Active ingredients: Oxycodone (Oxycodone hydrochloride)
OxyContin 5 mg, prolonged-release tablets
OxyContin 10 mg, prolonged-release tablets
OxyContin 20 mg, prolonged-release tablets
OxyContin 40 mg, prolonged-release tablets
OxyContin 80 mg, prolonged-release tablets
Why is Oxycontin used? What is it for?
These tablets were prescribed by the doctor to treat severe pain, their effect lasts 12 hours. The tablets contain the active ingredient oxycodone which is a powerful analgesic (pain reliever) belonging to a group of medicines called opioids.
Contraindications When Oxycontin should not be used
Do not take OxyContin if you:
- you are allergic (hypersensitive) to oxycodone or any of the other ingredients of this medicine or if you have had an allergic reaction to another strong analgesic or pain reliever (such as morphine or other opioids) in the past;
- have breathing problems, such as severe chronic obstruction of the lungs, severe bronchial asthma or severe respiratory depression. Symptoms may include shortness of breath, coughing, or breathing slower and weaker than expected;
- have a head injury which causes severe headache or malaise. This is because these tablets can lead to worsening of these symptoms or conceal the severity of the head injury;
- suffer from a condition where your bowels are not functioning well (paralytic ileus), if your stomach empties more slowly than it should (slowed gastric emptying), or if you have sudden severe abdominal pain (acute abdomen);
- have heart problems caused by long-lasting lung disease (cor pulmonale);
Precautions for use What you need to know before taking Oxycontin
Before starting treatment with OxyContin tell your doctor or pharmacist if:
- you are elderly or debilitated;
- have reduced thyroid function (hypothyroidism);
- suffer from myxedema (a thyroid disorder characterized by dryness, coldness and swelling of the skin, affecting the face and legs);
- suffer from severe headache or malaise, which may indicate increased intracranial pressure;
- have low blood pressure (hypotension);
- suffer from mental disorders resulting from an intoxication (toxic psychosis);
- suffer from inflammation of the pancreas (which can cause severe pain in the abdomen or back) or from gallbladder or bile duct disorders;
- suffer from intestinal blockage or intestinal inflammatory disorders;
- suffer from colic-like abdominal pain or discomfort;
- suffer from an enlarged prostate gland which can cause difficulty passing urine (in men);
- have reduced function of the adrenal gland (your adrenal gland does not work as it should), as is the case with Addison's disease;
- have breathing problems such as severe lung function impairment, chronic obstructive airway disorders, severe lung problems or reduced breathing capacity. Symptoms can include shortness of breath and cough;
- have kidney or liver problems;
- suffer from withdrawal symptoms such as agitation, anxiety, palpitations, tremors or sweating that occurred after stopping alcohol or medication;
- suffer from seizures, seizures or convulsions;
- suffer from mental confusion or fainting;
- need to take a higher dose of OxyContin to achieve the same level of pain relief (tolerance);
- has an "increased sensitivity to pain;
- you are taking medicines known as monoamine oxidase inhibitors (such as tranylcypromine, phenelzine, isocarboxiazid, moclobemide and linezolid) or have taken this type of medicine in the last two weeks.
If you are going to have a surgery, please tell your hospital doctor that you are taking these tablets.
The tablets should never be crushed or injected as this can lead to serious side effects which can be fatal.
For those who play sports: the use of the drug without therapeutic need constitutes doping and can in any case determine positive anti-doping tests
Interactions Which drugs or foods can modify the effect of Oxycontin
Tell your doctor or pharmacist if you are taking or have recently taken any other medicines, including medicines obtained without a prescription. If you take these tablets at the same time as certain other medicines, the effect of these tablets or the other medicines may be changed.
Tell your doctor or pharmacist if you are taking:
- some types of antidepressant medicines called monoamine oxidase inhibitors or if you have taken these medicines in the last two weeks (see section 'What you need to know before you take OxyContin').
- medicines to sleep or stay calm (for example tranquilizers, hypnotics or sedatives);
- medicines for depression (for example paroxetine);
- medicines for psychiatric or mental disorders (such as phenothiazines or neuroleptic drugs);
- other powerful analgesics (pain relievers);
- muscle relaxants; high blood pressure medicines;
- quinidine (antiarrhythmic medicine);
- cimetidine (anti-ulcer, indigestion or heartburn medicine);
- medicines to treat fungal infections (such as ketoconazole, voriconazole, itraconazole or posaconazole);
- medicines to treat infections (such as clarithromycin, erythromycin or telithromycin);
- a specific type of medicine known as a protease inhibitor used to treat HIV (such as boceprevir, ritonavir, indinavir, nelfinavir or saquinavir);
- rifampicin for the treatment of tuberculosis;
- carbamazepine (a medicine to treat fits and seizures, seizures and some types of pain);
- phenytoin (a medicine to treat seizures and seizures, convulsions);
- a herbal remedy called "St. John's wort" (also known as Hypericum perforatum)
- antihistamines
- medicines to treat Parkinson's disease
Also tell your doctor if you have recently taken an anesthetic.
OxyContin with food, drink and alcohol
These tablets can be taken with or without food.
