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220 Cards in this Set
- Front
- Back
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28 year old chemist presents with MPTP exposure
What NT is depleted? |
Dopamine
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Woman taking tetracycline exhibits photosensitivity
What are the clinical manifestations? |
Rash on sun-exposed regions of body
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Nondiabetic patient presents with hypoglycemia but low levels of C peptide
What is the diagnosis |
Surreptitious insulin injection
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African American male who goes to Africa develops hemolytic anemia after taking malaria prophylaxis
What is the enzyme defficiency |
Glucose 6 phosphate dehydrogenase
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27 year old female with history of psychiatric illness now has urinary retention due to neuroleptic
What do you treat it with? |
Bethanechol
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Farmer presents with dyspnea, salivation, miosis, diarrhea, cramping and blurry vision
What caused this and what is the mechanism |
Insecticide poisoning, inhibition of acetylcholinesterase
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Patient with recent kidney transplant is on cyclosporine for immunosuppresion, he requires antifungal agent for candidiasis
What antifungal drug would result in cyclosporine toxicity? |
Ketoconazole
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Man on several medications including antidepressants and antihypertensives, has mydriasis and becomes constipated
What is the cause of symptoms? |
TCA
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55 year old postmenopausal woman on tamoxifen therapy
What is she at increased risk of acquiring? |
Endometrial carcinoma
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Woman on MAO inhibitor has hypertensive crisis after meal
What did she ingest? |
Tyramine (wine or cheese)
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After taking clindamycin, patient develops toxic megacolon and diarrhea
What is the mechanism of diarrhea? |
Clostridium difficile overgrowth
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Man starts a medication for hyperlipidemia. He then develops rash, pruritus and GI upset
What drug was it? |
Niacin
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Patient is on carbamazepine
What routine workup should be done? |
LFT's
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23 year old female who is on rifampin for TB prophylaxis and on birth control (estrogen) gets pregnant
Why? |
Rifampin augments estrogen metabolism in liver rendering it less effective
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Patient develops cough and must discontinue captopril
WHat is a good replacement drug and why doesnt it have the same side effects? |
Losartan - an angiotensin II receptor antagonist, does not increase bradykinin as captopril does
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Relates the amount of drug in the body to plasma concentration
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Vd - volume of distribution
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Formule for volume of distribution
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Vd = amount of drug in the body/plasma drug concentration
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Vd of plasma protein-bound drugs can be altered by what disease?
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Liver and kidney
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Relates the rate of elimination to plasma concentration
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CLEARANCE
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Formula for clearance
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Cl = rate of elimination of drug/plasma drug concentration
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The time required to change the amount of drug in the body by 1/2 during elimination (or during constant infusion) is called _
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Half life T1/2
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After 1 half life concentration of drug equals _ %
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50%
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After 2 half lifes concentration of drug equals_
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75%
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A drug infused at constant rate reaches about _ % of steady state after 4 T1/2
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94
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Formula for T1/2
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T1/2 = 0.7 * Vd/CL
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Loading dose formula
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Loading dose = Cp * Vd/F
Cp= target plasma concentration F = bioavailibility |
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Formula for maintenance dose
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Cp * CL / F
Cp = target plasma concentration F = bioavailibility |
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In patients with impaired renal or hepatic function, the loading dose decreases, increases or remains unchanged?
Maintenance dose? |
Loading dose remains unchanged
Maintenance dose decreases |
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Rate of elimination is constant (constant amount of drug is eliminated per unit time) - what order elimination?
What happens to target plasma concentration? |
Zero order elimination
Target plasma concentration decreases linearly with time |
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Rate of elimination is proportional to drug concentration (constant fraction of drug eliminated per unit time) - what order elimination?
