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73 Cards in this Set
- Front
- Back
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Vincristine, Vinblastine, Colchicine, Paclitaxel
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Blocks Axonal Transport in Cholinergic(Ach) System. Causes side effects and decreases Ach effectiveness
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Local Anesthetics
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Prevents depolarization of cholinergic neurons which prevents NT release. Decreases Ach effectiveness
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Lecithin
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Phospholipid form of choline. Also called Phosphatidylcholine. Has quarternary ammonium group
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Synthesis of choline
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Primary MECH - high and low affinity transport systems
Secondary MECH- can be synthesized from serine |
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a-larotoxin
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Black Widow spider venom - binds to neurexins and causes explosive release of Ach. Increases effectiveness of Ach
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Botulinum Toxin (Botox)
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Inhibits Ach release - Decreases Ach effectiveness
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2 branches of Cholinergic Nervous System
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1) Nicotinic
2) Muscarinic |
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Varenicline Tartrate (Chantix)
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-Partial agonist @ a4b2 nicotinic receptors. Mitigates withdrawal symptoms of smoking cessation and produces pleasurable response.
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Polycyclic Aromatic Hydrocarbons
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-Consist of fused benzene rings
-CYP450 reacts with benzopyrene structure --> epoxide --> hydrolized-->epoxidized again. Intercalates between DNA bases --> Cancer |
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Zyban (Bupropion)
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Antidepressant that aids in smoking cessation
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NNK
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Most potent nitrosamine
Major cause of lung cancer |
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Methacholine (Provocholine)
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-Muscarinic Agonist
-Addition of Beta methyl group -Contains chiral center S form = equipotent with Ach and hydrolyzed half as fast; R form = 1/20 as active and not hydrolyzed at all |
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Carbachol (Isopto Carbachol)
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-Muscarinic Agonist
-Stable carbamate ester --> resistant to hydrolysis -Poor inhibitor of Ach -Has nicotinic activity @ autonomic ganglia -Activity due to release of ACh |
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Bethanechol Chloride (Urecholine and Duvoid)
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-Muscarinic Agonist
-Beta position methyl group -Resistant to hydrolysis due to methyl group and carbamate ester -Selective for GI tract and urinary bladder motility |
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Pilocarpine (Isopto Carpine)
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-Muscarinic agonist
-Contains basic imidazole ring that is protonated (+) -Can undergo hydrolysis and epimerization to form inactive -Contains ester like ACh -Used to treat xerostomia, urinary retention, glaucoma |
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(-)-Hyoscyamine
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-Naturally occurring muscarinic antagonist
- Epimerized to Atropine (different positions at chiral center) -Has unusually high acidic hydrogen due to alpha position to a carbonyl and it is next to the benzene group |
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Atropine
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-Tertiary amine
-Epimer of (-)-Hyoscyamine -Used to dilate the pupils -Side effects include dizziness, drowsiness, nervousness, constipation, delayed gastric emptying, xerostomia, urinary retention, blurred vision and dry eyes |
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Scopolamine
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-Naturally occurring muscarinic antagonist
-Contains epoxide group -Used to prevent motion sickness |
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Donnatal
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-Antimuscarinic Agent
-Gastrointestinal antipasmodic formed from a mixture of phenobarbital and atropine or scopolamine |
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Ipatropium Bromide (Atrovent)
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-Antimuscarinic Agent
-Quarternary analog of atropine(contains isopropyl group on N) -Doesnt cross BBB -More potent than atropine -Major use is COPD |
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Methscopolamine Bromide (Pamine)
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-Antimuscarinic Agent
-Quarternary analog of scopolamine -Treatment of peptic ulcer disease |
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Clindium Bromide
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-Antimuscarinic Agent
-Quarternary compound -Treatment of peptic ulcer disease |
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Glycopyrrolate Bromide(Robinul)
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-Antimuscarinic Agent
-Quarternary Agent -Used to treat peptic ulcer disease |
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Mepenzolate Bromide (Cantil)
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-Antimuscarinic Agent
-Phenyl ring instead of cyclopentyl group -Quarternary agent used in peptic ulcer disease |
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Propantheline Bromide (Probanthine)
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-Antimuscarinic Agent
-Cyclic R1 and R2 groups fuzed to form tricyclic compound -Most widely used nonselective synthetic muscarinic antagonist |
