Nagelhout Pharm 1- Exam 3 |83
Complete Q’s and A’s
General Cardiac Effects of Opiates - -Little to no effect
Minimal bradycardia
Effects more pronounced in shock or ambulating patients
- Groups of Endogenous Opioid Peptides (5) - -1. Enkephalins
a. Leu-enkephalin
b. Met-enkephalin
2. β -Endorphin
3. Dynorphins
a. Dynorphin
b. α-Neoendorphin
4. Endomorphin 1 and Endomorphin 2
5. Nociceptin
- Precursor to Enkephalins - -Proenkephalin A
- Precursor to β-Endophins - -Pro-opiomelanocortin (Pro-OMC)
- Precursor to Dynorphins - -Prodynorphin
- Precursor to Endomorpins 1 & 2 - -Unknown
- Precursor to Nociceptin - -Pronociceptin
- Location of endogenous opioid peptides - -Brain & Spinal cord
(second highest concentration in GI)
- Analgesic mechanism of action of opioids - -Actives opioid receptors on
pre-synaptic "pain pathway" nerve → prevents release of substance P (or
bradykinin/acetylcholine) to post-synaptic nerve
- Analgesic mechanism of action of endogenous endorphins - -Endorphins
released from pre-synaptic "pain relieving" nerve → pre-synaptic "pain
producing nerve" → prevents release of substance P (or
bradykinin/acetylcholine) to post-synaptic nerve
- 3 classes of opiate receptors - -1. Mu µ
2. Kappa κ
3. Delta δ
, - Mu receptors effects (11) - -1. Analgesia (supraspinal and spinal) (Mu-1 in
animals)
2. Euphoria & sedation
3. Physical dependence
4. Depression of respirations (Mu-2 in animals)
5. Miosis
6. Constipation
7. Urinary retention
8. Bradycardia
9. Pruritus
10. Skeletal rigidity
11. Biliary spasm
- Kappa receptor effects (6) - -1. Analgesia (spinal & supraspinal)
2. DYSPHORIA
3. Sedation
4. Low abuse potential
5. Miosis
6. ANTI-SHIVERING
- Delta receptor effects (5) - -(AUGMENTS MU & KAPPA EFFECTS)
1. Analgesia (supraspinal and spinal)
2. Physical dependence
3. Respiratory depression
4. Minimal constipation
5. Urinary retention
- Mu receptor Agonists (3) - -1. Endorphins
2. Morphine
3. Synthetic opioids
- Kappa receptor Agonists (1) - -Dynorphins
- Delta receptor Agonists (1) - -Enkephalins
- Antagonists for all classes of opioid receptors (3) - -1. Naloxone
2. Naltrexone (oral)
3. Nalmefene (long-lasting)
- The amount of analgesia is directly proportional to...(2) - -the amount of
respiratory depression
the amount of physical dependence
- Full agonist - -Has 100% efficacy
- Partial Agonist (Agonist/Antagonist) - -Does not have 100% efficacy
Complete Q’s and A’s
General Cardiac Effects of Opiates - -Little to no effect
Minimal bradycardia
Effects more pronounced in shock or ambulating patients
- Groups of Endogenous Opioid Peptides (5) - -1. Enkephalins
a. Leu-enkephalin
b. Met-enkephalin
2. β -Endorphin
3. Dynorphins
a. Dynorphin
b. α-Neoendorphin
4. Endomorphin 1 and Endomorphin 2
5. Nociceptin
- Precursor to Enkephalins - -Proenkephalin A
- Precursor to β-Endophins - -Pro-opiomelanocortin (Pro-OMC)
- Precursor to Dynorphins - -Prodynorphin
- Precursor to Endomorpins 1 & 2 - -Unknown
- Precursor to Nociceptin - -Pronociceptin
- Location of endogenous opioid peptides - -Brain & Spinal cord
(second highest concentration in GI)
- Analgesic mechanism of action of opioids - -Actives opioid receptors on
pre-synaptic "pain pathway" nerve → prevents release of substance P (or
bradykinin/acetylcholine) to post-synaptic nerve
- Analgesic mechanism of action of endogenous endorphins - -Endorphins
released from pre-synaptic "pain relieving" nerve → pre-synaptic "pain
producing nerve" → prevents release of substance P (or
bradykinin/acetylcholine) to post-synaptic nerve
- 3 classes of opiate receptors - -1. Mu µ
2. Kappa κ
3. Delta δ
, - Mu receptors effects (11) - -1. Analgesia (supraspinal and spinal) (Mu-1 in
animals)
2. Euphoria & sedation
3. Physical dependence
4. Depression of respirations (Mu-2 in animals)
5. Miosis
6. Constipation
7. Urinary retention
8. Bradycardia
9. Pruritus
10. Skeletal rigidity
11. Biliary spasm
- Kappa receptor effects (6) - -1. Analgesia (spinal & supraspinal)
2. DYSPHORIA
3. Sedation
4. Low abuse potential
5. Miosis
6. ANTI-SHIVERING
- Delta receptor effects (5) - -(AUGMENTS MU & KAPPA EFFECTS)
1. Analgesia (supraspinal and spinal)
2. Physical dependence
3. Respiratory depression
4. Minimal constipation
5. Urinary retention
- Mu receptor Agonists (3) - -1. Endorphins
2. Morphine
3. Synthetic opioids
- Kappa receptor Agonists (1) - -Dynorphins
- Delta receptor Agonists (1) - -Enkephalins
- Antagonists for all classes of opioid receptors (3) - -1. Naloxone
2. Naltrexone (oral)
3. Nalmefene (long-lasting)
- The amount of analgesia is directly proportional to...(2) - -the amount of
respiratory depression
the amount of physical dependence
- Full agonist - -Has 100% efficacy
- Partial Agonist (Agonist/Antagonist) - -Does not have 100% efficacy
