HD4 Pharm Flashcards

0
Q

Artemether/Iumafantrine (coartem)

A

Mech: unknown
Route: oral – CYP 450 metab.
Use: for acute P. falciparum malaria (*NOT for prophylaxis or severe)
SE: hypersensitivity (urticaria & angioedema)

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1
Q

Malarone

A

(combo of atovaquone & proguanil)
Mech: block pyrimidine synthesis
Route: oral; biliary & urinary excretion.
Use: to Tx malaria from P. falciparum (acute, uncomplicated)
(SE: headache, GI)

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2
Q

Nitazoxanide

A
Mech: interferes w/ energy production
Route: oral, hepatic metab (but NOT CYP)
Use: diarrhea from Giardia lamblia or Cryptosporidium parvum
SE: none
*NOT effective if immunocompromised
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3
Q

Paromycin

A

Mech: blocks protein synthesis
Route: oral, poor absorption –> Luminal
Use: intestinal amoebiasis (NOT for systemic inf)
SE: nausea, abdominal crampls, diarrhea

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4
Q

Types of malaria

A
  1. Plasmodium falciparum: => malignant tertiary fever (deadly), most drug resistance.
  2. Plasmodium vivex, ovale, malariae: => benign tertiary fever, relapse common.
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5
Q

three types/approaches to treatment for malaria

A
  1. clinical cure: eliminate all erythrocytic forms
  2. radical cure: eliminate all erythrocytic AND exoerythrocytic forms
  3. prophylaxis (prevention/protection)
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6
Q

Drugs used for superficial fungal infections (skin, gut, oral cavity, eyes)

A

*rarely life-threatening, unless immuno-compromised.
1. Nystatin
2. Griseofulvin
3. Clotrimazole
4. Terbinafine
(mostly used superficially only too toxic for systemic use)

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7
Q

drugs used for systemic fungal infections

A
  1. Amphotericin B
  2. Flucytosine
  3. Fluconazole
  4. caspogungin
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8
Q

Terbinafine

A

Mech: inhibits ergosterol synth. fungistatic OR fungicidal
Route: topical or oral & hepatic metab.
Use: onychomycosis (on fingernails), candida, trychophyton
SE: *watch for P450 induction/inhibition, liver dysfunction

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9
Q

Caspofungin

A

Mech:
Route:
Use: for aspergillous (esp. invasive) or candida
SE:

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10
Q

Nystatin

A

Mech: binds to ergosterol (same as ampho B)
Route: topical (to skin & mucous membranes), poor absorption
Use: candida infections (skin, bowel, etc.)
SE: —

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11
Q

Clotrimazole

A

Mech: inhibit ergosterol
Route: topical (NOT oral)
Use: candidiasis
SE: —

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12
Q

Prednisone

A

Mech: glucocorticoid, modulates gene expression
Use: immune-suppressant for RA, SLE, severe psoriasis, neoplasia
Route: prodrug, metab @ liver
SE: (not very selective) -> insomnia, weight gain, Cushings, susceptible to infection

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13
Q

Sirolimus

A

Anti-proliferative immune-suppressant
Mech: binds FKB-12 -> complex inhibits mTOR, so –l T cell activation
Use: kidney rejection prophylaxis or chronic rejection
*(NOT liver or lung)
Route: metab in liver
SE: edema, HTN, risk infections & malignancy

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14
Q

Drugs that inhibit CYP450

A
  1. Ca2+ blockers
  2. Anti-fungals (fluconazole, ketoconazole)
  3. erythromycin
  4. HIV protease inhibitors
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15
Q

Drugs that induce CYP450

A
  1. Rifampin

2. Phenytoin

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16
Q

Azathioprine

A

Anti-proliferative immune-suppressant prodrug
Mech: blocks de novo purine synthesis (active as 6-mercaptopurine)
Use: prevent kidney rejection OR refractory RA
SE: hepatotoxicity, myelosuppression, mucositis, GI Sxs, *teratogen & carcinogen!

