PENTAZOCINE

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Created Dec 2020

PENTAZOCINE

  • [TALWIN]
  • [TALWIN NX]
  • [TALACEN]
  • [TALWIN COMPOUND]

DEA CODE 9709: Schedule 4

Pentazocine is a generic drug, sold under the brand name Talwin as well as other trade names, prescribed to treat moderate to severe pain. Pentazocine is a unique drug in that it activates certain opioid receptors while blocking others. Because pentazocine activates some opioid receptors as a way to relieve pain, it is classified as an opioid.

The side effects of pentazocine are similar to other opioids. For example, side effects can include nausea, vomiting, constipation, itching or drowsiness. However, unlike many other opioids, Pentazocine can also cause hallucinations, bad dreams and delusions. What's unique about Pentazocine along with these side effects is the ceiling effect. Once someone reaches a certain dose, pentazocine doesn't provide any more pain relief or side effects. So, even if someone were to use a high dose of pentazocine to get high, there would be a ceiling on the potential effects. The ceiling effect in pentazocine is because naloxone is included with the formulation. If someone tries to crush or break the medication in any way, the naloxone prevents misuse. If pentazocine is taken as prescribed and used orally, the naloxone shouldn't have any effect. While pentazocine acts on brain receptors to provide pain relief, naloxone helps prevent the misuse of the drug. For this reason, pentazocine's official name is pentazocine-naloxone.

Talwin-NX:

  • Talwin is an analgesic (pain reliever) which contains the narcotic active ingredient called pentazocine. Talwin injectable contains 30mg of pentazocine (as lactate) per ml. In tablet form it is known as "Talwin-NX". The "NX" stands for naloxone. These tablets contain 50mg of pentazocine and 0.5mg of naloxone. Naloxone is added to the formulation to prevent drug abuse. If someone were to consume a high dose of Talwin-NX, the naloxone would kick in and reverse the effects of the pentazocine and cause a withdrawal response.

History:

Pentazocine Wasn't Non-Addictive as Originally Believed:
As a power pain killer, pentazocine was originally introduced to the public fifty years ago with great expectations. The medical community was excited about it due to it's positive effects against pain and its non-habit forming qualities. It was the replacement for morphine as a non-addictive treatment in helping those with chronic pain. As morphine had a reputation of being highly addictive and misused, pentazocine seemed like the perfect solution to a long occurring problem. The thought was that those who suffered from chronic pain weren't at risk of addiction. The medical field was convinced they didn't have to lock up pentazocine and it was placed in accessible aid kits fallout shelters. They believed it was non-addictive and not in jeopardy of being stolen by street addicts. Unfortunately, all the hype on the safety of this new pain killer was just hypothetical as four years later, scientists were focusing their studies on Pentazocine addiction risk and abuse.

About 38 mg of Pentazocine is considered to be the equivalent of 10 mg morphine, it begins working within 20 minutes and peaks at about 90 minutes.

Pentazocine, the Poor Man's Heroin:
Known as T's and blues, the combination of pentazocine and tripelennamine, was being abused as a heroin substitute. In the late 70's and early 80's, it gained popularity on the streets due to the low quality of heroin being sold at the time. The statistics on the toll it took on people on the streets include people dying violently from toxic shock. In fact, thousands of people became addicted to Pentazocine both in the U.S. and Europe. Pentazocine and Ritalin were combined and named the "Poor Man's Heroin," which gave people a high much like speedball which is a combination of cocaine and heroin. Antihistamines were combined with Pentazocine as well that would bring a kind of euphoria to the user. Heroin is a highly addictive substance so when a prescription drug can cause a similar high, it should be considered a very risky drug to prescribe.

Why Naloxone was Added to Pentazocine
The Pentazocine-Naloxone mixture was introduced as a way of counteracting the abuse surrounding Pentazocine. As it's an opioid pain medication and Naloxone blocks opioids from getting to the brain, it was thought to be the right combination to prevent abuse and addiction risk.

How does it work?
Pentazocine is a type of medicine called an opioid painkiller. Opioid painkillers such as pentazocine that work by mimicking the action of naturally occurring pain-reducing chemicals called endorphins. Endorphins are found in the brain and spinal cord. Pentazocine mimics the action of endorphins by combining with the opioid receptors in the brain and spinal cord. This blocks the transmission of pain signals sent by the nerves to the brain. Therefore, even though the cause of the pain may remain, less pain is actually felt. Pentazocine is used to relieve moderate to severe pain.

Uses:
This product is used to treat moderate to severe pain. It contains 2 medications, pentazocine and naloxone. Pentazocine is a narcotic pain reliever (opiate-type). It acts on certain centers in the brain to give you pain relief. Naloxone helps to prevent misuse of this product. It blocks the effect of pentazocine and may cause withdrawal reactions if this product is dissolved and injected. Naloxone does not have any effect when taken by mouth.

