WELCOME TO STREET DRUG PHARMACOLOGY Randall Webber, M.P.H. ESSENTIAL ISSUES IN UNDERSTANDING STREET DRUG PHARMACOLOGY Psychoactivity Dependence Tolerance Toxicity Psychiatric Impairment Set and setting Substance misrepresentation/misidentification Psychoactivity = ability to affect mood, thinking and/or behavior CONTROLLED SUBSTANCES Schedules I-V Schedule I: High potential for abuse, tendency to produce dependence, no accepted medical use in US Schedules II-V: Potential for abuse, tendency to produce dependency, does have accepted medical application SCHEDULE I SUBSTANCES LSD Heroin Cannabis PCP SCHEDULE II SUBSTANCES Morphine Cocaine Short-acting barbiturates Amphetamines DESIGNATED PRODUCTS: State of Illinois Schedule II substances with a higher potential for abuse and addiction - amphetamines - cocaine short-acting barbs methadone morphine OxyCodone DRUG NAMES Chemical (7-chloro-1,3-dyhydro-1-methyl-5phenyl-2H-1,4-benzodiazepin-2-one Generic: diazepam Brand : Valium Street: No common street names for Valium DRUG MEASUREMENT metric: micro = 1/1,000,000. Microgram (mcg./m, also called a "gamma“) = 1/1,000,000 gram) Street nickel/nickel bag & dime/dime bag = $5 or $10 worth of drug eightball = 1/8 oz. (3.75 grams) DRUG MEASUREMENT Street sixteenth = either 1/16 oz (1.875 gm) or 1/16 gm (62.5 mg, about three lines of cocaine) line = an elongated pattern of powdered drug. Quantity = whatever the user decides. joint = a marijuana cigarette. DRUG FORMS plant/botanical matter (marijuana, opium poppies, khat, coca, peyote, psilocybin mushrooms, jimsom weed). liquids (alcohol, pure LSD, injectable pharmaceuticals) powders (cocaine hcl., heroin, PCP, methamphetamine) DRUG FORMS pills (tablets, capsules, caplets of either pharmaceutical or illicit origin) other forms (ex: "rocks" of crack cocaine). Potency, purity & misrepresentation of street drugs potency = strength, compared to some other drug of a similar type. purity = the major determinant of potency. The more pure the drug, the more potent. Street drugs are seldom pure, but are commonly misrepresented in one of three ways DRUG MISREPRESENTATION adulteration: (to adulterate = to "step on"/"hit"/"dance on" "cut" a drug). Substitution/misrepresentation-1: None of the alleged drug is present, but another drug/drugs is/are. substitution/misrepresentation -2: None of the alleged drug is present, and neither is any other drug or active substance. The Problem with Pill Identifications: New York City May 2000 Amphetamine Chicago May 2000 MDMA Portland Oct 2000 MDMA Tucson AZ July 2000 PMA TIME FACTORS Onset of action: How quickly does the drug produced it’s effect? Duration of action: How long does the drug’s effect last? Residual effects: After-effects, extended drug reaction, flashbacks The route of circulation. Blood flows in a circle according to this pattern: Capillaries vena cava Lungs Aorta - veins - right side of the heart - left side of the heart - body (capillaries, etc.) Route of Circulation METHOD OF ADMINISTRATION Ingestion (oral): slower onset/longer duration Insufflation (sniffing/snorting): faster onset/shorter duration Intravenous (I.V.) Injection: faster onset (seconds)/shortest duration Smoking: fastest onset/shortest duration METHOD OF ADMINISTRATION Ingestion (oral): slower onset/longer duration Insufflation (sniffing/snorting): faster onset/shorter duration Intravenous (I.V.) Injection: faster onset (seconds)/shortest duration Smoking: fastest onset/shortest duration METHOD OF ADMINISTRATION Ingestion (oral): slower onset/longer duration Insufflation (sniffing/snorting): faster onset/shorter duration Intravenous (I.V.) Injection: faster onset (seconds)/shortest duration Smoking: fastest onset/shortest duration THE “RUSH” OR “FLASH” A highly pleasurable sensation produced by the instantaneous effect of i. v. injection or smoking* * If entire dose administered at once METABOLISM AND EXCRETION The break-down of a drug into simpler substances The removal of the drug from the body TOLERANCE Homeostasis The human body’s natural tendency to move toward a state of equilibrium or constancy SET POINT RESPONSE TO DRUG USE TOLERANCE Need to increase the dose of a drug in order to obtain the desired effect Decreased effect of drug after repeated administration Dependent on prior dosage level Develops in hours (cocaine), days (LSD), or weeks TOLERANCE Effective dose (ED) Intoxicating dose (ID) Lethal dose (LD) TYPES OF TOLERANCE Enzyme induction Pharmacodynamic Behavioral Need to increase the dose of a drug in order to obtain the desired effect DEPENDENCE Addiction Physical dependence ADDICTION POTENTIAL What percentage of first-time users will enjoy the effect of the drug enough that they will seek it out again? If an individual uses the drug on a regular basis, how likely is it that s/he will become dependent on the substance? ADDICTION POTENTIAL After being introduced to the drug, do sub-human animals (e.g., monkeys, rats, mice) seek out opportunities to self-administer the substance? Do they do so to the exclusion of eating, consuming water and engaging in reproductive behavior? ADDICTION POTENTIAL CAN ALSO BE PREDICTED IN PART BY OBSERVING ANIMAL SELFADMINISTRATION ADDICTION POTENTIAL Ability to stimulate the brain’s reward circuits Ability to meet a individualized neurochemical need Physical dependency potential Intensity of withdrawal symptoms ADDICTION POTENTIAL Ability to stimulate the brain’s reward circuits Ability to meet a individualized neurochemical need Physical dependency potential Intensity of withdrawal symptoms Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 400 350 300 250 200 Dopamine 150 100 50 0 Morphine Nic Coke Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 160 140 120 100 80 Dopamine Levels 60 40 20 0 Food Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 250 200 150 Dopamine Levels 100 50 0 Food Sex Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 200 180 160 140 120 100 80 60 40 20 0 Dopamine Morphine Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 240 230 220 210 Dopamine 200 190 180 Morphine Nicotine Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 1200 1000 800 600 Dopamine 400 200 0 Morphine Nic Coke Amphet Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 160 140 120 100 80 Dopamine Levels 60 40 20 0 Food Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 250 200 150 Dopamine Levels 100 50 0 Food Sex Dopamine Levels in the Shell of the Nucleus Accumbens (% of baseline) 1200 1000 800 600 Dopamine Levels 400 200 0 Food Sex Meth NEUROTRANSMITTERS Naturally-occurring brain chemicals Many psychoactive drugs resemble neurotransmitters: NEUROTRANSMITTERS DRUG NEUROTRANSMITTER LSD Serotonin Methamphetamine Norepinepherine heroin Endorphins NEUROTRANSMITTERS DRUG NEUROTRANSMITTER THC Anandamide PCP Receptor site identified but not associated neurotransmitter ADDICTION Compulsive drug-taking Loss of control Continued use despite negative consequences Tolerance and physical dependence not required but may be part of the addiction picture TOXICITY Ability to produce physical damage to the human body Long-range = months, years Short-range = days, weeks Physical vs behavioral TOXICITY Physical Behavioral Acute Vs Long-Term PSYCHIATRIC IMPAIRMENT Ability of drug to produce negative changes in thinking, learning, perception, mood or behavior Acute vs chronic PSYCHIATRIC IMPAIRMENT Short-term Long-term Affective Disorders Thought Disorders CNS Stimulants Amphetamines/Similar-Acting Stimulants Cocaine Khat OTC Stimulants CNS Stimulants pulse, breathing, BP Alertness/Reversal of fatigue Reduction in appetite Dilated pupils Euphoria, elation, grandiosity, confidence Talkativeness Racing thoughts CNS Stimulants (Amphetamines) "speed", "white cross", "black beauties", "357's", "purple hearts“ amphetamine sulfate (Obetrol) dextroamphetamine (Dexedrine) methampetamine (Desoxsyn) ("meth", "crystal", “crank”, “go fast") Mixed amphetamine: (Adderall) Methamphetamine “Crystal” Methamphetamine “Ice” WHITE CROSS CRANK ICE CNS Stimulants (Non-Amphetamines) benzphetamine (Didrex) mazindol (Sanorex) methylphenidate (Ritalin) phenmetrazine (Preludin/Prelud-2) diethylpropion (Tenuate) phedimetrazine (Plegine/Bontril) phentermine (Fastin) Ritalin CNS Stimulants (Cocaine) Local anesthesia coca (Erythoxlum Coca) cocaine hydrochloride (hcl) ("coke", "toot", "nose/nose candy", "blow", "freeze", "snow", "girl", "white lady", "la mujer blanca") alkaloidal cocaine ("free base", "crack", "rock/ready rock", "basuco") ERYTHROXYLOM COCA FLOWER COCA FARMER MAKING COCAINE Cocaine Hcl COCAINE PARAPHERNALIA VIALS OF CRACK MORE CRACK Crack Packaged for