Term
|
Definition
• Glucocorticoid-stimulated synthesis of lipocortin → PLA2 inhibition
• Directly suppresses COX2 expression |
|
|
Term
Non-selective COX 1/2 Inhibitors (mechanism)
Aspirin , Indomethacin, ibuprofen, naproxen, Acetaminophen (NSAIDs) |
|
Definition
• Irreversible acetylation of COX-1 & COX-2
• Increase leukotriene formation |
|
|
Term
Non-selective COX 1/2 Inhibitors (effects)
Aspirin , Indomethacin, ibuprofen, naproxen, Acetaminophen (NSAIDs) |
|
Definition
• Anti-inflammatory (except acetaminophen)
• Anti-pyretic
• Analgesic
• Anti-platelet aggregation (except acetaminophen)
• Relieve dysmenorrhea caused by excessive PGE2 & PGF2a |
|
|
Term
Non-selective COX 1/2 Inhibitors (Side effects)
Aspirin , Indomethacin, ibuprofen, naproxen, Acetaminophen (NSAIDs) |
|
Definition
• Gastric irritation
• Affect protective gastric mucosal prostaglandins
• Bleeding
• Occasionally rash, dizziness, salicylism (vomiting, auditory deficits)
• At high doses: hyperpnea, respiratory acidosis, cardiotoxicity
• Prolonged labor & premature ductus arteriosus closure
o Cross reactions
• Potentiate anticoagulants because of anti-platelet effects
• Also reduce effects of diuretics & anti-hypertensives
• Competition for binding of plasma proteins can affect many drugs |
|
|
Term
|
Definition
o Mostly a COX-3 inhibitor in the brain (a little COX1/2)
• CNS effects = anti-pyretic, analgesic
o Leading cause of acute liver failure |
|
|
Term
| • Acetylsalicylic Acid (ASA, Aspirin) |
|
Definition
o Low dose reduces risk of death from thrombosis & MI
- Irreversibly binds COX1/2 |
|
|
Term
Celecoxib (Celebrex)
[rofecoxib (Vioxx) removed from market]
MECHANISM |
|
Definition
Selective COX2 inhibitor
• COX-2 expression is regulated by proinflammatory factors
• Antagonists reduce local inflammatory response |
|
|
Term
| Celecoxib effects & side effect |
|
Definition
• Analgesic
• Antipyretic
• No effect on platelet aggregation or gastric mucosal prostaglandins
Side effects
• COX-2 inhibition allows elevation of platelet-generated COX1 production of thromboxanes → increases risk of MI |
|
|
Term
|
Definition
Lipoxygenase inhibitor
• Prevents leukotriene synthesis → reduces bronchoconstriction
• Used in Asthma & allergic reactions |
|
|
Term
Zafirlucast (Accolate)
montelucast (singulair) |
|
Definition
Leukotriene receptor antagonists
- bronchodilation
-used for asthma |
|
|
Term
|
Definition
PGE-1
• Vasodilator
• Inhibits platelet aggregation
• Contracts uterine / intestinal smooth muscle
o Adverse effects
• Bradycardia
• Hypotension
• Fever
• Ductal fragility
• Apnea
• Contraindicated with respiratory distress |
|
|
Term
|
Definition
• Prevents gastric ulcers associated with non-selective COX inhibitors
Adverse effects
• Abdnominal pain
• Diarrhea (infrequent)
• Contraindicated in pregnancy |
|
|
Term
|
Definition
PGE2
• Promotes uterine contraction & induces labor / abortion
Adverse effects
• Vomiting
• Diarrhea
• Fever
• Bronchoconstriction (at high doses) |
|
|
Term
|
Definition
PGF2
• Reduces intraocular pressure
• Treats glaucoma |
|
|
Term
| epoprostenol / treprostinil |
|
Definition
PGI1 / PGI1 analog
• Lowers vascular pressure
• Treats pulmonary hypertension
Side effects
• Nausea, headache, hypotension, flushing |
|
|
Term
|
Definition
PAF antagonist
-reduces vasodilation, edema, smooth muscle contraction, ulcers |
|
|
Term
| Tubocurarine, succinylcholine, morphine, Vancomycin |
|
Definition
|
|
Term
|
Definition
1st generation H1 receptor antagonist
CNS effects --> sedation
In addition to allergies, treats nausea/vomiting, motion sickness
Antiparkinsonian |
|
|
Term
|
Definition
Zyrtec
H1 receptor antagonist
2nd generation |
|
|
Term
|
Definition
Claritin
H1 receptor antagonist
2nd generation |
|
|
Term
|
Definition
Allegra
H1 receptor antagonist
2nd generation |
|
|
Term
|
Definition
H2 receptor antagonist
-Treatment of gastric ulcers / GERD
-50% bioavailability
-excreted by kidneys
-P450 inhibitor
Side effects
DO NOT GIVE TO ELDERLY! (CNS effects)
Androgen receptor --> gynecomastia |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
