Sotc: This material is cop?righted. - 4 1 rights reserved. Edward Goljan. M.D.

2002

HIGH YIELD NOTES PHARMACOLOGY @

I\Hopurinol: lnhiblts santhine oxidase

Isoniazid: causes pyridoxine deficiency lead~ngto peripheral neuropath)' and sideroblastic
mem;a. 110X- P.H is nicotinic acid derivative that rnhibits synthesis of mycoIlc acid m
rnycobacteria ccIl m~all
Succinylcholine: depoiarizing agent used as muscle relaxanr dunng surgery. binds to niconn~c
receptors In skeletal muscle causing persistent depolarization at motor end-platc. hydrolyes
plasma cholmesterase. inir~alfasciculatlons followed by muscle paralysis. duration of ac t ~ o n
only 3-10 min. m effects not reversed by cholinesterase inhibitors- no pharmacolo~~c antidote to
overdose. * some patients have atypical cholinesterasc and cannot metabolize the drug
Pregangiionic neurotransmitter acetylcholine: activates muscanmz and nicottnic receptors.
nuscannlc effects- * pupillary miosis (contracts ~rissphincte;. used after cataract surge?). *
accommodation of I a s for near l-islon (contracts ciliary muscles). bronchocons~ctor.* slow heart
rate (5.4 node effect). * increase PR interval (.4V node effect). * stimulate GI secretions. -
Increases GI motility (entcric nervous system stimularion), * mlcturitron (stimulate denvsor m s c l e .
xvh~chrelaxes internal sphincter of bladder)
Xitric oxide: potent vasodilator sqnthesized m endothelial cells. activates c ~ c l i cGMP. x h l c h
inactivates myosin lrght chain kinase in smooth muscle celIs Iead~ngro vasodilatat~on. lZch car:
lead to ~ t synthesis
s when injected into vessels
Woman in third trimester has premature contractions: use terbutaline. a seIective P7-adrenergli.
reccpror agonist that inhrbirs uterine contractions
Effect of aspirin on kidney: decrease PGE2 synthesis (vasodilator) leading to unopposed AT TI
effect. renal pap ilia^ necrosis
Methotrexate: blocks dihydrofolate reductase- macrocyrrc anemia due to folate deficiency. S
~ h a s e~nhibitnr. leucovorin rescue, interstitial fibrosis in lungs
Peripheral neuropathy and cancer drug: vincristine
Serve-ending locations affected by botulinum poison, reserpine, guanethidine
510.4 of sucralfate: viscous polqmcr of sucrose octasul fate - aluminum hydroxide tna; adhzrcs
to ulcer crater. stimulates PGE: in mucous cells- responsl'cle for mucous barrier
Effect of mixing statin drugs with niacin: rhabdornyolysis- each drug by Itself can produce
rhabdomyolysls
510.4 of amphotericin R: binds ergosterol ir, fungal cell membrane. uhlch increases Its
permeabili~. nystarin has same mechanism
Yl.10.4 of clotrimaxole: inhibits ergosterol synthesis. other azole compounds have sinliar actlo?.
410.4 of flucytosine: inhibits nucle~cacid s*vnthes~s
lCIOA of griseofulvin: inhlbits microtubule function and mitosis
Knot\- the definitions for potenc! and efficacy of drug
Propylthiouracil: drug of choice for decreasing synthesis of t h ~ o l dhormone in Graves d~sease.
agi-anulocytons. only dims that can be used in preFancy
Fastest wa! to increase heartbeat in shock: order of drugs with decreasing effectlvcness is
~soproterenol.dohutamme. and dopamine. dopamine in low doses is best for renal vasodilatation
Ljapsone: sulfone that Inhibits synthesrs of folic acid by ;.M. leprat.. rr,a>- precipltatt: hemoi>::c
znernla In CXPD deficiency. ma!: produce methemo~lobrnerr,l2. ncpnrotlc s?ndrornc.
prr:pheral neuropathy
Prolongation of QRS on ECG: qulnidinc
\ate: This material is copyrighted. . i l l rights reserved. Edward Goljan. \I.D. 2002

AnticonvulsantlantiepiIeptic drug with effect on epiphyseal plate: phenb~oinvra its re\x'rng up

of the cytochromc system m the liver and causing vitarnln D deficiency- increased rnctaboilsm of
25 h?,droxylated vitamm D
510.4 of ondansetron: selectii-e serotoriin 5-HT3 rcceptor antagonist, useful In biock~cy
chemorcccp~orrrrgger zone (CTZ) In the area postrema, hence prevcntlng vomiting
Opioid overdose: respiratory depression- respiratory acidosis. miotic pupils
First RYof alcoholic in ER: give XL' th~amlneto prevent acute Wernickz's encephaiopathy
Heparin: MCC: of thrombocytopenia in hospital
.Acute Rs for coumarin overdose when bleeding is life-threatening: fresh frozen plasma S c j i
choicc. use 1M . xitamm K for less serious bleeds
Sitrofurantoin: concentrated in urine. unnary r a c t antiseptic
C'yclophosphamide: hemorrhagic cystias. transitional ccll carcmomz. actrvxtd ( n o t
merabolized) In the Iiver
Doxoruhicin and prednisone: metabolized in liver
Gout after cancer therapy: prevent by grling allopunnol (xanthine oxldase ~nhlbitor). dangcr
of urate nephropathy
Given log dose curve for 2 drugs and must compare efficacy and potency
Muscle fasciculations after neuromuscular block: lnirial effect of succinylcholice
310A of levodopa: blocks pcnpheral dopa decarboxylase
Bronchial asthma: albuterol medihaler most often uscd for mrld to moderate asthrnz.
corticostcro~dmedihaler used for screre asthma
Rs of parox?-smal supraventricular tachycardia: adenosine. includmg its association W I L \i-Pki-
~
sqndrome
4 1 0 A of clonidine: activates a?-adrenerglc and imidazole receptors in the central nervous sys:cm
u h c h reduces s~mpathetlcoutflolv from the vasomotor center in the medulla
Captopril: bradykinin slde-effects include cough and angioedema- ACE normail? aegmd?.;
bradq-kinin. cough not seen with losartan
Hydralazine: better toIcrated In fast acetylators. cause of drug-induced SLE. csn bbe u 5 e i :n
hq-pcnension In pregnancy
Patient with hypertension. hypernatremia and hypolialernia: losanan. an AT11 receptor
antagonlsr. 1s the best drug. 4 corrects FITS and electrolyte problem {hiocks rtrlcasu of aldostrrocc..
Yence sodium 1s lost in he unne and potassium retained)
Rx of pulmonary edema: loop diuretic is very useful- decreases preload
Rx of opioid overdose: naloxone. u*hichis a competltlr-e oplold receptor antagonist
I-rinary retention in prostate h),perplasia: use selective a;-blockers- relax smooth musi.:c :n
'>ladder neck ar.d prostate. examples- * prazosln. * terazosin
110.iof saw palmetto: anti-androgen effect- blocks androgen uptakc and a ~ * a l l a b i l n:;.rloci
~b
altenng serum l e ~ ~ e i s causes
. shrinking of transit~onalzone of prosrare around the urethra
harcolepsy: Ru with amphcramlnes
Premature labor and must deliver baby: give glucocortlcoids to increase surfactant S ~ T I E ~ C S I ~
Interpret dose/responsc curves and whether antagonist is competitive and non-competitive
Drug used to eliminate caIcium in patient with hvpercalcemia: loop druretlc
Drug uscd to remove calcium from urine in a calcium stone former: hydrochlorothiaziiic.
Patient with respiratory alkalosis and then metabolic acidosis: saLlcy!ate ~ntoxiczaor:
S-phase drug used in treatment of acute lymphoblastic leukemia: mct:?o:re?;ate
Analog of hypoxanthine requiring HGPRTase f o r bioactivation: 6-merca?io?cr:nc.
,j;opurinol could cacse ;O.;ICIQ-, since the drug I S a purine
f)rug that competes with dl,->IP for thymidylate synthase: 5-fluorocurac il
Drug used in Rx of W'iirn's tumor: actmomycin D (dactlnomycin)
3otc.: This material is copyrighted. All rights resewed. Edward Goljan, S1.D. 2001

