Medication for Systemic Mast Cell Activation Disorders (MCAD)
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Medication for Systemic Mast Cell
Activation Disorders (MCAD)
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(mast cell activation syndrome MCAS, systemic mastocytosis SM,
mast cell leukemia MCL, histaminosis)
Therapeutic strategy for MCAD
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Active ingredients of medications, medical products, food supplements and foods for special
medical purposes: Mechanisms of action, application, advantages and disadvantages
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Recommendations for use in basic therapy, symptomatic adjunctive therapy and in special
situations (premedication before medical interventions and dental treatments, allergies, an-
aphylactic shock, infections, vaccinations, pregnancy and lactation, mental illnesses)
Guidance for the assessment of compatibility of products
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With references to the scientific literature
version 2019-01-03
Author: Heinz Lamprecht, MSc
Translated by Dr. med. Matthew Chaney
Publisher: Swiss Interest Group Histamine Intolerance (SIGHI)
www.mastzellaktivierung.info
© Copyright by Heinz Lamprecht, www.mastzellaktivierung.info
Table of Contents SIGHI Medication Manual: Medical treatment in histaminosis
Copyright, license for use
The content of this book is protected by copy-
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to download are strictly prohibited, whether in
part or in entirety, in the original or in a modified
form, for a fee or free of charge. SIGHI members
have a perpetual license for personal use of the
versions, which were downloaded from our web-
site during the duration of their membership:
• For affected persons personal use in-
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cludes sharing with persons living in the
same home and with the medical profes-
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dissemination is prohibited.
• Medical professionals may use this con-
tent for personal and commercial use, for
educational purposes for themselves and
for coworkers in the same institution.
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However, it is not permitted to pass this
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content on to patients, clients, partici-
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make available to download.
Instead one can recommend becoming a member
of SIGHI to those interested, which allows unlim-
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ited access to all our content. Thank you very
much.
Disclosure of possible conflicts of interest
The author is involved in the resale of a medical product. This is however a not-for-profit purchasing
group with the sole aim of passing on the price advantages as far as possible to those affected. Thus, a
conflict of interest in the sense of an incentive to represent a product more positively than it is or to
distort or suppress information in any other way, does not exist in the author's opinion. The author
has no (personal, financial or business) relationship with the manufacturers. The SIGHI does not sus-
tain itself by selling medical products, but through its credibility. The author strove to make the se-
lection and evaluation of the products specified here according to his best knowledge and belief for
the benefit of those concerned.
2 © www.mastzellaktivierung.info 03.01.2019SIGHI Medication Manual: Medical treatment in histaminosis Table of Contents
Table of Contents:
1 Preliminary remarks ................................................................................................. 8
1.1 Disclaimer, disclosure duty ............................................................................................................. 8
1.2 Abbreviations. Definitions ............................................................................................................... 8
1.3 Fundamentals of MCAD medical treatment .............................................................................. 10
1.4 Tolerability of medicines ................................................................................................................ 11
1.4.1 Incompatible active ingredients ....................................................................................... 12
1.4.2 Incompatible excipients ..................................................................................................... 13
2 Overview: Who needs which medication when? ...................................................... 15
2.1 Medical treatment for systemic mast cell activation disorders (MCAD) .............................. 15
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2.1.1 Therapeutic strategy for MCAD ....................................................................................... 15
2.1.2 Basic therapy ........................................................................................................................ 16
2.1.3 Symptomatic supplemental treatment ........................................................................... 17
2.1.3.1
2.1.3.2
2.1.3.3
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Pain .............................................................................................................................. 17
Disorders of the digestive tract............................................................................... 19
Miscellaneous symptoms and disorders .............................................................. 20
2.2 Medication for histamine intolerance (DAO associated histamine degradation disorder)22
2.2.1 Basic therapy ........................................................................................................................ 22
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2.2.2 Symptomatic supplemental treatment ........................................................................... 22
2.2.3 Additional measures in severe cases................................................................................ 23
2.3 Medication for intestinal dysbiosis, small intestinal bacterial overgrowth ......................... 23
3 Medicinal products (Medications) ........................................................................... 24
3.1 Antihistamines (histamine receptor antagonists) ..................................................................... 24
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3.1.1 H1 antihistamines (H1 receptor antagonists) ................................................................ 25
3.1.1.1 Bilastine ...................................................................................................................... 29
3.1.1.2 Cetirizine .................................................................................................................... 29
3.1.1.3 Clemastine (Tavegyl®) .............................................................................................. 29
3.1.1.4 Desloratadine (= descarboethoxyloratadine, DCL)............................................. 29
3.1.1.5 Dimenhydrinate ........................................................................................................ 29
3.1.1.6 Dimetindene (dimethindene) (CH: Feniallerg®, D: Fenistil®) ........................... 30
3.1.1.7 Diphenhydramine .................................................................................................... 30
3.1.1.8 Fexofenadine .............................................................................................................. 30
3.1.1.9 Hydroxizine ............................................................................................................... 30
3.1.1.10 Ketotifen (Zaditen®) .................................................................................................. 30
3.1.1.11 Levocetirizine, levocetirizine dihydrochloride (Xyzal®) ................................... 31
3.1.1.12 Loratadine .................................................................................................................. 31
3.1.1.13 Rupatadine ................................................................................................................. 31
03.01.2019 © www.mastzellaktivierung.info 3Table of Contents SIGHI Medication Manual: Medical treatment in histaminosis
3.1.2 H2-antihistamines (H2-receptor antagonists), ranitidine .......................................... 31
3.1.3 Other antihistaminergic agents ....................................................................................... 32
3.2 Mast cell stabilizers ......................................................................................................................... 33
3.2.1 Cromoglicinic acid, sodium cromoglicate ...................................................................... 33
3.2.1.1 Nalcrom®..................................................................................................................... 34
3.2.2 Ketotifen (Zaditen®) ............................................................................................................ 34
3.3 Prostaglandin synthesis inhibitors, nonsteroidal antiinflammatory drugs (NSAIDs) △ .. 35
3.3.1 Ibuprofen △ .......................................................................................................................... 37
