Desogestrel - instructions for use, dose, side effects, contraindications

Modulates the effects of estrogens: switching off hormone-sensitive genes, reducing the stability of the hormone-receptor complex due to direct interaction with the nuclear receptors of progesterone. Estrogens increase the number of progesterone receptors, increase the production of progesterone, which triggers a negative feedback mechanism for inhibiting the estrogen receptor. As a result, the epithelium of the endometrium passes from the proliferative phase to the secretory phase, and there is no attachment of the fertilized egg. It suppresses ovulation, increases the viscosity of the secretion of the cervix, reduces the level of estradiol to values that are characteristic of the early follicular phase.

Pharmacokinetics:

Fast and complete absorption, bioavailability - 70%, almost completely binds to plasma proteins. Rapidly metabolized in the intestinal wall and in the liver with the formation of an active metabolite (ethonogestrel). Half-life is 30 hours. Eliminated by the kidneys and through the gastrointestinal tract.

Indications:

Contraception.

ICD-10

XXI.Z30-Z39.Z30.0 General advice and advice on contraception

Contraindications:

- Hypersensitivity;

- Hormone-dependent tumors;

- Tumors of the mammary glands;

- Pregnancy;

- Thrombophlebitis or thromboembolism;

- Undiagnosed uterine or genital bleeding;

- Acute liver diseases, including malignant tumors, congenital hyperbilirubinemia and jaundice;

- Rvenous thromboembolism;

- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

Conditions that increase the risk of venous or arterial thrombosis or thromboembolism. Uncontrolled arterial hypertension, which develops on the background of taking the drug, porphyria, systemic lupus erythematosus, chloasma, diabetes mellitus (due to the possible effect of progestogens on peripheral insulin resistance and glucose tolerance), herpes during an earlier pregnancy, benign or malignant liver tumors.

Pregnancy and lactation:

Category FDA - X.

Progestins penetrate the placental barrier. In some studies, the possibility of genital anomalies in fetuses with the use of progestins in the first trimester of pregnancy was suggested, but their data are contradictory. When using contraceptives based on only progestins, it is possible to develop an ectopic pregnancy. Contraindicated in pregnancy.

Progestins excreted in breast milk. When using contraceptives containing only progestins, the effect on milk quality and quantity has not been fixed since the fifth day after delivery or lactation. If contraception is necessary for lactating women, it is recommended to use preparations containing only progestins. The drug can be used during breastfeeding. Nevertheless, it is necessary to carefully monitor the development and growth of the child during breastfeeding.

Dosing and Administration:

Orally, with a small amount of liquid, the average dose is 75 μg per day once for 28 days. The maximum dose is 150 mcg.

Side effects:

From the nervous system and sensory organs: mood change; rarely - headache, fatigue.

On the part of organs GIT: nausea; rarely vomiting.

From the genitourinary system: irregular spotting; rarely - amenorrhea, decreased libido; very rarely - vaginitis, dysmenorrhea, ovarian cysts.

From the endocrine system: morbidity of the mammary glands, weight gain, acne, alopecia.

Allergic reactions: in isolated cases - a rash, hives, erythema nodosum.

From the side of the circulatory system: thromboembolism, thrombosis, increased tendency to thrombosis, risk of thromboembolism.

Other: discomfort when using contact lenses.

Overdose:

Nausea, minor bleeding from the vagina, vomiting. Treatment is symptomatic.

Interaction:

With the simultaneous use of inducers of microsomal enzymes of the liver (phenytoin, barbiturates, carbamazepine, rifampicin, oxcarbazepine, rifabutin, griseofulvin), the effectiveness of oral contraceptives may decrease and the risk of developing breakthrough uterine bleeding may increase. The maximum level of induction of enzymes is usually achieved not earlier than 2-3 weeks and can be stored up to 4 weeks after the withdrawal of the concomitant drug.

Sugar reduction drugs - a change in the concentration of glucose in the blood.

Cyclosporine - inhibition of the metabolism of the latter, the risk of toxicity.

Antibiotics (for example ampicillin and tetracycline) reduce the effectiveness of the contraceptive effect.

The interaction between oral contraceptives (mainly combined and gestagen-containing) and other drugs can lead to "breakthrough" uterine bleeding and / or a decrease in contraceptive effectiveness.

Activated carbon - reduced absorption of the drug.

Special instructions:

No effect on the ability to drive a car or other machinery has been identified.

In patients with a large body weight, the contraceptive effect of the drug is less effective.

It is necessary to monitor the condition of the mammary glands, as well as to conduct examinations of the pelvic organs.

Despite regular use of the drug, irregular bloody discharge is possible. If the bleeding is frequent and irregular, it is necessary to decide on the appointment of another contraceptive.If the above symptoms continue to occur even after disogestrel cancellation, organic pathology should be ruled out.

Before using the drug, you should carefully collect anamnesis and conduct a thorough gynecological examination to exclude pregnancy.

Instructions

Desogestrel (Desogoestrelum)