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Autonomic System Pharmacology > Parasympathomimetic/ Cholinergic Agonist > Flashcards

Parasympathomimetic/ Cholinergic Agonist Flashcards

1
Q

Drugs acting on both nicotinic and M receptor

A

Ach, carbachol

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2
Q

Only muscarinic drugs

A

Muscarine
Pilocarpine
Bethanecol

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3
Q

Only Nicotinic drugs

A 
Nicotine
Succinylcholine (over stimulation-constant depolarisation- unresponsiveness)
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4
Q

AchI drugs

A

Neostigmine
Pyridostigmine
Edrophonium
Physostigmine(tertiary anime-naturally occurring)

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5
Q

Drugs that block nicotinic receptors in skeletal muscles

A

Tubocurarine

Other curare drugs

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6
Q

Block N receipts at ganglion

A

Trimethapan

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7
Q

Ach rarely used clinical why

A
  1. Oral administration- rapid hydrolysis

2. IV administration- rapid metabolism

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8
Q

treatment for postop/ neurogeni ileus and urinary retention

A

cholinergic drugs: bethanechol, carbachol

AchE inhibitors: neostigmine, pyridostigmine

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9
Q

used to diagnose type of myastina gravis and its features

A

small dose of Endophonium used to distinguish between chlinergic crisis and myastinic crisis (Tensilon Test)

  • alcohol, quatinery amine
  • do not enter CNS
  • active for 5-15min only
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10
Q

Tx for MG

A

AchE inhi: pyridostigmine(mostly used), neostigmine

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11
Q

tx for glaucoma

A

cholinergic drug: pilocarpine(open-angled), carbachol

AchEI: physostigmine, echothiopate (topical only)

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12
Q

tx xerostmia

A

bethanechol

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13
Q

Bezold-Jerisch reflex

A

caused by high dose of nicotine

3 signs: hypotension, braycardia, nausea

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14
Q

lethal dose of nicotine

A

60mg

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15
Q

AchEI used in tx of alzheimer

A

drugs that can pass through BBB:

  1. donepezil
  2. tacrine
  3. revastigmine
  4. galatamine
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16
Q

ecothiopate

A

organophosphate
irreversible AchEI
release slowly from AchE- active for 2-7 days

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17
Q

malathion

A

organophsphate
not harmful- degraded by enzymes in mamals
used as ectoparasiticide in clinical setting

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18
Q

parathion

A

organophosphate
dangerous- ^ lipid solubility
active: 7-30 days
used in insecticides- toxicity in farmer

19
Q

parlidoxime

A
  • organophosphate antagonist
  • oxime group has ^ affinity for the phosphorous
  • tx patient with organophosphate poisoning
  • does not enterCNS
  • acts on both N and M receptors
  • sideeffect: muscle weakness
  • no effect after “aging”
20
Q

aged organophosphate- AchE complex

A

strong irreversible covalent bond is formed

21
Q

use of antimuscarinic drugs

A
  1. motion sickness (diarrihea)
  2. post-op urinary spam
  3. parkinsons disease
  4. antidote for parathion poisoning
    other muscarinic functions
22
Q

side effect of antimuscarinic drugs (state 8)

A
  1. xerostomia
  2. constipation
  3. urinary retention
  4. mydrasis
  5. percipitation glaucoma
  6. decrease sweating
  7. tachycardia
  8. hyperventilation and dec respiratory secretions
23
Q

to block muscarinic action of following organs which receptors would you traget:

  1. CNS
  2. exocrine glands
  3. GIT
  4. Respiratory system
  5. eyes
  6. CVS
  7. Smooth muscles
  8. GUT
A
  1. several M receptors and effect depends on the dose
  2. M3, (M2)
  3. M1, M3( not sure)
  4. Nonselective
  5. M3
  6. M2
  7. (M2), M3
  8. M3, M1
24
Q

featues of Atropine

A
  1. atropa belladona
  2. non selective competetive antagonist atM receptors
  3. tertiary amine
  4. distributed in CNS and other organs
  5. acts only on muscarinic ( hence cant inhibit muscle skeletal mucle contraction[N] cause with ^ Ach )
  6. excreted unchaged in urine
  7. t1/2= 2hr, active = 4-8hr
  8. in eye active for72hr
25
Q

tissues most sensitive to atropine

A
  1. salivary glands
  2. bronchioles
  3. sweat glands
26
Q

uses of atropne

A
  1. preanesthetic preparation-> dec resp secretions-> allow intubation
  2. ^ HR
  3. organphosphate poisoning
  4. mydrasis and cyloplegia
27
Q

drugs that cause mydrastic and cyclopegic effects and duration of effect

A

tropicamide

28
Q

ganglionic blockade on heart and blood vessels

A

tachycardia and vaso/venidilation

29
Q

ganglionic blockade on respirtory

A

little effect of bronchodilation

30
Q

ganglionic blockade on GIT

A

hypomotility, decrease serections, constipation

31
Q

ganglionic blockade on GUT

A

urinary retention, impaired ejaculation

32
Q

ganglionic blockade on iris/ ciliary muscles

A

mydrasis, cyclopegia

33
Q

ganglionic blockade on glands

A

xerostomia, anhidrosis, dry eyes, dec gastric secretion

34
Q

ganglionic blocing drugs

A
  1. hexamethonium [C6] (prototype ganglionic blocker)
  2. tetraethylammonium[TEA]
  3. decamethonium [C10]- depolarising blocker
  4. mecamylamine- cross BBB, absob orally, mental abberations
  5. trimethapan- low lipid soulubility, inactive orally, short t1/2, tx hypertension
35
Q

non depolarizing anesthetics/NM blocker

A

competetive antagonist at Nm cause flacid paralysis 30-60mins

  1. tubocurarine
  2. cistracurium
  3. mivacurium
  4. pipecuronium
  5. rocuronium
  6. doxacurium
  7. pancuronium
  8. vecuronium
  9. atracurium
36
Q

depolarising NM blockers/ anesthetic

A

cholinergic agonist->continuous depolarisation-> flacid paralysis, fasiculation and (after tx) muscel pain

  1. succinylcholine
  2. dexamethonium
37
Q

tx malignant hyperthermia

A

succinylcholine

38
Q

succinylcholine hydrolysed by

A
  1. butyrylcholinesterase or

2. pseudocholinesterase

39
Q
  1. Skeletal muscles contain which receptor
A

Nm-> depolarization

β2 -> uptake of potassium (possible cause of skeletal muscle tremor not known for sure)

40
Q
  1. Blood vessels of Skeletal muscles contain which receptor
A

β2 -> relaxation
Alpha -> contraction (less imp)
Some M3-> relaxation

41
Q

drugs used as appetite suppressant/ weight loss

A

1.Phenylpropanolamine( can cause hemorrhage)
2. Ephedrine
3. Amphetamine
4.

42
Q

Tx. Narcolepsy

A
  1. Modafinil

2. Ephedrine

43
Q

Nasal decongestant

A
  1. Phenylephrine
  2. methoxamine
  3. NE
  4. Ephedrine
44
Q

Tx ADHD

A
  1. Methylphenidate

2. Atomoxitine

Autonomic System Pharmacology (4 decks)

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