What happens to target plasma concentration? |
First order elimination
Cp decreases exponentially with time |
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Give examples of drugs with zero order elimination
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Ethanol
Phenytoin Aspirin (at high or toxic concentration) |
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Phase I metabolism (reduction, oxidation, hydrolysis) yields _ metabolites (often still active)
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Slightly polar, water soluble
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What phase of metabolism associated with cytochrome P450
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Phase I
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What phase of metabolism associated with conjugation
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Phase iI
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Phase II metabolism (acetylation, glucoronidation, sulfation) yields _ metanolites (renally excreted)
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Very polar, inactive
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Geriatric patients lose which phase of metabolism first?
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Phase I
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Is it safe? Pharmacokinetics? - which phase of clinical testing of the drug
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Phase I
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Does it work in patients?- which phase of clinical testing of the drug
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Phase II
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Does it work? Double blind - which phase of clinical testing of the drug
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Phase III
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What happens in phase IV of clinical testing of the drug
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Postmarketing surveillance
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A competitive antagonist shifts agonist curve where?
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To the right
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A noncompetitive antagonist (irreversible) shifts agonist curve where?
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Downward
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Name antibiotics that block cell wall synthesis by inhibition of peptidoglycan cross linking
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Penicillin
Ampicillin Ticarcillin Pipercarcillin Imipenem Aztreonam Cephalosporins |
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Name antibiotics that block peptidoglycan synthesis
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Bacitracin
Vancomycin Cycloserine |
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Name antibiotics that block protein synthesis at 50S ribosomal unit
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Chloramphenicol
Erythromycin/macrolides Lincomycin Clindamycin Streptogramins (quinupristin, dalfopristin) Linezolid |
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Name antibiotics that block protein synthesis at 30S ribosomal unit
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Aminoglycosides
Tetracyclines |
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Name antibiotics that block nucleotide synthesis
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Sulfonamides
Trimethoprim |
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Name antibiotics that block DNA topoisomerase
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Quinolones
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Name antibiotic that blocks mRNA synthesis
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Rifampin
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Name bactericidal antibiotics
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Penicillin
Cephalosporins Vancomycin Aminoglycosides Fluoroquinolones Metronidazole |
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Name drugs that disrupt bacterial/fungal cell membrane
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Polymyxins
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Name drugs that disrupt fungal cell membranes
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Amphotericin B
Nystatin Flucoconazole/azoles |
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Oral form of penicillin is called _
IV form? |
Penicillin V
Penicillin G |
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Mechanism of penicillin
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- Binds penicillin binding proteins
- Blocks transpeptidase cross linking of cell walls - Activates autolytic enzymes |
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This antibiotic is bactericidal for gram positive cocci, gram positive rods, gram negative cocci and spirochetes. Not penicillinase resistant
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PENICILLIN
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Toxicity of penicillin
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Hypersensitivity reactions
Hemolytic anemia |
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Methicillin, nafcillin, dicloxacillin - mechanism of action?
Narrow or broad action? Penicillinase resistant or not? |
Same as penicillin
Narrow action Penicillinase resistant because of bulkier R groups |
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Methcillin, nafcillin and dicloxacillin are clinically used for treatment of what bug?
