Unit 5 Drugs in Random Order Flashcards

Question

Tenofovir

Answer 1

Antiviral agent Tx: Hep B Mech: Inh. Hep B reverse transcriptase SE: * Lactic acidosis * Hepatomegaly Discontinuation→Increase hepatitis symptoms

Answer 2

Antimycobacterial agent Mech: Produces inh. of multiply mycobacterial enzymes Inh CW synth Prodrug Cidal, but static for dormant cells Used alone for prophylaxis--in combo for active tx Metabolized by acetylation--slow acetylators affected SE: * Increase excretion of vit B6→pyroxidase deficiency→niacin deficiency * Pellegra * Peripheral neuropathy * Optic neuritis * Hepatotoxicity *Isoniazid is IHOPPIN* ***I**nh. mycobacterial enz.* * **H**epatotox. * *O**ptic neuritis.* ***P**eripheral neuropathy + Pellegra. * ***P**rodrug + Prophylaxis* ***I**ncrease excretion of vit B6→→* ***N**iacin def.*

Answer 3

Antifungal *tri*azole *-static* Mech: _Inh fungal P450_, including lanosterol-14-alpha-demethylase So inh. ergosterol synth SE: * Least effect on human P450 * Teratogenic * Liver damage * Hallucinations *FLUCking may lead to birth defects (teratogenic)* LUCy in the sky with diamonds=LSD=Hallucinations

Answer 4

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation inhibit an enzyme _B-lactamase resistant_ Narrow spectrum: G+ Does not readily enter CNS **Do not use anymore-too toxic**

Answer 5

Antibacterial **Class**: Aminoglycosides-inhibit protein synth** ** **-cidal** **Mech**: Irr. binds to 30s subunit Inh. or alter tRNA binding along mRNA including initiation site

Answer 6

Antibacterial **Class**: Aminoglycosides-inhibit protein synth** ** **-cidal** **Mech**: Irr. binds to 30s subunit Inh. or alter tRNA binding along mRNA including initiation site

Answer 7

Antimycobacterial agent Mech: Inh FA synth Prodrug converted in macrophase where TB lives SE: * Gout * Hepatitis

Answer 8

Antiviral agent **Tx**: CMV (herpes virus) CMV→retinitis+ blindness **Mech**: Inhibits viral DNA pol Prodrug-converted to ganciclovir by viral kinase

Answer 9

Antifungal *tri*azole *-static* Mech: _Inh fungal P450_, including lanosterol-14-alpha-demethylase So inh. ergosterol synth SE: * Less effect on human P450 (triazole vs imidazole) * Can cause visual disturbances ***_V_**oriconazole causes **_V_**isual disturbances*

Answer 10

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation _inhibit an enzyme_ **Broad spectrum** Does not readily enter CNS SE: * Allergic rxns→anaphylactic shock * High IV doses→seizures * B lactam ring may inh. GABAergic neurons

Answer 11

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation _inhibit an enzyme_ **Broad spectrum** Route: Oral Does not readily enter CNS SE: * Allergic rxns→anaphylactic shock * B lactam ring may inh. GABAergic neurons

Answer 12

**Class**: Antifungal *Polyene antibiotics* **Route**: _Topical_ **Mech**: Binds to ergosterol in fungal CM→pores→memb. leakage **Only one approved for use in eye**

Answer 13

Antibacterial **Class**: Aminoglycosides-inhibit protein synth** ** **-cidal** **Mech**: Irr. binds to 30s subunit Inh. or alter tRNA binding along mRNA including initiation site

Answer 14

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation _inhibit an enzyme_ **Broad spectrum** Does not readily enter CNS SE: * _Rash in pts who have mononucleosis +other viral inf._ * Allergic rxns→anaphylactic shock * High IV doses→seizures * B lactam ring may inh. GABAergic neurons

