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Pharmacology > Autonomic Drugs > Flashcards

Autonomic Drugs Flashcards

1
Q

Acetylcholine

A
  • direct cholinoceptor agonist; N or M, but doesn’t cross fat
  • rapidly degraded
  • administration: IV, bc not lipophilic, so poorly absorbed in GI tract
  • used for:
    1. Miosis (short-lived ) in eye surgery
    2. provocation test in coronary angiography
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2
Q

Methacholine

A
  • direct cholinoceptor agonist; choline ester; quaternary amine
  • longer half-life
  • used for bronchial challenge
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3
Q

Carbachol

A
  • direct cholinoceptor agonist; choline ester; quaternary amine; topical use; N and M receptors (N
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4
Q

Bethanechol

A
  • direct cholinergic agonst; choline ester; quaternary amine;
  • not susceptible to AChE
  • acts on M3 (used for GI/GU), weak M2
    - used for urinary retention, gastric emptying abnormalities
    - NOT FOR OBSTRUCTION
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5
Q

Muscarine

A
  • direct cholinergic agonist; muscarinic alkaloid; acts on muscarinic recpetors
  • not susceptible to AChE; long half-life; very potent
  • seen in poisoning; not therapeutic
    • salivation, tear flow
    • abdominal pain, nausea, diarrhea, blurred vision
    • resolve within 2 hrs
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6
Q

Pilocarpine

A
  • direct cholinergic agonist; muscarinic alkaoid; tertiary amine with poor systemic absorption
  • topical for eyes
  • M3 predominates; DRUG OF CHOICE FOR GLAUCOMA
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7
Q

Quinidine

A
  • antiarrhythmic

- has antimuscarinic properties

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8
Q

Procainamide

A
  • antiarrhythmic

- antimuscarinic properties

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9
Q

TCAs

A
  • anti-depressant, decreases catecholamine metabolism, increasing concentration at synaptic cleft
  • antimuscarinic properties
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10
Q

Nicotine

A
  • direct cholinoceptor agonist; acts on nicotinic receptors
  • varying effects
    - Nm receptor: depolarizing blockade, Ca++ rushes in, leads to fasciculations, spasm
    - Nn receptors; depends on predominate stimulation
    - Cardiac: increased HR, etc due to catecholamine release from stimulated adrenal medulla
    - Vasculature: peripheral vasoconstriction
    - GI: increased motility, secretion
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11
Q

Contraindications to cholinoceptor agonists

A
  • asthma
  • peptic ulcers
  • GI tract disorders
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12
Q

Edrophonium

A
  • indirect cholinoceptor agonist (AChE inhibitor); used for diagnosis of MG
  • short acting
  • given IV
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13
Q

Neostigmine, pyridostigmine

A
  • indirect cholinoceptor agonist (AChE inhibitor); quaternary amine (no CNS)
  • uses:
    • ileus
    • urinary retention
    • treatment of myasthenia gravis
    • reversal of succinyl choline
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14
Q

Physostigmine

A
  • indirect cholinoceptor agonist (AChE inhibitor); tertiary amine so ENTERS CNS
  • used for:
    • treatment of atropine
    • glaucoma
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15
Q

Donepazil

A
  • indirect cholinoceptor agonist (AChE inhibitor); lipid soluble
  • use for:
    • treatment Alzheimers
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16
Q

Tacrine

A
  • indirect cholinoceptor agonist (AChE inhibitor); lipid soluble
  • use for:
    • treatment Alzheimers
17
Q

Echothiophate

A
  • irreversible AChE inhibitor; lipid soluble, long acting

- is almost poison; instead treats glaucoma

18
Q

Malathion

A
  • irreversible AChE inhibitor; lipid soluble, long acting

- insecticide; v bad. treat with atropine

19
Q

Parathion

A
  • irreversible AChE inhibitor; lipid soluble, long acting

- insecticide; v bad. treat with atropine

20
Q

Sarin

A
  • irreversible AChE inhibitor; lipid soluble, long acting

- this is nerve gas. awkward.

21
Q

Atropine

A
  • is a blocker! tertiary amine (enters CNS); all the different M inhibitors; competes with AChE
  • progression from
    - mydriasis and cycloplegia (can’t accommodate)
    - hyperthermia
    - tachycardia
    - sedation
    - urinary retention
    - hallucination

minimal effect on BP along, because sympathetic tone predominates

uses:

  • antispasmodic
  • anti-secretory
  • anti-diarrheal

if intox:

  • sx
  • physostigmine
22
Q

ipratropium

A

properties: nonselective muscarinic inhibitor, but inhaled affects M3; quaternary amine

Effects: decreases bronchoconstriction, secretions

uses: first for COPD, second for asthma flares

23
Q

benztropine

A

properties: cholinergic inhibitor; tertiary amine so CNS absorption; acts on brain M receptors

Effects: re-establish dopaminergic-cholinergic balance

  • decrease GI/GU secretions
  • increased heart rate

Use:

  • Parkinson’s treatment (2nd line)
  • decrease bad effects antipsychotics
24
Q

hexamethonium, mecamylamine

A

nicotinic cholinergic inhibitors; no longer used because of toxicities

-reduce predominant autonomic tone

25
Q

D-tubocurarine

A

cholinoceptor blocking; non-depolarizing neuromuscular blocker; quaternary amine; competes with ACh

  • intereferes w/ transmission, doesn’t cross membrane
  • small does doens’t enter
  • large dose enters pores
  • can decrease ACh release
  • Use:
  • Paralysis in surgical
  • muscular manifestation of seizures

Sides effects:

  • hypotension d/t histamine release
  • increased IOP
  • increased gastric pressure
  • muscle pain
26
Q

Succinylcholine

A

cholinoceptor antagonist; depolarizing neuromuscular blocker

Sides effects:
- hyperkalemia

27
Q

dobutamine

A
  • doesn’t really change TPR
  • doesn’t damatically increase O2 demand
  • increased inotropy more than chronotropy
28
Q

norepinephrine

A

predominately alpha stim

  • increased BP

Pharmacology (6 decks)

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