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Sedatives

Antihistamines

Antihistamines are widely used for allergies and motion sickness. As they exhibit properties that can indirectly induce drowsiness, there is a class of antihistamines, sold as OTC sleeping pills. However, the American Academy of Sleep Medicine warns that such pills should be used only occasionally. Beware that there is a price to pay for buying OTC antihistamines. Some OTC sedatives combine antihistamines with pain relievers and some combine it with alcohol.


They can induce abnormal muscle spasms. Other side effects are blurred vision, constipation, diarrhea, nausea and vomiting, dry mouth and general dehydration. Therefore she needs to consume plenty of water if she is taking any antihistamine. In elders and children, antihistamines can cause nervousness and insomnia. Similarly, asthmatics should steer clear of antihistamines as these can aggravate their condition. They can affect the behavior of the fetus in the womb. Antihistamines also interfere with lactation. Be warned that OTC antihistamines should never be clubbed with alcohol or other sedatives.


Although it is construed that some antihistamines are non prescription sleep aids, and they are more sedating than prescription hypnotics, beware that their effectiveness may decrease over time. More importantly, OTC sedative is only meant for short-term insomnia and by and large the long term effectiveness and safety of the OTC drugs is questionable. However, for transient insomnia or insomnia based on illness or depression, antihistamines can be an effective OTC tool.


Sedative antihistamine list includes (the following list also contains suggested dosage for an adult. Always take the medications e.m.p (ex modo prescripto as directed by the physician):

  • Chlorpheniramine (Chlor-Trimeton) 4 mg every 4 to 6 hrs; maximum dose: 24 mg/day

  • Cyproheptadine (Periactin) , 4 mg at bedtime

  • Clemastine (Tavist), 50-100 mg every 4-6 hours, not to exceed 400 mg/day and it is supplied in table form chewable

  • Diphenhydramine (Benadryl), as a night sleep aid to be taken 30 minutes before bedtime, and the dosage is 50 mg for adults

  • Promethazine (Phenergan) Sedation: 25-50 mg orally or 50 mg rectally

  • Hydroxyzine (Atarax, Vistaril), oral sedation dosage 50-100 mg, IM 25-100 mg. Intravenous (IV), subcutaneous and intra-arterial administrations are not recommended as these can cause thrombosis and digital gangrene.


These come in various brand and trade names and they can be taken as tablets, syrups or nasal sprays. Droplet form for use in the eyes is also available. The effects of these antihistamines including drowsiness, dizziness, headache, loss of appetite, vision changes, irritability, dry mouth, stomach upset should subside, when the body begins to adjust with the medication. If these side effects continue, it is better to contact the medical practitioner. Sedative antihistamines may be taken with food and milk. Sustained release low acting tablets can be swallowed whole as chewing the sustained release long acting tablets may destroy the action and increase the side effects. Chewable tablets can be chewed thoroughly and swallowed. Suspensions should be shaken before food consumption.


Melatonin

This is a hormone produced by human body – by the pineal gland, a pea-sized structure at the center of the brain. This regulates sleep and wakefulness. Taken as a supplement, melatonin helps to reduce delayed sleep syndrome. This also improves sleep quality and lengthens the period of sleep. Day time alertness also seems to improve when this is taken. Melatonin can treat insomnia without altering the sleep pattern of the individual. It also does not impair any performance related skills.


This may help elders with insomnia as the amount of melatonin produced in the body seems to decrease as one gets older, although it is not recommended for chronic insomnia. Melatonin works on the circadian rhythm – the biological clock that regulates our sleep and wake cycles. Many become melatonin deficient due to age, work schedules and stress. Melatonin supplements are a quick way to adjust the lack of melatonin in the body and rebalance the sleep cycle. These are available OTC and when used in conjunction with herbs like chamomile and lemon balm, help lull the body to sleep acting as a true sedative.

Although Melatonin shows good effects for the treatment of insomnia, if used in excess, this sedative can produce side effects including sexual irregularities, mood swings and depression. Although by and large safe when used in moderation, it is unsafe for small children and pregnant women to use melatonin supplements. It is also not recommended for those with lymphoma, extreme allergies, depression, rheumatoid arthritis, auto immune diseases and for cancer patients. Some melatonin sedatives include:

  • clonazepam (Klonopin)

  • lorazepam (Ativan)

  • phenobarbital (Donnatal)

  • zolpidem (Ambien)


As such Melatonin can cause sleepiness and drowsiness, and if taken with sedatives that cause sleepiness, then too much of sleepiness can result. Research indicates that quick release Melatonin can be more effective than sustained-release formulations, especially when used as sedatives. Intramuscular injections of 20 mg of Melatonin are also available.


SAMe

This is also found naturally in the body. This OTC aid can not only help to sleep but also treats depression and chronic fatigue by promoting serotonin production in the body. Unless consumed in large quantities, SAMe has no known side effects.


