Indications
Extended-release product: Management of pain that
is severe enough to warrant daily, around-the-clock,
long-term opioid treatment where alternative treatment
options are inadequate. Combination products:
Management of moderate to severe pain. Antitussive
(usually in combination products with decongestants).
Action
Bind to opiate receptors in the CNS. Alter the perception
of and response to painful stimuli while producing
generalized CNS depression. Suppress the cough reflex
via a direct central action. Therapeutic Effects:
Decrease in severity of moderate pain. Suppression of
the cough reflex.
Pharmacokinetics
Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Mostly metabolized
by the liver; eliminated in the urine (50–60% as metabolites,
10% as unchanged drug).
Half-life: 2.2 hr; Extended-release—8 hr.
TIME/ACTION PROFILE (analgesic effect)
ROUTE ONSET PEAK DURATION
PO 10–30 min 30–60 min 4–6 hr
PO-ER unknown unknown unknown
Contraindications/Precautions
Contraindicated in: Hypersensitivity to hydrocodone
(cross-sensitivity may exist to other opioids); Significant
respiratory depression; Paralytic ileus; Acute or
severe bronchial asthma or hypercarbia; Congenital
long QT syndrome (Hysingla only); Hypersensitivity to
acetaminophen/ibuprofen (for combination products);
Ibuprofen-containing products should be avoided in
patients with bleeding disorders or thrombocytopenia;
Acetaminophen-containing products should be avoided
in patients with severe hepatic or renal disease; Ibuprofen-
containing products should be avoided in patients
undergoing coronary artery bypass graft surgery; OB,
Lactation: Avoid chronic use; Products containing alcohol,
aspartame, saccharin, sugar, or tartrazine (FDC
yellow dye #5) should be avoided in patients who have
hypersensitivity or intolerance to these compounds.
Use Cautiously in: Head trauma;qintracranial
pressure; Severe renal, hepatic, or pulmonary disease;
Cardiovascular disease (ibuprofen-containing products
only); History of peptic ulcer disease (ibuprofen-containing
products only); Alcoholism; Difficulty swallowing;
Patients with undiagnosed abdominal pain; Prostatic
hyperplasia; OB: Labor and delivery; OB, Lactation:
Avoid chronic use; prolonged use of opioids during
pregnancy can result in neonatal opioid withdrawal
syndrome; Geri: Geriatric or debilitated patients (initial
doseprequired; more prone to CNS depression, constipation).
Adverse Reactions/Side Effects
Noted for hydrocodone only; see acetaminophen/ibuprofen
monographs for specific information on individual
components.
CNS: confusion, dizziness, sedation, euphoria, hallucinations,
headache, unusual dreams. EENT: blurred vision,
diplopia, miosis. Resp: respiratory depression.
CV: hypotension, bradycardia, QT interval prolongation
(Hysingla only). GI: constipation, dyspepsia, nausea,
choking, dysphagia, esophageal obstruction, vomiting.
GU: urinary retention. Endo: adrenal
insufficiency. Derm: sweating. Misc: physical dependence,
psychological dependence, tolerance.
Interactions
Drug-Drug: Use with extreme caution in patients receiving
MAO inhibitors; may produce severe, unpredictable
reactions—do not use within 14 days of each
other. Concurrent use of CYP3A4 inhibitors including
ritonavir, ketoconazole, itraconazole, fluconazole,
clarithromycin, erythromycin, nefazodone,
diltiazem, verapamil, nelfinavir, and fosamprenavirqlevels
and risk of opioid toxicity; careful monitoring
during initiation, dose changes, or discontinuation
of the inhibitor is recommended. Concurrent use with
CYP3A4 inducers including barbiturates, carbamazepine,
efavirenz, corticosteroids, modafinil,
nevirapine, oxcarbazepine, phenobarbital, phenytoin,
rifabutin, or rifampin maypfentanyl levels
and analgesia; if inducers are discontinued or dosage p,
patients should be monitored for signs of opioid toxicity
and necessary dose adjustments should be made.
