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Pharmacology-USMLE-Step 1

copied fr dartmouthmed2010 (june 08)
STUDY
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Neutropenia
A common side effects of Interferon (INF) treatment is?
TMP-SMZ
Antimicrobial prophylaxis for a history of recurrent UTIs
Ceftriaxone
Antimicrobial prophylaxis for Gonorrhea
Rifampin (DOC), minocycline
Antimicrobial prophylaxis for Meningococcal infection
TMP-SMZ (DOC), aerosolized pentamidine
Antimicrobial prophylaxis for PCP
Benzathine penicillin G
Antimicrobial prophylaxis for Syphilis
Yes
Are Aminoglycosides Teratogenic?
No
Are Ampicillin and Amoxicillin penicillinase resistant?
No
Are Carbenicillin, Piperacillin, and Ticarcillin penicillinase resistant?
No, but they are less susceptible than the other Beta lactams
Are Cephalosporins resistant to penicillinase?
Yes
Are Methicillin, Nafcillin, and Dicloxacillin penicillinase resistant?
Mycobacterium tuberculosis, the only agent used as solo prophylaxis against TB
Clinical use of Isoniazid (INH)?
Pseudomembranous colitis (C. difficile), fever, diarrhea
Common side effects associated with Clindamycin include?
GI upset, Superinfections, Skin rashes, Headache, Dizziness
Common toxicities associated with Fluoroquinolones?
Teratogenic, Carcinogenic, Confusion, Headaches
Common toxicities associated with Griseofulvin?
Glycoproteins from leukocytes that block various stages of viral RNA and DNA synthesis
Describe the MOA of Interferons (INF)
Only in limited amounts
Do Tetracyclines penetrate the CNS?
AmOxicillin has greater Oral bioavailability
Does Ampicillin or Amoxicillin have a greater oral bioavailability?
No
Does Amprotericin B cross the BBB?
No
Does Foscarnet require activation by a viral kinase?
Nephrotoxicity
Foscarnet toxicity?
Leukopenia, Neutropenia, Thrombocytopenia, Renal toxicity
Ganciclovir associated toxicities?
Chronic Hepatitis A and B, Kaposi's Sarcoma
How are Interferons (INF) used clinically?
Gram +, Gram -, Norcardia, Chlamydia
How are Sulfonamides employed clinically?
Triple Therapy' 2 Nucleoside RT Inhibitors with a Protease Inhibitor
How are the HIV drugs used clinically?
Primaquine
How are the Latent Hypnozoite (Liver) forms of Malaria (P. vivax, P.ovale) treated?
Pyridoxine (B6) administration
How can Isoniazid (INH)-induced neurotoxicity be prevented?
Fast vs. Slow Acetylators
How can the t1/2 of INH be altered?
With supplemental Folic Acid
How can the toxic effects of TMP be ameliorated?
Pretreat with antihistamines and a slow infusion rate
How can Vancomycin-induced 'Red Man Syndrome' be prevented?
As PABA antimetabolites that inhibit Dihydropteroate Synthase, Bacteriostatic
How do Sulfonamides act on bacteria?
Inhibt Assembly of new virus by Blocking Protease Enzyme
How do the Protease Inhibitors work?
Ganciclovir is more toxic to host enzymes
How does Ganciclovir's toxicity relate to that of Acyclovir?
With an amino acid change of D-ala D-ala to D-ala D-lac
How does resistance to Vancomycin occur?
HSV, VZV, EBV, Mucocutaneous and Genital Herpes Lesions, Prophylaxis in Immunocompromised pts
How is Acyclovir used clinically?
Prophylaxis for Influenza A, Rubella; Parkinson's disease
How is Amantadine used clinically?
Intrathecally
How is Amphotericin B administered for fungal meningitis?
Wide spectrum of systemic mycoses: Cryptococcus, Blastomyces, Coccidioides, Aspergillus, Histoplasma, Candida, Mucor
How is Amphotericin B used clinically?
Meningitis (H. influenza, N. meningitidis, S. pneumoniae), Conserative treatment due to toxicities
How is Chloramphenical used clinically?
CMV Retinitis in IC pts when Ganciclovir fails
How is Foscarnet used clinically?
Phosphorylation by a Viral Kinase
How is Ganciclovir activated?
CMV, esp in Immunocompromised patients
How is Ganciclovir used clinically?
Oral treatment of superficial infections
How is Griseofulvin used clinically?
Pentavalent Antimony
How is Leishmaniasis treated?
for RSV
How is Ribavirin used clinically?
1. Mycobacterium tuberculosis 2. Delays resistance to Dapsone when used of Leprosy 3. Used in combination with other drugs
How is Rifampin used clinically?
Used in combination therapy with SMZ to sequentially block folate synthesis
How is Trimethoprim used clinically?
For serious, Gram + multidrug-resistant organisms
How is Vancomycin used clinically?
Suramin
How would you treat African Trypanosomiasis (sleeping sickness)?
Premature infants, because they lack UDP-glucuronyl transferase
In what population does Gray Baby Syndrome occur? Why?
No
Is Aztreonam cross-allergenic with penicillins?
Yes
Is Aztreonam resistant to penicillinase?
No
Is Aztreonam usually toxic?
Yes
Is Imipenem resistant to penicillinase?
No - duh
Is Penicillin penicillinase resistant?
Penicillin-G
IV Penicillin
Foscarnet = pyroFosphate analog
Mnemonic for Foscarnet?
1)Binds penicillin-binding proteins 2) Blocks transpeptidase cross- linking of cell wall 3) Activates autolytic enzymes
MOA for Penicillin (3 answers)?
Penicillin, Cephalosporins, Vancomycin, Aminoglycosides, Fluoroquinolones, Metronidazole
MOA: Bactericidal antibiotics
Penicillin, Ampicillin, Ticarcillin, Pipercillin, Imipenem, Aztreonam, Cephalosporins
MOA: Block cell wall synthesis by inhib. Peptidoglycan cross-linking (7)
Quinolones
MOA: Block DNA topoisomerases
Rifampin
MOA: Block mRNA synthesis
Sulfonamides, Trimethoprim
MOA: Block nucleotide synthesis
Bacitracin, Vancomycin
MOA: Block peptidoglycan synthesis
Aminoglycosides, Tetracyclines
MOA: Block protein synthesis at 30s subunit
Chloramphenicol, Erythromycin/macrolides, Lincomycin, Clindamycin, Streptogramins (quinupristin, dalfopristin)
MOA: Block protein synthesis at 50s subunit
Polymyxins
MOA: Disrupt bacterial/fungal cell membranes
Amphotericin B, Nystatin, Fluconazole/azoles
MOA: Disrupt fungal cell membranes
Polymyxin B, Polymyxin E
Name common Polymyxins
Erythromycin, Azithromycin, Clarithromycin
Name several common Macrolides (3)
Sulfamethoxazole (SMZ), Sulfisoxazole, Triple sulfas, Sulfadiazine
Name some common Sulfonamides (4)
Tetracycline, Doxycycline, Demeclocycline, Minocycline
Name some common Tetracyclines (4)
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Name the common Aminoglycosides (5)
Fluconazole, Ketoconazole, Clotrimazole, Miconazole, Itraconazole
Name the common Azoles
Ciprofloxacin, Norfloxacin, Ofloxacin, Grepafloxacin, Enoxacin, Nalidixic acid
Name the common Fluoroquinolones (6)
Nevirapine, Delavirdine
Name the common Non-Nucleoside Reverse Transcriptase Inhibitors
Zidovudine (AZT), Didanosine (ddI), Zalcitabine (ddC), Stavudine (d4T), Lamivudine (3TC)
Name the common Nucleoside Reverse Transcriptase Inhibitors
Saquinavir, Ritonavir, Indinavir, Nelfinavir
Name the Protease Inhibitors (4)
Protease Inhibitors and Reverse Transcriptase Inhibitors
Name two classes of drugs for HIV therapy
Staphlococcus aureus and Clostridium difficile (pseudomembranous colitis)
Name two organisms Vancomycin is commonly used for?
Penicillin-V
Oral Penicillin
Modification via Acetylation, Adenylation, or Phosphorylation
Resistance mechanisms for Aminoglycosides
Beta-lactamase cleavage of Beta-lactam ring
Resistance mechanisms for Cephalosporins/Penicillins
Modification via Acetylation
Resistance mechanisms for Chloramphenicol
Methylation of rRNA near Erythromycin's ribosome binding site
Resistance mechanisms for Macrolides
Altered bacterial Dihydropteroate Synthetase, Decreased uptake, or Increased PABA synthesis
Resistance mechanisms for Sulfonamides
Decreased uptake or Increased transport out of cell
Resistance mechanisms for Tetracycline
Terminal D-ala of cell wall replaced with D-lac; Decreased affinity
Resistance mechanisms for Vancomycin
Hemolysis (if G6PD deficient), Neurotoxicity, Hepatotoxicity, SLE-like syndrome
Side effects of Isoniazid (INH)?
Binds to the Pyrophosphate Binding Site of the enzyme
Specifically, how does Foscarnet inhibit viral DNA pol?
Inhibition of 50S peptidyl transferase, Bacteriostatic
The MOA for Chloramphenicol is?
