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

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:

  • 5 mg orally once a day.

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

  • 5 mg orally once a day.

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

  • 5 mg administered orally 30 minutes before a strong COX-1 inhibitor.

Desloratadine (Clarinex) Dose in Childrens

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

  • Infants 6 months to 11 months:
    • 1 mg once daily
  • Children 1 year to 5 years:
    • 2.5 mg once a day.
  • Children 6 years to 11 years:
    • 5 mg once a day.
  • Children ≥12 years and Adolescents:
    • 5 mg once a day.

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

  • Children 2 years to 5 years:
    • 2.5 mg once a day.
  • Children 6 years to 11 years:
    • 5 mg once a day.
  • Children ≥12 years and Adolescents:
    • 5 mg once a day.

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

  • Infants 6 months to 11 months:
    • 1 mg once a day
  • Children 1 year to 5 years:
    • 2.5 mg once a day.
  • Children 6 years to 11 years:
    • 5 mg once a day.
  • Children ≥12 years and Adolescents:
    • 5 mg once a day.

   Pregnancy Risk Factor C

  • Its use in pregnancy is not well documented. 
  • It is recommended that it be used in both pregnant and not-pregnant women.
  • For the treatment of allergic rhinitis, urticaria, or other symptoms, second-generation antihistamines are safe to use during pregnancy.

Use during breastfeeding:

  • Breast milk contains desloratadine. 
  • Manufacturers recommend weighing the benefits and risks to the mother of being exposed to drugs in her infant.
  • For more information, see loratadine.

Dose in Kidney Disease:

  • Mild to severe impairment:
    • 5 mg on alternate days.

Dose in Liver disease:

  • Mild to severe impairment:
    • 5 mg on alternate days.

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):

Allergic reactions to desloratadine, loratadine, or any component of the formulation.

Warnings and precautions

  • Hypersensitivity
    • Anaphylaxis can occur in patients with allergic reactions. If you notice signs of an allergic reaction, stop taking any medication immediately.
  • Hepatic impairment
    • Patients with impaired liver function should be cautious when using the drug. Dosage adjustments may be necessary.
  • Renal impairment
    • Patients with impaired renal function should be cautious when using the drug. A dosage adjustment may also be necessary.

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)?

  • It can be taken with or without meals.
  • RediTabs formulation disintegrates when they are kept over the tongue.
  • It should be immediately kept on the tongue when taken from the blister package.
  • After the tablet dissolves completely, it may be swallowed with or without a cup of water.   

Mechanism of action of Desloratadine (Clarinex):

It is a tricyclic, long-acting antihistamine. It selectively blocks the H1 receptors of peripheral histamines.

Start of action:

  • Within one hour

Time:

  • 24 hours

Protein binding:

  • Desloratadine: 82% to 87%;
  • 3-hydroxydesloratadine (active metabolite): 85% to 89%

Metabolism:

  • It is metabolized in the liver to the active metabolite, 3-hydroxydesloratadine (specific enzymes not identified) that subsequently undergoes glucuronidation.
  • The metabolism of the drug is reduced in individuals who are slow metabolizers of the drug.
  • When administered in normal doses, drugs that affect CYP enzymes have little effect on the metabolism of desloratadine.

Half-life elimination:

  • 27 hours

Time to peak:

  • 3 hours

Excretion:

  • 87% is excreted in the urine as metabolites.
  • feces as metabolites.

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.

Comments

NO Comments Found