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These Pharm Cards Have Been Compromised > Working My way Up > Flashcards

Working My way Up Flashcards

1
Q

lomitapide

mech, SE

A

ENZYME INHIBITOR: inhibits VLDL assembly in liver

hepatotoxic

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1
Q

Natural opiate analogs (2)

mech, admin, use

A

morphine, codeine

RECEPTOR AGONIST: activates opiate receptors

morphine admin IV; codeine admin oral (no first pass)

morphine is a painkiller
codeine partial opiate agonist; ↓nantinociceptive, ↑anticoughing

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1
Q

sodium valproate

mech, SE (5), use

A

↑GABA breakdown
↓GABA synthesis: ENZYME INHIBITOR
inhibits Na+ and Ca++ channels: CHANNEL BLOCKER

GI upset; CNS sedation; tremors; potentially fatal hepatitis
fetal damage (↓IQ)

antiepileptic for all siezure types

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1
Q

pralidoxime

use?

A

reverses permanent damage due to Acetylcholinesterase inhibitors

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1
Q

Cyclosporine

mech, use, SE (7)

A

binds to CYCLOPHYLLIN protein→COMPLEX inhibits calcineurin phosphatase
eventually incapacitates T-Cells

tx transplants, psoriasis, dry eye

metab by CYP450
nephrotoxicity, hepatotoxicity
cosmetic changes: hypertrichosis, gingival hyperplasia
↑cholesterol, mild HTN

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1
Q

the methylxanthine used for asthma

mech, SE (5)

A

theophylline

inhibits cAMP phosphodiesterase ENZYME (relaxes smmm by ↓cAMP breakdown)

♥ arrythmias (from heart stimulation)
CNS: tremors, insomnia, seizures
GI upset

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1
Q

bleomycin

mech, SE

A

intercalates with DNA→strand breakage

pulmonary fibrosis

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1
Q

NIBs

mechanism

A

kinase inhibitors

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2
Q

ß1 receptor agonists (2)

A

norepinephrine, dobutamine

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2
Q

leuprolide

mech, use

A

stimulates GnRH receptor→initially ↑testosterone, then downregulates receptor and then ↓↓↓testosterone synthesis

tx prostate tumors

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2
Q

glucocorticoids used for asthma tx (7)

mech? clinical use? admin? SE (2)?

A

beclomethasone, budesonide, fluticasone, mometasone, ciclesonide (all inhaled)
prednisone, dexamethasone (not inhaled)

bind to intracellular receptors→alter DNA trxn→↑lipocortin→inhibits PLA2 synth

DOC for chronic asthma

infections in mouth (thrush), dysphonia (abnormal speech)

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2
Q

celecoxib

mech, use, SE

A

specific COX2 inhibitor

used to treat arthritis

↑MI, ↑stroke due to greater effect of drug on PGI2 than TXA2

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3
Q

heparin

mech, admin, SEs (3), OD tx

A

ENZYME ACTIVATOR: activates blood LPLases;
↑↑↑affinity of antithrombin III for factors II, IX, XI, XII→ inhibited coagulation

admin IV or subq (too big to be absorbed)

↑bleeding
heparin induced thrombocytopoenia (HIT)
osteoporosis

OD tx with protamine sulfate/heparinase

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3
Q

What are the general effects of opioids? Which are the most severe?

CNS (8)

Systemic (6)

A

CNS: profound analgesia, mild sedation, euphoria/↑mood, nausea (stim CNS chemorec), ↓respiration (chief COD!!!!), ↓cough reflex, pinpoint pupils (stim. Edinger-Westphal nuc.), moderate hyperthermia

systemic: severe constipation, skin flushing (vasodil.), orthostatic hypotension (vasodil.), ↑CSF pressure, bronchoconstriction (histamine release), itching (histamine release)

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3
Q

highest potency glucocorticoids

A

dexamethasone, betamethasone

ISA:25
MCA: 0.01
duration 36-54h

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4
Q

barbiturate used to treat siezures

mech, clinical use, SE

A

phenobarbital

ACTIVATES GABAergic neuron

for all but petit mal siezures

drowsiness, sedation
STRONG CYP450 INDUCER

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4
Q

What is the mechanism of action for glucocorticoids?

A

enter target cell and binds to cytoplasmic receptor

steroid-receptor complex dimerizes and binds to steroid response element in DNA

lipocortin I is induced→activity of phospholipase A2 is inhibited

↓↓synthesis of prostaglandins and leukotrienes→inhibits immune response

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5
Q

phosphodiesterase inhibitors (2)

mech

A

cilostazol, dipyridamole

ENZYME INHIBITOR: inhibits phosphodiesterase→↓cAMP breakdown→↓platelet activation

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5
Q

What agent activates all adrenergic receptors?

A

epinephrine activates all α and ß receptors

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5
Q

formulas for:

elimination constant
half-life
volume of distribution
clearance
amount of drug at equilibrium
concentration of drug at equilibrium
loading dose

A

0.693=Ke*T1/2

C(dose-response)=dose/Vd

CL=Ke*Vd

Aeq=(1.44*(T1/2)*(dose))/(dose interval)

Ceq=(1.44*(T1/2)*(dose))/(Vd*dose interval)

Ceq*Vd=LD

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6
Q

Name the primary cause of microcytic anemia? How is it treated? What are the symptoms of an overdose of this agent ,and how is this treated?

A

primary cause is excessive Fe loss (can also be due to insufficient dietary intake, decreased absorption, or increased Fe requirements)

treated with oral/parenteral Ferrous sulfate (FeSO4)

acute OD tx with deferroxamine
chronic OD with phlebotomy

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6
Q

heparin analogs (3)

differences from heparin

A

enoxaparin, dalteparin, fondaparinux

longer half life
predictable dose response
greater effects on factor X compared to thrombin
↓serious SEs (HIT and osteoporosis)
no response to protamine sulfate treatment

fondaparinux crosses placenta

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7
Q

anastrozole

mech, use

A

inhibits aromatase enzyme (which converts testosterone to estrogen)

treats ladycancers

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8
Q

flutamide

mech, use

A

blocks intracellular androgen receptor

tx prostate tumors

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9
Q

What are the toxicities of cocaine?

CNS (5), systemic (6)

A

CNS: anxiety, paranoia, insomnia, psychoses, hallucinations, siezures
tolerance to euphoric effect (body cannot synth NTs to keep up with demand)
severe local vasoconstriction→tissue anoxia and death
urticaria (itching), cardiac arrythmia (Len Bias), ↓blood flow to uterus (low birthweight)

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9
Q

Phenytoin

mech, tox, clinical use, SE

A

inhibits Na+ channels in brain slowing neural activit

low TI

for all siezures except petit mal, DOC for Grand Mal

acute: respiratory depression, CV collapse, ataxia, nausea
chronic: gingival hyperplasia, vestibular efx (diplopia, ataxia, blurred vis)
teratogenic (fetal hydrantoin sx)
life threatening rash (Stevens-Johnson sx)

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9
Q

K+ sparing diuretics (4)

mechs, SE

A

spironolactone, eplerenone:

block aldosterone receptor→↓ synth of Na+K+ATPase pump (slow onset)
treats excess aldosterone activity
HYPERkalemia

triamterene, amiloride:

block Na+ from entering Na+K+ATPAase pump directly (rapid onset)
predictable dose reponse
HYPERkalemia

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11
Q

Antinicotinic Agents (4)

