Norprolac - instructions for use, dose, side effects, contraindications

Active substanceHinagolideHinagolide

Similar drugsTo uncover

Norprolac®

pills inwards

Ferring Artsynmittel GmbH Germany

Dosage form: & nbspPills

Composition:

1 tablet of 25 mcg contains:

active substance: quinagolide hydrochloride 27.3 μg (equivalent to 25 μg quinagolide).

Excipients: lactose monohydrate 89.908 mg microcrystalline cellulose 24.0 mg Corn starch 12.0 mg, 3.0 mg of hypromellose, 0.7 mg of magnesium stearate, colloidal silicon dioxide 0.3 mg Iron oxide red colorant 0.065 mg.

1 tablet of 50 mcg contains:

active substance: quinagolide hydrochloride 54.6 μg (equivalent to 50 μg quinagolide).

Excipients: lactose monohydrate 89.82 mg, cellulose

microcrystalline 24.0 mg, 12.0 mg of corn starch, 3.0 mg of hypromellose, 0.7 mg of magnesium stearate, silica colloidal 0.3 mg, 0.125 mg of indigo.

1 tablet 75 mcg contains:

active substance: quinagolide hydrochloride 81.9 μg (equivalent to 75 μg quinagolide).

Excipients: lactose monohydrate 86.993 mg, cellulose microcrystalline 25.80 mg corn starch 12.9 mg hypromellose 3.225 mg magnesium stearate 0.7 mg, silicon dioxide colloidal 0,3 mg.

1 tablet of 150 mcg contains:

active substance: quinagolide hydrochloride 163.8 μg (equivalent to 150 μg quinagolide).

Excipients: lactose monohydrate 173.97 mg, cellulose microcrystalline 51.6 mg, corn starch 25.8 mg, hypromellose 6.45 mg, magnesium stearate 1.4 mg, silicon dioxide colloid 0.6 mg.

Description:

Tablets 25 mcg: round, flat, with a beveled edge of light pink color (blotches of a darker color are allowed), with engraving "Norprolac" (radially) on one side and "25" (linearly) on the other.

Tablets 50 mcg: round, flat, with bevelled edge of light blue color (blotches of a darker color are allowed), with engraving "Norprolac" (radially) on one side and "50" (linearly) on the other.

Tablets 75 mcg: round, flat, with bevelled edge of white or almost white color and engraving "Norprolac" (radially) on one side and "75" (linearly) on the other.

Tablets 150 mcg: round, flat, with bevelled edge of white or almost white color and engraving "Norprolac" (radially) on one side and "150" (linear) on other.

Pharmacotherapeutic group:Dopamine receptor agonist

ATX: & nbsp

G.02.C.B.04 Hinagolide

Pharmacodynamics:Hinagolide is a selective dopamine D2 receptor agonist, not belonging to the chemical group of ergot derivatives. Due to its dopaminergic properties,the drug has a strong inhibitory effect on the secretion of prolactin in the anterior lobe of the pituitary gland, while not reducing the normal concentration of other pituitary hormones. In some patients, a decrease secretion, prolactin can short-term increase in the concentration of growth hormone in the blood plasma. The clinical significance of this phenomenon is unknown. Hinagolide, as an inhibitor of prolonged-release prolactin secretion, is effective in appointment once a day to patients from hyperprolactinemia, leading to a decrease in the severity of such clinical symptoms like galactorrhea, oligomenorrhoea, amenorrhea, infertility and decreased libido. It was found that prolonged treatment with quinagolide leads to a decrease in the size or arrest of growth of the prolactin secretant micro- and macroadenomas of the pituitary gland. Clinically significant decrease in prolactin concentration in the blood occurs after 2 hours after taking the drug, reaches a maximum in 4-6 hours and persists about 24hours.The direct dependence of the duration of action of quinagolide on magnesium was establishedits dose, while there is no such dependence for the prolactin reducing effect. The maximum prolactin inhibitory effect was noted after a single application of a dose of 50 mcg. An increase in the effect was observed not with an increase in the dose, but with an increase in the duration of use.

Pharmacokinetics:

After a single ingestion of the drug labeled with a radioactive label, its active substance quinagolide quickly and well absorbed from the gastrointestinal tract. The plasma concentrations measured for quinagolide and its metabolites by non-selective radioimmunoassay (RIA) were close to the threshold for quantitation and can not be used as a source of reliable information. After a single ingestion of the drug labeled with a radioactive label, the apparent volume of distribution of quinagolide is about 100 liters. The association of quinagolide with plasma proteins is about 90%. Hinagolide is largely metabolized by the "first pass" through the liver. Possessing biological activity quinagolide and its N-desethylated analogs are detected in the blood in small amounts.Their inactive conjugates with sulfuric and glucuronic acids circulate in the blood in more significant amounts. More than 95% of quinagolide is excreted from the body in the form of metabolites with feces and urine in approximately equal amounts. The main metabolites found in urine are conjugated sulfate and glucononide quinagolide and quinagolide analogues - N-desethyl- and N, N-didezetyl derivatives. In feces unconjugated forms of these substances. The half-life of unchanged quinagolide after a single dose is 11.5 hours when the equilibrium state is reached - 17 hours.

Indications:

Hyperprolactinemia (idiopathic or induced by prolactin secretion of micro- or macroadenoma of the pituitary gland).

Contraindications:

Hypersensitivity to the active substance or components of the drug. Impaired kidney or liver function. Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption. Children's age (up to 18 years).

Carefully:

Caution should be used Norprolak® in patients with mental illness, including in history. Experience with Norprolak® in elderly patients is lacking.

