Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
816 Cards in this Set
- Front
- Back
Mechanism of action of Ethambutol? Side effect?
|
Blocks carb polymerization (TB). Visual acuity issues, color blindness.
|
|
Side effect of chloramphenicol
|
aplastic anemia
|
|
Side effect of dapsone
|
agranulocytosis
|
|
Side effect of bactram
|
megaloblastic anemia (folate)
|
|
Mechanism of action and side effect of rifampin
|
Inhibit bacterial DNA dependent RNA polymerase. Side effects = orange body secretions.
|
|
Mech of action and Side effect of Cipro.
|
Fluoroquinolones mess with DNA unwinding-winding by blocking DNA gyrase.
|
|
Mechanism of Amphotericin B?
|
Interferes with egosterol binding and causes pore formation and lysis
|
|
Mechanism of Itraconazole?
|
Inhibits ergosterol synthesis
|
|
Mechanism of Terbinafine?
|
For fungal nail infections. Inhibits squalene 2,3-epoxidase causing decreased ergosterol synthesis
|
|
Mechanism of Griseofulvin?
|
blocks microtubules stopping mitosis - only dermatophyte fungi
|
|
Mechanism of Flucytosine?
|
targets DNA and RNA in fungal cells. Synergistic with amp B. Good for coccidio meningitis.
|
|
Mechanism of echinocandins? Capsofungin?
|
Blocks polysacchardie glucan in CELL WALL
|
|
Mechanism of Leuprolide?
|
GnRH analog - for prostate cancer.
|
|
Function of Norepinephrine?
|
Acts alpha 1 - increase SVR. Acts B1 - increase contractility.
|
|
Function of Isoproterenol?
|
Activates B1 and B2. B1 does increased contractility. B2 does decreased SVR.
|
|
Function of Phentolamine?
|
peripheral alpha blocker - vasodilation
|
|
Function of Labetalol?
|
Beta blocker - decrease contractility. A1 blocker - decrease SVR.
|
|
Phenylephrine effects?
|
Alpha1>alpha2
Increase SVR. |
|
What is the function of Anastrazole?
|
Blocks aromatase conversion. For breast cancer treatment. Similar to Letrozole and exemestane
|
|
What is the function of Ketoconazole?
|
Decreases androgen synthesis. An antifungal.
|
|
What is Tamoxifen?
|
Blocks ligand-receptor interaction of estrogen in breast tissue. Can cause endometrial hyperplasia.
|
|
What is Trastuzumab?
|
Blocks EGF-HER/neu-2 interactions. For Breast cancer.
|
|
What do Beta Blockers inhibit?
|
Renin
|
|
What are the teratogenic effects of Lithium?
|
Ebstein's anomaly
|
|
What is the function of Zileuton?
|
Lipoxygenase inhibitor. For allergic rhinitis and asthma.
|
|
What does finasteride do?
|
Inhibits 5alpha reductase. Stopping conversion of testosterone to DHT.
|
|
What is Rifampin tell tale sign? How is resistance to it mediated?
|
Orange body secretions. Inhibits DNA dependent RNA synthesis.
Resistance - altering structure for RNA synthesis. |
|
What does Isoniazid require for functioning? How does TB develop resistance?
|
Blocks mycolic acid syntehsis.
Needs bacterial catalase-peroxidase. Requires this for functioning. Decreasing this activity = resistance. |
|
What is reserpine?
|
Blocks adrenergic mediator storage in presynaptic vesicles!
Decreased NE, dopamine, 5HT |
|
What is pyrimethamine used to treat?
|
malaria and toxo
|
|
What is used to treat listeria meningitis?
|
Ampicillin
|
|
What antibacterial activity do 1st generation cephalosporins cover?
|
Gram positive cocci, E coli
|
|
What bacteria do 2nd generation cephalosporins cover?
|
gram positive coccci, some anaerobes, H flu
|
|
What bacteria do 3rd generation cephalosporins cover?
|
Gram negative bacteria - pseudomonas, enterobacter, h flu, neisseria
|
|
What bacteria do 4th generation cephalosporins cover?
|
Gram neg bacteria, gram positive bacteria
|
|
Mechanism of aminoglycoside?
|
30S subunit. Inhibits formation of initiation complex, causing misreading of mRNA
|
|
Mechanism for tetracyclines?
|
30S inhibitor. Prevents attachment of aminoacyl-tRNA to acceptor site
|
|
Mechanism for chloramphenicol?
|
50S inhibitor. Inhibits peptidyl trasnferase. Enzyme that incorporates new amino acid into growing peptide strand
|
|
Mechanism for erythromycin?
|
50S inhibitor. Blocks aminoacyl-tRNA complex translocation step.
|
|
Mechanism for Lindomycin?
|
50S inhibitor. Blocks aminoacyl-tRNA complex translocation step.
|
|
Mechanism for Clindamycin?
|
50S inhibitor. Blocks initiation complex formation and inhibits aminoacyl-tRNA complex translocation step.
|
|
Mechanism for sulfonamides?
|
Block dihydropteroate synthase. Structural analog of PABA, precursor for dihydrofolic acid.
|
|
Mechanism for trimethoprim?
|
Inhibits bacterial dihydrofolic acid reductase.
|
|
Mechanism for gamma Globulins?
|
block adsorption and penetration
|
|
Mechanism for amantadine?
|
Blocks uncoating of viral nucleic acid.
|
|
Mechanism for reverse transcriptase inhibitors?
|
Block synthesis of nucleic acids
|
|
Mechanism for rifampin?
|
Blocks assembly of viral particles
|
|
Mechanism for neuraminidase inhibitors?
|
Block release of viral particles from the host cell.
|
|
Mechanism for amphotericin B?
|
Binds ergosterol and causes the formation of holes in the fungal cell membrane
|
|
Mechanism for flucytosine?
|
Converted to nucleotide analogues by fungal enzymes and then acts to inhibit DNA and RNA synthesis
|
|
Mechanism for miconazole, fluconazole, clotrimazole?
|
Reduces ergosterol synthesis by inhibiting fungal cytochrome p-450 enzymes
|
|
Mechanism for caspofungin?
|
Disrupts fungal cell wall synthesis
|
|
Uses for pentamidine?
|
PCP prophylaxis, alternative treatment for Trypanosoma brucei and Leishmaniasis
|
|
Uses for nifurtimox?
|
Chagas disease
|
|
Use for suramin?
|
T brucei infection pre CNS
|
|
Use for melarsoprol?
|
T brucei after CNS
|
|
Use for sodium stibogluconate?
|
Leishmaniasis
|
|
Use for Ivermectin?
|
Onchocerciasis
|
|
Use for Mebendazole/Albendazole/thiabendazole?
|
Roundworm (ascaris), whipworm, hookworm, pinworm
|
|
Use for pyrantel pamoate?
|
Roundworm, hookworm, pinworm
|
|
Use for praziquantel?
|
Fluke (schistosomes), agent of choice for cysticercosis
|
|
Use for niclosamide?
|
Tapeworm, except cysticercosis
|
|
Pencillin Mechanism of action?
|
Binds penicillin binding proteins, blocking peptidoglycan cross linking.
|
|
Clinical uses for penicillin?
|
Gram positive cocci (step, enterococci), gram neg like Neisseria, and spirochetes like syphilis
|
|
Side effects of PCN?
|
Allergic reaction, Coombs positive hemolytic anemia
|
|
Mechanism of ampicillin?
|
Binds PBPs, blocking peptidoglycan cross linking.
|
|
Clinical uses for ampicillin?
|
Treats infections by gram negative rods - H flu, e coli, listeria, proteus, salmonella
as well as gram positive and negative cocci |
|
Side effects of amoxicillin/ampicillin?
|
Nonallergenic skin rash
|
|
Functions of clavulanic acid and sulbactam?
|
Inactivate bacterial B-lactamases. Added to broaden coverage for ampicillin and amoxicillin.
|
|
Drugs similar to methicillin?
|
Nafcillin, oxacillin, dicloxacillin
|
|
Mechanism of methicillin
|
Bind PBPs, blocking peptidoglycan cross-linking.
|
|
Clinical uses of methicillin?
|
Used for Staph infections. Inactive against enterococci, anaerobic bacteria, gram-negatives.
|
|
Side effects of methicillin?
|
Interstitial nephritis.
|
|
Side effect of nafcillin?
|
Neutropenia
|
|
Side effect of oxacillin?
|
hepatitis
|
|
What is methicillin's special feature?
|
B lactamase resistant
|
|
Mechanism of piperacillin?
|
Binds PBPs, blocking peptidoglycan crosslinking
|
|
Clinical use of piperacillin?
|
Treats Pseudomonas. and other gram negative rods like Klebsiella
|
|
Function of tazobactam?
|
Acts to inactivate bacterial Beta lactamases. Added to piperacillin to extend coverage to other gram neg organisms and Staph aureus.
|
|
Mechanism of aztreonam?
|
Monocyclic Beta-lactam ring binds PBPs, blocking peptidoglycan cross-linking.
|
|
Coverage for aztreonam?
|
GRAM NEGATIVE RODS - klebsiella and serratia.
|
|
Uses for aztreonam?
|
Pts allergic to PCN. Patients who are renally insufficient with gram negative infections who can't take aminoglycosides.
|
|
What is the mechanism of imipenem?
|
Binds PBPs, thereby blocking peptidoglycan cross linking.
|
|
Clinical uses for imipenem?
|
Broad spectrum antibiotic, used to treat infections from Enterobacter, anaerobes, pseudomonas. Enterococci, gram negative rods esp Klebsiella. Can't treat VRE or MRSA.
|
|
Side effects of imipenem?
|
Seizures at high serum levels esp renal insufficient patients.
|
|
What is cilastatin?
|
Inhibits renal dihydropeptidase I - so imipenem isn't inactivated in renal tubules.
|
|
Side effects of cephalosporins?
|
hypersensitivity rxn (10% of pts with PCN allergy)
Disulfiram-like activity with EtOH |
|
Mechanism for gentamicin?
|
30S inhibitor. Inhibits formation of initiation complex - mRNA misreading.
|
|
Drugs similar to gentamicin?
|
aminoglycosides - streptomycin, amikacin, neomycin, tobramycin
|
|
Clinical uses for aminoglycosides?
|
Severe gram negative rod - sepsis, chronic UTI, endocarditis, pneumonia, Pseudomonas.
|
|
Use for neomycin?
|
Prep for bowel surgery
|
|
Use for streptomycin?
|
TB regimen. Tularemia.
|
|
Side effects of aminoglycosides?
|
Nephrotoxicity, ototoxicity.
|
|
What do aminoglycosides require to function?
|
O2. not good against anaerobes
|
|
Uses of clindamycin?
|
Anaerobes - B fragilis, C perfringens. Some gram positive cocci like strep and staph.
Severe anaerobic infections above the diaphragm. |
|
Side effects of clindamycin?
|
Pseudomembranous colitis from C diff.
|
|
What is linezolid?
|
other 50S inhibitor to prevent formation of ribosomal complex. Treats MRSA and VRE.
|
|
clinical uses for chloramphenicol?
|
Broad spectrum - gram positive and negative like rickettsia, H flu, Neisseria, pneumoccocus, bacteriodes.
alternative treament for bacterial meningitis in pts intolerant of penicillins |
|
Side effects for chloramphenicol?
|
dose dependent anemia. Dose independent aplastic anemia.
Gray baby syndrome - due to lack of UDP-glucuronyl transferase in newborn liver. |
|
What drugs are like erythromycin?
|
Macrolides. Azithromycin, clarithromycin.
|
|
Uses for erythromycin?
|
Gram positive cocci, Corynebacteria like diphtheria, atypical pneumo.
atypical URIs, some stds like chlamydia, H pylori. |
|
Side effects for erythromycin?
|
GI upset. Acute cholestatic hepatitis. Eosinophilia.
|
|
Special notes for erythromycin?
|
Inhibits cyt p-450. Increased levels of warfarin, cyclosporine, theophylline.
|
|
Drugs like tetracycline?
|
Doxycycline, minocycline, demeclocycline.
|
|
Uses for tetracycline?
|
Mycoplasma, Chlamydia pneumonia. Lyme disease. Rocky mountain spotted fever. Cholera. STD chlamydia. Tularemia, brucellosis.
|
|
Side effects for tetracycline?
|
Fanconi syndrome. Teeth discoloration and bone deformity in children. Photosensitivity.
|
|
Who can doxycycline be used with?
|
Renal insufficient. Fecal elimination.
|
|
What should you not take tetracyclines with?
|
Divalent cations inhibiting absorption of tetracyclines - antacids, milk, iron containing substances.
|
|
What can demeclocycline also be used for?
|
Binds V2 receptors. Treatment of SIADH.
|
|
Clinical uses of TMP-SMX?
|
E coli, Nocardia, P carinii.
