Drugs Flashcards
Alefacept
Fully human IgG and extra cell part of LFA3. Blocks CD2 binding of LFA-3,preg B
LOW CD4 count
IM administration
Efalizumab
Humanized form of murine AB vs. CD11a. Blks CD11a of LFA-1 (So LFA-1 can’t bind ICAM-1). T cell can’t get out of vaculature
Preg C–PML, BLACK BOX
Etanercept
Human fusion protein–human p75 tnfa receptor, binds free soluble TNF-alpha, Preg B
SE: MS + LE symptoms, malig, worse CHF, infection
Infliximab
Chimeric, binds soluble and bound TNF-alpha, Preg B
Contraind In CHF, Rare demyelinating disease
Adalimumab
Human, Binds soluble and membrane bound, Preg B
Golimumab
Human, AB to TNFa
Certolizumab pegol (Cimzia)
Human, pegylated ab vs. TNFa, preg B
Ustekinumab
Human, Ab vs. p40 of IL-12 and 23, preg B
Reversible posterior leukoencephalopathy syndrome
Briakinumab
IL-12/23 inh
Rituximab
AB vs. CD20 for B cell NHL
Anakinra
IL-1 rec ab for periodic fever syd
Ipilimumab (Yervoy)
Human ab to CTLA-4 (blks the signal to inn T cells so they stay activated.) Usually CTLA-4 binds B7 to be turned off.
Dermatitis, Diarrhea, Hypophysitis
Denileukin Diftox (Ontak)
Fusion diphtheria toxin with IL-2
SE: Leaky synd, fluid retention, erythema, liver abnl.
Mycophenolate mofetil
Inhibits de novo purine synthesis by non competitively inhibiting inosine monophosphate dehydrogenase (IMPDH).
B and T cells lack purine salvage pathway so are preferentially inhibited
Exc by kidneys. After ingest, act metabol is mycophenolic acid; deactiv by liver and react by epiderm and GI tract via B-glucoronidase.
Se: Dose rel’d bm tox, Red cell aplasia, PML, GI mostly.
NOT HEPATO OR RENAL TOX careful with PUD. PREG D
Azathioprine
S specific. Act metabolite is 6-MP. Then can go 3 paths–XO and TPMT to get inapt metab and HPRT to get active thioguanine. If low TMPT get too much thioguan or if allopur blk XO get too much toxic thioguan and bone marrow supp.
Kidney excretion, PREG D. Hypersens reaction at 14 days. Lymphoprolif malig in RA
Metab to purine analogs purine and guanine that then inhibit DNA and RNA synthesis
Cyclosporine
complexes with cyclophilin which inhibits calcineurin and inhibits dephos of NFAT causing decreased IL-2 production. Also decreases IFN g
Avoid grapefruit juice.
SE: nephro, hyperk, hypomag, inc uric acid, if renal cr >30% then dec by 25%. Treat HTN with ACEI.
Metab by 3A4
Cyclophosphamide
Cell cycle nonspecific alkalating agent–depresses B cell more than T cells. Releases Cl- and forms reactive intermediate that binds DNA preferentially at the 7-nitrogen atom of guanine
Nitrogen mustard deriv. SE: Inc risk Lymphoma, leukemia, bladder CA due to acrolein, SCC. BM supp, pulm fibrosis, Hyperpig of hair and nails, azoospermia
For Wegners
Methotrexate
S phase specific. Antimetab and antifolate. Competivitely and irreversibly inhibits dihydrofolate hydrogenae so dihydrofolate isn’t covered to tetrahydrafolate.
Renal excretion. Liver bx at 1.5g. Caution in DM, alcohol or renal insuff. Causes radiation recall.
Se: Hep, pancytopenia (leucovorin)-esp w/ NSAID, dapsone, bactrim, acute interest pneumonia rare.
Inc levels w/TCN, pheny, NSAID, Salicyl, sulfon
Pyrethrin
Neurtotoxic to lice—not ovicidal
Natural extract to chrysanthemum
Permethrin
Synthetic pyrethrin. Disables Na transport channels in parasites–causes paralysis
Pediculicidal and ovoidal–Don’t use if chrysanthemum allergy
Lindane
Chlorinated hydrocarbon; interferes with GABA causes reap and musc paralysis.
For scabies, all 3 lice. Can give seizure, ICD
Malathion
Ovicidal. Organophosphate cholinesterase inhibitor. Flammable–for scbies, lice
Ivermectin
Blocks glutamate-gated chloride channel–paralysis of parasite. For strongyloides, norweign scabies, onchocerchiasis.
Crotamiton
Scabicide, unknown mech. Can give ACD
Precip Sulfur 6%
Unclear mech. To treat scabies in pre go and <2yoa
Thiabendazole/Albendazole
Inhibits FUMARATE REDUCTASE (helminth spec enzy). Used in cutan larva migrans and currens.
SE:Dizzy, drowsy, jaundice.
Na+ stibogluconate, meglumine antimoniate
Pentavalent antimonial. Treat leish.
