Part 2.3.1 - Autonomic Drugs - Parasympathetic drugs - Introduction, Cholinomimetics

ACETYLCHOLINE is located in:

(Multiple Answers)

a. vesicle

b. Cholinergic Post gangllion

c. Central Nervous System

d. Skeletal Muscles

e. Stomach

All

Choline is transported into the presynaptic nerve terminal by ________.

a. VAT
b. CHT
c. SNAPs
d. VAMPs

b. choline transporter (CHT)

Choline transport is sodium-________.

a. activated
b. inhibited
c. dependent
d. independent

c. dependent

Drug that inhibits the choline transporter (block entry of choline)

a. Vesamicol
b. Hemicholinium
c. Botulinum toxin
d. Acetylcholinesterase

b. Hemicholinium

Acetylcholine is synthesized from choline and ________.

a. Dopamine
b. Acetyl-CoA
c. Serotonin
d. ATP

b. Acetyl-CoA

Enzyme that synthesizes acetylcholine

a. Acetylcholinesterase
b. Choline acetyltransferase
c. MAO
d. COMT

b. Choline acetyltransferase

Acetylcholine is transported into the storage vesicle by ________.

a. CHT
b. VAT
c. SNAPs
d. VAMPs

b. vesicle-associated transporter (VAT)

Drug that inhibits VAT (inhibits storage of ACh into the vesicle)

a. Hemicholinium
b. Botulinum toxin
c. Vesamicol
d. Anticholinesterases

c. Vesamicol

Substances stored in the vesicle aside from Acetylcholine

a. ATP
b. Histamine
c. Insulin
d. Cortisol

e. Proteoglycan

f. Peptides (P)

a. ATP

e. Proteoglycan

f. Peptides (P)

Release of transmitter occurs when voltage-sensitive ________ channels are opened.

a. Sodium
b. Potassium
c. Calcium
d. Chloride

c. Calcium

-Allowing an influx of calcium

-The resulting increase in intracellular calcium causes fusion of vesicles with the surface membrane and exocytotic expulsion of acetylcholine and cotransmitters into the junctional cleft

Drug that blocks exocytotic expulsion of acetylcholine (inhibit exocytosis of Ach)

a. Vesamicol
b. Hemicholinium
c. Botulinum toxin
d. ATP

c. Botulinum toxin

Acetylcholine action is terminated by metabolism through ________.

a. ChAT
b. MAO
c. Acetylcholinesterase
d. COMT

c. Acetylcholinesterase

-Receptors on the presynaptic nerve ending modulate transmitter release. SNAPs, synaptosome-associated proteins; VAMPs, vesicle-associated membrane proteins.

Muscarinic 1 (M1) receptors are ________ linked.

a. Gi-linked
b. Gs-linked
c. Gq-linked
d. Na-linked

c. Gq-linked

M1 receptors are located in the ________ gland.

a. Lacrimal
b. Gastric
c. Salivary
d. Sweat

b. Gastric

Stimulation of M1 receptors causes ________ secretion.

a. Insulin
b. HCl
c. Dopamine
d. Histamine

b. HCl

Muscarinic 2 (M2) receptors are ________ linked.

a. Gq-linked
b. Gi-linked
c. Gs-linked
d. Ca-linked

b. Gi-linked

M2 receptors are found in the ________.

a. Gastric gland
b. Exocrine glands
c. Heart (atria)
d. Neuromuscular endplates

c. Heart (atria)

M2 receptor stimulation effects

a. bradycardia

b. tachycardia

c. bronchoconstriction

d. bronchodilation

a. Bradycardia

-↓heart rate and contractility of the atria

Muscarinic 3 (M3) receptors are ________ linked.

a. Gi-linked
b. Gs-linked
c. Gq-linked
d. Na-linked

c. Gq-linked

M3 receptors stimulate secretion in ________ glands.

a. Endocrine
b. Exocrine
c. Sebaceous
d. Thyroid

b. Exocrine

Which is an exocrine gland secretion stimulated by M3 receptors?

