Pharmacology - Midterm 2

Front 1

MOA of Cyclosporine

Back 1

Binds cylophilin and immunophilin which inhibits calcineurin and prevents IL2 prod and its receptor -> blocks differentiation and activation of T cells

calcineurin is a phosphatase for NFAT required for induction of cytokine genes

Front 2

Clinical use of Cyclosporine

Back 2

Organ transplants
Selected autoimmune (RA)

Front 3

Toxicity of Cyclosporins

Back 3

Predisposes to viral infections and lymphomas
Nephrotoxic

Front 4

MOA of Leflunomide

Back 4

Undergoes rapid conversion to A77-1726 which inhibits dihydroorotate dehydrogenase leading to decreased levels of UMP - cells arrest in G1
Lymphocytes lack salvage pathways and proliferate regularly (need pyrimadines 8x more than other cells) -> decreased autoimmune cells/antibodies

Front 5

Clinical use of Hydroxychloroquine

Back 5

anti malarial, used with MTX, sulfasalazine, as anti-inflamm

Leads to hemolysis in pts w G6P def

Front 6

Toxicity of hydroxychloroquine

Back 6

Corneal deposits - monitor
hemolysis in pts with G6PD def

Front 7

MOA of Azathioprene

Back 7

antimetabolite precursor of 6-MP interferes with nucleic acid synthesis
toxic to lymphocytes

Front 8

Clinical use of Azathioprene

Back 8

Kindey transplant, autoimmune, GN, hemolytic anemia

Front 9

Toxicity of Azathioprene

Back 9

BM suppression
metabolized by xanthine oxidase mercaptopurine
*pts receiving Azathioprene and Allopurinol for hyperuricemia need to decrease dosage of Azathiprene

Front 10

MOA of Mycophenolate mofetil

Back 10

converted to mycophenolic acid
inhibits guanine synthesis -> decreased lymphocyte prod
*does not affect salvage pathway
Blocks inosine monophosphate dehydrogenase (IMPDH) - rate limiting

Front 11

Erythropoietin (epoetin) MOA

Back 11

EPO receptor is a member of JAK/STAT superfam. increases prolif and differentiation
Increases reticulocyte release

Front 12

EPO AE

Back 12

>12Hb -> HTN, thrombotic complications
promotion of angiogenesis

Front 13

Darbepoitin

Back 13

long lasting EPO - added 2 carbon chains

Front 14

Filgrastim
Sargramostim
MOA

Back 14

G-CSF
GM-CSF

recovery of BM after chemo

Front 15

Interleukin 11 MOA/Use

Back 15

Megakayocyte GF
use is for thrombocytopenia after cancer chemo

Front 16

BChE polymorphism

Back 16

pts with this plymorph cannot metabolize succinylcholine as well -> prolonged paralysis after exposure

Front 17

NAT 2 Polymorphism

Back 17

acetylates isoniazid
slow acetylators have increased levels -> neurotoxicity
increased chance of drug induced lupus by Procainamide and hydralazine

Front 18

CYP2D6 metabolizes these drugs

Back 18

antidepressants
antiarrhythmics
analgesics
debrisoquine - anti HTN
Spartein - oxytotic

Front 19

CYP2D6
homozygous
hetero/homo for wild type
multiple copies
Race

Back 19

Homozygous - poor metabolizers
Hetero/homo for wild type are extensive metabolizers
Multiple copies of CYP2D6 gene are untrametabolizers
Caucasians > asians - poor metabolizers

Front 20

CYP2D6 Drugs

Back 20

Metoprolol
Haloperidol
Opiods (codein & dextromethorphan)
Fluoxetine
Imipramine
Desipramine

poor metabolizers have AE if given normal dose of metopralol
Codein is ineffective if given in poor metabolizers since codein is converted to morphine (active) by CYP
Ultra rapid metabolizers can overdose on codein leading to resp depression at standard doses

Front 21

TPMT pharmacogenomics

Back 21

Catalyzes S-methylation of:
-6 mercaptopurine
-Azathiprine
Thiopurines have narrow TI -> life threatening myelosuppression

Caucasians TMPT*3A - low
Homozygous - increased suppression - give 1/3 of dose
TPMT*3C in asians - almost no *3A

Front 22

5- Lipoxygenase encoded by ALOX 5
pharmacogenomics

Back 22

promoter has variable number of tandem repeats (VNTRs)
normal =1 allele of 5 repeat
Homozygous for an allele with anything other than 5 -> less enzyme

respond less to 5 lioxygenase inhibitors
polymorphism doesn't effect asthma

Front 23

Heparin MOA

Back 23

Cofactor for activation of anti-thrombin 3
Decreases thrombin and factor Xa
Heparin does not work on thrombin that is already bound

Front 24

What do you need to monitor with Heparin?