SE: PROLONG QT, pancreatitis, hepatitis, renal failure
Pentamidine
Inh protozoa DNA/RNA/phospholipid/protein synth
Trypanosomiasis and Leish
Diethylcarbamazine
Piperine deriv. Unknown mech. FOr filariasis and onchocerciasis.
Vemurafenib
BRAF inhr. V600E. (mutation trades valine for glutamic acid). Photosens and hyperkeratosis.
Vesmodigib
SMO inhibitor. Muscle spasm, Hyponatremia, fatigue, weight loss, dysgusia. Prolonged QT.
Tetracyclines
Inh ribosomal 30S–blks protein synthesis
Preg D
Tetracyc–Discolors gingival 3rd of teeth in t give with Ca and Iron.
Tetra–FDE
Macrolides
Clarithro, Azithro, Erythro–inh 50S
Alternative for pen allergy
Inh p450
PregC-clarith, PregB-Erythro,Azithro
Fluoroquinolones
Inh bacterial DNA gyrase, Preg C
Inc LFTs, nephrotoxicity
Decrease with Ca, Iron, sucralafate. Inh 1A2–>inc
Warfarin, Aminophylline, theophylline, procainamide
Erythro and other drugs
Increases: Warfarin, Digoxin, Statins, Anticonvulsants/BZD, CSA, methylprednisolone, theophylline
Give with statin=rhabdo. Give with CCB–bradycardia
Clindamycin
Inh 50S. Preg B
Rifampin
Inh RNA synthesys via inh DNA-dependent RNA polymerase. Preg C
Aminoglycoside
Gentamicin, Streptomycin
Inh ribo 30S. Preg D
SE-ototox, nephrotox
Sulfonamides/Sulfasalazine
Inh dihydropteroate synthetase–inh bact folic acid synthesis. PReg C and D in 3rd trimester.
Dapsone
Inh myeloperoxidase. Preg C. Agranulocytosis (2-12 wks in), hem anemia, cholestatic jaundice, motor periph neuropathy. acute psycosis
Vancomycin
Inh bacterial wall synthesis, preg Cat B.
Metronidazole
Inhibits nucleic acid synthesis via toxic metabs
Glossitis, Preg B.
Clofazamine
Preg C. Red-brown discoloration of leprosy lesions
ABX ok in Prego
Penicillin, Cephalosporin, Erythro/Azithro, Flagyl, Clindamycin, Vancomycin.
Itraconazole
Triazole. Blocks ergosterol synth via inh 14a-demethylase
FungiSTATIC, needs ACIDIC environ.
Don’t give with cisapride, pimozide, quinidine, because FATAL ARRYTHMIA.
SE: Inc. LFTs, dec WBC, Inc TG, nephrotoxicity. EXACERBATE CHF. PReg C
Voriconazole
Triazole. inh 14a-demethylase. Preg Cat C. SE-visual disturb. Inh cyp450 (Inc warf, bzd, csa)
FungiSTATIC
Fluconazole
Triazole. inh 14a-demethylase. Preg Cat C. 90% bioavailability (HIGHEST). Inh cyp450 (INC WARFARIN, bzd, csa)
FungiSTATIC
Ketoconazole
Interferes with androgen, glucocort synthesis. inh 14a-demethylase. Preg Cat C. Needs acidic envir
SE: Fulminant hepatitis
FungiSTATIC
Terbinafine
Inh squalene epoxidase. Preg Cat B. FungiCIDAL. DOES NOT inh cyt 450. SE: DILE
Ampho B
Binds ergosterol and makes pores. Cat B. Nephrotox, agranulocyt.
Caspofungin
Inh synthesis of glucan. Preg Cat C. -for asper/candidiasis
Griseofulvin
Disrupts microtubule function–metaphase arrest
Cat C. Fungistatic. INDUCES cyp 450 (dec war, etc)
Severe headache, DILE, worsens AIP
For dermatophytes only.
Acyclovir
Uses viral thymadine kinase to get phosphorylated to active acyc monophosphate that blocks viral DNA polymerase. PREG B. SE: IV assoc reversible nephropathy
Valacyclovir
Prodrug of acyc. Uses viral TK. PREG B. Best for Zoster. SE: TTP in HIV, IC
Penciclovir
Uses viral TK. Low bioava. Use topical
Famciclovir
Uses viral TK. PREG B. PO.
Ganciclovir
Uses viral TK. CMV retinitis. SE: neutropenia, bone marrow supp, thrombocytopenia. Don’t give with AZT.
Foscarnet
Doesn’t need phosphorylated. Noncom inh of viral DNA polymerases. CMV, resis HSV, VZV. SE: penile ulcerations
Cidofovir
Nucleoside analog. Inh DNA polymerase without phos. Only for resist to gangiclovir/foscarnet.
Amantadine/Rimantidine
Inhibs uncoating of viral DNA to prevent replication. For flu, rubella, SE: Anticholinergic.
Zidovudine (AZT)
Reverse transcriptase inhr. Se: melanonychia, oral pigmentation, BM suppression, lipodystrophy, trichomegaly. PREG C.