Drinking alcohol while taking OxyContin prolonged-release tablets may cause drowsiness or increase the risk of serious side effects such as shortness of breath with the risk of respiratory depression and loss of consciousness. It is recommended not to drink alcohol while taking OxyContin tablets. You should avoid drinking grapefruit juice while being treated with OxyContin.
Warnings It is important to know that:
Pregnancy and breastfeeding
If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.
Pregnancy
You should not take these tablets during pregnancy and labor, unless specifically advised to do so by your doctor. Depending on the dose and duration of oxycodone therapy, slow, shallow breathing (respiratory depression) or withdrawal syndrome may occur in newborns.
Feeding time
These tablets should not be taken during breastfeeding because the active ingredient can pass into breast milk.
Driving and using machines
These tablets can cause a number of side effects, such as sleepiness, which may affect your ability to drive and use machines (see section for full list of side effects). These are usually particularly relevant when starting to for the first time treatment with tablets or when the dose is increased If you feel drowsy you should avoid driving or using machines.
Important information about some of the ingredients of OxyContin
These tablets contain lactose, a sugar. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicinal product.
Dose, Method and Time of Administration How to use Oxycontin: Posology
Always take these tablets exactly as your doctor has told you. The package leaflet of the medicine states how many tablets to take and how often. If in doubt, consult your doctor or pharmacist.
Do not exceed the dose recommended by your doctor.
Take the tablets whole with a glass of water. The tablets should not be chewed, crushed or dissolved.
You must take the tablets every 12 hours. For example, if you take one tablet at 8 am, you should take the next one at 8 pm.
The tablets should not be crushed or injected as this can cause serious, potentially fatal side effects. You should only take the tablets by mouth.
OxyContin tablets are effective for a period of 12 hours when taken whole. If a tablet is broken, crushed, dissolved or chewed, the entire dose covering the 12 hours can be absorbed quickly into your body. This can be dangerous, leading to serious problems such as an overdose which can be fatal.
Adults (20 years and over)
The usual starting dose is one 10 mg tablet every 12 hours. However, your doctor will prescribe the dose required to treat your pain. If you still feel pain despite taking these tablets, discuss this with your doctor.
Children and adults under 20 years old
Children and adults under the age of 20 should not take these tablets.
Patients with kidney or liver problems
Tell your doctor if you have kidney or liver problems so that he can prescribe another medicine or a lower dose depending on your condition.
What to do if you have taken an overdose of
If you take more OxyContin than you should or if someone accidentally swallows the tablets
Contact your doctor or hospital immediately. An overdose can occur with:
- a reduction in the size of the pupils
- breathing slower or weaker than normal (respiratory depression)
- sleepiness or loss of consciousness
- loss of muscle tone (hypotonia)
- reduced heart rate
- decrease in blood pressure
- Difficulty breathing due to fluid in the lungs (pulmonary edema).
In severe cases, an overdose can lead to unconsciousness and even death.When you go to a doctor, take this leaflet and any remaining tablets with you to show the doctor. If you have taken too many tablets, do not put yourself in situations where attention is required, such as driving a car.
If you forget to take OxyContin
If you remember within 4 hours of taking the tablet, take it straight away. Then take the next tablet at the scheduled time. If it has been more than 4 hours since you were due to take the tablet, call your doctor or pharmacist and ask for advice. Do not take a double dose to make up for a forgotten tablet.
If you stop taking OxyContin
You should not abruptly stop taking the tablets unless directed by your doctor. If you want to stop the treatment, please discuss this with your doctor first. Effects. Withdrawal symptoms such as yawning, abnormal dilation of the pupils, watery eyes, runny nose, restlessness, anxiety, convulsions, difficulty sleeping, palpitations, tremors or sweating may occur if you suddenly stop taking these tablets.
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.
Side Effects What are the side effects of Oxycontin
Like all medicines, these tablets can cause side effects, although not everybody gets them.
This medicine can cause allergic reactions, although severe allergic reactions are reported in rare cases. Tell your doctor immediately if you experience sudden wheezing, difficulty breathing, swelling of the eyelids, face or lips, rash or itching, especially if it has spread to the whole body.
The most serious side effect occurs if you breathe more slowly or weakly than expected (respiratory depression - a typical manifestation of opioid overdose).
As with other potent pain relievers or pain relievers, there is a risk of developing physical or psychological dependence on these tablets.
Very common side effects (which may affect more than 1 in 10 patients being treated)
- Constipation (your doctor may prescribe a laxative to remedy this problem).
- Feeling sick or vomiting (they usually tend to subside within a few days, however your doctor may prescribe an anti-emetic medication if the problem persists).
- Somnolence (more easily at the start of treatment or following dose increases, but should resolve spontaneously after a few days).
- Dizziness
- Headache.
- Itching.
Common side effects (which may affect 1 to 10 in 100 patients being treated)
- Dry mouth, loss of appetite, indigestion, abdominal pain or discomfort, diarrhea.
- Confusion, depression, feelings of unusual weakness, tremors, lack of energy, tiredness, anxiety, nervousness, difficulty sleeping, abnormal dreams, abnormal thoughts.
- Wheezing or difficulty in breathing, shortness of breath.
- Difficulty urinating.
- Rash.
