Term
|
Definition
| -B1 receptors increase heart rate (SA and AV nodes) and contractility (myocardial cells) |
|
|
Term
| why a1 receptors predominates? |
|
Definition
|
|
Term
|
Definition
-decreased BP
-Baro Rs detect
-*increase SNS/decrease PSNS
-SNS stimulates adrenal medulla
-increases HR and stroke volume
-increases BP
-reflex tachycardia |
|
|
Term
|
Definition
-cardiac output
-total peripheral resistance |
|
|
Term
|
Definition
|
|
Term
|
Definition
-mydriasis (pupil dilation)
-contraction of iris radial smooth muscle
(dilator pupillae)(a1)
-effects on aqueous humor |
|
|
Term
| ocular effects (aqueous humor) |
|
Definition
-direct increase in production by B1
-direct decrease in production by a2
-indirect decrease in production by a2 and a1 |
|
|
Term
|
Definition
-bronchodilation (B2)
-inhibition of inflammatory mediator release from mast cells (B2)
-decreased bronchial gland secretions (a1)
-vasoconstriction in upper resp. tract muscosa (a1) |
|
|
Term
|
Definition
-glycogenolysis occurs in liver, skeletal muscle, heart, and adipose cells (B1,B3)
-inhibition of insulin secretion (a2)
-stimulation of glucagon secretion (B2) |
|
|
Term
|
Definition
-direct sympathetic innervation to prostate
-position of prostate can put pressure on urethra
-urinary retention
-frequency and urgency
-prostate expresses a1
-a1 stimulation results in contraction |
|
|
Term
| more genitourinary effect |
|
Definition
-a1 receptors cause vasoconstriction
-b2 receptors are in detrusor muscle and cause relaxation
-alpha effect dominates over PSNS response |
|
|
Term
|
Definition
-most important during pregnancy
-a1 activation leads to contraction
-B2 activation leads to relaxation |
|
|
Term
|
Definition
-coupled to Gq
-a1a,a1b,a1d
-primarily on smooth muscle
-GI tract
-pilomotor smooth muscle
-peripheral vasculature
-VASOCONSTRICTION
-MYDRIASIS |
|
|
Term
|
Definition
-activate Gi (decrease Ca, increase K, decreased NE release)
-both pre and post synaptic |
|
|
Term
|
Definition
-couple to Gs
-located primarily in HEART and kidney
-stimulate renin release in kidney
-increase inotropy (contractility) and chronotropy (HR)
-both effects increase CARDIAC OUTPUT |
|
|
Term
|
Definition
-couple to Gs
-located in lungs, vasculature, smooht muscle, and liver
-brochodilation
-vasodilation (skeletal muscle and coronary blood vessels)
-increases glycogenolysis |
|
|
Term
|
Definition
-H bonding
-rapidly metabolized by COMT
-ionized at physiological pH |
|
|
Term
|
Definition
| -substitution on amino nitrogen increases B selectivity |
|
|
Term
|
Definition
| -substitution of 2 methyl groups on amino nitrogen |
|
|
Term
|
Definition
| -mimic effects of transmitter substances in SNS |
|
|
Term
|
Definition
-indirect sympathomimetics
-diastereomer of ephedrine
-does not cross BBB as good as ephedrine
-nasal decongestant |
|
|
Term
| norepinephrine (levophed) |
|
Definition
-a1 agonists, weaker b1 agonist
-vasoconstriction
-reflex bradycardia (decreased HR)
-IV only
- |
|
|
Term
| Epinephrine (adrenalin chloride, sus-phrine) |
|
Definition
-a1,a2,b1,b2 agonist
-dose is important
-IV,inhalation,IM
-used for shock,asthma
-important to note if patient is on any adrenergic blockers |
|
|
Term
| *Phenylephrine (Neo-Synephrine) |
|
Definition
-*rebound congestion is common if used beyond 3 days
-OTC nasal decongestant
-induces mydriasis
-constrict blood vessels in blood shot eyes |
|
|
Term
| *Oxymetazoline (Afrin,Dristan,Sinex) |
|
Definition
-a1 and a2
-vasoconstriction
-nasal spray
-used during surgery |
|
|
Term
| tetrahydrolizine (visine) |
|
Definition
-vasoconstriction
-OTC eye drops and nasal spray |
|
|
Term
| direct acting sympathomimetics |
|
Definition
-NE
-Epi
-Phenyephrine
-Oxymetazoline
-Tetrahydrolizine |
|
|
Term
|
Definition
-Dobutamine
-Dopamine
-Albuterol
-Salmeterol
-Formoterol |
|
|
Term
|
Definition
-B1 activity
-racemate used clinically
-heart surgery, CHF, acute MI
-(+) a1 antagonist,potent at B1
-(-) a1 agonist
-stereochem affects EFFICACY not AFFINITY |
|
|
Term
|
Definition
-CNS actions
-*dilate renal blood vessels thru D1 Rs
-stimulate B1 Rs
-*IV only
-*shock,MI,trauma, CHF
-substrate for MOA |
|
|
Term
| Albuterol (Proventil,Ventolin) |
|
Definition
-oral or inhalation
-bronchospasm
-rapid acting 15 min
-oral can delay preterm labor bc B2 agonist
-side effect: jittery |
|
|
Term
|
Definition
-maintenance therapy for asthma
-slow onset, long duration bc lipophilic tail embeds in membrane
-component of advair
-more B2 selective than albuterol |
|
|
Term
|
Definition
-onset 3 mins, 12 hour duration
-boxed warning - increase risk of asthma related death |
|
|
Term
|
Definition
|
|
Term
| indirect sympatholytics (a2) |
|
Definition
-Clonidine
-Apraclonidine/Brimonidine
-Methyldopa |
|
|
Term
|
Definition
-*Tx for hypertension, opiate withdrawal
-oral or transdermal patch
-*side effects-dry mouth (a2 receptors in salivary glands), bradycardia, drowsiness
-with chlorthalidone-Combipres |
|
|
Term
| Apraclonidine and Brimonidine |
|
Definition
-Tx glaucoma
-topical but can be detected in plasma
-little effect on BP
-Brimonidine more a2 selective, can cross BBB |
|
|
Term
|
Definition
-active form is methyl-NE
-hypertension during pregnancy
-SE-hemolytic anemia |
|
|
Term
|
Definition
-nonselective and subtype selective
-chemically heterogenous-many different types of structures
-therapeutic uses-pheochromocytoma,HT,BPH |
|
|
Term
|
Definition
-Phentolamine
-Prazosin
-Doxazosin
-Terazosin
-Tamsulin |
|
|
Term
|
Definition
-reversible,*nonselective
-imidazoline-compare structure to clonidine
-stimulate GI smooth muscle-blocked by atropine
-Tx pheochromocytoma
-HT crisis |
|
|
Term
|
Definition
-binds all a1 subtypes
-does not increase HR
-may depress baroreceptor reflex
-decreases LDL and increases HDL
-orthostatic hypotension
-*1st dose given at bedtime
-short duration of action
-*no drowsiness or decreased HR |
|
|
Term
|
Definition
0same a prazosin
-but long duration of action allowing once a day dosing |
|
|
Term
|
Definition
-a1a selective
-Tx BPH
-little effect on BP
-once a day dosing
-side effect is abnormal ejaculation |
|
|
