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Drug Misuse & AbuseHallucinogens
Presented by/ Gina Tag Eldin
M.Sc. Pharmaceutical chemistry, 2016.
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Drug Misuse and Abuse
What is a drug?– A drug is any substance used safely to cure or prevent or diagnose
a disease. – Or Broadly defined as any chemical entity or mixture of entities
not required for the maintenance of health but that alters biological function or structure when administered.
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Drug abuse Vs Drug misuse!!!
– Drug misuse: To take medicine in a way that is not intended, without following the instructions on the label, inappropriate dose of legal drug, or for a long time. e.g. Dextromethorphan (Antitussive).
– Drug abuse: Any use of drugs that causes physical, psychological, or social harm to the individual user or to others affected by the drug user’s behavior or use of illegal drugs (psychoactive) to produce pleasure and remove stress. e.g. Tobacco.
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Habit Vs Dependence Vs Addiction
– Habit: A healthy continued involvement with an object or activity.
– Dependence: Physiological and psychological issues i.e. Dependence is characterized by the symptoms of tolerance and withdrawal. While it is possible to have a physical dependence without being addicted.
– Addiction: An unhealthy continued involvement with a mood-altering object or activity that creates harmful consequences. Or biological attachments to consumption of substances. Habits become addictions when a chemical dependence occur i.e marked by a change in behavior caused by the biochemical changes in the brain after continued substance abuse.
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Hallucinogens
– Chemical substances that alter thoughts, mood and perception. (altered sense of reality).
– Derived from the Latin verb alucinari “ to wonder in mind or to dream.”(illusion).
– Interchangeably with the term “psychedelic” which means mind revealing.
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Historically, magical mushrooms (psilocybin and psilocin), peyote button (mescaline), kykeon (barely, water, mint, ergot (LSD)), ipomea paste (teotlaqualli) from morning glory plants were used in religious ceremonies and medicines.
NH
NH
O
NH
NN O
OO
OHH
H
Ergotamine
N
NCH3
O
N
H
CH3
H3C
LSD-25
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Morning glory flower kykeon
Magic Mushroom Peyote button
Ergot Rye
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Religious ceremonies
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History– In 1938, Albert Hofman synthesized LSD-25 (ergot
derivative), accidently ingested few micrograms (250 μg) and experienced the 1st trip.
– In 1949, Sandoz began marketing LSD-25 to psychiatrists in US in psychotherapy.
– Due to recreational use, LSD has been prohibited by 1960s.
LSD-25
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STREET NAMESHALLUCINOGENIC SLANGGlossary of drug slang
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Clinical Symptoms (Intoxication)– Eidetic Imagery (endless)
– Depersonalization
– Perception: visual distortions, blurred vision, perception of distance and depth
– Synesthesia
– Delusions of supernatural abilities, suicide
– Euphoria or frightening experience may occur (extreme sensation)
– Flashbacks
– Prolonged adverse reactions: psychosis, paranoid states, depression
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Classes of Hallucinogens
– Classical are (similar to serotonin or LSDlike agents) that share common discriminative stimulus properties and that might act via a common mechanism of action.
– Non classical hallucinogens: these groups of agents act by different mechanisms and produce distinct effects common to members within each group.
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Classes (chemically)
– Indolealkylamines (Tryptamines)– Phenylethylamines (similar to nor-ep)– Anticholinergics (Deliriants)– Miscellaneous category
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N
N CH3H3C
OH
N
N HH
HO
N
NCH3
O
N
H
N
N CH3H3C
H
CH3
H3C
H H
Serotonin (5-HT) Psilocin
LSD-25DMT
5-hydroxytryptamine
N,N-dimethyltryptamine
Serotonergic Hallucinogens
(similar to 5-HT)
5-HT is associated with Mood, Sleep, Appetite,
Clinical Psychosis & Hallucinogens!!
