Meperidine is an opioid agonist with analgesic and sedative properties used to manage severe pain. A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor.
- Mechanism
- Curator reviewed
Meperidine is primarily a kappa-opiate receptor agonist and also has local anesthetic effects. Meperidine has more affinity for the kappa-receptor than morphine. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
- Primary indication
- Used to control moderate to severe pain.Curator reviewed · 7 structured indications
- Formula / weight
- C15H21NO2 · 247.3327 g/mol (avg)
- First approval
- Canada, 2004 · United States, 1942
- Also known as
- Isonipecaïne · Pethidine
- Code names
- IDS-NP-001
- Brand names
Resolves to
XADCESSVHJOZHK-UHFFFAOYSA-NSMILESCCOC(=O)C1(CCN(C)CC1)C1=CC=CC=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Meperidine, and which of those have an active Phase 3 trial?
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