Norprolak

General characteristics. Structure:

Active agent: хинаголид (in the form of a hydrochloride) 25 mkg

Excipients: silicon dioxide colloid anhydrous, magnesium stearate, methylhydroxypropyl cellulose, starch corn, cellulose microcrystallic, lactose, ferrous oxide red.

Active agent: хинаголид (in the form of a hydrochloride) 50 mkg

Excipients: silicon dioxide colloid anhydrous, magnesium stearate, methylhydroxypropyl cellulose, starch corn, cellulose microcrystallic, lactose, indigotin.

Active agent: хинаголид (in the form of a hydrochloride) 75 mkg

Excipients: silicon dioxide colloid anhydrous, magnesium stearate, methylhydroxypropyl cellulose, starch corn, cellulose microcrystallic, lactose.

Active agent: хинаголид (in the form of a hydrochloride) 150 mkg

Excipients: silicon dioxide colloid anhydrous, magnesium stearate, methylhydroxypropyl cellulose, starch corn, cellulose microcrystallic, lactose.

Pharmacological properties:

Prolactin secretion inhibitor, the selection agonist dopamine D2 receptors. Has the expressed inhibiting effect on prolactin secretion by a front share of a hypophysis, without reducing normal levels of other hypophyseal hormones. At some patients decrease in secretion of prolactin can be followed by short-term slight increase of level of a growth hormone in a blood plasma, but the clinical importance of this phenomenon is still unknown. Norprolak is effective at appointment inside once a day at a giperprolaktinemiya, reducing expressiveness of such clinical manifestations as a galactorrhoea, an oligomenorrhea, an amenorrhea, infertility and decrease in a libido.

Clinically significant decrease in level of prolactin in blood occurs in 2 h after administration of drug inside, reaches a maximum in 4-6 h and about 24 h remain direct dependence of duration of action of Norprolak on the size of his dose while for prolactin - there is no reducing effect of such dependence Was established. The maximum effect is noted after use in a single dose 50 mkg. At further increase in a dose increase in expressiveness of effect is not noted, but its duration increases.

It is established that long reception of Norprolak leads to involution or a growth inhibition prolactin - producing micro and macroadenomas of a hypophysis.

Pharmacokinetics. Absorption. After administration of drug inside хинаголид it is quickly and completely absorbed from a GIT. The values of plasma concentration measured for a hinagolid and its metabolites by a non-selective radio immunological method (RIA) were close to a threshold of quantitative definition and cannot be a source to a solid data.

Distribution. After a single dose in drug, marked a radioactive label, the seeming Vd makes about 100 l. Linkng with proteins of plasma - about 90%.

Metabolism. Hinagolid is substantially metabolized at "the first passing" through a liver. Having biological activity хинаголид and its N-dezetilirovanny an analog are found in blood in small quantities. Their inactive conjugates with sulfuric and glucuronic acids circulate in blood in more significant amounts.

Removal. More than 95% are brought out of an organism in the form of metabolites with a stake and urine approximately in equal quantities. The main metabolites found in urine are sulphatic and glucuronic conjugates of a hinagolid and its N-dezetilirovannogo and N, N-didezetilirovannogo of analogs. In Calais not conjugated forms of these three substances are found.

T1/2 of not changed hinagolid after a single dose makes 11.5ch; at achievement of an equilibrium state - 17 h.

Indications to use:

— a giperprolaktinemiya (idiopathic or caused prolactin - cosecreting micro or macroadenoma of a hypophysis).

Route of administration and doses:

The adult the optimum dose is selected individually depending on extent of reduction of level of prolactin and portability of drug. Therapy should be begun with reception of tablets from "starting packaging" of Norprolak, considering a possibility of development of orthostatic hypotension owing to dopaminergic stimulation.

In the first 3 days drug appoint 25 mkg/days in a dose; in the next 3 days - in a dose of 50 mkg/days. Since 7th day, the recommended dose makes 75 mkg/days.

If necessary carry out further gradual increase in a dose (not more often than weekly) before achievement of optimum therapeutic effect. The maintenance dose makes from 75 to 150 mkg/days.

