What are Antihistamines doing in a baby?

What are Antihistamines doing in a baby?

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In his song Lullaby, Tim Minchin sings:

Your nappy is dry and your tummy is full
Of enough antihistamine to chill out a bull
Yet still all this gringing

According to Wikipedia, antihistamines are used against allergies.

So, why is there antihistamine in his baby's tummy and why is it supposed to make her sleepy?

This song most likely refers to an off-label (and usually inappropriate) use for certain antihistamines like Benadryl. They are sometimes used by parents to sedate their children, functioning through the exact physiological mechanisms @Chris describes. Parents use it inappropriately as a means of behavioral control for active or upset children to make them more docile or sleepy, such as for airplane rides, etc. It's not recommended by most pediatricians, because even though adverse (bad) side effects are usually rare, it is an actual medication with another primary mechanism of action having effects on many body functions, not a medication designed as a sedative.

This is not only happening in babies… In short (I will look for some references later and edit the post) the antihistamines are effective in the whole body and block the histamines there. The antihistamines which cross the blood-brain barrier do the same in the brain and hinder the small amounts of histamines which stimulate the nerve cells there from doing so. This results in the typical sleepyness.

Antihistamines for Treating Nasal Allergies

Daniel More, MD, is a board-certified allergist and clinical immunologist with a background in internal medicine.

Corinne Savides Happel, MD, is a board-certified allergist and immunologist with a focus on allergic skin disorders, asthma, and other immune disorders.

Histamine is a chemical released from allergic cells in the body (such as mast cells and basophils), usually in response to an allergen like cat dander or pollen.  

When histamine is released by allergic cells in the nose and eyes, the result is sneezing, runny nose, itchy eyes/nose/throat, nasal congestion, and post-nasal drip. These are the symptoms of hay fever, also known as allergic rhinitis.  

Antihistamines are medications that block the receptor for histamine, thereby stopping the symptoms that histamine causes. Antihistamines are the most commonly used medications to treat allergic rhinitis.  


Histamine makes blood vessels more permeable (vascular permeability), causing fluid to escape from capillaries into tissues, which leads to the classic symptoms of an allergic reaction — a runny nose and watery eyes. Histamine also promotes angiogenesis. [6]

Antihistamines suppress the histamine-induced wheal response (swelling) and flare response (vasodilation) by blocking the binding of histamine to its receptors or reducing histamine receptor activity on nerves, vascular smooth muscle, glandular cells, endothelium, and mast cells.

Itching, sneezing, and inflammatory responses are suppressed by antihistamines that act on H1-receptors. [2] [7] In 2014, antihistamines such as desloratadine were found to be effective to complement standardized treatment of acne due to their anti-inflammatory properties and their ability to suppress sebum production. [8] [9]

H1-antihistamines Edit

H1-antihistamines refer to compounds that inhibit the activity of the H1 receptor. [4] [5] Since the H1 receptor exhibits constitutive activity, H1-antihistamines can be either neutral receptor antagonists or inverse agonists. [4] [5] Normally, histamine binds to the H1 receptor and heightens the receptor's activity the receptor antagonists work by binding to the receptor and blocking the activation of the receptor by histamine by comparison, the inverse agonists bind to the receptor and both block the binding of histamine, and reduce its constitutive activity, an effect which is opposite to histamine's. [4] Most antihistamines are inverse agonists at the H1 receptor, but it was previously thought that they were antagonists. [10]

Clinically, H1-antihistamines are used to treat allergic reactions and mast cell-related disorders. Sedation is a common side effect of H1-antihistamines that readily cross the blood–brain barrier some of these drugs, such as diphenhydramine and doxylamine, may therefore be used to treat insomnia. H1-antihistamines can also reduce inflammation, since the expression of NF-κB, the transcription factor the regulates inflammatory processes, is promoted by both the receptor's constitutive activity and agonist (i.e., histamine) binding at the H1 receptor. [2]

A combination of these effects, and in some cases metabolic ones as well, lead to most first-generation antihistamines having analgesic-sparing (potentiating) effects on opioid analgesics and to some extent with non-opioid ones as well. The most common antihistamines utilized for this purpose include hydroxyzine, promethazine (enzyme induction especially helps with codeine and similar prodrug opioids), phenyltoloxamine, orphenadrine, and tripelennamine some may also have intrinsic analgesic properties of their own, orphenadrine being an example.

