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
|
|
Term
Competitive blockers-non-depolarizing neuromuscular blockers prototype __________. |
|
Definition
|
|
Term
Depolarizing neuromuscular blockers are antagonists/agonists? |
|
Definition
|
|
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
|
|
Term
Depolarizing neuromuscular blockers elevate _____ plasma levels. |
|
Definition
|
|
Term
Depolarizing neuromuscular blockers prototype _________. |
|
Definition
|
|
Term
_________ neuromuscular blocker has cardiovascular effects. |
|
Definition
|
|
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
|
|
Term
_______- almost no histamine release- can cause tachycardia (in rare cases). |
|
Definition
|
|
Term
_________ - a non-depolarizing blocker similar to vecuronium. |
|
Definition
|
|
Term
Succinylcholine releases _______ & tends to slow ________. |
|
Definition
vasodilator histamine
heart rate |
|
|
Term
Succinylcholine reduces effectiveness of _______. |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
Term
d-tubocurarine is rarely used bc _______. |
|
Definition
cardiovascular difficulties |
|
|
Term
d-tubocurarine administered _________. |
|
Definition
|
|
Term
d-tubocurarine is only used as a _______ during general anesthesia |
|
Definition
|
|
Term
d-tubocurarine Duration of action: ________. |
|
Definition
|
|
Term
Pancuronium+ is short/long acting ________ neuromuscular blocker. |
|
Definition
|
|
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
|
|
Term
Vecuronium+ ______ acting and has what affect on ganglionic SNS and histamine? |
|
Definition
|
|
Term
Vecuronium+ is dangerous in ______ patients sensitized to _______. |
|
Definition
hyperthyroid patients sensitized to catecholamines |
|
|
Term
Only Depolarizing Neuromuscular Blocking Drug used? |
|
Definition
|
|
Term
succinylcholine+ has a very short duration of action- 5 min due to breakdown by _______ in the plasma |
|
Definition
|
|
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
|
|
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
|
|
Term
succinylcholine more prone to cause ______ than other skeletal muscle relaxants. |
|
Definition
|
|
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
|
|
Term
Hyperthyroid patients should not be given __________ Neuromuscular Blockers. |
|
Definition
|
|
Term
Drugs Acting on Skeletal Muscle to Produce Relaxation: ________. |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
Term
Drugs that Act Prejunctionally for muscle relaxation do what ? |
|
Definition
|
|
Term
Drug that acts Prejunctionally to reduce ACh release? |
|
Definition
|
|
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
|
|
Term
Cyclobenzaprine is useful for treating ________. |
|
Definition
|
|
Term
Cyclobenzaprine is useful for treating muscle spasms over Valium because ________. |
|
Definition
|
|
Term
Cyclobenzaprine overall effect? |
|
Definition
Blocks the reuptake of NE |
|
|
Term
Cyclobenzaprine should not be taken simultaneously with a ______. |
|
Definition
|
|
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
|
|
Term
All of the therapeutically useful cholinesterase inhibitors inhibit _______ |
|
Definition
|
|
Term
Pseudocholinesterase- more/less sensitive to inhibition by organophosphate compounds than AChE |
|
Definition
|
|
Term
Organophosphate compounds are __________. |
|
Definition
irreversible AChE inhibitors |
|
|
Term
|
Definition
the plasma and glial cells |
|
|
Term
In cases of suspected organophosphate intoxication, plasma pseudocholinesterase typically inhibited ______% when RBC AChE inhibited _____% |
|
Definition
|
|
Term
ACh binds to _____ different sites on AChE before its breakdown. |
|
Definition
|
|
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
|
|
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
|
|
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
|
Definition
|
|
Term
Neostigmine+ drug metabolism? |
|
Definition
Is hydrolyzed to edrophonium by AChE |
|
|
Term
Neostigmine+ duration of action? |
|
Definition
|
|
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
|
|
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
|
|
Term
Myasthenic Syndrome (_______) |
|
Definition
|
|
Term
Myasthenic Syndrome (Lambert Eaton) is more common or rarer than MG? |
|
Definition
|
|
Term
Myasthenic Syndrome (Lambert Eaton) also involves ________. |
|
Definition
|
|
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
|
|
Term
______ is drug of treat Myasthenia gravis. |
|
Definition
|
|
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
|
Definition
Competitively binds to both the esteratic & anionic sites |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
Edrophonium+ excreted by? |
|
Definition
|
|
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
