Ethinyl Estradiol / Norelgestromin is a contraceptive skin patch which is used to prevent pregnancy.
Indications for use
Mechanism of action
Ethinyl Estradiol / Norelgestromin is a transdermal delivery system (TDS), which delivers hormones to the dermis and hypodermis, that enter the body through the bloodstream. Delivered hormones cause changes in the body, preventing pregnancy. The active substances of the patch depress the pituitary activity in the synthesis of gonadotropic hormones. The drug prevents the follicle from ripening and ovulation does not occur. The drug creates an artificial temporary anovulatory infertility. In addition, the drug causes thickening of the cervical mucus, which worsens the penetration of spermatozoa into the uterus. In addition, the hormones cause changes in the endometrium, and it becomes immune to blastocyst transplantation. Contraception with the help of the transdermal system is characterized by high reliability (99.4%).
Dosage and mode of application
Ethinyl Estradiol / Norelgestromin is a patch that contains 6 mg of norelgestromin and 600 mcg of ethinyl estradiol. The patch is glued to the skin according to the instructions on the first day of menstruation and is changed every week. Do not use a patch from the 22nd to the 28th day of your period. Use a new patch with the first day of your next menstruation. The use of this drug requires consultation and supervision of a doctor.
In order to postpone menstruation for one period, a woman should stick a new plaster with the drug at the beginning of the 4th week (22nd day), thus missing the period free from the use of the contraceptive. Intermenstrual bleeding or spotting may occur. After 6 consecutive weeks of using the patch, you should be a 7-day interval. After the end of this interval, regular use of the drug is resumed.
If a woman wants to change the “change day” at the appointed day (during the week, free from the application), she must complete the current period by removing the third plaster with the drug. A woman can choose a new “change day” by gluing the first strip of the drug of the next period on the selected day. Period without using the drug, in no case should exceed 7 days. The shorter this period, the higher the probability that a woman will not have another menstrual period, and during the next contraceptive period, intermenstrual bleeding or spotting may occur.
Common side effects of Ethinyl Estradiol / Norelgestromin:
- central and peripheral nervous system: dizziness, migraine, paresthesia, hypesthesia, convulsions, tremor, emotional lability, depression, anxiety, insomnia, drowsiness;
- sense organs: conjunctivitis, visual impairment;
- CCC: increased blood pressure, palpitations, edematous syndrome, varicose veins;
- digestive system: gingivitis, anorexia or increased appetite, gastritis, gastroenteritis, dyspepsia, abdominal pain, vomiting, diarrhea, flatulence, constipation, hemorrhoids;
- respiratory system: infections of the upper respiratory tract, shortness of breath, bronchial asthma;
- reproductive system: pain with sexual intercourse (dyspareunia), vaginitis, decreased libido, breast enlargement, menstrual irregularities (including intermenstrual bleeding, hypermenorrhea), changes in vaginal secretion, changes in cervical mucus, lactation not occurring in connection with childbirth, abnormal ovarian function, mastitis, mammary fibroadenoma, ovarian cysts;
- urinary system: infection of the urinary tract;
- musculoskeletal system: muscle cramps, myalgia, arthralgia, tendonosis, muscle weakness;
- skin: itching, urticaria, rash (including bullous), contact dermatitis, acne, pigmentation disorder, eczema, increased sweating, alopecia, photosensitivity, dry skin;
- metabolism: weight gain, hypertriglyceridemia, hypercholesterolemia;
- other: flu-like syndrome, fatigue, allergic reactions, chest pain, asthenic syndrome, syncope, anemia, abscesses, lymphadenopathy.
Rare side effects: hyper- or hypotonic muscle, impaired coordination of movements, dysphonia, hemiplegia, neuralgia, stupor, increased libido, depersonalization, apathy, paranoia, benign breast tumors, pain in the perineum, ulceration of the mucous membrane of the vulva, atrophy of the mammary glands, lowering of the blood pressure, skin rash, dry mouth or increased salivation, colitis, pain during urination, hyperprolactinaemia, melanosis, skin pigmentation disorders, chloasma, xerophthalmia, inflammation of the subcutaneous tissue, intolerance to ethanol, cholecystitis, cholelithiasis, impaired liver function, purpura, blood flushes to the face, thrombosis (including deep vein thrombosis, pulmonary arterial thrombosis), thrombophlebitis of superficial veins, pain in the veins, embolism of the pulmonary artery.
Ethinyl Estradiol / Norelgestromin transdermal system is contraindicated in the following conditions (present or in the anamnesis):
- Arterial thrombosis, including acute disturbance of cerebral circulation, myocardial infarction, retinal arterial thrombosis or thrombosis precursors (including angina pectoris or transient ischemic attack);
- Hereditary hyslipoproteinemia;
- Risk factors for arterial thrombosis: diabetes mellitus with vascular lesions, severe arterial hypertension, hereditary dyslipoproteinemia;
- Hereditary predisposition to venous or arterial thrombosis, for example, resistance of activated protein C, deficiency of antithrombin III, deficiency of protein C, deficiency of protein S, hyperhomocysteinemia and presence of antiphospholipid antibodies (antibodies against cardiolipin, lupus anticoagulant);
- Venous thrombosis, including deep vein thrombosis, pulmonary thromboembolism;
- Migraine with aura;
- Adenoma or carcinoma of the liver;
- Age under 18 years;
- Breast cancer, endometrial cancer or other hormone-dependent tumors;
- Genital bleeding;
- Postmenopausal period;
- Postpartum period (4 weeks).
