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274 Cards in this Set
- Front
- Back
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What is the overall 5 year survival rate for cancer
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40%
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Describe the TNM Staging classification system
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T: The size of the primary tumor
N: The extent of regional lymph node spread M: The presence of metastatic spread to distant organs |
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What is the aim of anti cancer drugs
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To cause a lethal cytotoxic event in the cancer cell that can arrest a tumor’s progression.
The attack is generally directed against metabolic sites essential to cell replication (Example: The availability of purines and pyrimidines that are the building blocks for DNA or RNA synthesis) |
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Are anticancer drugs generally specific to recognize neoplastic cells
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No
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If the drugs cannot provide a long term remission then what do the drugs aim to do against cancer
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provide palliative care
(alleviation of symptoms and avoidance of life-threatening toxicity) |
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What is anticancer adjuvant care
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given in addition to surgical therapy, in order to reduce the risk of local or systemic relapse.
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What is anticancer combination care
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Using more than a single drug to exploit the varying levels of toxicity for the patient’s benefit. (Some combinations of anticancer drugs also appear to exert true synergism, wherein the effect of the two drugs is greater than the additive effect of both.)
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What kind of drug therapy is most effective in chemotherapy
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Combination-drug chemotherapy is more successful than single-drug treatment in most of the cancers for which chemotherapy is effective
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What cellular system leads to resistance against chemotherapy
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P-glycoprotein pump
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What normal body cells undergoe rapid proliferation and are thus prone to toxicity in chemotherapy
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cells of the buccal mucosa, bone marrow, gastrointestinal mucosa, and hair
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What is a problem with chemotherapy alkylating agents
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Treatment induced neoplasms
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What do chemotherapy antimetabolites interfere with
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availability of normal purine or pyrimidine nucleotide precursors by inhibiting their synthesis, or
competing with them in DNA or RNA synthesis |
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What is Methotrexate (MTX)
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a folic acid analog that acts to be an antagonist to it and prevent it from converting to its active form. This prevents growth of rapidly developing cells
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Methotrixate (MTX) inhibits what particular enzyme
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dihydrofolate reductase, DHF Reductase, the enzyme responsible for converting folic acid (folate) to reduced (active) folate cofactors (i.e., tetrahydrofolate, FH4 or THFA).
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What is the normal dosing regimen of MTX
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P.O. taken once a week, at 12-hr intervals
5mg dose- 25mg Giving this everyday will cause death |
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What the different indications for MTX
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PO: Psoriasis, R.A.
IV: Cancer |
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What does Flourounacil (5-FU) inhibit
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antimetabolite that interferes with thymidylate synthetase (TS)
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generic of Leucovorin Calcium
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Folinic Acid
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Name Brand of Folinic Acid
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Leucovorin Calcium
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What does Folinic Acid (Leucovorin Calcium) do
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counteracts the therapeutic and toxic effects of folic acid antagonists, such as MTX
given with high dose MTX restores body ability to make the red and white blood cells selective for only normal cells not cancer cells |
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Generic of Purinethol
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6-Mercaptopurine
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Brand Name of 6-Mercaptopurine
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Purinethol 6-MP
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What is Purinethol; 6-MP used for in cancer treatment
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maintenance of remission in acute lymphoblastic leukemia
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What treatment are 6-MP and its analog, azathioprine used for
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Crohn's disease
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What is the mechanism of action for 6-MP
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Prevention of Nucleotide formation
Inhibition of Purine Synthesis Incorporation into nucleic acids |
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What is the result of 6-MP being incorporated into nucleic acids
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nonfunctional RNA and DNA
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What causes resistance to 6-MP
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Lack of enzyme that transforms 6-MP to corresponding nucleotide
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What enzyme catalyzes 6-MP
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Xanthine oxidase
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What drug is a xanthine oxidase inhibitor
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Allopurinol
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What adjustments to 6-MP must be made if a patient is on the xanthine oxidase inhibitor -allopurinol
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6-MP must be decreased by 75% to avoid accumulation of the drug and exacerbation of toxicities
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What is the Mechanism of action for 5-Fluorouacil
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Acts as an antimetabolite.
It interferes with DNA synthesis by inhibiting thymidylate synthetase (TS), the enzyme that catalyzes the methylation of deoxyuridylic acid (dUMP) to deoxythymidylic acid (dTMP), a DNA precursor |
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What chemotherapy treatments is 5-FU primarily used for
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slowly growing solid tumors (for example, colorectal, breast, ovarian, pancreatic, and gastric carcinomas).
