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Flashcards in Drugs Deck (96)
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1
Q

Alefacept

A

Fully human IgG and extra cell part of LFA3. Blocks CD2 binding of LFA-3,preg B
LOW CD4 count
IM administration

2
Q

Efalizumab

A

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

3
Q

Etanercept

A

Human fusion protein–human p75 tnfa receptor, binds free soluble TNF-alpha, Preg B
SE: MS + LE symptoms, malig, worse CHF, infection

4
Q

Infliximab

A

Chimeric, binds soluble and bound TNF-alpha, Preg B

Contraind In CHF, Rare demyelinating disease

5
Q

Adalimumab

A

Human, Binds soluble and membrane bound, Preg B

6
Q

Golimumab

A

Human, AB to TNFa

7
Q

Certolizumab pegol (Cimzia)

A

Human, pegylated ab vs. TNFa, preg B

8
Q

Ustekinumab

A

Human, Ab vs. p40 of IL-12 and 23, preg B

Reversible posterior leukoencephalopathy syndrome

9
Q

Briakinumab

A

IL-12/23 inh

10
Q

Rituximab

A

AB vs. CD20 for B cell NHL

11
Q

Anakinra

A

IL-1 rec ab for periodic fever syd

12
Q

Ipilimumab (Yervoy)

A

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

13
Q

Denileukin Diftox (Ontak)

A

Fusion diphtheria toxin with IL-2

SE: Leaky synd, fluid retention, erythema, liver abnl.

14
Q

Mycophenolate mofetil

A

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

15
Q

Azathioprine

A

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

16
Q

Cyclosporine

A

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

17
Q

Cyclophosphamide

A

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

18
Q

Methotrexate

A

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

19
Q

Pyrethrin

A

Neurtotoxic to lice—not ovicidal

Natural extract to chrysanthemum

20
Q

Permethrin

A

Synthetic pyrethrin. Disables Na transport channels in parasites–causes paralysis
Pediculicidal and ovoidal–Don’t use if chrysanthemum allergy

21
Q

Lindane

A

Chlorinated hydrocarbon; interferes with GABA causes reap and musc paralysis.
For scabies, all 3 lice. Can give seizure, ICD

22
Q

Malathion

A

Ovicidal. Organophosphate cholinesterase inhibitor. Flammable–for scbies, lice

23
Q

Ivermectin

A

Blocks glutamate-gated chloride channel–paralysis of parasite. For strongyloides, norweign scabies, onchocerchiasis.

24
Q

Crotamiton

A

Scabicide, unknown mech. Can give ACD

25
Q

Precip Sulfur 6%

A

Unclear mech. To treat scabies in pre go and <2yoa

26
Q

Thiabendazole/Albendazole

A

Inhibits FUMARATE REDUCTASE (helminth spec enzy). Used in cutan larva migrans and currens.
SE:Dizzy, drowsy, jaundice.

27
Q

Na+ stibogluconate, meglumine antimoniate

A

Pentavalent antimonial. Treat leish.

SE: PROLONG QT, pancreatitis, hepatitis, renal failure

28
Q

Pentamidine

A

Inh protozoa DNA/RNA/phospholipid/protein synth

Trypanosomiasis and Leish

29
Q

Diethylcarbamazine

A

Piperine deriv. Unknown mech. FOr filariasis and onchocerciasis.

30
Q

Vemurafenib

A

BRAF inhr. V600E. (mutation trades valine for glutamic acid). Photosens and hyperkeratosis.

31
Q

Vesmodigib

A

SMO inhibitor. Muscle spasm, Hyponatremia, fatigue, weight loss, dysgusia. Prolonged QT.

32
Q

Tetracyclines

A

Inh ribosomal 30S–blks protein synthesis
Preg D
Tetracyc–Discolors gingival 3rd of teeth in t give with Ca and Iron.
Tetra–FDE

33
Q

Macrolides

A

Clarithro, Azithro, Erythro–inh 50S
Alternative for pen allergy
Inh p450
PregC-clarith, PregB-Erythro,Azithro

34
Q

Fluoroquinolones

A

Inh bacterial DNA gyrase, Preg C
Inc LFTs, nephrotoxicity
Decrease with Ca, Iron, sucralafate. Inh 1A2–>inc
Warfarin, Aminophylline, theophylline, procainamide

35
Q

Erythro and other drugs

A

Increases: Warfarin, Digoxin, Statins, Anticonvulsants/BZD, CSA, methylprednisolone, theophylline
Give with statin=rhabdo. Give with CCB–bradycardia

36
Q

Clindamycin

A

Inh 50S. Preg B

37
Q

Rifampin

A

Inh RNA synthesys via inh DNA-dependent RNA polymerase. Preg C

38
Q

Aminoglycoside

A

Gentamicin, Streptomycin
Inh ribo 30S. Preg D
SE-ototox, nephrotox

39
Q

Sulfonamides/Sulfasalazine

A

Inh dihydropteroate synthetase–inh bact folic acid synthesis. PReg C and D in 3rd trimester.

