Autonomic Pharmacology Flashcards
fight, fright or flight sympathetic stimulation heart rate - \_\_\_\_\_\_\_ feel cold - shunt blood to \_\_\_\_\_\_ breathing - \_\_\_\_\_\_\_ of bronchi pupils \_\_\_\_\_ - enhance visual acuity \_\_\_\_ mouth mobilize body's stored \_\_\_\_\_\_\_ metabolic: \_\_\_\_\_\_\_ and increased \_\_\_\_ -blood vessels: \_\_\_\_\_\_ in skin/mucosa
increases muscles dilation dilate dry energy glycogenolysis BMR constriction
sympathetic nervous system
- ________, _______. ________ & _______
- catecholamines
- synthesized in _____ tissues
- stored in _______ vesicles
- epinephrine = _________
- secreted from ________
epinephrine, norepinephrine, serotonin, & dopamine neural synaptic adrenaline adrenal gland
adrenergic receptors receptors for epinephrine and norepinephrine two types of receptors: \_\_\_\_\_ \_\_\_ \_\_\_ - presynaptic
_____
__
__
what is an alpha 2 stimulant?? and what would it do
-used when beta blockers arent working
alpha a1 a2 beta b1 b2 clonidine decrease blood pressure
adrenergic agonists
agonists
-mimic the action of ___
-sympathomimetics
-stimulate \_\_\_\_\_\_\_ receptors clinical applications -shock - \_\_\_\_\_\_\_ -cardiovascular - \_\_\_\_\_\_\_\_; \_\_\_\_\_\_\_; \_\_\_\_; \_\_\_\_\_\_ -\_\_\_\_\_\_\_\_
NE adrenergic anaphylaxis bradycardia; hypotension; CHF; cardiac arrest asthma
adrenergic agonists two types: 1. catecholamines -\_\_\_\_\_\_\_, \_\_\_\_\_\_, \_\_\_\_\_\_ -\_\_\_\_\_\_\_ 2. noncatecholamines -\_\_\_\_\_\_\_ -\_\_\_\_\_\_\_\_\_(derivative of \_\_\_\_\_\_\_) - increase blood pressure -\_\_\_\_\_\_\_\_\_ (\_\_\_\_\_\_\_\_)
_______ is ephedrine which is a __ stimulant found in nasal passages which cause them to constrict
norepinephrine, epinephrine, dopamine serotonin ephedrine amphetamine ephedrine phenylephrine neo-synephrine
adrenergic agonists
- Catecholamines
- _________ is prototype
- drug of choice to relieve _______
- ________ edema in anaphylactic shock
- _______
- used in ________
- metabolized by BOTH _____ and ____
- not given PO: destroyed by __/__ enzymes
epinephrine bronchospasm laryngeal cardiac arrest hypovolemic shock COMT and MAO GI/Liver enzymes
adrenergic agonists
- non-catecholamines
- ______, ______, _______
- metabolized slowly by ___ and NOT inactivated by ____
- _____ half lives
- can be given _____
- crosses BBB - centrally _____
- ephedrine available ___
ephedrine, phenylephrine, terbutaline MAO, COMT longer orally active OTC
inactivating enzymes
- rapid metabolism by
- _______ (___)
- present in liver; intestinal and __synaptic nerve endings
- ______________ (___)
- present in liver; intestinal wall and ___synaptic nerve endings
- ORAL administration is _______ (enzyme present in intestinal wall)
- _______ requires slow infusion, subcutateous or intramuscular
monoamine oxidase (MAO) pre catechol-O-methyltransferase (COMT) post ineffective dopamine
adrenergic agonists: pharmacological actions -CNS: \_\_\_\_\_/\_\_\_\_\_/\_\_\_\_\_\_ -CVS: increased \_\_\_\_\_, increased \_\_\_ -vasoconstriction: \_\_\_\_\_\_\_ -eye: \_\_\_\_\_\_/decreased \_\_\_ respiratory: \_\_\_\_\_\_\_\_\_\_ metabolic: \_\_\_\_\_\_\_ and increased \_\_\_\_ blood vessels: constriction in \_\_\_\_/\_\_\_\_\_
excitement, stimulation, anxiety heart rate, BP epinephrine mydriasis, IOP bronchodilatation glycogenolysis, BMR skin, mucosa
adrenergic agonists - clinical uses
beta 1 receptor (heart)
clinical application - mainly on heart
