antimicrobials, antifungals, antivirals, cancer, immunoregulatory Flashcards
(106 cards)
1
Q
Penicillin
A
antimicrobial - beta lactam
2
Q
cephalosporin
A
antimicrobial - beta lactam
3
Q
carbapenem
A
antimicrobial - beta lactam - imipenem/cilastatin
4
Q
monobactam
A
antimicrobial - aztreonam only one - beta lactam
5
Q
glycopeptide
A
antimicrobial - vancomycin, bacitracin - for topical use for gram-positive and certain gram-negative bacteria.
6
Q
tetracycline
A
antimicrobial - • Drug of choice • Rickettsial diseases: Rocky Mountain spotted fever, typhus • Mycoplasma pneumoniae
• Chlamydia pneumoniae
• Lyme disease (Borrelia burgdorferi) • Brucellosis
• Alternative agent • Plague
• Pelvic inflammatory disease
• As treatment of syndromes • Acne: low-dose oral or topical
7
Q
macrolide
A
antimicrobial - erythromycin
Drug of choice Mycoplasma pneumonia,
Streptococcal (group A streptococcus (GAS)) upper respiratory tract
infection (penicillin-allergic patient), Legionella infection
Alternative agent
• Lyme disease
• Chlamydia infection
As treatment of syndromes
• Bacterial bronchitis
• Otitis media (middle ear infection) with sulfonamide • Acne, topical
Prophylaxis
• Large bowel surgery • Oral surgery
and ketolides
8
Q
aminoglycosides
A
antimicrobial. ineffective against anaerobic bacteria and fungi
9
Q
chloramphenicol
A
antimicrobial - aplastic anemia!!!!!!
10
Q
sulfonamides
A
antimicrobial - sulfamethoxazole gastrointestinal disturbances (nausea, vomiting, anorexia) and allergic skin reactions (such as rash and urticaria).
11
Q
trimethoprim
A
antimicrobial - gastrointestinal disturbances (nausea, vomiting, anorexia) and allergic skin reactions (such as rash and urticaria).
12
Q
• Fluoroquinolones
A
antimicrobials - • The earlier generation agents are, in general, more narrow spectrum than the later ones.
13
Q
nitrofurans
A
antimicrobials - • Not to be used in patients with a creatinine clearance of 60 ml/min or less
urinary tract infection
14
Q
colistin (polymixin E), polymixin B
A
antimicrobials • Their use was abandoned, except in patients with cystic fibrosis, because of toxicity (they react with and affect the membranes of human cells, resulting in kidney damage and neurotoxicity).
• Because they are not well absorbed from the gastrointestinal tract, oral administration is occasionally used for the treatment of diarrhea.
15
Q
rifampin
A
antimicrobials - anti-tuberculosis
16
Q
isonazid
A
antimicrobials - anti-tuberculosis
17
Q
pyrazinamide
A
antimicrobials - anti-tuberculosis
18
Q
• rifampin, dapsone, clofazimine
A
antimicrobials - anti-leprosy
- Is presumed that rifampin acts by inhibition of Mycobacterium leprae DNA-dependent RNA polymerase.
- Similar to sulfonamides, dapsone (diamino-diphenyl sulphone) acts as an inhibitor of dihydropteroate synthetase in folate synthesis to produce a bacteriostatic effect.
19
Q
flucytosine
A
antifungals - nucelic acid synthesis
20
Q
caspofungin
A
antifungals - cell wall
o blocks the synthesis of a major fungal cell wall component, 1-3-beta-D-glucan.
21
Q
griseofulvin
A
antifungals - nuclear division - o inhibits fungal mitosis through interaction with polymerized microtubules
22
Q
amphotericin B
A
antifungals - cell membrane - o Polyenes act by binding to sterols in the cell membrane and forming channels, allowing K+ and Mg2+ to leak out.
o Fungi that not have ergosterol are not susceptible to amphotericin B.
o The initial reactions, usually fever to as high as 40° C, chills, headache, general discomfort, nausea, and occasionally hypotension.
o Anemia with hematocrits of 22% to 35% develops in most patients who receive a normal course of therapy. This is the result of reduced erythropoiesis due to inhibition of erythropoietin production.