Megaloblastic anemia, Leukopenia, Granulocytopenia
Toxic effects of TMP include?
Hormone synthesis inhibition (Gynecomastia), Liver dysfunction (Inhibits CYP450), Fever, Chills
Toxic side effects of the Azoles?
Delirium, Tremor, Nephrotoxicity
Toxicities associated with Acyclovir?
Rash, Pseudomembranous colitis
What additional side effects exist for Ampicillin?
Aminoglycosides
What antimicrobial class is Aztreonam syngergestic with?
Ataxia, Dizziness, Slurred speech
What are Amantadine-associated side effects?
Beta-lactam antibiotics
What are Aminoglycosides synergistic with?
Severe Gram - rod infections.
What are Aminoglycosides used for clinically?
Nephrotoxicity (esp. with Cephalosporins), Ototoxicity (esp. with Loop Diuretics)
What are common serious side effects of Aminoglycosides and what are these associated with?
Fever/Chills, Hypotension, Nephrotoxicity, Arrhythmias
What are common side effects of Amphotericin B?
GI intolerance (nausea, diarrhea), Hyperglycemia, Lipid abnormalities, Thrombocytopenia (Indinavir)
What are common side effects of Protease Inhibitors?
BM suppression (neutropenia, anemia), Peripheral neuropathy
What are common side effects of RT Inhibitors?
-Hypersensitivity reactions -Hemolysis -Nephrotoxicity (tubulointerstitial nephritis) -Kernicterus in infants Displace other drugs from albumin (e.g., warfarin)
What are common toxic side effects of Sulfonamides? (5)
GI discomfort, Acute cholestatic hepatitis, Eosinophilia, Skin rashes
What are common toxicities associated with Macrolides? (4)
GI distress, Tooth discoloration and Inhibition of bone growth in children, Fanconi's syndrome, Photosensitivity
What are common toxicities associated with Tetracyclines?
Well tolerated in general but occasionally, Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing='Red Man Syndrome'
What are common toxicities related to Vancomycin therapy?
1.Gram - rods of the Urinary and GI tracts (including Pseudomonas) 2.Neisseria 3. Some Gram + organisms
What are Fluoroquinolones indicated for? (3)
Hypersensitivity reactions
What are major side effects of Methicillin, Nafcillin, and Dicloxacillin?
Staphlococcus aureus
What are Methicillin, Nafcillin, and Dicloxacillin used for clinically?
Resistant Gram - infections
What are Polymyxins used for?
Rifampin, Ethambutol, Streptomycin, Pyrazinamide, Isoniazid (INH)
What are the Anti-TB drugs?
Systemic mycoses
What are the clinical indications for Azole therapy?
Gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae (PEcK)
What are the clinical uses for 1st 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 2nd Generation Cephalosporins?
1) Serious Gram - infections resistant to other Beta lactams 2) Meningitis (most penetrate the BBB)
What are the clinical uses for 3rd Generation Cephalosporins?
Gram - rods: Klebsiella species, Pseudomonas species, Serratia species
What are the clinical uses for Aztreonam?
Gram + cocci, Gram - rods, and Anerobes
What are the clinical uses for Imipenem/cilastatin?
-Upper respiratory tract infections -pneumonias -STDs: Gram+ cocci (streptococcal infect in pts allergic to penicillin) -Mycoplasma, Legionella,Chlamydia, Neisseria
What are the Macrolides used for clinically?
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 structural differences between Penicillin and Cephalosporin?
GI distress, Skin rash, and Seizures at high plasma levels
What are the major toxic side effects of Imipenem/cilastatin?
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 major toxic side effects of the Cephalosporins?
Neurotoxicity, Acute renal tubular necrosis
What are the side effects of Polymyxins?
Minor hepatotoxicity, Drug interactions (activates P450)
What are the side effects of Rifampin?
Disulfiram-like reaction with EtOH, Headache
What are toxic side effects for Metronidazole?
Aplastic anemia (dose independent), Gray Baby Syndrome
What are toxicities associated with Chloramphenicol?
Giardiasis, Amoebic dysentery (E. histolytica), Bacterial vaginitis (Gardnerella vaginalis), Trichomonas
What conditions are treated with Metronidazole?
Oxygen
What do Aminoglycosides require for uptake?
Mebendazole/Thiabendazole, Pyrantel Pamoate
What do you treat Nematode/roundworm (pinworm, whipworm) infections with?
Pentamidine
What drug is given for Pneumocystis carinii prophylaxis?
AZT, to reduce risk of Fetal Transmission
What drug is used during the pregnancy of an HIV+ mother?, Why?
Praziquantel
What drug is used to treat Trematode/fluke (e.g., Schistosomes, Paragonimus, Clonorchis) or Cysticercosis
Increases coumadin metabolism
What is a common drug interaction associated with Griseofulvin?
Blocks Influenza A and RubellA; causes problems with the cerebellA
What is a mnemonic to remember Amantadine's function?
It must be Phosphorylated by Viral Thymidine Kinase
What is a prerequisite for Acyclovir activation?
Hemolytic anemia
What is a Ribavirin toxicity?
RESPIre
What is an acronym to remember Anti-TB drugs?
Interstitial nephritis
What is an additional side effect of Methicillin?
GI upset
What is an occasional side effect of Aztreonam?
Anaerobic infections (e.g., B. fragilis, C. perfringens)
What is Clindamycin used for clinically?
Pseudomonas species and Gram - rods
What is clinical use for Carbenicillin, Piperacillin, and Ticarcillin?
Recurrent UTIs, Shigella, Salmonella, Pneumocystis carinii pneumonia
What is combination TMP-SMZ used to treat?
Clavulanic acid
What is combined with Ampicillin, Amoxicillin, Carbenicillin, Piperacillin, and Ticarcillin to enhance their spectrum?
Cryptococcal meningitis in AIDS patients and Candidal infections of all types
What is Fluconazole specifically used for?
Cilastatin
What is Imipenem always administered with?
Blastomyces, Coccidioides, Histoplasma, C. albicans; Hypercortisolism
What is Ketoconazole specifically used for?
Bismuth and Amoxicillin or Tetracycline; against Helobacter pylori
What is Metronidazole combined with for 'triple therapy'? Against what organism?
Antiprotozoal: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis Anaerobes: Bacteroides, Clostridium
What is Metronidazole used for clinically?
Cestode/tapeworm (e.g., D. latum, Taenia species Except Cysticercosis
What is Niclosamide used for?
Chagas' disease, American Trypanosomiasis (Trypanosoma cruzi)
What is Nifurtimox administered for?
DHPG (dihydroxy-2-propoxymethyl guanine)
What is the chemical name for Ganciclovir?
Extended spectrum penicillin: certain Gram + bacteria and Gram - rods
What is the clinical use for Ampicillin and Amoxicillin?
Topical and Oral, for Oral Candidiasis (Thrush)
What is the clinical use for Nystatin?
Bactericidal for: Gram + rod and cocci, Gram - cocci, and Spirochetes
What is the clinical use for Penicillin?
Hypersensitivity reactions
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?
Buy AT 30, CELL at 50'
What is the memory aid for subunit distribution of ribosomal inhibitors?
INH: Injures Neurons and Hepatocytes
What is the memory key for Isoniazid (INH) toxicity?
GET on the Metro
What is the memory key for Metronidazole's clinical uses?
VACUUM your Bed Room'
What is the memory key for organisms treated with Tetracyclines?
1. RNA pol inhibitor 2. Revs up P450 3. Red/orange body fluids 4. Rapid resistance if used alone
What is the memory key involving the '4 R's of Rifampin?'
Inhibit viral DNA polymerase
What is the MOA for Acyclovir?
Binds Ergosterol, forms Membrane Pores that Disrupt Homeostatis
What is the MOA for Amphotericin B?
Same as penicillin. Extended spectrum antibiotics
What is the MOA for Ampicillin and Amoxicillin?
Same as penicillin. Extended spectrum antibiotics
What is the MOA for Carbenicillin, Piperacillin, and Ticarcillin?
Blocks Peptide Bond formation at the 50S subunit, Bacteriostatic
What is the MOA for Clindamycin?
Same as penicillin. Act as narrow spectrum antibiotics
What is the MOA for Methicillin, Nafcillin, and Dicloxacillin?
Forms toxic metabolites in the bacterial cell, Bactericidal
What is the MOA for Metronidazole?
Binds ergosterol, Disrupts fungal membranes
What is the MOA for Nystatin?
Inhibits DNA dependent RNA polymerase
What is the MOA for Rifampin?
Inhibits formation of Initiation Complex, causes misreading of mRNA, Bactericidal
What is the MOA for the Aminoglycosides?
Inhibit Ergosterol synthesis
What is the MOA for the Azoles?
Beta lactams - inhibit cell wall synthesis, Bactericidal
What is the MOA for the Cephalosporins?
Inhibit DNA Gyrase (topoisomerase II), Bactericidal
What is the MOA for the Fluoroquinolones?
Blocks translocation, binds to the 23S rRNA of the 50S subunit, Bacteriostatic
What is the MOA for the Macrolides?
