The mechanism of action Vagifem 10 mcg
Vagifem contains a hydrophilic cellulose matrix, which, with the interaction with moisture, provide a gradual release of 17-beta-estradiol.
Estrogen 17-beta-estradiol contained in the product Vagifem is chemically and biologically identical to endogenous human estradiol.
Endogenous 17 beta-estradiol stimulates and supports the primary and secondary female sexual characteristics. The biological effect of 17 beta-estradiol through a number of nuclear receptors.
Estrogen controls the maturation of the vaginal epithelium, increases the amount of surface and intermediate cells of the mucosa. Estrogen keeps the pH in the vagina at the level of 4.5, which promotes the growth of normal vaginal flora – Lactobacillus Doerlein.
Pharmacokinetics Vagifem 10 mcg
Estrogen-containing drugs are well absorbed through the skin, mucous membranes, as well as through the gastrointestinal tract. Vaginal estrogen administration immediately get into the scene.
Single-center, randomized, double-blind crossover study the pharmacokinetics of Vagifem showed that the peak level of 17 beta-estradiol after a single application Vagifem reached 175 pmol / L (48 pg / ml). After 14 days of treatment was recorded only a slight uptake of 17-beta-estradiol, with an average level postmenopauznom estrogen.
Another study of patients with a mean age of 52 years, showed that when taking Vagifem for 12 weeks, the level of estrogen was detected 50 pg / ml, the accumulation of estradiol in the body have been recorded. The average concentration of 17-beta-estradiol remained within the normal postmenopausal range.
Monitoring the level of estrone in the 12 weeks of Vagifem have shown that increasing the concentration of estrone in the body does not occur, the concentrations are within the postmenopausal range.
Estrogen metabolites are derived primarily in the urine as glucuronides and sulfates.
Dosage and administration Vagifem 10 mcg
Vagifem is introduced deep into the vagina with an applicator.
Initial dosage: 1 tablet daily vaginal in two weeks.
Maintenance dose: 1 vaginal tablet twice a week.
Treatment can be initiated at any convenient day.
If you miss a dose, then continue the treatment as soon as you remember. You should not use two doses at once.
To start and continue treatment postmenopausal symptoms should use the lowest effective dose for a short time (see Warnings and Precautions).
Vagifem can be used in women with a healthy uterus, with extirpation or resection of the uterus.
During treatment, especially in the first 2 weeks, there may be a minimal absorption of estrogen, but estrogen levels in the blood does not exceed the average postmenopauzny and progestogen supplementation is not required.
How to use the drug Vagifem 10 mcg
Open the blister.
Enter the applicator deep into the vagina until resistance is felt (approximately 10-12 cm).
Enter the tablet by pressing the plunger of the applicator.
The applicator can be removed.
Contraindications Vagifem 10 mcg
Vagifem is not used in the presence of hypersensitivity to the drug, or if you suspect the presence of breast cancer.
Other conditions that contraindicated the use of Vagifem: Porphyria, genital bleeding of unknown etiology, pregnancy or suspected pregnancy, active deep venous thrombosis, thromboembolism, active or recent (eg last year) arterial thromboembolic disease (eg, angina, myocardial infarction, stroke), known or suspected estrogen-dependent cancers (eg endometrial cancer), endometrial hyperplasia, deep vein thrombosis, pulmonary embolism in history.
Warnings and Precautions Vagifem 10 mcg
For the treatment of postmenopausal symptoms, hormone replacement therapy should be initiated only when symptoms that reduce quality of life. In all cases, at least once a year should evaluate the risks and benefits of treatment. Treatment should last only as long as the benefits of treatment outweigh the risks.
Before starting hormone replacement therapy should be to compile a complete family history. During treatment, periodic check-ups are necessary. Women should be informed about any changes in the breast should be reported to your doctor or nurse. Investigations, including mammography, should be in accordance with the peculiarities of history and standard clinical practice. All women who have already started or start hormone replacement therapy should be informed about the risks and benefits of taking estrogen and progesterone. In most cases, when long-term hormone replacement therapy, the risk of complications exceeds the benefits.
Conditions that require monitoring Vagifem 10 mcg
If you marked any of the following conditions that are aggravated by pregnancy or hormone replacement therapy before, remember that you must be kept under close medical supervision:
Leiomyoma of the uterus or endometriosis
The presence of thromboembolic disorders, a history or presence of risk factors for venous thromboembolism
Hypertonic disease
Liver disease (eg liver adenoma)
Diabetes mellitus with vascular complications or without
Cholelithiasis
Migraine or severe headaches
Systemic lupus erythematosus
Endometrial hyperplasia
Epilepsy
Asthma
Otosclerosis.
Thanks to the local application of low doses of estradiol using Vagifem , renewal or worsening these diseases are less likely than a systemic treatment of estrogen.
Treatment should be discontinued in patients following conditions:
Jaundice or deterioration in liver function
Significant increase in blood pressure
Occurrence of migraine or headache
Pregnancy
Endometrial hyperplasia
Women with abnormal bleeding of unknown etiology should undergo a more thorough investigation because Vagifem may promote malignant growth of the endometrium.
The risk of endometrial cancer after treatment with oral administration of estrogen depends on the duration of treatment and received doses.
As a general rule, estrogen hormone replacement therapy is prescribed for no more than a year after that to pass muster gynecologist. As already mentioned, Vagifem provides the local release of estradiol and, hence, a complication referred to states is less likely in the treatment of Vagifem, than with the systemic treatment of estrogen.
Breast cancer Vagifem 10 mcg
Systemic estrogens may increase the risk of breast cancer. The relative risk of breast cancer higher when using combined estrogen and progesterone containing drugs.
Other conditions that require close supervision of a doctor for treatment:
Venous thromboembolism
Renal failure,
Ovarian Cancer
Stroke.
Pregnancy Vagifem 10 mcg
Vagifem is not indicated for pregnancy. If pregnancy occurred during treatment Vagifem , treatment should be discontinued immediately. Epidemiological studies have not revealed teratogenic or fetotoxic effect.
Use in lactation Vagifem 10 mcg
Vagifem is not shown during lactation.
Side Effects Vagifem 10 mcg
The most common side effects are registered at reception Vagifem: Headache, nausea, vomiting, abdominal discomfort, bloating, dyspepsia, vaginal bleeding, discomfort in the vagina, breast swelling and soreness in the chest, peripheral edema (1 per 10-100 patients).
Very rarely observed migraine, depression, insomnia, allergic reactions, hypersensitivity reactions, weight gain, deep vein thrombosis, diarrhea, breast cancer, endometrial hyperplasia, vaginal irritation, pain in the vagina, the vaginal mucosa ulceration, increased estrogen levels in the blood, the absence of the effect of the drug (1 case per 10,000 patients).
Overdose Vagifem 10 mcg
Overdoses have been reported.
Vagifem is intended for topical intravaginal treatment. Dose 17-beta-estradiol is so low that even some vaginal tablets do not lead to an increase in estrogen levels to numbers observed after oral treatment.
