Decreased GI and respiratory secretions.
Absorption: Incompletely absorbed (<10%) after oral administration. Well absorbed after IM administration.
Distribution: Distribution not fully known. Does not significantly cross the blood-brain barrier or eye. Crosses the placenta.
Metabolism and Excretion: Eliminated primarily unchanged in the urine and bile.
Half-life: 1.7 hr (0.6–4.6 hr).
TIME/ACTION PROFILE (anticholinergic effects)
|PO||1 hr||unknown||8–12 hr|
|IM||15–30 min||30–45 min||2–7 hr*|
|IV||1–10 min||unknown||2–7 hr*|
Use Cautiously in:
CV: tachycardia, orthostatic hypotension, palpitations
EENT: nasal congestion, blurred vision, cycloplegia, dry eyes, mydriasis
GI: dry mouth, vomiting, constipation
GU: urinary hesitancy, urinary retention
Neuro: headache, confusion, drowsiness.
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Control of Secretions during Surgery
IM (Adults): 4.4 mcg/kg 30–60 min preop (not to exceed 0.1 mg).
IM (Children >2 yr): 4.4 mcg/kg 30–60 min preop.
IM (Children <2 yr): 4.4–8.8 mcg/kg 30–60 min preop.
Control of Secretions (chronic)
IM IV Children: 4–10 mcg/kg/dose every 3–4 hr.
PO Children: 40–100 mcg/kg/dose 3–4 times/day.
IV (Adults and Children): 200 mcg for each 1 mg of neostigmine or 5 mg of pyridostigmine given at the same time.
IV (Adults): 100 mcg, may be repeated every 2–3 min.
IV Children: 4.4 mcg/kg (up to 100 mcg); may be repeated every 2–3 min.
PO (Adults): 1–2 mg 2–3 times daily. An additional 2 mg may be given at bedtime; may be ↓ to 1 mg twice daily (not to exceed 8 mg/day).
IM IV (Adults): 100–200 mcg every 4 hr up to 4 times daily.
Chronic Severe Drooling
PO (Children 3–16 yr): Oral solution– 0.02 mg/kg 3 times daily; may ↑ by 0.02 mg/kg 3 times daily every 5–7 days (not to exceed 0.1 mg/kg 3 times daily or 1.5–3 mg/dose).
Oral solution (cherry-flavor): 1 mg/5 mL
Solution for injection: 200 mcg (0.2 mg)/mL
Tablets: 1 mg, 1.5 mg, 2 mg
Pedi: Monitor amount and frequency of drooling periodically during therapy.
Lab Test Considerations:
Antagonizes effects of pentagastrin and histamine during the gastric acid secretion test. Avoid administration for 24 hr preceding the test.
If overdose occurs, neostigmine is the antidote.
Administer 30–60 min before meals to maximize absorption.
Pedi: Instruct parents to use a calibrated measuring device with solution for accurate dosing.
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