Consumer medicine information

Endone

Oxycodone hydrochloride

BRAND INFORMATION

Brand name

Endone

Active ingredient

Oxycodone hydrochloride

Schedule

What is in this leaflet

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

All medicines have risks and benefits. Your doctor has weighed the risks of you taking ENDONE against the benefits they expect it will have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may want to read it again.

What ENDONE is used for

This medicine is used for the short-term management of severe pain.

This medicine belongs to a group of medicines called narcotic analgesics.

The active ingredient in this medicine works by binding to receptors called opioid receptors, which are in your central nervous system. This binding action changes your body's perception of pain throughout the central nervous system producing the pain relieving (analgesic) effect.

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

This medicine is only available with a doctor’s prescription.

ADDICTION
You can become addicted to ENDONE even if you take it exactly as prescribed. ENDONE may become habit forming causing mental and physical dependence. If abused it may become less able to reduce pain.

DEPENDENCE
As with all other opioid containing products, your body may become used to you taking ENDONE. Taking it may result in physical dependence. Physical dependence means that you may experience withdrawal symptoms if you stop taking ENDONE suddenly, so it is important to take it exactly as directed by your doctor.

TOLERANCE
Tolerance to ENDONE may develop, which means that the effect of the medicine may decrease. If this happens, more may be needed to maintain the same effect. Speak to your doctor if this occurs.

WITHDRAWAL
Continue taking your medicine for as long as your doctor tells you. If you stop taking this medicine suddenly, your pain may worsen and you may experience some or all of the following withdrawal symptoms:

nervousness, restlessness, agitation, trouble sleeping or anxiety
body aches, weakness or stomach cramps
loss of appetite, nausea, vomiting or diarrhoea
increased heart rate, breathing rate or pupil size
watery eyes, runny nose, chills or yawning
increased sweating

ENDONE given to the mother during labour can cause breathing problems and signs of withdrawal in the newborn.

Before you take ENDONE

When you must not take it

Do not take ENDONE if you have an allergy to:

any medicine containing oxycodone hydrochloride
any other narcotic analgesics such as morphine, codeine, or opium
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

Do not take this medicine if you are pregnant. It may affect your developing baby if you take it during pregnancy.

Do not breast-feed if you are taking this medicine. The active ingredient in ENDONE passes into breast milk and there is a possibility that your baby may be affected.

Do not give this medicine to children. Safety and effectiveness in children have not been established.

Do not take this medicine if you have or have had any of the following:

head injury
brain tumour
epilepsy or other convulsive disorders
heart problems such as an irregular and/or rapid heartbeat
chronic obstructive pulmonary disease, asthma or other respiratory diseases
severe headaches, or headaches due to raised pressure in the head
a history of alcohol or drug abuse
a history of mental illness

Do not take this medicine if you are taking or have taken medicines for depression called Monoamine Oxidase Inhibitors (MAOs) within the last 14 days.

Do not take this medicine after the expiry date printed on the pack or if the packaging is torn or shows signs of tampering. If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should be taking this medicine, consult your doctor.

Before you start to take it

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

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

muscle weakness
underactive thyroid
kidney disease
liver disease
low blood pressure
prostate problems, or difficulty in passing urine
bowel disorders
prescription or illicit drug addiction

If you have not told your doctor about any of the above, tell them before you start taking ENDONE.

Taking other medicines

Tell your doctor or pharmacist if you are taking any other medicines, including any that you get without a prescription from your pharmacy, supermarket or health food shop.

Some medicines ENDONE may interfere with each other. These include:

anaesthetics
anticoagulants, medicines used to thin the blood
medicines used to treat epilepsy
medicines used to help with sleeping
medicines used to help lower blood pressure
medicines used to treat anxiety
medicines used to treat depression
medicines used to treat cold and flu symptoms
other medicines used to relieve pain
medicines, used to relieve nausea and vomiting
atropine-like medicines, used to prevent travel sickness and for stomach cramps and spasms
medicines used to treat chronic obstructive pulmonary disorder
antipsychotic medicines, used to treat psychosis, schizophrenia or bipolar disorder
antihistamine medicines, used to treat allergic skin conditions or hay fever
any medicine containing naloxone and/or naltrexone, used to reverse the effects of narcotic analgesics

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

Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.