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S. aureus
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Methicillin toxicity
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Interstitial nephritis
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Methcillin, nafcillin, dicloxacillin toxicity
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Hypersensitivity reactions
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Ampicillin, Amoxicillin- mechanism of action
Penicillinase sensitive or resistant? Spectrum narrow or wide? |
SAME AS PENICILLIN
Wide spectrum Penicillinase sensitive |
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Ampicillin, amoxicillin can be combined with _ to enhance spectrum
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Clavulinic acid
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Which has greater oral bioavailibility - amoxicillin or ampicillin
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AmOxicillin has greater Oral bioavailibility
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Name antibiotics that are extended-spectrum penicillins - against certain gram positive and gram negative rods
Name rods |
HELPS kill enterococci - H influenzae, E.coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, enterococci
Ampicillin, amoxicillin |
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Toxicity for ampicillin and amoxicillin
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Hypersensitivity reactions, ampicillin rash, pseudomembranous colitis
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Mechanism for carbenicillin, pipercillin, ticarcillin
Spectrum? |
Same as penicillin, extended spectrum
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Name penicillins used for treatment of Pseudomonas, and gram negative rods
Is it penicillinase resistant or sensitive Can it be used with clavulinic acid |
Carbencillin, Piperacillin, Ticarcillin
Penicillinase sensitive Use with clavulinic acid |
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Toxicity for carbencillin, piperacillin, ticarcillin
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Hypersensitivity reactions
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Beta lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases, bactericidal
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CEPHALOSPORINS
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Which cephalosporins target gram positive cocci + Proteus , E. coli,Klebsiella
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1st generation
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Which cephalosporins target gram positive cocci + H. flu, Enterobacter, Neisseria, Proteus, E coli Klebsiella, Serratia
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2nd generation
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Which cephalosporins target serious gram negative infections resitant to other beta lactams, meningitis (most penetrate BBB) - give examples
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3d generation - ceftazidime, ceftriaxone
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3d generation cephalosporin used for treatment of Pseudomonas
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Ceftazidime
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3d generation cephalosporin used for treatment of gonorrhea
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Ceftriaxone
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Which cephalosporins have increased activity agains Psedudomonas and gram positive organisms
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4th generation
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Is there cross hypersensitivity between cephalosporins and penicillin
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Yes, 5-10%
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Toxicity for cephalosporins
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Hypersensitivity reactions
Increase nephrotoxicity of aminoglycosides Disulfiram like reaction with ethanol (in cephalosporins with methylthiotetrazole group) - cefamandole |
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A monobactam resistant to beta lactamases. Inhibits cell wall synthesis (binds to PBP3), synergistic with aminoglycosides, no cross allerginicity with penicillins
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AZTREONAM
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This antibiotic is used for Gram negative rods (Klebsiella, Pseudomonas, Serratia), no activity agains gram positives or anaerobes, for penicillin allergic patients and those with renal insufficiency who cannot tolerate aminoglycosides
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AZTREONAM
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Is there any toxicity associated with AZTREONAM
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Usually nontoxic, occasional GI upset
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Broad spectrum beta lactamase resistant carbapenem
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Imipenem
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Imipenem is ALWAYS administered with _
WHY? |
CILASTATIN
Inhibitor of renal dihydropeptidase I - to decrease inactivation of the drug in renal tubules |
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Drug of choice for Enterobacter, also active against gram positive cocci, gram negative rods and anaerobes
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Imipenem + cilastatin
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Toxicity associated with Imipenem/cilastatin
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GI distress, skin rash, CNS toxicity (seizures) at high plasma levels
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Inhibits cell wall mucopeptide formation by binding D ala D ala portion of cell wall precursors. Resistance occurs with amino acid change of D ala D ala to D ala D lac
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VANCOMYCIN
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This antibiotic is used for serious gram positive multi drug resistant organisms, including S aureus, and Clostridium difficile (pseudomembranous colitis)
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VANCOMYCIN
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Diffuse flushing ("red man syndrome") associated with vancomycin can be largely prevented by?
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Pretreatment with antihistamines and slow infusion rate
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Toxicity for Vancomycin
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Nephrotoxicity
Ototoxicity Thrombophlebitis Well tolerated in general - does NOT have many problems |
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Gentamicin, neomycin, amikacin, tobramycin, streptomycin - what class of antibiotics?
