Anti-allergic Agent
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Anti-allergic agents are
medication Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to medical diagnosis, diagnose, cure, treat, or preventive medicine, prevent disease. Drug therapy (pharmaco ...
s used to treat allergic reactions. Anti-allergic agents have existed since 3000 B.C in countries such as
China China, officially the People's Republic of China (PRC), is a country in East Asia. With population of China, a population exceeding 1.4 billion, it is the list of countries by population (United Nations), second-most populous country after ...
and
Egypt Egypt ( , ), officially the Arab Republic of Egypt, is a country spanning the Northeast Africa, northeast corner of Africa and Western Asia, southwest corner of Asia via the Sinai Peninsula. It is bordered by the Mediterranean Sea to northe ...
. It was not until 1933 when antihistamines, the first type of anti-allergic agents, were developed. Common allergic diseases include
allergic rhinitis Allergic rhinitis, of which the seasonal type is called hay fever, is a type of inflammation in the nose that occurs when the immune system overreacts to allergens in the air. It is classified as a type I hypersensitivity reaction. Signs a ...
,
allergic asthma Asthma is a common chronic (medicine), long-term inflammation, inflammatory disease of the bronchiole, airways of the lungs. It is characterized by variable and recurring symptoms, reversible Airway obstruction, airflow obstruction, and easi ...
and
atopic dermatitis Atopic dermatitis (AD), also known as atopic eczema, is a long-term type of inflammation of the skin. Atopic dermatitis is also often called simply eczema but the same term is also used to refer to dermatitis, the larger group of skin conditi ...
with varying symptoms, including
runny nose Rhinorrhea (American English), also spelled rhinorrhoea or rhinorrhœa (British English), or informally runny nose is the free discharge of a thin mucus fluid from the nose; it is an extremely common condition. It is a common symptom of allergie ...
, watery eyes,
itch An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...
iness,
cough A cough is a sudden expulsion of air through the large breathing passages which can help clear them of fluids, irritants, foreign particles and Microorganism, microbes. As a protective reflex, coughing can be repetitive with the cough reflex fol ...
ing, and
shortness of breath Shortness of breath (SOB), known as dyspnea (in AmE) or dyspnoea (in BrE), is an uncomfortable feeling of not being able to breathe well enough. The American Thoracic Society defines it as "a subjective experience of breathing discomfort that con ...
. More than one-third of the world's population is currently being affected by one or more allergic conditions. Commonly used anti-allergic agents include
antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...
s,
decongestant A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal congestion in the upper respiratory tract. The active ingredient in most decongestants is either pseudoephedrine or phenylephrine (the latter o ...
s,
corticosteroid Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones. Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are invo ...
s, leukotriene pathway modifiers and
mast cell stabilizer Mast cell stabilizers are medications used to prevent or treat certain allergic disorders. They block mast cell degranulation, stabilizing the cell and thereby preventing the release of histamine and related mediators. One suspected pharmacody ...
s. Antihistamines and decongestants are generally the first-line treatment in mild to moderate allergic reactions. Corticosteroids are generally indicated for moderate cases. In severe cases,
adrenaline Adrenaline, also known as epinephrine, is a hormone and medication which is involved in regulating visceral functions (e.g., respiration). It appears as a white microcrystalline granule. Adrenaline is normally produced by the adrenal glands a ...
is used to reduce swelling and aid breathing.
Allergen immunotherapy Allergen immunotherapy, also known as desensitization or hypo-sensitization, is a medical treatment for environmental allergies (such as insect bites) and asthma. Immunotherapy involves exposing people to larger and larger amounts of allergens ...
is an alternative treatment considered in some patients, with a success rate of 80%-90% in reducing
symptoms Signs and symptoms are diagnostic indications of an illness, injury, or condition. Signs are objective and externally observable; symptoms are a person's reported subjective experiences. A sign for example may be a higher or lower temperature ...
, but requiring a much longer duration of therapy. The choice of medications depends on the disease to be treated, its severity and patient factors.


