Diseases

Sleep Aids And Stimulants Information

Antihistamines

Diphenhydramine (for example, Sominex, Nytol) and doxylamine (for example, Unisom) are antihistamines currently marketed as OTC sleep aids. Diphenhydramine is the only agent considered to be safe and effective by the Food and Drug Administration. Other uses for diphenhydramine include allergies, motion sickness, and cough suppression. Scientists believe that diphenhydramine and doxylamine cause sedation by blocking the action of histamine in the brain, but the exact mechanism of action is not known. If insomnia is associated with pain, there are numerous products containing a combination of an antihistamine and pain reliever. These combination products should not be used if pain is not present because the added pain reliever is not necessary. Pregnancy and lactation: The effects of diphenhydramine and doxylamine on the fetus have not been evaluated adequately. Diphenhydramine is classified as a pregnancy "category B" drug, and is routinely safely used during pregnancy. Although the likelihood of an adverse effect on the fetus is low, sleeping agents probably should be avoided during pregnancy. Both agents may decrease lactation (production of milk). Additionally, these drugs are secreted into the breast milk, which could affect the newborn. Nursing mothers should avoid both drugs. Consult a physician if you are pregnant and have insomnia. Children: Children less than 12 years of age should not use doxylamine because its use in this in age group has not been assessed. Elderly: Sedative effects of these drugs may interact with other potentially sedating medications. Consult a doctor before using these drugs. Drug interactions: Diphenhydramine and doxylamine add to the sedative effects of alcohol and other medications that cause drowsiness. Side effects: Drowsiness is the most frequent side effect of both diphenhydramine and doxylamine. These agents should not be used in situations where mental alertness is required (for example, driving). Diphenhydramine and doxylamine also cause constipation, dry mouth, and difficulty urinating. Both drugs may worsen the symptoms of glaucoma, asthma, heart problems, and prostate gland enlargement. People with these conditions should not use OTC sleep aids without consulting a physician. Both drugs may paradoxically cause excitation, resulting in nervousness and insomnia. This occurs most often in children and the elderly.

Caffeine

Caffeine (for example, NoDoz, Caffedrine) is the sole active ingredient in most non-prescription stimulants. It is the only drug approved by the FDA for this purpose. Caffeine is used for improving alertness and for staying awake. Caffeine is a powerful stimulant, but tolerance (the need to use increasing amounts) can be developed. Caffeine also is present in medications for menstrual cramps, headaches, and colds. Additionally, caffeine is found in coffee, tea, soft drinks, and chocolate. Caffeine increases alertness by stimulating the nerves in the brain and spinal cord. It decreases muscle fatigue by stimulating muscle contraction. Caffeine also increases the heart rate and the force of contraction of the heart. The effect of caffeine varies among individuals and some people are only affected minimally. Pregnancy and lactation: Studies have shown that moderate caffeine intake does not cause low birth weights, miscarriages, or premature births. However, there are reports of birth problems in women who consume more than 300 milligrams per day of caffeine. Daily caffeine intake should probably be limited to less than 300 milligrams during pregnancy. Caffeine passes into breast milk. The concentration of caffeine in breast milk is approximately one-percent of the amount in the mother's blood. A lack of sleep and irritation may occur in breastfed infants whose mothers consume more than 600 milligrams of caffeine per day. No adverse effects have been noted in breastfed infants whose mothers consume between 200-336 milligrams per day of caffeine. A mother can limit the amount of caffeine her infant receives by limiting the amount of her caffeine intake and ingesting the caffeine after nursing. Children: Caffeine is not recommended for children less than 12 years of age. Elderly: Older persons may be more sensitive to the effects of caffeine, and it may incrase the excretion of calcium from the body. In limited amounts, it is generally considered safe.Drug interactions: Cimetidine (Tagamet), norfloxacin Noroxin, ciprofloxacin (Cipro), and the estrogens in oral contraceptives block the break-down and elimination of caffeine from the body. Use of caffeine with these drugs could lead to increased levels of caffeine in the body and, therefore, a higher likelihood of side effects. Caffeine decreases the absorption of iron tablets. Iron should be administered one hour before or two hours after the consumption of caffeine. Caffeine decreases the effects of sedatives, and sedatives decrease the restlessness, alertness, and arousal caused by caffeine. Adverse effects: The most common adverse effects of caffeine are insomnia, nervousness, excitement, headaches, vomiting, diarrhea, and stomach pain. Caffeine also causes abnormal heartbeats and increases heart rate. Dependence can occur from the regular use of caffeine. If caffeine intake is stopped suddenly, a withdrawal reaction that consists of fatigue, headaches, anxiety, vomiting, and restlessness may occur. Symptoms of withdrawal start 12-24 hours after the last consumption of caffeine and may last for a week.

