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Final Year MBBS > Pharmacology - Infection > Flashcards

Pharmacology - Infection Flashcards

1
Q

Inhibitors of cell wall synthesis

A
  • β lactams:
    • ​Penicillins
    • Cephalosporins
  • Glycopeptides:
    • ​Vancomycin
    • Teicoplanin
  • Carbapenems:
    • ​Imipenem
  • Monobactams:
    • ​Aztreonam
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2
Q

Inhibitors of nucleic acid synthesis

A
  • Quinolones
    • ​Ciprofloxacin
  • Others:
    • ​Metronidazole
    • Trimethoprim
    • Rifampicin
    • Sulphonamides
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3
Q

Inhibitors of protein synthesis

A
  • Aminoglycosides:
    • ​Gentamicin
  • Tetracyclines
    • ​Tetracycline
    • Doxycyline
  • Macrolides
    • ​Erythromycin
    • Clarithromycin
  • Others
    • ​Chloramphenicol
    • Fusidic acid
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4
Q

Penicillins

A

Indications: Very useful against Gram +ve bacteria
MOA: Bactericidal → inhibit bacterial transpeptidase, an enzyme required for cell wall synthesis
SE’s: Hypersensitivity: rash, EM, anaphylaxis. GI upset, maculopapular rash in EBV, diarrhoea
CI’s: Hypersensitivity (10% cross-reactivity with cephalosporins)
Interactions: May reduce effect of OCP, increased by probenecid
Other: PenV + PenG (IV) = Strep’s N. meningitidis, syphilis
Amox + ampicillin = broad spec: pneumococcus, listeria, E.coli, enterococci
Fluclox = penicillinase-resistant, MRSA
Piperaccillin + ticarcillin = anti-pseudomonal
Coamoxiclav = severe CAP, UTI
Tazocin = Severe HAP, sepsis

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5
Q

Cephalosporins

A

Indications: Broad spec Abx - used in: septicaemia, pneumonia, meningitis, biliary tract infections, peritonitis, UTI’s
MOA: Bactericidal: inhibit bacterial transpeptidase → required for cell wall construction. Generations have increasing activity against Gram -ves
SE’s: GI upset → antibiotic associated colitis, headache, allergic reactions
CI’s: Hypersensitivity
Interactions:
Other: 1st gen: cephalexin → UTI (rarely used)
2nd gen: cefuroxime → mod/severe CAP, GI sepsis, pre-op
3rd gen: cefotaximine, cefriaxone, ceftazidime, cefixime → meningitis, epiglottitis, gonorrhoea, SBP

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6
Q

Carbapenems

A

Indications: Broad spec Abx: covers Gram -ve, +ve (except MRSA), anaerobes + pseudomonas. Used for nosocomial infections (neutropenic sepsis)
MOA: Bactericidal - inhibit bacterial transpeptidase - required for cell wall construction
SE’s: GI upset - N/V, seizures
CI’s: Avoid if pt has Hx of immediate hypersensitivity to β-lactams. Reduce dose in renal impairment
Interactions: Reduce concentration of valproate
Other: Imipenam = rapidly inactivated by kidney, give with cilastatin → blocks it’s metabolism
Meropenam
Ertapenam

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7
Q

Chloramphenicol

A

Indications: Superficial eye infections - conjunctivitis
MOA: Bacteriostatic - inhibits the 50s subunit → prevents peptide bond formation and thus inhibits protein synthesis
SE’s: Irreversible aplastic anaemia (not used for other infections), grey baby syndrome if oral use in 3rd trimester
CI’s: Pregnancy, lactation, renal disease
Interactions:
​Other:

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8
Q

Gentamicin

Amikacin

Tobramycin

Neomycin

Streptomycin

A
  • *Indications:** Gram -ve sepsis, neutropenic sepsis, otitis externa, anti-pseudomonal. Streptomycin used in TB
  • *MOA:** Aminoglycosides → bactericidal → inhibit aminoacyl site of 30s subunit, inhibiting protein synthesis
  • *SE’s:** Dose related. Nephrotoxic → check renal function before + during Rx. Ototoxic → direct damage to CN VIII
  • *CI’s:** MG, pregnancy, caution in renal impairment - alter dose/time
  • *Interactions:** Loop diuretics, ciclosporin. Reduced absorption with milk + antacids
  • *​Other:** Must monitor levels → peak + trough. Given IV (inactive orally)
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9
Q