How to take ENDONE

Follow all directions given to you by your doctor or pharmacist carefully. They may differ from the information contained in this leaflet.

If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How much to take

The usual dose is one tablet every six hours.

Your doctor may prescribe a different dose for you. Be sure to follow your doctor’s directions about when and how to take ENDONE.

How to take it

Swallow the tablets whole with a full glass of water.

When to take it

Take your medicine at about the same time each day. Taking it at the same time each day will have the best effect. It will also help you remember when to take it.

ENDONE should be taken after food or with milk.

How long to take it

Continue taking your medicine for as long as your doctor tells you.

If you have been using this medicine for a long period of time and it is no longer needed to manage your pain DO NOT stop taking ENDONE suddenly. Your doctor may want you to gradually reduce the amount of ENDONE you are taking before stopping completely in order to lessen the risk of withdrawal symptoms.

If you forget to take it

If it is less than 3 hours before your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take it as soon as you remember, and then go back to taking your medicine as you would normally.

Do not take a double dose to make up for the dose that you missed. This may increase the chance of you getting an unwanted side effect.

If you are not sure what to do, ask your doctor or pharmacist.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints.

If you take too much (overdose)

If you or someone else receives too much (overdose), and experience one or more of the symptoms below, immediately call triple zero (000) for an ambulance. Keep the person awake by talking to them or gently shaking them every now and then. You should follow the above steps even if someone other than you have accidentally used ENDONE that was prescribed for you. If someone takes an overdose, they may experience one or more of the following symptoms:

slow, unusual or difficult breathing
drowsiness, dizziness or unconsciousness
slow or weak heartbeat
nausea or vomiting
convulsions or fits
Clumsiness or loss of coordination
Difficulty walking
Facial drooping
Loss of vision
Personality changes
Trouble speaking
Weak muscles

If you think you or someone else may have used too much ENDONE, you should immediately:

phone the Poisons Information Centre (by calling 13 11 26), or
contact your doctor, or
go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

When seeking medical attention, take this leaflet and any remaining medicine with you to show the doctor. Also tell them about any other medicines or alcohol which have been taken.

While you are using ENDONE

Things you must do

If you are about to be started on any new medicine, remind your doctor and pharmacist that you are taking ENDONE.

Tell any other doctors, dentists and pharmacists who treat you that you are taking this medicine.

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

If you become pregnant while taking this medicine, tell your doctor immediately.

Keep all of your doctor's appointments so that your progress can be checked.

Things you must not do

Do not take ENDONE to treat any other complaints unless your doctor tells you to.

Do not give your medicine to anyone else, even if they have the same condition as you.

Do not stop taking your medicine or lower the dosage without first checking with your doctor. If you stop taking it suddenly, your condition may worsen, you may have unwanted side effects, or you may experience withdrawal symptoms. Your doctor will gradually reduce the amount you take each day before stopping this medicine completely.

Do not drive or operate machinery until you know how ENDONE affects you. This medicine may impair the mental and physical ability needed to drive a car or operate heavy machinery. It may cause drowsiness. If you have any of these symptoms, do not drive, operate machinery or do anything else that could be dangerous.

Do not drink alcohol while you are taking this medicine.

Things to be careful of

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 bed or chairs, 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 or pharmacist as soon as possible if you do not feel well while you are taking ENDONE.

This medicine helps most people with their pain, 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 attention if you get some of the side effects.

If you are over 65 years of age you may have an increased chance of getting side effects.

