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Pharmacology > Exam 9 > Flashcards

Exam 9 Flashcards

1
Q

Nucleoside Reverse Transcriptase Inhibitors

A

Zidovudine, Didanosine, Lamivudine, Emtricitabine, abacavir

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2
Q

Nucleotide Reverse Transcriptase Inhibitors

A

Tenofovir

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3
Q

Non-Nucleoside Reverse Transcriptase Inhibitors

A

Nevirapine, Efavirenz

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4
Q

Protease Inhibiors

A

Ritonavir, Indinavir sulfate, Nelfinavir mesylate, Lopinavir/Ritonavir, Atanavir sulfate

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5
Q

NRTI’s

A
  1. inhibit HIV reverse transcriptase

2. generally do not interact with other drugs or meals

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6
Q

Didanosine

A

NRTI that interacts with other drugs

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7
Q

Zidovudine-AZT

A
  1. NRTI (tx HIV)
  2. synthetic dideoxynucleoside (pyrimadine) antiviral
  3. thymidine analogue. can’t form phosphodiester linkages. lacks 3’ hydroxyl. leads to chain termination
  4. converted intracellularly to active triphosphate
  5. Plasma protein bound
  6. SE: anemia, neutropenia, bone marrow tox, granulocytopenia, CNS, GI
  7. CONTRAINDICATIONS: compromised bone marrow fxn
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8
Q

Combivir

A

lamivudine + zidovudine

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9
Q

Trizivir

A

lamivudine + zidovudine + abacavir

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10
Q

Drug that you do NOT give with Zidovudine

A

Stavudine. (antagonism)

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11
Q

Didanosine

A
  1. NTRI (tx HIV)
  2. Dideoxynucleoside (purine)
  3. inhibitor of reverse transcriptase by COMPETING with dATP for active site of enzyme
  4. converted to active triphosphate in cell
  5. lacks 3’ hydroxyl group. leads to chain termination
  6. absorption depends on food and pH
  7. SE: peripheral neuropathy, pancreatitis, GI
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12
Q

Zerit

A

DIdanosine + Zidovudine (or stavudine)

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13
Q

Lamivudine

A
  1. NTRI (tx HIV)
  2. carbon of ribose is replaced by sulfur
  3. less potent but LESS TOXIC
  4. competitive inhibition of reverse transcriptase
  5. ACTIVE AGAINST HEPATITIS B (flare ups if stop drug)
  6. resistance is rapidly developed (avoid monotherapy)
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14
Q

Epivir

A

Lamivudine

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15
Q

Epzicom

A

Abacavir + Lamivudine

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16
Q

Abacavir

A
  1. NRTI (tx HIV)

2. SE: SEVERE HSN RXN (rash, fever, malaise) + Resp and GI sx

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17
Q

Ziagen

A

Abacavir

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18
Q

Emtricitabine

A
  1. NRTI (tx HIV)
  2. derivative of Lamivudine
  3. BEST TOLERATED NRTI)
  4. SE: hyperpigmentation of palms and soles
  5. active against HEPATITIS B (can cause flare ups with drug withdrawl)
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19
Q

Emtriva

A

Emtricitabine

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20
Q

Truvada

A

fixed dose Emtricitabine + tenofovir

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21
Q

Atripla

A

efavirenz + tenofovir + emtricitabine

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22
Q

Tenofovir disoproxil

A
  1. NTRI (nucleotide)
  2. pro-drug of tenofovir
  3. effective against resistant HIV strains
  4. active against HEPATITIS B (flare up if discontinued)
  5. SE: N/V/D, renal tox
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23
Q

Nucleotides

A

phosphorylated nucleosides

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24
Q

Viread

A

tenofovir disoproxil

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25
Q

SIDE EFFECT OF ALL NNRTI’s

A

severe rash. metabolized by hepatic p450 enzymes

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26
Q

Nevirapine

A
  1. NNRTI (tx HIV)
  2. dipyridodiazepinone class
  3. binds directly to reverse transcriptase. blocks polymerase activity. disrupts enzyme’s catalytic site
  4. bound to plasma proteins, is a CSF concentration
  5. metabolized by cytochrome p450
  6. use in COMBO to prevent resistance
  7. SE: hepatotoxicity/failure/death (especially with underlying hepatitis or elevated transaminases), F/N/HA, early rash–>SJS
  8. use in combo with zidovudine/didanosine (nucleoside analogues)
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27
Q

Efavirenz

A
  1. NNRTI (tx HIV)
  2. long half-life. once daily dosing
  3. cytochrome p450
  4. plasma protein bound
  5. SE: Dizziness, HA, insomnia, rash
  6. CONSIDER: neural tube defects during first trimester of pregnancy
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28
Q

sustiva

A

efavirenz

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29
Q

protease inhibitor fxn

A
  1. prevent cleavage of protein precursors into individual functional proteins (required for maturation, infection and replication)
  2. inhibitors and metabolized by p45
  3. drug interactions are common
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30
Q

Ritonavir

A
  1. PI (tx HIV)
  2. enzyme then incapable of processing gal-pol polyprotein precursor. cannot infect.
  3. incomplete absorption and first pass-metabolism (by P450)
  4. highly bound to plasma proteins
  5. SE: N/V/D, CIRCUMORAL and PERIPHERAL PARESTHESIA, elevated liver enzymes
  6. used in combo with nucleoside analogues
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31
Q

Indinavir

A
  1. PI (tx HIV)
  2. binds to protease active site and inhibits enzyme
  3. incomplete absorption, first pass metabolism (p450)
  4. bound to plasma proteins (less than ritonavir)
  5. SE: NEPHROLITHIASIS (must drink lots of h20) hyperbilirubinemia, HA, vision change, dizziness, DERM CHANGES (alopecia, dry skin/mm)
  6. used in combo with nucleoside analogs
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32
Q

Indinavir + Ritonavir

A

cross resistance

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33
Q

Nelfinavir

A
  1. PI (tx HIV)
  2. highly plasma protein bound
  3. metabolism by p450
  4. SE: N/D
  5. MOST COMMONLY USED PROTEASE INHBITOR. GENERALLY TOLERATED
  6. used in combo with nucleoside analogs
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34
Q

Treatment Naive patients-HIV

A
  1. must have at lease three active antiretroviral meds that belong to different classes
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35
Q

Antiretroviral tx BACKBONE

A

2 nucleoside reverse transcriptase inhibitors (NRTIs)

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36
Q

Antiretroviral tx BASE

A

non-nucleoside reverse transcriptase inhibitor (NNRTI) OR protease inhibitor

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37
Q

NNRTI-based HIV treatment

A

1 NNRTI + 2 NRTIs

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38
Q

PI-based HIV treatment

A

1 or 2 PIs + 2 NRTIs

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39
Q

P. falciparum

A

malignant tartian malaria. most lethal. q3d.

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40
Q

P. vivax

A

benign tertian malaria. most common form. q3d. SECONDARY TISSUE FORMS

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41
Q

P. malariae

A

quartan malaria. q4d.

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42
Q

P. ovale

A

SECONDARY TISSUE FORMS

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43
Q

infectious form of malaria

A

sporozoite

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44
Q

malarial form that invades RBC

A

merozoite

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45
Q

Blood Schizonticides

A

“clinical cure”. suppress symptoms and do not affect secondary tissue forms

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46
Q

Tissue Shizonticides

A

do not suppress symptoms. know out secondary tissue forms of P. vivax and P. ovale. prevent relapse. higher toxicity

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47
Q

Clinical cure

A

erythrocytic forms of parasite have been eradicated. no symptoms.

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48
Q

Radical Cure

A

all forms of parasite have been eradicated

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49
Q

Gametocytocidal agents

A

act on gametocytes. slow the spread of the disease.

