LESSON 3 & 5 (M) Flashcards
It has 3 division which are:
Sympathetic
Parasympatheti c
Enteric
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
“fight-flight” response
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
neurotransmitter: norepinephrine or
noradrenaline
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
majority of the sympathetic fibers are adrenergic
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
craniosacral outflow
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
“rest-digest” response
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
neurotransmitter: acetylcholine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
True or false
Both are under CHOLINERGIC AGONISTS
When the Sympathetic is stimulated, there is increase in BP, HR, and respiratory rate. While the Parasympathetic when stimulated, there is decrease in BP and HR
True
also known as the brain of the gut
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
myenteric (Auerbach’s) plexus
submucosal (Meissner’s) plexus
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
act on the receptors activated by acetylcholine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
choline acetyltransferase catalyzes the reaction of choline with acetyl coenzyme A
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
packaged into presynaptic vesicles
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
release of their contents into synaptic space
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
diffuses across synaptic space & binds to either postsynaptic receptors on target cell or to presynaptic receptors in the membrane that released the acetylcholine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
→ choline & acetate
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
may be recaptured by the Na-coupled, high affinity uptake system
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
SYNAPSE
→ a communication between the neuron and the effector cell
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
found in the axon terminal
PRESYNAPTIC MEMBRANE
P
found in the effector or target cell
POSTSYNAPTIC MEMBRANE
parts of a synapse are the: (1) presynaptic membrane and
(2) postsynaptic membrane
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
→ area of myelinated axon which is not myelinated
→ does not have a covering of myelin or no myelin sheath
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
the other part of the axon that is not covered with myelin is
the _______
node of Ranvier
Once the action potential arrives at the nerve ending, then there is now an influx of ____ into the cell
calcium
→ Muscarinic Receptors
→ Nicotinic Receptors
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
→ Muscarinic Receptors
→ Nicotinic Receptors
milliseconds; chemical synapse; found in cell membrane
(extracellular)
NICOTINIC RECEPTORS
second messengers/neuromodulators amplify the duration
and intensity of the signal
MUSCARINIC RECEPTORS
primarily on autonomic effector cells innervated by
postganglionic parasympathetic nerve
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
M1 Receptors
M2 Receptors
M3 Receptors
M4 & M5 Receptors
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
→ “neural”
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
M1 receptors
→ “cardiac”
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
M2 receptor
“glandular/smooth muscle”
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
M3 receptor
CNS
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
M4 & M5 receptors
True or false
Acetylcholine promotes the secretion of hydrochloric acid by the parietal cells in the stomach.
True
True or false
The action of cholinergic agonists on the heart is to decrease the heart rate and decrease the cardiac contraction meaning (-) negative chronotropic and (-) negative inotropic.
True
CHOLINOMIMETIC DRUGS
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
bind to and active muscarinic or nicotinic receptors
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
Direct-Acting Cholinomimetic
produce their primary effects by inhibiting acetylcholinesterase which hydrolyzes acetylcholine to choline & acetate
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
Indirect-Acting Cholinomimetic
Naturally- Occurring Alkaloids
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
o Pilocarpine
o Muscarine
o Arecholine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
(-) chronotropic and (-) inotropic effect.
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
→ bronchoconstriction
→ increase in tracheobronchial secretion
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
→ increase in voiding pressure
→ increase in ureteral peristalsis
(promotion of urination)
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
increase in GI motility and increase in HCl production in the stomach
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
increase in GI motility and increase in HCl production in the stomach
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
stimulation of secretion of lacrimal, nasopharyngeal, salivary, & sweat glands (increase in secretion)
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
in the eyes, miosis or contraction of the pupil and accommodation for near vision
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
the substance responsible for this vasodilation is the nitric oxide
(NO)
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
BETHANECHOL
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
therapeutic uses:
o treatment of urinary retention & inadequate emptying in
post-op urinary retention
o stimulates peristalsis, increase in motility, increase in resting
lower esophageal sphincter pressure
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A.
BETHANECHOL
therapeutic uses:
o miotic agent to treat glaucoma by causing pupillary
contraction & decrease in intraocular pressure
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
CARBACHOL
treatment of xerostomia following head & neck radiation
treatment or associated with Sjogren syndrome
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
PILOCARPINE
XEROSTOMIA
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
a chronic autoimmune disorder that happens when the immune system attacks the glands that make moisture in the eyes, mouth, and other parts of the body.
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
SJOGREN SYNDROME
terminates the action of acetylcholine
acetylcholinesterase
inhibit the action of cholinesterases
anticholinesterase
True or false
by inhibiting acetylcholinesterase, they increase the endogenous acetylcholine concentration in the synaptic clefts and neuroeffector junctions
True
→ Edrophonium
→ Tacrine
→ Donepezil
→ Propidium
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
Reversible Inhibitors
→ Physostigmine
→ Neostigmine
→ Rivastigmine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
Carbamoylating Inhibitors
→ Soman
→ Sarin
→ Malathion
→ Echothiophate
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
Organophosphate Inhibitors
atony of smooth muscle of GIT & UB
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
thus can penetrate the blood-brain barrier
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
PHYSOSTIGMINE
NEOSTIGMINE
→ does not enter the CNS
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
used for chronic management of myasthenia gravis
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
PYRIDOSTIGMINE
DECARIUM
→ used for glaucoma
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
used for diagnosis of myasthenia gravis
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
EDROPHONIUM
used to slow the progression of Alzheimer’s disease
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
TACRINE, DONEPEZIL, RIVASTIGMINE, GALANTAMINE
What are the drugs used for Insecticides?
