Oxycodone

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The active ingredient oxycodone is a pain reliever from the opioid class and is used for severe to extremely severe pain. Opioids are widely considered to be the safest and most effective pain relievers available. The analgesic effect of oxycodone exceeds that of the well-known morphine. Here you can read everything you need to know about the effects, side effects and use of oxycodone.

This is how oxycodone works

Oxycodone is a strong pain reliever from the group of opioids. It also has anti-anxiety, cough-relieving and calming properties.

Generally, pain is triggered by a painful stimulus such as an injury or inflammation. Information about the severity and location of the pain is transmitted to the brain via peripheral nerves and the spinal cord.

Only there is the conscious processing and perception of the pain. Opioids such as oxycodone have the ability to block this central pain perception and are therefore used as analgesics (pain relievers).

Opioids are produced synthetically (artificially). These include, for example, oxycodone, fentanyl and methadone. Opiates, on the other hand, are of natural origin. These include, for example, morphine and codeine, both of which are obtained from the dried milky sap of the opium poppy.

The body's own messenger substances (so-called endorphins) bind to the same binding sites as opiates and opioids and also have an analgesic effect. They are therefore sometimes referred to as the body's own (endogenous) opioids.

Uptake, breakdown and excretion

Almost all of the active substance in an oxycodone tablet (around 60 to 85 percent) is absorbed into the body's bloodstream. The analgesic effect occurs in about 60 minutes and generally lasts for about four hours. But there are also preparations with a prolonged effect - they work for eleven to 14 hours.

Oxycodone is eventually broken down by certain enzymes in the liver (cytochrome P450 such as CYP3A4) and excreted via the kidneys.

When is oxycodone used?

Oxycodone is one of the very strong pain relievers. It is slightly more effective than morphine and is used to treat severe and severe pain, such as:

Pain due to damage to or disorder of the nervous system (neuropathic pain)
Pain as a result of cancer

This is how oxycodone is used

Oxycodone is only used to treat severe pain. The active ingredient is usually administered orally - usually as a tablet or capsule, sometimes as a solution. You can also give the pain reliever directly into a vein (as an intravenous injection / infusion).

The dosage is determined by the doctor and gradually increased until the desired effect is achieved. The dose required for this varies from person to person. At the beginning of a treatment, the patient usually receives the pain reliever twice a day.

The preparations usually contain the active ingredient in the form of salts as oxycodone hydrochloride (oxycodone HCl). The salt form of an active ingredient is necessary in the manufacture of pharmaceuticals in order to convert the active ingredient into a form that is soluble in the gastrointestinal tract.

What are the side effects of oxycodone?

Very common with the use of opioids such as oxycodone:

Constipation (constipation)
Constriction of the pupil (miosis)

The following side effects rarely occur:

Muscle twitching, hardening of the muscles of the chest (muscle rigidity)
Missing menstruation (secondary amenorrhoea)
sleep disorders
Mood swings (such as euphoria or depression)

Central side effects such as hallucinations, confusion, vomiting and nausea are less common with oxycodone than with other opioids. Allergic reactions are also much less common.

With regular use, tolerance to oxycodone can develop, so the pain reliever loses its effectiveness. Then you either have to increase the dosage to achieve the same pain relieving effect as at the beginning of the treatment, or switch to a different pain reliever.

Physical (physical) dependence may develop after prolonged use of high doses of oxycodone. This can be problematic, especially with chronic (long-term) pain therapy.

You should therefore not suddenly stop taking the pain reliever. Otherwise, withdrawal symptoms such as sweating, racing heart (tachycardia) and psychomotor restlessness would occur. If the intake is to be stopped, the dose of the pain reliever should be reduced gradually.

When should you not take oxycodone?

Contraindications

Oxycodone is not suitable as a pain reliever for:

severe breathing disorder (respiratory failure)
severe COPD (chronic obstructive pulmonary disease)
severe bronchial asthma
Obstruction of the intestine (ileus)
Hypersensitivity to the active ingredient or any other drug ingredient

Interactions

Oxycodone increases the effect of other central depressant substances such as tranquilizers (sedatives), muscle relaxants (muscle relaxants), agents against depression (antidepressants), agents against nausea and vomiting (antiemetics), allergy drugs (antihistamines) and alcohol.

Simultaneous use of drugs that are broken down by the same liver enzymes (CYP3A4, CYP2D6) as oxycodone can reduce or increase the breakdown and thus the effect of the pain reliever:

There are substances that inhibit CYP3A4 and thus increase the effect of oxycodone. These include ketoconazole and itraconazole (antifungal agents), clarithromycin and telithromycin (macrolide antibiotics), cimetidine (antihistamine) and grapefruit juice. Inhibitors of the liver enzyme CYP2D6 (e.g. the andidepressants paroxetine, bupropion and fluoxetine) have the same effect on the effect of oxycodone.

So-called CYP3A4 inducers, on the other hand, boost the activity of this liver enzyme and thus the breakdown of the pain reliever, which weakens its effect. This applies to rifampicin (antibiotic), phenytoin and carbamazepine (anti-epileptic drugs) and St. John's wort.

Age restriction

Oxycodone is contraindicated in children under the age of twelve. Combination preparations of oxycodone with naloxone are only approved from the age of 18 years.

pregnancy and breast feeding period

Previous studies have provided no evidence of a teratogenic effect of oxycodone. Its use during pregnancy is therefore acceptable if it is well founded (strict indication). However, the pain reliever should be used as briefly as possible. Or one switches to more suitable alternatives (morphine, tramadol, buprenorphine9.

Data are available on around 250 mother-child pairs in which the mother was treated with oxycodone. The breastfed infants were at an increased risk of side effects such as drowsiness and poor drinking. For this reason, other opioids such as fentanyl, morphine or buprenorphine are preferred during breastfeeding.

How to get oxycodone medication

Oxycodone is a strong opioid pain reliever and is subject to the Narcotics Act in Germany and Switzerland and the Narcotics Act in Austria. It can only be prescribed by the doctor on special prescriptions (narcotics or addictive substance prescriptions) and can be obtained from the pharmacy.

Since when has oxycodone been known?

Oxycodone has been on the market in Germany for pain therapy in the form of tablets since 1998. It was not until 2006 that it was also approved for parenteral injection into the vein (intravenous administration).

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