Stimulants and Depressants

Stimulants

Substances that keep a person going mentally and physically

Cocaine and amphetamine

Restricted stimulants

Caffeine and nicotine

Readily available stimulants

Coca paste

One form of cocaine, can be mixed with tobacco and smoked

Cocaine hydrochloride

Most common form of pure cocaine, stable water-soluble salt

Freebase

Prepared as a chemical base, can be heated and the vapors inhaled

Crack or rock

Lumps of dried, smokable cocaine, prepared by mixing cocaine with water and baking soda

Cocaine use

Began to increase again at the end of the 1960s

Crack

An inexpensive form of smokable cocaine, associated with greater abuse potential than snorted cocaine

Fair Sentencing Act of 2010

Reduced the disparity between crack and powder cocaine from 100:1 to 18:1 (weight ratio), eliminated the 5-year mandatory minimum sentence for crack, and reduced the prison population

Mechanism of Action

Cocaine blocks reuptake of dopamine, serotonin, and norepinephrine

Cocaine Administration

Can be chewed, snorted, injected, or smoked

Cocaine Elimination

Metabolized by enzymes in the blood and liver, has a half-life of about one hour

Local anesthetic properties of cocaine

Discovered in 1860, still used for surgery in the nasal, laryngeal, and esophageal regions

Acute cocaine toxicity

Causes profound CNS stimulation, difficult to estimate the size of a lethal dose, and can lead to rare, severe, and unpredictable reactions

Chronic Toxicity from High-Dose Use

Includes paranoid psychosis, damage to the heart muscle, and dependence

Cocaine use during pregnancy

Increases the risk of miscarriage and torn placenta, long-term effects still under study

Supply of Illicit Cocaine

Readily available in all major U.S. cities, street cocaine averages about 50-75 percent pure, and most comes from Peru, Bolivia, and Columbia

Positive Reinforcement

Abused drugs activate positive reinforcement mechanisms in the brain, most increase dopamine levels within the nucleus accumbens

Negative Reinforcement

Strengthens behaviors that avoid or escape aversive stimuli, may play a role in maintaining drug taking or acquiring a drug addiction

Amphetamines

New synthesized chemical similar to ephedrine, used medically for asthma, narcolepsy, hyperactivity in children, and as an appetite suppressant

Methamphetamine

Similar effects to those with amphetamine and cocaine, long-term smoking can lead to psychotic-like behavior and may result in long-term damage to dopamine and serotonin neurons

Amphetamine Absorption and Elimination

Peak effects occur 1.5 hours after oral ingestion, 5-20 minutes after intranasal administration, and 5-10 minutes following intravenous injection or smoking, with a half-life of 5-12 hours

Methylphenidate (Ritalin)

CNS stimulant with a half-life of 2-4 hours, increases dopamine release and blocks dopamine transporter, may lead to tolerance and dependence

Methylphenidate ER (Concerta)

CNS stimulant that gradually releases over 10 hours, benefits include decreased dosing and fluctuations in effects

Amphetamine (Dexedrine)

CNS stimulant, increases dopamine release and blocks dopamine transporter

Sudden death

A concern associated with ADHD meds, especially with Strattera

Acute Toxicity

Causes increases in feelings of power, suspicion, paranoia, potential risk of violent behavior, and very high doses may destroy catecholamine neurons

Chronic Toxicity from High-Dose Use

Includes paranoid psychosis, with possible reasons being heavy methamphetamine users having schizoid personalities and caused by sleep deprivation

Dependence Potential of Amphetamines

Often no obvious withdrawal symptoms, capable of producing psychological and physical dependence

Cathinones

Stimulants found in khat, widely used throughout East Africa and the Arabian Peninsula

Synthetic Cathinones

Known as 'bath salts,' have nothing to do with products used during bathing, dependence possible

Depressants

Drugs that slow activity in the central nervous system, include prescription drugs for anxiety and insomnia, and alcohol

Inhalants

Volatile solvents and other compounds used for intoxicating purposes, have depressant effects similar to sedative-hypnotics

Barbiturates

Drugs grouped based on the time of onset and duration of activity, used for anxiety relief and to induce sleep

Sodium Pentathol

Ultra-short acting barbiturate, used as an anesthetic for brief surgical procedures and to make people relaxed and talkative

Methaqualone

Introduced in the United States in 1965, quickly became widely misused and abused, put on Schedule I in 1985

Benzodiazepines

Drugs that enhance the normally inhibitory effects of GABA, used as anxiolytics, sedatives, and muscle relaxants

Benzodiazepines: Rohypnol

Produces profound intoxication when mixed with alcohol, used as a 'date-rape' drug

GABA Involvement

Implicated in anxiolytic and anxiogenic responses, important for mediating emotional responses

Benzodiazepine Effects

Relieves fear and anxiety, muscle relaxant, sedative, reduces epileptic seizures, and has reinforcing effects

Common Side Effects of Benzos

Include amnesia, delirium, depression, incoordination, rage reactions, and sedation

Antidepressants: Major Types

Include monoamine oxidase inhibitors, tricyclic antidepressants, selective serotonin reuptake inhibitors, and atypicals

Electroconvulsive Therapy (ECT)

Most effective treatment for relieving severe depression, works very rapidly, best treatment choice in cases with a risk of suicide

Bipolar Disorder: Mood Stabilizers

Lithium normalizes mood in bipolar patients, preventing both mania and depressed mood swings, often prescribed with valproic acid