40
Q

Dapsone

A

Inh myeloperoxidase. Preg C. Agranulocytosis (2-12 wks in), hem anemia, cholestatic jaundice, motor periph neuropathy. acute psycosis

41
Q

Vancomycin

A

Inh bacterial wall synthesis, preg Cat B.

42
Q

Metronidazole

A

Inhibits nucleic acid synthesis via toxic metabs

Glossitis, Preg B.

43
Q

Clofazamine

A

Preg C. Red-brown discoloration of leprosy lesions

44
Q

ABX ok in Prego

A

Penicillin, Cephalosporin, Erythro/Azithro, Flagyl, Clindamycin, Vancomycin.

45
Q

Itraconazole

A

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

46
Q

Voriconazole

A

Triazole. inh 14a-demethylase. Preg Cat C. SE-visual disturb. Inh cyp450 (Inc warf, bzd, csa)
FungiSTATIC

47
Q

Fluconazole

A

Triazole. inh 14a-demethylase. Preg Cat C. 90% bioavailability (HIGHEST). Inh cyp450 (INC WARFARIN, bzd, csa)
FungiSTATIC

48
Q

Ketoconazole

A

Interferes with androgen, glucocort synthesis. inh 14a-demethylase. Preg Cat C. Needs acidic envir
SE: Fulminant hepatitis
FungiSTATIC

49
Q

Terbinafine

A

Inh squalene epoxidase. Preg Cat B. FungiCIDAL. DOES NOT inh cyt 450. SE: DILE

50
Q

Ampho B

A

Binds ergosterol and makes pores. Cat B. Nephrotox, agranulocyt.

51
Q

Caspofungin

A

Inh synthesis of glucan. Preg Cat C. -for asper/candidiasis

52
Q

Griseofulvin

A

Disrupts microtubule function–metaphase arrest
Cat C. Fungistatic. INDUCES cyp 450 (dec war, etc)
Severe headache, DILE, worsens AIP
For dermatophytes only.

53
Q

Acyclovir

A

Uses viral thymadine kinase to get phosphorylated to active acyc monophosphate that blocks viral DNA polymerase. PREG B. SE: IV assoc reversible nephropathy

54
Q

Valacyclovir

A

Prodrug of acyc. Uses viral TK. PREG B. Best for Zoster. SE: TTP in HIV, IC

55
Q

Penciclovir

A

Uses viral TK. Low bioava. Use topical

56
Q

Famciclovir

A

Uses viral TK. PREG B. PO.

57
Q

Ganciclovir

A

Uses viral TK. CMV retinitis. SE: neutropenia, bone marrow supp, thrombocytopenia. Don’t give with AZT.

58
Q

Foscarnet

A

Doesn’t need phosphorylated. Noncom inh of viral DNA polymerases. CMV, resis HSV, VZV. SE: penile ulcerations

59
Q

Cidofovir

A

Nucleoside analog. Inh DNA polymerase without phos. Only for resist to gangiclovir/foscarnet.

60
Q

Amantadine/Rimantidine

A

Inhibs uncoating of viral DNA to prevent replication. For flu, rubella, SE: Anticholinergic.

61
Q

Zidovudine (AZT)

A

Reverse transcriptase inhr. Se: melanonychia, oral pigmentation, BM suppression, lipodystrophy, trichomegaly. PREG C.

62
Q

Didanosine

A

Reverse transcriptase inhr. Need basic environment. SE: Pancreatitis, optic neuropathy, perip neuropathy, lactic acidosis
PREG B

63
Q

Abacavir

A

Reverse transcriptase inhr. HLA 5701 PREG C

64
Q

Tenofovir

A

Rev transcriptase inhr. SE: peripheral wasting, cushingoid appear. PREG B.

65
Q

Indinavir, Ritonavir, Lopinavir

A

Protease inhibitors. SE: Lipodystrophy, gynecomastia, periung PGs, hepatotoxicity.