H2 receptor antagonist
• AChesterase inhibitor (increases GI motility)
- bioavailability higher- 90% |
|
|
Term
|
Definition
o Stimulate direct release of 5-HT
o Appetite suppressant (banned by FDA)
o Similar to MDMA |
|
|
Term
|
Definition
o SSRI
o Inhibits 5HT reuptake
o MDD & OCD treatment |
|
|
Term
|
Definition
• 5-HT1 agonist
• Causes vasoconstriction of cranial vessels
- treatment of acute migraines |
|
|
Term
|
Definition
| • 5HT4 partial agonist • stimulates peristalsis / gastric emptying - treatment of IBS w constipation |
|
|
Term
|
Definition
o 5-HT3 antagonists
o treats chemo-induced nausea & vomiting
(danse the nausea away!) |
|
|
Term
|
Definition
5-HT2A/B/C antagonist
• Prophylactic migraine treatment
• Tx of Diarrhea, malabsorption, dumping syndrome |
|
|
Term
|
Definition
5-HT2A antagonist AND H-1 blocker
• Postgastrectomy dumping syndrome |
|
|
Term
|
Definition
ACE inhibitors
o Block AT1 → AT2 AND block bradykinin catabolism
o → lowers BP by inhibiting vasoconstriction (AT) & promoting vasodilation (bradykinins)
o Side effects
• Buildup of kinins in lungs → edema / coughing |
|
|
Term
|
Definition
Angiotensin II receptor antagonists
-similar to ACE inhibitors but with fewer side effects |
|
|
Term
| Nitroprusside & nitroglycerin |
|
Definition
Generate NO
• NO contributes to vascular tone, cGMP relaxes smooth muscle (given to ppl having heart attack)
• Inhibits LDL oxidation → prevents foam cells (atherosclerosis)
• Inhibits platelet aggregation (thrombosis)
- Also for tx of erectile dysfunction (vasodilation) |
|
|
Term
|
Definition
Generates NO
• Induces cGMP by inhibiting breakdown by PDE
- used in tx of erectile dysfunction (viagra) |
|
|
Term
|
Definition
Narrow spectrum (G+)
Used against streptococci & meningococci
V = oral against pharyngitis from group A strep |
|
|
Term
| Nafcillin & Dicloxacillin |
|
Definition
penicillinase-resistant penicillins
G+
Used against staphy --> endocarditis, osteomyelitis, cellulitis |
|
|
Term
|
Definition
- 1st gen cephalosporin
- G+ cocci
- Surgical prophylaxis against staph |
|
|
Term
|
Definition
2nd gen Cephalosporin
- G+ and G-
- Treat otitis media (H influenzae) |
|
|
Term
|
Definition
3rd gen cephalosporin
-mostly G-
Treat meningitis
Ceftriaxone for gonorrhea |
|
|
Term
|
Definition
G+ only
IV infusion for MRSA
Oral for C difficile |
|
|
Term
|
Definition
Aminoglycoside
Aerobic G- and some G+
Enterococcal & staphylococcal infections |
|
|
Term
| Tetracycline, Doxycycline |
|
Definition
| Used against Rickettsia, Lyme disease, M pneumonia, Clamydia trachomatis, Acne, & shortens cholera therapy |
|
|
Term
|
Definition
macrolide
G+ bacteriostatic
Uses: pneumonia, chlamydia, H influenzae (otitis media), peptic ulcer (H pylori) |
|
|
Term
|
Definition
Penicillin-resistant Streptococci
Necrotizing fasciitis |
|
|
Term
|
Definition
UTI
otitis media
But causes crystalluria, skin rashes, kernicterus in neonates |
|
|
Term
| Ciprofloxacin, Levofloxacin |
|
Definition
broad spectrum bactericidal
UTI's, prostatitis, traveller's diarrhea |
|
|
Term
|
Definition
Inhibits synth of mycolic acid to treat TB
Adverse effects: peripheral neuropathy, hepatitis |
|
|
Term
|
Definition
| Binds to Beta subunit of RNA Polymerase -> inhibits DNA transcription |
|
|
Term
|
Definition
inhibits cell wall synth
TB treatment (resistant bacilli)
AE: optic neuritis, acute gout |
|
|
Term
|
Definition
Decreases time to treat TB
AE: acute gout |
|
|
Term
|
Definition
Amoxicillin
or Amoxicillin + clavulanate
If amox causes diarrhea --> Cefprozil |
|
|
Term
| Surgical prophylaxis treatment |
|
Definition
Cefazolin (IV) (cardio, orthopedic surgeries)
Vancomycin against MRSA
Neomycin + Erythromycin (Oral) + IV cefoxitin (colorectal, appendectomy) |
|
|
Term
| Community acquired pneumonia treatment |
|
Definition
Erythromycin (+ cefotaxime if in hospital)
If neutropenic --> levofloxacin |
|
|
Term
| Nosocomial pneumonia treatment |
|
Definition
piperacillin + gentamicin
alternative: ceftazidime + gentamicin |
|
|
Term
|
Definition
Ceftriaxone or Cefixime (oral)
