Autonomic Pharmacology Flashcards
1
Q
fight, fright or flight sympathetic stimulation: -heart rate: \_\_\_\_\_ -feel cold: shunt blood to \_\_\_\_\_ -breathing: \_\_\_\_\_ of \_\_\_\_\_ -pupils dilate: \_\_\_\_\_ visual acuity -\_\_\_\_\_ mouth -mobilize bodys stored \_\_\_\_\_ -metabolic: \_\_\_\_\_ and increased \_\_\_\_\_ -blood vessels: constriction in \_\_\_\_\_/\_\_\_\_\_
A
increases muscles dilation bronchi enhance dry energy glycogenolysis BMR skin/mucosa
2
Q
sympathetic nervous system
- _____, _____, _____ and _____
- catecholamines
- synthesized in _____
- stored in _____
- epinephrine = _____
- secreted from _____
A
epinephrine norepinephrine serotonin dopamine neural tissues synaptic vesicles adrenaline adrenal glands
3
Q
adrenergic receptors -receptors for epinephrine and norepinephrine -two types of receptors: alpha: -\_\_\_\_\_ -\_\_\_\_\_: \_\_\_\_\_
beta
- _____
- _____
A
a1 a2 presynaptic b1 b2
4
Q
adrenergic agonists
- agonists
- -mimic the acton of _____
- -_____/_____/_____
- stimulate _____ receptors
- clinical applications:
- -cardiovascular - _____, _____, _____, _____
- -_____
- -_____
- -shock - _____
A
epinephrine sympathomimetics adrenergics sympathetics adrenergic bradycardia hypotension CHF cardiac arrest asthma allergy anaphylaxis
5
Q
adrenergic agonists
- two types:
- -catecholamines
- –_____, _____, _____
- –_____
- -noncatecholamines
- –_____
- –_____ (derivative of Ephedrine)
- –_____ (neo-synephrine)
A
norepinephrine epinephrine dopamine serotonin ephedrine amphetamine phenylephrine
6
Q
adrenergic agonists
- catecholamines
- _____ is a prototype
- drug of choice to relieve _____
- _____ edema in anaphylactic shock
- _____
- used in _____ shock
- metabolized by both COMT (_____) and MAO (_____)
- not given _____: destroyed by _____ enzymes
A
epinephrine bronchospasm laryngeal cardiac arrest hypovolemic catechol-O-methyl transferase monoamine oxidase PO GI/Liver
7
Q
adrenergic agonists 2. non-catecholamines -\_\_\_\_\_, \_\_\_\_\_, \_\_\_\_\_ -metabolized slowly by \_\_\_\_\_ and NOT inactivated by \_\_\_\_\_ -\_\_\_\_\_ half-lives -can be given \_\_\_\_\_ -crosses \_\_\_\_\_: \_\_\_\_\_ active \_\_\_\_\_ available OTC
A
ephedrine phenylephrine terbutaline MAO COMT longer orally BBB centrally ephedrine
8
Q
inactivating enzymes
- rapid metabolism by:
- -monoamine oxidase (MAO)
- –present in _____; intestinal wall and _____ nerve endings
- -catechol-O-methyltransferase (COMT)
- –present in _____; intestinal wall and _____ nerve endings
–_____ administration of catecholamines is ineffective (enzyme present in _____)
A
liver presynaptic liver postsynaptic ORAL intestinal wall
9
Q
adrenergic agonists: pharmacological actions
- CNS: _____/stimulation/_____
- CVS: _____ heart rate, _____ BP
- vasoconstriction: _____
- eye: _____/ _____IOP
- respiratory: _____
- metabolic: _____ and increased _____
- blood vessels: constriction in _____/_____
A
excitement anxiety increased increased epinephrine mydriasis decreased bronchodilation glycogenolysis BMR skin muscosa
10
Q