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50
Q

Causal prophylaxis

A

prevent initial development of primary hepatic forms. Primiquine, pyrimethamine and proguanil may have some activity.

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51
Q

Suppressive Agents

A

MOST COMMON PROPHYLACTIC AGENT. do not affect secondary tissue forms. do not prevent relapses.

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52
Q

Chloroquine

A
  1. Antimalarial
  2. acts on erythrocytic forms
  3. interferes with parasite’s feeding mechanisms.
  4. drug concentrates in and raises pH in parasite’s food vacuoles
  5. SUPPRESSIVE AGENT. leads to clinical cure. RADICAL CURE FOR FALCIP AND MALARIAE
  6. RESISTANCE: transport pump removes drug from parasite
  7. Accumulates in melanin-rich tissues-the skin and retina, concentrated in parasitized erythrocytes
  8. taken once weekly for prophylaxis
  9. TOXICITY: less than quinine.
  10. SE: GI, CNS, RETINAL AND CORNEAL TOX (must monitor visual fxn), LUPUS-LIKE
  11. CONTRAINDICATIONS: Pts with psoriasis and porphyria, liver disease pts.
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53
Q

hydroxychloroquine

A
  1. Antimalarial
  2. acts on erythrocytic forms
  3. interferes with parasite’s feeding mechanisms.
  4. drug concentrates in and raises pH in parasite’s food vacuoles
  5. SUPPRESSIVE AGENT. leads to clinical cure. RADICAL CURE FOR FALCIP AND MALARIAE
  6. RESISTANCE: transport pump removes drug from parasite
  7. Accumulates in melanin-rich tissues-the skin and retina, concentrated in parasitized erythrocytes
  8. taken once weekly for prophylaxis
  9. TOXICITY: less than quinine.
  10. SE: GI, CNS, RETINAL AND CORNEAL TOX (must monitor visual fxn), LUPUS-LIKE
  11. CONTRAINDICATIONS: Pts with psoriasis and porphyria, liver disease pts.
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54
Q

used to treat rheumatoid arthritis and lupus erythematosus

A

Hydroxychloroquine-anti-inflammatory at high doses

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55
Q

Quinine/Quinidine gluconate

A
  1. Antimalarial
  2. found in cinchona bark
  3. acts on erythrocytic forms
  4. GAMETOCYTOCIDAL (vivax and malariae)
  5. interference with plasmodial digestion of hemoglobin
  6. USED TO TREAT CHLOROQUINE RESISTANT FALCIPARUM
  7. SE: GI, N/V, tinnitus, deafness, CV: depressant on heart, birth defects, abortion
  8. CINCHONISM: quinine toxicity that resembles salicylism (HA, VISION, TINNITUS)
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56
Q

Chloroquine resistant P. Falciparum treatment

A

Quinine/Quinidine gluconate, mefloquine, pyrimethamine, proguanil

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57
Q

Drug that has analgesia and antipyretic actions like aspirin

A

quinine/quinidine gluconate

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58
Q

Drug used for nocturnal leg cramps

A

quinine/quinidine gluconate

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59
Q

Mefloquine

A
  1. antimalarial
  2. effective against chloroquine resistant falcip
  3. acts on erythrocytic forms of parasite (schizonticidal)
  4. “irritating properties” - can only be used orally
  5. less toxic than chloroquine. SE: GI upset and depression of myocardium.
  6. BUT: SEIZURES AND AGGRAVATION OF LATENT PSYCHOSES TOO.
  7. CONTRAINDICATIONS: CV disorders, Psychiatric problems, epilepsy.
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60
Q

Sulfonamides

A
  1. antimalarial.
  2. inhibit the incorporation of PABA into folic acid
  3. Sulfadoxine
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61
Q

Dihydrofolate reductase inhibitors

A
  1. antimalarial
  2. block conversion of dihydrofolic acid to tetrahydrofolic acid
  3. Pyrimethamine, proguanil
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62
Q

Pyrimethamine and Proguanil

A
  1. antimalarial
  2. inhibits dihydrofolate reductase. main effect on erythrocytic forms.
  3. Prophylatic use. chloroquine resistant falcip
  4. PROGUANIL HAS CAUSAL PROPHYLACTIC ACTIVITY
  5. Proguanil is relatively nontoxic. PyrMethamine: rash, bone marrow suppression
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63
Q

Pyrimethamine plus sulfadoxine

A
  1. used for presumptive treatment of malaria
  2. can be used in conjunction with artemisinin analogs for treatment of chloroquine resistant falcip
  3. Allergic rxn to sulfonamides
  4. Dihydrofolate and PABA block
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64
Q

Atovaquone plus proguanil

A
  1. newer antimalarial
  2. atovaquone: acts by depolarizing the parasite’s mitochondria and inhibiting electron transport
    (proguanil=dihydrofolate reductase inhibitor)
  3. SE: HA/Abdominal pain
  4. alternative to mefloquine or doxycycline for prophylaxis against chloroquine resistant falcip
  5. daily dosage
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65
Q

halofantrine

A
  1. new antimalarial

2. SE: GI

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66
Q

artemisinin

A
  1. Chinese herbal preparation

2. antimalarial

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67
Q

tetrandine

A
  1. antimalarial

2. against chloroquine resistant falcip

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68
Q

tetracycline ab (doxy)

A
  1. antimalarial activity
  2. used as alternate or adjunctive and prophylaxis
  3. Inhibition of protein synthesis
  4. Phototox, discoloration of teeth in children
  5. Contraindicated in children under 8 and pregnancy
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69
Q

Primaquine

A
  1. antimalarial
  2. Tissue schizonticide
  3. active against tissue forms of all species, gametocytocidal too
  4. little effect on erythrocytic forms (will not suppress disease after development)
  5. CAN PRODUCE A RADICAL CURE (in vivax and ovale)
  6. can also prevent initial development (causal) but is not used as prophylaxis due to toxicity
  7. SE: GI, CNS, HEMOLYTIC ANEMIA (in G6P Hydrogenase def.–>asians, afs, meds)
  8. TERATOGEN
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70
Q

Coartem

A

(artemether) artemisinin derivative in combo with lumafantrine (similar to halofantrine)
- VERY POPULAR TREATMENT FOR MOST FORMS Of MALARIA
- Given IM for lifethreatening falcip
- given in combo

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71
Q

treatment of pneumocystosis

A

primaquine plus clindamycin

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72
Q

G6P Hydrogenase deficiency

A
  1. resistance to malaria

2. asians, afs, meds

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73
Q

Order of useage for acute uncomplicated attack

A
  1. chloroquine (most sensitive forms)
  2. artemether/lumefantrine (all forms)
  3. quinine/quinidine gluconate (c resistant falcip)
  4. mefloquine (multidrug resistant falcip)
  5. atovaquone + proguanil (
  6. doxy (adjunct)
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74
Q

PREVENTION OF RELAPSE

A

primaquine

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75
Q

prophylaxis

A
  1. chloroquine
  2. atovaquone + proguanil
  3. doxy
  4. mefloquine
  5. proguanil/chlorquanide
  6. pyrimethanime + sulfadoxine–>presumptive tx
  7. primaquine–>flollow up tx
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76
Q

Mechlorethamine

A
  1. chemotherapeutic CCNS
  2. Alkylating agent. DNA damaging drug
  3. Nitrogen mustard
  4. TX: Hodgkin’s disease
  5. MOA: intramolecular cyclization to form ethyleneimonium ion–>directly or thru carbonic ion transfers alkyl group to cell
  6. Major site of alkylation in DNA is N7 (Guanine)
  7. Alkylation leads to: miscoidng of DNA, incomplete repair of segment, excessive crosslinking of DNA.
  8. Most susceptible to alkylation in LATE G1 AND S PHASES (but are not cell cycle specific)
  9. TOX: Vesicant at site of injection, bone marrow, spermatogenesis, GIT, hair follicles
  10. ACUTE: emesis, phlebitis. DELAYED: thrombocytopenia, immunosupression, secondary neoplasia
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77
Q

