Table 1.

Cortisol lowering medications, their effectiveness and effects on hypertension in CS patients.

	Drug	Mechanism of action	Dose used	Hormonal control	Effects on BP	Overall effect on BP
Pituitary directed drugs	Cabergoline	Acts through D2R receptors express on adenocorticotroph	0.5–7 mg/week, oral	25–40%	↓cortisol levels ↑vasodilatation through D1 receptors
	Pasireotide	Somatostatin multi-ligand with particularly high SSTR5	300–1,800 μg/day Twice a day, sc	20–62%	↓cortisol levels
	Retinoic Acid	Reduces ACTH production through inhibition of AP-I and Nur77/Nurrl transcriptional activities	10–80 mg/day 1–3 times/day, oral	20–50%	↓cortisol levels
Steroidogenesis inhibitors	Metyrapone	11β-hydroxylase inhibitor	0.5–6 g/day 3–4 times/day, oral	45–100%	↓cortisol levels ↑11-deoxycorticosterone
	Ketoconazole	Cholesterol side-chain cleavage complex, 17,20-lyase, 11β-hydroxylase and 17α-hydroxylase inhibitor	200–1,200 mg/day 2–3 times/day, oral	~50%	↓cortisol levels
	Osilodrostat	11β-hydroxylase and aldosterone synthase inhibitor	4–60 mg/day 2 times/day, oral	~90%	↓cortisol levels ↑11-deoxycorticosterone
	Mitotane	Inhibition of steroid synthesis (inhibition of SOAT1, intracellular toxic lipid accumulation) + adrenolytic action	2–5 g/day 2–3 times/day, oral	~70%	↓cortisol levels ↓aldosterone levels
GR antagonist	Mifepristone	Glucocorticoid receptor antagonist	300–1,200 mg/day Once daily, oral	NA	↓cortisol action on GR ↑cortisol levels and its action on MR

↑ means increase; ↓ decrease; = neutral effect.