- Heroin is illegal in the US (schedule 1) -Heroin can be smoked, snorted, or taken IV (fastest) -The purity of street heroin varies because it may include adulterants to enhance the effects (ex: fentanyl)

Opiates/Opioids (Final Exam) Flashcards by Alexis Soliz

What type of drugs are opioids?

analgesics and sedative-hypnotics

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While they are the best pain killers known that cause euphoria, at high doses Opioids can lead to…

coma and death

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What type of flower specifically is the source of “opiates”?

The opium poppy

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Raw opium contains about 10% _______ or about 0.5% ______

morphine; codeine

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What are the routes of administration for opium?

oral and smoking

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True or false: Opium has been used for medical purposes since before recorded history?

True

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A drug that used opium in the 1680s was called Laudanum which was weak due to tinctures of opium. What are tinctures?

Tinctures = medicine made by dissolving a drug in alcohol

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What was Laudanum used for in the US until 1914?

primarily for pain; also diarrhea and coughing

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Recreationally, raw opium is usually ________?

smoked

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What are the principal active ingredients in opoim?

Morphine and codeine (natural source)

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What is morphine used for medically?

Medical use as an analgesic (schedule 2)

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What is codeine used for medically?

some analgesic effects, really good for cough (schedule 2 or 3 based on dose)

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What form of opioid is heroin?

semi-synthetic

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What is heroin derived from and what is it formed by?

Heroin is derived from morphine, and it is a semi-synthetic opioid formed from adding two acetyl groups to morphine

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What did bayer first advertise heroin as?

A less addictive replacement for morphine

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Facts about Heroin:

Heroin is illegal in the US (schedule 1)
-Heroin can be smoked, snorted, or taken IV (fastest)
-The purity of street heroin varies because it may include adulterants to enhance the effects (ex: fentanyl)

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What do the two acetyl groups added to morphine do?

increases lipid solubility and speed to the brain

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Which is more potent? Heroin or morphine?

Heroine is 2-4x more potent than morphine when taken IV

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What is desomorphine? Potency in relation to morphine?

It is Krokodil aka “flesh-eating drug” and it is 8-10 times more potent than morphine

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Is desomorphine natural, synthetic, or semi-synthetic?

semi-synthetic

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Fentanyl is a synthetic opioid used to treat pain that has a high potency. It is ____x more potent than morphine and ___ more potent than heroin

100; 50

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illicit fentanyl and opioids are laced with what drug?

xylazine aka “tranq”

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What could happen as a result of xylazine intake?

increased risk of respiratory depression and overdose

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Prescription opioids are used for what two purposes?

analgesic and antitussive (cough)

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What three things does chronic use of opioids increase potential for?

abuse, addicion, and overdose

What has there been a large increase in over the past 20 years?

opioid overdose deaths

What is one factor that contributed to the prescription opioid and heroin epidemic?

Purdue aggressively marketed OxyContin (controlled release oxycodone)

True or False: A large percentage of people with opioid prescriptions become addicted

False! Only about 3% of people that have a prescription for pain have an addiction

Factors leading to opioid crisis:

-Chronic use of Rx opioids -Lacing of heroin with fentanyl

Recreational routes of administration for opioids

-IV injection -SC injection -smoking/inhalation -snorting

IV heroin reaches the brain much faster than morphine due to _____ ________

lipid solubility

difference in half-life between morphine and methadone

Morphine and most oral Rx: 2-4 hours Methadone (oral (drank)): 24 hours due to depot binding

Effects of low doses of opioids

-analgesia -suppression of cough reflex -reduced GI motility (constipation) -euphoria -some dysphoria (unpleasant feelings) -Nausea/vomiting also: slowed respiration, pupil constriction, drowsiness, decreased concentration

Effects of high doses of opioids

-unconsciousness -pinpoint pupils -reduced temperature and blood pressure -respiratory depression -reversed rapidly by naloxone (antagonist for opioid receptors)

Withdrawal are (similar or opposite) to acute effects?

