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Prescription Sleeping Pills: What You Need to Know About Their Use

written by / December 9, 2019
Prescription Sleeping Pills - Featured

Seeking ways to ensure a good night’s sleep has been humanity’s quest since the dawn of civilization. Ancient physicians used a variety of natural sleep remedies to calm their patients and ease their restless nights. The tranquilizing and hypnotic effects of roots, leaves, fruits, and other extracts have been used for millennia. In time, their therapeutic potential was carefully perfected.

The expansion of pharmaceutical research in the 20th century gave birth to many fascinating sleep aids—some are even still in use today. According to the CDC, about 4% of the US adult population uses prescription sleeping pills.

Sleep medications are used for acute and chronic insomnia, helping people both fall asleep and stay asleep. Several drug classes are prescribed today. They’re classified based on their chemistry, how they affect the body, their strength, and how long they last. They all act on different levels of the central nervous system (CNS) and can produce serious side effects.

The main controversy regarding sleep medication is simple: there’s a very thin line between them being your best friend or your worst enemy. In some cases, one sleeping pill will spare you the trouble of late-night sheet creasing and make your next day much easier. In others, patients tend to develop high tolerance levels, which lead to overuse and addiction. Therefore, control mechanisms need to be in place when prescribing, dispensing, or using prescription medication for sleep disorders.

The Pharmacy’s Promise of a Good Night’s Rest

There are many substances that can affect sleep, and not all of them are originally sleeping pills. As long as the main acting compound can travel through the blood-brain barrier and mediate an inhibitory neuronal signal, it should affect a patient’s state of wakefulness.

A pharmacy will have a variety of sleep aids that can be natural or synthetic in origin. Natural sleep aids come as liquid extracts or in solid dosage forms, such as tablets, capsules, or powders. Valerian root, lemon balm leaves, passiflora flower, and hop plant have been commonly used as tranquilizers, but in stronger doses could be used as sleep remedies. They can be acquired without a prescription and are used to treat patients with mild difficulty falling asleep. 

Most recommended non-prescription sleeping pills are first-generation antihistamines, such as diphenhydramine and doxylamine. In low doses, they quickly induce drowsiness, and in higher doses can cause sedation, making it easier to fall asleep. However, in most cases, they don’t ensure a prolonged duration of sleep nor do they necessarily produce a high quality of sleep.

On the other hand, some over-the-counter medications out there can be used to treat both sleep duration and quality of sleep. Melatonin effectively treats non-organic sleep disorders. Fast-acting melatonin is more popular than the common, slow-acting option. Studies have shown that oral sprays are twice as effective as regular tablets. Plus, with melatonin, the side effects are rare and temporary. They include daytime drowsiness, feelings of depression, irritability, and headache. 

What Is Prescription Sleep Medication?

As a rule, prescription drugs are more efficient than over the counter sleep aids. To be more specific, hypnotics are medications used in the treatment of sleeplessness that are both efficient in inducing sleep and prolonging the duration of sleep. They’re related to sedatives but are technically high-potency psychoactive drugs. They represent the most effective type of prescription sleep aid and are used in the treatment of mild, moderate, and severe insomnia. 

However, they carry a high risk of dependency and abuse and are potentially life threatening. Therefore, their dispensing regime is prescription only. This means sedative-hypnotics can’t be bought without a prescription, and they can’t be prescribed without a medical examination. 

What Do Doctors Prescribe for Sleeping Problems?

Sleeping problems can occur for a variety of reasons. Primary insomnia is usually caused by psychological stress, due to trauma or socio-behavioral problems. It can also be induced by questionable lifestyle choices, such as excessive caffeine intake, smoking, overeating, and alcohol consumption. Secondary insomnia usually follows another pathology, such as neurological and psychiatric disorders, hyperthyroidism, or menopause.

