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Non catecholamines
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- 3. • Compounds lackingcatechol 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. ToMOA: 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. Totherapeutic 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. α1agonists – 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 α1agonist • Vasoconstrictor - SBP, DBP • Reflex bradycardia • Uses: – Hypotension, shock – Nasal decongestant – Mydriatic
- 9. METHOXAMINE • Selective α1agonist • Inc. total peripheral resistance • Not arrythmogenic • Uses: – Hypotension – PSVT – Nasal decongestant
- 10. METARAMINOL • Selective α1agonist • 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 bothdirectly and indirectly • BP, cardiac rate and contraction MIDODRINE • Prodrug converted to desglymidodrine • Vasoconstriction • Use: postural hypotension
- 12. OXYMETAZOLINE • Stimulates bothα receptors • Acts on BV of nasal mucosa & conjunctiva • Use – Eye drops – Nasal decongestant • SE – nervousness, HA, burning of nasal mucosa, sneezing
- 13. Naphazoline, Xylometazoline • Localvasoconstriction • Longer duration of action • SE: atrophic rhinitis, anosmia –Systemic – CNS depression, rise BP
- 14. AMPHETAMINES • It isphenyl 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 CNSeffects • 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 obtainedfrom 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 isomerof ephedrine • Vasoconstriction sp. Mucosa & skin • Use: – Nasal & sinus congestion – Allergic rhinitis – Blocked eustachian tubes – URTI
- 23. β2 STIMULANTS • Longerduration of action • Bronchodil, Vasodil, Uterine relax • Uses: – Br. Asthma – Uterine relaxants • SE: muscle tremor, tachycardia – Less likely arrythmias
- 24. ISOXSUPRINE • Smooth musclerelaxant • Use: – Threatened abortion – Dysmenorrhea – Premature labor – Peripheral disease • SE: nausea, tachycardia, hypotension
- 25. ANORECTIC AGENTS • Causecentral release of NA/DA • Inhibit reuptake of NA & DA
- 26. β3 agonists • Polymorphismin β3 receptor gene is related to risk of obesity • Targets for anti obesity drugs • BRL 37344 – No FDA clearance • AD 9677 – Phase III CT
Editor's Notes
- #4 Longer half lives as they are not inactivated by COMT Resistant to MAO – so longer duration of action Increased lipid solubility and has greater access to CNS Effective orally
- #5 Direct acting – act directly on α,β receptors producing effects similar to those that occur following stimulation of sympathetic nerves or release of Adr/ NA. eg. Phenylephrine, Methoxamine, Oxymetazoline, Clonidine, Metaproterenol, Salbutamol, Terbutaline, Salmeterol Indirect acting – They block the uptake of NA/ are taken up into the presynaptic neuron and cause release of NA from cytoplasmic pools/ vesicles of adrenergic neurons. Released NA then binds to α,β receptors. Eg.Amphetamines, Tyramine Mixed action – they have the capacity both to stimulate adrenoceptors directly and to release NA from adrenergic neuron. Eg. Ephedrine, Pseudephedrine, metaraminol
- #18 attention-deficit hyperactivity disorder (ADHD) of children, a poorly defined and overdiagnosed behavioral syndrome consisting of short attention span, hyperkinetic physical behavior, and learning problems. Narcolepsy is characterized by hypersomnia, including attacks of sleep that may occur suddenly under conditions that are not normally conducive to sleep.