3.3.2 Dexibuprofen △ ................................................................................................................... 38
3.3.3 Acetylsalicylic acid (ASS) △............................................................................................... 41
3.3.4 Etoricoxib (Arcoxia®) .......................................................................................................... 41
3.3.5 Celecoxib (Celebrex®) ......................................................................................................... 41
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3.4 Leukotriene inhibitors .................................................................................................................... 42
3.5 Analgesics ......................................................................................................................................... 42
3.5.1 Paracetamol (Acetaminophen) ......................................................................................... 43
3.6 Proton pump inhibitors.................................................................................................................. 44
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3.7 Cannabinoids, cannabinoid receptor agonists .......................................................................... 45
3.7.1 Hemp, cannabis ................................................................................................................... 46
3.7.2 Tetrahydrocannabinol (THC) ............................................................................................ 47
3.7.3 Cannabidiol (CBD) .............................................................................................................. 47
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3.7.4 Palmitoylethanolamide (PEA) .......................................................................................... 48
3.8 Opiates, opioids △ ........................................................................................................................... 49
3.9 Psychiatric medications ................................................................................................................. 50
3.9.1 Antidepressants................................................................................................................... 50
3.9.2 Neuroleptics, antipsychotics............................................................................................. 50
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3.9.3 Benzodiazepines.................................................................................................................. 50
3.10 Immunosuppressants, immunomodulators .............................................................................. 52
3.10.1 Glucocorticoids .................................................................................................................... 52
3.10.1.1 Natural Glucocorticoids ........................................................................................... 52
3.10.1.2 Synthetic glucocorticoids ........................................................................................ 52
3.10.2 Azathioprine ........................................................................................................................ 53
3.10.3 Methotrexate........................................................................................................................ 54
3.11 Anti-IgE monoclonal antibodies .................................................................................................. 54
3.11.1 Omalizumab ......................................................................................................................... 54
3.12 Tyrosine kinase inhibitors, inhibitors of other kinases ........................................................... 56
3.12.1 Imatinib................................................................................................................................. 57
3.12.2 Masitinib ............................................................................................................................... 57
3.12.3 Midostaurin.......................................................................................................................... 57
3.12.4 Crenolanib ............................................................................................................................ 57
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3.12.5 Sunitinib................................................................................................................................ 57
3.12.6 Nilotinib ................................................................................................................................ 58
3.12.7 Dasatinib ............................................................................................................................... 58
3.13 Cytoreductive therapy, chemotherapy, cytostatics .................................................................. 58
3.13.1 Interferon-α .......................................................................................................................... 58
3.13.2 Cladribine ............................................................................................................................. 59
3.13.3 Hydroxyurea......................................................................................................................... 59
3.13.4 Thalidomide ......................................................................................................................... 59
3.14 Stem cell transplantation ............................................................................................................... 59
4 Medical devices......................................................................................................... 60
4.1 Clinoptilolite, zeolite....................................................................................................................... 60
5 Foods for special medical purposes ......................................................................... 62
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5.1 Diamine oxidase (DAO) .................................................................................................................. 62
5.1.1 DAOSIN® ............................................................................................................................... 63
5.2 Probiotics........................................................................................................................................... 65
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5.2.1 Lactopia Probio Histamed®................................................................................................ 66
6 Nutritional supplements .......................................................................................... 67
6.1 Vitamin C........................................................................................................................................... 67
6.2 Vitamin D3 (cholecalciferol) ........................................................................................................... 69
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6.3 Zinc ..................................................................................................................................................... 72
6.4 Natural mast cell stabilizers .......................................................................................................... 73
6.4.1 Chondroitin sulfate, chondroitin ..................................................................................... 73
6.4.2 Flavonoids △ ........................................................................................................................ 73
6.4.2.1 Quercetin △ ................................................................................................................ 75
6.4.3 Curcumin .............................................................................................................................. 76
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6.4.4 Stilbene derivatives (stilbenoids) ..................................................................................... 77
6.4.5 Ellagic acid ............................................................................................................................ 78
6.5 Selenium ............................................................................................................................................ 78
7 Preparations for an emergency ................................................................................ 79
7.1 Anaphylaxis, anaphylactic shock ................................................................................................. 79
7.1.1 Definitions ............................................................................................................................ 79
7.1.2 Gradation of severity .......................................................................................................... 79
7.2 Interventions in anaphylactic / anaphylactoid shock .............................................................. 80
7.3 Emergency kit ................................................................................................................................... 82
