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Pharmacology dsorr
pharmacology
393
Pharmacology
Post-Graduate
12/11/2010

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Term
Increased FPE
Definition
- IV
Term
Vd
Definition
high-imipramine, olanzapine
low-heparin, warfarine
Term
PDE III inhibitors
Definition
"rinone" amrinone, milrinone, enoximone, vesnarinone

stop the breaking down of cAMP and gAMP
Term
cholinesterase inhibitors
Definition
pyridostigmine bromide
Term
beta blocker
Definition
"olol" propanalol
Term
Atropin
Definition
blocks muscarinic receptors-blocks parasympathetic-dry mouth-can't talk, mydiatris, no tears, constipation, bladder retention, increase heart rate, dilate lungs. blocks sweat glands-hyperthermia

small amount cause bradycardia by selectively blocking presynaptic receptors, taking away negative feedback and increasing para response.
Term
low therapeutic ratio
Definition
digoxin, theophyline, lithium, dimercaprol

antibiotics:gentamicin, amphotericin b, vancomycin, polymixin B
Term
PDE V inhibitors
Definition
"afil" used for ED, sildenifil citrate, vardenifil, tadalifil
Term
Na channel blockers
Definition
local anesthetics, anti-arrythmic, anti-epileptic
Term
local anesthetic
Definition
"-caine"- blocks Na channels, 1 I=ester, 2 I's= Amide
Term
cocaine
Definition
the only local anesthetic that vasoconstricts- releasing and blocking the reuptake of NTs (dopamine, norepi, epi)
Term
Ester vs. Amide
Definition
ester- short t 1/2,rapid plasma metabolism, possible allergic rxn, with low toxicity

Amide- long t 1/2, complex/hepatic metabolism, no allergic rxns, high dose can be toxic
Term
Vaughan-williams-singh classification
Definition
I. Na Channel blockers
A. slows phase 0 and 3
B. slows 0, speeds 3
c. slows 0
II. Beta Blockers
III. K blockers
IV. Ca blockers
V. Vagus boosters
Term
Torsade de pointes
Definition
can be caused by any porlongation of the K channels- class IA and III

Fix with IV Mg2+
Term
Supraventricular only
Definition
class IV
Term
broad range-supra and ventricular
Definition
Class IA- Quinidine, procainamide, disopyramide
Term
ventricular only
Definition
class IB- lidocaine, mexilitine
Term
class IC
Definition
flecainide
Term
quinidine sulfate
Definition
anti-arythmic- class IA- blocks muscarinic-decrease para, cinconism-blurred vision, tinnitus, headache. increase digitoxin toxicity. N and V, arrythmia
Term
Procaine-amide
Definition
anti-arythmic class IA-turns to class NAPA-N-acetyl procaineamide (class III) after phase II metabolism
Term
3 cyclic compound
Definition
can cause:
H1-receptor blocker:sedation
M receptor blocker: dry mouth
Na ch. blocker- arrythmia
K ch. blocker- arrythmia
alpha receptor blocker- hypotension
5HT blocker-weight gain
Term
phenytoin
Definition
Na and Ca channel block- anti-epilectic. gum hyperplasia, megaloblastic anemia, peripheral neuropathy, skin rash, hirsuitism, CNS symptoms, coursening of facial features

zero order kinetics
Term
endozepine
Definition
endogenous GABA agonist-opens cl- channel--> hyperpolarization
Term
carbolines
Definition
endogenous GABA antagonist
Term
GABA agonist
Definition
Benzodiazopine, barbiturate, propofol, alcohol
Term
Benzodiazipine
Definition

"zepam, zolam" hypnotic, amnestic, muscle tone decrease, anti-epileptic (no analgesia)

GABA agonist- opens Cl channels-hyperpolarize

Term
Short acting BDZ
Definition
TOMB
triazolom
oxazepam
midazolam
brotizolam
Term
intermediate acting BDZ
Definition
LETAL
lorazepam
estazolam
temazepam
alprozolam
loprazolam
Term
Long acting BDZ
Definition
DCNFF
Diazepam
Clotiazepam
Nitrazepam
Flurazepam
flunitrazepam
Term
BZD-no phase I
Definition
don't need liver TOL
Tomazepam
Oxyzepam
Lorazepam
Term
non-BDZ GABA agaonist
Definition
all begin with Z, extremely short lives, put you to sleep
Zaleplon
Zolpidem
Zopiclone
Term
Flumazenil
Definition
BDZ antagonist- replaces BDZ when overdosed with alcohol.
Term
Thiopental
Definition
barbiturate-hypnotic/sedative
Term
phenobarbital
Definition
barbiturate- anti-epileptic
Term
Propofol
Definition
GABA agonist, stardard used for anesthesia
Term
Vigabatrin
Definition
vigorous gaba transminase inhibitor
anti-epileptic-> slows GABA metabolism
Term
Tiagabin
Definition
gaba reuptake inhibitor- anti-epileptic
Term
Gabapentin
Definition
not a gaba agonist, trick,but antiepileptic
alpha-2-delta ligand- controls Ca+ channel permeability
(along with pregabalin)
Term
baclofen
Definition
presynaptic GABAb agonist- release NT, reduce muscle tone (treat spacicity)
Term
L calcium channels
Definition
slow voltage gates-Anti-arythmic

Myocardial vs. vasuclar
verapamil,diltiazem, nifedipine, felodipine, nimodipine
Term
T calcium channels
Definition
Transient (fast)- anti-epileptic/CNS
mibefradil, Succinimide, sulfanamide, valproylamide,

Hydantoins-both anti-epileptic and anti-artihmic-Na and K
Term
verapamil
Definition
phenyl-alkyl-amine- L calcium ch.
decreases HR and O2 demand, constipation, edema, increase digitoxin levels.
Term
nifedipine
Definition
dihydro-pyridine- L calcium ch.
Smooth muscle relaxation->vasodilation in arteries > veins, decrease afterload, decrease BP, increase HR,
t1/2= 3-4 hours
filo-dipine and nemo-dipine-longer half life (10 hours)
Term
Diltiazem
Definition
benzo-thia-zepine- L calcium ch.
decrease HR and O2 demand, CA vasospasm releif
Term
mibefradil
Definition
t-calcium channel blocker-blocks 3a4 metabolism-toxic effects, taken off market
Term
ethosuximide
Definition
t calcium ch, succinimide, anti-epileptic,
1st line against absence seizures
Term
methsuximide
Definition
t calcium channel, succinimide anti-epileptic
Term
zonisamide
Definition
t ca channel, sulfonimide, mixed moa
Term
valproate
Definition
t ca channel, valproylamide,
depakote
Term
folate antagnoism
Definition
triamterene, dapsone, phenytoin, trimethoprim, methotrexate
Term
NPQR
Definition
3rd group of Ca channel blockers- gabapentin and pregabalin
Term
Dantrolene
Definition
ryanodine receptor blocker, hydantoin derivitive, stops intracellular release of Ca+ in skeletal muscle
Use for hyperthermia relief-decrease mechanical work
Term
sotalol
Definition

K+ channel blocker and non specific beta blocker.

Blocks:

Beta 1-heart

Beta-2-lung->blocks sympathetic (bronchiodilation)->bronchioconstriction->bad for people with asthma

Term
Amiodarone
Definition
class X, does everything, 1 + 2 + 3 + 4,
also has every side effect
mostly K channel blocker
-not dialyzable
-half life of 58 days, 38 for active ingredient DEA
-can cause hypo/hyper thyroidism (similar structure to thyroxine)
pulmonary itis and fibrosis, hepatic LFT, metalic taste, photosenstitivity, grey color of face, peripheral neuropathy
Term
Sulfonyl-Urea (SU)
Definition
hypoglycemic drug- increase weight
Block K+ channels, depolarize Beta cells of pancrease,calcium released, triggers increase insulin, decrease blood glucose