Back 24

PTT

Front 25

Reversal of Heparin use?
High in?

Back 25

Protamine Sulfate
Arginine

Front 26

Low molecular weight heparin MOA
and benefits

Back 26

Acts moreso on Xa
Has better bioavailability than Heparin
Has a longer half life (2-4x)
Can be injected subcut (Vs IV)
No lab monitoring necessary
BUT not easily reversible

Front 27

Heparin induces thrombocytopenia

Back 27

Antibody develops to platelet factor 4 that destroys platelets and overactivates remaining ones resulting in:
thrombocytopenic
hypercoagulable state
IgG

Front 28

UFH - unfractionated heparin

Back 28

pentassach sequence accelerates inactivation of IIa by AT3 whereas LMWheparin has little acceleration of inactivation of IIa by AT3

Front 29

Lipirudin
Bivalirudin
Argatroban

Back 29

Directly inhibit thrombin
Used in pts with HIT
MONITOR PTT
No antidote
Independent of AT3
CAN inactivate fibrin bound thrombi

Front 30

Fondaparinux

Back 30

Synthetic pentasaccharide
binds to AT3 and induces conformational change in AT required for binding to Xa
Sp inhibitor of Xa which has negligable AT (works through AT to affect Xa but no effect to AT) activity
Use: DVT - 1 a day SC injection

Front 31

Warfarin MOA

Back 31

Interferes with gamma-carboxylation of Vit K dependent clotting factors (2,7, 9, 10 Protein C, S - 7 has shortest half life)
Metabolized by CYP450

Front 32

Monitor what when on warfarin?

Back 32

PT

Front 33

Use/Contraindications of Warfarin/coumadin

Back 33

Chronic anticoag
DO NOT use in pregnancy - crosses placenta - unlike helparin - teratogenic
Causes skin/tissue necrosis if reduced levels of Protein C

Front 34

Hep/warf:
Structure
Route of Admin
site of action
duration of action

Back 34

Hep - large anionic, acid polymer, parenteral, blood, seconds
Warfarin - small lipid sol, oral, liver, slow - limited by 1/2 lives of normal clotting factors

Front 35

chelator for Fe

Back 35

Deferoxamine
binds Fe that is already absorbed and excretes it in urine/feces

Front 36

Thrombolytics

Back 36

tPA
Urokinase
Streptokinase
Anistreplase

Front 37

MOA (tPA, urokinase, streptokinase, anistreplase)
Clinical Use

Back 37

tPA, urokinase, streptokinase, Anistreplase
activate plasminogen to plasmin

plasmin breaks fibrin and fibrinogen to degradation products and d-dimers
increase PT & PTT

Early MI, early Stroke

Front 38

Aminocaproic acid MOA

Back 38

inhibits plaminogen to plasmin
inhibits fibrinolysis

Front 39

Abciximab MOA

Back 39

monoclonal Ab that binds to activated platelet glycoproteins IIb,IIIa.

Front 40

Abciximab Use

Back 40

Acute coronary syndromes
percutaneous transluminal coronary angioplasty

Front 41

Cell cycle inhibitors of
Vinca alkaloids and taxols

Back 41

M

Front 42

Cell cycle inhibitors of
Bleomycin

Back 42

G2

Front 43

Cell cycle inhibitors of
Etoposide

Back 43

S/G2

Front 44

Cell cycle inhibitors of
Antimetabolites

Back 44

S

Front 45

Anti ca drugs against nucleotide synthesis

Back 45

Methotrexate, 5-FU ->
thymidine synthesis ->
6MP
decrease purine synthesis

Front 46

Anti ca drugs against DNA synthesis

Back 46

Alkylating agents, cisplatin:
cross link DNA
Dactinomycin, doxorubicin:
intercalate DNA
Etoposide:
inhibits topoisomerase II