Antimetabolite that together with an antibiotic is used in Rx of acute mq-elogenous leukemia:

cytarabine - daunomycin (anthracycline antibiotic)
Sephron site responsible for ACE inhibitors causing increase in serum creatinine: block rn A l '
I1 (\vt.orks as \.asoconstnctor of efferent anenole in glomerulus) by ACE ~ n h l b ~ t orcmovcs
r
~m?onant control for rnaintainrng intrarenal blood flow causing potenrial for renal fa~lure
(partlcuiarly with bllatcrai renal arteT stenosis)
Xephron site of action of thiazides: Xa.!Cl' pump in cortical thlck ascending 11mb
Vitamin given in Rs of TB: * pyridoxine (B6)- used up when usmg rsoniaz~d, rlsk of pzr~pheral
neuropathy and sidcroblastic anemia
Drugs that are generali~safe in pregnancy: safe- * methyldopa. * hydralazine, * la\\-doscs or'
~rop\..lthiouracil.* cephaIosporins. penicillin. not safe- * methotrexate, * ACE ~nhlbjtor.
-+

rettnoic: acid. * sulfur containing drugs

-
j 1 . h ~is gtntamicin ineffective in Legionella infections: arnlnoglycosldcs affect thr 30s
ribosomal subunlt. resistance to any drugs that are protein synthesis lnhibltors may be due to- *
inactivat~onof the drug by bacrerial enqmes. * decreased uptake of drugs vla porlns In bactcrlal
membranes. * decreased binding of drug to 30s ribosomal subunit
Classic ECG changes for cardiovascular drugs: prolonged QKS with qumldine, am~odarone.
prolonged QT interval xvith sotalol. amiodarone, prolonged PK intenal w ~ t hdlgltalls. 0-
blockers. calc~urnchannel blockers, giant U u,ave with qulnidine. ST depression with dlgltaI~s
(hockey stlck configurat~on),quinidine. short QT intenal with digitahs, flat T wa\.e n . ~ t h
qumldme, bradycard~a~ 1 1 t quinidine
h
Know mechanisms for resistance to various classes of antibiotics: note thc ones above for 30s
protein sqnthes~sinhibitors- * tetracyclines, * aminoglycosides. * spectinomycin
Patient with Salmonella and G6PD deficiency: avoid TMP!SMX. (suifur drug)
410X of disulfiram reaction with metronidazole: inhibits aldehyde dehydro,Oenase
310.4 of norflaxacin: inhibits DKA 3-ase
Avoid tetracvcline in pregnancy
YlOA of erythrom?;cin: mhibits 50s ribosomal subun~tin bactenal proteln sqnthesis. also othc:
rnaurol~des. chloramphenicol, clindamycm
Chloramphenicol: aplast~canemia in adults- idiosyncratic, not dose dependent a s it 1s In newborns
(graqr baby syndrome)
Know blockers for different acetylcholine receptors
Child eats honey and gets weak: botuljsm. intestinal coIonization of organism wltk toxin
production- toxln blocks thc release of Ach
.Antihypertensives increasing blood lipids: P-blockers, th~azides
3IOA of trimethoprim: blocks dihq~drofolatereductase
Muscle relaxant for electroconvulsive Rx: succinylcholine
Rx of prostate cancer: leuprolide- GnRH agonist blocks FSH and LH and lowers testosterone
and DHT. ilutamlde- comperes with testosterone for androgen receptor. * finasreride- * blocks
-a-reauczase. * decreases DHT. * increases testosterone (good for prevennng impotency ar?d ha~r
gou-th). * malnly used in prostate hyperplasia. * ketoconazole- * rcducc testosterone s!-nthes~s. *
more often used in hyperplasia
Young woman with vaginal cytoloo,~~ containing malignant cells: DES fxposurc with clear csi:
adenocarcinoma
C33\' infection: ganc~clovlrfirst. then foscarnet if it does not work
>lost common side-effcct of immunosuppressant drugs: w infect:on. squamous csnocr or skln
UC cancer
Rx o f absencc seizures: * ethosuxz.;lmrde
5ote: This marerial is copyrighted. All rights reserved. Edward Goljan. .\l.l).
2002

EEG in patient with absence seizures: shows 3!scc spike and waL,e d~scharee. increased 1~1th
h>?rn-cn trlat102
Drug abuser with flu-like syndrome, fever, rnydriasis: mehadone naloxone -
Patient \\ ith polyuria, polydipsia: taking lithium- produces nephrogenic dlabetcs lnsipldus
Rx of .ADH1): methylphenidate
Kx of depression: trlcycl~canridepressants- clomipnmine blocks ncuronal reuptake of NOK i-2 i
and serotonm ( - 3 )
Phcnytoin interaction with theophylline: phenyloin revs up cqtochromc sy srem and :ncreases
metab01 ism of theophylline
Effect of chronic use of a hypnotic drug to induce sleep: psycholoyic dependence
Patient with M'egener's granulomatosis has hemorrhagic cystitis: cyclophospham!dc c'5-ec:
ti, is the active form of vitamin K
Patient with h!-pertension has SLE-like syndrome: hydralazine
\-asoconstrictors that increases IP3:drugs activating u I -adrenergic receptors
Know drugs that have their effects on pacemaker action potentials
Know mechanisms of action at receptors (adrenergic, cholinergic, hypothalamic releasing
factors. histamine, VIP):e.g.. CAMP,TP3/diacyclglycerol. etc.
Iron poisoning in child: biggest concern I S hemorrhagic g a s ~ i t i sand liver necrosls
Keceptors. mechanisms of transduction. neuronaI tracts, functions: u l . u?. p l . 02. D
Qpes for doparnlne. GABA. histamine, 5-HT types for serotonm. muscarinic. nlcotlnlc.
SO. uploid receptors- &. K, u
Ring finger with blue discoloration on undersurface and Hx of drug abuse and frequent
sexual activi5: n' heroin abuser using finger as site of injection that rs selling sex for d r u g
Gold salts: used in Rx of rheumatoid arthritis. oral drug called auranotin, parenteral form
called gold sodium thiomalate, rakes 3-6 mths before effects are noticed. compilcat~ons- *
polentraIlq- fatal dematitisistomatitis common. * hone marrow depression. * flushicg. -
h?-po?cnsron, * tachycardia. * renal disease
Hydros~chloroquine: used In Rx of rhcumatold arthnrrs. complicat~ons- - rct:r,a:
dsgenerat~on.* dermatitis. * bone marrow depression
Penicillamine: used in l b of rheumatoid arthritis. cornpllcations- * aplastic anemla. renal
damage (membranous glornwulonephntis)
-
PenicilIin MOA: p-lactarn antibiotic- cell wall synthesis inhibitor. binds to receptors 12
bacterial cytoplasmic membrane. inhibits transpeptidase enzl;mes thar cross-link peptldogl>can
chains m bacterial cell wall, + activates autolq-tic enzymes in bacterial cell xvall
ChIoramphenicol MOA: inhibirs bacterial protein s_vnthens. binds ro 50s ribosomal s u b ~ r : : ~ .
hence indirtrcti> ~nhibitinctranspept~dationby peptidyltransferase
Mesna: rr,srcaptoethant.sulfonate, reduces incidence of hzmorrhagrc cystirrs associated L L I ~ ~

ch-clophospharnide by reducing formation of acroleln

Ribavirin 510.4: inhibits panosine triphosphate formation. xvhjch prevents cappln? u i 1,1731
d S . 4 . b l o c k KYA-dependent RN.4 polqmerases. used In Rrc of RSI' infcct~ons
Ondansetron JIOA: 5-HT; receptor blocker- central antemetic
Know pharmacolrinetics: half-life, volume of distribution. marntenance dose
.~rninoglycosides: affecr 30s ribosomal subunit in bacterial prore~nsyntnesis. neph;ntoxlc aoC
ototosic. MCC of drug-induced ~ephrotoxinacute tubular necrosis. ototoxlc~tyreiztcc t c
accumulation :n labyrinth and h a ~ rcells of cochlea, vestibular s ~ ~ s ~ s y ~ ~ p t *o nystaFrn.;s.
rns- *
d17.7.incss.* 1.2rt1~0.* S.V.cochlear sl~mslsqmptoms-* tinnitus. * scnsonneural heanng 105s
H. pj*fori Kx- amoxiclllin :clarithromycln - protor, pump blocker. ?rcventlon-- proton pump
'nlockcr - blsmuth
Sore: This material is copyrighted. .Ail rights reserved. Edward Goljan. M.D. 2002

