Medication and Mast Cell Disease

I wrote this article to provide an overview of the most common medications prescribed in mast cell disease, so readers are more confident discussing this topic with their medical team. I am not recommending any medication. Always consult your physician and pharmacist before taking medication, even over the counter medication. The chemical name and the most common brand names in Canada/United States are listed. The brand names may be different in other countries. I’ve also indicated if a generic version is available. The generic name will include the chemical name (and usually the company that produces it). Double check this information with your physician and pharmacist.

Good communication with your medical team is essential to find the most effective medications. Clients with the same diagnosis/symptoms will often have a different mix of medication to manage their symptoms. It is extremely important to find a physician and pharmacist that you are comfortable with.  The physician/pharmacist’s role is to:

  • provide information about the medications,
  • discuss any concerns the patient has,
  • work with the patient to make decisions about what medications to trial,
  • listen to the patient's feedback about how the medication is working.

The patient's role is to:

  • inform the medical team of current medications and supplements,
  • take the medication exactly as prescribed,
  • be systematic (e.g., don't start other treatments at the same time as new medication),
  • keep track of symptoms to discuss with the physician/pharmacist.

Many patients are reluctant to take medication because they are concerned about the side effects. Minimizing your symptoms through diet and lifestyle changes (especially relaxation) is very important, but sometimes this is not enough, and medication is necessary. Internet information about side effects is often inaccurate and exaggerated. A knowledgeable pharmacist is usually the best source of accurate information. Medication companies must conduct clinical trials to determine side effects and list any reported side effects on the medication label.  Keep in mind that natural supplements can have side effects as well. Unfortunately, these companies are not required to conduct clinical trials and list side effects, which gives the appearance of safety. When I had young children, I was amazed at how many parents would not give their baby Tylenol for teething pain, because of the potential liver damage (only if used at very high doses, over a long period). However, many would give supplements with the potential of completely unknown side effects.

For clients with mast cell activation syndrome, an excellent section on medication is available in Never Bet Against Occam: Mast Cell Activation Disease and the Modern Epidemics of Chronic Illness and Medical Complexity (2016) by Dr. Afrin. If you have a willing physician, he/she could use this information to help you through medication trials.

Common medications prescribed for mast cell disease symptoms are listed below.  In general, these medications have three different main actions (some of these medications fit into more than one category):

ActionExample Medications
Stabilize mast cells so inflammatory chemicals are not released Sodium Cromolyn
Ketotifen
Block the action of specific inflammatory chemicals.
Antihistamines (histamine inhibitors) Leukotriene inhibitors
Prostaglandin inhibitors
Reduce inflammation, regardless of the cause.
Corticosteroids

Sodium cromolyn is not absorbed into the body and likely works by stabilizing mast cells where it is applied (i.e., digestive system, eyes, nose, etc.).

Taken by mouth

Sodium cromolyn is available in liquid or capsules and is taken before meals.

Chemical NameCanadaUnited States
Sodium CromolynNalcrom Gastrocrom

Eye drops

Chemical NameCanadaUnited States
Sodium CromolynOpticromNot available

Nasal spray

Chemical NameCanadaUnited States
Sodium CromolynRhinaris- Anti-Allergic Nasal Mist
Generic
NasalCrom

Inhalation (nebulizer)

Chemical NameCanadaUnited States
Sodium CromolynGeneric
Not available

Taken by mouth

Ketotifen is available as a syrup or tablet. The timing is not related to meals. It is absorbed into the body and works as a mast cell stabilizer and an H1 antihistamine (see below for an explanation). Prevention of allergic asthma is the most common use.

Chemical NameCanadaUnited States
KetotifenZaditen
Generic

Not available

Eye Drops

Used to treat allergic conjunctivitis (allergic reaction in the eye).

Chemical NameCanadaUnited States
KetotifenZaditor

Zaditor
Alaway
Claritin Eye
Refresh Eye Itch Relief
Thera Tears Allergy
ZyrTEC Itchy Eye

Antihistamine medication blocks the effect of histamine. Mast cells are like tiny balloons filled with inflammatory chemicals – such as histamine. There are mast cells throughout the body, especially where the body meets the outside world (e.g., digestive, respiratory, urogenital systems & skin). Inflammatory chemicals leak out of mast cells (called mast cell activation or degranulation) primarily during an immune response (e.g., defending the body against germs) or allergic reaction. Histamine is the most well-known inflammatory chemical. Histamine moves through the body in the blood. The organs have four different receptors for histamine. A very simplified summary is:

  • When histamine binds to H1 receptors: 1) blood vessels dilate and become leaky (fluid leaks from blood vessels into surrounding tissue, contributing to tissue swelling) 2) nerves tingle (itching), 3) respiratory tubes contract (difficulty breathing) 4) mucus production increases. 5) Etc.
  • H2 receptor stimulation increases stomach acid production and may lead to digestive upset, such as heartburn.
  • The effect of H3 & H4 receptor stimulation is not well understood, but probably affects the central nervous system.

Antihistamine medications bind to the receptors, which prevents histamine from binding and changing how the organ functions (e.g., blocking the H1 receptors will reduce the blood vessel dilation).  Also, mast cells have histamine receptors. Stimulation of these receptors can lead to mast cell activation, so antihistamine medications could also be classified as mast cell stabilizers.

There are many reports on the internet that antihistamine medications cause the body to produce more histamine. To my knowledge, there is no research to prove or disprove this. However, if this were true, the side effect of H1 antihistamines would be increased stomach ulcers, and reflux (i.e., increased acid) and the side effect of H2 antihistamines would be increased allergic symptoms. These are not common side effects listed with these medications.