Didanosine
Reverse transcriptase inhr. Need basic environment. SE: Pancreatitis, optic neuropathy, perip neuropathy, lactic acidosis
PREG B
Abacavir
Reverse transcriptase inhr. HLA 5701 PREG C
Tenofovir
Rev transcriptase inhr. SE: peripheral wasting, cushingoid appear. PREG B.
Indinavir, Ritonavir, Lopinavir
Protease inhibitors. SE: Lipodystrophy, gynecomastia, periung PGs, hepatotoxicity.
Topical Tacrolimus (Protopic)
Binds to FKBP which then binds to CALCINEURIN, blocking its ability to dephosphorylate NFAT. This prevents transcription of IL-2.
cortisone, hydrocortisone
Shortest acting. Have most mineralcort act and least corticoid act.
Methylprednisolone, betamethasone, triamcinolone, dexamethasone
Intermed and long acting. No mineralcort act. Dex and beta with highest Glucocort act.
Hydroxyurea
S phase specific. Inh ribonucleotidase reductase. Inh DNA synth. Preg Cat D.
SE: Heme tox, photosens, mucosal ulcers, hepatitis, renal tox, poikiloderma hands/feet, diffuse hyperpig, leg ulcers, radiation recall, acral erythema, DM-like reaction.
Imiquimod/Resiquimod
Via TLR7 increases Th1 cytokines: TNFa, IFNa, IL6
Stims innate and adaptive
FDA AK, SBCC with nl immune, gen warts
SE: eruptive epid cysts
Hydroxychloroquine
Prob intercalates into DNA. Accumulates in melanin rich tissue. Blue grey color of mucocut and nails (hemosiderin and melanin deposition) 2nd worst for ocular retinopathy. Preg C. Bleach hair roots/alopecia. Can exacerbate PCT
Can add quinacrine
Chloroquine
Inh chemotaxis/phagocytosis. Worst for ocular toxicity. Yellow discoloration, skin/sclera. Can add quinacrine
Quinacrine
NO risk retinopathy. Yellows hair, conjunctiva and dorsal hands/feet.
Rapamycin
Sirolimus. Macrolide abx. Analog FK506. INH mTOR (mem PI3K kinase)
Chlorambucil
ALkalating agent.
SE: SEIZURE, BM tox, urticaria, mucositis.
5-FU
S-Phase. Blks methylation of deoxyuridyl to thymidylic acid. Blks DNA/RNA synthesis.
SE: inflam AKs, extrav rxn, chemo recall
Bleomycin
M and G2 specific. Damages dna by direct bind
SE: Raynaud’s, flagellate, pulm tox.
Doxorubicin (Adriamycin)
Cytotoxic abx. Intercalates with preformed DNA.
SE: Cardiotox, chemo and rad recall. Mucositis
Dactinomycin (Actinomycin)
Cytotoxic abx. Complexes with DNA
SE: RADIATION RECALL
Vinblastine
Microtubule linkage in METAPHASE.
Se: Extravas reaction.
Cytarabine
Blocks DNA synth in S phase.
SE: NEH, inflam SKs, eccrine squam syringometaplasia, acral erythema
Spironolactone
Antiandrogen–blks DHT from binding to receptor. Cat X. For hormonal acne, androgenic alopecia
SE:HyperK
Finasteride
Inh Type II 5a-reductase. Cat X.
Type II: Scalp, prostate, liver, beard, chest
Type I: Seb gland, liver.
Flutamide
Nonsteroidal antiandrogen. Competitive blk DHT from R
SE: hepatotoxicity
Stanazol/Danazol
Synthetic anabolic steroid made from testosterone
Cat X. For Cryo, C1esterase inh def
SE: insul resis, alopecia, cramps
OCP
Blks ovarian and adrenal androgens.
Low andro’s: Norethindrone, levonorgestrel, desogestrel, norgestimate, gestadone, Drosperinone.
Eflornithine hydrochloride
Irrev inh ornithine decarboxylase. Cat C.
Minoxidil
Cat C.
H1 antihist 1st gen
Cyproheptadine (Periactin)
Chlorpheniramine-safest in prego (Trimeton)
Hydroxyzine
H1 Antihistamine 2nd gen
Fexofenadine-Allegra, cat C
Loratadine-Claritin, cat B, long acting
Cetirizine-Zyrtec, cat B (metab of hydroxyzine)
H2 Antihistamines
Cimetidine-Comp inh DHT at andro receptor
Ranitidine
All Trans Retinoic Acid
For ApML, can cause scrotal/genital ulcers
Castellani’s Paint
fungicidal and bactericidal agent.
boric acid, resorcinol, phenol, acetone, water, industrial methylated spirit, magenta
Podophyllin
Contains kaempherol which is a potent mutagens. anti-mitotic agent that reversibly binds tubulin, arresting cells in metaphase
Podophyllotoxin
known as podofilox or Condolox, is a anti-mitotic agent that reversibly binds tubulin, arresting cells in metaphase. It is used topically to treat genital warts
Cantharidin
PDE inh’r. From blister beetle.