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Introduction
Sedatives and hypnotics are two classes of prescription drugs that are commonly called “tranquilizers,” “sleeping pills,” or “sedatives.” They affect your central nervous system – your brain and spinal cord – and have a relaxing, calming effect.
Sedation is a decrease in awareness and a decrease in response to external stimulation. By itself, it results in calmness and relaxation. General anesthesia is a reversible and controlled loss of consciousness. General anesthesia involves sedation, the inability to feel pain (analgesia), temporary amnesia and temporary muscle paralysis.
The most frequently prescribed sedatives are benzodiazepines (benzos). In 2017, there were nearly 120 million benzodiazepine prescriptions dispensed in the U.S. alone.
Benzodiazepines are meant to be used in the short term only. If you take them for extended periods of time, you increase the risk of dependence and addiction.
Mechanism
sedative-hypnotics and anxiolytics are two medication classes that target the central nervous system (CNS) to produce calming effects. While they may have slightly different applications, their mechanism of action often overlaps. Here's a breakdown of how these medications work:
GABAergic System
The primary mechanism of action for many sedative-hypnotics and anxiolytics involves enhancing the function of the gamma-aminobutyric acid (GABA) neurotransmitter system. GABA is the main inhibitory neurotransmitter in the brain, meaning it reduces the firing of neurons and promotes calmness. These medications don't directly increase GABA levels, but instead, they modulate the GABA receptors.
GABAA Receptors
There are two main types of GABA receptors: GABA-A and GABA-B. Most sedative-hypnotics and anxiolytics target the GABA-A receptors. These receptors are actually chloride channels. When GABA binds to the GABA-A receptor, it opens the chloride channel,, it allows chloride ions (Cl-) to enter the nerve cell. This influx of Cl- ions makes the inside of the nerve cell more negative, which makes it less likely to fire electrical impulses. This decrease in nerve cell activity leads to a calming effect.
Sedative-hypnotics and anxiolytics work by increasing the effect of GABA in two ways:
* By increasing the binding of GABA to GABA receptors: These drugs do not directly activate the GABA receptor, but they can increase the amount of time that GABA spends bound to the receptor. This allows more Cl- ions to enter the nerve cell and produce a greater calming effect.
* By increasing the release of GABA from nerve cells: Some sedative-hypnotics and anxiolytics can increase the amount of GABA that is released from nerve cells. This provides more GABA to bind to GABA receptors and produce a calming effect.
By increasing the calming effects of GABA in the brain, sedative-hypnotics and anxiolytics can produce a variety of effects, including: Relaxation,Reduced anxiety,Drowsiness,Sleep induction.
Contraindications and Cautions
Allergy to benzodiazepines. Prevent severe hypersensitivity reactions.
Psychosis. Can be exacerbated by sedation
Acute narrow-angle glaucoma, shock, coma, acute alcoholic intoxication. Can be exacerbated by the depressant effects of these drugs.
Pregnancy. Associated with development of cleft lip or palate, inguinal hernia, cardiac defects, microcephaly, and pyloric stenosis when taken in the first trimester of pregnancy. Neonatal withdrawal syndrome may also result.
Lactation. Potential adverse effects to the neonate (e.g. sedation)
Elderly, debilitated. Possibiliy of unpredictable reactions
Renal or hepatic dysfunction. May alter metabolism and excretion of drugs resulting in direct toxicity.
Uses
For sedating the patient. These drugs have been used to relieve anxiety and tension during treatment of hypertension, peptic ulcer and hyperthyroidism
2. Short acting barbiturates are employed to induce sleep. Intermediate acting barbiturates are used in patients who have tendency to wake up in middle of the night.
3. Phenobarbitone may be used in grandmal epilepsy. It also controls severe types of convulsions such as status epilepticus and eclamptic fits.
4. It was used as preanesthetic medication.
5. It is given in premature children to treat kernicterus.
Side Effects
sedative hypnotics and anxiolytic drugs carry effects on the CNS and the body in general, and Take sedative and hypnotic pills and rely on them daily causes many risks and many side effects
In short term:
•sleepiness
•Nausea, weight gain
•sleep problems
•Headache
•Constipation
•difficult to focus and think
•blurred vision
•Addiction
•drowsiness or dizziness.
The person may need to increase the dose to obtain the same result ,increase the dose he takes on their own without asking a doctor, which sometimes leads to a coma or death in an overdose ,
In daily long term used :
Frequent forgetfulness or losing your memory. •Depression symptomssuch as fatigue, feelings of hopelessness or suicidal thoughts
•Liver issues or liver failure
•difficulty breathing
•Leukopenia
•sexual problems
•suffer from high body temperature
•hallucinations, emotion, delirium
•slow brain function
Example of drugs in the Egyptian Market
References
https://www.sciencedirect.com/topics/pharmacology-toxicology-and-pharmaceutical-science/hypnotic-sedative-agent#:~:text=Sedative%2Dhypnotic%20drugs%20depress%20the,activity%20and%20level%20of%20awareness
https://www.ncbi.nlm.nih.gov/books/NBK562309/
https://www.slideshare.net/slideshow/sedative-hypnoticspptx-257523501/257523501
https://www.rxlist.com/sedativehypnotics/drug-class.htm#:~:text=Sedative%2Fhypnotics%20produce%20sedation%20by,release%20to%20transmit%20nerve%20signals
https://acnp.org/wp-content/uploads/2017/11/CH68_993-1006.pdf
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