A

succinylcholine (also a nicotinic agonist; depolarizes NMJ)

paracuronium, atracurium, rocuronium (nondepolarizing ACh receptor blockers on skeletal mm)

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12
Q

nicotine

mech

A

highly addictive: nicotine RECEPTOR AGONIST (may ↑DA)

enters CNS nearly instantly for a very short ‘high’ every puff

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12
Q

halogenated hydrocarbons

PK, clincal use, SE

A

very potent, but slower

maintains anaesthesia

malignant hyperthermia (↑↑Ca++ uptake by skmm→↑↑body temp)
liver dx with repeated exposure
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12
Q

nitroprusside

mech, clinical use, admin

A

very fast ↑cGMP→arterial and venous vasodilation→↓↓BP

DOC for HTN crisis

admin IV (quickly degrades to CN- in solution)

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12
Q

abatacept

mech, use

A

inhibits CD80 and CD86 receptors

treats RA

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12
Q

infliximab

mech, use, SE (5), admin

A

mAB binding to TNF molecule

RA, Chrohn’s disease

admin IV

hypersensitivity (chimeric MAB);
itching, hypotension, fever
worsens TB/fungus infections

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13
Q

AFILs (+1)

mech, SE(6), clinical usage

A

sildenafil, vardenafil, talafil, avanafil

type 5 cGMP phosphodiesterase inhibitors→↓degradation of cGMP→vasodilation

slight ↓BP (synergistic with α1 inhibitors and nitrates!!!)
stroke, MI
impaired blue green color vision
NAION retinal damage
metab by CYP450

tx erectile dysfunction, pulmonary HTN
alprostadil–injectabile PGE tx erectile dysfunction

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14
Q

cytarabine

mech

A

pyrimidine analog inhibiting DNA polymerase

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15
Q

etoposide

mech

A

inhibits topoisomerase II→irreperable DNA breaks

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15
Q

dactinomycin

mech

A

intercalates with DNA→interferes with RNA synthesis

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17
Q

cannabinoids (3)

mech, efx (8), tox (4), clinical use

A

THC, dronabinol, nabilone

RECEPTOR AGONIST: binds to cannabinoid receptors

CNS: euphoria, antiemetic, ↓intraocular pressure, anticonvulsant, ↑appetite
systemic: bronchodilation, conjunctival vasodilation, drymouth (anticholinergic)

TI>1000 (virtually impossible to OD)
lung probs, can pass placenta, no withdrawal symptoms, dont operate machinery

treat glaucoma, chemo SEs

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18
Q

atypical antipsychotics (5+5+1)

mech

A

PINEs (quetiapine, loxapine, asenapine, clozapine, olanzapine)
DONEs (risperidone, iloperidone, paliperidone, lurasidone, ziprasodone)
apiprazole

primarily a D2 RECEPTOR INHIBITOR, but has affinity for H1 and 5HT receptors too

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20
Q

Class III antiarrythmics (3)

mech, SE (6), clinical use

A

sotalol, amiodarone, dronedarone

CHANNEL BLOCKER:  primarily block K+ channels, but:
RECEPTOR BLOCKER:  all also have ß blocker effect (class II)
am. and dron. also block Na+ (class I) and Ca++ channels (class IV)

ß blocker efx (all)
blue-gray skin color, pulmonary fibrosis, liver dmg, GI upset, optic neuritis (ami, ↓efx from dron)

ami. is most effective anti arr, DOC for ♥ arrest

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21
Q

inhibitors of leukotriene system (3)

mech

A

zileuton inhibits E2 5-lipoxygenase in immune cells

zafirlukast, montelukast block leukotriene receptors on pulmonary smmm

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22
Q

anagrelide

general effect?

A

↓platelet formation, maturation, and number via unknown mechanism

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22
Q

non propionic acid, non acetic acid derived (6)

mech, SE

A

pyroxicam, diclofenac, bromfenac, nepafenac, etodolac, nabumetone

cyclooxygenase inhibitors (COX1 and COX2)

[see aspirin]
also in ↑doses: ↑MI, ↑stroke (due to greater effect on PGI prod. than TXA2)

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22
Q

abiraterone

mech, use

A

inhibits 17-hydroxylase lyase (CYP17)→ ↓testosterone synthesis

tx prostate tumors

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23
Q

Loop Diuretics (4)

mech, clinical use, SE (5)

A

furosemide, ethacrynic acid, bumetanide, torsemide

inhibit NaCl resoprtion from asc. LoH→extremely powerful

in px who don’t respond to thiazides/
w compromised renal function/ life threatening edema

dehydration
HYPOkalemia
HYPOcalcemia
↓uric acid secretion
auditory nerve damage

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24
Q

minor inhibitors of TG synthesis (2), mech

A

icosapent ethyl, omega-3 fatty acids

inhibits enzyme

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25
Q

natalizumab

mech, use, SE

A

inhibits to α-integrins (INHIBITS RECEPTORS) on CD4 T-Cells

Crohn’s Dx, MS

linked with progressive multifocal leukoencephalopathy (viral dx of CNS)

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27
Q

Common side effects of most local anaesthetics:

CNS (5)
systemic (2)

A

CNS: disorientation
drowiness
slurred speech
numbness
blurred vision

♥arrythmia/tachycardia

esters can cause allergic reactions

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28
Q

Third Generation Antidepressants (4)

mech, SE (7), PK

A

milnacipram, duloxetine, venlafaxine, desvenlafaxine

GI upset, insomnia, headache, ↓libido, ♥ stimulation
metabd by CYP450
​synergistic with alcohol

TI=low, effect takes a long time to develop (long t1/2 and Vd)

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30
Q

CNS α2 agonists for HTN (2)

mech, SE, clinical use

A

αMethylDOPA and clonidine

both enter CNS and ACTIVATES α2 RECEPTORS

SE: depression, drowsiness, impaired ejaculation
dry mouth, hepatic dysfunction (αMD only)

clonidine: off label for fibromyalgia, insomnia, Tourettes
opiate w/d (alternative to methodone)

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30
Q

Angiotension Receptor Blockers (7)

mech, SE

A

ARTANs (losartan, irbesartan, valartan, candesartan, telmisartan, eprosartan, olmesartan)

blocks AII receptor on BVs, ↓aldosterone secretion

fetal abnormalities (cat X)

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31
Q

acomprosate

general effect?

A

↓↓EtOH craving

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32
Q

ADP receptor blockers (4)

mech, which drug(s) have SEs (2)

A

ticlodipine, clopidogrel, ticagrelor, prasugrel

RECEPTOR BLOCKER: blocks platelet ADP receptor

ticlodipine SEs: neutropenia, agranulocytosis

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33
Q

propofol

clinical use, mech, PK

A

most commonly used GA

ACTIVATES GABA, antiemetic

rapid onset, short duration

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34
Q

STATINs

mech, SEs (3)

A

ENZYME INHIBITORS: HMG-CoA reductase inhibitors→↑LDL uptake from blood

myositis→rabdomyolysis
teratogenic (preg. cat. X)
heatotoxic

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35
Q

What is the toxicity of caffeine (5), TI?

What are the withdrawal symptoms?

A

nervousness, insomina, tremors, cardiac arrythmias, and siezures

TI is roughly 100

w/d: headache, lethargy, irritability

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35
Q

Barbiturates (5)

mech, PK, SE, clinical uses

A

ITALs (pentobarbital, secobarbital, butabarbital, amobarbital, phenobarbital*)

ENHANCE GABA action!