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Why is Leucovorin administered with 5-FU
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because the reduced folate coenzyme is required in the thymidylate synthase reaction
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What is 5-FU treatment effective for
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Superficial basal cell carcinomas
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What are the delivery methods for 5-FU
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Because of its severe toxicity to the GI tract, 5-FU is given IV or, in the case of skin cancer, topically
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What are the side effects of 5FU
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nausea, vomiting, diarrhea, and alopecia, severe ulceration of the oral and GI mucosa, bone marrow depression (with bolus injection), and anorexia
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What is the dermopathy that is seen with 5-FU with extended infusions
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erythematous desquamation of the
palms and soles called the “hand-foot syndrome” |
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What is given as a mouthwash to reduce oral toxicity of 5-FU
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Allopurinol
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Brand Name of 1% topical cream Flourouracil
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Fluoroplex
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Generic name of Fluoroplex
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Fluorouracil topical 1% cream
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Brand Name of 5% topical cream Flourouracil
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Efudex
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What is 1% Fluorouracil topical cream (Fluoroplex) given to treat
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Actinic Keratosis
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What is 5% Fluorouracil topical cream (Efudex) given to treat
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Basal Cell Carcinoma
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Generic name of Efudex
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Fluorouracil topical 5% cream
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Brand Name of 0.5% topical cream Flourouracil
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Carac
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Generic name of Carac
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Fluorouracil topical 0.5% cream
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When applying any fluorouracil cream what precaution must you take
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Avoid eyes
Avoid Sun (will cause blisters) |
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What are the mechanisms of action for Anti-tumor Antibiotics
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The get into the DNA and block the kalemic effect and are cytotoxic
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What are the 4 examples of antitumor antibiotics given in class
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Dactinomycin: Bone marrow suppression
Doxorubicin: Irreversible cardiotoxicity Daunorubicin: Irreversible cardiotoxicity Bleomycin: Pulmonary (the most free radicals produced) |
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What are the mechanisms of action for Alkylating Agents
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cross-linkages between guanine residues in the DNA chains and/or depurination, thus facilitating DNA strand breakage.
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Brand name of Mechlorethamine
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Mustargen
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Generic name of Mustargen
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Mechlorethamine
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What is Mechlorethamine (Mustargen) used for
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Hodgkins Disease
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What is the brand name of Cyclophosphamide
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Cytoxan
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Generic of Cytoxan
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Cyclophosphamide
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What is the mechanism of action for Cyclophosphamide (Cytoxan)
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alkylates or binds with many intracellular molecular structures, including nucleic acids.
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What are the adverse effects of Cyclophosphamide Cytoxan
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Hemorrhagic Cystitis
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Brand Name of Ifosamide
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Ifex
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Generic name of Ifex
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Ifosamide
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What is Ifosamide (Ifex)
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Synthetic analog of cyclphosphamide
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What product is given to decrease the toxic effect of hemorrhagic cystitis
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MESNA (sodium 2-mercaptoethane sulfonate)
Remember that in the hospital, when Cytoxan is given IV, MESNA is given IV to inactivate the toxic metabolite from the drug’s metabolism, and minimizes the bladder problem. It binds to the toxic product |
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What is the brand name of Chlorambucil
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Leukeran
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What is the generic name of Leukeran
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Chlorambucil
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What is the brand name of Melphalan
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Alkeran
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What is the generic name of Alkeran
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Melphalan
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What is Chlorambucil (Leukeran) used to treat
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multiple myeloma
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What is Melphalan (Alkeran) used to treat
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chronic lymphocytic leukemia
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What is the initial dose for Chlorambucil (Leukeran)
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0.1 to 0.2 mg/kg/day. (Average 4 to 10 mg PO/day)
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What two medications are referred to as vinca alkaloids
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Vincristine (ONCOVIN) and vinblastine (VELBAN)
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what type of medication are the vinca alkaloids
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Spindle Poisons-Their binding to the microtubular protein, tubulin, is GTP–dependent and blocks the ability of tubulin to polymerize to form microtubules.
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What two drugs are a part of the taxane family
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Paclitaxel (Taxol)
docetaxel (TAXOTERE), which is the more potent of the two drugs. |
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What types of cancers are paclitaxel indicated for
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advanced ovarian cancer metastatic breast cancer
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What are contraindications for taxane drugs
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Neutropenia
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What are patients with paclitaxel premedicated with
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dexamethasone and diphenhydramine as wellas an H2 blocker
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what other steroid does prednisone mimic
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Cortisol
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What type of steroid is prednisone
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Glucocorticoid
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What is the active form of prednisone
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prednisolone
This must be given to children bc they lack the converting enzymes |
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What are the adverse effects of prednisone
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It can predispose to infection (due to its immunosuppressant action) and to stomach ulcers and pancreatitis.
Other effects include hyperglycemia, cataract formation, glaucoma, osteoporosis, and change in mood (euphoria or psychosis) The drug prevents calcium uptake |
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how must high dose steroids be stopped
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High doses should be tapered down
The ACTH will decrease if high dose steroids given and then suddenly taken away The result will be addisons disease which can lead to death |
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What is a steroid psychosis of prednisone
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Acting in a manic way
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brand name of Tamoxifen
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Nolvadex
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generic name of Nolvadex
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Tamoxifen
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What is Tamoxifen (Nolvadex)
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Estrogen Receptor Blocker
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What is Tamoxifen (Nolvadex) used for
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Tx of estrogen receptor–positive breast cancer.
It also finds use prophylactically in reducing breast cancer in women who are at high risk. |
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What are the side effects of Tamoxifen (Nolvadox)
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Those similar to estrogen
Hot flashes, nausea, vomiting, skin rash, vaginal bleeding, and discharge |
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What Toxicities can Tamoxifen cause
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It can also lead to increased pain if the tumor has metastasized to bone.
