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Autonomic Drugs 2 Definition COMT Catechol O-methyltransferase (at synaptic space, metabolize noradrenalin) MAO Monoamine oxidase (located

at neuronal mitochondria, oxidize noradrenalin) Adrenergic Receptors Receptors stimulated by Noradrenalin, Adrenaline Groups 1 y At post-synaptic effector organs y Stimulation cause smooth muscle contraction (eg. vasoconstriction) 2 y Inhibitory in nature y Located at pre-synaptic nerve endings, other cells y Stimulation causes feedback inhibition of NA release 1 y Cause cardiac stimulation 2 y Produce vasodilatation (Relax vascular smooth muscle) y Bronchiolar relaxation IV Infusion of Adrenaline, Noradrenalin, Isoprenaline

Distribution & Functional Response of Adrenoceptors 1 receptors Contraction of majority of vascular smooth muscle Contraction of trigone & sphincter Ejaculation of male sex organs Contraction of pupillary dilator muscle (dilates pupils) Erect hair of pilomotor smooth muscle 2 receptors Central sympathetic outflow (CNS) Inhibit NA release (Adrenergic nerve terminals) 1 receptors Force of contraction, Contraction rate of heart Renin release in juxtaglomerular apparatus 2 receptors Relaxation of bronchial smooth muscle (bronchodilation) Relaxation of uterine smooth muscle Relaxation of vascular smooth muscle Glycogenolysis, Gluconeogenesis in liver Glycogenolysis in skeletal muscle

Therapeutic Uses of Drugs Drug Uses Adrenaline Acute asthma Anaphylactic shock Noradrenalin Shock Dopamine Shock Heart failure Dobutamine Heart failure Phenylephrine Nasal congestion Clonidine Hypertension Salbutamol Asthma Ritodrine Premature labour Terbutaline Ephedrine Nasal decongestion

Receptor 1, 2, 1, 2 1, 2, 1 D, 1 1 1 2 2

Adrenergic Agonists (Sympathomimetics) Catecholamines Adrenaline, Noradrenalin, Dopamine, Dobutamine Short duration of action Not given orally Do not penetrate BBB Rapidly inactivated by (short period of action) y COMT (post-synaptically) y MAO Ineffective orally (inactivated by GIT enzymes) Polar substance (poor CNS penetration) Adrenaline (SC, IV, ETT, Inhalation, Eye-topical) Act on , receptors ( 1- 2) Effects CVS ( ) y +ve inotropic, +ve chronotropic y CO, O2 demand Vascular ( , ) y Constricts arterioles in skin, mucous membranes, viscera y Dilates vessels to liver, skeletal muscle ( 2) y Systolic BP (SBP) Diastolic BP (DBP) Respiratory y Bronchodilation (direct action bronchial smooth muscle ( 2)) y Useful anaphylactic shock, acute asthma Metabolic Hyperglycemic y ( Glycogenolysis in liver) ( Glucagon release, 2 effect) Smooth muscle GIT y Tone & Motility ( 2, ) y Sphincter constriction ( ) Smooth muscle uterus y Relaxation ( 2) Bladder y Detrusor muscle relaxation ( 2) y Contraction trigone, sphincter ( 1) Kinetics Metabolized by COMT, MAO Oral ineffective (inactivated by intestinal enzymes) Therapeutic Uses Bronchospasm (bronchoconstriction) y Acute asthma y Anaphylactic shock Adverse Effects Arrhythmias Angina pain (IHD patient) Headache Tremor CNS disturbances y Anxiety y Fear Tension Noradrenalin Act on , 1 receptors (little effect on 2 receptor) Neurotransmitter of postganglionic adrenergic neuron 10-20% of catecholamine secreted by adrenal medulla (during sympathetic stimulation) Effects CVS Peripheral resistance y (due to vasoconstriction of vascular beds incl. kidney ( 1)) y Systolic BP (SBP) y Diastolic BP (DBP) BP Induce reflex rise vagal activity (stimulate baroreceptors) Bradycardia

Non-Catecholamines Ephedrine, Amphetamine Longer duration of action Not inactivated by COMT Poor substrates for MAO Lipid solubility (better penetration CNS)

Direct Acting ( 1 selective, 2 selective) (Oral, Inhaled) 2 selective agonists Salbutamol (albuterol), Terbutaline Action y Relax bronchial smooth muscle (bronchodilatation) y Uterine relaxation Therapeutic use y Bronchial asthma Premature labour ( 2) y Adverse Effects y Skeletal muscle tremor y Tachycardia y Hyperglycemia 2 agonist Clonidine, Methyldopa Action y Act centrally to inhibit sympathetic vasomotor center Therapeutic use Symptoms of opiate, y benzodiazepine withdrawal y Hypertension 1 selective agonists Phenylephrine, pseudoephedrine Therapeutic use y Nasal decongestant (topically)

Indirect Acting Amphetamine, Methamphetamine Effects NA release from pre-synaptic terminals (potentiate effects of endogenous NA) CNS y Wakefulness y Psychomotor activity y Respiratory stimulation y Appetite

Therapeutic Uses Shock BP Not used for asthma, hypersensitivity Adverse Effects Cardiac arrhythmias Headache Hyperactivity Insomnia Nausea Tremors

Adrenergic Antagonists (Sympatholytics) Central Acting Clonidine, Methyldopa Acts on central 2 receptors ( sympathetic outflow from brain vasopressor center) Presynaptically, 2 receptor on adrenergic nerves noradrenalin release Uses Hypertension (newer agents preferred now)

-Receptor Blockers Prazosin (selective -blocker) Selective 1 receptor blockers Actions y Inhibit endogenous catecholamine induced vasoconstriction (cause arteriolar, venous dilatation) PVR, VR BP Activation baroreceptor reflex HR, Fluid retention Relaxation of bladder neck, prostate capsule, prostatic urethra (blockade 1) ( resistance to urinary flow)

-Receptor Blockers Propranolol (non-selective blocker) Atenolol, Metoprolol (selective 1 blocker) CVS Effects HR (due to sinus rate)(block 1) Myocardial contractility Myocardial O2 demand Slow conduction atria, AV node Block 1 receptors at JGA y Renin production y Angiotensin II Therapeutic Uses CVS Non-CVS Antihypertensive Hyperthyroidism Anxiety states (Angina pectoris) Glaucoma Anti-arrhythmias Myocardial infarction Conditions with sympathetic manifestation

Therapeutic Uses Hypertension Benign Prostatic Hypertrophy (BPH ) (alternative to surgery) Adverse Effects Reflex tachycardia, arrhythmias st Postural hypotension 1 dose effect Sexual dysfunction Nasal congestion Na+, H2O retention

Adverse Effects Bronchoconstriction (asthmatic, COPD) Affect recovery from hypoglycaemia in diabetes (inhibit glycogenolysis, glucagon release) Mask warning signs of hypoglycaemia Bradycardia Sexual dysfunction Hyperlipidaemia Sleep disturbances Postural hypotension (lesser) Fatigue Drowsiness Effects on Eye Intraocular pressure (IOP) (esp. glaucomatous eyes) MOA - Aqueous humor production ( adrenoceptors on ciliary epithelium facilitate aqueus humor secretion from ciliary epithelium)