MOA pharm Flashcards
Digoxin
direct inhibition of Na/K ATPase
- > indirect inhibition of Na/Ca exchanger/ antiporter
- > increased Ca and contractility
Sucrafate
Binds to ulcer base providing PHYSICAL barrier, allowing HCO3 secretion to reestablish
- Bismuth also in this class
Misoprostol
PGE1 analog,
increases production of gastric mucous barrier and decreases acid production
Also used in : cervical ripening/labor inducing, maintaining PDA
Alteplase
tPA
directly aid in conversion of plasminogen to plasmin
->plasmin cleaves thrombin and fibrin clots
Also: reteplase and tenecteplase
Chloroquine
1st line antimalarial unless resistant
Methfloquine
2nd line antimalaria
Primaquine
Added to antimalrial treatment if Vivax or Ovale is suspected
Tx - hypnozoite
Atovaquone
Antimalarial for those allergic to chloroquine, often given w/ primaquine
Also for babesia
Clavulanic Acid/Clavulanate
beta lactamase inhibitor
given w/ amoxicillin or ticacillin
Sulbactam
beta lactamase inhibitor
given w/ ampicillin
Tazobactum
beta lactamse inhibitor
given w/ piperacillin
Lidocaine
blocks preferentially active voltage gated Na channels on the inner side of the channel -> local anesthetic
Amide
penetrated membrane uncharged then binds in charged form - problem w/ infected acidic tissue
may be given w/ vasoconstrictor to potentiate action
Mepivacaine
Amide
Na channel blocker -> local anesthetic
~lidocaine
bupivacaine
Amide
Na channel Blocker -> local anesthetic
Procaine
Ester
Na Channel Blocker -> local anesthetic
Tetracaine
Ester
Na Channel Blocker ->local anesthetic
Cimetidine
Reversible H2 blocker -> lower H secretion from parietal cell
Peptic Ulcer, Gastritis, mild refflux
Also: -‘dines
Ranitidine
Famotidine
Nizatidine
D penicillamine
Chelates copper - wilson’s disease
Terazosin
alpha 1 antagonist
- for BPH and HTN
Tamsulosin
selective alpha 1 antagonist
- BPH alone
vs. Terazosin - nonselective
Vinblastine
alkaloid that binds to tubulin in M phase
Blocks polymerization of microtubules so mitotic spindles cannot form
Vincristine
alkaloid that bind to tubulin in M phase,
Blocks polymerization of microtubules so mitotic spindle cannot form
Paclitaxel
hyper stabilizes polymerized microtubules so mitotic spindle cannot break down
5 fluororuacil
Pyrimidine analog that complexes w/ folic acid
Inhibits thymidate synthase -> less dTMP ad less DNA
SE: myelosuppression and photosynth
Methotrexate
Folic acid analog
Inhibits dihydrofolate reductase -> less dTMP -> less DNA and protein synth
SE: myelosuppression, macrovescular FA liver disease, teratogenic
Azathioprine
Purine analog ->less de novo purine Synth
Activated HGPRT
toxicity w/ allopurinol due to metabolization w/ xanthine oxidase
6 mercaptopurine
Purine analog -> less de novo purine Synth
Activated by HGPRT
toxicity w/ Allopurinol due to metabolization w/ xanthine oxidase
6 thioguanine
Purine analog -> less de novo Purine synth
Activated by HGPRT
toxicity w/ Allopurinol due to metabolization w/ xanthine oxidase
Cytarabine
Pyrimidine analog
inhibits DNA polymerase
SE: Thrombocytopenia, megaloblastic anemia
Sumatriptan
5 HT 1D/1B agonists inducing vasoconstriction
used in migraine w or w/out aura
Odansetron
5HT 3 block for antiemetic function
Trazadone
inhibits serotonin reuptake
Maprotiline
Blocks NE Reuptake
Mirtazapine
alpha 2 antagonist -> increase NE and serotonin
Buproprion
increases NE and dopamine via unknown mech
Bromocriptine
dopamine agonists (prolactinoma)
Parkinsons
ergot - vasoconstrictor
Cabergoline
dopamine agonist (Prolactinoma)
octreotide
Somatostatin analog - GH cell adenoma
Demeclocycline
Ab used to induce impaired renal response to ADH
Used for SIADH
Propylthiouracil
Blocks peroxidase in hyperthyroidism
Also blocks peripheral conversion of T4 to active T3
phenoxybenzamine
irreversible alpha blocker
prior to surgical removal of pheo
Docusate
aniionic surfactant - reduces surface tension allowing water and lipid to penetrate the stool
Clopidogrel
inhibit platelet aggregation by irreversible blocking ADP receptors.
Inhibit fibrinogen receptor binding by preventing glycoprotein IIb/IIIa from binding to fibrinogen
also: ticlopidine, ticagrelor, parasugrel
Ticlopidine
inhibit platelet aggregation by irreversible blocking ADP receptors.
Inhibit fibrinogen receptor binding by preventing glycoprotein IIb/IIIa from binding to fibrinogen
- Worry about neutropenia
Dimercarpol
chelator for arsenic, mercury and Pb
EDTA
Effective chelator of divalent and trivalent cations -> Na CaEDTA to avoid hypocalcemia
binds to mercury and lead
Cyclosporin
Binds to cyclophilins -> blocking of differentiation and activation of T cells by inhibiting calcineuron, preventing the production go IL2
Nephrotoxic, HTN, hyperlipidemia, gingival hyperplasia, hirsutism
Tacrolimus
binds to FK binding proteins -> inhibiting calcineurn and secretion of Il2
Nephrotoxic and HTN
NO gingival hyperplasia vs cyclosporin
Sirolimus
Binds to FKBP12 -> inhibits mTor, inhibits T cell proliferation in RESPONSE to IL2
(vs production in Tacrolimus and Cyclosporin)
NO nephrotoxicity
Azathioprine
antimetabolite precursor of 6 mercaptopurine
- interferes w/ metabolism and synthesis of nucleic acid (purine antimetabolite)
- toxic to lymphocytes
Bone marrow suppression, worry w/ allopurinol blocking metabolism and increased side effects
Muromonab CD3
Antcolonal antibody binding to CD3 of T cells - no signal transduction,, good for kidneys
Cytokine and hypersensitivity reaction
Phytonadione
Vitamin K analog - Warfarin overdose
Amphotericin B
Binds ergosterol - forming pores and allowing electrolyte leakage
-serious systemic mycoses
Nystatin
Binds ergosterol - forming pores and allowing electrolyte leakage
Topical though due to toxic systemic use- thrush and diaper rash/vaginal cndidiasis
fluconazole
inhibit fungal sterol (ergosterol synthesisi) by inhibiting P450 enzyme that converts lanosterol to ergosterol
Also Ketoconazole, clotimazole, miconazole, itraconazole, voriconazole
- gyenectomastia seen - inhibits 1st step desmolase in making testosterone
Flucytosine
Inhibits DNA nadn RNA biosynth by converting to 5 flurouracil by cytosine deaminase
- Systemic fungal infections- meningitis -> cryptococcus
- wary of bone marrow suppression (HIV)
Caspofungin
inhibits cell wall synth by inhibiting synthesis of beta glucan
- micafungin as well
- Invasive aspergillosis and Candida
Terbinafine
inhibits fungal enzyme squalene epoxidase
Rx for dematophytes
Griseofulvin
Interferes w/ microtubule function
Oral Rx for superficial infection - dematophytes
thiazolininediones
pioglitazone and rosiglitazone
increases insulin sensitivity in peripheral tissue by binding to PPAR-gamma nuclear transcription factor
-lowers serum glucose and lowers tryglycerides and C reactive protein levels and increases HDL
pioglitazone
increases insulin sensitivity in peripheral tissue by binding to PPAR-gamma nuclear transcription factor
-lowers serum glucose and lowers tryglycerides and C reactive protein levels and increases HDL
rosiglitazone
increases insulin sensitivity in peripheral tissue by binding to PPAR-gamma nuclear transcription factor
-lowers serum glucose and lowers tryglycerides and C reactive protein levels and increases HDL
flumazenil
competitive benzodiazapine antagonist
-blocking the action of GABA
Pralidoxime
acetylcolinesterase reactivater post organophosphorus actylecholinesterase activity
febuxostat
inhibits xanthine oxidase
cetirizine
