Working My way Up Flashcards
(249 cards)
1
Q
lomitapide
mech, SE
A
ENZYME INHIBITOR: inhibits VLDL assembly in liver
hepatotoxic
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
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
1
Q
pralidoxime
use?
A
reverses permanent damage due to Acetylcholinesterase inhibitors
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
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
1
Q
bleomycin
mech, SE
A
intercalates with DNA→strand breakage
pulmonary fibrosis
1
Q
NIBs
mechanism
A
kinase inhibitors
2
Q
ß1 receptor agonists (2)
A
norepinephrine, dobutamine
2
Q
leuprolide
mech, use
A
stimulates GnRH receptor→initially ↑testosterone, then downregulates receptor and then ↓↓↓testosterone synthesis
tx prostate tumors
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)
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
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
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)
3
Q
highest potency glucocorticoids
A
dexamethasone, betamethasone
ISA:25
MCA: 0.01
duration 36-54h
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
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
5
Q
phosphodiesterase inhibitors (2)
mech
A
cilostazol, dipyridamole
ENZYME INHIBITOR: inhibits phosphodiesterase→↓cAMP breakdown→↓platelet activation
5
Q
What agent activates all adrenergic receptors?
A
epinephrine activates all α and ß receptors
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
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
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
7
Q
anastrozole
mech, use
A
inhibits aromatase enzyme (which converts testosterone to estrogen)
treats ladycancers
8
Q
flutamide
mech, use
A
blocks intracellular androgen receptor
tx prostate tumors
9
What are the toxicities of cocaine?
CNS (5), systemic (6)
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)
9
Phenytoin
mech, tox, clinical use, SE
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)
9
K+ sparing diuretics (4)
mechs, SE
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
11
Antinicotinic Agents (4)
succinylcholine (also a nicotinic agonist; depolarizes NMJ)
paracuronium, atracurium, rocuronium (nondepolarizing ACh receptor blockers on skeletal mm)
12
nicotine
mech
highly addictive: nicotine RECEPTOR AGONIST (may ↑DA)
enters CNS nearly instantly for a very short 'high' every puff
12
halogenated hydrocarbons
PK, clincal use, SE
very potent, but slower
maintains anaesthesia
```
malignant hyperthermia (↑↑Ca++ uptake by skmm→↑↑body temp)
liver dx with repeated exposure
```
12
nitroprusside
mech, clinical use, admin
very fast ↑cGMP→arterial and venous vasodilation→↓↓BP
DOC for HTN crisis
admin IV (quickly degrades to CN- in solution)
12
abatacept
mech, use
inhibits CD80 and CD86 receptors
treats RA
12
infliximab
mech, use, SE (5), admin
mAB binding to TNF molecule
RA, Chrohn's disease
admin IV
hypersensitivity (chimeric MAB);
itching, hypotension, fever
worsens TB/fungus infections
13
AFILs (+1)
mech, SE(6), clinical usage
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
14
cytarabine
mech
pyrimidine analog inhibiting DNA polymerase
15
etoposide
mech
inhibits topoisomerase II→irreperable DNA breaks
15
dactinomycin
mech
intercalates with DNA→interferes with RNA synthesis
17
cannabinoids (3)
mech, efx (8), tox (4), clinical use
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
18
atypical antipsychotics (5+5+1)
mech
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
20
Class III antiarrythmics (3)
mech, SE (6), clinical use
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
21
inhibitors of leukotriene system (3)
mech
zileuton inhibits E2 5-lipoxygenase in immune cells
zafirlukast, montelukast block leukotriene receptors on pulmonary smmm
22
anagrelide
general effect?
