Chemistry:Cardiac stimulant
A cardiac stimulant is a drug which acts as a stimulant of the heart to increase cardiac output. They can work via positive chronotropic action (increased heart rate) and/or positive inotropic action (increased myocardial contractility).
Within positive inotropes, there are calcium mobilizers and calcium sensitizers.[1][2][3] Calcium mobilizers are conventional positive inotropes that elevate intracellular calcium, whereas calcium sensitizers do not elevated intracellular calcium but instead increase sensitivity to it.[1][2][3]
Cardiac stimulants are known to be used (and banned) as performance-enhancing drugs, including for doping in sport.[4][5]
Examples
- Sympathomimetics
- β1-Adrenergic receptor agonists like epinephrine, norepinephrine, dopamine, dobutamine, denopamine, isoproterenol, and xamoterol[6][7]
- Indirectly acting adrenergic agonists (via activation of β1-adrenergic receptors)[8]
- Norepinephrine prodrugs like droxidopa (L-DOPS)
- Norepinephrine reuptake inhibitors like atomoxetine, reboxetine, desipramine, nortriptyline, bupropion, milnacipran, methylphenidate, and cocaine[8]
- Norepinephrine releasing agents like amphetamine, methamphetamine, ephedrine, pseudoephedrine, phenylpropanolamine, and mephentermine[8]
- Sympatholytics
- Antimuscarinic anticholinergics like atropine[8]
- Adenosine receptor antagonists like caffeine, theophylline, and aminophylline[8]
- Phosphodiesterase PDE3 inhibitors like amrinone, milrinone, and pimobendan[6][7][8]
- Cardiac glycosides like digoxin[7]
- Calcium sensitizers like levosimendan, pimobendan, and omecamtiv mecarbil
- Other agents like hydralazine and cannabinoids[8]
Exercise is a cardiac stimulant by increasing levels of the sympathomimetic catecholamines epinephrine and norepinephrine.[9][10]
References
- ↑ 1.0 1.1 "Calcium sensitizers: What have we learned over the last 25 years?". Int J Cardiol 203: 543–548. January 2016. doi:10.1016/j.ijcard.2015.10.240. PMID 26580334.
- ↑ 2.0 2.1 "Pathogenesis and pathophysiology of heart failure with reduced ejection fraction: translation to human studies". Heart Fail Rev 24 (5): 743–758. September 2019. doi:10.1007/s10741-019-09806-0. PMID 31209771.
- ↑ 3.0 3.1 "Inotropes and inodilators for acute heart failure: sarcomere active drugs in focus". J Cardiovasc Pharmacol 64 (3): 199–208. September 2014. doi:10.1097/FJC.0000000000000113. PMID 24785346.
- ↑ "Pharmacology of stimulants prohibited by the World Anti-Doping Agency (WADA)". Br J Pharmacol 154 (3): 606–622. June 2008. doi:10.1038/bjp.2008.124. PMID 18500382.
- ↑ "Pharmacology of Drugs Used as Stimulants". J Clin Pharmacol 61 Suppl 2: S53–S69. August 2021. doi:10.1002/jcph.1918. PMID 34396557.
- ↑ 6.0 6.1 "Inotropes and vasopressors: review of physiology and clinical use in cardiovascular disease". Circulation 118 (10): 1047–56. September 2008. doi:10.1161/CIRCULATIONAHA.107.728840. PMID 18765387.
- ↑ 7.0 7.1 7.2 "Pharmacotherapeutics of positive inotropes". AORN J 71 (1): 173–8, 181–5; quiz 186–8, 190–2. January 2000. doi:10.1016/s0001-2092(06)62180-7. PMID 10686650.
- ↑ 8.0 8.1 8.2 8.3 8.4 8.5 8.6 8.7 8.8 "Comprehensive review of cardiovascular toxicity of drugs and related agents". Med Res Rev 38 (4): 1332–1403. July 2018. doi:10.1002/med.21476. PMID 29315692.
- ↑ "Stress and the neuroendocrine system: the role of exercise as a stressor and modifier of stress". Expert Rev Endocrinol Metab 1 (6): 783–792. November 2006. doi:10.1586/17446651.1.6.783. PMID 20948580.
- ↑ "Relationships among norepinephrine levels, exercise capacity, and chronotropic responses in heart failure patients". Heart Fail Rev 28 (1): 35–45. January 2023. doi:10.1007/s10741-022-10232-y. PMID 35325323.
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