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Acetylcholine(MIOCHOL-E)
- Choline ester, N, M Agonist
- Metabolism: Ach.esterase, Psudoesterase
- Therapeutic use: production of miosis during ophthalmic surgery (MIOCHOL-E)
- 5-10s 1/2 life, IM, SubQ for local effects
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Methacholine(PROVOCHOLINE)
- Choline ester, Selective M Agonist, little activity on N receptor
- Metabolism: more resistant to Ach.esterase
- Therapeutic use: diagnosis of bronchial hypersensitivity
- Systemic use is limited due to cardiovascular effects, Longer 1/2 life
-
Carbachol(CARBOPTIC)
- Choline ester, Selective N Agonist
- Metabolism: completely resistant to Ach.esterase
- Therapeutic use: wide angle glaucoma
- Greater effects on S.M. of eye, GI, urinary bladder than cardiovascular S.M.
-
Bethanechol(URECHOLINE)
- Choline ester, Selective M Agonist (Spe. GI, urinary)
- Metabolism: completely resistant to Ach.esterase and pseudoesterase
- Therapeutic use: stimulates GI and urinary bladder
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Muscarine
- Cholinomimetic alkaloids
- Only M Agonist
- No therapeutic application
- from Amanita muscaria
-
Nicotine
- Only N Agonist
- Therapeutic use: smoking cessation
- Has been used as an insecticide
-
Pilocarpine(SALAGEN, PILOCAR)
- Selective M Agonist
- Therapeutic use: xerostomia, ophthalmic solution for side angle glaucoma
- Derived from the Pilocarpus
-
Physostigmine(eserine)
- Reversible Carbamate Ach esterase inhibitors
- Therapeutic use: wide angle glaucoma, antidote for atrpine toxicity
- Lipophilic, 0.5-2hr 1/2 life, ordeal poison
-
Neostigmine
- Reversible Carbamate Ach esterase inhibitors
- Therapeutic use: Myasthenia gravis, stimulation of atonic S.M. of GI and urinary bladder, Reversal of neuromuschular blockade induced by curare, pancuronium, and skeletal muscle relaxant
- Stimulates Nm receptors in skeletal muscle
- No CNS effect (charged), 0.5-2hr 1/2 life
-
Pyridostigmine, ambenonium, demacarium
- Reversible Carbamate Ach esterase inhibitors
- Therapeutic use: myasthenia gravis
- Stimulates Nm receptors in skeletal muscle
- No CNS effect, 3-8hrs
-
Edrophonium
- Reversible noncarbamate Ach esterase inhibitors
- Therapeutic use: diagnosis of myasthenia gravis
- Stimulates Nm receptors in skeletal muscle
- Quick onset, short duration (5-15min)
-
Galantamine, Tacrine
- Reversible noncarbamate Ach esterase inhibitors
- Therapeutic use: Alzheimer's disease
-
diisopropylfluorophosphate(DFP)
- Irreversible organophosphate Ach esterase inhibitors
- Therapeutic use: glaucoma (ointment)
- lipid soluble, low MW, volatile = inhalation and transdermal, last 4 weeks, retina detachment and cataracts possible
-
ecothiophate
- Irreversible organophosphate Ach esterase inhibitors
- Therapeutic use: glaucoma
- aqueous solution, no CNS, last 4 weeks
-
parathion
- Irreversible organophosphate Ach esterase inhibitors
- converted to paraoxon-active metabolite
- Use: insecticide (not used anymore)
-
malathion(Chemathion, Mala-spray)
- Irreversible organophosphate Ach esterase inhibitors
- converted to malaoxon
- Use: insecticide, for lice (safe due to plasma carboxylesterase in mammals)
-
sarin, tabun, soman
- Irreversible organophosphate Ach esterase inhibitors
- Use: nerve gas
-
Pralidoxime (2-PAM)
- causes hydrolysis of the organophosphate from Ser of Ach esterase
- Therapeutic use: reverses Irreversible organophosphate Ach esterase inhibitors
-
Atropine
- competitive muscarinic antagonist
- Therapeutic use: to induce mydriasis, cylcloplegia, prevent respiratory secretions during surgery, Parkinson's disease, Decrease AV node block when vagal tone is hihg, antidote for Achesterase inhibitors, diarrhea (with Diphenoxylate)-Lomotil
-
Scopalamine
- competitive muscarinic antagonist
- Therapeutic use: Prevents motion sickness
- CNS effects
-
Glycopyrrolate
- competitive muscarinic antagonist
- Therapeutic use: inhibit GI motility, Peptic ulcer, Reduce salivation and bronchial secretion during surgery
-
Propantheline
- competitive muscarinic antagonist
- Therapeutic use: prevent spasms of GI smooth muscle, peptic ulcer
