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Pharm exam 3
Pharm exam 3
164
Medical
Professional
04/11/2011

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Term
uses for prostaglandins
Definition
• Protecting mucous membrane in the GI tract
• Circulatory system to keep PDA open
• Erectile dysfunction
• Glaucoma
• Abortifactant
Term
Production usually accompanies the production of histamine
---involved in asthmatic & allergic reactions (act to sustain inflammatory reactions)

Bronchonstriction
 Vascular permeability
 Secretion of mucus
Infiltration of inflammatory cells
Definition
Leukotrines
Term
leukotriene antagonists
Definition
prophylaxis of asthma (but not for quick relief of bronchoconstriction)
Term
• Will not work for rescue inhaler
Definition
leukotriene antagonists
Term
histamine is found
Definition
Increased concentration in Respiratory tract, GI tract, Skin
Also high concentrations in mast cells and basophils
Term
 Stimulation of gastric acid secretion
Definition
Histamine 2 Receptors
Term
Histamine 1 Receptors adverse effects
Definition
• ↑ Production of nasal & bronchial mucus
• Constriction of bronchioles
• Symptoms of asthma & decreased lung capacity
• Contraction of Intestinal Smooth Muscle
• GI cramping & diarrhea
• Sensory Nerve Endings
• Itching & pain
Term
antihistamines
Definition
• Block the receptor mediated response in target tissues
Term
1st generation antihistamines
Definition
effective
low cost
• Interact with histaminic, muscarinic/cholinergic, alpha adrenergic, and serotonin receptors
Term
2nd generation antihistamines
Definition
more specific for H1 receptors
Term
more specific for H1 receptors
Definition
2nd generation antihistamines
Term
Treatment of choice for allergic rhinitis and urticaria
Definition
antihistamines
Term
Treatment/prevention of motion sickness
Definition
antihistamines
Term
adverse effects of 1st generation antihistamines
Definition
sedation
dry mouth
blurred vision
Term
o 2nd generation antihistamines
Definition
lower adverse effects
Term
antihistamines interactions
Definition
alcohol, muscle relaxers, cholinesterase inhibitors
Term
Drug Interactions for antihistamines
Definition
CNS depressants
MAOIs
cholinesterase inhibitors
Alzheimer's medications
Term
5-HT 1D receptor agonists
Definition
triptans
Term
vasoconstriction or inhibit release of proinflammatory neuropeptides
Definition
triptans
Term
adverse effects of triptans
Definition
CV incidents
increased BP
Term
aspirin as an antiplatelet
Definition
Inhibits COX-1 and thromboxane A2 synthesis
Platelet cannot synthesize
Term
Prophylaxis of TIA and MI, reduces mortality of MI
Definition
aspirin
Term
ADP inhibitors
Definition
– Irreversibly inhibit the binding of ADP to its receptors on platelets (inhibiting the activation of the GP IIb/IIIa receptors)
Term
ADP inhibitors
Definition
– Reduces the possibility of platelet aggregation
Term
uses for ADP inhibitors
Definition
– Prevention of atherosclerotic events following recent myocardial infarction, stroke, or established peripheral arterial disease
– Prophylaxis of thrombotic events in acute coronary syndromes
Term
AE of ADP inhibitors
Definition
– Thrombotic thrombocytopenic purpura (TTP)
– Neutropenia
– Bleeding
Term
GPIIb/IIIa inhibitors
Definition
– Binds to GP IIb/IIIa receptors & blocks the binding of fibrinogen
Term
– Decrease the incidence of thrombotic complications associated with acute coronary syndromes
Definition
GPIIb/IIIa inhibitors
Term
Cornonary vasodilator
Definition
dipyridamole
Term
dipyridamole
Definition
• Increases intracellular of cAMP, resulting in decreased synthesis of thromboxane A2 & the inhibition of platelet aggregation
Term
• Typically used in combination with another medications for antiplatelet effects
Definition
• Aspirin + dipyridamole (Aggrenox®)
Term
– Accelerates interaction of antithrombin III & thrombin (leading to acclerated inactivation of thrombin); prevents conversion of fibringogen to fibrin
Definition
Heparin
Term
• Prophylactically to prevent postoperative venous thrombosis in patients undergoing elective surgery
Definition
Heparin
Term
• Requires monitoring aPTT
Definition
Heparin
Term
• Does NOT cross the placenta
Definition
Heparin
Term
Low Molecular Weight Heparins (LMWH)
Definition
– Better bioavailability with more predictable absorption & effects
– Doesn’t require monitoring of bleeding times
Term
• Disadvantages of Low Molecular Weight Heparins (LMWH)
Definition
– Not reversible
Term
• Adverse Effects of Heparin an LMWH
Definition
bleeding
hypersensitivity reactions
thrombosis
thrombocytopenia
Term
vitamin K antagonist
Definition
Warfarin (coumadin)
Term
– Prevention of progression or recurrence of acute DVT or PE after initial heparin treatment
Definition
vitamin K antagonists
Warfarin (Coumadin®)
Term
used Prophylactically for patients with acute myocardial infarction, prosthetic heart valves, or chronic a. fib
Definition
Warfarin (Coumadin®)
Term
used in chronic a. fib
Definition
vitamin k antagonist (coumadin)
Term
AE of thrombolytics
Definition
hemorrhage
Term
thrombolytics
Definition
may also dissolve beneficial clots
Term
• Dissolve blood clots by activating plasminogen (forming plasmin).
