Pharmacology BRS - Flash Cards

101
1 beclomethasone synthetic glucocorticoid that readily penetrates the airway mucosa, used for asthma thioridazine low potency dopamine receptor blocker thioridazine side effects are retinal deposits, torsades, postural hypotension, sedation, CNS depression valproic acid causes neural tube defects valproic acid used to treat all kinds of seizures, as well as bipolar disorder

Transcript of Pharmacology BRS - Flash Cards

Page 1: Pharmacology BRS - Flash Cards

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beclomethasone synthetic glucocorticoid that readily penetrates the airway mucosa, used for asthma

thioridazine low potency dopamine receptor blocker

thioridazine side effects are retinal deposits, torsades, postural hypotension, sedation, CNS depression

valproic acid causes neural tube defects

valproic acid used to treat all kinds of seizures, as well as bipolar disorder

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zolpidem binds benzodiazepine receptors, antagonized by flumazenil

zolpidem hypnotic drug that is not a benzodiazepine

amphetamines indirect sympathomimetic MOA

cocaine inhibits catecholamine reuptake, resulting in cardiotox and hypertension

disulfiram inhibits aldehyde dehydrogenase, causing an accumulation of acetaldehyde

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flunitrazepam benzodiazepine used as a date rape drug

lysergic acid diethylamide hallucinogenic, nausea, weakness

mescaline hallucinogenic, nausea, weakness

psilocybin hallucinogenic, nausea, weakness

marijuana lowers intraocular pressure in glaucoma

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methadone treatment of opiod withdrawal

opioid withdrawal syndrome nausea, chills, sweats, lacrimation, cramps, rhinorrhea, yawning, piloerection, diarrhea, tremor

MPTP destroys dopaminergic neurons of the nigrostriatal tract

morphine binds mu receptors

enkephalin binds delta receptors

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dynorphins bind kappa receptors

opioid overdose constricted pupils, clammy skin, nausea, drowsiness, resp depression

phencyclidine (pcp) nystagmus, hypertension, seizure

acetaminophen COX inhibitor which inhibits prostaglandin synthesis

acetaminophen analgesic, antipyretic (but not anti-inflammatory)

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allopurinol suicide inhibition of xanthine oxidase

allopurinol increases xanthine and hypoxanthine, which are less likely to form crystals than uric acid

allopurinol slows production of uric acid, used to treat gout (and cancer)

aspirin PGE inhibitor

aspirin predisposes to acute gastritis by inhibiting PGE in the stomach

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aspirin irreversible inhibitor of cyclooxygenase

aspirin analgesic, antipyretic, antiplatelet, anti-inflammatory

capsaicin impairs release of substance P

capsaicin used topically for RA

celecoxib COX-2 inhibitor

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rofecoxib COX-2 inhibitor

celecoxib sulfa drug

rofecoxib sulfa drug

colchicine inhibits microtubule assembly, and therefore leukocyte migration and phagocytosis

colchicine leukocyte inhibitor used to treat attacks of gouty arthritis

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cyclosporin binds to cyclophilins and inhibits the transcription of cytokine genes

tacrolimus binds to the immunophilin FK-binding protein

cyclosporin impairs T cell IL-2 production, used in transplant patients

tacrolimus used in transplant patients

etanercept a fusion product of TNF-alpha receptor and Fc portion of antibody

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infliximab binds and inhibits TNF-alpha

etanercept used in RA and inflammatory bowel disease

gold salts nephrotoxic

gold salts used in RA

gold salts decreases lysosomal and macrophage function

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ibuprofen similar to aspirin, lacks antiplatelet effects

ibuprofen reversibly inhibits COX

indomethacin potent NSAID used to close a PDA

PGE used to maintain a PDA in congenital heart disease

ketorolac parenteral NSAID

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meperidine causes relaxation of the sphincter of oddi

meperidine causes increased ICP

opiods causes biliary spasm

sumatriptan binds the serotonin 1D receptor

sumatriptan causes vasoconstriction of cerebral vasculature

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sumatriptan used for acute migraine and cluster headaches

thalidomide used to treat SLE, multiple myeloma, and leprosy

thalidomide suppresses production of TNF-alpha

thalidomidepotent

immunosuppressant

statins may cause elevated liver enzymes

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statins may cause myositis

statins may cause increased CK from skeletal muscle

reserpine enters the CNS and may cause suicidal depression and parkinsonian symptoms

