Drugs Flashcards
Finasteride MOA
5-alpha reductase inhibitor
Use for BPH
Tx of BPH:
Initial: alpha antag (terazosin, tamsulosin) relax sm mm in bladder neck/prostatic urethra
5 alpha reductase inhib (finasteride, dutasteride) to reduce large prostate volumes
Flutamide
Nonsteroidal competitive testosterone R antagonist
Use in prostate Ca
Cause pseudomembranous colitis:
aminopenicillins (ampicillin, amoxicillin), Clindamycin, cephalosporins
Tx: oral dose of vanco
First Gen Cephalosporins
Cephalexin, Cefazolin
Gram + cocci, PEK (Proteus, E. coli, Klebsiella pneumoniae)
Second Gen Cephalosporins (2A)
Cefaclor, Cefuroxime
Gram + cocci, HEN PEK (H. flu, Enterobacter, Neisseria)
Cephalosporins 2B
Cefotetan, Cefoxitin (Cephamycins)
Gram + cocci, HEN PEK, Anaerobes!!!
Third Gen Cephalosporins
Cefotaxime, Cefixime, Cefpodoxime, Ceftriaxone
Excellent Gram -, nosocomial G - infection resistant to other beta lactams
Ceftriaxone: Meningitis, gonorrhea
Unique 3rd Gen Cephalosporin
Ceftazadime
Less G +, good G -, Pseudomonas!
Fourth Gen Cephalosporin
Cefepime
Pseudomonas, G + great, G - great
Ceftaroline
broad G + and G -, MRSA
Atreonam
monobactam, binds PBP 3, resistant to beta lactamases
G - only, Pseudomonas
Use: penicillin allergy or renal unsuffic who can’t tol. aminoglycosides
Carbapenems
Doripenem, Imipenem, Meropenem, Ertapenem
Broad! G + cocci, G - rods, anaerobes
Ertapenem: no Acinetobacter, Pseudomonas, Enterococcus
Give Imipenem with Cilastatin - prevents inactivation in renal tubules
Carbapenem Side Effects
Seizures, GI, rash
Renal dose adjust
Vancomycin
inhibits peptidoglycan format. by binding D-ala D-ala
Gram + only! only resistant ones (MRSA, VRE)
Oral dose for C. dif
Resistance: D-ala D-lac modific
Vancomycin SEs
Red man syndrome (histamine mediated), Nephrotox, Ototox, Thrombophlebitis
Protein synth inhibitors that blocks A-site tRNA binding:
Tetracyclines (30S)
Protein synth inhibitors that block initiation complex formation:
Aminoglycosides (30S)
Also cause misreading of mRNA
Aminoglycosides SEs:
Nephrotoxic, Neuromuscular blockade, Ototoxic, Teratogen
Aminoglycoside names/uses:
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Aerobes only!! MOA requires 02
G +: synergy with BLs
Severe G - rod infections, Pseudomonas
Resistance: bacterial transferase enzymes add side chain
Tetracycline SEs:
N/V/D, bind to growing teeth/bones, photosensitivity, contraindic in preg, chelate with divalent cations
Tetracycline names/uses:
Tetracycline, Doxycycline, Minocycline
Borrelia burgdorferi, M. pneumonia, Rickettsia, Chlamydia
(Atypical pneumonia, tick bites, chlamydia)
Resistance: efflux pumps, plasmid-encoded
Macrolides
Azithromycin, Clarithromycin, Erythromycin
Block translocation, bind 23S rRNA of 50S ribosome
HELP SES Bugs
Aminopenicillins: Ampicillin, Amoxicillin (better oral) (ESBLs)
Haemophilus influenza, E. coli, L. monocytogenes, Proteus mirabalis, Salmonella, Enterococci, Shigella
Give with Clavulanic acid/sulbactam: BLase inhibitors
Phenoxybenzamine
Noncompetitive, irreversible alpha antagonist
To manage Pheo Sx preop
Phentolamine
competitive, reversible alpha antag
Give to tx HTN crisis when withdraw clonidine or eat tyramine containing foods on MAO-I
Prazosin
Alpha-1 selective antagonist
used to treat HTN, BPH urinary Sx, PTSD
Also Terazosin, doxazosin, tamsulosin (selective @ prostate’s alspha-1A Rs)
Mirtazapine
Selective alpha-2 antagonist
Used to treat depression, causes sedation