Definition
thrombolytics
Term
drugs used to treat prolonged bleeding due to heparin
Definition
Protamine
Term
drugs used to treat prolonged bleeding due to Warfarin
Definition
Vitamin K
Term
drugs used to treat prolonged bleeding due to LMWH
Definition
fresh frozen plasma
Term
• Folic acid
Definition
reverse hematologic abnormality but will MASK vitamin b 12 deficiency leading to severe neurological dysfunction and disease
Term
• Vitamin B12 deficiency OR Folate deficiency seen in
Definition
macrocytic anemia
Term
treatments for types of anemia
Definition
• PO Iron Therapy
• Parenteral Iron Therapy
• Colony Stimulating Factors (G-CSF)
Term
• Colony Stimulating Factors (G-CSF)
Definition
– Filgrastim (Neupogen®)
Term
drug given for Chemotherapy-induced Anemia
Definition
– Erythropoietin Alpha (Epogen®)
Term
chemotherapeutic drugs
Definition
• Augmented drug extrusion-increased p-glycoprotein that removes drug from cells
• Changes in cellular targets of drugs• Changes in transport or activating enzymes
• Increased ability for DNA repair
Term
adverse effects of chemotherapeutic drugs
Definition
– Infertility
– Hair loss
– Bone marrow, neutropenia
Term
minimize adverse effects of chemotherapeutic drugs
Definition
– Direct perfusion of the tumor with a chemotherapy agent (instead of systemic administration)
– Bone marrow harvest prior to therapy for implantation later (if needed)
– Intensive hydration & diuresis for bladder protection (if needed)
– Reversal of neutropenia with filgrastin
Term
most common principle of combination chemotherapeutic drugs
Definition
– Synergistic effects from 2 different MoA to treat the cancer
– Minimize organ toxicity by using lower doses
– Prevent resistance
Term
damage DNA &/or proteins in the cell, causing inhibition of replication
 Inhibition of DNA replication because interlined strands do not separate
Definition
alkylating agents
Term
AE of cyclophosphamide (alkylating agents)
Definition
 If cells are not killed, mutations occur making this class more likely to be carcinogenic (secondary malignancies like leukemia)
 Secondary malignancy

 Bone marrow suppression is the dose-limiting AE
Term
 Hemorrhagic cystitis (due to acrolein, may lead to fibrosis of the bladder)
Definition
Cyclophosphamide
Term
 Acts in any phase of the cell cycle, but cancer cells in the G1 & S phases are more susceptible
Definition
Platinum agents
Term
adverse effects of platinum agents
Definition
 Severe, persistent vomiting (esp. with Cisplatin)
 Dose-related nephrotoxicity
 Otoxicity
 Neuropathy
Term
 Effective in S2 & G phases

 Uncoiling of DNA & blocking of DNA & RNA synthesis
 Oxidative damage
Definition
anthracyclines
Term
adverse effects of anthracyclines
Definition
 Cardiotoxicity
red discoloration of urine
Term
AE is Pulmonary toxicity
Definition
bleomycin
Term
topoisomerase 1 inhibitors
Definition
inhibition of the function & synthesis of DNA
Term
adverse effects of TOP-1 inhibitors
Definition
 Myelosuppression

Delayed diarrhea
Term
topoisomerase 2 inhibitors
Definition
 Uncoiling of DNA, DNA ruptures
Term
methotrexate (antimetabolites)
Definition
 Inhibits dihydrofolate reductase (DHFR)
Term
Used as a rescue from methotrexate
Bypasses DHFR enzyme and replaces the folate supply
Definition
leucovorin
Term
 Inhibits DNA polymerase enzyme
 Interrupts chain elongation
Definition
pyrimidine antagonist
Term
vinca alkaloids, taxanes
Definition
microtubule inhibitors
Term
block mitosis in metaphase (M)
Definition
microtubule inhibitors (vinca alkaloids, taxanes)
Term
 Bind to microtubule protein (tubulin) resulting in a dysfunctional mitotic spindle apparatus
Definition
microtubule inhibitors (vinca alkaloids, taxanes)
Term
 Hyperuricemia seen with
Definition
vinca alkaloids
Term
Taxanes AE
Definition
• Dose-limiting neutropenia
• Serious hypersensitivity reactions
• Peripheral neuropathy
Term
 Binds to estrogen receptor but fails to induce estrogen-receptor genes & RNA synthesis
