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pharmachology > Parasympathomimetics > Flashcards

Parasympathomimetics Flashcards

1
Q

4 AMINOPYRIDINE

A

MECHANISM
K+ channel blocker

Research only!!

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2
Q

ACh

A

MECHANISM

nACh R and MACh R agonists

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3
Q

METACHOLINE

A

MECHANISM
selective mACh R agonist

INDICATION
Diagnosis of asthma / COPD bronchial hyperactivity. *Bronchial challenge test challenge test via M3 stimulation it constricts the bronchi.

SIDE EFFECTS: People with preexisting bronchial condition will react to lower dose of the drug (measured by spirometry)

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4
Q

CARBACHOL

A

MECHANISM:
NACh R and mACh R agonists
NO AChEsterase degradation!!

INDICATION:
Glaucoma

SIDE EFFECTS:

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5
Q

BETANECHOL

A

MECHANISM
mACh R agonist
NO AchEsterase degradation!!

INDICATION
Bladder and GI atonia fater spinal cord injury

SIDE EFFECTS

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6
Q

MUSCARINE

A

MECHANISM
mACh R agonist
NO CNS!!

INDICATION
none, it’s a mushroom poison!

SIDE EFFECTS

  • myosis and blurred vision
  • excessive salivation,sweating and lacrimation
  • bronchoconstriction and increased bronchial secretion
  • bradycardia
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7
Q

PILOCARPINE

A

MECHANISM
mACh R agonist
weak nACh R agonist in CNS

INDICATION

  • Sjogren syndrome (xerastomia)
  • Glaucoma : high IOP (in acute phase: 1st drug used)

SIDE EFFECTS

  • bronchospasm
  • bradycardia
  • vasodilation
  • diarrhea
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8
Q

ARECOLINE

A

MECHANISM
mACh R and nACh R agonists

INDICATION

  • Alzheimer’s : memory and cognitive improvement
  • antihelmintic drug

SIDE EFFECTS
carcinogenic (NOT 1st drug of choice)

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9
Q

NICOTINE

A

MECHANISM
nACh R agonist

INDICATION
smoking cessation (eg. dermal patches, gums)

SIDE EFFECTS
risk of CVD (in long term use)

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10
Q

LOBELINE

A

MECHANISM
nACh R agonist

INDICATION

  • smoking cessation (eg. dermal patches, gums)
  • drug addiction treatment (eg. amphetamines,cocaine and alcohol)

SIDE EFFECTS

  • nausea, vomiting and diarrhea
  • visual and hearing disturbances
  • dizziness

OTHERS:

  • SERT and DAT reuptake inhibition
  • VMAT 2 ligand : stimulate DA release alone, but dimishes DA release caused by metamphetamines
  • MDR inhibitor (reduce chemotherapeutic resistance)
  • nACh R AG/ATG
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11
Q

VARENICLINE

A

MECHANISM
partial nACh R agonist

INDICATION
-smoking cessation

SIDE EFFECTS

  • nausea, vomiting
  • nightmares and sleep disturbances
  • headache
  • depression
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12
Q

CEVIMELINE

A 
MECHANISM
mACh agonist (M1 and M3)
stimulate salivary gland secretion (M3)
INDICATION
Sjogren syndrome (xerostomia)

SIDE EFFECTS

  • nausea, vomiting and diarrhea
  • headache and blurred vision

CONTRAINDICATIONS

  • asthma
  • glaucoma
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13
Q

EDROPHONIUM

A

MECHANISM
AChEsterase inhibitor
NO CNS

INDICATION
differential diagnosis of myasthenia gravis (Ab against ACh R) and cholinergic crisis (AChE is inactive–>high ACh stimulation–>the muscles stop responding–>flaccid paralysis and respiratory failure

SIDE EFFECTS

  • myasthenia gravis: E reduces muscle weakness
  • cholinergic crisis: E inhibits more AChE thus worsening the muscle weakness

OTHER:
-15 mins duration

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14
Q

TACRIN

A

MECHANISM
AChEsterase inhibitor
CNS + !!

INDICATION
-Alzheimer’s (it is obsolete!)

