PHARMY Flashcards

1
Q

Antiglaucoma drugs:

A
  1. B-blockers: First line for POAG > and all others
    inhibit B-adrenergic receptors in ciliary body > decreased aqueous production
    Ocular iritation, corneal desens, DED, macular edema
    Bronchospasm, cough, arrythmia, headache, nausea
    Contra. chronic obstructive PD, asthma, Bradycardia
    1. Non-selective (B-1/2)
      1. Timolol/Levobunolol
        0.25% BID, IOP decreases 25%
    2. Selective (B-1)
      1. Betaxolol
        • Less side effect; less efficacy
  2. Prost-analogues: All but uveitis glauc: Greater IOP reduction, causes inflammtion
    Prodrug metabolized by corneal esterase > binds PGF2a receptor on ciliary muscle > ECM remodeling/MMP regulation > increase uveoscleral outflow
    Iris heterochromia, lid pigmentation, lash lengthening, redness, SPEE
    Contra. Ocular inflammation (HSK), CMO, allergy
    1. Latanoprost (Xalantan)
    0.005% daily, IOP decreased 30%
    1. Bimatoprost (Lumigan): 0.03%
    2. Travoprost (Travatan): 0.004%
  3. Adrenergic-agonist:
    Stimulate A-2 receptors > adenylate cyclase inhibition > decreased cMAP in ciliary cells > aqueous production loss
    Stimulation of A-1 receptor > vasoconstriction of CB vessels > reduced aqueous production
    • Photophobia, blur, stinging
    • Dry mouth, hypotension, fatigue
      1. Apraclonidine: selective A2 (weak A1)
        0.5% BID, IOP decrease 20%
        Causes tachyphylaxis
  4. Carbonic anhydrase inhib: CA is critical for aqueous formation
    Decreases bicarbonate ion formation > reduced fluid transport in ciliary epith.
    Causes blood acidosis, renal stones, metalic taste, confusion
    Contra. Heart/kidney disease
    1. Acetazolamide (Diamox/Diazamide): IV for Rapid IOP decrease, oral otherwise
    250mg BID, 20% decrease by 4h
    500mg IV, 20% decrease by 30min
    1. Dorzolamide (trusopt): topical, fewer systemic affects
      2% 3/d, 20% IOP decrease
  5. Hyperosmotics: ^Plasma osmolarity > fluid uptake from ocular tissue
    Nausea, heart faliure, confusion, kertoacidosis
    Contra. DM
    1. Glycerol: oral dose 4ml/kg
      20 onset, poor ocular penetration
    2. Mannitol: 20%
      Not contra. for renal faliure
  6. Cholinergic agonist: Stimulate muscarinic receptors in CB > Miosis > TM opening > increased outflow
    Accomodative spasm, pupil block, cataract
    Contra. cataract, myopia, young Px
    1. Pilocarpine: 2% QID, 15% IOP decrease
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2
Q

Acyclovir and ganciclovir:

A

Antiviral prodrug, metabolized by viral enzymes to acyclovir/ganciclovir triphosphate
1. Competes with dGTP for incorporation into viral DNA
2. Chain terminator for DNA formation / Faulty DNA replication
Viral enzymes have higher affinity for acyclovir than host cells
- HSV: 3% ointment 5/d (up to 10d)
- HSV: 400mg 5/d (up to 10d)
- HZO: 800mg 5/d (up to 10d)
Ganciclovir has high affinity for cyclomegalovirus enzymes, but also affects host cells moreso than acyclovir

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3
Q

Prednisolone and Dexamethasone:

A

Cortico, lipophilic (^penetration)
1. Binds glucocorticoid receptors in cytoplasm
2. Pred.-GR complex moves to nucleus and regulates gene expression
1. Reduces cytokines (IL-1, TNF-a, INF-y)
2. Inhibits cyclooxygenase-2 expression > reduced mediator synthesis (prostaglandins)
3. Inhibits T/B cell proliferation
Dexamethasone (0.1%) has higher potency for faster response, but greater risk (^IOP more)
Same dosage and taper though, Pred 1% QID, or loading dose hourly 6h

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3
Q

Cyclosporin:

A

Immunosuppressive, used when cortico. non-response or risk
Lipophilic ^Penetration
1. Binds cytoplasmic protein cyclophilin
2. CC complex inhibits calcineurin, which normally
1. Protein phosphate for T-cell activation
2. processes transcription factors for IL-2
Commercially used for organ transplant
Side effects:
- HT, kidney damage

