Oxycodone

DESCRIPTION / DEFINITIONS: Oxycodone (Oxycodone Hydrochloride) is a prescription painkiller formulated on its own or in a tablet combination with other painkillers, like acetaminophen. It is approved for severe, 24-hour pain that is not successfully controlled by any other treatment, although it is often prescribed for less painful situations.

ABUSE: Oxycodone has high potential for abuse similar to other opioids including fentanyl, hydrocodone, hydromorphone, methadone, morphine, oxymorphone.

ADDICTION / DEPENDENCE: Taking oxycodone for an extended period of time is likely to cause dependency and addiction. It is meant to be taken at the lowest effective dose for the shortest period of time.

SIDE EFFECTS:  According to the drug label, oxycodone can have serious side effects such as adrenal insufficiency, impaired or dim vision, anemia, bone pain, bronchitis, chest pain, difficulty breathing, erectile dysfunction, and feeling faint. See complete list below.

WITHDRAWAL SYMPTOMS: Common withdrawal symptoms include: abdominal cramps and pain that won’t go away, loss of appetite, anxiety, insomnia, increased blood pressure and heart rate and more. See more complete list below.

TREATMENT: Medical detox facilities are the most comfortable and safest way to stop taking oxycodone. Call us to talk to a Detox Advisor.

 

DESCRIPTION / DEFINITIONS

Oxycodone (Oxycodone hydrochloride) is a prescription painkiller formulated on its own or in a tablet combination with other painkillers, like acetaminophen.

It is a very strong medication, and is supposed to be used only by people with pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which no other medication or treatment has worked. It is also not supposed to be taken in combination with benzodiazepines or other central nervous system (CNS) depressants unless there are no other options. How much is prescribed and for how long is supposed to be held to the minimum required.

It is sold under several brand names, including, but not limited to:

  • Endocet® (also contains acetaminophen)
  • Endodan® (also contains aspirin)
  • Oxaydo®
  • Oxecta®
  • Oxycontin ®
  • Percocet® (also contains acetaminophen)
  • Percodan® (also contains aspirin)
  • Primlev®- (also contains acetaminophen)
  • Roxicet® – also contains acetaminophen, in solution or tablet form
  • Roxicodone®
  • Xartemis®
  • Xartemis XR® (also contains acetaminophen)
  • Xolox®-  (also contains acetaminophen)
  • Xtampza®

Oxycodone is dangerous and has a very high potential for abuse, addiction, misuse, and dependency.

One of the official warnings on the oxycodone label summarizes the potential problems:

WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME, CYTOCHROME P450 3A4 INTERACTION; HEPATOTOXICITY, and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS

Addiction, Abuse, and Misuse

Oxycodone Hydrochloride and Acetaminophen Tablets exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Assess each patient’s risk prior to prescribing Oxycodone Hydrochloride and Acetaminophen Tablets, and monitor all patients regularly for the development of these behaviors and conditions:

Life-Threatening Respiratory Depression

Serious, life-threatening, or fatal respiratory depression may occur with use of Oxycodone Hydrochloride and Acetaminophen Tablets. Monitor for respiratory depression, especially during initiation of Oxycodone Hydrochloride and Acetaminophen Tablets or following a dose increase.

Accidental Ingestion

Accidental ingestion of Oxycodone Hydrochloride and Acetaminophen Tablets, especially by children, can result in a fatal overdose of Oxycodone Hydrochloride and Acetaminophen Tablets.

Neonatal Opioid Withdrawal Syndrome

Prolonged use of Oxycodone Hydrochloride and Acetaminophen Tablets during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts. If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available.

Cytochrome P450 3A4 Interaction

The concomitant use of Oxycodone Hydrochloride Tablets with all cytochrome P450 3A4 inhibitors may result in an increase in Oxycodone plasma concentrations, which could increase or prolong adverse reactions and may cause potentially fatal respiratory depression. In addition, discontinuation of a concomitantly used cytochrome P450 3A4 inducer may result in an increase in Oxycodone plasma concentration. Monitor patients receiving Oxycodone Hydrochloride and Acetaminophen Tablets and any CYP3A4 inhibitor or inducer.