2nd generation H1 blocker for allergy
less sedation, less anti muscarinic effects
-also loratadine and fexofenadine
demeclocycline
anti-ADH for SIADH Rx
lepirudin
inhibits thrombin, derivative of hirudin
Alternative to heparin for HIT
-bivalirudin as well
Bivalirudin
inhibits thrombin, derivative of hirudin
Alternative to heparin for HIT
-lepirudin as well
Atropine
competitive muscarinic antagonist
Bethanechol
cholinergic Agonist - postop illeus and urinary retention
Carbachol
cholinergic agonist - glaucoma
pilocarpine
cholinergic agonist - induce sweating, tears and saliva
methacholine
cholinergic agonist - asthma test
edrophonium
anti cholinesterase activity (short) - Dx myasthenia gravis
pyridiostigmine
Anticholinesterase activity (long) - Rx for myasthenia gravis
neostigmine
Anticholinesterase activity - neuromuscular blockade reverse (non depolarizing) and myasthenia gravis
physiostigmine
anti cholinesterase activity - Atropine antidote
donepezil
anticholinesterse activity - alzheimers
rivastigmine
anti cholinesterase activity - alzheimers
galantamine
anti cholinesterase activity - alzheimers
ecothiophate
anti cholinesterase activity - open angle glaucoma
homatropine
antimuscarinic- eye dialation
tropicamide
antimuscarinic - eye dialation
cyclopentolate
antimuscarinic - eye dialation
Benztropine
anti muscarinic
-Parkinsons disease has excess cholinergic activity and this blocks the rigidity and tremor somewhat, little w/ bradykinesia
CNS effects
Scopolamine
Anti muscarinic - motion sickness and decreased salivation (ICU)
ipratropium
Antimuscarinic - COPD/asthma
tiotropium
antimuscarinic - COPD/asthma
Oxybutynin
antimuscarinic - COPD/asthma
Toterodine
Antimuscarinic - urge incontinence
Darfenacin
Antimuscarinic - urge incontinence
also solifenacin
Trospium
antimuscarinic - urge incontinence
Epinephrine
alpha 1 and 2 and Beta 1 and 2 - anaphylaxis and hypotension; asthma maybe
norepinephrine
alpha 1 and 2 beta 1;
uses for hypotension - septic shock, worry about kidneys
Isoprotenerol
beta 1 and 2
no real clinical use - maybe torsades and bradycardias
Dopamine
alpha 1 and 2 at high does
beta 1 and 2 and med doses
dopamine 1 and 2 at low does
- dopamine receptors in the blood vessels and kidney
Dobutamine
beta 1 > beta 2
Used in heart failure
Chemical stress test
DoBETAm1ne
Phenylephrine
direct alpha 1 and 2
myodriatic
rhinitis - > vasoconstriction (nasal decongestant)
levabuterol
B2 > B1 - used in acute asthma, more selective for beta 2 than albuterol
salmeterol
B2 > B1 - used in long term asmtha
Terbutaline
B2>B1 - given sub Q and used as a tocolytic and asthma
Clonadine
alpha 2 agonist - lowers blood pressure, worry of rebound HTN
Amphetamine
releases stored NE (catecholamines)
- narcolepsy, obesity, ADHD
Ephedrine
releases stored NE (catecholamines)
-nasal decongestion, urinary incontence
Cocaine
blocks reuptake of NE - > vasoconstriction
- never give with Beta blockade
pindolol
weak beta 1 and agonists -> antagonist
acebutolol
weak beta 1 and agonists -> antagonist
esmolol
selective beta 1 blocker
atenolol
selective beta 1 blocker
metoprolol
selective beta 1 blocker
propranolol
nonselective beta blocker - NOT for COPD
timolol
nonselective beta blocker - glaucoma
nadolol
nonselective beta blocker - NOT for COPD
labetolol
alpha1 and beta 1 antagonist
carvediol
alpha1 and beta 1 antagonist
Clomipramine
TCA used in OCD
May also use an SSRI- fluoxetine
Riframpin MOA?
inhibits DNA dependent RNA polymerase
Used in TB, leprosy and meningococcal (H influenza B prophylaxis)
Orange body fluids - TB Rx and chemoprophylaxis for H influenza contact
Probenecid
inhibits uric acid absorption
Gout medication
Quinidine
Class 1a anti arrhythmic
- phase 0 of myocytes, blocking Na channels -> increased ERP
Procainamide
Class 1a anti arrhythmic
- phase 0 of myocytes, blocking Na channels -> increased ERP
Disopyramide
Class 1a anti arrhythmic
- phase 0 of myocytes, blocking Na channels -> increased ERP
Lidocaine
Class 1b anti arrhythmic
- phase 0 of myocytes, blocking Na channels -> increased ERP
Mexiletine
Class 1b anti arrhythmic
- phase 0 of myocytes, blocking Na channels -> increased ERP
tocainide
Class 1b anti arrhythmic
- phase 0 of myocytes, blocking Na channels -> increased ERP
Flecanide
class 1c anti arrhythmic phase 0 of myocytes, blocking Na channels -> increased ERP
Propafenone
class 1c anti arrhythmic - phase 0 of myocytes, blocking Na channels -> increased ERP
Amiodarone
class III anti arrhythmic -phase 3 of myocytes, blocking K channels increasing ERP
Ibutilide
Class III Antiarrythmic
-phase 3 of myocytes, blocking K channels increasing ERP
Dofetilide
Class III anti arrhythmic
-phase 3 of myocytes, blocking K channels increasing ERP
Sotalol
Class III antiarrythmic
-phase 3 of myocytes, blocking K channels increasing ERP
verapamil
Class IV Antiarrhythmic
-phase 0 of nodes, blocking Ca channels increasing ERP
preferentially acts on heart w/ diltiazem
Dilatiazem
Class IV anti arrhythmic
-phase 0 of nodes, blocking Ca channels increasing ERP
Adenosine
decreases K out of the cell -> hyper polarization and also decreases Ca channel opening at the nodes -> AV node block
Used for SVT
Entanercept
TNF alpha inhibitor - differs from monoclonal antibody in that it is and TNP alpha pseudo receptor and IgG Fc fusion protein
decoy receptor
Infliximab
TNF alpha inhibitor
monoclonal Ab
adalimumab
TNF alpha inhibitor
monoclonal antibody
Golimumab
TNF alpha inhibitor
monoclonal antibody
Certoluzumab
TNF alpha inhibitor
monoclonal antibody
Prodenacid
increases uric acid secretion by blocking reabsorption in the proximal tubule
colchicine
stabilizes tubulin and inhibits polymerization leading to inhibition of leukocyte chemotaxis in acute gout exacerbation
allopurinol
xanthine oxidase inhibitor
- chronic use only for gout
febuxostat
xanthine oxidase inhibitor
- chronic use only for gout
finasteride
blocks 5 alpha reductase converting testosterone to DHT
- BPH and male pattern baldness
flutamide
anti androgen receptor (competitive antagonist) used in prostate cancer
ketoconazole - endocrine
(antifungal) inhibits steroid synthesis vis blocking 17, desmolase -> less testosterone and less hirutism in polycystic kidney disease
sprinolactone -endocrine
inhibits steroid binding leading to decreased hirutism due to androgens in polycystic kidney disease
Cyclophosphamide
Covalently x linked DNA at Guanine N7
- requires bioactivation by liver
- hemorragic cystitis
sildenafil
inhibits phosphodiesterase 5 -> increase in cGMP - > smooth muscle relaxation -> vasodialtion
vardenafil
inhibits phosphodiesterase 5 -> increase in cGMP - > smooth muscle relaxation -> vasodialtion
tadafenil
inhibits phosphodiesterase 5 -> increase in cGMP - > smooth muscle relaxation -> vasodialtion
Leuprolide
GnRH agonist (early flare)
used for infertility - pulsitile
continuous: (chemical menopause) -> down regulates FSH and LH release
- prostate CA,
- precocious puberty,
- uterine fibroids
- endometriosus
Clomiphene
partial estrogen agonist in hypothalamus
- stimulates receptors but not enough to cause a negative feedback like normal estrogen -> increase of LH and FSH
induce pregnancy
Letrozole
aromatase inhibitor -> decreased peripheral androgen conversion
- postmenopausal ER positive breast CA
Anastrozole
aromatase inhibitor -> decreased peripheral androgen conversion
-postmenopausal ER positive breast CA
Amitriptyline
Block reuptake of NE and serotonin (biogenic amines)