Answer 15

Antibacterial Class: Monobactam Route: IV or IM Not affected by lactamases Spectrum: Aerobic G- organisms _Not_ cross reactive w/ allergic pts SE: * Seizures

Answer 16

Tx: * Rickettsia * Spirochetes (lyme disease) * Helicobacter * Legionella Mech: Reversibly bind to 30s. Inhibits the binding of tRNA to the A site -static SE * Deposited in Ca storage sites-bones/teeth-esp fetus or child * Binds to cations, esp Ca, also Fe and Al. * Preg risk D * Renal and hepatic toxicity * Degrades to toxins--don't use after expiration date

Answer 17

Tx: HIV Mech: Inh. HIV-1 integrase Inh. insertion of viral genome into human Prevents propagation

Answer 18

Linezolid Tedizolid Mech: Inh. binding of fmet (start codon) tRNA to P site Prevents initiation of protein synth. SE * Anemia * Pseudomembranous colitis * Will happen w/ any powerful AB b/c of C. dificile

Answer 19

Antibacterial **Class**: Macrolides-inhibit protein synth** ** _Oral stability_ vs. Helicobacter Pylori * macROlides like erythROmycin inh. transLOcation* ***M**otility* ***A**rrythmia* ***C**holestatic hepatitis (liver tox)* ***R**estricts P450* ***O**ral stability*

Answer 20

Tx: Antibacterial--mixed infections Class: Carbapenem Penicillin analog Small penicillinase resistant B lactam Spectrum: Very broad-**Better against G+** Route: IV SE: * Can enter CNS→Seizures * Metabolized in kidney to nephrotoxic product * Given w/ **cilastatin** which inh. enzyme that produces toxic product

Answer 21

Antibacterial **Class**: Macrolides-inhibit protein synth** ** _Longer T1/2_ (3 days) *macROlides like erythROmycin inh. transLOcation* ***M**otility* ***A**rrythmia* ***C**holestatic hepatitis (liver tox)* ***R**estricts P450* *O------*

Answer 22

**Class**: Antifungal *Polyene antibiotics* **Mech**: Binds to ergosterol in fungal CM→pores→memb. leakage **Route**: _Topical_ Can give orally, but only for fungi in gut Too toxic for parenteral use

Answer 23

Mech: Binds to bacterial isoleucyl tRNA synthetase Route: Topical Use: Staph inf.

Answer 24

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation _inhibit an enzyme_ **Broad spectrum** Does not readily enter CNS SE: * Allergic rxns→anaphylactic shock * High IV doses→seizures * B lactam ring may inh. GABAergic neurons

Answer 25

Miconazole and other "conazoles" Route: Topical and systemic

Answer 26

Antibacterial agent--lipopeptide Mech: Forms pores in bacterial CM Targets: Aerobic G+ (staph, strep) Skin and soft tissue inf. or severe blood inf w/ S. aureus SE: * Muscle pain and weakness * *careful w/ statins* * Eosinophilic pneumonia

Answer 27

Zanamivir Oseltamivir Antiviral agent Tx: Influenza A+B virus (RNA virus) Virus leaves cell and is attached by tether of neuraminic acid Release of virus requires neuraminidase Mech: Neuraminidase inh. So virus cannot be released from cell and spread SE: * Nausea * Diarrhea * Psychosis * Hallucinations * Zanamivir is a powder that must be inhaled so asthma issues Only shorten influenza by about a day

Answer 28

Antibacterial **Class**: Non B lactam CW inhibitors Polypeptide **Mech**: Inh. recycling of bactoprenol carrier **Spectrum**: G+ **Route**: Topically--very toxic SE: * Nephrotoxicity--if not given topically

