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PHARM-EXAM1
CHOLINERGIC AGENTS AND AGENT BLOCKERS
72
Pharmacology
Graduate
12/02/2012

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Term
Nicotinic receptors
Definition
Located in ganglia of both the PSNS and SNS
Term
Nicotinic receptors
Definition
stimulated by alkaloid nicotine
Term
Muscarinic receptors
Definition
located postsynaptically:
smooth muscle: increase GI
cardiac muscle: decrease HR
Glands of PSNS fibers: increase secreation
Term
Muscarinic receptors
Definition
stimulated by alkaloid muscarine (mushroom
Term
Cholinergic Direct-acting agonist
Definition
bind to cholinergic receptors causing stimulation (muscarinic or nicotinic receptors)
Term
Cholinergic Indirect-acting agent
Definition
Inhibit the enzyme ecetylcholinesterase so the enzyme can't hydrolyzes ACH to choline and acetic acid resulting more Ach is available at the synaptic clefts
Term
Cholinergic Indirect-acting agent
Definition
Inhibit the enzyme pseudocholinesterase plays little role in action of indirect acting agents
Term
Cholinergic Indirect-acting agent
Definition
Reversible bind to cholinesterase
Or Irreversible bind to cholinesterase and form a permanent covalent bond
Term
Cholinergic Direct-acting agonist
Definition
Acetylcholine (muscarinic) or esters of choline
Term
Acetycholine
Methacholine
Carbachol(ine)
Bethanechol(ine)
Definition
are 4 important esters of Direct acting cholinoreceptor agonists
Term
Methacholine
Definition
Direct acting Cholinergic agonist
Used for:
glaucoma
Atropine poisoning
Diagnostic in Pheochromocytoma
Raynauds
Paroxysmal Atrial Tachycardia
Term
Methacholine
Definition
SE:
cause MYOSIC MYOSIC MYOSHIT
Term
Methacholine
Definition
can be cholilne: eyedrops
Term
Carbecholine
Definition
Direct acting
SE: cause MYOSIC MYOSIC again
USED to treat:
glaucoma
intracular surgery
Term
Bethanechol
Definition
Direct acting
Indication:
post op
Urinary retention
Term
Pilocarpine
Definition
Direct acting
Natural occuring agent
Semisynthetic
Treat:
Glaucoma
used as eye drop
MOA:
miosis of the pupil
Term
Pilocarpine
Definition
Direct acting Oral form called Salagel with parotid gland damage
Term
Edrophonium (alchohol)
Definition
Cholinesesterase inhibitors
Used for Myasthenia Gravis
Arrythmias
Term
Echothiphate (organophosphate)
Definition
Cholinesesterase inhibitors
Glaucoma
Term
Carbamates
Definition
Cholinesesterase inhibitors
Term
Neostigmine
Definition
Cholinesesterase inhibitors
treat Myastinia gravis, illeus
Term
Pyridostigmine MG
Definition
Cholinesesterase inhibitors
Term
Ambenonium MG
Definition
Cholinesesterase inhibitors
Term
Demecarium
Definition
Cholinesesterase inhibitors
treat glaucoma
Term
Acetycholine
Methacholine
Carbachol(ine)
Bethanechol(ine)
Definition
are poorly absorbed and distributed in CNS bc they are hydrophilic
Term
Acetycholine
Methacholine
Carbachol(ine)
Bethanechol(ine)
Definition
ACH rapid hydrolysis must give dose IV