Antidepressants used as sedatives

Although the FDA has not approved the use of antidepressants as sedatives, there are those who believe that insomnia is related to depression. As with any other medication for depression, there is a significant risk of suicidal thoughts particularly in adolescents and children. Approximate dosage of antidepressants s.o.s (si opus sit only if there is a need) :

Citalopram 20 mg
Escitalopram 5-10 mg
Fluvoxamine 100 mg
Fluoxetine 20 mg
Paroxetine 20 mg
Sertraline 50-75 mg
Venlafaxine 75 mg
Donormyl sleeping pills are available without prescription and they are approved by the FDA for non-prescription. They are used in the treatment of insomnia. 25 mg of Donormyl is the strongest non-prescription sleeping pill. Possible common side effects of antidepressant sedatives include diarrhea, dizziness, headache, insomnia, rash, vomiting, blurred vision, decreased appetite, cold symptoms, nervousness, cramps, hallucinations, hair loss and decreased coordination.


OTC sedatives side effects

Although OTC sedatives can be effective for an occasional sleepless night, the longer you take them, the less they are likely to make you sleepy. OTC sleep aids can leave you feeling groggy and unwell the next day. This is like the 'hangover' effect. Much remains unknown about the safety and effectiveness of OTC sleep aids.

Dizziness and forgetfulness, clumsiness, feeling off balance, dry mouth and throat are some common side effects. Serious risks of OTC sedatives include severe allergic reaction, facial swelling, memory lapses, hallucinations, suicidal tendencies, sleep-related complexities such as sleep-walking, sleep-driving, and sleep-eating. If any unusual sleep-related behavior is exhibited, consult the doctor immediately.


Over-the-counter sedative tips


  • Consult the doctor before taking OTC sedative, although you do not need the doctor concurrence to buy an OTC drug. This is because your doctor can make sure that the sedative does not interfere with other underlying medications.
  • Certain OTC drugs are not recommended for those with glaucoma, asthma, chronic pulmonary disorders, liver diseases and urinary retention.
  • Remember that OTC sedatives are only a temporary solution for insomnia and they are not intended to be used for longer than about two weeks.
  • Persistent insomnia is a symptom of an underlying medical or psychological problem. These cannot be cured with OTC sedatives. It is better to learn about safer and effective way of end sleepless nights.
  • Never mix alcohol with sedatives and this can increase the sedative effects of the medication.
  • Combining medications such as OTC sedatives and pain relievers and allergy medicines is very dangerous.
  • Do not drive or attempt any other activity that may require alertness while taking a sedative.
  • Over a period of time, you may build up intolerance to sedatives and this can in turn lead to more side effects.
  • You may also come to rely on sedatives and will be unable to sleep without them.

Thalidomide

Certain skin conditions like Multiple Myeloma (a type of Cancer due to abnormal plasma cells), Hansen's disease (Leprosy) can be treated or the symptoms mitigated using thalidomide. It reduces redness and inflammation in Hansen's disease. It reduces the formation of blood vessels that feed tumors and thus is used extensively in cancer treatment. Thalidomide is an immunomodulatory agent. It works on the immune system to decrease certain substances that cause skin inflammation. Thalidomide is also prescribed for treatment of Sarcoidosis, HIV and Crohn's disease.


Thalidomide as a drug was primarily developed and used as a sedative to treat insomnia, anxiety and tension. The drug is also known as Asmaval, Valgis, Tensival, Distaval Forte and Valgraine. The drug that was popular as a wonder drug was banned in the early 1960s as it was found to cause deformity in children born to mothers who consumed this drug. Thalidomide caused severe to life threatening birth defects when either the father or mother consumed it during the time of fetal conception. Studies prove that this drug did cause birth defects in body parts like the eyes, face, heart, legs, bones and ears. Thalidomide blocked the formation of blood vessels thereby limiting blood flow and creating limbless babies.


In the 1970s thalidomide was used to treat leprosy. Later it was used as an anti-angiogenic - to stop the formation of new blood vessels. The same property of the drug which caused birth defects actually played a vital role in shrinking tumors. Thalidomide is used to treat cancer as it:


  • Can block blood vessels and limit blood flow.
  • Stop growth of blood vessels that can feed cancerous growth in the body.
  • Stabilize blood flow around the site of the tumor.
  • Once blood flow is stabilized around the tumor affected area, treatments like chemotherapy reach more effectively to the affected area.
  • Thalidomide also plays a role in preventing cancer from recurring, post chemotherapy.

Using Thalidomide

This medication should be taken orally. It is usually taken at bedtime, an hour after taking a meal. Handle the capsules with care; do not take them out of the blister pack if not being used immediately. Do not break the capsule. In case of skin contact with the powder, wash the area with soap and water. Hands should be washed thoroughly after handling the drug.

Pregnant women should not consume this drug. Doctors provide dosage based on the prevailing conditions, dosage should not be increased or decreased by the patient. Increase in dosage can cause serious side effects. Do not donate blood or sperm while on this drug. Avoid sexual contact while on this drug as the semen carries the drug in it. To get the maximum benefit of this drug, it has to be used regularly and should not be stopped suddenly. Stopping intake of the drug suddenly may worsen the condition.

While on this drug, make sure that your blood does not come in contact with any other person's blood. Thalidomide can make a person feel sleepy; hence alcohol should not be consumed while on this drug.


Thalidomide side effects

Side effects may vary from person to person. Common side effects include dizziness, chest pain, risk of blood clots, general weakness, racing heartbeat, dry skin, seizures and muscle cramps. Nerve damage may cause permanent damage in a few cases. Rare side effects include blood in urine, low blood pressure, reduced urination and fever without rash.



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Bibliography / Reference

Collection of Pages - Last revised Date: November 22, 2019