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MIND ALTERING … SYNTHETIC (DESIGNER) AND NATURALLY OCCURING… DRUGS

MIND ALTERING … SYNTHETIC (DESIGNER) AND NATURALLY OCCURING… DRUGS. Cardwell C. Nuckols, PhD cnuckols@elitecorp1.com www.cnuckols.com (407) 758-1536. FDA CLASSIFICATION. Schedule I Controlled Substances

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MIND ALTERING … SYNTHETIC (DESIGNER) AND NATURALLY OCCURING… DRUGS

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  1. MIND ALTERING…SYNTHETIC (DESIGNER) AND NATURALLY OCCURING…DRUGS Cardwell C. Nuckols, PhD cnuckols@elitecorp1.com www.cnuckols.com (407) 758-1536

  2. 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").

  3. 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®).

  4. 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.

  5. 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®).

  6. 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) .

  7. PHARMACOLOGICAL CATEGORIES • STIMULANT DRUGS • “BATH SALTS” • KHAT (CATHINONE) • CANNABINOIDS • “SPICE” AND A WIDE VARIETY OF CANNABINOID RECEPTOR AGONISTS • DEPRESSANTS • GHB

  8. PHARMACOLOGICAL CATEGORIES • HALLUCINOGENS • 2C-E AND RELATED SYNTHETIC PSYCHEDELIC PHENETHYLAMINES • THE NEUROSOUP GUIDE (http://www.neurosoup.com/neurosoup_trip_guide.htm ) • MDMA • 3,4-methylenedioxymethamphetamine • SALVIA DIVINORUM

  9. PHARMACOLOGICAL CATEGORIES • OPIOIDS • KRATOM (7-HYDROXYMITRAGYNINE) • KROKODIL (DESOMORPHINE) • INHALANTS • JENKEM

  10. STIMULANT DRUGS IN GENERAL • Methamphetamine • Cocaine • Nicotine • Caffeine • Routes of Administration • Oral • IV • Pulmonary

  11. STIMULANT TOXICITY • Increased levels of Norepinephrine and Dopamine • Hyper-arousal • Pleasure • Paranoia • Increased levels of Serotonin • Reduced hunger • Difficulty sleeping

  12. STIMULANT CRASH • Reduced levels of Norepinephrine and Dopamine • Dysphoria • Depression • Anhedonia • Reduced levels of Serotonin • Mood swings • Sleep disturbances

  13. 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

  14. “BATH SALTS” AND RELATED STIMULANTS • In the 1970s, a medicinal chemist named Richard A. Glennonwas 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.

  15. “BATH SALTS” AND RELATED STIMULANTS

  16. “BATH SALTS” AND RELATED STIMULANTS

  17. “BATH SALTS” AND RELATED STIMULANTS

  18. “BATH SALTS” AND RELATED STIMULANTS

  19. “BATH SALTS” AND RELATED STIMULANTS

  20. “BATH SALTS” AND RELATED STIMULANTS

  21. “BATH SALTS” AND RELATED STIMULANTS • 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)

  22. “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.

  23. “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

  24. “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

  25. “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

  26. 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

  27. KHAT PHARMACOLOGY • EUPHORIANT (DOPAMINE) • ANOREXIGENIC • STIMULANT • DILATED PUPILS • INCREASED HEART RATE • INCREASED BLOOD PRESSURE • HYPNAGOGIC (AUDITORY DREAM LIKE) HALLUCINATIONS (COMING DOWN)

  28. KHAT

  29. KHAT

  30. KHAT

  31. KHAT

  32. KHAT

  33. KHAT

  34. “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)

  35. SYNTHETIC CANNABINOIDS • CANNABINOID AGONISTS-RESEARCH CHEMICALS • JWH-015 • JWH-018 • JWH-073 • JWH-081 • JWH-133 • JWH-200 • JWH-250 • JWH-398 • CP 47,497 • CP 55,244 • HU210 • WIN 55,212-2

  36. CANNABINOID EFFECTS • Appetite, feeding behavior and body weight • Reward and motivation • Mood and anxiety • Pain • Memory

  37. 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

  38. RIMONABANT • Clinical Trials • Test subjects • No psychiatric history • No family history • High Drop-out rate • Psychiatric Side-Effects • Anxiety • Depression BRAINWORK (May-June 2006)

  39. 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

  40. 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.

  41. 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.

  42. 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.

  43. 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.

  44. SYNTHETIC CANNABINOIDS (SPICE)

  45. SYNTHETIC CANNABINOIDS

  46. SYNTHETIC CANNABINOIDS

  47. SYNTHETIC CANNABINOIDS {K2 (JWH-018, JWH-073)}

  48. “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

  49. “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

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