Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
360 Cards in this Set
- Front
- Back
|
Cimetidine , Famotidine, Ranitidine, Nizatidine
|
H2 receptor blockers,
|
|
|
aluminum hdryoxide
|
antaacid, weak base that reacts with HCl in stomach, raises intragastric pH, CONSTIPATION, affects bioavailaibitliy of TC, digoxin, antimuscarinics reduced.
|
|
|
magnesium hydroxide
|
antaacid, weak base that reacts with HCl in stomach, raises intragastric pH, DAIRRHEAn, affects bioavailaibitliy of TC, digoxin reduced.
|
|
|
calcium carbonmate
|
antaacid, weak base that reacts with HCl in stomach, raises intragastric pH, kindey stones, dense fecal matter
|
|
|
histamine, Ach and gastrin
|
imp stimuli for gastric acid secretion from pareital cell , activate K/KATPase pump
|
|
|
Dycylomine
|
blocks cholinergic receptor and reduces gastric acid secretion
|
|
|
Cimetidine
|
H2 antagonist, reduces gastric acid secretion , via GS(+cAMP), given orally, excreted in urine, short half life, increased renal failure, inhibits C450 and slows metab of warfarin, diazepam, pheytoin, quinidine, carbamazepine, theophylline, and imipramine , AE- gynecomastia, galactorea, reduced perm count
|
|
|
misoprostol
|
stimulates prostaglandin receptiron and reduces acid secretion , via Gi(-cAMP)
|
|
|
omeprazole
|
blocks proton pump
|
|
|
Ranitidine , Famotidine, Nizatidine
|
H2 antagonist, single dose reduces basal secretion og gastric acid, used for gastric and duodenal unclers and preventing recurrence, only paritally inhibits gastric acid secretion induced by acetylcholine or bethanechol , reoccurence of peptic ulcers wit htehse , AE- HA, diarrhea, muscular pain, CNS( confusion, hallucinations) , reduces ketonacoazole reabsotion(needs gastric acid medium)
|
|
|
ranitidine
|
10 times more potent than cimetidine, no antiandrogenic and protein stimaution effects, does not inhibit mixed function oxygenase in liver
|
|
|
Famotidine
|
40-50X more potent than comeitine
|
|
|
nizatidine
|
no first pass metab, 100% bioavailability, elimiated by kidney, no IV
|
|
|
Omeprazole, esomeprazole
|
proton pump inhibitrs, binds to H/K ATPase, proton pump of parietal cell, supresses secretion of H ions into gastric lumen , approved for GERD, reduce risk of bleeding with NSAIDs, used for hemoragic ulcers, eradicate PPIs, AE- increased gastric carcinoid tumors, inhibits metabolism of warfarin, phenytoin, diazepam, cyclosporine, prolonged use of PPI and H2 blockers may decrease B12 bioavailability, calcium carbonate- requires low gastric pH, give calcium citrate, small increase inGI infections, rarely pancreatitis, hepatotoxicity, and intersitital nephritis
|
|
|
sucralfate
|
cytoprotentic(mucosal protective) agent, compel of AlOH and sulfated sucrose, bind to protiens forming complex gels with epithelial cells, sucralfate creates physical barrier againt HCl and prevents degradation of mucus by pepsin and acid , stimulates prostaglandin release as well as mucus and bicarb output, requires acidic pH for polymeriazation, dont give with H2 atnaogins
|
|
|
prostaglandins
|
PGE2 produced by gastric mucosa inhibits HCl secretion and stimulates secretion of mucus and bicar(cytoprotective effect), defieciency of PGs invovled in pathogenesis of peptic ulcers
|
|
|
misoprostol
|
analog of porstiglaidin E, approved for presenvtion of gastric ulcers induced by NSAIDs , less effective than H2 antagonists and PPIs for acute treatment of peptic ulcers
|
|
|
regimens for H pylori
|
1) PPI+claryothromycin+amoxillin2)PPI+clarithromycin+metronidazole3) bismuth subsalicyclate+metronidazole+tetracyline+ranitidine or PPI
|
|
|
rofecoxib and vioxx , celebrex
|
coxibs are superior gastro AE profile over conventiornal NSAIDs, taken off market in 2004 due to MI(bioxx),
|
|
|
pirenzipine
|
Anticholinergic, msucarinic antagonis, supresses acid secretion via M3, poor penetration through BBB low CNS toxicity, used for petic ulcer in regractory cases
|
|
|
dycyclomine
|
Anticholinergic, msucarinic antagonis, ihinits acid secretion by binding to mAchR in parietal cels, not as effective as H2 or PPI, use- IBS, AE- dryness of mouth, blurred vision, urinary retention, arrythmias and constipation at higher doses
|
|
|
cisapride
|
not avail in US, release Ach in myenteric plexus, increases muscle tone in esophageal sphicnter, GERD, increases gastric emptying in people with diabetic gastroparesis, treat bowel constipation , AE- long QT syndrome, predispoises to arrhythnmias with erythromycin, ketoconazole, diarrhea
|
|
|
senna
|
stimulant laxative, orally, 8-10 hrs, water and electrolute secretion into bowel, used in combo with docusate, to treat cases of opioid induced constipation
|
|
|
bisacodyl
|
suppositories and enteric coated tablets, potent stimulator of colon, AE- abd cramps and potential atonic colon with prolonged use, don’t take with antacids, could lead to stomac rirrilation and pain
|
|
|
castor oil
|
broken down in small intestine to ricinoleic acid- irritates gut, increases peristalisis, avoid in pregnant pts, stimuates uterine contractions
|
|
|
methycellulose(citrulcel), psylium seed(metamucil), bran
|
bulk laxative, hydrophilic substances(from indigestible parts of fruit and veggies), forms gen in LI causing water retention and intestinal distention, increases peristalitc acitlbity, use with caution in bed bound pts, can cause intestinal obstruction
|
|
|
bismuth salts
|
do not neutralize stomach acids
|
|
|
Mg citrate, Mg sulfate, Mg phsphate, Mg hydroxide
|
nonabsorbale salts that hold water by osmosis and distends bowel by causing stimulation follwoed by defecation
|
|
|
lactulose
|
ostomatic laxative, semysynthetic disacchraide sugar, large doseases- degreaded by colonic bacteria and form lactic, formicand acetic acid which increases osmotic effect, treating hepatoencephalopathy- helps draw out ammonia prevents hyperammonia
|
|
|
PEG(polyethyl glycol)
|
colonic lavage for endoscopic and radiological procedures
|
|
|
mineral oilds and glycerin suppositories
|
lubicrant laxatives, lubicatns aid easy passage of stools
|
|
|
docusate sodium, docusate calcdium, docusate potassium
|
stool softener, surface active agents emulsified with stools to make softer and eaiser passage
|
|
|
odansteron, graniststron
|
antiemetic, 5HT3 receptor blockers in periphery, long duration of action, administer prior to chemotherapy , prolongation of QT wave
|
|
|
prochorplerazine
|
D2 blockers, phenothiazine, low or moderately ematogenic chemotherapy, AE- hypotension, restlessness, dose limiting, extrapyrimidal sympotms and sedation
|
|
|
metoclorpamide
|
D2 antagonist, mixed HT3/HT4 antagonist. antiemetic action due to antagonistic activity at D2 in CTZ resubstituted benzamides with antiemetic acitivity, effective agaisnt cisplatin, AE- antidopinergic side efffects- sedation, diarrhea, extrapyrimidal symtpms, limits its use in high dose , precausitons- inhibitionsaction of DA, should be used with caution in parkinds, uses- diabetic gastroparesis, antiemetic, GERD , high doseases- 5HT3- antiemetic
|
|
|
lorazapam and alprazolam
|
low antiemetic potenticy, benzediapenies, sedative, anxiolytic and amnesic efect, useful for anticipatory vomiting
|
|
|
droperidol and haloperidok
|
antiemetic, butyrophenones that act by blcoksngi D2, doleperiodl- prolongs QT interval, reserved for refractory cases
|
|
|
dexamethasone and methyprednisolone
|
antiemetic, mildly to moderaltey emetogenic chemotherapy, may be due to blockage of prostaglandins AE- insomnia, hyperglycemia- DM
|
|
|
aprepitant
|
blocks neurokinin-1/substance P in brain, administered orally with dexamethasone and palonestron, CYP3A4 metabolism, it can affect the metabolism of other drugs metabolized by this enzyme, can also induce enzyme and affect response with warfarin, shorten half life of the anticoag, AE- constipation and fatigue
|
|
|
apomorphine and syrup ipecac
|
emetics, act by stimualtions CTZ, gastric mucosal irritation and used for accidental poisonings
|
|
|
diphenoxylate, loperamide
|
control diarrhea, opoid like function in gut, activate presynpatic opioid receptros to inhibit Ach release and peristalisis, atropine added to discourage abuse, AE- drowsiness, abd crampls, dizziness, toxic megacolon young children or in pts with severe colitis
