Suboxone (buprenorphine and naloxone) is a drug used to treat opiate addiction. It was produced in 2002 and it has been used for opioid replacement as it was methadone. It has the buprenorphine and naloxone in 4:1 ration. It acts on mu-opioid receptors (MOR) as a partial agonist. It can affect kappa and delta receptors too (KOR and DOR) on which he acts as an antagonist. It produces the state of being “high” which is followed up by elevated mood (euphoria), pleasure, relaxation and CNS depression.
It is considered an addictive drug due to its ingredient buprenorphine. It can lead to severe symptoms after withdrawal and it can provoke vomiting, nausea, depression, dizziness. There are also some long-term effects such as downregulation of endorphins. Some of the people on this drug are trying to quit, and these are the things you should now if you want to eliminate it from your system.
How Long Does Suboxone Stay In Your System?
The main property of the drug effect duration is the half-life. Since this drug contains two active ingredients, it is important to know the half-life of both substances in the Suboxone. The half-life of buprenorphine is about 37 hours which is a long period of elimination. It is approximately 2 days to excrete half of the buprenorphine in your system. If we consider just the buprenorphine, the drug clearance can take up to 8.48 days. The half-life of naloxone is much faster, between half an hour and 1 hour and 21 minutes. It can leave the system within 8 hours of intake which is faster than the buprenorphine. Even if the naloxone gets excreted, the buprenorphine effects act longer and can also exceed 37 hours and last longer than that. Some of the metabolites of buprenorphine (norbuprenorphine) stay in the system for longer than 9 days which can last up to 2 weeks after the last dosage of the drug.
Factors Which Can Influence Suboxone Elimination
There are numerous factors which can influence the Suboxone elimination. Among those is the dosage of the drug, individual factors, frequency, interaction with other drugs. While someone can clear the system from its metabolite under 9 days, it may not be the same for all. Some will take a longer period to get that done.
Among individual factors, there are many that can influence the drug elimination. Even if two persons have the same drug at the same time of the day, they can have different time of elimination, i.e., the half-life of the drug. This has to do with the person’s age, urinary pH, hydration, BMI, genetics, lifestyle.
There are no proven facts that elderly people have differences when compared to younger people when it comes to absorption, distribution and metabolism. Even though, this doesn’t mean that the elderly don’t have a slower metabolism in general which will work at a slower pace and excrete slowly. They have reduced circulation through kidneys and liver which can also be followed up with some organ problems and other health issues.
Body mass index, including body weight, height, and fat percentage have an impact on the Suboxone elimination. The dosage is linked with the body weight where persons take larger amounts of the drug for a greater body mass. The higher the dosage, the longer the time of elimination. Suboxone is a liposoluble drug which means it has a tendency of lipid accumulation. If a person has a higher fat percentage, it is more likely it is going to concentrate in the body lipids and create the depository. The more buprenorphine is stored in the system, the longer the drug effects will last.
Hydration is the key for kidney excretion. So is when it comes to Suboxone elimination. The clearance will be quicker when you take enough fluid to promote circulation flow through kidneys. Dehydration will lead to drug absorption which can result in prolonged effects and time of clearance.
Liver And Kidney Function
It is crucial to have functional liver and kidneys in order to metabolize and excrete the product from the system. Hepatic diseases such as cirrhosis or hepatitis can cut down the active cells which will metabolize the drug and it will lead to greater amount of active drug in the system. It will lead to reduced function of CYPA4 enzymes in the liver and slow Suboxone clearance. The same goes when it comes to kidneys. If any renal dysfunction happens, it can lead to drug retention and prolonged clearance.
Some persons have genes which promote enzyme synthesis and their function. These people are called fast metabolizers. On the other hand, there are people whose enzymes work at a slower pace and it will result in a poor metabolism.
Urinary pH can have an impact if it changes on one side or the other. Having alkaline urine will prolong the Suboxone elimination. Acidic urine can influence on Suboxone elimination in a way it can promote its clearance. Alkaline urine can extend the half-life of the Suboxone by a few hours which can have a significant impact on the drug excretion.