"Gl-"
1st-tolbutamid
2nd- Glibenclamid, glyburide, glipzid, 3rd- glimepirid
Term
metformin
Definition
used for metabolic syndrome, not K+ channel blocker
-suppresses hepatic glucose production
Term
Glinide
Definition
non-sulfonyl-urea insulin release
ROSA-rapid onset, short acting
repaglinid, nateglinid
-no weight gain (like sulfonyl-ureas)
Term
Nicorandil
Definition
K+ channel opener, aterial relaxation, treatment for angina, HT, congestive heart failure
-decrease O2 demand for heart-relief against angina
-can cause oral ulceration
Term
Dronadarone
Definition
class X, a less toxic amiodrarone. no thyroid function, less lipophilic, lower Vd
Term
glutamate
Definition
endogenous NMDA agonist- (w/e aspartate)
Term
aspartate
Definition
endogenous NMDA agonist(w/ glutamate)
Term
Zinc
Definition
endogenous NMDA antagonist (w/ Mg)- makes you sleepy
Term
Mg
Definition
Endogenous NMDA antagonist (w/ zinc-makes you sleepy)-lowers blood pressure, also side effects:lowers HR, RR, CNS, muscle force/reflex
Term
Ketamine
Definition
PCP- non-competitive NMDA antagonist (also blocks everything else)
-analgesic and not a respiratory depresent
S (+) form-eutomer-good form
Term
sympathomimetic anaesthesia
Definition
increase RR, HR, BP, O2 consumption, bronchodialation
Term
parasympathomimetic anaesthesic
Definition
bronchorhea-increase gland secretion and
sialorhea-increase saliva-->give atropine
Term
psychomimetic anaesthesia
Definition
vivid dreams- give GABA agonist-BDZ
Term
mementine
Definition
non-competitive NMDA antagonist, a better Mg
-does not affect reversible effect of cholinesterase inhibitors (donepezil, revastigamine, galantamine, tacrine
Term
cholinesterase inhibitor
Definition
donepezil, revastigamine, galantamine, tacrine
Term
methadone
Definition
mew opiate receptor agonist and NMDA antagonist
-long onset with long half life-helps cure chronic pain
-mostly used for heroin addiction
-10 times morphine
Term
opiate receptors
Definition
-mew- open K channel-hyperpolarize-supra-spinal-endorphine
-kappa- inhibit Ca channel and NT release-spinal-dynorphine
-Delta- modulate mew-supra-spinal-enkepharine
Term
Lamotrigine
Definition
anti-epileptic-glutamate release inhibitor. Na channel blocker
Term
felbamate
Definition
anti-epileptic-glycine (co-activator for NMDA) antagonist, GABA agonist
Term
topiramate
Definition
anti-epileptic- AMPA antagonist and GABA agonist
-induces weight loss (thin and stupid)
-blocks carbonic anhydrase- can't taste soda-can't turn CO2 to carbonic acid, also may cause parethesia (tingling), nephrolithiasis
-Ca and Na channel blocker
-causes myopia and glaucoma,
-dopamine release inhibitor-oligohidrosis (can't sweat)-->hyperthermia
-mentally slow (stupimax)
Term
5-HT receptors
Definition
1A-agonist-pirones-anxiety, piril-HT
1D/F-agonist-triptans-migraines
2-antagonist-psychosis
3-antagonist-setrons-emesis
4-agonist-prides-gastroperisis
RI-depression
Term
urapidil
Definition
hypertension medication
works with 5-HT-1A receptor agonist
and alpha-1 receptor antagonist
Term
5-HT-1 receptor
Definition
g-protien-metabolotropic-inhibitor of adenylyl cyclase (which makes cAMP)
Term
Buspirone
Definition
anti-anxiety- mostly 5-HT-1A agonist, dopamine, and 5-HT-2
-slow onset (4-6 weeks), give BDZ
Term
sumatriptans
Definition
5HT-1 D (reduce nociceptor transmission)/B (aterial-cerebral vasocontstriction)receptor agonist
-more triptan given,less affinity to brain, vasoconstriction, increase BP
-Don't give to someone with cardiovascular disease
Term
naratriptan
Definition
5HT-1 D (reduce nociceptor transmission)/B (aterial-cerebral vasocontstriction)receptor agonist
-use cytochrome for metabolism (not MAO A)
-more triptan given,less affinity to brain, vasoconstriction, increase BP
-Don't give to someone with cardiovascular disease
Term
MAO-A inhibitor
Definition
stop degradation of NE and 5-HT, used for depression
-st. john's wart
Term
MAO-B inhibitor
Definition
stops degradation of dopamine
-anti-parkinson-->increase dopamine, decrease GABA
Term
Selegeline
Definition
stops degradation of dopamine
MAO B inhibitor-anti-parkinson-->increase dopamine, decrease GABA
Term
Moclobemide
Definition
-MAO-A inhibitor
-stop degradation of NE and 5-HT, used for depression
-mild, similar to st. john's wart
Term
5-HT 2
Definition
stimulate DAG, IP3, PKC and release of calcium
Term
pizotifen
Definition
5-HT-2 antagonist (also H1 antagonist)-prevention of migraines (profalaxis)
Term
Mianserin
Definition
5-HT 2 antagonist- depression and anxiety
Term
ritanserin
Definition
5-HT- 2 antagonist- depression and anxiety
Term
Ketanserin
Definition
5-HT 2 antagonist- anti-hypertensive (w/ alpha 1 antagonist-postural hypotension)
-reynaud's disease- cold, discolored hands and feet because of lack of blood
Term
Nefazadone
Definition
5HT 2 antagnosit and SSRI- removed from market
Term
Trazodona
Definition
5HT-2 antagnosist with SSRI
Term
Quetiapine
Definition
D2=5HT-2 antagonist
-psychosis/schitzophrenia
-also has alpha 1 antagonist-hypotension
-H1 antagonist-sleepy
Term
Olanzapine
Definition
D2<5HT 2-
phycosis/schizophrenia
-H1, alpha 1, Ach (muscarinic), side effect
Term
Ziprasidone
Definition
D2<<5HT 2 antagonist
-H1, alpha 1 antagonist side effect
-psychosis,schizophrenia
Term
Aripiprazole
Definition

5HT1A agonist and 5HT-2 antagonist -psychosis -no CYP450 metabolism

-no QT elongation

Term
palanosetron
Definition
-ionotropic, 5 HT 3 antagonist, anti-emetic (reduce vomiting)
-given pre-chemo
-extremely long half life (56 hours-compares to 10 hours with dolasetron, granisetron, ondansetron)
Term
Ilosetron
Definition
5-HT-3 antagonist- used for IBS (diarrhea)
-removed from market
Term
Metoclopramide
Definition
-5HT4 agonist-increases gastic emptying
-5HT3 antagonist-anti-emetic
-cholinesterase inhibitor
-D2 antagonist- anti-nausea, anti-vomiting
-cause tardive dyskinesia and NMS (nueroleptic malignant syndrome)
Term
Cisapride
Definition
-5HT 4 agonist
-promote gastric emptying with diabetes side effects (autonomic neuropathy)
-removed from market- QT elongation-Torsade
Term
Mosapride
Definition
5-HT-4 agonist-
-increase gastric empyting
Term
itopride
Definition
5-HT-4 agonist-
-increase gastric empyting
-AchE inhibitor
-D2 antagonist
Term
tegaserod-
Definition
5-HT-4 agonist-
-increase gastric empyting
-5HT 2 antagonist-
used for IBS
-taken off market because of cardiac events and ischemic colitis
Term
SSRI
Definition
fluoxetine (54), flovoxamine, sertralin, paroxetine, citalopram (3400 times more 5-HT reuptake inhibitor than NE)
-delayed ejaculation and hyperthermia
-more increase in serotonin, more hyperthermia
Term
Fluvoxamine
Definition
-SSRI- worst side effects with inhibition of most cytochrome metabolism
Term
citalapram
Definition
most selective SSRI with minimal inhibition of cytochrome metabolism
Term
Venlafaxin
Definition
-NeSRI- new anti-depressent, like old 3-cyclic but with less side effects
-also used for chronic pain therapy
-major metbolite also used as drug-desvenlafaxine
Term
capsiacin
Definition
hot pepper-activates pain
Term
dynophine
Definition
kappa opioid receptor, inhibit Ca+ channel-->decrease NT release-spinal
-dysphoria, psychoto-mimetic effects, low addiction potential
Term
endorphine
Definition
mew opioid receptor, open K+ channel-->hyperpolarization
-supraspinal
-eurphoria-highly addictive
-respiratory depression-forget to breathe-stop hypercapnia relfex
-bradykardia,obstipation (give laxitive), urinary retention, miosis, highly addictive
Term
enkephaline
Definition
delta opioid receptor, modulates mew
Term
morphine
Definition
mew agonist
-itching=histamine release-->also, increases HR, bad for CAD
-emesis-D receptors
-t1/2= 3 hours
Term
piritramid
Definition
mew agonist
-.8 morphine, no itching
Term
codeine
Definition
methyl-morphine-must be metabolized to take effect (3A4 and 2D6)
-1/10 morphine
Term
Tramadol
Definition
-mew agonist (weak)
*NeSRI-anti-depresent-->mostly used for chronic pain
-central alpha 2 agonist
Term
Pentazocine
Definition
kappa-agonist, weak mew agonist
-dysphoria
-can have withdrawal syndromes
Term
Remifentanil
Definition
mew agonist, 100 times morphine, ultrashort half life
Term
sufentanil
Definition
mew agonist, most potent at 1000 times morphine
Term
pethidin
Definition
-mew agonist, 1/10 morphine
-anticholingergic, SSRI-->hyperthermia- major cause of hyperthermic conditions when coupled with other anti-depressants or ecstasy.
-alpha blocker-postural hypotension
-muscarinic blocker-only opiate that gives mydriasis (usually myosis)
Term
meperidine
Definition
-mew agonist, 1/10 morphine
-anticholingergic, SSRI-->hyperthermia- major cause of hyperthermic conditions when coupled with other anti-depressants or ecstasy.
-alpha blocker-postural hypotension
-muscarinic blocker-only opiate that gives mydriasis (usually myosis)
Term
Naloxone
Definition
mew receptor antagonist-antidote for overdose
Term
emesis therapy
Definition
-dopamine 2 blocker
-5-HT 3 blocker
-anti-muscarinic-blocks vestibular nucleus emesis (motion sickness)
Term
Droperidol
Definition
-D2 blocker
-anti-emesis
Term
metoclopramid
Definition
-D2 blocker with 5HT-3 antagonist and 5-HT4 agonist
-anti-emesis
-reglan-off market
-NMS and tardive dyskinesia
Term
scopolamine
Definition
-muscarinic antagonist
-motion sickness
-close relative of atropine-->touch patch-touch eye-->mydriasis in one eye
Term
nueroleptic/antipsychotic
Definition
D2 antagonist
-phenothiazine
-butyrophenones
-thioxanthenes
-benzamides
Term
H1 blocker-
Definition
-anti-itch
-sedation/weight gain "fat and tired"
Term
D2 antagonist
Definition
-anti-psychotic
-extra-pyramidil-parkinson-like
-anti-emetic
-prolactin release
Term
alpha-1 blocker
Definition
-hypotension (postrual)
-nasal congestion
Term
Na or K channel blocker
Definition
-torsade- QT elongation
Term
chlorpromazine
Definition
-Phenothiazine-TC
-anti-psychotic
-TC-side effects
Term
Laborit's Lytic cocktail
Definition
-Phenothiazine-TC
-anti-psychotic
-artificial hybernation-DPT
-demerol-pethidine/meperidine
-phenergan-promethazine
-Thorazine-chlorpromazine
Term
promethazine
Definition
-Phenothiazine-TC
-anti-psychotic
-blocks histamine-anti-itch and sedative
-blocks muscarinic-anti-motionsickness

