Norgestrel + ethinylestradiol

High risk of arterial or venous thrombotic diseases such as coronary artery disease, cerebrovascular disease, current or history of DVT or pulmonary embolism, inherited or acquired hypercoagulopathies (e.g. protein C or S deficiency, factor V Leiden mutation, prothrombin mutation, antithrombin deficiency), thrombogenic valvular or rhythm diseases of the heart (e.g. subacute bacterial endocarditis with vascular disease, atrial fibrillation); diabetes mellitus with vascular disease, uncontrolled hypertension or hypertension with vascular disease; headaches with focal neurological symptoms, migraine with aura or migraine headaches in women aged >35 years, SLE with unknown or positive antiphospholipid antibodies, women aged >35 years who smoke. Current or history of breast cancer or other estrogen- or progestin-sensitive cancer (e.g. endometrial cancer), undiagnosed abnormal uterine bleeding, cholestatic jaundice of pregnancy, jaundice with prior combination hormonal contraceptive use, hepatic tumours (benign or malignant) or hepatic disease (e.g. acute viral hepatitis, severe [decompensated] cirrhosis). Pregnancy. Concomitant use with hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir.

Patient with a tendency to or history of chloasma gravidarum; current or family history of hypertriglyceridaemia, risk factors for CV disease (e.g. hypertension, high LDL, low HDL, smoking), diabetes or prediabetes, diseases which may be exacerbated by fluid retention; history of depression; hereditary angioedema, strong family history of breast cancer, breast nodules. Not indicated for use prior to menarche or in postmenopausal women. Not recommended for women with complicated organ transplants. Obese patient. Renal impairment. Lactation. Consider discontinuation at least 4 weeks before and 2 weeks after elective surgery associated with increased risk of thromboembolism and during or after periods of prolonged immobilisation. Monitoring Parameters Assess pregnancy status prior to therapy and before initiating a new dosing cycle when 2 consecutive menstrual periods are missed. Monitor blood pressure (at baseline and yearly), lipid profile (in patients with hyperlipidaemias), glucose (in diabetic patients), and LFTs. Obtain weight at baseline (BMI at baseline may be helpful to monitor changes during therapy). Monitor signs and symptoms of depression, thromboembolic disorders, bleeding irregularities, and vision changes. Perform adequate diagnostic measures to rule out malignancy in all cases of undiagnosed abnormal vaginal bleeding.

Significant: Increased risk of breast and cervical cancer; chloasma; unscheduled (breakthrough or intracyclic) vaginal bleeding and spotting; amenorrhoea, oligomenorrhoea; cholestasis, gallbladder disease; changes in lipid levels (including serum triglycerides), decreased glucose tolerance, hypertension, fluid retention; increased thyroid-binding globulin, sex hormone-binding globulin and cortisol-binding globulin levels; retinal vascular thrombosis; depression; severe headache/migraine. Rarely, hepatocellular carcinoma (long-term use). Eye disorders: Steepening of corneal curvature, intolerance to contact lenses. Gastrointestinal disorders: Nausea, vomiting, abdominal pain or cramps, bloating. General disorders and administration site conditions: Fatigue. Investigations: Weight increase or decrease. Metabolism and nutrition disorders: Increased appetite. Nervous system disorders: Headache, nervousness. Reproductive system and breast disorders: Breast tenderness, enlargement, or secretion; cervical erosion, dysmenorrhoea, vaginal discharge, vaginal candidiasis. Skin and subcutaneous tissue disorders: Acne, rash. Vascular disorders: Aggravation of varicose veins.
Potentially Fatal: Venous thromboembolism, arterial thrombosis (e.g. MI, stroke). Rarely, hepatic adenomas.

Decreased serum concentration with CYP3A4 inducers (e.g. phenytoin, barbiturates, carbamazepine, topiramate, bosentan, felbamate, griseofulvin, oxcarbazepine, rifampicin, rifabutin, rufinamide, aprepitant, etravirine). Increased serum concentration with CYP3A4 inhibitors (e.g. itraconazole, ketoconazole). Ethinylestradiol: May decrease the serum concentration of lamotrigine. May increase the serum concentration of ciclosporin, tizanidine, and theophylline. May diminish the therapeutic effect of thyroid products. Decreased exposure with colesevelam. Increased serum concentration when given with ascorbic acid.

Oestrogens & Progesterones & Related Synthetic Drugs / Oral Contraceptives

G03CA01 - ethinylestradiol ; Belongs to the class of natural and semisynthetic estrogens used in estrogenic hormone preparations.
L02AA03 - ethinylestradiol ; Belongs to the class of estrogens.