Pharm (Pre Mid-Term) Flashcards by Christine Hou

Metabolite drug is always ___polar, ____active that parent drug

more polar, less active

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3 components of cytochrome p450

flavoprotein (cytochrome p450 reductase)
CYP enzyme (has heme)
cofactors NADPH and O2

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AH receptor belongs to which CYP family?

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CAR receptor which CYP family?

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steroid/nicotine in which CYP family

CYP2A

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warfarin, phenytoin, NSAIDS in which CYP family

2C9

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omeprazole, diazepam, clopidogrel in which CYP family

2C19

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codeine, metoprolol, antidrepressants, tamoxifin in which CYP family

2D6

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CYP3 family uses what receptors?

PXR

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Terfenadine and grapefruit?

CYP3A4 competitors

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disorder with mutation in promotor that downregulates UGTs?

Gilberts

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Mutation in gene sequence that kills UGT enzyme?

Crigler-Najjar syndrome

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which population has increased renal blood flow and which one has decreased?

pregnant women increased, old people decreased

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How does epinephrine affect drug target?

epi is vasoconstrictor, decreases blood flow, increased amount of drugs at site

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How does cholesteryamine affect drug drug interactions?

binds acetaminophen, warfarin, digoxin and prevent absorption

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What is Budd Chiari?

occlusion of hepatic portal system, decreases metabolism

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Grey baby syndrome caused by?

Chloramphenicol due to decreased glucoronidation and renal excretion in neonates

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Why is ethanol and acetaminophen mix dangerous?

ethanol induces CYP2E1

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Serum creatinine tells us what?

liver function. Increased serum creatinine means decreased excretion

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Probenecid causes drug drug interaction where and why?

kidney (excretion) because inhibits anion transporter

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Thalidomide

caused limb malformation

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DES

clear cell vaginal adenocarcinoma

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Warfarin is metablized by which CYP?

2C9

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Warfarin inhibits what?

VKORC1

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Therapeutic index calculated by?

Lethal dose/ED50

Competitive agonists affects efficacy or potency?

decreases potency (x)

Which G receptor activates PKA? inactivates PKA?

S, I

What does Gq do?

activates PKC

MAD2s belong to which G receptors

Ras Raf Mek are EGF that go throuh which receptors?

kinase linked

IL1 goes through which receptors?

Kinase

Which receptors are not bound my membrane?

nuclear receptors

Tamoxifen uses what receptors?

Nuclear

Tyrosine-->? by what?

L-DOPA by tyrosine hydroxylase

What inhibits the synthesis of L-DOPA from tyrosine?

Metyrosine and NE

What is metyrosine used as treatment for

pheochromocytoma

L-DOPA becomes what by what?

Dopamine by AAAD

What inhibts AAAD?

Carbidopa

Dopamine is broken down into MAO-B but this is inhibited by inhibitors. What's an example?

Deprenyl

Dopamine becomes what by what?

NE by DBH

What inhibits DBH?

copper chelators such as disulfiram for alcoholism

NE becomes what by what?

Epi by PNMT (only in adrenal medulla)

What inhibits PNMT?

SKFs

Can carbidopa cross BBB?

No. given as treatment for Parkinson's so that L-DOPA can build up in plasma

Catecholamine reuptake 2 ways?

sodium channels (uptake1) or broken down by COMT

What role does alpha2 play in release of catecholamines?

inhibits calcium channel

Mechanism and action of reserpine?

inhibts amineH catecholamine packaging into vesicles

Mechanism and action of clonidine?

alpha 2 agonist (inhibits release of catecholamine vesicle)

Metyrosine mechanism?

inhibits tyrosine

metyrosine use?

pheochromocytoma

Cocaine's action on CNS and PNS?

CNS: inhibits uptake 1 PNS: inhibits sodium channels

Epinephrine mechanism

alpha 1 and 2, beta 1 and 2 agonist

Norepi mechanism?

alpha 1 and 2 agonist, mild beta 1 agonist

corects hypotension in critical care setting?

norepi

alpha 1 agonists?

phenylephrine | methoxamine

alpha 2 agonist?

clonidine | alpha-methylnoradrenaline

Phenoxybenzamine and phentolamine

alpha 1 and 2 antagonist

use of phenoxybena and phentolamine?

pheochromocytoma (tumor of adrenal gland)

prazosin is what kind of antagonist?

alpha 1

Yohimbe

alpha 2 antagonist

carvedilol mech?

alpha 1 | beta 1 and 2 antagonist

Nebivolol mechanism?

beta 1 antagonist and vasodilation

Isoproternol

beta 1 and 2 agonist

Dobutamine

beta 1 agonist

beta 2 agonist?

albuterol and terbutaline

strict beta 1 antagonist?

atenolol | metoprolol

Propranalol

beta 1 and 2 antagonist

Prazosin and epinephrine together?

unopposed alpha 2 and beta 2 agonist. DECREASES BP

Tyramine alone

metabolized by MAO, no effect

tyramine and MAOI

tyramine not metabolized, causes hypertensive crisis

Tyramine and MAOI and TCA

TCA blocks uptake 1, no tyramine inside terminal, no effect

Choline transported into terminals via

symporter

Choline--?

ACh via choline acetyltransferase

Ach packaged into vesicles via

antiporter

How is Ach broken down?

Acetylcholinesterase cleaves

Re-uptake of Ach done by

symporter

How to treat supraventricular tachy?

Carotid massage (CN X) or adenosine

Why do we give adenosine for supraventricular tachy?

acts on purinergic receptor to increase activation of Potassium (Ach) channels

What drug inhibits Na/Ach symporter?

Hemicholinium

What drug inhibits antiporter?

Vesamincol

How does botulism work?

inhibits vesicle release

Latrotoxin and betatoxin (spider venom) works with what action?

destroys synaptic vesicles results in flooding of Ach into cleft, overload and synaptic failure

What treatment is 3,4 diaminopyridine used for?

Lambert Eaton Myasthenic Syndrome

How does 3,4 diamino work?

promotes vesicle fusion and release of ACh

Bethanechol use?

urinary retention (think bowel and bladder)

Pilocarpine binds what kind of receptor?

Muscuranic

PIlocarpine use?

glaucoma

Anticholinerastes work how?

inhibit ACE activity, results in SLUDGE effects

Short, medium, and long acting anticholinesterases?

short: edrophonium medium: stigmine long: organophosphates

Trimethaphan use?

emergent lowerin of BP works by competive nAch receptor blocker

Atropine mechism

binds and inhibits mAchR, lasts 4 hours

``` Red as beet hot as hare Made as a hatter Dry as bone talks about what? ```

atropine SE

Scopolamine vs. atropine?

stronger CNS effects but like atropine peripherally

Curare is used as what?

muscle relaxant in anesthesia from plants flaccid paralysis

How to overcome flaccid paralysis

Anticholinesterases

Succinylcholine use?

endotracheal intubation anesthesia infuction

Succinylcholine is ACE resistant and has 2 phases. what are they?

1. fasciculations | 2. paralysis

Patients on warfarin, pay attention to what pharmogenetics genotype?

VKORC1 A/A and CYP2C9 *3/*3