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Neuro Test Three TTUHSC
Neuro Test Three TTUHSC
563
Pharmacology
Professional
11/18/2013

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Term
Nicotinic receptor antagonists are mainly used to produce _______ during general anesthesia so less anesthetic is required.
Definition
skeletal muscle relaxation
Term
Two basic types of neuromuscular blocking
agents: ________.
Definition
Competitive blockers-non-depolarizing/depolarizing
Term
Competitive blockers-non-depolarizing neuromuscular blockers compete with ________ and act strictly as _______.
Definition
ACh

ACh antagonists
Term
Competitive blockers-non-depolarizing neuromuscular blockers prototype __________.
Definition
d-tubocurarine
Term
Depolarizing neuromuscular blockers are antagonists/agonists?
Definition
agonists
Term
Depolarizing neuromuscular blockers act by causing _______ followed by _________.
Definition
persistent depolarization followed by receptor desens
Term
Depolarizing neuromuscular blockers produce _______ prior to muscle relaxation.
Definition
fasiculations
Term
Depolarizing neuromuscular blockers elevate _____ plasma levels.
Definition
K+
Term
Depolarizing neuromuscular blockers prototype _________.
Definition
Succinylcholine
Term
_________ neuromuscular blocker has cardiovascular effects.
Definition
d-tubocurarine
Term
d-tubocurarine ______ b.p. by releasing __________ and blocking __________.
Definition
lowers

histamine and blocking SNS
Term
__________- not too much cardiovascular action relative to d-tubocurarine but can cause _______ in b.p. if given rapidly also, can cause _________.
Definition
Pancuronium

increase

tachycardia
Term
_________- a non-depolarizing blocker similar to pancuronium.
Definition
Doxacurium
Term
_______- almost no histamine release- can cause tachycardia (in rare cases).
Definition
Vecuronium
Term
_________ - a non-depolarizing blocker similar to vecuronium.
Definition
Atracurium
Term
Succinylcholine releases _______ & tends to slow ________.
Definition
vasodilator histamine

heart rate
Term
Succinylcholine reduces effectiveness
of _______.
Definition
digitalis
Term
Succinylcholine may be unwise to use in patients taking digitalis-like drugs that ________ or _________.
Definition
compete with K+ to increase ventricular contraction or diuretics that lower plasma K+ levels
Term
Succinylcholine length of duration?
Definition
5 minutes (short)
Term
Mivacurium is a slow/fast acting _________ neuromuscular blocker similar to pancuronium, but its onset of action is significantly slower/faster than succinylcholine.
Definition
fast

non-deploarizing blocker

slower
Term
Neuromuscular blockers that _______ such as: ___________ are dangerous to use in asthmatics, because they cause cause __________.
Definition
release histamine

d-tubocurarine, succinylcholine and mivacurium

broncho- constriction
Term
Depolarizing Neuromuscular blocker _______ elevates plasma K+ levels
Definition
succinylcholine
Term
Succinylcholine can trigger an attack
of ________ when its levels greatly elevated.
Definition
malignant hyperthermia- Ca2+
Term
_______ neuromuscular blocker can elevate _________ pressure & should not be used in patients with ___________.
Definition
succinylcholine

intraocular

narrow-angle glaucoma
Term
Too much d-tubocurarine causes ________.
Definition
skeletal muscle paralysis
Term
d-tubocurarine blockade can be overridden with __________.
Definition
AChE inhibitor
Term
d-tubocurarine is rarely used bc _______.
Definition
cardiovascular difficulties
Term
d-tubocurarine administered _________.
Definition
IV (broken down orally)
Term
d-tubocurarine is only used as a _______ during general anesthesia
Definition
surgical adjunct
Term
d-tubocurarine Duration of action: ________.
Definition
60-80 min
Term
Pancuronium+ is short/long acting ________ neuromuscular blocker.
Definition
long acting competitive
Term
Pancuronium+ doesn't _______ or _______ unlike d-tubocurarine+.
Definition
release histamine or block ganglionic SNS
Term
Pancuronium+ is a better drug than d-tubocurarine+, to use in _________ and ________.
Definition
patients with cardiovascular issues or asthama
Term
__________ long-acting competitive blocker similar to pancuronium that also doesn't affect cardio much.
Definition
Doxacuronium+
Term
Vecuronium+ ______ acting and has what affect on ganglionic SNS and histamine?
Definition
intermediate

no
Term
Vecuronium+ is dangerous in ______ patients sensitized to _______.
Definition
hyperthyroid patients sensitized
to catecholamines
Term
Only Depolarizing Neuromuscular Blocking Drug used?
Definition
succinylcholine+
Term
succinylcholine+ has a very short duration of action- 5 min due to breakdown by _______ in the plasma
Definition
pseudocholinesterase
Term
succinylcholine mainly used for short-term procedures such as _______ & to protect skeletal muscle during _______ therapy
Definition
endotracheal intubation

electroshock
Term
succinylcholine+ cause histamine release?
Definition
Yes, therefore will lower BP
Term
succinylcholine, a Depolarizing Neuromuscular Blocking Drug, causes ________cardia by ________.
Definition
bradycardia

stimulating Vagus
Term
succinylcholine elevates?
Definition
K+
Term
succinylcholine can cause prolonged apnea (or respiratory arrest) in patients with _____________.
Definition
atypical pseudocholinesterase (can not hydrolyze succinylcholine as effectively)
Term
succinylcholine antidote?
Definition
none
Term
succinylcholine more prone to cause ______ than other skeletal muscle relaxants.
Definition
malignant hyperthermia
Term
d-tubocurarine and competitive drug antidote? Which does what?
Definition
Neostigmine inhibits AChE,
Term
Asthma patients should not be given __________ Neuromuscular Blockers.
Definition
Asthma-d-tubocurarine, mivacurium,
and succinylcholine
Term
Narrow-angle glaucoma patients should not be given __________ Neuromuscular Blockers.
Definition
succinylcholine
Term
Hyperthyroid patients should not be given __________ Neuromuscular Blockers.
Definition
vecuronium
Term
Drugs Acting on Skeletal Muscle to Produce Relaxation: ________.
Definition
Dantrolene
Term
Dantrolene acts to ________ ______junctionally in skeletal muscle by _________.
Definition
Reduce intracellular Ca2+ postjunctionally

reducing Ca2+ realease from the SER.
Term
Dantrolene reduces Intra Ca2+ by acting on the SER and blocking _____.
Definition
ryanodine receptor channel
Term
Dantrolene causes ________.
Definition
muscle relaxation
Term
Dantrolene is used to provide muscle relaxation for pts. with: ________.
Definition
Stroke, MS, or Malignant Hyperthemia
Term
Dantrolene causes local or generalized muscle weakness?
Definition
Generalized
Term
Malignant hyperthermia can often occur in surgical patients who are given certain __________ in conjunction with ___________.
Definition
general anesthetics (e.g., halothane) in conjunction with succinylcholine
Term
Why is Dantrolene used for treating Malignant Hyperthemia?
Definition
Dantrolene helpful because it reduces Ca2+ release & prevents explosive muscle contraction
Term
Dantrolene influence on prejunctional release of ACh?
Definition
None
Term
Drugs that Act Prejunctionally for muscle relaxation do what ?
Definition
Reduce ACh Release
Term
Drug that acts Prejunctionally to reduce ACh release?
Definition
Botulism
Term
Botulism toxin is used to treat: ____________.
Definition
eye to treat blepharospasm (twitch of eyelid)

cerebral palsy spasms

into the eye to reduce spasmodic ocular movements
Term
Drugs Acting Centrally to Produce Skeletal Muscle Relaxation: __________
Definition
Cyclobenzaprine
Term
Cyclobenzaprine is useful for treating ________.
Definition
muscle spasms
Term
Cyclobenzaprine is useful for treating muscle spasms over Valium because ________.
Definition
dependence issues
Term
Cyclobenzaprine overall effect?
Definition
Blocks the reuptake of NE
Term
Cyclobenzaprine should not be taken simultaneously with a ______.
Definition
MOA inhibitor
Term
Cyclobenzaprine side effects?
Definition
dry mouth, drowsiness, tachycardia,
& blurred vision
Term
ACh acts at ______ and ______ receptors once before its hydrolysis by the enzyme AChE.
Definition
nicotinic

muscarinic
Term
All of the therapeutically useful cholinesterase inhibitors inhibit _______
Definition
AChE
Term
Pseudocholinesterase- more/less sensitive to inhibition by organophosphate compounds than AChE
Definition
More
Term
Organophosphate compounds are __________.
Definition
irreversible AChE inhibitors
Term
Pseudocholinesterase in?
Definition
the plasma and glial cells
Term
In cases of suspected organophosphate
intoxication, plasma pseudocholinesterase typically inhibited ______% when RBC AChE inhibited _____%
Definition
100%