7.3.1 Content of the emergency kit ............................................................................................ 82
7.3.2 Use of the emergency kit .................................................................................................... 82
7.3.2.1 At ONSET of reaction ............................................................................................... 82
7.3.2.2 In case of a SEVERE reaction .................................................................................. 83
03.01.2019 © www.mastzellaktivierung.info 5Table of Contents SIGHI Medication Manual: Medical treatment in histaminosis
7.4 Medical alert card ............................................................................................................................ 84
7.5 Living will ......................................................................................................................................... 84
8 Premedication before medical interventions .......................................................... 85
8.1 Rationale for the need for premedication ................................................................................... 85
8.2 Anesthesia / surgery / invasive examinations ........................................................................... 85
8.2.1 General considerations ...................................................................................................... 85
8.2.2 Prior to an operation (= preoperative) ............................................................................. 87
8.2.3 During an operation (= intraoperative) ........................................................................... 88
8.2.4 After an operation (= postoperative) ............................................................................... 88
8.2.5 Compatibility of frequently used active ingredients in medical interventions ...... 89
8.3 local anaesthesia, regional anaesthesia ....................................................................................... 91
8.4 Examinations containing contrast medium (X-ray, CT, MRI) ................................................ 92
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8.5 Dental medicine and MCAD / Histaminosis .............................................................................. 93
8.5.1 Premedication in dentistry................................................................................................ 93
8.5.2 General information for the dentist ................................................................................ 93
8.5.3.1
8.5.3.2
8.5.3.3
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8.5.3 Tolerable products for local anesthesia in dentistry .................................................... 94
Switzerland ................................................................................................................ 94
Germany ..................................................................................................................... 94
Austria ......................................................................................................................... 95
8.6 Vaccinations ..................................................................................................................................... 96
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8.6.1 Compatibility of vaccinations in MCAD......................................................................... 96
8.6.2 To vaccinate: yes or no? ..................................................................................................... 97
8.6.3 Self-centered versus societal considerations ................................................................. 98
8.6.4 Compulsory vaccination .................................................................................................... 98
8.6.5 Precautions for vaccinations ............................................................................................. 99
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9 Medicinal treatment in the event of disease........................................................... 100
9.1 Flu-like infection, common cold, sore throat, bacterial infection........................................ 100
9.1.1 Antipyretics, cold medication......................................................................................... 100
9.1.2 Sore throat .......................................................................................................................... 100
9.1.3 Nutritional supplementation .......................................................................................... 100
9.1.4 Bacterial secondary infections (frontal and maxillary sinusitis) ............................. 100
9.1.5 Inappropriate for infections............................................................................................ 101
9.2 Antibiotics....................................................................................................................................... 101
9.3 Allergies........................................................................................................................................... 102
9.3.1 Respiratory allergies......................................................................................................... 102
9.4 Swallowing disorders, dysphagia ............................................................................................... 105
10 Medicinal treatment in special situations.............................................................. 108
10.1 Pregnancy and lactation ............................................................................................................... 108
10.1.1 Medicinal treatment for pregnant and lactating women .......................................... 108
6 © www.mastzellaktivierung.info 03.01.2019SIGHI Medication Manual: Medical treatment in histaminosis Table of Contents
10.1.1.1 Recommended substances .................................................................................... 108
10.1.1.2 Less well suited ........................................................................................................ 109
10.1.1.3 Imperatively to be avoided .................................................................................... 109
10.1.2 Psychiatric medications during pregnancy .................................................................. 110
11 References .............................................................................................................. 111
12 Annex...................................................................................................................... 120
Annex: incompatible active substances .............................................................................................. 121
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03.01.2019 © www.mastzellaktivierung.info 7Preliminary remarks SIGHI Medication Manual: Medical treatment in histaminosis
1 Preliminary remarks
medical professional. Only your doctor has
1.1 Disclaimer, disclosure knowledge of your particular medical condi-
duty tions and can draw attention to any contrain-
dications or recognize other, potentially
This medication manual was created by a uni- more dangerous diseases.
versity educated professional in the natural
Disclaimer: The use of the information in this
sciences (MS in Environmental Sciences, ETH
medication manual is done at your own risk.
Zürich) without a formal medical education.
The author/editor disclaims all liability for
The information contained herein can be in-
the accuracy and completeness of the infor-
complete, incorrect, or outdated. Also, certain
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mation contained herein, for any damage,
active ingredients or products listed here may
consequential damage, or other disad-
be unsuitable in your individual case for par-
vantages of any kind incurred.
ticular medical reasons.
This document is updated continually. When-
ever possible you should access the current
version at www.mastzellaktivierung.info, ra-
ther than using a printed or locally stored
IE 1.2 Abbreviations. Definitions
→: a leading arrow (→) means “see”, for example
regarding references to page numbers or sec-
version. Never use the information provided tion numbers. Words or abbreviations with a
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here as the sole source, but instead seek ad- preceding arrow are explained in the current
vice from your doctor or pharmacist. section (1.2).
If a medical professional prescribes or di- A: Austria
rectly hands out medications to you, inform CH: Switzerland
him about diseases that you have and about D: Germany
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all the medications and medical products in- DAO: Diamine oxidase, ABP1. An enzyme, pro-
cluding supplements and over the counter duced mainly in the intestinal mucosa and in
remedies that you take occasionally or on a the kidneys, which can break down histamine,
regular basis. putrescine and other biogenic amines.
To be aware of potential risks and side effects Drag: Dragee. A →tablet with a sugar coating.
always carefully read the enclosed infor- Fct: film-coated tablet. A →tablet that is coated
mation leaflet: with a thin polymer layer.
