Desloratadine (Clarinex) - Uses, Dose, Side effects, MOA, Brands

Desloratadine is a second-generation antihistamine medication used primarily to treat allergies. It's commonly sold under the brand name Clarinex. Desloratadine works by blocking the action of histamine, a substance in the body that causes allergic symptoms like itching, sneezing, runny nose, and watery eyes.

As a non-sedating antihistamine, desloratadine generally causes less drowsiness compared to first-generation antihistamines like diphenhydramine (Benadryl). It's often used to alleviate symptoms associated with allergic rhinitis (hay fever) and chronic idiopathic urticaria (hives).

Desloratadine (Clarinex) is the active metabolite of loratadine that selectively blocks the histamine (H-1) receptors. It is used for the symptomatic treatment of allergic symptoms associated with allergic rhinitis and chronic idiopathic urticaria.

Desloratadine Uses:

  • Allergic rhinitis:
    • It is indicated for the symptomatic treatment of nasal and non-nasal symptoms of seasonal (SAR) and perennial (PAR) allergic rhinitis.
  • Urticaria:
    • It is used for the symptomatic treatment of pruritus and for the reduction in the number and size of hives associated with chronic idiopathic urticaria (CIU)
  • Off Label Use in Adults:
    • It may be used as a prophylactic treatment of NSAID-associated urticaria.

Desloratadine (Clarinex) Dose in Adults

Desloratadine (Clarinex) Dose in the treatment of chronic idiopathic urticaria:

  • For treating Chronic Idiopathic Urticaria, the usual dose of Desloratadine is 5 milligrams once a day.
  • However, in some cases, doctors may increase the dose to 10 milligrams twice a day, based on a study where this higher dose showed improvement in adults.

Desloratadine (Clarinex) Dose in the treatment of Seasonal or perennial allergic rhinitis:

  • For Seasonal or perennial allergic rhinitis, the typical dose of Desloratadine is 5 milligrams taken orally once a day.

Desloratadine (Clarinex) Dose in the prophylaxis of NSAID-associated urticaria (off-label):

  • In the prevention of NSAID-associated urticaria, which is not an officially approved use of Desloratadine, a typical dose is 5 milligrams taken orally about 30 minutes before consuming a strong COX-1 inhibitor.

Desloratadine (Clarinex) Dose in Childrens

Desloratadine (Clarinex) Dose in the treatment of Perennial allergic rhinitis: Oral:

  • Infants aged 6 months to 11 months: 1 milligram once daily
  • Children aged 1 year to 5 years: 1.25 milligrams once daily
  • Children aged 6 years to 11 years: 2.5 milligrams once daily
  • Children aged 12 years and older, including adolescents: 5 milligrams once daily

Desloratadine (Clarinex) Dose in the treatment of Seasonal allergic rhinitis: Oral:

  • Children aged 2 years to 5 years: 1.25 milligrams once daily
  • Children aged 6 years to 11 years: 2.5 milligrams once daily
  • Children aged 12 years and older, including adolescents: 5 milligrams once daily

Desloratadine (Clarinex) Dose in the treatment of chronic idiopathic Urticaria: Oral:

  • Infants aged 6 months to 11 months: 1 milligram once daily
  • Children aged 1 year to 5 years: 1.25 milligrams once daily
  • Children aged 6 years to 11 years: 2.5 milligrams once daily
  • Children aged 12 years and older, including adolescents: 5 milligrams once daily

 

   Pregnancy Risk Factor C

  • During pregnancy, it's generally recommended to follow similar guidelines for using antihistamines to treat allergic rhinitis or urticaria as for non-pregnant individuals.
  • Second-generation antihistamines, including desloratadine, can be considered for managing these conditions, but there's limited information available specifically about desloratadine use during pregnancy.

Use during breastfeeding:

  • Desloratadine has been found to be present in breast milk.
  • The manufacturer advises that when deciding whether to continue or discontinue breastfeeding while taking desloratadine, it's important to consider the potential risk of exposure to the infant as well as the benefits of the treatment to the mother.
  • It's worth noting that desloratadine is the main metabolite of loratadine.
  • For further details, additional information can be found in the loratadine monograph.

Dose in Kidney Disease:

  • For individuals with mild to severe renal impairment, the recommended dosage of Desloratadine is 5 milligrams taken every other day.
  • This adjusted dosing schedule is necessary to accommodate the reduced kidney function and prevent potential accumulation of the medication in the body.

