Naloxone: Difference between revisions

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{{Drugbox|
{{DrugProjectFormSinglePage
|IUPAC_name = ''17-allyl-4,5α-epoxy-<br>3,14-dihydroxymorphinan-6-one''
|authorTag=
| image=Naloxone.png
 
| image2=Naloxone-3D-balls.png
{{VP}}
| CAS_number=465-65-6
 
| ATC_prefix=V03
<!--Overview-->
| ATC_suffix=AB15
 
| PubChem=4425
|genericName=
| DrugBank=APRD00025
 
| C=19 | H=21 | N=1 | O=4
 
| molecular_weight = 327.27
 
| bioavailability= 2% (90% absorption but high first-pass metabolism)
|aOrAn=
| metabolism = [[Liver]]
 
| elimination_half-life=1-1.5 hours
an
| excretion = Urine, Biliary
 
| pregnancy_category = B ([[United States|USA]]) <br /> B1 ([[Australia|Aus]])
|drugClass=
| legal_CA = Schedule I
 
| legal_AU = S4
[[opioid]] antagonist
| routes_of_administration= [[Intravenous therapy|IV]], [[Intramuscular|IM]]
 
}}
|indication=
 
known or suspected [[opioid overdose]], as manifested by [[respiratory]] and/or [[central nervous system]] depression
 
|hasBlackBoxWarning=
 
|adverseReactions=
 
[[hypotension]], [[hypertension]], [[ventricular tachycardia]], [[ventricular fibrillation]], [[dyspnea]], [[pulmonary edema]], [[cardiac arrest]], death, [[coma]], and [[encephalopathy]]
 
<!--Black Box Warning-->
 
|blackBoxWarningTitle=
Title
 
|blackBoxWarningBody=
<i><span style="color:#FF0000;">ConditionName: </span></i>
 
* Content
 
<!--Adult Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Adult)-->
 
|fdaLIADAdult=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
* Dosing Information
 
:* Dosage
 
=====Condition3=====
 
* Dosing Information
 
:* Dosage
 
=====Condition4=====
 
* Dosing Information
 
:* Dosage
 
<!--Off-Label Use and Dosage (Adult)-->
 
<!--Guideline-Supported Use (Adult)-->
 
|offLabelAdultGuideSupport=
 
=====Condition1=====
 
* Developed by:
 
* Class of Recommendation:
 
* Strength of Evidence:
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
 
<!--Non–Guideline-Supported Use (Adult)-->
 
|offLabelAdultNoGuideSupport=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
 
<!--Pediatric Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Pediatric)-->
 
|fdaLIADPed=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Off-Label Use and Dosage (Pediatric)-->
 
<!--Guideline-Supported Use (Pediatric)-->
 
|offLabelPedGuideSupport=
 
=====Condition1=====
 
* Developed by:
 
* Class of Recommendation:
 
* Strength of Evidence:
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Non–Guideline-Supported Use (Pediatric)-->
 
|offLabelPedNoGuideSupport=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Contraindications-->
 
|contraindications=
 
*EVZIO is contraindicated in patients known to be [[hypersensitive]] to naloxone hydrochloride or to any of the other ingredients.
 
<!--Warnings-->
 
|warnings=
 
====Precautions====
 
* Duration of Effect
:*The duration of action of most opioids is likely to exceed that of EVZIO resulting in a return of respiratory and/or central nervous system depression after an initial improvement in symptoms. Therefore, it is necessary to seek immediate emergency medical assistance after delivering the first dose of EVZIO, keep the patient under continued surveillance, and repeat doses of EVZIO as necessary. Additional supportive and/or resuscitative measures may be helpful while awaiting emergency medical assistance.
 
*Limited Efficacy with Partial Agonists or Mixed Agonist/Antagonists
:*Reversal of respiratory depression by partial agonists or mixed agonist/antagonists such as buprenorphine and pentazocine, may be incomplete. Large doses of naloxone hydrochloride are required to antagonize buprenorphine because the latter has a long duration of action due to its slow rate of binding and subsequent slow dissociation from the opioid receptor. Buprenorphine antagonism is characterized by a gradual onset of the reversal effects and a decreased duration of action of the normally prolonged respiratory depression.
 
