Consumer medicine information

Junalox

Naloxone hydrochloride

BRAND INFORMATION

Brand name

Junalox

Active ingredient

Naloxone hydrochloride

Schedule

S3

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Junalox.

What is in this leaflet

This leaflet answers some common questions about JUNALOX. It does not contain all the available information and it does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor or pharmacist has weighed the risks of you being treated with this medicine against the benefits it is expected to have for you.

Please read this leaflet carefully and follow the instructions given to you by your doctor or pharmacist, and the advice contained in this leaflet.

If you have any concerns about being treated with this medicine, ask your doctor or pharmacist.

Keep this leaflet. You may need to read it again.

What JUNALOX is used for

Naloxone hydrochloride dihydrate belongs to a group of medicines called opioid antagonists.

Naloxone hydrochloride dihydrate works by reversing the effects of opium-like substances such as morphine, heroin and codeine.

Your doctor or pharmacist may have prescribed this medicine for another reason. Ask your doctor or pharmacist if you have any questions about why this medicine has been prescribed for you.

This medicine is available from your pharmacist.

Before you are given JUNALOX

When JUNALOX must not be given

You should not be given this medicine if you have an allergy to:

  • Any medicine containing naloxone hydrochloride dihydrate
  • Any of the ingredients listed at the end of this leaflet

Some of the symptoms of an allergic reaction may include:

  • Shortness of breath
  • Wheezing or difficulty breathing
  • Swelling of the face, lips, tongue or other parts of the body
  • Rash, itching or hives on the skin.

You should not be given this medicine if the solution is discoloured or cloudy, turbid or a precipitate is present. The injection is normally a clear and colourless solution, practically free from visible particles.

You should not be given this medicine after the expiry date printed on the pack, or if the packaging is torn or shows signs of tampering. In that case, return it to your pharmacist.

If you are not sure whether you should be given this medicine, talk to your doctor or pharmacist.

Before you are given JUNALOX

Tell your doctor or pharmacist if you have allergies to any other medicines, foods, preservatives or dyes.

Tell your doctor or pharmacist if you have any of the following medical conditions:

  • Heart disease
  • Lung disease
  • Kidney disease
  • Liver disease
  • Drug addiction (including an addition to alcohol)

Tell your doctor or pharmacist if you are pregnant or plan to become pregnant. Your doctor or pharmacist can discuss with you the risks and benefits involved.

Tell your doctor or pharmacist if you are breastfeeding or plan to breastfeed Your doctor or pharmacist can discuss with you the risks and benefits involved.

If you have not told your doctor or pharmacist about any of the above, tell them before you are given this medicine.

Taking other medicines

Tell your doctor or pharmacist about any other medicines you are taking including medicines that you buy without a prescription, in a pharmacy, supermarket or health food shop. Some medicines may interfere with JUNALOX.

These include but are not limited to:

  • Pain killers
  • Cough and cold remedies
  • Alcohol
  • Heart or blood pressure medications

These medicines may be affected or may affect how well JUNALOX works. You may need different amounts of your medicines, or you may need to take different medicines.

Your doctor or pharmacist has more information on medicines to be careful with or avoid while being given this medicine.

How JUNALOX is given

This medicine must only be given as directed by your doctor, pharmacist or nursel.

How it is given

This medicine can be given as an injection into a muscle (intramuscular).

How much is given

The entire contents of one ampoule (400 micrograms) should be injected into muscle of the upper arm or thigh.

IF THERE IS NO RESPONSE another dose (400 micrograms) should be injected in 2 to 5 minutes. Another dose can be given at any time If required.

If you are given too much JUNALOX)

Symptoms of an overdose may be the same as side effects but may be more severe. The symptoms of a side effect are listed under Side Effects below.

Immediately telephone your doctor or Poisons Information Centre for advice (in Australia telephone 13 11 26) or go to Accident & Emergency at your nearest hospital if you think you or anyone else has been given too much of this medicine.

While you being treated with JUNALOX

Things you must do

If you are about to be started on any new medicine, remind your doctor and pharmacist that you have been given JUNALOX.

Tell any other doctors, dentists and pharmacists who treat you that you have been treated with this medicine.

If you are going to have surgery, tell the surgeon or anaesthetist that you have been given this medicine. It may affect other medicines used during surgery.

