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Product Name
:
DE-HISTAMINE (syr)
Chemical Name
:
Loratadine
Therapeutic Category
:
Respiratory tract drugs
Pharmacologic Category
:
Histamine H1 - Antagonist - Histamine H1; Antagonist, Second Generation - Piperidine Derivative
Pharmaceutical Form
:
Syrup
Composition
:
Loratadine 5mg/5ml
Monitoring Parameters
Dosing
 
Dosing: Adult
Seasonal allergic rhinitis, chronic idiopathic urticaria: Oral: 10 mg/day

Dosing: Pediatric

Children 2-5 years: Seasonal allergic rhinitis, chronic idiopathic urticaria: Oral: 5 mg once daily
Children ≥6 years: Refer to adult dosing.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

Clcr ≤30 mL/minute:
Children 2-5 years: 5 mg every other day.
Children ≥6 years and Adults: 10 mg every other day.

Dosing: Hepatic Impairment

Elimination half-life increases with severity of disease.
Children 2-5 years: 5 mg every other day.
Children ≥6 years and Adults: 10 mg every other day.
Use
 
Relief of nasal and non-nasal symptoms of seasonal allergic rhinitis; treatment of chronic idiopathic urticaria
Adverse Reactions
 
Adults:
Central nervous system: Headache (12%), somnolence (8%), fatigue (4%)
Gastrointestinal: Xerostomia (3%)
Children:
Central nervous system: Nervousness (4% ages 6-12 years), fatigue (3% ages 6-12 years, 2% to 3% ages 2-5 years), malaise (2% ages 6-12 years)
Dermatologic: Rash (2% to 3% ages 2-5 years)
Gastrointestinal: Abdominal pain (2% ages 6-12 years), stomatitis (2% to 3% ages 2-5 years)
Neuromuscular & skeletal: Hyperkinesia (3% ages 6-12 years)
Ocular: Conjunctivitis (2% ages 6-12 years)
Respiratory: Wheezing (4% ages 6-12 years), dysphonia (2% ages 6-12 years), upper respiratory infection (2% ages 6-12 years), epistaxis (2% to 3% ages 2-5 years), pharyngitis (2% to 3% ages 2-5 years)
Miscellaneous: Flu-like syndrome (2% to 3% ages 2-5 years), viral infection (2% to 3% ages 2-5 years)
Adults and Children: <2% (Limited to important or life-threatening): Abnormal hepatic function, agitation, alopecia, altered lacrimation, altered micturition, altered salivation, altered taste, amnesia, anaphylaxis, angioneurotic edema, anorexia, arthralgia, back pain, blepharospasm, blurred vision, breast enlargement, breast pain, bronchospasm, chest pain, confusion, depression, dizziness, dysmenorrhea, dyspnea, erythema multiforme, hemoptysis, hepatic necrosis, hepatitis, hypotension, impaired concentration, impotence, insomnia, irritability, jaundice, menorrhagia, migraine, nausea, palpitation, paresthesia, paroniria, peripheral edema, photosensitivity, pruritus, purpura, rigors, seizure, supraventricular tachyarrhythmia, syncope, tachycardia, tremor, urinary discoloration, urticaria, thrombocytopenia, vaginitis, vertigo, vomiting, weight gain.
Contraindications
 
Hypersensitivity to loratadine or any component of the formulation
Warnings / Precautions Drug
 
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment recommended.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
Metabolism/Transport Effects
Substrate of CYP2D6 (minor), CYP3A4 (minor), P-glycoprotein; Inhibits CYP2C8 (weak), 2C19 (moderate), 2D6 (weak)
Interactions
 
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amiodarone: May increase the serum concentration of Loratadine. Management: Due to reported QT interval prolongation and Torsades de Pointes with this combination, consider an alternative to loratadine when possible. Risk D: Consider therapy modification
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (Low risk). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inhibitors: P-glycoprotein/ABCB1 Substrates may increase the serum concentration of P-glycoprotein/ABCB1 Inhibitors. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Pregnancy
 
Pregnancy Implications
Maternal use of loratadine has not been associated with an increased risk of major malformations. The use of antihistamines for the treatment of rhinitis during pregnancy is generally considered to be safe at recommended doses. Although safety data is limited, loratadine may be the preferred second generation antihistamine for the treatment of rhinitis or urticaria during pregnancy.
Lactation
 
Breast-Feeding Considerations
Small amounts of loratadine and its active metabolite, desloratadine, are excreted into breast milk.
Mechanism of Action
 
Long-acting tricyclic antihistamine with selective peripheral histamine H1-receptor antagonistic properties
Pharmacodynamics / Kinetics
 
Onset of action: 1-3 hours
Peak effect: 8-12 hours
Duration: >24 hours
Absorption: Rapid
Metabolism: Extensively hepatic via CYP2D6 and 3A4 to active metabolite
Half-life elimination: 12-15 hours
Excretion: Urine (40%) and feces (40%) as metabolites
 
   
 
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