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Ihab Abdallah
Under Supervision: Dr. Mayada Wazaify
References
1- drugabuse.gov
2- Uptodate

3- National Institute of Drug Abuse (NIDA).
• Cocaine
(Benzoylmethylecgonine)
Is a crystalline alkaloid prepared from the leaves of the
Erythroxylon coca plant

.
Cocaine

Crystalline

Odorless

White

Bitter
NIDA
According to the National Institute of Drug Abuse
(NIDA)

Cocaine

A powerfully addictive drug that can be
Snorted

Injected

Chewed

Smoked
Cocaine ( Schedule II )

The 2nd Harmful Drug
COCAINE ( SCHEDULE I )
Form’s of Cocaine
Cocaine HCL (powder)

Prepared by dissolving the alkaloid in hydrochloric
acid, forming a water soluble salt.
Crack Cocaine
Produced when cocaine hydrochloride is mixed with
sodium bicarbonate and water, and then heated.
Must Watch
• Video
Route of Administration
Cocaine can be administered as a drug of abuse in
the following ways :
1. Cocaine hydrochloride:
 Snorting (intranasal)

 Intravenous injection
Route of Administration
2. Crack Cocaine:
Inhalation of vapor from heated foil or pipe. (Smoked)

3. Coca leaves:
Chewed or ingested.
Comparison
Route

Onset of Action

Duration of Action

Smoking

7 seconds

20 minutes

Intravenous injection

15 seconds

22-30 minutes

Snorting

3 minutes

45-90 minutes

Oral

10 minutes

60 minutes
Brain Storming
The most common cause of Recurrent
Epistaxis in young adult is ???

3

2
Cocaine use

Ref: USMLE

1
Mechanism of Action
Mouse Party
Clinical Usage
 Cocaine is used by health care professionals to

temporarily numb the lining of the mouth, nose, and
throat (mucous membranes) before certain medical
procedures (biopsy, stitches, wound cleaning).

 It is an anesthetic that works quickly to numb the
area about 1-2 minutes after application.
Cycle of Addiction
Reward System
Cocaine
Dependence

Cocaine Addiction
(Craving)

(Anhedonia)

Inability to feel
pleasure

Cocaine
Release of the impulses from NA to activate the reward system
Craving

This pathway activated also in the absence of cocaine
Metabolism
• 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.
Short Term Effect
Initial Dose
Physical Effect

Psychological Effect

Tachycardia

Euphoria

Dilated pupils

Sense of well being

Sweating

Impaired reaction time

Reduced appetite

Impaired attention span

Reduced need for sleep

Impaired learning of new skills

Reduced lung function
Short Term Effect
Increased Doses
Physical Effect

Psychological Effect

Seizures

Anxiety, Irritability, Insomnia

Cardiac arrhythmias

Depression, Paranoia

Myocardial infarction

Aggressiveness, Impulsivity

Stroke

Delusions

Respiratory arrest

Agitated, Excited delirium
Reduced psychomotor function
Long Term Effect
Physical Effect

Psychological Effect

Erosions, necrosis

Dependence

Rhinorrhea and nasal eczema

Disturbed eating

Chest pain, muscle spasms

Disturbed sleeping patterns

Sexual impotence
Weight loss
Malnutrition
Vascular disease
Specific Organ Systems
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.
Central Nervous System
o Cerebral vasoconstriction, cerebrovascular disease, and

hemorrhagic and ischemic stroke are increased in
cocaine users.
o MRI, PET imaging in chronic cocaine users demonstrate
structural and functional brain abnormalities.
Central Nervous System
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.
Central Nervous System
o Cocaine use is associated with a variety of movement

disorders:
Stereotyped Behaviors

Choreoathetosis

Buccolingual Dyskinesia

Tourette’s Syndrome

Acute Dystonic Reactions

Akathisia (Crack Dancers)

• Cocaine users are at increased risk of acute dystonic
reactions from neuroleptic (antipsychotic) medications.
PET

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, oropharyngeal ulcers.

Why ??

Due to vasoconstriction and resulting ischemic
necrosis.
Respiratory System
o Smoked cocaine use produces acute respiratory symptoms in

up to half of users.
Including
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 being the most frequent symptom.

Cocaine

By

increasing

adrenergic

activity in the heart, and
• Increase HR
• Increase BP
• Increase SVR

indirectly via the CNS.
Cardiovascular System
 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.
Cardiovascular System
 Chronic use is associated with left ventricular hypertrophy,
cardiomyopathy, myocardial fibrosis, and myocarditis.
DSM V
1- 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.
9- Tolerance.
10- Withdrawal.