23
Q
nystatyn
A
antifungals - ergosterol component
24
Q
fluconazole
A
antifungals - CYTOCHROME P450!!!!!
25
itraconazole
antifungals - CYTOCHROME P450
26
terbinafine
o Terbinafine inhibits ergosterol biosynthesis
via inhibition of squalene epoxidase
27
antimetabolites (S phase)
cancer - cell cycle - growth fraction malignancies (high replicating cells), such as hematologic cancers.
28
taxanes
cancer - cell cycle - growth fraction malignancies (high replicating cells), such as hematologic cancers.
29
vinca alkaloids (M phase)
cancer - cell cycle - growth fraction malignancies (high replicating cells), such as hematologic cancers.
30
antitumor antibiotics (G2-M phase)
cancer - cell cycle - growth fraction malignancies (high replicating cells), such as hematologic cancers.
31
alkylating agents
cancer - Cell-cycle nonspecific (CCNS) drugs (useful against tumors that have a low percentage of replicating cells, also effective against replicating cells).
32
anthracyclines
cancer - Cell-cycle nonspecific (CCNS) drugs (useful against tumors that have a low percentage of replicating cells, also effective against replicating cells).
33
antitumor antibiotics
cancer - Cell-cycle nonspecific (CCNS) drugs (useful against tumors that have a low percentage of replicating cells, also effective against replicating cells).
34
platinum analogs
cancer - Cell-cycle nonspecific (CCNS) drugs (useful against tumors that have a low percentage of replicating cells, also effective against replicating cells).
35
antimetabolites (methotrexate, • 6-MP and 6-TG , • 5-FU (5-Fluorouracil) and Cytarabine )
cancer - antineoplastic drugs - antimetabolites
o Low dose of MTX is anti-inflammatory and immuno-suppressive.
36
antibiotics (• Doxorubicin and daunorubicin)
cancer - antineoplastic drugs
o Used in drug combinations, doxorubicin is one of the most important and widely used anticancer drugs.
o Cardiotoxicity or heart failure.
37
antibiotics (dactinomycin)
cancer - atineoplastic o This drug is also immunosuppressive.
38
antibiotics (bleomycin)
cancer - antineoplastic
pulmonary toxicity
39
topoisomerase inhibitors
cancer - antineoplastic - Topoisomerase inhibitors (Epipodophyllotoxins) (inhibit topoisomerase II- mediated religation of DNA breaks): Etoposide (VP-16), teniposide (VM-26).
• Etoposide (VP-16) is phase-specific (active in G2).
40
alkylating agents (mechlorethamine)
cancer - antineoplastic - • They are mutagenic and carcinogenic and can lead to a second malignancy, such as acute leukemia.
• Mechlorethamine
o It causes lymphocytopenia.
o It alkylates the N-7nitrogenof a guanine residue in one or both strands of a DNA molecule, leading to cross- linkage between guanine residues in the DNA chains.
41
alkylating agents (cyclophosphamide)
cancer - antineoplastic - o It is the most commonly used alkylating agent.
42
alkylating agents (temozolomide)
cancer - antineoplastic - can also cross blood-brain barrier
43
alkylating agents (nitrosoureas)
cancer - antineoplastic - another group of drugs that can cross blood-brain barrier and are used to treat brain cancers.
44
alkylating agents (cisplatin and carboplatin)
cancer - antineoplastic - can cross-link DNA
45
microtubule inhibitors (• Vincristine (VX, oncovin), vinblastine (VBL) and vinorelbine (VRB) )
cancer - antineoplastic - o They block cell mitosis in metaphase, are cell-cycle specific and phase-specific.
46
microtubule inhibitors (• Taxanes: paclitaxel (taxol) and docetaxel)
cancer - antineoplastic
47
steroid hormones and their antagonists (tamoxifen)
cancer - antineoplastic - • For example, anti-estrogen tamoxifen is used to prevent estrogen stimulation of breast cancer cells.
• Tamoxifen and similar drugs
• Tamoxifen is an estrogen antagonist.
• It binds to estrogen receptor but fails to induce estrogen-responsive genes, and RNA synthesis does not ensue. The growth-promoting effects of estrogen and other factors are suppressed.
