MEPROBAMATE

- Everything we could find out about it

Home ] [ Controlled Substances ] [ Depressants ]

Created Oct 2019 | Updated Oct 2020

MEPROBAMATE

  • [MILTOWN]
  • [EQUANIL]
  • [MICRAININ]
  • [EQUAGESIC]
  • [MEPROSPAN]

2-methyl-2-propylpropane-1,3-diol dicarbamate

DEA CODE 2820: Schedule 4

When Meprobamate (Miltown) came out in 1954, it was a miracle drug. Miltown, along with other newly invented "minor" tranquilizers introduced in the era, enabled half of the patients in America's mental hospitals to be released and lead everyday lives, saving taxpayers billions of dollars. At that time, Americans had not yet become cynical about drugs. "Staying calm" was a virtue when nuclear war was a threat. Indeed, the U.S. Civil Defense Department advised the public to keep a supply of tranquilizers in their fallout shelters.

Within ten years of its introduction, Miltown was America's number one addiction after cigarettes and alcohol, and it represented one-third of all prescribed drugs. It was a blockbuster drug among the Hollywood crowd, and considered safe, harmless and useful. Demand was patient-driven - people learned about its wonders from neighbors, friends and even Milton "Miltown" Berle, a popular TV comedian. By 1966, 80 million Americans had tried Miltown and 200 had committed suicide with it. It was becoming evident that Miltown was addictive and eventually, the U.S. government had to declare it a Schedule IV Classified Substance. In January 2012, the European Medicines Agency suspended the use of all products containing meprobamate, the ingredient in Miltown, because of serious side effects. The agency noted that "its benefits do not outweigh its risks." Today Miltown and other meprobamate drugs are still available and widely abused in the United States, even though they have been mostly replaced by better and more modern tranquilizers.

2012 European Medicines Agency Suspended Meprobamate Products:
The European Medicines Agency has completed a review of the safety and effectiveness of oral meprobamate-containing medicines, due to serious side effects seen with the medicine. The Agency's Committee for Medicinal Products for Human Use (CHMP) has concluded that the benefits of meprobamate do not outweigh its risks, and that all marketing authorisations for oral medicines containing meprobamate should be suspended throughout the European Union (EU). The Committee recommended that the suspension should be implemented gradually to avoid the risk of severe withdrawal symptoms in patients stopping treatment abruptly.

EMA PDF Meprobamate

Used for Anxiety Disorders:
Meprobamate is used to treat anxiety disorders or for short-term relief of the symptoms of anxiety in adults and children 6 years of age and older. Meprobamate is in a class of medications called tranquilizers. It works by slowing activity in the brain to allow for relaxation.

Not be used for stress of everyday life:
Meprobamate is used to relieve nervousness or tension. This medicine should not be used for nervousness or tension caused by the stress of everyday life. Meprobamate is available only with your doctor's prescription.

Pediatric:
Studies on this medicine have been done only in adult patients, and there is no specific information comparing use of meprobamate in children with use in other age groups.

Geriatric:
Elderly people may be especially sensitive to the effects of meprobamate. This may increase the chance of side effects during treatment.

Other Medical Problems:
Make sure you tell your doctor if you have any other medical problems, especially:

  • Alcohol abuse (or history of)
  • Drug abuse or dependence (or history of) - Dependence on meprobamate may develop
  • Epilepsy - The risk of seizures may be increased
  • Kidney disease
  • Liver disease - Higher blood levels of meprobamate may occur, increasing the chance of side effects
  • Porphyria - Meprobamate may make the condition worse

CNS Depressant:
A central nervous system depressant, meprobamate acts selectively upon the spinal cord and the higher centres in the brain. Physical dependence may be produced after utilization of high doses for prolonged periods. Possible side effects include drowsiness, lethargy, and unsteadiness of stance and gait.

Dosage:
Meprobamate is a white powder with a characteristic odor and a bitter taste. It is slightly soluble in water, freely soluble in acetone and alcohol, and sparingly soluble in ether. Meprobamate tablets are indicated for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually do not require treatment with an anxiolytic. The effectiveness of meprobamate tablets in long-term use, that is, more than 4 months, has not been assessed by systematic clinical studies. The physician should periodically reassess the usefulness of the drug for the individual patient. The usual adult daily dosage is 1200 mg to 1600 mg, in three or four divided doses; a daily dosage above 2400 mg is not recommended. The usual daily dosage for children ages six to twelve years is 200 mg to 600 mg, in two or three divided doses.