↓platelet formation, maturation, and number via unknown mechanism
22
non propionic acid, non acetic acid derived (6)
mech, SE
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)
22
abiraterone
mech, use
inhibits 17-hydroxylase lyase (CYP17)→ ↓testosterone synthesis
tx prostate tumors
23
Loop Diuretics (4)
mech, clinical use, SE (5)
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
24
minor inhibitors of TG synthesis (2), mech
icosapent ethyl, omega-3 fatty acids
inhibits enzyme
25
natalizumab
mech, use, SE
inhibits to α-integrins (INHIBITS RECEPTORS) on CD4 T-Cells
Crohn's Dx, MS
linked with progressive multifocal leukoencephalopathy (viral dx of CNS)
27
Common side effects of most local anaesthetics:
CNS (5)
systemic (2)
CNS: disorientation
drowiness
slurred speech
numbness
blurred vision
♥arrythmia/tachycardia
esters can cause allergic reactions
28
Third Generation Antidepressants (4)
mech, SE (7), PK
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)
30
CNS α2 agonists for HTN (2)
mech, SE, clinical use
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)
30
Angiotension Receptor Blockers (7)
mech, SE
ARTANs (losartan, irbesartan, valartan, candesartan, telmisartan, eprosartan, olmesartan)
blocks AII receptor on BVs, ↓aldosterone secretion
fetal abnormalities (cat X)
31
acomprosate
general effect?
↓↓EtOH craving
32
ADP receptor blockers (4)
mech, which drug(s) have SEs (2)
ticlodipine, clopidogrel, ticagrelor, prasugrel
RECEPTOR BLOCKER: blocks platelet ADP receptor
ticlodipine SEs: neutropenia, agranulocytosis
33
propofol
clinical use, mech, PK
most commonly used GA
ACTIVATES GABA, antiemetic
rapid onset, short duration
34
STATINs
mech, SEs (3)
ENZYME INHIBITORS: HMG-CoA reductase inhibitors→↑LDL uptake from blood
myositis→rabdomyolysis
teratogenic (preg. cat. X)
heatotoxic
35
What is the toxicity of caffeine (5), TI?
What are the withdrawal symptoms?
nervousness, insomina, tremors, cardiac arrythmias, and siezures
TI is roughly 100
w/d: headache, lethargy, irritability
35
Barbiturates (5)
mech, PK, SE, clinical uses
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
36
benzodiazepenes used as hypnotics (5)
mech, PK, clinical use, tox/SE (8)
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
37
sugammadex
use?
reverse effects of non-depolarizing antinicotinic agents (eg: rocuronium) by binding directly
39
LDOPA + carbidopa
mech, SEs (5)
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
39
define MAC, B/GC
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
39
central + peripheral acting HTN agents (3)
mech, clinical use
propranolol, reserpine, αMethyl-tyrosine
nonspecificßblocker, post-gang NT depletion, and tyrosine hydroxylase ENZYME INHIBITOR
αmethyl tyrosine treats pheochromocytoma
40
hydroxychloroquine
mech, SE (3)
taken up by macrophages, concentrated in lysosomes, and interferes with antigen processing
GI dysfunction, dermatitis,
irreversible retinal damage
41
Agents used to treat anemias due to chronic renal failure/chemo (3)
mech, SE (4)
epoeitin alfa, darbepoeitin, peginasetide
mimic/enhance activity of erythropoeitin
↑BP, ↑clotting, MI, stroke (due to ↑↑RBC count)
41
least potent glucocorticoids
cortisone (a prodrug→no topical admin), hydrocortisone
ISA:1
MCA: 1
duration 8-12h
42
class Ia antiarrythmics (3)
mech? SEs specific to drugs (8)
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)
44
dabigatran
mech, SE (2)
ENZYME INHIBITOR: directly inhibits thrombin (II)
metabd by CYP450
hemorrhage
45
What are the clinical uses of antihistamines (4)? What are they ineffective in treating?
dermatoses (itching, insect bites)
allergic rhinitis/conjunctivitis→ ↓ congestion, sneezing
antiemetic/antinausea→tx motion sickness
sedatives
DO NOT TREAT ASTHMA or COMMON COLD
45
metabolic side effects of glucocorticoids (3)
weight gain
fat redistribution (to abdomen, moon face, buffalo hump)
muscle wasting (thin arms, growth inhibition in children)
46
dopamine agonists (5)
mech, SE (5)
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.)