Sarin, Soiman
Malathion, Diazinon
Malathion, Diazinon
What are the nerve gases?
Sarin, Soiman
Malathion, Diazinon
What are the nerve gases?
Sarin, Soiman
→ ataxia
→ slurred speech
→ anorexia
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
What are the TREATMENT OF POISONING
Atropine
Pralidoxime
(Cholinergic agonist)
CONTRAINDICATION
o GI spasm
o hyperthyroidism
o acute iritis
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
→ adrenal gland which produces adrenaline or epinephrine
→ act on receptors that are stimulated by
norepinephrine/epinephrine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
are also known as sympathomimetic drugs
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
ADRENERGIC NEURON
→ releases norepinephrine as neurotransmitter
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
tyrosine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
o the metabolic precursor of norepinephrine
dihydroxyphenylalanine (DOPA)
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
is transported to synaptic vesicles
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
phenylethanolamine N-methyltransferase (PNMT) catalyzes the N-methylation of norepinephrine to epinephrine
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
vesicles fuse with cell membrane
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
norepinephrine expelled into synaptic cleft
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
a single neuron possesses thousands of varicosities, so one
impulse leads to the discharge of a few hundred vesicles scattered over a wide area
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
by acting on presynaptic B2 receptors, can regulate its own release, and also that of co-released ATP
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
chromogranin is released
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
Neuronal Uptake
Extraneuronal Uptake
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
- done by plasma membrane norepinephrine transporter (NET)
*75% recaptured & repackaged into the vesicles
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
Neuronal Uptake
- done by extraneuronal monoamine transporter (EMT)
- 25% captured by non-neuronal cells
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
Extraneuronal Uptake
METABOLIC DEGRADATION
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
monoamine oxidase (MAO)
catechol-O-methyltransferase (COMT)
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
abundant in noradrenergic nerve terminal, liver, intestinal epithelium
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
monoamine oxidase (MAO)
present in adrenal medulla
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
catechol-O-methyltransferase (COMT)
ALPHA RECEPTORS
BETA RECEPTORS
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
→ coupled to phospholipase C & produce their effects mainly by the release of intracellular calcium
→ present on postsynaptic membrane of effector cells
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
A1
→ coupled to adenylyl cyclase & decrease cAMP formation, inhibit calcium channels & activate potassium channels
→ primarily on presynaptic nerve endings
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
A2
→ also a G-protein coupled receptor
→ act by stimulating adenyl cyclase → converts ATP to cAMP
o adenyl cyclase is a G protein
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
BETA RECEPTORS
→ mainly in the heart
→ (+) inotropic & chronotropic effects
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
B1
causes smooth muscle relaxation in many organs
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
B2
hepatic glycogenolysis
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
A1
mydriasis
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
A1
→ inhibition of transmitter release, platelet aggregation, contraction of vascular smooth muscle
→ inhibition of insulin release
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
A2
→ increase in force & cardiac rate
→ delayed cardiac hypertrophy
→ release of renin
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
B1
muscle tremor
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
B2
lipolysis
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
B3
longer half-lives
NON-CATECHOLAMINES
(ADRENERGIC AGONISTS)
o epinephrine
o norepinephrine
o dopamine
o isoproterenol
CATECHOLAMINES
(ADRENERGIC AGONISTS)
o phenylephrine
o ephedrine
o amphetamine
NON-CATECHOLAMINES
(ADRENERGIC AGONISTS)
epinephrine, norepinephrine, isoproterenol, phenylephrine
DIRECT-ACTING SYMPATHOMIMETIC DRUGS
ADRENERGIC AGONISTS
act directly on alpha & beta receptors → produce effects similar to those following of sympathetic nerve or release of
epinephrine from adrenal medulla
DIRECT-ACTING SYMPATHOMIMETIC DRUGS
may exhibit selectivity
phenylephrine
A1
terbutaline
B2
DIRECT-ACTING SYMPATHOMIMETIC DRUGS
amphetamine, cocaine, tyramine
