Targin

Targin

oxycodone + naloxone

Manufacturer:

Mundipharma

Distributor:

Zuellig
Full Prescribing Info
Contents
Oxycodone hydrochloride, naloxone hydrochloride.
Description
OXYCODONE HCl/NALOXONE HCl (TARGIN) 5 mg/2.5 mg: Each prolonged-release tablet contains 5 mg of oxycodone HCl equivalent to 4.5 mg oxycodone, 2.73 mg of naloxone HCl dihydrate equivalent to 2.5 mg naloxone HCl and 2.25 mg naloxone.
OXYCODONE HCl/NALOXONE HCl (TARGIN) 10 mg/5 mg: Each prolonged-release tablet contains 10 mg of oxycodone HCl equivalent to 9.0 mg oxycodone, 5.45 mg of naloxone HCl dihydrate equivalent to 5.0 mg naloxone HCl and 4.5 mg naloxone.
OXYCODONE HCl/NALOXONE HCl (TARGIN) 20 mg/10 mg: Each prolonged-release tablet contains 20 mg of oxycodone HCl equivalent to 18.0 mg oxycodone, 10.9 mg of naloxone HCl dihydrate equivalent to 10.0 mg naloxone HCl and 9.0 mg naloxone.
OXYCODONE HCl/NALOXONE HCl (TARGIN) 40 mg/20 mg: Each prolonged-release tablet contains 40 mg of oxycodone HCl equivalent to 36.0 mg oxycodone, 21.8 mg of naloxone HCl dihydrate equivalent to 20.0 mg naloxone HCl and 18.0 mg naloxone.
Excipients/Inactive Ingredients: Tablet core: Ethylcellulose N 45, Stearyl alcohol, Lactose monohydrate, Talc, Magnesium stearate, OXYCODONE HCl/NALOXONE HCl (TARGIN) 5 mg/2.5 mg: Hydroxypropylcellulose; OXYCODONE HCl/NALOXONE HCl (TARGIN) 10 mg/5 mg, 20 mg/10 mg, 40 mg/20 mg: Povidone K30.
Tablet coat: Polyvinylalcohol, Titanium dioxide (E171), Macrogol 3350, Talc; OXYCODONE HCl/NALOXONE HCl (TARGIN) 5 mg/2.5 mg: Brilliant Blue FCF aluminium lake (E133), OXYCODONE HCl/NALOXONE HCl (TARGIN) 20 mg/10 mg: Iron oxide red (E172), OXYCODONE HCl/NALOXONE HCl (TARGIN) 40 mg/20 mg: Iron oxide yellow (E172).
Action
Pharmacotherapeutic group: Oxycodone combinations. ATC code: N02AA55.
Pharmacology: Pharmacodynamics: Oxycodone and naloxone have an affinity for kappa, mu and delta opiate receptors in the brain, spinal cord and peripheral organs (e.g. intestine). Oxycodone acts as opioid-receptor agonist at these receptors and affects pain relief by binding to the endogenous opioid receptors in the CNS. By contrast, naloxone is a pure antagonist acting on all types of opioid receptors.
Because of the pronounced first-pass metabolism, the bioavailability of naloxone upon oral administration is <3%, therefore a clinically relevant systemic effect is unlikely. Due to the local competitive antagonism of the opioid receptor mediated oxycodone effect by naloxone in the gut, naloxone reduces the bowel function disorders that are typical for opioid treatment.
In a 12 weeks parallel group double-blinded study in 322 patients with opioid-induced constipation, patients who were treated with oxycodone HCl - naloxone HCl had on average one extra complete spontaneous (without laxatives) bowel movement in the last week of treatment, compared to patients who continued using similar doses of oxycodone HCl prolonged release tablets (p<0.0001). The use of laxatives in the first four weeks was significantly lower in the oxycodone-naloxone group compared to the oxycodone monotherapy group (31% versus 55%, respectively, p<0.0001). Similar results were shown in a study with 265 non-cancer patients comparing daily doses of oxycodone HCl/naloxone HCl of 60 mg/30 mg to up to 80 mg/40 mg with oxycodone HCl monotherapy in the same dose range.