Used for UTIs like for E coli, PCP. |
|
Side effects of TMP-SMX?
|
SJS, hemolytic anemia, kernicterus in newborns. Granulocytopenia from folic acid drop.
|
|
Mechanism of ciprofloxacin?
|
Inhibits DNA topoisomerase II. Induces DNA strand breakage and death.
|
|
Clinical uses for fluoroquinolones?
|
Gram negs and newer ones like gatifloxacin, moxifloxacin, and levofloxacin have increased activit with gram positive like pneumococcus.
Used for UTIS, Pneumonias and gonococcal. |
|
Side effects of fluoroquinolones?
|
Tendonitis, tendon rupture.
|
|
Contraindications for fluoroquinolones?
|
Pregnant women and chilren.
|
|
What is nitrofurantoin?
|
Used for recurrent UTIs. Side effects - anemia in G6PD patients.
|
|
What is vancomycin's mechanism?
|
Binds D-ala D-ala terminus inhibiting transglycosylase. Results in weakened peptidoglycans in cell wall.
|
|
Clinical uses for vancomycin?
|
Gram positive bacteria. MRSA infections. C diff.
|
|
Side effects of vancomycin?
|
Ototoxicity, Nephrotoxicity, Red Man syndrome.
|
|
What are polymyxins?
|
Bind bacterial cell membranes and increase permeability of cell membrane to polar molecules. Only used topically to treat infected skin lesions due to high nephrotoxicity and neurotoxicity.
|
|
What is mechanism of action of metronidazole?
|
Metabolized by bacterial proteins into reduced reactive compounds that damage DNA, protein, and membranes LEADING TO CELL DEATH
|
|
Uses for metronidazole?
|
Anaerobic below the diaphragm
Trich Giardia Ameba H pylori (with tetracyline or amoxicillin) |
|
Side effects of metronidazole?
|
disulfiram like activity, metallic taste. Potentiates anticoagulants like warfarin.
|
|
Mechanism of rifampin?
|
Inhibits bacterial DNA-dependent RNA polymerase, decreasing NRA synth.
|
|
Uses for Rifampin?
|
Mycobacteria. TB and leprosy.
Prophylaxis for contacts for meningococcus and H flu type B |
|
Side effects of rifampin?
|
harmless orange color to urine and sweat. Hepatitis. Thrombocytopenia. Nephritis.
Induces cytochrome p-450 system - increasing metab of warfarin, OCs, prednisone, digoxin, glyburide |
|
Mechanism of Isoniazid?
|
Inhibits the synthesis of mycolic acids.
|
|
Uses for Isoniazid?
|
Treatment of mycobacterium tb.
Prophylaxis against active TB |
|
Side effects of Isoniazid?
|
Peripheral neuropathy. Drug-induced lupus, hepatitis. Give B6 (pyridoxine) for the peripheral neuropathy.
Metabolism varies depending on rate of N-acetyltransferase in liver. |
|
Medications other than rifampin and isoniazid used to treat TB?
|
ethambutol, pyrazinamide, dapsone
|
|
Mechanism of action of dapsone?
|
PABA antagonist inhibits folic acid synthesis
|
|
Mechanism of action of Ethambutol?
|
Inhibits mycobacterial arabinosyl transferase, enzyme part of cell wall.
|
|
Mechanism of action of pyrazinamide?
|
unknown
|
|
Use for dapsone?
|
Used in combination with rifampin and clofazimine to treat M leprae.
PCP prophylaxis in HIV pts |
|
Use for ethambutol and pyrazinamide?
|
TB
|
|
Side effects of dapsone?
|
G6PD deficient hemolytic anemia
|
|
Side effects of ethambutol?
|
Retrobulbar neuritis - red/green color blindness
|
|
Side effects of pyrazinamide?
|
Hepatotoxicity! Gout
|
|
Drugs that are nucleoside reverse transcriptase inhibitors?
|
Zidovudine (AZT), didanosine, zalcitabine, lamivudine, stavudine, emtricitabine, abacavir
|
|
Mechanism of action of NRTIs?
|
Inhibit HIV reverse transcriptase inhibiting DNA synthesis. Also compete with nucleoside triphosphates to be added to the newly synthesized viral DNA strand.
|
|
Uses for NRTIs?
|
treatment of HIV
|
|
Use for lamivudine?
|
Chronic hep B
|
|
Side effects of zidovudine?
|
Megaloblastic anemia
|
|
Side effects of didanosine?
|
pancreatitis
|
|
What are examples of nucleotide analg reverse transcriptase inhibitors?
|
tenofovir, adefovir. Treat HIV infection. Inhibit reverse transcriptase.
Adefovir - hep B too |
|
Examples of non-nucleoside reverse transcriptase inhibitors?
|
Nevirapine, efavirenz, delavirdine
|
|
Mechanism of non-nucleoside reverse transcriptase inhibitors?
|
speficially to HIV reverse transcriptase
|
|
Uses for NNRTIs?
|
HIV
|
|
Side effects of nevirapine?
|
SJS, inudction of cytochrome p-450 - increased metab of OCs, warfarin, ketoconazole, metronidazole
|
|
Side effects of efavirenz?
|
CNS disturbances
|
|
What are some protease inhibitors?
|
Saquinivir, ritonavir, indinavir, nelfinatvir, lopinavir, atazanavir, fosamprenavir, tipranavir, darunavir, amprenavir
|
|
Mechanism of action of protease inhibitors?
|
Inhibit the HIV protease enzyme - virus is unable to replicate
|
|
Clinical use for protease inhibitors?
|
HIV
|
|
Side effects of protease inhibitors?
|
Altered distribution of body fat (buffalo hump), hyperlipidemia
Ritonavir inhibits cytochrome p-450 - increased levels of ketoconazole, rifampin, erythromycin |
|
Mechanism of action of acyclovir?
|
Phosphorylated by viral thymidine kinase into an analogue of dGTP. After conversion, this drug acts to inhibit DNA synthesis through incorporation into the growing viral DNA strand. Chain termination.
|
|
Uses for acyclovir?
|
active against HSV 1, 2, VZV, EBV
genital herpes, herpes encephalitis |
|
Side effects of acyclovir?
|
Neurotoxicity
can crystallize if given really quickly in kidneys so hydrate |
|
Mechanism of action of ganciclovir?
|
Guanosine analog. After phosphorylation by a viral kinase into a nucleotide analogue, acts to preferentially inhibit CMV DNA polymerase.
|
|
Drugs like acyclovir?
|
valacyclovir, penciclovir, famciclovir
|
|
Uses for Ganciclovir?
|
CMV infections. Especially retinitis.
|
|
Side effects of ganciclovir?
|
Pancytopenia.
|
|
Mechanism of foscarnet?
|
Pyrophosphate analog inhibits viral DNA polymerase.
(can also affect reverse transcriptase) |
|
Uses for foscarnet?
|
second line treamtnet of CMV retinitis and other CMV infections and acyclovir-resistant HSV and VZV.
|
|
Side effect of foscarnet?
|
Nephrotoxicity Mg wasting, leading to low Ca
|
|
Mechanism of action of amantadine?
|
Binds to the M2 surface protein proton channel on influenza A viral particles. Blocks uncoating of viral RNA.
Stimulates the release of dopamine from neurons of the nigra striatum |
|
Uses for amantadine?
|
Reduces duration of influenza A symptoms.
Parksinon's |
|
Side effects of amantadine?
|
CNS symptoms - ataxia, slurred speech, dizziness
|
|
What is zanamivir?
|
Inhibits neruaminidase. Viral enzyme necessary for viral replication and release of viral particles.
|
|
Uses for zanamivir?
|
Treatment and prophylaxis of both influenza A and B
|
|
Mechanism of ribavirin?
|
Guanosine analog. Inhibits guanine nucleotide synthesis and inhibits viral RNA polymerase. Inhibits viral replication.
|
|
Uses for ribavirin?
|
RSV bronchiolitis
|
|
When is ribavirin contraindicated?
|
Pregnancy and pts with renal insufficiency
|
|
What is entecavir?
|
Guanosine nucleoside analog - inhibits hep B viral polymerase. Treats hep B infection.
|
|
Mechanism of Amphotericin B?
|
Binds to ergosterol, alters permeability of the fungal cell membrane
|
|
Clinical uses for amphotericin B?
|
Systemic mycotic infections.
Intrathecally for meningitis since doesn't cross BBB |
|
side effects of amphotericin B?
|
Nephrotoxicity
|
|
What is nystatin?
|
Similar mode of action to amp B. Treats oral and cutaneous candidiasis. Too many side effects for systemic.
|
|
Mechanism of flucytosine?
|
converted into nucleotide analogues within fungal cell, inhibits thymidylate synthetase, inhibits fungal DNA and RNA synthesis
|
|
Uses for flucytosine?
|
In combo with other antifungal agents usually amp B for treatment of systemic mycotic infections and fungal meningitis (crypto/candida)
|
|
Mechanism of Caspofungin? Use?
|
Inhibits enzyme B(1,3)-D-glucan synthase, disruption of cell wall. Treats candidemia, aspergillosis.
|
|
Mechanism of Ketoconazole?
|
Inhibits formation of ergosterol by inhibiting fungal cytochrome p-450 enzymes.
Affect gonadal and adrenal steroid synth |
|
Use for Ketoconzole?
|
broad-spectrum antifungal agent. Blast, Coccidio, Hiisto, Aspergillus, Mucor, Candida.
Also Cushing syndrome |
|
Side effects of ketoconazole?
|
Gynecomastia.
Inhibits cytochrome p-450 - higher levels of warfarin, phenytoin |
|
What are miconazole and clotrimazole?
|
Like ketoconzole. Limited to treat cutaneous fungal infections due to high levels of toxicity.
|
|
Mechanism of fluconazole?
|
Inhibits formation of ergosterol by inhibiting fungal cytochrome p-450. Not as much effect on gonadal and adrenal steroid synthesis are minimal.
|
|
Use for fluconazole?
|
Crypto meningitis. Treatment for Candidal sepsis.
|
|
Mechanism of Griseofulvin?
|
Interferes with microtubule function in fungal cells in keratin-rich tissues.
|
|
Uses for griseofulvin?
|
Oral antifungal agent for treatment of topical dermatophytic infections.
|
|
What is terbinafine? Use?
|
Inhibits qualene epoxidase (involved in ergosterol synth)
Treats topical dermatophytic infections |
|
Mechanism of action of chloroquine?
|
concentrates in parasite food vacuoles and prevents heme metabolism; leading to toxicity and cell death from buildup of soluble heme
|
|
Use for chloroquine?
|
Treatment of p falciparum malaria. Prophylaxis.
|
|
Use of quinine?
|
Treatment of drug resistant P falciparum
|
|
Use of mefloquine?
|
Treatment of drug resistant P falciparum
|
|
Side effects of mefloquine?
|
Mental status changes
|
|
Side effects of quinine?
|
cinchonism (tinnitus, headache, dizziness, nausea). coombs positive hemolytic anemia.
CONTRAINDICATED IN PREGNANCY |
|
Side effects of chloroquine?
|
GI upset, visual disturbances
|
|
Use for primaquine?
|
Hepatic forms of p vivax and ovale. G6PD anemia.
|
|
Mechanism of nifurtimox?
|
Generates oxygen radicals. Damages parasite.
|
|
What drugs provides prophylaxis for PCP and alternative treatment of T brucei?
|
Pentamidine
|
|
Mechanism of Ivermectin?
|
Activates GABA receptor sleading to worm paralysis and death
|
|
Mechanism for Mebendazole/albendazole/thiabnediazole?
|
Inhibits microtubule synthesis and function
|
|
Mechanism of pyrantel pamoate?
|
Activates parasitic nictoninic receptors, causing worm paralysis
|
|
Mechanism of praziquantel?
|
Increases cell Ca uptake, causing parasitic contraction and paralysis
|
|
Mechanism of Niclosamide?
|
Inhibits worm production of ATP
|
|
Action of alpha1 adrenergic receptor?
|
PLC activated --> IP3 and DAG --> Ca
Induce heart contractiliy. Vasoconstriction. Eye dilation |
|
Action of alpha 2 adrenergic receptor?
|
AC inhibited --> decreased cAMP
Inhibit release of neurotransmitters for nerve terminals |
|
Action of Beta 1 adrenergic receptor?
|
AC activated --> increase cAMP
Heart rate and contractility improve |
|
Action of Beta 2 adrenergic receptor?
|
AC activated --> increased cAMP. Smooth muscle of respiratory, vascular, and uterine tissue.
Bronchodilation, vasodilation. |
|
Action of D1 adrenergic recetpros?
|
AC activated --> increased cAMP
Vasodilation of renal blood vessels |
|
Action of D2 adrenergic receptor?
|
Nerve terminals of CNS neurons - regulating nt release
|
|
Epinephrine actions?
|
Low doses - B agonist - increases heart rate and contractility = B1
B2 = bronchodilation high dose - alpha agonist - vasconstriction Cardiac arrest, severe hypotension, bronchospasm and anaphylaxis. Also given with local anesthetics due to its vasoconstriction so other parts of body not affected |
|
Functions of Norepinephrine?
|
Alpha 1, alpha 2, Beta 1 agonist.
