to predict.
To open the bottle, first click on the cover, and then turn it as shown on the cover. The capsule with the bottle of silica is not removed and not eat inside.
The data on the efficacy and safety of parabolan dosage in patients with impaired hepatic or renal function is limited. The pharmacokinetics of parabolan dosage has not changed significantly in moderate or severe renal insufficiency. It has not been studied in patients with end-stage renal failure or dialysis. Therefore, in these patients the drug should be used with caution. The effects of alcohol on overall tolerability of parabolan dosage has not been established.
parabolan dosage can cause symptomatic hypotension, especially when co-administered with drugs that reduce blood pressure. It is recommended to regularly measure blood pressure in the first 3-4 days after initiation of treatment.
Hyperprolactinemia in conjunction with amenorrhea and infertility may be associated with pituitary tumors, so before treatment with parabolan dosage is necessary to find out the cause of hyperprolactinemia.
We recommend checking the content of prolactin in the blood serum of each month, as after achieving an effective therapeutic regimen normal prolactin level is maintained for 2-4 weeks.
after the cancellation of hyperprolactinemia drug usually occurs again. However, some patients experience a persistent decline in prolactin concentrations in a few months.
parabolan dosage restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Because pregnancy can occur before the resumption of menstruation, pregnancy tests are recommended during the period of amenorrhea, and after the restoration of the menstrual cycle – in all cases of delays of more than 3 days. Women who do not want to get pregnant, it is recommended to use effective non-hormonal contraception during treatment with parabolan dosage and after its completion. Women planning a pregnancy, it is recommended to conceive not earlier than 1 month after discontinuation of the drug. A number of patients ovulatory cycle was maintained for 6 months after discontinuation of the drug.
With prolonged use of parabolan dosage, as well as other ergot derivatives, pleural effusions may appear / pulmonary fibrosis and valvular heart disease. Sometimes these events occurred in patients previously treated with dopamine agonists of the ergot group. Cancel parabolan dosage in the case of the development of this pathology leads to an improvement of signs and symptoms.
In case of new clinical symptoms of the respiratory system is recommended X-ray light. Patients with pleural effusion / fibrosis was an increase in erythrocyte sedimentation rate (ESR), in this regard, at an elevated ESR, without overt clinical signs should also conduct X-ray examination. When using parabolan dosage and drowsiness may occur sudden episodes of sleep, especially in patients with Parkinson’s disease. Sudden falling asleep during daily activities, in some cases develops without warning, is rare.
The drug contains lactose. Patients with rare hereditary form of galactose intolerance, lactase deficiency or malabsorption of glucose-galactose should not take parabolan dosage.
Effects on ability to drive a car, and management mechanisms parabolan dosage reduces blood pressure, which may interfere with the reaction rate in some patients. This must be taken into account in situations requiring concentration, such as driving a car or operating machinery. Patients should be informed of the need to observe caution when driving or operating machinery.
Patients have been observed drowsiness and / or episodes of sudden sleep with parabolan dosage treatment, have to give up the car or other driving-related risk of the activity, when disturbances of the reaction rate can be for them and others at risk of serious injury or death. Sometimes it is advisable to decrease the dosage or withdrawal of the drug.
Product form tablets 0.5 mg. At 2 and 8 tablets in dark glass vials (type III) with a neck sealed by a membrane of aluminum foil and film (polyester / polyethylene), HDPE with a lid equipped with a system of opening against children vial contains cylindrically shaped capsule with silica gel and seal of cotton. 1 bottle with instruction for use in a cardboard box.