Second-generation antihistamines cross the blood–brain barrier to a much lesser extent than the first-generation antihistamines. They minimize sedatory effects due to their focused effect on peripheral histamine receptors. However, upon high doses second-generation antihistamines will begin to act on the central nervous system and thus can induce drowsiness when ingested in higher quantity. Additionally, some second-generation antihistamines, notably cetirizine, can interact with CNS psychoactive drugs such as bupropion and benzodiazepines. [11]

H1 antagonists/inverse agonists Edit

H2-antihistamines Edit

H2-antihistamines, like H1-antihistamines, exist as inverse agonists and neutral antagonists. They act on H2 histamine receptors found mainly in the parietal cells of the gastric mucosa, which are part of the endogenous signaling pathway for gastric acid secretion. Normally, histamine acts on H2 to stimulate acid secretion drugs that inhibit H2 signaling thus reduce the secretion of gastric acid.

H2-antihistamines are among first-line therapy to treat gastrointestinal conditions including peptic ulcers and gastroesophageal reflux disease. Some formulations are available over the counter. Most side effects are due to cross-reactivity with unintended receptors. Cimetidine, for example, is notorious for antagonizing androgenic testosterone and DHT receptors at high doses.

H3-antihistamines Edit

An H3-antihistamine is a classification of drugs used to inhibit the action of histamine at the H3 receptor. H3 receptors are primarily found in the brain and are inhibitory autoreceptors located on histaminergic nerve terminals, which modulate the release of histamine. Histamine release in the brain triggers secondary release of excitatory neurotransmitters such as glutamate and acetylcholine via stimulation of H1 receptors in the cerebral cortex. Consequently, unlike the H1-antihistamines which are sedating, H3-antihistamines have stimulant and cognition-modulating effects.

Examples of selective H3-antihistamines include:

H4-antihistamines Edit

H4-antihistamines inhibit the activity of the H4 receptor.

Are Antihistamines Safe During Pregnancy? Maybe Not

When I found out I was pregnant it was like I was back in college and needed to cram for a big exam. I was reading every pregnancy-related blog, magazine or book I could get my hands on so I could be prepared for what I𠅊nd my body—was about to go through. At my doctor&aposs visits, I was the annoying kid in class who kept raising her hand to ask yet another question. What can I say? Even though I hate to admit it, I&aposm Type A.

The internet is both a blessing and a curse when you&aposre pregnant, because you can Google anything and everything at any hour of the day to get answers, but there is so much conflicting information out there that you end up driving yourself crazy with worry.

I went into my check-ups thinking I had all of this medical knowledge from the internet, but most of the time my OB told me not to believe anything I read online𠅎specially when it came to medications and what was safe to take during pregnancy. (And even more importantly, what wasn&apost safe during pregnancy!) She told me what I could and couldn&apost take for cramps and headaches�taminophen was ok, but ibuprofen and naproxen weren&apost𠅊nd seasonal allergies—she suggested I not take anything, though Benadryl and Claritin were widely considered acceptable online.

Now a new study published in the European Journal of Obstetrics and Gynecology and Reproductive Biology conducted at UCLA with women who have hyperemesis gravidarum (HG), a severe form of morning sickness shared by Kate Middleton, show that those who took antihistamines (which are contained in many over the counter cold remedies, decongestants, sleep aids, and even products designed to relieve morning sickness) are significantly more likely to have premature births, babies with low birth weight, breathing and feeding problems, infections or developmental issues. In the study, more than 50 percent of the HG patients who experienced the above problems took some form of antihistamines.

While the study only proves a link between adverse birth outcomes in women with HG, it begs the question: Are antihistamines safe during pregnancy for any woman—whether she suffers from HG or not? Is taking something to relieve a short-term cold or allergy problem worth putting your unborn child at risk? Trying to figure this out on your own will drive you nuts. Consult your doctor before taking any over the counter medication—regardless of what you read on the internet. Your baby&aposs health is worth the extra effort.

