Adrenergic neuron blockers and ganglionic blockers Flashcards
Adrenergic neuron blockade MOA: Guanethedine
Inhibit NE release from adrenergic nerve terminals
Deplete catecholamine stores
Forms false neurotransmitters
Adrenergic neuron blockade MOA: Bretylium
Inhibit NE release from adrenergic nerve terminals
Adrenergic neuron blockade MOA: Reserpine
Deplete catecholamine stores
Adrenergic neuron blockade MOA: Methyldopa
Deplete catecholamine stores
Forms false neurotransmitters
Adrenergic neuron blockade MOA: Pargyline
MAO inhibitor
Adrenergic neuron blockade MOA: Metyltyrosine
Interfere with catecholamine synthesis
Adrenergic neuron blockade MOA: 6-Hydroxydopamine
Destroy adrenergic nerve fibers
Adrenergic neuron blocker which is worst for orthostatic hypotension ADR
Guanethedine and congeners
Reserpine: solubility, MOA, ADR, effect on CVS/Brain/GIT
Readily enters the brain
MOA: Irreversibly binds tightly to adrenergic storage vesicles: depletion of catecholamines in CNS and adrenal medulla
ADR: Extrapyramidal symptoms, Depression
CVS: decreased HR, CO, PVR, BP
-Salt and water retention–> pseudotolerance, edema
Brain: sedation, EPS, depression
GIT: parasympathetic predominance
Methyldopa: indication, MOA, ADR
Indication: Hypertension during pregnancy
MOA: central a2 agonist: decrease PVR; false neurotransmitter
ADR: Sedation at onset, EPS, amenorrhea, postural hypotension, lactation
Guanethedine: Indication, solubility, MOA
Indication: severe form of hypertension
Polar, cannot cross BBB, no sedation
Bretylium-like: blocks NE release by blocking impulse conduction in nerve terminals
Cocaine-like: inhibits neuronal uptake
Reserpine-like: catecholamine depletion
Tyramine-like: rapid release of NE from stores (sympathomimetic)
Guanethedine: ADR
Profound sympathoplegia
Pharmacologic sympathectomy
Metyrosine: MOA
Inhibits tyrosine hydroxylase
6-Hydroxydopamine: MOA
selectively neurotoxic for noradrenergic terminals
Converted to quinone–> chemical sympathectomy
Destruction of nerve fibers
Treatment of lifethreatening ventricular arrhytmias that dont respond to lidocaine or procainamide
Bretylium