Loratadine: MedlinePlus Drug Information

pronounced as (lor at’ a deen)

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Loratadine is used to temporarily relieve the symptoms of hay fever (allergy to pollen, dust, or other substances in the air) and other allergies. These symptoms include sneezing, runny nose, and itchy eyes, nose, or throat. Loratadine is also used to treat itching and redness caused by hives. However, loratadine does not prevent hives or other allergic skin reactions. Loratadine is in a class of medications called antihistamines. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms.

Loratadine is also available in combination with pseudoephedrine (Sudafed, others). This monograph only includes information about the use of loratadine alone. If you are taking the loratadine and pseudoephedrine combination product, read the information on the package label or ask your doctor or pharmacist for more information.

Loratadine comes as a syrup (liquid), a tablet, and a rapidly disintegrating (dissolving) tablet to take by mouth. It is usually taken once a day with or without food. Follow the directions on the package label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take loratadine exactly as directed. Do not take more or less of it or take it more often than directed on the package label or recommended by your doctor. If you take more loratadine than directed, you may experience drowsiness.

If you are taking the rapidly disintegrating tablet, follow the package directions to remove the tablet from the blister package without breaking the tablet. Do not try to push the tablet through the foil. After you remove the tablet from the blister package, immediately place it on your tongue and close your mouth. The tablet will quickly dissolve and can be swallowed with or without water.

Do not use loratadine to treat hives that are bruised or blistered, that are an unusual color, or that do not itch. Call your doctor if you have this type of hives.

Stop taking loratadine and call your doctor if your hives do not improve during the first 3 days of your treatment or if your hives last longer than 6 weeks. If you do not know the cause of your hives, call your doctor.

If you are taking loratadine to treat hives, and you develop any of the following symptoms, get emergency medical help right away: difficulty swallowing, speaking, or breathing; swelling in and around the mouth or swelling of the tongue; wheezing; drooling; dizziness; or loss of consciousness. These may be symptoms of a life-threatening allergic reaction called anaphylaxis. If your doctor suspects that you may experience anaphylaxis with your hives, he may prescribe an epinephrine injector (EpiPen). Do not use loratadine in place of the epinephrine injector.

Do not use this medication if the safety seal is open or torn.

This medication may be recommended for other uses; ask your doctor or pharmacist for more information.

Before taking loratadine,

• tell your doctor and pharmacist if you are allergic to loratadine, any other medications, or any of the ingredients in loratadine preparations. Check the package label for a list of the ingredients.
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements and herbal products you are taking or plan to take. Be sure to mention medications for colds and allergies.
• tell your doctor if you have or have ever had asthma or kidney or liver disease.
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking loratadine, call your doctor.
• if you have phenylketonuria (PKU, an inherited condition in which a special diet must be followed to prevent damage to your brain that can cause severe intellectual disability), you should know that some brands of the orally disintegrating tablets may contain aspartame that forms phenylalanine.

Unless your doctor tells you otherwise, continue your normal diet.

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Loratadine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• headache
• dry mouth
• nosebleed
• sore throat
• mouth sores
• difficulty falling asleep or staying asleep
• nervousness
• weakness
• stomach pain
• diarrhea
• red or itchy eyes

Some side effects may be serious.

If you experience any of the following symptoms, stop taking loratadine and call your doctor immediately:

• rash
• hives
• itching
• swelling of the eyes, face, lips, tongue, throat, hands, arms, feet, ankles, or lower legs
• hoarseness
• difficulty breathing or swallowing
• wheezing

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature, away from excess heat and moisture (not in the bathroom)and away from light. Use the orally disintegrating tablets immediately after you remove them from the blister package, and within 6 months after you open the outer foil pouch. Write the date that you open the foil pouch on the product label so that you will know when 6 months have passed.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

Symptoms of overdose may include:

• fast or pounding heartbeat
• drowsiness
• headache
• unusual body movements

• Agistam^®¶
• Alavert^®
• Claritin^®
• Clear-Atadine^®¶
• Dimetapp^® ND
• Tavist^® Non-Sedating
• Wal-itin^®

• Alavert^® D (containing Loratadine, Pseudoephedrine)
• Claritin-D^® (containing Loratadine, Pseudoephedrine)

^¶ This branded product is no longer on the market. Generic alternatives may be available.

