Parlodel
Parlodel: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Parlodel
ATX code: N04BC01
Active ingredient: bromocriptine (bromocriptine)
Manufacturer: MEDA, AB (Sweden), NOVARTIS FARMA (Italy)
Description and photo update: 2019-26-08
Parlodel is a prolactin secretion inhibitor used to treat parkinsonism, prolactin-dependent diseases and conditions.
Release form and composition
Parlodel is produced in the form of tablets: almost white, round, flat, with a beveled edge, on one side - the inscription "SANDOZ", on the other - risk and the code "XC" (30 pcs. In dark glass bottles or 10 pcs.. in blisters, in a cardboard box 1 bottle or 3 blisters).
Composition of 1 tablet:
- Active ingredient: bromocriptine (in the form of mesylate) - 2.5 mg;
- Excipients: maleic acid, disodium edetate, lactose monohydrate, corn starch, pregelatinized corn starch, colloidal silicon dioxide, magnesium stearate.
Pharmacological properties
Bromocriptine is a dopamine receptor agonist and has dopaminomimetic and hypoprolactinemic effects.
Pharmacodynamics
Bromocriptine inhibits the body's synthesis of prolactin, a hormone produced in the anterior pituitary gland, without altering the levels of other pituitary hormones. However, the drug can reduce elevated levels of growth hormone (STH) in patients with acromegaly, which is due to stimulation of dopamine receptors.
In the postpartum period, prolactin activates the lactation process and is necessary for its further maintenance. In patients in other periods of life, galactorrhea (abnormal lactation) and / or menstrual irregularities and ovulation are a consequence of an increase in the secretion of this hormone.
Bromocriptine as a specific inhibitor of prolactin production can be used in the treatment of pathological conditions associated with hypersecretion of prolactin, as well as to prevent or suppress physiological lactation. In patients with amenorrhea and / or anovulatory menstrual cycles, which are accompanied or not accompanied by galactorrhea, Parlodel can be used to normalize the menstrual cycle and restore ovulation.
The appointment of Parlodel in order to suppress lactation does not require restrictions on fluid intake. It also does not increase the risk of thromboembolism and does not disrupt the involution of the uterus in the postpartum period.
Bromocriptine inhibits the growth or reduces the size of prolactinomas - prolactin-secreting pituitary adenomas.
In patients with acromegaly, Parlodel not only reduces the content of GH and prolactin in the blood plasma, but also has a beneficial effect on clinical symptoms and glucose tolerance.
In Parkinson's disease, which is characterized by a specific dopamine deficiency in the black and striated nuclei of the brain, bromocriptine stimulates dopamine receptors, which leads to the restoration of neurochemical balance in the basal ganglia. Patients with this disease are usually prescribed Parlodel in higher doses than when used for endocrinological indications.
Bromocriptine reduces the slowness of movement, rigidity, tremors and other signs of parkinsonism, characteristic of all stages of the disease. It is suitable for long-term therapy as its effectiveness usually lasts for many years (currently, good treatment results have been described with a duration of therapy of 8 years).
Bromocriptine reduces the severity of symptoms of depression in patients with Parkinson's disease. This is due to its characteristic antidepressant properties, proven in controlled studies, in which patients with psychogenic or endogenous depression, who do not suffer from Parkinson's disease, participated.
Pharmacokinetics
After oral administration of the drug, bromocriptine is well absorbed. In healthy volunteers, after taking Parlodel orally in tablet form, the half-absorption period of its active ingredient is 0.2–0.5 hours, and the maximum level of bromocriptine in the blood plasma is reached within 1–3 hours. When taken orally 5 mg of bromocriptine, its maximum concentration is 0.465 ng / ml. The prolactin-lowering effect is observed 1–2 hours after taking Parlodel inside, reaches peak values (prolactin concentration decreases by more than 80%) after 5–10 hours and remains at a close to maximum level for 8–12 hours. The degree of binding of bromocriptine to plasma proteins is 96%.
Bromocriptine is extensively metabolized in the liver due to the first pass effect, forming a lot of metabolites. It is practically not excreted through the kidneys and intestines unchanged. This substance has a high affinity for CYP3A. The main metabolic pathway is the hydroxylation of the proline ring, which is part of the cyclopeptide. The combination of the drug with potential substrates and / or inhibitors of CYP3A4 can provoke inhibition of the clearance of bromocriptine and an increase in its concentration in blood plasma, with the calculated IC50 value being 1.69 μM. However, since the therapeutic concentrations of free bromocriptine in patients remain low, a significant change in metabolism is not expected when combined with Parlodel drugs, in the clearance of which isoenzyme CYP3A4 is involved.
