Ziconotide
- Atc Codes:N02BG08
- CAS Codes:107452-89-1
- PHARMGKB ID:107452-89-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Prialt; Cyprus: Prialt; Czech Republic: Prialt; Denmark: Prialt; Estonia: Prialt; Finland: Prialt; France: Prialt; Germany: Prialt; Greece: Prialt; Hungary: Prialt; Ireland: Prialt; Italy: Prialt; Latvia: Prialt; Lithuania: Prialt; Luxembourg: Prialt; Malta: Prialt; Netherlands: Prialt; Poland: Prialt; Portugal: Prialt; Romania: Prialt; Slovakia: Prialt; Slovenia: Prialt; Spain: Prialt; Sweden: Prialt; UK: Prialt.
North America
USA: Prialt.
Drug combinations
Chemistry
Ziconotide: C~102~H~172~N~36~O~32~S~7~. Mw: 2639.13. (1) ω-Conotoxin M VIIA; (2) L-Cysteinyl-L-lysylglycyl-L-lysylglycyl-L-alanyl-L-lysyl-L-cysteinyl-L-seryl-L-arginyl-L-leucyl-L-methionyl-L-tyrosyl-L-α-aspartyl-L-cysteinyl-L-cysteinyl-L-threonylglycyl-L-seryl-L-cysteinyl-L-arginyl-L-serylglycyl-L-lysyl-L-cysteinamide cyclic (1→16),(8→20),(15→25)-tris(disulfide). CAS-107452-89-1 (1997).
Pharmacologic Category
Analgesics and Antipyretics, Miscellaneous. Nonopioid Analgesic. N-Type Calcium Channel Blocker. (ATC-Code: N02BG08).
Mechanism of action
Ziconotide selectively binds to N-type voltage-sensitive calcium channels located on nociceptive afferent nerves of dorsal horn in spinal cord. This binding is thought to block N-type calcium channels, leading to blockade of excitatory neurotransmitter release and reducing sensitivity to painful stimuli.
Therapeutic use
Management of severe chronic pain in intrathecal (I.T.) therapy.
Pregnancy and lactiation implications
Maternal toxicity noted. There are as yet no adequate, well-controlled studies in pregnant women. Not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to ziconotide or any component of the formulation. History of psychosis. I.V. administration. I.T. administration contraindicated in infection at injection site, uncontrolled bleeding, or spinal canal obstruction which impairs CSF circulation.
Warnings and precautions
Severe psychiatric symptoms and neurological impairment reported. Cognitive impairment may appear gradually during treatment (generally reversible after discontinuation). May cause CNS depression. Elevated serum creatine kinase can occur (particularly during first 2 months of therapy). Meningitis may occur with use of I.T. pumps. Safety and efficacy not established in hepatic and renal impairment. May have additive effects with CNS-depressant medications. May have additive CNS effects with opiates and may potentiate opioid-induced decreased GI motility. Does not interact with opioid receptors or potentiate opiate-induced respiratory depression. Use with caution in the elderly (higher incidence of confusion). Ziconotide therapy can be interrupted abruptly or discontinued without evidence of withdrawal. Contraindicated in history of psychosis. Concomitant use with psychotropic agents may produce additive sedative effects. GI side-effects common. Concomitant use with SSRIs, valproic acid, or lithium may produce additive effects.