Binds 30S subunit and prevents attachment of aminoacyl-tRNA, Bacteriostatic
What is the MOA for the Tetracyclines?
Inhibits bacterial Dihydrofolate Reductase, Bacteriostatic
What is the MOA for Trimethoprim (TMP)?
Inhibits cell wall mucopeptide formation, Bactericidal
What is the MOA for Vancomycin?
Blocks viral penetration/uncoating; may act to buffer the pH of the endosome
What is the MOA of Amantadine?
Inhibits cell wall synthesis ( binds to PBP3). A monobactam
What is the MOA of Aztreonam?
Inhibits Viral DNA polymerase
What is the MOA of Foscarnet?
Inhibits CMV DNA polymerase
What is the MOA of Ganciclovir?
Interferes with microtubule function, disrupts mitosis, inhibits growth
What is the MOA of Griseofulvin?
Acts as a wide spectrum carbapenem
What is the MOA of Imipenem?
Decreases synthesis of Mycolic Acid
What is the MOA of Isoniazid (INH)?
Bind cell membrane, disrupt osmotic properties, Are Cationc, Basic and act as detergents
What is the MOA of Polymyxins?
Inhibits IMP Dehydrogenase (competitively), and therefore blocks Guanine Nucleotide synthesis
What is the MOA of Ribavirin?
Inhibit RT of HIV and prevent the incorporation of viral genome into the host DNA
What is the MOA of the RT Inhibitors?
GI discomfort
What is the most common cause of Pt noncompliance with Macrolides?
Malaria (P. falciparum)
What is treated with Chloroquine, Quinine, Mefloquine?
Anaerobes
What microorganisms are Aminoglycosides ineffective against?
Vibrio cholerae Acne Chlamydia Ureaplasma Urealyticum Mycoplasma pneumoniae Borrelia burgdorferi (Lyme's) Rickettsia Tularemia
What microorganisms are clinical indications for Tetracycline therapy?
Gram + and Anerobes
What microorganisms is Aztreonam not effective against?
Tendonitis and Tendon rupture
What musculo-skeletal side effects in Adults are associated with Floroquinolones?
Dopamine; causes its release from intact nerve terminals
What neurotransmitter does Amantadine affect? How does it influence this NT?
Enterobacter
What organism is Imipenem/cilastatin the Drug of Choice for?
Dermatophytes (tinea, ringworm)
What organisms does Griseofulvin target?
Giant Roundworm (Ascaris), Hookworm (Necator/Ancylostoma), Pinworm (Enterobius)
What parasites are treated with Pyrantel Pamoate (more specific)?
Onchocerciasis ('river blindness'--rIVER-mectin)
What parasitic condition is treated with Ivermectin?
Pregnant women, Children; because animal studies show Damage to Cartilage
What populations are Floroquinolones contraindicated in? Why?
Milk or Antacids, because divalent cations inhibit Tetracycline absorption in the gut
What should not be taken with Tetracyclines? / Why?
Triple sulfas or SMZ
What Sulfonamides are used for simple UTIs?
When pts have Low CD4+ (< 500 cells/cubic mm) or a High Viral Load
When is HIV therapy initiated?
1. Meningococcal carrier state 2. Chemoprophylaxis in contacts of children with H. influenzae type B
When is Rifampin not used in combination with other drugs?
Keratin containing tissues, e.g., nails
Where does Griseofulvin deposit?
Neomycin
Which Aminoglycoside is used for Bowel Surgery ?
1) Aminoglycosides = bactericidal 2) Tetracyclines = bacteriostatic
Which antimicrobial classes inhibit protein synthesis at the 30S subunit? (2)
1) Chloramphenical = bacteriostatic 2) Erythromycin = bacteriostatic 3) Lincomycin = bacteriostatic 4)cLindamycin = bacteriostatic
Which antimicrobials inhibit protein synthesis at the 50S subunit? (4)
G6PD deficient individuals
Which individuals are predisposed to Sulfonamide-induced hemolysis?
AZT
Which RT inhibitor causes Megaloblastic Anemia?
Non-Nucleosides
Which RT inhibitors cause a Rash?
Nucleosides
Which RT inhibitors cause Lactic Acidosis?
Doxycycline, because it is fecally eliminated
Which Tetracycline is used in patients with renal failure? / Why?
Due to the presence of a bulkier R group
Why are Methicillin, Nafcillin, and Dicloxacillin penicillinase resistant?
To inhibit renal Dihydropeptidase I and decrease Imipenem inactivation in the renal tubules
Why is Cilastatin administered with Imipenem?
-S-phase anti-metabolite Pyr analogue -Colon, solid tumors, & BCC/ -Irreversible myelosuppression
List the mechanism, clinical use, & toxicity of 5 FU.
-inhibits HGPRT (pur. Syn.) - Luk, Lymph,
List the mechanism, clinical use, & toxicity of 6 MP.
-DNA intercalator -testicular & lymphomas -Pulmonary fibrosis mild myelosuppression.
List the mechanism, clinical use, & toxicity of Bleomycin.
-Alkalates DNA -CML -Pulmonary fibrosis hyperpigmentation
List the mechanism, clinical use, & toxicity of Busulfan.
-Alkalating agent -testicular,bladder,ovary,& lung -Nephrotoxicity & CN VIII damage.
List the mechanism, clinical use, & toxicity of Cisplatin.
-Alkalating agent -NHL, Breast, ovary, & lung. - Myelosuppression, & hemorrhagic cystitis.
List the mechanism, clinical use, & toxicity of Cyclophosphamide.
-DNA intercalator -Hodgkin's, myeloma, sarcoma, and solid tumors -Cardiotoxicity & alopecia
List the mechanism, clinical use, & toxicity of Doxorubicin.
-Topo II inhibitor(GII specific) -Oat cell of Lung & prostate, & testicular -Myelosuppression & GI irritation.
List the mechanism, clinical use, & toxicity of Etoposide.
-S-phase anti-metabolite folate analogue -Luk, Lymp, sarc, RA, & psoriasis / -Reversible myelosuppression
List the mechanism, clinical use, & toxicity of Methotrexate.
-Alkalate DNA -Brain tumors -CNS toxicity
List the mechanism, clinical use, & toxicity of Nitrosureas.
-MT polymerization stabilizer -Ovarian & breast CA -Myelosupperession & hypersensitivity.
List the mechanism, clinical use, & toxicity of Paclitaxel.
-Triggers apoptosis -CLL, Hodgkin's in MOPP -Cushing-like syndrome
List the mechanism, clinical use, & toxicity of Prednisone.
-Estrogen receptor antagonist -Breast CA -increased endometrial CA risk
List the mechanism, clinical use, & toxicity of Tamoxifen.
-MT polymerization inhibitor(M phase) -MOPP, lymphoma, Willm's & choriocarcinoma -neurotoxicity and myelosuppression
List the mechanism, clinical use, & toxicity of Vincristine.
-Alkalating agents+cisplatin -Doxorubicin+Dactinomycin -Bleomycin -Etoposide
Which cancer drugs effect nuclear DNA (4)?
- Methotrexate - 5 FU - 6 mercaptopurine
Which cancer drugs inhibit nucleotide synthesis(3)?
-Steroids -Tamoxifen
Which cancer drugs work at the level of mRNA(2)?
-Vinca alkaloids(inhibit MT) -Paclitaxel
Which cancer drugs work at the level of proteins(2)?
hypertension, CHF, diabetic renal disease
ACE inhibitors- clinical use?
reduce levels of Angiotensin II, thereby preventing the inactivation of bradykinin (a potent vasodilator); renin level is increased
ACE inhibitors- mechanism?
fetal renal damage, hyperkalemia, Cough, Angioedema, Proteinuria, Taste changes, hypOtension, Pregnancy problems, Rash, Increased renin, Lower Angiotensin II (CAPTOPRIL)
ACE inhibitors- toxicity?
glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness
Acetazolamide- clinical uses?
acts at the proximal convoluted tubule to inhibit carbonic anhydrase. Causes self-limited sodium bicarb diuresis and reduction of total body bicarb stores.
Acetazolamide- mechanism?
proximal convoluted tubule
acetazolamide- site of action?
hyperchloremic metabolic acidosis, neuropathy, NH3 toxicity, sulfa allergy
Acetazolamide- toxicity?
ACIDazolamide' causes acidosis
Acetazolamide causes?
DOC in diagnosing and abolishing AV nodal arrhythmias
Adenosine- clinical use?
collecting ducts
ADH antagonists- site of action?
cyanide toxicity (releases CN)
adverse effect of Nitroprusside?
impotence, asthma, CV effects (bradycardia, CHF, AV block), CNS effects (sedation, sleep alterations)
adverse effects of beta-blockers?
fetal renal toxicity, hyperkalemia, Cough, Angioedema, Proteinuria, Taste changes, hypOtension, Pregnancy problems, Rash, Increased renin, Lower Angiotensin II (CAPTOPRIL)
adverse effects of Captopril?
dry mouth, sedation, severe rebound hypertension
adverse effects of Clonidine?
severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction
adverse effects of ganglionic blockers?
orthostatic and exercise hypotension, sexual dysfunction, diarrhea
adverse effects of Guanethidine?
nausea, headache, lupus-like syndrome, reflex tachycardia, angina, salt retention
adverse effects of Hydralazine?
hypokalemia, slight hyperlipidemia, hyperuricemia, lassitude, hypercalcemia, hyperglycemia
adverse effects of Hydrochlorothiazide?
