Exam 4: Opioid Analgesics-Part 1 Flashcards by Austin Shackelford

Opiates are for _______ to ______ dental pain that cannot be managed effectively with NSAIDS.

Moderate to severe

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What is the older term derived from Greek word meaning “stupor”?

Narcotics

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What term is used to describe substances from the white liquid extract derived from the seeds of poppy plant? Alkaloids found in opium…

Opiates

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What is the current/correct term used to describe opiates, their antagonists, and the receptors stimulated by opioid drugs?

Opioids

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What are the 4 mechanisms of action for opioid theraputics?

Agonists, Partial Agonists, Mixed (agoinists + antagoinists) and antagoinists

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Opioids bind to receptors in both _____ and spinal cord…Produce altered perception of _____ reaction…Opioid receptors that mediate specific pharmacologic effects and adverse reactions are stimulated to varying ______ by individual opioids.

CNS…pain….degrees

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The Analgesic Effect: Produced by _______ stimulation due to activation of a pain-modulating circuit which projects via the _____ to the spinal cord ______ horn.

midbrain…medulla..dorsal

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Where is the highest concentration of endogenous opioid?

the DESCENDING pain-modulating circuit

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What circuit is activated by stress (like running/birth)?

the DESCENDING pain-modulating circuit

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Opiates produce analgesia by direct action on the _____.

CNS

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The Pain suppression center involves ________ as neurotransmitter and it is partially _______-mediated (endogenous opioids)

serotonin…enkephalin

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What are the 3 areas of the CNS where all the Analgesia action takes place?

1.periaquaductal grey matter (MIDBRAIN)….2.nucleus raphe magnus (MEDULLA)….3.pain inhibitory neurons (DORSAL horns of the spinal cord)

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Projections from the Periaqueductal Gray Matter (PAG) and RVM (rostroventral medulla) are ________ and are highly sensitive to ________.

serotonergic…morphine

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Projections from the dorsolateral pons are _________…Application of NE to spinal cord blocks noxious stimuli in ______ horn.

noradrenergic….dorsal

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What are the 3 groups of endogenous opioids?

1.Endorphins 2.Enkephalins 3.Dynorphins

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What are the 3 different receptors that opioids work on? What type of signal transduction?

Mu, delta, and kappa….G protein

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Term “_______” = used synonymously with endogenous opioid peptides

endorphins

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Endorphins/endogenous opioid peptides are produced by the _______ gland and _________.

pituitary gland and the hypothalamus

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You can find endorphins/endogenous opioid peptides? mainly in ______ system and ______ areas
associated with pain reception and certain areas of the _____

limbic…brainstem…spinal cord

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The Endogenous Opioid Peptides: β-Endorphin = expressed in cells in the _______ nucleus of the _______ and in the _______….acts via ____: influences appetite, sexual behavior

arcuate…hypothalamus…brainstem..mu

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Enkephalin = widely distributed throughout the brain

– acts via ____ and _____

mu and delta

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Dynorphin = found in the spinal cord and in many parts of the brain, including the hypothalamus
– acts via ______

kappa

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More on ENDORPHINS: endogenous morphine is produced from _______ molecules (no I aint about to memorize those)

precursor

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Which group of endogenous opioid is found in the gut (pancreatic islet cells), sympathetic nervous system, adrenal medullary chromaffin cells, CNS?

Endorphins

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More on ENDORPHINS: B-endorphin distributed in _____

brain

Which group of endogenous opioid is involved in blood pressure regulation, temperature regulation and food intake?

Endorphins

More on ENDORPHINS: they act via the ____ receptor to produce the opiate effects.

Since the naturally occurring endorphins act via mu receptors in the GI tract, what is a MAJOR side effect when you prescribe opioids? What would you recommend to the Pt along with your Rx?

CONSITPATION!!! A stool softener like Colace

More on ENKEPHALINS: they are _________ synthesized and isolated from brain.

pentapeptides

More on ENKEPHALINS: they mimic opiate activity = and are ______ analgesics

weak

More on ENKEPHALINS: May be responsible for producing analgesia in placebo responders and _______.

acupuncture

More on ENKEPHALINS: act via ___ and _____ receptors.

mu and delta

More on DYNORPHINS: Found in the spinal cord and in many parts of the brain, including the _________....acit via ______ receptors.

hypothalamus...kappa

______ and ______ horn of spinal cord have dense concentrations of opiate binding sites

PAG (periaqueductal gray matter)....dorsal

Opiate receptors are also found in tissues that are NOT involved in analgesia, Accounts for side effects of respiratory ________, pupil _______, decreases in body _______ and decreases in gut ______!!!

depression....constriction....temperature...motility

What method do scientists use to measure opiate receptor locations? What are the three areas that showed lots of mu activity?