47
indirect acting cholinergic agonists (5)
mech
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
47
tolfacitinib
mech, SE
inhibits Janus Kinase→prevents effect of cytokines on gene expression (JAK-STAT)
↑infection chance, ↑malignancy
48
irinotecan
mech
topoisomerase I inhibitor
49
α2 receptor agonists (2)
clinical use?
clonidine, αmethylnorepinephrine
treat HTN, treat glaucoma
49
fulvestram
mech, use, SE (2)
blocks estrogen receptor
treats ladycancers
retinal changes, cataract formation
50
ACE inhibitors (7)
mech, SE (4)
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
50
vincristine
mech, admin
binds to microtubules→blocks cell mitosis
given IV
51
benzodiazepene used in general anaesthesia
admin?
midazolam, given IV
52
What are the toxicities of traditional antidepressants (1, 2, 3 gen)? (4)
siezures, respiratory depression, cardiac arrythmias, renal failure
52
neuroprotective Parkinsons drugs (2)
mech, PK, SE
selegiline, rasagiline
monoamine oxidase B ENZYME INHIBITORS
selegiline metabolised to meth. in body→severe insomnia (not with rasag)
52
cyclophosphamide
mech, admin
prodrug which alkylates DNA
oral/IV
54
combined α and ß receptor blockers for HTN (2)
mech, SE
labetalol, carvedilol
α1, ß1, and ß2 blockers!
postural hypotension, dry mouth
all the propanolol stuff (enters CNS)
55
propionic acid derivatives (7)
mech, SE
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)
56
agents always administered with LDOPA+carbidopa (2)
mech
tolcapone, entacapone
Catecholomethyltransferase (COMT) ENZYME INHIBITORS (prevents breakdown of DOPA in CNS)
56
mycophenolate mofetil
mech, use, SE
specific antimetabolite inhibiting inosine monophosphate dehydrogenase →inhibiting guanosine synthesis
transplants, lupus
```
GI cell disruption
bonemarrow depression (→thrombocytopoenia, megaloblastic anemia, leukopenia)
```
57
Class IV antiarrythmic (3)
mech
diltiazem, verapamil, nifedipine
CHANNEL BLOCKER :Ca++ channel blockers→↑♥ frefractory period
59
Local anaesthetics (general)
Structure, mech, PK, admin
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
60
niacin
mech, SEs (4)
ENZYME INHIBITOR: inhibits VLDL synthesis, ↑serum HDL
cutaneous flushing, itching (aspirin tx)
↑uric acid (gout risk)
↑DM incidence
61
amantadine
mech, SE(2)
antiviral agent which ↑release of stored DA from nerve terminals
insomnia, restlessness
62
second generation antihistamines (4)
mech? difference from first gen? tox? SE (3)?
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)
63
middle potency glucocorticoids
prednisone (a prodrug→no topical admin), prednisolone, triamcinolone
ISA:4
MCA: 0.25
duration 18-36h
64
aspirin
mech
ENZYME INHIBITOR: cyclooxygenase inhibitor→inhibits TXA2 synthesis→decreased platelet aggregation
64
behavioral changes associated with glucocorticoid uses (3)
euphoria/depression, psychosis, emotional lability
66
indirect cholinergic agonist Alzheimers tx (2)
donepezil, tacrine
66
methotrexate
mech, use, SE
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)
68
mannitol
mech, admin
admin IV;
not resorbed by tubule so H20 drawn out by osmotic efx
69
erbulin
mech
inhibits microtubules→prevents mitosis, causes apoptosis
70
agents used to treat partial siezures acting on NTs (5)
topiramate, gabapentin, tiagabine, vigabatrin (ACTIVATES GABA)
perampamel (INHIBITS glutamate activity)
71
Cholinergic blockers for COPD treatment (2)
mech? SE?
