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PCM1 > RHS Antimycobacterials, Antimalarials, & Chemo > Flashcards

RHS Antimycobacterials, Antimalarials, & Chemo Flashcards

1
Q

Rifampin

A

Rifamycin. Part of RIPE (first-line anti-Tb drugs). Also part of DR Clof (for Leprosy)

Inhibitor of bacterial RNA polymerase

Resistance: point mutations in rpoB gene (gene for b subunit of RNA pol)

AE: Red body fluids, nephrotoxicity, rashes, hepatotoxicity

CYP inducer, Safe in pregnancy

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2
Q

Rifabutin

A

Rifamycin. Part of RIPE (first-line anti-Tb drugs).

Inhibitor of bacterial RNA polymerase

Resistance: point mutations in rpoB gene (gene for b subunit of RNA pol)

AE: Red body fluids, nephrotoxicity, rashes, hepatotoxicity

Not a CYP inducer so preferred into Rifampin in HIV patients.

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3
Q

Isoniazid

A

Part of RIPE (first-line anti-Tb drugs).

Mycolic Acid synthesis inhibitor

Resistance: deletion of Kat G- catalase peroxidase (high resistance), overexpression of inhA and KasA (low resistance)

AE: Neurotoxicity (treatable with vit B6), Lupus-like syndrome, Hemolysis in G6PD, Hepatotoxicity!!

CYP inhibitor. Safe in pregnancy. Metabolized by N-Acetyltransferase so higher dose needed in fast acetylator.

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4
Q

Pyrazinamide

A

Part of RIPE (first-line anti-Tb drugs).

MOA unclear. Is activated by hydrolysis by mycobacterial pyrazinamidase (pncA).

Resistance: Impaired uptake or mutations in pncA

AE: Non-gouty polyarthalgia, Hyperuricema (not given in gout), Hepatotoxicity, Myalgia, Porphyria, Photosensitivity.

Can be given in pregnancy but has risks.

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5
Q

Ethambutol

A

Part of RIPE (first-line anti-Tb drugs).

Inhibits arabinosyltransferases (emb) leading to decreased carbohydrate polymerization of bac cell wall.

Resistance: Mutations/Overexpression of emb.

AE: Visual disturbance, colorblindness, retinal damage. Not given in children too young to assess for colorblindness.

Safe in pregnancy.

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6
Q

Streptomycin

A

Part of SEAL (2nd line anti-Tb drugs)

Aminoglycoside: binds 30s subunit, inhibits bacterial ribosome.

AE: Ototoxicity, Nephrotoxicity, Unsafe in pregnancy.

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7
Q

Ethionamide

A

Part of SEAL (2nd line anti-Tb drugs)

Isoniazid-like. Inhibits mycolic acid synthesis.

AE: GI upset, neurotoxicity (alleviated by Vit B6)

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8
Q

Amikacin

A

Part of SEAL (2nd line anti-Tb drugs)

Aminoglycoside: binds 30s subunit, inhibits bacterial ribosome.

AE: Ototoxicity, Nephrotoxicity, Unsafe in pregnancy.

Is still effective in multidrug-resistant strains of TB

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9
Q

Levofloxacin

A

Part of SEAL (2nd line anti-Tb drugs)

Fluoroquinolone. Inhibits bacterial DNA gyrase

AE: Tendinopathy. Unsafe in pregnancy.

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10
Q

Dapsone

A

Part of DR Clof- treatment for Leprosy.

Inhibits folate synthesis via dihydropteroate synthetase inhibition.

AE: Hemolysis in G6PD. Methemoglobinema (Fe3 hemoglobin), Erythema nodosum leprosum.

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11
Q

Clofazimine

A

Part of DR Clof- treatment for Leprosy. Only given in Multi-bacillary leprosy.

Binds bacterial DNA, inhibits replication.

AE: Discoloration of skin and conjunctiva.

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12
Q

Methotrexate

A

Antimetabolite: Folate Analog

Inhibits dihydrofolate reductase (DHFR), decreasing synthesis of dTMP & purines. Effect potentiated by conversion to polyglutamates (MTX-PG) by folylpolyglutamate synthase (FPGS).

Kills cells in S phase.

Resistance via: Decreased influx, decreased FPGS activity, Altered or amplified DHFR.

AE: Stomatitis, mucositis, BM sup, thrombocytopenia, erythema, rash, alopecia, N/V. Nephrotoxic at high doses. Hepatotoxic. Pneumonitis. Neurotoxic if administered into CSF (spinal).

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13
Q

Leucovorin

A

Folate Analog

Decreases BM suppressive effect of Methotrexate.

Potentiates 5-FU.

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14
Q

6-Mercaptopurine

A

Antimetabolite: Purine Analog (Thiol analog of hypoxanthine)

Converted to 6-MPRP/TIMP by HGPRT. TIMP inhibits first step of denovo purine synthesis & blocks formation of AMP & GMP from IMP.