Endocrine System: Opioids can influence the hypothalamic-pituitary-adrenal or gonadal axes. Some changes that can be seen include an increase in serum prolactin, and decreases in plasma cortisol and testosterone in the plasma. Clinical symptoms may be manifest from these hormone changes.
Gastrointestinal System: Opioids may induce spasm of the sphincter of Oddi.
Other Pharmacologic Effects: In vitro and animal studies indicate various effects of natural opioids, such as morphine, on components of the immune system; the clinical significance of these findings is unknown. Whether oxycodone, a semi-synthetic opioid, immunological effects similar to morphine is unknown.
Restless legs syndrome: In a 12-week double-blind efficacy study, 150 patients with severe to very severe idiopathic restless legs syndrome at randomisation were treated with oxycodone HCl/naloxone HCl. Severe syndrome is defined as IRLS score between 21 and 30, and very severe as score between 31 and 40. Patients showed a clinically relevant and a statistically significant improvement in mean IRLS score compared to placebo during the entire treatment period with a decrease in the mean IRLS score of 5.9 points compared to placebo at week 12 (assuming an effect similar to placebo completers for patients who discontinued the study representing a very conservative approach). The onset of efficacy was demonstrated from as early as week 1 of treatment. Similar results were shown for the RLS symptom severity improvement (as measured by the RLS-6-Rating scale), in quality of life as measured by a QoL-RLS questionnaire, in sleep quality (measured by MOS sleep scale), and for the proportion of IRLS score remitters. No subject had a confirmed case of augmentation during the study.
Pharmacokinetics: Oxycodone/naloxone tablets release both components in a controlled manner over a 12-hour period, allowing for twice-daily administration.
Absorption: Oxycodone has a high bioavailability of up to 87% following oral administration.
The prolonged-release tablets release oxycodone such that peak plasma concentrations are generally attained after 3-4 hours. The plasma elimination half-life is approximately 4.5 hours. Food intake has little or no effect on the absorption of oxycodone from oxycodone/naloxone prolonged-release tablets. The absolute bioavailability of oral oxycodone is approximately 50%.
The benefit of naloxone is achieved locally in the GI tract. Following absorption, naloxone is extensively metabolised in the liver and intestine to 6-beta naloxol and the glucuronides of naloxone and 6-beta naloxol. The absolute bioavailability of naloxone following oral administration is approximately 2%, resulting in only negligible systemic concentrations and no significant antagonism of oxycodone's central analgesic effect.
Distribution and Biotransformation: Following absorption, oxycodone is distributed throughout the entire body. Approximately 45% is bound to plasma protein. Oxycodone is metabolised in the liver and intestine via CYP3A4 and CYP2D6 to noroxycodone, oxymorphone and noroxymorphone, which are subsequently glucuronidated. Noroxycodone and noroxymorphone are the major circulating metabolites. Noroxycodone is a weak mu opioid agonist. Noroxymorphone is a potent mu opioid agonist; however, it does not cross the blood-brain barrier to a significant extent. Oxymorphone is a potent mu opioid agonist but is present at very low concentrations following oxycodone administration. None of these metabolites are thought to contribute significantly to the analgesic effect of oxycodone.
Elimination: The centrally active drug, oxycodone and its metabolites are excreted in both urine and feces.
The plasma concentrations of oxycodone and naloxone are only nominally affected by age. As for younger adults the dosage should be adjusted to the intensity of the pain and the sensitivity of the individual patient.
A clinical trial has shown that plasma concentrations of both oxycodone and naloxone are elevated in patients with hepatic impairment. Naloxone concentrations were affected to a higher degree than oxycodone. The clinical relevance of a relative high naloxone exposure in hepatic impaired patients is yet not known. Caution must be exercised when administering oxycodone/naloxone prolonged-release tablets to patients with mild hepatic impairment. In patients with moderate and severe hepatic impairment, the product is contraindicated.