ipratropium, tiotropium
muscarinic receptors blockers on pulmonary smmm
dry mouth
73
fomeprazole
mech
INHIBITS EtOH dehydrogenase ENZYME
74
Bile acid binding resins (3)
mech, SEs (2)
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
azathioprine
mech, use, SE
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
bortezomib
mech, use
inhibits proteasome→inhibits antigen presentation by APCs
tx multiple myeloma
78
dexmedetomidine
mech, SE
an α2 agonist that induces sleep WITHOUT respiratory depression
↓BP, bradycardia
(see clonidine, αmethylDOPA)
79
ergot alkaloids (2)
mech, SEs (2)
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
dobutamine
mech
ß1 agonist creating strong inotropic effect
82
What are the effects of the H1 blockers (6) and H2 blockers (1)?
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
A deficiency in thiamine intake in chronic alcoholics causes what?
thiamine deficiency leads to Weirncke's Encephalopathy ("wet brain")
86
high potency antipsychotics (2)
mech
haloperidol, pimozide
strong D2 (dopamine) RECEPTOR ANTAGONIST
88
How is iron absorbed and transported in the body? How is it stored?
Iron is absorbed as Fe++, converted to Fe+++ and transported by transferrin
Iron is storred as ferritin
89
BV α1 blockers
mech, SE, clinical use
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
flumazenil
mech, admin
a benzodiazepene receptor blocker
IV admin
90
thiazide diuretics (2)
mech, SE (6), tox
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
beta blockers for HTN (6)
mech, SEs (7)
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
migraine agents (7)
mech, admin, SE
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
agets treating partial siezures acting on CNS ion channels (6)
lamotrigine, zonisamide, refinamide, lacosamide (BLOCKS Na+ Channels)
pregabalin (Blocks Ca++ channels)
ezogabine (K+)
93
muscarinic agonists (3)
muscarine, pilocarpine, bethanechol
94
leech saliva protein analogs (3)
mech, admin, clinical use
bivalirudin, desirudin, argatroban
ENZYME INHIBITOR: directly inhibits thrombin
Admin IV (first pass)
for px with HIT
95
aspirin
where most readily absorbed? mech?
most readily absorbed in stomach (weak acid)
inhibits cyclooxygenase (both COX1 adn COX2)→ ↓prostaglandin synthesis
96
amphetamines and methamphetamine
mech, PK, clinical use, efx (8)
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
What are the side effects of most antipsychotics? (9ish) What class of drugs do they interact with?
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
ester local anaesthetics (3)
clinical use, admin
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
midazolam
mech
ACTIVATES benzodiazepene RECEPTOR (enhances GABA)
101
reserpine
mech, SE
depletes post-ganglionic neuron NT "α1 blockade"→no vasoconstriction→↓BP
CNS: depression, behavioral SE, drowsiness
diarrhea
102
betalacept
mech, use, SE
inhibits CD80, CD86 receptors
for renal transplants
↑malignancy associated
103
longer acting agents for asthma treatment
mech, admin, SE (3)
formoterol, arformoterol, salmeterol, indicaterol
specific ß2 agonist
inhaled usually
tremor, tachycardia, ♥ palpitations (due to ß1 effect)
104
What agent is used to treat sickle cell anemia?
mech, SE
hydroxyurea
↑ fetal Hb production
mutagenic (preg. cat D)
104
Skin/mucosal damage associated with glucocorticoids (4)
easy bruising (skin thinning)
poor wound healing
acne
increased incidence of infection (eg: thrush)
106
First Gen Antidepressants (2)
mech, SE (9), PK
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
Opiate antagonists (3)
mech
naloxone, naltrexone, methylnaltrexone
opiate RECEPTOR antagonists
(can be used with oxycodone to ↓euphoria)
108
lomustine
mech, admin
prodrug which alkylates DNA
given IV
109
nitrous oxide
PK, SE
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
benzodiazepenes used to treat anxiety (7)
mech, PK, clinical use, tox/SE (8)
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
neuronal antispastics (3)
mechs
baclofen: GABA AGONIST
diazepam (and other benzos): GABA AGONIST
tizanidine: α2 agonist (see clonidine, αmethylDOPA)
112
ATGAM antithymocyte globulin
mech, use, SE
polyclonal antibody
treats acute renal transplant rejection
↑risk for allergic response
113
acetazolamide
mech, clinical use
carbonic anhydrase ENZYME INHIBITOR
tx Grand Mal siezures
also can be used as a diuretic, or to treat bipolar disorder!