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Aminoglycosides
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Bactericidal, inhibit formation of initiation complex and cause misreading of mRNA. Require O2 for uptake, therefore ineffective against anaerobes
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AMINOGLYCOSIDES
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Which aminoglycoside is used for bowel surgery
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Neomycin
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Aminoglycosides are _ with beta lactams
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Synergistic
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Aminoglycosides are clinically used for treatment of _
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Severe gram negative rod infections
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Toxicity of aminoglycosides
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Nephrotoxicity (especially with cephalosporins)
Ototoxicity (especially with loop diuretics) |
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Doxycycline, demeclocycline, minocycline - name class of antibiotics
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Tetracyclines
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Bacteriostatic, bind to 30S and prevent attachment of aminoacyl-tRNA, limited CNS penetration
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Tetracyclines
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Which tetracycline is fecally eliminated and can be used in patients with renal failure
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Doxycycline
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Must NOT take tetracyclines with _
Why? |
Milk
Antacids Iron containing preparations Divalent cations inhibit its absorption in gut |
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Clinical use of tetracyclines
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Vibrio cholerae
Acne Chlamydia Ureaplasma Urealyticum Mycoplasma pneumonia Borelia burgdorferi Riccketsia Tularemia VACUUM your BedRoom Tonight |
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Toxicity of tetracyclines
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GI distress, discoloration of teeth and inhibition of bone growh in children, photosensitivity
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Erythromycin, azithromycin, clarithromycin- name class of antibiotics
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Macrolides
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Inhibit protein synthesis by blocking translocation - bind to 23S rRNA of 50S ribosomall subunit, bacteriostatic
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Macrolides
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Clinical use macrolides
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URI
Pneumonia STD gram positive cocci (streptococcal infections in patients allergic to penicillin), Mycoplasma, Legionella, Chlamydia, Neisseria |
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Toxicity macrolids
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GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rashes
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Patient on antibiotic therapy develops acute cholestatic hepatitis - which clas of drug?
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Macrolides
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Most common cause of non compliance with macrolides
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GI discomfort
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Inhibits 50S peptidyltransferase, bacteriostatic
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Chloramphenicol
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This drug is used for treatment of meningitis (H flu, N meningitidis, Strep pneumoniae) but conservatively used due to toxicities
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Chloramphenicol
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Toxicities with chloramphenicol
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Anemia (dose dependent)
Aplastic anemia (dose independent) Gray baby syndrome |
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Which drug causes gray baby syndrome and why
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Chloramphenicol - premature infants because they lack liver UDP-glucuronyl transferase)
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Blocks peptide bond formation at 50S ribosomal subunit, bacteriostatic
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Clindamycin
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Which antibiotic is used to treat anaerobic infections (Bacteroides fragilis, Clostridium perfringens)
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CLindamycin
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Toxicity associated with clindamycin
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Pseudomembranous colitis (C. difficile overgrowth), fever, diarrhea
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PABA antimetabolites inhibit dehydropteorate synthase, bacteriostatic
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Sulfonamides
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Which sulfonamides are used for treatment of simple UTI
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Triple sulfas or SMX
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Clinical use of sulfonamides
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Gram positive
Gram negative Nocardia Chlamydia |
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Toxicity with sulfonamides
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Hypersensitivity reactions
Hemolysis if G6PD deficient Nephrotoxicity (tubulointerstitial nephritis) Kernicterus in infants Displace other drugs from albumin (warfarin) |
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Antibiotic inhibits dihydropteorate synthase
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Sulfonamides
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Antibiotic inhibits dihydrofolate reductase
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Trimethoprim, pyrimethamine
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Inhibits bacterial dihydrofolate reductse, bacteriostatic
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Trimethoprim
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This drug is used in combination with sulfonamides causing sequential block of folate synthesis
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Trimethoprim
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This drug is used for recurrent UTI's, Shigella, Salmonella, Pneumocystis carinii pneumonia
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TMP-SMX
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Toxicity of trimethoprim
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Megaloblastic anemia
Leukopenia Granulocytopenia TMP - Treats Marrow Poorly |
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Toxicity connected with trimethoprim can be alleviated by _
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Supplemental folinic acid
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Ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin - name class
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Fluoroquinolones
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Antibiotics inhibit DNA gyrase (topoisomerase II), bactericidal
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Fluoroquinolones
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Used clinically for treatment of gram negative rods of urinary and GI tracts (including Pseudomonas), Neisseria, some gram positive organisms
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Fluoroquinolones
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Are fluoroquinolones safe in pregnant women
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Contraindicated in pregnant women and in children because animal studies show damage to cartilage.
