Transcript drug of abuse

DRUGS OF ABUSE
DEFINITIONS:
Abuse
- any use of a drug for non-medical purposes,
almost always, for altering consciousness
Misuse
Use of a drug for the wrong indication or wrong
dosage
Addiction
a state of psychic or physical dependence
Psychologic dependence
compulsive drug seeking behavior for personal
satisfaction like heavy cigarette smoking
Physiologic dependence
- - is present when withdrawal of the drug produces signs and
symptoms that are frequently the opposite of those sought by
the user ( eg. = alcohol or coffee withdrawal)
-
Tolerance
a decreased response to the effects of the drug
requiring ever larger doses to achieve the same effect
Metabolic tolerance –
due to increased disposition of the
drug
Behavioral tolerance –
 an ability to compensate for the
drug's effects
Functional tolerance
 - due to compensatory changes in
receptors, enzymes or membrane actions of
the drug
CULTURAL CONSIDERATIONS:
1. USA
- caffeine, nicotine and alcohol are legal
2. Middle East
- cannabis ( marijuana ) is legal while alcohol is illegal
3. American native tribes
- peyote, a hallucinogen, is legal for religious purposes
4. Andes of South America
- cocaine is used to allay hunger & enhance the
ability to work at high altitude" the price to pay for
considering drugs as illegal is the criminal activity
related to it like:
1. illegal traffic for profit
2. user may resort to robbery, prostitution or
violent crimes
 KINDS
 =Opiates & opioids

- opium, heroin, morphine, oxycodone, meperidine
 = Depressants & other

- barbiturates, alcohol,
sedatives
bromide, benzodiazepines
 = Stimulants

- caffeine, nicotine, cocaine, amphetamine
 = Hallucinogens
 - LSD, mescaline, psilocybin, phencyclidine, ketamine
 = Cannabinoids - marijuana
 = Inhalants
- anesthetics - chloroform, ether, halothane, nitrous
oxides
- industrial solvents - hydrocarbons
- aerosol propellants - fluorocarbons
- organic nitrites - amyl nitrites, butyl nitrites
 = Steroids
SCHEDULE POTENTIAL COMMENTS
OR CLASS FOR ABUSE
CLASS I
CLASS II
High
High
No accepted
medical use,
lack of
accepted safety
as a drug
Abuse may
lead to psychophysical
dependence.
No telephone
prescription.
No refill
SAMPLE
Narcotics
= heroin
Hallucinogens
= LSD
Opioids
= opium
Alkaloids
= morphine
= hydromorphone
= oxymorphone
= oxycodone
Synthetic
= meperidine
(Demerol)
= methadone
= levorphanol
= fentanyl (Sublimaze)
CLASS
II
Stimulants
= cocoa leaves
= cocaine
amphetamine
Depressants
= Barbiturates
amobarbital
pentobarbital
secobarbital
Cannabinoids
- Dronabinol
CLASS III Less than I
and II
Moderate or low
potential for
physical
dependence with
high potential for
psychological
dependence.
Prescription must
be rewritten after
6 months. Can be
given up to 5
refills
Opioids
codeine
dihydrocodeine
hydrocodeine
opium (paregoric)
Stimulants
benzphetamine
Phendimetrazine
Depressants
barbiturates in
Class II in
suppository form
aprobarbital
butarbital
gluthetimide
metharbital
talbutal
thiamylal
thiopental
(Penthotal)
Steroids
CLASS IV
Less than
that of
Class III
Opioids
Limited
potential for Difenoxin
dependence. Pentazocine
Propoxyphine
Prescription
must be
rewritten
after 6
months.
Given up to
5 refills.
Lesser
penalty for
illegal use
than that in
Class III
Stimulants
Diethylpropion
Mazindol
Phentermine
(Ionamin)
Fenfluramine
Pemoline
Depressants
Benzodiazepines
Chloral hydrate
Meprobamate
Phenobarbital
CLASS V
Less than
that of
Class IV
Limited
Opioids
dependence
Diphenoxyis possible.