Increased vasoconstriction with increased contractility - no change in heart rate. Treatment of severe hypotension and shock. See decrease in renal blood flow |
|
Function of dopamine as sympathomimetic?
|
B and D agonist at low doses.
Renal perfusion, increase in contractility and heart rate Alpha high - vasoconstriction. Pressor for treatment of severe hypotension and shock |
|
What is dobutamine?
|
B1 receptor agonist - increases CO. Side effects - peripheral vasodilation. Used for CHF or cardiogenic shock
|
|
Function of ephedrine?
|
Stimulates release of NE and epinephrine from neurons.
Increases systolic and diastolic blood pressure. Increases cardiac output. Bronchodilation. CNS - insomnia, decreases appetite, improved athletics. Nasal decongestant. |
|
How does amphetamine operate?
|
CNS entrance - stimulates release of NE, epinephrine, and Dopamine
see insomnia and decreased appetite. |
|
Functions of cocaine?
|
Inhibit Na/K ATPase responsible for reuptake of NE, serotonin, and dopamine. Can also block voltage gated Na channels.
can be used for local anesthetic |
|
Side effects of cocaine?
|
HTN, drug of abuse, cardiac ischemia, cardiac arrhtyhmias
|
|
What is Reserpine?
|
Inhibits neuron's ability to store NE, dopamine, serotonin. Used earlier to treat HTN, now rarely used bc causes depression and parkisonism.
|
|
What is Guanethidine?
|
Inhibits NE release from sympathetic neurons. Used to treat hypertension in the past. Rare due to orthostatic htn.
|
|
What is phenylephrine?
|
Alpha 1 agonist. Systemic vasoconstriction. Decrease in mucosal secretions. Pupil dilation.
Used for severe hypotension and shock. Nasal congestion. Produce mydriasis for retinal exam. |
|
Side effects for phenylephrine?
|
reflex bradycardia from vasoconstriction
|
|
What is Midodrine?
|
Alpha 1 agonist for hepatorenal syndrome and orthostatic hypotension.
|
|
What is clonidine?
|
Alpha 2 agonist. Stimulating these - the release of NE and other nts is reduced. Decreased central adrenergic activity - decrease in vasoconstriction and decrease in CO and HR.
Used for HTN |
|
Clonidine side effect?
|
Rebound HTN if withdrawn!
|
|
What is Isoproterenol?
|
B1 and B2 receptor agonist. Increases heart rate and contractility. Slightly increaseing systolic pressure.
B2 receptor - peripheral vasodilation and bronchodilation |
|
Uses for Isoproterenol?
|
Torsade de points with Mg
Treatment of cardiac arrest or complete heart block. |
|
What is Fenoldopam?
|
D1 receptor agonist - for splanchnic and renal vasodilation of severe htn.
|
|
What is Albuterol?
|
B2 receptor agonist - bronchodilation. Can also lead to K shifting into cell.
|
|
Uses for Albuterol?
|
Asthma.
Treating Hyperkalemia |
|
What is salmeterol?
|
Long acting B2 agonist - prevents asthmatic attacks.
|
|
What are terbutaline and ritodrine?
|
B2 receptor agonists - reduce uterine contractions during preterm labor.
|
|
What is methyldopa?
|
Alpha 2 agonist - reduces release of NE. Decreased central adrenergic activity with resulting decrease in vasoconstriction.
|
|
Use of methyldopa? Side effects?
|
Used for HTN
Can cause sedation and didzziness. |
|
What is phenoxybenzamine?
|
Irreversible alpha-receptor antagonist. Decrease in vasoconstriction.
|
|
Use for phenoxybenzamine?
|
Prevent HTN crisis in pheochromoctyoma.
|
|
What is phentolamine?
|
Reversible alpha receptor antagonist. Can dx pheochromocytoma if values far larger than expected.
|
|
Function of prazosin?
|
Selective alpha 1 antagonist. Blocking that - decrease in blood pressure. Also decreases prostatic and bladder neck contraction.
|
|
Use of prazosin?
|
HTN and BPH
|
|
Side effects of prazosin?
|
First dose syncope.
|
|
What is propranolol?
|
B1 and B2 receptor antagonist. Decreases HR and contractility. Reflex peripheral vasoconstriction. Total decreased blood pressure. Resultant bronchoconstriction from unopposed B2 blocking.
|
|
Clinical use of propranolol?
|
HTN, CAD CV disorders. Treatment of High HR with thyroid problems. Chronic migraines (cerebral vasodilation).
TREATS ESSENTIAL TREMOR |
|
Side effects of propranolol?
|
Bronchoconstriction; fasting hypoglycemia (decreased glycogenolysis from B2 blockage)
Really high toxicity, treat with glucagon |
|
What is pindolol?
|
weak B receptor agonist and B receptor antagonist. Treats pts with HTN and bradycardia.
|
|
What is timolol?
|
B1 and B2 receptor antagonist used for wide angle glaucoma. Decreases aqueous humor secretion.
|
|
What is carvedilol and labetalol?
|
Alpha receptor blockers as well as B receptor blockers. Used for CHF and refractory HTN respectively.
|
|
What is metoprolol?
|
Selective B1 receptor antagonist. Decreasing heart rate and contractility.
|
|
Uswe for metoprolol?
|
CAD and HTN. Esp in DM pts.
|
|
What is betaxolol?
|
Selective B1 receptor antagonist. Wide angle glaucoma - reducing aqueous humor production.
|
|
What is esmolol?
|
short acting B1 receptor antagonist. Critically ill pts with arrhythmias, htn, MI.
|
|
What is acebutolol?
|
B1 receptor antagonist with small agonist powers. Hyptertension and bradycardia
|
|
What are hexamethonium, mecamylamine, and trimethaphan?
|
antinicotinic drugs.
Competitively inhibit activation of Nn receptors on postsynaptic neuron of the autonomic ganglia. |
|
Uses for hexamethonium, mecamylamine, and trimethaphan?
|
Treat HTN emergencies in the past.
|
|
Side effects of hexamethonium, mecamylamine, and trimethaphan?
|
Hypotension, tachycardia, sedation, urinary retention.
|
|
What is pilocarpine?
|
muscarinic receptor agonist. Applied topically at eye = M3 receptor.
contraction of sphincter muscle of iris - opening canal of Schlemm. Also opens trabecular muscle by contracting the ciliary muscle. |
|
Clinical uses for pilocarpine?
|
Narrow and wide angle glaucoma
|
|
What is carbachol?
|
Muscarinic and nicotinic receptor agonist. M3 stimulation in eye = miosis. Treats wide angle glaucoma or producing pupillary constriction.
|
|
What is bethanechol?
|
Muscarinic M2 and M3 agonist. Bladder contraction increased with relaxation of bladder sphincter. Promotes urination.
|
|
Use of bethanechol?
|
Treat bladder atony
|
|
Side effects of bethanechol?
|
M2 - bradycardia, hypotension
M3 - sweating salivation diarrhea |
|
What is atropine?
|
Competitive muscarinic receptor antagonist.
Blocking M1 - atropine can cause sedation and psychosis Blocking M2 - Tachycardia, mild vasdilation Blocking M3 - decreased GI tract motility, cycloplegia |
|
Uses for atropine?
|
Antidote for cholinesterase inhibitor poisoning (nerve gas, insecticide)
Treatment of bradycardia |
|
Side effects of atropine?
|
Hyperthermia, decreased salivation, flushing, psychosis
|
|
Treatment of atropine poisoning?
|
Cholinesterase inhibitor. Physostigmine or pralidoxime.
|
|
What is scopolamine?
|
Muscarinic antagonist at M1 receptors. Prevents motion sickness.
|
|
What are homatropine and tropicamide?
|
Atropine analogs used in ophthalmic solution --> mydriasis.
|
|
M1 receptor is?
|
CNS stimulation. ACh substrate.
PLC activated - IP3 and DAG - increased Ca |
|
M2 receptor is?
|
Heart. Decreases heart rate and contractility.
AC inhibited - decreased cAMP, increase in K conductance |
|
M3 receptor is?
|
PLC activated - increased IP3 DAG - increased intracellular Ca.
Increases gut peristalsis, increases bladder contraction, relaxes bladder sphincter, increases bronchoconstriction and respiratory secretions. contracts sphincter muscle - pupil constriction. loss of far off vision from ciliary muscle contraction. |
|
Nm receptor?
|
NMJ. Activates Na/K channel. Promotes muscle contraction.
|
|
Nn receptor?
|
Activation of Na/K channel.
ANS ganglia - vasodilation of renal blood vessels Adrenal medulla - stimulates epinephrine release. |
|
What does sulcralfate do?
|
Binds mucosal ulcers and provides physical protection against acid
|
|
What does cilostazol do?
|
for PAD. Stops platelet aggregation and is a direct arterial vasodilator.
|
|
What drug factor is related to drug-associated lupus? Which drugs?
|
N-acetylation in the liver. Procainamide and hydralazine.
|
|
What is Benztropine?
|
Muscarinic (M1, M2, M3) receptor antagonist. Acts on M1 receptors in corpus striatum to stop cholinergic activity, restoring dopaminergic-cholinergic balance.
|
|
What is benztropine used for?
|
Treatment for Parkinson Disease
ALSO MEDICALLY INDUCED PARKINSON |
|
For what is benztropine contraindicated?
|
narrow-angle glaucoma
|
|
What is ipratropium?
|
Muscarinic receptor antagonist. Mostly M3 = bronchodilation.
|
|
Uses for ipratropium?
|
COPD and asthma
|
|
What is propantheline?
|
Muscarinic receptor antagonist. primarily M3 - increasing bladder sphincter tone and decreases GI motility and secretions. Used for urinary incontinence and duodenal ulcers.
|
|
What is oxybutynin?
|
Muscarinic receptor antagonist. By blocking M3, increases bladder sphincter tone and decreases bladder spasm. Used for urinary incontinence.
|
|
What is neostigmine?
|
Reversibly inhibits acetylcholinesterase. Increasing stimulation of both nicotinic and muscarinic receptors.
|
|
What is use for neostigmine?
|
Treatment of myasthenia gravis.
Stimulating GI tract and bladder Overcomes nondepolarizing neuromusclar blockade |
|
What is physostigmine?
|
Another acetylcholinesterase inhibitor. Used for atropine poisoning. Also for treatment of glaucoma - producing miosis and stimulating outflow of aqueous humor.
|
|
What are edrophonium and pyridostigmine?
|
Reversibly inhibit acetylcholinesterase. Increase stimulation of both nicotinic and muscarinic receptors.
|
|
What does edrophonium do?
|
Used to dx myasthenia gravis
Can differentiate overmedication from under. Overmedication will get worse. |
|
What does pyridostigmine do?
|
Long term treatment of myasthenia gravis
|
|
What is tacrine? Same as donepezil
|
Reversibly inhibits acetylcholinesterase. Increase stimulation of both nicotinic and muscarinic receptors.
|
|
Use for tacrine?
|
Treatment of Alzheimer's.
|
|
What is echothiophate?
|
Inhibits acetylcholinesterase. Increases stimulation of both nicotinic and muscarinic receptors.
|
|
What is echothiophate and isofluorophate use?
|
Treat wide angle glaucoma through M3 receptor
|
|
What are side effects from echothiophate use?
|
Seizures, psychosis, GI upset, salivation , blurry vision, bradycardia.
|
|
What is pralidoxime?
|
Antidote for acetylcholinesterase inhibitors, reactivates acetylcholinesterase.
|
|
What drugs are like fluoxetine?
|
Paroxetine, sertraline, fluvoxamine, escitalopram, citalopram
|
|
Mechanism of fluoxetine?
|
Prevents reuptake of serotonin from synaptic cleft
|
|
Clinical use for fluoxetine?
|
Treat major depression, anxiety disorders, OCD, eating disorders
|
|
Side effects for fluoxetine?
|
sexual dysfunction (decreased libido, difficulty with libido)
also inhibits cyt450 - TCAs, haloperidol, antiarrhythmics if with MAOs - serotonin syndrome |
|
What drugs are TCAs?
|
Desipramine, nortriptyline, imipramine, amitrptyline, doxepin.
second generation - amoxapine, trazodone, bupropion |
|
What is the action of nortriptyline/amitryptiline/trazodone/bupropion?
|
block the reuptake of NE and 5HT
|
|
Clinical uses for TCAs?
|
Major depression, panic disorder, enuresis, chronic pain syndromes.
|
|
TCA for insomnia?
|
trazodone
|
|
Use for amitriptyline?
|
neuropathic pain
|
|
Use for bupropion?
|
Smoking cessation
|
|
Side effects of TCAs?
|
Inhibited muscarinic, histamine, alpha-adrenergic receptors.