|
|
|
bismuth subsalycylate
|
antimcrobial, inhibits acitiiy of pepsin, increases mucus and interacts with glucorptiens in necrotic mucosal tissue to coat and protect ulcer crater antidirrheal, coats intestinal epithelium and decrease GI irritation
|
|
|
octreotide
|
somatostatin derivative, control diarrheas associated with met carcinoid tumors and vasoactive intestinal peptide tumors
|
|
|
steroids
|
ulcerative coilitis and crohns disease , acute cases and to control flares
|
|
|
sulfasalazine
|
sufolonamide derivative, antiinflammatory effect used in UC and CD, prodrug converted into sulfapyridine and 5-ASA in GI , inhibits PGs and LTs
|
|
|
hyoscyamine, dicylomine
|
antispasmodic that helps with cramps or diarrhea
|
|
|
ursodiol
|
aka ursodeoxylic acud(UDCA), secondary bile acid, used for gall stones where risk of surgery is too high, dissolves gallstoes in bile ducks
|
|
|
celecoxib
|
COX 2 selective inhbits, sulfonamide, may caus hypersensitivty(rashes),
|
|
|
warfarin
|
increase bleeding when used with NSAIDs
|
|
|
NSAID CI
|
pregnancy , cat 3 in 1 and 2 trimester, D in trim 3
|
|
|
aspirin
|
irreverible COX inhibitor
|
|
|
NSAIDS AE
|
epigastric distress, prolonged bleeding time, hypersnesitivty , hepatic injury with high doses of salicylcates
|
|
|
coxibs
|
cox 2 inhibitos, analgesic, antipyertic, antiinfl, fewwer GI effects, not cardioprotective, renal toxicity , linked to cardiovascualr thrombotic events , rofecoxib, valdecoxib, etoricoxib not available in US , colexocib only one avail in US
|
|
|
mexolicam
|
not as selective forCox 2 as coxibs
|
|
|
acetaminophen
|
analgesic and antipyertic, mild to moderate pain, DOC for OA, fever and flulike symptoms, short term fever and minor pain in opreg, RA use with other drugs, AE- liver impairment in high dosees , DOC for antipyerisis in children and teens , use acetylcysteine to tx overdose
|
|
|
|
|
|
|
methotrexate
|
DOC for treatment of RA, lower than for chemo doses, inhibits aminoimidazolecaboxamide ribonucleotide(AICAR) transformylase, AICAR transforlymlase catalyzed the final steps of de novo purine syntehsis-->IMPthymidylate synthase pathway may be invovled, inhibition of AICAR-->acumulation of adenosinde which is an antiinf mediator -->acts of A2b receptor and supresses NFkB indcued by TNF
|
|
|
cyclophosphamide
|
alkylating agents cross link DNA, preventing cell replication, AE0 bone marrow supresion, infertivility, hemoragic cystitis, long term use increases risk of infeciton nad malignancy
|
|
|
azathioprine
|
cytotxic agent-purine antimetabolite, converted to 6-mercaptopurine, inhibits de no vo purine syntehsis, leads to B and T cell supression, and decreased IL2 secretion , AE- xanthine oxidase splits active material to 6- thioruic acid prior to excretion in urine, pts receiving allopurinol for control of hyperuriciemia should have the dose of azathioprine reduced, AE- bone marrow suprression,GI disturbances, infections and malignancies
|
|
|
cyclosporine
|
immunophilin ligand, antifinammatory, forms complex with cyclophilin and immunophilin, complex inhibits calcineurin, which is needed to activate NFAT which induces cytokine, AE- nephrotxicity
|
|
|
Hydroxychoroquine
|
antiinfl, mechanism unknown, antimalarial, used in combo with other drugs, AE- serious effects rare, hemolysis in G6PD pts, retinal damange is rare, opthalmologic exam recomented for those that are high risk(over 60, liver disease, retinal disease), low risk- examine every 5 yrs
|
|
|
sulfasalazine
|
metablized by bacteria in colon, 5-ASA imp for RA, not imp in UC, AE- rash, nausea, vomting, dizziness, HA, leukopenia
|
|
|
gold sodium thiomalate
|
IM, rare due to toxicity
|
|
|
auranofin
|
oral, gold salts taken up by macropahges and supress phagocysosi and lysosomal enxyme, toxicity high, used infreunqcyly
|
|
|
adalimumab
|
anti TNF drug, fully human IgG1 anti-TNF monoclonal antibody, binds to soluble TNF alpha and prevents its interaction with TNF receptors, results in down regulation of macrophage and T cell function. AE- cytopenia(monitor CBC), serious infections, don’t give in pts with active infection, screen for latent TF before, and during tx with this drug
|
|
|
entanercept
|
anti TNF drug, recombinant fusion of two TNF receptors linked to Fc portion of human IgG-1, binds to hyuman TNF alpha , AE- cytopenia(monitor CBC), serious infections, don’t give in pts with active infection, screen for latent TF before, and during tx with this drug
|
|
|
Inflimiximab
|
anti TNF drug, chimeric monochomnal anti TNF alpha anbivoy, binds to hyuman TNF alpha , , AE- cytopenia(monitor CBC), serious infections, don’t give in pts with active infection, screen for latent TF before, and during tx with this drug
|
|
|
anakinra
|
IL-1 receptor antagoinst
|
|
|
glucocorticoids
|
prompt and dramatic but controvversical, use short course before you begin other drug, AE- lots, osteoporosoisi, wt gain , fluid retension, cataracts, poor wound healing, gastric ulcers, GI bleeding, hyperglycemia, hypertension, adrenal supresion, increase risk of infections
|
|
|
Leflunomide
|
cytotoxic agent, combo with methotrexates increases risk of hepaoxitcity, undergo rapid conversion to its active metabolize A77-1726 which inhibits dihydroratate dehydrogenase, leading to lower levels of UMP, arrest in G1 phase, inhibits autoimmune T cell proliferation and production of autoantiboeis by B cells,
|
|
|
NSAIDS
|
first line of treatment for acute gout , but aspirin CI because it comptees with uric acid for organic acid secretion mechanism in proximal tubule
|
|
|
cholchicine
|
binds to tubulin, inhibits its polymerization and prevents formation of microtubues, disrupts granulocytes decreasing migration into affected area, blocks cell fivision by disrupti g mitoic simple, inhibits synthesis and release of lekuotrienes, AE- nausea, vmting, abd pain, diarrhea, myopahty, neutropenia, aplastic anemia, alopecia
|
|
|
glucocorticoids
|
antiinflammantory and immunosuppresive, could be used for acute attack of gout, depot preperatiosn can be injected in site
|
|
|
allopurinal
|
decreases uric acid syn, used for gout, MOA- purine analong, inhibits xanthine oxidase, facilitates dissolution of tophi by lowering uric acid plasma concentration , NSAID or cholichocine given in first 4-6 mo to reduce chance of acute attack of gout AE- hypersnesitivty skin reactions, steven johnson syndrome, drug interactions- with anticanger drug mercaptorine and immunospreasant azathoprine which are also metabolzied by xanthine oxidase, toxic levels of these drugs with coadmin, dose reduction of other drugs
|
|
|
probenecid and sulfinpyrazone
|
enhance uric acid excretion, urate is filtehred,secreted and reabsorbed by kidneys, mediated by specific transporter, transporter exhcnages urate for anion, comptes with urate for transporter and inhibts reabsortion
|
|
|
probenecid
|
do not use with pts with kidney stones or overproduction of uric acid, given with cholcinine or NSAID to prevent acute attac kf gout, AE- mid GI irrtnat, hypersneticit reaction, lots of fluids to avoid kindey stones
|
|
|
sufinyarzone
|
AE- gi irritant, jhypersensity(rash with fever), depression of hemaptoeptisis, don’t use with underlying blood dysciraiss, risk of kidney stoens so take lots of fluids, inhibits warfarn metabolism
|
|
|
rasburicase
|
agents that enhance uric acid metabolsim, oxidizes uric acid to allatoin, a soulbule compound excreted by kineys, in chemo can cause increase in plkasma urate levels due to rapid lysis of tumor cellsand can lead to massive renal injury, exogenous uricase can reduce plasma urate levels and prevent renal damage, can use allupruinor to prevent tumor lysis sytem, a recomb version of aspergillus urincase avail in US
|
|
|
acetaminophen
|
|
|
|
NSAIDs
|
use for mild to moderate pain, in inflammatory conditions like arhtiritis and gout
|
|
|
codeine, hydrocodone, oxycodone, meperidine, propoxyphene, tramadol
|
opioids for mild-moderate pain
|
|
|
morphine, hydromirphine, oxymorphine, levorphanol, fentanyl, sufentanil, methadone
|
opidiods for moderate to severe pain
|
|
|
mepridine
|
