Sympathetic Drugs (Adrenergic) Flashcards
Neurotransmitter in Sympathetic
Preganglionic - Ach
Postganglionic - NE
Catecholamines Synthesis
Phenylalanine → L-tyrosine → L-Dopa → Dopamine → Norepinephrine → Epinephrine
Enzymes:
Phenylalanine hydroxylase
Tyrosine Hydroxylase
Dopa decarbocylase
Dopamine b-hydroxylase
Phenylethanolamine N-Methyltransferase
Neurotransmitter Synthesis
Tyrosine Uptake → DOPA → Dopamine → NE Synthesis → NE release → NE Binding → Metabolism (MAO, COMT), → Reuptake
Metyrosine
Inhibits Tyrosine Hydroxylase
Reserpine
Inh. reuptake of NE to vesicles
Bretylium
Inh. release of NE
TCA, Cocaine
Inh. reuptake of NE, Binds to NET
Non-Selective Direct-Acting
Epinephrine
Norepinephrine
Dopamine
Natural Catecholamines Pharmacodynamics
Higher affinity to Beta than alpha
Epinephrine: B1 = B2 > A1
Norepinephrine: B1 > A1
Dopamine: D1 > B1 > A1
Natural Catecholamines Pharmacokinetics
Undergo extensive first pass effect
(decreased oral BA)
- Routes: IV, SQ, inhalation
- Metabolism by MAO & COMT
DOC for Anaphylactic Shock & Cardiac stimulant
Epinephrine
Treating patients with bleeding conditions and ventricular fibrillation
Epinephrine
DOC for Septic Shock
Norepinephrine/Noradrenaline/Levaterenol - Inotropic Agent
Treatment of shock with Hypertension (Cardiogenic Shock, Septic Shock, Hypovolemic Shock)
Dopamine
Dopamine Doses
1-3 mcg/kg/min: D1 activation
2-5 mcg/kg/min: B1 activation
> 5 mcg/kg/min: A1 activation
Alpha1 Overstimulation
Digital necrosis
Beta 1 Overstimulation
Tachyarrhythmias