Novestrol

Novestrol - General Information

A semisynthetic alkylated estradiol with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in oral contraceptives. [PubChem]

Pharmacology of Novestrol

Ethinyl estradiol is a synthetic derivative of the natural estrogen estradiol. It is one of two estrogens currently used in oral contraceptive pills. The other, mestranol, is converted to ethinyl estradiol before it is biologically active. Ethinyl estradiol and norethindrone are used together as an oral contraceptive agent.

Novestrol for patients

PATIENT PACKAGE INSERT

Vaginal Cream, Oral Tablets, and Transdermal System

This information describes when and how to use estrogens, and the risks and benefits of estrogen treatment.

Estrogens have important benefits but also some risks. You must decide, with your doctor, whether the risks to you of estrogen use are acceptable because of their benefits. If you use estrogens, check with your doctor to be sure you are using the lowest possible dose that works, and that you don't use them longer than necessary. How long you need to use estrogens will depend on the reason for use.

Additional Information for the Climara System: The Climara system that your doctor has prescribed for you releases small amounts of estradiol through the skin in a continuous way. Estradiol is the same hormone that your ovaries produce abundantly before menopause. The dose of estradiol you require will depend upon your individual response. The dose is adjusted by the size of the Climara system used: the systems are avaialble in 4 sizes.

Novestrol Interactions

Certain endocrine and liver function tests may be affected by estrogen-containing oral contraceptives. The following similar changes may be expected with larger doses of estrogen:

Increased sulfobromophthalein retention; increased prothrombin and factors VII, VIII, IX, and X; decreased antithrombin 3; increased norepinephrine-induced platel et aggregation; increased thyroid binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by PBI, T₄ by column, or T₄ by radioimmunoassay. Free T₃ resin uptake is decreased, reflecting the elevated TBG; free T₄ concentration is unaltered: impaired glucose tolerance; decreased pregnanediol excretion; reduced response to metyrapone test; reduced serum folate concentration; increased serum triglyceride and phospholipid concentration.

Novestrol Contraindications

Estrogens should not be used in women (or men) with any of the following conditions:

1. Known or suspected cancer of the breast except in appropriately selected patients being treated for metastatic disease.

2. Known or suspected estrogen-dependent neoplasia.

3. Known or suspected pregnancy.

4. Undiagnosed abnormal genital bleeding.

5. Active thrombophlebitis or thromboembolic disorders.

6. A past history of thrombophlebitis, thrombosis, or thromboembolic disorders associated with previous estrogen use (except when used in treatment of breast or prostatic malignancy).