Sedation - histamine Postural hypotension and cardiac arrhythmias - adrenergic Anticholinergic effect - dry mouth retention, blurred vision Priapism = trazodone |
|
What happens with simultaneous use of MAOis and TCAs?
|
seizures!
|
|
Overdosing on TCAs looks like?
|
EKG changes - widening of QRS complex
arrhythmias, mental status changes, seizures fix cardiac abnormalities - Sodium bicarb |
|
What are nefazodone, mirtazapine, venlafaxine, and maprotiline?
|
Heterocyclic antidepressants
|
|
What is the mechanism of nefazodone, maprotiline, and venlafaxine?
|
Block the reuptake of NE, 5HT from the synaptic cleft.
|
|
What is the mechanism of mirtazapine?
|
inhibits activation at alpha2-adrenergic receptors and at 5-HT2 receptors. Thereby increasing release of NE and 5HT.
|
|
Clinical uses for heterocyclic antidepressants?
|
depressive disorders and generalized anxiety disorder
|
|
Side effects for heterocyclic antidepressants?
|
sedation;
|
|
Side effect for mirtazapine?
|
Weight gain with increased appetite
|
|
Side effect for venlaxafine?
|
Elevated blood pressure and heart rate
|
|
What are some MAOIs?
|
tranycypromine, phenelzine, and isocarboxazid
|
|
Mechanism of action of MAOIs?
|
Levels of 5HT, dopamine, and NE increase in presynaptic neuron.
MAO A- 5HT and NE MAO B - dopamine |
|
Clinical uses for MAOIs?
|
treatment of atypical depression, specific phobias, and panic disorder
|
|
Side effects of MAOIs?
|
sedation, hypotension, blurred vision, weight gain
|
|
What is selegiline?
|
selectively inhibits mao B, increased dopamine for neuron. Good for Parkinson.
|
|
What is a risk for all MAOIs?
|
Hypertensive crises with tyramine contianing foods
|
|
What does serotonin syndrome look like?
|
changes in mental status, muscle stiffness, hyperthermia
treat with cyproheptadine |
|
Mechanism of Lithium?
|
Inhibits phosphoinositol second messenger cascade, may interfere with synthesis, storage, release, and reuptake of 5HT, dopamine, and NE.
|
|
Clinical use for Lithium?
|
Bipolar disorder
|
|
Side effects for Lithium?
|
tremor, hypothyroidism; nephrogenic diabetes insipidus (ADH antagonism) [hypernatremia, polyuria, polydipsia]
MONITOR LI LEVELS NOT IN PREGNANCY |
|
What are some typical antipsychotic agents?
|
Haloperidol and fluphenazine (high potency)
Chlorpromazine and thioridazine (low-potency) |
|
What is the mechanism of typical antipsychotics?
|
Block postsynaptic dopamine D2 receptors in the limbic system of the brain, decreasing response of postsynaptic neuron to dopamine excitation.
|
|
Clinical uses of typical antipsychotic agents?
|
positive symptoms of schizophrenia (delusions, hallucinations), Tourette syndrome, delirium and agitation
|
|
Side effects of typical antipsychotic agents?
|
Sedation - histamine blockade
Anticohlinergic Extrapyramidal side effects - acute dystonia, akinesia, akathisia, tardive dyskinesia Galactorrhea and amennorhea from dopamine inhibition |
|
What causes neuroleptic malignant syndrome?
|
antipsychotic agents = muscle rigidity, change in mental status, elevated temperature, autonomic instability.
Can be treated with Dantrolene (muscle relaxant) and dopamine agonists |
|
What are some atypical antipsychotic agents?
|
clozapine, risperidone, olanzapine, ziprasidone, aripriprazole, quetiapine
|
|
Mechanism of action of clozapine/risperidone?
|
Block both 5HT and dopamine receptors. Decreasing response of postsynaptic neuron to dopamine and 5HT excitation.
Some inhibition at H1 histamine receptor, cholinergic receptors, and alpha adrenergic receptors. But less than typical. |
|
Uses for clozapine/olanzapine/risperidone?
|
treat positive and NEGATIVE symptoms of schizophrenia.
Olanzapine, risperidone, and quetiapine can be used for delirium. |
|
Side effects of atypical antipsychotics?
|
mild weight gain
fewer anticholinergic and extrapyramidal side effects than regular psychotics |
|
Side effect of clozapine?
|
Agranulocytosis
|
|
What are the short acting benzodiazepines?
|
triazolam alprazolam, oxazepam
|
|
What are the intermediate acting benzodiazepines?
|
lorazepam, temazepam, estrazolam
|
|
What are the long-acting benzodiazepines?
|
diazepam, clonazepam, flurazepam, chlordiazepoxide
|
|
Mechanism of action of the benzodiazepines?
|
enhanced GABAa receptor activation - increase flow of chloride ion through adjacent chloride channels - hyperpolarization - decreased activity of the neurons of the limbic, thalamic, and hypothalamic regions of CNS
|
|
Use for Benzodiazepines?
|
Anxiety, seizures, status epilepticus
Alcohol withdrawal |
|
What are other uses for midazolam and diazepam?
|
anesthetics
|
|
What are side effects of benzodiazepines?
|
sedation; altered mental status; ataxia
Withdrawal symptoms - seen with dependence Avoid with barbiturates, EtOH, depressants |
|
What is benzo overdose like? Treat it?
|
Cardiac and respiratory depression. Treat with flumazenil - competitive antagonist of benzos at the GABA receptor.
|
|
What are some barbiturates?
|
phenobarbital, thiopental, secobarbital, amobarbital, pentobarbitol
|
|
Mechanism of action of barbiturates?
|
Potentiate GABAa receptor activity in the brain
decreases activity of CNS neurons |
|
Use for barbiturates?
|
sedative (anxiety and insomnia)
|
|
Use of thiopental?
|
induction of anesthesia
|
|
Use of phenobarbitol?
|
Management of seizures and in treatment of neonatal hyperbilirubinemia
|
|
How do you treat overdose of barbiturates? What does it look like?
|
cardiac and respiratory depression. Treatment with ventilation, hemodialysis, and alkalinization of the urine.
|
|
Side effects of barbiturates?
|
P-450 induction
withdrawal avoid in pregnancy, liver disease, porphyria, alcohol, benzos |
|
Mechanism of phenytoin?
|
decreases flow of Na and Ca across cell membrane. Decreased depolarization.
|
|
Uses for phenytoin?
|
simple and complex partial seizures; grand mal seizures, status epilepticus.
Trigeminal neuralgia and torsades de pointes |
|
Side effects of phenytoin?
|
Nystagmus, gingival hyperplasia, drug-induced lupus, fetal hydantoin syndrome (prenatal growth deficiency and congenital cardiac and palate malformations)
|
|
What is Lamotrigine?
|
Inhibits Na channels on neurons and release of glutamate from tissue.
for simple and complex partial seizures and generalized tonic-clonic seizures |
|
What is Valproic acid's mechanism?
|
Unknown. May increases GABA concentrations. Also has effects on Na and K conductance.
|
|
Clinical uses of valproic acid?
|
generalized tonic-clonic seizures, myoclonic seizures, absence seizures
Treatment of mania associated with bipolar disorder |
|
Side effects of valproic acid?
|
Hepatotoxicity; neural tube defects
|
|
What is ethosuximide?
|
Decreases Ca currents across neuronal cells. Inhibits GABA metabolis.
For absence seizures. |
|
What is Carbamazepine's mechanism of action?
|
Inhibits flow of sodium ions through sodium channels. Hyperpolarization.
|
|
What are clinical uses for carbamazepine?
|
Partial seizures
Trigeminal neuralgia |
|
Side effects of carbamazepine?
|
hepatotoxicity, agranulocytosis, aplastic anemia
induces p-450, like phenytoin metabolism |
|
What is topiramate?
|
inhibits neural cell sodium channels. Adjunct treatment for simple and complex partial seizures.
|
|
Mechanism of tiagabine?
|
inhibits reuptake of GABA
|
|
Use for tiagabine?
|
Partial seizures
|
|
What is vigabatrin?
|
inhibits breakdown of GABA. For partial seizures.
|
|
What is levetiracetam?
|
adjunct for epilepsy and neuropathic pain.
|
|
What is succinylcholine's mech of action?
|
DEPOLARIZING neuromuscular blocker that competes with ACh to reversibly bind nicotinic receptors.
Phase I blockade - continuous depolarization with muscle fasciculations. Irreversible. Phase II - repolarization but desensitization with continuous interaction with succinylcholine = phase II = not transmitting an AP. Reverse by physostigmine |
|
What is clinical use for succinylcholine?
|
Muscle paralysis for endotracheal intubation
|
|
What happpens if succinylcholine is adminstered with halothane?
|
Malignant hyperthermia.
Cx by muscle rigidity and elevated body temp. Rx: dantrolene (releases Ca from SR, decreasing muscle contraction) |
|
What is pancuronium's mechanism of action?
|
Nondepolarizaing neuromuscular blocker that acts to competitively bind nicotinic receptors at NMJ.
Prevents ACh from binding. Inhibition of muscle contraction. |
|
What is clinical use of pancuronium?
|
Adjunct to general anesthesia induction - reducing skeletal muscle contraction for traching
|
|
Side effects of pancuronium?
|
Hypotension
|
|
How can you reverse pancuronium?
|
Cholinesterase inhibitor
|
|
Drugs like pancuronium?
|
Vecuronium, atracurium, cisatracurium, tubocurarine, mivacurium, rapacuronium
|
|
Two types of local anesthetics?
|
Amides - lidocaine, bupivacaine
Esters - procaine, cocaine, tetracaine, benzocaine Esters generally shorter duration |
|
Mechanism of action for local anesthetics?
|
Block Na channels. Most rapidly seen in myelinated fibers of small diameter.
Give epinephrine to avoid systemic spread |
|
Clinical use for local anesthetics?
|
Minor surgical procedures
|
|
Side effects of local anesthetics?
|
Seizures
|
|
Side effects of bupivacaine?
|
myocardial depression, hypotension
|
|
Side effects of cocaine?
|
HTN, cardiac arrhythmias
|
|
What are examples of some general inhaled anesthetic agents?
|
Halothane, isoflurane, desflurane, sevoflurane, enflurane, methoxyflurane
|
|
Mechanism of action for general inhaled anesthetic agents?
|
directly activate GABAa receptors, decreased neuronal activity.
|
|
Uses for general inhaled anesthetic agents?
|
General anesthetic induction and maintenance
|
|
Side effects for general inhaled anesthetic agents?
|
Myocardial and respiratory depression
|
|
Halothane side effects?
|
fulminant hepatic necrosis and cardiac arrhythmias
increased PT time |
|
Side effects for methoxyflurane and enflurane?
|
nephrotoxic.
|
|
What are some general IV anesthetic agents?
|
Propofol, etomidate, ketamine, benzodiazepines, barbiturates, opioids
|
|
Mechanism of propofol?
|
May prolong activity at GABAa receptor
|
|
Mechanism of etomidate?
|
prolongs activity at GABA receptor
|
|
Ketamine mechanism?
|
NDMA receptor antagonist
|
|
Clinical use for propofol?
|
Induction and maintenance of anesthesia
|
|
Clinical use for etomidate?
|
Induction of anesthesia
|
|
Clinical use for ketamine?
|
rarely used for side effects
|
|
Side effects for propofol?
|
Hypotension; chemical pancreatitis
|
|
Side effects for etomidate?
|
Vomiting; myoclonus; adrenal suppression
|
|
Side effects for ketamine?
|
Hallucinations, cardiac and respiratory depressant
|
|
What are some opioids?
|
morphine, codeine, oxycodone, hydrocodone, hydromorphone, heroin, meperidine, fentanyl, dextromethorphan
|
|
Mechanism of opioids?
|
Bindings specific opioid receptors. Hyperpolarization and decreased activity w/interaction of Ca and K ion channels.
Morphine causes K efflux with mu - GPCR |
|
Clinical uses for opioids?
|
Pain control
cough suppression = codeine and dextromethorphan Diarrhea - diphenoxylate = meperidine analog Acute pulmonary edema - morphine PENTAZOCINE = opioid antag/agonist - doesn't get withdrawal |
|
Side effects for opioids?
|
cardiac and respiratory depression; constipation
watch out for tolerance and dependence treat withdrawal in kids WITH TINCTURE OF OPIUM |
|
What are naloxone and naltrexone?
|
opioid receptor antagonists or overdoses
|
|
What is methadone?
|
Opioid for maintenance programs and eases withdrawal symptoms
|
|
Mechanism of levodopa?
|
converted into dopamine by DOPA-decarboxylase in the brain
|
|
Use for levodopa?
|
Parkinsonism
|
|
Side effects for levodopa?
|
Dyskinesia; cardiac arrhythmias;
|
|
What is carbidopa?
|
Inhibits DOPA-decarboxylase only in the periphery, since carbidopa doesn't cross BBB.
|
|
What is bromocriptine?
|
partial dopamine receptor agonist used as adjunct for parkinsonism and for treatment for hyperprolactinemia
|
|
What is sumatriptan?
|
Acts to stimulate presynaptic 5-HTD receptors. Inhibits vasodilation and inflammation of the dura.