(Multiple Answers)

a. Eccrine

b. Lacrimal

c. Renin

d. Insulin

e. Salivary

f. Gastric acid

a. Eccrine

b. Lacrimal

e. Salivary

f. Gastric acid

M3 receptor stimulation in smooth muscles causes ________.

a. Relaxation
b. Contraction
c. Sedation
d. Tremors

b. Contraction = Miosis, Bronchospasm, Diarrhea, Urination (DUMBELS)

Nicotinic neural (Nn) receptors are located in the ________.

a. Gastric gland
b. Neuromuscular endplates
c. Ganglion and CNS
d. Exocrine glands

c. Ganglion and CNS

Nn receptor stimulation causes ________ release.

a. Histamine
b. Renin
c. Epi
d. Insulin

c. Epi

Nm receptors are located in the ________.

a. Ganglion
b. CNS
c. Neuromuscular endplates
d. Gastric glands

c. Neuromuscular endplates

Skeletal muscle contraction due to Nm receptor stimulation may cause ________.

a. Tremor
b. Bronchospasm
c. Diarrhea
d. Miosis

a. Tremor

Parasympathomimetics are also called ________.

a. Adrenergic antagonists
b. Cholinergic agonists
c. Beta blockers
d. Antimuscarinic

b. Cholinergic agonists

-aka Cholinomimetics

-aka Mimicry

Parasympathomimetic classifications:

a. Direct-Acting

b. Indirect-Acting: Cholinesterase Inhibitors

c. both

c. both

Indirect-acting parasympathomimetics work by inhibiting metabolism of ________.

a. Dopamine
b. Epi
c. ACh
d. Histamine

c. ACh

[DIRECT-ACTING: Choline esters]

Non selective or Muscarinic-selective

___a. Acetylcholine

___b. Betanechol (Urecholine)

___c. Carbachol

___d. Metacholine

Non selective______a. Acetylcholine

Muscarinic-selective_b. Betanechol (Urecholine)

Non selective______c. Carbachol

Non selective______d. Metacholine

[DIRECT-ACTING: Alkaloids]

Non selective or Muscarinic-selective or Nicotinic-selective

___a. Muscarine

___b. Nicotine

___c. Arecholine

___d. Pilocarpine
___e. Lobeline
___f. Varenicline

Muscarinic-selective_a. Muscarine

Nicotinic selective___b. Nicotine

Non-selective______c. Arecholine

Muscarinic-selective_d. Pilocarpine
Nicotinic-selective___e. Lobeline
Nicotinic-selective___f. Varenicline

[DIRECT-ACTING]

Management of Urinary retention

a. Metacholine

b. Betanechol

c. Pilocarpine

d. Acetylcholine

b. Betanechol

[DIRECT-ACTING]

Post-operative abdominal distention and gastric atony

a. Metacholine

b. Betanechol

c. Pilocarpine

d. Acetylcholine

b. Betanechol

[DIRECT-ACTING]

Pulmonary challenge test (provocative test for bronchial hyperactivity)

a. Metacholine

b. Betanechol

c. Pilocarpine

d. Acetylcholine

a. Metacholine

[DIRECT-ACTING]

Reduces intraocular pressure in open angle and narrow angle glaucoma

a. Metacholine

b. Betanechol

c. Pilocarpine

d. Acetylcholine

c. Pilocarpine

[DIRECT-ACTING]

Binds preferentially at muscarinic receptors

a. Metacholine

b. Betanechol

c. Pilocarpine

d. Acetylcholine

c. Pilocarpine

[DIRECT-ACTING]

Produce miosis in ophthalmic surgery

a. Metacholine

b. Betanechol

c. Pilocarpine

d. Acetylcholine

d. Acetylcholine

[DIRECT-ACTING]