-TCA
- Anticholinergic
- Sedation
Imipramine
Block reuptake of NE and serotonin (biogenic amines)
-TCA
- Anticholinergic
- Sedation
Desipramine
Block reuptake of NE and serotonin (biogenic amines)
-TCA
- Anticholinergic
- Sedation
Clomipramine
Block reuptake of NE and serotonin (biogenic amines)
-TCA
- Anticholinergic
- Sedation
doxepin
- Odd end of a TCA
Block reuptake of NE and serotonin (Biogenic amines)
-TCA - Anticholinergic
- Sedation
Nortriptyline
Block reuptake of NE and serotonin (biogenic amines)
-TCA
- Anticholinergic
- Sedation
lovastatin
statins in general
inhibit conversion of HMG Co A to mevalonate
also secondarily increases LDL receptors to the cell surface for cells to take in LDL and lowering levels (decreases LDL mainly)
- rhabdomyolysis and hepatotoxicity
- myalgia,
Niacin
inhibits lipolysis in adipose tissue
reduces VLDL secretion
Flushed face concerns w/ hypoglycemia and hyperuricemia
itchy
Cholestryramine
Prevents intestinal reabsorption of bile acids
-decreases LDL mainly
unique in that it binds to C dif toxin from other bile acid resins
colestipol, colesevelam
GI discomfort and gallstones
colestipol
Prevents intestinal reabsorption of bile acids
decreases LDL mainly
GI discomfort and gallstones
Cholestryamine, Colesevelam
colesevelam
Prevents intestinal reabsorption of bile acids
Decreases LDL mainly
GI discomfort and gallstones
Cholestryramine, colestipol
ezetimibe
prevent cholesterol reabsorption at the small intestine brush border
Decreases LDL
Rarely may have increased liver enzymes, 2nd line to a statin
Diarrhea
gemfibrozil
fibrate
Upregulates LPL to increase tryglyceride clearance
May have RUQ pain w/ gallstones
clofibrate
fibrate
Upregulates LPL to increase tryglyceride clearance,
-activate peroxisome proliferator activated receptor alpha (PPAR alpha)
May have RUQ pain w/ gallstones
Mifepristone
competitive inhibitor of progesterone -> abortion
heave bleeding and GI/ Nausea experienced
Sulfonamides(sulfamethoxazole)
works on the first step of folate synthesis acting as a PABA antimetabolite blocking dihydropteroate synthase
-bacterialstatic
gram +/- UTIs, GIs, PCP prophylaxis
Trimethoprim
works on the second step of folate synthesis by blocking dihydrofolate reductase (methotrexate also acts here in humans)
Rx- supplemental folinic acid - leucovorin rescue
UTIs, GIs use
worry of anemia
Ciprofloxacin
Floroquinolones
inhibit DNA gyrase (topoisomerase II) and topo IV
bactericidal
not to be taken antacids/supplements (Ca, Fe, Mg)
Gram - rods, UTIs and GI, including pseudomonas, tessera and some gram +
levofloxacin
Floroquinolones - 3rd gen
inhibit DNA gyrase (topoisomerase II) and topo IV
bactericidal
not to be taken antacids/supplements (Ca, Fe, Mg)
Gram - rods, UTIs and GI, including pseudomonas, tessera and some gram +
moxifloxacin
Floroquinolones - 4th gen
inhibit DNA gyrase (topoisomerase II) and topo IV
bactericidal
not to be taken antacids/supplements (Ca, Fe, Mg)
Gram - rods, UTIs and GI, including pseudomonas, tessera and some gram +
metronidazole
forms free radicals that damage bacterial DNA
GET GAP on the Metro Giardia Entamoeba Trichomona Gardenella Anaerobes h Pylori
didsulfiram reaction
Nitrofurantoin
bactericidal
reduced by bacterial proteins to reactive intermediates that inactivates bacterial ribosomes
Used for UTIs
Isoniazid
decreases synth of mycolic acids.
bacterial catalase (KatG) needed to convert INH to active metabolite
Give w/ pyridoxine (B6) to prevent neurotoxicity
- lupes
- hepatotoxicity
Pyridoxine
vitamin B6
prevent neurotoxicity w/ INH
Rifampin Rs (4)
RnA polymerase inhibitor
Revs up microsomal p450
(increase warfarin and be wary of birth control)
Red/orange body fluids
Rapid resistance if used alone
-minor hepatic toxicity
Pyrazinamide
TB medication that acts by inhibiting my colic acid production by blocking mycobacterial pyrazinamidase -> decreased FA synth
effective in acidic pH of phagolysosomes
worry of
- hyperuricemia*
- hepatotoxicity
Ethambutol
decreases carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase
Worry of
-red/green colorblindness - optic neuropathy
Aldesleukin
IL2 analog given to encourage T cells in fighting renal cell carcinoma and metastatic melanoma
Erythropoeitin
Given to encourage RBC production with Renal failure leading to anemia
Filgrastim
GM-CSF ~ IL3
recovery of Bone marrow
sargramostim
GM-CSF ~ IL3
recovery of bone marrow
alpha interferon (exogenous)
Ramp up antiviral set _> ribonuclease activation
given to fight off Hep A and C, kaposis, leukemiasm malignant melanoma, hairy cell leukemia and genital warts
gamma interferon (exogenous)
given for chronic granulomatous disease to stimulate macrophages deficient in NADPH oxidase
Oprelvekin
~IL11
Used for thrombocytopenia
Thrombopoietin
Used to thrombocytopenia
Daclizumab
Binds to CD25, the IL 2 receptors in activated T cells for immune suppression
Mycophenolate mofetil
immune suppressor that inhibits purine synthesis through blocking IMP dehydrogenase (inosinemonophosphate dehydrogenase)
-> decrease guanine synthesis
Increase of lymphoma risk, teratogen
Thalidomide
immune suppressor that is historically important as a teratogen (phocomelia- limb agenisis)
Also used in immune suppression: anti-angiogenic
MOA- affects TNF alpha
Abciximab
Glycoprotein IIb/IIIa monoclonal antibody that is anti platelet,
Used post anioplasty and prevent cardiac ischemia in unstable angina
trastuzumab
HER/erb 2 neu receptor blocker in over expressing positive breast cancer
Rituximab
CD 20 monoclonal antibody that attacks B cells in non-hodgkin’s lymphoma
Omalizumab
IgE monocolonal antibody that is used in severe asthma relief,
Expensive
Tetrabenazine
inhibits DA release
used in huntingtons
pramipexole
dopamine receptor agonist
- Parkinsons
~Ropinirole, bromocriptine
ropinirole
dopamine receptor agonist
- Parkinsons
~Pramipexole, bromocriptine
Amantadine
Increases DA release in Parkinsons
used to be an antiviral
Levoadopa
dopamine precursor (L-DOPA) that is converted to Dopamine after crossing the BBB by dopamine decarboxylase
Given w/ carbidopa
Has tolerance- where it wears off and akinesia sets in
Carbidopa
simemet -blocks peripheral conversion of L Dopa to Dopamine minimizing SE of HTN, arrhythmia, hallucinations, psychosis
Given w/ levodopa
Selegiline
selective MAO typeB inhibitor blocking the breakdown of dopamine in Parkinsons
Entacapone
COMT inhibitor preventing L dopa degradation increasing availability of DA
~tolcapone
tolcapone
COMT inhibitor preventing L dopa degradation increasing availability of DA
~entacapone
riluzole
decreases presynaptic glutamate release in ALS
Memantine
NMDA receptor antagonist -> decreased levels of excitotoxity
-Glutamate receptor
Helps with alzheimers
Ondansetron
5HT3 antagonist used to block nausea post chemo, pregnant and post op
Omeprazole
Irreversible binds to the K/H ATPase in the stomach blocking H production
Used for Peptic ulcers, gastritis, Zollinger ellison, GERD
Bismuth
binds to ulcer base providing a physical barrier allowing the HCO3 secretion to reestablish pH gradient
Promotes healing
Misoprostol
PgE1 analog that is used in increased production of HCO3 and decreased gastric acid secretion
also increases uterine tone -> abortifant
Aluminum hydroxide
Antiacid that leads to constipation and hypokalemia and hypophosphatemia
Magnesium hydroxide
Antiacid that leads to diarrhea and hypokalemia
magnesium relaxes smooth muscles in general body wide