INDIRECT-ACTING SYMPATHOMIMETIC DRUGS
action is mainly to prevent reuptake of neurotransmitter back
into the terminal of the nerve where they come from, causing them to stay in the synaptic cleft; thus, there is enhancement of the action of the NT
INDIRECT-ACTING SYMPATHOMIMETIC DRUGS
→ ephedrine, pseudoephedrine, metaraminol, dopamine
→ indirectly release norepinephrine and also directly activate
receptors
MIXED-ACTING SYMPATHOMIMETIC DRUGS
→ potent stimulant of both alpha & beta receptors
→ a very potent VC and cardiac stimulant
o usually used in heart attacks
EPINEPHRINE
AA
a powerful cardiac stimulant, acting directly on the predominant
B1 receptors of myocardium & of cells of pacemaker &
conducting tissues
EPINEPHRINE
AA
increase in circulating WBCs
EPINEPHRINE
AA
*anaphylaxis–drug of choice)
* prolong the action of local anesthetics
EPINEPHRINE
→ 10-20% adrenal medulla
→ 97% pheochromocytoma
NOREPINEPHRINE
→ potent alpha agonist
→ ineffective when given orally
NOREPINEPHRINE
→ poorly absorbed from sites of subcutaneous injection
→ rapidly inactivated by uptake & actions of MAO & COMT
NOREPINEPHRINE
Baroreceptor Reflex
NOREPINEPHRINE
THERAPEUTIC USE
→ as vasoconstrictor to raise or support BP (treatment of shock)
NOREPINEPHRINE
→ immediate metabolic precursor of norepinephrine & epinephrine
→ central NT important in regulation of movement
DOPAMINE
→ ineffective when given orally
→ occurs naturally in basal ganglia & in adrenal medulla
DOPAMINE
a deficiency of dopamine
Parkinson’s disease
ischemic necrosis & sloughing
→ should be avoided in patients taking MAO inhibitor & TCA
DOPAMINE
→ a potent non-selective B receptor agonist
→ intense stimulation of the heart → increase HR and force of
contraction
→ cardiac effects may lead to palpitations, sinus tachycardia,
serious arrhythmias
ISOPROTERENOL
→ synthetic, direct-acting catecholamine
→ increases the HR & force of contraction
DOBUTAMINE
True or false
in the treatment of asthma, B2 agonists are used to activate pulmonary receptors that relax bronchial smooth muscles & decrease airway resistance
True
B2-SELECTIVE ADRENERGIC AGONISTS
resistant to methylation by COMT
METAPROTERENOL
→ bronchodilator
→ effective when given orally, subcutaneously, and through
inhalation:
TERBUTALINE
→ known as salbutamol
→ administered orally or inhalation
ALBUTEROL (VENTOLIN)
→ additive effect when used in combination with inhaled
Ipratropium or Theophylline
→ highly lipophilic
LONG-ACTING B2 ADRENERGIC AGONISTS
→ used as uterine relaxant
→ administered through IV to arrest premature labor
RITODRINE
→ activates B3 adrenergic receptors on the detrusor muscle of the urinary bladder to facilitate filling of bladder & storage of urine
→ uses:
o treatment of overactive bladder (urinary urgency,
frequency, urge incontinence)
MIRABEGRON
uses:
o treatment of hypotension (including orthostatic hypotension)
& shock
A1-SELECTIVE ADRENERGIC AGONISTS
used primarily for the treatment of systemic hypertension
A2-SELECTIVE ADRENERGIC AGONISTS
treating and preparing addictive subjects for withdrawal from narcotics, alcohol, and tobacco
CLONIDINE
→ has powerful CNS stimulant actions → depression of appetite
AMPHETAMINE
o hyperactivity in children
o narcolepsy
o appetite control
AMPHETAMINE
→ by-product of tyrosine metabolism
→ found in fermented foods such as cheese causing a “cheese
effect”
TYRAMINE
reuptake inhibitor by blocking Na-K activated ATPase on cell membrane of adrenergic neuron → norepinephrine accumulates in synaptic space
COCAINE
→ enhances the release of norepinephrine from sympathetic neurons
→ uses:
o nasal decongestant (discontinued) o hypotension (in spinal anesthesia) o promote urinary continence
EPHEDRINE
primarily used to treat nasal congestion or congestion of Eustachian tubes
PSEUDOEPHEDRINE
→ shares the pharmacologic properties of Ephedrine but less CNS stimulation
→ may increase the risk of hemorrhagic stroke
PHENYLPROPANOLAMINE
Regulates the sale of Ephedrine, Phenylpropanolamine, & Pseudoephedrine which can be used as precursors in the illicit manufacture of amphetamine & methamphetamine.
PHENYLPROPANOLAMINE
sympathomimetic
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
parasympathomimetic
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
(-) negative chronotropic and (-) negative inotropic.
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
A
o acetylcholine
o synthetic esters
Cholinergic Esters
Carbachol, Bethanechol
Cholinergic Esters
o Pilocarpine
o Muscarine
o Arecholine
Naturally- Occurring Alkaloids
in the eyes, miosis or contraction of the pupil and accommodation for near vision
ACETYLCHOLINE
treatment of xerostomia following head & neck radiation
treatment or associated with Sjogren syndrome
PILOCARPINE
drug of choice in emergency lowering of intraocular pressure in glaucoma
PILOCARPINE
→ (+) inotropic & chronotropic effects
A. CHOLINERGIC AGONISTS
B. ADRENERGIC AGONISTS
B
Beta receptors
is the drug of choice for shock (increases the BP)
dopamine