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Phenylephrine Methoxamine Ephedrine Metaraminol Intro Direct acting sympathomimetic amine Use Low SVR with spinals or drug induced -50-100mcg boluses nasal decongestant in cold and flu tabs mydriatic Direct acting sympathomimetic amine No longer in production Low SVR 1mg Naturally occurring Indirect and direct acting sympathomimetic amine Hypotension with GA spinal epidural Nocturnal enuresis Narcolepsy Diabetic autonomic neuropathy Hiccups and as nasal decongestant Synthetic Indirect and direct acting sympathomimetic amine Hypotension a/w spinal, epidural or GA 0.5-2mg boluses MOA Potent A1 agonist. No B effects Potent A1 agonist. No B effects Indirect and direct A1 but some B activity Pharmaceut ics CCS 10mg/ml CCS 20mg/ml Direct stim A and B R Indirect release of NA from nerve terminal CCS glass vial 30mg/ml 4 isomer l isomer active 15/30/60mg tablets elixir 3mg/ml 0.5 &1% nasal drops Iv rapid Im or sc longer duration Rapid and complete absorbed o, im sc, No quantitative data available Pharmacokinetics Absorption iv rapid &lasts 5-10mins im or sc takes 15min lasts 1hr Distribuin Metabolism MAO in Liver Excretion CNS No stim effects GIT GU ↓Renal BF Uterus Crosses placenta Resistant to MAO and COMT Liver oxidation, demethylation, aromatic hydroxylation 90% renal unchanged t1/2 6hrs Lasts 15mins or 1hr im Pharmacodynamics CVS ↑SVR and BP. Reflex brady =↓CO not arrythogenic RESP ↑SVR and BP. Reflex brady ↑CO HR BP CBF ↑CMyoRO2 may ppte arrythmias Respiratory stimulant Bronchodilation ↑CBF, stimulatory mydriases Anti nausea. Relaxes GI SM ↓Renal BF ↓GFR relaxes detrusor and contracts sphincter ↑SVR ↑BP Reflex brady =↓CO ↑ CBF by indirect mech. ↑PVR slight ↓RR and ↑TV ↓CBF ↓Renal BF Contraction of pregnant uterus Results in more favourable cord gas profile – not widespread use due to OD risk metabolic Other CCS glass vial 10mg/ml Hyperglycaemia. Glycogenolysis, lipolysis Caution with MAO