Wk 15 - Miotics Flashcards
Parasympathetic pathway
Remember that the ciliary muscle and iris sphincter muscle are controlled by parasympathetic fibers
Preganglionics begin at Edinger-Westphal nucleus in the brainstem, then synapse at ciliary ganglion.
o 3% of postganglionic fibers release Ach onto the iris sphincter muscle, causing pupil constriction
o 97% of postganglionic fibers release Ach onto the ciliary muscle, causing contraction and accommodation
Cholinergic agonists
AKA Miotics AKA parasympathomimetics
• These drugs mimic the parasympathetic effects of acetylcholine
Pilocarpine is the only drug in this class still used to treat glaucoma today o Direct acting – mimics Ach • Opposite effects of the cholinergic antagonists (Mydriatics = ASHCT)
Pilocarpine MOA
MOA
• Mimics Ach at the ciliary muscle and iris sphincter
• Thought that contraction of the ciliary muscle pulls on the scleral spur, widening the trabecular space
• Increases outflow through the trabecular meshwork
• Decreases IOP by 15-25%
o Works slightly better in blue eyes
Pilocarpine Clinical Uses
1) Acute angle-closure glaucoma
o Note that ischemic iris is nonresponsive to pilocarpine at pressures >60 mmHg
o Must use another drug to lower IOP below 60 before using pilocarpine
2) Secondary glaucomas
o Drug of choice for pigmentary glaucoma
o Moves iris away from the lens zonules to prevent rubbing and pigment dispersion
3) Primary open angle glaucoma
o Historical medication
o Rarely used today due to development of safer, more effective drugs
Pilocarpine Solution
Available in concentrations 0.5%, 1%, 2%, 3%, 4%, 6%
Dosing: q4h
• Bad for compliance
o Max effect achieved in a few days
Pilocarpine 4% Gel
Dosing: ½ inch ribbon qhs
o Increased compliance
o Decreased complaints of side effects since they peak while patient sleeps
BUT
Increased risk of retinal detachment
o May combine with a drop in the afternoon if IOP is not lowered consistently through the day
Ocusert Pilo-20/Ocusert Pilo-40
o Inserted into lower fornix
o Releases 20 or 40 ug/hour
Dosing: q7d
-Follows zero order kinetics
• Constant amount of drug delivered, released, and absorbed
• Release controlled by a polymer membrane to decrease systemic overload
Specific Side Effects
o Increased blur during first 12 hours after insertion
• Reduce complaints by inserting at night
o Possible foreign body sensation/discomfort
o May fall out of fornix
• Patient must monitor presence
Pilocarpine Ocular Side Effects
1) Miosis
2) Accommodative spasm and blur
o Especially in patients
Pilocarpine Systemic Side Effects
1) Brow ache
o Especially when beginning treatment
o Caused by miosis and accommodative spasm
o Minimized by starting at a low dose and working up
2) SLUDE
o Salivation, lacrimation, urination, defecation, emesis
o Parasympathetic-type effects
o Rare
3) Tremor
4) Heart
• Bradycardia
• Cardiac arrhythmia
• Hypotension
5) Lungs
• Bronchiolar spasm – rare
• Pulmonary edema
Pilocarpine Contraindications
1) Patients may cause pupillary block
5) Severe asthma
o Respiratory effects
6) Concurrent use with succinylcholine
o An anesthetic – make sure surgeon or anesthesiologist knows if patient is taking this med