50%
Term
ACh binds to _____ different sites on AChE before its breakdown.
Definition
two
Term
______ site on AChE binds _______ moiety of ACh.
Definition
Anionic

positively charged choline+
Term
_______ site- is the active site of AChE & binds _________ of ACh.
Definition
Esteratic

carbonyl carbon
Term
Even _______ can act as an AChE inhibitor, but a very weak one, because it ________
Definition
choline

binds one of the sites and competes with ACh then
Term
Some AChE inhibitors positively charged & act directly on the ________ to produce a _______ action.
Definition
nicotinic receptor site

positive agonist
Term
Nicotinic receptors at ______ appear more sensitive to agonist action of positively charged AChE inhibitors than nicotinic receptors on ________.
Definition
motor endplate region

ganglia or adrenal medulla
Term
Types of AChE Inhibitors reversible: ____________.
Definition
a. Neostigmine+
b. Edrophonium+
c. Pyridostigmine+
d. Physostigmine
e. Tacrine
f. Donepezil
Term
Types of AChE Inhibitors irreversible: ____________.
Definition
a. Echothiophate+
b. DFP (Diisopropyl flourophosphate)
C. Parathion
d. Sarin
Term
Reversible AChE inhibitors do what?
Definition
compete with ACh for binding to anionic and esteratic sites by
carbamylating esteratic site
Term
Reversible AChE inhibitors form a stronger bond with ________ site than ACh and thus time for breakdown is __________.
Definition
esteric

longer (60-120 min)
Term
Neostigmine-hydrolyzed to _______ by AChE.
Definition
edrophonium
Term
Edrophonium is not ______, but irreversibly/reversibly inhibits AChE by ________.
Definition
not hydrolyzed by AChE

competes with ACh for binding to both
esteratic and anionic sites
Term
Edrophonium binds which AChE sites and is ______ acting?
Definition
both esteratic and anionic sites

very short, rapidly excreted
Term
Irreversible AChE Inhibitors act by?
Definition
Phosphorylate esteratic site
Term
Irreversible AChE Inhibitors act by Phosphorylating esteratic sites which knocks them out for _______ duration and therefore must be ___________.
Definition
2 weeks

new AChE must be synthesized
Term
Irreversible AChE Inhibitors should not be taken ________.
Definition
Extremely dangerous compounds-should not
be taken parenterally
Term
Irreversible AChE Inhibitors can kill by causing __________.
Definition
Respiratory arrest
Term
Irreversible AChE Inhibitors can kill by causing Respiratory arrest by __________.
Definition
Paralyze diaphragm and intercostal muscles by building up ACh at nicotinic receptors to high enough levels that nicotinic receptors are desensitized
Term
Some irreversible AChE inhibitors, __________, can cause delayed ______toxicity.
Definition
organophosphates

neurotoxicity
Term
Delayed neurotoxicity caused by some irreversible AChE inhibitors, organophosphates, can cause: ________ & appears _____ days after drug admin.
Definition
ataxia, muscle paralysis and demyelination and appears 8-14 days
after drug exposure
Term
Therapeutic Uses of AChE Inhibitors for disorders: ___________.
Definition
G.I. tract or bladder atony

Glaucoma - wide and narrow angle

Myasthenia gravis - treatment and diagnosis
Term
AChE Inhibitors can be used to terminate an overdose of a ________ like uncompetitive /competitive blocker.
Definition
Curare like competitive blocker
Term
AChE Inhibitors can be used to terminate an attack of ________.
Definition
supraventricular tachycardia
Term
Neostigmine+ is a _______ type of drug.
Definition
Reversible AChE Inhibitor
Term
Neostigmine+ CNS affect?
Definition
None + charge
Term
Neostigmine+ drug metabolism?
Definition
Is hydrolyzed to edrophonium by AChE
Term
Neostigmine+ duration of action?
Definition
2-4hrs
Term
Neostigmine+ is used to treat?
Definition
paralytic ileus or bladder atony

wide-and narrow-angle glaucoma
Term
Myasthenia gravis Ab against?
Definition
nicotinic receptor at motor endplate of
neuromuscular junction
Term
Muscle biopsy will show a decrease in
binding of ______ which correlates with severity of disease.
Definition
alpha bungarotoxin
Term
Myasthenia gravis Ab do not recognize nicotinic receptors on?
Definition
ganglia or adrenal medulla
Term
______ are sometimes used if AChE inhibitors are not working for Myasthenia gravis.
Definition
Steroids
Term
Myasthenic Syndrome (_______)
Definition
Lambert Eaton
Term
Myasthenic Syndrome (Lambert Eaton) is more common or rarer than MG?
Definition
Rarer
Term
Myasthenic Syndrome (Lambert Eaton) also involves ________.
Definition
muscle weakness
Term
Myasthenic Syndrome (Lambert Eaton) Ab against?
Definition
Ca2+ channel mediating ACh release from motor nerve terminal
Term
_______ is used to treat Lambert Eaton.
Definition
Guanidine
Term
______ is drug of treat Myasthenia gravis.
Definition
Pyridostigmine+
Term
Pyridostigmine is ____ charged and has ______ duration than
Definition
neostigmine (another reversible AChE inhibitor)
Term
Why is Pyridostigmine better than neostigmine for MG treatment?
Definition
Longer duration

Better absorbed

Fewer side effects
Term
Edrophonium+ binds?
Definition
Competitively binds to both the esteratic
& anionic sites
Term
Edrophonium+ DOA?
Definition
Very short (5 minutes)
Term
Edrophonium+ metabolism?
Definition
Not hydrolyzed like AChE
Term
Edrophonium+ excreted by?
Definition
Kidneys
Term
Edrophonium+ is the drug of choice for?
Definition
diagnosis of myasthenia gravis
Term
_______ is the drug of choice for the treatment of MG.
Definition
Pyridostigmine+
Term
Edrophonium+ can be used to treat disorder?
Definition
supraventricular tachycardia
Term
Edrophonium+ can be used to treat overdose of?
Definition
d-tubocurarine like drug
Term
Physostigmine type of drug?
Definition
reversible AChE inhibitor
Term
Physostigmine charge?
Definition
neutral will cross BBB
Term
Physostigmine is mainly used in the ______ in conjunction with _______ for the treatment of _______ until _______.
Definition
eye

pilocarpine

narrow angle glaucoma

iridectomy can be done
Term
Physostigmine can be used as the antidote for?
Definition
atropine intoxication
Term
Tacrine is a _____ type of drug?
Definition
Reversible AChE inhibitor
Term
Tacrine charge?
Definition
Not can cross BBB
Term
Tacrine crosses the BBB and ________.
Definition
raises ACh levels centrally
Term
Tacrine is used to treat?
Definition
Alzheimer's
Term
Tacrine & ________ are used to treat Alzheimer's.
Definition
Donepezil
Term
Donepezil has a high degree for selectivity of ________.
Definition
AChE in the CNS
Term
Donepezil exhibits less ________ than Tacrine (other drug for Alzheimer's)
Definition
Hepatic toxicity
Term
Irreversible AChE Inhibitors: ________.
Definition
a. Echothiophate+
b. DFP (Diisopropyl flourophosphate)
C. Parathion
d. Sarin
Term
Echothiophate charge?
Definition
+
Term
Echothiophate+ only used ______ to treat ______.
Definition
Only used topically in the eye, mainly for
wide angle glaucoma,
Term
_______ an organophosphate irreversible AChE inhibitor used as an insecticide.
Definition
Mipafox
Term
Mipafoxan organophosphate irreversible AChE inhibitor used as an insecticide causes delayed _______ ______days after exposure.
Definition
delayed neurotoxicity 8-14 days
Term
Parathion is a _______ type of drug.
Definition
Irreversible AChE Inhibitor
Term
Parathion is a ________ type of compound.
Definition
organophosphate
Term
Parathion is a potent _____ & ______.
Definition
insecticide & acaricide
Term
Parathion does not cause ______, like the insecticide _____ does.
Definition
delayed neurotoxicity

Mipafox
Term
Sarin is a ______ compound.
Definition
organophosphate
Term
Antidotes for Organophosphate Intoxication: ___________.
Definition
Pralidoxime+ (2-PAM)

Obidoxime (similar to Pralidoxime+)