48
steroid hormones and their antagonists (toremifene)
cancer - antineoplastic - similar and closely related to tamoxifen
49
steroid hormones and their antagonists (fulvestrant)
cancer - antineoplastic - destroys estrogen receptors
50
steroid homrones and their antagonists (prednisone)
cancer - antineoplastic - o Is a potent, synthetic, anti-inflammatory corticosteroid with less mineralocorticoid activity than cortisol.
o For treatment of lymphoma and acute lymphocytic leukemia.
o Binds to intracellular receptors and triggers production of specific proteins.
Corticosteroids
• Among these drugs, prednisone is most widely used.
• Actions and mechanisms:
- Regression of lymphoid tissues.
- Enhance destruction of lymphocytes (especially T lymphocytes).
- Interfere with the cell cycle of activated lymphoid cells.
- Inhibit leukocyte and other cell functions (leukocyte recruitment, adhesion, migration, chemotaxis, phagocytosis, activation of CTLs, functions of endothelial cells, fibroblasts, etc.).
- Inhibit antibody formation due to the drug’s catabolic effect.
- Inhibit inflammatory mediators (eg, kinins, prostagladins, leukotriences, IL-1 and IL-6, etc.).
51
monoclonal antibodies (trastuzumab, cetuximab)
cancer - antineoplastic - They are employed as an informer,identifying malignant cells as targets for attack by complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC).
They are also used to block selected growth factor receptors to affect cell growth.
They are also used as biological “missiles” for carrying a radio-pharmaceutical or biologic toxin warhead to the targeted cancer cells.
Trastuzumab
Causes regression of breast cancer.
• Cetuximab
o used in combination for the 1st-line therapy of metastatic colorectal cancer, head and neck cancer.
52
biological response modifiers (interleukin 2)
cancer - antineoplastic - (interfere signal transduction pathways): e.g., IFN-
53
tyrosine kinase inhibitors (imatinib, gefinitib)
cancer - antineoplastic - Imatinib and gefitinib, are both oral drugs.
• Imatinib acts as a signal transduction inhibitor, is used specifically to inhibit the activity of tumor tyrosine kinase BCR-ABL, hence to inhibit cell proliferation, for very effective treatment of chronic myelogenous leukemia. Mutations in the BCR-ABL kinase domain occur that lead to resistance. (Similar drugs: dasatinib and nilotinib, more potent)
• Gefitinib is a specific inhibitor of the EGFR tyrosine kinase that competitively inhibits ATP binding. But it has a low response rate. Similar drug: erlotinib.
54
proteosome inhibitors (bortezomib)
cancer - antineoplastic - Bortezomib (Velcade): inhibit proteosome and permit activation of programmed cell death in neoplastic cells, for the treatment of multiple myeloma and mantle cell lymphoma.
55
angiogenesis inhibitors (bevacizumab)
cancer - antineoplastic - The best studied proangiogenic factor is VEGF whose elevated levels are associated with poor prognosis and increased risk of metastasis in a variety of malignancies. VEGFR-1 and -2 are expressed in endothelial cells and cancer cells.
(anti-VEGF) inhibits VEGF-A.
56
angiogenesis inhibitors (Vandetanib)
cancer - antineoplastic - is a kinase inhibitor mainly for
VEGFR.
57
angiogenesis inhibtiors (thalidomide and lenalidomide)
cancer - antineoplastic - inhibit TNF
58
differentiating agents - (all-trans-retinoic acid)
cancer - antineoplastic - All-trans-retinoic acid (ATRA, Tretinoin): drives leukemic promyelocytes
59
neuramidase inhibitors (oseltamivir)
antiviral - • an orally active prodrug, hydrolyzed by the liver to its active form. • • GI discomfort and nausea
60
neuramidase inhibitors (zanamivir)
antiviral - • is either inhaled or administered intranasally. Intravenous zanamivir is also available. • • Avoided in individuals with severe respiratory diseases or asthma.
61
neuramidase inhibitors (peramivir)
antiviral agents - • a new neuraminidase inhibitor (intravenous only), approved in Dec 2014.