*Precipitation of Severe Opioid Withdrawal
:*The use of EVZIO in patients who are opioid dependent may precipitate an acute abstinence syndrome characterized by the following signs and symptoms: body aches, diarrhea, tachycardia, fever, runny nose, sneezing, piloerection, sweating, yawning, nausea or vomiting, nervousness, restlessness or irritability, shivering or trembling, abdominal cramps, weakness, and increased blood pressure. In neonates, opioid withdrawal may be life-threatening if not recognized and properly treated and may include the following signs and symptoms: convulsions, excessive crying, and hyperactive reflexes.
:*Abrupt postoperative reversal of opioid depression after using naloxone hydrochloride may result in nausea, vomiting, sweating, tremulousness, tachycardia, hypotension, hypertension, seizures, ventricular tachycardia and fibrillation, pulmonary edema, and cardiac arrest. Death, coma, and encephalopathy have been reported as sequelae of these events. These events have occurred in patients most of whom had pre-existing cardiovascular disorders or received other drugs which may have similar adverse cardiovascular effects. Although a direct cause and effect relationship has not been established, after use of naloxone hydrochloride, patients with pre-existing cardiac disease or patients who have received medications with potential adverse cardiovascular effects should be monitored for hypotension, ventricular tachycardia or fibrillation, and pulmonary edema in an appropriate healthcare setting. It has been suggested that the pathogenesis of pulmonary edema associated with the use of naloxone hydrochloride is similar to neurogenic pulmonary edema, i.e., a centrally mediated massive catecholamine response leading to a dramatic shift of blood volume into the pulmonary vascular bed resulting in increased hydrostatic pressures.
 
<!--Adverse Reactions-->
 
<!--Clinical Trials Experience-->
 
|clinicalTrials=
 
*The following adverse reactions have been identified during post-approval use of naloxone hydrochloride in the post-operative setting. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure: Hypotension, hypertension, ventricular tachycardia and fibrillation, dyspnea, pulmonary edema, and cardiac arrest. Death, coma, and encephalopathy have been reported as sequelae of these events. Excessive doses of naloxone hydrochloride in post-operative patients have resulted in significant reversal of analgesia and have caused agitation [see Warnings and Precautions (5.3)].
 
*Abrupt reversal of opioid effects in persons who were physically dependent on opioids has precipitated an acute withdrawal syndrome. Signs and symptoms have included: body aches, fever, sweating, runny nose, sneezing, piloerection, yawning, weakness, shivering or trembling, nervousness, restlessness or irritability, diarrhea, nausea or vomiting, abdominal cramps, increased blood pressure, tachycardia. In the neonate, opioid withdrawal signs and symptoms also included: convulsions, excessive crying, hyperactive reflexes [see Warnings and Precautions (5.3)].
 
<!--Postmarketing Experience-->
 
|postmarketing=
 
There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
 
=====Body as a Whole=====
 
 
 
=====Cardiovascular=====
 
 
 
=====Digestive=====
 
 
 
=====Endocrine=====
 
 
 
=====Hematologic and Lymphatic=====
 
 
 
=====Metabolic and Nutritional=====
 
 
 
=====Musculoskeletal=====
 
 
 
=====Neurologic=====
 
 
 
=====Respiratory=====
 
 
 
=====Skin and Hypersensitivy Reactions=====
 
 
 
=====Special Senses=====
 
 
 
=====Urogenital=====
 
 
 
=====Miscellaneous=====
 
 
 
<!--Drug Interactions-->
 
|drugInteractions=
 
* Drug
:* Description
 
<!--Use in Specific Populations-->
 
|useInPregnancyFDA=
* '''Pregnancy Category'''
 
|useInPregnancyAUS=
* '''Australian Drug Evaluation Committee (ADEC) Pregnancy Category'''
 