reserpineantihypertensive agent that blocks the storage and

release of catecholamines and serotonin from neurons

probucol decreases HDL as well as LDL

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probucol prevents restenosis after angioplasty

probucol acts as an antioxidant

nitroglycerin postural hypotension, headache, flushing

nitroglycerin causes increase in cGMP in vascular smooth muscle

niacin directly reduces secretion of VLDLs

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niacin increases HDL

niacin causes cutaneous flushing

vincristine M phase inhibitor

vincristine blocks microtubule polymerization and spindle formation

ABVD adriamycin, bleomycin, vinblastine, dacarbazine

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MOPP mechlorethamine, oncovin, procarbazine, prednisone

vincristine used for lymphomas, wilms tumor, and choriocarinomas

heparin activates AT3

heparin inactivates thrombin

protamine sulfate reverses effects of heparin

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trastuzumab binds to receptor tyrosine kinase Erb-B2 (HER-2)

trastuzumab used for HER-2 positive breast cancer

tamoxifen estrogen receptor partial antagonist

tamoxifen increases risk of endometrial carcinoma

rituximab binds CD20 antigen on B cells

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rituximab treatment of non-hodgkin lymphoma

prednisone triggers apoptosis

prednisone treatment for leukemia, lymphoma, RA, asthma

paclitaxel prevents mitotic spindle breakdown

paclitaxelinterferes with

anaphase

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paclitaxel microtubule stabilizing agent

methotrexate S phase inhibitor

methotrexate inhibits DHFR

leucovorintreats

myelosuppression

methotrexate folic acid analog

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mercaptopurine (6-MP)

activated by hypoxanthine-guanine phosphoribosyltransferase (HGPRT)

mercaptopurine (6-MP)

inhibits many enzymes involved in purine metabolism

leuprolide treatment for endometriosis

leuprolide treatment for BPH and precocious puberty

leuprolide stimulates release of FSH and LH

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leuprolide GnRH agonist used to treat prostate cancer

interferon alpha produced by virally infected cells to prevent infection of adjacent cells

interferon alpha used to treat CML, malignant myeloma, kaposi sarcoma, hairy cell leukemia

interferon alpha recombinantly produced cytokine

flutamide used to antagonize residual androgens after orchiectomy

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flutamide side effects include gynecomastia and libido changes

flutamide androgen receptor antagonist

fluorouracil S phase antimetabolite

fluorouracilcauses

myelosuppression

fluorouracil inhibits thymidylate synthase

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fluorouracil used to treat colon cancer and basal cell carcinoma

etoposide G2 phase inhibitor

etoposide causes double stranded breaks in DNA

etoposide inhibits topoisomerase II

etoposide used to treat small cell carcinoma of the lung and prostate and testicular cancers

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doxorubicin intercalates in DNA to reduce replication and transcription

doxorubicin causes dilated cardiomyopathy

daunorubicin used to treat AML

cyclophosphamide causes hemorrhagic cystitis

cyclophosphamidealkylating agent used to treat

cancers

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cisplatin alkylating agent

cisplatin causes nephrotoxicity and acoustic nerve damage

carmustine alkylating agent that causes DNA cross-linking and strand breaks

carmustine used to treat brain tumors, highly lipophilic nitrosourea drug

bleomycin mixture of glycoproteins that produce free radicals upon binding DNA

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bleomycin causes strand breaks in DNA

bleomycin G2 phase inhibitor

bleomycin can cause pulmonary fibrosis

anastrozole inhibitor of steroid synthesis

anastrozole inhibits conversion of androstenedione to estrone

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aminoglutethimide blocks conversion of cholesterol to pregnenolone

anastrazole aromatase inhibitor

zidovudine inhibits viral reverse transcriptase

zidovudine chain terminator

zidovudine given to prevent transmission of HIV to neonates

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vancomycin used to treat MRSA

vancomycin used to treat c. difficile

vancomycin rapid IV infusion causes red man syndrome

TMP-SMX blocks folate synthesis

TMP-SMX can cause megaloblastic anemia

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TMP-SMX do not give to pts with G6PDH deficiency

trimethoprim blocks DHFR

sulfamethoxazole blocks dihydropteroate synthase

tetracycline inhibits 30s ribosome

tetracycline bacteriostatic drug

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tetracycline CI in pregnant women due to bone dysplasia and dental enamel defects