• • Adverse effect: serious skin reactions.
62
viral uncoating inhibitors (adamantane derivatines)
antiviral agents - • amantadine (Symmetrel) and
o minor neurologic symptoms include insomnia, dizziness and ataxia.
o • Use with caution in patients with psychiatric, neurologic and renal problems.
• rimantadine (Flumadine).
o Both were reported to be effective for prophylaxis and treatment of susceptible strains of influenza A.
o is equally effective, does not cross blood-brain barrier (less adverse effects).
o • Both drugs can cause GI intolerance.
• These drugs are not currently recommended for prophylaxis or treatment of influenza.
63
ribavirin
antiviral - • Oral ribavirin: for treating severe RSV infections in infants and young children.
• • Oral ribavirin: for treating chronic HCV infection (combined with injected pegIFN--2a or pegIFN--2b).
• • Intravenous and/or aerosol ribavirin: for severe influenza virus infection and for immunosuppressed patients with adenovirus, vaccinia, parainfluenza or
64
hepatic viral infections (adefovir)
antiviral agents - o a nucleotide, also for HIV infections.
65
hepatic viral infections (entecavir)
antiviral agents - a guanosine analog
66
hepatic viral infections (telbivudine)
a synthetic thymidine analog
67
hepatic viral infections (tenofovir)
antiviral agents - a nucleotide analog; also for HIV infections
68
hepatic viral infections (interferon)
antiviral agents - • Induction of host cell enzymes that inhibit viral RNA translation, degradation of viral RNA, and stimulation of immune system.
• Adverse effects: flu-like symptoms, bone marrow suppression, neurotoxicity, autoimmune disorders
69
hepatic viral infections (lamivudine)
* Inhibits both HBV DNA polymerase and HIV reverse transcriptase.
* Absorbed orally, well tolerated.
* • For treatment of HBV and HIV infections.
70
herpesvirus infections (acyclovir), • The drugs are effective only during acute phase of infections, cannot prevent recurrences.
antiviral - o Is the drug of choice in treating HSV1, HSV2, and VZV.
o Most common use is for treatment of genital herpes infections.
o Adverse effects depend on the routes: local irritation (topical); headache and GI upsets (oral); transient renal dysfunction at high dose (iv).
71
herpesvirus infections (valacyclovir, famciclovir, penciclovir), • The drugs are effective only during acute phase of infections, cannot prevent recurrences.
antiviral - o Mainly used for genital herpes and VZV
| o Penciclovir is only for topical use
72
herpesvirus infections (ganciclovir), • The drugs are effective only during acute phase of infections, cannot prevent recurrences.
antiviral - o For treatment of CMV retinitis in AIDS patients, and for CMV prophylaxis in transplant patients.
o • >100timesactiveagainstCMV (cytomegalovirus) than acyclovir.
73
herpesvirus infections (foscarnet), • The drugs are effective only during acute phase of infections, cannot prevent recurrences.
antiviral - o For the treatment of CMV retinitis in immunocompromised hosts, and for acyclovir- resistant HSV and herpes zoster infections.
o • Is only for iv administration.
o Adverse effects: nephrotoxicity, anemia, nausea and fever.
74
nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs) (zidovudine)
antiviral - anti HIV agents - • Toxic to bone marrow, headaches, toxicity can be potentiated by other drugs.
75
nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs) (didanosine)
antiviral - anti HIV agents - • o May cause pancreatitis (monitoring amylase is needed), peripheral neuropathy.
76
nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs) (lamivudine)
antiviral - anti HIV agents
77
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) (nevirapine)
antiviral - anti HIV agents - only for HIV 1 infection, lack of bone marrow, lack of cross-resistance with NRTIs
o Adverse effects: rash can be severe; fatal hepatotoxicity can occur (need to monitor transaminases).
o Induces CYP3A4 of cytochrome P450 enzymes, and metabolism of a number of other drugs. (drug interactions! --- It increases metabolism of oral contraceptives, ketoconazole, methadone, metronidazole, quinidine, theophylline, warfarin.)