Meprobamate
Side Effects:
Get emergency medical help if you have signs of an allergic reaction: hives; fever, chills; wheezing, difficult breathing; swelling of your face, lips, tongue, or throat.
RxList
Call your doctor at once if you have:
  • problems with balance or coordination
  • slurred speech
  • feelings of extreme happiness, feeling restless or excited
  • pounding heartbeats or fluttering in your chest
  • a light-headed feeling, like you might pass out
  • swelling in your hands, ankles, or feet
  • sudden weakness or ill feeling, fever, chills, sore throat, mouth sores
  • easy bruising, unusual bleeding
  • severe skin reaction - fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling
Common side effects may include:
  • drowsiness, weakness
  • dizziness, spinning sensation
  • headache
  • numbness or tingling
  • blurred vision
  • nausea, vomiting, diarrhea
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Anxiolytic action:
Cellular mechanism is unknown, but drug causes nonselective CNS depression similar to that of barbiturates. Meprobamate acts at multiple sites in the CNS, including the thalamus, hypothalamus, limbic system, and spinal cord, but not the medulla or reticular activating system.

Pharmacokinetics:

  • Absorption:
    Well absorbed after oral administration. Sedation usually occurs within 1 hour.
  • Distribution:
    Distributed throughout the body; 20% is protein-bound.
  • Metabolism:
    Metabolized rapidly in the liver to inactive glucuronide conjugates. Half-life of drug is 6 to 17 hours.
  • Excretion:
    Metabolites of drug and 10% to 20% of a single dose as unchanged drug are excreted in urine.


Side Effects:
  • Drowsiness, dizziness, headache, excitement, nausea, vomiting, and diarrhea may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
  • Tell your doctor right away if any of these unlikely but serious side effects occur: numbness/tingling/swelling of arms/legs.
  • Tell your doctor right away if any of these rare but very serious side effects occur: fast/irregular heartbeat, fainting, signs of infection (such as fever, persistent sore throat), easy bruising/bleeding, signs of kidney problems (such as change in the amount of urine), unusual tiredness.
  • A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Prescribed for:

    What Conditions does it Treat?
  • Anxious

Uses:
This medication is used short-term to treat symptoms of anxiety and nervousness. It acts on certain centers of the brain to help calm your nervous system.

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

  • A certain liver/blood disorder (porphyria)
  • Kidney disease
  • Liver disease
  • Brain disorders (such as seizures, brain damage)
  • Personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol)

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).

User Reviews:

32 Total User Reviews
Meprobamate Oral:
Read Reviews
Condition: Anxious (24 Reviews):
Effectiveness(4.63)

Ease of Use(4.58)

Satisfaction(4.13)

WebMD User Reviews:

  • Wonderful medication really does the job but do not do not do not take this shit with alcohol.
  • This was the first tranquilizer introduced in the 50s. Blockbuster! Prescribed for me as an alternative to Valium. Yes this drug is effective and I took it as directed for a few years. Relaxes muscles so you can sleep. Calms you down during the day. But if you are taking it at high doses for a long time....do not stop suddenly. Have your Dr. taper you off it. Otherwise you will have withdrawl symptioms and it is no fun, believe me.
  • I currently am not taking this drug because the cash price for 30 pills is over $400. My doctor substituted with generic Valium . It was prescribed for me over 25 years ago for skeletal pain and muscle tension. Do I like the generic Valium? No. I took a very low dose of meprobamate-not one side effect just relief.
  • Very weak. Not for serious anxiety. Anything that when you take 2 of, and things get worse,sux. I would not recommend this. Get at Ivan or valium

A Very Old Generic Tranquilizer Becomes Unaffordable:
Forty years ago the brand name Miltown cost $8.45 for 100 pills. The same amount today in its generic form could cost almost $350. We can think of no good explanation or justification for such a price hike. Because the tranquilizer meprobamate can cause dependence, the drug can be hard to discontinue suddenly. The dose of meprobamate must be tapered very gradually over a long period of time under medical supervision. Sadly, neither the FDA nor most drug companies provide detailed guidelines for getting off a tranquilizer or anti-anxiety agent. As a result patients and health professionals have to make up a program on their own. People also differ in the way their bodies react to these medications. As a result, some people can phase off a tranquilizer gradually over several weeks without too much distress while others may suffer terribly for months.

