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Pharmacology
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Pharmacology
Graduate
09/17/2009

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Term
sympathetic nervous system
Definition
-Important regulator of activities of organs
-Especially in responses to stress
-Regulator of heart and peripheral vasculature
Term
Sympathomimetic drugs
Definition
Drugs that mimic stimulation of sympathetic nervous system
Term
mode of action
Definition
direct and indirect
Term
direct activation
Definition
drug acts directly on the receptor
Term
example of direct activation
Definition
EPI and NE
Term
indirect activation
Definition
Drug actions depend on release of endogenous catecholamines
Term
mechanisms of indirect activation
Definition
1. displacement
2. reuptake inhibition
3. blockade of metabolism
Term
displacement/releasers
Definition
Drug causes displacement (dumping) of stored catecholamines
Term
drug displacement
Definition
amphetamine and tyramine
Term
reuptake inhibition
Definition
Drugs can inhibit reuptake of catecholamines already released
Term
examples of re-uptake inhibition
Definition
cocaine and tricyclic antidepressants
Term
Blockade of metabolism occurs via
Definition
Catechol-O-methyltransferase (COMT)
Monoamine oxidase (MAO)
Term
blockade or inhibition enzymes
Definition
Increases stores of catecholamines
Indirectly potentiates sympathomimetic actions
Example: MAO Inhibitors (Parnate, Nardil, Marplan)
Term
examples of MAO inhibitors
Definition
parnate

nardil

marplan
Term
spectrum of action
Definition
Drugs can be classified by the receptors they activate
Term
example of spectrum of action
Definition
B agonist
Term
catecholamines
Definition
NE, EPI, DA
Term
catecholamines
Definition
derived from amino acid-tyrosine
Term
availability of catecholamines
Definition
Endogenously (released from adrenal glands during stress)
and As a drug
Term
Catecholamines as a drug
Definition
Not given orally- Rapidly metabolized by COMT and MAO
Term
Catecholamines as a drug
Definition
Given parentally- Short duration of action
Does not significantly enter CNS through IV route
Term
examples of Phenylisopropylamines
Definition
amphetamine
Term
Phenylisopropylamines
Definition
Are NOT catecholamines
NOT metabolized by COMT and MAO
Given orally
Enter CNS readily
Effects last longer than catecholamines
Term
tyramine
Definition
Sympathomimetic found in foods
Not a phenylisopropylamine
Is rapidly metabolized by MAO
MAO Inhibitor drugs can cause tyramine toxicity
Term
Mechanism of Action of Sympathomimetics
Definition
Act via principal receptors

α – receptors
ß – receptors
DA – receptors
Term
A1 receptor subtypes
Definition
α1A
α1B
α1D
Term
A2 receptor subtypes
Definition
α2A
α2B
α2C
Term
subtypes within subtypes
Definition
Response to drugs differs in various tissues
Term
Beta adrenoreceptors subtypes
Definition
- ß1 and ß2 (ß3 novel)
- defined by affinity for EPI and NE
Term
ß1 receptors
Definition
EPI = NE (equal affinity)
Term
ß2 receptors
Definition
EPI > NE
Term
dopamine receptors
Definition
Distinct from α and ß receptors
Mainly important in brain and splanchnic and renal vasculature
Highly relevant to behavior and Parkinson’s Disease
Term
dopamine receptors main subtypes
Definition
D1 and D2
Term
dopamine receptors subtypes within subtypes
Definition
D1 like- D1 , D5
D2 like- D2 , D3 , D4
AE and efficacy of antipsychotic drugs vary between subtypes
Term
receptor selectivity
Definition
Drug may prefer to bind to one subgroup over another at low concentrations
Not absolute (“specificity” is nearly absolute)
Numeric subclass is important for drugs with selectivity
Term
NE selectivity
Definition
NE prefers ß1 > ß2
Term
EPI selectivity
Definition
EPI ß1 = ß2
Term
prostate drugs α1 blocker
Definition
Hytrin (terazosin)

Lowers BP and relaxes neck of bladder
Term
prostate drugs α1A blocker
Definition
Flomax (tamsulosin) developed
α1A selective, found mostly in prostate & neck bladder
Results in bladder relaxation without so much BP lowering
more selective
Term
Effects of catecholamines
Definition
are mediated by cell surface receptors
Term
surface receptors
Definition
are coupled by G (guanine) proteins to produce their effects
Term
effect of catecholamines
Definition
is changing intracellular calcium concentration
Term
Stimulation of α1 receptors leads to
Definition
-activation of Gq-coupling protein

-This leads to release of IP3 and DAG

-IP3 stimulates release of sequestered stores of Ca++

-Increase in intracellular Ca++ causes contraction/constriction
Term
α 1 receptors agonist
Definition
Phenylephrine
Effects: increase IP3, DAG
Term
α 1 receptors Antagonist
Definition
Prazosin
Term
α 2 receptors Agonist
Definition
Clonidine
Term
α 2 receptors antagonist
Definition
yohimbine
Term
Stimulation of β receptors
Definition
-activate Gs coupling protein

-Results in activation of adenylyl cyclase

-Catalyzes conversion of ATP to cAMP

-Leads to Ca++ influx and release of sequestered Ca++

-Cardiac tissue=heart contractility

-SA node=increased HR

-Smooth muscle=muscle relaxation
Term
beta 1 receptor agonist
Definition
dobutamine
Term
beta 1 receptor antagonist
Definition
betaxolol
Term
beta 2 receptor agonist
Definition
albuterol
Term
beta 2 receptor antagonist
Definition
butoxamine
Term
beta 1 and 2 receptor agonist
Definition
isoproterenol -increase CAMP
Term
beta 1 and 2 antagonist
Definition
propranolol
Term
D1 receptors stimulation
Definition
Stimulates adenylyl cyclase = ↑ cAMP in smooth muscle = relaxation of smooth muscle (vasodilator)
Term
D2 receptors stimulation
Definition
Inhibit adenylyl cyclase = ↓ cAMP, open K channels and ↓ Ca influx
Term
D1 receptors agonist
Definition
Fenoldopam (used for severe HTN)
Effect: increase cAMP
Term
D2 receptors agonist
Definition
Bromocriptine - many uses, Infertility, Parkinson‘s, prevent lactation
Effect: decrease cAMP
Term
D3 receptors agonist
Definition
Effect: decrease cAMP
Term
D4 receptors antagonist
Definition
Clozapine- Effect: decrease cAMP
Term
D5 receptors
Definition
effect- increase camp
Term
Desensitization
Definition
tissue becomes less responsive with repeated exposure by agonist
a.k.a-tolerance, refractoriness and tachyphylaxis
Term
Homologous desensitization
Definition
– loss of responsiveness exclusively only to directly exposed receptors
Term
Heterologous desensitization
Definition
loss of responsiveness to exposed and some non-exposed receptors
Term
a1
Definition
most vascular smooth muscle- constriction
Term
a1
Definition
pupillary dilator muscle- contraction= dilation of pupil
Term
a1
Definition
pilomotor smooth muscle- erects hair
Term
a1
Definition
prostate- constriction
Term
a1
Definition
heart- increases force of contraction
Term
a2
Definition
postsynaptic CNS adrenoceptors- multiple effects
Term
a2
Definition
platelets- aggregation
Term
a2
Definition
adrenergic nerve terminals- inhibition of transmitter release
Term
a2
Definition
cholinergic nerve terminals- inhibition of transmitter release
Term
a2
Definition
some vascular smooth muscle- contraction
Term
a2
Definition
fat cells- inhibition of lipolysis
Term
a2
Definition
pancreatic B cells- inhibits insulin release
Term
b1
Definition
heart- increase force and rate of contraction
Term
b1
Definition
kidney (juxtaglomerular cells)- increase renin release
Term
b2
Definition
respiratory muscle- promote smooth muscle relaxation
Term
b2
Definition
uterine muscle- promote smooth muscle relaxation
Term
b2
Definition
vascular smooth muscle- promote smooth muscle relaxation
Term
b2
Definition
skeletal muscle- promotes potassium uptake= tremor
Term
b2
Definition
pancreatic B cells- increase insulin release
Term
b2
Definition
liver- activates glycogenolysis= increase glucose
Term
b3
Definition
fat cells- stimulates lipolysis
Term
d1
Definition
renal blood vessels- dilates renal blood vessels
Term
d1
Definition
splanchnic blood vessels- dilates renal blood vessels
Term
d2
Definition
nerve endings- modulates transmitter release
Term
blood vessels
Definition
control peripheral vascular resistance
Term
a1 receptors
Definition
increase arterial resistance
Term
b2 receptors
Definition
promote smooth muscle relaxation
Term
d1 receptors
Definition
promote vasodilation of kidneys playing a role in natriuresis
Term
blood vessels
Definition
effect depending on anatomical site
Term
heart
Definition
Largely determined by β1 receptors
Term
heart
Definition
-Activation results in Ca++ influx
-SA node & purkinje fibers increase – positive chronotropic effect
-AV node – conduction velocity ↑ & refractory period ↓
-Intrinsic contractility is increased – positive inotropic effect and relaxation is accelerated
-Ejection time is decreased
Term
α1 agonist
Definition
-Produces peripheral vasoconstriction and resistance

