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COCAINE POISONING
DR.FAIZ AHMAD
What is Cocaine?• Cocaine (benzoyl-methyl-ecgonine)
(C17H21NO4) is a colorless,odorless,crystalline alkaloid with better taste prepared from the leaves of the Erythroxylon coca plant.
• Which grows in South America,India and Java.
Features of plantsPlant is 8-12 feet tall.Category: ShrubsFruits: Red oval shaped, 1 cm size and produces
only one seed.Seeds: Brownish ovalStem diameter: 16cms• Leaves: Green, smooth, glossy, opaque, oval,
tapering at extremities, 2-3 cm wide and 3-11 cm long.
Leaves when chewed have pleasant, pungent taste.
Poisonous parts: Leaves• Fatal dose- 1g IV,toxic symptom occure after
200mg.regular user can take upto 10g.• Fatal period-few min to few hrs.• Toxins: Methylbenzoylecgonine i.e. Cocaine an
active principal obtained from leaves.
• According to the National Institute of Drug Abuse (NIDA), cocaine is:“A powerfully addictive drug that can be sniffed, injected, chewed or smoked
• Cocaine has been classified as a Schedule II drug by the United States
The 2nd Harmful
Drug
Geographical Distribution• Grows throughout the tropical regions.• Whole of Latin American Countries such as
Columbia, mexico, ecuador, and other countries such as Chile, Peru, India, Indonesia, Sri Lanka, etc.
• Bolivia-leading producer-80% world total cocaine producer.
High risk geographical areas:
• 1. Bolivia• 2. Peru• 3. Brazil – Amazon
region• 4. Ecuador• 5. Columbia• 6. Chile
Street name Coke Snow Cadillac White Lady Blow Devils dandruff She(C)
History
• 3000 B.C:Leaves chewed throughout South America. Coca believed to be a gift from God.
• 1708 A.D. Coca first time mentioned in materia medica.
• 1850: Coca tinctures used in throat surgery• 1855: Cocaine 1st time extracted from coca leaves.
• 1884: Used as local anaesthetic in eye surgery
• 1886: Cocaine introduced in newly launched soft drink - Coca Cola.
• 1901: Cocaine removed from Coca Cola.• 1905: Snorting cocaine in the form of powder
became popular.• 1910:1st case of nasal damage seen.
• 1912: U.S. Govt. reports 5000 cocaine related fatalities in one year
• 1914: Banned of cocaine in U.S.• Cost of making 1 kg cocaine: $200-$400.• Cost of 1 kg cocaine- at present $15000 –
35000.
Form’s of Cocaine • Cocaine hydrochloride:Cocaine leaf contain less than 2% cocaine.By treating leaf with sulphuric acid,cocaine
sulphate is produced.Which convered to cocaine hydrochloride by
treating with HCl.Cocaine HCl contain 90% cocaine.Is either snorted or injected but cannot
besmoked.
• Smokeable form of cocaine (free cocaine,free base, crack cocaine)
Make a crackling sound when heated, is produced by treating cocaine HCl with Baking soda.
Act of snorting free base is refer to as Freebasing.
Route of Administration Cocaine can be administered as a drug
of abuse in the following ways 1. Cocaine hydrochlorideSnorting (intranasal)
Intravenous injection
2. Crack Cocaine: Inhalation of vapor from heated foil or pipe. (Smoked)
3. Coca leaves: Chewed or ingested.
COCAINE mechanism of action1.Block reuptake of biogenic amines: Dopamine,Nor-epinephrine,Epinephrine,Serotonin.↑epinephrine→tachycardia↑nor-epinephrine→hypertension↑dopamine,serotonin→cocaine addiction↑serotonin→seizures2.Increses excitatory amino acid concentration in brain:-psychomotor agitation-hyperthermia-seizures
When given locally• Cocaine produces anesthesia by inhibiting excitation
of nerve endings or by blocking conduction in peripheral nerves.
• This is achieved by reversibly binding to and inactivating sodium channels.
• Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve.
• When a nerve loses its ability to propagate an impulse, the individual loses sensation in the area supplied by the nerve.
• Desensitizes the terminal nerves and causes vasoconstriction at the site of local application.
Toxicokinetics• Absorption-rapidly absorbed following all
route of exposure.• Metabolism-• 50% is hydrolyzede to benzoylecgonin.• 45% metabolised by plasma cholinesterase to
ecgonine methyl ester.• 5% undergoes N- demethylation in the liver to
form norcocaine.