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
 
|useInLaborDelivery=
There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
 
|useInNursing=
There is no FDA guidance on the use of {{PAGENAME}} with respect to nursing mothers.
 
|useInPed=
There is no FDA guidance on the use of {{PAGENAME}} with respect to pediatric patients.
 
|useInGeri=
There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
 
|useInGender=
There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
 
|useInRace=
There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
 
|useInRenalImpair=
There is no FDA guidance on the use of {{PAGENAME}} in patients with renal impairment.
 
|useInHepaticImpair=
There is no FDA guidance on the use of {{PAGENAME}} in patients with hepatic impairment.
 
|useInReproPotential=
There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
 
|useInImmunocomp=
There is no FDA guidance one the use of {{PAGENAME}} in patients who are immunocompromised.
 
<!--Administration and Monitoring-->
 
|administration=
 
* Oral
 
* Intravenous
 
|monitoring=
 
There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
 
* Description
 
<!--IV Compatibility-->
 
|IVCompat=
 
There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.
 
<!--Overdosage-->
 
|overdose=
 
===Acute Overdose===
 
====Signs and Symptoms====
 
* Description
 
====Management====
 
* Description
 
===Chronic Overdose===
 
There is limited information regarding <i>Chronic Overdose</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacology-->
 
<!--Drug box 2-->
 
|drugBox=
 
 
 
<!--Mechanism of Action-->
 
|mechAction=
 
*
 
<!--Structure-->
 
|structure=
 
*
 
: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
 
<!--Pharmacodynamics-->
 
|PD=
 
There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacokinetics-->
 
|PK=
 
There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.
 
<!--Nonclinical Toxicology-->
 
|nonClinToxic=
 
There is limited information regarding <i>Nonclinical Toxicology</i> of {{PAGENAME}} in the drug label.
 
<!--Clinical Studies-->


{{SI}}
|clinicalStudies=


There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.


<!--How Supplied-->


{{CMG}}
|howSupplied=


==Overview==
*
'''Naloxone''' is a [[medication|drug]] used to counter the effects of [[opioid]] [[Drug overdose|overdose]], for example [[heroin]] or [[morphine]] overdose. Naloxone is specifically used to counteract life-threatening depression of the central nervous system and respiratory system. It is marketed under various trademarks including '''Narcan''', '''Nalone''', and '''Narcanti''', and has sometimes been mistakenly called "naltrexate."  It is not to be confused with [[Naltrexone]], another [[opioid receptor]] [[receptor antagonist|antagonist]] with qualitatively different effects, used for dependence treatment rather than emergency overdose treatment.


== Pharmacodynamics ==
<!--Patient Counseling Information-->


Naloxone has an extremely high affinity for μ-[[opioid receptor]]s in the [[central nervous system]]. Naloxone is a μ-opioid receptor [[competitive antagonist]], and its rapid blockade of those receptors often produces rapid onset of [[withdrawal]] symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- and δ-opioid receptors.
|fdaPatientInfo=


== Chemistry ==
There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.


Naloxone  is [[chemical synthesis|synthesized]] from [[thebaine]]. The [[chemical structure]] of naloxone resembles that of [[oxymorphone]], the only difference being the substitution of the [[amine|''N'']]-[[methyl]] [[functional group|group]] with an [[allyl]] (prop-2-enyl) group. The name ''naloxone'' has been derived from '''''N''-al'''lyl and '''ox'''ymorph'''one'''.
<!--Precautions with Alcohol-->


==Administration==
|alcohol=
Naloxone is injected, usually initially [[intravenous]]ly for fastest action. The drug acts after about two minutes, and its effects may last about 45 minutes. Other routes, including intramuscular injection, subcutaneous,endo-tracheal tube,and intranasal injection (use of a wedge device attached to the syringe to create a mist delivering the drug to the nasal [[mucosa]]) may also be utilized, although these are more likely in the prehospital setting.


