Adrenergic Agonist Flashcards
Direct Acting Alpha Agonist
Nonselective: NE
A1: Phenylephrine
A2: Clonidine
Direct Acting Beta Agonist
Nonselective: Isoproterenol
B1: Dobutamine
B2: Albuterol
Indirect acting Sympathetic Agonists
Releases: Amphetamine
Reuptake inhibitors: Cocaine
Epinephrine
- Rapid Nonselective brief Agonist
- Prominent CV action: Low dose Vasodilation, High Vsoconstriction; INC ionotropic effect
- Antiotensin II activation
- INC systolic; DEC diastolic
- Respiratory: Bronchodilation; inhibits allergy mediators
- Hyperglycemia; lipolysis; Open glaucoma
- Clinical: Emergency respiratory; Anaphylaxis; maintain midriasis
NE
- Rarely used clinically; favors alpha
- INC both systolic/diastolic
- Septic/neurogenic shock
Isoproterenol
- Both B1/2
- CV: INC HR, CO; DEC Peripheral Resistance
- STHMSC: hepatic glycogenolysis, INC glucagon. And RAAS activation
- Clinical: Rarely used; maintain idioventricular rate till pacemaker placed
Dobutamine
- Primary B1 agonist
- INC CO + Contraction Force; No change in HR, BP, or SVR
- Clinical: Cardiac decompensation, AHF
- CAUTION: AFib
Oxymetazoline
- Direct acting Alpha agonist 1/2
- Nasal conjunctiva/mucosa -> Vasocontriction + DEC Congestion
- Hypotension in large doses
Phenylephrine
- Selective alpha-1 direct acting
- Raises Sys/Dia BP
- Induces reflex bradycardia
- Cinical: PSTachy; Hypotension; Nasal Decong; induce Mydriasis
AR: Hpertensive headaches + Cardiac Irrhytmia; Dysuria
Midodrine
- Direct acting a1 selective agonist Prodrug
- INC BP vis VSMT
- Clinical: Chronic symptomatic orthostatic hypotension
- AE: Supine hypertension; Parasthesia, piloerection, dyspraxia + retention + Urgency
- Contra: CHD; HF; Renal impairment; Other BP Meds
Clonidine
- Selective central presynaptic a2 agonist
- Inhibit sympathetic outflow f/ CNS
- Clinical: Hypertension, Withdrawal, ADHD NON STIMULANT, diabetic diarrhea, menopausal hot flashes, anesthesia premedication
Apraclonidine + Brimonidine
Clonidine Congeners
Apraclonidine: Doesn’t Cross BBB; Short term intraocular pressure + Claucoma
Brimonidine: ore a2 selective for Short + Long term glaucoma
B2 Short acting
Albuterol; Metaproterenal; Terbutaline
- SABA
- Bronchial dilation + Uterine relaxation
- Contra: Tachycardia; Arrythmias; MAOIs
Long acting B2 agonist
Salmeterol; Formoterol; Arformoterol
- Asthma; Maintenance treatment COPD
- Salmeterol delayed action (Not for acute attacks)
- NOT for monotherapy AKA combine w/ corticosteroid
Indacaterol; Olodaterol; Vilanterol
- Ultra Long LABA (Once Daily)
- COPD. Emphysema, chronic bronchitis, and both
- NO Monotherapy
Mirabegron
- B3 agonist
- Detrusor muscle (Overactive bladder)
Dopamine
- DA Adrenergic agonists
- Mixed action D1/D2
- Ionotropic
- Reduce renal arterial resistance + INC BF
- Clincal: Cardiogenic/septic shock; Hypotension, CHF, bradycardia
Fenoldopam
- Peripheral Dopamine D1
- Clinical: Hypertensive Emergency - rapid acting vasodilator
Ephedrine
- Mixed action indirect adrenergic agonist
- Clinical: Peristent hypotension; Spinal anesthesia induced hypotensionl; Asthma
Contra: MAOIs
Amphetamine
- Inhibits reuptake transporter NET + DAT
- Aginist of TAAR1
- Binds postsynaptic adrenergic receptors
- High doses block MAO-A
- Clinical: ADHD; Depression; Narcolepsy
- Contra: `lactation, Obestiy, MAOIs, Hyperthyroidism, CVD, Glaucoma; - - *DependanceSched II
Lisdexampfetamine
- Prodrug if dextroamphetamine
- decrease abuse potential
- adhd + binge eating
Methylphenidate
- Ritalin
- Allosterically blocks DAT + NET
- ADHD in children
- Locks dopamine more than NE
Atomoxetine
- Nonstimulant drug for ADHD
- more selective for NE reuptake
- NOT habit-forming/controlled
Cocaine
- Blocks Na/Cl dependent NET + DAT allowing NE/DA to remain in cleft
- A1 agonist
- Local anesthetic
- Controlledsubstnace with HIGH abuse potential
Adverse effects of adrenergic agonists
- Hypertension
- Cerebral hemorrhage
- Pulmonary edema
- Cardiac Arrhythmias
- headache, dizziness, and tremor
Adrenergic agonist interactions
- Tricyclics blocks catecholamines reuptake
- Halogenic anesthetic agents