Maybe stimulates 5-HTB - vasoconstriction of intracranial vessels |
|
Clinical uses for sumatriptan?
|
Migraines and cluster headaches
|
|
Side effects from sumatriptan?
|
coronary vasospasm, contraindicated in pts with CAD
|
|
Action of bupropion?
|
inhibits reuptake of NE and DA, also nicotinic antagonist
|
|
Action of varenicline?
|
partial agonist and antagonist at alpha4B2 nicotinic acetylcholine receptors subtype
|
|
Side effects for bupropion?
|
psychosis, szs
|
|
What is buspirone?
|
5-HT presynaptic receptor patial agonist.
|
|
Uses for buspirone?
|
Generalized anxiety disorder. Maybe conjunction with SSRIs
|
|
Mechanism of Gabapentin?
|
GABA analogue.
|
|
Uses for gabapentin?
|
postherpetic neuralgia, partial seizures
|
|
Side effects for gabapentin?
|
Peripheral edema
|
|
What is pregabalin?
|
Binds Ca ion channels in CNS, decreasing glutamate and NE release.
Used now to treat neuropathic pain, fibromyalgia. |
|
Class IA antiarrythmics?
|
Procainamide, quinidine, disopyramide
|
|
Action of class IA antiarrythmics?
|
Block active Na channels. Some K activity.
Increasing AP, ERP, QT. Prolong Phase 0, some Phase 3. |
|
Use of Class IA antiarrhythmics?
|
A fib, V Tach.
|
|
Toxicity of Quinidine?
|
Cinchonism
|
|
Toxicity of Procainamide?
|
SLE drug induced
|
|
Class IB antiarrhythmics?
|
Lidocaine, Mexiletine, Tocainide
|
|
Action of class IB antiarrhythmics?
|
Block active and inactive Na channels.
Shorten phase 3. Decreased AP. Good for ischemic myocardium. |
|
Use for class IB antiarrhythmics?
|
post MI ventricular arrhythmias. Digitalis induced arrhythmias.
|
|
Side effects of Class 1B antiarrhythmics?
|
Local anesthetic. CNS stimulation/depression. CV depression
|
|
Class IC antiarrhythmics?
|
Flecainide, Encainide, Propafenone.
|
|
Action of Class IC antiarrhythmics?
|
Block Na channels.
Prolong Phase 0. |
|
Use of Class IC antiarrhythmics?
|
Refractory supraventricular arrhythmias.
For pts without structural abnormalities. |
|
Side effects of Class IC antiarrhythmics?
|
Pro arrhtyhmic. Prolong refractory period in AV node.
|
|
Class II antiarrhythmics?
|
B blockers.
|
|
Action of Class II antiarrhythmics?
|
Decrease slope of phase 4. Increasing PR interval.
|
|
Use of Class II antiarrhythmics?
|
A fib. A flutter.
|
|
Side effect of Metoprolol?
|
Dyslipidemia from hypoglycemia.
|
|
Class III antiarrhythmics?
|
Sotalol, ibutilide, dofetilide, amiodarone
|
|
Action of Class III antiarrhythmics?
|
Inactivate K channels.
Prolong AP, Prolong ERP. Prolong Phase III. Increase QT interval. |
|
Use of Class III antiarrhythmics?
|
Atrial arrhythmias when others fail.
|
|
Side effects of Class III antiarrhythmics?
|
Torsades de pointes.
|
|
Amiodarone actions?
|
Has class I, II, III, IV effects because it alters the lipid membrane.
|
|
Amiodarone side effects?
|
Pulmonary fibrosis, Hepatotoxicity, Thyroid dysfunction
|
|
Mechanism Class IV antiarrhythmics?
|
Primarily affects AV nodal cells
Block Ca channels, decreasing slope of phase IV. Increase ERP, Increase PR. |
|
Use for Class IV antiarrhythmics?
|
Prevention of nodal arrhythmias. SVT. A fib.
|
|
Side effects of Class IV antiarrhythmics?
|
Hypotension. Heart block.
|
|
Use of adenosine?
|
Dx and treatment of SVTs
|
|
Action of adenosine?
|
Increases K outside of cells. Hyperpolarizing the cell.
|
|
Side effects of adenosine?
|
Hypotension, heart block, flushing. Effects blocked by theophylline.
|
|
K as antiarrhythmics?
|
Depresses ectopic pacemakers; especially those with digoxin toxicity.
|
|
Mg as antiarrhythmic?
|
For torsades de points, also for digoxin toxicity.
|
|
Action of digoxin?
|
Inhibiting Na/K ATPase and leading to indirect inhibition of Na/Ca exchanger/antiport. Increasing intracellular Ca. Increased contractility. Stimulates Vagus too. Decreasing heart rates.
super careful with renal clearance |
|
Uses for digoxin?
|
CHF. A fib.
|
|
Side effects of digoxin?
|
GI upset; Blurry yellow vision; ECG changes - prolonged PR, decreased QT, ST scooping, T wave inversion.
|
|
What exacerbates side effects of amiodarone?
|
Renal failure
Hypokalemima Quinidine |
|
Antidote for digoxin toxicity?
|
correcting hypokalemia, administering anti-dig Fab fragments, Mg. Possible lidocaine.
|
|
Action of nitroglycerin or isosorbide dintrate?
|
Vasodilate by releasing nitric oxide in smooth muscle, increasing cGMP and smooth muscle relaxation. Reduction of preload as venodilator.
|
|
Use for nitroglycerin?
|
Angina, pulm edema.
|
|
Side effects of nitroglycerin?
|
Reflex tachycardia, Monday disease, hypotension, flushing, headache
|
|
Action of Nitroprusside?
|
Metabolized into nitric oxide in blood stream. Increase cGMP, smooth muscle relaxation of peripheral veins and arteries. Reduction in preload and afterload.
|
|
Use of nitroprusside?
|
Acute management of HTN crisis. Severe heart failure.
|
|
Side effects of nitroprusside?
|
CN toxicity.
can only be given IV becasue of this. Thiosulfate can treat toxicity. |
|
ACEi actions?
|
Inhibit ACE, peptidyl dipeptidase.Increases bradykinin, a vasdilator. Blocks vasoconstriction of AII and its activation of aldosterone. Decreases PVR and volume of fluid.
|
|
Use of ACEis?
|
treatment of HTN and CHF. Treat and prevent diabetic nephropathy.
Decreases mortality in post MI pts. |
|
Side effects of ACEis?
|
Cough, teratogen, angioedema.
High K in renal insufficient people |
|
Actions for angiotensin receptor blockers?
|
Block AT1 receptor. Decreases SVR from vasoconstriction prevention and decreases fluid volume in body.
|
|
Uses for angiotensin receptor blockers?
|
HTN and CHF. Treat and prevent diabetic nephropathy.
|
|
Side effects of angiotensin receptor blockers?
|
high K and renal failure in renal insufficient patients.
Teratogen NO RESULTANT COUGH OR ANGIOEDEMA |
|
Action of Hydralazine?
|
Increases cGMP --> smooth muscle relaxation. VASODILATES ARTERIOLAR SMOOTH MUSCLE.
|
|
Use for Hydralazine?
|
HTN as well as CHF. First line therapy for HTN in pregnancy with methyldopa. Frequently coadministered with B-blocker to prevent reflex tach.
|
|
Side effects for Hydralazine?
|
Reflex tach.
LUPUS LIKE SYNDROME |
|
Action of Minoxidil?
|
K channel opener --> hyperpolarizes and relaxes vascular smooth muscle. VASODILATOR.
|
|
Use for Minoxidil?
|
HTN.
|
|
Side effects for Minoxidil?
|
Hypertrichosis (hair growth), pericardial effusion.
|
|
Calcium Channel blocker action?
|
Block voltage gated (L-type) Ca channels of cardiac and smooth muscle, reducing muscle contraction = peripheral vasodilation. Decreased myocardial contractility?
|
|
Calcium Channel blockers?
|
Nifedipine, Nicardipine, Amlodipine.
Verapamil, diltiazem |
|
Uses for Ca channel blockers?
|
HTN. Prionzmetal angina. Raynaud's.
|
|
Toxicity of Ca channel blocerks?
|
Cardiac depression, AV block, peripheral edema
Amlodipine - flushing and peripheral edema Verapamil - gingival hyperplasia, constipation, HEART BLOCK |
|
Mannitol action?
|
osmotic diuretic, acts at PT and descending loop of Henle, increase tubular osmolarity drawing water into lumen. Increase urine outflow and decrease volume of body.
|
|
Drugs like mannitol?
|
urea, glycerin, isosorbide
|
|
Use of mannitol?
|
decrease ICP, intraocular pressure. Prevent ARF following shock or toxins.
Isosorbide and glycerin = intraocular pressure |
|
For whom is mannitol contraindicated?
|
patients with CHF, can cause expansion of volume before decrease.
|
|
Side effects of mannitol?
|
Pulm edema, dehydration
|
|
Drugs like acetazolamide?
|
Dorzolamide, brinzolamide.
|
|
Mechanism of acetazolamide?
|
Inhibits Carbonic Anhydrase in cells of PCT.
Less bicarb resorbed, more Na lost in lumen. (CA is also in the eye w/production of aqueous humor) |
|
Use for acetazolamide?
|
glaucoma, alkalinize urine for toxin ingestion like salicylate or barbiturates, treatment and prophylaxis of high altitude sickness (decreases CSF), metabolic alkalosis,
|
|
Side effects of acetazolamide?
|
hyperchloremic metabolic acidosis, hypokalemia
|
|
Loop diuretics?
|
furosemide, bumetanide, torsemide
|
|
Actions of furosemide?
|
Sulfonamide derivative. Inhibits coupled Na/K/2Cl transport in thick ascending loop. Retention of NaCl, K, and H2O in lumen. can't concentrate urine. Increased Ca excretion.
Causes PG release - increases RBF. (afferent) |
|
Uses for furosemide?
|
CHF with pulmonary edema, HTN, Hypercalcemia
|
|
Side effects of furosemide/loop diuretics?
|
Hypokalemia, Ototoxicity, Hyperuricemia/Gout, Allergic reaction with sulfa patients, Interstitial nephritis
|
|
What is ethacrynic acid?
|
Diuretic with same action as furosemide. For patients who can't tolerate solfa drugs. Or prone to gouty attacks.
|
|
Thiazides?
|
HCTZ, Chlorothiazide, chlorthalidone, indapamide
|
|
Mechanism of action of HCTZ?
|
inhibits Na/Cl cotransporter in early DCT of nephron. Reduces diluting capacity of nephron.
|
|
Uses of HCTZ?
|
HTN, nephrogenic Diabetes insipidus, recurrent kidney Ca stones, CHF
|
|
Side effects of HCTZ?
|
Hypokalemia, hyperuricemia, hypercalcemia, hyperglycemia, hyperlipidemia
Increased secretion of Na and K in urine |
|
K sparing diuretics?
|
Spirinolactone, triamterene, amiloride, eplerenone
|
|
Mechanism of spironolactone?
|
Competitive aldosterone receptor antagonist. Na and water retention is decreased at collecting tubule and late distal tubule. K excretion decreased.
|
|
Uses for spironolactone?
|
hyperaldosteronism, heart failure, K depletion
|
|
Side effects of spironolactone?
|
High K, gynecomastia
|
|
Mechanism of triameterene and amiloride?
|
Block Na channels in DCT of nephron. Used for sprionoloactone pts who lack endogenous aldosterone (Addison disease). Can be used for HTN.
|
|
What class of drugs are milrinone and amrinone?
|
PDE inhibitors
|
|
Action of milrinone and amrinone?
|
Inhibite PDE isozyme III. Increased cAMP. Opens Ca channels on surface of cell. Ca flows in = increased contractility.
|
|
When are milrinone and amrinone used?
|
acute decompensated CHF
|
|
Side effects of milrinone and amrinone?
|
Nausea and vomiting
|
|
Action of Sildenafil?
|
PDE inhibitor for ED. cGMP-type 5. In corpus cavernosum of penis. Relaxation of smooth muscle - increased blood flow. Contraindicated in pts on nitrates.
|
|
Mechanism of action of heparin?
|
binds to antithrombin III, inhibiting thrombin and factor Xa.
|
|
Clinical uses of heparin?
|
Treat and prevent DVTs, pulm embolism, myocardial ifarction.