adrenergic agonists- clinical uses beta 1 receptor (\_\_\_\_\_) -clinical application - mainly on \_\_\_\_\_ --cardiac arrest - \_\_\_\_\_ to "kick start" a stopped heart, use when all other methods have failed --heart failure - \_\_\_\_\_ receptor activation results in a positive \_\_\_\_\_ (force of contraction); thus improved cardiac performance --shock (profound \_\_\_\_\_; tissue \_\_\_\_\_) --may cause \_\_\_\_\_ (excessive heart rate) --may cause \_\_\_\_\_ (irregular heartbeat)
A
heart heart epinephrine b1 inotropic effect hypotension perfusion tachycardia dysrrhythmias
11
Q
adrenergic agonist - clinical uses
- beta 2 receptor (_____ and _____)
- -activated by:
- –_____; _____ (selective agonist)
- -clinical application
- –asthma - _____
- —_____ (_____): drug of choice for asthma
- –delay preterm labor
- —_____ receptor activation relaxes _____ smooth muscle (_____)
A
lungs uterus epinephrine albuterol bronchodilatation albuterol ventolin B2 uterine isoproterenol
12
Q
pharmacological effects of adrenergic agonists
cardiovascular system- heart
-mainly _____ receptors, some beta 2 and a effects
-beta receptor activation
–increased _____ influx in _____ cells
-increased _____ activity, positive _____ effect
-increased in conduction velocity in _____, positive _____ effect
-increase _____, positive _____ effect
A
beta 1 calcium cardiac pacemaker chronotropic AV node dromotropic intrinsic contractility inotropic
13
Q
pharmacological effects
eye
-_____ receptors activate radial pupillary dilator muscle of the _____
-receptor activation causes _____
-_____ increase the outflow of _____ from the eye
-_____ decrease the production of aqueous humor
A
alpha iris mydriasis alpha agonists aqueous humor beta antagonists
14
Q
pharmacological effects
respiratory tract
-_____ receptors on _____ smooth muscle
-activation causes _____
-beta agonists: _____ (_____)
-upper respiratory tract mucosa contain _____ receptors
-stimulation causes decongestant action of _____: _____ (_____)
A
beta 2 bronchial relaxation albuterol ventolin alpha 1 adrenoceptors pseudoephedrine sudafed
15
Q
pharmacological effect
gastrointestinal tract
-beta receptors
–activation cause relaxation via _____ and _____ spike activity in these cells
- alpha 2- selective agonists
- -decrease muscle activity indirectly by reducing the release of _____ and possibly other _____ in the _____
A
hyperpolarization decreased acetylcholine stimulants GIT
16
Q
pharmacological effects
exocrine glands
-salivary glands contain _____ that regulate the secretion of _____ and _____
-decreased _____/_____
-apocrine swear glands respond to adrenoceptor stimulants with increased _____
A
adrenoceptors amylase water salivation xerostomia sweat production
17
Q
pharmacological effects metabolic effects -adipose cells --\_\_\_\_\_ activation increases \_\_\_\_\_ --increased \_\_\_\_\_
- liver
- -sympathomimetic drugs enhance _____, leading to increased _____ release into the circulation- mainly via _____ receptors
A
B adrenoceptor lipolysis gluconeogenesis glycogenolysis glucose B
18
Q
uses of adrenergic agonists anaphylactic shock -severe allergy; \_\_\_\_\_ --clinical signs: --\_\_\_\_\_ (widespread \_\_\_\_\_) --\_\_\_\_\_ and edema of \_\_\_\_\_
- -emergency management
- –_____ (_____, _____) just get it in!