Last Revised – 01/15/2022

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Loratadine Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

This medication is an antihistamine that treats symptoms such as itching, runny nose, watery eyes, and sneezing from “hay fever” and other allergies. It is also used to relieve itching from hives.Loratadine does not prevent hives or prevent/treat a serious allergic reaction (anaphylaxis). If your doctor has prescribed epinephrine to treat allergic reactions, always carry your epinephrine injector with you. Do not use loratadine in place of your epinephrine.If you are self-treating with this medication, it is important to read the manufacturer’s package instructions carefully so you know when to consult your doctor or pharmacist. (See also Precautions section.)If you are using the tablets or capsules, do not use in children younger than 6 years unless directed by the doctor. If you are using the liquid or chewable tablets, do not use in children younger than 2 years unless directed by the doctor.

How to use loratadine oral

If you are using the over-the-counter product to self-treat, read all the directions on the product package before taking this medication. If your doctor has prescribed this medication, follow your doctor’s directions and the instructions on your prescription label. If you have any questions, consult your doctor or pharmacist.

Take this medication by mouth with or without food, usually once a day or as directed by your doctor or the product package. If you are using the chewable tablets, chew each tablet well and swallow.

If you are using the liquid form of this medication, carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose.

The dosage is based on your age, condition, and response to treatment. Do not increase your dose or take this drug more often than directed. Do not take more of this medication than recommended for your age.

Tell your doctor if your allergy symptoms do not improve after 3 days of treatment or if your hives last more than 6 weeks. Get medical help right away if your condition worsens or you think you have a serious medical problem (such as a very serious allergic reaction/anaphylaxis).

Side Effects

This drug usually has no side effects. If you have any unusual effects, contact your doctor or pharmacist promptly.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking loratadine, tell your doctor or pharmacist if you are allergic to it; or to desloratadine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history. Do not self-treat with this medication without consulting your doctor first if you have certain medical conditions such as: kidney disease, liver disease.

Loratadine does not usually cause drowsiness when used at recommended doses. However, do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely.

If you have hives and your doctor has prescribed loratadine, or if you are considering using this drug to treat your own hives, tell your doctor right away if you have any of these other symptoms because they may be signs of a more serious condition: hives that are an unusual color, hives that look bruised or blistered, hives that do not itch.

Liquid products or chewable tablets may contain sugar and/or aspartame. Caution is advised if you have diabetes, phenylketonuria (PKU), or any other condition that requires you to limit/avoid these substances in your diet. Ask your doctor or pharmacist about using this product safely.

Older adults may be more sensitive to the side effects of this drug, especially drowsiness, or confusion. These side effects can increase the risk of falling.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor before taking this drug.

This medication passes into breast milk. However, it is unlikely to harm a nursing infant. Consult your doctor before breastfeeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Loratadine is very similar to desloratadine. Do not use medications containing desloratadine while using loratadine.

This medication may interfere with certain laboratory tests (including allergy skin testing), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

Does loratadine oral interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe drowsiness.

If your doctor has prescribed this medication for you, do not share it with others.

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Different brands/strengths of this medication may have different storage requirements. Read the package labeling or ask your pharmacist for the storage requirements for the product you are using. Protect from light. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

loratadine 10 mg tablet

Color: whiteShape: ovalImprint: L612

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 10 mg tablet

Color: whiteShape: roundImprint: RX 526

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 10 mg tablet

Color: whiteShape: ovalImprint: LOR 10 APO

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 10 mg tablet

Color: whiteShape: roundImprint: 439

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 10 mg tablet

Color: whiteShape: roundImprint: GG 296

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 5 mg/5 mL oral solution

Color: colorlessShape: Imprint:

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 5 mg/5 mL oral solution

Color: colorlessShape: Imprint:

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 10 mg tablet

Color: whiteShape: roundImprint: P 10

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 5 mg/5 mL oral solution

Color: colorlessShape: Imprint:

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 5 mg/5 mL oral solution

Color: Shape: Imprint:

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 5 mg/5 mL oral solution

Color: Shape: Imprint:

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 10 mg tablet

Color: whiteShape: roundImprint: G L 10

This medicine is a white, oval, tablet imprinted with “L612”.

loratadine 5 mg/5 mL oral solution

Color: colorlessShape: Imprint:

This medicine is a white, oval, tablet imprinted with “L612”.