streptogramins p450 inhibitor

streptograminsarthralgias and

myalgias

streptogramins used to treat MRSA and VRE

rifampin inhibits DNA-dependent RNA polymerase

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rifampin imparts red-orange color to secretions

ribavirin guanosine analog

ribavirin inibits steps in RNA synthesis

ribavirin used to treat viral hemorrhagic fevers and hepatitis C

ribavirin used to treat RSV

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quinine blocks DNA replication and RNA transcription in p. falciparum within RBCs

quinine causes cinchonism

cinchonism headache, vertigo, blurry vision, tinnitus

mefloquine used for prophylaxis of p. falciparum due to low SE

quinine used for malaria

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pyrantel pamoate stimulates nicotinic receptors in nematodes

praziquantel used for fluke and tapeworm infections

polymyxin b cationic detergent that disrupts bacterial membranes

polymyxin b causes neurotoxicity and acute tubular necrosis

polymyxin b only used topically

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penicillins inhibits transpeptidation step in bacterial cell wall synthesis

oseltamivir neuraminidase inhibitor that prevent viral spreading

oseltamivirused against influenza

a

nystatin disrupts fungal membrane permeability by binding to ergosterol

nystatin used to treat oral candidiasis and diaper rash

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nitrofurantoin can cause hemolysis in G6PDH deficient patients

nitrofurantoin can accumulate to toxic levels in patients with renal failure

nitrofurantoin urinary antiseptic that requires acidification

nifurtimox used to treat chagas disease

nevirapineNNRTI used to treat

HIV

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neomycin used to treat hepatic encephalopathy

neomycin prevents accumulation of nitrogenous microbial metabolites

metronidazole activated by anaerobes and parasites

metronidazole interferes with nucleic acid synthesis

metronidazole used to treat amebiasis, trichomoniasis, giariasis, and c. diff

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methicillin bulky R-group prevents degradation by penicillinase

nafcillin bulky R-group prevents degradation by penicillinase

dicloxacillin bulky R-group prevents degradation by penicillinase

methi, naf, diclox beta lactams

mebendazole inhibits microtubule synthesis and glucose uptake by helminths

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mebendazole used to treat pinworms

albuterol selective b2 agonist

atenolol selective b1 blocker

acebutolol selective b1 blocker

metoprolol selective b1 blocker

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detromethrophan depresses cough center in the medulla

metoclopramide facilitates acetylcholine while blocking dopamine in the enteric nervous system

metoclopramide SE are sedation, diarrhea, extrapyramidal symptoms

metoclopramide prokinetic agent used to block emesis

metoclopramide blocks D2 receptors in the area postrema

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misoprostol PGE analog

misoprostol decreases gastric acid production, increases mucus production

misoprostol eicosanoid preparation used for pts taking lots of NSAIDs

omeprazole H/K ATPase inhibitor

ondansetron serotonin-3 inhibitor that acts at the area postrema

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sucralfate requires acidic environment to polymerize

sucralfate cannot be used with antacids or H2 blockers

folic acid will correct anemia but not neuro sx associated with b12 deficiency

EPO recombinant drug used for anemia

aminocaproic acidorally active inhibitor of plasminogen activation

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aminocaproic acid inhibits fibrinolysis

aminocaproic acid used for acute bleeding in hemophilic patients

abciximab antibody against glycoprotein 2b/3a receptor

abciximab prevents platelet activation

abciximab anticoagulant preventing restenosis after angioplasty

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benztropine antimuscarinic

benztropine CI are prostatic hyperplasia, GI obstruction, glaucoma

benztropine antimuscarinic used to treat tremors and rigidity in parkinsons, but does nothing for bradykinesia

