Sedative and Hypnotic Drugs

Sedatives, Hypnotics, & Insomnia Management

Welcome to this video tutorial on sedatives, hypnotics, & insomnia management.

Sedatives are drugs that promote relaxation, used for their calming effect to relieve irritability or anxiety. Hypnotics are higher doses of sedatives with the main purpose of inducing sleep. Sedative-hypnotic drugs are central nervous system (CNS) depressants that work by increasing the activity of GABA (gamma-aminobutyric acid), a neurotransmitter in the brain. Neurotransmitters are chemicals that serve as a means of communication between nerves. By increasing the GABA activity in the brain, the result is drowsiness and the ability to maintain sleep.

Insomnia is the prolonged difficulty falling asleep or staying asleep long enough to feel rested. It is a result of many varied causes, including poor sleep habits, depression, anxiety, pain, illness, changes in lifestyle or environment, and various medications. Insomnia that lasts from one night to a few weeks is considered acute insomnia. When insomnia lasts longer than a month, it is called chronic insomnia.

The main drugs used to treat insomnia are benzodiazepines and the nonbenzodiazepine hypnotics.

Benzodiazepines are a class of drugs that cause CNS depression, including excessive sedation, impairment of physical and mental activities, and respiratory depression. They are considered generally safe and effective for short-term use, but they are not recommended for long-term use. They are drugs of abuse and may cause physiologic dependence; therefore, withdrawal symptoms occur if the drugs are stopped abruptly.

Benzodiazepines given for insomnia include flurazepam (Dalmane), temazepam (Restoril), triazolam (Halcion), and quazepam (Doral). These medications are well absorbed orally. Side effects can include daytime drowsiness and dizziness, dependence and withdrawal symptoms, and physical problems, such as falling, especially in older people. Contraindications include severe respiratory disorders, severe liver or kidney disease, history of alcohol or other drug abuse, and hypersensitivity reactions. Extreme caution must be taken when given with other CNS depressant drugs.

With longer use and higher doses, physical dependence on benzodiazepines develops, indicated by withdrawal symptoms when the drugs are stopped. To prevent withdrawal symptoms, the drug should be tapered in dose and gradually discontinued.

Toxic effects of benzodiazepines include excessive sedation, respiratory depression, and coma. Flumazenil (Romazicon) is an antidote for benzodiazepines that reverses toxicity.

Several nonbenzodiazepine drugs are also used as sedative-hypnotic agents. These include chloral hydrate, eszopiclone (Lunesta), zaleplon (Sonata), ramelteon (Rozerem), and zolpidem (Ambien).

Chloral hydrate, the oldest sedative-hypnotic drug, is relatively safe and effective, but it is a drug of abuse and may cause physical dependence.

Lunesta increases total sleep time and reduces the amount of time needed to fall asleep. It is approved for long-term use and may be taken up to 12 months.

Sonata is approved for the short-term treatment of insomnia (7-10 days), but is contraindicated in patients with hypersensitivity reactions and during lactation. It should be used cautiously during pregnancy, patients with depression, and impaired hepatic or respiratory function.

Rozerem is the newest nonbenzodiazepine hypnotic and is approved for long-term use. Rozerem binds to melatonin receptors in the CNS and is thought to play a role in maintaining the circadian rhythm, helping to regulate the normal sleep-wake cycle. It is the only non-controlled hypnotic and does not produce physical dependence.

Ambien is the most commonly prescribed nonbenzodiazepine hypnotic, and it should not be taken for more than 10 days.

These drugs have similar adverse effects including daytime drowsiness, dizziness, nausea, depression, impaired coordination, and short-term memory impairment. They should not be taken with alcohol or other CNS depressants because of the increased risk of excessive sedation and respiratory depression.

When a patient has insomnia, it is best to start with nondrug measures first to promote relaxation, rest, and sleep. Some good sleep habits to teach patients include –

– Try to stay on a sleep schedule – go to sleep and get up about the same time each day. Try not to take naps during the day, which may make you less sleepy at night.
– Avoid caffeine, nicotine, and alcohol late in the day. Caffeine and nicotine are stimulants, making it difficult to fall asleep; alcohol interferes with sleep quality by causing waking in the night.
– Avoid using electronic devices that give off light before bed.
– Get regular exercise, preferably in the morning or at least 3-4 hours before bedtime.
– Avoid eating a heavy meal late in the day.
– Make your bedroom comfortable – dark, quiet, comfortable temperature – if needed, use earplugs, ‘white noise,’ or a sleeping mask.
– Follow a bedtime routine to help you relax before sleep.

Some herbal supplements can also be helpful to treat insomnia.

– Melatonin is a natural hormone secreted by the pineal gland that helps maintain the wake-sleep cycle. Environmental light at night, such as from smartphones or TV block the production of melatonin, leading to sleep disturbances. Melatonin production is stimulated by darkness, peaking between 11pm and 3am. Melatonin is made synthetically to mimic the effects of the natural hormone; and it is available over the counter.

– Valerian is an herbal supplement that acts like a sedative on the brain and nervous system to improve sleep quality.

Patient teaching guidelines for sedative-hypnotic drugs include:
– The drugs should not be taken every night – taking it intermittently helps maintain effectiveness of the drug and reduces risks of drug abuse and dependence. Most benzodiazepine hypnotics lose their effectiveness after 4 weeks of daily use.
– If drowsy from medication, do not perform tasks that require alertness, such as driving or operating machinery. Routine activities can be potentially hazardous, due to impaired mental and physical functioning, especially during the first few days of drug use.
– Avoid alcohol and other depressant drugs while taking sedative-hypnotic drugs, because combining them produces additive depression and may lead to excessive drowsiness, difficulty breathing, traumatic injuries, and other potential adverse effects.



by Mometrix Test Preparation | Last Updated: January 12, 2021