Calcium carbonate
Antiacid that leads to hypercalcemia (rebound acid secretion) and hypokalemia
Metoclopramide
Decreases D2 stim as an antagonists and stimulates 5HT4
Helps w/ gastroparesis - post surgical or diabetic
Mesalamine
5 ASA - activated in the colon by bacterial cleavage
Sulfasalazine
5 ASA - activated in the colon by bacterial cleavage
Ursodiol
natural bile acid that decreases synthesis of cholesterol in the liver and changes the composition of bile in the gallbladder
Delays progression in primary biliary cirrosis
bosentan
decreases pulmonary hypertension by competitively antagonizing endothelian receptor type 1
ambriesentan
decreases pulmonary hypertension by competitively antagonizing endothelian receptor type 1
etoposide
inhibits topo II -> increase in DNA degradation
teniposide
inhibitys topo II -> increase DNA degradation
Cisplatin
cross links DNA
Toxicity -> nephrotoxic, acuoustic nerve damage -amifostine prevents
carboplatin
cross links DNA
Toxicity -> nephrotoxic, acoustic nerve damage
-amifostine prevents
levabuterol
beta 2 agonists for acute Asthma attack
- less beta 1 spill than albuterol
Theophylline
inhibits phosphodiesterase thereby decreasing cAMP hydrolysis and causing bronchodialation
narrow TI -> cardiotoxic, neurotoxic, metabolized by p 450
Ipatropium
blocks M3 muscarinic receptor leading to bronchodialation - More for COPD
blocks vagal stimuation in general -> smooth muscle dialalation
Tiatropium
blocks M3 muscarinic receptor leading to bronchodialation - more for COPD
blocks vagal stimuation in general -> smooth muscle dialalation
fluticasone
inhaled steroid that blocks production of cytokines and TNF alpha by inactivating NF kappaB (transcription factor)
Used for chronic prophylactic asthma management
beclomethazone, budesinode
Beclomethasone
inhaled steroid that blocks production of cytokines and TNF alpha by inactivating NF kappaB (transcription factor)
Used for chronic prophylactic asthma management
-budesinode, fluticasone
budesinode
inhaled steroid that blocks production of cytokines and TNF alpha by inactivating NF kappaB (transcription factor)
Used for chronic prophylactic asthma management
-beclomethazone, fluticasone
Montelukast
blocks leukotriene receptors -> asthma, especially w/ allergic rhinits
zafirlukast
blocks leukotriene receptors-> asthma, especially w/ allergic rhinits
Zileuton
5 lipoxygenase pathway inhibitor blocking the formation leukotirenes
Cromolyn
blocks the mast cell release of mediators. Used prophylactically for asthma
- not to common anymore
Guaifenesin
expectorant - thins respiratory secretions
n acetylcystine(3)
acetaminophen overdose
expectorant - especially w/ mucous plugs in CF patients
Prophylactic protection of kidney function from contrast
diphenhydramine
H1 antagonist - 1st gen
- used for allergy motion sickness and sleep aid
- be wary of: sedation(enters CNS), antimuscarinic, and anti alpha adrenergic
demenhydrinate
H1 antagonist - 1st gen
- used for allergy motion sickness and sleep aid
- be wary of: sedation(enters CNS), antimuscarinic, and anti alpha adrenergic
chlorpheniramine
H1 antagonist - 1st gen
- used for allergy motion sickness and sleep aid
- be wary of: sedation(enters CNS), antimuscarinic, and anti alpha adrenergic
loratidine
H1 antagonist - 2nd gen
Used for allergy, less sedating
fexofenazine
H1 antagonist - 2nd gen
Used for allergy, less sedating
cetirizine
H1 antagonist - 2nd gen
Used for allergy, less sedating
desloratidine
H1 antagonist - 2nd gen
Used for allergy, less sedating
hydroxizine
H1 antagonist - 1st gen
- used for allergy motion sickness and sleep aid
- be wary of: VERY sedating (enters CNS),
antimuscarinic, and anti alpha adrenergic
meclizine
Antihistamine used for vertigo
Promethazine
antihistamine used for N/V
cyproheptadine
antihistamine used as an appetite stimulant
Dextromethorphan
derivative of morphine that antagonizes the NMDA glutamate receptor
used as a cough suppressant
mas mild opiod effect in excess
Pseudophederine
sympathomimetic alpha agonist used in nonprescription nasal decongestants
constricts dilated arterioles -> decreased airway resistance
- some CNS stimulation and anxiety
- phenylephrine is another
Minoxidil
opens K channels and hyper polarizes smooth muscles -> relaxation of vascular smooth muscle
(Ca channels stay closed, less contraction)
Used in HTN and topical hair loss (hypertichosis is S Fx)
Nifedipine
blocks voltage dependent L type Ca channels of smooth muscle and thereby reduce muscle contractility preventing formation of Ca Calmodulin complex
-> HTN
Also amlodipine
Hydralazine
increases cGMP directly -> increase myosin phosphatase activity and less myosin phophorylated -> smooth muscle relaxation
reduces after load by preferentially dilating arterioles
Co -administered w/ beta blocker frequently to prevent reflex tachy
Nitroprusside
short acting increases cGMP via direct release of NO (activates guanylyl cyclase); leads to increased myosin phosphatase activity
Risk of cyanide poisoning
Used for malignant HTN
Captopril
ACE inhibitor
inhibits angiotension II formation
- > decreased vasoconstriction
- > decreased aldosterone (less Na and fluid retention)
used for HTN and CHF and diabetic renal disease
Concern w. cough, andioedema, teratogen, creatine increase and hyperkalemia
enalapril
ACE inhibitor
inhibits angiotension II formation
- > decreased vasoconstriction
- > decreased aldosterone (less Na and fluid retention)
used for HTN and CHF and diabetic renal disease
Concern w. cough, andioedema, teratogen, creatine increase and hyperkalemia
Losartan
ARB
blocks angitenision II effect on its receptor leading to less aldosterone and decreased vasoconstriction
- used in HTN and CHF and post mI and diabetic renal disease
No Cough Sideeffect
Still have angioedema and teratogen,
Aliskern
renin inhibitor
- used for HTN, old drug
Causes hyperkalemia and renalinsufficency,
NOT for pregnancy, CHF, MI
Omega 3 FA
decreases tryglycerides
morphine
acts as an agonist at opiod receptors (mu, delta and kappa) - G protein linked
opens K channels and closes Ca channels -> decrease synaptic transmission through hyper polarization
inhibiting the release of ACh, NE, 5-HT and glutamate and substance P
fentanyl
acts as an agonist at opiod receptors (mu, delta and kappa) - G protein linked
opens K channels and closes Ca channels -> decrease synaptic transmission through hyper polarization
inhibiting the release of ACh, NE, 5-HT and glutamate and substance P
heroin
acts as an agonist at opiod receptors (mu, delta and kappa) - G protein linked
opens K channels and closes Ca channels -> decrease synaptic transmission through hyper polarization
inhibiting the release of ACh, NE, 5-HT and glutamate and substance P
Methadone
acts as an agonist at opiod receptors (mu, delta and kappa) - G protein linked
opens K channels and closes Ca channels -> decrease synaptic transmission through hyper polarization
inhibiting the release of ACh, NE, 5-HT and glutamate and substance P
meperidine
acts as an agonist at opiod receptors (mu, delta and kappa) - G protein linked
opens K channels and closes Ca channels -> decrease synaptic transmission through hyper polarization
inhibiting the release of ACh, NE, 5-HT and glutamate and substance P
Penicillin G - 3 MOA
IV - bactericidal
binds penicillin binding proteins preventing wall formation
binds to transpeptidase preventing cross linking
