Absorlent Matrix is a naturally occurring oestrogen. Oestrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. They modulate the pituitary secretion of gonadotrophins, LH and FSH through a negative feedback system.
Absorlent Matrix acts on the on the estrogen receptors to relieve vasomotor systems (such as hot flashes) and urogenital symptoms (such as vaginal dryness and dyspareunia).
Absorlent Matrix has also been shown to exert favorable effects on bone density by inhibiting bone resorption. Estrogen appears to inhibit bone resorption and may have beneficial effects on the plasma lipid profile. Estrogens cause an increase in hepatic synthesis of various proteins, which include sex hormone binding globulin (SHBG), and thyroid-binding globulin (TBG). Estrogens are known to suppress the formation of follicle-stimulating hormone (FSH) in the anterior pituitary gland.
A note on hyper-coagulable state, cardiovascular health, and blood pressure
Treatment of moderate to severe vasomotor symptoms associated with the menopause.
Treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with the menopause. When prescribing solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.
Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure.
Treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease.
Treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).
Prevention of osteoporosis. When prescribing solely for the prevention of postmenopausal osteoporosis, therapy should only be considered for women at significant risk of osteoporosis and for whom non-estrogen medications are not considered to be appropriate.
Absorlent Matrix is also used to associated treatment for these conditions: Atrophic Vaginitis, Breast Cancer, Breast engorgement caused by Postpartum state, Hypogonadism female, Kraurosis Vulvae, Metastatic Breast Cancer, Osteoporosis, Postmenopausal Osteoporosis, Premature Ovarian Failure (POF), Prostate Cancer, Urogenital atrophy, Vasomotor Symptoms Associated With Menopause, Vulvovaginal Atrophy, Advanced androgen dependent Prostate cancer, Female castration, Hypoestrogenism, Contraception, Hormone Replacement Therapy, Palliation
How Absorlent Matrix works
Estrogen is found in the the breast, uterine, ovarian, skin, prostate, bone, fat, and brain tissues. The main source of estrogen in adult women during the reproductive period of life is the ovarian follicle, which secretes 70 to 500 mcg of estradiol each day. After menopause, however, the majority of endogenous estrogen is produced by transformation of androstenedione (which is secreted by the adrenal cortex) to estrone in the peripheral tissues. Both estrone and its sulphate conjugated form, estrone sulphate, represent the most abundant estrogens found in postmenopausal women.
Absorlent Matrix, however, is considerably more potent than estrone and estriol at the estrogen receptor (ER). As a result, the higher estrone concentration in postmenopausal population, can cause various undesirable effects. These effects may include hot flashes, chills, vaginal dryness, mood swings, irregular menstruation, and chills, in addition to sleep problems.
Absorlent Matrix workings by binding to subtypes of the estrogen receptor: estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). It also exerts potent agonism of G Protein-coupled estrogen receptor (GPER), which is recognized an important regulator of this drug's rapid effects. Once the estrogen receptor has bound to its ligand, it enters the nucleus of the target cell, regulating gene transcription and formation of of messenger RNA. This mRNA makes contact with ribosomes producing specific proteins that express the effect of estradiol upon the target cell. Agonism of estrogen receptors increases pro-estrogenic effects, leading to the relief of vasomotor and urogenital symptoms of a postmenopausal or low estradiol state.
|Trade Name||Absorlent Matrix|
|Estradiol Other Names||17beta oestradiol, beta-Estradiol, cis-Estradiol, Estradiol, Estradiol-17beta, Estradiolum|
|Related Drugs||alendronate, finasteride, tamoxifen, Fosamax, Premarin, testosterone, norethindrone, medroxyprogesterone, megestrol, raloxifene|
More than 95% of estrogens are found to circulate in the blood bound to sex hormone binding globulin (SHBG) and albumin.
|Groups||Approved, Investigational, Vet approved|
|Therapeutic Class||Female Sex hormones|
|Last Updated:||June 7, 2022 at 8:55 pm|
Absorlent Matrix dosage
- Prostate cancer: 10 mg 3 times/day for at least 3 month.
