Pharmacology

Front 1

Norepinephrine

Back 1

Catecholamine
Activates alpha > beta,
beta2 least
No CNS activity
increases BP but constricts kidney vessles

Front 2

Epinephrine (adrenaline)

Back 2

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

Front 3

Dopamine

Back 3

Catecholamine
Shock, maintains renal blood flow

Front 4

Isoproterenol (isoprenaline)

Back 4

Catecholamine
synthetic, activates all beta R

Front 5

albuterol, salmeterol, terbutaline

Back 5

selective B2 agonist
Asthma--dilates bronchioles
can cause tremors

Front 6

Ritodrine

Back 6

selective B2 agonist
premature labor--relaxes uterine m.
can cause tremors

Front 7

Dobutamine

Back 7

selective B1 agonist
Cardiac stimulant
used in cardiogenic shock, acut congestive heart failure

Front 8

Phenylephrine, Oxymetazoline, Pseudoephedrine

Back 8

selective a1 agonists
nasal decongestants
Pressor agents for tx of hypotension
Adverse effects: cardiovascular (hypertension, reflex bradycardia) & CNS stimulation & urinary retention

Front 9

Clonidine, a-methyldopa

Back 9

Selective a2 agonists
Tx of htn
AE: sedation and weakness, rebound htn upon withdrawl

Front 10

tizanidine

Back 10

Selective a2 agonist
tx of spasticity assoc w/ neuropathy

Front 11

apraclonidine and brominidine

Back 11

Selective a2 agonist
tx glaucoma, HTN

Front 12

amphetamine, methamphetamine

Back 12

IDA: release NE
CNS stimulant, incr. alerness, mood, depression of appetite
Tx: Narcolepsy
AE: cardiovascular (htn, tachy), tremor and convulsions, dependence and psychosis

Front 13

ephedrine

Back 13

mixed action (direct and indirect)
like amphetamines, but milder

Front 14

Tyramine

Back 14

IDA: release NE
found in food (beer, wine, cheese, fermented sausage)
can cause HTN crisis

Front 15

IDA: release of NE plus taking an MAOI can cause?

Back 15

Hypertensive crisis

Front 16

Cocaine

Back 16

IDA sympathomimetic: inhibition of NE reuptake
sympathetic effects

Front 17

Tricyclic antidepressants

Back 17

IDA Sympathomimetic: inhibition of NE reuptake
sympathetic effects

Front 18

Phenelzine

Back 18

IDA sympathomimetic:
MAOI
antidepressant

Front 19

Selegiline

Back 19

IDA sympathomimetic:
MAOI
increases DA in brain--Parkinson's

Front 20

Horner's Syndrome in R eye, apply amphetamine eye drops, what happens?
apply phenylephrine drops, what happens?

Back 20

amphetamine-R eye will do nothing, L eye will dilate.
phenylephrine--R eye will dilate very large (supersensitivity) and L eye will dilate

Front 21

Prazocin

Back 21

competative, selective for a1 R, a1 adrenergic antagonist
tx: chronic HTN
postural hypotension
tachy, impaired sexual fxn, nasal stuffiness

Front 22

Tamsulosin

Back 22

a1 adrenergic antagonist
Tx: benign prostatic hypertrophy

Front 23

Labetalol, carvedilol

Back 23

competative, a1 and B receptor blockers

Front 24

Atenolol

Back 24

B1-selective receptor blocker
no CNS activity, 1/2 life: 6-9 hrs
Tx: HTN

Front 25

metoprolol

Back 25

B1 selective R blocker
Tx: HTN

Front 26

Pindolol

Back 26

partial B1 agonist
Tx: HTN

Front 27

Propranolol

Back 27

Prototype, non-selective B1 and B2
Tx: HTN

Front 28

B1 selective and non selective antagoinsts

Back 28

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

Front 29

Metoprolol

Back 29

B1 blocker
Tx: Arrhythmia

Front 30

Atenolol

Back 30

B1 blocker
Tx: Angina
with discontinued use get rebound angina

Front 31

Pindolol

Back 31

non-selective, partial agonist)
Tx: Angina w/o rebound angina

Front 32

Beta antagonists "beta blockers"

Back 32

Tx:Congestive Heart Failure,Angina, Arrhythmia, HTN, post MI, tremor, glaucoma, migraine prophylaxis, hyperthyroidism: block of cardiac manifestations

Front 33

Propranolol

Back 33

Tremor, performance anxiety, Hyperparathyroidism: block of cardiac manifestations

Front 34

Timolol

Back 34

Glaucoma: decreases aqueous humor formation
B blocker : adrenergic antagonist.

