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Ординатура / Офтальмология / Английские материалы / Becker-Shaffer's Diagnosis and Therapy of the Glaucomas_Stamper, Lieberman, Drake_2009.pdf
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part

 

 

 

 

 

 

6

 

medical treatment

 

 

 

 

 

 

 

 

 

 

 

 

Table 27-1  Cholinergic drugs used to treat glaucoma

 

 

 

 

 

 

 

 

 

Drug

 

Major mechanism

Concentration

Usual dosage in glaucoma

Duration of hypotensive

 

 

 

of action

(formulation)

 

effect

 

 

 

 

 

 

Pilocarpine

 

Direct

0.5–10% (solution)

4 times daily

4–8 hours

Carbachol

 

Strong direct; weak indirect

0.75–3%

3 or 4 times daily

6–12 hours

Methacholine (Mecholyl)

Direct

2–20% (solution)

Every 2–12 hours

1–12 hours

Aceclidine (Glaucostat)

Direct; weak indirect

0.5–4% (solution)

4 times daily

4–8 hours

Echothiophate iodide

 

 

 

 

(Phospholine Iodide,

Strong indirect

0.03–0.25% (solution)

Every 12 to 24 hours

0.5–7 days

Echodide)

 

 

 

 

 

Demecarium bromide

Strong indirect

0.125–0.25% (solution)

Every 12 to 24 hours

0.5–7 days

(Humorsol, Tosmilen)

 

 

 

 

Physostigmine (Eserine)

Weak indirect

0.25–1% (solution)

4 times daily

4–6 hours

 

 

 

0.25–0.5% (ointment)

at bedtime

 

 

 

 

 

Neostigmine (Prostigmine)

Weak indirect

3–5% (solution)

4 times daily

4–6 hours

Isoflurophate (DFP, Floropryl)

Strong indirect

0.25% (ointment)

Every 12 hours, at bedtime

0.5–7 days

 

 

 

 

 

 

 

Fig. 27-1  Direct-acting cholinergic agents.

Direct-acting cholinergic agents

Acetylcholine

Acetylcholine is the prototype direct-acting cholinergic drug.When injected into the anterior chamber, acetylcholine stimulates parasympathetic end organs in the iris and ciliary body. Acetylcholine is not used for the treatment of glaucoma because it penetrates the cornea poorly and is destroyed rapidly by cholinesterase.

Intracameral acetylcholine is used almost exclusively during ocular surgery to constrict the pupil. Intracameral acetylcholine causes rapid pupil contraction and reduces the risk of immediate postoperative IOP rise after extracapsular cataract extraction.40 Intracameral carbachol produces a slower miosis but extends protection from IOP elevation to over 24 hours 41 and is more effective at lowering IOP in the immediate postoperative period than placebo, pilocarpine gel, or acetylcholine.42,43

Pilocarpine

Pilocarpine is still

the most widely prescribed miotic agent. It

is more potent at

muscarinic than at nicotinic receptor sites.

Pilocarpine is manufactured as a water-soluble hydrochloride or nitrate in solutions ranging from 0.25–10% (Fig. 27-1). The aqueous solutions are stable at slightly acidic pH levels. Pilocarpine penetrates the cornea well and produces a low incidence of allergic reactions. Animal studies indicate that the cornea absorbs pilocarpine rapidly and then releases it slowly to the aqueous humor (i.e., the cornea serves as a drug reservoir).44 The usual vehicles for pilocarpine are hydroxypropyl methylcellulose and polyvinyl alcohol. Benzalkonium chloride and sodium ethylenediamine tetraacetic acid (EDTA) are added to prevent microbial growth and to facilitate penetration.

Topical pilocarpine administration produces a reduction in IOP that begins in an hour and lasts for 4 to 8 hours.45 Pilocarpine is prescribed for use four times daily (i.e., as close to every 6 hours as possible) to ensure good IOP control. Pilocarpine (as well as its other miotic cousins) works well with other antiglaucoma agents. Specifically, miotics have been shown to work well with - blocking agents, carbonic anhydrase inhibitors, adrenergic agonists, and latanoprost.When used in conjunction with other antiglaucoma

422