Penicillin allergy --> Ciprofloxacin |
|
|
Term
|
Definition
Ciprofloxacin
alternative = TMP-SMX |
|
|
Term
|
Definition
TMP-SMX
if that causes rash -> ciprofloxacin (or levo)
If pt is pregnant -> Cephalexin |
|
|
Term
|
Definition
Antiviral, lipophilic
blocks M2 protein / nucleocapsid release
AEs: CNS effects
Uses: Influenza A treatment & prevention, Parkinson's disease |
|
|
Term
|
Definition
Antiviral, less lipophilic
Blocks M2 protein / inhibits nucleocapsid release
Uses: influenza A treatment & prevention |
|
|
Term
|
Definition
Antiviral (tamiflu) prodrug
Mechanism: inhibits neruaminidase from influenza A & B viruses
AE's: nausea, vomiting, diarrhea, teratogenci |
|
|
Term
|
Definition
antiviral, guanosine analog (prodrug)
non-selective
inhibits host inosine monophosphate dehydrogenase & RNA polymerase of virus
Uses: RESPIRATORY SYNCYTIAL VIRUS, chronic hep c, viral hemorrhagic fevers
AE's: teratogenic (Cat X), need contraception (2 forms) |
|
|
Term
|
Definition
Herpes virus
Guanosine analog
Selectively targets host - phosphorylated by thymidine kinase
Inhibits viral DNA polymerase
AE's: not teratogenic
Tx: HSV, VZV treatment |
|
|
Term
|
Definition
antiviral, prodrug, non-selective
used for herpes keratitis (but replaced by acyclovir) |
|
|
Term
|
Definition
Antiviral, herpes
inhibits viral DNA Polymerase & decreases chain elongation rate
Not as specific
Treatment: CMV, cytomegalic retinitis
AE's: leukopenia, thrombocytopenia, teratogenic (C) |
|
|
Term
|
Definition
-Nitrogen mustards / alkylating agent (anti-cancer)
-administered by fast iv infusion
-Action = non-enzymatic, cross-linking of guanines
-high toxicity |
|
|
Term
|
Definition
-nitrogen mustard, alyklating agent, anti-cancer
-prodrug, can be taken orally
-Metabolized by Cyt P450 --> metabolizes to phosphoramide (active) + acrolein (toxic)
-Side effects: hemorrhagic cystitis (give Mesna)
-Drug interaction: allopurinol reduces levels of CYP450 --> decrease cyclophosphamide
-also used for Rheumatoid arthritis (immunosuppresant) |
|
|
Term
| Nitrosoureas (carmustine, lomustine, semustine, streptozotocin) |
|
Definition
alkylating agent - alkylates DNA
-Toxicity: Car, Lo, Sem = lipophilic = delayed myelosuppression (crosses BBB)
Strepto - hydrophilic = destroys B cells in pancreas |
|
|
Term
|
Definition
Alkylating agent, cross-linking of guanine residues
- IV
- Toxicity: ototoxicity, peripheral neuropathy, nephrotoxicity (need high water intake), mild myelosuppression (vs carboplatin) |
|
|
Term
|
Definition
-DNA Methylating agent (anticancer)
-Prodrug, activated by CYP450 and MAO
inhibits p450 and MAO
Interactions: + sympathomimetic agents (beer, wine, cheese, yogurt) -> hypertension; + sedatives (barbituates, phenothazines, narcotics) --> potentiates sedative |
|
|
Term
|
Definition
Folate antagonist (antineoplastic)
- Folic acid analog -> binds to dihydrofolate reductase (comp inhibition) --> can't synth dTMP nucleotide
-binds to albumin
-stays in tumor cells bc of added gulatmate residues
-Toxicity: increased dose to overcome resistance --> tissue damage - (give leucovorin)
-Interactions: aspirin, sulfonamides displace from albumin-> increase plasma levels/toxicity |
|
|
Term
|
Definition
Pyrimidine antagonist (anti-neoplastic)
-prodrug
-inactivates thymidylate synthase |
|
|
Term
|
Definition
-anti-neoplastic
-incorporates into DNA instead of dCTP --> terminates strand elongation
-Toxicity: cerebral dysfunction |
|
|
Term
| Thiopurines (mercaptopurine) |
|
Definition
-antineoplastic
-prodrug - inhibits de novo purine synth (IMP dehydrogenase)
Drug Interactions: +allopurinol (to reduce gouty attacks) -->metabolizes mercap to inactive form (reduce mercapt to 25%) |
|
|
Term
|
Definition
Vinca alkaloid, antineoplastic, spindle toxin
- binds to tubulin dimer --> prevents polymerization, enhances depolymerization
-Toxicity: peripheral neuropathy, GI, (minimal myelosuppression - compared to vinblastine) |
|
|
Term
|
Definition
- antineoplastic, natural product
- stabilizes microtubule by binding to polymer -> can't retract for division |
