Term
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Definition
5-fluorouracil
Azathioprine
Cytarabine
Methotrexate |
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Term
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Definition
PYRIMIDINE ANTIMETABOLITE
MOA: pyrimidine analogue; thymidylate synthase inhibitor
INDICATION: GI carcinoma, breast, ovarian, bladder, & prostate cancers
PHARM EFFECTS: prevents synthesis of thymine --> prevents DNA synthesis
ADVERSE EFECTS: continuous infusion --> mucositis; IV bolus --> bone marrow suppression |
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Term
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Definition
PYRIMIDINE ANTIMETABOLITE
MOA: inhibits DNA polymerase activity by incorporation into DNA
INDICATION: AML
ADVERSE EFECTS: myelosuppression, severe nausea & vomiting, severe diarrhea, cerebellar toxicity |
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Term
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Definition
azathioprine (Imuran)
mercaptopurine
thioguanine
MOA: affects incorporations of purine derivatives into nucleic acids
INDICATION: leukemias, severe RA; general immunosuppression
PHARM EFFECTS: inhibition of DNA & RNA synthesis
ADVERSE EFECTS: myelosuppression, pulmonary fibrosis, pancreatitis |
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Term
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Definition
FOLIC ACID ANTIMETABOLITE
MOA: inhibitor of dihydrofolate reductase
INDICATION: leukemia, lymphoma, sarcoma, testicular tumors, carcinoma of the breast and lung, allogenic bone marrow transplants to prevent GVH, steroid-dependent asthma, RA
PHARM EFFECTS: arrests cells in S-phase of cell cycle
ADVERSE EFECTS: bone marrow depression with secondary infection and hemorrhage, painful stomatitis w/ mucosal & epithelia ulceration, pharyngitis & dysphagia, esophagitis, gastroenterocolitis, procitis w/ watery & bloody diarrhea
CONTRAINDICATIONS: NSAIDs increase methotrexate's nephrotoxicity
NOTES: in acute high-dose therapy, leucovorin is administered 24 h after methotrexate infusion to "rescue" healthy cells from methotrexate while not rescuing malignant cells |
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Term
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Definition
FOLIC ACID ANTIMETABOLITE
MOA: inhibits thymidylate synthase, dihydrofolate reductase, & glycinamide ribonucleotide formyltransferase (GARFT)
INDICATION: combine w/ cisplatin --> first line treatment of non-small cell lung carcinoma
ADVERSE EFECTS: oral mucositis, leukopenia, nausea & vomiting, skin rash
NOTES: take folic acid & B12 to reduce frequency of adverse effects, dexamethasone is used to prevent skin rash |
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Term
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Definition
PROTEIN KINASE INHIBITOR
MOA: tyrosine kinase inhibitor
INDICATION: cancers which have tyrosine kinase locked into active position
PHARM EFFECTS: tyrosine kinase is responsible for cell differentiation and division; inhibition --> arrested cancer |
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Term
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Definition
Natural product
MOA: DNA scission & fragmentation, inhibition of DNA repair mechanisms
INDICATION: squamous cell carcinoma, testicular tumors & lymphomas
ADVERSE EFECTS: pulmonary fibrosis which can progress to fatal pulmonary insufficiency
NOTES: toxicity associated w/ total dose of > 400 U, age > 70 yrs, underlying pulmonary disease, & high oxygen exposure |
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Term
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Definition
MOA: binds to tubulin & interferes w/ its function
INDICATION: Hodgkin's lymphoma and other lymphomas
PHARM EFFECTS: arrests cell division by hampering formation of mitotic spindle apparatus
ADVERSE EFECTS: leukopenia, GI disturbances w/ nausea & vomiting, diarrhea, anorexia |
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Term
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Definition
MOA: intercalate into DNA between adjacent guanine-cytosine base pairs & inhibit RNA synthesis
INDICATION: leukemia, pediatric tumors, Ewing's sarcoma, rhadbomyosarcoma, testicular carcinoma, breast & ovarian cancer, Kaposi's sarcoma |
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Term
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Definition
MOA: monoclonal antibody to the protein encoded by HER2 gene (cancer cells express this protein in order to metastasize)
INDICATION:
PHARM EFFECTS: induces cellular toxicity & inhibits angiogenesis
NOTES: decreases rates of cancer recurrence by 50% |
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Term
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Definition
MOA: monoclonal antibody to VEGF