Sale Crack Pipes CNS Stimulants (General Characteristics) Addiction potential high (Except OTCs) Physical dependence absent or mild Tolerance develops (for cocaine, tachyphylaxis) Immediate and long-range toxicity moderate to high (low for OTCs) CNS Stimulants (General Characteristics) High potential for acute psychiatric impairment (except OTCs) Paranoid psychosis, confusion, violence “Crash”: depression, anhedonia Moderate potential for persistent psychiatric impairment (Depression, anhedonia) CNS Stimulants (General Characteristics) Methamphetamine: Potential for acute and persistent cognitive impairment due to neurological damage. CNS Depressants Barbiturate Hypnotics Non-Barbiturate Hypnotics Minor Tranquilizers (benzodiazepines) Ethyl Alcohol (Ethylene) Opiates CNS Depressants (Barbiturates Hypnotics) ("barbs", "beans", "downers") secobarbital (Seconal) ("reds") pentobarbital (Nembutal) ("yellow jackets") apobarbital (Alurate) mephobarbital (Mebaral) phenobarbital (Luminal) CNS Depressants (Non-Barbiturate Hypnotics) triazalam (Halcion) ethchlorvynol (Placidyl) flurazepam (Dalmane) estazolapam (ProSom) profol injection (Diprivan) tempazepam (Restoril) quazepam (Doral) CNS Depressants (Non-Barbiturate Hypnotics) zolpidem tartrate (Ambien) Rohypnol (“roofies”) GHB/gamma hydroxy amino acid (Liquid G/Somatomax/G-riffic) CNS Depressants (Hypnotics) Addiction potential moderate to high Physical dependence possible. Severity of withdrawal = moderate to high/potentially life-threatening (A & B), Tolerance develops, but at a different rate for intoxicating Vs lethal dose Potential for immediate toxicity = moderate to high/very high mixed with alcohol CNS Depressants (Hypnotics) Potential for long-range toxicity = mild to moderate Potential for immediate and persistent psychiatric impairment low except for during withdrawal CNS Depressants Minor Tranquilizers (benzodiazepines) chlorazepam (Tranxene) chlordiazepoxide (Librium) clonazepam (Klonopin) diazepam (Valium) oxazepam (Serax) prazepam (Centrax) alprazolam (Xanax) lorazepam (Ativan) Xanax Valium Klonopin CNS Depressants Minor Tranquilizers (benzodiazepines) Addiction potential moderate to high Physical dependence possible. High dose/short duration Low/therapeutic dose/long duration Severity of withdrawal = low for low dose/moderate to high for high dose Tolerance develops Potential for immediate toxicity = moderate to high/high when mixed with alcohol CNS Depressants Minor Tranquilizers (benzodiazepines) Potential for immediate toxicity = moderate to high/high when mixed with alcohol Potential for long-range toxicity = mild Potential for immediate psychiatric impairment = low Potential for chronic psychiatric impairment = low CNS Depressants (Ethyl Alcohol) Beer/Wine coolers Wine Fortified wines Distilled spirits CNS Depressants (Ethyl Alcohol) Addiction potential moderate to high Physical dependence possible. Severity of withdrawal = moderate to high/seldom life-threatening Tolerance develops Potential for immediate toxicity = moderate to high Potential for long-range toxicity = high CNS Depressants (Ethyl Alcohol) Potential for immediate psychiatric impairment except for alcohol-related personality change/pathological intoxication/hallucinosis and psychiatric impairment during withdrawal Potential for chronic psychiatric/neurological = high CNS Depressants (Opiates) Organic/semisynthetic opiates opium codeine (Tylenol/Empirin w/codeine, some Rx cough syrups) hydrocodone (Vicodin) morphine sulfate (M.S.-Contin) diacetylmorphine (Heroin) ("junk", "smack", "boy", "chicle", "black tar", "china white") "Thou has the keys of Paradise, oh just, subtle and mighty opium" Thomas de Quincy Confessions of an English Opium-Eater Brown & White Heroin Black Tar Heroin (“El Chicle”) CNS Depressants (Opiates) Synthetic opiates oxycodone (Percodan/Percocet/OxyContin) oxymorphone (Numorphan) hydromorphone (Dilaudid) meperidine (Demerol) oxycodone (Percodan) dolophine (Methadone) levorphanol (Levo-Dromoran) fentanyl (Sublimaze) CNS Depressants (Opiates) Synthetic opiates diphenoxylate/atropine (Lomotil) pentazocine/pentazocine w/ naloxone (Talwin/Talwin-NX) "Karachi" (Chicago area): Drug composition varies. Usually includes an opiate (ex: Methadone) and at least one sedative (ex: diazepam, phenobarbital). OxyContin Methadone