If you become pregnant while being treated with this medicine, tell your doctor immediately.

If you are about to have any blood tests, tell your doctor that you have been given this medicine. It may interfere with the results of some tests.

Things to be careful of

Do not drive or operate machinery after you have been given JUNALOX, for at least 24 hours (1 day).

Do not drink alcohol while you are being given this medicine.

If you feel light-headed, dizzy or faint when getting out of bed or standing up, get up slowly. Standing up slowly, especially when you get up from a bed or a chair, will help your body get used to the change in position and blood pressure. If this problem continues or gets worse, talk to your doctor.

Side effects

Tell your doctor, pharmacist or nurse as soon as possible if you do not feel well while you are being given this medicine.

This medicine helps most people reverse the life threatening opioid overdose, but it may have unwanted side effects in a few people.

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Do not be alarmed by the following list of side effects. You may not experience any of them.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor, pharmacist or nurse if you notice any of the following and they worry you.

  • Dizziness
  • Headache
  • Nausea
  • Vomiting
  • Pain at the site of injection

The above list includes the more common side effects of your medicine.

Tell your doctor as soon as possible if you notice any of the following:

  • Sweating
  • Tremor
  • Increased heart rate
  • Nervousness or restlessness
  • Irritability
  • Violent behavior or agitation

The above list includes serious side effects that may require medical attention.

If any of the following happen, tell your doctor or go to Accident and Emergency at your nearest hospital immediately:

  • Shortness of breath
  • Wheezing or difficulty breathing
  • Swelling of the face, lips, tongue or other parts of the body
  • Rash, itching or hives on the skin

The above list includes very serious side effects. You may need urgent medical attention or further hospitalization. These side effects are very rare.

Tell your doctor, pharmacist or nurse if you notice anything that is making you feel unwell.

Other side effects not listed above may also occur in some people.

After treatment with JUNALOX

Storage

This medicine should be kept in a cool dry place, protected from the light where the temperature stays below 25 degrees Celsius.

This medicine must only be opened when it is time for you to have the injection.

Product Description

What it looks like

JUNALOX Solution for Injection is a clear and colourless solution. It should not be given if there are any crystals or particles visible in the solution.

Ingredients

Active ingredient: Naloxone hydrochloride dihydrate.

The inactive ingredients are hydrochloric acid (for pH adjustment) and water for injections.

This medicine does not contain lactose, sucrose, gluten, tartrazine, alcohol, dyes or preservatives

The 1 mL ampoule (JUNALOX) contains 400 micrograms of naloxone hydrochloride (as dihydrate) and Water for Injections to 1 mL. It is available in packs of 5.

If you want to know more

If you have any questions about your treatment with this medicine, ask your doctor or pharmacist.

Supplier

Juno Pharmaceuticals Pty Ltd
42 Kelso Street,
Cremorne
VIC - 3121
Australia

JUNALOX AUST R 236004

This leaflet was prepared in May 2020.

Published by MIMS July 2020

BRAND INFORMATION

Brand name

Junalox

Active ingredient

Naloxone hydrochloride

Schedule

S3

 

1 Name of Medicine

The name of this medicine is naloxone hydrochloride dihydrate.

2 Qualitative and Quantitative Composition

Junalox, an opioid antagonist, is a synthetic congener of oxymorphone. In structure it differs from oxymorphone in that the methyl group on the nitrogen atom is replaced by an allyl group.
Naloxone hydrochloride dihydrate occurs as a white to slightly off-white powder, and is soluble in water, in dilute acids, and in strong alkalis, slightly soluble in alcohol, practically insoluble in ether and in chloroform.
Junalox is a clear, colourless solution. It is available as a sterile solution for intramuscular administration at a concentration of 400 micrograms of naloxone hydrochloride (as dihydrate) in 1 mL of water for injections. The pH is adjusted to 3.0 - 3.3 with hydrochloric acid.

3 Pharmaceutical Form

See Section 2 Qualitative and Quantitative Composition.

4 Clinical Particulars

4.1 Therapeutic Indications

Junalox is indicated for the treatment of opioid overdose.

4.2 Dose and Method of Administration

Junalox may be administered intramuscularly.
Since the duration of action of some opioids may exceed that of naloxone hydrochloride dihydrate the patient should be kept under continued surveillance, and repeated doses of naloxone hydrochloride dihydrate should be administered, as necessary.
Junalox contains no antimicrobial preservative, therefore are for use in one patient on one occasion only; after use, any remaining solution should be discarded.