A nonopioid. May
be
dispensed
w/o a
prescription
late
(Lomotil)
OPIATES & OPIOIDS:
History
- opium smoking - widely practiced in China
- recently - injecting morphine is increasing in the
West
= 400,000 - 600,000 in the US alone
Chemistry & Pharmacology:
-most commonly abused =
Heroin, morphine, meperidine , oxycodone
 =tolerance to mental effects develop w/ chronic use

= the need of ever increasing amounts to sustain
the desired euphoriant effects & avoid withdrawal
symptoms causes dependence or addiction
Clinical aspects
- factors = curiosity
= social pressure
IV use
= routine - most efficient; - rapid action to brain
= "rush", followed by - euphoria, feeling of tranquility,
sleepiness ( the "nod")
= dose: 25 mg usually ( lasts for 3 - 5 hrs )
= continuous use will eventually drain the victim
financially & when the supplies run out, withdrawal
symptoms set in
withdrawal symptoms= begins 8 - 10 hrs after the last
dose
= resemble increase sympathetic activity
Early:
lacrimation, rhinorrhea, yawning, sweating ,
hypertension
Later:
restless sleep, weakness, chills, gooseflesh ( cold
turkey),nausea / vomiting, muscle aches
involuntary
movements ( kicking the habit )
hyperpnea ( increase respiratory rate )
hyperthermia ( increase temp )
- the secondary phase of protracted abstinence last for 26-30 wks
characterized by: hypotension, bradycardia, hypothermia ,
mydriasis ( pupillary dilatation decreased responsiveness of the
respiratory center to the CO2
Opium flower
Opium plant
Elian smokes opium
Morphine
Heroin
Heroin user
Complications:
- overdose
Hepatitis B
- AIDS
- bacterial infection
= at injection site
= sepsis
= meningitis
= osteomyelitis
= systemic abscess
 - Parkinsonism (spasticity )
= noted in users of fake Meperidine due a
highly toxic neurotoxin
 - homicide
- suicide
- accident
Treatment
= pharmacologic or social approach or both
= chronic users prefer pharmacologic approach
=short term users are amenable to
psychosocial approach
= Pharmacologic Approach: Principle
- DETOXIFICATION
- to substitute a longer acting, orally
active drug
- stabilize the patient on that drug
- then gradually withdraw the drug
Agents:
= methadone (also an opiate)
= single dose daily then decrease frequency
= effect: saturates the opiate receptor and
prevents the
"rush" produced by an IV dose
= recently, Clonidine (Catapres) is being used
- a centrally acting sympatholytic agent
used for hypertension - decreases outflow of
norepinephrine, thus controlling the s/s of
sympathetic overactivity
- advantage
= no narcotic action & non addicting
Lofexidinea clonidine analog with less hypotensive effect, is being
developed for use
=L-acetyl methadol
a longer acting methadone homologue
allows 3x a week rather than daily dosing
and reduced abuse potential, but its
association with sudden cardiac death due to
prolonged QT arrhythmias has made its use
uncommon
Buprenorphine- a partial opioid agoinst
that can be given once daily or even
less often at sublingual doses of 4-32
mg daily depending on the patient.