-part of coast guard cocktail with ephedrine (amphetamine)-activates sympathetic
Term
prochlorperazine
Definition
-Phenothiazine-TC
-anti-psychotic
-used to treat drug induced nausea (w/ migraines)- cheap form of setrons/triptans
Term
fluphenazine
Definition
-Phenothiazine-TC
-anti-psycotic
-depot-inject for long lasting
Term
trifluoperazine
Definition
-Phenothiazine-TC
-anti-psychotic
Term
haloperidol
Definition
-butyrophenone
-highly selective,potent D2 blocker-->parkinson-like side effects
-->leading to irreversible tardive dyskinesia
-decrease Ach to decrease Ach dominance
Term
Phenothiazine
Definition
-Tricyclic-anti-psychotic
-H1, M, D2, alpha, Na/K side effects
Term
Benztropine
Definition
-Acetylcholine blocker (anticholinergic)-used to treat dystonia and parkinson-like symptoms
Term
Trihexyphenidyl
Definition
-anticholinergic-stops parkinson-like symptoms
Term
Diphenhydramine
Definition
-benadryl-anti-histamine and anticholinergic-makes you sleep
Term
Amitriptyline
Definition
-TC anti-depressant-side effects-preferred over clean venlafaxin because it makes you tired
-imipramine-other TC anti-depressant
Term
Amantadine
Definition
- anticholinergic-->stops parkinson-like symptoms
-decreased dopamine increases Ach-->parkinson
-w/ rimantadine(influenza antiviral)
Term
clozapine
Definition
-atypical anti-psychotic (shift to 5HT2)
-effective against negative (autistic) symptoms
-D2 blocker in limbic only-->no EPS
-causes agranulocytosis(stops WBC production and lowers immune)-->must monitor blood
-H1, alpha (with reflex tachycardia), QT elongation
-HYPERSALVATION
-hyperthermia
-seizures
-weight gain (10 in 10)
-increase TGs and GLU (diabetogenic)
Term
Olanzapine
Definition
-atypical anti-psychotic
-clozapine without the agranulocytosis
Term
Risperidone
Definition
-atypical anti-psychotic
-similar to clozapine (5HT2 > D2-atypical only at low dose)
-half the weight gain
-D2 side effects-EPS and increase prolactin
-QT elongation
Term
Ziprasidone
Definition
-atypical anti-psychotic
-NeSRI
-5-HT2 antagnosit
Term
Thioxanthines
Definition
-first atypical group of anti-psychotic
-shift to 5HT2 antagonism and less D2-->less/no EPS
Term
Benzamide
Definition
-Pure D2 blocker anti psychotic
-antidepressive
-sulprimide
-amisulprimide-no weight gain
-remoxipride
Term
Quetiapine
Definition
-atypical anti-psychotic
-cataract development
-hypothyroidism
Term
aripiprazole
Definition
-anti-psychotic
-5HT2-antagonist (synergystic with 5HT1 agonist)
-D2 partial agonist
-parkinson-like
Term
amisulpirid
Definition
-anti-psychotic
-only one not metabolized by CYP450
Term
Parkinson therapy
Definition
1.give levodopa with ddc inhibitor
2.MAO B inhibitor
3.ergontimin
4.non-ergontimin
5.Muscarinic blockers-->decrease Ach action
6. COMT inhibitor
Term
Dopamine-
psychosis
parkinson
weight
temperature
emesis
BP
Definition
Dopamine tracts
1. Nigostriatal- movement
-decrease dopamine-increase parkinson
2. Mesolimbic-mesocortical tracts-
-euphoria-addiction-increased dopamine
-positive symptoms of psychosis-increased dopamine
-decrease dopamine-->decrease cognitive function-->anti-psychotic
3. Tuberinfundibular-
-increase dopamine-decrease prolactin and GH
-decrease dopamine-reset thermostat-->hyperthermia
-increase dopamine-lose weight
4. Chemoreceptor trigger zone-
-increase dopamine-increase emsis
5.dopamine is a vasodilator-->hypotension
Term
levodopa
Definition
-always given with carbidopa
(inhibitis conversion in periphery)
-anti-parkinson
Term
bromcriptine
Definition
-ergotamine dopamine receptor agonist
-anti-parkinson
-increase dopamine in lymbic system->psychosis
-increase dopamine in CRTZ-> N and V
-hypotension
*pulmonary and retroperitoneal fibrosis
*vasospasm
-GI ulceration
Term
Ropinrole
Definition
-non-ergotamine dopamine receptor agonist
-anti-parkinson
-increase dopamine in lymbic system->psychosis
-increase dopamine in CRTZ-> N and V
-hypotension
*NO pulmonary and retroperitoneal fibrosis
*NO vasospasm
-GI ulceration
Term
pramipexole
Definition
-non-ergotamine dopamine receptor agonist
-anti-parkinson
-increase dopamine in lymbic system->psychosis
-increase dopamine in CRTZ-> N and V
-hypotension
*NO pulmonary and retroperitoneal fibrosis
*NO vasospasm
-GI ulceration
Term
enracapone
Definition
-COMT inhibitor(stops the breakdown of dopamine)
-anti-parkinson
Term
central antihttp://www.flashcardmachine.com/my-flashcards/quick-editor.cgi-cholinergic syndrome
Definition
-caused by excess atropine
-can't sweat, vasodilation to decrease body temperature (red), hot, blind, hallucinate
Term
cholinesterase inhibitor
Definition
DUMBBELLS
-diarrhea
-urination
-miosis
-bronchorhea, bronchospasm
-bradykardia
-emesis
-lacrimation-bloody tears
-laxation
-salivation