Cyclophosphamide

A
  1. chemotherapeutic CCNS
  2. alkylating agent. DNA damaging drug
  3. Nitrogen mustard
  4. derivative of mechlorethamine
  5. Requires metabolic activation by CYP450
  6. TX: leukemias, sex organ cancers, IMMUNOSUPPRESSIVE (organ transplant, wegener’s granuomatosis, RA)
  7. MOA: intramolecular cyclization to form ethyleneimonium ion–>directly or thru carbonic ion transfers alkyl group to cell
  8. Major site of alkylation in DNA is N7 (Guanine)
  9. Alkylation leads to: miscoidng of DNA, incomplete repair of segment, excessive crosslinking of DNA.
  10. Most susceptible to alkylation in LATE G1 AND S PHASES (but are not cell cycle specific)
  11. TOX: Vesicant at site of injection, bone marrow, spermatogenesis, GIT, hair follicles
  12. ACUTE: emesis, phlebitis. DELAYED: thrombocytopenia, immunosupression, secondary neoplasia
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78
Q

Carmustine

A
  1. chemotherapeutic CCNS
  2. nitrosourea
  3. alkylating agent/dna damaging (CCNS)
  4. requires activation
  5. lipid soluble
  6. TX: brain, lymphomas, myeloma
  7. bifunctional alkylator (2 Cl ions cleaved by hydrolysis, 2 sites for binding)
  8. phase nonspecific
  9. TOX: N/V, leukopenia, thrombocytopenia
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79
Q

Cisplatin

A
  1. chemotherapuetic CCNS
  2. platinum complex
  3. alkylating agent/dna damaging (CCNS)
  4. G1 may be most sensitive
  5. TX: sex organ CA, GI, lung, head
  6. bifunctional alkylating agent (2 Cl ions cleaved by hydrolysis, 2 sites for binding)
  7. inter/intrastrand crosslinking
  8. disrupts DNA double helix, interferes with DNA synthesis
  9. TOX: nephro and ototoxicity, bone marrow depression
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80
Q

Methotrexate

A
  1. chemotherapuetic CCS (S)
  2. antimetabolite (CCS/structural analogue)
  3. metabolized instead of normal substrate, incorporated, non-functional
  4. compete with normal metabolite at allosteric site on enzyme
  5. affect nucleotide/nucleic acid synthesis
  6. FOLIC ACID ANALOGUE. inhibitor of dihydrofolate reducatase. bloks conversion of folic acid to tetrahydrofolate. (inability to convert deoxyuridulate to thymidylate. blocks DNA, RNA, protein synth)
  7. poor CNS penetration
  8. highly bound to plasma proteins. displaced by salicylates
  9. can precipitate in renal tubules
  10. RESISTANCE: decreased uptake, increased concentration of target enzyme
  11. TX: leukemia, lymphomas, PSORIASIS, RA
  12. KILLS IN S PHASE
  13. TOX: ASCITES, EDEMA increase tox, N/V/D, GI, Oral ulcers, bone marrow suppresion, hepatotox, PULM INFILATRATES
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81
Q

Leucovirin

A

bypasses metabolic block by methotrexate and protects normal cells

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82
Q

Mercaptopurine

A
  1. chemotherapuetic CCS
  2. antimetabolite (CCS/structural analogue)
  3. metabolized instead of normal substrate, incorporated, non-functional
  4. compete with normal metabolite at allosteric site on enzyme
  5. affect nucleotide/nucleic acid synthesis
  6. PURINE ANALOG (of hypoxanthine)
  7. metabolized by xanthine oxidase–>6 thiouric acid
  8. TX: remission of leukemias
  9. MOA: converted by HGPRT. inhibits enzymes of purine conversion. INHIBIT PURINE NT SYNTH AND METABOLISM
  10. TOX: N/V/D, Bone marrow depression
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83
Q

Fluorouracil

A
  1. chemotherapuetic CCS
  2. antimetabolite cell cycle specific (CCS/structural analogue)
  3. metabolized instead of normal substrate, incorporated, non-functional
  4. compete with normal metabolite at allosteric site on enzyme
  5. affect nucleotide/nucleic acid synthesis
  6. PYRIMIDINE ANALOG
  7. converted to active 5-deoxyuridine
  8. TX: sex organ CA, GI, NECK
  9. 5-deoxyuridine binds to thymidylate synthetase. blocks conversion of deoxyuridylate to thymidylate (rate limiting step in DNA synthesis)
  10. Resistance: decreased activation, increased deactivation
  11. TOX: DONT CAUSE ACUTE TOX, delayed: GI ulceration, bone marrow depression
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84
Q

Cytarabine

A
  1. chemotherapuetic CCS
  2. antimetabolite- cell cycle specific (CCS/structural analogue)
  3. metabolized instead of normal substrate, incorporated, non-functional
  4. compete with normal metabolite at allosteric site on enzyme
  5. affect nucleotide/nucleic acid synthesis
  6. converted to Cytarabine triphosphate.
  7. TX: remission induction for leukemias
  8. inhibits DNA plyerase by competeing with substrate deoxycitidine triphosphate
  9. TOX: bone marrow depression, MEGALOBLASTOSIS, leukopenia, thrombocytopenia
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85
Q

Daunorubicin HCL

A
  1. Chemotherapeutic CCNS
  2. ‘natural product’ AB
  3. TX: acute non lymphocytic leukemia of adults
  4. GREATER ACTIVITY THAN DOXO
  5. intercalate adn bind to dNA between base pairs on adjacent strands…leads to uncoiling of DNA
  6. not CCS, but MAX EFFECT DURING S PHASSE
  7. Resistance: decreased uptake by tumors
  8. activity is dt tetracycline ring.
  9. different from DOXO by single hydroxyl group
  10. TOX: RED URINE, tissue necrosis, arrhytmias, BM depression, CARDIOMYOPATHY
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86
Q

Doxorubicin HCL

A
  1. chemotherapeutic CCNS
  2. ‘natural product’ AB
  3. TX: ADULT AND CHILD leukemias, CA of GU
  4. used in combo. synergy.
  5. intercalate adn bind to dNA between base pairs on adjacent strands…leads to uncoiling of DNA
  6. not CCS, but MAX EFFECT DURING S PHASSE
  7. Resistance: decreased uptake by tumors
  8. activity is dt tetracycline ring.
  9. different from DOXO by single hydroxyl group
  10. TOX: RED URINE, tissue necrosis, arrhytmias, BM depression, CARDIOMYOPATHY
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87
Q

Vinblastine Sulfate

A
  1. chemotherapeutic CCS (M)
  2. vinca alkaloid
  3. methyl group
  4. TX: Hodgkins, Kaposi’s, testicular, lung, bladder
  5. bind tubulin (microtubules) disruption of mitotic spindle. prevents segregation of chromosomes in METAPHASE
  6. TOX: mild N/V, phlebitis, DELAYED: neuro, bone marrow suppression
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88
Q

Vincristine Sulfate

A
  1. chemotherapuetic CCS (M)
  2. vinca alkaloid
  3. methyl group is replaced by formyl group from vinblastine
  4. TX: Breast, acute leukemia, H/N lymphoma
  5. bind tubulin (microtubules) disruption of mitotic spindle. prevents segregation of chromosomes in METAPHASE
  6. ACUTE TOX: local reactivity Delayed: neuro, alopecia
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89
Q

