Presentation on theme: "MIND ALTERING DRUGS MIND ALTERING… SYNTHETIC (DESIGNER) AND NATURALLY OCCURING…DRUGS Cardwell C. Nuckols, PhD"— Presentation transcript:
MIND ALTERING DRUGS MIND ALTERING… SYNTHETIC (DESIGNER) AND NATURALLY OCCURING…DRUGS Cardwell C. Nuckols, PhD email@example.com www.cnuckols.com (407) 758-1536
FDA CLASSIFICATION Schedule I Controlled Substances – Substances in this schedule have no currently accepted medical use in the United States, a lack of accepted safety for use under medical supervision, and a high potential for abuse. – Some examples of substances listed in Schedule I are: heroin, lysergic acid diethylamide (LSD), marijuana (cannabis), peyote, methaqualone, and 3,4-methylenedioxymethamphetamine ("Ecstasy").
FDA CLASSIFICATION Schedule II Controlled Substances – Substances in this schedule have a high potential for abuse which may lead to severe psychological or physical dependence. – Examples of Schedule II narcotics include: hydromorphone (Dilaudid®), methadone (Dolophine®), meperidine (Demerol®), oxycodone (OxyContin®, Percocet®), and fentanyl (Sublimaze®, Duragesic®). Other Schedule II narcotics include: morphine, opium, and codeine. – Examples of Schedule II stimulants include: amphetamine (Dexedrine®, Adderall®), methamphetamine (Desoxyn®), and methylphenidate (Ritalin®).
FDA CLASSIFICATION Schedule III Controlled Substances – Substances in this schedule have a potential for abuse less than substances in Schedules I or II and abuse may lead to moderate or low physical dependence or high psychological dependence. – Examples of Schedule III narcotics include: combination products containing less than 15 milligrams of hydrocodone per dosage unit (Vicodin®), products containing not more than 90 milligrams of codeine per dosage unit (Tylenol with Codeine®), and buprenorphine (Suboxone®). – Examples of Schedule III non-narcotics include: benzphetamine (Didrex®), phendimetrazine, ketamine, and anabolic steroids such as Depo®-Testosterone.
FDA CLASSIFICATION Schedule IV Controlled Substances – Substances in this schedule have a low potential for abuse relative to substances in Schedule III. – Examples of Schedule IV substances include: alprazolam (Xanax®), carisoprodol (Soma®), clonazepam (Klonopin®), clorazepate (Tranxene®), diazepam (Valium®), lorazepam (Ativan®), midazolam (Versed®), temazepam (Restoril®), and triazolam (Halcion®).
FDA CLASSIFICATION Schedule V Controlled Substances – Substances in this schedule have a low potential for abuse relative to substances listed in Schedule IV and consist primarily of preparations containing limited quantities of certain narcotics. – Examples of Schedule V substances include: cough preparations containing not more than 200 milligrams of codeine per 100 milliliters or per 100 grams (Robitussin AC®, Phenergan with Codeine®), ezogabine (Potiga, seizures) and pregabalin (Lyrica).