K+ wasting, metabolic alkalosis, hypotension, ototoxicity
adverse effects of Loop Diuretics?
fetal renal toxicity, hyperkalemia
adverse effects of Losartan?
sedation, positive Coombs' test
adverse effects of Methyldopa?
hypertrichosis, pericardial effusion, reflex tachycardia, angina, salt retention
adverse effects of Minoxidil?
dizziness, flushing, constipation (verapamil), nausea
adverse effects of Nifedipine, verapamil?
first dose orthostatic hypotension, dizziness, headache
adverse effects of Prazosin?
sedation, depression, nasal stuffiness, diarrhea
adverse effects of Reserpine?
pulmonary fibrosis, corneal deposits, hepatotoxicity, skin deposits resulting in photodermatitis, neurologic effects, consitpation, CV (bradycardia, heart block, CHF), and hypo- or hyperthyroidism.
Amiodarone- toxicity?
sedation, sleep alterations
Beta Blockers- CNS toxicity?
bradycardia, AV block, CHF
Beta Blockers- CV toxicity?
Beta adrenergic receptors and Ca2+ channels (stimulatory)
Beta Blockers- site of action?
decrease
Beta Blockers- BP?
new arrhythmias, hypotension
Bretyllium- toxicity?
hypertension, angina, arrhythmias
Ca2+ channel blockers- clinical use?
block voltage dependent L-type Ca2+ channels of cardiac and smooth muscle- decreasing contractility
Ca2+ channel blockers- mechanism?
Cell membrane Ca2+ channels of cardiac sarcomere
Ca2+ channel blockers- site of action?
cardiac depression, peripheral edema, flushing, dizziness, constipation
Ca2+ channel blockers- toxicity?
troponin-tropomyosin system
Ca2+ sensitizers'- site of action?
check PFTs, LFTs, and TFTs
Cautions when using Amiodarone?
increased AP duration, increased ERP increased QT interval. Atrial and ventricular.
Antiarrhythmic class IA effects?
post MI and digitalis induced arrhythmias
Antiarrhythmic class IB- clinical uses?
decrease AP duration, affects ischemic or depolarized Purkinje and ventricular system
Antiarrhythmic class IB- effects?
local anesthetic. CNS stimulation or depression. CV depression.
Antiarrhythmic class IB- toxicity?
NO AP duration effect. useful in V-tach that progresses to V-fib and in intractable SVT LAST RESORT
Antiarrhythmic class IC- effects?
proarrhythmic
Antiarrhythmic class IC- toxicity?
decrease the slope of phase 4, increase PR interval (the AV node is particularly sensitive)
Antiarrhythmic class II- effects?
blocking the beta adrenergic receptor leads to decreased cAMP, and decreased Ca2+ flux
Antiarrhythmic class II- mechanism?
impotence, exacerbation of asthma, CV effects, CNS effects, may mask hypoclycemia
Antiarrhythmic class II- toxicity?
increase AP duration, increase ERP, increase QT interval, for use when other arrhythmics fail
Antiarrhythmic Class III- effects?
prevention of nodal arrhythmias (SVT)
Antiarrhythmic class IV- clinical use?
decrease conduction velocity, increase ERP, increase PR interval
Antiarrhythmic class IV- effects?
AV nodal cells
Antiarrhythmic class IV- primary site of action?
constipation, flushing, edema, CV effects (CHF, AV block, sinus node depression), and torsade de pointes (Bepridil)
Antiarrhythmic class IV- toxicity?
diuretics, sympathoplegics, vasodilators, ACE inhibitors, Angiotensin II receptor inhibitors
classes of antihypertensive drugs?
NO
decrease Digitoxin dose in renal failure?
YES
decrease Digoxin dose in renal failure?
Na/K ATPase
Digitalis- site of action?
Digitoxin>95% Digoxin 75%
Digoxin v. Digitoxin: bioavailability?
Digoxin=urinary Digitoxin=biliary
Digoxin v. Digitoxin: excretion?
Digitoxin 168hrs Digoxin 40 hrs
Digoxin v. Digitoxin: half life?
Digitoxin 70% Digoxin 20-40%
Digoxin v. Digitoxin: protein binding?
very short acting
Esmolol- short or long acting?
Diuresis in pateints with sulfa allergy
Ethacrynic Acid- clinical use?
not a sulfonamide, but action is the same as furosemide
Ethacrynic Acid- mechanism?
NO HYPERURICEMIA, NO SULFA ALLERGY; same as furosemide otherwise
Ethacrynic Acid- toxicity?
Sulfonamide Loop Diuretic. Inhibits ion co-transport system of thick ascending loop. Abolishes hypertonicity of the medulla, thereby preventing concentration of the urine.
Furosemide- class and mechanism?
edematous states (CHF, cirrhosis, nephrotic syndrome, pulm edema), HTN, hypercalcemia
Furosemide- clinical use?
Ototoxicity, Hypokalemia, Dehydration, Allergy (sulfa), Nephritis (interstitial), Gout
Furosemide- toxicity? (OH DANG)
Ca2+ (Loops Lose calcium)
Furosemide increases the excretion of what ion?
decrease myocardial O2 consumption by: 1-decreasing end diastolic volume 2- decreasing BP 3- decreasing HR 4-decreasing contractility 5-decreasing ejection time
how do we stop angina?
vasodilator- increases cGMP to induce smooth muscle relaxation (arterioles>veins; afterload reduction)
Hydralazine- class and mechanism?
severe hypertension, CHF
Hydralazine- clinical use?
compensatory tachycardia, fluid retention, lupus-like syndrome
Hydralazine- toxicity?
HTN, CHF, calcium stone formation, nephrogenic DI.
Hydrochlorothiazide- clinical use?
Inhibits NaCl reabsorption in the early distal tubule. Decreases Ca2+ excretion.
Hydrochlorothiazide- mechanism?
Hypokalemic metabolic alkalosis, hyponatremia, hyperGlycemia, hyperLipidemia, hyperUricemia, hyperCalcemia, sulfa allergy.
Hydrochlorothiazide- toxicity? (hyperGLUC, plus others)
torsade de pointes
Ibutilide- toxicity?
depresses ectopic pacemakers, especially in digoxin toxicity
K+- clinical use?
hyperaldosteronism, K+ depletion, CHF
K+ sparing diuretics- clinical use?
cortical collecting tubule
K+ sparing diuretics- site of action?
hyperkalemia, endocrine effects (gynecomastia, anti-androgen)
K+ sparing diuretics- toxicity?
thick ascending limb
loop diuretics (furosemide)- site of action?
ARF, shock, drug overdose, decrease intracranial/intraocular pressure
Mannitol- clinical use?
anuria, CHF
Mannitol- contraindications?
osmotic diuretic- increase tubular fluid osmolarity, thereby increasing urine flow
Mannitol- mechanism?
proximal convoluted tubule, thin descending limb, and collecting duct
mannitol- site of action?
pulmonary edema, dehydration
Mannitol- toxicity?
effective in torsade de pointes and digoxin toxicity
Mg+- clinical use?
propanolol, esmolol, metoprolol, atenolol, timolol
name five Antiarrhythmic drugs in class II?
Lovastatin, Pravastatin, Simvastatin, Atorvastatin
name four HMG-CoA reductase inhibitors.
Quinidine, Amiodarone, Procainamide, Disopyramide
name four Antiarrhythmic drugs in class IA.
Sotalol, Ibutilide, Bretylium, Amiodarone
name four Antiarrhythmic drugs in class III.
Captopril, Enalapril, Lisinopril
name three ACE inhibitors?
Nifedipine, Verapamil, Diltiazem
name three calcium channel blockers?
Lidocaine, Mexiletine, Tocainide
name three Antiarrhythmic drugs in class IB.
Flecainide, Encainide, Propafenone
name three Antiarrhythmic drugs in class IC.
Verapamil, Diltiazem, Bepridil
name three Antiarrhythmic drugs in class IV.
Spironolactone, Triamterene, Amiloride (the K+ STAys)
name three K+ sparing diuretics?
cholestyramine, colestipol
name two bile acid resins.
Gemfibrozil, Clofibrate
name two LPL stimulators.
Nitrates
Nifedipine has similar action to?
cardiac muscle: Verapamil>Diltiazem>Nifedipine
preferential action of the Ca2+ channel blockers at cardiac muscle?
vascular sm. Mus.: Nifedipine>Diltiazem>Verapamil
preferential action of the Ca2+ channel blockers at vascular smooth muscle?
reversible SLE-like syndrome
Procainamide- toxicity?
cinchonism: HA, tinnitus, thrombocytopenia, torsade de pointes due to increased QT interval
Quinidine- toxicity?
blocks SR Ca2+ channels
Ryanodine- site of action?
torsade de pointes, excessive Beta block
Sotalol- toxicity?
competitive inhibirot of aldosterone in the cortical collecting tubule
Spironolactone- mechanism?
distal convoluted tubule (early)
thiazides- site of action?
block Na+ channels in the cortical collecting tubule
Triamterene and amiloride- mechanism?
