Chapter 11: Opioids Flashcards by Jennifer Lyons

Opioid drugs are narcotic analgesics, meaning?

They provide pain reduction without producing unconsciousness.
State of relaxation or sleep

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High doses of opioid drugs, seeing that they are narcotic analgesics, cause what?

Coma and death

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Opioid drugs produce a sense of

Euphoria

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Opioid drugs are the best ______ known.

Painkillers

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Opium is an extract of the _____.

Poppy plant

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Recreational use of opium is mentioned in _____

The Odyssey (9th century B.C.)

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Active ingredients of opium

Morphine and Codeine

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Morphine named after

Roman god, “Morpheus”

God of dreams

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Codeine has _____ analgesic effects than morphine, _____ side effects and is considered a _____.

Less; fewer; potent cough suppressant

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Heroin has been used for thousands of years, _____ for both recreation and medicine

Egyptians

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Eating or smoking opium in ancient _____ countries to replace alcohol consumption, which was prohibited.

Islamic

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Laudanum was used in 1680 for _____. Ingredients?

Pain relief and cough suppressant
Considered addictive today
Ingredients:
2 oz strained opium
1 oz saffron
1 dram of cinnamon and cloves dissolved in 1 pint of canary wine

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Year _____, _____ Act - Opiates and Cocaine
First law to _____ substances. Doctors could no longer treat addiction with _____ because addiction was not classified a medical issue. Revenue generated via _____

1914; Harrison

Control; agonists; tax

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Structural modification: Heroin

When we realized morphine was addictive, heroin was synthesized from morphine to replace it. Considered semi-synthetic because you needed morphine to make it. However, formulation increased its lipid solubility and it was able to reach the brain faster. IV heroin much more potent. More addictive

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Heroin is synthesized into _____ in the brain

morphine

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Morphine to Codeine: _____ group for hydroxyl (OH) group

methoxy (CHO3)

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Morphine to Codeine: _____ group for hydroxyl (OH) group

methoxy (CH3O)

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Taking buprenorphine would present any opioid with _____.

competition at the receptors site

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Naloxone is released and _____ the effects of buprenorphine or any other opioid that is taken to enhance the effects

blocks

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(1) Partial agonists
What’s the name?
Bind to the receptors with _____
_____ biological effect as compared to full agonist.
_____ potent and efficacious, _____ risk of respiratory depression

Buprenorphine

high affinity; reduced; less; reduced

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(2) Pure antagonists
What's the name?
Structurally similar to \_\_\_\_\_
Administration produces \_\_\_\_\_
Can prevent or reverse the effect of \_\_\_\_\_.

Naloxone (narcan)
morphine/heroine
no effect; opioids

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What makes up suboxone?

Considered a _____

Buprenorphine + naloxone.

Partial agonist; Antagonist is activated if sublingual route is avoided (route of administration)

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What makes up suboxone?

Considered a _____

Buprenorphine + naloxone.

Partial agonist; Antagonist is activated if sublingual route is avoided (route of administration)

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Opioids medically
-Routes of administration
_____% of individuals prescribed pain meds become addicted

IM or oral

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Opioids recreationally -Routes of administration _____ bioavailability _____ onset

Inhalation, intranasal, subcutaneous injection Higher bioavailability Faster onset

Effects of opioids on the CNS are related to _____.

dose and rate of absorption

Low dose opioids: | Effects

Pain relief, constricted pupils | Drowsiness, inability to concentrate, dreamy sleep, decreased sensitivity to the environment.

Low dose opioids | Hypothalamus:

Decreased appetite, drop in BT, reduced sex drive, hormone disregulation

Low dose opioids | Limbic system effects

Anxiety, aggressiveness, and feelings of inadequacy. Increase subsequent drug use

