Drug Detail:Oxycontin (Oxycodone [ ox-i-koe-done ])
Drug Class: Opioids (narcotic analgesics)
1. How it works
- OxyContin is a brand (trade name) of controlled-release oxycodone. OxyContin releases oxycodone slowly over 12 hours.
- Oxycodone is a morphine-like, strong pain-relief medicine used for the relief of severe pain that is unresponsive to less potent pain-relief medicines (analgesics). Oxycodone is relatively selective for the mu opioid receptor, although it may bind to other opioid receptors at higher dosages. Oxycodone is a full agonist at the mu receptor (full agonists have a larger effect at higher dosages).
- OxyContin belongs to the group of drugs known as opioids or opioid analgesics. Oxycontin may also be called a narcotic analgesic.
2. Upsides
- May be used to relieve pain that is severe enough to require daily, round-the-clock, opioid-like treatment in people whose pain is not relieved by less potent pain-relief medicines.
- Effective against severe pain including pain caused by cancer.
- OxyContin is long-lasting and only needs to be taken twice a day.
- Less likely to cause an itchy rash compared to other opioid-like medicines, such as morphine.
- Approved for use in adults and pediatric patients aged 11 years and older who have already tolerated immediate-release oxycodone but require around-the-clock pain relief.
- OxyContin has been manufactured in a way that makes it difficult to be misused by drug seekers. The tablet is difficult to crush or break and forms a thick, sticky gel if mixed with water which means it cannot be injected.
- Generic OxyContin is available (the generic name of OxyContin is oxycodone hydrochloride extended-release).
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Sedation, which may impair your reaction skills and affect your ability to drive or operate machinery. Avoid alcohol as the combination can lead to dangerous or fatal side effects.
- Other common side effects include constipation, dizziness, nausea, vomiting, and confusion. Oxycontin can lower blood pressure, which may increase your risk of falling. May also cause flushing, red eyes, sweating, and an itchy rash (although it is less likely than other opioids to cause a rash). OxyContin may also cause insomnia, anxiety, and abnormal dreams. May increase the risk of seizures in people with seizure disorders.
- OxyContin should only be used by people who have already tried and tolerated shorter-acting forms of oxycodone and who have severe pain requiring round-the-clock pain relief. OxyContin should not be taken on an 'as needed' or 'as required' basis.
- OxyContin is habit-forming (addictive), even at prescribed dosages. It has a high abuse potential, and personal legitimate supplies of OxyContin may be sought out by drug seekers.
- Respiratory depression (suppressed breathing), which may be fatal or life-threatening can occur with OxyContin use. The risk is greatest during the first 24 to 72 hours after drug initiation, after a dosage increase, or with overdosage. Children, the elderly, the frail, or those with pre-existing respiratory disease are more at risk.
- It may be difficult for doctors to work out the correct dosage of OxyContin that is needed when transferring from another opioid-like pain medication. OxyContin is best started at a low dosage (10mg twice daily) and titrated up as needed.
- Can interact with grapefruit juice or grapefruit products.
- OxyContin is formulated in a way that deters crushing or chewing; however, if OxyContin is successfully manipulated in this way, it may result in a fatal dose of oxycodone.
- OxyContin is generally not suitable for people with kidney or liver disease.
- OxyContin interacts with several different drugs, including those that inhibit or induce hepatic enzymes, particularly CYP3A4 or CYP2D6 (such as erythromycin, ketoconazole, or ritonavir); depress the CNS (such as benzodiazepines, muscle relaxants, or antipsychotics); have partial agonist or mixed effects on opioid receptors (such as buprenorphine or pentazocine); diuretics; with anticholinergic effects; and monoamine oxidase inhibitors.
- Interaction or overdosage may also cause serotonin syndrome. Symptoms include mental status changes such as agitation, hallucinations, coma, delirium, fast heart rate, dizziness, flushing, muscle tremor or rigidity, and stomach symptoms (including nausea, vomiting, and diarrhea).
- Abrupt discontinuation of Oxycontin in a person who has become physically dependent on it may lead to a withdrawal syndrome and symptoms such as restlessness, pupil dilation, watery eyes and a runny nose, sweating, muscle aches, insomnia, irritability, and gastrointestinal complaints. Babies born to mothers who are physically dependent on OxyContin will also be physically dependent. Do not use during pregnancy unless the benefits outweigh the risks. Breastfeeding is not recommended during treatment with Oxycontin.