|
|
Term
Edrophonium+ can be used to treat disorder? |
|
Definition
supraventricular tachycardia |
|
|
Term
Edrophonium+ can be used to treat overdose of? |
|
Definition
|
|
Term
Physostigmine type of drug? |
|
Definition
reversible AChE inhibitor |
|
|
Term
|
Definition
|
|
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
|
|
Term
Tacrine is a _____ type of drug? |
|
Definition
Reversible AChE inhibitor |
|
|
Term
|
Definition
|
|
Term
Tacrine crosses the BBB and ________. |
|
Definition
raises ACh levels centrally |
|
|
Term
Tacrine is used to treat? |
|
Definition
|
|
Term
Tacrine & ________ are used to treat Alzheimer's. |
|
Definition
|
|
Term
Donepezil has a high degree for selectivity of ________. |
|
Definition
|
|
Term
Donepezil exhibits less ________ than Tacrine (other drug for Alzheimer's) |
|
Definition
|
|
Term
Irreversible AChE Inhibitors: ________. |
|
Definition
a. Echothiophate+ b. DFP (Diisopropyl flourophosphate) C. Parathion d. Sarin |
|
|
Term
|
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
|
|
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
|
|
Term
Parathion is a potent _____ & ______. |
|
Definition
|
|
Term
Parathion does not cause ______, like the insecticide _____ does. |
|
Definition
delayed neurotoxicity
Mipafox |
|
|
Term
Sarin is a ______ compound. |
|
Definition
|
|
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
|
|
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
|
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
|
|
Term
Myasthenia Gravis, antibodies against the ________. |
|
Definition
nicotinic Acetylcholine (ACh) receptor |
|
|
Term
Myasthenia Gravis typically affects the _____ muscles. |
|
Definition
|
|
Term
_____ is the transmitter at neuromuscular junction (NMJ). |
|
Definition
|
|
Term
Is atrophy present in MG? |
|
Definition
|
|
Term
Is weakness present in MG? |
|
Definition
|
|
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
|
|
Term
In MG The amplitude of evoked ______ decreases rapidly. |
|
Definition
compound action potentials |
|
|
Term
In MG 15% of patients have a ________. |
|
Definition
|
|
Term
In MG the density of ______ in muscle fibers is reduced. |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
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
|
|
Term
Impaired ______ in congenital form of MG. |
|
Definition
|
|
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
|
|
Term
Indirect agents act ________. |
|
Definition
|
|
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
|
|
Term
Isoproterenol is a _______ agonist/antagonist. |
|
Definition
|
|
Term
Alpha receptors sensitivity with respect to NE, E, and Isoproterenol (Iso)? |
|
Definition
|
|
Term
Beta receptors sensitivity with respect to NE, E, and Isoproterenol (Iso)? |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
Term
Smooth Muscle in vascular, action of _______ & ________ receptors- relaxation. |
|
Definition
|
|
Term
Smooth Muscle in bronchioles, action of _______ receptor- relaxation. |
|
Definition
|
|
Term
Smooth Muscle in Gut/bladder, action of _______ receptor- sphincters to contract |
|
Definition
|
|
Term
Smooth Muscle in Uterine, action of _______ receptor- relaxation (only in late gestation) |
|
Definition
|
|
Term
Smooth Muscle in Prostate, action of _______ receptor- contraction. |
|
Definition
|
|
Term
Smooth Muscle in Eye, action of Alpha1 receptor- contraction of _____ muscle. |
|
Definition
|
|
Term
Adrenergic receptors in cardiac muscle: ________ |
|
Definition
|
|
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
|
|
Term
Adrenergic receptors in skeletal muscle: ________ |
|
Definition
|
|
Term
Beta2 receptors in skeletal muscle cause ____ ion uptake. |
|
Definition
|
|
Term
Beta2 receptors in skeletal muscle cause ______ with respect to energy stores. |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
a1 Agonists Major Responses in: _______ organs. |
|
Definition
|
|
Term
a1 Agonists Major Responses in Cardiovascular? |
|
Definition
Direct - vascular contraction Indirect - slow heart rate |
|
|
Term
a1 Agonists Major Responses in Eye? |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
Term
B1 Agonists major responses: __________. |
|
Definition
-Cardiovascular: increases calcium influx increases rate and force |
|
|
Term
B1 Agonists treatments: __________. |
|
Definition
|
|
Term
B1 Agonists adverse effects: ________. |
|
Definition
|
|
Term
B1 Agonists contradicted in: _______. |
|
Definition
|
|
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
|
|
Term
Indirect-acting Drug List:
-Block transport at nerve terminal- __________. |
|
Definition
|
|
Term
Indirect-acting Drug List:
Block of vesicular transport- _______. |
|
Definition
|
|
Term
Indirect-acting Drug List:
Promotion of exocytosis and displacement of transmitter- __________. |
|
Definition
|
|
Term
Indirect-acting Drug List:
Prevention of release of transmitter- __________. |
|
Definition
|
|
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
|
|
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
|
|
Term
Catecholamine & Sympathomimetic Actions: _______ = prototypical agent |
|
Definition
|
|
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
|
|
Term
Epinephrine has _____ & _____ effects on cardiac. |
|
Definition
|
|
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
|
|
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
|
|
Term
Epinephrine in low doses has no vascular effects on __________. |
|
Definition
|
|
Term
Epinephrine in low doses has results in a ______ cardiac response. |
|
Definition
|
|
Term
Epinephrine Low Doses- Blood pressure: Increase _______, decrease ________. |
|
Definition
|
|
Term
Epinephrine in high doses has vascular, cardiac, and blood pressure effects like __________. |
|
Definition
|
|
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
|
|
Term
Norepinephrine effects Cardiac ________. |
|
Definition
|
|
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
|
|
Term
Norepinephrine non cardiovascular effects? |
|
Definition
|
|
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
|
|
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
|
Definition
|
|
Term
Because of having to give via IV, Dopamine is useful for _____, but not ______. |
|
Definition
Acute cardiac failure, not chronic |
|
|
Term
|
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
|
Definition
|
|
Term
|
Definition
|
|
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
|
|
Term
Phenylephrine: is a ______ agonist/antagonist? |
|
Definition
|
|
Term
Phenylephrine clinical use? |
|
Definition
Ophthalmological – to produce: - mydriasis (a1 effect) |
|
|
Term
Phenylephrine MOA: ________. |
|
Definition
|
|
Term
Phenylephrine adverse effect? |
|
Definition
Rebound nasal/sinus hyperemia (a1 side effect) |
|
|
Term
Phenylephrine is contradicted in those who? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
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
|
|
Term
Isoproterenol MOA: _______. |
|
Definition
|
|
Term
Isoproterenol Vascular Effects: _______. |
|
Definition
|
|
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
|
|
Term
Dobutamine used as a ______? |
|
Definition
|
|
Term
|
Definition
Cardiogenic shock & Cardiac failure
(used as a Cardiac stimulant same as Dopamine and E) |
|
|
Term
|
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
|
Definition
|
|
Term
|
Definition
- asthma & COPD (Bronchodilator B2) |
|
|
Term
|
Definition
|
|
Term
Albuterol Adverse Effects: _______. |
|
Definition
|
|
Term
Albuterol contradictions:________. |
|
Definition
- drug sensitivity - tachyarrhythmias - pregnancy |
|
|
Term
|
Definition
any disturbance of the heart rhythm in which the heart rate is abnormally increased. |
|
|
Term
Fenoldopam MOA: ________. |
|
Definition
|
|
Term
Fenoldopam is the ________. |
|
Definition
|
|
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
|
|
Term
Fenoldopam Adverse effects? |
|
Definition
|
|
Term
|
Definition
Short t1/2 & not absorbed by gut (i.v. only) |
|
|
Term
Bromocriptine MOA: __________. |
|
Definition
|
|
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
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
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
|
|
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
|
|
Term
Non-selective a blockers have an _____junctional effect on ________ receptors. |
|
Definition
|
|
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
|
|
Term
The a2 antagonistic component of Non-selective a blockers, blocks _____ release. |
|
Definition
|
|
Term
Nonselective Adrenergic Antagonists of B and a1: ___________. |
|
Definition
|
|
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
|
|
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
|
Definition
|
|
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
|
|
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
|
|
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
|
|
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
|
|
Term
B Antagonists are less effective in treating ______ in _____ race. |
|
Definition
|
|
Term
Phenoxybenzamine MOA: ________. |
|
Definition
|
|
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
|
|
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
|
|
Term
Prazocin MOA: __________. |
|
Definition
|
|
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
|
Definition
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
Term
Atenolol clinical uses: ___________. |
|
Definition