-parasympathetic rxns-->opposite of atropine
Term
lipocortin
Definition
-steroids(glucocorticoids) inhibit lipocortin (annexin), which inhibit phospholipase A2, which no longer cuts arachidonic acid which will then no longer bind to COX and LOX to cause inflammation
Term
COX1B
Definition
-selective COX inhibitors (only COX 2)
-stop the production of prostoglandins, prostacyclins, thromboxane (endoperoxides)-->inflammation
Term
NSAID
Definition
-non-selective COX inhibitors
-stop the production of prostoglandins, prostacyclins, thromboxane
Term
zilueton
Definition
-LOX inhibitor
-stop the production of luekotriens
Term
montelukast
Definition
-leukotrien receptor blocker-->stop inflammation
Term
side effects of COX inhibitor
Definition
1.stomach/intestinal-prostoglandins (+) regulate mucosal secretion-->decrease PG, decrease mucosal-->uclers
2.kidney-prostocyclan vasodilates afferent arteries-->decrease PC, vasoconstrict, decrease blood supply
-fix by blocking adenosine (vasoconstrictor) with xanthenes
3.inhibit platelet aggregation-->increase bleeding and blood flow
Term
ASA
Definition
-asprin, NSAID
-increase LOX-->bronchoconstriction
-don't give to children-->cause reye disease because of virus
-causes hepatitis and cerebral edema
Term
diflunisal
Definition
NSAID
Term
Diclofenac
Definition
-NSAID, specifically for joints and bones
Term
Ketorolac
Definition
-most potent NSAID, used IV for acute pain
Term
"profen"
Definition
NSAID
Term
NSAID
Definition
indomethacin, ketorolac, sulindac, tometin,tiaprofenic acid, naproxen, phenylbutazone, piroxicam, tenoxicam
Term
celecoxib
Definition
-selective COX2IB
-50:1 COX2:COX1, selective
-Most off the market because increase incidence of cardiovascular incidents (also with NSAIDS)
Term
Acetaminophin
Definition
-COX3 inhibitor
-antipyretic and analgesic with no anti-inflammatory effect
-usually phase II but with some phase I metabolism-->NAPQI-->liver necrosis and fibrosis
Term
Paracetamol
Definition
-COX3 inhibitor
-antipyretic and analgesic with no anti-inflammatory effect
-usually phase II but with some phase I metabolism-->NAPQI-->liver necrosis and fibrosis
Term
N-Acetyl-Cystein
Definition
-NAC-give IV when potention COX3 overdose (acetaminophin or paracetamol)
-only side effect-->H1 agonist->vasodilation
Term
Metamizol
Definition
-COX3 inhibitor
-vasodilator,antipyretic, analgesic-->smooth muscle relaxant-->gall bladder and kidney pain (spasmolytic effect increase)
-decrease BP if giving IV
Term
Dipyrone
Definition
-COX3 inhibitor
-vasodilator,antipyretic, analgesic-->smooth muscle relaxant-->gall bladder and kidney pain (spasmolytic effect increase)
-decrease BP if giving IV
Term
ranitidine
Definition
"tidine"
-H2 blocker-->decrease gastric acid production
Term
betahistine
Definition
-anti-vertigo, potential for alzheimers
-H3 blocker-->presynaptic membrane receptors blocked-->decreease (-) feedback-->increase NT release
Term
H1 blocker
Definition
-stops allergic rhinitis and allergies
-also a sedative when crossing BBB
-1st generation-non-selective (M, alpha, etc.), CNS, short 1/2 life
-2nd generation-selective, limited/no CNS, CYP metabolized (leads to torsade-many removed from market), intermediate 1/2 life
-3rd generation-selective, no CNS, not CYP metabolized, long 1/2 life
Term
Chlorpheniramine
Definition
--1st generation-non-selective (M, alpha, etc.), CNS, short 1/2 life
-hypotension-->don't give to old people
Term
clemastine
Definition
-1st generation-non-selective (M, alpha, etc.), CNS, short 1/2 life
-hypotension-->don't give to old people
Term
-dyphenhydramine
Definition
-1st generation-non-selective (M, alpha, etc.), CNS, short 1/2 life
-hypotension-->don't give to old people
Term
promethazine
Definition
--1st generation-non-selective (M, alpha, etc.), CNS, short 1/2 life
-hypotension-->don't give to old people
-part of coast guard cocktail
Term
cyclizine
Definition
-1st generation-non-selective (M, alpha, etc.), CNS, short 1/2 life
-hypotension-->don't give to old people
Term
meclizine
Definition
-1st generation-non-selective (M, alpha, etc.), CNS, short 1/2 life
-hypotension-->don't give to old people
Term
cetrizine
Definition
-2nd generation-selective, limited/no CNS, CYP metabolized (leads to torsade), intermediate 1/2 life
Term
loratidine
Definition
-name lies, not H2 blocker
-2nd generation-selective, limited/no CNS, CYP metabolized (leads to torsade), intermediate 1/2 life
Term
levocetirizine
Definition
-3rd generation-selective, no CNS, not CYP metabolized, long 1/2 life
-really expensive
Term
fexofenadine
Definition
-3rd generation-selective, no CNS, not CYP metabolized, long 1/2 life
-really expensive
Term
rupatidine
Definition
-3rd generation-selective, no CNS, not CYP metabolized, long 1/2 life
-really expensive
Term
clofibrate
Definition
-PPAR-alpha
-used for hyperlipidemia
-binds to PPAR-alpha, increases amount of LPL synthesized, lowers TGs, VLDL, LDL
-lowers cholesterol moderately (use statins)
-increases HDL moderately (exercise or use niacin)
-Increases gall bladder stones
-rhobdomyolysis when combined with statins
Term
Gemfibrozil
Definition
-PPAR-alpha
-used for hyperlipidemia
-binds to PPAR-alpha, increases amount of LPL synthesized, lowers TGs, VLDL, LDL
-lowers cholesterol moderately (use statins)
-increases HDL moderately (exercise or use niacin)
-Increases gall bladder stones
-rhobdomyolysis when combined with statins
Term
Thiazolidinediones
Definition
-PPAR-gamma
-used for diabetes type II, increase insulin sensitivity
-"-glitazone"
-do not cause hypoglycemia (sufonyl-urea and repaglinide does)
-slow onset: 2-6 weeks
-lowers HbA1c (glycosylated Hb)
-weight gain (H20 volume)-->heart failure
-can't use with hepatic damage
Term
Troglitazone
Definition
-PPAR-gamma
-first on market-->taken off because hepatotoxicity
-used for diabetes type II, increase insulin sensitivity
-"-glitazone"
-do not cause hypoglycemia (sufonyl-urea and repaglinide does)
-slow onset: 2-6 weeks
-lowers HbA1c (glycosylated Hb)
-weight gain (H20 volume)-->heart failure
-can't use with hepatic damage
Term
Rosiglitazone
Definition
-PPAR-gamma
-used for diabetes type II, increase insulin sensitivity
-do not cause hypoglycemia (sufonyl-urea and repaglinide does)
-slow onset: 2-6 weeks
-lowers HbA1c (glycosylated Hb)
-weight gain (H20 volume)-->heart failure
-can't use with hepatic damage
Term
Pioglitazone
Definition
-PPAR-gamma
-used for diabetes type II, increase insulin sensitivity
-do not cause hypoglycemia (sufonyl-urea and repaglinide does)
-slow onset: 2-6 weeks
-lowers HbA1c (glycosylated Hb)
-weight gain (H20 volume)-->heart failure
-can't use with hepatic damage
Term
Aspart
Definition
-ROSA insulin
-AA acid switch-->monomeric
-eat 10 minutes after dosing
Term
Lispro
Definition
-ROSA insulin
-AA acid switch-->monomeric
-eat 10 minutes after dosing
Term
Lispro
Definition
-ROSA insulin
-AA acid switch-->monomeric
-eat 10 minutes after dosing
Term
Regular insulin (soluble)
Definition
-not true ROSA
-non-crystalized with zinc-->most dimeric, some hexameric
-only IV insulin
-can also be used for hypercalemia
Term
NPH
Definition
-neutral protamine hagedorn (isophane) insulin
-addition of protamine with zinc-->hexameric
-intermediate action (onset in 1-2 hours)
Term
Lente
Definition
-SOLA-slow onset/long acting insulin
-precipitation with higher zinc concentration (70/30)
Term
unltra-lente
Definition
-SOLA-slow onset/long acting insulin
-precipitation with higher zinc concentration (100% crystaline)
Term
glargine
Definition
-SOLA-slow onset/long acting insulin
-add amino acids-->insoluble
Term
detemir
Definition
-SOLA-slow onset/long acting insulin
-add amino acids-->insoluble
Term
psuedohyperaldosteronism
Definition
-licorice can inhibit the enzyme HSD11B2
-This enzyme usually deactivates glucocorticoids which if not deactivated, will activate MC receptors
Term
Hydrocortisone
Definition
-AIE/MCE-1/1
-similar to cortison (.8/.8)
-minerocorticoid and glucocorticoid (short acting)
Term
fludrocortisone
Definition
-AIE/MCE- 1/10
-MC
Term
deoxycorticosterone
Definition
-AIE/MCE- 0/10
-MC
Term