PHARMACOLOGICAL CATEGORIES STIMULANT DRUGS – “BATH SALTS” – KHAT (CATHINONE) CANNABINOIDS – “SPICE” AND A WIDE VARIETY OF CANNABINOID RECEPTOR AGONISTS DEPRESSANTS – GHB
PHARMACOLOGICAL CATEGORIES HALLUCINOGENS – 2C-E AND RELATED SYNTHETIC PSYCHEDELIC PHENETHYLAMINES THE NEUROSOUP GUIDE (http://www.neurosoup.com/neurosoup_trip_guide.h tm ) – MDMA 3,4-methylenedioxymethamphetamine – SALVIA DIVINORUM
STIMULANT DRUGS IN GENERAL Methamphetamine Cocaine Nicotine Caffeine Routes of Administration – Oral – IV – Pulmonary
STIMULANT TOXICITY Increased levels of Norepinephrine and Dopamine – Hyper-arousal – Pleasure – Paranoia Increased levels of Serotonin – Reduced hunger – Difficulty sleeping
STIMULANT CRASH Reduced levels of Norepinephrine and Dopamine – Dysphoria – Depression – Anhedonia Reduced levels of Serotonin – Mood swings – Sleep disturbances
ACUTE ABSTINENCE SYNDROME Reduced Noradrenergic activity 1 to 4 days – Low stimulant craving – High carbohydrate craving 4 to 10 days – Free floating anxiety – Euphoric dreams – Drug cravings
“BATH SALTS” AND RELATED STIMULANTS In the 1970s, a medicinal chemist named Richard A. Glennon was studying what it would take to convert a stimulant drug to a hallucinogen and vice versa in order to determine how these substances work in the brain. He knew that small modifications to a drug's molecular structure could result in major changes in its effects. By introducing an oxygen atom to the side chain of amphetamine, he created something called a beta-keto amphetamine. Beta-keto amphetamine was what we now call cathinone. Richard A. Glennon
INGREDIENTS – 3,4-METHYENEDIOXYPYROVALERONE (MDPV) MPPP MDPPP – 4-METHYLMETHCATHINONE (MEPHEDRONE OR 4-MMC) PHARMACOLOGY – MDPV IS A POWERFUL STIMULANT THAT FUNCTIONS AS DOPAMINE-NOREPINEPHRINE REUPTAKE INHIBITORS (NDRI)
“BATH SALTS” AND RELATED STIMULANTS Taking bath salts, it seemed, was similar to taking amphetamine and cocaine at the same time. Except for one thing: MDPV is as much as 10 times stronger than cocaine.
“BATH SALTS” AND RELATED STIMULANTS PHARMACOLOGY (CONTINUED) – 4-MMC IS CHEMICALLY SIMILAR TO AMPHETAMINE AND KHAT, MANUFACTURED IN CHINA AND COMES IN TABLETS OR POWDER THAT CAN BE SWALLOWED, SNORTED OR INJECTED – THEY HAVE STIMULATORY EFFECTS ON THE CENTRAL NERVOUS SYSTEM (CNS) AND CARDIOVASCULAR SYSTEM – MDPV AND 4-MMC PHYSICAL SYMPTOMS INCLUDE RAPID HEART RATE, INCREASED BLOOD PRESSURE, VASOCONSTRICTION AND SWEATING
“BATH SALTS” AND RELATED STIMULANTS PHARMACOLOGY (CONTINUED) – MDPV AND 4-MMC MENTAL SYMPTOMS INCLUDE EUPHORIA, INCREASED ALERTNESS, INCREASED WAKEFULNESS, ANXIETY, AGITATION, AND REDUCED DESIRE FOR FOOD AND SLEEP – MDPV IS REPORTEDLY FOUR TIMES AS STRONG A STIMULANT AS RITALIN AND IS SOMETIMES LABELED AS LEGAL COCAINE OR LEGAL AMPHETAMINE
“BATH SALTS” AND RELATED STIMULANTS TRADE NAMES-SOLD AS PLANT FOOD AN DFOR AROMATHERAPY ALSO – MDPV “RED DOVE”, “BLUE SILK”, “CLOUD NINE”, “ZOOM”, “BLOOM”, “VANILLA SKY”, “SCARFACE”, AND “STAR DUST” ALSO SOLD AS INSECT REPELLANT AND PLANT FOOD WITH NAMES LIKE “BONSAI GROW” – 4-MMC “MEPH”, “DRONE”, “MCAT” AND “MEOW, MEOW” DURATION OF EFFECTS – MDPV IS ROUGHLY 3-4 HOURS WITH AFTER EFFECTS LASTING 6-8 HOURS
KHAT NATIVE TO TROPICAL EAST AFRICA AND ARABIAN PENINSULA – PART OF SOCIAL CULTURE IN SOME AREAS FRESH LEAVES/TOPS CHEWED OR CONSUMED AS TEA STIMULANT AND EUPHORIANT CATHINONE (SCHEDULE 1) STRUCTURALLY SIMILAR TO AMPHETAMINE
“SPICE” AND OTHER SYNTHETIC CANNABINOIDS INGREDIENTS – A DIVERSE GROUP OF CANNABINOID RECEPTOR AGONISTS FALLING INTO SEVEN MAJOR STRUCTURAL GROUPS NAPHTOYLINDOLES NAPTHYLMETHYLINDOLES NAPTHOYLPYRROLES NAPTHYLMETHYLINDENES PHENYLACETYLINDOLES CYCLOHEXYLPHENOLS CLASSICAL CANNABINOIDS (DIBENZOPYRAN)