α
N
NH2
H
5-OMe MeT5-methoxymethyltryptamine
O
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Neuropharmacology
Serotonin is generally an inhibitory neurotransmitter that regulates sleep, pain sensation, appetite, mood, sensory perception; it often plays a role in helping us feel relaxed.
LSD or LSD likes act like an antagonist or partial agonist at 5-HT2 and 5-HT1c receptors, agonist at multiple 5-HT1receptors; it inhibits or blocks the release of serotonin at the receptor.
This slowdown in serotonin activity causes hyperactivity in the regions of the brain which regulate our visual and emotional responses.
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LSD Psilocybin/ Psilocin
DMT
Dose 70-140 g Perceptual and psychic
effects
4-10 mg 15-60 mg
Metabolism Liver, no active metabolites (6 metabolites).
Liver activation to psilocin by alkaline phosphatase
Deamination by MAOto indole acetic acid (IAA)
Administration Orally (tablets microdots or stamp)
Orally in form of mushroom or as white
powder
Inhalation or by smoking, injected (less common)
Successive breath
Toxicity LD 50 = 14 mg 17gm, 1 gm respectively not estimated
Potency 100 to 200 times than psilocin
1% as potent as LSD Difficult, due to different route of administration
Onset of action 30-40 min 30-40 min 5 min
Duration 8-12 hr 2-6 hr 15 -30 min"businessman's trip"
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N
NCH3
O
N
H
CH3
H3C
LSD-25
N
NH
O
N
H
CH3
H3C
Nor-LSD
N
NCH3
O
N
H
CH3
LAE
H
N
NCH3
O
N
H
CH3
H3C
2-Oxo-LSD
O
N
NCH3
O
N
H
CH3
H3C
OOH
2-oxo-3-hydroxy-LSD
N
NCH3
O
N
H
H3C
LEO
HO
N
NCH3
O
N
H
CH3
H3C
13 or 14-Hydroxy-LSD-glucuronide
O-glucoronoid
The Metabolites of LSD In active
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N
N CH3H3C
OH
HPsilocin
N
N CH3H2C
O
HPsilocybin
Alkaline Phosphatase
H
PO
OOH
Physiological Conditions
Psilcybe mushrooms(“Magic” mushrooms)
Prodrug Active
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N
N CH3H3C
H
DMT
N
COOH
H
MAO-A
IAA
X
Iproniazide
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LSD Psilocybin/ Psilocin
DMT
Dose 70-140 g Perceptual and psychic
effects
4-10 mg 15-60 mg
Metabolism Liver, no active metabolites (6 metabolites).
Liver activation to psilocin by alkaline phosphatase
Oxidation by MAOto indole acetic acid (IAA)
Administration Orally (tablets microdots or stamp)
Orally in form of mushroom or as white
powder
Inhalation or by smoking, injected (less common)
Successive breath
Toxicity LD 50 = 14 mg 17gm, 1 gm respectively not estimated
Potency 100 to 200 times than psilocin
1% as potent as LSD Difficult ,due to different route of administration
Onset of action 30-40 min 30-40 min 5 min
Duration 8-12 hr 2-6 hr 15 -30 min"businessman's trip"
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Classes
– Indolealkylamines (similar to 5-HT)– Phenylalkylamines (similar to nor-ep)– Anticholinergics (Deliriants)– Miscellaneous category
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Phenylalkylamines(Phenylethylamine)
Norepinephrine
OHNH2HO
HO
Dopamine
NH2HO
HO
Mescaline
NH2O
OO
CH3
H3C
H3C Weak hallucinogenic Dose (orally) = 350 mg1000-5000 times less
potent than LSDNauseating with bitter
taste ??Tea, smoked, ingested
Duration 6-12 hr.
Peyote Coctus
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CH3
NH2
Amphetamine
Modification of mescaline structure that produce both stimulant and hallucinogenic effects.
