opioids Flashcards

1
Q

opium derivatives

A

morphine 10%

Codeine <1%

Thebaine

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2
Q

Harrison Narcotic Tax Act of 1914

A

US law that regulated and taxed the production, importation, and distribution of opiates. eventually was extended into modern drug laws.

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3
Q

US Drug Schedule I

A

No Medical use

LSD, MDMA, heroin

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4
Q

US Drug Schedule II

A

High abuse potential

amphetamine, morphine

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5
Q

US Drug Schedule III

A

Moderate abuse potential

ketamine, codeine

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6
Q

US Drug Schedule IV

A

Mild Abuse Potential

benzodiazepines

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7
Q

US Drug Schedule V

A

Low abuse potential

buprenorpine

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8
Q

semisynthetic Opioids

A
  • heroin (diacetylmorphine)

- hydromorphone (Dilaudid)

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9
Q

synthetic Opioids

A
  • Methadone (Dolophine)
  • Meperidine (Demerol)
  • Propoxyphene (Darvon)
  • fentanyl (innovar)
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10
Q

Endogenous opioids

A

enkephalins
endorphins
dynorphins

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11
Q

criteria for opioid agonist classification

A

Exerts effects similar to morphine

Acts at opioid receptors

Effects blocked by antagonist, Naloxone

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12
Q

Naloxene

A

Opioid antagonist
other name is narcan

  • reverses effects of opioid agonists
  • precipitates withdrawal in users
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13
Q

Naltrexone (Trexan)

A

long acting form of opioid antagonist

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14
Q

opioid administration

weak base

A
  • oral
  • parenteral
  • inhalation
  • intranasal
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15
Q

opioid administration

onset and duration of action

A

depends on preperation
route of administration
metabolism

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16
Q

opioid receptors

A

metabotropic, inhibitory

inhibits formation of cyclic amp

post synaptic inhibition - k+ Efflux

Presynaptic inhibition - transmitter release

Autoreceptor activation - less transmitter release`

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17
Q

presynaptic inhibition

A
kappa receptors
-
Ca++ channels close
-
Reduced transmitter release
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18
Q

Autoreceptor activation

A
Autoreceptors
-
Ca++ channels close
-
Reduced Transmitter release
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19
Q

endogenous opioids

A

endomorphin - Mu receptor

Enkephalin - Proenkephalin precursor - Mu, Delta receptor

Dynorphin - Prodynorphin precursor, Kappa receptor

Endorphin - POMC precursor - Mu, Delta receptor

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20
Q

opioid Acute effects

cortex

A

sedation
drowsiness
relaxation

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21
Q

opioid Acute effects

(Mesolimbic DA pathway_

A

Euphoria

22
Q

opioid Acute effects

Meulla

A

Pupillary constriction
Nausea, Vomiting
Cough Suppression
Respiratory Suppression

23
Q

opioid Acute effects

Hypothalamus

A

Hypothermia

Reduced Sexual Drive

24
Q

opioid Acute effects

many areas

A

analgesia

25
Q

opioid Acute effects

intestine

A

Constipation

26
Q

sites of opiod induced analgesia

A
Spinal
-sensation
Brain stem
-Sensation
Limbic, Thalamic and Cortical
-Perception
27
Q
opioid overdose
(central nervous system)
A

sleepiness

loss of consciousness

28
Q
opioid overdose
(Pupils)
A

Widening

29
Q
opioid overdose
(Skin)
A

Coldness
Clamminess
Blueness

30
Q
opioid overdose
(Muscular)
A

Seizures

31
Q
opioid overdose
(Breathing)
A

Slowed
Shallow
Stopped

occurs in medulla (pontine respiratory centers)

32
Q

opioid thereapeutic use

A
analgesia
anesthesia
substance abuse treatment
cough suppression
Reduce intestinal
33
Q

Opioid Tolerance

cellular

A

Pharmacodynamic

Decrease in opioid receptors
increase in adenylyl cyclase

34
Q

opioid tolerance

situational

A

contextual

context in which drug is taken
induces tolerance

35
Q

opioid physical dependence

A

withdrawal syndrome
opposite of acute effects
not life threatening
1 - 2 weeks in duration

36
Q

opioid psychological dependence

A

powerful reinforcer
intense craving, ‘rush’
increases release of dopamine in accumbens

37
Q

opioid acute and withdrawal effects

A

withdrawal effects are literally the exact opposite of acute effects

38
Q

Opioid pleasurability

A

they inhibit GABA neurons in the VTA which Disinhibit the dopamine system

39
Q

Drug therapies for opioid dependence

A

methadone

buprenorphine

naltrexone

Clonidine

Mixed Preperations

40
Q

Drug therapies for opioid dependence

methadone

A

full agonist administered daily, typical opioid effects but milder, reduces effects of heroin and morphine

41
Q

Drug therapies for opioid dependence

Buprenorphine

A

Partial agonist at mu receptors, typical opioid effects but milder, reduced risk of overdose, reduced intensity of withdrawal

42
Q

Drug therapies for opioid dependence

naltrexone

A

opioid antagonist blocks effects of opioids,precpitates withdrawal in users, blocks life threatening effects

43
Q

Drug therapies for opioid dependence

Clonidine

A

Noradrenergic alpha autoreceptor agonist, suppresses physical withdrawal symptoms during week of withdrawal

44
Q

Drug therapies for opioid dependence

mixed preperations

A

various combinations of medications are under study

45
Q

dealin drugs

A

people love dealin drugs, even when their not on heroine any more

46
Q

opioid overdose signs

A

Deep slow snoring or gurgling

Heavy nod, not responsive to stimulation - apply sternal rub (rub breastbone hard with knuckles)

slowed breathing

cyanotic - bluish lips and nail beds

-pinpoint pupils

47
Q

risks of opioid overdose

A

loss of tolerance

Mixing drugs

using alone

variation in strength of ‘street’ drugs

Serious illnesses

48
Q

risks of opioid overdose

loss of tolerance

A

increased risk after period of abstinence

49
Q

risks of opioid overdose

mixing drugs

A

mixing opioids with other drugs, especially depressants such as benzodiazepine or alcohol

50
Q

risks of opioid overdose

using alone

A

when using drugs alone there is no one present to see signs of overdose

51
Q

risks of opioid overdose

variation in strength of ‘street’ drugs

A

street drugs may vary in strength and effect based on purity of the drug and the amount of other ingredients used to cut the drug

52
Q

risks of opioid overdose

serious illnesses

A

AIDS, liver disease, diabetes and heart disease