Pharma Flashcards
Analog of clofibrate
More active in decreasing triglycerides
Gemfibrozil (Iopid)
Bis-phenol in a sulfur linkage and is highly hydrophobic
Probucol
Reduces plasma cholesterol
Probucol
Peripheral catabolism of VLDL and chylomicrons
Decrease triglycerides
This also targets triglycerides
CLOFIBRATE
Increases bile acid secretion
Probucol
No effects on triglycerides
Probucol
Positive Coomb’s test associated with hemolytic anemia
Methyldopa
Lactation (increase prolactin)
Methyldopa
Can cause impotence in males
Methyldopa
Beta blockers
Drugs that can cause lupus-like syndrome
Hydralazine, Methyldopa
Rebound hypertension after sudden withdrawal
Clonidine (Catapres)
Aloha blockers
PraZOSIN, TeraZOSIN, DoxaZOSINe
Decreases peripheral resistance
Alpha blockers
Orthostatic hypertension
Alpha blockers
Blocks a1 adrenergic receptors
Alpha blockers
Drug for pheochromocytoma
Phenoxybenzamine
Bronchoconstriction
Beta blockers
Beta blockers
PropanOLOL, MetoprOLOL, AtenOLOL, LabetOLOL, CarvediLOL
Inhibit the effect of B-adrenergic stimulation
Renin release
Vasodilation
Bronchodilation
Dec PR and CO
Metabolic effects: inc insulin secretion, glycogenolysis, gluconeogenesis in both thebliver and the skeletal muscle
B-blockers lowers BP by
Dec CO
Inhibiting the release of renin and the production of angiotensin II
Possible reducing NE release frim sympathetic neurons
Dec central vasomotor activity
B-blockers used for
Portal HPN
Migraine
Aortic aneurysms (dec HR)
Post MI
Pre eclampsia
Hydralazine
Hirsutism
Minoxidil
Used to treat mal baldness
Minoxidil
Direct vasodilator drugs
Hydralazine
Minoxidil
Sodium nitroprusside
Dilates both resistance and capacitance vessels
Sodium nitroprusside
Used in hypertensive emergencies
Sodium nitroprusside
Rapid vasodilatation and hypotension
Sodium nitroprusside
Risk of toxicity of sodium nitroprusside
Cyanide and thiocyanide toxicity
Cyanide toxicity is reduced by
Sodium thiosulfate
Antihypertensive drugs most widely used acutely during pregnancy
Nifedipine
Labetalol
Hydralazine
Methyldopa
Blocks formation of angiotensin II
ACE inhibitors
Promoting vasodilation and decreased aldosterone
ACE inhibitors
Inc bradykinin and vasodilator prostaglandins by inhibiting kininase II
ACE inhibitors
15-20% develop dry, hacking cough (duento bradykinin or substance P)
ACE inhibitors
Angioedema
ACE inhbitors
Classifications of Diuretics
Osmotic diuretics
Carbonic anhydrase inhibitors
Loop diuretics
Thiazide diuretics
Potassium sparing diuretics
Proximal convulated tubule
Acetazolamide
Thick ascending limb of the loop of Henle
Loop diuretics
Distal convoluted tubule
Thiazides
Selectively inhibit NaCl reabsorption
Loop diuretics
Inhibit NaCl transport
Thiazides
Toxicity: HYPOkalemic metabolic alkalosis, ototoxicity, HYPERuricemia, HYPOmagnesemia, allergic reactions, severe dehydration, HYPERcalcemia
Loop diuretics
Loop diuretic drugs
Furosemide, Ethacrynic acid (not a sulfonamides)
Prototype drug for Thiazides
Hydrochlorothiazide
Thiazide drugs
Indapamide, Metolazone
Compete with secretion of uric acid
Thiazides
Enhance calcium reabsorption
Thiazides
A competitive aldosterone receptor antagonist in thencortical collecting tubule
Spironolactone
Blocks Na channels in the cortical collecting tubule
Triamterene, Amiloride
Potassium Sparing Diuretics
Spironolactone (prototype), Eplerenone, Triamterene, Amiloride
Toxicity of Potassium Sparing Diuretics
Hypercholeremic metabolic acidosis
Gynecomastia
Acute renal failure
Kidney stone
Drugs that can cause gynecomastia
Cimitidine, Spironolactine, Ketoconazole
Osmotic diuretic drugs
Mannitol (prototype)
Inc tubular osmolarity, producing inc urine flow
Osmotic diuretics
DOC for AV nodal arrythmias (SVT)
Adenosine
Treatment for digitalis toxicity
K+
Treatment for torsade de pointes/digoxin toxicity
Mg++
Na-K-ATPase blocker
Inc refractory period and dec AV node conduction time
Digoxin
For SV arrythmias and CHF
Digoxin
Low molecular weight heparin
Enoxaparin
Acts more on factor Xa
Enoxaparin
Better availability, 2 to 4 times longer half-life