Increase autolytic enzymes
syphilis
Penicillin V - 3 MOA
Oral - bactericidal
binds penicillin binding proteins preventing wall formation
binds to transpeptidase preventing cross linking
Increase autolytic enzymes
Oxacillin
narrow spectrum
w/ naficillin, dicloxacilin
penicillinase resistant blocking degradtion
Used for MSSA; not MRSA
naficillin
narrow spectrum
w/ oxacillin, dicloxacilin
penicillinase resistant blocking degradtion
Used for MSSA; not MRSA
dicloxacilin
narrow spectrum - same 3 MOA as penicillin
w/ naficillin, oxacillin
penicillinase resistant blocking degradtion
Used for MSSA; not MRSA
Ampicillin
IV mainly
same 3 MOA of penicillin but wider spec
Gram +
HELPSS Haemophilus E Coli Listeria Proteus mirabilis Salmonella Shigella
ampicillin rash w/ EBV
-neonatal infect/ URI/UTI
Amoxicillin
Oral - given w/ clavulanic acid
same 3 MOA of penicillin but wider spec
Gram +
HELPSS Haemophilus E Coli Listeria Proteus mirabilis Salmonella Shigella
ampicillin rash w/ EBV
-neonatal infect/ URI/UTI
Ticarcillin
antipseuedomonal penicillin
piperacillin
antipseuedomonal penicillin
carbenicillin
antipseuedomonal penicillin
Clavulanic acide
beta lactamase inhibitor
given w/ amoxicillin and ticarcillin
Sulbactam
beta lactamase inhibitor
given w/ ampicillin
Tazobactam
beta lactamase inhibitor
given w/ piperacillin
cefazolin
1st gen cephalosporin
gram + and PEcK
Proteus mirabilis
E Coli
Klebiella
cephalexin
1st gen ceph
gram + and PEcK
Proteus mirabilis
E Coli
Klebiella
cefoxitin
2nd gen ceph
gram + and HEN PEcKS
Haemophilus Enterobacter nesseiria (not gon) Proteus mirabilis E Coli Klebsiella Serratia
cefaclor
2nd gen ceph
gram + and HENS PEcK
Haemophilus Enterobacter nesseiria (not gon) Serratia Proteus mirabilis E Coli Klebsiella
cefuroxime
2nd gen ceph
gram + and HENS PEcK
Haemophilus Enterobacter nesseiria (not gon) Serratia Proteus mirabilis E Coli Klebsiella
cefprozile
2nd gen ceph
gram + and HENS PEcK
Haemophilus Enterobacter nesseiria (not gon) Serratia Proteus mirabilis E Coli Klebsiella Serratia
ceftriaxone
3rd gen ceph
only gram + is strep pneumo
serious gram -
Haemophilus Enterobacter nesseiria **** Proteus mirabilis E Coli Citrobacter (new) Klebsiella Serratia
ceftiazidime
3rd gen ceph
ANTIPSEUDOMONIAL
only gram + is strep pneumo
serious gram -
Haemophilus Enterobacter nesseiria Proteus mirabilis E Coli Citrobacter (new) Klebsiella Serratia
cefotaxime
3rd gen ceph
only gram + is strep pneumo
serious gram -
Haemophilus Enterobacter nesseiria Proteus mirabilis E Coli Citrobacter (new) Klebsiella Serratia
cefdinir
3rd gen ceph
only gram + is strep pneumo
serious gram -
Haemophilus Enterobacter nesseiria Proteus mirabilis E Coli Citrobacter (new) Klebsiella Serratia
cefepime
4th gen ceph
BIG GUN - wide spectrum
antipseudomonial and gram + again
Aztreonam
Cell wall inhibitor that binds to PBP3
prevents peptidoglycan cross linking in gram - only
monobactum resistant to beta lactamase as well
Imipenem
Carbapenem that binds to penicillin binding proteins inhibiting cell wall synthesis
Broad spectrum covering everything except MRSA
CNS toxicity (seizures); GI; Skin Rash
Given w/ Cilastatin to decrease renal breakdown (inactivates renal dehydropeptidase)
Cilastatin
given w/ imipenem to block renal breakdown of the drug via blocking renal dehydropeptidase I
Meropenam
Carbapenem that binds to penicillin binding proteins inhibiting cell wall synthesis
Broad spectrum covering everything except MRSA
CNS toxicity (seizures); GI; Skin Rash
Vancomycin
binds to D-ala D-ala moitey to inhibit cell wall synthesis in Gram + peptidoglycan polymerization
MRSA, enterococci, and oral 2nd line for C Dif
bactericidal
NOTs
Nephrotoxic
Ototoxic
thrombophelbitis
Red man syndrome
Gentamicin(3)
aminoglycoside
inhibits formation of initiation complex- binds to 30s
causes misreading of mRNA
blocks transloction
Bactericidal - severe gram (-)
Neomycin (3)
aminoglycoside
inhibits formation of initiation complex- binds to 30s
causes misreading of mRNA
blocks transloction
Bactericidal -severe gram (-)
Streptomycin (3)
aminoglycoside
inhibits formation of initiation complex - binds to 30s
causes misreading of mRNA
blocks transloction
Bactericidal - severe gram (-)
Tobramycin (3)
aminoglycoside
inhibits formation of initiation complex - binds to 30s
causes misreading of mRNA
blocks transloction
Bactericidal - severe gram (-)
Amikacin (3)
aminoglycoside -
inhibits formation of initiation complex - binds to 30s
causes misreading of mRNA
blocks transloction
Bactericidal - severe gram (-)
Tetracycline
Bacteriostatic- tetracycline
binds to 30s subunit and prevents attachment of aminoacyl TRNA,
limited CNS penetration
Fecal elimination limits renal concerns
Do not tale w/ antacids/Vitamins
VACUUM The BedRoom
doxycycline
Bacteriostatic - tetracycline
binds to 30s subunit and prevents attachment of aminoacyl TRNA,
limited CNS penetration
Fecal elimination limits renal concerns
Do not tale w/ antacids/Vitamins
VACUUM The BedRoom
demeclocycline
Bacteriostatic - tetracycline
binds to 30s subunit and prevents attachment of aminoacyl TRNA,
limited CNS penetration
Fecal elimination limits renal concerns
Do not tale w/ antacids/Vitamins
VACUUM The BedRoom
MORE ADH Antagonist -> dieuretic in SIADH
minocycline
Bacteriostatic - tetracycline
binds to 30s subunit and prevents attachment of aminoacyl TRNA,
limited CNS penetration
Fecal elimination limits renal concerns
Do not tale w/ antacids/Vitamins
VACUUM The BedRoom
Azithromycin
Macrolide - bacteriostatic
Binds to 23s unit of 50s subunit blocking translocation (macroslide) in protein synthesis
Prolonged QT, p450 inhib, cholestatic hep
PUS- atyp Pneumonia; URI; STD (chlamydia)
Resistance w/ methylation of the side
Erythromycin
Macrolide - bacteriostatic
Binds to 23s unit of 50s subunit blocking translocation (macroslide) in protein synthesis
Prolonged QT, p450 inhib, cholestatic hep
PUS- atyp Pneumonia; URI; STD (chlamydia)
Resistance w/ methylation of the side
Clarithromycin
Macrolide - bacteriostatic
Binds to 23s unit of 50s subunit blocking translocation (macroslide) in protein synthesis
Prolonged QT, p450 inhib, cholestatic hep
PUS- atyp Pneumonia; URI; STD (chlamydia)
Resistance w/ methylation of the side
Chloramphenical
bacteriostatic
binds to 50s subunit blocking the peptidyltransferase (formation of peptide bond)
Old use - meningitis
ALOT of side effects
-gray baby, dose dependent aplastic anemia
Clindamycin
bacteriostatic
Blocks peptide transfer (transpeptidation) at 50s ribosomal subunit
used in Anaerobes primary
Worry of C dif post use
Quinupristin/dalfoprisitin
a streptogramin
Synthesized by Strep virginias
- binds to the 23S portion of the 50s ribosome,
Used for MRSA, VRE, staph and skin infections
SE- hepatoxicity, pseudomonas colitis, p450 inhibit
polymyxin
cationic detergent (disrupts cell membranes)
Used for very serious gram - IV
-Neurotoxic and nephrotoxic
More likely used topical
methylphenidate
ritalin
CNS stimulant that increases NE release
~dextroamphetamine
dextroampthetamine
adderol
CNS stimulant that increases NE release
~ethyphenidate
Atomoxetine
NE reuptake inhibitor
Strattera
used in adult ADHD
Haloperidal
typical antipsychotic - HP
-> blocks D2 receptors in the brain (increase in cAMP)
SFX - extrapyramidal
endocrine dysruption
Neuroleptic malignant syndrome risk
Tardive dyskenesia
fluphenazine
typical antipsychotic - HP
-> blocks D2 receptors in the brain (increase in cAMP)
SFX - extrapyramidal
