Non catecholamines

Ephedrine Amphetamine Tyramine

source 1.natural: from ephedra plant. 1.synthetic 1.natural:in cheese ,
2.synthetic yoghourt , broad
beans, salted fish.
chemistry Non catecholamine – alkaloid - stable Non catecholamine - basic Non catecholamine
k absorption Well absorbed orally- delayed onset – long duration
i distribution Can penetrate BBB
n fate -Not metabolised by MAO or COMT -Not metabolised by MAO or metabolised by MAO
e (may inhibit MAO) COMT (in contrast to all
t -part is metabolised in liver and other -part is metabolised in liver and non Catecholamines)
i pass unchanged in urine. other pass unchanged in urine.
c -acidification of urine ++ absorption. -acidification of urine ++absorp.
s Routes of -oral -oral -oral
administration -S.C
-I.M
-local as eye drops &nasal drops
p Mechanism of Dual action : -indirect by stimulate NA -indirect by stimulate
h action -direct on all R (as adrenaline ) release from adrenergic n. (α1- NA release from
a -indirect by stimulate NA release from weak β1) adrenergic n. (α1-
r adrenergic n. (α1- weak β1) weak β1)
m Pharmacological a)local: 1.CVS: -Normally it has no
a action 1.skin: -heart:++ all action as it is
c -decongestion -bl.v. :VC in skin & m.m metabolised by MAO
o -haemostasis -ABP: hypertension as it enzyme in liver
d -cause irritation→ rebound congestion increase both systolic& diastolic -in psychic patients
y 2.eye: → reflex bradycardia who are treated
n -decongestion tachyphylaxis occur in repeated with MAO inhibitors
a -↓IOP(↓aqueous h. by α1) injection → Tyramine will not
m -active mydriasis except in negroes with 2.eye: be metabolised and
i heavily pigmented iris → racial tolerance -decongestion cause release of NA
c b)systemic: -↓IOP(↓aqueous h. by α1) → hypertensive crisis
s 1.CVS : -active mydriasis → may be fatal due
-heart:++ all 3.skeletal m. as ephedrine to cerebral
-bl.v. :VC in skin & m.m - VD in coronary & 4.antiallergic as ephedrine hemorrhage
sk.m 5.CNS : → it is treated by α
-ABP: hypertension → when IV it act Marked action blocker or
only indirect → ↑ both systolic & 1-psychic: combination of α, β
diastolic → no change in pulse p. → -small dose: euphoria, blockers.
hypertension is abolished by α blocker. wakefulness , alertness ,insomnia -interaction bet.
tachyphylaxis occur in repeated injection -moderate dose: anxiety ,tremor Tyramine and MAO
2.bronchi : -large dose: schizophrenia inhibitors us called
Decongestion & bronchodilatation ,convulsions cheese interaction
3.GIT : 2-analgesic: (one of the drug
relax wall & contract sphincter Potentiate morphine action food interaction )
4.urinary bladder : 3-anorexigenic:
relax wall & contract sphincter (marked) ↓feeding center of hypothalamus
5.CNS: ↓acuity of smell and taste
Stimulate cerebral cortex and RAS → 4-analeptic:
wakefulness, alertness ,insomnia Stimulate RC & VMC
Stimulate RC &VMC (analeptic) 5-spinal
6.skeletal muscle : Stimulate mono & poly s. reflexes
VD –facilitate NMT → in myasthenia g. 6-tolerance and addiction occurs
7. antiallergic : on prolonged use
8.no metabolic action
Therapeutic uses 1.nasal decongestant →it cause rebound
congestion so pseudoephedrine is better
2.mydriatics in fundus examination
3.hypotension in spinal anaesthesia or
overdose of GB or sympathectomy
4. AV block
5.prophylaxis of bronchial asthma (SABA
is better)
6.nocturnal enuresis (TCAS are better)
7.nacrolepsy (amphetamine is better)
8.adjuvant to neostigmine in myasthenia
Adverse effect -tachycardia
-palpitation
-anginal pain
-hypertension
-urine retention especially in prostatic
hyperplasia
-CNS stimulation (insomnia)
-tolerance (no addiction)
contraindications -As adrenaline
-prostatic hyperplasia
(Not commonly used nowadays)
1.nacrolepsy
2.attention deficient
hyperkinetic disorders (ADHD)
3.psychic depression in
parkinsonism and chronic
alcoholics → to elevate mood
4.obesity
5.ttt of acute toxicity in drugs
that inhibit RC as morphine
5.nocturnal enuresis
-hypertension
-reflex bradycardia
-insomnia
-anorexia & weight loss
-tolerance & addiction
-Acute toxicity:
1)Manifestation:
Hypertension-bradycardia-
active mydriasis-insomnia-
hallucination then convulsion
then coma and death
2)treatment:
-Stomach wash
-artificial respiration
-no specific antidote –-
symptomatic treatment
-↑ urinary acidity to↑ excretion
-hypertension
-bradycardia
-psychic disorders as
schizophrenia
-MAO inhibitors as they cause
hypertensive crisis→ treated
by α blocker or combination of
α, β blocker
N.B :

1) Vasopressor sympathomimetics :
-include : phenylephrine – methoxamine – midodrine
-actions: 1)VC → decongestion, haemostasis & prolong action of LA , → hypertension and reflex bradycardia
2)Active mydriasis
-therapeutic uses:
1)phenylephrine & methoxamine: decongestion - haemostasis – ↑action of LA – hypotension _ PAT –fundus examination
2)midodrine : prodrug converted to active metabolite in treatment of chronic postural (orthostatic) hypotension

2) Nasal decongestants :
a)local: naphazoline – tetrahydrazoline – oxymetazoline – xylometazoline → used in common cold. Sinusitis, rhinitis
but they cause drowziness in children and may cause atrophy of olfactory mucosa and ansomnia in long term use.
b) systemic(oral): pseudoephedrine – phenylpropnolamine ( not used as it cause hemorrhagic strokes)

3) non selective β agonists :

Includes adrenaline – isoprenaline – isoxsuprine (used in PVD and contraction ring of uterus)

4) selective β1 agonists :
Includes : dobutamine – Prenalterol ( given orally or IV and is used in treatment of heart failure

5) selective β2 agonists :
Includes :
1- isoetharine : catecholamine metabolized by COMT
2- salbutamol – terbutaline : non catecholamine , short acting selective β2 agonist = SABA
→ in treatment of acute attacks of bronchial asthma
3- salmeterol – formeterol – bambuterol : non catecholamine , long acting selective β2 agonist = LABA
→ in prophylaxis of bronchial asthma
4- ritodrine : non catecholamine used in uterine relaxation (tocolytic) in contraction ring of the uterus , premature
labor, threatened abortion , dysmenorrhea

Pharmacological action :
-VD in skeletal muscle → ↓↓ABP
-bronchodilatation and mast cell stabilization and inhibition of release leukotrienes
-uterine relaxation
-tachycardia (reflex or direct if it is given in large doses as selectivity is not absolute )
-tremors

Therapeutic uses :
-bronchial asthma
- contraction ring of the uterus , premature labor, threatened abortion , dysmenorrhea

Adverse effects :
-tachycardia
-hypotension , flushing
-tremors
-hypokalemia
-tolerance due to down regulation of receptors ( prevented by cortisone)