Management of pain is one of clinical medicine’s greatest challenges. Before going into details of methadone have some discussion on pain which is defined as an unpleasant sensation that can be either acute in onset or have a long history and results from various and complex neurochemical processes in the central and peripheral nervous system. Pain can be neuropathic or nociceptive and for neuropathic pain, opioids are the best option.
What are opioids?
Opioids are natural, semi-synthetic, or synthetic compounds that produce morphine-like effects and they are divided into different chemical classes based on their chemical structure.
How do opioids work?
All opioids work by binding to specific opioid receptors in the central and peripheral nervous system that mimic the action of special neurotransmitters involved in pain management like endorphins, dynorphins, and enkephalins.
Visit To Buy More Products:
- Buy tramadol
- Buy soma gen carisoprodo
It is a strong opioid agonist and is a synthetic orally effective opioid that mediates its action by binding to the mu receptor. Sold under the brand names Methadose, Dolophine, Amidone, Symoron, Metadon, Metadol, etc.
Made in Germany in 1937 and 1947 methadone name was given. It was introduced in 1947 in the United States.
Being less expensive it costs up to 2 dollars.
- Highly efficacious in the treatment of nociceptive and neuropathic pain.
- Used to manage withdrawal of dependant abusers from opioids and heroin.
Depends upon either taking for pain management or opioid dependence and is available in powder, tablet, or liquid forms.
Opioid dependence: 20 to 30 mg are prescribed to be taken by mouth.
Chronic pain: Up to 5mg by mouth every 7 to 10 hrs depending upon intensity and frequency of pain.
Pharmacodynamics: Along with the action on the mu receptor, it has an antagonist effect on the N-methyl-D-aspartate receptor and serotonin reuptake inhibition.
Pharmacokinetics: Following oral administration, it gets readily absorbed and gets biotransformed in the liver, and excretion takes place mostly through feces. Due to its lipid-soluble property, it accumulates in the fat tissue.
Half-life: Ranges from 13 to 40 hrs and the time frame to reach a steady-state range from 30 hrs to 2 weeks.
Other opioid agonists: Strong agonists: Alfentanil, morphine, fentanyl, oxycodone, remifentanil and sufentanil.
Moderate agonist: Codeine.
Why it is better than morphine?
It can produce physical dependence like that of morphine but has less neurotoxicity than morphine due to a lack of active metabolites.
Why monitor it?
As it has a high addiction and overdose potential so continuous monitoring is essential.
- Has a long duration of action.
- Induces less euphoria.
- Produces less neurotoxicity.
- Has less physical dependence than other opioids.
- Available at a lower cost.
- Used in the controlled withdrawal of dependant abusers from opioids and heroin.
- Used to manage severe pain.
- Has no active metabolites.
- This leads to prolongation of QT interval and causes torsades de pointes due to interaction with cardiac potassium channels.
- Duration to produce an analgesic effect is much shorter than the elimination half-life and repeated dosing can leads to accumulation and overdosage.
- Contraindicated in pregnancy as it crosses the blood-placental barrier and leads to a condition in which the baby becomes dependent on it.
- Causes respiratory depression so contraindicated to use in patients having respiratory problems.
- This leads to constipation and stool softeners are prescribed along with this.
Points to ponder:
- Not to stop it immediately as it leads to withdrawal symptoms like lightheadedness, photophobia, tremors, depression, etc.
- As the duration of analgesia is much shorter so repeated dosing can lead to accumulation and overdose situations.
- Causes dizziness so activities like driving, doing surgeries, etc are avoided.
Having more positive aspects as compared to negative aspects it is safe to use and has more efficacy than other drugs in this class. Well, that was all. Hopefully, this brief article will help you a lot.
There are no reviews yet.