- Sweating, increased body temperature.
Uncommon side effects (may affect 1 to 10 in 1,000 patients being treated)
- A condition where you breathe slower or weaker than normal (respiratory depression).
- Difficulty swallowing, belching, hiccups, bloating, a condition where the bowel is not functioning as it should (ileus), inflammation of the stomach, gastrointestinal disturbances (eg stomach upset), taste changes, mouth ulcers, pain in the mouth.
- A condition that causes abnormal antidiuretic hormone production (syndrome of inappropriate antidiuretic hormone secretion).
- Feeling dizzy or lightheaded (vertigo), hallucinations, mood swings, euphoria, agitation, general feeling of being unwell, memory loss, difficulty speaking, reduced sensitivity to pain or touch, tingling or numbness, seizure, seizure or convulsions, abnormal gait, depersonalization, unusual hyperactivity, fainting, decreased consciousness, unusual muscle stiffness or relaxation, involuntary muscle contractions.
- Impotence, decreased desire, low levels of sex hormones in the blood (hypogonadism, which can be seen in blood tests).
- Flushes.
- Dehydration, changes in body weight, thirst, swelling of the hands, ankles or feet.
- Dry skin.
- Disturbances in lacrimation, blurred vision, reduction in the size of the pupils.
- Desire to take higher and higher doses to achieve the same pain-relieving effect (tolerance).
- Auditory perception of rattles or sounds.
- Swelling and irritation inside the nose, nosebleeds, voice changes.
- Chills.
- Chest pain.
- Inability to completely empty the bladder.
- Worsening of liver function tests (to be seen in blood tests).
- Withdrawal symptoms (see section "If you stop taking OxyContin").
Rare side effects (may affect 1 to 10 users in 10,000 being treated)
- A feeling of fainting, especially when standing.
- Low pressure.
- Urticaria.
Frequency not known (frequency cannot be estimated from the available data)
- Sudden wheezing, difficulty in breathing, swelling of the eyelids, face or lips, rash or itching especially when it occurs all over the body.
- Deterioration of the teeth.
- Colic-like abdominal pain or discomfort.
- Blockage of the flow of bile from the liver. This can cause itching, yellow skin, very dark urine, and very pale stools.
- Absence of the menstrual cycle.
- Increased sensitivity to pain.
- Aggression.
- Long-term use of OxyContin during pregnancy can cause life-threatening infant withdrawal syndrome. Symptoms in the infant include irritability, hyperactivity and altered sleep patterns, sharp crying, tremor, malaise, diarrhea and failure to gain weight.
You may see the remnants of the tablets in your stool. This should not affect the effectiveness of the tablet.
Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. Side effects can also be reported directly via the national reporting system at www.aifa.gov.it/responsabili. By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
Keep this medicine out of the sight and reach of children. An accidental overdose in a child is extremely dangerous and life-threatening.
Do not use this medicine after the expiry date which is stated on the blister and carton. The expiry date refers to the last day of that month. For example EXP 08 2020 means that the tablets should not be taken after the last day of August 2020.
Do not store above 25 ° C.
Do not take broken or crushed tablets, as it can be dangerous and cause serious problems such as an overdose.
Do not throw any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. This will help protect the environment.
Contents of the pack and other information
What OxyContin contains
The active ingredient is oxycodone hydrochloride. Each tablet contains 5 mg, 10 mg, 20 mg, 40 mg or 80 mg of oxycodone hydrochloride. The other ingredients are:
- Lactose monohydrate
- Povidone
- Ammoniomethacrylate copolymer in dispersion
- Sorbic acid
- Triacetin
- Stearyl alcohol
- Talc
- Magnesium stearate
- Hypromellose (E464)
- Macrogol titanium dioxide (E171)
In addition, the coating of the tablets contains:
5 mg - brilliant blue (E133)
10 mg - hydroxypropylcellulose
20 mg & 40 mg - polysorbate 80 (E433) and iron oxide (E172)
80 mg - hydroxypropylcellulose, iron oxide (E172) and indigo carmine (E132).
Description of what OxyContin looks like and contents of the pack.
The tablets are printed OC on one side and the dosage on the other (5, 10, etc).
All tablets are round and bi-convex. The 5, 10, 20 and 40 mg tablets are approximately 7 mm in diameter and the 80 mg tablets are approximately 9 mm in diameter. All tablets are coated in the following colors: 5 mg - light blue, 10 mg - white, 20 mg - pink, 40 mg - yellow, 80 mg - green.
The tablets are packaged in blisters and then placed in the boxes. In each pack there are 28 tablets.
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT
OXYCONTIN PROLONGED RELEASE TABLETS
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 5 mg tablet contains 4.5 mg of oxycodone equivalent to 5 mg of oxycodone hydrochloride.
Each 10 mg tablet contains 9.0 mg of oxycodone equivalent to 10 mg of oxycodone hydrochloride.
Each 20 mg tablet contains 18.0 mg of oxycodone equivalent to 20 mg of oxycodone hydrochloride.
Each 40 mg tablet contains 36.0 mg of oxycodone equivalent to 40 mg of oxycodone hydrochloride.
Each 80 mg tablet contains 72.0 mg of oxycodone equivalent to 80 mg of oxycodone hydrochloride.