u receptor agonist, metabolic toxicity, half life of 3h, its metabolite normeperidine has no analgesic properities, has half life of 15-20 hr, AE- tremulousness, dysphoria, myoclonus and seizures , convulsion, refelxes, serotonin syndrome(deilrium, hyperthermia, head ache, hyper or hypotension, rigidity, convulsions, coma, death
|
|
|
propxyphene
|
administered doses that produce little analgesia, dose escalation could lead to norpropoxyphene, renal dysfucntion eledery at risk
|
|
|
pentazocine, butorphanol, nalbuphine
|
mixed opioid agonist-antagonist . Pentacozine and butorphanol can cause psychomimetic effects
|
|
|
antideperransatns, anticonvulsants, corticosteroids, hydroxyzine, clonidine, lidocaine, capsaicin, caffeine
|
analgesic adjunctive agents
|
|
|
SSRIs
|
less effective for enuropathic pain
|
|
|
TCAs
|
can releive neuropathic pain including diabetic neuropathy and postherpetic neuralgia
|
|
|
carbamazepine
|
DOC for trigem neuralgia , anticonvulsant
|
|
|
gabapentin
|
postherpetic neuralagia and diabetic neuropathy, anticonvulsant
|
|
|
pregabalin
|
anticonvulsant ,postherpetic neuralgia, diabetic neuropathy, fibromyalgia
|
|
|
valproate and topiramate
|
anticonvulsant , migraine prophylaxis
|
|
|
dexamethasone
|
DOC out analgesic adjunctive agents
|
|
|
methadone
|
less euphoria and longer duration of action, u receptor agonist, NMDA antagonist, serotonin and NE reuptake inhibitors, detoxification and for maintaince of chronic relapsing heroid addict, AE- QT prolongation, torsades, death
|
|
|
levomethadyl acetate
|
longer half life than methadone, approved for detox clinics
|
|
|
codeine, oxycodone, and hydrocodone
|
less efficanous than morphine, used in combo, CYP2D6
|
|
|
Dextropropoxyphene
|
u agonist, weaker analgesic than codeine, propoxyphe has increased risk of seixures and cardiac conduction abdnomlarities and should be avoided in elderly , mild to moderate agonist
|
|
|
propoxyphene
|
mold to moderate agonsit, half life is 30 hrs, accumulation canlead to toxicity, don’t give routinely, cardiotoxicity, no logner used in US
|
|
|
tramadol
|
mold to moderate agonist, weak u afonist and NE and serootonin reuptake inhibitor, useful for neuropathic pain, increased risk of seizires in pts pts with seizure disorder and those taking medication for lower seizure threshold, serotonin syndrome
|
|
|
pentazocine butorphanol, nalbuphine, buprenorphine
|
mixed agonist antagonist, mixed opiod- agonist-antagonist potent analgesic in opiod naïve pts, precpipate withardwa in people who are physciall depedent on opioid , useful for mild to mod pain, ceiling effect, AE- psychomemtiectic effects with petazocine, butorphanol, nalbuphine
|
|
|
pentazocine , butorphanol
|
k agonist and a u antagonist or partial agonist
|
|
|
nalbuphine
|
k agonist and a u antagonist
|
|
|
buprenorpihine
|
partial u agonsit and k antagonist , approved for mamangement of opioid addiction
|
|
|
naloxone and naltrexone
|
naloxone- tx acute opioid overdose , Naltrexone- opoinoid addition, decreased craving for alcohol in chornic alcoholics
|
|
|
dextrometoprhan and codine
|
antitussives, most effective supression of cough, differ from other opinoids
|
|
|
diphenoxylate, loperamide
|
anitmotility agents, used to tx diarrhea, act by different mechanisms by mu or delta receptros on enetic nerves, epitheial cells and muscle
|
|
|
Carbenicillin, ticarcillin, piperacillin
|
used to tx psuedomonas , effective agaisnt g- bacilli, combied with B lactamase inhbiitor
|
|
|
Methicillin, naficillin, oxacillinm, dicloxacillin
|
B lactamase resistant, infective agaisnt MRSA, restricted to treatment of B lactamase producing staphylcocci, recommended as first line tx for staphylcocci endocarditis in pts without artifical hrt valves
|
|
|
ampicillin and amoxiccilin
|
similar to pencilin G, g- acitivty, suspective to B lactamase, activity enhanced with B lactamase inhibitor , amoxicillin higher bioavailability than other pencillins(including ampicillin), amoxicillin- prescribed to children and in pregnacy , tx of acute otitis media, streptococcus pharyngitis, pneumonia, skin infections, UTI, used to tx URI, amoxillin- standard regimen for endocarditis propylaxis during dental or respiratry tract procedures, ampicillin- combo with aminoglycosides to treat entercocci and listerial infections
|
|
|
Oxacillin
|
|
|
|
pencillins
|
resistance due to inactivation of B lactamase, modication of target PBPs, impaired pepentration of drug ot target PBPs, impaired pentration of drug to target PBPs, increased efflux, resistance- MRSA- altered target PBPs(low affinity for B lactam antibtiocis, half life- 30 to 60 min, oral absoprtion- absorption impaired by foox(except amixiclin) naficillin(erratic not good for oral), amoxicillin( high oral biovailabiltiy) AE- hypersnesitivity, penicolic acid major antigenic determinant, macupolapular rash, anaphylaxis, cross allergic rxn, diarrhea, pseudomembrane colitis(ampiccilin), macuopapulr rah(ampicillin, amoxicillin), intersitital nephritis(methicillin), neurtotoxicity(epileptic pts at risk), hematologic toxicities(ticarcillin), neutropenia(nafcillin) , hepatitis(oxacillin), secondary infeciton- caginal candiadiss
|
|
|
Penicillin G
|
DOC for syphilis, strep infections, suseptible pnuemococci , active against G+, g- cocci(neiserria) most anaerboes(not bacteroides), suspetible to B lactamases , AE- hypersnesitivity, penicolic acid major antigenic determinant, macupolapular rash, anaphylaxis, cross allergic rxn, diarrhea, pseudomembrane colitis(ampiccilin), macuopapulr rah(ampicillin, amoxicillin), intersitital nephritis(methicillin), neurtotoxicity(epileptic pts at risk), hematologic toxicities(ticarcillin), neutropenia(nafcillin) , hepatitis(oxacillin), secondary infeciton- caginal candiadiss
|
|
|
Penicillin G benzathine
|
repositary oencillin , IM, half life- 3-4w
|
|
|
Penicillin G procaine
|
repository pencillin IM not IV(risk of procaine toxicity) half life- 12-24hrs, seldom used(icnreased resistance)
|
|
|
Penicillin V
|
similar to pencillin G, less active agaisnt G- bacteria, more acid stable than G, orally for mild to mod infecitons, pharyngitis, tosilltis, skin ifnections(caused by strep)
|
|
|
Cephalosporins
|
B lactam antibiotics, bactericidal, affected by same resistace mechansimsg+ acitvtiy diminsiehd while g- activity increases from 1st to 3rd, 4th against g+ and gi, inactive agaisnt MRSA enterocci, listeria, legionella, chlamydia, mycoplasma, actinobacter, 3rd gen(cefoperazone, cefotaxime, ceftazidime, ceftriaxone, cefixime)- enhanced activity agaisnt G- cocci, highly active agaisnt enterobacteriscia, Neisseira and H infleunza, cefotaxime and ceftriaxone- active agaisnt pneumococci, 4th gen- tx with suseptible organims PK- parentarly(exceot cephalexin, cefaclor, cefixime), 3rd generation reaches adequate levels in CSF, mainly eliminated by kidneys(except- ceftriaxone and cefoperazone excreted in bile) AE- allergic rxns, pain at infection site(MI), thrombophlebiis(IV), superinfections(C difficile)
|
|
|
cefazolin, cephalexin
|
1st gen, rarely DOC for any infection, cefazolin- DOC for surgical prophylaxis, pencillin G substitutes, resistant to staphylcoccus pencillinase , activity agaisnt G+ cocci and p mirablis, e coli and k pneumonia
|
|
|
Cefamandole, cefoprazone, cofetan
|
AE- hypoprothemobenia(Vit K admin can prevent) disulfiram like rxn(avoid alochol)
|
|
|
Cefepime
|
4th genergation, parental amin, wide spectrum, gram + acitivty of 1st gen and G- activity of 3rd gen, ex enterobacter, hemophilus, neisseria, ecoli, pneumococci, p. mirabalisis qand p aeruoginosa
|
|
|
ceflaclor, cefoxitin, cefotetan, cefamandole
|
2nd gen, extended g- coverage, H influenza, enterobacter aeroginoas, neisseria, weaker against G+, app- used to tx sinusitis, otitis and lower RTI, cefotan and cefoxitin- prophylaxis and therapy of abdominal and pelvic cavity infections
|
|
|
Cefoperazone,cefotaxime, ceftazidime, ceftriazone, cefixime
|
3rd generation, enhaced acitivty against g- cocci, highly active against enterobactericeae, Neisseria, and H influenza, less active against most G+ organisms, cefotaxime and ceftriaxone- usually active against pneumococci
|
|
|
Ceftazidime
|
3rd gen cephalospor
|
|
|
Ceftriaxone
|