It has the potential to cause endometrial cancer. Other toxicities include thromboembolism and effects on vision. |
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What drug cannot be given with tamoxifen
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Estrogens from hormone replacement products (Premarin)- cancellation of effect
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What drugs are being used before tamoxifen because they are more safe
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Aromatase inhibitors
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What is the generic of Arimidex
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Anastrozole
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What is the brand name of Anastrozole
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Arimidex
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What is the generic of Femara
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Letrozole
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What is the brand name of Letrozole
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Femara
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What are non steroidal aromatase inhibitors used for
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second-line therapy after tamoxifen for hormone-dependent breast cancer
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Brand name of Megestrol Acetate
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Megace
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Generic name of megace
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Megestrol Acetate
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what is Megace used to treat
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Last line type drug for breast cancer
Weight Gain stimulant |
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When should Megace ES be prescribed
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very expensive and shouldn’t be prescribed unless you have to
most insurance companies dont cover it |
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What is the mechanism of action for Leuprolide (Lupron)
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As GnRH agonist, it occupies the GnRH receptor in the pituitary.This leads to its desensitization & inhibition of release of FSH and LH. Both androgen and estrogen syntheses are reduced
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Brand name of Leuprolide
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Lupron
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Generic name of Lupron
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Leuprolide
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What treatments are Lupron and Leuprolide used for
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endometriosis, Breast Cancer, Prostate Cancer
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What is Goserelin
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Goserelin acetate is similar to lupron that is implanted intramuscularly to treat prostate cancer
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What are the adverse effects of Leuprolide (Lupron)
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impotence (similar to chemical castruation), hot flashes, and tumor flare, are minimal compared to those experienced with estrogen treatment
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name brand of Flutamide
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Eulexin
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generic name of Eulexin
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Flutamide
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Generic of Casodex
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bicalutamide
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Name brand of bicalutamide
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Casodex
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what is Flutamide (EULEXIN) and bicalutamide (CASODEX) used to treat
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prostate cancer- known as “blockers of testosterone target tissue” in prostate cancer
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what is Flutamide (EULEXIN) and bicalutamide (CASODEX) given in conjuction with
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They are always administered in combination with leuprolide or goserelin. (LHRH Agonists)
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what are the side effects of Flutamide (EULEXIN) and bicalutamide (CASODEX)
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gynecomastia and GI distress and, in the case of Flutamide, liver failure
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Brand Name of Leucovorin Calcium
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Folinic Acid
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Generic name of Folinic Acid
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Leucovorin Calcium
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What is Leucovorin Calcium given for
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Antidote (to folic acid antagonists) it rescues bone marrow and gastrointestinal cells from MTX.
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When prescribing Leucovorin what must you do
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Use the full official name to avoid confusion with Leukeran or folic acid
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Brand name of Azathioprine
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Imuran
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Generic Name of Imuran
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Azathioprine
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What is Azathioprine (Imuran) used for
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immunosuppression of rheumatoid arthritis and other immunologic diseases
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If given with Allopurinol, what should the dose of Imuran be
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decrease dose of Imuran by ¾, or 75%)
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Brand Name of Mycophenolate
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Cellcept
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Generic of Cellcept
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Mycophenolate
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What are the uses of Mycophenolate (Cellcept)
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Prophylaxis of organ rejection in allogenic renal, cardiac, or hepatic transplants
Other uses: psoriasis, rheumatoid arthritis, myasthenia gravis, and lupus erythematosus |
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Why is Cellcept used more often than Imuran
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less suppression of other bone marrow elements than does Imuran
Also, there is no dose adjustment with CellCept as there is with Imuran (Azathioprine) when allopurinol is used. |
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What does Cellcept work on
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lymphocytes- It inhibits the formation of cytotoxic T lymphocytes.
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What medications must not be given simultaneously with Cellcept
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Antacids and cholestyramine
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What adverse effects does Cellcept have
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Increased susceptibility to infection
and possible development of lymphoma. Fetal damage has been reported |
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what 2 conditions does COPD usually refer to?
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Chronic Bronchitis
Emphysema |
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What is asthma?
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Asthma is a disease of diffuse airway inflammation caused by a variety of triggering stimuli resulting in partially or completely reversible bronchoconstriction. Symptoms and signs include dyspnea, chest tightness, and wheezing. The diagnosis is based on history, physical examination, and pulmonary function tests. Treatment involves controlling triggering factors and drug therapy, most commonly with inhaled beta agonists and inhaled corticosteroids. Prognosis is good with treatment. It can exist in the same patient with COPD
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What is chronic bronchitis?
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A condition of the bronchial tree characterized by cough, hypersecretion of mucus, and expectoration of sputum over a long period of time, associated with frequent bronchial infections
Usually due to inhalation, over a prolonged period, of air contaminated by dust or by noxious gases of combustion (smoking) |
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What is emphysema?
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A condition of the lung characterized by an increase beyond the normal in the size of air spaces distal to the terminal bronchiole (those parts containing alveoli), with destructive changes in their walls and reduction in their number.
