Opiates Flashcards

1
Q

what is morphine

A

refined active ingredient of the opium poppy

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2
Q

what is codeine

A

substitution of one group in morphine produces codeine
less analgesic effect but fewer side effects
potent cough supressant

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3
Q

what is heroin

A

derivative of morphine
3X as potent (more lipid soluble)
Addition of acetyl group increases oil water coefficient
Once inside the brain, acetyl groups are removed making morphine

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4
Q

what are characteristic opiate effects

A

dreamy, euphoric state, lessened sensation of pain, slowed breathing, constipation, pinpoint pupils

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5
Q

what is fentanyl

A

80x more potent than morphine
mostly used for anesthesia and neuropathic pain
similar effects to heroin but more potent

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6
Q

what is carfentanil

A

10,000x more potent than morphine
100x more potent than fentanyl
depressed the CNS and ability to breathe

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7
Q

what are the medical uses of opiates

A

relief of severe pain (analgesic)
treatment of acute diarrhea
cough suppression

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8
Q

what are the routes of administration for medical use of opiates

A

oral
transdermal
mucous membranes
intravenous

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9
Q

what are the routes of administration for recreational use of opiates

A

inhalation
mucous membrane
subcutaneous
intravenous

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10
Q

what is the distribution of opiates

A

high levels usually not present in the brain (except for heroin)

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11
Q

How are opiates excreted

A

90% of morphine in metabolized by liver and excreted as urine; 10% as pure morphine

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12
Q

what effects do opiates have on the PNS

A

constricts pupils
decreases GI motility
dilation of peripheral blood vessels
warm, flushed skin due to dilation of subcutaneous blood vessels
itchy skin (release of histamines)

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13
Q

what effects do opiates have on the CNS

A

Analgesic
-Actions in medulla suppress cough and decrease rate and depth of breathing
- Depresses release of NT associated with pain
Reduces “psychological” pain
-pain signals aren’t experiences as unpleasant
- Acts on the limbic system
Sedative effects
-depress neuronal firing rate

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14
Q

what part of the brain do opiates effect to produce the sedative/hypnotic effects

A

cerebral cortex

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15
Q

what part of the brain do opiates effect to produce the euphoric effects

A

limbic system/nucleus accumbens

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16
Q

what part of the brain do opiates effect to produce analgesic effects

A

brainstem, spinal cord, and thalamus

17
Q

what part of the brain do opiates effect to produce the respiratory depression, suppression of cough reflex, and nausea/vomiting

A

medulla

18
Q

what are the opiate receptors

A

mu
delta
kappa
- all metabotropic

19
Q

what happens when opiate receptors are activated

A

decrease in neuronal activity

20
Q

How do opiates produce euphoria

A

heroin is converted to morphine in the brain which acts on the mu and delta receptors expressed on GABA neurons; Reduced amount of GABA disinhibits the VTA causing increase of DA release

21
Q

what shows the fastest tolerance in opiate use

A

tolerance to euphoria effects

22
Q

what are effects of opiates that show little to no tolerance

A

constipation
pupil constriction

23
Q

what kinds of tolerance can you develop to opiates

A

Metabolic tolerance
- increase in liver enzymes
Receptor desensitization/down-reg.
Context Dependent tolerance
- likely to be attached to cue

24
Q

Describe dependence to opiates

A

both psychological and physical dependence can develop

25
Q

Describe physical dependence to opiates

A

serious and unpleasant withdrawal
intensity and duration of withdrawal directly correlated to intensity and duration of drug effects
withdrawal NEVER fatal on its own

26
Q

what are opiate withdrawal symptoms

A

6 hours: drug craving, anxiety, restlessness, agitation
12-14 hours: yawning, increased agitation, perspiration
14-16 hours: hot and cold flashes, goosebumps, tremors, muscle aches
24-36: stomach, back and leg cramps, uncontrolled movements of limbs, nausea and vomiting, sweating
36-48: fetal position, vomiting, diarrhea

27
Q

what are the leading factors in opiate overdose

A

1) concentration of drug bought on black market is high than the accustomed concentration
2) Patient abstains from use, relapses, then uses same amount before withdrawal
3) drugs in combination
4) context specific tolerance

28
Q

treatment of opiate dependence

A

Antagonist treatment (naloxone)
Maintenance therapy (methadone)
- Opiate Agonist

29
Q

what is methadone

A

Long acting mu receptor agonist with pharmacological properties similar to morphine
- blocks effects of other opiates, suppresses withdrawal, decreases craving

30
Q

what is buprenorphine

A

partial agonist