.Antifungal drug destroying fungal cell membranes: p o l ~ e n e slike amphotcncln B- * polyrncs

31nd to ergosterol in cell membrane and cause formation of artificial pores In the membrane, *
roxlclc of amphotericin: distal RTA with magnesium and potassium u-asting. azoles block
s!mtkes~s of er~osterolin cell membrane. flucj~osineblocks nucleic acid s4mrhesis. ~seofu11-rn
dlsxpts mlcrotubules
Aikylating agents 410~:alkylate DKA. RN.4. other protcms. Ieads to breakage of DS.4
strands and cross-linking u-hlch lnhiblts strand replication
tXlrIG-CoA reductase inhibitors: statin drugs block CH synthesis, * hcpatocytes compensate b>-
up-resulation of LDL receptor synthesis leading to increased clearance of LDL and LDL remnsnts
derived from VLDL
Sildenafil: drug for R s of erectile dysfunction. inhibits breakdo~wof cGMP by tqps 5
phosphodiestzrase- increases levels of cGMP, uhlch causes vasodilzration in corpus cavcrnosu?
and penls. should not receive nitroglycerin. since ~t causes release of n i m c oxldc (,potent
b,asod~lator).which elevates levels of cGMP
Yitroglycerin MOA: rdease nitric oxide (vasodilator) in cndothehal cells. prlmaril>- a
\.enodllator- causes venous pooling and reduces preload, has some arterial vasodilatatron ivhm
admlnlstered TV- reduces afterload, uses- * angina, * acute myocardial infarction
Sitroprusside 310.4: r used in h-vpertensivc emergencies and in dissecting aontc aneuysms.
merabollzcd to cbpanide in RjBCs- cyanide converted to thlocyanate, must mcasurs Itveis of
thlocyanate dunng Rx ro avoid toxictt)?
fhentolaminc: nonselective a-adrenerglc receptor antagonist- competitive receptor antagonist.
produces \,asodilatation- reduces TPR and blood pressure. reverses effects of epinephr~~c.
cl~nicaiuses- * hypertensive ep~sodesdue to pheochromocj.toma. * reversal of effects of accldcntal
injccrlon of epinephrine in subcutaneous tissue
Yaproxen: newer. long-acting %SAD that blocks cyclooxygenase. ve;er\.-signi ficam potentla!
fo: rcnal darnaze in those u-rth preexrsting renal disease
Doxorubicin: antibiotic. MOA- * intercalate base pairs. * interact with topolsumerast 11. *
generate frec radicals. * block synthesis of DXA!RUA and cause DN.4 strand sc~ss:on. s ~ d z
effects- * dosz-dependent congestive cardiomyopathy via f f e e radical damagc. * rnarrou-
suppression. dexrazoxane, a FR scavenger. may protect against cardiotoxicih.
M A 0 inhibitor used in treating a patient with resting tremor: seiegilice. r blocks M0.4tqpe
B. xxhlch normally metabolizes dopamine. so brain levels increase. hepatlc metabolism produces
amphetamine
Danrrolene \ I O A : blocks calcium release from sarcoplasmic reticulum of skelcta! mucc\e.
D0:I In RTof malignant hqperthermla: used in RYof muscle spasms in cerebral palsy
Digitalis: blocks N a X - ATPase pump in cardiac muscle- 3 Na' Into muscle and 2 Ii- ou: of
rnuscrc
Antihypertensive with Coombs positive hernoiytic anemia: methq,ldopa. alters Rh arttlgcns
on surface of so lgG autoantibodies rcacr against it. type TI hypersensitivl~
Know different insulin preparations and times of onset of activie
Fluoroquinolone MOA: blocks bacterial Dh'A synthesis by inhibltrng toporsomerasc II (I3X:l
~ ~ a sandc )ropolsornerasz n'. * DXA s-rase important in relaxation of superco~ledDS.4 I ~ oix
L e2
in normal trznscnptlon and duplicat~on. Qpc W topoisomerase IrnFortant In szparztloz o:'
re?iicared chromosomal DNA durins cell division
Benzodiazcpines: retrogade amnesia
Prop?;lthiouraciI JIOA: reduces lodination of ~ ~ o s i n r reduces
. coupling of MIT and DIT :o
forrr, T: and T:. inhibits peripheral conversion of T: to T , by inhib~tingthe outer rlng 5 ' -
Cciodinase. sldc-effects- rash. aganulocq-tosis
Uure: This material i s copyrighted. All rights reserved. Edward Goljan. 41.D. 2002

Drug Iowering HDL: probucol. may cause torsade de pointes- * var~ation of QRS
config~rat~on. * type of polqmorphic venrrrcuiar tachycardia. may prolong QT ~ n t e n a l
Drugs causing torsade de pointes: drugs that slow \*enrrlcular repoiarlzatlon and prolong C)1-
:ztcr\ a!- * quin~d~ne, * sotalol. * phenothiazines. * cisapride
J1O.A inhibitor associations: inhibit M.40 type -4(metabolizes XOR. seroronin. ~ ~ a r n ~and nc?
L3 ( rnctahollzes dopamine). hqperrensive reactions if taking foods w ~ t hlyrarnine- * b>product of
F'oslne metaboiism. * bananas. * ferrncnted products Iike cheese, becr. u-lne. *- sqmpathomrmct~c
reacI1on in that ~t causes the release of stored catecholamines lead~ng to h>pcrtensioc.
acml~isteredwith fluoxetinc ( SSRI) produces serotonin syndrome- * hqpcnhennlz. * myoc ionus
({allure to rclar: muscle)
Stage fright!test anxiec: sive propranolol
HI antagonists for Rs of bay-fever
p-2 agonists: actlvatc adenylate cyclase to increase c..ZMP
Bronchial asthma: zileuton- mhibits 5-lipoxygenase. zafirlukast and montelukasi block
leukotrienc receptors
51CIO.A of methadone: Rx of opiold abuse, sahirates CSS opiate receptors
Receptor involved in tardive dyskinesia: D2
Phencyclidine t o b c i e : angel dust, reacts with opioid-like sigma receptors and s u b ~ ~ of es
g!utarnate receptors, dissociative anesthesia- e.g., loss of sensarlon in lower Ilrnbs.
aglta:ion,violent behavior- cannot hold patient doun
.4cyclovir 5 I O A : 9uanoslne analog that is activated to form acyclovir tnphosphatc a cornpcr~t~r-e
5-bstrate for DNA polymer~se- subsequent cham termination following incorporation into viral
DNA. clmical uses- varicella~zostervirus. rnucocutaneous::' semral herpes
Girl on rifampin becomes pregnant while on birth control pills: rifarnpin revs up thc 11ver
ck~ochromesystem (like alcohol, barbiturates. phenytoin) and caused increased metabolism of hlnb.
contro! pills
Antagonist of al-blocker: a1 -agonist like pscudoephednne
C:omplications o f thiazides: hqponatrerma. h~pokalemlz. metabolic alkalosls.
hqperuncemra. h>-perglycem~a. hypercalccmia- thiazides are used m the Kx of caic~urns:or,c
tbmer5 o u m g to increased reabsorption of calcium out of rhe urine
ACE inhibitor effect on plasma renin activity: increases due ro decrease in AT 11 and aldo:+zone
Drugs affecting tubulin in mitotic phase: vrnca alkaloids. paclltaxel
Rx of benzodiazepam overdose: flumazenil
1-se of aqueous epinephrine in shock: 1: I000 dilution subcutancousl~~
Dantrolene: used in the treatment of malrFant hyperthemla post halothanr exposure
Treatment of acetaminophen overdose: aceqlcysternc to replace used up GSH- neutrairzer
acetammopher. free radicals formed in the liver cytochrome system
M 0 . A of Ioop diuretic: blocks NaT-K--2CI-cotransport pump in the thick ascending 1:mb ~r.thc
rece j rnedu1la. also blocks calcium reabsorption- used in the Rx of h?.percalcem;a
Cyanide poisoning treatment: amyl nitrite is firsr adrninrsrered to produce methemo~Io5ln.
u i c h cornblnes with cyanide to form cyanmethemoglobin. rhlosulfatz :s added and cornpu1c.s
lv1:t. mcthemoglobin for cyanide to form thlocyanate. ~vhlchI S excreted
Thrush: may bc a complication of a cort~costeroidlnhalzr
Isotrerinoin: aiivaq-s order a prewwcy test in females, put paticnts or, BC'P
51012 of prop~lthiouracil:a blocks iodrnation of the tyrosine residues o f th>~vglobul~n.aijo
Slocks coupilng of DI?' and MTT. only drug that can be used in pregnancy (low doscsi but ma>-
produce yorter ;n the newborn and nail defects
P450 system in the liver: makes drugs water soluble
Angioedema and renal failure: ACE lnhibltor relatlonskp
Yote: This material is copyrighted. All rights reserved. Edward Goljan. 3l.D. 2002

