Exluton^® (Tablets) Instructions for Use

Marketing Authorization Holder

N.V. Organon (Netherlands)

ATC Code

G03AC02 (Lynestrenol)

Active Substance

Lynestrenol (Rec.INN registered by WHO)

Dosage Form

Exluton®

Tablets 500 mcg: 28 or 84 pcs.

Dosage Form, Packaging, and Composition

Tablets are white, round, flat, with beveled edges, engraved with “TT” over “2” on one side and with the inscription “ORGANON” on the other.

Excipients: potato starch, amylopectin, lactose monohydrate, magnesium stearate.

28 pcs. – blisters (1) – cardboard packs.
28 pcs. – blisters (3) – cardboard packs.

Clinical-Pharmacological Group

Gestagen for oral contraception

Pharmacotherapeutic Group

Progestogen

Pharmacological Action

Synthetic gestagen.

It causes the transition of the endometrium from the proliferation phase to the secretory phase.

It suppresses ovulation.

The mechanism of contraceptive action is associated mainly with the peripheral gestagenic effect on the reproductive system, which is expressed in a decrease in the amount and an increase in the viscosity of cervical mucus, and a decrease in the penetrating ability of spermatozoa.

It inhibits the transport function of the fallopian tubes and reduces the implantation properties of the endometrium.

Pharmacokinetics

After oral administration, Lynestrenol is rapidly absorbed and undergoes conversion in the liver into the pharmacologically active norethisterone.

The maximum level of norethisterone in blood plasma is observed 2-4 hours after taking lynestrenol.

The T_1/2 of norethisterone after taking lynestrenol is approximately 8-11 hours.

Lynestrenol and its metabolites are predominantly excreted by the kidneys and, to a lesser extent, through the intestines.

Indications

For use as a therapeutic agent: polymenorrhea; menorrhagia and metrorrhagia; some cases of primary or secondary amenorrhea or oligomenorrhea; endometriosis, some cases of endometrial carcinoma; benign breast diseases; for suppression of ovulation (not for contraception), ovulatory pain and menstruation; dysmenorrhea; for postponement of normal menstruation; supplement to estrogen replacement therapy in perimenopause and postmenopause to prevent endometrial hyperplasia.

Oral contraception.

ICD codes

Dosage Regimen

Determine the dosage regimen individually based on the specific therapeutic indication.

For oral contraception, take one 500 mcg tablet daily without interruption.

Start the first tablet on the first day of the menstrual cycle.

Take subsequent tablets at the same time each day.

Continue taking one tablet daily from each new pack immediately after finishing the previous one.

For menstrual cycle regulation, the typical dose is one 500 mcg tablet daily for 10 to 14 days during the second half of the cycle.

For endometriosis, administer one 500 mcg tablet daily for uninterrupted periods of 3 to 6 months.

For estrogen replacement therapy supplementation, take one 500 mcg tablet daily for the last 12 to 14 days of each estrogen cycle.

For postponement of menstruation, take one tablet daily, starting 14 days before the expected onset of menstruation.

Adjust the dose and duration for benign breast diseases and endometrial carcinoma based on clinical response.

Take the tablet orally with water, with or without food.

If vomiting occurs within 3-4 hours of intake, consider it a missed tablet and follow the relevant instructions.

Manage a missed dose by taking it as soon as remembered and the next dose at the regular time.

If more than 27 hours have passed, contraceptive reliability may be reduced; use a barrier method for 7 days.

Adverse Reactions

When used as a therapeutic agent, the following are possible: metrorrhagia, breast tenderness, amenorrhea, vaginal discharge, cervical discharge; headache, migraine, dizziness, increased libido, decreased libido, increased nervous excitability, depression; weight gain, fluid retention, incl. peripheral edema, decreased glucose tolerance, abnormalities in lipid parameters; nausea, vomiting, abdominal pain, diarrhea, constipation; jaundice, changes in liver function tests; increased sweating, acne, seborrhea, hirsutism, chloasma, rash, urticaria; hypercoagulation; hypersensitivity reactions.

When used as an oral contraceptive, the following are possible: hypersensitivity, tenderness, breast enlargement; irregular bleeding, changes in vaginal secretion; headache, migraine, changes in libido, depression, mood changes; skin rash, erythema nodosum, erythema multiforme; nausea, vomiting, abdominal pain, diarrhea, constipation; fluid retention, weight changes, hypersensitivity reactions; contact lens intolerance; chloasma.

Contraindications

For use as a therapeutic agent: hypersensitivity to lynestrenol; pregnancy or suspected pregnancy, breastfeeding period; ectopic pregnancy (in history); severe liver diseases, such as cholestatic jaundice or hepatitis (or a history of severe liver disease if liver function tests have not returned to normal), hepatoma; Rotor syndrome, Dubin-Johnson syndrome; Gilbert’s syndrome; vaginal bleeding of unknown etiology; conditions (current or in history) that may be aggravated by the intake of sex steroid hormones (incl. gestational herpes, gestational jaundice, otosclerosis, chloasma of pregnancy, severe itching, porphyria).

