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KMK Ocular Pharm > 2 - Autonomic Drugs > Flashcards

2 - Autonomic Drugs Flashcards

1
Q

Basics: SNS vs PNS

  • location of cell bodies
  • pre vs post ganglionic
  • receptor types
A

SNS: thoraco-lumbar, shorter pre-gang, releases epi/norepi, alpha/beta receptors

PNS: cranio-sacral, longer pre-gang, releases ACh, muscarinic receptors

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2
Q

Cholinergic receptors in the eye

A

Iris sphincter (M3) = miosis

Ciliary muscle (M2/3) = accommodation

Lacrimal gland (M2/3) = tear production

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3
Q

Adrenergic receptors in the eye

A

Iris dilator (a1) = dilation
TM (B2) = relaxation, incr outflow
Ciliary muscle (B2) = relaxation (opposes accomm)
NPCE (B2, some B1) = incr AH formation
CB vasculature (a2) = constricts, reducing AH formation

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4
Q

Ocular cholinergic agonists

  • promote __ acitivity
  • 3 main structures that rec’v this innerv
  • therapeutic uses
A

PNS

Sphincter, ciliary muscle, lacrimal g

Tx of glaucoma and accomm ET, less commonly for miosis prior to surgery or for pupillary testing

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5
Q

Pilocarpine

  • type of drug
  • use and effectiveness
A

Direct cholinergic agonist (PNS)

Decr IOP, 30% reduction

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6
Q

Pilocarpine

  • MOA
  • uses
A

Stimulate longitudinal muscle of CB -> pulls posteriorly on SS -> opens TM for incr corneoscleral outflow and decr IOP

After an angle closure attack (e.g. IOP is in low 20s)
Preparation for LPI
Fixed dilated pupil: 1% used to differentiate 3rd nerve palsy (will constrict) from sphincter tear
Acute dilated pupil: 0.125% diagnoses ADie’s (will constrict due to supersensitization)

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7
Q

Pilocarpine

-main SE

A

Browache/HA and myopic shifts - a ton of accomm turned on
Miosis
Cataracts: long-term use
RDs: rare, due to retinal break -> detachment from ciliary muscle pulling on ora
Secondary angle-closure: contraction of ciliary m + secondary relaxation of lens zonules -> lens moves anteriorly
Pupillary block: combo of forward movement and myopic shift, etc.

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8
Q

Edrophonium

  • type of drug
  • MOA
  • use
A

Indirect cholinergic agonist (PNS)

AChase inhibitor = incr ACh

Diagnosis of Myasthenia Gravis

  • rapid onset (30-60s), short duration (10m)
  • if ptosis improves 1-2m after injection = (+) for MG
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9
Q

Neostigmine

  • type of drug
  • MOA
  • use
A

Indirect cholinergic agonist (PNS)

AChase inhibitor = incr ACh

Treatment of Myasthenia Gravis
-also limb strength eval in MG suspects

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10
Q

Echothiophate

  • type of drug
  • MOA
  • use
A

Indirect cholinergic agonist (PNS)

Irreversible AChase inhibitor = incr ACh

Diagnosis/treatment of accommodative ET
Rarely used for glaucoma

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11
Q

Pyridostigmine

  • type of drug
  • MOA
  • use
A

Indirect cholinergic agonist (PNS)

AChase inhibitor = incr ACh

Treatment of Myasthenia Gravis

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12
Q

Recall ocular characteristics of Myasthenia Gravis

A

Ptosis - worse with BBs

Diplopia worse at end of the day

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13
Q

Drug that’s administered IV to reverse effects of irreversible AChase inhibitors

Drug that’s administered to reverse muscarinic effects of reversible AChase inhibitors

A

Pralidoxime/Protopam

Atropine

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14
Q

Ocular cholineric antagonists

  • mnemonic to remember all
  • mnemonic for order of cyclo and mydriatic effects
  • MOA for all
  • SE for all
  • toxicity
A

STop ACH

ASH CiTy

Bloch ACh at muscarinic sites in CB/iris

Dry eye, mydriasis, incr IOP

Hot as a hare, red as a beet, dry as a bone, mad as a hatter, blind as a bat

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15
Q

Scopolamine

  • type of drug
  • use
  • SE
  • contraindications
A

Cholinergic antagonist (decr PNS)

Similar to atropine, but rarely used due to severe SE

CNS toxicity (penetrates BBB)= hallucinations, amnesia, unconsciousness, confusion, incoherence, vomiting, urinary incontinence

Same as atropine

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16
Q

Tropicamide

  • type of drug
  • use
  • SE
  • contraindications
A

Cholinergic antagonist (decr PNS)

Dilation: fastest onset (25m) and shortest duration (6h), stronger mydriatic than cycloplegic
-cycloplegic effects are dose-dependent, mydriatic are not

Very safe overall

17
Q

Atropine

  • type of drug
  • use
  • SE
  • contraindications
A

Cholinergic antagonist (decr PNS)

Treatment of uveitis (homatropine better here)
Amblyopia penalization: mild-mod (acuity 20/100 or better)
Too prolonged for routine dilation: onset 60-180m, duration 7-12 days

Safe if correctly dosed
Toxicity = dry mouth (1st sign), dry flushed skin (vasoconstriction), rapid pulse, disorientation, fever (CNS hypothalamus effects)
-think SNS effects for toxicity

Special caution in pts with Down’s syndrome, small children, elderly

18
Q

Cyclopentolate

  • type of drug
  • use
A

Cholinergic antagonist (decr PNS)

Cycloplegia: fastest onset (45m) and shortest duration (24h)
-better than homatropine, similar overall effects to atropine
-mydriasis max at 45m
Tx of anterior uveitis + synechiae prevention

