16-ADR, MOA, USE, PRODRUG, RESISTANCE, 45 NOTES TO PG .pdf

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  • 7/26/2019 16-ADR, MOA, USE, PRODRUG, RESISTANCE, 45 NOTES TO PG .pdf

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    45 NOTES TO PG

    Dr. Ankit Yadavendra, M.B.B.S., Dr.V.M.G.M.C., Solapur

    16-ADR MOA USE PRODRUG RESISTANCE

    DRUG-ADR

    ACEI-affect lung&kidn developm, dry cough, angioedema, hyperkalem, ren dysfn

    acetazolamide-metab acidosis, tingling numbness

    actinomycinD(Dactinomycin)-radiation recall phenom

    acyclovir-nephrotox

    adriamycin(doxorubicin)-cardiotoxic, hand foot synd

    alkylat agent-venoocclus ds liver(Rx-defibrotide)

    1adr antag-retrograde ejaculation, miosis

    2adr agonist-depression, anticholinergic, rebound HTN(Rx-phentolamine, tolazoline)

    alosetron-ischemic colitisamantadine-ankle edema, livido reticularis

    aminoglycoside-irrevers ototoxicity(mtDNA), nephrotoxicity

    amiodarone

    Please-Photosensitivity, blue grey Pigmentat skin, Periph neuropathy

    Check-Corneal microdeposition

    PFT-Pulm Fibrosis

    LFT-Liver cirrhosis, pseudoalcoh Liver inj, Mallory hyaline body

    TFT-hypoThy, hyperThy

    amlodipine-ankle edema

    amoxapine-EPS, galactorrhea, NMS, tardive dyskinesia

    amphetamine-addiction, appetite, cardiotoxicity

    amphotericin B-dose limit RTA, AKI, hypokalem, hypomagnesem, anem

    ampicillin, cisapride, mosapride, tegaserod, colchicine, fosfomycin, irinotecan,

    leflunomide-diarrh

    antimetabolite-acidic urine(crystaluria)

    apraclonidine-lid lag, itch, lid dermatitis, follicular conjunctivitis, mydriasis, dry mouth

    aprotinin-death

    atenolol-fatigue

    azathioprine-bone marrow suppression

    2adr agonist-hyperglycemia, hypokalemia, tremor(MC), HR, MI, card arrest, pulm

    edembimatoprost-iris pigmentation, eyelash growth

    bleomycin-pulm fibrosis, HSR, mucocut fibrosis

    bortezomib-periph neuropath

    bosentan, flutamide, lumiracoxib, nefazodone, sitaxentan, stanozolol,

    ximelagatran-hepatotox

    bremelanotide, methergin-HTN

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    bRimOnidINE-ant uveitis, dROwsINEss, headache, allergic blepharoconjunctivitis

    bromocryptine-psychosis, confusion, erythromelalgia

    bupropion- suicidal tendency, wt loss, sz, restlessness, tremor

    busulphan-pulm fibrosis, cataract, gynaecomastia, adr insuff, hyperpigmentation,

    hyperuricemia

    CBZ-hyponatremia, aplastic anemcapecitabine-hand foot mouth synd

    carbenicillin- PLT aggregat

    carbimazole-maculopapular rash(MC), agranulocytosis

    carboplatin-myelosuppression

    carboprost-diarrh(MC), asthma

    carmustine-sustained myelosuppress

    cefoperazone-disulfiram rxn

    ceftazidime-neutropenia, PLT

    cephaloridine-nephrotoxicity

    chloroquine-retinal pigmentation, optic neuritis, lichenoid erupt, szchlorpropamide- PLT

    cisplatin-vomiting, nephrotox(Rx-amifostine), neurotox, ototox, hypokalemia,

    hypomagnesemia, hypocalcemia, hypophosphatemia, sec ca

    clarithromycin-reversible hearing loss

    clofazimine-brown black skin discoloration, icthyosis(crocodile skin/sauroderma)

    clomiphene citrate-hotflush(MC), ovarian cyst, ovarian hyperstimulat synd(

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    disulfiram-nausea, vomiting, headache, flushing, hypotension

    diuretic-oligohydramnios

    dorsolamide-corneal edema

    echothiophate-cataract

    ergot alkaloid-HTN, IHD, ergotism(foot gangrene, Saint Antony fire)