Follow PTT Short half life and rapid onset of action |
|
Side effects of heparin usage?
|
Bleeding, (treated with protamine sulfate [pos charge binding neg charge])
HIT |
|
Pathogenesis of Heparin Induced Thrombocytopenia?
|
Heparin binds to platelets - autoantibody production destroying platelets and overactivating the remaining ones, resulting in a thrombocytopenic, hypercoagulable state
|
|
What are enoxaprin and dalteparin?
|
Low m-w forms of heparin. Focus more on degrading factor X. Longer duration of action, requiring less dosing. Doesn't need as much monitoring.
|
|
Action of warfarin/dicumarol?
|
Inhibits vit K-dependent gamma-carboxylation of factors II, VII, IX, and X and protein C and S.
|
|
Use for warfarin?
|
chronic anticoagulation. Like a fib.
Long half life; takes long to act. |
|
Which drugs affect warfarin?
|
Increase - cimetidine, metronidazole, Bactram
Decrease - barbiturates, rifampin, cholestyramine |
|
Side effects of warfarin?
|
Not used in pregnant women. Teratogenic. Follow PT/INR values. Bleeding
|
|
What drugs are the direct thrombin inhibitors?
|
Hirudin, bivalirudin, lepirudin, desirudin, argatroban, melagatran, dabigatran
|
|
Mechanism of action of hirudin/argatroban?
|
Direct thrombin inhibition.
|
|
Use for hirudin?
|
Anticoagulation in patients who are unable to take heparin - DVTs, acute coronary syndrome.
PT and PTT will be increased with these drugs |
|
What is used to treat HIT?
|
Argatroban
|
|
Side effects of hirudin/argatroban?
|
Bleeding
|
|
Action of aspirin?
|
Inhibits Cox-1 and Cox-2. Decreasing PG synthesis. W/o PGE2, analgesia, antipyretic, decreased synth of protective gastric mucus.
W/o TXA2, decreased platelet aggregation. W/o PGI2, increased gastric secretion. |
|
Uses for aspirin?
|
Antipyretic, analgesic, anti-inflammatory, antiplalatelet (risk for CV or cerebrovascular disease)
|
|
Side effects of aspirin?
|
Bleeding, gastric ulcers, hyperventilation, Reye's syndrome, tinnitus [resp/metabolic acidosis]
|
|
Mechanism of clopidogrel/ticlopidine?
|
Decreased platelet aggregation by inhibiting the ADP pathway. Decreases expression of GPIIb/IIIa
|
|
Uses for clopidogrel?
|
Treat ACS with apsirin, coronary stinitng, alternative antiplatelet for those unable to tolerate aspirin
|
|
Side effects of clopidogrel?
|
Bleeding
|
|
Ticlopidine specific side effects?
|
Neutropenia and TTP
|
|
What is dipyridamole?
|
Used to perform cardiac stress tests and secondary prevention of stroke with aspirin.
Inhibits cyclic PDE, increasing cAMP. Inhibits TXA2 synth and promote prostacyclin action. |
|
Drugs like abciximab?
|
Eptifibatide, tirofiban
|
|
Mechanism of abciximab?
|
Bind to GPIIB/IIIa receptor. Inhibits binding of fibrinogen and vWF to the receptor.
Inhibits cross linking of fibrinogen - impeding platelet aggregation. |
|
Uses for abciximab?
|
Treatment of ACS. Percutaneous coronary intervention.
|
|
Side effects of abciximab?
|
bleeding, thrombocytopenia
|
|
What are some fibrinolytic agents?
|
streptokinase, urokinase, anistreplase, alteplase (tPA), reteplase
|
|
Action of fibrinolytic agents?
|
Directly or indirectly aid conversion of plasminogen to plasmin, cleaves thrombin and fibrin clots. Increases PT, PTT.
|
|
Use for fibrinolytic agents?
|
pulm embolism, stroke, acute MI
|
|
Toxicity for fibrinolytic agents?
|
Bleeding. Treat toxicity with aminocaproic acid.
|
|
What is aminocaproic acid?
|
Similar to tranexamic acid.
|
|
Mechanism of aminocaproic acid?
|
Inhibit plasminogen activation. Inhibition of fibrinolysis results.
|
|
Uses for aminocaproic acid?
|
Bleeding treatment. Maybe hemophilia.
|
|
Side effects of aminocaproic acid?
|
Thrombosis
|
|
Drugs like synthetic EPO?
|
Epoetin, darbepoetin
|
|
Mechanism of action of EPO?
|
Stimulates the bone marrow to enhance erythroid proliferation and differentiation, thereby increasing HCT.
|
|
Clinical use for EPO?
|
Anemia associated with CKD, chemo
|
|
Side effects of EPO?
|
CV events and thromboses. HTN
|
|
What drugs are sulfonylureas?
|
1st = Chlorpropamide, tolbutamide, tolazamide
2nd = glyburide, glipizide 3rd = glimepiride |
|
Action of Sulfonylureas?
|
Stimulate insulin release by closing K channels on B cell membrane so the cell depolarizes - triggering of insulin release via increased Ca influx
2) prolong binding of insulin to target tissue receptors 3) reduce glucagon from direct inhibition of insulin on glucagon |
|
Use for Sulfonylureas?
|
non-insulin dependent type 2 DM
|
|
Side effects of sulfonylureas?
|
Hypoglycemia
not for pregnancy or renal/hepatic patients Chlorpropamide causes disulfiram like effects |
|
What is the biguanide prototype?
|
Metformin
|
|
Action of metformin?
|
Inhibits hepatic gluconeogenesis, increase peripheral utilization of glucose
|
|
Uses for Metformin?
|
type 2 DM.
[also PCOS] |
|
Side effects of metformin?
|
Lactic acidosis; GI upset.
Contraindicated in renal insufficiency |
|
Which drugs are thiazolidinediones?
|
Rosiglitazone, pioglitazone, troglitazone
|
|
Mechanism of rosiglitazone?
|
bind to PPAR-gamma, upregulation of multiple genes. Decrease in insulin resistance.
|
|
Clinical uses of rosiglitazone?
|
Treatment of non-insulin-dependent type 2DM
Monitor LFTs |
|
Side effects of rosiglitazone?
|
Hypglycemia, edema
|
|
Side effects of trogltiazone?
|
Liver damage
|
|
Which drugs are alpha-glucosidase inhibitors?
|
Acarbose, miglitol
|
|
Mechanism of action of acarbose?
|
Inhibit intestinal brush border alpha-glucosidase. Can't breakdown sugarys. Absorption of postprandial carbohydrates is decreased.
|
|
Uses for acarbose/miglitol?
|
Non-insulin-dependent type 2 DM.
|
|
Side effects of acarbose?
|
flatulence/diarrhea
|
|
What are the meglitinides?
|
Repaglinide, nateglinide
|
|
What are the DDP-4 inhibitors?
|
Sitagliptin, vildagliptin
|
|
Action of repaglinide/nateglinide?
|
Binds to a K channel on pancreatic Beta cells, stimulating release of insulin from the pancreas
|
|
What is the Glucagon-like peptide-1 analog?
|
Exanatide
|
|
What is the action of sitagliptin, vildagliptin?
|
DDP-4 degrades GLP-1 which acts to increase insulin secretion and decrease glucagon secretion. By inhibiting DPP-4, GLP-1 increases, leading to increased insulin secretion.
|
|
What is action of exanatide?
|
Increases insulin secretion and decrease glucagon secretion.
|
|
Side effects of repaglinide?
|
weight gain; hypoglycemia
|
|
Side effects of Sitagliptin?
|
Nausea
|
|
Side effect of exanatide?
|
Pancreatitis; hypoglycemia
|
|
Statin action?
|
Inhibit HMG-CoA reductase. Enzyme that catalyzes first step in chol biosynthesis in liver. Increase in conc of LDLr on hepatocytes.
|
|
Use for statins?
|
Decrease total cholesterol and LDL levels. Triglycerides mildly decrease and HDL mildly increase
|
|
Side effects of statins?
|
Myopathy and abnormal LFTs
|
|
What is ezetimibe?
|
Cholesterol lowering medication decreases chol absorption in GI tract. Decreased LDL levels.
|
|
Which drugs are bile acid resins?
|
Cholestyramine, colestipol, colesevelam
|
|
Mechanism of cholestyramine?
|
Inhibit reabsorption of bile acids in jejunum and ileum. Lower levels of bile acid result in increased conversion of cholesterol to bile acids, leading to lower levels of IC cholesterol. Cells increase LDLR.
|
|
Uses for cholestyramine?
|
Decrease LDL levels. No effect on HDL. Also treats pruritus associated with liver failure and diarrhea after gallbladder removal.
|
|
Side effects of cholestyramine?
|
GI upset. Bad taste of medication.
|
|
Which drugs are fibrates?
|
Gemfibrozil, ciprofibrate, bezafibrate, fenofibrate
|
|
Action of gemfibrozil?
|
Stimulates lipoprotein lipase. Enzyme responsible for breaking down triglycerides into VLDL and chylomicrons. Decreasee hepatic chol biosynth.
|
|
Uses of gemfibrozil?
|
decrease triglyceride levels. Mildly decrease LDL. Mildly increase HDL.
|
|
Gemfibrozil side effects?
|
GI upset; more gallstone formation.
compete with plasma proteins; may increase warfarin effects |
|
What is Niacin?
|
lipid-lowering agent increases HDL levels. Decreases LDL (HEPATIC VLDL PRODUCTION). Decreases lipolysis in adipose tissue. Flushing = side effect.
|
|
Which drugs are bisphophonates?
|
Alendronate. - dronate
|
|
Action of alendronate?
|
Decrease osteoclastic bone reabsorption. Inhibit osteoclastic activity and increasing osteoclastic cellular death.
|
|
Uses for alendronate?
|
prevention and treatment of osteoporosis; Paget disease of the bone; bone metastasis with hypercalcemia, multiple myeloma
|
|
Side effects of alendronate?
|
GI upset (esophageal erosions); osteonecrosis of the jaw
|
|
Drug like propylthiouracil?
|
Methimazole
|
|
Mechanism of action of propylthiouracil?
|
Inhibits thyroid peroxidase, enzyme involved in iodine organification, inhibiting the coupling of iodotyrosines. Results in inhibition of thyroid hormone synth in thyroid gland and peripheral conversion of T4 to T3.
|
|
Use of propylthiouracil?
|
Hyperthyroidism
|
|
Side effects of propylthiouracil?
|
Skin rash, AGRANULOCYTOSIS, aplastic anemia
|
|
Gout agents?
|
Colchicine, probenecid, allopurinol
|
|
Mechanism of action of colchicine?
|
Induced microtubular depolymerization binding tubulin. Decreased migration of leukocytes to affected site. Colchicine blocks formation of leukotriene B4 too.
|
|
Action of probenecid?
|
Decreases reabsorption of uric acid in PT. Blocks active transport of uric acid.
|
|
Action of allopurinol?
|
Inhibits xanthine oxidase.
|
|
Clinical use of colchicine?
|
Acute gouty attack. Also Behcet disease and scleroderma.
|
|
Clinical use of probenecid and allopurinol?
|
Prevention of further gouty attacks; prevention and treatment of hyperuricemia (tumor lysis syndrome)
|
|
Side effects of colchicine?
|
Diarrhea; bone marrow suppression
|
|
Side effects of probenecid?
|
GI upset; inhibition of renal excretion of PCN and NSAIDs
|
|
Side effects of allopurinol?
|
GI upset; hypersensitivity reactions; decreased metabolism of 6-MP and Azathioprine
|
|
Mechanism of prednisone?
|
Mimics actions of endogenous glucocorticoids. Vasoconstriction, stimulation of gluconeogenesis, protein catabolism, decrease of circulating leukocytes, inhibition of PG and leukotriene formation through inhibition of PLA2, stimulation of gastric acid and pepsin production.
|
|
Clinical uses of prednisone?
|
Adrenocortical insufficiency, collagen vascular disorders (SLE, RA, polymyositis), inflammatory bowel dz, asthma, spinal ocrd compression.
|
|
Side effects of prednisone?
|
symptoms of Cushing syndrome. Osteoporosis, irritability, hyperglycemia, fat redistribituion, impaired wound healing, thin skin, peptic ulcers
|
|
What is beclomethasone?
|
Inhaled glucocorticoid for asthma.
|
|
Action of orlistat?
|
Inhibits pancreatic lipase. Reducing intestinal fat absorption.
|
|
Action of sibutramine?
|
Neurotransmitter reuptake inhibitor (5HT, NE, Dopamine) at synpatic clefts
|
|
Uses for orlistat and sibutramine?
|
Obesity
|
|
Side effects of orlistat?
|
Fecal incontinence; steatorrhea
|
|
Side effects of sibutramine?
|
Nausea, sexual dysfunction
|
|
What is action of flutamide?
|
Competitive antagonist at the androgen receptor. Decreases growth effects of testosterone on prostate. Higher LH will result so counteract with leuprolide.
|
|
Uses of flutamide?
|
Prostate cancer
|
|
Side effects of flutamide?
|
GI upset; gynecomastia
|
|
What is Danazol?
|
Mild agonist at androgen and progesterone receptors, decrease of LH and FSH secretion. Treats endometriosis and fibrocystic disease of the breast.
|
|
What is finasteride?
|
Inhibits 5-alpha reductase. Enzyme responsible for Test--> DHT.
|
|
Uses of finasteride?
|
BPH, prostate cancer, early male-pattern baldness.
|
|
Side effects of finasteride?
|
Decreased libido, ED
|
|
What is anastrozole?
|
Inhibits aromatase. Use for Estrogen receptor positive Breast Ca.
|
|
What drugs are GnRH agonists?
|
Leuprolide, nafarelin, goserelin
|
|
Action of Leuprolide/nafareline/goserelin?
|
binds GnRH receptors - with continuous stimulation blocks levels of LH and FSH w/downregulation of GnRH receptors.
|
|
Uses of leuprolide?
|
Metastatic prostate cancer, leiomyomas, emdometriosis w/continuous fashion.