= the lower doses are useful for detoxification
from heroin while the higher doses are for
longer maintenance treatment
Naltrexone - narcotic antagonist
= blocks the action of opiates
= long acting
= oral
=3x/week
= 100 - 150 mg / day
= psychosocial approach
- peer group pressure
= confrontation
- group or individual psychotherapy
- didactic approach
- alternative lifestyle
= work or communal meditation
- takes months or yrs
- many users may tire of their habit or burn out
even w/o therapy
BARBITURATES & OTHER SEDATIVES
History:
- alcohol = oldest, most abused
- bromides = first used as a sedative and an anticonvulsant
in 1857
= now, obsolete due to:
- excessive drowsiness
- toxic
- replaces chloride ion w/ bromide ion
leading to toxic delirium
- slow onset
- barbiturates = 1903
meprobamate = 1954; non barbiturate sedative
- gluthetimide & methaqualone
= sedative hypnotic
= worse than barbiturates
= more abuse potential
benzodiazepines= 1960
= less abuse potential
Chemistry & Pharmacology
> effects are dose dependent
= sedation
= coma
= hypnosis
= death
= anesthesia
> mechanism of psychic & physical dependence unclear
- barbiturates
= drugs w/ very short half life ( 4 hrs ) cannot be taken frequently
enough
to sustain a high concentration and are rarely
associated w/
withdrawal reactions
= drugs w/ half life ( 8 - 24 hrs) produce rapidly evolving severe
withdrawal symptoms
- = those w/ long half life ( 48 - 96 hrs ) have a slow onset with less
severe but longer duration withdrawal symptoms
= those w/ longer half lives have a built in tapering off actions w/ reduced
possibility of withdrawal symptoms
Clinical aspect
> mainly psychologic dependence
> physical dependence
= rare w/ benzodiazepines
= may occur w/ long term use of more than
40 mg / day of diazepam or the equivalent dose
of other kinds
> therapeutic dose dependence
= abrupt withdrawal after several months or years
of therapeutic use may result to symptoms noted
only in high dose long term users
- weight loss
- changes in perception -headache paresthesias
Abusers
= w/ emotional disorders
= used to escape into oblivion, to alter
mental state, w/ disinhibition, slurred
speech, incoordination, then
drowsiness ( similar to alcohol abusers )
= others alternate it w/ a stimulant or
polydrug use
> tolerance may develop to the sedative effect, but not to the
respiratory depressant effect = this is fatal if mixed w/ other similar
drugs or alcohol
> withdrawal symptoms ( alcohol - barbiturate type )= from short
acting drugs
- first 8 hrs - sign of chronic intoxication
disappear

- next 16 hrs - followed by tremors,
anxiety, twitches, nausea,vomitng
Propranolol or Clonidine may reduce these
symptoms
- 16 - 48 hrs - convulsion, delirium, hallucination,
psychosis-like symptoms
= for long acting drugs
- 2 - 3 days = no symptoms
- 4th - 5th day = start of withdrawal
symptoms
- 8th - 9th day = convulsion
- then the syndrome subsides
- this slow evolution may warn the patient &
force him to resume the drug again
- others may just go thru the syndrome w/o
knowing what is happening
> Treatment'
- short acting drug abuse= phenobarbital is
used at pharmacologically equivalent dose
- long acting drugs = the same drug may be
continued at a lower dose w/c does not
produce s/s & gradually tapered &withdrawn
= rate of decrement
- 15 - 20 % of the daily dose
- completed in 2 wks
Benzodiazepines
Flunitrazepam
Gamma hydroxy butyrate
STIMULANTS
History:
- Caffeine = most widely used
= effect: disturbed sleep & heart rate
withdrawal symptoms is noted for heavy users of 600
mg /
day ( 6 cups/ day )
Nicotine = also widely used ( up to 28 % of adult
population)
- Cocaine = used for over 1200 yrs
= South American natives chew coca leaves
= isolated as the active substance from coca
leaves in 1860
= anesthetic properties noted in 1870
Coffee beans
Tobacco
Cocaine
Cocaine powder
Cocaine
Cocaine powder
Cocaine tea
Cocaine wine
Cocaine used as Pomade
Cocaine toothache drops
Crack Tools
Paraphernalia for cocaine
Guy sniffing cocaine
Guy snorting cocaine
Cocaine user
CNS site of action of cocaine
Amphetamines
synthesized in 1920 and introduced in medical
practice in 1936
= dextroamphetamine - major kind
= others - methamphetamine - methedrine, speed,
shabu
- phenmetrazine
- methyl phenidate
- dimethoxy methylamphetamine
- methylene dioxyamphetamine = more
serotoxic or serotonergic
- cathinine - from leaves of khat in
Middle East & Africa
Shabu powder
Metamphetamine various form
Smokeable form of
metamphetamine
Site of action of metamphetamine
Ecstasy
Clinical Pharmacology
> Caffeine
= increase cAMP by blocking the catabolic
enzyme phosphodiesterase but increasing
