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74 Cards in this Set
- Front
- Back
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Valacyclovir
How much of it is absorbed in the GI? Where is it excreted? What side effects? |
55%
Kidneys Blood disorders |
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ValGanciclovir
Absorption in GI? What is it used to treat? |
60%
CMV Retinitis |
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Foscarnet
What is it an analogue of and mechanism of action? Side effect? |
Pyrophosphate analogue
BLocks viral DNA polymerase and reverse transcriptase by binding to their pyrophosphate site. Nephrotoxicity |
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Palivizumab
What is it? and what is it used for? Mechanism of action? |
mAb used for prevention of RSV
Binds to viral envelope and prevents replication. |
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Fomivirsen
What is it and what does it do? What is it used for? Side Effects? |
Oligopeptide that inhibits protein synthesis trhough an anti-sense mechanism
CMV Iritis, cataracts, increase in intraocular pressure. . |
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What is amantadine and rimantidine used for?
Suggested mechanism of action? Side Effects? Drug rxn? |
Prophylaxis and treatment of influenza A
Bind Viral M2 membrane preventing viral uncoating and cell penetration. Nervousness, dizziness, insomnia, and hamper concentration Anticholinergics - psychotic Teratogenic Can cause CHF |
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Oseltamivir
Where is it activated and eliminated? Where does it deposit? Zanamivir How is it administered and absorbed? |
Liver, Kidneys
Throat and oropharynx It is not absorbed in GI. Oral inhalation |
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Zidovudine
What is it's analogue? |
Thymidine
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What is a property of all NRTIs?
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They all cause lactic acidosis
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TB is what type of organism G- or G+?
Why? |
Neither
Their cell walls are structurally different. |
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Difference between TB infection and TB disease
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Look at the slide bitch.
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TB vaccine BCG
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It's not 100% effective. And it fucks up the PPD test and doesn't circumvent reactivation. Thats why its not used in US.
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Isoniazid
What are the 2 side effects |
Peripheral Neuropathy
Hepatoxicity |
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Ethambutol
Mechanism of action Side effect |
Blocks mycolic acid
Optic Neuritis Hyperuricemia Resistance can develop |
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Rifamycin
Mechanism of action What does it do to P450 |
Inhibits RNA polymerase. Selective since mammalian RNA polymerase does not have high affinity to this drug like TB.
Strongly induces p450 |
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Dapsone
Mechanism of action Used in combo with? Side effect? |
Folic acid blockade, works like a sulfonamide
Rifampin and Clofazimine Hemolytic anemia (like all other sulfonamides) |
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Amphotericin B
What type of drug? Mechanism of action Side Effect Route of administration Synergistic effects |
Polyene macrolide for systemic mycoses
Binds to ergosterol and causes cell membrane leakage (K+) Nephrotoxic and can't be used with aminoglycosides. Must be IV Used with flucytosine. Amphotericin helps this drug get in. |
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Nystatin
Type of drug Use |
Same as amphotericin B but more toxic
Since it is not absorbed well in the GI it is used for the GI and mouth candididis. |
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Imidazoles and Triazoles
Mechanism of action Fungal effects P450? |
Inhibits enzyme for ergosterol synth.
Both fungicidal and static Inhibits p450 |
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Capsofungin
Type of drug Mech of action Fungal effects Side effect |
Echinocandids
Inhibits 1,3 Glucan synthase enzyme for fungal cell wall synth. Fungicidal Histamine release |
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Antiprotozoal
Selective toxicity |
Agents to selectively choose what they do without damage to host cells.
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Malaria
Acute Attack treatment - caused by P vivax and P f. If they are chloroquine resistant what would you do? Which organism Pv or Pf has dormant hepatic form? what is the drug of choice for radical cure? Selection of drug for malaria is based what 2 factors? |
Chloroquine
Artesunate or Quinine combined with translation inhibitiors (Doxcycline, clindamycin, Fansidar, Lumefantrine) P vivax. Drug of choice - primaquine 1. The goal of treatment. 2. Drug resistance of causitive strain of plasmodium. |
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Name the drugs for Malaria.
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Inhibitors Heme metabolisms
Inhibitors of ETC Inhibitors of DNA metabolism Inhibitors of Translation New Therapies Vaccines |
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What is the difference between cholorquine and quinine.
