Naloxone Hydrochloride

Pronunciation

Class: Opiate Antagonists
VA Class: CN102
CAS Number: 357-08-4
Brands: Evzio, Suboxone

Warning(s)

REMS:

FDA approved a REMS for naloxone to ensure that the benefits outweigh the risks. The REMS may apply to one or more preparations of naloxone and consists of the following: medication guide, elements to assure safe use, and implementation system. See the FDA REMS page () or the ASHP REMS Resource Center ().

Introduction

Essentially a pure opiate antagonist.113 119

Uses for Naloxone Hydrochloride

Opiate-induced Depression and Acute Opiate Overdosage

Treatment of opiate-induced depression, including respiratory depression, caused by natural and synthetic opiates such as anileridine, codeine, diphenoxylate, fentanyl, heroin, hydromorphone, levorphanol, meperidine, methadone, morphine, oxymorphone, concentrated opium alkaloids hydrochlorides, and propoxyphene.113 116 119

Useful for the treatment of opiate-induced depression, including respiratory depression, caused by certain opiate partial agonists including butorphanol, nalbuphine, pentazocine, and cyclazocine.113 119 However, reversal of respiratory depression resulting from overdosage of opiate partial agonists may be incomplete or require higher naloxone dosages.119

May be used in community (nonmedical) settings for emergency treatment of known or suspected opiate overdosage, as manifested by respiratory and/or CNS depression.119 123 124 125 126 Availability as auto-injector facilitates administration by family members or other caregivers; such treatment is not a substitute for emergency medical care.119 123

Slideshow: Prescription Drug Addiction - Top 18 Facts for You and Your Family

Useful for the treatment of mild or moderate as well as severe opiate-induced respiratory depression.b

Administration should be accompanied by other resuscitative measures such as administration of oxygen, mechanical ventilation, or artificial respiration.116 119

Duration of respiratory depression following opiate agonist overdosage may be longer than the duration of naloxone action and other more immediate supportive and symptomatic treatment also should be initiated.d

Use in patients physically dependent on opiate agonists may precipitate an acute withdrawal syndrome that cannot be readily suppressed while the action of the antagonist (naloxone) persists.d

If opiate abstinence syndrome is precipitated by naloxone, symptoms will be apparent within a few minutes and maximal within 30 minutes after administration; effects usually will be more severe than those following withdrawal of the opiate agonist.d

Some value in the management of buprenorphine overdosage but should not be relied on for treatment of respiratory depression.c Reversal of agonist effects develops slowly.113

Not effective in the management of acute toxicity caused by levopropoxyphene.b

Diagnosis of Opiate Overdosage

Aid in the diagnosis of suspected acute opiate overdosage (e.g., in the absence of confirmatory history and/or definitive diagnostic clinical findings).113 e

Diagnosis of Chronic Opiate Abuse (Naloxone Challenge Test)

Has been used as an aid in the diagnosis of chronic opiate abuse, but preferable to use chemical methods to detect the presence of opiates in urine, since naloxone may precipitate severe withdrawal symptoms in patients physically dependent on opiates.b

Screening test (the naloxone challenge test) prior to induction of naltrexone therapy for opiate cessation in patients formerly dependent on opiates who have completed detoxification.b Such screening can avoid precipitating opiate withdrawal following administration of naltrexone.d

Alcohol- or Clonidine-induced Coma

Has been used in intoxicated patients to reverse alcohol-induced coma and to reverse clonidine-induced coma and respiratory depression.b

Detoxification and Maintenance Treatment of Opiate Dependence

A combination of methadone hydrochloride and naloxone hydrochloride in a ratio of 20:1 has been administered orally in the detoxification or maintenance treatment of opiate dependence in conjunction with appropriate social and medical services.b

May prevent opiate euphoria and thus decrease the desire for opiates.b

Has been used for rapid or ultrarapid detoxification in the management of opiate withdrawal in opiate-dependent individuals, both in inpatient and outpatient settings.112

Rapid opiate detoxification involves the administration of opiate antagonists such as naloxone and/or naltrexone to shorten the time period of detoxification.112

