quick drugs hankk Flashcards
rapid acting insulin
Lispro, aspart, and glulisine.
long acting insulin
detemir and glargine
Biguanides (metformin)
increases insulin sensitivity lactic acidosis (contraindicated in renal insufficiency)
sulfonyl ureas
1st gen- chlorpropamide, tolbutamide
2nd gen- glimepiride glyburide and glipizide
glipizide associated with hepatotoxicity and glimepiride and glyburide with hypoglyceia because of long action
MOA: closes K+ channel in beta cell leading cell depolarization and insulin release.
first generation disulfuram like effects
weight gain and hypoglycemia
Glitazones/TZDs
pioglitzone rosiglitazone
increases insulin sensitivoty. binds to PPAR-gamma nuclear transcription regulator.
AE: weight gain, edema, hepatotoxicity, heart failure and increases risk of fracture.
meglitinides
nateglinide, repaglinide.
bind to K+ channel in beta cell increasing insulin release.
AE: hypoglycemia and weight gain.
GLP-1 analogs
exenatide liraglutide.
AE: pancreatitis, modest weight loss
DPP-4 inhibitors
linagliptin, saxagliptin, sitagliptin
AE: mild urinary or respiratory infections.
amylin analogs
pramlinitide.
MOA: decrease gastric emptying and decrease glucagon.
hypoglycemia and nausea.
SGLT-2 inhibitors
canagliflozin, dapagliflozin, and empagliflozin.
block reabsorption of glucose in PCT.
AE: glucosuria, UTIs, vaginal yeast infections, hyperkalemia, dehydration.
alpha glusidase inhibitors
acarbose, miglitol
inhibit intestinal brush border alpha glucosidases.
propylthiouracil (thionamides)
block thyoid peroxidase, inhibiting oxidation of iodide and organification of iodine. (methimazole also).
PTU also inhibits 5’-deiodinase decreasing peripheral conversion of T4 to T3.
demeocycline
ADH antogonist.
member of tetracycline family.
fludricortisone
synthetic analog of aldosterone
AE: worsens HF and leads to hyperpigmentation.
H2 blockers
cimentidine, ranitidine, famotidine, nizatidine.
reversible block of H2 receptor.
cimentidine is also a potent blocker of the CYP450 system. also has antoandrogenic effects(prolactin release), gynecomastia, impotence, decreased libido.
both ranitidine and cimentidine decrease renal excretion of creatinine.
PPIs
irreversibly inhibit H+/K+ ATPase.
AE: increase risk of C diff infection, pneumonia, decreases serum Mg2+ with long term use, osteoporotic hip fractures
aluminum hydroxide
constipation, hyperphosphatemia, prox muscle weakness, osteodystrophy, and seizures.
magnesium hydroxide.
diarrhea, hyporeflexia, hypotension, cardiac arrest.
ondansetron
5-HT3 antagonist.
post op patients and chemo patients.
AE: headache, constipation and QT interval prolongation
memantine
NMDA receptor antagonist (helps prevent exitotoxicity)
used in alzheimer disease
Sumitriptan.
5HT 1B/1D agonist. inhibit trigeminal nerve activation. prevent vasoactive peptide release; induce vasoconstriction
AE: coronary vasospasm (contraindicated in patients with CAD or prinzmetal angina); mild paresthesia.
antipsychotics
Haloperidol, trifluoperazine, thioridazine, chlorpromazine
block D2 receptors.
high potency: trifluoperazine, fluphenazine, and haloperidol
low potency: chlopromazine thioridazine.
atypical antipsychotics
aripripazole, asenapine, clozapine, iloperidone, lurasidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone
AE: all cause prolonged QT interval
pines-metabolic syndrome, clozapine agranulocytosis,
risperidone-hyperprolactinemia.
SSRIs
fluoxetine, paroxetine, setraline, citalopram.
SNRIs
venlafaxine, desvenlafaxine, duloxetine, levomilnacipran, milnacipran.
AE: increase BP.
treatment of serotonin syndrome.
cyproheptadine.
