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Akinci et al. Vessel Plus 2021;5:56 https://dx.doi.org/10.20517/2574-1209.2021.20 Page 15 of 20

Table 2. Pharmacological characteristics of intravenous and transdermal antihypertensive agents used in acute blood pressure management in intracerebral hemorrhage patients in clinical trials

Platelet
Agent Mechanism of action Intravenous dose Onset Half-life CBF ICP Autoregulation Trial name
activity
Labetalol [13,17,77,78] α , β , and β -receptor blocker 5-20 mg bolus every 15 min 1-2 min 9 min … … … - INTERACT [38] , INTERACT-2 [49] ,
1
1
2
ATACH-2 [48] , Koch et al. [52]
Metoprolol [77,78] Selective β -receptor blocker 20-80 mg every 10 min 5-10 min 3-7 h … … … - INTERACT, INTERACT-2 [38,49]
1
[49]
Esmolol [17] Selective β -receptor blocker 250 μg/kg bolus followed by 25 1-2 min 9 min … … … + INTERACT-2
1
to 300 μg/kg/min
Urapidil [79,80] Peripheral α1-receptor antagonist 12.5-25 mg bolus followed by 5- 3-5 min 2-4.8 h … … … - INTERACT, INTERACT-2,
and central serotonin 1A receptor 40 mg/h infusion ATACH-2 [38,48,49]
stimulator
Phentolamine [81,82] Peripheral nonselective α-receptor 1-5 mg bolus every 5-10 min 1-2 min 19 min … … ... - INTERACT, INTERACT-2 [38,49]
antagonist
Clonidine [83] Central α -receptor agonist 1.2-7.2 μg/min 5-10 min 12 h … … … … INTERACT-2 [49]
2
Sodium nitroprusside [17,93] Mixed arterial/venous vasodilator 0.25-4 μg/kg/min 1-2 min < 10 min ++ ++ - - INTERACT [38] , INTERACT-2 [49] ,
(nitric oxide donor) Koch et al. [52]
Nitroglycerine [17] Mixed arterial/venous vasodilator 20-400 μg/min 1-2 min 3-5 min + … … - INTERACT [38] , INTERACT-2 [49] ,
(nitric oxide donor) Gong et al. [66]
Transdermal glyceryl Mixed arterial/venous vasodilator 0.2 mg/h, 5 mg/24 h 15-30 min Up to 24 h … … … … INTERACT, ENOS, RIGHT,
[38,64,72,73]
trinitrate [64,84-87] (nitric oxide donor) RIGHT-2
Nicardipine [13,88] Calcium channel blocker 5-15 mg/h 5-10 min 2-4 h + … - - INTERACT [38] , ATACH [48] ,
INTERACT-2 [49] , ATACH-2 [54] ,
[52]
Koch et al.
Diltiazem [88,89] Calcium channel blocker 0.25 mg/kg bolus followed by 5- 2-7 min 3.4 h … … … - ATACH-2 [54]
15 mg/h infusion

Hydralazine [17] Arterial vasodilator 5-20 mg bolus every 15 min 5-20 min 2-8 h ++ ++ - - INTERACT, ICH ADAPT,
INTERACT-2 [38,49,59]
Enalapril [17] ACE inhibitor 1.25-5 mg every 6 h 15-30 min 11 h … … ++ -
[38,49]
Diuretics (furosemide, Inhibits reabsorption of Na/Cl in the Furosemide: 20-40 mg bolus Furosemide: Furosemide: …/… …/… …/… -/- INTERACT, INTERACT-2
bumetanide) [90-92] ascending loop of Henle followed by 10-40 mg/h 5 min 30-60 min
Bumetanide: 0.5-1 mg/dose up to Bumetanide: Bumetanide: 1-
2 times a day followed by 2-3 min 1.5 h
0.5-2 mg/h

ACE: Angiotensin-converting enzyme; CBF: cerebral blood flow; ICP: intracranial pressure; +: increase or favorable effects; ++: subctantial increase or favorable effects; -: decrease or negative effects; …: no
documented direct effect.