methadone hydrochloride

(meth' a done)
Dolophine, Methadone HCl Diskets, Methadone HCl Intensol, Methadose

Pregnancy Category C
Controlled Substance C-II

Drug class
Opioid agonist analgesic

Therapeutic actions
Acts as agonist at specific opioid receptors in the CNS to produce analgesia, euphoria,
sedation; the receptors mediating these effects are thought to be the same as those
mediating the effects of endogenous opioids (enkephalins, endorphins); when used in
approved methadone maintenance programs, can substitute for heroin, other illicit opioids
in patients who want to terminate a drug use.

Indications
• Relief of severe pain
• Detoxification and temporary maintenance treatment of opioid addiction
(ineffective for relief of general anxiety)

Contraindications and cautions

• Contraindicated with hypersensitivity to opioids, diarrhea caused by poisoning
(before toxins are eliminated), bronchial asthma, COPD, cor pulmonale,
respiratory depression, anoxia, kyphoscoliosis, acute alcoholism, increased
intracranial pressure.
• Use cautiously with acute abdominal conditions, CV disease, supraventricular
tachycardias, myxedema, seizure disorders, delirium tremens, cerebral
arteriosclerosis, ulcerative colitis, fever, Addison's disease, prostatic hypertrophy,
urethral stricture, recent GI or GU surgery, toxic psychosis, pregnancy prior to
labor (crosses placenta; neonatal withdrawal observed in infants born to drug-
using mothers; safety for use in pregnancy before labor not established), labor or
delivery (administration of opioids to mother can cause respiratory depression of
neonate—risk greatest for prematures), renal or hepatic dysfunction, lactation.

Available forms
Tablets—5, 10 mg; oral solution—5 mg/5 mL, 10 mg/5 mL; oral concentrate—
10 mg/mL; injection—10 mg/mL; dispersible tablets—40 mg

Dosages
Oral methadone is approximately one-half as potent as parenteral methadone.
ADULTS
• Relief of pain: 2.5–10 mg IM, SC, or PO q 3–4 hr as necessary. IM route is
preferred to SC for repeated doses (SC may cause local irritation). Individualize
 dosage; patients with excessively severe pain and those who have become tolerant
to the analgesic effect of opioids may need higher dosage.
• Detoxification: Initially, 15–20 mg PO or parenteral; PO preferred. Increase dose
to suppress withdrawal signs. 40 mg/day in single or divided doses is usually an
adequate stabilizing dose for those physically dependent on high doses. Continue
stabilizing doses for 2–3 days, then gradually decrease dosage every day or every
2 days. A daily reduction of 20% of the total dose may be tolerated. Provide
sufficient dosage to keep withdrawal symptoms at tolerable level. Treatment
should not exceed 21 days and may not be repeated earlier than 4 wk after
completion of previous course. Detoxification treatment continued longer than 21
days becomes maintenance treatment, which may be undertaken only by approved
programs (addicts hospitalized for other medical conditions may receive
methadone maintenance treatment).
• Maintenance treatment: For patients who are heavy heroin users up until hospital
admission, initial dose of 20 mg 4–8 hr after heroin is stopped or 40 mg in a
single dose PO. For patients with little or no opioid tolerance, half this dose may
suffice. Dosage should suppress withdrawal symptoms but not produce acute
narcotic effects of sedation, respiratory depression. Give additional 10 mg doses if
needed to suppress withdrawal syndrome. Adjust dosage, up to 120 mg/day.
PEDIATRIC PATIENTS
Not recommended for relief of pain in children due to insufficient documentation.
GERIATRIC PATIENTS OR IMPAIRED ADULTS
Use caution. Respiratory depression may occur in the elderly, the very ill, those with
respiratory problems. Reduced dosage may be necessary.

