Nagelhout Pharm 1- Exam 3
Cause of urinary retention with opioids - ANSWER-Smooth muscle spasm
Antidiuretic effect
First drug choice for anti-shivering? - ANSWER-Meperidine (Demerol)
Acute skeletal muscle effects of opioids - ANSWER-Muscle rigidity of chest wall,
contraction of pharyngeal and laryngeal muscles
Cause of skeletal muscle rigidity with opioids - ANSWER-1. Large doses
2. Given rapidly
3. Concurrent use of N2O
4. Older age
5. Absence of muscle relaxants
Associated with: *Alfentanil, *Remifentanil, Sufentanil, Fentanyl
Treatment for chest wall rigidity - ANSWER-Neuromuscular blocker
Acute dermatologic effects of opioids - ANSWER-Rash, itching, warmth
R/t mu receptors more than histamine release
Cause of tolerance in opioids - ANSWER-Down regulation (starts within 24 hours)
Analgesic mechanism of action of opioids - ANSWER-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 - ANSWER-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 - ANSWER-1. Mu µ
2. Kappa κ
3. Delta δ
Mu receptors effects (11) - ANSWER-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) - ANSWER-1. Analgesia (spinal & supraspinal)
2. DYSPHORIA
3. Sedation
4. Low abuse potential
5. Miosis
6. ANTI-SHIVERING
General Cardiac Effects of Opiates - ANSWER-Little to no effect
Minimal bradycardia
Effects more pronounced in shock or ambulating patients
Groups of Endogenous Opioid Peptides (5) - ANSWER-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 - ANSWER-Proenkephalin A
Precursor to β-Endophins - ANSWER-Pro-opiomelanocortin (Pro-OMC)
Precursor to Dynorphins - ANSWER-Prodynorphin
Precursor to Endomorpins 1 & 2 - ANSWER-Unknown
Precursor to Nociceptin - ANSWER-Pronociceptin
Location of endogenous opioid peptides - ANSWER-Brain & Spinal cord
(second highest concentration in GI)
Delta receptor effects (5) - ANSWER-(AUGMENTS MU & KAPPA EFFECTS)
1. Analgesia (supraspinal and spinal)
2. Physical dependence
Cause of urinary retention with opioids - ANSWER-Smooth muscle spasm
Antidiuretic effect
First drug choice for anti-shivering? - ANSWER-Meperidine (Demerol)
Acute skeletal muscle effects of opioids - ANSWER-Muscle rigidity of chest wall,
contraction of pharyngeal and laryngeal muscles
Cause of skeletal muscle rigidity with opioids - ANSWER-1. Large doses
2. Given rapidly
3. Concurrent use of N2O
4. Older age
5. Absence of muscle relaxants
Associated with: *Alfentanil, *Remifentanil, Sufentanil, Fentanyl
Treatment for chest wall rigidity - ANSWER-Neuromuscular blocker
Acute dermatologic effects of opioids - ANSWER-Rash, itching, warmth
R/t mu receptors more than histamine release
Cause of tolerance in opioids - ANSWER-Down regulation (starts within 24 hours)
Analgesic mechanism of action of opioids - ANSWER-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 - ANSWER-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 - ANSWER-1. Mu µ
2. Kappa κ
3. Delta δ
Mu receptors effects (11) - ANSWER-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) - ANSWER-1. Analgesia (spinal & supraspinal)
2. DYSPHORIA
3. Sedation
4. Low abuse potential
5. Miosis
6. ANTI-SHIVERING
General Cardiac Effects of Opiates - ANSWER-Little to no effect
Minimal bradycardia
Effects more pronounced in shock or ambulating patients
Groups of Endogenous Opioid Peptides (5) - ANSWER-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 - ANSWER-Proenkephalin A
Precursor to β-Endophins - ANSWER-Pro-opiomelanocortin (Pro-OMC)
Precursor to Dynorphins - ANSWER-Prodynorphin
Precursor to Endomorpins 1 & 2 - ANSWER-Unknown
Precursor to Nociceptin - ANSWER-Pronociceptin
Location of endogenous opioid peptides - ANSWER-Brain & Spinal cord
(second highest concentration in GI)
Delta receptor effects (5) - ANSWER-(AUGMENTS MU & KAPPA EFFECTS)
1. Analgesia (supraspinal and spinal)
2. Physical dependence
