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Pharmacology > 37_Drugs of Abuse > Flashcards

37_Drugs of Abuse Flashcards

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1
Q

What is tolerance?

A

Used to a certain dose of a drug so have to increase the dose just to get the same effect.

This is an adaptive change to a drug

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2
Q

What is dependence?

A

When the drug dose decreases or starts wearing off, you get WITHDRAWAL symptoms

Adaptive change becomes maladaptive.

Formerly called physical dependence

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3
Q

What is addiction?

A

Compulsive relapsing drug use despite negative consequences

Formerly called psychological dependence

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4
Q

What pathway do addictive drugs use? What is it about this pathway that causes the drug to become addictive?

A

If a drug uses the mesolimbic dopamine system then it will become addictive

This pathway involves dopamine which is involved the rewarding of constructive behaviors
-drugs that increase dopaminergic tone in these pthwys INAPPROPRIATELY reinforce behaviors which can become compulsive

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5
Q

Not all drugs that use the dopamine pathway are addictive. What are these drugs?

A

Antipsychotics
Antidepressants
Anti-Parkinsonian

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6
Q

What is an opiate and what drugs are derived from it?

A

It is a naturally occurring analgesic alkaloid found in opium

Drugs
- Morphine, Codeine, many others

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7
Q

What is an opioid?

A

These are agents that produce opiate like effects &/o bind to opiate receptors

Natural Opioid: Its an Endorphin
Semi-Synthetic: Chemical modification of opiate (Oxycodone, Heroin)
Synthetic: Structurally different from morphine but has similar effects (Fentanyl, Methadone, Meperidine)

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8
Q

What are the Semi Synthetic Opioids?

A

Oxycodone, Heroin

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9
Q

What are the synthetic Opioids?

A

Fentanyl, Methadone, Meperidine

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10
Q

What is heroin AKA? what is the difference btwn heroin and morphine?

A

It is AKA diacetylmorphine

Two of the hydroxyl groups acetylated (morphine just has the two hydroxyl groups which make it more polar). The acetylation makes it more lipid soluble so it can cross the BBB. This causes stronger euphoriant effects

De-acetylation can occur spontanously

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11
Q

How do you use heroin?

A

The faster its gets into your brain, the better the euphoriant effects

PO: delay in absorption (opium eating)
Inhalation: Large respiratory surface area
Parenteral Injection: IV so 100% bioavailability

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12
Q

Describe IV Heroin use injection sites.

A

Most common are the injections into the Antecubital and forearm veins. They are superficial and easily accessible.

Track Marks

If these aren’t available or want to avoid them then use

Dorsum of foot btwn toes
Breast Veins
Penile Dorsal Vein

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13
Q

What are the alternate venous access sites for heroin use?

A

Dorsum of Foot btwn toes
Breast Veins
Penile Dorsal Veins

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14
Q

Describe Jugular vein access in heroin abuse

ie Pocket Shot & Shooting Gallery

A

Pocket shot is where there is an IV injection lateral to SCM and above clavicle to hit INTERNAL JUGULAR. Hold nose and do Valsalva maneuver so the IJ & EJ veins are dilated

Shooting Gallery is a place where you pay someone to give you a pocket shot

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15
Q

What is the risk for doing Pocket Shots

A 
Pneumothorax
Hematoma
Aneurysm
Infection
AV fistula
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16
Q

What is skin popping? who is this seen in? what are the risks of this?

A

When venous access not an option, so the drug is injected under the skin.

common in long term users, and get recurrent skin & soft tissue infections that leave cratered scars

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17
Q

What are the risks of parenteral Heroin Injection?

A

Overdose
Primary Infection
- Bloodborne, ie HIV, Hep B/C, Malaria
- Bacterial ie Endocarditis, Phlebitis (DVT, Aneurysm, Fistula), Local Skin & Soft Tissue Necrosis

Secondary Infection
- esp in Skin Poppers ie wound botulism, tetanus

Non Drug Effects

  • Pulmonary Talc microemboli
  • Cotton Fever
  • Contamination (Quinine, Strychnine, Atropine, Thallium, etc)
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18
Q

How is heroin inhaled?

What is chasing the dragon associated with?