Hepatotoxicity

(For Oxycodone when combined the acetaminophen). Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at doses that exceed 4000 mg per day, and often involve more than one acetaminophen-containing product.

Risks From Concomitant Use With Benzodiazepines Or Other CNS Depressants

Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death.

Oxycodone is classed by the DEA as a Schedule II, which means:

A. The drug or substance has a high potential for abuse.

B. The drug or other substance has a currently accepted medical use in treatment in the United States or a currently accepted medical use with severe restrictions.

C. Abuse of the drug or other substances may lead to severe psychological or physical dependence.

Other members of the class of opioid agonists include morphine, hydromorphone, fentanyl, codeine, and hydrocodone.

 

ABUSE

Oxycodone has  high potential for abuse – and is one of the most commonly abused painkillers, similar to other opioids including fentanyl, hydrocodone, hydromorphone, methadone, morphine, and oxymorphone as well as Oxycontin, Percocet and other painkillers that contain oxycodone as their active ingredient.

One can abuse oxycodone taking more of it than was prescribed, taking it without a prescription, or changing the way it is supposed to be taken. With oxycodone, for example, instead of swallowing a pill, one could crush the pills and snort (inhale) the powder, or dissolve it in water and inject it in the blood, muscle, or under the skin.

 

ADDiCTION / DEPENDENCE

Taking oxycodone for an extended period of time is likely to cause dependency and addiction. It is meant to be taken at the lowest effective dose for the shortest period of time.

The longer you take oxycodone, the more dangerous it becomes. The body builds a tolerance to the drug so that more of it is needed to create the pain-relieving effects. But the more it is taken, the greater the risk of dependency and addiction, and also of illness, overdose, and death.

The side effects can also get worse with increased use and endanger your health. And getting off the drug can be more difficult and dangerous.

 

HALF LIFE AND METABOLISM

The biological half-life of a substance is the time it takes for a drug to lose half of its pharmacologic activity. This is significant because it affects how soon withdrawal symptoms may appear.

The half life of Oxycodone is between 3 to 5 hours.

Oxycodone is extensively metabolized to norOxycodone by means of CYP3A-mediated N- demethylation, oxymorphone by means of CYP2D6-mediated O-demethylation, and their glucuronides.

The CYP enzymes are the major enzymes involved in drug metabolism, and since many drugs may increase or decrease the activity of various CYP isozymes, this is a major source of adverse drug interactions, since changes in CYP enzyme activity may affect the metabolism and clearance of various drugs. For example, if one drug inhibits the CYP-mediated metabolism of another drug, the second drug may accumulate within the body to toxic levels, possibly causing an overdose.

The half life of acetaminophen – with which oxycodone is frequently combined – is 1.25 to 3 hours. It is primarily metabolized in the liver by first-order kinetics and involves three principal separate pathways: conjugation with glucuronide; conjugation with sulfate; and oxidation via the cytochrome, P450-dependent, mixed-function oxidase enzyme pathway to form a reactive intermediate metabolite, which conjugates with glutathione and is then further metabolized to form cysteine and mercapturic acid conjugates. The principal cytochrome P450 isoenzyme involved appears to be CYP2E1, with CYP1A2 and CYP3A4 as additional pathways.

OPIOID INDUCED HYPERALGESIA

There is increasing medical research showing that taking opioids like oxycodone for longer than six months will create a condition called Opioid Induced Hyperalgesia. This is a condition where the opioids actually make the pain receptors more sensitive and, therefore, make the pain greater. A person with this condition is required to take more and more of the opioid to try to address the pain but finds that the pain actually increases.