Histamine: A biogenic amine, that due to its
Switzerland: www.swissmedicinfo.ch (official),
numerous features as an endogenous messen-
https://compendium.ch, https://ch.oddb.org.
ger, a neurotransmitter and inflammatory me-
Germany: http://oddb.org. diator can be described as the most important
symptom inducing mast cell mediator. Hista-
Austria: https://aspregister.basg.gv.at.
mine is not only produced by the body, but is
This medication manual should only serve as also a degradation product of proteins in rotting
a complement to the physician-patient rela- or fermented foods.
tionship and does not replace consulting a
8 © www.mastzellaktivierung.info 03.01.2019SIGHI Medication Manual: Medical treatment in histaminosis Preliminary remarks
Histaminosis: We define histaminosis as the histamine mediated intolerance reactions of
condition in which the histamine status in the unknown or not enzyme related cause it
body deviates so far from the ideal range (either would be better to use the concept of histamine
locally or systemically), that well-being or phy- incompatibility.
sical / mental performance are impaired to a Intravenous, i.v.: Using a vein, i.e. a venous
significant degree. Usually the deviation is such blood vessel (leading to the heart), as the route
that the levels are above the normal range, i.e. of administration administration for a sub-
there is a histamine surplus. This term does not stance. For example, by injection or infusion.
refer to the cause of this condition, which may
Cap: Capsules, a medication form consisting of
have physical causes (originating in the body)
a solid shell and a filling.
or be due to environmental factors. Possible
MCAD: Abbreviation of “mast cell activation
physical causes are for example the excessive
disease”. Otherwise referred to as “systemic
release from mast cells, basophilic granulocytes
mast cell activation disease”. An umbrella term
or other histamine storing cells (e.g. due to
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for diseases in which one or more acquired or
MCAD, allergies, autoimmune diseases, certain
inherited genetic mutations or epigenetic alter-
tumors) or disorders in degradation (i.e. insuffi-
ations lead to an incorrect permanent activa-
cient enzymatic activity of DAO).
tion, an increased sensitivity, or excessive pro-
Histamine intolerance (abbreviation:
HIT):
The term “intolerance” comes from the Latin:
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intolerantia, derived from tolerare = “to bear”, “to
liferation of mast cells and thereby lead to an
excessive non-specific release of mast cell me-
diators. MCAD include the very common
→MCAS, the rare →SM, and the extremely rare
endure”, with the negating prefix “in-“. →MCL.
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Different conceptions are encountered about MCAS: Abbreviation of “mast cell activation
how histamine intolerance should be defined: syndrome”. Otherwise referred to as →systemic
In the strictest sense histamine intolerance is mast cell activation syndrome.
an acquired or congenital reduction of the func- MCL: Abbreviation for “mast cell leukemia”.
tion of the histamine degrading enzyme dia-
Oral (per os, peroral): Route of administra-
mine oxidase (DAO).
tion of a substance via the mouth, i.e. to swal-
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In a broader sense HIT can be defined as a dis- low.
turbance at any point in the various enzymatic
SM: Abbreviation for “systemic mastocytosis”.
degradation pathways of histamine and other
Systemic mastocytosis (SM):
biogenic amines (enzymopathy, quantitative or
qualitative enzyme deficiencies). A subtype of →MCAD.
We recommend only referring to HIT when his- Systemic mast cell activation syndrome
tamine degredation disorders with a proven en- (MCAS): A subtype of →MCAD.
zymatic cause are present and to otherwise use Tab: Tablets, a solid form of medications,
the term →histamine incompatibility. formed by compression of powders or granu-
Histamine incompatibility: Only hista- lates under pressure.
mine degradation disorders with a demonstra-
ble enzymatic cause should be referred to as a
histamine intolerance (in analogy to lactose
and fructose intolerances, which are also
caused by lacking enzymes or reduced enzyme
activity). For all other “histamine disorders” or
03.01.2019 © www.mastzellaktivierung.info 9Preliminary remarks SIGHI Medication Manual: Medical treatment in histaminosis
apropiate by reducing their amount). A second
1.3 Fundamentals of MCAD
important principle is blocking the effect of re-
medical treatment leased mast cell mediators.
According to the current state of knowledge, Mast cell activation diseases (MCAD) do
mast cell activation diseases (MCAD) have their not have a homogeneous presentation,
origin in particular, complex patterns of multi- but instead every affected person has
ple genetic and epigenetic mast cell activating their individual constellation of symp-
factors, for which to date there is no curative
toms with an individual degree of sever-
(healing the root causes) therapy. Treatment is
ity that is subject to temporal fluctua-
therefore mainly limited to keeping the inten-
tions. Therefore, an individually adapted
sity of the symptoms under control for life and
to reducing the frequency of acute reactions. therapy needs to be found for each pa-
tient.
The mainstay of treatment is identifying
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and avoiding the mast cell activating
triggering stimuli. To a certain degree
the strength of a reaction to particular
stimuli is different among different indi- IE
viduals. Due to the wide variety of stim-
uli with which one is confronted daily,
identifying the triggering stimulus
proves to be a difficult and lengthy task.
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See www.mastzellaktivierung.info.
Medications are in most cases useful or With MCAD, there is no uniform clinical
even indispensable to support the treat- presentation and the degree of severity is very
ment, but in the medium term and long individual. Therefore, no universally valid rec-
term can not replace strict avoidance of ommendations regarding treatment and dosage
of medications can be given, but instead the
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triggers!
medical therapy should be guided by the unique
The symptoms have to be alleviated as much as type and severity of symptoms [MOLDERINGS ET
possible by avoiding the triggers (see AL. 2011; SIGHI].
www.mastzellaktivierung.info) [MOLDERINGS ET The basic medication at standard doses usually
AL. 2011; SIGHI]. In particular, all histamine lib- already has a quite beneficial effect, but the
erators contained in food, sweets, beverages, quality of life can be further improved by dos-
and tobacco products should be strictly age adjustments and additional active ingredi-
avoided. To the degree that one reacts to hista- ents. Over time, the affected person will find out
mine rich foods, these should be limited to a tol- through patient experimentation, the specific
erable amount. combinations and dosages out of the numerous
In most cases symptoms will still emerge de- possible treatment options that will help him
spite avoiding the triggers as well as possible. best in particular situations [AFRIN ET AL. 2016;
Under these conditions additional pharmaco- SIGHI]. In the course of goal-directed experi-
logical therapy is necessary. The main objec- menting, the patient will depend on the assis-
tive is to reduce the release and synthesis of me- tance of a physician at least regarding the pre-
diators (by stabilizing the mast cells and where scription medications.