PHARM EFFECTS: prevents interaction of VEGF w/ its receptors --> increases vascular permeability --> increases drug delivery to tumors |
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Term
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Definition
MOA: aromatase inhibitor
PHARM EFFECTS: inhibits estrogen synthesis |
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Term
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Definition
MOA: selective estrogen receptor modulator
NOTES: risk of uterine cancer due to agonist activity in endometrial tissue |
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Term
| alginic acid (Alka-Seltzer) |
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Definition
MOA: alginic acid reacts with sodium bicarbonate present in saliva to form sodium alginate
PHARM EFFECTS: viscous gel floats on the surface of gastric contents (and makes an excellent impression of your last meal), thereby physically preventing reflux into the esophagus |
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Term
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Definition
MOA: anionic surfactant (detergent) which lowers the surface tension of the feces, thereby allowing water in the intestines to penetrate and soften
INDICATION: constipation, post-MI |
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Term
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Definition
Stimulant Laxative
Increase mucosal permeability, resulting in movement of fluid across the intestinal lumen
Effect obtained in 6-8 hrs
Adverse Effects: diarrhea, dependence |
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Term
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Definition
CHLORIDE CHANNEL ACTIVATOR
Fatty acid derived form PGE1
Indications: Chronic Idiopathic Constipation, Irritable Bowel Syndrome with Constipation
Mechanism of action:
Activates Chloride channel protein-2 (ClC-2). chloride channel in the membrane of the human intestine
A chloride-rich intestinal fluid secretion
By increasing intestinal fluid secretion, lubiprostone increases motility in the intestine |
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Term
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Definition
-hydrated magnesium aluminum silicate
-crystalline structure
-Absorbs 8 times of its weight in water |
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Term
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Definition
MOA: blocks the action of acetylcholine at parasympathetic sites in smooth mm., secretory glands, & CNS
INDICATION: irritable bowel syndrome |
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Term
diphenoxylate (Lomotil)
loperamid (Imodium D) |
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Definition
MOA: alters motor function in the intestine
PHARM EFFECTS: delays passage of fluid
ADVERSE EFECTS: drowsiness, dry mouth, gingival swelling
NOTES:loperamide has fewer adverse effects than diphenoxylate because it doesn't penetrate the BBB
overdose symptoms are similar to opiates: respiratory depression, unconsciousness
schedule 5 |
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Term
| Drugs ending in "ovir" are |
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Definition
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Term
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Definition
-Guanosine analog, 2 carbon atoms missing from ribose, no –OH for polymerase rxn
-Selective phosphorylation:
Basis for selectivity of drug for virus infected cells
3000 fold greater concentration required to inhibit non-infected cell growth (in vitro therapeutic index) |
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Term
| Acyclovir usage and dosage |
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Definition
Ointment: Symptomatic relief of recurrent herpes (simplex) labialis
Oral
Prophylaxis and treatment primary and recurrent of genital herpes
Preventing reactivation in immunosuppressed patients
Bioavailability: 20 %, dose is 200 mg 5 x’s/day |
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Term
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Definition
2G q12h
has a greater bioavailability than acyclovir |
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Term
| Penciclovir (Denavir) Cream |
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Definition
-Inhibits HSV polymerase competitively with deoxyguanosine triphosphate
-Indicated for HSV-1 and HSV-2
-Off-label varicella-zoster
Dose: Apply every 2 hours while awake for 4 days. Treatment should be started as early as possible (during prodrome phase)
½ day shorter duration of disease |
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Term
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Definition
Same specificity for viral thymidine kinase (always IV)
Inhibits viral DNA polymerase
Used for acyclovir resistant HSV infections
Adverse effects: aspermatogenesis, carcinogenic and teratogenic |
