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Pharmacology > Block 9 > Flashcards

Flashcards in Block 9 Deck (47):
1

Paracetamol
Use
Actions
MOA

Use: when NSAIDs cannot be used e.g. peptic ulcer
Action: analgesia + antipyretic
MOA: COX + COX 3 inhibitor (analgesia) hypothalamus -> vasodilation + sweating (antipyretic)

2

Amoxicillin
Class
Gram +ve/-ve
MOA

Beta-lactam antibiotic
Inhibits bacterial cell wall synthesis
Mostly gram +ve some gram -ve

3

Clauvulanic acid
MOA
Use

B-lactamase inhibitor
Combined w/ amoxicillin - overcome antibiotic resistance

4

Methicillin
Class
Gram +ve/-ve
MOA
Resistance?

Narrow spectrum beta lactam antibiotic
Gram +ve
Transpeptidase inhibitor - Inhibits bacterial cell wall synthesis
MRSA

5

Cefuroxime
Class
Gram +ve/-ve
MOA
Considerations

Cephalosporin antibiotic
Gram +ve and Gram -ve
Transpeptidase inhibitor - Inhibits bacterial cell wall synthesis
Crosses blood-brain barrier

6

Benzylpenicillin
Class
Gram +ve/-ve
MOA
Resistance?

Beta lactam antibiotic
Mostly gram +ve some gram -ve
Transpeptidase inhibitor
V. stable against beta lactamases

7

Oxytetracycline
Class
Use
Gram +ve/-ve
MOA

Broad spectrum antibiotic
Acne
Gram +ve and Gram -ve
30s inhibitor - inhibits translation

8

Erthromycin
Class
Use
MOA
Considerations

Macrolide antibiotic
Resp inf., syphillis, skin inf., chronic prostatitis,
50s inhibitor - inhibits protein synth
Pregnancy - breast milk + crosses placenta

9

Gentamycin
Class
Gram +ve/-ve
Use
MOA
Considerations

Broad spectrum aminoglycoside
Mostly gram -ve: pseudomonas, acinetobacter, enterobacter
Some gram +ve
TB
30s/50s inhibitor - inhibits protein synthesis
Ear + Kidney damage

10

Rifampacin
Class
Use
Gram +ve/-ve
MOA

Broad spectrum antibiotic
TB
Gram +ve and Gram -ve
Inhibits RNA polymerase

11

Trimethoprim
Class
Use
Gram +ve/-ve
MOA

antibacterial - folate antagonist
UTIs + bronchitis
Gram +ve and Gram -ve
Inhibits dihydrofolate reductase

12

Sulfamethoxazole
Class
Use
Gram +ve/-ve
MOA

sulfonamide bacteriostatic antibiotic
UTIs, bronchitis, chronic prostatitis, lysteria monocytogenes
Gram +ve and Gram -ve
Dihydrofolate synthesase inhibitor - folate antagonist

13

Vancomycin
Class
Use
Gram +ve/-ve
MOA

Glycopeptide antibiotic
"Drug of last resort" - Listeria, penicillin res. strep. pn. , strep p. , strep a., actinomyces, lactobacillus sp.,
Gram +ve only
Peptidoglycan inhibitor, also incr. memb. permeability + inhibits RNA synthesis

14

Colistin
Class
Use
Gram +ve/-ve
MOA

Phospholipid detergent - polymixin antibiotic agent
Multi-drug resistant gram -ve bacteria, v effective against pseudamonas aeruginosa
Incr. bact. memb. permeability + precipitates ribosomes

15

Ciprofloxacin
Class
Use
Gram +ve/-ve
MOA

Fluoroquinolone antibiotic
Bacterial infections resistant to other antibiotics
Gram +ve and Gram -ve
Topoisomerase II and IV inhibitor - inhibits DNA replication + transcription