78
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) (efavirenz)
antiviral - anti HIV agents - only for HIV 1 infection, lack of bone marrow, lack of cross-resistance with NRTIs
o Efavirenz plus 2 NRTIs remains a preferred regimen for treatment-naïve patients.
o ATRIPLA: efavirenz + tenofovir + emtricitabine (once daily co-formulation single pill).
o Etravirine: is used when HIV-1 is resistant to other NNRTIs.
79
protease inhibitors
antiviral - • Are selective, reversible inhibitors of HIV aspartyl protease (for formation of reverse transcriptase, protease, integrase and structural proteins), and block viral maturation.
• Potential dangerous interactions: – Excessive sedation from midazolam,
• triazolam
– Bleeding from warfarin
– Respiratory depression from fetanyl
• GI intolerance.
• Disturbances in glucose and lipid metabolism (diabetes, hypertriacylglycerolemia, hypercholesterolemia, and fat redistribution: “buffalo hump”, and breast enlargement.).
• Ritonavir
• Saquinavir
• Lopinavir
• Indinavir and other PIs
• Well absorbed orally.
• • GI symptoms and headache.
• • Nephrolithiasis( kidneystone) mayoccur (It is not widely prescribed now).
80
Viral entry inhibitors
antiviral - • Enfuvirtide
o Can be combined with other antiviral agents.
o – Is costly and is only given subcutaneously (twice daily).
• Maraviroc
81
Integrase inhibitors (raltegravir)
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antiviral - • Raltegravir (Isentress), the first in a new class of oral HIV drugs called HIV-1 integrase strand transfer inhibitors (InSTI), was approval for use in combination therapy for treatment– experienced adults infected with HIV-1 strains resistant to multiple anti-retroviral agents.
• Dolutegravir and elvitegravir: two newly approved integrase inhibitors for HIV treatment.
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82
glucocorticoids (prednisone, prednisolone, methylprednisolone)
immunoregulatory agents - immunosuppressive drugs - • Among these drugs, prednisone is most widely used.
• Immunosuppressive actions and mechanisms:
- Regression of lymphoid tissues.
- Enhance destruction of lymphocytes (esp. T lymphocytes).
- Interfere with the cell cycle of activated lymphoid cells.
- Inhibit leukocyte functions (leukocyte recruitment, migration, chemotaxis, phagocytosis, activation of CTLs, etc.).
- Inhibit antibody formation due to the drug’s catabolic effect.
- Inhibit inflammatory mediators (eg, kinins, prostaglandins, leukotrienes, IL-1 and IL-6, etc.).
• Prednisone and other glucocorticoids inhibit the action of COX-2 and the formation of prostaglandins by:
o Repressing COX-2 gene and enzyme expression;
o repressing the expression of cytokines that activate COX-2;
o blocking the function of phospholipase A2 therefore limiting the availability of arachidonic acids (the COX-2 substrates).
Clinical Uses:
• Organ and tissue transplantation.
• Auto-immune diseases: prednisone is the drug of choice in treating various autoimmune diseases.
• Inflammatory diseases: eg, allergy and bronchial asthma, rheumatoid arthritis, inflammatory bowel disease, etc.
• Adverse effects: suppression of pituitary- adrenal axis, peptic ulcer, catabolic effects, and increased susceptibility to serious infections.
83
cytokine inhibitors (cyclosporine (CsA))
immunoregulatory agents - immunosuppressive - • • Cytokines are soluble, antigen-nonspecific, signaling proteins that bind to cell surface receptors on a variety of cells.
• • Cytokinesinclude:
– Interleukins (ILs).
– Interferons (IFNs).
– Tumor necrosis factors (TNFs).
– Transforming growth factors (TGFs). – Colony-stimulating factors (CSFs).
• – Chemokines.
• IL-2 is a cytokine that stimulates the proliferation of antigen-primed (helper) T cells, which subsequently produce more IL-2, IFN-
84
cytokine inhibitors (tacrolimus)
immunoregulatory agents - immunosuppressive - • • Cytokines are soluble, antigen-nonspecific, signaling proteins that bind to cell surface receptors on a variety of cells.
• • Cytokinesinclude:
– Interleukins (ILs).
– Interferons (IFNs).
– Tumor necrosis factors (TNFs).