10x greater efficacy than benzos, way less potent

↓↓↓respiration (acts on medullary respiratory center, contra in px w/ breathing probs)
TI=10 (suicide risk)
synergistic with ethanol (CNS depression)
supress REM sleep
+Benzo SEs

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36
Q

benzodiazepenes used as hypnotics (5)

mech, PK, clinical use, tox/SE (8)

A

flurazepam, temazepam, estazolam, quazepam, triazolam

ACTIVATES benzodiazepene RECEPTOR: enhances activity of endogenous GABA

longer duration of action

flurazepam DOC for insomnia

very high TI (limited efficacy)
dizziness, ataxia, impaired judgement, ↓learning
confusion, vision changes (diplopia, nystagmus)
interacts with EtOH

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37
Q

sugammadex

use?

A

reverse effects of non-depolarizing antinicotinic agents (eg: rocuronium) by binding directly

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39
Q

LDOPA + carbidopa

mech, SEs (5)

A

LDOPA: prodrug precursor of DA, can cross BBB
carbidopa: a DOPA decarboxylase ENZYME INHIBITOR (prevents breakdown of DOPA in CNS)

after 4-5 yrs of tx: ↑dyskinesia/akinesia (large fluctuations of DA in brain)
discontinuation→neurileptic malignant sx (↑↑fever with muscle rigidity)
nausea (chemoreceptor induced)
hallucinations, confusion, worsens open angle glaucoma

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39
Q

define MAC, B/GC

A

MAC: concentration at which 50% of px are unresponsive (↓MAC=↑potency)

B/GC: the amount that is dissolved in plasma before it reached target tissues
(↑B/GC→slower onset and recovery; higher plasma solubility gives a bigger ‘reservoir’ in the blood for the GA to overcome

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39
Q

central + peripheral acting HTN agents (3)

mech, clinical use

A

propranolol, reserpine, αMethyl-tyrosine

nonspecificßblocker, post-gang NT depletion, and tyrosine hydroxylase ENZYME INHIBITOR

αmethyl tyrosine treats pheochromocytoma

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40
Q

hydroxychloroquine

mech, SE (3)

A

taken up by macrophages, concentrated in lysosomes, and interferes with antigen processing

GI dysfunction, dermatitis,
irreversible retinal damage

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41
Q

Agents used to treat anemias due to chronic renal failure/chemo (3)

mech, SE (4)

A

epoeitin alfa, darbepoeitin, peginasetide

mimic/enhance activity of erythropoeitin

↑BP, ↑clotting, MI, stroke (due to ↑↑RBC count)

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41
Q

least potent glucocorticoids

A

cortisone (a prodrug→no topical admin), hydrocortisone

ISA:1
MCA: 1
duration 8-12h

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42
Q

class Ia antiarrythmics (3)

mech? SEs specific to drugs (8)

A

quinidine, procainamide, disopyramide

CHANNEL BLOCKER: Na+ channel blocker, with anticholinergic (q,p) and antivagal (d) efx

GI: anorexia, nausea, vomiting, ↓appetite (all)
CNS: tinnitus, altererd color vision (q only)
lupus like sx in slow acetylators (p only)
‘Mad Hatter’ anti DUMBBELS system (d only)

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44
Q

dabigatran

mech, SE (2)

A

ENZYME INHIBITOR: directly inhibits thrombin (II)

metabd by CYP450
hemorrhage

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45
Q

What are the clinical uses of antihistamines (4)? What are they ineffective in treating?

A

dermatoses (itching, insect bites)
allergic rhinitis/conjunctivitis→ ↓ congestion, sneezing
antiemetic/antinausea→tx motion sickness
sedatives

DO NOT TREAT ASTHMA or COMMON COLD

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45
Q

metabolic side effects of glucocorticoids (3)

A

weight gain

fat redistribution (to abdomen, moon face, buffalo hump)

muscle wasting (thin arms, growth inhibition in children)

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46
Q

dopamine agonists (5)

mech, SE (5)

A

bromocryptine, pramipexole, ropinirole, rotigotine, apomorphine

D2 receptor agonists

nausea, hypotension (all)
hallucinations (brom. only)
confusion, sudden sleep syndrome (not. brom)
DISORDERS OF IMPULSE CONTROL (not brom.)

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47
Q

indirect acting cholinergic agonists (5)

mech

A

physostigmine, neostigmine, demarcarium (hours)
edrophonium (short duration)
echothiophate (direct phosphorylator of AChE):

inhibit acetylcholinesterase

all used to treat glaucoma, myaesthenia gravis, and Sjogren’s sx

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47
Q

tolfacitinib

mech, SE

A

inhibits Janus Kinase→prevents effect of cytokines on gene expression (JAK-STAT)

↑infection chance, ↑malignancy

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48
Q

irinotecan

mech

A

topoisomerase I inhibitor

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49
Q

α2 receptor agonists (2)

clinical use?

A

clonidine, αmethylnorepinephrine

treat HTN, treat glaucoma

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49
Q

fulvestram

mech, use, SE (2)

A

blocks estrogen receptor

treats ladycancers

retinal changes, cataract formation

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50
Q

ACE inhibitors (7)

mech, SE (4)

A

PRILs (captopril, lisinopril, fosinopril, benazepril, quinapril, ramipril, enalapril)

inhibits Angiotensin Converting Enzyme (ACE) (converts AI→AII)
↓breakdown of bradykinin
↓aldosterone secretion

rash, change in taste
angioneurotic edema
fetal damage
PERSISTENT DRY COUGH

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50
Q

vincristine

mech, admin

A

binds to microtubules→blocks cell mitosis

given IV

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51
Q

benzodiazepene used in general anaesthesia

admin?

A

midazolam, given IV

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52
Q

What are the toxicities of traditional antidepressants (1, 2, 3 gen)? (4)

A

siezures, respiratory depression, cardiac arrythmias, renal failure

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52
Q

neuroprotective Parkinsons drugs (2)

mech, PK, SE

A

selegiline, rasagiline

monoamine oxidase B ENZYME INHIBITORS

selegiline metabolised to meth. in body→severe insomnia (not with rasag)

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52
Q

cyclophosphamide

mech, admin

A

prodrug which alkylates DNA

oral/IV

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54
Q

combined α and ß receptor blockers for HTN (2)

mech, SE

A

labetalol, carvedilol

α1, ß1, and ß2 blockers!

postural hypotension, dry mouth
all the propanolol stuff (enters CNS)

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55
Q

propionic acid derivatives (7)

mech, SE

A

PROs (ibuPROfen, naPROxyn, fenoPROfen, ketoPROfen, flurbiPROfen, oxaPROzin, suPROfen)

cyclooxygenase inhibitors (COX1 and COX2)

[see aspirin]
also in ↑doses: ↑MI, ↑stroke (due to greater effect on PGI prod. than TXA2)

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56
Q

agents always administered with LDOPA+carbidopa (2)

mech

A

tolcapone, entacapone

Catecholomethyltransferase (COMT) ENZYME INHIBITORS (prevents breakdown of DOPA in CNS)

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56
Q

mycophenolate mofetil

mech, use, SE

A

specific antimetabolite inhibiting inosine monophosphate dehydrogenase →inhibiting guanosine synthesis

transplants, lupus

GI cell disruption
bonemarrow depression (→thrombocytopoenia, megaloblastic anemia, leukopenia)
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57
Q

