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LENZETTO® (Estradiol) 1,53 mg/Dose Transdermal Spray (8.1 ml / 56 Dose)

$29.40

LENZETTO® transdermal spray is an oestrogen only hormone replacement therapy (HRT) effective at relieving unpleasant and uncomfortable symptoms of the menopause.

 

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Description

Lenzetto® is a systemic estrogen replacement therapy that releases estradiol, the main estrogen secreted by the ovaries. The active ingredient, synthetic 17-beta-estradiol, is chemically and biologically identical to endogenous human estradiol, replaces lost estrogen production in postmenopausal women and alleviates menopausal symptoms.

Other brand names (estradiol): Acrux, Alora, Climara, Divigel, Elestrin, Esclim, Estraderm, Estrasorb, EstroGel, EvaMist, Ellavie, Menostar, Minivelle, Vivelle, Vivelle-Dot

 


Lenzetto is a spray solution which contains:

1 dose of the drug contains the active substance – estradiol hemihydrate 1.58 mg/dose (equivalent to estradiol 1.53 mg/dose).
Excipients: Octisalate, ethanol 96%.

 

Indications for use

– Continuous hormone replacement therapy (HRT) in the presence of symptoms of estrogen deficiency in postmenopausal women (women with no menstrual bleeding for at least 6 months or women with surgical menopause with a preserved or removed uterus).

Experience in treating women over 65 years of age is limited.

 

How to use Lenzetto

Doses

Lenzetto® is used once a day in monotherapy mode, or in a continuous sequential mode (in combination with a progestogen).

One fixed dose spray is applied once daily to dry and intact forearm skin. The dose may be increased to two applications per day on the skin of the forearm, depending on the severity of the clinical response. Dose escalation should be based on the severity of postmenopausal symptoms, and it is possible after at least 4 weeks of continuous treatment with Lenzetto®. The maximum daily dose is 3 applications (4.59 mg / day) on the skin of the forearm. Dose increases should be agreed with your doctor. For patients who have difficulty in applying the drug in the prescribed dose to separate, non-overlapping areas of the forearm, Lenzetto® can be applied to areas of the skin of the other forearm or to areas of the skin of the inner thigh. After application of Lenzetto® to the skin, the average drying time is 90 seconds (median is 67 seconds).

To initiate and continue treatment of postmenopausal symptoms, the lowest effective dose should be administered for the shortest period of time.

If a dose is missed, the patient should apply the drug the next day at the usual time. Skipping a dose in women with a preserved uterus increases the risk of breakthrough bleeding and spotting bleeding.

If, after increasing the dose, the severity of postmenopausal symptoms does not decrease, the patient should return to the previous dose.

The feasibility of continuing treatment should be assessed every 3-6 months.

When prescribing a drug containing estrogen, women with a preserved uterus in the postmenopausal period should begin treatment with a progestogen intended for combined estrogen-progestogen therapy to reduce the risk of endometrial cancer.

Women with a preserved uterus

For women with a preserved uterus, Lenzetto® should be prescribed in combination with a progestogen intended for estrogen-progestogen therapy. Progestogen is used for at least 12-14 days during each 28-day cycle in a continuous-sequential mode of administration, estrogen is used continuously.

Patients who have not previously received hormone replacement therapy, as well as patients switching from other types of HRT (cyclic, continuous or permanent), should be given recommendations on how to properly start treatment.

During the period of use of estrogen in combination with a progestogen, breakthrough uterine bleeding may occur. A new 28-day treatment cycle begins without interruption in the use of drugs.

Women with a removed uterus

If the woman has not previously been diagnosed with endometriosis, then the additional use of progestogen is not recommended.

Mode of application

When applying the spray, the bottle should be kept strictly vertical. The first time you use a new applicator, you must fill it by releasing the first three doses of spray inside the cap.

The daily dose is one application of a fixed dose of spray to adjacent non-overlapping skin areas (about 20 cm2) of the inner surface of the forearm. Wait approximately 2 minutes for the solution to dry completely. Do not allow the treated skin to come into contact with water for at least 60 minutes. Other persons should not touch the treated areas within 60 minutes after applying the drug. After drying, the site of application of the drug should be covered with clothing to exclude contact with other persons.

Children should not be allowed to touch skin areas with applied Lenzetto®. If a child touches such an area, wash the area of ​​the child’s skin with soap and water as soon as possible.