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Benztropine Mesylate (Cogentin)
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-Tertiary amino antimuscarinic
-Readily penetrates the CNS -Aminoether readily penetrates BBB -Useful in treating Parkinsons |
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Biperiden HCl (Akineton)
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-Tertiary amino antimuscarinic
-Readily penetrates CNS -Aminoalcohol on it -Used in early Parkinsonism |
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Procyclidine HCl (Kemadrin)
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-Tertiary amino antimuscarinic
-Readily penetrates CNS -Aminoalcohol on it -Used in early Parkinsonism |
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Trihexyphenidyl HCl (Artane)
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-Tertiary amino antimuscarinic
-Readily penetrates CNS -Aminoalcohol on it -Used in early Parkinsonism |
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Tiotropium Bromide (Spiriva)
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-Quarternary Antimuscarinic Agent used to reverse increased vagal tone in treatment of COPD
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Flavoxate HCl (Urispas)
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-Tertiary Aminoester used to treat overactive bladder/ urinary incontinence
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Tolterodine Tartrate (Detrol)
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-Nonselective competitive muscarinic antagonist used to treat overactive bladder/ urinary incontinence
-Tertiary Amine |
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Fesoterodine Fumarate (Toviaz)
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-Ester prodrug form of Tolterodine
-Increased antagonist activity by hydrolysis of the ester -Used in overactive bladder/ urinary incontinence |
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Oxybutynin Chloride (Ditropan)
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Synthetic Tertiary Amine
Used in overactive bladder/ urinary incontinence |
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Tropsium Chloride (Sanctura)
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-Quarternary ammonium antimuscarinic agent used to treat overactive bladder
-Low absorption from GI tract -Not metabolized by CYP enzymes |
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Darifenacin (Enablex)
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-Tertiary amine that is antimuscarinic agent used to treat overactive bladder
-Highly selective for M3 receptors -Small inhibition of salivary glands |
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Solifenacin (VESIcare)
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-Tertiary Amino agent used in overactive bladder/ urinary incontinence
-Increased selectivity for bladder over salivary glands |
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Ketoconazole
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-CYP3A4 inhibitor that can cause drug interactions with drugs that are metabolized by CYP3A4 enzymes
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Tubocurarine
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-Monoquarternary and monotertiary amino nicotinic agent
-Competitive neuromuscular blocker -Hydrate |
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Metocurine Iodide (Metubine Iodide)
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-Bi-quarternary amino compound
-Analog of Tubocurarine -Type of tubocurarine neuromuscular blocker -Has additional methyl ether group -More potent than Tubocurarine -Causes less histamine release and ganglionic blockade (GOOD!) |
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Ammoniosteroids
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-Second class of competitive neuromuscular blockers
-Derivatives of malouetine - arrow poisoning -All 3 aminosteroids contain 2 positively charged centers -Pancuronium, Vecuronium, Rocuronium |
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Benzylisoquinolines
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-3rd class of neuromuscular nicotinic blockers
-Derivatives of papaverine |
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Atracurium Besylate (Tracrium)
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-Dimer of reduced papaverine
-Linked by alkyl substituent that contains two ester groups |
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Sulfonic acid salts
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-Methanesulfonic Acid (Mesylate)
-Benzenesulfonic Acid (Besylate) -Toluenesulfonic Acid (Tosylate) |
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Mivacurium Chloride (Mivacron)
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-Benzylisoquinoline Derivative
-Undergoes ester hydrolysis b/c beta hydrogen is not adjacent to carbonyl group |
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Doxacurium Chloride (Nuromax)
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-Benzylisoquinoline Derivative
-Undergoes hydrolysis more slowly and has longer duration of action than atracurium |
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Cisatracurium Besylate (Nimbex)
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-Neuromuscular Blocker
-Benzylisoquinoline Derivative -Single isomer (atracurium has 10 |
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Hexamethonium
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-six carbon analogue
-Depolarizing neuromuscular blocker -Ganglionic blocker |
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Decamethonium
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-ten carbon analogue
-Depolarizing neuromuscular blocker -Neuromuscular blocker |
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Succinylcholine Chloride (Anectine)
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-Leptocurares
-10 atoms between 2 quaternary nitrogens -Ester groups make it incompatible with alkaline solutions such as barbituate salts -Decomposes at pH greater than 4.5 -Can cause malignant hyperthermia when interacted with general anesthetic |
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Mecamylamine (Inversine)