– Transforming growth factors (TGFs). – Colony-stimulating factors (CSFs).
• – Chemokines.
Tacrolimus is more potent and allows lower dose of glucocorticoid to be used.
• Tacrolimus binds to a different immunophilin (FKBP-12).
85
cytokine inhibitors (sirolimus)
immunoregulatory agents - immunosuppressive - • • Cytokines are soluble, antigen-nonspecific, signaling proteins that bind to cell surface receptors on a variety of cells.
• • Cytokinesinclude:
– Interleukins (ILs).
– Interferons (IFNs).
– Tumor necrosis factors (TNFs).
– Transforming growth factors (TGFs). – Colony-stimulating factors (CSFs).
• – Chemokines.
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o Sirolimus (rapamycin): also binds to FKBP-12, then forming a complex with mTOR (mammalian Target Of Rapamycin).
o Sirolimus binding to mTOR blocks the progression of activated T cells from the G1 to the S phase of cell cycle, consequently, the proliferation of these cells. (Sirolimus does not owe its effect to lowering IL-2 production but rather, to inhibiting the cellular response to IL-2.)
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86
cytotoxic drugs (azathioprine)
immunoregulatory agents - immunosuppressive - Antimetabolites: methotrexate (MTX), leflunomide,
azathioprine, mycophenolate mofetil (MMF).
• Immunosuppressive antimetabolites
Are generally used in combination with glucocorticoids and calcineurin inhibitors CsA and tacrolimus.
Azathioprine is metabolized in vivo to 6- mercaptopurine (6-MP) and then thioinosinic acid to have antitumor and immuno- suppressive effects.
87
cytotoxic drugs (mycophenolate mofetil)
immunoregulatory agents - immunosuppressive - Antimetabolites: methotrexate (MTX), leflunomide,
azathioprine, mycophenolate mofetil (MMF).
• Immunosuppressive antimetabolites
Are generally used in combination with glucocorticoids and calcineurin inhibitors CsA and tacrolimus.
(MMF) inhibits T and B lymphocyte proliferation through inhibition of purine synthesis (therefore inhibits the generation of CTLs and plasma cells).
88
cytotoxic drugs (alkylating agents: cyclophosphamide)
immunoregulatory agents - immunosuppressive
89
cytotoxic drugs (antimetabolites: methotrexate)
immunoregulatory agents - immunosuppressive - Is the mainstay of disease- modifying anti-rheumatic drugs. Doses are much lower than those needed in cancer chemotherapy.
MTX is structurally related to folic acid, and acts as an antagonist of that vitamin by inhibiting dihydrofolate reductase – the enzyme that converts folic acid to its active coenzyme form: tetrahydrofolic acid (FH4).
It decreases biosynthesis of adenine, guanine, thymidine, methionine and serine, leads to depressed DNA, RNA and protein synthesis and ultimately cell death.
90
cytotoxic drugs (antimetabolites: leflunomide)
immunoregulatory agents - immunosuppressive - o Leflunomide reversibly inhibits dihydroorotate dehydrogenase (DHODH), and therefore deprives the cells of the precursor for uridine monophosphate.
o It reduces pain and inflammation associated with the disease, slows the progression of structural damage.
91
immunosuppressive alkylating agents
immunoregulatory agents - immunosuppressive - Alkylation of DNA (covalent binding) is the cytotoxic reaction that is lethal to the cells.
They do not discriminate between cycling and resting cells (cell-cycle nonspecific).
They are mutagenic and carcinogenic and can lead to a second malignancy, such as acute leukemia.
92
antibodies and biological agents (antithymocyte globulins)
immunoregulatory agents - immunosuppressive - purified polyclonal Abs (
93
antibodies and biological agents (muromonab)
immunoregulatory agents - immunosuppressive - murine mAbs, for the depletion of human T cells. Used in autoimmune disorders and renal, cardiac and hepatic transplant patients, and depletion of T cells from the donor bone marrow.
• Adverse effects: “cytokine release syndrome” (cytokine storm: release of TNF
94
antibodies and biological agents (intravenous immunoglobulins (IVIg))
immunoregulatory agents - immunostimulatory - ): the IV use of polyclonal human Ig (usually prepared as IgG) pooled from thousands of healthy human donors, for treatment of Ig deficiencies, AIDS, autoimmune disorders, and bone marrow transplants.