effects of catecholamine neurotransmitters
receptors for adenosine
> Cocaine
= facilitate catecholaminergic
neurotransmission by reducing norepinephrine
> Amphetamine
= increase release of catecholamine
= weak inhibitors of monoamine oxidase
thus increasing catecholamine activity
or interaction w/
= psychic dependence – common
= physical dependence - rare
= withdrawal symptoms result to symptoms
opposite to that of the original effect w/c lasts for
several days (sleepy, appetite, exhaustion,
mental depression)
= tolerance develops quickly so that abusers may
take increasing dose
Clinical aspect
Amphetamine abuse - 1940
= present in inhalers for nasal decongestion
= 1960 's - methamphetamine became popular for
IV
injection because it is easily synthesized
= abuse is called a "run"= repeated IV injection -> "rush"
- an orgasm-like reaction
- followed by a feeling of mental alertness
& marked euphoria
- if repeated for several days:
= paranoid schizophrenia-like state
delusions - bugs crawling in skin ->
scratches all over
= necrotizing arteritis may lead to fatal
brain or kidney hemorrhage
finally = exhaustion from lack of sleep, food then,
withdrawal symptoms occurs
overdose - rarely fatal ( treatment — haloperidol)
later - methamphetamine crystals ( ice ) or "shabu" are
smoked
- this is similar to the cocaine called "crack" w/ is
also smoked
- smoking delivers a rapid bolus of the drug to the
brain, whose effects last for several hours, longer
than cocaine
> Cocaine
= more magnified effect than amphetamine
= before - very expensive - used only by the
very rich
= now - even students & workers are using it
= route — sniffing, smoking, IV (rarely used)
= short half life = 1-2 hrs
= "speedball" = if used w/ heroin, IV
= effects
vasoconstriction ( hypertensive crisis, M.I. , strokes )
- anesthetic effect - seizure
- overdose - rapidly fatal - w/in minutes
(arrythmias, respiratory depression,
seizure)
treatment: IV diazepam, propranolol
Long term treatment
- there is no specific treatment program
= may use the rehabilitative programs for
opiate dependent persons
= if w/ residual emotional disorder like
schizophrenia, psychosis, depression
treatment: antipsychotic
antidepressants
under investigation
= desipramine,
clonidine,
bromopramine, buprenorphine
amantadine , buspirone
HALLUCINOGENS
- Lysergic Acid Diethylamide (LSD)
- Mescaline & Psilocybin
= cactus buttons or magical mushrooms
- Deliriants = atropa belladona & datura
stramonium
- also in morning glory seeds = monoethyl amide
Definition:
= Hallucinogen - distorted perception
= psychotomimetic - psychosis like
= psychedelic - mind revealing
chemistry & pharmacology
= LSD - semisynthetic, do not occur in nature
= mescaline - phenethylamine derivative,
natural
= psilocybin - indolethylamine derivative,
natural
= morning glory seeds - monoethylamide,
natural
= all have chemical resemblance to the 3
major
neurotransmitters
Norepinephrine
dopamine
serotonin
effects = produce a state of hyperarousal to the CNS
= LSD - works mainly on the serotonergic, system,
decreasing the activity of this
neurotransmitter
- may act on the presynaptic serotonin
receptor inhibiting release of serotonin
- increase brain concentration of serotonin &
decrease concentration of its metabolite 5hydroxy indole acetic acid
clinical effects
= produces a series of somatic perceptual & psychic effect
overlapping w/ one another
= somatic symptoms - dizziness, weakness, tremors, nausea,
paresthesia
= perceptual symptoms (LSD) - blurring of vision
- distortion of perspective
- organize visual illusions and hallucinations
- less discriminant hearing
- change in sense of time
= psychic effect:
- impaired memory
- difficulty in thinking
- poor judgement
- altered mood
= Physiologic
over activity of sympathetic nervous system
and central stimulant ( dilated pupils,
tachycardia, hypertension, tremors, alertnes
= deliriant hallucinogen:
scopolamine = blocks central muscarinic
receptors
= similar mental effects maybe seen with
therapeutic or deliberate overdose of drugs with
anti-muscarinic action like anti Parkinson's &
tricyclic antidepressants
= effects: delirium, fluctuating levels of
awareness, disorientation, marked
difficulty in thinking, marked loss
of memory, bizarre delusion, may last 1
day or more
Lysergic acid
LSD
Mescaline
Angel dust
Phencyclidine (PCP) ="angel dust“
= initially introduced as dissociative anesthesia in
1957
= mechanism of action:
blocks uptake of dopamine
= may be :> smoked by mixing powder with
tobacco
> sniffed
> taken orally
> injected IV
= presumed effect
> makes patient insensitive to pain by
separating their bodily function from their
mind without causing loss of consciousness.