Excipients:
Each 5 mg tablet contains 77.30 mg of lactose monohydrate
Each 10 mg tablet contains 69.25 mg of lactose monohydrate
Each 20 mg tablet contains 59.25 mg of lactose monohydrate
Each 40 mg tablet contains 35.25 mg of lactose monohydrate
Each 80 mg tablet contains 78.50 mg of lactose monohydrate
For the full list of excipients, see section 6.1.
03.0 PHARMACEUTICAL FORM
Prolonged-release tablets.
Each 5 mg tablet is light blue, round, convex, approximately 7 mm in diameter, with OC imprinted on one side and 5 on the other.
Each 10 mg tablet is white, round, convex, approximately 7 mm in diameter, embossed with OC on one side and 10 on the other.
Each 20 mg tablet is pink, round, convex, approximately 7 mm in diameter, with OC debossed on one side and 20 on the other.
Each 40 mg tablet is yellow, round, convex, approximately 7 mm in diameter, embossed with OC on one side and 40 on the other.
Each 80 mg tablet is green, round, convex, approximately 9 mm in diameter, embossed with OC on one side and 80 on the other.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Treatment of severe pain. OxyContin is indicated in adults aged 20 years and over.
04.2 Posology and method of administration
Dosage
Prescribers should consider concomitant treatment with antiemetics and laxatives for the prevention of nausea, vomiting and constipation.
Adults:
OxyContin tablets are taken at 12 hour intervals. The dosage depends on the intensity of the pain, the patient's need for analgesics in the past, the patient's body weight and sex (plasma concentrations are higher in women).
The usual starting dose for debilitated elderly patients, opioid-naïve patients, or patients with severe pain that cannot be controlled with weaker opioids is 10 mg every 12 hours. Some patients may benefit from a starting dose of 5 mg to minimize the incidence of side effects. To achieve pain relief, the dose should be carefully adjusted as needed every day. Given the time it takes to reach steady state, the Doses should only be adjusted up after 24 hours and, when possible, 25% -50% increments should be made. The correct dosage for each patient is the one that controls pain and is well tolerated over a 12 hour period. need for rescue medication more than twice a day indicates that the dosage of OxyContin tablets should be increased.
Conversion from oral morphine:
In patients treated with oral morphine prior to oxycodone treatment, the daily dose should be calculated based on the following ratio: 10 mg of oral oxycodone is equivalent to 20 mg of oral morphine. It should be emphasized that this report serves as a guide in determining the required dose of OxyContin tablets. Inter-patient variability requires that the dose be carefully adjusted for each patient.
Elderly patients:
Dose adjustment is not usually necessary in elderly patients.
Controlled pharmacokinetic studies in elderly patients (over 65 years) have shown that, compared to younger adults, the clearance of oxycodone is only slightly reduced. No age-dependent adverse drug reactions were observed; therefore, in the elderly, the doses and dosage intervals used for adults are adequate.
Non-malignant pain:
Treatment with oxycodone should be short-lived and not continuous to minimize the risk of addiction. The need for continued treatment should be assessed at regular intervals. Patients usually do not need more than 160 mg per day.
Cancer pain:
In patients, the dose should be adjusted to that which produces pain relief unless this is prevented by the occurrence of uncontrollable adverse drug reactions.
Patients with kidney or liver damage:
Unlike morphine preparations, administration of oxycodone does not produce significant levels of active metabolites. However, in this patient population, the plasma concentration of oxycodone may increase compared to patients with normal renal or hepatic function. The starting dose should be chosen with caution in these patients. The recommended starting dose for adults should be reduced by 50% (e.g. a total oral daily dose of 10 mg in opioid-naive patients) and for each patient the dose should be adjusted to achieve adequate pain control based on the situation. individual clinic.
Pediatric population and adults under 20 years:
Not recommended. Experience in children is limited. Currently available data are described in sections 4.8, 5.1 and 5.2, but no recommendation on a posology can be made.
Method of administration
OxyContin tablets are to be taken orally.
OxyContin tablets must be swallowed whole and must not be broken, chewed or crushed. Taking broken, chewed or crushed OxyContin tablets can lead to rapid release and absorption of a potentially lethal amount of oxycodone.
Missing a dose:
If a patient forgets to take a dose but remembers it within 4 hours of the dose being taken, the tablets can be taken immediately. The next dose should be taken at the usual time. Beyond 4 hours, the prescriber should consider using a rescue medication pending the next dose.
Duration of treatment:
Oxycodone should not be taken for longer than necessary.
Treatment interruption:
When a patient no longer requires oxycodone treatment, it may be appropriate to gradually decrease the dose in order to avoid the occurrence of a withdrawal syndrome.
04.3 Contraindications
Hypersensitivity to oxycodone or to any of the excipients listed in section 6.1.
Oxycodone should not be taken in all situations where opioid drugs are contraindicated: severe respiratory depression with hypoxia, high levels of carbon dioxide in the blood (hypercarbia), head trauma, paralytic ileus, acute abdomen, delayed gastric emptying, obstructive disease severe chronic lung disease, severe bronchial asthma, cor pulmonale, known sensitivity to morphine or other opioids.