Ultrarapid detoxification is similar, but involves the administration of opiate antagonists (i.e., naloxone, naltrexone) while the patient is sedated or under general anesthesia.112

Risk of adverse respiratory and cardiovascular effects associated with this procedure must be considered as well as the costs of general anesthesia and hospitalization.112

Minimization of Pentazocine or Buprenorphine Abuse Potential

Used orally in fixed combination with pentazocine hydrochloride or sublingually in fixed combination with buprenorphine hydrochloride to minimize abuse potential of pentazocine or buprenorphine; antagonistic effect of naloxone will predominate if the combinations are administered parenterally and/or if usual oral doses are exceeded.114 115

Naloxone Hydrochloride Dosage and Administration

Administration

Administer by IV, sub-Q, or IM injection, or by IV infusion;113 116 119 IV use recommended for emergency situations.113 116 120

Because absorption may be erratic or delayed, AAP does not endorse sub-Q or IM injection for emergency medical management of opiate intoxication in children or neonates.110 113

When IV access cannot be established in emergency situations, consider intraosseous injection in pediatric patients116 or administration via an endotracheal tube in adults and pediatric patients.100 101 102 104 105 106 107 108 109 110 111 116

IV Infusion

For drug compatibility information, see Compatibility under Stability.

Continuous IV infusions may be most appropriate in patients who require higher doses, continue to experience recurrent respiratory or CNS depression after effective therapy with repeated doses, and/or in whom the effects of long-acting opiates are being antagonized.b

Dilution

Continuous IV infusion: Dilute 2 mg of naloxone hydrochloride in 500 mL of 0.9% sodium chloride or 5% dextrose injection to produce a solution containing 0.004 mg/mL (4 mcg/mL).120

Rate of Administration

Titrate in accordance with patient’s response.120

IM or Sub-Q Injection Using Auto-injector (Evzio)

May be administered by family members or other caregivers prior to emergency medical response to individuals with known or suspected opiate overdosage.119 Caregivers should seek emergency medical care immediately after administering the initial dose.119

Each carton contains 2 auto-injectors and 1 training device.119

Depending on thickness of adipose tissue at injection site, injection via auto-injector may be either sub-Q or IM.119 123

Technique for Using Auto-injector

Remove an auto-injector from the outer case, then remove red safety guard and firmly press black base of auto-injector against anterolateral aspect of thigh for 5 seconds until dose is delivered.119 121 Administer through clothing if necessary.119 Do not remove red safety guard until ready to use.119

For pediatric patients <1 year of age, pinch thigh prior to administration to provide a thicker injection area (to minimize risk that the needle might strike bone and break); following administration, observe injection site for residual needle fragments and/or signs of infection.119 123

After use, needle will retract into case and auto-injector will indicate that dose was delivered; auto-injectors cannot be reused.119

If the electronic voice instruction system of the auto-injector malfunctions, the intended dose will be delivered when the device is activated according to the printed instructions.119

Dosage

Available as naloxone hydrochloride; dosage expressed in terms of the salt.113

Pediatric Patients

Postoperative Opiate Depression
IV

Initial dosage: Usually, 0.005–0.01 mg, given at 2- to 3-minute intervals until desired response (i.e., adequate ventilation and alertness without substantial pain or discomfort) is obtained.113

Additional doses may be necessary at 1- to 2-hour intervals depending on response and dosage and duration of action of the opiate administered.113 (See Excessive Dosage in Surgery under Cautions.)

Opiate Overdosage
Diagnosis
IV

Children: Initially, 0.01 mg/kg; if this dose does not produce the expected response, may give a subsequent 0.1-mg/kg dose.113

Treatment in Health Care Setting

Duration of opiate action often exceeds that of naloxone; opiate depressant effects may return as the effects of naloxone diminish, and additional naloxone doses (or a continuous IV infusion) may be required.113 116

Manufacturers recommend that pediatric patients be closely observed for a day or longer regardless of degree of apparent improvement.119 120

IV

Children: Initially, 0.01 mg/kg; if this dose does not produce the desired degree of response, may give a subsequent 0.1-mg/kg dose.113 f

Alternatively, children <5 years of age or weight ≤20 kg: 0.1 mg/kg; repeat as necessary.110 116 b