3 310.3. of retinoic acid: bchar-es like a sreroid in that ~t blnds to receptors in the nucleus 1 ~ 1 t h
subsequcnr uanscrrptlon of genes, proteins produced by t h ~ sactlon are important m growth.
d fferentiation. reproduction, and embryonic development. also used in ueatment of acute
?roganuloc~ticleukemia. where ~tIncreases the rnaturatlon of the blasts
Allopurinol action in purine synthesis: blocks xanthins oxidasc- schematic of punnc
xctabollsm x a s provrded and had to identify- the reacrions hqpoxanthine to xanrhine and xanthlnc
to ur:c acrd. mzrcaptopurine degadation I S inhibited as well
'Ilost common antibiotic used to prevent endocarditis in patients with valvular diseasc:
arnoxicill~n is the drug of cholce. a11 valvular diseases except asyrnptornatlc MVP and a11
congenital heart disease except asynvtomatic ASD
Yellow coloration of the skin that can be mistaken for jaundice-? drug: qumacnnz.
chlorpromazinc and arsenic produce a blue-gay color to the skin
Diffuse erythema followed by separation of the skin (scalded skin syndrome o r toxic
epidermal necrolysisj--?drug: barbiturates, sulfonamrdes, phsnytoin. NS.AHls
Hair loss in a woman--?drug: r oral contraceptives- predictable side effect, e s r r o p causes hair
:o be a: same stage of development, may aIso occur after deliveq,
Erythematous, hyperpigmented plaque-like lesion that recurs at the same site ever) time:
fixeC drug eruption- * phenolphthalein. * NSADs, * teracycline. * Bactrirn. * barblturatcs
Group of drugs bas the highest association with urticaria1 and maculopapular lesions:
amox~cillin. T,W!SMX. ampicillinipenlciilin. rashes are the MC adverse rcacrion to drugs.
x;th macuIopapular rashes leading the Iist, most drug reactions involving s k ~ nare not QTe I
h>persensin\rn. hlstarnine-related. however, those involving penrcilIin arc usually t!pe I
h>persenslti\lh.
Elderly woman on thiazides is most at risk for developing?: gout
Tardive dyskinesia, malignant syndrome (sweating, hyperpyrexia. autonomic instabilit?):
ncurolcptics
Antips?,chotic drug requiring visual examination: throridazine- also produces heart conduc tlon
dcfects
Sephrogenic diabetes insipidus--? drug: lithium for b~polardis:urbances
Drug contraindicated w-ith 31-40 inhibitors: epinephne
Use of phentolarnine: non-selective a-blocker hat lowers blood pressure d u n g surge? for a
pheochromocqtoma
MOA of AZT: inhiblts reverse transcriptase, produces a macrocytic anemia uEela:ed ro
folatr £3 i 7 . lnitral dm5 regimen used in F b of HIV- 3 nucleoside analogs jc.g., ?LZT, lam11 cdinc)
- 1 protcase ~nhlbltor(e.g.. indma~qr)
Tests to monitor Rx of HJV: HW KXA by polyrr~erasechain reaction (PCK)- * monitors \,Ira;
'nureen durlng. * best test. CD, T helper count- * immune status. * prophylaxis marker
510.4 of nucleoside drugs: block reverse transcnptasc
J10.4 of protease inhibitors: suppress HIV replication by blocking protein processing later In [he
HI\' cycle
310.4 of nonnucleoside reverse transcriptase inhibitors: non-compenrively lnhibl; revcrw
mnscrlptase- e .g.. nevirapine
Side-effects of didanosine: pancrearitis, hepatitis. peripheral neuropathy
Side-effects of lamivudine (3TC): rash, r peripheral neuropathy. b o ~ marrow e toxiclb
Side effects of indinarir: protease inhibrtor associated with renal stones
Side-effect of non-nucleoside reverse transcriptase inhibitors: rash
C:D, helper T cell count for prophylaxis against PCP: <ZOO ce1ls:'uL- Rx with TXTP.SUN
CD, helper T cell count for prophylaxis against toxoplasmosis: <I00 celIs,uL- Ks ~-111!
ThIP,SL?X
h o t e : This material iq copyrighted. All rights reserved. Edward Goljan. XI-D. 2002

CD, helpcr T cell count for prophylaxis against 51.41: <50-100 cells:',uL- E
h with
i.iarlt'nr~rxycln
of Pb poisoning: BAL and EDTA
R\;
Drugs involved in foIate metabolism: phen!qoin blocks intestma1 conju_gase- pol)-zlurarnate :o
~ o n o s i c t a m a ~ r . BCP and alcohol block uptakc of monoglutamatc In rhc jejunfin.
methutrusate 'TMP-SMX block dihydrofolate reductase
Cromolyn sodium: stabilizes mast ceil mernbranc preventing release of preformed med~atorsand
rtlcasc of prostaglandins~leukotrlenesafter the release reaction
3lethotrexate: blocks dihydrofolate reducrase and the conversion of aihydrofolate Ir)
:emah)-drofolate
Cycloosygenase: aspirin mhibits irreversibly. h'S.4lDs reversible
Thrornboxane A?: synthesized in platelet. vasoconstrictor. Increases piatelet a,zrregatlor..
bronchoconstrlcror
310.4 of proton blockers: blocks H--K'-ATPasc proton pump in paneta] ccll- no: a receptor
mcdlated event. useful in the treatment of ZE syndrome. GERD, and H.p ~ l o r ilnfictions
210A of H z blockers: blocks Hz receptor, which normally activates adenylate cyciasz producing
cXSlP which st;mulates proteir! hnase
MOA of acetylcholine: activates cholinergic receptor causing the reizase of calcium. 11-hich
stimulates protein k ~ n a s e
510.S of misoprostol: blocks the prostaglandin receptor, which normally lnh~bitsadenq late q c l a s r
and cL%\lP production
7-fold membrane spanning protein-? drug: propranolol. a non-selective !?-blocker
Phase 3 clinical trials: double blind
Ticlopidine: ,210,4- inhibrts ADP-induced expression of platele: glycoproiein receptors. rs.h~~;":
redcces fibrinogen binding and platelet aggreganon, substitute for aspirin In prevcntmg strokes.
CAD ~fthe patient is allerg~cto aspirin. causes neutropema, prolon~sthe bjeeding t ~ m e
Drug induced SLE: procainamide. hydralazine
Overdose of succinylcholine: use acerylcholine blockers
.ACE inhibitors: lncrcasc in r c n ~ nand AT]. but a decrease in ATII and aldostzrone. aldosieronc
eventualiy mcreases, hence the additlon of spironolactonc ro keep aldosrerone sappressed->
lncreases longerin In CHF
Arsenic poisoning: Rx with dlmercaprol
C:hIoroquine was used in the treatment of malaria and malaria recurred-l~h?;?:
esocr?;tb~ocq.t~c:kepatic stage- e.g., P. vivax. P. ovule. drug h i l s a c m e disease but does 7 0 ;
zradlcate hcparic stage
Primaquine in treatment of malaria: not good in the actlve stage 5ut does k111 thc hcpatlc stagc of
P. vii.a.c and o ~ n l e
Dantrolene: reduccs the release of calcium from the sarcoplasmic retrculun of skeletal musclc.
an~~spasmodlc dm:. also used in treatrng mali-pant h>perthermia
\lethanol: increased anlon gap metabolic acidosis due to conversion of methanol Into formic
aci-2. optlc c e n e degeneration and blindness, treat with alcohol infusior, to block rnc~abol~sm of
mc:hanoi by alcohol dchydro,"enase
Botulism toxin: blocks the releasc of aceplchollne- diagram ma!- bc given of neurotransrnir;er
s must locate the block. used to treat LES spasm in achalasia
5 ~ t h e s i and
Ribavirin: used in s e w r e KSL,' rnfectlons in children
t t u of asthma with albuterol: p2-selective agonist- bronchodilator. albaterol m2> c2uqr
hhpokaizmia- drrves K ' Into cells b!, actlvatlng the -4TPase pump
.4cet?,lcholinebreakdown: occurs in the synapse ~ n t ochoiine and acetate b ~acer);lcholmesterasz
.
: rhe cieft. producrs are recycled and not excreted
This material is copyrighted. All rights reserved. Edward Goljan. 3l.D. 2002