Do not apply the patch to the mammary glands, hyperemic or damaged skin.
- Systemic lupus erythematosus;
- Family history of venous or arterial thromboembolism;
- Violations of the menstrual period;
- Diseases of the liver or kidney;
- Hemolytic-uremic syndrome;
- Thrombophlebitis of superficial veins;
- Arterial hypertension;
- Long-term immobilization;
- Crohn’s disease;
- Ulcerative colitis;
- Acute disruption of liver function during a previous pregnancy or previous use of oral hormonal contraceptives;
- Damage to the valvular apparatus of the heart;
- Impaired renal function.
Medicines or herbal products that can reduce the effectiveness of Ethinyl Estradiol / Norelgestromin:
- some antiepileptic drugs (carbamazepine, felbamate, oxcarbazepine, phenytoin, rufinamide, topiramate);
- some HIV protease inhibitors or their combinations (nelfinavir, ritonavir, protease inhibitors, ritonavir-boosted);
- some non-nucleoside reverse-inhibitors.
Some drugs and grapefruit juice can increase the level of ethinyl estradiol in blood plasma, provided they are co-administered. These include:
- ascorbic acid;
- inhibitors CYP3A4 (including itraconazole, ketoconazole, voriconazole, fluconazole and non-peptide juice);
- some HIV protease inhibitors (eg, atazanavir, indinavir);
- HMG-CoA reductase inhibitors (including atorvastatin and rosuvastatin);
- some non-nucleoside reverse-inhibitor transcriptase (e.g., etravirine).
Ethinyl estradiol/norelgestromin can increase the levels of the following drugs in blood plasma:
The transdermal patch can reduce the level of the following drugs in plasma:
- salicylic acid;
Breastfeeding and pregnancy
Ethinyl Estradiol / Norelgestromin TDS is contraindicated during pregnancy and breastfeeding.
What to do if the contraceptive patch falls off?
If Ethinyl Estradiol / Norelgestromin transdermal patch has completely or partially fallen off, then an insufficient amount of its active ingredients is supplied to the blood.
Even with a partial falling off of the transdermal patch:
- less than within a day (up to 24 h): re-glue the patch to the same place or immediately replace it with a new transdermal patch. No additional contraceptives are required. The next patch must be glued on the usual “change day”.
- more than 24 hours and longer, and if the woman does not know exactly when the transdermal patch has partially or completely fallen off: pregnancy may occur. A woman should immediately begin a new period by gluing a new patch and consider this day as the first day of the period.
Additional methods of contraception should be used only in the first 7 days of a new period. Do not try to glue the transdermal patch again if it has lost its adhesive properties; instead, you need to immediately glue a new transdermal delivery system. Do not use additional adhesive tapes or bandages in place the patch.
What if I miss a “change day”?
At the beginning of any contraceptive period (1st week / 1st day):
- a woman should glue the first transdermal patch of a new period as soon as she remembers it. This day is considered a new “1st day” and a new “change day”. Barrier birth control methods should be used during the first 7 days of a new period. In the case of sexual contact during an extended period without the use of contraception, conception may occur.
In the middle of the cycle (2nd week / 8th day or 3rd week / 15th day):
- one or two days (up to 48 hours) passed from the “change day”: a woman should immediately glue a new patch. The next transdermal patch must be glued to the usual “change day”. If the woman correctly applied the transdermal patch within 7 days preceding the first missed “change day” of the transdermal patch, additional contraception is not required;
- more than two days (48 hours or more) have passed from the “change day”: there is an increased risk of pregnancy. A woman should stop the current contraceptive period and immediately begin a new 4-week period by gluing a new transdermal patch. This day is considered a new “1st day” and a new “change day” is counted. Barrier contraception should be used during the first 7 days of the new period.
At the end of the period (week 4 / day 22):
- If Ethinyl Estradiol / Norelgestromin transdermal patch is not removed at the beginning of the 4th week (22nd day), then it should be removed as soon as possible. The next contraceptive period should begin on the usual “change day”, which is the next day after the 28th day. Additional contraception is not required.
In women with a body weight of more than 90 kg, the contraceptive effect of Ethinyl Estradiol / Norelgestromin patch may be reduced.
There is no clinical evidence that the transdermal delivery system is safer than oral contraceptives.
Before starting or resuming the use of the transdermal therapeutic system, it is necessary to collect a detailed medical history (including a family history) and to exclude pregnancy. It is necessary to measure blood pressure and conduct a physical examination taking into account contraindications and warnings.
If you suspect a hereditary predisposition to venous thromboembolism, you should get advice from a specialist before deciding whether to use hormonal contraception.
Women who use combined oral contraceptives may develop liver tumors that can cause life-threatening intra-abdominal bleeding. If you have a severe pain in the upper abdomen, augmentation of the liver, or symptoms of intra-abdominal bleeding, the differential diagnosis should be performed to exclude a possible liver tumor.
In women with hypertriglyceridemia or this disease in a family history, the risk of pancreatitis may be increased.
Hormonal contraceptives can affect some endocrine indicators, markers of liver function and blood components:
Ethinyl Estradiol / Norelgestromin does not protect against HIV infection (AIDS) and other sexually transmitted diseases.
Influence on the ability to driving motor transport and management of mechanisms is not revealed.