Additional information about Novestrol

Novestrol Indication: For treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.
Mechanism Of Action: Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).
Drug Interactions: Aminophylline The contraceptive increases the effect and toxicity of theophylline
Dyphylline The contraceptive increases the effect and toxicity of theophylline
Oxtriphylline The contraceptive increases the effect and toxicity of theophylline
Theophylline The contraceptive increases the effect and toxicity of theophylline
Amobarbital This product may cause a slight decrease of contraceptive effect
Aprobarbital This product may cause a slight decrease of contraceptive effect
Butabarbital This product may cause a slight decrease of contraceptive effect
Butalbital This product may cause a slight decrease of contraceptive effect
Butethal This product may cause a slight decrease of contraceptive effect
Carbamazepine This product may cause a slight decrease of contraceptive effect
Ethotoin This product may cause a slight decrease of contraceptive effect
Fosphenytoin This product may cause a slight decrease of contraceptive effect
Griseofulvin This product may cause a slight decrease of contraceptive effect
Heptabarbital This product may cause a slight decrease of contraceptive effect
Hexobarbital This product may cause a slight decrease of contraceptive effect
Mephenytoin This product may cause a slight decrease of contraceptive effect
Methohexital This product may cause a slight decrease of contraceptive effect
Methylphenobarbital This product may cause a slight decrease of contraceptive effect
Pentobarbital This product may cause a slight decrease of contraceptive effect
Phenobarbital This product may cause a slight decrease of contraceptive effect
Phenytoin This product may cause a slight decrease of contraceptive effect
Primidone This product may cause a slight decrease of contraceptive effect
Rifabutin This product may cause a slight decrease of contraceptive effect
Rifampin This product may cause a slight decrease of contraceptive effect
Rifapentine This product may cause a slight decrease of contraceptive effect
Secobarbital This product may cause a slight decrease of contraceptive effect
Talbutal This product may cause a slight decrease of contraceptive effect
Amoxicillin This anti-infectious agent could decrease the effect of the oral contraceptive
Ampicillin This anti-infectious agent could decrease the effect of the oral contraceptive
Azlocillin This anti-infectious agent could decrease the effect of the oral contraceptive
Aztreonam This anti-infectious agent could decrease the effect of the oral contraceptive
Bacampicillin This anti-infectious agent could decrease the effect of the oral contraceptive
Carbenicillin This anti-infectious agent could decrease the effect of the oral contraceptive
Clavulanate This anti-infectious agent could decrease the effect of the oral contraceptive
Cloxacillin This anti-infectious agent could decrease the effect of the oral contraceptive
Cyclacillin This anti-infectious agent could decrease the effect of the oral contraceptive
Demeclocycline This anti-infectious agent could decrease the effect of the oral contraceptive
Dicloxacillin This anti-infectious agent could decrease the effect of the oral contraceptive
Doxycycline This anti-infectious agent could decrease the effect of the oral contraceptive
Flucloxacillin This anti-infectious agent could decrease the effect of the oral contraceptive
Hetacillin This anti-infectious agent could decrease the effect of the oral contraceptive
Penicillin G This anti-infectious agent could decrease the effect of the oral contraceptive
Penicillin V This anti-infectious agent could decrease the effect of the oral contraceptive
Oxytetracycline This anti-infectious agent could decrease the effect of the oral contraceptive
Oxacillin This anti-infectious agent could decrease the effect of the oral contraceptive
Nafcillin This anti-infectious agent could decrease the effect of the oral contraceptive
Minocycline This anti-infectious agent could decrease the effect of the oral contraceptive
Mezlocillin This anti-infectious agent could decrease the effect of the oral contraceptive
Meticillin This anti-infectious agent could decrease the effect of the oral contraceptive
Methacycline This anti-infectious agent could decrease the effect of the oral contraceptive
Itraconazole This anti-infectious agent could decrease the effect of the oral contraceptive
Ketoconazole This anti-infectious agent could decrease the effect of the oral contraceptive
Piperacillin This anti-infectious agent could decrease the effect of the oral contraceptive
Pivampicillin This anti-infectious agent could decrease the effect of the oral contraceptive
Rolitetracycline This anti-infectious agent could decrease the effect of the oral contraceptive
Tazobactam This anti-infectious agent could decrease the effect of the oral contraceptive
Tetracycline This anti-infectious agent could decrease the effect of the oral contraceptive
Ticarcillin This anti-infectious agent could decrease the effect of the oral contraceptive
Amprenavir Ritonavir could decrease the contraceptive efficacy
Nelfinavir Ritonavir could decrease the contraceptive efficacy
Ritonavir Ritonavir could decrease the contraceptive efficacy
Anisindione Increased thrombotic risk due to estrogen
Dicumarol Increased thrombotic risk due to estrogen
Acenocoumarol Increased thrombotic risk due to estrogen
Warfarin Increased thrombotic risk due to estrogen
Aprepitant Aprepitant could decrease the effect of the oral contraceptive
Bosentan Bosentan decreases the effect of contraceptive
Cyclosporine The contraceptive increases the effect and toxicity of cyclosporine
Etoricoxib Etoricoxib increases the levels of ethinyl estradiol
Lamotrigine The oral contraceptive decreases the effect of lamotrigine
Modafinil Modafinil decreases the effect of contraceptive
Oxcarbazepine Oxcarbazepine decreases the effect of the contracepitve
Pioglitazone Possible loss of contracepitve effect
Troglitazone Possible loss of contracepitve effect
Prednisolone The estrogenic agent increases the effect of corticosteroid
Prednisone The estrogenic agent increases the effect of corticosteroid
Raloxifene Association not recommended
St. John's Wort St. John's Wort could reduce the contraceptive effect
Tizanidine The contraceptive increases the effect of tizanidine
Topiramate Topiramate decreases the effect of estrogen
Ursodeoxycholic acid Estrogens decreases the effect of ursodiol
Food Interactions: Not Available
Generic Name: Ethinyl Estradiol
Synonyms: Ethinylestradiolum [Inn-Latin]; Ethinyl-Oestranol; Ethinylestriol; Ethinyloestradiol; Ethynylestradiol; Ethynyloestradiol; Etinilestradiol [Inn-Spanish]; EE; EO; Aethinyoestradiol [German]; 17 alpha-Ethinylestradiol; Aethinyloestradiolum; 17 alpha-Ethynyloestradiol; 17 alpha-Ethynylestradiol
Drug Category: Estrogens
Drug Type: Small Molecule; Approved

Other Brand Names containing Ethinyl Estradiol: Amenoron; Amenorone; Anovlar; Cyclosa; Dicromil; Diognat-E; Diogyn E; Diogyn-E; Diprol; Dyloform; Ertonyl; Esteed; Estigyn; Eston-E; Estopherol; Estoral; Estorals; Ethidol; Ethinoral; Ethy 11; Eticyclin; Eticyclol; Eticylol; Etinestrol; Etinestryl; Etinoestryl; Etistradiol; Etivex; Follicoral; Ginestrene; Gynolett; Halodrin; Inestra; Kolpolyn; Linoral; Marvelon; Menolyn; Mercilon; Microfollin; Neo-Estrone; Nogest-S; Novestrol; Oradiol; Orestralyn; Orestrayln; Ortho-Cyclen; Oviol; Primogyn; Primogyn C; Primogyn M; Progynon C; Progynon M; Prosexol; Spanestrin; Varnoline; Ylestrol;
Absorption: Rapid and complete absorption follows oral intake of ethinyl estradiol (bioavailability 43%).
Toxicity (Overdose): Oral, mouse LD₅₀: 1737 mg/kg. Symptoms of overdose include nausea and vomiting, and withdrawal bleeding may occur in females.
Protein Binding: 97%
Biotransformation: Hepatic. Quantitatively, the major metabolic pathway for ethinyl estradiol, both in rats and in humans, is aromatic hydroxylation, as it is for the natural estrogens.
Half Life: 36 +/- 13 hours
Dosage Forms of Novestrol: Tablet Oral
Insert, extended release Transdermal
Cream Intravaginal
Chemical IUPAC Name: (8R,9S,13S,14S,17R)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17-diol
Chemical Formula: C20H24O2
Ethinyl Estradiol on Wikipedia: https://en.wikipedia.org/wiki/Ethinylestradiol
Organisms Affected: Humans and other mammals