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Cholorquine is less toxic and potent than quinine.
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Mefloquine
Efffective against what forms What is this drug used for? Adverse effects come about how? |
Erythroytic forms of both Pv and Pf
Drug of choice for prophylaxis of Pv and Pf The higher the dosage the more you see the adverse effects |
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Quinine
Mech of Act. Side effects |
Prevents parasite from converting heme to nontoxic metabolites.
CNS and CV toxicities |
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Artemether and Artesunate
When and why are these drugs used? Mech of action |
Used for treatment of severe attacks of Pf where multi drug resistant Pf is endemic.
Heme activates these drugs so it releases free radicals that alkylate proteins and lipids. |
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Artmeisinin Combo Therapy
Which drug would you use for this combo? |
Mefloquiine
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Halofantrine
Effect against? Side effects Why is this drug not used for prophylaxis? |
Drug resistant Pf
Cardiac Toxicity/ Embryotoxic It interferes with mefloquinine |
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Artemether and Lumefantrine
What is the trade name Highly effective against? Should not be used for what? |
Coartem
Pf Severe malaria |
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Primaquine
What is it used for? What may it generate? Mech of action Side effect? |
Radical cure Pv
ROS Inhibits ETC G6PD deficiency causes hemolysis |
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Pyrimethamine
What is it effective for? Mech of action |
Acute malaria attacks
Inhibits dhihydrofolate reductase to inhibits folic acid synth. |
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Pyrimethamine + sulfadoxine (Fansidar)
Mech of action Not effective against? |
Blockade of folic acid synth
Pv, Ovale, Malariae |
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Pyrimethamine + Dapsone (Maloprim)
mech of action Side effect Not recommended for what? |
Folic acid inhibitor
Fatal agranulocytosis Not recommended for wide prophylaxis against chloroquine resistant Pf. |
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Atovaquone + Proguanil (Malarone)
What is it primarily used for? |
Prophylaxis
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Atovaquone
Mech of action What is it used to treat? |
Inhibits ETC
PCP, Malaria, Toxoplasmosis |
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Proguanil
Mech of action What is the active metabolite? |
Inhibits plasmodial dihydrofolate reducatase preventing nucleic acid synthesis
Cycloguanil |
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Disease - Amebiasis (Dysentery)
What is the responsible organism? Drug of choice |
Entamoeba Histolytica
Iodoquinol, paromomycin, metronidazole |
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Disease - Toxoplasmosis
Drug of choice? |
Fansidar (Pyrimethamine + Sulfadiazine)
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BEAVER FEVER - Giardisis
What is organism responsible? Where is it's primary habitat Drug of choice |
Giardia L.
Upper intestine Metronidazole |
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Drug of choice African trypanosomasis?
Mech of act of this drug. |
Eflornithine
Inhibits ornithine decarboxylase so it inhibits polyamine |
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Valacyclovir
What is it? How much is absorbed is GI? Where is it excreted? |
Valine ester of acyclovir. A prodrug that turns into acyclovir.
55% and excreted in kidneys |
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Valganciclovir
Is better absorbed in GI. |
Than ganciclovir
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Foscarnet
mech of action Side effect |
Blocks viral DNA polyermase and RT by binding to their pyrophosphate binding site.
Nephrotoxicity |
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Palivizumab
What is it and what is it used for? Mech of action |
Monoclonal Ab used for prevention of RSV in infants and young children.
Binds viral envelope and prevents replication |
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Fomivirisen
What is it and mech of act? Side effect |
Oligonucleotide that inhibits protein synthesis through anti-sense mechanism.
Iritis, cataracts and increase intraocular pressure |
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What is the analogue of zidovudine (AZT)
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Thymidine
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Zalcitabine
What is it's analogue |
cytidine
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Stavudine
What is its analogue. |
Thymidine
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Lamivudine
What is it's analogue? This is the best tolerated of NRTI |
Cytodine
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Nevirapine
What does it do to p450. |
Induces
Not all NRTI inhibit p450 |
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Efavirenz
what does it do to p450 |
Induces
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Protease Inhibitors
what are the 2 side effects that we should know? |
Hyperlipidemia
Inhibits p450 |
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Delavridine
What does it do to p450? |
Inhibits
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Enfuvirtide
What is it and mech of act. |
A synthetic 36 amino acid long polypeptide that binds to viral gp41 protein and inhibits fusion of the viral envelope with cd4 t cell membranes
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Chemotherapeutic drugs are much more toxic to tissues with high growth factor than to tissue with low growth fraction.
