(Neuro) Opioids

Front 1

Drug Name: Meperidine (Demerol)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 1

USES: Analgesiac, biliary colic
MECHANISM: Synthetic opioid with anticholinergic properties. Shorter duration than morphine (reduces dependence/withdraw)
SIDE EFFECTS:
TOXICITY: Cardiovascular dysfunction & serotonin effects
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: Lethal interactions with non-specific MAO inhibitors
OTHER: Widely abused by health professionals.

Front 2

Drug Name: Loperamide (Immodium)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 2

USES: Antidiarrheal
MECHANISM: Derivative of meperidine. Not well absorbed from the GI tract. Increases anal sphinctor tone. Poorly soluble in water.
SIDE EFFECTS:
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Less abuse potential

Front 3

Drug Name: Methadone
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 3

USES: Pain & heroin abuse programs
MECHANISM: Very similar to morphine except with longer duration. Prodces smoother withdraw than morphine.
SIDE EFFECTS:
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: In practice those maintained on methadone and wishing to abuse opioids continue to do so

Front 4

Drug Name: Propoxyphene (Darvon)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 4

USES: Weak analgesic
MECHANISM: Congener of methadone. Stimulant activity
SIDE EFFECTS:
TOXICITY: Toxic psychosis
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: No superiority over codeine and ASA

Front 5

Drug Name: Codeine
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 5

USES: Cough, mild pain, diarrhea
MECHANISM: Opioid that biotransforms to morphine with exception of antitussive effect. Good kinetics for oral administration.
SIDE EFFECTS:
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:

Front 6

Drug Name: Fentanyl (Sublimaze)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 6

USES: Neuroleptic anesthesia, breakthrough pain.
MECHANISM: Pure mu agonist 80 times more potent than morphine. Available in patch or lozenges.
SIDE EFFECTS:
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Combined with butyrophenone (droperdol) to make Innovar)

Front 7

Drug Name: Tramadol
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 7

USES: Analgesic
MECHANISM: Weak mu agonist that blocks reuptake of serotonin and norepinephrine.
SIDE EFFECTS: Nausea, constipation, drowsiness
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS: Same as morphine
INTERACTIONS:
OTHER:

Front 8

Drug Name: Buprenorphine (Temgesic)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 8

USES: Analgesic
MECHANISM: Partial mu (only) agonist. Highly lipophilic. Analgesia and side effects last longer than morphine.
SIDE EFFECTS: Similar to morphine. Respiratory depression reaches a ceiling at low doses (higher than other drugs)
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Possible treatment for opioid dependence

Front 9

Drug Name: Pentazocine (Talwin)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 9

USES: Analgesic
MECHANISM: Kappa / mu partial agonist. Spectrum similar to morphine. Low intrinsic activity.
SIDE EFFECTS: Less steep respiratory depression than other opioids. Otherwise similar to the rest.
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: Has more CNS / cardiovascular stimulations in folks with psychotic reactions.
OTHER: In morphine dependent person, high doses may precipitate withdrawal.

Front 10

Drug Name: Nalbuphrine (Nubain)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 10

USES: Analgesic
MECHANISM: Related to naloxone and oxymorphine. Antagonist to mu receptors (agonist to kappa receptors).
SIDE EFFECTS: Ceiling effect on respiratory depression and pentazocine like cardiovascular effects observed.
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:

Front 11

Drug Name: Butorphanol
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:

Back 11

USES: Analgesic
MECHANISM: Morphinan congener similar to pentazocine. Affects kappa receptors, not mu receptors.
SIDE EFFECTS: Increased cardiac workload (limits its use). Ceiling respiratory depression
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:

Front 12

FrontOfCard

Back 12

BackOfCard

Front 13

Which positions on the structure of morphine are often altered in order to change its dependence and tolerance?

Back 13

Substitutions on the phenolic hydroxyl (position 3)

Substitution of -OCH3 (used in codeine derivatives)

Substitution of the alcoholic hydroxyl group

Substitution of the nitrogen at position 17. (Full mu agonists have a methyl group, while antagonists have an allyl group there)

Front 14

Are opioid anagesics more effective in dulling dull pain or sharp pain?

Back 14

They are better at reducing dull pain, although high doses will dull both.

Front 15

(T/F) Opioids produce a picture with a mixture of depression and stimulation.

Back 15

True

Front 16

What is the effect of morphine in the following:

Pupil size
Frequency of bowel movements
Bladder sphincter
Biliary sphincter
Respiration

Back 16

Morphine causes MIOSIS, CONSTIPATION, CONSTRICTION of both the bladder and biliary sphincters, and it REDUCES respiration.

Front 17

Cerebral blood vessles tend to dilate with opioid agents, in large part due to what affect?

Back 17

Due to a buildup of carbon dioxide

Front 18

What is a good alternative to morphine used to treat biliary colic?

Back 18

Meperidine (Demerol)

Front 19

Is morphine often used in labor? Why or why not?