04.4 Special warnings and appropriate precautions for use
The greatest risk of opioid excess is respiratory depression.
Caution should be exercised when administering oxycodone to debilitated elderly; to patients with severely impaired lung function, with impaired renal or hepatic function; to patients with myxedema, hypothyroidism, Addison's disease, toxic psychosis, adrenocortical insufficiency, prostatic hypertrophy, head trauma (due to the risk of elevated intracranial pressure), convulsive disorders, delirium tremens, disturbances of consciousness, hypotension, hypovolemia. Use with caution in patients with opioid dependence, biliary tract disease, biliary or renal colic, pancreatitis, obstructive and inflammatory bowel disease, chronic obstructive airway disease, reduced respiratory reserve or alcoholism, or patients taking MAO inhibitors. In patients requiring caution, a reduction in dosage may be advisable.
Doses of OxyContin greater than 60 mg can cause fatal respiratory depression when administered to patients not previously treated with opioids and should only be used in opioid-tolerant patients. Caution should be exercised in prescribing daily oxycodone dosages of 120 mg and above.
Oxycontin tablets should not be used when there is a possibility of paralytic ileus. If paralytic ileus is suspected or occurs during use, administration of OxyContin tablets should be discontinued immediately (see section 4.3). As with all opioid preparations, to relieve pain in patients undergoing treatment. further procedures (surgery, plexus block) oxycodone should not be administered in the 12 hours prior to surgery. If an additional is required
treatment with OxyContin tablets, the dosage should be adjusted according to the subsequent postoperative needs.
As with all opioid preparations, oxycodone products should be used with caution after abdominal surgery, as opioids are known to impair intestinal motility and should not be used until the physician is certain of the presence. of a normal intestinal function.
OxyContin is not recommended for pre-operative use or 12-24 hours after surgery.
The patient on chronic therapy may develop tolerance to the drug and require progressively higher doses to maintain pain control. Prolonged use of the drug can cause physical dependence and a withdrawal syndrome may occur in the event of abrupt discontinuation of therapy. In the event that the patient no longer requires therapy with oxycodone, it is advisable to gradually decrease the dose to prevent withdrawal symptoms Withdrawal symptoms include yawning, mydriasis, lacrimation, runny nose, tremors, hyperhidrosis, anxiety, agitation, seizures, and insomnia.
Hyperalgesia may occur which does not respond to an increase in the oxycodone dose, particularly at high doses. Dose reduction or switching to another opioid may be required.
Oxycodone has a similar abuse profile to other strong opioid agonists.
Oxycodone can be sought and taken for abuse by people with underlying or overt addictive disorders. There is a potential for psychological dependence on opioid analgesics (addiction), including oxycodone. OxyContin tablets should be used with particular care by patients with a history of alcohol and drug abuse.
The prolonged-release tablets must be taken whole, they must not be broken, chewed or crushed. Taking broken, chewed or crushed slow-release oxycodone tablets leads to rapid release and absorption of a life-threatening dose of oxycodone (see section 4.9).
Concomitant use of alcohol and OxyContin may increase the undesirable effects of OxyContin; concomitant use should be avoided.
Abuse of parenterally administered oral pharmaceutical forms can lead to serious adverse events, which can be fatal.
It should be emphasized that once the dose has been adjusted to achieve that for a certain opioid, patients cannot be treated with other analgesic preparations without clinical evaluation and careful dose adjustment if necessary. Otherwise, continuous analgesic action is not ensured.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
It may happen that the empty matrix of the tablets is visible in the stool.
04.5 Interactions with other medicinal products and other forms of interaction
Interaction studies have only been performed in adults.
Potentiation of the CNS depressant effect may occur during concomitant therapy with CNS acting medicinal products such as phenothiazines, antidepressants, anesthetics, hypnotics, sedatives, muscle relaxants, other opioids, neuroleptics, antihypertensives and SSRIs.
Oxycodone should be used with caution and their dosage may need to be reduced in patients using such medicines.
Concomitant use of oxycodone with anticholinergics or drugs with anticholinergic activity (eg tricycyl antidepressants, antihistamines, antipsychotics, muscle relaxants, anti-Parkinson drugs) may result in an increase in anticholinergic side effects. "Oxycodone should be used with caution and the dosage may need to be reduced.
Monoamine oxidase inhibitors are known to interact with narcotic analgesics resulting in excitation or depression associated with hypertensive or hypotensive crisis in the CNS (see section 4.4).
Oxycodone should be used with caution in patients who are taking or have taken MAO inhibitor drugs within the last two weeks (see section 4.4).
Alcohol may enhance the pharmacodynamic effects of OxyContin; concomitant use should be avoided.
Oxycodone is mainly metabolised by cytochrome CYP3A4 and partially by CYP2D6. The activation of these metabolic pathways can be inhibited or induced by the concomitant administration of different drugs or by elements of the diet.
CYP3A4 inhibitors such as macrolide class antibiotics (e.g. clarithromycin, erythromycin and telithromycin), azole antifungals (e.g. ketoconazole, voriconazole, itraconazole and posaconazole), protease inhibitors (e.g. bocepirrevir, ritonavir) indinavir, nelfinavir and saquinavir), cimetidine and grapefruit juice may cause a reduction in the clearance of oxycodone which may result in an increase in its plasma concentration. Therefore, the oxycodone dose may need to be adjusted accordingly.