 

SIDE EFFECTS

According to the label, serious adverse reactions that may be associated with oxycodone include:

  • abdominal pain
  • accidental injury
  • adrenal insufficiency (after greater than one month of use) – the adrenal glands do not produce enough hormones. This can result in chronic, or long lasting, fatigue
    muscle weakness, loss of appetite, weight loss, abdominal pain, nausea, vomiting, diarrhea, low blood pressure that drops further when a person stands up, causing dizziness or fainting, irritability and depression, craving salty foods, hypoglycemia (low blood sugar), headache, sweating, irregular or absent menstrual periods in women, loss of interest in sex.
  • agitation
  • ambylopia – impaired or dim vision
  • amenorrhea – abnormal or lack of menstruation
  • anaphylaxis –  – an acute allergic reaction that prompts the immune system to respond. The symptoms can include: fainting, lightheadedness, low blood pressure, dizziness,  flushing, difficulty breathing, rapid breathing, shortness of breath,  wheezing, hives, swelling under the skin, blue skin from poor circulation, rashes, nausea,  vomiting, fast heart rate, feeling of impending doom, itching, tongue swelling, difficulty swallowing, facial swelling, mental confusion, nasal congestion, or impaired voice.
  • androgen deficiency (with chronic use) – reduction of  male hormones (in men or women) which may cause hot flashes, sweating, insomnia, nervousness, irritability, tiredness, loss of motivation, short-term memory problems, declining self-esteem, depression, decreased energy levels, diminished muscle strength, decline or loss of libido or sexual desire, poor erections, reduced orgasmic quality, reduced volume of semen, diminished muscle mass, hair loss, abdominal obesity, reduction in high-density lipoprotein (HDL) cholesterol, an increase in total body fat, and osteoporosis
  • anemia – reduction in red blood cells
  • anxiety
  • arthralgia – pain in a joint
  • arthritis – painful inflammation and stiffness of the joints
  • back pain
  • bone pain
  • bronchitis – an inflammation of the lining of your bronchial tubes, which carry air to and from your lungs. People who have bronchitis often cough up thickened mucus, which can be discolored. Bronchitis may be either acute or chronic.
  • central nervous system (CNS) depression – inhibition of brain activity resulting in decreased rate of breathing, decreased heart rate, and loss of consciousness, possibly leading to coma or death
  • changes in heartbeat
  • chest pain
  • chills
  • constipation
  • cough increased
  • decreased sexual desire
  • deep thrombophlebitis – an inflammatory process that causes a blood clot to form and block one or more veins, usually in your legs
  • development of tolerance, creating a need to take more of the drug to get the same effects   
  • diarrhea
  • difficulty breathing
  • difficulty swallowing
  • digestion of food inhibited
  • dizziness
  • drowsiness
  • dry mouth
  • dyspepsia – indigestion
  • dysphagia – difficulty or discomfort in swallowing
  • edema – watery fluid collecting in the cavities or tissues of the body, ‘retaining water’
  • epistaxis – nosebleeds
  • erectile dysfunction
  • extreme drowsiness
  • feeling faint
  • fever
  • flu syndrome
  • flushing
  • gingivitis – gum infection
  • glossitis –  tongue swollen along with change in color and development of a different appearance on the surface
  • gout – arthritis, especially in the smaller bones of the feet, causing episodes of acute pain
  • hallucinations (seeing things or hearing voices that do not exist)
  • headache
  • heart failure
  • hemorrhage
  • herpes simplex
  • hives
  • hoarseness
  • hyperglycmia – too much glucose in the bloodstream
  • hypertonia – too much muscle tone so that arms or legs, for example, are stiff and difficult to move
  • hypesthesia – an abnormally weak sense of pain, heat, cold, or touch
  • hypogonadism – insufficient sex hormones, male or female. Symptoms can include: lack of menstruation, slow or absent breast growth, hot flashes, loss of body hair, low or absent sex drive, milky discharge from breasts, muscle loss, abnormal breast growth, reduced growth of penis and testicles, erectile dysfunction, osteoporosis (bones become brittle and fragile from loss of tissue), low or absent sex drive, infertility, fatigue, hot flashes, difficulty concentrating
  • hypotension – low blood pressure
  • immune system suppressive
  • impotence
  • inability to get or keep an erection
  • infection
  • infertility
  • iron deficiency
  • irregular menstruation
  • itching
  • jaundice – a yellowish tinge to the skin and eyes
  • laryngimus -laryngitis, an inflammation of the larynx, typically resulting in huskiness or loss of the voice, harsh breathing, and a painful cough
  • leukopenia – a decrease in white or red blood cells, a sign of disease
  • light-headedness when changing positions
  • loss of appetite
  • loss of coordination
  • low libido – decrease in sex drive
  • lung disorder
  • mental changes such as confusion
  • migraine
  • miosis – excessive constriction of the pupil of the eye, even in total darkness. (Marked mydriasis (dilation of the pupil of the eye) rather than miosis may be seen due to hypoxia (deficiency in the amount of oxygen reaching the tissues) in overdose situations.)
  • mood changes
  • myalgia
  • nausea
  • neck pain
  • nervousness
  • neuralgia – intense, typically intermittent pain along the course of a nerve, especially in the head or face
  • orthostatic hypotension – dizziness and fainting upon standing up
  • pain
  • pale stools
  • palpitation  – a noticeably rapid, strong, or irregular heartbeat
  • pathological fracture – a bone fracture caused by disease that led to weakness of the bone structure
  • personality changes
  • pharnygitis – inflammation of the pharynx, causing a sore throat
  • photosensitivity reaction – eyes sensitive to light
  • pruritus – severe itching of the skin
  • rash
  • red eyes
  • respiratory depression – in the early stages may cause fatigue, anxiety, shortness of breath, slow breathing, shallow breathing, being tired during the day
  • rhinitis – inflammation of the mucous membrane of the nose, caused by a virus infection (e.g., the common cold) or by an allergic reaction (e.g., hay fever)
  • seizures
  • sepsis – a potentially life-threatening complication of an infection
  • serotonin syndrome (when taken in combination with serotonergic drugs) -serotonin syndrome is a group of side effects that include high body temperature, agitation, increased reflexes, tremor, sweating, dilated pupils, and diarrhea, associated with serotonergic drugs. Serotonergic drugs are used to treat migraine. depression and other mood disorders.
  • severe muscle stiffness or twitching
  • shivering
  • shortness of breath
  • sinusitis – inflammation of a nasal sinus
  • sleepiness
  • syncope – temporary loss of consciousness caused by a fall in blood pressure
  • sweating
  • swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
  • tachycardia – abnormally rapid heart rate
  • tea-colored urine
  • tiredness
  • tremor
  • trouble breathing
  • trouble walking
  • urinary tract infection
  • urticaria – a rash of very itchy round, red welts on the skin. It is sometimes accompanied by dangerous swelling and is generally an allergic reaction.
  • vomiting
  • weakness