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Fluoroquinolones toxicity
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Tendonitis and tendon rupture in adults
GI upset Superinfections Skin rashes Headache Dizziness FluoroquinoLONES hurt attachments to your BONES |
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Forms toxic metabolites in bacterial cells, bactericidal
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Metronidazole
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Antiprotozoal, Giardia, Entamoeba, Trichomonas, Gardenrella vaginalis, anearobes (bacteroides, clostridium) - name drug
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Metronidazole
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This drug is used with bismuth and amoxicillin (or tetracycline) for "triple therapy" against H pylori
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Metronidazole
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Anaerobic infections above diaphragm - ?
Anaerobic infections below diaphragm? |
Above - clindamycin
Below - metronidazole |
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Toxicity of metronidazole
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Disulfiram like reaction with alcohol, headache
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Bind to cell membranes of bacteria and disrupt their osmotic properties, cationic, basic proteins that act like detergents - treat resistant gram negativ infections
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Polymyxins
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Toxicity for polymyxins
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Neurotoxicity
Acute renal tubular necrosis |
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Name anti TB drugs
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RESPIre
Rifampin Ethambutol Streptomycin Pyrazinamide Isoniazid |
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2nd line therapy for TB
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Cycloserine
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All anti TB drugs have same toxicity - name it
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liver toxicity
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Anti TB drug - decreases synthesis of mycolic acids
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Isoniazid
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The only agent used as solo prophylaxis against TB
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Isoniazid
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Toxicity for INH (Isoniazid)
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Hemolysis if G6PD defficient
Neurotoxicity Hepatoxocitiy SLE like syndrome INH - Injures Neurons and Hepatocytes |
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_ can prevent neurotoxicity caused by isoniazid
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Pyridoxine (B6)
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Which anti TB drug has different half lifes in fast vs slow acetylators
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Isoniazid
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Anti TB drug - inhibits DNA dependent RNA polymerase
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Rifampin
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Delays resistance to dapsone when used for leprosy
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Rifampin
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Used for meningococcal prophylaxis and chemoprophylaxis in contacts of children with H influenzae type B
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Rifampin
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Rifampin toxicity
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Minor hepatoxicity and drug interactions (increases P450)
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Rifampin 4 R's
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RNA polymerase inhibitos
Revs up P450 Red/orange body fluids Rapid resistance if used alone |
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Beta lactamase cleavage of beta lactam drug is a resistance mechanism against which drugs
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Penicillins and cephalosporins
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Modification via acetylation, adenylation, or phosphorylation is resistance mechanism against which drugs
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Aminoglycosides
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Terminal D ala component of cell wall replaced with D lac, decreases affinity - resistance mechanism against which drug
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Vancomycin
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Modification via acetylation - resistance mechanism against which drug
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Chloramphenicol
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Decreased uptake or increased transport out of cell is resistance mechanism against which drugs
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Tetracyclines
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Altered enzyme (bacterial dihdropteorate synthetase), decreased uptake or increased PABA synthesis is resistance against which drugs
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Sulfonamides
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Drug of choice for prophylaxis of meningococcal infections
Alternative? |
Rifampin
Minocyclin |
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Prophylaxis of gonorrhea
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Ceftriaxone
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Prophylaxis of syphillis
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Benzathine penicillin G
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Prophylaxis in patients with history of recurrent UTI
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TMP-SMX
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Drug of choice for prophylaxis for pneumocystic carinii pneumonia
Alternative |
TMP-SMX
Aerosolized pentamidine |
