Introduction
Sleep is required by everyone. You can live without food for 21 days but only 10 days without sleep.
It is a condition of body and mind in which your consciousness is altered, your voluntary muscles are relaxed and you have limited interactions with your surroundings. The body uses this time to restore your nervous, immune, skeletal and muscular systems. That is the reason lack of sleep can take a toll on your health, work performance and quality of life.
Sleep can get affected by a number of factors and cause insomnia. A sleep disorder in which you find it difficult to fall or stay asleep, even when you have a chance to do so is called insomnia. People with insomnia experience ‘early morning wakening’ or are unable to have restorative sleep. Daytime fatigue, confusion, irritability and mood disturbance are some of their common complaints.
How much sleep you require, varies from person to person and therefore cannot be used as a defining characteristic for defining insomnia. Insomnia is a condition that is faced by almost everyone at some point of their life. If you are a woman, you have 50% more chances of developing insomnia than your male counterparts. As you age, you are more prone to become insomniac.
Symptoms
Insomnia, in some cases, can point towards an underlying health condition. Following are the symptoms associated with insomnia:
- Difficulty falling asleep at night
- Waking up frequently during the night
- Irritation, depression or anxiety
- Tension headaches
- Difficulty in socializing
- Being uncoordinated
- Poor concentration and focus
- Increased accidents and errors
- Gastrointestinal symptoms like nausea and stomach ache
- Worrying about sleeping
- Daytime fatigue and sleepiness
- Feeling unrefreshed upon waking
- Waking up too early
Treatment Methods and Drugs Used Generally for Treatment
When you are unable to manage insomnia through non medication techniques like lifestyle changes, diet and behavior therapies, medicines are prescribed. It is important to determine the underlying cause of insomnia for the treatment to be effective. Some of the commonly prescribed drugs and their classes are mentioned below:
1. Sedative-Hypnotics
Sedatives are the drugs that are prescribed for decreasing excitement by calming you down, without inducing sleep; although, they can cause drowsiness. Sedation refers to a condition in which there is decrease in the level of responsiveness to any level of stimulation, and is accompanied by some decrease in motor activity and ideation. Sedatives are slow acting drugs.
Hypnotics, on the other hand, are the drugs that help you in inducing and/or maintaining sleep, similar to natural sleep. This sleep should not be confused with hypnosis in which you are in a trans-like state and become passive and highly suggestible. These drugs have quicker onset of action, and show their action for shorter duration of time.
Sedatives and hypnotics can generally be referred to as CNS depressants. Their action also depends on their dose as a hypnotic at lower dose can also act as sedative.
Following classes of drugs come under the category of sedative and hypnotic:
a. Barbiturates: These have been popular as sedative-hypnotics for a long period of time. These drugs act on gamma amino butyric acid (GABA) receptor. GABA is the chief inhibitory neurotransmitter found in your central nervous system (CNS). Barbiturates stimulate the inhibitory action of GABA in the brain. They decrease the communications occurring between neurons of brain and hence makes you relaxed.
However, these drugs are not prescribed generally due to risk of over dose and addiction in patients.
Drug: Secobarbital
Brand Name: Seconal Sodium
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Allergic reaction, depression, dark urine, shortness of breath, change in balance, dizziness, slow heartbeat and memory problems
Drug: Butabarbital
Brand Name: Butisol Sodium
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Allergic reaction, depression, shortness of breath, Stomach upset, dizziness and slow heartbeat
Drug: Pentobarbital
Brand Name: Nembutal Sodium
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Injection
Indicated in Pregnancy: No
Alcohol Content: Yes, 10%
Side Effects: Behavioral problems, impaired memory, impaired cognition, life threatening respiratory depression, hallucinations, sweating, hypertension and rashes.
Drug: Butabarbital
Brand Name: Butisol Sodium
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Allergic reaction, shortness of breath, slurred speech, confusion, anxiety, slow heartbeat, hallucinations and change in balance
Drug: Amobarbital
Brand Name: Amytal
The U.S. FDA Status: Discontinued
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Allergic reaction, depression, nervousness, anxiety and trouble breathing
b. Benzodiazepines: These are the drugs which generally act on the midbrain. They act by increasing the efficiency of a neurotransmitter, GABA in decreasing the excitability of neurons. This causes a decrease in communication between the neurons and calms you.