16

Fusidic acid
Class
Gram +ve/-ve
MOA

Bacteriostatic antibiotic
Gram +ve only
Translocation inhibitor (elongation factor g) - therefore inhibiting protein synthesis

17

Ibuprofen
Class
Action
MOA

NSAID
Analgesia
Antipyretic
COX-2 inhibition - reduces prod. of prostaglandins
Antipyretic effects - works on hypothalamus (vasodilation)

18

Aspirin
Class
Action
MOA

NSAID
Analgesia
Antipyretic
Antiplatelet
COX-1 and COX-2 inhibitor (non-selective) - reduces prod of prostaglandins
Platelets - irreversible binding to COX stops prod. of thromboxane A2, effects last 7 to 10 days (lifetime of platelets)

19

Acyclovir
Class
Use
Action
MOA

Antiviral
Herpes simples
Immunocompromised: varicella zoster and herpes zoster
Inhibits HSV specific DNA polymerases
Nucleoside analogue - converted by viral thymidine kinase

20

Amantadine
Class
Use
MOA

Antiviral + Antiparkinsonian
Parkinsons, post-herpetic neuralgia, Infl. A (not reccomended)
Inhibits viral M2 ion channel - required for viral "uncoating"

21

Amprenavir (pro-drug: fosamprenavir)
Class
Use
MOA
Side effects

Antiretroviral
HIV
Protease inhibitor - inhibits HIV-1 protease -> formation of immature virus particles
Hepatic dysfunction

22

Aspirin
Class
Action
Use
MOA
Side effects

NSAID
Analgesic
Antipyretic
Anti-inflammatory
Antiplatelet
MI, TIA, Stroke, AF, CVD
Irreversibly inhibits COX -> prostaglandins (inc IL-1 mediated realese in hypothalamus)
Antiplatelet - prevents thromboxane A2 synthesis
GI ulcers, haemorrhage, tinnitus

23

Diamorphine
Class
Use
MOA
Side effects

Opioid
Acute/chronic pain
Prodrug -> morphine, binds mu opioid receptors -> analgesia
Cardiorespiratory depression, constipation

24

Ibuprofen
Class
Use/action
MOA
Side effects

NSAID
Analgesic, anti-inflammatory, anti-pyretic
Irreversible COX binding, mainly COX-2 -> decr. prostaglandin prod.
GI ulcer, worsens asthma, cardiovascular events

25

Naproxen
Class
Use/action
MOA
Side effects

NSAID
Analgesic, anti-inflammatory, anti-pyretic
Irreversible COX binding, mainly COX-2 -> decr. prostaglandin prod.
GI ulcer, worsens asthma, cardiovascular events

26

Phenoxymethylpenicillin (Pen V)
Class
Use
Gram +ve/-ve
MOA

Beta-lactam antibiotic
Oral inf., tonsillitis, Otitis media
Mostly gram+ve, narrow spectrum
Pen V = oral form of penicillin, binds PBPs to inhibit cell wall synthesis

27

Zidovudine
Class
Use
MOA

Antiretroviral (NRTI)
HIV
Prodrug -> zidovudine triphosphate, a thymidine analogue -> inhibits HIV-1 RT

28

Amphotericin
Class
Use
MOA

Antifungal
Systemic fungal inf., Aspergilosis, Leishmaniasis
Binds ergosterol -> formation of pores in cell wall

29

Artmether
Class
Use
MOA
Side effects

Antimalarial
Malaria
Unknown - inhibition of anti-oxidant + metabolic enzymes -> reduced growth of parasite
QT prolongation

30

Clotrimazole
Class
Use
MOA

Antifungal
Fungal otitis media + skin inf.
Vaginal + vulvar candidiasis
Inhibits 14-a demthylase which converts lanosterol -> ergosterol, pore formation

31

Fluconazole
Class
Use
MOA

Antifungal
Candida balanitis
Vulvovaginal candidiasis
Inhibits 14-a demthylase which converts lanosterol -> ergosterol, pore formation