Dose in Liver disease:

  • For individuals with mild to severe hepatic (liver) impairment, the recommended dosage of Desloratadine is 5 milligrams taken every other day.
  • Adjusting the dosage in this manner helps to account for the decreased liver function and reduces the risk of potential side effects or medication accumulation.

Common Side Effects of Desloratadine (Clarinex):

  • Central Nervous System:
    • Headache
    • Irritability
  • Gastrointestinal:
    • Diarrhea
  • Respiratory:
    • Upper Respiratory Tract Infection
    • Cough
  • Miscellaneous:
    • Fever

Less Common Side Effects Of Desloratadine (Clarinex):

  • Central Nervous System:
    • Drowsiness
    • Insomnia
    • Fatigue
    • Dizziness
    • Emotional Lability
  • Dermatologic:
    • Erythema Of Skin
    • Maculopapular Rash
  • Gastrointestinal:
    • Vomiting
    • Anorexia
    • Nausea
    • Dyspepsia
    • Increased Appetite
    • Xerostomia
  • Genitourinary:
    • Urinary Tract Infection
  • Infection:
    • Varicella Zoster Infection
    • Parasitic Infection
  • Neuromuscular & Skeletal:
    • Myalgia
  • Otic:
    • Otitis Media
  • Respiratory:
    • Bronchitis
    • Rhinorrhea
    • Pharyngitis
    • Epistaxis

Contraindications to Desloratadine (Clarinex):

Individuals with a hypersensitivity (allergic reaction) to desloratadine, loratadine, or any component of the formulation should avoid using Desloratadine.

Warnings and precautions

Hypersensitivity

  • Hypersensitivity reactions, including severe allergic reactions like anaphylaxis, have been reported with the use of Desloratadine.
  • If any signs or symptoms of hypersensitivity occur during treatment, it is important to discontinue therapy immediately and seek medical attention.
  • These signs may include rash, itching, swelling, dizziness, difficulty breathing, or any other unusual symptoms.
  • Prompt action is necessary to address potential allergic reactions and ensure the individual's safety.

Hepatic impairment

  • Desloratadine should be used with caution in patients with hepatic (liver) impairment, and dosage adjustment may be necessary.
  • Individuals with liver problems may metabolize the medication differently, leading to potential accumulation of the drug in the body.

Renal impairment

  • Desloratadine should be used cautiously in patients with renal (kidney) impairment, and dosage adjustment may be necessary.
  • Individuals with kidney problems may clear the medication from their bodies at a different rate, potentially leading to higher levels of the drug in the bloodstream.

Desloratadine: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

 

Alcohol (Ethyl)

CNS Depressants can increase the CNS depressant effects of Alcohol (Ethyl).

Alizapride

CNS Depressants may increase the CNS depressant effects.

Amezinium

Amezinium may have a stronger stimulatory effect if it is combined with antihistamines.

Amphetamines

May decrease the sedative effects of Antihistamines.

Betahistine

Betahistine's therapeutic effects may be diminished by antihistamines.

Brexanolone

CNS Depressants can increase the CNS depressant effects of Brexanolone.

Brimonidine (Topical)

CNS Depressants may increase the CNS depressant effects.

Bromopride

CNS Depressants may increase the CNS depressant effects.

Cannabidiol

CNS Depressants may increase the CNS depressant effects.

Cannabis

CNS Depressants may increase the CNS depressant effects.

Chlorphenesin Carbamate

CNS Depressants may have an adverse/toxic effect that can be exacerbated by them.

CNS Depressants

Can increase the toxic/adverse effects of CNS Depressants.

Moderate CYP2C8 inhibitors

Might increase serum Desloratadine concentrations.

Strong CYP2C8 inhibitors

Might increase serum Desloratadine concentrations.

Dimethindene (Topical).

CNS Depressants may increase the CNS depressant effects.

Doxylamine

CNS Depressants may have a greater CNS depressant effect if taken with other CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended.

Dronabinol

CNS Depressants may increase the CNS depressant effects.

Erdafitinib

Increased serum concentrations of P-glycoprotein/ABCB1 Substrates may be possible.

Esketamine

CNS Depressants may increase the CNS depressant effects.

HydrOXYzine

CNS Depressants may increase the CNS depressant effects.

Kava Kava

CNS Depressants may have an adverse/toxic effect that can be exacerbated by them.

