Estradiol Norgestimate Brand Name– Prefest
What is Estradiol Norgestimate
Estradiol and norgestimate are used together in oral combination products.
Estradiol is the principal intracellular human estrogen and is substantially more active than its metabolites, estrone and estriol, at the cellular level.
Norgestimate is a derivative of 19-nortestosterone and binds to androgen and progestogen receptors, similar to that of the natural hormone progesterone; it does not bind to estrogen receptors.
The combination products are primarily used together in women with an intact uterus to treat moderate to severe vasomotor and genitourinary symptoms associated with menopause and for the prevention of osteoporosis.
The addition of a progestin to the estrogen replacement therapy (HRT) substantially reduces, but does not eliminate, the risk for endometrial hyperplasia.
However, combination HRT may add additional health risks for some women, and hormone replacement regimens are recommended to be used for the shortest duration consistent with the treatment goals of the individual patient.
The combination of estradiol norgestimate was granted FDA approval in October 1999.
Indications
- atrophic vaginitis
- hot flashes
- menopause
- osteoporosis prophylaxis
For treatment of moderate to severe vasomotor symptoms (hot flashes) of menopause and/or related genitourinary symptoms including atrophic vaginitis, vulvar atrophy (kraurosis vulvae) in women with an intact uterus
Side Effects
- abdominal pain
- acne vulgaris
- alopecia
- amenorrhea
- anaphylactoid reactions
- angioedema
- anxiety
- arthralgia
- back pain
- biliary obstruction
- bowel ischemia
- breakthrough bleeding
- breast cancer
- breast discharge
- breast enlargement
- candidiasis
- cervicitis
- cholecystitis
- cholelithiasis
- cholestasis
- colitis
- dementia
- depression
- diplopia
- dizziness
- dysmenorrhea
- edema
- elevated hepatic enzymes
- emotional lability
- endometrial cancer
- endometrial hyperplasia
- erythema multiforme
- erythema nodosum
- fatigue
- flatulence
- fluid retention
- galactorrhea
- headache
- hepatitis
- hirsutism
- hypercalcemia
- hyperglycemia
- hypertension
- hypocalcemia
- impaired cognition
- infection
- insomnia
- irritability
- jaundice
- libido decrease
- libido increase
- mastalgia
- melasma
- menorrhagia
- migraine
- muscle cramps
- myalgia
- myocardial infarction
- nausea
- new primary malignancy
- ovarian cancer
- pancreatitis
- papilledema
- peliosis hepatis
- peripheral edema
- pruritus
- pulmonary embolism
- rash
- retinal thrombosis
- stroke
- teratogenesis
- thromboembolism
- thrombosis
- urinary incontinence
- urticaria
- vaginal bleeding
- vaginitis
- visual impairment
- weight gain
Monitoring Parameters
- pap smear
- pelvic exam
Contraindications
- asthma
- breast cancer
- breast-feeding
- cardiac disease
- cerebrovascular disease
- cervical cancer
- children
- contact lenses
- coronary artery disease
- dementia
- depression
- diabetes mellitus
- endometrial cancer
- endometrial hyperplasia
- endometriosis
- gallbladder disease
- geriatric
- hepatic disease
- hepatocellular cancer
- hereditary angioedema
- history of angioedema
- hypercalcemia
- hypercholesterolemia
- hypertension
- hypertriglyceridemia
- hypocalcemia
- hypoparathyroidism
- hypothyroidism
- infants
- jaundice
- migraine
- myocardial infarction
- new primary malignancy
- obesity
- ovarian cancer
- pancreatitis
- porphyria
- pregnancy
- protein C deficiency
- protein S deficiency
- renal disease
- seizure disorder
- stroke
- surgery
- systemic lupus erythematosus (SLE)
- thromboembolic disease
- thromboembolism
- thrombophlebitis
- thyroid disease
- tobacco smoking
- uterine cancer
- uterine leiomyomata
- vaginal bleeding
- vaginal cancer
- visual disturbance
Interactions
- Acarbose
- Acetaminophen; Butalbital
- Acetaminophen; Butalbital; Caffeine
- Acetaminophen; Butalbital; Caffeine; Codeine
- Acetaminophen; Propoxyphene
- Acetohexamide
- Albiglutide
- Alogliptin
- Alogliptin; Metformin
- Alogliptin; Pioglitazone
- Alpha-glucosidase Inhibitors
- Amikacin
- Aminoglycosides
- Amiodarone
- Amobarbital
- Amoxicillin
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Amoxicillin; Clavulanic Acid
- Ampicillin
- Ampicillin; Sulbactam
- Amprenavir
- Anastrozole
- Apalutamide
- Aprepitant, Fosaprepitant
- Armodafinil
