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(Para obtener información adicional, consulte "Loratadina: información sobre el medicamento para el paciente" y consulte "Loratadina: información sobre el
medicamento pediátrico" )
Para consultar las definiciones de abreviaturas, símbolos y grupos de edad utilizados en Lexicomp ( mostrar tabla )
Categoría farmacológica
antagonista de histamina H1 ;
antagonista de histamina H1 , segunda generación;
Derivado de piperidina
Posología: Adulto
Collapse All
Rinitis alérgica o conjuntivitis: Oral: 10 mg una vez al día o 5 mg dos veces al día.
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Etiquetado OTC
(terapia guiada por el paciente para los síntomas de la fiebre del heno u otras alergias de las vías respiratorias
superiores): Oral: 10 mg una vez al día o 5 mg dos veces al día; dosis máxima: 10 mg/día.
Nuevo inicio: Oral: Inicial: 10 mg una vez al día. Si el control de los síntomas es inadecuado, puede aumentar
inmediatamente a 10 mg dos veces al día (Asero 2021).
Espontáneo crónico: Oral: Inicial: 10 mg una vez al día. Si el control de los síntomas es inadecuado después de 1 a 4
semanas, se puede aumentar a 10 mg dos veces al día. Aunque las pautas actuales establecen que las dosis de
antihistamínicos pueden aumentarse hasta 4 veces la dosis estándar (p. ej., a 20 mg dos veces al día), existe evidencia
limitada de una mayor eficacia con esta dosis de loratadina y se prefieren otros antihistamínicos. Reevaluar periódicamente la
necesidad de continuar el tratamiento (EAACI [Zuberbier 2018]; Khan 2021).
Nota: Las recomendaciones de dosis ajustadas por riñón se basan en una dosis habitual de 10 mg/día.
Oral:
CrCl ≥30 ml/minuto: No es necesario ajustar la dosis (Matzke 1990; etiqueta del fabricante).
CrCl <30 ml/minuto: 10 mg cada 48 horas (Matzke 1990; opinión de expertos; etiquetado del fabricante).
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Hemodiálisis, intermitente (tres veces por semana): No dializable (Matzke 1990): Oral: 10 mg cada 48 horas (Matzke 1990;
opinión de expertos).
Diálisis peritoneal: Es improbable que sea significativamente dializable (V d grande , alta unión a proteínas): Oral: 10 mg cada 48
horas (opinión de un experto).
TRRC:
Note: Drug clearance is dependent on the effluent flow rate, filter type, and method of renal replacement. Recommendations
are based on high-flux dialyzers and effluent flow rates of 20 to 25 mL/kg/hour (or ~1,500 to 3,000 mL/hour) unless otherwise
noted.
Note: Drug clearance is dependent on the effluent flow rate, filter type, and method of renal replacement.
Dosing: Pediatric
General dosing:
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Product-specific dosing:
Children ≥2 to <6 years: Oral: Oral liquid or chewable tablet: 5 mg once daily.
Urticaria, chronic spontaneous (idiopathic): Limited data available (Kliegman 2020; Pozzo-Magaña 2017): Note: Considered first-
line therapy for management of chronic urticaria; if response inadequate after 2 to 4 weeks of therapy or symptoms intolerable,
consider increasing the dose of loratadine (as age and weight permits) as second-line treatment rather than changing therapy
(Zuberbier 2018).
There are no dosage adjustments provided in manufacturer's labeling, however, the following recommendations have been
recommended (Aronoff 2007):
Children ≥2 years and Adolescents: No dosage adjustment necessary for any degree of renal impairment.
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Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] =
Discontinued product
Capsule, Oral:
GoodSense Allergy Relief: 10 mg [contains brilliant blue fcf (fd&c blue #1)]
Generic: 10 mg
Solution, Oral:
Childrens Loratadine: 5 mg/5 mL (120 mL) [alcohol free, dye free, sugar free; contains propylene glycol, sodium benzoate; grape
flavor]
Loratadine Childrens: 5 mg/5 mL (120 mL [DSC]) [alcohol free, dye free, sugar free; contains polyethylene glycol (macrogol),
propylene glycol, sodium benzoate]
Syrup, Oral:
Childrens Loratadine: 5 mg/5 mL (120 mL) [alcohol free, dye free; contains propylene glycol, sodium benzoate, sodium
metabisulfite; grape flavor]
Claritin Allergy Childrens: 5 mg/5 mL (240 mL) [alcohol free, dye free, sugar free; contains edetate (edta) disodium, propylene
glycol, sodium benzoate, sorbitol]
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Loratadine Childrens: 5 mg/5 mL (120 mL) [alcohol free, dye free, gluten free, sugar free; contains edetate (edta) disodium,
propylene glycol, sodium benzoate; grape flavor]
Loratadine Childrens: 5 mg/5 mL (120 mL, 240 mL) [alcohol free, dye free, sugar free; contains edetate (edta) disodium
dihydrate, propylene glycol, sodium benzoate; grape flavor]
Loratadine Childrens: 5 mg/5 mL (10 mL) [alcohol free, dye free, sugar free; contains propylene glycol, sodium benzoate; grape
flavor]
Loratadine Childrens: 5 mg/5 mL (120 mL) [sugar free; contains polyethylene glycol (macrogol), propylene glycol, sodium
benzoate, sodium metabisulfite; grape flavor]
Tablet, Oral:
Allergy: 10 mg [DSC]
Allergy Relief: 10 mg
Claritin: 10 mg
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Loradamed: 10 mg
Generic: 10 mg
Triaminic Allerchews: 10 mg
Generic: 10 mg
Administration: Adult
May be administered without regard to meals.