Do not be alarmed by the following lists 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 or pharmacist if you notice any of the following and they worry you:

dizziness, light-headedness, and confusion
drowsiness
constipation
vomiting
nausea
unusual tiredness or weakness

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:

difficulty passing urine
decreased frequency of passing urine
dry mouth
sweating
redness of the face
loss of appetite
fainting or feeling weak
slow heart rate
abnormal and fast heart rate
irregular heart beat
feeling light headed when standing up or when getting out of bed
decrease in body temperature
restlessness or nervousness
changes in mood
constriction of pupils
hallucinations
muscle rigidity
severe headache due to increased pressure in the head

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

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

loss of consciousness
difficulty or an inability to breathe properly
severe dizziness, drowsiness or disorientation
symptoms of an allergic reaction (itchy skin rash, skin blisters or discolouration of skin upon exposure to sunlight)

The above list includes very serious side effects. You may need urgent medical attention or hospitalisation.

Tell your doctor if you notice anything that is making you feel unwell.

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

In long-term use, physical dependence and tolerance to the medicine may develop. The following withdrawal symptoms may be experienced after stopping treatment with ENDONE:

nervousness, restlessness, agitation, trouble sleeping or anxiety
body aches, weakness or stomach cramps
loss of appetite, nausea, vomiting or diarrhoea
increased heart rate, breathing rate or pupil size
watery eyes, runny nose, chills or yawning
increased sweating

After using ENDONE

Storage

Keep your tablets in the pack until it is time to take them. If you take the tablets out of the pack, they may not keep as well.

Keep your tablets in a cool, dry place where the temperature stays below 30°C.

Do not store ENDONE or any other medication in the bathroom or near a sink. Do not leave it on a window sill or in the car. Heat and dampness can ruin some medicines.

Keep it where young children cannot reach it. A locked cupboard at least one-and-half-metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking this medicine or the expiry date has passed, ask your pharmacist what to do with any medicine that is left over.

Product description

What it looks like

ENDONE is available in blister packs of 20 tablets.

ENDONE tablets are white and round tablets, with one side embossed "O 5" and a break bar on the other side.

Ingredients

ENDONE contains 5 mg of oxycodone (as oxycodone hydrochloride) as the active ingredient.

The tablets also contain the following inactive ingredients:

lactose
microcrystalline cellulose
stearic acid

ENDONE contains sugars as lactose.

Distributor

ENDONE is distributed in Australia by:

Alphapharm Pty Ltd trading as Viatris
Level 1, 30 The Bond
30-34 Hickson Road
Millers Point NSW 2000
www.viatris.com.au
Phone: 1800 274 276

This leaflet was prepared in September 2023.

Australian registration numbers:
AUST R 14945

ENDONE® is a Viatris company trade mark

endone_cmi\Sep23/00

Published by MIMS November 2023

BRAND INFORMATION

Brand name

Endone

Active ingredient

Oxycodone hydrochloride

Schedule

1 Name of Medicine

Oxycodone hydrochloride.

2 Qualitative and Quantitative Composition

Each Endone tablet contains 5 mg of oxycodone hydrochloride as the active ingredient.

Excipients of known effect.

Sugars as lactose.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Endone tablets are a white, round, biconvex 10 mm tablet with one side embossed "O 5" with a break bar on the other side.

4 Clinical Particulars

4.1 Therapeutic Indications

Endone is indicated for the short-term management of severe pain for which other treatment options have failed, are contraindicated, not tolerated or are otherwise inappropriate to provide sufficient management of pain.

4.2 Dose and Method of Administration

Usual adult dose.

5 mg every six hours, preferably after meals or with milk. Do not divide the tablet.
It may be necessary to increase the usual dose in cases of more severe pain or in those who have become tolerant of narcotics.
In patients with hepatic and renal impairment, dosage should be reduced and adjusted according to the clinical situation (see Section 4.4 Special Warnings and Precautions for Use).

4.3 Contraindications

Hypersensitivity to opiate narcotics, cor pulmonale, cardiac arrhythmias, bronchial asthma, acute alcoholism, brain tumour, head injuries, increased cerebrospinal or intracranial pressure, severe CNS depression, severe respiratory disease, acute respiratory disease and respiratory depression, convulsive disorders, delirium tremens, suspected surgical abdomen and concomitant MAOIs or within 14 days of such therapy.

