meprobamate

Action and Spectrum

Actions and Spectrum: 

• meprobamate is a medication that belongs to the class of drugs known as anxiolytics or tranquilizers. It is commonly used to treat anxiety disorders and muscle spasms. 
• The exact mechanism of action of meprobamate has yet to be fully understood. Still, it is believed to act on the central nervous system (CNS) by enhancing the activity of the neurotransmitter gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter. meprobamate enhances the binding of GABA to its receptors in the CNS, leading to an increase in GABA-mediated inhibition of neurotransmission. This results in a calming effect and anxiety reduction. 
• meprobamate also has muscle-relaxant properties and can relieve muscle spasms by acting on the spinal cord and the brainstem. 
• The spectrum of activity of meprobamate includes a wide range of anxiety disorders, including generalized anxiety disorder, panic disorder, and obsessive-compulsive disorder. It also treats muscle spasms associated with spinal cord injury, cerebral palsy, and multiple sclerosis. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Common 

Palpitations 

Abnormal ECG 

Tachyarrhythmia 

Asthenia  

Dizziness 

Diarrhea 

Maculopapular eruption 

Hives,  

Erythematous 

Nausea 

Vomiting 

Disorder of accommodation (ocular) 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

The following conditions contraindicate it: 

• Hypersensitivity: meprobamate should not be used in patients allergic to meprobamate or its components. 
• Porphyria: meprobamate should not be used in patients with porphyria, a group of disorders that affect heme production, a hemoglobin component. 
• Severe respiratory depression: meprobamate should not be used in patients with severe respiratory depression or acute pulmonary insufficiency. 
• Liver disease: meprobamate should be used cautiously in patients with liver disease, as it can worsen liver function and cause liver damage. 
• Renal impairment: meprobamate should be used cautiously in patients with renal impairment, as it can accumulate in the body and cause toxicity. 
• Pregnancy and breastfeeding: meprobamate should not be used during pregnancy or breastfeeding, as it can harm the fetus or infant. 

Caution: 

• Elderly patients: meprobamate should be used cautiously in elderly patients, as they may be more sensitive to its effects, especially sedation and dizziness. 
• Respiratory impairment: meprobamate should be used cautiously in patients with respiratory impairment, as it can cause respiratory depression and worsen the condition. 
• CNS depression: meprobamate can cause CNS depression, such as sedation, dizziness, and impaired coordination. Therefore, caution should be exercised when driving or operating machinery. 
• Drug interactions: meprobamate can interact with drugs with CNS depressant effects, such as alcohol, opioids, and benzodiazepines. It can also interact with drugs metabolized by the liver, such as warfarin and phenytoin. 
• Withdrawal syndrome: meprobamate can cause a withdrawal syndrome if stopped abruptly after prolonged use, including insomnia, anxiety, tremors, and seizures.  
• Addiction and dependence: meprobamate has a high potential for addiction and dependence, mainly when used at high doses or for prolonged periods 

Pregnancy / Lactation

Pregnancy consideration: D 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

• meprobamate is a centrally acting muscle relaxant and anxiolytic medication structurally related to the barbiturate family of drugs. It is metabolized in the liver, and its metabolites are excreted in the urine. 
• meprobamate works by increasing the activity of the neurotransmitter gamma-aminobutyric acid (GABA) in the central nervous system (CNS). It binds to specific GABA receptors, which enhances GABA-mediated inhibition of neurotransmission. This results in a reduction in anxiety, muscle spasms, and tension. 

Pharmacodynamics: 

• The pharmacodynamics of meprobamate involve its actions on the central nervous system (CNS) and its interactions with neurotransmitters and receptors. 
• meprobamate is a GABAergic drug, meaning that it enhances the activity of the neurotransmitter gamma-aminobutyric acid (GABA) in the CNS. It binds to specific GABA receptors, which increases GABA-mediated inhibition of neurotransmission. This results in a reduction in anxiety, muscle spasms, and tension. 

Pharmacokinetics: 

Absorption 

meprobamate is well absorbed after oral administration, with a bioavailability of around 80-90%. Peak plasma concentrations are reached within 1-2 hours after oral administration. 

Distribution 

meprobamate is extensively distributed throughout the body, with a volume of distribution of approximately 0.8 L/kg. It crosses the blood-brain barrier and the placenta and is excreted into breast milk. 

Metabolism 

meprobamate is extensively metabolized in the liver by hydroxylation and conjugation reactions, forming inactive metabolites excreted in the urine. One of the significant metabolites is hydroxy meprobamate, which has similar pharmacological effects as meprobamate and contributes to its overall activity. 

Elimination and Excretion 

meprobamate and its metabolites are primarily excreted in the urine, with only a small amount excreted in the feces. The elimination half-life of meprobamate is relatively short, ranging from 6-17 hours in adults, but it may be longer in elderly patients and those with impaired renal or hepatic function. 

Adminstartion

Administration: 

• meprobamate is usually administered orally in the form of tablets or capsules. The recommended dose of meprobamate for adults is 400-800 mg daily in divided doses, depending on the severity of symptoms and the individual’s response to treatment. The maximum recommended daily dose is 2400 mg. 
• meprobamate should be taken with food or milk to minimize gastrointestinal side effects and be swallowed whole with a glass of water. Patients should not crush or chew tablets or capsules, as this can increase the risk of adverse effects and overdose. 
• meprobamate should be used only for short-term treatment of anxiety and muscle spasms, usually for no longer than 2-3 weeks. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: meprobamate 

Pronunciation: [ ME-proe-BAM-ate ] 

Why do we use meprobamate? 

meprobamate is a medication that has been used for the treatment of anxiety and muscle spasms. It is a central nervous system depressant that works by enhancing the activity of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain, which reduces anxiety and muscle tension.  

The following are some of the specific uses of meprobamate: 

• Anxiety: meprobamate has been used to treat anxiety disorders, including generalized anxiety and panic disorders. It can help reduce anxiety symptoms, such as excessive worry, tension, and nervousness. 
• Muscle spasms: meprobamate treats muscle spasms associated with muscle strains, sprains, or back pain. It works by relaxing the muscles and reducing pain.