- Menopausal vasomotor symptoms: 1-2 mg/day on a cyclical or continuous regimen
- Prevention of postmenopausal osteoporosis: 0.5 mg/day in cyclical regimen.
- Hypogonadism: 1-2 mg/day in a cyclic regimen.
- Vulvular and vag atrophy: Insert 2-4 g/day for 2 wk. Maintenance: 1 g 1-3 times/wk.
- Postmenopausal vag atrophy; Urogenital symptoms: Insert a ring and keep in place for 90 days.
- Atrophic vaginitis: Insert 1 tab once daily for 2 wk. Maintenance: 1 tab twice wkly. Attempt to discontinue or taper medication at 3-6 monthly intervals.
GI disturbances, genitourinary changes, haematologic disorders, CV and CNS effects, endocrine and metabolic disorders, cholestatic jaundice, local skin reactions, chorea, contact lens intolerance, steeping of corneal curvature, pulmonary thromboembolism, carbohydrate intolerance.
The NOAEL (no-observed-adverse-effect-level) oral toxicity of estradiol after 90 day in rats was 0.003 mg/kg/day for blood, female reproductive, and male reproductive, endocrine, and liver toxicity. Oral TDLO of ethinyl estradiol is 21 mg/kg/21D intermittent, woman) with an oral LD50 of 960 mg/kg in the rat.
There is limited information in the literature regarding estrogen overdose. Absorlent Matrix overdose likely leads to the occurrence of estrogen-associated adverse effects, including nausea, vomiting, abdominal pain, breast tenderness, venous thrombosis, and vaginal bleeding. It is generally recommend to discontinue estradiol treatment and offer supportive care in the case of an overdose.
Conditions exacerbated by fluid retention; hypercalcaemia, cerebrovascular diorders, coronary artery disease, gall bladder diseases; lipid effects; familial defects of lipoprotein metabolism. May increase BP, risk of venous thromboembolism, breast cancer, benign hepatic adenoma, endometrial cancer and size of preexisting uterine leiomyomata. Dosage should be reduced in hepatic impairment. Lactation. Child.
CYP1A2 and CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together.
Food InteractionNo interactions found.
[Minor] Coadministration with grapefruit juice may increase the bioavailability of oral estrogens.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall induced by certain compounds present in grapefruits.
In a small, randomized, crossover study, the administration of ethinyl estradiol with grapefruit juice (compared to herbal tea) increased peak plasma drug concentration (Cmax) by 37% and area under the concentration-time curve (AUC) by 28%.
Based on these findings, grapefruit juice is unlikely to affect the overall safety profile of ethinyl estradiol.
However, as with other drug interactions involving grapefruit juice, the pharmacokinetic alterations are subject to a high degree of interpatient variability.
Also, the effect on other estrogens has not been studied.
Absorlent Matrix Cholesterol interaction
[Moderate] Although estrogens have generally favorable effects on plasma lipids, including increases in HDL and decreases in total cholesterol and LDL, they have also been associated with significant elevations in triglyceride levels, particularly when high dosages are used.
Severe hyperlipidemia is known to sometimes cause pancreatitis.
Patients with preexisting hyperlipidemia may require closer monitoring during estrogen therapy, and adjustments made accordingly in their lipid-lowering regimen.
Absorlent Matrix Hypertension interaction
[Major] The risk of myocardial infarction and strokes, including those associated with oral contraceptive use and some estrogen use, is increased in patients with hypertension.
Moreover, estrogens (and progestogens) may elevate blood pressure and worsen the hypertension, thus compounding the risk.
Clinically significant blood pressure increases have been reported during estrogen therapy, particularly in patients receiving high dosages or treated with oral contraceptive combinations having high progestational activity.
These effects also increase with duration of therapy and patient age.
Therapy with estrogens should be administered cautiously in patients with preexisting hypertension.
Patients should be monitored for changes in cardiovascular status, and their antihypertensive regimen adjusted or estrogen therapy withdrawn as necessary.
In patients requiring contraception, alternative methods should be considered for those who are hypertensive, over age 35, and smoke.