Definition
selective estrogen receptor modulators (SERMs)
Term
adverse effects of SERMs
Definition
 Hot flashes,
 Thromboembolism, endometrial cancer
Term
aromatase inhibitors
Definition
 ↓production of estrogen by preventing the conversion of androstenedione to estrogen in the liver, fat, muscle, skin, & breast tissue
Term
 Occupy the GnRH receptors in the pituitary, leading inhibition of release of FSH & LH
Definition
gonadotropin releasing hormone analogs
Term
androgen antagonists
Definition
 Competes with testosterone for binding to androgen receptors (antagonizes the effects of testosterone and dihydrotestosterone)
Term
 Trigger immune system resulting in cell death through complement-mediated cellular toxicity or the antigen-antibody cell complex is internalized into cancer cell resulting in cell death
Definition
monoclonal antibodies
Term
risk factors for chemotherapy induced nausea & vomiting
Definition
 poor emetic control w/prior chemo, female gender, low chronic alcohol intake, younger age
Term
classes of medications used to treat chemotherapy induced nausea & vomiting
Definition
– 5HT3 antagonist
– corticosteroids
– Benzodiazepines
– Cannabinoids
Term
Arrest growth of invading organism while immune system destroys organism
Definition
 Bacteriostatic
Term
Causes direct death of invading organisms
Definition
 Bactericidal
Term
 Lowest concentration of antibiotic that inhibits bacterial growth; To provide effective antimicrobial actions the drug should exceed the MIC in the appropriate location of the body
Definition
minimum inhibitory concentration
Term
Prophylactic therapy
Definition
 Prevention of infection
Term
Empiric Treatment
Definition
 Treatment of current infection
Term
penicillins
Definition
 Interfere with bacterial cell wall synthesis/repair through penicillin binding proteins (PBP), causing weakening of the cell membrane and cell lysis; bactericidal
Term
 Effective against rapidly growing organisms that synthesize a peptidoglycan cell wall
Definition
penicillins
Term
adverse effects of penicillins
Definition
Allergy- hypersensitivity and rash
Term
classes of antibiotics may be combined for synergistic effects
Definition
 Penicillins & Aminoglycosides
Term
cephalosporins
Definition
 Same as penicillin: Interfere with bacterial cell wall synthesis, causing weakening of the cell membrane and cell lysis; bactericidal
Term
if you are allergic to penicillin, you will most likely be allergic to
Definition
cephalosporins
10% Cross-allergenicity between penicillins & cephalosporins
looks the same as penicillin- most who are allergic are also allergic to cephalosporins
Term
 1st Generation cephalosporins used in
Definition
surgery
Term
3rd generation cephalosporins
Definition
used in meningitis
Term
○ Inhibits synthesis of bacterial cell wall phospholipids, causing the cell wall to be weakened & damage to the underlying cell membrane; bactericidal
Definition
vancomycin
Term
○ Reserve for serious infections caused by b-lactam resistant, gram (+) microorganisms or patients that have a life-threatening allergy to betalactam antibiotics
Definition
vancomycin
Term
AE of vancomycin
Definition
○ Infusion reaction (red man syndrome):
 Results from histamine release w/rapid infusion
 slow the infusion or give antihistamines
Term
tetracyclines
Definition
 Drug binds to the 30S subunit of the ribosome causing inhibition of bacterial protein synthesis
Term
Do not give to kids under 8 years old- in active growing phase. This will pull the calcium out of their teeth and bones
Definition
tetracyclines
Term
aminoglycosides
Definition
 diffuse through porin channels and bind to the 30 S ribosomal subunit, interrupting protein synthesis, same as tetracyclines
Term
 can only be give IV
Definition
aminoglycosides
Term
adverse effects of aminoglycosides
Definition
– Ototoxicity
– Nephrotoxicity
Term
macrolides
Definition
