Questions and Answers
Which statement about opioid analgesic drugs is correct?
Prolonged use can lead to addiction
Which of the following is a natural alkaloid opioid agonist?
Codeine
What is the main constituent of the opium alkaloids?
Morphine
Which of the following is a mixed agonist-antagonist opioid?
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What is the oral bioavailability of morphine?
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Which of the following is an endogenous natural opioid peptide?
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What is the mechanism of action of morphine and related compounds?
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Which of the following statements about papaverine is correct?
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Which of the following is a semisynthetic opioid agonist?
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What is the primary metabolic pathway for morphine?
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Which type of pain are opioid analgesic drugs NOT effective in treating?
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Which of the following is a natural alkaloid opioid agonist derived from opium?
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Which of the following opioids is classified as a mixed agonist-antagonist?
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What is the primary metabolic product of morphine in the liver?
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Which of the following endogenous natural opioid peptides bind to opioid receptors?
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What is the primary route of excretion for morphine?
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Which of the following opioids has negligible CNS action and is spasmolytic on smooth muscles?
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Which of the following opioids are primarily used parenterally due to low oral bioavailability?
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Which opioids act on opioid receptors present in both the CNS and peripheral tissues?
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Which of the following opioids induces euphoria along with its analgesic effects?
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Which one of the following opioid agonists is a synthetic compound?
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What is the primary reason why morphine is typically administered parenterally rather than orally?
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Which of the following endogenous natural opioid peptides is responsible for inducing euphoria and analgesia when binding to opioid receptors?
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Which type of pain are opioid analgesic drugs LEAST effective in treating?
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Which of the following statements about papaverine is CORRECT?
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Which of the following is the PRIMARY metabolic pathway for morphine in the liver?
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Which of the following opioid agonists is classified as a natural alkaloid derived from the opium plant?
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Which of the following statements about the mechanism of action of opioid analgesic drugs is CORRECT?
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Which of the following opioid agonists is classified as a semisynthetic compound?
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Which of the following statements about mixed agonist-antagonist opioids is CORRECT?
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Study Notes
Opioid Analgesic Drugs
- Opioid analgesic drugs are CNS depressants, potent analgesics for all types of pain (except itching), without loss of consciousness, and prolonged use leads to addiction.
Opioid Agonists
- Natural alkaloids: Morphine and Codeine, which are analgesic, addictive (centrally acting), and spasmogenic on smooth muscles, producing euphoria.
- Semisynthetic: Diacetyl Morphine.
- Synthetic: Meperidine, Methadone, and Fentanyl.
Mixed Agonist Antagonist Opioids
- Pentazocine, Butorphanol, and Nalbuphine.
Morphine
Pharmacokinetics
- Adequately absorbed from the gut, but oral bioavailability is 25%, so it is used parenterally.
- Conjugated in the liver with glucuronic acid to form Morphine-6-Conjugate, which is active.
- Excreted in urine partly unchanged and partly excreted in saliva, bile, milk, and stomach.
Mechanism of Action
- Morphine and related compounds act on "stimulate receptor" opioid receptors present in CNS and peripheral tissue, such as gut and adrenal medulla, and smooth muscle.
- Endogenous natural opioid peptides, such as endorphins, enkephalins, and dynorphins, bind to opioid receptors.
Papaverine
- Has negligible CNS action and is spasmolytic on smooth muscles.
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