There is evidence of interaction between hormonal contraceptives (estrogen and progesterone) and the inner ear functions, which can result in hearing loss and vestibular dysfunction. Hormonal contraceptives can cause alteration in inner ear fluids homeostasis, affecting the endolymph regulation and transmission of the audiovestibular impulse from the inner ear to higher centers. In addition, it leads to enhancement of the effect of angiotensin Ⅱ, which causes vasoconstriction and reduction in inner ear blood flow. Consequently, hormonal contraceptives can cause tinnitus, hearing loss, vertigo, and aural fullness. The objectives of this review article are to discuss the types, and mechanism of action of hormonal contraceptives, and their effects on the audiovestibular system and inner ear homeostasis.