Do not allow pets to lick or touch skin areas treated with Lenzetto®. Small pets can be especially susceptible to the effects of estrogen. If your pet has breast / nipple enlargement and / or vulvar swelling or other abnormalities, contact your veterinarian.

The absorption of estradiol when Lensetto® is applied to the skin of the thighs is comparable to the degree of absorption from the surface of the skin of the forearms, but lower when the drug is applied to the skin of the anterior abdominal wall. Patients who have difficulty applying the drug to non-overlapping skin areas of the same forearm can apply Lenzetto® to the other forearm or inner thighs.

Increased skin temperature

An increase in ambient temperature (for example, in a sauna or while sunbathing) has practically no effect on the degree of absorption of Lenzetto®. However, Lenzetto® should be used with caution at elevated ambient temperatures, that is, in a sauna or while sunbathing.

Applying sunscreen to the skin

When applying sunscreens to the site of application of Lenzetto® in less than 1 hour after its application, the degree of absorption of estradiol may decrease by 10%. The use of sunscreens 1 hour after the application of Lenzetto® can also reduce the absorption of estradiol.

Overweight and obesity

There are limited data on the possibility of reducing the degree of absorption of Lenzetto® in overweight or obese women. During treatment, a dose adjustment of the drug may be required. Dose changes should be agreed with your doctor.

Application in children

Lenzetto® is contraindicated in children.

Elderly patients (over 65 years old)

Experience in treating women over 65 years of age is limited.

 

Possible side effects

The following terminology is used to classify the frequency of adverse effects (according to MedDRA): very frequent (≥1 / 10), frequent (≥1 / 100 to <1/10), infrequent (≥1 / 1000 to <1/100 ), rare (≥1 / 10000 to <1/1000), very rare (<1/10000), frequency unknown (based on available data, frequency cannot be estimated). The only side effect constantly observed and associated with taking the drug is a transient increase in the concentration of uric acid in serum and urine. Uric acid concentrations return to baseline values ​​within a few days after drug withdrawal.

Often (≥1 / 100 to <1/10)

  • headache
  • abdominal pain
  • nausea
  • rash
  • itching
  • uterine / vaginal bleeding, including spotting
  • metrorrhagia
  • weight gain
  • weight loss

Uncommon (≥1 / 1000 to <1/100)

  • hypersensitivity reactions
  • depressed mood
  • insomnia
  • vertigo
  • vertigo
  • visual impairment
  • feeling of a rapid heartbeat
  • increased blood pressure
  • diarrhea
  • dyspepsia
  • erythema nodosum
  • hives
  • skin irritation
  • myalgia
  • breast pain
  • breast tenderness
  • discoloration of the skin in the area of ​​the mammary glands
  • discharge from the mammary glands.
  • polyp of the cervix.
  • endometrial hyperplasia.
  • ovarian cysts.
  • vaginitis.
  • increased activity of gamma glutamyl transferase.
  • increased blood cholesterol levels.
  • swelling.
  • axillary pain.

Rarely (≥1 / 10,000 to <1/1000)

  • anxiety
  • decreased libido
  • increased libido
  • migraine
  • intolerance to contact lenses
  • bloating
  • vomit
  • hirsutism
  • acne
  • muscle spasms
  • dysmenorrhea
  • vaginal bleeding
  • premenstrual syndrome
  • enlargement of the mammary glands
  • increased fatigue

As part of post-registration observation, the following adverse events were recorded:
Skin and subcutaneous tissue disorders

– alopecia
– chloasma
– discoloration of the skin

During treatment with estrogens and / or progestogens, the following adverse reactions were also recorded: angioedema, anaphylactoid / anaphylactic reactions, impaired glucose tolerance, depression, mood swings, irritability, exacerbation of chorea, exacerbation of epilepsy, dementia, exacerbation of bronchial asthma , exacerbation of gallstone disease, pancreatitis, an increase in the size of the liver hemangioma, chloasma or melasma, which may persist even after the drug is discontinued; erythema multiforme, hemorrhagic rash, hair loss on the head, arthralgia, galactorrhea, cystic-fibrous changes in breast tissue, an increase in the size of uterine leiomyoma, changes in the amount of cervical mucus, cervical erosion, vaginal candidiasis, increased existing hypocalcemia.

Contraindications

It is not recommended to start hormone replacement therapy (HRT) if you have any of the conditions listed below. If any of these conditions occurs during HRT, then you should immediately stop using the drug.