Tetracycline

Doxycyline

A
  • *Indications:** COPD exacerbation, acne, chlamydia, rickettsia, brucella, lyme disease (intracellular organisms)
  • *MOA:** Bacteriostatic - inhibit 30s subunit → inhibit protein synthesis
  • *SE’s:** GI upset, hypersensitivity, photosensitivity
  • *CI’s:** Children < 12 yrs, liver + renal disease, pregnancy → causes discolouration of baby’s teeth
  • *Interactions:** Toxicity increased by frusemide, cephalosporins, vancomysin, ciclosporin
  • *​Other:**
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10
Q

Linezolid

A

Indications: Active against gram +ve including MRSA + VRE. No action against gram -ves
MOA: Oxazolidinone → bacteriostatic - inhibit 23s component of 50s subunit (also is a MAOI)
SE’s: Diarrhoea (Abx associated colitis), N+V, blood dyscrasias
CI’s: Giving with another MAOI, SSRIs, triptans, TCAs, opioids, tyramine, uncontrolled HTN, phaeo, thyrotoxicosis, BPAD, schizo etc.
Interactions:
​Other: Monitor FBC

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11
Q

Erythromycin

Clarithromycin

Azithromycin

A
  • *Indications:** Penicillin allergy, atypical pneumonia, chlamydia, H.pylori
  • *MOA:** Macrolides: bacteriostatic → inhibits the 50s subunit - inhibiting protein synthesis
  • *SE’s:** Dry skin, cholestatic hepatitis, N+V, prolonged QTc
  • *CI’s:** Caution if prolonged QTc
  • *Interactions:** P450 inhibitor. Increases digoxin.
  • *​Other:** Also have GI prokinetic action. Don’t cross BBB
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12
Q

Synercid

A

Indications: VRE, MRSA
MOA: Streptogramins - bacteriostatic: 50S subunit inhibition of protein synthesis
SE’s:
CI’s:
Interactions:
Other:Only used when other agents failed

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13
Q

Clindamycin

A
  • *Indications:** Gram +ve cocci (strep + penicillin resistant staph) and many anaerobes (osteomyelitis, MRSA)
  • *MOA:** Lincosamides - bacteriostatic - 50S subunit, inhibits protein synthesis
  • *SE’s:** Antibiotic associated colitis!! Hepatotoxicity, N+V, oesophageal ulcers etc.
  • *CI’s:** Diarrhoea
  • *Interactions:** Enhances suxamethonium
  • *Other:** Stop if patient develops diarrhoea
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14
Q

Vancomycin

Teicoplanin

A
  • *Indications:** Gram +ve (aerobic + anaerobic), MRSA, infective endocarditis, Abx associated colitis
  • *MOA:** Glycopeptides - bactericidal: inhibits cell wall synthesis - prevents NAM + NAG form. Not active against Gram -ve as can’t penetrate cell wall
  • *SE’s:** Nephrotoxic, ototoxic (tinnitus, SNHL), hypersensitivity, neutropenia
  • *CI’s:** Renal impariment → reduce dose
  • *Interactions:** Aminoglycosides - increased risk of nephro/ototoxicity with vanc
  • *Other:** Must monitor levels → predose trough level
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15
Q

Ciprofloxacin

Levofloxacin

Ofloxacin

Moxifloxacin

A
  • *Indications:** Broad spec, esp Gram -ves, GI infections (campylobacter, shigella etc), pseudomonas esp in CF, prostatitis, PID, anthrax
  • *MOA:** Fluoroquinilones - bactericidal → inhibits DNA gyrase
  • *SE’s:** GI upset, tendonitis +/- rupture, reduced seizure threshold, photosensitivity, prolonged QTc
  • *CI’s:** Pregnancy, epilepsy, Hx of tendon damage
  • *Interactions:** P450 inhibitor. Antacids reduce absorption
  • *Other:**
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16
Q

