Glycopyrrolate

GLYCOPYRROLATE- glycopyrrolate solution
Par Pharmaceutical, Inc.

1 INDICATIONS AND USAGE

Glycopyrrolate oral solution is indicated to reduce chronic severe drooling in patients aged 3 to 16 years with neurologic conditions associated with problem drooling (e.g., cerebral palsy).

2 DOSAGE AND ADMINISTRATION

Glycopyrrolate oral solution must be measured and administered with an accurate measuring device [ see Patient Counseling Information (17)].

Initiate dosing at 0.02 mg/kg orally three times daily and titrate in increments of 0.02 mg/kg every 5to7 days based on therapeutic response and adverse reactions. The maximum recommended dosage is 0.1 mg/kg three times daily not to exceed 1.5-3 mg per dose based upon weight. For greater detail, see Table 1.

During the four-week titration period, dosing can be increased with the recommended dose titration schedule while ensuring that the anticholinergic adverse events are tolerable. Prior to each increase in dose, review the tolerability of the current dose level with the patient’s caregiver.

Glycopyrrolate oral solution should be dosed at least one hour before or two hours after meals.

The presence of high fat food reduces the oral bioavailability of glycopyrrolate oral solution if taken shortly after a meal [see Clinical Pharmacology (12.3)].

Table 1: Recommended Dose Titration Schedule (each dose to be given three times daily)

Weight		Dose Level 1		Dose Level 2		Dose Level 3		Dose Level 4		Dose Level 5
Kg	lbs	(~0.02 mg/kg)		(~0.04 mg/kg)		(~0.06 mg/kg)		(~0.08 mg/kg)		(~0.1 mg/kg)
13-17	27-38	0.3 mg	1.5 mL	0.6 mg	3 mL	0.9 mg	4.5 mL	1.2 mg	6 mL	1.5 mg	7.5 mL
18-22	39-49	0.4 mg	2 mL	0.8 mg	4 mL	1.2 mg	6 mL	1.6 mg	8 mL	2.0 mg	10 mL
23-27	50-60	0.5 mg	2.5 mL	1.0 mg	5 mL	1.5 mg	7.5 mL	2.0 mg	10 mL	2.5 mg	12.5 mL
28-32	61-71	0.6 mg	3 mL	1.2 mg	6 mL	1.8 mg	9 mL	2.4 mg	12 mL	3.0 mg	15 mL
33-37	72-82	0.7 mg	3.5 mL	1.4 mg	7 mL	2.1 mg	10.5 mL	2.8 mg	14 mL	3.0 mg	15 mL
38-42	83-93	0.8 mg	4 mL	1.6 mg	8 mL	2.4 mg	12 mL	3.0 mg	15 mL	3.0 mg	15 mL
43-47	94-104	0.9 mg	4.5 mL	1.8 mg	9 mL	2.7 mg	13.5 mL	3.0 mg	15 mL	3.0 mg	15 mL
≥48	≥105	1.0 mg	5 mL	2.0 mg	10 mL	3.0 mg	15 mL	3.0 mg	15 mL	3.0 mg	15 mL

3 DOSAGE FORMS AND STRENGTHS

Glycopyrrolate oral solution is available as a 1mg/5 mL clear, cherry-flavored solution for oral administration in 16 ounce bottles.

4 CONTRAINDICATIONS

Glycopyrrolate oral solution is contraindicated in:

• Patients with medical conditions that preclude anticholinergic therapy (e.g., glaucoma, paralytic ileus, unstable cardiovascular status in acute hemorrhage, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis, myasthenia gravis).

• Patients taking solid oral dosage forms of potassium chloride. The passage of potassium chloride tablets through the gastrointestinal (GI) tract may be arrested or delayed with coadministration of glycopyrrolate oral solution.

5 WARNINGS AND PRECAUTIONS

5.1 Constipation or Intestinal Pseudo-obstruction

Constipation is a common dose-limiting adverse reaction which sometimes leads to glycopyrrolate discontinuation [see Adverse Reactions (6.1)].Assess patients for constipation, particularly within 4to5 days of initial dosing or after a dose increase. Intestinal pseudo-obstruction has been reported and may present as abdominal distention, pain, nausea or vomiting.