Upenn Sdm Pharm Final 2011

Front 1

Hallmarks of Cancer
-6 alterations in cell physio

Back 1

1. self sufficiency of growth factor
2. Insensitive to growth inhibition factors
3. Evading apoptosis
4. Limitless replication potential
5. Sustained angiogenesis
6. Tissue invasion/metastasis

Front 2

What stimulates angiogenesis of tumor cells?

Back 2

Hypoxia of tumor cells initiates signal for BV growth

Front 3

What is the primary mediator of angiogenesis (its a protein)?

Back 3

VEGF - vascular endothelial growth factor

Front 4

T/F - All cancers of WBCs are malignant

Back 4

True - they are all called Leukemia

Front 5

T/F - All cancers of lymphoid tissue are malignant

Back 5

True - all are called lymphoma

Front 6

Kinetics of tumor growth - Early growth
1. How does growth fraction relate to cell death here?
2. Growth fraction decreases in response to ________ increasing?

Back 6

1. Growth fraction is HIGH; Cell death is LOW
2. Cell mass (tumor mass) increases --> growth decreases

Front 7

7 Warning Signs of Cancer - CAUTION

Back 7

C- change in bowel movements
A - A sore that doesn't heal
U - Unusual bleeding/discharge
T - Thickening or lump develops
I - Indigestion or difficulty swallowing
O - Obvious change in wart/mole
N - Nagging cough/hoarseness

Front 8

Cancer Chemo Treatment - Induction therapy

Back 8

1. 1st step in shrinking cancer
2. Evaluation of cancer's response to Tx
3. Patient may be given additional chemo to remove disease

Front 9

Cancer Chem Tx - Adjuvant Therapy

Back 9

1. Given to eradicate MIICROMETASTIC disease
2. Follows surgery or radiation

Front 10

Cancer Chemo Tx - Neoadjuvant therapy

Back 10

1. Given to shrink tumor prior to surgery

Front 11

4 separate anti-cancer med questions:
1.Name 2 Antimetabolite drugs examples
2.Name 2Tubulin-binding proteins
3. What is their role (What do they block?)
4. Schedule or dose-dependent

Back 11

1. methotrexate or fluorouracil
2. vincristine, vinblastine
3. Block cell activities at some stage of cell cycle
--> Thus, they are CELL CYCLE-DEPENDENT AGENTS
4. Schedule dependent only

Front 12

1. Alkylating agents drug examples
2. Are they specific to a stage of cell cycle?
3. Schedule or dose dependent?

Back 12

1. cyclophosphamide, busulfan
2. NO
3. Dose-dependent - cell survival is exponentially related to dose

Front 13

Most chemotherapeutic agents are most effective when tumor mass size is_____ and growth fraction is _______?

Back 13

tumor mass is small and growth fraction is high

Front 14

Effects of chemotherapy on tumor cell populations follows ______ kinetic principles: fraction of cells killed is proportional to the dose used

Back 14

1. first-order
- Percentage of cells killed remains constant - thus its exponential

Front 15

In cancer chemo, treatment results are a direct function of...
1. ?
2. ?

Back 15

1. dose of drug administered number & - dose intensity
2. frequency of repeated treatments - dose density

Front 16

(Cancer) Dose in which patients experience serious, life-threatening toxicity

Back 16

Dose-limiting toxicity (DLT)

Front 17

(Cancer) highest possible dose that does not produce life-threatening toxicity

Back 17

Maximum tolerated dose (MTD)

Front 18

(Cancer) minimum dose to produce pharmacologic effect

Back 18

Biologically effective dose (BED)

Front 19

(Cancer) Dose _______ is the amount of chemotherapy administered to a patient over a specific unit of time. (e.g. Cumulative dose/28 days)

Back 19

Intensity

Front 20

(Cancer) Dose _______ A scheduling approach designed to decrease the time period between chemotherapy administration (e.g. The amount of dose per administration)

Back 20

Density

Front 21

T/F - The scheduling of the dose in relation to circadian rhythms can alter the therapeutic index with cancer drugs

Back 21

True

Front 22

_____________ will require the drug to be held, a dosage reduction and/or drug discontinuation

Back 22

Dose-limiting toxicities

Front 23

Myleosuppresion and Cytopenias are the result of ____________________?

Back 23

Bone marrow suppression

Front 24

(In cancer chemo) ______________ (3 side fx) are seen increasingly with signal transduction agents, including mTOR inhibitors, and ionizing radiation

Back 24

Mucositis, stomatitis, esophagitis - inflammatory process of the oral mucosa in response to anticancer agents or ionizing radiation

Front 25

Anthracycline and Trastuzumab are 2 cancer drugs that are likely to produce this side effect ________?

Back 25

Drug-induced cardiomyopathy

Front 26

1.Cancer drugs most likely to cause Hemorrhagic cystitis (bladder).

2. This is due to the active metabolite of these drugs called ________.

3. _________ is given in conjunction with these drugs because it binds the metabolite

Back 26

Cyclophosphamide and ifosfamide

Acrolein

Mensa (Mesnex)

Front 27

cisplatin, methotrexate, nitrosoureas, mitomycin-C are cancer drugs that are most toxic to the ____________ system (human organ system).

Back 27

Renal

Front 28

Bleomycin is an anti-cancer agent that is most commonly associated with __________ toxicity.

Back 28

Pulmonary

Front 29

Alkylating agents
1. MOA

Back 29

1. Add covalent bonds to nucleic acid bases --> cross links that prevent replication, transcription

Front 30

Name the anti-cancer med: **Also, RA med**
1. Classic alkylating agent
2. Hemorrhagic cystitis - bladder toxic
3. used for leukemia, lymphoma
4. Immunosuppressant - used for RA
5. Given with Mesna to protect bladder
6. Prodrug activated by CYP450

Back 30

Cyclophosphamide

Front 31

Name anti-cancer med:
1. Neurotoxic
2. Toxic to bladder (hemorrhagic cystitis)
3. Classic Alkylating agent

Back 31

Ifosfamide

Front 32

Class of anti-cancer meds that are a Type of alkylating agent - cross link DNA --> prevent transcription, replication

Back 32

Nitrosureas

Front 33

1. Nitrosurea alk agent
2. **Crosses BBB -- used to treat brain tumors**
3. ADR - interstitial pneumonitis & pulmonary fibrosis
4. ADR - myleosuppression (bone marrow), N/V, stomatitis, teratogen

Back 33

Carmustine (BCNU, BiCNU)

Front 34

Name the anti-cancer med:
1. Nitrosurea alk agent
2. used in treatment of pancreatic cancer (beta-cells target)
3. Use to treat GI cancer
4. Particularly nephrotoxic

Back 34

Streptozocin (Zanosar)

Front 35

DRUG Class
1. Bind topo-I--DNA complex
2. Prevents religation of DNA
3. Causes ssDNA and cleavable complexes

Back 35

Topoisomerase I inhibitors

Front 36

1. Topo-I inhibitor
2. Pro-drug that is cleaved to active metab -- SN-38
3. Used for: ovarian cancer, colorectal cancer, Lung cancer, leukemia
4. ADRs - Bone marrow suppresion, gonadal suppression, teratogen
5. ***Diarrhea that can be life-threatening develops***

Back 36

Irinotecan – classic drug of class
(Camptosar, CPT-11)

Front 37

Name the DRUG CLASS of anti-cancer meds:
1. Cause freezing of DNA in DNA complex with enzyme
2. Causes dsDNA breaks

Back 37

Topoisomerase II Inhibitors

Front 38

Name the anti-cancer meds:
1. Intercalating type of drug in this class
2. Causes conformational changes due to intercalating
3. Also generates free radicals --> causes toxicities/cytotoxicities
4. Key factor - makes you have red-orange urine
5. many uses
6. Available in liposomal formulas

Back 38

Doxorubicin (AdriamycinR, DoxilR)
or
Daunorubicin (Daunomycin,
CerubidineR,
DaunoXomeR)

Front 39

Liposomal formulations of Daunorubicin

Back 39

Doxil and DaunoXome are
liposomal products

Front 40

Name the anti-cancer med:
1. Non-intercalating Topo II inhibitor
2. Causes HYPOtension
3. Uses: testicular, lung,
leukemias, lymphomas, myeloablation

Back 40

Etoposide (VePesidR, VP-16)

Front 41

DRUG CLASS
1. Structural analogs of naturally occurring metabolites: interfere with the normal synthesis of nucleic acids by false substitution
2. Cause DNA damage
3. Cytotoxic - particularly S-phase

Back 41

Antimetabolites

Front 42

DRUG sub-class
1. Anti-metabolite
2. fluorodeoxyuridine monophosphate (FdUMP) which, in the presence of folates, binds tightly to and interferes with the function
of thymidylate synthase
3. Stops DNA synthesis

Back 42

Pyrimidine antagonists

Front 43

1. Pyrimidine antagonists
2. Anti-metabolite class
3. Used for: GI and breast cancers

Back 43

Fluorouracil (5-FU, Efudex, Adrucil)

Front 44

DRUG Subclass of antimetabolites
1. bind to enzyme dihydrofolate reductase, thereby blocking the
reduction of folate to its active form, tetrahydrofolate.
2. Stops both DNA and RNA synthesis
3.Stops thymidine and PURINE synthesis

Back 44

Folate Analog Metabolic Antagonists

Front 45

Name that anti-cancer med:
1. Antimetabolite
2. Folate analog antagonist
3. HIGHLY protein bound
4. **Can be used for RA**
5. Highly nephrotoxic
6. leucovorin used
as “rescue” with high
doses
7. Salicylates, probenicid decreases renal clearance
8. Used for: leukemias, breast,
head and neck,
lymphomas

Back 45

Methotrexate (Folex, Mexate)

Front 46

DRUG Subclass of anti-metabolite
1. Must be phosphorylated intracellularly to an active triphosphate form which competes with deoxycitidine for DNA polymerase
2.