    estrogen-vomiting, ca breast, ca endom, DVT, hep adenoma, cholestat jaundice,migraine

    etanercept-TB reactivation

    Ethambutol-optic neuritis(grEEn)

    ethionamide-hypothy

    ethosuximide- sedat

    etoposide-sec leukemia(early)

    exenatide-nausea

    felbamate-aplastic anem, sever hepatitis

    fenfluramine-ECG abnorm, valvular def, pulm HTN, sudden death

    fibrate-GB stone, pancreatitis, myopathyfingolimod- HR, 1AV node block

    5FU-diarrh(MC), myelosuppress, hand foot synd

    fluoxetine-nausea, vomiting(MC), delayed orgasm, insomnia, anxiety, sweating,

    diarrh, urinary retention

    furosemide-hypomagnesemia

    Gatifloxacin-dysGlycemia

    GnRH agonist-hist release, hot flush, flare up after 12h, nausea, headache, libido,

    hypercholesterolem, osteoporosis, depression

    griseofulvin-disulfiram rxn

    halothane-hepatic necrosis, jaundice

    hCG-ovarian hyperstimulat synd(VEGF)heparin

    A-Alopecia

    B-Blding

    O-Osteoporosis

    U-Urticaria

    T-Thrombocytopenia

    HEpaRin-HypERkalemia

    hydralazine-reflex HR

    hydrochlorothiazide-photosensitivity

    ifosfamide-neurotox, RTAIL2, permetrexed-hand foot synd

    imipenem, loracarbef, procaine penicillin-sz

    ipratropium-dry mouth(MC), bad taste, scratch in trachea, urine retention

    INH-periph neuropathy, neuropsychosis, SLE, hepatotox, shoulder hand synd, RA,

    gynecomastia

    ivabradine-luminous phen(object app bright)

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    lamotrigine-SJS

    l asparaginase-hypercoagulation, hgic pancreatitis

    latanoprost-iris pigmentation, conjunct hyperemia, periocular dermatitis, lth

    eyelash(hypertrichosis), inflammation

    levodopa-visual nonthreatening hallucination, chorea, mydriasis

    Li-hypothy, nephrogenic DI like nephropathy, bn&coarse tremorlignocaine-sz, nystagmus, cardiotox, HSR

    linezolid- PLT, neutropenia

    melphalan-sec ca

    metformin-vitB12 def

    methicillin-interstitial nephritis

    mtx-periph neuropathy, oligospermia/defect oogenesis, acidic urine, hepatotox,

    myelosuppression

    methyldopa-hemolysis in mother

    methysergide-retrolental/orbital fibrosis, retroperit fibrosis, pulm fibrosis

    mexiletine-nausea, tremorMianSerin-sz, Myelosuppress

    minocycline-blue black pigmentation nail

    minoxidil-hirsutism, fluid retention

    Misoprostol-shivering, hyperpyrexia, hyperstimulat, Moebius synd(CNVI,VII palsy)

    Mitomycin-Myelosuppress, HUS, delay bronchospasm

    mitoxantrone-cardiomyopathy

    molindone-wt loss

    montelukast, zafirlukast-headache, eosinophilia, vasculitis

    mycophenolate mofetil-diarrh, vomiting

    Naficillin-Neutropenia

    naloxone-HTN, pulm edema, ventr dysrrhythmianaproxen-pseudoporphyria

    nitrate-throbbing headache, hypotension, tolerance(Monday morning headache),

    MethHbemia, rash

    nitrofurantoin-nausea, vomiting, coffee colour urine, disulfiram rxn, pulm fibrosis

    nitrosourea-delayed myelosuppress

    octreotide-GB stone, vitB12 def

    olanzapine-stroke, sedation, wt gain(max), DM

    omeprazole-carcinoid tm in rat

    ondansetron-headache

    IA antiarrhythmic-diarrh(35%), PLToxacillin-hepatitis

    oxaliplatin-neuropathy, laryngopharyngeal paraesthesia

    OxytOcin-hypOtension

    paracetamol-RCC, phototox, metab acidosis

    paroxetine-teratogenic(CVS anomal), wt gain

    pentaerythritol tetraNO3-skin rash

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    pentazocin, pethidine-angina