Clinical manifestation is breathlessness on exertion, due to the combined effect (in varying degrees) of reduction of alveolar surface for gas exchange and collapse of smaller airways with trapping of alveolar gas in expiration; this causes the chest to be held in the position of inspiration (“barrel chest”), with prolonged expiration and increased residual volume. |
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What is the 4th most common cause of preventable death?
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COPD
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How does allergic rhinits present?
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characterized by itchy, watery eyes, runny nose, and a nonproductive cough
-an extremely common condition which significantly decreases quality of life. |
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Which delivery method of drug is preferred for respiratory disease?
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Topical
delivery methods, such as nasal sprays or inhalers, are preferred so as to target affected tissues while minimizing systemic side effects. |
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What are the common routes for drug administration in respiratory disease?
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Topical
Orally Parenterally |
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what is the most commonly prescribed rescue inhaler available?
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albuterol, a selective beta-2 agonist.
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How is asthma unlike chronic bronchitis, cystic fibrosis, or bronchiectasis?
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asthma is usually not a progressive disease
It does not inevitably lead to crippled airways Asthma is a chronic disease with an underlying inflammatory pathophysiology which, if untreated, might involve airway remodeling resulting in increased severity and incidence of exacerbations and/or death. |
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How is airflow obstructed in asthma?
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-Due to bronchoconstriction that results from contraction of bronchial smooth muscle
-Inflammation of the bronchial wall -Increased mucous secretion. |
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How are asthma attacks precipitated?
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may be related to recent exposure to allergens or inhaled irritants, leading to bronchial hyperactivity and inflammation of the airway mucosa.
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Is asthma curable?
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The symptoms of asthma may be effectively treated by several drugs, but no agent provides a cure for
this obstructive lung disease. |
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What is the role of phenotype in asthma?
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Recent research demonstrates a link between ß receptor polymorphism (phenotype) and response to long-acting ß2-agonists
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What are the drugs of choice for mild asthma?
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Inhaled adrenergic agonists with beta-2 activity
These are the “rescue” inhalers |
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How long do the quick-acting rescue inhalers work?
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Most clinically useful beta-2 agonists have a rapid onset of action (five to thirty minutes) and provide relief for four to six hours.
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What signs and symptoms would alert the care giver to asthma that is not well controlled?
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Regardless of the severity of the asthma, the frequent need for a rescue beta-2 agonist indicates that the asthma is not well-controlled.
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What is the drug of choice for acute anaphylaxis?
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Epinephrine
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Would beta-2 agonists be used to treat anaphylaxis?
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Beta-2 agonists have no anti-inflammatory effects, and they should never be used as the sole therapeutic agents for patients with persistent asthma.
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What are pirbuterol, terbutaline, and albuterol examples of?
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direct-acting beta-2 selective agonists provide maximally attainable bronchodilation with little of the undesired effect of alpha or beta-1 stimulation.
Terbutaline is mainly used in the hospital by injection. |
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Are beta-2 agonists catecholamines?
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No, they are not activated by COMT
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What are adverse effects of beta-2 agonists?
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tachycardia, hyperglycemia, hypokalemia, & hypomagnesemia
These AEs are minimized with dosing via inhalation versus systemic routes |
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Salmeterol Xinafoate is aka
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Serevent
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serevent is aka
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salmeterol xinfoate
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What are LABAs?
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long acting beta-2-adrenergic bronchodilators. LAßAs
serevent and formoterol |
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Formoterol is aka?
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Foradil
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Foradil is aka
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formoterol
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How long do LABAs last?
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at least 12 hrs
They are chemical analogs of albuterol but differ by having a lipophilic side chain, increasing the affinity of the drug for the beta-2 adrenoceptor. |
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What is the boxed warning for LABAs?
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Long-acting beta-2 agonists may increase the risk of asthma-related death.
Use only as add-on therapy Due to them being used as a rescue inhaler and having a slow onset of action. |
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What are the adverse effects of LABAs?
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Similar to Beta-2 agonists
tachycardia, hyperglycemia, hypokalemia, & hypomagnesemia |
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What is status asthmaticus and how do we treat it?
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severe exacerbation of asthma
may require intravenous administration of methylprednisolone (MEDROL), or oral prednisone as well as Beta-2 agonist inhaled. |
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Is a tapering dose reduction needed in an acute asthma exacerbation?
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In most cases, suppression of the hypothalamic-pituitary axis (HPA) will not occur during the short course of oral prednisone “burst” typically prescribed for an asthma exacerbation therefore dose reduction is not necessary.
Care is needed in patients who are transferred from systemically active corticosteroids (example: Prednisone 20mg PO/day) to corticosteroid inhalation aerosol. |
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What do long-term steroids do systemically?
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Exogenous corticosteroid therapy suppresses production of corticotropin-releasing hormone and corticotropin and may lead to adrenal atrophy.
Some degree of adrenal suppression should be anticipated in individuals who receive more than 30 mg of hydrocortisone or 7.5 mg of prednisone (the average daily equivalent output of the adrenal glands) for more than three weeks. Risk of disease flare after short-course treatment probably related to treatment duration and specific disease. |
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What are the first choice drugs for persistent asthma?
