A common side effects of INF treatment is?
Neutropenia
Antimicrobial prophylaxis for a history of recurrent UTIs
TMP-SMZ
Antimicrobial prophylaxis for Gonorrhea
Ceftriaxone
Antimicrobial prophylaxis for Meningococcal infection
Rifampin (DOC), minocycline
Antimicrobial prophylaxis for PCP
TMP-SMZ (DOC), aerosolized pentamidine
Antimicrobial prophylaxis for Syphilis
Benzathine penicillin G
Are Aminoglycosides Teratogenic?
Yes
Are Ampicillin and Amoxicillin penicillinase resistant?
No
Are Carbenicillin, Piperacillin, and Ticarcillin penicillinase resistant?
No
Are Cephalosporins resistant to penicillinase?
No, but they are less susceptible than the other Beta lactams
Are Methicillin, Nafcillin, and Dicloxacillin penicillinase resistant?
Yes
Clinical use of Isoniazid (INH)?
Mycobacterium tuberculosis, the only agent used as solo prophylaxis against TB
Common side effects associated with Clindamycin include?
Pseudomembranous colitis (C. difficile), fever, diarrhea
Common toxicities associated with Fluoroquinolones?
GI upset, Superinfections, Skin rashes, Headache, Dizziness
Common toxicities associated with Griseofulvin are…...?
Teratogenic, Carcinogenic, Confusion, Headaches
Describe the MOA of Interferons (INF)
Glycoproteins from leukocytes that block various stages of viral RNA and DNA synthesis
Do Tetracyclines penetrate the CNS?
Only in limited amounts
Does Ampicillin or Amoxicillin have a greater oral bioavailability?
AmOxicillin has greater Oral bioavailability
Does Amprotericin B cross the BBB?
No
Does Foscarnet require activation by a viral kinase?
No
Foscarnet toxicity?
Nephrotoxicity 
Ganciclovir associated toxicities?
Leukopenia, Neutropenia, Thrombocytopenia, Renal toxicity
How are INFs used clinically?
Chronic Hepatitis A and B, Kaposi's Sarcoma
How are Sulfonamides employed clinically?
Gram +, Gram -, Norcardia, Chlamydia
How are the HIV drugs used clinically?
Triple Therapy' 2 Nucleoside RT Inhibitors with a Protease Inhibitor
How are the Latent Hypnozoite (Liver) forms of Malaria (P. vivax, P.ovale) treated?
Primaquine
How can Isoniazid (INH)-induced neurotoxicity be prevented?
Pyridoxine (B6) administration
How can the t1/2 of INH be altered?
Fast vs. Slow Acetylators
How can the toxic effects fo TMP be ameliorated?
With supplemental Folic Acid
How can Vancomycin-induced 'Red Man Syndrome' be prevented?
Pretreat with antihistamines and a slow infusion rate
How do Sulfonamides act on bacteria?
As PABA antimetabolites that inhibit Dihydropteroate Synthase, Bacteriostatic
How do the Protease Inhibitors work?
Inhibt Assembly of new virus by Blocking Protease Enzyme
How does Ganciclovir's toxicity relate to that of Acyclovir?
Ganciclovir is more toxic to host enzymes
How does resistance to Vancomycin occur?
With an amino acid change of D-ala D-ala to D-ala D-lac
How is Acyclovir used clinically?
HSV, VZV, EBV, Mucocutaneous and Genital Herpes Lesions, Prophylaxis in Immunocompromised pts
How is Amantadine used clinically?
Prophylaxis for Influenza A, Rubella ; Parkinson's disease
How is Amphotericin B administered for fungal meningitis?
Intrathecally
How is Amphotericin B used clinically?
Wide spectrum of systemic mycoses: Cryptococcus, Blastomyces, Coccidioides, Aspergillus, Histoplasma, Candida, Mucor
How is Chloramphenical used clinically?
Meningitis (H. influenza, N. meningitidis, S. pneumoniae), Conserative treatment due to toxicities
How is Foscarnet used clinically?
CMV Retinitis in IC pts when Ganciclovir fails
How is Ganciclovir activated?
Phosphorylation by a Viral Kinase
How is Ganciclovir used clinically?
CMV, esp in Immunocompromised patients
How is Griseofulvin used clinically?
Oral treatment of superficial infections
How is Leishmaniasis treated?
Pentavalent Antimony
How is Ribavirin used clinically?
for RSV
How is Rifampin used clinically?
1. Mycobacterium tuberculosis 2. Delays resistance to Dapsone when used of Leprosy 3. Used in combination with other drugs
How is Trimethoprim used clinically?
Used in combination therapy with SMZ to sequentially block folate synthesis
How is Vancomycin used clinically?
For serious, Gram + multidrug-resistant organisms
How would you treat African Trypanosomiasis (sleeping sickness)?
Suramin
In what population does Gray Baby Syndrome occur? Why?
Premature infants, because they lack UDP-glucuronyl transferase
Is Aztreonam cross-allergenic with penicillins?
No
Is Aztreonam resistant to penicillinase?
Yes
Is Aztreonam usually toxic?
No
Is Imipenem resistant to penicillinase?
Yes
Is Penicillin penicillinase resistant?
No - duh
IV Penicillin
G
Mnemonic for Foscarnet?
Foscarnet = pyroFosphate analog
MOA for Penicillin (3 answers)?
1)Binds penicillin-binding proteins 2) Blocks transpeptidase cross- linking of cell wall 3) Activates autolytic enzymes
MOA: Bactericidal antibiotics
Penicillin, Cephalosporins, Vancomycin, Aminoglycosides, Fluoroquinolones, Metronidazole
MOA: Block cell wall synthesis by inhib. Peptidoglycan cross-linking (7)
Penicillin, Ampicillin, Ticarcillin, Pipercillin, Imipenem, Aztreonam, Cephalosporins
MOA: Block DNA topoisomerases
Quinolones
MOA: Block mRNA synthesis
Rifampin
MOA: Block nucleotide synthesis
Sulfonamides, Trimethoprim
MOA: Block peptidoglycan synthesis
Bacitracin, Vancomycin
MOA: Block protein synthesis at 30s subunit
Aminoglycosides, Tetracyclines
MOA: Block protein synthesis at 50s subunit
Chloramphenicol, Erythromycin/macrolides, Lincomycin, Clindamycin, Streptogramins (quinupristin, dalfopristin)
MOA: Disrupt bacterial/fungal cell membranes
Polymyxins
MOA: Unkown
Pentamidine
MOA:Disrupt fungal cell membranes
Amphotericin B, Nystatin, Fluconazole/azoles
Name common Polymyxins
Polymyxin B, Polymyxin E
Name several common Macrolides (3)
Erythromycin, Azithromycin, Clarithromycin
Name some common Sulfonamides (4)
Sulfamethoxazole (SMZ), Sulfisoxazole, Triple sulfas, Sulfadiazine
Name some common Tetracyclines (4)
Tetracycline, Doxycycline, Demeclocycline, Minocycline
Name the common Aminoglycosides (5)
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Name the common Azoles
Fluconazole, Ketoconazole, Clotrimazole, Miconazole, Itraconazole
Name the common Fluoroquinolones (6)
Ciprofloxacin, Norfloxacin, Ofloxacin, Grepafloxacin, Enoxacin, Nalidixic acid
Name the common Non-Nucleoside Reverse Transcriptase Inhibitors
Nevirapine, Delavirdine
Name the common Nucleoside Reverse Transcriptase Inhibitors
Zidovudine (AZT), Didanosine (ddI), Zalcitabine (ddC), Stavudine (d4T), Lamivudine (3TC)
Name the Protease Inhibitors (4)
Saquinavir, Ritonavir, Indinavir, Nelfinavir
Name two classes of drugs for HIV therapy
Protease Inhibitors and Reverse Transcriptase Inhibitors
Name two organisms Vancomycin is commonly used for?
Staphlococcus aureus and Clostridium difficile (pseudomembranous colitis)
Oral Penicillin
V
Resistance mechanisms for Aminoglycosides
Modification via Acetylation, Adenylation, or Phosphorylation
Resistance mechanisms for Cephalosporins/Penicillins
Beta-lactamase cleavage of Beta-lactam ring
Resistance mechanisms for Chloramphenicol
Modification via Acetylation
Resistance mechanisms for Macrolides
Methylation of rRNA near Erythromycin's ribosome binding site
Resistance mechanisms for Sulfonamides
Altered bacterial Dihydropteroate Synthetase, Decreased uptake, or Increased PABA synthesis
Resistance mechanisms for Tetracycline
Decreased uptake or Increased transport out of cell
Resistance mechanisms for Vancomycin
Terminal D-ala of cell wall replaced with D-lac; Decreased affinity
Side effects of Isoniazid (INH)?
Hemolysis (if G6PD deficient), Neurotoxicity, Hepatotoxicity, SLE-like syndrome
Specifically, how does Foscarnet inhibit viral DNA pol?
Binds to the Pyrophosphate Binding Site of the enzyme
The MOA for Chloramphenicol is ……………..?
Inhibition of 50S peptidyl transferase, Bacteriostatic
Toxic effects of TMP include………?
Megaloblastic anemia, Leukopenia, Granulocytopenia
Toxic side effects of the Azoles?
Hormone synthesis inhibition (Gynecomastia), Liver dysfunction (Inhibits CYP450), Fever, Chills
Toxicities associated with Acyclovir?
Delirium, Tremor, Nephrotoxicity
What additional side effects exist for Ampicillin?
Rash, Pseudomembranous colitis
What antimicrobial class is Aztreonam syngergestic with?
Aminoglycosides
What are Amantadine-associated side effects?
Ataxia, Dizziness, Slurred speech
What are Aminoglycosides synergistic with?
Beta-lactam antibiotics
What are Aminoglycosides used for clinically?
Severe Gram - rod infections.
What are common serious side effects of Aminoglycosides and what are these associated with?
Nephrotoxicity (esp. with Cephalosporins), Ototoxicity (esp. with Loop Diuretics)
What are common side effects of Amphotericin B?
Fever/Chills, Hypotension, Nephrotoxicity, Arrhythmias
What are common side effects of Protease Inhibitors?