  • diagnosed, suspected, or a history of breast cancer
  • diagnosed, suspected estrogen-dependent malignant tumors or their history (including endometrial cancer)
  • vaginal bleeding of unknown etiology
  • untreated endometrial hyperplasia
  • current or history of venous thrombosis or thromboembolism (deep vein thrombosis or pulmonary embolism)
  • diagnosed thrombophilic conditions (eg, protein C, protein S, or antithrombin deficiency)
  • current or history of arterial thromboembolic diseases (including angina pectoris, myocardial infarction, stroke)
  • a history of acute liver disease or liver disease with abnormal liver function tests
  • severe hypertriglyceridemia
  • porphyria
  • hypersensitivity to the active substance or to any of the excipients
  • pregnancy and lactation.
  • children and adolescents up to 18 years old

 

Special instructions

Experience in treating women over 65 years of age is limited.

For the treatment of postmenopausal symptoms, HRT is prescribed only in cases where the existing symptoms have a pronounced effect on the woman’s quality of life. In all cases, a thorough assessment of the risks and benefits is required at least once a year. HRT should be continued as long as the benefits of using the drug outweigh the risks.

Data on the risks associated with HRT in the treatment of early menopause are limited. Because the absolute risk is lower in younger women, the benefit / risk ratio may be more favorable for them than for older women.

Medical examination / follow-up

Before starting or resuming HRT, a thorough medical and family history should be taken. The collected history should be guided by a physical examination (including examination of the pelvic organs and mammary glands), as well as contraindications and precautions for use. During treatment, it is recommended to carry out periodic examinations, the frequency and nature of which must be selected individually for each patient. Women should report breast changes to their doctor or nurse (see Breast Cancer section below). In accordance with the accepted standards of screening, special studies, including mammography, should be carried out, taking into account individual clinical indications.

Conditions to be monitored

Patients should be closely monitored if any of the following conditions / risk factors are present or have a history, as well as their exacerbation during a previous pregnancy or during hormone therapy.

In case of deterioration, exacerbation of the disease or the occurrence of any of these conditions for the first time, a woman should consult a doctor:

– leiomyoma (uterine fibroids) or endometriosis;
– risk factors for the development of thromboembolic diseases (see below);
– risk factors for estrogen-dependent tumors, for example, breast cancer in 1st degree relatives;
– arterial hypertension;
– liver disease (including hepatocellular adenoma);
– diabetes mellitus with or without angiopathy;
– cholelithiasis;
– migraine or severe headaches;
– systemic lupus erythematosus (SLE);
– a history of endometrial hyperplasia (see below);
– epilepsy;
– bronchial asthma;
– otosclerosis.

Reasons for immediate discontinuation of therapy

Therapy should be discontinued if contraindications are identified and under the following conditions:

– cholestatic jaundice or liver dysfunction;

– a significant increase in blood pressure;

– attacks of migraine or unusually severe and frequent headaches for the first time, as well as other symptoms – precursors of cerebrovascular occlusion, the appearance of a migraine-like headache;

– symptoms of thrombotic disorders or if their occurrence is suspected;

– pregnancy.

If the state of health or risk factors change (the appearance of new disorders, worsening of existing ones), it is necessary to re-evaluate the benefit / risk ratio for the patient, taking into account the possible need to discontinue therapy.

Consideration should be given to the likelihood of an increased synergistic risk of thrombosis in women, for whom the increased risk may be higher than the normal cumulative risk of factors. HRT should not be prescribed if the benefit / risk ratio is negative.

Endometrial hyperplasia and cancer

In women with a preserved uterus, the risk of developing endometrial hyperplasia and cancer increases with prolonged estrogen monotherapy. The risk of endometrial cancer is 2 to 12 times higher than in women who have not received hormones, and depends on the duration of treatment and the dose of estrogen. After stopping treatment, the risk remains high for 10 years.

Cyclic administration of progestogens for at least 12 days per month on a 28-day cycle or continuous combination therapy with estrogen and progestogen in women with an intact uterus may prevent this risk from increasing.

The safety of the additional prescription of progestogens against the background of the use of Lenzetto® in relation to the endometrium has not been studied.

Breakthrough bleeding and spotting are sometimes seen in the first few months of treatment. If breakthrough bleeding and spotting are noted some time after the start of therapy or continues after the termination of treatment, it is necessary to conduct an examination and biopsy of the endometrium to exclude malignant neoplasm.

