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131 Cards in this Set

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Norepinephrine
Catecholamine
Activates alpha > beta,
beta2 least
No CNS activity
increases BP but constricts kidney vessles
Epinephrine (adrenaline)
Catecholamine
Drug of choice for acute hypersensitivity reactions (anaphylactic shock)
Used in heart block and cardiac arrest (emergency use)
Used as a basoconstrictor in local anesthetic preparations
Dopamine
Catecholamine
Shock, maintains renal blood flow
Isoproterenol (isoprenaline)
Catecholamine
synthetic, activates all beta R
albuterol, salmeterol, terbutaline
selective B2 agonist
Asthma--dilates bronchioles
can cause tremors
Ritodrine
selective B2 agonist
premature labor--relaxes uterine m.
can cause tremors
Dobutamine
selective B1 agonist
Cardiac stimulant
used in cardiogenic shock, acut congestive heart failure
Phenylephrine, Oxymetazoline, Pseudoephedrine
selective a1 agonists
nasal decongestants
Pressor agents for tx of hypotension
Adverse effects: cardiovascular (hypertension, reflex bradycardia) & CNS stimulation & urinary retention
Clonidine, a-methyldopa
Selective a2 agonists
Tx of htn
AE: sedation and weakness, rebound htn upon withdrawl
tizanidine
Selective a2 agonist
tx of spasticity assoc w/ neuropathy
apraclonidine and brominidine
Selective a2 agonist
tx glaucoma, HTN
amphetamine, methamphetamine
IDA: release NE
CNS stimulant, incr. alerness, mood, depression of appetite
Tx: Narcolepsy
AE: cardiovascular (htn, tachy), tremor and convulsions, dependence and psychosis
ephedrine
mixed action (direct and indirect)
like amphetamines, but milder
Tyramine
IDA: release NE
found in food (beer, wine, cheese, fermented sausage)
can cause HTN crisis
IDA: release of NE plus taking an MAOI can cause?
Hypertensive crisis
Cocaine
IDA sympathomimetic: inhibition of NE reuptake
sympathetic effects
Tricyclic antidepressants
IDA Sympathomimetic: inhibition of NE reuptake
sympathetic effects
Phenelzine
IDA sympathomimetic:
MAOI
antidepressant
Selegiline
IDA sympathomimetic:
MAOI
increases DA in brain--Parkinson's
Horner's Syndrome in R eye, apply amphetamine eye drops, what happens?
apply phenylephrine drops, what happens?
amphetamine-R eye will do nothing, L eye will dilate.
phenylephrine--R eye will dilate very large (supersensitivity) and L eye will dilate
Prazocin
competative, selective for a1 R, a1 adrenergic antagonist
tx: chronic HTN
postural hypotension
tachy, impaired sexual fxn, nasal stuffiness
Tamsulosin
a1 adrenergic antagonist
Tx: benign prostatic hypertrophy
Labetalol, carvedilol
competative, a1 and B receptor blockers
Atenolol
B1-selective receptor blocker
no CNS activity, 1/2 life: 6-9 hrs
Tx: HTN
metoprolol
B1 selective R blocker
Tx: HTN
Pindolol
partial B1 agonist
Tx: HTN
Propranolol
Prototype, non-selective B1 and B2
Tx: HTN
B1 selective and non selective antagoinsts
Tx:first line for HTN (see gradual decrease in TPR in spite of long-term decrease in Q)
mechanism is unclear
decreases renein release
doesn't work as well in AA ppl
Metoprolol
B1 blocker
Tx: Arrhythmia
Atenolol
B1 blocker
Tx: Angina
with discontinued use get rebound angina
Pindolol
non-selective, partial agonist)
Tx: Angina w/o rebound angina
Beta antagonists "beta blockers"
Tx:Congestive Heart Failure,Angina, Arrhythmia, HTN, post MI, tremor, glaucoma, migraine prophylaxis, hyperthyroidism: block of cardiac manifestations
Propranolol
Tremor, performance anxiety, Hyperparathyroidism: block of cardiac manifestations
Timolol
Glaucoma: decreases aqueous humor formation
B blocker : adrenergic antagonist.
