Sedatives

Sedatives: Types, Uses, Side Effects, Examples, Abuse

Sedative medications, also known as sedatives or tranquilizers, are a class of drugs that are used to promote relaxation, reduce anxiety, and induce sedation or sleep. These medications work by depressing the central nervous system, slowing down brain activity, and producing a calming effect on the body.

Sedative medications act on various neurotransmitters in the brain, with the most common target being gamma-aminobutyric acid (GABA). GABA is an inhibitory neurotransmitter that helps regulate brain activity and has a calming effect when activated. Sedatives enhance the effects of GABA, leading to a reduction in neuronal activity and an overall sedating effect.

The primary purposes of sedative medications include:

  • Anxiolysis: Sedatives can help alleviate symptoms of anxiety and promote a sense of calmness by reducing excessive brain activity associated with anxiety disorders.
  • Sedation: Sedatives induce a state of relaxation and calmness, making them useful for managing agitation, restlessness, and insomnia.
  • Hypnosis: Some sedatives have stronger hypnotic properties, meaning they can induce sleep and promote a deeper level of sedation.
  • Muscle relaxation: Certain sedatives have muscle relaxant properties and are used to relieve muscle tension and spasms.

What is the most common sedative?

The most common sedative drugs include:

1.      Benzodiazepines: Benzodiazepines work by enhancing the effects of a neurotransmitter called gamma-aminobutyric acid (GABA) in the brain. They are commonly prescribed for anxiety disorders, insomnia, muscle relaxation, and as premedication before certain medical procedures. Benzodiazepines can produce sedation, induce sleep, and reduce anxiety. However, they can also cause side effects such as drowsiness, dizziness, confusion, and the risk of dependency with long-term use. Examples include diazepam (Valium), lorazepam (Ativan), and alprazolam (Xanax).

2.      Barbiturates: Barbiturates act as central nervous system depressants by enhancing the effects of GABA. They were once widely used as sedatives and sleep aids but have been largely replaced by safer medications. Barbiturates have a higher potential for abuse and can cause significant side effects, including respiratory depression, drowsiness, dizziness, and the risk of overdose. Examples include phenobarbital and pentobarbital.

3.      Non-Benzodiazepine Sedative-Hypnotics: This class of medications includes drugs that have similar effects to benzodiazepines but differ in their chemical structure. They are primarily used for the short-term treatment of insomnia. Non-benzodiazepine sedative-hypnotics bind to specific receptors in the brain, enhancing the effects of GABA. They generally have a lower risk of dependence compared to benzodiazepines but can still cause side effects such as daytime drowsiness, dizziness, and impaired coordination. Commonly prescribed non-benzodiazepine sedative-hypnotics include zolpidem (Ambien), eszopiclone (Lunesta), and zaleplon (Sonata).

4.      Antihistamines: Certain antihistamines, such as diphenhydramine and doxylamine succinate, have sedating properties and can be used as mild sedatives. They block the effects of histamine, a chemical involved in allergic reactions, but also have a sedative effect on the central nervous system. Antihistamines are available over the counter and are commonly used to relieve allergies and occasional sleeplessness. Side effects may include drowsiness, dry mouth, blurred vision, and constipation.

5.      Alpha-2 Agonists: Alpha-2 agonists work by stimulating receptors in the brain that decrease the release of norepinephrine, a neurotransmitter involved in arousal and stress response. These medications are primarily used to treat conditions such as hypertension and ADHD but can also produce sedative effects. Alpha-2 agonists, such as clonidine and dexmedetomidine, can cause side effects like sedation, dry mouth, low blood pressure, and dizziness. Examples include clonidine and dexmedetomidine.

6.      General Anesthetics: While primarily used for inducing unconsciousness during surgical procedures, general anesthetics also have sedative properties. They work by depressing the central nervous system and altering brain activity. General anesthetics, such as propofol, thiopental, and isoflurane, are administered by healthcare professionals in controlled settings. They can cause a deep state of sedation or unconsciousness and are associated with potential risks and side effects, including respiratory depression, nausea, vomiting, and post-operative confusion. Examples include propofol, thiopental, and isoflurane.

It’s important to consult with a healthcare professional for a proper diagnosis and prescription of sedative medications. They can provide guidance on the appropriate use, potential side effects, and any precautions or contraindications associated with these medications.