Drug: Zaleplon
Brand Name: Sonata
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Anxiety, Blurred vision, nose bleed, dizziness, headache, nausea and muscle pain
Drug: Triazolam
Brand Name: Halcion
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Lightheadedness, irritability, tiredness, abdominal pain, anxiety, chills, chest pain and dark urine
Drug: Estazolam
Brand Name: ProSom
The U.S. FDA Status: Discontinued
Dosage Form: Tablet
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Decrease in body movements, dizziness, sleepiness, dry mouth, headache, dementia and tiredness
Drug: Temazepam
Brand Name: Restoril
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Unusual sense of well being, fear, mood changes, labored breathing, appetite loss, memory loss, nightmares and weight loss
c. New Non-Benzodiazepine Hypnotics: Also known as Z-drugs, these are psychoactive drugs that are benzodiazepine-like in action. They also act on GABA receptors present in brain and increase the inhibitory action of neurotransmitter, GABA. They help in reducing communication between neuron present in brain, which produces a sense of relaxation in the body.
Drug: Zolpidem
Brand Names: Ambien
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Confusion, fever, irritability, lightheadedness, tiredness, shakiness and feeling sad
Drug: Eszoplicone
Brand Name: Lunesta
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Allergic reaction, cough, fever, painful urination, bladder pain, confusion, irritability, nerve pain and tiredness
2. Melatonin Receptor Agonist:
Melatonin is a hormone which is secreted by a small gland present in brain, called pineal gland, which helps in maintaining sleep-wake cycles. Melatonin binds to melatonin receptors found generally in brain. Drugs that act as melatonin receptor agonists can help you in maintaining your circadian rhythm and promote sleep.
Drug: Tasimelteon
Brand Name: Hetlioz
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Bladder, lower back pain, bloody or cloudy urine, difficult urination, chills or fever, headache, nasal congestion and nightmares
Drug: Ramelteon
Brand Name: Rozerem
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Dizziness, body ache, chills, cough, fatigue, fever, nausea, joint pain, shivering, sneezing, sore throat, swollen joints, vomiting and loss of taste
3. Anti-Depressants:
Apart from low-dose doxepin, anti-depressant drugs are not approved for treating general insomnia by the U.S. Food (FDA). Drugs belonging to the following classes of anti depressants are used for treating insomnia arising due to depression:
a. Tricyclic Antidepressants: These drugs increase the levels of two neurotransmitters, norepinephrine and serotonin and block the action of acetylcholine in your brain. By restoring balance between these three neurotransmitters in the brain, depression can be reduced. By improving depression, insomnia also gets improved. These drugs also cause sleepiness.
Drug: Amitriptyline
Brand Name: Elavil
The U.S. FDA Status: Discontinued
Dosage form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Abdominal pain, agitation, bleeding gums, chills, coma, confusion, convulsions, difficulty in breathing and speaking
Drug: Doxepine
Brand Name: Silenor
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Abdominal pain, agitation, bleeding gums, blurred vision, canker sores, chest pain, convulsions and difficultly in breathing
Drug: Nortriptyline hydrochloride
Brand Names: Pamelor
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Abdominal pain, blurred vision, agitation, decreased urination, double vision, irritability, hostility and muscle spasm
b. Atypical Anti-depressants: These drugs are called atypical because they do not fit into any other class of anti-depressants. Each drug helps in treating depression in its own way. They help in lowering the levels of dopamine, norepinephrine and serotonin in the brain. They can also cause drowsiness and help a person in falling asleep.
Drug: Mirtazapine
Brand Name: Remeron
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless extremely important
Alcohol Content: No
Side Effects: Severe sedation, drowsiness, weight gain, fatigue, decreased appetite, tremor, bitter taste, dyspepsia, vertigo and palpitations
Drug: Trazodone
Brand Name: Desyrel
The U.S. FDA Status: Discontinued
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Blurred vision, dizziness, lightheadedness, sweating confusion about place, identity and time, fainting, swelling, nervousness and lack of coordination
Drug: Nefazodone
Brand Name: Serzone
The U.S. FDA Status: Discontinued
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Blurred vision, clumsiness, ringing in ears, skin rash, bladder pain, diarrhea, eye pain, dizziness, nausea, stomach pain, abnormal vaginal discharge and muscle stiffness
4. NSAIDs:
Insomnia due to pain can be managed by taking over-the-counter non-steroidal anti-inflammatory drugs (NSAIDs). These drugs help in reducing inflammation and have pain-killer action. They have an added advantage of not causing day time sleepiness. However, these should not be taken on a regular basis as they can cause a number of side effects like stomach ulcers, high blood pressure, liver or kidney problems and increased tendency to bleed while taking aspirin.
Drug: Ibuprofen
Brand Names: Advil
The U.S. FDA Status: Approved
Availability: OTC
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Abdominal pain, belching, bloating, cloudy urine, decreased amount of urine, diarrhea, nausea and rash
Drug: Aspirin
Brand Names: Aspirin
The U.S. FDA Status: Approved
Availability: OTC
Dosage Form: Capsule
Indicated in Pregnancy: 100 mg/day or less- Use with caution. Avoid in third trimester.
