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pharmachology > Parasympathomimetics > Flashcards

Parasympathomimetics Flashcards

(45 cards)

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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

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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

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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

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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

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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

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A

MECHANISM
Na/Choline transporter inhibitor (ChT)

INDICATION
No clinical use, only research!

24
Q

TETRADOTOXIN

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A

MECHANISM
Na channel inhibitor (no AP)

INDICATION
-local anesthetic

SIDE EFFECTS

  • paresthesia of lips, tongue and extremities
  • hypersalivation, sweating
  • respiratory difficulty
25
OMEGA CONOTOXIN | ZICONOTIDE
MECHANISM - Ca channel imhibitor - NT vescicle release inhibitor INDICATION -CSF injection for chronic pain, FDA approved
26
VESAMICOL
MECHANISM VAT (vesicular ACh Transporter) inhibitor INDICATION No clinical use, only research!
27
BOTULINUM TOXIN
``` 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
ATROPINE
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
SCOPOLAMINE
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
HOMATROPINE
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
TROPICAMIDE
``` 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
CYCLOPENTOLATE
``` 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
BENZATROPINE
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
BIPERIDEN
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
PROCYCLIDINE
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
OXYBUTYNIN
MECHANISM mACh R antagonist CNS: passes BBB! INDICATION -hyperactive bladder syndrome SIDE EFFECTS - dry mouth - difficulty in urination - constipation - blurred vision - drowsiness - dizziness.
37
TROSPIUM
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
PIRENZEPINE
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
TELEZEPINE
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
BUTYL-SCOPOLAMINE
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
IPRATROPIUM
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
TIOTROPIUM
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
HEXAMETHONIUM
MECHANISM nACh R antagonist (Nneural) it's a ganglion blocker!! NO BBB! INDICATION poorly absorbed by GI -chronic HTN (not used)
44
TRIMETAPHAN
MECHANISM nACh R antagonist (Nneural) it's a ganglion blocker!! INDICATION - Hypertensive crisis (not used) - Aortic dissection (not used)
45
MECAMYLAMINE
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

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