Remaining are more resistant to hydrolysis Metha>carbachol>bethanechol
Term
Cholinergic Agents agonist
Definition
SE:
SLUDGE
Salivation
Lacrimaiton
Urinary incontinence
Diarrhea
Gastrointestinal cramps
Emesis
Term
Organophosphate insecticides malthione, parathione (fertilizer)
Definition
MOA:
binds to ACHesterase enzyme "irreversibly" and cause toxicity
Term
Organophosphate insecticides malthione, parathione (fertilizer)
Definition
Net effect:
Mucarinic and nicotinic toxicity
blurred vision
bradycardia
Nv
Diarrhea
Sludge
Axonal degeneration and demyelination of nerves
Term
Pralidoxime (2-Pam) iv
Definition
to treat Organophosphate toxicity by reverse binding of drug to ACHesterase enzyme and allow enzyme to hydrolyze ACH
Term
ATROPHINE
Definition
is given first to prevent Tachycardia
Term
ATROPHINE
Definition
Organophosphate treatment of symptoms
Term
Cholinergic agonist
Definition
at recommended doses, primarily affect the Muscarinic receptors
Term
Cholinergic agonist
Definition
at high doses, cholinergics stimulate the NICOTINIC receptors
Term
Cholinergic agonist
Definition
Desired effects from muscarinic receptor stimulation
Term
Cholinergic agonist
Definition
Undesirable effects are due to stimulation of the nicotinic receptors
Term
ACH
CARBACHOL
PILOCARPINE
BARTHENECOLINE
METHANCOLINE
Definition
Direct acting agonist to:
reduce intraocular pressure
useful for glaucoma and intraocular surgery

Topical application due to poor oral absorption
Term
ACH
CARBACHOL
PILOCARPINE
BARTHENECOLINE
METHANCOLINE
Definition
Direct acting agonist:
increases tone and motility of bladder and GI tract
relaxes sphincters in bladder and GI tract allowing them to empty

Helpful for postsurgical atony of the bladder and GI tract
Term
ACH
CARBACHOL
PILOCARPINE
BARTHENECOLINE
METHANCOLINE
Definition
oral dose or SC injection
Term
Physostigmine
Pyridostigmine
Definition
Indirect-Acting ACH agonist
Cause skeletal muscle contractions
Used for Diagnosis and treatment of Myasthenia Gravis
Used to reverse Neuromuscular blocking agents
Used to reverse Anticholinergic Poisoning (antidote)
Term
DONEPEZIL
TACRINE
Definition
Indirect Acting ACH agonist to treat
from mild to moderate Alzheimer's disease
and helps to increase or maintain memory and learning capabilities
Term
ACH AGONISTS
Definition
SE are a result of overstimulaiton of PSNS
bradycardia
hypotension
conduction abnomalities (AV block and cardiac arrest)
Headache
Dizziness
Convulsions
Abdominal cramps
Increased secretions
Nausea
Vomiting
Increased bronchial secreations
Bronchospasms
Lacrimation
Sweating
Salivation
Loss of Binocular accomodation
Miosis
Term
Anticholinergics
Antihistamines
Sympathomimetics
Definition
antagonize cholinergic agents resulting in decreased responses
Term
Donepezil
Definition
is used to manage Alzheimer's symptoms not to cure
It may take up to 6 weeks to reach therapeutic effects
Term
Atropine
Definition
is the antidote for cholinergics
Term
Atropine
Definition
atropine belladonna-beautiful naked girl
Term
Cholinergic (muscarinic) Blocking agents
Definition
competitive antagonists compete with ACH
and block ACH at muscarinic receptors in PSNS reversible
As a result, Ach is unable to bind to the receptor site to cause a cholinergic effect
Term
ATROPINE
Definition
NOT ABSORBED IN THE GI
has halflife is 1/2 hr
Term
Cholinergic (muscarinic) Blocking agents
Definition
Most are well absorbed from the GI
Widely distributed throughout the body in CNS in 30min-1hr
Term
SCOPOLAMINE
Definition
ACH ANTAGONIST
PATCH FOR MOTION SICKNESS
Term
ATROPINE (NATURAL)
Definition
SYNTHETIC: ANISOTROPINE
SEMISYNTHETIC: CLIDINIUM
Term
BELLADONNA
Definition
SYTHETIC: DICYCLOMINE
SEMISYN: GLYCOPYRROLATE
Term
HYOSCYAMINE
Definition
SYNTHETIC: HEXOCYCLIUM
SEMISYN: HOMATROPINE
Term
SCOPOLAMINE
Definition
SYNTHETIC: IPRATROPIUM, OXYBUTYNIN, TOLTERODINE
SEMI: ISOPRPAMIDE, PROPANTHELINE, TRIDIHEXETHYL
Term
DONNATAL
Definition
HAS BELLADONNA
Term
ONE DOSE OF ATROPINE
Definition
SAVE A PATIENT LIFE IN AN OR
Term
DOBUTAMINE
Definition
give to end stage CHF patient
Term
Cholinergic (muscarinic) Blocking agents
Definition
small doses: decrease heart rate, decrease muscle rigidity and tremors for Parkinson's disease and drug-induced extrapyramidal reactions