Answer 29

-navir Antiviral agent Tx: HIV Mech: Protease inh. Prevent formation of active viral proteins from their peptide precursor Most inh. P450 Some are absorbed poorly via oral route and 18 capsules must be taken/day Ritonavir is most potent known P450 inh so it is given w/ the poorly absorbed protease inh to avoid taking so many Ritonavir given w/: SALTD * Saquinavir * Atazanavir * Lopinavir * Tipranavir * Darunavir SE: * Alter fat distribution * Loss of fat in face and limbs * Gain fait in gut, chest, and back * Increase diabetes * Some have sulfur groups→allergies * Tipranavir * Fosamprenavir

Answer 30

PABA\*→folic acid→DHFA\*\*→THFA \*→=Dihydropterate synthetase \*\*→DHFR Mech: Reversible inh. dihydropterate synthetase For UTIs SE: * Allergic whole body rash (Stevens Johnson syndrome) * Hemolytic anemia in G6PDH deficient pts * Megaloblastic anemia *Sulfa drugs have sulf or sul*

Answer 31

Antiviral agent Tx: HIV Mech: bind to non active sites and Inh reverse trans Not competetive inh. 1st gen NNRTI SE * CNS- so some people crush it up and smoke it * hallucinations * memory loss * Rash * Smoke **_EF_**avirenz to get **_EF_**fed up* * hallucinations and mem loss*

Answer 32

Antifungal *tri*azole *-static* Mech: _Inh fungal P450_, including lanosterol-14-alpha-demethylase So inh. ergosterol synth SE: * Less effect on human P450 (triazole vs imidazole) **_Posa_**conazole is sucha **_pussy_**, it hardly inhibits our P450

Answer 33

Antiviral agent **Tx**: CMV (herpes virus) CMV→retinitis+ blindness **Mech**: Inhibits viral DNA pol Prodrug-activated by viral kinase SE: * Neutropenia * Thrombocytopenia * Teratogen

Answer 34

Antifungal agent Pyrimidine analog **Mech**: Inh thymidine synth. in fungi Converted to 5-fluororacil→inh. thymidilate synthatase So inh DNA and RNA synth Prodrug-enters fungus by specific enzymes Does not enter human SE: * Bone marrow depression→anemia * Liver toxicity * GI upset

Answer 35

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation _inhibit an enzyme_ _B-lactamase resistant_ Narrow spectrum: G+ Does not readily enter CNS SE: * Allergic rxns→anaphylactic shock * High IV doses→seizures * B lactam ring may inh. GABAergic neurons *OXacillin=OX is strong animal, resistant to penicillinase*

Answer 36

Antiviral agent Tx: RNA virus (Influenza A virus) Virus taken up by cell endosome→opens channel in endosome→H enters→virus can release genes Mech: Blocks process by which H channel forms in endosome _Blocks transporter or ion channel_ Used proph. or very early _Widespread resistance_ SE: Fewer than amantidine but similar SE * Renal failure * Teratogen * CNS fx * Dizziness * Slurred speech * Confusion * Seizures * Nausea

Answer 37

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation inhibit an enzyme _B-lactamase resistant_ Narrow spectrum: G+ Does not readily enter CNS SE: * Allergic rxns→anaphylactic shock * High IV doses→seizures * B lactam ring may inh. GABAergic neurons *NAFcillin=Not AFfected by penicillinase*

Answer 38

Caspofungin Micafungin Anidulafungin Antifungal agent -cidal Mech: Inh. synth of fungal CW component **Enzyme inhibitor** Route: Slow IV Not readily absorbed SE: * Rash * Fever * Fetal Damage

Answer 39

Tx: HIV Mech: binds to specific site on virus that binds to target Fusion inhibitor SE: Insomnia

Answer 40

Antibacterial agent Mech: inh. peptidyl transferase Route: Topical Use: skin staph or strep inf.

Answer 41

Antiviral agent Tx: Hep B Mech: Inh. Hep B reverse transcriptase Discontinuation→Increase hepatitis symptoms

Answer 42

Antiviral drug Tx: Herpes simplex and zoster Mech: Prodrug converted to acyclovir Must be given orally-prodrug metab. by 1st pass metab.

