Parlodelum

Parlodelum – the prolactin secretion inhibitor applied to treatment of parkinsonism, prolaktinzavisimy diseases and states.

Form of release and structure

Parlodelum is released in the form of tablets: almost white color, a round form, flat, with slanted edge, on one party – a text of "SANDOZ", on another – risk and the XC code (on 30 pieces in bottles of dark glass or on 10 pieces in blisters, in a pack a cardboard 1 bottle or 3 blisters).

Structure of 1 tablet:

• Active ingredient: Bromocriptinum (in the form of a mezilat) – 2,5 mg;
• Excipients: maleic acid, dinatrium эдетат, lactoses monohydrate, starch corn, starch corn prezhelatinizirovanny, silicon dioxide colloid, magnesium stearate.

Indications to use

Prolaktinnezavisimy female infertility:

• Anovulatory cycles (as a part of a combination therapy with anti-estrogen);
• Syndrome of a polycystosis of ovaries.

Prolaktinzavisimy female infertility and disturbances of a menstrual cycle:

• Oligomenorrhea;
• Amenorrhea (including followed by a galactorrhoea);
• Insufficiency of a lyuteinovy phase;
• Secondary giperprolaktinemiya owing to reception of medicines (for example, some psychotropic or hypotensive drugs).

Prolaktinoma:

• Conservative therapy prolaktinsekretiruyushchy micro and macroadenomas of a hypophysis;
• Preoperative training of the patient (drug is used for the purpose of reduction of volume of a tumor and simplification of its removal);
• Postoperative treatment of states which are followed by the increased prolactin level.

Suppression of a lactation:

• Prevention of a lactation after abortion;
• Prevention or the termination of a lactation after the delivery on medical indications, including at an initial stage of a lactational mastitis.

Besides, Parlodelum is applied in the following cases:

• Prolaktinzavisimy hypogonadism at men – loss a libido, an oligospermatism, impotence;
• Acromegalia – as a rule, in addition to the main therapy, but use as an alternative to beam or surgical treatment is in some cases possible;
• Idiopathic disease of Parkinson and postencephalitic parkinsonism – in a combination with protivoparkinsonichesky drugs or as monotherapy.

Contraindications

Absolute:

• Heavy mental disorders, including data in the anamnesis;
• Coronary heart disease, and also other serious cardiovascular illness;
• Arterial hypertension which does not manage to be controlled by means of medicines;
• The arterial hypertension diagnosed at pregnancy and further in a puerperal period;
• Gestosis (including eclampsia and preeclampsia);
• Children's age up to 7 years;
• Hypersensitivity to components of Parlodelum or alkaloids of an ergot.

Patients should not appoint drug with rare hereditary forms of malabsorption of glucose galactose, a heavy lactose intolerance and intolerance of a galactose.

In connection with the insufficient number of clinical data it is not recommended to appoint Parlodelum for treatment of benign diseases of a mammary gland and a premenstrual syndrome (PMS).

Route of administration and dosage

Parlodelum should be accepted inside during food.

The recommended schemes of use of drug depending on indications:

• Female infertility and disturbances of a menstrual cycle: on 1,25 mg (½ tablets) 2-3 times a day. If necessary the daily dose is gradually increased to 5-7,5 mg in 2-3 receptions. Duration of treatment is defined by the moment when the ovulation is recovered or the menstrual cycle is normalized. For prevention of a recurrence the doctor can advise to continue therapy during several cycles;
• Prolaktinoma: in an initiation of treatment – on 1,25 mg 2-3 times a day, further a dose gradually raise to optimum effective which provides adequate decrease in concentration of prolactin in a blood plasma. The maximum recommended doses in days: children of 7-12 years – 5 mg, teenagers of 13-17 years – 20 mg;
• Suppression of a lactation on medical indications: the first day – on 1,25 mg 2 times a day (at breakfast and a dinner), during the next 14 days – on 2,5 mg 2 times a day. To begin to accept drug follows in several hours after abortion or childbirth, but only after stabilization of the vital functions. 2-3 days later after cancellation of Parlodelum perhaps insignificant release of milk that it is possible to eliminate with additional administration of drug in the same dose within 7 days;
• The beginning puerperal mastitis (in a combination with an antibiotic): the first day – on 1,25 mg 2 times a day (in the morning and in the evening), the next 14 days – on 2,5 mg 2 times a day;
• Acromegalia: in an initiation of treatment – on 1,25 mg 2-3 times a day, further a dose gradually raise, depending on clinical effect and portability, to 10-20 mg a day. Maximum daily doses: children of 7-12 years – 10 mg, teenagers of 13-17 years – 20 mg;
• Giperprolaktinemiya at men: on 1,25 mg 2-3 times a day, further a daily dose gradually increase up to 5-10 mg;
• Parkinson's disease: the first 7 days – on 1,25 mg of 1 times a day, preferably in the evening. Further the dose is selected individually by a titration method, i.e. every week it is raised on 1,25 mg and divided into 2-3 receptions. The adequate therapeutic effect usually manages to be reached within 6-8 weeks of therapy. If the clinical answer later this time is absent, the dose is increased by 2,5 mg every week. The effective daily dose of Bromocriptinum varies within 10-40 mg, however higher doses in certain cases are required. If during titration of a dose there are undesirable effects, the daily dose should be lowered at least for 1 week. After stopping of side reactions the dose can be raised again. Patients who have motive disturbances owing to reception of a levodopa are recommended to lower a levodopa dose to purpose of Parlodelum. After Bromocriptinum possible to reach satisfactory clinical effect, it is possible to reduce a levodopa dose gradually further. At some patients thanks to Parlodelum it is possible to cancel it completely.