-↑ SBP and DBP
Term
b1 agonist
Definition
Increases cardiac output (↑ HR and contractility)
Term
b2 agonist
Definition
Vasodilatation and ↓ peripheral vascular resistance
Term
α receptors
Definition
mydriasis (dilation)
Term
α receptors
Definition
increases outflow of aqueous humor from the eye – reduces IOP
Term
β antagonists
Definition
decrease production of aqueous humor
Term
β agonist
Definition
decrease in accommodation- ciliary muscle
Term
b2 receptors
Definition
relaxation- bronchodilation
Term
a receptors
Definition
vasoconstriction- Blood vessels of upper respiratory tract mucosa (sinuses)
Term
a receptors mostly (b also)
Definition
GI smooth muscle relaxation
Term
a2 receptors
Definition
decrease salt and water flux into the lumen of the intestine
Term
a and b receptors contained?
Definition
uterus
Term
a receptors
Definition
mediate contraction – promotes urinary incontinence
Term
b2 receptors
Definition
bladder wall relaxation
Term
a receptors
Definition
Ejaculation- (ductus deferens, seminal vesicles & prostate)
Term
Many symphathomimetic drugs causes what?
Definition
dry mouth
Term
apocrine sweat glands is stimulated by?
Definition
adrenoceptor stimulants that causes sweaty palms
Term
b3 in fat cells causes what? (metabolic)
Definition
increase lipolysis
Term
increase in glycogenolysis in liver cause an increase in?
Definition
glucose (sympathomimetic drugs)
Term
insulin secretion is stimulated by this receptor?
Definition
b receptors
Term
insulin secretion is inhibited by this receptor?
Definition
a2 receptors
Term
renin secretion is stimulated by this receptors?
Definition
b1 receptors
Term
renin secretion is inhibited by this receptors?
Definition
a2 receptors
Term
beta blockers can lower what?
Definition
plasma renin and BP
Term
leukocytosis or an increase in WBC can be caused by what?
Definition
high doses of EPI
Term
CNS
Definition
Actions vary dramatically
Depending on ability to cross BBB
Usually cross in high rates of infusion
Nervousness, tachycardia, tremor
Elevation of mood, insomnia, anorexia
Term
Sympathomimetic Drugs
Definition
Epinephrine

Norepinephrine

Isoproterenol

Fenoldopam
Term
Sympathomimetic Drugs
Definition
Dopamine

Dopamine agonist

Dobutamine
Term
Epinephrine (adrenaline) is a potent agonist at all?
Definition
α- and β- receptors
Term
a1
Definition
increases BP and vasoconstriction
Term
b1
Definition
increase HR and increase contractility= cardiac stimulation
Term
b2
Definition
blood vessel dilation in skeletal muscle= bronchodilation
Term
types of NE?
Definition
levarterenol and noradrenaline
Term
NE stimulates what?
Definition
a and b1 receptors
Term
EPI stimulates what?
Definition
a and b1 receptors
Term
NE
Definition
a1 is greater than b1 and little effect on b2
Term
NE
Definition
increase PVR and both SBP and DBP
Term
a1 (NE)
Definition
increase BP = vasoconstriction
Term
b1 (NE)
Definition
increase HR and increase contractility= cardiac stimulation
Term
Sympathomimetic Drugs?
Definition
isoproterenol or isoprenaline
Term
Isoproterenol (isoprenaline)
Definition
Potent β- agonist (little α- effect)
Term
Isoproterenol (isoprenaline)
Definition
Positive chronotropic & inotropic actions= ↑ cardiac output
Term
Isoproterenol (isoprenaline)
Definition
Potent vasodilator
Term
Isoproterenol (isoprenaline)
Definition
↓ in diastolic & mean arterial pressure
Term
Isoproterenol (isoprenaline) b1 agonist
Definition
increase HR and increase contractility= cardiac stimulation
Term
Isoproterenol (isoprenaline) b2 agonist
Definition
blood vessel dilation in skeletal muscle= bronchodilation
Term
dopamine
Definition
precursor to NE
Term
dopamine
Definition
Activates presynaptic D2=↓ EPI release
Term
dopamine
Definition
Activates D1 and β2 = vasodilation (↓ PVR)
Term
dopamine
Definition
Activates β1 in the heart = some ↑ in HR
Term
dopamine
Definition
Low doses = ↓ PVR
Term
dopamine
Definition
High doses = activates α; mimics EPI
Term
fenoldopam
Definition
d1 receptor agonist
Term
fenoldopam
Definition
vasodilation
Term
fenoldopam
Definition
IV treatment of severe HTN
Term
other dopamine agonist?
Definition
Bromocriptine-dopamine 2 agonist
Term
Bromocriptine-dopamine 2 agonist
Definition
Tx of Parkinson’s disease
Term
Bromocriptine-dopamine 2 agonist
Definition
Tx of hyperprolactinemia
Term
dobutamine
Definition
mainly beta 1 agonist
Term
dobutamine has some?
Definition
alpha 1 agonist activity
Term
dobutamine is used in?
Definition
heart failure and shock
Term
Phenylephrine (Neo-synephrine) is an?
Definition
alpha agonist
Term
Phenylephrine (Neo-synephrine) is used for?
Definition
decongestant and to increase BP
Term
midodrine is an?
Definition
alpha agonist
Term
midodrine is used for treating?
Definition
postural hypotension
Term
Ephedrine (ma-huang) is a stimulant that releases?
Definition
catecholamines (never studied)
Term
Oxymetazoline (Afrin, Visine) is a?
Definition
direct alpha agonist
Term
Oxymetazoline (Afrin, Visine) is a vasoconstrictor used for?
Definition
decongestant and decrease eye redness
Term
Oxymetazoline (Afrin, Visine) is a type of drug?
Definition
Sympathomimetics
Term
Amphetamine is misused as a?
Definition
CNS stimulant (anorexiant and alertness)
Term
Amphetamine is a stimulant that releases?
Definition
catecholamines
Term
Methamphetamine is similar to what?
Definition
amphetamine but more CNS effect
Term
Methylphenidate (Ritalin) is stimulant used for?
Definition
ADHD
Term
pemoline is a stimulant used for?
Definition
ADHD but no longer available due to hepatic failure
Term
modafinil or provigil is a stimulant used for?
Definition
narcolepsy
Term
a2 agonists are used for?
Definition
decreasing BP and HTN
Term
give examples of a2 agonists?
Definition
clonidine, methyldopa, guanfacine, guanabenz
Term
beta 1 agonist is a?
Definition
selective agonist
Term
an example of a beta 1 selective agonist is?
Definition
-dobutamine
- Less vasodilation (less β2) = increase CO w/less tachycardia
Term
beta 2 selective agents are?
Definition
-Albuterol -used for asthma

-Terbutaline -used for uterine relaxation (premature labor)
Term
an example of a special sympathomimetics is?
Definition
cocaine
Term
cocaine causes?
Definition
nerve permeability to Na=↓nerve impulse conduction
Topical anesthetic (oral and nasal membranes)
Term
cocaine stimulates the release of?
Definition
catecholamines
Term
cocaine inhibits what?
Definition
reuptake - stimulant/sympathomimetic
Term
cocaine stimulates the release of ?
Definition
DA and inhibits reuptake that causes significant euphoria = addiction
Term
an example of a special sympathomimetic drug?
Definition
tyramine
Term
tyramine
Definition
Natural occurring in body
Also found in some fermented foods
Not a drug, but interacts with drugs
Term
tyramine
Definition
Rapidly degraded by MAO in gut and liver
When MAO is not available to degrade tyramine = high amounts of tyramine = release of catecholamines
MAO inhibitors (Nardil, Marplan, Parnate)
Results in sympathomimetic effects
Increase in BP
Term
examples of MAO inhibitors are ?
Definition
nardil, marplan, parnate
Term
Foods that contain tyramine?
Definition
Beer
Broad beans/fava beans
Cheese
Chicken liver
Chocolate
Term
Foods that contain tyramine ?
Definition
sausage
Salami
Pepperoni
Pickled herring
Snails
Red wine
Term
medications that are needed to enhance blood flow and pressure?
Definition
Norepinepherine
Phenylephrine
Methoxamine
Ephedrine
Midodrine
Term
shock is a reduction in ?
Definition
perfusion of vital tissues
Term
3 major mechanisms responsible for shock
Definition
Hypovolemia
Cardiac insufficiency
Altered vascular resistance
Term
volume replacement is ?
Definition
One of the mainstays of treatment of shock
Term
volume replacement is an ?
Definition
Efficacy of sympathomimetic drugs are used but efficacy unclear
Term
medications for treating cardiogenic shock?
Definition
dopamine and dobutamine
Term
cardiogenic shock is usually due to ?
Definition
massive MI
Term
cardiogenic shock have poor ?
Definition
prognosis
Term
cardiogenic shock have ?
Definition
positive inotropic agents with little peripheral vasoconstriction
Term
Conditions in which reduction of local or regional blood is needed
Definition
Achieving hemostasis in surgery
Reducing diffusion of anesthetics away from site of administration
Reducing mucous membrane congestions
α receptor activation usually desired
Term
EPI (cardiovascular applications)
Definition
topical nasal packs for epistaxis
In gingival string for gingivectomy
Combined with local anesthetics prolongs effects and reduces toxicity
Term
cocaine (cardiovascular applications)
Definition
Used for nasopharyngeal surgery
Has combination hemostatic and local anesthetic effect
Term
phenylphrine (cardiovascular applications)
Definition
Used for nasal decongestant
Prolonged use can cause rebound congestions due to ischemic changes
Term
isoproterenol (cardiovascular application) is used for?
Definition
Emergency management of complete heart block and cardiac arrest
Term
EPI (cardiovascular application) is used for ?
Definition
Emergency management of complete heart block and cardiac arrest
Term
dobutamine (cardiovascular application) is used for ?
Definition
heart failure
Term
type of b2 selective agents ?
Definition
metaproterenol, terbutaline, and albuterol
Term
metaproterenol is used for ?
Definition
bronchial asthma
Term
terbutaline is used for ?
Definition
bronchial asthma
Term
albuterol is used for ?
Definition
bronchial asthma
Term
anaphylaxis affect both ?
Definition
respiratory and CV system
Term
anaphylaxis can have ?
Definition
Bronchospasm

