Lynostrenol Tablets BP 0.5mg Taj Pharma
Description
Lynestrenol, , is a progestin medication which is used in birth control pills and in the treatment of gynecological disorders. The medication is available both alone and in combination with an estrogen. It is taken by mouth.
Lynestrenol is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.
It has weak androgenic and estrogenic activity and no other important hormonal activity. The medication is a prodrug of norethisterone in the body, with etynodiol occurring as an intermediate.
Lynestrenol was discovered in the late 1950s and was introduced for medical use in 1961.
Chemistry
IUPAC
ETHYNYL-17ALPHA HYDROXY-17BETA ESTRENE-4
Composition
Each tablet contains
Lynestrenol 0.5mg
Excipients q.s.
Pharmacology
Mechanism of action Lynestrenol is a progestogen structurally related to norethisterone. It may be used alone or as the progestogenic component of some oral contraceptives.
Indications
This generic drug is indicated in the following cases:
Benign breast disease
Combination treatment with estrogen therapy for menopause
Dysmenorrhea
Endometriosis
Fibromas with menorrhagia
Functional gynecological hemorrhage
Gynecological disorders due to luteal insufficiency
Mastodynia
Menstrual irregularity
Premenstrual syndrome [PMS]
Second-line contraception
Therapeutic Categories
Progestin
Hormonal contraceptive for systemic use
Dosage
Oral
Contraception
Adult: 0.5 mg daily when used alone or 0.75-2.5 mg daily when used in combination with an oestrogen.
Oral
Menstrual disorders
Adult: 5-10 mg daily as cyclic regimen.
Warnings for use
Herbal interaction: St John’s wort
Other Warnings
Warnings for special population
Pregnancy
This medicine is not recommended for use in pregnant women.
Breast-feeding
This medicine is not recommended for use in breastfeeding women unless absolutely necessary. All the risks and benefits should be discussed with the doctor before taking this medicine. Your doctor may prescribe a safer alternative based on your clinical condition.
General warnings
Abnormal vaginal bleeding
This medicine is not recommended for use in patients with an undiagnosed vaginal bleeding since it may worsen the patient’s condition. Appropriate diagnostic tests should be undertaken to determine the cause of the vaginal bleeding. Replacement with a suitable alternative may be needed in some cases based on the clinical condition.
Breast Cancer
This medicine may increase the risk of breast cancer in some patients. This risk is especially high in patients over 40 years of age and in patients with a family history of breast cancer. Discuss all the risks and benefits with your doctor before taking this medicine. Replacement with a suitable alternative may be required in some cases based on the clinical condition.
Treatment monitoring
Monitor the endometrium before starting the treatment
Perform breast screening before starting the treatment
Drug interactions
Severity: Contraindication
| Contraceptive progestins + St John’s wort (oral route) | |
| Risks and Mechanisms | Reduced plasma concentrations of the hormonal contraceptive, due to the enzyme inducing effect of St John’s wort, with risk of reduced effectiveness even cancellation of the effect with possibly serious consequences (onset of pregnancy). |
Severity: Combination not recommended
| Contraceptive progestins + Enzyme inducers (except anticonvulsants) | |
| Risks and Mechanisms | Reduced contraceptive effectiveness of the hormonal contraceptive due to its increased hepatic metabolism by the inducer. |
| Course of Action | Preferably use another contraceptive method, particularly a mechanical method for the duration of the association and the following cycle. |
| Contraceptive progestins + Enzyme inducing anticonvulsants | |
| Risks and Mechanisms | Reduced contraceptive effectiveness of the hormonal contraceptive due to its increased hepatic metabolism by the inducer. |
| Course of Action | Preferably use another contraceptive method, particularly a mechanical method for the duration of the association and the following cycle. |
| Contraceptive progestins + Ritonavir-boosted protease inhibitors | |
