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Pharmacology N225B: Review, Spring 2008Review, Spring 2008
UCLA School of NursingSophie Sokolow, PhD, MPHARM
Factor 6-266
Peripheral Nervous system
Anatomi para simpatis & simpatis
Peripheral nervous system
Somatic motor systemConscious control ofmovement, respiration, postureFunction:
Autonomic nervous systemInvoluntary control of visceral functions. Parasympathetic Sympathetic nervous systemsFunction:
Control Skeletal muscle via neuromuscular junction
Sympathetic nervous systems
3 principal functions:1. Regulate Heart 2. Regulate Secretory glands (salivary, gastric, sweat, bronchial)
3. Regulate Smooth muscles (bronchi, blood vessels, urogenital, GI)
Autonomous Nervous system
Anatomic considerations
Figure 13-3 The basic anatomy of the parasympathetic and sympathetic nervous systems and the somatic motor system.
Locations of cholinergic and adrenergic receptor subtypes
Figure 13-6
Neurotransmitters
Norepinephrine(NA,
adrenergic)
Practically all SNS post-
ganglionic neurons (except sweat
Acetylcholine (Ach,
cholinergic)
All PNS pre-ganglionic
neurons ganglionic neurons (except sweat
glands)
Epinephrine
Released from Adrenal
medulla
neurons
All PNS post-ganglionic
neurons
All SNS pre-ganglionic
neurons
Most SNS post-ganglionic
neurons to sweat glands
All motor neurons to skeletal
muscles
Parasympathetic (PNS)/ Sympathetic nervous (SNS) systems
PNS (Cholinergic)7 functions1. HR 2.gastric secretion
SNS (Adrenergic)3 functions1. Regulating cardiovascular system 2.gastric secretion
3.Emptying of bladder4.Emptying of bowel5.Focusing for near vision6.Constriction pupils (miosis)
7.Bronchoconstriction
system 2. Regulating body temperature3. Implementing fight-or-flight reaction
HR and BPDilate pupils (mydriasis)Dilate bronchiMobilize stored energy
SNS vs. PNS functions
CholinergicAdrenergic
Cholinergic drugs
Direct cholinomimetics
Cholinergic Receptor subtypes
Muscarinic receptors CNS PNS postganglionic endings
Sweat glands
Nicotinic receptors CNS Autonomic ganglia Neuromuscular junction Adrenal medulla Sweat glands Adrenal medulla
Cholinergic Drugs: direct cholinomimetics
MOA: enhance transmission at cholinergic synapsesDrugs:Acetylcholine limited because of short duration ofactionMuscarinic agonistsMuscarinic agonists1.Muscarine: mushroom alkaloid used to discoversubtypes
2.Bethanechol (Urecholine) Treatment of urinary retention Also increases GI motility
3.Pilocarpine Glaucoma
Nicotine
Natural liquid alkaloidMOA: Stimulates nicotinic receptors CNS and CV effectsDrugs:
Varenicline (Chantix):Varenicline (Chantix): Nicotinic partial agonist for smoking cessation
Cholinergic Drugs
Cholinesterases Inhibitors
Anticholinesterase drugs Indirect acting cholinomimetics
MOA: inhibit the enzyme that degrades acetylcholineDrugs and Clinical uses:Reversible agents
Edrophonium (Tensilon)
Myasthenia Gravis
Donepezil (Aricept), Tacrine (Cognex)
Alzheimers disease
Irreversible agentsEchothiophate (phospholine iodide)
GlaucomaMalathion, sarin (nerve gas, no clinical use)
Anti-Cholinergic Drugs
Muscarinic Antagonists
Anti-cholinergic drugs: Muscarinic Antagonists
Agents:Atropine
Clinical uses: Motion sickness
MOA: Block muscarinic receptors
AtropineScopolamine Ipratropium bromidePropantheline Trihexyphenidyl Benztropine...
Motion sicknessAsthmaIncontinence (OAB)AntispasmodicBradyarrhythmiasAnti-parkinsonPreoperativeOpthalmology
Overactive Bladder (OAB) Therapy
Anti-muscarinic agents:Nonselective (block M2 and M3 receptors)Tolterodine (Detrol); older
M3 selective (block M3 receptors, most M3selective)selective)Oxybutynin (Ditropan)Solifenacin (Vesicare)Darifenacin (Enablex)
Anti-Cholinergic Drugs
Neuromuscular blocking agents
Neuromuscular blocking agents
MOA:Block nicotinic receptors at neuromuscular junctionNo CNS effects!Drugs and Clinical uses:Relaxation for surgical procedures, intubationRelaxation for surgical procedures, intubationNon-depolarizing:
Tubocurarine, pancuronium bromide (Pavulon),vecuronium, cisatracurium
Rapid hydrolysis by AChE; NM block lasts 5-10 min
Depolarizing (persistent depolarization makes themuscle fiber resistant to further stimulation byACh)
Succinylcholine (Anectine)
Botulinum toxin
Produced by Clostridium botulinumMOA:Act pre-synaptically inhibit ACh release at the NMJ cause temporary local paralysis of injected muscleEffects last weeks to several monthsEffects last weeks to several monthsClinical Use:FDA Approved for limited disorders (i.e. strabismus, severe primary axillary hyperhidrosis, cervical dystonia)
Worlwide 21 indications are approved for BotoxUnder FDA investigations for several disorders:
Chronic migraineLimb Muscle pain, Back painOAB, etc.