Here are some examples:
• Itraconazole, a potent CYP3A4 inhibitor, given orally at a dose of 200 mg for five days, increases the AUC of oral oxycodone. On average, the AUC of oxycodone is greater than 2.4 times (range: 1.5 -3.4).
• Voriconazole, a potent CYP3A4 inhibitor, given as 200 mg in two doses daily for four days (400 mg on the first two doses), increases the AUC of oral oxycodone. On average, the AUC of oxycodone is greater than 3. , 6 times (range: 2.7-5.6).
• Telithromycin, a CYP3A4 inhibitor, given orally at a dose of 800 mg for four days, increases the AUC of oral oxycodone. On average, the AUC of oxycodone is 1.8 times higher (range: 1.3- 2.3).
• Grapefruit juice, a CYP3A4 inhibitor, given in the amount of 200 ml for five days, increases the AUC of oral oxycodone. On average, the AUC of oxycodone is greater than 1.7 times (range: 1.1-2 , 1)
CYP3A4 inducers such as rifampicin, carbamazepine, phenytoin and the supplement known as "St. John's wort" may increase the metabolism and clearance of oxycodone, which may result in a decrease in its plasma concentration. The dose of oxycodone may require supplementation. be modified accordingly.
Here are some examples:
• "St. John's wort", a CYP3A4 inducer, given at a dosage of 300 mg three times a day for fifteen days, reduces the AUC of oxycodone. On average, the AUC of oxycodone is reduced by 50% (range: 37% -57%).
• Rifampicin, a CYP3A4 inducer, given at a dose of 600 mg once daily for seven days, reduces the AUC of oral oxycodone. On average, the AUC of oxycodone is reduced by 86%.
Medicinal products that inhibit CYP2D6 activity, such as paroxetine and quinidine, may cause a reduction in the clearance of oxycodone which may lead to an increase in its plasma concentration.
04.6 Pregnancy and lactation
The use of this medicinal product should be avoided as far as possible in pregnant or lactating patients.
Pregnancy
There are limited data from the use of oxycodone in pregnant women. Infants whose mothers have been treated with opioids in the 3-4 weeks prior to delivery should be monitored for respiratory depression. Withdrawal symptoms may be observed in patients. infants whose mothers have been treated with oxycodone.
Oxycodone penetrates the placenta. Oxycodone should not be used during pregnancy and labor as it impairs uterine contractility and the risk of neonatal respiratory depression.
For animal studies, see section 5.3.
Pregnancy
Oxycodone can be secreted into breast milk and can cause respiratory depression in the newborn.
Therefore, oxycodone should not be used in nursing mothers.
Fertility
Non-clinical toxicological studies in rats showed no effect on fertility (see section 5.3).
04.7 Effects on ability to drive and use machines
Oxycodone may affect the ability to drive or use machines. Oxycodone may affect patient reactions to varying degrees depending on individual dosage and sensitivity. Patients experiencing these effects should not drive or operate machinery.
04.8 Undesirable effects
The most commonly observed adverse reactions are nausea and constipation, both occurring in approximately 25-30% of patients. If nausea or vomiting is bothersome, an antiemetic can be associated with oxycodone. As with all strong opioids, constipation must be anticipated and adequately treated with laxatives. If opioid-related adverse events persist, other causes must be sought. .
Adverse reactions are typical of pure opioid agonists and tend to decrease over time, except for constipation. Prediction of adverse drug reactions and adequate patient management can improve acceptability.
The most serious adverse reaction, as with other opioids, is respiratory depression (see section 4.9). This reaction is more likely to occur in the elderly, and in debilitated or opioid intolerant patients.
The table shows the frequency categories used for the classification of undesirable effects:
Tolerance may occur in patients treated with oxycodone, although this was not a major issue during the clinical trial program. Those patients who require a marked increase in dose should undergo a careful evaluation of their pain control regimen.
Pediatric population and adults under 20 years
The frequency, type and severity of adverse reactions in children and adults under 20 years of age are not expected to differ from those seen for adults aged 20 and over.
In the case of neonates of mothers who have taken oxycodone, see section 4.6.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions occurring after authorization of the medicinal product is important as it allows continuous monitoring of the benefit / risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system. "address https://www.aifa.gov.it/content/segnalazioni-reazioni-avverse".
04.9 Overdose
Acute overdose of oxycodone can manifest itself as respiratory depression, somnolence, progression to stupor or coma, hypotonia, miosis, bradycardia, hypotension, pulmonary edema and death.
Treatment of oxycodone overdose
The open airway must be maintained. Pure opioid antagonists, such as naloxone, are specific antidotes against the symptoms of opioid overdose. If necessary, additional measures can be introduced.
In severe overdose, 0.8 mg of naloxone should be administered intravenously. Repeat at 2-3 minute intervals as needed, or by infusing 2 mg in 500 ml of saline or 5% dextrose (0.004 mg / ml).