Usage in adults.

Opioid overdose.

Known or suspected. An initial dose of 400 micrograms to 2 mg of Junalox may be administered by intramuscular injection. If the desired degree of counteraction and improvement in respiratory functions is not obtained it may be repeated at 2 to 3 minute intervals. If no response is observed after 10 mg of naloxone hydrochloride dihydrate has been administered, the diagnosis of opioid induced or partial narcotic induced toxicity should be questioned.

Overdose action plan.

1. Prepare needle and syringe for muscular injection by unwrapping 3 mL syringe and screwing on 23 G needle.
2. Remove naloxone ampoule tray from pack.
3. Take ampoule and hold ampoule between thumb and index finger in one hand.
4. With the other hand, pinch top of ampoule with index finger on one side and thumb on other side.
5. Snap ampoule open by breaking the top of the ampoule at the white ring.
6. Draw all of the naloxone out of the ampoule by inserting the needle in the naloxone solution and drawing the plunger from the syringe barrel.
It is recommended to have at least 5 ampoules (one pack) on hand as multiple doses may be required, and it is possible to break an ampoule on opening.

4.3 Contraindications

Junalox is contraindicated in patients known to be hypersensitive to naloxone hydrochloride dihydrate or to any other ingredients in Junalox.

4.4 Special Warnings and Precautions for Use

Naloxone hydrochloride dihydrate should be administered cautiously to persons including newborns of mothers who are known or suspected to be physically dependent on opioids. In such cases an abrupt and complete reversal of opioid effects may precipitate an acute withdrawal syndrome.
The signs and symptoms of opioid withdrawal in patients physically dependent on opioids may include, but are not limited to, the following: body aches, diarrhoea, tachycardia, fever, runny nose, sneezing, piloerection, sweating, yawning, nausea and vomiting, nervousness, restlessness or irritability, shivering or trembling, abdominal cramps, weakness, and increased blood pressure. In the neonate opioid withdrawal may also include: convulsions, excessive crying and hyperactive reflexes.
The patient who has satisfactorily responded to naloxone hydrochloride dihydrate should be kept under continued surveillance and repeated doses of naloxone hydrochloride dihydrate should be administered, as necessary, since the duration of action of some opioids may exceed that of naloxone hydrochloride dihydrate. Large doses of naloxone hydrochloride dihydrate in postoperative patients may result in a clear reversal in analgesia, excitement and an elevation in blood pressure. A reversal of opioid effects achieved too rapidly may induce nausea, vomiting, sweating or tachycardia.
Naloxone hydrochloride dihydrate is not effective against respiratory depression due to nonopioid drugs.
Reversal of buprenorphine-induced respiratory depression may be incomplete. If an incomplete response occurs, respiration should be mechanically assisted.
In addition to naloxone hydrochloride dihydrate, other resuscitative measures such as maintenance of a free airway, artificial ventilation, cardiac massage, and vasopressor agents should be available and employed when necessary to counteract acute opioid poisoning.
Naloxone hydrochloride dihydrate should also be used with caution in patients with pre-existing pulmonary disease, since sudden exacerbation of underlying pulmonary disease may occur.

Use in hepatic impairment.

The safety and effectiveness of naloxone hydrochloride dihydrate in patients with liver disease have not been established in well-controlled clinical trials. In one small study in patients with liver cirrhosis, plasma naloxone hydrochloride dihydrate concentrations were approximately six times higher than in patients without liver disease. Caution should be exercised when naloxone hydrochloride dihydrate is administered to patients with hepatic disease.

Use in renal impairment.

The safety and effectiveness of naloxone hydrochloride dihydrate in patients with renal insufficiency / failure have not been established in well-controlled clinical trials. Caution should be exercised when naloxone hydrochloride dihydrate is administered to this patient population.

Use in the elderly.

No data available.

Paediatric use.