Unchanged bromocriptine is excreted from plasma in a biphasic manner. The final half-life is approximately 15 hours (range of variation is from 8 to 20 hours). Bromocriptine and its metabolites are almost completely excreted through the liver, only 6% of the dose taken is excreted through the kidneys.
In patients with liver dysfunctions, the rate of elimination of the drug may decrease, and its content in blood plasma may increase. In this case, correction of the dosage regimen is necessary.
Indications for use
Prolactin-independent female infertility:
- Anovulatory cycles (as part of combination therapy with antiestrogens);
- Polycystic ovary syndrome.
Prolactin-dependent female infertility and menstrual irregularities:
- Oligomenorrhea;
- Amenorrhea (including accompanied by galactorrhea);
- Insufficiency of the luteal phase;
- Secondary hyperprolactinemia due to taking medications (for example, some psychotropic or antihypertensive drugs).
Prolactinomas:
- Conservative therapy of prolactin-secreting micro- and macroadenomas of the pituitary gland;
- Preoperative preparation of the patient (Parlodel is used to reduce the volume of the tumor and facilitate its removal);
- Postoperative treatment of conditions that are accompanied by elevated prolactin levels.
Suppression of lactation:
- Prevention of lactation after abortion;
- Prevention or cessation of lactation after childbirth for medical reasons, including at the initial stage of postpartum mastitis.
In addition, Parlodel is used in the following cases:
- Prolactin-dependent hypogonadism in men - loss of libido, oligospermia, impotence;
- Acromegaly - as a rule, in addition to the main therapy, but in some cases it is possible to use it as an alternative to radiation or surgical treatment;
- Idiopathic Parkinson's disease and post-encephalitic parkinsonism - in combination with antiparkinsonian drugs or as monotherapy.
Contraindications
Absolute:
- Severe mental disorders, including data in anamnesis;
- Ischemic heart disease, as well as other severe cardiovascular diseases;
- Arterial hypertension that cannot be controlled with drugs;
- Arterial hypertension diagnosed during pregnancy and later in the postpartum period;
- Gestosis (including eclampsia and preeclampsia);
- Children up to age 7;
- Hypersensitivity to drug components or ergot alkaloids.
According to the instructions, Parlodel should not be prescribed to patients with rare hereditary forms of glucose-galactose malabsorption, severe lactase deficiency and galactose intolerance.
Due to the insufficient amount of clinical data, Parlodel is not recommended for the treatment of benign breast diseases and premenstrual syndrome (PMS).
Instructions for the use of Parlodel: method and dosage
Parlodel tablets should be taken orally with meals.
Recommended dosage regimens of the drug, depending on the indications:
- Female infertility and menstrual irregularities: 1.25 mg (½ tablet) 2-3 times a day. If necessary, the daily dose is gradually increased to 5-7.5 mg in 2-3 doses. The duration of treatment is determined by the moment when ovulation is restored or the menstrual cycle normalizes. To prevent relapses, the doctor may advise you to continue therapy for several cycles;
- Prolactinomas: at the beginning of treatment - 1.25 mg 2-3 times a day, then the dose is gradually increased to the optimal effective, which provides an adequate decrease in the concentration of prolactin in the blood plasma. The maximum recommended doses per day: children 7-12 years old - 5 mg, adolescents 13-17 years old - 20 mg;
- Suppression of lactation for medical reasons: the first day - 1.25 mg 2 times a day (for breakfast and dinner), over the next 14 days - 2.5 mg 2 times a day. You should start taking the drug a few hours after an abortion or childbirth, but only after stabilization of vital functions. 2-3 days after the cancellation of Parlodel, a slight release of milk is possible, which can be eliminated by additional intake of the drug in the same dose for another 7 days;
- Beginning postpartum mastitis (in combination with an antibiotic): the first day - 1.25 mg 2 times a day (morning and evening), the next 14 days - 2.5 mg 2 times a day;
- Acromegaly: at the beginning of treatment - 1.25 mg 2-3 times a day, then the dose is gradually increased, depending on the clinical effect and tolerance, up to 10-20 mg per day. Maximum daily doses: children 7-12 years old - 10 mg, adolescents 13-17 years old - 20 mg;
- Hyperprolactinemia in men: 1.25 mg 2-3 times a day, then the daily dose is gradually increased to 5-10 mg;
- Parkinson's disease: the first 7 days - 1.25 mg 1 time per day, preferably in the evening. Then the dose is selected individually by titration, i.e. every week it is increased by 1.25 mg and divided into 2-3 doses. Adequate therapeutic effect can usually be achieved within 6-8 weeks of therapy. If there is no clinical response after this time, the dose is increased by 2.5 mg every week. The effective daily dose of bromocriptine varies between 10-40 mg, but in some cases higher doses are required. In the event that undesirable effects occur during the dose titration period, the daily dose should be reduced by at least 1 week. After relief of adverse reactions, the dose can be increased again. Patients who experience movement disorders due to taking levodopa,before the appointment of Parlodel, it is recommended to reduce the dose of levodopa. After a satisfactory clinical effect is achieved with bromocriptine, the dose of levodopa can be gradually reduced further. In some patients, thanks to Parlodel, it is possible to completely cancel it.