Absorlent Matrix Drug Interaction
Moderate: levothyroxine, levothyroxine
Unknown: duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, montelukast, montelukast, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam, cetirizine, cetirizine
Absorlent Matrix Disease Interaction
Major: abnormal vaginal bleeding, carcinomas (estrogenic), hypercalcemia in breast cancer, hypertension, thromboembolism/cardiovascular, hepatic neoplasms
Moderate: angioedema, gallbladder disease, hypercalcemia, hyperlipidemia, liver disease, melasma, depression, fluid retention, glucose intolerance, retinal thrombosis, thyroid function tests
Volume of Distribution
Estrogens administered exogenously distribute in a similar fashion to endogenous estrogens. They can be found throughout the body, especially in the sex hormone target organs, such as the breast, ovaries and uterus.
The absorption of several formulations of estradiol is described below:
Oral tablets and injections
First-pass metabolism in the gastrointestinal tract rapidly breaks down estradiol tablets before entering the systemic circulation. The bioavailability of oral estrogens is said to be 2-10% due to significant first-pass effects. The esterification of estradiol improves the administration (such as with estradiol valerate) or to sustain release from intramuscular depot injections (including estradiol cypionate) via higher lipophilicity. After absorption, the esters are cleaved, which leads to the release of endogenous estradiol, or 17β-estradiol.
The transdermal preparations slowly release estradiol through intact skin, which sustains circulating levels of estradiol during a 1 week period of time. Notably, the bioavailability of estradiol after transdermal administration is about 20 times higher than after oral administration. Transdermal estradiol avoids first pass metabolism effects that reduce bioavailability. Administration via the buttock leads to a Cmax of about 174 pg/mL compared to 147 pg/mL via the abdomen.
After daily administration, the spray formulations of estradiol reach steady state within 7-8 days. After 3 sprays daily, Cmax is about 54 pg/mL with a Tmax of 20 hours. AUC is about 471 pg•hr/mL.
Vaginal ring and cream preparations
Absorlent Matrix is efficiently absorbed through the mucous membranes of the vagina. The vaginal administration of estrogens evades first-pass metabolism. Tmax after vaginal ring delivery ranges from 0.5 to 1 hour. Cmax is about 63 pg/mL. The vaginal cream preparation has a Cmax of estradiol (a component of Premarin vaginal estrogen conjugate cream) was a Cmax of 12.8 ± 16.6 pg/mL, Tmax of 8.5 ± 6.2 hours, with an AUC of 231 ± 285 pg•hr/mL.
The terminal half-lives for various estrogen products post oral or intravenous administration has been reported to range from 1-12 hours. One pharmacokinetic study of oral estradiol valerate administration in postmenopausal women revealed a terminal elimination half-life of 16.9 ± 6.0 h. A pharmacokinetic study of intravenous estradiol administration in postmenopausal women showed an elimination half-life of 27.45 ± 5.65 minutes. The half-life of estradiol appears to vary by route of administration.
In one pharmacokinetic study, the clearance of orally administered micronized estradiol in postmenopausal women was 29.9±15.5 mL/min/kg. Another study revealed a clearance of intravenously administered estradiol was 1.3 mL/min/kg.
Absorlent Matrix is excreted in the urine with both glucuronide and sulfate conjugates.
Pregnancy & Breastfeeding use
Pregnancy Category X. Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Hypersensitivity; undiagnosed vag bleeding; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumor; porphyria; pregnancy.
Store at room temperature.
You find simplified version here Absorlent Matrix
Absorlent Matrix contains Estradiol see full prescribing information from innovator Absorlent Matrix Monograph, Absorlent Matrix MSDS, Absorlent Matrix FDA label
What is Absorlent Matrix used for?
Absorlent Matrix is a form of estrogen, a female sex hormone that regulates many processes in the body. Absorlent Matrix is used to treat menopause symptoms such as hot flashes and vaginal changes, and to prevent osteoporosis (bone loss) in menopausal women.
How safe is Absorlent Matrix?