    pergolide-cardiac valvular fibrosis

    phenylbutazone-agranulocytosis

    pHenytoin-Hypersensitivity, Hyperglycem, Hyperplasia gum(MC, collagen

    accumulat), Hirsutism, Hepatitis, Hypotension, osteomalacia, megaloblast anem,

    gynecomastia, ataxiaPilocarpine-cataract, Pseudomyopia, headache

    pioGlitazone-Na,H2O retent, wt Gain

    plicamYCin-hypoglYCemia

    procainamide-lupus, arthritis

    procarbazine-disulfiram rxn, sec ca

    propafenone-asthma, PVD, hypoglycem

    pyrazinamid-hepatotox, hyperuricemia

    quetIAPIne-cataract, prIAPIsm

    quinidine-VT, nausea, vomiting, diarrh, ataxia, tinnitus, vertigo

    quinine-optic neuritis, PLT, hemolysisreserpine-suicidal depression

    retinoid-dryness of skin& mucosa

    Rifampicin-AI PLT, flu like syndR, red orange urine, contact lens staining, hepatotox,

    purpura, jaundice, resp synd

    rimonabant-psychiatric ds, wt loss

    risperidone, rofecoxib, SibuTRamine, tegaserod, valdecoxib-MI, STRoke

    RopiniroLE-RestLEss LEg synd

    rosiglitazone-CHF

    rotigotine-impulsibe behav, shopping, sexual desire

    sildenafil-blue vision defect( PDE6 enz in retina), flushing, hypotension, headache

    Na nitrOprusside-hypOthysoFosbuvir-Fatigue, headache

    sotalol-torsade de pointes

    steroid-glaucOma(tOpical), post subcapsular CataraCt(systemiC), behav worsen

    child, osteoporosis, avasc necrosis fem neck

    streptogRAmin-arthRAlgia

    sulfonamide-acidic urine(crystaluria)

    surfactant-pulm hge(MC)

    tamoxifen-ca endom, cataract, hotflush, thromboembolism

    tamsulosin-floppy iris synd

    taxane-myelosuppress, periph neuropathyteriparatide-osteogenic sarcoma

    tetrazepam-skin rxn

    thalidomide-constipation, periph neuropathy

    thiazide-impotence, PLT

    thioridazin-pigm retinopathy, arrhythmia

    thiothixene-neuroleptic malign synd

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    chloramphenicol-bind 50S ribosome transfer of peptide chain fr P A site

    clofazimine- template fn DNA

    cocaine- reuptake of 5HT,NE,D

    colchicine-bind Microtubule of Mitotic spindle Metaphase arrest Mitotic arrest

    cycloserine- Ala ligase N acetyl muramic acid cell wall synth

    cyclosporine, voclosporine, tacrolimus, sirolimus, everolimus- calcineurin NFATc does not move fr cytoplasm to nucleus transcript IL2 act on MTOR recept

    daunorubicin, doxorubicin- topoisomerase I&II

    Disulfiram- alDehyde DH>alcohol DH

    ecallanitide- kallikrien

    echinocandin- 1,3glucan synthase

    ethambutol- arabinogalactan

    ezetimibe- cholesterol absorpt intest

    fasudil- Rho kinase

    5fluorocytosine-attack fungal nucleus

    GABA-bind subunitglucarpidase-mtx adjuvant

    griseofUlvin- microtUbUle

    hemicholinium- choline cotransporter

    heparin- antithrombin III

    hydroxyurea-Sphase ribonucleoside diP reductase DNA synth

    icatibant-bradykinin antag

    INH-INHA gene mycolic acid synth

    Pb- ALA synthase, ALA dehydratase, ferrochelatase

    leflunomide- dihydroorotate DH

    levosimendon-Ca sensitiser, open ATP sensit Kch

    lincosamide, macrolide, streptogramin-bind 50s ribosome translocation ofelongated peptide chain fr A P site

    linezolid- 23S,50S ribosome prot synth

    mtx- DHFR

    metyrosine- methyl paraTyr

    mitoxantrone-break DNA strand, DNA&RNA synth

    mycophenolate mofetil- IMP DH

    nikkomycin- chitin synth

    nitisone- urine excretion homogentisic acid

    nitrate-bind SH-cysteine NO release soluble guanyl cyclase cGMP

    (Ca)(phosphorylat MLCK) sm m relaxpanobinostat, vorinostat, romidepsin- histone deacetylase