Large doses: block inhibitory vagal effects on SA and AV node resulting increase heart rate, drowsiness, disorientation, halluciantions
Term
Cholinergic (muscarinic) Blocking agents
Definition
Dilated pupils (mydriasis)
Decreased accommodation due to paralysis
of ciliary muscle (cycloplegia)
Term
Cholinergic (muscarinic) Blocking agents
Definition
Relax smooth muscle tone of GI tract
Decrease Intestinal and gastric secretion
Decrease motility and peristalsis
Term
Cholinergic (muscarinic) Blocking agents
Definition
Relaxed detrusor muscle
Increased constriction of internal sphincter resulting urinary retention
Term
Cholinergic (muscarinic) Blocking agents
Definition
Decreased Bronchial secretions,
Decreased salivation
Decreased sweating
Decreased Bronchial secretions
Dilated bronchial airways
Term
ATROPINE
Definition
USED PRIMARILY FOR CARDIOVAS DISORDERS
SINUS NODE DYSFUNCTION
SYMPTOMATIC SECOND-DEGREE HEART BLOCK
SINUS BRADYCARDIA WITH HEMODYNAMIC COMPROMISE
Term
Cholinergic (muscarinic) Blocking agents
Definition
Dcreased secretions from nose, mouth, pharynx, bronchi
Relax smooth musccles in bronchi and bronchioles
Decreased airway resistance
Bronchodilation
Term
Cholinergic (muscarinic) Blocking agents-respiratory agents
Definition
used to treat:
exercise induced bronchospasms
chronic bronchitis
asthma
chronic obstructive pulmonary disease
Term
Cholinergic (muscarinic) Blocking agents
Definition
resulting GI in:
decreased secretions
relaxation of smooth muscle
decreased GI motility and peristalsis
Used to treat:
Peptic ulcer disease
Irritable bowel disease
GI hypersecretory states
Term
Cholinergic (muscarinic) Blocking agents
Definition
Relaxed detrusor muscle of the bladder
Increased constriction of the internal sphinter
Reflex neurogenic bladder
Incontinence
Decrease Urination
Term
Cholinergic (muscarinic) Blocking agents
Definition
SE:
increased hr
dysrhythmias
CNS excitation
restlessness
irritability
disorientation
hallucination
delirium
Term
Cholinergic (muscarinic) Blocking agents
Definition
SE:
dilated pupils,
decreased visual accomodation
increased intraocular pressure
decreased salivation
decreased gastric secretions
decreased motility
Term
Cholinergic (muscarinic) Blocking agents
Definition
SE:
urinary retention
decreased sweating
decreased bronchial
Term
Cholinergic (muscarinic) Blocking agents
Definition
Antihistimines,
Phenothiazines
Tricyclic Antidepressant
MAOIs
Term
Cholinergic (muscarinic) Blocking agents
Definition
SE:
allergies
presence of BPH
glaucoma
tachycardia
MI
CHF
hiatal hernia
GI and GU obstruction
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