Exam 1 part 2
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| Mechanism of antidote 2PAM | regeneration of ACHE via hydrolysis of poison
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| What drugs produce a drastic dip in plasma ChE activity followed by a gradual increase | Isofluorophate and 2PAM (sarin and atropine)
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| What is the shortest acting for cycloplegia | tropicamide
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| Which is used to reduce broncho secretions and constriction to help treat asthma | ipratropium
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| What would you expect if you had a problem with pseudocholinesterase | succinylcholine
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| What are cholinergic receptors classified by | muscarine and nicotine
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| Two different drugs that can achieve increased heart rate | beta 1 agonist and muscarinic antagonist
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| What is the mechanism of myasthenia gravis | autoimmune reaction
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| what is sued to treat motion sickness | scopalamine
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| What does disulfiram inhibit | aldehyde dehydrogenase MEOS
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| what is used for long term alcohol abuse therapy | disulfiram, naltrexone, acamprosate
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| drug abuse by 8th graders | inhalants, maryjuana, cocaine, lsd
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| if young adults go to heroin replacement therapy what is the drug used | buprenorphine
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| what is true of buprenorphine | all of the above
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| the pharmacologic use of methadone is to give a dose as potent as heroin to satisfy opiate craving | false
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| drug class of choice for management of alcohol abstinence symptom | benzodiazepines
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| mechanism of psychomotor stimulant action of amphetamine is blockade of vesicular membrane dopamine transporter | true
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| what drug should a person experiencing cachexia take | dronabinol
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| elimination of alcohol is what order | zero
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| for stimulation of addication where is the release of dopamine from | ventral tegmental area
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| varenicline (chantix) is efficacious for smoking cessation because you can smoke it | false
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| Not FDA approved skin patch | GH, insulin
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| weak acid mostly not ionized at | 1 pH
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| Orphan drug act | gives incentive for pharms to make orphan drugs
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| user fee act | makes pharms pay for review fees at FDA
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| durham humphrey act | difference between RX and otc
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| 6 centers of FDA | drug eval, biologic eval, food safety, devices, vet meds, toxicology
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| drug induced orthostatic hypertension category | CV system
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| ibuprophen produces what CV symptom | edema
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| grapefruit juice is substrate of CYP3A4 | false
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| most common CYP | CYP3A4/5
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| role of cytochrome c reductase | reduce Fe3 to Fe2
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| sequence of events with P450 | drug binds to oxidized P450, complex is reduced, molecular oxygen binds to reduce complex
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| Components of P450 | heme, ferric ion 2+, cytochrome
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| first pass occurs in liver | true
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| efflux transporter in intestinal cells and capillary endothelium of brain capillaries | protein carbohydrate complex
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| Tetracycline side effect | stains kids teeth
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| simple diffusion based on lipophilic nature of drug | true
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| level of drug in blood to remain therapeutic | optimal therapeutic plasma level
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| dose azithromycin for patient | 500mg
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| risk of adverse effect to statin causing rhabdomyolysis | clarithromycin
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| alcohol is contraindicated | metronidazole
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| depends on absence of oxygen | metronidazole
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| CYP2D6 is inhibited by fluoxetine, what is substrate | codeine
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| phase of clinical trial to develop dose range | phase II
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| UGT stands for | Uridine glucuronosyl transferase
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| calcium pills plus tetracycline is what type of interaction | problem with absorption
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| diabetic drug plus aspirin is what interaction | protein displacement
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| prodrug used for anesthesia | fospropofol
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| Erythromycin inhibits CYP3A4/5 so metabolism of diazepam will increase | false
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| what is not a mode of excretion | hepatic metabolism
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| throbocytpenia is what category effect | hematologic
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| drug interaction between iron and tetracycline is | absorption effect
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| nanoscale definition | 1-100nm
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| eqn for Kel | 0.693/T1/2
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| calssification of caugh | respiratory effect
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| source of most drugs | chemical synthesis
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| classification of dizziness | CNS effect
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| who is tested for LD50 | mice
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| thalidomide is used to treat | multiple myeloma
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| lexicomp pharmacologic class of thalidomide | antineoplastic
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| technique to allow production of a lot of chemicals in a short time | combinatorial chemistry
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| discovered penicllin | Fleming
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| weak acids absorbed where | areas of lower pH
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| Not water miscible, semi solid | ointment
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| water miscible, semi solid | creams
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| water miscible, contains dissolved drug | topically applied gels
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| water miscible, medication oral | local orally applied gels
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| Parenteral liquid | drug that is injected, (ie dental anesthesia)
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| morphine is (more/less) potent than demerol | more
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| to form drug receptor complex it requires _____, to produce effect _______ | affinity, intrinsic activity
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| LDR curve shows what | efficacy, potency, ~mechanism of drug action