GI intolerance (nausea, diarrhea), Hyperglycemia, Lipid abnormalities, Thrombocytopenia (Indinavir)
What are common side effects of RT Inhibitors?
BM suppression (neutropenia, anemia), Peripheral neuropathy
What are common toxic side effects of Sulfonamides? (5)
-Hypersensitivity reactions -Hemolysis -Nephrotoxicity (tubulointerstitial nephritis) -Kernicterus in infants Displace other drugs from albumin (e.g., warfarin)
What are common toxicities associated with Macrolides? (4)
GI discomfort, Acute cholestatic hepatitis, Eosinophilia, Skin rashes
What are common toxicities associated with Tetracyclines?
GI distress, Tooth discoloration and Inhibition of bone growth in children, Fanconi's syndrome, Photosensitivity
What are common toxicities related to Vancomycin therapy?
Well tolerated in general but occasionally, Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing='Red Man Syndrome'
What are Fluoroquinolones indicated for? (3)
1.Gram - rods of the Urinary and GI tracts (including Pseudomonas) 2.Neisseria 3. Some Gram + organisms
What are major side effects of Methicillin, Nafcillin, and Dicloxacillin?
Hypersensitivity reactions
What are Methicillin, Nafcillin, and Dicloxacillin used for clinically?
Staphlococcus aureus
What are Polymyxins used for?
Resistant Gram - infections
What are the Anti-TB drugs?
Rifampin, Ethambutol, Streptomycin, Pyrazinamide, Isoniazid (INH)
What are the clinical indications for Azole therapy?
Systemic mycoses
What are the clinical uses for 1st Generation Cephalosporins?
Gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae (PEcK)
What are the clinical uses for 2nd Generation Cephalosporins?
Gram + cocci, Haemophilus influenza, Enterobacter aerogenes, Neisseria species, P. mirabilis, E. coli, K. pneumoniae, Serratia marcescens ( HEN PEcKS )
What are the clinical uses for 3rd Generation Cephalosporins?
1) Serious Gram - infections resistant to other Beta lactams 2) Meningitis (most penetrate the BBB)
What are the clinical uses for Aztreonam?
Gram - rods: Klebsiella species, Pseudomonas species, Serratia species
What are the clinical uses for Imipenem/cilastatin?
Gram + cocci, Gram - rods, and Anerobes
What are the Macrolides used for clinically?
-Upper respiratory tract infections -pneumonias -STDs: Gram+ cocci (streptococcal infect in pts allergic to penicillin) -Mycoplasma, Legionella,Chlamydia, Neisseria
What are the major structural differences between Penicillin and Cephalosporin?
Cephalosporin: 1) has a 6 member ring attached to the Beta lactam instead of a 5 member ring 2)has an extra functional group ( attached to the 6 member ring)
What are the major toxic side effects of Imipenem/cilastatin?
GI distress, Skin rash, and Seizures at high plasma levels
What are the major toxic side effects of the Cephalosporins?
1) Hypersensitivity reactions 2) Increased nephrotoxicity of Aminoglycosides 3) Disulfiram-like reaction with ethanol (those with a methylthiotetrazole group, e.g., cefamandole)
What are the side effects of Polymyxins?
Neurotoxicity, Acute renal tubular necrosis
What are the side effects of Rifampin?
Minor hepatotoxicity, Drug interactions (activates P450)
What are toxic side effects for Metronidazole?
Disulfiram-like reaction with EtOH, Headache
What are toxicities associated with Chloramphenicol?
Aplastic anemia (dose independent), Gray Baby Syndrome
What conditions are treated with Metronidazole?
Giardiasis, Amoebic dysentery (E. histolytica), Bacterial vaginitis (Gardnerella vaginalis), Trichomonas
What do Aminoglycosides require for uptake?
Oxygen
What do you treat Nematode/roundworm (pinworm, whipworm) infections with?
Mebendazole/Thiabendazole, Pyrantel Pamoate
What drug is given for Pneumocystis carinii prophylaxis?
Pentamidine
What drug is used during the pregnancy of an HIV + mother?, Why?
AZT, to reduce risk of Fetal Transmission
What drug is used to treat Trematode/fluke (e.g., Schistosomes, Paragonimus, Clonorchis) or Cysticercosis
Praziquantel
What is a common drug interaction associated with Griseofulvin?
Increases coumadin metabolism
What is a mnemonic to remember Amantadine's function?
Blocks Influenza A and RubellA; causes problems with the cerebellA
What is a prerequisite for Acyclovir activation?
It must be Phosphorylated by Viral Thymidine Kinase
What is a Ribavirin toxicity?
Hemolytic anemia
What is an acronym to remember Anti-TB drugs?
RESPIre
What is an additional side effect of Methicillin?
Interstitial nephritis
What is an occasional side effect of Aztreonam?
GI upset
What is Clindamycin used for clinically?
Anaerobic infections (e.g., B. fragilis, C. perfringens)
What is clinical use for Carbenicillin, Piperacillin, and Ticarcillin?
Pseudomonas species and Gram - rods
What is combination TMP-SMZ used to treat?
Recurrent UTIs, Shigella, Salmonella, Pneumocystis carinii pneumonia
What is combined with Ampicillin, Amoxicillin, Carbenicillin, Piperacillin, and Ticarcillin to enhance their spectrum?
Clavulanic acid
What is Fluconazole specifically used for?
Cryptococcal meningitis in AIDS patients and Candidal infections of all types
What is Imipenem always administered with?
Cilastatin
What is Ketoconazole specifically used for?
Blastomyces, Coccidioides, Histoplasma, C. albicans; Hypercortisolism
What is Metronidazole combined with for 'triple therapy'? Against what organism?
Bismuth and Amoxicillin or Tetracycline; against Helobacter pylori
What is Metronidazole used for clinically?
Antiprotozoal: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis Anaerobes: Bacteroides, Clostridium
What is Niclosamide used for?
Cestode/tapeworm (e.g., D. latum, Taenia species Except Cysticercosis
What is Nifurtimox administered for?
Chagas' disease, American Trypanosomiasis (Trypanosoma cruzi)
What is the chemical name for Ganciclovir?
DHPG (dihydroxy-2-propoxymethyl guanine)
What is the clinical use for Ampicillin and Amoxicillin?
Extended spectrum penicillin: certain Gram + bacteria and Gram - rods
What is the clinical use for Nystatin?
Topical and Oral, for Oral Candidiasis (Thrush)
What is the clinical use for Penicillin?
Bactericidal for: Gram + rod and cocci, Gram - cocci, and Spirochetes
What is the major side effect for Ampicillin and Amoxicillin?
Hypersensitivity reactions
What is the major side effect for Carbenicillin, Piperacillin, and Ticarcillin?
Hypersensitivity reactions
What is the major toxic side effect of Penicillin?
Hypersensitivity reactions
What is the memory aid for subunit distribution of ribosomal inhibitors?
Buy AT 30, CELL at 50'
What is the memory key for Isoniazid (INH) toxicity?
INH: Injures Neurons and Hepatocytes
What is the memory key for Metronidazole's clinical uses?
GET on the Metro
What is the memory key for organisms treated with Tetracyclines?
VACUUM your Bed Room'
What is the memory key involving the '4 R's of Rifampin?'
1. RNA pol inhibitor 2. Revs up P450 3. Red/orange body fluids 4. Rapid resistance if used alone
What is the MOA for Acyclovir?
Inhibit viral DNA polymerase
What is the MOA for Amphotericin B?
Binds Ergosterol, forms Membrane Pores that Disrupt Homeostatis
What is the MOA for Ampicillin and Amoxicillin?
Same as penicillin. Extended spectrum antibiotics
What is the MOA for Carbenicillin, Piperacillin, and Ticarcillin?
Same as penicillin. Extended spectrum antibiotics
What is the MOA for Clindamycin?
Blocks Peptide Bond formation at the 50S subunit, Bacteriostatic
What is the MOA for Methicillin, Nafcillin, and Dicloxacillin?
Same as penicillin. Act as narrow spectrum antibiotics
What is the MOA for Metronidazole?
Forms toxic metabolites in the bacterial cell, Bactericidal
What is the MOA for Nystatin?
Binds ergosterol, Disrupts fungal membranes
What is the MOA for Rifampin?
Inhibits DNA dependent RNA polymerase
What is the MOA for the Aminoglycosides?
Inhibits formation of Initiation Complex, causes misreading of mRNA, Bactericidal
What is the MOA for the Azoles?
Inhibit Ergosterol synthesis
What is the MOA for the Cephalosporins?
Beta lactams - inhibit cell wall synthesis, Bactericidal
What is the MOA for the Fluoroquinolones?
Inhibit DNA Gyrase (topoisomerase II), Bactericidal
What is the MOA for the Macrolides?
Blocks translocation, binds to the 23S rRNA of the 50S subunit, Bacteriostatic
What is the MOA for the Tetracyclines?
Binds 30S subunit and prevents attachment of aminoacyl-tRNA, Bacteriostatic
What is the MOA for Trimethoprim (TMP)?
Inhibits bacterial Dihydrofolate Reductase, Bacteriostatic
What is the MOA for Vancomycin?
Inhibits cell wall mucopeptide formation, Bactericidal
What is the MOA of Amantadine?
Blocks viral penetration/uncoating; may act to buffer the pH of the endosome
What is the MOA of Aztreonam?
Inhibits cell wall synthesis ( binds to PBP3). A monobactam
What is the MOA of Foscarnet?
Inhibits Viral DNA polymerase
What is the MOA of Ganciclovir?
Inhibits CMV DNA polymerase
What is the MOA of Griseofulvin?
Interferes with microtubule function, disrupts mitosis, inhibits growth
What is the MOA of Imipenem?
Acts as a wide spectrum carbapenem
What is the MOA of Isoniazid (INH)?
Decreases synthesis of Mycolic Acid
What is the MOA of Polymyxins?
Bind cell membrane, disrupt osmotic properties, Are Cationc, Basic and act as detergents
What is the MOA of Ribavirin?
Inhibits IMP Dehydrogenase (competitively), and therefore blocks Guanine Nucleotide synthesis
What is the MOA of the RT Inhibitors?
Inhibit RT of HIV and prevent the incorporation of viral genome into the host DNA
What is the most common cause of Pt noncompliance with Macrolides?