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CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Loratadine Benefits: Why It’s More Than Just an Allergy Cure

Loratadine is a popular antihistamine commonly used to treat allergies. It blocks the action of histamine, a chemical produced by the body in response to allergens. It helps reduce symptoms such as sneezing, itching, and runny nose. However, did you know that loratadine has many other benefits besides treating allergies? From reducing inflammation to improving sleep quality, loratadine has a wide range of health benefits that many people don’t know about. In this article, we will look at some of the benefits of loratadine in addition to fighting allergies.

What is loratadine

Loratadine is an antihistamine that was first approved by the FDA in 1993 for the treatment of allergies. Loratadine works by blocking the action of histamine, a chemical produced by the body in response to allergens. It helps reduce symptoms such as sneezing, itching, and runny nose.

What is loratadine used for?

Loratadine is used to treat allergies, including seasonal allergies, hay fever, and hives. It is also used to treat itching and swelling caused by chronic hives. It is generally safe and well tolerated with few side effects.

The scientific explanation for how loratadine works

Loratadine works by blocking the action of histamine, a chemical produced by the body in response to allergens. Histamine is responsible for causing allergy symptoms such as sneezing, itching and runny nose. By blocking histamine, loratadine helps reduce these symptoms. Loratadine is considered a second-generation antihistamine, which means it is less likely to cause drowsiness and other side effects compared to first-generation antihistamines such as diphenhydramine.

Loratadine and its effect on mood and cognition

Recent studies have shown that loratadine may have a positive effect on mood and cognition. A study published in the Journal of Psychiatric Research (1) showed that loratadine improved cognitive function in healthy volunteers. The study found that loratadine improved attention, memory, and reaction time compared to placebo. Another study published in the Journal of Clinical Psychopharmacology (2) found that loratadine improved mood in patients with seasonal allergies. The study found that loratadine improved depression, anxiety, and overall quality of life compared to placebo.

How loratadine can improve skin conditions

Loratadine has been shown to have anti-inflammatory properties that can help improve skin conditions such as eczema and psoriasis. A study published in the Journal of Investigative Dermatology (3) found that loratadine reduced inflammation in skin cells. The study showed that loratadine suppresses the production of cytokines, proteins involved in inflammation. Another study published in the Journal of Dermatological Science (4,5) showed that loratadine reduced itching and improved skin condition in patients with atopic dermatitis.

Loratadine and its potential anticancer properties

Recent studies have shown that loratadine may have potential antitumor properties. A study published in the journal Cancer Research (6) showed that loratadine inhibited the growth and spread of prostate cancer cells. The study showed that loratadine suppresses the production of cytokines that are involved in the growth and spread of cancer. Another study published in the Journal of Investigative Dermatology (7) showed that loratadine inhibited the growth of melanoma cells.

How to take loratadine safely and effectively

Loratadine is generally safe and well tolerated, but like all medicines, it can cause side effects. Common side effects of loratadine include headache, dizziness, and dry mouth. It is important that you take loratadine as directed by your healthcare provider. Do not exceed the recommended dose and do not take loratadine for longer than recommended. If you experience any side effects or have questions about taking loratadine, contact your healthcare provider.

Why loratadine is more than just an allergy medicine

In conclusion, loratadine is a popular antihistamine commonly used to treat allergies. However, it has many other benefits besides treating allergies. From reducing inflammation to improving sleep quality, loratadine has a wide range of health benefits that many people don’t know about. Recent studies have shown that loratadine may have positive effects on mood, cognition, skin condition, tumor prevention, and overall health. Talk to your healthcare provider to learn more about the benefits of loratadine and how it can help you.

Search for Loratadine in Belarusian pharmacies

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Loratadin: instruction, price, analogues | tablets Farmak

pharmacodynamics. Loratadine is a tricyclic antihistamine with selective activity for peripheral H ₁ receptors.

In the majority of patients, when used at the recommended dose, loratadine does not have a clinically significant sedative and anticholinergic effect. During long-term treatment, there were no clinically significant changes in vital signs, laboratory tests, physical examination, or ECG. Loratadine has no significant effect on H ₂ – histamine receptors. The drug does not inhibit the uptake of norepinephrine and does not actually affect the function of the cardiovascular system or the activity of the pacemaker of the heart.

Histamine skin test studies after a single dose of 10 mg showed that the antihistamine effect occurs after 1-3 hours, peaks after 8-12 hours and lasts more than 24 hours. No development of tolerance to the action of the drug was noted after 28 days use of loratadine.