32

Nystatin
Class
Use
MOA

Antifungal
Oral candidiasis
Binds ergosterol, pore formation

33

Pyrimethamine
Class
Use
MOA

Antimalarial/folate antagonist
Toxoplasmosis in preg., Malaria
Inhibits dihydrofolate reductase -> reduces tetrahydrofolic acid prod. -> Inhibits DNA and RNA synthesis

34

Quinine
Class
Use
MOA

Antimalarial
Choloroquine resistant plasmodium falciparum malaria
Inhibits haem polymerase - parasite can no longer digest haemoglobin -> starves
QT prolongation

35

Clobetasone
Class
Use
MOA

Moderate glucocorticoid
Eczema
Anti-inflammatory - prevents expression of cox-1 and cox-2 and prod. of eicosanoids

36

Griseofulvin
Class
Use
MOA

Fungal mitosis inhibitor
Dermatophyte infections
Inhibits fungal cell mitosis + nucleic acid synth.
Binds alpha/beta tubulin to inhibit spindle + microtubule function

37

5-fluorouracil
Class
Use
MOA

Pyrimidine analogue
GIT + breast tumours (malignant)
Skin lesions (malignant + pre-malignant)

38

Cyclophosphamide
Class
Use
MOA

Alkylating agent
Severe RA
Leukaemias + lymphomas
Active metabolite = aldo phosphamide
Binds to DNA bases causing damage and preventing transcription

39

Dacarbazine
Class
Use
MOA

Alkylating agent
Melanoma, Sarcoma, Hodgkin's disease
Unknown - possibly a purine analogue, possibly binds DNA like normal alkylating agents

40

Doxorubicin
Class
Use
MOA

Anticancer - topoisomerase II inhibitor
Leukaemia, Lymphomas, Solid tumours (e.g. breast cancer), Sarcoma, Bladder tumours
Antibiotic w/ antimitotic and cytotoxic properties. Inhibits topoisomerase II -> stops DNA from unwinding

41

Etoposide
Class
Use
MOA

Anticancer
Small cell carcinoma, lymphomas, testicular cancer
Topoismerase II inhibitor - cancers depend more heavily on this enzyme, inhibition leads to DNA breakages

42

Imatinib
Class
Use
MOA
Considerations

Tyrosine kinase inhibitor
leukaemias, GI tumours, dermatofibrosarcoma protuberans
In CML, the philadelphia chromosome forms a mutated kinase called Bcr-ABL
Hep B reactivation

43

Paclitaxel
Class
Use
MOA

Anticancer (taxane)
Ovarian + breast cancer
NSCLC
Kaposi's sarcoma
Pancreatic adenocarcinoma
Binds tubulin and induces apoptosis through bcl-2 binding

44

Rituximab
Class
Use
MOA
Considerations

Anti-CD20 monoclonal antibody
RA patients (where DMARDs = ineffective)
Lymphomas + leukaemias
Binds CD20 receptor on B cells inducing cell lysis
Cardiac events

45

Tamoxifen
Class
Use
MOA
Considerations

SERM
ER positive breast cancer
Gynaecomastia
Anovulatory infertility
Conformational changes to the ER inhibiting oestrogen induced proliferation. Has oestrogenic and anti-oestrogenic effects
Endometrial changes: hyperplasia, polyps, cancer
Thromboembolism risk

46

Tretinoin
Class
Use
MOA
Considerations

Vitamin A analogue
Acute promyelocytic leukaemia
Binds to Retinoic acid receptors (RaRs). RaRa and RaRb linked with acute promyelocytic leukaemia
Retinoic acid syndrome

47

Vinblastine
Class
Use
MOA
Considerations

Vinca alkaloid
Leukaemias
Lymphomas
Inhibits metaphase -> causes crystallisation of microtubules at mitotic spindle -> cell cycle arrest or apoptosis
Neurotoxicity