B blockers are bad for:
Heart failure
Asthma & Hypoglycemia (B1 selective preferred)
Reserpine
Inhibition of intraneuronal storage of CAs, inhibits transport of NE from cytosol to vesicle, leads to depletion of NE and seretonin stores
Bretylium
prevention of N transmitter release, local anesthetic action
List Antihypertensive Drugs
a2 agonists (clonidine, methyldopa)--inhibit NE release
Ganglionic blockers (mecamylamine)--block Ach signal to sympathetic ganglia
a1 blockers (prazocin)
ARBs (losartan)
Ca channel blockers (nifedipine, verapamil)
Vasodilators (minoxidil, nitroprusside)
ACE inhibitors (catopril, enalapril)
Diuretics (hydrochlorothiazide, furosemide)
B blockers (propranolol, metoprolol)
NMJ is______ and is not ______
NMJ:
IS part of the cholinergic NS but is
NOT part of the ANS.
hemicholinium
inhibits Ach formation by blocking choline and Na transport
vesamicol
inhibits Ach formation by inhibiting its storage in vessicles
ChAT
choline acetyltransferase synthesizes ACh from choline and acetyl CoA
botulism toxin and bungarotoxin (snake venom)
BT:inhibit ACh release
Bungaro: blocks post-synaptic ACh Receptor
black widow spider venom
increases ACh release
Bethanechol
Direct Acting Cholinomimetic at M receptor
Choline ester: quaternary
sm m of GIT and bladder
Muscarine
Direct acting Cholinnomimetic at M receptor
Alkaloid (N)
in mushroom amanita, competative antagonist
Pilocarpine
Direct acting Cholinnomimetic at M receptor
Alkaloid (N)--tertiary
tx: glaucoma, xerostomia
Physostigmine
Anticholinesterase, indirect acting
Reversible
Tertiary
CNS activity
Neostigmine
Anticholinesterase, indirect acting
Reversible
Quaternary amine
Little CNS activity
increases muscle strength in myasthenia gravis
Rivastigmine, Donepezil, Tacrine
Anticholinesterase, indirect acting
Reversible
Centrally acting
Tx: Alzheimers, incr ACh in CNS
Echothiophate
Irreversible Anticholinesterases
Organophosphate
long acting miotic
Malathion
Irreversible Anticholinesterases
Organophosphate insecticide
absorbed through skin
SLUDE, bronchoconstriction, bronchosecretions, bradycardia, decreased Q
Sarin gas
nerve gas
Irreversible Anticholinesterases
Organophosphate
pralidoxime
oxime: cholinesterase reactivation if aging hasn't occurred w/i 30-60 mins.
but give atropine first
poisoning by anticholinergic, antimuscarinics
atropine; also for antimuscarinic effects of TCAs. Physostigmine preferred b/c it enters CNS
Acturium, Pancuronium, Vecuronium, Mivacurium
Cholinergic Nicotinic NMJ Non-Deporarizing/Competative Blockers--> flaccid paralysis
how do you reverse non depolarizing blockers?
atropine then anticholinesterase (neostigmine)
Succinylcholine
Nicotinic, Depolarizing (partial agonist) blocker--> initial stimulation (fasciculations) then paralysis --short acting
succinylcholine toxicity can be reversed by?
giving new plasma. it's broken down by pseudocholinesterase, so by boosting the levels of this you can increase its metab. neostigmine or organophosphates will make it worse!
Mecamylamine
nicotinic Ganglion blocker direct
for hypertensive crisis, tertiary, oral/injection, short term
How is non-depolarizing NMJ blockade reversed?
ex: Atracurium;
first--atropine
second--anticholinesterase (neostigmine)
Which drug may cause muscarinic effects?
d-tubocurare
succinylcholine
vecuronium
succinylcholine
activation of muscarinic R (cholinergic) what effects will this have?
SLUDE + bradycardia, bronchial secretions
(parasympathetic actions)
If you OD on cholinergic drug, which will you NOT see?