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Atazanavir
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Azelastine; Fluticasone
- Azithromycin
- Aztreonam
- Bacitracin
- Barbiturates
- Beclomethasone
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Betamethasone
- Bexarotene
- Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
- Bismuth Subsalicylate; Metronidazole; Tetracycline
- Boceprevir
- Bosentan
- Bromocriptine
- Budesonide
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- Butabarbital
- Calaspargase pegol
- Calcium
- Canagliflozin
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- Ceftibuten
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- Cephalexin
- Charcoal
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- Daptomycin
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- Elvitegravir
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- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Empagliflozin
- Empagliflozin; Linagliptin
- Empagliflozin; Linagliptin; Metformin
- Empagliflozin; Metformin
- Enasidenib
- Encorafenib
- Enzalutamide
- Eravacycline
- Ertapenem
- Ertugliflozin
- Ertugliflozin; Metformin
- Ertugliflozin; Sitagliptin
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- Eslicarbazepine
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- Gentamicin
- Glimepiride
- Glimepiride; Pioglitazone
- Glimepiride; Rosiglitazone
- Glipizide
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- Glyburide
- Glyburide; Metformin
- Glycylcyclines
- grapefruit juice
- Griseofulvin
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- Hyaluronidase
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- Hydralazine
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- Levothyroxine; Liothyronine (Porcine)
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- Linagliptin
- Linagliptin; Metformin
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- Meropenem; Vaborbactam
- Metformin
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- Metformin; Repaglinide
- Metformin; Rosiglitazone
- Metformin; Saxagliptin
- Metformin; Sitagliptin
- Methohexital
- Methylprednisolone
- Metreleptin
- Metronidazole
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- Mineral Oil
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- Norfloxacin
- Ofloxacin
- Omadacycline
- Ombitasvir; Paritaprevir; Ritonavir
- Omeprazole; Amoxicillin; Rifabutin
- Oritavancin
- Ospemifene
- Oxacillin
- Oxcarbazepine
- Paromomycin
- Pegaspargase
- Penicillin G
- Penicillin G Benzathine
- Penicillin G Benzathine; Penicillin G Procaine
- Penicillin G Procaine
- Penicillin V
- Pentobarbital
- Pexidartinib
- Phenobarbital
- Phentermine; Topiramate
- Phenytoin
- Piperacillin
- Piperacillin; Tazobactam
- Pitolisant
- Plazomicin
- Polymyxin B
- Polymyxins
- Posaconazole
- Pramlintide
- Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
- Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
- Prednisolone
- Prednisone
- Primidone
- Propoxyphene
- Pyrimethamine; Sulfadoxine
- Raloxifene
- Ribociclib; Letrozole
- Rifamycins
- Riluzole
- Ritonavir
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- Roflumilast
- Ropinirole
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- Saquinavir
- Sarilumab
- Saxagliptin
- Secobarbital
- Semaglutide
- SGLT2 Inhibitors
- Siltuximab
- Simvastatin; Sitagliptin
- Sitagliptin
- Somatropin, rh-GH
- St. John’s Wort, Hypericum perforatum
- Streptogramins
- Streptomycin
- Succinylcholine
- Sugammadex
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- Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
- Sulfasalazine
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- Sulfonylureas
- Tacrine
- Tazemetostat
- Tedizolid
- Telavancin
- Telithromycin
- Tenofovir Alafenamide
- Teriflunomide
- Testolactone
- Tetracycline
- Thalidomide
- Thiazolidinediones
- Thiopental
- Thyroid hormones
- Ticarcillin
- Ticarcillin; Clavulanic Acid
- Tigecycline
- Tinidazole
- Tipranavir
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- Tocilizumab
- Tolazamide
- Tolbutamide
- Topiramate
- Toremifene
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- Trastuzumab; Hyaluronidase
- Triamcinolone
- Tricyclic antidepressants
- Trimethoprim
- Ulipristal
- Ursodeoxycholic Acid, Ursodiol
- Vancomycin
- Verapamil
- Voriconazole
- Warfarin
- Zafirlukast