A clinical trial has shown that plasma concentrations of both oxycodone and naloxone are elevated in patients with renal impairment. Naloxone concentrations were affected to a higher degree than oxycodone. The clinical relevance of a relatively high naloxone exposure in renal impaired patients is yet not known. Caution should be exercised when administering oxycodone/naloxone prolonged-release tablets to patients with renal impairment.
Abuse or misuse: To avoid damage to the prolonged-release properties of the tablets, oxycodone/naloxone prolonged-release tablets must not be broken, crushed or chewed, as this leads to a rapid release of the active substances. Parenteral administration of crushed material will lead to a significant systemic exposure of naloxone. In addition, following intranasal administration, effective naloxone (antagonising) plasma concentrations would be maintained over several hours. Both properties act as deterrents of the abuse of oxycodone/naloxone prolonged-release tablets.
Toxicology: Preclinical safety information: There are no preclinical data pertaining to the genotoxicity/carcinogenicity/reproductive toxicity of the combination of oxycodone and naloxone at the 2:1 ratio. The data presented here are for studies with the single compounds.
Genotoxicity: Oxycodone and naloxone were each tested as single entities in in vitro and in vivo genotoxicity studies. The results from in vitro clastogenicity assays were equivocal, but neither oxycodone nor naloxone were mutagenic in the in vitro bacterial mutagenicity assay. However, when evaluated in vivo, oxycodone and naloxone were not genotoxic in the mouse bone marrow micronucleus test even at doses that caused significant adverse effects. The weight of evidence indicates that the combination of oxycodone and naloxone poses minimal if any risk for human genotoxicity at systemic concentrations that are achieved therapeutically.
Carcinogenicity: Long-term carcinogenicity studies with oxycodone/naloxone in combination or oxycodone as a single entity have not been performed.
For naloxone, a 24-month oral carcinogenicity study was performed in rats with doses up to 100 mg/kg/day and a 6 month carcinogenicity study was performed in TgrasH2 mice at doses up to 200 mg/kg/day. The results of the two studies indicate that naloxone was not carcinogenic under these conditions.
Reproductive and Developmental Toxicity: Oxycodone and naloxone were not teratogenic, even at maternally toxic doses in rats and rabbits. Oxycodone and naloxone did not affect fertility, reproductive performance or adversely affect long-term development of pups (F1 generation) born to rats treated with oxycodone during late pregnancy and lactation, with the exception of decreased body weights noted at doses associated with maternal toxicity. Moreover, neither oxycodone nor naloxone exhibited any developmental effects on pups born to the F1 generation females.
Indications/Uses
Management of moderate to severe chronic pain unresponsive to non-narcotic analgesia. The naloxone component in a fixed combination with oxycodone is indicated for the therapy and/or prophylaxis of opioid-induced constipation.
Second line symptomatic treatment of patients with severe to very severe idiopathic restless legs syndrome after failure of dopaminergic therapy.
The opioid antagonist naloxone counteracts opioid induced constipation by blocking the action of oxycodone at opioid receptors locally in the gut.
Dosage/Direction for Use
Analgesia: The analgesic efficacy of OXYCODONE HCl/NALOXONE HCl (TARGIN) is equivalent to oxycodone HCl prolonged-release formulations.
The dosage should be adjusted to the intensity of pain and the sensitivity of the individual patient. Unless otherwise prescribed, OXYCODONE HCl/NALOXONE HCl (TARGIN) should be administered as follows: Adults: The usual starting dose for an opioid naive patient is 10 mg/5 mg of oxycodone HCl/naloxone HCl at 12 hourly intervals.
Lower strengths are available to facilitate dose titration when initiating opioid therapy and for individual dose adjustment.
OXYCODONE HCl/NALOXONE HCl (TARGIN) 5 mg/2.5 mg is available to facilitate dose titration when initiating opioid therapy and for individual dose adjustment.
Patients already receiving opioids may be started on higher doses of OXYCODONE HCl/NALOXONE HCl (TARGIN) depending on their previous opioid experience.