Beta Blockers
Verapamil has similar action to?
Hydralazine and Minoxidil
what two vasodilators require simultaneous treatment with beta blockers to prevent reflex tachycardia and diuretics to prevent salt retention?
carbonic anhydrase inhibitors, K+ sparing diuretics
which diuretics cause acidosis?
loop diuretics, thiazides
which diuretics cause alkalosis?
thiazides, amiloride
which diuretics decrease urine Ca2+?
loop diuretics, spironolactone
which diuretics increase urine Ca2+?
all except the K+ sparing diuretics Spironolactone, Triamterene, Amiloride
which diuretics increase urine K+?
all of them
which diuretics increase urine NaCl?
Acetaminophen has antipyretic and analgesic properties, but lacks anti-inflammatory properties.
Acetaminophen has what two clinical uses and lacks what one clinical use of the NSAIDs?
Yes, it does not cross the placenta.
Can Heparin be used during pregnancy?
No, warfarin, unlike heparin, can cross the placenta.
Can Warfarin be used during pregnancy?
Short.
Does Heparin have a long, medium, or short half life?
Long.
Does Warfarin have a long, medium, or short half life?
Large anionic polymer, acidic
For Heparin what is the Structure
Paranteral (IV, SC)
For Heparin what is the Route of administration
Rapid (seconds)
For Heparin what is the Onset of action
Activates antithrombin III
For Heparin what is the Mechanism of action
Acute (hours)
For Heparin what is the Duration of action
Yes
For Heparin what is the Ability to inhibit coagulation in vitro
Protamine sulfate
For Heparin what is the Treatment for overdose
aPTT (intrinsic pathway)
For Heparin what is the Lab value to monitor
Blood
For Heparin what is the Site of action
Small lipid-soluble molecule
For Warfarin what is the Structure
Oral
For Warfarin what is the Route of administration
Slow, limited by half lives of clotting factors
For Warfarin what is the Onset of action
Impairs the synthesis of vitamin K-dependent clotting factors
For Warfarin what is the Mechanism of action
Chronic (weeks or months)
For Warfarin what is the Duration of action
No
For Warfarin what is the Ability to inhibit coagulation in vitro
IV vitamin K and fresh frozen plasma
For Warfarin what is the Treatment for overdose
PT
For Warfarin what is the Lab value to monitor
Liver
For Warfarin what is the Site of action
Rare.
Is toxicity rare or common whith Cromolyn used in Asthma prevention?
1. Hydrocortisone 2. Predisone 3. Triamcinolone 4. Dexamethasone 5. Beclomethasone
List five common glucocorticoids.
Penicillin.
Secretion of what drug is inhibited by Probenacid used to treat chronic gout?
The COX-2 inhibitors should not have the corrosive effects of other NSAIDs on the gastrointestinal lining.
The COX-2 inhibitors (celecoxib, rofecoxib) have similar side effects to the NSAIDs with what one exception?
Sulfonylureas are oral hypoglycemic agents, they are used to stimulate release of endogenous insulin in NIDDM (type-2).
What are are the Sulfonylureas (general description) and what is their use?
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 advantages 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 disadvantages of Oral Contraceptives (synthetic progestins, estrogen)?
1. Gastric ulceration 2. Bleeding 3. Hyperventilation 4. Reye's syndrome 5. Tinnitus (CN VIII)
What are five possible toxic effects of Aspirin therapy?
1. Significant: nephrotoxicity 2. Peripheral neuropathy 3. Hypertension 4. Pleural effusion 5. Hyperglycemia.
What are five toxicities associated with Tacrolimus (FK506)?
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 advantages of newer low-molecular-weight heparins (Enoxaparin)?
1. Antipyretic 2. Analgesic 3. Anti-inflammatory 4. Antiplatelet drug.
What are four clinical activities of Aspirin?
1. Addison's disease 2. Inflammation 3. Immune suppression 4. Asthma
What are four clinical uses of glucocorticoids?
1. Peptic ulcer 2. Gastritis 3. Esophageal reflux 4. Zollinger-Ellison syndrome
What are four conditions in which H2 Blockers are used clinically?
1. Cimetadine 2. Ranitidine 3. Famotidine 4. Nizatidine
What are four H2 Blockers?
1. Tolbutamide 2. Chlorpropamide 3. Glyburide 4. Glipizide
What are four Sulfonylureas?
1. Streptokinase 2. Urokinase 3. tPA (alteplase), APSAC (anistreplase)
What are four thrombolytics?
1. Hot flashes 2. Ovarian enlargement 3. Multiple simultaneous pregnancies 4. Visual disturbances
What are four unwanted effects of Clomiphene use?
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 nine findings of Iatrogenic Cushing's syndrome caused by glucocorticoid therapy?
Headache, flushing , dyspepsia, blue-green color vision.
What are signs of Sildenafil (Viagra) toxicity?
Acute coronary syndrome; coronary stenting. Decreases the incidence or recurrence of thrombotic stroke.
What are the clinical uses for Ticlopidine, Clopidogrel?
1. Peptic ulcer 2. Gastritis 3. Esophageal reflux 4. Zollinger-Ellison syndrome
What are the four conditions in which Omeprazole, Lansoprazole is used?
1. Infertility (pulsatile) 2. Prostate cancer (continuous: use with flutamide) 3. Uterine fibroids
What are three clinical uses of the Leuprolide?
1. Antipyretic 2. Analgesic 3. Anti-inflammatory
What are three clinical uses of the NSAIDs?
Ibuprofen, Naproxen, and Indomethacin
What are three common NSAIDS other than Aspirin?
1. Bleeding 2. Teratogenicity 3. Drug-drug interactions
What are three complications of Warfarin usage?
1. Bleeding 2. Thrombocytopenia 3. Drug-drug interactions
What are three possible complications of Heparin therapy?
1. Renal damage 2. Aplastic anemia 3. GI distress
What are three possible toxicities of NSAID usage?
1. Antiandrogen 2. Nausea 3. Vomiting
What are three toxicities of Leuprolied?
1. Skin rash 2. Agranulocytosis (rare) 3. Aplastic anemia
What are three toxicities of Propylthiouracil?
1. Aluminum hydroxide: constipation and hypophosphatemia 2. Magnesium hydroxide: diarrhea 3. Calcium carbonate: Hypercalcemia, rebound acid increase - All may cause hypokalemia
What are three types of antacids and the problems that can result from their overuse?
1. Heavy bleeding 2. GI effects (n/v, anorexia) 3. Abdominal pain
What are three unwanted effects of Mifepristone?
1. Acarbose 2. Miglitol
What are two Alpha-glucosidase inhibitors?
1. Kidney transplantation 2. Autoimmune disorders (including glomerulonephritis and hemolytic anemia)
What are two clinical uses of Azathioprine?
Rheumatoid and osteoarthritis.
What are two conditions in which COX-2 inhibitors might be used?
1. Pioglitazone 2. Rosiglitazone.
What are two Glitazones?
Inhibits organification and coupling of thyroid hormone synthesis. Also decreases peripheral conversion of T4 to T3.
What are two mechanisms of action of Propythiouracil?
1. Phospholipase A2 is prevented from releasing arachidonic acid 2. Decreases protein synthesis thus lowering amount of Cyclooxygenase enzymes
What are two processes Corticosteroids inhibit leading to decreased inflammation?
1. Predisposes to viral infections and lymphoma 2. Nephrotoxic (preventable with mannitol diuresis)
What are two toxicities associated with Cyclosporine?
1. Weight gain 2. Hepatotoxicity (troglitazone)
What are two toxicities of the Glitazones?
1. Hypoglycemia (more common with 2nd-generation drugs: glyburide, glipizide) 2. Disulfiram-like effects (not seen with 2nd-generation drugs).
What are two toxicities of the Sulfonylureas?
Sucralfate cannot work in the presence of antacids or H2 blockers because it requires an acidic environment to polymerize.
What are two types of drugs that interfere with the action of Sucralfate and why?
Can affect absorption, bioavailability, or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying.
What can result due to antacid overuse?
Lipoxygenase
What enzyme does Zileuton inhibit?
Cyclooxygenases (COX I, COX II).
What enzymes are inhibited by NSAIDs, acetaminophen and COX II inhibitors?
GI side effects. (Note: Indomethacin is less toxic, more commonly used.)
What is a common side effect of Colchicine used to treat acute gout, especially when given orally?
Diarrhea
What is a common side effect of Misoprostol?
Overdose produces hepatic necrosis; acetaminophen metablolite depletes glutathione and forms toxic tissue adducts in liver.
What is a possible result of overdose of Acetaminophen?
GI disturbances.
What is a possible toxicity of Alpha-glucosidase inhibitors used in type-2 diabetes?
Neutropenia (ticlopidine); reserved for those who cannot tolerate aspirin.
What is a possible toxicity of Ticlopidine, Clopidogrel usage?
Bleeding.
What is a sign of toxicity with the use of thrombolytics?
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 action of insulin in the liver, in muscle, and in adipose tissue?