GI discomfort
What is treated with Chloroquine, Quinine, Mefloquine?
Malaria (P. falciparum)
What microorganisms are Aminoglycosides ineffective against?
Anaerobes
What microorganisms are clinical indications for Tetracycline therapy?
Vibrio cholerae Acne Chlamydia Ureaplasma Urealyticum Mycoplasma pneumoniae Borrelia burgdorferi (Lyme's) Rickettsia Tularemia
What microorganisms is Aztreonam not effective against?
Gram + and Anerobes
What musculo-skeletal side effects in Adults are associated with Floroquinolones?
Tendonitis and Tendon rupture
What neurotransmitter does Amantadine affect? How does it influence this NT?
Dopamine; causes its release from intact nerve terminals
What organism is Imipenem/cilastatin the Drug of Choice for?
Enterobacter
What organisms does Griseofulvin target?
Dermatophytes (tinea, ringworm)
What parasites are treated with Pyrantel Pamoate (more specific)?
Giant Roundworm (Ascaris), Hookworm (Necator/Ancylostoma), Pinworm (Enterobius)
What parasitic condition is treated with Ivermectin?
Onchocerciasis ('river blindness'--rIVER-mectin)
What populations are Floroquinolones contraindicated in? Why?
Pregnant women, Children; because animal studies show Damage to Cartilage
What should not be taken with Tetracyclines? / Why?
Milk or Antacids, because divalent cations inhibit Tetracycline absorption in the gut
What Sulfonamides are used for simple UTIs?
Triple sulfas or SMZ
When is HIV therapy initiated?
When pts have Low CD4+ (< 500 cells/cubic mm) or a High Viral Load
When is Rifampin not used in combination with other drugs?
1. Meningococcal carrier state 2. Chemoprophylaxis in contacts of children with H. influenzae type B
Where does Griseofulvin deposit?
Keratin containing tissues, e.g., nails
Which Aminoglycoside is used for Bowel Surgery ?
Neomycin
Which antimicrobial classes inhibit protein synthesis at the 30S subunit? (2)
1) Aminoglycosides = bactericidal 2) Tetracyclines = bacteriostatic
Which antimicrobials inhibit protein synthesis at the 50S subunit? (4)
1) Chloramphenical = bacteriostatic 2) Erythromycin = bacteriostatic 3) Lincomycin = bacteriostatic 4)cLindamycin = bacteriostatic
Which individuals are predisposed to Sulfonamide-induced hemolysis?
G6PD deficient individuals
Which RT inhibitor causes Megaloblastic Anemia?
AZT
Which RT inhibitors cause a Rash?
Non-Nucleosides
Which RT inhibitors cause Lactic Acidosis?
Nucleosides
Which Tetracycline is used in patients with renal failure? / Why?
Doxycycline, because it is fecally eliminated
Who's your daddy?
B.W. !!!, Ha. Good Luck on Boards
Why are Methicillin, Nafcillin, and Dicloxacillin penicillinase resistant?
Due to the presence of a bulkier R group
Why is Cilastatin administered with Imipenem?
To inhibit renal Dihydropeptidase I and decrease Imipenem inactivation in the renal tubules
List the mechanism, clinical use, & toxicity of 5 FU.
-S-phase anti-metabolite Pyr analogue -Colon, solid tumors, & BCC/ -Irreversible myelosuppression
List the mechanism, clinical use, & toxicity of 6 MP.
-inhibits HGPRT (pur. Syn.) - Luk, Lymph,
List the mechanism, clinical use, & toxicity of Bleomycin.
-DNA intercalator -testicular & lymphomas -Pulmonary fibrosis mild myelosuppression.
List the mechanism, clinical use, & toxicity of Busulfan.
-Alkalates DNA -CML -Pulmonary fibrosis hyperpigmentation
List the mechanism, clinical use, & toxicity of Cisplatin.
-Alkalating agent -testicular,bladder,ovary,&lung -Nephrotoxicity & CN VIII damage.
List the mechanism, clinical use, & toxicity of Cyclophosphamide.
-Alkalating agent -NHL, Breast, ovary, & lung. - Myelosuppression, & hemorrhagic cystitis.
List the mechanism, clinical use, & toxicity of Doxorubicin.
-DNA intercalator -Hodgkin's, myeloma, sarcoma, and solid tumors -Cardiotoxicity & alopecia
List the mechanism, clinical use, & toxicity of Etoposide.
-Topo II inhibitor(GII specific) -Oat cell of Lung & prostate, & testicular -Myelosuppression & GI irritation.
List the mechanism, clinical use, & toxicity of Methotrexate.
-S-phase anti-metabolite folate analogue -Luk, Lymp, sarc, RA, &psoriasis / -Reversible myelosuppression
List the mechanism, clinical use, & toxicity of Nitrosureas.
-Alkalate DNA -Brain tumors -CNS toxicity
List the mechanism, clinical use, & toxicity of Paclitaxel.
-MT polymerization stabilizer -Ovarian & breast CA -Myelosupperession & hypersensitivity.
List the mechanism, clinical use, & toxicity of Prednisone.
-Triggers apoptosis -CLL, Hodgkin's in MOPP -Cushing-like syndrome
List the mechanism, clinical use, & toxicity of Tamoxifen.
-Estrogen receptor antagonist -Breast CA -increased endometrial CA risk
List the mechanism, clinical use, & toxicity of Vincristine.
-MT polymerization inhibitor(M phase) -MOPP, lymphoma, Willm's & choriocarcinoma -neurotoxicity and myelosuppression
Which cancer drugs effect nuclear DNA (4)?
-Alkalating agents+cisplatin -Doxorubicin+Dactinomycin -Bleomycin -Etoposide
Which cancer drugs inhibit nucleotide synthesis(3)?
- Methotrexate - 5 FU - 6 mercaptopurine
Which cancer drugs work at the level of mRNA(2)?
-Steroids -Tamoxifen
Which cancer drugs work at the level of proteins(2)?
-Vinca alkaloids(inhibit MT) -Paclitaxel
ACE inhibitors- clinical use?
hypertension, CHF, diabetic renal disease
ACE inhibitors- mechanism?
reduce levels of Angiotensin II, thereby preventing the inactivation of bradykinin (a potent vasodilator); renin level is increased
ACE inhibitors- toxicity?
fetal renal damage, hyperkalemia, Cough, Angioedema, Proteinuria, Taste changes, hypOtension, Pregnancy problems, Rash, Increased renin, Lower Angiotensin II (CAPTOPRIL)
Acetazolamide- clinical uses?
glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness
Acetazolamide- mechanism?
acts at the proximal convoluted tubule to inhibit carbonic anhydrase. Causes self-limited sodium bicarb diuresis and reduction of total body bicarb stores.
acetazolamide- site of action?
proximal convoluted tubule
Acetazolamide- toxicity?
hyperchloremic metabolic acidosis, neuropathy, NH3 toxicity, sulfa allergy
Acetazolamide causesÉ?
ACIDazolamide' causes acidosis
Adenosine- clinical use?
DOC in diagnosing and abolishing AV nodal arrhythmias
ADH antagonists- site of action?
collecting ducts
adverse effect of Nitroprusside?
cyanide toxicity (releases CN)
adverse effects of beta-blockers?
impotence, asthma, CV effects (bradycardia, CHF, AV block), CNS effects (sedation, sleep alterations)
adverse effects of Captopril?
fetal renal toxicity, hyperkalemia, Cough, Angioedema, Proteinuria, Taste changes, hypOtension, Pregnancy problems, Rash, Increased renin, Lower Angiotensin II (CAPTOPRIL)
adverse effects of Clonidine?
dry mouth, sedation, severe rebound hypertension
adverse effects of ganglionic blockers?
severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction
adverse effects of Guanethidine?
orthostatic and exercise hypotension, sexual dysfunction, diarrhea
adverse effects of Hydralazine?
nausea, headache, lupus-like syndrome, reflex tachycardia, angina, salt retention
adverse effects of Hydrochlorothiazide?
hypokalemia, slight hyperlipidemia, hyperuricemia, lassitude, hypercalcemia, hyperglycemia
adverse effects of Loop Diuretics?
K+ wasting, metabolic alkalosis, hypotension, ototoxicity
adverse effects of Losartan?
fetal renal toxicity, hyperkalemia
adverse effects of Methyldopa?
sedation, positive Coombs' test
adverse effects of Minoxidil?
hypertrichosis, pericardial effusion, reflex tachycardia, angina, salt retention
adverse effects of Nifedipine, verapamil?
dizziness, flushing, constipation (verapamil), nausea
adverse effects of Prazosin?
first dose orthostatic hypotension, dizziness, headache
adverse effects of Reserpine?
sedation, depression, nasal stuffiness, diarrhea
Amiodarone- toxicity?
pulmonary fibrosis, corneal deposits, hepatotoxicity, skin deposits resulting in photodermatitis, neurologic effects, consitpation, CV (bradycardia, heart block, CHF), and hypo- or hyperthyroidism.
antidote?
slowly normalize K+, lidocaine, cardiac pacer, and anti-Dig Fab fragments
Beta Blockers- CNS toxicity?
sedation, sleep alterations
Beta Blockers- CV toxicity?
bradycardia, AV block, CHF
Beta Blockers- site of action?
Beta adrenergic receptors and  Ca2+ channels (stimulatory)
BP?
decrease
BP?
decrease
Bretyllium- toxicity?
new arrhythmias, hypotension
Ca2+ channel blockers- clinical use?
hypertension, angina, arrhythmias
Ca2+ channel blockers- mechanism?
block voltage dependent L-type Ca2+ channels of cardiac and smooth muscle- decreasing contractility
Ca2+ channel blockers- site of action?
Cell membrane Ca2+ channels of cardiac sarcomere
Ca2+ channel blockers- toxicity?
cardiac depression, peripheral edema, flushing, dizziness, constipation
Ca2+ sensitizers'- site of action?
troponin-tropomyosin system
Cautions when using Amiodarone?
check PFTs, LFTs, and TFTs
class IA effects?
increased AP duration, increased ERP increased QT interval. Atrial and ventricular.
class IB- clinical uses?
post MI and digitalis induced arrhythmias
class IB- effects?
decrease AP duration, affects ischemic or depolarized Purkinje and ventricular system
class IB- toxicity?
local anesthetic.  CNS stimulation or depression. CV depression.
class IC- effects?