Cosmetic use: treat frown lines between the brows
Adrenergic Agonists
Beta1Heart
Heart rate Force of contraction Velocity of conduction in
Main Functions of Adrenergic Receptor Subtypes
Alpha1Vasoconstriction
Alpha2Located in presynaptic junction Velocity of conduction in
AV nodeKidney
Renin release
Beta2Bronchial dilationRelaxation of uterine muscleVasodilationGlycogenolysis
junctionMinimal clinical significance
DopamineDilates renal blood vessels
Sympathomimetic drugs: catecholamines
1.Epinephrine1 cardiac stimulation2 bronchodilation constriction of arterioles
2.Isoproterenol (-selective)
1 cardiac stimulation
2 bronchodilation
2.DobutaminearteriolesClinical Use: Acute hypersensitivity reactions
Cardiac stimulant
2.Dobutamine1 cardiac stimulation(some 1)
Clinical Use: Increase contractility and cardiacoutput in hypotension and surgery
Sympathomimetic drugs: catecholamines (cont)
4.Norepinephrine(Levophed)
vasoconstriction1 cardiac stimulation
5.Dopamine
MOA:Stimulates dopamine receptors
1 cardiac stimulation
Clinical Use:Hypotension
Stimulates dopamine receptors vasodilation of renal and mesenteric arteries
Clinical Use:Hypotension and shock
Sympathomimetic drugs: Non-Catecholamines
1.1.1.1. 2 selective agonists Terbutaline (Brethine) Albuterol (Proventil, Ventolin)
Ritodrine
2.2.2.2. 1 selective agonists Phenylephrine
3.3.3.3. 2 selective agonists Clonidine (Catapres)
Ritodrine
4.Miscellaneous adrenergic agonists Amphetamine, Methylphenidate Ephedrine Phenylpropanolamine Cocaine
Adrenergic Antagonists
Adrenergic Receptor Antagonists1 selective antagonists
Drugs and Clinical uses:HypertensionPrazosin (Minipres)Doxazosin (Cardura)Terazosin (Hytrin)
Non selective antagonistsDrugs and Clinical uses: Pheochromocytoma
PhenoxybenzamineTerazosin (Hytrin)
Benign Prostatic Hypertrophy (BPH)Tamsulosin (Flomax)selective for prostate smoothmuscle vs. vascular smooth muscle
Other agent used in BPH therapy:Finasteride (Propecia): has different MOA blocks 5- reductase blocks conversion of testosterone to dihydroxytestosterone
PhenoxybenzaminePhentolamine
Adrenergic Receptor -Antagonists: : : : -blockers
Nonselective 1 and 2Propranolol (Inderal)Nadolol (Corgard)
Selective 1(cardioselective)
Partial agonistsBlockers with intrinsic sympathomimetic activity (ISA)PindololAcebutolol: depress heart rate
(cardioselective)Metoprolol (Lopressor) Atenolol (Tenormin)
GlaucomaTimolol (timoptic)Carteolol (occupress) oral or drops
Acebutolol: depress heart rateless than other -blockers
Nonselective -blockade with blockadeLower BP without alterations in heart rate or cardiac outputLabetololCarvedilol
Adrenergic Receptor -Antagonists
3.3.3.3. antagonists (-blockers)
Clinical uses: Hypertension Angina Myocardial Infarction (MI) Myocardial Infarction (MI) Cardiac Heart Failure (CHF) Antiarrhythmics Migraine Pheochromocytoma Glaucoma
Respiratory Pharmacology
Drugs used in the treatment of COPD
1. Bronchodilators short acting (as initial agents):a)Anti-cholinergics (ipratropium bromide), 1st linebronchodilatator alone or in combination with b.
b)2-agonists (albuterol),
2. Bronchodilators long acting (are added to 1.) :a) -agonists (salmoterol, formoterol),a) 2-agonists (salmoterol, formoterol),b)Anti-cholinergics (tiotropium bromide)c) Theophylline
3. Corticosteroids ( of acute COPDexacerbations or chronically in severe patients):a)Oral (prednisone, prednisolone)b)Inhaled (fluticasone, beclomethasone, budesoinde), lessprominent role than in asthma
4. Others (antibiotics, mucolytics, expectorants)