Lofexidine

CNS Depressants may have a greater depressant effect on the brain. Management: Separate drug interaction monographs are available for drugs listed as an exception to this monograph.

Lumacaftor

May lower the serum concentrations of P-glycoprotein/ABCB1 Substrates. Lumacaftor could increase serum levels of P-glycoprotein/ABCB1 Substrates.

Magnesium Sulfate

CNS Depressants may increase the CNS depressant effects.

MetyroSINE

MetyroSINE may have a sedative effect that can be enhanced by CNS depressants.

Minocycline

CNS Depressants may increase the CNS depressant effects.

Mirtazapine

CNS Depressants can increase the CNS depressant effects of Mirtazapine.

Nabilone

CNS Depressants may increase the CNS depressant effects.

P-glycoprotein/ABCB1 Inducers

The serum concentrations of Pglycoprotein/ABCB1 Substrates may be decreased. Inducers of pglycoprotein may limit the distribution to certain cells/tissues/organs in which p-glycoprotein exists in high amounts (e.g. brain, testes and T-lymphocytes). .

P-glycoprotein/ABCB1 Inhibitors

Increases serum concentrations of Pglycoprotein/ABCB1 substrates. P-glycoprotein inhibitors can also increase the distribution of pglycoprotein substrates to certain cells/tissues/organs in which p-glycoprotein exists in high amounts (e.g. brain, T-lymphocytes and testes). .

Piribedil

CNS Depressants could increase the CNS depressant effects of Piribedil.

Pitolisant

Pitolisant's therapeutic effects may be diminished by antihistamines.

Pramipexole

Pramipexole may have a greater sedative effect if it is combined with CNS depressants.

Ranolazine

Increased serum concentrations of P-glycoprotein/ABCB1 Substrates may be possible.

ROPINIRole

CNS Depressants can increase the sedative effects of ROPINIRole.

Rotigotine

CNS Depressants can increase the sedative effects of Rotigotine.

Rufinamide

CNS Depressants may have an adverse/toxic effect that can be exacerbated by this. Particularly, dizziness and sleepiness may be increased.

Selective Serotonin Reuptake inhibitors

CNS Depressants can increase the toxic/adverse effects of Selective Serotonin Resuptake Inhibitors. Particularly, psychomotor impairment could be increased.

Tetrahydrocannabinol

CNS Depressants may increase the CNS depressant effects.

Tetrahydrocannabinol, and Cannabidiol

CNS Depressants may increase the CNS depressant effects.

Trimeprazine

CNS Depressants may increase the CNS depressant effects.

Risk Factor D (Consider therapy modifications)

Benzylpenicilloyl polylysine

Antihistamines can reduce the diagnostic effectiveness of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. To assess for persistent antihistaminic effects, a histamine skin test can be performed.

Blonanserin

CNS Depressants can increase the CNS depressant effects of Blonanserin.

Buprenorphine

CNS Depressants can increase the CNS depressant effects of buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Buprenorphine patches (Butrans) should be initiated at 5 mg/hr for adults. This is when it is combined with other CNS depression drugs.

Chlormethiazole

CNS Depressants may increase the CNS depressant effects. Monitoring: Look out for signs of CNS depression. If a combination of chlormethiazole and other drugs is required, a reduced dose should be used.

Droperidol

CNS Depressants may increase the CNS depressant effects. Management: Droperidol and other CNS agents, such as opioids, may be reduced or used in combination with droperidol. Separate drug interaction monographs provide more detail on exceptions to this monograph.

Flunitrazepam

CNS Depressants can increase the CNS depressant effects of Flunitrazepam.

Hyaluronidase

Hyaluronidase's therapeutic effects may be diminished by antihistamines. Management: Patients who are taking antihistamines, especially at higher doses, may not have the desired clinical response to standard doses hyaluronidase. Higher doses of hyaluronidase might be necessary.

HYDROcodone

CNS Depressants can increase the CNS depressant effects of HYDROcodone. When possible, avoid concomitant use with hydrocodone and other CNS depressants. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

Methotrimeprazine

Methotrimeprazine may have a higher CNS depressant activity than CNS Depressants. Methotrimeprazine can increase the CNS depressant effects of CNS Depressants. Management: Lower the adult dose of CNS Depressants by 50% and start concomitant methotrimeprazine treatment. After clinically proven efficacy of methotrimeprazine, further CNS depressant dose adjustments should only be made.