114
benzodiazepene used to treat siezures
mech, tox, clinical use
diazepam
ACTIVATES GABAergic neurons
very high TI
used to treat Statuse Epilepticus (because it can be administered in large doses)
also Grand Mal
116
Synthetic opiate analogs (6)
mech, admin, clinical efx
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
imitinib
mech, use, admin, SE
protein kinase inhibitor of a kinase which turns off cell apoptosis
tx chronic myelogenous leukemia (CML)
given orally→causes edema
119
What 3 classes of drugs can be used to treat angina?
nitrates (DOC)
beta blockers
Ca++ channel blockers
120
5-fluorouracil
mech
pyrimidine analog inhibiting thymidylate syntetase→inhibits thymidine synthesis
121
Non-traditional sleep inducers (2)
mech, SE
ramelteon, tasimelteon
melatonin RECEPTOR AGONISTS (no eff on GABA)
sleepiness, fatigue, ↓testosterone
122
What are the desired effects of aspirin and other NSAIDs (4)? What are the SE/toxicities (8)? Where is it contraindicated (2)?
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
vorapaxar
mech, careful use where?
RECEPTOR BLOCKER: blocks platelet thrombin receptor
careful use in px with intracranial bleeding
126
warfarin
mech, PK, SE(4)
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
mipomersen
mech, admin
antisense mRNA: to apolipoprotein B→inh. VLDL synth in liver
only antihyperlipidemic given IV
130
'other' CNS stimulants (4)
mech, clinical use
modafinil, armodafinil, dexymethylphenidate, methylphenidate
REUPTAKE INHIBITORS
tx narcolepsy or ADHD
131
low potency antipsychotics (6+1)
mech
one has a nasty side effect--name and describe
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
rilonacept
mech, use, admin, SE
binds to IL-1 molecule!
admin subQ
RA; admin with methotrexate
NOT USED with TNF inhibitors (synergistic)
133
ustekinumab
mech, use
binds to IL-12 and IL-23 molecules
psoriasis
134
adalimumab
mech, use
binds to TNF molecule
RA
135
dantrolene
mech, SE (2), clinicale use
acts directly on muscle cells to inhibit Ca++ induced Ca++ release from SR
muscle weakness, hepatits
used to treat malignant hyperthermic sx
137
digoxin
mech, SE (5)
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
omalizumab
mech, admin?
anti IgE mAB
IV only
139
Shorter acting agents for treatment of asthma (1+5)
mech? admin? SE (3)?
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
nitrates (2)
mech, admin, SE(3)
nitroglycerin, isosorbide dinitrate
ENZYME ACTIVATOR: activates guanylate cyclase→↑↑cGMP→profound coronary vasodilation
nit IV, iso orally
hypotension, headache, skin flushing
142
N-acetyl cysteine
mech
used to treat acetaminophen overdose
a reducing agent to ↑glutathione (GSH) levels in liver
143
Factor X inhibitors (2)
mech, SE
apiXaban, rivaroXaban
ENZYME INHIBITORS: directly inhibits factor Xa
bleeding esp. after spinal surgery
144
What are the symptoms of opiate withdrawal (8)?
severe vasoconstriction: cold and clammy, runny nose, goosebumps
↑GI mobility: diarrhea, cramping
CNS: dysphoria, restless twitching, dilated pupils
145
What is the general mechanism and effects of caffeine?