Effects of Sedatives

The effects of sedatives can last anywhere from a couple of hours to more than a day. Generally, sedatives cause physical depression, muscular relaxation and sedation; due to the varying types of sedatives, there is a range of other effects depending on which substance has been taken.  Sedatives depress most body functions, so they greatly impact the ability to drive, operate machinery and participate in tasks requiring muscle coordination.  An individual who is under the influence of a sedative, especially if in combination with another drug, should never drive. Here are some effects of sedatives:

  • Feeling of relaxation
  • Reduced anxiety
  • Lowered inhibitions
  • Reduced intensity of physical sensations
  • Lightheadedness
  • Drowsiness
  • Slurred speech
  • Shallow breathing
  • Slowed heart rate
  • Muscle incoordination
  • Reduced dexterity
  • Impaired learning during the period the sedative is active
  • Interruptions in memory

Sometimes unexpected paradoxical side effects occur, such as anxiety, nightmares, and hostility.

Mixing with Other Substances

Though sedatives should never be mixed with other substances, they are particularly dangerous when mixed with any other controlled substances that make a person drowsy; this includes other sedatives/depressants such as alcohol, cold medicines, and opiates (Codeine, Heroin). Fatal suppression of breathing can occur if two sedating substances are mixed. If someone is difficult to rouse and you suspect they have used sedatives, seek medical help immediately.

Withdrawal

If an individual has become dependent on a sedative, even if just for a few months, withdrawal can be severe. The severity of withdrawal increases as the dose and duration of use increases. A sedative dependent individual should taper off the drug, as seizures or even death can occur if withdrawal is too sudden. Other withdrawal symptoms generally include the magnification or recurrence of the original symptoms being treated.

Sedatives Safety

The safety of sedative medications depends on several factors, including the specific medication, dosage, individual health characteristics, and proper use under the guidance of a healthcare professional. While sedatives can be effective for managing certain conditions, it is important to be aware of their potential risks and to use them responsibly. Here are some considerations regarding the safety of sedative medications:

1.      Prescription and Medical Supervision: Sedatives should always be obtained through a valid prescription from a healthcare professional. They have the knowledge and expertise to assess your medical condition, consider potential interactions with other medications, and determine the appropriate dosage. Sedatives in high doses can harm a fetus unless taken in a controlled medical environment. It is crucial to follow their instructions and communicate any concerns or changes in your health.

2.      Potential Side Effects: Sedatives can cause a range of side effects, including drowsiness, dizziness, impaired coordination, confusion, and memory problems. The severity and likelihood of these side effects can vary among individuals and medications. It is important to be aware of the possible effects and to exercise caution when performing activities that require alertness, such as driving or operating machinery.

3.      Risk of Dependence and Addiction: Some sedative medications, particularly those in the benzodiazepine and barbiturate classes, carry a risk of dependence or addiction, especially when used long-term or in high doses. It is important to use these medications as prescribed and to avoid sudden discontinuation without medical supervision, as it can lead to withdrawal symptoms. Regular communication with your healthcare professional is important to monitor your response to the medication and consider potential alternatives if necessary.

4.      Drug Interactions: Sedative medications can interact with other medications, including prescription drugs, over-the-counter medications, and herbal supplements. These interactions can affect the efficacy and safety of both the sedative and the other substances involved. Using marijuana can reduce the effects of sedatives, particularly ones used for anesthesia. A 2019 study found that marijuana users needed a higher dose of sedatives to get the same effects as a regular dose for someone who doesn’t use marijuana. Alcohol also works like a sedative, so drinking and taking a sedative at the same time can compound the effects and lead to dangerous, life-threatening symptoms, such as loss of consciousness or stopping breathing. It is crucial to inform your healthcare professional about all the medications and supplements you are taking to prevent potential interactions.

5.      Individual Factors: Each person’s response to sedatives can vary based on factors such as age, overall health, liver or kidney function, and susceptibility to side effects. Dosage adjustments may be necessary for certain individuals, such as older adults or those with specific medical conditions. Older adults may be more susceptible to certain sedatives, such as benzodiazepines, than younger people.

6.      Short-term Use and Treatment Goals: In many cases, sedative medications are prescribed for short-term use to manage acute symptoms or during specific treatment periods. Long-term use should be carefully evaluated to ensure the benefits outweigh the potential risks. Alternative treatment options, such as therapy or lifestyle changes, may be considered for certain conditions to reduce reliance on sedative medications.

It is essential to have open and honest communication with your healthcare professional regarding your medical history, concerns, and any potential risks associated with sedative medications. They can provide personalized guidance and ensure that the medication is used safely and effectively in your specific situation.

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Dr. Oche Otorkpa PG Cert, MPH, PhD

Dr. Oche is a seasoned Public Health specialist who holds a post graduate certificate in Pharmacology and Therapeutics, an MPH, and a PhD both from Texila American University. He is a member of the International Society of Substance Use Professionals and a Fellow of the Royal Society for Public Health in the UK. He authored two books: "The Unseen Terrorist," published by AuthorHouse UK, and "The Night Before I Killed Addiction."
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