A

Placed on foil heated with lighter or matches that liquefies into a glob (dragon)

Dragon moves around emitting vapors which move around and you chase and inhale through a straw

Chasing the dragon is associated with Leukoencephalopathy

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19
Q

Other Opioid Abuses

Meperidine…why is it not used as much anymore? What is the metabolite and what does it cause?

A

Not used as much bc drug seeking patients kept asking for it by name. Now they ask for dilaudid (hydromorphine)

Metabolite is normeperidine and is NEUROTOXIC
-causes agitation and seizures

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20
Q

Other Opioid Abuses

MPTP…What is it, and what drug what is it modeled after? What is it metabolized into and what effects does this metabolite have on the body?

A

It is a synthetic designer drug modeled on MEPERIDINE

Metabolized into MPP+ which KILLS DOPAMINERGIC CELLS IN THE SUBSTANTIA NIGRA…leads to Parkinsons Disease

These are called frozen addicts

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21
Q

What is the toxidrome of Opiate Overdose?

What does overdose mimic, i guess meaning, what other things could it look like?

A

Toxidrome:
CNS depression
Respiratory Depression
Miosis

Potential Mimics:
Hypoglycemia, Hypoxia, Hypothermia
Imidazoline Drugs: central a2 agonists
CNS Injury / Pontine Hemorrhage

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22
Q

How do you treat opiate overdose?

What is death most likely due to?

A

ABCs / supportive care

Antidote = Naloxone

  • Narcan which is a NARCotic ANtagonist
  • IV, IM, IN, nebulized, per ETT

Its short acting tho, need to observe for re-sedation

May bring about acute w/drawal so use smallest dose necessary

Overdose death most likely due to decreased ventilation

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23
Q

What are signs & symptoms of opioid w/drawal?

A 
Signs:
Pupillary Dilation
Sweating
Piloerection (goosebumps)
Tachy
N/V Diarrhea
HTN
Yawning

Symptoms
Cravings for Opioids
Restlessness, Irritability
Increased Sensitivity to pain
Nausea, cramps
Myalgia
Insomnia, Anxiety
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24
Q

Is Opioid Withdrawal life threatening?