Alternatively, children ≥5 years of age or weight >20 kg: 2 mg; repeat as necessary.110 116 b

For reversal of respiratory depression associated with therapeutic opiate use, some experts recommend lower dosages (e.g., 0.001–0.015 mg/kg for reversal of peri-arrest respiratory depression, 0.001–0.005 mg/kg for respiratory depression during procedural sedation to maintain some opiate analgesia).116 117 118

Continuous IV infusion dosage regimens have not been well established; titrate rate of administration according to the patient’s response.b

Experience with continuous IV infusions in children is limited, but children may require higher infusion rates on a mg/kg basis than adults.b

Infusion rates in children usually have ranged from 0.024–0.16 mg/kg per hour; alternatively, a pediatric infusion rate of 0.4 mg/hour has been suggested.b

Intraosseous or Endotracheal

Children <5 years of age or weighing ≤20 kg: Some experts suggest dose of 0.1 mg/kg.116

Children ≥5 years of age or weighing >20 kg: Some experts suggest dose of 2 mg.116

Optimum dose for administration via an endotracheal tube not established.116

Community-based Treatment

Duration of opiate action often exceeds that of naloxone; opiate depressant effects may return as the effects of naloxone diminish, and additional naloxone doses may be required.119

Caregivers should seek emergency medical care immediately after administering the initial naloxone dose and closely monitor the patient until emergency care arrives.119

IM or Sub-Q

0.4 mg (contents of one Evzio auto-injector); repeat as necessary at 2- to 3-minute intervals until emergency care arrives.119

Adults

Postoperative Opiate Depression
IV

Initial dosage: Usually, 0.1–0.2 mg, given at 2- to 3-minute intervals until desired response (i.e., adequate ventilation and alertness without substantial pain or discomfort) is obtained; additional doses may be necessary at 1- to 2-hour intervals depending on response and dosage and duration of action of the opiate administered.113

Alternatively, 0.005 mg/kg, repeated after 15 minutes if necessary.b

Continuous IV infusion: 0.0037 mg/kg per hour.b

Opiate Overdosage
Diagnosis
IV

Initial dosage: Usually, 0.4–2 mg IV, administered at 2- to 3-minute intervals if necessary; if no response is observed after a total of 10 mg of the drug has been administered, the depressive condition may be caused by a drug or disease process not responsive to naloxone.113

Treatment in Health Care Setting

Duration of opiate action often exceeds that of naloxone; opiate depressant effects may return as the effects of naloxone diminish, and additional naloxone doses (or a continuous IV infusion) may be required.113 116

Carefully monitor patient for recurrence of opiate depressant effects.113 116 119

IV

Initial dosage: Usually, 0.4–2 mg IV, administered at 2- to 3-minute intervals if necessary; if no response is observed after a total of 10 mg of the drug has been administered, the depressive condition may be caused by a drug or disease process not responsive to naloxone.113

Higher doses may be required following massive opiate overdosage or overdosage of certain opiates (e.g., propoxyphene [no longer commercially available in US]).116

Opiate-dependent individuals: Use initial dose of 0.04–0.4 mg to minimize adverse cardiovascular effects and withdrawal symptoms; if initial response is inadequate, repeat dose or titrate up to 2 mg.116

Continuous IV infusion dosage regimens of naloxone have not been well established; titrate rate of administration according to the patient’s response.b

IV infusion: IV loading dose of 0.4 mg, followed by a continuous IV infusion at an initial rate of 0.4 mg/hour; alternatively, other clinicians have recommended an IV loading dose of 0.005 mg/kg, followed by continuous infusion of 0.0025 mg/kg per hour.b

IV infusion: Alternatively, IV loading dose of 0.005 mg/kg, followed by continuous IV infusion of 0.0025 mg/kg per hour.b

Endotracheal

Higher dose (as compared with other routes) may be required;116 however, optimum dose not established.116

Community-based Treatment

Duration of opiate action often exceeds that of naloxone; opiate depressant effects may return as the effects of naloxone diminish, and additional naloxone doses may be required.119

Caregivers should seek emergency medical care immediately after administering the initial naloxone dose and closely monitor the patient until emergency care arrives.119

IM or Sub-Q

0.4 mg (contents of one Evzio auto-injector); repeat as necessary at 2- to 3-minute intervals until emergency care arrives.119

Diagnosis of Chronic Opiate Abuse (Naloxone Challenge Test)

Performed prior to induction of naltrexone therapy in patients formerly physically dependent on opiates who have completed detoxification and in those suspected of having been dependent on opiates.