Monotherapy with estrogens can lead to precancerous or malignant changes in the foci of endometriosis. Thus, the need for additional inclusion of progestogens in replacement therapy regimens should be assessed in women with a removed uterus due to the possible presence of residual foci of endometriosis.

Mammary cancer

Women who take estrogen in combination with a progestogen or estrogen alone have an increased risk of breast cancer, depending on the duration of therapy.

Combined estrogen-progestogen therapy

A significant increase in the risk of developing breast cancer in women taking combined estrogen-progestogen drugs for HRT was noted 3 years after the start of treatment.

The use of estrogens as monotherapy

There was no increase in the risk of developing breast cancer in women with a removed uterus receiving HRT only on the basis of estrogen. There is some evidence of a slight increase in the risk of breast cancer, which was significantly lower than in women receiving estrogen-progestogen therapy.

The increase in risk manifests itself over several years of therapy, but it returns to the baseline level within several years (no more than five) after stopping treatment.

With HRT, especially with the combined use of estrogen and progestogen, there is an increase in the density of mammographic images, which can complicate the radiological diagnosis of breast cancer.

Ovarian cancer

The incidence of ovarian cancer is much lower than that of breast cancer.

There is a slightly higher risk in women taking estrogen-containing HRT or combined estrogen- and progestogen-containing drugs, which increases within 5 years of use and gradually decreases after discontinuation of treatment.

Venous thromboembolism

With HRT, the risk of developing venous thromboembolism (VTE), i.e. deep vein thrombosis and pulmonary embolism, increased by 1.3-3 times. The likelihood of VTE is higher in the first year of HRT use.

Patients with a history of VTE or diagnosed thrombophilic conditions have an increased risk of VTE. HRT can increase this risk, so it is contraindicated in this group of patients.

Risk factors for VTE include estrogen intake, advanced age, major surgery, prolonged immobilization, obesity (body mass index> 30 kg / m2), pregnancy / puerperium, SLE, and cancer.

In the postoperative period, all patients should take preventive measures against VTE. In case of anticipated long-term immobilization after planned surgery, it is recommended to suspend HRT 4-6 weeks before surgery. Treatment resumes after full recovery of physical activity.

Women without a history of VTE, but having first-degree relatives with a history of thrombosis and / or thromboembolism at a young age should be offered an examination (screening reveals only a part of thrombophilic disorders). HRT is contraindicated if a thrombophilic defect has been identified that is not associated with thrombosis in other family members or if it is a “severe” defect (eg, antithrombin deficiency, protein S, protein C deficiency, or a combination of defects).

When evaluating the indications for the appointment of HRT, a careful assessment of the benefit / risk ratio in women who are constantly receiving anticoagulants is required.

With the development of VTE, the drug should be discontinued. When the first symptoms of thromboembolism appear (for example, painful swelling of the lower extremities, sudden chest pain, shortness of breath), the patient should immediately consult a doctor.

Coronary artery disease (CHD)

There is no evidence that HRT prevents the development of myocardial infarction in women with or without coronary artery disease.

Combined HRT therapy

The relative risk of coronary artery disease during treatment with combined estrogen-progestogen drugs for HRT slightly increases, including with age. Since the initial absolute risk of developing coronary artery disease largely depends on age, the incidence of additional cases of coronary artery disease in women receiving combined HRT is very low in the group of healthy women at an age close to the onset of menopause, but increases with age.

Estrogen monotherapy

An increase in the risk of coronary heart disease in women after hysterectomy, receiving HRT with estrogens, has not been identified.

Ischemic stroke

The risk of ischemic stroke during therapy with combined drugs and only estrogens increases by 1.5 times. The relative risk does not depend on age or duration of menopause. However, it is known that the initial risk of stroke is highly dependent on age, so the overall risk of stroke in women taking HRT increases with age.

Visual impairment

Cases of retinal vascular thrombosis have been reported in women receiving estrogen treatment. The use of the drug should be discontinued immediately depending on the results of physical examination, that is, sudden complete or partial loss of vision or sudden development of proptosis, diplopia or migraine. If edema of the optic nerve head or retinal vascular lesions is detected, estrogen treatment should be completely canceled.

Dementia

HRT does not improve cognitive function. There are limited data on the risk of dementia in women who have started continuous combined HRT or HRT with estrogens over the age of 65 years.

