Adrenergic Receptor Agonist (Sympathomimetic Agents)

Direct-Acting receptor agonist

Nonselectiv
e
Indication.Pharmacology Pk ADR/CI/SP
alpha & beta agonists NE (all except B2) Vasoconstrictor Uptake 1, not given orally severe HPN, arrhythmia, sloughing &
tissue necrosis
E (all) Vasoconstrictor Uptake 2 Coronary artery ->angina
w/ NS beta blocker aggravate COPD &
asthma
Beta 1 & Beta 2 agonist
Isoproterenol (pure B)
CHF, acute MI or acute emboli, bradychardia or
heart block
Uptake 2 Cardicac ischemia, arrhythmia
Tachycardia, palpitation, HA, flushing
Selective
alpha 1
PhenylE Nasal decongestant, mydriatic agent w/o
cyclopegia, hemostatic agent, vasopressor
Paroxysmal supraventricular tachychardia
Long duration
Orally bioavailable



Prolong use damage to mucosa
Topical: do not give >3-5days
Imidazoles (topical & nasal
decongestants)



Topical & nasal decongestants

Naphazoline Short-Acting
Tetrahydrozoline
Oxymetazoline Long-Acting
Xylometazoline
Midorine Pro-drug autonomic insufficiency & postural
hypotension
Peak: 1hr
Duration: 4-6hrs
Complication: supine HPN
alpha 2 Clonidine Anti HPN
Methyldopa
Guanfacine
Guanabenz
Lofexidine
Apraclonidine Dec. IOP (Wide Angle Glaucoma)
Bimonidine
Tizanidine Ms relaxant
Mivazerol Anti-MI
beta 1 Dobutamine
Prenalterol
beta 2 Terbutaline Asthma, bronchodilator
COPD, enhance blood flow, delay labor,
vasospastic dse.

Oral, SQ, inhalation, very rapid onset, Short-
Acting
Duration: 3-6hrs




Black box warning Arformoterol
ADR: skeletal ms tremor, restlessness,
apprehension, axniety, tachycardia,
hypoglycemia in Diabetics
CI: MAOI, NE
Tocolytic: Pulmonary edema
Salbutamol/Albuterol Rapid onset: 15mins ER
Duration: 3-4hrs Short-Acting
Arformeterol Long term tx - asthma
Carmoterol

COPD & asthma 5x more beta 2
Rapid onset, long duration OD
Salmeterol COPD Duration: 12hrs, not for acute conditions,
Long-Acting
Nocturnal Asthma + Formoterol
Salmeterol + fluticasone
Formoterol Nocturnal asthma & COPD Onset: w/in mins. Long-Acting
Formoterol + Budesonide
Indacaterol COPD Ultra long acting, fast onset,
Isoxuprine Tocolytic
Ritodrine
Dopa Dopamine
renal & splanchnic blood vessels, vasodilation,
inc. tissue perfussion cardiogenic & septic shock
CHF
Poorly absorbed; not used orally Same as Epi
P: MAOI, TCAS
Dobutamine
Fenoldopam Severe HPN
(Malignant HPN w/ end organ damage)
Indirect-Acting
Displaces NE stores Amphetamine Narcolepsy
ADHD
Norexiant
CNS than ephedrine, mood, alertness,
appetite suppression
Prolong use: depression & fatigue
Chronic use: dependence
ADR: vivid hallucination,& paranoid
delusion
Metamphetamine More pronounce, less peripheral High potential for abuse
Phenmetrizine Anorexiant Aggravating glaucoma release of NE
Methylphenidate ADHD, narcolepsy, mild CNS stimulant
Pemoline
Modafinil Narcolepsy, psychostimulant
Tyramine Not drug Low bioavailability Avoid w/ MAOI
Dec. clearance of
released NE

Reuptake inh Cocaine Local anesthetic w/ peripheral actin
Vasoconstriction
Rapid onset Heavily abused drug
TCA Antidepressant (ex. imipramine)
ADHD

Atemoxetine
Reboxitine ADHD
Serotonin reuptake inh Sibutramine Appetite suppressant long term tx - obesity Withdrawn because of stroke
Duloxetine Antidepressant
Tx pain in fibromyalgia

Minalcipran Fibromyalgia
Block metabolizing
enzymes
Pargyline MAOI
Mixed-Acting
Ephedrine Potent CNS stimulant
Similar to EPI; less efficacious
Mydriasis w/o cyclopedia
Tx narcolepsy
Promote urinary continence
High bioavailability
Long duration of action
Cannot be used in acute conditions
Half life: 3-6hrs; less efficacious than EPI
Adjuvant to general anesthestics
ADR: Inc. PVR, HPN, insomnia,
tachyphylaxis
Psuedoephedrine oral nasal decongestant
similar to ephedrine
Requires S-2 license
Regulated drug
PPE Oral nasal decongestant
Less CNS stimualtion
Same w/ ephedrine ADR: Hemorrhagic stroke