Tricyclic antidepressants.
amitryptiline, nortriptiline, imipramine, desipramine, clomipramine, doxepin, amoxapine.
Tri C’s- coma convulsions and cardiotoxicity (arrhythmia due to Na+ channel inhibition.
NaHCO3 can prevent arrhythmia in overdose.
monoamine oxidase inhibitors
tranylcypromine, phenylzine, isocarboxazid, selegiline.
bethanechol
activates bowel and bladder smooth muscle. resistant to ACHE
postop ileus, neurogenic ileus and urinary retention
carbachol
constricts pupil and relieves intraocular pressure in open angle glaucoma.
pilocarpine
potent stimulator of sweat, tears and saliva
used in open and closed angle glaucoma and xerostomia (sjogren syndrome)
neostigmine
increases Ach
postop and neurogenic ileus, urinary retention, myasthenia gravis and reversal of neuromuscular junction blockade
physostigmine
increases Ach
phyxes atropine overdose
used in anticholinergic toxicity, crosses BBB
pyridostigmine
increases Ach
myasthenia gravis; does not penetrate CNS.
glycopyrolate
muscarinic antagonist GI and respiratory
parenteral: preoperative to reduce airway secretions
oral: drooling, peptic ulcer.
hyoscyamine, dicyclomine
GI
antispasmotics for IBS
reduce bladder spasms and urge urinary incontinence
oxybutynin, solifenacin and tolterodine.
fenoldopam
D1
post op HTN, hyper tensive crisis. promotes natriuresis. can cause hypotension and tachycardia.
midodrine
autonomic insufficiency and postural hypotension. may exacerbate supine HTN.
cephalosporins
1st gen. cefazolin, cephalexin
2nd gen. cefaclor, cefoxitin, cefuroxime
3rd gen. ceftriaxone, cefotaxime,
cefpodoxime, ceftazidime ( for psuedomonas)
4th gen cefepime
5th gen ceftaroline (does not cover psuedomonas but does cover MRSA)
MECHANISM OF RESISTANCE Structural change in penicillin-binding proteins
(transpeptidases).
carbapenams
Imipenem, meropenem, ertapenem, doripenem.
Imipenem is a broad-spectrum, β-lactamase–
resistant carbapenem. Always administered
with cilastatin (inhibitor of renal
dehydropeptidase I) to decrease inactivation of drug
in renal tubules.
imipenam is associated with seizures
Monobactams (Aztreonam)
Less susceptible to β-lactamases. Prevents peptidoglycan cross-linking by binding to penicillinbinding
protein 3. Synergistic with aminoglycosides. No cross-allergenicity with penicillins.
only works against gram - rods. not effective against anaerobes
aminoglycosides
Bactericidal; irreversible inhibition of initiation
complex through binding of the 30S subunit.
Can cause misreading of mRNA. Also block
translocation. Require O2 for uptake; therefore
ineffective against anaerobes.
AE: Nephrotoxicity, Neuromuscular blockade,
Ototoxicity (especially when used with loop
diuretics). Teratogen.
MECHANISM OF RESISTANCE Bacterial transferase enzymes inactivate the
drug by acetylation, phosphorylation, or
adenylation
tetracycline
Bacteriostatic; bind to 30S and prevent attachment of aminoacyl-tRNA; limited CNS penetration.
Doxycycline is fecally eliminated and can be used in patients with renal failure. Do not take
tetracyclines with milk (Ca2+), antacids (Ca2+ or Mg2+), or iron-containing preparations because
divalent cations inhibit drugs’ absorption in the gut.
AE:Bacteriostatic; bind to 30S and prevent attachment of aminoacyl-tRNA; limited CNS penetration.
Doxycycline is fecally eliminated and can be used in patients with renal failure. Do not take
tetracyclines with milk (Ca2+), antacids (Ca2+ or Mg2+), or iron-containing preparations because
divalent cations inhibit drugs’ absorption in the gut.
decreased uptake or increased efflux out of bacterial cells by plasmid-encoded transport pumps.