- —beta 1: increase _____, elevate _____
- —alpha 1: _____ leading to an increase in _____ and suppress _____
- —beta 2: _____
A
type 1 anaphylaxis hypotension vasodilation bronchoconstriction glottis epinephrine subcutaneous IM CO BP vasoconstriction BP edema bronchodilation
19
Q
adrenergic receptor activation: four mechanisms
- direct-acting adrenergic agonists
- _____
- _____ - promote NE release
- _____
3. inhibit NE reuptake cocaine tricyclic antidepressants -\_\_\_\_\_ (Tofranil) -\_\_\_\_\_ (Elavil) -\_\_\_\_\_ (Sinequan)
- inhibit NE inactivation
MAO inhibitors
-_____ (Naril)
-_____ (parcate)
A
epinephrine isoproterenol amphetamines imipramine amitryptyline doxepin phenelzine tranylcypromine
20
Q
adrenergic antagonists
- drugs that block _____ receptors
- two groups
- -alpha-adrenergic blocking agents
- –non-selective: block _____ and _____ (_____, _____)
- –selective: block alpha 1 only (_____, _____)
- -beta-adrenergic blocking agents
- –non-selective; block _____ and _____ (_____)
- –selective blocks beta 1 only (_____)
A
adrenergic alpha 1 alpha 2 phentolamine phenoxybenzamine prazosin terazosin beta 1 beta 2 propranolol atenolol
21
Q
alpha adrenergic antagonists
- blood vessel (_____)
- -_____: lowers blood pressure via massive vasodilation
- -pheochromocytoma
- –_____ secreting tumor in the _____
- –in patients with very hypertensive crisis or malignant hypertension (Blood pressure > _____ Hg)
A
vasodilation essential hypertension catecholamine adrenal medulla 180/120
22
Q
alpha adrenergic antagonists
Raynaud’s disease
-_____ induced disease (nicotine)
-_____ disorder, _____ in toes and fingers
A
smoking
peripheral vascular
vasospasm
23
Q
alpha 1 antagonists
- _____ (minipress)
- -competitive antagonist (_____)
- -indication - _____
- other a1 antagonists
- -_____ (Hytrin)
- -_____ (regitine)
- -_____ (dibenzyline)
A
prazosin selective hypertension terazosin phentolamine phenoxybenzamine
24
Q
beta blockers
- beta blockers competitively block receptors in the _____
- their names end in _____
- beta stimulation produces _____, _____, and _____: beta blockers reverse these effects
- effects: initially _____ followed by _____, _____ and _____
- _____, _____, _____
A
autonomic nervous system -olol vasoconstriction bronchodilation tachycardia vasoconstriction vasodilation bradycardia bronchoconstriction propranolol atenolol metoprolol
25
beta blockers
- beta 1 blockage of cardiac tissue results in
- decreased _____
- reduced force of _____
- reduced velocity of impulse conduction via _____
- thus reduced _____
- beta 2 antagonists
- -beta 2 blockage causes _____
- -minimal clinical uses
```
heart rate
contraction
AV node
cardiac workload
bronchospasm
```
26
```
beta adrenergic antagonists
clinical application of beta 1 blockage
--_____ failure
--_____
--_____
--_____
--_____
```
```
heart
hyperthyroidism
migraine
stage fright
glaucoma
```
27
atropine
blind as a bat
-_____, _____
dry as a bone
-_____ of secretions
hot as hell
-no sweat _____ action
mad as a hatter
-_____ confusion, _____, _____
red as a beet
-_____, _____
```
mydriasis
cycloplegia
drying
CNS
CNS
hallucination
mania
flushing
vasodilation
```
28
```
Autonomic nervous system
parasympathetic
-decreased _____
-fall in _____
-constriction of the pupil (_____)
-contraction of the _____
-watery secretion of _____
-neurotransmitter?
```
```
heart rate
blood pressure
miosis
GIT
saliva
```
29
synthesis and storage
- ACh is synthesized from _____ and _____
- via _____ (CAT)
- ACh synthesis is a _____ process
- synthesized ACh is transported into _____ by a transporter
- metabolized by _____ (AChE)
- acetyl-co-a: synthesized in _____
- choline: transported from _____ into _____ by a transporter (carrier)
```
acetyl-co-a
choline
choline acetyl transferase
rapid
vesicles
cholinesterase enzyme
mitochondria
extra-cellular fluid
nerve terminal
```
30
acetylcholine
effects:
-heart: negative _____ and negative _____ effect. decrease in _____ output
-blood vessels: relaxation of _____. _____
-bronchi: _____, _____
-GIT: increased _____, _____ and secretion
-eye: _____ and _____. decreases IOP
```
inotropic
chronotropic
cardiac
smooth muscle
vasodilation
bronchoconstriction
bronchospasm
motility
contraction
miosis
