Cocaine Flashcards
T/F: Cocaine is considered one of the 5 most addictive drugs in common use
T
What is the PK of cocaine?
- Absorbed from mucous membranes
- Onset: ~1 min
- Peak: ~5 min
- Effects persist: ~30 min
- T1/2 =. 50 min
- Hydrolyzed via serum esterase
- Major metabolite: benzoylecgonine
- Found in urine 2-5 days after a binge
- Partial hepatic demethylation and renal excretion
What does cocaine do in the peripheral nervous system?
Local anesthesia
* Blocks voltage-gated sodium channels
* Prevents depolarization of membranes and conduction of action potentials
What does cocaine do in the central nervous system?
Stimulation
* Blocks monoamine transporter (DAT, NAT, SERT)
* Blocks re-uptake of monoamine from synaptic cleft, thereby enhancing monoaminergic signaling
Brompton’s Cocktail
- An alcohol solution containing
- An opioid (morphine/heroin): analgesic
- Cocaine: Euphoriant
- Antiemetics
- Can be used to alleviate terminal pain
What are the CNS effects of cocaine?
- Used to produce feelings of intense euphoria, high energy, mental alertness
- Other effects can include irritability, paranoia, restlessness, tremors, vasomotor symptoms, seizures, respiratory, and cardiac suppression
What is the mechanism of the rewarding effect of cocaine?
- Blockade of DAT results in increasing dopamine concentrations in the nucleus accumbens (mesolimbic pathway)
What are the three characteristics of cocaine that promote abuse and addictive behaviors?
- Euphoria
- Strong reinforcement properties
- Rapid onset
What are some methods of abuse?
- Smoking (produces rapid and intense euphoria)
- Crack cocaine
- Intranasal
How often will cocaine abusers take the drug?
Every 30-40 min to maintain euphoria
What is the fatal dosage of cocaine?
1.2 grams
* Severe toxic effects have been noted from doses as low as 20 mg
What is the treatment for acute overdose?
- IV lorazepam
- IV nitrate (nitroprusside)
- Mechanical respiration may be necessary
To lower BP, slow HR, and maintain breathing
