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PSYC 475 > FINAL EXAM - RED STUFF > Flashcards

FINAL EXAM - RED STUFF Flashcards

1
Q

What is the difference between Dependence and Abuse.

A

Dependence

Tolerance
Withdrawal
Taken in larger amounts (over time) than initially
Desire or effort to cut down or control use
Great deal of time spent
Other activities are given up
Use is continued despite knowledge of problems created by usage

Abuse

Maladaptive pattern of use leading to clinically significant impairment or distress characterized by one or more of the following (12 months)
A failure to fulfill major role obligations (work, school, home)
Use in physically hazardous situations
Legal problems
Continued use despite recurrent social/interpersonal problems

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2
Q

What does Agonist Substitution mean?

A

Does not necessarily cure the addiction, but often improves outcomes for patient and communities
Tend to have longer half-lives
Opiates – Methadone (dolophine)
Nicotine – patches, gum, lozenges, bupropion (Zyban)
Stimulants – modafinil (Provigil)

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3
Q

What does partial agonist substitution mean?

A

Provide a level of receptor stimulation that prevents cravings, but does not induce abuse
Opiates – buprenorphine (Butrans)
Longer half life than Methadone
Often combined with an opiate antagonist such as naloxone (Narcan)
Nicotine – varenicline (Chantix)
Stimulants – aripiprazole (Abilify) ?

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4
Q

What does Agonists mean?

A

Block receptors stimulated by the abused drug so that taking the drug no longer has an effect.
Pxt non-compliance is the biggest problem
Opiates – naloxone (Narcan), naltrexone (Revia), nalmefene (Revex)
Alcohol – naltrexone
Cannabis – rimonabant (Accomplia)

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5
Q

What does withdrawal maintenance mean?

A

Easing withdrawal symptoms can make a pxt less likely to relapse
Opiates/Alcohol – clonidine (Catapres), lofexidine (Britlofex; not currently available in US)
Alpha-2-adrenergic agonists
Ease sympathomimetic withdrawal symptoms
Stimulants – propanolol (Inderal)
Beta-adrenergic antagonists (beta blockers)

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6
Q

What does Mesolimbic DA regulation mean?

A

Blocking DA receptors does not seem to work.
Increasing DA does seem to be beneficial
bupropion (Zyban/Welbutrin)
Antabuse (blocks β-hydroxylase)

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7
Q

What are some NT system regulations?

A

Just as certain drugs stimulate the mesolimbic DA system through other NT systems, those systems can be targeted in an attempt to modulate the DA system.
Glutamate
NMDA agonists; D-cycloserine (DCS), N-acetyl cysteine
GABA
GABAB agonists; baclofen (Lioresal)
Anticonvulsants; vigabatrin (Sabril), tiagabine (Gabitril)
Norepinephrine
Beta receptor antagonists; propranolol (Inderal)
Opioid
Mu receptor antagonists; naltrexone (Revia)
Cannabinoid
Endocannabinoid system interacts with endorphin system
rimonabant (Accomplia)

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8
Q

What’s the difference between Acute versus Chronic pain?

A

Acute

Tissue damage
Injury
Surgery
Serves a useful purpose
Helps to avoid further injury by limiting activity in a productive way
Helps to avoid future injuries by enhancing perception/learning/memory

Chronic (+3 Months)

Not immediately associated with tissue damage
Fibromyalgia
Chronic fatigue syndrome
Back pain
Depression
Anxiety
Does not serve a useful purpose
Limits activity in a non-productive manner
Does not heighten perception or learning

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9
Q

What are NSAIDS?

A

Nonsteroidal anti-inflammatory drugs (NSAIDS)

Diverse molecules
Peripheral site of Action
Inhibit release of Prostaglandins
Inhibit Cyclooxygenase (COX)
COX inhibitors
“Ceiling” where increased doses do not increase pain relief
Aspirin, Ibuprofen (Advil, Motrin), Phenylbutazone (Butazolidine), Diclofenac (Voltaren), Indomethacin (Indocin), Ketorolac (Toradol), Naproxen (Aleve, Naprosyn), Celecoxib (Celebrex), Refecoxib (Vioxx), Valdecoxib (Bextra)

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10
Q

What are COX Inhibitors?

A

Inhibition of COX-1
GI upset, ulcers, kidney disease
Anticoagulant
Can reduce risk of heart attack and stroke
80-160mg/day*
Durlaza
Inhibition of COX-2
Reduction of inflammation
Pain relief
Fever relief (antipyretic)
Aspirin, Acetaminophen (Tylenol), Ibuprofen (Advil), Indomethin (Indocin), Sulindac (Clinoril), Ketorolac (Toradol), Diclofenac (Voltaren), Nabumetone (Relafen), Naproxen (Aleve), Meloxicam (Mobic), Oxaprozin (Daypro), Piroxican (Feldene), Tolmetin (Tolectin)

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11
Q

Name three NSAIDS

A

Aspirin, Ibuprofen (Advil and Motrin), Naproxen (Aleve, Naprosyn).