Enoxaparin
Can be administered subcutaneously without laboratory monitoring
Enoxaparin
Interferes with normal synthesis and y-carboxylation of vitamin K-dependent clotting factors II, VII, IX and X
Warfarin
Affects extrinsic pathway
Warfarin
Acetylates and irriversibly inhibits cyclooxygenase (both COX-1 and COX-2) to prevent conversion of arachidonic acid to TXA2
Aspirin
Inhibit platelet aggregation by irreversibly blocking ADP receptors
Clopidogrel, Ticlopidine
Nitrogen mustards
Mechlorethamine
Alkylation
Methochlorethamine
Metabolized in the P450 system
Cyclophosphamide
Drugs for brain tumors
Carmustine, Lomustine
Specially toxic to beta cells of Islets of Langerhans
Streptozocin
Treatment for insulinomas
Streptozocin
Adverse effects of Nitrosureas
CNS toxicity
Nausea and vomiting
Bone marriw suppression
SKIN FLUSHING
Platinum coordination complex
Carboplatin, Cisplatin
Adverse effects of Cisplatin
Nephrotoxicity
Ototoxicity
Paresthesia
AXONAL NEUROPATHY
Binds to double helix of DNA and for complex with it that inhibits RNA polymerase
Dactinomycin
For Wilm’s tumor
Dactinomycin
Kaposi sarcoma
Dactinomycin
Adverse effects: bone marrow suppression, skin reactions, GI irritation
Dactinomycin
Drugs that can cause pulmonary fibrosis
Bleomycin or Busulfan
Amiodaron
Nitrofurantoin
Methotrexate
Folic acid antagonist that prevents conversion of dihydrofolate to tetrahydrofolate and decreases synthesisnof thymidilate, aa, purine nucleotides
Methotrexate
Purine analog
6-Mercaptopurine
For ALL and AML
6-Mercaptopurine
Adverse effects: Bone marrow, hepatotoxicity
Used as oral
6-Mercaptopurine
Pyrimidine analog
Cytarabine
5-Fluorouracil
For treating AML only
Cytarabine
Inhibits thymidilate synthetase
Also inhibits RNA synthesis
5-Fluorouracil
For breast cancer and GI cancer
5-Fluorouracil
For Hodgkin’s disease, testicular CA
AE: bone marrow suppression
Vinblastine
For hodgkin’s lymphoma, leukemias, Wilm’s tumor, Ewing’s sarcoma
AE: peripheral neuropathy
Vincristine
Prevent the formation of mitotic spindle
Vinca Alkaloids
Inhibits topoisomerase I
Camptothecins
Inhibit topoisomerase II
Podophyllotoxins
Inhibits DNA topoisomerase II-DNA complex
Single stranded DNA breaks
Etoposide
Promote microtubule assembly and stabilization thus inhibiting cell division
Taxanes
Promotes microtubule formation butbprevents dissassembly
Malformed microtubules
Paclitaxel
For Ovarian and Breast CA
Paclitaxel
Estrogen antagonist
Tamoxifen
Competitive inhibitor of estradiol
Tamoxifen
Treatment of ER + breast ca
Tamoxifen
Inhibits translocation of androgen receptor to the nucleus
Flutamide
For prostate ca
Flutamide
Inhibits release of FSH and LH
Leuprolide
For prostate CA and endometriosis
Leuprolide
May trigger apoptosis and may even work on nondividing cells
Prednisone
Used in CLL, Hodgkin’s lymphomas
Prednisone
Toxicities associated with steroid use
Prednisone
Philadelphia chromosome bcr/abl tyrosine kinase inhibitor
Imatinib (Gleevec)
Used for CML, GI stromal tumors
Imatinib (Gleevec)
Toxicity: fluid retention
Imatinib (Gleevec)
Monoclonal antibody against HER-2 (erb-B2)
Trastuzumab (Herceptin)
Helps kill breast cancer cells that overexpress HER-2, possibly through antibody dependent cytotoxicity
Trastuzumab (Herceptin)
Used for metastatic breast cancer
Tradtuzumab (Herceptin)
Toxicity: cardiotoxicity
Trastuzumab (Herceptin)
Degrades asparagine
L-asparaginase
Childhood ALL
L-asparaginase
Bactericidal
Aminoglycosides Quinolone Cycloserine Vancomycin Carbapenems Penicillins Cephalosporins
All anti-TB meds are bactericidal except
Ethambutol
Bacteriostatic
Chloramphenicol Nitrofurantoin Clindamycin Tetracycline Erythromycin Trimethoprim Lincomycin Sulfonamides Ethambutol
Can penetrate the CNS if meninges are inflamed (menigitis)
Penicillin
1st gen cephalosporins
CEFAdroxil CEFAzolin CEPHAlexin CEPHAlothin CEPHApirin CEPHradin
2nd gen cephalosporins
CEFmetazole CEFAclor CEFAmandole CEFOxitin CEFOtetan CEFOranide CEFUroxime COFOnicid
3rd gen cephalosporins