10 © www.mastzellaktivierung.info 03.01.2019SIGHI Medication Manual: Medical treatment in histaminosis Overview: Who needs which medication when?
2 Overview: Who needs which medication when?
(within minutes). If signs of anaphylactic or an-
2.1 Medical treatment for aphylactoid reactions arise, proceed as de-
systemic mast cell activa- scribed in chapter 7.1 “Anaphylaxis, anaphy-
lactic shock” on page 79. In cases without ana-
tion disorders (MCAD) phylaxis in the prior medical history, in the
event of non-alarming newly emerging or in-
2.1.1 Therapeutic strategy for tensifying preexisting symptoms, the dosage
MCAD of the basic medication and/or sympto-
matic supplemental therapy can simply
▶ Treatment in the chronic phase: be increased up to at most the maximum per-
• Basic medication: Even without be- missible daily amount. With antihistamines
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ing in contact with mast cell-activating many affected people even need up to four to six
substances the level of release of mast times the usual daily dose on a long-term basis.
cell mediators is often so high that it Naturally pharmacological agents with a rapid
should be treated with medication on a onset of action are to be preferred, while the
permanent basis. In section 2.1.2 (page
16) we describe the basic medication to
stabilize the mast cells and to control
the symptoms while the condition is at
IE dosage of very slow-acting long term medica-
tions (e.g. ketotifen) does not have to be adapted
to one-off acute events.
Also suitable for acute short-term treatment:
the long-term baseline level of severity. Benzodiazepines: Flunitrazepam per os for a
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• Symptomatic supplemental treat- maximum of 3 to 4 days; inhibits mediator re-
ment: Each affected person has an in- lease from mast cells. [HOMANN ET AL. 2010]
dividual symptomatology. Which par-
In severe cases: Vitamin C 750 mg as an intra-
ticular symptoms arise at which body
venous infusion dissolved in a glucose solution
site and with what intensity depends,
5% (0.5 l / day for 3 to 4 days). Page 67. [HOMANN
among other things, on the particular
ET AL. 2010]
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set of causally involved mast cell muta-
tions, which organs or tissues are af-
fected by mutated mast cells and to
which mast cell-activating substances Treatment of
one has been exposed. In section 2.1.3 MCAS/mastocytosis
(page 17) we present possibilities to spe-
cifically supplement the basic medica-
tion if necessary and to adapt it for the Avoid
symptoms occurring in the particular Medication
triggers
case.
▶ Treatment in the acute phase: Not all
triggering substances are reliably avoidable. Mast cell Mediator Degradation
This can lead to temporal fluctuations in symp- stabilizer inhibitor promoters
tom severity. Disease relapses can flare up both
slowly (within hours to days) and very quickly
03.01.2019 © www.mastzellaktivierung.info 15Overview: Who needs which medication when? SIGHI Medication Manual: Medical treatment in histaminosis
Second-line therapy Stop estrogen (hormonal contraception) and
Peroral potassium supplementation, on a pro- take leuprorelin [THEOHARIDES ET AL. 2008].
batory basis for 2-3 days [WIRZ AND MOLDERINGS NK1R antagonists: gabapentin and L-703606
2017]. [AICH, AFRIN AND GUPTA 2015].
Antihypertensive treatment, if (undetected) CaMKII-inhibitor: KN-93 [AICH, AFRIN AND
nocturnal hypertension could be the cause GUPTA 2015].
[WIRZ AND MOLDERINGS 2017]. Amphetamines [MOLDERINGS ET AL. 2011].
Dihydroergotamine (serotonine receptor ago-
nist with a potentially unfavorable risk and Prostatitis, chronic pelvic pain syn-
side-effect profile) [AICH, AFRIN AND GUPTA 2015]. drome
Must absolutely not be taken together with Quercetin (page 74) [SHOSKES ET AL. 1999].
Triptans.
Disodium cromoglycate (DNCG, page 33) [AICH,
Triptans (e.g. sumatriptan) are proven in ani- AFRIN AND GUPTA 2015]
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mal studies to stimulate mast cell proliferation
H1-antihistamines: cetirizine [AICH, AFRIN AND
and should therefore only be used with great
GUPTA 2015].
caution. [DUBAYLE ET AL. 2005; WIRZ AND
MOLDERINGS 2017; AICH, AFRIN AND GUPTA 2015] H2-antihistamines: ranitidine [AICH, AFRIN AND
IE GUPTA 2015].
APETx2 (selective ASIC3-inhibitor) [AICH, AFRIN
AND GUPTA 2015]. See also: [DIOCHOT ET AL. 2004].
NGF neutralizing antibody AB-256-NA [AICH,
AFRIN AND GUPTA 2015].
Endometriosis pain
Chronic pelvic pain syndrome in women
Palmitoylethanolamide (PEA): see page 48
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[INDRACCOLO AND BARBIERI 2010; IUVONE ET AL. 2016] Zafirlukast (leukotriene antagonist, page 42)
[AICH, AFRIN AND GUPTA 2015].