SIDE EFFECTS
-liver damage

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15
Q

DONEPEZIL

A

MECHANISM
AChEsterase inhibitor
CNS + !!

INDICATION
-palliative treatment of Alzheimer’s: improves cognition

SIDE EFFECTS

  • NO liver damage
  • loss of appetite
  • diarrhea, vomiting
  • muscle cramping
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16
Q

PHYSOSTIGMINE

A

MECHANISM
AChEsterase inhibitor
CNS + !!

INDICATIONS

  • Atropine or Scopolamine overdose
  • Glaucoma
  • Delayed gastric emptying
  • Orthostatic hypotension

SIDE EFFECTS

  • nausea, vomiting and diarrhea
  • tremor

OTHER
2-3 hours duration

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17
Q

NEOSTIGMINE

A

MECHANISM
AChEsterase inhibitor
NO CNS!!

INDICATIONS

  • Gut/bladder atonia
  • Myasthenia gravis
  • Glaucoma
  • Stop muscle relaxant effect (Curare antidote)

SIDE EFFECTS

  • bradycardia
  • increased salivation
  • nausea

OTHER
0.5-2 hours duration

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18
Q

PYRIDOSTIGMINE

A

MECHANISM
AChEsterase inhibitor
NO CNS !!!

INDICATIONS

  • Gut/bladder atonia
  • Myasthenia gravis
  • Glaucoma
  • Stop muscle relaxant effect (Curare antidote)

SIDE EFFECTS

OTHER
3-6 hours duration (P.O. administration)

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19
Q

DEMECARIUM

A

MECHANISM
AChEsterase inhibitor
NO CNS!!!

INDICATION
(P.O. administration)
-Glaucoma: reduce IOP (via myosis and ciliary muscle constriction–> facilitating aqueous humor outflow)

SIDE EFFECTS

  • bradycardia and cardiac disturbance
  • nausea and vomiting
  • urinary incontinence
20
Q

AMBENOMIUM

A

MECHANISM
AChEsterase inhibitor
NO CNS!!

INDICATION
(P.O. administration)
-Myasthenia gravis

SIDE EFFECTS
-nausea and vomiting

OTHER
4-8 hours duration

21
Q

RIVASTIGMINE

A

MECHANISM
AChEsterase inhibitor
CNS!!!

INDICATION
(administration: P.O. or dermal patches)
cognitive,functional and behavioural improvement
-Alzheimer's 
-Parkinson's induced dementia

SIDE EFFECTS

  • nausea
  • vomiting
22
Q

Poison, Nerve gases

A

MECHANISM
AChEsterase inhibitor

NO indication

SIDE EFFECTS
(prolonged effect)
-convulsions 
-involuntary urination and defecation
-pupil constriction, profuse salivation
-death by asphyxiation

OTHER
Oximes can be given to reverse the effect of the poison while the enzyme is still not irreversibly inhibited.

23
Q

HEMICHOLINUM

A

MECHANISM
Na/Choline transporter inhibitor (ChT)

INDICATION
No clinical use, only research!

24
Q

TETRADOTOXIN

A

MECHANISM
Na channel inhibitor (no AP)

INDICATION
-local anesthetic

SIDE EFFECTS

  • paresthesia of lips, tongue and extremities
  • hypersalivation, sweating
  • respiratory difficulty
25
Q

OMEGA CONOTOXIN

ZICONOTIDE

A

MECHANISM

  • Ca channel imhibitor
  • NT vescicle release inhibitor

INDICATION
-CSF injection for chronic pain, FDA approved

26
Q

VESAMICOL

A

MECHANISM
VAT (vesicular ACh Transporter) inhibitor

INDICATION
No clinical use, only research!

27
Q

BOTULINUM TOXIN

A 
MECHANISM
NT vescicle release (SNARE) inhibitor
(Clostridium Botulinum, gram + 
INDICATION
-plastic surgery
-muscle relaxant

SIDE EFFECTS

  • infant (cause: honey):
    1. floppy baby syndrome (hypotonia)
    2. SIDS (sudden infant death syndrome) due to respiratory insufficiency
  • adult (cause: unproperly canned food)
    1. blurred vision, nausea, vomiting
    2. breathing/swallowing problem
    3. muscle weakness
    4. consitipation
28
Q

ATROPINE

A

MECHANISM
mACh R antagonist
CNS: passes BBB!!