Back 46

Cytidine Analogs

Front 47

1. Anti-metabolite, Cytidine analog
2. Main use = Leukemia
3. Uses: Gastro-intestinal, leukemia, breast, lung

Back 47

Cytarabine (Ara-C, (Cytosar-U)

Front 48

DRUG Subclass of anti-metabolites
1. prodrugs converted to ribonucleotides that incorporate into DNA, thereby blocking de novo purine synthesis
3. Immunosuppresion is found with some of these drugs

Back 48

Purine Antagonists

Front 49

Name the anti-cancer med:
1. Purine antagonists, anti-metabolite
2. Used for: leukemias, lymphomas, post-organ
transplant
3. ADR - Hepatic stasis; 75%
dose reduction required with use of allopurinol

Back 49

Mercaptopurine (6-MP, Purinethol)

Front 50

1. DRUG CLASS
2. Bind to tubulin - interfere with mitotic spindle
3. Drugs are NOT water soluble - patients experience most problems with drug solvent

Back 50

Microtubule interacting agents

Front 51

1. Drug subclass of microtubule IA
2. Bind to specific sites on tubulin, thereby inhibiting tubulin polymerization and
subsequent disappearance of the spindle apparatus. Agents block the progression of cells beyond mitosis

Back 51

Vinca alkaloids

Front 52

Name the Anti-cancer med:
1. Vinca Alkaloid ( Mt-interacting)
2. Unique feature - causes SIADH (syndrome of inappropriate anti-diuretic hormone secretion)
3. Treats: Lymphoma, Lung, Breast cancers

Back 52

Vincristine (Oncovin)

Front 53

Name the anti-cancer med SUB-Class:
1. Drug Subclass of microtubule-interacting agents
2. Bind to a specific site on tubulin, inducing the formation of aberrant microtubules.
3. Block cells in pre-mitosis (G2-M) by overstabilizing microtubules, rather than inhibiting their assembly.

Back 53

Taxanes

Front 54

Name this anti-cancer med:
1. Taxane subclass of Mt-interacting
2. Unique feature - Cremaphor diluent: premedicate for hypersensitivity reaction
3. Treats: Lung, breast, head/neck, and ovarian cancers

Back 54

Paclitaxel (Taxol)

Front 55

Name this sub-class of anti-cancer meds:
1. Subclass of Mt-interacting agents
2. bind to β-tubulin subunits on microtubules, thereby suppressing microtubule dynamics
3. Major site of action --> blocks cells during mitotic phase of cell division
4. low level of susceptibility to MRP-1 or P-gp efflux transporters.

Back 55

Epothilones

Front 56

Name the anti-cancer med:
1. Epothiones subclass (Mt-IA class)
2. Used to treat breast cancer

Back 56

Ixabepilone (Ixempra)

Front 57

Name that SUB-Class of anti-cancer meds:
1. Subclass of Microtubule-interacting agents
2. Non-taxane microtubule dynamics inhibitor
3. Eribulin (Halaven) - is the prototypical drug of this class
--> used to treat breast cancer

Back 57

Halichondrin B analog

Front 58

Name the class of anti-cancer meds:
1. Differentiating Class
2. Drug subclass that: stimulates differentiation of several cell lines, including squamous, erythroid and myeloid progenitor cells
3. Classic examples:
a. All-trans-retinoic acid (ATRA, tretinoin, Vesanoid) - acute promyelocytic leukemia

B. Bexarotene (Targretin) - cutaneous T-cell lymphoma

Back 58

Vitamin-A Derivatives

Front 59

Name that anti-cancer drug:
1. Drug in Misc Class
2. Inhibits the enzyme ribonucleotide reductase, which plays a key role in DNA synthesis by catalyzing the conversion of ribonucleotides to deoxyribonucleotides. Most toxic to cells that are actively synthesizing DNA
3. Used to treat: leukemias, cervical cancer, radiation sensitizer

Back 59

Hydroxyurea (Hydrea)

Front 60

Name that anti-cancer med:
1. Misc class of drug
2. Inhibits protein synthesis in tumor cells dependent upon exogenous asparagine
3. This drug breaks down asparagine in blood and tumors can’t use this as source of exogenous ASN
4. Used to treat: Leukemia and lymphoma

Back 60

Asparaginase (Elspar)
Pegaspargase (PEG-L-asparaginase, Oncospar)

Front 61

1. Drug Class
2. A number of tumors arise from tissues normally sensitive to hormonal growth controls.
3. The more differentiated tumors often retain hormone receptors.
4. Strategies involve ablation of various hormone-secreting tissues or administration of hormones that down-regulate tumor growth

Back 61

Hormonal Agents

Front 62

Name that anti-cancer med:
1. Estrogen receptor modulator
2. Estrogen antagonist and agonist properties
3. Solely used to treat breast cancer

Back 62

Tamoxifen (Nolvadex)

Front 63

Name the anti-cancer med SUB-CLASS
1. Hormonal agent
2. inhibit intracellular uptake and binding of testosterone and dihydrotestosterone to
specific receptors.

Back 63

Anti-androgens

Front 64

Name the anti-cancer med:
1. Antiandrogen agent (hormonal agent)
2. Used to treat prostate cancer

Back 64

Flutamide (Eulexin)

Front 65

1. Drug subclass of hormonal agents
2. Initial effect causes release of FSH and LH from the pituitary.
3. Since the normal release
of FSH and LH is cyclical and regulated by feedback inhibition, continued administration results in downregulation of pituitary GnRH receptors, suppressing FSH and LH release.
4. Continued administration
in males - little or no testosterone; in females - little or no estradiol

Back 65

LHRH agonists

Front 66

Name that anti-cancer med
1. LHRH agonist
2. used to treat breast and prostate cancers

Back 66

Leuprolide (Lupron, Viadur)

Front 67

1. Drug subclass of hormonal agents
2. inhibit conversion of adrenal androgens to estrogens via inhibition of aromatase enzyme

Back 67

Aromatase inhibitors

Front 68

1. Aromatase Inhibitor
2. Treats Breast cancer

Back 68

Anastrozole (Arimidex)

Front 69

1. Monoclonal Antibody
2. Chimeric antibody
3. Ab target = CD20 antigen on B-lymphocytes (not found on normal cells or stem cells); mediates B-cell lysis by ADCC and complement-dependent cell lysis
4. Used to treat: Lymphomas, leukemias, autoimmune disorders

Back 69

Rituximab (Rituxan)

Front 70

Name drug class (general) of anti-cancer meds:
1. Drug Class
2. Drugs that influence the transmission of a signal through the cell, leading to changes that influence cell cycling or other cellular processes
3. Major class = Kinase inhibitors, EGF-inhibitors, mTOR inhibitors
4. ***MANY drugs undergo transformation via CYP450***

Back 70

Signal Transduction Inhibitors

Front 71

1. Inhibits the Bcr-Abl tyrosine kinase created by the Philadelphia chromosome, platelet-derived growth factor (PDGF), c-kit, and stem cell factor
3. Inhibiting cell proliferation and promoting apoptosis

Back 71

Imatinib mesylate (Gleevec)

Front 72

1. Inhibits epidermal growth factor receptor (EGFR) tyrosine kinase, thereby inhibiting intracellular phosphorylation of signaling pathways
2. Treats - pancreatic cancer & lung cancer

Back 72

Erlotinib (Tarceva)

Front 73

1. Monoclonal antibody directed against the extracellular domain of the erbB1 receptor
2. Treats: Head/neck cancer and colorectal cancer

Back 73

Cetuximab (IMC-225; Erbitux)

Front 74

Name that anti-cancer drug:
1. Rapamycin derivative; inhibits mTOR, which induces G1 growth and inhibits proteins
2. Treats Renal cell carcinoma and pancreatic cancer

Back 74

Everolimus (Afinitor)

Front 75

1. Anti-angiogenesis agents
2. Drugs prevent wound-healing
3. Bevacizumab (Avastin) -- antibody directed against ____receptor

Back 75

VEGFR- Inhibitors

Front 76

Name the anti-cancer med:
1. reversible inhibitor of 26S proteasome, which is essential for degrading ubiquitinated proteins
2. build-up of non-degraded proteins disrupts the cell cycle and multiple signaling cascades, leading to cell death

Back 76

Bortezomib (Velcade)

Front 77

1. Extrinsic factors of asthma
2. Intrinsic factors of asthma

Back 77

1. Environmental factors (pollen, allergens, etc.)
2. Infections or emotional distress

Front 78

What are the 2 components that cause asthmatic attack
1.?
2.?