Dispersible tablet: Place in mouth and allow to dissolve. Swallow with or without water.
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Administration: Pediatric
Oral: Administer without regard to meals.
Rapidly disintegrating tablet: Place rapidly disintegrating tablet on the tongue; tablet disintegration occurs rapidly; may administer
with or without water.
Allergic rhinitis or conjunctivitis: Relief of nasal and non-nasal symptoms of seasonal allergies.
OTC labeling: Patient-guided therapy for symptoms of hay fever or other upper respiratory allergies.
Urticaria, new onset and chronic spontaneous: Treatment of itching due to hives (urticaria).
Adverse Reactions
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions
reported in adults and pediatric patients unless otherwise indicated.
1% to 10%:
Cardiovascular: Chest pain (<2%), flushing (<2%), hypertension (<2%), hypotension (<2%), palpitations (<2%), supraventricular
tachycardia (<2%), syncope (<2%), tachycardia (<2%)
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Dermatologic: Dermatitis (<2%), diaphoresis (<2%), dry hair (<2%), pruritus (<2%), skin photosensitivity (<2%), skin rash (children:
2% to 3%), xeroderma (<2%)
Endocrine & metabolic: Decreased libido (<2%), heavy menstrual bleeding (<2%), increased thirst (<2%), weight gain (<2%)
Gastrointestinal: Abdominal pain (children: 2%), altered salivation (<2%), anorexia (<2%), constipation (<2%), diarrhea (children:
2% to 3%), dysgeusia (<2%), dyspepsia (<2%), flatulence (<2%), gastritis (<2%), hiccups (<2%), increased appetite (<2%), loose
stools (<2%), nausea (<2%), stomatitis (children: 2% to 3%), vomiting (<2%), xerostomia (adolescents and adults: 3%)
Genitourinary: Altered micturition (<2%), dysmenorrhea (<2%), impotence (<2%), mastalgia (<2%), urinary incontinence (<2%),
urinary retention (<2%), urine discoloration (<2%), vaginitis (<2%)
Nervous system: Agitation (<2%), amnesia (<2%), anxiety (<2%), confusion (<2%), depression (<2%), dizziness (<2%), drowsiness
(adolescents and adults: 8%), fatigue (2% to 4%), hypertonia (<2%), hypoesthesia (<2%), insomnia (<2%), irritability (<2%), lack of
concentration (<2%), malaise (children: 2%), migraine (<2%), nervousness (children: 4%), nightmares (<2%), paresthesia (<2%),
rigors (<2%), vertigo (<2%), voice disorder (children: 2%)
Neuromuscular & skeletal: Arthralgia (<2%), asthenia (<2%), back pain (<2%), hyperkinetic muscle activity (children: 3%), lower
limb cramp (<2%), myalgia (<2%), tremor (<2%)
Ophthalmic: Blepharospasm (<2%), blurred vision (<2%), conjunctivitis (children: 2%), eye pain (<2%)
Respiratory: Bronchitis (<2%), bronchospasm (<2%), cough (<2%), dry nose (<2%), dyspnea (<2%), epistaxis (children: 2% to 3%),
flu-like symptoms (children: 2% to 3%), hemoptysis (<2%), laryngitis (<2%), pharyngitis (children: 2% to 3%), upper respiratory
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Postmarketing:
Hypersensitivity: Anaphylaxis
Contraindications
Hypersensitivity to loratadine or any component of the formulation
Warnings/Precautions
Disease-related concerns:
• Hepatic impairment: Hepatic impairment increases systemic exposure. Use with caution.
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
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• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a
metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal
toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping
respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP
["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001);
avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer’s labeling.
Metabolism/Transport Effects
Substrate of CYP2D6 (minor), CYP3A4 (minor), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based
on clinically relevant drug interaction potential
Drug Interactions
(For additional information: Launch drug interactions program)
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4
Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management
recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
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Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish
the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy
Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Amezinium: Antihistamines may enhance the stimulatory effect of Amezinium. 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. If concomitant use cannot be
avoided, monitor QT interval and for signs of dyshythmias (eg, syncope). Risk D: Consider therapy modification
Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy
Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
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: May diminish the therapeutic effect of Antihistamines. Antihistamines may diminish the therapeutic effect of
Betahistine. Risk C: Monitor therapy
Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering
blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not
be coadministered with blonanserin. Risk D: Consider therapy modification
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Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses
of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate
buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products.
Risk C: Monitor therapy
Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products.