True or false |
True
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What are problems of chemotherapy?
(2) |
1. No selectivity.
2. Follow first order kinetics |
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Combo Chemotherapy
Advantages |
1. Suppression of drug resistance
2. Increased cancer cell kill 3. Reduced injury to normal cells |
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Alkylating Agents
Nitrogen mustards Cyclophosphamide Frequently used with what drugs after breast cancer surgery? What else is it used for? Toxicities? What is acrolein and what does it cause? |
Most widely used alkylating agents
A prodrug activated in liver Methotrexate, Doxorubicin and Fluorouracil Leukemias, Lymphomas, and soft tissue cancers Bone marrow suppression, alopecia, and GI distress It is a toxic metabolite causing hemorraghic cystitis which can lead to fibrosis of liver. |
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Chemotherapy: Platinum Compounds
Cisplatin and Carboplatin Mech of act. Especially effective for what? |
Bifunctional binding of DNA and protients inhibiting both DNA replication and transcription leading to strand breaks and miscoding.
Testicular and ovarian cancer |
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Cisplatin
Side effect (4) |
Nephroxicity
GI distress Otoxocitiy Mutagenic, Teratogenic, carcinogenic |
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Carboplatin (1)
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Bone marrow suppression
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Chemotherapy: Antimetabolites
Pyrimidine analogs: 5-flurorouracil Mech of act. Used for? Used in combo with? Resistance (4) (Look it up) |
Inhibits DNA/RNA metabolism
Used for solid tumors Folinic Acid |
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Chemotherapy: Antimetabolites
Pyrimidine Analogs: 5-flurorouracil SE |
Bone marrow depression
Oral and GI ulceration Alopecia Hyperpigmentation Neurologic effects |
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Chemotherapy: Antitumor Antibiotics
Doxorubicin Resistance (3) |
Acceleration of drug efflux
Decreased DNA topoisomerase II activity Increased Glutathione peroxidase |
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Chemotherapy: Antitumor Antibiotics
Bleomycin Which cell cycle is it most effective on? Mech of act. It causes little bone marrow depression. |
G2
Binds to DNA causing strand scission and chain fragmentation. |
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Chemotherapy: Antitumor Antibiotics
Bleomycin SE |
Severe injury to the lungs
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Chemotherapy: Mitotic INhibitors
Vincristine Mech of act. This + corticosteroid is a tx of choice for what? Administration |
M phase specific. Drug disrupts the assembly of microtubles.
Childhood leukemia Poor penetration of CNS |
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Chemotherapy: Mitotic INhibitors
Vincristine SE |
Peripheral Neuropathy
Bone marrow sparing Strong Vesicant! (Causes blisters) |
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Chemotherapy: Mitotic INhibitors
Taxol Mech of Act Used for: Elimination: Resistance |
Stabilizes microtubules, binds to tubulin subunits, disrupts mitosis, acts during late g2 by promoting formation of stable microtuble bundles.
Breast, ovarian, lung, esophagus, bladder, and head and neck cancers. Extensive p450 metabolism and excreted in urine. Modified Beta tubulin MDR gene production |
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Chemotherapy: DNA topoisomerase II inhibitors
Etoposide Mech of act. Used for: |
It forms a ternary complex with DNA topoisomerase II and DNA leading to strand scission. The cell cycle is arrested at S to G2 transition.
Testicular, leukemia, small cell carcinoma of lung, hodgkins and large cell lymphomas |
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Chemotherapy: Drugs for breast cancer
Antiestrogens (SERMS): Tamoxifen First drug of choice for breast cancer Mech of act. |
Blocks E2 receptors in breast and agonist of endometrium.
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Chemotherapy: Drugs for breast cancer
Antiestrogens (SERMS): Raloxifene Mech of act. This drug is also used for what? |
Same as tamoxifene but this has no effect on endometrium.
Osteoperosis |
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Chemotherapy: Targeted Drugs
Angiogensis inhibitors Bevacizumab Mech of act. |
Inhibitors block the formation of new blood vessels so tumors can no longer grow.
So they don't kill directly. |