Back 78

1. Bronchiole constriction
2. Inflammation of bronchial smooth muscle

Front 79

What are the 2 phases of an asthmatic attack

Back 79

Early and Late phases

Front 80

This describes what phase of an asthmatic attack:
1. Bronchoconstriction within
within 20 minutes after exposure to an extrinsic
or intrinsic bronchospastic stimulus.
2. Probably caused by mast cell mediators such as histamine,
proteases (heparin), PAF and leukotrienes (LTD4)

Back 80

Early phase of attack

Front 81

What phase of asthma attack is described?
1.Begins 3 -4 hours and peaks 4 – 8 hours after exposure to extrinsic or intrinsic stimuli.
2. Initial activation of mast cells release chemotactic factors (ECF and NCF) which attracts inflammatory cells into area
3. Any non-allergic stimuli may precipitate bronchioconstriction

Back 81

Late phase asthma attack

Front 82

1. Mast Cells in late phase release _______ and _________?

2. Which one can cause permanent scarring of bronchial tissue

Back 82

1. Cytokines and Major basic protein

2. Major basic protein

Front 83

1. What is NOW used for prophylaxis against asthma?

2. What is reserved only for acute attacks?

Back 83

1. Inhaled glucocorticoids and oral leukotriene modulators = prophy

2. Beta-2 agonists are used for acute attacks

Front 84

1. Why are Beta-2 agonists not used for prophy anymore with asthma

Back 84

1. People become conditioned to these drugs -- will need more to illicit response = RECEPTOR DOWN REGULATION
2. there are better prophy drugs available now

Front 85

1. What specifically to corticosteroids block
2. What 2 products does this indirectly block?
3. Corticosteroids block ________ of inflammatory cells?
4. How do corticosteriods enhance effect of beta-2 agonists

Back 85

1. Phospholipase A2
2. Prostaglandins and Leukotrienes
3. Migration
4. They increase the amount of beta-2 receptors in lung tissue and WBCs (mast cells)

Front 86

High _________ levels in mast cells prevents mast cell degranulation

Back 86

cAMP

Front 87

High cAMP levels causes what effect in lungs?

Back 87

Bronchodilation

Front 88

What phase of asthma are best effected by corticosteroids?

Back 88

Late phase -- because they take a while to work (DNA binding/modulating effect)

Front 89

Name 2 reasons why corticosteriods are not given PO for asthma

Back 89

1. Cut down on systemic absorption - nasty side effects
2. Deposit drug where needed at much lower dose

Front 90

1. Drug class of:
Beclamethasone (Beclovent®)
Flunisolide (Aerobid®)
Fluticasone (Flovent®)
Triamcinolone (Azmacort®)
2. Which 2 have almost no mineralocorticoid effect

Back 90

1. Topical/inhaled corticosteroids
2. Beclamethasone and Triamcinolone

Front 91

What is a major ADR or inhaled steroids?

What must your patient do after they use this type of inhaler?

Back 91

1. Local immunosuppression --> Candidial infections

2. Wash their mouth out with water to reduce the risk of oral yeast infection

Front 92

1.When would you give a corticosteroid PO instead of INH?

2. How long should this treatment be given for? No longer than _______?

Back 92

1. acute exacerbation of asthma where B2 response is diminished due to increased tolerance

2. No longer than 10 days

Front 93

What are 5 common side effects from prolonged cortiocosteroid dose, PO?

Back 93

1. suppression of the hypothalamic-pituitary- adrenal axis
2. osteoporosis
3. increased blood sugar
4. increased risk of infection
5. cataracts

Front 94

1. Non-steroidal prophy asthma drugs
2. NON-bronchodilating
3. Decrease Calcium efflux --> prevent mast cell degranulation
4. Prevents BOTH early and late phase attack
5. Decreases dose of more toxic drugs
6. ***LEAST TOXIC OF ANTI-ASTHMATICS***

Back 94

Cromolyn sodium (Intal®), Nedocromil (Tilade®)-inhalants

Front 95

In what type of an attack should NEVER instruct a patient to use Cromolyn sodium (Intal®), Nedocromil (Tilade®)-inhalants

Back 95

1. Never use in acute attack --> b/c they are not bronchodilators

Front 96

1. ______________ stimulate:
a. Bronchoconstriction
b. increase capillary permeability leading to edema in smooth muscles of bronchi
c. stimulate mucous secretion
d.impair mucocilliary clearance

Back 96

Leukotrienes (LTD4, LTC4)

Front 97

1. What are the 2 mechanisms of action of leukotriene modifiers?
2. Which MOA is better/preferred?
3. What type of asthma are Leukotriene modifiers very effective at preventing

Back 97

1. Inhibit lipoxygenase enzyme or block leukotriene receptor
2. Preferred = blocking receptor
3. ASA/NSAID induced asthma

Front 98

T/F Leukotrienes are better than corticosteroids at improving airway constriction.

Back 98

False

Front 99

Why would you not recommend giving a Leukotriene modulator for an acute attack?

Back 99

1. its given PO
2. Takes a while to work
3. Must only be used for prophy

Front 100

1. First drug to be FDA approved in its class
2. Pill taken PO q 6 h
3. 5-Lipoxygenase inhibitor
4.. Drug WILL block metabolism of warafin and theophylline --> both of these drugs have LOW therapeutic indicies
-->Will increase risk of bleeding with warafin
-->If theophylline levels get too high (Cardiac and CNS stimulant) Cardiac arrhythmias
Seizures

Back 100

Zileuton (Zyflo®)

Front 101

1. These 2 drugs are Leukotriene receptor blockers
2. __________ is the better of the 2 drugs and can be used for seasonal allergies also
3. Not used for acute attacks

Back 101

1. Zafirlukast (Accolate®) & Montelukast (Singulair®)

Front 102

Why is Montelukast (Singulair®) preferred over Zileuton (Zyflo®) ?

Back 102

1. Because singulair does NOT interact with warafin

Front 103

What is the mechanism of beta-2 agonists?

Back 103

Directly stimulate Beta-2 adrenergic receptors --> Bronchodilation

Front 104

1. What are the effects of Theophylline/caffiene and beta-2 agonists on mast cells?
2. __________ (drug) decreases the break down of cAMP in mast cells
3. __________ (drug) stimulates adenylate cyclase enyzme

Back 104

1. They increase cAMP levels in mast cells which prevents their degranulation
2. Theophylline
3. Beta-2 agonists

Front 105

Name that asthma drug:
1. This drug stimulates BOTH beta-1 and beta-2 receptors
2. What 2 serious side fx come from this drug?

Back 105

1. Isoproterenol (Isuprel®)
2. Increased heart rate and contraction force ---> can cause tachyarrthymias

Front 106

Name the drug:
1. stimulates alpha-1, beta-1, and beta-2 receptors
2. alpha-1 effect causes blood vessel constriction which reduces mucosal edema
3. Given SQ/IM injection 1:1000 for status asthmaticus

Back 106

Epinephrine

Front 107

Name drug used in asthma:
1. a1, b1, b2 agonist
2. Tachyphylaxis can develop quickly
3. CAN Cross BBB--which means its not a ____________.

Back 107

1. Ephedrine
2. NOT a catecholamine (not epi) --> b/c it can cross BBB

Front 108

Name this asthma drug:
1. – inhalant and pill.
2. Same structure as isoproterenol except OH group moved from C4 to C5 on benzene nucleus.
3. IF you Push dose and you can lose β2 selectivity

Back 108

Metaproterenol (Alupent®)

Front 109

1. inhalant and injection.
2. A congener of metaproterenol with greater β2 selectivity
3. Can be given chronically to prego women that are having premature contractions to prevent uterine contractions (B2 receptor stimulation relaxes the uterus)

Back 109

Terbutaline (Brethaire)

Front 110

Name this asthma med:
1. inhalant and pill
2. Most commonly prescribed β2 agonist.
3. Selectivity for β2 receptor greater than metaproterenol and also a longer acting drug.
4. STANDARD OF CARE/DRUG of CHOICE

Back 110

Albuterol (Proventil®)

Front 111

Name that Asthma drug:
1. inhalant.
2. Longest acting (12 hours) of the β2 selective agents.
3. Less problem with development of tolerance because of less frequent dosing. 4. **However slower onset (10 minutes) than other inhalants.

Back 111

Salmeterol (Serevent®)

Front 112

Which 2 anti-asthmatic drugs can actually precipitate an asthma attack?