3rd gen, DOC for pencillin resistant gonorreha, DOC for meinigitis due to ampicillin resistant H infelunza, tx of lyme disease(CNS or joint infection), prophylaxis of meningitis in exposed individuals , activitliy agaisnt P auerignoas
|
|
|
Carbapenems
|
synthetic b lactam antibtioics, ex- imipenem and meropeneme clincial app- used to avoid resistance, DOC for enterobacter infections, extedned spectrum B lactamase producing gram-,PK- IV, imipenem- nephrotoxic metabolite but combine with inhibitor cilastatin will prevent this AE- GI distress( nausea, vomiting, diarrhea), high levels of imipenem- seizures, allergic rxns(partial cross reactiblity iwht pencillins)
|
|
|
Imipenem/Meropenem
|
imipenem- nephrotoxic metabolite but combine with inhibitor cilastatin will prevent this, resist hydrolysis by most B lactamases, very broad spectrum of actiity, activity agaisnt penicillanse production g+ and negative orgnais, aerobes and anaerobes, p aeruginoas, not active against MRSA
|
|
|
Cilastatin
|
use with impent in order to avoid nephrotoxic metabolite , dihydropeptidase inhibitor
|
|
|
Aztreonam
|
spectrum- aerobic gram negative rods only, no activity agasint g+ bacteria or anaerobes, resistatn to action of B lactamases, application- UTI, lower RTI, speticemia, skin/structure infections, intrabdominal infections, gynecoligcal infections caused by g- bacteria PK- IV or IM, inhalation in CF pts, penetrates CSF when inflamend, exrecreted by urine, AE- littlecross reactvity, skin rases, elevated serum aminotransferases, GI upset, vertigo, head ache, phlebeitis or thrombophlebitis reported with IV use
|
|
|
β-lactamase Inhibitors
|
|
|
|
Clavulanic acid, sulbactam, tazobactam
|
contain B lactam ring but does not have sig antibacterial activity, bind to and inactivate most B lactamases, avail only in fixed combos with specific pencillins
|
|
|
Vancomycin
|
useful agaisnt multidrug resistant bacteria, effective agaisnt MDR organisms(MRSA, enterococci, PRSP, bactericital, bacterial glycoprotein, active agaisnt G+ only, all g- are resistnceresistance- plasmid mediated changes in drug permeability, modification of D-ala-Dala binding site, tehratputic app- in combo with aminoglycoside for treatment of enterococcal endocarditis or PRSP, tx of serious infections caused by B lactam resistant G+ orgaims, tx of G+ infectins in pts severly allergic to B lactams, given orally for treatment of staphococcal enterocolitis or antibiotic assoicated pseudomembrane colitis, PK- poor oral absorption, slow IV infusion, penetrates CSF when inflamed, 90-100% excreted via kidneys, AE-fever, chills, phebitis in infusion site, red man/red neck syn(infusion related flushin over face and upper torso), otoxicity(drug accumulation, nephrotoxicity(drug accumulation)
|
|
|
Daptomycin
|
binds to cell membrane via calcium dependent insertion of lipid tail, depol of cell membranes with K efflux and eventual cell death bacteriocidal, effective agaisnt G+(MRSA(ORSA), enterococci, VRE, VRSA), inactive against G-, not effective in tx of pneumonia, IV, can accumulate in renal insufficiency, AE- constipation, nausea, head ache, insomnia, elevated creatinine phosphokiases(recommended to discontinue coadmin of statins), tx of complciated skin/structure infections caused by suseptible S aurues, recommended tx for severe infections caused by MRSA or VRE
|
|
|
Bacitracin
|
no cross resistance, interferse in late cell wall syntehsis, effective against G+ organism, marked nephrotoxicity, mainly topical
|
|
|
Fosfomycin
|
inhibits cytoplasmic enzyme enolpyruvate transferase in early stage of cell wall syntehsis , active against G+ and G- organisms, oral, used for tx of uncomplicated lower UTIs
|
|
|
Protein Synthesis Inhibitorss
|
mostly bacteristatic, tetracyclines, glycoclines, aminoglycosides, macrolides, chloramphenicol, clindamycin, stretogramins, linezolid
|
|
|
Tetracyclines
|
AE- gastric effects, superinfections, discoloation and hypolasia of teeth, stuning of growht, teratogenic, fetal hepatoxicity, photosensitization, diziness and vertigo
|
|
|
Tetracycline
|
docycline, minocyline, tetracycline, broad specrum, bacteriostatic, activity agaisnt aerobic and anaerobic g+ and g- organisms, MOA- entry via passive diffusion and erngy depedent transoprt, concentrate drug intracellualryy, binds reversiby to 30S subunti of ribosome, prevents binding of aminoacyl tRNA ,DOC for chlamydia, mycoplasma pneumona, lyme disease, cholera, anthrax prophylaxis, rickettsia, used for H pyorli, malaria prophyslaixs, tx of plague, tularemia, brucellosis , variable oral absorption , PK- excreted in urine , except doxycline(bile) resistance- impaired influx or icnreased efflux by active protein pump, production of proteins that interefere with binding of ribosome, enzymatic activation, therapetuc use- secere acne and rosacea, community acquired penumonia, RTI, middle ear, UTI, intesine,
|
|
|
Doxycycline
|
prereffered for parental amdin and good choice for STDs and prostatits, tetracyle fam , secreted via bile
|
|
|
Minocycline
|
reaches high conetration I nall secretions(useful for eradication of menigococcal carrier state
|
|
|
Glycylcylines
|
tigecline, structurally simialr to tetracycline, broad spectrum against multidrug resistant g+ , some g- and anaerobic organisms
|
|
|
Tigecycline
|
little resistance, not subject to same resistant mechansims as tetracyclines(exceptions- efflux pumps of proteis and pseudomonas species), tx of complciated skin, sof tissue and intraabdominal infections
|
|
|
Aminoglycosides- amikacin, gentamicin, tobramycin, streptomycin, neomycin, netilmycin
|
spectrum- aerobic G-,app- empric for serious infections(septicemia, nosocomia RTI, uncomplicated UTIs, endocarditis), DOC for infective endocarditis in combo with pencillin or vancomycin, PK- parenteral admin, once daily, high levels in renal cortex and inner ear , AE- otoxocity, nephrotxic, neuromusciar blockate(CI in MG), pregnancy- category D
|
|
|
Streptomycin
|
first like drug, used for drug resistant TBs, use in combo in life threathening compiclaiotns with meinigits, miliaryspread, severe organ TB
|
|
|
Macrolides- erythromycin, clarithromycin, azitrhomycin, telithromycin
|
app- tx of upper respiratory tract and soft tissue infections(staph, H infleunza, S pneumonia, enterococci), used in empiric therapy of community acquired penumonia(outpt and in combo with B lactam for inpts), common substitude for pts with pencillin allergy, g+, bacteriostatic, reversibly binds to 50S subunit inhibiting translocation, binding site indeintal or close to clindamycin and chloramphenicol, resistance- reduced membrane permability or acrice efflux, production of esertase that hdyrozlye durgs, modifivation of ribosomal binding site by chromosomal mutation or by a methylase , complete cross resistance between ertythromycin, azithromycin, and clarithromycin, partial corss resistance with clindamycin and streptogramins , g+ bacterila, specturm wider than pencillins, azirthrmyic, clarhtriomyic and terlinoy borader than erthmymycin , PK- clarothriphycin, azithro, terliit- oral, longer half life, icnreased bioavi to ertthromycin, azithro, telrit- greater tissue, CYP450 inhinitio
|
|
|
Dalfopristin/Quinupristin
|
given as combo(synergistic to have bacerticidal action) long post antibiotic effect, MOA- bind to sperate sites on 50s bacterial ribosome, reisstance is uncommon , spectrum- g+ cocci, MDR(streptococci, PRSP, MRSA, Efaceium, app- restricted tx of infections caused by drug resistant staph or VRE, PK- IV, penetrates macrophages and polymorphonucleocytes, inhibitor of CYP3A4, AE- infsuion related(venous irristaiton, atrhaliga and myalgia), GI effects, CNS effects(HA and pain)
|
|
|
Chloramphenicol
|
