Drugs Flashcards
(96 cards)
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