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17
Q

Cyclophosphamide

A

anti-proliferative immune-suppressant, Prodrug (metab by liver)
Mech: electrophile cross-linking of DNA
Use: BMT conditioning, RA (off-label)
SE: myelosuppression, GI, bladder toxicity, ovarian failure & sterility

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18
Q

Methotrexate

A

anti-proliferative immune-suppressant,
Mech: –l dihydrofolate reductase, methylated: –l Thymidilate synthase
(for incorporation of dUTP into DNA)
Use: severe RA *even kids w/ juvenile RA, recalcitrant psoriasis
SE: myelosuppression, mucositis, acute renal failure

19
Q

Equine Thymocyte Immune Globulin (ETIG)

A

Mech: lymphcyte selective immune-suppressant;
Use: renal allograft rejection prophylaxis, acute rejection, induce immuno-suppression
SE: leukopenia, thrombocytopenia, transfusion rxn, risk infection or malignancy

20
Q

OKT3

A

monoclonal Ab for CD3 Ag on human T cells => reduce # circulating T cells
Use: Acute renal allograft rejection
SE: cytokine storm, anaphylactic or transfusion rxn, risk of inf or malignancy

21
Q

Misoprostol

A

Mech: PGE4 analog => anti-secretory and mucosal protectant
Use: Reduce risk of NSAID-induced gastric ulcers
PK: oral prodrug with rapid clearance
SE: Teratogenic! (Preg. category X), GI & CNS Sxs

22
Q

Dexamethasone

A

corticosteroid, *hepatic metab.
Use: anti-emetic (mech unknown), and for Ulcerative Colitis
SE: insomnia, mood changes, weight gain/Cushings, susceptible to infection

23
Q

Arepitant

A
Mech: NK1 R antagonist --l substance P
Use: anti-emetic (for chemotherapy pts)
*hepatic metabolism
SE: Contraind if liver failure, GI & CNS effects
DDIs: anti-fungals, warfarin, etc.
24
Q

Scopolamine

A

Mech: muscarinic R antagonist (belladona)
Route: percutaneous patch placed behind ear
Use: prevent nausea & vomiting from motion sickness or post-surgical
SE: Dry mouth, drowsiness
Contraind: liver or kidney impairment

25
Q

Primary induction therapy for cancer

A

= medication used as palliative

  • reduce progression of tumor
  • reduce tumor-related Sxs
  • prolong survival
  • not expected to cure.
26
Q

Neoadjuvant therapy for cancer

A

= medication used, complimentary to surgical management

improve surgical outcome, survival, and quality of life

27
Q

Adjuvant Therapy for cancer

A

medication used to prevent recurrence of cancer (local and systemic), improves overall survival.
*used AFTER initial (surgical) treatment

28
Q

Mitotane

A

Mech: Adrenolytic agent (selectively toxicity to adrenal cortical tissue)
Use: adrenocortical cancers
SE: adrenal insufficiency, nausea & vomiting

29
Q

Tamoxifen

A

Mech: Selective estrogen R modulator (antagonist, competes w/ endog. estradiol)
Use: adjunct to breast cancer treatment (only if ER+)
SE: (Many, significant!) Menopausal Sxs, fluid retention/periph. edema, endometrial cancer…
* DDI w/ other CYP450-associated drugs bc activated by CYP450!

30
Q

Anastrazole

A

Mech: non-steroidal aromatase inhibitor (–l androgen to estrogen conversion)
Use: Metastatic breast cancer or adjuvant Tx (if early & HR+) in POST-menopausal women
SE: hot flashes, arthralgia, peripheral edema, headache, etc.