“Ceiling” where
increased doses do
not increase pain
relief

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12
Q

What are the CNS mechanisms for Opioid analgescis?

A

CNS mechanisms
Endorphins
Natural ligands
Opiates
Derived from opium poppy
Opium, heroin, codeine, morphine
Opioids
Anything exogenous that binds to opiate receptors and stimulates
Synthetic, semisynthetic, natural

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13
Q

What are some pure agonists opioids?

A

Binds to opiate receptors and stimulates
Affinity determines potency
Morphine, Codeine, Heroin (3x), Hydromorphone (6x; Dilauded, Palladone, Exalgo), Oxymorphone (10x), Meperidine (.1x), Methadone, Levo-alpha acetylmethadol (LAAM), Oxycodone (Percodan, OxyContin), Propoxyphene (Darvon), Fentanyl (80x; Sublimaze)

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14
Q

What are the alcohol pharmacokinetics? *****

A

ROAs: oral
**Absorption: water and lipid soluble (but does not tend to stay in fat), GI tract, rapid
Bioavailability: Excellent
Peak times: 30-90 minutes, depending on stomach contents
Distribution: concentration dependent on water content
**Half-life: varies, dependent on several factors:
size and weight
individual metabolism rate
related food intake
the specific beverage consumed
Women metabolize less ethanol than men
Less gastric metabolism
Less blood (less muscle)
More fat (alcohol concentrates in plasma)

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15
Q

What are Sedative Hypnotics?

A

Hypnotics: Agents that induce sleep
Pharmacologic effects are dose related
small doses: sedation
medium doses: hypnosis (sleep)
larger doses: loss of sensation (anesthesia)
Hypnotics are usually anxiolytic
But not all
Most common cause of insomnia!

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16
Q

What are sedative hypnotics that are GABA agonists?

A

Barbiturates
Amytal, Alurate, Butisol, Nembutal, Luminal, Seconal, Latusate
Low safety index
Non-barbiturate sedatives
Doriden, Placidyl, Noludar, Noctec
Same safety index problems as barbiturates but with shorter half-lives
BZDs
Dalmane, Dormalin, ProSom, Restoril
Fairly rapid onset
12-80 hr half-life
**Active metabolites
Halcion, Versed, Rohypnol
Rapid onset
2-3 hr half-life
No active metabolites
**Amnestic effects ED50 lower than somnolent ED50
Low toxicity
Unless combined with other GABA agonists (ALCOHOL)

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17
Q

What are psychedelics?

A

-Hallucinogens
-Alterations in perception, mood, cognition
-Used in many cultures
Religious rituals, spirituality
-Types
Anticholinergic
**Scopolamine; ACh antagonist
Natural sources: belladonna, datura, mandrake, moonflower
**Sometimes found in motion-sickness preparations

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18
Q

What are catecholaminelike?

A

Enactogens
Combined stimulant and psychedelic effects
Increased energy, sociability, hyperthermia, increased blood pressure, tachycardia
Hallucinations
**DA, NE and 5-HT agonists
-OCH3 (methoxy) addition to phenyl ring
Mescaline
Myristicin, Elemicin
Found in nutmeg and mace, respectively
Synthetics
Derived from amphetamine
DOM, MDA, MDE, TMA, AMT, 50MeO-DIPT,
**MDMA (hyperthermia; increases release of DA, NE, 5-HT via reuptake mechanism)

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19
Q

What are adverse effects for psychedelics?

A

“Bad trip”
Paranoia, anxiety
Damage to oneself or others
**“Set and Setting”
The context of the experience has a tremendous impact on the quality of the experience
**Flashbacks
Hallucinogen Persisting Perception Disorder
Exacerbation of existing psychosis or emotional disturbance

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20
Q

What is the #1 cause of acute liver failure?

A

Acetamineophen -> metablized in the liver.

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21
Q

Don’t take ___ after a hangover

A

Tylenol

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22
Q

What are non-specific COX inhibitors?