potent inhibitor of protein syntehsis, broad spectrum(aerobic and anaerboci g+ and g- organisms, bacteriostatic, toxicity limits use of life threatneing infections with no alternatives, MOA- enters via active transport process, binds reversily to 50S ribosomal subunit(site adjacent to site of action of macrolides and clindamycin, can inhibit protein syntehsis in mitochondrial ribosomes(bone marrow toxicity), resistance- presence of fractor that code for chloramphenicol acetyltransferase(inactivates drug) , changes in membrane permeability, spectrum- very broad, against g+ and g-, including rickettsae and anaerboes, N meningitis, H influenza, salmonella and bacteroides, never given systematically for minor infecitons, App- sierous infections resistant to less toxic drugs, when its penetrabiltiy to site of infection is clinically superior to other drugs, activity against many VRE, topical tx for ear and eye infections, PK- oval, IV or tpical, wide distrubtion, inhibits hepatic oxidases(3A4 and 2C9) , AE- GI distress, bone marrow depression( dose related reversible depression, severe irreversible aplastic anemia), grey baby syndrome(cyanosis)
|
|
|
Clindamycin
|
MOA-same as macrolides, mainly bacteriostatic, primary used against g+ anaerobic bacteria(including bacteroides) . Resistance- mutation of ribosomal receptor site, modification of receptor, enzymatic inactivation of drug, g- aerobes and enterococci- intrisically resistant, corss resistant with macrolides, APP- skin and soft tissue infections(strep and staph, MRSA), anaerobci infections(bacteroides), in combo with primaquine as alternative to PCP , in combo with pyrimethamine as alternative in toxoplasmosis of brain , app- prophylaxis of endocarditis in valvulvar pts allergic to pencillin , PK- oral or IV, good penetration including abscesses and bones , AE- GI irritant, potentially fatal C difficle, skin rashes, neutropenia and impaired liver ufnction
|
|
|
Linezolid
|
bacteriostatic(cidial agaisnt streptococcal and clostrodium difficile), MOA- inhibits formation of 70s initation ocmplex, binds the unique site on 23 s ribosomal RNA of 50s subunit, spectrum- most g+ org(staph, strep, enterococci, coryne,listeria), moderate against mycobacerium, app- tx of MDR infecitons, reistance- decreased binding to target site, no cross resistance twith other drugs, CI- reversible non selective inhibitor of MAOI-->potential to interact with adrenergic and serotonergic drugs , PK- oral, widely distributed, weak irreversible inhibitor of MAO
|
|
|
Fluoroquinilones
|
affects nuclkeic acid, MOA- broad spec, bacteriocidal, enter bacterium via porins, inhibit bacterial DNA replciation via interference with topoimerase II(DNA gyrase) and IV
|
|
|
Nalidixic acid
|
1st gen fluoroquinone, uncomplciated UTIs , g- activity
|
|
|
Ciprofloxacin
|
2nd generation fluoroquinilone, travelers diarrea, p aueriginoasa, prophylaxis agaisnt meninigits, alterative to cefritraxone and rifampin , synergistic with B lactams, expanded g- and some g+, atypicals , resistance- in C diffice, C jejuni, gonoccoci, g+ cocci, P auerigonas and serratia, due to chromosam muatiosn that encode subuntis of DNA gyrase, and topo IV, regulate expression of efflux pumps, cross resistance
|
|
|
Levofloxacin
|
3rd generation fluoroquinilone, prostatitis(Ecoli), STDs(not syphulis), skin infections, acute sinusitis, bronchitis, TB, communpty acwuired pheumonia (first line failed, comorbity, in pt) , expanded g-, imoproves with activity, g_ and atypical organism, excellent against S pneumonia , improves gram+ and anaerobic activity
|
|
|
Moxifloxacin, gemifoxacin
|
4th generation fluoroquinolinw, community acquired pneumonai (first line failed, comorbity, in pt)
|
|
|
Sulfonamides-sufisozole, suflametooxazole, sulfadoxine, sulfacetamide, sufadiaze, sulfaxalazine
|
affects nucleuc acid, sturctural analog of PABA, bacteriostatic against G+ and G- organisms MOA- competes with PABA and blocks dihydropertroate synthase, inhbits bacterial folic acid syntehis, compeitive inhibitor of dihydropteoate synthase, App- topical agents for ocular and burn infections, simple UTI oral agent, ulcerative coilitis, enteritis, IBD DI- warfarin, phenytoin, mehtotrexate increased plasma levels , AE- kenicterus(less an 2 mo, comes with bilirubin for binding sites on albumin), crystallura(nephrotxoci), GI distress, fever, rsah, photosensitivty, hyersernsity, hematpoeic distrubnces (G6PD) , PK- oral or topical, can accumulate in renal failure, acetylated in liver, can lead to aciditic pH- kideny damage , Resistance- alterd dihydropteroate synthase, decreased cellular permeability, enhanced PABA production, decreased intracellular drug accumulation
|
|
|
Trimethoprim
|
affects nucleic acid, MOA- potent inhibitor of bacterial dihidrofolate reductase, inhibits purine, pyrimidine and aa syntehsis, similar to sulfamethoxazole(20-50X more potent), app- UTIs, bacterial prostitis and vaginitis, PK- kidneys, high conc in prostatic and vaginal fluids, AE- antifolate effects(CI in pregnancy), skin rash, pruritis
|
|
|
Co-trimoxazole
|
App- uncomplicated UTIs, PCP(DOC), norcardiosis and toxopolasmosis(DOC), respiratory, ear, and sinus infections(H influenza and M cartarrhalis) PK- oral, IV, well distributed even in CSF, AE- CI in opregn(first term), dermatologic, GI, hematolgic, AIDS
|
|
|
Metronidazole
|
anitmicrobial, amecide, antiprotozoal, aitivity agaisnt bacteroides and clorhstridium, bacteriocidalMOA- anaerobic conditions, reductive biocactication of nitro group by ferredoxin, forms cytotoxic protducts that interferences with nucelic acid syntehsis App- C difficile DOC, anaerobic or mixed intra abd infections, vagintis(tricomonas, bacterial vaginosis, g vaginalis), brain abscess, H yplori comboAE- disulfiram like effect, not advied in first term, GI irritant, stomatitis, peripheral neuropahty, HA, dark coloration of urine, leukopenia, dizzness, ataxia, opportunistic fungal nfections , PK- oral, IV, topical, wide distribution(including CSF, hepatic metabolism
|
|
|
nitrofuratoin
|
urinary antiseptic, bacteriocidal and bacteriostatis, G+ and G-, PK- rapid elimiation(adequate levels in urine), AE- anorexia, nausea and vomting, nueropatheis, hemolytic anemia(G6Pdef) , MOA- reduction of this drug by bacteria in urine, reactice intermeidates that damage bacerial DNA, slow emergenice of resistance and no cross resistance
|
|
|
ANTIMYCOBACTERIALS
|
|
|
|
Amikacin
|
2nd line TB, alternative, used for streptomyic or MDR strains, AE- teratogenic, same as streptomycin
|
|
|
Levofloxacin
|
2nd line TB, alternative,use against lifrst line drug resistant, only use in combo, AE- teratogenic
|
|
|
Clofazimine
|
leprosy drug, AE- red brown discoloation of skin, GI irritaiton, eosinophilic enteritis, NO erythema nodosum, Details- phenazine dye, binds to DNA and inhibits replication, redox properties may generate cytotoxic oxygen radicals, bactericidal to M leprae
|
|
|
Cycloserine
|
|
|
|
Dapsone
|
leprosy drug, strucutally related to sufonamides, bacteriostatic, inhibits folate syntehssi(dihidropteoraoate synthetase inhibition) , also used in tx of PCP in HIV +, high levels in skin and well absprted, acedapsone- repository form, AE- hemolysis, erythemia nodosum leprosum(tx with corticosteroid or thalidomide) , AE- GI irritation, fever, hepatitis, methemglobinemia, CYP inhibitor
|
|
|
Ethambutol
|
first line agent for tx of TB, M. TB and M. kansassi, inhibits arabinosyl trasnferases, use in cobo with pyrazinamdine, isoniazid and rifampin, dose dependent visual disturbances, head ache, confusion, hyperuricemia, peripheral neuritis, safe in pregnacy , resistance- if used alone(mutations in emb gene), well absorrbed orally including CSF, large fraction eliminated unchanged in urine
|
|
|
Ethionamide
|
|
|
|
Isoniazid
|
synthetic analog of pyridoxine, first line agent, most poetneti of antitubercular drugs, part of combo therapy, sole drug in tx of latent infection, MOA- prodrug(activated by mycobacterial catalase peroxidase-KatG), targets enzymes invovled in mycolic acid- enoyl acyl carrier protein reductase, B ketoacyl ACP synthase(KasA), spectrum- bacteriostatic effects against bacilli in stationary phase, bactericidal against rapidly diving bacilli, specific for M.tb, used alone- resistace mermgges, Resistance- mutation of deletion of KatG, mutation of acyl carrier proteins, overexpression of inhA, cross rxn between other antiTB drugs do not occur, PK- oral, IV, and IM, diffuses into all body fluids, cells and caseious material, undergoes N acetylation , AE- peripheral neruitis, hepatoxicity, CYP 450 inhibiotr, lupus like syndrome, safe in pregancy, risk of hepatits icnreases
|
|
|
Pyrazinamide
|
