Exam 9 Flashcards
1
Q
Nucleoside Reverse Transcriptase Inhibitors
A
Zidovudine, Didanosine, Lamivudine, Emtricitabine, abacavir
2
Q
Nucleotide Reverse Transcriptase Inhibitors
A
Tenofovir
3
Q
Non-Nucleoside Reverse Transcriptase Inhibitors
A
Nevirapine, Efavirenz
4
Q
Protease Inhibiors
A
Ritonavir, Indinavir sulfate, Nelfinavir mesylate, Lopinavir/Ritonavir, Atanavir sulfate
5
Q
NRTI’s
A
- inhibit HIV reverse transcriptase
2. generally do not interact with other drugs or meals
6
Q
Didanosine
A
NRTI that interacts with other drugs
7
Q
Zidovudine-AZT
A
- NRTI (tx HIV)
- synthetic dideoxynucleoside (pyrimadine) antiviral
- thymidine analogue. can’t form phosphodiester linkages. lacks 3’ hydroxyl. leads to chain termination
- converted intracellularly to active triphosphate
- Plasma protein bound
- SE: anemia, neutropenia, bone marrow tox, granulocytopenia, CNS, GI
- CONTRAINDICATIONS: compromised bone marrow fxn
8
Q
Combivir
A
lamivudine + zidovudine
9
Q
Trizivir
A
lamivudine + zidovudine + abacavir
10
Q
Drug that you do NOT give with Zidovudine
A
Stavudine. (antagonism)
11
Q
Didanosine
A
- NTRI (tx HIV)
- Dideoxynucleoside (purine)
- inhibitor of reverse transcriptase by COMPETING with dATP for active site of enzyme
- converted to active triphosphate in cell
- lacks 3’ hydroxyl group. leads to chain termination
- absorption depends on food and pH
- SE: peripheral neuropathy, pancreatitis, GI
12
Q
Zerit
A
DIdanosine + Zidovudine (or stavudine)
13
Q
Lamivudine
A
- NTRI (tx HIV)
- carbon of ribose is replaced by sulfur
- less potent but LESS TOXIC
- competitive inhibition of reverse transcriptase
- ACTIVE AGAINST HEPATITIS B (flare ups if stop drug)
- resistance is rapidly developed (avoid monotherapy)
14
Q
Epivir
A
Lamivudine
15
Q
Epzicom
A
Abacavir + Lamivudine
16
Q
Abacavir
A
- NRTI (tx HIV)
2. SE: SEVERE HSN RXN (rash, fever, malaise) + Resp and GI sx
17
Q
Ziagen
A
Abacavir
18
Q
Emtricitabine
A
- NRTI (tx HIV)
- derivative of Lamivudine
- BEST TOLERATED NRTI)
- SE: hyperpigmentation of palms and soles
- active against HEPATITIS B (can cause flare ups with drug withdrawl)
19
Q
Emtriva
A
Emtricitabine
20
Q
Truvada
A
fixed dose Emtricitabine + tenofovir
21
Q
Atripla
A
efavirenz + tenofovir + emtricitabine
22
Q
Tenofovir disoproxil
A
- NTRI (nucleotide)
- pro-drug of tenofovir
- effective against resistant HIV strains
- active against HEPATITIS B (flare up if discontinued)
- SE: N/V/D, renal tox
23
Q
Nucleotides
A
phosphorylated nucleosides
24
Q
Viread
A
tenofovir disoproxil
25
SIDE EFFECT OF ALL NNRTI's
severe rash. metabolized by hepatic p450 enzymes
26
Nevirapine
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)
27
Efavirenz
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
28
sustiva
efavirenz
29
protease inhibitor fxn
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
30
Ritonavir
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
31
Indinavir
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
32
Indinavir + Ritonavir
cross resistance
33
Nelfinavir
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
34
Treatment Naive patients-HIV
1. must have at lease three active antiretroviral meds that belong to different classes
35
Antiretroviral tx BACKBONE
2 nucleoside reverse transcriptase inhibitors (NRTIs)
36
Antiretroviral tx BASE
non-nucleoside reverse transcriptase inhibitor (NNRTI) OR protease inhibitor
37
NNRTI-based HIV treatment
1 NNRTI + 2 NRTIs
38
PI-based HIV treatment
1 or 2 PIs + 2 NRTIs
39
P. falciparum
malignant tartian malaria. most lethal. q3d.
40
P. vivax
benign tertian malaria. most common form. q3d. SECONDARY TISSUE FORMS
41
P. malariae
quartan malaria. q4d.