Pregnancy and lactation:

The results of animal studies indicate the absence of embryotoxic or teratogenic action in the preparation of Norprolac®, but experience with its use in pregnant women is still limited. Patients wishing to maintain a pregnancy in the event of its onset, taking Norprolac® should be discontinued, except when continued treatment is vital. The discontinuation of Norprolac® did not result in an increase in the number of spontaneous abortions. In the case of the withdrawal of the drug Norprolak® when pregnancy occurs in a patient with pituitary adenoma, careful monitoring of the patient throughout the gestation period is indicated. Since Norprolac® suppresses lactation, breastfeeding is usually not possible. If, however, during lactation with Norprolak®, lactation continues, breast-feeding is not recommended, since it is not known whether quinagolide with breast milk.

Dosing and Administration:

Given the possibility of developing orthostatic hypotension due to dopaminergic stimulation, the dose of the drug Norprolak® to the therapeutic should be increased gradually, starting treatment with the application of the "starting" package.It is preferable to take Norprolac® at night before going to bed, with a small amount of food. Adults: The optimal dose should be selected individually, based on the degree of decrease in prolactin concentration in the blood plasma and tolerability. Treatment begins with the use of "starter" packaging. In the first 3 days the drug is prescribed in a dose of 25 mcg / day (pills of light pink color); in the following 3 days - at a dose of 50 mcg / day (pills of light blue color). Starting from the 7th day onwards, the recommended dose is 75 μg / day. If necessary, further gradual increase of the dose (but not more often than once a week) until the optimal therapeutic effect is achieved. The maintenance dose is 75-150 μg / day. In 1/3 of patients, a daily dose of 300 μg / day or more is necessary.

In such cases, the daily dose of the drug can be increased by 75-150 μg, but not more often than once in 4 weeks until a satisfactory therapeutic effect is achieved or until the tolerance of the drug worsens, which may require a break in treatment. Children and elderly patients: No experience of use.

Side effects:

Adverse reactions described with the administration of the drug Norprolak®, are characteristic for dopamine receptor agonists. Usually they are not expressed so severely as to lead to the withdrawal of the drug, and tend to disappear when continuing treatment.

	Often (< 10 %)	Often (> 1% and <10%)	Rarely (> 0.01% and <1.0%)
From the nervous system	Headache, dizziness	Insomnia	Sudden sleep, acute psychosis
From the side of the cardiovascular system		Reduction of blood pressure
From the digestive system	Nausea, vomiting	Anorexia, abdominal pain, constipation or - diarrhea
Other	Weakness	"Tides", nasal congestion

Overdose:

Data on overdose are absent. It can be expected that it will be accompanied by severe nausea, vomiting, headaches, dizziness, drowsiness, lowering of blood pressure and, possibly, collapse. Also, the appearance of hallucinations is likely. Treatment should be symptomatic

Interaction:

To date, no interaction has been reported with Norprolac® with other drugs. There is a theoretical possibility,that with the simultaneous use of Norprolak® and powerful dopamine receptor blockers (eg, antipsychotics), the ability of the first to inhibit the secretion of prolactin may decrease. In this regard, with the simultaneous use of these drugs should be careful. Drinking alcohol impairs the tolerability of the drug Norprolak®.

Special instructions:

Treatment with adenomas with Norprolac does not replace surgery! Against the background of treatment with the drug Norprolak®, it is possible to restore the childbearing function, oppressed hyperprolactics. If pregnancy is undesirable, adequate contraceptive methods should be used during therapy. To prevent nausea and vomiting, if necessary, a dopamine antagonist may be used, for example, domperidone, which is prescribed at least 1 hour before taking Norprolac®. In the first days of therapy, as well as increasing the dose of the drug is recommended to regularly monitor blood pressure in the horizontal and vertical positions of the body in connection with the possibility of developing orthostatic hypotension and fainting.When prescribing Norprolac®, like any other dopamine receptor agonist, it is necessary to prevent patients, especially those suffering from Parkinson's, of the possibility of a narcolepsy attack (sudden falling asleep). In patients with mental illness, taking Norprolak® can cause acute psychosis. In patients with Parkinson's disease, the development of pathological gambling (gambling addiction, gambling), increased libido is possible with high doses of the drug "Norprolak®." These undesirable events go away independently when the dose is lowered or the drug is withdrawn.

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

Since sometimes, against the background of treatment, especially in the early days, there may be drowsiness, a decrease in the rate of motor and mental reactions, hypotension, patients should be especially careful when driving vehicles and controlling mechanisms, and in some cases should not drive vehicles and / or participate in the mechanized production process.

Form release / dosage:Pills 25 mcg, 50 μg, 75 μg, 150 μg

Packaging:Tablets 25 μg + 50 μg ("Start" packaging): 3 tablets of 25 μg and 3 tablets of 50 μg each in a PVC / Al blister (6 tablets in a blister pack). 1 blister together with instructions for use in a cardboard pack. Tablets 75 mcg and 150 mcg: 10 tablets per blister of PVC / Al. For 3 blisters together with instructions for use in a cardboard bundle.

Storage conditions:

At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

5 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012402 / 01

Date of registration:10.10.2011

The owner of the registration certificate:Ferring Artsynmittel GmbHFerring Artsynmittel GmbH Germany

Manufacturer: & nbsp

NOVARTIS PHARMACEUTICALS UK, Ltd. United Kingdom

Information update date: & nbsp16.09.2015

Illustrated instructions

Instructions

Norprolac® (Norprolac® )