Oxymorphone: Characteristics, Side Effects And Precautions
Oxymorphone is an analgesic type drug Prescribed especially for chronic pain. It is not considered one of the main avenues of treatment for pain and, since it is an opioid, treatments with this medication are very controlled.
Below we are going to see in more detail the pharmacological properties of this medication, what it is used for, what its side effects are, precautions to take if consumed and the effects of its overdose.
Oxymorphone, whose chemical formula is C17H19NO4, is an opioid pain reliever, marketed under the brand names Numorphan, Numorphone and Opana It is used to relieve moderate and severe pain in people in whom other pain-reducing drugs have had no effect. Oxymorphone is also indicated as a treatment for acute post-surgical pain.
Normally, non-pharmacological agents and non-opioids are used as the first option for chronic pain, since opioids pose serious dangers. For any chronic pain treatment, long-term use should only be considered if there are significant clinical benefits that outweigh the risks. The first-line treatment options for chronic pain are non-pharmacological agents and non-opioids, that is, oxymorphone would not be one of the first options since it is an opioid.
This drug was originally designed in Germany in 1914 and was patented in 1955, and its medical use was approved in 1959. It is a highly addictive drug, which has rarely been the subject of debate The US Food and Drug Administration (FDA) in 2017 asked the manufacturer to withdraw the product from the market, especially concerned about the consumption of opioids in North American society.
Pharmacokinetics and pharmacodynamics
Its oral bioavailability is 10%, and intranasal is 43%. Its metabolism is hepatic, through glucuronidation and cytochrome CYP3A. Its half-life in the body is 7 to 9 hours and is excreted in urine and feces. Its routes of administration are oral, intravenous, intramuscular, subcutaneous, rectal and intranasal.
The mechanism of action of oxymorphone consists of activating the μ-opioid receptor and, to a lesser extent, the δ-opioid and κ-opioid receptors. The activity of oxymorphone appears to be 10 times greater than that of morphine.
Its administration can be done in several ways. If it is done by injection, its effects on pain relief begin shortly after approximately between 5 and 10 minutes, and 15 to 30 minutes after rectal administration, its effects lasting approximately between 3 and 4 hours for immediate-release tablets and 12 hours for slow-release tablets.
Slow-release tablets, administered orally, are the most common. It is advisable to consume it orally, at least one or two hours after meals. Generally, pills are taken every 4 or 6 hours. It is very important to take this drug as prescribed by the doctor, without taking more or less than the prescribed amount or increasing the frequency indicated by the doctor. The tablet should be swallowed, without being chewed or crushed.
It is common that when starting treatment with oxymorphone, the first doses are low and are gradually increased until the pain is controlled. In case the medicine is not working, The doctor will be in charge of adjusting the dose and it should never be the patient who takes the liberty of increasing or reducing it
If you miss a dose, you should take that dose as soon as you remember. However, if the missed dose is remembered just shortly before it is time to take the next dose, it is recommended to skip the missed dose and continue with the regular dosing schedule. The dose should not be doubled to make up for a missed dose
Side effects
Oxymorphone, like any other drug, can cause side effects, either due to a too high dose of the medication or to characteristics of the patient’s body that consumes it that has caused such symptoms to occur. Between the most common side effects What we can find we have:
Some of these side effects may not go away and may even increase their medical severity If these symptoms appear, the doctor should be kept informed. However, the following symptoms are considered more serious and, if they appear, you should urgently seek medical advice.
In addition to these effects, There is the possibility of developing dependence on the medication, fertility problems in both men and women, and constipation In the latter case, it is possible that some changes will have to be included in the diet to facilitate defecation, although it is normal that this symptom does not appear and it is not recommended to change the diet as soon as treatment begins unless the doctor so advises. has explicitly said.
Among the symptoms of oxymorphone overdose we have:
In the event of an overdose, it will be necessary to call emergency services while a family member or acquaintance takes care of the patient, especially if he has collapsed to the ground, has a seizure, has trouble breathing, or cannot wake up. Normally, to avoid these situations, it is recommended to have on hand the antidote for oxymorphone, naloxone, a drug that works by blocking the effects of opiates, reducing their dangerous effects.
Overdose symptoms may return within a few minutes after taking naloxone. If these symptoms recur, the person should take another dose of naloxone. Additional doses may be given every 2 to 3 minutes if symptoms return before medical help arrives.
Abstinence syndrome
It’s very important follow the doctor’s guidelines and do not take the liberty of stopping the drug without telling him or her, since, if you do it abruptly, there is a risk of the effects of withdrawal syndrome occurring. Among the symptoms of this oxymorphone syndrome we have.
Concern
Crying eyes
Runny nose
yawns
Sweating
Shaking chills
Muscle, joint and/or back pain
Dilated pupils
Irritability
Anxiety
Weakness
Stomach cramps
Difficulty falling asleep or staying asleep
Nausea, vomiting
Diarrhea
Loss of appetite
Tachycardia
Fast breathing
Precautions
There are several precautions that must be taken into account if treatment with oxymorphone is to be started, just like any other drug. Below we will see the main ones.
1. Allergies
In case it is known, It will be necessary to tell your doctor or pharmacist if you are allergic to oxymorphone and related drugs including oxycodone, codeine, hydrocodone, dihydrocodeine, hydromorphone or any other medication.
2. Interactions
Interactions may occur with other drugs, with which it will be necessary to inform the doctor that you are taking another medication if this is the case, in addition to indicating the dose and frequency. It is also important to inform them whether they are prescription or non-prescription, also including vitamins, nutritional supplements and herbal medicine.
The main medications with which it can interact are: antihistamines; buprenorphine, butorphanol, cimetidine, diuretics, ipratropium, medicines for irritable bowel disease, for motion sickness, for Parkinson’s disease; or for urinary problems; nalbuphine and pentazocine.
It will be necessary to report the following health problems before starting treatment with oxymorphone: obstruction in the stomach or intestines, paralytic ileus, seizures, difficulty urinating, kidney disease, liver disease, thyroid disease, or gallbladder problems.
4. Respiratory problems
Oxymorphone can cause serious respiratory problems, especially during the first 72 hours after starting treatment or at any time when the dose of the drug is increased. For this reason, special caution should be taken in patients with respiratory problems, such as asthma, chronic obstructive pulmonary disease and sleep apnea.
5. Special populations
Patients who have already suffered some type of debilitating illness are more prone to respiratory depression In this type of population, the prescription of non-opioid analgesics should be considered.
Older patients are more sensitive to adverse effects, such as falls, cognitive decline, and constipation. Decreased kidney function associated with aging can increase the harms of this drug, especially its overdose. If it is the only drug that can be prescribed in this population, it is recommended to prescribe low doses when starting treatment.
There is a risk that the baby may be affected if the pregnant woman has taken the drug for a long time. Oxymorphone crosses the placenta and can involve damage at birth, as well as poor fetal growth and premature birth. Children of mothers who are physically dependent on the drug are more likely to develop that same dependence.
6. Machinery handling
Oxymorphone may cause drowsiness, dizziness, or lightheadedness, so It is not recommended to operate heavy machinery after taking the drug Dizziness can appear just by getting up from lying down, so it is recommended to rest your feet on the floor for a few minutes before standing up.
Hussain MA, Aungst BJ (August 1997). Intranasal absorption of oxymorphone. Journal of Pharmaceutical Sciences 86 (8): 975-6. PMID 9269879. doi:10.1021/js960513x.
Davis, M.P.; Glare, PA; Hardy, J (2009). Oxford University Press, ed. Opioids in Cancer Pain (2nd edition). Oxford, UK. ISBN 978-0-19-157532-7.