Resistance: HGPRT deficiency, increased metabolism of drug, increased dephosphorylation.

AE: N/V, diarrhea, BM sup, hepatotoxicity.

Special: Used in Acute Lymphatic Leukemia. Dose needs to be reduced in poor TMPT metabolizers. Dose needs to be reduced if given with allopurinol (allopurinol inhibits enzyme that metabolized 6-MP to inactive form).

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15
Q

6-Thioguanine

A

Antimetabolite: Purine Analog

Converted to TGMP by HGPRT. TGMP inhibits purine ring synthesis & phosphorylation of GMP to GDP.

AE: N/V, diarrhea, BM sup, hepatotoxicity.

Special: Used in Acute non-lymphocytic Leukemia. Dose needs to be reduced in poor TPMT metabolizers. No Allopurinol interactions.

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16
Q

5-Fluorouracil

A

Antimetabolite: Pyrimidine Analog

Converted to 5-FdUMP which inhibits formation of dTMP from dUMP. Causes thymine-less death. Also converted to 5-FUTP which is incorporated into RNA. Given IV due to GI toxicity.

Resistance: No conversion to 5-FdUMP, altered thimydilate synthase, increased catabolism of 5-FU.

AE: N/V, diarrhea, alopecia, GI ulceration, BM sup, anorexia. Dermatopathy: Hand-Foot syndrome.

Special: Used in colorectal cancer (with Leucovorin)

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17
Q

Cytarabine

A

Antimetabolite: Pyrimidine Analog

Converted to ara-CTP, incorporated into DNA, inhibits DNA polymerase. Not orally effective.

AE: N/V, diarrhea, Severe BM sup, hepatotoxicity, seizures or AMS.

Special: Used in acute non-lymphocytic leukemia.

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18
Q

Doxorubicin

A

Antitumor Antibiotic: Anthracycline

Topoisomerase II inhibition, DNA intercalation, iron-dependent generation of free radicals which break DNA strands, altering membrane ion transport & fluidity.

Resistance: P-glycoprotein increased efflux, glutathione peroxidase increase, mutation in topoisomerase 2.

AE: BM suppression, cardiotoxicity (can be alleviated with dexrazoxane).

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19
Q

Daunorubicin

A

Antitumor Antibiotic: Anthracycline

Topoisomerase II inhibition, DNA intercalation, iron-dependent generation of free radicals which break DNA strands, altering membrane ion transport & fluidity.

Resistance: P-glycoprotein increased efflux, glutathione peroxidase increase, mutation in topoisomerase 2.

AE: BM suppression, cardiotoxicity (can be alleviated with dexrazoxane).

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20
Q

Bleomycin

A

Antitumor Antibiotic.

Mixture of glycopeptides. Binds to DNA, generates free radicals which cause strand breakage.

Resistance in tissues with Bleomycin hydrolase.

AE: Very mild BM sup. Pulmonary toxicity!

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21
Q

Mechlorethamine

A

Alkylating Agent: Nitrogen Mustard

Cytotoxic by transfer of alkyl groups to DNA.

AE: N/V, severe BM sup, alopecia.

Special: Unstable & causes blisters (given IV only). Largely replaced by cyclophosphamide & other agents.

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22
Q

Cyclophosphamide

A

Alkylating Agent: Nitrogen Mustard

Cytotoxic by transfer of alkyl groups to DNA. Prodrug activated by CYP2B. Most widely used.

AE: N/V, BM sup, Hemorrhagic cystitis!!!, Alopecia, Sterility.

Special: Hemorrhagic cystitis caused by Acrolein metabolite. Prevented thru adequate fluid intake + Mesna.

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23
Q

Mesna

A

Sulfhydryl compound which neutralizes acrolein in the bladder.

Prevents Hemorrhagic Cystitis adverse effect of Cyclophosphamide & Ifosfamide.

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24
Q

Ifosfamide

A

Alkylating Agent: Nitrogen Mustard

Cytotoxic by transfer of alkyl groups to DNA. Analog of Cyclophosphamide. Prodrug activated by hydroxylation by CYP3A4.

AE: Greater BM sup, Neurotoxicity, Greater urinary tract toxicity. Only given with adequate hydration & mesna.

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25
Q

Melphalan

A

Alkylating Agent: Nitrogen Mustard

Cytotoxic by transfer of alkyl groups to DNA.

AE: BM sup

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26
Q

Carmustine

A

Alkylating Agent: Nitrosoureas

Cytotoxic by transfer of alkyl groups to DNA.

Very lipophilic, crosses blood-brain barrier, treats brain tumors.

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27
Q

Lomustine

A

Alkylating Agent: Nitrosoureas

Cytotoxic by transfer of alkyl groups to DNA.