NO AP duration effect. useful in V-tach that progresses to V-fib and in intractable SVT LAST RESORT
class IC- toxicity?
proarrhythmic
class II- effects?
decrease the slope of phase 4, increase PR interval (the AV node is particularly sensitive)
class II- mechanism?
blocking the beta adrenergic receptor leads to decreased cAMP, and decreased Ca2+ flux
class II- toxicity?
impotence, exacerbation of asthma, CV effects, CNS effects, may mask hypoclycemia
Class III- effects?
increase AP duration, increase ERP, increase QT interval, for use when other arrhythmics fail
class IV- clinical use?
prevention of nodal arrhythmias (SVT)
class IV- effects?
decrease conduction velocity, increase ERP, increase PR interval
class IV- primary site of action?
AV nodal cells
class IV- toxicity?
constipation, flushing, edema, CV effects (CHF, AV block, sinus node depression), and torsade de pointes (Bepridil)
classes of antihypertensive drugs?
diuretics, sympathoplegics, vasodilators, ACE inhibitors, Angiotensin II receptor inhibitors
clinical use?
angina, pulmonary edema (also, erection enhancer)
clinical use?
CHF, atrial fibrillation
contractility?
increase (reflex response)
contractility?
decrease
contraindications?
renal failure, hypokalemia, pt on quinidine
decrease Digitoxin dose in renal failure?
NO
decrease Digoxin dose in renal failure?
YES
Digitalis- site of action?
Na/K ATPase
Digoxin v. Digitoxin: bioavailability?
Digitoxin>95% Digoxin 75%
Digoxin v. Digitoxin: excretion?
Digoxin=urinary Digitoxin=biliary
Digoxin v. Digitoxin: half life?
Digitoxin 168hrs Digoxin 40 hrs
Digoxin v. Digitoxin: protein binding?
Digitoxin 70% Digoxin 20-40%
ejection time?
decrease
ejection time?
increase
EKG results?
inc PR, dec QT, scooping of ST, and T wave inversion
end diastolic volume?
decrease
end diastolic volume?
increase
Esmolol- short or long acting?
very short acting
Ethacrynic Acid- clinical use?
Diuresis in pateints with sulfa allergy
Ethacrynic Acid- mechanism?
not a sulfonamide, but action is the same as furosemide
Ethacrynic Acid- toxicity?
NO HYPERURICEMIA, NO SULFA ALLERGY; same as furosemide otherwise
Furosemide- class and mechanism?
Sulfonamide Loop Diuretic. Inhibits ion co-transport system of thick ascending loop. Abolishes hypertonicity of the medulla, thereby preventing concentration of the urine.
Furosemide- clinical use?
edematous states (CHF, cirrhosis, nephrotic syndrome, pulm edema), HTN, hypercalcemia
Furosemide- toxicity? (OH DANG)
Ototoxicity, Hypokalemia, Dehydration, Allergy (sulfa), Nephritis (interstitial), Gout
Furosemide increases the excretion of what ion?
Ca2+ (Loops Lose calcium)
HDL effect?
no effect
HDL effect?
increase
HDL effect?
moderate increase
HDL effect?
increase
HDL effect?
DECREASE
how do we stop angina?
decrease myocardial O2 consumption by: 1-decreasing end diastolic volume 2- decreasing BP 3- decreasing HR 4-decreasing contractility 5-decreasing ejection time
HR?
increase (reflex response)
HR?
decrease
Hydralazine- class and mechanism?
vasodilator- increases cGMP to induce smooth muscle relaxation (arterioles>veins; afterload reduction)
Hydralazine- clinical use?
severe hypertension, CHF
Hydralazine- toxicity?
compensatory tachycardia, fluid retention, lupus-like syndrome
Hydrochlorothiazide- clinical use?
HTN, CHF, calcium stone formation, nephrogenic DI.
Hydrochlorothiazide- mechanism?
Inhibits NaCl reabsorption in the early distal tubule. Decreases Ca2+ excretion.
Hydrochlorothiazide- toxicity? (hyperGLUC, plus others)
Hypokalemic metabolic alkalosis, hyponatremia, hyperGlycemia, hyperLipidemia, hyperUricemia, hyperCalcemia, sulfa allergy.
Ibutilide- toxicity?
torsade de pointes
K+- clinical use?
depresses ectopic pacemakers, especially in digoxin toxicity
K+ sparing diuretics- clinical use?
hyperaldosteronism, K+ depletion, CHF
K+ sparing diuretics- site of action?
cortical collecting tubule
K+ sparing diuretics- toxicity?
hyperkalemia, endocrine effects (gynecomastia, anti-androgen)
LDL effect?
moderate decrease
LDL effect?
large decrease
LDL effect?
moderate decrease
LDL effect?
decrease
LDL effect?
decrease
loop diuretics (furosemide)- site of action?
thick ascending limb
Mannitol- clinical use?
ARF, shock, drug overdose, decrease intracranial/intraocular pressure
Mannitol- contraindications?
anuria, CHF
Mannitol- mechanism?
osmotic diuretic- increase tubular fluid osmolarity, thereby increasing urine flow
mannitol- site of action?
proximal convoluted tubule, thin descending limb, and collecting duct
Mannitol- toxicity?
pulmonary edema, dehydration
mechanism?
vasodilate by releasing NO in smooth muscle, causing and increase in cGMP and smooth muscle relaxation (veins>>arteries)
mechanism?
inhibits the Na/K ATPase,  increasing intracellular Na+ decreasing the function of the Na/Ca antiport causing an increase in intracellular Ca2+
mechanism?
Na+ channel blockers. Slow or block conduction. Decreased slope in phase 4 and increased threshold for firing in abnormal pacemaker cells.
Mg+- clinical use?
effective in torsade de pointes and digoxin toxicity
MVO2?
decrease
MVO2?
decrease
name five in class II?
propanolol, esmolol, metoprolol, atenolol, timolol
name four HMG-CoA reductase inhibitors.
Lovastatin, Pravastatin, Simvastatin, Atorvastatin
name four in class IA.
Quinidine, Amiodarone, Procainamide, Disopyramide
name four in class III.
Sotalol, Ibutilide, Bretylium, Amiodarone
name three ACE inhibitors?
Captopril, Enalapril, Lisinopril
name three calcium channel blockers?
Nifedipine, Verapamil, Diltiazem
name three in class IB.
Lidocaine, Mexiletine, Tocainide
name three in class IC.
Flecainide, Encainide, Propafenone
name three in class IV.
Verapamil, Diltiazem, Bepridil
name three K+ sparing diuretics?
Spironolactone, Triamterene, Amiloride (the K+ STAys)
name two bile acid resins.
cholestyramine, colestipol
name two LPL stimulators.
Gemfibrozil, Clofibrate
Nifedipine has similar action to?
Nitrates
preferential action of the Ca2+ channel blockers at cardiac muscle?
cardiac muscle: Verapamil>Diltiazem>Nifedipine
preferential action of the Ca2+ channel blockers at vascular smooth muscle?
vascular sm. Mus.: Nifedipine>Diltiazem>Verapamil
Procainamide- toxicity?
reversible SLE-like syndrome
Quinidine- toxicity?
cinchonism: HA, tinnitus, thrombocytopenia, torsade de pointes due to increased QT interval
Ryanodine- stie of action?
blocks SR Ca2+ channels
selectivity?
slectively depress tissue that is frequently depolarized (fast tachycardia)
side effects/problems?
tastes bad and causes GI discomfort
side effects/problems?
expensive, reversible increase in LFTs, and myositis
side effects/problems?
red, flushed face which is decreased by ASA or long term use
side effects/problems?
myositis, increased LFTs
side effects/problems?
DECREASED HDL
Sotalol- toxicity?
torsade de pointes, excessive Beta block
Spironolactone- mechanism?
competitive inhibirot of aldosterone in the cortical collecting tubule
TG effect?
slight increase
TG effect?
decrease
TG effect?
decrease
TG effect?
large decrease
TG effect?
no effect
thiazides- site of action?
distal convoluted tubule (early)
toxicity?
tachycardia, hypotension, headache - 'Monday disease'
toxicity?
nausea, vomiting, diarrhea, blurred vision, arrhythmia
Triamterene and amiloride- mechanism?
block Na+ channels in the cortical collecting tubule
Verapamil has similar action to?
Beta Blockers
what two vasodilators require simultaneous treatment with beta blockers to prevent reflex tachycardia and diuretics to prevent salt retention?
Hydralazine and Minoxidil
which diuretics cause acidosis?
carbonic anhydrase inhibitors, K+ sparing diuretics
which diuretics cause alkalosis?
loop diuretics, thiazides
which diuretics decrease urine Ca2+?
thiazides, amiloride
which diuretics increase urine Ca2+?
loop diuretics, spironolactone
which diuretics increase urine K+?
all except the K+ sparing diuretics Spironolactone, Triamterene, Amiloride
which diuretics increase urine NaCl?
all of them
Acetaminophen has what two clinical uses and lacks what one clinical use of the NSAIDs?
Acetaminophen has antipyretic and analgesic properties, but lacks anti-inflammatory properties.
Can Heparin be used during pregnancy?
Yes, it does not cross the placenta.
Can Warfarin be used during pregnancy?
No, warfarin, unlike heparin, can cross the placenta.
Does Heparin have a long, medium, or short half life?
Short.
Does Warfarin have a long, medium, or short half life?
Long.