Ketocooazole: inhlbrts the metabolism of nonsedating antihistamines Ilke Seldane leading to

cardlac arrh)zhmlas
Codeine: metabolized into morphlne in small amounts owing to significant first pass mztabohsrn of
morphine m the liver
Delirium trcmens: Rx with benzodlazepines
Lovastatin: Inhibits H3.3G Co.4 reductase
Patent ductus arteriosus: keep open with PGE:
Cephalosporins +- aminoglycosides: synergistic effect of enhancing nephrotox~cq'
Erythromycin: rnteracts with the 50s subunit of bacterial ribosomes leading to inhlbltion of
protein sqnthesls. inhibits the formarion of the initiation complex and interieres 1~-rrhtranslocatlor.
reac:ions. rcslstance develops secondary to plasmid-mediared formallon of enqmes thar
mcthylate the receptor that eq+thromycln binds with, * coli foms produce a transmlssibic plasmld
that produces an estcrase that hydrolyzes the lactone nng of erqthrornycrn
Chlorarnpbenicol: gray baby spdrome- dose related aplastic anemia
TMP: ~ n h ~ b l dihydrofolate
ts -
reductase, plasmid-medlated resistance. TMP SMX has a
sqacrget~c effect from the sequenhal blockade of folatc synthesis. since SMX biocks
dlhydropreratc s)nthase, lvhich is an e n m e that converts paraafinobenzoic acid lnro d~hq,drofollc
acrd
>letronidazole: prod-uces a disul firam-like reaction
FluconazoIe: treatment of esophageal candidiasrs in AIDS
Cholinornimetic used in treating open angle glaucoma: pilocarpine. phvsostlom&
Dobutamine: inotropic (increase conzactility) vasodilator (decreases afierload) r-hat activates a1
and (31 > $32 activity \v.t-lfhout much chronotropic effect. used in the treatment of shock
(cardiogenic) associated wlth hypotension and hypotension associated with renal failure or CHF
Dopamine: stimulates cardlac p l receptors, penpheral a-receptors. and doparnlnerg~creceprors
!n 1-essclsin the renal and splanchnic bed. r at Iow doses. it is pnmanly a vasodilator that iccreases
renal and splanchic blood flou. * at high doses, it increases cardiac contractilrty (motroprc) and
cardlac output vla its activation of cardiac (31 receptors
Benzodiazepines: via 11s own receptors m the thalamus, lrrnblc smcttlres. and cerebral corte.x
w'hich are part of the G . a . 4 receptor-chloride ion channel macromolecular complex.
benzodlazepines facilitate the ~nhibitoryacrron of GA3A via increased conductance ~nthe chlonde
Ion channels. flumazenll blocks thls effect by blochng the receptor for benzodiazepines ar.d is the
treatment of choice for benzodiazepam overdose
An elderly n-oman on thiazides is most at risk for developing?: diabetcs mellrrus
.A child who ingests 30 adult aspirins will most Iikely develop?: an increased anlon gzp
netabollc ac~dosls. children. unlike adults. do not commonll;. develop a rn~xedmetabolic acidoslj
and respiraton a l h l o s ~ s . RY is to perform 5astric la\-age and add act]\-ated charcoai and :o
prodzce an alkaline urrne for rncreased excretion of the acid
Open angle glaucoma is best treated with?: P l and P3 blocicer, tlmorol is a favored ager.t.
pilocarpinc may also be used. open angle glaucoma is the MC tqpe of glaucoma- producc~
l of peripheral v~sion(runnel vision) and optlc atrophq'
~ a a u a loss
Trazodone: second generation anti-depressant, inhibition of seroronin reuptake. sedation.
ma! cause pnapism
I'hioridazine: rctlnlris pigmentosum may be a complrcation
Tamoxifen: ~ e a kestrosen thar acts as an antagonist In breast tissue [esrrogen competes \xlt:1
:arnoxrf'en for blnd~ngto the receptor, and partral agonlst In uterus (can produce endometnal
kxperplas~a). aiso protects against osteoporosis and can be used m women kxho naxe ER,I
pnslt~vcrumors. can be used m treating progestm-resistant endometrlai cancer. comp11cat:or.s.
f7r;shing (rnenopausai symptoms). vag~nalbleeding. potentla1 for endometnal h!~erplasra czncer
\ole: This material is copyrighted. A11 rights reserved. Edward Goljan, %I.D.2002

.Acetaminophen: analgcslc and antipyetic but not an anti-lnflammaton. agent. ~nhrb~ts

prostagland~r;synthesis in the CSS. very \n-eak cyciooxygenase ichbitor. 51C drug causing
zcutc fulminant hepatitis. converted into free radicals ir. the liver- * zlutathione inactivates thf
FRs. * aceclcq-stelne treatment replaces GSH
Digitalis toxicit?,: treat with dlgoxin antibodies ( F a fragments)
Cephalosporins: first generation- drug of choice for surgrcal prophqrlaxis In man! cases.
second sencration- * Rx of sinusitis (cefuroxime), * Rx of mlxed anaerobic infections. thlrd
generation-. * KKof men~ngitls.* Rx of GC and L p e ' s disease: c e f r r ~ a ~ o n e
Clozapine: blocks D;. (dopamine) and 5 - H T I , receptors morcso than D I receptors
Fever in a patient on a loop diuretic: do not use any type of SS.4LD (inc!udln_r asp~n?)s l n z i:
blocks renal sq-nthes~s of prostaglandin. whlch vasodilates thc afferent artenole, xsc
acctamlnophen to lower fever. since 11 does not interfere w ~ t hprostaglandin s!nthesis. loop
d:uretics lead to volume dcpletlon, hence angiotcnsin II will be eievated (vasoconstncts zfferen:
ertcrio1e)- loss of prostaglandin effect predisposes the patlent to renal fallurc
Red man syndrome: IIT vancomycin
Drug for bacterial carrier states (S. aureus, N. meningitidis, H. influenzae): nfampln
Single dose drug for GC and Chlamydia: azrthrornycln
Kx of malignant hypertension: n~troprusside
Antihypertensive and antiarrhymic drug that lowers blood pressure and increases heart rate:
caicium channel blocker- e.3.. nifedipine
Estrogen: llp~deffects- * lowers LDL,WLDL. prevents osteoporosts- ~nhlbirsosteoc!ast
autrvanng factor (a-I) secreted by osteoblasts, thromboeenic- * natural estrogens are less
thrombogmic than sqnthetic estrogens, * increase synthcsls of coagulation factors. * decrrasc
XTUJ. increases lrver sqnthesis of transcortin and thyroid b l n a l n ~~lobulin- increases tot21
con~sol!thyroxine levels without an increase in free homonc, increases hcer s ~ n r h e a sof sex
hormone 4 testosterone or androcen) binding globulin- lowers free res~osterone. cancer risk- -
endometrial. * breast. intrahepatic cholestasis, choleli~hiasis
Oral contraceptives: pill effects- * inhibit LH surge. whlch prcvccts o\ulation. Increase rnaizr
eminencc plymentation- "pregnancy mask". ethinyl estradiol (sqnthctlc tsaogen) mcreases I I \ , ~ :
s\.nthesls of many proteins, 19-nortestosterone (progestational agent) effects- * u z t e r
re:entlon,we~ghrgain. * reduction in estrogen receptor sqnthesis ( a ~ o p n yof endornetnal glands). *
rncrcasc LDL. * decrease HDL. complrcat~ons- * thrombogeclc. i- sr~mulaten-ptophan
metabolism: Iowers serotonin+ depression, * increases liver symthcs~sof ~n:n,~orensmogen: XICC of
h>pertensron in young women. * intrahcpat~ccholestasis. * hepatlc adenorxa: tendency to rJplurc. *
increasc gallstone forinanon. cancer risks- * cervical. * breast conro~ersial.* hepatocc1:ular
carcinoma. ?rotectlve.'preventlve effects of pills- * fibrocy s ~ i change c lr: the breast. * er.dometr!s!
cancer. orarran cancer: less o~ulationreduces risk for cancer. * pelvic inflammatorq. d i s c a x :
?-

'\risseriu go~rurrl~oeue not C h l a m ~ d i airuchornatis, * uterine Ierornyomas. * endometnosis. * acne.

