Pharmacology

Front 1

binds to cyclophilins.

complex blocks the differentiation and activation of T cells by inhibiting calcineurin >> prevents productions of IL-2 and its receptor

suppresses organ rejection; AI diseases

Back 1

Cyclosporine

SE: viral infections, lymphomas, nephrotoxic (prevent w/ mannitol)

Front 2

binds to FK-binding protein, inhibiting secretion of IL-2 and other cytokines

used in organ transplant recipients for immunosuppression

Back 2

Tacrolimus (FK506)

SE: nephrotoxicity

Front 3

binds to mTOR. inhibits T-cell proliferation in response to IL-2

post kidney transplantation in combination with cyclosporine and corticosteroids

Back 3

Sirolimus (Rapamycin)

SE: hyperlipidemia thrombocytopenia, leukopenia

Front 4

monoclonal antibody with high affinity for the IL-2 receptor on activated T cells

Back 4

Daclizumab

Front 5

Antimetabolite precursor of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids. Toxic to proliferating lymphocytes

kidney transplantation, AI disorders (glomerulonephritis and hemolytic anemia)

Back 5

Azathioprine

Front 6

monoclonal antibody that binds to CD3 (epsilon chain) on the surface of T cells.

Blocks cellular interatction with CD3 protein responsible for T-cell signal transduction

kidney transplantation

Back 6

Muromonab-CD3 (OKT3)

SE: cytokine release syndrome, hypersensitivity reaction

Front 7

erythropoeietin (epoetin)

clinical use?

Back 7

anemias (especially in renal failure)

Front 8

Aldesleukin
(IL-2)

clinical use?

Back 8

Renal cell carcinoma

metastatic melanoma

Front 9

what is the equation to find the half-life of a drug?

Back 9

t1/2 = (0.7 x Vd) / (CL)

Front 10

a drug infused at a constant rate takes _____ half-lives to reach steady state.

Back 10

4-5 half-lives

Front 11

phenytoin, ethanol, aspirin?

Back 11

all follow zero-order elimination

Front 12

phenobarbital, methotrexate, aspirin

treat this type of overdose with?

Back 12

weak acids (trapped in basic environment)

tx: bicarbonate

Front 13

amphetamines represent what type of pH?

treat this type of overdose with?

Back 13

weak bases (trapped in acidic environment)

tx: ammonium chloride

Front 14

reduction, oxidation, hydrolysis...

where do these occur (under what system)?

what do they often yield as product?

Back 14

Phase I metabolism

P-450

yields slightly polar, water-soluble metabolites (often still active)

Front 15

acetylation, glucuronidation, sulfation

where do these occur (under what system)?

what do they often yield as product?

Back 15

Phase II

conjugation

yields very polar, inactive metabolites (renally excreted)

Front 16

geriatric patients lose which phase of metabolism first?

Back 16

Phase I

Front 17

1st pass metabolism is via ____ (oral) and is relative to the bioavailability in systemic circulation

therefore, these types of drug routes can bypass this step for quicker distribution

Back 17

liver

subL
subQT
suppositories (rectal)
IV

Front 18

metabolizes steroids, alcohol, toxins, etc; can also activate inactive pro-carcinogens

Back 18

cytochrome P450 monooxygenase

Front 19

glutathione-S-transferase

Back 19

detoxification

converts toxics >>> inactive metabolites

Front 20

botulinum toxin prevents release of neurotransmitter at all _______ terminals

Back 20

cholinergic

Front 21

Nicotinic ACh receptors are ligand-gated ___ channels

Back 21

Na+/K+ channels

Front 22

Muscarinic ACh receptors are _________ receptors that act through second messengers

