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A psychoactive drug, psychopharmaceutical, mind-altering drug, consciousness-altering drug, psychoactive substance, or psychotropic substance is a chemical substance that alters psychological functioning by modulating central nervous system (CNS) activity.9780724533619 . ISBN 9780724533619 Psychoactive and psychotropic drugs both affect the brain, with psychotropics sometimes referring to psychiatric drugs or high-abuse substances, while “drug” can have negative connotations. Designer drug are designer drugs made to mimic illegal ones and bypass laws.
Psychoactive drug use dates back to prehistory for medicinal and consciousness-altering purposes, with evidence of widespread cultural use. Many animals intentionally consume psychoactive substances, and some traditional legends suggest animals first introduced humans to their use. Psychoactive substances are used across cultures for purposes ranging from medicinal and therapeutic treatment of Mental disorder and pain, to performance enhancement. Their effects are influenced by the drug itself, the environment, and individual factors. Psychoactive drugs are categorized by their pharmacological effects into types such as Anxiolytic (reduce anxiety), Entactogen (enhance empathy), Stimulant (increase CNS activity), Depressant (decrease CNS activity), and Hallucinogen (alter perception and emotions). Psychoactive drugs are administered through various routes—including oral ingestion, injection, rectal use, and inhalation—with the method and efficiency differing by drug.
Psychoactive drugs alter brain function by interacting with neurotransmitter systems—either Agonist or inhibiting activity—which can affect mood, perception, cognition, behavior, and potentially lead to dependence or long-term neural adaptations such as sensitization or Drug tolerance. Addiction and dependence involve psychological and physical reliance on psychoactive substances, with treatments ranging from psychotherapy and medication to emerging psychedelic therapies; global prevalence is highest for Alcoholism, cannabis, and opioid use disorders.
The legality of psychoactive drugs has long been controversial, shaped by international treaties like the 1961 Single Convention on Narcotic Drugs and national laws such as the United States Controlled Substances Act. Distinctions are made between recreational and medical use. Enforcement varies across countries. While the 20th century saw global criminalization, recent shifts favor harm reduction and regulation over prohibition. Widely used psychoactive drugs include legal substances like caffeine, alcohol, and nicotine; prescribed medications such as SSRIs, Opioid, and Benzodiazepine; and illegal recreational drugs like cocaine, LSD, and MDMA.
Psychoactive substances have been used medicinally and to alter consciousness. Consciousness altering may be a primary drive, akin to the need to satiate thirst, hunger, or sexual desire. This may be manifest in the long history of drug use, and even in children's desire for spinning, swinging, or sliding, suggesting that the drive to alter one's state of mind is universal.
In The Hasheesh Eater (1857), American author Fitz Hugh Ludlow was one of the first to describe in modern terms the desire to change one's consciousness through drug use:
During the 20th century, the majority of countries initially responded to the use of recreational drugs by prohibiting production, distribution, or use through criminalization. A notable example occurred with Prohibition in the United States, where early in the century alcohol was made illegal for 13 years. In recent decades, an emerging perspective among governments and law enforcement holds that illicit drug use cannot be stopped through prohibition. One organization holding that view, Law Enforcement Against Prohibition (LEAP), concluded that "in fighting a war on drugs the government has increased the problems of society and made them far worse. A system of regulation rather than prohibition is a less harmful, more ethical and a more effective public policy."
In some countries, there has been a move toward harm reduction, where the use of illicit drugs is neither condoned nor promoted, but services and support are provided to ensure users have adequate factual information readily available, and that the negative effects of their use be minimized. Such is the case with Portugal's drug policy of decriminalization, with a primary goal of reducing the adverse health effects of drug use.
The term "drug" has become a skunked term. "Drugs" can have a negative connotation, often associated with illegal substances like cocaine or heroin, despite the fact that the terms "drug" and "medicine" are sometimes used interchangeably. (2025). 9781441999016 ISBN 9781441999016
Novel psychoactive substances (NPS), also known as "Designer drug" are a category of psychoactive drugs (substances) that are designed to mimic the effects of often illegal drugs, usually in efforts to circumvent existing drug laws.
In addition, several psychoactive substances are currently employed to treat various addictions. These include acamprosate or naltrexone in the treatment of alcoholism, or methadone or buprenorphine maintenance therapy in the case of opioid addiction. (2025). 9780199381708, Oxford University Press. ISBN 9780199381708
Exposure to psychoactive drugs can cause neuroplasticity that counteract or augment some of their effects; these changes may be beneficial or harmful. However, there is a significant amount of evidence that the relapse rate of mental disorders negatively corresponds with the length of properly followed treatment regimens (that is, relapse rate substantially declines over time), and to a much greater degree than placebo.