1. Suppresses organ rejection after transplantation 2. Selected autoimmune disorders.
What is are two clinical uses of Cyclosporine?
Antileukotriene; blocks leukotriene receptors.
What is the category and mechanism of action of Zafirlukast in Asthma treatment?
Antileukotriene; blocks synthesis by lipoxygenase.
What is the category and mechanism of action of Zileuton in Asthma treatment?
Inhalational general anesthetic.
What is the category of drug names ending in -ane (e.g. Halothane)
Benzodiazepine.
What is the category of drug names ending in -azepam (e.g. Diazepam)
Phenothiazine (neuroleptic, antiemetic).
What is the category of drug names ending in -azine (e.g. Chlorpromazine)
Antifungal.
What is the category of drug names ending in -azol (e.g. Ketoconazole)
Babiturate.
What is the category of drug names ending in -barbital (e.g. Phenobarbital)
Local anesthetic.
What is the category of drug names ending in -caine (e.g. Lidocaine)
Penicillin.
What is the category of drug names ending in -cillin (e.g. Methicillin)
Antibiotic, protein synthesis inhibitor.
What is the category of drug names ending in -cycline (e.g. Tetracycline)
Tricyclic antidepressant.
What is the category of drug names ending in -ipramine (e.g. Imipramine)
Protease inhibitor.
What is the category of drug names ending in -navir (e.g. Saquinavir)
Beta antagonist.
What is the category of drug names ending in -olol (e.g. Propranolol)
Butyrophenone (neuroleptic).
What is the category of drug names ending in -operidol (e.g. Haloperidol)
Cardiac glycoside (inotropic agent).
What is the category of drug names ending in -oxin (e.g. Digoxin)
Methylxanthine.
What is the category of drug names ending in -phylline (e.g. Theophylline)
ACE inhibitor.
What is the category of drug names ending in -pril (e.g. Captopril)
Beta-2 agonist.
What is the category of drug names ending in -terol (e.g. Albuterol)
H2 antagonist
What is the category of drug names ending in -tidine (e.g. Cimetidine)
Tricyclic antidepressant.
What is the category of drug names ending in -triptyline (e.g. Amitriptyline)
Pituitary hormone.
What is the category of drug names ending in -tropin (e.g. Somatotropin)
Alpha-1 antagonist
What is the category of drug names ending in -zosin (e.g. Prazosin)
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 adverse effect of Isoproterenol 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 period of use of albuterol in the treatment of Asthma?
Methylzanthine; desired effect is bronchodilation, may cause bronchodilation by inhibiting phosphodiesterase, enzyme involved in degrading cAMP (controversial).
What is the category, desired effect, and possible mechanism of Theophylline in treating Asthma?
Muscarinic antagonist; competatively blocks muscarinic receptors, preventing bronchoconstriction.
What is the category, mechanism of action, and effect of Ipratroprium 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, mechanism of action, and particular use of beclomethasone and prednisone in Asthma treatment?
Beta 2 agonist; used as a long-acting agent for prophylaxis. Adverse effects are tremor and arrhythmia.
What is the category, method of use, and adverse effects of Salmeterol in Asthma treatment?
Prevention of NSAID-induced peptic ulcers, maintains a PDA.
What is the clincial use for Misoprostol?
Treatment of infertility.
What is the clinical use for Clomiphene?
Immediate anticoagulation for PE, stroke, angina, MI, DVT.
What is the clinical use for Heparin?
Erectile dysfunction.
What is the clinical use for Sildenafil (Viagra)?
Peptic ulcer disease.
What is the clinical use for Sucralfate?
Chronic anticoagulation.
What is the clinical use for Warfarin?
Abortifacient.
What is the clinical use of Mifepristone (RU486)?
Potent immunosuppressive used in organ transplant recipients.
What is the clinical use of Tacrolimus (FK506)?
Increase target cell response to insulin.
What is the effect of the Glitazones in diabetes treatment?
Finasteride inhibits 5 Alpha-reductase, this decreases the conversion of testosterone to dihydrotestosterone, useful in BPH
What is the enzyme inhibited, the effect of this inhibition, and the clinical use of the antiandrogren Finasteride?
The PTT.
What is the lab value used to monitor the effectiveness of Heparin therapy?
The PT.
What is the lab value used to monitor the effectiveness of Warfarin therapy?
Early myocardial infarction.
What is the main clinical use for the thrombolytics?
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 Sucralfate?
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 of the COX-2 inhibitors (celecoxib, rofecoxib)?
Prevents release of mediators from mast cells. Effective only for the prophylaxis of asthma. Not effective during an acute attack.
What is the mecanism of action, effective period, and ineffective period of use for Cromolyn in treating Asthma?
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 antiandrogen Flutamide?
Inhibit steroid synthesis, used in the treatment of polycystic ovarian syndrome to prevent hirsutism.
What is the mechanism of action and clinical use of the antiandrogens Ketoconazole and Spironolactone?
Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally.
What is the mechanism of action of Acetaminophen?
Inhibits xanthine oxidase, decresing conversion of xanthine to uric acid.
What is the mechanism of action of Allopurinol used to treat chronic gout?
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 Aspirin?
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 Clomiphene?
Depolymerizes microtubules, impairing leukocyte chemotaxis and degranulation.
What is the mechanism of action of Colchicine used to treat acute gout?
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 Cyclosporine?
Heparin catalyzes the activation of antithrombin III.
What is the mechanism of action of Heparin?
Competitive inibitor of progestins at progesterone receptors.
What is the mechanism of action of Mifepristone (RU486)?
Misoprostol is a PGE1 analog that increases the production and secretion of the gastic mucous barrier.
What is the mechanism of action of Misoprostol?
Reversibly inhibit cyclooxygenase (COX I and COX II). Block prostaglandin synthesis.
What is the mechanism of action of NSAIDs other than Aspirin?
Irreversibly inhibits H+/K+ ATPase in stomach parietal cells.
What is the mechanism of action of Omeprazole, Lansoprazole?
Inhibits reabsorption of uric acid.
What is the mechanism of action of Probenacid used to treat chronic gout?
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 Sildenafil (Viagra)?
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 Alpha-glucosidase inhibitors?
Decrease the production of leukotrienes and protaglandins by inhibiting phospholipase A2 and expression of COX-2.
What is the mechanism of action of the glucocorticoids?
Reversible block of histamine H2 receptors
What is the mechanism of action of the H2 Blockers?
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 Sulfonylureas?
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 the thrombolytics?
Inhibits platelet aggregation by irreversibly inhibiting the ADP pathway involved in the binding of fibrinogen.
What is the mechanism of action of Ticlopidine, Clopidogrel
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 action of Warfarin (Coumadin)?
Antimetabolite derivative of 6-mercaptopurine that interferes with the metablolism and synthesis of nucleic acid.
What is the mechanism of Azathioprine?
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 Leuprolide?
Similar to cyclosporine; binds to FK-binding protein, inhibiting secretion of IL-2 and other cytokines.
What is the mechanism of Tacrolimus (FK506)?
Sildenafil fills the penis
What is the memory key for the action of Sildenafil (Viagra)?
AluMINIMUM amount of feces.
What is the memory key for the effect of aluminum hydroxide overuse?
Mg = Must go to the bathroom.
What is the memory key for the effect of magnesium hydroxide overuse?
WEPT: Warfarin affects the Extrinsic pathway and prolongs the PT.
What is the memory key to remember which pathway (extrinsic vs. intrinsic) and which lab value Warfarin affects?
Mechanism unknown; possibly inhibits gluconeogenesis and increases glycolysis; effect is to decrease serum glucose levels
What is the possible mechanism and effect of Metformin in treating diabetes?
Indomethacin is used to close a patent ductus arteriosus.
What is the specific clinical use of Indomethacin in neonates?
Protamine Sulfate is used for rapid reversal of heparinization (positively charged molecule that binds to negatively charged heparin).
What is used to reverse the action of Heparin?
Those patients who are taking nitrates.
What patients are at risk for life threatening hypotension when taking Sildenafil (Viagra)?
Leukotrienes increasing bronchial tone.
What process does Zafirlukast interfere with?
Chronic gout.
What type of gout is treated with Allopurinol?
Acute gout.
What type of gout is treated with Colchicine?
Chronic gout.
What type of gout is treated with Probenacid?
Misoprostol is contraindicated in women of childbearing potential because it is an abortifacient.
What type of patient should not take Misoprostol and why?
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.
Which H2 Blocker has the most toxic effects and what are they?
Because they require some residual islet function.
Why are the Sulfonylureas inactive in IDDM (type-1)?
-Disulfram & also sulfonylureas, metronidazole
Acetaldehyde is metabolized by Acetaldehyde dehydrogenase, which drug inhibs this enzyme?
-Weak Acids>Alkinalize urine(CO3) to remove more -Weak bases>acidify urine to remove more
Explain pH dependent urinary drug elimination?
-Airway -Breathing -Circulation -Dextrose (thiamine & narcan) -ABCD
How do you treat coma in the ER (4)?
-Infections -Trauma -Seizures -CO -Overdose -Metabolic -Alcohol (IT'S COMA)
In coma situations you rule out what (7)?