RhoGAM antibody to Rh(D) antigen that opsonizes

probenecid competes with uric acid for reabsorption in the proximal tubule

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probenecid inhibits secretion of weak acids

sulfinpyrazone acts simliarly to probenecid

methylsergide blocks serotonin receptors

methylsergidecauses fibroplasia of retroperitoneum and subendocardium

methylsergide used to prevent migraines

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daclizumab binds IL-2 receptor on activated T cells

daclizumab used for patients with renal allografts

bromocriptine D2 agonist

bromocriptine inhibits PRL release

diphenhydramineinhibit histamine binding to H1

receptors

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diphenhydramine causes drowsiness

diphenhydramine used for allergies and motion sickness

cromolyn sodium stabilizes mast cell membrane

lithium inhibits IP3 and DAG

lithium causes tremor, hypothyroidism, polydipsia, polyuria

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methylphenidate stimulates the release of catecholamines

phenytoin inducer of p450

carbamazepine inducer of p450

griseofulvin inducer of p450

rifampin inducer of p450

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barbiturates inducer of p450

penicillins bactericidal

cephalosporins bactericidal

vancomycin bactericidal

aminoglycosides bactericidal

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fluoroquinolones bactericidal

metronidazole bactericidal

calcium channel blockers

causes cutaneous flushing

adenosine causes cutaneous flushing

vancomycin causes cutaneous flushing

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metronidazole causes disulfiram-like reaction

cephalosporins causes disulfiram-like reaction

procarbazine causes disulfiram-like reaction

nitrous oxide has a high MAC

phenelzine MAOI

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tranylcypromine MAOI

isocarboxazid MAOI

MAOI + SSRI serotonin syndrome

MAOI inhibits breakdown of amine neurotransmitters

mebendazole microtubule inhibitor

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thiabendazole microtubule inhibitor

paclitaxel microtubule inhibitor

vincristine microtubule inhibitor

colchicine microtubule inhibitor

griseofulvin microtubule inhibitor

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hydralazine SLE like syndrome

procainamide SLE like syndrome

isoniazid SLE like syndrome

phenytoin SLE like syndrome

halothanemassive hepatic

necrosis

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acetaminophenmassive hepatic

necrosis

valproic acidmassive hepatic

necrosis

cimetidine p450 inhibitor

ketoconazole p450 inhibitor

erythromycin p450 inhibitor

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cimetidine gynecomastia

ketoconazole gynecomastia

spironolactone gynecomastia

bleomycin pulmonary fibrosis

amiodarone pulmonary fibrosis

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busulfan pulmonary fibrosis

aminoglycosidesototoxic and nephrotoxic

loop diureticsototoxic and nephrotoxic

cisplatinototoxic and nephrotoxic

vancomycin mildly ototoxic and nephrotoxic

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penicillamine used to treat wilson disease

penicillamine used to treat RA

penicillamine used to treat copper toxicity bc it is a chelator

organophosphates anticholinesterases used in chemical warfare

pralidoxime antidote for anticholinesterases such as organophosphates

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naloxone mu opioid receptor antagonist

naloxone used to treat opioid overdose

phenobarbital binds GABA receptors

phenobarbital increases the duration of chloride channel opening

phenobarbital used to treat tonic-clonic seizures and crigler-najjar

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phenytoin interferes with folate absorption

phenytoin SE are gingival hyperplasia, hirsutism, anemia, and birth defects

phenytoin class 1b antiarrhythmic

risperidone blocks D2 and serotonin-2 receptors

risperidone causes high sedation

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risperidone atypical antipsychotic with lots of extrapyramidal SE

ropinirole forestalls the use of levodopa in parkinson's disease

methanol causes damage by being converted to formaldehyde in the liver

methanol retinal damage, blindness, metabolic acidosis, coma

flumazenil antagonizes benzodiazepines and zolpidem

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flumazenil used for benzodiazepine overdose

ethylene glycol causes metabolic acidosis and precipitation of oxalate crystals in the kidney

dimercaprol chelates metals to keep them from damaging proteins

succimer orally active metal chelator

dimercaprol used to treat heavy metal poisoning

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digibind fab fragment antibody

deferoxamine rapid infusion causes hypotensive shock

deferoxamine used to treat acute iron toxicity

dantrolene decreases the release of calcium from the sarcoplasmic reticulum

dantrolene used to treat malignant hyperthermia

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selegiline inhibits MAO-B

MAO-B degrades dopamine

selegiline inhibits degradation of dopamine in CNS, used with levodopa for parkinson's

thiopental ultra-short acting barbiturate used to induce surgical anesthesia

alprazolam intermediate-acting benzodiazepine used for panic disorder and phobias