Etoposide

A
  1. chemotherapuetic CCS (G2)
  2. Natural product. epipodophylotoxin
  3. semisynthetic derivative of podophylootoxoin
  4. TX: testicular (plus belomycin and cisplatin), SSC of lung (plus cisplatin)
  5. forms complex with topoisomerase II and DNA. DNA breaks. cell death
  6. TOX: N/V/D with oral more so, leukopenia, alopecia
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90
Q

block action of xanthine oxidase

A

allopurinol

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91
Q

Paclitaxel

A
  1. chemotherapeutic CCS (G2/M)
  2. Natural product, taxene
  3. diterpene extracted from bark of “yew”
  4. TX: metastatic breast. ovarian, non SSC of lung
  5. MOA: antimicrotubule agent. promotes microtubule assembly, enhancing tubular polymerization
  6. TOX: N/V/D, bone marrow suppression, HSN, neuropathy, alopecia (IN ALMOST ALL PTS)
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92
Q

Prednisone

A
  1. chemotherapeutic
  2. hormonal agent
  3. adenocorticosteroid
  4. palliative management of leukemia and lymphoma in adults, acute leukemia of childhood, breast CA
  5. suppress mitosis in lymphocytes and macrophages
  6. binds to cytosolic receptors and affects DNA/RNA/Protein synth
  7. TOX: CUSHING’S SYNDROME, osteoporosis, infections, psych, peptic ulcers, HTN edema
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93
Q

Dexamethasone

A
  1. chemotherapeutic
  2. hormonal agent
  3. adenocorticosteroid
  4. palliative management of leukemia and lymphoma in adults, acute leukemia of childhood, breast CA
  5. suppress mitosis in lymphocytes and macrophages
  6. binds to cytosolic receptors and affects DNA/RNA/Protein synth
  7. TOX: CUSHING’S SYNDROME, osteoporosis, infections, psych, peptic ulcers, HTN edema
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94
Q

Tamoxifen

A
  1. chemotherapeutic CCS? (G1)
  2. nonsteroidal ANTIESTROGEN
  3. absorbed rapidly
  4. once daily administration
  5. extensive metabolism in the liver
  6. TX: estrogen + breast CA. adjuvent tx of breast CA (decreased recurrence and development of new ones). most frequently for breast cancer of MEN
  7. competitive inhibition of estrogen binding to receptors in sensitive tissues. Receptors are nuclear transription factors
  8. inhibits expression of estrogen related genes
  9. BLOCKS G1 PHASE OF CELL CYCLE
  10. works like estrogen in other tissues. decreased cholesterol, slows bone loss
  11. TOX: menopausal sx. ht flashes, HA, fatigue, vaginal dryness, visual disturbance, ocular tox THROMBOEMBOLIC EVENTS. POTENTIAL TUMOR PROMOTING ACTIVITY.
  12. increased incidence of endometrial CA
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95
Q

Imatinib Mesylate

A
  1. chemotherapeutic
  2. tyrosine kinase inhibitor
  3. well absorbed orally
  4. highly protein bound
  5. CYP3A4
  6. TX: leukemia, philadelphia chromosome + leukemia, GI stromal + cKit
  7. dermatofibrosarcoma, HYPEREOSINOPHILIC SYNDROME
  8. inhibits Bcr-Abl tyrosine kinase. prevents phosphorylation of kinase substrate by ATP
  9. induces apoptosis in bcr-abl leukemia in cell lines derived from pts with CML in blast crisis
  10. TOX: abdominal pain, N/V/D, fatigue, joint pain, muscle cramps, fluid retention, rash
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96
Q

Trastuzumab

A
  1. chemotherapeutic (CCS? G1)
  2. HUMANIZED IgG1 MoAB
  3. IV
  4. TX: EGR2 overexpressing CA (breast cancer) in combo with doxorubicin, cyclophosphamide, paclitaxel. Metastatic Breast CA: in combo with paclitaxel for 1st line of HER2-overexpressing
  5. MOA: binds to HUMAN EPDIERMAL GROWTH FACTER RECEPTOR (HER2). blocks binding. downregulates tyrosine kinase signaling activity.
  6. G1 CELL CYCLE ARREST
  7. TOX: N/V/D, anemia, neutropenia, infections, CARDIOMYOPATHY, INFUSION RXNS
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97
Q

Bcr-Abl fusion protein

A

constitutive abnormal tyrosine kinase created by t(9:22) philadelphia chromosomal translocation in CML

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98
Q

Chlorpromazine

A
  1. Antipsychotic
  2. phenothiazine
  3. first modern antipsychotic
    - -
  4. greater effect on positive sx
  5. neuroleptic effect
  6. effects slow over 2-4 w
  7. tolerance not an issue
  8. issue with compliance. effects seem unpleasant
  9. lowered seizure threshold
  10. ENTIEMETIC: desnsitization of CRTZ
  11. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
  12. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
  13. ANTIHISTAMINIC
  14. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
  15. Inhibition of ejaculation
  16. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)–>gynecomastia, lactation, menstrual problems
  17. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
  18. AFFECTS SIMILAR TO T2DM
  19. inhibition of Ca calmodulin-dependent processes
  20. Teratogenesis
  21. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
  22. drugs can interact with other receptors too. like muscarinic. serotonergic…Blocking 5HT2 effective against negative sx of schizo
  23. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
  24. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
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99
Q

Fluphenazine

A
  1. Antipsychotic
  2. phenothiazine
  3. piperazine phenothiazine (SIMILAR TO TRIFLUOPERAZINE)
  4. long acting can be given depot injection q3-4w
    - -
  5. greater effect on positive sx
  6. neuroleptic effect
  7. effects slow over 2-4 w
  8. tolerance not an issue
  9. issue with compliance. effects seem unpleasant
  10. lowered seizure threshold
  11. ENTIEMETIC: desnsitization of CRTZ
  12. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
  13. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
  14. ANTIHISTAMINIC
  15. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
  16. Inhibition of ejaculation
  17. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)–>gynecomastia, lactation, menstrual problems
  18. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
  19. AFFECTS SIMILAR TO T2DM
  20. inhibition of Ca calmodulin-dependent processes
  21. Teratogenesis
  22. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
  23. drugs can interact with other receptors too. like muscarinic. serotonergic…Blocking 5HT2 effective against negative sx of schizo
  24. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
  25. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
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100
Q

Prochlorperazine

A
  1. Antipsychotic
  2. phenothiazine
  3. aliphatic phenothiazine (SIMILAR TO TRIFLUOPERAZINE)
  4. COMMONLY USED AS ANTIEMETIC
    - -
  5. greater effect on positive sx
  6. neuroleptic effect
  7. effects slow over 2-4 w
  8. tolerance not an issue
  9. issue with compliance. effects seem unpleasant
  10. lowered seizure threshold
  11. ENTIEMETIC: desnsitization of CRTZ
  12. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
  13. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
  14. ANTIHISTAMINIC
  15. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
  16. Inhibition of ejaculation
  17. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)–>gynecomastia, lactation, menstrual problems
  18. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
  19. AFFECTS SIMILAR TO T2DM
  20. inhibition of Ca calmodulin-dependent processes
  21. Teratogenesis
  22. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
  23. drugs can interact with other receptors too. like muscarinic. serotonergic…Blocking 5HT2 effective against negative sx of schizo
  24. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
  25. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
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101
Q

Trifluoperazine

A
  1. Antipsychotic
  2. phenothiazine
  3. piperazine phenothiazine
  4. MORE POTENT THAN CHLORPROMAZINE. less sedation, less anti-Ach activity, more pyramidal motor problems
    - -
  5. greater effect on positive sx
  6. neuroleptic effect
  7. effects slow over 2-4 w
  8. tolerance not an issue
  9. issue with compliance. effects seem unpleasant
  10. lowered seizure threshold
  11. ENTIEMETIC: desnsitization of CRTZ
  12. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
  13. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
  14. ANTIHISTAMINIC
  15. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
  16. Inhibition of ejaculation
  17. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)–>gynecomastia, lactation, menstrual problems
  18. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
  19. AFFECTS SIMILAR TO T2DM
  20. inhibition of Ca calmodulin-dependent processes
  21. Teratogenesis
  22. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocortical,tuberoinfundibular..D2??)
  23. drugs can interact with other receptors too. like muscarinic. serotonergic…Blocking 5HT2 effective against negative sx of schizo
  24. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
  25. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
102
Q