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-Only ganglionic blocker used (rare)
-Bicyclic -Used in hypertension -Low doses show efficacy in depression and smoking cessation |
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Physostigmine Salicylate (Antilirium)
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-Phenolic carbamate used as AChE inhibitor
-Transfer carbamate group more readily than aliphatic alcohols -Tertiary amine (Advantage b/c can penetrate CNS) -Used in anticholinergic overdoses |
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Neostigmine Bromide (Prostigmin)
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-Has carbamate and tertiary ammonium
-More chemically stable than physostigmine therefore has longer duration of action |
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Pyridostigmine Bromide (Mestinon)
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-Quarternary nitrogen in neostigmine has been brought into the aromatic ring
-Gives it steadier effects, longer duration of action and decrease in side effects -Used to treat myasthenia gravis |
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Demecarium Bromide (Humorsol)
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-Two neostigmine molecules bonded together
-Second quaternary group binds at site near gorge of active site |
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Ambenonium Chloride (Mytelase Chloride)
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-Non-carbamate inhibitor that binds to AChE and makes use of second anionic site within active site gorge
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Edrophonium Chloride (Tensilon)
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-Contains no carbamate group; instead contains hydroxyl group
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Tacrine-Cognex
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-Alzheimer's treatment
-Cholinesterase Inhibitor which binds reversible with and inactivates cholinesterase which inhibits the hydrolysis of acetylcholine -Very lipophilic so more readily enters CNS |
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Donepezil Hydrochloride (Aricept)
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Inhibitor of acetylcholinesterase used in treatment of Alzheimers
-More potent that Tacrine which leads to longer half lives and once daily dosing |
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Rivastigmine Tartrate (Exelon)
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-Carbamate derivative used to inhibit acetylcholinesterase in the treatment of Alzheimers
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Galantamine Hydrobromide (Razadyne)
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-Reversibly inhibits acetylcholinesterase and allosterically binds to nicotinic receptors
-Used in Alzheimers treatment |
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Memantine (Namenda)
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-Used in Alzheimers treatment
-NMDA antagonist (glutamate) -Decreases excitotoxcity of NMDA receptor activation -Additional benefit with Donepezil |
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Echothiophate (Phospholine Iodide)
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-Organophosphate
-Opthalmic Agent -Quaternary group directs compound into active site and prevents it from leaving the eye |
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Isoflurophate (Floropryl)
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-Organophosphate used in the eye
-Used to treat glaucoma |
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Pralidoxime Chloride (Protopam)
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-Weakly acid oxime portion displaces electrophilic phosphoruous atom bonded to serine-203
-Used to treat poisoning(pesticides) in children |
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Cevimeline Hydrochloride (Evoxac)
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-Marketed to treat xerostomia in patients with Sjogren syndrome
-Agonist activity at M3 receptors Initially developed as cholinergic cognition enhancer for Alzheimers |
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a-Methyl p-Tyrosine Metyrosine (Demser)
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-Competitive inhibitor of tyrosine hydroxylase which prevents formation of catechol
-Used to prevent pheochromacytomia |
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a-Methyldopa (Aldomet)
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-Originally developed as inhibitor of L-aromatic amino acid decarboxylase which prevents formation of dopamine.
-Doesn't completely inhibit the enzyme instead is a substrate for the enzyme |
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Disulfiram (Antabuse)
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-Tried as antihelminitic agent (worms)
-Inhibits acetaldehyde dehydrogenase which leads to an increase in acetaldehyde -Alcohol is broken down to acetaldehyde so when taken with this drug can lead to nausea, vomiting, palpitations, and even death |
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Rauwolfia Alkaloids (Reserpine)
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-Affects catecholamine NT storage
-Inhibit the ATPase dependent transport of dopamine and norepinephrine into storage vesicles |
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Guanethidine Monosulfate (Ismelin Sulfate)
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-Drugs that binds to sites within storage vesicles to inhibit storage process in catecholamines
-Used to treat hypertension and renal hypertension |
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Guanadrel Sulfate (Hylorel)
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-Antihypertensive agent
-Drugs that binds to sites within storage vesicles to inhibit storage process in catecholamines -Also depletes norepinephrine storage -Acts as false neurotransmitter |
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Bretylium Tosylate (Bretylol)
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-Originally developed as antihypertensive agent
-Now used as antiarrhythmic agent -Catecholaminergic drug -Poor oral absorption to to quaternary amine |