first line agent, combo with isoniazid, rifampin and ethambutol, enzymatically hydrolzyed to active pyrazinoic acid, resistant strains lack pyrazanidimase or have increased effluc of drug, PK- well absorbed orally and well distructied(indcusing CSF), renal and hepatic isuf, adjsut dosage, AE- non gouty polyathralgia, acute gouty arhtiits(rare), hyeruricemia, hepatotoxicity, myalgia, GI irritation, porphyia, rash, photosensitiy, recommended for use in pregnancy when benefits outweigs risks
|
|
|
Rifabutin
|
preferefed for HIV pts, leser eeffects on CYP, rifampin substitude if intolerant, TB tx
|
|
|
Rifampin
|
leprosy, latent TB in INH inotlerant pts, prophylaxis for meningitst, MRSA with vancomycin , PK- oral and parenteal, well distributed, enterohepatic cycling, excreted into feces, strong CYP 450 inducer , resistance- point mutations in rpoB, gene for B subunit of RNA polymerase, decfreased affinity for bacterial DNA dep RNA pol for the drug, decreased permeability , MOA- blcoks transcirpiton by bidning to B subunit of bacterial DNA dep RNA pol-->inhibition of RNA syntehsis
|
|
|
Foscarnet
|
" 1) Doenst require phosphoryaltion
|
|
|
Oseltamivir and Zamamivir
|
" i) Slow down symptoms but not blocking effect on cell ii) Effective against both A and B iii) DOC for flu iv) MOA- neuroaminase allows the cleavage of receptor to infection other cells, the drug , analog/ihibitor of sialic acid substrate for neuroaminidase, inhibit release of virus v) Oseltamivir- oral, Zanamivir- inhale, intrasal vi) AE- oseltamavri(GI issues, better with food), zanamivir(airway irritation, avoid with COPD) vii) Resistance- less infective and virulent neuromanse mutations
|
|
|
Amantadine and Rimantidine
|
" 2) Only on infleunza A 3) Not recommended by first line tx 4) Issues with resistance 5) MOA- blocks viral membrane protein, M2, needed for fusion of viral with cell membrane to endosome(needed for viral uncoating) 6) PK- widely distributed, BBB(amantidine), rimanditine( not metab a lot, exctreted through urine) 7) AE- Aminitidie(CNS- insombina, dizziness, ataxia), rimantidine- fewer problems 8) CI- psychiatic pts, cerebral atehrosclerpis, pregnancy 9) Resistance- huge , GI inotelrase seen with both
|
|
|
Ribavirin
|
" 1) A and B, C 2) MOA- prevents viral mRNA capping , inhibition of DNA dep RNA pol resulting in hihbition of viral preotin synthesis
|
|
|
Interferons
|
" 1) Naturally occuring inducible glycoportiens and cytokins 2) MOA- innate immue resposne, PKR, no directio action, inhibit RNA and DNA syntehsis by activating/inducing protein expression that inhibit virus infection 3) PK- natural proteins, give IV, short half life, PEGylated extends haf life 4) AE- flu like, fatigue mental depression 5) DI- hepatic drug metab, toxic accumuation of theophylline 6) Potentiate zidovudine indlcuded myelow 7) App- inferferon B- MS
|
|
|
Interferon α, β, γ
|
alpha- HCV, HBV, condyloma acumminata, hairy cell lukemia, kaposis sarcoma, beta- MS
|
|
|
Adefovir
|
" 1) AE- discitonues, severe exacerbartion of heptits
|
|
|
Entecavir
|
" 1) Laminvudant renstant HBV and HIV 2) Blocking polymeasr 3) Montior discutnation-> severe hepatitc , phosphoralted form competes with natural substrates for viral polymerase, inhibition of polymerase blocks RT actictiy, renal function should be assencted
|
|
|
Lamivudine
|
"
|
|
|
Telbivudine
|
only effective against HBV, phosphorylated form competes with natural substrates for viral polymerase, oral once a day admin, eliminated unchnaged in ruine
|
|
|
Acyclovir
|
" 1) Guanicine analog 2) HSV type I and 2, VZV, HSV4(EBV) 3) Does NOT work with CMV 4) DOC in HSV encephalitis 5) Used for prophlactic in immunocomplrised and for gentical herpes infevtion i) Compltes with dGTP, inhibitions of DNA syntehsis 8) Resistanc i) Rare, cross resistance can occur ii) Altered or defincient thymidinine kinase 9) Kinase i) Oral- valvycovir better 10) AE- depents on route- topcial(irritation) oral(HA, diarrhea, nacusea), IV- acute renal failure
|
|
|
Cidofovir
|
" 1) Not phosphorylated by viral kinases 2) requires Activation of host cell kinases 3) Effective against HSV and gangliocylcovir HSV 4) Resistance- mutation in DNA pol 5) PK- IV, topical 6) AE- nephrotoxic MOA- DNA chain terminnator and DNA pol inhibitor, PK- IV, intravitreal and topical, coadministered with probenecid(blocks renal tubular secretion)
|
|
|
Famciclovir and Penciciclovir
|
" 1) Famciclovir- prodrug of penciclovir 2) Active agaisnt HSV1, 2, VZV 3) MOA- Monophosphorylated by viral thymidine kinase, inhibits HSV DNA pol/chain terminator 4) PK- topical(PENCICLOVIR) 5) Resistance- low 6) PK- penci- topical, famcli- oral , AE- HA, nausea, diarrhea
|
|
|
Ganciclovir
|
" 1) Guanisien analog 2) More active against CMV 3) DOC for CMV retinit and CMV prolphylaxis 4) MOA- phosphorylated by Viral UL97 and cell pkinases , DNA chain terminatory and DNA pol inhibitor 5) Resistance- mutation in UL97(reduced intracellular phospitrlarion), mutation in viral DNA pol 6) PK- IV, urine 7) CI- pregnacy 8) AE- myelosupresison, dose dep neutropenia
|
|
|
Trifluridine
|
effective against HSV1,2 and vaccina virus, DOC for HSV heratoconjunctivitis and epithelial kertarits, MOA- triphophate form incorporated into viral DNA causing fragmentation, PK- opthalmuc ointment(too toxic for systemic) , AE- eye irritation nad palpebral edema , thymidine analog
|
|
|
Valcyclovir
|
Better oral bioltviliy, Prodrug of acyclovir
|
|
|
Vidarabine
|
adenoside analog 1) Limit to tx of immunocompromoed with herpetic and vaccinal kertatits and HSV keratoconjunctive 2) Useful agaisnt HSV, CMV, VZV 3) PK- opthalmic ointment AE- keratitis, pain, photophobia. MOA- triphosphate form ihibits viral DNA syn
|
|
|
Fomivirsen
|
" 1) Binds to mRNA 2) PK- intraviterally 3)Binds to CMV mRNA bloking mRNA translation 4) AE- changes in vision , used when other therparites of CMV retinitis fail, MOA- binds to CMV mRNA blocking viral mRNA translation PK- intravitreally, AE- iritis, viritis, changes in vision and increases in intraocular presusre
|
|
|
Foscarnet
|
" 1) Doenst require phosphoryaltion 2) Used for CMV retinitis, acyclovir reistant HSV and CMV resitin, ganclicovir resitance 3) MOA- ihibtals DNA 4) AE- nephrotoxic and hypocalcemia, organic analog of inaorgangic pyrophosphate , MOA- selectively inhiniys birus specific DNA pol and RT, resistance- point mutations in polymerase, PK- IV, AE- anemia, nausea, fever, CNS(hallicuonations, seziaures, HA
|
|
|
chloramphenicol
|
bone marrow toxicity
|
|
|
chloramphenicol
|
inhibits hepatic oxidases
|
|
|
chloramphenicol
|
broad spectrum- G+ and G-(N menin, H inf, Salmonella, bacteroides)
|
|
|
chloramphenicol
|
grey baby syn
|
|
|
bacteroides
|
chloramphenicol, clindamycin, metronidazole,
|
|
|
Clindamycin
|
PCP alternative
|
|
|
Clindamycin
|
skin and soft tissue infections
|
|
|
Clindamycin
|
prophylaxis of endocarditis in pts allergic to pencillin
|
|
|
fluoroquinilones
|
theophylline, NSAIDs, corticosteroids increase toxicity of this
|
|
|
ok in pregnancy
|
Isoniazid, Rifampin, Ethampbutol, amoxicillin, tetracycline , tigecycline, aminoglycoside
|
|
|
CI in pregnancy
|
fluoroquiniline , trimethoprim, cotrimoxazole, Nitrofurantoin,
|
|
|
fluoroquinilones
|
connective tissue problems , QT prolognation, superinfections
|
|
|
Linezolid
|
weak irreversible inhibitor of MAO
|
|
|
Naficillin
|
excreted in bile
|
|
|
Pencillin
|
AE- hypersnesicity
|
|
|
Ampicillin, Amoxicillin
|
maculopapular rash
|
|
|
intersittial npehritis
|
methicillin
|
|
|
pseudomembrane colitis
|
ampicillin
|
|
|
ticacillin
|
hematologic toxicity
|
|
|
naficillin
|
neutropenia
|
|
|
oxacillin
|
hepatitis
|
|
|
cefazolin
|
DOC for surgical prophylaxis
|
|
|
2nd gen (cefaclor, cefoxitin, cefotetan, cefamandole)
|
sinusiits, otitis, LRTI
|
|
|
cofetetan and cefoxitin
|
propylasis and therapy for abd and pelvic cavitiy infections
|
|
|
ceftriaxone (3)
|
DOC for pencillin resistant gonorreal
|
|
|
ceftriaxone (3)
|
DOC for meningitis due to ampliccilin H infleunza
|
|
|
ceftriaxone (3)
|
tx of lyme disease(CNS or joint)
|
|
|
ceftriaxone (3)
|
prophylaxis of meninigits in exposed individuals
|
|
|
cefoperazone+ceftazidime (3)
|
P aeuriginoas
|
|
|
cefepime (4)
|
parental only
|
|
|
cephalosporin
|
minor infection to pencilin pts are given?