Schizophrenia

A

excess DA activity in frontal cortex/limbic system

103
Q

Traditional antipsychs act on what receptor

104
Q

Clozapine receptor antagonism

A

D4, 5Ht2. thus doesn’t produce extrapyramidal effects

105
Q

5HT2 blockers

A

effective against negative sx of schizo

106
Q

drug to treat dystonia, akathisia, parkinsonism

A

anticholinergics

107
Q

Neuroleptic malignant syndrome tx

A

dantrolene (inhibits CA release), Bromocryptine (DA antagonist)

108
Q

Tardive dyskinesia

A
  1. long term therapy sx
  2. appears upon removal of med
    3 anticholinergics make worse. suppressed w. more drug
  3. no adequate treatment
109
Q

Haloperidol

A
  1. antipsychotic
  2. nonphenothiazine
  3. LESS ANTICHOLINERGIC ACTIVITY THAN CHLORPROMAZINE
  4. more extrapyramidal effects
  5. less sedation. available in long acting form
    - -
  6. greater effect on positive sx
  7. neuroleptic effect
  8. effects slow over 2-4 w
  9. tolerance not an issue
  10. issue with compliance. effects seem unpleasant
  11. lowered seizure threshold
  12. ENTIEMETIC: desnsitization of CRTZ
  13. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
  14. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
  15. ANTIHISTAMINIC
  16. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
  17. Inhibition of ejaculation
  18. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)–>gynecomastia, lactation, menstrual problems
  19. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
  20. AFFECTS SIMILAR TO T2DM
  21. inhibition of Ca calmodulin-dependent processes
  22. Teratogenesis
  23. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
  24. drugs can interact with other receptors too. like muscarinic. serotonergic…Blocking 5HT2 effective against negative sx of schizo
  25. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
  26. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
110
Q

Clozapine

A
  1. antipsych
  2. 2nd generation “atypical antipsych”
  3. useful in pts who don’t respond to toher drugs
  4. effective against NEGATIVE SYMPTOMS
  5. MOST EFFICACIOUS ANTIPSYCHOTIC
  6. APPROVED FOR SUICIDAL BEHAVIOR
  7. preferentially blocks MESOLIMBIC DA RECEPTORS (D4) not striatum or tubuloinfundibulum. also blocks 5HT2
  8. STRONG ANTICHOLINGERGIC ACTIVITY
  9. TOX: few extrapyramidal effects. granulocytopenia, agranulocytosis, seizure, weight gain, hyperglycemia T2DM, myocarditis
  10. potetnial cytotoxicity: 2nd line drug
  11. EXPENSIVE
111
Q

Olanzapine

A
  1. antipsych
  2. 2nd generation “atypical antipsych”
  3. tx of schizo and mania
  4. preferentially blocks MESOLIMBIC DA RECEPTORS (D4) not striatum or tubuloinfundibulum. also blocks 5HT2
  5. STRONG ANTICHOLINGERGIC ACTIVITY
  6. DOES NOT CAUSE BONE MARROW TOX
  7. WEIGHT GAIN and HYPERGLYCEMIA
  8. MORE CHANCE OF EXTRAPYRAMIDAL SE. less than other drugs though. safer than clozapine otherwise
112
Q

Risperdone

A
  1. antipsych
  2. 2nd generation “atypical antipsych”
  3. ONE OF MOST WIDELY USED ANTIPSYCHS
  4. depot form q2-4w
  5. Blocks D2 and 5HT1a receptors
  6. less chance for ESP than older drugs. MORE THAN CLOZAPINE/OLANZAPINE
  7. SE: weight gain/hyperglycemia
113
Q

Aripiprazole

A
  1. antipsych
  2. 2nd generation “atypical antipsych”
  3. effective against positive and negative sx. AND FOR MANIA
  4. less efficacious than claz, olaza, resperd
  5. PARTIAL AGONIST/ANTAGONIST at D2 and 5HT1a receptors
  6. little tendency for EPS, less chance of weight gain or hyperglycemia
114
Q

Quetiapine

A
  1. antipsych
  2. 2nd generation “atypical antipsych”
  3. EFFECTIVE AGAINST POS AND NEG SX
  4. less efficacious than cloza, olaza, resperd
  5. preferentially blocks MESOLIMBIC DA RECEPTORS (D4) not striatum or tubuloinfundibulum. also blocks 5HT2
  6. STRONG ANTICHOLINGERGIC ACTIVITY
  7. low chance for EPS. no agranuloctosis
  8. EXPENSIVE
115
Q

Ziprasidone

A
  1. antipsych
  2. 2nd generation “atypical antipsych”
  3. EFFECTIVE AGAINST POS AND NEG SX
  4. less efficacious than cloza, olaza, resperd
  5. preferentially blocks MESOLIMBIC DA RECEPTORS (D4) not striatum or tubuloinfundibulum. also blocks 5HT2
  6. STRONG ANTICHOLINGERGIC ACTIVITY
  7. low chance for EPS. no agranuloctosis
  8. EXPENSIVE
  9. FEWER METABOLIC COMPLICATIONS THAN CLOZA, OLAZA, RISPERD
116
Q

DOC for Depression

A

SSRIs and 2nd gen antidepressants

117
Q

2nd-3rd line for depression

A

Tricyclics and MAO-Is due to toxicity

118
Q

Anxiolytics that have antidepressant asctivity

A

alprazolam/xanax

119
Q

antidepressants with bipolar

A

may cause switch to mania

120
Q

monoamine theory of depression

A

caused by deficit of monoamine NT (NE 5HT) in brain

121
Q

tricyclics

A

block reuptake of NE and 5HT to a lesser extent

122
Q

tertiary amines

A

have greater 5HT tahn seondary

123
Q

SSRIs

A

inhibit 5HT reuptake

124
Q

Bupoprion

A

selectively inhibits DA reuptake

125
Q

Venlafaxine

A

inhibits both NE and 5HT

126
Q

Trazodone and nefazodone

A

inhibit 5HT reuptake and block 5HT2

127
Q

Antidepressent with worst anticholinergic SE

A

amitriptyline

128
Q

Antidepressant with least anticholinergic SE

129
Q

decreases cardiotoxic effects of tricyclics

A

sodium bicarb

130
Q

what is not recommended in TCA overdose

A

physostigmine

131
Q

serotonin syndrome

A

MAO inhibitors-tremors, HTN, hyperpyrexia, seizures

132
Q

hormone involved in platelet aggregation and blood clotting

133
Q

treatment of enuresis and urinary incontinence

A

imipramine

134
Q

treatment of pain from neuropathies

A

tricyclics, dulozetine

135
Q

withdrawl symptoms of antidepressants

A

lethargy, chills, neuro disturbances, muscle aches

136
Q

Imipramine

A
  1. Tricyclic antidepressant (serotonin/NE reuptake inhibitor)
  2. prototype
  3. change in density of neurotransmitter receptors with chronic treatment
137
Q

amitriptyline

A
  1. tricyclic antidepressant (serotonin/ NE reuptake inhibitor)
  2. more sedation and anticholinergic activity than imipramine
  3. change in density of neurotransmitter receptors with chronic treatment
138
Q

guanethidine

A
  1. antihypertensive. reduce release of catecholamines

2. antidepressants decrease effect by blocking uptake by nerve endings

139
Q

SE of antidepressants

A

CNS: tremor anxiety, irritability, parkinsonism, increased risk of seizures
CV: postural hypotension (alpha block), flattening/iversion of T waves, arrhythmias
Random: weight gain (tricyclics), delay of orgasm (alpha block) retrograde ejac, blood dyscrasia