Allergy

Allergies Allergies, also known as allergic diseases, are various conditions caused by hypersensitivity of the immune system to typically harmless substances in the environment. These diseases include Allergic rhinitis, hay fever, Food allergy, food al ...
, also known as type 1 hypersensitivity, are a type of immune response which takes place when our body's protective mechanism defends us against triggers called
allergen An allergen is an otherwise harmless substance that triggers an allergic reaction in sensitive individuals by stimulating an immune response. In technical terms, an allergen is an antigen that is capable of stimulating a type-I hypersensitivi ...
s.


Common causes

An allergic reaction can be caused by direct contact with an allergen. For example, through consuming a certain food, inhalation of
pollen Pollen is a powdery substance produced by most types of flowers of seed plants for the purpose of sexual reproduction. It consists of pollen grains (highly reduced Gametophyte#Heterospory, microgametophytes), which produce male gametes (sperm ...
s or
dust mites House dust mites (HDM, or simply dust mites) are various species of acariform mites belonging to the family Pyroglyphidae that are found in association with dust in dwellings. They are known for causing allergies. Biology Species The curren ...
, or direct contact with a certain material. A family history of allergies also leads to a higher risk of developing allergic diseases.


Mechanism

When a person comes in contact with a specific trigger, their immune system produces antibodies called
immunoglobulin E Immunoglobulin E (IgE) is a type of antibody (or immunoglobulin (Ig) " isoform") that has been found only in mammals. IgE is synthesised by plasma cells. Monomers of IgE consist of two heavy chains (ε chain) and two light chains, with the ε ...
(IgE) molecules that bind to
mast cell A mast cell (also known as a mastocyte or a labrocyte) is a resident cell of connective tissue that contains many granules rich in histamine and heparin. Specifically, it is a type of granulocyte derived from the myeloid stem cell that is a p ...
s (immune cells found mainly in the
skin Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation. Other animal coverings, such as the arthropod exoskeleton, have different ...
,
respiratory tract The respiratory tract is the subdivision of the respiratory system involved with the process of conducting air to the alveoli for the purposes of gas exchange in mammals. The respiratory tract is lined with respiratory epithelium as respirato ...
and
digestive tract The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the Digestion, digestive system that leads from the mouth to the anus. The tract is the largest of the body's systems, after the cardiovascula ...
) and triggers the release of
histamine Histamine is an organic nitrogenous compound involved in local immune responses communication, as well as regulating physiological functions in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. Discovered in 19 ...
and other chemicals that guards our immune system. Histamine increases the level of vascular permeability and increases the swelling and dilation of vessels. This induces allergic symptoms, such as runny nose,
sneezing A sneeze (also known as sternutation) is a semi-autonomous, convulsive expulsion of air from the lungs through the nose and mouth, usually caused by foreign particles irritating the nasal mucosa. A sneeze expels air forcibly from the mouth a ...
, watery eyes and itching.


Types

Allergic reactions can range from mild to severe. Common allergic diseases include allergic rhinitis, allergic asthma, allergic conjunctivitis and atopic dermatitis. Each condition presents its own set of symptoms. In severe cases, certain allergies can lead to a life-threatening reaction called anaphylaxis. This is a medical emergency that requires immediate treatment, as it can be fatal if not treated properly. Symptoms can vary in severity from person to person. Proper diagnosis and management are crucial as allergies can affect daily activities, sleep quality, work or school performance, and mood, directly impacting an individual's quality of life.


Management

The most effective management of allergies is avoiding allergens to reduce the risk of an allergic reaction. If the allergic reaction continues, medications may be needed to help reduce symptoms.