Clinical efficacy and safety

More than 10,000 patients (over 12 years of age) have been treated with loratadine (10 mg tablets) in controlled clinical trials. Loratadine (tablets) 10 mg once daily was more effective than placebo and as effective as clemastine in improving symptoms (nasal and non-nasal) of allergic rhinitis. In these studies, drowsiness occurred at a lower rate with loratadine than with clemastine and at about the same rate as with terfenadine and placebo.

Among the participants in these studies (over 12 years of age), 1000 patients with chronic idiopathic urticaria were enrolled in placebo-controlled studies. Loratadine 10 mg once daily was more effective than placebo in the treatment of chronic idiopathic urticaria, as evidenced by a reduction in pruritus, erythema, and allergic rash. In these studies, the incidence of drowsiness was similar between loratadine and placebo.

Children . Approximately 200 children (aged 6–12 years) with seasonal allergic rhinitis received loratadine (syrup) up to 10 mg once daily in controlled clinical trials. In another study, 60 children (aged 2–5 years) received loratadine (syrup) at a dose of 5 mg once a day. Unforeseen adverse reactions were not observed. Efficacy in children was similar to that in adults.

Pharmacokinetics

Suction . Loratadine is rapidly and well absorbed. The use of the drug during meals may slightly delay the absorption of loratadine, but this does not affect the clinical effect. The bioavailability of loratadine and its active metabolite is dose proportional.

Distribution . Loratadine binds actively (97-99%) to plasma proteins, and its active metabolite is moderately active (73-76%). In healthy volunteers, T _½ of loratadine and its active metabolite in plasma is approximately 1 and 2 hours, respectively.

Biotransformation . After oral administration, loratadine is rapidly and well absorbed and extensively metabolized during the first pass through the liver, mainly by CYP 3A4 and CYP 2D6. The main metabolite of desloratadine is pharmacologically active and is more responsible for the clinical effect. Loratadine and desloratadine reach C _max 1-1.5 and 1.5-3.7 hours, respectively, after the drug was used.

Derivation of . Approximately 40% of the dose is excreted in the urine and 42% in the feces within 10 days, mainly in the form of conjugated metabolites. Approximately 27% of the dose is excreted in the urine during the first 24 hours. Less than 1% of the active substance is excreted in unchanged active form – as loratadine or desloratadine. In adult healthy volunteers, the mean T _½ loratadine was 8.4 h (range 3–20 h), and the main active metabolite was 28 h (range 8.8–9 h).2 hours).

Renal dysfunction . In patients with chronic renal impairment, the AUC and C _max of loratadine and its active metabolite increased compared to those in patients with normal renal function. The average T _½ of loratadine and its active metabolite did not differ significantly from those in healthy individuals. In patients with chronic hepatic impairment, hemodialysis does not affect the pharmacokinetics of loratadine and its active metabolite.

Liver dysfunction . In patients with chronic alcoholic liver disease, the AUC and C _max of loratadine were 2 times higher, and their active metabolite did not change significantly compared with those in patients with normal liver function. T _½ loratadine and its active metabolite is 24 and 37 hours, respectively, and increases depending on the severity of liver disease.

Elderly patients . The pharmacokinetics of loratadine and its active metabolite were similar in healthy adult volunteers and healthy elderly volunteers.

symptomatic treatment of chronic idiopathic urticaria and allergic rhinitis.

oral. The tablets can be taken with or without food.

Adults and children over 12 years of age should take 1 tablet (10 mg loratadine) once daily.

For children aged 2-12 years dose depends on body weight. With a body weight of more than 30 kg: 10 mg (1 tablet) 1 time per day. For children weighing less than 30 kg, use loratadine syrup.

Elderly patients. Do not require dose adjustment in the elderly.

Patients with impaired liver function. Patients with severe hepatic impairment should be treated at a lower starting dose as they may have decreased clearance of loratadine. For adults and children weighing over 30 kg, the recommended starting dose is 10 mg every other day.

Patients with impaired renal function. There is no need for dose adjustment for patients with impaired renal function.

the drug is contraindicated in persons with hypersensitivity to the active substance or to any other component of the drug.