    pegvisomant-GH antag

    pentostatin- adenosine deaminase

    Piperazine citrate-flaccid Paralysis worm

    protC- fact V,VIII

    pyrazinamide- mycolic acid

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    pyrimidine antimetab- thiamidylate synthase

    racecadotril- encephalinase

    rifampicin- DNA dep RNA polymerase initiat RNA synth

    riluzole- NMDA

    riuonest-hr C1 esterase

    ruxolitinib- JAKsulfonamide- dihydropteroate(folate) synthase competitively

    taxane- depolymerisat mitotic spindle

    teicoplanin,vancomycin- elongat peptide chain cell wall

    terbinafine- squalene epoxide cell memb

    tetrabenazine-D depleter

    tetracycline-bind 30S ribosome block AA deposition

    theophylline- phosphodiesterase, ade nosine, histone deacetylation

    trilostane- 3OHsteroidDH

    ulinastatin- trypsin

    vesamicol- ACh tpt synaptic vesicle vinka alkaloid- microtubule polymerisation mitotic spindle

    warfarin- epoxide reductase

    black widow spider toxin- ACh release& depletion

    botulinum toxin-close presynapt Ca ch ACh release NM transm flaccid

    paralysis

    choler tox- ADP ribosylat Gs adenyl cyclase GI epith cAMP

    Cl difficle

    toxinA(enterotoxin)-neutrophil chemoattractant, GTP binding prot glycosylat

    toxinB(cytotoxin)-cytoskeleton disrupt

    diphtheria toxin- ADP ribosylat AA(diphthamide) on elongat fact2 translocation rRNA prot synth

    EHEC verocytotoxin/shigalike toxin- ribosome prot synth

    ETEC heat labile toxin- adenyl cyclase cAMP

    ETEC stable toxin- guanylyl cyclase cGMP

    pertussis toxin-modif (i) fail to inh adenyl cyclase ADP ribosylat Gprot fn

    adenyl cyclase, phospholipase, ion ch

    Pseudomonas exotoxinA- ADP ribosylation elongat fact2 prot synth

    shiga toxin- 28sRNA prot synth

    tetanospasmin-bind periph motor neuron enter axon retrograde tpt to cell body

    in brain&spinal cord presynaptic block release of Gly&GABA

    DRUG-USE

    ACEI-CHF, HTN+DM, HTN+proteinuria, scleroderma crisis

    acetazolamide-periodic paralysis, abs sz, catamenial epilepsy(menstruation)

    aldesleukin-malign melanoma, RCC

    alosetron-diarrh dominant IBS fem

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    alprostadil-erectile dysfn, maintain PDA patency

    amifostine-radioprotector, cisplatin induced nephrotox

    anagrelide-essential thrombocytosis

    apafant, lexipafant-pancreatitis

    BCG, mitomycinC-ca UB

    bleomycin-GCT, capillary hemangiomabortezomib-multiple myeloma, mantle cell lymphoma

    botulinum toxA-wrinkle, blepharospasm, cosmetic Sx, strabismus, dystonia

    botulinum toxB-SMR, cervical dystonia

    bremelanotide-erectile dysfn

    bretylium-hypothermia induced VT, bupivacaine induced VT

    bromocryptine, cabergoline, quinagolide (D2agonist)-galactorrhoea, hepat coma,

    cyclic mastalgia, Parkinson ds, acromegaly, T2DM

    carboprost-PPH

    carmustine-brain tm

    cephalosporine I-G+ve bact

    II-Pseudomonas, B fragilis

    III-Pseudomonas

    V-MRSA

    cisplatin-ca cx, ca ovary

    clonidine-HTN, secretory diarrh

    cycloserine-TB

    cytarabine, doxorubicin-AML

    dapsone-acne, leprosy, pemph vulgaris, SLE, subcorneal pustule

    dalfampridin(4aminopyridin)- walking ability multiple sclerosis pt, Lambert Eaton

    synddenileukin deftitox(IL2+diphtheria tox)-cutan Tcell lymphoma

    dexmedetomidine-sedation in ICU pt

    diazoxide-HTN, insulinoma

    digoxin-CHF, disopyramide induced HR

    ecallanitide, riunest-heredit angioedema

    echinocandin-Candida, Aspergillus

    epoprostenol-dialysis, CABG, store PLT, maintain PDA

    fasudil-angina, SAH

    felypressin- lignocaine action, esoph varices

    5FU-ca colon, keratosis, superf BCCfludarabine-CLL, hairy cell leukemia

    flutamide-ca prostate

    fosfomycin-UTI

    ganaxolone-abs sz, catamenial sz

    GCSF-neutropenia

    gemcitabine-radiosensitiser

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    streptograMin-Enterococcus faeciuM