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Binds ergosterol (unique to fungi), forms membrane pores that allow leakage of electrolytes and disrupt homeostasis
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Amphotericin B
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Used for wide spectrum of systemic mycoses (Cryptococcus, Blastomyces, Coccidioides, Aspergillus, Histoplasma, Candida, Mucor). Intrathecally for fungal meningitis, does NOT cross BBB
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Amphotericin B
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Toxicity of Amphotericin B
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NEPHROTOXICITY
Arrhythmias (amphoterrible) Fever/chills (shake and bake) Hypotension |
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Binds to ergosterol, disrupting fungal membranes, used as "swish and swallow" for oral candidiasis (thrush)
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NYSTATIN
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Inhibit fungal steroid (ergosterol) synthesis
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AZOLES
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Drug of choice for cryptococcal meningitis in AIDS patients and candidal infections of all types (i.e yeast infections)
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FLuconazole
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Drug of choice for Blastomyces, Coccidioides, Histoplasma, Candida albicans, hypercortisolism
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Ketoconazole
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Toxicity of azoles
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Hormone synthesis inhibition (gynecomastia)
Liver dysfuntion (inhibits cytochrome P450) Fever, chills |
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Inhibits DNA synthesis by conversion to fluorouracil which competes with uracil, used in systemic fungal infections (Candida, Cryptococcus), causes bone marrow suppression, n/v/d
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FLUCYTOSINE
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Antifungal medication, inhibits cell wall synthesis, clinically used for invasive aspergillosis, can cause GI upset and flushing
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CASPOFUNGIN
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Antifungal, inhibits fungal enzyme squalene epoxidase, used to treat dermatophytoses (especially onychomycosis)
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TERBINAFINE
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Anti fungal, interferes with microtubule function, disrupts mitosis, deposits in keratin containing tissues (nails) - oral treatment of superficial infections, inhibits growth of dermatophytes (tinea, ringworm)
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GRISEOFULVIN
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|
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Toxicity Griseofulvin
|
Teratogenic
Carcinogenic Confusion' Headache Increased warfarin metabolism |
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Antiviral drug used for prophylaxis for influenza A and treatment of Parkinsons
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Amantadine
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Derivative of Amantadine with fewer CNS side effects
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Rimantidine
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Anti viral medication, blocks biral penetration/uncoating, may buffer pH of endosome, also causes release of dopamine from intact nerve terminals
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Amantadien
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Toxicity of amantadine
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Ataxia + dizziness+ slurred speech
Amantadine causes problems with cerebellA |
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Two antiviral medications that inhibits influenza neuraminidase, both used for influenza A and B
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Zanamivir
Oseltamivir |
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Antiviral - inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase, used for treatment of RSV and chronic hep C
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Ribavirin
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Toxicity for Ribavirin
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Severe teratogen
Hemolytic anemia |
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THis antiviral medication preferentially inhibits viral DNA polymerase when phosphorylated by viral thymidine kinase
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Acyclovir
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Antiviral medication used for treatment of VZV, HSV, EBV, mucocutaneous and genital herpes lesions, prophylaxis in immunocompromised patients
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Acyclovir
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Toxicity for acyclovir
|
Delirium
Tremor Nephrotoxicity |
|
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Antiviral drug - works by phosphorylation viral kinase, preferentially inhibits CMV DNA polymerase, drug of choice for CMV especialy in immunocopromised patients
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Ganciclovir
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Which drug is more toxic - acyclovir or ganciclovir to host enzymes
|
Ganciclovir
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Ganciclovir toxicity
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Leukopenia
Neutropenia Thrombocytopenia Renal toxicity |
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Viral DNA polymerase inhibitor that binds to the pyrophosphate binding site of the enzyme. Does not require activation by viral kinase
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FOSCARNET = pyroFOSphate analog
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Antiviral drug used for treatment of CMV retinitis in immunocompromised patients when ganciclovir fails
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FOSCARNET
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Patient is on foscarnet for CMV retinitis, which toxicity could be suspected?
