Livial

Livial - Contraindications | Interactions | Use

Livial is a drug that contains tibolone and belongs to the group of estrogens. It is metabolized in the body into the three active metabolites of which two metabolites (3-alpha-hydroxy-tibolone and 3-beta-hydroxy-tibolone) exhibit estrogenic activity. Third metabolite of this drug (delta isomer of tibolone) exhibits androgenic and progestagenic effects.

It is used as hormone replacement therapy in postmenopausal women. Postmenopausal women are faced with a decreased levels of estrogen which may cause osteoporosis (decreased bone density). Livial acts to increase the production of female sex hormone, and thus prevents the occurrence of osteoporosis.

Contraindications and precautions

Livial is contraindicated in the following conditions:

  • In women who have a history of thromboembolic events (e.g. deep vein thrombosis)
  • In women who have a high risk of heart attack or stroke
  • In women with breast or endometrial cancer
  • In women who have endometrial hyperplasia
  • In women suffering from porphyria
  • In women with severe hepatic impairment

Since this medication increases the risk of heart attack, stroke, and other thromboembolic complications, and considering that its use is associated with an increased incidence of cancer in high-risk patients, Livial should be used only in patients in which climacteric symptoms adversely affect quality of life and use of other, safer drugs for the treatment of postmenopausal symptoms, is not possible.

The risk of cancer is higher if this drug is taken for a long time.

Doctors are advised to take from patients a complete personal and family medical history, to carefully consider the benefit / risk ratio and to be sure to advise women to contact a doctor if they notice any changes in the breasts.

Migraine attacks have been reported in women who were treated with this drug, and treatment should be discontinued immediately if you are experiencing severe headache.

Livial may raise your blood pressure, and regular control of blood pressure while taking this drug is recommended.

Ginsburg, J. et al have analyzed a safety profile of this drug in 301 post-menopausal women. The most common adverse event in this study was weight gain. Due to estrogen activity, this drug tends to produce edema and vaginal bleeding. If vaginal bleeding does not stop even a few months after taking the drug, then you should see your doctor.

How to take

Postmenopausal symptoms usually disappear 3-5 weeks after initiation of therapy.

The recommended dose is 2.5 mg (one tablet) daily. Take your pill every day at the same time.

Treatment should start no later than one year after the last menstrual period.

Treatment should last as short as possible.

It can be taken with meals or on an empty stomach.

Interactions

Livial should not be used simultaneously with the following medicines:

  • Antiepileptic drugs that are substrates for the enzyme CYP3A4 (e.g. phenytoin, carbamazepine and phenobarbital). These drugs bind to the CYP3A4 enzyme which metabolize and eliminate Livial from the body. For this reason, the concomitant use of these drugs can significantly increase the concentration of Livial in the blood and thus leading to side effects.
  • Anticoagulants (e.g. warfarin). Livial exhibits a fibrinolytic activity, and therefore concomitant use increases the risk of bleeding.
  • Drugs used for the treatment of tuberculosis (e.g. rifampicin)
  • Antifungal drugs (itraconazole, ketoconazole and fluconazole)
  • St. John's Wort

Side effects

Livial may cause the following side effects:

  • Increased hair growth
  • Vaginal bleeding
  • Pain in the lower abdomen
  • Breast changes
  • Itching in the genital area
  • Vaginal yeast infection
  • Weight gain
  • Flatulence
  • Edema
  • Dizziness
  • Seborrheic dermatitis
  • Headache (including migraine attacks)
  • Inflammation of the joints
  • Inflammation of muscles
  • Depression

References

  1. NCBI link