After complete discontinuation of therapy with OXYCODONE HCl/NALOXONE HCl (TARGIN) with a subsequent switch to another opioid a worsening of the bowel function can be expected.
Some patients taking OXYCODONE HCl/NALOXONE HCl (TARGIN) according to a regular time schedule require immediate-release analgesics as "rescue" medication for breakthrough pain. OXYCODONE HCl/NALOXONE HCl (TARGIN) is a prolonged-release formulation and therefore not intended for the treatment of breakthrough pain. For the treatment of breakthrough pain, a single dose of "rescue medication" should approximate one sixth of the equivalent daily dose of oxycodone HCl. The need for more than two "rescues" per day is usually an indication that the dose of OXYCODONE HCl/NALOXONE HCl (TARGIN) requires upward adjustment. This adjustment should be made every 1-2 days in steps of 5 mg/2.5 mg twice daily, or where necessary 10 mg/5 mg, oxycodone HCl/naloxone HCl until a stable dose is reached. The aim is to establish a patient-specific twice daily dose that will maintain adequate analgesia and make use of as little rescue medication as possible for as long as pain therapy is necessary.
The maximum daily dose of OXYCODONE HCl/NALOXONE HCl (TARGIN) is 160 mg oxycodone hydrochloride and 80 mg naloxone hydrochloride. The maximum daily dose is reserved for patients who have previously been maintained on a stable daily dose of OXYCODONE HCl/NALOXONE HCl (TARGIN) and who have become in need of an increased dose. Special attention should be given to patients with compromised renal function and patients with mild hepatic impairment if an increased dose is considered. For patients requiring higher doses of OXYCODONE HCl/NALOXONE HCl (TARGIN), administration of supplemental oxycodone hydrochloride prolonged-release at the same time intervals should be considered, taking into account the maximum daily dose of 400 mg prolonged-release oxycodone hydrochloride. In the case of supplemental oxycodone hydrochloride dosing, the beneficial effect of naloxone hydrochloride on bowel function may be impaired.
OXYCODONE HCl/NALOXONE HCl (TARGIN) is taken at the determined dosage twice daily according to a fixed time schedule. While symmetric administration (the same dose mornings and evenings) subject to a fixed time schedule (every 12 hours) is appropriate for the majority of patients, some patients, depending on the individual pain situation, may benefit from asymmetric dosing tailored to their pain pattern. In general, the lowest effective analgesic dose should be selected.
In non-malignant pain therapy, daily doses of up to 40 mg/20 mg oxycodone HCl/naloxone HCl are usually sufficient, but higher doses may be needed.
Restless legs syndrome (RLS): OXYCODONE HCl/NALOXONE HCl (TARGIN) is indicated for patients suffering from RLS for at least 6 months. RLS symptoms should be present daily and during daytime (≥4 days/week). OXYCODONE HCl/NALOXONE HCl (TARGIN) should be used after failure of previous dopaminergic treatment. Dopaminergic treatment failure is defined as inadequate initial response, a response that has become inadequate with time, occurrence of augmentation or unacceptable tolerability despite adequate doses. Previous treatment with at least one dopaminergic medicinal product should have lasted in general 4 weeks. A shorter period might be acceptable in case of unacceptable tolerability with dopaminergic therapy.
The dosage should be adjusted to the sensitivity of the individual patient.
Treatment of patients with restless legs syndrome with OXYCODONE HCl/NALOXONE HCl (TARGIN) should be under the supervision of a clinician with experience in the management of restless legs syndrome.
Unless otherwise prescribed, OXYCODONE HCl/NALOXONE HCl (TARGIN) should be administered as follows: Adults: The usual starting dose for is 5 mg/2.5 mg of oxycodone HCl/naloxone HCl at 12 hourly intervals.
Titration on a weekly basis is recommended in case higher doses are required. The mean daily dose in the pivotal study was 20 mg/10 mg oxycodone HCl/naloxone HCl. Some patients may benefit from higher daily doses up to a maximum of 60 mg/30 mg oxycodone HCl/naloxone HCl.