Front 35

B blockers are bad for:

Back 35

Heart failure
Asthma & Hypoglycemia (B1 selective preferred)

Front 36

Reserpine

Back 36

Inhibition of intraneuronal storage of CAs, inhibits transport of NE from cytosol to vesicle, leads to depletion of NE and seretonin stores

Front 37

Bretylium

Back 37

prevention of N transmitter release, local anesthetic action

Front 38

List Antihypertensive Drugs

Back 38

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)

Front 39

NMJ is______ and is not ______

Back 39

NMJ:
IS part of the cholinergic NS but is
NOT part of the ANS.

Front 40

hemicholinium

Back 40

inhibits Ach formation by blocking choline and Na transport

Front 41

vesamicol

Back 41

inhibits Ach formation by inhibiting its storage in vessicles

Front 42

ChAT

Back 42

choline acetyltransferase synthesizes ACh from choline and acetyl CoA

Front 43

botulism toxin and bungarotoxin (snake venom)

Back 43

BT:inhibit ACh release
Bungaro: blocks post-synaptic ACh Receptor

Front 44

black widow spider venom

Back 44

increases ACh release

Front 45

Bethanechol

Back 45

Direct Acting Cholinomimetic at M receptor
Choline ester: quaternary
sm m of GIT and bladder

Front 46

Muscarine

Back 46

Direct acting Cholinnomimetic at M receptor
Alkaloid (N)
in mushroom amanita, competative antagonist

Front 47

Pilocarpine

Back 47

Direct acting Cholinnomimetic at M receptor
Alkaloid (N)--tertiary
tx: glaucoma, xerostomia

Front 48

Physostigmine

Back 48

Anticholinesterase, indirect acting
Reversible
Tertiary
CNS activity

Front 49

Neostigmine

Back 49

Anticholinesterase, indirect acting
Reversible
Quaternary amine
Little CNS activity
increases muscle strength in myasthenia gravis

Front 50

Rivastigmine, Donepezil, Tacrine

Back 50

Anticholinesterase, indirect acting
Reversible
Centrally acting
Tx: Alzheimers, incr ACh in CNS

Front 51

Echothiophate

Back 51

Irreversible Anticholinesterases
Organophosphate
long acting miotic

Front 52

Malathion

Back 52

Irreversible Anticholinesterases
Organophosphate insecticide
absorbed through skin
SLUDE, bronchoconstriction, bronchosecretions, bradycardia, decreased Q

Front 53

Sarin gas

Back 53

nerve gas
Irreversible Anticholinesterases
Organophosphate

Front 54

pralidoxime

Back 54

oxime: cholinesterase reactivation if aging hasn't occurred w/i 30-60 mins.
but give atropine first

Front 55

poisoning by anticholinergic, antimuscarinics

Back 55

atropine; also for antimuscarinic effects of TCAs. Physostigmine preferred b/c it enters CNS

Front 56

Acturium, Pancuronium, Vecuronium, Mivacurium

Back 56

Cholinergic Nicotinic NMJ Non-Deporarizing/Competative Blockers--> flaccid paralysis

Front 57

how do you reverse non depolarizing blockers?

Back 57

atropine then anticholinesterase (neostigmine)

Front 58

Succinylcholine

Back 58

Nicotinic, Depolarizing (partial agonist) blocker--> initial stimulation (fasciculations) then paralysis --short acting

Front 59

succinylcholine toxicity can be reversed by?

Back 59

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!

Front 60

Mecamylamine

Back 60

nicotinic Ganglion blocker direct
for hypertensive crisis, tertiary, oral/injection, short term

Front 61

How is non-depolarizing NMJ blockade reversed?

Back 61

ex: Atracurium;
first--atropine
second--anticholinesterase (neostigmine)

Front 62

Which drug may cause muscarinic effects?
d-tubocurare
succinylcholine
vecuronium

Back 62

succinylcholine

Front 63

activation of muscarinic R (cholinergic) what effects will this have?