42
P. ovale
SECONDARY TISSUE FORMS
43
infectious form of malaria
sporozoite
44
malarial form that invades RBC
merozoite
45
Blood Schizonticides
"clinical cure". suppress symptoms and do not affect secondary tissue forms
46
Tissue Shizonticides
do not suppress symptoms. know out secondary tissue forms of P. vivax and P. ovale. prevent relapse. higher toxicity
47
Clinical cure
erythrocytic forms of parasite have been eradicated. no symptoms.
48
Radical Cure
all forms of parasite have been eradicated
49
Gametocytocidal agents
act on gametocytes. slow the spread of the disease.
50
Causal prophylaxis
prevent initial development of primary hepatic forms. Primiquine, pyrimethamine and proguanil may have some activity.
51
Suppressive Agents
MOST COMMON PROPHYLACTIC AGENT. do not affect secondary tissue forms. do not prevent relapses.
52
Chloroquine
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.
53
hydroxychloroquine
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.
54
used to treat rheumatoid arthritis and lupus erythematosus
Hydroxychloroquine-anti-inflammatory at high doses
55
Quinine/Quinidine gluconate
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)
56
Chloroquine resistant P. Falciparum treatment
Quinine/Quinidine gluconate, mefloquine, pyrimethamine, proguanil
57
Drug that has analgesia and antipyretic actions like aspirin
quinine/quinidine gluconate
58
Drug used for nocturnal leg cramps
quinine/quinidine gluconate
59
Mefloquine
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.
60
Sulfonamides
1. antimalarial.
2. inhibit the incorporation of PABA into folic acid
3. Sulfadoxine
61
Dihydrofolate reductase inhibitors
1. antimalarial
2. block conversion of dihydrofolic acid to tetrahydrofolic acid
3. Pyrimethamine, proguanil
62
Pyrimethamine and Proguanil
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
63
Pyrimethamine plus sulfadoxine
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
64
Atovaquone plus proguanil
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
65
halofantrine
1. new antimalarial
| 2. SE: GI
66
artemisinin
1. Chinese herbal preparation
| 2. antimalarial
67
tetrandine
1. antimalarial
| 2. against chloroquine resistant falcip
68
tetracycline ab (doxy)
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
69
Primaquine
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
70
Coartem
(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
71
treatment of pneumocystosis
primaquine plus clindamycin
72
G6P Hydrogenase deficiency
1. resistance to malaria
| 2. asians, afs, meds
73
Order of useage for acute uncomplicated attack
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)
74
PREVENTION OF RELAPSE
primaquine
75
prophylaxis
1. chloroquine
2. atovaquone + proguanil
3. doxy
4. mefloquine
5. proguanil/chlorquanide
6. pyrimethanime + sulfadoxine-->presumptive tx
7. primaquine-->flollow up tx
76
Mechlorethamine
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
77
Cyclophosphamide
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)
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
78
Carmustine
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
79
Cisplatin
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
80
Methotrexate
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
81
Leucovirin
bypasses metabolic block by methotrexate and protects normal cells
82
Mercaptopurine
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
83
Fluorouracil
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
84
Cytarabine
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
85
Daunorubicin HCL
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
86
Doxorubicin HCL
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
87
Vinblastine Sulfate
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
88
Vincristine Sulfate
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
89
Etoposide
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
90
block action of xanthine oxidase
allopurinol
91
Paclitaxel
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)
92
Prednisone
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
93
Dexamethasone
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
94
Tamoxifen
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
95
Imatinib Mesylate
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
96
Trastuzumab
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
97
Bcr-Abl fusion protein
constitutive abnormal tyrosine kinase created by t(9:22) philadelphia chromosomal translocation in CML
98
Chlorpromazine
1. Antipsychotic
2. phenothiazine
3. first modern antipsychotic
- -
1. greater effect on positive sx
2. neuroleptic effect
3. effects slow over 2-4 w
4. tolerance not an issue
5. issue with compliance. effects seem unpleasant
6. lowered seizure threshold
7. ENTIEMETIC: desnsitization of CRTZ
8. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
9. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
10. ANTIHISTAMINIC
11. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
12. Inhibition of ejaculation
13. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)-->gynecomastia, lactation, menstrual problems
14. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
15. AFFECTS SIMILAR TO T2DM
16. inhibition of Ca calmodulin-dependent processes
17. Teratogenesis
18. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