OXYCODONE HCl/NALOXONE HCl (TARGIN) is taken at the determined dosage twice daily according to a fixed time schedule. While symmetric administration (the same dose mornings and evenings) subject to a fixed time schedule (every 12 hours) is appropriate for the majority of patients, some patients, depending on the individual situation, may benefit from asymmetric dosing tailored to the individual patient. In general, the lowest effective dose should be selected.
For doses not realisable/practicable with this strength other strengths of this medicinal product are available.
Analgesia/Restless legs syndrome: Pediatric population: The safety and efficacy of OXYCODONE HCl/NALOXONE HCl (TARGIN) in children aged below 18 years has not been established. No data are available.
Elderly patients: As for younger adults the dosage should be adjusted to the intensity of the pain or RLS symptoms and the sensitivity of the individual patient.
Patients with impaired hepatic function: A clinical trial has shown that plasma concentrations of both oxycodone and naloxone are elevated in patients with hepatic impairment. Naloxone concentrations were affected to a higher degree than oxycodone (see Pharmacology: Pharmacokinetics under Actions). The clinical relevance of a relative high naloxone exposure in hepatic impaired patients is yet not known. Caution must be exercised when administering OXYCODONE HCl/NALOXONE HCl (TARGIN) to patients with mild hepatic impairment (see Precautions). In patients with moderate and severe hepatic impairment OXYCODONE HCl/NALOXONE HCl (TARGIN) is contraindicated (see Contraindications).
Patients with impaired renal function: A clinical trial has shown that plasma concentrations of both oxycodone and naloxone are elevated in patients with renal impairment (see Pharmacology: Pharmacokinetics under Actions). Naloxone concentrations were affected to a higher degree than oxycodone. The clinical relevance of a relative high naloxone exposure in renal impaired patients is yet not known. Caution should be exercised when administering OXYCODONE HCl/NALOXONE HCl (TARGIN) to patients with renal impairment (see Precautions).
Method of administration: To be taken by mouth every 12 hours. The tablets must be swallowed whole, and not broken, chewed or crushed.
Duration of use: OXYCODONE HCl/NALOXONE HCl (TARGIN) should not be administered for longer than absolutely necessary. If long-term treatment is necessary in view of the nature and severity of the illness, careful and regular monitoring is required to establish whether and to what extent further treatment is necessary.
Analgesia: When patient no longer requires opioid therapy, it may be advisable to taper the dose gradually (see Precautions).
Restless legs syndrome: At least every three months during therapy with OXYCODONE HCl/NALOXONE HCl (TARGIN) patients should be clinically evaluated. Treatment should only be continued if OXYCODONE HCl/NALOXONE HCl (TARGIN) is considered effective and the benefit is considered to outweigh adverse effects and potential harms in individual patients. Prior to continuation of RLS treatment beyond 1 year a discharge regimen by gradually tapering down of OXYCODONE HCl/NALOXONE HCl (TARGIN) over a period of approximately one week should be considered to establish if continued treatment with OXYCODONE HCl/NALOXONE HCl (TARGIN) is indicated.
When the patient no longer requires opioid therapy, tapering down over a period of approximately one week is recommended in order to reduce the risk of a withdrawal reaction (see Precautions).
Overdosage
Symptoms of intoxication: Depending on the history of the patient, an overdose of OXYCODONE HCl/NALOXONE HCl (TARGIN) may be manifested by symptoms that are either triggered by oxycodone (opioid receptor agonist) or by naloxone (opioid receptor antagonist).
Acute overdose with oxycodone can be manifested by respiratory depression, somnolence progressing to stupor or coma, hypotonia, miosis, bradycardia, hypotension and death.
Symptoms of a naloxone overdose alone are unlikely. Withdrawal symptoms due to an overdose of naloxone should be treated symptomatically in a closely-supervised environment.