= withdrawn from use in humans
> still used by veterinarians
street name - "hog"
clinical effects (PCP) = detachment, disorientation ,
distortion of body image, loss of
proprioception
=somatic signs and symptoms - numbness,
nystagmus, tachycardia,hypertension
Ketamine vial
Ketamine (Ketalar)
= also a dissociative anesthesia
= replaced PCP for human use
= also prduces emergent hallucination
toxicity of hallucinogen
1. panic reaction - bad trip
- treatment: = sedation w/ barbiturates or
benzodiazepine
= "talking down"
2. PCP overdose
- acute depressive or psychotic reaction
= treatment - give antipsychotics if
prolonged schizophrenia follows
= errors of judgment may threaten life
= treatment - physostigmine
- if w/ seizure or excitation
= treatment – diazepam
Treatment for hallucinogens in general
= no specific program for rehabilitation
= separation of individual from the drug
culture should be tried & it should be
voluntary
MARIJUANA
- plant = Cannabis sativa, cannabinoids
- street names = grass
= hashish - a resin extract of the plant w/c is
more potent
Chemistry & Pharmacokinetics
= 3 kinds.
- cannabidiol (CBD)
- tetrahydrocannabinol (THC)
- cannabinol (CBN)
Marijuana
= route of administration: smoking
= high lipid solubility of THC -- readily trapped in
surfactant lining
= rapid systemic absorption
= similar to IV dose
- short duration - few min. to hrs.
= effects noted after 2-3 inhalations, peaks 20 min.
after, & disappears after 3 hrs.
- oral = mixed w/ food
= slow absorption - peaks in 3-4 hrs
= longer duration - last for 6-8 hrs
= may stay in lipid compartment for 1 wk. before
complete excretion
Pharmacodynamics:
- distinct receptors were identified in substantia
nigra, globus pallidus, hippocampus,
cerebellum, forebrain
- receptors are distinct only for cannabinoids
- may also act on the cell membrane itself
w/ various effects that suggest actions like in:
amphetamines, alcohol, sedative, atropine, morphine
effects:
- > early stage- "high" = euphoria, uncontrollable laughter,
alteration of time sense, depersonalization,
sharpened vision
> later effects. relaxed, dream-like state, difficulty in
thinking straight & in concentrating
- cannabis intoxication
= increase pulse rate, reddish conjunctiva, hypotension,
antiemetic, muscle weakness, unsteadiness,
increased deep tendon reflexes, impaired psychotic test
= tolerance develop in heavy long term use
= w/drawal symptom noted after a very high
dose
= health hazard= decrease testosterone?,
bronchoconstriction?
(bronchitis,obstruction,,
metaplasia), altered immunity?, fetal
effects?,angina may be aggravated
(increased heart rate, decreased BP, increased
carboxyhemoglobin), loss of interest?
(amotivational syndrome), acute panic
reaction?, toxic delirium?, paranoia?, frank
psychosis?, brain damage?