==Uses==
* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Naloxone has been distributed as part of emergency kits to heroin users, and this has been shown to reduce rates of fatal overdose. Projects of this type are under way in San Francisco, New Mexico, Philadelphia, New York State, Baltimore, Boston, Los Angeles and Chicago, with pilot projects started in Scotland in 2006.


The drug also blocks the action of pain-lowering [[endorphin]]s which the body produces naturally. The likely reason for this is that these endorphins operate on the same opioid receptors. In one experiment, women treated with naloxone reported higher pain levels during [[childbirth]] than women not so treated. Naloxone is capable of blocking a [[placebo]] pain-lowering response, both in clinical and experimental pain, if the placebo is administered together with a hidden or blind injection of naloxone.<ref>Sauro, Marie D; Greenberg, Roger P. ''Endogenous opiates and the placebo effect: A meta-analytic review''. Journal of Psychosomatic Research. Vol 58(2) Feb 2005, 115-120.</ref>
<!--Brand Names-->


While naloxone is still often used in emergency treatments for opioid overdose, its clinical use in the long-term treatment of opioid [[addiction]] is being increasingly superseded by [[naltrexone]]. Naltrexone is structurally similar but has a slightly increased affinity for κ-opioid receptors over naloxone, can be administered orally and has a longer duration of action.
|brandNames=


Enteral naloxone has been successfully used in the reduction of [[gastritis]] and [[esophagitis|oesophagitis]] associated with opioid therapy in mechanically-ventilated acute care patients.
* ®<ref>{{Cite web | title =  | url =  }}</ref>


The effect of the hallucinogenic plant [[Salvia Divinorum]] and its primary active chemical Salvinorin-A, a κ-opioid agonist, can be inhibited by the pre-administration of naloxone. Naloxone has similar inhibitory effects on [[PCP]], [[ketamine]], and [[dextromethorphan]].
<!--Look-Alike Drug Names-->


Naloxone is also being used as a secondary chemical in the [[FDA]] approved medicine [[Suboxone]]. [[Suboxone]] and [[Subutex]] were created as part of a detox program to help [[opiate]] addicted patients stop using opiates. Suboxone contains 4 parts [[Buprenorphine]] and 1 part Naloxone, while Subutex contains only Buprenorphrine.
|lookAlike=


Naloxone was added to Suboxone in an effort to dissuade patients from grinding up the Suboxone tablet and using it as part of a combination of opiates that the user would inject into their body. Intravenously administered Naloxone is supposed to block the effects of any opiates and cause the user to go into immediate withdrawal. However, buprenorphine has a higher affinity for the opiate receptors, and many users have reported that Suboxone is injectable without inducing withdrawal effects. Oral or sublingual administration affects only the gastronintestinal tract, and has the added benefit of helping to reverse constipation and lowered bowel motility caused by chronic medical use or abuse of a variety of opioids. Buprenorphine itself has less of an effect on the central nervous system and produces far less [[euphoria]] than other [[opioid]] drugs, while still being effective in the treatment of pain. For this reason, buprenorphine is gaining acceptance in the treatment of chronic pain, as well as opioid addiction withdrawal, since it produces fewer side effects and less sedation. On the whole, it is a drug moderately useful in pain management that is further attractive due to its relative lack of desireability to opioid abusers. Currently, only certified addictionologists (physicians specializing in the treatment of drug addiction and dependence) are legally permitted to prescribe Suboxone or other drugs containing buprenorphine. Like [[methadone]], buprenorphine has only recently been approved for use in the management of pain, and likely restrictions on prescribing authority will be eased over time as buprenorphine sees wider use and acceptance by the medical profession, and concerns over diversion and abuse lessen.
* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>