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Nephrotoxicity
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Saquinavir, ritonavir, indinavir, nelfinavir, aprenavir - class of drugs
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HIV therapy, protease inhibitors - inhibit assembly of new virus by blocking protease enzyme
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HIV patient is taking anti HIV drugs, develops GI intolerance - nausea, diarrhea, hyperglycemia, lipid abnormalities, thrombocytopenia - which drugs was he taking
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PROTEASE INHIBITORS
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Zidovudine (AZT), didanosine, zalcitobine, stavudine, lamivudine, abacavir - what class of drugs
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Reverse transcriptase inhibitors, nucleosides
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Name non-nucleosides reverse transcriptase inhibitors
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Nevirapine
Delavirdine Efavirenz |
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Toxicity associated with reverse transcriptase inhibitors
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Bone marrow suppression (neutropenia, anemia)
Peripheral neuropathy Lactic acidosis (nucleosides) Megaloblastic anemia Rash (non-nucleosides) |
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Highly active antiretroviral therapy (HAART) generally entails combination of?
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Protease inhibitors + reverse transcriptase inhibitors
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Which antiretroviral drug is used during pregnancy to reduce risk of fetal transmission
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AZT
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Patient on anti HIV therapy develops megaloblastic anemia - which drug most likely caused it
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AZT
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When is HAART initiated?
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When patients have low CD4 counts (<500 cell/mm3) or high viral load
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Glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis, used for treatment of chronic hep B and C, Kaposis sarcoma
Name drug and what toxicity associated with it |
Interferons
Neutropenia |
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Antiparasitic drug from onchocerciasis
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Ivermectin (rIVER blindness treated with IVERmectin)
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Antiparasitic drug used to treat nematode/roundworm (pinworm, whipworm) infections
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Mebendazole/thiabendazole
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Antiparasitic drugs used to treat gian roundowrm (ascaris), hookworm (Necator/Ancylostoma) and pinworm (Enterobius)
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Pyrantel pamoate
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Antiparasitic used to treat trematode/fluke (shistosomes, Paragonimus, Clonorchis) and cysticercosis
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Praziquantel
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Niclosamide is used to treat?
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Cestode/tapeworm infections except cysticercosis
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Drug of choice for leishmaniasis
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Pentavalent antimony
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Name anti malaria drugs
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Chloroquine
Quinine Mefloquine Atovaquone Proguanil |
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Name drug used for treatment of latent hypnozoite (liver) forms of malaria (Plasmodium vivax, P.ovale)
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Primaquine
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Drug of choice agains giardiasis, amebic dysentery, bacteria vaginitis, Trichomonas
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Metronidazole
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Drug of choice for Chagas disease, American trypanosomiasis (trypanosoma cruzi)
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Nifurtimox
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Drug of choice for African trypanosomiasis (sleeping sickness)
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Suramin
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Cholinomimetic used for postoperative and neurogenic ileus and urinary retention - activates bowel and bladder smooth muscle
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BETHANECHOL
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Direct agonist, cholinomimetic used for treatment of glaucoma, activates ciliary muscle of eye (open angle), pupillary sphincter (narrow angle)
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Carbachol, pilocarpine
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Anticholinesterase, used in treatment of postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative), increases endogenous Ach
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Neostigmine
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Anticholinesterase used in treatment of myasthenia gravis - increases endogenous Ach, increases strength
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Pyridostigmine
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This anticholinesterase is used for diagnosis of myasthenia gravis (extremely short acting), increases endogenous Ach
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Edrophonium
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Anticholinesterase, used in treatment of glaucoma (crosses BBB to CNS) and atropine overdose, increases endogenous Ach
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Physostigmine
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Anticholinergic, used for treatment of glaucoma, increases endogenous Ach
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Echothiophate
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Name symptoms of cholinesterase inhibitor poisoning
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DUMBBELSS
Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle Lacrimation Sweating Salivation (also abdominal cramping) |
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Name substances that can lead to cholinesterase inhibitor poisoning
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Parathion and other organophosphates
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Antidote used in treatment of organophosphate poisoning
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Atropine (muscarinic antagonist) plus pralidoxime (chemical antagonist used to regenerate active cholinesterase)
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