Use with benzodiazepines or other CNS depressants
including otheropioids, non-benzodiazepine
sedative/hypnotics, anxiolytics, general anesthetics,
muscle relaxants, antipsychotics, and alcohol
may cause profound sedation, respiratory depression,
coma, and death; reserve concurrent use for when alternative
treatment options are inadequate. Administration
of partial antagonist opioids (buprenorphine,
butorphanol, nalbuphine, or pentazocine) mayp
analgesia or precipitate opioid withdrawal in physically
dependent patients. Anticholinergic drugs mayq
risk of urinary retention and constipation. Drugs that
affect serotonergic neurotransmitter systems, including
tricyclic antidepressants, SSRIs, SNRIs, MAO inhibitors,
TCAs, tramadol, trazodone, mirtazapine,
5–HT3 receptor antagonists, linezolid,
methylene blue, and triptansqrisk of serotonin syndrome.
Drug-Natural Products: Concomitant use of
kava-kava, valerian, skullcap, chamomile, or
hops canqCNS depression.
Route/Dosage
PO (Adults): Analgesic—2.5–10 mg q 3–6 hr as
needed; if using combination products, acetaminophen
dosage should not exceed 4 g/day and should not exceed
5 tablets/day of ibuprofen-containing products;
Antitussive—5 mg q 4–6 hr as needed; Extended-release
(Zohydro ER)—10 mg q 12 hr; mayqas needed
in increments of 10 mg q 12 hr q 3–7 days; Extendedrelease
(Hysingla)—20 mg once daily; mayqas
needed in increments of 10–20 mg/day q 3–5 days.
PO (Children): Analgesic (1–13 yr)—0.1–0.2 mg/
kg q 3–4 hr. Antitussive —0.6 mg/kg/day divided q
6–8 hr; (maximum doses 2 yr: 1.25 mg/dose; 2–12
yr: 5 mg/dose; 12 yr: 10 mg/dose).
Renal Impairment
PO (Adults): CCr 45 mL/min—Extended-release
(Hysingla):pinitial dose by 50%.
Hepatic Impairment
PO (Adults): Extended-release (Hysingla)—pinitial
dose by 50%.
Availability
Hydrocodone (generic available)
Extended-release capsules (Zohydro ER) (abuse
deterrent): 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 50
mg. Extended-release tablets (Hysingla ER)
(abuse deterrent): 20 mg, 30 mg, 40 mg, 60 mg, 80
mg, 100 mg, 120 mg. Syrup: 1 mg/mL. In combination
with: chlorpheniramine (Tussicaps, Tussionex,
Vituz); chlorpheniramine and pseudoephedrine
(Zutripro); guaifenesin (Flowtuss, Obredon); guaifenesin
and pseudoephedrine (Hycofenix); pseudoephedrine
(Rezira). See Appendix B.
Hydrocodone/Acetaminophen (generic
available)
Tablets: 2.5 mg hydrocodone/325 mg acetaminophen,
5 mg hydrocodone/325 mg acetaminophen (Anexsia 5/
325, Norco), 7.5 mg hydrocodone/325 mg acetaminophen
(Anexsia 7.5/325, Norco), 10 mg hydrocodone/
325 mg acetaminophen (Norco). Cost: Generic—5
mg/325 mg $15.08/100, 7.5 mg/325 mg $30.93/100,
10 mg/325 mg $41.59/100. Elixir/oral solution: 7.5
mg hydrocodone plus 325 mg acetaminophen/15 mL,
10 mg hydrocodone plus 325 mg acetaminophen/15
mL. Cost: Generic—$58.12/473 mL.
Hydrocodone/Ibuprofen (generic available)
Tablets: 2.5 mg hydrocodone/200 mg ibuprofen (Reprexain),
5 mg hydrocodone/200 mg ibuprofen, 7.5
mg hydrocodone/200 mg ibuprofen, 10 mg hydrocodone/
200 mg ibuprofen (Reprexain). Cost: Generic—
7.5 mg/200 mg $48.40/100.
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