Pharmacology Flashcards
Allopurinol
Purine analog that inhibits PRPP amidotransferase.
6-mercaptopurine
Purine analog that inhibits PRPP amidotransferase.
Hydroxyurea
Inhibits ribonucleotide reductase
5-Fluorouracil
Inhibits thymidylate synthase
Methotrexate
Inhibits dihydrofolate reductase. Used in Hodgkin’s lymphoma, non-Hodgkin’s lymphoma, lung cancer, breast cancer, osteosarcomas.
Pyrimethamine
Inhibits dihydrofolate reductase
Trimethoprim
Antimetabolite that inhibits bacterial dihydrofolate reductase. Often used in combo with sulfonamides, e.g. sulfamethoxazole) to sequentially block folate synthesis
Quinolone antibiotics
Inhibit bacterial topoisomerase IV
Rifampicin
Binds B subunit of RNA polymerase and inhibits initiation of RNA synth. Notably lipophilic thus readily crosses BBB.
Actinomycin D
Binds DNA and prevents RNA polym from moving along template. Originally used as antibiotic but now as chemo for gestational trophoblastic tumors, Wilms’ tumor, rhabdomyosarcoma
Abx that inhibit 30s subunit
Aminoglycosides, tetracycline
Abx that inhibit 50s subunit
Chloramphenicol, erythromycin, clindamycin, lincomycin
Tetracycline
Prevents initiation since charged tRNA cannot bind ribosome
Streptomycin
Prevents initiation since code is misread
Erythromycin
Inhibits translocation
Disulfiram
Inhibits conversion of aldehyde to acetic acid (in alcohol metabolism) so meant to stop alcoholics from drinking since they feel like crap
Ethanol
Antidote to methanol poisoning. Competitively inhibits ADH by binding to active site thus preventing enzyme from binding to methanol. Prevents further accumulation of formic acid and formaldehyde by favoring conversion to acetaldehyde.
Disulfiram effect
I.e. same effect with other medications.
Metronidazole, tolbutamide, cefoperazone, cefotetan
Cardiac glycosides
Bind and inhibit Na-K-ATPase by competing for sites on extracellular side. Results in increased cardiac contractility through Ca-dependent mechanism
Melatonin
Can treat circadian rhythm disorders like jet lag
Sildenafil citrate
Aka viagra. Selective inhibitor or the phosphodiesterase that prolongs the effects of NO
Orlistat
Inhibits pancreatic lipase thus prevents absorption of dietary fat. As result–> steatorrhea.
Fibrates
Class of lipid-lowering drugs that activate peroxisome proliferator-activated receptor-a (PPAR-a) causing increase in LPL activity. Decrease blood TG but little effect on plasma cholesterol levels
Drugs that lower cholesterol
Resins and ezetimibe
Drugs that lower TG
Fibrates
Drugs that lower cholesterol and TG
Niacin and statins (esp atorvastatin)
Niacin
Lowers TG and chol by inhibiting VLDL secretion
Terbinafine
Antifungal. Inhibits conversion of squalene to lanosterol in fungi. Esp useful for onychomycosis.
Imidazole and triazle antifungals
Inhibit conversion of lanosterol to ergosterol in fungi. Cytochrome p450 inhibitors.
Urodeoxycholate
Used in tx of radiolucent gallstones. Solubilizes cholesterol and inhibits its production. However cholecystectomy preferred tx so used in poor surgical candidates
Corticosteroids
Block PLA2 and interrupt COX synthesis
Zileuton
Blocks lipoxygenase
Zafirlukast
Blocks leukotriene receptors
Montelukast
Blocks leukotriene receptors
Indomethacin
COX inhibitor. Closes PDAs
Most commonly known P450 inducers
Carbamazepine, phenytoin, barbiturates, alcohol, griseofulvin, rifampicin
Treatment of lead poisoning
EDTA, dimercaprol, succimer
Deferoxamine
Iron chelator
Chemo-alkylating agents
Cisplatin, carboplatin
imatinib mesylate
Specific inhibitor of tyrosine kinase domain in abl and c-kit; useful in CML
Ethyl methanesulfonate (EMS)
Introduces mutations by transferrinh methyl groups to DNA nucleotide bases. Do not cause cell death so not used as chemo
Ribavirin
RSV (resp synctial virus)
Foscarnet
CMV retinitis
Acyclovir
HSV1, HSV2, VZV, EBV.
Inhibits viral DNA polymerase
Amantidine
Influenza A
Reserpine
Minimizes motor abnormalities in Huntingtons.