Warning:
This medication should only be taken by mouth. Do not try to dissolve and inject the tablets. Injecting this product, alone or with other substances, may cause serious, possibly fatal, side effects.

Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic (opioid analgesic) drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain. Pentazocine is sold under several brand names, such as Fortral, Sosegon, Talwin NX. This compound may exist as one of two enantiomers, named (+)-pentazocine and (−)-pentazocine. Side effects are similar to those of morphine, but pentazocine, due to its action at the kappa opioid receptor is more likely to invoke psychotomimetic effects. High dose may cause high blood pressure or high heart rate.

Prescribed for:
  • Pain

Used for:
This product is used to treat moderate to severe pain. It contains 2 medications, pentazocine and naloxone.

  • Pentazocine is an opioid pain reliever. It acts on certain centers in the brain to give you pain relief.
  • Naloxone helps to prevent misuse of this product. It blocks the effect of pentazocine and may cause withdrawal reactions if this product is dissolved and injected. Naloxone does not have any effect when taken by mouth.

Before using:
Tell your doctor or pharmacist your medical history, especially of:

  • Brain disorders (such as seizures, head injury, tumor)
  • Breathing problems (such as asthma, sleep apnea, chronic obstructive pulmonary disease-COPD)
  • Gallbladder disease
  • Heart problems (such as irregular heartbeat, recent heart attack)
  • Kidney disease
  • Liver disease
  • Mental/mood disorders (such as confusion, depression, thoughts of suicide)
  • Personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol)
  • Stomach/intestinal problems (such as blockage, constipation, diarrhea due to infection, paralytic ileus)
  • Disease of the pancreas (pancreatitis), difficulty urinating (such as due to enlarged prostate)
  • Certain blood disorder (porphyria)

Precautions:

  • This drug may make you dizzy or drowsy.
  • Alcohol or marijuana (cannabis) can make you more dizzy or drowsy.
  • Do not drive, use machinery, or do anything that needs alertness until you can do it safely.
  • Avoid alcoholic beverages.
  • Talk to your doctor if you are using marijuana (cannabis).

WARNINGS:

Pentazocine has a risk for abuse and addiction, which can lead to overdose and death.

Pentazocine may also cause severe, possibly fatal, breathing problems.

To lower your risk, your doctor should have you take the smallest dose of pentazocine that works, and take it for the shortest possible time.

The risk for severe breathing problems is higher when you start this medication and after a dose increase, or if you take the wrong dose/strength.

Taking this medication with alcohol or other drugs that can cause drowsiness or breathing problems may cause very serious side effects, including death.

Be sure you know how to take this medication and what other drugs you should avoid taking with it. Get medical help right away if any of these very serious side effects occur: slow/shallow breathing, unusual lightheadedness, severe drowsiness/dizziness, difficulty waking up.

This medication should only be taken by mouth. Do not try to dissolve and inject the tablets. Injecting this product, alone or with other substances, may cause serious, possibly fatal, side effects.

User Reviews:

39 Total User Reviews
Pentazocine Naloxone Oral:
Read Reviews
Condition: Pain (39 Reviews):
Effectiveness(2.56)

Ease of Use(3.23)

Satisfaction(2.13)

Liver:
Pentazocine has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.

Pentazocine Hepatotoxicity:
Therapy with pentazocine has not been linked to serum enzyme elevations or to idiosyncratic acute, clinically apparent liver injury.

Interactions:

Drug Interactions (392) Alcohol/Food Interactions (2) Disease Interactions (15)


What other drugs will affect Pentazocine?

A total of 392 drugs are known to interact with Pentazocine.

  • 140 major drug interactions
  • 251 moderate drug interactions
  • 1 minor drug interaction

Drug Interactions:
Some products that may interact with this drug include:

  • Fluoxetine
  • Naltrexone
Taking MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Avoid taking MAO inhibitors (isocarboxazid, linezolid, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before treatment with this medication. Ask your doctor when to start or stop taking this medication.

Cigarette smoking decreases blood levels of this medication. Tell your doctor if you smoke or if you have recently stopped smoking.