Answer 43

Antibacterial **Class**: Aminoglycosides-inhibit protein synth** ** **-cidal** **Mech**: Irr. binds to 30s subunit Inh. or alter tRNA binding along mRNA including initiation site **Spectrum**: Aerobic G- Must be absorbed by active transport **SE:** * Ototoxicity * Hearing and balance affected * hearing loss may be permanent * Nephrotoxic * Most common cause of drug induced renal failure * Used very widely * High doses * Neuromuscular blockade * Decrease in ACh+ ACh receptors on mm * Fetal damage * _Preg cat. D_ __ * Strippers fornicate* * Strep. FORNICAT* ***F**etal damage* ***O**totox.* ***R**enal tox* ***N**egative (G-)* ***I**rr. bind 30s* ***C**idal* ***A**Ch block * ***t**RNA can't bind to mRNA* * *

Answer 44

Antiviral agent Tx: HIV Mech: bind to non active sites and Inh reverse trans Not competetive inh. 1st gen NNRTI SE * Hepatotoxicity * Stevens Johnson syndrome

Answer 45

Etravirine Rilpivirine Antiviral agent Tx: HIV Mech: bind to non active sites and Inh reverse trans Not competetive inh. 2nd gen NNRTI Differ from first gen: * Higher potency * Longer T1/2 * Fewer SE

Answer 46

Antiviral agent Tx: RNA virus (RSV) Only for severe lower resp inf. Mech: Inh RNA dep DNA pol Phosphorylated in cell. SE: * Preg cat X * Hemolytic anemia * Decrease pulmonary fxn in infants * Cardiac arrest Not used much anymore. Very expensive

Answer 47

Tx: Antibacterial--mixed infections Class: Carbapenem Penicillin analog Small penicillinase resistant B lactam Spectrum: Very broad-**Better against G-** Route: IV SE: * Can enter CNS→Seizures

Answer 48

Antibacterial **Class**: Non B lactam CW inhibitors **Mech**: Inh. incorporation of alanine into NAM _Enzyme inhibitor_ Used against mycobacterium TB SE: * CNS * Sedation * Tremor * Psychosis * Cyclo- gives you psycho-* * Go to war in **NAM**, when you come back you have **PTS**d* * Psychosis* * Tremors* * Sedation*

Answer 49

Antibacterial **Class**: Macrolides-inhibit protein synth -static **Mech**: Reversibly binds to 50s subunit and inh. translocation of mRNA Inh binding of tRNA to P site **Spectrum**: G+ SE: * GI upset, nausea, and heartburn * Increase in GI activity b/c activates motilin * Inh P450 * Liver damage * Arrythmias *macROlides like erythROmycin inh. transLOcation* ***M**otility* ***A**rrythmia* ***C**holestatic hepatitis (liver tox)* ***R**estricts P450* *O------*

Answer 50

**Quinupristin** (A+P site) **Dalfopristin** (P site) Mech: Inh. A and P sites Always used together--synergistic SE: Muscle pain Spectrum: G+

Answer 51

**Class**: Antifungal * Polyene antibiotic* * -cidal* ***_DOC_*** of systemic mycotic inf. **Mech**: Binds to ergosterol in fungal CM→pores→memb. leakage **Route**: Slow IV (2-4 mnths) or intrathecal Must be given w/ detergent b/c not soluble in H2O Topical too SE: "amphoterrible" * Impaired renal fxn * Fever, chills, vomiting, convulsions, severe headache * Anemia *Amph SE=ANF (sounds similar)* ***A**nemia, **N**ephro fxn impaired, **F**ever * or AMPHTERIC **A**nemia **M**uscular contractions **P**ores in membrane **H**eadache **T**emp increase **E**mesis **R**enal fxn impaired **I**V or intrathecal **C**hills

