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Pharm 5 > Unit 5 Drugs in Random Order > Flashcards

Unit 5 Drugs in Random Order Flashcards

1
Q

Maraviroc

A

Tx: HIV

Mech: Blocks binding site on macrophage preventing entry of virus

Fusion inhibitor

SE:

  • Hepatotoxicity
  • Allergies
  • Increase MI
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1
Q

Ethambutol

A

Antimycobacterial agent

Mech: Inh arabinosyl transferase

Necessary for CW synth

SE:

  • Optic neuritis
  • Impaired red/green discrimination
  • Decreased vision
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2
Q

Cilastatin

A

Given w/ impenem

Prevents nephrotoxic product by inh. enzyme

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2
Q

Antimycoplasma agents

A

NO CELL WALL!

So use non CW inhibitors:

Erythromycin

Tetracycline

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3
Q

Vancomycin

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Binds to dialanine residue on CW and prevents cross linking

Use: Severe infection in which B lactams can’t be used

Primary alt. to penicillins for staph infections.

Spectrum: G+

Route: IV–unless target in gut (pseudomembranous colitis)

SE:

  • Nephrotoxicity
  • Ototoxicity
  • If given rapidly via IV→histamine release→Redman or red neck syndrome
    • Flushing
    • Rash
    • Itching

Resistance:

  • Target changed
  • Dialanine changed to lactic acid

Dr. Van Ron

Dialanine Residue. Vancomycin. Redman. Ototox. Nephrotox

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4
Q

Sofosbuvir

A

Antiviral agent

Tx: Hepatitis virus (esp Hep C)

Mech: Inh HCV RNA dep RNA pol

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4
Q

Clindamycin

A

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
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4
Q

Rifampin

A

Antimycobacterial agent

Antibacterial agent

Mech: Inh DNA dep. RNA polymerase

-cidal

SE:

  • Hepatic toxicity
  • Red color in all body fluids
  • Induces P450–very strong
    • Can metabolize BC!

Rifampin=red

Will metabolize BC (induce P450) so the sperm will LIVEr

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5
Q

SE of cephalosporins

A

Allergic cross activity w/ penicillin sensitive pts

Possibility of superinfection

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6
Q

Cidofovir

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Prodrug-converted by host kinase

Used if resistance has occured so that host cells convert prodrug

SE: Renal damage

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7
Q

-floxacin

A

Antibacterial agent

Mech:

  • Inh topoisomerase II (DNA gyrase)
  • Inh topoisomerase IV

No effect on mammalian topoisomerase

SE:

  • May damage developing cartilage
    • Not for children or pregnant women
  • Tendonitis–achilles tendon rupture
  • Phototoxicity (drug in skin responds to sunlight)
  • May worsen myasthenia gravis

Spectrum: Broad–G+,G-, Acid fast

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8
Q

Metronidazole

A

Mech: Prodrug-converted to a free radical active molecule by obligate anaerobic bacteria

Route: IV for severe anaerobic bacterial inf.

Use: Protozoal inf:

  • Trichoma (STD)
  • Giardia (from water)

SE:

  • Seizures
  • Peripheral neuropathy
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9
Q

Famciclovir

A

Antiviral agent

Tx: herpes simplex and zoster

Mech: prodrug converted to acyclovir analog

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10
Q

Chloramphenicol

A

Antibacterial agent

Mech: inh. peptidyl transferase

SE:

  • Inh. P450
  • Can cause aplastic anemia
  • Gray baby syndrome
    • Metabolized by a phase II enzyme that is not active in newborns.
    • Can’t metabolize it→baby turns blue and circulatory system inhibited
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11
Q

-previr

A

Boceprevir

Telaprevir

Simeprevir

Antiviral agent

Tx: Hepatitis virus (esp Hep C)

Mech: HCV protease inh.

Virus makes proteins but cannot be processed to final stage

Used in comb. w/ interferon

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11
Q

Gramicidin

A

Antibacterial agent

Mixture of 3 diff peptide AB

Mech: forms pores in bacterial CM

Route: topical

NEVER give IV–toxic

Spectrum: G+

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12
Q

Foscarnet

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Not a prodrug–directly inh. DNA pol

Route: IV 3x/day

SE: Renal damage

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14
Q

Palivizumab

A

Antiviral agent

Tx: RNA virus (RSV)

Mech: vs antigenic site of RSV–blocks fusion of virus w/ target

Only used prophylactically

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14
Q

Terbinafine

A

Class: Antifungal

Mech: Inh. squalene epoxidase→inh. ergosterol synth

Inh. ergosterol synth→Increase in sqalene

Route: Systemic

Not well absorbed on skin

Most excreted unchanged

Metabolized and inhibits P450

SE:

  • Headache
  • Inhibit P450
  • Allergies
    • Derived from penicillium mold
  • Liver damage
  • SquaTer*
  • inh. Squalene epoxidase TERbinfine*
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14
Q

Carbenicillin

A

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
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14
Q

Telithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Same sites as erythromycin (50s) but induces less resistance b/c not readily transported out of bacterial cell

SE:

  • GI upset, nausea, and heartburn
  • Increase in GI activity b/c activates motilin
  • Inh P450
  • Liver damage-_SEVERE liver toxicity_
  • Arrythmias
  • Block cholinergic receptor
    • Worsen myasthenia gravis
    • Inh long ciliary ganglion→Decrease visual accomodation

macROlides like erythROmycin inh. transLOcation

Motility/ Myasthenia gravis worsens

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Ocular inh.