140
Q

Fluoxetine

A
  1. SSRI antidepressant
  2. prototype
  3. effective as antidepressant AND TX OCD, anxiety, MPDD
  4. also for things involving 5HT. bulimia, anorexia, eating disorders
  5. selective serotonin reuptake inhibitor
  6. requires 4-5 weeks of tx to reach steady state. same thing for it to be cleared
  7. much less sedation, anticholinergic, and CV effects as tricyclics
  8. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
  9. association with suicidal behavior
141
Q

Fluvoxamine

A
  1. SSRI antidepressant
  2. OCD in US. Depression in foreign countries
  3. selective inhibitor of 5HT reuptake, SIMILAR TO FLUOXETINE
  4. much less sedation, anticholinergic, and CV effects as tricyclics
  5. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
  6. association with suicidal behavior
142
Q

Sertraline

A
  1. SSRI antidepressant
  2. selective inhibitor of 5HT reuptake, RESEMBLES FLUOXETINE IN SE AND EFFECTS
  3. much less sedation, anticholinergic, and CV effects as tricyclics
  4. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
  5. association with suicidal behavior
  6. Slow elimination. LONGER IN OLDER PATIENTS
  7. several active metabolites
  8. LESS POTENTIAL FOR DRUG INTERACTIONS THAN FLUOXETINE
143
Q

Paroxetine

A
  1. SSRI antidepressant
  2. selective inhibitor of 5HT reuptake, resemble luoxetine
    much less sedation, anticholinergic, and CV effects as tricyclics
  3. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
  4. association with suicidal behavior
  5. DIFFERS FROM FLUOXETINE AND SERTRALINE BC IT IS MORE RAPIDLY METABOLISED. DOES NOT FORM ACTIVE METABOLITES
  6. can interact with many other drugs
  7. more WEIGHT GAIN than other SSRIs
144
Q

Citalopram

A

“LIKE SERTRALINE”…Newest SSRI

  1. SSRI antidepressant
  2. selective inhibitor of 5HT reuptake, RESEMBLES FLUOXETINE IN SE AND EFFECTS
  3. much less sedation, anticholinergic, and CV effects as tricyclics
  4. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
  5. association with suicidal behavior
  6. Slow elimination. LONGER IN OLDER PATIENTS
  7. several active metabolites
  8. LESS POTENTIAL FOR DRUG INTERACTIONS THAN FLUOXETINE
145
Q

Escitalopram

A

“LIKE SERTRALINE”..ISOMER OF CITALOPRAM

  1. SSRI antidepressant
  2. selective inhibitor of 5HT reuptake, RESEMBLES FLUOXETINE IN SE AND EFFECTS
  3. much less sedation, anticholinergic, and CV effects as tricyclics
  4. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
  5. association with suicidal behavior
  6. Slow elimination. LONGER IN OLDER PATIENTS
  7. several active metabolites
  8. LESS POTENTIAL FOR DRUG INTERACTIONS THAN FLUOXETINE
146
Q

Venlafixine

A
  1. Serotonin-Norepinephrine Reuptake inhibitor
  2. TX: depression, recently approved for anxiety
  3. mild “stimulant” energizes depressed ppl
  4. may work in ppl that SSRIs dont work in
    PERHAPS ADD in children
  5. also inhibits DA reuptake
  6. may have more rapid onset of action (1-2w) than others antidepressants
  7. SE: FEWER CV than tricyclics. does cause HTN and tachycardia. nausea, nervousness, anxiety, sweating, palpitations, sexual dysfunction
147
Q

Desvenlafixine

A
  1. Serotonin-Norepinephrine Reuptake inhibitor
  2. TX: depression, recently approved for anxiety
  3. mild “stimulant” energizes depressed ppl
  4. may work in ppl that SSRIs dont work in
  5. also inhibits DA reuptake
  6. may have more rapid onset of action (1-2w) than others antidepressants
  7. SE: FEWER CV than tricyclics. does cause HTN and tachycardia. nausea, nervousness, anxiety, sweating, palpitations, sexual dysfunction
148
Q

Duloxetine

A

APPROVED FOR NEUROPATHIC PAIN AND PSYCHOTHERAPEUTIC USES
“similar to venlafaxine”…
1. Serotonin-Norepinephrine Reuptake inhibitor
2. TX: depression, recently approved for anxiety
3. mild “stimulant” energizes depressed ppl
4. may work in ppl that SSRIs dont work in

  1. also inhibits DA reuptake
  2. may have more rapid onset of action (1-2w) than others antidepressants
  3. SE: FEWER CV than tricyclics. does cause HTN and tachycardia. nausea, nervousness, anxiety, sweating, palpitations, sexual dysfunction
149
Q

Trazadone

A
  1. 2nd gen antidepressant
  2. SEDATION can be beneficial at night for depressed patients
  3. inhibits reuptake of 5HT and blocks 5HT2 receptors
  4. lower incidence of anticholinergic and CV side effects than tricyclics
  5. CAN CAUSE PRIAPISM (penis stays erect) and other sexual dysfunctions in males.
  6. Very sedating
150
Q

Nefazodone

A
  1. 2nd gen antidepressant
  2. SEDATION can be beneficial at night for depressed patients
  3. inhibits reuptake of 5HT and blocks 5HT2 receptors
  4. lower incidence of anticholinergic and CV side effects than tricyclics
  5. CAN CAUSE PRIAPISM (penis stays erect) and other sexual dysfunctions in males.
  6. Very sedating
151
Q

Bupropion

A
  1. 2nd gen antidepressant
  2. mild stimulant activity, “psychic energizer”
  3. tx nicotine, cocaine, and amphetamine dependence
  4. selectively blocks reuptake of DA
  5. MORE LIKELY THAN OTHER ANTIDEPRESSANTS TO CAUSE SEIZURES
152
Q

Mirtazepine

A
  1. 2nd gen antidepressant
  2. chemically different than tricyclics and SSRIs
  3. Antidepressant and anxiolytic activity
  4. good in depressed patients with anxiety
  5. MOA: blocks presynaptic a2 adrenergic receptors. increases NE/5HT (blocks some 5HT receptors)
  6. Similar SE to tricyclics (anticholinergic, hypotension, tachy)
153
Q

Atomexitine

A
  1. selective norepinephrine reuptake inhibitor
  2. APPROVED TO TX ADHD in kids and adults
  3. qualitatively different than stimulant drugs
  4. selective NE reuptake inhibitor
  5. SE: suppression of appetite, DECREASED weight gain, INCREASED BP, tachy, sexual dysfunction in males
154
Q

Phenelzine

A
  1. MAO inhibitor
  2. increased synaptic levels of NE, 5HT, DA (chronically, decreased sensitivity of receptors)
  3. antidepressant action takes several weeks to develop
  4. normalization of sleep paterns
  5. CNS stimulation in some patients (tremors, insomnia, hallucinations)
  6. can cause switch to manic phase in bipolar
  7. TX: depression in pts who dont respond to other drugs, bulimia, OCD, PTSD, narcolepsy
  8. INHIBITS MAO-A/B
  9. when drug is stopped, several weeks to enzyme activity to return to normal
  10. SE: orthostatic hypotension, HTN, GI, HA, dizziness, CNS, Liver damage, allergic rxns
    potentiation of sympathomimetic agents
    -TYRAMINE: CHEESE TOXICITY-present in certain foods and stimulates release of catecholamines. leads to severe HTN, fever, convulsions
    -Tricyclics and antidepressants: fever, convusions, death (3-4w post MAO-I to tricyclic)
    -slowed metabolism
    CONTAINS A HYDRIAZIDE GROUP THAT CAN FORM COVALENT BONDS WITH MAO–>IRREVERSIBLE INACTIVATION OF MAO
155
Q