INDICATIONS
A.OPHTALMOLOGY
-Pupil dilation, long lasting (8days, not good, can cause glaucoma–> high IOP!!)
B.GASTROENTEROLOGY
-Biliary cramps (decreases SMC in gall bladder)–>always used together with PAPAVERIN (SMC relaxant, also used in erectile dysfunciton)
-Diarrhea: atropine + DIPHENOXYLATE –> centrally acting opioid with local GI effect–>decreases the peristalsis for stool consolidation
C. PULMONOLOGY
-Bronchodilation + inhibition of bronchial secretion
(not used)
D.NEUROLOGY
-Parkinson: Inhibits tremors. Side effect is mental depression.
E.ANESTHESIOLOGY
-Inhibits gastric acid secretion
-Prevents bradycardia and AV block during surgery
F.CARDIOLOGY
-Increases heart rate to normal tone–>inhibits parasympathetic effect on heart!
-2nd/3rd degree AV block treatment

G.NO effect on skeletal muscle (only nACh R!)

H.CHOLINERGIC POISONING: caused by organophosphate (eg.insecticides,nerve gases)–> AChE inhibition: high ACh
I.ANTIEMETIC (antivomiting)
Inhibits the vomiting triggering area of the medulla

SIDE EFFECTS

  1. Systemic 2-3h
  2. Local eye drops 7-10d!!!

Dose related effects:

  • 0.5mg therapeutic dose
  • 2-3mg tachycardia, fever in children (thermoregulation is via sweat glands–>inhibition=no sweating=high T)
  • 3-5mg aphonia (speaking disturbance), swallowing difficulty
  • 5-10mg confusion, hallucination, epilepsy, CNS extrapyrimidal effect
  • > 10mg respiratory depression, vasodilation, hypotension
  • 100mg lethal dose

Atropine poisoning:
1. Peripheral effect: dry mouth/skin, wide pupils, constipation, dysuria
2. CNS: hallucinations, restlessness, dyskinesia, epilepsy, coma, death
Therapy:
-Physostigmine IV for CNS
-Neostigmine for pheriphery

OTHER
MNEMONIC for indications!!!  "DUMBBELSS"
Diarrhea
Urination
Myosis
Bradycardia
Bronchoconstriction
Excitation (CNS: decrease EPSP, used for low tremor)
Lacrimation
Salivation
Sweating (only sympathetic innervation using muscarinic receptors).
29
Q

SCOPOLAMINE

A

MECHANISM
mACh R antagonist
CNS: passes BBB!

INDICATION

  • Vomiting (kinetosis, motion sickness)
  • Enhance anaesthesia effect

SIDE EFFECTS

  • sedation
  • amnesia (memory loss)
OTHER
2-3h shorter local effect!
Dosage:
-0.4mg therapeutic dose
-500mg lethal dose
30
Q

HOMATROPINE

A

MECHANISM
mACh R antagonist
CNS: psses BBB!

INDICATION

  • Eye examination
  • Mydriasis (pupil dilation=mAchR on sphincter pupil muscle)

SIDE EFFECTS

  • 2-3d local effect
  • less potent than atropine
  • blurred vision, photosensitivity
31
Q

TROPICAMIDE

A 
MECHANISM
mACh R antagonist
CNS: passes BBB!
INDICATION
-Eye examination
-Mydriasis (pupil dilation=mAchR on sphincter pupil muscle)

SIDE EFFECTS

  • high IOP
  • blurred vision
  • photosensitivity
32
Q

CYCLOPENTOLATE

A 
MECHANISM
mACh R antagonist
CNS: passes BBB!
INDICATION
-Eye examination
-Mydriasis (pupil dilation=mAchR on sphincter pupil muscle)

SIDE EFFECTS

  • high IOP
  • blurred vision
  • photosensitivity
33
Q

BENZATROPINE

A

MECHANISM
mACh R antagonist
CNS: passes BBB!