Atropine
Term
Pralidoxime+ (2-PAM) MOA?
Definition
"Pulls" organophosphate off esteratic
site of AChE
Term
Atropine (an effective ______ antagonist)
Definition
muscarinic
Term
Atropine controls signs of muscarinic excess: ________, caused by ______.
Definition
Controls signs of muscarinic excess; it blocks muscarinic effects of excess salivation, miosis, bronchoconstriction, bronchiole secretions, &sweating caused by inhibition of AChE at muscarinic receptor sites.
Term
Atropine is used when?
Definition
Only needed for approximately two weeks during treatment for myasthenia gravis because muscarinic side effects of AChE inhibitors dissipate.
Term
Myasthenia Gravis An autoimmune disorder of function at the synapse between ______ motor neurons and skeletal muscle
Definition
cholinergic
Term
Myasthenia Gravis, antibodies against the ________.
Definition
nicotinic Acetylcholine (ACh) receptor
Term
Myasthenia Gravis typically affects the _____ muscles.
Definition
Cranial (ptosis)
Term
_____ is the transmitter at neuromuscular
junction (NMJ).
Definition
ACh
Term
Is atrophy present in MG?
Definition
No
Term
Is weakness present in MG?
Definition
Yes
Term
The weakness of MG is reversed by intravenous injection of inhibitors of acetylcholinesterase (______, _______, ________).
Definition
edrophonium, pyridostigmine, physostigmine
Term
Neostigmine increases the _____ of ACh.
Definition
duration of action
Term
In MG The amplitude of evoked ______ decreases rapidly.
Definition
compound action potentials
Term
In MG 15% of patients have a ________.
Definition
benign tumor of thymus
Term
In MG the density of ______ in muscle fibers is reduced.
Definition
density of ACh receptors
Term
ACh receptors are marked and detected using?
Definition
alpha-bungarotoxin (in MG reduced density on muscle fibers)
Term
Draining ______ from ______ improve symptoms of MG.
Definition
lymph from the thoracic lymph ducts
Term
In addition to draining the lymph, _______ procedure also improves symptoms of MG.
Definition
Plasmapheresis
Term
In the normal neuromuscular junction the amplitude of the end-plate potential is _________ (_________ principle)
Definition
very large,well above the threshold for a muscle action potential

large safety factor
Term
Because of the large amplitude of the end-plate potential (large safety factor) a muscle has _______ under repetitive stimulation.
Definition
compound muscle action potential is constant and invariable
Term
In MG postsynaptic changes _______ the motor end plate potential, which means that with repetitive stimulation the end plate potential ______.
Definition
reduce the amplitude of

will not meet threshold
Term
Is ACh release impaired in MG?
Definition
No
Term
What happens to geometry of end plate in MG?
Definition
disturbed and normal infolding is reduced and synaptic cleft is enlarged
Term
The autoimmune reaction of MG depends on: _________ components.
Definition
antigen (the immunogenic peptide of the ACh receptor), an antigen- specific T cell receptor, and class II molecule of MHC expressed on the APC.
Term
In MG the ___ cells become reactive against the ACh receptor and recognize the receptor in the _______.
Definition
T

thymus
Term
Two categories of MG: __________.
Definition
Acquired autoimmune older children/adults

A nonimmune heritable congenital form
without ACh receptor antibodies.
Term
Which type of MG is heterogeneous?
Definition
A nonimmune heritable congenital form
without ACh receptor antibodies.
Term
Slow Channel Syndrome is a form of ________ and results from __________.
Definition
A nonimmune heritable congenital form of MG without ACh receptor antibodies.

alteration in ACh receptor capacity to react with ACh
Term
Slow Channel Syndrome is characterized by ________.
Definition
little weakness of cranial muscle and major weakness of limbs (opposite pattern usually seen in myasthenia
Term
Slow Channel Syndrome is characterized by end-plate potentials that are _______, despite normal _______, because the ACh Receptor __________.
Definition
Prolonged

normal AChE

stays opened for prolonged periods
Term
Some patients with lung cancer have a neuro-muscular disorder called ________.
Definition
presynaptic (facilitating) neuromuscular block (Lambert-Eaton Syndrome?)
Term
Lambert-Eaton Syndrome (presynaptic (facilitating) neuromuscular block) physiological response is opposite of myasthenia, showing gradual __________.
Definition
increase to repetitive stimulation so that the final summated action potential is 2-4 times the amplitude of the first potential.
Term
Lambert-Eaton Syndrome is due to Ab against?
Definition
voltage-gated calcium channels in the presynaptic terminals
Term
Symptoms in patients with Lambert-Eaton Syndrome often improve after ________ or _______ therapy.
Definition
plasmapheresis or immunosuppressive
Term
In Lambert-Eaton Syndrome ACh release is?
Definition
impaired
Term
Impaired ______ in congenital form of MG.
Definition
Endocytosis
Term
Botulism and Tetanus toxins affect _________ involved in what process?
Definition
SNARE proteins involved in vesicle fusion (NT release)
Term
Botulism as well as Lambert-Eaton syndrome are treated with ________ & ________ (agents that ________).
Definition
calcium gluconate and guanidine

enhance the release of ACh
Term
Sympathomimetic- ________.
Definition
mimicking action of SNS
(adrenomimetic – action similar to Epi, NE)
Term
Sympatholytic – ________.
Definition
inhibition of adrenergic action
(adrenolytic – blocking action of Epi, NE)
Term
Chronotropic – ____________.
Definition
altering the rate of rhythmic movement (i.e., heartbeats).
Term
Inotropic – ____________.
Definition
altering the force of muscular contraction
Term
Direct agents act ________.
Definition
postjuntionally
Term
Indirect agents act ________.
Definition
prejunctionally
Term
Indirect agents act prejunctionally by influencing the ______ or ______ of NT.
Definition
- release of transmitter
- reuptake of transmitter
Term
Direct response- ________.
Definition
response of target organ to agent
Term
Reflex response- ________.
Definition
an autonomic reaction to peripheral-acting agent
Term
Integrated response- ________.
Definition
Direct + Reflex
Term
Isoproterenol is a _______ agonist/antagonist.
Definition
beta agonist
Term
Alpha receptors sensitivity with respect to NE, E, and Isoproterenol (Iso)?
Definition
E ≥ NE >> Iso
Term
Beta receptors sensitivity with respect to NE, E, and Isoproterenol (Iso)?
Definition
Iso > E ≥ NE
Term
General Pharmacology of Direct-acting Sympathomimetics categories: ________.
Definition
Catecholamines

Non-catecholamines
Term
Catecholamines (Direct-acting Sympathomimetics) Metabolized? Bioavail? half-life?
Definition
Metabolized quickly

Reduced Bioavail

Reduced Half Life
Term
Catecholamines (Direct-acting Sympathomimetics) more or less polar than non-catecholamines ? and therefore oral bioavail? CNS entry?
Definition
More

low oral bioavail

low CNS entry
Term
Catecholamines (Direct-acting Sympathomimetics) more or less selective than non-catecholamines ?
Definition
Less
Term
Non-catecholamines (Direct-acting Sympathomimetics) Metabolized? Bioavail? half-life?
Definition
Resistant to met.
* increased bioavail.
*Longer half life
Term
non-Catecholamines (Direct-acting Sympathomimetics) more or less polar than catecholamines ? and therefore oral bioavail? CNS entry?
Definition
Less polar
*increased oral bioavail.
*Increased in CNS
Term
non-Catecholamines (Direct-acting Sympathomimetics) more or less selective than catecholamines ?
Definition
More selectivity
Term
The Chemistry of specificity of Direct-acting Sympathomimetics depends on: __________.
Definition
1.Substitution on the amino group
2.Substitution of the benzene ring
3.Substitution on the alpha carbon
4.Substitution on the beta carbon
Term
Smooth Muscle in vascular, action of alpha1- ________ receptor.
Definition
contraction
Term
Smooth Muscle in vascular, action of _______ & ________ receptors- relaxation.
Definition
Beta2/Dopamine1
Term
Smooth Muscle in bronchioles, action of _______ receptor- relaxation.
Definition
Beta2
Term
Smooth Muscle in Gut/bladder, action of _______ receptor- sphincters to contract
Definition
Alpha1
Term
Smooth Muscle in Uterine, action of _______ receptor- relaxation (only in late gestation)
Definition
Beta2
Term
Smooth Muscle in Prostate, action of _______ receptor- contraction.
Definition
Alpha1
Term
Smooth Muscle in Eye, action of Alpha1 receptor- contraction of _____ muscle.
Definition
radial muscle
Term
Adrenergic receptors in cardiac muscle: ________
Definition
Alpha 1, beta1/2
Term
Beta 1 receptors in cardiac muscle are ______tropic.
Definition
* Inotropic
* Chronotropic
much lesser extent
Term
Alpha 1 and Beta 2 receptors in cardiac muscle are ______tropic.
Definition
Inotropic
Term
Adrenergic receptors in skeletal muscle: ________
Definition
Beta2
Term
Beta2 receptors in skeletal muscle cause ____ ion uptake.
Definition
K+
Term
Beta2 receptors in skeletal muscle cause ______ with respect to energy stores.
Definition
Glycogenolysis
Term
Ep
Definition
Term
α2
Definition
Term
α2
Definition
test
Term
a1 Agonists Major Responses in: _______ organs.
Definition
Cardiovascular