Very lipophilic, crosses blood-brain barrier, treats brain tumors.

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28
Q

Busulfan

A

Alkylating Agent

Cytotoxic by transfer of alkyl groups to DNA.

AE: BM sup!, Pulmonary fibrosis!

29
Q

Dacarbazine

A

Alkylating Agent

Cytotoxic by transfer of alkyl groups to DNA. Prodrug activated in the liver.

AE: N/V, BM sup.

30
Q

Procarbazine

A

Alkylating Agent

Cytotoxic by transfer of alkyl groups to DNA. Prodrug activated in the liver.

AE: N/V, BM sup, MAO inhibitor- hypertensive reactions with tyramine foods or sympathetic agents, disulfuram-like reactions, teratogen.

31
Q

Cisplatin

A

Platinum Coordination Complex

Cytotoxic by covalently bonding to DNA & cross-linking.

AE: N/V, Ototoxic, Peripheral Neuropathy, Nephrotoxic, BM sup.

Special: Treatment of Testicular & Ovarian cancer. Treatment of cancers of head, neck, bladder, esophagus, lung & colon. Amifostine can reduce nephrotoxicity.

32
Q

Carboplatin

A

Platinum Coordination Complex

Cytotoxic by covalently bonding to DNA & cross-linking.

AE: Dose-limiting myelosuppression. Also N/V, neurotoxic, ototoxic, nephrotoxic- but these are less than in Cisplatin.

Special: Treatment of Testicular & Ovarian cancer. Treatment of cancers of head, neck, bladder, esophagus, lung & colon.

33
Q

Amifostine

A

Reduces Nephrotoxicity of Cisplatin.

34
Q

Vincristine

A

Microtubule Inhibitors: Vinca Alkaloid

Destabilizing agents, arresting cells in metaphase.

AE: Severe Peripheral Neuropathy, mild BM sup, Alopecia

35
Q

Vinblastine

A

Microtubule Inhibitors: Vinca Alkaloid

Destabilizing agents, arresting cells in metaphase.

AE: Peripheral Neuropathy, severe BM sup, Alopecia

36
Q

Paclitaxel

A

Microtubule Inhibitors: Taxane

Stabilizing agent, arrests cells in mitosis.

AE: Hypersensitivity, BM sup, peripheral neuropathy, alopecia.

Special: Hypersensitivity reduced by premedicating with dexamethasone, diphenhydramine & H2 blocker.

37
Q

Etoposide

A

Epipodophyllotoxin.

Topoisomerase 2 inhibitor. Arrests cells in late S, G2 phase.

AE: N/V, alopecia, BM sup.

38
Q

Topotecan

A

Camptothecin

Topoisomerase 1 inhibitor.

AE: BM sup, diarrhea.

39
Q

Irinotecan

A

Camptothecin

Topoisomerase 1 inhibitor.

AE: BM sup, diarrhea.

40
Q

Prednisone

A

Glucocorticoid

Steroid action suppresses lymphocytes

Used in acute leukemia & malignant lymphomas.

41
Q

Tamoxifen

A

Estrogen Inhibitor: Selective Estrogen-Receptor Modulator (SERM)

Estrogen antagonist in breast tissue. Estrogen agonist elsewhere. Activated by CYP2D6.

AE: Hot flashes, N/V, fluid retention, vaginal bleeding, venous thromboembolism, increased risk of endometrial cancer.

Use: Metastatic breast cancer. Preventative agent in women at risk for breast cancer. Avoid using with CYP2D6 inhibitors- Bupropion, Fluoxetine, Paroxetine.

42
Q

Raloxifene

A

Estrogen Inhibitor: Selective Estrogen-Receptor Modulator (SERM)

Estrogen antagonist in breast and uterus. Estrogen agonist in bone.

AE: Hot flashes, leg cramps, venous thromboembolism.

Use: Treatment & prevention of osteoporosis in postmenopausal women. Prophylaxis of breast cancer in postmenopausal women.

43
Q

Fulvestrant

A

Estrogen Inhibitor: Pure Estrogen Antagonist

Use: Treatment of metastatic breast cancer in post-menopausal woman when initial therapy fails.

44
Q

Anastrozole

A

Estrogen Inhibitor: Aromatase Inhibitor

Non-steroidal, reversible competitive inhibitor.

Use: Standard adjuvant treatment for breast cancer in postmenopausal women.

45
Q

Letrozole

A

Estrogen Inhibitor: Aromatase Inhibitor

Non-steroidal, reversible competitive inhibitor.

Use: Standard adjuvant treatment for breast cancer in postmenopausal women.

46
Q

Exemestane

A

Estrogen Inhibitor: Aromatase Inhibitor

Steroidal, irreversible inhibitor.