Do not perform the naloxone challenge test in patients who are exhibiting manifestations of opiate withdrawal, those whose urine shows evidence of opiates, or those in whom there is a high degree of suspicion that opiates are still being used, since naloxone may precipitate potentially severe opiate withdrawal.

If manifestations of opiate withdrawal are evident following naloxone challenge test, naltrexone therapy should not be attempted.

During the appropriate period in the naloxone challenge test, the patient should be closely monitored for the appearance of manifestations of opiate withdrawal and vital signs should be monitored.

If manifestations of opiate withdrawal are evident following the naloxone challenge test, do not initiate naltrexone therapy due to potential risk of precipitating more severe and prolonged withdrawal with naltrexone; naloxone challenge test may be repeated in 24 hours in these patients.

If evidence of withdrawal is absent, naltrexone therapy may be initiated.

Some clinicians caution that even minor and/or transient GI symptoms following naloxone challenge be considered evidence of withdrawal since patients with such symptoms will often develop severe and disturbing GI symptoms if naltrexone therapy is then initiated.

IV

Use a sterile syringe containing 0.8 mg of naloxone hydrochloride.

Initially, a 0.2-mg IV dose and, while the needle remains in the vein, observe the patient for 30 seconds for evidence of opiate withdrawal.

Alternatively, an initial 0.2-mg IV dose, then observe patient for 15 minutes for evidence of withdrawal.

Manifestations of withdrawal include, but are not limited to, nasal stuffiness, rhinorrhea, lacrimation, yawning, sweating, tremor, abdominal cramps, vomiting, piloerection, myalgia, and skin crawling.

If no evidence of withdrawal, inject the remaining 0.6-mg IV dose and observe the patient for an additional 20 minutes for evidence of withdrawal.

Some clinicians recommend that a total IV dose of 2 mg be used in the test since withdrawal has been precipitated by the first oral dose of naltrexone despite a negative naloxone challenge test using lower doses and a false-negative test rarely occurs with the 2-mg naloxone hydrochloride dose.

Sub-Q

Inject the entire 0.8-mg dose and observe the patient for 20 minutes for evidence of opiate withdrawal.

If evidence of opiate withdrawal is present, naltrexone therapy should be delayed and the naloxone challenge test repeated in 24 hours with the 0.8-mg dose and every 24 hours until results are negative.

If it is uncertain whether the patient is opiate free or is undergoing opiate withdrawal following an initial test, the naloxone challenge test should be repeated at that time with a 1.6-mg dose.

To repeat the naloxone challenge test in these patients, a 1.6-mg dose of naloxone hydrochloride should be injected IV and the patient observed for evidence of opiate withdrawal; if evidence of opiate withdrawal is absent, naltrexone therapy may be initiated.

Diagnosis of Opiate Dependence
IM, then IV

Initial single dose of 0.16 mg IM; if no withdrawal manifestations are evident after 20–30 minutes, a second dose of 0.24 mg is given IV.b

Negative test results assumed if no withdrawal manifestations are apparent within 30 minutes after the second dose.b

Withdrawal manifestations induced by naloxone begin to diminish 20–40 minutes after injection and are essentially gone within 1.5 hours.b

Prescribing Limits

Adults

Known or Suspected Opiate Overdosage
IV, IM or Sub-Q

If no response is observed after a total of 10 mg is been administered, the depressive condition may be caused by a drug or disease process not responsive to naloxone.113

Special Populations

Hepatic Impairment

No specific dosage recommendations.b

Renal Impairment

No specific dosage recommendations.b

Geriatric Patients

No specific dosage recommendations; in general, dose selection should be cautious, usually initiating at the lower end or the normal range.113

