Zohydro Er (hydrocodone bitartrate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Hydrocodone bitartrate is a phenanthrene-derivative opioid agonist.
Hydrocodone bitartrate is a phenanthrene-derivative opioid agonist that is used as an analgesic and antitussive agent. Hydrocodone is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. The principal therapeutic action of hydrocodone is analgesia; however, the precise mechanism of analgesic action is unknown.
Specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug. Like all full opioid agonists, there is no ceiling effect for analgesia with hydrocodone. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.
Hydrocodone produces respiratory depression by direct action on brainstem respiratory centers. Other opioid-induced effects may include a reduction in biliary and pancreatic secretions, spasm of sphincter of Oddi, and transient elevations in serum amylase. Cardiovascular effects of the drug include peripheral vasodilation, which may result in orthostatic hypotension or syncope, inhibition of adrenocorticotropic hormone (ACTH), cortisol, and luteinizing hormone (LH) secretion, and stimulation of prolactin, growth hormone, and pancreatic secretion of insulin and glucagon.
Hydrocodone is believed to act centrally on the cough center, which may contribute to its therapeutic effects in the management of cough; however, the exact mechanism is not known.
Overall systemic exposure or bioavailability of hydrocodone bitartrate following administration as extended-release capsules or tablets is similar to that observed following administration of immediate-release fixed-combination preparations containing the drug in the same or similar dosage; however, peak plasma concentrations of the drug are lower with the extended-release formulations. Peak plasma concentrations of hydrocodone are attained approximately 5 hours after administration as extended-release capsules, and 6-30 hours after administration as extended-release tablets. After administration of the extended-release capsules for 7 days, AUC and peak concentrations of hydrocodone are approximately 2-fold higher than values attained on the first day of administration.
Administration of the extended-release capsules with food does not substantially affect the extent of absorption, although peak plasma hydrocodone concentrations were increased by 27% following administration of a 20-mg dose of the extended-release capsules with a high-fat meal.
After single-dose administration of hydrocodone bitartrate extended-release tablets, peak concentrations and AUC of the drug increased linearly and in a slightly more than dose-proportional manner over the dose range of 20-120 mg. With once-daily dosing, peak plasma concentrations and AUC were 1.1- and 1.3-fold higher at steady state. Higher doses (80 or 120 mg versus 30 mg) produced larger fluctuations in peak-to-trough plasma concentrations of the drug.
Although administration of the 120-mg extended-release tablets with a high-fat meal increased peak plasma concentrations by 54% compared with administration in the fasted state, AUC was increased by only 20% and the manufacturer states that the extended-release tablets may be administered without regard to meals.
Hydrocodone is metabolized by N-demethylation, O-demethylation, and 6-keto reduction to the corresponding 6-alpha- and 6-beta-hydroxy metabolites. Hydrocodone is metabolized principally by cytochrome P-450 (CYP) isoenzyme 3A4 to form norhydrocodone (N-demethylation) and to a lesser extent by CYP2D6 to form hydromorphone (O-demethylation). Hydromorphone accounts for less than 3% of the circulating parent drug, but may contribute to the total analgesic effect of hydrocodone.
Hydrocodone and its metabolites are eliminated mainly in urine; only about 6.5% of an administered dose is excreted as unchanged drug. About 99% of an administered dose is eliminated within 72 hours. The mean plasma half-life is approximately 7-9 hours after oral administration as extended-release capsules or tablets.
Hydrocodone is about 36% bound to plasma proteins.
USES: Hydrocodone is used to help relieve severe ongoing pain. Hydrocodone belongs to a class of drugs known as opioid analgesics. It works in the brain to change how your body feels and responds to pain.
Do not use the extended-release form of hydrocodone to relieve pain that is mild or that will go away in a few days. This medication is not for occasional ("as needed") use.
Generic name: hydrocodone bitartrate
Pronunciation: (HYE-droe-KOE-done)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Zohydro Er
Indications
The following indications are listed for Zohydro Er:
- Severe Chronic Pain Requiring Long-Term Opioid Treatment
Dosing
Dosage of hydrocodone bitartrate and hydrocodone polistirex is expressed in terms of hydrocodone bitartrate.
Hydrocodone-containing preparations are administered orally.
Hydrocodone bitartrate is commercially available as single-entity extended-release tablets or capsules and in various fixed-combination oral preparations with acetaminophen, ibuprofen, or aspirin for the management of pain. Hydrocodone bitartrate is also commercially available in various fixed combination preparations with chlorpheniramine or homatropine methylbromide for the management of cough. See the full prescribing information for additional information on fixed combination preparations.
Store hydrocodone extended-release capsules and tablets at 25degreesC (excursions permitted between 15-30degreesC) in tight, light-resistant containers in a secure location.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Significant respiratory depression.
*Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment.
*Known or suspected GI obstruction, including paralytic ileus.
*Hypersensitivity to hydrocodone or any ingredient in the formulations.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects reported in patients receiving hydrocodone bitartrate extended-release tablets are constipation, nausea, vomiting, fatigue, upper respiratory tract infection, dizziness, headache, and somnolence; common adverse effects in patients receiving hydrocodone bitartrate extended-release capsules include constipation, nausea, somnolence, fatigue, headache, dizziness, dry mouth, vomiting, pruritus, abdominal pain, peripheral edema, upper respiratory tract infection, muscle spasms, urinary tract infection, back pain, and tremor.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The safety and effectiveness of hydrocodone bitartrate extended-release capsules and tablets have not been established in pediatric patients.
Use of opioid analgesics for an extended period of time during pregnancy may cause neonatal opioid withdrawal syndrome.
Available data with extended-release hydrocodone preparations in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage.
Opioids cross the placenta and may produce respiratory depression and psycho-physiologic effects in neonates. An opioid antagonist, such as naloxone, must be available for reversal of opioid-induced respiratory depression in the neonate. Monitor neonates exposed to opioid analgesics during labor for signs of excessive sedation and respiratory depression.
Hydrocodone is present in human milk. Variable concentrations of hydrocodone and hydromorphone (an active metabolite) have been detected in breast milk with administration of immediate-release hydrocodone to nursing mothers in the early post-partum period. Because of the potential for serious adverse reactions, including excess sedation and respiratory depression in a breastfed infant, advise patients that breastfeeding is not recommended during treatment with hydrocodone.
In general, select dosage with caution for an elderly patient, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy. When used for the management of pain, titrate slowly in geriatric patients and frequently reevaluate the patient for signs of CNS and respiratory depression.
Geriatric patients may have increased sensitivity to hydrocodone. Use caution when selecting dosage. Respiratory depression is the main risk for geriatric patients treated with opioids and has occurred after administration of large initial doses in patients who were not opioid-tolerant or when opioids were co-administered with other drugs that depress respiration. Titrate dosage slowly and frequently re-evaluate patients for signs of CNS and respiratory depression.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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