Drugs of Abuse and General anesthetics Flashcards
- “Herbal marijuana alternative”
- Marketed as incense, “not for human
consumption” - Structurally dissimilar to THC but acts on
CB1 and CB2 receptors and possibly NMDA - 2 – 100 times more potent than THC
- Sprayed onto herbal mixture and smoked
Synthetic Cannabinoids (SC)
What receptors do the Synthetic cannabinoids act upon?
CB1 and CB2
Intake and Output
* No human evidence for ADME
* Anecdotal reports of onset and duration
* Onset within minutes
* Duration varies, average 1 hour
– May vary according to chemical type
* Available as either plant-based material to
be rolled and smoked, or as an oil to be
vaped.
Synthetic Cannabinoids (SC)
Effects
Euphoria
Anxiolytic
Stimulant
Dream enhancement
“Benefits”
Not detected in
standard urine drug
screen
Smells like incense
Sympathomimetic effects
Paranoia
Agitation
Seizure
Renal failure
Rhabdomyolysis
Difficult to distinguish from
primary psychiatric illness
Synthetic Cannabinoids (SC)
- Low dose (<10 mg)
– Methyphenidate - High dose (> 10 – 15 mg)
– Cocaine, methamphetamine - Onset ~ 30 minutes
- Dose-dependent duration (0-12h)
Methylenedioxypyrovalerone
(MDPV)
- Amphetamines, ecstasy, cocaine
- Average dose 100 – 200 mg
- Onset 30 – 45 minutes
- Short duration (1–2h)
- Strong desire to re-dose
4-Methylenemethcathinone
(Mephedrone)
Mechanism of ____
* Strong inhibition of dopamine,
serotonin, and norepinephrine
reuptake
* Also increases presynaptic release
Cathinones
____ effects
* Euphoria
* Heightened alertness
* Energy
* Talkativeness
* Libido increase
Agitation
Paranoia
Hallucination (audio, visual, tactile)
Sympathomimetic toxidrome
Seizures, hyperthermia,
hyponatremia, rhabdomyolysis
Cathinone
- ⍺-pyrrolidinopentiophenone (⍺-PVP)
– AKA: Gravel, $5 Insanity - Synthetic cathinone, structurally similar to
MDPV - Dopamine, norepinephrine reuptake
inhibition - Developed in the 1960’s by Boehringer-
Ingelheim, but never marketed
Flakka
What is tx for SC and cathinones?
BZDs
- 100x more potent than fentanyl
- 10,000x more potent than morphine
W18
– 8x more potent than morphine
– Fatalities reported
* Pulmonary edema
* Opioid toxidrome
U-47700
– 10,000x more potent than morphine
– 1kg = 50,000,000 fatal doses
* Grain of sand lethality
– Developed by Janssen 1970s
* Wildnil®
Who said the opioid crisis couldn’t get any worse? Gussow L. Emergency Medicine News. November 2016:29-30
Carfentanil
How do you treat non-pharmaceutical fentanyl effects?
Naloxone
Hypnotic, no analgesia
0.1 - 0.3 mg/kg IV
Each 0.1 mg/kg = 100 sec sedation
Onset within seconds
RSI gold standard, minimal use in
procedural sedation
Won’t control pain after procedure
Neutral hemodynamic profile
Myoclonic activity
EEG activity increased
Emetogenic
Etomidate
Inhibits 11β-hydroxylase
Cholesterol cortisol
Adrenal suppression
Etomidate
Midazolam
Most lipid soluble
Slower, unreliable, difficult to titrate
Better suited as anxiolytic
Great amnesia, no analgesia
BZD
What is the reversal agent for BZDs?
Flemazenil
GABA agonist
Quick on, quick off
Lipid emulsion
No analgesia
Propofol
Burns on administration
May give lidocaine (2 - 4mL of 1%)
Negative inotrope
Elderly, volume depleted, rate of
administration
Respiratory depression
Propofol
Similar to PCP
Less euphoria and sensory distortion
Dissociative anesthetic
Corticothalamic and limbic dissociation
Bronchodilation, airway reflexes
maintained
Ketamine
Multiple mechanisms
GABA
μ receptor agonist
Catecholamine reuptake inhibition
Cholinergic receptor antagonism in
prefrontal cortex
NMDA receptor antagonism
Ketamine
Indications
Sedation, analgesia, anesthesia
Seizure
Depression
Excited delirium
Opioid induced hyperalgesia
Opioid sparing treatment
Delayed sequence intubation
Adverse reactions
Sympathomimetic
Can be good or bad
Psychic phenomena
Emergence vs. dysphoria
Intracranial pressure
Ketamine
Ketamine + propofol
1:1 most common
20mL syringe; 10 mL propofol, 10 mL ketamine.
Note concentration!
Dosing, typically 0.5 mg/kg of each
component
0.1 mL/kg
Ketofol