Pharmacokinetics
Route Onset Peak Duration
PO 30–60 min 1.5–2 hr 4–12 hr
IM 10–20 min 1–2 hr 4–6 hr
SC 10–20 min 1–2 hr 4–6 hr

Metabolism: Liver; T1/2: 25 hr

Distribution: Crosses placenta and enters breast milk
Excretion: Bile and feces

Adverse effects
• CNS: Light-headedness, dizziness, sedation, euphoria, dysphoria, delirium,
insomnia, agitation, anxiety, fear, hallucinations, disorientation, drowsiness,
lethargy, impaired mental and physical performance, coma, mood changes,
weakness, headache, tremor, seizures, miosis, visual disturbances, suppression of
cough reflex
• CV: Facial flushing, peripheral circulatory collapse, arrhythmia, palpitations,
chest wall rigidity, hypertension, hypotension, orthostatic hypotension, syncope
• Dermatologic: Pruritus, urticaria, laryngospasm, bronchospasm, edema,
hemorrhagic urticaria (rare)
• GI: Nausea, vomiting, dry mouth, anorexia, constipation, biliary tract spasm;
increased colonic motility in patients with chronic ulcerative colitis
 • GU: Ureteral spasm, spasm of vesical sphincters, urinary retention or hesitancy,
oliguria, antidiuretic effect, reduced libido or potency
• Local: Tissue irritation and induration (SC injection)
• Major hazards: Respiratory depression, apnea, circulatory depression,
respiratory arrest, shock, cardiac arrest
• Other: Sweating (more common in ambulatory patients and those without severe
pain), physical tolerance and dependence, psychological dependence

Interactions
Drug-drug
• Potentiation of effects of methadone with barbiturate anesthetics—decrease dose
of meperidine when coadministering
• Decreased effectiveness of methadone with hydantoins, rifampin, urinary
acidifiers (ammonium chloride, potassium acid phosphate, sodium acid
phosphate)
• Increased effects and toxicity of methadone with cimetidine, ranitidine
Drug-lab test
• Elevated biliary tract pressure (opioid effect) may cause increases in plasma
amylase, lipase; determinations of these levels may be unreliable for 24 hr after
administration of opioids

Nursing considerations
Assessment
• History: Hypersensitivity to opioids, diarrhea caused by poisoning, bronchial
asthma, COPD, cor pulmonale, respiratory depression, kyphoscoliosis, acute
alcoholism, increased intracranial pressure; acute abdominal conditions, CV
disease, supraventricular tachycardias, myxedema, seizure disorders, delirium
tremens, cerebral arteriosclerosis, ulcerative colitis, fever, Addison's disease,
prostatic hypertrophy, urethral stricture, recent GI or GU surgery, toxic psychosis;
pregnancy; labor; lactation
• Physical: T; skin color, texture, lesions; orientation, reflexes, bilateral grip
strength, affect, pupil size; pulse, auscultation, BP, orthostatic BP, perfusion; R,
adventitious sounds; bowel sounds, normal output; frequency and pattern of
voiding, normal output; ECG; EEG; thyroid, liver, kidney function tests

Interventions
• Give to lactating women 4–6 hr before the next feeding to minimize the amount in
milk.
• Keep opioid antagonist and equipment for assisted or controlled respiration
readily available during parenteral administration.
• Use caution when injecting SC into chilled areas of the body or in patients with
hypotension or in shock—impaired perfusion may delay absorption; with repeated
doses, an excessive amount may be absorbed when circulation is restored.

Teaching points
 • Take drug exactly as prescribed.
• Avoid alcohol—serious adverse effects may occur.
• Do not take leftover medication for other disorders; do not let anyone else take the
prescription.
• Avoid pregnancy while taking this drug; using barrier contraceptives is advised.
• These side effects may occur: Nausea, loss of appetite (take with food, lie quietly,
eat frequent small meals); constipation (laxative may help); dizziness, sedation,
drowsiness, impaired visual acuity (avoid driving, performing other tasks that
require alertness, visual acuity).
• Report severe nausea, vomiting, constipation, shortness of breath, or difficulty
breathing.

Adverse effects in Italic are most common; those in Bold are life-threatening.