19. drugs can interact with other receptors too. like muscarinic. serotonergic...Blocking 5HT2 effective against negative sx of schizo
20. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
21. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
99
Fluphenazine
1. Antipsychotic
2. phenothiazine
3. piperazine phenothiazine (SIMILAR TO TRIFLUOPERAZINE)
4. long acting can be given depot injection q3-4w
- -
1. greater effect on positive sx
2. neuroleptic effect
3. effects slow over 2-4 w
4. tolerance not an issue
5. issue with compliance. effects seem unpleasant
6. lowered seizure threshold
7. ENTIEMETIC: desnsitization of CRTZ
8. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
9. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
10. ANTIHISTAMINIC
11. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
12. Inhibition of ejaculation
13. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)-->gynecomastia, lactation, menstrual problems
14. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
15. AFFECTS SIMILAR TO T2DM
16. inhibition of Ca calmodulin-dependent processes
17. Teratogenesis
18. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
19. drugs can interact with other receptors too. like muscarinic. serotonergic...Blocking 5HT2 effective against negative sx of schizo
20. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
21. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
100
Prochlorperazine
1. Antipsychotic
2. phenothiazine
3. aliphatic phenothiazine (SIMILAR TO TRIFLUOPERAZINE)
4. COMMONLY USED AS ANTIEMETIC
- -
1. greater effect on positive sx
2. neuroleptic effect
3. effects slow over 2-4 w
4. tolerance not an issue
5. issue with compliance. effects seem unpleasant
6. lowered seizure threshold
7. ENTIEMETIC: desnsitization of CRTZ
8. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
9. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
10. ANTIHISTAMINIC
11. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
12. Inhibition of ejaculation
13. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)-->gynecomastia, lactation, menstrual problems
14. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
15. AFFECTS SIMILAR TO T2DM
16. inhibition of Ca calmodulin-dependent processes
17. Teratogenesis
18. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
19. drugs can interact with other receptors too. like muscarinic. serotonergic...Blocking 5HT2 effective against negative sx of schizo
20. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
21. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
101
Trifluoperazine
1. Antipsychotic
2. phenothiazine
3. piperazine phenothiazine
4. MORE POTENT THAN CHLORPROMAZINE. less sedation, less anti-Ach activity, more pyramidal motor problems
- -
1. greater effect on positive sx
2. neuroleptic effect
3. effects slow over 2-4 w
4. tolerance not an issue
5. issue with compliance. effects seem unpleasant
6. lowered seizure threshold
7. ENTIEMETIC: desnsitization of CRTZ
8. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
9. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
10. ANTIHISTAMINIC
11. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
12. Inhibition of ejaculation
13. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)-->gynecomastia, lactation, menstrual problems
14. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
15. AFFECTS SIMILAR TO T2DM
16. inhibition of Ca calmodulin-dependent processes
17. Teratogenesis
18. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocortical,tuberoinfundibular..D2??)
19. drugs can interact with other receptors too. like muscarinic. serotonergic...Blocking 5HT2 effective against negative sx of schizo
20. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
21. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
102
Schizophrenia
excess DA activity in frontal cortex/limbic system
103
Traditional antipsychs act on what receptor
D2
104
Clozapine receptor antagonism
D4, 5Ht2. thus doesn't produce extrapyramidal effects
105
5HT2 blockers
effective against negative sx of schizo
106
drug to treat dystonia, akathisia, parkinsonism
anticholinergics
107
Neuroleptic malignant syndrome tx
dantrolene (inhibits CA release), Bromocryptine (DA antagonist)
108
Tardive dyskinesia
1. long term therapy sx
2. appears upon removal of med
3 anticholinergics make worse. suppressed w. more drug
4. no adequate treatment
109
Haloperidol
1. antipsychotic
2. nonphenothiazine
3. LESS ANTICHOLINERGIC ACTIVITY THAN CHLORPROMAZINE
4. more extrapyramidal effects
5. less sedation. available in long acting form
- -
1. greater effect on positive sx
2. neuroleptic effect
3. effects slow over 2-4 w
4. tolerance not an issue
5. issue with compliance. effects seem unpleasant
6. lowered seizure threshold
7. ENTIEMETIC: desnsitization of CRTZ
8. POIKILOTHERMIC: (less ability to control temp) effect on temp control center in hypothalamus
9. ANTICHOLINERGIC: dry mouth, less accommodatoin, constipation, urine retention
10. ANTIHISTAMINIC
11. CV Effects: ortho hypotension (a-receptor antagonism), tachycardia, EKG changes, cardiac arrest, sudden death
12. Inhibition of ejaculation
13. Endocrine: increased prolactin (dt blockade of hypothalamic and pituitary dopamine receptors)-->gynecomastia, lactation, menstrual problems
14. weight gain. stimulates appetite, fluid retention, affects insulin/glucose metabolism.