Prednison
Definition
-AIE/MCE- 4/.3
-intermediate acting GC
Term
prednisolone
Definition
-AIE/MCE- 5/.8
-intermediate acting GC
Term
triamcinolone
Definition
-AIE/MCE- 4/.3
-intermediate acting GC
Term
methasone
Definition
-AIE/MCE- (10, 30, 36)/0
-long acting GC
Term
beclomethasone
Definition
-inhaled steroid
-lowest receptor infinity
-increased FPE makes safe
-also metabolized in lung to slow cleared metabolite
Term
Fluticasone
Definition
-inhaled steroid
-highest receptor affinity and increased FPE
-bioavailablilty around 10%
Term
budesonide
Definition
-inhaled steroid
-high receptor affinity and increased FPE
-bioavailablilty around 10%
Term
Flunisolide
Definition
-inhaled steroid
-high receptor affinity and increased FPE
-bioavailablilty around 20-30% (higher than others)
Term
rimonbant
Definition
-cannabinoide antagonist
-used to lose weight
-bad mood-->taken off market
Term
ropivacaine
Definition
-local anesthetic (Na channel blocker)
-longest duration of action (420 minutes)
Term
digoxin
Definition
class V
-slows conduction velocity of AV node
-controls atrial flibrillation and flutter
Term
adenosine
Definition
-class V
-abolishes acute supraventricular tachychardia
-extremely short duration of actiong (15 seconds)
Term
minoxidil
Definition
-similar mechanism to nicorandil-->opens K channels-->hyperpol-->vasodilation
-not used for BP, used for hair growth
-rogaine
Term
depoxetine
Definition
-short acting SSRI-->used for premature ejactulation
Term
Ethacrynic Acid
Definition
-non sulfonamide loop diuretic (high ceiling)
-used when patient w/sulfonamide allergy
-loop diuretic-high ceiling
-"semide" oral and IV
-secreted with PSOASS-->ascending loop of henle
-inhibition of NA/2CL/K cotransport
-increase urine volume,broncho/vaso dilation,smooth muscle relaxation,uric acid,glucose,TG,
-decrease renal 02 consumption,CSF production,CA,K,Mg,Ca,Cl,HDL,acid
-GFR and RPF unchanged-save on renal
-Ototoxicity-cochlear>vestibular
-IV use for glaucoma/IOP, ICP, pulmonary edema, ARF
-Oral use- decrease BP, Cardiac and Renal insufficiency
Term
Furosemide
Definition
-"the" loop diuretic-high ceiling
-"semide" oral and IV
-secreted with PSOASS-->ascending loop of henle
-inhibition of NA/2CL/K cotransport
-increase urine volume,broncho/vaso dilation,smooth muscle relaxation,uric acid,glucose,TG,
-decrease renal 02 consumption,CSF production,CA,K,Mg,Ca,Cl,HDL,acid
-GFR and RPF unchanged-save on renal
-Ototoxicity-cochlear>vestibular
-IV use for glaucoma/IOP, ICP, pulmonary edema, ARF
-Oral use- decrease BP, Cardiac and Renal insufficiency
Term
probenecide
Definition
-Probenecide sensitive organic anion secretory system-PSOASS
-used to block receptor and keep penicillin in system
-transporter also competitive with uric acid
Term
tinnitus
Definition
-coclhlear>vestibular
-caused by NSAIDS, Loops, Mycin (antibiotics), quinine, cisplatin (chemo)
-CAVE-combo chemo treatment-aminoglycoside (mycin) and cisplatin
Term
Torsemide
Definition
-loop diuretic-high ceiling
-"semide" oral and IV
-secreted with PSOASS-->ascending loop of henle
-inhibition of NA/2CL/K cotransport
-increase urine volume,broncho/vaso dilation,smooth muscle relaxation,uric acid,glucose,TG,
-decrease renal 02 consumption,CSF production,CA,K,Mg,Ca,Cl,HDL,acid
-GFR and RPF unchanged-save on renal
-Ototoxicity-cochlear>vestibular
-IV use for glaucoma/IOP, ICP, pulmonary edema, ARF
-Oral use- decrease BP, Cardiac and Renal insufficiency
Term
Bumetanide
Definition
-loop diuretic-high ceiling
-"semide" oral and IV
-secreted with PSOASS-->ascending loop of henle
-inhibition of NA/2CL/K cotransport
-increase urine volume,broncho/vaso dilation,smooth muscle relaxation,uric acid,glucose,TG,
-decrease renal 02 consumption,CSF production,CA,K,Mg,Ca,Cl,HDL,acid
-GFR and RPF unchanged-save on renal
-Ototoxicity-cochlear>vestibular
-IV use for glaucoma/IOP, ICP, pulmonary edema, ARF
-Oral use- decrease BP, Cardiac and Renal insufficiency
Term
diuretics
Definition
-loop, thiazide, potassium sparing, carboanhydrase inhibitors, xanthine derivitives
Term
chlorothiazide
Definition
-thiazide-low ceiling-oral only
-secreted with PSOASS-->Early distal tubule-inhibition of NA/Cl cotransport
-increase urine volume moderately-->less than loops
-decrease urine volume in diabetes insipidus
-decrease CA, GFR and RPF, K,Mg, Cl, HDL, acids
-increase Ca,uric acid, glucose, TGs
-oral use: decrease BP, cardiac insufficiency(relaxes smooth muscle), diabetes insipidus, urinary calculi(keeps Ca+ out of kidney)
-combine with K sparing
Term
chlorthalidone
Definition
-chemically different from thiazides, but with exact same clinical use
Term
indapamide
Definition
-chemically different from thiazides, but with exact same clinical use
Term
Spironolactone
Definition
-potassium sparing
-aldosterone antagonist-->steroid side effects
-spironolactone-->canrenone (both stop aldosterone binding to cyto receptor
-no aldosterone effects
-decrease Na and increase K
-oral only- 1/2 life 2 hours
Term
canrenone
Definition
-potassium sparing
-aldosterone antagonist-->steroid side effects
-spironolactone-->canrenone (both stop aldosterone binding to cyto receptor
-no aldosterone effects
-decrease Na and increase K
-IV only- 1/2 life 17 hours
Term
Triamterene
Definition
-potassium sparing-cycloamidine derivitive
-Na channel blocker and Na/H exchange blocker (alkoline urine)
-organic base- organice base cation exchange decretory system
-short half life (4-6 hours) because increased metabolism
-folic acid antagonism
-collecting duct
Term
K+ toxicity
Definition
-do no combine any K+ increasing agents
-ACE, Potassium sparing, or K+ supplements
Term
Amiloride
Definition
-potassium sparing-cycloamidine derivitive
-Na channel blocker and Na/H exchange blocker (alkoline urine)
-organic base- organice base cation exchange decretory system
-long half life (18-20 hours)
-collecting duct
-increase Ca+
Term
Acetazolamide
Definition
-carbo-anhydrase inhibitor
-sulfonamide group-->CA inhibitor
-PSOASS-->early proximal tubule
-prevention of mountain sickness-->induces acidosis in blood to keep breathing reflux
-secondary increase in urine volume/pH and K
-decrease glaucoma and IOP and nephron blockade
Term
Theophylline
Definition
-xanthine derivitive
-Adenosine-1-receptor blocker-->vasodilation
--caffeine derivatives
-adenosine-1 receptor blocker
-high doses lead to unselective PDE inhibition
-decrease PDE, increase cAMP-->smooth muscle relaxtion
-seizure risk with high doses because of release of catacholomines
-1A2 metablism-induced by smoke and protien
-high doses-->switch to zero order-->tachycardia, N&V, tremor, rhabdomyolysis
Term
captopril
Definition
-ace inhibitor
-only active drug (with lisinopril)
-short half life (2 hours)
-persistent dry cough, angioedema, hypotension, hyperkalemia, taste disturbance, fever, rash
-only sulfur containing -pril-->rashes and taste disturbance
Term
lisinopril
Definition
-ace inhibitor
-only active drug (with captopril)
-half life 12 hours
-persistent dry cough, angioedema, hypotension, hyperkalemia, taste disturbance, fever, rash
Term
enalaprilat
Definition
-only ace inhibitor given IV-->ER
-captopril without sulfur group
-persistent dry cough, angioedema, hypotension, hyperkalemia, taste disturbance, fever, rash
Term
fosinopril
Definition
-Ace inhibitor
-only one to be eliminated through liver (both kidney and liver)-->because of phosphate group
-persistent dry cough, angioedema, hypotension, hyperkalemia, taste disturbance, fever, rash
Term
Candesartan
Definition
-ARB-block AT1 receptor
-only prodrug (with olmesartan)
-all distributed orally
-persistent dry cough, angioedema, hypotension, hyperkalemia, taste disturbance, fever, rash
-only one predominantly eliminated through kidney (rest through liver)
Term
Olmesartan
Definition
-ARB-block AT1 receptor
-only prodrug (except candesartan)
-all oral
-persistent dry cough, angioedema, hypotension, hyperkalemia, taste disturbance, fever, rash
Term
rampril
Definition
--Ace inhibitor
-protects heart and against neuropath in diabetes patients and also reduces new cases of diabetes