With caution, regular examination of patients with any of the following conditions should be performed: chronic heart failure; arterial hypertension; thromboembolism (in history); depression (in history).

For oral contraception: hypersensitivity to lynestrenol; established or suspected pregnancy; current venous thromboembolism; current or history of severe liver disease – until liver function tests normalize; cholestatic jaundice; porphyria (diagnosed or in history); otosclerosis (diagnosed or in history); history of herpes of pregnancy; progestogen-dependent tumors; vaginal bleeding of unknown etiology.

With caution. In the presence of any of the conditions/diseases listed below, the benefit of using a progestogen and the possible risks for each individual woman should be weighed.

This should be discussed with the woman before she starts taking lynestrenol.

In cases of worsening, exacerbation of the disease or the occurrence of any of these conditions for the first time, the woman should consult a doctor to decide on the possibility of further use of lynestrenol.

Risk of breast cancer. Increases with age.

During the use of oral contraceptives (OCs), the risk of breast cancer slightly increases, which may be due to earlier diagnosis, the action of lynestrenol, or a combination of these two factors.

However, this increased risk gradually disappears within 10 years after stopping OC use, it is not related to the duration of use and depends on the woman’s age during OC use.

Cases of breast cancer diagnosed in women using oral contraceptives are clinically less pronounced than cancer detected in women who have never used OCs.

Individual assessment of the benefit-risk ratio of contraceptive use should be carried out in the presence of breast cancer.

Since it is impossible to exclude a negative effect of progestogens on the development of liver cancer, an individual assessment of the benefit-risk ratio should be carried out in women with liver cancer.

Epidemiological studies have established a connection between the use of combined oral contraceptives (COCs) and an increased incidence of venous thromboembolism (deep vein thrombosis and pulmonary embolism).

And although this is not clinically confirmed for contraceptives that do not contain an estrogen component, Lynestrenol should be discontinued in case of thrombosis development.

Discontinuation of lynestrenol should also be considered in case of possible surgery or in the presence of another disease requiring prolonged immobilization.

Women with a history of thromboembolic disorders should be warned about the possibility of their recurrence.

Although progestogens can affect peripheral tissue insulin resistance and glucose tolerance, there is no evidence that there is a need to change hypoglycemic therapy in patients with diabetes using progestogen-containing OCs.

However, women with diabetes should be closely monitored throughout the period of use of progestogen-containing OCs.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy as a therapeutic agent.

Not prescribed during pregnancy as an oral contraceptive.

The safety of using lynestrenol during lactation (breastfeeding) has not been established to date.

Use in Hepatic Impairment

Contraindicated in severe liver diseases.

Special Precautions

When used as a therapeutic agent, use with caution in cases of symptoms of heart failure, arterial hypertension, depression, and a history of thromboembolic processes.

When used as a contraceptive, in case of acyclic bloody discharge or oligomenorrhea, it is necessary to exclude pregnancy and organic pathology.

Women should be informed that Lynestrenol does not protect against HIV infections (AIDS) and other sexually transmitted diseases.

With long-term use as a therapeutic agent, systematic medical examinations are indicated: monitoring of lipid and carbohydrate metabolism parameters, bilirubin concentration, transaminases, and the coagulation system.

The frequency and nature of systematic medical examinations depend on the circumstances in each individual case and should be determined in accordance with the clinical conclusion, but not less than once every 6 months.

Epidemiological studies have revealed a connection between the use of progestogen in combination with estrogens and an increase in the frequency of cases of venous thromboembolism (deep vein thrombosis and pulmonary embolism).

Despite the fact that the clinical significance of these data for lynestrenol without an estrogen component is unknown, in case of thrombosis, lynestrenol should be discontinued.

The need to discontinue lynestrenol should also be considered in case of prolonged immobilization due to surgery or illness.

Women with a history of thromboembolic diseases should be informed about the possibility of their recurrence.

During the intake of lynestrenol, it is recommended to limit the intake of fats and carbohydrates (which is especially important for women with initially increased body weight).

Drug Interactions

Rifamycin, hydantoin derivatives (including phenytoin), barbiturates (including primidone), carbamazepine, aminoglutethimide, rifampicin, laxatives, activated charcoal; oxcarbazepine, topiramate, rifabutin, felbamate, ritonavir, griseofulvin and preparations containing St. John’s wort (Hypericum perforatum) may also reduce the effectiveness of lynestrenol.

Women who use Lynestrenol for contraception and simultaneously use any of these medicines should temporarily use a barrier method in addition to lynestrenol or choose another method of contraception.

The barrier method should be used both during the concomitant use of medicines and for 28 days after their discontinuation.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°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.