Front 47

Anti ca drugs against cellular division

Back 47

Vinca alkaloids: inhibit microtubule formation
Paclitaxel: inhibits microtubule disassembly

Front 48

Methotrexate MOA

Back 48

Folic acid analog
inhibits dihidrofolate reductase
decreases dTMP

Front 49

Methotrexate Use

Back 49

Leuk/lymph, chorio ca
Abortion, ectopic preg, RA, psoriasis

Front 50

Methotrexate contraindications and remedy

Back 50

Myelosuppression - REVERSIBLE w Leucovorin
Hepatotoxicity, cirrhosis, renal damage
Pregnancy category X

Front 51

5-FU MOA

Back 51

Pyrimidine analogue bioactivated to 5F-dUMP which covalently complexes folic acid
Inhibits thymidylate synthase -> decrease thymidylate synthase -> decrease protein synthase

Front 52

5-FU Use

Back 52

Colon Ca, BC, Ovarian, Pancreatic, basal cell/malig keratosis
Synergistic with MTX

Front 53

5-FU AE

Back 53

Myelosuppression - NOT REVERSIBLE with leucovorin.
Overdose rescue with thymidine
Hand and foot syndrome

Front 54

6-MP MOA

Back 54

Purine analogue
activated by HGPRTase to TIMP which inhibits first stem in de novo synthesis of purines

TIMP:
decreases IMP
decreases feedback inhibition of phosphoribosylamine synth
thioGMP - non funcitonal RNA

Front 55

6-MP use

Back 55

leuk/lymph, ALL remission, Crohns
NOT CLL OR HODGKINS

Front 56

6-MP AE

Back 56

Metabolized by xanthine oxidase - > increased toxicity with Allopurinol
Genotyping required b4 therapy for TPMT

Front 57

This purine analogue can be used with Allopurinol

Back 57

6-TG

Front 58

This antimetabolite is ACTIVATED by HGPRTase

Back 58

6-TG, 6-MP

Front 59

Antimetabolite used for Crohns

Back 59

6-MP

Front 60

Antimetabolite used for ALL maint

Back 60

MTX,6-MP

Front 61

DOC for AML

Back 61

Cytarabine

Front 62

Antimetabolite which inhibits DNA polymerase

Back 62

Cytarabine

Front 63

Rescue for 5-FU

Back 63

Thymidine

Front 64

Hand and foot syndrome caused by?

Back 64

5-FU

Front 65

Capecitabine MOA

Back 65

oral prodrug of 5-FU
phosphorylated via thymidine phosphorylase

Front 66

Antimetabolite Category D in pregnancy

Back 66

capecitabine

Front 67

Antimetabolite contraindicated with coumadin and phentoin

Back 67

Capecitabine

Front 68

Antimetabolites specific or nonspecific to cell cycle?

Back 68

S Phase specific

Front 69

Gemcitabine MOA

Back 69

phosphorylates to triphos via ribonucleotide reductase
inhibits DNA synthesis via incoporating into strands that usually contain cytosine

Front 70

Gemcitabine Use

Back 70

advanced pancreatic, NSCLC, Ovarian

Front 71

DOC for Gestational choreo Ca
what other drug do you use with it

Back 71

Dactinomycin
MTX

Front 72

DOC for Wilm's tumor
What drug do you give with it

Back 72

Dactinomycin
Vincristine

Front 73

Dactinomycin MOA

Back 73

Intercalates DNA

interferes with DNA dependent RNA polymerase

Front 74

Anthracyclines (names)

Back 74

Doxorubicin (Adriamycin)
Daunorubicin

Front 75

Anthracyclines MOA

Back 75

Create free radicals via CYP P450 reductase and NONCOVALENTLY intercalate in DNA

Binds to cell mem and alters fluidity of membrane

Inhibits Topo II

Front 76

Resistance in anthracyclines

Back 76

efflux pump
inc glutathione activity
mutation in Topo II
enhanced ability to repair DNA breaks

Front 77

ABVD

Back 77

Adriamycin
Bleomycin
Vincristine
Dacarbazine

Front 78

Toxicity of Anthracyclines (4)

Back 78

Cardiotoxicity
Myelosuppression
Extravasation (dark veins & urine)
Radiation Recall

Front 79

MOA of Bleomycin

Back 79

Copper chelating gp
causes DNA scission by oxidation

Front 80

Bleomycin works on what enzyme
Where is it most/least found
toxicities?