In postmenopausal women, estrogens, taken with or without a Absorlent Matrix, increase the risk of cancer of the breast/ovaries, stroke, dementia, and serious blood clots. When used along with a Absorlent Matrix, estrogens also increase the risk of heart disease (such as heart attacks). Absorlent Matrix topical should not be used to prevent heart disease, stroke, or dementia.
How does Absorlent Matrix work?
Absorlent Matrix works by replacing Absorlent Matrix that your body normally produces.
What are the common side effects of Absorlent Matrix?
Common side effects of Absorlent Matrix are include:
- Abdominal cramping.
- Breakthrough bleeding.
- Breast enlargement.
- Breast tenderness/pain/swelling.
- Freckles or darkening of facial skin (melasma)
- Changes in menstrual periods.
Is Absorlent Matrix safe during pregnancy?
Absorlent Matrix should not be used during pregnancy. There appears to be little or no increased risk of birth defects in children born to women who inadvertently used Absorlent Matrix during early pregnancy.
Is Absorlent Matrix safe during breastfeeding?
Absorlent Matrix is not recommended in nursing mothers. Absorlent Matrix pass into the breast milk and may decrease the amount and quality of breast milk. Caution should be exercised in mothers who are using estrogen and breast-feeding
Can I drink alcohol with Absorlent Matrix?
You should avoid smoking and drinking alcohol. You may also wish to not consume grapefruit or grapefruit juice while using Absorlent Matrix as it may result in increased levels in the blood.
What is the best time to take Absorlent Matrix?
Take this medication by mouth with or without food as directed by your doctor. You may take it with food or right after a meal to prevent stomach upset.
How many time can I take Absorlent Matrix daily?
One to three times a day for 3 to 6 months.
How long does Absorlent Matrix take to work?
It can take up to 4 months to see the full effect of the Absorlent Matrix. Your doctor may reconsider continuing your Absorlent Matrix treatment or may lower your dose several times within the first one or two months, and every 3 to 6 months after that.
Who should not take Absorlent Matrix?
You should not use Absorlent Matrix if you have: undiagnosed vaginal bleeding, liver disease, a bleeding disorder, or if you have ever had a heart attack, a stroke, a blood clot, or cancer of the breast, uterus/cervix, or vagina. Do not use Absorlent Matrix if you are pregnant.
What happen If I missed Absorlent Matrix?
If you miss a dose and it is more than 2 hours until your next dose, take the missed dose as soon as possible with food, then go back to your regular time. If you miss a dose and it is within 2 hours of your next evening dose, skip the missed dose and go back to your regular dosing schedule.
What happens if I overdose?
Seek emergency medical attention. Overdose can result in nausea, vomiting and vaginal bleeding. Symptoms of an Absorlent Matrix overdose include: Breast tenderness. Drowsiness. Excessive vaginal bleeding (2 to 7 days after overdose).
What happen If I stop taking Absorlent Matrix?
Most don't have any problems while they stop, however, stopping suddenly does increase the risk of menopausal symptoms returning, so you should not stop taking your HRT without consulting your doctor. Doctors may differ in how they taper their patients off HRT.
Will Absorlent Matrix affect my fertility?
Yes, and on either end of the spectrum. Absorlent Matrix is one of the hormones that keep our menstrual cycles going, so when levels are too low or too high, that can cause disruption.
Can Absorlent Matrix cause heart palpitations?
Another common symptom that women experience during menopause due to low Absorlent Matrix levels are heart palpitations. Lower Absorlent Matrix levels can overstimulate the heart and cause arrhythmias.
Can Absorlent Matrix cause liver problems?
Postmenopausal women are also reported to have a higher risk of liver fibrosis than premenopausal women, suggesting that Absorlent Matrix is associated with liver protection from fibrosis.
Can Absorlent Matrix affet my kidney?
One of the most important actions of the Absorlent Matrix is represented by the protective effect on the kidneys, Absorlent Matrix attenuating glomerulosclerosis and tubulo-interstitial fibrosis.
Does Absorlent Matrix make my gain weight?
Lower levels of Absorlent Matrix may lead to weight gain.
Can Absorlent Matrix cause hair loss?
Absorlent Matrix is related to hair growth — and hair loss.