Classes/Types of Depressants b b 1. Anesthetics (ex. ether, nitrous oxide) b b 2. Barbiturates b b 3. Benzodiazepines (anxiolytics - ex. ? ) b b 4. Buspar b b Many labels have been used to describe them, which can be confusing: -tranquilizers-anti-anxiety pills -sleeping pills -sedatives
Depressants b Mechanism of action: GABA: acts mainly on inhibitory receptorsGABA: acts mainly on inhibitory receptors –taking off the brakes – e.g. GHB (gamma hydroxy butyrate) Separate receptors identified for barbiturates and benzosSeparate receptors identified for barbiturates and benzos
Etherdome
History / Development of Depressants b b Nitrous oxide (1776) (laughing gas) development of ether (MGH-etherdome) flammable liquid which vaporizes at room temperature b b Chloral hydrate, bromides, paraldehyde b b Barbiturates came next in 1860s developed in Germany drug names end with ‘-al’ ( phenobarbital) On street, named for color of pills – –“blues”, “reds”
Barbiturates b USES: some used as anesthetics if they work quickly and then wear offsome used as anesthetics if they work quickly and then wear off others used to prevent seizures because their sedating effects lasted longerothers used to prevent seizures because their sedating effects lasted longer often used as sleeping pills and anxiolyticsoften used as sleeping pills and anxiolytics
Barbiturate Use Total %.1%.4%1.8% %.2%.3%1.7% For example, Nembutal®, Pentobarbital, Seconal®, Secobarbital, or Butalbital. Source: SAMHSA, Office of Applied Studies, National Survey on Drug Use and Health.
BARBITURATE USE declined due to their unwanted effects: -drunken euphoria and loss of behavioral and emotional control - respiratory depression - tolerance and addiction develop rapidly - lethal dose is low and nearer to drug’s ED compared with other drugs, so potential for overdose is high withdrawal SX similar to alcohol: – –rebound insomnia – –rebound in REM sleep > vivid dreams/nightmares
Quaaludes (Methaqualone) came next in the 50s and 60s and were developed as alternatives to barbs for sleep/anxiety disorders they became a street drug; not much different than barbiturates now a schedule I drug no longer produced for medical reasons
Depressants (con’t) b b Benzodiazepines classic anti-anxiety drugs synthesized initially in 1950s more potent in 1960s with the advent of Valium similar to barbs but less dangerous in that: – –tolerance develops more slowly, and to primarily the sedative not anxiolytic effects – –need higher doses for tolerance to occur
Benzodiazepine Use Total %.14%.30%.22% %.14%.29%.25% Includes Klonopin® or clonazepam, Xanax®, or alprazolam, Ativan®, or lorazepam, Valium® or diazepam, Librium®, Limbitrol®, Rohypnol®, Serax®, and Tranxene®.
Depressants b b Benzodiazepines Withdrawal symptoms: increased anxiety, insomnia, tremors, sweating Dangers: cross tolerance and potentiation b b what are the clinical implications of treating anxiety with drugs? b b difficult to estimate non-medical misuse or abuse of sedatives and tranquilizers
The case of Rohypnol (flunitrazepam) b b a.k.a. roofies, rib, circles, wolfies, rope, ropies, ruffies, roach-2, “roaches” after drug company Hoffman-La Roche a Benzodiazepine used in the short-term treatment of insomnia and as a pre- anesthetic medication similar to valium in effect but 10 times stronger effects begin within 30 minutes, may last for 8 hours or more
Rohypnol made in Europe and Latin America and sold by prescription there, not in U.S. so it is usually smuggled via mail into country, or comes across Mexican border b b distribution and abuse especially in southwest & south (Texas & Florida most) b b low cost < $5 per tab b b popularity among young people; “Said to be south Florida’s fastest growing drug problem”
Rohypnol b b 2 COMMON MISPERCEPTIONS: the drug is safe and “pure” because it comes in pre-sealed bubble packages can’t be detected through urinalysis
Adverse Effects of Rohypnol b b memory impairment, drowsiness, dizziness, confusion; can induce excitability or aggressiveness in some users b b can cause dependence: tolerance may develop; withdrawal symptoms include - headaches, anxiety, muscle pain, confusion, restlessness, numbness, tingling of extremities, convulsions and cardiac problems
Rohypnol b b used in date rape situations….WHY? it’s odorless, (initially) colorless, tasteless and produces drunkenness, stupor, and blackout Federal law, since 1996, dictates a 20-year sentence for use of this drug in connection with sexual assault or other violence b b used to augment an alcohol high without elevating BAL b b used as a “parachute” or remedy for depression that follows a stimulant high
Inhalants b USES: varied as products “huffed” include gasoline, glues, solvents, paint.. b Mostly young kids, adolescents b highly destructive to brain with OD potential