Talacen (pentazocine and acetaminophen tablets)
Side Effects:
Nausea, vomiting, constipation, lightheadedness, dizziness, drowsiness, increased sweating, or dry mouth may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
RxList
To prevent constipation, maintain a diet adequate in fiber, drink plenty of water, and exercise. Consult your pharmacist for help in selecting a laxative (such as a stimulant type with stool softener).
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as agitation, hallucinations, confusion), difficulty urinating, vision changes, fast heartbeat, change in the amount of urine, signs of infection (such as fever, persistent sore throat), easy bruising/bleeding.
Get medical help right away if you have any very serious side effects, including: fainting, slow/shallow breathing, seizures.
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
In the US - Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Maximum Dosage:

Talwin (pentazocine)
Maximum Dosage:
Prescribers Digital Reference
Adults:360 mg/day IV/IM/SQ, not to exceed 30 mg/dose IV or 60 mg/dose IM/SQ.
Geriatric:360 mg/day IV/IM/SQ, not to exceed 30 mg/dose IV or 60 mg/dose IM/SQ.
Adolescents:17 years: 360 mg/day IV/IM/SQ, not to exceed 30 mg/dose IV or 60 mg/dose IM/SQ.
Adolescents:< 17 years: 0.5 mg/kg IM (up to 30 mg) x1 dose.
Children:0.5 mg/kg IM (up to 30 mg) x1 dose.
Infants:Safety and efficacy have not been established.
Neonates:Safety and efficacy have not been established.

Pentazocine
Duration:

A synthetic opioid used as an analgesic. It is only used IM and IV in the medical field and has respiratory depressant effects.

RouteOnsetDurationAfter Effects
Tripsit Factsheets
IM:15-20 minutes2-3 hours1-12 hours
IV:2-3 minutes2-3 hours1-12 hours
Pentazocine Duration
Avoid:
All other CNS depressants
Warning:
When mixed with a barbituate in a syringe it will crystallize which can be fatal.

Pediatric:
Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of pentazocine injection in children 1 to 16 years of age.

Safety and efficacy have not been established in children younger than 1 year of age.

Geriatric:
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of pentazocine injection in the elderly. However, elderly patients may be more sensitive to the effects of pentazocine injection than younger adults, and are more likely to have age-related kidney problems, which may require caution and an adjustment in the dose for patients receiving pentazocine injection.

Other Interactions:

  • Ethanol

Other Medical Problems:
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Adrenal problems
  • Alcohol abuse, or history of
  • Allergy to sulfites
  • Breathing problems, severe (eg, COPD, hypercapnia, hypoxia)
  • Cor pulmonale
  • Depression, history of
  • Drug dependence, especially with narcotics, or history of
  • Head injuries, history of
  • Mental health problems
  • Weakened physical condition - Use with caution. May increase risk for more serious side effects
  • Asthma, severe
  • Respiratory depression (very slow breathing)
  • Stomach or bowel blockage (eg, paralytic ileus) - Should not be used in patients with these conditions
  • Heart attack, recent
  • Heart failure
  • Hypertension (high blood pressure)
  • Seizures, history of - Use with caution. May make these conditions worse
  • Kidney disease
  • Liver disease - Use with caution. The effects may be increased because of slower removal of the medicine from the body

Breastfeeding:

Summary of Use During Lactation:
No information is available on the use of pentazocine during breastfeeding.

Maternal use of oral narcotics during breastfeeding can cause infant drowsiness, central nervous system depression and even death.

Newborn infants seem to be particularly sensitive to the effects of even small dosages of narcotic analgesics. Once the mother's milk comes in, it is best to provide pain control with a nonnarcotic analgesic and limit maternal intake of pentazocine to a few days at a low dosage with close infant monitoring.

If the baby shows signs of increased sleepiness (more than usual), difficulty breastfeeding, breathing difficulties, or limpness, a physician should be contacted immediately.

Other agents are preferred over pentazocine during breastfeeding.

Effects on Lactation and Breastmilk:

Pentazocine can increase serum prolactin.

However, the prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Alternate Drugs to Consider:

What is the most important information I should know about naloxone and pentazocine?
  • MISUSE OF OPIOID MEDICINE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH. Keep the medication in a place where others cannot get to it.
  • Taking opioid medicine during pregnancy may cause life-threatening withdrawal symptoms in the newborn.
  • Fatal side effects can occur if you use opioid medicine with alcohol, or with other drugs that cause drowsiness or slow your breathing.

What should I watch for while using this medicine?
Tell your doctor or health care professional if your pain does not go away, if it gets worse, or if you have new or a different type of pain. You may develop tolerance to the medicine. Tolerance means that you will need a higher dose of the medicine for pain relief. Tolerance is normal and is expected if you take the medicine for a long time.

Do not suddenly stop taking your medicine because you may develop a severe reaction. Your body becomes used to the medicine. This does NOT mean you are addicted. Addiction is a behavior related to getting and using a drug for a non-medical reason. If you have pain, you have a medical reason to take pain medicine. Your doctor will tell you how much medicine to take. If your doctor wants you to stop the medicine, the dose will be slowly lowered over time to avoid any side effects.

If you are also taking a narcotic medicine for pain or cough or another medicine that also causes drowsiness, you may have more side effects. Give your health care provider a list of all medicines you use. Your doctor will tell you how much medicine to take. Do not take more medicine than directed. Call emergency for help if you have problems breathing or unusual sleepiness.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

This medicine will cause constipation. Try to have a bowel movement at least every 2 to 3 days. If you do not have a bowel movement for 3 days, call your doctor or health care professional.