A

Indomethin (Indocin)
– Pain, fever, inflammation
* Rheumatoid arthritis
**– Increased side-effect liability
* GI upset, headache (?)
* Sulindac (Clinoril)
– Similar to indomethin
– Active metabolite = sulindac sulfide
**– Less GI upset than indomethin

Diclofenac (Voltaren)
– Pain, inflammation
* Arthritis, menstrual pain
– Half-life = 2 hrs
**– Several preparations: delayed release,
topical, skin patch
* Nabumetone (Relafen)
– Pain, inflammation
* Arthritis
– Less GI upset vs. aspirin
**– Recommended for long-term txt

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23
Q

What are COX-2 Inhibitors?

A

Celecoxib (Celebrex)
– Pain, inflammation
– Rheumatoid arthritis,
osteoarthritis
– Low liability for GI upset
***– No cardioprotective
effects
** May actually increase
risk
– May reduce risk for
certain cancers (colon,
breast)
21

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24
Q

What are the side effects of Morphine?

A

Side Effects: respiratory
depression, pupillary
constriction, constipation,
decreased sex drive/fertility
problems, itching

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25
What is Codeine?
Commonly prescribed to manage mild- moderate pain and coughs – Often combined with aspirin or acetaminophen (Empirin, Tylenol with codeine) * Analgesia, euphoria, addiction * Usually taken in tablet or liquid form – Also available i.v. * Half-life = 3-4 hrs **** Metabolized to morphine (CYP 2D6) ***– SSRIs can block this transformation
26
What is Hydrocodone?
Hysingla ER, Zohydro ER **** Often mixed with acetaminophen: Vicodin, Norco **** Mild-Moderate pain, cough suppression * ROA: oral 31
27
What is the tolerance for Hydrocodone?
Tolerance/Dependence ***– Hydrocodone is one of the most frequently abused prescription drugs in the US (Covvery, 2015) – Should gradually taper dosage to avoid withdrawal symptoms – Abuse seen more with ER capsules/tablets
28
What is Heroin?
Heroin * Semi-synthetic **** Increased lipid solubility * Metabolized into morphine and monoacetylmorphine and excreted by kidneys **** 3X potency of morphine * Intense euphoria * Highly addictive
29
What is Hydromorphone/Oxymorphone?
* Dilauded/Numorphan * Semi-synthetic – Increased lipid solubility ***– 6-10X potency of morphine – Half-life = 2-3 hrs – Oral, i.v. – Palladone, Exalgo = extended release (once daily) * Analgesic efficacy = morphine * Less sedation, equal respiratory effects, lower risk of dependence * Mod-severe pain, cough, chronic pain **** Antihistamines, MAOIs may inhibit effects
30
What is Meperidine?
* Demerol * Synthetic – 1/10th potency of morphine – Half-life = 3-5 hrs – Oral, i.v., i.m., s.c. – Active metabolite = normeperidine; activating effects (tremor, delirium, seizures) **** Greater euphoric effects than morphine * Risk of dependence * Mod-severe pain, fast acting * Interactions with MAOIs, SSRI (serotonin syndrome)
31
What is the half-life of methadone?
24-36 hours
32
What is the half-life of Levo-alpha acetylmaethadol?
2.5 days. *** There is also an increased risk of risk effects
33
What is propoxyphene?
* Darvon, Darvocet (when combined with acetaminophen) * Synthetic – Weak agonist – Half-life = 3-7 hrs – Oral ***– Effects do not depend on metabolism; good choice for “poor metabolizers” – Less GI upset **** Lower risk of dependence * Chronic pain
34
What is Fentanyl?
* Sublimaze * Synthetic – ROA: i.v., oral, transdermal – 80-125mg/day for methadone maintenance – Half-life = 2.5min (i.v.), 6min (intranasal/mucosal), 3-12hrs (transdermal) – i.v. most common ***– 80-500X potency of morphine – Powerful respiratory depressants * Surgical pain (during and after) * Sometimes abused; very dangerous due to respiratory effects
35
What is Buprenorphine?
* Subutex * Semi-synthetic – 80-125mg/day for methadone maintenance – Half-life = 20-70 hrs – Oral **** Opioid dependency (suppresses craving, decreased euphoria) **** Suboxone; combination of buprenorphine and naloxone **** Txts opioid dependency without risk of abuse
36
Tapentadol is a ____ agonist and blocks ____?
Mu agonist + blocks NET
37
What is Pentazocine?
* Talwin * Synthetic – Half-life = 2-3 hrs – IV, IM * Weak mu antagonist, kappa agonist * Analgesia at low doses * Adverse effects include hallucinations **** Low risk of dependence or respiratory depression * Mod – severe pain, rheumatoid arthritis, fibromyalgia * Should not be taken with SSRIs (serotonin syndrome)
37
What is Naloxone?