Back 112

Albuterol and Salmeterol

Front 113

Name that Anti-asthmatic drug
1. Blocks phosphodiesterase
III and IV
2. Blocks adenosine receptors
Stimulates catecholamine
release
3. Antiinflammatory effects
Pill and injection
4. Low therapeutic index
5. Drug interactions – CYP1A2 substrate

Back 113

Theophylline (Theodur®)

Front 114

In the case of status asthmaticus, When patient is on propranolol you must give _________ instead of epi - because epi has lower affinity for receptor

Back 114

Theophylline (Theodur®)

Front 115

In the case of Theophylline (a CYP1A2 substrate):
1. Erythromycin and ciprofloxacin ___________ blood levels
2. Phenobarbital and carbamazepine _______ blood levels

Back 115

1. Increase - because eryth and cipro are inhibitors
2. Decrease - because phenobarb & carbamazepine are enzyme inducers

Front 116

Name this Anti-Cholinergic Anti-asthmatic drug:
1.. Permanently charged atropine-like molecule
2. ANTI-MUSCARINIC
3. Blocks ACH action at M3 receptor
4. Combivent = this + albuterol
5. Common side fx = xerastomia, bad taste

Back 116

Ipatropium (Atrovent®)

Front 117

This antibiotic is the classic example of a bacteriostatic AB

Back 117

Tetracycline

Front 118

This antibiotic is the classic example of a bacteriocidal agent

Back 118

Penicillin

Front 119

Why are bacteriocidal agents preferred? (2 reasons)

Back 119

1. More efficacious
2. Depend less on immune system

Front 120

Name the grouping of antibiotics:
1. erythromycin
2. Tetracycline
3. Clarithromycin
4. Clindamycin
5. Azithromycin
6. Sulfonamides

Back 120

Bacteriostatic

Front 121

Name the antibiotic group:
1. Penicillins
2. Cephalosporins
3. Metranidazole
4. Quinolones - Ciprofloxicin
5. aminoglycosides

Back 121

Bacteriocidal

Front 122

1. Name antibiotic
2. More broad spectrum – cause more side fx
3. 10% cross-allergenicity of _________ and cephalosporin because of relation in structure
4. Drug class is number 3 on the list (behind NSAIDs and ASA) for causing allergenicity

Back 122

Penicillins

Front 123

Good at treating staph infections (penicillins not good at this)

Back 123

Cephalosporins

Front 124

Name Antibiotic
1. Interactions – drug is a CYP2C9 inhibitor
2. EtOH – disulfiram effects
3. Increases warafin levels
4. DNA interactions
5. **Used solely for anaerobic infections – not effective at aerobics

Back 124

Metranidazole

Front 125

Antibiotic that is Bacteriocidal by inhibiting DNA gyrase

Back 125

Quinolones - Ciprofloxicin

Front 126

Name Antibiotic
1. Typically all end in “mycin”
2. **Gram-negative aerobic infections use**
-->Must be aerobic b/c oxygen is used to get drug into body
3. Attack bacterial ribosomes (30s???)
4. Streptomycin, genomycin – a lot of these are given by injection
-->These drugs have lower therapeutic indicies
5. Have CNS toxicity – go deaf
6. Have neuromuscular blocking activity at high doses – can become paralyzed

Back 126

Aminoglycosides

Front 127

Name antiobiotic
1. Z-packs
2. Good at getting rid of resistant respiratory infections
3. Doesn’t fit into CYP450 – too big to fit into binding site

Back 127

Azithromycin

Front 128

Name antiobiotic:
1. Can be static is some people while it can be cidal in other people
2. Used a lot in Endodontics – used because it hits anaerobes

Back 128

Clindamycin

Front 129

Endocarditis antibiotics when patient is allergic to penicllin (NO Amoxicillin)

Back 129

1. Clarithromycin and azithromycin – used to treat when penicillin allergic patients
2. Clindamycin is used more to treat penicillin allergic pateints because its cheaper

Front 130

Name antibiotic class:
1.inhibit synthesis of folic acid at various steps
2. Bactrum – combination of 2 antibiotics
3. These drugs are NOT GOOD FOR ODONTOGENIC INFECTIONS

Back 130

Sulfonamides

Front 131

Combo ABs:
Static + Static = ?

Back 131

Additive Effect (1+1=2)

Front 132

Combo ABs:
Cidal + Cidal = ?

Back 132

Synergistic Effect (1+1>2)

Front 133

Combo ABs:
Static + Cidal = ?

Back 133

Antagonistic Effect (1+1<1)

Front 134

Don’t combine cidal agent and static agent at the same time because ??

Back 134

--> the cidal agent generally needs the cell to be functioning to be effective

Front 135

Name 3 Antibiotics that are:
Inhibitors of Cell Membrane Synthesis

Back 135

1. Nystatin
2. Amphotericin B
3. Vancomycin

Front 136

Name 2 ABs that are:
Inhibitors of the 30s bacterial ribosome

Back 136

1. Tetracycline - static
2. Aminoglycosides - cidal

Front 137

Name 2 Antibiotics that are:
Inhibitors of the 50s bacterial ribosome

Back 137

1. Erythromycin - static
2. Clindamycin - static

Front 138

Name 3 Antibiotics that are:
DNA synthesis inhibitor

Back 138

1. Metranidazole - cidal
2. Quinolones - cidal
3. Rifampin - indicates TB infection

Front 139

1. What antibiotic blocks folic acid synthesis?

2. What type of Local anesthetics CANNOT be used with these?
3. Why?

Back 139

1. Sulfonamides
2. Ester locals
3. b/c esters are metabolized to PABA which is a precursor to Folic acid and could overcome the competitive blockade that sulfonamides cause

Front 140

Name 3 Antibiotics that are:
Cell Wall Inhibitors

Back 140

1. Penicillins
2. Cephalosporins
3. Vancomycin

Front 141

1.What is the ONLY antibiotic that has been shown scientifically to lower oral contraceptive levels to sub-therapeutic ranges?

2. If she is on the drug, other than the risk of eggo = prego why wouldn't you want to sleep with her anyway?

Back 141

1. Rifampin
2. Rifampin means that the girl has or had Tuberculosis, and besides the fact that she might be contagious, she is most definitely gross!

Front 142

___________ is The range of pathogenic organisms
against which an antibiotic is active.

Broad vs narrow

Back 142

Spectrum

Front 143

What are 3 common problems/adverse effects seen with broad spectrum Antibiotics?

Back 143

1. GI complaints
2. Diarrhea
3. Superinfections from other pathogens (C. albicans, C difficle)

Front 144

Name Antibiotic:
1. Mechanism: Inhibition of cell wall synthesis
2. Bactericidal (against actively growing cells
3. Most inactivated by penicillinase (B-lactamase)
4. Elimination: Kidney mainly unchanged
5. Toxicity: Low

Back 144

Penicillin I

Front 145

2 Narrow spectrum Penicillins?

Back 145

1. Penicillin G (benzyl penicillin)
2. Penicillin V (phenoxy methyl penicillin)

Front 146

2 Broad spectrum Penicillins?

Back 146

1. Ampicillin (Omnipen®)
2. Amoxicillin (Trimox®, Amoxil®)

Front 147

2 BroadEST spectrum Penicillins?

Back 147

1. Carbenicillin (Geopen®)
2. Ticarcillin (Ticar®)

Front 148

2 Penicillins used for b-lactamase resistant bacteria

Back 148

1. Methicillin (Staphcillin®)
2. Oxacillin (Bactocil®), other “oxa” penicillins

Front 149

1. Whats the difference between penicillin G and penicillin V?

Back 149

1. G = acid labile & effects are unpredictable while V = acid stable and shows predictable absorption

Front 150

What bacteria will Penicillin G and V be effective against?

Back 150

1. Gram positive bacteria including:
-->Streptococci
-->Non-penicillinase producing Staphylococci
2. Some gram negative cocci
-->Neiserria
3. Some anaerobes
-->Fusobacterium
-->Porphyromonas

Front 151

Dose Penicillin V for:
1. Adult
2. Child
3. Penicillin is best absorbed with _____________ so take _________?