Cause gingival hyperplasia: (4)
Phenytoin, verapamil, cyclosporine, nifedipine
Cause Myopathy:
Fibrates, niacin, colchicine, hydroxychloroquine, IFN-alpha, penicillamine, statins, glucocorticoids
Cause SLE-like syndrome:
Sulfa drugs, hydralazine, INH, Procainamide, Phenytoin, Etanercept
Cause SIADH:
Carbamazepine, cyclophosphamide, SSRIs
Cause Pulmonary fibrosis
Bleomycin, Amiodarone, Busulfan, Methotrexate
Sulfa Drugs:
Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide ABs, Sulfasalazine, Sulfonylureas
PROfessional FACTSSS
May cause fever, UTI, SJS, hemolytic anemia, thrombocytopenia, agranulocyt, and urticaria in ppl w/ allergies
Insulin release mediated by:
Decreased by alpha-2
Increased by beta-2
Metronidazole Treats:
GET GAP on the Metro
Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes below belt (Bacteroides, C. dif), H. Pylori - triple ther with PPI and clarithromycin
ABs to avoid during pregnancy:
SAFe Children Take Really Good Care
Sulfonamides, Aminoglycosides, FQs, Clarithromycin, Tetracyclines, Ribavirin, Griseofulvin, Chloramphenicol
Opioid MOA
Open K channels, close Ca channels
Increase K efflux and Decrease Ca influx hyperpolarizes post syn neurons.
Inhibit release of ACh, NE, 5HT, glutamate, substance P
Ethosuximide
DOC for absence seizures
Blocks thalamic T-type Ca chan
SE: GI, rash, SJS, HA, fatigue
Benzos for Seizures
IV tx of status epilepticus (followed by IV Phenobarbital or fosphenytoin)
Also for eclampsia seizures (MgSO4 is DOC)
Diazepam/Lorazepam (longer DoA, preferred)
Increase GABAa action
Phenytoin
Tonic-clonic and status epilep prophylaxis: 1st line, also used in partial
Na channel inactivation, zero order kinetics
SE: nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, periph neuropathy, megaloblastic anemia, teratogen, SLE like sindrome, SJS, osteopenia
CYP inducer
Carbamazepine
partial, tonic clonic: 1st line
Increased Na chan inactivation
SE: diplopia, ataxia, blood dyscrasias, liver tox, teratogen, SIADH, SJS
CYP inducer
Also used for BPD and Trigeminal neuralgia
Valproic acid
Tonic clonic: 1st line, also used in absence, partial, myoclonic seizures
Na chan inactivation, Increased GABA conc by inhib GABA transaminase
GI, hepatotox-can be fatal-monitor LFTs, tremor, wt gain. CONTRAINDIC in preg-NTDs
Also used for BPD
Gabapentin
not 1st line, partial, tonic-clonic
Inhibits high-voltage-activated Ca chan
SE: sedation, ataxia
Also used for periph neuropathy, postherpetic neuralgia, migraine prophylaxis, BPD
First Line Partial seizures:
Carbamazepine*, oxcarbazepine, valproate, lamotrigine, phenytoin
First line generalized tonic clonic:
Carbamazepine, phenytoin, valproate, lamotrigine, oxcarbazepine
Phenobarbital
1st line in Neonates! Other uses: partial, tonic clonic
Increases GABAa
SE: sedation, tolerance, dependence, cardioresp depression
CYP Inducer
Topiramate
Blocks Na channels, increases GABA action
Partial, tonic clonic
Sedation, mental dulling, cidney stones, wt loss
also migraine prophylaxis
Lamotrigine
Partial, tonic clonic, absence
Blocks voltage-gated Na chan
SE: SJS
Also used for depressive phase of BPD
Levetiracetam
Partial, tonic-clonic
unknown MOA
Tigabine
partial
Increased GABA by inhibiting reuptake
Vigabatrin
partial
increases GABA by irreversibly inhibiting GABA transaminase
Tx of serotonin syndrome:
cyproheptadine (5HT2 R antag)
Which antiviral polymerase inhibitors do not require phosphorylation by cellular kinases?