endocrine dysruption
Neuroleptic malignant syndrome risk
Tardive dyskenesia
trifluoperazine
typical antipsychotic - HP
-> blocks D2 receptors in the brain (increase in cAMP)
SFX - extrapyramidal
endocrine dysruption
Neuroleptic malignant syndrome risk
Tardive dyskenesia
loxapine
typical antipsychotic - HP
-> blocks D2 receptors in the brain (increase in cAMP)
SFX - extrapyramidal
endocrine dysruption
Neuroleptic malignant syndrome risk
Tardive dyskenesia
thiothixene
typical antipsychotic - HP
-> blocks D2 receptors in the brain (increase in cAMP)
SFX - extrapyramidal
endocrine dysruption
Neuroleptic malignant syndrome risk
Tardive dyskenesia
thioridazine
typical antipsychotic - LP
-> blocks D2 receptors in the brain (increase in cAMP)
SFX more antimuscarinic - dry mouth, constipation alpha1 block -> hypotenison histamine block -> sedation
Chlopromazine
typical antipsychotic - LP
-> blocks D2 receptors in the brain (increase in cAMP)
SFX more antimuscarinic - dry mouth, constipation alpha1 block -> hypotenison histamine block -> sedation
Olanzaprine
atypical antipsychotic
-> varied effects blocking 5HT2, Dopamine, alpha and H1
SFX
- less extrapyramidal and fewer anticholinergic effects that typical antipsychotics
UNIQUE- more concern w metabolic disorder and DM
Clozapine
atypical antipsychotic
-> varied effects blocking 5HT2, Dopamine, alpha and H1
SFX
- less extrapyramidal and fewer anticholinergic effects that typical antipsychotics
UNIQUE - agranulocytosis (weekly CBC checks)
Quetiapine
atypical antipsychotic
-> varied effects blocking 5HT2, Dopamine, alpha and H1
SFX
- less extrapyramidal and fewer anticholinergic effects that typical antipsychotics
UNIQUE - used for psychotic symptoms brought on due to parkinson medications, less side effect profile
Risperadone
atypical antipsychotic
-> varied effects blocking 5HT2, Dopamine, alpha and H1
SFX
- less extrapyramidal and fewer anticholinergic effects that typical antipsychotics
Aripiprazole
atypical antipsychotic
-> varied effects blocking 5HT2, Dopamine, alpha and H1
SFX
- less extrapyramidal and fewer anticholinergic effects that typical antipsychotics
Fluoxetine
SSRI
concern w/ sexual dysfunction and serotonin syndrome
(MSC, neuromuscular abnormalities, autonomic instability)
useful in bulimia
Paroxetine
SSRI
concern w/ sexual dysfunction and serotonin syndrome
MSC, neuromuscular abnormalities, autonomic instability
Sertraline
SSRI
concern w/ sexual dysfunction and serotonin syndrome (MSC, neuromuscular abnormalities, autonomic instability)
citalopram
SSRI
concern w/ sexual dysfunction and serotonin syndrome (MSC, neuromuscular abnormalities, autonomic instability)
venlafaxine
SNRI
concern w/ stimulant effects and increased BP
duloxetine
SNRI
also used for diabetic peripheral nueropathy and fibromyalgia
concern w/ stimulant effects and increased BP
Amytriptyline
TCA - blocks NE and 5 HT reuptake
but also alpha1 blocker, antimuscarinic, sedation
concern w/ overdose -> cardiotoxicity, convulsions, coma, fever, confusions/hallucinations - Rx NaHCO3
used for fibromyalgia mainly
nortriptyline
TCA - blocks NE and 5 HT reuptake
but also alpha1 blocker, antimuscarinic, sedation
concern w/ overdose -> cardiotoxicity, convulsions, coma, fever, confusions/hallucinations - Rx NaHCO3
imipramine
TCA - blocks NE and 5 HT reuptake
but also alpha1 blocker, antimuscarinic, sedation
concern w/ overdose -> cardiotoxicity, convulsions, coma, fever, confusions/hallucinations - Rx NaHCO3
Used for bedwetting
clomipramine
TCA - blocks NE and 5 HT reuptake
but also alpha1 blocker, antimuscarinic, sedation
concern w/ overdose -> cardiotoxicity, convulsions, coma, fever, confusions/hallucinations - Rx NaHCO3
Used in OCD
doxepin
TCA - blocks NE and 5 HT reuptake
but also alpha1 blocker, antimuscarinic, sedation
concern w/ overdose -> cardiotoxicity, convulsions, coma, fever, confusions/hallucinations - Rx NaHCO3
tranylcypromine
MAOI - blocks the breakdown of NE, 5Ht and Dopamine
Concern w/ hypertensive crisis in the presence of tyramine and excess NE
Phenelzine
MAOI - blocks the breakdown of NE, 5Ht and Dopamine
Concern w/ hypertensive crisis in the presence of tyramine and excess NE
Isocarboxazid
MAOI - blocks the breakdown of NE, 5Ht and Dopamine
Concern w/ hypertensive crisis in the presence of tyramine and excess NE
Buproprion
NDRI - blocks the reuptake of dopamine and NE, synergistic w/ SSRI
Useful in smoking cessation and NO sexual side effects
Concern w/ seizures in bulemics, some stimulant effects
Mirtazapine
tetracyclic antidepressant that blocks alpha2
increasing the release of NE and 5 HT
also potent 5Ht2 and 5 Ht3 receptor antagonist
concern w/ sedation and weight gain (may be a good thing)
- dry mouth
Trazodone
tetracyclic that blocks serotonin reuptake
Used primarily for insomnia
concern w/ priaprism and sedation
Buspirone
Stimulates 5 HT1a receptors
Used in GAD
takes 2 weeks work
No real side effects, can be used w/ alcohol, non sedating or addictive
Mannitol
osmotic diuertic -> increased vascular osmolarity and tubular fluid osmolarity (works in proximal tubule)
helps w/ shock, increased Intracranial pressure and as a diuretic, glaucoma
acetazolamide
carbonic anhydrase inhibitor -> self limited NaHCO3 diuresis (works in the proximal tubule)
used in glaucoma, urinary alkalization, fix metabolic acidosis, altitude sickness
Worry of hyperchloremic metabolic alkalosis and SULFA allergy
Furosimide
SULFA loop dieuretic
inhibits cotransport of Na/K/2Cl in the ascending loop of hence thus disrupting the medullary hypertonicity and leads diuresis of water (in addition to the electrolytes)
Loops lose Ca
Ototoxic, Nephrotoxic, hypokalemia, dehyd, gout,
toresemide
SULFA loop dieuretic
inhibits cotransport of Na/K/2Cl in the ascending loop of hence thus disrupting the medullary hypertonicity and leads diuresis of water (in addition to the electrolytes)
Loops lose Ca
Ototoxic, Nephrotoxic, hypokalemia, dehyd, gout,
bumetanide
SULFA loop dieuretic
inhibits cotransport of Na/K/2Cl in the ascending loop of hence thus disrupting the medullary hypertonicity and leads diuresis of water (in addition to the electrolytes)
Loops lose Ca
Ototoxic, Nephrotoxic, hypokalemia, dehyd, gout,
ethycrynic acide
inhibits cotransport of Na/K/2Cl in the ascending loop of hence thus disrupting the medullary hypertonicity and leads diuresis of water (in addition to the electrolytes)
Loops lose Ca
NO SULFA ALLERGY
Hydrochlothiazide
prevents Na/Cl reabsorption in the distal convoluted tubule reducing the diluting capacity of the nephron
retains Ca from the lumen
Use in HTN,
nephrogenic DI(encourages earlier reabsorption in the proximal tubule?)
idiopathic hypercalciuria
metolazone
prevents Na/Cl reabsorption in the distal convoluted tubule reducing the diluting capacity of the nephron
retains Ca from the lumen
Use in HTN,
nephrogenic DI(encourages earlier reabsorption in the proximal tubule?)
idiopathic hypercalciuria
chorthalidone
prevents Na/Cl reabsorption in the distal convoluted tubule reducing the diluting capacity of the nephron
retains Ca from the lumen
Use in HTN,
nephrogenic DI(encourages earlier reabsorption in the proximal tubule?)
idiopathic hypercalciuria
chlorothiazide
prevents Na/Cl reabsorption in the distal convoluted tubule reducing the diluting capacity of the nephron
retains Ca from the lumen
Use in HTN,
nephrogenic DI(encourages earlier reabsorption in the proximal tubule?)