* rhcurnarord arthntls. * hirsulism
Iron toxicit?.: clrnical senlng- accidental overdose of ferrous sulfatc rn children. S.'S of iror:
t o u ~ c i e -* hemorrhagrc gastritis, * hepat~cnecrosis with liver falure. * shock,metabo!lc ac~dos!~. *
.i-ray~ru\eaIundigested radiopaque pills in GI tract. Rx - * ~ron-bindingaFents. * orzl phosp33:c.
or hcarbonate salts (precrpitatc unabsorbed iron), * parentera1 deferoxamme
Organophosphate poisoning: M0.4- * irreversible block 0:'- acenlchollne es:t':asc
(noncornpet1r:ve inhibitor). -* accumulation of acetylcho1ine at sqnapszs: myonecrai junctions.
so:!rcc'- pesticides. lnitlal autonomic system overactiv1:y- * excesslvz lacrirnat~onsal~r-anon.
ftca! :ncontrcence. c o n ~ t ~ c t e pupils,d nlcotinlc cffects Iater :n :oxlci~-- * rnsc!~
Sotc: This material is copyrighted. A11 rights reserved. Edward Goljan, 3i.D. 2002

~veaknejs:paraIysis. * muscle fasciculations. low serum and RBC chol~nesteresr

(pseudochol~nesterase). Ru- * atroplne Rx of choice. * pralidox~me(2-PPLV) also may be used
Rs of hypertension (HTS): weight reduction is the most imponant factor in lou enng BP
-- Carbonic anhydrase inhibitors: MOA- * blocks the proximal reclamation of brcarbonarc. *
bicarbonate brnds with Na' ions and is excreted in the urine (diuretic effect). * produces a normal
XG metabolic acidosis from bicarbonzre lost in the urine. clinical uses- * chronic manaqement of
elaucoma: rcduces the rate of aqueous humor formation and reduces inrraocular pressure. *
akahnizes the unne: good for Rx of drug toxicities (e.g., salicylatc intox~cation).* &of _a_c_utu
mountain s 1 c . h ~produces
: metabolic acidosis. which 1s the compensation for respiratory alkalosis
CIinical uses of thiazides: initial drug used in Rx of HTN in elderly patients- also reduces r'r;~
lncldence of srrokes and fatal . M I S in this age group. initlal drug uscd In Rx of sq-sro1:c HTS In
thz elderly. one of the ~mtlaldrugs uscd in Rx of HTS In African-thericans. Kx oi cholcc in
trcatmenr 0:' nephrogenic diabetes insipidus: volume deplet~on from increased proximal
rcabsorptlon of Na- and water reduces degree of polq.uria, Rx of hq-percalciuria in calcium stone
formers. IRx of pro~imalRTA- increases reclamation of bicarbonate
"'
Clinical uses of Ioop diuretics: initial drug used in RY of HTN in chron~crenal failure. R\; of
choice for hypercalcernla after a diuresis is started with isotonic saline, congestrve hean failurc.
wlth acute pulmonary edema, Rx of halide poisonings- * fluonde. * Srom~de. acute rrnai
failure- flush out tubular ceIls obstructing the lumen and can change an oligunc to a poly~ricrcnal
failure
-- 410.4 of spironolactone: blocks the aldosterone-enhanced Na',:KA pump in the lare distal
convoluted tubule and collecting duct- * K- spanng effect, * danger of hqperkalemia. blocks the
protonX- ATPase pump in the collecting tubules- danger of normal PIG metabolic acidosis.
blocks androgen receptors- * Rx of hirsutism, * produces gynecornastia in men
310.4 of triamtereoelamiloride: they are not aldosterontr ~nhihltors. they block S a -
reabsorptlon and the secretion of K- in the aldosrerone-enhanced NaA:K-pump- K - sparing effect
-
--J

210.4 of nonselective P-blockers: block P,-receprors in the heart- * reduce s)mpathetlc

stimulation. * reduce blood pressure, * decreased contractiliry of ;he heart. * decrease hezn rate. *
:educe secretion of renin in kidneys, block PI-receptors in the smooth nuscle and lil zr. blocks
catecholamlne-induced glycogenolysis
- MOA of selective P,-blockers: cardioselecrive P-blockers- * pnmari1y rarger P: -receptors In hean.
* less bronchoconstric~~on than nonselective blockers
2 Side-effects of f3-blockers: conduction disturbances- e.g.. A\.' block. block a d r e n e r ~ l ~
srgs:'symptoms of ~nsulin.!'oralsul fonylurea-lnduced hypoglycemia In diabetes mellihrs- does ~ o t
hlock swearing. induce bronchospasm in those with asthma- less bronchoconstrlction xvith
sclcznvs types. depression. lipid effecrs (mainly in non-selective P-blockers)- * increase TG. *
dccrcasc HDL. rebound angina. hypertension if abruptly withdraw- up-reglatlon of ;3-
adrenergic receptors occurs when they are blocked
-: Clinical uses of @bIockers: hypertension. angina. congestive hearr failure and acutc
rnyocard~al ~nfarction- increases survival. cardiac arrhythmias. essential tremor- ben:gr:
condition \vi:h trembling of hands. prevention of migaine headaches. Graves' dlseasz- binck.~
adrcnrrgic s ~ g n and
s sqmptorns. pheochromocy-torna. h);pertrophic subaonic stenosls
-
- +,
Y10A of a-adrenergic blockers: In lowering BP. they block post-syaptlc a-adrznzrg:~
receptors- * vasoc~lateartenoles:'venules, * reduce vascular rcsistancc. * relax smooth muscle :::
urlna? bladder acd prostate: uscful in Rs of BPH. * unIike P-adrcnergic blockers. they iouer TC:
and CH. and increase HDL. nonselective types block a , and a?-adrener~icblockers- product too
mcch compensatory tqpes of effects (e.g., tachycardia)
Sote: This material is copyrighted. All rights reserved. Edward Goljan. M.D. 2007,

Side-effects of a-adrenergic blockers: dizziness due to orthostatlc h!porension. prazosln n;2!