Foscarnet (for CMV retinitis in AIDS or resistant HSV/VZV)
Cidofovir (preferentially inhib viral DNA pol, CMV in immunocomp, resistant HSV)
Tenofovir (only NRTI that doesn’t require phosphorylation)
all the NNRTIs (Efavirenz, Nevirapine, Delaviridine - bind RT)
Drugs that prolong QT:
Some Risky Meds Can Prolong QT:
Sotalol Risperidone Macrolides Chloroquine Protease Inhibitors (-navir) Quinidine Thiazides Ziprasidone
Meds that may cause seizures
Bupropion (antidepressant), clozapine (APD), Isoniazid (if given without pyridoxine), ciprofloxacin, imipenem
First Gen Antihistamines:
Diphenhydramine, dimenhydrinate, chlorpheniramine
H1 blockers
Uses: allergy, motion sickness, sleep aid
SEs: Anti-HAM
2nd gen antihistamines:
Loratadine, fenoxfenadine, desloratadine, cetirizine
Allergy
Less sedating
H2 blockers:
Cimetidine, ranitidine, famotidine, nizatidine
reversibly block H2 Rs to decrease H+ sec by parietal cells
Uses: peptic ulcer, gastritis, mild reflux
Cimetidine is Potent CYP INHIBITOR, also anti-androgenic effects, can cross BBB and placenta
Cimetidine and ranitidine decr renal creatinine excretion
PPIs
Omeprazole, lansoprazole, esomeprazole, pantoprazole, dexlansoprazole
Irrevers inhib H+/K+ ATPase in stomach parietal cells
Uses: peptic ulcer, gastritis, reflux, ZES
Cilostazol
PDE 3 Inhibitor, increases cAMP in platelets, inhibiting platelet agg, also vasodilates
Dipyridamole does same thing
Can use for claudication
Watch out, can cause coronary steal b/c vasodilate
Tx for methemoglobinemia:
IV methylene blue
helps reduce Fe3+ back to 2+
(can be caused by nitrates/sulfa drugs)
Tx of atrial flutter:
Conversion to sinus rhythm: class 1A, 1C, or 3
Rate control: beta block or Ca chan blocker
Tx for Diptheria:
DT antitoxin (passive immunity) GIVE FIRST
Penicillin/erythromycin
DPT vaccine
Listeria tx
ampicillin in infants/immunocomp/elderly
Actinomyces tx:
Penicillin
G+ anaerobe, branching filamentous oral flora
oral/facial abscesses that drain through sinus tracts
Tx for nocardia:
Sulfonamides
G + aerobe, filamentous branching, weak acid fast, in soil
Pulm infections in immunocomp and cutaneous infections after trauma
MAC prophylaxis
Azithromycin
disseminated non-TB dz in AIDS
grows at high temps
Mycobacterium leprae tx:
Lepromatous (Th2 response): Dapsone, rifampin, clofazimine for 2-5 years
Tuberculoid (Th1 response): Dapsone and rifampin 6 mo
Hydralazine
increases cGMP, vasodilates arterioles > veins
Reduces afterload
First line for HTN in pregnancy w/ methyldoa
SE: causes reflex tachycardia, can give with beta blocker
lupus-like syndrome, fluid retention, nausea, headache, angina
Hypertensive emergency tx:
nitroprusside, nicardipine, clevidipine, labetalol, fenoldopam
Nitroprusside: increases cGMP via direct release of NO, short acting
-SE: cyanide toxicity! releases cyanide, tx w/ sodium thiosulfate
Fenoldopam: D1 agonist - coronary, peripheral, renal, and splanchnic vasodilation –> decr BP and incr natriuresis
-improves renal perfusion
H. flu mucosal infection tx:
amox +/- clav
H. flu meningitis tx/prophylaxis:
Tx: ceftriaxone, rifampin prophylaxis in close contacts
Meningococcus treatment:
ceftriaxone or penicillin G
Prophylaxis: rifampin, cipro, or ceftriaxone in close contacts
Legionella treatment
macrolide or quinolone
Pseudomonas tx:
Aminoglycoside plus ESBL (piperacillin, ticarcillin, cefepime, imipenem, meropenem)
Lyme dz tx:
doxycycline, ceftriaxone
Rickettsial dz tx:
Doxycycline
Mycoplasma pneumoniae tx:
macrolide, doxy, or FQ
cardioselective beta blockers
atenolol, acebutolol, betaxolol, esmolol, metoprolol
beta blockers for MI:
metoprolol, carvedilol, bisoprolol - decrease mortality
Partial beta agonists:
Pindolol, Acebutolol