Opioids - Lacks Partial agonist and mixed agonist (copy)

Mu Receptors

The receptor that mediates the analgesic property of the opioids; also modulate responses to thermal, mechanical, and chemical nociception

Kappa Receptors

These are located in the dorsal horn, that also contribute to analgesia by modulating response to chemical and thermal nociception

Delta Receptors

These are the selective receptors of enkephalins in the periphery

All opioid receptors are G-protein coupled receptors and are Gi (Inhibit adenylyl cyclase

All opioid receptors are ________________ receptors and are G_

Codeine and Morphine

2 Natural Opioids

Morphine

This natural opioid has greater affinity to the receptors than the other

HOHO
Hydrocodone
Oxycodone
Hydromorphone
Oxymorphone

4 Semi synthetic opioids

Buprenorphine

The opioid that is a partial agonist

1. Nalbuphine
2. Butorphanol
3. Pentazocine

These 3 are mixed agonist/antagonist opioids

Codeine

The prototype weak opioid agonist

Morphine

The prototype strong mu receptor agonist

Codeine

A naturally occurring opioid but weak

Only for mild an moderate pain

Codeine

This opioid is usually in combination with acetaminophen for management of pain

Codeine

This opioid is metabolized by CYP2D6 Enzymes

Oxycodone

A semi-synthetic derivative of morphine which is sometimes formulated with Aspirin or Acetaminophen

Oxycodone

The oral analgesic effect of this opioid is twice that of morphine

Oxycodone

This opioid is metabolized by CYP2D6 and CYP3A4

Oxycodone

The main cause of death for this opioid is by crushing the tablets

Oxymorphone

when given parentally, this is (10x) ten times more potent than morphine

If orally, 3x more potent than morphine

Hydromorphone

Oral ______________is 8 to 10 time more potent than morphine

Oral Hydromorphone

This drug is preferred for patients with renal dysfunction

Hydrocodone

This is the methyl Ester of hydromorphone

Hydrocodone

In combination with ibuprofen or acetaminophen.

For moderate to severe pain and has antitussive effect

Fentanyl

This opioid is related to meperidine

Fentanyl

This opioid 100x more potent than morphine, used as local anesthesia

Fentanyl

The onset and duration of this opioid is around 15 to 30 minutes

Fentanyl

This opioid is combined with local anesthesia to provide epidural analgesia for labor and postoperative pain

1. Sulfentanil
2. Alfentanil
3. Remifentanil

These 3 drugs are related to fentanyl

1. Naloxone
2. Naltrexone

These are opioid receptors antagonist

Naltrexone

The antagonist has the longer duration of action but it can lead to hepatotoxicity

Naltrexone

A single oral dose of this can block effect of injected heroin for up to 24 hours

naltrexone

This can be used to treat chronic alcoholism

Naloxone

This reverses the coma and respiratory opioid overdose

Naloxone

This drug is a competitive antagonist at all opioid receptors with 10-fold affinity for mu and kappa receptors

Naloxone

This drug is in IV formulation and works within 30 secs for respiratory depression and coma characteristics

Tapentadol and Tramadol

These are centrally acting analgesics

Tapentadol

This centrally acting analgesic is used to manage moderate to sever pain for both chronic and acute

Tapentadol

This centrally acting analgesic has IR and ER DF

Tramadol

This centrally acting analgesic undergoes extensive metabolism with CYP2D6

Naloxone

The effects of Tramadol can only partially be reversed by _______________

Sulfentanil - More potent than fentanyl

Alfentanil and Remifentanil - Less potent, shorter acting

_____________ is more potent than fentanyl, while ___________ and ____________ are less potent and shorter acting

Methadone

An Oral effective opioid that has variable equianalgesic potency compared to that of morphine

Methadone

Antagonist of NMDA receptors and is a SNRI, so they can be used for both nociceptive and neuropathic pain

Methadone

Used in controlled withdrawal from opioids and heroin

Methadone

has 12 to 40 hours of half life but may extend to 150 hours but the actual duration of analgesia is from 4 to 8 hours


Steady state is achieved by patient from 35 hours to 2 weeks

Methadone

Can prolong the QT interval and cause torsades de pointe (a type of arrythmia because of K+ channel changes)

Methadone

This drug produces less euphoria and longer duration of action than Morphine

Sulfentanil, Alfentanil, Remifentanil

These are usually used for their analgesic and sedative properties during surgery

Meperidine

Less potent and is used for acute pain only

Meperidine

This is a kappa agonist with some my agonist activity

Normeperidine

The metabolite of meperidine which has significant neurotoxic actions which can lead to delirium, hyperreflexia, myoclonus, and possibly seizures

Meperidine

Contraindicated to elderly patients, especially with renal insufficiency, hepatic insufficiency, preexisting respiratory compromise, or with MAOIs.