For Heparin what is the 1. Structure 2. Route of administration 3. Onset of action 4. Mechanism of action 5. Duration of action 6. Ability to inhibit coagulation in vitro 7. Treatment for overdose 8. Lab value to monitor 9. Site of action
Heparin 1. Structure - Large anionic polymer, acidic 2. Route of administration - Paranteral (IV, SC) 3. Onset of action - Rapid (seconds) 4. Mechanism of action - Activates antithrombin III 5. Duration of action - Acute (hours) 6. Ability to inhibit coagulation in vitro - Yes 7. Treatment for overdose - Protamine sulfate 8. Lab value to monitor-aPTT (intrinsic pathway) 9. Site of action - Blood
For Warfarin what is the 1. Structure 2. Route of administration 3. Onset of action 4. Mechanism of action 5. Duration of action 6. Ability to inhibit coagulation in vitro 7. Treatment for overdose 8. Lab value to monitor 9. Site of action
Warfarin 1. Structure - Small lipid-soluble molecule 2. Route of administration -Oral 3. Onset of action - Slow, limited by half lives of clotting factors 4. Mechanism of action - Impairs the synthesis of vitamin K-dependent clotting factors 5. Duration of action - Chronic (weeks or months) 6. Ability to inhibit coagulation in vitro - No 
For Warfarin what is the (continued):
7. Treatment for overdose - IV vitamin K and fresh frozen plasma 8. Lab value to monitor - PT 9. Site of action - Liver
Is toxicity rare or common whith Cromolyn used in Asthma prevention?
Rare.
List five common glucocorticoids.
1. Hydrocortisone 2. Predisone 3. Triamcinolone 4. Dexamethasone 5. Beclomethasone
Secretion of what drug is inhibited by Probenacid used to treat chronic gout?
Penicillin.
The COX-2 inhibitors (celecoxib, rofecoxib) have similar side effects to the NSAIDs with what one exception?
The COX-2 inhibitors should not have the corrosive effects of other NSAIDs on the gastrointestinal lining.
What are are the Sulfonylureas (general description) and what is their use?
Sulfonylureas are oral hypoglycemic agents, they are used to stimulate release of endogenous insulin in NIDDM (type-2).
What are five advantages of Oral Contraceptives (synthetic progestins, estrogen)?
1. Reliable (<1% failure) 2. Lowers risk of endometrial and ovarian cancer 3. Decreased incidence of ectopic pregnancy 4. Lower risk of pelvic infections 5. Regulation of menses
What are five disadvantages of Oral Contraceptives (synthetic progestins, estrogen)?
1. Taken daily 2. No protection against STDs 3. Raises triglycerides 4. Depression, weight gain, nausea, HTN 5. Hypercoagulable state
What are five possible toxic effects of Aspirin therapy?
1. Gastric ulceration 2. Bleeding 3. Hyperventilation 4. Reye's syndrome 5. Tinnitus (CN VIII)
What are five toxicities associated with Tacrolimus (FK506)?
1. Significant: nephrotoxicity 2. Peripheral neuropathy 3. Hypertension 4. Pleural effusion 5. Hyperglycemia.
What are four advantages of newer low-molecular-weight heparins (Enoxaparin)?
1. Better bioavailability 2. 2 to 4 times longer half life 3. Can be administered subcutaneously 4. Does not require laboratory monitoring
What are four clinical activities of Aspirin?
1. Antipyretic 2. Analgesic 3. Anti-inflammatory 4. Antiplatelet drug.
What are four clinical uses of glucocorticoids?
1. Addison's disease 2. Inflammation 3. Immune suppression 4. Asthma
What are four conditions in which H2 Blockers are used clinically?
1. Peptic ulcer 2. Gastritis 3. Esophageal reflux 4. Zollinger-Ellison syndrome
What are four H2 Blockers?
1. Cimetadine 2. Ranitidine 3. Famotidine 4. Nizatidine
What are four Sulfonylureas?
1. Tolbutamide 2. Chlorpropamide 3. Glyburide 4. Glipizide
What are four thrombolytics?
1. Streptokinase 2. Urokinase 3. tPA (alteplase), APSAC (anistreplase)
What are four unwanted effects of Clomiphene use?
1. Hot flashes 2. Ovarian enlargement 3. Multiple simultaneous pregnancies 4. Visual disturbances
What are nine findings of Iatrogenic Cushing's syndrome caused by glucocorticoid therapy? 
1. Buffalo hump 2. Moon facies 3. Truncal obesity 4. Muscle wasting 5. Thin skin 6. Easy bruisability 7. Osteoporosis 8. Adrenocortical atrophy 9. Peptic ulcers
What are signs of Sildenafil (Viagra) toxicity?
Headache, flushing , dyspepsia, blue-green color vision.
What are the clinical uses for Ticlopidine, Clopidogrel?
Acute coronary syndrome; coronary stenting. Decreases the incidence or recurrence of thrombotic stroke.
What are the four conditions in which Omeprazole, Lansoprazole is used?
1. Peptic ulcer 2. Gastritis 3. Esophageal reflux 4. Zollinger-Ellison syndrome
What are three clinical uses of the Leuprolide?
1. Infertility (pulsatile) 2. Prostate cancer (continuous: use with flutamide) 3. Uterine fibroids
What are three clinical uses of the NSAIDs?
1. Antipyretic 2. Analgesic 3. Anti-inflammatory
What are three common NSAIDS other than Aspirin?
Ibuprofen, Naproxen, and Indomethacin
What are three complications of Warfarin usage?
1. Bleeding 2. Teratogenicity 3. Drug-drug interactions
What are three possible complications of Heparin therapy?
1. Bleeding 2. Thrombocytopenia 3. Drug-drug interactions
What are three possible toxicities of NSAID usage?
1. Renal damage 2. Aplastic anemia 3. GI distress
What are three toxicities of Leuprolied?
1. Antiandrogen 2. Nausea 3. Vomiting
What are three toxicities of Propylthiouracil?
1. Skin rash 2. Agranulocytosis (rare) 3. Aplastic anemia
What are three types of antacids and the problems that can result from their overuse?
1. Aluminum hydroxide: constipation and hypophosphatemia 2. Magnesium hydroxide: diarrhea 3. Calcium carbonate: Hypercalcemia, rebound acid increase - All may cause hypokalemia
What are three unwanted effects of Mifepristone?
1. Heavy bleeding 2. GI effects (n/v, anorexia) 3. Abdominal pain
What are two Alpha-glucosidase inhibitors?
1. Acarbose 2. Miglitol
What are two clinical uses of Azathioprine?
1. Kidney transplantation 2. Autoimmune disorders (including glomerulonephritis and hemolytic anemia)
What are two conditions in which COX-2 inhibitors might be used?
Rheumatoid and osteoarthritis.
What are two Glitazones?
1. Pioglitazone 2. Rosiglitazone.
What are two mechanisms of action of Propythiouracil?
Inhibits organification and coupling of thyroid hormone synthesis. Also decreases peripheral conversion of T4 to T3.
What are two processes Corticosteroids inhibit leading to decreased inflammation?
1. Phospholipase A2 is prevented from releasing arachidonic acid 2. Decreases protein synthesis thus lowering amount of Cyclooxygenase enzymes
What are two toxicities associated with Cyclosporine?
1. Predisposes to viral infections and lymphoma 2. Nephrotoxic (preventable with mannitol diuresis)
What are two toxicities of the Glitazones?
1. Weight gain 2. Hepatotoxicity (troglitazone)
What are two toxicities of the Sulfonylureas?
1. Hypoglycemia (more common with 2nd-generation drugs: glyburide, glipizide) 2. Disulfiram-like effects (not seen with 2nd-generation drugs).
What are two types of drugs that interfere with the action of Sucralfate and why?
Sucralfate cannot work in the presence of antacids or H2 blockers because it requires an acidic environment to polymerize.
What can result due to antacid overuse?
Can affect absorption, bioavailability, or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying.
What enzyme does Zileuton inhibit?
Lipoxygenase
What enzymes are inhibited by NSAIDs, acetaminophen and COX II inhibitors?
Cyclooxygenases (COX I, COX II).
What is a common side effect of Colchicine used to treat acute gout, especially when given orally?
GI side effects. (Note: Indomethacin is less toxic, more commonly used.)
What is a common side effect of Misoprostol?
Diarrhea
What is a possible result of overdose of Acetaminophen?
Overdose produces hepatic necrosis; acetaminophen metablolite depletes glutathione and forms toxic tissue adducts in liver.
What is a possible toxicity of Alpha-glucosidase inhibitors used in type-2 diabetes?
GI disturbances.
What is a possible toxicity of Ticlopidine, Clopidogrel usage?
Neutropenia (ticlopidine); reserved for those who cannot tolerate aspirin.
What is a sign of toxicity with the use of thrombolytics?
Bleeding.
What is action of insulin in the liver, in muscle, and in adipose tissue?
1. In liver, increases storage of glucose as glycogen. 2. In muscle, stimulates glycogen and protein synthesis, and K+ uptake. 3. In adipose tissue, facilitates triglyceride storage.
What is are two clinical uses of Cyclosporine?
1. Suppresses organ rejection after transplantation 2. Selected autoimmune disorders.
What is the category and mechanism of action of Zafirlukast in Asthma treatment?
Antileukotriene; blocks leukotriene receptors.
What is the category and mechanism of action of Zileuton in Asthma treatment?
Antileukotriene; blocks synthesis by lipoxygenase.
What is the category of drug names ending in -ane (e.g. Halothane)
Inhalational general anesthetic.
What is the category of drug names ending in -azepam (e.g. Diazepam)
Benzodiazepine.
What is the category of drug names ending in -azine (e.g. Chlorpromazine)
Phenothiazine (neuroleptic, antiemetic).
What is the category of drug names ending in -azol (e.g. Ketoconazole)
Antifungal.
What is the category of drug names ending in -barbital (e.g. Phenobarbital)
Babiturate.
What is the category of drug names ending in -caine (e.g. Lidocaine)
Local anesthetic.
What is the category of drug names ending in -cillin (e.g. Methicillin)
Penicillin.
What is the category of drug names ending in -cycline (e.g. Tetracycline)
Antibiotic, protein synthesis inhibitor.
What is the category of drug names ending in -ipramine (e.g. Imipramine)
Tricyclic antidepressant.
What is the category of drug names ending in -navir (e.g. Saquinavir)
Protease inhibitor.
What is the category of drug names ending in -olol (e.g. Propranolol)
Beta antagonist.
What is the category of drug names ending in -operidol (e.g. Haloperidol)
Butyrophenone (neuroleptic).
What is the category of drug names ending in -oxin (e.g. Digoxin)
Cardiac glycoside (inotropic agent).
What is the category of drug names ending in -phylline (e.g. Theophylline)
Methylxanthine.