Back 151

1. Adult: 500 mg q 6h for 7-10 days (1000mg for bad infections)
2. Child: 3 to 6 mg/lb q 6h for 7-10 days
3. Best absorbed on empty stomach -- take 1 hour before meal or 2 hours after

Front 152

Which penicillins are described here:
1. Indications - UTI, URI, Gonad infections
2. Less effective than Pen V against gram positive cocci
3. More effective than Pen V against gram negative cocci and bacilli

Back 152

Broad spectrum penicillins
1. Amoxicillin preferred and used way more than ampicillin

Front 153

1. What compound is added with amoxicillin to combat penicillnase producing bugs
--> this is called Augmentin
2. What about its structure allows this

Back 153

1. Clavulanic acid
2. Possess a beta-lactam ring and thus it increases beta-lactam concentration --> outcompetes beta-lactamase enzyme for binding actual beta lactam ring in Amoxicillin

Front 154

Broadest spectrum Antibiotics:
1. Medical indications
2. T/F they are inactivated by beta-lactamase
3. What are the 2 drug names

Back 154

1. Serious gram negative infections (Pseudomonas, Proteus, Bacterioides Fragilis)
--> Urinary and GI tract
2. True
3. Carbenicillin (Geopen®, Geocillin®) & Ticarcillin (Ticar®)

Front 155

Penicillinase Resistant Penicillins:
1. Medical Indications
2. T/F You should use the penicillins empirically
3. T/ F these penicillins are better than Pen V against strep and bacterial infections of teeth
4. Name the Antibiotics of this subclass

Back 155

1. Those bacteria harboring beta-lactamase - **Staph aureus
2. False
3. False
4. Methicillin - poor oral absorption/nephrotoxic
5. Oxa, Cloxa, Dicloxa, Floxa-cillin – better oral absorption

Front 156

There are Staphylcoccal strains that are resistant to: (6 different antibiotic classes)

Back 156

1. All penicillins including penicillinase resistant
2. All cephalosporins
3. All aminoglycosides
4. All tetracyclines
5. Erythromycin
6. Clindamycin

Front 157

Mechanisms of Resistance - Name the antibiotic class for each example
1. Enzymes that destroy the drug
2. Decreased cell permeability or increased efflux of drug (spitters)
3. Altered antibiotic target

Back 157

1. Penicillins
2. Tetracyclines
3. Erythromycin

Front 158

T/F - If you are allergic to 1 penicillin you are allergic to them all

Back 158

True

Front 159

T/F - Allergy to penicillin is dose-dependent

Back 159

False

Front 160

Drugs to give for penicillin allergic reaction:
1. Mild case
2. Severe case

Back 160

1. Benadryl - diphenhydramine or another H1-receptor blocker
2. Epinephrine injection 1:1000

Front 161

Drug Toxicity is VERY different from allergic response in 4 specific ways:

Back 161

1. Can occur on 1st exposure
2. Phenomenon is dose-related
3. Involves specific tissue receptors
4. Symptoms appear in tissues harboring specific receptors

Front 162

MOA of cephalosporins

Back 162

Cell wall synthesis - bacteriocidal

Front 163

1. ____% incidence of cross-allergenicity of cephalosporins and penicillins
2. Cephalosporins are specifically indicated in the prophy of ________

Back 163

1. 10%
2. Joint replacement patients

Front 164

1. Name gram positive bacteria covered by Cephalosporins (4 of them)
2. ame gram positive negative covered by Cephalosporins (5 of them)

Back 164

1. Staphylococci
Streptococci
Pneumococci
Clostridium
2. Escherichia coli
Proteus
Klebsiella
Neiserria
Bacteroides

Front 165

1. Name 3 examples of Macrolide antibiotics
2. Are these bacteriocidal or -static
3. Whats their MOA?

Back 165

1. Erythromycin, Clarithromycin, Azithromycin
2. static
3. Attack 50s bacterial ribosome subunit

Front 166

Name Antiobiotic:
1. Indications - Diptheria, Legionairre’s, Mycoplasma, Bordatella, Pen-V sensitive infections in penicillin-allergic individuals
2. Main side effect - Bad GI upsets
3. Cytochrome P-450 (CYP-3A4, -1A2) inhibition

Back 166

Erythromycin

Front 167

Name that Antibiotic:
1. More rapid and complete absorption than E-mycin
2. Longer T1/2 than erythromycin
3. Better tolerated (GI) than erythromycin
4. Endocarditis prophylaxis (500 mg) in penicillin allergic individuals
5. Cytochrome P-450 (CYP-3A4) inhibitor

Back 167

Clarithromycin

Front 168

What foods do YOU NOT want to eat when taking erythromycin and clarithromycin?

Both ABs and the food above are __________

Back 168

Grape Fruit juice

CYP450-3A4 inhibitors

Front 169

Macrolides especially clarithromycin CANNOT be combined with ____________ (an antipyschotic med) - can cause death.

Back 169

Pimozide

Front 170

What Antibiotics cannot be combined with the following and why?
Terfenadine (Seldane®)
Astemizole (Hismanal®)
Theophylline
Warfarin
Statins
Midazolam
Cisapride (Propulsid®)
Pimozide (Orap®)
Bromocriptine (Parlodel®)
Carbamazepine (Tegretol®)
Cyclosporine (Sandimmune®)

Back 170

Macrolides, particularly erythromycin and clarithromycin

they are 3A4 & 2C9 inhibitors and will cause Increase in drug levels -- nasty/fatal consequences

Front 171

Name that Antibiotic:
1. Indications - Periodontal Abscesses, URIs, LRIs, skin and soft tissue, occasionally oral infections
2. Unique Feature - taken up by phagocytes and delivered by them to the infected site
3. Very Expensive
4. ****NO CYP450- 3A4 Interactions*** -- ONLY macrolide that has this property

Back 171

Azithromycin (Zithromax)

Front 172

1. This Antibiotic Class is infamous for CHELATING divalent and trivalent cations
2. Problems in developing teeth when mother takes it while preggo

Back 172

Tetracyclines

Front 173

This antibiotic must not be taken with milk or Iron supplements - it will lower the blood levels of antibiotic

Back 173

Tetracyclines

Front 174

Name that Antibiotic:
1. Very broad spectrum
2. Bacteriostatic
3. Inhibits 30s bacterial ribosomal subunit
-->binds aminoacyl-tRNA synthetases to ribosomal receptor
4. Other effects: inhibit tissue collagenases and metalloproteinases
5. Other effects: Enhance periodontal reattachment and bone formation

Back 174

Tetracyclines

Front 175

What is the main UNIQUE feature of tetracyclines (where do they concetrate)?

Back 175

They will be concentrated in gingival crevicular fluid

Front 176

Name that antibiotic:
1. Mechanism of action - 50S
ribosome, protein synthesis
inhibitor
2. Absorption - nearly 100% PO
Actively transported into
macrophages and WBC providing high [ ] in abscesses and bone (similar to Azithromycin)
3. Uses: Prophylactic endocarditis and joint regimens, patients allergic to penicillin, Endodontist love this antibiotic

Back 176

Clindamycin

Front 177

1. What antibiotics can causes pseudomembranous colitis?
2. Whats the treatment?
3. Should you use narcotics as therapy

Back 177

1. Clindamycin, cephalosporins, and other broad spectrum ABs
2. Vancomycin or Metranidazole
3. NO - its contraindicated

Front 178

Name that antibiotic:
1. Indications: Trichomonas, amebic infections, Giardia, and anaerobic bacterial infections
2. MOA - bacterialcidal --> disrupt bacterial DNA
3. Uses - **Highly effective against anaerobic bacteria **
-> Perio, endo, oral surgery
--> Most often given with Pen V
4. ADR - CYP450-2C9 inhibitor
-->Disulfram effect with EtOH
--> Warafin --> Increases levels --> bleeding

Back 178

Metranidazole

Front 179

Name that Antibiotic:
1. Inhibits bacterial DNA gyrase
2. Bacterialcidal
3. Spectrum: Facultative gram negative Bacteria, but not strict anaerobes
4. Absorption: Inhibited by divalent and trivalent cations (like tetracyclines)

Back 179

Fluoroquinolones - Ciprofloxacin

Front 180

Fluoroquinolone ADRs
1.?
2.?

Back 180

1. Increased photosensitivity (like tetracyclines)
2. CYP450 - 1A2 inhibitor

Front 181

T/F - Dental procedures cause the most cases of Endocarditis

Back 181

False - cause ~4% of the cases

Front 182

In which cases Are Prophylactic antibiotics for Endocarditis Indicated/reasonable?
1. Prosthetic cardiac valve or prosthetic material used for valve repair
2. Previous infective endocarditis
3. Unrepaired cyanotic CHD including palliative shunts and conduits
4. Completely repaired congenital heart defect with prosthetic material -- 6 months after surgery
5. Repaired CHD with residual defects adjacent to the site of prosthetic patch
6. Ventricular-septal defect
7. Heart transplants - no valvulopathy
8. Mitral valve prolapse
9. Pacemakers placed
10. CABG patients
11. Functional or innocent murmurs

Back 182

1-->6 -- prophy indicated
7-->11 -- prophy is not indicated

Front 183

For those patients who are indicated for Endocarditis prophy, what procedures are indicated for prophy? (VERY general)

Back 183

those that cause gingival or mucosal bleeding

Front 184

1997/2007 Endocarditis Prophy Recommendations
1. Non-Pen Allergy
2. Pen allergy
3. When to take

Back 184

1. Standard: Amoxicillin 2 grams (50 mg/kg Peds)

2. Penicillin Allergic: -->Clindamycin 600 mg (20 mg/kg Peds)

-->Azithromycin or Clarithromycin 500 mg (15 mg/kg Peds)

-->Cephalexin or Cefadroxil 2 grams‡ (50 mg/kg Peds)

3. All regimens one hour before procedure

Front 185

Joint Prophylaxis Regimens
1. Non-pen allergic
2. allergic to Pen
3. What type of bacteria are these trying to target?