The dose can alter the drug effectiveness where the higher dose will act for a longer period and it will stay in the system for a longer time. The lower the dosage, the faster the excretion of the Suboxone. As we mentioned above, Suboxone has a ratio of 4:1 of buprenorphine and naloxone. There are a few types of therapies including several doses:
- Lowest dose: 2 mg/0.5 mg
- Normal dose: 4 mg/1 mg
- Moderate dose: 8 mg/2 mg
- High dose: 12 mg/3 mg
- Highest dose: 24 mg/6 mg.
Those who are taking smaller doses such as 2 mg/0.5 mg are going to clear their system faster in compared to those who take highest doses of 24 mg (buprenorphine)/6 mg (naloxone). The buprenorphine will accumulate in the fat tissue and it will create deposit which will affect the body further on. The higher the dose, the more burden goes to the liver which has to work in an altered manner to metabolize all the drug which is in the system. It can lower the enzyme function which is not enough for drug elimination.
Another thing which can be linked with the high dose is the greater amount of metabolites that remain in the system after the drug metabolism. They can circulate the system and prolong the body clearance.
Frequency Of Use And Time Span
It is important to state the frequency of use were the ones having multiple drugs per day will have a higher concentration in the system which will lead to longer elimination. Infrequent users will take once per day or maybe even less often. Sublingual forms are for once a day intake. Some patients don’t follow the doctor’s instructions and take more or less than prescribed. This can lead to Suboxone accumulation and slower clearance of the body. Those who do not intake such quantity in a day or “as needed” will not accumulate the amount of the Suboxone in the body for it to slow down the clearance.
Interaction With Drugs
When taking certain medication simultaneously with Suboxone, it can have an impact on its clearance. The drugs can act as an inhibitors or inducers where it can promote or reduce the potential of excretion. The drugs affecting the enzymes in the liver (especially CYP3A4 which are used for the Suboxone) can affect the liver function. Inhibitors can prolong the clearance were among those are Clarithromycin, Chloramphenicol, Ritonavir, Indinavir, Ketoconazole, Nefazodone.
Inducers can promote Suboxone elimination and enhance CYP3A4 isoenzyme expression in the liver which will eventually lead to a faster metabolism. Those medications are Phenobarbital, Rifampicin, Carbamazepine, Glucocorticoids, Oxcarbazepine, Modafinil, etc. It can shorten the half-life of the medication and end up in faster clearance.
It is being produced in tablets and films which are sublingual forms of medication. It goes under your tongue and into the bloodstream. It is quickly absorbed and it will express its effects from 40 minutes to 3.5 hours after the drug intake. It is bound to the proteins in the bloodstream and it goes into the liver. It converts into its metabolites and buprenorphine becomes “norbuprenorphine” which can also be pharmacologically active as 20% of the active product. It goes through glucuronidation and gets excreted. The half-life of buprenorphine is between 20 and 73 hours. Some will excrete it for a shorter or longer time, between 4.58 to 16.72 days after the last dosage. It can stay in your system for a longer, depending on many factors.
Naloxone goes through glucuronidation and becomes naloxone-3-glucuornide (N3G). Its half-life is between 30 minutes and hour and 21 minutes which can be excreted within 5.5 to 14.9 hours after the last dose. About 40% of the drug is excreted within the first 6 hours after the last dose, and up to 70% after 72 hours of ingestion.
Tips For Faster Suboxone Clearance
You can start by applying some tips to your everyday life which can promote Suboxone clearance and help with its elimination. This may not help everyone and it can vary from person to person.
Cut The Use
Stop using Suboxone. This is the first step. This will ensure that your body will start to eliminate the leftovers from the body to a complete excretion from the system. It can be longer or shorter, depending on many factors which we mentioned.
If you take enough liquids, you will promote circulation and blood flow through kidneys which will help with drug excretion and blood flow through the liver. It is important to stay hydrated since dehydration will lead to reabsorption in the kidneys and will promote drug accumulation.
Doing some cardio and aerobic exercises can benefit your body and help with drug elimination. If you exercise, you will burn fat which will be likely for you to accumulate the drug inside the fat storage and you will work on your circulation flow which will benefit the function of the kidneys and the liver.
Taking the drugs which are CYP3A4 inducers can accelerate the drug metabolism. When taking simultaneously with the Suboxone, it can affect the half-life of the drug and affect its elimination from the system.