Chapter 5: Psychopharmacology

5.2: Pharmacokinetics: What Is It and Why Is It Important?

While this section may sound more like pharmacology, it is important to realize how important pharmacokinetics can be when considering psychoactive drugs. Pharmacokinetics refers to how the body handles a drug that we take. As mentioned earlier, psychoactive drugs exert their effects on behavior by altering neuronal communication in the brain, and the majority of drugs reach the brain by traveling in the blood. The acronym ADME is often used in pharmacology and stands for Absorption (how the drug gets into the blood), Distribution (how the drug gets to the organ of interest – in this chapter, that is the brain), Metabolism (how the drug is broken down so it no longer exerts its psychoactive effects), and Excretion (how the drug leaves the body). We will talk about a couple of these to show their importance for psychoactive drugs.

Drug Administration

There are many ways to take drugs, and these routes of drug administration have a significant impact on how quickly that drug reaches the brain. The most common route of administration is oral administration, which is relatively slow and perhaps surprisingly often the most variable and complex route of administration. Drugs enter the stomach and then get absorbed by the blood supply and capillaries that line the small intestine. The rate of absorption can be affected by a variety of factors, including the quantity and the type of food in the stomach (e.g., fats vs. proteins). This is why the medicine labels for some drugs (like antibiotics) may specifically state foods that you should or should NOT consume within an hour of taking the drug because they can affect the rate of absorption. Two of the most rapid routes of administration include inhalation (i.e., smoking or gaseous anesthesia) and intravenous (IV) in which the drug is injected directly into the vein and hence the blood supply. Both of these routes of administration can get the drug to the brain in less than 10 seconds. IV administration also has the distinction of being the most dangerous because if there is an adverse  drug reaction, there is very little time to administer any antidote, as in the case of an IV heroin overdose.


Image showing the delivery of drug by IV into arm.
Figure 2. A drug delivered by IV reaches the brain more quickly than if the drug is taken orally. While rapid delivery has advantages, there are also risks involved with IV administration.

Why might how quickly a drug gets to the brain be important? If a drug activates the reward circuits in the brain AND it reaches the brain very quickly, the drug has a high risk for abuse and addiction. Psychostimulants like amphetamine or cocaine are examples of drugs that have a high risk for abuse because they are agonists at dopamine (DA) neurons involved in reward AND because these drugs exist in forms that can be either smoked or injected intravenously. Some argue that cigarette smoking is one of the hardest addictions to quit, and although part of the reason for this may be that smoking gets the nicotine into the brain very quickly (and indirectly acts on DA neurons), it is a more complicated story. For drugs that reach the brain very quickly, not only is the drug very addictive, but so are the cues associated with the drug (see Rohsenow et al., 1990). For a crack user, this could be the pipe that they use to smoke the drug. For a cigarette smoker, however, it could be something as normal as finishing dinner or waking up in the morning (if that is when the smoker usually has a cigarette). For both the crack user and the cigarette smoker, the cues associated with the drug may actually cause craving that is alleviated by (you guessed it)—lighting a cigarette or using crack (i.e., relapse). This is one of the reasons individuals who enroll in drug treatment programs, especially out-of-town programs, are at significant risk of relapse if they later find themselves in proximity to old haunts, friends, etc. But this is much more difficult for a cigarette smoker. How can someone avoid eating or avoid waking up in the morning, etc.? These examples help you begin to understand how important the route of administration can be for psychoactive drugs.

Drug Metabolism

Metabolism involves the breakdown of psychoactive drugs, and this occurs primarily in the liver. The liver produces enzymes (proteins that speed up a chemical reaction), and these enzymes help catalyze a chemical reaction that breaks down psychoactive drugs. Enzymes exist in “families,” and many psychoactive drugs are broken down by the same family of enzymes, the cytochrome P450 superfamily. There is not a unique enzyme for each drug; rather, certain enzymes can break down a wide variety of drugs. Tolerance to the effects of many drugs can occur with repeated exposure; that is, the drug produces less of an effect over time, so more of the drug is needed to get the same effect. This is particularly true for sedative drugs like alcohol or opiate-based painkillers. Metabolic tolerance is one kind of tolerance, and it takes place in the liver. Some drugs (like alcohol) cause enzyme induction—an increase in the enzymes produced by the liver. For example, chronic drinking results in alcohol being broken down more quickly, so an alcoholic needs to drink more to get the same effect—of course, until so much alcohol is consumed that it damages the liver (alcohol can cause fatty liver or cirrhosis).

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