As a result, there are a few different options among the more commonly prescribed sleep meds. Depending on the cause, a doctor will prescribe sleep medication from a diverse group of pharmaceuticals:

  1. Sedative-Hypnotics
  • Barbiturates
  • Benzodiazepines
  • Non-benzodiazepine hypnotics
  • Orexin antagonists
  • Melatonin receptor agonists
  1. Antidepressants
  2. Antipsychotics
  3. Antiepileptics
  4. Antiparkinson drugs

What Are Barbiturates?

Barbiturates are an old drug class, introduced to medicine about 150 years ago. For a century, they were the most effective sleeping pills by prescription. During the first two-thirds of the 20th century, barbiturates were prescribed for headaches, epilepsy, sleep disorders, anxiety, and even depression. They were high in popularity during the 1950s, when a wave of illicit misuse caught the US. As a result, barbiturates were the main pharmacological cause of death for almost two decades.

Barbiturates are CNS depressants. They prolong the action of inhibitory GABA receptors deep within the brain’s structure. Regarding insomnia treatment, barbiturates act quickly and can have a long-lasting effect, prolonging total sleep time and reducing REM sleep time. Barbiturates are possibly the strongest prescription sleeping pills, but due to their narrow therapeutic range, they can easily induce coma or cause death. 

They stay in the body for a long time, therefore enhancing the effects of depressing the central nervous system. And a repeated dose is more likely to result in an overdose. Their use is consistent with strong withdrawal symptoms. Today, they’re prescribed only in the case of severe insomnia or excessive tension headaches, or they’re used in general anesthesia.

The main criteria in differentiating barbiturates from other sleep aids are based on how long they stay in the body.

List of Barbiturates (with Their Pharmacological Half-life)

  • Long Acting
      • Phenobarbital (37–140 hours)
      • Mephobarbital (34–130 hours)
      • Butabarbital (about 100 hours)
  • Intermediate Acting
      • Amobarbital (15–40 hours)
      • Pentobarbital (15–50 hours)
      • Secobarbital (15–40 hours)
  • Short Acting
    • Thiopental (3–11.5 hours)
    • Primidone (5–15 hours)

Due to their safety issues, barbiturates are rarely prescribed today. Their place as the most popular prescription sleep aids has been usurped by benzodiazepines.

Benzodiazepines Have Conquered the World

Prescription Sleeping Pills - Benzodiazepines

Since they were first introduced in the 1960s, benzodiazepines have transformed medical treatments worldwide. Today, these drugs are prescribed as anxiolytics, mood stabilizers, sleep aids, anticonvulsants, antihypertensives, and myorelaxants. 

According to the CDC, the number of adults who filled a benzodiazepine prescription in the US between 1996 and 2013 has increased by 67%. However, during this time period, the overdose rate increased by a full 830%.

Today, they are common prescription sleep aids, irreplaceable in the treatment of insomnia. Nevertheless, they are very potent psychoactive substances, with high abuse potential, and therefore should not be taken for granted.

Benzodiazepines: Their Effects Depend on the Half-life

Their activity is mainly based on binding to GABA receptors in the CNS, thus prolonging their inhibitory activity. Given that these receptors are present in millions of inter-reacting neurons, neural inhibition can produce a variety of effects. In small doses, they can relax muscles, but in high-affinity reactions, they can induce anterograde amnesia, followed by coma.

Benzodiazepine sedative-hypnotics have a fast onset of action. Thus, as prescription sleep medications, they’re very effective. When used for mild to moderate insomnia, most of the short- and intermediate-acting drugs from this group can quickly induce sleep and efficiently maintain it. However, for severe cases, long-acting equivalents are used.

The relationship between sleep quality and the use of benzodiazepines depends on the half-life and the prescribed medication. Furthermore, their half-life determines the incidence of their most frequent undesired therapeutic effects, such as the following: 

In insomniacs, all of these effects must be considered before the prescription is ever written.

Long-Acting Benzodiazepines

They stay in the body for 40–250 hours and are prescribed for severe insomnia. This class of sleep aid you get by prescription, and it’s considered effective with a low tolerance potential. Long-acting drugs offer a greater quality of sleep in comparison to shorter-acting ones. However, because they take longer to metabolize, they tend to cause drowsiness the following day (the hangover effect). 

