Opioid Drugs Flashcards
1
Q
List the common opioid drugs (and their relative strengths)
A
Morphine - strong agonist Fentanyl - strong agonist Codeine - moderate agonist Buprenorphine - mixed agonist and antagonist Naloxone - antagonist
2
Q
List the following for: Morphine
- Use
- Drug class
- Mechanism of action
- Adverse effects
- Warnings / contraindications
A
Analgesia (and euphoria)
Opioid
Strong agonist
- Strong affinity to Mu receptor (complete activation)
- Respiratory Depression
- Emesis
- GI tract – constipation and nausea
- Cardiovascular
- Miosis
- Histamine release (asthmatics)
- Manual labourers/Drivers
- Elderly
- Bed-bound
- Asthmatics
- Biliary tract obstruction
- Respiratory Diseases
- Renal impairment
- Pregnancy
3
Q
List the following for: Fentanyl
- Use
- Drug class
- Mechanism of action
- Adverse effects
- Warnings / contraindications
A
- Analgesia
- Anaesthetic
Opioid
Strong agonist
- Higher affinity to Mu receptor compared to Morphine
- 100Xs greater potency compared to Morphine
- Respiratory Depression
- Constipation
- Nausea / vomitting
Less histamine release, sedation and constipation - Manual labourers/drivers
- Elderly
- Bed-bound
- Asthmatics
- Biliary tract obstruction
- Respiratory Diseases
- Renal impairment
- Pregnancy
4
Q
List the following for: Codeine
- Use
- Drug class
- Mechanism of action
- Adverse effects
- Warnings / contraindications
A
- Mild-moderate analgesia
- Cough depressant
Opioid
Moderate agonist
- Approx. 1/10th potency compared to morphine
- Respiratory Depression (worse in children)
- Constipation
- Nausea / vomitting
- Manual labourers/drivers
- Elderly
- Bed-bound
- Asthmatics
- Biliary tract obstruction
- Respiratory Diseases
- Renal impairment
- Pregnancy
5
Q
List the following for: Buprenorphine
- Use
- Drug class
- Mechanism of action
- Adverse effects
- Warnings / contraindications
A
- Moderate to severe pain
- Opioid addiction treatment
Opioid
Compared to morphine:
Mixed agonist-antagonist
- Very high affinity for Mu receptor – Low Kd
- Long duration of action
- Not easily displaced
- Lower E(max) as partial agonist, lower efficacy
- Antagonist at κ receptors
- Respiratory depression
- Low BP
- Nausea
- Dizziness
- Manual labourers/drivers
- Elderly
- Bed-bound
- Asthmatics
- Biliary tract obstruction
- Respiratory Diseases
- Renal impairment
- Pregnancy
6
Q
List the following for: Naloxone
- Use
- Drug class
- Mechanism of action
- Adverse effects
A
Reverse overdose - competitive antagonism of opioid
Opioid
Compared to morphine: ANTAGONIST – competitive antagonism of opioid - Affinity μ>δ>κ - Greater affinity than morphine - Affinity less than buprenorphine
- Short half life
- Slow infusion