Side effects

Classification of side effects:

• Often: ≥ 1/100-<1/10;
• Sometimes: ≥ 1/1000-<1/100;
• Seldom: ≥ 1/10 000-<1/1000;
• Very seldom: <1/10 000, including isolated cases.

Possible side effects:

• Dermatological and allergic reactions: sometimes – a hair loss, skin manifestations;
• From the central and peripheral nervous system: often – вертиго, a somnolence, a headache; sometimes – hallucinations, confusion of consciousness, motive frustration, psychomotor excitement; seldom – psychotic disturbances, sleeplessness, paresthesias, drowsiness; very seldom – sudden backfilling, the increased drowsiness in the afternoon, hyper sexuality, increase in a libido;
• From respiratory system: often – a nose congestion; seldom – an asthma, a pleural exudate, pleurisy, pleural fibrosis, pulmonary fibrosis;
• From cardiovascular system: sometimes – orthostatic hypotension (in rare instances leading to a faint), arterial hypotension; seldom – tachycardia, chronic cardial compression, arrhythmia, an exudate in a pericardium, bradycardia; very seldom – reversible pallor of fingers on hands and legs owing to overcooling (especially at patients with a syndrome of Reynaud in the anamnesis); very seldom – fibrosis of heart valves;
• From a musculoskeletal system: sometimes – spasms of gastrocnemius muscles;
• From sense bodys: seldom – a sonitus, disturbance and misting of sight;
• From the alimentary system: often – nausea and/or vomiting, a lock; sometimes – dryness in a mouth; seldom – an abdominal pain, diarrhea, digestive tract cankers, gastrointestinal bleedings (blood in emetic masses and/or black kcal), retroperitoneal fibrosis;
• Others: sometimes – increased fatigue; seldom – peripheral hypostases; very seldom at sharp drug withdrawal – the state similar to a malignant antipsychotic syndrome.

At use of Parlodelum for suppression of a lactation in a puerperal period development of mental disturbances, arterial hypertension, spasms, a myocardial infarction or a stroke is in rare instances possible, however relationship of cause and effect of these side effects using drug is not established.

Special instructions

In the presence at women of the pathologies which are not connected with increase in level of hormone of prolactin in blood, Parlodelum should be applied in the minimal effective dose necessary for elimination of symptoms of a disease. It is important to this recommendation to adhere, otherwise decrease in level of prolactin in a blood plasma below norm is possible that leads to dysfunction of a yellow body.

Women in a puerperal period along with Parlodelum should not appoint vasoconstrictive drugs.

During treatment careful observation is required to patients with a peptic ulcer in the anamnesis.

Patients with pleuropulmonary diseases of not clear etiology in case of progressing of disturbances should cancel drug and to conduct examination.

For early diagnosis of retroperitoneal fibrosis at a reversible initial stage of process the doctor needs to watch a condition of the patient in time to reveal such symptoms as hypostasis of the lower extremities, a dorsodynia, renal failures. If there are bases to suspect existence in retroperitoneal space of fibrotichesky changes, it is necessary to cancel Parlodelum immediately.

At patients with secondary adrenal insufficiency it is necessary to carry out replacement glucocorticosteroid therapy.

At patients with hypophysis macroadenomas during treatment it is necessary to estimate dynamics of the sizes of a tumor constantly. In case of its increase the surgical method of treatment can be applied.

Due to the risk of increase in a tumor under careful observation there have to be pregnant women who received Parlodelum for treatment of prolaktinsekretiruyushchy adenoma of a hypophysis earlier.

During treatment it is necessary to be careful when driving the car and performing potentially dangerous types of works, especially in the first days of use of drug.

Patients with Parkinson's disease are recommended to refrain from control of vehicles and occupations the types of activity demanding the speed of reactions and special attention. In case of the expressed drowsiness or episodes of sudden backfilling it is necessary to lower a dose of Parlodelum or to cancel it at all.

As drug can recover fertility, the women of childbearing age who are not planning pregnancy should use reliable methods of contraception.

Medicinal interaction

Bromocriptinum should be applied about care in a combination with other substrates and/or inhibitors of CYP3A4 enzyme (for example, inhibitors of protease of a human immunodeficiency virus or antifungal means from group of azoles).

At the combined use with makrolidny antibiotics (dzhozamitsiny or erythromycin) increase in concentration of Bromocriptinum in a blood plasma is noted.

At simultaneous use of an oktreotid for patients to an acromegalia there is an increase in level of Bromocriptinum in a blood plasma.

In case of use of a domperidon, Metoclopramidum or antagonists of dopamine receptors (for example, such neuroleptics as thioxanthenes, phenyl propyl ketones or fenotiazina) the therapeutic effectiveness of Bromocriptinum can decrease.

Parlodelum can bring to expressed to a lowering of arterial pressure at the patients receiving anti-hypertensive drugs.

At patients with Parkinson's disease drug strengthens protivoparkinsonichesky action of a levodopa that quite often allows to reduce a dose of the last. Purpose of Parlodelum is reasonable in cases of easing of medical effect of a levodopa and at development of the complications connected with its use, such as phenomenon of "inclusion switching off" (on-off), effect exhaustion syndrome by the end of action of a dose of a levodopa, the involuntary movements (painful dystonia and/or choreoathetoid dyskinesia).

Ethanol can promote deterioration in portability of Bromocriptinum.

Terms and storage conditions

To store at a temperature, not exceeding 25 °C, in the unavailable to children and protected from light place.

Period of validity – 3 years.