 

WITHDRAWAL SYMPTOMS

Oxycodone is a highly addictive drug. If you use it for a long time, you’re likely to become either dependent on or addicted to the drug. If you try to stop taking it, you will most likely experience withdrawal symptoms, unless you’ve been taking it for a very short time – days, rather than several weeks, months or years. Many people don’t want to quit taking the drug because the withdrawal symptoms are so uncomfortable. Quitting suddenly can be dangerous.

The oxycodone withdrawal symptoms include:

  • abdominal cramps and pain that won’t go away
  • anorexia
  • anxiety and agitation
  • backache
  • chills
  • coughing fits
  • diarrhea
  • dilated pupils
  • frequent nausea and vomiting
  • goose bumps
  • heavy sweating
  • hot and cold flashes
  • increased blood pressure
  • increased heart rate
  • increased respiratory rate
  • insomnia
  • irritability
  • joint pain
  • muscle pain
  • rapid or irregular heartbeat
  • runny nose
  • sleeplessness
  • weakness

TREATMENT

Trying to withdraw from oxycodone on your own can be so uncomfortable that 95 percent of the people who try don’t succeed. To relieve the pain, they take another pill. The best treatment protocol is in a medical detox facility that through various technologies can assist with the withdrawal and make it safe and much less uncomfortable. Call us to talk to a Detox Advisor.