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Term
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Definition
oral form (prodrug) of Ganciclovir
900 mg once daily with food
More potent than acyclovir against HSV, CMV and VZV |
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Term
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Definition
Over the counter so you can recommend
MOA: inhibits fusion between the human cell membrane and HSV— Prohibits entry into human cell
Directions for use: apply 5 x’s/day starting at the early stage (redness) to stop progressing to the blister stage
One day shorter
Use a maximum of 10 days |
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Term
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Definition
Prevents the release of infectious viral nucleic acid into the host cell
Interferes with the influx of protons through a transmembrane domain of the viral M2 protein
Reduces infection rates by 50 % and illness rates by 60 %
CNS depression |
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Term
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Definition
Low pH in viral envelop triggers fusion
Blocks ion channel function
Inhibits acidification and un-coating |
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Term
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Definition
Neuraminidase inhibitor:
present on the surface of influenza virus particles
enables the virus to separate itself from cells
Uses:
uncomplicated acute illness due to influenza A and B virus
adults and pediatric patients 1 year of age and older
symptomatic for no more than 2 days
Prophylaxis
Not Recommended with underlying airway disease (asthma or COPD) |
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Term
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Definition
CCR5 Antagonist
Selectively and reversibly binds to the CCR5 co-receptor located on human CD4 cells
Prevents interaction between the human CCR5 co-receptor and the gp120 subunit of the viral envelope glycoprotein
Inhibits gp120 conformational change required for CCR5 HIV-1 fusion with the CD4 cell and subsequent cell entry |
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Term
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Definition
entry inhibitor
Gp41 initiates fusion of the virus into the lymphocyte cell surface
Binds to the first heptad repeat in the gp41 subunit of the viral glycoprotein
Prevents conformational changes and formation of entry pore
Evidence of HIV-1 replication despite ongoing antiretroviral therapy
Resistance: Substitutions in the aa’s in the gp41 protein |
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Term
| Efavirenz and Zidovudine (AZT) are: |
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Definition
NRTI
Nucleoside reverse transcriptase inhibitor. |
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Term
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Definition
Protease inhibitors
Inhibit the HIV protease enzyme
Cuts proteins into usable portions to make new functional virions
Uncut proteins means that the virions leave the cells without the ability to infect other cells
Combination therapy
Many are given with a low dose of another PI (Ritonavir, Norvir) |
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Term
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Definition
strong inhibition of CYP3A4
Used in small doses (100 mg) to “boost” other Pis
Inhibits their metabolism
Other Pis can be given in higher concentrations for longer period of time |
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Term
| Saquinavir drug interactions |
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Definition
increases blood levels of: Diazepam (Valium), Alprazolam (Xanax)
Triazolam (Halcion) and Midazolam (Versed) are contraindicated
Inhibitors: Fluconazole, Itraconazole, Ketoconazole,
Increase Saquinavir blood levels |
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Term
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Definition
integrase inhibitor and integrase
Integrase:
Creates available ends on viral DNA
Splices viral DNA into the host DNA inside the nucleus |
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Term
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Definition
Victrelis (boceprevir)
Incivek (telaprevir)
Protease inhibitors
1st drugs to work directly on the hepatitis C virus |
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Term
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Definition
Polyene
MOA: Binds to cell membrane ergosterol
Forms pores leading to K+ leakage and cell death |
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Term
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Definition
Oral Suspension 100,000 u/mL: 5mL S and S 5x/day
Lozenges 200,000 units: Dissolve completely in mouth (do not chew or swallow whole) 5x/day