Back 80

Hydrolase
highest in Liver/spleen
lowest in lung/skin
Tox: Pulm fibrosis
Skin changes, hyperpigmentation
MINIMAL MYELOSUPPRESSION

Front 81

How do you deliver Epipodophyllatoxins and why?

Back 81

Cremphor vehicle bc it is not soluble in H2O

Front 82

Which antitumor antibiotics are phase specific?

Back 82

Epipodophyllotoxins (S-G2)
Bleomycin (G2)

Front 83

MOA of Etoposide/teniposide

Back 83

Inhibits topoisomerase II

Front 84

Clinical use of bleomycin

Back 84

Testicular Ca + etoposide, cisplatin, vincristine
PVB (Platinol (cisplatin), vincristine, Bleo),
PEB (Platinol, Etoposide, Bleo)
Part of ABVD for Hodgkins

Front 85

Clinical Use of Etoposide

Back 85

SCLC, NSCLC
Germ cell cancers
Testicular Ca
Hodgkin and non
Gastric Ca

Front 86

Teniposide Use

Back 86

Refractory ALL

Front 87

Are alkylating agents specific?

Back 87

no

Front 88

Chloambucil
Cyclophosphamide
Ifosphamide
MOA

Back 88

Covalent x-linked to DNA at Guanine N-7
*Requires bioactivation from liver
Ifosfamide - 3A4
Cyclophosphamide - P2B

Front 89

Causes Hemorrhagic Cystitis?
Due to what metabolite?
What should you administer?
Other toxicities?
Administered?

Back 89

Cyclophosphamide
Acrolein
Mesna
Increased risk of neoplasia
Affects germ cells
Orally

Front 90

Clinical use of cyclophosphamides

Back 90

Leuk/lymph
Breast, ovarian
Immunosuppressants

Front 91

Nitrosureas (3)

Back 91

Carmustine (unstable)
lomustine
semustine

Front 92

Nitrosureas stable orally

Back 92

Semustine, lomustine

Front 93

Neurotoxic metabolite of cyclophosphamide

Back 93

Chloracetylaldehyde

Front 94

Nitrosureas directly active?
Clinical use?
Toxicities?

Back 94

Require bioactivation
Brain tumors
MM
Hodgkins
CNS toxicity

Front 95

Busulfan MOA
Use
Coadmin with

Back 95

Alkylates DNA
CML
Pulm fibrosis
Addisons like syndrome
Coadmin with Allopurinol

Front 96

Carmustine Toxicity

Back 96

Aplastic marrow in long term use
Hepatic toxicity

Front 97

FDA category D mutagenic and teratogenic oxidative cytotoxic agent

Back 97

Methyl hydrazine

Front 98

Methyl hydrazine clinical use
Toxicity

Back 98

Hodgkins
FDA category D mutagenic and teratogenic
Inhibits MAO - contraindication with beer, wine and aged food

Front 99

Mechlorethamine MOA

Back 99

Binds to 2 separate nts and alkylates N7 of guanine causing breakage and miscoding mutations

Front 100

Mechlorethamine use

Back 100

Chronic lymphomas
lymphosarcoma

Front 101

Mechlorethamine toxicity (4)
Tx for extravasation

Back 101

extreme blistering
SEVERE nausea - give dexamethasone
Menstrual abn
BM depression - dose dep
Na thiosulfate for extravasation

NO nephrotoxicity

Front 102

Melphalan use:
Toxicity

Back 102

MM
The usual Alopecia is INFREQUENT!

Front 103

Dacarbazine transformed into?
By?