H1 Antihistamines (block H1 receptors)

Taken by mouth:

First Generation: Diphenhydramine was the first antihistamine developed. It is the fastest acting and is often used to treat acute allergic reactions (in conjunction with epinephrine, see below). Diphenhydramine is in many cold medications, but I’ve only listed the medications which are 100% diphenhydramine.

Chemical NameCanadaUnited States
DiphenhydramineBenadryl
Generic


Benadryl
Generic

Second Generation: These antihistamines were developed later and had fewer side effects (especially less sedation). Each of these medications is a different chemical and binds to H1 receptors differently. Therefore, the side effects and effectiveness can vary between individuals. Work with your doctor and pharmacist to experiment and find the best one for you.

Chemical NameCanadaUnited States
CetirizineReactine
Extra Strength Allergy Relief
Aller-Relief
Generic
All Day Allergy
ZyrTEC
Generic
DesloratadineAerius
Generic
Clarinex
FexofenadineAllegraAllergra
Mucinex Allergy
Generic
LoratadineClaritin
Generic

Alavert
Allergy Relief
Claritin
Loramed
Triaminic Allerchews
Generic

Eye drops:

Chemical NameCanadaUnited States
AzelastineNot availableOptivar
EmedastineNot availableEmadine

Nasal Spray:

Chemical NameCanadaUnited States
AzelastineAstelinAstelin
Astepro

H2 Antihistamines (block H2 receptors)

These chemicals bind to H2 receptors. They are commonly used to treat ulcers and gastroesophageal reflux.

Chemical NameCanadaUnited States
CimetidineGenericTagamet
Generic
Famotidine Pepcid
Acid Control
Generic
Pepcid
Acid Reducer
Heartburn Relief
NizatidineAxid
Generic
Axid
RanitidineZantac
Acid Reducer
Generic
Zantac
Acid Reducer
Deprizine FusePaq

 

Leukotrienes are a group of inflammatory chemicals produced during mast cell activation, so the effects are more delayed compared with histamine (because histamine is stored in mast cells and is released immediately upon activation). Leukotrienes have diverse effects throughout the body, including swelling and narrowing of the respiratory tubes. The most common use of leukotriene inhibitors is asthma and season allergies.

Chemical NameCanadaUnited States
MontelukastSingulair
Generic
Singulair
ZafirlukastAccolateAccolate

Prostaglandins are another group of inflammatory chemicals produced during mast cell activation. Non-steroidal anti-inflammatory medications (NSAID’s) block the enzymes which produce prostaglandins. Several different types are listed below. Aspirin is the most commonly prescribed NSAID in mast cell disease . In addition to reducing inflammation, NSAID medications reduce pain, and some also reduce fevers.

Chemical NameCanadaUnited States
Acetylsalicylic acidAspirin
Entrophen
ASA
Many different names
Aspirin
Ascriptin
Many different names
IbuprofenAdvil
Caldolor
Motrin
Generic (also called profen)
Advil
Caldolor
Addaprin
Dypel
Enepril
Motrin
Generic (also called profen)
IndomethacinGenericIndocin
Tivorbex
NaproxenAleve
Naprosyn
Generic
Aleve
Anaprox
Flanax Pain Relief
Generic

Corticosteroids reduce inflammation by suppressing the immune system. They are a synthetic version of cortisol, which is a hormone produced by the immune system. In most cases, they are used for short term treatment.

Taken by mouth

Corticosteroids are absorbed into the body and are used to reduce inflammation throughout the body.

Chemical NameCanadaUnited States
PrednisoneWinpred
Generic
Deltasone;
PredniSONE
Intensol
Rayos
HydrocortisoneCortefCortef
BudesonideEntocortEntocort
Uceris

Creams

Reduces inflammatory skin rashes.

Chemical NameCanadaUnited States
Betamethasone valerateBetadermBetaderm
Mometason furoateElocomElocom
HydrocortisoneHydermHyderm
Clobetasol propionateDermovateDermovate
Fluticasone CutivateCutivate
MometasoneElocom
Generic
Elocom

Nasal sprays

Reduces inflammation in the nasal passages, sinuses and surrounding tissues.

Chemical NameCanadaUnited States
Beclomethasone Rivanase
Generic
Beconase
Qnasl
BudesonideRhinocort
Generic
Rhinocort
CiclesonideDrymira;
Omnaris
Omnaris
Zetonna
Fluticasone Flonase
Avamys
Generic
Flonase
Veramyst
MometasoneNasonex
Generic
Nasonex
Propel Mini

Inhaled through the mouth

Chemical NameCanadaUnited States
Beclomethasone Qvar
Qvar
BudesonidePulmicort Pulmicort
CiclesonideAlvescoAlvesco
Fluticasone Flovent
Arnuity Ellipta
Flovent
Arnuity Ellipta
MometasoneAsmanexAsmanex

Eye drops

Reduces inflammation in the eyes, eye lids and surrounding tissue.

Chemical NameCanadaUnited States
Loteprednol Alrex
Lotemax
Alrex
Lotemax
DifluprednateDurezolDurezol

An epinephrine auto-injector may be prescribed if a patient has experienced anaphylactic symptoms. Epinephrine (also called adrenaline) is a hormone that is released in the body when we are scared (flight or fright syndrome). It can temporarily reduce anaphylactic symptoms, by opening the airways, improving blood pressure and increasing the heart rate.

Chemical NameCanadaUnited States
EpinephrineEpiPenEpiPen
Impax
Adrenaclick
Auvi-Q

 

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