Desogestrel (Tablets) Instructions for Use

Marketing Authorization Holder

Alkaloid AD Skopje (Republic of North Macedonia)

Manufactured By

Lupin, Ltd. (India)

ATC Code

G03AC09 (Desogestrel)

Active Substance

Desogestrel (Rec.INN registered by WHO)

Dosage Form

Desogestrel

Film-coated tablets 75 mcg

Dosage Form, Packaging, and Composition

Film-coated tablets

28 pcs. – blisters – cardboard packs (28 pcs.) – By prescription

Clinical-Pharmacological Group

Gestagen for oral contraception

Pharmacotherapeutic Group

Sex hormones and modulators of the genital system; systemic hormonal contraceptives; progestogens

Pharmacological Action

Synthetic progestin, chemically similar to levonorgestrel. It has progestogenic activity. It causes the transition of the endometrial epithelium from the proliferative phase to the secretory phase.

It increases the viscosity of cervical mucus. It inhibits the secretion of LH by the pituitary gland and, thus, causes inhibition of ovulation. It has weak androgenic activity, which may not manifest.

Pharmacokinetics

After oral administration, Desogestrel is rapidly absorbed. The mean C_max in serum is reached after 1.8 h (T_max) after administration. The bioavailability of etonogestrel is about 70%.

Etonogestrel is 95.5-99% bound to plasma proteins, mainly to albumin and to a lesser extent to sex hormone-binding globulin (SHBG).

C_ss in plasma is established after 4-5 days.

Desogestrel is metabolized by hydroxylation and dehydrogenation into the active metabolite etonogestrel. Etonogestrel is metabolized by the formation of sulfate and glucuronide conjugates.

The mean T_1/2 of etonogestrel is about 30 h, both after single and multiple administration. Etonogestrel and its metabolites are excreted by the kidneys and through the intestines (in a ratio of 1.5:1) in the form of free steroids and conjugates.

Etonogestrel is excreted in breast milk.

Indications

Contraception.

ICD codes

Dosage Regimen

Take one 75 mcg tablet orally once daily. Administer at approximately the same time every day.

Start taking the tablets on the first day of your menstrual cycle. If starting after day one of menstruation, use an additional barrier method of contraception for the first 7 days of tablet intake.

Take the tablets continuously without a break. After finishing one pack, immediately start the next pack the following day.

If a vomiting episode occurs within 3-4 hours of taking a tablet, take another tablet from the pack. If you do not take this replacement tablet, use a barrier method for 7 days.

In case of severe diarrhea, use a barrier method of contraception during the illness and for 7 days after recovery.

If you miss a dose by less than 12 hours, take the missed tablet immediately. Take the next tablet at the usual time. Contraceptive protection is not reduced.

If you miss a dose by more than 12 hours, take the missed tablet immediately, even if it means taking two tablets in one day. Take subsequent tablets at the usual time. Use a barrier method of contraception for the next 7 days.

Consult a physician for specific instructions following missed doses, particularly if they occur in the first week of a new pack.

Adverse Reactions

Psychiatric disorders: frequent – mood changes, decreased libido, depressive disorder.

Nervous system disorders: frequent – headache.

Eye disorders infrequent – contact lens intolerance.

Gastrointestinal disorders: frequent – nausea; infrequent – vomiting.

Skin and subcutaneous tissue disorders: frequent – acne; infrequent – alopecia; rare – skin rash, urticaria, erythema nodosum.

Reproductive system and breast disorders frequent – breast tenderness, irregular menstrual bleeding, amenorrhea; infrequent – dysmenorrhea, ovarian cyst, vaginitis; rare – breast discharge, ectopic pregnancy.

General disorders frequent – weight increased; infrequent – fatigue.

In women receiving (combined) oral contraceptives, various serious adverse effects have been rarely observed venous and arterial thrombosis and thromboembolism, hormone-dependent tumors (e.g., breast cancer) and chloasma.

Contraindications

Hypersensitivity to desogestrel; current or history of venous thromboembolism (including deep vein thrombosis of the lower extremities, pulmonary embolism); current or history of severe liver disease (until liver function tests normalize); current or history of hepatic insufficiency; established or suspected malignant hormone-dependent tumors (including breast cancer); vaginal bleeding of unknown etiology; established or suspected pregnancy; children and adolescents under 18 years of age.

With caution persistent arterial hypertension; prolonged immobilization associated with surgery, disease, or injury, liver cancer, chloasma, especially in women with a history of chloasma during pregnancy, diabetes mellitus, porphyria, systemic lupus erythematosus, herpes (with a history of herpes during pregnancy).

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy.

May be used during breastfeeding if indicated.

Use in Hepatic Impairment

Contraindicated for use in severe liver diseases, including history (until liver function tests normalize), as well as in hepatic insufficiency, including history.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

Before using desogestrel, a thorough history should be taken and a gynecological examination should be performed to rule out pregnancy.

Despite regular use of desogestrel, irregular spotting may occur. If bleeding is frequent and irregular, the issue of prescribing another contraceptive method should be considered. If the above symptoms persist even after discontinuation of desogestrel, organic pathology should be ruled out.

The contraceptive effect of desogestrel is less effective in patients with high body weight.

Desogestrel can be used in combination with ethinylestradiol.

Drug Interactions

Drug interaction of desogestrel with drugs that induce microsomal enzymes, leading to an increase in the clearance of sex hormones, is possible, for example, hydantoins (phenytoin), barbiturates (phenobarbital), primidone, carbamazepine, rifampicin; and probably also oxcarbazepine, rifabutin, topiramate, felbamate, ritonavir, nelfinavir, griseofulvin and preparations containing St. John’s wort . Women using any of these drugs should use another method of contraception during the use of desogestrel.

When using activated charcoal, the absorption of desogestrel may decrease and, consequently, the contraceptive effectiveness may decrease.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.