15. AFFECTS SIMILAR TO T2DM
16. inhibition of Ca calmodulin-dependent processes
17. Teratogenesis
18. INHIBITION OF DA RECEPTORS. in all systems (nigrostriatal, mesolimbic/mesocoritcla,tuberoinfundibular)
19. drugs can interact with other receptors too. like muscarinic. serotonergic...Blocking 5HT2 effective against negative sx of schizo
20. TOX: high margin of safety. allergic rxns, jaundice, rah, retinopathy, pigmentation of skin, CARDIOTOX,
21. EXTRAPYRAMIDAL MOTOR SX. acute dystonia (grimacing, spasms), akathisia (need to be moving all time), parkinsonism, Neuroleptic malignant syndrome (stupor, rigidity, hyperthermia), Tardive dyskinesia
110
Clozapine
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
Olanzapine
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
Risperdone
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
Aripiprazole
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
Quetiapine
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
Ziprasidone
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
DOC for Depression
SSRIs and 2nd gen antidepressants
117
2nd-3rd line for depression
Tricyclics and MAO-Is due to toxicity
118
Anxiolytics that have antidepressant asctivity
alprazolam/xanax
119
antidepressants with bipolar
may cause switch to mania
120
monoamine theory of depression
caused by deficit of monoamine NT (NE 5HT) in brain
121
tricyclics
block reuptake of NE and 5HT to a lesser extent
122
tertiary amines
have greater 5HT tahn seondary
123
SSRIs
inhibit 5HT reuptake
124
Bupoprion
selectively inhibits DA reuptake
125
Venlafaxine
inhibits both NE and 5HT
126
Trazodone and nefazodone
inhibit 5HT reuptake and block 5HT2
127
Antidepressent with worst anticholinergic SE
amitriptyline
128
Antidepressant with least anticholinergic SE
SSRIs
129
decreases cardiotoxic effects of tricyclics
sodium bicarb
130
what is not recommended in TCA overdose
physostigmine
131
serotonin syndrome
MAO inhibitors-tremors, HTN, hyperpyrexia, seizures
132
hormone involved in platelet aggregation and blood clotting
Serotonin
133
treatment of enuresis and urinary incontinence
imipramine
134
treatment of pain from neuropathies
tricyclics, dulozetine
135
withdrawl symptoms of antidepressants
lethargy, chills, neuro disturbances, muscle aches
136
Imipramine
1. Tricyclic antidepressant (serotonin/NE reuptake inhibitor)
2. prototype
3. change in density of neurotransmitter receptors with chronic treatment
137
amitriptyline
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
guanethidine
1. antihypertensive. reduce release of catecholamines
| 2. antidepressants decrease effect by blocking uptake by nerve endings
139
SE of antidepressants
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
Fluoxetine
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
Fluvoxamine
1. SSRI antidepressant
2. OCD in US. Depression in foreign countries
3. selective inhibitor of 5HT reuptake, SIMILAR TO FLUOXETINE
7. much less sedation, anticholinergic, and CV effects as tricyclics
8. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
9. association with suicidal behavior
142
Sertraline
1. SSRI antidepressant
2. selective inhibitor of 5HT reuptake, RESEMBLES FLUOXETINE IN SE AND EFFECTS
7. much less sedation, anticholinergic, and CV effects as tricyclics
8. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
9. association with suicidal behavior
3. Slow elimination. LONGER IN OLDER PATIENTS
4. several active metabolites
5. LESS POTENTIAL FOR DRUG INTERACTIONS THAN FLUOXETINE
143
Paroxetine
1. SSRI antidepressant
2. selective inhibitor of 5HT reuptake, resemble luoxetine
much less sedation, anticholinergic, and CV effects as tricyclics
8. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
9. association with suicidal behavior
3. DIFFERS FROM FLUOXETINE AND SERTRALINE BC IT IS MORE RAPIDLY METABOLISED. DOES NOT FORM ACTIVE METABOLITES
4. can interact with many other drugs
5. more WEIGHT GAIN than other SSRIs
144
Citalopram
"LIKE SERTRALINE"...Newest SSRI
1. SSRI antidepressant
2. selective inhibitor of 5HT reuptake, RESEMBLES FLUOXETINE IN SE AND EFFECTS
7. much less sedation, anticholinergic, and CV effects as tricyclics
8. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
9. association with suicidal behavior
3. Slow elimination. LONGER IN OLDER PATIENTS
4. several active metabolites
5. LESS POTENTIAL FOR DRUG INTERACTIONS THAN FLUOXETINE
145
Escitalopram
"LIKE SERTRALINE"..ISOMER OF CITALOPRAM
