Carbachol

Store in airtight containers. Protect from light.

Aqueous solutions are most stable to autoclaving when buffered to pH 3.5. Up to 5% decomposition may occur when unbuffered solutions are heated in an autoclave, and the decomposition increases the pH of the solutions; such autoclaved solutions should not be stored for more than a yr.

1.4 [mg/m3]

15 [mg/m3]

90 [mg/m3]

For emergency situations, wear a positive pressure, pressure-demand, full facepiece self-contained breathing apparatus (SCBA) or pressure- demand supplied air respirator with escape SCBA and a fully-encapsulating, chemical resistant suit. (EPA, 1998)

Acetylcholine and methacholine are hydrolyzed by acetylcholinesterase and their effects are markedly enhanced by the prior administration of anticholinesterase agents. The latter drugs produce only additive effects with the stable analogs, carbachol and bethanechol. The muscarinic actions of all the drugs of this class are blocked selectively by atropine, through competitive occupation of cholinergic receptor sites on the autonomic effector cells and on the secondary muscarinic receptors of autonomic ganglion cells.

When used in conjunction with topical epinephrine, topical timolol, and/or systemically admin carbonic anhydrase inhibitiors, the effect of miotics in lowering intraocular pressure may be additive. /Miotics/

Although the clinical importance has not been established, the miotic and/or ocular hypotensive effects of miotics reportedly may be antagonized by long-term topical or systemic corticosteroid therapy, systemic anticholinergics, antihistamines, meperidine, sympathomimetics, & tricyclic antidepressants ... .

Ophthalmic carbachol may be ineffective when administred following ophthalmic flubiprofen; the pharmacologic basis for this interference is not known.

Concurrent use of ... /ophthalmic belladona alkaloids or cyclopentolate/ may interfere with the antiglucoma action of carbachol; also concurrent use with carbachol counteracts the myrdiatic effects of these medications ... .

Systemic reactions after chronic topical application of /some/ ... miotics to the eye or intraocular injection of acetylcholine or carbachol are rare and usually occur only with very frequent admin. ... Adverse systemic effects of miotics result from parasympathetic stimulation and the most common effects, especially in children, include nausea, vomiting, diarrhea, abdominal pain, and intestinal cramps.

A 58-yr-old man developed esophageal rupture 2 hr after a subcutaneous injection of carbachol to relieve urinary retention.

A report of life-threatening attacks of profuse sweating, intestinal cramps ... defecation, hypothermia, hypotension, and bradycardia in a 36-yr-old man due to carbachol intoxication /was recorded/. A 10-yr-old boy had died following similar attacks associated with repeated carbachol ingestion.

The most common ... effects of miotic therapy are painful ciliary or accommodative spasm, blurred vision or myopia, and poor vision in dim light. ... Other adverse effects ... include ciliary or conjunctival congestion, lacrimal passage stenosis, twitching of the eyelids, stinging, burning, lacrimation, ocular or brow pain, headache, photophobia ... /Miotics/

Tests of 0.01% solution introduced into the anterior chamber of eyes of human beings ... have shown no significant irritating or injurious action, but prompt miotic effect.

Carbachol, in doses sufficient to cause purgation /in animals/, produces a profound drop in the diastolic blood pressure. Larger doses aggravate this by inhibiting the heart itself.

All parasympathomimetic drugs, in toxic doses, stimulate all the secretions and produce severe gastrointestinal colic and diarrhea and dyspnea; the iris is markedly constricted; the heart rate is first increased and then slowed. Death may be due to respiratory paralysis or heart block. /Parasympathomimetic drugs/

The phenomenon of sudden mortality in the chick embryo, induced by the exogenous neurotransmitter /such as/ carbachol, is described. When introduced singly into eggs (albumen) in doses of 0.1 mg/egg, /the cmpd/ induced highly significant, sharply incr mortality (60-100%) when the introduction was on embryonic (incubation) days 8 to 12, but none if introduction was earlier. These ages follow the appearance of functional receptors (or receptor-effectors) for the substance. ... The involvement of receptors here have not been proved. Solvent alone (Ringer's solution for chick) had no effect, indicating that the procedures used were in themselves not lethal. ...

Tests of 0.01% solution intrduced into the anterior chamber of eyes of rabbits, cats ... have shown no significant irritating or injurious action, but prompt miotic effect.

LD50 Mouse oral 5 mg/kg

LD50 Mouse iv 0.3 mg/kg

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed drug products, incl carbachol, approved on the basis of safety and effectiveness by FDA under sections 505 and 507 of the Federal Food, Drug, and Cosmetic Act. /From Appendix A, Product Name Index/

Releases of CERCLA hazardous substances are subject to the release reporting requirement of CERCLA section 103, codified at 40 CFR part 302, in addition to the requirements of 40 CFR part 355. Carbachol chloride is an extremely hazardous substance (EHS) subject to reporting requirements when stored in amounts in excess of its threshold planning quantity (TPQ) of 500/10,000 lbs.

MEDICATION (VET)

MEDICATION

Commercially available ophthalmic solutions contain benzalkonium chloride as preservative and wetting agent. ... Preparations: Ophthalmic - Injection, for intraocular use only 100 ug/ml (0.01%) Miostat Intraocular. Solution: 0.75%, Isopto Carbachol (with benzalkonium chloride; viscous); 1.5%, Isopto Carbachol (with benzalkonium chloride; viscous); 2.25%, Isopto (with benzalkonium chloride: viscous); 3% Isotop Carbachol (with benzalkomum chloride; viscous).

Eyedrops: APF has carbachol 750 mg, sodium chloride 700 mg, benzalkonium chloride soln 0.02 ml, disodium edetate 50 mg. Water for injections to 100 ml ... Another formula: carbachol 800 mg, anhydrous dextrose 5 g, chlorhexidine acetate 5 mg. Water for injection to 100 ml ...

Carbachol intraocular soln is a sterile soln of carbachol in an aqueous medium. It contains not less than 90.0% & not more than 115.0% of the labeled amt of Carbachol. It contains no preservatives or antimicrobial agents.