The addition of naloxone to bruprenorphine in Suboxone tablets is intended to prevent misuse and abuse by injection. However, the Naloxone in Suboxone does cause side effects in some people. These side effects include, but are not limited to, [[asthenia]], [[chills]], [[headache]], [[infection]], [[pain and nociception|pain]], [[pain and nociception|pain]] in the [[abdomen]], [[back pain]], [[withdrawal]] syndrome, [[vasodilation]], [[constipation]], [[diarrhea]], [[nausea]], [[vomiting]], [[insomnia]], and [[sweating]].  Because of these side effects, the FDA recommends that doctors begin any chemical detox using [[Subutex]], which does not contain any Naloxone. In this way, if for some reason the doctor moves the patient to Suboxone and the patient begins having side effects related to Naloxone, the doctor can easily move the patient back to Subutex.
<!--Drug Shortage Status-->


For these reasons and others, it has been reported that Subutex is easier to withdraw from than is Suboxone.
|drugShortage=
}}


==Legal status==
<!--Pill Image-->
The [[patent]] for Naloxone has expired and the drug is currently available in various [[generic drug|generic]] forms.


==Identification==
{{PillImage
The [[CAS number]] of naloxone is 465-65-6; the anhydrous [[hydrochloride]] [[salt]] has CAS 357-08-4 and the hydrochloride salt with 2 molecules of water has CAS 51481-60-8.
|fileName=No image.jpg|This image is provided by the National Library of Medicine.
|drugName=
|NDC=
|drugAuthor=
|ingredients=
|pillImprint=
|dosageValue=
|dosageUnit=
|pillColor=
|pillShape=
|pillSize=
|pillScore=
}}


==References==
<!--Label Display Image-->
{{reflist|1}}


== External links ==
{{LabelImage
* [http://www.anypositivechange.org/NALOXONE/ Chicago Recovery Alliance's naloxone distribution project]
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
* [http://www.inchem.org/documents/antidote/antidote/ant01.htm Report on Naloxone and other opiate antidotes], by the International Programme on Chemical Safety
}}


{{Opioids}}
{{LabelImage
{{Antidotes}}
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
[[bg:Налоксон]]
}}
[[da:Naloxon]]
[[de:Naloxon]]
[[es:Naloxona]]
[[fr:Naloxone]]
[[it:Naloxone]]
[[ja:ナロキソン]]
[[he:נרקאן]]
[[no:Naloxon]]
[[ru:Налоксон]]
[[sv:Naloxon]]


[[Category:Antidotes]]
<!--Category-->
[[Category:Opioids]]
[[Category:Opioid antagonists]]
[[Category:Drugs]]
[[Category:Emergency medicine]]
[[Category:Anesthesiology]]


[[pl:Nalokson]]
[[Category:Drug]]
{{WH}}
{{WikiDoc Sources}}

Revision as of 17:01, 15 December 2014

Naloxone
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Vignesh Ponnusamy, M.B.B.S. [2]

Disclaimer

WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.

Overview

Naloxone is an opioid antagonist that is FDA approved for the {{{indicationType}}} of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression. Common adverse reactions include hypotension, hypertension, ventricular tachycardia, ventricular fibrillation, dyspnea, pulmonary edema, cardiac arrest, death, coma, and encephalopathy.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition1
  • Dosing Information
  • Dosage
Condition2
  • Dosing Information
  • Dosage
Condition3
  • Dosing Information
  • Dosage
Condition4
  • Dosing Information
  • Dosage

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Naloxone in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Naloxone in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Naloxone in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Naloxone in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Naloxone in pediatric patients.

Contraindications

  • EVZIO is contraindicated in patients known to be hypersensitive to naloxone hydrochloride or to any of the other ingredients.