Class IV antiarrythmic (3)

mech

A

diltiazem, verapamil, nifedipine

CHANNEL BLOCKER :Ca++ channel blockers→↑♥ frefractory period

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59
Q

Local anaesthetics (general)

Structure, mech, PK, admin

A

a hydrophilic+hydrophobic end connected by an ester/aminoamide link

block Na+ channel of excitable cells (nerves which fire more rapidly are ↑affected)
pain>>>cold/warm>pressure/touch>>motor

ester links: short duration (broken down by plasma cholinesterase)
amino amide: longer duration (CYP450)
weak bases, so injection into acidic environ ↓↓action (infection)

topical, parenteral (infiltration, nerve block, epidural, spinal)

all usually admin with epinephrine

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60
Q

niacin

mech, SEs (4)

A

ENZYME INHIBITOR: inhibits VLDL synthesis, ↑serum HDL

cutaneous flushing, itching (aspirin tx)
↑uric acid (gout risk)
↑DM incidence

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61
Q

amantadine

mech, SE(2)

A

antiviral agent which ↑release of stored DA from nerve terminals

insomnia, restlessness

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62
Q

second generation antihistamines (4)

mech? difference from first gen? tox? SE (3)?

A

loratadine, fexofenadine, desloratadine, cetirizine

block peripheral H1 receptors ONLY

do not cause drowsiness (don’t enter CNS)

high TI

dry mouth, blurred vision, constipation (antimuscarinic efx)

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63
Q

middle potency glucocorticoids

A

prednisone (a prodrug→no topical admin), prednisolone, triamcinolone

ISA:4
MCA: 0.25
duration 18-36h

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64
Q

aspirin

mech

A

ENZYME INHIBITOR: cyclooxygenase inhibitor→inhibits TXA2 synthesis→decreased platelet aggregation

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64
Q

behavioral changes associated with glucocorticoid uses (3)

A

euphoria/depression, psychosis, emotional lability

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66
Q

indirect cholinergic agonist Alzheimers tx (2)

A

donepezil, tacrine

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66
Q

methotrexate

mech, use, SE

A

antimetabolite for folic acid inhibiting dihydrofolate reductase

DOC for early tx of RA

affects cells with rapid turnover (GI, bone marrow, fetal development)

(eventually ihiits cell division)

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68
Q

mannitol

mech, admin

A

admin IV;
not resorbed by tubule so H20 drawn out by osmotic efx

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69
Q

erbulin

mech

A

inhibits microtubules→prevents mitosis, causes apoptosis

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70
Q

agents used to treat partial siezures acting on NTs (5)

A

topiramate, gabapentin, tiagabine, vigabatrin (ACTIVATES GABA)

perampamel (INHIBITS glutamate activity)

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71
Q

Cholinergic blockers for COPD treatment (2)

mech? SE?

A

ipratropium, tiotropium

muscarinic receptors blockers on pulmonary smmm

dry mouth

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73
Q

fomeprazole

mech

A

INHIBITS EtOH dehydrogenase ENZYME

74
Q

Bile acid binding resins (3)

mech, SEs (2)

A

cholestyramine, coleselevam, colestipol

SPECIFIC BINDING TO LARGE MOLECULE: binds to bile acids in gut→↑cholesterol metabolism

binds acidic drugs (eg digoxin, oral anticoags)
↓absorption of fat soluble vitamins

75
Q

azathioprine

mech, use, SE

A

prodrug converted to 6-mercaptopurine→inhibits synthesis of purines; inhibits enzymes responsible for GMP synthesis

transplants, RA, Crohns

Bone marrow depression (→thrombocytopoenia, megaloblastic anemia, leukopenia)

76
Q

bortezomib

mech, use

A

inhibits proteasome→inhibits antigen presentation by APCs

tx multiple myeloma

78
Q

dexmedetomidine

mech, SE

A

an α2 agonist that induces sleep WITHOUT respiratory depression

↓BP, bradycardia

(see clonidine, αmethylDOPA)

79
Q

ergot alkaloids (2)

mech, SEs (2)

A

ergotamine, dihydroergotamine

partial 5HT receptor agonists

synergistic with 5HT agonists (MAOIs/SSRIs)→serotonin syndrome
(HTN, fever, confusion, muscle twitch/rigidity, severe vasospasm)
pregnancy category X

81
Q

dobutamine

mech

A

ß1 agonist creating strong inotropic effect

82
Q

What are the effects of the H1 blockers (6) and H2 blockers (1)?

A

H1 Blockers: CNS: sedation, anti-nausea
drying of mucous membranes
local anaesthesia
dilates bronchial smmm
inhibits secretion of interleukins→ ↓↓immune/inflammation

H2 Blockers: inhibits acid secretion from parietal cells

84
Q

A deficiency in thiamine intake in chronic alcoholics causes what?

A

thiamine deficiency leads to Weirncke’s Encephalopathy (“wet brain”)

86
Q

high potency antipsychotics (2)

mech

A

haloperidol, pimozide

strong D2 (dopamine) RECEPTOR ANTAGONIST

88
Q

How is iron absorbed and transported in the body? How is it stored?

A

Iron is absorbed as Fe++, converted to Fe+++ and transported by transferrin

Iron is storred as ferritin

89
Q

BV α1 blockers

mech, SE, clinical use

A

OSINs: prazosin, terazosin, doxazosin
tamsulosin, alfuzosin, silodosin (only used to treat BPH)

α1 receptor on vascular mm

subject ot first dose effect→orthostatic hypotension

90
Q

flumazenil

mech, admin

A

a benzodiazepene receptor blocker

IV admin

90
Q

thiazide diuretics (2)

mech, SE (6), tox

A

chlorothiazide, hydrochlorothiazide

inhibits Na+ transport out of DCT→H20 follows out and is excreted

HYPERcalcemia
HYPOkalemia (action of Na+K+ATPase pump in Coll Duct)
↑serum LDL, ↑serum TG (↓↓action of niacin and fibrates)
↓uric acid secretion
inhibits insulin secretion→hypoglycemia
contains sulfur ions→allergies

high TI

91
Q

beta blockers for HTN (6)

mech, SEs (7)

A

propranolol, metoprolol, acebutolol, atenolol, betaxolol, nebivolol

prop. is nonspecific ßblocker which also ↓renin
rest are ß1 blockers

bradycardia, fatigue (all)
depression, impotence, ↓HDL, ↑TG, asthma exacerbation (prop only)

91
Q

migraine agents (7)

mech, admin, SE

A

TRIPTANS (sumatriptan, rizatriptan, zomitriptan, naratriptan, almotriptan, eletriptan, frovatriptan)

serotonin receptor agonist

admin oral/IV/nasal spray

synergistic effect with MAOIs or SSRIs→serotonin syndrome
(hyperthermia, muscle twitching)

92
Q

agets treating partial siezures acting on CNS ion channels (6)

A

lamotrigine, zonisamide, refinamide, lacosamide (BLOCKS Na+ Channels)

pregabalin (Blocks Ca++ channels)

ezogabine (K+)

93
Q

muscarinic agonists (3)

A

muscarine, pilocarpine, bethanechol

94
Q

leech saliva protein analogs (3)

mech, admin, clinical use

A

bivalirudin, desirudin, argatroban

ENZYME INHIBITOR: directly inhibits thrombin

Admin IV (first pass)

for px with HIT

95
Q

aspirin

where most readily absorbed? mech?