-persistent dry cough, angioedema, hypotension, hyperkalemia, taste disturbance, fever, rash
Term
Aliskiren
Definition
-direct renin inhibitor
-hypertension medication
-high water solubility
-prevents conversion of angiotensin to angiotensin 1
Term
bradykinin
Definition
-broken down by ACE
-increased by ACE I
-increases NO and vasodilation
Term
xanthines
Definition
-caffeine derivatives
-adenosine-1 receptor blocker
-high doses lead to unselective PDE inhibition
Term
aminophylline
Definition
-xanthine derivitive
-Adenosine-1-receptor blocker-->vasodilation
--caffeine derivatives
-adenosine-1 receptor blocker
-high doses lead to unselective PDE inhibition
-decrease PDE, increase cAMP-->smooth muscle relaxtion
-seizure risk with high doses because of release of catacholomines
-1A2 metablism-induced by smoke and protien
-high doses-->switch to zero order-->tachycardia, N&V, tremor, rhabdomyolysis
Term
amrinone
Definition
-PDE III-inodilation
-increase stroke volume and CO-no increase in O2 consumption or BP
-smooth muscle relaxant
Term
enoximone
Definition
-PDE III-inodilation
-increase stroke volume and CO-no increase in O2 consumption or BP
Term
cilomilast
Definition
-PDE IV inhibitor
-used for COPD-->increases cAMP and reduces inflammatory cells
Term
sildenifil
Definition
-PDE V
-vasodilation-->ED
-can cause visual impairment
-3A4
-heartburn, headache, nasal congestion, flushing
-contraindicated with heart problems-->too much vasodliation-->decrease BP-->can't get blood to brain-->pass out
-don't use with nitrates
-also marketed under different trade name for pulmonary hypertension
Term
vardenafil
Definition
-PDE V
-vasodilation-->ED
-can cause visual impairment
-3A4
-heartburn, headache, nasal congestion, flushing
-contraindicated with heart problems-->too much vasodliation-->decrease BP-->can't get blood to brain-->pass out
-don't use with nitrates
Term
tadalafil
Definition
-PDE V
-vasodilation-->ED
-no visual impairment, PDE 11-no problems
-3A4
-prodrug with long half life
-heartburn, headache, nasal congestion, flushing
-contraindicated with heart problems-->too much vasodliation-->decrease BP-->can't get blood to brain-->pass out
-don't use with nitrates
Term
type 1 statins
Definition
-natural statins
-lovasatin, simvastatin, pravastatin
Term
type II statins
Definition
-synthetic
-atorvastatin, fluvastatin, rosuvastatin
Term
OAT/diffusion statins
Definition
-OAT-Rosuvastatin,pravastatin
-Diffusion-Lovastatin, Simvastatin, fluvastatin, atorvastatin
Term
statin
Definition
-decrease intracellular cholesterol-->activates genes for LDL receptor-->reduces extracellular chol.
-greatly reduces LDL-C, moderately reduces TGs (fibrates), slightly increases HDL-C (niacin)
-Atorvastatin and rosuvastatin-most potent
-plietropic effects-decrease protient prenylation-->decrease cancer, cardiovascular disorders, osteoporosis, multiple sclerosis, alzheimers
-decrease melvalonic acid-->which inhibits NO production less
-decreases arterial thickening and re-stenosis
-decrease CRP-->less aggregation and decreased risk of MI
-increase plaque stability-increased collagen production and decreased matrix protease and monocyte endothelial adherence
-decrease plasminogen activator inhibitor 1-->allows plasminogen-->plasmin-->fibrin degradation
-decreases osteoclast formation (~bisphosphonates)
-absorbed in GIT with high FPE
-most fecal elimination
-can lead to myotoxicity (increase with lipophilic and with fibrates) and hepatotoxicity
-category X
-all are single isomers with low bioavailability
Term
solubility of statins
Definition
-lipophilic-simvastatin, lovastatin,fluvastatin, atorvastatin
-hydrophilic-provastatin, -->more hepatic selective
Term
Pro/active statins
Definition
-prodrug-lovastatin, simvastatin
-active-fluvostatin, pravastatin, atorvastatin, rosuvastatin
Term
provastatin
Definition
-only one with no cyp450 metabolism
-only 50% protien binding (the rest ~100)
-
Term
half life of statins
Definition
-atorvastatin-14 hours
-rosuvastatin-20 hours
-all others around 1-3-->give in evening when most cholesterol is synthesized
Term
nitroglycerin
Definition
-converts to NO with cysteine-->vasodilation
-trinitrate-shortest half-life
-no FPE
-nitrate tolerance-->depletion of sulfhydryl group needed for nitrates to vasodilate
-do not mix with PDE V inhibitors or alpha-1 blockers
Term
amyl nitrate
Definition
-dinitrate-medium half-life
-used for angina and cyanide poisening-->sequesters cyanide as cyanomethemoglobin
-also used as "popper"
-do not mix with PDE V inhibitors or alpha-1 blockers
Term
isosorbide mononitrate
Definition
-mononitrate-longest half life (5 hours)
-dinitrate- medium (1 hour)
--do not mix with PDE V inhibitors or alpha-1 blockers
Term
nicorandil
Definition
-NO donor and K channel opener
-hyperpolarize-->smooth muscle relaxant
-mouth ulceration
-palpitation, weakness, N&V, headache, flushing
--do not mix with PDE V inhibitors or alpha-1 blockers
Term
Tacrine
Definition
-first drug approved for alzheimers
-non-specific cholinesterase inhibitor
(AChE and BChe)
-SE-N&V and liver damage (increases LFTs)
Term
Donepezil
Definition
-ChEI with greater specificity for AChE in the CNS (not BChE in perphery)
-NO liver damage
-1/2 life-70 hours-->once a day
Term
Rivastigmine
Definition
-AChE and BChE inhibitor
-patch
Term
Curare
Definition
-natural
-synthesized to intocostrin
Term
tubocurarine
Definition
-blocks ACh receptor sites at nueromuscular junctions
Term
NDMR
Definition
non-depolarizing muscle relaxants
-used by surgeons to keep muscles loose
-block muscarinic receptors-->nerves don't interact with muscles
-no CNS involvment
Term
aminosteroid
Definition
-muscarinic blocking effect
-NDMR
Term
edrophonium
Definition
-reversibly binds AChE-->increasing ACh-->out competes muscle relaxant after surgery
-no CNS penetration
-terminates action in 10 minutes
-fewer muscarinic effects than neostigmine
-low potency
Term
neostigmine
Definition
-reversibly binds AChE-->increasing ACh-->out competes muscle relaxant after surgery
-no CNS penetration
-terminates action in 10 minutes
-more muscarinic effects than edrophonium
-higher potency
-lasts 20-30 minutes
-excreted in the urine
Term
pyridostigmine
Definition
-AChE I used for Myaethania Gravis
-No CNS penetration, more potent, long acting
-pre-treatment for nerve gas (organo phosphate) exposure-->weaker AChE I
Term
methotrexate
Definition
-anti-cancer drug
-blocks conversion of folic acid-->THF
by blocking dihydrofolic reductase
-given in low dose with folate will inhibit T-cell activation and be used as an immunosupressent w/ myaesthenia
-excretion can be competitive with beta-lactam (penicillin like antibiotics)-->cause toxicity
-
Term
cyclosporin A
Definition
-calcineurin inhibitor (which is reponsible for IL-2)
-immunosupressent that can be used for myaesthenia
Term
treatment for OP
Definition
A-atropine
FL-fluid
O-oxygen
P- pyrodoxine-reactivates cholinesterase
or
pyrodostigmine-pre-exposure-weaker AChE I
Term
physostigmine
Definition
-only AChE I that penetrates the brain
-used for treatment of anticholinergic syndrome
-"Niagerian trial"
Term
tropicamide
Definition
-short acting cholinergic antagonist
-short acting mydriatic
Term
phenylephrine
Definition
alpha-andrenergic agonist
-short acting mydriatic
Term
atropine
Definition
-muscarinic blocker (PS)
-mydriatic
-resuscitation (jump start heart~epi)
-decrease secretions and bronchoconstriction
-antidote for OP
-central anticholinergic syndrome
Term
glycopyrrolate
Definition
-weak atropine that can't enter brain
-no CAS
Term
tiotropium
Definition
"tropium"
-only long acting inhalitive antimuscarinic
-used for asthma/COPD
Term
Darifenacin
Definition
-stops urinary incontinence (leakage)
-M3 receptor blocker-->stops smooth muscle bladder contraction
Term
oxibutinin
Definition
-M1 and M3 blocker
-less selective darifenicin
-may cause dry mouth
Term
tolterodine
Definition
-non-selective muscarinic blocker used for urinary incontinence
Term
benzotropin
Definition
-atropine derivitive
-muscarinic blocker-->decreases ACh and restores ACh/dopamine imbalance in Parkinson's disease
