Individual Compounds

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Chapter: Essential pharmacology : Cholinergic System And Drugs

Physostigmine eye drops are usually prepared freshly by ophthalmology departments.


INDIVIDUAL COMPOUNDS

 

The important features of physostigmine and neostigmine are presented in Table 7.6.



 

Physostigmine eye drops are usually prepared freshly by ophthalmology departments.

BIMIOTIC 0.25% eye drops with 2% pilocarpine nitrate.


Neostigmine PROSTIGMIN, MYOSTIGMIN, TILSTIGMIN 15 mg tab, 0.5 mg/ml in 1 ml and 5 ml inj.

 

Pyridostigmine Resembles neostigmine in all respects but is dose to dose less potent and longer acting, less frequent dosing is required in myasthenia gravis.

DISTINON, MYESTIN 60 mg tab; 1–3 tab TDS. Ambenonium is another longacting congener used in myasthenia.

 

Edrophonium Resembles neostigmine in action, has a brief duration (10–30 min), suitable as a diagnostic agent for myasthenia gravis and for postoperative decurarization. Dose: 1–10 mg i.v.

 

Tacrine It is a lipophilic acridine compound which interacts with ChE in a manner analogous to edrophonium. It crosses bloodbrain barrier and has a longer duration of action. By increasing brain ACh levels it has been found to produce partial symptomatic improvement in Alzheimer’s disease (AD).

 

Rivastigmine This lipophilic relatively cerebroselective ChE inhibitor has been introduced for AD.

 

Donepezil Another centrally acting antiAChE that has produced cognitive and behavioral improvement in AD. It is longacting and suitable for once daily administration.

 

Galantamine This natural alkaloid inhibitor of cerebral AChE has in addition weak agonistic action on nicotinic receptors. It is being used to afford symptomatic relief in AD.

 

Dyflos It is Diisopropylfluorophosphate (DFP), a very potent and longacting antiChE. It has been used as a miotic (0.025%) but is not preferred because it has to be used as oily solution, causes local irritation.

 

Echothiophate It is an organophosphate with quaternary structure. It is water soluble; local irritancy is low. A 0.025– 0.25% solution is rarely used in resistant cases of glaucoma as it is a potent and longacting (1–3 days) miotic.

 

Precautions AntiChEs are contraindicated in sick sinus, AV conduction defects and hypotensive states. They are to be used cautiously in peptic ulcer, asthma, COPD and seizure patients.

 

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