Back 103

MTIC (Methyltriazenoimidazole carboxymide)
CYP450

Front 104

Dacarbazine MOA
Use

Back 104

DNA methylation
Melanoma
Hodgkins - 2nd line

Front 105

Melphalan use:
Toxicity

Back 105

MM
The usual Alopecia is INFREQUENT!

Front 106

Dacarbazine transformed into?
By?

Back 106

MTIC (Methyltriazenoimidazole carboxymide)
CYP450

Front 107

Dacarbazine MOA
Use

Back 107

DNA methylation
Melanoma
Hodgkins - 2nd line

Front 108

Campothecans MOA
Cell specific?

Back 108

Inhibit topo I
S phase sp leads to arrest in G2

Front 109

Irinotecan use
toxicity

Back 109

Mets Colon Ca
GI toxicity, myelosuppresion -> dose limiting

Front 110

Topotecan use
toxicity

Back 110

Mets Ovarian, cervical, SCLC
myelosppresion -> dose limiting, GI toxicity, alopecia

Front 111

Vinorelbine
Vincristine
Vinblastine
MOA
Phase specific?

Back 111

Alkaloids bind to tubulin in M phase and block polymerization - mitotic spindle can't form

Front 112

MOPP

Back 112

Mechlorethamine
Onchovin (vincristine)
Procarbazine
Prednisone

Used for Hodgkins or medulloblastoma

Front 113

Vincristine use
toxicity
Coadmin

Back 113

MOPP for Hodgkins, ALL, Wilms, Ewings
Neurotoxicity - peripheral neuropathy
Hyperuricemia - give allopurinol

Front 114

Vinblastine use
toxicity
Coadmin

Back 114

Mets Testicular Ca (+bleo +cis), hodgkins, non, kaposis, chorio
Bone marrow suppression
Hyperuricemia - give allopurinol

Front 115

Paclitaxel
use, toxicity
Docetaxel
use, toxicity

Back 115

Paclitaxel: adv ovarian, mets breast, NSCLC (+cisplatin)
AE: Myelosuppression (does limiting), hypersensitivity
peripheral neuropathy
Docetaxel:same applications fewer AE

Front 116

Docetaxel coadmin with?

Back 116

Dexamethasone
Diphenhydramine

Front 117

Microtubule inhibitors metabolized by?

Back 117

CYP450

Front 118

Vinorelbine use

Back 118

Advanced NSCLC

Front 119

Cisplatin
Carboplatin
Oxaliplatin
AE:
Coadmin:
least nephrotoxic:

Back 119

Nephrotoxicity (dose limiting - requires aggressive hydration), acoustic nerve damage
Coadmin with amifoostine
least nephrotoxic carboplatin

Front 120

Cisplatin
Carboplatin
Oxaliplatin
use:
MOA:
Stage of life cycle?

Back 120

Testicular (BEP)
Bladder, ovary (intraperitoneally +cyclophosphamide)
Cross links DNA
At all stages of life cycle

Front 121

Oxiplatin use:

Back 121

Adv colon Ca

Front 122

2 drugs which inhibit ribonucleotide reductase

Back 122

hydroxyurea
Gemcitabine

Front 123

Hydroxyurea
phase of cell cycle?
Use?
MOA

Back 123

S
Sickle cell (inc HbF), CML, ALL blast crisis, ovarian, Melanoma
inhibits ribonubleotide reductase which dec deoxy nucleotide triphosphate pools

Front 124

Toxicity of Hydroxyurea

Back 124

Cutaneous vasculitis
GI
BM

Front 125

MOA of Prednisone
Use
Toxicity

Back 125

triggers apoptosis - binds recepton and produces specific proteins
Used for lymphomas
part of MOPP for hodgkins
Autoimmune diseases - hemolytic anemia, thrombocytopenia
Cushing like sx
+ glaucoma

Front 126

Ethinylestradiol/DES
MOA

Back 126

suppress pituitary LH secretion which decreases testosterone -> decreases prostatic growth
Replaced by GnRH d/t AE

Front 127

AE of estrogens in prostate ca

Back 127

Thromboemboli, stroke, hyperCa, gynecomastia, impotence, libido

Front 128

Aminoglutethemide/Aromatase inhib. MOA
Coadmin with
Clinical use
AE

Back 128

inhibit aromatase - turns andrestenedione to estrone in body fat
Coadmin with hydrocortisone
Post menopausal mets Breast Ca.
AE - visual dist, adrenal insuff, myelosuppresion

