A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Estrostep Side Effects, and Drug Interactions - Norethindrone Acetate and Ethinyl Estradiol
Estrostep Side Effects, and Drug Interactions - Norethindrone Acetate and Ethinyl Estradiol
SIDE EFFECTS
An increased risk of the following serious adverse reactions
has been associated with the use of oral contraceptives (see WARNINGS
section):
· Thrombophlebitis
· Arterial thromboembolism
· Pulmonary embolism
· Myocardial infarction
· Cerebral hemorrhage
· Cerebral thrombosis
· Hypertension
· Gallbladder disease
· Hepatic adenomas or benign liver tumors
There is evidence of an association between the following conditions
and the use of oral contraceptives, although additional confirmatory studies
are needed:
· Mesenteric thrombosis
· Retinal thrombosis
The following adverse reactions have been reported in patients
receiving oral contraceptives and are believed to be drug-related:
· Nausea
· Vomiting
· Gastrointestinal symptoms (such as abdominal
cramps and bloating)
· Breakthrough bleeding
· Spotting
· Change in menstrual flow
· Amenorrhea
· Temporary infertility after discontinuation
of treatment
· Edema
· Melasma which may persist
· Breast changes: tenderness, enlargement,
secretion
· Change in weight (increase or decrease)
· Change in cervical erosion and secretion
· Diminution in lactation when given immediately
postpartum
· Cholestatic jaundice
· Migraine
· Rash (allergic)
· Mental depression
· Reduced tolerance to carbohydrates
· Vaginal candidiasis
· Change in corneal curvature (steepening)
· Intolerance to contact lenses
The following adverse reactions have been reported in users
of oral contraceptives and the association has been neither confirmed nor refuted:
· Pre-menstrual syndrome
· Cataracts
· Changes in appetite
· Cystitis-like syndrome
· Headache
· Nervousness
· Dizziness
· Hirsutism
· Loss of scalp hair
· Erythema multiforme
· Erythema nodosum
· Hemorrhagic eruption
· Vaginitis
· Porphyria
· Impaired renal function
· Hemolytic uremic syndrome
· Budd-Chiari syndrome
· Acne
· Changes in libido
· Colitis
8. DRUG INTERACTIONS
Effects of Other Drugs on Oral Contraceptives
Rifampin: Metabolism of both norethindrone and ethinyl
estradiol is increased by rifampin. A reduction in contraceptive effectiveness
and increased incidence of breakthrough bleeding and menstrual irregularities
have been associated with concomitant use of rifampin.
Anticonvulsants: Anticonvulsants such as phenobarbital,
phenytoin, and carbamazepine, have been shown to increase the metabolism of
ethinyl estradiol and/or norethindrone, which could result in a reduction in
contraceptive effectiveness.
Antibiotics: Pregnancy while taking oral contraceptives
has been reported when the oral contraceptives were administered with antimicrobials
such as ampicillin, tetracycline, and griseofulvin. However, clinical pharmacokinetic
studies have not demonstrated any consistent effect of antibiotics (other than
rifampin) on plasma concentrations of synthetic steroids.
Atorvastatin: Coadministration of atorvastatin and an
oral contraceptive increased AUC values for norethindrone and ethinyl estradiol
by approximately 30% and 20%, respectively.
St. John’s Wort: Herbal products containing St. John’s
Wort (hypericum perforatum) may induce hepatic enzymes (cytochrome P450) and
p-glycoprotein transporter and may reduce the effectiveness of oral contraceptives.
This may also result in breakthrough bleeding.
Other: Ascorbic acid and acetaminophen may increase
plasma ethinyl estradiol concentrations, possibly by inhibition of conjugation.
A reduction in contraceptive effectiveness and increased incidence of breakthrough
bleeding has been suggested with phenylbutazone.
Effects of Oral Contraceptives on Other Drugs
Oral contraceptive combinations containing ethinyl estradiol
may inhibit the metabolism of other compounds. Increased plasma concentrations
of cyclosporine, prednisolone, and theophylline have been reported with concomitant
administration of oral contraceptives. In addition, oral contraceptives may
induce the conjugation of other compounds.
Decreased plasma concentrations of acetaminophen and increased
clearance of temazepam, salicylic acid, morphine, and clofibric acid have been
noted when these drugs were administered with oral contraceptives.
9. Interactions with Laboratory Tests
Certain endocrine and liver function tests and blood components
may be affected by oral contraceptives:
a. ncreased prothrombin and factors VII, VIII, IX,
and X; decreased antithrombin 3; increased norepinephrine-induced platelet
aggregability.
b. ncreased thyroid binding globulin (TBG) leading
to increased circulating total hyroid hormone, as measured by protein-bound
iodine (PBI), T4 by column or by radioimmunoassay. Free T3
resin uptake is decreased, reflecting the elevated TBG; free T4
concentration is unaltered.
c. ther binding proteins may be elevated in serum.
d. ex-binding globulins are increased and result in elevated levels
of total circulating sex steroids and corticoids; however, free or biologically
active levels remain unchanged.
e. riglycerides may be increased.
f. lucose tolerance may be decreased.
g. erum folate levels may be depressed by oral contraceptive
therapy. This may be of clinical significance if a woman becomes pregnant
shortly after discontinuing oral contraceptives.
10. Carcinogenesis
See WARNINGS section.
11. Pregnancy
Pregnancy Category X. See CONTRAINDICATIONS
and WARNINGS sections.
12. Nursing Mothers
Small amounts of oral contraceptive steroids have been identified
in the milk of nursing mothers, and a few adverse effects on the child have
been reported, including jaundice and breast enlargement. In addition, oral
contraceptives given in the postpartum period may interfere with lactation by
decreasing the quantity and quality of breast milk. If possible, the nursing
mother should be advised not to use oral contraceptives but to use other forms
of contraception until she has completely weaned her child.
13. Pediatric Use
Safety and efficacy of ESTROSTEP have been established in women
of reproductive age. Safety and efficacy are expected to be the same for postpubertal
adolescents under the age of 16 and for users 16 years and older. Use of this
product before menarche is not indicated.
14. Geriatric Use
This product has not been studied in women over 65 years of
age and is not indicated in this population.
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