≥2
10
Cocaine Tolerance
Initially

o 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

o A craving as well as a tolerance for the drug develops.
Cocaine Tolerance
• Over time, the high produced by a given amount of

cocaine decreases while the depression when the drug
wears off deepens.
• 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
o As tolerance to cocaine develops, an increased susceptibility

to seizures and psychosis also develops.
• An extreme form of this reverse tolerance can be called

• The person in a cocaine frenzy displays psychotic and
violent behavior, panic, and superhuman strength.
HIV & Hepatitis B and C
o Cocaine abusers are at increased risk for contracting such
infectious diseases as

and

.

o This risk stems not only from sharing contaminated needles
and drug paraphernalia but also from engaging in risky

behaviors as a result of intoxication.
o Potentially lead to risky:
1-sexual encounters

2- Needle sharing

3-Trading sex for drugs—by both men and womens.
HIV & Hepatitis B and C
o Hepatitis C

has spread rapidly among injecting drug

users.
o Risk begins with the first injection, and within 2 years,
nearly 40% of injection drug users (IDUs) are exposed to

HCV.
o By the time IDUs have been injecting for 5 years, their
chances of being infected with HCV are between 50-80%.
Pregnancy
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.
Brain Storming
Why baby look like this ???

3 2 1
Crack Baby !!!!

A baby who is not strong and healthy at
birth and whose mother used crack
cocaine while she was pregnant.
Treatment
Psychosocial Treatment
lead to small reductions in cocaine use
BY:
Motivational
interviewing

Psychodynamic

Cognitive
therapy

Behavioral
therapy

Supportive
therapy
o More intensive treatment.

o More frequent visits.
o Longer duration of treatment.
o Cocaine Anonymous.

Associated with better outcomes
Behavioral Treatment
o One of behavioral therapy that is showing positive results

in cocaine addicted population is contingency management
or motivational incentives (MI).
o MI: is particularly useful for helping patients achieve initial

abstinence from cocaine and for helping patients stay in
treatment.
o Cognitive behavioral therapy: is an effective approach for
preventing relapse.
Medications
1- 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.
Medications
2- Others:
Disulfiram
Vigabtrin

Modafinil

Tiagabine
Topiramate

Show promise and have been reported to
reduce cocaine use in controlled clinical trials.
Cocaine