Front 129

Erlatinib
LapatiNIB
Gigitinib
Cefuximab
MOA
Use

Back 129

all inhibit EGFR
Erlotinib - ErbB1
Lapatinib - ErbB2
Erlotinib and Lapatinib both for NSCLC and Pancreatic Ca
Gefitinib - NSCLC
Cefuximab - Colorectal and H&N AE- interstitial lung disease

Front 130

Trastuzumab
MOA
Use
AE

Back 130

Herceptin
Ab against HER-2 (erb-B2)
Mets Breast Ca
Cardiotoxicity -> CHF

Front 131

Imatinib
MOA
Use
AE

Back 131

Gleevac
bcr-abl tyrosine kinase inhib
CML, GIST
Fluid retention

Front 132

Cocktail for Colon Ca

Back 132

5 FU
Leucovorin

Front 133

Anastrozole
Letrozole
MOA
Use
AE

Back 133

reversible competative, nonsteroidal aromatase inhib
mosre selective than AMINOGLUTETHAMIDE - no need for hydrocortisone
no predisposition for endometrial Ca
Estrogen R + breast cancer
mild AE

Front 134

Exemestane
Formestane

Back 134

Steroidal irreversible inhibitors of aromatase
Mild AE

Front 135

Hydroxyprogesterone
Megestrol Progestin
MOA
Use
AE

Back 135

Aromatase inhibitor - replace it in therapy
Breast, endometrial Ca (2nd line)
Stimulates appetite - give to pts with AIDS, adv cancer

Front 136

Fluoxymesterone
Testosterone
Use

Back 136

Palliative care for pts with BC

Front 137

Sorafenib
MOA
Use

Back 137

inhibits serine/threonine kinase RAF
renal cell Ca

Front 138

Bortezomib
MOA
Use

Back 138

inhibits proteosome - growth inhibition and apoptosis of tumor cells (not much toxicity)
MM, Mantle cell lymphoma

Front 139

Sunitimib
MOA
Use

Back 139

angiogenesis inhib - inhibits VEGFR-1,2 & PDGFR
Renal cell Ca & GIST

Front 140

L - Asparaginase
MOA
Use
AE

Back 140

Neoplastic cells have lowe levels of asparagine synthetase, without asparagine no protein synthesis can occur and toxic metabolites aspartic acid and ammonia accum in cell
ammonia responsible for AE
ALL + VX +Prednisone
AE ammonia tox, hypersensitivity, liver abnormalities, pancreatitis, seizures, coma

Front 141

Arsenic trioxide
MOA
Use
AE

Back 141

Induces differentiation and apoptosis
M3 with t(15:17)
AE - QT elongation, arrythmias, FDA Category D

Front 142

Protease inhibitors mneumomic

Back 142

Navir tease a pretease

Front 143

Ritonavir
MOA
use

Back 143

protease inhibitor - enhances other protease inhibitors EXCEPT Nelinavir

Front 144

MOA of protease inhibitors
Contraindications

Back 144

inhibit maturation of new virus by blocking protease in progeny
All PIs are CYP3A4 inhibitors DO NOT COMBINE WITH ST JOHNS WORT
RIFAMPIN

Front 145

Tipranavir AE

Back 145

Severe & fatal hepatitis
intracranial hemorrhages

Front 146

Saquinavir & Nelfinavir absorption?
Indinavie absorption?

Back 146

increase with fat absorption
decrese with fat absorption

Front 147

used for general prophylaxis during pregnancy for HIV

Back 147

Ziduvodine

Front 148

Lamivudine
MOA
Resistance

Back 148

Inhibits HBV DNA polymerase
doesn't affect mitochndrial DNA synthesis
Res: single substitution

Front 149

Adefovir
MOA

Back 149

Incorporates into viral DNA which terminates DNA synth
Discontinued d/t hep exacerbation, use cautiously with renal dys

Front 150

Entecavir
MOA
Use

Back 150

competes with triphosphate for viral RT
Use for Amivodine resistant strants of HBV

