Brand Name: Targiniq ER
Generic Name: oxycodone hydrochloride and naloxone hydrochloride extended-release tablets, for oral use
Medication Class: Opioid analgesic agonist/antagonist
Similar drugs: buprenorphine/naloxone (Suboxone) and pentazocine/naloxone
Manufacturer: Purdue Pharma L.P.
FDA Approval Date: July 23, 2014
What is Targiniq ER and its mechanism of action?
Targiniq ER is an extended-release combination medication that contains oxycodone (an opioid agonist) and naloxone (an opioid antagonist). Oxycodone inhibits pain signals by binding to opioid receptors and producing a feeling of analgesia (pain relief). Opioid receptors are mainly found in the brain and spinal cord and can produce a feeling of euphoria when activated. This effect makes it prone to abuse. Targiniq is a schedule II controlled substance.
Naloxone works by competing with oxycodone for its receptor binding site and blocking or reversing its effect. Therefore, when Targiniq ER is crushed and snorted or dissolved and injected, naloxone blocks the euphoric effect of oxycodone, reducing the likelihood of abuse. Naloxone also produces symptoms of opioid withdrawal when injected by individuals who are physically dependent on opioid agonists such as oxycodone.
After oral absorption of Targiniq ER, oxycodone reaches its maximum plasma concentration within 3 to 4 hours with a bioavailability (amount absorbed) of 60 to 87%. The oral bioavailability of naloxone is 2% or less. However, after intranasal administration, the bioavailability of naloxone is much higher (31%). This property helps make Targiniq abuse-deterrent, since naloxone is activated when the drug is crushed and snorted. Steady-state plasma concentrations are reached in about 2 days for both oxycodone and naloxone.
The half-life (the amount of time it takes for the concentration to be reduced by half) is 3.9 to 5.3 hours for oxycodone and 4.1 to 17.2 hours for naloxone.
What is Targiniq ER used to treat?
Targiniq ER is used to treat pain that is severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are not adequate.
How effective is Targiniq ER?
A clinical study of 1,095 patients was done to determine how well Targiniq ER works compared to a placebo pill. These patients were opioid-experienced and had uncontrolled moderate to severe chronic low back pain. The duration of treatment was 12 weeks. 55% of patients on Targiniq ER achieved adequate pain relief and tolerability.
Interesting Facts about Targiniq ER
Targiniq ER is an extended release oxycodone formulation containing naloxone
It is a Schedule II controlled substance
Naloxone becomes activated to block the effects of oxycodone when the drug is crushed and snorted or dissolved and injected.
Targiniq has abuse-deterrent properties but there is still potential for abuse, misuse and addiction
What are the side effects of Targiniq ER?
The most common side effects are nausea and vomiting. It may also cause headache, constipation, abdominal pain and itching. Targiniq ER may also cause life-threatening respiratory depression (breathing problems), severe hypotension (low blood Pressure), and seizures or make existing seizures worse.
What is the dosage of Targiniq ER?
Targiniq ER is available as oral tablets in the following strengths:
oxycodone 10 mg/ naloxone 5 mg
oxycodone 20 mg/ naloxone 10 mg
oxycodone 40 mg/ naloxone 20 mg
The recommended starting dose for opioid-naive and people who are not opioid tolerant is 10 mg/5 mg tablets orally every 12 hours. The dose may be increased by 10 mg/5 mg every 12 hours every 1-2 days.
The total daily dose should not exceed 80 mg/40 mg (40 mg/20 mg every 12 hours) because higher doses may be associated with symptoms of opioid withdrawal.
What are the drug interactions of Targiniq ER?
The following are examples of drugs that may interact with Targiniq ER:
Central, nervous system depressants such as diazepam, zolpidem, alcohol, and other opioids can increase the risk of respiratory depression (breathing problems), hypotension (low blood pressure), sedation, coma, or death.
Liver enzyme inhibitors such as ketoconazole and ritonavir inhibit the enzyme that metabolizes oxycodone. This could lead to an increase in the concentration of oxycodone and the risk of fatal overdose.
Liver enzyme inducers such as rifampin and St. John’s wort increase the Activity of enzymes that breakdown oxycodone. This could reduce the concentration and effectiveness of oxycodone or result in abstinence syndrome.
Mixed agonist/antagonists (such as pentazocine) and partial agonist opioids (such as buprenorphine) can cause withdrawal symptoms or reduce the analgesic effect of Targiniq ER.
Oxycodone may increase the effect of muscle relaxants and the risk of respiratory depression.
Targiniq ER can reduce the effectiveness of diuretics by inducing the release of antidiuretic hormone. It may also cause bladder spasms and urinary retention especially in men with enlarged prostates.
Anticholinergic drugs such as diphenhydramine (Benadryl) can increase the risk of constipation and urinary retention when used together with Targiniq ER.
There are other medications that can interact with Targiniq ER. Patients should consult their physician or pharmacist to confirm drug interactions with specific products.
What are the warnings and precautions for Targiniq ER?
Targiniq ER can cause addiction, abuse and misuse.
The extended release formulation increases the risk of overdose and death.
Elderly, debilitated and patients with COPD are at an increased risk for life-threatening respiratory depression. Avoid use of Targiniq ER in patients with impaired consciousness or coma due to the added risk of sedation.
Targiniq ER should not be suddenly discontinued in a physically dependent patient. It may cause abstinence syndrome. When discontinuing Targiniq ER in any patient, the dose should be gradually tapered.
Targiniq ER tablets must be swallowed whole and should not to be cut, broken, chewed, crushed, or dissolved due to risk of fatal overdose.
It should be kept out of children’s reach. Accidental ingestion and overdosing can lead to serious breathing problems and death.
Use of Targiniq ER should be avoided in patients with circulatory shock due to the risk of severe hypotension.
Targiniq ER may cause or worsen seizures in patients with seizure disorders.
Use of Targiniq ER is contraindicated in patients with:
Severe respiratory depression
Acute or severe asthma
Gastrointestinal obstruction and paralytic ileus (paralysis of the intestinal muscles)
Hypersensitivity to oxycodone or naloxone
Moderate to severe liver impairment
Pregnancy Category C: Prolonged use during pregnancy can cause opioid withdrawal syndrome in newborns.
Nursing mothers: Targiniq ER is likely secreted in breast milk and may cause sedation and respiratory depression in an infant
What is the cost of Targiniq ER?
The cost of Targiniq ER has not yet been finalized.