CNS (4), systemic (4)
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
CV side effects of glucocorticoids (5)
stroke, CHF, MI, HTN, ↑intracranial pressure
147
anakinra
mech, admin, use, SE
blocks IL-1 receptor
admin subcutaneously
RA; admin with methotrexate
NOT USED with TNF inhibitors (synergistic)
148
GI side effects of glucocorticoids (3)
↑risk of ulcers, gastritic, GI bleeding
149
α1 receptor blockers (2)
clinical use
prazosin (HTN, BPH tx), phenoxybenzamine
150
sirolimus
mech, use, SE (3)
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
ixabepilone
mech
binds to microtubules
152
skeletal side effects of glucocorticoids (3)
osteoporosis
osteonecrosis
↓growth in children
153
tamoxifen
mech, use, SE (2)
blocks estrogen receptor
treats ladycancers
retinal changes, ↑cataract formation
155
Lithium
mech, SE/tox (9), PK
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
topotecan
mech
topoisomerase I inhibitor
157
ß2 receptor agonists (4)
clinical use?
metaproterenol, terbutaline, fenoterol, albuterol
158
Ca++ channel blockers for HTN
mech, SE(2)
IPINEs (nifedipine, nicardipine, amlodipine, felodipine)
blocks Ca++ influx into vasc smmm→no vasoconstriction
heartburn, worsens CHF
160
disulfiram
mech, SE
INHIBITS aldehyde dehydrogenase ENZYME
awful hangover (EtO buildup)
162
daunorubicin
mech, admin, SE
intercalates with DNA→produces free radicals
given IV
♥ muscle degeneration
163
carbamazepine
mech, clinical use, SE
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
buspirone
mech, PK
partial 5HT agonist for anxiolysis w/o sedative/hypnotic efx
slow onset
no X-rxn with benzos or EtOH
164
etanercept
mech, admin, use
binds to TNF
given subq
RA
165
endothelin blockers
mech, clinical use, SE(3)
ENTANs (bosentan, ambrisentan, macitentan)
endothelin receptor blocker on BVs
treats pulmonary HTN well
fetal damage, hepatic tox, testicular atrophy
167
Antimuscarinic agents (3)
SEs
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
leflunomide
mech, SE (4)
antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase
diarrhea, abdominal pain
teratogen (especially for lymphocytes)
inhibits CYP450
169
direct agonists of both muscarinic, nicotinic receptors (2)
acetylcholine, bethanechol
170
Class Ib antiarrythmics (2)
mech, admin, SE (2) clinical use
lidocaine, mexiletine
CHANNEL BLOCKER: Na+ channel blocker
lido IV, mex oral
CNS: tremors, siezures
not likely to cause arr, for Vtach
171
methohexital
clinical use, mech
general anaesthetic
GABA ACTIVATOR
171
mast cell inhibitors (2)
mech
cromolyn sodium, nedocromil
inhibits release of mediators from immune cells by INHIBITING Cl- CHANNELS, which ↓Ca++ uptake
173
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?
epinephrine
activates ALL α and ß receptors
inhaled or IV
SE: ↑HR (from ß1) and ↑BP (from α1 induced vasoconstriction)
174
carfilzomib
mech, use
inhibits proteosomes→inhibits antigen presentation by APCs
tx multiple myeloma
176
agents which affect absorption of lipids (4)
mechs, SE
sitostanol, orlistat, olestra, ezetimibe
```
AFFECTS TRANSPORT (sit, ol, ez): blocks cholesterol transporters in SI
ENZYME INHIBITOR (or): inhibits GI lipases
```
loose stools
178
diazoxide
mech, SE
opens K+ channels in arterial smmm→vasodilation
↓↓insulin secretion from ßcells in pancreas→hyperglycemia
180
Henderson-Hasselbalch stuff (ionized vs non ionized form)
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
THE non-narcotic analgesic
mech, tox (2)
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
Second Generation Antidepressants (7)
mech, SE (6), PK
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
botulinum toxin A
mech? clinical use?
