How Common Is Oxycodone Abuse?

Oxycodone hydrochloride sustained-release tablets are indicated for the relief of persistent moderate to severe pain.

Oxycodone hydrochloride sustained-release tablets are indicated for the relief of persistent moderate to severe pain.

Drug Name

Oxycodone hydrochloride sustained-release tablets

Drug type

prescription

Special medicine

Narcotic drugs, stimulants

Use classification

Analgesics

Ingredients of oxycodone hydrochloride sustained-release tablets

The active ingredient of this product is oxycodone hydrochloride.
Chemical name: 4,5-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one hydrochloride.
Chemical Structure:

Molecular formula: C _l8 H ₂₁ N0 ₄ · HCl
Molecular weight: 351.83

Properties of Oxycodone Hydrochloride Sustained Release Tablets

This product is a round, biconvex film-coated tablet. One side is marked with OC, and the other side is marked with oxycodone hydrochloride specifications (ie: 5, 10, 20, 40) according to different specifications.
5mg is a light blue tablet; 10mg is a white tablet;
20mg is a pale red tablet; 40mg is a yellow tablet.

Indications of oxycodone hydrochloride sustained-release tablets

Used to relieve persistent moderate to severe pain.

Specification of oxycodone hydrochloride sustained-release tablets

(1) 5mg (2) 10mg (3) 20mg (4) 40mg

Oxycodone hydrochloride sustained-release tablets

It must be swallowed whole, not split, chewed, or ground. If broken, chewed, or ground, tablets can result in rapid release of oxycodone and absorption of potentially lethal amounts.
Every 12 hours, the dosage depends on the patient's pain severity and previous analgesic history.
The degree of pain increases, and the dose needs to be increased to achieve pain relief. For all patients, the proper dose is 12 hours of pain control and the patient is well tolerated. In addition to the effects of difficult to control adverse reactions, titration should be given to patients for pain relief. When the need to detach from the dosing regimen (when breakthrough pain is treated with an immediate release analgesic) exceeds 2 times a day, it is indicated that the dosage of the drug should be increased. The magnitude of each dose adjustment is increased by 25-50% based on the previous dose.
For patients with moderate to severe pain who cannot take pain for the first time with opioids or with weak opioids, the initial dose is generally 5 mg, and it is taken every 12 hours. Then, carefully titrate the dose according to the condition until the ideal pain relief. The maximum dose for most patients is 200 mg / 12 h, and a few patients may require higher doses. So far, the highest clinically reported dose for individuals has been 520mg / 12h.
Patients who have been treated with oral morphine switch to the daily dose conversion ratio of this product: 10 mg of this product is equivalent to 20 mg of oral morphine.
Due to individual differences, the dosage should be titrated according to the individual circumstances of the patient.

Adverse reactions of oxycodone hydrochloride sustained-release tablets

Adverse effects of opioid agonists may occur. Tolerance and dependence may develop.
Common adverse reactions: constipation (laxatives can prevent constipation), nausea, vomiting, dizziness, itching, headache, dry mouth, sweating, sleepiness and fatigue. If nausea and vomiting occur, antiemetics can be used.
Occasional adverse reactions: anorexia, nervousness, insomnia, fever, insanity, diarrhea, abdominal pain, vasodilation, indigestion, paresthesia, rash, anxiety, euphoria, depression, dyspnea, hypotension, chills, nightmares, Thinking abnormally, hiccups.
Rare adverse reactions: dizziness, convulsions, gastritis, disorientation, flushing, mood changes, palpitations (in the case of withdrawal syndrome), hallucinations, bronchospasm, difficulty swallowing, belching, flatulence, intestinal obstruction, abnormal taste, Agitation, forgetting, hypertension, hyperalgesia, hypotension, discomfort, involuntary muscle contraction, speech disturbance, tremor, visual abnormalities, withdrawal syndrome, amenorrhea, hyposexuality, impotence, hypotension, supraventricular tachycardia Tachycardia, syncope, dehydration, edema, peripheral edema, thirst, dry skin, urticaria, allergies, allergic reactions, allergic reactions, dilated pupils and colic. Dysuria, biliary tract; cramps or ureteral cramps may occur.
Respiratory depression may occur with overdose.

Contraindications of oxycodone hydrochloride sustained-release tablets

Hypoxic respiratory depression, craniocerebral injury, paralytic intestinal obstruction, acute abdomen, delayed gastric emptying, chronic obstructive respiratory disease, pulmonary heart disease, acute or severe bronchial asthma, hypercapnia, known to Oxycodone allergy, moderate to severe liver dysfunction, severe renal dysfunction (creatinine clearance [10ml / min), chronic constipation, taking monoamine oxidase inhibitor at the same time, discontinuing monoamine oxidase inhibitor [2 weeks. Banned for pregnant or lactating women. It should not be used before surgery or within 24 hours after surgery.