Term
diphenhydramine
Definition
-antihistamine with strong anticholinergic effect
Term
orphenadrine
Definition
-anticholinergic, NMDA receptor antagonist, and antihistamine
-diphenhydramine derivitive
-2/3 atropine
Term
biperider
Definition
-tertiary amine
-anticholinergic-->restors AcH/Dopamine balance and stops parkinson-like symptoms
Term
trihexyphenidyl
Definition
-tertiary amine
-anticholinergic-->restors AcH/Dopamine balance and stops parkinson-like symptoms
Term
musimol
Definition
-GABA agonist
Term
pilocarpine
Definition
-nonselective muscarinic agonist
-decreases IOP and gluacoma
Term
cevimeline
Definition
-M3 agonist
-increases saliva production (~clozapine)
-used for dry mouth
Term
phentolamine
Definition
-nonselective alpha receptor blocker
-vasodilation-->decrease BP in hypertensive emergencies
-used for emergency phaeochromocytoma or cocaine induces hypertension
Term
tamsulosin
Definition
-"osin"- alpha 1 A blockers (specific for prostate)
-uroselective blocker
-"flomax"-increases flow
-1:40 beta:alpha
Term
doxasosin
Definition
"osin"-alpha 1 blocker
-non uroselective (prostate and peripheral)
-side effect->hypotension
Term
terazosin
Definition
"osin"-alpha 1 blocker
-non uroselective (prostate and peripheral)
-side effect->hypotension
Term
alfuzosin
Definition
"osin"-alpha 1 blocker
-functionally uroselective
Term
silodosin
Definition
"osin" alpha 1 blocker -ueoselective -->alpha 1 a -no orthostatic hypotension -inhibit ejeculation, not orgasm
Term
clonidine
Definition
-central alpha 2 and imidazoline agonist--> negative feedback on presynaptic terminal-->decrease NT release
-turn off sympathetic activity
-imidazoline-decrease BP and reduce anxiety
SE:bradykardia, constipation, water retention
- alpha 1-analgesia, sedation
SE: dry mouth, parotid pain
-"nidine"
Term
alphamethyldopa
Definition
-alpha 2 agonist (not imidazol)
-pregnancy category B-> safe way to lower BP during pregnancy
Term
dexmedetomidine
Definition
-sedative anciolytic without respiratory depression
-clonidine like drug (only alpha 2)
Term
moxonidine
Definition
-clonidine like-selective for imidazol->specific for decreasing BP
Term
oxymetazoline
Definition
-alpha 1 agonist->nasal vasocontriction for decongestion
-use too much, go to system-> increase BP
"zoline"
-can lead to nasal necrosis
Term
xylometazoline
Definition
-alpha 1 agonist->nasal vasocontriction for decongestion
-use too much, go to system-> increase BP
"zoline"
-can lead to nasal necrosis
Term
phenylephrine
Definition
-alpha 1 agonist->nasal vasocontriction for decongestion
-use too much, go to system-> increase BP
"zoline"
-can lead to nasal necrosis
Term
albuterol
Definition
-beta 2/beta 1 agonist-4/1
"terol"-beta 2 agonist
-also called salbutamol
-secreted in urin
-racemic with eutomer and distomer
-ROSA reliever asthma inhalent
Term
salbutamol
Definition
-beta 2/beta 1 agonist-4/1
"terol"-beta 2 agonist
-also called albuterol
-secreted in urin
-racemic with eutomer and distomer
-ROSA reliever asthma inhalent
Term
levalbuterol
Definition
-beta 2/beta 1 agonist-4/1
"terol"-beta 2 agonist
-ROSA reliever asthma inhalent
-concentrated eutomer of albuterol
Term
salmeterol
Definition
-beta 2 agonist
-true SOLA controller for asthma
Term
formoterol
Definition
-beta 2 agonist
-only ROLA-->can be a controller or reliever in asthma
Term
salmeterol
Definition
-beta 2 agonist
-true SOLA controller for asthma
Term
formoterol
Definition
-beta 2 agonist
-only ROLA-->can be a controller or reliever in asthma
Term
dobutamine
Definition
-psuedo beta 1 agonist
-beta 1>>beta 2 agonism
-racemic mixture- cancels out alpha effects
-increase HR and + ionotropic
-support failing heart
Term
dopamine
Definition
small dose- D1 agonist-in periphery acts on kidney and GI to increase profusion
"renal dose"-->protects kidneys
-medium dose-beta 1 agonist-increase HR and + ionotropic
-high dose- alpha 1 agonist-vasoconstriction and increase BP
Term
isoprenaline
Definition
-synthetic catecholamine
-increase cAMP through beta 1 and beta 2
-increase HR and contraction while vasodilating
-same as PDE III inhibitor-->inodilator
Term
propranolol
Definition
-non selective, no ISA beta blocker
-fat soluble-dreams and hepatic metab.
-Na CB
Term
nadolol
Definition
not selective, no ISA beta blocker
-water soluble
Term
pindolol
Definition
-not selectrive with ISA beta blocker
-water soluble-kindeys
-Na CB
-partial 5-HT-1a agonist
Term
metoprolol
Definition
selective, no ISA beta blocker
-fat soluble-dreams and hepatic metab
Term
atenolol
Definition
selective, no ISA beta blocker
-water soluble-kidney
Term
acebutolol
Definition
selective with ISA
-fat soluble-dreams
-renal elimination
-Na CB
Term
esmolol
Definition
-beta blocker used by anaesthetists because of ultra-short half life
-ester compound=ultra short half life
Term
carvedilol
Definition
mixed-non cardio specific alpha and beta blocker (1:3)
Term
labetalol
Definition
mixed-non cardio specific alpha and beta blocker (1:3)
Term
nebivolol
Definition
-cardioselective Beta 1 blocker with vasodilation by NO
Term
glucagon
Definition
-beta blocker overdose
-increases cAMP without beta receptor
Term
ether
Definition
-first inhaled anesthetic for surgery
Term
halothane
Definition
-inhaled anesthetic with lowest MAC,highest potency and lipid solubility
-first introduces, rarely used in western world
-can trigger malignant hyperthermia (release of Ca)
-20% metabolized (most)-->hepatitis
-slow onset/offset
Term
enflurane
Definition
-inhaled anesthetic
-2% metabolized
-increased risk of seizures
Term
isoflurane
Definition
-inhaled anesthetic
-.2% metabolized
Term
sevoflurane
Definition
-inhaled anesthetic
-4 % metabolized
-kidney damage
Term
desflurane
Definition
-highest MAC of inhaled anesthetics, lowest fat solubility and potency
-.004% metabolized
-rapid onset/offset
Term
nitrous oxide
Definition
-laughing gas-NMDA antagonist(not GABA agonist) inhaled anesthetic
-highest MAC, lease fat soluble and potent
-cannot use alone for proper anesthesia
-sympatho-mimetic (like ketamine)
-inhibits B12 dependent enzymes-myelin production (paralysis) and RBC production (megoblastic anemia)
Term
pipecuronium
Definition
-"cronium"-aminosteroid NDMR
-less vasolytic->increases HR
-longest length (90-120 min)
-renal/hepatic elimination
Term
pancuronium
Definition
"curonium"aminosteroid NDMR
-very vagolytic-->increase HR-->don't give to patients with CAD
-second longest lasting (60-90)
Term
vecuronium
Definition
"curonium" aminosteroid NDMR
-hepatic/renal/bile elimination
-intermediate acting (30-40min)
Term
rocuronium
Definition
-"curonium"-aminosteroid NDMR
-not metabolized-->renal/bile elimination
-intermediate acting (30-40min)
Term
Mivacurium
Definition
-"curium" isoquinoline NDMR
-histamine release->bronchoconstriction and tachycardia
-ester-shortest acting (5-15 min)
Term
-atracurium
Definition
-"curium" isoquinoline NDMR
-histamine release->bronchoconstriction and tachycardia
-mixture of 10 isomers
-partially degraded by Hofmann
-rest by plasma esterases-->laudanosine (increases CNS and causes seizures)
-intermediate duration (20 min)
Term
cisatracurium
Definition
-"curium" isoquinoline NDMR -histamine release->bronchoconstriction and tachycardia -cleaner atracurium-->only active isomers -Hoffman with laudanosine (increased CNS and seizures) -intermediate (30min)
Term
doxacurium
Definition
-"curium" isoquinoline NDMR
-histamine release->bronchoconstriction and tachycardia
-not metabolized-renal
-long duration (120 min)
Term
succinylcholine
Definition
-di-acetyl-choline
-depolarizing muscle relaxant
-only 1-10% reaches target (unless atypical)
-ultra-short 1/2 life (3 minutes)
-very rapid onset (60 seconds)
-train four response-fade
-fasiculations, myalgia (young women), increased pressure (ICP, IOP, intragastric)-->don't give with head trauma, glaucoma, eye injury
-bradycardia, bronchospasm
-hyperkalemia (higher ith muscle disease or burns)
-masseter muscle spasm and malignant hypertherm
Term
dibucaine
Definition
-test to determine the amount of ChE in plasma