 Irreversibly bind to the 50S bacterial ribosomal subunit, inhibiting protein synthesis; generally considered bacteriostatic, but may have bactericidal at high dosages
Term
Adverse effects of macrolides
Definition
 GI upset
Term
chloramphenicol
Definition
 Binds to the 50S bacterial ribosomal subunit, inhibiting protein synthesis
Term
adverse effects of chloramphenicol
Definition
– Superinfections-Candida of mucous membranes
– Anemias
– Gray baby syndrome
Term
clindamycin
Definition
 Irreversibly bind to the 50S bacterial ribosomal subunit, inhibiting protein synthesis (same as erythromycin)
Term
adverse effects of clindamycin
Definition
○ Pseudomembranous colitis:C. difficile (potentially fatal)
Term
fluorouinolones (FQ)
Definition
 Enter the bacterium by passive diffusion through porins in the outer membrane

 Once inside the cell, they inhibit the replication of bacterial DNA by interfering with enzymes (gyrase & topoisomerases) involved in bacterial growth & reproduction
Term
interacts with Dietary supplements with iron or zinc, Ca (supplements or food)
Definition
fluorouinolones (FQ)
Term
 Do not give under 18 years old
Definition
fluorouinolones (FQ)
Term
 Inhibition of the synthesis of bacterial dihydrofolate acid (essential cofactor)
Definition
sulfonamides
Term
adverse effects of sulfonamides
Definition
 Hypersensitivity: rashes, angioedema, SJS
 Steven Johnson syndrome
Term
trimethoprim
Definition
Inhibits of bacterial dihydrofolate reductase (similar to sulfonamides, but different enzyme)
Term
 Typically used with sulfamethoxazole
Definition
trimethoprim
Term
nucleic acid inhibitors
Definition
• Nucleic acid analogs-compete as a substrate for viral DNA polymerase & incorporation into viral DNA (causing premature chain termination); inhibition of DNA polymerase &/or reverse transcriptase
Term
• Acts as a noncompetitive inhibitor of many viral RNA and DNA polymerases as well as HIV reverse transcriptase
Definition
pyrophosphate analogs
Term
neuraminidase inhibitors adverse effects
Definition
• Nephrotoxicity, Anemia, Seizures, Arrhythmias
Term
neuraminidase inhibitor
Definition
Oseltamivir (Tamiflu®)
Term
prevent the release of new visions
given 24-48 hours after exposure to decrease the intensity and duration of symptoms
Definition
Oseltamivir (Tamiflu®)
neuraminidase inhibitors
Term
• Selectively inhibits viral DNA & RNA synthesis
• Pediatrics with severe RSV
Definition
ribavirin
Term
Naturally occurring glycoproteins that interfere with the ability of viruses to infect penetrate host cells and uncoat
Definition
Interferon
Term
HIV therapy selection criteria
Definition
1. Avoid the use of 2 agents of same nucleoside analog
2. Avoid overlapping toxicities & genotypic and phenotypic characteristics of the virus
3. Patient factors: symptoms, concurrent illnesses
4. Impact of drug interactions
5. Ease of adherence to regimen
Term
NRTIs in treatment of HIV
Definition
• Cells and are incorporated into viral DNA by reverse transcriptase
• DNA-chain elongation is terminated
Term
adverse effects of NRTIs used in HIV
Definition
• Peripheral neuropathy
• Lipoatrophy (swiss cheese)
Term
NNRTIs used in HIV
Definition
• Highly selective, noncompetitive inhibitors of HIV-1 reverse transcriptase
Term
adverse effects of NNRTIs
Definition
• Hypersensitivity reactions
Term
protease inhibitors used to treat HIV
Definition
• Reversible inhibitors of HIV protease (involved with essential enzymes)
• This inhibition results decreased production of virions
Term
adverse effects of protease inhibitors used in HIV
Definition
• Disturbances in lipid & glucose metabolism
• Fat redistribution (redistributes from extremities to the trunk)
Term
(protease inhibitor)
Definition
Ritonavir
Term
• Typically used as a pharmacokinetic enhancer or booster of other protease inhibitors
• Increases the bioavailability & allows for less frequent dosing
• Help prevent the resistance to the other protease inhibitors
Definition
Ritonavir used to treat HIV
Term
• Prevents the fusion of the membrane of the HIV cell to the membrane of the host cell