inhibits ACh release from NMJ
cosmetically;
cerebral palsy, tics, strabismus, nystagmus
184
hemostatic agents (2)
mech
aminocaproic acid, tranexemic acid
ENZYME INHIBITOR: inhibits plasminogen activation
184
What other agents can be used to treat bipolar disorder? (5)
valproic acid, carbamazepene, lemotregene (anti-siezure)
acetezolamide (anti-diuretic/anti-siezure)
amiprazole (antipsychotic)
185
hydralazine
mech, SE
↑cGMP in art smmm→vasodilation
lupus like sx in slow acetylators
186
cocaine
mech, PK, clinical use, efx (7)
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
fenoldopam
mech, admin, clinical use
activates D1 receptors on BVs→vasodilation
admin IV for HTN crises
189
6-mercaptopurine
mech
prodrug purine analog inhibiting enzymes required for purine synthesis
190
fibrinogen receptor inhibitors (3)
mech, admin, SE, clinical use
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
etomidate
clinical use, mech, SE (2)
General anaesthetic
GABA RECEPTOR ACTIVATOR
relatively high TI, nausea
192
What is the synthetic path for glucocorticoids? Which reactions require P450?
cholesterol → pregnenolone → 17-OH pregnenolone → 17-OH progesterone →11-deoxycortisol → cortisol
all require CYP450 except the pregnenolone→17OHpregnenolone reaction
194
ketamine
clinical use, mech, PK, SE
Gen Anaesthetic
Glutamate RECEPTOR INHIBITOR
short induction and duration
dissociative anaesthesia: ↑↑↑amnesia and analgesia
can cause hallucinations
195
leucovorin
mech
a tetrahydrofolic acid analog which requires DHF Reductase
rescues cells methotrexate toxicity
197
ocular side effects of glucocorticoids (2)
cataracts, glaucoma
199
Name the primary cause of megaloblastic anemia. What are the symptoms of this condition? How is it treated?
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
fibrates (2)
mech, SEs(2)
gemfibrozil, fenofibrate
RECEPTOR INHIBITOR: binds to PPAR→ ↓TG, ↓VLDL, ↑LPLase synthesis
GI upset
displaces warfarin
202
trastuzumab
mech, use
blocks a HR2 receptor (a tyrosine kinase)
tx breast cancer
202
acetic acid derivatives (3)
mech, SE
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
What are the 4 classes of drugs used to treat congestive heart failure and how do they work?
cardiac glycosides (eg digoxin)--↑ contractility
ACE inhibitors--↓BP, ↓fluid retention
Beta blockers--↓HR
vasodilators--↓BP
(diuretics)
205
Semisynthetic opiate agents (3)
mech, admin, clinical efx
heroin, hydromorphone, oxycodone
opiate RECEPTOR AGONIST
heroin (5xM, IV), hydromorphone (10xM, IV), oxycodone (0.5xM partial agonist, avail orally)
206
adenosine
mech, admin, PK, clinical use
RECEPTOR AGONIST: binds to adenosine receptors→↓AV node firing
admin IV
t1/2=10 seconds (VERY SHORT)
for A-tach and coronary vasodilation
208
indirect acting amines--sympathetic agonists (5)
mech
amphetamine, methamphetamine, tyramine, phenylpropanolamine, pseuoephedrine
induce NE release from nerve terminals
210
Name some causes of macrocytic anemia. How is this condition treated?
Caused by folic acid deficiency (via pregnancy, infection, alcoholism, etc), which is required for DNA replication
treated with oral administration of folic acid
212
tocilizumab
mech, use
binds to IL-6 receptors on T-cells
RA
213
doxorubicin
mech, admin, SE
intercalates with DNA→produces free radicals
given IV
♥ muscle degeneration
214
Which reactions are CYP450 Phase I, non-CYP450 Phase I, or Phase II reactions?