|
|
Term
|
Definition
Epipodophyllotoxin, antineoplastic
- blocks G2 phase by binding to topoisomerase II |
|
|
Term
| Anthracyclines (doxorubicin, daunorubicin) |
|
Definition
-Antibiotic, antineoplastic
- binds between bases in DNA --> decreases synthesis; inhibits topoisomerase II, generates O2 radicals (arrest cells in G2)
- Toxicity: cardiomyopathy, O2 radicals |
|
|
Term
|
Definition
Antibiotic, antineoplastic
-Reduces Fe2+, Cu+--> O2 radicals --> DNA strand breaks (inhibits G2)
-Toxicity: pulmonary fibrosis, 100% O2 contraindicated, minimal O2 before surgery, but no myelosuppression |
|
|
Term
|
Definition
Glucocorticoid, antineoplastic
-induces apoptosis in T lymphocytes
-can be given in case of liver failure |
|
|
Term
Estrogens
-ethinyl estradiol
-Diethylstibestrol |
|
Definition
-antineoplastic
-Treat prostate carcinomas --> inhibits LH thru neg feedback
-Side effects: tumor flare, hypertension, CHF, oxygen radicals |
|
|
Term
|
Definition
-Antiestrogen, antineoplastic
-targets ER+ breast tumors, most effective if also PR+
-Side effects: hot flashes, tumor flare, endometrial cancer (Raloxifen is a better alternative) |
|
|
Term
Aromatase inhibitors
-Anastrozole
-Letrozole |
|
Definition
-antineoplastic
-used in post-menopausal breast ca, when estrogen is synth mostly in adipose tissue --> decreases estradiol
Side effects: Cyt P 450 inhibitor |
|
|
Term
|
Definition
antiandrogen, antineoplastic
-treat prostatic carcinoma
-competes with testosterone
Side effects: blocks feedback inhibition of LH -> LH & testosterone (so use w LHRH) |
|
|
Term
LHRH agonsists
-Leuprolide
-goserelin |
|
Definition
-antineoplastic
-First causes LH rise, tumor flare ->internatlization & downregulation of receptors -> decrease LH / testosterone / estradiol (same as castration / oophorectomy) |
|
|
Term
|
Definition
| Accute (fire)-->carboxy Hb--> hypoxia-->headache, tachycardia, tachypnea, coma, convulsions, resp failure, tightness in temporal area, confusion, loss of vision, |
|
|
Term
|
Definition
| O2: 100% initially, hyperbaric if severe |
|
|
Term
|
Definition
| Industrial: fumigation of ships, sterilization of soil, metallurgy |
|
|
Term
|
Definition
| plant seeds, silver polish, pesticides |
|
|
Term
|
Definition
| metabolite of nitroprusside, a vasodilator for HTN |
|
|
Term
|
Definition
| binds to cytochrome oxidase, stops ETC, blocks O2 utilization, death is due to resp failure |
|
|
Term
|
Definition
| cellular hypoxia, no cyanosis, bright red venous blood, bitter almond breath, rapid coma |
|
|
Term
|
Definition
| amyl nitrite oxidizes limited Hb to methemoglobin, which competes with Cyt oxidase for CN and is eliminated, followed by IV sodium thiosulfate to accelerate detox via mitochondrial rhodanese. Last step is methylene blue to reduce methemoglobin to Hb. |
|
|
Term
|
Definition
| alcohol dehydrogenase converts to formic acid, limited conversion to CO2 by folate dependent system, formic acid accumulates |
|
|
Term
|
Definition
| irreversible blindness, metabolic acidosis, death |
|
|
Term
|
Definition
| EtOH competitive inhibitor, 10-20x greater affinity, Bicarb for metabolic acidosis, hemodialysis to remove MeOH and formic acid, folate to increase conversion to CO2 |
|
|
Term
|
Definition
| GI irritation and bleeding, met. acidosis, hepatic failure, pulmonary edema |
|
|
Term
|
Definition
| deferoxamine (desferal) if serum Fe greater than 400ug/ml |
|
|
Term
|
Definition
| erythrocytes, soft tissues, bone |
|
|
Term
|
Definition
| hypochromic microcytic anemia due to inhibition of heme synthesis and shortened RBC lifespan |
|
|
Term
|
Definition
| peripheral neuropathy (wrist drop), encephalopathy, interstitial kidney damage, decreased fertility in women, GI issues |
|
|
Term
|
Definition
| Calcium disodium EDTA to remove from bone, dimercaprol to remove from tissues |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| persistent in environment, lipophilic, cross BBB to affect CNS, cross placenta, secreted in milk |
|
|
Term
| Acute CAH poisoning symptoms |
|
Definition
