Doxylamine is an antihistamine that can be used as a sleeping aid and for overnight cough and cold relief. It can be combined with the pain-relievers paracetamol, codeine and pregabalin. With its “A” fetal safety rating in the Briggs’ Reference Guide, doxylamine is sometimes prescribed — along with vitamin B6 — to treat morning sickness in prenatal women. Doxylamine succinate doses of 25 mg and under are used in prescription and over-the-counter medicines. The drug can be used with decongestants, but doing so is known to cause side effects that range from minimal to severe. While the drug has hypnotic and anesthetic effects, it is not related to antidepressants.
As part of the ethanolamine group, doxylamine is second only to diphenhydramine as the most powerful anti-allergen on the antihistamine market. Doxylamine is also the strongest prescription sleeping aid in the U.S., even more so than phenobarbital. In other countries, doxylamine is marketed under the names Dozile (Australia), Vomentin (India) and Valocordin-Doxylamine (Russia).
Formulations of Doxylamine
Doxylamine is mainly used as doxylamine succinate — a succinic acid — and is the active ingredient in various medications around the world, including the following:
- In NyQuil, doxylamine is the sedative within a three-agent formulation along with acetaminophen and dextromethorphan.
- Doxylamine is sold as a pain-reliever in combination with codeine and paracetamol (acetaminophen) under various names — Dolased, Mersyndol and Propain Plus — in Canada, Oceania and South Africa. In 2015, a similar drug in the United Kingdom was taken off the market.
- Sleep aids sold to the general public throughout Europe and the Commonwealth use doxylamine, including the French drug Donormyl, the Iberian drug Dormidina and the South African drug Somnil.
- In the U.S., the Unisom brand — which otherwise uses diphenhydramine hydrochloride — contains doxylamine succinate in its SleepTabs product, which is sold over-the-counter.
- Until recently, Unisom sold SleepGels — another sleep aid with doxylamine succinate — to Canadian consumers. Now, the drug maker’s gel caps contain diphenhydramine hydrochloride.
- Evanorm by Ion Healthcare is made from a mixture of doxylamine, folic acid and vitamin B6.
- Diclectin, sold in Canada, is an anti-morning sickness drug made from a combination of doxylamine succinate and vitamin B6.
- In April 2013, the FDA approved Diclegis, an anti-morning sickness medicine containing doxylamine succinate and vitamin B6, for U.S. consumers. For pregnant women, the drug has been given a class A rating of safety.
Doxylamine Addiction: Does It Occur?
Doxylamine is not an addictive substance. When people come off of medications that contain the antihistamine, withdrawal symptoms are an unlikely occurrence. As a drug without euphoric or energizing effects, there’s no phenomenon of doxylamine succinate recreational use. However, even though no one takes a doxylamine succinate trip, a range of mental and physical side effects could result if a dose is exceeded beyond the daily amount that doctors recommend.
Before taking doxylamine, you should consult your doctor to see whether you have any of the following conditions: asthma, hypertension, glaucoma, prostate trouble, lung disease, ulcer, liver disease or heart problems. You should also seek a medical consultation about using the antihistamine if you plan to get pregnant. The daily rundown of doxylamine usage is as follows:
- Doxylamine is administered in tablet form at dosages of 25 mg.
- Prescriptions are not meant to exceed one dose per day.
- An average dose of doxylamine stays in effect for anywhere from six to eight hours.
- The best time to take doxylamine is 30 minutes before bedtime.
If sleeping problems persist for more than 14 days after beginning the medication, your doctor should be notified immediately.
Interactions With Other Drugs
As with numerous medications, doxylamine can come into conflict with other substances, such as the following drugs:
- Anxiety suppressants
- Pain killers
Of particular concern are drugs that impact the nervous system, such as opioid analgesics and antimuscarinic medications, none of which should be taken with doxylamine.
Doxylamine and Alcohol
The consumption of caffeine, alcohol, tobacco and hard drugs can also cause reactions when mixed with doxylamine. Before starting doxylamine, talk with your doctor about any other drugs, supplements or herbal remedies you’re currently taking to see whether there could be side effects. Also notify your doctor if allergies don’t subside after two days of taking doxylamine.
Doxylamine Succinate Side Effects
Symptoms to watch out for when taking doxylamine include dizziness, drowsiness, fever and shortness of breath. Doxylamine Succinate side effects include the following:
Furthermore, people with allergic reactions to doxylamine might experience the following symptoms:
- Difficulty with eyesight
If you experience any of these side effects while on doxylamine, notify your doctor immediately.
Due to the drug’s sedative effects, it’s inadvisable to operate vehicles or machinery while a dosage is active in your system. For older folks especially, doses should be administered with caution if side effects like dizziness or fainting could be a factor. Doxylamine should never be mixed with alcoholic beverages, which can exaggerate the drug’s sedative effects.
To avoid the risk of doxylamine dependency, pay attention to dosage advice and instructions that come with your prescription. Never exceed the recommended dose amount without first consulting your doctor for guidance. In the event of an overdose, call your doctor or the nearest emergency center right away.
Doxylamine and Children
Not much is known about the effects of doxylamine on young children at present, so the drug should not be used by anyone 12 or under. Antihistamines in general should never be administered as sleeping aids for children, who are likelier to have nervous systems that are more prone to the effects of doxylamine, even in smaller amounts. This can lead to overdoses for kids in that age group.
Doxylamine Abuse: The Serious Side Effects
Overdoses of doxylamine succinate can lead to serious side effects, such as convulsions, disorientation and tremors. Extreme usage has also been tied to rhabdomyolysis, a condition that causes rapid deterioration of skeletal muscle. Furthermore, an overdose of the antihistamine can possibly lead to kidney failure or even a comatose state.