Common anti-allergic agents


Antihistamines

Antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...
s, specifically H1-antihistamines, are medicines which provide relief for allergic symptoms such as runny nose, sneezing, itching, and watery eyes from seasonal allergies (
hay fever Allergic rhinitis, of which the seasonal type is called hay fever, is a type of rhinitis, inflammation in the nose that occurs when the immune system overreacts to allergens in the air. It is classified as a Allergy, type I hypersensitivity re ...
). They are usually the first line of medications prescribed by a general practitioner, or a pharmacist for allergies in a community pharmacy. H1-antihistamines are further split into three groups known as the first-generation, second-generation and third-generation antihistamines. Another type of antihistamines known as H2-antihistamines are used to treat gastrointestinal conditions caused by excessive
stomach acid Gastric acid or stomach acid is the acidic component – hydrochloric acid – of gastric juice, produced by parietal cells in the gastric glands of the stomach lining. In humans, the pH is between one and three, much lower than most other an ...
. Mechanism H-1 antihistamines work by inhibiting histamine from binding to H-1 receptors. Histamine receptors expressed in
smooth muscle Smooth muscle is one of the three major types of vertebrate muscle tissue, the others being skeletal and cardiac muscle. It can also be found in invertebrates and is controlled by the autonomic nervous system. It is non- striated, so-called bec ...
s,
vascular endothelial cells The endothelium (: endothelia) is a single layer of squamous endothelial cells that line the interior surface of blood vessels and lymphatic vessels. The endothelium forms an interface between circulating blood or lymph in the lumen and the res ...
, the heart, and the
central nervous system The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain, spinal cord and retina. The CNS is so named because the brain integrates the received information and coordinates and influences the activity o ...
. This prevents a range of cellular signaling cascades that lead to
vasodilation Vasodilation, also known as vasorelaxation, is the widening of blood vessels. It results from relaxation of smooth muscle cells within the vessel walls, in particular in the large veins, large arteries, and smaller arterioles. Blood vessel wa ...
and increased membrane permeability from happening, thus preventing allergic symptoms.
First-generation antihistamine H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of his ...
s can easily cross the blood-brain barrier into the central nervous system to reach the H-1 receptors within, often causing drowsiness. Second-generation antihistamines selectively bind to the peripheral H-1 receptors outside the blood-brain barrier, therefore they are less likely to cause sedation.
First-generation antihistamine H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of his ...
s usually last around 4–6 hours whilst second-generation antihistamines work for 12–24 hours. Third generation antihistamines are metabolites of the second-generation antihistamines but without
cardiac toxicity Cardiotoxicity is the occurrence of heart dysfunction as electric or muscle damage, resulting in heart toxicity. This can cause heart failure, arrhythmia, myocarditis, and cardiomyopathy in patients. Some effects are reversible, while in others, p ...
. Indications and route of administration
Antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...
s are generally indicated for the alleviation of conditions such as allergic rhinitis, allergic conjunctivitis, or atopic dermatitis. Other indications may include nausea and vomiting. Antihistamines are usually for short-term treatment. Chronic allergies, such as
allergic asthma Asthma is a common chronic (medicine), long-term inflammation, inflammatory disease of the bronchiole, airways of the lungs. It is characterized by variable and recurring symptoms, reversible Airway obstruction, airflow obstruction, and easi ...
may include health problems which
antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...
s alone cannot treat. The routes of administration of
antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...
s are usually oral,
intranasal Nasal administration, popularly known as snorting, is a route of administration in which drugs are insufflation (medicine), insufflated through the nose. It can be a form of either topical administration or systemic administration, as the drugs t ...
, intraocular and
topical A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes ...
. Side effects Side effects generally exist more in first-generation antihistamines, for example
drowsiness Somnolence (alternatively sleepiness or drowsiness) is a state of strong desire for sleep, or sleeping for unusually long periods (compare hypersomnia). It has distinct meanings and causes. It can refer to the usual state preceding falling asleep ...
,
blurred vision Blurred vision is an ocular symptom where vision becomes less precise and there is added difficulty to resolve fine details. Temporary blurred vision may involve dry eyes, eye infections, alcohol poisoning, hypoglycemia, or low blood pressur ...
and
dry mouth Xerostomia, also known as dry mouth, is a subjective complaint of dryness in the mouth, which may be associated with a change in the composition of saliva, reduced salivary flow, or have no identifiable cause. This symptom is very common and is o ...
. Other common side effects for all generations include gastrointestinal side effects, headaches and tiredness. Antihistamines are generally safe to use during
pregnancy Pregnancy is the time during which one or more offspring gestation, gestates inside a woman's uterus. A multiple birth, multiple pregnancy involves more than one offspring, such as with twins. Conception (biology), Conception usually occurs ...
with second-generation antihistamines being more preferred due to their lack of sedation.


