Pharm - Psych - Substance Abuse

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Opioids - site of action and drugs (5)

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Mu receptors.

Heroin
Morphine
Oxycodone
Hydromorphone
Fentanyl

Tolerance doesn't develop uniformly and physical dependence occurs.

Front 2

Tx of opioid dependence

Back 2

Admin of an opioid antagonist precipitates acute abstinence syndrome (withdrawal)

Front 3

Withdrawal of opioids

Back 3

Not life-threatening

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Tolerance of opioids

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Minimal/no - miosis (constriction), constipation, convulsions. This is also seen with antagonist actions.

Moderate tolerance - Bradycardia

High tolerance - Analgesia, euphoria, dysphoria (in elderly), mental clouding, sedation, resp depression (this is why it helps with dyspnea), antidiuresis, N/V (goes away quickly), cough supp.

Front 5

2 regimens for opioid abuse tx

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withdrawal
need to go to hospital, need to be very motivated. only works for a small amt of time bc the change in brain/synaptic plasticity makes pt relapse.

maintenance

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Opioid agonist

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MAINT TX OF OPIOID ABUSE


Methadone - NMDA antagonist activity too.

Levo-a-acetylmethadol (LAAM) - can prolong QT interval.

So these two are mu receptor agonists.

No withdrawal bc very long acting

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Partial opioid agonist

Back 7

MAINT TX OF OPIOID ABUSE

Buprenoprhine - Can be combined with naloxone (mu antagonist) so that it isn't abused.

No withdrawal bc very long acting

Buprenorphine is probably better than methadone.

Front 8

Sedatives

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GABA A agonists

Benzodiazepines (e.g. Diazepam [Valium]) or barbituates

Lethal dose for chronic used close to that for non-chronic users.

Cross-tolerance to other hypnotics, anxiolytics and alcohol (all through GABA)

Front 9

Barbituates

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Not used medically that often.

e.g. phenobarbital

Induces high degree of tolerance and physical dependence. Strongly induces p450s

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Withdrawal from hypnotics

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From barbituates - Severe and life-threatening

With. from benzos - probably won't die - anxiety, agitation, inc sensitivity to light/sound, parasthesia, muscle cramps, myoclonic jerks, sleep dist, dizziness. And after high drug usage - seizures and delirium.

Front 11

Flumazenil

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Specific benzo receptor antagonist (so the GABAa receptor?) - good for tx of overdose or reversing effects of long acting benzos used in anesthesia.

Front 12

CNS stimulants

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Caffeine, nicotine, cocaine, amphetamines (e.g. methamphetamine (speed) and methylphenidate (Ritalin))

Action to release dopamine.

Tx - antipsychotics or antidepressants.

Front 13

Cocaine babies

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Immune dysfunction, simulated ADHD, long-term effects on learning.

Front 14

Caffeine

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Antagonist to adenosine receptors.

Mildly increase DA and NE.

Probably only causes physical dependence (e.g. morning HA) rather than being truly addictive.

Front 15

Hallucinogens

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Lysergic acid diethylamide, mascaline (cactus), psilocybin (mushrooms), MDMA (ecstasy), PCP, ketamine.

Act pretty diffusely.

TOLERANCE IS NOT PRODUCED. Synaptic plasticity isn't changed, so you don't need to keep taking the drug to feel ok.

People aren't sure what causes flashbacks.

Front 16

LSD - NT involved?

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Alters serotonin turnover.

Front 17

PCP receptors involved?

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sigma/NMDA receptors (this might be a subunit of the NMDA receptor...not quite sure).

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Marijauna

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Binds to cannabinoid receptors in basal ganglia, substantia nigra, globus pallidus, hippocampus, spinal cord, brain stem (very diffuse basically, as opposed to cocaine).

Active ing. - 9-tetrahydrocannabinol - causes dopamine release.

Endogenous ligand - anandamide.

Tolerance develops slowly to the high, but rapidly to any clinical benefit.

Front 19

CB agonists

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Pain management and increase in appetite.

Front 20

CB1 antagonists

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Tx of nausea, obesity.

Front 21

Marijauna effects

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Doesn't permanently change cells, but produces amotivational syndrome.

Safer in lungs compared to nicotine.

Front 22

When prepping a pt for surgery...

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be sure to ask about opioid use so they get proper pain management.

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Alcohol abuse

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Long-term use - better able to metabolize ethanol. Produces tolerance and physical dependence.

Withdrawal syndrome is similar to sedative-hypnotics (so it can be life threatening like barbituates, but usually not as bad)

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Disulfiram

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Tx of alcoholism

Inhibits aldehyde dehydrogenase so acetaldehyde accumulates and you start to feel sick with alcohol.

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Acamprosate (Campral)

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Tx of alcoholism

More used in Europe. Decreases glutaminergic transmission.

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Naltrexone or Vivitrol

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Tx of alcoholism

IM. Blocks release of endogenous opioids so motivation is reduced.

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Potential pharm target for alcoholism

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Deletion of N-type calcium channels because they change reward from alcohol and thus its consumption in mice.

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Nicotine

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Less powerful reinforcer than amphetamine or cocaine.

SE: hand tremor, change in EEG, N/V (initially), facilitates memory, reduces aggression, decreases weight gain. So it really is a performance enhancer.

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Tx of nicotine abuse

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Nicotine replacement therapy (gum, patches)

Bupropion (zyban) - reduces the feeling of stress when you are craving a cig. Inhibits NE and DA uptake.

Varenicline (Chantix)

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Varenicline (Chantix)

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Nicotinic receptor partial agonist. Binds nicotinic ACh receptors with higher affin than nicotine. Stimulation leads to release of DA which relieves craving and withdrawal sx.

SE: weight gain, N/V, constipation, insomnia, HA, suicide perhaps, heart arrythmias.

Suicide probably because you are blocking and stopping all that reward you used to have and it gives you really bad depression.

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Flunitrazepam

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AKA Rohypnol, roofies, rope, forget pill.

Potent benzodiazepine

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Gamma-Hydroxybutyric acid (GHB)

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AKA liquid ecstasy or scoop. A metabolite of GABA, CNS depressant, easy to synth., colorless, odorless,

GABAb agonist.

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Ketamine

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Special K, new ecstasy

Dissociative anesthetic, potentially fatal respiratory problems. Used by vets often.

NMDA antagonist.

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MDMA (Ecstasy)

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Methylene-dioxy methamphetamine

Rave culture. People often take a barbituate later to get to sleep.

Produces degeneration of serotinergic neurons in rats.

Can be used in binge use and not chronically.

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Rimonabant

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CB1 blocker used to stop cravings for a host of addictions.

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Vaccines may be promising for...

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cocaine.

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Quick recovery from opioid OD

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Naltrexone IV

because it is a mu-receptor antagonist and has long duration of action.