19
Q

Homatropine

  • type of drug
  • use
A

Cholinergic antagonist (decr PNS)

Standard for tx anterior uveitis

  • dilates pupil + keeps it mobile = prevents synechiae
  • paralyzes ciliary/sphincter m = reduces pain
  • constricts iris/ciliary vasculature = stabilizes BAB, limit cells/flare

Prolonged mydriatic and cycloplegic (weak cyclo)

20
Q

Botulina toxin

  • type of drug/MOA
  • use
A

Somatic drug, blocks ACh release at NMJ to inhibit muscle contraction

Blepharospasm treatment - temporary (few mo)
Strabismus correction - permanent

21
Q

Phenylephrine

  • type of drug
  • MOA
  • uses (4)
  • 10% use, SE, contraindications
A

Adrenergic agonist (SNS)

Alpha1 agonist

Dilation of radial muscle without cycloplegia

  • 2.5% used with tropicamide for routine dilation
  • in isolation cannot produce fixed dilation

Palpebral widening: acts on Mullers, good for BIO

Differentiate scleritis and episcleritis: blanching of conj vessels

Horners diagnosis: 1%

10% = Breaking posterior synechiae

  • limited due to adverse CV effects (HTN, arrhythmia)
  • contra: MAOIs, TCAs, atropine, Grave’s disease
22
Q

Naphazoline

  • type of drug
  • MOA
  • use
  • SE
A

Adrenergic agonist (SNS)

Alpha > beta effects

Topical ocular decongestant - constrict conj BVs

Potential to depress CNS

23
Q

Tetrahydrozoline

  • type of drug
  • MOA
  • use
  • SE
A

Adrenergic agonist (SNS)

Alpha > beta effects

Topical ocular decongestant - constrict conj BVs

Potential to depress CNS
Fixed dilated pupil due to alpha effects on radial muscle

24
Q

Brimonidine

  • type of drug
  • MOA
  • use
  • SE
  • contraindications
A

Adrenergic agonist (SNS)

Highly selective alpha2 agonist = decr AH production, incr uveoscleral outflow

Glaucoma (TID, short duration): IOP lowering + long-term use
-neuroprotective properties shown in crushed rat nerve model
Miosis: reduce glare, halos, other night vision symp post-refractive surgery

Follicular conj-itis: largely eliminated SE with Alphagan-P (purite preservative)
Systemic = dry mouth

MAOIs

25
Q

Apraclonidine

  • type of drug
  • MOA
  • use
  • SE
A

Adrenergic agonist (SNS)

Alpha2 agonist
Weak alpha1 = only dilates if Horner’s

Control IOP spikes before/after ocular surgery
Acute angle closure attack: rapid, potent decr in IOP
-IOP reduces 30-40%
-onset 1h, peak 3-5h
-not effective in chronic therapy due to SE
Diagnosis of Horner’s

Tachyphylaxis: loses efficacy over time
Long-term use =allergic response

26
Q

Horner’s diagnosis

A

1) cocaine = no dilation, apraclonidine = dilation

2) hydroxyamphetamine = dilate if preganglionic, phenylephrine = no dilation if preganglionic

27
Q

Beta-blocker effects

  • CNS
  • CV
  • pulmonary
  • GI
  • reproductive
A

Fatigue, disorientation, depression

Bradycardia, arrhythmia, syncope

Bronchoconstrict = dyspnea, wheezing, spasm

Nausea, vomiting, diarrhea, ab pain

Erectile dysfunction

28
Q

MOA of beta adrenergic receptor blockers for glaucoma

A

Block B2 at NPCE to decr AH production

29
Q

Timolol

  • type of drug
  • MOA
  • use
  • dosing
  • SE/pharmacokinetics
  • contraindications
A

Adrenergic antagonist (decr SNS)

Non-selective BB

Most effective at lowering IOP (~25%)

  • unstable
  • also available in gel form as timoptic xe

0.25% once daily in the morning

Crossover effect (unique!): reduces IOP in contralateral eye
Long-term drift: extended use -> IOP gradually rises
Short-term escape: IOP initially lowers, but returns to normal within weeks of starting therapy

Caution in diabetes (masks hypoglycemia), hyperthyroidism (masks signs/symp), and myasthenia gravis (exacerbate fatigue)

30
Q

Timolol combo drugs available

A

Cosopt = timolol 0.5% + dorzolamide 2.0%

Combigan = timolol 0.5% + brimonidine 0.2%

Both dosed Q12h

31
Q

Carteolol

  • type of drug
  • MOA
  • use
  • SE
A

Adrenergic antagonist (decr SNS)

Non-selective BB

Not used clinically, poor IOP reduction vs other BBs
Intrinsic sympathomimetic activity: reduce nocturnal bradycardia, generally less stinging than timolol
Modest reduction in cholesterol (very small)

Potentially less SE than other BBs

32
Q

Betaxolol

  • type of drug
  • MOA
  • use
  • SE
A

Adrenergic antagonist (decr SNS)

Cardioselective B1 blocker
-limits risk of respiratory effects

Questionable neuroprotective qualities
Overall less effective than timolol

Can worsen CHF

33
Q

Levobunolol

  • type of drug
  • MOA
  • use
A

Adrenergic antagonist (decr SNS)

Non-selective BB

Similar to timolol in effectiveness

34
Q

Metipranolol

  • type of drug
  • MOA
  • use
A

Adrenergic antagonist (decr SNS)

Non-selective BB

Not used due to ineffectiveness vs other BBs

KMK Ocular Pharm (9 decks)

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