Both military and civilian American intelligence officials are known to have used psychoactive drugs while interrogating captives apprehended in its "war on terror". In July 2012 Jason Leopold and Jeffrey Kaye, psychologists and human rights workers, had a Freedom of Information Act request fulfilled that confirmed that the use of psychoactive drugs during interrogation was a long-standing practice. Captives and former captives had been reporting medical staff collaborating with interrogators to drug captives with powerful psychoactive drugs prior to interrogation since the very first captives release. In May 2003 recently released Pakistani captive Sha Mohammed Alikhel described the routine use of psychoactive drugs. He said that Jihan Wali, a captive kept in a nearby cell, was rendered catatonic through the use of these drugs.
Alcohol has a long association of military use, and has been called "liquid courage" for its role in preparing troops for battle, Anesthesia injured soldiers, and celebrate military Victory. It has also served as a coping mechanism for combat stress reactions and a means of decompression from combat to everyday life. However, this reliance on alcohol can have negative consequences for physical and mental health.
The first documented case of a soldier overdosing on methamphetamine during combat, was the Finnish corporal Aimo Koivunen, a soldier who fought in the Winter War and the Continuation War.
In some modern and ancient cultures, drug usage is seen as a Social status symbol. Recreational drugs are seen as status symbols in settings such as at and parties. For example, in ancient Egypt, gods were commonly pictured holding hallucinogenic plants.
Because there is controversy about regulation of recreational drugs, there is an ongoing debate about drug prohibition. Critics of prohibition believe that regulation of recreational drug use is a violation of personal autonomy and liberty. In the United States, critics have noted that prohibition or regulation of recreational and spiritual drug use might be unconstitutional, and causing more harm than is prevented.Barnett, Randy E. "The Presumption of Liberty and the Public Interest: Medical Marijuana and Fundamental Rights" . Retrieved 4 July 2007.
Some people who take psychoactive drugs experience drug or substance induced psychosis. A 2019 systematic review and meta-analysis by Murrie et al. found that the pooled proportion of transition from substance-induced psychosis to schizophrenia was 25% (95% CI 18%–35%), compared with 36% (95% CI 30%–43%) for brief, atypical and not otherwise specified psychoses. Type of substance was the primary predictor of transition from drug-induced psychosis to schizophrenia, with highest rates associated with cannabis (6 studies, 34%, CI 25%–46%), hallucinogens (3 studies, 26%, CI 14%–43%) and amphetamines (5 studies, 22%, CI 14%–34%). Lower rates were reported for opioid (12%), alcohol (10%) and sedative (9%) induced psychoses. Transition rates were slightly lower in older cohorts but were not affected by sex, country of the study, hospital or community location, urban or rural setting, diagnostic methods, or duration of follow-up.
§3 The wine must be natural, made from grapes of the vine, and not corrupt. Code of Canon Law, 1983
The use of entheogens for religious purposes resurfaced in the West during the counterculture movements of the 1960s and 70s. Under the leadership of Timothy Leary, new spiritual and intention-based movements began to use LSD and other hallucinogens as tools to access deeper inner exploration. In the United States, the use of peyote for ritual purposes is protected only for members of the Native American Church, which is allowed to cultivate and distribute peyote. However, the genuine religious use of peyote, regardless of one's personal ancestry, is protected in Colorado, Arizona, New Mexico, Nevada, and Oregon.
The substances most widely used in self-medication are over-the-counter drugs and dietary supplements, which are used to treat common health issues at home. These do not require a Physician prescription to obtain and, in some countries, are available in supermarkets and convenience stores.
There are many different types of drugs that are commonly associated with their effects on sex, including alcohol, cannabis, cocaine, MDMA, GHB, amphetamines, , , and many others.
Most people are under the influence of sedative (such as alcohol or benzodiazepines) when they die by suicide, with alcoholism present in between 15% and 61% of cases. Countries that have higher rates of alcohol use and a greater density of bars generally also have higher rates of suicide. About 2.2–3.4% of those who have been treated for alcoholism at some point in their life die by suicide. Alcoholics who attempt suicide are usually male, older, and have tried to take their own lives in the past. In adolescents who misuse alcohol, neurological and psychological dysfunctions may contribute to the increased risk of suicide.
Overdose attempts using Analgesics are among the most common, due to their easy availability over-the-counter.
The psychiatric drugs fluoxetine, quetiapine, and lorazepam are orally in tablet or capsule form. Grain alcohol and caffeine are ingested in beverage form; nicotine and cannabis are smoked or vaporized; peyote and psilocybin mushrooms are ingested in botanical form or dried; and crystalline drugs such as cocaine and methamphetamine are usually inhaled or snorted.
This theory clearly states that the effects are equally the result of chemical, pharmacological, psychological, and physical influences. The model that Timothy Leary proposed applied to the psychedelics, although it also applies to other psychoactives.