A

most readily absorbed in stomach (weak acid)

inhibits cyclooxygenase (both COX1 adn COX2)→ ↓prostaglandin synthesis

96
Q

amphetamines and methamphetamine

mech, PK, clinical use, efx (8)

A

RECEPTOR AGONIST: indirect acting amine ↑NE and DA in CNS

t1/2 = 10 hr

treat severe ADHD or narcolepsy

CNS: ↑mood, ↑energy, ↑appetite, temporary ↓need for sleep
systemic: ↑BP, local vasoconstrictor (contra. w/ epi), ↑temp
(basicall the same efx as cocaine + ​meth mouth)

(ultimately the same effect as cocaine)

97
Q

What are the side effects of most antipsychotics? (9ish) What class of drugs do they interact with?

A

CNS: Extrapyramidal: Parkinsons like sx (brady/akinesia, tremor); dystonia, Tardive dyskinesia, akasthesia (use anticholinergics to reverse)

mild sedation (H1 blockade)
α1 blockade causing hypotension
anticholinergic effects (dry mouth/dry eye)
endocrine problems (↓hGH, ↓CRH, ↑prolactin)
neuroleptic malignant sx (related to malignant hyperthermia)
dysphoria, allergic rash

interact with CNS depressants (both inhibit neural activity in different ways)

99
Q

ester local anaesthetics (3)

clinical use, admin

A

cocaine: for ophthalmic/nasal surgery; inhibits NE reuptake in CNS; NOT WITH EPI
benzocaine: topically for burns, long duration for ester LA
procaine: parentarally (short t/12)

100
Q

midazolam

mech

A

ACTIVATES benzodiazepene RECEPTOR (enhances GABA)

101
Q

reserpine

mech, SE

A

depletes post-ganglionic neuron NT “α1 blockade”→no vasoconstriction→↓BP

CNS: depression, behavioral SE, drowsiness
diarrhea

102
Q

betalacept

mech, use, SE

A

inhibits CD80, CD86 receptors

for renal transplants

↑malignancy associated

103
Q

longer acting agents for asthma treatment

mech, admin, SE (3)

A

formoterol, arformoterol, salmeterol, indicaterol

specific ß2 agonist

inhaled usually

tremor, tachycardia, ♥ palpitations (due to ß1 effect)

104
Q

What agent is used to treat sickle cell anemia?

mech, SE

A

hydroxyurea

↑ fetal Hb production

mutagenic (preg. cat D)

104
Q

Skin/mucosal damage associated with glucocorticoids (4)

A

easy bruising (skin thinning)

poor wound healing

acne

increased incidence of infection (eg: thrush)

106
Q

First Gen Antidepressants (2)

mech, SE (9), PK

A

imipramine, amitriptylene

TRANSPORT BLOCKERS: Inhibit NE reuptake in CNS

↑suicide risk, sedation, weight gain
dry mouth, dry eye (anticholinergic)
↓BP, ♥ arrythmia (α1 blockade→contra with ‘AFIL’ drugs)
metabd by CYP450
synergistic with alcohol

TI=5-6, effect takes a long time to develop (long t1/2 and Vd)

107
Q

Opiate antagonists (3)

mech

A

naloxone, naltrexone, methylnaltrexone

opiate RECEPTOR antagonists

(can be used with oxycodone to ↓euphoria)

108
Q

lomustine

mech, admin

A

prodrug which alkylates DNA

given IV

109
Q

nitrous oxide

PK, SE

A

low BGC, MAC>100% (very rapid, but cant put anyone completely out)

good analgesia w/o amnesia
tends to form gas bubbles in body cavities
repeated exposure→megaloblastic leukemia/leukopoenia

111
Q

benzodiazepenes used to treat anxiety (7)

mech, PK, clinical use, tox/SE (8)

A

chlordiazepoxide, diazepam, alprazolam, clonazepam, clorazepate, oxazepam, lorazepam

ACTIVATES benzodiazepene RECEPTOR: enhances activity of endogenous GABA

longer duration of action

diazepam tx status epilepticus siezures

very high TI (limited efficacy)
dizziness, ataxia, impaired judgement, ↓learning
confusion, vision changes (diplopia, nystagmus)
interacts with EtOH

112
Q

neuronal antispastics (3)

mechs

A

baclofen: GABA AGONIST

diazepam (and other benzos): GABA AGONIST

tizanidine: α2 agonist (see clonidine, αmethylDOPA)

112
Q

ATGAM antithymocyte globulin

mech, use, SE

A

polyclonal antibody

treats acute renal transplant rejection

↑risk for allergic response

113
Q

acetazolamide

mech, clinical use

A

carbonic anhydrase ENZYME INHIBITOR

tx Grand Mal siezures
also can be used as a diuretic, or to treat bipolar disorder!

114
Q

benzodiazepene used to treat siezures

mech, tox, clinical use

A

diazepam

ACTIVATES GABAergic neurons

very high TI

used to treat Statuse Epilepticus (because it can be administered in large doses)
also Grand Mal

116
Q

Synthetic opiate analogs (6)

mech, admin, clinical efx

A

fentanyl (100xM), sulfentanil, alfentanil, remifentanil (500xM), merperidine (0.5xM), methadone (1xM)

opiate RECEPTOR AGONIST

all except methadone IV, methadone orally

merperidine has no pupil constriction
methadone ↓euphoria, ↓w/d symptoms→used for opiate w/d tx

117
Q

imitinib

mech, use, admin, SE

A

protein kinase inhibitor of a kinase which turns off cell apoptosis

tx chronic myelogenous leukemia (CML)

given orally→causes edema

119
Q

What 3 classes of drugs can be used to treat angina?

A

nitrates (DOC)

beta blockers

Ca++ channel blockers

120
Q

5-fluorouracil

mech

A

pyrimidine analog inhibiting thymidylate syntetase→inhibits thymidine synthesis

121
Q

Non-traditional sleep inducers (2)

mech, SE

A

ramelteon, tasimelteon

melatonin RECEPTOR AGONISTS (no eff on GABA)

sleepiness, fatigue, ↓testosterone

122
Q

What are the desired effects of aspirin and other NSAIDs (4)? What are the SE/toxicities (8)? Where is it contraindicated (2)?

A

antipyretic effects (for fever px only)
limited analgesia (due to ↓prostaglandins)
antiinflammatory
anticlotting (irreversible inhibitor of platelet COX2→↓TXA2)

GI upset (gastric irritant→↓PG production via intestinal mucosa)
tinnitus
↑respiration
↓miosis, ↓kidney perfusion, hypersensitivity, bronchospasms, inhibits labor

contrx with clotting deficiencies
contrx in children with viral infections (→Reyes sx)

124
Q

vorapaxar

mech, careful use where?