• Serum half life of 45-90 minutes.
• Only 1% of the drug is recovered in urine after
ingestion.
• Cocaine can be detected in blood or urine only for
several hours after its use.
• Cocaine metabolites are detectable for 2-5 days.
• Hair analysis provides a very sensitive marker for
cocaine use within the preceding weeks to months.
Onset of actionRoute Onset of action Peak action Duration of action
Smoking/IV 7-15 sec(within minutes)
3-5 min 20-30min
Snorting 1-5min 20-30min 45-90min
Oral 15-30min 60min 90min
Therapeutic Uses of Cocaine• Cocaine is used by health care professionals to
temporarily numb the lining of the mouth, nose, and throat (mucous membranes) before certain medical procedures (e.g., biopsy, stitches, wound cleaning).
• It is an anesthetic that works quickly to numb the area about 1-2 minutes after application.
•
• Cocaine also causes blood vessels to narrow, an effect that can decrease bleeding and swelling from the procedure.
• It is also sometimes used in palliative care of terminally ill patient
Effects of Cocaine Initial Low Doses A. Physical Effects :1.Tachycardia, tachypnoea,2.hypertension,3.Dilated pupils (& flattened lenses), 4.sweating5. reduced appetite, reduced need for sleep, reduced lung function,6. dry mouth,7. impaired motor control & performance of delicate skills and driving.
B. Psychological Effects :1.Euphoria, sense of well being, 2.Impaired reaction time and attention span,3. Impaired learning of new skills.
Increased doses A- Physical Effects :1.Seizures, 2.cardiac arrhythmias,3.myocardial infarction, 4.stroke,5.respiratory arrest.
B. Psychological Effects :1.Anxiety,2. irritability,3. insomnia,4.depression, paranoia,5.aggressiveness,6. impulsivity, 7.delusions,8. agitated/ excited delirium, 9.reduced psychomotor function.
Chronic Use A- Physical Effects :•Erosions,• Necrosis and perforation of nasal septum,• Anosmia, rhinorrhea and nasal eczema (snorting), • Chest pain, muscle spasms,• Sexual impotence, • Weight loss, malnutrition, vascular disease.
B- Psychological Effects :•Dependence, •disturbed eating and sleeping patterns
Central Nervous System o Cocaine euphoria is associated with transient increases in EEG
activity.
o Seizures may occur in persons without a seizure history, even
with first time use of cocaine.
o These are usually single, generalized tonic-clonic seizures
occurring within 90 minutes of cocaine use.
o Cerebral vasoconstriction, cerebrovascular
disease,hemorrhagic and ischemic stroke are
increased in cocaine users.
o MRI, PET imaging in chronic cocaine users
demonstrate structural and functional brain
abnormalities.
o A pathologic study using melanin immunoreactivity
found cocaine users to have 16 percent fewer midbrain
dopamine neurons than non-using subjects.
This and related findings
o suggest that cocaine may have a neurotoxic effect on
dopamine neurons, contributing to development of
cocaine dependence in some users.
• Cocaine use is associated with a variety of movement disorders:
• Cocaine users are at increased risk of acute dystonic reactions from neuroleptic (antipsychotic) medications.
Stereotyped Behaviors Choreoathetosis
Buccolingual Dyskinesia
Tourette’s Syndrome
Acute Dystonic Reactions
Akathisia (Crack Dancers)
Brain images showing decreased dopamine2 receptors in the brain of
a person addicted to cocaine versus a nondrug user. The dopamine
system is important for conditioning and motivation, and alterations
such as this are likely responsible, in part, for the diminished
sensitivity to natural rewards that develops with addiction.
Respiratory System o The effects of cocaine on the
respiratory system depend on the
route of administration.
o Intranasal cocaine use (snorting) may
cause chronic rhinitis, perforation of
the nasal septum, saddle nose,
oropharyngeal ulcers,granuloma of
nose.• Due to vasoconstriction
and resulting ischemic necrosis
• Regular snorting can lead to loss of sensation of smell,
nose bleeding, problem of swallowing, hoarseness and
irritation of nasal septum leading to chronically
inflammed running nose.
Smoked cocaine use produces acute respiratory symptoms in up to half of users.
Productive Cough Shortness of Breath Chest Pain
Hemoptysis Wheezing Exacerbation of Asthma
These effects are probably due to direct damage to the
alveolar-capillary membrane by cocaine or inhaled micro
particles.
Cardiovascular System • Cardiopulmonary symptoms are the most
frequent complaints in cocaine users who seek medical help, with chest pain.
