Product Information
Registration Status: ActiveEVRA TRANSDERMAL PATCH (6mg/600mcg) is approved to be sold in Singapore with effective from 2003-09-17. It is marketed by JOHNSON & JOHNSON PTE LTD, with the registration number of SIN12423P.
This product contains Ethinylestradiol 600mcg/patch, and Norelgestromin 6mg/patch in the form of PATCH. It is approved for TRANSDERMAL use.
This product is manufactured by LTS LOHMANN THERAPIE-SYSTEME AG in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A semisynthetic alkylated estradiol with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally and is often used as the estrogenic component in oral contraceptives. Ethinyl estradiol is marketed mostly as a combination oral contraceptive under several brand names such as Alesse, Tri-Cyclen, Triphasil, and Yasmin. The FDA label includes a black box warning that states that combination oral contraceptives should not be used in women over 35 years old who smoke due to the increased risk of serious cardiovascular side effects.
Indication
For treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.
Mechanism of Action
Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. This cascade is initiated by initially binding to the estrogen receptors. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).
Pharmacokinetics
- Absorption
- Rapid and complete absorption follows oral intake of ethinyl estradiol (bioavailability 43%).
- Distribution
- Metabolism
- Hepatic. Quantitatively, the major metabolic pathway for ethinyl estradiol, both in rats and in humans, is aromatic hydroxylation, as it is for the natural estrogens.
- Elimination
Toxicity
Oral, mouse LD50: 1737 mg/kg. Symptoms of overdose include nausea and vomiting, and withdrawal bleeding may occur in females. The FDA label includes a black box warning that states that combination oral contraceptives with ethinyl estradiol should not be used in women over 35 years old who smoke due to the increased risk of serious cardiovascular side effects.
Active Ingredient/Synonyms
17-ethinyl-3,17-estradiol | 17-ethinyl-3,17-oestradiol | 17-ethinylestradiol | 17alpha-Ethinyl estradiol | 17α-ethynylestradiol | Ethinylestradiol | Ethinylestradiolum | Ethinyloestradiol | Ethynyl estradiol | Etinilestradiol | Ethinyl Estradiol |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
Description
Norelgestromin is a drug used in contraception. Norelgestromin is the active progestin responsible for the progestational activity that occurs in women after application of ORTHO EVRA patch.
Indication
Norelgestromin is used for contraception and menopausal hormonal therapy. Norelgestromin may potentially be used in breast cancer treatment due to its inhibitory effect on estrone sulfatase . They convert sulfated steroid precursors to estrogen during pregnancy.
Mechanism of Action
Norelgestromin inhibits estrone sulfatase, which converts sulfated steroid precursors to estrogen during pregnancy. Norgelgestromin/ethinylestradiol suppresses follicular development, induces changes to the endometrium, which decreases chances of implantation and thickens the cervical mucus, impeding sperm swimming into the uterus. It also has similar agonisting binding affinities as its parent compound, Norgestimate, for progesterone and estrogen receptors.
Active Ingredient/Synonyms
17-Deacetylnorgestimate | 17-Deacylnorgestimate | 18-Methylnorethindrone oxime | D-Norgestrel 3-oxime | Deacetylnorgestimate | Levonorgestrel 3-oxime | Levonorgestrel oxime | Norplant 3-oxime | Norelgestromin |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.