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Inhaled corticosteroids (ICS)
No other medications are as effective as ICS in the long-term control of asthma in children and adults. If appropriately prescribed and used, ICS therapy may reduce or eliminate the need for oral glucocorticoids in patients with severe asthma. To be effective in controlling inflammation, glucocorticoids must be taken continuously. |
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How do ICS acton on lungs?
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ICS therapy directly targets underlying airway inflammation by decreasing the inflammatory cascade (eosinophils, macrophages, and T lymphocytes), reversing mucosal edema, decreasing the permeability of capillaries, and inhibiting the release of inflammatory leukotrienes.
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What happens after using ICS for several months?
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After several months of regular use, ICS reduce the hyper-responsiveness of the airway smooth muscle to a variety of bronchoconstrictor stimuli, such as allergens, irritants, cold air, and exercise.
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What are some common misuse patterns with MDI (meter dose inhalers)?
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-Using the inhaler longer than there is medication in the MDI
-Forgeting to shake the MDI before administration -Improper storage of the MDI -Inhaling too quickly (should be slow and deep) |
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How are patients instructed to inhale their DPIs? (dry powder inhalers)
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inhale QUICKLY and DEEPLY to optimize drug delivery to the lungs
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What are adverse effects of ICS in DPI administration?
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Even properly administered, ICS deposition on the oral and laryngeal mucosa can cause adverse effects such as oropharyngeal candidiasis (THRUSH) and hoarseness.
Patient counseling incorporating a rinsing of these tissues via the “swish and spit” method should avoid these adverse events |
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What are spacers and what do they do?
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A large-volume chamber attached to a metered-dose inhaler.
Spacers minimize the problem of adrenal suppression by reducing the amount of glucocorticoid deposited in the oropharynx. Spacers improve delivery of inhaled glucocorticoids and are advised for virtually all patients but especially Spacers decrease the deposition of drug in the mouth caused by improper inhaler technique. The chamber reduces the velocity of the injected aerosol before entering the mouth, allowing large drug particles to be deposited in the device. The smaller, higher-velocity drug particles are less likely to be deposited in the mouth and more likely to reach the target airway tissue. |
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When are spacers contraindicated?
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Children less than five years old and
√ Elderly patients who may have difficulty coordinating actuation with inhalation. |
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What are leuokotrienes?
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Leukotrienes (LTB4, LTC4, LTD4, and LTE4), are products of the 5-lipoxygenase pathway of arachidonic acid metabolism and part of the inflammatory cascade
5-Lipoxygenase is found in cells of myeloid origin, such as mast cells, basophils, eosinophils, and neutrophils LTB4 is a potent chemoattractant for neutrophils and eosinophils Other leukotrienes constrict bronchiolar smooth muscle, increase endothelial permeability, and promote mucus secretion. |
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Zafirlukast is aka?
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Accolate
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Accolate is aka?
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Zafirlukast
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Montelukast is aka?
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Singulair
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Singulair is aka?
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Montelukast
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What is the most common LTRA?
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leukotriene receptor antagonist
Singulair |
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Zileuton is aka?
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Zyflo
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Zyflo is aka?
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Zileuton
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What is the action of zyflo?
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a selective and specific inhibitor of 5-lipoxygenase, preventing the formation of LTs.
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What are important things to know about LTRAs?
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All three drugs are approved for the prophylaxis of asthma but are not effective in situations where immediate bronchodilation is required.
Modest reductions in the doses of beta-2-adrenergic agonists and corticosteroids, as well as improved respiratory function, are among the therapeutic benefits. |
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what is the main function of mast cell stabilizers?
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inhibit the release of inflammatory histamine
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what are the indications of prescribing cromolyn?
|
Pretreatment with cromolyn blocks allergen- and exercise-induced bronchoconstriction.
Cromolyn is also useful in reducing the symptoms of allergic rhinitis. |
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what are adverse effects of cromolyn?
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bitter taste & irritation of the pharynx and larynx
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How often is cromolyn needed throughout a day?
|
Due to short duration of action, these agents require frequent daily dosing which has been shown to affect adherence and therefore therapeutic efficacy.
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What are some properties of anticholinergic agents?
|
Anticholinergic agents are generally less effective than beta 2-adrenergic agonists.
They block the vagally mediated contraction of airway smooth muscle and mucus secretion. useful in patients who are unable to tolerate adrenergic agonists. These agents are not traditionally effective for patients with asthma unless COPD is also present. |
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Which has a slower onset of action and is essentially free of serious side effects, atrovent or albuterol?
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atrovent
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What was the mainstay for asthma therapy before albuterol?
|
Previously the mainstay of asthma therapy, theophylline has been largely replaced with beta-2 agonists and corticosteroids due to a narrow therapeutic window, high side effect profile, and potential for drug interactions.
Overdose may cause seizures or potentially fatal arrhythmias |
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what are properties of theophylline?
|
A bronchodilator that relieves airflow obstruction in chronic asthma and decreases its symptoms.