Cocaine
• Increase HR • Increase BP• Increase SVR
By increasing adrenergic activity
in the heart, and indirectly via the
CNS.
The increased myocardial oxygen demand, coupled
with decreased coronary blood flow from vasospasm
and vasoconstriction, can cause acute myocardial
infarction.
Cocaine appears to enhance the progression of renal
disease in patients with hypertension.
Cocaine use increases risk for cardiac arrhythmias and
sudden death.
• Chronic use is associated with left ventricular
hypertrophy, cardiomyopathy, myocardial fibrosis, and
myocarditis.
Gastrointestinal System o Cocaine use by any route of administration reduces salivary
secretions (xerostomia) and causes bruxism.
o Cocaine reduces gastric motility and delays gastric emptying.
o Cocaine induced vasoconstriction and ischemia may result in
gastrointestinal ulceration, infarction, perforation, and ischemic
colitis.
Ingested cocaine can cause bowel gangrene due to
reduced blood flow.
Many chronic cocaine habitual suffers loss of appetites
and can experience significant weight loss and
malnourishment.
Tongue and teeth are black
Urinary System
Cocaine use is known to have caused:•Renal infarction
•Renal thrombosis
•Haemolytic uraemic syndrome
•Rhabdomyolysis with myoglobinuric renal failure
Eyes
• Acute angle closer glucoma-due to mydriasis.
• Loss of vision-vasospasm of retinal vessels.
• Madarosis(loss of eyebro and eyelash)-tharmal
injury associated with crack cocaine.
• Crack eye -corneal defect-corneal anesthesia-
loss of corneal sensation-corneal injury.
• Cocaine bugs phenomenon (Magnans,s symptom,Formication): Grains of sand are lying under skin or some small insects are creeping on the skin giving rise to itching sensation – a form of tactile hallucination-results in scratches,excoriation and ulcers.
• Crack Babies: Increased risk of foetal malformation fo cardiovascular and cerebrovascular system due to chronic abuse of cocaine by the mother.
• Crack dancing - choreoathetoide movement due to dysregulation of dopamine.
Common Adverse Effect of Cocaine use in Pregnancy!!
• 1- Restricts blood flow to the uterus, cause fetal hypoxia.• 2- Uterine contractions, CNS infarction, Heart defects.• 3- Persistent neonatal arterial hypertension.• 4- Decreased neonatal weight and size ( head
circumference).• 5-sudden infant death syndrome, Mental retardation.• 6- Babies may be irritable at birth and exhibit symptoms
such as: tremor, hypertension, abnormal reflexes, tachypnea, autonomic instability, vomiting, diarrhea, seizures and poor feeding.
Cocaine addiction• Next to methamphetamine,* cocaine creates the
greatest psychological dependence of any drug. It stimulates key pleasure centres within the brain and causes extremely heightened euphoria.
• The addictive properties of cocaine are thought to be due to brain dopamine D2-receptor stimulation.
Once having tried, an individual may have difficulty in predicting the extent to which he will continue to use the drug.
Abusers are of upper class society peoples to enhance self image or improve professional performance.
• Its stimulant and addictive effects are thought to be primarily a result of its ability to inhibit the reabsorption of dopamine by nerve cells.
DSM- V1- Cocaine is often taken in larger amounts or over a longer period
than was intended.
2- There is a persistent desire or unsuccessful efforts to cut down or
control cocaine use
3- A great deal of time is spent in activities necessary to obtain
cocaine, use cocaine, or recover from its effects
4- Craving, or a strong desire or urge to use cocaine
5- Recurrent cocaine use resulting in a failure to fulfill major role
obligations at work, school, or home.
6- Continued cocaine use despite having persistent or
recurrent social or interpersonal problems caused or
exacerbated by the effects of cocaine.
7- Important social, occupational, or recreational
activities are given up or reduced because of cocaine
use.
8- Recurrent cocaine use in situations in which it is
physically hazardous.
Cocaine Tolerance Initially
Cocaine produces an intense high and may not cause an emotional depression when the drug wears off
As a result
The user may conclude that cocaine is harmless.With Repeated
use A craving as well as a tolerance for the drug develops.
The addict ends up "chasing a high" by taking ever-increasing amounts of cocaine more and more frequently. When the supply of cocaine is gone, the addict is left with an intense craving along with severe depression that may reach a suicidal level.