-A57Blue lines in gingiva & long bones -Encephalopathy & Foot drop -Abdominal colic / -Sideroblastic anemia
List some specifics of lead poisoning(4)?
-N-acetylcystine
List the specific antidote for this toxin: Acetaminophen
-Ammonium Chloride
List the specific antidote for this toxin: Amphetamine
-Atropine & pralidoxime
List the specific antidote for this toxin: Anticholinesterases (organophosphate.)
-Physostigmine salicylate
List the specific antidote for this toxin: Antimuscarinic (anticholinergic)
-Dimercaprol, succimer
List the specific antidote for this toxin: Arsenic (all heavy metals)
-Flumazenil
List the specific antidote for this toxin: Benzodiazepines
-Glucagon
List the specific antidote for this toxin: Beta Blockers
-100% oxygen, hyperbaric
List the specific antidote for this toxin: Carbon monoxide
-Penicillamine
List the specific antidote for this toxin: Copper
-Nitrate, hydroxocobalamin thiosulfate
List the specific antidote for this toxin: Cyanide
-Normalize K+, Lidocaine, & Anti-dig Mab
List the specific antidote for this toxin: Digitalis
-Protamine
List the specific antidote for this toxin: Heparin
-Deferoxamine
List the specific antidote for this toxin: Iron
-EDTA, dimercaprol, succimer, & penicillamine
List the specific antidote for this toxin: Lead
-Ethanol, dialysis, & fomepizole
List the specific antidote for this toxin: Methanol & Ethylene glycol
-Methylene blue
List the specific antidote for this toxin: Methemoglobin
-B51Naloxone / naltrexone (Narcan)
List the specific antidote for this toxin: Opioids
-Alkalinize urine & dialysis
List the specific antidote for this toxin: Salicylates
-Aminocaproic acid
List the specific antidote for this toxin: TPA & Streptokinase
-NaHCO3
List the specific antidote for this toxin: Tricyclic antidepressants
-Vitamin K & fresh frozen plasma
List the specific antidote for this toxin: Warfarin
-Acetaldehyde -Nausea, vomiting, headache, & hypotension
What are the products and their toxicities of the metabolism of ethanol by / alcohol dehydrogenase?
-Oxalic acid -Acidosis & nephrotoxicity
What are the products and their toxicities of the metabolism of Ethylene Glycol by / alcohol dehydrogenase?
-Formaldehyde & formic acid -severe acidosis & retinal damage
What are the products and their toxicities of the metabolism of Methanol by / alcohol dehydrogenase?
-Glucocorticoid withdrawal
Which drug(s) cause this reaction: Adrenocortical Insufficiency
-Cloazapine -carbamazapine -colchicine -PTU
Which drug(s) cause this reaction: Agranulocytosis (3)?
-Penicillin
Which drug(s) cause this reaction: Anaphylaxis?
-Chloramphenicol -benzene -NSAIDS -PTU -phenytoin
Which drug(s) cause this reaction: Aplastic anemia (5)?
-Tricyclic antidepressants
Which drug(s) cause this reaction: Atropine-like side effects?
-Daunorubicin & Doxorubicin
Which drug(s) cause this reaction: Cardiac toxicity?
-Quinidine -quinine
Which drug(s) cause this reaction: Cinchonism (2)?
-ACE inhibitors (Losartan>no cough)
Which drug(s) cause this reaction: Cough?
-Niacin -Ca++ channel blockers -adenosine -vancomycin
Which drug(s) cause this reaction: Cutaneous flushing (4)?
-Lithium
Which drug(s) cause this reaction: Diabetes insipidus?
-Metronidazole -certain cephalosporins -procarbazine -sulfonylureas
Which drug(s) cause this reaction: Disulfram-like reaction (4) ?
-Haloperidol -chlorpromazine -reserpine -MPTP
Which drug(s) cause this reaction: Drug induced Parkinson's (4) ?
-Chlorpromazine -thioridazine -haloperidol
Which drug(s) cause this reaction: Extrapyramidal side effects (3)?
-Tetracycline
Which drug(s) cause this reaction: Fanconi's syndrome?
-Halothane -Valproic acid -acetaminophen -Amantia phalloides
Which drug(s) cause this reaction: Focal to massive hepatic necrosis (4)?
-Sulfonamides -INH -ASA -Ibuprofen -primaquine -nitrofurantoin /-pyrimethamine -chloramphenicol
Which drug(s) cause this reaction: G6PD hemolysis(8)?
-Phenytoin
Which drug(s) cause this reaction: Gingival hyperplasia?
-Chloramphenicol
Which drug(s) cause this reaction: Gray baby syndrome?
-Cimetidine -ketoconazole -spironolactone -digitalis -EtOH -estrogens
Which drug(s) cause this reaction: Gynecomastia (6)?
-Isoniazid
Which drug(s) cause this reaction: Hepatitis?
-Tamoxifen
Which drug(s) cause this reaction: Hot flashes?
-polymyxins
Which drug(s) cause this reaction: Neuro and Nephrotoxic?
-Corticosteroids -heparin
Which drug(s) cause this reaction: Osteoporosis (2)?
-aminoglycosides -loop diuretics -cisplatin
Which drug(s) cause this reaction: Oto and Nephrotoxicity (3)?
-Barbiturates -phenytoin -carbamazipine -rifampin -griseofulvin -quinidine
Which drug(s) cause this reaction: P450 induction(6)?
-Cimetidine -ketoconazole -grapefruit juice -erythromycin -INH -sulfonamides
Which drug(s) cause this reaction: P450 inhibition(6)?
-Tetracycline -amiodarone -sulfonamides
Which drug(s) cause this reaction: Photosensitivity(3)?
-Clindamycin
Which drug(s) cause this reaction: Pseudomembranous colitis?
-Bleomycin -amiodarone -busulfan
Which drug(s) cause this reaction: Pulmonary fibrosis(3)?
-Hydralazine -Procainamide -INH -phenytoin
Which drug(s) cause this reaction: SLE-like syndrome?
-Ethosuxamide -sulfonamides -lamotrigine
Which drug(s) cause this reaction: Stevens-Johnson syn. (3)?
-Antipsychotics
Which drug(s) cause this reaction: Tardive dyskinesia?
-Fluoroquinolones
Which drug(s) cause this reaction: Tendonitis and rupture?
-Oral Contraceptives
Which drug(s) cause this reaction: Thrombotic complications?
-Class III antiarrhythmics (sotalol) -class IA (quinidine)
Which drug(s) cause this reaction: Torsade de pointes (2)?
-Sulfonamides -furosemide -methicillin -rifampin -NSAIDS (ex. ASA)
Which drug(s) cause this reaction: Tubulointerstitial Nephritis (5)?
Constant FRACTION eliminated per unit time.(exponential)
Describe first-order kinetics?
-reduction, oxy, & hydrolysis -H2O sol. Polar product -P450
Describe Phase I metabolism in liver(3)?
-acetylation, glucuron., & sulfation -Conjugation -Polar product
Describe Phase II metabolism in liver(3)?
- Act on same receptor - Full has greater efficacy
Explain differences between full and partial agonists(2).
- partial agonist can have increased, decreased, /A21or equal potency as full agonist. - Potency is an independent factor.
Explain potency in relation to full and partial agonists(2).
- ED 50 is less than the Km (less than 50% of receptors)
How do spare receptors effect the Km?
Md= (CpxCL)/F Cp= plas. Conc. CL=clear. F=bioaval.
How do you calculate maintenance dose?
-Shifts the curve to the right -increases Km
How does a competitive antagonist effect an agonist?
- Shifts the curve down -reduces Vmax
How does a noncompetitive antagonist effect an agonist?
-Phase I (clinical tests) -Phase II -Phase III -PhaseIV (surveillance)
Name the steps in drug approval(4)?
In 4 half-lifes= (94%) T1/2 = (0.7x Vd)/CL
Steady state concentration is reached in __ number of half-lifes
-Constant AMOUNT eliminated per unit time. -Etoh & ASA
What is the definition of zero-order kinetics? Example?
CL= (rate of elimination of drug/ Plasma drug conc.)
What is the formula for Clearance (CL)
Vd= (Amt. of drug in body/ Plasma drug conc.)
What is the formula for Volume of distribution (Vd)
Ld= (CpxVd)/F Cp=plasma conc. F= Bioaval.
What is the loading dose formula?
Epinephirine(Alpha1,2 and Beta 1,2)
A 12yo patient was treated for a reaction to a bee sting, what drug provides the best coverage of sympathomimetic receptors?
Dopamine
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
scopolamine
A fellow passenger on a Carnival cruise ship looks pale and diaphoretic, what antimuscarinic agent would you give them?
Atropine pts are suffering from Cholinestrase inhibitor poisining (Nerve gas/Organophosphate poisining)
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
Succinylcholine
As an Anes you want to use a depolarizing neuromuscular blocking drug on your pt, what do you use
Prevents the release of Ca from SR of skeletal muscle
MOA of Succinylcholine
Centrally acting alpha agonist, thus causing a decrease in central adrenergic outflow, spairing renal blood flow
Clonidine is the preferred sym pathomimetic tx of HTN in pts with renal disease, why??