-should get broken down 80%, if less-->less ChE present
Term
heparin
Definition
-large polysaccharide, water soluble, not protein bound-->short 1/2 life (fast acting)
-safe for pregnancy
-parenterally-->in plasma
-catalyzes antithrombin III to inactivate 2,9,10,11,12 (intrinsic), also inhibits FII (thrombin)
-measured with partial thromboplastin time (PTT)
-can cause HIT(heparin induced thrombocytopenia)-long term-->autoimmune against platelets-->bleed more and clot
-osteoporosis
-antagonist-protamine (a vasodilator or anticoag)
-LMW-clean-only AT III activator-increased 1/2 life, expensive with no reliable antagonist
Term
warfarin
Definition
-small, lipid soluble-->goes to liver, protein bound-->long half life (displaced by fibrates)
-oral
-binds to vit. K epoxide reductase-->stops production of vit. K dependent factors-2,7, 9, 10, s, c (extrinsic)
-don't take if pregnant
-measured with Prothrombin time (PT), or INR- INR increases with efficacy (decrease in Vit. K)
-VKORC1 and CYP2C9 polymorphism
-antagonize with Vit. K (long term) or Frozen Fresh Plasma
-can lead to skin necrosis (avoid if heparin bridge)
-ADR-osteoporosis, purple toe (necrosis)
Term
Hirudin
Definition
-direct thrombin inhibitor (from leech)
-"rudin"
-reversal of HIT
Term
Lepirudin
Definition
-"rudin"-direct thrombin inhibitor
-IV-->reversal of HIT from heparin
Term
argatroban
Definition
-direct thrombin inhibitor and anticoagulant
-IV-->reversal of HIT from heparin
-can be used in replace of heparin as an anticoagulant
Term
melagatran
Definition
-"gatran"- oral
-direct thrombin inhibitor
Term
platlet aggregation
Definition
(+) 5-HT, adrenalin, ADP, TXA2, PAF, Thrombin
(-) adenosine, NO/EDRF, PGI2, cAMP, cGMP
Term
ASA
Definition
-low dose-inhibits platelet aggregation
-inhibits COX on platelets->inhibits TXA2 (which causes platelet aggregation)
Term
Ticlopidine
Definition
-decreases platelet aggregation
-ADP-inhibitor- stops the activation of P2Y12->which then cannot activate IIbIIIa
-used when ASA cannot be used, but is not being used in place of
-ester, only 15% makes it to liver
Term
clopidogrel
Definition
-decreases platelet aggregation "grel"
-ADP-inhibitor- stops the activation of P2Y12->which then cannot activate IIbIIIa
-used when ASA cannot be used, but is not being used in place of
-pro-drug
-ester, only 15% makes it to liver
Term
prasugrel
Definition
-decreases platelet aggregation "grel"
-ADP-inhibitor- stops the activation of P2Y12->which then cannot activate IIbIIIa
-used when ASA cannot be used, but is not being used in place of
-pro-drug
-ester, only 15% makes it to liver
Term
Abciximab
Definition
-direct GP-IIb/IIIA inhibitor
Term
tirofiban
Definition
-direct GP-IIb/IIIA inhibitor
Term
eptifbatide
Definition
-direct GP-IIb/IIIA inhibitor
Term
dipyridamole
Definition
-adenosine-re-uptake inhibitor
-increase adenosine-->decreases platelet aggregation
-also reduces heart rate
-PDE I do the same thing (cAMP and cGMP decrease aggregation)
Term
alteplase
Definition
-thrombolytic->catalyze formation of plasmin
-tissue plasminogen activator (tPA)
-use post surgery, MI, Stroke, etc.
-binds to clot itself, more specific
-cost more
-also increases platelet aggregation by increasing thrombin levels (must counter with ASA)
Term
streptokinase
Definition
-thrombolytic
-catalyzes formation of plasmin
-binds to plasminogen (not clot)-less specific, can cause increased bleeding
-can form antibodies against
-use post surgery, MI, Stroke, etc.
-also increases platelet aggregation by increasing thrombin levels (must counter with ASA)
Term
Rifamycin
Definition
-TB
-stops bacteria RNA polymerase
-potent inducer of metabolism
-red child syndrome-orange skin and secretions and contact lenses
Term
rifabutin
Definition
-TB
-stops bacteria RNA polymerase
-potent inducer of metabolism
-red child syndrome-orange skin and secretions and contact lenses
-less drug interaction-used in HAART for HIV treatment
Term
rifapentine
Definition
-TB
-stops bacteria RNA polymerase
-potent inducer of metabolism
-red child syndrome-orange skin and secretions and contact lenses
-longer half life
Term
ethambutol
Definition
-TB
-inhibits arabinosyl-->bacterial cell wall synthesis
-OPTIC NEURITIS, red/green discrimination, decrease uric acid-->goute
-neuropathy, nystagmus
Term
isoniazid
Definition
-TB
-prodrug-->INA-->gets incorporated into NAD-->decreases mycolic acid synthesis-->cell death
-uses acetyl transferase-->sight for polymorphism in people
-NAT-2 gene-further north, better acetylators-->less toxicity
-can be measured with xanthine metab.
-inactivates pyridoxal (B6)-peripheral neuropathy
-stops conversion of glutamate->GABA- CNS stimulant-BDZ resistant siezures
-stops conversion of lactic acid to pyruvate-->lactic aciduria
-decreases conversion from tryptophan->niacin (vit. B3)-pellegra (dermatitis, diarrhea, dementia, death)
-hepatotoxicity->lupas-like symptoms
Term
dapsone
Definition
-diamino diphenyl sulfone (DDS)
-rafampin and clofazamine
-used for leprocy
Term
sulfonamides
Definition
-blocks the conversion of PABA to folate
-dihydropteroate synthetase
-hemolysis w/ glucose6P dehydrase deficiency (also caused by fava beans)
-
Term
clofazamine
Definition
-inhibits DNA replication
-anti-inflammatory-->given for leprosy
rxn erythema nodosum leprosum-->hypersensitivity rxn
Term
methotrexate
Definition
-stops the conversion of dihydrofolate to tetrahydrofolate-->inhibits diyhydrofolate reductase
-slows DNA and RNA synthesis-->anti-cancer (trimethoprim and pyrimethaprim)
-immunosuppressent because it stops t-cell activation (used for AI-rheumatoid arthitis, crohns, psoriasis)
-supplement with folate
-renal comp. and toxicity with B-lactams
-
Term
beta-lactams
Definition
-cause toxicity of methyltraxate
-penicillin, cephalosporin, carbapenems, monolactam
Term
cyclosporin
Definition
-binds to cyclophilin and inhibit calcineurin-->decreases IL-2
-immunosuppresent-used for rhematoids
-can cause neprhotoxity, increased malignancy, 3A4 substrate (induced by BCGPRS)-inhibited by grapefruit
Term
sirolimus
Definition
=rapamycin
-"limus"-immunosupressent
Term
tacrolimus
Definition
-tsukuba macolide immunosupressent
-similar to cyclopsporin (calcineurin-IL2)
Term
pimecrolimus
Definition
-tsukuba macolide immunosupressent
-similar to cyclopsporin (calcineurin-IL2)
Term
azothioprine
Definition
-inhibits purine synthesis->slows DNA synthesis (B and T cells)
-pro-drug-->6-merpcaptopurine
-bone marrow toxicity
-teratogenic
-metabolized by TPMT-polymorphisms
(also metabolizes 6-thioguanine)
TPMT deficient-->leads to hematotoxicity
Term
mycophenolate
Definition
-inhibits purine synthesis-->DNA synthesis-->T and B cells
-delayed onset of action (6-12 months)
-no side effects
-expensive
Term
colchicine
Definition
-inhibits microtubule polymerzation, decreases mitosis
-affects axonomal transport
-stops luekocytes from getting to inflamed area-->stops acute flare from gout arthritis (big toe)
Term
probenecid uricosuric
Definition
-interferes with excretion and increases the elimination of uric acid
-used for gout
Term
xanthine oxidase inhibitor
Definition
-stops the synthesis of uric acid
-used for gout
Term
5-fluorouracil
Definition
-used in the treatment of solid tumors
-polymorphism-->dihydro-pyrimidine-dehydrogenase (DPD)-rate limiting step in catabolism-->toxicity if absent
-toxicity-myolsupression, mouth ulcers, skin changes, neuro tox, diarrhea
Term
capecitabine
Definition
-used in the treatment of solid tumors
-polymorphism-->dihydro-pyrimidine-dehydrogenase (DPD)-rate limiting step in catabolism
-toxicity-myolsupression, mouth ulcers, skin changes, neuro tox, diarrhea
Term
minocycline
Definition
-5 lipoxidase (LO)inhibitor-decreases leukotrienes
-broad spectrum antibiotic
Term
auronofin
Definition
-decreases macrophage activation
-gold
Term
tnf-alpha inhibitor/IL-1 antagonist
-cept, ximab, zumab, mumab, ra
Definition
-cept-receptor Ab fusion protein
-ximab-chimeric monoclonal Ab
-zumab-humanized monoclonal Ab
-mumab-human monoclonal Ab
-ra-receptor agonist
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