    tamsulosin-ureteric stone

    temozolomide-glioblastoma multiforma, malign melanoma

    tezosentan-a/c heart failure

    thalidomide(R)-multiple myeloma, lepra rxn2, aphthous ulcer, SLE

    topiramate-anticraving for both smoking &alcoholtopotecan-ca ovary

    ulinastatin-pancreatitis, sepsis

    valrubin-BCG resist ca UB

    vancomycin-inf endocarditis

    voclosporin-inf uveitis(LUMINATE)

    DRUG-RESISTANCE

    ceftriaxone-horizont tranfer plasmid coated AmpC lactamase

    ethambutol-embB gene

    fluoroquinolone-pt mutat DNA gyrase gene gyrA,B INH-katG gene mutat(katG catalase peroxidase activat INH), mycobact inh A,

    kasA gen mutat, cross resist-ethionamide

    mtx-DHFR overexpression, efflux by P glycoprot

    rifampicin-rpoB gene

    pyrazinamide-pncA gene

    streptomycin-16S rRNA, ribosom prot S12 gene

    zidovudine-alter reverse transcriptase

    PRODRUG-ACTIVE FORM

    methyldopa-methylNE

    bacampicillin-ampicillinbambuterol-terbutaline

    capecitabine-5FU

    canrenone-spironolactone

    cyclophosphamide-phosphoramide mustard, aldophosphamide

    dabigatran

    dipivefrine-epinephrine

    dipyridamole-adenosine

    enalapril-enalaprilat

    5fluorocytosine-5fluorouracil

    fluoxetinefosphenytoin-phenytoin

    heroin-morphine

    hydralazine MAOI-hydrazide derivative

    isoniazid

    levodopa-dopamine

    lovastatin&simvastatin-OH derivative

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    melagatran-ximelagatran

    mercaptopurine-methylmercaptopurine ribonucleotide

    minoxidil-minoxidil SO4

    mycophenolate mofetil

    nitazoxanide

    omeprazolephenacetin-acetaminophen

    prednisone-prednisolone

    proguanil-proguanil triazine

    psylocybin-psylocin

    sertraline

    sulfasalazine-5ASA

    sulindac-sulfide metabolite

    valaciclovir-aciclovir

    Abbreviationsa-artery, AA-amino acid, abtc-antibiotic, AI-autoimmunebef-before, bel-below, b/l-bilateral, bld-blood, b/n-between, bn-benign, br-branch,Bx-biopsyca-carcinoma, carb-carbohydrate, c/i-contraindication, c/l-contralateral,conc-concentration, cong-congenital, Cx-cervixd-day, def-deficient, ds-disease, d/t-due to, Dx-diagnosisE-estrogenfem-female, fr-fromgld-gland, glu-glucoseh-hormoneidiop-idiopathic, i/l-ipsilateral, inf-infection, inj-injurylig-ligament, LL-lower limb, l/t-leading to

    m-muscle, maj-major, mal-male, MC-most common, met-metastasis, min-minor,mtx-methotrexate, Mx-managementn-nerve, norm-normalP-progesterone, pl-plasma, prot-protein, pt-patientRx-treatmentSCC-squamous cell carcinoma, sr-serum, Sx-surgery, sz-seizuretm-tumour, ts-tissueUL-upper limb, u/l-unilateralvag-vagina, VC-vocal cord, vel-velocity, vert-vertebra, vit-vitamin, vol-volumew-week, wt-weightXr-X rayy-year

    #-fracture-degree

    -(N.B.-THESE NOTES ARE ONLY FOR THE PURPOSE OF GUIDANCE AND HELP

    TO PG ASPIRANTS, NOT FOR COMMERCIAL OR OTHER PURPOSE. REFERENCE

    HAS BEEN TAKEN FROM VARIOUS STANDARD TEXTBOOKS. FOR ANY

    FEEDBACK/QUERY PLEASE CONTACT- [email protected]

    [email protected])