Eye
Term
a1 Agonists Major Responses in Cardiovascular?
Definition
Direct - vascular contraction
Indirect - slow heart rate
Term
a1 Agonists Major Responses in Eye?
Definition
mydriasis (dilation)
Term
a1 Agonists bc of their _________ Cardiovascular effect, are useful for treating: __________.
Definition
Hypotension

Paroxysmal supraventricular (atrial) tachycardia

Nasal congestion
Term
a1 Agonists are used to treat
Paroxysmal supraventricular (atrial) tachycardia because of the _____ response to __________.
Definition
Reflex response to slow heart (indirect response)
Term
a1 Agonists are used in optical exams to induce _______.
Definition
mydriasis (dilation)
Term
a1 Agonists adverse effects: __________.
Definition
Hypertension

Ischemia to organs

Rebound nasal/sinus hyperemia (desensitization)
Term
Hyperaemia or hyperemia is the increase of blood flow to different tissues in the body.
Definition
WIKI
Term
a1 Agonists are contradicted in patients suffering from: ____________.
Definition
•Hypertension
•Ischemic organ diseases
•Prostate enlargement
Term
a1 Agonists are contradicted with co-administration of: ________.
Definition
–MAO inhibitors
–Indirect-acting sympathomimetics
Term
a2 Agonists major responses: __________.
Definition
vasodilation (a1 constriction)

decrease aqueous humor production (a1 dilation)
Term
a2 Agonists treatments: __________.
Definition
antihypertensive (a1 antihypotensive)

lower intraocular pressure in open angle glaucoma (decrease aqueous humor production)a2 Agonists

minimize withdrawal symptoms
Term
a2 Agonists adverse effects: ________.
Definition
Bradycardia

CNS (>50% population)- Sedation & Dry mouth

Sexual dysfunction
Term
a2 Agonists contradicted in: _______.
Definition
drug hypersensitivity
Term
B1 Agonists major responses: __________.
Definition
-Cardiovascular:
increases calcium influx
increases rate and force
Term
B1 Agonists treatments: __________.
Definition
cardiogenic shock
Term
B1 Agonists adverse effects: ________.
Definition
several CV effects
Term
B1 Agonists contradicted in: _______.
Definition
drug sensitivity
Term
B2 major responses: __________.
Definition
Bronchodilation

Uterine dilation
Term
B2 Agonists treatments: __________.
Definition
Bronchodilators
–Asthma
–COPD

Tocolytic agents (reverse effects of?)
-Late term gestation
Term
B2 Agonists adverse effects: ________.
Definition
Symptoms of b1 stimulation
–Tachycardia
–Widening pulse pressure (systolic pressure rise)

Symptoms of b2 stimulation
–Widening pulse pressure (diastolic pressure drop)
–Drop in serum K+ (skeletal muscle uptake)
–Skeletal muscle tremor
Term
B2 Agonists contradicted in: _______.
Definition
Cardiac disease
–Coronary artery disease
–Arrhythmias

Diabetes

Hyperthyroidism

•Co-administration (same as a1)
–MAO inhibitors
–Indirect-acting sympathomimetics
Term
B2 Agonists adverse effects relatively uncommon when given as _______, more likely when given _________– i.e. ____ dependent)
Definition
inhalant

systemically

dose
Term
Indirect-acting Drug List:

-Interfere with neurotransmitter metabolism- ___________.
Definition
α-methyltyrosine
Term
Indirect-acting Drug List:

-Block transport at nerve terminal- __________.
Definition
cocaine
Term
Indirect-acting Drug List:

Block of vesicular transport- _______.
Definition
reserpine
Term
Indirect-acting Drug List:

Promotion of exocytosis and displacement of transmitter- __________.
Definition
amphetamine
Term
Indirect-acting Drug List:

Prevention of release of transmitter- __________.
Definition
bretylium
Term
Indirect-acting Drug List:

Inhibition to transmitter degradation- __________.
Definition
tranylcypromine: MAO inhibitor
Term
Tyramine is a byproduct of fermentation process that is an intermediate in _____ metabolism
Definition
NE
Term
Tyramine can have indirect/direct _______ effect via stimulation of _______.
Definition
indirect

sympathomimetic

NE release
Term
Patients taking ______ should avoid foods high in tyramine
Definition
MAOIs
Term
Catecholamine & Sympathomimetic Actions: _______ = prototypical agent
Definition
Epinephrine
Term
Catecholamine & Sympathomimetic Actions:
cardiac ________-> HR _____ & Contraction force _________
Definition
excitation

Heart rate and contraction force up
Term
Catecholamine & Sympathomimetic Actions:

Metabolic effects: __________.
Definition
Increase glycogenolysis, adipose -> FFA
Term
Sympathomimetics /Agonists:

Endogenous to Sympathetic NS: ______.
Definition
* Epinephrine
* Norepinephrine
* Dopamine
Term
Sympathomimetics /Agonists:

Exogenous to Sympathetic NS: ______.
Definition
Phenylephrine
Clonidine
Isoproterenol
Dobutamine
Albuterol
Fenoldopam
Bromocriptine
Term
Epinephrine bind what receptors?
Definition
adrenergic

a1 a2 B1 B2
Term
Epinephrine has _____ & _____ effects on cardiac.
Definition
direct + reflex
Term
Epinephrine Non-cardiovascular Effects: ________.
Definition
–Smooth Muscle
–Respiratory
–Metabolic
Term
Epinephrine has a respiratory effect by indirect/direct action on __ receptor causing _______.
Definition
direct B2: bronchodilation
Term
Epinephrine clinical uses: ________.
Definition
Hypersensitivity

Bronchodilator
•Asthma
•Anaphylaxis

Vasoconstriction
•Angioedema
•Adjunct to local anesthetics

Cardiac stimulant

Lower intraocular pressure in wide angle glaucoma (a2)
Term
Epinephrine Adverse Effects: ________.
Definition
–Arrhythmias
–Cerebral hemorrhage
–Anxiety symptoms (somatic)
Term
Epinephrine Adverse Effects: ________.
Definition
nonselective B?
Term
Epinephrine in low doses has vascular effects by causing ________.
Definition
redistribution of blood flow (regional responses)
Term
Epinephrine in low doses has vascular effects by causing redistribution of blood flow: regions rich in ____ see vasoconstriction & regions rich in ____ see vasodilation
Definition
a1

B2
Term
Epinephrine in low doses has no vascular effects on __________.
Definition
TPR
Term
Epinephrine in low doses has results in a ______ cardiac response.
Definition
direct responses
Term
Epinephrine Low Doses- Blood pressure: Increase _______, decrease ________.
Definition
systolic

diastolic
Term
Epinephrine in high doses has vascular, cardiac, and blood pressure effects like __________.
Definition
NE
Term
Epinephrine in high doses effects vasculature predominately ______ globally and _____ locally resulting in an net effect __________.
Definition
a1 global

b2 local

net effect increase TPR
Term
In high doses Epinephrine has ___ like cardiac effects, giving _____ responses.
Definition
NE Like

direct effects + reflex responses
Term
In high doses Epinephrine has ___ like BP effects, resulting in ______.
Definition
NE like

pulse pressure narrowing
Term
Norepinephrine acts on what receptors?
Definition
adrenergic

a1 a2 B1 (NOT B2 like E)
Term
Norepinephrine effects Vascular directly through ____ receptor causing ___________.
Definition
a1 vasoconstriction
Term
Norepinephrine effects Cardiac ________.
Definition
Directly and Reflex
Term
Norepinephrine effects Cardiac directly through ____ receptors and causes ____.
Definition
B1 [increase in force & HR]
Term
Norepinephrine effects BP by _____ the TPR and ______ the CO.
Definition
Increasing TPR and CO
Term
Norepinephrine non cardiovascular effects?
Definition
Minor
Term
Norepinephrine clinical use?
Definition
Limited: Vasoconstriction
Term
Norepinephrine Adverse Effects: __________.
Definition
–Arrhythmias
–Cerebral hemorrhage