Drugs that increase activity in particular neurotransmitter systems are called agonists. They act by increasing the synthesis of one or more neurotransmitters, by reducing its reuptake from the synapses, or by mimicking the action by binding directly to the postsynaptic receptor. Drugs that reduce neurotransmitter activity are called antagonists, and operate by interfering with synthesis or blocking postsynaptic receptors so that neurotransmitters cannot bind to them.Martin E.P. Seligma (1984). 039394459X, W. W. Norton & Company. 039394459X
Exposure to a psychoactive substance can cause changes in the structure and functioning of neurons, as the nervous system tries to re-establish the homeostasis disrupted by the presence of the drug (see also, neuroplasticity). Exposure to antagonists for a particular neurotransmitter can increase the number of receptors for that neurotransmitter or the receptors themselves may become more responsive to neurotransmitters; this is called sensitization. Conversely, overstimulation of receptors for a particular neurotransmitter may cause a decrease in both number and sensitivity of these receptors, a process called desensitization or Drug tolerance. Sensitization and desensitization are more likely to occur with long-term exposure, although they may occur after only a single exposure. These processes are thought to play a role in drug dependence and addiction. Physical dependence on antidepressants or anxiolytics may result in worse depression or anxiety, respectively, as withdrawal symptoms. Unfortunately, because clinical depression (also called major depressive disorder) is often referred to simply as depression, antidepressants are often requested by and prescribed for patients who are depressed, but not clinically depressed.
| (acetylcholine receptor agonists) | arecoline, nicotine, piracetam | |
| Muscarinic antagonists (acetylcholine receptor antagonists) | scopolamine, benzatropine, dimenhydrinate, diphenhydramine, trihexiphenidyl, doxylamine, atropine, quetiapine, olanzapine, most tricyclics | |
| Nicotinic antagonists (acetylcholine receptor antagonists) | memantine, bupropion | |
| Adenosine receptor antagonistsFord, Marsha. Clinical Toxicology. Philadelphia: Saunders, 2001. Chapter 36 – Caffeine and Related Nonprescription Sympathomimetics. | caffeine, theobromine, theophylline | |
| Dopamine reuptake inhibitors | cocaine, bupropion, methylphenidate, modafinil, St John's wort | |
| Dopamine releasing agents | amphetamine, methamphetamine, MDMA, cathinone, phentermine, phenmetrazine, aminorex | |
| pramipexole, Ropinirole, L-DOPA (prodrug), memantine | ||
| Dopamine antagonists | haloperidol, droperidol, many antipsychotics (e.g., risperidone, olanzapine, quetiapine) | |
| Dopamine partial agonists | LSD, aripiprazole | |
| GABA reuptake inhibitors | tiagabine, St John's wort, vigabatrin, deramciclane | |
| GABAA receptor agonists | ethanol, niacin, barbiturates, diazepam, clonazepam, lorazepam, temazepam, alprazolam and other benzodiazepines, zolpidem, eszopiclone, zaleplon and other nonbenzodiazepines, muscimol, phenibut | |
| GABAA receptor positive allosteric modulators | ||
| GABA receptor antagonists | thujone, bicuculline | |
| GABAA receptor negative allosteric modulators | ||
| Norepinephrine reuptake inhibitors | St John's wort, most non-SSRI antidepressants such as amoxapine, atomoxetine, bupropion, reboxetine, the tricyclics, methylphenidate, such as duloxetine, venlafaxine, cocaine, tramadol | |
| Norepinephrine releasing agents | ephedrine, PPA, pseudoephedrine, amphetamine, phenethylamine, methamphetamine | |
| Adrenergic agonists | clonidine, guanfacine, phenylephrine | |
| Adrenergic antagonists | carvedilol, metoprolol, mianserin, prazosin, propranolol, trazodone, yohimbine, olanzapine | |
| Serotonin receptor agonists | triptans (e.g. sumatriptan, eletriptan), Psychedelic drug (e.g. lysergic acid diethylamide, psilocybin, mescaline), ergolines (e.g. lisuride, bromocriptine) | |
| Serotonin reuptake inhibitors | most antidepressants including St John's wort, tricyclics such as imipramine, SSRIs (e.g. fluoxetine, sertraline, escitalopram), SNRIs (e.g. duloxetine, venlafaxine) | |
| Serotonin releasing agents | fenfluramine, MDMA (ecstasy), tryptamine | |
| Serotonin receptor antagonists | ritanserin, mirtazapine, mianserin, trazodone, cyproheptadine, memantine, atypical antipsychotics (e.g., risperidone, olanzapine, quetiapine) | |
| AMPA receptor positive allosteric modulators | aniracetam, CX717, piracetam | |
| AMPA receptor antagonists | kynurenic acid, NBQX, topiramate | |
| Cannabinoid receptor agonists | JWH-018 | |
