Ophthalmic Drugs Flashcards
What are the receptors of the Iris Sphincter?
- Muscarinic
2. Few Alpha and Beta
What are the receptors of the Ciliary Muscle?
- Muscarinic
2. Some Beta 1
What are the receptors of the Iris Dilator?
- Mostly Alpha 1
2. Few Beta
What are the receptors of the Ciliary Process?
- Mostly Beta 2
- Some Alpha 2 and Beta 1
- Muscarinic
What are the receptors of Mueller’s Muscle?
- Alpha 1
Which ocular muscles are mainly parasympathetic?
- Iris Sphincter
2. Ciliary Muscle
Which ocular muscles are mainly sympathetic?
- Iris Dilator
- Ciliary Process
- Mueller Muscle
What are 3 functions of Adrenergic Agonists for the eye?
- Mydriasis
- Treatment of Glaucoma
- Decongestant
What is Epinephrine?
An Alpha 1,2 and Beta 1,2 Adrenergic Agonist
What are the ocular uses of Epinephrine?
- Vasoconstriction
2. Glaucoma (not much anymore)
How does Epinephrine work to treat Glaucoma?
Alpha 1 and Beta 2 –> Increased Aq Production, but Beta 2 also increases Aq Outflow –> Decreased IOP
What are the side effects of Epinephrine?
- HA
- Hyperglycemia
- Tachycardia
- HTN
- Thyrotoxicosis
What are the ocular side effects of Epinephrine?
- Dilation
- Lid Retraction
- Lacrimation
- Pigmentation of the Iris/Lens (w/ Oxidized Epinephrine)
- Angle Closure
- Increased IOP
- Cystoid Macular Edema
What is significant about the cystoid macular edema caused by Epinephrine?
It can –> swelling of central part of the retina –> blindness if not treated early
What is Phenylephrine?
A Direct Alpha 1 Agonist
What are the ocular uses of Phenylephrine?
- Mydriasis
- Decongestant
- Breaking Posterior Synchia to the lens
How long does Mydriasis occur with Phenylephrine?
Onset- 1hr
Duration- 7hrs
What drug is commonly used for DFE?
Phenylephrine
What is the role of the decongestant use of phenylephrine?
To differentiate Episcleritis from Scleritis
What are the ocular side effects of Phenylephrine?
- Lid Retraction
- Lacrimation
- Angle Closure
Why is phenylephrine not used for narrow angle dilation?
Because phenylephrine may –> Angle Closure, and it is harder to reverse its mydriasis
Which drug class worsens the sympathomimetic side effects of Phenylephrine?
MAOIs
Does Phenylephrine induce Cycloplegia?
No- because the ciliary body muscle has few Alpha receptors
Is the Active Light reflex present with Phenylephrine?
Yes- because the Parasympathetics to the Iris Sphincter are still intact
What is Apraclonidine?
Direct Alpha Adrenergic Agonist; some specificity for Alpha 2
What is the ocular use of Apraclonidine?
- Treatment of glaucoma
- Fast reduction of High IOP
- Pre and Post-Op Glaucoma/Laser Treatment
How long does the reduction of IOP with Apraclonidine last?
3-5 hours - but fast acting
Why is Apraclonidine not used for long term use?
Significant Drift
What are the 3 Mechanisms by which Apraclonidine reduces IOP?
- Binds presynaptic A2 receptrs –> Decreased NE, so less stimulation of B2 on the Ciliary Process –> Decreased Aq Production
- Binds postjunctional A2 receptors in the Epithelium of the Ciliary Process –> reduction of intracellular cAMP –> Decreased Aq Production
- Binds A2 receptors on the episcleral veins –> Dilation –> increased Aq outflow through the uveoscleral pathway
What are the side effects of Apraclonidine?
Dry Mouth, HA, Lethargy
What are the ocular side effects of Apraclonidine?
- Allergic RXN and Red Eyes
2. Mydriasis, Conjunctival Vascular Constriction, Lid Retraction (mild- due to some Alpha 1 Stimulation)
What is Brimonidine?