Back 185

Not Allergic to Penicillin:
-->Cephalexin 2 grams
or
-->Cephradine 2 grams
or
--> Amoxicillin 2 grams

2.Allergic to Penicillin:
-->Clindamycin 600 mg
3. Staphylococcal infections

Front 186

1. Fungal membranes have _________ which is very close in structure to cholesterol
2. This causes problems with systemic dosing of antifungals because there is lower __________

Back 186

1. Ergosterol
2. Selective toxicity

Front 187

1. 3 things in fungi are close to humans which antifungals attack

Back 187

1. Ergosterol close to cholesterol
2. RNA similar to humans
3. CYP450 is similar to humans

Front 188

3 reason why fungal infections are becoming more prevalent

Back 188

1. Increased AIDS/HIV infection
2. Patients undergoing chemotherapy
3. Increased use of broad spectrum antibiotics

Front 189

Name that anti-fungal:
1. MOA - punches holes in membranes with ergosterol - binds ergosterol
2. Can be used as an antibiotic
3. Very large structure like macrolide antibiotics
4. Administration routes - orally (rinse), systemically, lozenge

Back 189

Amphotericin B

Front 190

T/F - oral rinse/lozenge amphotericin B is not absorbed systemically

Back 190

True

Front 191

1. IV formulation - very nasty drug to give via IV
2. Nephrotoxicity is the dose-limiting factor
3. MOA - binds ergosterol

Back 191

Amphotericin B - IV formulation = Amphotec ®

Front 192

T/F - amphotericin has greater affinity for ergosterol than for cholesterol
--> if it hits ergosterol it will leave lipsome
--> if it hits cholesterol it will stay in liiposome

Back 192

True

Front 193

Name that Anti-fungal
1. Similar to Amphotericin B
2. Also can be used as anti-biotic - binds membranes (ergosterol)
3. There is NO IV formulation
4. Used for Candida infections and stomatitis
5. Huge polar molecule that won't get absorbed systemically
6. Major problem = AWFUL taste

Back 193

Nystatin (Mycostatin ®)

Front 194

Name that anti-fungal
1. Binds to fungal RNA inhibits DNA and RNA synthesis
2. Active metabolite, 5-flurouracil, is actually an anticancer drug

Back 194

Fluorocytosine or Flucytosine

Front 195

Name that anti-fungal:
1. Mitotic spindle poison
2. used for nail infections
3. Major Side effect - can lower count of blood cells
4. Unique - **BEST absorbed when taken with fatty meals**
5. It is a CYP450 inducer -- lowers warfarin levels

Back 195

Griseofulvin

Front 196

Name that class of anti-fungal
1. much better therapeutic index than amphotericin or flucytosine
2. MOA - work by inhibiting cytochrome P-450 in the fungus, which in turn blocks the conversion of lanosterol to ergosterol
3. **Many drug interactions because it inhibits CYP450 3A4**

Back 196

Azoles

Front 197

Name the anti-fungal
1. greatest affinity for human CYP-3A4
2. It is best absorbed at lower gastric pHs (increased acidity) and it is thus recommended that it be taken with acidifiers such as orange juice or with a meal.
3. decrease the synthesis of human adrenal and gonadol steroid hormones--> gynecomastia (enlarged breasts in men), infertility and menstrual irregularities

Back 197

Ketoconazole (Nizoral®) and Itraconzole (Sporanox®)

Front 198

Name that Anti-fungal
1. most commonly prescribed systemic azole
2. used frequently in oropharyngeal and esophageal candidiasis, especially in AIDS
3. good penetration into the central nervous system, which is unlike ketoconazole or itraconazole
4. lowest affinity for human cytochrome P-450

Back 198

Fluconazole (Diflucan®)

Front 199

Name that Anti-fungal
1. Topical antifungals marketed as creams and suppositories to treat vaginal candidiasis

Back 199

Clotrimazole (Lotrimin® and Mycelex®) - available as lozenge
Miconazole (Monistat®)

Front 200

These drugs are used for the treatment of _______?
1. Acyclovir (Zovirax®)
2. Valacyclovir (Valtrex®)
3. Ganciclovir (Cytovene®)

Back 200

Herpes Virus treatments

Front 201

Name that Anti-viral:
1. Major drug directed against Herpes Simplex and Varicella virus including genital and labial herpes
2. requires 3 phosphorylation steps (the first using viral enzymes, the next two using host cell enzymes)
3. inhibits viral DNA synthesis - with triphosphate form of drug
4. Only infected cells phosphorylate the parent compound
5. Anti-herpes

Back 201

Acyclovir (Zovirax®)

Front 202

Name that anti-viral
1. Prodrug rapidly converted to Acyclovir by first pass effects in gastrointestinal tract and liver. 2. Everything else is similar to Acyclovir.
3. Anti-herpes

Back 202

Valacyclovir (Valtrex®)

Front 203

Name that anti-viral:
1. Similar to Acyclovir with 100 times the potency and greater selectivity for the Cytomegalovirus (CMV)
2. Anti-herpes meds
3. Bone marrow suppression including neutropenia, anemia and thrombocytopenia can occur with this drug

Back 203

Ganciclovir (Cytovene®)

Front 204

Cocktail normally given to HIV/AIDS patient

Back 204

1. Two reverse transcriptase inhibitors
2. Protease Inhibitor

Front 205

These drugs are in the ________ class of __________
1. Zidovudine (AZT, Retrovir®)
2. Didanosine (DDI, Videx®)
3. Lamivudine (Epivir®)
4. Efavirenz (Sustiva®)

Back 205

1. Reverse Transcriptase inhibitors
2. Anti-virals

Front 206

Name that Anti-viral
1. Inhibits the synthesis of viral DNA from RNA and ultimate HIV replication.
2. Reverse transcriptase inhibitor
3. Major toxicity is bone marrow suppresion

Back 206

Zidovudine (AZT, Retrovir®)

Front 207

Name the anti-viral:
1. Most often combined with Zidovudine --> reduces HIV resistance
2. Major toxicity = dose-dependent pancreatitis
3. Reverse transcriptase inhibitor

Back 207

Didanosine (DDI, Videx®)
OR
Lamivudine (Epivir®) - less pancreatitis

Front 208

Name that anti-viral
1. new non-nucleotide reverse transcriptase inhibitor
2. Better tolerated than other drugs of this class
3. part of a triple drug regimen when protease inhibitors are contraindicated.

Back 208

Efavirenz (Sustiva®)

Front 209

HIV drug class where large polyproteins are produced that need to be cleaved by a viral encoded protease for final assembly by the mature virion --Inhibit the process

Back 209

Protease inhibitors

Front 210

1. Drugs in class are:
a. Indinavir (Crixavan®)
b. Ritonavir (Novir®)
c. Saquinavir (Invirase®)
2. produce elevated blood glucose and lipids, plus lipodystophy (a peripheral fat wasting with central adiposity). 3. Diarrhea is also frequent with these drugs.
4. Cytochrome P-450 inhibition is common
5. Used as HIV drug

Back 210

Protease Inhibitors

Front 211

Drug class for anti-virals:
1. work by preventing HIV from entering healthy CD4 cells
2. CCR5 receptor is located on other immunocompetent cells, there is a theoretical risk of developing life-threatening infections and cancers while on this drug

Back 211

Entry and Fusion Inhibitors

Front 212

Name that anti-viral
1. Entry and fusion inhibitor
2. MOA - attaching themselves to proteins (CCR5 receptor) on the surface of the CD4 cells

Back 212

Maraviroc (Selzentry®)

Front 213

Name that anti-viral:
1. MOA - bind to proteins (gp120 or gp 41) on the on the HIV surface
2. injectable agent given twice per day subcutaneously
3. Can develop bacterial pneumonia on this drug

Back 213

Enfuvirtide (Fuzeon®)

Front 214

Name that anti-viral
1. MOA - blocks the incorporation (or integration) of the new form viral DNA (via reverse-transcriptase) into the CD4 cell’s DNA
2. NOT prescribed in conjunction with STATIN - due to increased muscle pain

Back 214

Integrase Inhibitor - Raltegravir (Isentress®)

Front 215

Name 2 anti-flu drugs (NOT neurominidase inhibitors)
1. Drugs directed against influenza virus
2. Most effective when taken at first sign of flu symptoms
3. Both drugs inhibit the viral uncoating process

Back 215

Amantadine (Symmetrel®) and Rimantadine (Flumadine)

Front 216

1. Anti-parkinson's drug that is used to treat the flu
2. Increases dopamine levels

Back 216

Amantadine

Front 217

1. Anti-flu drugs
2. Neurominidase inhibitors
-->Inhibits enzyme on the surface of the influenza virus that plays an essential role in the release of viruses from infected cells