Precautions for oxycodone hydrochloride sustained-release tablets

This product is administered in accordance with narcotic drugs. When used in the treatment of non-cancer chronic pain, the provisions of the "Guiding Principles of Strong Opioids in the Treatment of Chronic Non-Cancer Pain" should be followed.
caveat:
Misuse, abuse and abuse of opioids <br /> Oxycodone is a morphine opioid agonist, and this type of drug may be a target for drug abusers and drug addicts.
Oxycodone is abused similarly to other opioid agonists and can be legal or illegal. When a physician prescribes or a pharmacist issues medication, consider whether it increases the risk of misuse, abuse, or abuse.
It has been reported that OxyContin can be abused by crushing, chewing, inhaling or injecting a solution that dissolves this product. These practices can lead to uncontrolled release of opioids, posing a greater danger to abusers, and may lead to Overdose and death.
However, concerns about abuse, addiction and abuse do not prevent the rational use of these drugs in analgesic treatments.
Medical personnel should strictly abide by relevant national regulations in use.
Interactions with Alcohol and Substances of Abuse < br Oxycodone may have an additive effect when it is used with alcohol, other opioids, or other illegal drugs that inhibit the central nervous system.
Drug abuse and addiction Oxycodone contained in OxyContin is a "full opiate agonist with a similar tendency to abuse as morphine. It is a narcotic analgesic. It is the same as morphine and other analgesics. Like opioids, oxycodone has the potential for abuse and illegal abuse.
Drug addiction is characterized by forced use, non-medical use, and continued use regardless of whether it is harmful or dangerous. After using opioids (including oxycodone), there is the possibility of developing a drug addiction. Drug addiction is treatable using a multidisciplinary approach, but relapses are also more common.
"Drug-seeking" behavior is common in patients with drug addiction and abuse. Common practices for drug seekers include making emergency phone calls or seeking medical treatment close to off hours-refusing normal inspections, tests or referrals, often "losing" prescriptions; tampering with prescriptions; unwillingness to provide previous medical records or contact with other therapists the way. "Getting around" to get more prescriptions is a common method for drug abusers and untreated addicts.
Abuse and addiction are different concepts and are not the same as physical dependence and tolerance. Not all addicts have symptoms of tolerance and physical dependence at the same time. In addition, opioid abuse can occur without real addiction, and is characterized by misuse for non-medical purposes, often in combination with other antipsychotic drugs. Therefore, it is strongly recommended that doctors strictly follow relevant regulations when prescribing drugs.
Measures such as reasonable assessment of patients, reasonable prescription, regular re-evaluation of treatment, reasonable drug distribution and storage are all beneficial measures to limit the abuse of opioids.
OxyContin consists of a binary polymer matrix for oral use only. The abuse of crushed tablets can cause overdose and the risk of death, and the abuse of alcohol and other drugs can increase this risk. If this product is abused by parenteral route of administration, the excipient ingredients (especially talc) in the tablet may cause local tissue necrosis, infection, pulmonary granulomas, and increase endocarditis and heart valve damage risks of. Drug abuse for parenteral administration is also often associated with the spread of infectious diseases such as hepatitis and HIV.
In the correct treatment of pain patients, reports of psychological dependence on opioid analgesics are rare. However, data on psychological dependence in patients with chronic pain are lacking.
Respiratory depression < br Respiratory depression is the main harmful effect of the active ingredient oxycodone (and all opioid agonists) in OxyContin. The problem of respiratory depression is particularly acute in elderly or frail patients, which usually occurs after a very high initial dose of non-tolerant patients, or when opioids are used in combination with other drugs that have respiratory depression.
Patients with significantly severe chronic obstructive pulmonary disease or pulmonary heart disease, as well as patients with significant decline in respiratory reserve, hypoxia, hypercapnia, or previous respiratory depression should be used with extreme caution ketone. In such patients, even conventional oxycodone treatment doses can cause reduced respiratory motility and apnea. For these patients, consideration should be given to switching to non-opioid analgesics, and opioids should only be used under strict medical monitoring and at the lowest effective dose.
Craniocerebral injury <br /> Respiratory suppression of opiates includes carbon dioxide retention and secondary cerebrospinal fluid pressure, and may cause preexisting intracranial injury due to existing brain injury, intracranial injury, or other reasons Symptoms such as elevated blood pressure were significantly worsened. Oxycodone can also have effects on the pupillary response and brain consciousness, which may hide neurological signs that further increase intracranial pressure in patients with craniocerebral injury.