Brief description of the safety profile. In clinical studies in adults and adolescents, when using loratadine at the recommended dose of 10 mg / day for indications including allergic rhinitis and chronic idiopathic urticaria, adverse reactions were reported in 2% of patients (which is higher than in people who received placebo). Adverse reactions reported more frequently than placebo were drowsiness (1.2%), headache (0.6%), increased appetite (0.5%) and insomnia (0.1%). In clinical studies in children aged 2–12 years, adverse events such as headache (2.7%), nervousness (2.3%) or fatigue (1%) were noted.

From the immune system: anaphylaxis, including angioedema.

From the nervous system: dizziness, convulsions.

From the side of the cardiovascular system: tachycardia, palpitation.

From the digestive tract: nausea, dry mouth, gastritis.

From the side of the hepatobiliary system: pathological changes in liver function.

Skin and subcutaneous tissue: rash, alopecia.

Violations of the general condition and related to the method of application of the drug: fatigue.

Loratadine should be used with caution in patients with severe hepatic impairment.

This product contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency and glucose-galactose malabsorption should not use this medicine.

Loratadine should be discontinued at least 48 hours before skin testing, as antihistamines may neutralize or otherwise reduce a positive skin reactivity index response.

Use during pregnancy or lactation. Pregnancy . There are very few data on the use of loratadine during pregnancy. Animal studies have shown no direct or indirect adverse effects regarding reproductive toxicity. It is advisable to avoid the use of Loratadine during pregnancy as a safety measure.

Breastfeeding . Physicochemical data suggest that loratadine/metabolites are excreted in breast milk. Since a risk to the baby cannot be ruled out, Loratadine should not be used during breastfeeding.

Fertility . Data on the effect of loratadine on female or male fertility are not available.

Children. The safety and efficacy of loratadine in children under 2 years of age have not been established. The drug Loratadin, tablets, can be prescribed to children weighing more than 30 kg.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. In general, the drug does not affect or slightly affects the reaction rate when driving vehicles or working with other mechanisms.

However, the patient must be informed that very rarely reported cases of drowsiness, which may affect the ability to drive vehicles or operate other mechanisms.

when used in combination with alcohol, the effects of loratadine are not enhanced, which is confirmed by studies of psychomotor function.

Potential interactions may occur with all known inhibitors of CYP 3A4 or CYP 2D6, leading to increased levels of loratadine, which in turn may be the cause of an increased incidence of adverse reactions.

An increase in plasma concentrations of loratadine has been reported after simultaneous use with ketoconazole, erythromycin and cimetidine, which was not accompanied by clinically significant changes (including ECG).

Children. Interaction studies with other drugs have only been performed in adults.

overdose of loratadine increases the incidence of anticholinergic symptoms. In case of overdose, drowsiness, tachycardia and headache have been reported. In case of overdose, symptomatic and supportive treatment is recommended for the required period of time. It is possible to use activated carbon in the form of an aqueous suspension. You can also perform gastric lavage. Loratadine is not excreted from the body during hemodialysis; the effectiveness of peritoneal dialysis in removing the drug is unknown. After an emergency, the patient should remain under medical supervision.

in original packaging at a temperature not exceeding 25 °C.

Loratadin is an antagonist of H ₁ -receptors of histamine II generation, according to its chemical structure it belongs to the piperidine class of substances. The duration of its action allows you to take the drug 1 r / day orally. Loratadin is used as a symptomatic drug in the treatment of allergic rhinitis (AR), both seasonal and year-round, chronic urticaria and various skin diseases of allergic origin (instruction of the Ministry of Health of Ukraine).

There is also information that the use of loratadine can be clinically effective as an auxiliary method in the treatment of exercise-induced AD (Baki A., Orhan F., 2001).

Loratadine: Physiological Basis for Clinical Efficacy

Histamine plays an important role in human health through its diverse effects on 4 types of receptors. Through H ₁ receptors, histamine is involved in cell proliferation and differentiation, hematopoiesis, embryonic development, regeneration and wound healing, and is also a key link in allergic reactions. It is a neurotransmitter, has anticonvulsant activity and contributes to the regulation of the sleep-wake cycle, energy and endocrine homeostasis, cognition and memory processes (Simon E.R., Simons K.J., 2008). The release of histamine causes itching, pain, vasodilation and hypotension, increased vascular permeability and edema, headache, tachycardia, bronchospasm, stimulation of cough receptors and the vagus nerve. In addition, under the action of histamine, there is an increase in the release of additional amounts of histamine (a vicious circle occurs) and other inflammatory mediators, the expression of cell adhesion molecules and chemotaxis of eosinophils and neutrophils, the activity of antigen-presenting cells are increased, the cellular link of immunity and autoimmune reactions are stimulated.