Therapy of intoxication: A patient airway must be maintained. The pure opioid antagonists such as naloxone are specific antidotes against symptoms from opioid overdose. Other supportive measures should be employed as needed.
Contraindications
Known hypersensitivity to oxycodone and naloxone or to any of the excipients listed in Description.
Severe chronic obstructive lung disease.
Cor pulmonale.
Severe bronchial asthma.
Severe respiratory depression with hypoxia and/or hypercapnia.
Non-opioid induced paralytic ileus.
Special Precautions
The major risk from opioids is respiratory depression.
Caution must be exercised when administering OXYCODONE HCl/NALOXONE HCl (TARGIN) to the debilitated elderly.
Oxycodone/naloxone has to be administered with caution in patients with: severely impaired pulmonary function; renal impairment; mild hepatic impairment; opioid-induced paralytic ileus; myxedema; hypothyroidism; Addison's disease; prostate hypertrophy; toxic psychosis; alcoholism; delirium tremens; pancreatitis; hypotension; head injury (due to risk of increased intracranial pressure); or patients taking MAO inhibitors.
Caution must also be exercised when administering OXYCODONE HCl/NALOXONE HCl (TARGIN) to patients with mild hepatic or renal impairment. A careful medical monitoring is particularly necessary for patients with severe renal impairment.
In patients under long-term opioid treatment with higher doses of opioids, the switch to OXYCODONE HCl/NALOXONE HCl (TARGIN) may initially provoke withdrawal symptoms or diarrhea.
OXYCODONE HCl/NALOXONE HCl (TARGIN) is not suitable for the treatment of withdrawal symptoms.
The patient may develop tolerance to the drug with chronic use and require progressively higher doses to maintain pain control. Prolonged use of OXYCODONE HCl/NALOXONE HCl (TARGIN) may lead to physical dependence and a withdrawal syndrome may occur upon abrupt cessation of therapy. When a patient no longer requires therapy with OXYCODONE HCl/NALOXONE HCl (TARGIN), it may be advisable to taper the dose gradually to prevent symptoms of withdrawal.
Oxycodone has an abuse profile similar to other strong agonist opioids. Oxycodone may be sought and abused by people with latent or manifest addiction disorders. There is potential for development of psychological dependence (addiction) to opioid analgesics, including oxycodone. OXYCODONE HCl/NALOXONE HCl (TARGIN) should be used with particular care in patients with a history of alcohol and drug abuse.
The controlled release tablets must be swallowed whole, and not broken, chewed or crushed. The administration of broken chewed or crushed controlled release oxycodone/naloxone tablets leads to a rapid release and absorption of a potentially fatal dose of oxycodone (see Overdosage).
If abused by individuals dependent on opioid agonists such as heroin, morphine, or methadone, OXYCODONE HCl/NALOXONE HCl (TARGIN) is expected to produce marked withdrawal symptoms - because of the opioid receptor antagonist characteristics of naloxone - or to intensify withdrawal symptoms already present (see Overdosage).
Abuse of oral dosage forms by parenteral administration can be expected to result in serious adverse events, which may be fatal.
OXYCODONE HCl/NALOXONE HCl (TARGIN) is not recommended for pre-operative use or within the first 12-24 hours post-operatively.
Caution is advised in treating restless legs syndrome patients with additional sleep apnea syndrome with OXYCODONE HCl/NALOXONE HCl (TARGIN) due to the additive risk of respiratory depression. No data about the risk exist because in the clinical trial patients with sleep apnea syndrome were excluded.
There is no clinical experience with OXYCODONE HCl/NALOXONE HCl (TARGIN) in the long-term treatment of RLS beyond 1 year (see Dosage & Administration).
Studies have not been performed on the safety and efficacy of OXYCODONE HCl/NALOXONE HCl (TARGIN) in children and adolescents below the age of 18 years. Therefore, their use in children and adolescents under 18 years of age is not recommended.