What is the category of drug names ending in -pril (e.g. Captopril)
ACE inhibitor.
What is the category of drug names ending in -terol (e.g. Albuterol)
Beta-2 agonist.
What is the category of drug names ending in -tidine (e.g. Cimetidine)
H2 antagonist
What is the category of drug names ending in -triptyline (e.g. Amitriptyline)
Tricyclic antidepressant.
What is the category of drug names ending in -tropin (e.g. Somatotropin)
Pituitary hormone.
What is the category of drug names ending in -zosin (e.g. Prazosin)
Alpha-1 antagonist
What is the category, desired effect, and adverse effect of Isoproterenol in the treatment of Asthma?
Nonspecific beta-agonist; desired effect is the relaxation of bronchial smooth muscle (Beta 2). Adverse effect is tachycardia (Beta 1).
What is the category, desired effect, and period of use of albuterol in the treatment of Asthma?
Beta 2 agonist; desired effect is the relaxation of bronchial smooth muscle (Beta 2). Use during acute exacerbation.
What is the category, desired effect, and possible mechanism of Theophylline in treating Asthma?
Methylzanthine; desired effect is bronchodilation, may cause bronchodilation by inhibiting phosphodiesterase, enzyme involved in degrading cAMP (controversial).
What is the category, mechanism of action, and effect of Ipratroprium in Asthma treatment?
Muscarinic antagonist; competatively blocks muscarinic receptors, preventing bronchoconstriction.
What is the category, mechanism of action, and particular use of beclomethasone and prednisone in Asthma treatment?
Corticosteroids; prevent production of leukotrienes from arachodonic acid by blocking phospholipase A2. Drugs of choice in a patient with status asthmaticus (in combination with albuterol.)
What is the category, method of use, and adverse effects of Salmeterol in Asthma treatment?
Beta 2 agonist; used as a long-acting agent for prophylaxis. Adverse effects are tremor and arrhythmia.
What is the clincial use for Misoprostol?
Prevention of NSAID-induced peptic ulcers, maintains a PDA.
What is the clinical use for Clomiphene?
Treatment of infertility.
What is the clinical use for Heparin?
Immediate anticoagulation for PE, stroke, angina, MI, DVT.
What is the clinical use for Sildenafil (Viagra)?
Erectile dysfunction.
What is the clinical use for Sucralfate?
Peptic ulcer disease.
What is the clinical use for Warfarin?
Chronic anticoagulation.
What is the clinical use of Mifepristone (RU486)?
Abortifacient.
What is the clinical use of Tacrolimus (FK506)?
Potent immunosuppressive used in organ transplant recipients.
What is the effect of the Glitazones in diabetes treatment?
Increase target cell response to insulin.
What is the enzyme inhibited, the effect of this inhibition, and the clinical use of the antiandrogren Finasteride?
Finasteride inhibits 5 Alpha-reductase, this decreases the conversion of testosterone to dihydrotestosterone, useful in BPH
What is the lab value used to monitor the effectiveness of Heparin therapy?
The PTT.
What is the lab value used to monitor the effectiveness of Warfarin therapy?
The PT.
What is the main clinical use for the thrombolytics?
Early myocardial infarction.
What is the mecanism of action of Sucralfate?
Aluminum sucrose sulfate polymerizes in the acid environment of the stomach and selectively binds necrotic peptic ulcer tissue. Acts as a barrier to acid, pepsin, and bile.
What is the mecanism of action of the COX-2 inhibitors (celecoxib, rofecoxib)?
Selectively inhibit cyclooxygenase (COX) isoform 2, which is found in inflammatory cells nad mediates inflammation and pain; spares COX-1 which helps maintain the gastric mucosa.
What is the mecanism of action, effective period, and ineffective period of use for Cromolyn in treating Asthma?
Prevents release of mediators from mast cells. Effective only for the prophylaxis of asthma. Not effective during an acute attack.
What is the mechanism of action and clinical use of the antiandrogen Flutamide?
Flutamide is a nonsteroidal competitive inhibitor of androgens at the testosterone receptor, used in prostate carcinoma.
What is the mechanism of action and clinical use of the antiandrogens Ketoconazole and Spironolactone?
Inhibit steroid synthesis, used in the treatment of polycystic ovarian syndrome to prevent hirsutism.
What is the mechanism of action of Acetaminophen?
Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally.
What is the mechanism of action of Allopurinol used to treat chronic gout?
Inhibits xanthine oxidase, decresing conversion of xanthine to uric acid.
What is the mechanism of action of Aspirin?
Acetylates and irreversibly inhibits cyclooxygenase (COX I and COX II) to prevent the conversion of arachidonic acid to prostaglandins.
What is the mechanism of action of Clomiphene?
Clomiphene is a partial agonist at estrogen receptors in the pituitary gland. Prevents normal feedback inhibition and increses release of LH and FSHfrom the pituitary, which stimulates ovulation.
What is the mechanism of action of Colchicine used to treat acute gout?
Depolymerizes microtubules, impairing leukocyte chemotaxis and degranulation.
What is the mechanism of action of Cyclosporine?
Binds to cyclophilins (peptidyl proline cis-trans isomerase), blocking the differentiation and activation of T cells mainly by inhibiting the production of IL-2 and its receptor.
What is the mechanism of action of Heparin?
Heparin catalyzes the activation of antithrombin III.
What is the mechanism of action of Mifepristone (RU486)?
Competitive inibitor of progestins at progesterone receptors.
What is the mechanism of action of Misoprostol?
Misoprostol is a PGE1 analog that increases the production and secretion of the gastic mucous barrier.
What is the mechanism of action of NSAIDs other than Aspirin?
Reversibly inhibit cyclooxygenase (COX I and COX II). Block prostaglandin synthesis.
What is the mechanism of action of Omeprazole, Lansoprazole?
Irreversibly inhibits H+/K+ ATPase in stomach parietal cells.
What is the mechanism of action of Probenacid used to treat chronic gout?
Inhibits reabsorption of uric acid.
What is the mechanism of action of Sildenafil (Viagra)?
Inhibits cGMP phosphodiesterase, casuing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow, and penile erection.
What is the mechanism of action of the Alpha-glucosidase inhibitors?
Inhibit intestinal bursh border Alpha-glucosidases; delayed hydrolysis of sugars and absorption of sugars leading to decresed postprandial hyperglycemia.
What is the mechanism of action of the glucocorticoids?
Decrease the production of leukotrienes and protaglandins by inhibiting phospholipase A2 and expression of COX-2.
What is the mechanism of action of the H2 Blockers?
Reversible block of histamine H2 receptors
What is the mechanism of action of the Sulfonylureas?
Close K+ channels in Beta-cell membrane leading to cell depolarization causing insulin release triggered by increase in Calcium ion influx.
What is the mechanism of action of the thrombolytics?
Directly of indirectly aid conversion of plasminogen to plasmin which cleaves thrombin and fibrin clots. (It is claimed that tPA specifically converts fibrin-bound plasminogen to plasmin.)
What is the mechanism of action of Ticlopidine, Clopidogrel
Inhibits platelet aggregation by irreversibly inhibiting the ADP pathway involved in the binding of fibrinogen.
What is the mechanism of action of Warfarin (Coumadin)?
Warfarin interferes with the normal synthesis and gamma-carboxylation of vitamin K-dependent clotting factors II, VII, IX, and X, Protein C and S via vitamin K antagonism.
What is the mechanism of Azathioprine?
Antimetabolite derivative of 6-mercaptopurine that interferes with the metablolism and synthesis of nucleic acid.
What is the mechanism of Leuprolide?
GnRH analog with agonist properties when used in pulsatile fashion and antagonist properties when used in continuous fashion, causing a transient initial burst of LH and FSH
What is the mechanism of Tacrolimus (FK506)?
Similar to cyclosporine; binds to FK-binding protein, inhibiting secretion of IL-2 and other cytokines.
What is the memory key for the action of Sildenafil (Viagra)?
Sildenafil fills the penis
What is the memory key for the effect of aluminum hydroxide overuse?
AluMINIMUM amount of feces.
What is the memory key for the effect of magnesium hydroxide overuse?
Mg = Must go to the bathroom.
What is the memory key to remember which pathway (extrinsic vs. intrinsic) and which lab value Warfarin affects?
WEPT: Warfarin affects the Extrinsic pathway and prolongs the PT.
What is the possible mechanism and effect of Metformin in treating diabetes?
Mechanism unknown; possibly inhibits gluconeogenesis and increases glycolysis; effect is to decrease serum glucose levels
What is the specific clinical use of Indomethacin in neonates?
Indomethacin is used to close a patent ductus arteriosus.
What is used to reverse the action of Heparin?
Protamine Sulfate is used for rapid reversal of heparinization (positively charged molecule that binds to negatively charged heparin).
What patients are at risk for life threatening hypotension when taking Sildenafil (Viagra)?
Those patients who are taking nitrates.
What process does Zafirlukast interfere with?
Leukotrienes increasing bronchial tone.
What type of gout is treated with Allopurinol?
Chronic gout.
What type of gout is treated with Colchicine?
Acute gout.
What type of gout is treated with Probenacid?
Chronic gout.
What type of patient should not take Misoprostol and why?
Misoprostol is contraindicated in women of childbearing potential because it is an abortifacient.
Which H2 Blocker has the most toxic effects and what are they?
Cimetidine is a potent inhibitor of P450; it also has an antiandrogenic effect and decreases renal excretion of creatinine. Other H2 blockers are relatively free of these effects.
Why are the Sulfonylureas inactive in IDDM (type-1)?
Because they require some residual islet function.
Acetaldehyde is metabolized by Acetaldehyde dehydrogenase, which drug inhibs this enzyme?
-Disulfram & also sulfonylureas, metronidazole
Explain pH dependent urinary drug elimination?
-Weak Acids>Alkinalize urine(CO3) to remove more -Weak bases>acidify urine to remove more
How do you treat coma in the ER (4)?
-Airway -Breathing -Circulation -Dextrose(thiamine &narcan) -ABCD
In coma situations you rule out what (7)?
-Infections -Trauma -Seizures -CO -Overdose -Metabolic -Alcohol (IT'S COMA)
List some specifics of lead poisoning(4)?