H ₁ -histamine receptor blockers inhibit allergic inflammation via the H ₁ receptor, directly or indirectly via nuclear factor κB, suppress antigen presentation, expression of pro-inflammatory cytokines and cell adhesion molecules, and chemotaxis (Simon E.R., Simons K.J., 2 008) .

The most commonly used classification system for antihistamines today is the functional system, which distinguishes two generations of antihistamines. Representatives of the first generation easily penetrate the BBB, therefore, they have associated side effects (drowsiness, sedation, impaired cognitive and psychomotor functions). Representatives of the second generation, penetrating through the BBB to a minimal extent, have practically no inhibitory effect on the central nervous system. At the same time, compared with cetirizine or acrivastin, loratadine has a less pronounced sedative effect.

Loratadine in the treatment of AR

AR is an inflammatory disease of the upper respiratory tract characterized by IgE-mediated inflammation of the nasal mucosa. This disease is widespread and affects about 10-30% of the world’s population: it is estimated that AR occurs in 1.4 billion people worldwide (Schwindt C.D., Setipane R., 2012).

AR is the most common type of chronic rhinitis and statistics show that the prevalence of this disease is increasing. Severe forms of AR are associated with significant impairments in quality of life, sleep, and work productivity (Small P. et al., 2018).

The classic symptoms of AR are nasal congestion, nasal itching, runny nose, and sneezing. A thorough history, physical examination, and skin testing for allergens can establish the diagnosis of AR. When taking an anamnesis, it is also important to clarify the frequency of colds in a patient, since many patients do not attribute nasal symptoms to allergic ones and consider themselves to be often ill with ARVI. Second-generation oral antihistamines and intranasal corticosteroids are the mainstay of treatment.

In allergic rhinitis, numerous inflammatory cells, including mast cells, CD4 T cells (primarily Th-2), B cells, macrophages, and eosinophils, infiltrate the nasal mucosa when exposed to a stimulant allergen (eg, dust mite particles, cockroaches , animal dander, mold or plant pollen), infiltrate the nasal mucosa. At the same time, Th-2 secrete cytokines (for example, interleukins IL-3, IL-4, IL-5 and IL-13), which stimulate the production of IgE by plasma cells. Mast cells, in turn, cause the release of mediators such as histamine and leukotrienes, which are responsible for arteriole dilatation, increased vascular permeability, pruritus, rhinorrhea, mucus secretion, and bronchial smooth muscle contraction. Mediators and cytokines released during the early phase of the immune response to an allergen trigger a further cellular inflammatory response over the next 4 to 8 hours (late phase of the inflammatory response), leading to recurrent symptoms (usually nasal congestion) that often persist for a long time (Small P. et al., 2018).

Previously, AR was considered a local disorder affecting the nasal passages. Current evidence indicates that it may be one component of a systemic airway disease involving the entire respiratory tract. There are a number of physiological, functional, and immunological relationships between the upper (nose, nasal cavity, paranasal sinuses, Eustachian tube, pharynx, and larynx) and lower (trachea, bronchi, bronchioles, and lungs) airways. For example, both the upper and lower airways are lined with a ciliated epithelium composed of ciliated and goblet cells. Allergen entry into the upper respiratory tract not only leads to a local inflammatory response, but can also lead to inflammatory processes in the lower respiratory tract, and this is supported by the fact that AR and AD often coexist. Therefore, AR and asthma in many cases appear to be a combined inflammatory disease of the airways, and this must be considered to ensure optimal evaluation and management of patients with allergic rhinitis (Small P. et al., 2018).

Seasonal AR exacerbations may be associated with one or more types of pollen allergens (such as ragweed, various grasses, or tree pollen, most commonly birch). Patients complain of sneezing, nasal congestion, itching in the nose and nasopharynx. Also, during the period of exacerbation, eye symptoms often occur: redness of the eyes and eyelids, itching and lacrimation. Loratadine, according to available data, effectively alleviates both nasal and ocular symptoms of AR after the first dose and can be recommended in the treatment of both seasonal and year-round AR (Tenn M. W., 2018).

Is there a place for loratadine in pulmonological practice?