It is well absorbed by the gastrointestinal tract Sustained-release preparations are available. |
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Omalizumab is aka
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Xolair
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Xolair is aka?
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Omalizumab
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What is xolair?
|
A recombinant DNA-derived monoclonal antibody that binds to human immunoglobulin E (IgE).
Reduction in surface-bound IgE limits the degree of release of mediators of the allergic response. |
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when is xolair indicated?
|
It may be useful for treatment of moderate to severe allergic asthma in patients who are poorly controlled with conventional therapy.
Due to the high cost of the drug, limitations on dosage, it is not presently used as first-line therapy. |
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what is a major advantage of salmeterol and tiotropium?
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less frequent dosing
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when should ICS be restricted to COPD patients?
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FEV1 < 50% of predicted and three or more exacerbations in the last three years.
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What drugs are recommended for COPD?
|
longer acting and less frequent dosing salmeterol and tioptropium
Addition of a long-acting beta 2 agonist improves lung function compared to either a short-acting beta 2-agonist or steroid alone. |
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how is rhinitis precipitated?
|
An attack may be precipitated by inhalation of an allergen (such as dust, pollen, or animal dander).
The foreign material interacts with mast cells coated with IgE generated in response to a previous allergen exposure The mast cells release mediators, such as histamine, leukotrienes, and chemotactic factors, which promote bronchiolar spasm and mucosal thickening from edema and cellular infiltration. |
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what are the first-line therapies for allergic rhinitis?
|
Combinations of oral antihistamines with decongestants
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what are the most frequently used agents in the treatment of sneezing and watery rhinorrhea associated with allergic rhinitis?
|
H1-histamine–receptor blockers, such as diphenhydramine, chlorpheniramine, loratadine, and fexofenadine,
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what are adverse effects of antihistamines?
|
anticholinergic side effects of the first generation antihistamines (dry eyes/mouth, difficulty urinating and/or defecating) are transient and may resolve in seven to ten days
Constipation associated with chronic use of the first generation antihistamines is not transient and may require treatment with a stool softener, especially in more susceptible patients |
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How do alpha agonists work for allergies and why is it important to only administer for a few days?
|
Short acting alpha adrenergic agonists (“nasal decongestants”), constrict dilated arterioles in the nasal mucosa and reduce airway resistance.
When administered as a spray or drop, these drugs have a rapid onset of action Combinations of these agents with antihistamines are frequently used They should be used no longer than several days due to the risk of rebound nasal congestion (rhinitis medicamentosa). |
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what is important advice must be given in nasally inhaled corticosteroid administration?
|
In order to avoid systemic absorption, tell patients NOT to deeply inhale while administering these drugs since the target tissue is in the nose, not in the lungs or the throat.
Treatment of chronic rhinitis may not result in improvement until 1 to 2 weeks after starting therapy |
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When should nasocromolyn be administered for full therapeutic effect?
|
In order to optimize the therapeutic effect of cromolyn, dosing should occur at least 1 to 2 weeks prior to allergen exposure.
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what is the gold standard treatment for cough suppression?
|
codeine due to its long history of availability and use.
It decreases the sensitivity of cough centers in the central nervous system to peripheral stimuli and decreases mucosal secretion. |
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what is better for cough suppression dextromethorphan or codeine?
|
Dextromethorphan has a significantly better side effect profile than codeine and has been shown to be equally effective for cough
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what does HFA stand for and what is it important for?
|
Propellant in rescue inhalers, hydrofluoroalkane (HFA) instead of CFC (chlorofluorocarbons)
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Albuterol is aka
|
PROVENTIL HFA
VENTOLIN HFA PROAIR HFA |
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How does albuterol work in the lungs?
|
Selectively stimulates beta 2 receptors of the smooth muscle in lungs (& other tissues)
This activates second messengers: adenylyl cyclase & ↑ intracellular cAMP Protein kinase A is activated This inhibits phosphorylation of myosin & intracellular ionic Ca2+ → relaxation of smooth muscles from trachea to terminal bronchioles. The result is bronchodilation |
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when is albuterol indicated?
|
Bronchospasm in patients with reversible
obstructive airway disease & to prevent exercise- induced bronchospasm |
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what are side effects of albuterol?
|
Positive chronotropic effect on heart due to direct
sympathetic effects and peripheral vascular dilation with reflex tachycardia * Stimulates skeletal muscle → fine hand tremor (Low dose Lorazepam can help) |
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what is the caution about albuterol syrup?
|
potential risk of syncope
The child is sensitive to the vasodilating effects and skeletal muscle tremors due to beta-2 stimulation. Notice the autonomic picture at the beginning of the handout. Although there are mainly beta-1 receptors in the heart, there are SOME beta-2 receptors. That is why albuterol and other beta-2 agonists tend to speed up the heart at the same time that they are opening the airways (causing bronchodilation). |
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What is the order of administration for
|
# 1 Beta-2 Agonist
# 2 Anticholinergic # 3 Corticosteroid |
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how long can a can of albuterol last?
|
Each can= 200 sprays. If using 2 sprays QID, each can should last 25 days.