Opposite (Rebound hyperactivity in GI tract, autonomic nervous system, brain, and spinal cord)

Is opioid withdrawal deadly?

it is not life threatening

True or False: there is cross-dependence and cross tolerance for all opioids

True

______ duration opioid causes longer withdrawal with ______ intensity

lower; lower

Factors driving tolerance

-metabolic tolerance -pharmacodynamic tolerance -psychological tolerance

Treatment options for opioids

-detoxification -pharmacological support (opioid agonists and antagonists) -group/individual counseling -harmful reduction programs

What is the pharmacodynamic action for all opioid drugs?

Bind to opioid receptors in the central nervous system and periphery

The first endogenous opioid discovered was...?

beta-endorphin

what type of neurotransmitters are all endogenous opioids?

peptide neurotransmitters

What are the types of endogenous opioids that act as NT and hormones?

endorphins, enkephalins, and dynorphins

How many gene families (that encode long propeptides) are all opioid peptides products of?

4 families

Endogenous peptide synthesis

peptides are made in the soma, cleaved and packaged into vesicles in the Golgi, and then transported into terminals

Release of peptide transmitters (aka endogenous opioids)

Neuropeptides are not typically the only transmitter at a synapse. Instead, they are co-released together with a classical neurotransmitter

inactivation of peptide transmitters

after release, peptides are degraded together with a classical neurotransmitter

Where are opioid receptors located?

in both the CNS and periphery

Bioassay for opioids

ability of opioids to influence contractions of guinea pig intestine (ileum) strongly predicts human analgesic properties

the 4 major types of opioid receptors

mu, delta, kappa, nociceptin/orphanin FQ

What receptor do abused opioids bind to?

the mu-opioid receptor

Are opioid receptors ionotropic or metabotropic?

all are metabotropic receptors and all are Gi coupled opioid binding causes inhibition of AC and actions at G-protein-gated ion channels (opening K+ and closing Ca2+ channels)

Opioid _______ can be presynaptic or postsynaptic

receptors

What occurs in the brain regions where endogenous opioids are found?

pain and emotion signaling

Locations of opioid receptors

CNS, PNS, Periphery

Opioid Agonists and Antagonists

Agonists: many Rx and abused opioid drugs Competitive Antagonists: naloxone, naltrexone (SHIFTS CURVE RIGHT) Partial agonists: buprenorphine

Genetic knockout of mu receptor that leads to loss of morphine effects:

-spinal analgesia -supraspinal analgesia -reward -withdrawal -respiratory depression -inhibition of GI motility -psychomotor activation

Analgesia effects of opioids due to actions at:

1. Spinal Cord: opioids inhibit incoming pain signal 2. Periaqueductal gray 3. Forebrain: sensory and emotional response to pain

Reward associated with Mu receptors

-strongly implicated in reward and euphoria -strong self-administration and CPP for selective mu receptor agonists

Evidence that DA does mediate opioid reward

-mu agonists: increase VTA DA cell firing and DA release in striatum (NAc) -DA antagonists: sometimes reduce opioid CPP and self-administration

Evidence that DA does not mediate opioid reward

-DA receptor antagonists and 6-OHDA lesions do not have large effects of heroin self-administration -DA-deficient mice still show morphine CPP

Respiratory control levles

1. fundamental drive generated by brainstem 2.conscious modulations from cortex 3.subconscious modulations from blood chemoreceptors

What is considered the "gold standard" in antitussive therapy (cough suppression)

Codeine

What was developed as a non-addictive substitute for codeine that does not act at opioid receptors?

Dextromethorphan (DM)

Mechanisms of opioid-induced nausea

1. trigger zone is area postrema (has weak BBB) 2. increased vestibular sensitivity 3. Delayed gastric emptying

What causes pupil constriction?

opioid disinhibition of brainstem nuclei

Where do opioid drugs act to produce their major effects? Analgesia

spinal cord, periaqueductal gray, forebrain

Where do opioid drugs act to produce their major effects? Reward

Brain- dopamine neurons

Where do opioid drugs act to produce their major effects? Gastrointestinal

stomach, small/large intestine

Where do opioid drugs act to produce their major effects? Respiratory Depression

brainstem, cortex, blood chemoreceptors

Where do opioid drugs act to produce their major effects? Cough suppression

brainstem and sensory nerves

Where do opioid drugs act to produce their major effects? Nausea and Vomiting

area postrema, vestibular system, and GI

Where do opioid drugs act to produce their major effects? Pupil constriction

brainstem