1. SSRI antidepressant
2. selective inhibitor of 5HT reuptake, RESEMBLES FLUOXETINE IN SE AND EFFECTS
7. much less sedation, anticholinergic, and CV effects as tricyclics
8. SE: HA, anxiety, tremor, agitation, nausea, sexual dysfunction
9. association with suicidal behavior
3. Slow elimination. LONGER IN OLDER PATIENTS
4. several active metabolites
5. LESS POTENTIAL FOR DRUG INTERACTIONS THAN FLUOXETINE
146
Venlafixine
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
Desvenlafixine
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
Duloxetine
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
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
149
Trazadone
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
Nefazodone
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
Bupropion
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
Mirtazepine
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
Atomexitine
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
Phenelzine
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
Tranylcypromine
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
Selegiline
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
action of MAO-A
metabolizes NE and 5HT
158
action of MAO-B
metabolizes DA
159
Lithium Carbonate
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
Valproic acid analog
1. mood stabilizers.
2. anti-epileptic
3. tx manic depressive disorders (bipolar)
161
carbamazepine
1. mood stabilizers.
2. anti-epileptic
3. tx manic depressive disorders (bipolar)
162
clonazepam
1. mood stabilizers.
2. anti-epileptic
3. tx manic depressive disorders (bipolar)
163
depakene
valproic acid analog
164
depakote
valproic acid analog
165
most common helminth infection in US
pinworm-nematode
166
symptoms of heave pinworm infection
anorexia, restlessness, insomnia
167
preferred treatments for pinworm
albendazole, pyrantel
168
2nd most common helminth in US, most common worldwide
roundworm. ascaris-nematode
169
risk factor for roundworm
nightsoil usage
170
symptoms of roundworm
"wandering worms", appendicitis, occlusion of common bile duct, intestinal perf
171
preferred treatment of roundworm
albendazole--asymptomatic
| pyrantel--heavy infection
172
second most common worldwide helminth
hookworm-nematode
173
common complication of hookworm
iron deficiency anemia
174
preferred treatment of hookworm
albendazole for "creeping eruptions"
175
symptoms of cestodes
GI upset, loss of appetite, CYSTICERCOSIS (only in pork. T. solium)
176
cysticercosis
caused by ingestion of T. solium eggs or by autoinfection-->muscle, CNS
177
preferred treatment for T. saginata
praziquantel. examine stool sample 3 mo. post
178
preferred treatment for T. solium
praziquantel
179
what happens when treat T. solium
disintegration of gravid segments. release of embryos from eggs. GIVE PURGATIVE
180
neurocysticercosis
dexamethasone 1-2 d before antihelminthic 4-7d after completion. decrease inflammatory rxns
181
Albendazole
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
Pyrantel
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
Praziquantel
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
transmission of entamoeba histolytica
ingestion of cysts. water, oral/anal
185
symptoms of entamoeba histolytica
bloody diarrhea, hepatic abscess
186
preferred drugs for entamoeba
asymptomatic carriers: iodoquinol, paromomycin
| symptomatic: metronidazole followed by iodoquino or paromomycin
187
Giardia lamblia
most common reported pathogen for infectious diarrhea US
188
symptoms of giardia
profuse watery foul smelling diarrhea, only intestinal parasite
189
transmissionof giardia
water, oral/anal, unwashed hands
190
preferred tx of giardia
metronidazole, nitazoxanide
191
trichomonas vaginalis
sexually transmitted urogenital protozoan. treat partners to prevent recurrence
192
symptoms of trichomonas
malodorous yellow-green vaginal discharge, pruritis, dysuria, strawberry vagina
193
preferred treatment of the trich
metronidazole
194
cryptosporidium parvum
GI protozoan
195
symptoms of crypto
liver, biliary, pancreas, lymphatics, lungs. large amounts of water diarrhea N/V, cramping and flatulence
196
preferred treatment of crypto
nitazoxanidde, paromomycin
197
metronidazole
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
Iodoquionol
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
paromomycin
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
Nitazoxanide