Back 63

SLUDE + bradycardia, bronchial secretions
(parasympathetic actions)

Front 64

If you OD on cholinergic drug, which will you NOT see?
Myosis
Mydriasis
incontinence
impotency

Back 64

mydriasis (photophobia) is an adverse effect of antimuscarinic drugs

Front 65

antimuscarinic drugs are _____ of acetylcholine. They act selectively at _____ receptors

Back 65

competative antagonists
muscarinic

Front 66

small doses atropine

Back 66

tertiary amine; antimuscarinic agent; decrease salivation, bronchial secretions, and sweating

Front 67

scopolamine

Back 67

tertiary amine; antimuscarinic; alkaloid; CNS depressant, drowsiness, amnesia, fatigue; anti-emetic

Front 68

dicyclomine

Back 68

tertiary amine; antimuscarinic; tx: bowel spasm

Front 69

tropicamide

Back 69

tertiary amine; antimuscarinic; topical to produce mydriasis (dilation) and cyclolegia (nearsightedness)

Front 70

benztropine
trihexyphenidyl

Back 70

tertiary amine; antimuscarinic; tx: Parkinsons

Front 71

Ipratropium

Back 71

quaternary nitrogen; antimuscarinic; tx: COPD

Front 72

Trospium, tolterodine, oxybutynin

Back 72

quaternary nitrogen; antimuscarinic; tx: urinary incontinence

Front 73

larger doses atropine

Back 73

tertiary amine; antimuscarinic agent; pupil dilates, accommodation is inhibited, increased HR, inhibit PNS of GIT and bladder

Front 74

toxic dose of atropine

Back 74

tertiary amine; antimuscarinic agent; restlessness, irritability, disorientation and hallucinations, depression, coma, medullary paralysis and death

Front 75

Posioing with atropine

Back 75

Red, hot, dry, blind, mad
dry mouth, blurred vision, photophobia, hot, dry, flushed skin, increased temp, tachycardia, urinary retention

Front 76

Lomotil

Back 76

tx diarrhea

Front 77

Antimuscarinic in the Respiratory tract

Back 77

emphysema induces bronchial dilatation
Ipratropium

Front 78

Antimuscarinic in the GU tract

Back 78

reduces urinary frequency or urgency
Trospium, tolteridine, oxybutynin

Front 79

Antimuscarinic in the GI tract

Back 79

dicyclomine; IBS, diverticulosis

Front 80

Antimuscarinic for Ophthalmological

Back 80

for mydriasis and cycloplegia
homatropine, tropicamide

Front 81

antimuscarinic for CVS

Back 81

atropine for bradycardia or for heart block

Front 82

antimuscarinic for cholinergic poisoning

Back 82

atropine; treats amanita muscaria and anticholinesterases (pesticides)

Front 83

antimuscarinic for parkinson's

Back 83

benztropine, trihexyphenidyl

Front 84

Antimuscarinic for Anti-emetic

Back 84

scopolamine to treat motion sickness

Front 85

treat antimuscarinic toxicity with

Back 85

physostigmine (tertiary anticholinesterase, reversible) or neostigmine (quaternary)
benzodiazepine for agitation

Front 86

vincristine

Back 86

blocks mitosis

Front 87

Fractional cell kill hypothesis

Back 87

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

Front 88

1cm mass

Back 88

clincally detected, 10 to the 9 cells, 30 divisions

Front 89

Alters drug transport

Back 89

Multi-drug resistance phenotype with enhanced expression oth the membrane p-glycoprotein pump

Front 90

Imatinib

Back 90

Tyrosine Kinase Inhibitor
inhibits ABL-BCR fusion
CML

Front 91

Gefitinib

Back 91

Tyrosine Kinase Inhibitor
inhibits EDGF
non small cell lung cancer
rash

Front 92

Sunitinib

Back 92

Tyrosine Kinase Inhibitor
inhibits VEGF
renal cancer

Front 93

Rituximab

Back 93

Monoclonal Ab
CD20
B cell lymphoma
infusion rxn, B cell depletion, neutropenia

Front 94

Alemtuzumab

Back 94

Monoclonal Ab
CD52
T-cell lymphoma
infusion rxn, pancytopenia

Front 95

Trastuzumab

Back 95

Monoclonal Ab
Her2/neu--Erb-2
breast ca.
CARDIOMYOPATHY

Front 96

Cetuximab

Back 96

Monoclonal Ab
EGFR
colorectal cancer
infusion rxn

Front 97

Bevacizumab

Back 97

Monoclonal Ab
VEGF
colorectal cancer
HTN, CHF, pulmonary or GI hemorrhage

Front 98

IL-2

Back 98

cytokine:
produces lymphocytes cytolytic for tumor cells

renal cell carcinoma, metastatic melanoma

Front 99

Colony stimulating factors

Back 99

differentiating agents
at various stages in hematopoietic hierarchy.
use to replenish blood cells

Front 100

Retinoic Acid

Back 100

Differentiating Agent
influence epithelial cells
Tx: BPL, acute myelocytic leukemia

Front 101

Antiangiogenesis agents do what?