4.4 Special Warnings and Precautions for Use

Hazardous and harmful use.

Endone contains the opioid oxycodone and is a potential drug of abuse, misuse and addiction. Addiction can occur in patients appropriately prescribed Endone at recommended doses.
The risk of addiction is increased in patients with a personal or family history of substance abuse (including alcohol and prescription and illicit drugs) or mental illness. The risk also increases the longer the drug is used and with higher doses. Patients should be assessed for their risks for opioid abuse or addiction prior to being prescribed Endone.
All patients receiving opioids should be routinely monitored for signs of misuse and abuse. Opioids are sought by people with addiction and may be subject to diversion. Strategies to reduce these risks include prescribing the drug in the smallest appropriate quantity and advising the patient on the safe storage and proper disposal of any unused drugs (see Section 6.4 Special Precautions for Storage; Section 6.6 Special Precautions for Disposal). Caution patients that abuse of oral or transdermal forms of opioids by parenteral administration can result in serious adverse events, which may be fatal.
Patients should be advised not to share Endone with anyone else.

Respiratory depression.

Serious, life-threatening or fatal respiratory depression can occur with the use of opioids even when used as recommended. It can occur at any time during the use of Endone, but the risk is greatest during initiation of therapy or following an increase in dose. Patients should be monitored closely for respiratory depression at these times.
The risk of life-threatening respiratory depression is also higher in elderly, frail or debilitated patients; in patients with existing impairment of respiratory function (e.g. chronic obstructive pulmonary disease; asthma) and in patients with hepatic and renal impairment (see Section 4.4 Special Warnings and Precautions for Use, Use in hepatic and renal impairment). Opioids should be used with caution and with close monitoring in these patients (see Section 4.2 Dose and Method of Administration). The use of opioids is contraindicated in patients with severe respiratory disease, acute respiratory disease and respiratory depression (see Section 4.3 Contraindications).
The risk of respiratory depression is greater with the use of high doses of opioids, especially high potency and modified release formulations, and in opioid-naïve patients. Initiation of opioid treatment should be at the lower end of the dosage recommendations with careful titration of doses to achieve effective pain relief. Careful calculation of equianalgesic doses is required when changing opioids or switching from immediate-release to modified-release formulations, together with consideration of pharmacological differences between opioids. Consider starting the new opioid at a reduced dose to account for individual variation in response.

Risks from concomitant use of benzodiazepines or other CNS depressants, including alcohol.

Concomitant use of opioids and benzodiazepines or other CNS depressants, including alcohol, may result in sedation, respiratory depression, coma and death. Because of these risks, concomitant prescribing of Endone with CNS depressant medicines, such as other opioid analgesics, benzodiazepines, gabapentinoids, cannabis, sedatives, hypnotics, tricyclic antidepressants, antipsychotics, antihistamines, centrally-active anti-emetics and other CNS depressants, should be reserved for patients for whom other treatment options are not possible. If a decision is made to prescribe Endone concomitantly with any of the medicines, the lowest effective dose should be used, and the duration of treatment should be as short as possible. Patients should be followed closely for signs and symptoms of respiratory depression and sedation. Patients and their caregivers should be made aware of these symptoms. Patients and their caregivers should also be informed of the potential harms of consuming alcohol whilst taking Endone.

Use of opioids in chronic (long-term) non-cancer pain (CNCP).

