FARLUTAL ® - Medroxyprogesterone

FARLUTAL ® is a drug based on Medroxyprogesterone acetate

THERAPEUTIC GROUP: Progestinic

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications FARLUTAL ® - Medroxyprogesterone

FARLUTAL ® is a progestin used in the treatment of certain female gynecological disorders such as secondary amenorrhea and functional menometrorrhagia.

Experimental data also tested its efficacy, also achieving good successes, during hormone-dependent tumors and in cases of advanced cachexia.

As a progestin it is also combined with hormone therapy replacing estrogen, to reduce the risk of endometrial carcinomas.

Mechanism of action FARLUTAL ® - Medroxyprogesterone

FARLUTAL ® is a drug based on medroxyprogesterone, a progestational derivative characterized by a different pharmacokinetic profile and selective biological activity.

From the pharmacokinetic point of view this active principle is distinguished from the other progestogens and from the endogenous progesterone for the long duration of action, estimated between 20 and 30 hours, after which, after a hepatic metabolism, it is mainly excreted via the urine .

Like endogenous progesterone, medroxyprogesterone is able to interact predominantly with endometrial cells by reprogramming gene expression and mediating the transition from proliferative to secretive, necessary in nature to adequately accommodate the newly formed embryo, facilitating its nesting .

This active principle also maintains the androgenic activity, which is fundamental in the treatment of cachectic states, while it is devoid of estrogenic activity and modulatory activity on the hypothalamic-pituitary axis when taken orally in a single dose.

In the latter case, therefore, the intake of FARLUTAL ® does not inhibit neither folliculogenesis nor oogenesis.

Studies carried out and clinical efficacy

1. FARLUTAL AND ENDOMETRIAL HYPERPLASIA: the molecular structure

Although medroxyprogesterone therapy has not proved particularly useful in improving bone health during work, good results have instead been observed following the arrival of menopause, guaranteeing a significant increase in bone density in ex-users.

2. MEDAHSSIPROGESTERONE ANAPHYLAXIS

Important case-report that reveals the appearance of anaphylactic reactions in a young 16-year-old girl who was treated with medroxyprogesterone. These reactions, which are also present in the absence of a previous clinical history, underline the importance of continuous medical supervision.

3. MEDROSSIPROGESTERONE AND CELL TRANSFORMATION

Study conducted on over 1500 women, which assesses the presence of side effects related to histological health of the cervix monitored through colposcopy, following prolonged administration of medroxyprogesterone. The results show, even in the absence of a frank transformation, an increase in atypical glandular cells for which continuous medical monitoring becomes useful.

Method of use and dosage

FARLUTAL ® film-coated tablets of 10 - 20 mg of medroxyprogesterone:

the dosage of FARLUTAL ® must necessarily be established by the doctor after a careful evaluation of the patient's clinical picture and the related therapeutic goals.

In fact the very wide range of application leaves the doctor an excellent possibility of therapeutic modulation, in order to optimize its effectiveness while reducing the potential side effects

Usually the therapy with FARLUTAL ® follows cyclic protocols with blood losses that occur about 3 days after the suspension of therapy.

Warnings FARLUTAL ® - Medroxyprogesterone

The therapy with FARLUTAL ® must necessarily be preceded by a careful check-up useful to clarify the need for therapy, the therapeutic objectives and the possible presence of predisposing factors for the development of potential side effects.

In the latter case, patients suffering from changes in liver function, renal insufficiency, asthma, diabetes, lupus, psychiatric disorders, porphyria and cholestasis should be closely followed by their doctor in order to avoid the onset of unpleasant adverse reactions.

At the onset of the first side effects such as: vision disorders, headache and vaginal discharge, the patient should be subjected to careful controls to opt for therapy suspension if necessary.

Given the potential side effects, the patient must be informed by his doctor of both the possible advantages and potential adverse reactions, in order to carefully evaluate the cost / benefit ratio.

In the event that FARLUTAL ® was administered in conjunction with estrogen therapy it would also be necessary to evaluate interactions, contraindications, warnings and side effects of estrogen-based replacement therapy.

FARLUTAL ® contains lactose, so its intake could cause more or less serious side effects in patients with lactase enzyme deficiency, glucose / galactose malabsorption and lactose intolerance.

PREGNANCY AND BREASTFEEDING

The administration of progestogens during the pregnancy period should be limited to cases of real need and only under strict medical supervision.

The ability of these hormones to easily cross the hematoplacental barrier, could expose the fetus to cardiac risks and structural malformations of the urethra.

FARLUTAL ® is instead contraindicated during the lactation period due to the ability of medroxyprogesterone to pass through the breast filter and be secreted in breast milk.

Interactions

It is necessary to remember, even in the absence of clinically relevant drug interactions, that the concomitant intake of active ingredients capable of altering the activity of the liver enzymes responsible for the metabolism of medroxyprogesterone could determine a significant variation in the blood concentrations of the aforementioned active ingredient and its biological effectiveness.

Contraindications FARLUTAL ® - Medroxyprogesterone

FARLUTAL ® is contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients, in case of vaginal bleeding of unknown origin, breast cancer or dependent estrogen-progestin tumors, changes in liver function and previous or existing thromboembolic processes.

Undesirable effects - Side effects

The intake of FARLUTAL ® like that of other progestogens, can expose the patient to clinically relevant side effects on different organs and systems.

The most affected are:

the gastro-enteric system with diarrhea, nausea, vomiting and abdominal cramps;
The nervous system with depression, migraine, headache and other neurological symptoms;
the genitourinary system, with lesions affecting the uterine and vaginal mucosa, increased secretions and cervical erosions;
the breast, with increased breast tenderness;
the integumentary apparatus subject to rashes, rash and hives.

On the other hand, the long-term side effects of estrogen-progestin therapy with a significant increase in the incidence of breast cancer, progestin-dependent neoplasms, venous thrombosis and myocardial infarction have been clinically more important.