| Risks and Mechanisms | Risk of reduced contraceptive effectiveness due to reduced concentrations of the hormonal contraceptive, due to its increased hepatic metabolism by ritonavir. |
| Course of Action | Preferably use another contraceptive method, particularly a mechanical method (condom or intrauterine device) for the duration of the association and the following cycle. |
II Moderate
Severity: Precaution
| Contraceptive progestins + Bosentan | |
| Risks and Mechanisms | Risk of reduced contraceptive effectiveness due to increased hepatic metabolism of the hormonal contraceptive. |
| Course of Action | Use another reliable, additional or alternative contraceptive method for the duration of the association and the following cycle. |
| Contraceptive progestins + Griseofulvin | |
| Risks and Mechanisms | Risk of reduced effectiveness of the hormonal contraceptive due to its increased hepatic metabolism. |
| Course of Action | Preferably use another contraceptive method, particularly a mechanical method for the duration of the association and the following cycle. |
| Contraceptive progestins + Sugammadex | |
| Risks and Mechanisms | Reduced contraceptive effectiveness of the hormonal contraceptive. |
| Course of Action | Preferably use another contraceptive method, particularly a mechanical method. |
| Non-contraceptive progestins whether or not related with an oestrogen + Enzyme inducers (except anticonvulsants) | |
| Risks and Mechanisms | Reduced effectiveness of progestin. |
| Course of Action | Clinical monitoring and possible dose adjustment of the hormonal treatment during the administration of the anticonvulsant inhibitor and after its discontinuation. |
| Non-contraceptive progestins whether or not related with an oestrogen + Enzyme inducing anticonvulsants | |
| Risks and Mechanisms | Reduced effectiveness of progestin. |
| Course of Action | Clinical monitoring and possible dose adjustment of the hormonal treatment during the administration of the anticonvulsant inhibitor and after its discontinuation. |
| Orally administered drugs + Cholestyramine | |
| Risks and Mechanisms | Cholestyramine can reduced intestinal absorption, and potentially, the effectiveness of other drugs taken at the same time. This interaction was proved for some substances or therapeutic classes (thyroid hormones, statins, digoxin, oral anticoagulants, hydrochlorothiazide, paracetamol, bile acids) but probably concerns also many other drugs. |
| Course of Action | In general, cholestyramine should be taken sometime after the other drugs (more than two hours, if possible). |
| Orally administered drugs + Topical gastrointestinal agents, antacids and adsorbents | |
| Risks and Mechanisms | Reduced absorption of certain other drugs ingested simultaneously. |
| Course of Action | As a precaution, these topical agents or antacids should be taken some time after any other drug (more than 2 hours, if possible). |
Contraindications
Severity: Absolute contraindication
| History of thromboembolic event Hypersensitivity to one of the components Idiopathic gynecological hemorrhage Severe hepatic failure Thromboembolic event |
Severity: Precaution
| Blindness Cardiovascular disease Diabetes Diplopia Epilepsy History of cardiovascular disease History of chloasma during pregnancy History of diabetes History of epilepsy History of migraine History of smoking Metrorrhagia Migraine Prolonged treatment Renal failure Smoking Thromboembolic disease Vascular retinopathy |
Adverse effects
| System | Medium to high frequency (≥1/1 000) | Low frequency (<1/1 000) | Unknown frequency |
| Cardiovascular system | Venous insufficiency | ||
| Dermatology | Acne Hypertrichosis Pruritus Seborrhea Skin rash | ||
| Digestive system | Digestive disorder Nausea | ||
| Gynecology, Obstetrics | Mastodynia (Exceptionnal) | Amenorrhea Chloasma Menstrual disorder Metrorrhagia | |
| Hepatology | Cholestatic jaundice | ||
| Nervous system | Headache Migraine Vertigo | ||
| Nutrition, Metabolism | Glucose intolerance Weight gain | ||
| Other | Edema | ||
| Psychiatry | Depression Libido disorder Nervousness |
Pregnancy and lactation
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Manufactured in India by:
TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com
