Adrenergic Drugs Flashcards
Epinephrine
Direct Acting Endogenous Catecholamine
Receptors: a &B2 (low dose B, high Dose a)
Effect: Increase lipolysis, hyperglycemia,High dose-potent vasopressor, bronchodilation Low dose-tachycardia , Does not Enter CNS
Uses: DOC patient in anaphylactic shock
AE: Not given orally, CNS disturbances, intracranial hemorrhage, cardiac arrhythmias, pulm. edema
Norepinephrine
Direct Acting Endogenous Catecholamine
Receptors: A&B1> B2
Effects: Bradycardia, vasoconstriction, induces hyperglycemia
Uses: Limited therapeutic value, can treat shock, control BP
AE: may cause kidney shutdown
Dopamine
Direct Acting Endogenous Catecholamine
Receptors: D& a& B
Effects: Low dose-vasodilate, Intermediate-increasing release of NE, High Dose-a1 mediated vasoconstriction( increase BP)
Uses: DOC for cardiogenic and hypovolemic shock, TXT for severe CHF
AE: ineffective orally, Overdose causes sympathomimetic symptoms, causes nausea.
Isoproterenol
Direct Acting B-agonist
Receptor: B1 & 2
Effects: CVS-increase: CO, lipolysis,HR, hyperglycemia Decrease: MAP, TPR, DBP GI relax
Uses: Stimulate heart in emergency pts. bradycardia or heart lock + cardiogenic shock
AI: Similar adverse effects
Dobutamine
Direct acting B-agonist
Receptor: B1
Effect: increase CO with little change in heart rate
Uses:Acute management of congestive heart failure
AE: can build up tolerance
Albuterol
Direct Acting B-Agonist
Uses: Relief symptoms in asthma (no effect on heart)
AE: tremor, restlessness, apprehension and anxiety
Salmeterol
Direct Acting B-agonist
Uses: long acting Bronchodilator (note used for prompt relief of bronchospasm)
AE: tremor, restlessness, apprehension and anxiety
Formoterol
Direct Acting B-agonist
Uses: long acting Bronchodilator (note used for prompt relief of bronchospasm)
AE: tremor, restlessness, apprehension and anxiety
Phenylephrine
Direct Acting a-agonist
Receptor:a1
MOA: peripheral vasoconstriction
Effect: vasoconstrictor, increases: SBP and DBP(No effect on hear but causes reflex bradycardia)
Uses: Nasal decongestant, TXT of supraventricular tachycardia
Clodine
Direct Acting a-agonist
Receptor:a2
MOA: Partial agonist
Uses: Antihypertensive
AE: Sedation, Mental lassitude, impaired concentration, Xerostomia, Lethargy
Methyldopa
Direct Acting a-agonist
Receptor:a2
MOA: central acting anti-HTN
Uses: DOC in pregnant patient with HT N
AE: Sedation, Mental lassitude, impaired concentration, Xerostomia, Lethargy
Brimonidine
Direct Acting a-agonist
Receptor:a2
MOA: decreases aqueous humor production along with increased outflow
Uses: Glucom
Amphetamine
Indirect Acting Agonist
Receptor:little effect on post sympatic a and B
MOA: displaces catechol form storage vesicle,weak MAO, blocks catecholamine reuptake
Uses: Depression, narcolepsy, appetite suppression
AE: fatigue and depression following stimulation
Methylphenidate
Indirect Acting Adrenergic Agonist
Receptor: structural analog of amphetamine
Uses: ADHD in children, Narcolepsy
Tyramine
Indirect Acting Agonist
Uses:not clinically useful but is found in fermented foods(cheese & wine)
AE: serious vasopressor episodes in patients on MAO-I release of NE
Cocaine
Presynaptic Indirect Agonist
Receptor: DAT,SERT, NET
MOA: Blocks dopamine(major), serotonin NE transporters
Uses: local anesthetic of the resp. tract
AE: Intense euphoria
Atomoxetine
Presynaptic Indirect Agonist
Receptor:NET
MOA:selective NET inhibitor
Uses:ADHD
Modafinil
Presynaptic Indirect Agonist
Receptor: DAT,NET
MOA:inhibit NE and Dopamine transporter (increases: NE, Dopamine, Serotonin, glutamate Decreases: GABA)
Uses: Narcolepsy
Ephedrine
Mixed Acting Agonist
Receptor: a & B
Uses:Asthma, synergistic effect with anti- AChe in treatment of MG, increases athletic performance
AE: Banned in 2004 due to life-threatening cardiovascular reactions
Pseudoephedrine
Mixed Acting Agonist
Receptor: a & B
MOA: Ephedrine enantiomer
Uses: Nasal decongestant with H1 histamine antagonist
Phenoxybenzamine
a-antagonist
Receptor: non selective a
MOA:Alkylation irreversibly blocks receptor, slight a1 selective also block:H1, M and 5-Ht receptors, inhibits NET
Effects: prevents vasoconstriction of peripheral vessels, increases CO
Uses: DOC pheochromocytoma
AE: Postural hypotension, Nasal stuffiness, Inhibits ejucatation. Contraindicated in pts with low coronary perfusion
Phentolamine
a-antagonist
Receptor: non selective a
MOA:reversible a block, Serotonin blocker, Muscarinic, H1 and H2 agonist
Uses: hypertensive episodes of pheochromocytoma, prevents dermal necrosis, antihypertensive in stimulant overdose,
AE: Postural hypotension, Arrhythmia & angina, contraindicated in pts with low coronary perfusion
Prazosin
a-antagonist
Receptor: selective a1, useful in treatment of HTN
MOA:↓TPR through relaxation of
arterial and venous smooth
muscle
Effects:↓ BP without reflex
tachycardia […α2]↓ LDL/TAG, ↑HDL Improves urinary
blood flow
Uses: TXT of HTN, BPH
AE:First dose effect may cause exaggerated
hypotensive response and syncope [adjust 1st
dose ¼ of normal]
Terazosin
a-antagonist
Receptor: selective a1, useful in treatment of HTN
MOA:Structural analog of prazosin →longer t1/2 → Less frequent dosing
Effects:↓ BP without reflex
tachycardia […α2]↓ LDL/TAG, ↑HDL Improves urinary
blood flow
Uses: TXT of HTN, BPH
AE:First dose effect may cause exaggerated
hypotensive response and syncope [adjust 1st
dose ¼ of normal]