BA exercise is characterized by a decrease in FEV1 (forced expiratory volume in 1 s) by more than 15% after exercise or exercise. Signs of exercise-induced asthma are noted in 70–80% of children with asthma. It is known that loratadine has some bronchodilating effect in allergen-induced bronchoconstriction. The study evaluated the effect of loratadine on the severity of symptoms of exercise-induced asthma in children (n=11). Children took the study drug for 3 days, 10 mg 1 r / day. After the therapy, their FEV1 was measured, then the children started training on a treadmill, and FEV1 was measured again after 2; 5; 10 and 30 minutes after training. Loratadine significantly reduced FEV1 after exercise, while it did not prevent exercise-induced bronchoconstriction, but significantly reduced its severity (Baki A., Orhan F., 2001).

Antihistamines have an antitussive effect in patients with asthma, postnasal drip, and AR. Elevated histamine levels may contribute to persistent cough in these patients. In one study (n=28, of which 10 patients with rhinitis, 7 with chronic idiopathic cough and 11 healthy volunteers) studied the effect of loratadine on cough caused by irritation of cough receptors. To provoke a cough, distilled water was sprayed using an ultrasonic inhaler. Loratadine significantly reduced cough intensity in patients with postnasal drip and unexplained chronic cough, but not in healthy volunteers. At the same time, according to spirography, it did not affect lung function (Tanaka S. et al., 1996).

Loratadine in dermatology

Allergic reactions to insect stings, including itching, swelling and redness of the bite site, are a common problem. Loratadine is one of the drugs that effectively and safely relieves these symptoms in both adults and children (Foëx B.A., Lee C).

Most often, children suffer from itching and swelling at the site of a bite of blood-sucking insects. The effect of loratadine (0.3 mg/kg body weight) was studied in 28 children aged 2–11 years with allergy to mosquito bites. It was found that loratadine reduced the size of blisters that arose at the site of bites of laboratory Aedes aegypti mosquitoes by 45%. The intensity of concomitant itching (as determined by the visual analogue scale, VAS, 0-10 points) decreased by 78% already 15 minutes after taking loratadine. The drug was well tolerated, no adverse reactions were noted. These results allow loratadine to be recommended for symptom relief in children allergic to mosquito bites (Karppinen A. et al., 2000).

Another dermatological disease for which loratadine has been successfully used in symptomatic therapy is urticaria.

Urticaria is a heterogeneous skin disease that may be acute or chronic, intermittent or persistent. In addition, it can occur alone or in combination with other comorbidities such as angioedema. Urticaria is usually defined as the sudden appearance of pruritic papules on the skin with central swelling and surrounding erythema, which then resolve without scarring. The rash can appear on any part of the body and is often polymorphic. Isolated urticaria without angioedema occurs in about 40% of cases, while angioedema occurs simultaneously with urticaria in up to 40% of cases and, in fact, is the spread of the inflammatory process and edema into the deeper layers of the skin. Loratadine can be recommended both for symptomatic treatment of acute urticaria and for long-term use in chronic urticaria (Fine L.M., Bernstein J.A., 2016).

Potential uses for loratadine

Skin hyperpigmentation is a serious dermatological problem.

Various types of immune cells, including mast cells, are believed to play an important role in melanogenesis. Various inflammatory dermatoses can cause post-inflammatory hyperpigmentation by affecting the functional activity of melanocytes. In addition, inflammatory mediators such as histamine, prostaglandins, and nitric oxide play an important role. A study was conducted on the effectiveness of H 9 antagonists0076 1 receptors to determine if they inhibit melanogenesis. It was found that loratadine, without having a cytotoxic effect, was especially effective in this regard. Loratadine inhibits tyrosinase in melanocytes and reduces melanin content in melanocytes, regulates melanogenesis by inhibiting melanogenic proteins. The antimelanogenic effects of loratadine can potentially be applied in dermatological practice (Moon H.R. et al., 2019).

Another potential application for loratadine is oncology. The effect of radiotherapy varies depending on the phase of the cell cycle. In particular, cells in the G2/M phase are particularly sensitive to the effects of radiation. Found that in vitro loratadine inhibits the growth of tumor cells by increasing the proportion of cells in the G2/M phase of the cell cycle by altering the activity of regulatory proteins. Pre-treatment of colon cancer cells with loratadine increased radiation-induced cytotoxicity, thereby increasing the effectiveness of radiotherapy. In addition, DNA analysis revealed a pattern of DNA damage in cells treated with loratadine, in addition to that due to radiotherapy.