Psychological pain may be derived from actions within the _____

limbic system

Increased subsequent drug use encouraged through _____

Negative reinforcement

Increased subsequent drug use encouraged through _____

Negative reinforcement

GI Tract: drugs are now designed so they don’t cross the _____

BBB

``` High dose opioids: Effects Morphine affects regions of the _____ Morphine also affects the _____. Causes _____ Severe bacterial and parasitic diseases. Effect is resistant to _____ ```

Sedative effects become stronger, unconsciousness Decreased body temperature and blood pressure, coma, respiratory failure brainstem; GI tract; constipation tolerance

_____ becomes a classic sign of OD..ultimately occurs due to respiratory failure.

Pupil constriction

GI Tract: drugs are now designed so they don’t cross the _____

BBB

4 opioid receptors

μ (mu) δ (delta) κ (kappa) NOP-R

The 4 opioid receptors are slow-acting or _____

Metabotropic

μ (mu) has a high affinity for

Morphine

μ (mu) produce analgesic effects when located in

Thalamus, periaqueductal gray, median raphe, spinal cord

μ (mu) produce Positive reinforcement effects when located in

Nucleus accumbens

μ (mu) receptors in the brainstem causes

Respiratory depression, cough suppressant, nausea, vomiting

δ-receptors are predominantly found in _____.

forebrain structures

Possible effects of δ-receptors (4)

Modulating olfaction, motor integration, reinforcement, and cognitive function.

Areas of overlap with μ-receptors suggest modulation of both _____ and _____.

spinal and supraspinal analgesia

κ- receptors located in hypothalamus and pituitary gland cause

Pain perception, gut motility, temperature control, neuroendocrine fx.

The endogenous ligand for opioid receptors

Endorphins and enkephalins

The ligand for kappa opioid receptors is

dynorphin

Peptides made from large precursor peptides Manufactured in _____ Packaged with enzymes called _____

POMC and proenkyphalin Soma Proteases

3 ways opioids inhibit nerve activity

1. Postsynaptic inhibition 2. Axoaxonic inhibition 3. Presynaptic autoreceptors

All four types of opioid receptor are also coupled to inhibitory _____

G proteins (Gi)

Axoaxonic inhibition

Receptors activate G proteins, close Ca2+ channels | Reducing the release of neurotransmitter

Adenylyl cyclase inhibitions will inhibit

second messenger cAMP

All four types of opioid receptor are also coupled to inhibitory _____ Which may be partly responsible for opioid-induced ion channel changes.

G proteins (Gi)

G proteins inhibit

adenylyl cyclase

Adenylyl cyclase inhibitions will inhibit

second messenger cAMP.

cAMP inhibition

May be partly responsible for opioid-induced ion channel changes.

With electrical self-stimulation, opioids _____ threshold

reduce

Opioids have significant _____ properties.

Reinforcing

With self-administration, pre-treatment with an opioid _____ responding

Reduces

With self-administration, pre-treatment with naloxone _____ responding

Increases

The _____ pathway contributes to opioid reinforcement.

dopaminergic mesolimbic

Administration of opioids and β-endorphin: _____ cell firing and release of DA in NAcc _____ threshold of electrical self-stimulation Produces _____

Increase; reduces; CPP

Administration of the κ- agonist (dynorphin): _____ rate of cell firing and release of DA in NAcc _____ threshold of electrical self-stimulation Produces _____

Decreases; Increases; conditioned place avoidance

Long-Term Opioid Use leads to _____ that produce _____.

neuroadaptive changes that produce tolerance, sensitization, dependence

κ-receptors (dynorphin) can reduce the release of DA via same mechanisms as opioid drugs and β-endorphin Causes _____

dysphoria

Rapid tolerance to

analgesia

No tolerance for

constipation or pupil constriction

Cross-tolerance among the opioids also exists such as in _____

Heroin and codeine

Rapid tolerance to

analgesia

No tolerance for

constipation or pupil constriction

The locus coeruleus and the periaqueductal gray (PAG) associated with _____

physical withdrawal

Long-term opioid use: Sensitization _____ in drug effects that occurs with repeated administration. _____ or _____ can become sensitized

Increase; craving or desire

Aversive affects (mental) of withdrawal associated with

NAcc

The locus coeruleus and the periaqueductal gray (PAG) associated with _____

physical withdrawal

The classic hypothesis of opioid tolerance and dependence was first developed by _____ in _____

Himmelsbach in 1943.

When opioids withdrawn, system

rebounds

After two days of morphine exposure: | The cells adapted to producing _____ cAMP.

When morphine was removed or nalaxone added: | Levels of cAMP _____ significantly.

increased

Withdrawal can be suppressed by increasing synthesis of _____

endorphins

Electroacupuncture EA restored the low levels of _____ for precursor peptides in the spinal cord, hypothalamus, and PAG

mRNA

Most common and effective treatment program for opioid addiction

Methadone maintenance program (relieves craving)

Ibogaine

Alleviates withdrawal