Back 19

Morphine is rarely used in labor.

It prolongs labor, clouds the mother's mind, and suppresses neonatal respiration.

Front 20

Which individuals are more like to expereince dysphoria when taking morphine?

Back 20

Individuals who are pain free

Front 21

How does morphine cause vomiting?

Back 21

Morphine stimulates the chemoreceptor trigger zone (CTZ) in the midulla which sends impulses to the vomiting center.

Note that vomiting disappears after the first several administrations. Also ambulatory patients are more likely to vomit.

Front 22

How can morphine lead to increased intracranial pressure?

Back 22

Opioids cause cerebral blood vessels to dilate in part to the increase in carbon dioxide which results from a depressed respiratory rate.

Front 23

Suppose a drug is a partial agonist on mu receptors ONLY. How will it affect individuals in the following scenarios?

Giving the drug alone to a person receiving no other drugs
Giving the drug to a person already receiving a small dose of morphine (acutely)
Giving a small dose of the drug to a person who is taking morphine and who is tolerant and dependent on morphine
Giving a large dose to a person who is tolerant and dependent on morphine?

Back 23

When given alone, it causes a MORPHINE-LIKE picture.
When given to an individual receiving a small dose acutely, it will ADD to morphine's action.
When given to a morphine dependent person in small dose it will substitute for morphine.
When given to the same person in high doses it will antagonize morphine and precipitate withdraw.

Front 24

(T/F) Opioids that are mixed agonist-antagonists are primarily mu agonists with weak action on kappa receptors and tend to produce fellings of dysphoria, particularily in the pain free.

Back 24

False. While they tend to produce dysphoria in the pain free, they are primarily kappa agonists with weak mu action.

Front 25

What will happen if you give a kappa agonist to a person who recently received a single dose of morphine?

Back 25

The kappa agonist will reverse mu effects and substitute kappa effects.

Front 26

What will happen if you give a kappa agonist to a person who is tolerant and dependent to morphine?

Back 26

The kappa agonist will precipitate withdraw

Front 27

If a person is tolerant to mu agonists, are they also tolerant to kappa agonists?

Back 27

No!

Front 28

Naloxone, Naltrexone, and Nalmefene are all drugs in which class (be specific)

Back 28

These are pure opioid antagonists.

Front 29

What does a pure opioid antagonist do when given alone (without opioid agonist)?

Back 29

Nothing

Front 30

What does a pure opioid antagonist do when given to someone who has taken morphine?

Back 30

They will reduce the effects and can precipitate withdrawal if the person is tolerant and dependent on morphine.

Front 31

Where does most detoxification of morphine take place?

Back 31

In the liver or gut

Front 32

In which tissues do opioids tend to distribute the most?

Back 32

Trick question! Opioids don't have a preference for tissue distribution.

Front 33

When considering tolerance to opioids, do you see more tolerance to its depressant effects or its stimulating effects?

Back 33

You see more tolerance to the depressant activities.

Thus, in addicts you see less euphoria, less respiratory depression, and less analgesia which according to the notes are depressant properties.

Front 34

How is heroin converted to morphine?

Back 34

Heroin is deacetylated to morphine.

Front 35

Why does heroin cause a rush compared to morphine?

Back 35

Because it is more lipid soluble than morphine.

Front 36

(T/F) Many symptoms of physiological withdrawal result from NE over-activity.

Back 36

True. This makes sense because morphine causes causes decreased NE transmission.

This is the basis for using Clonidine to treat withdrawal.

Front 37

Symptoms of heroin or morphine withdrawal:

Back 37

Vomiting, diarrhea, cramps, yawning, leg twitching, sweating, chills, and goose flesh.

Front 38

Three main symptoms of opioid overdose:

Back 38

Respiratory depression, coma, pinpoint pupils. (Dilated pupils may be evident with severe hypoxia)

Front 39

(T/F) Since opioids cross the placental membrane, it's possible for the newborn child to become dependent to opioids if the mother has been abusing them.

Back 39

True

Front 40

What is an emergency condition in which opioids would be of great use?

Back 40

Acute left ventricular failure since they decrease oxygen consumption and workload.

They are also good for pulmonary edema.

Front 41

Why should opioids be used with great caution in a patient with a cranial injury?

Back 41

Because opioids increase CSF pressure, and because they depress the CNS and respiration which could mask symptoms of cranial injuries.

Front 42

What is the effect of combining opioids with NSAIDS or ASA?

Back 42

Good pain control with lower doses of each drug.

Front 43

What are four drug interactions for opioids?

Back 43

1. MAO inhibitors (use less dose, avoid meperidine and its congeners)
2. Additive effect of opoids with NSAID or ASA
3. Hightened euphoria and analgesia when combined with amphetamine
4. Depressant effects are enhanced by tricyclic antidepresants and phenothiazines (analgesic effects may increase, decrease or stay the same).