Liver tumors

Against the background of the use of hormonal substances, which in particular are contained in preparations for HRT, in rare cases, benign, and even less often, malignant liver tumors were observed. In some cases, these tumors have led to life-threatening intra-abdominal bleeding.

In the case of severe pain in the upper abdomen, enlarged liver, or signs of intra-abdominal bleeding, liver tumor should be considered when making a differential diagnosis.

Other states

Estrogens contribute to fluid retention, so patients with heart or renal failure should be monitored closely.

Women with hypertriglyceridemia require careful monitoring with estrogen HRT or combined HRT, since with the use of estrogens, rare cases of a significant increase in the concentration of triglycerides in the blood plasma with the subsequent development of pancreatitis have been observed.

Estrogens increase the level of thyroxine-binding globulin (TSH), which leads to an increase in the total level of thyroid hormones in the blood, measured by levels of protein-bound iodine (PBI), T4 (column chromatography or radioimmunoassay) or T3 (radioimmunoassay). The decrease in the intensity of T3 uptake by the resin reflects an increase in TSH levels. The concentration of free T4 and free T3 does not change. It is possible to increase the content of other binding proteins in plasma, for example, corticosteroid-binding globulin (CBG), sex hormone-binding globulin (SHBG), which leads to an increase in the content of circulating corticosteroid and sex hormones, respectively. Concentrations of free or biologically active hormones do not change. Concentrations of other plasma proteins (angiotensin / renin substrate, alpha-1-antitrypsin, ceruloplasmin) may increase.

Flammable liquids containing ethyl alcohol

Avoid contact with open flames and do not smoke until the spray is completely dry.

Applying sunscreen to the skin

When applying sunscreens to the skin earlier than 1 hour after using Lenzetto®, the degree of absorption of estradiol may decrease by 10%. When sunscreens were applied to the skin approximately 1 hour before the use of Lenzetto®, the degree of absorption of estradiol did not change.

Increased skin temperature

The effect of an increase in ambient temperature when using Lenzetto® was studied, with a 10% difference in the degree of absorption of estradiol. This effect was not clinically significant with daily use of Lenzetto®. Lenzetto® should be used with caution under conditions associated with high temperatures, that is, in a sauna or sunbathing.

Children and adolescents under 18 years of age

There is no indication for the use of estradiol as a transdermal spray, 1.53 mg / dose in children.

Cases of swelling and enlargement of the mammary glands in prepubertal girls, signs of premature puberty, gynecomastia and enlargement of the mammary glands in prepubertal boys after unintentional contact with Lenzetto® are described. In most cases, the changes disappeared after the termination of contact with the drug Lenzetto®.

The physician should pay special attention to unintentional mediated effects of Lenzetto®. The doctor must reliably establish the causes of violations of sexual development in children. When detecting changes in the mammary glands resulting from unintentional exposure to Lenzetto®, the doctor should additionally educate women who communicate with children how to handle Lenzetto®. Women should cover the areas of the skin treated with Lenzetto with clothing in case of possible contact with other persons (especially children). If it is impossible to safely use the drug Lenzetto®, it should be canceled.

Pregnancy and lactation

Lenzetto® is contraindicated during pregnancy. If pregnancy occurs while using Lenzetto®, treatment should be discontinued immediately.

With an unintentional effect on the fetus of a combination of estrogens and progestogens, teratogenic and fetotoxic effects have not been identified.

Lenzetto® is contraindicated during breastfeeding.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Studies of the effect of the drug Lenzetto® on the ability to drive vehicles or work with mechanisms have not been conducted.

 

Overdose

There were no significant adverse reactions after taking high doses of estrogens.

Symptoms: An estrogen overdose may result in nausea, vomiting, breast tenderness, dizziness, abdominal pain, drowsiness / fatigue, and withdrawal bleeding.

Treatment: cancellation of the drug Lenzetto®, symptomatic therapy.

 

How to store Lenzetto

  • Store at a temperature not exceeding 25 °C (77 °F)
  • Do not refrigerate or freeze!
  • Contains ethanol which is flammable. Store away from heaters, open flames, and other sources of ignition.

 

Shelf life – 3 years
Do not use this medicine after the expiry date which is stated on the carton and on the label of the container. The expiry date refers to the last day of that month.


 

Scientific Studies

Additional information

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