Decongestants

Decongestants A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal congestion in the upper respiratory tract. The active ingredient in most decongestants is either pseudoephedrine or phenylephrine (the latter of ...
are medicines which relieve nasal obstruction due to inflammation in the
upper respiratory tract The respiratory tract is the subdivision of the respiratory system involved with the process of conducting air to the alveoli for the purposes of gas exchange in mammals. The respiratory tract is lined with respiratory epithelium as respiratory ...
. They are also often used as the first-line therapy for nasal congestion from
common cold The common cold, or the cold, is a virus, viral infectious disease of the upper respiratory tract that primarily affects the Respiratory epithelium, respiratory mucosa of the human nose, nose, throat, Paranasal sinuses, sinuses, and larynx. ...
or
allergic rhinitis Allergic rhinitis, of which the seasonal type is called hay fever, is a type of inflammation in the nose that occurs when the immune system overreacts to allergens in the air. It is classified as a type I hypersensitivity reaction. Signs a ...
. Mechanism
Decongestant A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal congestion in the upper respiratory tract. The active ingredient in most decongestants is either pseudoephedrine or phenylephrine (the latter o ...
s work by binding to the
alpha-adrenergic receptors The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like bet ...
in the
sympathetic nervous system The sympathetic nervous system (SNS or SANS, sympathetic autonomic nervous system, to differentiate it from the somatic nervous system) is one of the three divisions of the autonomic nervous system, the others being the parasympathetic nervous sy ...
(controls our body's " fight or flight" response) on the
smooth muscle cells Smooth muscle is one of the three major types of vertebrate muscle tissue, the others being skeletal muscle, skeletal and cardiac muscle. It can also be found in invertebrates and is controlled by the autonomic nervous system. It is non-striated ...
situated on the blood vessels in nasal passages. This causes
vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vesse ...
(narrowing of blood vessels), helps reduce blood flow to the nasal mucosa and decreases swelling. Decongestants help open up nasal passages thus allowing for easier breathing. Indications and route of administration Decongestants are mainly used in conditions like common cold, allergic rhinitis, and
sinusitis Sinusitis, also known as rhinosinusitis, is an inflammation of the mucous membranes that line the sinuses resulting in symptoms that may include production of thick nasal mucus, nasal congestion, facial congestion, facial pain, facial pressure ...
. They provide temporary relief from symptoms of nasal congestion. Decongestants are available in oral and
intranasal Nasal administration, popularly known as snorting, is a route of administration in which drugs are insufflation (medicine), insufflated through the nose. It can be a form of either topical administration or systemic administration, as the drugs t ...
forms.
Naphazoline Naphazoline is a medicine used as a decongestant, and a vasoconstrictor added to eye drops to relieve red eye. It has a rapid action in reducing swelling when applied to mucous membranes. It is a sympathomimetic agent with marked alpha adrener ...
and
oxymetazoline Oxymetazoline, sold under the brand name Afrin among others, is a topical decongestant and vasoconstrictor medication. It is available over-the-counter as a nasal spray to treat nasal congestion and nosebleeds, as eye drops to treat eye rednes ...
are common topical (intranasal) decongestants, whilst
pseudoephedrine Pseudoephedrine, sold under the brand name Sudafed among others, is a sympathomimetic medication which is used as a decongestant to treat nasal congestion. It has also been used off-label for certain other indications, like treatment of lo ...
is the most common example of oral decongestant used to reduce nasal congestion. Topical decongestants have a faster onset of action compared with oral ones. Side effects Topical decongestants should not be used for longer than a week as prolonged use may result in
rhinitis medicamentosa Rhinitis medicamentosa (or RM, also known as rebound congestion) is a condition of rebound nasal congestion suspected to be brought on by extended use of topical decongestants (e.g., oxymetazoline, phenylephrine, xylometazoline, and naphazoli ...
(rebound nasal congestion). Common side effects for oral decongestants include
insomnia Insomnia, also known as sleeplessness, is a sleep disorder where people have difficulty sleeping. They may have difficulty falling asleep, or staying asleep for as long as desired. Insomnia is typically followed by daytime sleepiness, low ene ...
,
hypertension Hypertension, also known as high blood pressure, is a Chronic condition, long-term Disease, medical condition in which the blood pressure in the artery, arteries is persistently elevated. High blood pressure usually does not cause symptoms i ...
(elevated blood pressure), and difficulty in urination. Avoid use during pregnancy as it may cause
vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vesse ...
of uterine arteries thus reducing fetal blood supply. Combination therapy with antihistamines
Antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides ...
s and
decongestant A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal congestion in the upper respiratory tract. The active ingredient in most decongestants is either pseudoephedrine or phenylephrine (the latter o ...
s can be used as a combination to treat nasal congestion, runny nose, and sneezing symptoms caused by common cold and hay fever. Some examples include: #
Pseudoephedrine Pseudoephedrine, sold under the brand name Sudafed among others, is a sympathomimetic medication which is used as a decongestant to treat nasal congestion. It has also been used off-label for certain other indications, like treatment of lo ...
+
Loratadine Loratadine, sold under the brand name Claritin among others, is a medication used to treat allergies. This includes allergic rhinitis (hay fever) and hives. It is also available in drug combinations such as loratadine/pseudoephedrine, in whic ...
( Claritin-D®) #
Pseudoephedrine Pseudoephedrine, sold under the brand name Sudafed among others, is a sympathomimetic medication which is used as a decongestant to treat nasal congestion. It has also been used off-label for certain other indications, like treatment of lo ...
+
Cetirizine Cetirizine is a second-generation antihistamine, second-generation Peripherally selective antihistamine used to treat allergic rhinitis (hay fever), dermatitis, and urticaria (hives). It is taken by mouth. Effects generally begin within thirty ...
( Zyrtec-D®) #
Pseudoephedrine Pseudoephedrine, sold under the brand name Sudafed among others, is a sympathomimetic medication which is used as a decongestant to treat nasal congestion. It has also been used off-label for certain other indications, like treatment of lo ...
+
Fexofenadine Fexofenadine, sold under the brand name Allegra among others, is an antihistamine medication used in the treatment of allergy symptoms such as allergic rhinitis and urticaria. Therapeutically, fexofenadine is a selective peripheral H1 blocke ...
(Telfast-D®)


