etizolam/propranolol

Action and Spectrum

Actions and Spectrum: 

Action: 

etizolam 

etizolam is a medication belonging to the class of drugs known as thienodiazepines. It primarily acts as an anxiolytic (anxiety-reducing) and sedative agent. It works by enhancing the effect of a neurotransmitter called gamma-aminobutyric acid (GABA) in the brain, leading to a calming and relaxing effect.  

propranolol 

propranolol is a non-selective beta-blocker, so its main action is to inhibit the effects of adrenaline and other stress hormones on the beta-adrenergic receptors in the body.  

Spectrum: 

etizolam 

etizolam’s effects are primarily focused on the central nervous system (CNS). It affects specific brain and spinal cord receptors to produce its anxiolytic and sedative effects. It is not used for other medical conditions and is generally not recommended for long-term use because of the potential for dependency and symptoms of withdrawal. 

propranolol 

propranolol’s effects are systemic and affect various parts of the body, as it works on beta-adrenergic receptors throughout the cardiovascular system, the central nervous system, and other tissues. It helps regulate heart rate, blood pressure, and reduce anxiety symptoms. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Cold extremities 

Nightmare 

Uncoordinated body movements 

Tiredness 

Slow heart rate 

Drowsiness 

Memory impairment 

Confusion 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Allergy: The combination of these drugs is contraindicated in individuals with a known allergy or hypersensitivity to related compounds. 

Pregnancy and Lactation: The combination of these drugs is not recommended during pregnancy or while breastfeeding, because the developing foetus or nursing newborn may be at risk. 

Liver Impairment: The combination of these drugs is contraindicated or used with caution in individuals with severe liver impairment, as it may affect drug metabolism and lead to adverse effects. 

Respiratory Depression: Both etizolam and propranolol can cause respiratory depression, albeit through different mechanisms. Combining them may increase the risk of slowed or shallow breathing, which can be dangerous. 

Drug Interactions: Both medications have the potential to interact dangerously with other medications. To analyse potential interactions, it is imperative that you disclose to your healthcare provider all drugs, supplements, or substances that you are taking. 

Increased Sedation: Combining etizolam and propranolol can intensify sedation, making it hazardous to operate machinery or drive vehicles. It may also lead to falls, accidents, or other unintended injuries. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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: etizolam is a thienodiazepine derivative and is structurally related to benzodiazepines like diazepam. propranolol is a non-selective beta-adrenergic receptor antagonist (beta-blocker). 

Pharmacodynamics:  

etizolam 

etizolam primarily acts as a central nervous system (CNS) depressant by enhancing the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) in the brain. It binds to GABA receptors, leading to increased GABAergic transmission, which results in sedative, anxiolytic (anti-anxiety), muscle relaxant, and hypnotic effects. 

propranolol 

propranolol blocks the effects of adrenaline and noradrenaline (epinephrine and norepinephrine) on beta-adrenergic receptors. By doing so, it reduces the heart rate, decreases blood pressure, and has antiarrhythmic effects. It also has some central nervous system effects.  

Pharmacokinetics: 

Absorption 

etizolam is rapidly absorbed when taken orally. 

It has a high bioavailability, that means a significant portion of the drug reaches the systemic circulation after oral administration. 

propranolol is well absorbed when taken orally. Its absorption can be variable and influenced by factors like food. 

Distribution 

etizolam is lipophilic, it can easily cross cell membranes and distribute throughout the body. 

It binds to plasma proteins, primarily albumin. 

propranolol is highly lipophilic and can penetrate various tissues, including the brain. It also binds to plasma proteins, including albumin. 

Metabolism 

etizolam is metabolized primarily in the liver, primarily through the cytochrome P450 (CYP) enzyme system, specifically CYP3A4 and CYP2C19. 

The major metabolite is alpha-hydroxyetizolam, which is pharmacologically active. 

propranolol is extensively metabolized in the liver, primarily by the CYP2D6 enzyme. 

Excretion and Elimination 

etizolam and its metabolites are primarily excreted through the urine. 

The elimination half-life of etizolam is relatively short, typically around 3 to 4 hours. 

propranolol and its metabolites are mainly excreted in the urine. The elimination half-life of propranolol is about 3 to 6 hours. 

Adminstartion

Administration:  

The route of administration is oral. 

Always take your medications exactly as prescribed by your healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: etizolam/propranolol 

Why do we use etizolam/propranolol?  

The combination may be used to address both the psychological and physiological aspects of anxiety, such as reducing anxiety-related symptoms with and managing the underlying anxiety disorder.