Chloramphenicol
Blocks peptidyltransferase at 50S ribosomal subunit. Bacteriostatic.
AE: Anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome (in premature
infants because they lack liver UDP-glucuronyltransferase).
MECHANISM OF RESISTANCE Plasmid-encoded acetyltransferase inactivates the drug.
Oxazolidinones (Linezolid)
Inhibit protein synthesis by binding to 50S subunit and preventing formation of the initiation
complex.
AE: Bone marrow suppression (especially thrombocytopenia), peripheral neuropathy, serotonin
syndrome.
MECHANISM OF RESISTANCE Point mutation of ribosomal RNA.
Macrolides
Azithromycin, clarithromycin, erythromycin.
Inhibit protein synthesis by blocking translocation (“macroslides”); bind to the 23S rRNA of the
50S ribosomal subunit. Bacteriostatic.
AE: MACRO: Gastrointestinal Motility issues, Arrhythmia caused by prolonged QT interval, acute
Cholestatic hepatitis, Rash, eOsinophilia. Increases serum concentration of theophylline, oral
anticoagulants. Clarithromycin and erythromycin inhibit cytochrome P-450.
MECHANISM OF RESISTANCE Methylation of 23S rRNA-binding site prevents binding of drug.
Sulfamethoxazole (SMX), sulfisoxazole,
sulfadiazine.
Inhibit dihydropteroate synthase, thus inhibiting
folate synthesis. Bacteriostatic (bactericidal
when combined with trimethoprim).
AE: Hypersensitivity reactions, hemolysis if G6PD
deficient, nephrotoxicity (tubulointerstitial
nephritis), photosensitivity, Stevens-Johnson
syndrome, kernicterus in infants, displace
other drugs from albumin (eg, warfarin
resistance: Altered enzyme (bacterial dihydropteroate
synthase), uptake, or PABA synthesis.
Fluoroquinolones
Inhibit prokaryotic enzymes topoisomerase
II (DNA gyrase) and topoisomerase IV.
Bactericidal. Must not be taken with antacids.
AE: GI upset, superinfections, skin rashes, headache,
dizziness. Less commonly, can cause leg
cramps and myalgias. Contraindicated in
pregnant women, nursing mothers, and
children < 18 years old due to possible damage
to cartilage. Some may prolong QT interval.
May cause tendonitis or tendon rupture in
people > 60 years old and in patients taking
prednisone. Ciprofloxacin inhibits cytochrome
P-450.
MECHANISM OF RESISTANCE Chromosome-encoded mutation in DNA
gyrase, plasmid-mediated resistance, efflux
pumps.
Daptomycin
Lipopeptide that disrupts cell membranes of
gram ⊕ cocci by creating transmembrane
channels.
ADVERSE EFFECTS Myopathy, rhabdomyolysis.
selective arterial dilators
minoxidil and hydralazine
result in sodium and fluid retention because of the reflex tachycardia which is provided by the sympathetic nervous which also causes renin release
side affects of mannitol
Pulmonary edema, dehydration. Contraindicated in anuria, HF.
Ethacrynic acid
Nonsulfonamide inhibitor of cotransport system
(Na+/K+/2Cl−) of thick ascending limb of loop
of Henle.
more ototoxic than furosemide
thiazide dirutics adverse effects
Hypokalemic metabolic alkalosis,
hyponatremia, hyperGlycemia,
hyperLipidemia, hyperUricemia,
hyperCalcemia. Sulfa allergy.
Hydrochlorothiazide, chlorthalidone,
metolazone.
Potassium-sparing diuretics
Spironolactone and eplerenone; Triamterene,
and Amiloride
Spironolactone and eplerenone are competitive
aldosterone receptor antagonists in cortical
collecting tubule. Triamterene and amiloride
act at the same part of the tubule by blocking
Na+ channels in the cortical collecting tubule.
Aliskiren
Direct renin inhibitor, blocks conversion of angiotensinogen to angiotensin I.