TELL US: Have you given up any medications while pregnant? 

How Antihistamines Work

Allergic reactions are effectively your body’s immune response to a substance which is otherwise harmless. When a substance like pollen, pet dander or dust makes contact with your mucus membranes whether in the nose, throat, mouth or lungs an immune response occurs which causes histamine to be released.

Histamine is actually a protein and its release into your system is responsible for the many familiar allergic symptoms that you are so desperate to be free of.

Antihistamines, as the name implies, inhibit the production of histamines and prevent allergic reaction from happening.

If you suffer from allergies, then no doubt you have tried various antihistamine medications and you may well have also suffered from their side effects.

Fortunately there are alternatives to be found in nature and various foods and herbs may be an effective and much safer option. Let’s take a look at some of the best-known natural antihistamines.

Antihistamines May Not Be Safe During Pregnancy

Research has found that women who suffer from severe morning sickness while pregnant may have adverse reactions to antihistamines.

When you fall pregnant, you're suddenly confronted with a barrage of advice from everyone around you on what you should and shouldn't take when it comes to medications. There are the obvious no-no's, like Ibuprofen and Naproxen, but as it turns out, some medications previously regarded as safe should be avoided too. Most of what you read online tells you that it's perfectly fine to take Benadryl and Claritin for that pesky summer hayfever, but according to a study they could do more harm than good in the long run.

The European Journal of Obstetrics, Gynecology and Reproductive Biology conducted the research by looking at women who had severe morning sickness, known as hyperemesis gravidarum (HG). Their findings showed that those who took antihistamines explicitly for allergies or not (antihistamines are contained in cold remedies, decongestants, and sleeping aids) were far more likely to have serious complications in pregnancy, such as premature births, babies with a lower weight, or breathing or feeding issues. The study showed that more than 50% of the HG patients who experienced these problems took antihistamines.

Although the study shows a link between those women suffering from intense morning sickness and antihistamines, further research is needed to establish the long-term effects of an otherwise healthy mother taking the medication on a regular basis.

An estimated 23.7 million cases of hay fever are reported every year in the US alone, with the antihistamine business raking in millions of dollars annually. Even if you don't have hay fever, the handy tablets can stop other allergies in their tracks, such as pet or skin reactions. With so many of us quick to pop a pill or two for our ailments, it's important to be vigilant when you're self-medicating and pregnant. After all, there's a reason why a lot of store-bought medicines have the disclaimer, "Consult your doctor before taking."

Be sure to follow that advice and give your medical professional a visit before you go ahead. You can't trust everything that you read online!

Have you ever had to stop any medications while pregnant? Or have you found allergy relief without antihistamines? Let us know in the comments.

Top 5 natural antihistamines for allergies

People with allergies may find relief by using natural plant extracts and foods that act as antihistamines.

Antihistamines are substances that block histamine activity in the body. Histamine is a protein that triggers allergy symptoms, such as sneezing, itchy eyes, and a scratchy throat.

Over-the-counter (OTC) and prescription antihistamine medications are effective for symptom relief, but they can cause side effects, such as drowsiness and nausea. As a result, some people wish to try natural alternatives.

In this article, we describe the five best natural antihistamines, and we take a look at the science behind them.

Share on Pinterest There are a number of natural antihistamines that may help relieve allergy symptoms.

Vitamin C boosts the immune system. It also acts as a natural antihistamine.

According to a 2018 study on vitamin C in the treatment of allergies, oxidative stress plays a key role in allergic diseases. As vitamin C is a powerful antioxidant and anti-inflammatory, it may act as a treatment for allergies.

The researchers observed that high doses of intravenous vitamin C reduced allergy symptoms. They also reported that a deficiency in vitamin C might lead to allergy-related diseases.

Another study from 2000 suggests taking 2 grams (g) of vitamin C daily to act as an antihistamine.