CefoTaxime CefTazidime CefTriaxone CefbuTen Cefoperazone Cefixime
4th gen cephalosporin
Cefipime
Increased activity against pseudomonas and gram positive organisms
Cefipime
Resistant to B-lactamase
Carbapenems
Usually combined with CILASTATIN to prevent inactivation by dihydropeptidase enzyme in the brush border of proximal tubule
Imipenem
Adverse effects: seizures, GI effects
Imipenem
Binds to D-alanyl-D-alanine portion of cell wall precursors that inhibits peptidoglycan ploymerization
Vancomycin
Blocks transfer of peptidoglycan unit to growing cell wall
Bacitracin
For topical use only
Bacitracin
Analog of D-alanine 2nd line drug for TB
Cycloserine
Because of potential toxicity, should be employed only in well-defined and indicated conditions
Chloramphenicol (Chloromycetin)
Adverse reaction of Chloramphenicol
Anemia
Aplastic anemia
Gray baby syndrome
Bone marrow suppression
They lack UDP-glucuronyl transferase
Gray baby syndrome
Narrow spectrum antibiotic used as a substitute for penicillin G
Erythromycin
Antimicrobial activity:
Very effective against gram-positive bacteria
Bacteriostatic at low concentrations
Bacteriocidal at high concentrations
Erytnhromycin
Macrolide drugs
Erythromycin (prototype)
Clarithromycin
Azithromycin
Anti-TB causing hepatitis
Pyrazinamide
Increased bioavailability of erythromycin
Digoxin
Inhibits protein synthesisnby binding to 50s subunitnof bacterial ribosome (like erythromycin)
Clindamycin
Exhibits cross-resistance with macrolides
Clindamycin
Clinical use of Clindamycin
Tx of severe anaerobic infections
Treat penetrating wounds of abdomen and gut
Female genital tract infections
Aspiration pneumonia
Drug thatbm is very specific for Neisseria only
Spectinomycin
Fluoroquinolones
Norfloxacin
Levofloxacin
Ciprofloxacin
Ofloxacin
DNA gyrase inhibitor (topoisomerase II)
Fluoroquinolones
Modern sulfa drugs
Sulfonamides
PABA analog
Sulfonamides
Most common cause of SJS
Sulfonamides
Adverse effects of Trimethoprim
Megaloblastic anemia
Leukopenia
Granulocytopenia
Dihydrofolate reductase inhibitor
Trimethoprim
Antifungal drugs
Amphotericin B Flucytosine Ketoconazole Fluconazole Itraconazole Grieseofulvin Terbinafine
DOC for systemic mycotic infection
Amphotericin B
Binds to ergosterol
Amphotericin B
Inhibits thymidylate synthethase
Flucytosine
For cutaneous chronomycoses
Flucytosine
Antifungals for superficial infection
Griseofulvin Nystatin Miconazole Clotrimazole Econazole
Inhibits microtubule function
Griseofulvin
Used to treat aspergillosis
Caspofungin
Inhibits mycolic acid
Isoniazid
Antifreeze
Metabolic acidosis
Ethyl glycol
Snowstorm blindness
Methanol
Adverse effects: gout, arthralgia, myalgia
Pyrazinamide
Adverse effects: optic neuritis or red-green blindness, gout
Ethambutol
Leprosy meds
Dapsone
Clofazimine
Rifampicin
Used for both MTB and leprosy
Rifampicin
Antistaphylococcal Penicillins
Methicillin Nafcillin Oxacillin Dicloxacillin Cloxacillin
Drug that can cause interstitial nephritis
Methicillin
Antipseudomonal penicillin
Mezlocillin Piperacillin Azlocillin Carbenicillin Ticarcillin
Drug that can cause platelet dysfunction
Ticarcillin
Carbenicillin
Binds to outer membrane thereby disrupting membrane integrity
Aminoglycosides
Binds to 30s ribosomal unit
Aminoglycosides
Accumulat in the renal cortex and endolymph of the inne ear
Aminoglycosides
Postantibiotic effect: concentration dependent, explains why it can be given in single daily doses depsite the short half-life
Aminoglycosides
All are given IV except for neomycin which is given topically
Aminoglycosides
For aerobic gram negative enteric bacteria such as E coli, Enterobacter, Klebsiella, Pseudomonas
Aminoglycosides
Adverse effects: the triple punch of “a mean guy”
Ototoxicity
Nephrotixicity -> acute tubular necrosis
Neuromuscular blockade
Aminoglycosides
Must not take with milk or antacids that are divalent cations inhibit its absorption in the gut
Tetracyclines
Most common side effects of tetracyclines
Nausea and vomiting
Narrow spectrum antibiotic used as a substitute for penicillin G
Erythromycin