Do not exceed 200 sprays: the correct amount of medication in each inhalation cannot be assured after 200 actuations, or sprays. Patients commonly use the spray after 200 since they can shake it and it appears that there is more medication. |
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what other drugs and products should not be taken by an asthmatic patient?
|
No ASA
No NSAIDs No yellow-colored products |
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Levalbuterol is aka
|
Xopenex
|
|
|
Xopenex is aka
|
levalbuterol
|
|
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How does levalbuterol compare to albuterol?
|
For most patients, albuterol will be safe and well-tolerated. However, it is possible that certain subsets of patients might achieve greater bronchodilation from levalbuterol than albuterol. This includes patients requiring high doses of albuterol.
MOA: Bronchodilator (with little effect on heart rate) |
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pirbuterol
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maxair
|
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|
maxair
|
pirbuterol
|
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what is the advantage of pirbuterol?
|
MOA: Similar to albuterol
(more sprays per can) Autohaler: “Automatic” inhaler (Breath activated) The unit is breath-activated so that the medication is delivered automatically during inspiration without the need for the patient to coordinate actuation by hand with inspiration (breathing in). In other words, just by breathing in, the canister clicks and the metered dose is inhaled. This is an advantage for people who cannot accurately depress the canister by hand and at the same time, inhale properly. This Autohaler does it automatically. |
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What are four good counseling techniques for breathing medications?
|
1) For the MDI oral inhalation, look up at the ceiling when inhaling
2) For the nasal inhalation, look down at the floor when inhaling it through the nostril. Then look up to avoid the medication from dripping out 3) For the plastic flat Diskus, look straight ahead, and place it in the mouth in the manner of “eating a sandwich” 4) For the mouth products: cup lips around upper and lower front teeth to avoid the drug from attaching to the teeth |
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how often is salmeterol administered?
|
Q 12 hours
|
|
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which medication comes in diskus form?
|
salmeterol xinafoate (serevent)
Activate DISKUS, hold horizontally → Inhale Powder |
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what is the MOA of foradil?
|
Bronchodilator (Similar to SEREVENT)
*****LONG-ACTING***** Frequency: Q 12 hours |
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Ipratropium is aka?
|
atrovent
|
|
|
Atrovent is aka?
|
ipratropium
|
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What is the MOA of atrovent and when is it indicated?
|
MOA: Prevent increases in intracellular cGMP,
which are caused by interaction of ACh with muscarinic receptor on bronchial smooth muscle Quaternary ammonium compound chemically related to atropine Less absorption & systemic effects than atropine |
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|
what is the advantage of atrovent over B2 agonists?
|
Less tachycardia than B2 agonists.
Typically, beta-2 agonists are used more in asthma, and the anticholinergics more in chronic bronchitis and emphysema |
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what is a caution in using Atrovent?
|
Aerosol spray (not solution) contains soy lecithin as suspending agent (Same family as peanuts)
Contraindicated: In pts with peanut allergy |
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COMBIVENT is aka?
|
Albuterol/ Ipratropium
|
|
|
Albuterol/ Ipratropium is aka?
|
(COMBIVENT)
|
|
|
What is the MOA of combivent?
|
Two different mechanisms → bronchodilation
(Greater bronchodilator effect than when either drug used alone) Indication: COPD pts on a regular aerosol bronchodilator who continue to have evidence of bronchospasm & require a second bronchodilator |
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|
what is a caution in combivent?
|
Contains soy lecithin, as suspending agent
Contraindicated In patients with peanut allergy |
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|
Tiotropium bromide is aka
|
SPIRIVA
|
|
|
SPIRIVA is aka
|
Tiotropium bromide
|
|
|
Spiriva MOA and administration
|
HANDIHALER: 18 mcg (1 capsule of inhalation powder)
MOA: Bronchodilator (like ATROVENT) Frequency: QD (Long-acting, unlike ATROVENT) Note: Capsules should always be stored in the sealed blisters, removed immediately before use and placed in device |
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|
What caution is there in using Spiriva?
|
Capsules MUST be inhaled: NOT SWALLOWED
|
|
|
Nedocromil is aka
|
TILADE
|
|
|
TILADE is aka
|
Nedocromil
|
|
|
Cromolyn sodium is aka
|
INTAL
|
|
|
INTAL is aka
|
Cromolyn sodium
|
|
|
What is the MOA of mast cell stabilizers?
|
MOA: Inhibit the degranulation of sensitized and
nonsensitized mast cells that occur after exposure to specific antigens – acts locally on the lungs |
|
|
Theophylline is aka
|
(many brands & formulations)
Tabs: THEOCRON - 100, 200, 300 mg UNIPHYL – 400, 600 mg Caps: THEO-24 – 100, 200, 300, 400 mg Oral liquid: 80 mg/15 ml (generic) |
|
|
How does theophylline work?
|
MOA: Unclear, possible inhibition of bronchoconstriction caused by adenosine
Acts by direct relaxation of smooth muscle of bronchi and pulmonary blood vessels, CNS stimulation, induction of diuresis, central respiratory stimulation |
|
|
What is the therapeutic range for theophylline?
