Pharmacology Flashcards

1
Q

Muscarinic receptors in the eye

A

Sphincter and ciliary mm

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2
Q

Adrenergic receptors in the eye

A

Dilator (alpha) and ciliary epithelium (beta)

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3
Q

Sphincter pupillae

A
  • Contraction causes MIOSIS

- Contraction mediated by ligand/agonist at M3 receptors (Gq»IP3»Ca2+)

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4
Q

Ciliary muscle

A
  • M3 induced contraction causes:
  • Accomodation
  • Cyclospasm
  • Increased tension on trabecular meshwork
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5
Q

Dilator pupillae

A
  • Alpha1 receptors induce contraction causing MYDRIASIS

- Gq»IP3»Ca2+

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6
Q

Increased production of aqueous humor secretion

A

B-adrenergic receptors (Gs)»increased cAMP»increased secretion

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7
Q

Decreased production of aqueous humor secretion

A

Alpha2-adrenergic receptors (Gi)»decreased cAMP»decreased secretion

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8
Q

Carbonic anhydrase

A
  • Mediates the transport of bicarbonate across the ciliary epithelium by the reversible hydration of CO2to form HCO3- and protons
  • Influences fluid transport by affecting Na+
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9
Q

Open-Angle glaucoma

A
  • Optic neuropathy characterized by progressive peripheral visual loss followed by central visual field loss
  • ↑ IOP is common, but not always present
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10
Q

Angle-closure glaucoma

A

-Narrowing or closure of the anterior chamber angle
-Impairment of drainage&raquo_space; increased IOP and damage to optic nerve
(Normal anterior chamber angle provides drainage for aqueous humor)

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11
Q

Symptoms of open-angle glaucoma

A

Symptoms rare and often diagnosed during eye exams

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12
Q

Symptoms of angle-closure glaucoma

A

Redness, pain (mild»severe), blurred vision, tearing, photophobia, N/V, headache, halos around light

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13
Q

Open-angle glaucoma treatment

A
  • Topical
  • -Increase aqueous outflow
  • –Prostaglandins
  • –Muscarinic agonists
  • –Alpha-2 adrenergic agonists
  • –rho kinase inhibitor
  • -Decreasing aqueous production
  • –Alpha-2 adrenergic agonists
  • –Beta blockers
  • –Carbonic anhydrase inhibitors (less effective therapy)
  • Systemic
  • -Decreasing aqueous production
  • –Carbonic anhydrase inhibitors
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14
Q

Angle-closure glaucoma treatment

A

Acute setting:

  • Treated initially with drugs to reverse or reduce IOP
  • -Topical pressure lowering agents
  • –Beta-blockers
  • –Alpha-2 agonists
  • –Muscarinic agonists
  • -Systemic medications
  • –Carbonic anhydrase inhibitors
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15
Q

Modifying autonomic signaling for treatment of glaucoma

A
  • Cholinergic agonists and AChE inhibitors enhance aqueous outflow
  • Beta-adrenergic antagonists and alpha-adrenergic agonists decrease aqueous inflow
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16
Q

PGDs

A

Latanoprost
Bimatoprost
-increase outflow of aqueous humor
-topical use for treatment of open angle glaucoma (more effective than beta-blockers)

17
Q

Beta-blockers

A
Betaxolol (beta-1)
Carteolol (non)
Levobunolol (non)
Metipranolol (non)
Timolol (non)
-Decrease aqueous humor production
18
Q

Alpha-2 adrenergic agonists

A

Apraclonidine
Brimonidine
-Topical agents with similar effectiveness to beta blockers in lowering IOP in open-angle glaucoma (useful for treating normal pressure glaucoma)
MOA: Inhibiting release of catecholamine&raquo_space; decreasing aqueous humor production
-Brimonidine may also increase outflow

19
Q

Muscarinic agonists

A

Pilocarpine

  • topical
  • Causes contraction of the sphincter pupillae (miosis) and ciliary muscle (loss of accommodation)
  • Lowers IOP - decreases resistance to aqueous humor outflow
  • Used in open-angle and angle-closure glaucoma
20
Q

Carbonic anhydrase inhibitors

A

Acetazolamide
Dorzolamide
-Both agents decrease production of aqueous humor by inhibiting carbonic anhydrase

21
Q

Netarsudil

A

-Topical agent
-Mechanism:
rho kinase inhibitor
-believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork

22
Q

Adverse effects of beta-blockers

A

Stinging of eyes
Conjunctival hyperemia
Limited – asthma, nodal issues

23
Q

Adverse effects of beta-blockers

A

Stinging of eyes
Conjunctival hyperemia
Limited – asthma, nodal issues

24
Q

Alpha-agonists adverse effects

A

Allergic conjunctivitis, hyperemia, ocular pruritus

25
Q

Adverse effects of muscarinic (cholinergic) agonists

A

DUMBELS
diarrhea, urination, miosis and muscle weakness, bronchospasm, excitation, lacrimation, and seizures, sweating, and salivation

26
Q

Acetazolamide

A
  • Systemic administration
  • -Mostly replaced by topical agents
  • Inhibits carbonic anhydrase to increase HCO3- excretion in the urine
27
Q

Dorzolamide

A
  • Topical administration

- Does not appear to be as effective in treating open-angle glaucoma compared with other pharmacologic therapies

28
Q

Adverse effects of netarsudil

A

Application site pain
Conjunctival hyperemia
Conjunctival hemorrhage

29
Q

Drug combinations

A
  • Combining drugs can cause greater reduction in the IOP after failed monotherapy
  • -Carbonic anhydrase inhibitor + a-agonist
  • -a-agonist + b-blocker
  • -b-blocker + carbonic anhydrase inhibitor