Indirect agonist, uptake inhibitor
Cocaine casues vasoconstriction and local anesthesia by what mechanism
TCA
Cocaine shares is mechanism of action with what antidepressant
Beta1 more than B2
Dobutamine used for the tx of shock acts on which receptors
No, it inhibits the release of Nor Epi
Guanethidine enhances the release of Norepi?
It acts presynaptically to increase NE release.
How does angiotensin II affect NE release?
Prevents the release of ACh, which results in muscle paralysis.
How does botulinum toxin result in respiratory arrest?
Prevents the release of calcium from the sarcoplasmic reticulum of skeletal muscle.
How does dantrolene work?
NE acts presynaptically on alpha-2 receptors to inhibit its own release. ACh also acts presynaptically through M1 receptors to inhibit NE release.
How does NE modulate its own release? What other neurotransmitter has this same effect?
Hemicholinium inhibits the transport of choline into the nerve, thus inhibiting formation of ACh.
How would hemicholinium treatment affect cholinergic neurons?
Give an antichloinesterase - neostigmine, edrophonium, etc
How would you reverse the effect of a neuromuscular blocking agent?
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.
If a patient is given hexamethonium, what would happen to his/her heart rate?
Stimulates beta adrenergic receptors
Isopoterenol was given to a patient with a developing AV block, why?
Binding to the presynaptic alpha 2 release modulating receptors
Norepi feedbacks and inhibits the presynaptic receptor by what mechanism
Blocks Norepi, but not Dopamine
Reserpine will block the syntheis of this drug and but not its precursor.
Amphetamine and Ephedrine
These drugs acts indirectly by releasing strored catecholamines in the presynaptic terminal
physostigmine
What anticholinesterase crosses the blood-brain-barrier?
Ipratropium
What antimuscarinic agent is used in asthma and COPD?
Ipratropium
What antimuscarinic drug is useful for the tx of asthma
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, and Salivation = DUMBBELS; also abdominal cramping
What are the classic symptoms of cholinesterase inhibitor poisoning (parathion or other organophosphates)?
Activates cholinergic receptors on bladder and bowel smooth muscle, alleviating post-op and neurogenic ileus and urinary retention.
What are the clinical indications for bethanechol?
Post-op and neurogenic ileus and urinary retention, myasthenia gravis, and reversal of neuromuscular junction blockade (post-op) through anticholinesterase activity.
What are the clinical indications for neostigmine?
narcolepsy, obesity, and attention deficit disorder (I wouldn't recommend this)
What are the indications for using amphetamine?
Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rapacuronium
What are the nondepolarizing neuromuscular blocking drugs?
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 the phases of succinylcholine neuromuscular blockade?
amphetamine and ephedrine
What are two indirect acting adrenergic agonists?
Albuterol, tertbutaline
What beta 2 agonist will help your 21yo Astma pt?
Botulinum
What cholinergic inhibitor acts by directly inhibiting Ach release at the presynaptic terminal
Edrophonium
What cholinomimetic is useful in the diagnosis of Myasthenia Gravis
Carbachol, pilocarpine, physostigmine, echothiophate
What cholinomimetics might your pt be taking for his glaucoma
anticholinesterase glaucoma
What class of drug is echothiophate? What is its indication?
In treatment of malignant hyperthermia, due to concomitant use of halothane and succinylcholine. Also in neuroleptic malignant syndrome, a toxicity of antipsychotic drugs.
What conditions would you use dantrolene?
edrophonium (extremely short acting anticholinesterase)
What drug is used to diagnose myasthenia gravis?
Neostigmine, pyridostigmine edrophonium, physostigmine echothiophate
What drugs target anticholinesterase
Theoretically it could be used to block the cephalic phase of acid secretion (vagal stimulation).
What effect would atropine have on a patient with peptic ulcer disease?
None. No, because atropine would block the postganglionic muscarinic receptors involved in sweat gland stimulation.
What effect would atropine have on the preganglionic sympathetic activation of sweat glands? Would this person sweat?
Acetylcholinesterase; ACh is broken down into choline and acetate.
What enzyme is responsible for the breakdown of ACh in the synaptic cleft?
Acetylcholine esterase
What enzyme is responsible for the degredation of Ach
Choline acetyltransferase
What enzyme is responsible for the production of Ach from Acetyl CoA and Choline
Treatment of hypertension, especially with renal disease (lowers bp centrally, so flow is maintained to kidney).
What is the clinical utility of clonidine?
The only local anesthetic with vasoconstrictive properties.
What is the clinical utility of cocaine?
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 between the affinity for beta receptors between albuterol/terbutaline and dantroline?
Prefers beta's at low doses, but at higher doses alpha agonist effects are predominantly seen.
What is the difference in receptor affinity of epinephrine at low doses? High doses?
Increased systolic and pulse pressure, decreased diastolic pressure, and little change in mean pressure.
What is the effect of epinephrine infusion on bp and pulse pressure?
It inhibits release of NE.
What is the effect of guanethidine on adrenergic NE release?
Increases mean, systolic, and diastolic bp, while there is little change in pulse pressure.
What is the effect of norepinephrine on bp and pulse pressure?
They inhibit reuptake of NE at the nerve terminal (as does cocaine).
What is the effect of TCA's on the adrenergic nerve?
Succinylcholine
What is the only depolarizing neuromuscular blocking agent?
It affects beta receptors equally and is used in AV heart block (rare).
What is the receptor affinity and clinical use of isoproterenol?
SLUD (salivation, Lacrimation, urination, Defecation)as well as airway secretion, GI motility, acid secretions
What physiological effects was the Anes using Atropine to tx
Bethanechol, Neostigmine, physostigmine
What reversal agent could a Anes give to reverse the effects of Atropine
Atropine would also block the receptors in the ciliary muscle, causing an impairment in accommodation (cycloplegia).
What side effect of using atropine to induce pupillary dilation would you expect?
Norepinephrine (Alpha1,2 and beta 1)
What sympathomimetic would you not prescribe for hypotension in a pt with renal artery sclerosis.
Hexamethonium is a nicotinic antagonist, and thus is a ganglionic blocker.
What type of neurological blockade would hexamethonium create?
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 effect on blood pressure with infusion of the alpha -2 agonist clonidine?
atropine, homatropine, tropicamide
Which antimuscarinic agents are used in producing mydriasis and cycloplegia?
Epinephrine
Which drug increases Sys BP w/o affecting Pulse Pressure
Norepinephrine
Which of epi, norepi, or isoproterenol results in bradycardia?
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 the following would atropine administration cause? Hypothermia, bradycardia, excess salivation, dry flushed skin, or diarrhea
Norepinephrine
Which of these three drugs will cause a reflex bradycardia in your pt (Norepi, Epi, or Isoporterenol)
alpha-1 > alpha-2; used as a pupil dilator, vasoconstrictor, and for nasal decongestion
Which receptors does phenylephrine act upon?
Epinephrine to treat anaphylaxis. Also useful if you have open angle glaucoma, asthma, or hypotension.
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?
These B-2 agonists cause respiratory smooth muscle to relax.
Why are albuterol and terbutaline effective in tx of acute asthmatic attacks?
Blocking muscarinic receptors in the circular fibers of the eye, results in unopposed action of radial muscles to dilate.
Why does atropine dilate the pupil?
NE increases bp, which stimulates baroreceptors in the carotid sinus and the aorta. The CNS signals through vagal stimulation to decrease heart rate.
Why does NE result in bradycardia?
They activate the ciliary muscle of the eye (open angle) and pupillary sphincter (narrow angle).
Why is carbachol and pilocarpine useful in treatment of glaucoma?
As an anticholinesterase it increases endogenous ACh and thus increases strength.
Why is pyridostigmine effective in the treatment of myasthenia gravis?
Reserpine inhibits dopamine transport into vesicles, attenuating its conversion to NE by dopamine beta-hydroxylase.
Why is reserpine effective in treating HTN?
Stimulating beta receptors stimulates heart rate, but beta receptor induced vasodilation reduces peripheral resistance.
Why is there a drop in systolic, mean, and diastolic bp with infusion of isoproterenol?
Parkinson patients benefit from antimuscarinic agents through its inhibitory action within the indirect pathway.
Why would a patient with cog-wheel rigidity and a shuffling gait be given benztropine?
Receptors = D1=D2>beta>alpha, thus increasing heart rate (beta) and blood pressure (alpha vasoconstriction) while maintaining kidney perfusion (dopamine receptors)
Why would dopamine be useful in treating shock?
Useful in muscle paralysis during surgery or mechanical ventilation.
Why would you give a drug like pancuronium or succinylcholine?
Pralidoxime regenerates active cholinesterase.
Why would you use pralidoxime after exposure to an organophosphate?
No, hemicholinum block the uptake of Choline and thus Ach synthesis
Will Hemicholinum affect the release of stored Ach during Cholinergic Stimulation
No. Atropine is used to reduce urgency in mild cystitis. So it would aggravate the urinary retention.
Would blockade of muscarininc receptors in the bladder be useful in treating urinary retention?
Scopolamine
Your patient wants an effective drug to treat his motion sickness, what would you prescribe