The incapacitating effect of benzodiazepines on memory and psychomotor performance is high—and unlike short-acting medications, they completely suppress the REM phase of sleep. They aren’t always the best choice for elderly patients who need help sleeping since these prescription pills tend to cause falls and fractures.

List of Long-Acting Benzodiazepines (with Their Pharmacological Half-life)
  • Flurazepam (40–114 hours)
  • Nitrazepam (24–40 hours)
  • Quazepam (25–41 hours)

Intermediate-Acting Benzodiazepines 

They stay in the body for 12–40 hours and are prescribed for the treatment of moderate to severe chronic insomnia. These medications provide a good quality of sleep without the hangover effect. Keep in mind, they also have disabling effects on memory and psychomotor performance. However, they carry a high tolerance risk, and a patient’s sleep can actually worsen when they stop taking it (rebound insomnia). They’re common sleep medications on prescription, with a share of 50% in all prescribed benzodiazepine-hypnotics. 

Most of them are also used as anxiety pills and for neurologically induced insomnia.

List of Intermediate-Acting Benzodiazepines (and Their Pharmacological Half-life)
  • Flunitrazepam (19–22 hours)
  • Lormetazepam (12–20 hours)
  • Loprazolam (5–8 hours)
  • Alprazolam (6–15 hours)
  • Estazolam (8–31 hours)
  • Clonazepam (19–60 hours)
  • Temazepam (5–18 hours)
  • Lorazepam (12–20 hours)

Short-Acting Benzodiazepines

They are common prescription sleep aids for the elderly and are generally metabolized within 12 hours. They’re also used in some cases of secondary insomnia, consistent with psychiatric patients and addicts. They have no hangover effect, but they do have a greater risk of patients developing a tolerance and experiencing rebound insomnia. These drugs are regularly quoted in US drug abuse lists.

List of Short-Acting Benzodiazepines (and Their Pharmacological Half-life)
  • Brotizolam (about 5 hours)
  • Midazolam (1–4 hours)
  • Triazolam (1–7.5 hours)

Non-Benzodiazepine Hypnotics Offer Better Sleep Benefits

These drugs are used for the short-term treatment of acute insomnia. They have a fast onset and provide a longer sleep period. They also modify the GABA system within the CNS—though they’re chemically different from their predecessors. In comparison to benzodiazepines, they have low anxiolytic properties and are mainly used to treat insomnia. These new prescription sleep aids have no risk of rebound insomnia nor any residual effects the following day. Tolerance develops after a month of consistent use, so they’re for short-term use only.

They are also referred to as Z-drugs.

List of Non-Benzodiazepines (and Their Pharmacological Half-life)

  • Zolpidem (1.5–4.5 hours)
  • Zopiclone (3–6 hours)
  • Zaleplon (about 1 hour)
  • Eszopiclone (about 6 hours)

Orexin Antagonists

These medications target the binding place of orexin, a brain-protein that plays a crucial role in the regulation of wakefulness. By antagonizing the receptors for awakeness, the drug induces natural sleep. These novelty drugs are changing the game of sleep treatment. They’re non-habit-forming prescription sleep aids that have no drowsiness side effects and have a low toxic potential. Suvorexant is the only available drug within this group. They are prescription-only and have shown great therapeutic promise.

Melatonin Receptor Agonists

These are designed to mimic the behavior of melatonin and induce a state of sleep. These drugs are used for primary insomnia and circadian rhythm sleep disorders. They also show promising results in the treatment of secondary insomnia with comorbidities. This drug-class shows additional neuroprotective benefits. Some of the available data indicates positive results in the treatment of depression. To date, the FDA has put three of these drugs on its approved sleeping pills prescription list: Ramelteon, Agomelatine, and Tasimelteon.