A

RECEPTOR BLOCKER: blocks platelet thrombin receptor

careful use in px with intracranial bleeding

126
Q

warfarin

mech, PK, SE(4)

A

ENZYME INHIBITOR: vitamin K analog preventing body’s recycling of Vitamin K→indirectly inhibits synthesis of prothrombin (II), factors VII, IX, and X

slow onset (24+ hours—because it’s an indirect synthesis inhibitor)

metabolized by CYP450
watch vitamin K in diet
hemorrhage
passes placenta (pregnancy cat X)

128
Q

mipomersen

mech, admin

A

antisense mRNA: to apolipoprotein B→inh. VLDL synth in liver

only antihyperlipidemic given IV

130
Q

‘other’ CNS stimulants (4)

mech, clinical use

A

modafinil, armodafinil, dexymethylphenidate, methylphenidate

REUPTAKE INHIBITORS

tx narcolepsy or ADHD

131
Q

low potency antipsychotics (6+1)

mech

one has a nasty side effect–name and describe

A

thiothixene + ZINEs

primarily D2 RECEPTOR ANTAGONISTS, can also block H2 (histamine) receptors

chlorpromazine deposits in lens and causes irreversible pigmentation

(thoridazine, chlorpromazine, fluphenazine, perphenazine, prochlorperazine, trifluoperazine)

132
Q

rilonacept

mech, use, admin, SE

A

binds to IL-1 molecule!

admin subQ

RA; admin with methotrexate

NOT USED with TNF inhibitors (synergistic)

133
Q

ustekinumab

mech, use

A

binds to IL-12 and IL-23 molecules

psoriasis

134
Q

adalimumab

mech, use

A

binds to TNF molecule

RA

135
Q

dantrolene

mech, SE (2), clinicale use

A

acts directly on muscle cells to inhibit Ca++ induced Ca++ release from SR

muscle weakness, hepatits

used to treat malignant hyperthermic sx

137
Q

digoxin

mech, SE (5)

A

ENZYME INHIBITOR: inhibits Na+K+ATPase→↑Na+ in cell→↓Ca++ loss→greater contractility

♥ arrythmia
CNS: yellow-green vision, hallucinations, chemorec. induced nausea
hypokalemia ↑↑↑ efx (watch it with Loop diuretics and thiazides!)

138
Q

omalizumab

mech, admin?

A

anti IgE mAB

IV only

139
Q

Shorter acting agents for treatment of asthma (1+5)

mech? admin? SE (3)?

A

isoproterenol (less selective)

albuterol, pirbuterol, bitolterol, levalbuterol, terbutaline

specific ß2 agonists (RECALL: any agent which acts to activate a receptor can cause downregulation and loss of effect!)

admin via inhalation

tremor, tachycardia, ♥ palpitations (due to ß1 effect)

141
Q

nitrates (2)

mech, admin, SE(3)

A

nitroglycerin, isosorbide dinitrate

ENZYME ACTIVATOR: activates guanylate cyclase→↑↑cGMP→profound coronary vasodilation

nit IV, iso orally

hypotension, headache, skin flushing

142
Q

N-acetyl cysteine

mech

A

used to treat acetaminophen overdose

a reducing agent to ↑glutathione (GSH) levels in liver

143
Q

Factor X inhibitors (2)

mech, SE

A

apiXaban, rivaroXaban

ENZYME INHIBITORS: directly inhibits factor Xa

bleeding esp. after spinal surgery

144
Q

What are the symptoms of opiate withdrawal (8)?

A

severe vasoconstriction: cold and clammy, runny nose, goosebumps

↑GI mobility: diarrhea, cramping

CNS: dysphoria, restless twitching, dilated pupils

145
Q

What is the general mechanism and effects of caffeine?

CNS (4), systemic (4)

A

ENZYME INHIBITOR: inhibits cAMP phosphodiesterase, among other things

CNS stimulant: ↑mood, ↓fatigue, ↑work capacity, ↑respiration

systemic: ↑HR, relax bronchial smmm, weak diuretic, ↑stmm contraction strength

(chronic use: insomnia, tachycardia, GI upset)

(see cilostazol, dipyridamole)

146
Q

CV side effects of glucocorticoids (5)

A

stroke, CHF, MI, HTN, ↑intracranial pressure

147
Q

anakinra

mech, admin, use, SE

A

blocks IL-1 receptor

admin subcutaneously

RA; admin with methotrexate

NOT USED with TNF inhibitors (synergistic)

148
Q

GI side effects of glucocorticoids (3)

A

↑risk of ulcers, gastritic, GI bleeding

149
Q

α1 receptor blockers (2)

clinical use

A

prazosin (HTN, BPH tx), phenoxybenzamine

150
Q

sirolimus

mech, use, SE (3)

A

BINDS to FK-BINDING PROTEIN→COMPLEX inhibits a kinase required for IL-2 induced transcription of cytokines

tx transplantation, psoriasis

renal toxicity
lung toxicity
metab by CYP 450

151
Q

ixabepilone

mech

A

binds to microtubules

152
Q

skeletal side effects of glucocorticoids (3)

A

osteoporosis

osteonecrosis

↓growth in children

153
Q

tamoxifen

mech, use, SE (2)

A

blocks estrogen receptor

treats ladycancers

retinal changes, ↑cataract formation

155
Q

Lithium

mech, SE/tox (9), PK

A

ENZYME ACTIVITY?: alters glutamate metabolism, ↓NE release

TI< 2!!! very toxic, 5-7 day onset of action

tremors, edema, weight gain, nystagmus
↑thirst, ↑urination (blocks efx of ADH)
nausea, delirium, coma

156
Q

topotecan

mech

A

topoisomerase I inhibitor

157
Q

ß2 receptor agonists (4)

clinical use?

A

metaproterenol, terbutaline, fenoterol, albuterol

158
Q

Ca++ channel blockers for HTN

mech, SE(2)

A

IPINEs (nifedipine, nicardipine, amlodipine, felodipine)

blocks Ca++ influx into vasc smmm→no vasoconstriction

heartburn, worsens CHF

160
Q

disulfiram

mech, SE

A

INHIBITS aldehyde dehydrogenase ENZYME

awful hangover (EtO buildup)

162
Q

daunorubicin

mech, admin, SE

A

intercalates with DNA→produces free radicals

given IV

♥ muscle degeneration

163
Q

carbamazepine

mech, clinical use, SE

A

inhibits Na+ channels inhibiting propagation of signals in CNS

DOC for partial siezures

blurred vision, diplopia (eye effects)
drowsiness
fetal defect (teratogenic–spina bifida)
aplastic anemia (agranulocytosis?)

INDUCES CYP450

164
Q

buspirone

mech, PK

A

partial 5HT agonist for anxiolysis w/o sedative/hypnotic efx

slow onset
no X-rxn with benzos or EtOH

164
Q

etanercept

mech, admin, use

A

binds to TNF

given subq

RA

165
Q

endothelin blockers

mech, clinical use, SE(3)

A

ENTANs (bosentan, ambrisentan, macitentan)

endothelin receptor blocker on BVs

treats pulmonary HTN well

fetal damage, hepatic tox, testicular atrophy

167
Q

Antimuscarinic agents (3)

SEs

A

atropine, scopolamine, ipratropium

Mad Hatter (opposite of DUMBBELS)

↑HR, CNS: psychoses
pupil dilation, inhibition of ciliary muscle
bronchodilation
↓GI motility
urine retention
↓↓sweating, lacrimation, salivation

168
Q

leflunomide

mech, SE (4)

A

antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase

diarrhea, abdominal pain
teratogen (especially for lymphocytes)
inhibits CYP450

169
Q

direct agonists of both muscarinic, nicotinic receptors (2)

A

acetylcholine, bethanechol

170
Q

Class Ib antiarrythmics (2)

mech, admin, SE (2) clinical use

A

lidocaine, mexiletine

CHANNEL BLOCKER: Na+ channel blocker

lido IV, mex oral

CNS: tremors, siezures

not likely to cause arr, for Vtach

171
Q

methohexital

clinical use, mech

A

general anaesthetic

GABA ACTIVATOR

171
Q

mast cell inhibitors (2)

mech

A

cromolyn sodium, nedocromil

inhibits release of mediators from immune cells by INHIBITING Cl- CHANNELS, which ↓Ca++ uptake

173
Q

Which agent for asthma treatment is the least selective in its method of action? Which receptors does it bind? What are some side effects (2)? How is it administered?