Mucous membrane congestion

Angioedema

Severe hypotension
Term
what is the treatment of anaphylaxis ?
Definition
EPI - IV or IM
Term
phenylephrine is what type of medication?
Definition
ophthalmic medication
Term
phenlylephrine is a ?
Definition
mydriatic agent to facilitate examination of the retina
Term
apraclonidine and brimonidine (a2 agonist) is what type of medication ? and what are they used for ?
Definition
ophthalmic medication and are used to lower IOP (glaucoma)
Term
ritodrine and terbutaline are medications of the ?
Definition
genitourinary
Term
ritodrine and terbutaline are b2 agonists that are used to what?
Definition
relaxes the uterus and suppress premature labor
Term
amphetamines are medication used for the ?
Definition
CNS
Term
amphetamines are used for the following effects?
Definition
mood elevating (euphoria) causing abuse
Increases alertness (modafinil for narcolepsy)
Improved attention (ADHD)
Appetite suppressant
Term
toxicity effects of sympathomimetic drugs on CV system?
Definition
increase BP, increased cardiac work which precipitates cardiac ischemia and failure
Term
toxicity effects of sympathomimetic drugs on CNS ?
Definition
restlessness, tremor, insomnia, anxiety and induced paranoid state
Term
cocaine toxicity of sympathomimetic drugs ?
Definition
convulsions, cerebral hemorrhage, arrhythmias, MI
Term
alpha receptor antagonists can be ?
Definition
reversible or irreversible
Term
alpha receptor antagonist (reversible)
Definition
Dissociate from receptors & can be surmounted by high agonist concentrations
Duration of action depends on t1/2 and rate of dissociation from receptor
Term
examples of apha receptor antagonist (reversible)?
Definition
prazosin and phentolamine
Term
alpha receptor antagonists (irreversible)
Definition
Do not dissociate & can’t be surmounted
Effects of drug may persist after drug has cleared plasma
Term
an example of alpha receptor antagonist ?
Definition
Phenoxybenzamine- restoration of tissue responsiveness is dependent on synthesis of new receptors which takes several days
Term
cardiovascular effects of alpha receptor antagonists can ?
Definition
Cause lowering of peripheral vascular resistance and blood pressure
Term
often causes of alpha receptor antagonist are ?
Definition
Postural hypotension
Reflex tachycardia
More selective to alpha-1 the less tachycardia
Term
other effects of alpha receptor antagonists are ?
Definition
Miosis (constriction of pupil)
Nasal stuffiness
Decrease resistance in urine flow
Term
an example of a specific alpha blocking agents is ?
Definition
phentolamine
Term
Phentolamine is an ?
Definition
-Antagonist at alpha 1 & 2

-Causes reduction in peripheral resistance

-Has limited absorption after oral administration

-Half life is 5-7 hrs

-Adverse effect: HA, nasal congestion, severe tachycardia, arrhythmias & myocardial ischemia
Term
phentolamine is used for treating ?
Definition
pheochromocytoma and erectile dysfunction
Term
an example of specific alpha blocking agents is ?
Definition
Phenoxybenzamine
Term
Phenoxybenzamine is used for treating ?
Definition
pheochromocytoma
Term
Phenoxybenzamine
Definition
Irreversible blockade
Long duration of action:14-48 h or longer
Somewhat selective for alpha-1
Also blocks H1, acetylcholine and serotonin
Adverse effects: postural hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation
Other effects: fatigue, sedation & nausea
Term
an example of a specific alpha blocking agent is?
Definition
prazosin (minipress)
Term
prazosin is used for treating ?
Definition
HTN
Term
prazosin (minipress) is ?
Definition
Highly selective for alpha-1
Significantly less tachycardia because less blocking of α-2
Relaxation of both arterial & venous vascular smooth muscle and smooth muscle of prostate
Metabolized by the liver
Half life: 3 hrs
Term
an example of a specific alpha blocking agents is ?
Definition
terazosin (hytrin)
Term
terazosin (hytrin) is used for treating ?
Definition
HTN and BPH
Term
terazosin (hytrin) is ?
Definition
Alpha-1 selective
Metabolized in the liver
Half life: 9-12 hrs
Term
an example of a specific alpha blocking agent is ?
Definition
doxazosin (cardura)
Term
doxazosin is used for treating ?
Definition
HTN and BPH
Term
doxazosin (cardura) is ?
Definition
Half life: 22 hrs
longer than prazosin and terazosin
Term
an example of a specific alpha blocking agent is ?
Definition
tamsulosin (flomax)
Term
Tamsulosin (Flomax) used for treating ?
Definition
BPH
Term
Tamsulosin (Flomax) is
Definition
Selective to alpha-1A subtype
Greater potency in inhibiting contraction in prostate smooth muscle than vascular smooth muscle compared to other alpha blockers
Half life: 9-15 hrs
Term
examples of other alpha antagonists are
Definition
alfuzosin (uroxatrol), indoramin, urapidil (european drug), labetalol, yohimbine
Term
alfuzosin (uroxatrol) is used for treating ?
Definition
BPH

Selective alpha-1 antagonist

Half life: 5 hrs
Term
indoramin is used for treating ?
Definition
HTN

selective alpha 1 antagonist
Term
urapidil is used for treating ?
Definition
HTN and BPH
Term
labetalol is used for treating ?
Definition
HTN
both a1 and beta blocker
Term
examples of neuroleptic drugs ?
Definition
chlorpromazine and haloperidol
Term
chlorpromazine and haloperidol are ?
Definition
potent DA receptro antagonists

also alpha antagonists

contributes to AE of hypotension
Term
yohimbine is used for ?
Definition
erectile dysfuntion
Term
yohimbine can ?
Definition
abruptly reverse the antihypertensive effects of alpha 2 agonist (clonidine)
Serious drug interaction
Term
yohimbine is an ?
Definition
alpha 2 selective antagonist
Term
pheochromocytoma is a ?
Definition
Tumor usually found on the adrenal medulla
Typically releases EPI & NE in excess
Sx: HTN, HA, palpitations & ↑ sweating
Unavoidable release of catecholamines can occur during surgery
Term
pheochromocytoma can be pretreated by this medication to control HTN before surgery ?
Definition
phenoxybenzamine
Term
can use this medication for hypertensive emergency ?
Definition
labetalol
Term
this medication can be use for treating mild to moderate hypertension ?
Definition
member of prazosin family
Term
“First Dose Phenomenon”
Definition
Interesting side effect of α-1 selective blockers
Occurs within 1-3 hours of 1st dose or increased dose
Transient dizziness or faintness
Palpitations
Orthostatic hypotension
Helps to have patient take 1st or 1st increase dose at bedtime
Term
drugs that are used for peripheral vascular disease ?
Definition
phentolamine, prazosin, or phenoxybenzamine

May be used in Raynaud’s phenomenon or other conditions involving excessive reversible vasospasms
Term
phentolamine is used to ?
Definition
reverse intense local vasoconstriction caused by inadvertent infiltration of catecholamines into subcutaneous tissue that was intended to be IV
Term
preferred drug for urinary obstruction (BPH) ?
Definition
tamsulosin- Relieving symptoms involves reversal of smooth muscle contraction of neck of bladder and enlarged prostate

prazosin, doxazosin, & terazosin considered if HTN as well
Term
drugs that are used to treat erectile dysfunction ?
Definition
phentolamine with nonspecific smooth muscle relaxant papaverine

phentolamine with nonspecific smooth muscle relaxant papaverine
Helps with ED when directly injected into penis
Longterm use can cause fibrotic changes
Other AE: priapism, orthostatic hypotension
Term
alpha 2 blocker has ?
Definition
little clinical usefulness

Research looking into
Raynaud’s phenomenon-inhibit smooth muscle contraction
Type 2 DM (alpha 2 inhibits insulin secretion)
Psychiatric depression
Term
common features of beta blockers ?
Definition
Occupy & block catecholamines effects at β receptors
End in –olol or –alol
Term
differences of beta blockers ?
Definition
Cardioselectivity
Partial agonist activity/ISA
Lipid solubility
Term
receptors that are all over the body but predominate in certain tissues and organs ?
Definition
b1 and b2 receptors
Term
receptors that are in teh heart and kidney ?
Definition
b1
Term
the stimulation of b1 receptors causes ?
Definition
↑HR, ↑contractility, ↑renin release= increase BP
Term
receptors that are located in the lungs, liver, pancreas, and arteriolar smooth muscle ?
Definition
b2
Term
the stimulation of b2 receptors causes ?
Definition
bronchodilation and vasodilation
Pancreas = ↑ insulin secretion
Liver = ↑ glycogenolysis
Term
higher affinity for β1
Definition
Blocks increase HR, contractility and renin
Without blocking broncho and vasodilation of β2 receptors in lungs, glucose and arteriolar smooth muscle
Term
Cardioselective beta blockers are preferred in ?
Definition
asthma, COPD, DM and PVD