Opioid Agonists

CNS Depressants can increase the CNS depressant effects of Opioid Aggonists. Management: When possible, avoid concomitant use opioid agonists, benzodiazepines, or other CNS depressionants. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

OxyCODONE

CNS Depressants can increase OxyCODONE's CNS depressant effects. When possible, avoid the simultaneous use of oxycodone and other CNS depressants. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

Perampanel

CNS Depressants may have a greater CNS depressant effect. Perampanel and any other CNS depressant drug should be used in combination. Patients who take perampanel together with other drugs that have CNS depressant activity should not engage in complex or high-risk activities until they are familiar with the combination.

Sodium Oxybate

CNS Depressants may have a greater depressant effect if taken in combination. Management: Look for alternatives to the combination use. If you must combine use, reduce the doses of any one or more drugs. It is not recommended to combine sodium oxybate and alcohol, or any sedative hypnotics.

Suvorexant

CNS Depressants can increase the CNS depressant effects of Suvorexant. Management: Suvorexant or any other CNS depressionant can be reduced in doses. Suvorexant should not be taken with alcohol. It is also not recommended to take suvorexant along with any other drugs for insomnia.

Tapentadol

CNS Depressants may increase the CNS depressant effects. Tapentadol, benzodiazepines and other CNS depressants should be avoided when possible. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

Zolpidem

CNS Depressants can increase the CNS depressant effects of Zolpidem. Management: For men who also take CNS depressants, reduce the adult Intermezzo brand sublingual Zolpidem dose to 1.75mg. For women, no dose adjustment is advised. Avoid using CNS depressants at night; do not use alcohol.

Risk Factor X (Avoid Combination)

Azelastine (Nasal)

CNS Depressants could increase the CNS depressant effects of Azelastine.

Bromperidol

CNS Depressants may increase the CNS depressant effects.

Orphenadrine

Orphenadrine may be more effective against CNS depression than other drugs.

Oxomemazine

CNS Depressants may increase the CNS depressant effects.

Paraldehyde

Paraldehyde may be enhanced by CNS depressants.

Thalidomide

CNS Depressants can increase Thalidomide's CNS depressant effects.

     

Monitoring Parameters:

None mentioned.   

How to administer Desloratadine (Clarinex)?

  • With or Without Food: Desloratadine can be taken with or without food.
  • RediTabs Instructions:
    • Placement: Place the RediTabs on your tongue.
    • Disintegration: The tablet will dissolve immediately.
    • Timing: Take it right after removing it from the blister package.
    • Complete Dissolution: Allow the tablet to dissolve completely before swallowing.
    • Water Usage: You may take it with or without water.

Mechanism of action of Desloratadine (Clarinex):

  • Desloratadine is a significant active compound derived from loratadine.
  • It belongs to the class of long-acting tricyclic antihistamines, which work by blocking specific histamine receptors in the body.
  • Desloratadine has a particular affinity for peripheral histamine H receptors, which are involved in allergic reactions.
  • By antagonizing these receptors, desloratadine helps to alleviate symptoms associated with allergies, such as itching, sneezing, runny nose, and watery eyes.

Onset of Action:

  • Desloratadine typically starts working within 1 hour after ingestion.

Duration:

  • Its effects can last for up to 24 hours.

Protein Binding:

  • Desloratadine and its active metabolite, 3-hydroxydesloratadine, are highly bound to proteins in the blood, with percentages ranging from 82% to 89%.

Metabolism:

  • Desloratadine is primarily metabolized in the liver to its active form, 3-hydroxydesloratadine.
  • Specific enzymes responsible for this process have not been identified.
  • Afterwards, it undergoes glucuronidation.
  • The metabolism may be reduced in individuals who are slow metabolizers of desloratadine.
  • The medication's metabolism is not expected to affect or be affected by drugs metabolized by typical liver enzymes (CYP enzymes) at normal doses.

Half-life:

  • The elimination half-life of desloratadine is approximately 27 hours.

Time to Peak:

  • It reaches peak plasma concentration about 3 hours after administration.

Excretion:

  • Desloratadine and its metabolites are primarily excreted in the urine (87%) and feces.