| CNS issues, cardiac arrhythmias, fibrillation, liver and kidney damage, severe skin eruptions (chloracne) |
|
|
Term
| Chronic CAH poisoning symptoms |
|
Definition
| liver damage and enlargement, hepatic porphyria 2' to induction of d-aminolevulinate synthase-->overproduction, accumulation, and increased excretion of porphyrins in urine, reproductive damage, cancer |
|
|
Term
|
Definition
| cholestyramine increases fecal elimination by removing bile salts. Also, activated charcoal and anticonvulsants can help. |
|
|
Term
|
Definition
| bipyridyl herbicide, targets lungs, liver, kidneys |
|
|
Term
|
Definition
| undergoes cyclic redox, generates superoxide radicals, H2O2, and OH radicals, which induce lipid peroxidation. Lipid peroxides damage membranes and enzymes--> inflammation--> widespread proliferation of fibroblasts--> pulmonary fibrosis |
|
|
Term
|
Definition
| gastric lavage, hemodialysis, hemoperfusion, activated charcoal, NOT O2!!! |
|
|
Term
| Warfarin clinical presentation |
|
Definition
| GI bleeding (melena), hematuria, epistaxis, multiple ecchymotic lesions, increased prothrombin time. |
|
|
Term
|
Definition
| Vitamin K. If seriously bleeding, fresh frozen plasma or factor IX concentrate is given. Activated charcoal removes it from the gut and cholestyramine directly binds warfarin and blocks enterohepatic recirculation. |
|
|
Term
| Warfarin interactions as drug |
|
Definition
| Sulfa potentiates it by inhibiting the inactivator, cyt. P-450. dose must be lowered |
|
|
Term
| phase I of drug biotransformation |
|
Definition
| creation or unmasking of chemical group required for phase II |
|
|
Term
| phase II of drug biotransformation |
|
Definition
| drug undergoes conjugation rxns with endogenous substances, usually cytoplasmic (except glucuronosyltransferases) |
|
|
Term
| Cytochrome P450 rxns require what components? |
|
Definition
| requires NADPH cyt P450 reductase (a flavoprotein), cytochrome P450 (a hemoprotein), and membrane lipids. |
|
|
Term
| CYP reactions catalyze what? |
|
Definition
| oxidization, using one O atom to hydroxylate drug- Monooxygenase. most commonly oxidates, hydroxylates, dealkylates, and deaminates |
|
|
Term
|
Definition
| CYP3A4, accounts for 50% of all Cyp-mediated drug oxidation rxns. Large active site, which can be occupied by 2 drugs at once! |
|
|
Term
|
Definition
| Induced by chronic EtOH abuse |
|
|
Term
| drug that skips phase I and phase II, can be directly excreted? |
|
Definition
| Streptomycin and Gentamycin |
|
|
Term
|
Definition
| Grapefruit juice, ketoconazole, metronidazole, erythromycin |
|
|
Term
|
Definition
| Rifampin, Isoniazid, St. John's Wort |
|
|
Term
| cause of red-man syndrome |
|
Definition
| vancomycin allergic response |
|
|
Term
|
Definition
| Prostaglandins (PGs), prostacyclins(PGI2), thromboxane (TXA2) |
|
|
Term
| Products of lipoxygenases |
|
Definition
|
|
Term
|
Definition
| cleaves phospholipids to release arachadonic acid for processing into eicosanoids. Dexamethasone inhibits it. |
|
|
Term
|
Definition
| glucocorticoid, inhibits PLA2, also directly suppresses COX-2 expression |
|
|
Term
| Drug that irreversibly inactivates COX 1 |
|
Definition
|
|
Term
| Reversible inactivators of COX 1 |
|
Definition
|
|
Term
| COX-2 selective antagonist |
|
Definition
| celecoxib (also vioxx, but it was too selective) avoids some kidney/GI irritation |
|
|
Term
|
Definition
| local inflammation (not GI or Kidney) |
|
|
Term
|
Definition
| COX-1 variant, targeted by acetominophen in CNS |
|
|
Term
|
Definition
Increase cAMP (Good)
- vasodilator
- decrease platelet aggregation
- decrease gastric acid
- relax bronchial muscle
Decrease cAMP (Bad)
- increase uterine muscle tone
- increase pain & temperature |
|
|
Term
|
Definition
Increase cAMP (good)
vasodilator
decrease platelet aggregation
increases Renin
Decrease gastric acid
Relax bronchial muscle & uterine tone
(side effect = pain) |
|
|
Term
|
Definition
Increases Ca++ (bad)
vasoconstrictor
increase platelet aggregation
contract bronchial muscle
increase uterine muscle tone |
|
|