Side effects amiodarone
Pulm fibrosis (restrictive), interstitial pneumonitis, photosensitivity, thyroid disorders, GI disturbances
Cholestyramine
Bile acid resin. Decreases serum TGs and chol
Thiazide diuretics
Inhibit NaCl reabsorption in early distal tubule. Increased Na delivery to principal cells of late DCT causes increased Na reabsorption and an increase in K secretion to maintain electroneutrality. (Note not K+ sparing.)
Limit Ca loss
Amiloride
K+ sparing diuretic. Acits on Na channels of collecting duct to prevent its reabsorption and thus K+ secretion
Ketorolac
NSAID
Diphenhydramine
H1 antag. Tx-allergic rxns, motion sickness, dystonic rxns. May cause sedation, anticholinergic effects, anti-alpha-adrenergic effects
Lithium, demeclocycline
ADH antags, act along collecting tubule
Carbonic anhydrase inhibitors
act in PCT
Osmotic diuretics
Act in loop, PCT, collecting duct
Loop diuretic toxicity
metabolic alklalosis
Important side effect statins
Rhabdomyolysis
Acetazolamide
Helps with acute mtn sickness by causing metabolic acidosis….increased breathing drive and higher O2 levels in body
NSAID toxicity
Acute interstitial nephritis
Urinary flow rate
GFR*[inulin]plasma/[insulin]urinary
Km
inversely proportional to the affinity of the enzyme for the substrate
Vancomycin
Only Gram +ve. Resistance-precents vanco from binding by mutating terminal aa in microorganism’s cell wall
Resistance to macrolides
Through methyltion of its rRNA at ribo binding site
Tx for neurocysticerosis
Albendazole
Reserpine
Minimizes motor abnormalities in Huntingtons
Penacillamine
Chelating agent for Cu
Prochlorperazine
Acts on area postrema of medulla (CTZ)
Bismuth
Triple therapy in H pylori
Ranitidine
Mild reflux
Sulcrafate
Coats gastric mucosa
Unfractionated heparin
DVT/PE. Catalyzes activation antithrombin III, decreases available thrombin, inhibits factor Xa. Monitor with PTT.
PTT
Intrinsic pathway
Bleeding time
Measures platelet fn. If bad, think von Willebrand.
INR
Measures PT. Extrinsic. Warfarin.
LWMH
$$$. No need to monitor.
Trastuzumab
Ab to HER-2. Binds to EC domain
All-trans retinoic acid
acute promyelocytic leukemia
Imantinib mesylate
CML
Methotrexate
Folic acid analog
Specific for S phase of cell cycle. Can cause myelosuppression.
Reversed with leucovorin.
Rituximab
non-Hodgkins lymphoma
Cyclosporine
Immunosuppressant. -IL-2. Blocks differentiation and activation T-lymphos. Metab by p450
P450 inhibitors
Macrolides Amiodarone Grapefruit juice Isoniazid Cimetidine Ritonavir Acute alcohol abuse Ketoconazole Sulfonamides
Drugs for Hodgkins
Adriamycin (doxorubicin)
Bleomycin
Vinblastine
Dacarbazine
Hydroxyurea
Sickle cell. Antimetabolite.
TB drugs
Rifampicin, isoniazid, pyrazinamide, ethambutol, streptomycin
Abciximab
IIb/IIIa inhib-prevents fibrinogen from binding, interferes with platelet agg
Clopidogrel
ADP inhibitor which is involved in binding of fibrinogen to platelets
Selegiline
MAOB inhib. Increases Da availability. PD.
Artesunate
Treats p. falciparum infection
Platelet phsopholipids
Intrinsic and extrinsic clotting pathways.
Bleomycin toxicity
Pulmonary fibrosis, pigmentation
Aminocaproic acid
Reverses tPA. Blocks plasminogen–>plasminogen
Recomb factor VIII
Hemophilia A
Vit k
Cofactors for epoxide reductase….II, VII, IX, X. Warfarin reversal.
Prednisone SE
Glucocorticoid psychosis
Vincristine SE
Areflexia, peripheral neuritis
Imantinib
CML
Bisphosphonates
Bind to hydroxyapatite and inhibit osteoclast mediated resorption
Isoniazid
TB exposure prophylaxis, decreases synth mycolic acids.
Treatment for syphilis
Penicillin
P450 Inducers
Quinidine Barbiturates St John's wort Phenytoin Rifampicin Griseofulvin Carbamazepine Chronic alcohol use