Dextroamphetamine (Dexedrine) and methylphenidate (Ritalin) are used for the treatment of narcolepsy and for attention-deficit disorders in children. Methamphetamine ("crank," "speed"), 3,4-methylenedioxymethamphetamine (MDMA; "ecstasy"), paramethoxyamphetamine (PMA), and several other amphetamine derivatives, as well as a number of prescription drugs, are used as illicit stimulants and hallucinogens (see also "Lysergic Acid Diethylamide [LSD] and Other Hallucinogens"). "Ice" is a high purity, smokable crystalline form of methamphetamine. Methamphetamine precursors such as pseudoephedrine, ephedrine, and other over-the-counter decongestants are discussed on Pseudoephedrine, Phenylephrine, and other Decongestants. Several amphetamine-related drugs (benzphetamine, diethylpropion, phendimetrazine, phenmetrazine, and phentermine) are marketed as prescription anorectic medications for use in weight reduction (Table II–1). Fenfluramine and dexfenfluramine were marketed as anorectic medications but were withdrawn from the market in 1997 because of concerns about cardiopulmonary toxicity with long-term use.
++ Table Graphic Jump Location TABLE II–1.AMPHETAMINEMINE-LIKE PRESCRIPTION DRUGSa ||Download (.pdf) TABLE II–1. AMPHETAMINEMINE-LIKE PRESCRIPTION DRUGSa
|Drug ||Clinical Indications ||Typical Adult Dose (mg) ||Half-life (h)b |
|Atomoxetinec ||Hyperactivity ||40–120 ||3–4 |
|Benzphetamine ||Anorectant ||25–50 ||6–12 |
|Dexfenfluramine (withdrawn from US market in 1997) ||Anorectant ||15 ||17–20 |
|Dextroamphetamine ||Narcolepsy, hyperactivity (children) ||5–15 ||10–12 |
|Diethylpropion ||Anorectant ||25, 75 (sustained-release) ||2.5–6 |
|Fenfluramine (withdrawn from US market in 1997) ||Anorectant ||20–40 ||10–30 |
|Mazindol ||Anorectant ||1–2 ||10 |
|Methamphetamine ||Narcolepsy, hyperactivity (children) ||5–15 ||4–15 |
|Methylphenidate ||Hyperactivity (children) ||5–20 ||2–7 |
|Modafinilc ||Narcolepsy, shift work sleepdisorder, sleep apnea ||100–600 ||15 |
|Pemoline ||Narcolepsy, hyperactivity (children) ||18.7–75 ||9–14 |
|Phendimetrazine ||Anorectant ||35, 105 (sustained-release) ||5–12.5 |
|Phenmetrazine ||Anorectant ||25, 75 (sustained-release) ||8 |
|Phentermine ||Anorectant ||8, 30 (sustained release) ||7–24 |
Cathinone (found in the shrub Catha edulis, or khat), methcathinone, and mephedrone (4-methylmethcathinone) are chemically related drugs with amphetamine-like effects. Newer synthetic analogs, such as 3,4-methylenedioxypyrovalerone and various derivatives of methcathinone, are becoming popular drugs of abuse, often sold on the Internet as "bath salts" with names such as "Ivory Wave," "Bounce," "Bubbles," "Mad Cow," and "Meow Meow." Piperazine-like compounds such as 1-benzyl-piperazine (BZP), 1-(4-methoxyphenyl)-piperazine (pMeOPP), 1-(3-chlorophenyl)-piperazine (mCPP), and 1-(3-trifluoromethylphenyl)-piperazine (TFMPP) are also designer drugs of abuse with stimulant effects.
Atomoxetine is a specific norepinephrine reuptake inhibitor approved as a nonstimulant alternative for the treatment of attention-deficit/hyperactivity disorder (ADHD). Modafinil is a nonamphetamine stimulant used in the treatment of narcolepsy, sleep disorders associated with shift work, and sleep apnea.
MECHANISM OF TOXICITY
Amphetamine and related drugs activate the sympathetic nervous system via CNS stimulation, peripheral release of catecholamines, inhibition of neuronal reuptake of catecholamines, and inhibition of monoamine oxidase. Amphetamines, particularly MDMA, PMA, fenfluramine, and dexfenfluramine, also cause serotonin release and block neuronal serotonin uptake. The various drugs in this group have different profiles of catecholamine and serotonin action, resulting in different levels of CNS and peripheral stimulation.
Modafinil is a nonamphetamine stimulant. ...