Metronidazole

Nitrofurantoin

Tinidazole

A
  • *Indications:** Anaerobes, GI sepsis, aspiration pneumonia, Abx assoc colitis, H.pylori, PID, protozoa (Giardia)
  • *MOA:** Nitroimidazoles: bactericidal → inhibitis enzymes thus DNA synthesis
  • *SE’s:** Metallic taste, GI upset, gynaecomastia (metronidazole)
  • *CI’s:** Hepatic impairment
  • *Interactions:** Avoid EtOH → disulfiram-like reaction → inhibitis aldehyde dehydrogenase. Increases warfarin + phenytoin levels
  • *Other:**
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17
Q

Rifampicin

Rifaximin

Rifabutin

A
  • *Indications:** Mycobacteria (TB), legionella, prophylaxis vs. meningitis
  • *MOA:** Rifamycins: bactericidal → inhibits bacterial DNA-dependent RNA polymerase → inhibits RNA synthesis
  • *SE’s:** Orange secretions, hepatitis
  • *CI’s:** Jaundice
  • *Interactions:** P450 inducer
  • *Other:** Rifaximin has very poor oral absorption thus is used in hepatic encephalopathy
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18
Q

Trimethoprim

Sulfamethoxazole

Sulfadiazine

Co-trimoxazole

A

Indications: UTI, PCP, toxoplasmosis
MOA: Folate antagonists: bacteriostatic → inhibits bacterial DNA syntheisis
SE’s: Blood dyscrasias, EM→SJS, EN, nephrotoxic, hepatotoxic
CI’s: Severe renal and liver impairment, pregnancy. Don’t use with methotrexate
Interactions:
Other: Stop immediately if rash or dyscrasias occur

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19
Q

Daptomycin

A
  • *Indications:** MRSA - alternative to linezolid + syndercid
  • *MOA:** Cell membrane toxin → alters membrane causing holes, reducing potential → inhibits protein/DNA/RNA syntheisis → cell death
  • *SE’s:** N+V, abdo pain, diarrhoea etc
  • *CI’s:** Caution in severe hepatic impairment
  • *Interactions:** Ciclosporin, fibrates, statins → increased risk of myopathy
  • *Other:**
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20
Q

Colistin

A
  • *Indications:** Active against Gram -ve → inhaled for CF
  • *MOA:** Cell membrane toxin: bactericidal, acts like a detergent solubilising the bacterial cell wall
  • *SE’s:** Parenteral Rx: neurotoxicity, nephrotoxicity, rash. Inhaled Rx: sore throat/mouth, taste disturbance, N+V etc.
  • *CI’s:** MG
  • *Interactions:** Loop diuretics → increased risk of ototoxicity
  • *Other:**
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21
Q

Ethambutol

A

Indications: Anti TB
MOA: Bacteriostatic → inhibitis mycobacterial cell wall synthesis
SE’s: Optic neuritis, red/green colour blindness, peripheral neuritis
CI’s: Optic neuritis, poor vision
Interactions:
Other: Monitor vision - lose colour vision first

22
Q

Pyrazinamide

A

Indications: Anti TB
MOA: Bactericidal: Prodrug that stops growth of TB
SE’s: Hepatotoxicity → hepatitis, jaundice, N+V etc
CI’s: Acute attack of gout, caution in DM, severe hepatic impairment
Interactions:
Other: Monitor LFTs

23
Q

Isoniazid

A
  • *Indications:** Anti TB
  • *MOA:** Bacteriostatic: Prodrug → inhibits synthesis of mycolic acid which is needed for mycobacterial cell walls
  • *SE’s:** Peripheral neuropathy, N+V, constipation, hepatitis
  • *CI’s:** Drug induced liver disease
  • *Interactions:** Increases levels of CBZ, increased risk of hepatotoxicity with rifampicin
  • *Other:** P450 inhibitor. Increased risk of SE’s if slow acetylator. Give with pyridoxine (vit B6)
24
Q

Fusidate (Fusidic acid)

