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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