95
antibodies and biological agents (hyperimmune immunoglobulins)
immunoregulatory agents - immunostimulatory - IV Ig with high titers of Abs against particular agents of interest such as viruses or toxins. Various hyperimmune IVIgs are available for respiratory syncytial virus, cytomegalovirus, varicella zoster, human herpes virus 3, HBV, rabies, tetanus, and digoxin overdose.
96
antibodies and biological agents (omalizumab)
immunoregulatory agents - immunosuppressive - anti-IgE recombinant humanized
mAb blocking the binding of IgE to Fc
97
antibodies and biological agents (IL-2 receptor antagonis) (basiliximab, daclizumab)
immunoregulatory agents - immunosuppressive - o Are used for prophylaxis of acute organ rejection in adult patients.
98
antibodies and biological agents (anti-TNF reagent) (infliximab)
immunoregulatory agents - immunosuppressive - , is a chimeric humanized anti-TNF
99
antibodies and biological agents (LFA-1 inhibition (efalizumab))
immunoregulatory agents - immunosuppressive - efalizumab, is a humanized IgG1 mAb against LFA-1 (lymphocyte function associated antigen- 1), blocks LFA-1
100
antibodies and biological agents (TNF alpha antagonists (TNF alpha blockers))(infliximab, adalimumab, etanercept)
Infliximab:
• – chimeric and humanized antibody (Ab)
• Adalimumab:
• – Humanized Ab
• Etanercept:
• – fusion protein comprising part of TNF p75 receptor and the Fc portion of human IgG. It binds to TNF
101
Anakinra
* IsarecombinantformofIL-1receptorantagonist (IL-1Ra), which differs from the natural protein by a single methionine residue at its amino terminus.
* Clinicalusesandadverseeffects:similartothe TNF
102
Interferon (alpha-2 beta)
immunoregulatory agents - immunostimulatory - • Clinical uses: to treat infections, immunodeficiency, and cancer.
• Recombinant cytokines: IFNs, IL-2, CSFs.
• Vaccines (active immunization).
• Immune globulins (passive immunization).
Interferons (IFNs)
• Bind to cell surface receptors that initiate a series of intracellular events: induction of certain enzymes, inhibition of cell proliferation, and enhancement of immune activities, including increase phagocytosis by macrophages and augmentation of specific cytotoxicity by T lymphocytes.
for treatment of tumors, AIDS, and chronic hepatitis B infections.
103
Interferon (alpha - 1beta)
immunoregulatory agents - immunostimulatory - • Clinical uses: to treat infections, immunodeficiency, and cancer.
• Recombinant cytokines: IFNs, IL-2, CSFs.
• Vaccines (active immunization).
• Immune globulins (passive immunization).
Interferons (IFNs)
• Bind to cell surface receptors that initiate a series of intracellular events: induction of certain enzymes, inhibition of cell proliferation, and enhancement of immune activities, including increase phagocytosis by macrophages and augmentation of specific cytotoxicity by T lymphocytes.
for treatment of chronic granulomatous disease to activate phagocytes and induce their generation of oxygen metabolites.
104
interferon - 1a and interon alpha - 1beta
areapprovedforthe treatment of relapsing multiple sclerosis.
These last two are both immunomudulatory and immunosuppressive
105
interleukin - 2 (IL-2)
immunoregulatory agents - immunostimulatory - Its in vivo actions:
• - Enhancement of cellular immunity (IL-2 promotes proliferation and differentiation of lymphocytes into CTLs and activation of NK cells).
- Lymphocytosis, eosinophilia, and thrombocytopenia.
• - Release of multiple cytokines (e.g., TNF, IL-1 and IFN-
106
Colony stimulating factors (CSFs)
immunoregulatory agents - immunostimulatory agents - • Granulocyte-CSF (G-CSF) stimulates the production of neutrophils.
• Granulocyte-macrophage CSF (GM- CSF) stimulates production of granulocytes, platelets, erythrocytes, eosinophils and macrophages.
