ziconotide


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ziconotide

(zi-ko-no-tide) ,

Prialt

(trade name)

Classification

Therapeutic: analgesics
Pharmacologic: n type calcium channel blockers
Pregnancy Category: C

Indications

Management of severe chronic pain when conventional therapies (analgesics or other adjunctive measures) have failed.

Action

Blocks spinal N-channel calcium channels, decreasing transmission of pain signals to the brain.
Has no effect on opioid receptors.

Therapeutic effects

Decrease in severe pain.

Pharmacokinetics

Absorption: IT administration results in complete bioavailability in the CSF. Minimal plasma distribution.
Distribution: Distributes in entire CSF volume.
Metabolism and Excretion: Degraded by enzymes in tissues and fluids.
Half-life: 4.6 hr (in CSF).

Time/action profile

ROUTEONSETPEAKDURATION
ITrapid2–3 daysunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity; History of psychosis; Infection at microinfusion injection site; Uncontrolled bleeding; Spinal cord obstruction; Lactation: Can cause sedation and side effects in the infant.
Use Cautiously in: History of suicidal ideation/psychiatric disorder; Pediatric: Safety not established; Obstetric: Pregnancy; Geriatric: ↑ susceptibility to adverse CNS effects.

Adverse Reactions/Side Effects

Central nervous system

  • meningitis (life-threatening)
  • confusion (most frequent)
  • dizziness (most frequent)
  • drowsiness (most frequent)
  • headache (most frequent)
  • impaired memory (most frequent)
  • weakness (most frequent)
  • aphasaia
  • ↓ alertness/responsiveness
  • cognitive impairment
  • hallucinations
  • memory impairment
  • psychiatric symptoms
  • speech disorder

Cardiovascular

  • changes in BP

Ear, Eye, Nose, Throat

  • nystagmus (most frequent)
  • abnormal vision

Gastrointestinal

  • nausea (most frequent)
  • anorexia
  • vomiting

Local

  • catheter/injection site reactions

Musculoskeletal

  • hypertonia (most frequent)
  • urinary retention (most frequent)
  • ↑ creatine kinase

Neurologic

  • abnormal gait (most frequent)
  • ataxia (most frequent)

Miscellaneous

  • fever

Interactions

Drug-Drug interaction

↑ risk of CNS depression with other CNS depressants including anticonvulsants, phenothiazines, antipsychotics, antihistamines, opioids, sedatives, or diuretics.

Route/Dosage

Intrathecal (Adults) up to 2.4 mcg/day initially (0.1 mcg/hr), may be gradually ↑ 2–3 times/wk in increments of 2.4 mcg/day up to a maximum of 19.2 mcg/day (0.8 mcg/hr) over 21 days.

Availability

Solution for intrathecal use: 25 mcg/mL, 100 mcg/mL

Nursing implications

Nursing assessment

  • Assess level of pain prior to and periodically during therapy.
  • Assess mental status during therapy. If psychiatric symptoms (cognitive impairment, hallucinations, changes in mood or level of consciousness) or neurological impairment. Discontinuation of therapy may be required, but other causes should be considered. Ziconotide may be discontinued abruptly without withdrawal symptoms.
  • Monitor for signs of meningitis (fever, headache, stiff neck, altered mental status, nausea, vomiting, seizures) frequently during therapy. May occur within 24 hr of breach in sterility. If meningitis occurs, obtain CSF cultures and institute antibiotic therapy. Usually requires removal of microinfusion system, catheter, and any other foreign body within the IT space.
  • Lab Test Considerations: Monitor serum CK levels every other week for the first month, monthly thereafter, and if neuromuscular symptoms (myalgias, myasthenia, muscle cramps, asthenia, reduction in physical activity) occur. May cause ↑CK levels. If symptoms continue and CK remains ↑ or continues to rise, dose reduction or discontinuation may be required.