Term
|
Definition
Increases Ca++ (bad)
decrease blood volume
Increase leukocyte aggregatoin
GI muscle contraction
bronchial muscle contraction --> edema
pain |
|
|
Term
|
Definition
• Stimulates G-protein coupled receptors → phospholipase C, D, A2
• Vasodilator, increases vascular permeability (edema), platelet aggregation, generates superoxide (reactive oxygen species)
• Stimulates smooth muscle contraction
• MOST POTENT ULCEROGENIC SUBSTANCE
• Inhibitor = prostacyclins |
|
|
Term
| Serotonin is synthesized from |
|
Definition
|
|
Term
| Kinin effects on cardiovascular system |
|
Definition
Vasodilate arteries
Vasoconstrict veins
Contraction of endothelial cells |
|
|
Term
|
Definition
| activates guanylyl cyclase -> produces cGMP -> activates protein kinase G -> relaxes smooth muscle & increases vascular tone; facilitates neurotransmitter release |
|
|
Term
|
Definition
Cell wall synthesis inhibitor
B-lactam binds to PBPs
-inhibited by B lactamase |
|
|
Term
|
Definition
cell wall inhibitor, bind to PBPs but more resistant to B-lactamase
1st gen = G+ --> later gen = G- |
|
|
Term
|
Definition
cell wall synth inhibitor
irriversibly binds peptidoglycan precursor
not susceptible to B-lactamase |
|
|
Term
|
Definition
binds to 30S subunit to inhibit protein synth
high renal & ototoxicity (cochlear = irriversible, vestibular = reversible) |
|
|
Term
|
Definition
Block tRNA binding to 30S subunit
Adverse effects
-discoloration of teeth
-hepatotoxicity
-nephrotoxicity, phototoxicity |
|
|
Term
|
Definition
-bind 50S subunit
-ex: erythromycin
-G+ |
|
|
Term
|
Definition
Binds to 50S
Adverse effects = may cause superinfection by C difficile |
|
|
Term
|
Definition
Inhibit DNA gyrase (topoisomerase)
CNS problems w/ coffee
Phototoxicity |
|
|
Term
|
Definition
| aminoglycosides & vancomycin |
|
|
Term
| Antibiotics not used in children |
|
Definition
| tetracycline, doxycycline, fluoroquinolones |
|
|
Term
| Azoles & erythromycin - common mechanism |
|
Definition
|
|
Term
|
Definition
aminoglycosides (ototoxicity)
tetracycline
TMP-SMX (neural tube defects)
Fluoroquinolones |
|
|
Term
Cell wall synth inhibitors (abx)
Pregnancy safe? |
|
Definition
| yes! human cells don't have cell walls |
|
|
Term
| Solution for ototoxicity from aminoglycosides? |
|
Definition
Once-daily dosing
- higher initial dose doesn't affect renal toxicity because receptors are saturated
- drug levels below toxicity line still work due to post-antibiotic effect |
|
|
Term
|
Definition
Aminoglycosides interfere w protein synthesis (bactericidal)
which leads to wrong acids incorporated --> bad proteins continue after abx given (bacteriostatic) |
|
|
Term
|
Definition
Rifampin & Isoniazid - 6 months
Pyrazinamide & Ethambutol - first 2 months |
|
|
Term
|
Definition
Metabolized by n-acetyltransferase in the liver (Phase 2)
-> CYP2E1 & CYP450 (phase 1) -> acetylhydrazine then reacts w proteins --> liver necrosis (heptatitis) |
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Term
| Ampicillin + Gentamicin / vancomycin + gentamicin interaction |
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Definition
Ampicillin/vanco makes pores in cell wall --> aminoglycoside can enter
Then aminoglycoside dose is reduced, reducing toxicity |
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Term
| eryhtromycin / -azole's + cyclosporin / warfarin |
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Definition
| inhibit cyp450 -> increase plasma concentration of CSA / warfarin -> increase renal toxicity / bleeding |
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Term
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Definition
| rifampin is a cyp-inducer ->incerases metabolism of azoles -> decreases their action |
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Term
| Sulfonamides / TMP-SMX + methotrexate / warfarin |
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Definition
Sulfonamides occupy albumin -> displace other drugs -> increase toxicity of methotrexate / warfarin
TMP-SMX also inhibits Cyp450 -> prevents metabolism of warfarin |
