Adrenergic and Cholinergic Drugs

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Adrenergic and Cholinergic Drugs by Mind Map: Adrenergic and Cholinergic Drugs

1. Cholinergics

1.1. Cholinomimetic

1.1.1. Direct acting Muscarinic Choline Esters Alkaloids Nicotinic

1.1.2. Indirect acting-inhibits ACHe Short acting-usually alcohol types (-OH) Duration of Action: 15-30 mins ⚫ Chemical: Aminoalcohol ⚫ Interaction with Acetylcholinesterase: Reversible Intermediate acting(-STIGMINE) Duration of Action: 2-8 hours ⚫ Chemical: Carbamates ⚫ Interaction with Acetylcholinesterase: Reversible Long acting Duration of Action: > 24 hours ⚫ Chemical: Organophosphates ⚫ Interaction with Acetylcholinesterase: Reversible (1-2 days); Irreversible (>48 hrs)

1.2. Parasympatholytics/Cholinergic Antagonists

1.2.1. Antimuscarinic Non selective Atropine M1-selective Pirenzepine

1.2.2. Antinicotinic Ganglion (Nicotinic) blockers Hexamethonium, Trimetaphan, Mecamylamine Neuromuscular blockers Tubocurarine

1.2.3. Cholinesterase regenerators Oximes Pralidoxime

1.3. Other Drugs: Based on Site of Action

1.3.1. CNS-FOR PARKINSONS Scopolamine Motion sickness Benztropine,Bipyriden, and trihexyphenidyl

1.3.2. Eyes Homatropine,Anistropine,Cyclopentolate, Tropicamide

1.3.3. Bronchi- for Asthma and COPD Ipratropium Tiotropium Aclidinium – Long-acting

1.3.4. GIT Pirenzepine & Telenzepine – M1 selective blocker Methscopolamine, Propantheline – obsolete for acid-peptic disease

1.3.5. Urinary Bladder-Urinary incontinence ⚫ Methscopolamine, ⚫ Scopolamine ⚫ Dicycloverine ⚫ Hyoscine-MOST USED ⚫ Oxybutynin ⚫ Glycopyrrolate

2. Adrenergic

2.1. Direct Acting- directly binds to Adrenergic receptors

2.1.1. Non selective sympa(NE,EPI,DOPA) NE Inotropic agent for septic shock EPI Cardiac stimulant(b1), Anaphylaxis (b2), local vasoconstrictor(longer anesthetic action, glaucoma mngmt DOPA 1-3 ug/kg/min: d1,inc gfr and diuresis 2-5 ug/kg/min: b1, inc inotropy,chrono,dromo >5ug/kg/min:a1, vasoconstriction Dopa toxicity: -> Alpha-1 Overstimulation = vasoconstriction -> Beta -1 Overstimulation = Tachyarrythmias (Increased HR with irregular heart rhythm) Management of cardiogenic shock and septic shock; Management of Acute HF with Oliguria or Anuria

2.1.2. Selective sympa Non selective b agonist(activates both b1 and b2) Isoproterenol/isoprenaline Selective b1 agonist Dobutamine Selective b2 agonist Short acting (SABA) Long acting (LABA) Tocolytics Selective a1 agonist Phenylephrine, Propylhexedrine Methoxamine, Naphazoline, Oxymetazoline, and Tetrahydrozoline Selective a2 agonist Effects: ✔ Pre-synaptic: autoregulation –self-regulating • Central: Sedation, Depression • Peripheral: Vasodilation ✔ Post-synaptic: vasoconstriction Selective d1 agonist Fenoldopam

2.2. Indirect Acting- inc SE by inc NE release and NE reuptake inhibition

2.2.1. Release NE through exocytosis Ex: Tyramine, Ephedrine, Amphetamine, Alpha-latrotoxin, Angiotensin II

2.2.2. ReuptakeInhibitors Ex: Cocaine, TCA, REBOXETINE(NE-Reuptake Inhibitor)

2.2.3. Side-effect of Ephedrine: o Hypertension Exacerbation o Precipitates urinary retention o Tachyarrhythmia

2.3. Centrally Acting- acts on cns

2.3.1. Phenylpropanolamine, Phentermine, Phenmetrazine, Amphetamine, Methylphenidate USES: 􏰀 Management of ADHD o 1st line: METHYLPHENIDATE o Alternative: AMPHETAMINE 􏰀 Anorexiants – APPETITE SUPPRESSANTS (Phentermine, Phenmetrazine, Phenylpropanolamine) 􏰀 Management of Narcolepsy –SLEEPINESS (Phentermine & AMPHETAMINE) Side Effects: o Risk of addiction o Risk of Hemorraghic Stroke (PHENYLPROPANOLAMINE) o Risk of Pulmonary Hypertension (PHENTERMINE)

2.4. Sympatolytics

2.4.1. Alpha blockers Effects: Vasodilation; Relief of urinary retention (difficulty in urination) Non selective a blockers Acts of alpha 1 and 2 receptors ⚫ Example: o Phenoxybenzamine (Irreversible or permanent blocker) o Phentolamine (Reversible blocker)-safer Mngmt of phaeochromocytoa Selective a1 blockers Acts on ALPHA 1 only (-zosins) ⚫ Example: o Alfuzosin o Doxazosin o Prazosin o Tamsulosin o Terazosin Mngmt of raynaud’s syndrome Mngmt of urinary retention in BPH Select a2 blockers

2.4.2. Beta blockers NS b blockers Block Beta-1 and Beta-2 receptors ⚫ Exhibits BRONCHOCONSTRICTION effect on the lungs. ⚫ Examples: (NSTP) ⚫ Nadolol ⚫ Sotalol ⚫ Timolol-glaucoma mngmt ⚫ Propranolol-hyperthyroidism,stage fright, prophylaxis of migraine Selective b1 blockers Examples: (CAMBABE) Celiprolol ⚫ Betaxolol-glaucoma mngmt ⚫ Bisoprolol-stable heart failure ⚫ Atenolol ⚫ Acebutolol ⚫ Metoprolol-stable heart failure ESMOLOL B blockers w/ intrinsic activity Contains alpha agonist effects B blockers w a1 blocking effect Labetalol and carvedilol Beta-Blockers with Membrane Stabilizing Action Includes local anesthetic effect