Potential Nursing Diagnoses

Chronic pain (Indications)

Implementation

  • Ziconotide is not an opioid and cannot prevent or relieve symptoms of opioid withdrawal. Do not discontinue opioids abruptly. For withdrawal from IT opioid, gradually taper opioid IT infusion over several weeks, and replace with an equianalgesic dose of oral opioids. Ziconotide does not potentiate opioid-induced respiratory depression.
    • Ziconotide should be administered under the direction of a physician experienced in IT therapy. Do not administer IV.
  • Intrathecal: IT dose is delivered using a programmable implanted variable-rate microinfusion device or an external microinfusion device and catheter. Ziconotide may be administered undiluted (25 mcg/mL in 20-mL vial) or diluted (100 mg/mL in 1-, 2-, or 5-mL vials). Dilute with 0.9% NaCl (preservative—free) using aseptic technique. 100 mg/mL formulation may be administered undiluted once an appropriate dose is established. Refrigerate, but do not freeze, after preparation; administer within 24 hr. Discard solution if discolored or containing particulate matter or any unused portion in vial. Pump refills should be done every 40 days if diluted solution is used or every 60 days if solution is undiluted. Pump should be rinsed and filled according to manufacturer's directions.
  • Rate: Dose should be adjusted according to patient's severity of pain, response to therapy, and occurrence of side effects.

Patient/Family Teaching

  • Instruct patient on correct technique for care of equipment.
  • May cause dizziness and drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to ziconotide is known.
  • Advise patient to avoid taking alcohol and other CNS depressants during ziconotide therapy. Consult health care professional prior to taking Rx, OTC, or herbal products during therapy.
  • Instruct patient and caregiver to contact health care professional immediately if changes in mental status (lethargy, confusion, disorientation, decreased alertness), changes in mood or perception (hallucinations, including unusual tactile sensations in oral cavity), symptoms of depression or suicidal ideation, or nausea, vomiting, seizures, fever, headache, or still neck occur; may be symptoms of developing meningitis.
  • Advise patient to consult health care professional if new or worsening muscle pain, soreness, or weakness with or without darkened urine occur.

Evaluation/Desired Outcomes

  • Decrease in pain intensity.
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References in periodicals archive ?
In the second quarter of 2018, GAAP net income included an impairment charge of $42.9 million resulting from the company's sale of its rights related to Prialt (ziconotide) intrathecal infusion.
Cone shells contain therapeutically useful peptides including the conotoxins, and one such peptide, ziconotide, has been approved.
Eisai's medicines in Europe include Aricept[R] (donepezil hydrochloride) used in the treatment of Alzheimer's disease, Pariet[R] (rabeprazole sodium) a proton pump inhibitor (PPI) used in the treatment of gastro-intestinal disorders, Zonegran[R] (zonisamide) for the treatment of epilepsy, Inovelon[R] (rufinamide) for Lennox Gastaut Syndrome, NeuroBloc[R] (botulinum toxin type B) for cervical dystonia and Prialt[R] (ziconotide) for severe, chronic pain.
SynchroMed II was initially indicated to administer Infumorph (a morphine sulfate sterile solution) to treat chronic intractable pain and Prialt (a ziconotide sterile solution) to manage severe chronic pain.
announced today that it has entered into an agreement to transfer the exclusive development and marketing rights for the non-opioid severe chronic pain treatment Prialt (ziconotide acetate) in Europe to Riemser Pharma GmbH.
Ziconotide - A novel neuron-specific calcium channel blocker for the intrathecal treatment of severe chronic pain - A short review.
The first ever marine derived product to gain approval as a potential anticancer drug is Ziconotide, a non-narcotic analgesic that is currently marketed as PrialtA(r) [1].
The discovery of ziconotide (Prialt[R]), a unique non-opioid analgesic that is an N-type calcium channel blocker, has its roots beginning in the 1940s when a young Filipino boy, Baldomero Olivera, would sort seashells while waiting for his father to finish playing tennis at a local club.
Toxins from cone snails such as [omega]-conotoxin MVIIA or Ziconotide, initially purified as SNX-111, is a potent reversible blocker of N type calcium channels (OLIVERA et al., 1985), capable to inhibit, in synaptosomes, neurotransmitters release such as norepinephrine (BOWERSOX et al., 1995) and glutamate (GONCAVES et al., 2011), essential in the development of secondary spinal injury.
Ten years ago, the FDA approved a license for the drug Prialt (Ziconotide), manufactured by Elan Corp., which is derived from the toxin of a small oceanic Cone Snail (Conus magnus).
Though ziconotide, the only drug created from conotoxins is available to treat pain, it is less used as it involves an invasive method of infusing the drug directly into the spinal cord.