At higher doses cardioselectivity is less
Term
examples of cardioselective beta blockers ?
Definition
Acebutolol
Atenolol
Betaxolol
Bisoprolol
Term
examples of cardioselective beta blockers ?
Definition
Celiprolol
Esmolol
Metoprolol
Nebivolol
Term
examples of non-selective beta blockers ?
Definition
Carteolol
Carvedilol
Labetolol
Nadolol
Term
examples of non-selective beta blockers ?
Definition
penbutol
Pindolol
Propranolol
Sotalol
Timolol
Term
partial β-agonist activity
Definition
Block effects of excessive sympathetic activity
Moderately activate receptors when sympathetic tone low
Therefore at rest, HR, CO and peripheral blood flow not reduced
Ideally for borderline HF, sinus bradycardia
aka: Intrinsic Sympathomimetic Activity (ISA)
Term
examples of beta blockers with ISA ?
Definition
Acebutolol
Carteolol
Celiprolol
Term
examples of beta blockers with ISA ?
Definition
Labetalol
Penbutolol
Pindolol
Term
more lipophilic the more ?
Definition
CNS penetration

Increase in side effects
Depression
Sedation
Term
beta blockers and high lipid solubility ?
Definition
Carvedilol
Penbutolol
Propranolol
Term
beta blockers and moderate lipid solubility ?
Definition
Labetolol
Metoprolol
Pindolol
Timolol
Term
beta blockers and low lipid solubility ?
Definition
Acebutolol
Atenolol
Betaxolol
Bisoprolol
Carteolol
Celiprolol
Esmolol
Nadolol
Sotalol
Term
labetolol and carvedilol are ?
Definition
Non selective BB
Alpha 1 blocker
Term
nebivolol (bystlic) are ?
Definition
Newest BB (approved 12/07)
Cardioselective BB
Nitric oxide mediated vasodilation
Term
blocking b1 can make the heart have a ?
Definition
negative chronotropic and inotropic effects
Term
blocking b1 can make the kidney ?
Definition
decrease renin release
Term
Antiarrhythmic
Definition
Decrease in SA and AV node conduction
Term
blocking b2 (non cardioselective BB) leads to ?
Definition
increased airway constriction and bronchospasms

Use in caution w/ asthma or COPD
Pts with COPD tolerate the drugs better
Select cardioselective BB in these pts
Term
Can increase or decrease glucose (B2)
Definition
decrease insulin
decrease glycogenolysis
use with caution in diabetics
Term
Altered lipid metabolism
Definition
Chronic use can reduce HDL
ISA BB’s have less altered lipid effects
Term
special agents are ?
Definition
propranolol, metoprolol, atenolol, nadolol, timolol, levobunolol, betaxolol, and esmolol
Term
propranolol
Definition
1st BB approved for clinical use
Half life: 3.5-6hrs
Selectivity: none
Partial agonist activity: no
Highly lipid soluble
Term
metoprolol and atenolol
Definition
Cardioselective
Preferred in respiratory diseases and PVD
Term
nadolol
Definition
Longest durations of action
Half life: 14-24 hrs
Term
timolol, levobunolol, and betaxolol
Definition
Non selective
Excellent ocular hypotensive effects with opthalmic use
Used in glaucoma
Term
esmolol
Definition
Ultra short acting
Half life: 10 min
Given as continuous IV infusion
Selectivity: Beta 1
Useful in tx supraventricular arrhythmias
Term
the use of BB can effectively treatment this disease ?
Definition
hypertension

Proven to be effective & well tolerated
Less effective in elderly & African-Americans
Term
BB can also treat ?
Definition
Ischemic Heart Disease
Reduce frequency of anginal episodes & improve exercise tolerance
Reduces oxygen demand
Relative contraindications: bradycardia, hypotension, left ventricular failure, shock, heart block, active airway disease
Term
BB can also treat ?
Definition
Cardiac Arrhythmias


Effective in tx supraventricular & ventricular arrhythmias
Slows ventricular response rates in AFib & AFlutter
Term
BB can also treat ?
Definition
Heart Failure

Can worsen acute CHF
Chronic use can prolong life
MOA uncertain

Proven efficacy
metoprolol, bisoprolol or carvedilol
Term
BB can also treat ?
Definition
Chronic Glaucoma (open angle glaucoma)

Leading cause of Blindness
As eyes age increase in IOP can occur by
Over production of aqueous fluid and build up
Drainage system clogging
Increase in pressure causes damage to optic nerve and retina
Term
open glaucoma
Definition
Pressure is due to overproduction or blocked drainage of fluid despite open space between iris and cornea
Term
narrow glaucoma
Definition
Pressure is due to outflow of fluid being blocked due to structural abnormality
Term
Narrow Angle or closed angle is usually ?
Definition
acute & causes pain (unlike open)
Usually treated urgently with surgery or drugs
Term
Pre-op drugs limited to ? (narrow angle or closed angle)
Definition
Cholinomimetics
Acetazolamide
Osmotic agents
Onset of action of others too slow
Term
5 General Drug Classes used for glaucoma ?
Definition
Cholinomimetics
α agonists
BB
Prostaglandin analogs
Diuretics
Term
Cholinomimetics
Definition
Parasympathomimetic
Directly stimulates cholinergic receptors
Produces contraction of iris sphincter muscle
pupillary constriction (miosis)
constriction of the ciliary muscle
resulting in increased accommodation
reduction in intraocular pressure
associated with an increase in the outflow and a decrease in the inflow of aqueous humor
Term
examples of cholinomimetic drugs ?
Definition
Pilocarpine
Carbachol
Physostigmine
Echothiophate
Demecarium
Term
unselective alpha agonists ?
Definition
Epinephrine and dipivefrin
Mechanism: increase outflow
Term
alpha 2 selective alpha agonists ?
Definition
Apraclonidine and brimonidine
Mechanism: decrease aqueous secretion
Term
examples of beta blockers?
Definition
Timolol, betaxolol, carteolol, levobunolol, metipranolol
Mechanism: decrease aqueous secretion from the epithelium
Timolol drops can be systemically absorbed
Heart rate and airway effects
Can interact with other oral drugs like verapamil
Term
Carbonic anhydrase inhibitors (diurectics)
Definition
Carbonic anhydrase enzyme is responsible for productions of forming hydrogen and bicarb ions from carbon dioxide and water
Inhibiting this enzyme causes decrease HCO3- resulting in diuretic effect
Also causes decrease aqueous secretion
Term
examples of carbonic anhydrase inhibitors (diuretics) ?
Definition
Dorzolamide, brinzolamide, acetazolamide, dichlorphenamide, methazolamide
Term
Prostaglandin F2α
Definition
Selective agonists for FP prostaglandin receptor
Results in increase outflow of aqueous humor
Term
examples of Prostaglandin F2α ?
Definition
Latanoprost, bimatoprost, travoprost, unoprostone
Term
BB can also treat ?
Definition
Hyperthyroidism

