Drug abuse 1 Flashcards
WV Stats
In West Virginia 8% of people over 12 have
used illicit drugs in the last month (Figures
from 2010-2012, National Survey on Drug
Use and Health)
– McDowell County has the 5th highest
rate of drug abuse for counties within
the US.
• In 2008, even though WV has approximately
the national average rate of drug abuse
(according to government statistics) we have
double the national average of drug
overdoses (2nd to only the Land of
Enchantment, New Mexico in 2008.
• In 2010, despite no change in national rate
(c.f. 2008) the rate of overdose death in WV
increased to 28.9 per 100,000 (#1 in US, CDC
state statistics), now leading cause of death
in WV.
Why are certain drugs addictive?
• Its all about mesolimbic
dopamine.
• Promotes pleasure
sensations
Drugs of abuse either directly or indirectly
increase DA levels within the nucleus
acumbens.
In general stimulants have a direct effect while
depressants are indirect via disinhibition
circuits:
Direct: Cocaine, Ampetamines
Indirect: Nicotine, Alcohol, Opioids, Benzos, Cannabinoids, PCP
Other brain regions are involved in the “craving” associated with addiction (PFC /
Hippocampus), and also the various withdrawal / negative effects associated with abuse
(Hypothalamus / Brain stem).
Prescription v’s street
• In the last 20 years drug abuse in the US has shifted from a street supply to pharmaceutical grade drugs largely via prescription diversion. • Many drug abusers believe prescription are safer. • The number of emergency visits for drug abuse has increased and this is largely due to increased use of pharmaceutical agents • Though new street drugs are constantly being designed – Bath salts, ecstasy, spice, krokodil, NBome.
Opioids
• All opioids are potentially drugs of abuse, strong
opioids are just better at it!
• Prescription use as pain killers
– Morphine, hydocodone, oxycodone, methadone
tramadol, fentanyl, carfentanil , loperamide
– As a class, most diverted and abused prescription
medications in USA.
• Street drugs
– Heroine, opium, krokodil
Opioids: Mechanism
Stimulate opioid receptors (mu, kappa, delta) in several areas of the mesolimbic reward
circuit
• opioid receptor activation can inhibit GABAergic transmission
• initially results in increased nucleus accumbens dopamine release
• euphoria
• Followed by a profound sense of tranquility and potentially drowsiness
Opioids: Effects at abuse
doses
Euphoria / Dysphoria, tranquility
Opioids: Overdose
• Depressed mental status, decreased respiratory rate, decreased tidal volume,
decreased bowel sounds, constricted pupils (though neither meperidine nor
propoxyphene constrict pupils).
• Can be complicated by hypothermia, coma, seizure, head trauma, aspiration
pneumonia and rhabdomyolysis.
Loperamide:
Poor man’s methadone 100 x therapeutic dose
OD gives dysrhythmia and prolonged QT, death from cardiac rather
than respiratory
Also check for needle tracks and skin popping
Opioids: Treatment: Emergent
Goal is to improve ventilation not mental status
• Ventilation
• IV or IM naloxone
• If respiratory depression remains give more naloxone as bolus
Opioids: Treatment: Maintenance
Methadone maintenance gold standard
• t1/2 24 to 36 hours
• Relieves opioid craving and withdrawal symptoms and when given in sufficient
doses, blocks the euphoric effects of opioids.
• Detoxification involves the use of tapering doses to achieve a smooth transition from
opioid use to a drug-free state.
IS AN OPIOID and can also be abused
Buprenorphine
• Partial Mu agonist Kappa antagonist
• can induce withdrawal abstinence for at least 24hr required prior to buprenorphine
• Oral with our without naloxone (Nal doesn’t cross gut – reduces abuse)
• Gradual taper to “wean “
Naltrexone:
• Antagonist
• Used for prevention of relapse
Opioids: Withdrawal
Physical exam:
• Pupil dilation
• Yawning
• Increased bowel sounds
• Hypotension (volume depletion due to diarrhea and vomiting)
Patient complains of:
• Dysphoria and restlessness (clonidine)
• Rhinorrhea and lacrimation
• Myalgias and arthralgias(NSAID of acetaminophen)
• Nausea, vomiting, abdominal cramping, and diarrhea (Loperamide)
Can treat these symptoms to ease withdrawal
Oxycodone (Dazidox, Oxycontin) “Hillbilly Heroin”
• Oxycodone (OxyContin) delayed release formulation
• Acts for 12 h (longest acting pain reliever on the market)
• Crushing pills and then swallowing, snorting or injecting leads to
heroin high
• Cheap
Remember Oxycodone can come in combinations with
other drugs
• Acetaminophen – potential liver issues
Heroin
• Diacetylmorphine metabolized to 6-monoacetylmorphine then morphine
• Both Diacetylmorphine and 6-monoacetylmorphine have higher BBB
penetration than morphine
• Effect due to both 6-monoacetylmorphine and morphine
• 6-monoacetylmorphine specific heroin metabolite detectable in urine tests
• Very rarely supplied pure, often cut with other stuff
Cheese Heroin
Street Names Nut job Muck Frown Slab
Mixture of Black Tar Heroin & Tylenol PM
Krokodil
The Living Dead: Why Thousands of
Russian Addicts Are Rotting to Death
There is a new drug in Russia, and addicts
are using it until their skin falls off.
Opioids plus gabapentin
• Very common in WV
• Gabapentin potentiates opioid action
(unknown mechanism)
• Means more bang for your buck
• Major issue in pregnant women, we have 50
ish confirmed NAS cases of opioid +
gabapentin (Dr. Loudin will talk about this)