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14
Q

Bedaquiline

A

Antimycobacterial agent

Mech: inh. mycobacterial ATP synthetase

Always used w/ 3 other anti-TB drugs

SE:

  • Arrythmias
  • Increase incidence of death

*You’re in your bed MASTurbating and you go too hard and have an arrythmia *

_Bed_aquiline. Mycobacterial Atp SyntheTase. Arrythmia.

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15
Q

Penicillin G

A

Tx: Antibacterial

Mech: Bind to PBP→inh. transpeptidation

​inhibit an enzyme

Narrow spectrum: G+

Natural penicillin

Route: IV or IM–hydrolyzed w/ stomach acid

Given w/ procaine to slow release

Destroyed by B lactamase

Does not readily enter CNS

SE:

  • Allergic rxns→anaphylactic shock
  • High IV doses→seizures
  • B lactam ring may inh. GABAergic neurons
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17
Q

Ledipasvir

A

Antiviral agent

Tx: Hepatitis virus (esp Hep C)

Mech: Binds to and inh. protein thats necessary for HCV replication

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20
Q

Tenofovir

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE:

  • Lactic acidosis
  • Hepatomegaly

Discontinuation→Increase hepatitis symptoms

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20
Q

Isoniazid

A

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

Inh. mycobacterial enz.

  • Hepatotox.
  • O**ptic neuritis.

*Peripheral neuropathy + Pellegra. *

Prodrug + Prophylaxis

Increase excretion of vit B6→→

Niacin def.

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21
Q

Fluconazole

A

Antifungal triazole

-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

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22
Q

Methicillin

A

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

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22
Q

Amikacin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

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23
Q

Kanamycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

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23
Q

Pyrazinamide

A

Antimycobacterial agent

Mech: Inh FA synth

Prodrug converted in macrophase where TB lives

SE:

  • Gout
  • Hepatitis
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24
Q

Valganciclovir

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Prodrug-converted to ganciclovir by viral kinase

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24
Q

Voriconazole

A

Antifungal triazole

-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

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24
Q

Mezlocillin

A

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
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25
Q

Amoxicillin

A

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
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27
Q

Natamycin

A

Class: Antifungal

Polyene antibiotics

Route: Topical

Mech: Binds to ergosterol in fungal CM→pores→memb. leakage

Only one approved for use in eye

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27
Q

Tobramycin

A

Antibacterial

Class: Aminoglycosides-inhibit protein synth** **

-cidal

Mech: Irr. binds to 30s subunit

Inh. or alter tRNA binding along mRNA including initiation site

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28
Q

Ampicillin

A

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
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29
Q

Aztreonam

A

Antibacterial

Class: Monobactam

Route: IV or IM

Not affected by lactamases

Spectrum: Aerobic G- organisms

Not cross reactive w/ allergic pts

SE:

  • Seizures
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29
Q

Tetracycline

A

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
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31
Q

-gravir

A

Tx: HIV

Mech: Inh. HIV-1 integrase

Inh. insertion of viral genome into human

Prevents propagation

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32
Q

-zolid

A

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
33
Q

Clarithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Oral stability

vs. Helicobacter Pylori
* macROlides like erythROmycin inh. transLOcation*

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

Oral stability

34
Q

Imipenem

A

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
34
Q

Azithromycin

A

Antibacterial

Class: Macrolides-inhibit protein synth** **

Longer T1/2 (3 days)

macROlides like erythROmycin inh. transLOcation

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

O——

36
Q

Nystatin

A

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

36
Q

Mupirocin

A

Mech: Binds to bacterial isoleucyl tRNA synthetase

Route: Topical

Use: Staph inf.

37
Q

Piperacillin

A

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
39
Q

Antifungals for candida+ ringworm

A

Miconazole

and other “conazoles”

Route: Topical and systemic

39
Q

Daptomycin

A

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
40
Q

-amivir

A

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

40
Q

Bacitracin

A

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
42
Q

Protease inh.

A

-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
43
Q

Sulfisoxazole

A

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

44
Q

Efavirenz

A

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 EFavirenz to get EFfed up*
  • hallucinations and mem loss*
45
Q

Posaconazole

A

Antifungal triazole

-static

Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase

So inh. ergosterol synth

SE:

  • Less effect on human P450 (triazole vs imidazole)

Posaconazole is sucha pussy, it hardly inhibits our P450

46
Q

Ganciclovir

A

Antiviral agent

Tx: CMV (herpes virus)

CMV→retinitis+ blindness

Mech: Inhibits viral DNA pol

Prodrug-activated by viral kinase

SE:

  • Neutropenia
  • Thrombocytopenia
  • Teratogen
48
Q

Flucytosine

A

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
50
Q

“-oxacillin”s

A

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

52
Q

Rimantadine

A

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
54
Q

Nafcillin

A

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

55
Q

-fungin

A

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
56
Q

Enfuvirtide

A

Tx: HIV

Mech: binds to specific site on virus that binds to target

Fusion inhibitor

SE: Insomnia

57
Q

Retapamulin

A

Antibacterial agent

Mech: inh. peptidyl transferase

Route: Topical

Use: skin staph or strep inf.