Tranylcypromine

A
  1. MAO inhibitor
  2. increased synaptic levels of NE, 5HT, DA acutely (chronically, decreased sensitivity of receptors)
  3. antidepressant action takes several weeks to develop
  4. normalization of sleep paterns
  5. CNS stimulation in some patients (tremors, insomnia, hallucinations)
  6. can cause switch to manic phase in bipolar
  7. TX: depression in pts who dont respond to other drugs, bulimia, OCD, PTSD, narcolepsy
  8. INHIBITS MAO-A/B
  9. when drug is stopped, several weeks to enzyme activity to return to normal
  10. SE: orthostatic hypotension, HTN, GI, HA, dizziness, CNS, Liver damage, allergic rxns
    potentiation of sympathomimetic agents
    -TYRAMINE: CHEESE TOXICITY-present in certain foods and stimulates release of catecholamines. leads to severe HTN, fever, convulsions
    -Tricyclics and antidepressants: fever, convusions, death (3-4w post MAO-I to tricyclic)
    -slowed metabolism
    DOES NOT FORM COVALENT BOND WITH MAO. binds very tightly.
156
Q

Selegiline

A
  1. MAO inhibitor
  2. increased synaptic levels of NE, 5HT, DA acutely (chronically, decreased sensitivity of receptors)
  3. TX: parkinsons disease, TRANSDERMAL PATCH FOR TX OF DEPRESSION
  4. selective MAO-B inhibitor
  5. decreased food/drug effects when used at recommended dose
157
Q

action of MAO-A

A

metabolizes NE and 5HT

158
Q

action of MAO-B

A

metabolizes DA

159
Q

Lithium Carbonate

A
  1. mood stabilizer
  2. MOST EFFECTIVE DRUG FOR manic-depressive disorders
  3. most effective during manic phase
  4. little CNS effect
  5. MOA: ionic theory: may alter neuronal distribution of Na/K/Ca in CNS. biogenic amine theory: may delay release/reuptake of NT amine. phospholipid theory: alter metabolism of phospholipids that are involved in signaling pathway.
  6. gradual accumulation in tissues
  7. enhanced reabsorption in Na-depleted patients
  8. careful with renal function! problems can change excretion of lithium
  9. 4-5 d to reach steady state
  10. SE: LOW THERAPEUTIC INDEX!! carefully monitor in serum–>looks like alcohol tox
  11. acute intoxication: N/V/D, fatigue, weakness, tremor, blurred vision, tinnitus, slurred speach, arrhythmias
  12. TX of intoxication: remove drug, supportive (fluids, other drugs), diuresis, hemodialysis
  13. other toxicity: hypothyroid, polydipsia, uria, kidney damage, weight gain, skin stuff, teratogen
  14. drug interactions: NSAIDS interfere with excretion, carbamazepine, antidepressants enhance neurotox, Li can enhance effects of other CNS drugs
160
Q

Valproic acid analog

A
  1. mood stabilizers.
  2. anti-epileptic
  3. tx manic depressive disorders (bipolar)
161
Q

carbamazepine

A
  1. mood stabilizers.
  2. anti-epileptic
  3. tx manic depressive disorders (bipolar)
162
Q

clonazepam

A
  1. mood stabilizers.
  2. anti-epileptic
  3. tx manic depressive disorders (bipolar)
163
Q

depakene

A

valproic acid analog

164
Q

depakote

A

valproic acid analog

165
Q

most common helminth infection in US

A

pinworm-nematode

166
Q

symptoms of heave pinworm infection

A

anorexia, restlessness, insomnia

167
Q

preferred treatments for pinworm

A

albendazole, pyrantel

168
Q

2nd most common helminth in US, most common worldwide

A

roundworm. ascaris-nematode

169
Q

risk factor for roundworm

A

nightsoil usage

170
Q

symptoms of roundworm

A

“wandering worms”, appendicitis, occlusion of common bile duct, intestinal perf

171
Q

preferred treatment of roundworm

A

albendazole–asymptomatic

pyrantel–heavy infection

172
Q

second most common worldwide helminth

A

hookworm-nematode

173
Q

common complication of hookworm

A

iron deficiency anemia

174
Q

preferred treatment of hookworm

A

albendazole for “creeping eruptions”

175
Q

symptoms of cestodes

A

GI upset, loss of appetite, CYSTICERCOSIS (only in pork. T. solium)

176
Q

cysticercosis

A

caused by ingestion of T. solium eggs or by autoinfection–>muscle, CNS

177
Q

preferred treatment for T. saginata

A

praziquantel. examine stool sample 3 mo. post

178
Q

preferred treatment for T. solium

A

praziquantel

179
Q

what happens when treat T. solium

A

disintegration of gravid segments. release of embryos from eggs. GIVE PURGATIVE

180
Q

neurocysticercosis

A

dexamethasone 1-2 d before antihelminthic 4-7d after completion. decrease inflammatory rxns

181
Q

Albendazole

A
  1. Antihelminthic
  2. absorption increased with fatty meal
  3. active drug metabolite: albendazole sulfoxide
  4. binds to B-tubulin of parasite. inhibition of microtubule polmerization and inhibition of microtubule dependent glucose uptake
  5. doesnt bind well to mammal cells
  6. SE: N/V/D, Teratogenic, increase LFTs (perform prior to tx and q2w), leukopenia (CBC prior to and q2w)
182
Q

Pyrantel

A
  1. antihelminthic
  2. pyrimidine derivative
  3. poorly absorbed from GIT
  4. broad spectrum OTC that is effective against variety of nematodes
  5. activation of cholinergic nicotinic receptors in nematode. depolarizing NM blockade=paralysis. expulsion from GIT
  6. SE: GI, HA, Liver stuff, pregnancy issues. not for children under 2 generally
183
Q

Praziquantel

A
  1. antihelminthic
  2. wide tissue distribution
  3. eliminated by kidneys and bile
  4. broad spectrum activity against SCHISTOSOMES (trematodes) and TAPEWORMS
  5. effective against neuroschistosomiasis
  6. induces muscle contraction–>spastic paralysis of musculature of worms by causing INCREASE IN CA ION INFLUX. suckers become dislodged
  7. SE: dizziness, HA, decreased mental alertness, N/V, increase in LFTs, rash, arthralgias, myalgias, issues with pregnancy
184
Q

transmission of entamoeba histolytica

A

ingestion of cysts. water, oral/anal

185
Q

symptoms of entamoeba histolytica

A

bloody diarrhea, hepatic abscess

186
Q

preferred drugs for entamoeba

A

asymptomatic carriers: iodoquinol, paromomycin

symptomatic: metronidazole followed by iodoquino or paromomycin

187
Q

Giardia lamblia

A

most common reported pathogen for infectious diarrhea US

188
Q

symptoms of giardia

A

profuse watery foul smelling diarrhea, only intestinal parasite

189
Q

transmissionof giardia

A

water, oral/anal, unwashed hands

190
Q

preferred tx of giardia

A

metronidazole, nitazoxanide

191
Q

trichomonas vaginalis

A

sexually transmitted urogenital protozoan. treat partners to prevent recurrence

192
Q

symptoms of trichomonas

A

malodorous yellow-green vaginal discharge, pruritis, dysuria, strawberry vagina

193
Q

preferred treatment of the trich

A

metronidazole

194
Q

cryptosporidium parvum

A

GI protozoan

195
Q

symptoms of crypto

A

liver, biliary, pancreas, lymphatics, lungs. large amounts of water diarrhea N/V, cramping and flatulence