hypertension - elderly patients with isolated systolic HT - angina - post MI treatment (Carvedilol B antagonist also) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
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
|
Definition
|
|
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
|
|
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
|
|
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
|
|
Term
Betaxolol clinical use: ________. |
|
Definition
chronic open angle glaucoma1
hypertension2 |
|
|
Term
Betaxolol Adverse effects: __________. |
|
Definition
- ocular discomfort1 - bradycardia2 - depression2 - bronchospasm2 |
|
|
Term
Betaxolol Contraindications: ________. |
|
Definition
|
|
Term
Butoxamine MOA: ________. |
|
Definition
|
|
Term
|
Definition
|
|
Term
Clozapine Clinical Uses: __________. |
|
Definition
|
|
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
|
|
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
|
|
Term
ACh breakdown mediated by ___________. |
|
Definition
acetylcholinesterase (AChE) |
|
|
Term
Muscarinic Receptor Mediated Responses ______ acting & ______ lasting. |
|
Definition
|
|
Term
_______ - classical competitive antagonist for Muscarinic Receptor. |
|
Definition
|
|
Term
Muscarinic Receptors located: ________. |
|
Definition
smooth muscle, glands, & the heart |
|
|
Term
Atropine- a competitive blocker at ______ muscarinic receptors |
|
Definition
|
|
Term
________ - a competitive antagonist at M1 receptors |
|
Definition
|
|
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
|
|
Term
Nicotinic Receptor Mediated Responses ______ acting & ______ lasting. |
|
Definition
|
|
Term
Nicotinic Receptor Mediated Responses inhibitory/excitatory? |
|
Definition
|
|
Term
Muscarinic Receptor Mediated Responses inhibitory/excitatory? |
|
Definition
|
|
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
|
|
Term
Muscarinic Receptor Agonists: _____________. |
|
Definition
ACh
Methacholine+ Carbachol+ Bethanechol+ Pilocarpine Cevimeline |
|
|
Term
Which Muscarinic Receptor Agonist is broken down by AChE? |
|
Definition
|
|
Term
Methacholine+ is antagonist/agonist at? |
|
Definition
mainly agonist muscarinic |
|
|
Term
|
Definition
diagnose bronchial hyperactivity & asthmatic
diagnosis of achalasia |
|
|
Term
Methacholine+ used to diagnosis achalasia when it causes? |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
Term
Cevimeline is antagonist/agonist at? |
|
Definition
|
|
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
|
|
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
|
Definition
|
|
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
|
Definition
|
|
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
|
|
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
|
|
Term
Glycopyrrolate+ drug type? |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
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
|
|
Term
All clinically useful ganglionic blockers act at ______ receptors |
|
Definition
|
|
Term
Primary Pathway of Ganglionic Transmission mediated by __________. |
|
Definition
|
|
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
|
|
Term
Slow inhibitory potential of Secondary Pathway of Ganglionic Transmission is produced by action of _______ onto _______ receptors. |
|
Definition
|
|
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
|
Definition
nterneurons of the sympathetic ganglia (postganglionic neurons |
|
|
Term
_______ blocks dopamine action at ganglia. |
|
Definition
|
|
Term
Metoclopramide blocks dopamine action at ganglia, which would typically __________. |
|
Definition
|
|
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
|
|
Term
Ganglionic Stimulants example? |
|
Definition
|
|
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
|
|
Term
Nicotine activates nicotinic Rc’s on autonomic ganglia, stimulating transmission through __________. |
|
Definition
both parasympath & sympath ganglia |
|
|
Term
Overall Cardiovascular effect of nicotine? |
|
Definition
|
|
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
|
|
Term
nicotine increases respiration by? |
|
Definition
activate chemoreceptors in aortic arch & carotid body |
|
|
Term
In GI tracct ________ has dominant tone in GI tract. |
|
Definition
|
|
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
|
|
Term
At high toxic doses, Nicotine becomes? |
|
Definition
ganglionic blocker at high doses |
|
|
Term
Nicotine can enter the _____ easily? |
|
Definition
|
|
Term
Toxic Nicotine kills by __________. |
|
Definition
|
|
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
|
|
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
|
|
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
|
|
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 |
|
|