A

epinephrine

activates ALL α and ß receptors

inhaled or IV

SE: ↑HR (from ß1) and ↑BP (from α1 induced vasoconstriction)

174
Q

carfilzomib

mech, use

A

inhibits proteosomes→inhibits antigen presentation by APCs

tx multiple myeloma

176
Q

agents which affect absorption of lipids (4)

mechs, SE

A

sitostanol, orlistat, olestra, ezetimibe

AFFECTS TRANSPORT (sit, ol, ez):  blocks cholesterol transporters in SI
ENZYME INHIBITOR (or):  inhibits GI lipases

loose stools

178
Q

diazoxide

mech, SE

A

opens K+ channels in arterial smmm→vasodilation

↓↓insulin secretion from ßcells in pancreas→hyperglycemia

180
Q

Henderson-Hasselbalch stuff (ionized vs non ionized form)

A

pH=pK + log ([non-protonated]/[protonated])

small molecules are more available
lipid soluble molecules are more available
ionized molecules do not readily diffuse thru membranes and are not available

181
Q

THE non-narcotic analgesic

mech, tox (2)

A

acetaminophen

NOT AN NSAID→NO antiinflammatory or NO antiplatelet efx

specific COX2 inhibitor?

fewer GI upset than NSAIDs
acute liver failure (↓↓glutathione tx with N-acetyl cysteine)

182
Q

Second Generation Antidepressants (7)

mech, SE (6), PK

A

fluoxetine, fluvoxamine, vilazodone, sertraline, escitalopram, citalopram, paroxetine

TRANSPORT AFFECT: 5HT reuptake inhibitors

GI upset, headache, insomnia, ↓libido

metabd by CYP450
​synergistic with alcohol

TI=low, effect takes a long time to develop (long t1/2 and Vd)

183
Q

botulinum toxin A

mech? clinical use?

A

inhibits ACh release from NMJ

cosmetically;
cerebral palsy, tics, strabismus, nystagmus

184
Q

hemostatic agents (2)

mech

A

aminocaproic acid, tranexemic acid

ENZYME INHIBITOR: inhibits plasminogen activation

184
Q

What other agents can be used to treat bipolar disorder? (5)

A

valproic acid, carbamazepene, lemotregene (anti-siezure)

acetezolamide (anti-diuretic/anti-siezure)

amiprazole (antipsychotic)

185
Q

hydralazine

mech, SE

A

↑cGMP in art smmm→vasodilation

lupus like sx in slow acetylators

186
Q

cocaine

mech, PK, clinical use, efx (7)

A

TRANSPORT SYSTEM EFFECT: prevents reuptake of NE, 5HT, and DA in the CNS

t1/2 = 1 hour, more effect when it’s freebased

local anaesthetic for eye and nasal surgery

CNS: ↑mood, ↑energy, ↑appetite, temporary ↓need for sleep
systemic: ↑BP, local vasoconstrictor (contra. w/ epi), ↑temp

188
Q

fenoldopam

mech, admin, clinical use

A

activates D1 receptors on BVs→vasodilation

admin IV for HTN crises

189
Q

6-mercaptopurine

mech

A

prodrug purine analog inhibiting enzymes required for purine synthesis

190
Q

fibrinogen receptor inhibitors (3)

mech, admin, SE, clinical use

A

abciximab, tirofiban, eptifibatide

RECEPTOR INHIBITOR: decreases platelet activation by binding to GP IIB/IIIA receptors on platelets, preventing fibrinogen from binding

thrombocytopoenia

↓white thrombi, used during coronary vascular procs.

191
Q

etomidate

clinical use, mech, SE (2)

A

General anaesthetic

GABA RECEPTOR ACTIVATOR

relatively high TI, nausea

192
Q

What is the synthetic path for glucocorticoids? Which reactions require P450?

A

cholesterol → pregnenolone → 17-OH pregnenolone → 17-OH progesterone →11-deoxycortisol → cortisol

all require CYP450 except the pregnenolone→17OHpregnenolone reaction

194
Q

ketamine

clinical use, mech, PK, SE

A

Gen Anaesthetic

Glutamate RECEPTOR INHIBITOR

short induction and duration

dissociative anaesthesia: ↑↑↑amnesia and analgesia
can cause hallucinations

195
Q

leucovorin

mech

A

a tetrahydrofolic acid analog which requires DHF Reductase
rescues cells methotrexate toxicity

197
Q

ocular side effects of glucocorticoids (2)

A

cataracts, glaucoma

199
Q

Name the primary cause of megaloblastic anemia. What are the symptoms of this condition? How is it treated?

A

Caused by ↓absorption of B12: can be dietary or genetic inability to produce gastric intrinsic factor (→pernicious anemia)

the lack of methionine causes ↓myelin synthesis

admin oral or parenteral (for pernicious anemia) B12

201
Q

fibrates (2)

mech, SEs(2)

A

gemfibrozil, fenofibrate

RECEPTOR INHIBITOR: binds to PPAR→ ↓TG, ↓VLDL, ↑LPLase synthesis

GI upset
displaces warfarin

202
Q

trastuzumab

mech, use

A

blocks a HR2 receptor (a tyrosine kinase)

tx breast cancer

202
Q

acetic acid derivatives (3)

mech, SE

A

indomethacin, tolmetin, sulinadac

cyclooxygenase inhibitors (COX1 and COX2)

[see aspirin]
also in ↑doses: ↑MI, ↑stroke (due to greater effect on PGI prod. than TXA2)

Indomethacin is extremely potent COX inhibitor:
used for newborns with patent ductus arteriosus
causes thrombocytopoenia, aplastic anemia, corneal opacities

204
Q

What are the 4 classes of drugs used to treat congestive heart failure and how do they work?

A

cardiac glycosides (eg digoxin)–↑ contractility
ACE inhibitors–↓BP, ↓fluid retention
Beta blockers–↓HR
vasodilators–↓BP
(diuretics)

205
Q

Semisynthetic opiate agents (3)

mech, admin, clinical efx

A

heroin, hydromorphone, oxycodone

opiate RECEPTOR AGONIST

heroin (5xM, IV), hydromorphone (10xM, IV), oxycodone (0.5xM partial agonist, avail orally)

206
Q

adenosine

mech, admin, PK, clinical use

A

RECEPTOR AGONIST: binds to adenosine receptors→↓AV node firing

admin IV

t1/2=10 seconds (VERY SHORT)

for A-tach and coronary vasodilation

208
Q

indirect acting amines–sympathetic agonists (5)

mech

A

amphetamine, methamphetamine, tyramine, phenylpropanolamine, pseuoephedrine

induce NE release from nerve terminals

210
Q

Name some causes of macrocytic anemia. How is this condition treated?

