心脏移植免疫抑制治疗旨在预防或治疗移植术后排斥反应，同时尽量减少不良反应。在全球范围内，IL-2受体拮抗剂已成为心脏移植最常用的免疫诱导剂。临床结果一致表明他克莫司抗排斥反应的作用至少等于或优于环孢素，但接受以两种CNI为基础的维持免疫抑制方案的心脏移植受者术后生存率无差异；快代谢基因型黄种人受者服用环孢素比他克莫司更易以较低剂量达到目标血药浓度。与硫唑嘌呤相比，吗替麦考酚酯可降低受者死亡率和移植心脏功能障碍发生率，并减缓移植心脏血管病的发生和进展。哺乳动物雷帕霉素靶蛋白抑制剂西罗莫司和依维莫司已被用于合并肾功能不全或心脏移植物血管病的受者，但其不良反应发生率较高。关于糖皮质激素撤除及减量的时机，目前仍存在争议。

The goal of immunosuppression after heart transplantation is to prevent or treat allograft rejection while minimizing drug toxicities and adverse effects of immunodeficiency. Currently, Interleukin-2 receptor antagonists had become the most commonly used immune inducers in heart transplantation. The clinical results showed that tacrolimus-based regimens may be associated with lower rejection rates but not with superior survival than cyclosporine-based regimens, the recipients who had extensive metabolism genotype among yellow race taking cyclosporine is more likely to achieve the target plasma concentration with lower doses. Compared with azathioprine, mycophenolate mofetil had been shown to reduce the mortality, the incidence of heart allograft dysfunction, and associated with slower progression of cardiac allograft vasculopathy. Mammalian target of rapamycin (mTOR) inhibitors, Sirolimus and Everolimus, have been used in selected patients with renal insufficiency or cardiac allograft vasculopathy in an attempt to reverse or slow progression of these conditions. However, the high incidence of drug-related adverse effects may limit the widespread use of these agents in heart transplantation. For glucocorticoid, when to stop or reduce it is still a matter of controversy. The timing of corticosteroid withdrawal or reduction remain controversial.