Norgestrel + Ethinyl Estradiol

Indications

Norgestrel + Ethinyl Estradiol is used for: Contraception

Adult Dose

Oral Contraception Adult The dosage of norgestrel and ethinyl estradiol tablets is one white tablet daily for 21 consecutive days, followed by one inert tablet daily for 7 consecutive days, according to the prescribed schedule. It is recommended that this tablets should be taken at the same time each day. If >2 tablets are missed or in newly started patients, non-hormonal birth control method should be used until the active tablet has been taken consecutively for 7 days. Hepatic Impairment Do not administer

Child Dose

Renal Dose

Renal Impairment Use caution; monitor blood pressure

Administration

Contra Indications

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.

Precautions

Sex-steroid dependent cancer; past ectopic pregnancy; malabsorption syndromes; functional ovarian cysts; active liver disease, recurrent cholestatic jaundice, history of jaundice in pregnancy; history of CV or renal impairment; DM; asthma; epilepsy; migraine; depression; lactation; conditions exacerbated by fluid retention; hypercalcaemia; CV and gall bladder diseases; lipid effects; familial defects of lipoprotein metabolism; patients at risk of venous thromboembolism, breast cancer, preexisting uterine leiomyomata and benign hepatic adenoma; family history of arterial disease in 1st degree relative <45 yr; BP > systolic 140 mmHg and diastolic 90 mmHg; >35 yr; BMI 30-39 kg/m2; migraine without focal aura, controlled with 5HT1; GI upset (vomiting and diarrhoea), missed pills and interaction with other drugs may require additional contraceptive precautions. Should be taken at same time each day.

Pregnancy-Lactation

Interactions

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.

Adverse Effects

Side effects of Norgestrel + Ethinyl Estradiol : 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. Potentially Fatal: Hepatic tumours; increased risk of thromboembolism.

Mechanism of Action

Ethinylestradiol (EE): Reduces LHRH release from hypothalamus, reduces gonadotropin release from pituitary; increase synthesis of DNA, RNA, and various proteins in target tissues. Norgestrel: Progestin; inhibits gonadotropin secretion from pituitary; prevents follicular maturation and ovulation, stimulates growth of mammary tissues. Norgestrel is a progestogen derived from nortestosterone while ethinylestradiol is a synthetic oestrogen. When used together, they inhibit ovulation, and affect other changes such as changes in the cervical mucus and the endometrium, which makes conception unfavourable.