Oral modified-release tranexamic acid for heavy menstrual bleeding.
OBJECTIVE
To review the pharmacology, pharmacokinetics, efficacy, and safety profile of an oral modified-release (MR) formulation of tranexamic acid.


METHODS
Literature was accessed through MEDLINE (1966-July 2012), Iowa Drug Information Service (1997-July 2012), and bibliographies of pertinent articles. Search terms included tranexamic acid, Lysteda, menorrhagia, menstrual blood loss, and heavy menstrual bleeding.


METHODS
All available English-language abstracts and human studies were identified for review. Data provided by the manufacturer and the Food and Drug Administration were also evaluated. Efficacy was evaluated in 2 clinical trials, change in quality of life was evaluated in 3 clinical trials, and safety was evaluated in 4 clinical trials.


RESULTS
Tranexamic acid is a synthetic lysine analogue with antifibrinolytic activity. It interferes with the binding of plasminogen to fibrin, resulting in enhanced fibrin clot integrity. A novel MR formulation of oral tranexamic acid is approved for treatment of cyclic heavy menstrual bleeding. MR tranexamic acid is initiated at the beginning of heavy menstrual bleeding and can be taken for up to 5 days per cycle. Clinical trials show it to be safe and effective. Dosage adjustments are needed for women with renal insufficiency. Adverse effects are considered mild to moderate, with the most common being menstrual discomfort, headache, and back pain. The most significant safety concerns relate to the risk of thromboembolism.


CONCLUSIONS
MR tranexamic acid offers a new first-line therapy for patients with cyclic heavy menstrual bleeding. It is reported to be safe and effective. There are no labeled equivalents to MR tranexamic acid for cyclic heavy menstrual bleeding.
Department of Pharmaceutical and Biomedical Sciences, Raabe College of Pharmacy, Ohio Northern University, Ada, USA. s-hrometz@onu.edu
Sandra L
SL
Hrometz
D000284:Administration, Oral; D000818:Animals; D000933:Antifibrinolytic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D008595:Menorrhagia / Q000188:drug therapy*; D011788:Quality of Life; D014148:Tranexamic Acid / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D016896:Treatment Outcome
D000933:Antifibrinolytic Agents; D014148:Tranexamic Acid