Inhibition of thyroxine (T4) conversion to triiodothyronine (T3)
Tx: thyroid storm w/ propranolol
Controls supraventricular tachycardias that often precipitate heart failure
Term
BB can also treat ?
Definition
Neurologic Disease
Migraines: propranolol reduces frequency & intensity
“Stage fright”: propranolol
Alcohol withdrawal in some pts
Term
BB can also treat ?
Definition
Esophageal varicies
BB reduce portal vein pressure in cirrhosis pts
Propranolol and nadolol can also prevent bleeding and decrease mortality
Term
BB and Clinical Toxicology
Definition
Rash, fever, sedation, sleep disturbances, depression
More lipid soluble = more CNS side effects
Nadolol and atenolol are most water soluble
Term
BB and Clinical Toxicology
Definition
Major Side Effects
Worsening or respiratory diseases
Life saving CVD benefits likely outweigh risk
Worsening of PVD
Worsening or heart failure
Hypotension
Bradycardia
Term
BB and Clinical Toxicology
Definition
Can produce a syndrome of sympathetic over activity
agitation, headache, sweating, and nausea
Can provoke rapid upswings in blood pressure
Term
BB and Clinical Toxicology
Definition
May mask symptoms of hypoglycemia in diabetics
Except sweating
Important counseling point
Term
therapeutic uses of BB ?
Definition
Performance anxiety
Mitral valve prolapse
Post-MI
HTN
Open angle glaucoma
Cardiac dysrythmias
Thyroid storm
Term
therapeutic uses of BB ?
Definition
Angina
Migraine prophylaxis
CHF
Aggressive behavior
Pheochromocytoma
GI hemorrhage
Essential tremors
Drug overdose???
Term
Cocaine Overdose Management
Definition
Avoid beta-blockers to treat HTN
Term
Sympathetic
Definition
Thoracolumbar
“fight or flight”
Term
Enteric Nervous System
Definition
Collection of neurons in the walls of the gastrointestinal system
Term
Parasympathetic
Definition
“rest and digest”
Craniosacral
Term
Afferent (sensory) fibers
Definition
Run from periphery to integrating centers
Enteric plexus in gut
Term
Cholinergic fibers release
Definition
ACH
Term
Noradrenergic (adrenergic) fibers releases
Definition
Norepinephrine (noradrenaline)
Term
is an important vasodilator transmitter in renal blood vessels
Definition
dopamine
Term
cells that release Epi & NE?
Definition
adrenal medulla
Term
Most autonomic nerves also releases ?
Definition
contransmitters
Term
In most sympathetic postganglionic neurons, this is the primary transmitter ?
Definition
NE
Term
examples of transmitters ?
Definition
ATP
CGRP
CCK
Dopamine
Enkephalin
Galanin
GABA
GRP
Term
examples of transmitters ?
Definition
Neuropeptide Y
Nitric oxide
NE
Serotonin (5-HT)
Substance P
Vasoactive intestinal peptide
Term
cholinergic receptors are affected by ?
Definition
ACH
Term
subtypes of cholinergic receptors are
Definition
muscarinic receptors
nicotinic receptors
Term
CNS, sympathetic postganglionic neurons, some presynaptic sites
Definition
M1
Term
Myocardium, smooth muscle, some presynaptic sites, CNS
Definition
M2
Term
Exocrine glands, vessels (smooth muscle & endothelium), CNS neurons
Definition
M3
Term
CNS, possibly vagal nerve endings
Definition
M4
Term
Vascular endothelium, esp. cerebral vessels, CNS
Definition
M5
Term
cholinoceptors are from ?
Definition
M1 to M5 and Nn, Nm
Term
Postganglionic neurons, some presynaptic cholinergic terminals
Definition
Nn
Term
Skeletal muscle neuromuscular end plates
Definition
Nm
Term
adrenergic receptors are affected by ?
Definition
catecholamines
Term
examples of catecholamine are ?
Definition
Norepinephrine (NE)
Epinephrine (EPI)
Dopamine (DA)
Term
subtypes of adrenergic receptors are
Definition
α-adrenoceptors
β-adrenoceptors
Dopaminergic
Term
types of adrenoceptors are ?
Definition
A1, A2, B1, B2, and B3
Term
Postsynaptic effector cells, esp. smooth muscle
Definition
alpha 1
Term
Presynaptic adrenergic nerve terminals, platelets, lipocytes, smooth muscle
Definition
alpha 2
Term
Post-synaptic effector cells, esp. heart, lipocytes, brain
Definition
Beta 1
Term
Post-synaptic effector cells, esp. smooth muscle and cardiac muscle
Definition
Beta 2
Term
Post-synaptic effector cells, esp. lipocytes and heart
Definition
Beta 3
Term
autonomic receptors (dopamine receptors)
Definition
D1, D2, D3, D4
Term
Brain, effector tissue, esp. smooth muscle of the renal vascular bed
Definition
D1
Term
Brain, effector tissues, esp. smooth muscle, presynaptic nerve terminals
Definition
D2
Term
brain
Definition
D3
Term
Brain, cardiovascular system
Definition
D4
Term
Iris radial muscle – alpha 1 (SA)
Definition
contracts
Term
Ciliary muscle – beta – (SA)
Definition
relaxes
Term
Iris circular muscle – M3 – (PA)
Definition
contracts
Term
Ciliary muscle – M3 - (PA)
Definition
contracts
Term
SA node – Beta1/Beta2 – (SA)
Definition
accelerates
Term
Ectopic pacemakers – Beta1/Beta2 – (SA)
Definition
accelerates
Term
Contractility – Beta 1/Beta2 – (SA)
Definition
increases
Term
SA node – M2 – (PA)
Definition
decelerates
Term
Contractility – M2 – (PA)
Definition
decreases (atria)
Term
Skin, splanchnic vessels – alpha (SA)
Definition
contracts
Term
Skeletal muscle vessels – Beta2 – (SA)
Definition
relaxes
Term
Skeletal muscle vessels – alpha (SA)
Definition
contracts
Term
Skeletal muscle vessels – M3 – (SA)
Definition
relaxes
Term
Endothelium – M3/M5 (PA)
Definition
release EDRF
Term
Bronchiolar Smooth Muscle- Beta2 (SA)
Definition
relaxes
Term
Bronchiolar Smooth Muscle-M3- (PA)
Definition
contracts
Term
Gastrointestinal Tract-Smooth muscle of wall – alpha 2/Beta 2 – (SA)
Definition
relaxes
Term
Gastrointestinal Tract- Smooth muscles of sphincters – alpha 1 – (SA)
Definition
contracts
Term
Gastrointestinal Tract- Smooth muscle of wall – M3 – (SA)
Definition
contracts
Term
Gastrointestinal Tract- Smooth muscles of sphincters – M3 – (SA)
Definition
relaxes
Term
Gastrointestinal Tract- Secretion – M3 – (SA)
Definition
increases
Term
Genitourinary Smooth Muscle- Bladder wall – Beta 2 – (SA)
Definition
relaxes
Term
Genitourinary Smooth Muscle- Sphincter – alpha 1 – (SA)
Definition
contracts
Term
Genitourinary Smooth Muscle- Uterus, pregnant – Beta 2 (SA)
Definition
relaxes
Term
Genitourinary Smooth Muscle- Uterus, pregnant – alpha – (SA)
Definition
contracts
Term
Genitourinary Smooth Muscle- Penis, seminal vesicle – alpha – (SA)
Definition
ejaculation
Term
Genitourinary Smooth Muscle- Bladder wall – M3 – (PA)
Definition
contracts
Term
Genitourinary Smooth Muscle- Sphincter – M3 – (PA)
Definition
relaxes
Term
Genitourinary Smooth Muscle- Uterus, pregnant – M3 (PA)
Definition
contracts
Term
Genitourinary Smooth Muscle- Penis, seminal vesicle – M3- (PA)
Definition
erection
Term
Pilomotor smooth muscle – alpha -(SA)
Definition
contracts
Term
Sweat glands – thermoregulatory – M (SA)
Definition
increases
Term
Sweat glands – apocrine (stress) – alpha (SA)
Definition
increases
Term
Liver -Beta2/alpha (SA)
Definition
gluconeogenesis
Term
liver Beta2/alpha (SA)
Definition
glycogenolysis
Term
Fat cells Beta3 (SA)
Definition
lipolysis
Term
kidney beta 1(SA)
Definition
renin release
Term
central integration occurs in ?
Definition
Occurs in midbrain and medulla
ANS fully integrated
Term
Cooperative interactions in ANS Occur in ?
Definition
brain stem, medulla, spinal cord
Baroreceptor in glossopharyngeal nerve
Sensory fibers in the urinary bladder wall
Term
Example: slow infusion of NE
Definition
Powerful vasoconstriction: ↑ peripheral vascular resistance → ↑ MAP
Term
Example: slow infusion of NE (cardiac)
Definition
Negative feedback baroreceptor responds to ↑ MAP
Term
NET effect of ↑ peripheral vascular resistance, ↑ MAP, and a ?
Definition
decrease in HR
Term
autoreceptors respond to ?
Definition
primary NT
Term
autoreceptors modulate release of ?
Definition
NT by the nerve
Usually inhibitory
Term
Heteroreceptors May be activated by ?
Definition
NTs released by other nerve terminals that synapse with the nerve ending
Term
example of heteroreceptor action
Definition
Vagal fibers in myocardium synapse on sympathetic adrenergic nerve terminals and inhibit NE release.
Term
Modulation by history of activity (postsynaptic regulation)
Definition
Up-regulation or down-regulation of receptor
Term
example of Modulation by history of activity (postsynaptic regulation)
Definition
Denervation supersensitivity
Reserpine
Term
Potential Pharmacologic Targets
Definition
Synthesis
Storage
Release
Termination of action
Function of receptor
Term
Action potential propagation
Definition
-Examples: local anesthetics, tetrodotoxin (toxin of puffer fish), saxitoxin (toxin of gonyaulax – red tide organism)

-Site: nerve axons

-Action: blocks sodium channel, blocks conduction
Term
Transmitter synthesis
Definition
-Example: hemicholinium

-Site: membrane of cholinergic nerve terminals

-Action: blocks uptake of choline and slows synthesis
Term
Transmitter synthesis
Definition
-Example: alpha-methyltyrosine (metyrosine)

-Site: cytoplasm of adrenergic nerve terminals and adrenal medulla

-Action: blocks synthesis
Term
Transmitter storage
Definition
-Example: vesamicol

-Site: cholinergic terminal vesicles

-Action: prevents storage, depletes ACh
Term
Transmitter storage
Definition
-Example: reserpine

-Site: adrenergic terminal vesicles

-Action: prevents storage, depletes NE and dopamine
Term
Transmitter release
Definition
-Example: NE, DA, ACh, angiotensin II, various prostaglandins

-Site: nerve terminal membrane receptor

-Action: modulates release
Term
Transmitter release
Definition
-Example: omega-conotoxin GVIA (toxin of marine snails)

-Site: nerve terminal calcium channel

-Action: reduces transmitter release
Term
Transmitter release
Definition
-Example: Botulinum toxin

-Site: cholinergic vesicles

-Action: prevents release
Term
Transmitter release
Definition
-Example: alpha latrotoxin (black widow spider venom)

-Site: cholinergic and adrenergic vesicles

-Action: causes explosive transmitter release
Term
Transmitter release
Definition
-Example: tyramine, amphetamine

-Site: adrenergic nerve terminals

-Action: promote transmitter release
Term
Transmitter uptake after release
Definition
-Example: cocaine, tricyclic antidepressants

-Site: adrenergic nerve terminals

-Action: inhibit uptake, increase transmitter effect on postsynaptic receptors
Term
Receptor activation or blockade
Definition
-Example: norepinephrine

-Site: receptors at adrenergic junctions

-Action: binds alpha receptors, causes contraction
Term
Receptor activation or blockade
Definition
-Example: phentolamine

-Site: receptors at adrenergic junctions

-Action: binds alpha receptors, prevents activation
Term
Receptor activation or blockade
Definition
-Example: isoproterenol

-Site: receptors at adrenergic junctions

-Action: binds beta receptors
Term
Receptor activation or blockade
Definition
-Example: propranolol