Cromoglicic acid or di-sodium cromoglycate:
page 33 [ZHU ET AL. 2015]. Anti-CCL2 / JE (AB479NA) and anti-CCL3
(AB450NA) [AICH, AFRIN AND GUPTA 2015].
Throat pain
Complex regional pain syndrome
Increase the dose of H1-antihistamines,
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(CRPS)
etoricoxib (page 41) [WIRZ AND MOLDERINGS 2017]
LY303870 (NK1R antagonist) [AICH, AFRIN AND
GUPTA 2015].
Bladder pain syndrome, chronic non-
bacterial cystitis, mast cell-mediated in-
Venom-induced hyperalgesia, excessive
terstitial cystitis
sensitivity to pain
H1-antihistamines, e. g. cetirizine [AICH, AFRIN
Disodium cromoglycate (DNCG, page 33) [AICH,
AND GUPTA 2015], hydroxyzine [MINOGIANNIS ET
AFRIN AND GUPTA 2015]
AL. 1998].
H1-antihistamines: chlorphenamine, mepyra-
H2-antihistamines, e. g. ranitidine, cimetidine,
mine (= pyrilamine) [AICH, AFRIN AND GUPTA
famotidine [AICH, AFRIN AND GUPTA 2015].
2015].
Pentosan polysulphate (a noticeable improve-
H2-antihistamines: cimetidine (not available in
ment usually only occurs after more than six
Switzerland) [AICH, AFRIN AND GUPTA 2015].
months of therapy.) [TEICHMAN 2002; CHIANG ET
AL. 2000; CHIANG ET AL. DAVIS ET AL. 2008; ANDERSON
AND PERRY 2006].
18 © www.mastzellaktivierung.info 03.01.2019Overview: Who needs which medication when? SIGHI Medication Manual: Medical treatment in histaminosis
Diarrhea Sensitivity to histamine-rich foods
Colestyramine [MOLDERINGS ET AL. 2011; HOMANN Diamine oxidase (DAO): to be taken as needed
ET AL. 2010]. (depending on the amount of histamine ex-
Leukotriene receptor antagonists (page 42): e.g. pected in a meal) or as long-term medication.
montelukast. [MOLDERINGS ET AL. 2011; HOMANN ET Only to be taken as a prophylactic measure, and
AL. 2010] only for problems elicited by foodstuffs. Page
62. [SIGHI]
Psyllium husks regularize bowel movements,
are of use with diarrhea as well as with consti-
pation (e. g. ground psyllium husks as available 2.1.3.3 Miscellaneous symptoms and
at www.dm.de) [SIGHI]. disorders
5-HT3 receptor antagonists: e.g. ondansetron
Inability to fall asleep or stay asleep
[MOLDERINGS ET AL. 2011]
Benzodiazepines (3.9.3 on page 50):
W
Nystatin [MOLDERINGS ET AL. 2011].
Triazolam [MOLDERINGS ET AL. 2011]
Anal eczema, inflamed rear end Oxazepam [MOLDERINGS ET AL. 2011]
After every bowel movement immediately
wash the affected area thoroughly with water IE Depression
without using soap. For example, with a wet Doxepin (page 50) [GONZÁLEZ-DE-OLANO ET AL.
washcloth, using a bidet, a toilet shower, or a 2016].
shower toilet (Closomat) or by sitting on the
edge of the bathtub and using the shower head. Anxiety, panic attacks
Then gently pat dry with a cloth, do not rub. Do
EV
Benzodiazepines (3.9.3 on page 50):
not use oily creams or ointments. If fatty sub-
e.g. lorazepam, alprazolam, clonazepam.
stances are to be used at all, at the utmost some
coconut oil or olive oil can be applied after
Mast cell activation by neuronal excita-
cleaning with water.
tion or irritation
During strenuous activities (e.g. multi-day bi-
In some people mast cells, eosinophil granulo-
cycle tours or horse trekking) unscented baby
PR
cytes and lymphocytes are overly sensitive to
powder might also be helpful.
the excitation of nerve cells in the vicinity (me-
Only use local cortisone for a short time period diator release by neuronal effector cell trigger-
because it causes the skin to become thin.
ing).
[SIGHI]
Treatment options:
Nausea, vomiting Stress reduction, relaxation techniques, seda-
tive antihistamines of the first generation (page
Clonazepam, diazepam [AFRIN ET AL. 2015]
25), low dose benzodiazepines 1 to 2 times a
Lorazepam [HOMANN ET AL. 2010] week (see page 50, e.g. oxazepam, diazepam).
Metoclopramide (Caution: DAO inhibitor!) [VAEM.EU]
[HOMANN ET AL. 2010]
Domperidon [HOMANN ET AL. 2010] Asthma
5-HT3 receptor antagonists: e.g. ondansetron Leukotriene antagonists [HOMANN ET AL. 2010].
[MOLDERINGS ET AL. 2011; HOMANN ET AL. 2010]. (Caution with paracetamol (acetaminophen)! It
can increase the bronchial constriction.) [SIGHI]
20 © www.mastzellaktivierung.info 03.01.2019Medicinal products (Medications) SIGHI Medication Manual: Medical treatment in histaminosis
3 Medicinal products (Medications)
Definition: Medicinal products (medica- 3.1 Antihistamines (histamine
tions) are products (substances or mixtures of
substances) with the intended purpose to treat
receptor antagonists)
or prevent human or animal diseases, injuries
Other designations:
or disabilities or with the capacity to influence
W
physiological functions or permit and facilitate Histamine receptor blockers, histamine block-
making a medical diagnosis. This definition co- ers, histamine receptor inhibitors.
vers products, which are manufactured for this Einzahl: das Antihistaminikum, der Histamin-
purpose and proclaimed as such (regardless of rezeptorantagonist.
whether they are suitable for the purpose), as
well as substances which are suitable (regard-
less of whether they are manufactured to this
end or promoted as such).