Antihypertensive effect < br Oxiconidine can cause severe hypotension symptoms. For patients who need to compensate to maintain blood pressure due to depletion of blood volume, or need to use a combination of drugs such as phenothiazines or other drugs to compensate for vascular tension Patients who use OxyContin may increase their risk of developing hypotension. Orthopaedic patients may develop orthostatic hypotension after using oxycodone. Like all morphine opioid analgesics, oxycodone should also be used with caution in patients with shock, as this product can produce vasodilation, which further reduces cardiac output and blood pressure.
Therefore, patients with hypotension should use this product with caution.
note:
General matters < br Opioid analgesics have a narrow therapeutic index in some patient groups, especially when combined with other central nervous system inhibitors. Use only where the benefits of opioid analgesia outweigh the risks of possible respiratory depression, mental changes, and orthostatic hypotension.
The following situations increase the potential risk of taking OxyContin and should be carefully considered:
Acute alcoholism, adrenal insufficiency (such as Addison's disease), central nervous system depression or coma, tremor delirium, frail patients, scoliosis with respiratory depression, myxedema, hypothyroidism, enlarged prostate or Urethral stricture, severe liver or lung or kidney impairment, toxic psychosis.
The use of oxycodone may obscure the clinical manifestations of acute abdomen and affect the diagnosis, and may exacerbate the seizure symptoms in patients with convulsive disorders. Opioids can induce and exacerbate seizures in certain clinical situations.
Due to factors such as medication dosage and individual sensitivity to drugs, oxycodone may change the patient's ability to respond. Therefore, if the patient's responsiveness is affected by the drug, he should not be engaged in driving or operating machinery.
For interactions with other central nervous system inhibitors, see [Drug Interactions].
For interactions with agonist / antagonist mixed analgesics, see [Drug Interactions].
Outpatient surgery and postoperative use <br /> Oxiconidine is not suitable for advanced analgesia (preoperative administration to treat postoperative pain).
In patients who have not used this product before, since the safety of this product has not been established in this case, OxyContin is not suitable for immediate analgesia after surgery (within 12 to 24 hours after surgery).
OxyContin is not suitable for mild or non-continuous pain treatment after surgery.
OxyContin is only suitable for postoperative patients who have been treated with the drug before surgery, or for moderate to severe and long-lasting pain after surgery. Physicians should use individualized treatment regimens to switch from parenteral administration to oral analgesics.
For some patients who are using OxyContin tablets as an analgesic treatment, if other drugs are given and temporary physiological changes occur due to surgery, the dose should be adjusted accordingly and can still be used safely OxyContin was treated.
OxyContin and other morphine-like opioids have the effect of reducing intestinal motility. Intestinal obstruction is a common postoperative complication, especially after intra-abdominal surgery with opioid analgesia. Postoperative patients receiving opioids should be closely monitored for reduced bowel movements and standard supportive therapies can be used. It is not recommended for patients who may have paralytic intestinal obstruction. The medication should be discontinued as soon as paralytic intestinal obstruction occurs or is suspected.
Application in pancreatic / biliary tract disease <br /> Hydroxycodone can cause sphincter spasm in Oedipus, so it should be used with caution in patients with biliary tract disease (including acute pancreatitis). Opioids (such as oxycodone) can also cause elevated serum amylase levels.
Tolerance and physical dependence <br /> Tolerance means the need to increase the dose of opioids to maintain the analgesic effect achieved (in the absence of disease deterioration or other external factors), physical dependence It is manifested as withdrawal symptoms after abrupt discontinuation of the drug or after administration of the antagonist. After long-term use of opioids, physical dependence and tolerance are not uncommon.
Long-term use in patients may become tolerant to this product and higher doses should be used gradually to maintain pain control. Patients may develop physical dependence, in which case abrupt withdrawal may lead to withdrawal syndrome. Opioid withdrawal or withdrawal symptoms include two or more of the following symptoms: irritability, tearing, runny nose, yawning, sweating, chills, skeletal muscle pain, and dilated pupils. Other symptoms may also occur, including irritability, anxiety, back pain, joint pain, fatigue, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhea, or increased blood pressure, increased breathing, or increased heart rate.
In general, opioid therapy cannot be abruptly discontinued. When patients no longer require oxycodone treatment, the dose should be gradually reduced to prevent the occurrence of withdrawal symptoms.
This product can be used when the diagnosis of non-cancerous chronic pain (such as: bone and joint pain, low back pain, neurovascular pain, neurogenic pain, etc.) is not effective after non-opioid treatment. During the treatment period, if the patient is found to prescribe this medicine with two or more physicians at the same time, the medicine should be discontinued when the dosage increases sharply or there are other abnormal behaviors.