Opioid analgesics have an established role in the treatment of acute pain, cancer pain and palliative and end-of-life care. Current evidence does not generally support opioid analgesics in improving pain and function for most patients with CNCP. The development of tolerance and physical dependence and risks of adverse effects, including hazardous and harmful use, increase with the length of time a patient takes an opioid. The use of opioids for long-term treatment of CNCP is not recommended.
The use of an opioid to treat CNCP should only be considered after maximised non-pharmacological and non-opioid treatments have been tried and found ineffective, not tolerated or otherwise inadequate to provide sufficient management of pain. Opioids should only be prescribed as a component of comprehensive multidisciplinary and multimodal pain management.
Opioid therapy for CNCP should be initiated as a trial in accordance with clinical guidelines and after a comprehensive biopsychosocial assessment has established a cause for the pain and the appropriateness of opioid therapy for the patient (see Hazardous and harmful use). The expected outcome of therapy (pain reduction rather than complete abolition of pain, improved function and quality of life) should be discussed with the patient before commencing opioid treatment, with agreement to discontinue treatment if these objectives are not met.
Owing to the varied response to opioids between individuals, it is recommended that all patients be started at the lowest appropriate dose and titrated to achieve an adequate level of analgesia and functional improvement with minimum adverse reactions. Immediate-release products should not be used to treat chronic pain but may be used for a short period in opioid-naïve patients to develop a level of tolerance before switching to a modified-release formulation. Careful and regular assessment and monitoring is required to establish the clinical need for ongoing treatment. Discontinue opioid therapy if there is no improvement of pain and/or function during the trial period or if there is any evidence of misuse or abuse. Treatment should only continue if the trial has demonstrated that the pain is opioid responsive and there has been functional improvement. The patient's condition should be reviewed regularly, and the dose tapered off slowly if opioid treatment is no longer appropriate (see Ceasing opioids).

Tolerance, dependence and withdrawal.

Neuroadaptation of the opioid receptors to repeated administration of opioids can produce tolerance and physical dependence. Tolerance is the need for increasing doses to maintain analgesia. Tolerance may occur to both the desired and undesired effects of the opioid.
Physical dependence, which can occur after several days to weeks of continued opioid usage, results in withdrawal symptoms if the opioid is ceased abruptly or the dose is significantly reduced. Withdrawal symptoms can also occur following the administration of an opioid antagonist (e.g. naloxone) or partial agonist (e.g. buprenorphine). Withdrawal can result in some or all of the following symptoms: dysphoria, restlessness/agitation, lacrimation, rhinorrhoea, yawning, sweating, chills, myalgia, mydriasis, irritability, anxiety, increasing pain, backache, joint pain, weakness, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhoea, increased blood pressure, increased respiratory rate and increased heart rate.
When discontinuing Endone in a person who may be physically-dependent, the drug should not be ceased abruptly but withdrawn by tapering the dose gradually (see Ceasing opioids; see Section 4.2 Dose and Method of Administration).

Accidental ingestion/exposure.

Accidental ingestion or exposure of Endone, especially by children, can result in a fatal overdose of oxycodone. Patients and their caregivers should be given information on safe storage and disposal of unused Endone (see Section 6.4 Special Precautions for Storage; Section 6.6 Special Precautions for Disposal).

Hyperalgesia.

Hyperalgesia may occur with the use of opioids, particularly at high doses. Hyperalgesia may manifest as an unexplained increase in pain, increased levels of pain with increasing opioid dosages or diffuse sensitivity not associated with the original pain. Hyperalgesia should not be confused with tolerance (see Tolerance, dependence and withdrawal). If opioid induced hyperalgesia is suspected, the dose should be reduced and tapered off if possible. A change to a different opioid may be required.

Ceasing opioids.

Abrupt discontinuation or rapid decreasing of the dose in a person physically dependent on an opioid may result in serious withdrawal symptoms and uncontrolled pain (see Tolerance, dependence and withdrawal above). Such symptoms may lead the patient to seek other sources of licit or illicit opioids. Opioids should not be ceased abruptly in a patient who is physically dependent but withdrawn by tapering the dose slowly. Factors to take into account when deciding how to discontinue or decrease therapy include the dose and duration of the opioid the patient has been taking, the type of pain being treated and the physical and psychological attributes of the patient. A multimodal approach to pain management should be in place before initiating an opioid analgesic taper. During tapering, patients require regular review and support to manage any increase in pain, psychological distress and withdrawal symptoms.
There are no standard tapering schedules suitable for all patients and an individualised plan is necessary. In general, tapering should involve a dose reduction of no more than 10 to 25% every 2 to 4 weeks (see Section 4.2 Dose and Method of Administration). If the patient is experiencing increased pain or serious withdrawal symptoms, it may be necessary to go back to the previous dose until stable before proceeding with a more gradual taper.
When ceasing opioids in a patient who has a suspected opioid use disorder, the need for medication assisted treatment and/or referral to a specialist should be considered.