-Site: receptors at adrenergic junctions

-Action: binds beta receptors, prevents activation
Term
Receptor activation or blockade
Definition
-Example: nicotine

-Site: receptors at nicotinic cholinergic junctions (autonomic ganglion, neuromuscular end plates)

-Action: binds nicotinic receptors, opens ion channel in postsynaptic membrane
Term
Receptor activation or blockade
Definition
-Example: bethanechol

-Site: receptors, parasympathetic effector cells (smooth muscle, glands)

-Action: binds and activates muscarinic receptors
Term
Receptor activation or blockade
Definition
-Example: atropine

-Site: receptors, parasympathetic effector cells

-Action: binds muscarinic receptors, prevents activation
Term
Enzymatic inactivation of transmitter
Definition
-Example: neostigmine

-Site: cholinergic synapses (acetylcholinesterase)

-Action: inhibits enzyme which prolongs and intensifies transmitter action
Term
Enzymatic inactivation of transmitter
Definition
-Example: tranylcypromine

-Site: adrenergic nerve terminals (monoamine oxidase)

-Action: inhibits enzyme which increases stored transmitter pool
Term
types of cholinomimetics drugs ?
Definition
ACh agonists, achE inhibitors, muscarinic, and nicotinic
Term
drugs that mimic ACH action?
Definition
ach agonists and ACHE inhibitors
Term
affect cholinoceptors
Definition
muscarinic and nicotinic
Term
tissues that are effected by muscarinic
Definition
smooth muscle, heart, & exocrine glands
Term
tissue that are effected by nicotinic
Definition
Skeletal muscle & autonomic ganglia
Term
muscarinic receptors (cholinoceptors)
Definition
G-protein-linked
Term
nicotinic (cholinoceptors)
Definition
ion channel
Term
M1
Location:
Definition
nerves
Term
M1 structural feature
Definition
seven transmembrane segments, Gq/11 protein linked
Term
M1 Postreceptor Mechanism:
Definition
IP3, DAG cascade
Term
M2 (cardiac M2)
Location:
Definition
heart, nerves, smooth muscle
Term
M2 (cardiac M2) Structural features:
Definition
seven transmembrane segments, Gi/0 protein linked
Term
M2 (cardiac M2) Postreceptor Mechanism:
Definition
inhibition of cAMP production, activation of K+ channels
Term
cholinoceptors
Definition
M1 to M5, and Nm, and Nn
Term
M3
Location:
Definition
Glands, smooth muscle, endothelium
Term
M3 Structural Features:
Definition
seven transmembrane segments, Gq/11 protein linked
Term
M4 Postreceptor Mechanism:
Definition
IP3, DAG cascade
Term
M4
Location:
Definition
Structural Features: seven transmembrane segments, Gi/0 protein linked
Term
M4 Postreceptor Mechanism:
Definition
inhibition of cAMP production
Term
M5
Location:
Definition
CNS
Term
M5 Structural Features:
Definition
seven transmembrane segments, Gq/11 protein linked
Term
M5 Postreceptor Mechanism:
Definition
IP3, DAG cascade
Term
NM (muscle type, end plate receptor)
Location:
Definition
Skeletal muscle neuromuscular junction)
Term
NM (muscle type, end plate receptor) Structural Features:
Definition
pentamer
Term
NM (muscle type, end plate receptor) Postreceptor Mechanism:
Definition
Na+, K+ depolarizing ion channel
Term
NN (neuronal type, ganglion receptor)
Location:
Definition
postganglionic cell body, dendrites
Term
NN (neuronal type, ganglion receptor) Structural Features:
Definition
α2β2/ α 3 β3
Term
NN (neuronal type, ganglion receptor) Postreceptor Mechanism:
Definition
Na+, K+ depolarizing ion channel
Term
Direct acting cholinomimetic agents
Bind M receptors and/or N receptors
Definition
Choline Esters
Alkaloids
Term
Indirect acting agents
Definition
“reversible”
“irreversible”
Term
are Poorly absorbed and distributed into CNS
Definition
hydrophilics
Term
Choline Ester Characteristics
Definition
-Hydrophilic
Poorly absorbed and distributed into CNS

-Hydrolyzed in GI tract
-Differing susceptibility to hydrolysis
ACh is rapidly hydrolyzed
A large IV bolus lasts 5-20 seconds

-Methacholine → Carbachol, bethanechol
Term
Alkaloid Characteristics
Definition
-Well absorbed from most sites of administration

-Nicotine can be absorbed through the skin

-Mainly excreted by the kidneys

-Acidifying the urine increases clearance
Term
Direct agonist: action on Cholinoceptor
Definition
muscarinic, and nicotinic
Term
Muscarinic (ACh released from PNS)
Definition
Directly alters effector organ function
Binds muscarinic receptors on neurons which inhibits release of neurotransmitters
Term
Nicotinic
Definition
Depolarizing blockade
Term
Eye Receptor: muscarinic Sphincter muscle of iris
Definition
contraction – miosis
Term
Eye Receptor: muscarinic
Ciliary muscle
Definition
contraction -accommodation
Term
Cardiovascular
Receptors: muscarinic
SA Node
Definition
Decrease in rate
Term
Cardiovascular
Receptors: muscarinic
atria
Definition
Decrease in contractile strength & refractory period
Term
Cardiovascular
Receptors: muscarinic
AV node
Definition
Decrease in conduction velocity
Increase in refractory period
Term
Cardiovascular
Receptors: muscarinic
ventricles
Definition
Small decrease in contractile strength
Term
Cardiovascular
Receptors: muscarinic
net effect:
Definition
reduction in peripheral vascular resistance and change in heart rate
Term
Blood Vessels
muscarinic
Arteries
Definition
Dilation (via EDRF)
High dose direct effector response - constriction
Term
Blood Vessels
muscarinic
veins
Definition
Dilation (via EDRF)
High dose direct effector response - constriction
Term
Respiratory System (Lungs)
Receptor: Muscarinic
bronchial muscle
Definition
constriction (bronchoconstriction)
Term
Respiratory System (Lungs)
Receptor: Muscarinic
bronchial glands
Definition
stimulation
Term
Gastrointestinal Tract
Receptor: muscarinic
Motility
Definition
increase
Term
Gastrointestinal Tract
Receptor: muscarinic
sphincters
Definition
relaxation
Term
Gastrointestinal Tract
Receptor: muscarinic
secretion
Definition
stimulation
Term
Genitourinary tract (urinary bladder)
Receptors: muscarinic
Detrusor
Definition
contraction
Term
Genitourinary tract (urinary bladder)
Receptors: muscarinic
trigone and sphincter
Definition
relaxation
Term
Secretory Glands
Receptors: muscarinic
Sweat
Definition
secretion
Term
Secretory Glands
Receptors: muscarinic
salivary
Definition
secretion
Term
Secretory Glands
Receptors: muscarinic
lacrimal
Definition
secretion
Term
Secretory Glands
Receptors: muscarinic
nasopharyngeal
Definition
secretion
Term
CNS receptors are
Definition
muscarinic and nicotinic
Term
brain is richer in what receptors?
Definition
muscarinic
Term
spinal cord is richer in what receptors ?
Definition
nicotinic
Term
nicotinic receptors in high levels causes ?
Definition
tremor, emesis, and stimulation of the respiratory system
Term
nicotinic receptors in higher levels causes ?
Definition
convulsions which can lead to fatal coma
Term
PNS
Definition
Nicotine has greater affinity for neuronal nicotinic receptors
hypertension
nausea
vomiting
diarrhea
Voiding of urine
Term
Neuromuscular junction
Receptor:
Definition
nicotinic on the neuromuscular end plate
Term
nicotinic on the neuromuscular end plate result in ?
Definition
immediate depolarization of the end-plates
Term
primary target of MOA ?
Definition
ACHE

note:Butyrylcholinesterase – also inhibited
Term
examples of cholinesterase inhibitors ?
Definition
edrophonium
carbamates
neostigmine
organophosphates
echothiophate
Term
types of direct-acting cholinomimetics ?
Definition
MOA and cholinesterase inhibitors
Term
carbamates
Definition
-Relatively insoluble due to permanent charge

-Poor absorption from conjunctiva, skin, and lungs

-Larger oral doses required

-Negligible distribution to CNS

-Physostigmine is well absorbed though
Duration determined by stability of inhibitor-enzyme complex
Term
Organophosphates
Definition
-Well absorbed from skin, lung, gut, and conjunctiva

-Effective insecticides but dangerous to humans

-Distributed to all parts of the body
Exception is echothiophate

-CNS toxicity
Term
(Alcohols) Edrophonium Uses for ?
Definition
Myasthenia gravis
Ileus

2-10 minutes
Term
(Carbamates and related agents) Neostigmine Uses for ?
Definition
Myasthenia gravis
Ileus

1/2 hour to 2 hours
Term
(Carbamates and related agents) pyridostigmine uses for ?
Definition
myasthenia gravis

3 to 6 hours
Term
(Carbamates and related agents) Physostigmine Uses for ?
Definition
glaucoma

1/2 hour to 2 hours
Term
(Carbamates and related agents) ambenonium uses for ?
Definition
myasthenia gravis

4 to 8 hours
Term
(Organophosphates) Echothiophate Uses for ?
Definition
glaucoma

100 hours
Term
(Organophosphates) malathion and parathion are ?
Definition
Highly lipid soluble
Thiophosphate prodrugs
Insecticides
Term
Indirect Pharmacodynamics- AGING!
Definition
-Involves the breaking down of one oxygen-phosphorus bond of the inhibitor