(Both same as E, except E also has skeletal somatic tremors)
Term
Dopamine mainly has effects on?
Definition
Cardiovascular (like NE minimal non cardiovascular)
Term
Dopamine can be used to treat _______ and ________.
Definition
•Shock
•Cardiac failure
Term
Dopamine can be used to treat shock by __________.
Definition
Increase renal blood flow
Term
Dopamine can be used to treat Cardiac failure by __________.
Definition
acting as cardiac stimulant
&
Increase renal blood flow
Term
Dopamine admin?
Definition
Must be given IV
Term
Because of having to give via IV, Dopamine is useful for _____, but not ______.
Definition
Acute cardiac failure, not chronic
Term
Dopamine adverse effect?
Definition
Arrhythmias (just like NE and E)
Term
Oxymethazoline: is a ______ agonist/antagonist?
Definition
a-adrenergic agonist (a1 and a2)
Term
Oxymethazoline MOA: ______.
Definition
a1 & a2 adrenergic agonist
Term
Oxymethazoline clinical use?
Definition
decongestant (a1 main use)
Term
Skip
Definition
skip
Term
skip
Definition
skip
Term
Oxymethazoline adverse effect?
Definition
continued use causes rebound congestion
Term
Oxymethazoline adverse effect of continued use causing rebound congestion is a result of?
Definition
down regulation of a2 receptors
Term
Oxymethazoline is contradicted in those who?
Definition
drug sensitivity
Term
Phenylephrine: is a ______ agonist/antagonist?
Definition
a1 agonist
Term
Phenylephrine clinical use?
Definition
Ophthalmological – to produce: - mydriasis (a1 effect)
Term
Phenylephrine MOA: ________.
Definition
a1 agonist
Term
Phenylephrine adverse effect?
Definition
Rebound nasal/sinus hyperemia (a1 side effect)
Term
Phenylephrine is contradicted in those who?
Definition
drug sensitivity
Term
Clonidine MOA: _______.
Definition
a2 agonist
Term
Clonidine used to treat?
Definition
mild-to-moderate hypertension (a2 vasodilation)
Term
Clonidine Adverse effects: _______.
Definition
- drowsiness
- dry mouth
- GI disturbance
- muscle weakness
- withdrawal symp.
Term
Clonidine contraindications: _______.
Definition
drug sensitivity
Term
Isoproterenol MOA: _______.
Definition
b1 + b2 agonist
Term
Isoproterenol Vascular Effects: _______.
Definition
direct B2: vasodilation
Term
Isoproterenol Cardiac Effects: _______.
Definition
direct b1: force, rate + reflex
Term
Isoproterenol Blood Pressure Effects: _______.
Definition
widening pulse pressure (B2)
Term
Isoproterenol Non-cardiovascular Effects: _______.
Definition
Smooth muscle
-Bronchial
-GI/Bladder
-Uterine

Metabolic
Term
Isoproterenol Bronchial effect: _______
Definition
direct b2: bronchodilation
Term
Isoproterenol Uterine effect- __________.
Definition
(direct b2: dilation in late gestation)
Term
Dobutamine MOA: __________.
Definition
b1 Agonist
Term
Dobutamine used as a ______?
Definition
Cardiac stimulant (b1)
Term
Dobutamine treats?
Definition
Cardiogenic shock & Cardiac failure

(used as a Cardiac stimulant same as Dopamine and E)
Term
Dobutamine administered?
Definition
IV (just like Dopamine)

–Limits its usefulness in chronic cardiac failure.
–Can be advantage in acute cardiac failure. (just like dopamine)
Term
Dobutamine Adverse Effects: ________.
Definition
Arrhythmias (just like dopamine)

Tolerance develops with use
Term
Albuterol use?
Definition
bronchodilator (B2)
Term
Albuterol treats?
Definition
- asthma & COPD (Bronchodilator B2)
Term
Albuterol MOA: _______.
Definition
B2 agonist
Term
Albuterol Adverse Effects: _______.
Definition
angina
muscle cramps
Term
Albuterol contradictions:________.
Definition
- drug sensitivity
- tachyarrhythmias
- pregnancy
Term
tachyarrhythmias WIKI
Definition
any disturbance of the heart rhythm in which the heart rate is abnormally increased.
Term
Fenoldopam MOA: ________.
Definition
D1 Agonist
Term
Fenoldopam is the ________.
Definition
Prototype – D1 Agonist
Term
Fenoldopam causes and is used to treat?
Definition
Vasodilation

Severe hypertension
Term
______ is used to treat Mild-Moderate Hypertension as an a2 agonist.
Definition
Clonidine
Term
Fenoldopam Adverse effects?
Definition
–Hypotension
–Tachycardia
Term
Fenoldopam limitation?
Definition
Short t1/2 & not absorbed by gut (i.v. only)
Term
Bromocriptine MOA: __________.
Definition
D2 Agonist
Term
Bromocriptine Clinical use?
Definition
– hyperprolactinemia
- Parkinson’s
Term
Bromocriptine acts to suppress _______, causing ________ in order to improve ________.
Definition
suppress prolactin release from adenomas and shrink tumor, improve motor function
Term
aB agonist?
Definition
epinephrine
Term
a1 agonist?
Definition
phenylephrine
Term
a2 agonist?
Definition
clonidine
Term
B1/2 agonist?
Definition
isoproterenol
Term
B1 agonist?
Definition
dobutamine
Term
B2 agonist?
Definition
albuterol
Term
D1 agonist?
Definition
fenoldopam
Term
D2 agonist?
Definition
Bromocriptine
Term
Nonselective a Antagonists: ________.
Definition
Phenoxybenzamine & phentolamine & Ergot alkaloids
Term
Phenoxybenzamine is used to treat?
Definition
(Nonselective a Antagonist)
Pheochromocytoma

Benign prostatic obstruction
Term
Ergot alkaloids used to treat?
Definition
(Nonselective a Antagonist)

Migranes
Term
Nonselective a Antagonists (Phenoxybenzamine & phentolamine) adverse effects?
Definition
–Cardiovascular
•Tachycardia (reflex)
•Orthostatic hypotension
•Nasal congestion (a1)

–Non cardiovascular
•GI (Phentolamine)
•Impotence (Phenoxybenzamine)
•Potential mutagen
(Phenoxybenzamine)
Term
•Orthostatic hypotension WIKI
Definition
form of hypotension in which a person's blood pressure suddenly falls when standing up or stretching.
Term
Pheochromocytoma is a ______ tumor of the ___________.
Definition
neuroendocrine tumor of the medulla of the adrenal glands
Term
Pheochromocytoma is a neuroendocrine tumor of the medulla of the adrenal glands that secretes: __________.
Definition
catecholamines; Epi, NE
Term
Pheochromocytoma is treated with?
Definition
prazocin (a1 inhibitor over Phenoxybenzamine a non-selective a inhibitor because of side effects)
Term
Pheochromocytoma ______% with genetic contribution.
Definition
25%
Term
Non-selective a blockers have an _____junctional effect on ________ receptors.
Definition
prejunctional

a2
Term
The a2 component of Non-selective a blockers causes a ______ blockade leading to a __________.
Definition
prejunctional blockade -> reflex tachycardia
Term
Because of the tachycardia side effect of the a2 component, Non-selective a blockers are avoided in treating?
Definition
Hypertension
Term
The a2 antagonistic component of Non-selective a blockers, blocks _____ release.
Definition
NE
Term
Nonselective Adrenergic Antagonists of B and a1: ___________.
Definition
Labetalol

Carvedilol
Term
Carvedilol is a _____ antagonist and is used as a anti-______ agent and improves the survival
Definition
B and a1

–Anti-ischemic agent
–Improves survival in chronic heart failure
Term
Selective a1 Antagonists have an advantage over non-selective a antagonists, because ________.
Definition
lack a2 component
•less prejunctional blockade -> less reflex tachycardia
Term
Selective a1 Antagonists are used to clinically treat: ________.
Definition
Benign prostatic hyperplasia
Hypertension
Congestive heart failure
Pheochromocytoma (same as nonselective)
Term
Pheochromocytoma is treated by which Selective a1 Antagonist?
Definition
prazocin
Term
Benign prostatic hyperplasia is treated by which Selective a1 Antagonists?
Definition
•Prazosin (BID dosage)
•Doxazosin & Terazosin (QD dosage)
Term
Selective a1 Antagonists Adverse Effects: _______.
Definition
Orthostatic hypotension (just like nonselective) (from a1 obviously)