Other Medication That Treats Sleep Deprivation

Antidepressants act on the serotonin and noradrenaline reuptake system within the neural synapses, thus retaining the right levels of “good mood” hormones. Consequently, they alter the circadian rhythm and induce proper melatonin metabolism. Tricyclic antidepressants are used to treat insomnia that’s connected to depression.

Trazodone is a drug popularly used in the treatment of major depressive disorder. It affects mood and eating and has a high hypnotic potential. Trazodone’s side effects include headache, fatigue, drowsiness, blurred vision, and dry mouth. This drug is on the sleep aids prescription list for patients with severe depression.

Antipsychotics act as CNS depressants, lowering the levels of excitatory neurotransmitters, thus inducing sleep. They are used with psychiatric patients with excessive dopamine levels.

Mirtazapine and Quetiapine induce stable sleep habits in patients and are commonly prescribed to treat sleep deprivation in psychiatry.

Antiepileptics are used in treatments that contribute to the loss of sleep, such as restless leg syndrome, epilepsy, and bipolar disorder. They can induce long-term sleep but can’t necessarily provide the highest quality sleep. They often will be combined with another prescription sleep aid.

Although used for polyneuropathy, Gabapentin is one of the most popular anti-epileptic drugs on the market. It has little to no sedation effect, but it successfully compensates for neuronal excitation. It’s used for the treatment of mild insomnia brought on by substance abuse.

Antiparkinson meds are used in the treatment of restless leg syndrome and periodic limb movement disorder. They can ease the onset of sleep but are usually introduced with other prescription sleep medications.

The Use of Sleeping Pills During Pregnancy and While Breastfeeding

Prescription Sleeping Pills - Pregnancy

Researchers do not study drugs on pregnant women, so there’s little information regarding the use of sleeping medication in gravidity. The available data shows that benzodiazepines are harmful in the first trimester. In the case of severe insomnia during pregnancy, a short-acting drug can be administered, but preferably from the fourth month forward. Melatonin supplements have proved safer, but there’s still need for more information on this topic. 

The Use of Prescription Sleeping Pills Among the Elderly

Older people tend to carry comorbidities and usually have a case of polypharmacy (taking multiple medications). As a result of aging, the hormonal secretion within the brain’s structures changes pattern, leaving a person deprived of sleep. Both polypharmacy and circadian changes make it a challenge to prescribe the right medication.

A doctor may prescribe a short- or intermediate-acting benzodiazepine, if it doesn’t interact with other medication. Keep in mind, some studies show a correlation between the use of these drugs and sleep apnea in old age. The Z-drugs also show good potential in the elderly, but they can impact memory and therefore can’t be used for dementia patients.

Children and Sleeping Pills

It’s no surprise that if you’re looking for a list of prescription sleep medications intended for children, you’ll come up empty. These drugs are dangerous and are not designed for little ones. However, on occasion, a doctor may prescribe an antihistamine. There’s also evidence that zolpidem can be used in some severe psychiatric cases.

The Most Popular Sleeping Pills for Students

According to the National Institute on Drug Abuse, the most popular medications used among college students are intermediate-acting benzodiazepines. According to data from 1997 and 2001, the usage of hypnotics in students doubled. And even now, their abuse has reached alarming proportions. But there’s still inconsistent data on students, and the volume of the misuse is hard to quantify. 

Additional Risks Associated with Prescription Sleep Aids for Adults

The FDA has issued a warning regarding “sleep driving.” This is a behavior that’s typical with the use of long-lasting sleeping meds, and it results in a state of wakefulness under a residue drug level. Because the drug remains in the bloodstream, it can be powerful enough to break the driver’s physical coordination and mental sharpness. Consequently, pharmaceutical companies were required to create a warning in the relevant patient information leaflets.

Daytime drowsiness is considered one of the most harmful side effects of sleep therapy because it affects memory, concentration, and over time could induce severe depression. This is one of the major factors that needs to be calculated in order to adequately prescribe the safest prescription sleep aid. The use of CNS depressants can lead to dizziness, which can lead to falls. Additionally, problems can occur with daytime memory and performance.