58
Q

Lamivudine

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

Discontinuation→Increase hepatitis symptoms

59
Q

Valacyclovir

A

Antiviral drug

Tx: Herpes simplex and zoster

Mech: Prodrug converted to acyclovir

Must be given orally-prodrug metab. by 1st pass metab.

60
Q

Streptomycin

A

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*

Fetal damage

Ototox.

Renal tox

Negative (G-)

Irr. bind 30s

Cidal

*ACh block *

tRNA can’t bind to mRNA

  • *
62
Q

Nevirapine

A

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
62
Q

-virine

A

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
63
Q

Ribavirin

A

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

64
Q

Meropenem

A

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
66
Q

Cycloserine

A

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 PTSd*
  • Psychosis*
  • Tremors*
  • Sedation*
66
Q

Erythromycin

A

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

Motility

Arrythmia

Cholestatic hepatitis (liver tox)

Restricts P450

O——

67
Q

-pristin

A

Quinupristin (A+P site)

Dalfopristin (P site)

Mech: Inh. A and P sites

Always used together–synergistic

SE: Muscle pain

Spectrum: G+

69
Q

Amphotericin B

A

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)

*Anemia, Nephro fxn impaired, Fever *

or

AMPHTERIC

Anemia

Muscular contractions

Pores in membrane

Headache

Temp increase

Emesis

Renal fxn impaired

IV or intrathecal

Chills

71
Q

Carbapenems

A

Tx: Antibacterial–mixed infections

Penicillin analog

Small penicillinase resistant B lactam

Spectrum: Very broad

Route: IV

SE:

  • Can enter CNS→Seizures
72
Q

Lincomycin

A

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
73
Q

Clavulanic acid

A

Mech: Bind to and inh. B lactamase

Non antibiotic B-lactam ring compounds

74
Q

Antifungals for ringworm

A

Tolfnaftate

Ciclopirox

Terbinafines and other “fines”

Route: Topical

75
Q

Telbivudine

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE:

  • Lactic acidosis
  • Hepatomegaly

Discontinuation→Increase hepatitis symptoms

76
Q

Nitrofurantoin

A

Mech: Reduced by bacteria to a highly reactive molecule

Concentrates in urine

Use: UTI

SE:

  • Cough
  • Chest pain
  • Brown urine
78
Q

Entecavir

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE:

  • Lactic acidosis
  • Hepatomegaly

Discontinuation→Increase hepatitis symptoms

79
Q

Ticarcillin

A

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
81
Q

Amantadine

A

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
82
Q

Gentamycin

A

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

83
Q

Sulbactam

A

Mech: Bind to and inh. B lactamase

Non antibiotic B-lactam ring compounds

84
Q

“-vancin”s

A

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
85
Q

Fidaxomycin

A

Antibacterial agent

Mech: Inh. C. dificile RNA pol

Orally–Not systemically absorbed

Target: C. dificile

86
Q

Adefovir

A

Antiviral agent

Tx: Hep B

Mech: Inh. Hep B reverse transcriptase

SE: Liver and renal damage

Discontinuation→Increase hepatitis symptoms

88
Q

Itraconazole

A

Antifungal triazole

-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

ItrAConazole→Arrythmias or CHF

89
Q

Delavirdine

A

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.
90
Q

Neomycin

A

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

91
Q

Ketoconazole

A

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 LIVEr forever…l_iver tox_*
92
Q

Netilmicin

A

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

93
Q

Griseofulvin

A

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. P450 induction, Headache, Allergies, t_reats _Toenail inf.

95
Q

Fosfomycin

A

Antibacterial

Class: Non B lactam CW inhibitors

Mech: Blocks synth of NAM

Spectrum: Aerobic G-

Use: Uncomplicated UTI

SE:

  • Diarrhea–killing bacteria in gut
96
Q

Penicillin V

A

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
98
Q

Acyclovir

A

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
99
Q

Polymixin B

A

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. Perioral paresthesia. Ataxia. Neurotoxic. Nephrotoxic. Neuromuscular blockade. binds to Negatively charged sites on LPS*
100
Q

Harvoni

A

DOC for HCV

Ledipasvir+sofosbuvir

101
Q

Dapsone

A

Antimycobacterial agent

Related to sulfonamides

Mech: Reversible inh. dihydropterate synthetase

Use: For mycobacterium leprae (leprosy

102
Q

Recombinant interferon alpha

A

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.
103
Q

Trimethoprim

A

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

Pharm 5 (4 decks)

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