LYSTEDA- tranexamic acid tablet
Ferring Pharmaceuticals Inc.
1 INDICATIONS AND USAGE
LYSTEDA� (tranexamic acid, USP) Tablets is indicated for the treatment of cyclic heavy menstrual bleeding [see Clinical Studies (14)].
Prior to prescribing LYSTEDA, exclude endometrial pathology that can be associated with heavy menstrual bleeding.
2 DOSAGE AND ADMINISTRATION
2.1 Recommended Dosage
The recommended dose of LYSTEDA for women with normal renal function is two 650 mg tablets taken three times daily (3900 mg/day) for a maximum of 5 days during monthly menstruation. LYSTEDA may be administered without regard to meals. Tablets should be swallowed whole and not chewed or broken apart
3 DOSAGE FORMS AND STRENGTHS
650 mg tablets
4 CONTRAINDICATIONS
4.1 Thromboembolic Risk
Do not prescribe LYSTEDA to women who are
using combination hormonal contraception
known to have any of the following conditions:
Active thromboembolic disease (e.g., deep vein thrombosis, pulmonary embolism, or cerebral thrombosis)
A history of thrombosis or thromboembolism, including retinal vein or artery occlusion
An intrinsic risk of thrombosis or thromboembolism (e.g., thrombogenic valvular disease, thrombogenic cardiac rhythm disease, or hypercoagulopathy)
Venous and arterial thrombosis or thromboembolism, as well as cases of retinal artery and retinal vein occlusions, have been reported with tranexamic acid.
USE IN SPECIFIC POPULATIONS
8.1 Pregnancy (Category B)
DESCRIPTION
LYSTEDA is an antifibrinolytic drug. The chemical name is trans-4-aminomethyl-cyclohexanecarboxylic acid.
Tranexamic acid is a white crystalline powder. It is freely soluble in water and in glacial acetic acid and is very slightly soluble in ethanol and practically insoluble in ether. The molecular formula is C8 H15 N02 and the molecular weight is 157.2.
Tranexamic acid tablets are provided as white oval-shaped tablets and are not scored. Each tablet is debossed with the marking �FP650." The active ingredient in each tablet is 650 mg tranexamic acid. The inactive ingredients contained in each tablet are: microcrystalline cellulose, colloidal silicon dioxide, pregelatinized corn starch, povidone, hypromellose, stearic acid, and magnesium stearate.
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
Tranexamic acid is a synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin. In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin�s matrix structure.
The antifibrinolytic effects of tranexamic acid are mediated by reversible interactions at multiple binding sites within plasminogen. Native human plasminogen contains 4 to 5 lysine binding sites with low affinity for tranexamic acid (Kd = 750 ?mol/L) and 1 with high affinity (Kd = 1.1 ?mol/L). The high affinity lysine site of plasminogen is involved in its binding to fibrin. Saturation of the high affinity binding site with tranexamic acid displaces plasminogen from the surface of fibrin. Although plasmin may be formed by conformational changes in plasminogen, binding to and dissolution of the fibrin matrix is inhibited.
12.2 Pharmacodynamics
Tranexamic acid, at in vitro concentrations of 25 � 100 �M, reduces by 20 � 60% the maximal rate of plasmin lysis of fibrin catalyzed by tissue plasminogen activator (tPA).
What is LYSTEDA?
LYSTEDA is a prescription medicine used to treat your heavy monthly period (menstruation) when your bleeding gets in the way of social, leisure and physical activities. LYSTEDA does not contain any hormones. On average, LYSTEDA has been shown to lower the amount of blood lost during your monthly period by about one-third, but it is not meant to stop your period.
LYSTEDA is taken only during your period and is not meant to treat pre-menstrual symptoms (symptoms that occur before your bleeding starts). LYSTEDA does not affect your fertility and cannot be used as birth control. LYSTEDA does not protect you against diseases that you may get if you have unprotected sex.
LYSTEDA has not been studied in adolescents younger than 18 years of age.
LYSTEDA is not for women who have already gone through menopause (post-menopausal).
