The pharmacokinetic approach to treatment targets the drug molecules themselves, aiming to reduce their concentration at the site of action, thereby reducing or preventing any pharmacodynamic effect. This approach might be useful in the treatment of acute drug toxicity/overdose and in the long-term treatment of addiction. Early clinical trials with anticocaine and antinicotine vaccines have shown reduced drug use and good tolerability. Also showing promise in animal studies are monoclonal antibodies against cocaine, methamphetamine and phencyclidine, as well as the enhancment of cocaine metabolism with genetic variants of human butyrylcholinesterase, using a bacterial esterase or catalytic monoclonal antibodies. Pharmacokinetic treatments offer potential advantages in terms of patient compliance, absence of medication interactions and benefit for patients who cannot take standard medications.