A

Nope. Its just unpleasant

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25
How is opioid withdrawal treated?
Cross Tolerance - switch to a Rx opioid and gradually decrease the dose Clonidine: this is an a2 agonist used for HTN; reduces autonomic symptoms of withdrawal Activate endogenous opioids
26
How can Methadone deter opioid abuse?
Use Methadone Substitute long acting once daily methadone for multiple doses of illicit and more dangerous drug Have to monitor this so this is limited to accredited outpatient programs Patients can be weaned off methadone but many continue indefinitely
27
How can Naltrexone deter opioid abuse?
Naltrexone It competes for u-opioid receptor. Oral dosing or 30 day injection
28
How can Buprenorphine deter opioid abuse?
Buprenophine can be used w/ or w/o Naloxone If with Naloxone its called Suboxone. If w/o Naloxone its called Subutex Buprenorphine is a PARTIAL opioid agonist, and blocks heroin effects. There is a low potential for OD, tho and can get mild w/drawal No special treatment center required, but physician needs special qualification
29
How does ultra rapid opiate detox work? Why doesn't it work?
It induces acute severe opiate w/drawal while patient under general anesthesia It doesn't work bc patients suffer lots of w/drawal symptoms, does nothing to treat psych symptoms Some implant naltrexone while pt under anesthesia, but patients will try to dig them out
30
What does freebasing do to Cocaine?
It is converted into an uncharged molecule that can cross membranes easier, giving a more intense euphoric effect. Also, it doesn't burn up
31
How is cocaine freebased?
Dissolve the cocaine-HCl salt in water Add NaOH to raise the pH Heat over flame. this vaporizes off the organic solvent (base) until only freebase is left smoke and enjoy
32
What is crack cocaine and how is it made?
This is cocaine that has already been freebased, so there is no risk of immolation Called crack bc air pockets in crystals causes rocks to break with a cracking noise when heated
33
What is the MOA of Cocaine?
It works by blocking Nav channel - this produces a local anesthetic effect that has topical use as well (ENT, Ophtho, Laceration Repair) - For laceration repair, Tetracaine/Adrenalin/Cocaine (TAC) is used BioAmine Reuptake Inhibition of: - Dopamine, Serotonin, Norepi These levels are increased in the synapse so cocaine is an INDIRECT SYMPATHOMIMETIC
34
Describe the cardiotoxicity from cocaine use. What is used to treat this?
Wide QRS | Treat with wide complex tachydysrhythmias with NaHCO3
35
Describe the sympathomimetic Toxidrome and how you treat it. What should you monitor for?
``` Tachycardia HTN Mydriasis Diaphoresis Neurocognitive (Agitation, Paranoia, Delirium, Seizures) Hyperthermia (Bad sign!!) ``` ``` Treat: Supportive Care Reduce Hyperthermia IV Hydration Benzodiazepines (Reduce central sympathetic outflow) ``` Monitor for: Cardiotoxicity Rhabdomyolysis (prob from hyperthermia)
36
What is cocaethylene? What's significant about its toxicity?
This is produced when you do cocaine and drink alcohol Get an transesterification when cocaine and ethanol consumed together More cardiotoxic then cocaine alone
37
What drug class is amphetamine based on? What is it structurally similar to? Is it like cocaine? Does it bind adrenergic receptors?
Based on alpha-methyl phenyl amine Structurally similar to endogenous catecholamines No No
38
How does amphetamine work? | What is the only difference btwn clinical effects of amphetamine and cocaine?
Competitively inhibits biogenic amine re-uptake Prevents filling of presynaptic vesicles This causes even more inhibition of biogenic amine reuptake Amphetamine is an INDIRECT SYMPATHOMIMETIC Has same clinical effects and Tx as cocaine but difference is that Amphetamine does not block Nav channel.
39
Ecstasy AKA? Induces release of? Causes risk of what? What increases serotonergic effects?
AKA MDMA, its an amphetamine Induces release of ADH, and this can cause an increased risk for Hyponatremia Substitution on the phenol group of amphetamine increases the serotonergic effects -get feelings of empathy and intimacy, was used in psychotherapy, now at raves
40
Methamphetamine Whats the Rx Drug? what was it used for? What's the common base ingredient of meth and where can it be found?
Desoxyn - used for weight loss and ADHD (Pseudo)ephedrine found in cold medicine. Removal of the hydroxyl group from B carbon takes (pseudo)ephedrine to meth
41
What is mephedrone and MPDV?
These are latest methamphetamine trends that are fraudulently sold in head shops gas stations as "bath salts" or plant food - if not intended for human consumption then won't get in trouble
42
What is psychostimulant withdrawal?
Get cravings, but is there really a w/drawal syndrome??? still unknown Cocaine and Meth often used in binges til its all gone - Cocaine washed out syndrome: depressed mental status, normal labs, but this could be related to depletion of presynaptic NTs
43
Describe the signaling of endogenous cannabinoids?
Backward signaling - Released from POST synaptic membrane, diffuse across synapse, inhibit GABA or glutamate release
44
What are the clinical effects of cannabinoids?
Therapeutic: - Increased appetite, Decr N/V - Decreased IOP in glaucoma - Relief of Chronic Pain Medical Marijuana clinics Recreational: - Euphoria, Relaxation, Altered perception, Drowsiness, Conjunctival Injection, Paranoia