| Cannabinoid receptor partial agonists | Anandamide, THC, cannabidiol, cannabinol | |
| Cannabinoid receptor inverse agonists | Rimonabant | |
| Anandamide reuptake inhibitors | LY 2183240, VDM 11, AM 404 | |
| FAAH enzyme inhibitors | MAFP, URB597, N-Arachidonylglycine | |
| NMDA receptor antagonists | ethanol, ketamine, deschloroketamine, 2-Fluorodeschloroketamine, Phencyclidine, DXM, Nitrous Oxide, memantine | |
| GHB receptor agonists | GHB, T-HCA | |
| Sigma receptor | Sigma-1 receptor agonists | cocaine, DMT, DXM, fluvoxamine, ibogaine, opipramol, phencyclidine, methamphetamine |
| Sigma-2 receptor agonists | methamphetamine | |
| Opioid receptor | μ-opioid receptor agonists | Narcotic opioids (e.g. codeine, morphine, hydrocodone, hydromorphone, oxycodone, oxymorphone, heroin, fentanyl) |
| μ-opioid receptor partial agonists | buprenorphine | |
| μ-opioid receptor inverse agonists | naloxone | |
| μ-opioid receptor antagonists | naltrexone | |
| κ-opioid receptor agonists | salvinorin A, butorphanol, nalbuphine, pentazocine, ibogaine | |
| κ-opioid receptor antagonists | buprenorphine | |
| Antihistamine | diphenhydramine, doxylamine, mirtazapine, mianserin, quetiapine, olanzapine, meclozine, most tricyclics | |
| H3 receptor antagonists | pitolisant | |
| Indirect histamine receptor agonists | modafinil | |
| Monoamine oxidase inhibitors (MAOIs) | phenelzine, iproniazid, tranylcypromine, selegiline, rasagiline, moclobemide, isocarboxazid, Linezolid, benmoxin, St John's wort, coffee, garlic | |
| Melatonin receptor agonists | agomelatine, melatonin, ramelteon, tasimelteon | |
| Imidazoline receptor agonists | apraclonidine, clonidine, moxonidine, rilmenidine | |
| Orexin receptor | Inderict Orexin receptor agonists | modafinil |
| Orexin receptor antagonists | SB-334,867, SB-408,124, TCS-OX2-29, suvorexant |
Globally, as of 2016, Alcoholism were the most prevalent of all substance use disorders (SUD) worldwide; cannabis dependence and opioid dependence were the next most prevalent SUDs.
Many professionals, self-help groups, and businesses specialize in drug rehabilitation, with varying degrees of success, and many parents attempt to influence the actions and choices of their children regarding psychoactives.
Common forms of rehabilitation include psychotherapy, support groups and pharmacotherapy, which uses psychoactive substances to reduce cravings and physiological Drug withdrawal symptoms while a user is going through detox. Methadone, itself an opioid and a psychoactive substance, is a common treatment for heroin addiction, as is another opioid, buprenorphine. Recent research on addiction has shown some promise in using psychedelic drug such as ibogaine to treat and even cure , although this has yet to become a widely accepted practice.
In the United States, the Food and Drug Administration (FDA) has authority over all drugs, including psychoactive drugs. The FDA regulates which psychoactive drugs are over the counter and which are only available with a prescription.History of the Food and Drug Administration. Retrieved at FDA's website on June 23, 2007. However, certain psychoactive drugs, like alcohol, tobacco, and drugs listed in the Single Convention on Narcotic Drugs are subject to criminal laws. The Controlled Substances Act of 1970 regulates the recreational drugs outlined in the Single Convention on Narcotic Drugs.United States Controlled Substances Act of 1970. Retrieved from the DEA's website on June 20, 2007. Alcohol is regulated by state governments, but the federal National Minimum Drinking Age Act penalizes states for not following a national drinking age. Title 23 of the United States Code, Highways. Retrieved on June 20, 2007. Tobacco is also regulated by all fifty state governments.Taxadmin.org. State Excise Tax Rates on Cigarettes. Retrieved on June 20, 2007. Most people accept such restrictions and prohibitions of certain drugs, especially the "hard" drugs, which are illegal in most countries.
RR Griffiths (1995). 078170166X, Lippincott Williams & Wilkins. 078170166XGriffith Edwards (2025). 031233883X, Thomas Dunne Books. 031233883X
In the medical context, psychoactive drugs as a treatment for illness is widespread and generally accepted. Little controversy exists concerning over the counter psychoactive medications in antiemetics and Cough medicine. Psychoactive drugs are commonly prescribed to patients with psychiatric disorders. However, certain critics believe that certain prescription psychoactives, such as antidepressants and stimulants, are overprescribed and threaten patients' judgement and autonomy.Dworkin, Ronald. Artificial Happiness. New York: Carroll & Graf, 2006. pp.2–6.
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