The rate of the infusion should be adjusted in relation to the previous bolus doses and according to the patient's response. However, since the duration of action of naloxone is relatively short, the patient should be carefully monitored until spontaneous breathing occurs. it is clearly restored. OxyContin tablets continue to release oxycodone and increase the amount of oxycodone for up to 12 hours after administration and the management of oxycodone overdose should be adapted to this.
In the event of a less severe overdose, administer 0.2 mg of naloxone intravenously and, if necessary, continue in increments of 0.1 mg every 2 minutes.
Naloxone should not be administered in the absence of clinically significant respiratory or circulatory depression resulting from oxycodone overdose. Naloxone should be administered with caution to people who are, or are suspected to be, physically dependent on "oxycodone. In these cases," sudden or complete reversal of opioid effects can precipitate pain and an acute withdrawal syndrome.
Gastric contents may need to be emptied as this may be helpful in removing unabsorbed drug, particularly if a sustained release formulation has been taken.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: natural opium alkaloids, opioids, analgesics
ATC code: N02AA05
Oxycodone is a pure opioid agonist with no antagonistic properties and has an affinity for the κ, µ and δ opioid receptors of the brain and spinal cord. The therapeutic effect is mainly analgesic, anxiolytic, antitussive and sedative. The mechanism of action involves CNS opioid receptors for endogenous compounds with opioid-like activity.
Gastrointestinal system
Opioids can cause sphincter of Oddi spasm.
Endocrine system
Opioids can affect the hypothalamus - pituitary - adrenal or gonadal axis. Some changes that may be observed include an increase in serum prolactin and a decrease in plasma cortisol and testosterone. Clinical symptoms may occur from these hormonal changes.
Other pharmacological effects
In vitro and animal studies indicate several effects of natural opioids, such as morphine, on the immune system; the clinical significance of these effects is unknown.
It is not known whether oxycodone, a semi-synthetic opioid, has morphine-like immunological effects.
Pediatric population
Overall safety data obtained for orally administered oxycodone in 9 clinical, pharmacodynamic and pharmacokinetic studies including 629 infants and children (2 months to 17 years) demonstrated that oral oxycodone is well tolerated in pediatric patients with only minor adverse events predominantly on the gastrointestinal and nervous system levels. The positive safety data of oral oxycodone are confirmed by 9 studies performed with oxycodone administered buccally, intramuscularly and intravenously in a total of 1860 infants and children, all of whom experienced only mild adverse events compared to those seen with the use of oral oxycodone.
The parenteral dose of oxycodone to infants and children in clinical trials ranged from 0.025 mg / kg to 0.1 mg / kg; 0.1 mg / kg was the most used dosage followed by 0.05 mg / kg. The dose of oxycodone i.v. it ranged from 0.025 mg / kg to 0.1 mg / kg; 0.1 mg / kg was the most used dosage followed by 0.05 mg / kg. The dose of oxycodone i.m. it ranged from 0.02 mg / kg to 0.1 mg / kg. The orally administered oxycodone dose ranged from 0.1 mg / kg (starting dose) to 1.24 mg / kg / day. The oral dose of oxycodone was 0.1 mg / kg.
Overall, the adverse events of oxycodone in these studies in infants and children appear consistent with the known safety profile of oxycodone, as elaborated on the basis of the numerous clinical studies conducted in adults and described in the Summary of Product Characteristics. No new or unexpected safety signals were identified in these studies. All reported adverse events were consistent with the known safety profile of oxycodone as well as that of other comparable strong opioids. However, OxyContin is not recommended for children and adults under 20 years of age due to insufficient data on safety and efficacy.
05.2 Pharmacokinetic properties
Oxycodone has a "high absolute bioavailability of up to" 87% after oral administration. It has an elimination half-life of approximately 3 hours and is metabolised primarily to noroxycodone via CYP 3A4 and oxymorphone via CYP 2D6. Oxymorphone has some analgesic activity but its plasma concentration is low and therefore it is not believed to contribute to the pharmacological effect of oxycodone.
The release of oxycodone from the Oxycontin tablets occurs in two phases with a relatively fast initial release which produces an early onset of analgesic effect followed by a more controlled release which determines the duration of action of 12 hours.
The apparent mean elimination half-life of Oxycontin tablets is 4.5 hours, which leads to steady state over a period of approximately one day.
The release of oxycodone from Oxycontin tablets is independent of pH.
Oycontin tablets have an oral bioavailability compatible with that of oxycodone administered as a conventional oral pharmaceutical form, but the former reaches maximum plasma concentrations in approximately 3 hours instead of approximately 1 to 1.5. The maximum and minimum concentrations of oxycodone of Oxycontin 10 mg tablets administered at 12 hour intervals are equivalent to those obtained from 5 mg of oxycodone administered as the conventional pharmaceutical form every 6 hours.
All dosages of Oxycontin are bioequivalent in terms of both speed and degree of absorption. Ingestion of a standard high-fat meal does not change the maximum concentration of oxycodone or the extent of absorption of Oxycontin tablets.
Pediatric population
The pharmacokinetic properties of oral oxycodone in infants and children were investigated in 3 studies involving a total population of 63 infants and children aged 0.5 to 7.6 years. In addition, the pharmacokinetics of buccal and sublingual oxycodone were studied in 30 children aged 0.5 to 7.5 years. These studies did not reveal any significant results that differ from adults. Oral oxycodone was well tolerated in these pharmacokinetic studies with only minor adverse events.