Tolerance to and Dependence:
In the past, meprobamate was commonly used to relieve anxiety, however it is now rarely used as other medicines, such as benzodiazepines, are more effective. The MHRA now recommend that treatment with meprobamate is not started in people with anxiety, it can cause dependence and is also more harmful than benzodiazepines if an overdose is taken.

Warning!
This medicine is generally only suitable for short-term use. If it is used for long periods or in high doses, tolerance to and dependence upon the medicine may develop, and withdrawal symptoms may occur if treatment is stopped suddenly. For this reason, treatment with this medicine should usually be stopped gradually, following the instructions given by your doctor, in order to avoid withdrawal symptoms such as rebound insomnia or anxiety, confusion, sweating, tremor, loss of appetite, irritability or convulsions.

Liver:
Meprobamate therapy was not associated with liver enzyme elevations and has not been linked to instances of clinically apparent liver injury.

Meprobamate Hepatotoxicity:
Rates of serum enzyme elevations during meprobamate therapy have not been reported. While instances of clinically apparent liver injury due to meprobamate have been mentioned in review articles, no cases with specific information on clinical features have appeared in the published literature. Thus, meprobamate may be capable of causing clinically apparent liver injury, but it must be rare. Meprobamate is metabolized in the liver via the cytochrome P450 system and has major potential for drug-drug interactions. Meprobamate can exacerbate symptoms of porphyria. Serious allergic reactions to meprobamate have been reported including Stevens Johnson syndrome. In cases of meprobamate overdose, the cause of death has been respiratory suppression and not liver failure, although liver histology was not well defined.

E* Likelihood score: E* (unproven but suspected cause of liver injury).


Metabolism and Excretion:
Meprobamate is rapidly metabolized in the liver, where it can induce liver microsomal enzymes. It is unclear whether it induces the enzymes responsible for its own metabolism.Meprobamate metabolites are pharmacologically inactive and include 2-beta-hydroxymeprobamate, as well as glucosyluronide and glucuronide conjugates of meprobamate. In the overall population, some persons can acetylate the drug rapidly ("fast acetylators") and thereby detoxify it quickly, whereas others acetylate meprobamate more slowly ("slow acetylators").

Important Information
You should not take meprobamate if you have porphyria.

Drinking alcohol with meprobamate can cause side effects.

This medicine may cause blurred vision and may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Interactions:

Drug Interactions (304) Alcohol/Food Interactions (1) Disease Interactions (10)


What other drugs will affect Meprobamate?
Taking meprobamate with other drugs that make you sleepy can worsen this effect. Ask your doctor before taking meprobamate with a sleeping pill, narcotic pain medicine, muscle relaxer, or medicine for anxiety, depression, or seizures. Other drugs may interact with meprobamate, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

A total of 304 drugs are known to interact with Meprobamate.

  • 24 major drug interactions
  • 280 moderate drug interactions

Meprobamate Overdose:
Meprobamate overdose occurs when someone takes more than the normal or recommended amount of this medicine. This can be by accident or on purpose. Meprobamate can be poisonous in large amounts. Seek medical help right away. DO NOT make the person throw up unless poison control or a health care provider tells you to. How well someone does depends on the amount of meprobamate swallowed and how quickly treatment is received. The sooner medical help is given, the better the chance for recovery. With proper care, most people recover. But, recovery may be more difficult in people with aplastic anemia. This is because their bone marrow does not produce enough red blood cells.

If you or someone you are with has an overdose, call your local emergency number (such as 911), or your local poison center can be reached directly by calling the national toll-free Poison Help hotline (1-800-222-1222) from anywhere in the United States.

Symptoms of meprobamate overdose include:
  • drowsiness
  • sluggishness
  • unresponsiveness
  • or coma
  • loss of muscle control
  • severe impairment or cessation of breathing
  • or shock.
Death has been reported with ingestion of as little as 12 g of meprobamate and survival with as much as 40 g. In an overdose, meprobamate tablets may form a gastric bezoar, requiring physical removal of the undissolved mass of tablets through an endoscope; therefore, administration of activated charcoal should be considered even after 4 or more hours or if levels are rising.

Pregnancy & Lactation:
Pregnancy: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. Lactation: secreted into breast milk at 2-4x plasma concentration; avoid.