A
  • *Indications:** Active against staphs: impetigo (topical), blepharitis (topical), osteomyelitis (PO)
  • *MOA:** Bacteriostatic: inhibits protein synthesis
  • *SE’s:** N+V, abdo pain, diarrhoea, hepatitis (in high doses)
  • *CI’s:** Caution in hepatic impairment
  • *Interactions:** Increased risk of myopathy/rhabdo with statins
  • *Other:** Needs 2nd Abx to prevent resistance
25
Q

Chloroquine

A
  • *Indications:** Chemoprophylaxis and Rx of non-falciparum malaria, RA + SLE
  • *MOA:** Kills the parasite by causing a build-up of metabolic products
  • *SE’s:** Visual change - rarely retinopathy, seizures, EM→SJS, GI disturbance
  • *CI’s:** Caution in G6PD deficiency
  • *Interactions:** Increases digoxin levels, increased risk of ventricular arrhythmiasa with amiodarone
  • *Other:**
26
Q

Primaquine

A

Indications: Adjunct in Rx of P.vivax and P.ovale → eradication of liver stages
MOA:
SE’s: N+V, anorexia, abdo pain
CI’s: G6PD deficiency, SLE, RA
Interactions:
Other:

27
Q

Malarone: proguanil + atovaquone

A

Indications: Rx of acute uncomplicated P.falciparum, prophylaxis of P.falciparum, Rx of non-falciparum malaria
MOA:
SE’s: Abdo pain, N+V, diarrhoea etc.
CI’s: Caution in diarrhoea + vomiting, avoid in renal impariment if possible
Interactions:
Other:

28
Q

Mefloquine

A

Indications: Prophylaxis of malaria where there is a high risk of chloroquine-resistant P.falciparum
MOA:
SE’s: N+V, abdo pain, diarrhoea, headache, dizziness, neuropsychiatric signs
CI’s: Hypersensitivity to quinine, Hx of epilepsy or psychosis
Interactions: Increases the risk of arrhythmias with amiodarone, reduces the effects of AED
Other: Avoid if low risk of resistance

29
Q

Riamet: artemether + lumefantrine

A

Indications: Treatment of P.falciparum and non-falciparum malaria
MOA:
SE’s: GI upset, abdo pain, prolonged QTc
CI’s: Hx of arrhythmias, pronlonged QTc, caution in renal or liver disease
Interactions:
Other:

30
Q

Aciclovir

A

Indications: Initial and recurrent labial and genital HSV, herpes meningitis, VZV (shingles), Ramsay Hunt syndrome
MOA: Guanosine analogue, phosophorylated by viral thymidine kinase, di-+tri-phosphorylated by cellular kinase → Aciclovir triphosphate inhibits viral DNA polymerase
SE’s: GI upset, ARF, encephalopathy, myelosuppression
CI’s: Avoid contact with eyes + mucous membranes, caution in renal impairment
Interactions:
Other:

31
Q

Valaciclovir

A

Indications: Genital herpes, herpes meningitis, Herpes zoster, VZV, Ramsay Hunt syndrome
MOA: Aciclovir prodrug → converted to aciclovir by hepatic esterases during 1st pass metabolism, better oral bioavailability
SE’s: GI upset, ARF, encephalopathy, myelosuppression
CI’s: Caution in renal impairment
Interactions:
Other:

32
Q

Famciclovir

A

Indications: Genital herpes, herpes meningitis, herpes zoster, VZV, Ramsay Hunt syndrome
MOA: Prodrug → same MOA as aciclovir
SE’s: GI upset, ARF, encephalopthay, myelosuppression
CI’s: Caution in renal impairment
Interactions:
Other:

33
Q

Ganciclovir

A
  • *Indications:** Life threatening or sight threatening CMV infection - retinitis, pneumonitis, CMV prophylaxis during immunosuppression post transplant
  • *MOA:** 2-dexyguanosine analogue - phosophorylated to dGTD analogue by viral UL97, triphosphate competitively inhibits viral DNA polymerase
  • *SE’s:** BM suppression, CNS toxicity
  • *CI’s:** Hypersensitivity to the ‘clovirs’. Low Hb, neutrophil or platelet count. Avoid in pregnancy
  • *Interactions:** Greatly increased risk of BM suppression with zidovudine
  • *Other:** Given IV only
34
Q