Corticosteroids

Corticosteroid Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones. Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are invo ...
s, specifically
glucocorticoid Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebra ...
s, are
anti-inflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation, fever or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs reduce pain by inhibiting mechan ...
agents used to treat allergic conditions. Corticosteroids can be classified into
mineralocorticoid Mineralocorticoids are a class of corticosteroids, which in turn are a class of steroid hormones. Mineralocorticoids are produced in the adrenal cortex and influence salt and water balances (electrolyte balance and fluid balance). The primary ...
s, which regulate salt and water balances, and glucocorticoids that play a role in
glucose Glucose is a sugar with the Chemical formula#Molecular formula, molecular formula , which is often abbreviated as Glc. It is overall the most abundant monosaccharide, a subcategory of carbohydrates. It is mainly made by plants and most algae d ...
homeostasis In biology, homeostasis (British English, British also homoeostasis; ) is the state of steady internal physics, physical and chemistry, chemical conditions maintained by organism, living systems. This is the condition of optimal functioning fo ...
and regulating the activation of immune cells. The word "glucocorticoid" is derived from "glucose +
cortex Cortex or cortical may refer to: Biology * Cortex (anatomy), the outermost layer of an organ ** Cerebral cortex, the outer layer of the vertebrate cerebrum, part of which is the ''forebrain'' *** Motor cortex, the regions of the cerebral cortex i ...
+
steroid A steroid is an organic compound with four fused compound, fused rings (designated A, B, C, and D) arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes t ...
", representing its role in the regulation of glucose
metabolism Metabolism (, from ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the co ...
, its
biosynthesis Biosynthesis, i.e., chemical synthesis occurring in biological contexts, is a term most often referring to multi-step, enzyme-Catalysis, catalyzed processes where chemical substances absorbed as nutrients (or previously converted through biosynthe ...
in the
adrenal cortex The adrenal cortex is the outer region and also the largest part of the adrenal gland. It is divided into three separate zones: zona glomerulosa, zona fasciculata and zona reticularis. Each zone is responsible for producing specific hormones. I ...
, and the steroid structure it possesses.