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
paclitaxel
mech
forms abnormal microtubules
217
prednisone
mech, use
inhibits immune functioning
treats neoplasia of immune system (like leukemias, lymphomas)
218
teriflunomide
mech, SE
prodrug; converted to antimetabolite of pyridine inhibiting dihydroorotate dehydrogenase
diarrhea, abdominal pain
teratogen (especially for lymphocytes)
219
non-benzodiazepene hypnotics (3)
mech, SE (4)
zolpidem, zaleplon, eszopiclone
binds to α-subunit of benzo receptor (↓ effect on muscle relax or siezure activity)
↓inhibitions, bizzare behavior, sleep actions, hallucinations
220
ethosuximide
mech, SE (2), clinical use
inhibits Ca++ channels
GI upset, drowsiness
DOC for petit mal
221
certolizumab
mech, use
binds to TNF molecule
RA, Chrohn's Dx
222
bevacizumab
mech
blocks VEGF (vascular endothelial growth factor)→inhibits formation of blood supply to tumors
223
nonspecific ß blockers (5)
OLOLs (propranolol, timolol, carteolol, metipranolol, levobunolol)
224
acetazolamide
mech, clinical use
inhibits carbonic anhydrase→inhibits bicarbonate resorption in PCT
primary use is not as diuretic:
open angle glaucoma, MOUNTAIN SICKNESS, epilepsy, bipolar dx
225
malathion and sarin
mech?
irreversible AChE inhibitors (very potent nerve gases)
226
cisplatin
mech, SE(2)
alkylates DNA
renal damage, ototoxicity
227
MAOIs (3)
mech, SE/tox (10)
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
first generation antihistamines (6)
mech? clinical use for each? tox? SE (4)
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
rituximab
mech, use
blocks CD20 receptor
tx Chronic lymphocytic leukemia, RA
231
specific H2 blockers (4)
mech, SE
blocks peripheral H2 receptors (doesn't cross BBB)
cimetidine (has antiandrogenic efx→gynecomastia/galactorrhea)
ranitidine
tamotidine
nizatidine
232
everolimus
mech, use, SE (3)
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
methotrexate
mech, SE
folic acid antimetabolite inhibiting dihydrofolate reductase
myelosuppression (inhibition of blood cell formation)→fixed with leucovorin
234
basiliximab
mech, use, SE (4)
mAB that blocks IL-2 receptor
used with cyclosporine A
```
hypersensitivity rxns (chimeric)
HTN, bronchospasms, pulmonary edema
```
235
vinblastine
mech, admin
binds to microtubules→blocks cell mitosis
given IV
236
tetrodotoxin and saxitoxin
mech
irreversible Na+ channel blockers
237
ibritumomab
SE
its pure mouse, so superduper antigenic
238
amino amide local anaesthetics (8)
clinical use, admin, SEs
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
tacrolimus
mech, use, SE (5)
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
Class II antiarrythmics (3)
mech, SE (3)
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
minoxidil
mech, clinical use, SE
opens K+ channels in art. smmm.→inhibits contraction
for very refractory patients; also packaged as Rogaine
hypertrichosis, edema, cardiac tampanade
242
Anticholinergics for Parkinsons (2)
mech, SE (3)
trihexyphenidyl, benztropine, amantadine
trihex, benz: mucarinic blockers which restore DA-Ach balance in CNS
memory loss
hallucinations
anti DUMBBELS mad hatter stuff
243
aliskiren
mech, SE (4)
direct renin inhibitor (renin converts angiotensinogen to AI)
fetal damage, cough, diarrhea, angioedema
244
α1 receptor agonist (3)
clinical use?
phenylephrine, tetrahydrazoline, naphazoline
dry eye, decrease congestion intranasally
245
golimumab
mech, use
binds to TNF molecule
ulcerative colitis, psoriatic arthritis, RA
246
ß1 receptor blockers (5)
clinical use
OLOLs (metoprolol, acebutolol, alprenolol, atenolol, esmolol)
tx CHF, HTN, glaucoma
247
nicotinic agonists (3)
nicotine, succinylcholine, varenicline (partial)
248
thrombolytic agents (3)
mech, admin, SE
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
Toxicities of Cholinergic Agonists?
DUMBBELS:
Diarrhea
Urination
Miosis (pupil shrinkage)
Bronchodilation
Bradycardia
Excitation of CNS (paralysis, ataxia, siezures, amnesia)
Lacrimation
Salivation
