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Pharmacology Block 1 > Cholinoceptor Activating & Cholinesterase inhibiting Drugs > Flashcards

Cholinoceptor Activating & Cholinesterase inhibiting Drugs Flashcards

1
Q

what are the 2 main cholinergic receptors?

A

Nicotinic (Nm, Nn) and muscarinic (M1, M2, M3)

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2
Q

fill in the red spaces or say where do we find these receptors?

A
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3
Q

Fill in the red spaces or mention what effect will the receptor have in the target organ

A

Also remember that M2 will have decreased AV conduction

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4
Q

Acetylcholine or drugs acting like acetylcholine produces following effects in body:

  • Heart
  • blood vessels
  • smooth muscle of lungs
  • smooth muscle of ballder
  • spincters of the GI and bladder
  • pupils
  • glands
A
  1. Heart : Reduces HR (Bradycardia),FOC, CO and BP
  2. Blood vessel: Vasodilatation and lowers BP
  3. Smooth muscle contraction in GIT, bronchus, and bladder: Thus there will be Diarrhea, Bronchoconstriction and Urination
  4. Sphincters in GIT and bladder: Relaxation
  5. Pupil: Miosis and ciliary muscle contraction
  6. Glands : more Salivation, sweating, gastric acid secretion , tracheobronchial secretion, lacrimation and urination
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5
Q

ACh carrying nerves are called as what?

A

cholinergic fibers

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6
Q

cholinergic fibers are present in what divisions of the nervous system?

A

somatic and ANS

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7
Q

what is a cholinergic agonist?

what are the 2 types of cholinergic agonist? define them

A

Drugs which mimic or increases the actions of ACh

  1. Direct Cholinergic Agonists: drugs that act at receptors
  2. Indirect Cholinergic Agonists: drugs that inhibit the metabolism of Ach and increase its level in synapses and increases the actions of ACh
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8
Q

what are the Direct cholinergic agonists drugs?

A
  1. Bethanechol
  2. Carbachol
  3. Methacholine
  4. Pilocarpine
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9
Q

what are the Indirect cholinergic agonists drugs?

A
  1. Neostigmine
  2. Physostigmine
  3. Pyridostigmine
  4. Edrophonium
  5. Tacrine
  6. Donepezil
  7. Ecothiophate
  8. Malathion
  9. Parathion
  10. Sarin
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10
Q

what indirect cholinergic agonist gets used in alzheimer’s?

A

Tacrine, Donepezil

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11
Q

what indirect cholinergic agonist are used as insecteside?

A

Malathion, Parathion

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12
Q

what indirect cholinergic agonist is used as nerve gas?

A

sabrin

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13
Q

why does Acetylcholine have no clinical use?

A

Because of non-specific actions & rapid inactivation by acetylcholinesterases

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14
Q

Methacholine is used to diagnose what? what do you call the test?

What type of action does it have? (does it bind muscarinic or nicotinic receptors more?)

A

bronchial asthma

methacholine challenge test

It has strong Muscarinic action & least or no Nicotinic action

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15
Q

what are the therapeutic uses of Bethanechol?

A
  1. Paralytic ileus: condition characterised by reduced bowel movements. mostly seen in post-op patients
  2. Urinary retention: Typically seen in postoperative patients and many other neurological diseases
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16
Q

what is Pilocarpine?

what type of receptor does it utilize?

is it water or lipid soluble?

what organ does it penetrate easily?

what are its therapeutic uses?

A

an alkaloid

It has Muscarinic activity only

lipid soluble

cornea

  1. glaucoma
  2. Sjogren syndrome: xerostomia (dry mouth), dry eye (keratoconjunctivitis) and arthritis
17
Q

what Indirect Cholinergic agonists are reversible?

A
  • Neostigmine
  • Physostigmine
  • Pyridostigmine
  • Edrophonium
  • Tacrine
  • Donepezil
18
Q

what Indirect Cholinergic agonists are irreversible?