|
|
|
carbepens
|
DOC for enterobacter
|
|
|
|
DOC for extended spectrum B lactamase production G-
|
|
|
aztreonam
|
g negative rods only
|
|
|
vancomycin
|
g positive bacteiral only
|
|
|
vancomycin
|
red man sydnrome
|
|
|
daptomycin
|
tx of complicated skin/sturcutre infections caused by S aurues
|
|
|
daptomycin
|
elevated creatineine phosphokinases
|
|
|
bacitracin
|
topical due to marked nephrotoxicity
|
|
|
fosfomycin
|
tx for uncomplicated UTIs
|
|
|
tetracycline
|
severe acne and rosaciea
|
|
|
tetracycline
|
community acquired pnumonia out pts
|
|
|
tetracycline
|
syhilis in pts allergic to penicillin
|
|
|
tetracycline
|
DOC for chlamydia
|
|
|
tetracycline
|
DOC for mycoplasma
|
|
|
tetracycline
|
DOC for lyme disease
|
|
|
tetracycline
|
DOC for cholera
|
|
|
tetracycline
|
DOC for anthrax propylaixs
|
|
|
tetracycline
|
DOC for rickettsia
|
|
|
docycline
|
STDs and prostaticis
|
|
|
minocycline
|
eradication of meningococcal carrier state
|
|
|
clofazime
|
red brown discloration of skin
|
|
|
dapsone
|
erythema nodosum leprosum
|
|
|
pyrazinamide
|
nongouty polyathralgia
|
|
|
ethambutol
|
dose dependent visual disturbances
|
|
|
isoniazid
|
peripheral neuritis
|
|
|
pencillin G
|
doc for syphilis
|
|
|
pencillin G
|
DOC for strep infections
|
|
|
pencillin G
|
DOC in suspetible pnumocooi
|
|
|
pencillins
|
secondary infection of vaginal candiadisis
|
|
|
cefamandole, cefoperazone, cefotetam
|
hypoprothrombineia, disulfiram like rxns
|
|
|
vancomycin
|
resistance- modification of D-ala-Dala
|
|
|
tetracycline
|
tx of plague, tularemia, brucellosis
|
|
|
aminoglycosides
|
once daily dosing
|
|
|
aminoglycosides
|
amikacin, gentamycin, tobramycin, streptomycin, neopmycin, netilimicin
|
|
|
aminoglycosides
|
otoxic and nephrotoxic
|
|
|
macrolides
|
erythromycin, clarithromycin, azithromycin, telitrhomycin
|
|
|
telithromycin
|
fatal hepatoxicity
|
|
|
chloramphenicol
|
topical treatment of ear and eye infections
|
|
|
moxifloxin, gemifloxacin
|
community acquired pnumonia
|
|
|
levoflaxcin
|
prostitis, STDs
|
|
|
Ciporfolxin
|
travelers diarrhea, meningiits prophylaxis
|
|
|
sulfanamides
|
inhbit dihydropetroate syntahse
|
|
|
trimethoprim
|
inhibts didhyrofolate reductase
|
|
|
suflonamides
|
UC, entertitis IBD
|
|
|
sulfanamides
|
crystalluria+kernicterus
|
|
|
trimethoprim
|
antifolate effects
|
|
|
cotrimoxazole
|
DOC for PCP
|
|
|
cotrimoxazole
|
DOC for norcaoidsosi and toxoplasmosis
|
|
|
metronidazole
|
brain abscesses
|
|
|
metronidazole
|
disufiram like effect
|
|
|
fluroquinlones
|
tendon rupture/damange in fetus
|
|
|
neitrofurantoin
|
hemolytic anemia in fetus
|
|
|
aminoglycosides
|
damange to VIII cranial nerve
|
|
|
metronidazole or vancomycin
|
tx for c difficiline
|
|
|
metronidazole
|
DOC for tricamonas
|
|
|
amibicllin
|
DOC for proteus
|
|
|
docycline
|
DOC for rickettsia
|
|
|
oseltamivir, zanamivir
|
neuraminidase inhibitors
|
|
|
zanamivir
|
airway irritaiton
|
|
|
amantidine, rimatadine
|
ion channel blockers
|
|
|
ribavarin
|
prevents viral mRNA capping
|
|
|
ribavarin
|
pregenacy category X
|
|
|
interferons
|
flu like, fatigue mental depression- AE
|
|
|
interferon alpha
|
HCV, HBC, condyloma acumnata, hairy cell, kapisis
|
|
|
interferon B
|
MS
|
|
|
adefovir
|
severe exacerbation of hepatitis
|
|
|
ganciclovir
|
DOC for CMV retitnitis and CMV prophylaxis in immunocomprised
|
|
|
cidofovir
|
requires activation by host cell kinase
|
|
|
trifuluridine
|
DOC for HSV keratoconjunctivitis and recurrent epithelial keratitis
|
|
|
fomivirsen
|
use for CMV when other therapies for CMV fail
|
|
|
foscarnet
|
nephtrotoxicity and hypocalcemia
|
|
|
amantidine, rimatadine
|
inhibit uncoating by blocking M2 proton channel
|
|
|
ursodiol
|
dissovles gall stones in bile ducts
|
|
|
pancreatic enzymes
|
tx for chronic pancreatitis, maabsortion syndrome
|
|
|
diphenoxylate and loperamidie
|
toxic megacolon
|
|
|
droperidon haloperidol , prochlorperazine , metocloprimonade
|
blcoks D2 recetors
|
|
|
lactulose
|
tx of heaptic encephalotpahty that prvents hyperammonia
|
|
|
Metaclorpomaide
|
CI in Parkinsons
|
|
|
Metaclorpomaide
|
diabetic gastroperises, anti emetic and GERD
|
|
|
pirenzepine and dicylcomine
|
muscarinic antagonists used for IBS
|
|
|
misoprostol
|
prevention of gastric ulcers induced by NSAIDs
|
|
|
sucralfate
|
requires acid pH for plymeraziation
|
|
|
cimetidine
|
gynecomastia, galtorreha, reduced sperm count
|
|
|
calcrium carbomnate
|
kidney stoens
|
|
|
aluminum hdyroxide
|
constipation
|
|
|
MgOH
|
diarrhea
|
|
|
Artemisinins
|
" derived from quinghaosu plant, artesunate- all mentals of PK, dihydroatenemism- oral only, coartem- artemether and lumenfantrine1) MOA- binding iron, breaking down peroxide bridges and genreates free radicals that damage parasite proteins 2) PK- short half life 3) AE- remarkably safe, neurotoxity QT prolognation in high doeses, can be used in 2nd and 3rd tripmester of pregnancy , app- artemisinin- tx of severe multi drug resistant falciparum malaria(IV), no effect on hepatic stages, should not be used as single agent to protect agaisnt resistance,
|
|
|
Atovaquone
|
" 1) Malarone- atavaquone and proguanil 2) MOA- oral 3) AE- Category C 4) Chemoprophylaxis- resistance, app- malaroine- tx and prophylaxis of p falciparum , antimalarial action- agaisnt tissue and erthrycytic schizons, chemoprorpylaxis discontonued post 1 w
|
|
|
Chloroquine
|
DOC for tx and prophylaxis of all pviax and p ovale malaria 1) Most places resistnace 2) Highly effective for blood shintocinde 3) MOA- prevents biocrystallization of hemoglobin breakdown product heme to non toxic hemozoin 4) PK- oral 5) Resistance- very common, mutations in PfCT and purative transporter CI- psoriasis and retinal abnormaltieis, app- DOC in tx of non falciparum and sensitive uncomplciated falciparum malaria, preferred chemophroprylyac in areas w/o resistant falciparum malaria
|
|
|
Clindamycin
|
alternative to doxycylcone for antimalaria
|
|
|
Doxycycline
|
active against etrhyrocytic shizonts of all human paraized, NOT active agaisnt liver stage, app- doxy and quinine-->tx of severe f. malaria, used to complete tx couse after malaria is treated with quinine, quinidine or artesunate , AE- photosensitivty, discoloration and hypoplasia of teeth and stunting og growth, AE- pregnancy or before age 8, cateogry D
|
|
|
Halofantrine
|
effective against erthrylcytic stage of all paraized, AE- teratogenic, irregular absoriton and cardiac toxicity
|
|
|
Lumefantrine
|
effective agaisnt eyrthoicytic stages of all parasites, fixed dose, minor QT prolognaiton, well togerlated
|
|
|
Mefloquine
|
" 1) Againt chlorroquine resistent 2) App- chemophorylysis for preg women, chemoprhorlyalsi in areas 3) In combo with artesunate for uncompicated amalai 4) PK- oral, long hafe life, once weekly 5) AE- psychiatric problems, vomting, dizzness, epigastric pain, diarrhea, leukocytosis, thromboscitoma 6) CI- hx of psychiatric issues, mOA- destruction of asexual blood forms of malarial pathogens , resistance0 uncommon
|
|
|
inhibitos of folate sysnthesis
|
pyrimethamine, proguanil, sulfadoxine, app- chemoprophylaxis, intermittent preventive therpay, tx of chloroquine resistant falciparum malaria, DO not use for severe malaria(pyrimethamine-sulfadoxine
|
|
|
Primaquine
|
1) DOC for eradication for liver form of P vivax AE- hemolysis in G6P def, CI- rpregnancy , used for chemoprophylais all trains, APP- acute vivax and ovale, terminal proxlypais of vivax and ovale, chemoprophylaxis, PK- oral, resistance- repeated or increased dose ,
|
|
|
Proguanil and
|
" 1) Inhibitors of folate sysmteiss 2) MOA- inhibit plasmodial dihydrofolate reductase, safe in pregnacy, proguianil- mouth ulcers, alopecia(AE), some activity against hepatic forms , progionanisl and pyrimethaine- ihibit plasmodial dihydrofolate reductase
|
|
|
Quinidine and quininine
|
" 1) First like therapies for severe falciparum disease2) Resistance is uncommon but increasing 3) Cinchoma tree bark 4) Ap= parental tx of severe falciularpum , oral tx of falciparum malaria 5) Quinine- oral, quinidine- IV 6) AE- cinchonism, hyerpesentivity, hematologic abodnomalities, hypoglycemia, uterine contractions , black water fever(blood in urine), ECH abnormaltieis and severe hypotension 7) CI- severe side effects, visual issues, cardiac issuesm don’t use with mefloquine, category C FDA, MOA- depresses O2 uptake and carb metabolism, disrupting parasite replication and transcirption