3roducc a poslti\,e serum ILYA
a-Adrenergic blockers phenoxybenzarnine and phentolamine: produces a chzmicai
s~mparhectornq.. Rx of hbpertensive episodes with phzochromoc!toma unnl surgical remo\,al of
:.Jrnor. p:?entolammc- * Rx of'hypertenslve episodes due to pheochromocl;toma during s u r y n . -
Kx of s k ~ nnccrosls and ~schemiain accldcntal ~ nections
j of epinephrine or o ~ h e vasoconstrictors
r
VIOA of clonidine: centrally acting adrenergic drugs- * examples rnclude clonidlne. rnethy:dopa.
* stlrnulate a?-adrcncrgic receptors and irnidazolinc receptors rn the C I S . * reduccs c fferert
peripheral sympathctlc outflow. * ruductlon in blood pressure due to reduction in cardiac outpur:
decreased heart rate and vasodilatation of resistance vessels, * increase renai blood fiou.. k1LlO:'i of'
xcthyldopa- * same as for clonidlne. * converted by central nonadrenergic neuron> ixn
rnet'hyinorcp~nephnne,its actlve metabolite, stde-effects for methyldopa- * Coom'ns' pOjitlv:
hcrnolq-tic anurnla. * drug-induce SLE, * dmg-induced hepatitis: may be fulmlnant
510.4 of calcium channel blockers: examples- * verapamil. * dilriazem. * n~modipine.
mcardrp~ne.* block L-type calcium channels in smooth muscle and cardiac muscie. * pzrlpheral
-
artcr~olevasodiiator: no venular dilatation. * decrease cardiac contractility and heart ratt.: ncgarlvc
inotropic and c'nronotrop~ceffect, respectively. * coronary arten. vasodilatation
310.4 of hvdralazine, minoxidil, nitroprusside: arteriolar vasodilaror- hydralazlne and
mlnos~ail. anenolar:venular vasodilator- nitroprusside. no effect on reducing left ventricular
muscle mass. srdc effects- * drug-induced SLE w i ~ ha poslrive serum .%";A: hydralazme.
rmoxrdli: hypemchosis. * nitroprusside: thiocyanate toxicity
-
Initial drugs used in Rx of hypertension (HTS) in African-Americans: diuretics. calclum
channel blockers- added if the desired goal is not established. ACE inhibitors or X?' 11-rcccptor
biockcrs
Initial drug used in Rx of HTS in DM: ACE inhibitors arc thc Rx of choice- H T S control ;s rhc
srngle most imporiant factor in preventing a loss of renal functior, in DM
initial drug used in R x of HTS in CHF: ACE inhibitors are lZx of chorce
Drugs used in Rs of HTS in (diastoIic BP > 100 mrn Hg) in pregnancy: methyjaopa.
hydralazine- a!ternatlve drug choice
Drug used in Kx of HTS in a patient with urinary retention from prostate h?;perplasia: a -
adrenergic blockcr
Drugs used in R x of HTS in asthmatics: calcium channel blockers
Initial drug used in Kx of HTS in a patient with osteoporosis: thiazides- increased ca'- IC~UT-
reabsorpnor! In the kidneys
.ACE inhibitor: decreases preload- inhibit aldosterone. decreases afterload- inhibl: AT I1
Hydralazine, minoxidil: decrease afterioad alone- vasodilators
Sitroprusside: * decreases preload- venodilator. decreases afterload- vasodilator. R s of choict
:r, rrea:ment of rnali_=ant hhpertension and lowenng blood pressure :n a dlssectrns aortrc a x c a y 5 7
Thiazides: decreases preload alone- reduces volume by loslng salt and ware:
Caicium channel blocker: decreases afterload alone- vasodilator
Probucol: an antlosldant that 1s used ir, treating recurrent xanthelasmas. may produce ~ o r s a d e
ds pointes (polynorphic ventricular tachycardia). lowers HDL le\.cls
Sicotinic acid and fibric acid derivatives: activate c a p l l l a ~Ilpoprotern 1:pase. hence lncrcaslng
the hydroiysls of XYLDL in the circulat~on
HJIG T o - 4 reductasc inhibitors and fibric acid derivatives: should nor bc uscd ioge:h?r S : C i t '
:hey both may be associated ~ l t rhabdomyolysls
h '
and the potentlal for poiyuric acute renal fhallure‘
H\IG C:oA reductase inhibitors, nicotinic acid, and fibric acid derivatives: associated K::?
crus-mduced h e p a t ~ t with
~ s elevation of the transaminases
3ote: ?'his material is copyrighted. -41rights reserved. Edward Goljan. M.D. 2002.

A3IG CoA reductase inhibitors and bile acid resins: upreplatc LDL receptor s>nthcs.. ' 5 or!
'nepatocfles. hcnce loweriny serum CH and LDL
HMG Co A reductase inhibitors and nicotinic acid: inhlblt e n q m e s in t h u r mechanism of
actron of 1on:ertng l i p ~ d s
Flushing associated with nicotinic acid: conrrollcd by pretreatment wlth asp~rin
Fibric acid derivatives: greatest overall effect of all lrptd loivenng agents in ralsmg HDL levels
H3IG CoA reductasc inhibitor and fibric acid derivatives: increase the chance for u-arfarir.
toxicity
Bile acid resins: lower warfarm levels, hence causing undercoagulation of patlents on uarfar~n
Bile acid derivatives: cause a malassimilatron of drugs that are commonly used in thc hC2tmCnt ot"
next drseasc
Sicotinic acid: drug of choice for familial combined hypercholesterolemia and In 1oxx.erin~Lp ( a )
HMG Co.4 reductase inhibitors: drugs of choice for Iokvcnng LDL
Sicotinic acid and fibric acid derivatives: slpificant cffcct In lowerin: rr~glyccridcIcvcls
Estrogen: lowers LDI, levels, increases bone density
Fibric acid derivatives: associated with the inappropriate -4DH syndrome
Types of drugs of abuse (DOA): sedatives- * barbiturates, * alcohol. st~mulants- cocalnc.
haliaclnogens- lysergc acid diethylamide
31C D 0 . b in adolescents: marijuana, alcohol
CSS effects of long-term drug abuse: damage to neurotransmitter receptor sites
Drug screening: urrne best screening medium for DOA, blood also used in drug assays
Syrnpathomimetic DOA syndrome: examples- * amphetamines. * cocaine, S ,S- *
tachycardla'swcating. * mydriasrs: pupillary dilatation. * hypertensron. * hyperthennia
Opiatelsedative DOA syndrome: examples- * heroin, * benzodlazeynes. * barblmrates. S S-
* respiratory deprcss~on-+respiratory acidosis, * miotic pupils pinpo~ntpup~ls,* h>potznslon
Anticholinergic DOA syndrome: examples- * antidepressants. * antihistamines. *
antiparkmson-type medications. * atropine, * muscle relaxants. S:S- * rnydnas:~.* fel-er. * dr?.
skin
Ps~chedeliclhallucinogenicDOA syndrome: examples- * PCP. * LSD
.4ntidotes used in unconscious patients: dextrose- RjO possible hqpoglycemra frorr: ~nsuhr!
overdose. naloxone- poss~bleopiate overdose, intravenous thiamine- giucose ma>-preclpltare
Li,'ernlcke's encephalopathy in alcoholics with thiamine deficiency
Intravenous drug abuse (IVDA): MC localized infection is skln abscesses due to
S~ap/~~~lacoc~c.us aweus. HBV MC sysrernic infection. Hn', Infective endocardltls- * M C
tricuspid and aortic valve. * S. aureus MCC, tetanus- complication of "skin popping"
Heroin: derlved from poppy plant. usually "cut" ~vith some agenr (e.g.. quininc. talc)-
p a u l o r n a t u u s rcactlons occur in shmlungs from the cutting agents, non-cardlogenlc pulmonan
edema- frothins from the mouth is common, focal seqnental ~lomerulosclerosis- h>pzrtenslon -
3ephro:ic sqndrome, Rx- naloxone, a morphine dei-ivatlve xvith a high affim? for opioid bindlng
s~:csof thc mu rcceptor QTe
5leperidine: ,MC DOA in health professionals, 1-methyl-3-phenyl-I. 2. 3. 6-tecahydrop!nd;ns
(3lPTP)- * by-product of attempted synthesis of meperidine, * produccs ~rrcvcrs~hlc Park~n-:
c>-totoxicto neurons in ni~ostriataldopaminergic pathways
%lethadone: legaI syntheric opioid taken orally- mainly used to detoxify op~ateabusers. Ions-
act iny drug- * saturates CN S opiate receptors, * prevents sudden euphoric ac:lor, associ:~ed u.::?.
hero~n.* causcs phvs~caldependence.!tolerance
Benzodiaxepine toxicity: h10,4- * enhance the frequencv of opening up of Ci.AB.4, rcccprar-
chlo:lde ion channels-+ increases chloride ~ o nconductance, * GABA (:,-armnobuhmc acid) 15 zr.
~ n h i b ~ t o n3eurotransmirter.
. drug of choice for alcohol withdrawal svndrome. Rs of
\ole: 'This material is copyrighted. -41rights reserved. Edward Goljan. 1I.D. ZOO2

tos~cirl,- flumazenil. an antagon~stof bcnzodiazcprne and does not block barbiturates or orhur
depressanrs
Rarbiturate tosicity: 410A- * enhance the duratton of opemng up of the G.WA., receptor-
chlor!de ion channels-) Increases chloride ion conductance. * depress neuronal activity in rctlcular
act!v2t1n_gsystem-) ~nhlbltsthe inhibltoq effects of GABA and glycinc (an amino acld i n h ~ h ~ t o p
necrotransrn~iter). u l a e over pressure points: erythema multiforme, alkalinixing the urine
increases its excretion and lowers blood concentrations
Cocainc: MC' COD from D0.4 in United States. MOA- blocks uptake of neurohansm:nrrs