Your mouth may get dry. Chewing sugarless gum or sucking on hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

IMPORTANT WARNING:
Pentazocine may be habit forming, especially with prolonged use. Take pentazocine exactly as directed. Do not take more of it, take it more often, or take it in a different way than directed by your doctor. While you are taking pentazocine, discuss with your health care provider your pain treatment goals, length of treatment, and other ways to manage your pain. Tell your doctor if you or anyone in your family drinks or has ever drunk large amounts of alcohol, uses or has ever used street drugs, or has overused prescription medications, or if you have or have ever had depression or another mental illness. There is a greater risk that you will overuse pentazocine if you have or have ever had any of these conditions. Talk to your health care provider immediately and ask for guidance if you think that you have an opioid addiction or call the U.S. Substance Abuse and Mental Health Services Administration (SAMHSA) National Helpline at 1-800-662-HELP.

Pentazocine may cause serious or life-threatening breathing problems, especially during the first 24 to 72 hours of your treatment and any time your dose is increased. Your doctor will monitor you carefully during your treatment. Tell your doctor if you have or have ever had slowed breathing or asthma. Your doctor will probably tell you not to take pentazocine. Also tell your doctor if you have or have ever had lung disease such as chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs and airways), a head injury, or any condition that increases the amount of pressure in your brain. The risk that you will develop breathing problems may be higher if you are an older adult or are weak or malnourished due to disease. If you experience any of the following symptoms, call your doctor immediately or get emergency medical treatment: slowed breathing, long pauses between breaths, or shortness of breath.

Continued..

Pharmacokinetics:

  • Absorption:
    Well absorbed after oral or parenteral administration. However, orally administered drug undergoes first-pass metabolism in liver; less than 20% of dose reaches systemic circulation unchanged. Increased bioavailability in patients with hepatic dysfunction; patients with cirrhosis absorb 60% to 70% of drug.
  • Distribution:
    Widely distributed in body.
  • Metabolism:
    Metabolized in liver, mainly by oxidation and secondarily by glucuronidation. Metabolism may be prolonged in patients with impaired hepatic function.
  • Excretion:
    Duration of effect is 3 hours. Considerable variability among patients in its urinary excretion. Small amounts excreted in feces after oral or parenteral administration.

Half Life: 2 to 3 hours:
Pentazocine is only found in individuals that have used or taken this drug. It is the first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. The preponderance of evidence suggests that pentazocine antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor. Hepatic Half Life: 2 to 3 hours. Route of Exposure: Intravenous, Oral. Well absorbed from the gastro-intestinal tract.

Obscure Benzomorphan:
Pentazocine is the most widely prescribed and used benzomorphan, prescribed for pain in situations where other opioids are indicated against. It was invented in the 1950's and saw usage in the U.S. throughout the 1970's until it eventually fell into obscurity. It is now mostly prescribed only outside of western nations.

Where its prescribed more commonly, most notably in Nigeria, it is known as a drug of abuse, documented in a number of case studies that demonstrate symptoms typical of opioid dependence.

Pentazocine is normally administered either in 30 mg injections or as a 50 mg oral tablet (This is a formulation of Pentazocine/Naloxone called Talwin- the inclusion of Naloxone is to discourage abuse by intravenous administration, Naloxone is not active orally)

FDA PDF Talacen

Caymanchem PDF Talacen

A painkiller used to treat moderate to severe pain. It shares many of the side effects of other opioids like constipation, nausea, itching, drowsiness and respiratory depression, but unlike most other opioids it fairly frequently causes hallucinations, nightmares and delusions. It is also, unlike most other opioids, subject to a ceiling effect, which is when at a certain dose (which differs from person-to-person) no more pain relief, or side effects, is obtained by increasing the dose any further.

It was patented in 1960 and approved for medical use in 1964. The analgesic compound was first made at Sterling in 1958. U.S. testing was conducted between 1961 and 1967.It was approved by the Food and Drug Administration in June 1967. Usually, in its oral formulations, it is combined with naloxone so as to prevent people from crushing the tablets, dissolving them in a solvent (like water) and injecting them for a high.

Orally administered naloxone produces no opioid-negating effects. Intravenous or intramuscular administration, however, does

In the 1970s, recreational drug users discovered that combining pentazocine with tripelennamine produced a euphoric sensation. Since tripelennamine tablets are typically blue in color and brand-name Pentazocine is known as Talwin (hence "Ts"), the pentazocine/tripelennamine combination acquired the slang name Ts and blues. After health-care professionals and drug-enforcement officials became aware of this scenario, the mu-opioid-antagonist naloxone was added to oral preparations containing pentazocine to prevent perceived "misuse" via injection, and the reported incidence of its recreational use has declined precipitously since.

  
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