Answer 52

Tx: Antibacterial--mixed infections Penicillin analog Small penicillinase resistant B lactam Spectrum: Very broad Route: IV SE: * Can enter CNS→Seizures

Answer 53

Antibacterial agent--lincosamide Mech: like erythromycin-inh. translocation SE: Severe superinf. w/ C. dificile Targets: * Severe anaerobic infections (penetrating gut wound) * Dental prophylaxis in pts w/ heart valve problems

Answer 54

Mech: Bind to and inh. B lactamase Non antibiotic B-lactam ring compounds

Answer 55

Tolfnaftate Ciclopirox Terbinafines and other "fines" Route: Topical

Answer 56

Antiviral agent Tx: Hep B Mech: Inh. Hep B reverse transcriptase SE: * Lactic acidosis * Hepatomegaly Discontinuation→Increase hepatitis symptoms

Answer 57

Mech: Reduced by bacteria to a highly reactive molecule Concentrates in urine Use: UTI SE: * Cough * Chest pain * Brown urine

Answer 58

Antiviral agent Tx: Hep B Mech: Inh. Hep B reverse transcriptase SE: * Lactic acidosis * Hepatomegaly Discontinuation→Increase hepatitis symptoms

Answer 59

Tx: Antibacterial Mech: Bind to PBP→inh. transpeptidation _inhibit an enzyme_ **Broad spectrum** Does not readily enter CNS SE: * Allergic rxns→anaphylactic shock * High IV doses→seizures * B lactam ring may inh. GABAergic neurons

Answer 60

Antiviral agent Tx: RNA virus (Influenza A virus) Virus taken up by cell endosome→opens channel in endosome→H enters→virus can release genes Mech: Blocks process by which H channel forms in endosome _Blocks transporter or ion channel_ Used proph. or very early SE: * Renal failure * Teratogen * CNS fx * Dizziness * Slurred speech * Confusion * Seizures * Nausea

Answer 61

Antibacterial **Class**: Aminoglycosides-inhibit protein synth** ** **-cidal** **Mech**: Irr. binds to 30s subunit Inh. or alter tRNA binding along mRNA including initiation site _**Use: **Ointment for eye_

Answer 62

Mech: Bind to and inh. B lactamase Non antibiotic B-lactam ring compounds

Answer 63

**Televancin** **Dalbavancin** Antibacterial **Class**: Non B lactam CW inhibitors Lipoglycopeptide **Mech**: Binds to _dialanine residue_ on CW and prevents cross linking + disrupt bacterial CM SE: * Nephrotoxicity * Fetal damage * Metallic taste

Answer 64

Antibacterial agent Mech: Inh. C. dificile RNA pol Orally--Not systemically absorbed Target: C. dificile

Answer 65

Antiviral agent Tx: Hep B Mech: Inh. Hep B reverse transcriptase SE: Liver and renal damage Discontinuation→Increase hepatitis symptoms

Answer 66

Antifungal *tri*azole *-static* Mech: _Inh fungal P450_, including lanosterol-14-alpha-demethylase So inh. ergosterol synth SE: * *Strongest* effect on human P450 of the triazoles * Worsen CHF or arrythmias ***_I**_traconazole is the strongest _**I_**nhibitor of P450* *Itr**AC**onazole→**A**rrythmias or **C**HF*

Answer 67

Antiviral agent Tx: HIV Mech: bind to non active sites and Inh reverse trans Not competetive inh. _Not as effective_ 1st gen NNRTI SE * Hepatotoxicity * Stevens Johnson syndrome * _P450 inh._

Answer 68

Antibacterial **Class**: Aminoglycosides-inhibit protein synth** ** **-cidal** **Mech**: Irr. binds to 30s subunit Inh. or alter tRNA binding along mRNA including initiation site Route: Topical or oral _**SE: **Very nephrotoxic_*--so only topically or orally*