05.3 Preclinical safety data
Teratogenicity
Oxycodone showed no effects on fertility or fetal development in rats and rabbits except for doses which resulted in toxic effects in the parents.
Carcinogenicity
No animal studies have been conducted to evaluate the carcinogenic effects of oxycodone.
Mutagenicity
Oxycodone was not mutagenic in bacterial mutation tests or in the in vivo micronucleus assay (s) in mice. As with other opioids, oxycodone was shown to be genotoxic in some in-vitro assays (e.g. mouse lymphoma assay).
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
Lactose monohydrate
Povidone
Ammoniomethacrylate copolymer in dispersion
Sorbic acid
Glycerol triacetate
Stearyl alcohol
Talc
Magnesium stearate
Hypromellose (E464)
Hydroxypropylcellulose (10 mg and 80 mg tablets only)
Titanium dioxide (E171)
Macrogol
Polysorbate 80 (20mg and 40mg tablets only)
Brilliant blue (E133) (5 mg tablets only)
Iron oxide (E 172) (20mg, 40mg and 80mg tablets only)
Indigo carmine (E132) (80 mg tablets only).
06.2 Incompatibility
Not relevant.
06.3 Period of validity
3 years.
06.4 Special precautions for storage
Do not store above 25 ° C.
06.5 Nature of the immediate packaging and contents of the package
Aluminum foil backed PVC blister (containing 10, 28, 30, 56 or 112 tablets).
Only 10 mg, 20 mg, 40 mg and 80 mg
Polypropylene containers with polyethylene lids (containing 28, 56 or 112 tablets).
Not all pack sizes may be marketed.
06.6 Instructions for use and handling
None.
07.0 MARKETING AUTHORIZATION HOLDER
Mundipharma Pharmaceuticals Srl
Via G. Serbelloni 4
20122 Milan
08.0 MARKETING AUTHORIZATION NUMBER
OxyContin 5 mg prolonged release tablets - blister of 10 tablets - AIC 034435255;
OxyContin 5 mg prolonged release tablets - blister of 28 tablets - AIC 034435267;
OxyContin 5 mg prolonged release tablets - blister of 30 tablets - AIC 034435279;
OxyContin 5 mg prolonged release tablets - blister of 56 tablets - AIC 034435281;
OxyContin 5 mg prolonged-release tablets - blister of 112 tablets - AIC 034435293 / M;
OxyContin 10 mg prolonged-release tablets - blister of 28 tablets - AIC 034435014;
OxyContin 10 mg prolonged release tablets - blister of 56 tablets - AIC 034435026 / M;
OxyContin 10 mg prolonged-release tablets - blister of 112 tablets - AIC 034435038;
OxyContin 10 mg prolonged release tablets - bottle of 28 tablets - AIC 034435040;
OxyContin 10 mg prolonged release tablets - bottle of 56 tablets - AIC 034435053;
OxyContin 10 mg prolonged-release tablets - bottle of 112 tablets - AIC 034435065;
OxyContin 20 mg prolonged release tablets - blister of 28 tablets - AIC 034435077;
OxyContin 20 mg prolonged release tablets - blister of 56 tablets - AIC 034435089;
OxyContin 20 mg prolonged-release tablets - blister of 112 tablets - AIC 034435091;
OxyContin 20 mg prolonged release tablets - bottle of 28 tablets - AIC 034435103;
OxyContin 20 mg prolonged release tablets - bottle of 56 tablets - AIC 034435115;
OxyContin 20 mg prolonged release tablets - bottle of 112 tablets - AIC 034435127;
OxyContin 40mg prolonged release tablets - blister of 28 tablets - AIC 034435139;
OxyContin 40mg prolonged release tablets - blister of 56 tablets - AIC 034435141;
OxyContin 40mg prolonged-release tablets - blister of 112 tablets - AIC 034435154;
OxyContin 40mg prolonged release tablets - bottle of 28 tablets - AIC 034435166;
OxyContin 40mg prolonged release tablets - bottle of 56 tablets - AIC 034435178;
OxyContin 40mg prolonged release tablets - bottle of 112 tablets - AIC 034435180
OxyContin 80mg prolonged release tablets - blister of 28 tablets - AIC 034435192;
OxyContin 80mg prolonged release tablets - blister of 56 tablets - AIC 034435204;
OxyContin 80mg prolonged release tablets - blister of 112 tablets - AIC 034435216;
OxyContin 80mg prolonged release tablets - bottle of 28 tablets - AIC 034435228;
OxyContin 80mg prolonged release tablets - bottle of 56 tablets - AIC 034435230;
OxyContin 80mg prolonged release tablets - bottle of 112 tablets - AIC 034435242
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
OxyContin 5 mg
Date of first authorization: June 2007 / Date of last renewal: November 2007
OxyContin 10mg, 20mg, 40mg, 80mg:
Date of first authorization: May 2000 / Date of last renewal: November 2007
10.0 DATE OF REVISION OF THE TEXT
06/2015