Infertility - intermittent |
|
What is clomiphene?
|
Partial agonist at estrogen receptors in pituitary - increasing release of gonadotropins. Induces ovulation - treats infertility. Side effects - hot flushes and multiple pregnancies
|
|
Side effects of leuprolide/nafarelin/goserelin?
|
impotence, hot flashes; GI upset
|
|
Mechanism of OCs?
|
Progestins decrease GnRH and decreases FSH and LH.
Estrogen - decreasese FSH and doesn't stim LH release. Decrease in follicle devo; absence of ovulation |
|
Uses for OCs?
|
birth control; dysfunctional uterine bleeding; PCOS; endometriosis, dysmenorrhea
Decrease risk of ovarian and endometrial cancer |
|
Side effects of OCPs?
|
Breast fullness; N/v; HA; thromboembolism
|
|
What is mechanism of Emergency contraception?
|
high dose progestins taken up to 72 hr after sex
|
|
What is mifepristone?
|
Antagonist at progesterone receptor. Abortifacient at high doses by breaking down endometrial lining and cervical dilation.
|
|
What is octreotide?
|
somatostain. Inhibits release of many hormones, reduces GI motility, causes vasoconstriction
|
|
Uses of octreotide?
|
Endocrine disorders like Diarrhea associated with VIPomas, treatment of acromegaly, treatment of Zollinger-Ellison.
Treats esophageal varices associated with cirrhosis-induced portal htn |
|
side effects of octreotide?
|
GI upset; cardiac arrhythmias
|
|
Action of vasopressin?
|
Naturally occurring hormone. Released by posterior pituitary.
V1 - vasoconstriction V2 - increases permeability of H2O in collecting ducts V3 - V2 like to facilitate factor VIII activity |
|
Uses for Vasopressin?
|
Central DI
Septic shock and cardiac arrest Increasing factor VIII/vWF for VWD dz or hemophilia A |
|
Side effects of vasopressin?
|
Hyponatremia; vasoconstriction with vasopressin
|
|
What is oxytocin?
|
Induces labor and stimulates breast milk let down
|
|
What type of drugs are aluminum hydroxide, magnesium hydroxide, calcium carbonate, and sodium bicarbonate?
|
Antacids
|
|
What is mechanism of action of antacids?
|
Weak bases that form a salt and water upon reaction with HCl. Increase pH and reduce acidity of gastric contents. Furthermore, since pepsin is inactivated at higher pH, antacids may act to decrease peptic activity of protein breakdown.
|
|
Use of antacids?
|
GERD, promote healing of duodenal ulcers
|
|
Side effects of antacids?
|
Aluminum hydroxide: Constipation
Magnesium hydroxide: Diarrhea Calcium Carbonate: Hypercalcemia; milk-alkali syndrome Sodium bicarb: Flatulence; metabolic alkalosis |
|
Mechanism of sucralfate?
|
promotes duodenal ulcer healing, enhances mucosal barrier either through stimulating PG synthesis or by acting as a physical barrier
|
|
Drugs like Ranitidine?
|
Cimetidine, Famotidine, Nizatidine
|
|
Mechanism of action of ranitidine?
|
Block binding of histamine to H2 receptor present on parietal cells of the gastric mucosa. cAMP levels decrease, leading to decreased activity of H/K proton pump.
|
|
Uses for ranitidine?
|
GERD, peptic ulcer disease
|
|
Side effects of Ranitidine?
|
Gynecomastia, decreased hepatic metab of warfarin (cimetidine)
|
|
Mechanism of Omeprazole?
|
Inhibits the H/K ATPase pump on parietal cells of the mucosa. Suppresses gastric acid secretion.
|
|
Use of omeprazole?
|
Treatment of PUD, GERD, Zollinger-Ellison syndrome, esophagitis.
Treat H pylori infection. |
|
Side effects of omeprazole?
|
HA, rash, increased risk of fractures in the elderly
|
|
What drugs are antiemetics?
|
ondansetron, metoclopramide, prochlorperazine, promethazine
|
|
Mechanism of ondansetron?
|
Blocks 5-HT3 receptors.
Serotonin receptors are present in the chemoreceptor trigger zone in the brainstem, which is part of the vomiting reflex pathway, and in the GI tract. When the 5HT3 receptors are activated in the GI tract by release of 5HT from damaged enterochromaffin cells, signal is sent by vagus nerve to brainstem to activate the vomiting reflex pathway. |
|
Mechanism of metoclopramide and prochlorperazine?
|
Dopamine antagonist. Activation of D2 receptors in the chemoreceptor trigger zone can lead to activation of the vomiting reflex pathway.
|
|
Mechanism of promethazine?
|
H1 receptor antagonist. H1 receptors are present everywhere including GI tract. By blocking these GI receptors, motility is decreased.
|
|
Uses for Promethazine or Prochlorperazine?
|
n/v
|
|
Side effects of Ondansetron?
|
HA
|
|
Side effects of Metoclopramide and prochlorperazine?
|
Sedation, hypotension, diarrhea, extrapyramidal symptoms
|
|
Side effect of promethazine?
|
Blurry vision; confusion; dry mouth
|
|
What drugs are laxatives?
|
castor oil, senna, bisacodyl, lactulose, sorbitol, polyethylene glycol, magnesium salts, docusate, mineral oil
|
|
Mechanism of irritants or stimulants for laxatives?
|
Castor oil, senna, bisacodyl
Increase intestinal peristalsis through mucosal irritation or stimulation - leading to increased gut motility. |
|
Mechanism of bulking laxatives?
|
lactulose, sorbitol, polethylene glycol, magnesium salts
Draw water into intestine via osmosis. Distend bowel, resulting in increased intestinal motility. |
|
Mechanism of stool softeners?
|
Docusate, mineral oil
Emulsify with stool, softening it. |
|
Use for laxatives?
|
Constipation. Bowel prep.
|
|
Side effects of laxatives?
|
abdominal cramps
|
|
What drugs are antidiarrheal agents?
|
Diphenoxylate, loperamide, kaolin, bismuth subsalicylate
|
|
Mechanism of diphenoxylate and loperamide?
|
Bind to opioid receptors in the intestine, leading to inhibition of ACh release, leading to decreased peristalsis.
|
|
Mechanism of Kaolin?
|
Absorbs potential intestinal toxins
|
|
Mechanism of bismuth subsalicylate?
|
decreases secretion of fluid into bowel lumen.
Traveler's diarrhea. |
|
Mechanism of sulfasalazine?
|
Metabolized to sulfapyridine and 5-ASA. 5-ASA acts as anti-inflammatory inhibiting PG and Leukotriene production through COX inhibition.
|
|
Uses for sulfasalazine?
|
IBD (RA and juvenile arthritis)
give it with folic acid due to sulfapyridine affects |
|
Side effects of sulfasalazine?
|
GI upset; skin rash; bone marrow suppression; infertility
|
|
What is ursodiol/chenodiol?
|
Decreases incidence of cholesterol gallstones
1) blocking HMG-CoA reductase 2) decrease intestinal reabsorption of cholesterol 3) inhibits secretion of cholesterol into bile |
|
Uses for ursodiol?
|
Treatment of primary biliary cirrhosis; also for treating cholesterol gallstones.
|
|
What drugs are anthracyclines?
|
-rubicins
|
|
Mechanism of anthracyclines?
|
1) insert between DNA bps, blocking DNA and RNA synth
2) Production of O2 radicals 3) Disrupt fluid and ion transport |
|
Uses of anthracyclines?
|
Doxorubicin - Chemo agent for variety of solid tumors and hematologic malignancies
Daunorubicin Idarubicin - chemo also |
|
Side effects of anthracyclines?
|
cardiac toxicity - adminster dexrazoxane with it for decreasing radicals (makes dilated cardiomyopathy)
alopecia; bone marrow suppression |
|
What is agent of choice for Wilms tumor?
|
Dactinomycin
|
|
What is action of dactinomycin?
|
inhibit DNA-dependent RNA polymerase
|
|
Drugs like dactinomycin?
|
Plicamycin - similar action - testicular and Paget's dz
Mitomycin - alkylating agent damaging DNA via cross linking of strands |
|
Action of Bleomycin?
|
Triggers formation of O2 radicals after binding DNA.
|
|
Uses for bleomycin?
|
Testicular tumors
|
|
Side effects of Bleomycin?
|
Pulmonary fibrosis. Myelosuppression is RARE
mainly for G2 cell cycle specific |
|
What is Busulfan?
|
Alkylating agent. For CML and PV. Pulm fibrosis = side effect. Adrenal insufficiency.
|
|
Mechanism of Cyclophosphamide/Ifosfamide?
|
Alkylating agent and cross-links DNA, decreasing DNA and RNA synth.
Drug has been implicated in suppression of B and T cell function. |
|
Clinical uses for cyclophosphamide?
|
Chemo
Immunosuppressive - RA, SLE, WG, nephrotic |
|
Side effects of cyclophosphamide?
|
Hemorrhagic cystitis (acrolein accumulates, decreased with MESNA). Bone marrow suppression.
|
|
What is Mechlorethamine treatment protocol for?
|
Hodgkin lymphoma
|
|
What drugs are nitrosureas?
|
Carmustine, lomustine, semustine, streptozocin
|
|
What is mechanism for nitrosureas?
|
Alkylating agents, cross-link DNA strands.
|
|
Use for Nitrosureas?
|
-ustines + streptozocin
Brain tumors. cross BBB |
|
Mechanism of platins?
|
Alkylating agent.
|
|
Use for platin?
|
Chemo for genitourinary tumors.
|
|
Side effects of platins?
|
Nephrotoxicity. Ototoxicity
|
|
What is Procarbazine?
|
alkylating agent. Also MOPP protocol for Hodgkin. Metabolite inhibits MAO. Don't ingest tyramine.
|
|
Mechanism of Methotrexate?
|
Inhibits DHFR, necessary for formation of thymidylate.
|
|
Use of Methotrexate?
|
Chemo agent
Immunosuppressant - for RA (Crohn, psoriasis) Abortifacient w/Progstaglandin |
|
Side effects for MTX?
|
bone marrow suppression, teratogen, pulm toxicity
stomatitis, hepatotoxicity give Leucovorin for rescue. Minimizes bone marrow suppression from lack of folate. |
|
Action of 6-MP?
|
inhibits purine synthesis when it gets converted to thio-IMP, inhibiting de novo purine sythesis.
|
|
Clinical uses for 6-MP?
|
Chemo - ALL
Immunosuppressant - IBD, psoriasis |
|
Side effects of 6-MP?
|
Bone marrow suppression
metabolized by xanthine oxidase. Don't give it with allopurinol - really increases level. |
|
Function of Azathioprine?
|
Immunosuppresant also inhibiting purine synth. Used for SLE,, IBD, RA.
|
|
Mechanism of 5-FU?
|
inhibits thymidylate synthase. Inhibition leads to disruption of DNA synth. Gets converted to 5-FdUMP
|
|
Uses for 5-FU?
|
Chemo agent for adenocarcinomas. Like Colon.
|
|
Side effects of 5-FU?
|
Bone marrow suppression.
Cell cycle specific - S |
|
Action of cytarabine?
|
Competitively inhibits DNA polymerase after being converted into araCTP.
|
|
Use for Cytarabine?
|
Chemo. AML
|
|
Side effects of cytarabine?
|
Bone marrow suppression w/resulting pancytopenia
Cell cycle specific to S phase |
|
Action of etoposide?
|
inhibits topoisomerase II, leading to DNA strand breakage.
|
|
Uses for etoposide?
|
Chemo agent. Small cell lung.
|
|
Side effects of etoposide?
|
Bone marrow suppression.
Cell cycle specific - S-G2 phase |
|
Mechanism of vincristine/vinblastine?
|
Bind to tubulin - lead to depolymerization of mitotic spindle. Unable to progress past metaphase.
|
|
Uses for Vincristine? Vinblastine?
|
Vincristine - ALL, lymphoma (hodgkin!)