Answer 69

Antifungal imidazole Mech: _Inh fungal P450_, including lanosterol-14-alpha-demethylase So inh. ergosterol synth SE: * Nausea * GI upset * Hepatic toxicity * Inh. human P450-Strongest inh. of the conazoles * Decrease in adrenal and gonal steroid synth * Decrease cortisol (tx of Cushing's) * Decrease test. (tx of prostate cancer) * Ket...ocon..azole* * Ket azole=cat asshole* * So GI, nausea, and prostate cancer tx* * And cat's have 9 lives so they **_LIVE_**r forever...l_iver tox_*

Answer 70

Antibacterial **Class**: Aminoglycosides-inhibit protein synth** ** **-cidal** **Mech**: Irr. binds to 30s subunit Inh. or alter tRNA binding along mRNA including initiation site _DROPPED in the US_

Answer 71

**Class**: Antifungal **Tx:** Nail inf. *Nail inf. must be treated systemically to avoid painful tx* **Mech**: Binds to fungal microtubules→inh. fungal mitosis *Taken up by growing human skin cells and concentrated in keratin* **Route**: Systemic Not well absorbed on skin Most excreted unchanged SE: * Headache * Induction of P450 * Allergies * Derived from penicillium mold * Eat _greasy_ fries and you will get _fat_ * * Eat _grise_ _microtubules_ (fries) and you will get _PHAT_* *_Griseofulvin_ binds _microtubules_. _**P**450 induction, **H**eadache, **A**llergies, t_reats _**T**oenail inf._*

Answer 72

Antibacterial **Class**: Non B lactam CW inhibitors **Mech**: Blocks synth of NAM **Spectrum**: Aerobic G- **Use**: Uncomplicated UTI SE: * Diarrhea--killing bacteria in gut

Answer 73

Tx: Antibacterial **Mech**: Bind to PBP→inh. transpeptidation _inhibit an enzyme_ Narrow spectrum: G+ **Route**: **Oral** _Natural_ penicillin Absorption unpredictable Destroyed by B lactamase Does not readily enter CNS SE: * Allergic rxns→anaphylactic shock * B lactam ring may inh. GABAergic neurons

Answer 74

Antiviral drug Tx: Herpes simplex and zoster **Mech**: Incorporated into DNA and inh. viral DNA pol Prodrug-must be phosphorylated by viral kinase Only occurs in active cells Much higher affinity for viral DNA pol **Route**: IV and oral (not well absorbed though) SE: * GI upset * Renal damage * CNS problems * Delerium when given IV

Answer 75

Antibacterial agent Mech: Binds to negatively charged sites on LPS of G- bact →to memb. permeability Route: Topical SE: (all reversible) * Nephrotoxic * Neurotoxic * Neuromuscular blockade * Ataxia * Perioral paresthesia * Poly mixes in her PANNNN* * Polymixin B. **P**erioral paresthesia. **A**taxia. **N**eurotoxic. **N**ephrotoxic. **N**euromuscular blockade. binds to **N**egatively charged sites on LPS*

Answer 76

DOC for HCV Ledipasvir+sofosbuvir

Answer 77

Antimycobacterial agent Related to sulfonamides Mech: Reversible inh. dihydropterate synthetase Use: For mycobacterium leprae (leprosy

Answer 78

Antiviral agent Tx: Hepatitis virus (esp Hep C) Cytokine w/ multiple mech Mech: * Immunostimulant * Inh. mRNA processing * Decrese viral synth SE: * Fatigue * Flu-like symptoms * Depression * Hypertensino * Retinopathy * Myelosuppression→fewer platelets, granulocytes, etc.

Answer 79

Antibacterial agent Mech: Inh. DHFR (like methotrexate) Specific for bact. enzyme *Used in conj. w/ sulfamethoxazole * SE: * Megaloblastic anemia * Can be avoided w/ leucovorin Targets: * G- bacteria * UTIs * Concentrates in acidic prostate and vaginal tissue