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Phenylpropanolamine HCl and Chlorpheniramine Maleate
Each extended-release capsule contains Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg. Phenylpropanolamine Hydrochloride is (±)-NorephedrineHydrochloride, an adrenergic agent. Chlorpheniramine Maleate is 2-(p-Chloro-a-(2-(dimethylamino)ethyl)benzyl) pyridine maleate (1:1), an antihistamine. Phenylpropanolamine HCl has a molecular weight of 187.67.
Phenylpropanolamine Hydrochloride The drug may directly stimulate adrenergic receptors but probably indirectly stimulates both alpha (a) and beta (ß) adrenergic receptors by releasing norepinephrine from its storage sites. Phenylpropanolamine increases heart rate, force of contraction and cardiac output, and excitability. It acts on alpha receptors in the mucosa of the respiratory tract, producing vasoconstriction which results in shrinkage of swollen mucous membranes, reduction of tissue, hyperemia, edema and nasal congestion, and an increase in nasal airway patency. Phenylpropanolamine causes CNS stimulation and reportedly has an anorexigenic effect. Chlorpheniramine Maleate An antihistamine with anticholinergic (drying) and sedative side effects. Antihistamines appear to compete with histamine for H1 cell receptor sites on effector cells. Pharmacokinetics Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Capsules in extended-release form, was compared in 14 adult males against aqueous solutions of Phenylpropanolamine HCl 37.5 mg and Chlorpheniramine Maleate 12 mg taken at 0 and 6 hours. Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules was found to produce blood levels of Phenylpropanolamine HCl and Chlorpheniramine Maleate equivalent to that produced by the administration of the solution form of Phenylpropanolamine HCl and Chlorpheniramine Maleate. Additionally, Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules produced blood levels during the first hour that were identical to those produced by the solution form of the two actives while maintaining equivalent blood levels for a period of 12 hours or longer. Pharmacokinetics parameters are as follows: Phenylpropanolamine Hydrochloride The area under the curve to infinity for Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules was 1869 ng/mL•hr, and for the reference solution, 1729 ng/mL•hr. Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules did not produce the high-peak concentrations associated with multiple dosing of immediate release Phenylpropanolamine HCl and had a Cmax of 137 ng/mL as compared to the reference solution Cmax of 155 ng/mL. The Tmax for Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules was 3.07 hours and for the reference solution was 7.36 hours. The elimination half life was 6.34 hours for Phenypropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules and 4.52 hours for the reference solution. Chlorpheniramine Maleate The area under the curve to infinity for Phenylpropanolamine Hydrochloride
75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules was
514 ng/mL•hr as compared to the reference solution of 504 ng/mL•hr. The
Cmax for Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine
Maleate 12 mg Extended-release Capsules was 17.5 ng/mL and for the reference
solution, 19.2 ng/mL. The Tmax for Phenylpropanolamine Hydrochloride
75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules was
7.32 hours and for the reference solution 9.07 hours. The elimination
half life for Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine
Maleate 12 mg Extended-release Capsules was 19.15 hours and for the reference
solution 14.7 hours.
For the treatment of the symptoms of seasonal and perennial allergic rhinitis, and vasomotor rhinitis, including nasal obstruction (congestion).
Adults and children over 12 years of age - one capsule orally every 12 hours. Should not be used in children under 12. HOW SUPPLIED Each Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsule is a blue and clear capsule imprinted M 0421.
Dispense in a tight, light-resistant container as defined in the USP. Storage: Store at controlled room temperature 15°- 30°C (59°- 86°F). CAUTION:M Federal law prohibits dispensing without prescription.
General: Urticaria, drug rash, anaphylactic shock, photosensitivity, excessive perspiration, chills, dryness of mouth, nose and throat. Cardiovascular System: Hypotension, hypertension, headache, palpitations, tachycardia, extrasystoles, and angina pain. Hematologic System: Hemolytic anemia, thrombocytopenia, agranulocytosis. Nervous System: Sedation, dizziness, disturbed coordination, fatigue, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesias, blurred vision, diplopia, vertigo, tinnitus, acute labyrinthitis, hysteria, neuritis and convulsions. Gastrointestinal System: Epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation. Genitourinary System: Urinary frequency, difficult urination, urinary retention, early menses. Respiratory System: Thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness.
Should not be used in patients taking MAO inhibitors. Antihistamines
have additive effects with alcohol and other CNS depressants (hypnotics,
sedatives, tranquilizers, etc.).
Caution patients about activities requiring alertness (e.g., operating vehicles or machinery). Patients should also be warned about the possible additive effects of alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc.).
General Should be used with considerable caution in patients with narrow angle glaucoma, stenosing peptic ulcer, pyloroduodenal obstruction, symptomatic prostatic hypertrophy, bladder neck obstruction, hypertension, thyroid disease, diabetes and heart disease. The risk of antihistamine-induced dizziness, sedation and hypotension is greater in elderly patients (over 60 years). Drug Interactions See DRUG INTERACTIONS section. Usage in Pregnancy Pregnancy Category C. Animal reproduction studies have not been conducted. It is also not known whether this product can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules should be given to a pregnant woman only if clearly needed. Nursing Mothers It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Phenylpropanolamine Hydrochloride 75 mg and Chlorpheniramine Maleate 12 mg Extended-release Capsules is administered to a nursing mother. Pediatric Use Safety and effectiveness in children below the age of 12 have not been
established.
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