-
dopamrnc;SOR by presynaptic axon. predisposes to- * sudden death. * acute m y c a r d l a ;
~nt'arctlon(.4MT). stroke. * pulmonary edema. * ventricular arrhythmias. .- rnyocardlt:~. S S -
hypencnsion'sinus tachycardiz. psq-chos~s:!se~zure activity. mydnasis
-
Amphetamines: MOA- rcIease catecholzmlnes from presynaptlc t e n n a l s .
amphetamines: * dexrroamphetamine: Rx obesity, * methylphenidate: RYADHD and narcolepsy.
csampics- of

rnethamphctamine: '-ice" is street form of the drug. hallucinations- drug thar most slmulatrs
-
sch:zop;uema
Marijuana: MC illegal DOP, used In United States. MOA- * contains the psq-choact:vr
s::mulant A'-1etrah~drocamabino1(THC), * THC binds to receptors ,n substanria niya. globus
pai1;dus. h~ppocampus.cerebellum. * derives from leaves/flowering tops of hemp plants (C'u~-rrtuhis-
.saril:a). * hashish I S extracted resin of marijuana that has 5-10 times thc potency of' the pawn;
com;lound. * h19I: 11pidsolub;lity: THC is present in urine for more than a week. clln1caI usc.5- *
cancer: decrcase S;Y in cancer patienrs. * lower intraocular pressure in glaucoma. * analgcsla.
S S of marijuana use- * reddening of conjunctiva. * euphona, * delayed rcacnon time: znglneer
driving a train invo1vcd in a crash xith an oncoming train was found to have THC: metabolites In
IS urlne
LSl) (lysergic acid diethylamide): * MOA- *ergot alkaloid that binds to D, dopamlntl r c c e p t o r s i
!he bra:n. * also blocks 5-HT, serotonin reccptor In peripheral tissue. pred~sposesto chromosomal
breakage leadine to con~enltaldefects. S/S of LSD toxicity- * hallucinat~oxls.* flashbacks
PCP (phenc~clidinc): angel dust. MOA- reacts with opioid-like s i m a receptors and scb>~c.:
pi-glutamate reczptofi (antagonist), +. initlallv introduced as a dlssoc~ativean.csthet1c: srparatcs
'nodil! functlnns from the mind without a loss of consciousness. S.:S of PCP rox~c::!-- *
auitazon violent behaylor. * coma with the eyes open. * impervious to patn
I:se of pblocker in Rx of Grave's disease: tlq-roid hormones normally upre_slatc sqnthcs~sof'
r3-receptors :ha{ ~nteractw-lth catecholamincs and produce many of the symptoms of t h y ~ o ~ o x l c o s ~ ~ .
g11-:ns P-biockers. blocks the 0-receptors, hence blockiag the adrenergic scmptoms of
t h > ~ o r ot cosis
s
Electrolyte changes w-hen giving insulin: drives glucose into the celI along ~ i t potass:urr:
h and
phos~~hare
Rx of carcinoid syndrome: octrcotide (,somatostatin analogue), also used rn Rx of acromttgaly
ar,c VTPomas
Patient went into congestive heart failure. What drug could have potentiated thirl':
\-erapamil. potcnt negative inotropic effect
Patient with asthma not responding to albuterol: Rx with conicosterord medlhaler
Patient with pneumonia due to a gram positive diplococcus (Streptococcus pneurnuniar): K\
11-:;:7 ?unicilIin Ci. uhlcn blocks cel: a-ail sqnthesrs
Yohimbe: vasodilator used to ILK Impotence
Ginkgo biloha: ImFroves memory
Ginseng: s~ess-protective
Saw palmetto: Ks prostax hyperplasia
Echinacea: xvound healing. irnmunostimuIant
Sote: This material is copyrighted. .+I1 rights reserved. Edward GoIjan. Xl.1). 2002

Kava: scdatlve
2 5lelatonin: sleep. Kx of jet-lag
2 St.John\Vort:Rxofdepressron
Jojoba: cosrnerlc. hair g r o u ~ h
Soy: phytoestrogec
Green tea: antioxidant. decrease cancer
1-aterian: sleep

HIGH YIELD NOTES PHYSIOLOGY@

Proximal renal tubule functions (see nephron diagram): primary site for S a ' reabsorption.
p r ~ r n a qsrtc for reclamation of HC03-- loss of reclamation leads to Gpe I1 proxlrnaI rend tubular
ac~dosisdue to loss of bicarbonate, primary nephron slte for synthes~sof ammonia vra c n c m a l i c
conversion of glutamine (non-toxic vehicle for carry KAj- m blood) into NH,'- a-ketoglurarare.
pnrnarl; site for rcabsorprion of glucosc (cotransport with Na-). urea, amino acids. phosphalu
Functions of thin descending limb: only permeable to water. hence the urine becomes estreme1:-
hqpenonic by the rime it reaches the loop of Henre
'
Functions of thin ascending Iimb: rrnpmeable to water but permeable to Na- and C1.. hence thc
I_:Osm b e s ~ n sto decrease
Functions of thick ascending limb (TAL medullary segment): generation of free u a t e r vla the
act1i.e S a '-K--2 C1- co-transport pump. this pump is the most sensitive part of the nephron for
damage due to tlssue hypoxra. blocked by loop diuretics, pump also reabsorbs calcium (not
PTH-enhanced)
Functions of the cortical TAL segment: NaAiC1'pump in early d~staltubule- S a ' and Ca' '

(PTFI-enhanced reabsorption) cat~onsshare the same channel for reabsorpt~on. blocked b!

th1azidt.s
*' Functions of the rnacula densa: interacts with the juxtaglomerular (JG} apparatus on :hc af5erc.n:
arterrole. ~ncreasedNa' In the urine inhibits renin release and wce versa
"'
Functions of aldosterone-enhanced GTPase T ~ - - K +exchange pump in distal collecting tubule
and collecting ducts: Na- is reabsorbcd in exchange for KL. effect of ~ncrcaseddrstal dzllvcr~;
of S a L from more proxlrnal acting diuretics (e.g..Ioop diuretic or thiazlde diuretic)- * there IS an
au-menred NaL:K- exchange. which may lead to hvpokaiemia and ~ncreasedreabsorpt~on of
bicarbonate (rnetabollc alkalosis)
- Functions of the aldosterone enhanced H't'K' ATPase pump and H+ATPase pumps in rhe a-
intercalated cells in the collecting ducts (L7SMLE):pnmarq sites for the excretion of cxcess H-
Ions- dysfunction of the H-!K- ATPasc pump is the pnmary cause for h p e I distal RT.4
2 _\'ormatdilution of urine: UOsm in the Iate distal collecting tubu1e:'collecting duct 1s noma!ly
--I50 mOsrwk~-primarily contains free waler and a smaller amount of obligated water that must
zccompany solute. when POsm is low. ADH is inhibited- absence of ADH causes the loss of frec
n a t c r In the urlne, poslnve free water cIearance - * CH?O = V - COsrn. xvhere C H 2 0= free lvater
clearance. 1,'= volume of urine in mL!mm. COsm = obligated u-ater. * to calculate COsm: COsm =
LUOsmx I':POsm, * a posit~veC H 2 0 indicates dilution (free water is lost in rhe =me). * example
unne volume 10 mL. POsm 250 m0sm. UOsm 150 rnOsm: COsm = 150 x 10.250 6 rnl.. C.II:C> =
iO - 6=-3r;;L
-
"'
Sormal concentration of urine: increase in POsm is a srimulus for .4DH rciease. , U l H rezdcr.i
t:7c 1 . x ~~ l s r a land col!ectlng ducts permeabIe to free uater (not Na-. canno: rcabsorb obiigatzd
~ v a t e r f -zrrae I S concentrated. negative CH:O (fiee water 1s reabsorbed back into thc blood)- c . ~ . .

94