Therapeutic THC-Dronabinol
= reduce nausea and vomiting in patients
undergoing cancer chemotherapy and to
stimulate appetite in AIDS patients
= shown to reduce intraocular pressure in
glaucoma
Levonantradol, an analog may be used as an
analgesic
= stopping the drug results to clarity
of thinking
Marijuana user
INHALANTS
- kinds:= anesthetics
= nitrous oxide, chloroform, ether,
halothane
= industrial solvents
= hydrocarbons (toluene)
= aerosol propellants
= fluorocarbons
= organic nitrites
= amyl nitrites, butyl nitrites
chemistry & pharmacology
= clinical aspects
1. nitrous oxide
= taken as 35% mixed w/ oxygen
= inhalation of 100% may cause asphyxia or
death
= effects - difficulty in concentrating,
dreaminess, euphoria, numbness,
tingling, unsteadiness, visual /
auditory disturbance
2. ether & chloroform
= effects - exhiliration initially followed by
loss of consciousness
= highly flammable
3. industrial solvents - gasoline, paint thinner, glue, rubber cement, acrylic paint
spray, shoe polish, degreasers
4. toxic ingredients - toluene, heptane, hexane, benzene,
trichloroethylene, methylethylketone
= motives for abuse - peer influence, low cost,
readily available, convenient packing, quick
intoxication of short duration (5-15 min.), mood
enhancement
= principal users - boys, early teens, low socio economic status,
problematic
= develops psychologic dependence
= manner of abuse:
> cloth is soaked w/ solvent & fumes are inhaled
> aerosol propellants are inhaled from
plastic bag
= effect - initially euphoria w/ relaxed &
a drunk feeling, followed later on by
disorientation, slow passage of time &
hallucination
5. organic nitrates
= effects - sexual enhancer
6. amyl nitrates
- used medically for angina
- contained in fragile ampoules covered by
cloth w/c easily can be broken
(w/ popping sound) & inhaled - called "poppers"
7. isobutyl nitrates
- bottled
- "locker room", "rush“
- effects = giddiness (lightheadedness), dizziness,
rapid heart rate, decreased BP, flushing of skin,
"speeding", decreased inhibition, decreased
strength of erection thus prolonging sexual
intercourse
toxicity
> chloroform - liver & kidney damage
> solvents - damage to liver, kidney, peripheral
nerve, brain, bone marrow, lungs
> fluorocarbon - sudden death due to ventricular arrythmia &
asphyxiation
- > nitrites - hazard to patients w/ cardiovascular disease
Inhalants
Inhalants
Polyethylene glycol
Inhalant user
Inhalant hazards
Ct scan showing marked atrophy of
the brain 2° to Toluene abuse
Brain lesion of inhalant abuser
STEROIDS:
Anabolic Steroids were first used in competitive sports during the
1940’s and by the late 1980’s
Use was widespread in adolescents in
gymnasiums and physical fitness centers
Clinical Use and Effects:
Oral and injectable formulations are used simultaneously
Effects:
increased muscle mass and strength
increases in aggression
changes in libido and sexual functions
mood changes with occasional psychotic
features
Cognitive impairment, including
distractability, forgetfulness,
and confusion

Withdrawal syndrome – fatigue,
depressed mood, and a craving
for steroids
STEROIDS
Clinical findings:
hypertrophied muscles
acne, oily skin
hirsutism in females
gynecomastia in males
needle punctures
edema and jaundice may develop in
heavy users
Common lab abnormalities include:
elevated
hemoglobin and hematocrit,
elevated LDL, and depressed HDL,
elevated liver function test and depressed LH.
STEROID USER
GYNECOMASTIA OF STEROID
COMPLICATIONS OF STEROIDS
Treatment:
1. Mental health professionals
2. Peer counseling by former body
builders and group support
3. Nutritional counseling
4. Consultation with a fitness expert
5. Abusers need to avoid gymnasiums
until recovery is firmly established
Free crack and pot
THANK YOU VERY MUCH
GOOD LUCK
STUDY WELL!