Use: Standard adjuvant treatment for breast cancer in postmenopausal women.

47
Q

Goserelin

A

Androgen Inhibitor: GNRH Agonist

Cause GNRH receptor desensitization, lowering FSH, LH and Androgen levels.

Use: Advanced prostate cancer, advanced breast cancer in premenopausal women, management of endometriosis.

Special: Flare phenomenon initially due to normal effects of GNRH receptor activation, countered by flutamide.

48
Q

Leuprolide

A

Androgen Inhibitor: GNRH Agonist

Cause GNRH receptor desensitization, lowering FSH, LH and Androgen levels.

Use: Advanced prostate cancer, advanced breast cancer in premenopausal women, management of endometriosis.

Special: Flare phenomenon initially due to normal effects of GNRH receptor activation, countered by flutamide.

49
Q

Flutamide

A

Androgen Inhibitor: Androgen Receptor Blocker

Prodrug. Blocks flare phenomenon of GNRH agonist.

50
Q

Gefitinib

A

EGFR Tyrosine Kinase Inhibitor

Use: Nonsmall cell lung cancer

51
Q

Erlotinib

A

EGFR Tyrosine Kinase Inhibitor

Use: Nonsmall cell lung cancer. Pancreatic cancer.

52
Q

Lapatinib

A

EGFR and Her2 tyrosine kinase inhibitor

Use: Breast Cancer with Her2 overexpression

53
Q

Imatinib

A

Bcr-Abl tyrosine kinase inhibitor

Use: CML, ALL, Myelodysplastic/Myeloproliferative diseases

54
Q

Trastuzumab

A

Monoclonal antibody against Her2 Tyrosine Kinase

Use: DOC for breast cancer with Her2 overexpression

55
Q

Bevacizumab

A

Monoclonal Antibody against VEGF

Use: Metastatic Colorectal cancer, non-small cell lung cancer, glioblastoma, renal cell carcinoma.

56
Q

Asparaginase

A

Hydrolyzes serum asparagine, depriving tumors of asparagine.

AE: Hypersensitivity, hepatotoxicity, decrease in clotting factors, pancreatitis, ammonia toxicity.

57
Q

Hydroxyurea

A

Ribonucleotide reductase inhibitor

Depletes DNA nucleotides, kills cells in S phase.

58
Q

INF-a

A

Use: Hairy Cell Leukemia, CML, malignant melanoma, Kaposi sarcoma.

59
Q

Chloroquine

A

DOC for non-falciparum and uncomplicated falciparum malaria.

Preferred chemoprophylactic agent in areas without resistant malaria.

AE: Hemolysis in G6PD. Can’t be given IV. Visual problems.

Special: Safe in pregnancy.

60
Q

Hydroxychloroquine

A

Alternative for chloroquine in chemoprophylaxis and treatment of uncomplicated malaria.

AE: Hemolysis in G6PD, visual problems, pruritus.

Special: Safe in pregnancy & children

61
Q

Quinine/Quinidine

A

First-line treatment for severe falciparum malaria. Treatment of CR uncomplicated falciparum & other species.

AE: Blackwater fever, uterine contractions, cinchonism, cardiotoxicity, hypersensitivity, hypoglycemia, cytopenia, hemolysis.

62
Q

Sulfadoxine + Pyrimethamine

A

No longer recommended because of resistance.

Folate synthesis inhibitors.

63
Q

Atovaquone + Proguanil (Malarone)

A

Treatment & prophylaxis of CR falciparum.

AE: Avoid in pregnancy, unknown safety.

Disrupts mitochondrial electron transport.

64
Q

Doxycycline

A

Treatment & prophylaxis of uncomplicated CR falciparum & other species. Treatment of severe falciparum.

AE: Photosensitivity, teeth discoloration, growth stunting, avoided in pregnancy and kids under 8.

Binds 30s ribosome.

65
Q

Clindamycin

A

Alternative to doxycycline in treatment of severe falciparum & uncomplicated malaria in pregnancy.

AE: Pseudomembranous colitis.

Safe in pregnancy & children.

66
Q

Mefloquine

A

Last resort treatment of severe falciparum. Only chemoprophylaxis for CR strains in pregnancy. Treatment of uncomplicated CR falciparum & other species.

AE: Neuropsychiatric, don’t administer with quinidine.

Safe in pregnancy & children.

67
Q

Artemisinin

A

Treatment of uncomplicated CR falciparum & other species. Treatment of severe falciparum (IV). Not used as prophylaxis.

Safe in pregnancy, more safety evidence in 2nd and 3rd trimesters.

68
Q

Primaquine

A

DOC for eradication of Vivax & Ovale hypnozoites. Only gametocidal agent. Prophylaxis of CRstrains.

AE: Hemolysis, Methemoglobinemia.

PCM1 (7 decks)

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