idiopathic hypercalciuria
spironolactone
k sparing dieuretic - aldosterone receptor antagonist
also used in acne and polycystic kidney disease
tox- hyperkalemia and antiandrogen (worse than eplerenone)
eplerenene
k sparing dieuretic - aldosterone receptor antagonist
toxicity - hyperkalemia
amiloride
K sparing dieuretic - blocks Na channel
concern of hyperkalemia
triamterene
K sparing dieuretic - blocks Na channel
concern of hyperkalemia
Hydrocortisone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
~ cortisol
prednisone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
triamcinolone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
Topical
dexamethasone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
Used dexamethasone suppression test
beclomethasone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
Inhaled for asthma
fluticasone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
inhaled for asthma
prednisolone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
IV
methylpredisiolone
glucocorticoid
blocks the production of leukotriene and prostaglandins by inhibiting phospholipase A2 and expression of COX2
Tox
- iatagenic Cushing’s syndrome
- Adrenal insufficiency
- osteoprosisi
- ulcers
- DM
IV
lispro
rapid acting insulin
aspart
rapid acting insulin
gluisine
rapid acting insulin
regular insulin
regular acting insulin
NPH
intermediate acting insulin
Glargine
long acting insulin
Determir
long acting insulin
Metformin
decreases gluconeogenisis, increases glycolysis, increases peripheral glucose uptake
lowers LDL and triglycerides
Tox: lactic acidosis, contraindicated in renal failure
glyburide
sulfonylureas
close K channel in the beta cell membrane -> depolarization of the cell-> triggering insulin release via Ca influx
risk of hypoglycemia, some weight gain
glimepiride
sulfonylureas
close K channel in the beta cell membrane -> depolarization of the cell-> triggering insulin release via Ca influx
risk of hypoglycemia, some weight gain
glipizide
sulfonylureas
close K channel in the beta cell membrane -> depolarization of the cell-> triggering insulin release via Ca influx
risk of hypoglycemia, some weight gain
pioglitazone
increases insulin sensitivity by binding to PPAR-gamma nuclear TF which is responsible for regulating FA storage and glucose metabolism
-> increased response to insulin
Risk
- Bladder CA
- osteoperosis
- hepatoxicity
- weight gain/edema
- Heart failure
rosiglitazone
increases insulin sensitivity by binding to PPAR-gamma nuclear TF which is responsible for regulating FA storage and glucose metabolism
-> increased response to insulin
Risk
- hepatotoxicity
- weight gain/edema
- Heart failure*
acarbose
alpha glucosidase inhibitors
delays sugar hydrolysis and glucose absorption
- thus passed in the stool
- > less postprandial hyperglycemia
Toxicity: GI disturbance (diarrhea/flatulence)
miglitol
alpha glucosidase inhibitors
delays sugar hydrolysis and glucose absorption
- thus passed in the stool
- > less postprandial hyperglycemia
Toxicity: GI disturbance (diarrhea/flatulence)
pramlintide
amylin analog
acting as a amylin which is normally secreted w/ insulin that leads to depression of glucagon secretion and delaying gastric emptying
Used only in patients taking insulin (type I or Type II)
- injected after every meal
risk of hypoglycemia, nausea, diarrhea
Exenatide
GLP 1 analog (an incretin)
analog of exendin which acts like GLP 1 ->
- decreases glucagon secretion
- increases insulin secretion
- delays gastric emptying
do not use while on insulin
Risk of pancreatitis and N/V
liraglutide
GLP 1 analog (an incretin)
analog of GLP 1 ->
- decreases glucagon secretion
- increases insulin secretion
- delays gastric emptying
do not use while on insulin
Risk of pancreatitis and N/V
Sitagliptin
inhibits dipeptidyl peptidase IV (DPP-IV) which affects glucagon like peptide (GLP-1)
-Normally DPP-IV breaks down GLP but this allows the incretin to remain
Prolongs insulin actions
- decreases glucagon secretion
- increases insulin secretion
- delays gastric emptying
heparin
cofactor for increasing the efficacy of antithrombin inhibiting the intrinsic pathway cascade
elevated PTT
worry of heparin induced thrombocytopenia ( binds to platelet factor 4 - IgG then binds and removes)
enoxaparin
LMWH
acts more on factor Xa than inducing antithrombin
2-4x the half life, not easily reversible
does on weight
dalteparin
LMWH
acts more on factor Xa than inducing antithrombin
2-4x the half life, not easily reversible
does on weight
lepirudin
derivative of hirudin (leeches) and it inhibits thrombin via another mech (not inducing antithrombin)
alternative to heparin w/ HIT complications
bivalirudin
derivative of hirudin (leeches) and it inhibits thrombin via another mech (not inducing antithrombin)
alternative to heparin w/ HIT complications
desirudin
derivative of hirudin (leeches) and it inhibits thrombin via another mech (not inducing antithrombin)
alternative to heparin w/ HIT complications
Fondaparinux
activates antithrombin and inhibits factor Xa
not the same as LWMH
rivaroxaban
direct factor Xa inhibitor
apixaban
direct factor Xa inhibitor
Alteplase
thrombolytic
activates plasminogen ->plasmin to lyse clots
streptokinase
thrombolytic
activates plasminogen ->plasmin to lyse clots
reteplase
thrombolytic
activates plasminogen ->plasmin to lyse clots
tenecteplase
thrombolytic
activates plasminogen ->plasmin to lyse clots
Clopidogrel
ADP receptor inhibitor,
blocks ADP released from activated platelets from binding and up regulating Gp IIb/IIIa receptors up to the cell surface and allowing aggregation
ticlopidine
ADP receptor inhibitor,
blocks ADP released from activated platelets from binding and up regulating Gp IIb/IIIa receptors up to the cell surface and allowing aggregation
Tox - neutropenia
prasugrel
ADP receptor inhibitor,
blocks ADP released from activated platelets from binding and up regulating Gp IIb/IIIa receptors up to the cell surface and allowing aggregation
ticagrelor
ADP receptor inhibitor,
blocks ADP released from activated platelets from binding and up regulating Gp IIb/IIIa receptors up to the cell surface and allowing aggregation
Abciximab
binds to glycoproetien receptor IIb/IIIa directly inhibiting fibrinogen from binding preventing cross linking
eptifibatide
binds to glycoproetien receptor IIb/IIIa directly inhibiting fibrinogen from binding preventing cross linking
tirofiban
binds to glycoproetien receptor IIb/IIIa directly inhibiting fibrinogen from binding preventing cross linking
Acyclovir
monophophorylated guanosine analog that is phosphorylated by HSV/VZV thyrimidine kinase
preferentially inhibits viral DNA polymerase
Used for HSV and VZV, weak EBV
valacyclovir is oral viral prodrug
Famciclovir
acycyclic guanosine analog
prodrug of peniclovir
needs to be phosphorylated by thymidine kinase to work inhibit viral DNA polymerase in HSV and VZV
ganciclovir
monophosphate formed by CMV viral kinase leads to active guanine analog that inserts itself in viral DNA via DNA polymerase, inhibiting it
valgancyclovir is oral viral prodrug
toxicity: bone marrow suppression and renal toxicity
Foscarnet
Viral DNA polymerase inhibitor that does NOT require activation by a viral kinase
Used for CMV retinitis and acyclovir resistant HSV
Concern w/ Nephrotoxicity and anemia
Zanamivir
inhibits influenza neurmainidase, blocking viral release
used in rx and prevention of influenza A and B
-need to be used w/in 24-48 hrs
oseltamivir
inhibits influenza neuraminidase, blocking viral release
used in rx and prevention of influenza A and B
need to be used in 24-48hrs
Ribavirin
inhibits synthesis of guanine nucleotides by competively inhibing IMP dehydrogenase
used in RSV (adults mainly), and hep C*
Toxicity : hemolytic anemia and teratogen
maraviroc
CCR5 co-receptor antagonists,
Bonds to host cell co-receptor preventing HIV gp100 from binding and infusiion
lopinovir
Protease inhibitor (HIV 1- protease; gag gene)
blocks maturation of HIV viral proteins post translation
Concern of lipodystrpohy, hyperglycemia, GI intolerance, p450 inhibition
atazanivir
Protease inhibitor (HIV 1- protease; gag gene)
blocks maturation of HIV viral proteins post translation
Concern of lipodystrpohy, hyperglycemia, GI intolerance, p450 inhibition
- nephrolithias convern
- increased bilirubin
darunavir
Protease inhibitor (HIV 1- protease; gag gene)
blocks maturation of HIV viral proteins post translation
Concern of lipodystrpohy, hyperglycemia, GI intolerance, p450 inhibition
fosamprenavir
Protease inhibitor (HIV 1- protease; gag gene)
blocks maturation of HIV viral proteins post translation
Concern of lipodystrpohy, hyperglycemia, GI intolerance, p450 inhibition
Saquinavir
Protease inhibitor (HIV 1- protease; gag gene)
blocks maturation of HIV viral proteins post translation
Concern of lipodystrpohy, hyperglycemia, GI intolerance, p450 inhibition
ritonavir
Protease inhibitor (HIV 1- protease; gag gene)
blocks maturation of HIV viral proteins post translation
Concern of lipodystrpohy, hyperglycemia, GI intolerance, p450 inhibition
Especially used to BOOST other PI functions
*pancreatitis
indinavir
Protease inhibitor (HIV 1- protease; gag gene)