A Direct acting Alpha 2 Agonist (Highly Selective)
What is the treatment for Normal Tension Glaucoma?
Brimonidine
What is the secondary function of Brimonidine?
Primary Open Angle Glaucoma
How does Brimonidine similar/different from Apraclonidine?
Similar- Reduces IOP (same mechanism)
Different- Less long term drift (b/c more selective for Alpha 2), less Allergic RXN
What are the side effects of Brimonidine?
- Dry Mouth
- HA
- Lethargy
What are the ocular side effects of Brimonidine?
- Allergic RXN (less severe than Apraclonidine)
* *No Alpha 1 effects because so selective
What are the Direct Acting Adrenergic Agonists?
- Norepinephrine
- Epinephrine
- Phenylephrine
- Apraclonidine
- Brimonidine
What are the Indirect Adrenergic Agonists?
- Cocaine
2. Hydroxyamphetamine
What is the MOA of Cocaine?
Blocks NE reuptake
What is the use of Cocaine?
Diagnosis of Horner’s Syndrome
What is Horner’s Syndrome?
- Loss of sympathetics
1. Miosis - Loss of Iris Dilator FXN
2. Ptosis- Mild eyelid droop (loss of Mueller’s, but LPS and CNIII still ok)
3. Anhydrosis- loss of sweat gland FXN
What will be the result of Cocaine admin in a Horner’s eye or a Normal eye?
Normal- dilation
Horner’s- Nothing
What is the MOA of Hydroxyamphetamine?
Stimulates NE release onto the Iris Dilator from Presynaptic terminals of Post-Ganglionic Neurons
If Horner’s Syndrome is PRE-ganglionic, what is the result of Hydroxamphetamin admin? What are possible causes?
- Pupil dilates
- Causes of Pre-Ganglionic Horner’s: Pancoast Tumor, Thoracic Aortic Aneurysm, S/P Carotid Endarterectomy
If Horner’s Syndrome is POST-ganglionic, what is the result of Hydroxamphetamin admin? What are possible causes?
- No Pupil Dilation
- Goiter, Cavernous Sinus Syndrome
Which drug is an Alpha Blocker?
Dapiprazole
What is the function of Dapiprazole?
Reverse mydriasis
What is the MOA of Dapiprazole?
Competitively binds to post-synaptic receptors of the iris dilator muscle
What are the side effects of Dapiprazole?
- Hyperemia (Blocks Alpha 1)
2. Mild Ptosis (blocks Mueller’s)
What is Timolol?
A non-specific Beta-Blocker
What is the ocular use of Timolol?
Treatment of Glaucoma
What is the MOA of Timolol?
Blocks B Receptors at the Ciliary Process which results in decreased Aq production –> decreased IOP
What does Beta stimulation cause at the Ciliary Process and what is the mechanism?
Increased Aq production through adenylate cyclase/cAMP pathway
What are 4 factors that make Timolol the first line for glaucoma treatment?
- No Intrinsic Sympathomimetic Activity
- No Pupil dilation
- Does not bind to melanin
- Only mild long-term drift
What are Levobunolol and Metripranolol?
Non-specific Beta Blockers (work similar to Timolol)
What drug has the same function but a longer duration than Timolol?
Levobunolol
What are the side effects of the Beta Blockers?
- Bradycardia, conduction arrhythmias (B1)
- Respiratory depression/bronchodilation (B2)
- Worsens Myasthenia Gravis
- Depression
Beta Blockers are contraindicated in which patients?
- CHF
2. COPD/Bronchitis and Asthma
What are the ocular side effects of Beta Blockers?
- Corneal Anesthesia
What are the non-selective Beta Blockers?
- Timolol
- Levobunolol
- Metipranolol
- Carteolol
What is the B1 selective Beta Blocker?
Betaxolol
What is the advantage of Betaxolol over the non-selective Beta Blockers?
Can be used in COPD/Asthma patients
Betaxolol is contraindicated in which patients?
Patients with cardiac issues
How is the potency of betaxolol?
Lower than non-selective Beta Blockers, because there are significantly fewer B1 receptors in the Ciliary Process
What is Carteolol?
