What is hydrocodone 15 500

Oxycodone

Like most analgesics from the opioid group, oxycodone is used primarily for severe and very severe pain. Oxycodone is about twice as strong as morphine and is therefore not one of the extremely strong opioids.

application

The active ingredient oxycodone is indicated for the therapy of severe pain that can only be adequately treated with opioid analgesics. The combination with naloxone is intended to counteract constipation that can occur during opioid therapy.

Mechanism of action

Oxycodone is one of the opioids and therefore one of the strong analgesics. The active ingredient belongs to the dihydro derivatives of morphine. These also include dihydrocodeine, hydromorphone and hydrocodone. Oxycodone and hydromorphone are used as analgesics, while dihydrocodeine and hydrocodone are used as antitussives.

Oxycodone has an activating effect on µ-, κ- and δ-opioid receptors in the brain and spinal cord. Oxycodone acts on these receptors as an opioid agonist without an antagonistic effect. Its therapeutic effect is mainly analgesic and sedating. As with all opioids, the use of oxycodone is associated with the risk of developing addiction.

Pharmacokinetics

With regard to the pharmacokinetics of oxycodone, it should be noted that the active ingredient is also available in the form of sustained-release formulations.

After oral administration, the absolute bioavailability of oxycodone is 42-87%, the maximum plasma concentration is reached after about 1 to 1.5 hours, with prolonged-release tablets after 3 hours. In the case of prolonged-release tablets, absorption takes place in two phases with an initially relatively short half-life of 0.6 hours for the smaller part of the amount of active ingredient. The second absorption phase is slower and lasts about 6.9 hours.

The protein binding of oxycodone is 38-45%. The half-life is 4-6 hours.

Oxycodone is metabolized in the intestine and liver via the P450 cytochrome system to noroxycodone, oxymorphone and various glucuronide conjugates. The route of elimination is 33-61% renal.

dosage

Oxycodone is mainly available in the form of prolonged-release tablets. The dosage should be adjusted to the intensity of pain and the individual sensitivity of the patient. The starting dose for opioid-naïve patients is usually 10 mg every 12 hours for prolonged-release formulations. Further dosages can be found in the respective technical information.

Since dependence can develop on oxycodone therapy, therapy should not be stopped abruptly.

Side effects

The most common side effects of oxycodone therapy are nausea and constipation. In addition, respiratory depression, miosis, spasms of the bronchial muscles and a dampening of the cough reflex can occur.

The side effects are listed below according to their frequency.

Very often:

  • Sedation (tiredness to drowsiness)
  • dizziness
  • a headache
  • Constipation
  • nausea
  • Vomit
  • Itching.

Often:

  • Decrease in appetite
  • Psychological side effects, e.g. B. Changes in mood, lack of drive, confusion
  • tremor
  • Dyspnea
  • Bronchospasm
  • Dry mouth
  • Gastrointestinal complaints, e.g. B. Abdominal pain
  • Skin symptoms such as rash, rarely increased photosensitivity
  • Increased need to urinate
  • Weaknesses.

Occasionally:

  • Syndrome of inadequate ADH secretion
  • Immune system hypersensitivity
  • Dehydration
  • Changed perception
  • Drug addiction
  • Increased / decreased muscle tension
  • Seizures, especially in people with epilepsy or those prone to seizures
  • Hypesthesia, paraesthesia
  • Incoordination
  • amnesia
  • Lacrimation disorders
  • Miosis
  • Visual disturbances
  • Hyperacusis
  • Vertigo
  • Pulse acceleration
  • Palpitations (associated with withdrawal syndrome)
  • Vasodilation
  • Respiratory depression
  • Increased cough
  • Sore throat
  • sniff
  • Change of voice
  • Mouth ulcers and inflammation of the gums
  • flatulence
  • Ileus
  • Increase in liver enzymes
  • Dry skin
  • Urinary retention
  • Erectile dysfunction
  • chills
  • Edema, also peripheral
  • migraine
  • Drug tolerance
  • Drug withdrawal syndrome
  • Accidental injuries.

Rare:

  • Herpes simplex
  • Lymphadenopathy
  • Increased appetite
  • (Orthostatic) hypotension
  • Bleeding gums
  • Tarry stool
  • Tooth changes
  • Urticaria
  • Muscle spasms
  • Hematuria
  • Weight changes
  • Cell tissue inflammation.

Side effects of unknown frequency:

  • Anaphylactic reactions
  • aggressiveness
  • Hyperalgesia
  • Dental caries
  • Cholestasis
  • Biliary colic
  • Amenorrhea.

Interactions

With the simultaneous use of oxycodone and drugs that have an effect on the CNS, the CNS depressant effect can be increased. This includes other opioids, sedatives, hypnotics, antidepressants, phenothiazines, neuroleptics, anesthetics, muscle relaxants, antihistamines and antiemetics.

Monoamine oxidase inhibitors (MAOIs) and oxycodone should be administered with caution. This also applies to patients who have received MAOIs in the past two weeks.

Concomitant use of oxycodone and alcohol should be avoided.

The anticholinergic side effects of oxycdone, e.g. Other drugs with an anticholinergic effect may exacerbate them, such as constipation and dry mouth.

CYP3A4 inhibitors

CYP3A4 inhibitors can reduce the clearance of oxycodone. The resulting increase in the plasma concentration of oxycodone may have to be countered by adjusting the dose.

The CYP3A4 inhibitors include:

CYP3A4 inducers

CYP3A4 inducers may increase the clearance of oxycodone. Here, too, the oxycodone dosage may have to be adjusted to avoid a reduction in the plasma concentration.

CYP3A4 inducers include:

CYP2D6 inhibitors and other inhibitors of the cytochrome system

CYP2D6 inhibitors, such as paroxetine and quinidine, can reduce clearance and thus increase the plasma concentration of oxycodone.

To what extent the metabolism of oxycodone is influenced by other relevant isoenzyme inhibitors of the cytochrome system is unclear. Possible interactions should be considered.

In rare cases, there has been a clinically relevant decrease or increase in the International Normalized Ration (INR) with simultaneous use of oxycodone and coumarin-based anticoagulants.

Contraindication

Hypersensitivity to oxycodone or any of the other ingredients of the drug in question is a contraindication.

Furthermore, oxycodone must not be used in situations where opioids are contraindicated. Which includes:

  • Severe respiratory depression with hypoxia and / or hypercapnia
  • Severe chronic obstructive pulmonary disease
  • Cor pulmonale
  • Severe bronchial asthma
  • Paralytic ileus
  • Acute abdomen
  • Delayed gastric emptying.

Pregnancy / lactation

The use of oxycodone during pregnancy and breastfeeding should be avoided as much as possible, as it can lead to respiratory depression and withdrawal symptoms in newborns and infants.

In animal studies, oxycodone did not show any negative effects on fertility. Human data are not available.

Ability to drive

Oxycodone can change alertness and the ability to react to such an extent that active participation in road traffic or the use of machines is impaired or no longer permitted.

A general driving ban is not absolutely necessary for patients with stable therapy. The assessment must be made individually by the attending physician.

Further details on this active ingredient can be found in the relevant information for professionals.

Active ingredient information

Product information Oxycodon-HCl AbZ 10 mg prolonged-release tablets, Product information Oxycodon-HCl-CT 10 mg prolonged-release tablets