Nasal congestion (just like nonselective) (from a1)
Term
Selective a1 Antagonists side effect of Orthostatic hypotension usually becomes _______ and requires first does to be __________.
Definition
•Usually becomes tolerated
•Give first dose at night
Term
“Uroselective” a1A Antagonist: ________.
Definition
Tamsulosin (aka flomax)

alfuzosin
Term
Tamsulosin & alfuzosin is used to treat?
Definition
Benign Prostatic Hyperplasia (BPH) (“Uroselective” a1A Antagonist)
Term
“Uroselective” a1A Antagonist adverse effect? and which one is to a lesser extent?
Definition
Retrograde ejaculation (less with alfuzosin)
Term
“Uroselective” a1A Antagonist avoids _____ adverse effect in most.
Definition
orthostatic hypotension (a Selective a1 Antagonist side effect)
Term
B antagonists are used cardiovascularly to treat?
Definition
–Hypertension
–Angina
–Arrhythmias
–Myocardial infarction
–Heart failure
–CV Symptoms of
•Hyperthyroidism
•Pheochromocytoma
•Aortic aneurysm
–Migraine headache
Term
B antagonists are used to treat non-cardiovascularlly?
Definition
–Glaucoma
–Somatic symptoms of anxiety (e.g. stage fright)
–Fine muscle tremors
Term
Prototypic B Antagonist?
Definition
Propranolol
Term
Propranolol is a _____ B Antagonist, meaning it has no __________ activity and therefore not a ______ agonist.
Definition
Pure antagonist, no Intrinsic Sympathomimetic Activity (ISA) (i.e. not a partial agonist)
Term
Propranolol selective or non-selective for _____ receptors.
Definition
non-selective for B receptors
Term
Propranolol has high ____ and therefore enters __________.
Definition
High lipid solubility - Enters gut & CNS
Term
Propranolol has _____ first pass metabolism, causing ________
Definition
high

low bioavailability
Term
Propranolol exhibits ______ activity, giving it ______ effects.
Definition
Has membrane-stabilizing activity

Quinidine-like effects,
Term
Propranolol exhibits membrane-stabilizing activity giving it Quinidine-like effects, meaning it causes _______ and acts as a ________ and therefore should be avoided in the treatment of _______.
Definition
Na+ channel blockade, (local anesthetic)
•Avoid for topical administration to eye (glaucoma Tx)
Term
Nonselective B antagonists and their significance: __________.
Definition
–Propranolol
–Nadolol: long half-life
–Timolol: low local anesthetic action - use in glaucoma (can't with Propranolol)
–Pindolol: ISA (Propranolol has none, pure)
Term
Selective B1 antagonists and their significance: __________.
Definition
–Atenolol: low lipid sol.
–Betaxolol: opthal.
–Esmolol: short half-life
–Metoprolol
Term
B Antagonists have adverse effects on the cardivascular system of: _______.
Definition
•Induce CHF or bradycardial arrhythmia
•Sudden withdrawal - in anginal patients may cause sudden death
Term
The sudden withdrawal of B Antagonists from angina pts. is due to ________.
Definition
receptor supersensitivity
Term
B Antagonists have adverse effect of increasing _______ levels.
Definition
cholersterol
Term
B Antagonists non-cardio adverse effects: ________.
Definition
–Bronchiospasm
–CNS - sleep disturbance, depression
–(Mask symptoms & recognition of hypoglycemia)
Term
B Antagonists are the first choice in treating __________ if the patient is _______ stable.
Definition
hypertensive (1st choice if stable angina present)
Term
B Antagonists being used to treat hypertension in older patients is often used with ______ as the 1st choice.
Definition
Diuretics
Term
B Antagonists cardiovascular treatments: ________.
Definition
Hypertension
angina
heart failure – both acute (MI) & chronic
Term
B Antagonists treat heart failure (both acute (MI) & chronic) by ___________.
Definition
Decrease heart work & protect against arrythmias
Term
B Antagonists are contradicted in pts with: ________.
Definition
Asthma

Diabetes until recently many felt caution needed - still caution in persons with frequent hypoglycemia
Term
B Antagonists are contradicted in Asthma pts. because ____________.
Definition
bronchoconstriction (adverse effect of bronchospasm)
Term
B Antagonists are contradicted in pts. with Diabetes because ________.
Definition
•(mask symptoms of insulin-induced hypoglycemia & glycogenolysis inhibited)
•(augment insulin-induced hypoglycemia)
Term
B Antagonists effect on cholesterol levels?
Definition
Raise VLDL and lower HDL
Term
B Antagonists are less effective in treating ______ in _____ race.
Definition
Hypertension

Blacks
Term
Phenoxybenzamine MOA: ________.
Definition
a antagonist
Term
Phenoxybenzamine used to treat: __________.
Definition
- symptomatic management of pheochromacytoma

- treatment of hypertensive
crisis caused by sympathomimetic amines

- micturition problems
Term
Phenoxybenzamine is a irreversible/reversible a antagonist.
Definition
irreversible
Term
Phenoxybenzamine overall results in a decrease/increase in ________ by ________.
Definition
decrease vasocon. by Epi & NE
Term
Phenoxybenzamine Adverse effects: ________.
Definition
- decrease blood pressure
- postural hypotens.
- reflex CV stim.
- pupil constriction
- partial agon/antag. (not pure) at 5HT2A
Term
Phenoxybenzamine contradicted in _______.
Definition
drug sensitivity pts.
Term
Prazocin MOA: __________.
Definition
a1 antagonist
Term
Prazocin clinical use: ___________.
Definition
- hypertension
- PTSD
- benign prostatic hyperplasia
- scorpion stings
Term
Prazocin causes _____ muscle to relax/contract resulting in a ________.
Definition
smooth muscle to relax

drop in BP
Term
In addition to being a a1 antagonist, Prazocin, inhibits ________.
Definition
PDE (phosphodiesterase) breaks down cAMP
Term
Prazocin Adverse effects: __________.
Definition
- postural hypotens. (same as Phenoxybenzamine, non selective a antag)
- syncope
Term
Yohimbine MOA: ________.
Definition
a2 antagonist
Term
Yohimbine Clinical Uses: ________.
Definition
- sexual dysfunction*
- diabetic neuropathy
- postural hypotension (side effect of a1 antagonist and non-selective a)
Term
Yohimbine decreases/increases _______ outflow.
Definition
increases SNS outflow
Term
Yohimbine overall effect?
Definition
(α2 antagonist)

increases HR and BP (Prazocin: α1 antagonist lowers BP)
Term
Yohimbine Adverse Effets: _______.
Definition
-Increase motor activity
- tremors
- also antagonist of
most 5HT receptors (same w/ Phenoxybenzamine a nonselective a antagonist)
- anxiety
- insomnia
Term
Propranolol MOA: ________.
Definition
B antagonist (prototypical one)
Term
Propranolol clinical uses: ________.
Definition
- hypertension
- angina
- arrhythmias / tachycardia
- pheochromocytoma
- prophylaxis of migrane
- tremor, Parkinson, alcohol WD*
Term
Propranolol selective or non-selective B antagonist?
Definition
Non
Term
Propranolol relaxes/constricts _____ muscle.
Definition
constricts bronchial smooth muscle
Term
Propranolol Adverse effects: ________.
Definition
- CV: angina (don't treat HT unless angina stable)
Term
Propranolol Contradictions: _______.
Definition
- congestive heart failure
- COPD (broncho constrictor)
Term
Timolol MOA: ___________.
Definition
B antagonist
Term
Timolol Clinical uses: ___________.
Definition
open-angle glaucoma

Ischemic Heart disease
Term
Timolol can be used to treat open-angle glaucoma, unlike ______, bc of its quidine like effect.
Definition
Propranolol
Term
Timolol is better tolerated than _______ for treating open-angle glaucoma.
Definition
Pilocarpine (a parasympathetic akaloid)
Term
Timolol adverse effects: ________.
Definition
- cardiac arrhythmias
- bradycardia (used to treat tacha)
- blurred vision
- bronchospasms
Term
Timolol Contraindications: __________.
Definition
bronchial asthma,COPD (bronchoconstrictor)
heart failure
Term
Carvedilol MOA: ________.
Definition
a1,B antagonist
Term
Carvedilol clinical use: ________.
Definition
- Heart failure progression:
reduce sudden death
rate
- Post MI: reduce death rate
-Hypertension
Term
Carvedilol treats hypertension by reducing: ___________.
Definition
reduce bp & heart rate, plasma renin activity & renal vascular resistence
Term
Carvedilol MOA: α1,b antagonist (a ______ mixture)
Definition
racemic
Term
Carvedilol adverse effects: __________.
Definition
bradycardia & hypotension (reduces BP and HR)

-CNS: dizziness, abnormal vision

-GI disturbance: diarrhea, nausea, vomiting
Term
Carvedilol Contraindications: ________.
Definition
-bronchial asthma (B2 antagonist),
AV block (B1), severe bradycardia (B1), severe renal impairment (decreases renin and renal vascular resistance)
Term
Atenolol MOA: __________.
Definition
B1 antagonist
Term
Atenolol clinical uses: ___________.
Definition
hypertension
- elderly patients with
isolated systolic HT
- angina
- post MI treatment (Carvedilol B antagonist also)
Term
Atenolol
Definition
Term
Atenolol MOA: ________.
Definition
B1 antagonist
Term
Atenolol can be used to treat ______ in the elderly when combined with ________.
Definition
isolated systolic HT

diuretic
Term
Atenolol Adverse effects: ________.
Definition
- CV: bradycardia (B1)