No data available.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

The effect of naloxone hydrochloride dihydrate is based on the interaction with opioids and opioid agonists, reversing effects of opioids; rapid reversal may precipitate acute withdrawal syndrome in opioid dependence. At the usual naloxone hydrochloride dihydrate dose there is no interaction with barbiturates and tranquillizers. Data on the interaction with alcohol are not uniform. In patients with multiple intoxication with opioids and sedatives or alcohol, the result of naloxone hydrochloride dihydrate administration may be delayed, dependent on the cause of intoxication.
Complete analgesia can be restored following administration of naloxone hydrochloride dihydrate to patients that had buprenorphine as analgesic. It is assumed that this effect is caused by the arched form of the dose-response curve of buprenorphine with decreasing analgesia at (too) high doses. However, reversal of respiratory depression caused by buprenorphine is limited.
Serious hypertension has been reported following administration of naloxone hydrochloride dihydrate to patients in a coma caused by clonidine-overdosing, naloxone hydrochloride dihydrate reverses the analgesic and other effects of opioid agonist/ antagonists such as pentazocine, so may precipitate withdrawal symptoms if used concurrently with these medicines in physically dependent patients.
Naloxone hydrochloride dihydrate reverses the analgesic and other effects of opioid agonist analgesics, and may precipitate withdrawal symptoms if used concurrently with these medicines in physically dependent patients, including patients receiving methadone to treat opioid dependence.
When naloxone hydrochloride dihydrate is used postoperatively to reverse the central depressive effects of opioid agonists used as anaesthesia adjuncts, the dose of naloxone hydrochloride dihydrate must be carefully titrated to achieve the desired effect without interfering with control of postoperative pain, or causing other adverse effects.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

Reproductive studies in mice and rats demonstrated no impairment of fertility.
(Category B1)
Teratogenic effects. Reproduction studies performed in mice and rats at high subcutaneous doses, revealed no evidence of impaired fertility or harm to the foetus due to naloxone hydrochloride dihydrate. There are, however, no adequate and well controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, naloxone hydrochloride dihydrate should, therefore, be administered to pregnant patients only when, in the judgement of the physician, the potential benefits outweigh the possible hazards.
Non-teratogenic effects. Risk/ benefit must be considered before naloxone hydrochloride dihydrate is administered to a pregnant woman who is known or suspected to be opioid dependent since maternal dependence may often be accompanied by foetal dependence. Naloxone crosses the placenta and may precipitate withdrawal in the foetus as well as in the mother.

Use in labour and delivery.

It is not known if naloxone hydrochloride dihydrate affects the duration of labour and/or delivery.
 It is not known whether naloxone hydrochloride dihydrate is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when naloxone hydrochloride dihydrate is administered to a nursing woman.

4.7 Effects on Ability to Drive and Use Machines

No studies on the effects on the ability to drive and use machines have been performed.
Patients who have received naloxone hydrochloride dihydrate to reverse the effect of opioids should be warned not to take part in road traffic, to operate machinery or to engage in other activities demanding physical or mental exertion for at least 24 hours, since the effect of the opioids may return.

4.8 Adverse Effects (Undesirable Effects)

The following undesirable effects are ranked according to system organ class and to their frequency: Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.
Very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1,000 to < 1/100); rare (≥ 1/10,000 to < 1/1,000); very rare (< 1/10,000); not known (cannot be estimated from the available data).

Immune system disorders.

Very rare: Allergic reactions (urticaria, rhinitis, dyspnoea, Quincke's oedema), anaphylactic shock.

Nervous system disorders.

Common: Dizziness, headache.
Uncommon: Tremor, sweating.
Rare: Seizures, tension.
Seizures have occurred rarely following administration of naloxone hydrochloride dihydrate; however, a causal relationship to the drug has not been established.

Cardiac disorders.

Common: tachycardia.
Uncommon: Arrhythmia, bradycardia.
Very rare: fibrillation, cardiac arrest.

Vascular disorders.

Common: hypotension, hypertension.

Respiratory, thoracic and mediastinal disorders.

Very rare: pulmonary oedema.

Gastrointestinal disorders.

Very common: nausea.
Common: vomiting.
Uncommon: diarrhoea, dry mouth.

Skin and subcutaneous tissue disorders.

Very rare: erythema multiforme.
One case of erythema multiforme cleared promptly after naloxone hydrochloride dihydrate was discontinued.

General disorders and administration site conditions.