196
Q

preferred treatment of crypto

A

nitazoxanidde, paromomycin

197
Q

metronidazole

A
  1. antiprotozoal
  2. good oral absorption. not used as luminal amebicide for asymptomaitc E. histolytica b/c of this
  3. use in SYMPTOMATIC PTS
  4. CIDAL DRUG
  5. gets reduced and binds to intracellular macromolecules DNA. inhibition of DNA synthesis
  6. good activity against ANAEROBIC BACTERIA. b fragilis, c. diff
  7. good activity against protozoa. entamoeba, trich, giardia
  8. resistance in some trich
  9. SE: disulfiram like interaction with alcohol. increased action of anticoagulants. N/HA, dry mouth, metallic taste, V/D, dark urine, seizures, neuropathies
  10. carcinogenic in rodents. avoid in pregnancy
198
Q

Iodoquionol

A
  1. antiprotozoal
  2. not well absorbed from GIT (luminal/contact amebicide)
  3. EFFECTIVE AGAINST ENTAMOEBA IN THE INTESTINAL LUMEN
  4. used in combo with metronidazole to treat symptomatic infections
  5. used alone for asymptomatic carriers
  6. Se: neurotoxicity, optic neuritis, loss of vision, GI upset,
199
Q

paromomycin

A
  1. antiprotozoal
  2. poor absorption for GIT, elminated in feces (contact/luminal amebicide)
  3. AN AMINOGLYCOSIDE. inhibits protein synthesis via binding 30s ribosomal subunit
  4. activity against entameoba. used alone for asymptomatic cyst passers
  5. used in combo with metronidazole for extraintestinal amebiasis
  6. treat CRYPTOSPORIDIOSIS in AIDs pts. it is DOC.
  7. SE: GI. increased motility, diarrhea, N/V, nephrotoxicity, ototoxicity, NM blocking effects
200
Q

Nitazoxanide

A
  1. antiprotozoal
  2. synthetic nitrothiazolyl salycyclamide derivative
  3. active metabolite-tizoxanide
  4. highly plasma protein bound. displaces other drugs. warfarin
  5. interferes with anaerobic energy metabolism by inhibits pyruvate:ferredoxin 2 oxidoreductase enzyme (electron transfer rxn)–>important for anaerobic metabolism of CRYPTO and GIARDIA
  6. activity against metronidazole resistant protozoans
  7. USES: treatment of diarrhea caused by crypto in immunocompetent children 1 y and on. diarrhea by giardia in children >1 y
  8. SE: abdominal pain, D/N/V/HA. FREE OF MUTAGENIC/CARCINOGENIC EFFECTS
201
Q

tumor must be what size to be diagnosed clinically

A

1 cm. reaching the gompertzian growth curve plateau phase

202
Q

debulking

A

removing large tumor volumes in order to increase growth rate, and thus improve effectiveness of drugs

203
Q

large tumor burden problems

A
  1. penetration
  2. metastases
  3. resistance
  4. large tumor mass
204
Q

log kill hypothesis

A

relationship of tumor cell number to 1. time of dx. 2. sx. 3. tx. 4. survival

205
Q

late G1 phase

A

burst of RNA synthesis

206
Q

G2 period

A

cell is tetraploid

207
Q

M phase

A

chromosomes form. daughter cells created

208
Q

chemotherapeutic failure

A

may be related to clonigenic/stem cells that retain potential to produce unlimited line of descendants

209
Q

CCNS agents

A

effective in low growth solid tumors

210
Q

CCS agents

A

good with hematologic malgnancies and proliferating ca

211
Q

resistance to methotrexate

A

decreased levels of target enzyme

altered affinity for target enzyme

212
Q

resistance to mercaptopurine

A

decreased activation/inacivation of drug

213
Q

resistance to alkylating agents

A

increased DNA repair

214
Q

resistance to antimetabolites

A

increased utilzation of salvage pathways for purine/pyrimidine biosynthesis

215
Q

karnofsky scale

A

performance status of CA pt. overall health and well being-used to determine if treatment should be adjusted/started

216
Q

Antineoplastic drugs with broad spectrum

A

cyclophsphamide, methotrexate, vincristine, doxorubicin

217
Q

streptozocin usage as antineoplastic

A

tx. of beta cells of islets of langerhans

218
Q

ways to test susceptibility to chemo

A

specific in vitro chemo-sensitivity testing
predictive drug sensitivity assays
drug receptor testing in biopsy specimens (endocrine responsive tumors-ER)

219
Q

Hashish

A

resin of marijuana

220
Q

hash oil

A

oily extract of resin of marijuana

221
Q

sinsemilla

A

dried tops, buds and flowers of marijuana

222
Q

dope

A

he doesn’t describe what this actually is..

223
Q

K2 or Spice

A

mixture of plant residues fortified with synthetic “designer” cannabinoid derivatives

224
Q

main active constituent of marijuana

A

tetrahydrocannabinol (THC)

225
Q

endogenous compounds that act on cannabinoid receptors

A

analog of arachidonic acid: anandamide, 2 arachidonylgylcerol. LIPID neuromodulators

226
Q

neuromodulators in CNS

A

act as retrograde neuromodulators to cause presynaptic inhibition of transmitter release

227
Q

CB1

A

found in CNS. frontal cortex, basal ganglia, limbic system (n accumbens and hippocampus), cerebellum, dorsal horn of spinal cord

228
Q

CB2

A

found in periphery

229
Q

cannabinoid receptors modulate

A

pain, appetite, mood, N/V, memory,motor, immune

230
Q

High

A

relaxation and increased sense of well being

231
Q

stoned

A

sedation and drowsiness, confusion, memory and cognitive impairment

232
Q

high doses of marijuana

A

hallucinations, paranoia, psychotic rxns

233
Q

CV effects of pot

A

tachycardia, postural hypotension, reddening of conjunctiva

234
Q

decreased intraocular pressure

A

only at high doses

235
Q

THC for chemotherapy

A

inhibition of vomiting reflex. Dronabinol, marinol

236
Q

Toxic effects of pot

A

lowered testosterone, teratogensis (like tobacco), amotivational syndrome, latent psychosis
DAMAGE TO LUNGS

237
Q

paraquat, glycophosphate

A

cause damage to lungs when used as pesticide on pot plants

238
Q

drugs to reduce toxic effects

A

anxiolytics (lorazepam, diazepam)

239
Q

withdrawl syndrome of marijuana

A

irritability, insomnia, tremors, depression, hyperalgesia, N/V

240
Q

Dronabinol/Marinol

A

cannabinoid derived drug

approved for tx of nausea in cancer chemo and tx of cachexia in AIDS pts

241
Q

Nabilone

A

cannabinoid derived drug

antiemetic

242
Q

cannabidiol

A

cannibinoid derived drug
lacks mind altering effects
signiicant antiseizure activity

243
Q

Rimonibant

A

antagonist of cannibinoid
appetite suppressant for tx of obesity
increased risk of depression and suicide

244
Q

designer cannabinoids

A

fake weed, K2, spice

structurally similar to interact with cannabinoid receptors

245
Q

States that allow recreational use of pot

A

colorado, washington

246
Q

does illinois allow medical marijuana?

247
Q

is chronic pain included in medical marijuana permission?

A

no (33 conditions)

248
Q

medical marijuana smoking

A

titrated easily dosage wise

BAD. filthy. fires.

249
Q

oral medical marijuana

A

slow, variable absorption

poor titration of dose

250
Q

alternative means of pot delivery

A

electronic joints
injection
transdermal
suppositories

251
Q

Salvia

A

spice, false weed, legal marijuana

  1. used in religious rituals by native ppl of mexico
  2. active agent is Salvinorin A. agonist at kappa opioid and D2 dopamine receptors
  3. hallucinogenic activities
  4. usually leafy material smoked
  5. has been criminalized. under review by DEA
252
Q

Kratom

A
  1. plant indigenous to thailand
  2. opioid like effects. chemically different from opioids
  3. useful for controlling opioid withdrawal symtpoms
  4. responses very different depending on person
  5. currently legal but being looked at

Pharmacology (6 decks)

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