NON CATECHOLAMINES

1. NON
CATECHOLAMINE
S
-Dr.D.RAJESH;M.D.
DEPARTMENT Of
PHARMACOLOGY
RIMS ONGOLE

2. Definition
Classification
Drugs

3. • Compounds lacking catechol hydroxyl
groups are called non catecholamines
• Characteristics
Longer half lives – long duration of action
Increased lipid solubility – access to CNS
Effective orally

4. CLASSIFICATION
I. Acc. To MOA:
1. Direct acting – Phenylephrine, Methoxamine,
Oxymetazoline, Clonidine, Metaproterenol,
Salbutamol, Terbutaline, Salmeterol
2. Indirect acting – Amphetamines, Tyramine
3. Mixed action – Ephedrine, Pseudoephedrine,
metaraminol

5. II. Acc. To therapeutic uses:
1. Vasopressor agents: phenylephrine,
methoxamine, ephedrine, mephenteramine
2. Bronchodilators – salbutamol, terbutaline,
salmeterol, formeterol, bambuterol
3. Nasal decongestants – phenyephrine,
naphazoline, oxymetazoline, xylometazoline,
pseudoephedrine, phenylpropanolamine

6. 4. CNS stimulants – amphetamine,
methamphetamine, dexamphetamine
5. Anorectics – fenfluramine, dexfenflramine,
sibutramine
6. Uterine relaxants – ritodrine, isoxsuprine,
salbutamol, terbutaline

7. III.Receptor action:
1. α1 agonists – phenylephrine, methoxamine,
metaraminol, mephenteramine
2. α2 agonists – clonidine, apraclonidine
3. β2 agonists – salbutamol, terbutaline,
isoetharine, ritodrine
4. β3 agonists – BRL 37344, AD 9677

8. PHENYLEPHRINE
• Selective α1 agonist
• Vasoconstrictor - SBP, DBP
• Reflex bradycardia
• Uses:
– Hypotension, shock
– Nasal decongestant
– Mydriatic

9. METHOXAMINE
• Selective α1 agonist
• Inc. total peripheral resistance
• Not arrythmogenic
• Uses:
– Hypotension
– PSVT
– Nasal decongestant

10. METARAMINOL
• Selective α1 agonist
• More direct action, also release NA
• Inc. force of contraction, CO, raise BP
• Gradual onset, longer duration
• Uses:
– Ac. hypotensive states – SA/ Shock
– Nasal decongestant
– PAT

11. MEPHENTERAMINE
• Acts both directly and
indirectly
• BP, cardiac rate and
contraction
MIDODRINE
• Prodrug converted to
desglymidodrine
• Vasoconstriction
• Use: postural
hypotension

12. OXYMETAZOLINE
• Stimulates both α receptors
• Acts on BV of nasal mucosa & conjunctiva
• Use
– Eye drops
– Nasal decongestant
• SE – nervousness, HA, burning of nasal mucosa,
sneezing

13. Naphazoline, Xylometazoline
• Local vasoconstriction
• Longer duration of action
• SE: atrophic rhinitis, anosmia
–Systemic – CNS depression, rise BP

14. AMPHETAMINES
• It is phenyl isopropylamine
• Indirectly acting sympathomimetic
• CNS actions: CNS stimulant
– Inc. mental & physical activity, euphoria
– Clinical dose – wakefulness, dec. fatigue
– Larger doses – tremor, restlessness, confusion
• CVS: Inc. SBP, DBP

15. • Smooth muscle: contracts bladder
sphincter, relax bronchial muscle
• Appetite: suppress appetite – wt. loss
• Weak analgesic, anticonvulsant, anti
emetic
• ADR :palpitations, restlessness, HA,
anxiety, psychosis

16. • Ac. Toxicity:
– CNS – restlessness, tremors, irritability
– Behavior – delirium, confusion, psychosis,
suicidal/ homicidal tendencies
– ANS instability – angina, arrythmias, HTN
– GI – anorexia, vomiting, abd. Cramps
– Mx – symptomatic,
• Diazepam
• α blocker phentolamine
• Peritoneal dialysis

17. • Dependence: psychological – euphoria,
mental confusion, wt loss
• Withdrawal symptoms
– Chr. Fatigue, depression
– GI disturbances
– Drowsiness
– Intense craving
• Uses:
– ADHD
– Narcolepsy

18. • Only CNS effects
• Piperidine derivative
• Used in ADHD
METHAMPHETAMINE
METHYLPHENIDATE

19. TYRAMINE
• Indirect action
• Normal byproduct of tyrosine metabolism
• Metabolized by MAO
• CHEESE REACTION – inc. BP
• Not used clinically

20. EPHEDRINE
• Alkaloid obtained from Ephedra vulgaris
• Acts on both α, β receptors
• CVS: BP, CO.
– Repeated adm.- tacyphylaxis
• Smooth muscle: relax
• CNS – stimulation – tremors, insomnia, anxiety

21. • Eye: mydriasis
• Metabolic: inc metabolic rate, O2 consump.
• SE: GI upset, insomnia, rarely psychosis
• Uses:
– Br.asthma
– Nasal decongestion
– Hypotension
– Stokes Adams syndrome
– Mydriatic
– Narcolepsy
– Misc. – myasthenia gravis, allergic bronchospasm

22. PSEUDOEPHEDRINE
• Stereo isomer of ephedrine
• Vasoconstriction sp. Mucosa & skin
• Use:
– Nasal & sinus congestion
– Allergic rhinitis
– Blocked eustachian tubes
– URTI

23. β2 STIMULANTS
• Longer duration of action
• Bronchodil, Vasodil, Uterine relax
• Uses:
– Br. Asthma
– Uterine relaxants
• SE: muscle tremor, tachycardia
– Less likely arrythmias

24. ISOXSUPRINE
• Smooth muscle relaxant
• Use:
– Threatened abortion
– Dysmenorrhea
– Premature labor
– Peripheral disease
• SE: nausea, tachycardia, hypotension

25. ANORECTIC AGENTS
• Cause central release of NA/DA
• Inhibit reuptake of NA & DA

26. β3 agonists
• Polymorphism in β3 receptor gene is related
to risk of obesity
• Targets for anti obesity drugs
• BRL 37344 – No FDA clearance
• AD 9677 – Phase III CT