Jastinda coated tablets 2 mg/0.03 mg. №63

Description

Jastinda Composition
active ingredients: dienogest; ethinyl estradiol;

1 coated tablet contains ethinylestradiol 0.03 mg and dienogest 2 mg;

excipients: lactose monohydrate, corn povidone starch, magnesium stearate, talc;

tablet shell: Opaglos 2 purified containing: sodium carboxymethyl cellulose, maltodextrin, dextrose monohydrate, lecithin soy, sodium dihydrate.

Jastinda Dosage form
Film-coated tablets.

Basic physical and chemical properties: white or almost white, round biconvex, film-coated tablets free from foreign contamination.

Jastinda Pharmacotherapeutic group
Hormonal contraceptives for systemic use. ATX code G03A A16.

Pharmacodynamics
All hormonal methods of contraception have very low contraceptive failure rates when used as directed. Contraceptive failure rates may be higher if used as directed (eg, skipping a pill).

In the course of clinical studies, the following Pearl index was calculated:

unadjusted Pearl index: 0.454 (upper 95% confidence interval (CI): 0.701)
adjusted Pearl index: 0.182 (upper 95% confidence interval: 0.358).
Justinda is a combined oral contraceptive (COC) with ethinyl estradiol and the progestogen dienogest.

The contraceptive effect of the drug Justinda is based on the interaction of various factors, the most important of which are suppression of ovulation and changes in cervical secretion.

Dienogest is a derivative of nortestosterone with in vitro affinity for progesterone receptors 10-30 times less than other synthetic progestogens. In vivo data in animals indicate strong progestogenic activity and antiandrogenic activity. Dienogest does not exhibit significant androgenic, mineralocorticoid, or glucocorticoid activity in vivo.

The dose of dienogest, which leads to the suppression of ovulation, is 1 mg / day.

When used in high COCs (50 μg ethinyl estradiol), the risk of endometrial and ovarian cancer is reduced. Whether this concerns low COCs remains unclear.

Pharmacokinetics
Ethinylestradiol

Adsorption. When taken orally, ethinyl estradiol is rapidly and completely absorbed. The maximum serum concentration is approximately 67 pg / ml and is reached within 1.5-4 hours. During absorption and first passage through the liver, ethinyl estradiol is extensively metabolized, resulting in an average oral bioavailability of approximately 44%.

Distribution. Ethinylestradiol strongly, but nonspecifically, binds to albumin (98%) and causes an increase in serum concentrations of sex hormone binding globulin (SHBG). The volume of distribution of ethinylestradiol is approximately 2.8-8.6 l / kg.

Metabolism. Ethinylestradiol undergoes presystemic conjugation in the mucous membrane of the small intestine and in the liver. Ethinylestradiol is metabolized mainly by aromatic hydroxylation, however, a large number of hydroxylated and methylated metabolites are additionally formed, among which there are both free metabolites and conjugates with glucuronides and sulfates. The clearance is 2.3-7 ml / min / kg.