Mescaline
NH2O
OO
CH3
H3C
H3C
N
CH3
CH3O
O
H
MDMAMethylenedioxymethamphetamine
Ecstacy, XTC, love or hug drugWidespread among teenagersCommon in ravesDose = 125 mgPills or pure crystals dissolved in waterOnset of action 30 min -1 hrDuration 3-6 hrPurity issue??? 42.22 celeciousAuthentication problem???
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Ecstacy, XTC, love or hug drugNeurotoxicWidespread among teenagers in ravesDose = 125 mgPills or pure crystals dissolved in waterOnset of action =30 min -1 hrDuration = 3-6 hrPurity issue ??? Authentication???
Bad trip
RAVES
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Neuropharmacology Presynaptic releasing agent of serotonin, norepinephrine, and
dopamine. High affinity for 5-HT receptor specially 5-HT 2. Binds with less affinity to DA 1 and 2 and NE receptors. long term use cause serotonin neurotoxicity and memory
impairment which is directed to the dose administered.
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Symptoms Oral effects include xerostomia, bruxism and dry mouth. (characteristic).
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Classes
– Indolealkylamines (similar to 5-HT)– Phenylalkylamines (similar to nor-ep)– Anticholinergics (Deliriants)– Miscellaneous category
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Anticholinergic Hallucinogenic Atropine and scopolamine block acetylcholine receptors in the
brain muscarinic receptors. In low doses they are used for a variety of medical purposes.
atropine, if administered rapidly after exposure, is an antidote for nerve gas.
Anticholinergic hallucinogens produce such physiological effects as dry mouth, blurred vision (mydriasis), loss of motor control, and increased heart rate and body temperature
They can be fatal as they cause respiratory failure at doses only slightly higher than the effective dose
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Datura stramonium Atropa Belladonna Henbane
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Classes
– Indolealkylamines (similar to 5-HT)– Phenylalkylamines (similar to nor-ep)– Anticholinergics (Deliriants)– Miscellaneous category
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DissociativeNon-classical
NMDA receptor antagonistse.g. Ketamine, PCPκ-opioid receptor agonistse.g. Ibogaine, Salvinorin A
Β-carbolinesClassical
Act as 5-HT2 antagonists and some members have MAO inhibition
activitye.g. Harmine, Harmoline
Less potent than DMT
CannabinoidNon-classical
Miscellaneous
CB-1 receptor antagonists
e.g. Dronabinol
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Designer Drugs
– Structurally altered or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances (club drugs) or bath salts.
– Tested on animals with no expectation of potency and unexpected side-effects
– Synthesized in underground labs (no Q.C).
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List of Designer Drugs (psychedelics)
Lysergamidese.g. 1-Acetyl LSD
Tryptaminese.g. psilacetin or 4-
acetoxy-DMT
Phenethylaminese.g. 3C-E
N
NCH3
O
N
CH3
H3C
1-Acetyl LSD
O
N
N CH3H3C
H
4- Acetoxy DMTPsilacetin
OO
3C-E
NH2O
OO
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Solvents!!! 2015
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References
– Mehling R, Triggle DJ. Hallucinogens. Infobase Publishing; 2009. book
– Foye WO. Foye's principles of medicinal chemistry. Lemke TL, Williams DA, editors. Lippincott Williams & Wilkins; 2008. book
– Maisto SA, Galizio M, Connors GJ. Drug use and abuse. Cengage Learning; 2014. book
– Rivera-García MT, López-Rubalcava C, Cruz SL. Preclinical characterization of toluene as a non-classical hallucinogen drug in rats: participation of 5-HT, dopamine and glutamate systems. Psychopharmacology. 2015 Oct 1;232(20):3797-808.
– Canezin J, Cailleux A, Turcant A, Le Bouil A, Harry P, Allain P. Determination of LSD and its metabolites in human biological fluids by high-performance liquid chromatography with electrospray tandem mass spectrometry. Journal of Chromatography B: Biomedical Sciences and Applications. 2001 Dec 5;765(1):15-27.
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