Have you ever taken a prescription drug labeled “extended-release?”
Unlike an immediate-release drug, an extended-release drug has a slow drug release rate. That means it enters your system gradually throughout the day, which reduces the risk of overdose and allows you to take the drug less frequently.
The most common types of extended-release drugs are extended-release opioids.
If you take an extended-release drug with alcohol (also called ethanol) or certain foods, you may experience a phenomenon called “dose dumping.”
What Is Dose Dumping?
Dose dumping occurs when an extended-release drug enters the body too quickly. This rapid release can happen with any extended-release oral dosage form, including pills, tablets, capsules, and liquid solutions.
There are two main forms of dose dumping: alcohol-induced dose dumping and food-induced dose dumping.
Alcohol-Induced Dose Dumping
In an extended-release drug delivery system, drug release is controlled by a polymer matrix or polymer film coating.
These controlling agents often dissolve in the presence of alcohol. That’s because alcohol is a solvent, and most polymers have high solubility. The resulting dissolution can cause alcohol-induced dose dumping (AAID).
To reduce the risk of AAID, the United States Food and Drug Administration (FDA) recommends in vitro dissolution testing for all extended-release formulations.
It also recommends that people who are taking certain extended-release drugs avoid the consumption of alcoholic beverages, especially those with high alcohol concentrations.
AAID first gained attention in 2005, thanks to the drug Palladone.
Palladone was an extended-release formulation of the opioid analgesic (painkiller) hydromorphone. It contained highly soluble release-controlling polymers that dissolved in the presence of alcohol. Because the drug caused various cases of AAID, the FDA discontinued it.
Food-Induced Dose Dumping
Like alcohol, some foods (especially fatty foods like meat and dairy) can damage a drug’s release-controlling polymers. They can also speed up drug absorption by stimulating the body’s absorptive surfaces.
Both of these effects can cause dose dumping. Dose dumping may also occur when food causes pH variability in the gastrointestinal tract.
One of the most popular drug products linked to food-induced dose dumping is the controlled-release dosage form of theophylline.
Meant to be taken once a day, this medication treats asthma and other lung issues. It should be taken on an empty stomach to prevent dose dumping.
Dangers Of Dose Dumping
The most common negative effects of alcohol or food-induced dose dumping include:
One of the main advantages of extended-release medications is that their effects last a long time. That’s why, in most cases, you only need to take an extended-release tablet once or twice a day. Dose dumping removes this benefit because it makes the drug’s effects wear off more quickly.
Increased Risk Of Overdose
An extended-release delivery system ensures that a drug’s active pharmaceutical ingredient (API) and excipients (substances that support the drug’s stability, bioavailability, bioequivalence, and biopharmaceutical characterization) stay at a therapeutic level in the blood.
With dose dumping, API and excipient levels can increase to the point of toxicity or overdose, especially if the drug is an opioid (such as oxycodone, hydrocodone, or fentanyl). Common signs of overdose include:
- nausea and vomiting
- anxiety or irritability
- change in pupil size
- sudden change in body temperature
- chest pain
- slow or irregular heartbeat
- slow, shallow, or irregular breathing
- loss of consciousness
If you or someone you know experiences these symptoms, seek emergency health care services right away. When left untreated, an overdose can be fatal.
Increased Side Effects
Since dose dumping makes a drug enters your system so rapidly, it can increase the risk of side effects. It can also make the side effects more severe.
Side effects vary among different extended-release medications. Common side effects of extended-release opioids include:
The Fight Against Dose Dumping
Researchers specializing in pharmacokinetics (the study of how drugs move through the body) have conducted a number of clinical trials to identify extended-release medications with physicochemical properties that reduce the risk of dose dumping.
For example, researchers have found that extended-release matrix tablets (which are made with hydrophilic polymers) pose a very low risk of alcohol-induced dose dumping compared to other extended-release tablets.
In addition, researchers can test a drug’s potential for food-induced dose dumping by conducting in vivo food effect studies. These studies determine how food impacts drug absorption. They allow the FDA to issue warnings for drugs that pose a high risk of dose dumping.
If you or someone you love struggles with drug abuse, please contact us today.