Back 217

Zanamivir (Relenza®) - available as inhalant

Oseltamivir (Tamiflu®) - only in pill form

Front 218

1. What claims can herbals and supplements make?

2. What claims can herbals and supplements NOT make

Back 218

1. Maintenance of health - based on structure/function claims
2. Cannot claim treatment of specific disease state

Front 219

1. Are herbals classified as drugs or foods?
2. What must they provide to FDA?

Back 219

1. Foods
2. Safety - very minimal data

Front 220

What herbal was removed from the market because it contained ________, an indirect sympathomimetic

Back 220

1. Ma Haung
2. Ephedra

Front 221

T/F - If the FDA or some 3rd party challenges the claims made by herbal company they are urged to provide evidence but are NOT required to substantiate the claims

Back 221

False - must substantiate or remove it

Front 222

Name that Herbal:
1. Topical use - anesthetic and antimicrobial; found in many moisturizers; used for burns
2. Oral - used as laxative - irritating to large intestine
3. **May inhibit absorption of other oral meds***

Back 222

Aloe vera

Front 223

Name that herbal:
1. Uses: improve immune function, strengthen cardio system, improve memory
2. Adverse Rxn - Inhibts platelet aggregation/coagulation, Reduces blood glucose
3. Drug Interactions - Additive hypoglycemia (hypoglycemi-ER) when on other diabetes meds

Back 223

Astragalus (huang chi, milk vetch)

Front 224

Name that Herbal:
1. Uses - astringent used to treat inflammation of mouth and throat, may treat diarrhea when in tea
2. Claims to treat Diabetes Retinopathy - need more evidence
3. Adverse Rxn - mild anti-platelet activity
4. Drug interactions - mild hypoglycemia with other diabetes meds

Back 224

Bilberry fruit (Huckleberry, European blueberry)

Front 225

Name that herbal:
1. Used widely in China as female health tonic
2. Uses - PMS, menopause, Fibrolytic breast cancer
3. Adverse Rxns - hypotension and anti-platelet activity in excessive doses; Photosensivity
4. Drug interactions - increases hypotension with BP meds, increases anti-platelet effects with blood thinners (e.g. warfarin)

Back 225

Dong quai (Chinese angelica)

Front 226

Name that Herbal:
1. Uses - immune system booster; coughs, colds, flu, infections
2. Adverse Rxns - aggravates autoimmune disorders (lupus, AIDS), other collagen disorders, tuberculosis
3. Drug interactions - May counteract immunosuppressive drugs (corticosteroids, cyclosporine, anti-cancer meds)

Back 226

Echinacea (Purple cornflower)

Front 227

Name that Herbal:
1. Uses - digestive aid, hypertension, hyperlipidemia, lower LDL and triglycerides, Raise HDL
2. Adverse Rxns - allergic respiratory and skin rxns; bleeding from anti-platelet aggregation
3. Drug Interactions - anti-platelet, anti-coagulants --> increased bleeding risk

Back 227

Garlic (Allium, stinking rose)

Front 228

Name that Herbal:
1. ONE of the only herbals scientifically proven to increase cognitive function - improves memory
2. Uses - Alzheimer's, Dementia, vertigo, peripheral artery occlusion
3. Adverse Rxns - anti-platelet activity, GI upset, headache
4. Drug Interactions - anti-platelet drugs --> increased bleeding risk

Back 228

Gingko biloba (Maidenhair tree)

Front 229

Name that Herbal:
1. Active components = lactones --> muscle relaxants, anticonvulsants, anti-anxiety
2. Uses - nervousness, insomnia, tension, stress and agitation
3. Orally - has local anesthetic activity
4. Adverse Rxns - LA activity causes numbness of oral mucosa, psychomotor impairment/drowsiness, scaly skin/rash
5. Drug Interactions - supra-additive/additive effects with other CNS depressants (EtOH, diazepams)

Back 229

Kava-kava

Front 230

Name that Herbal:
1. Scientific data showing improvement of prostate health
2. Uses - anti-inflammatory and testosterone-moderating effects (inhibits dihydroxytestosterone), bladder irritability
3. Adverse Rxns - Mild GI upset, may delay diagnosis of prostate cancer
4. Drug Interactions - possible with other hormone drugs

Back 230

Saw palmetto (Sabal)

Front 231

Name that Herbal:
1. Better studied supplement
2. Uses - efficacy in moderate to mild depression, PMS cramps, skin injuries/inflammation topically
3. Adverse Rxns - Photosensitivity, headache, GI upset
4. Drug interactions - ***Induces CYP3A4 and CYP1A2 isoforms in GI tract and liver --> decrease blood levels of lots of drugs including oral contraceptives, statins, cyclosporine and warfarin

Back 231

St. John’s Wort

Front 232

What receptors will histamine stimulate?

Back 232

H1, H2, H3

Front 233

Describe the triple response

Back 233

1. Red, raised area at injection site = capillary vasoconstriction
2. edematous area around injection site - BV's become leaky
3. Diffuse red area - called flare area = histamine activating nerve endings

Front 234

1. H1 receptor stimulation elicits _______? (very general)
2. H2 receptor stimulation causes _______?
3. H3 receptor stimulation causes ______?

Back 234

1. Classic allergic response
2. Gastric acid secretion
3. Reduced release of histamine in brain found PRE-SYNAPTICALLY

Front 235

Modifications to histamine structure:
1. Methylation @ C2 -->
2. Methylation @ C4 -->
3. Methylation @ NH2 on aliphatic chain -->

Back 235

1. Specific H1 stimulation
2. Specific H2 stimulation
3. --> (R-alpha methyl histamine) Specific H3 stimulation

Front 236

Classic Antihistamines have 2 functions (what receptors do they hit?)

Back 236

1. Block Histamine receptors
2. Anti-Muscarinic activity
- dry mouth
-**Drowsiness - block Ach**

Front 237

What are 4 functions/treatment uses for Diphenhydramine?

Back 237

1. Allergy
2. Parkinson's Disease - Blocks Ach
3. Anti-Emetic/motion sickness - blocks Ach vomiting center
4. Local Anesthetic

Front 238

Histamine is an ___________, chemical naturally produced by the body

Back 238

autocoid

Front 239

T/F - Mast cells contain H1 receptors

Back 239

False - they contain H2

Front 240

T/F - Tissues that Mast cells act upon contain H2 receptors

Back 240

False - they contain H1

Front 241

Name the receptor subtype:
1. Found in SM, endothelium, brain
2. 2nd messengers - Inositol, DAG
3. Response - vasodilation, urticaria, triple response, bronchoconstriction, hypotension, reflex tachycardia, pain, diarrhea

Back 241

H1 receptor

Front 242

Name that receptor subtype:
1. Found in - gastric mucosa, mast cells, brain, cardiac muscle
2. Agonist - 4 -methyl histamine
3. Second messenger - cAMP
4. Response - HCl and pepsinogen release, positive inotorpic and chronotropic effects

Back 242

H2 receptor

Front 243

Name that receptor subtype:
1. Found in - pre-synaptic neurons in the brain
2. Agonist - R-alpha methyl histamine
3. 2nd messenger - G proteins
4. Response - Decreased NT release in brain, may increase appetite, maintain wakefulness, decreased Ca influx

Back 243

H3 receptor

Front 244

1. Histamine release and stimulation of allergic response proceeds thru the ______ pathway (antibody).

Back 244

1. IgE --> mast cell degranulation

Front 245

T/F - Anti-histamines are good for treating asthma

Back 245

False

Front 246

T/F - 2nd generation anti-histamines cross the Blood brain barrier while 1st generation anti-histamines do NOT cross BBB

Back 246

False - 1st gens cross BBB

Front 247

1.Treatment for motion sickness should involve antagonism of which type of receptor?
2. What class of drug would you use to do achieve this?

Back 247

1. Block Ach in vestibular system
2. 1st gen anti-histamine --> crosses BBB to block muscarinic receptor

Front 248

What 2 powerful sedatives used in Dental sedation (mainly of Peds cases) are anti-histamines

Back 248

1. Chloral hydrate
2. Promethazine

Front 249

1. Promethazine has 3 functions (effects multiple receptor types)
2. What Disease must NEVER be treated with Promethazine?