31
Q

Tretinoin

A

Mech: ~unknown. Vit A analog => induces differentiation of promyelocytes to myelocytes
Use: ChemoTx for Acute Promyelocytic Leukemia
SE: Vit A toxicity, Retinoid acid syndrome, MI, cardiac ischemia, stroke, pulm. HTN

32
Q

Cetuximab

A

Mech: anti-EGFR monoclonal Ab (blocks mitogenic & anti-apoptotic signals)
Use: colorectal, head, & neck cancers
SE: Infusion-related reactions (if once, will never give again)

33
Q

Pentostatin

A

Mech: purine analog, Inhibits adenosine deaminase & 1 C transfers (& DNA synthesis)
Use: hairy cell leukemia
SE: myelosuppression

34
Q

Erlotnib

A

Mech: EGFR tyrosine kinase inhibitor => growth arrest
Use: lung or pancreatic cancer (non-small cell)
SE: Interstitial lung disease!, GI perforation, hepatotoxicity, renal failure
*CYP450 metabolism

35
Q

Bevacizumab

A

Mech: Anti-VEGF monoclonal Ab
Use: inhibit angiogenesis, targets HEALTHY cells! (cancer chemoTx)
SE: GI bleeding, poor wound healing, pulmonary hemorrhage, arterial thrombotic events

36
Q

Osetamavir

A

Mech: inhibits viral Neuraminidase *= esterified pro-drug
Use: influenza (type A and B) – prophylaxis or acute Tx if age <2 yrs
SE: stevens-Johnson syndrome (rare, fatal)
*not as effective as amantadine, but used more

37
Q

Foscarnet

A

Mech: inhibits DNA polymerase (of HSV, CMV, others)
Use: CMV retinitis, acyclovir-resistant CMV or VZV
SE: renal impairment

38
Q

Acyclovir

A

Mech: inhibits viral DNA polymerase,
*prodrug, selectively activated by viral thymidine kinase
Use: HSV & VZV (if immunocompromised), HSV encephalitis, transplant pt prophylaxis
SE: WELL tolerated :)

39
Q

Gancyclovir

A

Mech: inhibits DNA polymerase & suppresses chain elongation,
* prodrug (phosphorylated by CMV)
Use: to manage (NOT cure) CMV in immunocompromised pts
Route: oral or IV, crosses BBB. renal excretion
SE: toxicity limits dosing
(may co-treat w/ valgancyclovir or famcyclovir)

40
Q

AZT (aka: Zidovudine)

A

Mech: inhibits HIV reverse transcriptase (blocks reverse transcriptase) and inhibits chain elongation
Use: Tx/control HIV infections, reduce vertical transmission, post-exposure prophylaxis
SE: BM suppression/anemia, headaches, rashes, fever, diarrhea, insomnia (many ppl cannot tolerate it)

41
Q

Nevirapine

A

Mech: inhibits RT (reverse transcriptase), an “NNRTI”
*does NOT compete w/ nucleoside RT inhibitors (“nRTIs”)
Use: combo therapy of HIV-1
SE: Severe skin rxns, hepatotoxicity, DDI (bc CYP450 INDUCER)
*CYP450 metab. (risk DDIs, ie: reduces HIV protease inhibitor effect)

42
Q

Inidavir

A

Mech: HIV protease inhibitor (block polyprotein maturation)
Use: combo Tx for HIV (1 or 2, with other anti-retrovirals)
SE: –

43
Q

Enfuvertide

A

Mech: inhibits fusion of viral & cellular membranes
(synthetic AA, binds to gp41 subunit of HIV1)
Use: HIV-1 in “treatment-experienced patients” (w/ HIV replication still)
Route: subcut. injection 2x/day
SE: injection site rxn, pneumonia, hypersensitivity rxns, *NO DDIs

44
Q

Raltegravir

A

Mech: inhibits catalytic activity of HIV-1 integrase
Use: HIV-1 in treatment-experienced pts
SE: rhabdomyolysis, myopathy, (& headache, fatigue, etc.)

45
Q

Maraviroc

A

Mech: CCR5 coR antagonist (reversible), blocks interaction w/ HIV1
Use: only CCR5-tropic strains of HIV1 (adults)
SE: hepatoxicity & rash, allergic rxn
*CYP450 metab

46
Q

Why viral infections are hard to treat

A
  1. viruses = intracellular parasites, use host cell machinery to replicate
  2. replication starts before Sxs occur
  3. broad-selectivity not possible for anti-virals