A

Caused by folic acid deficiency (via pregnancy, infection, alcoholism, etc), which is required for DNA replication

treated with oral administration of folic acid

212
Q

tocilizumab

mech, use

A

binds to IL-6 receptors on T-cells

RA

213
Q

doxorubicin

mech, admin, SE

A

intercalates with DNA→produces free radicals

given IV

♥ muscle degeneration

214
Q

Which reactions are CYP450 Phase I, non-CYP450 Phase I, or Phase II reactions?

A

CYP450 Phase I (oxidation of drug): hydroxylation, N-oxidation, S-oxidation, N-dealkylation , O-dealkylation

Non-CYP450 Phase I: deamination, hydrolysis, peptidase, phosphatase

Phase II: acetylation, glucuronidation, methylation, sulfation, glycination

215
Q

paclitaxel

mech

A

forms abnormal microtubules

217
Q

prednisone

mech, use

A

inhibits immune functioning

treats neoplasia of immune system (like leukemias, lymphomas)

218
Q

teriflunomide

mech, SE

A

prodrug; converted to antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase

diarrhea, abdominal pain
teratogen (especially for lymphocytes)

219
Q

non-benzodiazepene hypnotics (3)

mech, SE (4)

A

zolpidem, zaleplon, eszopiclone

binds to α-subunit of benzo receptor (↓ effect on muscle relax or siezure activity)

↓inhibitions, bizzare behavior, sleep actions, hallucinations

220
Q

ethosuximide

mech, SE (2), clinical use

A

inhibits Ca++ channels

GI upset, drowsiness

DOC for petit mal

221
Q

certolizumab

mech, use

A

binds to TNF molecule

RA, Chrohn’s Dx

222
Q

bevacizumab

mech

A

blocks VEGF (vascular endothelial growth factor)→inhibits formation of blood supply to tumors

223
Q

nonspecific ß blockers (5)

A

OLOLs (propranolol, timolol, carteolol, metipranolol, levobunolol)

224
Q

acetazolamide

mech, clinical use

A

inhibits carbonic anhydrase→inhibits bicarbonate resorption in PCT

primary use is not as diuretic:
open angle glaucoma, MOUNTAIN SICKNESS, epilepsy, bipolar dx

225
Q

malathion and sarin

mech?

A

irreversible AChE inhibitors (very potent nerve gases)

226
Q

cisplatin

mech, SE(2)

A

alkylates DNA

renal damage, ototoxicity

227
Q

MAOIs (3)

mech, SE/tox (10)

A

phenylzine, isocarboxazide, tranylcypromine

inhibit Monoamine Oxidase (MAO) in the brain (↓NE and 5HT metabolism)

CNS: ↑suicide, siezures, insomnia, agitation, hallucinations
hepatotoxic, wt gain, hypotension,
synergistic with EtOH
synergistic with indirect acting amines (eg: tyramine)→HTN crisis

228
Q

first generation antihistamines (6)

mech? clinical use for each? tox? SE (4)

A

block both central and peripheral H1 receptors

diphenhydramine (sedative, motion sickness)
clemastine (motion sickness)_
chlorpheniramine (NOT A SEDATIVE, uticaria, motion sickness)
hydroxyzine (sedative, uticaria)
promethazine (STRONG sedative, STRONG antiemetic)
tripelennamine (sedative, local anaesthetic)

high TI

dry mouth, blurred vision, constipation (antimuscarinic efx)
synergistic with CNS depressants

229
Q

rituximab

mech, use

A

blocks CD20 receptor

tx Chronic lymphocytic leukemia, RA

231
Q

specific H2 blockers (4)

mech, SE

A

blocks peripheral H2 receptors (doesn’t cross BBB)

cimetidine (has antiandrogenic efx→gynecomastia/galactorrhea)

ranitidine
tamotidine
nizatidine

232
Q

everolimus

mech, use, SE (3)

A

BINDS to FK-BINDING PROTEIN→COMPLEX inhibits a kinase required for IL-2 induced transcription of cytokines

tx transplantation, psoriasis

renal toxicity
lung toxicity
metab by CYP 450

233
Q

methotrexate

mech, SE

A

folic acid antimetabolite inhibiting dihydrofolate reductase

myelosuppression (inhibition of blood cell formation)→fixed with leucovorin

234
Q

basiliximab

mech, use, SE (4)

A

mAB that blocks IL-2 receptor

used with cyclosporine A

hypersensitivity rxns (chimeric)
HTN, bronchospasms, pulmonary edema
235
Q

vinblastine

mech, admin

A

binds to microtubules→blocks cell mitosis

given IV

236
Q

tetrodotoxin and saxitoxin

mech

A

irreversible Na+ channel blockers

237
Q

ibritumomab

SE

A

its pure mouse, so superduper antigenic

238
Q

amino amide local anaesthetics (8)

clinical use, admin, SEs

A

procainamide: IV for ♥ arrythmia; can cause lupus-sx in slow acetylators
lidocaine: IV for ♥ arrythmia; tremors, slurred speech, drowsiness

articaine, mepivacaine, bupivacaine, prilocaine, ropivacaine, etidocaine

239
Q

tacrolimus

mech, use, SE (5)

A

binds to FK-BINDING PROTEIN→COMPLEX inhibits calcineurin phosphatase

tx transplants

nephrotoxic
neurotoxic
alopecia, diabetes
metab by CYP450

(ultimately prevents activation of Tcells; more efficacious than cyclosporin)

240
Q

Class II antiarrythmics (3)

mech, SE (3)

A

propranolol, metoprolol, esmolol

RECEPTOR BLOCKER: ß blockers on ♥→effectively ↓HR; (prop is nonselective, met and esm. are both selective ß1 only)

bradycardia, hypotension, asthma exacerbation (prop only)

241
Q

minoxidil

mech, clinical use, SE

A

opens K+ channels in art. smmm.→inhibits contraction

for very refractory patients; also packaged as Rogaine

hypertrichosis, edema, cardiac tampanade

242
Q

Anticholinergics for Parkinsons (2)

mech, SE (3)

A

trihexyphenidyl, benztropine, amantadine

trihex, benz: mucarinic blockers which restore DA-Ach balance in CNS

memory loss
hallucinations
anti DUMBBELS mad hatter stuff

243
Q

aliskiren

mech, SE (4)

A

direct renin inhibitor (renin converts angiotensinogen to AI)

fetal damage, cough, diarrhea, angioedema

244
Q

α1 receptor agonist (3)

clinical use?

A

phenylephrine, tetrahydrazoline, naphazoline

dry eye, decrease congestion intranasally

245
Q

golimumab

mech, use

A

binds to TNF molecule

ulcerative colitis, psoriatic arthritis, RA

246
Q

ß1 receptor blockers (5)

clinical use

A

OLOLs (metoprolol, acebutolol, alprenolol, atenolol, esmolol)

tx CHF, HTN, glaucoma

247
Q

nicotinic agonists (3)

A

nicotine, succinylcholine, varenicline (partial)

248
Q

thrombolytic agents (3)

mech, admin, SE

A

streptokinase, urokinase, Tissue Plasminogen Activator (TPA)

ENZYMES: convert plasminogen→plasmin, which causes clot breakup
also degrades fibrinogen, factors V and VII directly

given IV

prolonged bleeding time

249
Q

Toxicities of Cholinergic Agonists?

A

DUMBBELS:

Diarrhea
Urination
Miosis (pupil shrinkage)
Bronchodilation
Bradycardia
Excitation of CNS (paralysis, ataxia, siezures, amnesia)
Lacrimation
Salivation

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