Cocaine-induced Cardiomyopathy

Kearston A. S. Barnes, PharmD; Esther O. Fasanmi, PharmD; Ogechi P. Iwuorie, PharmD; Patrick S. Simon, PharmD; Ericka V. Hylick, PharmD

Disclosures

US Pharmacist. 2015;40(2):HS11-HS15. 

In This Article

Background

Cocaine (benzoylmethylecgonine) is a highly addictive crystalline tropine alkaloid derived from the coca plant, which is native to South America.[3] The two forms of cocaine are the hydrochloride salt form, which is commonly injected or sniffed, and its freebase formulation (also known as "crack" or "crack cocaine"), which is typically smoked. Cocaine produces physiological responses ranging from euphoric effects to cardiovascular complications.

With cocaine use, stimulation of the sympathetic nervous system results in blockage of catecholamine reuptake at the sympathetic nerve terminals.[3] This inhibition excites central nervous system sympathetic outflow and increases the adrenergic nerve endings' sensitivity to norepinephrine.[3] Euphoric effects are caused by the modulation of neurotransmitter activity, particularly an increase in dopamine in the brain's mesolimbic region.[4] The potency and duration of the euphoric effects are contingent upon the route of administration. Because of the lack of absorption with IV administration, injection of cocaine has a more rapid effect than other routes of administration (e.g., oral ingestion, nasal inhalation). Absorption rates for nasal inhalation and oral ingestion are similar; however, faster rates have been observed with nasal inhalation.[4]

Inhalation results in a more rapid onset and a shorter duration of action compared with ingestion.[4] The half-life of cocaine depends upon its route of administration and varies from 1 minute up to 2 hours.[4] Cholinesterase, an enzyme found in the liver and the blood, metabolizes cocaine into inactive water-soluble metabolites of benzoylecgonine and ecgonine methyl ester.[4] These by-products, which are excreted primarily via urination, remain detectable in the urine or bloodstream for up to 72 hours.[4]

A multitude of health consequences, particularly adverse cardiovascular events, are likely to result from the use of cocaine. Cocaine exerts effects on endothelial cells by stimulating the release of endothelin-1, a potent vasoconstrictor, and inhibiting the production of nitric oxide, a major vasodilator.[5] In addition, cocaine stimulates the cardiovascular system, increasing the heart rate and blood pressure by blocking the peripheral norepinephrine transporter.[3] Cocaine use is associated with cardiovascular diseases including myocardial infarction (MI), arrhythmias, congestive heart failure (CHF), aortic dissection, endocarditis, and cardiomyopathy.[6]

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