Myosis
Mydriasis
incontinence
impotency
mydriasis (photophobia) is an adverse effect of antimuscarinic drugs
antimuscarinic drugs are _____ of acetylcholine. They act selectively at _____ receptors
competative antagonists
muscarinic
small doses atropine
tertiary amine; antimuscarinic agent; decrease salivation, bronchial secretions, and sweating
scopolamine
tertiary amine; antimuscarinic; alkaloid; CNS depressant, drowsiness, amnesia, fatigue; anti-emetic
dicyclomine
tertiary amine; antimuscarinic; tx: bowel spasm
tropicamide
tertiary amine; antimuscarinic; topical to produce mydriasis (dilation) and cyclolegia (nearsightedness)
benztropine
trihexyphenidyl
tertiary amine; antimuscarinic; tx: Parkinsons
Ipratropium
quaternary nitrogen; antimuscarinic; tx: COPD
Trospium, tolterodine, oxybutynin
quaternary nitrogen; antimuscarinic; tx: urinary incontinence
larger doses atropine
tertiary amine; antimuscarinic agent; pupil dilates, accommodation is inhibited, increased HR, inhibit PNS of GIT and bladder
toxic dose of atropine
tertiary amine; antimuscarinic agent; restlessness, irritability, disorientation and hallucinations, depression, coma, medullary paralysis and death
Posioing with atropine
Red, hot, dry, blind, mad
dry mouth, blurred vision, photophobia, hot, dry, flushed skin, increased temp, tachycardia, urinary retention
Lomotil
tx diarrhea
Antimuscarinic in the Respiratory tract
emphysema induces bronchial dilatation
Ipratropium
Antimuscarinic in the GU tract
reduces urinary frequency or urgency
Trospium, tolteridine, oxybutynin
Antimuscarinic in the GI tract
dicyclomine; IBS, diverticulosis
Antimuscarinic for Ophthalmological
for mydriasis and cycloplegia
homatropine, tropicamide
antimuscarinic for CVS
atropine for bradycardia or for heart block
antimuscarinic for cholinergic poisoning
atropine; treats amanita muscaria and anticholinesterases (pesticides)
antimuscarinic for parkinson's
benztropine, trihexyphenidyl
Antimuscarinic for Anti-emetic
scopolamine to treat motion sickness
treat antimuscarinic toxicity with
physostigmine (tertiary anticholinesterase, reversible) or neostigmine (quaternary)
benzodiazepine for agitation
vincristine
blocks mitosis
Fractional cell kill hypothesis
kill a constant fraction of cell population, it's concentration dependent
log kill 1 = .9 fraction killed
log kill 2 = .99 fraction killed
log kill 9 = .999999999 fraction killed, 0.000000001 surviving
1cm mass
clincally detected, 10 to the 9 cells, 30 divisions
Alters drug transport
Multi-drug resistance phenotype with enhanced expression oth the membrane p-glycoprotein pump
Imatinib
Tyrosine Kinase Inhibitor
inhibits ABL-BCR fusion
CML
Gefitinib
Tyrosine Kinase Inhibitor
inhibits EDGF
non small cell lung cancer
rash
Sunitinib
Tyrosine Kinase Inhibitor
inhibits VEGF
renal cancer
Rituximab
Monoclonal Ab
CD20
B cell lymphoma
infusion rxn, B cell depletion, neutropenia
Alemtuzumab
Monoclonal Ab
CD52
T-cell lymphoma
infusion rxn, pancytopenia
Trastuzumab
Monoclonal Ab
Her2/neu--Erb-2
breast ca.
CARDIOMYOPATHY
Cetuximab
Monoclonal Ab
EGFR
colorectal cancer
infusion rxn
Bevacizumab
Monoclonal Ab
VEGF
colorectal cancer
HTN, CHF, pulmonary or GI hemorrhage
IL-2
cytokine:
produces lymphocytes cytolytic for tumor cells

renal cell carcinoma, metastatic melanoma
Colony stimulating factors
differentiating agents
at various stages in hematopoietic hierarchy.
use to replenish blood cells
Retinoic Acid
Differentiating Agent
influence epithelial cells
Tx: BPL, acute myelocytic leukemia
Antiangiogenesis agents do what?