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Term
| Fluoroquinolones + caffeine / theophylline |
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Definition
| Fluoroquinolones inhibit caffeine/theophylline metabolism -> increases levels -> causes seizures (caffeine) |
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Term
| Causes arthropathy in children |
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Definition
|
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Term
| Causes kernicterus in neonates / fetuses |
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Definition
|
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Term
| Cause calcification of teeth & bone |
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Definition
|
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Term
| What drug can you use when erythromycin causes adverse effects / interactions? |
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Definition
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Term
| Tetracyclines / fluoroquinolones + milk & antacids (metals) |
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Definition
| abx absorption is inhibited --> phototoxicity - don't drink milk or take antacids, stay out of sun |
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Term
| Erythromycin contraindication |
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Definition
| impaired liver function (because it accumulates in the liver) |
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Term
|
Definition
1) amoxicillin (mostly G+ - for staph pneumo)
2) if resistant to penicillin - Amoxicillin + Clavulanate
3) If amoxicillin causes diarrhea - 2nd gen ceph (Cefprozil / Cefuroxime) |
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Term
| Surgical prophylaxis regimin |
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Definition
Protects against Staph
1) Cefazolin (IV) - 1st gen ceph
2) Penicillin allergy / MRSA -> Vancomycin |
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Term
|
Definition
Caused by E coli, E fecalis, Proteus, S saprophyticus
1) TMP-SMX (oral)
2) if causes rash -> Ciprofloxacin
3) If pregnant -> Cephalexin - 1st gen ceph |
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Term
| 1st gen Cephalosporin coverage |
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Definition
Cefazolin
PEcK - proteus, E coli, Klebsiella |
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Term
| 2nd gen cephalosporin coverage |
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Definition
Cefprozil, Cefurozime
HENPEcK
- H influenza, E aerogenes, Neisseria, Proteus, E coli, Klebsiella |
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Term
| 3rd Gen cephalosporin coverage |
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Definition
Ceftriaxone, Cefotaxime
- More gram - (like pseudomonas)
- used for meningitis & gonorrhea |
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Term
|
Definition
binds to ergasterol on fungal membrane
fungalcidal |
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Term
| Amphotericin B adverse effects |
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Definition
given IV
Renal toxicity
**OK for pregnant women |
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Term
|
Definition
Inhibits thymidylate synthase & RNA synthesis in fungus
Can combine w amphotericin B |
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Term
| Flucytosine adverse effects |
|
Definition
| Bone marrow depression (don't use in ADIS pts) |
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Term
Ketoconazle (itraconazole, fluconazole)
Mechanism |
|
Definition
blocks Ergasterol synthesis by inhibiting Cyp-450
Fungistatic |
|
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Term
| Ketoconazole adverse effects |
|
Definition
| inhibits sex steroid synthesis -> impotence, infertility |
|
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Term
|
Definition
Keto - candidiasis, coccidoidomycosis
Itraconazole - Aspergillosis