Cocaine Frenzy
Cocaine withdrawal• Those who use cocaine heavily or regularly find it
extremely difficult to stop and often suffer through serious withdrawal symptoms such as:
Severe irritability Excessive Chronic depression Eating disorder Paranoia Nausea/vomiting Lose of sex drive Diarrhea Insomnia Heart attack
Additives of cocaine1.Levamisole –used to adulterate cocaine because,Add bulk and weightAppear more pureStimulant effectPass street purity test2.Local anesthetics3.Phencyclidine4.Strychanine5.Thiamine
Test for cocaine1.Gold chloride test:Reagent-gold chloride in acetic acidSuspected material+one drop reagent---crystaline form appears2.Scott test: suspected material+5drops of cobaltthiocynate(shake)----blue colour develop at once
Management Acute cocaine poisoninga)Decontamination Gastric lavage with warm water containing KMno4-if taken orally.Nasal irrigation with NaCl if snuffedSurgical removal of cocaine packets in body packersb)General supportive care1.Maintan ABC2.Rapid cooling with ice water-for hyperthermia
3.For agitation-sedation with benzodiazepines(midazolam,diazepam),barbiturate,propofol.4.For hypoglycaemia-hypertonic dextrose5.For hypertension-direct acting vasodilator(nitroglycerine,nitropruside)c)Specific management Management of acute coronary syndromeWide complex dysrhythmias
Chronic cocaine poisoninga) Psychosocial Treatment lead to reductions in cocaine use by Motivational interviewing Cognitive therapy Behavioral therapy Supportive therapy o More intensive treatment.o More frequent visits.o Longer duration of treatment.o Cocaine Anonymous.
Behavioral Treatment oOne of behavioral therapy that is showing positive results in
cocaine addicted population is contingency management or
motivational incentives (MI).
oMI: is particularly useful for helping patients achieve initial
abstinence from cocaine and for helping patients stay in
treatment.
oCognitive behavioral therapy: is an effective approach for
preventing relapse.
Medications1- Cocaine Vaccine:
Is composed of a cocaine hapten conjugated to inactivated
cholera toxin B, resulting in the creation of a molecule
capable of stimulating an antibody response.
Cocaine vaccine that prevents entry of cocaine into the
brain holds great promise for reducing the risk of relapse.
2.Other possible medications include:
– Modafinil - blocks euphoria
– Propranolol - reduces stress
– Baclofen - reduces cue-craving
– Topiramate - relapse prevention
– Disulfiram - reduces alcohol use,
– Cocaine vaccine - blocks euphoria
11 Ways To Die From Cocaine Drug Addiction1.Acute hypertensive crises - quickly elevating blood
pressure - blows out a weak blood vessel in brain causing cerebral hemorrhage.
2.Hypertension chronic users may weaken blood vessels in their brain. Die from strokes or complications after.
3.Acute hypotension - no blood with oxygen to the brain causing an anaphylaxis - allergic reaction.
4.Status epilepticus - repeated convulsions - increased EEG activity.
5.C.N.S. Rebound - physical and emotional depression - depressed medullary/respiratory centers of the brain knock you OUT - this is the most common cause of cocaine death.
6. Hyperpyrexia - Cocaine can raise the body to an extremely high temperature. May feel cold on the outside. Shows bruising easily - temp 106 degrees (anal)7. Pulmonary insult - heat fumes and chemicals in lungs cause lungs to collapse.8. Paranoid miscalculation - accidental death due to delusions and hallucinations.9. Suicide - during post-cocaine depression10. Needle borne - infections from needle use.11. Allergic Reaction - anticholinesterase (enzyme) deficiency 10-20 mg. of cocaine will kill them - the drug never gets destroyed and recycles continuously throughout the body.
Medico-legal importance of cocaine1.Bromptons cocktail-mixture of cocaine+morphine(heroin)+chlorpromazine+alcohol,used for pain management in terminal illnes like cancer.2.Contaminated currency: paper money in all part of the world shows drug contamination. Due to-Handling during drug deals.Use of rolled note for snorting.Cross infectionServe as vector of disease if associated with infective agents.
5.Speedball:Hazardous IV use of heroin and cocaine (amphetamine) together.The combination when smoked is known as moonrocks.
6.Stereo shooting:A shot of heroin in one arm and cocaine in other.7.Toxicity due to additive.8.Driving under influence of cocaine- u/s185(b) of MVA ,1988.9.Controle of illegal coca plants with herbicides.10.Children of mothers who used cocaine during pregnancy have increased risk of SIDS.
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