Risk C: Monitor therapy
Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy
Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of
excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a
combination must be used. Risk D: Consider therapy modification
Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy
Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination
CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this
combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider
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CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or
any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant
with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification
DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for
increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of
either agent to avoid excessive CNS depression. Risk D: Consider therapy modification
Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Doxylamine: May enhance the CNS depressant effect of 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. 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 (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination
Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination
Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS
depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory
depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification
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Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents
(Prokinetic). Risk C: Monitor therapy
Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse
effects may be increased. Risk C: Monitor therapy
Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation).
Risk X: Avoid combination
Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Risk C: Monitor therapy
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS
depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression
in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification
Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy
Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Ketoconazole (Systemic): May increase the serum concentration of Loratadine. Risk C: Monitor therapy
Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and
of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant
effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification
Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination
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Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may
enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting
methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D:
Consider therapy modification
Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy
Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy
Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease
the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy
Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use
of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if
alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy
modification
Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination
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Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider
alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants
(including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D:
Consider therapy modification
OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of
oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative
treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification
Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination
Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy
Pitolisant: Antihistamines may diminish the therapeutic effect of Pitolisant. Risk X: Avoid combination
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on
drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid
combination
Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Risk X: Avoid combination
Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid
combination
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Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy
Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination
Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of
neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS
depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal
ideation, aggression, mania). Risk D: Consider therapy modification
ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy
Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy
Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk
C: Monitor therapy
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of
anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D:
Consider therapy modification
Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant
and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant
with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination
Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like
Diuretics. Risk C: Monitor therapy
Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination
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Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand
sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is
recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy
modification
Food Interactions
Food increases bioavailability and delays peak. Management: Administer without regard to meals.
Pregnancy Considerations
Guidelines for the use of antihistamines in the treatment of allergic rhinitis or urticaria in pregnancy are generally the same as in
nonpregnant females. Loratadine may be used when a second generation antihistamine is needed. The lowest effective dose should be
used (BSACI [Powell 2015]; BSACI [Scadding 2017]; Zuberbier 2018).
Breastfeeding Considerations
Loratadine and its active metabolite, desloratadine, are present in breast milk.
The relative infant dose (RID) of loratadine plus desloratadine has been calculated to be 1.1% when compared to a maternal dose of 40
mg/day of loratadine (Hilbert 1988).
In general, breastfeeding is considered acceptable when the RID is <10% (Anderson 2016; Ito 2000).
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The RID was calculated by the authors of a study following maternal administration of a single oral dose of loratadine 40 mg to six
breastfeeding women between 1 and 12 months' postpartum. The estimated daily infant dose of loratadine equivalents via breast milk
was calculated to be 29.1 mcg/day in a theoretical 4 kg infant. The half-life of loratadine in breast milk was reported to be 10.7 hours in
one woman (Hilbert 1988).
Drowsiness and irritability have been reported in breastfed infants exposed to antihistamines (Ito 1993). In general, second generation
antihistamines (eg, loratadine) are less sedating as compared to their first generation counterparts. If a breastfed infant is exposed to a
second generation antihistamine via breast milk, they should be monitored for irritability, jitteriness, or drowsiness (Butler 2014).
When treatment with an antihistamine is needed for the treatment of rhinitis and urticaria in breastfeeding women, a second
generation antihistamine, such as loratadine, is preferred (BSACI [Powell 2015]; BSACI [Scadding 2017]; Butler 2014; Zuberbier 2018).
Antihistamines may decrease maternal serum prolactin concentrations when administered prior to the establishment of lactation
(Messinis 1985).
Dietary Considerations
May be taken without regard to meals. Some products may contain phenylalanine and/or sodium.
Mechanism of Action
Long-acting tricyclic antihistamine with selective peripheral histamine H1-receptor antagonistic properties
Pharmacokinetics
Note: The pharmacokinetic profile of children 2 to 12 years is similar to that of adults (Claritin prescribing information 2000)
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Absorption: Rapid; food increases total bioavailability (AUC) by 40% to 48% (Claritin prescribing information 2000)
Distribution: Vd: 119 L/kg (Haria 1994); binds preferentially to peripheral nervous system H1 receptors; no appreciable entry into CNS
(Claritin prescribing information 2000)
Protein binding: 97% to 99% (loratadine), 73% to 76% (metabolite) (Haria 1994)
Metabolism: Extensively hepatic via CYP2D6 and 3A4 to active metabolite (descarboethoxyloratadine) (Claritin prescribing
information 2000)
Half-life elimination: 8.4 hours (range: 3 to 20 hours) (loratadine), 28 hours (range: 8.8 to 92 hours) (metabolite) (Claritin prescribing
information 2000); hepatic impairment: 24 hours (loratadine), 37 hours (metabolite) (Claritin prescribing information 2000)
Time to peak, serum: Loratadine: 1.3 hours (loratadine), 2.3 hours (metabolite) (Claritin prescribing information 2000)
Altered kidney function: With CrCl <30 mL/minute, AUC and Cmax are increased approximately 73% for loratadine and 120% for its
metabolite.
Older adult: AUC and Cmax are increased approximately 50%, and t½ ranged from 6.7 to 37 hours
Pricing: US
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when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine
the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate
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Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to
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