|
|
|
Sulfadoxine
|
AE- hematologic, GI, CNS, dermatoloc, renal toxicity, MOA- inhibitors of folate syntehsis , weakly active against erythrocytic shizonts , ihibits dihdyroptreate synthase
|
|
|
Pyrimethamine
|
AE( erythema multiforme, steven johnsone syndrome, toxic epidermal necrolysis, MOA- inhibitors of folate syntehsis
|
|
|
Amphotericin B
|
"polyene antiboitic, taken by fungal cells via cytosine permase, topical and used for cutaneous candiazis , 1) Long chain of hydrocarbons 2) Can get into the lipid layer of fungal cell membrane 3) PK- IV only i) Pentration into CSF low ii) Intrathecal- menigeal iii) Highly insoluble- deoxycholate suspention iv) Safe in pregnancy 4) Uses- broad spec and fungicial, life threatning fungal infections, continue therpay with azole 5) AE- infusion related(fever, chills, spasms, vomiting, HA, hypotension), slower toxicity(renal toxoicity, anemia, seizures and neurological damage) 6) Nephrotoxiciy is less ccommon with lipid formaitons , MOA- convertals intracellular to 5 fulurouraci than to 5udUMP which inhibits thymydilate synthetase, blcks sysntehsis of dTMP, inhibits protein sysntehsis
|
|
|
Nystatin
|
topical for superficial mycosis, polyene macroline, smimilar to amph B, AE- too toxic for IV, app- candiasis, PK- cutanous, vag, oral,
|
|
|
azoles
|
MOA- cyp 450 enzyme 14 alpha sterol demythlase catalzyes conversion of lanosterol to ergosterol, inubit enzyme, reduces ergestrol sysntehsis, disrupms membrane function and increases permeability, greater affinity for cyp450
|
|
|
Ketoconazole
|
" Inhibts p450 enzymes, Decrease testespotne levels- gynecomastia, decreased lipido, loss of potency , high doses inhibit adrenal steroid sysntheiss and decrease plasma cortisol cocnetrations , best absorbed at low gastric pH- antacids, H2B, PPI interefere with absoprtion of ketoconazole, poor CSF penetration
|
|
|
Fluconazole
|
" CSF penetration , Oral bioablaitor, Inhibitor of CYP2C9- increase plasma pheytoin, ziduno, DOC in esophageal, oropharyal, vaginal or urinary candiasis, invasive candida infections , DOC for toxoidosisis, DOC for consolidation of cryptocolloc memingisit after amph B- immunocompromised, DOC for initial and secodnary propylaxis agaisnt cryptoccoal , Not good for aspergillus or fillameuns
|
|
|
Itraconazole
|
" Strstrong inhibitor of CYP3A4, and metalzied by CYP3A4, AE- fatal arryhtmias when given with cisaprine or quinidine,Poor bioavailbity , Absortption reduced by antacids , H2B and antacids , Effective against aspergillus, repleaced by vorincanazole , Toe nail infections , app- Blastomyces, sporothrix, histomasma, dermatophytsis and onhychomoscis
|
|
|
Voriconazole
|
" Visual disturbances , invasive Aspergillus, lots of DI( CYP2C19, CYP2C( and CYP3A4 inhibitors)
|
|
|
Posaconazole
|
mucor (zygomacetes), inhibits CYP3A4, similar to ictranazole
|
|
|
Clotrimazole and miconazole
|
two OTC topcial azoles
|
|
|
Terbinafine
|
AE- NO EFFECT ON P450 systen, HA, taste disturvances, topical cream, tinea cruris and tinea corporis , app- more effective for onchymoysis , allyamine, oral formualtion, MOA- inhibits squalene epoxidase prevents syntehsis of ergosterol, causes accumulation of toxic levels of squalene in fungal cell
|
|
|
Pyrimidine analog
|
|
|
|
Flucytosine
|
1) Pyrimidine antimetabolite 2) Taken by fungal cells via cytosine permease 3) Flucocytosne and amphoteracin B- synergistic 4) Spectrum- narrow, don’t use alone, resistance quickly, give with amph B 5) Serious infections caused by candida or cryotp 6) Result rom metabalism of 5-flurouracil AE- bone marrow toxcitiy
|
|
|
Griseofulvin
|
tx of dermatophytolate, absorption improved with fatty foods, MOA- disrupts mitotic spindle and inhibits mitosis, severe dermatomytosies of skin, hair and nails, AE- Cp450 inducer, including warfarin
|
|
|
Caspofungin
|
enchinocandin,large cyclic peptides linked to long chain fatty acid, active agaisnt candida and aspergillus but not cryptococus neoformans, only IV, inhibts syntsis of B 1-3 D glucans in fungal cell wal, disrupts cell wall and cell death
|
|
|
Co-trimoxazole
|
DOC for PCP, also DOC for prophylaxis in immune compromsied ppl
|
|
|
Clindamycin+primaquine
|
alternative PCP
|
|
|
Dapsone
|
with trimepthpribn, PCP anteraive
|
|
|
Atovaquone
|
PCP alternative
|
|
|
Pentamidine
|
PCP alternative
|
|
|
Prednisone
|
given to mts with moderate to severe diseases for PCP along with other therapy
|
|
|
Metronidazole
|
" ► MOA- reduced by reacting with reduced ferredoxin ► PK- oral, DI , hepatic oxidation and glucornisation(cyp450) ► AE- disulfiram rxn and GI distress, DOC- tx indaive amebiais , app- giardia lamblia, trichomonas vaginalis, anaerobic cocci, anaerobic g- bacilli, combo of H pylori eradication
|
|
|
Tinidazole
|
|
|
|
Diloxanide Furoate
|
" ► Sole agent for asympomtatic amebiasis ► Converted in gut to diloxanine freebase active form
|
|
|
Iodoquinol
|
" One. AE- rash, neurobathy , orally active against luminal trophozoite and cyst forms of E histolytica, long term use should be avoided
|
|
|
Paromomycin
|
" ► Aminoglyccosides► lumnial forms of E histolytica and tapeworm , alternative agent for crypto in AIDS pts ► MOA- 30S ribosome subunit , reduces intestinal piulaiton ► AE- GI distress and diarreha
|
|
|
Chloroquine
|
used in combo with metronizasole and diloxanide furoate, MOA- eliminates trophozoites in liver abscess
|
|
|
Dehydroemetine
|
|
|
|
Emetine and dehydrometine
|
" ► Back up drogs for severe intesital or severe hepatic amebiasis ► PK- IM or SC, slow eplitaiton ► AE- pain at infection site , cardiotoxicity, neuromsuclar wekaness, diziness, rash , MOA- inhibits protein sysntehsis by blocking ribosoma movement along mRNA
|
|
|
Tetracycline
|
|
|
|
Antihelminthics
|
|
|
|
Albendazole
|
" 1) Tx of cestodal infections- cystisercosis and hyatid 2) MOA- miscortuble systentic and glucose uptake 3) PK-oral , rapid sufloxidation
|
|
|
Mebendazole
|
" 1) DOC for whipworm, pinwork , MOA- inhibits formation of helminth microtubules, irreversibly blocks glucose uptake, affected parasits in feces, PK- oral, first pass
|
|
|
Thiabendazole
|
" 1) Larval migrans , strongloides(threatworkm), MOA- microtubular aggregation affected, PK- oral, not soluble in H20 2) Trichonsis
|
|
|
Bithionol
|
" 1) DOC for fasciolosis , alternative drug for pulmoanry paragonimiasis, inhibition of helminths electrol transport chain
|
|
|
Diethylcarbamazine
|
1) DOC for tx of lymphiatic filiaris, loasis, tropical eosinophilia 2) PK- oral,AE- dmange/death of parasite--> fever, malaise, rash, athralgia, HA, leukocysos(common) antihistamine condinistered, MOA- immobilizes microlifilare and makes them suseptible to host defense,
|
|
|
Doxycycline
|
tetracycline antibiotic, good for wurcheria bancrofi, active gain onchocerciais, MOA- acits inidrectly by killing wolbachia bacteria(filiaria sympbiont)
|
|
|
Ivermectin
|
" 1) GABA agonist- diff than human, death due to apralysis due to Cl inflku, PK- oral 2) DOC for ochocercisais, cutaenous larva migrans and strongloides 3) AE- mazotti like rxns with onchocieris(fever, dizziness, somnolences, hypotension) , CI in pregancy, CI in meningitis , DI with barbiduates and benzodiazepines
|
|
|
Niclosamide
|
" 1) 2nd line for cestode 2) Not uusually sicne sicne prazuqantel great 3) Discrupts ADP to ATP 4) Lethal to cestode and not for ova 5) PK- laxatives prior to niclosamide 6) AE- disulfiram effect
|
|
|
Piperazine
|
" 1) Pinworm and round worm 2) MOA- depolaziring, neuromuscular blocker 3) PK- poorly absorbed orally
|
|
|
Praziquantel
|
" 1) DOC for shistosomiasis and trematode and cestode 2) Cysticerosis(but albendazole DOC) 3) MOA- increases cell permabiltiy to Ca -->Paralysis of worm- contracture and paralysis 4) PK- extensive pass first pass metabolsim(CYPs) 5) AE- DI, CI in pregnacy, CI in tx for ocular cysticercosis
|
|
|
Pyrantel Pamoate
|
round worms, pinkwrms and hookworms, MOA- depolarizing nueromusuclar blocker(causes persistent activation of parasites nicotinic receptors by release of acetylcholine and inhibition of cholinerstease), PK- poorly absorbed orally, AE- mild nausea, vomiting, diarrhea
|
