Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
131 Cards in this Set
- Front
- Back
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. |