- Not for use in patients with severe asthma or other breathing problems, or a blockage in the stomach or intestines.
- Long-term use of OxyContin also affects the endocrine system, which may cause symptoms such as sexual dysfunction, an absence of periods, or infertility.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- OxyContin may be taken with or without food.
- Swallow OxyContin tablets whole, one tablet at a time, with a big glass of water.
- Take OxyContin exactly as directed by your doctor. Do not take more than prescribed unless advised to do so by your doctor. The effective dosage for pain relief varies significantly from person to person. Over time, your dosage may need adjusting, especially if you find that your pain is no longer being controlled. Talk to your doctor if this happens. Also, talk to your doctor regularly about the need for continued treatment with OxyContin.
- Do not cut, break, crush, chew or attempt to dissolve OxyContin as this will impair the controlled-release delivery system and may result in a potentially fatal dose of oxycodone.
- OxyContin may cause sedation which may impair your reaction skills and affect your ability to drive or operate machinery. Do not drive or operate machinery if OxyContin impairs you in this way.
- Do not stop taking OxyContin tablets suddenly as withdrawal symptoms (muscle and bone pain, diarrhea, insomnia, vomiting) may occur. If you need to discontinue this drug, it should be done slowly, and your doctor will explain the tapering schedule to you.
- Avoid alcohol while taking OxyContin, as it may contribute to side effects such as sedation and respiratory depression (impaired breathing).
- If you develop constipation while taking OxyContin, laxatives may help. Antiemetics may be used to treat nausea or vomiting which may occur as a side effect.
- OxyContin may cause your blood pressure to lower when going from a lying down or sitting position to standing. This may be felt as dizziness. Take your time when standing.
- Talk to your doctor if you experience any symptoms such as agitation, hallucinations, fast heart rate, dizziness, flushing, muscle tremor or rigidity, and stomach symptoms (including nausea, vomiting, and diarrhea) while taking OxyContin.
- Avoid grapefruit juice, grapefruit products, Seville oranges (used to make orange marmalade), and tangelos (a tangerine-grapefruit cross) due to possible food-drug interactions.
- Do not use during pregnancy and breastfeeding unless specifically recommended by your doctor.
- Keep this medicine in a safe place and out of the reach of children and pets. Accidental ingestion of even one dose of OxyContin, especially by children, can be fatal.
5. Response and effectiveness
- Peak concentrations of oxycodone are reached within 5 hours. OxyContin is designed to provide delivery of oxycodone over 12 hours. Oxycontin should not be initiated without a trial of shorter-acting oxycodone first.
- Side effects (such as nausea, vomiting, and respiratory depression) are more likely with higher dosages of OxyContin. However, long-term users of OxyContin may develop a tolerance to these effects.
6. Interactions
Medicines that interact with OxyContin may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with OxyContin. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with OxyContin include:
- antibiotics, such as clarithromycin and erythromycin
- antidepressants, such as tricyclic antidepressants (eg, amitriptyline), monoamine oxidase inhibitors (eg, isocarboxazid, phenelzine, and tranylcypromine), or SSRIs (eg, fluoxetine, sertraline)
- antifungal agents, such as itraconazole and ketoconazole
- anticonvulsants, such as carbamazepine, phenytoin, phenobarbital, or primidone
- antipsychotics (such as butyrophenones, phenothiazines, or thioxanthenes) and atypical antipsychotics (eg, olanzapine, quetiapine, ziprasidone)
- any medication that may cause drowsiness, such as benzodiazepines (eg, diazepam, lorazepam), first-generation antihistamines (such as doxylamine or promethazine), metoclopramide, or opioids (such as codeine, morphine)
- buprenorphine
- migraine medications, such as almotriptan, eletriptan, or sumatriptan
- muscle relaxants, such as cyclobenzaprine
- rifampin
- any other medication that inhibits hepatic enzymes CYP3A4 or CYP2D6 or induces CYP3A4.
- other medications that affect serotonin, such as amphetamines, fentanyl, lithium, tramadol, triptans (eg, almotriptan, eletriptan, or sumatriptan), or St. John's Wort.
Avoid grapefruit products and drinking alcohol or taking illegal or recreational drugs while taking OxyContin.
Note that this list is not all-inclusive and includes only common medications that may interact with OxyContin. You should refer to the prescribing information for OxyContin for a complete list of interactions.