Back 101

reduce vascular supply to tumor. none are on market now

Front 102

bortezomib

Back 102

Proteasome inhibitors
inhibits 26S proteasome
Tx of: mult. myeloma

Front 103

Radioimmunoconjugates
ex: Iodine-131 tositumomab

Back 103

Proteosome inhibitors
bind to CD20 antigen on malignant B cells
used in non-Hodgkin's lymphoma
SE: thyroid toxicity, prolonged myelosuppression

Front 104

Mechanisms of Antineoplastic Drugs

Back 104

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

Front 105

Selectivity of antineoplastic drugs

Back 105

differences btwn host and malignant cells; often differences aren't great

Front 106

Mech of resistance of antinoplastic drugs

Back 106

altered affinity for binding site
decreased activation or increased deactivation
altered transport
**most drugs increase in efflux via MDR pump**

Front 107

Host toxicity -- generally to more rapidly dividing cells

Back 107

myelosuppression
GI mucosal irritation
alopecia and inhibits fertility

Front 108

Methotrexate

Back 108

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

Front 109

5-Fluorouracil

Back 109

pyrimidine antimetabolite (S phase)not affected by MDR
inhibitor of thymidylate synthetase
tx: breast and GI tumors, skin lesions and warts

Front 110

Cytosine Arabinose

Back 110

pyrimidine antimetabolite (S phase)not affected by MDR
competes w/ dCTP for incorporation into DNA; inhibits DNA synthesis
tx: potent antileukemic

Front 111

6-mercaptopurine and 6-thioguanine

Back 111

purine antimetabolite (S phase)not affected by MDR
guanine and hypoxanthine analogs
--> to deoxyribonucleotide derivatives by HGPRT; incorporate into DNA
toxicity: PANCREATITIS

Front 112

Hydroxyurea

Back 112

analog of urea
inhib of ribonucleotide reductase inhibits DNA synthesis
Tx:acute and chronic leukemia; myeloproliferative disorders
toxicity: bone marrow and GI

Front 113

Adriamycin (Doxorubicin);
Daunorubicin

Back 113

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

Front 114

Mixoxantrone

Back 114

like anthracycline, but decreased free radicals and reduces cardiotoxicity

Front 115

VP-16 (etoposide);
VM-26 (teniposide)

Back 115

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

Front 116

(topotecan, irinotecan)
camptothecins

Back 116

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

Front 117

Vincristine

Back 117

Microtubule inhibitor
Vinca alkaloid
Hodgkin's, acute lymphoblastic leukemia
toxicity: Neurotoxicity

Front 118

Paclitaxel, docetaxel

Back 118

yew tree
interacts w/ microtubules, prevents depolymerization
tx: solid tumors: ovarian, breast, lund ca.
MRD
toxicity: neurotoxicity, BM

Front 119

Nitrogen mustards, nitrosoureas, cyclophosphamide

Back 119

alkylating agent
not cell cycle specific most sensitive
no MDR
Alkylation of DNA
toxicity: bone marrow suppression, immunosuppression

Front 120

procarbazine, hexamethylmelamine

Back 120

require metabolic activation, Hodgkin's disease (procarbazine)
Ovarian
(hexa)

Front 121

Streptozotocin

Back 121

methylnitrosourea derivative
alkylates DNA, single strand breaks in DNA
toxicity: bone marrow depression and GI and nephrotoxicity

Front 122

Dacarbazine

Back 122

requires micorsomal activation
monofunctional alkylator
inhibits DNA and RNA protein synthesis
not cell cycle specific
toxicity: nausea

Front 123

Mitomycin C

Back 123

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

Front 124

CIS (PLatinol)

Back 124

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

Front 125

Bleomycin

Back 125

breaks DNA by free radical mech
use: squamous cell carcinoma; Hodgkins and non Hodgkins lymphoma
toxicity: pulmonary toxicity

Front 126

Aspariginase

Back 126

inhibition of protein synthesis

Front 127

Tamoxifen

Back 127

compete w/ N estrogens
prevent growth in estrogen dependent tumors

Front 128

Anastrazole

Back 128

Aromatase inhibitor
reduce synthesis of estrogen

Front 129

flutamide

Back 129

compete with N androgens for binding sites
tx: prostate ca.

Front 130

Leuprolide

Back 130

LHRH agonist
inhibit androgen release
prostate ca. -->flare

Front 131

GnRH antagonist

Back 131

for pt who need to avoid flare
prostate ca.