PET scan...thalamus, cerebral cortex, and basal ganglia

Recognition site of receptor is highly ______!! analgesic action of opioid drugs is stereospecific: ONLY _____-isomers have biological activity

specific...LEVO-isomers

What are the 5 opioid receptors? (we've talked about 3 of them)

mu, delta, kappa, epsilon, sigma(aint a receptor no more)

Which receptor? Supraspinal analgesia • Euphoria | • Physical dependence

Mu 1

Which receptor? Respiratory depression

Mu 2

Must bind to ____ to be physically addicting!

Drugs that bind to ___ (___ agonists) exhibit the | BEST analgesic properties!

Mu...Mu

Downside: always the risk of ______ and risk for respiratory _______

addiction...depression

If decrease the ______ for Mu (e.g. partial Mu agonist), then decrease the risk for ______, but also decrease the level of _______.

affinity...addiction...analgesia

Which receptor? – Spinal analgesia – Miosis (pinpoint pupils) -SEDATION

Kappa (think soccer ladies)

Which receptor? Analgesia – Emotion – Seizures

Delta

Which receptor? just analgesia....

Epsilon

Which receptor? – Autonomic stimulation – Dysphoria – Hallucinations – Nightmares – Respiratory stimulation – Vasomotor stimulation (tachycardia) – Anxiety...(not really a receptor...)

Sigma

Strength of attachment of an opioid drug to its binding site (binding affinity) is proportional to its ______.

potency

INTERESTING! Opioids cause _________ of nerve cells, inhibition of nerve _____ and presynaptic inhibition of _______ release

hyperpolarization...firing...transmitter

What are two examples of opium alkaloids?

morphine and codiene

What are 4 examples of semi-synthetic opioids?

heroin, oxy-codone, hydro-codone, hydro-morphone

What are 4 examples of fully synthetic opiods?

meper-id-ine, metha-done, fentanyl, penta-zo-cine

Which type of opioid drug elicits receptor responses of opiate receptors....there are Pure and partial..

agoinists

Which type of opioid drug has no inherent action after binding to receptor but block any agonist activity?

pure Antagonists

What is our prime example of a PURE agonist?

morphine

Which type of opioid? Complete receptor activation, Mu and Kappa activated, Unlimited analgesia..ex-morphine

pure agonist

What is this phenomenon called? With continued exposure of tissues to high concentrations of opioid agonists, the potency of the drug DECLINES so that progressively HIGHER concentrations are required to produce the same degree of analgesia.

Tolerance

How many of the opioids exhibit tolerance?

ALL of them

______-tolerance develops to other opioid analgesics as well

Cross

What type of opioid am I talkin bout? Drug example: buprenorphine (Buprenex), Partial Mu activation, Weak Kappa antagonist, Good analgesia but limited effect, Not typically used in dentistry, Injection (C-V/III) for moderate to severe pain, Tablets (C-III) – treatment of opioid dependence; chronic pain; investigational for opiate and heroin withdrawal

Partial Agonist

Partial Agonists: Drug example: _________ (Buprenex)

Bu-Pren-or-phine

Partial Agonists: Partial ___ activation

Partial Agonists: weak _____ ANtagonist

kappa

Partial Agonists: good ______ but limited effect

analgesia

Partial Agonists: Not typically used in ______

dentistry

We use a _____ agonist for the treatment of opioid dependence.

partial

Agonist/Antagonist mixes are used as a _______ prior to surgery... they are agonists for ____ receptors and antagonists for _____ receptors.

sedative...kappa....mu

Need to know this drug! What is our PRIME example of a PURE Antagonist?

Naloxone (Narcan)

A Pure antagonist works by blocking ____ and ___ receptors.

mu and kappa

______ antagonist, used in dentistry to reduce overdose of opiates (fentanyl and meperidine) used during conscious sedation...Used for complete or partial ______ of opioid depression

pure...reversal

Kinetics: Ditribution-_______ effect reduces bioavailability | – Passes to ______ = produces ________ depression in fetus if taken by mother

first pass...fetus...respiratiory

Kinetics: Metabolism-Conjugation with _______ acid in liver

glu-cur-on-ic acid

Kinetics: Excreted in ______, usually a way of testing for their over use.

urine

Kinetics: Duration-most opiates produce analgesia for ___-___ hours

4-6 hours