Cocaine Flashcards by Celina MacLeod

What are the 3 consumable forms of cocaine?

Coca leves
Cocaine hydrochloride (powder)
Free-base cocaine = crack

How well did you know this?

Not at all

Perfectly

How is cocaine powder absorbed?

Absorbed through mucous membranes

How well did you know this?

Not at all

Perfectly

What is the bioavailability of cocaine powder?

70%

How well did you know this?

Not at all

Perfectly

What does the dissolution of cocaine powder do?

Makes HCl which damages the nasal structures

How well did you know this?

Not at all

Perfectly

What is the onset and duration of cocaine powder?

Onset = 3-5 minutes
Duration = 30-40 minutes

How well did you know this?

Not at all

Perfectly

What is the onset and duration of crack?

Onset = 6-10 seconds
Duration = 5-30 minutes (intense)

How well did you know this?

Not at all

Perfectly

Why can we smoke crack but not cocaine?

Cocaine pyrolyzes before it vaporizes while crack does not

How well did you know this?

Not at all

Perfectly

What is the onset and duration of injecting crack?

Onset = 10-15 seconds
Duration = 10-20 minutes

How well did you know this?

Not at all

Perfectly

Which enzyme primarily metabolizes cocaine?

Liver CYP3A4

How well did you know this?

Not at all

Perfectly

Which major metabolite is produced by the hydrolysis of cocaine?

Benzoylecgonine (40%)
Spontaneously produced, non-enzymatic

How well did you know this?

Not at all

Perfectly

What do liver/plasma esterases generate while breaking down cocaine?

Ecgonine methylester (30-50%)

How well did you know this?

Not at all

Perfectly

What is the half-life of cocaine?

12 hours

How well did you know this?

Not at all

Perfectly

How long is cocaine detectable in urine?

4 days

How well did you know this?

Not at all

Perfectly

Where is cocaine distributed?

Brain
Spleen
Kidney

How well did you know this?

Not at all

Perfectly

What are the psychological effects of cocaine?

Euphoria
Arousal
Increased energy
Takes longer to fall asleep

How well did you know this?

Not at all

Perfectly

What are the effects of cocaine on the head?

Dry mouth
Headache

How well did you know this?

Not at all

Perfectly

What are the effects of cocaine on the heart?

Increased heart rate and blood pressure
Constricted blood vessels
Promotes blood clot formation

How well did you know this?

Not at all

Perfectly

What are the effects of cocaine on the skin?

Increased body temperature
Sweating

How well did you know this?

Not at all

Perfectly

What are the effects of cocaine on the lungs?

Increased respiratory rate
Dilated bronchi

What are the effects of cocaine on the digestive system?

Decreased appetite
Increased fat breakdown

What are the effects of cocaine on the reproductive system?

Hyper-sexuality

What are the anesthetic properties of cocaine?

Blocks Na channels which block neurotransmission so there is no pain

What are the sympathomimetic effects of cocaine?

Increased heart rate, blood pressure
Anorexia, insomnia, agitation, hyperthermia

How does cocaine affect the basal ganglia?

Repetitive, compulsive movements

How does cocaine affect the PFC?

Influences planning, problem-solving, and social behaviours

How does cocaine affect the NAc?

It is extremely rewarding

How does cocaine affect the medulla?

High doses can cause respiratory and circulatory failure

What are the physiological mechanisms of cocaine?

Blocks transporter activity within synapses Prolonged stimulation of post-synaptic nerves The aromatic ring and amine group mimics NTs

Where does excess DA build up from cocaine use?

In the basal ganglia, PFC, VTA, and NAc

What does excess 5HT from cocaine use underlie?

Mood, sleep, appetite, and temperature

What does excess NE from cocaine use underlie?

Sympathomimetic effects Enhances VTA sensitivity to Glu and reward

What are the adverse effects of acute cocaine use?

Irritability, hostility, anxiety, fear, depression Formication = delusion of bugs crawling under skin Depression, aggression, paranoia Increased acute infections in GI tract Nosebleeds Allergic reactions at injection sites

What does the reinforcing mechanism of cocaine involve?

Block of DA reuptake

Where does cocaine bind in the brain?

To the same site as dopamine (dopamine transporter) Locks the transporter in a stable conformation so dopamine cannot be reuptaken

Do exclusive DAT blockers mimic cocaine effects?

No, so not just DA is involved

What are the cocaine-induced mechanisms of tolerance?

Reduced euphoria caused by depleted DA and increased DAT efficiency Internalization of D1 and D2 receptors via rapid mechanisms Altered opioid-ergic signaling which induces striatal dynorphin expression

What are the symptoms of reverse tolerance?

Increased susceptibility to hyperthermia, convulsions, stereotyped movements

What is intermittent use of cocaine associated with?

Strong behavioural sensitization, increased locomotor activity

What are the symptoms of cocaine withdrawal?

Depression, anxiety, appetite changes Strong drug cue-associated cravings Long-term DAT efficiency increases so there is less dopamine in synapses causing episodes of depression

Cocaine and dependence

Mild physical symptoms Intense psychological symptoms due to hijacked reward pathway and cue association

Do most cocaine users become addicted?

No, anxiety or loss of motor control is not fun 10-15% of users that snort become addicted

How do benzos treat acute cocaine intoxication?

Control agitation and overstimulation Decrease BP, heart rate

How does nitroglycerine treat acute cocaine intoxication?

Evokes NO production to counteract vasoconstrictive effects Useful to supply heart with oxygen

how does an ice bath treat acute cocaine intoxication?

Cooling body temperature

How does butyrylcholinesterase treat acute cocaine intoxication?

Causes rapid elimination of cocaine

How does topiramate help maintain cocaine abstinence?

The anti-seizure med that enhances GABAa receptor activity and inhibits Glu receptor activity -reduce cravings

What are the long-term consequences of cocaine use?

Cardiovascular disease -arrhythmias, arrest due to inhibited Na channels Constricts vessels and organs can die if their blood supply is limited Psychosis accelerated brain aging Rhabdomyolysis breakdown of muscle tissue due to hyperthermia which releases myoglobinuria which causes kidney failure Increased stroke risk Brain shrinkage - enlarged ventricles and sulci