Definition
entry inhibitors used to treat HIV
Term
• Inhibits the final step in integration of strand transfer of the viral DNA to the host cell
Definition
integrase inhibitors used to treat HIV
Term
amphotericin
Definition
fungal infection treatment

• Bind to ergosterol in the fungal cell membrane forming pores that disrupt membrane function, resulting in cell death
Term
adverse effects of amphotericin
Definition
• Low therapeutic index
• Fever/chills/hypotension
• Renal impairment/nephrotoxicity
Term
• Interfers with fungal cell membrane permeability by inhibiting the synthesis of ergosterol
Definition
azole antifungals
Term
adverse effects of azole antifungals
Definition
• GI: vomiting, diarrhea, hepatotoxicity
• Skin: rash
Term
echinocandins AE
Definition
• Viral illness like sypmptoms: Fever, Rash, Nausea
Term
• Inhibits fungal squalene epoxidase leading to decreased ergosterol synthesis
Definition
terbinafine
Term
• Drug of choice for treatment of dermatophytoses
Definition
terbinafine
Term
AE of terbinafine
Definition
• Liver enzyme elevation, hepatoxicity
Term
• Accumulates in newly synthesized tissue containing keratin and causes disruption of the mitotic spindle & inhibition of fungal mitosis
Definition
griseofulvin
Term
topical antifungals
Definition
(Interfere with fungal cell membrane permeability by inhibiting the synthesis of ergosterol)
• Disrupts mitotic spindle
Term
most common cause of TB resistance
Definition
Noncompliance
Term
• Synthetic pyridoxine analog

• Prodrug is activated by mycobacterial catalase-peroxidase (katG) and inhibits enzymes that are essential for the formation of mycolic acid (essential component of the mycobacterial cell wall)
Definition
isoniazide (INH)
Term
• Use-1st line treatment for M. Tuberculosis (in combination therapy)
Definition
isoniazide (INH)
Term
identify adverse effects of INH
Definition
• Vitamin B6 depletion
• Peripheral neuritis
• Hepatitis/Hepatoxicity
Term
• Interacts with the β subunit of bacterial RNA polymerase to block transcription
Definition
rifampin
Term
adverse effects of rifampin
Definition
• Discoloration-Orange/red discoloration to secretions (urine, tears, etc.)
• Flu-like syndrome-Fever, chills, myalgias
Term
• Inhibits an essential enzyme (arabinosyl transferase) causing disruption of cell wall synthesis
Definition
ethambutol
Term
adverse effects of ethambutol
Definition
• Optic neuritis
Term
the 4 drug treatment for TB
Definition
• Isoniazide, Rifampin, Pyrazinamide, Ethambutol
Term
Interferes with electron transport proteins in amebic cells, resulting in damage to DNA & proteins and cause cell death
Definition
metronidazole
Term
adverse effects of metronidazole
Definition
– GI upset, metallic taste
– Alcohol: disulfiram (vomiting)-like reaction
Term
• Tissue schizonticide; eradicates the exoerythrocytic forms of falciparum, vivax, and ovale
• Gametocide: the gametocyte form is prevented from maturing later in the mosquito-interupts the transmission of the disease
Definition
primaquine
Term
chloroquine
Definition
• Causes the organism to not be able to convert heme to hemozoin & the build up of heme is toxic to the organism
Term
adverse effects of chloroquine
Definition
• GI upset, HA, blurred vision, pruritis, Discoloration of the nail beds & mucous membranes; May exacerbate neurologic or hematologic disorders
Term
• Typically reserved for severe or resistant malaria infections
Definition
quinine
Term
• Blood schizonticide (no effect in liver stage); Forms complexes with DNA, interfering with DNA & RNA replication
Definition
quinine
Term
benzimidazole
Definition
Mebendazole, thiabendazole, albendazole
Term
– bind & interfers w/parasites’ microtubule assembly & ↓ glucose uptake by parasite
– acts as a depolarizing neuromuscular-blocking agent in parasite causing the paralyzed worm to be
excreted
Definition
benzimidazole
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