Front 151

Telbivudine
MOA
Use

Back 151

Competes with thymidine triphosphate or incorporates in viral DNA
HBV - NOTHING ELSE

Front 152

RT Nucleosides mneumonic

Back 152

Ha VUDINEd with my nuclear family

Front 153

Resistance in RT Nucleosides

Back 153

mutation in viral codon

Front 154

MOA of RT Inhib

Back 154

inhibits RT of HIV preventing the viral DNA from incorporating into host DNA

Front 155

Nucleoside sp RT Inhib
MOA

Back 155

Lack OH group
needs to become triple phosph to become active

Front 156

Stavudine
MOA
AE

Back 156

Nucleoside - inhibits beta, gamma DNA Polymerase which decreases mitochondrial DNA synth ->tox
AE - peripheral neuropathy
lipodystrophy, hyperlipidemia

Front 157

Zidovidine
MOA
AE

Back 157

Prophylaxis of prenatal infection
AE: BM, GI
Contraindications:
PROBENICID, ACETOMINOPHEN,
LARAZEPAM, INDOMETHACIN, CIMETADINE

Front 158

Abacavir
MOA
AE

Back 158

Guanoside analogue
Hypersensitivity - NEVER RECHALLENGE
Genetically screen

Front 159

Lamivudine
made up of?
MOA
AE
Resistance

Back 159

Tenofivir + Zidovudine
No effect on mitochondria DNA
used for HBV and HIV
Resistance d/t single substitution

Front 160

Emtricitabine
MOA

Back 160

relative of Lamivudine
few AE
1/day

Front 161

Tenofovir
Admin

Back 161

Drug interations, dose reduction
boost with Ritonavir which increases conc of didanasine
give 1/day

Front 162

Didanosine
Admin
AE

Back 162

Take on an empty stomach or with antiacids
AE: pancreatitis, Peripheral neuropathy

Front 163

Non-Nucleosides
MOA
Advantages

Back 163

Do not require activation
Highly selevctive non-competative

Front 164

Nevirapine
MOA
AE
Resistance

Back 164

CYP3A4, 2B6
AE: Rash - Steven Johnson + epidermal necrolysis - titrate dose at 1/2 for 2 wks
CYP3A4 inducer - induces protease inhibition, oral contraceptives, ketoconazole, methadone, metronidazole, quinidine, theophyline, warfarin
Resistance develops rapidly

Front 165

HIV therapy contraindicated: Category D in pregnancy

Back 165

Efavirenz

Front 166

Preferred NNRTI

Back 166

Efavirenz

Front 167

Efavirenz
AE
Dose

Back 167

Rash
potent inducer of CYP P450
Pregnancy D
1/day

Front 168

Fusion inhibitor:
MOA
Toxicity
Use

Back 168

Enfuvirtide
Bings gp41 subunit - inhibits conformational change required for fusion with CD4 cells - blocks entry
Hypersens, subcutaneous rxns, inc risk of bacterial pneumonia
Used in pts with persistent viral replication despite antiretroviral therapy

Front 169

Maraviroc
MOA
Metabolism

Back 169

blocks CCR5 coreceptor w/ gp41 - prevents entry
CYP3A4 metabolism

Front 170

Raltegravir
MOA
Metabolism

Back 170

Inhibits integrase strand transfer into host via UGTIAI
NO CYP INTERACTIONS

Front 171

Vidarabine
MOA
Toxicity
Use

Back 171

Adenine analogue inhibits DNA synth after triphos conversion
TX of herpatic and vaccinal keratitis and HSV keratoconjunctivitis (opthalmic ointment)
AE: Superficial punctate keratitis, photophobia, pain

Front 172

Triflurodine
MOA
Use

Back 172

Thymidine analogue
HSV1, 2, Vaccina virus
DOC for HSV Keratoconjunctivitis and epithelial keratitis
Need to apply very frequently t1/2 is 12 min

Front 173

DOC for keratoconjunctivitis and epithelial keratitis

Back 173

Triflurodine

Front 174

HIV prophylaxis after needlestick

Back 174

less severe 2 NRTI (AZT Lami)
More severe 2 NRTI +
PI or NNRTI