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
tumor must be what size to be diagnosed clinically
1 cm. reaching the gompertzian growth curve plateau phase
202
debulking
removing large tumor volumes in order to increase growth rate, and thus improve effectiveness of drugs
203
large tumor burden problems
1. penetration
2. metastases
3. resistance
4. large tumor mass
204
log kill hypothesis
relationship of tumor cell number to 1. time of dx. 2. sx. 3. tx. 4. survival
205
late G1 phase
burst of RNA synthesis
206
G2 period
cell is tetraploid
207
M phase
chromosomes form. daughter cells created
208
chemotherapeutic failure
may be related to clonigenic/stem cells that retain potential to produce unlimited line of descendants
209
CCNS agents
effective in low growth solid tumors
210
CCS agents
good with hematologic malgnancies and proliferating ca
211
resistance to methotrexate
decreased levels of target enzyme
| altered affinity for target enzyme
212
resistance to mercaptopurine
decreased activation/inacivation of drug
213
resistance to alkylating agents
increased DNA repair
214
resistance to antimetabolites
increased utilzation of salvage pathways for purine/pyrimidine biosynthesis
215
karnofsky scale
performance status of CA pt. overall health and well being-used to determine if treatment should be adjusted/started
216
Antineoplastic drugs with broad spectrum
cyclophsphamide, methotrexate, vincristine, doxorubicin
217
streptozocin usage as antineoplastic
tx. of beta cells of islets of langerhans
218
ways to test susceptibility to chemo
specific in vitro chemo-sensitivity testing
predictive drug sensitivity assays
drug receptor testing in biopsy specimens (endocrine responsive tumors-ER)
219
Hashish
resin of marijuana
220
hash oil
oily extract of resin of marijuana
221
sinsemilla
dried tops, buds and flowers of marijuana
222
dope
he doesn't describe what this actually is..
223
K2 or Spice
mixture of plant residues fortified with synthetic "designer" cannabinoid derivatives
224
main active constituent of marijuana
tetrahydrocannabinol (THC)
225
endogenous compounds that act on cannabinoid receptors
analog of arachidonic acid: anandamide, 2 arachidonylgylcerol. LIPID neuromodulators
226
neuromodulators in CNS
act as retrograde neuromodulators to cause presynaptic inhibition of transmitter release
227
CB1
found in CNS. frontal cortex, basal ganglia, limbic system (n accumbens and hippocampus), cerebellum, dorsal horn of spinal cord
228
CB2
found in periphery
229
cannabinoid receptors modulate
pain, appetite, mood, N/V, memory,motor, immune
230
High
relaxation and increased sense of well being
231
stoned
sedation and drowsiness, confusion, memory and cognitive impairment
232
high doses of marijuana
hallucinations, paranoia, psychotic rxns
233
CV effects of pot
tachycardia, postural hypotension, reddening of conjunctiva
234
decreased intraocular pressure
only at high doses
235
THC for chemotherapy
inhibition of vomiting reflex. Dronabinol, marinol
236
Toxic effects of pot
lowered testosterone, teratogensis (like tobacco), amotivational syndrome, latent psychosis
DAMAGE TO LUNGS
237
paraquat, glycophosphate
cause damage to lungs when used as pesticide on pot plants
238
drugs to reduce toxic effects
anxiolytics (lorazepam, diazepam)
239
withdrawl syndrome of marijuana
irritability, insomnia, tremors, depression, hyperalgesia, N/V
240
Dronabinol/Marinol
cannabinoid derived drug
| approved for tx of nausea in cancer chemo and tx of cachexia in AIDS pts
241
Nabilone
cannabinoid derived drug
| antiemetic
242
cannabidiol
cannibinoid derived drug
lacks mind altering effects
signiicant antiseizure activity
243
Rimonibant
antagonist of cannibinoid
appetite suppressant for tx of obesity
increased risk of depression and suicide
244
designer cannabinoids
fake weed, K2, spice
| structurally similar to interact with cannabinoid receptors
245
States that allow recreational use of pot
colorado, washington
246
does illinois allow medical marijuana?
yes
247
is chronic pain included in medical marijuana permission?
no (33 conditions)
248
medical marijuana smoking
titrated easily dosage wise
| BAD. filthy. fires.
249
oral medical marijuana
slow, variable absorption
| poor titration of dose
250
alternative means of pot delivery
electronic joints
injection
transdermal
suppositories
251
Salvia
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
Kratom
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
