What was the 1st glaucoma drug invented?
Pilocarpine
NOTE: short half life so need frequent admin (QID). Reduces pressures by 30%
MOA of Pilocarpine?
(+) longitudinal muscles of CB (corneo-scleral pathway) –> pulls posteriorly on scleral spur & secondarily opens up trabecular spaces for INC outflow & DEC IOP
Pilocarpine is considered what kind of drug?
Direct cholinergic agonist
Uses for pilocarpine?
ADEs of pilocarpine?
Neostigmine, edrophonium, echothiophate, and pyridostigmine are considered what kind of medications?
Indirect Cholinergic Agnoists: Anti-cholinesterase agents
NOTE: this is considered “indirect” bc it inhibits AchE which is the enzyme that breaks down ACh
Which is the most dangerous cholinergic antagonist?
Scopolamine
NOTE: similar clinical indications as atropine but rarely used side effects
ADEs of scopolamine?
Hallucinations, amnesia, unconsciousness, confusion, restlessness, incoherence, vomiting, urinary incontinence
Major actions of parasympathetic nervous system?
Major actions of sympathetic nervous system?
What receptors are on the iris sphincter?
M3
Effect = miosis
RECALL: the iris muscles develop from NEURAL ECTODERM
What receptors are located on the ciliary muscle?
M2, M3
Effect = accommodation
RECALL: ciliary muscles develop from the neural crest. Abnormal neural crest development –> irregular iridocorneal adhesions
What receptors are located on the lacrimal gland?
M2, M3
Effect = tear production
RECALL: lacrimal gland is derived from surface ectoderm. Surface ectoderm gives rise to “surface” structures.
What receptor is located on the iris dilator?
a. Alpha 1
b. Alpha 2
c. Beta 1
d. Beta 2
e. M2
f. M2 & M3
a. Alpha 1
RECALL: Alpha 2 --> CB vasculature Beta 1 /2 --> NPCE Beta 2 + M2/M3 --> Ciliary muscles, TM M3 --> Iris sphincter M2/M3 --> Lacrimal gland
What receptors are located on the Ciliary Muscles & Trabecular meshwork?
Ciliary Muscles: M2/M3 + Beta 2
Trabecular Meshwork: Beta 2
Beta 2 agonists cause what to the TM & CM & NPCE?
RELAXATION
INC outflow & DEC Accommodation & INC IOP
Which cholinergic antagonist works the fastest and has the shortest duration of MYDRIATIC effect?
Tropicamide
What are the ADEs of Atropine?
1 is DRY MOUTH
Dry skin
Rapid pulse
Disorientation
Fever due to CNS effects of hypothalamus
NOTE: do NOT give to pts w DOWN’s SYNDROME, small children, and elderly
Which anti-cholinergic antagonist has the fastest onset & shortest duration of CYCLOPLEGIC effects?
Cycloplentolate
NOTE: this drug is the standard for cycloplegia in clinic
Which anti-cholinergic antagonist is the standard for Treating ANTERIOR Uveitis?
Homatropine
Which medication is a SOMATIC drug that blocks the release of ACh at the neuromuscular junction, inhibiting muscle contractions?
Botulin A Toxin (Botox)
Single injections have been effective in providing permanent correction for strabismus; cosmetic wrinkles
Used in blepharospasm Tx but effects only laast a couple hours
What are the uses of adrenergic agonists?
What receptors does Norepinephrine act on?
A1 (dilator)
A2 (CB vasculature)
B1 (NPCE + heart)
NOT B2
What receptors does Epinephrine act on?
A1 (dilator)
A2 (CB vasculature)
B1 (NPCE + heart)
B2 (Lungs)