Side effects
Classification of side effects:
- Often: ≥ 1 / 100- <1/10;
- Sometimes: ≥ 1 / 1000- <1/100;
- Rarely: ≥ 1/10 000- <1/1000;
- Very rare: <1/10 000, including isolated cases.
Possible side effects of Parlodel:
- Dermatological and allergic reactions: sometimes - hair loss, skin manifestations;
- From the central and peripheral nervous system: often - vertigo, drowsiness, headache; sometimes - hallucinations, confusion, movement disorders, psychomotor agitation; rarely - psychotic disorders, insomnia, paresthesia, drowsiness; very rarely - sudden falling asleep, increased daytime sleepiness, hypersexuality, increased libido;
- From the respiratory system: often - nasal congestion; rarely - shortness of breath, pleural effusion, pleurisy, pleural fibrosis, pulmonary fibrosis;
- From the side of the cardiovascular system: sometimes - orthostatic hypotension (in rare cases leading to fainting), arterial hypotension; rarely - tachycardia, constrictive pericarditis, arrhythmia, pericardial effusion, bradycardia; very rarely - reversible pallor of fingers and toes due to hypothermia (especially in patients with Raynaud's syndrome in history); very rarely - fibrosis of the heart valves;
- From the musculoskeletal system: sometimes - cramps of the calf muscles;
- From the senses: rarely - tinnitus, disturbance and blurred vision;
- From the digestive system: often - nausea and / or vomiting, constipation; sometimes dry mouth; rarely - abdominal pain, diarrhea, ulcerative lesions of the gastrointestinal tract, gastrointestinal bleeding (blood in the vomit and / or black feces), retroperitoneal fibrosis;
- Others: sometimes - increased fatigue; rarely - peripheral edema; very rarely with a sharp withdrawal of the drug - a condition similar to neuroleptic malignant syndrome.
When using Parlodel to suppress lactation in the postpartum period, in rare cases, the development of mental disorders, arterial hypertension, seizures, myocardial infarction or stroke is possible, however, the causal relationship of these side effects with the use of the drug has not been established.
Overdose
In all cases of registered overdose of Parlodel, no lethal outcomes were observed. The maximum currently known single dose of bromocriptine is 325 mg. Overdose symptoms include drowsiness, drowsiness, lethargy, hallucinations, dizziness, nausea, vomiting, tachycardia, hypotension, postural hypotension.
There are sporadic reports of accidental ingestion of the drug by children who have experienced drowsiness, fever and vomiting. The patients' condition improved spontaneously or several hours after the appointment of appropriate therapy.
When taking high doses of Parlodel orally, you must take activated charcoal. It is allowed to carry out gastric lavage immediately after taking the drug. In case of acute intoxication, symptomatic treatment is recommended. To stop hallucinations or vomiting, metoclopramide may be prescribed.
special instructions
If women have pathologies that are not associated with an increase in the level of the hormone prolactin in the blood, Parlodel should be used in the minimum effective dose necessary to eliminate the symptoms of the disease. It is important to adhere to this recommendation, otherwise a decrease in the level of prolactin in the blood plasma below normal is possible, which leads to a violation of the function of the corpus luteum.
Women in the postpartum period should not be prescribed vasoconstrictor drugs simultaneously with Parlodel.