cycloplegia
```
31
cholinergic receptors
- receptors for acetylcholine have 2 subtypes:
- _____ (M): poisonous mushrooms (_____)
- _____ (N): nicotine in tobacco
muscarinic
amanita muscaria
nicotinic
32
```
cholinergics:
classified as:
-_____- act directly on receptor: _____
-_____ - act by inhibiting the destruction of Ach by _____
-further divided into:
--reversible: _____
--irreversible: _____
```
```
directly acting
pilocarpine
indirectly acting
cholinesterase
neostigmine
organophosphates
```
33
```
cholinergics
diret acting:
-_____ (used for urinary retention)
-causes contraction of _____
-should not be used in patients with mechanical obstruction of the _____ or _____
-_____ (used for glaucoma)
```
```
bethanechol
bladder
bladder
GIT
pilocarpine
```
34
pilocarpine (_____)
- pilocarpine: used for _____
- decreases outflow resistance and therefore helps in decreasing _____ (_____)
- adverse effects:
- -_____, _____, _____, _____, _____, _____
- contraindications: patients with uncontrolled or poorly controlled _____
- also used for _____/stimulation
- _____ syndrome / _____ cancers
```
salagen
glaucoma
IOP
intra ocular pressure
sweating
nausea
chills
flushing
urinary frequency
dizziness
asthma
salivary production
sjorgen's
H and N
```
35
```
adverse effects of cholinergic:
extension of pharmacological effects
-_____
-_____/_____
-_____
-_____
-_____
-CNS symptoms: confusion, _____
```
```
bronchospasm
salivation
drooling
lacrimation
urination
defecation
coma
```
36
anticholinergics
- prevent action of _____
- _____ is not affected
- receptor is _____
- anticholinergics only block _____ action... no effect of _____
- action blocked: smooth muscles, _____, _____
```
acetylcholine
release
competitively blocked
muscarinic
nicotinic
glands
heart
```
37
belladonna alkaloids
- plant sources: _____
- atropa 'belladonna' (deadly _____)
- -"beautiful lady"; _____
- examples:
- -_____
- -_____
```
atropine
nightshade
pupillary dilatation
atropine
scopolamine
```
38
anticholinergics
- atropine and scopolamine (given _____ or _____)
- ipratropium (_____/_____)
- tiotropium (_____)
```
orally
topical
atrovent inhaler
oral
spiriva
```
39
pharmacological effects of anticholinergics:
- decreased _____
- smooth muscles: _____
- _____ and _____
- eye: _____ and _____
- CVS: positive _____ and _____ effects result in _____
```
secretions
relaxed
bronchodilation
constipation
mydriasis
cycloplegia
inotropic
chronotropic
tachycardia
```
40
```
atropine and scopolamine
GI effects:
-secretions: decrease _____
-relax GI muscle except _____ and reduce _____
-decrease _____ secretion
```
urinary tract effects:
-inhibit the contractility of the _____ and may cause urinary _____
```
salivation
sphincters
intestinal motility
gastric acid
urinary bladder
retention
```
41
atropine and scopolamine
-respiratory: relax _____- therefore used in _____
CNS effects:
- atropine: causes mild stimulation followed by slower and longer-lasting _____ effects (CNS _____)
- scopolamine is more _____ than atropine
- uses: _____ - prevent motion sickness (transderm V)
```
bronchi
asthma
sedative
depression
sedating
transdermal scopolamine patches
```
42
```
adverse effects of anticholinergics:
extensions of the pharmacological effects
-blurred vision (_____)
-_____ (mydriasis)
-_____ (dry mouth)
-_____
-_____/_____ retention
```
```
cycloplegia
photophobia
xerostomia
tachycardia
urinary
GI
```
43
contradictions of anticholinergics
- glaucoma: increased _____ in glaucoma
- prostatic hypertrophy (BPH): _____ retention
- intestinal or urinary obstruction: _____ risk
- cardiovascular disease: _____/_____
```
IOP
urinary
perforation
tachycardia
arrhythmias
```
44
uses of anticholinergics
- pre-operative medication: to decrease _____, _____ secretions
- GIT disorders: _____ and increased _____ : _____/Travelers _____
- IBS: _____
- eye exams: refractive measurements
- motion sickness: _____
- post prostatectomy bladder spasm/ involuntary voiding: _____ (ditropan)
```
bronchial
GIT
hyperacidity
motility
diarrhea
dicyclonine
scopolamine
oxybutynin
```
45
nicotine preparations
- nicotine inhaler:
- -_____ (nasal)
- nicotine chewing gum:
- -_____
- _____ (varenicline)
- nicotine transdermal: _____
nicotrol
nicorette
champix
nicoderm