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n-acetylcysteine protects against fulminant hepatic failure

n-acetylcysteine used for acetaminophen overdose

carvedilol used for CHF

carvedilol nonselective beta blocker and alpha-1 blocker

amiodaroneblocks sodium

channels

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amiodarone corneal microdeposits

amiodarone class III antiarrythmic

adenosine short acting agent given IV for AV nodal arrhythmias

spironolactone potassium sparing diuretic

spironolactone aldosterone antagonist

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spironolactone functions at the collecting tubule

nitroprusside stimulates guanyl cyclase

nitroprusside increases cGMP in vascular smooth muscle

minoxidil direct-acting vasodilator

minoxidil used topically bc of benefit of hypertrichosis

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cholestyramine bind bile acids to prevent enterohepatic recycling

fexofenadine nonsedating antihistaminic

loratadine nonsedating antihistaminic

ipratropium dry mouth side effect

ipratropium antimuscarinic for COPD and asthma

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salmeterol may cause tremors and arrhythmias

theophylline methylxanthine used for asthma

theophylline inhibits phosphodiesterase

theophylline inhibits conversion of cAMP to AMP

octreotide used to treat carcinoid, gastrinoma, somatotropic pituitary adenoma

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propylthiouracil inhibits iodination step of thyroid hormone synthesis

methimazole same as PTU but crosses placenta and enters breast milk

raloxifeneestrogen partial

agonist

raloxifene does not increase the risk of endometrial cancer

tamoxifen increases risk of endometrial cancer

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repagliniderapid onset sulfonylurea

repaglinide binds potassium channels to facilitate insulin release

glitazones increase insulin sensitivity

glitazones stimulate PPAR-gamma receptor

troglitazone hepatotoxic

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sulfonylureas stimulate closure of potassium channels

sulfonylureas glyburide and glipizide

sulfonylureas cause release of preformed insulin

acyclovir used to treat herpes

acyclovir guanosine analog

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acyclovir activated by thymidine kinase of the virus it treats

acyclovir functions as a chain terminator when incorporated into viral DNA

amantadine prophylaxis against influenza A and rubella

amantidine inhibits fusion of viral particles within endosome of the cell

amantidine not effective against influenza B

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amantidine binds to M2 protein

amphotericin B disrupts fungal membranes by binding ergosterol

mifepristone blocks binding of progesterone to cytoplasmic receptors

ampicillin extended spectrum penicillin used to treat gram negatives

aztreonam b-lactamase resistant monobactam

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aztreonam used only with aminoglycosides against gram negative rods

aztreonam cannot be used against gram positives or anaerobic bacteria

bacitraicin inhibits bacterial cell wall synthesis

piperacillin used against enterobacter and pseudomonas

carbenicillin used against enterobacter and pseudomonas

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ticarcillin used against enterobacter and pseudomonas

ceftriaxone used for septic meningitis

cefiximeused to treat gonnorhea

chloramphenicol gray baby syndrome in babies deficient in hepatic gluconosyltransferase

chloramphenicol aplastic anemia

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fludrocortisone used in postadrenalectomy therapy

chloroquine primary drug for acute malaria

chloroquine disrupts hemoglobin breakdown, with toxic accumulation of heme in RBC

clavulanic acidbeta lactamase

inhibitor

sulbactambeta lactamase

inhibitor

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tazobactambeta lactamase

inhibitor

clindamycin bacteriostatic at the 50s ribosome

clindamycintreatment of bacteroides

didanosine (ddI) dose-limiting pancreatitis

lamivudine inhibits reverse transcriptase of hepatitis B

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erythromycin bacteriostatic inhibitor of 50s

erythromycin macrolide

azithromycin macrolide

clarithromycin macrolide

erythromycin GI irritation and acute cholestatic hepatitis

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metformin biguanide compound

metformin increases peripheral glycolysis

clomiphene blocks negative feedback at the pituitary

cosyntropin used for diagnosis of addison's disease

danazol inhibitor of p450

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danazol used for endometriosis and fibrocystic disease of the breast

desmopressin selective V2 agonist

vasopression V1 and V2 agonist

vasopressin used to treat esophageal varices

DES clear cell carcinoma of the vagina in daughters

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ethinyl estradiol/mestranol lowers risk of coronary disease, slows osteoporosis, ameliorates hot flashes