Alcohol Content: No
Side Effects: Abdominal pain, bloody urine, confusion, constipation, dark urine, diarrhea, fainting, fast breathing, fever, headache, heart burn, loss of appetite, muscle tremors and nausea
Drug: Acetaminophen (paracetamol)
Brand Names: Tylenol
The U.S. FDA Status: Approved
Availability: OTC
Dosage Form: Tablet
Indicated in Pregnancy: Yes, with caution
Alcohol Content: No
Side Effects: Nausea, abdominal pain, diarrhea, dyspepsia, anemia, rash and pruritis
Drug: Naproxen Sodium
Brand Names: Aleve
The U.S. FDA Status: Approved
Availability: OTC
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Belching, bruising, indigestion, headache, itching skin, swelling, bloating and double vision
5. Anti-Histamines:
These are drugs that are known to have sedating properties and are available as over-the-counter drugs for managing short term sleeplessness. These drugs enter into the brain and block the action of a neurotransmitter, histamine which is responsible for maintaining sleep/wake cycle. When the action of histamine gets disrupted, it causes drowsiness.
As anti-histamines have high potential of developing tolerance, these are not prescribed for treating long term insomnia. They are only minimally effective in inducing sleep, can reduce sleep quality and might even cause residual drowsiness during the day.
Drug: Diphenhydramine
Brand Name: Diphenhydramine
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless absolutely necessary
Alcohol Content: No
Side Effects: Disturbed coordination, epigastric distress, thickening of bronchial secretion, headache, dry mouth, diarrhea, confusion and hypotension
6. Anticonvulsants:
Drugs belonging to the classes GABA analog, benzodiazepines and barbiturates can help in treating insomnia by increasing the inhibitory effect of GABA, which is a neurotransmitter found in brain. Drugs belonging to this class decrease the communication occurring between neurons found in brain and hence promote relaxation.
a. Benzodiazepines:
Drug: Clonazepam
Brand Name: Klonopin
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Body aches or pain, fever, dizziness, ear congestion, cough, difficulty breathing and irritability
Drug: Lorazepam
Brand Name: Ativan
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Abdominal pain, aggressiveness, agitation, chills, confusion, convulsions, drooling, feeling sad, headache, increased thirst, loss of breathing control and memory
b. Barbiturates:
Drug: Phenobarbital
Brand Name: Luminal
The U.S. FDA Status: Disapproved
Dosage Form: Capsule
Indicated in Pregnancy: No
Alcohol Content: No
Side Effects: Behavioral problems, impaired memory, impaired cognition, life threatening respiratory depression, hallucinations, sweating, hypertension and rashes.
c. GABA Analog
Drug: Gabapentin
Brand Names: Neurontin
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Depression, dizziness, ataxia, lethargy, vertigo, headache, hypotension, nystagmus, rash, frozen shoulder, general joint pain and megaloblastic anemia
7. Anti-Psychotics:
Drugs belonging to the class atypical anti-psychotics is known to possess sedative action. They act as antagonists of dopamine and serotonin neurotransmitters, which promote wakefulness.
Drug: Quetiapine
Brand Name: Seroquel
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Chills, confusion, dizziness, blurred vision, chest pain, drooling, loss of balance control, painful or difficult urination, sweating and swollen gland
Drug: Olanzepine
Brand Name: Zyprexa
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Capsule
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Dizziness, hyperkinesia, weight gain, back pain, personality disorder, dyspepsia, dry skin and extrapyramidal reaction
Drug: Clozapine
Brand Name: Clozaril
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefits outweigh risks
Alcohol Content: No
Side Effects: Dizziness, fever, irregular heart beat, confusion, blurred vision, sweating, trembling, fatigue, anxiety, chest pain and chills
Drug: RisperidoneBehavioral problems, impaired memory, impaired cognition, life threatening respiratory depression, hallucinations, sweating, hypertension and rashes.
Brand Name: Risperdal
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefit outweighs risk
Alcohol Content: No
Side Effects: Agitation, dizziness, dystonia, extrapyramidal reaction, memory problems, skin rash, twisting body movements and restlessness
8. Orexin Receptor Antagonists:
Also known as hyprocretin, orexin is a neuropeptide that is involved in regulating arousal, appetite and wakefulness. It is thought to play an important role in regulating your sleep/wake states. Orexin promotes wakefulness. Drugs acting as antagonists at these sites help in suppressing the action of orexin and induce sleep.
Drug: Suvorexant
Brand Name: Belsomra
The U.S. FDA Status: Approved
Availability: Prescription only
Dosage Form: Tablet
Indicated in Pregnancy: No, unless benefit outweighs risk
Alcohol Content: No
Side Effects: Changes in behavior, nervousness, irritability, lack of appetite, irritability, suicidal thoughts, trouble concentrating and unusual dreams
OTC Drugs Used
| Diphenhydramine | Ibuprofen | Pracetamol | Naproxen | Aspirin | Doxylamine succinate | Nitrazepam |
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