Back 22

G-protein-coupled receptors

Front 23

(Drug) inhibits conversion of Choline >> Acetyl-CoA+Choline

Back 23

Hemicholinium

Front 24

(drug) inhibits ChAT >> ACh

Back 24

Vesamicol

Front 25

(drug) inhibits conversion tyrosine >> DOPA

Back 25

Metyrosine

Front 26

(drug) inhibits conversion Dopamine >> NE

Back 26

Reserpine

Front 27

(drug) inhibits release of NE in presynaptic terminal

Back 27

Guanethidine

Front 28

(drug) activates NE release from presynaptic terminal

Back 28

Amaphetamine

Front 29

(drug) inhibit NE reuptake

Back 29

Cocaine, TCAs, amphetamine

Front 30

Release of NE from a sympathetic nerve ending is modulated by NE itself, acting on presynaptic ___ autoreceptors, and by ACh, _________, and other substance

Back 30

a2; angiotensin II

Front 31

bethanechol
carbachol
pilocarpine
methacholine

Back 31

direct ACh agonists

Front 32

neostigmine
pyridostigmine
edrophonium
physostigmine
edrophonium
physostigmine
echothiophate

Back 32

indirect ACh antagonists
(anticholinesterases)

Front 33

cholinomimetic agents lead to COPD, __, and _____ in some susceptible patients

Back 33

asthma, peptic ulcers

Front 34

farmer with diarrhea, urination, miosis, bronchospasm, bradycardia, lacrimation, sweating, salivation

what is the antidote?

Back 34

cholinesterase inhibitor poisoning

often due to organophosphates, such as parathion that irreversibly inhibit AchE; found in insecticides

Antidote -- atropine + pralidoxime
(regenerates active AchE)

Front 35

atropine, homatropine, tropicamide

clinical use?

Back 35

produce mydriasis and cycloplegia (eye)

Front 36

benztropine

clinical use?

Back 36

Parkinson's disease (CNS)

Front 37

scopalamine

Back 37

motion sickness (CNS)

Front 38

Ipratoprium

Back 38

Asthma, COPD (respiratory)

Front 39

Oxybutynin,
glycopyrrolate

Back 39

reduce urgency in mild cystitis and reduce bladder spasms (Genitourinary)

Front 40

Methscopolmaine,
pirenzepine,
propantheline

Back 40

peptic ulcer treatment (GI)

Front 41

after administration of this drug, SEs include fever, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation

Back 41

Atropine

acute angle-closure glaucoma (elderly)
urinary retention in men with prostatic hyperplasia
hyperthermia in infants

Front 42

ganglionic blocker
prevent vagal reflex responses to changes in blood pressure (prevents reflex bradycardia caused by NE

Back 42

Nicotinic antagonist

SEs: severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction

Front 43

atropine
TCAs (amitriptyline)
HI receptor antagonists (diphenihydramine)
neuroleptics
antiparkinsonian drugs

Back 43

all lead to antimuscarinic effects

Front 44

Epinephrine

Back 44

anaphylaxis, glaucoma (open angle),
asthma
hypotension

Front 45

NE

Back 45

hypotension (but decrease in renal perfusion)

Front 46

Isoproterenol

Back 46

AV block (rare)

Front 47

Dopamine

Back 47

shock (increased renal perfusion)
heart failure

Front 48

Dobutamine

Back 48

heart failure,
cardiac stress testing

Front 49

Phenylephrine

Back 49

pupillary dilation,
vasoconstriction,
nasal decongestion

Front 50

Metaproterenol,
albuterol,
salmeterol,
terbutaline

Back 50

metaproterenol + albuterol = acute asthma

salmeterol = long-term tx

terbutaline = reduce premature uterine contractions

Front 51

ritodrine

Back 51

reduces premature uterine contractions

Front 52

amphetamine

Back 52

narcolepsy, obesity, ADD

(releases stored catecholamines; indirect sympathomimetics)

Front 53

ephedrine

Back 53

nasal decongestion,
urinary incontinence,
hypotension
(releases stored catecholamines; indirect sympathomimetics)

Front 54

cocaine

Back 54

causes vasoconstriction and local anesthesia

(uptake inhibitor)

Front 55

clonidine,
a-methyldopa

Back 55

hypertension, especially with renal disease (no decrease in blood flow to kidney)

Front 56

phenoxybenzamine (irrev)
phentolamine (reversible)

Back 56

nonselective a-blockers

pheochromocytoma

NE extravasation/vasoconstriction/vein blanching (within 12 hr)

