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Pharmacology > Prelim Chapter 4 CHOLINERGIC AGONISTS > Flashcards

Prelim Chapter 4 CHOLINERGIC AGONISTS Flashcards

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1
Q

•act on receptors (muscarinic or nicotinic) that are activated by acetylcholine (ACh)

A

Cholinergic Agonists

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2
Q

•drugs that mimic the actions of acetylcholine

A

Cholinomimetic Drugs

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3
Q

•neurotransmitter on the following sites:
– preganglionic fibers terminating in the adrenal medulla
– autonomic ganglia (both sympathetic & parasympathetic)
– postganglionic fibers of the parasympathetic division
– postganglionic sympathetic divison of sweat glands
– cholinergic neurons that innervate the muscles of the somatic system

A

Acetylcholine (ACh)

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4
Q

Neurotransmission at Cholinergic Neurons
•Synthesis
•Storage
•Release
•Binding of ACh to a receptor
•Degregadation of the neurotransmitter in the synaptic cleft
•Recycling of choline and acetate

A

…

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5
Q

•named after the alkaloid muscarine that mimics the effects of acetylcholine
•belongs to the class of G protein coupled receptors (metabotropic)
•5 subtypes but M1, M2 and M3 have been functionally characterized

A

Muscarinic Receptor

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6
Q

•drugs that bind in the muscarinic receptors and elicit pharmacological actions

A

Muscarinic Agonists

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7
Q

•ganglion and skeletal muscle receptors stimulated by low concentration of nicotine
– NM - found in the neuromuscular junctions
– NN - found in the CNS, adrenal medulla, autonomic ganglia

A

Nicotinic Receptors

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8
Q
  • found in the neuromuscular junctions
A

NM

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9
Q
  • found in the CNS, adrenal medulla, autonomic ganglia
A

NN

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10
Q

Parasympathetic Effects
•D - Diarrhea/ Diaphoresis
•U - Urination
•M - Miosis
•B - Bradycardia/ Bronchoconstriction
•E - Emesis
•L - Lacrimation
•S - Salivation

A

…

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11
Q

Dumbels means

A

•D - Diarrhea/ Diaphoresis
•U - Urination
•M - Miosis
•B - Bradycardia/ Bronchoconstriction
•E - Emesis
•L - Lacrimation
•S - Salivation

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12
Q

Organ Effects of Direct-Acting Cholinoceptor Drugs

Organ-Response
Eye (Sphincter muscle of iris)- Contraction (Miosis)
(Ciliary Muscle)-Contraction for near vision
Heart-Negative chronotropy, inotropy and dromotropy
Blood Vessels-Dilation; Constriction (high doses)
Lungs-Bronchoconstriction; Bronchial glands stimulation
GI Tract-Increase motility, Secretion stimulation

Urinary Bladder-Contraction; Relaxation of sphincters
Glands-(sweat, salivary, lacrimal, nasopharyngeal)

A
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13
Q

MOA of Cholinomimetic Drugs
•Direct-acting Cholinomimetic Drugs - bind to and activate muscarinic or nicotinic receptors

•Indirect-acting Drugs - inhibits acetylcholinesterase (AChE), which hydrolyzes acetylcholine to choline and acetic acid

A

…

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14
Q
  • bind to and activate muscarinic or nicotinic receptors
A

Direct-acting Cholinomimetic Drugs

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15
Q

inhibits acetylcholinesterase (AChE), which hydrolyzes acetylcholine to choline and acetic acid

A

Indirect-acting Drugs

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16
Q

•a quaternary ammonium compound that cannot penetrate membranes
•Effects:
–decrease in heart rate and cardiac output
– decrease in blood pressure
– DUMBELS

A

ACETYLCHOLINE

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17
Q

•Urecholine®
•Actions: Causes increased secretion, smooth muscle contraction (except vascular smooth muscle - relaxes), and changes in heart rate

CA: Postoperative and neurogenic ileus and urinary retention
•S/E: Generalized cholinergic stimulation (sweating, salivation, flushing, decreased blood pressure, nausea, abdominal pain, diarrhea, bronchospasm
•Antidote: Atropine

A

BETANECHOL

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18
Q

•Carboptic®, Miostat®, Carbastat®
•Actions: similar to betanechol
•CA: used topically almost exclusively for glaucoma

A

Carbachol

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19
Q

Endogenous Choline Esters

A

ACETYLCHOLINE

BETANECHOL

Carbachol

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20
Q

Direct-Acting Muscarinic Alkaloids or Synthetics

A

PILOCARPINE

Cevimeline

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21
Q

•Isopto Carpine®
•Actions: effects are similar to betanechol; produces rapid miosis
•CA: Glaucoma, Sjogren’s Syndrome
S/E: blurred vision, night blindness, brow ache, exaggeration of various parasympathetic actions
•Antidote: Atropine