During the treatment period, careful observation is required for patients with a history of peptic ulcer disease.
Patients with pleuropulmonary diseases of unclear etiology in case of progression of disorders should cancel Parlodel and conduct an examination.
For early diagnosis of retroperitoneal fibrosis at a reversible initial stage of the process, the doctor needs to monitor the patient's condition in order to identify symptoms such as edema of the lower extremities, back pain, and renal dysfunction in time. If there is reason to suspect the presence of fibrotic changes in the retroperitoneal space, Parlodel should be canceled immediately.
In patients with secondary adrenal insufficiency, it is necessary to carry out glucocorticosteroid replacement therapy.
In patients with pituitary macroadenomas, the dynamics of tumor size should be constantly assessed during treatment. In case of its increase, a surgical method of treatment can be applied.
Due to the risk of tumor enlargement, pregnant women who have previously received Parlodel for the treatment of prolactin-secreting pituitary adenoma should be closely monitored.
Since the drug can restore fertility, women of childbearing age who are not planning a pregnancy should use reliable methods of contraception.
Influence on the ability to drive vehicles and complex mechanisms
During treatment, care should be taken when driving a car and performing potentially dangerous types of work, especially in the first days of using the drug.
Patients with Parkinson's disease are advised to refrain from driving and engaging in activities that require speed of reactions and increased attention. In the event of severe drowsiness or episodes of sudden falling asleep, you need to reduce the dose of Parlodel or cancel it altogether.
Application during pregnancy and lactation
In patients planning a pregnancy, after receiving a positive pregnancy test result, the drug, like other drugs, should be canceled, except in cases in which it is necessary to continue treatment for medical reasons. Cancellation of Parlodel in pregnant women did not lead to an increase in the incidence of spontaneous abortions. The results of clinical studies indicate that the use of bromocriptine during pregnancy does not adversely affect its course or outcome.
Termination of treatment with Parlodel for pregnant women with pituitary adenoma requires careful monitoring of the patient's condition throughout the entire period of pregnancy. If signs of a pronounced increase in prolactinoma appear, for example, narrowing of the visual fields or headaches, bromocriptine therapy should be resumed or surgery should be resorted to.
Since Parlodel suppresses lactation, it is not prescribed for mothers whose children are breastfed.
Pediatric use
Parlodel is not used to treat children under 7 years of age.
For violations of liver function
Patients with impaired hepatic function may require dose adjustment of Parlodel.
Use in the elderly
Patients over 65 years of age should be careful when taking Parlodel.
Drug interactions
Bromocriptine should be used with caution in combination with other substrates and / or inhibitors of the CYP3A4 enzyme (for example, human immunodeficiency virus protease inhibitors or azoles antifungal agents).
When combined with macrolide antibiotics (josamycin or erythromycin), there is an increase in the concentration of bromocriptine in the blood plasma.
With the simultaneous use of octreotide in patients with acromegaly, an increase in the level of bromocriptine in the blood plasma occurs.
In the case of the use of domperidone, metoclopramide or dopamine receptor antagonists (for example, neuroleptics such as thioxanthenes, butyrophenones or phenothiazines), the therapeutic efficacy of bromocriptine may decrease.
Parlodel can lead to a marked decrease in blood pressure in patients receiving antihypertensive drugs.
In patients with Parkinson's disease, the drug enhances the antiparkinsonian effect of levodopa, which often makes it possible to reduce the dose of the latter. The appointment of Parlodel is advisable in cases of weakening of the therapeutic effect of levodopa and the development of complications associated with its use, such as the phenomenon of "on-off" (on-off), the syndrome of depletion of the effect by the end of the dose of levodopa, involuntary movements (painful dystonia and / or choreoathetoid dyskinesia).
Ethanol may impair the tolerability of bromocriptine.
Analogs
Parlodel's analogues are: Abergin, Bromocriptine, Bromocriptine-Richter, Bromocriptine-KV, Ronalin.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C, out of the reach of children and protected from light.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Parlodel
Reviews of Parlodel mainly indicate its high efficiency, provided that the patient follows the doctor's recommendations. There are some reports of negative effects of such treatment, in particular, fainting, excessive hair growth on the legs and a sharp increase in appetite.
Parlodel price in pharmacies
On average, the price of Parlodel in pharmacy chains is 2300‒2410 rubles (the package includes 30 tablets).
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