Oxycodone hydrochloride sustained-release tablets for pregnant and lactating women

Prohibited in pregnant and lactating women. Oxycodone is secreted with breast milk and may cause respiratory depression in newborns.

Oxycodone hydrochloride sustained-release tablets for children

At present, no medication information is available for patients under the age of 18, so it is not recommended for patients under the age of 18.

Oxycodone hydrochloride sustained-release tablets for elderly

The pharmacokinetic results showed that the clearance of oxycodone in elderly patients (aged more than 65 years) was only slightly lower than in young people. Adverse drug reactions are not affected by age. Therefore, the dosage and interval of medication for adults are also applicable to elderly patients.

Drug interactions of oxycodone hydrochloride sustained-release tablets

Similar to other opioids, this product can have additive effects with the following drugs: sedatives, narcotics, hypnotics, alcohol, antipsychotics, muscle relaxants, antidepressants, phenothiazines and antihypertensives. Patients receiving other CNS inhibitors should use oxcontin with caution and reduce the initial dose (1/3 to 1/2 of the conventional dose). OxyContin at regular doses may cause drug interactions when combined with these drugs, leading to symptoms such as respiratory depression, hypotension, deep sedation or coma.
For patients who have been or are being treated with pure agonist opioid analgesics (such as oxycodone), when using agonist / antagonist mixed analgesics (such as pentazocine, nalbuphine, and butorphino) Care should be taken. In this case, agonistic / antagonistic mixed analgesics may reduce the analgesic effect of oxycodone and / or induce withdrawal symptoms in these patients.
Although no interactions between oxycodone and monoamine oxidase inhibitors have been observed, the simultaneous use of any opioid should avoid the simultaneous use of monoamine oxidase inhibitors. Some oxycodone is metabolized to hydroxyhydromorphone by the action of cytochrome P450-2D6 enzyme. The concentration of hydroxyhydromorphone is less than the total dose of 15 0700. Certain drugs (such as antidepressants, cardiovascular drugs such as amiodarone and quinidine) may block this metabolic pathway. However, the combined use of quinidine, which has an inhibitory effect on cytochrome P450-2D6 enzymes, did not affect the efficacy of oxycodone. Other drugs that may inhibit the metabolism of oxycodone include cytochrome P450-3A enzyme inhibitors such as cimetidine, ketoconazole and erythromycin.

Oxycodone hydrochloride sustained release tablets overdose

Symptoms of oxycodone overdose and poisoning are pinpoint pupils, respiratory depression, and hypotension. In severe cases, drowsiness, coma may develop, circulatory failure and deep coma, skeletal muscle relaxation, bradycardia, and death.
Rescue treatment for oxycodone excess: first keep the airway open, then give the corresponding supportive therapy (improve ventilation, oxygen, boost drugs), correct shock and pulmonary edema, cardiac arrest or arrhythmia may require cardiac massage or removal Tremble. If necessary, gastric lavage and removal of gastric contents can remove unabsorbed drugs, especially for sustained release pharmaceutical preparations.
Rescue medication: naloxone 0.4mg-0.8mg, intravenous injection. If necessary, repeat administration at intervals of 2-3 minutes, or dissolve 2 mg of naloxone in 500 ml of physiological saline or 5% glucose (0.004 mg / ml) and inject it intravenously. The rate of drug infusion is determined based on the situation and the doses taken in the past. Due to the relatively short duration of naloxone and the release of oxycodone by this product for 12 hours, the condition must be closely observed until the patient resumes stable spontaneous breathing.
For a few patients with severe overdose, 0.2 mg of naloxone was administered intravenously, followed by an increase of 0.1 mg every 2 minutes. Patients who overdose oxycodone do not need to use naloxone if they have no clinically significant respiratory depression or circulatory disturbances. Naloxone should be used with caution in patients with or dependent on oxycodone. Because the use of naloxone in this case may suddenly and completely block the effects of opioids, leading to acute pain episodes and acute withdrawal syndrome.