International Brand Names of Desloratadine:

  • Clarinex
  • Aeriallerg
  • Aerius
  • Aler Free
  • Alergaway
  • Aleros
  • Alersis
  • Allergostop
  • Allora
  • Aloret
  • Apitus
  • Aviant
  • Azomyr
  • Brevy
  • Campos
  • Claramax
  • Dasselta
  • Deline
  • Delopa
  • Delorat
  • Denosin 5
  • Desa
  • Desalex
  • Desarius
  • Desatrol
  • Deschu
  • Desdin
  • Deslatyne
  • Desloderma 5
  • Deslodine
  • Deslogen
  • Deslor
  • Deslora
  • Desloran
  • Deslorastal
  • Deslotine
  • Desora
  • Desorus
  • Despej
  • Destina
  • Edem
  • Efestad
  • Eridez
  • Eslorat
  • Flynise
  • Histacare
  • Iris
  • Larinex
  • Letizia
  • Lomid
  • Loralergan
  • Lorax
  • Lorius
  • Mailen
  • Neo-Loridin
  • Neoclaritine
  • Neoclarityn
  • Rina
  • Rinofil
  • Ruradin
  • Sedno
  • Sednox
  • Supraler

Desloratadine Brand Names in Pakistan:

Desloratadine Syrup 0.5 mg/ml in Pakistan

Delergia

Pharmevo (Pvt) Ltd.

Neo-Antial

Sami Pharmaceuticals (Pvt) Ltd.

Desloratadine Syrup 0.5 mg/5ml in Pakistan

Desora

S.J. & G. Fazul Ellahie (Pvt) Ltd.

Desora

S.J. & G. Fazul Ellahie (Pvt) Ltd.

Desloratadine Syrup 2.5 mg/5ml in Pakistan

Alenor

Macter International (Pvt) Ltd.

Allorx

Raazee Theraputics (Pvt) Ltd.

Deslet

Efroze Chemical Industries (Pvt) Ltd.

Slorit

Hiranis Pharmaceuticals Pvt Ltd

Desloratadine Tablets 5 mg in Pakistan

Alenor

Macter International (Pvt) Ltd.

Alenor Reditab

Macter International (Pvt) Ltd.

Alerfass

Fassgen Pharmaceuticals

Aloret

Pharma Health Pakistan (Pvt) Ltd

Atmos

Scotmann Pharmaceuticals

D-Lor

Everest Pharmaceuticals

D-Loraata

Weather Folds Pharmaceuticals

Dastak

Shrooq Pharmaceuticals

Descover

Kinsa Pharmaceuticals

Desgen

Envoy Pharma

Desgood

Goodman Laboratories

Deslo

Neutro Pharma (Pvt) Ltd.

Desloradvan

Advanced Pharmaceuticals

Desloreal

Wns Field Pharmaceuticals

Deslort

Panacea Pharmaceuticals

Desmak

Makson Pharmaceuticals

Desoline

Candid Pharmaceuticals

Desora

S.J. & G. Fazul Ellahie (Pvt) Ltd.

Destazine

Sante (Pvt) Limited

Destidine

Wellborne Pharmachem And Biologicals

Destina

Hilton Pharma (Pvt) Limited

Destra

Zephyr Pharmatec (Pvt) Ltd.

Destrex

Wns Field Pharmaceuticals

Dictrin

Barrett Hodgson Pakistan (Pvt) Ltd.

Disdine

Wisdom Therapeutics

Dulin

Genome Pharmaceuticals (Pvt) Ltd

E-Din

English Pharmaceuticals Industries

Histanil D

Wilshire Laboratories (Pvt) Ltd.

Histanil D

Wilshire Laboratories (Pvt) Ltd.

Larinex

Getz Pharma Pakistan (Pvt) Ltd.

Loratolive

Olive Pharmaceuticals

Lotodine

Lotus Pharmaceuticals (Pvt) Ltd

Neo-Antial

Sami Pharmaceuticals (Pvt) Ltd.

Novak

Rogen Pharmaceuticals

Reetag

Tagma Pharma (Pvt) Ltd.

Retoret

Pharma Health Pakistan (Pvt) Ltd

Rinex

Jawa Pharmaceuticals(Pvt) Ltd.

Slorit

Hiranis Pharmaceuticals Pvt Ltd

Desloratadine Tablets 10 mg in Pakistan

Atmos

Scotmann Pharmaceuticals

Desloratadine Tablets 2.5 mg in Pakistan

Alenor Reditab

Macter International (Pvt) Ltd.

Desloratadine Capsules 5 mg in Pakistan

Slorate

Neutro Pharma (Pvt) Ltd.