Valganciclovir

A
  • *Indications:** CMV retinitis in AIDS patients, CMV prophylaxis during immunosuppression post transplant
  • *MOA:** Prodrug of ganciclovir, has better oral bioavailability
  • *SE’s:** BM suppression, CNS toxicity
  • *CI’s:** Hypersensitivity to the ‘clovirs’. Low Hb, neutrophil or platelet count.
  • *Interactions:** Greatly increased risk of BM suppression with zidovudine
  • *Other:**
35
Q

Foscarnet

A

Indications: CMV infection
MOA: Binds to pyrophosphate-binding site and inhibitis viral DNA polymerase → doesn’t need viral thymidine kinase
SE’s: Nephrotoxic → avoid in renal transplant, monitor U+Es
CI’s: Renal transplant
Interactions:
Other: IV only

36
Q

Cidofovir

A
  • *Indications:** Resistant CMV infections, CMV retinitis in AIDs patients
  • *MOA:** Inhibits viral DNA polymerase, no activation required
  • *SE’s:** Nephrotoxic
  • *CI’s:** Avoid in renal impairment, pregnancy/lactation
  • *Interactions:** Tenofovir
  • *Other:**
37
Q

NRTI:

Abacavir
Lamivudine
Zidovudine
Tenofovir

A

Indications: HIV infection in combination with other antiretrovirals, Hep B infection → tenofovir
MOA: Nucleoside analogues → nucleoside reverse transcriptase inhibitors except tenofovir which is a nucleotide reverse transcriptase inhibitor (NRTIs)
SE’s: Hepatitis - stop if rising LFTs, lactic acidosis (type B), painful peripheral neuropathy, rash, GI disturbance
CI’s:
Interactions:
Other: Abacavir may cause SJS. Didanosine: pancreatitis, peripheral neuropathy. Lamivudine: well tolerated, 1st line. Zidovudine: myelotoxicity (anaemia, neuropenia). Atripla = tenofovir, etavirenz and emtricitabine

38
Q

NNRTI:

Efavirenz
Nevirapine

A

Indications: HIV infection in combination with other antiretrovirals
MOA: NNRTI → non-competitive inhibition of reverse transcriptase
SE’s: Insomnia, vivid dreams, dizziness, EM→SJS
CI’s: Acute porphyria, avoid in mod-severe hepatic impairment, caution in the elderly, Hx of mental illness or seizures
Interactions:
Other:

39
Q

PI:

Ritonavir
Indinavir
Saquinavir

A
  • *Indications:** HIV infection in combination with other antiretrovirals
  • *MOA:** Protease inhibitors → inhibit viral protease required for virus assembly. Ritonavir is used to boost levels of other PI’s
  • *SE’s:** GI disturbance, anorexia, hepatic dysfunction, pancreatitis etc. Metabolic syndrome, lipodystrophy
  • *CI’s:** Acute porphyria, caution in DM (risk of hyperglycaemia), caution in chronic Hep B or C infection
  • *Interactions:** P450 inhibitors
  • *Other:** Lipodystrophy = fat redistribution → reduced SC fat, increased abdo fat, buffalo hump, insulin resistance, dyslipidaemia
40
Q

Integrase inhibitors:

Raltegravir
Elvitegravir

A

Indications: HIV infection in combination with other antiretrovirals
MOA: Inhibit integration of transcribed viral DNA into host genome
SE’s: GI disturbance, increased TG’s etc.
CI’s:
Interactions:
Other:

41
Q

CCR5 inhibitor:

Maraviroc

A

Indications: CCR5 - tropic HIV infection in combination with other antiretrovirals
MOA: Bind CCR5 (CCR5 inhibitor), preventing interaction with gp120 → inhibits attachment of HIV
SE’s: GI upset, anorexia, insomnia etc., caution in hepatic/renal impairment
CI’s: Caution: cardiovascular disease, chronic hep B or C
Interactions:
Other:

42
Q

Fusion inhibitor:

Enfuvirtide

A

Indications: HIV infection in combination with other antiretrovirals
MOA: Binds gp41 and inhibits fusion
SE’s: Injection site reactions
CI’s: Caution in hepatic impairment
Interactions:
Other:

43
Q

Polyenes:

  • *Amphotericin B**
  • *Nystatin**
A

Indications: Amphotericin B = severe systemic fungal infections e.g. cryptococcal meningitis, pulmonary aspergillosis, systemic candidiasis. Nystatin = candidiasis (cutanrous, vaginal, mucosal, oesophageal)
MOA: Interacts with ergosterol → pore formation. Fungicidal
SE’s: IV = nephrotoxic (Ampho.B) → can get IV reaction after 1-3 hrs = fever, hypotension, N+V. Nystatin is toxic if given IV
CI’s:
Interactions:
Other: Monitor creatinine with IV ampho.B (PO version is non-toxic). Nystatins given PO or topical

44
Q

Imidazoles:

Ketoconazole
Miconazole
Clotrimazole

A

Indications: Ketoconazole = chronic mucocutaneous candidiasis. Miconazole/clotrimazole = dermatophyte infections, mucocutaneous candidiasis
MOA: Fungistatic → blocks ergosterol synthesis by inhibiting 14-alpha-demethylase thus reduces membrane fluidity, inhibits replication, and prevents hyphae formation
SE’s: Ketoconazole = hepatotoxic, reduces androgen synthesis
CI’s:
Interactions:
Other:

45
Q

Triazoles:

Fluconazole
Itraconazole
Voriconazole
Posaconazole

A

Indications: Fluconazole = oral/vag/oesophagus candida (can be used for systemic infections). Itraconazole = aspergillosis, candidiasis, cryptococcosis, blastomycosis, sporotrichosis, histoplasmosis, onychomycosis and chromomycosis. Voriconazole = invasive candida or aspergillus in immuno-compromised, and BMT prophylaxis. Posaconazole = invasive candida, mucor and aspergillus in immuno-compromised
MOA: Fungistatic: blocks ergosterol synthesis by inhibiting 14-alpha-demthylase → reduces membrane fluidity, inhibits replication, prevents hyphae formation
SE’s: Voriconazole = photophobia, rash, hepatotoxic
CI’s:
Interactions:
Other:

46
Q

Allylamines:

Terbinafine

A

Indications: Dermatophyte infections
MOS: Blocks ergosterol synthesis by inhibiting squalene epoxidase causing membrane disruption → fungicidal
SE’s: GI effects, hives, raised LFTs, reversible agrannulocytosis
CI’s:
Interactions:
Others:

47
Q

Echinocandins:

Caspofungin

A
  • *Indications:** Invasive aspergillosis or candidiasis
  • *MOA:** Inhibit beta-glucan synthesis. Fungicidal vs yeasts, fungistatic vs moulds
  • *SE’s:** Very low toxicity, GI upset, hypersensitivity
  • *CI’s:** Avoid in pregnancy/lactation
  • *Interactions:**
  • *Other:** IV only
48
Q

Flucytosine

A
  • *Interactions:** Systemic yeast and fungal infections, adjunct to amphotericin in crytococcal meningitis
  • *MOA:** Inhibits DNA/RNA synthesis
  • *SE’s:** Bone marrow suppression, derranged LFTs, GI upset
  • *CI’s:** Caution in elderly, blood disorders → need FBC, LFTs, U+Es
  • *Interactions:**
  • *Other:**
49
Q

Griseofulvin

A

Indications: Dermatophyte infections of skin, hair and nails
MOA: disrupts spindle formation in mitosis
SE’s:
CI’s:
Interactions:
Other:Very slow acting, only used orally.

50
Q

Oseltamivir

A

Indications: Influenza A + B - must be started within 48hrs of symptoms
MOA: Neuraminidase inhibitor
SE’s: N+V, abdo pain, headache
CI’s:
Interactions:
Other:Must be >1yr old

51
Q

Zanamivir

A

Indications: Influenza A+B - must be started within 48hrs of symptoms
MOA: Inhaled neuraminidase inhibitor
SE’s: rash
CI’s:
Interactions:
Other:Must be > 5yrs

Final Year MBBS (39 decks)

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