-impotence (Phenoxybenzamine gets a1 in penis) don't know why these B1 does though?
Term
Atenolol Contraindications: ________.
Definition
- bradycardia (adverse effect)
- pregnancy
Term
Esmolol MOA: ________.
Definition
B1 antagonist
Term
Esmolol clinical use: ________.
Definition
supraventricular tachycardia (e.g., atrial fibrillation & atrial flutter)

reduce systolic pressure (Atenolol B1 antagonist also)
Term
Esmolol length of action?
Definition
Very short
Term
Esmolol Adverse effects: __________.
Definition
-CV: cardiac arrest,hypotension peripheral ischemia
CNS: dizziness,headache, convulsion, anxiety, depression, confusional state, agitation
Term
Esmolol Contraindications: ________.
Definition
- bradycardia
- cardiogenic shock
- pulmonary hypotension
Term
Metoprolol MOA: __________.
Definition
B1 antagonist
Term
Metoprolol clinical use: ________.
Definition
-Hypertension
- Angina
- Heart failure
Term
Metoprolol is more effective at treating HT when?
Definition
comb. w/ diuretic (same with Atenolol)
Term
Metoprolol Adverse effects: __________.
Definition
- CV: slow heart rate, symptoms of heart
failure
- CNS: dizziness, drowsiness, tiredness, shortness of breath, mood swings, depression (same with Esmolol)
Term
Metoprolol Contraindications: ________.
Definition
- severe bradycardia,
cardiogenic shock,
Term
Betaxolol MOA: __________.
Definition
B1 antagonist
Term
Betaxolol clinical use: ________.
Definition
chronic open angle glaucoma1

hypertension2
Term
Betaxolol Adverse effects: __________.
Definition
- ocular discomfort1
- bradycardia2
- depression2
- bronchospasm2
Term
Betaxolol Contraindications: ________.
Definition
pregnancy
Term
Butoxamine MOA: ________.
Definition
B2 antagonist
Term
Clozapine MOA: ______.
Definition
D2 antagonist
Term
Clozapine Clinical Uses: __________.
Definition
refractory schizophrenia
Term
Clozapine has weak action on __________.
Definition
all other DA receptors (α adrenergic, cholinergic, H1 and 5HT as well).
Term
Clozapine Adverse effects: __________.
Definition
- CV: tachy., angin.
- CNS; drowsy, dizzy
Term
Clozapine Contraindications: ________.
Definition
- epilepsy
- CNS depression
- myeloprolif. disor.
Term
BHP treated with ________ or __________ (____________).
Definition
•5-a-reductase inhibitors (Finasteride)
•a1 adrenergic antagonists:
Prazocin and Tamsulosin
Term
Acetylcholine (ACh) acts where?
Definition
postganglionic parasympathetic fibers

Autonomic ganglia

Adrenal medulla

Motor endplate

Sweat glands (Sympathetic postganglionic nerve terminals ACh)
Term
Two basic types of ACh release: _______.
Definition
Spontaneous

Evoked
Term
Spontaneous ACh release is ____+ independent/dependent & Evoked ACh release is ____+ independent/dependent.
Definition
Spontaneous- Ca2+- independent

Evoked- Ca2+- dependent
Term
Evoked ACh release occurs where?
Definition
from synaptic vesicles by exocytosis
Term
Receptor types responding to ACh: __________.
Definition
Muscarinic

Nicotinic
Term
ACh breakdown mediated by ___________.
Definition
acetylcholinesterase (AChE)
Term
Muscarinic Receptor Mediated Responses ______ acting & ______ lasting.
Definition
Slow, long
Term
_______ - classical competitive antagonist for Muscarinic Receptor.
Definition
Atropine
Term
Muscarinic Receptors located: ________.
Definition
smooth muscle, glands, & the heart
Term
Atropine- a competitive blocker at ______ muscarinic receptors
Definition
all
Term
________ - a competitive antagonist at M1 receptors
Definition
Pirenzepine
Term
Pirenzepine acts at M_ receptors in _______ & ________.
Definition
1

myenteric plexus (gut muscles) and in cerebral cortex
Term
Known Muscarinic receptor agonists don't/do discriminate between the muscarinic receptor subtypes.
Definition
don't
Term
Nicotinic Receptor Mediated Responses ______ acting & ______ lasting.
Definition
Quick, short lived
Term
Nicotinic Receptor Mediated Responses inhibitory/excitatory?
Definition
ALWAYS excitatory
Term
Muscarinic Receptor Mediated Responses inhibitory/excitatory?
Definition
inhibitory & excitatory
Term
Nicotinic Receptor located: _______.
Definition
autonomic ganglia, adrenal medulla, motor endplate region
Term
Nicotinic receptors on ______ & ______ are similar but differ from those at ___________.
Definition
drenal medulla & ganglia

motor-endplate region
Term
Nicotinic receptors on ganglia- stimulated by _____________.
Definition
dimethyl 4-phenyl piperazinium (DMPP)
Term
Classical nicotinic receptor antagonist at ganglia: ________, which acts non-competitively/competitively
Definition
hexamethonium (C-6)

competitively
Term
Classical nicotinic receptor antagonist at motor endplate region: _______, which acts non-competitively/competitively
Definition
d-tubocurarine

competitively
Term
Is ACh used therapeutically? Not useful because of its ________.
Definition
short duration
Term
Muscarinic Receptor Agonists: _____________.
Definition
ACh

Methacholine+
Carbachol+
Bethanechol+
Pilocarpine
Cevimeline
Term
Which Muscarinic Receptor Agonist is broken down by AChE?
Definition
Methacholine+
Term
Methacholine+ is antagonist/agonist at?
Definition
mainly agonist muscarinic
Term
Methacholine+ use?
Definition
diagnose bronchial hyperactivity & asthmatic

diagnosis of achalasia
Term
Methacholine+ used to diagnosis achalasia when it causes?
Definition
induced swallowing
Term
Carbachol+ shorter/longer duration than Methacholine+ and why?
Definition
Longer, not hydrolyzed by AChE
Term
Methacholine+ is antagonist/agonist at?
Definition
agonist at both muscarinic and nicotinic
Term
Carbachol+ is clinical use?
Definition
topically in the eye for wide angle (open-angle) glaucoma
Term
______ is the best among the three synthetic Muscarinic Receptor Agonists.
Definition
Bethanechol+

(Bethanechol+, Methacholine+ Carbachol+)
Term
Bethanechol+ is antagonist/agonist at?
Definition
pure agonist muscarinic
Term
Bethanechol+ Stimulates __________.
Definition
smooth muscle of bladder and G.I. tract preferentially over heart
Term
Bethanechol+ clinical use?
Definition
treat postoperative distension, gastric atony, urinary retention, reflux esophagitis
Term
Bethanechol+ adverse effects?
Definition
gastric distress & bronchiole constriction
Term
_______ is a naturally occurring muscarinic agonist which is not charged.
Definition
Pilocarpine
Term
Pilocarpine is the ______ drug of choice for treating _____________.
Definition
***Cholinergic drug of choice for treatment of wide angle glaucoma (Carbachol+ can also be used)
Term
Pilocarpine in combination with ________ is used to treat ________ preoperatively.
Definition
physostigmine (reversible cholinesterase inhibitor)

narrow angle glaucoma until
surgery
Term
Pilocarpine is also used to treat _______ that follows _________ treatments.
Definition
xerostomia

head & neck radiation treatments
Term
Xerostomia is an autoimmune disease that ________.
Definition
decreases salivary secretions
Term
Pilocarpine side effects?
Definition
irritability & restlessness
Term
_______ is a relatively new drug used
to treat dry mouth associated with Sjogren's syndrome.
Definition
Cevimeline
Term
Cevimeline is antagonist/agonist at?
Definition
Muscarinic agnoist
Term
Side Effects of Muscarinic Stimulants (agonists)?
Definition
Urinary frequency, diarrhea, bronchiole constriction, salivation, nausea, vomiting, bradycardia, increased HCl secretion
Term
Use of cholinergic stimulants contraindicated in: __________.
Definition
asthma, hyperthyroidism, & peptic ulcer
Term
Anti-Muscarinic Drugs Two major ones: _______.
Definition
Atropine

Scopolamine
Term
Atropine & Scopolamine: ________.