Doxylamine and Pregnancy: The Bendectin Controversy
Up to four-fifths of pregnant women between six weeks and three months of gestation suffer vomiting and nausea. Approximately a third of these women are affected to an extent that jeopardizes their overall quality of life. Roughly one percent of prenatal women suffer what is known as hyperemesis gravidarum. This is a condition marked by vomiting, dehydration, lagging nutrition, imbalanced electrolytes, drastic weight loss and diminished nutrition; the condition can be very dangerous for expectant moms and fetuses.
A combination of doxylamine succinate and pyridoxine hydrochloride (vitamin B6), Bendectin was originally brought to market to help expectant moms combat vomiting and nausea in the early stages of pregnancy. Bendectin first hit the market in 1956, when it consisted of 10 mg each of doxylamine, pyridoxine and dicyclomine hydrochloride. The last of those was dropped from the formula during the 1970s, when it was found that dicyclomine offered no remedial benefits against pregnancy-related vomiting and nausea.
In 1976, Bendectin gained approval as a two-agent formula. At the height of the drug’s popularity in the U.S., one-fourth of pregnant women were using Bendectin.
During the early 1980s, Bendectin aroused safety concerns after reports surfaced of birth defects that were being associated with the drug. As the general news media caught wind of these claims, law firms began closing in on Bendectin, claiming that the drug was a teratogen (an agent of malformation in an embryo). Starting in 1980, a series of lawsuits linked the drug to assorted birth defects; over 300 lawsuits were pending by the time the drug was yanked from shelves in 1983. Conditions associated with the drug included cleft palates, limb deformities, genital malformation and heart trouble.
The ultimate withdrawal of Bendectin from the market came down to financial matters following the lawsuits. After the initial allegations, the drug’s manufacturer incurred a $10 million annual rise in insurance premiums, which came within $3 million of wiping out the profit margin from Bendectin sales.
Doxylamine and Birth Defects: No Verifiable Link
In a 1979 FDA document, it was observed that animal studies showed no link between Bendectin and birth defects. The following year, 11 out of 13 studies conducted by the FDA Fertility and Maternal Health Drugs Advisory Committee found no correlation between the drug and birth defects, while two showed only a minor bit of evidence that possibly linked Bendectin to cleft palates and heart trouble. The committee concluded that there wasn’t sufficient evidence to hold the drug accountable for birth defects, but it did suggest that the labels on Bendectin be revised to let consumers know that further reviews were being conducted.
Doxylamine: Not a Teratogen
After the drug was taken off the market, two further Bendectin analyses were conducted, neither of which showed any conclusive proof that the drug was a human teratogen. One analysis examined 17 studies that took place between 1963 and 1985; the other examined 27 studies that occurred over a 28-year period, starting in the early 1960s.
The supposed link between Bendectin and birth defects was also debunked in a study by the Birth Defect Monitoring Program of the Centers for Disease Control and Prevention (CDC). Here, it was examined that between 1985 and 1987, between two and four years after the drug was pulled from the market, the rate of birth defects was the same as it had been between 1978 and 1980 — when use of the drug was at its height. This was a considerable finding, since nearly a fourth of all pregnant women in the U.S. were using Bendectin at the start of the 1980s.
Doxylamine for Pregnant Women: Benefits Outweigh Detriments
Beyond the lack of evidence produced during this time to support the notion that Bendectin was a teratogenic drug, there were actually some indications that its withdrawal from the market may have instead been detrimental to pregnant women. Data compiled by the National Center for Health Statistics showed that cases of nausea and vomiting among prenatal women more than doubled between 1981 and 1987 — averaging 16 cases per 1000 births — over the preceding six-year timeframe. What isn’t known is the number of women who may have had abortions out of fear that their actions, while pregnant, may have damaged their fetuses.
Scientific evidence is always the foundation on which to determine the safety and effectiveness of doxylamine-pyridoxine. After a series of placebo-controlled trials showed that there are no teratogenic effects from the two-agent formulation of doxylamine succinate and pyridoxine hydrochloride, Diclegis was approved by the FDA. While the formulation has long been the most researched form of treatment for pregnancy-related health problems, the agency will continue examining the effects of Diclegis now and into the future.
The approval of Diclegis — which replicates the formula of an earlier drug that was taken off the market due to inconclusive data — shows the importance of using evidence from a variety of studies over a lengthy period of time to determine whether a drug should be released on the market.
The 12 Keys Rehab Model
Doxylamine may not be chemically addictive, but use of medications that contain the antihistamine can cause serious ill-effects if allergic reactions persist or daily doses far exceed the recommended usage. If you have been taking excess amounts of doxylamine to cope with stress, insomnia, prenatal nausea or other issues, there could be a more serious problem at hand. The best place to overcome dependency on illicit and over-the-counter drugs is 12 Keys Rehab Recovery Center.
At 12 Keys Rehab, we approach treatment on a client-by-client basis. Early into a treatment cycle, we evaluate a client’s response to various surroundings and situations to pinpoint what exactly drives his or her addictive impulses. This process helps us to determine the best course of treatment for each individual.
Clients at our center take part in daily 12-step group meetings where everyone shares their struggles with substance abuse and the progress they’ve made with the program. Through this peer-based setting, each client understands that addiction affects people from all walks of life and that no one is alone in their fight to overcome a dependency.
Here at 12 Keys Rehab, we know about the trauma that addiction can cause sufferers and their families, as some of our own staff have overcome similar personal experiences. If you or a person close to you is suffering from dependency, addiction or withdrawal symptoms, get in touch with 12 Keys Rehab Center today to learn more about what we offer.