66
Q

Topical Tacrolimus (Protopic)

A

Binds to FKBP which then binds to CALCINEURIN, blocking its ability to dephosphorylate NFAT. This prevents transcription of IL-2.

67
Q

cortisone, hydrocortisone

A

Shortest acting. Have most mineralcort act and least corticoid act.

68
Q

Methylprednisolone, betamethasone, triamcinolone, dexamethasone

A

Intermed and long acting. No mineralcort act. Dex and beta with highest Glucocort act.

69
Q

Hydroxyurea

A

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.

70
Q

Imiquimod/Resiquimod

A

Via TLR7 increases Th1 cytokines: TNFa, IFNa, IL6
Stims innate and adaptive
FDA AK, SBCC with nl immune, gen warts
SE: eruptive epid cysts

71
Q

Hydroxychloroquine

A

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

72
Q

Chloroquine

A

Inh chemotaxis/phagocytosis. Worst for ocular toxicity. Yellow discoloration, skin/sclera. Can add quinacrine

73
Q

Quinacrine

A

NO risk retinopathy. Yellows hair, conjunctiva and dorsal hands/feet.

74
Q

Rapamycin

A

Sirolimus. Macrolide abx. Analog FK506. INH mTOR (mem PI3K kinase)

75
Q

Chlorambucil

A

ALkalating agent.

SE: SEIZURE, BM tox, urticaria, mucositis.

76
Q

5-FU

A

S-Phase. Blks methylation of deoxyuridyl to thymidylic acid. Blks DNA/RNA synthesis.
SE: inflam AKs, extrav rxn, chemo recall

77
Q

Bleomycin

A

M and G2 specific. Damages dna by direct bind

SE: Raynaud’s, flagellate, pulm tox.

78
Q

Doxorubicin (Adriamycin)

A

Cytotoxic abx. Intercalates with preformed DNA.

SE: Cardiotox, chemo and rad recall. Mucositis

79
Q

Dactinomycin (Actinomycin)

A

Cytotoxic abx. Complexes with DNA

SE: RADIATION RECALL

80
Q

Vinblastine

A

Microtubule linkage in METAPHASE.

Se: Extravas reaction.

81
Q

Cytarabine

A

Blocks DNA synth in S phase.

SE: NEH, inflam SKs, eccrine squam syringometaplasia, acral erythema

82
Q

Spironolactone

A

Antiandrogen–blks DHT from binding to receptor. Cat X. For hormonal acne, androgenic alopecia
SE:HyperK

83
Q

Finasteride

A

Inh Type II 5a-reductase. Cat X.
Type II: Scalp, prostate, liver, beard, chest
Type I: Seb gland, liver.

84
Q

Flutamide

A

Nonsteroidal antiandrogen. Competitive blk DHT from R

SE: hepatotoxicity

85
Q

Stanazol/Danazol

A

Synthetic anabolic steroid made from testosterone
Cat X. For Cryo, C1esterase inh def
SE: insul resis, alopecia, cramps

86
Q

OCP

A

Blks ovarian and adrenal androgens.

Low andro’s: Norethindrone, levonorgestrel, desogestrel, norgestimate, gestadone, Drosperinone.

87
Q

Eflornithine hydrochloride

A

Irrev inh ornithine decarboxylase. Cat C.

88
Q

Minoxidil

A

Cat C.

89
Q

H1 antihist 1st gen

A

Cyproheptadine (Periactin)
Chlorpheniramine-safest in prego (Trimeton)
Hydroxyzine

90
Q

H1 Antihistamine 2nd gen

A

Fexofenadine-Allegra, cat C
Loratadine-Claritin, cat B, long acting
Cetirizine-Zyrtec, cat B (metab of hydroxyzine)

91
Q

H2 Antihistamines

A

Cimetidine-Comp inh DHT at andro receptor

Ranitidine

92
Q

All Trans Retinoic Acid

A

For ApML, can cause scrotal/genital ulcers

93
Q

Castellani’s Paint

A

fungicidal and bactericidal agent.

boric acid, resorcinol, phenol, acetone, water, industrial methylated spirit, magenta

94
Q

Podophyllin

A

Contains kaempherol which is a potent mutagens. anti-mitotic agent that reversibly binds tubulin, arresting cells in metaphase

95
Q

Podophyllotoxin

A

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

96
Q

Cantharidin

A

PDE inh’r. From blister beetle.