Cautions for Naloxone Hydrochloride

Contraindications

  • Known hypersensitivity to naloxone or any ingredient in the formulation.113 119

Warnings/Precautions

Warnings

Additional Resuscitative Measures

When used in the management of acute opiate overdosage, other resuscitative measures (e.g., maintenance of an adequate airway, artificial respiration, cardiac massage, vasopressor agents) should be readily available and used when necessary.113

Excessive Dosage in Surgery

Avoid excessive dosage following the use of opiates during surgery because naloxone may result in excitement, agitation, an increase in BP, and clinically important reversal of analgesia; a reversal of opiate effects achieved too rapidly may induce nausea, vomiting, sweating, tremor, tachycardia, hypotension, hypertension, seizures, ventricular tachycardia and fibrillation, pulmonary edema, and cardiac arrest, which may result in death.113 119

Physical Opiate Dependence

Caution in patients known or suspected to be physically dependent on opiates (including neonates born to women who are opiate dependent) because severe withdrawal manifestations may be precipitated.113 116 119

General Precautions

Cardiovascular Disease

Caution and monitoring for adverse cardiopulmonary effects advised in patients with preexisting cardiovascular disease and in those receiving potentially cardiotoxic drugs; serious adverse cardiopulmonary effects (e.g., ventricular tachycardia and fibrillation, pulmonary edema, cardiac arrest) resulting in death, coma, and encephalopathy have occurred in postoperative patients following administration of naloxone.113 119 (See Common Adverse Effects under Cautions.)

Repeat Administration

Carefully monitor patients who have responded to naloxone since the duration of action of some opiates may exceed that of naloxone.113 116 119 Give repeated doses of naloxone to these patients when necessary.113 116 119

Some experts state that while a brief observation period may be adequate following overdosage of certain opiates with a shorter duration of action (morphine, heroin), patients with life-threatening overdosage of a long-acting or extended-release opiate may require longer periods of observation.116 The manufacturers recommend that pediatric patients be carefully monitored for ≥24 hours.119 120

Use of Fixed Combination

When used in fixed combination with other agents, consider the cautions, precautions, and contraindications associated with the concomitant agents.

Specific Populations

Pregnancy

Naloxone hydrochloride injection: Category C.113 120

Evzio auto-injector: Category B.119

Risk of opiate withdrawal in both mother and fetus when naloxone is administered to an opiate-dependent pregnant woman; monitor for fetal distress.119

Lactation

Not known whether naloxone is distributed into milk.113 119 g Caution advised if used in nursing women.113 119

Pediatric Use

Safety and efficacy in management of hypotension associated with septic shock not established in pediatric patients.113 In a study of 2 neonates with septic shock, treatment with naloxone produced positive pressor response; however, one patient subsequently died after intractable seizures.113

Naloxone may be used to reverse effects of opiates in infants and children.120 Safety and efficacy of naloxone administered via auto-injector (Evzio) established in pediatric patients with known or suspected opiate overdosage manifested by respiratory and/or CNS depression.119 Use of naloxone for reversal of opiate effects in pediatric patients is supported by well-controlled studies in adults, additional data from controlled and uncontrolled studies in which neonates and children received parenteral naloxone hydrochloride (0.005–0.01 mg/kg), other published data, and postmarketing experience with the drug.119

May precipitate opiate withdrawal in patients who are physically dependent on opiates.119 Opiate withdrawal in neonates may be life-threatening; treat according to protocols developed by neonatology experts.119

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.113 119 Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.113 119

Hepatic Impairment

Safety and efficacy not established; use with caution.113

Renal Impairment

Safety and efficacy not established; use with caution.113

Common Adverse Effects

Nausea and vomiting rarely postoperatively with parenteral dose exceeding that usually recommended; a causal relationship has not been established.b

Analgesia reversal, excitement, agitation, and increased BP may occur with excessive postoperative doses.113

Postoperative use: Hypotension, hypertension, ventricular tachycardia and fibrillation, dyspnea, pulmonary edema, and cardiac arrest; sequelae include death, coma, and encephalopathy.113

Opiate overdosage: Tremor and hyperventilation associated with an abrupt return to consciousness.b

Opiate dependence: Abrupt dependence reversal may precipitate acute withdrawal.113

Adverse cardiovascular effects have occurred most frequently in postoperative patients with preexisting cardiovascular disease or in those receiving other drugs that produce similar adverse cardiovascular effects. (See Cardiovascular Disease under Cautions.)