|
Therapeutic range: 5 – 15 mcg/mL
Old range was 10 – 20 mcg/mL -Saturation (non-linear) elimination kinetics: Hepatic CYP-450 enzymes -Toxicity at high doses (GI, CNS) |
|
|
What are precautions for taking theophylline?
|
Interactions: CYP-450 inhibitors: Cipro, erythromycin, Biaxin, etc
Inducers: Smoking, Barbiturates, Charcoal- cooked meat, Rifampin etc. Advise patient who smokes to notify prescriber if he/she quits. The dose of Theophylline will probably need to be decreased to avoid toxicity |
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|
Fluticasone is aka
|
FLOVENT
|
|
|
FLOVENT is aka
|
Fluticasone
|
|
|
what is the MOA of flovent?
|
MOA: Direct inhibitory effects on many cells involved in airway inflammation in asthma
(anti-inflammatory) Result: Reduction in eosinophils, mast cells, macrophages, T-lymphocytes in the bronchioles |
|
|
Flunisolide is aka
|
(AEROBID), also AEROBID-M
(M contains menthol for flavor or taste) |
|
|
Aerobid also AEROBID-M are known as
|
Flunisolide
|
|
|
Warning for budesoneide?
|
it is the only Preg Cat. B
Buddy inside |
|
|
Budesonide is aka
|
Pulmicort
|
|
|
Pulmicort is aka
|
Budesonide
|
|
|
Beclomethasone dipropionate is aka
|
QVAR
|
|
|
QVAR is aka
|
Beclomethasone dipropionate
|
|
|
what is a flexhaler?
|
inhalation driven, multi-dose dry powder
|
|
|
what is a respule?
|
ampules for use in jet nebulizer
|
|
|
Triamcinolone is aka
|
azmacort
|
|
|
azmacort is aka
|
Triamcinolone
|
|
|
azmacort properties
|
Spacer Mouthpiece – plastic actuator part of product
Indication: Chronic asthma Boxed warning: Care with patients who are transferred from systemically active corticosteroids (example: Prednisone 20 mg PO/day to aerosol) |
|
|
Mometasone Furoate is aka
|
asmanex
|
|
|
asmanex is aka
|
Mometasone Furoate
|
|
|
What is a twisthaler?
|
Plastic cap-activated dosing mechanism with dose counter
This way the patient knows exactly when to get a refill from the pharmacy |
|
|
Fluticasone/Salmeterol is aka
|
Advair
|
|
|
Advair is aka
|
Fluticasone/Salmeterol
|
|
|
Advair properties
|
MOA: Corticosteroid with beta-2 agonist (2 long-acting products)
Frequency: every 12 hours Also HFA MDI Patients who cannot utilize the diskus properly can be switched to the MDI |
|
|
Symbicort is aka
|
formoterol/budesonide
|
|
|
formoterol/budesonide is aka
|
symbicort
|
|
|
symbicort properties
|
A metered dose inhaler that combines a long-acting beta-2 agonist (formoterol) with a corticosteroid (budesonide).
Indicated for the treatment of asthma in patients 12 years of age and older. Use should be limited to patients with inadequate control with inhaled corticosteroids, or whose asthma severity indicates use of combination therapy Onset of action of formoterol is quicker than salmeterol Long-acting beta-2 agonists have been associated with increased risk of asthma-related death |
|
|
Fluticasone is aka
|
flonase
|
|
|
Flonase is aka
|
fluticasone
|
|
|
Flonase properties
|
Glucocorticoid (corticosteroid) for allergic rhinitis
(adults & children > 4 y. o.) Starting dose: 2 sprays per nostril once daily same dosage divided twice daily – 8AM and 8PM, also effective Maximum daily dosage should not exceed 2 sprays/nostril |
|
|
What is the only pregnancy category b of the nasal products?
|
Rhinocort AQ (budesonide)
|
|
|
what advice do we give patients taking nasal products?
|
Counsel: Use Saline spray prior to use to
reduce nasal irritation |
|
|
what is the indication for LTRBs like Montelukast (SINGULAIR)?
|
Indication: For the chronic treatment and prevention of the symptoms of asthma, either as monotherapy or as add-on therapy in patients whose persistent mild-moderate asthma is inadequately controlled with inhaled corticosteroids
|
|
|
what are the labeled and unlabeled uses for montelukast?
|
Asthma prophylaxis & chronic treatment
Relief of symptoms of Allergic Rhinitis Unlabeled use: Chronic urticaria NOT for acute asthma attacks |
|
|
what is the MOA of accolate similar to?
|
Singulair
Inhibits CYP-450 2C9 and 3A4 Interaction with Warfarin (clinically significant) Hepatotoxicity precautions Due to complex BID dose and interactions, Singulair is the more commonly used product in this category |
|
|
How do we calculate pack-years?
|
It is calculated by multiplying the number of packs of cigarettes smoked per day by the number of years the person has smoked. For example, 1 pack-year is equal to smoking 1 pack per day for 1 year, or 2 packs per day for half a year, and so on.
Critical comment: A person who lives with a smoker also shares the risk with the smoker due to inhalation of second-hand smoke. |