Antagonist/Agonist of ______
Acting?
Side effect?
Competitive/uncompetitive?
Definition
Anti-Muscarinic
Atropine- long acting & tends to cause anxiety- competitive antagonist

Scopolamine- shorter acting and tends to cause sedation-competitive antagonist
Term
Atropine clinical use?
Definition
Retinal examination
Term
Atropine is used for Retinal examination, because it causes?
Definition
mydriasis & loss of accommodation
Term
Atropine is an antidote for?
Definition
organophosphate intoxication
Term
Atropine is used as an adjunct with ________ in the treatment of _________.
Definition
AChE inhbitors

myasthenia gravis
Term
Atropine is used as an adjunct for myasthenia gravis to reduce _______ receptor side effects due to AChE
inhibition at ______ & _______ organs.
Definition
muscarinic

GI tract & bladder
Term
Scopolamine is used to treat?
Definition
motion sickness

bedwetting (enuresis)
Term
Scopolamine gives fewer side effects when administered ______ as ________.
Definition
topically (rather than orally) Transderm Scop®
Term
Scopolamine drug type?
Definition
Anti-Muscarinic
Term
Scopolamine is used to treat bedwetting (enuresis), because it blocks ________ receptors & increases ________.
Definition
muscarinic

bladder capacity
Term
______ is used in retinal examination in adults, because it is shorter acting than atropine.
Definition
Homatropine (Anti-Muscarinic )
Term
______ is used in retinal examination in adults, because it is shorter acting than atropine & Homatropine.
Definition
Tropicamide (Anti-Muscarinic )
Term
Glycopyrrolate+ drug type?
Definition
(Anti-Muscarinic )
Term
Glycopyrrolate+ reduces _______ and is therefore useful in treating ___________.
Definition
stomach acid production-used for treating peptic ulcer
Term
Glycopyrrolate+ can be used as a ______ medication surgery to ___________.
Definition
preanesthetic medication during surgery to dry up mouth, throat & stomach
Term
Glycopyrrolate+ can be injected during surgery to reverse ______-induced _______.
Definition
vagal-stimulated bradycardia
Term
Glycopyrrolate+ can be used to treat ________ in addition to peptic ulcer disease.
Definition
hyperhydrosis
Term
Glycopyrrolate+ drug type?
Definition
(Anti-Muscarinic )
Term
Unlike the other Anti-Muscarinics, Glycopyrrolate+ has less __________.
Definition
CNS side effects (unlike atropine, scopolamine)
Term
________ & ____________ can be used to treat irritable bowel syndrome.
Definition
Methantheline+ & Propantheline+
Term
Methantheline+ & Propantheline+ drug type?
Definition
(Anti-Muscarinic )
Term
Methantheline+ & Propantheline+ do what?
Definition
Block ganglionic transmission and*** antagonize ACh at muscarinic receptors
Term
Anti Muscarinic Drugs very dangerous in patients with ________.
Definition
narrow angle glaucoma
Term
______, _______, & ________ have enough antimuscarinic receptor activity to cause atropine- like toxicity
Definition
antihistamines, phenothiazines, & tricyclic antidepressants
Term
Anti Muscarinic Drugs Contraindicated in: _____________.
Definition
narrow angle glaucoma

prostatic hypertrophy, achalasia, intestinal atony
Term
______ Indicative of atropine toxicity & especially dangerous in young children
Definition
Atropine flush
Term
With Atropine flush, ________ must be done to save life.
Definition
Body temp must be reduced (e.g., ice bath
Term
Classical ganglionic blocker:_________ - competitive antagonist
Definition
hexamethonium (C-6)
Term
All clinically useful ganglionic blockers
act at ______ receptors
Definition
nicotinic
Term
Primary Pathway of Ganglionic Transmission mediated by __________.
Definition
nicotinic receptors
Term
Primary Pathway of Ganglionic Transmission fast or slow?
Definition
fast excitatory potential
Term
Secondary Pathway of Ganglionic Transmission fast or slow?
Definition
Slow excitatory/inhibitory potential
Term
Slow excitatory potential of Secondary Pathway of Ganglionic Transmission is produced by action of _______ onto _______ receptors.
Definition
ACh on M1 receptor
Term
Slow inhibitory potential of Secondary Pathway of Ganglionic Transmission is produced by action of _______ onto _______ receptors.
Definition
ACh on M2 receptor
Term
Slow inhibitory potential produced by release of ACh from preganglionic nerve terminal, activation of M2 receptor on – SIF cell, and release of _______ or ________ which hyperpolarize ganglia
Definition
norepinephrine or dopamine
Term
SIF cell WIKI
Definition
nterneurons of the sympathetic ganglia (postganglionic neurons
Term
_______ blocks dopamine action at ganglia.
Definition
Metoclopramide
Term
Metoclopramide blocks dopamine action at ganglia, which would typically __________.
Definition
inhibit the ganglion
Term
Metoclopramide blocks dopamine action at ganglia, which leads to increase ________, without _________.
Definition
G.I. tract motility without stimulating HCl secretion
Term
Ganglionic Stimulants are not used?
Definition
therapeutically
Term
Ganglionic Stimulants example?
Definition
Nicotine in low doses
Term
Nicotine is considered a nonselective/selective _________ receptor antagonist/agonist.
Definition
nonselective nicotinic Receptor agonist (ganglionic stimulant)
Term
Nicotine activates nicotinic Rc’s on _________.
Definition
autonomic ganglia
Term
Nicotine activates nicotinic Rc’s on
autonomic ganglia, stimulating
transmission through __________.
Definition
both parasympath & sympath ganglia
Term
Overall Cardiovascular effect of nicotine?
Definition
elevate blood pressure
Term
Cardiovascular: Nicotine increases ________ and ________ by stimulating the ganglia of ______ and ______.
Definition
TPR & Ventricular Contractions

Venous Return and Heart
Term
Overall Respiratory effect of nicotine?
Definition
increase respiration
Term
nicotine increases respiration by?
Definition
activate chemoreceptors in aortic arch & carotid body
Term
In GI tracct ________ has dominant tone in GI tract.
Definition
Parasympathetic
Term
Overall GI effect of nicotine?
Definition
increase G.I. tract motility & HCl release (Para is dom tone of GI)
Term
Overall CNS effect of nicotine?
Definition
emesis by acting at chemoreceptor trigger zone

Increases ADH release
Term
The Increases ADH release from Nicotine causes?
Definition
fluid retention
Term
At high toxic doses, Nicotine becomes?
Definition
ganglionic blocker at high doses
Term
Nicotine can enter the _____ easily?
Definition
Placenta (skin also)
Term
Toxic Nicotine kills by __________.
Definition
Resp Arrest
Term
Nicotine in high doses _____ nicotinic receptors at medulla oblongata causing ___________.
Definition
desensitizes

to stop breathing
Term
Nicotine in high doses _____ nicotinic receptors at motor endplate causing ___________.
Definition
desensitizes

paralysis of diaphragm & intercostal muscles
Term
__________ stimulates ganglionic transmission without causing receptor desensitization- only used as laboratory tool
Definition
DMPP (dimethyl 4-phenyl piperazinium ion)
Term
DMPP (dimethyl 4-phenyl piperazinium ion is specific for _____ receptors on _______ and _______ (doesn't affect _______).
Definition
nicotinic

ganglia & adrenal medulla, not NMJ
Term
DMPP (dimethyl 4-phenyl piperazinium ion) Cardiovascular effects?
Definition
same as nicotine
Term
Ganglionic Blockers are Only used chronically to control ________ in patients with __________.
Definition
blood pressure

acute dissecting aortic aneurysm
Term
Ganglionic Blockers can be used to produce ______ during surgery to minimize ____________.
Definition
hypotension

minimize hemorrhage at operative site
Term
Ganglionic stimulants: ________.
Definition
DMPP and Nicotine
Term
Ganglionic Blockers: ____________.
Definition
Tetraethylammonium+ (TEA)

Hexamethonium+ (C-6)

Trimethaphan+

Mecamylamine
Term
Ganglionic Blockers:

Tetraethylammonium (TEA): ______ charged and & ______ acting.
Definition
1. Positively charged, so does not cross BBB
2. Short duration of action
Term
Ganglionic Blockers:

Hexamethonium (C-6): ______ charged and & ______ acting & ______ absorbed.
Definition
1. Positively charged, so does not cross BBB
2. Long duration of action
3. Not well absorbed
Term
______ is only uncharged Ganglionic Blocker that can cause CNS effects.
Definition
Mecamylamine
Term
Side Effects of Ganglionic Blockers.
Definition
interfere with body's ability to maintain
homeostasis:
1. Abolish autonomic reflexes such as
miosis & accommodation of eyes
2. Reduces transmission through division
of ANS which is dominant to produce
physiological responses (e.g., will
generally increase heart rate by blocking
dominant parasympathetic tone at SA
node)
Also, gastrointestinal tract motility is inhibited,
causing constipation.
- orthostatic hypotension (due to block in
sympathetic tone to veins),
- urinary retention (due to block in
parasympathetic tone) &
- impotence due to block in both
parasympathetic & sympathetic control of
erection & ejaculation
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