The vitamin is present in many fruits and vegetables, including:

  • bell peppers
  • broccoli
  • cantaloupe melon
  • cauliflower
  • citrus fruits
  • kiwifruit
  • strawberries
  • tomatoes and tomato juice
  • winter squash

Vitamin C supplements, with and without bioflavonoids, are available in health stores, drug stores, and online.

Butterbur is a plant extract from a shrub that grows in Asia, Europe, and some parts of North America. People often use butterbur to treat migraines and hay fever, also known as allergic rhinitis.

According to the National Center for Complementary and Integrative Health (NCCIH), butterbur may have antihistamine effects.

A 2007 review of 16 randomized controlled trials, testing 10 herbal products, suggests that butterbur could be an effective herbal treatment for hay fever.

This review suggested that butterbur was better than a placebo, or as effective as antihistamine medications, for relieving allergy symptoms.

However, the authors of the review point out that some large studies received funding from industry manufacturers, and so further independent research is needed.

Most people tolerate butterbur well, according to the NCCIH , but it may cause side effects such as:

Raw butterbur extracts contain certain compounds called alkaloids that can cause liver damage and cancer. Extracts of butterbur that do not contain these substances are available. However, no studies have looked into the long-term effects of using these products.

The plant extract can also cause allergic reactions in people with sensitivities to ragweed, chrysanthemums, marigolds, and daisies.

Bromelain is an enzyme found in the core and juice of pineapples and is also available as a supplement.

Bromelain is a popular natural remedy for swelling or inflammation, especially of the sinuses and following injury or surgery.

Research on mice suggests that bromelain can reduce allergic sensitization and allergic airway disease thanks to its anti-inflammatory and anti-allergic properties.

In some people, oral supplementation of bromelain may cause adverse reactions such as:

Benadryl Baby: Should You Give Allergy Drugs to Calm Kids Before Flying?

My nightmare began at 10 p.m. on March 15 at John F. Kennedy Airport and lasted 12 long hours. I boarded a transatlantic flight with my one-month-old baby girl and my 18-month-old son. My goal was to spend the final month of my maternity leave with my family before going back to work.

My friends assured me that because it was a night flight, my children would sleep right through it. While no one conceded it would be a breeze, none warned me it would be akin to a scene from Dante's Inferno.

I do not blame my friends. After all, I had travelled overseas with my son when he was 4 months old and then again two months later with no major issues. The difference was I only had one child and he was a baby who could be calmed by breastfeeding. This time, he was a fully mobile and highly opinionated toddler who, as my mother would say, "is very, very hyper."

Upon boarding the plane, my son proceeded to wreak havoc (screaming at the top of his lungs, "Aaaaalllll done!" throwing his beloved toy cars and and food treats at nearby sleeping passengers, climbing onto aforementioned passengers while running down the aisle away from his desperate mother and, of course, hysterically crying for no discernable reason). He napped for only 30 minutes, during which time I sobbed while sitting on the edge of his chair. Half way through the trip, one flight attendant who had retrieved my son far too many times tapped me on the shoulder and said, "Why didn't you give him something?"

"Give him what?" I asked, genuinely puzzled.

"You know!" she snapped, "Something to make him sleep!"

"But he's a year and a half," I retorted.

After I recovered from my trip, I recounted my misadventure to a group of mothers who regularly travel with their toddlers, fully expecting them to dismiss or condemn the flight attendant for her unsolicited advice. Instead, they looked at me in shock and said - almost with one voice - "you didn't give him Benadryl or cough medicine or any antihistamine?"

The same advice was reiterated by two friends of mine when I returned to the U.S. One friend endorsed it saying, "I'm all for it! Morphine!" while another recalled how his sister had wanted to give her son 10 times the recommended dosage before boarding (he stopped her) and humorously added, "I believe we should petition the airline industry to remove emergency exits because I was going to use one mid-flight. It happened on the same flight as the one with my dear sister and my (non-Benadrlyled) nephew."

My flight attendant was not a lone voice in the airline industry. I discovered that "Good Morning America" had done a story on it in 2007 when a flight attendant from Continental ExpressJet flight gave the same advice to Kate Penland, who was traveling with her 19-month-old son, Garren. Her trip did not end as well as mine did, even though it seemed her son was much better behaved.