IE Mode of action
Histamine is one of the most important symp-
tom-causing mast cell mediators. Histamine, a
For medicinal products specific and stringent chemical messenger, affects the targeted cells
EV
legal requirements have to be met regarding by binding to histamine receptors on their sur-
proof of efficacy, the procedure of approval, face, triggering a specific biochemical process.
their production, advertising, putting on the Antihistamines (histamine receptor antago-
market and their dispensation. nists, histamine receptor blockers) have their
Other legally defined and recognized product effect countering histamine-induced symp-
categories with a relation to health, such as toms by specifically blocking a particular type
PR
medical products and devices (page 60), food- of histamine receptor. Figuratively speaking,
stuffs for particular medical purposes (page 62), they clog certain keyholes (receptors) so that
or dietary supplements (page 67) do not belong the key (histamine) no longer can fit there. An-
to the category of medicinal products. tihistamines therefore do not directly counter-
act the histamine and do not reduce the level of
histamine in the body. Instead they temporarily
suppress certain effects that histamine would
have on the targeted cells mediated by one spe-
cific type of receptor.
Four distinct histamine receptor types have
at present been discovered and are designated
as H1, H2, H3, H4. Antihistaminergic sub-
stances usually bind very specifically to only
one of the four different types of histamine re-
ceptors, without having effects on the other
24 © www.mastzellaktivierung.info 03.01.2019SIGHI Medication Manual: Medical treatment in histaminosis Medicinal products (Medications)
ones. Therefore, an H1-AH (H1-receptor spe- 3.1.1 H1 antihistamines (H1 re-
cific antihistamine) cannot the have the effects
ceptor antagonists)
of an H2-AH and the same applies vice versa.
The H1-antihistamines can be used to suppress H1-antihistamines (abbr.: H1-AH) are
the most symptoms and therefore have the among the most important active sub-
greatest therapeutic significance. Additionally,
stances in the treatment of MCAD and
in the eventuality of excessive stomach acid
other histamine-mediated disorders and
production (heartburn, acid reflux) or other dis-
symptoms. They have a favorable risk-
orders of the digestive tract (especially diar-
rhea) taking an H2-antihistamine might be of benefit profile.
benefit. H3- and H4-blockers are currently of Their mechanism of action is to prevent
little therapeutic importance. histamine from having an effect by
The various substances with H1-receptor an- blocking the histamine-H1-receptor
W
tagonistic activity all have the same mode of ac- through which the majority of the symp-
tion, but they may differ in terms of their over- toms caused by histamine is mediated.
all effect, potency, duration of action, tolerabil-
With only one active substance a very
ity etc. The individual substances differ in the
wide range of symptoms can be treated.
characteristics regarding absorption into and IE
distribution in the body as well as degradation Older substances also affect the central
and elimination from the body, and also in nervous system and cause drowsiness
other properties (toxicity, side effects, taste, (and therefore can be used to treat in-
etc.). It is therefore not irrelevant which H1-an- somnia). This is not the case for the
tihistamine one takes and the particular sub-
EV
newer substances.
stance should be specifically selected for the de-
sired attributes. If the results are not satisfac- They are taken either continuously on a
tory after a few weeks or months another sub- long-term basis or as required. H1-AH
stance can be used on a trial basis. can be taken both with the intent to pre-
Sometimes certain H1-antihistamines are even vent as well as the intent to cure.
claimed to have a certain mast cell stabilizing
PR
effect. This is probably explainable by antihis- Application and dosage:
tamines causing the H1-receptor density to be H1-antihistamines can be used for all types of
reduced (i.e. a reduced receptor production by histaminosis. The administration is usually
the cells) as a consequence of a lack of their →peroral, in severe cases additionally →intra-
stimulation due to being blocked. For this rea- venous. Topical external application in an oint-
son, it is recommended for people with pollen ment also exists (for example in soothing insect
allergies that they prophylactically begin with bites and itching).
H1-antihistamines a few days or weeks before
Unless otherwise stated, they may either be
the beginning of the pollen season in order to
taken on a regular basis or as required depend-
minimize the stimulation of H1-receptors from
ing on the situation, preferably prophylacti-
the beginning. [MIZUGUCHI ET AL. 2011, MIZUGUCHI
cally (before expected symptoms arise), or al-
ET AL. 2010]
ternatively curatively (to relieve existing symp-
toms).
03.01.2019 © www.mastzellaktivierung.info 25Medical devices SIGHI Medication Manual: Medical treatment in histaminosis
4 Medical devices
Definition: Medical devices are objects or The physical properties, not the chemical ones
(pharmacologically inert) substances used for of this silicate structure are important:
therapeutic or diagnostic purposes in humans. As other zeolites cli-
In contrast to medications the principal in- noptilolite consists
tended effect of medical devices is mainly of a of a microporous
physical or physicochemical nature, i.e. with- scaffold structure of
out uptake of a pharmacologically / metaboli- [AlO4]-- and [SiO4]--
cally / immunologically active substance in the tetrahedra. Water
body or without direct Intervening in the me- and other small
tabolism. molecules with spe-
Market access and marketability are differently cific properties can fit in the interstices of this
W
regulated for medical devices than for medica- crystal lattice. Due to this the material can be
tions. In this matter the Medical Devices Di- used as a molecular sieve or ion exchanger, in
rective of the European Council 93/42/EEC short: as a kind of “filter”. For this purpose, the
(with applicability in the EU and also in Swit- rock is ground finely. The finer the particle size,
zerland) and the Medical Devices Ordinance of
the Swiss Federal Council (CH) are authorative.
