Karbinal Drug Information

General

Administration Instructions The dosage of Karbinal ER should be individualized based on the severity of the condition and the response of the patient. Start with lower doses and increase as needed and tolerated. Administer Karbinal ER by the oral route only.

Measure Karbinal ER with an accurate milliliter measuring device. A household teaspoon is not an accurate measuring device and could lead to overdosage. A pharmacist can provide an appropriate measuring device and can provide instructions for measuring correct dose.

Shake Karbinal ER well before use.

Recommended Dosage for Adults and Adolescents 12 years of age and older

Administer 7.5 mL to 20 mL (6 mg to 16 mg) orally every 12 hours

Recommended Dosage for Pediatric Patients 2 years to 11 years of age

(approximately 0.2 mg/kg/day to 0.4 mg/kg/day) 2 years to 3 years: Administer 3.75 mL to 5 mL (3 mg to 4 mg) orally every 12 hours administered orally 4 years to 5 years: Administer 3.75 mL to 10 mL (3 mg to 8 mg) orally every 12 hours administered orally 6 years to 11 years: Administer 7.5 mL to 15 mL (6 mg to 12 mg) orally every 12 hours administered orally

The following clinically significant adverse reactions are descrived elsewhere in the labeling: Somnolense and Impaired Mental Alertness. Allergic Reactions due to Sulfites, including Anaphylaxis. The most frequent adverse reactions include: sedation, sleepiness, dizziness, disturbed coordination, epigastric distress, and thickening of bronchial secretions.

In clinical use, younger children and older adults may be particularly sensitive to adverse reactions. The following adverse reactions, listed by body system, have been identified in case reports and during the use of carbinoxamine in observational studies. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Body as a Whole : Urticaria, drug rash, anaphylactic shock, photosensitivity, excessive perspiration, chills, dryness of mouth, nose and throat. Cardiovascular : Hypotension, headache, palpitations, tachycardia, extrasystoles. Central Nervous System : Fatigue, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, blurred vision, diplopia, vertigo, tinnitus, acute labyrinthitis, hysteria, neuritis, convulsions.

Gastrointestinal : Anorexia, nausea, vomiting, diarrhea, constipation. Hematologic : Hemolytic anemia, thrombocytopenia, agranulocytosis. Laboratory : Increase in uric acid levels.

Respiratory : Tightness of chest and wheezing, nasal stuffiness. Urogenital : Urinary frequency, difficult urination, urinary retention, early menses. Most common adverse reactions are: sedation, sleepiness, dizziness, disturbed coordination, epigastric distress, and thickening of bronchial secretions.

To report SUSPECTED ADVERSE REACTIONS, contact Cerecor, Inc., at 1-866-416-9637 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Do not use of Karbinal ER in patients who are taking monoamine oxidase inhibitors (MAOIs), which prolong and intensify the anticholinergic (drying) effects of antihistamines. Avoid use of Karbinal ER with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc.) due to additive effects. Monoamine oxidase inhibitors (MAOIs): Prolong and intensify the anticholinergic (drying) effects. ( 4 and 7 ) Alcohol and CNS depressants (hypnotics, sedatives, tranquilizers, etc.): Avoid concomitant use due to additive adverse effects.

Pregnancy Risk Summary Published data over decades of use of antihistamines, including carbinoxamine, have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal out comes. However, published dat a specifically evaluating the risk of carbinoxamine were not found. Animal reproductive studies have not been conducted with carbinoxamine maleate.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Pediatric Use Karbinal ER is contraindicated in pediatric patients younger than 2 years of age because deaths have been reported in this patient population who were taking carbinoxamine-containing drug products . The safety and effectiveness of Karbinal ER in pediatric patients aged 2 years and older have been established and is based on demonstration of bioequivalence to the immediate-release reference product . Carbinoxamine may diminish mental alertness or produce sedation in children. Paradoxical reactions with excitation are more likely in younger children.

Karbinal ER is contraindicated in: children younger than 2 years of age because deaths have been reported in this age group (see Warnings and Precautions ] patients who are hypersensitive to carbinoxamine maleate or any of the inactive ingredients in Karbinal ER patients who are taking monoamine oxidase inhibitors (MAOI). Children younger than 2 years of age Patients with known hypersensitivity to the drug or any of the inactive ingredients Monoamine oxidase inhibitors (MAOI)

10. OVERDOSAGE Overdosage with carbinoxamine may cause central nervous system depression or stimulation, hallucinations, convulsions, and death. Atropine-like signs and symptoms – dry mouth; fixed, dilated pupils; flushing; and gastrointestinal symptoms may also occur. The treatment of overdosage consists of discontinuation of Karbinal ER and institution of symptomatic and supportive therapy.

Vital signs (including respiration, pulse, blood pressure, and temperature) and EKG should be monitored. Induction of vomiting is not recommended. Activated charcoal should be given and gastric lavage should be considered after ingestion of a potentially life-threatening amount of drug.

In the presence of severe anticholinergic effects, physostigmine may be useful. Vasopressors may be used to treat hypotension.