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