Classes
DEA Class; Rx
Common Brand Names; Apadaz
- Analgesics, Opioid Combos
Description
Benzhydrocodone: Prodrug of hydrocodone, which is an opioid analgesic agonist; blocks pain perception in the cerebral cortex; decreases synaptic chemical transmission throughout the CNS, which in turn inhibits pain sensation into higher centers; when ingested, enzymes in the GI tract cleave the ligand from the prodrug (benzhydrocodone) and release the parent drug (hydrocodone)
Acetaminophen: Acts on the hypothalamus to produce antipyresis; inhibits prostaglandin synthetase
Indications
Indicated for short-term (ie, not to exceed 14 days) management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate
Use lowest effective dosage for the shortest duration consistent with individual patient treatment goals
Total dosage of benzhydrocodone/acetaminophen and any concomitant acetaminophen-containing products should not exceed 4000 mg/day of acetaminophen
Initiate dosing regimen for each patient individually, taking into account the severity of pain, patient response, prior analgesic treatment experience, and risk factors for addiction, abuse, and misuse
Contraindications
Significant respiratory depression
Acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment
Known or suspected gastrointestinal obstruction, including paralytic ileus
Hypersensitivity to hydrocodone or acetaminophen
Adverse Effects
>10%
Nausea (21.5%)
Somnolence (18.5%)
Vomiting (13%)
Constipation (12%)
Pruritus (11.5%)
1-10%
Dizziness (7.5%)
Headache (6%)
1-5%
Gastrointestinal disorder: Abdominal distension, abdominal pain, flatulence
General disorders and administration site conditions: Asthenia
Nervous system disorders: Presyncope, tremor
Respiratory, thoracic and mediastinal disorders: Dyspnea
Vascular disorders: Hot flush, hypotension
<1%
Eye disorders: Eye pruritus
Gastrointestinal disorders: Diarrhea, gastroesophageal reflux disease, hematemesis
General disorders and administration site conditions: Chest discomfort
Infections and infestations: Rhinitis
Nervous system disorders: Hypoesthesia, syncope
Psychiatric disorders: Agitation, euphoric mood, nightmare
Warnings
Contains benzhydrocodone, a Schedule II controlled substance; as an opioid, benzhydrocodone exposes users to the risks of addiction, abuse, and misuse (see Black Box Warnings)
Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even when used as recommended (see Black Box Warnings)
Opioids can cause sleep-related breathing disorders including central sleep apnea (CSA) and sleep-related hypoxemia; opioid use increases risk of CSA in a dose-dependent fashion; in patients who present with CSA, consider decreasing opioid dosage using best practices for opioid taper
Use in patients with acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment is contraindicated; life-threatening respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients because they may have altered pharmacokinetics or altered clearance
Do not abruptly discontinue buprenorphine in a patient physically dependent on opioids; when discontinuing therapy, in a physically dependent patient, gradually taper the dosage; rapid tapering in a patient physically dependent on opioids may lead to a withdrawal syndrome and return of pain
Pregnancy and Lactation
Pregnancy
Prolonged use of opioid analgesics during pregnancy can result in physical dependence in the neonate and neonatal opioid withdrawal syndrome shortly after birth (see Black Box Warnings)
Neonatal opioid withdrawal syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high pitched cry, tremor, vomiting, diarrhea and failure to gain weight
Onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing, amount of last maternal use, and rate of elimination of the drug by the newborn
Published studies with oral acetaminophen use during pregnancy have not reported an association with major congenital malformations
Lactation
Hydrocodone
Present in human milk
Variable concentrations of hydrocodone and hydromorphone (active metabolite) reported in breast milk when administered to nursing mothers in the early postpartum period
Potential for sedation and respiratory depression in the breastfed infant
Acetaminophen
Present in human milk in small quantities after PO administration
Maximum Dosage
Total dosage of benzhydrocodone/acetaminophen and any concomitant acetaminophen-containing products should not exceed 4000 mg/day of acetaminophen
Use as first opioid analgesic (ie, opioid-naïve): 1-2 tablets PO q4-6hr prn pain
Not to exceed 12 tablets/24 hr
Pediatric
<18 years: Safety and efficacy not established