A non-selective Beta Blocker
What is the MOA of Carteolol?
It has Intrinsic Sympathomimetic Activity and competes with NE and EPI in binding to Beta receptors at the Ciliary Process- but it has only 1-2% efficacy of NE and EPI, so it results in a decreased activity
Which structures are mainly innervated by Parasympathetics (Muscarinic Receptors)?
- Iris Sphincter
2. Ciliary Muscle
Which structures are mainly innervated by Sympathetics (Adrenergic Receptors)?
- Iris Dilator
- Ciliary Process
- Mueller Muscle
Which structures mostly have A1 receptors?
- Iris Dilator
2. Mueller Muscle
Which structure mostly has B1 receptors?
- Ciliary Process
What is Pilocarpine?
A direct acting Cholinergic Agonist- selective for Muscarinic
Why is pilocarpine long lasting?
It is not susceptible to AchE
What is the primary usage of Pilocarpine, and what is its MOA?
- Acute treatment of Angle Closure Glaucoma
- stimulates Iris Sphincter Muscle –> Miosis –> pulls iris out of angle –> allows Aq drainage
How is Pilocarpine used in the treatment of POAG?
Stimulates Muscarinic R of Ciliary Muscle –> pulls on trabecular meshwork to widen it –> increased Aq outflow
What are the side effects of Pilocarpine?
- HA
- Bradycardia
- Hypotension
- Bronchoconstriction and PE
- Mental Status Changes
What are the ocular side effects of Pilocarpine?
- Blurred Vision- distance
- Accommodative Spasm
- Miosis
What are the three direct acting Cholinergic Agonists?
- Pilocarpine (M)
- Acetylcholine (M=N)
- Carbachol (M=N)
What is the ocular effect of Acetylcholine?
Miosis- lasting about 25mins
Why is Acetylcholine not frequently used?
Rapid metabolism by AchE
What is the ocular use of Carbachol?
Miosis (up to 24hrs) used in complicated cataracts surgeries
What are the indirect acting Cholinergic agonists?
- Short Acting- Physostigmine and Neostigmine
2. Long Acting- Ecothiophate and Isoflurophate
What is the MOA for the Indirect Acting Cholinergic Agonists?
Inhibit Acetylcholinesterase
Why are Ecothiophate and Isoflurophate not commonly used?
Excessive side effects:
- Accelerated cataract formation
- Increased risk of retinal detachment
- Iris Cysts
- Diarrhea, Nausea and Vomiting
What effects do Cholinergic Antagonists have?
- Mydriasis (Inhibits Iris Sphincter)
- Cycloplegia (Inhibit Ciliary Muscles)
- Pain Relief for Uveitis/Inflammation (Inhibition of Ciliary Muscle Movement and reduces risk of Posterior Synechia to the lens)
What is the clinical use of Cycloplegia?
- Accurate refraction in Hyperopes
2. Vision therapy in Accommodative Esotropia
What are the Cholinergic Antagonists (Anti-muscarinics)?
- Tropicamide
- Cyclopentolate
- Homatropine
- Atropine
What are the features and uses of Tropicamide?
- Good Mydriasis (20-30mins, lasts 4hrs)
- No Cycloplegia
* *Used for DFE
What are the features and uses of Cyclopentolate?
- Great Mydriasis (15-30mins, lasts 24hrs)
* *surgical dilation - Good Cycloplegia
* *refraction in Hyperopes
What are the features and uses of Homatropine?
- Great Mydriasis and Cycloplegia (1-30mins, lasts 48hrs)
* *Used in pain relief for inflammation
What are the features and uses of Atropine?
- Extreme Mydriasis and Cycloplegia (30-40mins, last 7-12 DAYS)
* *DFE in infants and children, vision therapy for accommodative seotropia)
Atropine is contraindication in which patients?
Down Syndrome and Glaucoma Patients
What are the side effects of anti-muscarinics?
- Tachycardia
- Dry Mouth
- Fever
* Worse with Atropine, minimal with Tropicamide
What is the ocular side effect of Atropine (and to a lesser extent the other anti-muscarinics)?
Increased IOP