CANNABINOID MODULATORS Work on CB-1 and CB-2 receptor sites Rimonabant (Acomplia) – Blocks CB-1 receptors – Suppresses appetite – Favorable changes in blood fats, cholesterol and glucose tolerance – High drop out rate
RIMONABANT Clinical Trials – Test subjects No psychiatric history No family history – High Drop-out rate – Psychiatric Side-Effects Anxiety Depression BRAINWORK (May-June 2006)
CANNABINOID MODULATORS Anxiety and depression involve the endocannabinoid system – Rimonabant blocks receptors May see increase in psychiatric symptoms – If boost endocannabinoid system get antianxiety and antidepressant effects
SYNTHETIC CANNABINOIDS- COMMERCIAL Rimonabant (also known as SR141716; trade names Acomplia, Bethin, Monaslim, Remonabent, Riobant, Slimona, Rimoslim, Zimulti, and Riomont) is an anorectic antiobesity drug. It is an inverse agonist for the cannabinoid receptor CB1. Its main effect is reduction in appetite. Rimonabant blocks the psychoactive and some of the cardiovascular effects of Δ9- tetrahydrocannabinol (THC) in humans without affecting the pharmacokinetics.
SYNTHETIC CANNABINOIDS- COMMERCIAL Dronabinol (Marinol, Delta-9- tetrahydrocannabinol, delta-9-THC) is synthetic THC. It is used to treat nausea and vomiting caused by chemotherapy in people who have already taken other medications to treat this type of nausea and vomiting without good results. Dronabinol is also used to treat loss of appetite and weight loss in people who have acquired immunodeficiency syndrome (AIDS). Dronabinol is in a class of medications called cannabinoids. It works by affecting the area of the brain that controls nausea, vomiting, and appetite.
SYNTHETIC CANNABINOIDS- COMMERCIAL Nabilone is a synthetic cannabinoid with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It is a synthetic cannabinoid, which mimics the main ingredient of cannabis (THC). Chemically, nabilone is similar to the active ingredient found in naturally occurring Cannabis sativa L. In Canada, the United States, the United Kingdom and Mexico, nabilone is marketed as Cesamet. It was approved in 1985 by the U.S. Food and Drug Administration (FDA) for treatment of chemotherapy-induced nausea and vomiting that has not responded to conventional antiemetics. Though it was approved by the FDA in 1985, the drug only began marketing in the United States in 2006. It is also approved for use in treatment of anorexia and weight loss in patients with AIDS. Although it doesn't have the official indication (except in Mexico), nabilone is widely used as an adjunct therapy for chronic pain management. Numerous trials and case studies have demonstrated various benefits for condition such as fibromyalgia and multiple sclerosis.
SYNTHETIC CANNABINOIDS- COMMERCIAL Sativex is an oromucosal (mouth) spray developed by the UK company GW Pharmaceuticals for multiple sclerosis patients, who can use it to alleviate neuropathic pain, spasticity, overactive bladder, and other symptoms. Sativex is also being prescribed to alleviate pain due to cancer and has been researched in various models of peripheral and central neuropathic pain. Sativex is distinct from all other pharmaceutically produced cannabinoids currently available because it is derived from botanical material, rather than a solely synthetic process. Sativex is a pharmaceutical product standardized in composition, formulation, and dose. Its principal active cannabinoid components are the cannabinoids: tetrahydrocannabinol (THC) and cannabidiol (CBD). The product is formulated as an oromucosal spray which is administered by spraying into the mouth. Each spray of Sativex delivers a fixed dose of 2.7mg THC and 2.5mg CBD.
