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Pronunciation: zi-KOE-noe-tide
Class: Analgesic

Trade Names

- Solution 25 mcg/mL
- Solution 100 mcg/mL


Undetermined; however, animal data indicate that ziconotide blocks N-type calcium channels by binding to them, which leads to blockade of excitatory neurotransmitter release in primary afferent nerve terminals and antinociception.

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Following intrathecal administration, both total exposure and peak exposure values in the CSF were variable and dose-dependent but appear to be dose-proportional.


About 50% bound to plasma proteins. Mean CSF Vd approximates the CSF volume (140 mL).


Cleaved by endopeptidases and exopeptidases at multiple sites on the peptide. In the systemic circulation, ziconotide is expected to be susceptible to proteolytic cleavage in most organs (eg, kidney, liver, lung muscle), and thus degraded to peptide fragments and their individual free amino acid constituents.


Less than 1% of ziconotide is recovered in the urine. Terminal t ½ is approximately 4.6 h. Mean CSF Cl is about 0.3 to 0.4 mL/min.

Indications and Usage

Management of severe chronic pain in patients for whom intrathecal therapy is warranted, and who are intolerant of or refractory to other treatment.


Preexisting history of psychosis; infection at the microinfusion injection site, uncontrolled bleeding diathesis, spinal canal obstruction that impairs circulation of CSF, hypersensitivity to any component of the product.

Dosage and Administration


Intrathecal Start at no more than 2.4 mcg/day (0.1 mcg/h) and titrate to patient response. Doses may be titrated upward by up to 2.4 mcg/day (0.1 mcg/h) at intervals of no more than 2 to 3 times/wk (max, 19.2 mcg/day [0.8 mcg/h] by day 21). Dose increases in increments of less than 2.4 mcg/day (0.1 mcg/h) and increases in dose less frequently than 2 to 3 times/wk may be used. For each dose titration, assess the dosing requirements and adjust the pump infusion flow rate as required to achieve the new dosing.


Store vials in refrigerator (36° to 46°F). Ziconotide diluted with saline may be stored in refrigerator but infusion should begin with 24 h of preparation. Do not freeze. Protect from light. Discard any unused solution remaining in vial(s). Do not combine contents of vials or save for future use.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Hypertension, hypotension, postural hypotension, syncope, tachycardia, vasodilation (at least 2%); atrial fibrillation (less than 2%).


Dizziness (47%); confusion (33%); asthenia, memory impairment, somnolence, (22%); ataxia (16%); abnormal gait, headache (15%); speech disorder (14%); aphasia, hallucinations (12%); hypertonia (11%); anxiety (9%); nystagmus, abnormal thinking (8%); dysesthesia, hallucinations, nervousness, paresthesia, vertigo (7%); paranoid reactions (3%); delirium, hostility, unresponsiveness/stupor (2%); psychosis, vertigo (1%); abnormal CSF, abnormal dreams, agitation, decreased reflexes, depression, difficulty concentrating, dizziness, emotional lability, hostility, hyperesthesia, incoordination, malaise, meningitis, mental slowing, neuralgia, tremor, twitching (at least 2%); cerebrovascular accident, grand mal convulsion, meningitis, psychosis, suicidal ideations (less than 2%).


Cutaneous surgical complication, dry skin, pruritus, rash, skin disorder, sweating (at least 2%).


Abnormal vision (10%); diplopia, pharyngitis, photophobia, rhinitis, tinnitus (at least 2%).


Nausea (41%); diarrhea (19%); vomiting (15%); anorexia (10%); constipation, dry mouth, dyspepsia, GI disorder, taste perversion (at least 2%).


Urinary retention (9%); dysuria, impaired urination, urinary incontinence, UTI, (at least 2%); acute kidney failure (less than 2%).


Anemia, ecchymosis (at least 2%).

Lab Tests

Elevated creatine kinase (11%); ECG abnormalities (less than 2%).


Dehydration, hypokalemia, increased creatinine phosphokinase, peripheral edema, weight loss (at least 2%).


Arthralgia, arthritis, back pain, leg cramps, myalgia, myasthenia, neck pain, neck rigidity (at least 2%); myoclonus, rhabdomyolysis (less than 2%).


Bronchitis, dyspnea, increased cough, lung disorder, pneumonia, sinusitis (at least 2%); respiratory distress (less than 2%).


Pain (11%); fever (7%); abdominal pain, accidental injury, catheter complication, catheter site pain, cellulitis, chest pain, chills, edema, fever, flu syndrome, infection, pain, pump site complication, mass, or pain, viral infection (at least 2%); sepsis (less than 2%).



Severe psychiatric symptoms and neurological impairment may occur with ziconotide treatment. Frequently monitor all patients for evidence of cognitive impairment, hallucinations, or changes in mood or consciousness. If necessary, therapy can be interrupted or discontinued abruptly without evidence of withdrawal.


Category C .




Safety and efficacy not established.


Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.


Can occur because of inadvertent contamination of the microinfusion device and other means such as CSF seeding resulting from hematogenous or direct spread from an infected pump pocket or catheter tract.

Neuromuscular symptoms

Monitor patient for neuromuscular symptoms (eg, myalgia, myasthenia, muscle cramps) or reduction in physical activity. Ensure serum creatine kinase is periodically monitored during therapy with ziconotide (eg, every other week for first month and then monthly, as appropriate, thereafter). Be prepared to reduce the dose or discontinue ziconotide therapy.

Opiate withdrawal

Ziconotide is not an opiate, does not potentiate opiate-induced respiratory depression, and cannot prevent or relieve the symptoms of opiate withdrawal. To prevent opiate withdrawal syndrome, when opiate withdrawal is necessary, ensure patient is not abruptly withdrawn from opiates. Ensure the opiate IT infusion is tapered gradually over a few weeks and replaced with a pharmacologically equivalent dose of oral opiate.

Reduced consciousness

Patients may become unresponsive or stuporous.



Ataxia, confusion, dizziness, garbled speech, hypotension, nausea, nystagmus, sedation, spinal myoclonus, stupor, unresponsiveness, vomiting, word-finding difficulties.

Patient Information

  • To reduce risk of meningitis and other infections, ensure patient or caregiver with external microinfusion device is familiar with handling of the device and care of the catheter skin exit site.
  • Advise patient that medication usually is started at a low dose and then gradually increased as tolerated until max benefit is obtained.
  • Instruct patient to continue to take other medications for pain as prescribed by health care provider.
  • Advise patient to notify health care provider immediately if any of the following occur: change in mental status (eg, confusion, decreased alertness, disorientation, lethargy); change in mood or perceptions; symptoms of depression of suicidal ideation; symptoms of meningitis (eg, fever, headache, nausea, seizures, stiff neck, vomiting); new or worsening muscle pain, soreness, or weakness.
  • Caution patient that alcohol and other CNS depressants (eg, sedatives) will have additional sedative effects if taken while on ziconotide therapy.
  • Caution patient to avoid engaging in driving or performing other activities requiring complete mental alertness or motor coordination during treatment with ziconotide.

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