45
What are the concerns for Marijuana?
Gateway Drug - Not that bad by itself but can lead to using harder stuff "Amotivational Syndrome" Withdrawal - Mostly neurospychotic after abrupt cessation of chronic daily use
46
What is K2 & Spice?
These are latest in cannabinoid trends...synthetic cannabinoids, sold OTC at gas stations, head shops, etc
47
What are the agents of Sedative Hypnotics? What channel do they work through? What is the toxidrome?
There are several agents (EtOH, BZD, Barbs, etc) Most are cross tolerant Act through GABA Cl- Channels Toxidrome CNS Depression Normal VS except severe cases Pupils: normal but large in some
48
Is Sedative Hypnotic Withdrawal life threatening? What could happen as a result of withdrawal? Withdrawal symptoms with moderate and high dose usage?
Withdrawal from sedative addiction is potentially life threatening (in contrast to opiate withdrawal which isn't) Could get seizures / status epilepticus ``` W/drawal symptoms with MODERATE use Anxiety, Agitation Increased sensitivity to light and sound Parasthesias, strange sensations Myalgias, muscle cramps, myoclonic jerks Sleep disturbance, Dizziness ``` Withdrawal symptoms with High dose use Seizures Delirium
49
What is gamma hydroxybutyrate (GHB)? What is it structurally similar to?
It is an endogenous chemical structurally similar to GABA Investigated as general anesthetic, but has narrow safety margin and addiction potential Abused for the Euphoriant effects
50
How was GHB originally marketed and replaced with?
Marketed as dietary supplement in head shops. Then made illegal Replaced with GBL, then with 1,4-BD because both can be metabolized into GHB
51
What are the effects of GHB?
CNS Depression - Rapid onset and offset - Breathing preserved, even in coma - mild brady, myoclonic jerks may occur
52
What is a classic case of GHB overdose?
Brought to ED from party/rave comatose Intubated and awaiting ICU bed, then self extubates, and leaves hospital AMA
53
What are the therapeutic uses for GHB? What is the name of the therapeutic drug?
Drug is Xyrem or Na Oxybate Indication: Cataplexy (sudden transient muscle weakness while being conscious) or excessive daytime sleepiness due to narcolepsy Dose: take a dose, set alarm, fall asleep, wake up and take another dose
54
What does PCP and Ketamine have in common?
They are both dissociative anesthetic agents that are NMDA receptor antagonists
55
What is Ketamine used for? | What are the SEs?
Often used for procedural sedation - Sedation, AMNESIA, analgesia - Doesn't depress respiratory drive - Rapid On & Offset SEs - Tachy, HTN, Increased ICP - Nystagmus, Increased Oral secretions - Emergence Reactions (bad trips as patient wakes up)
56
What are the date rape drugs?
GHB, Roofies & Ketamine | Flunitrazepam aka Rohypnol is an intermediate acting benzodiazopene
57
Describe Inhalant Abuse? What molecule is inhaled? What are the three methods?
Molecules: Severa Hydrocarbons cause CNS effects when inhaled Sniffing: Open container and sniff it Huffing: Soak a rag and breath it Bagging: Put rag in plastic sack and put over ur head
58
What are the dangers of inhalant abuse?
Injury & Stupidity Sudden sniffing death - Halogenated hydrocarbons cause myocardium to be more sensitive to catecholamines. Increased risk for fatal tachydysrhythmias Neurotoxicity: - From several hydrocarbons, esp n-hexane
59
What is nitrous oxide and what is it used for? why is it abused? What deficiency does it cause?
N2O or laughing gass Used therapeutically for sedation / anesthesia Abused as euphoriant - source is whipped cream chargers Induces B12 deficiency - chronic abuse leads to neuropathy, degeneration of spinal cord that can improve with treatment, but rarely cured
60
Hallucinogens What psychological effects do they produce? Do they induce dependence or addiction? What effect do they have in the body?
Dpersonalization, altered time perception Does NOT induce addiction or dependence bc doesn't work thru mesolimbic enhanced dopamine release Enhance glutamate release in the cortex
61
Hallucinogen LSD is what kind of alkaloid? Potent or weak?
It is an Ergot alkaloid that is SEROTONERGIC very potent that only a little needs to be used, can be hard to detect on drug screens
62
Hallucinogen What is Mescaline, what does it resemble?
It is a substituted phenylethylamine that chemically resembles amphetamine. Pro-serotonergic This is Peyote, from peyote cactus
63
Hallucinogen What is Psilocybin
Mushrooms! Structurally similar to serotonin Found in over 200 mushroom species
64
What is the goal of nicotine replacement therapy?
To reduce withdrawal symptoms 20% abstinence rate at 12 mos
65
Nicotine Addiction Drugs How do these drugs work? SEs?
They are partial agonists at the Nicotinic Ach receptor - Cytisine - Varenicline They sit on nAChR on DOPAMINE NEUROMS preventing the nicotine reward effect SEs Mood Behavior Changes Increased CV risk
66
Nicotine Addiction Drugs What is Bupropion?
If it is for anti-smoking: Zyban | If it is for antidepressant: Wellbutrin
67
Nicotine Addiction Drugs What is Rimonabant? What is it used for originally? SEs?
It is an iverse agonist at the CB1 receptor Used for weight loss, but off label in US for smoking cessation SE: Depression / Suicide

Pharmacology (17 decks)

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