Estellis Tablet
Drospirenone + Estetrol
3 mg + 14.2 mg
Renata PLC.
| Pack size | 28's pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 1500.00 AED |
Indications
Estellis Tablet is used for:
Contraception for the prevention of pregnancy
Adult Dose
Oral
Indicated for use by females of reproductive potential to prevent pregnancy
Days 1-24: 1 active tablet (3 mg drospirenone [DRSP]/14.2 mg estetrol [E4]) PO once a day, THEN
Days 25-28: 1 inert tablet PO once a day
Hepatic impairment
All severities of hepatic impairment: Contraindicated
Moderate: Mean exposure to DRSP was ~3x higher than females with normal liver function
Severe: Not studied
Child Dose
Renal Dose
Renal impairment
All severities of renal impairment: Contraindicated
CrCl 30-49 mL/min: Serum DRSP concentrations were ~37 higher than control group
Females with renal impairment whose serum potassium is in upper reference range and are concomitantly using potassium-sparing drugs may potentially develop hyperkalemia
Administration
Take it at the same time every day
May take with or without food
Contra Indications
History of, increased risk for, or current arterial or venous thrombotic/thromboembolic diseases
Current or history of a hormonally-sensitive malignancy (eg, breast cancer)
Hepatic adenoma, hepatocellular carcinoma, acute hepatitis, or severe (decompensated) cirrhosis
Use of hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir
Abnormal uterine bleeding with undiagnosed etiology
Renal impairment
Adrenal insufficiency
Precautions
• Thromboembolic Disorders and Other Vascular Problems: Stop this if a thrombotic or thromboembolic event occurs. Start no earlier than 4 weeks after delivery. Consider all cardiovascular risk factors before initiating in any female, particularly in the presence of multiple risk factors.
• Hyperkalemia: Check serum potassium concentration during the first treatment cycle in females on long-term treatment with medications that may increase serum potassium concentration.
• Hypertension: Monitor blood pressure periodically and stop use if blood pressure rises significantly.
• Migraine: Discontinue if new, recurrent, persistent, or severe migraines occur.
• Hormonally-Sensitive Malignancy: Discontinue Liana if a hormonally-sensitive malignancy is diagnosed.
• Liver Disease: Withhold or permanently discontinue for the persistent or significant elevation of liver enzymes.
• Glucose Tolerance and Hypertriglyceridemia: Monitor glucose in females with prediabetes or diabetes.
Consider an alternate contraceptive method for females with hypertriglyceridemia.
• Gallbladder Disease and Cholestasis: Consider discontinuing Liana in females with symptomatic gallbladder or cholestatic disease.
• Bleeding Irregularities and Amenorrhea: May cause irregular bleeding or amenorrhea. Evaluate for other causes if symptoms persist.
Pregnancy-Lactation
Pregnancy
Discontinue if pregnancy occurs
Epidemiologic studies and meta-analyses have not found an increased risk of genital or nongenital birth defects (eg, cardiac anomalies, limb-reduction defects) following COC exposure before conception or during early pregnancy
Animal studies
Reproductive toxic studies performed with E4 alone have shown expected pharmacologic effects in animals, which are consistent with estrogen exposure
Lactation
Contraceptive hormones and/or metabolites are present in human milk
COCs can reduce milk production in breastfeeding females; reduction may occur at any time, but less likely to occur once breastfeeding is well established
When possible, advise nursing females to use other methods of contraception until breastfeeding is discontinued
After oral administration of DRSP 3 mg/ethinyl estradiol 30 mcg, about 0.02% of the DRSP dose was excreted into the breast milk of postpartum females within 24 hr; results in a potential maximal daily dose <1 mcg DRSP in an infant
Interactions
CYP3A Inducers: May lead to contraceptive failure and/or increase breakthrough bleeding. Concomitant use must be avoided.
If concomitant use is unavoidable, an alternative or backup contraceptive method during co-administration and up to 28 days after discontinuation of the CYP3A inducer must be used.
Antidiabetic drugs
Increase frequency of glucose monitoring and increase antidiabetic drug dosage, as needed, based on glucose levels
DRSP/E4 may reduce blood glucose–lowering effects of antidiabetic drugs
Drugs that may increase serum potassium concentration
Monitor serum potassium concentration in females at increased risk for hyperkalemia
DRSP/E4 may increase serum potassium concentration in females concurrently taking other drugs that may increase serum potassium
Lamotrigine
Adjust lamotrigine dosage as recommended by prescribing information
DRSP/E4 may decrease exposure and efficacy of lamotrigine
Systemic corticosteroids
Follow recommendations in accordance with prescribing information of corticosteroids consider more frequent monitoring for corticosteroid adverse reactions
DRSP/E4 may increase exposure and toxicities of systemic corticosteroids (owing to increased corticosteroid-binding globulin) and mineralocorticoids (owing to increased aldosterone)
Thyroid hormone replacement therapy
Increase thyroid hormone replacement dose as needed
Estrogen component may increase the serum concentrations of thyroxine-binding globulin
Sex hormones
Coadministration may decrease androstenedione, progesterone, and free testosterone owing to increased sex hormone-binding globulin
Adverse Effects
Side effects of Drospirenone + Estetrol :
>10%
Bleeding irregularities (9.7-10.8%)
Mood disturbance (9.1-10.9%)
1-10%
Headache (4.8-6.3%)
Breast symptoms (5.3-5.4%)
Dysmenorrhea (3.7-4.1%)
Weight increased (3-3.3%)
Acne (3.2-3.7%)
Libido decreased/lost (1.3-2%)
Depression (1.7%)
Frequency Not Defined
Thromboembolic event reported in a female who had been taking therapy for 75 days and had normal BMI < 25 kg/m2
Mechanism of Action
Drospirenone: Progestin; spironolactone analogue with anti-mineralocorticoid and anti-androgenic activity that provides contraception primarily by suppressing ovulation
Estetrol (E4): Synthetic analogue of a native estrogen present during pregnancy, that is selective for nuclear estrogen receptor-alpha (ER-alpha) and ER-beta; treatment results in decrease of follicle-stimulating hormone and luteinizing hormone, ultimately leading to ovulation suppression
Note
Estellis 3 mg + 14.2 mg Tablet manufactured by Renata PLC.. Its generic name is Drospirenone + Estetrol. Estellis is availble in Bangladesh.
Farmaco BD drug index information on Estellis Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.