-
Prienzepine
- competitive muscarinic antagonist
- Therapeutic use: inhibits gastric acid secretion
- Selective for M1 and M4
-
Ipratropium
- competitive muscarinic antagonist
- Therapeutic use: chronic obstructive pulmonary disease (aerosol), rhinorrhea associated with common cold
-
Oxybutynin
- competitive muscarinic antagonist
- Therapeutic use: relieve bladder spasms following urologic surgery(prostatectomy), incontinence with neurologic diseases
-
Tolterodine(Detrol)
- competitive muscarinic antagonist
- Therapeutic use:incontinence
- Selective for M3
-
Opthamology(mydriasis, cycloplegia) M receptor antagonists
- Atropine: 7-10 days
- Scopalamine: 3-7 days
- Homatropine: 1-3 days
- Tropicamide: 0.25 days
-
M receptors
- M1: neurons, some glands, CNS
- M2: myocardium, smooth muscle, CNS
- M3: smooth muscle, glands, endothelium, CNS
- M4: smooth muscle, glands, CNS
- M5: CNS
- GPCR
-
Direct-Acting Sympathomimetic Drugs
a1
- Epi, NorEpi
- Phenylephrine
- Methoxamine
- Mephentermine
- Metaraminol
- Midodrine
-
Direct-Acting Sympathomimetic Drugs
a2
- Epi, NorEpi
- Peripheral: Oxymetazoline, Tetrahydrozoline, Naphazoline
- CNS: a-Methyldopa, Clonidine, Guanabenz
- apraclonidine
- Guanfacine
- bromidine
-
Direct-Acting Sympathomimetic Drugs
b1
- Epi, NorEpi, Isoproterenol
- Dobutamine
- Dopamine
-
Direct-Acting Sympathomimetic Drugs
b2
- Epi, Isoproterenol
- Terbutaline
- Albuterol
- Levalbuterol
- Bitolterol
- Ritodrine
- Salmetertol
- formoterol
-
Amphetamine/methamphetamine
- Orally active
- CNS effects
- MOA: induce the relase of NorEpi
- Increase BP, decrease CO by baro
- Meth has greater CNS effects over Am
- Uses: suppress appetite(Dexedrine), narcolepsy, ADHD, cocaine-dependece, reverse fatigue, increase altertness
-
Methylphenidate (Ritalin)
- orally active, sig. for abuse
- Uses: ADHD, narcolepsy
-
Tyramine
- Metabolite of tyrosine in fermented foods, not a therapeutic drug
- Caution with MAO inhibitors
- MOA: induces the release of NorEpi
- Foods: Cheese, Meat, Fruit(figs, raisins), Fermented beverages (beer, wine), soy sauce, yogurt
-
Tricyclic antidepressants
- desipramine, imipramine, amitriptyline, clomipramine, nortriptyline, cocaine
- MOA: prevent reuptake of NorEpi, also inhibits reuptake of serotonin and dopamine
-
Cocaine
MOA: prevent reuptake of NorEpi, also inhibits reuptake of serotonin and dopamine, blocks VG Na channels (anesthetic for opthamology)
-
Monoamine oxidase inhibitors
- Phenelzine, Tranylcypromine, Isocarboxazid, Pargyline, Selegeline
- Selegeline is MAO B selective
- MOA: Inhibit MAO irreversibly
- Danger of fatal hypertensive crisis: Tyramine, Methylphenidate, Amphetamine, Meth, Tri. antidepressants
-
Ephedrine
- Agonist at a and b
- Enhances release of NorEpi
- orally effective, Increase CO, BP=stroke!
- Uses: Asthma (decrease likelyhood of acute asthma attack), Nasal congestion, Enhance athletic performance, Weight loss
-
Pseudoephedrine (Sudafed)
- Weak agonist at a, no activity at b
- Enhances release of NorEpi
- Uses: Nasal congestion
-
Phenylpropanolamine
- Agonist at a but little activity at b
- Enhances release of NorEpi
- Uses: Nasal congestion and weight loss
- Discontinued due to hemorrhagic stroke
-
Cariovascular
- Cardiac Arrest: Epi, dobutamine
- Cardiogenic Shock: dopamine, dobutamine
- Cariac arrhythmias: AV node block=isoproterenol, paroxysmal atrial tachycardia=phenylephrine, methoxamine
- Hypotension: phenylephrine, methoxamine, norepinephrine
- Essential Hypertension: clonidine, guanabenz, a-methyldopa
-
Respiratory (asthma, COPD)
- Short acting: albuterol, rebutaline, metaproterenol, epinephrine (<1hr)
- Long acting: salmeterol (12hr)
-
Nasal Congestion
pseudoephedrine, ephedrine, phenylephrine, oxymetazoline, naphazoline
-
Uterus
Delay premature labor: ritodine, terbutaline
-
Ophthalmic
- Induce mydriasis: phenylephrine
- Wide angle glaucoma
- Ocular congestion: phenylephrine, tetrahydrozoline
-
Anaphylactic shock
- Epi(b2)
- Severe allergic reactions
-
Increase duration of action of local anesthetics
Epi
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