Other information.

Oxycodone should be used with extreme caution in patients with head injuries and raised intracranial pressure as respiratory depression and ability to increase CSF pressure may be exaggerated, thereby complicating the clinical course.
Administration of oxycodone may result in severe hypotension in patients whose ability to maintain adequate blood pressure is compromised by reduced blood volume, or concurrent administration of such drugs as phenothiazines or certain anaesthetics. Oxycodone may obscure the diagnosis or clinical course of patients with acute abdominal conditions.
Opioid analgesics should be used with caution in patients with myasthenia gravis.
The euphoric activity of opioid compounds has led to their abuse. It should be given with caution or in reduced doses to patients with hypothyroidism, adrenocortical insufficiency, impaired kidney or liver function, prostatic hypertrophy or shock. It should be used with caution in patients with obstructive bowel disorders.

Use in hepatic and renal impairment.

The plasma concentration of oxycodone may be increased in patients with hepatic or renal impairment. Therefore, dosage in such patients should be reduced and adjusted according to the clinical situation.

Use in the elderly.

Oxycodone should be administered with caution, and in reduced dosages, to elderly or debilitated patients.

Paediatric use.

Oxycodone should not be administered to children.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Generally, the effects of oxycodone may be antagonised by acidifying agents and potentiated by alkalising agents.
Concurrent administration of oxycodone with anticholinergic agents may result in an increased risk of severe constipation and/or urinary retention.
Oxycodone may potentiate hypotensive effects when used concurrently with antihypertensive agents, especially ganglionic blockers, leading to increased risk of orthostatic hypotension.
Concurrent use of oxycodone with hydroxyzine or alcohol and CNS depressants (including other opioid agonist analgesics, sedative hypnotics, general anaesthetics, phenothiazines, tricyclic antidepressants, antihistamines, centrally-active anti-emetics, gabapentinoids and cannabis) may result in increased CNS depressant, respiratory depressant and hypotensive effects. Caution is recommended and the dosage of one or both agents should be reduced (see Section 4.4 Special Warnings and Precautions for Use, Risks from concomitant use of benzodiazepines or other CNS depressants, including alcohol).
Mixed agonist/ antagonist analgesics (including pentazocine, butorphanol, buprenorphine) may reduce the analgesic effect of oxycodone and/or may precipitate withdrawal symptoms. Naloxone and naltrexone antagonise the analgesic, CNS and respiratory depressant effects of oxycodone and precipitate withdrawal symptoms. Dosage of the antagonist agents should be carefully titrated when used to treat opioid overdosage in dependent patients.
Oxycodone hydrochloride is metabolised in the intestine and liver to form noroxycodone and oxymorphone via cytochrome P450 isoenzymes of the CYP3A4 and CYP2D6, respectively. Metabolic interactions with drugs that involve the cytochrome P450 enzyme system (CYP3A4, CYP2D6) can cause the plasma concentration of oxycodone to increase. Quinidine, which is a potent CYP2D6 inhibitor, has blocked the formation of oxymorphone, while the oxycodone concentration increased marginally. Concurrent administration of quinidine does not alter the pharmacodynamic effects of oxycodone. The metabolic pathway may be blocked by various drugs (e.g. cimetidine, certain cardiovascular drugs and antidepressants), although such blockade has not yet been shown to be of clinical significance with oxycodone. The potential effects of oxycodone on CYP enzymes have not been studied either in vitro or in vivo.
Oxycodone may antagonise the effects of metoclopramide on gastrointestinal motility.
Oxycodone may enhance the effects of neuromuscular blocking agents resulting in increased respiratory depression.
Nonselective MAOIs (including furazolidone, pargyline and procarbazine) intensify the effects of oxycodone which can cause anxiety, confusion and significant respiratory depression. Oxycodone should not be given to patients taking nonselective MAOIs or within 14 days of stopping such treatment. As it is unknown whether there is an interaction between selective MAOIs (e.g. selegiline) and oxycodone, caution is advised with this drug combination.
Oxycodone may increase the anticoagulant activity of coumarin derivatives.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