Medical devices are not officially approved, but
IE the greater the surface area and consequently
the more pronounced the physical filter effect
of this material. When buying, do not only com-
instead, depending on their risk classification, pare the price per kg, but also the declared par-
are monitored by an external body (conformity ticle size.
EV
assessment body) for compliance with legal re- In brief it is “flour” made of rocks, in which cer-
quirements before and during the placing of tain substances are captured and others are not.
these on the market.
Clinoptilolite is one of the most abundant zeo-
lites and has many important industrial appli-
4.1 Clinoptilolite, zeolite cations, where it is used in huge quantities in
building materials, in horticulture, in animal
PR
Other names / brands: feed, as a fertilizer carrier material, as stable
Zeolites, Megamin®, MANC® (Modified, Acti- bedding, cat litter, in household products, as a
vated Natural Clinoptilolite), Froximun® Tox- desiccant, and in environmental technology.
aprevent®. Amongst other things, zeolites are used for the
Mode of action: purification of substances, in wastewater treat-
ment, and as an additive in laundry detergents
The crystalline mineral clinoptilolite belongs to
to decalcify hard water.
the category of sedimentary rocks, but was
originally formed in volcanic deposits. In Clinoptilolite is marketed as a medical device
chemical terms clinoptilolite is a group of hy- and certain claims of therapeutic abilities are
drous aluminosilicates with calcium, potassium associated with the products, for which we have
or sodium as connecting cations: so far found no convincing evidence, neither in
literature nor in self-experiments (see also:
Clinoptilolite-Ca: Ca3(Si30Al6)O72·20H2O
[KERSCHNER 2015]).
Clinoptilolite-K: K6(Si30Al6)O72·20H2O
The insoluble material is ingested in powder
Clinoptilolite-Na: Na6(Si30Al6)O72·20H2O form and passes through the digestive tract un-
changed, without being taken up by the body.
60 © www.mastzellaktivierung.info 03.01.2019SIGHI Medication Manual: Medical treatment in histaminosis Medical devices
According to the manufacturers it should “de- Use:
toxify” by absorbing harmful substances Depending on the particular manufacturer the
(binding them to itself) and thereby decreasing specifications are for example from 3 to 8 grams
their uptake from food by the body. According of powder (one teaspoon) in the morning stirred
to the manufacturers' claims ammonium, lead, in water or in food and ingested.
mercury, histamine and other amines are
Adverse effects
bound. “Essential substances, such as zinc, and iron
Clinoptilolite is regarded as a comparatively in-
are demonstrably not bound and left at the disposal of
ocuous substance with few side effects. It is still
the body.”, is written in a leaflet.
not entirely without risks:
Should this actually work, at best it would be
It is conceivable that with regular use the crys-
the meal consumed at the same time and not the
tal particles could abrasively damage the intes-
body that would be “detoxified”. It seems to be
tinal mucosal cells or at least irritate and injure
proven that ammonium, cesium, strontium,
them.
and heavy metals are partially absorbed. Natu-
W
rally this material does not have any innate “in- A report by the EFSA (European Food Safety
telligence” which could distinguish which sub- Authority) indicates that zeolites significantly
stances would be “harmful” or “useful” for hu- increase the aluminum blood levels in animal
mans. Anything is simply indiscriminately ab- studies performed on dairy cows [EFSA 2007].
lattice due to its molecular size, shape and
charge. In our opinion it does not seem to be
IE
sorbed that fits into the interstices of the crystal Aluminium is suspected to be able to trigger
Alzheimer's and other diseases.
In addition to pollutants, beneficial nutrients
could possibly also be absorbed, which in the
sufficiently researched whether this would also
include useful or essential nutrients. long term could lead to deficiencies. EFSA re-
EV
Six SIGHI members have volunteered and ports a “dramatic depression of feed intake” with a -
tested the preparation “Froximun Toxaprevent” albeit not severe - phosphate deficiency (“hypo-
in a self-experiment. None of the subjects could phosphataemia”) as an observed result in a trial
determine an effect after 1-2 months. This non- with dairy cows [EFSA 2007].
representative small trial of course does not In an enclosed information leaflet one manu-
prove the ineffectiveness of the preparation, facturer warns that their product should not be
PR
but did not manage to convince us, that the ef- taken with medications, but only with an inter-
fect is worth the price. val of at least one hour. This shows that even
For this dirt-cheap substance of which tons are manufacturers expect that desired substances
used in industry all of a sudden comparatively could also be absorbed. Aspirin, theophylline,
very high prices are charged for a few grams as propanolol, and phenobarbital are absorbed to
soon as the stone flour is filled into capsules and a slight degree in vitro. Regarding some medi-
packaged like a medication. Of course, there cally used metal ions such as lithium or cispla-
might be some differences in purity require- tin, interactions with this substance can be ex-
ments and particle sizes, but whether they jus- pected. However, for most medications, inter-
tify the high price is an open question. actions with clinoptilolite are unlikely due to
their molecular size.
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