Fluconazole - meningeal, UTIs, prophylaxis |
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|
Term
| Candida albicans treatment |
|
Definition
Severe = amphotericin B
Mild = fluconazole / itraconazole |
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Term
Cryptococcosis treatment
Coccidioidomycosis tx |
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Definition
Nonmeningial = Ampho B
Meningitis = Ampho B + Flucytosine (intrathecal ampho for AIDS)
Mild = fluconazole |
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Term
|
Definition
amphotericin
mild = itracon / fluconazole |
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|
Term
|
Definition
amphotericin B
Mild = itra/fluc |
|
|
Term
|
Definition
Amphotericin B
Mild = itra / ketoconazole |
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Term
| Prophylactic fungal treatment for AIDS |
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Definition
|
|
Term
| Athletes foot, vaginal candidiasis treatmetn |
|
Definition
Clotrimazole / miconazole (topical)
Fluconazole for vaginal candidiasis |
|
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Term
| Amphotericin + Flucytosine interaction |
|
Definition
Amphotericin makes pores
Flucytosine enters thru pores |
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Term
|
Definition
| cardiomyopathy (from O2 radicals) |
|
|
Term
| Cyclophosphamide toxicity + solution |
|
Definition
| Hemorrhagic cystitis - urine appears pink Solution - take with Mesna |
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|
Term
| Bleomycin / Busulfan toxicity |
|
Definition
Pulmonary fibrosis (drug accumulates in lung)
Symptoms: dyspnea, non-productive cough |
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|
Term
|
Definition
|
|
Term
|
Definition
Peripheral neuropathy
Symptoms: tingling of hands/feet
Solution: give vinblastine |
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|
Term
|
Definition
Cerebral dysfunction
Symptoms: ataxia, poor coordination, confusion, seizure, coma |
|
|
Term
| Synthetic nitrosoureas uses & toxicity |
|
Definition
Tx of Brain tumors
Toxicity: myelosuppression |
|
|
Term
| Streptozotocin uses & toxicity |
|
Definition
Used for pancreatic islet cell carcinoma
Toxicity: diabetogenic - kills beta cells |
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Term
|
Definition
Treat breast cancer in postmenopausal women
Blocks estrone synthesis in adipose tissue |
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Term
| Prostate cancer hormonal therapy |
|
Definition
LHRH agonist (leuporide, goserelin)
Diethylstilbestrol
Flutamide (anti-androgen) |
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|
Term
LHRH agonist mechanism
(Leuprolide, Goserelin) |
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Definition
| Synthetic LHRH -> pituitary constantly secreting LH -> continuous stimulation of receptors at testis (or ovary) -> desensitization & internatlization of receptors -> decrease testosterone (or estradiol) |
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Term
|
Definition
- For prostate cancer
- Use in combo w LHRH
- -> hydroxyflutamine -> Competitive inhibitor of testosterone receptor
- Consequence = testosterone can't act as negative feedback at hypothalamus/pituitary -> produces more LH / testosterone (opposite of what you want, so use in combo w LHRH agonist)
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Term
| Methotrexate toxicity + solution |
|
Definition
| High dose methotrexate (given due to decreased dihydrofolate reductase affinity mutation) -> give leucovorin to protect regular cells |
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Term
|
Definition
cyst ingested -> trophozoites form & can cross lumen into tissues. cysts remain in lumen -> excreted -> infect others
- Metronidazole: DNA damage to parasite; oxygen inhibits this
- Tissue amebicide + partial lumen (use w other lumen amebicide - like paramomycin - ok in pregnant women bc not absorbed at all)
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