Interactions for Naloxone Hydrochloride

Specific Drugs

Drug

Interaction

Comments

Cardiotoxic drugs

Serious adverse cardiovascular effects (e.g., ventricular tachycardia and fibrillation, pulmonary edema, cardiac arrest) resulting in death, coma, and encephalopathy reported in postoperative patients113

Use concomitantly with caution113

Methohexital

Methohexital appears to block the acute onset of withdrawal symptoms induced by naloxone in opiate addicts113

Naloxone Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Rapidly inactivated following oral administration.b

Although effective orally, doses much larger than those required for parenteral administration are required for complete antagonism.b

Evzio auto-injector: Bioequivalent to naloxone hydrochloride administered by sub-Q or IM injection using a standard syringe.119 123

Onset

IV: Within 1–2 minutes.b

Sub-Q or IM: Within 2–5 minutes.b

Duration

Depends on the dose and route of administration and is more prolonged following IM than IV administration.113 119

Distribution

Extent

Parenteral: Rapidly distributed into body tissues and fluids.113 119 123

Readily (within 2 minutes) crosses the placenta.113 119 g

Unknown whether distributed into milk.113 119 g

Plasma Protein Binding

Weakly bound to plasma proteins (mainly albumin).113 119

Elimination

Metabolism

Rapidly metabolized in the liver, principally by conjugation with glucuronic acid.113 119

Major metabolite is naloxone-3-glucuronide.113 119

Also undergoes N-dealkylation and reduction of the 6-keto group followed by conjugation.b

Elimination Route

Oral or IV dose: 25–40% excreted as metabolites in urine in 6 hours, about 50% in 24 hours, and 60–70% in 72 hours.113 119

Half-life

Adults: 30–81 minutes.113

Neonates: About 3 hours.113

Evzio auto-injector: 1.28 hours.119

Stability

Storage

Parenteral

Injection

Vials and ampuls: 20–25°C; protect from light.120

Auto-injector (Evzio): Store in outer case at 15–25°C (may be exposed to 4–40°C).119

Stable at pH 2.5–5.b

Use diluted solutions (e.g., 4 mcg/mL in 5% dextrose or 0.9% sodium chloride injection) within 24 hours; discard unused portions after 24 hours.120

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Do not mix with preparations containing bisulfite, metabisulfite, long-chain or high molecular weight anions, or any solution having an alkaline pH.120

Drug Compatibility
Admixture CompatibilityHID

Compatible

Verapamil HCl

Y-Site CompatibilityHID

Compatible

Fenoldopam mesylate

Linezolid

Propofol

Incompatible

Amphotericin B cholesteryl sulfate complex

Actions

  • Essentially a pure opiate antagonist.113 119

  • In usual doses in patients who have not recently received opiates, naloxone exerts little or no pharmacologic effect.113

  • In patients who have received large doses of morphine or other analgesic drugs with morphine-like effects, naloxone antagonizes most of the effects of the opiate.113

  • Increase in respiratory rate and minute volume, decrease toward normal in arterial PCO2, and return to normal in blood pressure if depressed.b

  • Because the duration of action of naloxone is generally shorter than that of the opiate, the effects of the opiate may return as the effects of naloxone dissipate.113 119

  • Antagonizes opiate-induced sedation or sleep.b

  • Does not produce tolerance or physical or psychological dependence.113

  • It is thought to act as a competitive antagonist at mc, κ, and σ opiate receptors in the CNS; it is thought that the drug has the highest affinity for the μ receptor.113

Advice to Patients

  • Instruct patients receiving naloxone auto-injector (Evizo) and their family members or caregivers about clinical manifestations requiring naloxone administration and proper administration techniques; encourage familiarity with the training device provided in each carton.119

  • Seek immediate medical attention after injecting naloxone in an out-of-hospital setting.119 Monitor patient closely until emergency care arrives.119

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Naloxone Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection

0.4 mg/mL*

Naloxone Hydrochloride Injection

1 mg/mL*

Evzio (available as kit with 2 prefilled, single-use 0.4-mL auto-injectors and 1 drug-free, needleless, reusable training device)

Kaleo

Naloxone Hydrochloride Injection

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Pentazocine and Naloxone Hydrochlorides

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

Pentazocine Hydrochloride 50 mg (of pentazocine) and Naloxone Hydrochloride 0.5 mg (of naloxone)*

Pentazocine and Naloxone Hydrochlorides Tablets (C-IV)

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Naloxone Hydrochloride Dihydrate Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Sublingual

Strips, sublingually dissolving

0.5 mg (of naloxone) with Buprenorphine Hydrochloride 2 mg (of buprenorphine)

Suboxone (C-III)

Reckitt Benckiser

1 mg (of naloxone) with Buprenorphine Hydrochloride 4 mg (of buprenorphine)

Suboxone (C-III)

Reckitt Benckiser

2 mg (of naloxone) with Buprenorphine Hydrochloride 8 mg (of buprenorphine)

Suboxone (C-III)

Reckitt Benckiser

3 mg (of naloxone) with Buprenorphine Hydrochloride 12 mg (of buprenorphine)

Suboxone (C-III)

Reckitt Benckiser

Tablets

0.5 mg (of naloxone) with Buprenorphine Hydrochloride 2 mg (of buprenorphine)*

Buprenorphine Hydrochloride and Naloxone Hydrochloride Sublingual Tablets (C-III)

2 mg (of naloxone) with Buprenorphine Hydrochloride 8 mg (of buprenorphine)*

Buprenorphine Hydrochloride and Naloxone Hydrochloride Sublingual Tablets (C-III)

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 01/2015. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Pentazocine-Naloxone HCl 50-0.5MG Tablets (WATSON LABS): 30/$42.99 or 90/$112.97

AHFS DI Essentials. © Copyright, 2004-2015, Selected Revisions December 11, 2014. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

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101. Ward JT Jr. Endotracheal drug therapy. Am J Emerg Med. 1983; 1:71-2. [PubMed 6393996]

102. Tandberg D. Endotracheal naloxone. Am J Emerg Med. 1983; 1:366-7. [PubMed 6680644]

103. Tandberg D, Abercrombie D. Treatment of heroin overdose with endotracheal naloxone. Ann Emerg Med. 1982; 11:443-5. [PubMed 7103164]

104. Greenberg MI. The use of endotracheal medication in cardiac emergencies. Resuscitation. 1984; 12:155-65. [PubMed 6096940]

105. Hahnel J, Lindner KH, Ahnefeld FW. Endobroncial administration of emergency drugs. Resuscitation. 1989; 17:261-72. [PubMed 2548271]

106. Greenberg MI, Roberts JR, Baskin SI. Endotracheal naloxone reversal of morphine-induced respiratory depression in rabbits. Ann Emerg Med. 1980; 9:289-92. [PubMed 7386953]

107. Raehl CL. Endotracheal drug therapy in cardiopulmonary resuscitation. Clin Pharm. 1986; 5:572-9. [IDIS 217499] [PubMed 3527527]

108. American Academy of Pediatrics Committee on Drugs. Emergency drug doses for infants and children. Pediatrics. 1988; 81:462-5. [PubMed 3422026]

109. American Academy of Pediatrics Committee on Drugs. Emergency drug doses for infants and children and naloxone use in newborns: clarification. Pediatrics. 1989; 83:803. [IDIS 254337] [PubMed 2717301]

110. American Academy of Pediatrics Committee on Drugs. Naloxone dosage and route of administration for infants and children: addendum to emergency drug doses for infants and children. Pediatrics. 1990; 86:484-5. [IDIS 273346] [PubMed 2388800]

111. Emergency Cardiac Care Committee and Subcommittees, American Heart Association. Guidelines for cardiopulmonary resuscitation and emergency cardiac care. JAMA. 1992; 268:2171-302. [PubMed 1404767]

112. O’Connor PG, Kosten TR. Rapid and ultrarapid opioid detoxification techniques. JAMA. 1998; 279:229-34.

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