A

PILOCARPINE

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22
Q

•Evoxac®
•Synthetic
•Similar to pilocarpine

23
Q

Direct-Acting Nicotinic Agonists

24
Q

•Activates autonomic postganglionic neurons and skeletal muscle neuromuscular end plates
•CA: medical use in smoking cessation
•S/E: N & V, Increased BP, Long term GI and CV risk factor
•Interaction: Additive to CNS stimulant

25
INDIRECT-ACTING CHOLINOMIMETICS 3 Chemical Groups of Cholinesterase Inhibitors •Simple alcohols bearing a quaternary ammonium group (eg. Edrophonium) •Carbamic acid esters of alcohols having quaternary or tertiary ammonium groups (carbamates, eg. Neostigmine) •Organic derivatives of phosphoric acid (organophosphates)
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ORGANOPHOSPHATES •Echothiophate - has a clinical value •Soman - an extremely potent "nerve gas" •Parathion & Malathion - (sulfur-containing phosphate) prodrugs that are converted to phosphate derivatives in animals and plants and used as insecticide MOA •Increase the concentration of endogenous acetylcholine at cholinoreceptors by inhibiting acetylcholinesterase enzyme
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- "irreversible" cholinesterase inhibitor
Organophosphates
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- "reversible" cholinesterase inhibitor
Edrophonium and Carbamates
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The EYE •Glaucoma - a disease characterized by increased intraocular pressure •Acute angle-closure glaucoma - a medical emergency that is frequently treated initially with drugs but usually requires surgery for permanent correction •Accomodative esotropia (strabismus caused by hypermetropic accomodative error)
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The EYE - a disease characterized by increased intraocular pressure
•Glaucoma
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- a medical emergency that is frequently treated initially with drugs but usually requires surgery for permanent correction
•Acute angle-closure glaucoma
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•(strabismus caused by hypermetropic accomodative error
Accomodative esotropia
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GI and URINARY TRACTS •Postoperative atony - paralysis of the stomach or bowel following surgical manipulation •Neurogenic bladder
…
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•Myasthenia gravis •Curare-induced neuromuscular paralysis..
Neuromuscular Junction
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In HEART •———- was used to treat supraventricular tachyarrhythmias
Edrophonium
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In Central Nervous System •———-(Cognex) - drug with anticholinesterase and other cholinomimetic actions used for the treatment of mild to moderate Alzheimer's disease
TACRINE
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Donepezil - Aricept •Galantamine - Reminyl •Rivastigmine - Exelon
…
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Short-Acting Cholinesterase Inhibitor
EDROPHONIUM Myasthenia Gravis AMBENONIUM
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•Tensilon® •MOA: Binds briefly to active site of AChE and prevents access of ACh •Effects: Amplifies all actions of ACh (increases parasympathetic activity and somatic neuromuscular transmission) CA: Diagnosis and acute treatment of myasthenia gravis •Toxicity: Parasympathomimetic excess
EDROPHONIUM
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•an autoimmune disease affecting skeletal muscle neuromuscular junctions •S/Sx: ptosis, diplopia, difficulty in swallowing and extremity weakness ium given IV after baseline muscle strength is measured •if no reaction occurs after 45 sec, an additional 8 mg may be injected •Positive result = the patient has improvement in muscle strength that lasts for 5 minutes
Myasthenia Gravis
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•Mytelase®
AMBENONIUM
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Intermediate-Acting Cholinesterase Inhibitors
NEOSTIGMINE PYRIDOSTIGMINE PHYSOSTIGMINE RIVASTIGMINE
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•Prostigmin® •MOA: forms covalent bond with AChE, but hydrolyzed and released •Effect: like Edrophonium but longer-acting •CA: Myasthenia gravis
NEOSTIGMINE
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•Mestinon®, Regonol® •Like neostigmine, but longer-acting •also used in myasthenia gravis
PYRIDOSTIGMINE
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•Eserine® •like neostigmine •a natural alkaloid tertiary amine •enters CNS
PHYSOSTIGMINE
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•Exelon®
RIVASTIGMINE
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Long-Acting Cholinesterase Inhibitor
Echothiophate Malathion Parathion Sarin TOXICITY •Antidote: ATROPINE •Organophosphate Posioning: ATROPINE, DIAZEPAM, PRALIDOXIME
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•MOA: like neostigmine, but released more slowly •Obsolete - was used in glaucoma
Echothiophate
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•insecticide •relatively safe for mammals and birds because metabolized by other enzymes to inactive products •some medical use as ectoparasiticide
Malathion
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•Insecticide •Dangerous for all animals •Toxicity is important because of agricultural use and exposure of farm workers
Parathion
52
•"Nerve gas" •used exclusively in warfare and terrorism
Sarin
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Pharmacology (7 decks)

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