Pauzogest

Pauzogest is a monophasic drug, which is used during HRT. The medicine includes a complex of the following elements - progestogen with estrogen. Due to the action of drugs, the deficiency of sex hormones in a woman occurs, which develops during postmenopause. The preparation contains components such as norethisterone acetate and 17b-estradiol; It must be taken without interruption.

At low dosages, progestogen leads to endometrial atrophy and supports it. During the use of drugs menstruation does not occur.

Indications Pauzogesta

It is used in the case of estrogen deficiency syndrome during menopause.

The drug is used to prevent common metabolic disorders, including osteoporosis, which develops during postmenopause, if there is a high probability of bone fracture (for example, in case of low weight, early menopause, calcium deficiency, presence in the family history of osteoporosis of a severe nature, and moreover when smoking or alcoholism, severe movement disorders and taking GCS).

In addition to osteoporosis, the drug is prescribed to prevent other common metabolic disorders that occur during postmenopause (among those changes affecting the mucous membranes and epidermis, skin atrophy, cosmetic disorders, etc.).

Release form

The release of the drug component is implemented in tablets - 28 pieces inside the cell plate. In a pack - 1 or 3 records.

Pharmacodynamics

Estradiol has a therapeutic effect through specific estrogen endings. The steroid-receptor structure is synthesized with cellular DNA, and then induces the binding of specific proteins. The substance affects the metabolic processes - for example, it reduces the levels of LDL cholesterol, and in addition increases the values of triglycerides and HDL cholesterol inside the blood serum.

Norethisterone acetate is a progestogen, which also has an effect with endings. It affects the reproductive activity of the female body (this includes changes in the structure of the endometrium). This component affects the processes of lipid metabolism.

Using a combination of the above components leads to a decrease in LDL and cholesterol values; however, serum levels of triglycerides and HDL remain the same.

Pharmacokinetics

Microcrystalline estradiol is well absorbed at high speed. Plasma Cmax values are noted after 4-6 hours from the moment of use, amounting to 90-100 pg / ml. At the same time, the equilibrium plasma level is 70-100 pg / ml.

The term half-life is approximately 14-16 hours. More than 90% of the substance is involved in intraplasma protein synthesis. First, estradiol is oxidized to form estrone, and then transformed into estriol. These processes take place inside the liver.

Estradiol with its metabolic elements are excreted mostly by the kidneys (by 90-95%), and also in the form of a glucuronide or sulphate conjugate with no bioactivity. The rest (about 5-10%) is excreted in an unchanged condition with faeces.

Norethisterone acetate is also absorbed at high speed and transformed into the element norethisterone, after which it undergoes metabolic processes and is excreted in the form of sulfate and glucuronide conjugates. The term half-life is about 3-6 hours.

Dosing and administration

Use the medication should be continuous - usually on the 1st tablet per day. Prescribing such treatment is required at least after 1 year since the start of menopause.

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Use Pauzogesta during pregnancy

Pregnant women (or if there is a suspicion that the pregnancy has come), and besides, when breastfeeding, Pauzogest cannot be prescribed.

Contraindications

Among the contraindications:

• diagnosed malignant neoplasm in the area of the mammary glands, its history or suspicion of it;
• a diagnosed neoplasm of an estrogen-dependent type (for example, endometrial cancer) or a suspicion of its presence;
• chronic or acute phases of hepatic diseases or the presence of a history of pathology, after which the values of the liver are not normalized;
• enzymopathic jaundice or Rotor syndrome;
• previously transferred or staying in the phase of exacerbation of DVT of the legs, and in addition to this thromboembolic pathology;
• bleeding from genitalia, having an unknown genesis;
• severe stages of disease in the area of the cardiovascular system or cerebrovascular nature;
• severe intolerance against any component of the drug;
• porphyria or hemoglobinopathy.

Side effects Pauzogesta

During the first months of use, short lasting or breakthrough bleedings may occur, and besides this, breast sensitivity is temporarily increased. More rarely, nausea, headaches and swelling appear.

The use of progestogen with estrogen occasionally causes dizziness, migraines, alopecia, epidermal manifestations (for example, chloasma, which can remain after the completion of the drug) and problems with the use of contact lenses.

[1]

Overdose

Intoxication can cause vomiting with nausea.

The drug does not have an antidote, symptomatic measures are taken.

Interactions with other drugs

Combined use with inducers of liver enzymes leads to potentiation of estrogen metabolic processes and weakened therapeutic efficacy of Pausogest.

The development of drug interaction with the combination of drugs with phenytoin, carbamazepine, and in addition with rifampicin and barbiturates has been revealed.

[3], [4]

Storage conditions

Pause test should be maintained at temperature indices in the range of 15-30 ° C.

Shelf life

Pausesogest can be used for a 36-month term from the moment of drug implementation.

Analogs

Analogues of drugs are the substances Evian and Kliogest with Triaclym.