Studies have not been performed to assess the effects of oxycodone on fertility.
(Category C)
Reproductive toxicity studies with oxycodone in animals have not been conducted. Opioid analgesics cross the placenta. The use of oxycodone during labour may cause respiratory depression in the newborn infant. Babies born to opioid-dependent mothers may be physically dependent and suffer withdrawal symptoms (convulsions, irritability, excessive crying, tremors, hyperactive reflexes, fever, vomiting, diarrhoea, sneezing and yawning).
Reproductive toxicity studies with oxycodone in animals have not been conducted. Oxycodone is excreted into human milk in low concentrations. Because of the possibility of adverse effects in breastfed infants (sedation, respiratory depression, withdrawal symptoms upon cessation of maternal administration), oxycodone is not recommended for breastfeeding mothers unless the expected benefits outweigh the potential risk.

4.7 Effects on Ability to Drive and Use Machines

Oxycodone may impair the mental and/or physical abilities needed for certain potentially hazardous activities, such as driving a car or operating machinery. Patients should be cautioned accordingly.
This medication may cause drowsiness. Avoid alcohol.

4.8 Adverse Effects (Undesirable Effects)

Adverse drug reactions are typical of full opioid agonists; tolerance (except constipation) generally develops with long-term use. In normal doses, the most common side effects of oxycodone are nausea, vomiting, constipation, drowsiness, unusual tiredness or weakness, vertigo, faintness, light-headedness, orthostatic hypotension and confusion. Less frequent side effects include dry mouth, sweating, facial flushing, nervousness or restlessness. Micturition may be difficult and there may be ureteric or biliary spasm; there is also an anti-diuretic effect. Raised intracranial pressure occurs in some patients. Other uncommon side effects such as bradycardia, supraventricular tachycardia, palpitations, anorexia, changes of mood, respiratory depression, hallucinations have been reported; CNS stimulation, paradoxical and convulsions may occur especially in children. Due to the histamine releasing effect, allergic reactions such as urticaria and pruritus occur in some individuals. Muscle rigidity has been reported following high doses. Larger doses produce respiratory depression and hypotension, with circulatory failure and deepening coma. Convulsions may occur in infants and children. Death may occur from respiratory failure.
In long-term use, physical and psychological dependence and tolerance may develop.
The following withdrawal symptoms may be observed after narcotics are discontinued: body aches, diarrhoea, gooseflesh, loss of appetite, nervousness, restlessness, runny nose, sneezing, tremors or shivering, stomach cramps, nausea, trouble with sleeping, unusual increase in sweating and yawning, weakness, tachycardia and unexplained fever. With appropriate medical use of narcotics and gradual withdrawal from the drug, these symptoms are usually mild.

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 www.tga.gov.au/reporting-problems.

4.9 Overdose

Symptoms.

Toxic doses of opioids vary considerably with the individual and regular users may tolerate large doses. Serious overdosage with oxycodone is characterised by respiratory depression and somnolence progressing to coma and skeletal muscle flaccidity. Toxic leukoencephalopathy has been observed with oxycodone overdose. Cardiac arrest and death may occur. Rhabdomyolysis progressing to renal failure has been reported in opioid overdosage. Pulmonary oedema after overdosage is a common cause of fatalities among opiate addicts.

Treatment.

