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