-_______ - ______ to “kick start” a stopped heart, use when all other methods have failed
-____ failure - b1 receptor activation results in a positive _____ effect (force of contraction); thus improved cardiac performance
- shock (profound ________; tissue ______)
-may cause ________ (excessive heart rate)
-may cause _______ (irregular heartbeat
cardiac arrest epinephrine heart failure inotropic hypotension, perfusion tachycardia dysrrythmias
adrenergic agonist - clinical uses beta 2 receptor (lungs & uterus) -activated by -\_\_\_\_\_\_; albuterol (\_\_\_\_\_\_\_) clinical application -asthma - \_\_\_\_\_\_\_ - \_\_\_\_\_\_ (\_\_\_\_\_\_): drug of choice for asthma delay \_\_\_\_\_ labor -b2 receptor activation relaxes uterine smooth muscle (\_\_\_\_\_\_\_)
epinephrine selective agonist bronchodilatation albuterol, ventolin preterm isoproterenol
pharmacological effects
cardiovascular system - heart
-mainly __ receptors, some __ and _ effects
beta receptor activation
-increased ______ influx in cardiac cells
-increased _______ activity, positive ______ effect
-increased in conduction velocity in __ node, positive ______ effect
-increased ______ contractility, positive _____ effect
b1, b2, a calcium pacemaker, chronotropic AV Dromotropic intrinsic lnotropic
pharmacological effects
eye
-__ receptors activate _________ dilator muscles of the iris
-receptor activation causes _______
-_ agonists increase the outflow of _________ from the eye
-__ antagonists decrease the production of aqueous uhmor
a radial pupillary mydriasis aqueous humor b
pharmalogical effects
respiratory tract
-__ receptors on bronchial smooth muscle
-activation cause _______
-__ agonists: _______ (ventolin)
-upper resp tract mucosa contain ___ receptors
-stimulation causes _______ action of ______
b2 relaxation b albuterol a1 decongestant andrenoceptors
pharmalogical effects
gastrointestinal tract
b receptors - activation causes relaxation via _______ and decreased ____ activity in these cells
a2- selective agonists
-decrease muscle activity _____ by reducing the release of _______ and possibly other stimulants in the GIT
hyperpolarization
spike
indirectly
acetylcholine
exocrine glands
- salivary glands contains _____ that regulate the secretion of _____ and ___
- decreased _______/_____
- _______ sweat glands respond to adrenoceptor stimulants with _____ sweat production
adrenoceptors amylase, water salivation/xerostomia apocrine increased
pharmacologic
metabolic effects
-adipose cells
- __ adrenoceptor activation increases ____
-increased __________
liver
-________ drugs enhance _______, leading to increased glucose release into the circulation - mainly via __ receptors
B, lipolysis gluconeogenesis sympathoimetic glycogenolysis B
USES of adrenergic agonists anaphylactic shock -severe allergy; type I anaphylaxis clinical signs -\_\_\_\_\_\_\_ (widespread vasodilation) -\_\_\_\_\_\_\_\_ & \_\_\_\_\_ of glottis emergency management -\_\_\_\_\_\_\_\_ (subcutaneous, IM) just get it in! -\_\_: increase CO, elevate BP -\_\_: vasoconstriction leading to an increase in \_\_ & suppress \_\_\_\_ -\_\_: bronchodilatation
hypotension bronchoconstriction, edema epinephrine beta 1 alpha 1 BP, edema b2
adrenergic receptor activation mechanisms
- _________
adrenergic agonists
__________
isoproterenol - promote ___ release
- _______
3. \_\_\_\_\_\_\_\_ cocaine tricyclic antidepressants imipramine (Tofranil) amitryptline (Elavil) doxepin ( Sinequan)