Primary attention should be given to the re-establishment of adequate respiratory exchange through provision of a patent airway and the institution of assisted or controlled ventilation. The narcotic antagonist naloxone is a specific antidote against respiratory depression which may result from overdosage or unusual sensitivity to narcotics, including oxycodone. Therefore, an appropriate dose of naloxone (usual adult dose: 0.4 mg) should be administered, preferably by the intravenous route, simultaneously with efforts at respiratory resuscitation. Since the duration of action of oxycodone may exceed that of the antagonist, the patient should be kept under continued surveillance and repeated doses of the antagonist should be administered as needed to maintain adequate respiration.
An antagonist should not be administered in the absence of clinically significant respiratory or cardiovascular depression.
Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated. Activated charcoal may be given by mouth in conscious patients if an overdose has been ingested within 1 hour or so.
In an individual physically dependent on narcotics, the administration of the usual dose of a narcotic antagonist will precipitate an acute withdrawal syndrome. The severity of this syndrome will depend on the degree of physical dependence and the dose of antagonist administered. The use of narcotic antagonists in such individuals should be avoided if possible. If a narcotic antagonist must be used to treat serious respiratory depression in the physically dependent patient, only 10 to 20% of the usual initial dose of the antagonist should be administered.
In severe toxicity, the cardiovascular system is usually depressed and requires supportive treatment. If hypotension is due to vasodilatation, plasma expansion, or even vasopressors may be required. Additional measures include support of electrolyte balance, maintenance of normal temperature, catheterisation of the bladder to avoid distension and symptomatic treatment of itching, nausea, vomiting, headache and confusion during the recovery period.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Oxycodone, the principal ingredient, is 14-hydroxydihydrocodeinone, which is derived from the opium alkaloid thebaine. It is a semisynthetic narcotic analgesic with multiple actions qualitatively similar to those of morphine. Oxycodone is an opioid agonist and binds to mu and more weakly to κ- (kappa) and δ- (delta) opioid receptor subtypes. Opioid receptor binding by oxycodone in the central nervous system produces analgesia with some associated sedation. Additional pharmacologically mediated effects of oxycodone involve the CNS, smooth muscle and cardiovascular system.

Clinical trials.

No data available.

5.2 Pharmacokinetic Properties

Absorption.

Oxycodone is absorbed from the gastrointestinal tract.

Distribution.

Following oral administration of Endone, the analgesic effect occurs within 10 to 15 minutes, reaches its maximum in 30 to 60 minutes, and persists for 3 to 6 hours (nontolerant patients only; duration decreases as tolerance develops during chronic therapy).

Metabolism.

It is extensively metabolised to noroxycodone via cytochrome P450 isoenzymes of the CYP3A family and, to a lesser extent, to oxymorphone via CYP2D6.

Excretion.

Oxycodone metabolites undergo glucuronidation and are excreted with unchanged drug in urine. The elimination half-life is reported to be 2 to 4 hours.

5.3 Preclinical Safety Data

Genotoxicity.

Oxycodone was not mutagenic in the Ames Salmonella and Escherichia coli assays; but was positive in the mouse lymphoma assay. In assays of chromosomal damage, genotoxic effects occurred in the human lymphocyte chromosomal aberration assay in vitro, but not in the in vivo bone marrow micronucleus assay in mice.

Carcinogenicity.

Studies of oxycodone in animals to evaluate its carcinogenic potential have not been conducted.

6 Pharmaceutical Particulars

6.1 List of Excipients

Endone tablets also contain stearic acid, microcrystalline cellulose and lactose.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

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

Store below 30°C.

6.5 Nature and Contents of Container

Container type: blister pack (PVC/PVDC/Al).
Pack size: 6, 8, 10, 20 and 500.
Some strengths, pack sizes and/or pack types may not be marketed.

6.6 Special Precautions for Disposal

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

6.7 Physicochemical Properties

Chemical structure.

Oxycodone hydrochloride occurs as white to off-white, odourless, crystals or powder.
Oxycodone 1 g dissolves in 10 mL water. It is sparingly soluble in alcohol and nearly insoluble in ether.
Chemical name: 4,5α-epoxy-14-hydroxy- 3-methoxy-17-methylmorphinan- 6-one hydrochloride.
Molecular formula: C₁₈H₂₁NO₄.HCl.
Molecular weight: 351.9.

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Endone

Oxycodone hydrochloride

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Endone 5 mg