-Further strengthens the phosphorus enzyme bond

-“Cholinesterase regenerators” can break the phosphorus enzyme bond if given before aging

-More difficult to break if aging has occurred
Term
Indirect – Organ System Effects - most prominent effects are seen in ?
Definition
CV system
GI system
Eye
Skeletal muscle neuromuscular junction
Term
CNS in Low concentrations (Indirect – Organ System Effects)
Definition
diffuse activation on electroencephalogram and subjective alerting response
Term
CNS in higher concentration (indirect-organ system effects)
Definition
generalized convulsions that can lead to coma and respiratory arrest
Term
EYE- sphincter muscle of iris (indirect organ system effect
Definition
contraction- miosis
Term
EYE- ciliary muscle (indirect organ system effect
Definition
contraction for near vision
Term
RESPIRATORY- bronchial muscle (indirect organ system effect
Definition
constriction (bronchoconstriction)
Term
RESPIRATORY -bronchial glands (indirect organ system effect
Definition
stimulation
Term
Gastrointestinal tract -Motility (Indirect – Organ System Effect)
Definition
increase
Term
Gastrointestinal tract- sphincters (Indirect – Organ System Effects)
Definition
relaxed
Term
Gastrointestinal tract-secretion (Indirect – Organ System Effects)
Definition
stimulation
Term
Urinary Tract-Detrusor (Indirect – Organ System Effects)
Definition
contraction
Term
Urinary Tract- trigone and sphincter (Indirect – Organ System Effects)
Definition
relaxation
Term
Cardiovascular System (Indirect – Organ System Effects)
Definition
Increases activity in both sympathetic and parasympathetic ganglia

Fall in cardiac output due to bradycardia

Decrease in atrial contractility

Reduction in ventricular contractility
Term
Vascular smooth muscle – minimal effect (Indirect – Organ System Effects)
Definition
Vascular resistance may be increased
Term
Neuromuscular junction- Low (therapeutic) concentrations (Indirect – Organ System Effects)
Definition
Moderately prolong and intensify actions of ACh
Increases strength of muscle contraction
Term
Neuromuscular junction- Higher concentrations
(Indirect – Organ System Effects)
Definition
Accumulation of ACh
Fibrillation of muscle fibers
Fasciculations of entire motor unit
Term
Eye diseases (Cholinomimetics – Clinical Use)
Definition
Glaucoma
Accommodative esotropia
Term
GI/GU (Cholinomimetics – Clinical Use)
Definition
Post operative atony, neurogenic bladder
Term
Neuromuscular junction (Cholinomimetics – Clinical Use)
Definition
myasthenia gravis
Term
heart (Cholinomimetics – Clinical Use)
Definition
certain atrial arrhythmias
Term
Bethanechol- Cholinomimetics – Clinical Use for ?
Definition
Post-op and Neurogenic Ileus and Urinary Retention
Term
Carbachol- Cholinomimetics – Clinical Use for ?
Definition
glaucoma
Term
Pilocarpine- Cholinomimetics – Clinical Use for ?
Definition
Glaucoma, Sjogren’s Syndrome
Term
Nicotine- Cholinomimetics – Clinical Use for ?
Definition
smoking deterrence
Term
Glaucoma –
Definition
increased intraocular pressure
Term
Muscarinic stimulants and AChE inhibitors reduces ?
Definition
intraocular pressure

Contraction of ciliary body
Facilitate outflow of aqueous humor
Decrease rate of secretion of aqueous humor
Term
Glaucoma Treatment (direct agonist) medications ?
Definition
pilocarpine, methacholine, carbachol
Term
Glaucoma Treatment (cholinesterase inhibitors)
Definition
physostigmine, echothiophate
Term
Glaucoma Treatment
Definition
Topical Beta Blockers and Prostaglandin derivatives
Term
Acute angle-closure glaucoma is a medical emergency
and treated initially with ?
Definition
direct muscarinic agonist and a cholinesterase inhibitor (pilocarpine plus physostigmine)

Once intraocular pressure is controlled and danger of vision loss is diminished – surgery (iridectomy)
Term
Postoperative ileus w/o obstruction and Increase tone of LES (pts w/ reflux esophagitis/GERD/reflux) can be treated with ?
Definition
Bethanechol 10-25 mg PO TID or QID
Neostigmine 15 mg PO
Term
Sjogren’s syndrome is treated with ?
Definition
pilocarpine to increase salivary secretions
Term
Urinary retention – postoperative or postpartum
and Neurogenic bladder (secondary to spinal cord injury or disease) can be treated with ?
Definition
Bethanechol 5mg subcutaneously, may be repeated in 30 min if necessary

Neostigmine 0.5 to 1 mg subcutaneously

Neostigmine 15 mg PO
Term
Myasthenia gravis is disease ?
Definition
affecting skeletal muscle neuromuscular junction (autoimmune process)
Term
Neuromuscular Junction is ?
Definition
Extremely sensitive to actions of drugs that interfere with neuromuscular junction – aminoglycoside antibiotics
Term
are valuable in treating myasthenia gravis ?
Definition
cholinesterase inhibitors
Term
is used in diagnosing myasthenia gravis ?
Definition
edrophonium
Term
long term treatment myasthenia gravis ?
Definition
pyridostigmine with neostigmine or ambenonium as alternatives

Doses titrated based on changes in muscle strength

Require frequent dosing
Term
treatment for Supraventricular tachyarrhythmias ?
Definition
adenosine and calcium channel blockers

Edrophonium was once used
Term
is amodest efficacy and significant hepatic toxicity in treatment of Alzheimer’s ? (CNS)
Definition
tacrine
Term
is a modest clinical benefit in treatment of Alzheimer’s ? (CNS)
Definition
donepezil
Term
is a direct acting nicotinic agonist used in smoking cessation ? (CNS)
Definition
varenicline

Toxicity includes nausea, headache, and sleep disturbance
Term
Direct acting Muscarinic (toxicity)- pilocarpine
Definition
nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, and bronchial constriction
Term
Mushrooms (toxicity)
Definition
nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation and bronchial constriction

symptoms within 15-30 minutes of ingestion

Treatment: Atropine 1-2 mg parenterally
Term
Direct acting Nicotinic (toxicity)
Definition
Fatal dose of nicotine 40 mg or 1 drop of pure liquid (same amount of nicotine in 2 regular cigarettes)

CNS stimulation: convulsions, coma, respiratory arrest
Skeletal muscle end plate depolarization leading to respiratory paralysis
Hypertension and cardiac arrhythmias
Term
Direct acting Nicotinic (toxicity)
Definition
Acute toxicity treatment: directed towards symptoms

Muscarinic – atropine

Central stimulation – anticonvulsants (diazepam)

Neuromuscular – does not respond to drugs so mechanical respiration required

Nicotine is metabolized and excreted rapidly – pt may survive and recover completely if hypoxia and brain damage hasn’t occurred in the first 4 hrs
Term
Cholinesterase Inhibitors (toxicity)
Definition
Usually from pesticides in agriculture or home use

Signs of muscarinic excess: diarrhea, urination, miosis, bronchoconstriction, excitation (of skeletal muscle and CNS), lacrimation, and salivation and sweating → “DUMBELS”
Term
treatment of cholinesterase inhibitors toxicity ?
Definition
Maintenance of vital signs

Decontamination

Atropine parenterally as needed to control signs of muscarinic excess
Term
examples of Direct acting Cholinomimetics ?
Definition
ACh (Miochol-E)
Bethanechol (Urecholine)
Carbachol (Miostat)
Cevimeline (Evoxac)
Pilocarpine (Isopto Carpine)
Varenicline (Chantix)
Term
examples of Cholinesterase Inhibitors ?
Definition
Ambenonium (Mytelase)
Donepezil (Aricept)
Echothiophate (Phospholine)
Edrophonium (Tensilon)
Galantamine (Reminyl)
Term
examples of
Definition
Neostigmine (Prostigmin)
Physostigmine
Pyridostigmine (Mestinon, Regonol)
Rivastigmine (Exelon)
Tacrine (Cognex)
Term
Cholinoceptor blocking agents block the effect of ?
Definition
parasympathetic activation
Term
examples of Antinicotinic drugs (Cholinoceptor blocking agents)?
Definition
Ganglion Blockers
Neuromuscular Blockers
Term
example of Antimuscarinic (anticholinergic)
/ Cholinoceptor blocking agents
Definition
atropine is the prototype
Term
examples of Muscarinic antagonists (Antimuscarinic Agents) ?
Definition
atropine and scopolamine
Term
atropine
Definition
Naturally occurring tertiary amine alkaloid esters
Atropa belladonna and Datura stramonium

Absorbed well from the gut and conjunctival membrane
Term
scopolamine
Definition
Hyoscyamus niger
Absorbed across the skin
Term
antimuscarinic agents -structure - tertiary amines ?
Definition
Useful in eye and CNS conditions
Similar structures
Antihistamines, antipsychotics, antidepressants
Term
antimuscarinic agents -structure - quaternary amines
Definition
More peripheral effects
Less CNS penetration
Term
atropine (Pharmacokinetics)
Definition
Distribution: CNS within 30 min to 1 hour
Metabolism: plasma half life of 2 hours
Excretion: 60% excreted unchanged
Effects on the iris and ciliary muscle persist for more than 72 hours
Term
Atropine (MOA)
Definition
Atropine causes reversible blockade
Binds to muscarinic receptor and prevents release of IP3 and inhibits adenylyl cyclase
Effect varies by tissue
Tissues most affected: salivary, bronchial, and sweat glands
Term
atropine (MOA)
Definition
Highly selective for muscarinic receptors