SE: orthostatic hypotension, reflex tachycardia

Front 57

prazosin, terazosin, doxazosin

Back 57

a1 selective a-blocker
hypertension, urinary retention in BPH

SE: 1st dose orthostatic hypotension, dizziness, HA

Front 58

mirtazapine

Back 58

a2 selective a-blocker
depression

SE: sedation, increased serum cholesterol, increased appetite

Front 59

increased vascular smooth muscle contraction
increased pupillary dilator muscle contraction (mydriasis)
increased intestinal and bladder sphincter muscle contraction

Back 59

a1 receptor

(Epi, NE, Pheylephrine, Methoxamine)

Front 60

decreased sympathetic outflow
decreased insulin release

Back 60

a2 receptor

Front 61

increased HR
increased contractility
increased renin release
increased lipolysis

Back 61

b1 receptor

(Epi, DA, dobutamine, isoproterenol)

Front 62

vasodilation
bronchodilation
increased HR
increased contractility
increased lipolysis
increased insulin release
decreased uterine tone

Back 62

b2 receptor

(isoproterenol, terbutanine, ritodrine)

Front 63

(receptor)
CNS, enteric nervous system

Back 63

M1 receptor

Front 64

(receptor)
decreased heart rate and contractility of atria

Back 64

M2 receptor

Front 65

(receptor)
increased exocrine gland secretions
increased gut peristalsis
increased bladder contraction
bronchoconstriction
increased pupillary sphincter muscle contraction (miosis)
ciliary muscle contraction (accommodation)

Back 65

M3 receptor

Front 66

(receptor)
relaxes renal vascular smooth muscle

Back 66

D1 receptor

Front 67

(receptor)
modulates transmitter release, especially in brain

Back 67

D2 receptor

Front 68

(receptor)
increased nasal and bronchial mucus production,
contraction of bronchioles, pruritis, and pain

Back 68

H1 receptor

Front 69

(receptor)
increased gastric acid secretion

Back 69

H2 receptor

Front 70

(receptor)
increased vascular smooth muscle contraction

Back 70

V1 receptor

Front 71

(receptor)
increased H2O permeability and reabsorption in the collecting tubules of the kidney

Back 71

V2 receptor

Front 72

class of drugs used to treat:
hypertension
angina pectoris
MI
SVT
CHR
glaucoma

Back 72

beta-blockers

Front 73

propranolol, timolol, nadolol, pindolol

Back 73

nonselective antagonists (b1=b2)

Front 74

betaxolol, esmolol (short acting), atenolol, metoprolol

Back 74

b1-selective antagonists

Front 75

carvedilol, labetalol

Back 75

nonselective a- and b-antagonists

Front 76

pindolol, acebutolol

Back 76

partial b-agonists

Front 77

quinidine
barbiturates
St. John's wort
phenytoin

Back 77

p-450 inducers

Front 78

griseofulvin
carbamazepine
alcohol (chronic)
phenobarbitol

Back 78

p-450 inducers

Front 79

HIV protease inhibitors
ketoconazole
erythromycin
grapefruit juice

Back 79

p-450 inhibitors

Front 80

acute alcohol use
sulfonamides
isoniazid
ritonavir

Back 80

p-450 inhibitors

Front 81

cimetidine
ciprofloxacin
Azole antifungals

Back 81

p-450 inhibitors

Front 82

-ane

Back 82

inhalational gneeral anesthetic

(halothane)

Front 83

-azine

Back 83

phenothiazine (neuroleptic, antiemetic)

chlorpromazine

Front 84

-cycline

Back 84

antibiotic, protein synthesis inhibitor

Front 85

-etine

Back 85

SSRI

(fluoxetine)

Front 86

-ipramine

Back 86

TCA
(imipramine)

Front 87

-navir

Back 87

protease inhibitor
(saquinavir)

Front 88

-phylline

Back 88

methylxanthine
(theophylline)

Front 89

-triptan

Back 89

5-HT1B/1D agonists (migraine)

Sumatriptan

Front 90

-triptyline

Back 90

TCA
(Amitriptyline)