Loratadine + Pseudoephedrine

Oral
Allergic rhinitis, Cold and flu

Severe: Initial dose of 1 tab (containing loratadine 5 mg and pseudoephedrine sulfate 120 mg) daily or ½ the usual syrup dose.

Extended-Release: May be taken with or without food. Swallow whole, do not break, chew or dissolve.

Lactation. Narrow angle glaucoma, urinary retention, severe hypertension, severe coronary artery disease and hyperthyroidism. Patients on MAOI therapy or within 14 days of discontinuing MAOI.

Glaucoma, increased intraocular pressure, stenosing peptic ulcer and pyloroduodenal obstruction, prostatic hypertrophy, bladder neck obstruction, CV disease, DM, severe liver impairment. Not recommended for use in pregnancy. Elderly. Tablets to be swallowed whole and patients should be instructed not to break, chew, or dissolve such tablets.

Insomnia, dry mouth, headache, nervousness, epistaxis, pharyngitis, dizziness, fatigue, tachycardia, postural hypotension, transient abnormal hepatic function, urinary retention, CNS stimulation, excitability.

Symptoms: CNS depression (sedation, apnoea, decreased mental alertness, cyanosis, coma, CV collapse), CNS stimulation (insomnia, hallucination, convulsions) and even death. Management: Induce emesis, followed by supportive and symptomatic treatment.

Loratadine: Increased loratadine levels with ritonavir, amprenavir; increased loratadine levels with erythromycin, cimetidine and ketoconazole without evidence of clinical significance or toxicity; may block effects of betahistine. Pseudoephedrine: Increased adverse effects (e.g. somnolence, agitation) with atomoxetine; increased BP or heart rate with sibutramine.
Potentially Fatal: Pseudoephedrine: Increased risk of psychosis with bromocriptine; increased risk of fatal hypertensive crisis with MAOI, avoid concurrent use during and for 2 wk after stopping the MAOI; increased BP with linezolid and selegiline.

Reactions to skin testing procedures may be reduced, antihistamines should be discontinued 48 hr before procedure.

Description: Loratadine is a long-acting, non-sedating antihistamine with little antimuscarinic activity. Pseudoephedrine, a vasoconstrictor, acts on the α-receptors and produces a decongestant effect by shrinking congested mucosa in the upper respiratory areas.
Onset: Nasal decongestion: 30 minutes.
Duration: Nasal decongestion: 8 hr (60 mg pseudoephedrine) and 12 hr (120 mg pseudoephedrine in extended release preparations).
Pharmacokinetics:
Absorption: Loratadine: Absorbed rapidly from GI tract, peak plasma concentrations reached in about 1 hr, bioavailability increased and time to peak plasma concentrations delayed when taken with food.
Distribution: Loratadine: 98% bound to plasma proteins; desloratadine 73-76% bound to plasma proteins; loratadine and its metabolites enters into breast milk, but do not to cross the blood-brain barrier significantly. Pseudoephedrine: May distribute into milk, crosses placenta and into CSF.
Metabolism: Loratadine: Undergoes extensive metabolism by cytochrome P450 isoenzymes CYP3A4 and CYP2D6; its major metabolite desloratadine has potent antihistaminic activity; elimination half-lives 8.4 hr (loratadine), 28 hr (desloratadine).
Excretion: Loratadine: Excreted equally in the urine and faeces, mainly in the form of metabolites. Pseudoephedrine: Undergoes incomplete metabolism in the liver by N-demethylation to inactive metabolite; excreted in urine with 55-75% of dose excreted unchanged.

Store below 25°C.

Nasal Decongestants & Other Nasal Preparations / Antihistamines & Antiallergics