Ethinylestradiol + Levonorgestrel

This is indicated for the prevention of pregnancy in women who elect to use oral contraceptives as a method of contraception. Oral contraceptives are highly effective. Table II lists the typical accidental pregnancy rates for users of combination oral contraceptives and other methods of contraception. The efficacy of these contraceptive methods, except sterilization, the IUD, depends upon the reliability with which they are used. Correct and consistent use of methods can result in lower failure rates.

Combination of hormonal contraceptives inhibits ovulation by modulating pituitary secretion of gonadotrophins, luteinising hormone and follicle stimulating hormone through a negative feedback system. They reduce sperm penetration if ovulation does occur by altering the cervical mucus; cause changes in the endometrium which reduce the risk of nidation and may change the tubal transport of the ova through the fallopian tubes.

Monophasic combined oral contraceptive (COC): levonorgestrel 150-250 mcg + ethinylestradiol 30 mcg once daily.

Triphasic COC: levonorgestrel 50-125 mcg + ethinylestradiol 30-40 mcg once daily.

CYP3A4 inducers may decrease levels/effects eg aminoglutethimide, carbamazepine, nafcillin, nevirapine, atazanavir, nelfinavir, phenobarbital, phenytoin, lamotrigine, rifamycins, griseofulvin and ritonavir; ampicillin, tetracycline and other antibiotics may reduce efficacy; oestrogens may antagonise anticoagulant effect of coumarins; may inhibit metabolism of prednisolone and ciclosporin; may reduce clearance of alprazolam, chlordiazepoxide, diazepam; may increase clearance of lorazepam, oxazepam, temazepam.

Pregnancy, undiagnosed vaginal bleeding, severe arterial disease (or family history of atherogenic lipid profile); liver adenoma; porphyria; after evacuation of hydatidiform mole; history of breast cancer; hepatic impairment; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumour; smoking ≥40 cigarettes daily; >50 yr; diabetes complications present; BMI >39 kg/m2; migraine with typical focal aura, lasting >72 hr despite treatment or migraine treated with ergot derivatives; BP >160 mmHg systolic and 100 mmHg diastolic; transient ischaemic attacks without headaches; SLE; gallstones; history of haemolytic uraemic syndrome, pruritis during pregnancy; cholestatic jaundice; chorea or deterioration of otosclerosis pemphigoid; breast feeding during 1st 6 mth after delivery.

Menstrual irregularities; headache, dizziness; breast discomfort; gynaecomastia; depression; disturbance of appetite; wt changes; fluid retention; oedema; changes in libido; hair loss or hirsutism; GI disturbances (nausea and vomiting); genitourinary changes; haematologic disorders; endocrine and metabolic disorders; cholestatic jaundice; local skin reactions; chorea; contact lens intolerance; steeping of corneal curvature; pulmonary thromboembolism; carbohydrate and/or glucose intolerance; depression; chloasma; BP increase, liver impairment; reduced menstrual loss, 'spotting' in early cycles, absence of withdrawal bleeding; rarely photosensitivity; increased risk in breast cancer; elevation of plasma bound iodine, cortisol and thyroid binding, erythrocyte sedimentation may be accelerated; increases in plasma copper, iron and alkaline phosphatase; may affect serum triglyceride and lipoprotein levels; retinal vascular thrombosis.

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.

Symptoms: nausea and vomiting, withdrawal bleeding may occur in females.
Treatment: symptom specific and supportive; emesis and charcoal administration may be used.

Levonorgestrel + Ethinyl Estradiol (0.15 mg+0.03 mg)