Mechanism

Glucocorticoids bind to
glucocorticoid receptors Steroid hormone receptors are found in the nucleus, cytosol, and also on the plasma membrane of target cells. They are generally intracellular receptors (typically cytoplasmic or nuclear) and initiate signal transduction for steroid hormones which ...
to form a complex which activates the
transcription Transcription refers to the process of converting sounds (voice, music etc.) into letters or musical notes, or producing a copy of something in another medium, including: Genetics * Transcription (biology), the copying of DNA into RNA, often th ...
of anti-inflammatory genes in the
nucleus Nucleus (: nuclei) is a Latin word for the seed inside a fruit. It most often refers to: *Atomic nucleus, the very dense central region of an atom *Cell nucleus, a central organelle of a eukaryotic cell, containing most of the cell's DNA Nucleu ...
(
transactivation In the context of gene regulation: transactivation is the increased rate of gene expression triggered either by biological processes or by artificial means, through the expression of an intermediate transactivator protein. In the context of recep ...
) and represses the expression of
pro-inflammatory Inflammation (from ) is part of the biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or irritants. The five cardinal signs are heat, pain, redness, swelling, and loss of function (Latin ''calor'', ''d ...
factors in the
cytosol The cytosol, also known as cytoplasmic matrix or groundplasm, is one of the liquids found inside cells ( intracellular fluid (ICF)). It is separated into compartments by membranes. For example, the mitochondrial matrix separates the mitochondri ...
(transrepression). Ultimately, they decrease the synthesis and release of inflammatory mediators such as mast cells,
eosinophil Eosinophils, sometimes called eosinophiles or, less commonly, acidophils, are a variety of white blood cells and one of the immune system components responsible for combating multicellular parasites and certain infections in vertebrates. Along wi ...
s, and
cytokine Cytokines () are a broad and loose category of small proteins (~5–25 kDa) important in cell signaling. Cytokines are produced by a broad range of cells, including immune cells like macrophages, B cell, B lymphocytes, T cell, T lymphocytes ...
s.


Indications

Glucocorticoids have a wide range of
therapeutic A therapy or medical treatment is the attempted remediation of a health problem, usually following a medical diagnosis. Both words, ''treatment'' and ''therapy'', are often abbreviated tx, Tx, or Tx. As a rule, each therapy has indications an ...
uses. Since they suppress inflammation and reduce the signs and symptoms such as swelling, redness and itching, they are commonly used to treat allergic conditions including allergic rhinitis, asthma and eczema. Glucocorticoids can be given via different routes of administration, depending on the condition and severity. The most common ones are oral, inhalation, topical and injection.


Side effects

Common side effects of glucocorticoids include fluid retention, mood changes and weight gain. The side effects are associated with the dosage, type of drug used and the duration of treatment. Systemic corticosteroids are not considered first-line therapy for chronic management due to common and significant risks of
adverse reaction An adverse effect is an undesired harmful effect resulting from a medication or other intervention, such as surgery. An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. The term complic ...
s. These include
osteoporosis Osteoporosis is a systemic skeletal disorder characterized by low bone mass, micro-architectural deterioration of bone tissue leading to more porous bone, and consequent increase in Bone fracture, fracture risk. It is the most common reason f ...
,
cataract A cataract is a cloudy area in the lens (anatomy), lens of the eye that leads to a visual impairment, decrease in vision of the eye. Cataracts often develop slowly and can affect one or both eyes. Symptoms may include faded colours, blurry or ...
s, depressed immunity and
Cushing's syndrome Cushing's syndrome is a collection of signs and symptoms due to prolonged exposure to glucocorticoids such as cortisol. Signs and symptoms may include high blood pressure, abdominal obesity but with thin arms and legs, reddish stretch marks, ...
.