“SPICE” AND OTHER SYNTHETIC CANNABINOIDS PHARMACOLOGY – CANNABINOID RECEPTOR AGONISTS MIMIC THE EFFECTS OF THC AND ANADAMIDE BY INTERACTING WITH THE CB1 RECEPTOR IN THE BRAIN – SOME OF THESE SYNTHETICS HAVE A HIGHER AFFINITY FOR THE RECEPTOR THAN CANNABIS THC AND MAY BE PARTICULARLY LONG ACTING – OFTEN LARGE AMOUNTS OF TOCOPHEROL (VITAMIN E) ADDED TO MASK ANALYSIS
“SPICE” AND OTHER SYNTHETIC CANNABINOIDS PHARMACOLOGY (CONTINUED) – SMOKING MIXTURES ARE USUALLY SOLD IN METAL-FOIL SACHETS TYPICALLY CONTAINING THREE GRAMS OF DRIED VEGETABLE MATTER TO WHICH ONE OR MORE OF THE CANNABINOIDS HAVE BEEN ADDED TRADE NAMES – “SPICE GOLD”, “SPICE SILVER”, “YUCATAN FIRE”, “CHILL X”, “SENSE” AND MANY OTHERS
GHB (CNS DEPRESSANT) γ-Hydroxybutyric acid (GHB), also known as 4- hydroxybutanoic acid Naturally occurring substance found in the human Central nervous System (CNS) General anesthetic, to treat conditions such as insomnia, clinical depression, narcolepsy, and alcoholism, and to improve athletic performance (elevates Human Growth Hormone). It is also used as an intoxicant or as a “date rape drug”. Has a salty taste like baking soda
GHB Georgia Home Boy", "Juice", “Grievous Bodily Harm”, "Liquid Ecstasy", "Mils", "G", "Liquid X", and "Liquid G", as well as "Fantasy" Its effects have been described anecdotally as comparable with alcohol and ecstasy use, such as euphoria, disinhibition, enhanced sensuality and empathogenic states
GHB TOXICITY LOW DOSE (.5-1.5 GRAMS) EQUAL TO 1-3 ALCOHOLIC DRINKS) – Reduces anxiety – Acts as a depressant – Slurred speech – Energetic – Playful – Reduction in motor skills – Mild dizziness
GHB TOXICITY MEDIUM DOSE (1-2.5 GRAMS) – Affectionate and sensual response – Increased erectile capacity – Heightened orgasm – Tactile sensitivity – Nausea and grogginess – Increased appreciation for music, dancing and/or talking
GHBTOXICITY GHB TOXICITY High dose (2.5 grams +) – Euphoria – Increased grogginess and nausea/vomiting Overdose (greater than 2 grams) – Nausea and vomiting – Like other CNS depressant drugs( alcohol, heroin) – Seizure activity – Coma NOTE: Dose is hard to titrate so might quickly move from medium to overdose
GHB ACUTE ABSTINENCE SYNDROME Initially feel drowsy, groggy and sleepy as the “morning after” effects The AAS includes… – Insomnia – Anxiety and tremor – Resolved in 3-12 days – Prolonged and difficult
HALLUCINOGENS 2C-E NICKNAMED “EUROPA” SYNTHESIZED IN 1970’S-1980’S PSYCHEDELIC PHENETHYLAMINE 4-ETHYL-2,5 DIMETHOXYPHENETHYLAMINE TAKEN ORALLY POWERFUL HALLUCINOGENIC EFFECTS HIGH LASTS 4-9 HOURS SOLD THROUGH EUROPEAN SOURCES
2C-E NICKNAMED “EUROPA” SYNTHESIZED BY ALEXANDER SHULGIN POPULARIZED MDMA (ECSTASY) PIHKAL BOOK (1991) – PHENETHYLAMINES I HAVE KNOW AND LOVED 2C-I ANOTHER PHENETHYLAMINE IS AVAILABLE 2C-E IS SCHEDULE I
MDMA 3,4 methylenedioxy-methamphetamine Ecstasy, XTC Synthetic psychoactive drug similar to both the stimulant drug methamphetamine and the hallucinogen mescaline Introduced in the 1970’s as an aid in psychotherapy Initially popular with the adolescent and young adult population but now has a broad audience “Raves”
MDMA-SUBJECTIVE EXPERIENCE Increased energy Euphoria Emotional warmth Empathy towards others Distortions in sensory and time perception Usually taken orally as a tablet or capsule Some gay and bisexual men use MDMA mixed with cocaine, GHB, methamphetamine, ketamine and sildenafil (Viagra)