NPO ½ hour after use
Both treatments usually last 14 days
-Patients say it has a bitter, foul taste
-Continue 48 hrs after symptoms disappear
Patients with liver disease or alcoholism: Nystatin is the drug of choice |
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Term
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Definition
Imidazole
Can be used topically (cream 2 %) or orally (tablets 200 mg)
Well absorbed from the GI tract in conditions of low pH
Drug interaction with drugs that increase the pH of the stomach
Dose: 1 tab qd with orange juice or a meal for 14 days
Adverse Effects: hepatoxicity (0.01 %)
Inhibits synthesis of testosterone and estradiol
Inhibitor of Cytochrome p450 3A4:
Cyclosporin
Phenytoin
Sulfonylureas
Warfarin |
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Term
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Definition
Nitrogen atoms of the azole ring bind to lanosterol 14α-sterol demethylase (fungal cytochrome p450 enzyme)
The conversion of lanosterol to ergosterol is inhibited
Ergosterol is part of the cell membrane
Imidazole antifungals primarily used for simple candidiasis. |
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Term
| Clotrimazole Troches 10 mg |
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Definition
Imidazole
Dissolve completely in mouth (do not chew or swallow whole) 5 times per day
NPO ½ hour after use
Only used topically because not absorbed from the GI tract
Binds to the oral mucosa, gradually released, fungistatic concentrations for several hours
Patients report that it tastes better than nystatin |
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Term
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Definition
A triazole derivative: more selective inhibitor of fungal cell membrane 14a-sterol demethylase
Adverse Effects: GI upset, less hepatoxicity than ketoconazole
Weak inhibitor of p450 3A4: fewer drug interactions
Uses: Candidemia, osteomyelitis, meningitis (IV)
Therapy for 3-6 months
Life long in HIV patients
Prophylaxis in bond marrow transplant |
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Term
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Definition
Tablets 100 mg
2 tabs stat, then 1 qd for 13 days
Suspension 50 mg/5 mL
Rinse mouth with 20 mL on day 1 for 1 minute then swallow. Repeat with 10 mL qd for 14 days total |
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Term
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Definition
Triazole, mechanism like fluconazole
-If infection is resistant to nystatin, ketoconazole, fluconazole
-Resistance in Candida species isolated from patients on prolonged therapy
-Significant inhibitor of p450 3A4 |
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Term
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Definition
Dosage forms are capsules 100 mg and suspension 10 mg/mL
Take 1 capsule bid
Rinse mouth with 20 mL for 1 minute qd then swallow and continue for 14 days |
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Term
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Definition
Halogenated hydroxyquinoline with amebicidal, antitrichomonal, antibacterial and antifungal activity
-Chelates trace metals at bacterial surfaces that are essential for growth
-Indications: angular cheilitis
-Dosage forms: 1 % topical cream with 1 % hydrocortisone
Apply to affected areas after each meal and hs (bedtime) |
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Term
| Antifungal treatment in immunocompetent patient |
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Definition
Clotrimazole Lozenges 10 mg
Nystatin Lozenges 200,000 units
Dissolve slowly in mouth (do not chew or swallow whole) 5 times per day
NPO ½ hour after use
Fluconazole tablets 150 mg
Take one tablet po stat |
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Term
| Antifungal treatment in immunocompromised patients or Mucocutaneous Candidiasis |
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Definition
Fluconazole Oral Suspension 50 mg/5 mL
Itraconazole Oral Suspension 10 mg/ mL
Rinse mouth with 20 mL for 1 minute then swallow qd and continue for 14 days
Fluconazole tablets 100 mg
Take 2 tablets stat, then 1 tablet qd for 13 days |
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Term
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Definition
ends in "fungin"
inhibitors of fungal cell wall synthesis.
Inhibition of glucan synthase
Enzyme is present in fungal cells not mammalian cells
Inhibit synthesis of 1,3-β-D-glucan
Essential component of fungal cell walls
Candidemia, invasive aspergillus, candida abscesses, deep tissue infections, refractory or invasive infections |
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Term
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Definition
| Newer triazole antifungals |
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