部分中文Pilopine HS处方资料（仅供参考）
英文药名: Pilopine HS (pilocarpine Gel)
中文药名: 毛果芸香碱眼用凝胶
药品简介
毛果芸香碱眼凝胶属化药新药5类。 作为眼科局部应用的缩瞳药，毛果芸香碱属拟胆碱药，它直接作用于M-胆碱受体产生毒蕈碱样作用。
作用机理：
1、作用于瞳孔括约肌，引起缩瞳，牵引巩膜小梁，拉开虹膜根部，开放房角使房水流畅而降低眼压。
2、作用于睫状体使其收缩，牵引巩膜，扩大巩膜小梁网眼，改善房水外流而降低眼压。
临床利用其缩瞳、降眼压作用治疗开角型青光眼和闭角型青光眼。
青光眼的发病率和患病率较高，在眼科的门诊病人中占8.5%。因此，开发研制新的治疗青光眼的药物制剂具有较大的市场空间。毛果芸香碱用于治疗青光眼已有100多年的历史，虽然近年来，国内外相继开发出几种新的治疗青光眼的药物（噻吗心安、碳酸酐酶抑制剂等），但因副作用较大，或药物的价格昂贵，使其应用受到限制，而毛果芸香碱因疗效好、价格低廉，目前仍是大多数医生作为治疗青光眼的首选药物。
但由于其滴眼液在治疗时，作用时间较短，每天需要多次用药，因有缩瞳及增强调节作用，白天常引起瞳孔大小和屈光度波动，存在较大的局限性，因此它的使用也受到限制。
国外早在二十世纪70年代就开始了毛果芸香碱新剂型的研究，现在已经有凝胶剂和眼用植入剂等新剂型上市。国内对毛果芸香碱的制剂研究很少，现在仍然只有滴眼液一个眼用品种，制剂的品种单一，极大地限制了毛果芸香碱的临床应用。为此，研究开发了硝酸毛果芸香碱眼凝胶。
硝酸毛果芸香碱眼凝胶，选择卡波沫为凝胶基质。作为一种药用辅料，卡波沫在国外已应用多年，具有释药快、药效持久、无油腻性、易涂展、粘附性好、对皮肤及粘膜无刺激等特点，已被中国药典2000年版收载。硝酸毛果芸香碱眼凝胶与硝酸毛果芸香碱滴眼液比较，具有在眼内停留时间长，具缓释效果，副作用小，给药方便，患者耐受性好等特点。
国外对于毛果芸香碱眼用凝胶的研究开展得较早，1996年Alcon公司就分别在美国和英国上市了该制剂，美国上市的商品名为Pilopine HS,英国上市的商品名为Pilogel。本品原料药已被中国药典2000版收载；国内仅有滴眼液用于治疗青光眼，为治疗青光眼的首选一线用药，临床用量居各类抗青光眼药物的前列；近年又有片剂批准上市，但其适应症为治疗癌症患者放化疗引起的口干，未见有其他的剂型被批准进行临床研究或生产。
PILOPINE HS - pilocarpine hydrochloride gel 
Physicians Total Care, Inc.
DESCRIPTION
PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is a sterile topical ophthalmic aqueous gel which contains more than 90% water and employs carbopol 940, a synthetic high molecular weight cross-linked polymer of acrylic acid, to impart a high viscosity. The active ingredient, pilocarpine hydrochloride, is a cholinergic agent and is represented by the chemical structure:
Established name: Pilocarpine Hydrochloride
Chemical name: 2(3H )-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)-methyl]-, monohydrochloride, (3S-cis)-.
PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% - Each Gram Contains: Active: pilocarpine hydrochloride 4% (40 mg). Preservative: benzalkonium chloride 0.008%. Inactives: carbopol 940, edetate disodium, hydrochloric acid and/or sodium hydroxide (to adjust pH) and purified water.
CLINICAL PHARMACOLOGY
PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is a direct acting cholinergic parasympathomimetic agent which acts through direct stimulation of muscarinic neuroreceptors and smooth muscle such as the iris and secretory glands. Pilocarpine produces miosis through contraction of the iris sphincter, causing increased tension on the scleral spur and opening of the trabecular meshwork spaces to facilitate outflow of aqueous humor. Outflow resistance is thereby reduced, lowering intraocular pressure.
INDICATIONS AND USAGE
PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is a miotic (parasympathomimetic) used to control intraocular pressure. It may be used in combination with other miotics, beta-blockers, carbonic anhydrase inhibitors, sympathomimetics or hyperosmotic agents.
CONTRAINDICATIONS
Miotics are contraindicated where constriction is undesirable, such as in acute iritis, and in those persons showing hypersensitivity to any of their components.
WARNINGS
FOR TOPICAL OPHTHALMIC USE ONLY.
PRECAUTIONS
General
The miosis usually causes difficulty in dark adaptation. Patient should be advised to exercise caution in night driving and other hazardous occupations in poor illumination.
Information For Patients
Do not touch tube tip to any surface, as this may contaminate the gel.
Carcinogenesis, Mutagenesis, Impairment of Fertility
There have been no long-term studies done using pilocarpine hydrochloride in animals to eva luate carcinogenic potential.
Pregnancy
Pregnancy Category C. Animal reproduction studies have not been conducted with pilocarpine hydrochloride. It is also not known whether pilocarpine hydrochloride can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% should be given to a pregnant woman only if clearly needed.
Nursing Mothers
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when pilocarpine hydrochloride is administered to a nursing woman.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients.
ADVERSE REACTIONS
The following adverse experiences associated with pilocarpine therapy have been reported: lacrimation, burning or discomfort, temporal or periorbital headache, ciliary spasm, conjunctival vascular congestion, superficial keratitis and induced myopia. Systemic reactions following topical administration are extremely rare, but occasional patients are peculiarly sensitive to develop sweating and gastrointestinal overactivity following suggested dosage and administration. Ocular reactions usually occur during initiation of therapy and often will not persist with continued therapy. Reduced visual acuity in poor illumination is frequently experienced in older individuals and in those with lens opacity. A subtle corneal granularity was observed in about 10% of patients treated with PILOPINE HS®. Cases of retinal detachment have been reported during treatment with miotic agents; especially in young myopic patients. Lens opacity may occur with prolonged use of pilocarpine.
OVERDOSAGE
Overdosage can produce sweating, salivation, nausea, tremors, and slowing of the pulse and a decrease in blood pressure. Bronchial constriction may develop in asthmatic patients. In moderate overdosage, spontaneous recovery is to be expected and is aided by intravenous fluids to compensate for dehydration. For cases demonstrating severe poisoning, atropine is the pharmacologic antagonist to pilocarpine.
A topical ocular overdose of an ophthalmic product containing pilocarpine may be flushed from the eye(s) with warm tap water.
DOSAGE AND ADMINISTRATION
Apply a one-half inch ribbon in the lower conjunctival sac of the affected eye(s) once a day at bedtime.
HOW SUPPLIED
PILOPINE HS® (pilocarpine hydrochloride ophthalmic gel) 4% is supplied as a 4% sterile aqueous gel in 4 gram tubes with ophthalmic tip.
4 gram: NDC 54868-0631-0
STORAGE: Store at room temperature 2°-27°C (36° -80° F). Avoid excessive heat. Do not freeze.