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Cocaine

  • 1. Ihab Abdallah Under Supervision: Dr. Mayada Wazaify
  • 2. References 1- drugabuse.gov 2- Uptodate 3- National Institute of Drug Abuse (NIDA).
  • 3. • Cocaine (Benzoylmethylecgonine) Is a crystalline alkaloid prepared from the leaves of the Erythroxylon coca plant . Cocaine Crystalline Odorless White Bitter
  • 4. NIDA According to the National Institute of Drug Abuse (NIDA) Cocaine A powerfully addictive drug that can be Snorted Injected Chewed Smoked
  • 5. Cocaine ( Schedule II ) The 2nd Harmful Drug
  • 7. Form’s of Cocaine Cocaine HCL (powder) Prepared by dissolving the alkaloid in hydrochloric acid, forming a water soluble salt. Crack Cocaine Produced when cocaine hydrochloride is mixed with sodium bicarbonate and water, and then heated.
  • 9. Route of Administration Cocaine can be administered as a drug of abuse in the following ways : 1. Cocaine hydrochloride:  Snorting (intranasal)  Intravenous injection
  • 10. Route of Administration 2. Crack Cocaine: Inhalation of vapor from heated foil or pipe. (Smoked) 3. Coca leaves: Chewed or ingested.
  • 11. Comparison Route Onset of Action Duration of Action Smoking 7 seconds 20 minutes Intravenous injection 15 seconds 22-30 minutes Snorting 3 minutes 45-90 minutes Oral 10 minutes 60 minutes
  • 12. Brain Storming The most common cause of Recurrent Epistaxis in young adult is ??? 3 2 Cocaine use Ref: USMLE 1
  • 15. Clinical Usage  Cocaine is used by health care professionals to temporarily numb the lining of the mouth, nose, and throat (mucous membranes) before certain medical procedures (biopsy, stitches, wound cleaning).  It is an anesthetic that works quickly to numb the area about 1-2 minutes after application.
  • 16. Cycle of Addiction Reward System Cocaine Dependence Cocaine Addiction (Craving) (Anhedonia) Inability to feel pleasure Cocaine Release of the impulses from NA to activate the reward system Craving This pathway activated also in the absence of cocaine
  • 17. Metabolism • 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.
  • 18. Short Term Effect Initial Dose Physical Effect Psychological Effect Tachycardia Euphoria Dilated pupils Sense of well being Sweating Impaired reaction time Reduced appetite Impaired attention span Reduced need for sleep Impaired learning of new skills Reduced lung function
  • 19. Short Term Effect Increased Doses Physical Effect Psychological Effect Seizures Anxiety, Irritability, Insomnia Cardiac arrhythmias Depression, Paranoia Myocardial infarction Aggressiveness, Impulsivity Stroke Delusions Respiratory arrest Agitated, Excited delirium Reduced psychomotor function
  • 20. Long Term Effect Physical Effect Psychological Effect Erosions, necrosis Dependence Rhinorrhea and nasal eczema Disturbed eating Chest pain, muscle spasms Disturbed sleeping patterns Sexual impotence Weight loss Malnutrition Vascular disease
  • 22. 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.
  • 23. Central Nervous System o Cerebral vasoconstriction, cerebrovascular disease, and hemorrhagic and ischemic stroke are increased in cocaine users. o MRI, PET imaging in chronic cocaine users demonstrate structural and functional brain abnormalities.
  • 24. Central Nervous System 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.
  • 25. Central Nervous System o Cocaine use is associated with a variety of movement disorders: Stereotyped Behaviors Choreoathetosis Buccolingual Dyskinesia Tourette’s Syndrome Acute Dystonic Reactions Akathisia (Crack Dancers) • Cocaine users are at increased risk of acute dystonic reactions from neuroleptic (antipsychotic) medications.
  • 26. PET 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.
  • 27. 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, oropharyngeal ulcers. Why ?? Due to vasoconstriction and resulting ischemic necrosis.
  • 28. Respiratory System o Smoked cocaine use produces acute respiratory symptoms in up to half of users. Including 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.
  • 29. Cardiovascular System  Cardiopulmonary symptoms are the most frequent complaints in cocaine users who seek medical help, with chest pain being the most frequent symptom. Cocaine By increasing adrenergic activity in the heart, and • Increase HR • Increase BP • Increase SVR indirectly via the CNS.
  • 30. Cardiovascular System  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.
  • 31. Cardiovascular System  Chronic use is associated with left ventricular hypertrophy, cardiomyopathy, myocardial fibrosis, and myocarditis.
  • 32. DSM V 1- 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.
  • 33. 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. 9- Tolerance. 10- Withdrawal. ≥2 10
  • 34. Cocaine Tolerance Initially o 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 o A craving as well as a tolerance for the drug develops.
  • 35. Cocaine Tolerance • Over time, the high produced by a given amount of cocaine decreases while the depression when the drug wears off deepens. • 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.
  • 36. Cocaine Frenzy o As tolerance to cocaine develops, an increased susceptibility to seizures and psychosis also develops. • An extreme form of this reverse tolerance can be called • The person in a cocaine frenzy displays psychotic and violent behavior, panic, and superhuman strength.
  • 37. HIV & Hepatitis B and C o Cocaine abusers are at increased risk for contracting such infectious diseases as and . o This risk stems not only from sharing contaminated needles and drug paraphernalia but also from engaging in risky behaviors as a result of intoxication. o Potentially lead to risky: 1-sexual encounters 2- Needle sharing 3-Trading sex for drugs—by both men and womens.
  • 38. HIV & Hepatitis B and C o Hepatitis C has spread rapidly among injecting drug users. o Risk begins with the first injection, and within 2 years, nearly 40% of injection drug users (IDUs) are exposed to HCV. o By the time IDUs have been injecting for 5 years, their chances of being infected with HCV are between 50-80%.
  • 39. Pregnancy 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.
  • 40. Brain Storming Why baby look like this ??? 3 2 1 Crack Baby !!!! A baby who is not strong and healthy at birth and whose mother used crack cocaine while she was pregnant.
  • 42. Psychosocial Treatment lead to small reductions in cocaine use BY: Motivational interviewing Psychodynamic Cognitive therapy Behavioral therapy Supportive therapy
  • 43. o More intensive treatment. o More frequent visits. o Longer duration of treatment. o Cocaine Anonymous. Associated with better outcomes
  • 44. Behavioral Treatment o One of behavioral therapy that is showing positive results in cocaine addicted population is contingency management or motivational incentives (MI). o MI: is particularly useful for helping patients achieve initial abstinence from cocaine and for helping patients stay in treatment. o Cognitive behavioral therapy: is an effective approach for preventing relapse.
  • 45. Medications 1- 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.
  • 46. Medications 2- Others: Disulfiram Vigabtrin Modafinil Tiagabine Topiramate Show promise and have been reported to reduce cocaine use in controlled clinical trials.