reduce vascular supply to tumor. none are on market now
bortezomib
Proteasome inhibitors
inhibits 26S proteasome
Tx of: mult. myeloma
Radioimmunoconjugates
ex: Iodine-131 tositumomab
Proteosome inhibitors
bind to CD20 antigen on malignant B cells
used in non-Hodgkin's lymphoma
SE: thyroid toxicity, prolonged myelosuppression
Mechanisms of Antineoplastic Drugs
Cell specific (S and M) or non cell specific
--inhibition nucleic a or protein synthesis
--direct binding to NA
--interference w/ microtubule fxn
--inhibition of growth factor
Selectivity of antineoplastic drugs
differences btwn host and malignant cells; often differences aren't great
Mech of resistance of antinoplastic drugs
altered affinity for binding site
decreased activation or increased deactivation
altered transport
**most drugs increase in efflux via MDR pump**
Host toxicity -- generally to more rapidly dividing cells
myelosuppression
GI mucosal irritation
alopecia and inhibits fertility
Methotrexate
folate antimetabolite (S phase)not affected by MDR
inhibitor of dihydrofolate reductase
toxicity: myelosuppression GI mucositis
tx for: acute leukemias, choriocarcinoma
inhibition of purine, pyrimidine and AA synthesis
5-Fluorouracil
pyrimidine antimetabolite (S phase)not affected by MDR
inhibitor of thymidylate synthetase
tx: breast and GI tumors, skin lesions and warts
Cytosine Arabinose
pyrimidine antimetabolite (S phase)not affected by MDR
competes w/ dCTP for incorporation into DNA; inhibits DNA synthesis
tx: potent antileukemic
6-mercaptopurine and 6-thioguanine
purine antimetabolite (S phase)not affected by MDR
guanine and hypoxanthine analogs
--> to deoxyribonucleotide derivatives by HGPRT; incorporate into DNA
toxicity: PANCREATITIS
Hydroxyurea
analog of urea
inhib of ribonucleotide reductase inhibits DNA synthesis
Tx:acute and chronic leukemia; myeloproliferative disorders
toxicity: bone marrow and GI
Adriamycin (Doxorubicin);
Daunorubicin
Anthracycline (not cell specific and subject to MDR pump)
affect intercalation, formation of free radicals, inhibition of topoisomerase II
tx: doxorubicin--solid tumors and leukemia
daunorubicin--acute leukemia
toxicity: acute and chronic (CHF) cardiotoxicity
Mixoxantrone
like anthracycline, but decreased free radicals and reduces cardiotoxicity
VP-16 (etoposide);
VM-26 (teniposide)
Epipodophyllotoxins
plant derivatives
S and G2 cycles are most sensitive
inhibit topoisomerase II
tx:acute leukemia, lymphomas, small cell carcinoma or lung
tox: BM depression, GI
(topotecan, irinotecan)
camptothecins
inhibit topoisomerase I; induction of single strand DNA breaks then double strand breaks
S phase is best
NO MDR
too toxic for tx: but CPT-II for colon cancer
Vincristine
Microtubule inhibitor
Vinca alkaloid
Hodgkin's, acute lymphoblastic leukemia
toxicity: Neurotoxicity
Paclitaxel, docetaxel
yew tree
interacts w/ microtubules, prevents depolymerization
tx: solid tumors: ovarian, breast, lund ca.
MRD
toxicity: neurotoxicity, BM
Nitrogen mustards, nitrosoureas, cyclophosphamide
alkylating agent
not cell cycle specific most sensitive
no MDR
Alkylation of DNA
toxicity: bone marrow suppression, immunosuppression
procarbazine, hexamethylmelamine
require metabolic activation, Hodgkin's disease (procarbazine)
Ovarian
(hexa)
Streptozotocin
methylnitrosourea derivative
alkylates DNA, single strand breaks in DNA
toxicity: bone marrow depression and GI and nephrotoxicity
Dacarbazine
requires micorsomal activation
monofunctional alkylator
inhibits DNA and RNA protein synthesis
not cell cycle specific
toxicity: nausea
Mitomycin C
metabolic activation in absence of O2, bioreductive alkylator
x links DNA; single strand breaks
inhib DNA and RNA & protein synthesis
breast, GI, lung, head neck tumors
toxicity: delayed myelosupression
CIS (PLatinol)
Platinum compound
binds to DNA forming interstrand and intrastrand x link; interferes with DNA transcription and translocation
used:testicular, ovarian, bladder, head and neck
toxicity: nephrotoxicity most serious, nausea vomiting
Bleomycin
breaks DNA by free radical mech
use: squamous cell carcinoma; Hodgkins and non Hodgkins lymphoma
toxicity: pulmonary toxicity
Aspariginase
inhibition of protein synthesis
Tamoxifen
compete w/ N estrogens
prevent growth in estrogen dependent tumors
Anastrazole
Aromatase inhibitor
reduce synthesis of estrogen
flutamide
compete with N androgens for binding sites
tx: prostate ca.
Leuprolide
LHRH agonist
inhibit androgen release
prostate ca. -->flare
GnRH antagonist
for pt who need to avoid flare
prostate ca.