Lower potency at nicotinic receptors

Does not distinguish between M1 - M3

Other antimuscarinics are moderately selective for one of the receptor subgroups
Term
order of effects of increased dose of atropine
Definition
Decreased salivary and bronchial secretions

Decreased sweating

Pupil dilation and tachycardia

Inhibition of voiding

Decreased GI motility

Decreased gastric secretions
Term
CNS (atropine)- organ system effects
Definition
Minimal stimulant effects

Longer lasting sedative effect on the brain

One of the 1st drugs used for tremor of Parkinson’s
Term
CNS-scopolamine -organ system effects (atropine)
Definition
Prevents motion sickness of vestibular disturbances

Drowsiness and amnesia

Toxic doses – excitement, agitation, hallucinations, and coma
Term
Eye - Topical atropine -organ system effects (atropine)
Definition
blocks activation in pupillary constrictor muscle

Leads to unopposed sympathetic dilator activity and mydriasis

Weakens contraction of the ciliary muscle (cycloplegia)

Loss of ability to focus for near vision

Reduces lacrimal secretion
Term
Cardiovascular
SA node (organ system effects) (atropine)
Definition
very sensitive to blockade

Moderate to high doses of atropine cause tachycardia

Lower doses initially cause bradycardia
Term
cardiovascular- AV node- organ system effects (atropine)
Definition
blockade can reduce PR interval
Term
cardiovascular- ventricles- organ system effects (atropine)
Definition
intraventricular conduction block in toxic concentrations
Term
cardiovascular- blood vessels- organ system effects (atropine)
Definition
vasodilation can be blocked
Term
Respiratory System- organ system effects
(atropine)
Definition
Atropine can cause some bronchodilation and reduce secretion

Limited effectiveness in treating chronic obstructive pulmonary disease (COPD)

May be valuable in some asthma patients

Often used before administration of inhalant anesthetics to reduce the accumulation of secretions and the possibility of laryngospasm
Term
Gastrointestinal tract (organ system effects) (atropine)
Definition
Blocks motility (from stomach to colon) and some secretory functions

Blocks parasympathetic vagal nerve input
But GI function also controlled by local hormones and noncholinergic neurons

Blocks salivary gland leading to dry mouth

Reduction in gastric secretions

Little effect on pancreatic and intestinal secretions
Term
Genitourinary tract (organ system effects) (atropine)
Definition
Relaxes smooth muscle of ureters and bladder wall which slows voiding

Useful in treatment of spasm due to mild inflammation, surgery, and certain neurologic conditions

Urinary retention in males with prostatic hyperplasia

No significant effect on the uterus
Term
Sweat Glands- organ system effects -atropine
Definition
Atropine suppresses thermoregulatory sweating

Adults only affected when large doses used

Infants and children are more affected – “atropine fever”
Term
CNS Disorders (Therapeutic Applications) Parkinson’s disease
Definition
Adjunctive therapy in some patients
Term
CNS Disorders-Therapeutic Applications-Motion sickness
Definition
Vestibular disorders

Scopolamine for seasickness

Scopolamine patch can last 48-72 hrs but can cause sedation and dry mouth
Term
Ophthalmologic Disorders- Therapeutic Applications- Antimuscarinics useful in eye examinations
Definition
Help examine the retina
Use shorter acting drugs in adults and older children
Younger children may require atropine but the possibility of antimuscarinic poisoning is increased

Antimuscarinics should never be used for dilation unless cycloplegia or prolonged action is required

Prevent synechia formation in uveitis & iritis
Longer lasting agents are useful
Term
Ophthalmologic Disorders (atropine)
Definition
Atropine effects last 7-10 days

Cyclopentolate effects last 1 day

Tropicamide effects last 6 hours
Term
Atropine or scopolamine used preoperatively to decrease
Definition
airway secretions and decrease laryngospasms
Term
Scopolamine produced a postoperative ?
Definition
amnesia of the events

However they increased urinary retention & intestinal hypomotility
Term
is useful in asthma & COPD ?
Definition
ipratropium
Term
is useful to reduced incidence of COPD exacerbations ?
Definition
tiotropium

Longer bronchodilator action than ipratropium
Term
Cardiovascular Disorders- info!
Definition
Can overcome the depression of SA or AV node function that is due to reflex vagal discharge in an MI

Useful in blocking the parasympathetic actions in some people with idiopathic dilated cardiomyopathy
Due to antibody formation
Term
Gastrointestinal Disorders (Therapeutic Applications)
Definition
Used to treat traveler’s diarrhea and other mild self limited hypermotility conditions
Often combined with an opioid antidiarrheal drug
The antimuscarinic drug is mainly present to discourage abuse of the opioid agent
Term
Is Used to relieve bladder spasms after urologic surgery and Used to reduce involuntary voiding ?
Definition
oxybutynin
Term
Darifenacin & solifenacin
Definition
Greater selectivity for M3
Once daily dosing
Reduced incidence of xerostomia & constipation
Term
Is Used in adults with urinary incontinence and Reduced incidence of dry mouth ?
Definition
Tolterodine

M3 selective
Term
IS Used to reduce urinary incontinence in institutionalized elderly patients and Causes significant CNS toxicity ?
Definition
Imipramine

Tricyclic antidepressant with antimuscarinic actions
Term
Cholinergic Poisoning (antimuscarinic therapy)
Definition
Both nicotinic & muscarinic effects of cholinesterase inhibitors can be life threatening

To reverse muscarinic effects a tertiary amine must be used – atropine preferably

Use atropine for effects of organophosphate inhibitors, parathion, & chemical warfare nerve gas

Atropine sulfate 1-2 mg IV every 5-15 min until signs of reversal
Term
Cholinergic Poisoning (Cholinesterase regenerator compound)
Definition
Pralidoxime (PAM) & diacetylmonoxime (DAM) used for organophosphorus poisoning

Can hydrolyze the phosphorylated enzyme if the complex has not aged

Pralidoxime 1-2 g IV infusion over 15-30 min

Diacetylmonoxime crosses the BBB
Term
Cholinergic Poisoning (Mushroom poisoning)
Definition
Rapid onset within 15-30 min – nausea, vomiting, diarrhea, urinary urgency, vasodilation, reflex tachycardia (sometimes bradycardia), sweating, salivation, bronchoconstriction
Parenteral Atropine 1-2 mg

Delayed onset within 6-12 hrs – nausea, vomiting, hepatic injury, renal injury

Atropine has no value
Term
atropine adverse effects
Definition
Directed at one organ almost always induces undesirable effects in other organs

Atropine poisoning – dry mouth, mydriasis, tachycardia, hot & flushed skin, agitation, & delirium

“Dry as a bone, blind as a bat, red as a beet, and mad as a hatter”

Children and infants are very sensitive to the hyperthermic effects of atropine – death in doses as low as 2 mg
Term
Contraindications of Antimuscarinic drugs
Definition
contraindicated in pts with glaucoma

Elderly male pts use caution & avoid if pt has prostatic hyperplasia

Slows gastric emptying – increase gastric ulcer symptoms
Term
Ganglionic Blockade:
Non-depolarizing
Definition
Blockade can be overcome by increasing the concentration of an agonist
Term
Ganglionic Blockade:
depolarizing
Definition
Can be produced by nicotine and even ACh
Term
CNS
Mecamylamine (Ganglion Blocking Organ System Effect)
Definition
crosses BBB

Can cause sedation, tremor, choreiform movements, mental aberrations
Term
Eye
Ciliary muscle (Ganglion Blocking Organ System Effect)
Definition
cycloplegia with the loss of accommodation
Term
eye- pupil (Ganglion Blocking Organ System Effect)
Definition
hard to predict

Sympathetic innervation – pupillary dilation

Parasympathetic innervation – pupillary constriction

Ganglionic blockade often causes moderate dilation
Ganglionic blockade often causes moderate dilation
Term
CV
Blood vessels
(Ganglion Blocking Organ System Effect)
Definition
Decrease in arteriolar and venomotor tone leading to a fall in blood pressure

Hypotension in the upright position (orthostatic hypotension)
Term
CV- cardiac (Ganglion Blocking Organ System Effect)
Definition
Diminished contractility

Moderate tachycardia
Term
GI tract (Ganglion Blocking Organ System Effect)
Definition
Reduced secretions

Motility inhibited

Constipation
Term
GU (Ganglion Blocking Organ System Effect)
Definition
Urinary hesitancy

Urinary retention

Impaired erection

Impaired ejaculation
Term
Thermoregulatory sweating reduced (Ganglion Blocking Organ System Effect)
Definition
Hyperthermia usually not a concern due to cutaneous vasodilation
Term
examples of Antimuscarinic Anticholinergic Drugs ?
Definition
Atropine

Belladonna alkaloids

Dicyclomine (Bentyl)
Term
examples of Antimuscarinic Anticholinergic Drugs ?
Definition
Flavoxate (Urispas)

Glycopyrrolate (Robinul)

I-Hyoscyamine

Ipratropium (Atrovent)
Term
examples of Antimuscarinic Anticholinergic Drugs ?
Definition
Methscopolamine (Pamine)

Oxybutynin (Ditropan)

Scopolamine

Solifenacin (Vesicare)
Term
examples of Antimuscarinic Anticholinergic Drugs ?
Definition
Tiotropium (Spiriva)

Tolterodine (Detrol)

Trospium (Spasmex)
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