Leukotriene pathway modifiers

Leukotriene Leukotrienes are a family of eicosanoid inflammation, inflammatory mediators produced in leukocytes by the redox, oxidation of arachidonic acid (AA) and the essential fatty acid eicosapentaenoic acid (EPA) by the enzyme arachidonate 5-lipoxyg ...
s are lipid mediators formed from
arachidonic acid Arachidonic acid (AA, sometimes ARA) is a polyunsaturated omega−6 fatty acid 20:4(ω−6), or 20:4(5,8,11,14). It is a precursor in the formation of leukotrienes, prostaglandins, and thromboxanes. Together with omega−3 fatty acids an ...
by the
enzyme An enzyme () is a protein that acts as a biological catalyst by accelerating chemical reactions. The molecules upon which enzymes may act are called substrate (chemistry), substrates, and the enzyme converts the substrates into different mol ...
5-lipoxygenase Arachidonate 5-lipoxygenase, also known as ALOX5, 5-lipoxygenase, 5-LOX, or 5-LO, is a non-heme iron-containing enzyme (EC 1.13.11.34) that in humans is encoded by the ''ALOX5'' gene. Arachidonate 5-lipoxygenase is a member of the lipoxygenase fa ...
, causing constriction of the airway smooth muscle, increased
mucus Mucus (, ) is a slippery aqueous secretion produced by, and covering, mucous membranes. It is typically produced from cells found in mucous glands, although it may also originate from mixed glands, which contain both Serous fluid, serous and muc ...
secretion and enhanced immune response, resulting in allergic inflammation. Leukotriene pathway modifiers can be classified into two types: the cysteinyl leukotriene receptor antagonists (including
Montelukast Montelukast, sold under the brand name Singulair among others, is a medication used in the maintenance treatment of asthma. It is generally less preferred for this use than inhaled corticosteroids. It is not useful for acute asthma attacks. ...
and
Zafirlukast Zafirlukast is an orally administered leukotriene receptor antagonist (LTRA) used for the chronic treatment of asthma. While zafirlukast is generally well tolerated, headaches and stomach upset often occur. Some rare side effects can occur, whic ...
) that bind to leukotriene receptors to inhibit
bronchoconstriction Bronchoconstriction is the constriction of the airways in the lungs due to the tightening of surrounding smooth muscle, with consequent coughing, wheezing, and shortness of breath. Causes The condition has a number of causes, the most common bei ...
and other effects of leukotrienes, and
Zileuton Zileuton (trade name Zyflo) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used for the maintenance treatment of asthma. Zileuton was introduced in 1996 by Abbott Laborato ...
, a 5-lipoxygenase inhibitor which directly prevents the synthesis of leukotrienes. All three leukotriene pathway modifiers are indicated for the treatment of chronic asthma, but only Montelukast is approved to treat allergic rhinitis, with a similar effectiveness as antihistamines, but lower effectiveness than nasal corticosteroids in relieving the symptoms of seasonal allergic rhinitis.