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| two drugs produce opposite effects | physiologic antagonism
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| competitive reversible antagonism curve shifts where | to the right
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| competitive irreversible antagonism curve shifts where | right and max effect decreases
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| onset time for intramuscular | ~5 mins
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| onset time for intravenous | ~10 secs
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| Onset time for subcutaneous | ~10-15 secs
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| efflux systems do what | export drug back to circulation
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| these nonpolar lipophilic groups are best at simple diffusion | ethyls, propyls, phenyls
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| Major eflux carrier in intestine and CNS capillary endothelium | P-glycoprotein
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| main drug excretion routes | pee, poo
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| main FDA function | ensure safety of drug for consumer
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| food drug act | 1906 first to establish guidlines
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| food drug cosmetic act | 1938 requires drug safety, clinical tests, makes FDA
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| kefauver harris act | 1962 requires proof of effectiveness in humans
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| controlled substances act | 1970 creates schedules
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| hatch waxman act | 1984 generics approved without testing
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| poison preventio act | 1970 save the children
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| fda modernization act | 1997 drugs that help with life threatening diseases get priority
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| drug safety oversight act | 2005 monitors drugs after release
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| 5 phases of drug development | synthesis of new chem, safety eval, effective eval, new drug app, post market survey
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| margin of safety | LD50/ED50
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| toxicity | cell damage/tissue damage, usually intolerable
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| side effect | undesired effect, usually tolerated
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| Issues with thalidomide | caused 20% abnormal offspring in europe in 1960s
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| phase I metabolism occurs where | liver
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| phase II metabolism is what | conjugate with glucuronic acid, excretion by kidney
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| Hydrolysis metabolizes | ester drugs
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| CYP2C19 | Substrate: diazepam Inhibitor: fluoxetine
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| CYP1A2 | substrate: theophylline Inhibitor: erythromycin
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| CYP2C9 | substrate: warfarin Inhibitor: metronidazole
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| Antiplatelet prodrug for thrombosis | clopidogrel
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| major drug interaction of the 1950s | phenobarbital and warfarin
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| easier to identify the peak dose in IV or oral drugs | oral
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| Ach is neurtransmitter for ____ while NE is NT for? | all ganglia, sympathetic target organs
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| exceptions to Ach/NE neurtransmitter rule | Adrenal medula doesnt ahve post ganglionic fibers, Sweat glands are innervated by SNS but transmitter is Ach, not NE
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| Acetyl CoA + Choline = | acetylcholine
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| subtypes of nicotinic receptors | NM (skeletal muscle), NN (Neuronal)
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| Ach binds to what subunit | alpha
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| Muscarinic subtypes | M1/3/5 (IP3/DAG), M2/4 (cAMP)
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| Action/Receptor for iris radial/dilator muscle | mydriasis, a1
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| action/receptor for iris circular/constrictor muscle | miosis, m3
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| In the heart, receptors B1/B2 _____ while M2 _____ | accelerates, decelerates
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| M3 receptor in respiratory system is ____ for asthma patient while B2 is _____ | bad, good
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| receptor in GI that causes movement | M3
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| Levels of acetycholine (which is direct acting) | acetylecholine, methacholine, carachol, bethanechol
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| Indirect acting cholinergic drugs do | inhibit activity of ACHE, allowing Ach to build up
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| what reverses irreversables | pralidoxime (pam/2pam)
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| can quaternary drugs make it to brain | no, stay in periphery
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| diagnostic tool for myasthenia gravis | edrophonium
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| treatment of myasthenia gravis | neostigmine, pyridostigmine, ambenonium, atropine
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| treatment of glaucoma | physostigmine, dysflos, eccothiopate
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| myocardial infarction can be treated with | atropine
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| nondepolarizing blocker does, while depolarizing does | blocks opening of channel, opens channel but blocks it up
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| botulinum toxin used for | treatment of hemifacial spasm
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| migraines with aura vs migraines without | 25 vs 75%
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| origin of migraines | vascular and nervous (trigeminal)
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| two phases of migrain | vasoconstriction, vasodilation
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| what enzymes are targets of drugs for alzheimers/parkins | COMT, DDC, MAO2 (all of above)
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| what needs to cross BBB to work for Alz/parks | selegeline
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| what combo therapy for alz is not reasonable | tacarine and donepezil
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| what is normal goal of alz treatment | preserve existing Ach
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| what is main goal of prophylactic 5HT-2 antagonists | prevention of vasoconstriction by seratonin
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| What is most common drug for acute migrains | sumatriptan
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| what is target of antagonists other than triptans | CGRP
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| rule for treatment of migrains | start simple
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| what causes alz | neuronal degeneratino/ neuritic plaques containing AB Amyloids and Tau rich neruofibrillary...protein misfolding/buildup
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| genes involved in alz | PS2/PS2/APP
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| ACEInhibitors for alz | T / D / R Hydrochloride, Galantamine
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| NMDA antagonists for alz | Memantine
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| Cardinal signs of parks | tremor, rigidity, bradykinseia, akinesia, posture instability
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| issue with parks | dopamine neurons dying
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