Warnings

Precautions

  • Duration of Effect
  • The duration of action of most opioids is likely to exceed that of EVZIO resulting in a return of respiratory and/or central nervous system depression after an initial improvement in symptoms. Therefore, it is necessary to seek immediate emergency medical assistance after delivering the first dose of EVZIO, keep the patient under continued surveillance, and repeat doses of EVZIO as necessary. Additional supportive and/or resuscitative measures may be helpful while awaiting emergency medical assistance.
  • Limited Efficacy with Partial Agonists or Mixed Agonist/Antagonists
  • Reversal of respiratory depression by partial agonists or mixed agonist/antagonists such as buprenorphine and pentazocine, may be incomplete. Large doses of naloxone hydrochloride are required to antagonize buprenorphine because the latter has a long duration of action due to its slow rate of binding and subsequent slow dissociation from the opioid receptor. Buprenorphine antagonism is characterized by a gradual onset of the reversal effects and a decreased duration of action of the normally prolonged respiratory depression.
  • Precipitation of Severe Opioid Withdrawal
  • The use of EVZIO in patients who are opioid dependent may precipitate an acute abstinence syndrome characterized by the following signs and symptoms: body aches, diarrhea, tachycardia, fever, runny nose, sneezing, piloerection, sweating, yawning, nausea or vomiting, nervousness, restlessness or irritability, shivering or trembling, abdominal cramps, weakness, and increased blood pressure. In neonates, opioid withdrawal may be life-threatening if not recognized and properly treated and may include the following signs and symptoms: convulsions, excessive crying, and hyperactive reflexes.
  • Abrupt postoperative reversal of opioid depression after using naloxone hydrochloride may result in nausea, vomiting, sweating, tremulousness, tachycardia, hypotension, hypertension, seizures, ventricular tachycardia and fibrillation, pulmonary edema, and cardiac arrest. Death, coma, and encephalopathy have been reported as sequelae of these events. These events have occurred in patients most of whom had pre-existing cardiovascular disorders or received other drugs which may have similar adverse cardiovascular effects. Although a direct cause and effect relationship has not been established, after use of naloxone hydrochloride, patients with pre-existing cardiac disease or patients who have received medications with potential adverse cardiovascular effects should be monitored for hypotension, ventricular tachycardia or fibrillation, and pulmonary edema in an appropriate healthcare setting. It has been suggested that the pathogenesis of pulmonary edema associated with the use of naloxone hydrochloride is similar to neurogenic pulmonary edema, i.e., a centrally mediated massive catecholamine response leading to a dramatic shift of blood volume into the pulmonary vascular bed resulting in increased hydrostatic pressures.

Adverse Reactions

Clinical Trials Experience

  • The following adverse reactions have been identified during post-approval use of naloxone hydrochloride in the post-operative setting. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure: Hypotension, hypertension, ventricular tachycardia and fibrillation, dyspnea, pulmonary edema, and cardiac arrest. Death, coma, and encephalopathy have been reported as sequelae of these events. Excessive doses of naloxone hydrochloride in post-operative patients have resulted in significant reversal of analgesia and have caused agitation [see Warnings and Precautions (5.3)].
  • Abrupt reversal of opioid effects in persons who were physically dependent on opioids has precipitated an acute withdrawal syndrome. Signs and symptoms have included: body aches, fever, sweating, runny nose, sneezing, piloerection, yawning, weakness, shivering or trembling, nervousness, restlessness or irritability, diarrhea, nausea or vomiting, abdominal cramps, increased blood pressure, tachycardia. In the neonate, opioid withdrawal signs and symptoms also included: convulsions, excessive crying, hyperactive reflexes [see Warnings and Precautions (5.3)].

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Naloxone in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Naloxone in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Naloxone during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Naloxone with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Naloxone with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Naloxone with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Naloxone with respect to specific gender populations.

Race

There is no FDA guidance on the use of Naloxone with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Naloxone in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Naloxone in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Naloxone in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Naloxone in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

There is limited information regarding Monitoring of Naloxone in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Naloxone in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Naloxone in the drug label.

Pharmacology

There is limited information regarding Naloxone Pharmacology in the drug label.

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Naloxone in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Naloxone in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Naloxone in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Naloxone in the drug label.

How Supplied

Storage

There is limited information regarding Naloxone Storage in the drug label.

Images

Drug Images

{{#ask: Page Name::Naloxone |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Naloxone |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Naloxone in the drug label.

Precautions with Alcohol

  • Alcohol-Naloxone interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ Empty citation (help)
  2. ↑ "http://www.ismp.org". External link in |title= (help)


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