MDMA PHARMACOLOGY Increases the activity of… – Serotonin – Norepinephrine – Dopamine Serotonin triggers the release of oxytocin and vasopressin – Love – Trust – Sexual arousal
There are at least two sides to the neurotransmitter story Sex Appetite Aggression Concentration Interest Motivation Depressed Mood Anxiety Irritability Thought process Norepinephrine (NE) Both serotonin and norepinephrine mediate a broad spectrum of depressive symptoms Serotonin (5-HT) Vague Aches and pain Functional domains of Serotonin and Norepinephrine 1-4
MDMA TOXICITY Dehydration Hyperthermia Increased ANS functioning – Seizures Heart and kidney failure “Stacking and combining” Serotonin damage
MDMA WITHDRAWAL Acute Abstinence Syndrome – Pale – Dysphoric – Depressed – Confusion and anxiety – Somnolent – Paranoia(can last for weeks)
MDMA MEDICAL MANAGEMENT Benzodiazepines(Ativan) – Sedation, muscle relaxation and seizure management Benzodiazepines(Valium) – Depresses the CNS Anticonvulsants(Dilantin) Barbiturates(Phenobarbital) – Anticonvulsant when Benzo and Dilantin fail
MDMA MEDICAL MANAGEMENT Antihypertensives (Regitine) – Lower blood pressure GI Decontaminate – Activated charcoal Absorbs MDMA and limits absorption
SALVIA DIVINORUM DIVINER’S SAGE INDUCES DISSOCIATIVE STATES AND PRODUCER OF “VISIONS” AND OTHER HALLUCINATORY EXPERIENCES SIERRA MAZATECA OF OAXACA, MEXICO USED BY MAZATEC SHAMANS FOR RELIGIOUS AND SPIRITUAL HEALING SESSIONS
SALVIA DIVINORUM PHARAMCOLOGY ACTIVE INGREDIENT SALVINORUM A IS A POTENT K-OPIOID AND D2 RECEPTOR AGONIST USUALLY SMOKED OFTEN WITH WATER PIPE POTENT NATURALLY OCCURRING HALLUCINOGEN ALTHOUGHT DOES NOT SEEM TO WORK THROUGH THE SEROTONIN SYSTEM
SALVIA DIVINORUM-SUBJECTIVE POSITIVE – SHORT DURATION ESPECIALLY WHEN SMOKED – RADICAL PERSPECTIVE SHIFTING – INCREASE IN SENSUAL APPRECIATION – DREAMLIKE EXPERIENCES – INSIGHT INTO SELF NEUTRAL – CHANGE IN BODY TEMPERATURE, FLUSHING – SENSATION OF ENTERING OR PERCEIVING OTHER DIMENSIONS
SALVIA DIVINORUM-SUBJECTIVE NEUTRAL (CONTINUED) – FEELING OF PRESENCE OR ENTITY CONTACT – DISSOCIATION AT HIGHER DOSES NEGATIVE – OVERLY-INTENSE EXPERIENCES – FEAR, TERROR AN DPANIC – MILD TO MODERATE HEADACHE – COORDINATION PROBLEMS
KRATOM (OPIOIDS) LEAF FROM LARGE TREES NATIVE TO SOUTHEAST ASIA MITRAGYNA SPECIOSA FOUND IN – MALAYSIA – THAILAND – INDONESIA ITHANG, BIAK BIAK, KETUM, KAKUAM, THOM
Journal of Psychoactive Drugs Vol. 20 (No 4) 1988...leaves of Mitragyna speciosa, tree of Malaysia and Thailand, used as opium substitute, methods included tea, smoking and chewing. Found to suppress opiate withdrawal syndrome. Chronic users said to have darkened skin. Said to have both stimulating and depressant qualities as if chewing coca leaves and smoking opium simultaneously. Large doses lead to stupor. Withdrawal said to be considerably milder than that with the opiates. Mitragynine is thus a drug with a highly unusual but never the less well-documented history of being described as both a stimulant and depressant while at the same time possessing the chemical structure one might expect of a psychedelic. The Thai narcotic book described Kratom as weaker than morphine and less harmful than cocaine.