Breastfeeding:

Summary of Use During Lactation:
If meprobamate is required by the mother, it is not necessarily a reason to discontinue breastfeeding.

However, because there is little published experience with meprobamate during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant, or when other drugs that can cause sedation are used simultaneously.

Alternate Drugs to Consider:

What is the most important information I should know about meprobamate (Equanil, MB-TAB, Miltown)?
You should not take meprobamate if you have porphyria.

EMC PDF Meprobamate

Meprobamate is a carbamate derivative used as an anxiolytic drug. Meprobamate enhances GABA-A currents, and at higher concentration, exhibits a separate channel-blocking effect that limits the magnitude of GABA(A) receptor potentiation. It is also a potent adenosine reuptake inhibitor (AdoRI), which is most likely responsible for its lesser degree of sedation compared to barbiturates. Meprobamate was withdrawn from European and Canadian markets due to its potential to cause physical and psychological dependence.

A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of anxiety disorders, and also for the short-term management of insomnia but has largely been superseded by the benzodiazepines. This compound belongs to the class of organic compounds known as carbamate esters.

Caymanchem PDF Meprobamate

History:
In the mid-1940s, Frank Berger was working in a laboratory of a British drug company, looking for a preservative for penicillin, when he noticed that a compound called mephenesin calmed laboratory rodents without actually sedating them. Berger subsequently referred to this sedating or "tranquilizing" effect in a now-historic article (https://ajp.psychiatryonline.org/doi/pdfplus/10.1176/appi.ajp.2008.08040552), published by the British Journal of Pharmacology in 1946. However, three major drawbacks existed to the use of mephenesin as a tranquilizer: a very short duration of action, greater effect on the spinal cord than on the brain, and a weak activity.

In May 1950, Berger and a chemist, Bernard John Ludwig, synthesized a chemically related tranquilizing compound, meprobamate, that was able to overcome these three drawbacks. Wallace Laboratories, a subsidiary of Carter Products, bought the license and named their new product "Miltown" after the borough of Milltown, New Jersey. Launched in 1955, it rapidly became the first blockbuster psychotropic drug in American history, becoming popular in Hollywood and gaining notoriety for its seemingly miraculous effects.

Meprobamate was one of the first drugs to be widely advertised to the general public, with user Milton Berle promoting the drug heavily on his television show, calling himself 'Uncle Miltown'. Miltown soon became ubiquitous in 1950s American life, with 1 in 20 Americans having used it by late 1956, and popular comedians making as many jokes about the drug as they did about Elvis Presley. In April 1965, meprobamate was removed from the list of tranquilizers when experts ruled that the drug was a sedative, instead.

Although it was marketed as being safer, meprobamate has most of the pharmacological effects and dangers of the barbiturates and acts at the barbiturate binding site (though it is less sedating at effective doses).

  
Meprobamate W/Aspirin Oral Side Effects by Likelihood and Severity - The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is ...
Monday May 24, 2021 - webmd.com

What should I Know Regarding Pregnancy, Nursing and Administering Meprobamate W/Aspirin Oral to Children or the Elderly? - management or monitoring precaution: Neuro/Psych-High risk of dependence and sedation. High fall risk drug. Generally avoid in the elderly. General- Withdrawn from market in Canada August 2013.
Friday April 09, 2021 - webmd.com

A Controlled Evaluation of Deanol and Benactyzine-Meprobamate - Since 1958 numerous reports have appeared concerning the successful treatment of depressed patients with deanol and meprobamate combined with benactyzine. Both drugs are currently prescribed by ...
Wednesday January 18, 2023 - nejm.org

Meprobamate and Aspirin - Indications, Dosage, Side Effects and Precautions - Latest prescription information about Meprobamate and Aspirin. Learn how to pronounce the drug's name, its indications, dosage, how to take, when to take, when not to take, side effects ...
Monday October 29, 2012 - medindia.net

Side effect(s) of Meprobamate and Aspirin - Meprobamate and Aspirin(Equagesic and Micrainin) generic contains a non-steroidal anti-inflammatory drug (NSAID) and an anxiolytic, prescribed for pain with anxiety or tension from muscle/bone ...
Sunday March 18, 2018 - medindia.net

  
Depressants | Link to this page

Home ] [ Controlled Substances ] [ Sources ]


· Controlled Substances
· Depressants
· Meprobamate