Common: postoperative pain.
Uncommon: hyperventilation, irritation of vessel wall (after i.v. administration).
Opioid dependence. Agitation and paraesthesias have been infrequently reported with the use of naloxone hydrochloride dihydrate.
Drug abuse and dependence. Naloxone hydrochloride dihydrate is an opioid antagonist.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at http://www.tga.gov.au/reporting-problems.

4.9 Overdose

There is limited clinical experience with naloxone hydrochloride dihydrate overdosage in humans.
In a study, 36 patients with acute stroke received a loading dose of 4 mg/kg (10 mg/m2/min) of naloxone hydrochloride dihydrate followed immediately by 2 mg/kg/hour for 24 hours. There were a few reports of serious adverse events: seizures (2 patients), severe hypertension (1), and hypotension and/or bradycardia (3). At doses of 2 mg/kg in normal subjects, memory impairment has been reported.

Patient management.

Patients who experience a naloxone hydrochloride dihydrate overdose should be treated symptomatically in a closely-supervised environment. Physicians should contact a poison control centre for the most up to date patient management information.
Some chemical impurities in naloxone hydrochloride dihydrate i.e., noroxymorphone and bisnaloxone, have been shown to produce emesis in dogs when administered alone at intravenous doses equivalent to impurity levels present in naloxone hydrochloride dihydrate at 60 times the usual human dose (10 mg/day).
For information on the management of overdose, contact the Poison Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Naloxone hydrochloride dihydrate prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.
Naloxone hydrochloride dihydrate is an essentially pure opioid antagonist, i.e. it does not possess the "agonistic" or morphine-like properties characteristic of other opioid antagonists; naloxone hydrochloride dihydrate does not produce respiratory depression or psychotomimetic effects of pupillary constriction. In the absence of opioid or agonistic effects of other opioid antagonists it exhibits essentially no pharmacologic activity.
Naloxone hydrochloride dihydrate has not been shown to produce tolerance or to cause physical or psychological dependence. In the presence of physical dependence on opioids, naloxone hydrochloride dihydrate will produce withdrawal symptoms. While the mechanism of action of naloxone hydrochloride dihydrate is not fully understood, the preponderance of evidence suggests that naloxone hydrochloride dihydrate antagonises the opioid effects by competing for the same receptor sites.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

When naloxone hydrochloride dihydrate is administered intravenously the onset of action is generally apparent within two minutes; the onset of action is only slightly less rapid when it is administered subcutaneously or intramuscularly. The duration of action is dependent upon the dose and route of administration of naloxone hydrochloride dihydrate. Intramuscular administration produces a more prolonged effect than intravenous administration. The requirement for repeat doses of naloxone hydrochloride dihydrate, however, will also be dependent upon the amount, type and route of administration of the opioid being antagonised.

Distribution.

Following parenteral administration, naloxone hydrochloride dihydrate is rapidly distributed in the body.

Metabolism and excretion.

Naloxone hydrochloride dihydrate is metabolised in the liver, primarily by glucuronide conjugation, and excreted in the urine. In one study the serum half-life in adults ranged from 30 to 81 minutes (mean 64 ± 12 minutes).
In a neonatal study the mean plasma half-life was observed to be 3.1 ± 0.5 hours.

5.3 Preclinical Safety Data

Genotoxicity, carcinogenicity.

Carcinogenicity and mutagenicity studies have not been performed with naloxone hydrochloride dihydrate.

6 Pharmaceutical Particulars

6.1 List of Excipients

See Section 2 Qualitative and Quantitative Composition.

6.2 Incompatibilities

No drug or chemical agent should be added to Junalox unless its effect on the chemical and physical stability of the solution has first been established. JUNALOX should not be mixed with preparations containing sulfite, metabisulfite, long chain or high molecular weight anions, or any solution having an alkaline pH.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Protect from light. Store below 25°C.

6.5 Nature and Contents of Container

Container type.

Clear glass ampoules.

Pack sizes.

1, 5 and 10 ampoules.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Naloxone hydrochloride dihydrate.

Chemical name: 4,5α-Epoxy-3,14-dihydroxy-17- (prop-2-enyl)morphinan-6-one hydrochloride dihydrate.

Chemical structure.


CAS number.

51481-60-8.
Molecular formula: C19H22ClNO4.2H2O.
Molecular weight: 399.87.

7 Medicine Schedule (Poisons Standard)

Schedule 3 (Pharmacist Only Medicine).

Summary Table of Changes