KRATOM PHARMACOLOGY MITRAGYNINE – 7-HYDROXYMITRAGYNINE (MAIN ACTIVE INGREDIENT) – SIMILAR IN STRUCTURE TO PSYHEDELICS BUT HAS NO REAL PSYCHEDELIC EFFECTS – INTERACTS WITH OPIOID RECEPTORS LOW DOSE-ATTACHES TO DELTA OPIOID RECEPTOR HIGHER DOSES-ATTACHES TO MU OPIOID RECEPTOR
KRATOM PHARMACOLOGY 7-HYDROXYMITRAGYNINE – POTENT OPIATE AGONIST – NATURAL CEILING EFFECT LIMITS EUPHORIA LIMITS RESPIRATORY DEPRESSION LIMITS OD POTENTIAL – NO KNOWN FATAL OD
KRATOM PHARMACOLOGY USED IN TREATMENT OF OPIATE DEPENDENCE – 1897, EUROPEANS BELIEVE LEAVES OF THE PLAN TO BE A CURE FOR OPIATE DEPENDENCE – CURRENTLY, USED FOR METHADONE DETOXIFICATION IN SOME COUNTRIES (EX. NEW ZEALAND) AND IN THAILAND TO DETOX AND MANAGE HEROIN ACUTE ABSTINENCE SYNDROME (AAS) – TO PREVENT ONSET OF AAS SYMPTOMS
KRATOM PHARMACOLOGY SEEMS TO BE… – A STIMULANT AT LOWER DOSES (MITRAGYNINE) – A SEDATIVE AT HIGHER DOSES (7- HYDROXYMITRAGYNINE) ONSET OF ACTION: 5-10 MINUTES DURATION OF ACTION: SEVERAL HOURS
KRATOM PHARMACOLOGY SHORT TERM EFFECTS: – DRY MOUTH – INCREASED OR REDUCED URINATION – LOSS OF APPETITE – NAUSEA/ VOMITING INTERMEDIATE EFFECTS – ANOREXIA WITH WEIGHT LOSS – INSOMNIA – DEPENDENCE
KRATOM PHARMACOLOGY LONG TERM HIGH DOSE EFFECTS – NERVOUSNESS – SLEEPLESSNESS – LOSS OF LIBIDO – CONSTIPATION – DARKENING OF SKIN
KRATOM PHARMACOLOGY ACUTE ABSTINENCE SYNDROME – SIMILAR TO OPIOIDS AROUSED SYMPATHETIC NERVOUS SYSTEM – INCREASED HEART RATE – INCREASED BLOOD PRESSURE – DILATED PUPILS – TREMORS CASE OF BODY FLU – MUSCLE ACHES – NAUSEA/VOMITING
KROKODIL RAMPANT ABUSE IN RUSSIA MIXTURE OF CODEINE AND GASOLINE, PAINT THINNER, IODINE, HYDROCHLORIC ACID AND RED PHOSPHOROUS DESOMORPHINE-SYNTHESIZED IN US IN 1932 HEROIN-LIKE EFFECTS (8-10 stronger than morphine) MUCH CHEAPER TO OBTAIN-CODEINE SOLD OTC IN RUSSIA
KROKODIL PHARMACOLOGY Half-life short so have to inject every 90 -120 minutes Short half-life means Acute Abstinence Syndrome comes on very quickly Pharmacology similar to other opioids with typical subjective effects and acute abstinence syndrome
KROKODIL Name comes from the appearance of the skin of chronic users and the derivative of codeine (chlorocodide) used in production Severe tissue damage, phlebitis and gangrene The amount of tissue damage is so severe the life expectancy of a chronic addict is only 3-4 years
“JENKEM” (INHALANT) FERMENTATION OF HUMAN WASTE FECES AND URINE STORED IN TIGHT CONTAINER FOR SEVERAL DAYS REACTION PRODUCES METHANE GAS “HUFFED” BY USERS TO CREATE ANOXIA