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18-2 Cholinergics
Table 18-2 Cholinergics
| Generic (Brand) | Route and Dosage | Uses and Considerations |
|---|---|---|
| carbachol (Miostat) | Ophthalmic: 0.75%-3%, 1–2 gtt, 3 daily | To reduce IOP, miosis. |
| pilocarpine HCl (Pilocar) | Ophthalmic: 0.5%-4%, 1 gt | To reduce IOP, miosis |
| tacrine HCl (Cognex) | Alzheimer's disease: A: PO: 10 mg, q.i.d., increase dose at 6 wk intervals A: PO: 40–160 mg/d p.c.; max: 160 mg/d | To improve memory in mild to moderate Alzheimer's dementia. Drug enhances cholinergic function. Pregnancy category: C; PB: 55%; t½: 1.5-3.5 h |
| demecarium bromide (Humorsol) | 0.125%-0.25%, 1 gt q12-48 h | To reduce IOP in glaucoma; long-acting miotic |
| echothiophate iodide (Phospholine Iodide) | 0.03%-0.25%, 1 gt daily or b.i.d. | To reduce IOP; long-acting miotic |
| isoflurophate (Floropryl) | 0.25%, ointment q8-72 h | To treat glaucoma. Apply to the conjunctival sac. |
| ambenonium Cl (Mytelase) | A: PO: 2.5-5.0 mg t.i.d./q.i.d.; dose may be increased; maint: 5–25 mg t.i.d./q.i.d. | To increase muscle strength in myasthenia gravis; long acting. May be used with glucocorticoids. Pregnancy category: C; PB: UK; t½: UK |
| edrophonium Cl (Tensilon) | A: IV: 2 mg; then 8 mg if no responseIM: 10 mg; may repeat with 2 mg in 30 minC: 34 kg: IV: 1 mg; repeat in 30–45 sec if no response; max: 5 mgC: 34 kg: IV: 2 mg; repeat with 1 mg if no response; max: 10 mg | To diagnose myasthenia gravis; very short- acting. Pregnancy category: C; PB: UK; t½: 1.2-2 h |
| neostigmine (Prostigmin); neostigmine methylsulfate (injectable form) | A: PO: Initially 15 mg t.i.d.; maint: 150 mg/d in divided doses; range: 15–375 mg/d IM/IV: 0.5-2.5 mg PRNC: PO: 2 mg/kg/d in 6 divided doses | To increase muscle strength in myasthenia gravis; short acting. Used also to prevent or treat postoperative urinary retention. Pregnancy category: C; PB: 15%-25%; t½: 1-1.5 h |
| physostigmine salicylate (Eserine Salicylate) | 0.25%-0.5%, 1 gt daily or q.i.d. | To reduce IOP, miosis; short-acting |
| pyridostigmine bromide (Mestinon) | A: PO: 60–120 mg t.i.d./q.i.d.; maint: 600 mg/d in 3–4 divided doses; max: 1.5 g/dSR: 180–540 mg daily or b.i.d.IM/IV: 2 mg q2-3hC: PO: 7 mg/kg/d in 5–6 divided doses | To increase muscle strength in myasthenia gravis; moderate- acting. Prevents destruction of the neurotransmitter acetylcholine. Pregnancy category: C; PB: 10%; t½: 3–4 h |
| pralidoxime Cl (Protopam) | A: IM: 1–2 g, repeat in 1–2 h, then 10 to 12 h intervalsA: IV: 1–2 g in 100 ml of saline solution infused over 15–30 minA: PO: 1–3 g, repeat in 5 h PRNC: IV: 20–40 mg/kg/dose; repeat in 1–2 h; 10- to 12-h intervals PRN | To treat overdose of organophosphate pesticides that cause muscle paralysis and to treat overdose of a cholinesterase inhibitor for myasthenia gravis. Pregnancy category: C; PB: UK; t½: 1- 2.7 h |
| bethanechol Cl (Urecholine) | A: PO: 10–50 mg b.i.d./t.i.d./q.i.d.; max: 120 mg/dsubQ: 2.5-5 mg, repeat at 15–30 min intervals; PRNDo NOT give IM or IV.C: PO: 0.5 mg/kg/d in 3–4 divided doses | To treat urinary retention, abdominal distention; Stimulate the cholinergic (muscarinic) receptor; promote contraction of the bladder; increase GI peristalsis, GI secretion, pupillary constriction, and bronchoconstriction |
| metoclopramide HCl (Reglan, Maxolon) | A: PO: 10–15 mg t.i.d. a.c.C: PO/IM/IV: 0.4-0.8 mg/kg/d in 4 divided doses | For GERD and gastroparesis. Central dopamine receptor antagonist. Increases gastric emptying time. Pregnancy category: B; PB: UK; t½: 2.5-6 h |
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