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4
Q

Antiglaucoma drugs:

A
  1. B-blockers: First line for POAG > and all others
    inhibit B-adrenergic receptors in ciliary body > decreased aqueous production
    Ocular iritation, corneal desens, DED, macular edema
    Bronchospasm, cough, arrythmia, headache, nausea
    Contra. chronic obstructive PD, asthma, Bradycardia
    1. Non-selective (B-1/2)
      1. Timolol/Levobunolol
        0.25% BID, IOP decreases 25%
    2. Selective (B-1)
      1. Betaxolol
        • Less side effect; less efficacy
  2. Prost-analogues: All but uveitis glauc: Greater IOP reduction, causes inflammtion
    Prodrug metabolized by corneal esterase > binds PGF2a receptor on ciliary muscle > ECM remodeling/MMP regulation > increase uveoscleral outflow
    Iris heterochromia, lid pigmentation, lash lengthening, redness, SPEE
    Contra. Ocular inflammation (HSK), CMO, allergy
    1. Latanoprost (Xalantan)
    0.005% daily, IOP decreased 30%
    1. Bimatoprost (Lumigan): 0.03%
    2. Travoprost (Travatan): 0.004%
  3. Adrenergic-agonist:
    Stimulate A-2 receptors > adenylate cyclase inhibition > decreased cMAP in ciliary cells > aqueous production loss
    Stimulation of A-1 receptor > vasoconstriction of CB vessels > reduced aqueous production
    • Photophobia, blur, stinging
    • Dry mouth, hypotension, fatigue
      1. Apraclonidine: selective A2 (weak A1)
        0.5% BID, IOP decrease 20%
        Causes tachyphylaxis
  4. Carbonic anhydrase inhib: CA is critical for aqueous formation
    Decreases bicarbonate ion formation > reduced fluid transport in ciliary epith.
    Causes blood acidosis, renal stones, metalic taste, confusion
    Contra. Heart/kidney disease
    1. Acetazolamide (Diamox/Diazamide): IV for Rapid IOP decrease, oral otherwise
    250mg BID, 20% decrease by 4h
    500mg IV, 20% decrease by 30min
    1. Dorzolamide (trusopt): topical, fewer systemic affects
      2% 3/d, 20% IOP decrease
  5. Hyperosmotics: ^Plasma osmolarity > fluid uptake from ocular tissue
    Nausea, heart faliure, confusion, kertoacidosis
    Contra. DM
    1. Glycerol: oral dose 4ml/kg
      20 onset, poor ocular penetration
    2. Mannitol: 20%
      Not contra. for renal faliure (no renal metabolism)
  6. Cholinergic agonist: Stimulate muscarinic receptors in CB > Miosis > TM opening > increased outflow
    Accomodative spasm, pupil block, cataract
    Contra. cataract, myopia, young Px
    1. Pilocarpine: 2% QID, 15% IOP decrease
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5
Q

Chemotherapeutic agents topical:

A

Indicated for OSSN as corneal extension or contacting more than half the limbus
Mitomycin C (0.02%): inhibits DNA/protein synthesis, cell migration, ECM production
- causes hyperemia, punctate erosions, DED
5-fluorouracil (1%): inhibits thymidylate synthetase, DNA/RNA syntesis
- causes conj. hyperemia, lid erythema
Interferon a2b 1million IU/ml: anti-microbial
- causes SPEE, follicular conjunctivitis

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6
Q

50S subunit drugs:

A

Antibacterial, binds 50s ribosomal subunit, inhibiting peptide formation
- Chloramphenicol
- Azithromycin
- Erythromycin .5%

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7
Q

Quinolones:

A

BS antibacterial
Inhibition of topoiosomerase-2 (DNA gyrase) and topoisomerase 4 > transcription/replication loss
- Ciprofloxacin .3%
- Ofloxacin .3%
- moxifloxacin

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8
Q

30S subunit drugs:

A

Aminoglycosides: bactericidal via faulty protein synthesis
- Gentamicin: Gram-ve species
- Tobramycin .3%
- Framycetin
Tetracyclines: Bacteriostatic via inhibited protein synthesis
- Tetracycline: alternate trachoma management
- Doxycycline

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9
Q

NSAIDs

A

COX enzyme inhibition > loss of prostaglandin synthesis
- Ketorolac .5 QID
- Diclofenac .1%

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