-A57Blue lines in gingiva& long bones -Encephalopathy & Foot drop -Abdominal colic / -Sideroblastic anemia
List the specific antidote for this toxin: Acetaminophen
-N-acetylcystine
List the specific antidote for this toxin: Amphetamine
-Ammonium Chloride
List the specific antidote for this toxin: Anticholinesterases (organophosphate.)
-Atropine & pralidoxime
List the specific antidote for this toxin: Antimuscarinic (anticholinergic)
-Physostigmine salicylate
List the specific antidote for this toxin: Arsenic (all heavy metals)
-Dimercaprol, succimer
List the specific antidote for this toxin: Benzodiazepines
-Flumazenil
List the specific antidote for this toxin: Beta Blockers
-Glucagon
List the specific antidote for this toxin: Carbon monoxide
-100% oxygen, hyperbaric
List the specific antidote for this toxin: Copper
-Penicillamine
List the specific antidote for this toxin: Cyanide
-Nitrate, hydroxocobalamin thiosulfate
List the specific antidote for this toxin: Digitalis
-Normalize K+, Lidocaine, & Anti-dig Mab
List the specific antidote for this toxin: Heparin
-Protamine
List the specific antidote for this toxin: Iron
-Deferoxamine
List the specific antidote for this toxin: Lead
-EDTA, dimercaprol, succimer, & penicillamine
List the specific antidote for this toxin: Methanol & Ethylene glycol
-Ethanol, dialysis, & fomepizole
List the specific antidote for this toxin: Methemoglobin
-Methylene blue
List the specific antidote for this toxin: Opioids
-B51Naloxone / naltrexone (Narcan)
List the specific antidote for this toxin: Salicylates
-Alkalinize urine & dialysis
List the specific antidote for this toxin: TPA & Streptokinase
-Aminocaproic acid
List the specific antidote for this toxin: Tricyclic antidepressants
-NaHCO3
List the specific antidote for this toxin: Warfarin
-Vitamin K & fresh frozen plasma
What are the products and their toxicities of the metabolism of ethanol by / alcohol dehydrogenase?
-Acetaldehyde -Nausea, vomiting, headache, & hypotension
What are the products and their toxicities of the metabolism of Ethylene Glycol by / alcohol dehydrogenase?
-Oxalic acid -Acidosis & nephrotoxicity
What are the products and their toxicities of the metabolism of Methanol by / alcohol dehydrogenase?
-Formaldehyde & formic acid -severe acidosis & retinal damage
Which drug(s) cause this reaction: Adrenocortical Insufficiency
-Glucocorticoid withdrawal
Which drug(s) cause this reaction: Agranulocytosis (3)?
-Cloazapine -carbamazapine -colchicine -PTU
Which drug(s) cause this reaction: Anaphylaxis?
-Penicillin
Which drug(s) cause this reaction: Aplastic anemia (5)?
-Chloramphenicol -benzene -NSAIDS -PTU -phenytoin
Which drug(s) cause this reaction: Atropine-like side effects?
-Tricyclic antidepressants
Which drug(s) cause this reaction: Cardiac toxicity?
-Daunorubicin & Doxorubicin
Which drug(s) cause this reaction: Cinchonism (2)?
-Quinidine -quinine
Which drug(s) cause this reaction: Cough?
-ACE inhibitors (Losartan>no cough)
Which drug(s) cause this reaction: Cutaneous flushing (4)?
-Niacin -Ca++ channel blockers -adenosine -vancomycin
Which drug(s) cause this reaction: Diabetes insipidus?
-Lithium
Which drug(s) cause this reaction: Disulfram-like reaction (4) ?
-Metronidazole -certain cephalosporins -procarbazine -sulfonylureas
Which drug(s) cause this reaction: Drug induced Parkinson's (4) ?
-Haloperidol -chlorpromazine -reserpine -MPTP
Which drug(s) cause this reaction: Extrapyramidal side effects (3)?
-Chlorpromazine -thioridazine -haloperidol
Which drug(s) cause this reaction: Fanconi's syndrome?
-Tetracycline
Which drug(s) cause this reaction: Focal to massive hepatic necrosis (4)?
-Halothane -Valproic acid -acetaminophen -Amantia phalloides
Which drug(s) cause this reaction: G6PD hemolysis(8)?
-Sulfonamides -INH -ASA -Ibuprofen -primaquine -nitrofurantoin /-pyrimethamine -chloramphenicol
Which drug(s) cause this reaction: Gingival hyperplasia?
-Phenytoin
Which drug(s) cause this reaction: Gray baby syndrome?
-Chloramphenicol
Which drug(s) cause this reaction: Gynecomastia (6) ?
-Cimetidine -ketoconazole -spironolactone -digitalis -EtOH -estrogens
Which drug(s) cause this reaction: Hepatitis?
-Isoniazid
Which drug(s) cause this reaction: Hot flashes?
-Tamoxifen
Which drug(s) cause this reaction: Neuro and Nephrotoxic?
-polymyxins
Which drug(s) cause this reaction: Osteoporosis (2)?
-Corticosteroids -heparin
Which drug(s) cause this reaction: Oto and Nephrotoxicity (3)?
-aminoglycosides -loop diuretics -cisplatin
Which drug(s) cause this reaction: P450 induction(6)?
-Barbiturates -phenytoin -carbamazipine -rifampin -griseofulvin -quinidine
Which drug(s) cause this reaction: P450 inhibition(6)?
-Cimetidine -ketoconazole -grapefruit juice -erythromycin -INH -sulfonamides
Which drug(s) cause this reaction: Photosensitivity(3)?
-Tetracycline -amiodarone -sulfonamides
Which drug(s) cause this reaction: Pseudomembranous colitis?
-Clindamycin
Which drug(s) cause this reaction: Pulmonary fibrosis(3)?
-Bleomycin -amiodarone -busulfan
Which drug(s) cause this reaction: SLE-like syndrome
-Hydralazine -Procainamide -INH -phenytoin
Which drug(s) cause this reaction: Stevens-Johnson syn. (3) ?
-Ethosuxamide -sulfonamides -lamotrigine
Which drug(s) cause this reaction: Tardive dyskinesia?
-Antipsychotics
Which drug(s) cause this reaction: Tendonitis and rupture?
-Fluoroquinolones
Which drug(s) cause this reaction: Thrombotic complications?
-Oral Contraceptives
Which drug(s) cause this reaction: Torsade de pointes (2) ?
-Class III antiarrhythmics (sotalol) -class IA (quinidine)
Which drug(s) cause this reaction: Tubulointerstitial Nephritis (5)?
-Sulfonamides -furosemide -methicillin -rifampin -NSAIDS (ex. ASA)
Describe first-order kinetics? 
Constant FRACTION eliminated per unit time.(exponential)
Describe Phase I metabolism in liver(3)?
-reduction, oxy, & hydrolysis -H2O sol. Polar product -P450
Describe Phase II metabolism in liver(3)?
-acetylation, glucuron.,& sulfation -Conjugation -Polar product
Explain differences between full and partial agonists(2).
- Act on same receptor - Full has greater efficacy
Explain potency in relation to full and partial agonists(2).
- partial agonist can have increased, decreased, /A21or equal potency as full agonist. - Potency is an independent factor.
How do spare receptors effect the Km?
- ED 50 is less than the Km (less than 50% of receptors)
How do you calculate maintenance dose?
Md= (CpxCL)/F Cp= plas. Conc. CL=clear. F=bioaval.
How does a competitive antagonist effect an agonist?
-Shifts the curve to the right -increases Km
How does a noncompetitive antagonist effect an agonist?
- Shifts the curve down -reduces Vmax
Name the steps in drug approval(4)?
-Phase I (clinical tests) -Phase II -Phase III -PhaseIV (surveillance)
Steady state concentration is reached in __#half-lifes
In 4 half-lifes= (94%) T1/2 = (0.7x Vd)/CL
What is the definition of zero-order kinetics? Example?
-Constant AMOUNT eliminated per unit time. -Etoh &ASA
What is the formula for Clearance (CL)
CL= (rate of elimination of drug/ Plasma drug conc.)
What is the formula for Volume of distribution (Vd)
Vd= (Amt. of drug in body/ Plasma drug conc.)
What is the loading dose formula?
Ld= (CpxVd)/F    Cp=plasma conc. F= Bioaval.
A 12yo patient was treated for a reaction to a bee sting, what drug provides the best coverage of sympathomimetic receptors?
Epinephirine(Alpha1,2 and Beta 1,2)
A 57 yo heart failure pt develops cardiac decompensation, what drug will give you adequate perfusion of his kidneys as well as tx for his Hypotension
Dopamine
A fellow passenger on a Carnival cruise ship looks pale and diaphoretic, what antimuscarinic agent would you give them?
scopolamine
A group of pts are rushed into the ER complaining of excessive sweating, tearing, salivation, HA, N and V, muscle twitching, difficulty breathing and diarrhea. What drug would be the most effective immediate tx
Atropine pts are suffering from Cholinestrase inhibitor poisining(Nerve gas/Organophosphate poisining)
As an Anes you want to use a depolarizing neuromuscular blocking drug on your pt, what do you use
Succinylcholine
By what mechanism does this drug help
Prevents the release of Ca from SR of skeletal muscle
Clonidine is the preferred sym pathomimetic tx of HTN in pts with renal disease, why??
Centrally acting alpha agonist, thus causing a decrease in central adrenergic outflow, spairing renal blood flow
Cocaine casues vasoconstriction and local anesthesia by what mechanism
Indirect agonist, uptake inhibitor
Cocaine shares is mechanism of action with what antidepressant
TCA
Dobutamine used for the tx of shock acts on which receptors
Beta1 more than B2
Guanethidine enhances the release of Norepi?
No, it inhibits the release of Nor Epi
How does angiotensin II affect NE release?
It acts presynaptically to increase NE release.
How does botulinum toxin result in respiratory arrest?
Prevents the release of ACh, which results in muscle paralysis.
How does dantrolene work?
Prevents the release of calcium from the sarcoplasmic reticulum of skeletal muscle.
How does NE modulate its own release?  What other neurotransmitter has this same effect?
NE acts presynaptically on alpha-2 receptors to inhibit its own release.  ACh also acts presynaptically through M1 receptors to inhibit NE release.