A
  • Ecothiophate
  • Malathion
  • Parathion
  • Sarin
19
Q

how long do reversible enzyme inhibitors act?

how long do irreversible enzyme inhibitors act?

of the irreversible indirect cholinergic agonist list, which one is used clinically? for what is it used?

A

short period of time

long period of time

Ecothiopate, is used for glaucoma

20
Q

what drugs are used in sjogren, alzheimers, glaucoma?

what category are these? (reversible or irreversible?)

what drug is used in glaucoma? why?

A

pilocarpine and donepazil/tacrine

Reversible Cholinesterase inhibitors

Physostigmine, it penetrates the cornea well due to lipid solubility

21
Q

why cant neostigmine be used in the treatment of glaucoma?

A

it is lipid insoluble and cant penetrate cornea too well

22
Q

what is the mechanism of action of physostigmine?

A

reversible inhibition of AChE enzyme (↑ Ach)

23
Q

what acetyl cholinesterase inhibitors are used in the treatment of myasthenia gravis?

which do you use only to diagnose myasthenia gravis?

A
  1. Neostigmine
  2. Pyridostigmine

Edrophonium

24
Q

when is neostigmine used in Myasthenia gravis?

when is pyridostigmine used in myasthenia gravis?

when is Edrophonium used in myasthenia gravis?

A

it is used in acute cases

maintenance/ long term therapy due to longetivity of drug

shortest acting drug, so it is used in diagnosis of M. Gravis

25
Q

how do you differentiate myasthenic crisis and cholinergic crisis?

what is another name for the test used to differentiate myasthenic crisis and cholinergic crisis?

A

use Edrophonium in small amount and there is contraction of muscle then it is myasthenic crisis since in cholinergic crisis the muscles would be more flaxid and not respond

tensilon test

26
Q

If drug therapy is inadequate during myasthenic crisis, patients develop what?

what happens If excessive amounts of drugs have been used in patients with cholinergic crisis?

A

severe muscle weakness.

patients may become paradoxically weak because of nicotinic depolarizing blockade of the motor end plate.

27
Q

what is belladona poisoning?

what symptoms can be seen?

A

the same thing as atropine poisoning, blocking muscarinic receptors

tachycardia, constipation, dry eye, dry mouth, urinary retention, dilated pupils

28
Q

Tacrine, Rivastigmine and Donepezil, Malathion, Parathion…of these, which is used in the treatment of alzheimer’s?

what about the other 2 options?

what type of drug is the answer for the first question?

A

Tacrine, Rivastigmine and Donepezil

they are used as insectisides

irreversible acetylcholinesterase inhibitor

29
Q

what are organophosphates?

signs and symptoms of organophosphate poisoning are due to what?

symptoms occur due to what?

what are the symtoms of organophosphate poisoning?

A

irreversible cholinesterase inhibitors

Phosphorylation (irreversible inhibition ) of the enzyme resulting in excess acetylcholine

stimulation of muscarinic receptors

miosis, blurred vision, bradycardia, salivation, sweating, urination, bronchial constriction, vomiting, and diarrhea

30
Q

what is the drug of choice for organophosphate poisoning? why?

what is the problem of giving atropine alone?

what is given as well during Org. Phosphate poisoning?

A

Atropine a muscarinic receptor blocker is used to control signs of muscarinic excess stimulation of OP compounds.

  • it cannot control the nicotinic effects OP poisoning
  • can’t reverse the CNS effects

Pralidoxime: a Acetylcholine esterase reactivator that acts by hydrolysing (reactivating) the drug bound enzyme

31
Q

what are the symptoms of Org. Phosphate poisoning?

A

DUMBELSS

  • Diarrhea, Abdominal cramps, vomiting,
  • Urination
  • Miosis
  • Bradycardia
  • Bronchospasm
  • Excitation of Skeletal muscle
  • Lacrimation
  • Salivation
  • Sweating

Pharmacology Block 1 (10 decks)

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