There is no clinical experience in patients with cancer associated to peritoneal carcinomatosis or with sub-occlusive syndrome in advanced stages of digestive and pelvic cancers. Therefore, the use of OXYCODONE HCl/NALOXONE HCl (TARGIN) in this population is not recommended. The empty prolonged-release tablet matrix may be visible in the stool.
The use of OXYCODONE HCl/NALOXONE HCl (TARGIN) may produce positive results in doping controls.
The use of OXYCODONE HCl/NALOXONE HCl (TARGIN) as a doping agent may become a health hazard.
This medicinal product contains lactose. Patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take OXYCODONE HCl/NALOXONE HCl (TARGIN).
Effects on ability to drive and use machines: Oxycodone may impair the ability to drive and use machines.
Use In Pregnancy & Lactation
Use of this medicinal product should be avoided to the extent possible in patients who are pregnant or lactating.
Both oxycodone and naloxone pass into the placenta. Prolonged use of oxycodone during pregnancy can result in neonatal opioid withdrawal syndrome.
Oxycodone passes into the breast milk. It has not been established whether naloxone also passes into the breast milk.
Adverse Reactions
The following frequencies are the basis for assessing undesirable effects: 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).
The undesirable effects listed as follows are classified by body system according to their incidence (common or uncommon). Common adverse drug reactions have an incidence of ≥1% and uncommon adverse drug reactions have an incidence of <1%. (See Table 1.)

Click on icon to see table/diagram/image

For the active substance oxycodone, the following additional undesirable effects are known: See Table 2.

Click on icon to see table/diagram/image
Drug Interactions
There can be an enhanced CNS-depressant effect during concomitant therapy with drugs which affect CNS such as alcohol, other opioids, sedatives, hypnotics, anti-depressants, phenothiazines, neuroleptics etc.
Concomitant administration of oxycodone with anticholinergics or medications with anticholinergic activity (e.g. tricyclic antidepressants, antihistamines, antipsychotics, muscle relaxants, anti-Parkinson drugs) may result in increased anticholinergic adverse effects.
Oxycodone is metabolised primarily via the CYP3A4 and partly via the CYP2D6 pathways. The activities of these metabolic pathways may be inhibited or induced by various co-administered drugs or dietary elements. OXYCODONE HCl/NALOXONE HCl (TARGIN) doses may need to be adjusted accordingly.
CYP3A4 inhibitors, such as macrolide antibiotics (e.g. clarithromycin), azole-antifungal agents (e.g. ketoconazole), protease inhibitors (e.g. ritonavir), and grapefruit juice may cause decreased clearance of oxycodone which could lead to an increase in oxycodone plasma concentrations.
CYP3A4 inducers, such as rifampin, carbamazepine, phenytoin and St. John's wort, may induce the metabolism of oxycodone and cause increased clearance of the drug, resulting in a decrease in oxycodone plasma concentrations.
Drugs that inhibit CYP2D6 activity, such as paroxetine and quinidine, may cause decreased clearance of oxycodone which could lead to an increase in oxycodone plasma concentrations.
Caution For Usage
Incompatibilities: Not applicable.
Special precautions for disposal: Any unused product or waste material should be disposed of in accordance with local requirements.
Storage
Do not store above 30°C.
Shelf life: 3 years.
MIMS Class
ATC Classification
N02AA55 - oxycodone and naloxone ; Belongs to the class of natural opium alkaloids. Used to relieve pain.
Presentation/Packing
PR tab 5 mg/2.5 mg (capsule shaped biconvex, blue, film-coated, approximately 9.5 mm long, marked "OXN" on one side and "5" on the other side) x 28's. 10 mg/5 mg (capsule shaped biconvex, white, film-coated, approximately 9.5 mm long, marked "OXN" on one side and "10" on the other side) x 28's. 20 mg/10 mg (capsule shaped biconvex, pink, film-coated, approximately 9.5 mm long, marked "OXN" on one side and "20" on the other side) x 28's. 40 mg/20 mg (capsule shaped biconvex, yellow, film-coated, approximately 14 mm long marked "OXN" on one side and "40" on the other side) x 28's.
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