Vinblastine - Bone marrow suppression |
|
Side effects of vincristine?
|
Peripheral neuropathy. Not really myelosuppresion.
|
|
Side effects of vinblastine?
|
Bone marrow suppresion.
|
|
Mechanism of Paclitaxel/Docetaxel?
|
Binds to tubulin. Promotes stabilization and polymerization of mitotic spindle. Not allowing anaphase.
|
|
Use of paclitaxel?
|
Ovarian and breast Ca.
Coats coronary artery stents to prevent restenosis. |
|
Side effects of paclitaxel?
|
Bone marrow suppression
|
|
Mechanism of Tamoxifen?
|
Competitive estrogen-receptor antagonist. Lower affinity for estrogen receptor than estrogen. Most effective in post-menopausal women.
|
|
Use for Tamoxifen?
|
Chemo - breast cancer
(Osteoporosis?) |
|
Side effects of tamoxifen?
|
Increased risk for endometrial cancer; increased risk of thromboembolism; hot flashes
|
|
Use of raloxifene?
|
Doesn't increase risk of endometrial cancer - yes for thromboembolism.
Mixed estrogen agonist/antagonist. Osteoporosis rx |
|
Mechanism of hydroxyurea?
|
Inhibits ribonucleotide reductase, resulting in decreased DNA synthesis.
|
|
Clinical use for hydroxyurea?
|
Chemo agent - CML
SCD |
|
Side effects of hydroxyurea?
|
Bone marrow suppression
cell specific to S phase |
|
Mechanism of pentostatin?
|
For hairy cell leukemia. Inhibits adenosine deaminase.
|
|
Action of trastuzumab?
|
Mab against HER-2
|
|
Use of Trastuzumab?
|
Breast Ca with HER-2 receptor (erb-B2)
|
|
Side effects of trastuzumab?
|
Cardiac toxicity
|
|
Action of Imatinib?
|
Competitive inhibitor of tyrosine kinase (abl, c-kit, PDGF-R)
|
|
Use for imatinib?
|
CML, GIST
|
|
Action of theophylline?
|
Decrease PDE. Leading to increased cAMP --> bronchodilation
|
|
How should you treat drug-induced Parkinson's?
|
Antimuscarinic Benztropine
|
|
Inhaled anesthetic affects on body parameters?
|
Increase cerebral blood flow, decrease cardiac output, decrease RPF, decrease GFR
|
|
Mechanism differences between Benzos and Barbiturates?
|
Benzos - increase frequency of GABA opening
Barbiturates - increase duration of GABA opening |
|
Action of Propranolol for thyroid?
|
Decrease peripheral conversion for T4-->T3
|
|
Why wait 2 weeks after phenelzine before giving sertraline?
|
wait for enzyme re-synthesis
|
|
Donepezil use?
|
cholinesterase inhibitor for Alzheimers. In addition with Vit E and NMDA analgo memantine
|
|
Ibuprofen like drugs?
|
Naproxen, indomethacin, diclofenac, sulindac, oxaprozin
|
|
Mechanism of ibuprofen?
|
reversible inhibitor of COX 1 and 2, resulting in decreasing prostaglandin synthesis
PGE2 - analgesia, antipyretic, decreased gastric mucus PGI2 - increased gastric secretion |
|
Uses for ibuprofen?
|
Antipyretic, analgesic, anti-inflammatory
no sig antiplatelet effect bc it reversibly inhibits |
|
Side effects of ibuprofen?
|
GI bleeding, interstitial nephritis, tinnitus
|
|
Use for indomethacin?
|
Delaying labor, agent to close PDA, analgesic, antipyretic, antiinflammatory
|
|
Mechanism of Celecoxib?
|
Irreversibly inhibits Cox-2, decreased PG synth - anti-inflammatory.
|
|
Use for Celecoxib?
|
RA, osteoarthritis, other acute pain
reduce colonic polyps in FAP |
|
Side effects of Celecoxib?
|
GI, interstitial nephritis, increased thrombosis risk, allergic if can't tolerate solfa
Rofecoxib killed with MI and stroke |
|
Mechanism of Acetaminophen?
|
Reversibly inhibits Cox 1 and Cox 2 in the nervous system: analgesia, antipyretic w/o Pge2.
|
|
Use of acetaminophen?
|
Antipyretic and analgesic. Good for those who can't tolerate aspirin or other NSAIDs.
|
|
Side effects of acetaminophen?
|
Fatal hepatotoxicity with overdose
|
|
Antidote for acetaminophen overdose?
|
Acetylcysteine
|
|
Action of Zafirlukast/Montelukast?
|
Reversible inhibitor of cysteinyl leukotriene-1 receptor.
Blocking Lt C4, D4, E4 - bronchoconstriction and increased mucus are blocked |
|
Uses of zafkirlukast?
|
Preventative treatment of asthma
potentiates warfarin by inhibiting cyp-450 |
|
Side effects of zaifrlukast?
|
abnormal LFTs; HA; eosinophilic vasculitis
|
|
Mechanism of Zileuton?
|
Inhibits 5-lipoxygenase. Decreases Leukotriene leves from arachidonic acids. Downstream products for Leukotriene B decrease too - B4 acts to attract eosinophils and neutrophils.
|
|
Uses for Zileuton?
|
Preventative treatment of asthma
|
|
Side effects of zileuton?
|
abnormal LFTs, HA, eosinohpilic vasculitis
|
|
What is cromolyn?
|
Anti-inflammatory for prevention of asthma exacerbations. Used also for allergic rhinitis or conjunctivitis. Inhibits release of histamine and other compounds from mast cells.
|
|
Mechanism of cyclosporine?
|
Inhibits calcineurin, which normally activates IL-2. Production decreased, decreased activation of T cells.
|
|
Uses for cyclosporine?
|
Immunosuppressant in transplant patients; GVHD treatment; RA treatment
metab by cyp p-450 (3A4) |
|
Side effects of cyclosporine?
|
Nephrotoxicity; hepatotoxicity
(hyperglycemia, HTN, high K) |
|
What is tacrolimus?
|
Binds FKBP - inhibits calcineurin.
Calcineurin then dephosphorylates the transcription factor NF-AT (nuclear factor of activated T-cells), which moves to the nucleus of the T-cell and increases the activity of genes coding for IL-2 Immunosuppressant in transplant pts |
|
Mechanism of Mycophenolate mofetil?
|
Acts within B and T lymphocytes to inhibit IMP dehydrogenase for purine synthesis. W/o GMP, DNA is decreased.
|
|
Uses for mycophenolate mofetil?
|
Immunosuppresant in transplant pts; autoimmune disorders too
|
|
Side effects of mycophenolate mofetil?
|
increased lymphomas, allergic, pancytopenia
|
|
Interferon producers?
|
alpha - leukocyte
beta - fibroblasts gamma - CD4 T cells |
|
Mechanism of inteferons?
|
Boost the immune system in response to viral infection. Increase MHC, nK cells, CD8 t cells, increased ribonuclease activitiy, inhibition of EF-2
|
|
Uses for interferons?
|
Cancer
Chronic hep C MSclerosis |
|
Side effects of interferons?
|
Fatigue; bone marrow suppression
|
|
Alprostadil action use?
|
PGE1 analog. For erectile dysfunction, maintaining PDA.
|
|
Misoprostol action use?
|
PGE1 analog. Increases uterine contractions, inhibits gastric acid secretion, and increases mucosal protection in the stomach
prevention of Gastric ulcers; abortifacient with MTX |
|
Latanoprost action use?
|
PGF 2alpha - increases aqueous humor drainiage.
For chronic glaucoma |
|
Dinoprostone action use?
|
analog of PGE2; increases uterine contractions
Abortifacient |
|
Carboprost action use?
|
PGF2alpha, abortifacient
|
|
Epoprostenol action use?
|
PGI2. Prostacyclin, vasodilator
For Pulm HTN. |
|
Action of Etanercept?
|
Inhibits binding of TNF-alpha and TNF-B molecules to their receptors.
TNF stimulates IL-1, IL-6, IL8 |
|
Etanercept use?
|
Autoimmune disease, RA.
|
|
Gold salt uses?
|
RA.
|
|
Mechanism of Infliximab?
|
Chimeric antibody, inhibits binding of TNF-alpha with its receptor.
TNF-alpha is a cytokine produced by macs that stimulates IL-1, 6, 8. So decrease = anti-inflammatory |
|
Uses of infliximab?
|
autoimmune diseases - RA, IBD
|
|
Side effects of infliximab?
|
infusion reaction, abnormal LFTs
|
|
Adalimumab use?
|
MaB, binds to TNF-alpha and inhibits binding of TNF-alpha with its receptor.
|
|
Thalidomide action?
|
Believes decreases TNF-alpha production
|
|
Use of thalidomide?
|
treatment of erythema nodosum leprae; also for multiple myeloma
|
|
Side effects of thalidomide?
|
Sedation, increased DVTs
|
|
Special notes for thalidomide?
|
teratogenic and contraindicated during pregnancy
|
|
First generation antihistamines?
|
Diphenhydramine, promethazine, meclizine, hydroxyzine, doxylamine
|
|
Mechanism of Diphenhydramine?
|
Block H1 histamine sites. Producing bronchodilation, decreased pruritus, decreased peripheral vascular resistance, decreased GI tract motility, decreased rash formation. Some antagonism on cholinergic and alpha-adrenergic.
|
|
Uses for diphenhydramine?
|
Urticaria, allergic reactions, motion sickness
|
|
Use for promethazine?
|
Antiemetic
|
|
Use for meclizine?
|
Vertigo treatmnet
|
|
Side effects of diphenhydramine/first generation antihistamines?
|
Sedation; anticholinergic
|
|
Second generation H1 histamine blockers?
|
Loratadine, cetirizine, fexofenadine
|
|
Mechanism of fexofenadine?
|
Block H1 histamine receptor sites
doesn't cross BBB - less sedation |
|
Uses of fexofenadine?
|
Allergic rhinitis
|
|
Mechanism of ethanol?
|
Potentiate inhibitory effects of GABA
|
|
Use for ethanol?
|
Treatment of ethylene glycol and methanol overdose to prevent dangerous metabolites
|
|
Side effects of ethanol?
|
CNS depression, GI inflammation
|
|
Disulfiram action?
|
Treats alcohol cessation. Inhibiting acetaldehyde dehydrogenase.
|
|
Theophylline action?
|
Inhibits PDE (responsible for breaking down cAMP) - keeping bronchodilation
|
|
Uses for theophylline?
|
Chronic and acute asthma
|
|
Side effects of theophylline?
|
Cardiac arrhythmias; seizures
narrrow therapeutic index; metab by cyp-450 |
|
Iron mechanism and clinical signs?
|
forms reactive O2 species
signs - ab pain; bloody diarrhea; unconsciousness |
|
Iron treatment?
|
Deferoxamine
|
|
Lead mechanism and clinical signs?
|
Interferes with heme synthesis; altering cell membrane structure
Clinical signs - ab pain; neuropathy; anemia; basophilic stippling; lead line at the gums |
|
Antidote to Pb?
|
Calcium EDTA; dimercaprol; pencillamine
|
|
Arsenic mechanism and signs?
|
Inhibits several enzymatic processes - esp ox phos
Signs - Garlic odor on breath; bloody diarrhea; hair loss; neuropathy |
|
Antidote to arsenic?
|
Dimercaprol; pencillamine
|
|
Cyanide mechanism and signs?
|
block cytochrome complex in ETC
HA; GI upset; szs; coma |
|
Cyanide antidote?
|
Sodium thiosulfate; nitrites
|
|
Carbon monoxide mechanism and signs?
|
Mechanism: binds to Hb, reducing o2 binding and delivery to tissues
Signs: HA; GI upset; SZs; coma |
|
Antidote to CO?
|
100% O2
|
|
Phentermine and Fenfluramine?
|
Appetite suppressants. CAUSE PULM HTN.
|
|
OKT3?
|
Anti Cd3 against t lymphocytes
|
|
Rituximab?
|
anti-cd20 - b cell lymphomas and RA
|
|
Perchlorate and Pertechnetate?
|
block iodide absorption via comeptitive inhibition
|
|
Breakdown seizure treatments?
|
Partial - CBZ
Absence - Ethosuximide Myoclonic or Absence plus others =VPA Tonic-clonic = Phenytoin, CBZ, VPA |
|
T 1/2?
|
Vd x .7 / CL
|
|
Antidote for platin?
|
Amifostine
|
|
Antidote for anthracyclins?
|
Dexrazoxane
|
|
Antidote for methanol/ethylene glycol?
|
Fomepizole
|
|
Determinants of low Vd?
|
high MW, high binding protein, high charge, hydrophilic
|
|
Primidone?
|
Anti convulsant. Metabolized to phenobarbitol.
|
|
Quick waking from thiopental results from?
|
Redistribution of drug to lean body tissue: fat/muscle
|