Estradiol Valerate/Dienolest- Natazia- @- Hormone (May 2010)
Drug Name:Estradiol Valerate/Dienolest- Natazia- @- Hormone (May 2010)
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Drugs or herbal products that induce certain enzymes (for example CYP3A4)
may decrease the effectiveness of COCs or increase breakthrough bleeding.
Counsel patients to use a back-up or alternative method of contraception
when enzyme inducers are used with COCs.
Indication:
Proprietary Name- Natazia
Established Name - Estradial valerate /Dienogest
Applicant- Bayer Health Care Pharmaceuticals Inc.
Indication-
Indication for prevention of pregnancy
Approved by FDA on 6-5-2010 (Ref- FDA approved List- 2010)
Adverse Reaction:
The most common adverse reactions (2%) in clinical trials for
Natazia are headaches, irregular uterine bleeding, breast tenderness,
nausea/vomiting, acne and increased weight.
Contra-Indications:
CONTRAINDICATIONS
A high risk of arterial or venous thrombotic diseases
Undiagnosed abnormal uterine bleeding
Breast cancer or other estrogen- or progestin-sensitive cancer
Liver tumors or liver disease
Pregnancy
WARNING:
CIGARETTE SMOKING AND SERIOUS CARDIOVASCULAR EVENTS
1 Women over 35 years old who smoke should not use Natazia.
Cigarette smoking increases the risk of serious cardiovascular events
from combination oral contraceptive (COC) use.
PRECAUTIONS
Vascular risks: Stop Natazia if a thrombotic event occurs.
Stop Natazia at least 4 weeks before and through 2 weeks after major surgery.
Start Natazia no earlier than 4 weeks after delivery, in women who are not
breastfeeding
Liver disease: Discontinue Natazia if jaundice occurs.
High blood pressure: Do not prescribe Natazia for women with uncontrolled
hypertension or hypertension with vascular disease.
Carbohydrate and lipid metabolic effects: Monitor prediabetic and diabetic
women taking Natazia. Consider an alternate contraceptive method for
women with uncontrolled dyslipidemia.
Headache: Evaluate significant change in headaches and discontinue
Natazia if indicated.
Uterine bleeding: Evaluate irregular bleeding or amenorrhea.
CYP3A4 induction: Women taking strong CYP3A4 inducers (for
example, carbamazepine, phenytoin, rifampicin, and St. John¡¦s wort)
should not choose Natazia as their oral contraceptive due to the possibility
of decreased contraceptive efficacy.
Dosages/ Overdosage Etc:
Indication-
Indication for prevention of pregnancy
INDICATIONS AND USAGE
Natazia is an estrogen/progestin COC, indicated for use by women to
prevent pregnancy.
The efficacy of Natazia in women with a body mass index (BMI) of >30 kg/m2
has not been evaluated.
DOSAGE AND ADMINISTRATION
Take one tablet daily by mouth at the same time every day.
Tablets must be taken in the order directed on the blister pack.
Do not skip or delay intake by more than 12 hours.
DOSAGE FORMS AND STRENGTHS
Natazia consists of 28 film-coated, unscored tablets in the following order -
1. 2 dark yellow tablets each containing 3 mg estradiol valerate
2.5 medium red tablets each containing 2 mg estradiol valerate and 2 mg
dienogest
3.17 light yellow tablets each containing 2 mg estradiol valerate and 3 mg
dienogest
4. 2 dark red tablets each containing 1 mg estradiol valerate
5. 2 white tablets (inert)
Patient Information:
PATIENT COUNSELING INFORMATION
¨
1.Counsel patients that cigarette smoking increases the risk of serious
cardiovascular events from COC use, and that women who are over 35 years
old and smoke should not use COCs.
2.Counsel patients that the increased risk of VTE compared to non-users of COCs
is greatest after initially starting a COC or restarting (following a 4 week
or greater pill-free interval) the same or a different COC.
3. Counsel patients that Natazia does not protect against HIV infection (AIDS)
and other sexually transmitted diseases.
4.Counsel patients on Warnings and Precautions associated with COCs.
5. Inform patients that Natazia is not indicated during pregnancy.
If pregnancy occurs during treatment with Natazia, instruct the patient
to stop further intake.
6.Counsel patients to take one tablet daily by mouth at the same time every day
in the exact order noted on the blister. Instruct patients what to do in the event
pills are missed.
7. Counsel women who are taking strong CYP3A4 inducers (for example,
carbamazepine, phenytoin, rifampicin, and St. John¡¦s wort) not to choose
Natazia as their oral contraceptive due to the possibility of decreased contraceptive efficacy.
8. Counsel patients to use a back-up or alternative method of contraception
when weak or moderate enzyme inducers are used with Natazia.
9. Counsel patients who are breastfeeding or who desire to breastfeed that
COCs may reduce breast milk production. This is less likely to occur
if breastfeeding is well established.
10. Counsel any patient who starts COCs postpartum, and who has not yet
had a period, to use an additional method of contraception until she has
taken Natazia for 9 consecutive days.
11. Counsel patients that amenorrhea may occur. Rule out pregnancy
in the event of amenorrhea in two or more consecutive cycles.
Pharmacology/ Pharmacokinetics:
1 Mechanism of Action
COCs lower the risk of becoming pregnant primarily by suppressing ovulation.
Other possible mechanisms may include cervical mucus changes that inhibit
sperm penetration and endometrial changes that reduce the likelihood
of implantation.
2 Pharmacodynamics
The estrogen in Natazia is estradiol valerate, a synthetic prodrug of 17ß-estradiol.
The progestin in Natazia is dienogest (DNG). DNG displays properties of
19-nortestosterone derivatives as well as properties associated with
progesterone derivatives.
3 Pharmacokinetics
Absorption
After oral administration of estradiol valerate, cleavage to 17â-estradiol and
valeric acid takes place during absorption by the intestinal mucosa or
in the course of the first liver passage.
This gives rise to estradiol and its metabolites, estrone and other metabolites.
Maximum serum estradiol concentrations of 73.3 pg/mL are reached at a
median of approximately 6 hours (range: 1.5–12 hours) and the area
under the estradiol concentration curve [AUC(0–24hr)] was
1301 pg·hr/mL after single ingestion of a tablet containing 3 mg estradiol
valerate under fasted condition on Day 1 of the 28-day sequential regimen.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1 Pregnancy
There is little or no increased risk of birth defects in women who inadvertently
use COCs during early pregnancy. Epidemiologic studies and meta-analyses
have not found an increased risk of genital or non-genital birth defects
(including cardiac anomalies and limb-reduction defects) following exposure
to low dose COCs prior to conception or during early pregnancy.
The administration of COCs to induce withdrawal bleeding should not be
used as a test for pregnancy. COCs should not be used during pregnancy
to treat threatened or habitual abortion.
Women who do not breastfeed may start COCs no earlier than four weeks postpartum.
2. Nursing Mothers
When possible, advise the nursing mother to use other forms of contraception until
she has weaned her child.
Estrogen-containing COCs can reduce milk production in breastfeeding mothers.
This is less likely to occur once breastfeeding is well-established; however,
it can occur at any time in some women.
Small amounts of oral contraceptive steroids and/or metabolites are present
in breast milk.
3. Pediatric Use
Safety and efficacy of Natazia have been established in women of reproductive age.
Efficacy is expected to be the same for postpubertal adolescents under the age
of 18 and for users 18 years and older.
Use of this product before menarche is not indicated.
4 Geriatric Use
Natazia has not been studied in postmenopausal women and is not indicated
in this population.
