Carbachol

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[[Image:{{{image|Carbachol.png}}}|{{{width|220}}}px|Carbachol chemical structure]]
Carbachol

2-carbamoyloxyethyl-trimethyl-azanium
IUPAC name
CAS number
51-83-2 		}}}
PubChem
2551 		DrugBank
APRD00845
Chemical formula C6H15N2O2+
Molecular weight 147.196
Bioavailability  ?
Metabolism  ?
Elimination half-life  ?
Excretion  ?
Pregnancy category C (US)
Legal status  ?
Routes of administration Tablet, liquid

Carbachol (Kar-ba-kol [[Wikipedia:English_phonetic_spelling|key]), also known as carbamylcholine (marketed under the brand names Carbastat®, Carboptic®, Isopto Carbachol®, Miostat®), is classified as a cholinergic. It is primarily used for various opthalmic purposes, such as for treating glaucoma, or for use during ophthalmic surgery. It is generally administered as an intraocular solution (i.e. eyedrop).

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Chemistry and pharmacology

Carbachol is a choline ester and a positively charged quaternary ammonium compound. It is not well absorbed in the gastro-intestinal tract and does not cross the blood-brain barrier. It is usually administered topical ocular or through intraocular injection. Carbachol is not easily metabolized by cholinesterase, its duration of action is 4 to 8 hours with topical administration and 24 hours for intraocular administration. Since carbachol is poorly absorbed through topical administration, benzalkonium chloride is mixed in to promote absorption.

Carbachol is a parasympathomimetic that stimulates both muscarinic and nicotinic receptors. In topical ocular and intraocular administration its principal effects are miosis and increased aqueous humour outflow.

In the cat and rat, carbachol is well-known for its ability to induce rapid eye movement (REM) sleep when microinjected into the pontine reticular formation. Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic cholinergic receptors (mAChRs).

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Indications

Carbachol is primarily used in the treatment of glaucoma, but it is also used during ophthalmic surgery. Carbachol eyedrops are used to decrease the pressure in the eye for people with glaucoma. It is sometimes used to constrict the pupils during cataract surgery.

Topical occular administration is used to decrease intraocular pressure in people with primary open-angle glaucoma. Intraocular administration is used to produce miosis after lens implantation during cataract surgery. Carbachol can also be used to stimulate bladder emptying if the normal emptying mechanism is not working properly.

In most countries carbachol is only available by prescription.

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Contraindications

Use of carbachol, as well as all other muscarinic receptor agonists, is contraindicated in patients with asthma, coronary insufficiency, gastroduodenal ulcers, and incontinence. The parasympathomimetic action of this drug will exacerbate the symptoms of these disorders.

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Overdose

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External links

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References

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