Cocaine

Cocaine

Ihab Abdallah

Under Supervision: Dr. Mayada Wazaify

References

1- drugabuse.gov

2- Uptodate

3- National Institute of Drug Abuse (NIDA).

What is Cocaine

• Cocaine  (Benzoylmethylecgonine)

Is a crystalline alkaloid prepared from the leaves of the

Erythroxylon coca plant .Cocaine

White

Bitter Odorless

Crystalline

NIDA

According to the National Institute of Drug Abuse (NIDA)

A powerfully addictive drug that can be

Cocaine

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

2. Crack Cocaine: Inhalation of vapor from heated foil or pipe. (Smoked)

3. Coca leaves: Chewed or ingested.

Route of Administration

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

3 12

The most common cause of

Recurrent Epistaxis in young adult

is ???

Cocaine use

Ref: USMLE

Mechanism of Action Mechanism of Action

Mouse Party 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.

Reward System

Cycle of Addiction

Cocaine

Release of the impulses from NA to activate the reward system

This pathway activated also in the absence of cocaine Craving

Cocaine Addiction

(Craving)

Cocaine Dependence

(Anhedonia)

Inability to feel pleasure

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 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,

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 Central Nervous System

Central Nervous System 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 Central Nervous System

o 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

Acute Dystonic Reactions

Choreoathetosis

Akathisia (Crack Dancers)

Buccolingual Dyskinesia

Tourette’s Syndrome

PET 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

These effects are probably due to direct damage to the alveolar-

capillary membrane by cocaine or inhaled micro particles.

Productive Cough

Wheezing Exacerbation of

Asthma

Shortness of Breath Chest Pain

Hemoptysis

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

• Increase HR • Increase BP• Increase SVR

By increasing adrenergic

activity in the heart, and

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

o Cocaine produces an intense high and may not cause

an emotional depression when the drug wears off. 

The user may conclude that cocaine is

harmless. 

o A craving as well as a tolerance for the drug develops.

With Repeated use

As a result

Initially

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

“Cocaine frenzy"

• 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 HIV (AIDs) and viral

hepatitis.

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.

o Hepatitis C (HCV) 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%.

HIV & Hepatitis B and C

PregnancyPregnancy

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 StormingBrain Storming

Why baby look like this ???

 Crack Baby !!!!

A baby who is not strong and

healthy at birth and whose mother

used crack cocaine while she was

pregnant.

3 2 1

Treatment

Psychosocial Treatment

 lead to small reductions in cocaine useBY:

Motivational interviewing

Cognitive therapy

Behavioral therapy

Supportive therapy

Psychodynamic

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.

2- Others:

Medications

TopiramateVigabtrin

Disulfiram Modafinil Tiagabine

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

trials.