- _________
____ inhibitors
- phenelzine (Naril)
- trancyclpromine (parcate
2 3 AND 4 ARE INDIRECT ACTING ADRENERGIC AGONISTS
adrenergic agonists epinephrine isoproterenol NE amphetamines inhibit NE reuptake inhibit NE activation MAO
adrenergic antagonists -drugs that block \_\_\_\_\_\_ receptors -two groups alpha adrenergic blocking agents -non-selective: block a1 and a2 (\_\_\_\_\_\_\_\_\_, \_\_\_\_\_\_\_\_\_) selective: block \_\_ only (\_\_\_\_\_, \_\_\_\_\_\_) beta-adrenergic blocking agents -non-selective: block b1 and b2 (\_\_\_\_\_\_\_\_\_) selective blocks \_\_ only (\_\_\_\_\_\_\_)
adrenergic phentolamine, phenoxybenzamine a1 prazosin, terazosin propranolol b1 atenolol
alpha (a) adrenergic antagonists
- blood vessel (______)
- essential hypertension: lowers blood pressure via massive _________
__________
- catecholamine secreting tumor in the adrenal _______
- in patients with very hypertensive crisis or malignant hypertension (bloodpressure > 180/120 mm Hg)
vasodilation
vasodilation
pheocromocytoma
medulla
alpha adrenergic antagonists
Raynaud’s disease
-_____ induced disease (_______)
-peripheral vascular disorder, ______ in ___ & _____
smoking, nicotine
vasospasm
toes, fingers
alpha 1 antagonists
________ (minipress)
-competitive a1 antagonist (selective)
indication - ______
other a1 antagonists
- _______ (Hytrin)
- ______ (Regitine)
- _________ (Dibenzyline)
Prazosin hypertension Terazosin Phentolamine Phenoxybenzamine
Beta Blockers
- competitively block receptors in autonomic nervous system
- their names end in __
- beta stimulation produces ________, ________ and ______: beta blockers reverse these effecs
- effects: initially _______ followed by ______, ____ and _______
- ______, ______, ________
olol vasoconstriction, bronchodilation, tachycardia vasoconstriction vasodilation bradycardia bronchoconstriction propanolol, atenolol, metoprolol
beta blockers
- b1 blockage of cardiac tissue results in
-_______ heart rate
-reduced force of _______
-reduced _______ of impulse conduction via ___ node
thus reduced _______
-b2 antagonists
-b2 blockage causes _________
minimal clinical uses
decreased contraction velocity AV cardiac workload bronchospasm
b1 adrenergic antagonists clinical application of b1 blockage - \_\_\_\_\_\_\_\_ -\_\_\_\_\_\_ -\_\_\_\_\_\_ -\_\_\_\_\_ -\_\_\_\_\_\_
heart failure hyperthyroidism migraine stage fright glaucoma
autonomic nervous system parasympathetic -decreased \_\_\_\_\_\_\_\_\_ - fall in \_\_\_\_\_\_ -constriction of the \_\_\_\_\_ (miosis) -contraction of the \_\_\_ -watery secretion of \_\_\_\_\_ neurotransmitter
heart rate blood pressure pupil GIT saliva
synthesis and storage
-ACh is synthesized from ______ and _____
via __________ (CAT)
-ACh sythensis is a rapid process
-synthesized ACh is transported into vesicles by a transporter
-metabolized by _________ (____)
acetyl Co A - synthesized in the _______
choline - transported from ___ into nerve terminal, by a transporter (carrier)
Acetyl-Co-A choline choline acetyl transferase cholinesterase enzyme (AChE) mitochondria ECF
acetylcholine
effects:
-heart: negative _____ and negative ______ effect. Decrease in ______
-blood vessels: ________ of smooth muscle, ______
-bronchi: _______, ________
GIT: increased ____, _____ and ______
EYE: ____ and ____. decreases ___
inotropic chronotropic cardiac output relaxation vasodilation bronchoconstriction, bronchospasm motility, contraction, secretion miosis, cycloplegia IOP