Back 249

1. anti-histamine, anti-cholinergic, anti-dopaminergic
2. Parkinson's disease - b/c of anti-Ach and Anti-dopa functions

Front 250

Name anti-histamine class:
1. Contains drugs - diphenhydramine and Dimenhydrinate (Dramamine)
2. most pronounced anti-cholinergic effects
3. Good treatment for Parkinson's

Back 250

Ethanolamines

Front 251

Name that class of anti-histamines:
1. Drugs in class - Pyrilamine and Triplenamine
2. Pretty strong anticholinergic activity.
3. They are popular drugs for available OTC sleeping aids

Back 251

Ethylenediamines

Front 252

Name that class of Anti-histamines:
1.Drugs in class:
i. Meclizine (bonine)
ii. Cylcizine
iii. Hydroxyzine – more sedating that previous 2
2. Cause little sedation
3. Excellent anti-motion activity b/c anti-cholinergic effects

Back 252

Piperazines

Front 253

Name that class of Anti-histamines:
1. They are OTC cold remedies mainly b/c of anticholinergic activity
2. Drugs in class - chlorpheniramine -- very similar to Dimeatapp
3. Dries Nasal passages

Back 253

Alkylamines

Front 254

Name that class of Anti-histamines:
1. Drug example - Promethazine
2. good antiemetic for drug induced vomiting and motion sickness
3. Both Anti-Ach and Anti-dopa activity
4. **alpha1 blockage so SEs can include postural hypotension**
5. Side FX - extrapyramidal effects, CYP450-2D6 inhibitor

Back 254

Phenothiazides

Front 255

Name that class of Anti-histamines:
1. Drugs -
a. Fexofenadine (allegra)
b. Loratidine (Claritin)
c. Cetirizine (Zyrtec)
2. NOT cardiotoxic
3. Do NOT cause a lot of antimuscarinic effects
4. Do NOT cross BBB

Back 255

2nd generation H1 receptors blockers

Front 256

1. Emergency drug used for laryngospasm
2. Rec Dose

Back 256

1.Succinylcholine (Anectine)
2. 10-40 mg IV

Front 257

1. Emergency Drugs for asthmatic attack? (name 3)
2. Rec dose

Back 257

1. B-2 agonists like -
i. Albuterol (Proventil)
ii. Metaproterenol (Alupent)
iii. Terbutaline (Brethaire)
2. 2-puffs off inhaler

Front 258

1. Emergency Drug used to treat Acute Angina attack
2. Rec Dose
3. How many doses can be given?
4. What are 2 side fx?

Back 258

1. Nitroglycerine (Nitrostat)
2. Treatment --> 0.15 – 0.60 mg sublingually
3. 3 doses
4. Orthostatic hypotension & methemhemoglobinemia

Front 259

1. Emergency Drugs given for Allergic Rxns
2. Rec Dose

Back 259

1. Diphenhydramine for mild attack; Epinephrine for severe attack
2. Diphenhydramine - 10-15 mg IM or 25-50 mg PO
3. Epinephrine (Adrenaline) → 1:1000 (1 mg/ml)

Front 260

1. Emergency Drug Given for Convulsions
2. Rec Dose
3. Realistically what do you want to do?

Back 260

1. Diazepam
2. 10 mg (slowly) – 2 mg/min – IV
3. 1st – get everything out of there mouth
2nd – clear the area and put them in to safety position

Front 261

1. Emergency Drug used to prevent additional platelet aggregation during MI
2. Rec Dose

Back 261

1. Aspirin --325 mg PO (If conscious)

Front 262

1. Recommended Drugs and Dose used to treat pain from MI

Back 262

1. Morphine → 10 mg IM
2. Meperidine (Demerol) → 50-100 mg IM
3. Nitrous Oxide/O2 → 50% by inhalation

Front 263

1. If you use opiod you must have ________ and _________in office in case of respiratory depression
2. Rec Dose

Back 263

1. Naloxone and Naltrexone
2. Dose → 0.4 mg IM or IV followed by 50 mg naltrexone PO when patient become conscious

Front 264

1. Emergency drugs and doses used for treatment of hypoglycemia

Back 264

1. Conscious pt- give sugar- orange juice, cake icing
-->3-4 ounces PO every 5 minutes until symptoms are gone
-->Cake icing can be place sublingually
Unconscious- glucagon 1mg IM

Front 265

1. Emergency drug used to treat poisoning
2. Rec Dose

Back 265

1.Syrup of ipecac (Emetine)-
2. Dosing – 15-30 mg PO

Front 266

T/F - Ipecac (Emetine) works best on empty stomach

Back 266

False - works better if taken with full glass of water

Front 267

1. Anti-muscarinic drugs used to treat GI ulcers/symptoms
2. Side FX of these drugs?

Back 267

1. Atropine and Pirenzepine
2. Xerostomia, Dry eye, Mydriasis, increased HR and contraction force, NO sweating

Front 268

1. Anti-histamine drugs used to treat GI ulcers/symptoms

Back 268

1. H-2 blockers -
1. Cimetidine (Tagamet)
2. Ranitidine (Zantac)
3. Famotidine (Pepcid)
4. Nizatidine (Aczid)

Front 269

1. Side Fx of H2 blockers - mainly with Cimetidine (Tagament)

Back 269

1. Anti-androgen effects like gynecomastia, galactorrhea in women
--> (elevations in prolactin/endometriosis/cross BBB)
2. Inhibits cyp 450 3A4 enzymes

Front 270

1. Prostaglandin Agonists/analogs used to treat GI ulcer/symptoms
2. Are these recommended and why?

Back 270

1. Misoprostol (Cytotec) and Arthrotec (combination of Diclofenac/Misoprostol)
2. NO - misoprostol is an abortofactant - induces uterine contractions

Front 271

1. Proton-Pump Inhibitors used to treat GI ulcer/symptoms

Back 271

1. Omeprazole (Prilosec)
--> (used to txt heart burn and dyspepsia)
2. Lansoprazole (Prevacid)
3. Esomeprazole (Nexium)
-->a. Active isomer (S) of omeprazole

Front 272

Omeprazole is processed by ____________ so can have drug accumulation with an inhibitor on board too

Back 272

CYP 450 2C9 - same as diazepam, warfarin, etc

Front 273

Name the New Side Effect seen in women when on chronic high dose PPI’s

Back 273

→ Osteoporosis

Front 274

2 Drugs used to treat H. pylori and GI ulcer symptoms as combo drugs?
1. _______ = clarithromycin + bismuth + ASA
2. _______ = amoxicillin + bismuth + ASA

Back 274

Biaxin = clarithromycin + bismuth + ASA
Trimox = amoxicillin + bismuth + ASA

Front 275

1. Antacids are salts of _________ (4 of them)
2. Tums = _______
3. Side Fx of _________ = diarrhea
4. Side Fx of ________ = constipation
5. Maylox and Mylanta are 50/50 mixes of these 2 cations ____ & _____?

Back 275

1. Salts of Al, Mg, Ca, or Na
2. Calcium carbonate
3. Mg
4. Al
5. Mg and Al

Front 276

1. __________ is a "crater filler" used for people who can't tolerate H2 blockers or PPI's
2. What is the molecule made up of (2 things)?
3. What is the consequence of its make up?

Back 276

1. Sucralfate (carafate)
2. Sucrose with many Al cations sticking off of it
3. Lots of Al --> causes extreme constipation

Front 277

Name that GERD drug:
1. Prokinetic class
2. Stimulates Peripheral cholinergic receptors
3. Increase contraction of esophageal sphincter
4. Relaxes duodenal sphincter
5 ***Increases Peristalsis***
6. **Blocks Dopaminergic Receptors**

Back 277

Metoclopramide (Reglan).

Front 278

Name that GERD drug:
1. Increases peripheral action of Ach
2. Prokinetic drug
3. Many many problems with this drug
4. i. Inducing cardiac arrhythmias
ii. Torsades de pointes
iii. CYP450-3A4 interactions
iv. High incidence of ventricular arrhythmias

Back 278

Cisapride

Front 279

Name that Anti-Emetic drug:
1. Anti-dopaminergic
2. Used for drug-induced vomiting
3. In phenothiazide class (with Promethazine)

Back 279

Prochlorperazine (compazine)

Front 280

Name that Anti-Emetic drug:
1. Anti-dopaminergic
2. Used for drug-induced vomiting
3. rectal suppository admin (it is for projective vomiting)

Back 280

trimethobenzamide (tigan)

Front 281

Name that Anti-Emetic drug:
1. Anti-dopaminergic
2. Used for drug-induced vomiting
3. Anti-histamine
4. Anti-cholinergic
5. Anti-dopaminergic
6. Used in Sedation of children

Back 281

Promethazine (Phenergan)

Front 282

Name that Anti-Emetic drug:
1. Anti-dopaminergic
2. Used for drug-induced vomiting
3. Prokinetic drug used to treat GERD
4. If you push dose it starts blocking 5-HT receptors

Back 282

Metoclopramide (reglan)

Front 283

Name that Anti-Emetic:
1. Seretonergic blocking agent
2. Good for drug-induced vomiting
3. Used for anti-cancer chemo-induced vomiting
4. Major drug given pre-infusion of cancer chemotherapy agent.
5. Used for severe vomiting caused by opioids and LA drugs too.

Back 283

Ondansetron (zofran)

Front 284

Name that Anti-Emetic:
1. Seretonergic blocking agent
2. Good for drug-induced vomiting
3. Used for anti-cancer chemo-induced vomiting
4. Active ingredient in Marijuana
5. Blocks 5HT-3 as well as cannibanoid receptors

Back 284

Dronabinol (marinol)