HRT increased risk of breast and ovarian cancer

zileutin inhibits leukotriene synthesis

monteleukastLTD4 and LTE4

antagonist

acarbose inhibits a-galactosidase

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bisphosphonates esophageal ulcerations

bromocriptine used to treat hyperprolactinemia due to pituitary adenoma

bromocriptine ergot alkaloid

diphenoxylate suppress GI motility

loperamide suppress GI motility

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cisapride stimulates peristalsis by release of Ach from myenteric plexus

cisapride long QT

magnesium hydroxide laxative antacid

aluminum hydroxide constipating antacid

ipecac syrup acts to stimulate chemoreceptor trigger zone of the medulla

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cimetidine gynecomastia and galactorrhea

cimetidine p450 inhibitor

calcium carbonate hypercalcemic alkalosis

calcium carbonate renal calculi

bismuth subsalicylate used with metronidazole and tetracycline for PUD caused by h.pylori

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warfarin interferes with vitamin K dependent clotting factors

alteplase converts fibrin-bound plasminogen to plasmin

ticlopidine platelet antiaggregant

ticlopidine interferes with binding of fibrin to Gp2b/3a receptor on platelets

streptokinase catalyzes conversion of plasminogen to plasmin

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fluconazole inhibits formation of ergosterol

fluconazole prophylaxis against cryptococcus neoformans

fluconazole used to treat oral candidiasis

fluoroquinolones bactericidal inhibitor of DNA gyrase

fluoroquinolones used for gram negative rods, some gram positives, and neisseria

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fluoroquinolones bad for cartilage

sargramostim recombinant GM-CSF

filgrastim G-CSF

hydroxyurea used for sickle cell crisis

hydroxyurea increases levels of HbF

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hydroxyurea inhbits DNA synthesis by blocking conversion of ribonucleotides to deoxyribonucleotides

foscarnet treats CMV

foscarnet inhibits viral DNA polymerase

ganciclovir metabolized by viral transferases

ganciclovir requires phosphorylation by viral kinases to work

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ganciclovir guanosine analog converted by CMV to triphosphorylated form

ganciclovir SE: neutropenia, leukopenia, thrombocytopenia

griseofulvin keratinized tissue

griseofulvin ringworm

griseofulvin binds tubulin

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carbapenem given with cliastatin

carbapenem used against gram positive cocci, gram negative rods, and anaerobes

ritonavir inhibit protease in the HIV pol gene

isoniazid inhibits synthesis of mycolic acid

isoniazid SE neuritis and hepatitis

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ethambutol TB

pyrazinamide TB

rifampin TB

streptomycin TB

sulfonamides stevens-johnson

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ethosuxamide stevens-johnson

lamotrigine stevens-johnson

penicillins erythema multiforme

barbiturates erythema multiforme

salicylates erythema multiforme

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hydantoins erythema multiforme

antimalarials erythema multiforme

sulfonamides G6PDH

isoniazid G6PDH

primaquine G6PDH

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tetracycline photosensitivity

amiodarone photosensitivity

sulfonamides photosensitivity

bethanechol muscarinic agonist

carbachol nicotinic and muscarinic agonist

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ephedrine ma-huang

phenoxybenzamine adrenergic antagonist (alpha receptors)

phentolamine used in diagnosing pheochromocytoma

ivermectin onchocera volvulus and strongyloides stercoralis

ivermectin increases GABA transmission in the worm

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ketoconazole interfere with fungal cell wall synthesis

pilocarpine treatment of glaucoma

pilocarpine muscarinic agonist

prazosin first dose syncope

prazosin miosis

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pyridostigmine used for tubocurarine toxicity

scopolamine competitive cholinergic antagonist used for motion sickness

succinylcholine muscle relaxant

succinylcholine nicotinic agonist that opens sodium channels

tubocurarine nondepolarizing neuromuscular ganglionic blockers

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acetazolamide inhibits carbonic anhydrase in the proximal convoluted tubule

acetazolamide metabolic acidosis

acetazolamide give to alkalinize the urine in aspirin toxicity

amiloride block sodium channels in the cortical collecting tubules

amiloride hyperkalemic metabolic acidosis

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captopril inhibit breakdown of bradykinin

ketamine should be given with benzodiazepines

gabapentin partial seizures

ethosuxamide inhbits T-type calcium channels

entacapone inhibits conversion of levodopa to 3-0-methyldopa

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HCTZ hypokalemia, alkalosis, hyperuricemia, hyperlipidemia

captopril functions at the collecting tubules

losartan functions at the collecting tubules

losartan CI in pregnancy

captopril CI in pregnancy