Drug

Oxycodone

Trade names

Oxycontin®, Oxygesic®

Chemical name and molecular formula

(5R, 9R, 13S, 14S) -14-hydroxy-3-methoxy-17-methyl-4,5-epoxymorphinan-6-one;
C18H21NO4

Definition / explanation

Oxycodone is often given in capsule form.

Oxycodone belongs to the class of strong opioid analgesics. It is used to relieve severe to very severe pain, but it also has an antitussive effect.
It is also a very effective antitussive (cough suppressant) like codeine.
The WHO level scheme (scheme of pain therapy) classifies oxycodone at level III.

Application form and dosage

Oxycodone can be taken in various forms and dosages. There are both fast-acting capsulessuch as sublingual capsules, as well as slow-dosing Retard capsules.
Oxycodone can also be sent by injection be given, for example. To suppress unbearable pain, such as occur more often in cancer patients. Such a pain is called Breakthrough pain.
The dosage starts at 5 mg (as a capsule) and can take up to 80 mg in a retard capsule.
The drug is prescription only and is subject to Narcotics Act. It must therefore be on BtM prescription be prescribed. Any intake and its dosage are strictly controlled by doctors and tailored to the patient and his pain level.

indication

Oxycodone can also be used as a cough suppressant. In Germany, on the other hand, codeine and dihydrocodeine are more commonly used.

The active ingredient oxycodone is used for very severe pain, such as Tumor pain, postoperative or traumatic Jokes prescribed. It can also be used as an antitussive, but this is more commonly used in Germany Codeine and Dihydrocodeine.

Mechanism of action

Oxycodone works on the body's own Opioid receptors in the central nervous system. These opioid receptors are the body's system for Pain relief. They practically represent a natural protective mechanism against pain.
Oxycodone works here agonistic, that is, it's the action of the opioid receptors reinforced. Compared to Morphine is about oxycodone twice as strong. It also works on the brain Cough center and works like that cough suppressant.
In combination with the active ingredient Naloxone can be a typical one for analgesics Indolence avoided, which is one of the benefits of oxycodone. After ingestion, the drug is distributed throughout the body and has a Half-life of four hours. This means that after four hours, half of the active ingredient is broken down by the body. Morphine takes about twice as long. The breakdown products (Metabolites) become with the urine and stool eliminated.

Side effects

As with all drugs from the class of opioid analgesics, a number of undesirable side effects can occur. First of all, it should be said that oxycodone is a very high one Addictive potential which the patient must be informed about in advance.
It can be too strong Euphoria lead and therefore holds a high Risk of abuse. This is particularly dangerous if, for example, slow-acting sustained-release capsules are ground and taken in this way, since the entire active ingredient then unfolds its effect at the same time.
It can be serious Respiratory depression come that can be fatal. Other side effects are nausea, Vomit and dizziness.
Continue to step Bradycardia (abnormal heart rhythm), Hypotension (low blood pressure) and fatigue on.
It can be used for Miosis (Constriction of the pupil), Constipation (Constipation), Urinary retention and sweat come. Most of the side effects are reversible and occur at the beginning of therapy.

Interactions

The following drugs and substances can increase the effect of oxycodone: benzodiazepines, barbiturates, tricyclic antidepressants, phenotiazines, muscle relaxants, Antihistamines, Ethanol and anesthetics.
It refers to sedating Substances. If taken at the same time, side effects can occur unpredictably.

Pharmacokinetic interaction

Oxycodone can interact with a number of substances that are metabolized by the same enzymes. The important enzymes are called CYP3A4-Isoenzymes.
Inhibitors of these enzymes (substances that block the enzymes) amplify the effect of oxycodone. These substances include: verapamil, erythromycin, fluconazole, imatinib, diltiazem, clarithromycin, voriconazole, ritonavir, indinavir, nelfinavir, ketoconazole, itraconazole, telithromycin, cyclosporin and grapefruit juice.
There are also substances that have the opposite effect on these enzymes and thus the effect of oxycodone reduce. These include: rifampicin, penytoin, primidone, Carbamazepine, Efavirenz, Johannis herbs, Oxcarbazepine, phenobarbital, and nevirapine.

Contraindications

The use of oxycodone is contraindicated if one allergy against the active ingredient. Furthermore, the intake is for a paralytic Ileus, one Respiratory depression and severe bronchial obstruction (e.g. asthma) contraindicated.