Norgestrel + Ethinylestradiol


Concise Prescribing Info
Indications/Uses
OC.
Dosage/Direction for Use
Adult : PO Per tab contains norgestrel 0.3 mg and ethinylestradiol 0.03 mg: Start on day 1 of the menstrual cycle, 1 tab once daily for 21 days, then stop for 7 days or take the placebo tablet for 7 days. Breakthrough bleeding should occur w/in 3 days following discontinuation. Start 2nd cycle on the 8th day regardless whether menstruation has occurred or still in progress.
Dosage Details
Oral
Oral contraception
Adult: As combination containing 0.3 mg norgestrel and 0.03 mg ethinyl estradiol per tablet: Starting on day 1 of the menstrual cycle, take 1 tablet daily at the same time for 21 days, then stop for 7 days or take the placebo tablet for 7 days. Breakthrough bleeding should occur within 3 days following discontinuation. Start the 2nd cycle on the 8th day regardless whether the menstruation has occurred or still in progress. 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.
Contraindications
Present or history of thromboembolic disorders, cerebral-vascular or coronary-artery disease; thrombogenic valvulopathies or rhythm disorders; surgery with prolonged immobilisation; diabetes with vascular involvement; headaches with focal neurological symptoms; uncontrolled hypertension; breast or endometrium cancer or other oestrogen dependent tumours; liver cancers or active liver disease; undiagnosed abnormal genital bleeding; jaundice or history of cholestatic jaundice of pregnancy. Pregnancy.
Special Precautions
Hypertension, hypercholesterolaemia, obesity, DM, surgery or trauma with thrombotic risk, conditions which may be worsened by fluid retention, renal disease, impaired liver function. History of depression. May worsen gallbladder disease. Increased risk of severe CV side effects with smoking. Discontinue if there is unexplained partial or loss of vision, significant increase in BP or persistent or severe headache. Lactation.
Adverse Reactions
GI disturbances, breakthrough bleeding (especially in 1st 3 mth of use), hypercholesterolaemia, hypertension, headache, oedema, mood changes, melasma.
Potentially Fatal: Increased risk of MI, venous thromboembolic and thrombotic disease, cerebrovascular events, vascular disease, ocular lesions (e.g. retinal thrombosis), breast, cervical and liver cancer.
Drug Interactions
Reduced contraceptive effectiveness with antibiotics, anticonvulsants and drugs that may increase contraceptive steroids clearance (e.g. bosentan, rifampicin, rifabutin, barbiturates, primidone, phenytoin, carbamazepine, oxcarbazepine, topiramate, griseofulvin, aprepitant). Severe pruritus and jaundice with troleandomycin, avoid concurrent use. Decreased effectiveness of ursodeoxycholic acid by increasing the elimination of cholesterol in bile. Effects of danazol or gestrinone and hormonal contraceptives might be altered or reduced by concurrent use, avoid concomittant use. Decreased contraceptive effectiveness with anti-HIV protease inhibitors. Increased tacrolimus levels with ethinyl estradiol. May increase theophylline, selegiline and tizanidine levels with oral contraceptives.
Food Interaction
Reduced contraceptive effectiveness with St. John's wort.
Lab Interference
Decreased response to the metyrapone test; false-positive results in the nitro blue tetrazolium (NBT) test; some endocrine and LFTs may be affected. Inform the pathologist when specimens of oral contraceptive users are submitted.
Action
Description: 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.
Pharmacokinetics:
Absorption: Ethinyl estradiol: Well absorbed from GI tract. Systemic bioavailability: 40%.
Distribution: Ethinyl estradiol: Highly protein bound to albumin.
Metabolism: Norgestrel: Metabolised in liver to sulfate and glucuronide conjugates. Ethinyl estradiol: Undergoes initial conjugation by the gut wall and then metabolised by the liver.
Excretion: Norgestrel: Excreted in urine and to lesser extent in faeces. Ethinyl estradiol: Excreted in urine and faeces; metabolites undergo enterohepatic recycling.
Storage
Store between 20-25°C (68-77°F).
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Norgestrel + Ethinylestradiol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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