Melatonin

Melatonin (for example, Melatonex) is the only hormone available OTC for insomnia. Melatonin is a hormone produced by the pineal gland that helps regulate the body's clock or sleep-wake cycle. The secretion of melatonin is increased by darkness and decreased by light. The exact mechanism of how melatonin induces sleep has not been determined. Melatonin also decreases mental alertness and body temperature.Melatonin is sold as a dietary supplement and is, therefore, not regulated by the FDA. It is commonly used for jet lag, insomnia, and sleep disturbances related to working night shifts. Some limited evidence suggests melatonin may be useful for treating sleep disturbances.In 2005, MIT analyzed 17 peer-reviewed studies using melatonin. The analysis showed that melatonin was effective in helping people fall asleep at doses of 0.3 milligrams (mg). In some preparations the dosage of melatonin is significantly higher and these larger doses have shown to be less effective after only a few days of use. If possible, patients may want to stay with the same formulation or brand if it is effective for them.If a person would like to try melatonin tablets, consult a doctor first.Dosing: There is no established dose or time of administration. Individuals should follow the product labeling for dosing and administration.Pregnancy and lactation: The use of melatonin during pregnancy or lactation has not been studied adequately. Based on past experience with other agents and the possibility of unknown risks to the fetus, melatonin should be avoided during pregnancy while breastfeeding. Consult your doctor before you use melatonin if you are pregnant or breastfeeding.Children: The use of melatonin in children may be effective, particularly in children with disturbed sleep due to autism spectrum disorders. However, it should not be used as a first-choice treatment in children. Consult your pediatrician before giving your child melatonin for sleep.Drug interactions: Although melatonin is sold as a dietary supplement, it should be thought of as a drug. It has side effects and may have drug interactions that have not been identified. The level of melatonin that the body produces is increased by certain drugs, such as selective serotonin reuptake inhibitor antidepressants or SRRIs (for example, fluoxetine [Prozac], sertraline [Zoloft], paroxetine [Paxil]) and monoamine oxidase inhibitors (for example, tranylcypromine [Parnate], phenelzine [Nardil]). The interaction between these antidepressants and melatonin used as a sleeping aid has not been assessed.Side effects: The most common adverse effect of melatonin is drowsiness. Therefore, tasks that require alertness (for example, driving) should be avoided for four to five hours after taking melatonin. Melatonin also may also cause itching, abnormal heartbeats, and headaches. Melatonin appears to be safe when used short-term (less than three months). Long-term side effects of melatonin are unkown.Melatonin is either derived from animal sources or synthesized in a laboratory. Melatonin obtained from animal sources has a higher likelihood of contamination, which can cause allergic reactions and viral transmission, than synthetic melatonin.Melatonin may stimulate the immune system. People with severe allergies or other disorders that may be caused by an overactive immune system (for example, systemic lupus erythematosus, rheumatoid arthritis) should avoid using melatonin.Other herbal products: Natural herbal supplements such as valerian, chamomile, kava kava, and others have been touted as remedies for insomnia; however, the safety or effectiveness of these products has not been documented. Consult your doctor before taking any herbal supplements to treat insomnia.