Adrenergic drugs

epinephrine

a1,2,b1,b2 (B's MORE)

NE

a1,2 (b1 MOST)

isoproternol

b1,b2

oxymetazoline

a1,a2

terbutaline
albuterol
salmerterol

b2

dobutamin

b1

clonidine
apraclonidine

a2

phenylephrine

a1

release agents

amphetamine
tyramine

uptake inhibitor

cocaine

mao/comt inhibitor

paragyline
entacapone

mix-acting

ephedeine
all of the receptors + Releasing agent

dopamine

D1, d2

b1,b2,b3 mechanism?

gs (cAMP increase)
L type ca+2 channels

a1 mechanism

Gq (phospolipase C, Ca+2 channels)

a2 mechanism

Gi (cAMP decrease, K+ increase, PLC incease)

EPI pharmokinetics

0% oral bioavail
no CNS
metabolized by liver (MAO/COMT)
2 min t1/2
IM faster absorbtion

USES OF EPI

acute hypersenitivity (anaphyalaxi/angioedema)

surgical bleeding

open angle glaucoma (decrease pressure)

cardiopulm resus/ cardiac arrest (a1 activation, reduce BF to renal...back to heart)

NE

causes BRADYcARDIA (w/ baroreflex)

vasodialation on all conornay/pulm vessels

use with HYPOTENSION & VASODILATRY SHOCK (sepsis, spinal anethesisa, spinal trauma)
- use with local anestehesis (to slow absorbtion)

Dopamine

LD d1 receptor (vasodilation/renal, stop Na+ resorb in prox tub)
ID b1 + release of NE (SV and HR UP)
HD a1 + D2 (area postrema) (increase sys vasc resistance, vomiting/nausea)

ALL UNDERGO TOLERANCE

DOES NOT ENTER BRAIN/not active oral
t1/2 = 2mins
IV only

USES - cardiogenic/neurogenic/spetic shock (cuz poor renal perfusion)

Phenlephirine

a1 (selective)
not inact by COMT

adverse affects
hyperten, photophobia

USES
hypotension, nasal decongest, myrdiatics, local vasoconstricters

a2 drugs...control

presyn nerve terminal control NE release

Clondine/apraclonidine

a2 selective

ativates Nucles of Tractus solatarious & rostal ventrolateral medulla

activates Imidazoline receptors

all leads to Decreased firing of reticulospinal tract (central adernergic tone)

Effects.....
hypotension (LD) high does HYPERTENSION (a1/a2 activated)

craving reducing affects, sedative, anaglesic

Decease intraoc pressure (dec aq humor)
increase absorb of fluid in intesttine

USES
hypertension
open angle glaucoma (apraclonaine)

hot flashes, ADD, autism, tourettes

Dobutamine

B1 selective

heart - increase conttract/condction

not active by oral. t1/2 = 2mins

uses - given by IV with severaly depressed left Venct fucntion

albuterol/salmerterol/terbutaline

b2

resp- broncodialation, mucus clearance, supression of inflam mediators (hist/leukotiries)
reduce microvasc perm

oral bioval (first pass maybe high)
BBB limited
t1/2 - 1 to 14 hours
INHALINATION main route

B2 agonist time lasting

1.5 hours (EPI, isoprotenol)
3-6 hours (albuterol)
>12 hours (salmeterol/formoterol)

B2 adverse affects

CNS - tremors/cramps/restlessness

Cardio - tachycardia, hypotension

Resp - hypoxemia (too much dialation, decrease V/Q ratio, paradox broncoconstiction

Othersystems - hypokalemai, stimulates K+ into cells
hyperglycemia

b2 contraindiactions

don't use in eldery
hyperthyroidism
seizures

b2 theraputic uses

asthma (as needed)
COPD
premature LABOR (defer delivey)
hyperkalemia (puts K+ in cells)

Tyramine

Indirect acting
taken up by neurons - changed to octopamine....displaces NE

inactive due to large first pass (oral)

Adverse affects bad with MAO inhibitor (leathal hypertensive crisis, due to NE release)

USE - localize lesion of symp nerves

Methyldopa

taken up by neurons....hcanged to methlyNE...a2 agonist (similar to clondine)

Amphetamines

stimulate release of NE, dope, Seroton

blocks catecholamine reuptake

elevation of mood/euphoria (CNS)

similar to NE in periper

uses - ADD, hyperact disorder/narcolepsy/wt reduction

cocaine

blocks cat reuptake

local ansesteia
perip - same as NE
CNS - similar to amph...more intest/shorter

ephedrine

actives all receptors (adernergic)
enhances release of NE

similar to NE
lower potency
longer duraction
oral activiy

ADverse affects - Restlessness/insomnia/urinary rention

clincial - nasal decongestant