Need of use of a daily dose of 300 mkg arises only at 1/3 patients also above, thus the dose is raised gradually on 75-150 bucketed mkg by not less than 4 weeks to achievement of satisfactory therapeutic effect or before decrease in portability of drug (can be required having rummaged in reception).

Pill is taken by 1 times/days, for the night, together with reception of a small amount of food.

Features of use:

In the first days of treatment by Norprolak and at increase in a dose it is regularly necessary to carry out control of the ABP in prone positions and standing, in connection with a possibility of development of orthostatic hypotension and faint.

At Norprolak's use several cases of developing of acute psychosis (including at the patients who did not have in the anamnesis of mental diseases) which, as a rule, passed at drug withdrawal are noted. At Norprolak's appointment patients with mental disturbances in the anamnesis should observe extra care.

The concomitant use of alcohol can worsen Norprolak's portability.

Experience of use of Norprolak for elderly patients is absent.

Use in pediatrics

Experience of use of Norprolak for children is absent.

Influence on ability to driving of motor transport and to control of mechanisms

The patients who are engaged in potentially dangerous types of activity should be careful since sometimes, especially in the first days of use of Norprolak, developing of arterial hypotension and reduction in the rate of motor and mental reactions is possible.

Side effects:

From the alimentary system: often (> 10%) - nausea, vomiting; seldom (1-10%) - anorexia, pains and a stomach, a lock, diarrhea.

From TsNS: often (> 10%) - a headache, dizziness and weakness; seldom (1-10%) - sleeplessness; in some cases - acute psychosis (which disappeared after the termination of administration of drug).

From cardiovascular system: seldom (1-10%) - hypostases, inflows, orthostatic hypotension (which can result in the expressed weakness or a faint).

Others: seldom (1-10%) - a nose congestion.

The side reactions described at Norprolak's reception are characteristic of treatment by agonists of dopamine receptors, usually do not lead to drug withdrawal and tend to disappearance at treatment continuation.

Frequent side effects (> 10%) arise preferential in the first few days uses of drug or at increase in a dose (in this case they very quickly take place). If necessary for prevention of nausea and vomiting within several days in 1 hour prior to Norprolak's reception it is possible to appoint домперидон.

Interaction with other medicines:

So far it was not reported about Norprolak's interaction with other medicines. There is a theoretical possibility of reduction Norprolak prolactin inhibiting effect at his co-administration with the drugs having the expressed anti-dopaminergic effect (for example, neuroleptics) therefore at simultaneous use of these drugs it is necessary to be careful.

Contraindications:

— abnormal liver functions;
— renal failures;
— hypersensitivity to drug.

Use of the drug NORPROLAK® at pregnancy and feeding by a breast
Experience of use of Norprolak at pregnancy is limited. At pregnancy approach Norprolak's reception should be stopped unless continuation of therapy is vital. At Norprolak's cancellation increase in frequency of spontaneous abortions was not noted. In a case approach of pregnancy at the patient with adenoma of a hypophysis and Norprolak's cancellation careful observation of the patient during all pregnancy is shown.
In pilot studies of embriotoksichesky or teratogenic action of Norprolak it is not established.
As Norprolak suppresses a lactation, breastfeeding, as a rule, is impossible. At preservation of a lactation it is necessary to stop breastfeeding (since it is unknown whether it is allocated хинаголид with breast milk).
Treatment by Norprolak can recover fertility. To women of childbearing age, not persons interested to become pregnant in the course of treatment by Norprolak, it is necessary to apply reliable methods of contraception.

Use at abnormal liver functions
It is contraindicated at abnormal liver functions.

Use at renal failures
It is contraindicated at renal failures.

Use for elderly patients
Experience of use of Norprolak for elderly patients is absent.

Use for children
Experience of use of Norprolak for children is absent.

Overdose:

The acute overdose of tablets Norprolaka is not described.
Possible symptoms include severe nausea, vomiting, headaches, dizziness, drowsiness, arterial hypotension, a collapse, hallucinations.

Treatment: if necessary carry out symptomatic therapy.

Storage conditions:

Drug should be stored in the place, unavailable to children, at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets of 25 mkg: 3 pieces and tablets of 50 mkg: 3 pieces.

Tablets of 75 mkg: 30 pieces.

Tablets of 150 mkg: 30 pieces.