Adrenergic Drugs Flashcards
Direct acting - Non-selective
Adrenaline (a1a2b1b2), Noradrenaline (a1a2b1), isoprenaline (b1b2)
Direct selective -a1
phenylephrine, methoxamine, oxymetazoline, xylometazoline
direct selective a2
clonidine, guanabenz, guanfacine, methyldopa
direct selective b1
dopamine, dobutamine, salbutamol
direct selective b2
salbutamol, salmeterol, terbutaline, formoterol, fenoterol, metaproterenol, clebuterol
Mixed acting
a1a2b1b2 releasing: ephedrine
Indirect acting releasing agents
Amphetamine, tyramine
Indirect acting uptake inhibitor
cocaine
Indirect acting MAO/ COMT inhibitor
pargyline, entacapone
Noradrenaline action
equipotent to Epinephrine (adr) on B1, less potent on alpha, little effect on B2
Noradrenaline pharmacodynamics
similar to epinephrine, especially on arterioles and small veins VC and TPR increase, increase SBP and DBP, compensatory vagal reflex slows heart rate, cardiac output decrease, CBF increase
Noradrenaline indications
serious acute hypotensive (vascular collapse, systolic <50
Noradrenaline adverse effects
anorexia, palpitations, headaches, HBP
Dopamine mechanism
direct catecholamine, acts on adrenergic and dopaminergic D1, D2, D3
Dopamine pharmacodynamics
Positive inotropism (activates B1, increased myocardial contractility, increased cardiac output), increase SBP little effect DBP, low doses enhance GFR, RBF, increase plasma Cl
Dopamine indications
shock (in patients with oliguria, low diuresis - cariogenic, traumatic, hypovolemic) , acute pulmonary edema, chronic refractory congestive heart failure
Dopamine SE
tachycardia, arrhythmia, angina
Dobutamine mechanism
direct B1 agonist, no dopaminergic receptors
Dobutamine pharmacodynamics
strong positive inotropic, limited increase in HR (medium chronotropic), increase CO and CBF
Dobutamine indications
congestive HF (after MI), chronic congestive HF
Dobutamine SE
arrhythmia (ventricular ectopy), increased ventricular rate in AFib, angina
Ephedrine mechanism
mixed, indirectly by releasing NE in sympathetic ends, directly by acting on a and B
Ephedrine pharmacodynamics
Similar to epinephrine & NE, lasts longer and not destroyed by MAO, high SBP and DBP by cardiac stimulation and VC
Ephedrine indications
hypotension, rhinitis (decongestant), bronchial asthma (not often due to tachyphylaxis)
Sympatholytic Alpha blockers - Synthetic Nonselective (a1 and a2)
phentolamine, phenoxybenzamine, tolazoline
Symp. Alpha blockers - Synthetic selective (a1)
doxazosin, prazosin, terazosin
Symp Alpha blockers Natural ergot alkaloids ANTIMIGRAIN
ergotamine, dihydroergotamine, methysergide
Symp Alpha blockers Natural ergot alkaloids ANTIISCHEMIA
ergotoxine, dihydroergotoxine
Symp Alpha blockers Natural ergot alkaloids UTERINE CONTRACTION STIMULANTS
nicergoline, ergometrine, methylergometrine
Ergotamine mechanisms
glomerular a blocker after high doses; a adrenergic drug after low doses (therapeutic)
Ergotamine pharmacodynamics
antimigraine, weak increase in uterine tone
Ergotamine therapeutic uses
Migraine, vascular cause headaches
Ergotoxine pharmacodynamics
VD by eliminating spasms, increases CBF, retinal BF, muscular BF, if sympathetic tone is increased in VW: bradycardia
Ergotoxine indications
Chronic treatment in : cerebral atherosclerosis, ischemic cerebral, retinal circulation, vestibular; Raynaud, obliterating arteriopathies (low efficiency)
Ergometrine pharmacodynamics
Stimulates tone, frequency, amplitude of uterine contraction, hemostatic uterine action closing venous sinuses in myometrium
Ergometrine indications
prophylaxis and treatment of postpartum and post- abortum bleedings, lochie retention