INDICATION
Tremor dominant Parkinson’s patients:
-improves tremor and rigidity
-alleviates bradykinesia (slow movements)

SIDE EFFECTS

  • Dry mouth
  • Blurred vision
  • Cognitive changes
  • Constipation and urinary retention
  • Tachycardia
  • Anorexia
34
Q

BIPERIDEN

A

MECHANISM
mACh R antagonist

INDICATION
Tremor dominant Parkinson’s patients:
-improves tremor and rigidity
-alleviates bradykinesia (slow movements)

SIDE EFFECTS

  • blurred vision
  • dry mouth
  • sleepiness
  • constipation
  • confusion
35
Q

PROCYCLIDINE

A

MECHANISM
mACh R antagonist
CNS: passes BBB!

INDICATION
Tremor dominant Parkinson’s patients:
-improves tremor and rigidity
-alleviates bradykinesia (slow movements)

SIDE EFFECTS

  • tachycardia
  • hallucinantions
36
Q

OXYBUTYNIN

A

MECHANISM
mACh R antagonist
CNS: passes BBB!

INDICATION
-hyperactive bladder syndrome

SIDE EFFECTS

  • dry mouth
  • difficulty in urination
  • constipation
  • blurred vision
  • drowsiness
  • dizziness.
37
Q

TROSPIUM

A

MECHANISM
mACh R antagonist
NO BBB!

INDICATION
-hyperactive bladder syndrome: relaxation of the smooth muscle in the urinary bladder (detrusor muscle)

SIDE EFFECTS

  • dry mouth
  • indigestion
  • constipation
38
Q

PIRENZEPINE

A

MECHANISM
mACh R antagonist (M1)
NO BBB!

INDICATION

  • High dose is needed, not good for therapeutic use
  • ->PPI and H2 blockers are used instead
  • peptic ulcer: reduces the gastric acid secretions and muscle spasm

SIDE EFFECTS

  • delayed gastric emptying
  • constipation
39
Q

TELEZEPINE

A

MECHANISM
mACh R antagonist (M1)
CNS: passes BBB!

INDICATION
it’s 25 more potent than Pirenzepine!!
-peptic ulcer

SIDE EFFECTS

  • delayed gastric emptying
  • constipation
40
Q

BUTYL-SCOPOLAMINE

A

MECHANISM
mACh R antagonist
NO BBB! (medulla oblongata: weak BBB, thus has little effect against nausea)

INDICATION

  • SMC spasm (GI/bladder/biliary)
  • antiemetic: chemoreceptor triggering zone inhibition
SIDE EFFECTS (minimal)
-somnolence
41
Q

IPRATROPIUM

A

MECHANISM
mACh R antagonist
NO BBB!

INDICATION
Administration: Inhalation (local effect only!)
-COPD
-Bronchodilation 
-Anti bronchial secretion

SIDE EFFECTS (minimal)

  • nausea, dry mouth
  • sedation
42
Q

TIOTROPIUM

A

MECHANISM
mACh R antagonist (M3)
NO BBB!

INDICATION
Long acting: 24 hours! Not used for acute state!
-Asthma treatment: bronchodilation effect
-Anti brochial secretion

SIDE EFFECTS (minimal)

  • dry mouth
  • throat irritation
43
Q

HEXAMETHONIUM

A

MECHANISM
nACh R antagonist (Nneural)
it’s a ganglion blocker!! NO BBB!

INDICATION
poorly absorbed by GI
-chronic HTN (not used)

44
Q

TRIMETAPHAN

A

MECHANISM
nACh R antagonist (Nneural)
it’s a ganglion blocker!!

INDICATION

  • Hypertensive crisis (not used)
  • Aortic dissection (not used)
45
Q

MECAMYLAMINE

A

MECHANISM
nACh R antagonist (Nneural)
it’s a ganglion blocker!!

INDICATION
research!!
-anti HTN (not used)
-smoking cessation: lowers nicotine cravings

SIDE EFFECTS

  • nausea, decreased appetite and vomiting
  • orthostatic hypotension
  • dry mouth

pharmachology (7 decks)

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