blocks maturation of HIV viral proteins post translation
Concern of lipodystrpohy, hyperglycemia, GI intolerance, p450 inhibition
*nephrolithias concern
Tenofovir
NRTI - nucleotide vs nucleoside
- DOES NOT need phosphorylation from thrymidine kinase to work like other NRTI
competitively inhibits nucleotide binding to reverse transcriptase and terminate the DNA chain
lactic acidosis
Emtricitabine
NRTI
competitively inhibits nucleotide binding to reverse transcriptase and terminate the DNA chain, needs to phosphorylated by thrimidine kinase to work
lactic acidosis
Abacavir
NRTI
competitively inhibits nucleotide binding to reverse transcriptase and terminate the DNA chain, needs to phosphorylated by thrimidine kinase to work
lactic acidosis
*life threatening hypersensitivity
lamivudine
NRTI
competitively inhibits nucleotide binding to reverse transcriptase and terminate the DNA chain, needs to phosphorylated by thrimidine kinase to work
lactic acidosis
Zidovudine
NRTI
competitively inhibits nucleotide binding to reverse transcriptase and terminate the DNA chain, needs to phosphorylated by thrimidine kinase to work
-prophylactically given to moms peri-delivery if not on HAART prior
lactic acidosis
- bone marrow suppression
- anemia
Didanosine
NRTI
competitively inhibits nucleotide binding to reverse transcriptase and terminate the DNA chain, needs to phosphorylated by thrimidine kinase to work
lactic acidosis
- Pancreatitis
- hepatic steatosis
- peripheral neuropathy
Stavudine
NRTI
competitively inhibits nucleotide binding to reverse transcriptase and terminate the DNA chain, needs to phosphorylated by thrimidine kinase to work
lactic acidosis
- peripheral neuropathy
- hepatic steastosis
Nevirapine
NNRTI
noncompetative inhibitor of the reverse transcriptase, binds to another site, does not need phosphorylation like NRTI
Rash
efavirenz
NNRTI
noncompetative inhibitor of the reverse transcriptase, binds to another site, does not need phosphorylation like NRTI
Rash
- neuropsychiatric disorders
- false + cannaboid
- teratogenic
delavirdine
NNRTI
noncompetative inhibitor of the reverse transcriptase, binds to another site, does not need phosphorylation like NRTI
Rash
etravine
NNRTI
noncompetative inhibitor of the reverse transcriptase, binds to another site, does not need phosphorylation like NRTI
Rash
rilpivirine
NNRTI
noncompetative inhibitor of the reverse transcriptase, binds to another site, does not need phosphorylation like NRTI
Rash
Raltegravir
HIV viral integrase inhibitor, prevents the viral DNA from combing w/ host DNA
SFX : hypercholesterolemia, Nausea, vomitting, rash
Enfuvirtide
HIV fusion inhibitor blocking gp41 binding and infection of a cell
injection site reaction and increased risk of bacterial pneumonia
Griseofulvin
interferes w/ microtubule function, disrupts mitosis, deposits in keratin containing tissues
Used in oral Rx for superficial infection (inhibits dermatophyes)
concern w/ teratogen, HA and increased p450 metabolism (rarely confusion)
Terbinafine
inhibits fungal enzyme squalene epoxidase
(sqaulene -> lamosterol)
used for dermatophytes (onchomycosis esp)
Concerne w/ abnormal LFTs/hepatotoxicity and GI
Amphoteracin B
binds to ergosterol and forms holes in fungal cell membrane
Serious systemic mycoses
-cryptococcal, blastomyces, coccidiodes, histoplasma, mucor
Concern w/ fever, chills, hypotension, nephrotoxicity * (supplement K and Mg w/ hypokalemia), arrythmias, aneima
Nystatin
binds to ergosterol and forms holes in fungal cell membrane
Used topically b/c otherwise it is too toxic for use
thrush, diaper rash, vaginal candidiasis
Fluconazole and other azoles
inhibits fungal sterol (elgosterol synth) by blocking p450 conversion of lamosterol -> ergosterol
local and lass serious systemic mycoses use
Fluconazole for chronic suppression of cryptococcal meningitis
concern w/
- testosterone synth inhib (impotence and gynectomastia)
- liver dysfunciton ( blocks p450 metab)
Flucytosine
inhibits DNA/ RNA biosynthesis by converting to 5 fluorouracil by cytosine demaninase
-> nucleoside analog
used in systemic fungal infections, like cryptoccocal (w/ amphoteracin B)
concern w/ cone marrow suppression and GI
Caspofungin
inhibits cell wall synthesis by inhibition synthesis of beta glucan
-> cell lysis and death
used in invasive aspergillus and candid
Concern w/ GI upset and flushing
micafungin
inhibits cell wall synthesis by inhibition synthesis of beta glucan
-> cell lysis and death
used in invasive aspergillus and candid
Concern w/ GI upset and flushing
Cyproheptadine
antihistamine w/ 5HT2 receptor antagonist
used in serotonin syndrome
Methotrexate
folic acid analog that inhibits dihydrofolate reductase
(s phase)
inhibiting conversion of DHF back to THF -> less dTMP and ultimately less DNA
used in: ALL/AML, immune supp (RA, psoriasis), and Uterine path (ectopic, choriocarcinoma, hydradidiform mole)
Tox: myelosuppresion, fibrotic lung disease
teratogenic
give leucovorin
leucovorin
folinic acid used in methotrexate rescue
5 fluororacil
pyrimidine analog (S phase) that covalently complexes to folic acid, the complex then inhibits thymidylate synthase -> decreases dTMP and less DNA in general
used in colon and pancreatic CA
especially topically basal cell and actinic keratosis
Tox: myelosuppression and photosensitivity
cytarabine
pyrimidine analog (s phase) -> inhibition of DNA polymerase
used in leukemia and lymphoma
concern w/ leukopenia
6 mercaptopurine
purine (thiol analog) (s phase) -> less purine synthesis
blocks PRPP amidotransferase
used in leukemias
Metabolized xanthine oxidase -> increased toxicity w/ allopurinol ( myelosuppression and hepatotoxicity)
6 thioguanine
purine (thiol analog) (s phase) -> less purine synthesis
blocks PRPP amidotransferase
used in leukemias
differs from 6 mercaptopurine in that it is not metabolized by xanthine oxidase
Dactinomycin
antibiotic that intercalates DNA
used in Ewing sarcoma, rhabdomyosarcomas and Wilms
Doxorubicin
(adriamycin) antibiotic that
1. generates free radicals
2. noncovalently intercalates in DNA -> DNA breaks
used in solid tumors
Risk of cardiotoxicity - rx w/ dexrazoxane
Daunorubicin
antibiotic that
- generates free radicals
- noncovalently intercalates in DNA -> DNA breaks
used in solid tumors
Risk of cardiotoxicity - rx w/ dexrazoxane
bleomycin
antibiotic that induces free radicals -> DNA strand breaks
Used in testicular CA and Hodgkins lymphoma
Pulmonary fibrosis toxicity
cyclophosphamide
alkalating agent that covertly cross links DNA at Guanine N-7, needs bioactivation by liver
Uesd in
- Solid tumors
- Immune suppression : lupes nephritis and PAN
Toxicity: hemorragic cystits, Rx w/ Mensa
increased transitional cell CA risk
Mensa
used in hemorragic cystitis caused by cyclophosphamide’s metabolite acrolein
Nitrosourease (carmustine etc..)
alkylating agent used in brain tumors
Crossed the BBB
Concern w/ CNS toxicity - dizzy, ataxia
Busulfan
alkylates DNA
used in CML
Concern w/ pulmonary fibrosis and hyperpigmentation
ifosphamide
similar to cyclophosphamide
alkalating agent that covertly cross links DNA at Guanine N-7, needs bioactivation by liver
Used in testicular CA
vincristine
binds to tubulin in the M phase to block polymerization so microtubules can’t form
used in: hodgkin lymphoma, wilma, ewing, choricarcinoma
Worry of: neurotoxicity and peripheral neuritis
vinblastine
binds to tubulin in the M phase to block polymerization so microtubules can’t form
used in: hodgkin lymphoma, wilma, ewing, choricarcinoma
Worry of myelosuppression (Blasts bone marrow0
Paclitaxel
hyperstabilize polymerized microtubules in the M phase so mitotic spindles cannot break down
used in ovarian and breast
worry of myelosuppression and hypersensitivity
Cisplatin
cross links w/ DNA - damage
used in testicular, bladder, ovary cA
causes nephrotoxicity and acoustic nerve damage
carboplatin
cross links w/ DNA - damage
used in testicular, bladder, ovary cA
causes nephrotoxicity and acoustic nerve damage
oxaliplatin
cross links w/ DNA - damage
used in testicular, bladder, ovary cA
causes nephrotoxicity and acoustic nerve damage
Etoposide
inhibits topoisomerase II -> unwinds supercoiling usually -> DNA degradation
Used in call cell Lung, prostate, and testicular CA
concern are usual w/ CA myelosup, GI and aloplecia
teniposide
inhibits topoisomerase II -> unwinds supercoiling usually -> DNA degradation
Used in call cell Lung, prostate, and testicular CA
concern are usual w/ CA myelosup, GI and aloplecia
Irinotecan
inhibits topoisomerase I
used in METS Colon Ca
topotecan
inhibits topoisomerase I
used in
-small cell lung CA,
-ovarian CA
Cervical CA
Hydroxyurea
inhibits ribonucleotide reductase -> decreased DNA synthesis in antineoplastic function
Increases HbF in sickle cell
Prednisone antineoplastic MOA
may trigger apoptosis
used in CLL and NHL
worry of BAM CUSHINGOID
Trastuzumab
monoclonal ab against her-2 Neu, a tyrosine kinase
needs to be her2 + breast CA
worry of cardiotoxicity
Rituximab
monoclonal Ab against CD20, found on most B cell neoplasms
Used in Non hodgkin lymphoma, RA, phemigus vulgaris, ITP and vasculitis
imatinib
enzyme inhibitor for chromosome bcr-abl tyrosine kinase
Used in CML (ALL and AML if positive)