* Narcan * Synthetic – Half-life = 1-1.5 hrs – IV, IM, intranasal * No effect on non-addicts, but blocks effects of opioids * Quickly induces withdrawal symptoms **** Reverses respiratory depression caused by opiate OD * Can also be used in newborns * Nalmefene (Revex) ***– Similar to naloxone, but lasts longer – Used primarily for opioid OD
38
What is Naltrexone?
* Trexan * Synthetic – Half-life = 4 hrs – Oral * No effect on non-addicts, but blocks effects of alcohol and opioids * Must be taken daily; a s.c. ROA has been developed **** Used to txt opioid and alcohol dependence
39
What is Methylnaltrexone/Alvimopan?
* Relistor/Enterg * Synthetic – Oral, IV, SC **** Do not cross BBB, so only peripheral effects * Primarily used to reduce constipation, especially in pxts on opioid txt * May also be useful as an antiemetic
40
What is formication
the feeling of insects crawling on one’s body or under one’s skin
41
What is the primary indication for Meridia?
Obesity
42
What is the primary indication for Provigil?
Narcolepsy, shift- work sleep disorder, sleep apnea
43
___% of all fatal car accidents is due to alcohol
50%
44
What is the absorption of alcohol? (pharmacokinetics)
water and lipid soluble (but does not tend to stay in fat), GI tract, rapid Women metabolize less ethanol than men (it's constant over time)
45
What is the half-life of alcohol? (pharmacokinetics)
Half-life: varies, dependent on several factors: – size and weight – individual metabolism rate – related food intake – the specific beverage consumed
46
What's the toxicity for alcohol?
*****Respiratory depression * Organ failure – Acetaldehyde and acetic acid * Thiamine deficiency can prevent metabolism
47
What is liver damage for alcohol?
Liver damage – Hepatitis/cirrhosis – 75% of alcoholism deaths – 12th cause of death in US (CDC, 2015 data)
48
How does Antabuse and Temposil maintain abstinence from alcohol?
blocks metabolism, allowing acetaldehyde build-up.
49
How does Vivitrol/REvia (naltrexone) maintain abstinence from alcohol?
blocks opioid receptors, decreases reinforcing value of alcohol
50
How does Campral (acamprosate) maintain abstinence from alcohol?
****GABA agonist/glutamate NMDA antagonist – 2mg/day, 18 hr half-life, best when combined with naltrexone and/or psychotherapy
51
How does Wellbutrin (buproprion) maintain abstinence?
DA agonist, especially good when pxts are also depressed
52
How does Serotonin agonists maintain abstinence?
SRIs, 5-HT1A, 5-HT3; best for pxts who started drinking later and less psychopathology
53
How does Chantix (varenicline) maintain abstinence?
nicotinic partial agonist
54
How does Accomplia (rimonabant) maintain abstinence?
cannabinoid antagonist
55
Flurazepam (Dalmane)
More effective the longer you take it due to accumulation of active metabolite with long half-life
56
Triazolam (Halcion)
Best for sleep-onset insomnia
56
Flunitrazepam (Rohypnol)
amnestic
56
Non-benzodiazepine BZRAs
lower risk for dependence
57
What is the distribution (pharmacokinetics) for Cannabinoids?
lipid-soluble, concentrated in fat
58
What receptor is the most populous in the brain for cannabinoid receptors?
CB1; central
59
What are the effects of cannabis?
CNS – Motor * Impaired coordination – Some evidence it can improve coordination in pxts with movement disorders * Reaction time ****– 2-5ng/ml plasma associated with increased auto accidents (i.e. you might not feel effects!)
60
What is a common withdrawal symptom from cannabis?
irritability
61
What's the toxicity for cannabis?
none known for humans
62
What is the primary indication for Rimonabant?
***Primary Indication – Adjunct to diet and exercise in the treatment of obese patients with associated risk factors, i.e. type 2 diabetes, dyslipidaemia – Marijuana dependence
63
What are the pharmacodynamcs for rimonabant?
***Inverse agonist for cannabinoid receptor CB-1 * Reduces appetite
64
What does "set and setting" for psychedelics mean?
Set and Setting” ***– The context of the experience has a tremendous impact on the quality of the experience – Flashbacks * Hallucinogen Persisting Perception Disorder
65
Catecholaminelike
DA, NE and 5-HT agonists
66
Myristicin and Elemicin
Found in nutmeg and mace
67
Methylated Amphetamines
Very potent, highly toxic
68
What's a MAJOR adverse effect for MDMA
hyperthermia
69
what does MDMA do?
increases of DA, NE, 5-HT, via reuptake mechanism
70
Ketamine
No bp or respiratory effects
71
Dextromethrophan
opiate derivative
72

PSYC 475 (7 decks)

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