Mast cell stabilizers

Mast cell stabilizer Mast cell stabilizers are medications used to prevent or treat certain allergic disorders. They block mast cell degranulation, stabilizing the cell and thereby preventing the release of histamine and related mediators. One suspected pharmacody ...
s inhibit the release of allergic and inflammatory mediators, helping to prevent and treat allergic conditions. They work by blocking a
calcium channel A calcium channel is an ion channel which shows selective permeability to calcium ions. It is sometimes synonymous with voltage-gated calcium channel, which are a type of calcium channel regulated by changes in membrane potential. Some calcium chan ...
which is essential for mast cell
degranulation Degranulation is a cellular process that releases antimicrobial, cytotoxic, or other molecules from secretory vesicles called granules found inside some cells. It is used by several different cells involved in the immune system, including gran ...
, inhibiting the release of histamine and other mediators from mast cells. Examples of mast cell stabilizers include
cromolyn sodium Cromoglicic acid ( INN)—also referred to as cromolyn ( USAN), cromoglycate (former BAN), or cromoglicate—is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate or cromolyn sodiu ...
and nedocromil sodium. They are commonly used in
eye drop Eye drops or eyedrops are liquid drops applied directly to the surface of the eye usually in small amounts such as a single drop or a few drops. Eye drops usually contain saline to match the salinity of the eye. Drops containing only saline ...
s to treat allergic conjunctivitis, in intranasal formulations for allergic rhinitis and given by inhalation for asthma. Common side effects include
irritation Irritation, in biology and physiology, is a state of inflammation or painful reaction to allergy or cell-lining damage. A stimulus or agent which induces the state of irritation is an irritant. Irritants are typically thought of as chemical age ...
, itching, and cough.


Less common anti allergic agents


Adrenaline

Adrenaline Adrenaline, also known as epinephrine, is a hormone and medication which is involved in regulating visceral functions (e.g., respiration). It appears as a white microcrystalline granule. Adrenaline is normally produced by the adrenal glands a ...
(or epinephrine) is the first-line treatment for the life-threatening allergic reaction known as
anaphylaxis Anaphylaxis (Greek: 'up' + 'guarding') is a serious, potentially fatal allergic reaction and medical emergency that is rapid in onset and requires immediate medical attention regardless of the use of emergency medication on site. It typicall ...
. The most common anaphylactic reactions are induced by foods, insect stings and medications. Adrenaline is both a
hormone A hormone (from the Ancient Greek, Greek participle , "setting in motion") is a class of cell signaling, signaling molecules in multicellular organisms that are sent to distant organs or tissues by complex biological processes to regulate physio ...
and a medication which plays an important role in the body's "fight-or-flight" response (the acute stress response). It is used to treat anaphylaxis as it provides immediate symptomatic relief. It helps open up the airways, maintain heart function and raise
blood pressure Blood pressure (BP) is the pressure of Circulatory system, circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term ...
, reducing or reversing severe symptoms like throat swelling and difficulty in breathing.


Immunotherapy

Allergen immunotherapy Allergen immunotherapy, also known as desensitization or hypo-sensitization, is a medical treatment for environmental allergies (such as insect bites) and asthma. Immunotherapy involves exposing people to larger and larger amounts of allergens ...
is the last line of medications, also known as the closest "cure" for allergies. It is often recommended for patients whose symptoms cannot be controlled by medications, or those who require multiple medications to control their allergies. This immunotherapy involves regular administration of gradually increasing doses of the substance to which the person is allergic over several years. Treatment can be given as an injection, tablet, sprays or
sublingual Sublingual (List of abbreviations used in medical prescriptions, abbreviated SL), from the Latin for "under the tongue", refers to the pharmacological route of administration by which substances diffuse into the blood through Tissue (biology), t ...
drops. The gradual increase of allergen causes the immune system to become less sensitive to the substance ( desensitization), reducing symptoms during future exposures to the allergen, and possibly preventing new allergies.


Future developments

Research led by ''Professor Billy K C Chow from the School of Biological Sciences, Faculty of Sciences, the University of Hong Kong'' has been conducted into the use of small novel MRGPRX2 antagonists as some cases of allergies are refractive to currently available treatments.{{Cite web , title=HKU biologists designed and developed novel anti-allergic drugs by targeting Mas-related G protein-coupled receptor (GPCR) X2 (MRGPRX2) - News - Faculty of Science, HKU , url=https://www.scifac.hku.hk/news/hku-biologists-designed-and-developed-novel-anti-allergic-drugs-by-targeting-mas-related-g-protein-coupled-receptor-gpcr-x2-mrgprx2 , access-date=2024-04-04 , website=www.scifac.hku.hk , language=en MRGPRX2 receptors are discovered to be responsible for producing inflammatory allergic reactions. The absence of this drug on the current market also emphasises its importance in future use.


References

Immunosuppressants