How would hemicholinium treatment affect cholinergic neurons?
Hemicholinium inhibits the transport of choline into the nerve, thus inhibiting formation of ACh.
How would you reverse the effect of a neuromuscular blocking agent?
Give an antichloinesterase - neostigmine, edrophonium, etc
If a patient is given hexamethonium, what would happen to his/her heart rate?
It would increase to ~ 100 beats/min. Both sympathetic and vagal stimulation would be knocked out, but the SA node has an intrinsic pace of 100 beats/min, which is normally checked by vagal stimulation.
Isopoterenol was given to a patient with a developing AV block, why?
Stimulates beta adrenergic receptors
Norepi feedbacks and inhibits the presynaptic receptor by what mechanism
Binding to the presynaptic alpha 2 release modulating receptors
Reserpine will block the syntheis of this drug and but not its precursor.
Blocks Norepi, but not Dopamine
These drugs acts indirectly by releasing strored catecholamines in the presynaptic terminal
Amphetamine and Ephedrine
What anticholinesterase crosses the blood-brain-barrier?
physostigmine
What antimuscarinic agent is used in asthma and COPD?
Ipratropium
What antimuscarinic drug is useful for the tx of asthma
Ipratropium
What are the classic symptoms of cholinesterase inhibitor poisoning (parathion or other organophosphates)?
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, and Salivation = DUMBBELS; also abdominal cramping
What are the clinical indications for bethanechol?
Activates cholinergic receptors on bladder and bowel smooth muscle, alleviating post-op and neurogenic ileus and urinary retention.
What are the clinical indications for neostigmine?
Post-op and neurogenic ileus and urinary retention, myasthenia gravis, and reversal of neuromuscular junction blockade (post-op) through anticholinesterase activity.
What are the indications for using amphetamine?
narcolepsy, obesity, and attention deficit disorder (I wouldn't recommend this)
What are the nondepolarizing neuromuscular blocking drugs?
Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rapacuronium
What are the phases of succinylcholine neuromuscular blockade?
Phase 1 = prolonged depolarization, no antidote, effect potentiated by anticholinesterase; Phase 2 = repolarized but blocked, an anticholinesterase is the antidote for this phase.
What are two indirect acting adrenergic agonists?
amphetamine and ephedrine
What beta 2 agonist will help your 21yo Astma pt?
Albuterol, tertbutaline
What cholinergic inhibitor acts by directly inhibiting Ach release at the presynaptic terminal
Botulinum
What cholinomimetic is useful in the diagnosis of Myasthenia Gravis
Edrophonium
What cholinomimetics might your pt be taking for his glaucoma
Carbachol, pilocarpine, physostigmine, echothiophate
What class of drug is echothiophate?  What is its indication?
anticholinesterase  glaucoma
What conditions would you use dantrolene?
In treatment of malignant hyperthermia, due to concomitant use of halothane and succinylcholine. Also in neuroleptic malignant syndrome, a toxicity of antipsychotic drugs.
What drug is used to diagnose myasthenia gravis?
edrophonium (extremely short acting anticholinesterase)
What drugs target this enzyme
Neostigmine, pyridostigmine edrophonium physostigmine echothiophate
What effect would atropine have on a patient with peptic ulcer disease?
Theoretically it could be used to block the cephalic phase of acid secretion (vagal stimulation).
What effect would atropine have on the preganglionic sympathetic activation of sweat glands? Would this person sweat?
None. No, because atropine would block the postganglionic muscarinic receptors involved in sweat gland stimulation.
What enzyme is responsible for the breakdown of ACh in the synaptic cleft?
Acetylcholinesterase; ACh is broken down into choline and acetate.
What enzyme is responsible for the degredation of Ach
Acetylcholine esterase
What enzyme is responsible for the production of Ach from Acetyl CoA and Choline
Choline acetyltransferase
What is the clinical utility of clonidine?
Treatment of hypertension, especially with renal disease (lowers bp centrally, so flow is maintained to kidney).
What is the clinical utility of cocaine?
The only local anesthetic with vasoconstrictive properties.
What is the difference between the affinity for beta receptors between albuterol/terbutaline and dantroline?
Dobutamine has more of an affintiy for beta-1 than beta-2, and is used for treating heart failure and shock. Albuterol and terbutaline is the reverse, and is used in treatment of acute asthma.
What is the difference in receptor affinity of epinephrine at low doses? High doses?
Prefers beta's at low doses, but at higher doses alpha agonist effects are predominantly seen.
What is the effect of epinephrine infusion on bp and pulse pressure?
Increased systolic and pulse pressure, decreased diastolic pressure, and little change in mean pressure.
What is the effect of guanethidine on adrenergic NE release?
It inhibits release of NE.
What is the effect of norepinephrine on bp and pulse pressure?
Increases mean, systolic, and diastolic bp, while there is little change in pulse pressure.
What is the effect of TCA's on the adrenergic nerve?
They inhibit reuptake of NE at the nerve terminal (as does cocaine).
What is the only depolarizing neuromuscular blocking agent?
Succinylcholine
What is the receptor affinity and clinical use of isoproterenol?
It affects beta receptors equally and is used in AV heart block (rare).
What makes this drug effective
It antagonizes Ach M receptors and decreases parasym (GI) rxn
What nondepolorizing agents could you have used
Tubocurarine, atra-, miv-, pan-,ve-, rapacuronium
What other substances regulate the Norepi nerve ending
Ach, AngiotensinII
What other syndrome can this drug tx
Neuroleptic malignant syndrome
What physiological effects was the Anes using Atropine to tx
SLUD (salivation, Lacrimation, urination, Defecation)as well as airway secretion, GI motility, acid secretions
What reversal agent could a Anes give to reverse the effects of Atropine
Bethanechol, Neostigmine, physostigmine
What side effect of using atropine to induce pupillary dilation would you expect?
Atropine would also block the receptors in the ciliary muscle, causing an impairment in accommodation (cycloplegia).
What sympathomimetic would you not prescribe for hypotension in a pt with renal artery sclerosis.
Norepinephrine (Alpha1,2 and beta 1)
What type of neurological blockade would hexamethonium create?
Hexamethonium is a nicotinic antagonist, and thus is a ganglionic blocker.
What would be the effect on blood pressure with infusion of the alpha -2 agonist clonidine?
Initially vasoconstriction would increase bp, but then it acts on central alpha-2 receptors to decrease adrenergic outflow resulting in decreased bp.
What would be the next drug that you would give and why
Pralidoxime, regenerates active cholinestrase
Which antimuscarinic agents are used in producing mydriasis and cycloplegia?
atropine, homatropine, tropicamide
Which drug increases Sys BP w/o affecting Pulse Pressure
Epinephrine
Which of epi, norepi, or isoproterenol results in bradycardia?
Norepinephrine
Which of the following would atropine administration cause? Hypothermia, bradycardia, excess salivation, dry flushed skin, or diarrhea
Dry flushed skin, due to inhibition of sympathetic post-ganglionic blockade on muscarinic receptors of sweat glands. All others are opposite of what would be expected.
Which of these three drugs will cause a reflex bradycardia in your pt (Norepi, Epi, or Isoporterenol)
Norepinephrine
Which receptors does phenylephrine act upon?
alpha-1 > alpha-2; used as a pupil dilator, vasoconstrictor, and for nasal decongestion
While at a tail gait party, you bite into a sandwich that a yellow jacket is also enjoying. Knowing your allergy to this creature, what should you do?
Epinephrine to treat anaphylaxis. Also useful if you have open angle glaucoma, asthma, or hypotension.
Why are albuterol and terbutaline effective in tx of acute asthmatic attacks?
These B-2 agonists cause respiratory smooth muscle to relax.
Why does atropine dilate the pupil?
Blocking muscarinic receptors in the circular fibers of the eye, results in unopposed action of radial muscles to dilate.
Why does NE result in bradycardia?
NE increases bp, which stimulates baroreceptors in the carotid sinus and the aorta. The CNS signals through vagal stimulation to decrease heart rate.
Why is carbachol and pilocarpine useful in treatment of glaucoma?
They activate the ciliary muscle of the eye (open angle) and pupillary sphincter (narrow angle).
Why is pyridostigmine effective in the treatment of myasthenia gravis?
As an anticholinesterase it increases endogenous ACh and thus increases strength.
Why is reserpine effective in treating HTN?
Reserpine inhibits dopamine transport into vesicles, attenuating its conversion to NE by dopamine beta-hydroxylase.
Why is there a drop in systolic, mean, and diastolic bp with infusion of isoproterenol?
Stimulating beta receptors stimulates heart rate, but beta receptor induced vasodilation reduces peripheral resistance.
Why would a patient with cog-wheel rigidity and a shuffling gait be given benztropine?
Parkinson patients benefit from antimuscarinic agents through its inhibitory action within the indirect pathway.
Why would dopamine be useful in treating shock?
Receptors = D1=D2>beta>alpha, thus increasing heart rate (beta) and blood pressure (alpha vasoconstriction) while maintaining kidney perfusion (dopamine receptors)
Why would you give a drug like pancuronium or succinylcholine?
Useful in muscle paralysis during surgery or mechanical ventilation.
Why would you use pralidoxime after exposure to an organophosphate?
Pralidoxime regenerates active cholinesterase.
Will Hemicholinum affect the release of stored Ach during Cholinergic Stimulation
No, hemicholinum block the uptake of Choline and thus Ach synthesis
Would blockade of muscarininc receptors in the bladder be useful in treating urinary retention?
No. Atropine is used to reduce urgency in mild cystitis. So it would aggravate the urinary retention.
Would Hexamethonium be an effective substitute
No, hexamethonium targets Nicotinc receptors and will block Parasym, Sym, as well as Somatic systems
You tx your pt with halothane as well and he has also developed malignant hypothermia, what drug can you give
Dantrolene
Your patient develops a marked arrythmia due to a prolonged depolarization, can you tx this w/ Neostigmine
No cholinesterase inhibitors will potentiate the stimulating action of Succinlycholine
Your patient has acute angle glaucoma, does this affect your tx
Yes, Scopolamine would antagonize his glaucoma
Your patient wants an effective drug to treat his motion sickness, what would you prescribe
Scopolamine