Nicotinic-selective alkaloids (Nicotine, Lobeline, & Varenicline) are used in

a. Urinary retention

b. Glaucoma

c. Smoking cessation

d. Gastric atony

c. Smoking cessation

Organophosphates are _____ inhibitors

a. Irreversible

b. Reversible

a. Irreversible

[INDIRECT ACTING]

Aminoalcohol are _____ inhibitors

a. Irreversible

b. Reversible

b. Reversible

[INDIRECT ACTING]

Carbamates are _____ inhibitors

a. Irreversible

b. Reversible

b. Reversible

Nerve Gases:

I. Sarin

II. Malathion

III. Tabbun

IV. Soman

Sarin

Tabbun

Soman

Organophosphates:

I. Echothiophate

II. Malathion

III. Parathion

IV. Nerve Gases

V. Endrophonium (Tensilon)

I. Echothiophate

II. Malathion

III. Parathion

IV. Nerve Gases

Endrophonium (Tensilon) is an Aminoalcohol

[INDIRECT ACTING]

Aminoalcohol or Carbamates or CNS-acting

___a. Demecarium

___b. Physostigmine/Eserine

___c. Tacrine

___d. Endrophonium (Tensilon)

___e. Donepezil

___f. Pyridostigmine

___g. Neostigmine

___h. Galantamine

___i. Rivastigmine

___j. Ambenonium

Carbamates___a. Demecarium

Carbamates___b. Physostigmine/Eserine

CNS- acting___c. Tacrine

Aminoalcohol__d. Endrophonium (Tensilon)

CNS- acting___e. Donepezil

Carbamates___f. Pyridostigmine

Carbamates___g. Neostigmine

CNS- acting___h. Galantamine

CNS- acting___i. Rivastigmine

Carbamates___j. Ambenonium

[INDIRECT ACTING]

Physostigmine indication

a. Myasthenia Gravis

b. GI and Urinary Tract Anatomy

c. Glaucoma

d. Alzheimer’s Disease

c. Glaucoma

[INDIRECT ACTING]

Demecarium indication

a. Myasthenia Gravis

b. GI and Urinary Tract Anatomy

c. Glaucoma

d. Alzheimer’s Disease

b. GI and Urinary Tract Anatomy

[INDIRECT ACTING]

Edrophonium indication

a. Myasthenia Gravis

b. GI and Urinary Tract Anatomy

c. Glaucoma

d. Alzheimer’s Disease

a. Myasthenia Gravis

[INDIRECT ACTING]

Tensilon Test is used to diagnose:

a. Myasthenia Gravis

b. GI and Urinary Tract Anatomy

c. Glaucoma

d. Alzheimer’s Disease

a. Myasthenia Gravis

[INDIRECT ACTING]

An autoimmune disease (Progressive muscle, weakness, dropping of eyelids, Repiratory paralysis)

a. Myasthenia Gravis

b. GI and Urinary Tract Anatomy

c. Glaucoma

d. Alzheimer’s Disease

a. Myasthenia Gravis

[INDIRECT ACTING]

CNS-acting Cholinomimetics (like Tacrine, Donepezil, Galantamine, Rivastigmine) indication

a. Myasthenia Gravis

b. GI and Urinary Tract Anatomy

c. Glaucoma

d. Alzheimer’s Disease

d. Alzheimer’s Disease

Symptoms included in cholinergic toxicity

Adverse Effects: "DUMBELS"

Diarrhea

Urination

Miosis

Bradycardia, Bronchoconstriction

Emesis

Lacrimation

Salivation, Sweating

Primary treatment for cholinergic toxicity

a. Pralidoxime
b. Diacetylmonoxime
c. Atropine
d. Pilocarpine

c. Atropine

cholinesterase reactivators:

a. Pralidoxime
b. Scopolamine
c. Bethanechol
d. Diacetylmonoxime

a. Pralidoxime

d. Diacetylmonoxime