cholinergic receptors
-receptors for acetylcholine have 2 subtypes
_________ (M) - __________ (Amanita muscaria)
________ (N) - ______ in tobacco
muscarinic
poisonous mushroom
nicotinic
nicotine
cholinergics
classified as:
-directly acting - act directly on receptor - ______-
-indirectly acting - act by inhibiting the destruction of Ach by ________
further divided into
reversible: ________
irreversible: ________
pilocarpine
cholinesterase
neostigmine
organophosphates
cholinergics direct 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 bladde,r GI tract pilocarpine Salogen
anticholinergics -prevent action of \_\_\_\_\_\_\_\_ -\_\_\_\_\_\_ is not affected -receptor is competitively blocked -anticholinergics only block \_\_\_\_\_\_\_ action ... no effect of nicotinic -action blocked: \_\_\_\_\_\_, \_\_\_\_, \_\_\_\_\_\_
acetylcholine
release
muscarinic
smooth muscles, glands, heart
belladonna alkaloids plant sources: \_\_\_\_\_\_\_\_ atropa bella donna means beautiful lady; \_\_\_\_\_\_\_\_\_\_ examples 1 2
atropine
pupillary dilation
scopolamine
atropine
anticholinergics atropine and scopolomine (given \_\_\_\_\_\_\_ or \_\_\_\_\_\_\_) -\_\_\_\_\_\_\_\_ (Atrovent inhaler/oral) -\_\_\_\_\_\_\_\_ (spiriva)
orally, topical
Ipratropium
tiotropium
anticholinergics Pharmacologic effects -decreased \_\_\_\_\_\_\_ -smooth muscles: \_\_\_\_\_\_ -\_\_\_\_\_\_\_\_ and \_\_\_\_\_\_\_ -eye: \_\_\_\_\_\_ and \_\_\_\_\_\_\_ -CVS: positive \_\_\_\_\_\_ and \_\_\_\_\_\_\_ effectts result in tachycardia
secretions relaxed bronchodilation, constipation mydriasis, cycloplegia inotropic, chronotropic
atropine & scopolamine GI effects -secretions: decrease \_\_\_\_\_\_\_ -relax GI muscle except \_\_\_\_\_ and reduce intestinal \_\_\_\_ -decrease \_\_\_\_\_\_ secretion
urinary tract effects
-inhibit the contractility of the urinary bladder and may cause ______ retention
salivation sphincters motility gastric acid urinary
adverse effects atropine & scopolomine extensions of the phrmacological effects -blurred vision (\_\_\_\_\_) -photophobia (\_\_\_\_\_\_) -xerostomia (\_\_\_\_\_\_) -\_\_\_\_\_\_\_ -\_\_\_\_\_\_\_\_\_ retention
cycloplegia mydriasis dry mouth tachycardia urinary/gi
atropine & scopolomine
contraindications
-_____: increased IOP in glaucoma
-prostatic hypertrophy (BPH): urinary ______
intestinal or urinary obstruction: _______ risk
-cardiovascular diseases: ______/______
glaucoma
retention
perforation
tachycardia, arrythmias
atropine & scopolomine
-respiratory: relax bronchi - therefore used in ________
CNS effects
-_____: causes milkd stimulation followed y slower and longer-lasting sedative effects (CNS depression)
scopolomine is more ____ than atropine
uses: ____________ patches - prevent motion sickness (Transderm V)
asthma
atropine
sedating
transdermal scolopamine patches
atropine & scopolomine
pre-operative medication: to decrease ____, ___ secretions
-GIT disorders: _____ and increased _____: Ulcers/Traveler’s diarrhea
-Irritable Bowel syndrome: ___________
-Eye exams: ______ measurements
-Motion sickness: ________
-post prostatectomy bladder spasm/ involuntary voiding: _______(_____)
bronchial, GIT hyperacidity motility dicyclonine refractive scopolomine oxybutynin (ditropan)
nicotine preparations nicotine inhaler: \_\_\_\_\_\_\_ (nasal) nicotine chewing gum - \_\_\_\_\_\_\_\_ -\_\_\_\_\_\_ (Varenicline) -Nicotine transdermal - \_\_\_\_\_\_\_
nicotrol
nicorette
champix
nicoderm