Sleepwalking and sleep-eating are conditions that happen when the drug has a fast onset and long-acting performance. In some cases of chronic sleeping pill use, the receptors in the brain become tolerant to sleeping pills by prescription, and new doses only induce “partial sleep.” While the motoric parts of the brain still function, a person can walk or eat without recalling the event later.

Drug dependency manifests as an intensive withdrawal period, usually with behavioral exacerbations. It’s often followed by rebound insomnia, and even depression. Depressant addiction can be a year-long condition and requires multiple interventions, both pharmaceutical and therapeutic.

FAQs

What’s the difference between a hypnotic and an anxiolytic?

Although the names of prescription sleeping pills may sound similar to the names of sedatives (e.g., bromazepam vs. lorazepam), their therapeutic effects differ. 

A sedative is a drug that mainly causes mental relaxation. These drugs are used mostly to relieve symptoms of anxiety. A person taking a sedative can still engage in conscious action. Conversely, hypnotics are stronger depressants and are mainly used to induce sleep.

Their structures may be alike, but the main therapeutical differences between a sedative and a sleeping med are in the dosage and the drug’s half-life.

Can you take sleeping pills with antidepressants?

Doctors can prescribe the simultaneous use of these two drug groups, depending on the symptoms or underlying psychology. Although it isn’t recommended for someone to take both drugs during the whole course of treatment. Taking multiple strong prescription sleeping pills at once can intensify daytime drowsiness, which increases the feelings of depression. On the other hand, some antidepressants have hypnotic properties that might induce a significantly prolonged sleep time.

The best course of action is to prescribe an antidepressant with optimal sleep effects, without additional medication. 

Which sleeping pill is the most dangerous?

Any sleep medication can be dangerous if used incorrectly. But even in therapeutic doses that follow the right protocols, the drug class that carries the greatest risk of death is barbiturates. The difference between a therapeutic dose and a coma dose can be small (a narrow therapeutic range). 

How long after drinking can you take a sleeping pill?

Alcohol acts as a CNS depressant. When used with a drug that acts as a GABA modulator, such as barbiturates, benzodiazepines, and nonbenzodiazepines, it can prolong their action. Taking sleeping pills with alcohol can easily lead to coma. Therefore, it’s incredibly dangerous to drink alcohol and take any sleeping medication.

In the case of using a sleeping pill, the time to consume alcohol would reflect at least the half-life of the drug.

What is the strongest over-the-counter sleep aid?

So far, first-generation antihistamines are the preferred drugs that potently induce sleep. In comparison to supplements, such as melatonin or herbs, these drugs act directly on the brain’s dopaminergic pathways. Their action is similar to that of antipsychotics.

Conclusion

Prescription sleeping medication is common and widely used. These drugs alleviate the hard symptoms of sleeplessness and provide troubled patients with a good night’s sleep. They can help a person rest, even dream. Because of this, they might seem sweet, easy, and desirable.

But this is just a soft promise of hard pharmacology. In the long run, these medications make a person slow, forgetful, weak, and unhappy.

For insomniacs, taking a drug is justified only as a form of short-term therapy. Research has shown that in comparison to prescription sleeping pills, behavioral therapy shows better progress.

Since the beginning of civilization, people have been using sleep remedies. There has never been a richer assortment of sleeping aids than in today’s market. But, that’s the thing with markets, they behave similarly to drugs—prices change, need and demand shift, there’s always a toll, and of course, precaution is necessary.

I think about milligrams every day. How much is enough, and how they can cure or hurt. My morning dose of caffeine gives me focus. And for the rest of the day, I think about herbal remedies, medical devices, supplements, nutrients, and heavy medication. By day I work with drugs behind the counter. By night I think about apostrophe misplacement. By day I try to explain substances to others and by night I explain sentences to myself. I am a pharmacist and a writer.

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