I decided to consult America's leading sleep and toddler expert, Dr. Harvey Karp, the creator of the DVD and Book, "The Happiest Toddler on the Block," and whose new book, "Happiest Baby's Guide to Great Sleep," will be on-sale June 12. He laughed when I told him my story and said, "It's so funny because I had a patient with the same experience. Their family was traveling from Los Angeles to South Africa. So I recommended Benadryl, but their child had a 'so-called' paradoxical reaction to it, which means that the child was acting like she had taken speed and she was driving everyone absolutely crazy."

"You recommend Benadryl?" I asked in disbelief.

His response: "Benadryl can be helpful when you are taking young children on a plane."

He explained that in his first book, "Happiest Baby on the Block," the key premise is that all babies are born three months before they are fully ready for the world and, thus, there is the "fourth trimester."

In "Happiest Toddler," the most important concept for parents to understand is that toddlers are not as much little children as "little cavemen!"

"No wonder they want to run up and down the aisles of the plane," said Karp.

When you do decide to take your little primate friend on a plane, Karp advises parents to be armed with lots of treats and toys, which should be given to them in stages (keep some hidden in a pocket that you only reveal when you are halfway through the trip), and to be prepared to walk them up and down the aisle for as long as they need.

Benadryl, he added, may be a help to put them to sleep and make them less jetlagged.

"Always start with the dose on the package, but ask your doctor if you can give more if it does not make your little one sleepy," he recommended.

However, Karp cautioned, to find out whether or not your child will have the opposite reaction, the best strategy is to try a dose on an afternoon a week before the intended trip. If the child becomes hyper, at least he or she would have time to run off their excess energy by bedtime. If not, then it would be close enough to nap time without disrupting his or her sleep pattern.

Once you are at your destination, Karp advised exposing your child to a lot of sunlight during the day to regulate the brain's melatonin (a sleep hormone) and to dim the lights one hour before bedtime to fool the body into adopting the new time zone.

Dr. Blair Hammond, who is a general pediatrician with a focus on medical education at Mt. Sinai Hospital, has a slightly different point of view.

"People ask me all the time" about giving their children Benadryl or any antihistamines, Hammond said. "Technically, it is not recommended to give your children anything before they fly."

She agreed with Karp that you run the risk of your child becoming hyper from the medication instead of drowsy. (Hammond said about 5 percent of children will have a "crazy" reaction.) If at all possible, she advised doing other things like "packing a good game bag" and "treats."

She conceded that Benadryl is "technically safe" for children older than six months and if a parent opts to do it, and that, apart from testing it out first, the dosage is 1.25 mg per kilo and should not be given more often than once every six hours. Hammond urged parents considering Benadryl before a flight to consult with pediatricians first because "every medicine has a side effect."

"I have two horribly behaved children on planes, but I have never given them Benadryl. I would rather give them lollipops," she said.

However, Hammond does recommend that traveling parents should pack Tylenol, ibuprofen and Benadryl, along with a thermometer, in their travel pack because Benadryl would be used should your child suffer from an allergic reaction.

Good advice, Drs. Karp and Hammond.

However, I have no imminent plans to take my son on a plane any time soon. My baby girl, for the record, was an angel and, thus, will not be relegated to my "no-fly list."

For all you traveling parents out there, please consult with your personal pediatrician before giving your children any medication. Treats, on the other hand, are a must!

The best antihistamines-third generation

As you are aware by now, first generation antihistamines can potentially cause problems because of their tendency to cause sedation. Second generation antihistamines such as loratadine and cetirizine were developed in the early 1980s, and they provided a distinct benefit in that they did not cause the antihistamine side-effects of sedation, among others. A problem developed, however, when some of these newer drugs were found to cause cardiac problems.

Third generation antihistamines may soon be the best antihistamines for many patients. They are now being developed in order to eliminate the possibility of cardiac toxicity. One of the first of these, fexofenadine, was approved in July of 1996, and more third generation antihistamines are under development.