Pharmacotoxicology of oxycodone hydrochloride sustained-release tablets

Pharmacological effects < br Oxycodone hydrochloride is an opioid analgesic, a pure opioid receptor agonist, and its main therapeutic effect is analgesia. Like all other pure opioid receptor agonists, oxycodone increases the analgesic effect with increasing dose, while mixed opioid receptor agonists / antagonists or non-opioid analgesics are different, increasing the analgesic effect of dose To a limited extent. For pure opioid receptor agonistic analgesics, there is no determined maximum dosage; the maximum analgesic effect can only be determined by side effects, and more serious side effects may include drowsiness and respiratory depression.
The exact mechanism of oxycodone analgesic effect is unknown. Some specific CNS opioid receptors with opioid endogenous substances have been found in the brain and spinal cord, which may be related to the analgesic effect of oxycodone.
Oxycodone produces respiratory depression by directly acting on the brainstem respiratory center, including reduced responsiveness to carbon dioxide and electrical stimulation. Oxycodone directly acts on the cough center and suppresses cough reflex. Antitussive effects may occur at less than conventional analgesic doses. Oxycodone can cause pupils to shrink, even in completely dark environments. In the case of oxycodone overdose, dilated pupils may appear rather than dilated pupils.
Toxicological studies of genotoxicity <br /> The results of Ames test of oxycodone and micronucleus test of mice were negative. In human lymphocytic chromosome aberration test, the result was negative when the dose was 1500 g / ml in the absence of metabolic activation and 5000 g / ml in the case of metabolic activation, but the result was positive when the metabolic activation was applied for 24 hours (Dose 125 0 ug / ml); in the mouse lymphoma test, the result was positive when there was a metabolic activation dose 501ig / ml and no metabolic activation dose 400ug / ml.
Reproductive toxicity < br Oral administration of oxycodone in rats and rabbits reached 8 mg / kg and 125 mg / kg, respectively. No abnormalities of fetuses caused by oxycodone were observed. The above doses are equivalent to 3 times and 46 times the human 160 mg / day dose in terms of mg / kg, respectively.

Pharmacokinetics of oxycodone hydrochloride sustained-release tablets

The active ingredient of this product is oxycodone. After oral administration, there will be two release phases, namely an early fast release phase that provides rapid analgesia and a subsequent sustained release phase. The drug will last for 12 hours. This product is well absorbed, the oral bioavailability is 60% to 87%, and the relative bioavailability of the immediate release oral preparation is 100%. After several doses of plant health volunteers, the steady-state blood drug concentration is reached within 24 to 36 hours. The dosage is proportional to the peak plasma concentration (Cmax), and the dosage is proportional to the area under the curve (AUC). Its average apparent elimination half-life is 4,5 hours, reaching a steady state in about 1 day. The main metabolites of oxycodone are noroxycodone and hydroxyhydromorphone. The metabolites are mainly excreted by the kidneys. The peak drug concentration was reached about 3 hours after the oral administration of this product. Compared with taking 5mg of this product every 12 hours and 5mg of oxycodone common preparation every 6 hours, the peak and valley blood concentrations are the same.

The release of oxycodone from this product is not affected by pH. Ingestion of high-fat foods does not affect the drug absorption and peak concentration.
Age: The AUC of elderly people is 15% higher than that of young people.
Gender: On the basis of weight adjustment, the average plasma oxycodone concentration in women is 25% higher than that in men.
Renal dysfunction: Compared with normal people, the peak concentrations of oxycodone and noroxycodone in patients with mild to moderate renal dysfunction increased by about 50% and 20%, respectively; oxycodone, noroxycodone, and hydroxycodone The AUC of hydromorphone increased by about 60%, 60%, and 40%, respectively. The half-life of oxycodone was extended by only 1 hour.
Mild to moderate hepatic dysfunction: Compared with normal people, the peak plasma oxycodone and noroxycodone concentrations of patients with mild to moderate hepatic dysfunction increased by approximately 50070 and 20070l AUC, respectively, and the plasma oxyhydromorphone peak increased by approximately 95070 and 750700 Concentration and AUC were reduced by 15% to 50%. The elimination half-life of oxycodone was extended by 2.3 hours.

Storage of oxycodone hydrochloride sustained-release tablets

The storage temperature does not exceed 25 ° C (25 ° C).

Packaging of oxycodone hydrochloride sustained-release tablets

Aluminum-plastic packaging.
(1) 1 plate per box, 10 pieces per plate (2) 1 plate per box, 6 pieces per plate.

Duration of Oxycodone Hydrochloride Sustained-release Tablets

36 months.

Executive standard for oxycodone hydrochloride sustained-release tablets

Import drug registration standard JM20030007 ^[1]